Chalcogen Bonded Directly To A Ring Carbon Of The Six-membered Hetero Ring Patents (Class 514/335)
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Patent number: 5407948Abstract: Substituted mono- and bipyridylmethylpyridones are prepared either by reaction of pyridones with mono- or bipyridylmethylhalogen compounds or by reaction of pyridone-substituted halogenopyridines with tetrazolylphenylboronic acids. The substituted mono- and bipyridylmethylpyridones can be employed as active compounds in medicaments, in particular for the treatment of arterial hypertension and atherosclerosis.Type: GrantFiled: May 6, 1994Date of Patent: April 18, 1995Assignee: Bayer AktiengesellschaftInventors: Peter Fey, Walter Hubsch, Jurgen Dressel, Rudolf Hanko, Thomas Kramer, Ulrich Muller, Matthias Muller-Gliemann, Martin Beuck, Hilmar Bischoff, Stefan Wohlfeil, Dirk Denzer, Stanislav Kazda, Johannes-Peter Stasch, Andreas Knorr, Siegfried Zaiss
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Patent number: 5395854Abstract: Ortho-substituted phenyl-acetamides I ##STR1## (R.sup.1 =H, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkynyl, alkoxyalkyl, alkoxycarbonyl, phenyl, phenylalkyl, phenylalkenyl or phenoxyalkyl, 5- or 6-membered heterocycle with 1-3 hetero atoms to which a benzene ring or a 5- or 6-membered heterocycle can be fused; R.sup.2 and R.sup.3 =H, CN, halogen, alkyl, alkoxy; R.sub.4 and R.sup.5 =H, alkyl and R.sup.4 or R.sup.5 =alkoxy; Y=O, S, SO, SO.sub.2, N=N, O--CO, CO--O, CO--O--CH.sub.2, alkylene or haloalkylene, alkenylene, alkynylene, oxy- alkylene, thio-alkylene, alkyleneoxy, carbonylalkylene or alkylenecarbonyl, W=alkoxyimino, alkoxymethylene or alkylthiomethylene), excepting compounds where R.sup.1 is hydrogen, phenyl or 2,2-dimethyl-3-(2,2-dichlorovinyl)cyclopropyl, R.sup.2 to R.sup.5 are each hydrogen, Y is carbonyloxymethylene and W is methoxymethylene or methylthiomethylene, are suitable as fungicides and for controlling pests.Type: GrantFiled: September 22, 1993Date of Patent: March 7, 1995Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Eberhard Ammermann, Gisela Lorenz, Hubert Sauter, Klaus Oberdorf, Uwe Kardorff, Christoph Kuenast
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Patent number: 5364873Abstract: The invention relates to pyridine-2,4- and -2,5-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2 and X have the meanings given, a process for the preparation of these compounds and their use, in particular in medicaments for influencing the metabolism of collagen and collagen-like substances or the biosynthesis of C1.sub.q.Type: GrantFiled: April 1, 1993Date of Patent: November 15, 1994Assignee: Hoechst AktiengesellschaftInventors: Martin Bickel, Dietrich Brocks, Harald Burghard, Volkmar Gunzier, Stephan Henke
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Patent number: 5364853Abstract: Thioformamide compounds of formula (I) are disclosed in which R is alkyl, Y is methylene, ethylene or a direct bond, A is optionally substituted phenyl or pyridyl, R.sup.1 is hydrogen and R.sup.2 is N-alkylsulphonyl-, N-phenylsulphonyl-N'-alkylamidino or an arylsulphonyl group; R.sup.1 and R.sup.2 may both independently represent alkyl- or arylsulphonyl groups.Type: GrantFiled: August 20, 1992Date of Patent: November 15, 1994Assignee: Rhone-Poulenc Rorer LimitedInventors: Malcolm N. Palfreyman, Nigel Vicker
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Patent number: 5360808Abstract: Arylcarbonylaminoalkyl-dihydro-oxo-pyridines of Formula I ##STR1## are disclosed wherein aryl is an aromatic or heteroaromatic system, n is zero through 5; R and R(1), are hydrogen, or loweralkyl; W is hydrogen, (hetero)-(aryl)-loweralkyl; Z is hydrogen, CH.sub.2 OR(2.sub.), CHO, (CO)OR(2), (CO)NR(2).sub.2.Processes for the preparation of compound I are also disclosed.Compounds I are suitable for the treatment of disorders of the cardiovascular system, for example of hypertension, of cardiac insufficiency or of disturbances of blood flow in the coronary systems such as, for example, angina. Disturbances of cerebral and peripheral blood flow are likewise influenced beneficially. Furthermore, compounds I are able to influence smooth-muscle organs such as uterus, bronchi, intestines and biliary system, the urinary tract (ureter, bladder and urethra) in the sense of spasmolysis.Type: GrantFiled: February 18, 1993Date of Patent: November 1, 1994Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, David Wettlaufer, Erik Klaus
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Patent number: 5356909Abstract: The invention relates to substituted pyridine-2,4-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The invention also relates to a process for the preparation of the abovementioned compounds and to their use as medicaments, in particular as fibrosuppressants and immunosuppressants.Type: GrantFiled: June 25, 1992Date of Patent: October 18, 1994Assignee: Hoechst AktiengesellschaftInventors: Ekkehard Baader, Martin Bickel, Dietrich Brocks, Volkmar Gunzler, Stephan Henke, Hartmut Hanauske-Abel
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Patent number: 5354739Abstract: Highly concentrated emulsifiable concentrates of neophanes and azaneophanes for use in plant protectionHighly concentrated emulsifiable concentrates of compounds of the general formula I ##STR1## in which A, B=independently of one another CH, CR.sub.4 or N,X=CH.sub.2, O or S,Y=CH or N,Z=H or F,R.sub.1 and R.sub.4 =independently of one another H, halogen, (C.sub.1 -C.sub.3)-alkyl, (C.sub.1 -C.sub.3)-halogenoalkyl, (C.sub.1 -C.sub.3)-alkoxy, (C.sub.1 -C.sub.3)-halogenoalkoxy, (C.sub.1 -C.sub.4)-alkylthio or (C.sub.1 -C.sub.4)-halogenoalkylthio, or R.sub.1 and R.sub.4 together=--CH.sub.2 --O--CH.sub.2 --;R.sub.2 =H, (C.sub.1 -C.sub.3)-alkyl, ethynyl, vinyl, halogen or cyano,R.sub.3 =H, halogen, (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.3)-alkoxy andM=C or Si, which contain a combination of an anionic and a nonionic emulsifier with a (C.sub.2 -C.sub.16)-alkanol.also have, in addition to a very good spontaneous emulsiliability, a very high emulsion stability.Type: GrantFiled: October 5, 1992Date of Patent: October 11, 1994Assignee: Hoechst AktiengesellschaftInventor: Hans Rochling
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Patent number: 5342848Abstract: Thioformamide derivatives of formula (I): ##STR1## wherein R represents alkyl; A represents optionally substituted pyrid-4-yl; Y represents ethylene or methylene or a direct bond and X represents an optionally substituted phenyl, pyridyl, furyl or thienyl group or optionally substituted alkyl, alkenyl or cycloalkyl, and salts thereof possessing useful pharmacological properties.Type: GrantFiled: August 7, 1992Date of Patent: August 30, 1994Assignee: Rhone-Poulenc Rorer LimitedInventors: Terance W. Hart, Bernard Y. J. Vacher
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Patent number: 5334614Abstract: The invention concerns hydroxylamine derivatives of the formula I ##STR1## wherein R.sup.4 is hydrogen, carbamoyl, (1-4C)alkyl, cyclopentyl, cyclohexyl, tetrahydrofuran-3-yl, tetrahydropyran-4-yl, piperidin-4-yl, N-(1-4C)alkylpiperidin-4-yl, (2-5C)alkanoyl, (1-4C)alkylsulphonyl, N-(1-4C)alkylcarbamoyl, N,N-di-(1-4C)alkylcarbamoyl, phenyl, phenyl-(1-4C)alkyl, di-phenyl-(1-4C)alkyl, benzoyl, phenylsulphonyl or a heteroarylmethyl group;R.sup.5 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, cyano-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl;A.sup.4 is (1-4C)alkylene;Ar.sup.1 is phenylene, pyridinediyl or pyrimidinediyl;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl or thiazolediyl;R.sup.1 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 -wherein each of A.sup.2 and A.sup.Type: GrantFiled: May 11, 1993Date of Patent: August 2, 1994Assignees: Zeneca Ltd., Zeneca Pharma SAInventors: Philip N. Edwards, Michael S. Large
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Patent number: 5332757Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 - which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.Type: GrantFiled: February 8, 1993Date of Patent: July 26, 1994Assignees: Zeneca Limited, Zeneca PHARMA S AInventors: Thomas G. C. Bird, Patrick Ple
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Patent number: 5322845Abstract: An acrylic acid compound useful for fungicides is provided. The compound has the following formula (I) ##STR1## wherein X represents a phenyl group which may be substituted, or a methylene group, n represents 0 or 1, Y represents an oxygen atom or a sulfur atom, Z represents a phenyl group, an aralkyl group, an aromatic heterocyclyl group or an aromatic heterocyclylmethylene group and Z may be substituted.Type: GrantFiled: October 1, 1992Date of Patent: June 21, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Tsuguhiro Katoh, Atsuo Mizuguchi, Hirotaka Takano
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Patent number: 5292758Abstract: Sulfonamide derivatives of the general formula (I): ##STR1## wherein preferably R.sup.1 represents a lower alkoxy group, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different from one another and each represent a hydrogen atom, halogen atom or lower alkyl group, A and B may be the same or different from each other and each represent .dbd.N-- or .dbd.CH--, E represents an aromatic 6-membered cyclic group, which may have 1 or 2 nitrogen atoms in the ring, and be substituted with 1 to 3 substituents which may be the same or different from one another with the proviso that a combination of R.sup.1 which is a hydrogen atom, lower alkyl group, nitro group or amino group which may be protected, R.sup.2 and R.sup.3 which are each a hydrogen atom, A and B which are each .dbd.Type: GrantFiled: July 31, 1992Date of Patent: March 8, 1994Assignee: Eisai Co., Ltd.Inventors: Hiroshi Yoshino, Norihiro Ueda, Hiroyuki Sugumi, Jun Niijima, Yoshihiko Kotake, Toshimi Okada, Nozomu Koyanagi, Tatsuo Watanabe, Makoto Asada, Kentaro Yoshimatsu, Atsumi Iijima, Takeshi Nagasu, Kappei Tsukahara, Kyosuke Kitoh
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Patent number: 5254543Abstract: Sulphonylbenzyl-substituted pyridones can be prepared by reacting pyridones with sulphonylbenzyl compounds. The sulphonylbenzyl-substituted pyridones can be employed as active compounds in medicaments, in particular for the treatment of arterial hypertension and atherosclerosis.Type: GrantFiled: February 18, 1993Date of Patent: October 19, 1993Assignee: Bayer AktiengesellschaftInventors: Rudolf Hanko, Walter Hubsch, Jurgen Dressel, Peter Fey, Thomas Kramer, Ulrich Muller, Matthias Muller-Gliemann, Martin Beuck, Stanislav Kazda, Claudia Hirth-Dietrich, Andreas Knorr, Johannes-Peter Stasch, Stefan Wohlfeil, Ozkan Yalkinoglu
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Patent number: 5204357Abstract: The invention relates to compounds of the formula I ##STR1## in which A represents a substituted thio-, sulfinyl- or sulfonyl-alkanoyl radical or a four- to eleven-membered heterocycle, B is an amino acid residue, R.sup.1 denotes hydrogen (substituted) alkyl, (substituted)cycloalkyl or aryl, R.sup.2 represents hydrogen, (substituted)alkyl or aryl, R.sup.3 denotes a radical of the formula --(CH.sub.2).sub.q --(X).sub.r --(CH.sub.2).sub.s --R.sup.6 with X denoting CF.sub.2, CO or CHR.sup.8, R.sup.6 denoting a (substituted)heteroaromatic, R.sup.8 denoting alkyl, alkoxy, alkylthio, alkylamino, hydroxyl, azide or halogen, q and s denoting 1 to 4, and r denoting 0 or 1, and R.sup.9 is hydrogen, (substituted)alkyl, alkanoyl, cycloalkanoyl, (substituted) aroyl or (substituted)aryl, and to the salts thereof. In addition, processes for the preparation of these compounds, and the use thereof as renin inhibitors are described.Type: GrantFiled: February 14, 1989Date of Patent: April 20, 1993Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
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Patent number: 5198444Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.Type: GrantFiled: October 15, 1990Date of Patent: March 30, 1993Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
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Patent number: 5185342Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.Type: GrantFiled: May 16, 1990Date of Patent: February 9, 1993Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
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Patent number: 5185348Abstract: The compounds according to the invention can be prepared by reaction of the corresponding amines with sulphonic acid derivatives, or in the case of the aminooxy compounds by reacton of ketones with aminooxy compounds or alkylation of hydroxylamines, or in the case of the alkene compounds by reaction of ketones with phosphorusylides. The phenylsulphonamide substituted pyridinealkene- and -aminooxyalkencarboxylic acid derivatives can be used for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, allergies and asthma.Type: GrantFiled: May 21, 1992Date of Patent: February 9, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich Niewohner, Ulrich E. Muller, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
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Patent number: 5177089Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.Type: GrantFiled: July 25, 1990Date of Patent: January 5, 1993Assignee: Eisai Co., Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
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Patent number: 5158962Abstract: Fungicidal substituted amino acid amides of the formula ##STR1## in which Ar and Ar' are identical or different and represent unsubstituted or substituted aryl, unsubstituted or substituted aralkyl, unsubstituted or substituted heteroaryl and unsubstituted or substituted heteroarylalkyl, andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are identical or different and represent hydrogen or alkyl orR.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a cycloalkyl ring.Type: GrantFiled: October 2, 1990Date of Patent: October 27, 1992Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Detlef Wollweber, Wilhelm Brandes
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Patent number: 5158954Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.Type: GrantFiled: October 15, 1990Date of Patent: October 27, 1992Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
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Patent number: 5153199Abstract: Compounds having the general formula (I): ##STR1## and optical isomers thereof, wherein X is oxygen or sulphur; R.sup.1 is halogen, C.sub.1-4 alkoxy or C.sub.1-4 haloalkoxy; R.sup.2 and R.sup.3, which are the same or different, are hydrogen, --CO.sub.2 R.sup.5 or C.sub.1-4 alkyl; R.sup.4 is hydrogen, cyano, C.sub.1-4 alkyl (optionally substituted with cyano or halogen), --(CH.sub.2).sub.n CO.sub.2 R.sup.6, --CONR.sup.6 R.sup.7, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, optionally substituted phenyl or optionally substituted heteroaromatic; or the group CR.sup.2 R.sup.3 R.sup.4 can form an allene moiety optionally substituted with C.sub.1-4 alkyl; R.sup.5, R.sup.6 and R.sup.7, which are the same or different, are hydrogen or C.sub.1-4 alkyl; n is 0, 1, 2, 3 or 4; and metal complexes thereof are active as fungicides.Type: GrantFiled: December 19, 1990Date of Patent: October 6, 1992Assignee: Imperial Chemical Industries PLCInventors: Don R. Baker, Patrick J. Crowley, Paul A. Worthington, Ian R. Matthews
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Patent number: 5126358Abstract: The invention relates to novel isonicotinoylpyridinyl hydrazine derivatives of formula I ##STR1## wherein Hal is halogen,R.sub.1 is hydrogen, methyl or --COR.sub.5,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl, or a radical selected from --COR.sub.5 and --CO--Z--R.sub.6,R.sub.3 is hydrogen, halogen, trifluoromethyl, trichloromethyl, --COOH, --COOCH.sub.3, --OH or nitro.R.sub.4 is hydrogen, halogen, methoxy or methyl,R.sub.5,R.sub.6, Z are as defined hereinafter.with the exception of 1-(pyridin-2'-yl)-2-(2,6-dichloroisonicotinoyl) hydrazine.The novel compounds have plant-protective properties and are especially suitable for protecting plants from attack by phytopathogenic microorganisms such as fungi, bacteria and viruses.Type: GrantFiled: December 21, 1990Date of Patent: June 30, 1992Assignee: Ciba-Geigy CorporationInventor: Walter Kunz
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Patent number: 5112386Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur, A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 --S(O).sub.n R.sup.3 groups; any two of the groups, A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.Type: GrantFiled: December 30, 1988Date of Patent: May 12, 1992Assignee: Imperial Chemical Industries PLCInventors: Anthony Vivienne, John M. Clough, Paul deFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
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Patent number: 5100892Abstract: Compounds of the following formula (I): ##STR1## where R.sup.1 and R.sup.2 are alkyl or cycloalkyl, which may be substituted, R.sup.4 is aryl such as phenyl which may be substituted, L is a direct bond or an oxygen containing linking group, R is a hydrogen, alkyloxy, alkyl, halogen or haloalkyl and Het is a pyridinyl or pyridazinyl group. The compounds can be used antihypertensives or myocardial relaxants. Also part of the invention are pharmaceutical compositions, intermediates and methods of synthesis.Type: GrantFiled: November 13, 1990Date of Patent: March 31, 1992Assignee: Glaxo Inc.Inventors: Thomas N. Wheeler, Terrence P. Kenakin
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Patent number: 5075324Abstract: 1,4-dihydropyridines of formula I ##STR1## wherein X is --CO.sub.2 R.sub.1, cyano, nitro, --COCH.sub.3 ; each of R and R.sub.1, which are the same or different, is a primary, secondary or tertiary, saturated or unsaturated, linear or branched C.sub.1 -C.sub.6 alkyl group optionally substituted by one or more hydroxy, C.sub.1 -C.sub.7 -monoalkylamino, di-C.sub.1 -C.sub.7 -alkylamino, benzylamino, C.sub.1 -C.sub.6 -alkoxy, phenoxy groups which are optionally substituted; R.sub.2 is hydrogen; R.sub.3 is hydrogen or hydroxy, --OCOR.sub.5, OSO.sub.2 R.sub.6, azide, amino, --NHPO(OR.sub.7).sub.2, --NHCOR.sub.5, C.sub.1 -C.sub.4 -alkoxy or fluorine, chlorine, bromine or iodine, SH, SCOR.sub.6 or C.sub.1 -C.sub.6 -alkylthio, phenylthio or benzylthio; R.sub.4 is an optionally substituted aromatic or an optionally substituted 5- or 6-membered heteroaromatic group; Y is one or more substituents, which may be the same or different, selected from C.sub.1 -C.sub.4 -alkoxy, halogen, nitro, cyano, C.sub.1 -C.sub.Type: GrantFiled: June 22, 1989Date of Patent: December 24, 1991Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Marco Frigerio, Andrea Zaliani, Carmelo A. Gandolfi, Mauro Germini, Odoardo Tofanetti, Sergio Tognella
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Patent number: 5071860Abstract: Insecticidally active substituted heteroaryl phenyl ethers of the formula ##STR1## in which Het represents an optionally substituted heteroaromatic radical,X represents O, S, --CH.sub.2 --, --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.sub.2 --O--, ##STR2## Y represents O, --O--CH.sub.2 -- or S, Z represents an optionally substituted aromatic or heteroaromatic radical;m represents integers from 1-4n represents 0, 1, 2, 3, 4O represents 0, 1, 2, 3, 4, provided than n and o do not simultaneously represent 0p represents integers from 1-4,R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently of one another represent hydrogen, C.sub.1 -C.sub.6 -alkyl which is optionally substituted; two radicals adjacent to one another can also, together with the C atoms to which they are bonded, form a saturated carbocyclic 5- or 6-ring,R.sup.1 represents identical or different radicals hydrogen, halogen, CN, C.sub.1-4 -alkyl, 1-5-halogeno-C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, 1-5-halogeno-C.sub.Type: GrantFiled: March 7, 1990Date of Patent: December 10, 1991Assignee: Bayer AktiengesellschaftInventors: Bernd Alig, Wilhelm Stendel, Michael Londershausen
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Patent number: 5055471Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.Type: GrantFiled: November 15, 1989Date of Patent: October 8, 1991Assignee: Imperial Chemical Industries PLCInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5047414Abstract: Compounds of formula I, and pharmaceutical compositions containing compounds of formula I ##STR1## wherein: R.sub.1 is:(a) COCH.sub.3, COC.sub.6 H.sub.5, CN or NO.sub.2 ;(b) COORa wherein Ra is hydrogen, or optionally substituted C.sub.1 -C.sub.6 straight or branched alkyl;R.sub.2 is optionally substituted phenyl; pentafluorophenyl; .alpha.- or .beta.-naphthyl; a five- or six-membered heterocyclic ring; .alpha.-benzo[2,3-b]-1,4-dioxan-.alpha.-yl; or .alpha.-benzofuroxanyl;R.sub.3 is COORa;P is hydrogen, --(CH.sub.2).sub.p --W, or C.sub.1 -C.sub.8 linear or branched alkyl;N--P.sub.1 is the residue of a primary or secondary amino group wherein P.sub.1 is hydrogen, C.sub.1 -C.sub.6 lower linear or branched alkyl group, or --(CH.sub.2).sub.p --W; and P, taken together with P.sub.1 and the nitrogen atom to which P.sub.1 is linked, may form a pyrrolidine or a piperidine ring; W is hydroxymethyl, formyloxymethyl, CO.sub.2 R wherein R is hydrogen or C.sub.1 -C.sub.Type: GrantFiled: December 21, 1990Date of Patent: September 10, 1991Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Carmelo A. Gandolfi, Marco Frigerio, Silvano Spinelli, Odoardo Tofanetti, Sergio Tognella
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Patent number: 5028617Abstract: A compound for promoting livestock production and for controlling obesity in humans and animals, of the formula ##STR1## in which A represents .dbd.CH-- or .dbd.N--,R.sup.0 represents hydrogen or methyl,R.sup.1 and R.sup.3 each independently represents hydrogen, hydroxyl, halogen, cyano, alkyl, halogenoalkyl, hydroxyalkyl, alkoxycarbonyl, aminocarbonyl, mono- and dialkylaminocarbonyl, alkoxy, halogenoalkoxy, halogenoalkylthio, NHSO.sub.2 -alkyl,R.sup.2 represents hydrogen, hydroxyl, alkoxy or the radical --NR.sup.5 R.sup.6,R.sup.4 represents hydrogen, C.sub.1 -C.sub.10 -alkyl which is optionally substituted by hydroxyl, halogen, alkoxy, acyloxy or the radical --NH.sup.7 R.sup.8, or represents the radical COR.sup.9 or the radical --O--Z--R.sup.10,Z represents C.sub.1 -C.sub.10 -alkylene, -alkenylene or alkynylene,R.sup.5 represents hydrogen or alkyl,R.sup.6 represents hydrogen, alkyl, halogenoalkyl or acyl, or R.sup.5 and R.sup.Type: GrantFiled: January 19, 1990Date of Patent: July 2, 1991Assignee: Bayer AktiengesellschaftInventors: Hans Lindel, Werner Hallenbach, Friedrich Berschauer, Heinrich A. Greife, Gernot Klotz
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Patent number: 5008276Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.Type: GrantFiled: October 17, 1988Date of Patent: April 16, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
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Patent number: 5002957Abstract: Azaneophyl and silazaneophyl sulfides, processes for their preparation, agents containing them, and their use as pesticides.Compounds of the formula I, their optical isomers and mixtures thereof ##STR1## where M denotes C or Si,R.sup.1 denotes unsubstituted or substituted pyridyl, unsubstituted or substituted pyrimidyl, andwhen M=C- denotes unsubstituted or substituted pyridazinyl, unsubstituted or substituted pyrazinyl, unsubstituted or substituted 1,2,4-triazinyl, unsubstituted or substituted 1,2,4,5-tetrazinyl,R.sup.2, R.sup.3 independently or one another denote alkyl, alkenyl, haloalkyl, phenyl, or R.sup.2 and R.sup.3 denote an alkylene chain which - together with the quaternary central atom (M) - form an unsubstituted or fluorine-substituted ring having four to six ring members (when M=Si) or having three to six ring members (when M=C),R.sup.4 denotes H, F, --CN, --CCl.sub.3, --C.dbd.CH, (C.sub.1 -C.sub.4)alkyl, ##STR2## R.sup.Type: GrantFiled: March 23, 1989Date of Patent: March 26, 1991Assignee: Hoechst AktiengesellschaftInventors: Hans H. Schubert, Gerhard Salbeck, Hans-Peter Krause, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5001137Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.Type: GrantFiled: September 14, 1989Date of Patent: March 19, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
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Patent number: 4997834Abstract: A trans-4-amino(alkyl)-1-pyridylcarbamoylcyclohexane compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different, and respectively represent hydrogen, C.sub.1-10 alkyl, C.sub.2-5 alkanoyl, formyl, C.sub.1-4 alkoxy-carbonyl, amidino, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylcarbonyl, phenyl, phenylalkyl, benzoyl, naphthoyl, phenylalkoxycarbonyl, benzylidene, pyridylcarbonyl, piperidyl, pyrrolidylidene or piperidylidene which may be optionally substituted on the ring or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom form 5 to 6-membered cycle which may have oxygen atom, sulfur atom or optionally substituted nitrogen atom in the cycle, or together with the adjacent nitrogen atom form phthalimido, R.sup.3 represents hydrogen or C.sub.1-4 alkyl, R.sup.4 represents hydrogen or C.sub.1-4 alkyl, R.sup.5 represents hydrogen, hydroxy, C.sub.1-4 alkyl or phenylalkoxy. R.sup.6 represents hydrogen or C.sub.1-4 alkyl, A represents single bond, C.sub.Type: GrantFiled: November 22, 1989Date of Patent: March 5, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tomio Muro, Toshio Seki, Masao Abe, Jun Inui, Hiroyuki Sato
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Patent number: 4994473Abstract: Insecticides of the general formula ##STR1## wherein R.sub.1 is an optionally substituted 5- to 10-member heterocyclic moiety; R.sub.2 is an optionally substituted alkyl, cycloalkyl or alkenyl moiety; X is oxygen, sulfur or --NH--; and R.sub.3 is: (a) an optionally substituted 3-phenoxyphenalkyl, 3-phenoxypyridylalkyl, 3-(pyridyloxy)phenalkyl, 3-phenylaminophenoalkyl, 3-benzylphenalkyl or 3-benzyloxyphenalkyl moiety; (b) a benzylfuranylmethyl moiety; (c) a 3- or 4-substituted benzyl or tetrafluorobenzyl moiety; (d) 4-phenoxy-2-butyn-2-yl; or (e) 2-methyl-3-phenylbenzyl.Type: GrantFiled: October 31, 1988Date of Patent: February 19, 1991Assignee: ICI Americas Inc.Inventor: Michael D. Broadhurst
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Patent number: 4994465Abstract: Certain trisubstituted urea compounds as potent inhibitors of the enzyme acyl-CoA:cholesterol acyltransferase, their method of manufacture, pharmaceutical compositions containing such compounds as well as methods of inhibiting the interstitial absorption of cholesterol and lowering blood plasma cholesterol with such compounds as described.Type: GrantFiled: February 5, 1990Date of Patent: February 19, 1991Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4992452Abstract: Novel 5-acyl-2-(1H)-pyridinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.Type: GrantFiled: May 1, 1989Date of Patent: February 12, 1991Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Winton D. Jones, Richard C. Dage, Richard A. Schnettler
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Patent number: 4987141Abstract: The invention provides insecticidally active compounds of formula: ##STR1## wherein X is N or CH; R.sup.a is the group (R.sup.1)(R.sup.2)NS(O).sub.n --wherein R.sup.1 and R.sup.2 are independently selected from H, alkyl, haloalkyl, alkoxy, alkoxyalkyl, formyl, alkanoyl, alkenyl, alkynyl, optionally substituted cycloalkyl, optionally substituted cycloalkylmethyl, optionally substituted benzyl and optionally substituted phenyl, and n is 0, 1 or 2; R.sup.b is the group --OSO.sub.2 R.sup.3 wherein R.sup.3 is alkyl optionally substituted by an optionally substituted phenyl group, haloalkyl, alkenyl optionally substituted by an optionally substituted phenyl group, optionally substituted aryl or N(R.sup.4)(R.sup.5), wherein R.sup.4 and R.sup.5 are independently selected from H and alkyl; and wherein the groups R.sup.a and R.sup.b occupy either a 1,3 configuration relative to each other when X is CH, or a 2,4 or 2,6 configuration relative to X when X is N.Type: GrantFiled: August 9, 1989Date of Patent: January 22, 1991Assignee: Imperial Chemical Industries PLCInventors: Michael J. Bushell, Robin A. E. Carr, Donn W. Moseley, Nan C. Sillars
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Patent number: 4987140Abstract: Novel pyridines of the formula ##STR1## wherein R is selected from the group consisting of (a) phenyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen --CF.sub.3 and --NO.sub.2 and (b) a 5 to 6 member heterocyclic optionally substituted with alkyl of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of (a) alkyl of 1 to 5 carbon atoms, (b) 5 to 6 member heterocyclic optionally substituted with alkyl of 1 to 5 carbon atoms and (c) phenyl and naphthyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --NO.sub.3 and --CF.sub.3, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, --(CF.sub.2).sub.n --CF.sub.Type: GrantFiled: November 27, 1989Date of Patent: January 22, 1991Assignee: Roussel UclafInventors: Francois Clemence, Odile Le Martret, Francoise Delevallee
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Patent number: 4980355Abstract: Novel substituted isonicotinic acid amides of the general formula ##STR1## in which X in ortho/ortho'-position are equal and represent fluorine, chlorine, bromine or iodine;Q.sub.1 is unsubstituted pyridimin-4-yl, or pyrimidin-4-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.2 is unsubstituted pyrimidin-2-yl, or pyrimidin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.3 is unsubstituted pyrimidin-5-yl, or pyrimidin-5-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.4 is pyridin-2-yl, pyridin-3-yl or pyridin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.5 is pyridazin-3-yl or pyridazin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.6 is unsubstituted pyrazin-2-yl, or pyrazin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;R.sub.1, R.sub.2, R.sub.3 are hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl having from 1 to 3 halogen atoms, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.Type: GrantFiled: March 3, 1989Date of Patent: December 25, 1990Assignee: Ciba-Geigy CorporationInventors: Helmut Zondler, Alfred Meyer, Wolfgang Eckhardt, Walter Kunz
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Patent number: 4975443Abstract: Novel fungicidal pyridyl iminocarbonates having the general structural formula ##STR1## wherein R is selected from the group consisting of C.sub.1 -C.sub.16 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 substituted alkenyl, C.sub.3 -C.sub.4 carboalkoxyalkyl, aryl, arylalkyl having C.sub.1 -C.sub.3 alkyl, substituted aryl and arylalkyl wherein the substituents are --Cl, --Br, --F and --NO.sub.2 ; furfuryl, pyridyl, C.sub.1 -C.sub.6 alkyl substituted phosphorus, alkanoyl, alkoxycarbonyl, aroyl, preferably benzoyl, alkylthioarbonyl, alkylthioalkyl, alkoxyalkyl, alkoxybenzyl and ##STR2## wherein R.sub.3 and R.sub.4 are C.sub.1 -C.sub.10 alkyl and can form a heterocyclic ring;R.sub.1 is selected from the group consisting of halogen, C.sub.1 -C.sub.3 alkoxy, C.sub.3 -C.sub.4 alkenyloxy and C.sub.1 -C.sub.3 haloalkoxy;R.sub.2 is selected from the group consisting of C.sub.1 -C.sub.Type: GrantFiled: February 10, 1989Date of Patent: December 4, 1990Assignee: ICI Americas Inc.Inventors: Don R. Baker, Keith H. Brownell
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Patent number: 4966902Abstract: Compounds of the formula (I) and their stereoisomers ##STR1## wherein A, B, C' and D independently of one another denote CH or N, in which at least one of the symbols A, B, C' or D must correspond to a nitrogen atom,X denotes CH.sub.2 or oxygen,R.sup.1 denotes a radical bonded to a carbon atom from the series comprising H, trialkylsilyl, halogen, nitro, cyano, alkenyl, alkynyl, amino, cycloalkyl, phenyl, phenxy, alkoxy, alkenyloxy, alkynyloxy, hydroxycarbonyl, alkylthio, cycloalkyloxy, alkylcarbonyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxy, halogenoalkylthio, halogenoalkoxyalkyl, alkylthioalkyl, alkoxyalkoxy, halogenoalkoxyalkoxy, alkenyloxyalkoxy, halogenoalkenyloxy, alkoxyalkylthio, alkylthioalkoxy, alkylthioalkylthio, halogenoalkoxycarbonyl, halogenoalkenyloxycarbonyl or dialkylamino or two radicals R.sup.1 when they are positioned ortho to one another together denote a methylenedioxy, ethylenedioxy or alkylene radical,R.sup.2 and R.sup.Type: GrantFiled: April 13, 1988Date of Patent: October 30, 1990Assignee: Hoechst AktiengesellschaftInventors: Hans H. Schubert, Gerhard Salbeck, Hans-Peter Krause, Walter Luders, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 4938793Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, alkanoyloxy, benzyloxy, substituted benzyloxy, amino, substituted amino, and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl;R.sup.4 is selected from hydrogen, halogen, alkyl, cyano and alkoxycarbonyl; andn is selected from the integers 1 and 2.Type: GrantFiled: June 20, 1988Date of Patent: July 3, 1990Assignee: ICI Australia LimitedInventors: Keith G. Watson, Graeme J. Farquharson
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Patent number: 4939160Abstract: Hydropyridine derivatives of the formula ##STR1## in which R.sub.1 represents carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl, R.sub.2 represents hydrogen, an optionally etherified or acylated hydroxy group or an optionally acylated amino group, and R.sub.3 represents a radical of the formula R- (Ia), R-alk.sub.1 - (Ib) or R'=alk.sub.2 - (Ic) in which R represents a benzocycloalkenyl radical having a total of from 8 to 12 ring carbon atoms which is bonded via a saturated carbon atom and which is unsubstituted or is mono- or poly-substituted in the benzo moiety by hydroxy, lower alkoxy, lower alkanoyloxy, halogen, lower alkyl and/or by trifluoromethyl, and/or substituted in the .alpha.Type: GrantFiled: December 9, 1988Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventors: Georg von Sprecher, Wolfgang Frostl, Armin Zust
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Patent number: 4931451Abstract: Novel fungicidal pyridyl sulfenyl carbamates having the formula ##STR1## wherein R is selected from the group consisting of haloalkyl, C.sub.1 -C.sub.8 alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, alkanoyl, alkylamino, arylamino, arylalkylamino and substituted pyridylcarbamoyl;R.sub.1 is C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 haloalkoxy or halomethoxy; alkenyloxy; and halogen;R.sub.2 is C.sub.1 -C.sub.3 alkyl;X is oxygen or sulfur; andY is oxygen or sulfurand fungicidally acceptable organic and inorganic salts thereof which are highly effective fungicides for use both as preventive and curative fungicides are disclosed herein.Type: GrantFiled: October 17, 1988Date of Patent: June 5, 1990Assignee: ICI Americas Inc.Inventors: Don R. Baker, Francis H. Walker, Keith H. Brownell
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Patent number: 4929736Abstract: Certain amino-acid derivatives are disclosed as effective inhibitors of human leukocyte elastase and therefore useful in preventing the imbalance of this proteolytic enzyme in vivo. The compounds specifically are derivatives L-valine, L-norvaline, L-norleucine, and L-methionine methyl ester azolides succinimides or pyridones and sulfonate salts, and related compounds such as L-leucine and L-phenylalanine methyl ester derivatives. The compounds were found to be excellent inhibitors in that they embody both inhibitory and anti-oxidant or anti-inflammatory activity.Type: GrantFiled: November 6, 1987Date of Patent: May 29, 1990Assignee: Board of Trustees of the Wichita State UniversityInventor: William C. Groutas
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Patent number: 4900750Abstract: This invention concerns compounds of formula ##STR1## or salts thereof, wherein: Ar is an optionally substituted aryl radical;R represents hydrogen or an optionally substituted alkyl, aralkyl, or aryl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optionally substituted aryl;A and B independently represent a group of formula --XR.sup.3 whereinX is a group of formula --(CHR.sup.6).sub.p Y(CHR.sup.7).sub.q --whereinY represents --O--, --S--, --NR.sup.8 -- or a direct bond; p and q each represent 0, 1 or 2 providing that p and q do not both represent O when Y is a direct bond; and R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or alkyl; and R.sup.Type: GrantFiled: August 3, 1987Date of Patent: February 13, 1990Assignee: John Wyeth & Brother, LimitedInventors: John L. Archibald, Terence J. Ward, Albert Opalko
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Patent number: 4889865Abstract: Mono, di and tri-esters of 1,8-dihydroxy-10-phenyl-9-anthrone or -9-anthranol have the formula ##STR1## wherein p is 0 or 1,(a) when p=0, t=1 and R.sub.2 represents hydrogen or --COR.sub.3,(b) when p=1, t=0 and R.sub.1 and R.sub.2 each independently represent hydrogen or --COR.sub.3,R.sub.3 represents linear or branched alkyl having 1-17 carbon atoms, cycloalkyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, halogen, a nitro function, --CF.sub.3 or a hydroxyl function, and mixtures of said esters. These esters are prepared by reacting 1,8-dihydroxy-10-phenyl-9-anthrone with an activated form of an acid. The esters are useful in human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 21, 1989Date of Patent: December 26, 1989Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Gerard Lang, Jean Maignan, Serge Restle, Christopher Hensby, Michel Colin
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Patent number: 4877797Abstract: Compounds are described of the formula ##STR1## wherein R.sub.1 is a nitro or trifluoromethyl group; R.sub.2 is a C.sub.1 -C.sub.6 alkyl group; R.sub.3 is a pyridyl or pyridyl N-oxide group which may be substituted with halogen, hydroxyl, haloalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl and further may be fused with a benzene or naphthalene ring, said ring being optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen or haloalkyl, and a pharmaceutically acceptable acid addition salt thereof. The compounds of the formula (I) are of vasodilating and blood pressure lowering activities and thus may be useful for the treatment of cardiac diseases, cerebrovascular diseases and hypertension.Type: GrantFiled: June 15, 1987Date of Patent: October 31, 1989Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Hiroaki Satoh, Hiroyasu Koyama, Yoshikuni Suzuki, Toshiji Sugai, Koichi Watanabe
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Patent number: 4873253Abstract: A phenylalanine derivative having the formula (I): ##STR1## wherein A represents ##STR2## B represents ##STR3## wherein m is 0, 1, or 2 and n is 3, 4, or 5; X represents (a) hydroxy, (b) nitro, (c) amino, (d) phenoxy which may be substituted with (i) halogen or (ii) nitro, (e) c.sub.1 -C.sub.4 alkyloxy which may be substituted wit (i) phenyl or (ii) benzoyl, (f) benzoyl, (g) pyridyloxy which may be substituted with (i) halogen or (ii) nitro, or (h) c.sub.1 -C.sub.4 alkyl which may by substituted with halogen;Y represents ##STR4## or --OR.sup.3 wherein R.sup.1 R.sup.2 are independently (a) hydrogen, (b) phenyl which may be substituted with (i) benzoyl, (ii) C.sub.1 -C.sub.4 alkylcarbonyl, (iii) C.sub.1 -C.sub.4 alkyl which may be further substituted with C.sub.1 -C.sub.4 alkoxycarbonyl or hydroxycarbonyl, (iv) C.sub.2 -C.sub.5 alkenyl which may be further substituted with hydroxycarbonyl or C.sub.1 -C.sub.4 alkoxycarbonyl, (v) C.sub.1 -C.sub.Type: GrantFiled: March 30, 1987Date of Patent: October 10, 1989Assignees: Shosuke Okamoto, Showa Denko Kabushiki KaishaInventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Hiroshi Nojima, Takashi Shishikura
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Patent number: 4863938Abstract: Pyridine derivatives of the formula ##STR1## their tautomers and their salts, in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and n have the meanings given in the claims, can be used as active ingredients in medicaments and are manufactured in a manner known per se.Type: GrantFiled: October 31, 1988Date of Patent: September 5, 1989Assignee: Ciba-Geigy CorporationInventors: Georg von Sprecher, Peter Waldmeier