Oxygen Bonded Directly To The Diazine Ring Patents (Class 544/123)
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Patent number: 5250533Abstract: Fungicidal pyridinylpyrimidines of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, alkoxy, alkylthio, halogenoalkyl, amino or dialkylamino, where, in the case of dialkylamino, the two radicals may, together with the nitrogen to which they are bonded, form a 5- to 7-membered, saturated or unsaturated ring which optionally contains a further hetero atom and which is optionally substituted by 1 or 2 alkyl groups; orR.sup.1 represents in each case optionally substituted aryloxy, arylthio, aralkyloxy or aralkylthio,R.sup.2 and R.sup.3 are independent of one another and are identical or different and in each case represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, alkylthio or alkoxycarbonyl,orR.sup.2 and R.sup.3 together represent anaylene chain having 3 to 6 carbon atoms which are linked via the ring positions 3 and 4 or 4 and 5,R.sup.Type: GrantFiled: March 2, 1992Date of Patent: October 5, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Alexander Klausener, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes
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Patent number: 5234923Abstract: Novel compounds are disclosed having the formula ##STR1## or its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.Type: GrantFiled: December 16, 1991Date of Patent: August 10, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Michael A. Poss, Karnail S. Atwal
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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: 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: 5215569Abstract: Substituted pyridines of the formula ##STR1## in which A represents nitrogen or a C-X group where X represents hydrogen or halogen,Q represents oxygen or sulphur,R.sup.1 and R.sup.2 are identical or different and represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxyalkyl, alkoxy, halogenoalkoxy, alkylthio, alkylamino or dialkylamino,R.sup.3 represents hydrogen, amino, nitro, hydroxyl, halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylamino, dialkylamino, alkylcarbonylamino, alkoxycarbonylamino or alkysulphonylamino,R.sup.4 represents hydrogen or alkyl andZ represents oxygen or one of the groups below: ##STR2## where R.sup.5, R.sup.6 and R.sup.7 are defined herein and their use in herbicide compositions.Type: GrantFiled: July 31, 1991Date of Patent: June 1, 1993Assignee: Bayer AktiengesellschaftInventors: Mark W. Drewes, Peter Muller, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5196533Abstract: 6,6-Disubstituted pteridines which are useful for the regulation of enzymes are disclosed, along with a general method of synthesizing these compounds.Type: GrantFiled: March 14, 1991Date of Patent: March 23, 1993Assignee: South Alabama Medical Science Foundation, USAInventors: June E. Ayling, Steven W. Bailey
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Patent number: 5194608Abstract: A dipeptide derivative of formula (I) is provided, which is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure. ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, aryl, or heterocyclic radical;R.sup.2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C.sub.1 -C.sub.12 alkyl-S--, C.sub.1 -C.sub.12 alkyl-S--CH.sub.2 --, or C.sub.3 -C.sub.10 cycloalkyl-S--;R.sup.3 is aryl or 5- or 6-membered heterocyclic radical;R.sup.4 is R.sup.4' --SO.sub.2 or R.sup.4' --CO;R.sup.4' is aryl, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl; C.sub.3 -C.sub.10 cycloalkyl, or heterocyclic radical;X is CH.sub.2, NH, O, or S; andY is CO or NHSO.sub.2, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4' each may be substituted with one to three substituents.Type: GrantFiled: June 24, 1991Date of Patent: March 16, 1993Assignee: Shionogi & Co., Ltd.Inventors: Tatsuo Toyoda, Toshihiro Fujioka, Kunio Hayashi, Masuhisa Nakamura, Naofumi Hashimoto
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Patent number: 5169430Abstract: A compound having the structural formula ##STR1## wherein: R is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, formyl, C.sub.2 -C.sub.6 alkanoyl, C.sub.3 -C.sub.4 alkenyl or C.sub.3 -C.sub.4 alkynyl, or alkali metal;X is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.8 alkoxy, cyano, or halogen;Y is hydrogen, halogen, or C.sub.1 -C.sub.4 dialkylamino;R.sup.1 is hydrogen, C.sub.1 -C.sub.8 straight chain or branched alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 alkoxy or C.sub.3 -C.sub.8 hydroxyalkyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.8 straight chain or branched alkyl, C.sub.3 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, halo substituted C.sub.3 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.1 -C.sub.4 alkoxy, hydroxy C.sub.1 -C.sub.4 alkyl, cyano C.sub.1 -C.sub.4 alkyl, 2,3-epoxypropyl, 2,2-dialkoxyethyl, alkoxyalkyl, phenyl, aralkyl, C.sub.1 -C.sub.4 acyl, C.sub.1 -C.sub.4 carbalkoxyalkyl, C.sub.1 -C.sub.4 carbalkoxyalkyl substituted by C.sub.1 -C.sub.Type: GrantFiled: August 9, 1991Date of Patent: December 8, 1992Assignee: Uniroyal Chemical Company, Inc.Inventors: Richard J. Strunk, Allyn R. Bell
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Patent number: 5167693Abstract: Herbicidal substituted azines of the formula ##STR1## in which m represents the numbers 0, 1, 2 or 3,A represents nitrogen or a C-X group where X represents hydrogen or halogen,Q represents oxygen or sulphur,R.sup.1 and R.sup.2 are identical or different and represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy-alkyl, alkoxy, halogenoalkoxy, alkylthio, alkylamino or dialkylamino,R.sup.3 represents amino, hydroxyl, halogen, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylamino, dialkylamino, alkylcarbonylamino, alkoxycarbonyl-amino or alkylsulphonylamino,R.sup.4 represents hydrogen or alkyl andZ represents N--R.sup.Type: GrantFiled: May 23, 1991Date of Patent: December 1, 1992Assignee: Bayer AktiengesellschaftInventors: Mark W. Drewes, Rolf Kirsten, Wolfgang Kramer, Bernd W. Kruger, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5162326Abstract: Novel pyrimidinedione derivatives of the formula (I): ##STR1## wherein R.sup.1 is hydrogen or a hydrocarbon residue which may be substituted; R.sup.2 is hydrogen, halogen, nitro, optionally substituted amino, formyl or a hydrocarbon residue which may be substituted; R.sup.3 is a hydrocarbon residue which may be substituted; R.sup.4 is hydrogen, halogen or nitro; R.sup.5 is a residue capable of forming an anion or a residue convertible into an anion; X is a direct bond or a spacer having one atomic length and containing an oxygen, nitrogen or sulfur atom; Y is a direct bond or a spacer having atomic length of two or less between the phenylene group and the phenyl group; n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof have potent angiotensin II antagonistic activity and hypotensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes, etc.Type: GrantFiled: February 13, 1991Date of Patent: November 10, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Kohei Nishikawa
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Patent number: 5147876Abstract: 2,6-di-, 2,4,6-, 2,5,6-tri- or 2,4,5,6-tetra-substituted pyrimidines, and 2,6-di-substituted pyridines. These compounds are useful for treatment of neurological diseases.Type: GrantFiled: December 29, 1989Date of Patent: September 15, 1992Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Akira Mizuchi, Kazutoshi Horikomi, Tadayuki Sasaki, Akira Awaya, Ikuo Tomino, Mitsuyuki Takesue, Noriaki Kihara
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Patent number: 5142047Abstract: A composition of polymer molecules effective to bind, with substantially uniform binding affinity, to a single-stranded polynucleotide containing a target sequence of bases. The polymer molecules are composed of a sequence of base-pairing moieties effective to hydrogen bond to corresponding, complementary bases in the target sequence, under selected binding conditions, and a predominantly uncharged, achiral backbone supporting the base-pairing moieties at positions and in orientations which allow hydrogen bonding between the pairing moieties of the polymer and the corresponding complementary bases in the target sequence. The composition has diagnostic uses, in a solid-support assay system, and therapeutic uses involving inhibition or inactivation of target polynucleotides.Type: GrantFiled: September 23, 1987Date of Patent: August 25, 1992Assignee: Anti-Gene Development GroupInventors: James Summerton, Dwight Weller, Eugene Stirchak
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Patent number: 5135563Abstract: The present invention relates to a pyrimidine derivative having the formula ##STR1## (wherein the variables are defined in the full text of the patent), a method for producing the same, and its use as a herbicide.Type: GrantFiled: July 5, 1991Date of Patent: August 4, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saitoh, Hideyuki Shibata
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Patent number: 5130317Abstract: Pyrimidine-4,6-dicarboxylic acid diamides, processes for the use thereof, and pharmaceuticals based on these compoundsThe invention relates to pyrimidine-4,6-dicarboxylic acid diamides of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The compounds according to the invention inhibit proline hydroxylase and lysine hydroxylase and can be employed as fibrosuppressants and immunosuppressants.Type: GrantFiled: September 19, 1990Date of Patent: July 14, 1992Assignee: Hoechst AktiengesellschaftInventors: Ekkehard Baader, Martin Bickel, Volkmar Gunzler-Pukall, Stephan Henke
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Patent number: 5125957Abstract: A pyrimidine derivative represented by the formula ##STR1## wherein the variables are defined below in the specification, and their production and herbicidal activities are described.Type: GrantFiled: October 24, 1990Date of Patent: June 30, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
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Patent number: 5120843Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).Type: GrantFiled: October 23, 1989Date of Patent: June 9, 1992Assignee: UpjohnInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
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Patent number: 5102444Abstract: This invention relates to herbicidal pyridine-sulfonylureas which are highly active as preemergence and postemergence herbicides.Type: GrantFiled: April 12, 1990Date of Patent: April 7, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Paul H. Liang
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Patent number: 5102884Abstract: A substituted benzoylurea compound of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a halogen atom or a nitro group, each of R.sup.2 and R.sup.3 is a hydrogen atom, an alkyl group, --COR.sup.6 (wherein R.sup.6 is an alkyl group or an alkoxy group) or --SO.sub.2 R.sup.6 (wherein R.sup.6 is as defined above), or R.sup.2 and R.sup.3 may form together with the adjacent nitrogen atom a heterocyclic ring, R.sup.4 is a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkylthio group or a nitro group, and R.sup.5 is a halogen atom, a nitro group or a substituted or unsubstituted alkyl group, or its salt.Type: GrantFiled: July 19, 1990Date of Patent: April 7, 1992Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Takahiro Haga, Nobutoshi Yamada, Hideo Sugi, Toru Koyanagi, Hiroshi Okada
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Patent number: 5093336Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: July 6, 1989Date of Patent: March 3, 1992Assignee: Hoechat-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Bettina Spahl
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Patent number: 5093492Abstract: Methine dyes of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, Y and the rings A and B each have specific meanings, and methine dyes obtainable by reacting an organic mono- or polyisocyanate with such a methine dye of the abovementioned formal where only the radicals R.sup.1 and/and R.sup.4 have a group reacting with an organic mono- or polyisocyanate are useful in optical recording media.Type: GrantFiled: August 7, 1990Date of Patent: March 3, 1992Assignee: BASF AktiengesellschaftInventors: Michael Acker, Mathias Dust, Peter Neumann, Sibylle Brosius, Klaus D. Schomann, Harald Kuppelmaier
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Patent number: 5084459Abstract: There is provided a pest control composition containing a compound represented by the formula, ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and independently mean a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted and X means an electron attracting group or a salt thereof.The compounds are of minimal toxicity to man, domestic animals and fish and selectively display remarkable control effect on pests.Type: GrantFiled: October 25, 1989Date of Patent: January 28, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Isao Minamida, Tetsuo Okauchi, Noriko Higuchi
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Patent number: 5075316Abstract: Novel compounds of the formula ##STR1## in which: R.sub.1 and R.sub.2 independently of one another are hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.2 halogenoalkyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 halogenoalkoxy; R.sub.3 is C.sub.3 -C.sub.6 cycloalkyl or C.sub.3 -C.sub.6 cycloalkyl which is substituted by up to three identical or different methyl or halogen groups; R.sub.4 is halogen, thiocyano, --OR.sub.5, --SR.sub.5 or --NR.sub.5 R.sub.6, in which R.sub.5 and R.sub.6 are halogen groups; R.sub.4 is halogen, thiocyano, --OR.sub.5, --SR.sub.5 or --NR.sub.5 R.sub.6, in which R.sub.5 and R.sub.6 are as defined herein, are novel active compounds for preventing attack of plants by microorganisms. The compounds can be employed as microbicides as such or in the form of suitable agents.Type: GrantFiled: March 20, 1990Date of Patent: December 24, 1991Assignee: Ciba-Geigy CorporationInventor: Adolf Hubele
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Patent number: 5073544Abstract: This invention provides compositions for enhancing penetration of physiologically active agents through the skin or mucosal membranes and for retaining these agents in body tissues, said composition comprising effective amounts of a physiologically-active agent and a compound represented by the general formula ##STR1## wherein X may represent sulfur, oxygen or nitrogen; a and b may be 0 or 1, c may be 0, 1 or 2, except that when X is oxygen, a, b and c are 0, when X is nitrogen c is 0 and only one of a or b is 1, and when X is sulfur a and b are 0; A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl; and R is hydrogen or a lower alkyl group having from 1 to 4 carbon atoms, ##STR2## wherein R" is H orType: GrantFiled: March 23, 1989Date of Patent: December 17, 1991Assignee: Whitby, Inc.Inventors: James V. Peck, Gevork Minaskanian
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Patent number: 5064826Abstract: This invention relates to novel triazolopyrimidine derivatives of formulae (Ia) and (Ib), ##STR1## wherein Q represents hydrogen, a heterocyclic group optionally substituted by a C.sub.1-4 alkyl group and containing one or more oxygen and/or nitrogen atoms or a group of formula--SR.sup.1 wherein R.sup.1 is alkyl or aralkyl, or a group of formula--NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl or a heterocyclic group,m and n are independently 0, 1, 2, 3 or 4, with the provision that if m stands for 0, then n is different from 0, and if both n and m are 1 or m stands for 0 and n is 2, the Q is different from methylthio or morpholino group, their mixtures or pharmaceutically acceptable salts. Furthermore, the invention relates to a process for preparing these compounds.The compounds of formulae (Ia) and (Ib) are able to inhibit the ptosis caused by tetrabenazine and they have analgetic activity.Type: GrantFiled: March 2, 1990Date of Patent: November 12, 1991Inventors: Klara Reiter nee Esses, Jozsef Reiter, Zoltan Budai, Endre Rivo, Peter Trinka, Lujza Petocz, Gabor Gigler, Istvan Gyertyan, Istvan Gacsalyi
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Patent number: 5053072Abstract: Compounds of the formula I or salts thereof ##STR1## where R.sup.1 is H or an aliphatic radical; R.sup.2 and R.sup.3 are H, alkyl or phenyl; W is O, S, NR.sup.4 or NOR.sup.4 ; X is CHR.sup.2, O or NR.sup.4 ; L is a (substituted) phenyl, naphthyl or monocyclic heteroaryl radical, A is a (substituted) pyrimidyl, triazinyl, triazolyl or bicyclic heteroaryl radical, and m and n are 0 or 1, have advantageously herbicidal or plant growth-regulating properties.Type: GrantFiled: July 31, 1989Date of Patent: October 1, 1991Assignee: Hoechst AktiengesellschaftInventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz
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Patent number: 5047409Abstract: Salts of thiazolidine-4-carboxylic acids with 6-Piperidino-2,4-diaminopyrimidine-3-oxide are described of Formula I. ##STR1## Compounds I are useful in the field of cosmetics and pharmaceuticals for the treatment of loss of hair or in pathological forms such as alopecia, flaking dermatitis, etc. . . . Topical formulations containing compounds I are also described.Type: GrantFiled: May 21, 1986Date of Patent: September 10, 1991Assignee: Serono OTC S.A.Inventors: Michele G. Di Schiena, Vittoria Orru
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Patent number: 5043337Abstract: Insecticidal pyrimidin-4-yl carbamates of the formula ##STR1## in which R.sup.1 represents alkoxy, alkylthio, alkylthioalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl or dialkylamino,R.sup.2 represents hydrogen or alkyl,R.sup.3 represents hydrogen, alkyl or alkoxy orR.sup.2 and R.sup.3 together represent a double-linked alkanediyl radical,R.sup.4 represents hydrogen or alkyl,R.sup.5 represents hydrogen or alkyl andA represents oxygen, sulphur or a radical ##STR2## where R.sup.6 represents alkyl.Type: GrantFiled: April 4, 1990Date of Patent: August 27, 1991Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Kurt Findeisen, Jurgen Hartwig, Benedikt Becker
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Patent number: 5043443Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.Type: GrantFiled: July 24, 1990Date of Patent: August 27, 1991Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
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Patent number: 5032166Abstract: The invention relates to certain 6-amino-substituted 2-pyridinesulfonylureas, intermediates thereof, and compositions and methods of their use.Type: GrantFiled: February 9, 1990Date of Patent: July 16, 1991Assignee: E. I. du Pont de Nemours and CompanyInventor: Eric D. Taylor
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Patent number: 5032167Abstract: Substituted sulfonylureas of the formula I ##STR1## where the substituents and indices have the following meanings: x is oxygen or sulfur;z is nitrogen or methine (=CH--);R.sup.1 is halogen or substituted or unsubstituted C.sub.1 -C.sub.4 -alkoxycarbonyl or C.sub.1 -C.sub.3 -alkoxy, or a radical --CONR.sup.6 R.sup.7, whereR.sup.6 is hydrogen, C.sub.1 -C.sub.8 -alkyl or C.sub.1 -C.sub.6 -alkoxy andR.sup.7 is hydrogen or C.sub.1 -C.sub.8 -alkyl;R.sup.2 is halogen or substituted or unsubstituted C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -alkyl;R.sup.3 is C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -haloalkylthio, halogen, cyano, nitro, amino, mono-C.sub.1 -C.sub.4 -alkylamino, di-C.sub.1 -C.sub.4 -alkylamino, C.sub.2 -C.sub.6 -alkenyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, C.sub.1 -C.sub.Type: GrantFiled: December 12, 1989Date of Patent: July 16, 1991Assignee: BASFInventors: Horst Mayer, Gerhard Hamprecht, Bruno Wuerzer, Karl-Otto Westphalen
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Patent number: 5026418Abstract: Pyrimidine compounds useful as plant growth regulators have the formula (I): ##STR1## wherein Y is an optionally substituted secondary or tertiary alkyl group containing from 3 to 7 carbon atoms or an optionally substituted cycloalkyl or alkylcycloalkyl group containing from 3 to 7 carbon atoms; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or a lower alkyl group; A is an optionally substituted heterocyclic group, for example thienyl or pyridyl; n is an integer which may be from 0 to 2 and is preferably 0; and R.sup.3 is hydrogen, an alkyl group containing from 1 to 4 carbon atoms, or an alkenyl or alkynyl group containing from 2 to 4 carbon atoms.Type: GrantFiled: February 20, 1990Date of Patent: June 25, 1991Assignee: Imperial Chemical Industries PLCInventor: Kevin R. Lawson
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Patent number: 5022915Abstract: 2,4-Diarylpyrimidines of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## R.sub.1 and R.sub.2 are independently selected from the group consisting of H, Br, Cl, F, C.tbd.N, CF.sub.3 and OCF.sub.3 ;R.sub.3 is selected from the group consisting of H, C.sub.1 -C.sub.4 alkyl, CO.sub.2 CH.sub.3, CO.sub.2 CH.sub.2 CH.sub.3, CH.sub.2 Cl, CH.sub.2 OCH.sub.3, CH.dbd.CH.sub.2, C.sub.1 -C.sub.3 thioalkyl, and C.sub.1 -C.sub.3 alkoxy;R.sub.4 is selected from the group consisting of H, --OH, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 thioalkyl, C.sub.1 -C.sub.3 alkoxy; andR.sub.5 is selected from the group consisting of H and F are useful as herbicidal agents.Type: GrantFiled: March 1, 1990Date of Patent: June 11, 1991Assignee: ICI Americas Inc.Inventor: Michael P. Prisbylla
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Patent number: 5017211Abstract: The invention is concerned with novel compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the significances given in the description, as well as enol ethers and salts thereof and their manufacture, weed control compositions which contain such compounds as the active substance and the use of the active substances or compositions for the control of weeds. The invention is also concerned with certain novel starting materials and their production.Type: GrantFiled: May 19, 1989Date of Patent: May 21, 1991Assignee: Ciba-Geigy CorporationInventors: Jean Wenger, Paul Winternitz, Martin Zeller
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Patent number: 5015284Abstract: Compounds of the formula I, their stereoisomers or their salts ##STR1## wherein A denotes >C(R.sup.4).sub.2 or >C.dbd.C(R.sup.5).sub.2 ; R.sup.1 denotes H, an optionally substituted aliphatic or cycloaliphatic radical, forfuryl, tetrahydrofurfuryl or (substituted) phenyl; R.sup.2 denotes H, alkyl, alkenyl, alkynyl or alkoxy; R.sup.3 denotes a radical of the formulae ##STR2## X denotes O, S or NR.sup.12 and Y denotes O or S, possess excellent herbicidal and plant-growth regulating properties.Type: GrantFiled: April 6, 1989Date of Patent: May 14, 1991Assignee: Hoechst AktiengesellschaftInventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 4987135Abstract: A substituted benzene derivative represented by a formula: ##STR1## where A represents: ##STR2## wherein X is a hydrogen atom, a halogen atom or a nitro group, R.sup.1 is --X.sup.1 Z.sup.1 (X.sup.1 is an oxygen atom or a sulfur atom and Z.sup.1 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group), --COZ.sup.1 group (Z.sup.1 is as defined above), ##STR3## group (Z.sup.1 is as defined above, Z.sup.2 is --CO.sub.2 Z.sup.3 wherein Z.sup.3 is the same as Z.sup.1, or --SO.sub.2 Z.sup.3 wherein Z.sup.3 is as defined above and n is 0 or 1), ##STR4## (Z.sup.1 and Z.sup.3 are as defined above) or ##STR5## (X.sup.2, X.sup.3 and X.sup.4 are, respectively, an oxygen atom or a sulfur atom and Z.sup.4 and Z.sup.5 are the same as Z.sup.1), and R.sup.3 is a nitro group or ##STR6## (R.sup.4 and R.sup.Type: GrantFiled: March 16, 1989Date of Patent: January 22, 1991Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Takahiro Haga, Nobutoshi Yamada, Hideo Sugi, Toru Koyanagi, Hiroshi Okada
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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: 4975433Abstract: A compound of the formula: ##STR1## wherein: R and R.sub.1 may be the same or different and are selected from the group consisting of H; cycloalkyl groups having up to 10 carbon atoms; or straight or branched chain alkyl, alkenyl or alkynyl of 1 to 10 carbon atoms;R.sub.2 and R.sub.3 together with the nitrogen atom to which they are bonded form a pyrrolidine, piperidine, N-methyl piperazine, piperazine or morpholine ring;or a non-toxic pharmaceutically acceptable salt, adduct, oxide or other derivative thereof; and pharmaceutical compositions adapted for topical administration to a human or non-human animal and methods of topically administering the compositions to humans and non-human animals.Type: GrantFiled: January 31, 1989Date of Patent: December 4, 1990Assignee: University of FloridaInventor: Kenneth B. Sloan
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Patent number: 4962109Abstract: This invention provides novel insecticidally and acaricidally active pyrimidine derivatives of formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is selected from alkyl; alkenyl; alkynyl; haloalkyl; haloalkenyl; and cycloalkyl optionally substituted by alkyl or halogen;R.sup.2 is selected from alkyl; haloalkyl; alkoxy; alkylamino; dialkylamino; halogen; cycloalkyl optionally substituted by halogen or alkyl; and phenyl optionally substituted by alkyl, haloalkyl, halogen or alkoxy;R.sup.3 is selected from hydrogen and halogen;R.sup.4 is the residue of an alcohol of formula R.sup.4 --OH which forms an insecticidal ester when combined with chrysanthemic acid, permethrin acid or cyhalothrin acid; andX is selected from oxygen and sulphur.Type: GrantFiled: June 13, 1988Date of Patent: October 9, 1990Assignee: Imperial Chemical Industries PLCInventors: Edward McDonald, Roger Salmon, Alan J. Whittle
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Patent number: 4960777Abstract: Heteroaryloxy-.beta.-carboline derivatives of general Formula I ##STR1## wherein R.sup.1 is an optionally substituted heteroaryl residue,R.sup.2 is hydrogen, lower alkyl or lower alkoxyalkyl,X is a COOR.sup.3 -group wherein R.sup.3 means H or lower alkyl, or represents a CONR.sup.4 R.sup.5 -group wherein R.sup.4 and R.sup.5 mean respectively hydrogen or lower alkyl, R.sup.4 and R.sup.5 being capable of forming, together with the nitrogen atom, a 5- to 6-membered heterocycle, or means an oxadiazolyl residue of the formula ##STR2## wherein R.sup.6 means hydrogen, lower alkyl or cycloalkyl, are valuable pharmaceuticals.Type: GrantFiled: September 20, 1989Date of Patent: October 2, 1990Assignee: Schering AktiengesellschaftInventors: Helmut Biere, Andreas Huth, Dieter Rahtz, Ralph Schmiechen, Dieter Seidelmann, David Stephens, Mogens Engelstoft, John B. Hansen
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Patent number: 4957921Abstract: Substituted cyclohexanols are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: December 6, 1989Date of Patent: September 18, 1990Assignee: Warner-Lambert CompanyInventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
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Patent number: 4958043Abstract: A composition useful for incorporation into polymer compositions employed for food packaging or the like comprising a bis- or tris-methine compound having the structural formula ##STR1## wherein A is selected from the radicals ##STR2## wherein R' and R" are each selected from chlorine, bromine, fluorine, alkyl, alkoxy, aryl, aryloxy and arylthio;each n is independently 0, 1, 2;R.sub.1 is selected from a large variety of radicals such as cycloalkyl, phenyl, and straight or branched alkyl which may be substituted;R.sub.2 is alkylene or the like;R.sub.3, R.sub.4, and R.sub.5 are each selected from hydrogen and alkyl; andP and Q and P.sup.1 and Q.sup.1 are selected from cyano, carbalkoxy, carbaryloxy, carbaralkyloxy, or the like.The invention compositions are especially useful in combination with molding or fiber-grade condensation polymer; most preferably such polymer having copolymerized therein a total of from 1.Type: GrantFiled: April 18, 1988Date of Patent: September 18, 1990Assignee: Eastman Kodak CompanyInventors: Max A. Weaver, Wayne P. Pruett, Samuel D. Hilbert
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Patent number: 4956366Abstract: Substituted thienoimidazole derivatives, a process for the preparation thereof, pharmaceutical compositions containing them, and the use thereof as inhibitors of gastric acid secretion, as gastroprotectives and as medicaments for intestinal inflammationsThe invention relates to compounds of the formula ##STR1## in which A represents ##STR2## T denotes --S--, --SO-- or --SO.sub.2 --, R.sup.1 to R.sup.10, X, Y and Z have the meanings indicated in the description, to a process for the preparation thereof, to pharmaceutical compositions containing them, and to the use thereof as inhibitors of gastric acid secretion, as gastroprotectives and as medicaments for intestinal inflammations.Type: GrantFiled: July 13, 1988Date of Patent: September 11, 1990Assignee: Hoechst AktiengesellschaftInventors: Hildegard Nimmesgern, Klaus Weidmann, Hans-Jochen Lang, Robert Rippel, Andreas W. Herling
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Patent number: 4948416Abstract: This invention relates to novel condensed ring sulfonylureas and their use as herbicides and growth regulants.Type: GrantFiled: March 27, 1989Date of Patent: August 14, 1990Assignee: E. I. du Pont de Nemours and CompanyInventor: Robert J. Pasteris
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Patent number: 4945093Abstract: A compound having formula: ##STR1## is described, where R.sub.3 and R.sub.4 may be identical or different and represent a hydrogen atom, alkyl, alkenyl, cycloalkyl;or R.sub.3 and R.sub.4 represent aryl aralkyl;or R.sub.3 and R.sub.4 together with the nitrogen atom linked thereto form a heterocycle;R.sub.1 and/or R.sub.2, independent of each other, represent hydrogen or carbanoyl having formula: ##STR2## where R.sub.7 represents alkyl, alkenyl, cycloalkyl, aryl or aralkyl. The compounds of formula (I) can be used in cosmetic or pharmaceutical compositions for the cosmetic treatment of hair, the treatment of alopecia, and also for the treatment of desquamating dermatitis.Type: GrantFiled: July 29, 1988Date of Patent: July 31, 1990Assignee: L'OrealInventors: Jean Maignan, Serge Restle, Gerard Lang
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Patent number: 4940792Abstract: Novel substituted N-sulfonyl-N'-pyrimidinylureas or N-sulfonyl-N'-triazinylureas of the formula I ##STR1## have good pre- and postemergence selective herbicidal and growth regulating properties.In this formulaE is nitrogen or --CH.dbd.,the group ##STR2## is a phenyl, naphthyl, furyl, thiophenyl, pyrrole or pyridinyl radical which is substituted in accordance with the definitions ofR.sup.1 and R.sup.2,R.sup.3 and R.sup.4 are hydrogen, lower alkyl or lower alkoxy, or one of R.sup.3 and R.sup.4 may also be halogen, lower alkenyl, lower haloalkenyl, lower haloalkoxy, amino, lower alkylamino, --CH(OCH.sub.3).sub.2, a cyclized ketal group or a saturated 5- or 7-membered heterocycle which is bound through the nitrogen atom,R.sup.5 is hydrogen, lower alkyl, lower haloalkyl, or an unsubstituted or substituted phenyl, benzyl or naphthyl radical, andR.sup.Type: GrantFiled: December 4, 1987Date of Patent: July 10, 1990Assignee: Ciba-Geigy CorporationInventors: Werner Topfl, Willy Meyer, Hans-Dieter Schneider
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Patent number: 4929726Abstract: A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof.The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product.Type: GrantFiled: February 9, 1988Date of Patent: May 29, 1990Assignee: Georgia State University Foundation, Inc.Inventors: Lucjan Strekowski, Maria Mokrosz, Donald B. Harden
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Patent number: 4921527Abstract: The invention relates to sulfonylurea compounds with a substituted or unsubstituted bicyclic nine-membered ring having one to five heteroatoms which are preemergent and/or postemergent herbicides or plant growth regulants.Type: GrantFiled: May 4, 1988Date of Patent: May 1, 1990Assignee: E. I. du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4920134Abstract: Novel compounds having the formula: ##STR1## wherein ##STR2## represents a nitrogen-containing aromatic 6-membered ring; R.sup.1 represents a higher alkyl group which may be substituted; R.sup.2 represents a tertiary amino group or a quaternary ammonium group; and m represents 2 or 3; and salts thereof have superior antitumor activities including differentiation-inducing activity, and are useful as antitumor agents.Type: GrantFiled: August 3, 1988Date of Patent: April 24, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Eiko Imamiya
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Patent number: 4908056Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: February 17, 1989Date of Patent: March 13, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4906283Abstract: This invention relates to herbicidally active sulfonamide compounds having a heterocyclic carbonyl group ortho to the sulfonyl bridge.Type: GrantFiled: April 25, 1988Date of Patent: March 6, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joel R. Christensen