At 2-position And At 4- Or 6-position Patents (Class 544/323)
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Patent number: 5574040Abstract: A compound according to the formula: ##STR1## wherein A=CH.sub.3 or CH.sub.2 CH.sub.3 and ##STR2## wherein X=NH.sub.2, CH.sub.2 or CH.sub.2 CH.sub.3 ; X'=CH.sub.3 or CH.sub.2 CH.sub.3 ; Y=NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2 ; and Z=H, CH.sub.3 or CH.sub.2 CH.sub.3 ; or ##STR3## wherein Y' and Z', indepedently, = H, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2 or N.sup.+ (CH.sub.3).sub.3 ; and salts thereof.Type: GrantFiled: January 6, 1995Date of Patent: November 12, 1996Assignee: Picower Institute for Medical ResearchInventors: Michael I. Bukrinsky, Anthony Cerami, Peter Ulrich
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Patent number: 5569761Abstract: Process for the preparation of sulfonylureasHerbicidal sulfonylureas of the formula I, ##STR1## in which X is --O--, --0--NR.sup.2 -- or --SO.sub.2 --NR.sup.2 --, Y is --N-- or CH,R.sup.1 is (substituted) alkyl, (substituted) alkenyl or (substituted) alkynyl, or else, where X.dbd.O, (substituted) phenyl,R.sup.2 is H, alkyl, alkenyl, alkynyl or cycloalkyl,R.sup.3, R.sup.4 are H, (substituted) alkyl or (substituted) alkoxy, halogen, alkylthio, alkylamino or dialkylamino andR.sup.5, R.sup.Type: GrantFiled: February 7, 1995Date of Patent: October 29, 1996Assignee: Hoechst AktiengesellschaftInventors: Lothar Willms, Stephen Lacchein, Gunter Schlegel, Heinz Kehne
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Patent number: 5550238Abstract: This invention relates to a process for preparing sulfonylureas comprising reacting a sulfonyl chloride with a cyanate salt and an amine base in the presence of an inert aprotic solvent to give an isocyanate complex which is then reacted with an amino heterocycle to form the sulfonylurea product and a process for converting the crystal form of the prepared sulfonylurea product to a more stable crystal product form.Type: GrantFiled: August 23, 1995Date of Patent: August 27, 1996Assignee: E. I. Du Pont de Nemours and CompanyInventors: George C. Chiang, Richard F. Davis, Kwaku O. Temeng
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Patent number: 5536837Abstract: The present invention provides an N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring represented by formula [I]: ##STR1## wherein R.sup.1 represents an alkyl group, an alkenyl group, or the like, R.sup.2 represents a hydrogen atom, an alkyl group, or the like, R.sup.3 and R.sup.4 represent independently an alkyl group, alkoxy group, or the like, and X and Y represent independently a methyne group or a nitrogen atom; or the salt of the same, a method for producing the same, and a biocide containing the same as an active ingredient. The N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring according to the present invention exhibits superior effects against blight caused by plant pathogenic fungi belonging to Oomycetes such as downy mildew, late blight, or the like in a low concentration as well as controls weeds occurring in paddy fields and plowed fields.Type: GrantFiled: May 18, 1995Date of Patent: July 16, 1996Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Ikumi Urushibata, Takumi Yoshimura, Takeshi Deguchi, Norihisa Yonekura, Junetsu Sakai, Shigeru Hayashi
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Patent number: 5525604Abstract: A 4-aminopyrimidine of the formula (I): ##STR1## wherein A is a bond, C1-4 alkylene or C1-4 oxyalkylene;Y is a bond, C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenylene or phenyl(C1-4)alkylene;Z is a bond or vinylene;R1 is 4-15 membered heterocyclic ring containing one or two nitrogen atom;R2 is (i) 4-15 membered heterocyclic ring containing one or two nitrogen, one or two of oxygen or one sulfur atom,(ii) C4-15 carbocyclic ring,(iii) C1-4 alkoxy,(iv) hydroxy(C1-4 alkoxy) or(v) hydroxy;R3 is (i) 4-15 membered heterocyclic ring containing one or two nitrogen, one oxygen, one sulfur, or one nitrogen and one sulfur atom,(ii) C4-15 carbocyclic ring,(iii) formula:CH2.dbd.CH(X)--whereinX is halogen.(iv) hydrogen.l is 1 or 2.and some compounds are excluded.and acid addition salts thereof, salts thereof; have inhibitory effect on cGMP-PDE, or additionally on TXA2 synthetase.Type: GrantFiled: August 24, 1994Date of Patent: June 11, 1996Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Sung J. Lee, Yoshitaka Konishi, Orest T. Macina, Kigen Kondo, Dingwei T. Yu, Tamara A. Miskowski
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Patent number: 5525724Abstract: A process for the preparation of chloropyrimidines of the formula ##STR1## in which the substituents may be alkyl, cycloalkyl, aryl or radicals containing heteroatoms, but in which at least one of the substituents R.sup.1 to R.sup.4 must be Cl, which involves:reacting a hydroxy-pyrimidine or its tautomeric keto form with phosphoryl chloride in the presence of an amine or amine hydrochloride;recovering phosphoryl chloride after the reaction by adding phosphorus pentachloride and distilling the phosphoryl chloride; andseparating the chloropyrimidine from the amine hydrochloride by addition of a solvent which will dissolve the chloropyrimidine but not the amine hydrochloride and removing the amine hydrochloride.Type: GrantFiled: February 27, 1995Date of Patent: June 11, 1996Assignee: Huels AktiengesellschaftInventor: Artur Hunds
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Patent number: 5518994Abstract: Disclosed are a herbicide and a plant growth regulator comprising a 2-arylaminopyrimidinone derivative represented by the formula (1): ##STR1## (wherein Q represents various kinds of aromatic ring or heterocyclic ring).This compound can be used safely to main crops and shows high herbicidal effect to many weeds with a low dosage, and also shows plant growth regulating effect.Type: GrantFiled: December 6, 1994Date of Patent: May 21, 1996Assignee: Nissan Chemical Industries, Ltd.Inventors: Yasuo Kawamura, Jun Satow, Kenzo Fukuda, Eiichi Oya, Kaoru Itoh, Hiroshi Kita, Hisashi Nakata, Tsutomu Nawamaki, Seiichi Fujii, Shigeomi Watanabe, Kimihiro Ishikawa, Yoichi Ito
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Patent number: 5508402Abstract: A process for the preparation of substituted benzenes or benzenesulfonic acid and its derivatives comprising diazotisation of an aminobenzene or ortho-amino-benzenesulfonic acid derivative followed by homogeneous palladium-catalysed coupling with an olefine and heterogeneous palladium-catalysed hydrogenation of the olefinic substituent, wherein the homogeneous catalyst is reduced and precipitated as metal after the coupling in the reaction mixture and used as a heterogeneous palladium catalyst for the hydrogenation step. The process is particular suitable for the preparation N-benzenesulfon-N'-triazinyl-urea herbicides.Type: GrantFiled: May 26, 1995Date of Patent: April 16, 1996Assignee: Ciba-Geigy CorporationInventors: Peter Baumeister, Gottfried Seifert, Heinz Steiner
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Patent number: 5500406Abstract: The present invention provides novel iminosulfonylurea derivatives which are useful as herbicides with excellent activity and selectivity. These derivatives can be used to protect rice, wheat, corn, soybean, cotton and sugar beet from weeds.Type: GrantFiled: April 15, 1994Date of Patent: March 19, 1996Assignee: Nissan Chemical Industries Ltd.Inventors: Kenzi Makino, Shigeaki Akiyama, Hideaki Suzuki, Takeshi Nagaoka, Toshio Niki, Koichi Suzuki, Tsutomu Nawamaki, Shigeomi Watanabe, Kimihiro Ishikawa
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Patent number: 5478934Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.Type: GrantFiled: November 23, 1994Date of Patent: December 26, 1995Inventors: Jun Yuan, Jan W. F. Wasley
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Patent number: 5470856Abstract: The invention is concerned with a tetrahydropyrimidine derivative having formula I ##STR1## wherein R.sub.1 is hydrogen;R.sub.2 is hydrogen, a lower alkyl group, or lower acyl; orR.sub.1 and R.sub.2 represent together a bond;R.sub.3 is hydrogen, a lower hydrocarbon group optionally substituted with halogen, CN, aryl, or COR.sub.7 ;R.sub.4 is hydrogen, a lower alk(en)yl group, or aryl;R.sub.5 is hydrogen, amino, lower alkyl substituted amino, or a lower alkyl group; andR.sub.6 is hydrogen or methyl;R.sub.7 is amino, lower alkyl substituted amino, or a lower alkyl group; ora pharmaceutically acceptable salt thereof.The compounds of this invention have muscarinic properties and can be used for the treatment of cognition disorders, and for the treatment of cholinergic deficiencies.Type: GrantFiled: March 3, 1993Date of Patent: November 28, 1995Assignee: Akzo Nobel N.V.Inventor: Ralf Plate
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Patent number: 5461025Abstract: The present invention relates to novel benzenesulfonylurea derivatives, having a herbicidal activity, which is described in the following structure of general formula (I) ##STR1## wherein R.sup.1 is H,C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, halogen, CN, NO.sub.2, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 haloalkoxy, SO.sub.2 NR.sup.I R.sup.II, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 alkylsulfinyl, C.sub.1 -C.sub.3 alkylsulfonyl, SCH.sub.2 F, NH.sub.2, NHCH.sub.3, N(Me).sub.2, C.sub.1 -C.sub.2 alkyl substituted with C.sub.1 -C.sub.2 alkoxy, C.sub.1 -C.sub.2 haloalkoxy, SH, SCH.sub.3, CN or OH, or CO.sub.2 R.sup.III ; and then R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.3 cyanoalkyl, methoxy or ethoxy; R.sup.II is H, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, or when taken together connecting R.sup.I and R.sup.II, --(CH.sub.2).sub.3 --, --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 -- or --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 -- , may be formed;R.sup.III is C.sub.1 -C.sub.Type: GrantFiled: December 9, 1993Date of Patent: October 24, 1995Assignee: Korea Research Institute of Chemical TechnologyInventors: Dae-Whang Kim, Young Kwan Ko, Jin-Seog Kim, Dong Whan Ku
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Patent number: 5461152Abstract: Compounds of the formulae I and Ia and their racemates ##STR1## in which A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, R.sub.1 is hydrogen or a protective group, R.sub.2 is hydrogen or a protective group or a radical forming a phosphorus-containing nucleotide bridge group and B is a purine or pyrimidine radical or an analogue thereof, can be used as antiviral active ingredients or for the preparation of biologically active oligonucleotides.Type: GrantFiled: June 28, 1993Date of Patent: October 24, 1995Assignee: Ciba-Geigy CorporationInventors: Karl-Heinz Altmann, Rene Imwinkelried, Albert Eschenmoser
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Patent number: 5434124Abstract: Sulfonylurea derivatives of the formula I ##STR1## where R.sup.1 is unsubstituted or substituted alkyl or phenyl; alkenyl or propargyl, alkylamino or dialkylamino; R.sup.2 is hydrogen, halogen, unsubstituted or substituted methyl, methoxy or ethoxy, alkylsulfonyl, nitro or cyano;R.sup.3 is difluoromethoxy, trifluoromethoxy, bromodifluoromethoxy, chlorodifluoromethoxy or fluorine;R.sup.4 is halogen, unsubstituted or halogen-substituted methyl, ethyl, methoxy or ethoxy or is methylamino or dimethylamino;R.sup.5 is hydrogen, alkyl or alkenyl or alkynyl, andZ is CH or N,with the proviso thata) when R.sup.3 is difluoromethoxy, R.sup.1 is not dialkylamino, R.sup.2 is not alkylsulfonyl and R.sup.4 is not methyl or methoxy andb) when R.sup.3 is fluorine and Z is N, R.sup.4 is not alkylamino, and salts thereof are suitable as herbicides.Type: GrantFiled: August 6, 1993Date of Patent: July 18, 1995Assignee: BASF AktiengesellschaftInventors: Horst Mayer, Gerhard Hamprecht, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5414084Abstract: Herbicidal sulfonylureas of the formula I, ##STR1## in which X is --O--, --O--NR.sup.2 -- or --SO.sub.2 --NR.sup.2 --, Y is --N-- or CH,R.sup.1 is (substituted) alkyl, (substituted) alkenyl or (substituted) alkynyl, or else, where X=O, (substituted) phenyl,R.sup.2 is H, alkyl, alkenyl, alkynyl or cycloalkyl,R.sup.3, R.sup.4 are H, (substituted) alkyl or (substituted) alkoxy, halogen, alkylthio, alkylamino or dialkylamino andR.sup.5, R.sup.Type: GrantFiled: March 5, 1992Date of Patent: May 9, 1995Assignee: Hoechst AktiengesellschaftInventors: Lothar Willms, Stephen Lachhein, Gunter Schlegel, Heinz Kehne
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Patent number: 5401710Abstract: Herbicidal compositions which comprise one or more compounds of the formula: ##STR1## or salts thereof, where: A is --CH.dbd. or --N.dbd.;R.sup.1 is alkyl, alkoxy, halo or --NR.sup.7 R.sup.8 ;R.sup.2 is alkyl or alkoxy;R.sup.3 is hydrogen, alkenyl or alkynyl, or substituted or unsubstituted alkyl, alkanoyl or alkoxycarbonyl;R.sup.4 is hydrogen or substituted or unsubstituted alkyl;R.sup.5 is halo or substituted or unsubstituted alkyl or aryl; andX is --CO.sub.2 R.sup.6, --CONR.sup.7 R.sup.8 or --CN;in which R.sup.6, R.sup.7 and R.sup.8, which may be the same or different, each represent hydrogen, substituted or unsubstituted alkyl, or one of R.sup.7 and R.sup.8 represents substituted amino;in association with a suitable carrier and/or surface active agent, together with the compounds of formula I per se where R.sup.5 represents isopropyl, and/or X represents methoxycarbonyl, and salts thereof.Type: GrantFiled: July 9, 1993Date of Patent: March 28, 1995Assignee: Schering Agrochemicals LimitedInventor: Peter S. Gates
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Patent number: 5397781Abstract: The present invention relates to novel 5-(.omega.-substituted amino-alkanoyl amino)pyrimidine derivatives, processes for producing the derivatives, and pharmaceutical compositions containing said derivatives. The compounds in the present invention have potent effects of inhibiting ACAT activity and lowering serum cholesterol. The compounds of the present invention are extremely useful for the treatment and/or prevention of arteriosclerosis or hyperlipidemia.Type: GrantFiled: February 11, 1993Date of Patent: March 14, 1995Assignee: Mochida Pharmaceutical Company, LimitedInventors: Kazutoshi Yanagibashi, Kiyoshi Mizuguchi, Shuhei Ohnishi, Kimihiro Murakami
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Patent number: 5374725Abstract: A compound of formula I or salt thereof can be prepared in a process which comprises reacting a compound of formula II with a compound of formula III: ##STR1## wherein the formulae I-III the radical X is O, ONR.sup.2 or SO.sub.2 NR.sup.2 ; Y is N or CH;R.sup.1 is (subst.) alkyl, (subst.) alkenyl, (subst.) alkynyl, or in case X.dbd.O, also (subst.) phenyl;R.sup.2 is H, alkyl, alkenyl, alkynyl or cycloalkyl,R.sup.3 -R.sup.6 are defined in claim 1;Z is S or NR.sup.8 ; R.sup.7, R.sup.8 are H, alkyl, (subst.) phenyl or (subst.) benzyl, or, in case Z.dbd.NR.sup.8, R.sup.7 and NR.sup.8 are also a 5- to 7-membered heterocycle.Type: GrantFiled: February 22, 1994Date of Patent: December 20, 1994Assignee: Hoechst AktiengesellschaftInventors: Gunter Schlegel, Hilmar Mildenberger
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Patent number: 5373012Abstract: A 5-fluoro-minoxidil compound and compositions are disclosed which are useful in the treatment of hair growth and cardiovascular disorders. The 5-fluoro-minoxidil compounds have been shown to have increased transdermal transport than minoxidil and therefore can be used in decreased amounts to achieve the same pharmacological efficacy of minoxidil.Type: GrantFiled: May 10, 1993Date of Patent: December 13, 1994Assignee: The Upjohn CompanyInventor: Heinrich J. Schostarez
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Patent number: 5371062Abstract: The present invention relates to new substituted azines, of the general formula (I) ##STR1## in which n, Q.sup.1, Q.sup.2, Q.sup.3, R.sup.1, R.sup.2, R.sup.3, X, Y and Z have the meanings given in the description, to a plurality of processes for their preparation, and to their use as herbicides.Type: GrantFiled: April 1, 1993Date of Patent: December 6, 1994Assignee: Bayer AktiengesellschaftInventors: Roland Andreee, Mark W. Drewes, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5364937Abstract: Compounds of the formula I or salts thereof, ##STR1## in which X is oxygen, --O--NR.sup.2 -- or --SO.sub.2 --NR.sup.2 --, and Y is N or CH,R.sup.1 is (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl or (C.sub.2 -C.sub.6)alkynyl, which are in each case optionally substituted, or, in the case where X=oxygen, also (subst.) phenyl,R.sup.2 is H, (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl or -alkynyl or (C.sub.3 -C.sub.6) cycloalkyl,R.sup.3 and R.sup.4 are H, (subst.) (C.sub.1 -C.sub.4)alkyl or (subst.) (C.sub.1 -C.sub.4)alkoxy or halogen, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkylamino or di[(C.sub.1 -C.sub.4)alkyl]-amino,R.sup.5 is H or (C.sub.1 -C.sub.4)alkyl and R.sup.6 is hydrogen,may be prepared by reacting compounds of the formula II,R.sup.1 --X--R.sup.7 (II)with compounds of the formulae III, IV and VR.sup.8 --OCN (III)SO.sub.2 Cl.sub.2 (IV) ##STR2## where R.sup.7 and R.sup.8 are H, a quarternary ammonium ion or one equivalent of a metal cation.Type: GrantFiled: March 4, 1993Date of Patent: November 15, 1994Assignee: Hoechst AktiengesellschaftInventor: Gunter Schlegel
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Patent number: 5360804Abstract: Multicomponent agent or kit for preparing the sulpho-conjugated form of pyridino, pyrimidino or triazino N-oxide compounds and method of use.The present invention relates to a multicomponent agent or kit for preparing the sulpho-conjugated form of pyridino, pyrimidino or triazino N-oxide compounds,comprising at least one compound of the pyridino, pyrimidino or triazino N-oxide type, on the one hand,and a sulphating agent, on the other hand.Type: GrantFiled: December 12, 1991Date of Patent: November 1, 1994Assignee: L'OrealInventors: Quintino Gaetani, Andre Rougier, Albert Duranton, Michel Hocquaux
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Patent number: 5358945Abstract: The present invention relates to pyrimidine compounds represented by the formula ##STR1## (wherein X is a substituted or a cyclic amino group and Y is a substituted amino group or a substituted carbonyl group) or their pharmaceutically acceptable salts, and a therapeutic agent for neurological diseases comprising the compounds.These compounds are useful for treatment of various disorders in nervous systems since they are effective on growth of neurons and promotion of the formation and elongation of neutrites.Type: GrantFiled: March 30, 1992Date of Patent: October 25, 1994Assignees: Mitsui Petrochemical Industries, Ltd., Mitsui Pharmaceuticals, Inc.Inventors: Akira Mizuchi, Ken Ikeda, Yuichiro Kokubun, Kazutoshi Horikomi, Tadayuki Sasaki, Akira Awaya, Ikuo Tomino, Masaharu Ishiguro, Takumi Kitahara, Noriaki Kihara
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Patent number: 5356862Abstract: The invention relates to herbicidal sulfonylurea compounds, agriculturally suitable compositions thereof and a method for their use as general or selective preemergent or postemergent herbicides or plant growth regulants.Type: GrantFiled: July 22, 1992Date of Patent: October 18, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventor: William T. Zimmerman
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Patent number: 5350851Abstract: Intermediates and a process for the synthesis of 6-monosubstituted tetrahydropteridine C6-stereoisomers, including (6S)-tetrahydrofolic acid. The intermediates are shown in their two enantiomeric forms as follows: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and represent hydrogen, methyl, hydroxy, amino, alkyl or dialkylamino, alkoxy, benzyloxy, or benzylthio; R.sub.3 represents an alkene, alkyne, cycloalkyl, benzyl, alkyl (substituted with hydroxy, acetoxy, benzyloxy, alkoxy, alkylthio, amino, carboxy, oxo, or phosphate), a protected aldehyde, or ##STR2## wherein n=1 or 2, R.sub.4 is hydrogen, formyl, methyl, or propargyl, and ZZ represents an amino acid or amino acid polymer.Type: GrantFiled: November 25, 1992Date of Patent: September 27, 1994Assignee: South Alabama Medical Science FoundationInventors: Steven W. Bailey, June E. Ayling
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Patent number: 5330989Abstract: Biphenyl derivatives of cyclobutene-1,2-dione of formula 1 are angiotensin II antagonists and are useful for the treatment of hypertension and congestive heart failure ##STR1## wherein: Y is O, NR.sup.7, NCOR.sup.7 ; or R.sup.5 and Y taken together represent a linking chain of N.dbd.CR.sup.8 N; or R.sup.5 and Y taken together represent a linking chain of (CR.sup.9 R.sup.10).sub.n CON where n=1,2,3,4, or 5;X is N, CR.sup.7 ;Z is N, CR.sup.7 ;R.sup.1 is H, alkyl, benzyl, alkoxyalkyl, phenyl;R.sup.2 is H, alkyl, benzyl, alkoxyalkyl, phenyl, alkoxy, alkyl-OH, perfluoroalkyl, F, Cl, Br, I, NR.sup.7 R.sup.8 ;R.sup.3 is H, alkyl, benzyl, alkoxyalkyl, phenyl, alkoxy, alkyl-OH, perfluoroalkyl, F, Cl, Br, I, NR.sup.7 R.sup.8 ;R.sup.4 is H, NR.sup.7 R.sup.8, OR.sup.1, CN, F, Cl, I, Br, perfluoroalkyl, alkyl, phenyl, alkoxy, alkyl-OH, alkoxyalkyl, --(CH.sub.2).sub.n CO.sub.2 R.sup.1, --(CH.sub.2).sub.n CONR.sup.7 R.sup.8 where n=1, 2, 3, 4, or 5;R.sup.5, R.sup.Type: GrantFiled: September 11, 1992Date of Patent: July 19, 1994Assignee: American Home Products CorporationInventors: Richard M. Soll, William A. Kinney
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Patent number: 5324710Abstract: Compounds of the formula I or their salts ##STR1## in which R.sup.1 to R.sup.6, W, X, a and b are as defined in claim 1 and L is a heterocyclic or isocyclic aromatic radical having 5 to 6 ring atoms, which can be condensed with an aromatic or non-aromatic 5- or 6-membered ring, where the radical can be unsubstituted or substituted, and a, b and c independently of one another are 0 or 1, are suitable as herbicides, plant growth regulators and fungicides. They can be prepared by the processes defined herein, it being possible in some cases to use novel intermediates.Type: GrantFiled: April 21, 1992Date of Patent: June 28, 1994Assignee: Hoechst AktiengesellschaftInventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz, Burkhard Sachse, Peter Braun
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Patent number: 5317021Abstract: Amino acid compounds of the formula: ##STR1## wherein the various symbols are as hereinafter described, which have inhibiting effect on enkephalinase.Type: GrantFiled: November 4, 1992Date of Patent: May 31, 1994Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Masanori Kawamura, Yoshinobu Arai, Hideki Aishita
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Patent number: 5312919Abstract: This invention relates to novel photooxidation products, and derivatives thereof, of Merocyanine 540, their preparation and their uses as anticancer and antiviral agents.Type: GrantFiled: June 12, 1992Date of Patent: May 17, 1994Assignee: Baylor Research InstituteInventors: Kirpal S. Gulliya, Burchard Franck, J. Lester Matthews, Udo Schneider
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Patent number: 5306693Abstract: N-phenylsulfonyl-N'-pyrimidinyl- and -triazinyl-ureas of formula I ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.5 alkenyl, C.sub.1 -C.sub.4 haloalkyl, COO--R.sub.2 or A--R.sub.3 ;R.sub.2 is C.sub.1 -C.sub.5 alkyl;R.sub.3 is C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.4 alkoxyalkyl or C.sub.1 -C.sub.5 haloalkyl;X is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkyl mono- to tri-substituted by halogen; C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 alkoxy mono- to tri-substituted by halogen;A is oxygen, sulfur, SO or SO.sub.2 ;Y is halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkyl mono- to tri-substituted by halogen; C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.Type: GrantFiled: August 18, 1992Date of Patent: April 26, 1994Assignee: Ciba-Geigy CorporationInventor: Willy Meyer
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Patent number: 5284820Abstract: Herbicidal substituted cycloalkenes of the formula ##STR1## in which A is a straight-chain or branched, optionally substituted alkanediyl group,X is O, S, N--R.sup.8 or CR.sup.9 R.sup.10,Y is O, S, NH or N-alkyl,Z is N or R.sup.11, andR.sup.1 to R.sup.11 represent various organic radicals.Type: GrantFiled: September 2, 1992Date of Patent: February 8, 1994Assignee: Bayer AktiengesellschaftInventors: Mark-Wilhelm Drewes, Peter Muller, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5280009Abstract: Pyrimidine derivatives of the Formula Ia or Ib ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen or alkyl;A is a substituted or unsubstituted bi- or tricyclic carbo- or heterocyclic radical which may contain one or several double bonds;R.sup.5 is H or alkyl;X is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio or haloalkylthio; and addition salts thereof with organic or inorganic acids and the use of said pyrimidine derivative to control undesirable plant growth.Type: GrantFiled: July 16, 1992Date of Patent: January 18, 1994Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Klaus Ditrich, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5252575Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydrogen or hydroxy; andR.sub.2 is C.sub.1-6 alkyl;which are pro-drugs for 9-(3-hydroxyprop-1-oxy)guanine having antiviral activity, a process for their preparation and their use as pharmaceuticals.Type: GrantFiled: May 21, 1992Date of Patent: October 12, 1993Assignee: Beecham Group p.l.c.Inventors: Michael R. Harnden, Paul G. Wyatt, Leslie J. A. Jennings
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Patent number: 5252567Abstract: This invention concerns compounds of the formula I: ##STR1## wherein R.sup.1 is (1-10C)alkyl, (3-8C)cycloalkyl, (3-8C)cycloalkyl-(1-4C)-alkyl, phenyl or phenyl(1-4C)alkyl, the phenyl moiety of the latter two optionally bearing one or more substituents; R.sup.2 is hydrogen, (1-4C)alkyl, amino or (1-4C)alkylamino; R.sup.6 is (1-4C)alkyl, amino or (1-4C)alkylamino; Q is a group of formula II, in which case R.sup.3 and R.sup.4 are independently hydrogen, (1-4C)alkyl, phenyl or benzyl the phenyl moiety of the latter two optionally bearing one or two substituents; R.sup.5 is hydrogen, (1-4C)alkyl or (2-4C)alkenyl; A and B are independently ethylene or trimethylene; Z is a direct bond between A and B, or an oxy, thio, carbonyl, methylene, ethylenedioxymethylene, ethylidene, or isopropylidene link, or Z is a group of the formula .dbd.N.Type: GrantFiled: December 18, 1990Date of Patent: October 12, 1993Assignee: Imperial Chemical Industries PLCInventors: Stuart D. Mills, Rodney B. Hargreaves, Bernard J. McLoughlin
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Patent number: 5250685Abstract: A process for the preparation of an S-alkyl-isothioureidoazine of the formula ##STR1## in which R is alkyl,X and Y each independently is selected from the group consisting of hydrogen, halogen, and alkyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxy, alkoxy, alkylthio, halogenoalkylthio, alkylamino or dialkylamino, each of which is optionally substitued, andZ is nitrogen or CHwhich comprises in a first step reacting an thioureidoazine of the formula ##STR2## with a dialkyl sulphate of the formulaRO--SO.sub.2 --ORat a temperature between about 20.degree. C. and 150.degree. C., thereby to form an adduct of the formula ##STR3## and in a second step reacting the adduct with an acid acceptor in the presence of an aprotic polar diluent at a temperature between about 0.degree. C. and 50.degree. C.Type: GrantFiled: September 21, 1992Date of Patent: October 5, 1993Assignee: Bayer AktiengesellschaftInventor: Hans-Jochem Riebel
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Patent number: 5227493Abstract: N-fluoro perfluoroheterocyclic sulfonamides of the following Formula I ##STR1## wherein Het.sub.f represents an aromatic perfluoroheterocyclic radical of valency n and each R independently represents a substituted or unsubstituted C.sub.1 -C.sub.30 alkyl, C.sub.6 -C.sub.14 aryl substituted C.sub.1 -C.sub.10 alkyl, C.sub.6 -C.sub.14 aryl, or C.sub.1 -C.sub.10 alkyl substituted C.sub.6 -C.sub.14 aryl group, are novel electrophilic fluorinating agents. Preferably Het.sub.f is a perfluorinated nitrogen-containing aromatic group, especially pyridyl, pyrimidinyl, pyrazinyl or 1,3,5-triazinyl; n is 1; and R is perfluorinated, especially trifluoromethyl.Type: GrantFiled: August 31, 1990Date of Patent: July 13, 1993Assignee: Air Products and Chemicals, Inc.Inventor: Ronald E. Banks
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Patent number: 5225555Abstract: The present invention involves two processes for the purification of a mixture of 2,4-di(1-pyrrolidinyl)-6-chloropyrimidine (III) ##STR1## and 4,6-di(1-pyrrolidinyl)-2-chloropyrimidine (IV) ##STR2## to where <1.0% of 4,6-di(1-pyrrolidinyl)-2-chloropyrimidine (IV) is present. In addition also disclosed is a process which not only purifies 2,4-di(1-pyrrolidinyl)-6-chloropyrimidine (III) but produces the commercially important 2,4-di(1-pyrrolidinyl)-6-(1-piperazinyl)pyrimidine (IX) directly.Type: GrantFiled: August 19, 1992Date of Patent: July 6, 1993Assignee: The Upjohn CompanyInventors: Bruce A. Pearlman, Amphlett G. Padilla
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Patent number: 5223017Abstract: Compounds of formula (I) or salts thereof, ##STR1## in which J is a radical of the formula R.sup.1 SO.sub.2 --CR.sup.2 R.sup.3 --, R.sup.4 R.sup.5 N--SO.sub.2 --CR.sup.2 R.sup.3 --, or ##STR2## and wherein the radicals R.sup.1, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.*, A, W, m, n and 0 are defined as set forth in the specification, are suitable as selective herbicides and plant growth regulators.Type: GrantFiled: July 3, 1991Date of Patent: June 29, 1993Assignee: Hoechst AktiengesellschaftInventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer
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Patent number: 5223505Abstract: This invention concerns novel aminopyrimidinium salts of the formula I: ##STR1## in which R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl, alkenyl, alkoxyalkyl, phenyl, phenylalkyl, cycloalkyl or cycloalkyl-alkyl; or both of R.sup.2 and R.sup.6 are basic groups as mentioned above; and R.sup.5 is hydrogen, (1-4C)alkyl or (3-6C)alkenyl; or R.sup.2 is a basic group as mentioned above, and R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyrimidine ring, complete a benzene ring; R.sup.4 is hydrogen, alkyl, cycloalkyl-alkyl, alkenyl, alkynyl or phenylalkyl; or R.sup.4 is an optionally substitutued alkylene or alkenylene linked to the nitrogen atom of the group Q.A.Type: GrantFiled: April 20, 1990Date of Patent: June 29, 1993Assignee: Imperial Chemical Industries PlcInventors: Rodney B. Hargreaves, Paul W. Marshall, Bernard J. McLoughlin, Stuart D. Mills
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Patent number: 5217522Abstract: Herbicidal sulphonylguanidinoazines of the formula ##STR1## in which n represents the numbers 1 or 2,A represents nitrogen or a C-X group, where X represents hydrogen or halogen.Type: GrantFiled: March 27, 1992Date of Patent: June 8, 1993Assignee: Bayer AktiengesellschaftInventors: Hans-Jochem Riebel, Christa Fest, Ernst R. F. Gesing, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Klaus Lurssen, Hans-Joachim Santel, Robert E. Schmidt
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Patent number: 5213608Abstract: Herbicidal substituted sulphonylamidinohydrazones of the formula ##STR1## in which R.sup.1 represents in each case optionally substituted aryl, aralkyl or heteroaryl,R.sup.2 represents hydrogen, or represents in each case optionally substituted alkyl, aryl or aralkyl,R.sup.3 represents hydrogen, or represents in each case optionally substituted alkyl, alkenyl, alkadienyl, alkinyl, (hetero)aryl, aralkyl, aralkenyl, alkoxy, alkoxycarbonyl or dialkylamino, or together with R.sup.2 represents optionally substituted alkanediyl,R.sup.4 represents hydrogen, halogen, hydroxyl, alkyl, halogenoalkyl, alkoxyalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, alkylamino or dialkylamino,X represents nitrogen or a --CH group,Y represents nitrogen or a --CR.sup.5 group whereR.sup.5 represents hydrogen, halogen, cyano, alkyl, formyl, alkyl-carbonyl or alkoxy-carbonyl, andZ represents nitrogen or a --CR.sup.6 group whereR.sup.Type: GrantFiled: July 16, 1992Date of Patent: May 25, 1993Assignee: Bayer AktiengesellschaftInventors: Christa Fest, Ernst R. F. Gesing, Rolf Kirsten, Joachim Kluth, Reinhard Lantzsch, Klaus-Helmut Muller, Theodor Pfister, Hans-Jochem Riebel, Frank Rosenfeldt, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5176716Abstract: Hair dye composition for oxidative dyeing of human or animal hair containing as developing substances alone or in admixture with other developing substances, a hydroxytriaminopyrimidine, preferably 6-OH-2,4,5-triaminopyrimidine (4-OH-2,5,6-triaminopyrimidine) or 2-OH-4,5,6-triaminopyrimidine and/or a dihydroxydiaminopyrimidine, preferably 2,6-dihydroxy-4,5-diamino-pyrimidine or 4,6-dihydroxy-2,5-diaminopyrimidine.Type: GrantFiled: May 21, 1991Date of Patent: January 5, 1993Assignee: Goldwell AGInventors: Heribert Lorenz, Frank Kufner, Jurgen Tennigkeit
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Patent number: 5175292Abstract: A therapeutic method is provided, employing an antiviral compound of the general formula: ##STR1## wherein Z is H, OR' or N(R) .sub.2, wherein R' is H, (C.sub.1 -C.sub.4)alkyl, aryl, CHO, (C.sub.1 -C.sub.16)alkanoyl or O.dbd.P(OH) .sub.2, Y is CH or N, and X is selected from the group consisting of H, N(R) .sub.2, SR, OR' or halogen, wherein R is H, lower (C.sub.1 -C.sub.4)alkyl, aryl or mixtures thereof, and the pharmaceutically acceptable salts thereof.Type: GrantFiled: June 5, 1991Date of Patent: December 29, 1992Assignee: Regents of the University of MinnesotaInventors: Robert Vince, Mei Hua
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Patent number: 5169856Abstract: The present invention relates to unsaturated carboxylic acid amide derivatives of the formula ##STR1## wherein ring A stands for an optionally substituted aromatic ring; R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon residue or forms an optionally substituted carbocyclic ring with the adjacent group --CH.dbd.C-- together with two carbon atoms constituting the ring A; R.sup.2 stands for a hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group; R.sup.3 stands for an optionally substituted hydrocarbon residue; and n denotes an integer ranging from 2 to 6, and salts thereof, as well as the production thereof.The compounds of the present invention act on the central nervous system of mammals and has a strong anti-cholinesterase activity, which can be used for the prophylaxis and therapy of, for example, senile dementia, Alzheimer's diseases, Huntington's chorea, et., and are useful as medicines.Type: GrantFiled: February 6, 1989Date of Patent: December 8, 1992Assignee: Takeda Chemical Industries, Inc.Inventors: Giichi Goto, Akinobu Nagaoka
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Patent number: 5166206Abstract: Substituted pyrimidines, pyrimidinones and pyridopyrimidines of formula (I) are as angiotensin II antagonists useful in the treatment of hypertension, ocular hypertension and certain CNS ailments: ##STR1## wherein K is --N(R.sup.8a)--C(.dbd.M) or --N.dbd.C(R.sup.8b) where M is O or NR.sup.22.Type: GrantFiled: March 27, 1991Date of Patent: November 24, 1992Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, William J. Greenlee, Malcolm MacCoss, Arthur A. Patchett
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Patent number: 5163996Abstract: N-phenyl-sulfonyl-N'-pyrimidinyl- and -triazinyl-ureas of formula I ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.5 alkenyl, C.sub.1 -C.sub.4 haloalkyl, COO--R.sub.2 or A--R.sub.3 ;R.sub.2 is C.sub.1 -C.sub.5 alkyl;R.sub.3 is C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.4 alkoxyalkyl or C.sub.1 -C.sub.5 haloalkyl;X is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkyl mono- to tri-substituted by halogen; C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 alkoxy mono- to tri-substituted by halogen;A is oxygen, sulfur, SO or SO.sub.2 ;Y is halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkyl mono- to tri-substituted by halogen; C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.Type: GrantFiled: August 12, 1991Date of Patent: November 17, 1992Assignee: Ciba-Geigy CorporationInventor: Willy Meyer
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Patent number: 5160363Abstract: The novel compounds of Formula I are active as pre-emergent and/or post-emergent herbicides or plant growth regulants. Some of the compounds of the invention show safety to sugarbeets.Type: GrantFiled: November 2, 1990Date of Patent: November 3, 1992Assignee: E. I. du Pont de Nemours and CompanyInventor: Robert T. Dean
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Patent number: 5157119Abstract: This invention relates to a process for the preparation of a benzene sulfonylurea herbicide by reacting a sulfonyl chloride with a cyanate salt in the presence of a heterocyclic amine, a base and a solvent.Type: GrantFiled: February 20, 1992Date of Patent: October 20, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventors: Onorato Campopiano, Marcus P. Moon
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Patent number: 5157121Abstract: Known herbicides of the formula (I) ##STR1## in which R.sup.1 is alkyl, alkenyl or alkynyl, which are optionally substituted by halogen, alkoxy or alkoxycarbonyl,R.sup.2 is H, alkyl, alkenyl, alkynyl or cycloalkyl,R.sup.3 and R.sup.4 are H or alkyl,R.sup.5 and R.sup.6 are H, alkyl or alkoxy, each of which can be substituted by halogen, alkoxy or alkylthio, or are halogen, alkylthio, alkylamino or dialkylamino,or, if R.sup.2 or R.sup.3 is H, their salts with bases, can be obtained when compounds of the formula IIR.sup.1 --SO.sub.2 --NR.sup.2 --SO.sub.2 --NR.sup.3 --CO--OR.sup.7(II)in whichR.sup.1, R.sup.2 and R.sup.3 are as defined above,are reacted with compounds of the formula III ##STR2## in which R.sup.4, R.sup.5 and R.sup.6 are as defined above andR.sup.7 is alkyl, haloalkyl or optionally substituted phenyl,in an inert organic solvent, to give the compounds of the formula I.Type: GrantFiled: July 17, 1991Date of Patent: October 20, 1992Assignee: Hoechst AktiengesellschaftInventors: Stephen Lachhein, Lothar Willms
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Patent number: 5155222Abstract: Known herbicides of the formula (I) ##STR1## in which R.sup.1 is alkyl, alkenyl or alkynyl, which are optionally substituted by halogen, alkoxy or alkoxycarbonyl,R.sup.2 is H, alkyl, alkenyl, alkynyl or cycloalkyl,R.sup.3 and R.sup.4 are H or alkyl,R.sup.5 and R.sup.6 are H, alkyl or alkoxy, each of which can be substituted by halogen, alkoxy or alkylthio, or are halogen, alkylthio, alkylamino or dialkylamino,or, if R.sup.2 or R.sup.3 is H, their salts with bases, can be obtained when compounds of the formula IIR.sup.1 -SO.sub.2 -NR.sup.2 -SO.sub.2 -NHR.sup.3 (II)in whichR.sup.1, R.sup.2 and R.sup.3 are as defined above,are reacted with compounds of the formula III ##STR2## in which R.sup.4, R.sup.5 and R.sup.6 are as defined above andR.sup.7 is alkyl, haloalkyl or optionally substituted phenyl,in an inert organic solvent, to give the compounds of the formula I.Type: GrantFiled: July 17, 1991Date of Patent: October 13, 1992Assignee: Hoechst AktiengesellschaftInventors: Stephen Lachhein, Lothar Willms