Nitrogen Patents (Class 562/430)
-
Patent number: 5463083Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i,e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.Type: GrantFiled: January 6, 1994Date of Patent: October 31, 1995Assignee: Cytomed, Inc.Inventors: Tesfaye Biftu, Xiong Cai, Sajjet Hussion, Gurmit Grewal, T. Y. Shen
-
Patent number: 5463115Abstract: Novel bleach catalysts, a method for bleaching substrates using these catalysts and detergent compositions containing the catalysts are reported. The catalysts are sulfonimines. Substrates such as fabrics may be bleached in an aqueous solution containing the sulfonimine and a peroxygen compound.Type: GrantFiled: July 16, 1991Date of Patent: October 31, 1995Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: David J. Batal, Stephen A. Madison
-
Patent number: 5457131Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.Type: GrantFiled: August 18, 1994Date of Patent: October 10, 1995Assignee: Allergan, Inc.Inventor: Steven W. Andrews
-
Patent number: 5442104Abstract: The present invention provides inhibitors of kynureninase having the formula ##STR1## where X is CHOH, S, SO.sub.2, SO, SONH.sub.2, PO.sub.2 H or PONH.sub.2, R.sub.a and R.sub.b, independently of one another are H, a halogen, CF.sub.3 or a small alkyl group having one to three carbon atoms; R.sub.1 is H, NH.sub.2, NR.sub.6 RT, NO.sub.2, halogen, CF.sub.3 or a small alkyl group having from one to three carbon atoms, wherein: R.sub.6 and R.sub.7, independently of one another, are H, a formyl group or a small alkyl group having from one to three carbon atoms with the exception that only one of R.sub.6 or R.sub.7 can be a formyl group; R.sub.2 is OH, H, halogen, CF.sub.3 or a small alkyl group having from one to three carbon atoms; and R.sub.3, R.sub.4 and R.sub.5, independently of one another, are H, halogen, CF.sub.3, NO.sub.2, NH.sub.2, or small alkyl group having from one to three carbon atoms. In particular, compounds of this formula in which X is CHOH, S or SO.sub.2 are provided.Type: GrantFiled: January 21, 1994Date of Patent: August 15, 1995Assignee: University of Georgia Research Foundation, Inc.Inventors: Robert S. Phillips, Rajesh K. Dua
-
Patent number: 5436343Abstract: Compounds of formula (I): ##STR1## in which: R.sub.1 and R.sub.2, which may be identical or different, represent a linear or branched (C.sub.1 C.sub.6) alkyl radical, a substituted or unsubstituted phenyl radical, a pyridyl radical or a thienyl radical, or, with the carbon atom to which they are attached, a substituted or unsubstituted (C.sub.4 -C.sub.7) cycloalkyl ring,R.sub.3 representsa substituted or unsubstituted phenylsulfonyl radical,a linear or branched (C.sub.1 -C.sub.6) alkyl radical,an alkylaminocarbonyl radical,or a linear or branched (C.sub.1 -C.sub.6) acyl radical,R.sub.4 represents any one of the radicals:--CH.dbd.CH--(CH.sub.2).sub.p --CO.sub.2 H or --CH.sub.2 --CH.sub.2 --(CH.sub.2)p--CO.sub.2 Hin which p is equal to 0, 1, 2 or 3, n and m, which may be identical or different, represent 0, 1 or 2,their isomers, enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid or base.Type: GrantFiled: May 14, 1993Date of Patent: July 25, 1995Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Michel Laubie, Tony Verbeuren
-
Patent number: 5424280Abstract: There are provided aryloxybenzene compounds of formula I ##STR1## Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.Type: GrantFiled: October 7, 1993Date of Patent: June 13, 1995Assignee: American Cyanamid CompanyInventors: Michael E. Condon, Alvin D. Crews, Jr.
-
Patent number: 5424481Abstract: A process for preparing methylsulfonylbenzoic acids comprises oxidizing the corresponding methylsulfonyltoluenes with nitric acid and air in sulfuric acid in the presence of vanadium or cobalt compounds.Type: GrantFiled: October 13, 1993Date of Patent: June 13, 1995Assignee: BASF AktiengesellschaftInventor: Helmut Hagen
-
Patent number: 5424334Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions--of such phenyl amidines derivatives.Type: GrantFiled: December 19, 1991Date of Patent: June 13, 1995Assignee: G. D. Searle & Co.Inventors: Norman A. Abood, Robert B. Garland, Masateru Miyano
-
Patent number: 5409939Abstract: This invention relates to compounds having the following formula ##STR1## which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine thio derivatives.Type: GrantFiled: February 12, 1993Date of Patent: April 25, 1995Assignee: G. D. Searle & Co.Inventors: Steven P. Adams, Richard J. Lindmark, Masateru Miyano, Joseph G. Rico
-
Patent number: 5407951Abstract: The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5-C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m --radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 -alkylene radical, whereby a methylene radical --CH.sub.Type: GrantFiled: June 30, 1992Date of Patent: April 18, 1995Assignee: Boehringer Mannheim GmbHInventors: Ernst-Christian Witte, Karlheinz Stegmeier, Liesel Doerge
-
Patent number: 5405993Abstract: There are described formazan dyes of the formula ##STR1## where n is 1 or 2,Kat.cndot. is the equivalent of a cation,Me is copper or nickel,X is a radical of the formula CO-O or SO.sub.2 -O,Y is vinyl or a radical of the formula C.sub.2 H.sub.4 -Q, where Q is a group which is detachable under alkaline reaction conditions,the ring A may be substituted and benzofused,the ring B is substituted and may be benzofused, andthe ring C may be substituted,the use thereof for dyeing or printing hydroxyl- or nitrogen-containing organic substrates, and novel hydrazones.Type: GrantFiled: August 9, 1994Date of Patent: April 11, 1995Assignee: BASF AktiengesellschaftInventors: Claus Marschner, Manfred Patsch
-
Patent number: 5405988Abstract: The invention relates to 9-substituted bicyclo[3.3.0]octane derivatives of formula I, ##STR1## and their salts with physiologically compatible bases, as well as the .alpha.-, .beta.- or .gamma.-cyclodextrin clathrates, as well as the compounds of formula I encapsulated with liposomes, process for their production and their pharmaceutical use.Type: GrantFiled: June 11, 1993Date of Patent: April 11, 1995Assignee: Schering AktiengesellschaftInventors: Ulrich Klar, Helmut Vorbruggen, Hartmut Rehwinkel, Karl Thierauch, Peter Verhallen
-
DNA gyrase inhibitors, process for their manufacture and pharmaceutical preparations containing same
Patent number: 5399741Abstract: Compounds of the formula ##STR1## in which P is hydroxy and T is the group -X.sup.2 -CR.sup.7a R.sup.7b -CHR.sup.8 -OH or T is hydrogen and P is the group O-CHR.sup.8 -CR.sup.7a R.sup.7b -X.sup.2 -OH and, wherein X.sup.1, X.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7a, R.sup.7b, and R.sup.8 are as defined in the specification,or a reactive derivative thereof. These compounds are useful in the preparation of DNA gyrase inhibitors.Type: GrantFiled: January 6, 1994Date of Patent: March 21, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Mikio Arisawa, Erwin Gotschi, Paulfaello Hebeisen, Tsutomu Kamiyama, Helmut Link, Raffaello Masciadri, Hisao Shimada, Junko Watanabe -
Patent number: 5399748Abstract: Arylsulfonamide derivatives of .alpha.-amino dicarboxylic acids such as aspartic acid and glutamic acid posses anti-cholecystokinin activity. They are useful in the treatment of cholecystokinin-related disorders such as anorexia nervosa, pancreatic inflammation, biliary tract disease, Zollinger-Ellison syndrome and various psychiatric disorders, as well as in the potentiation of opiate analgesia, and in the treatment of certain cancers.Type: GrantFiled: January 12, 1993Date of Patent: March 21, 1995Assignee: James Black Foundation LimitedInventors: Howard B. Broughton, Sarkis B. Kalindjian, Caroline M. R. Low, Iain M. McDonald, Robert A. D. Hull, Nigel P. Shankley
-
Patent number: 5393921Abstract: A process for synthesizing O-substituted oxime compounds, which includes (a) reacting an alkali metal or alkaline earth metal hydroxide compound and a solution of an oxime compound to form a first mixture including the alkali metal or alkaline earth metal salt of the oxime compound and water; and (b) adding an organohalide compound while stirring to the first mixture to form a second mixture including an O-substituted oxime compound, the alkali metal or alkaline earth metal salt of the oxime compound, water, unreacted organohalide compound and excess oxime compound. The second mixture is heated in the presence of an amount of water sufficient to react hydroxide with the unreacted organohalide compound to obtain an O-substituted oxime compound substantially free of unreacted organohalide compound.In a further embodiment, the O-substituted oxime compound can be hydrolyzed to the corresponding O-substituted hydroxylamine.Type: GrantFiled: July 7, 1993Date of Patent: February 28, 1995Assignee: The Gillette CompanyInventor: Harvey A. Lazar
-
Patent number: 5389682Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.Type: GrantFiled: September 13, 1993Date of Patent: February 14, 1995Assignee: Warner-Lambert CompanyInventors: Bradley D. Tait, Michael W. Wilson
-
Patent number: 5387594Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: August 4, 1992Date of Patent: February 7, 1995Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, William R. Pilgrim
-
Patent number: 5387608Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.Type: GrantFiled: August 17, 1993Date of Patent: February 7, 1995Assignee: Allergan, Inc.Inventor: Steven W. Andrews
-
Patent number: 5385917Abstract: Carboxylic acid derivatives of the formula: ##STR1## are provided, which are useful for treatment of androgen dependent diseases.Type: GrantFiled: July 16, 1993Date of Patent: January 31, 1995Assignee: Mitsubishi Kasei CorporationInventors: Hiroaki Ueno, Masahiko Morioka, Fumiko Hatanaka
-
Patent number: 5385931Abstract: The invention relates to new sulphonamide derivatives of benzo-cyclic or benzo-heterocyclic acids and their derivatives of general formula I ##STR1## in which: R represents a straight-chain or branched lower alkyl radical having 1 to 9 C;a phenyl radical which is unsubstituted or substituted by one or more groups:straight-chain or branched lower alkyl having 1 to 4 C, halogeno, alkoxy, nitro, amino, dialkylamino or CF.sub.3 ;a substituted or unsubstituted naphthalene;a thiophenyl radical;R.sub.1 represents a hydrogen or a straight-chain or branched lower alkyl or a benzyl;R.sub.2 represents a hydrogen, a straight-chain or branched lower alkyl group, a substituted or unsubstituted phenyl group or an aralkyl group;R.sub.3 represents a hydrogen or a straight-chain or branched lower alkyl (1 to 6 C);--X-- represents a divalent functional radical chosen from the following: --CH.sub.2 --; ##STR2## where R.sub.Type: GrantFiled: December 28, 1990Date of Patent: January 31, 1995Assignee: Pierre Fabre MedicamentInventors: Dennis Bigg, Alain Duflos, Jean-Pierre Rieu
-
Patent number: 5380941Abstract: A process for preparing ureas of the formula ##STR1## where the ring A can be substituted and benzo-fused andn is 0 or 2,R.sup.4 and R.sup.5 are hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,L is unsubstituted or substituted C.sub.2 -C.sub.4 -alkylene, or NR.sup.5 and L are together the radical of the formula ##STR2## and Z is hydroxyl or a radical which can be eliminated under alkaline reaction conditions,by reacting a phenylurea of the formula ##STR3## where R.sup.4 and the ring A each have the abovementioned meanings, with an amine of the formula ##STR4## where n, R.sup.5, L and Z each have the abovementioned meanings, at from 80.degree. to 180.degree. C. in the presence or absence of an inert diluent is described.Type: GrantFiled: October 1, 1993Date of Patent: January 10, 1995Assignee: BASF AktiengesellschaftInventors: Bernd Siegel, Manfred Patsch
-
Patent number: 5362902Abstract: Compounds of formula (I) are diuretic agents for treating various cardiovascular diseases including hypertension, heart failure and renal insufficiency.Type: GrantFiled: July 21, 1992Date of Patent: November 8, 1994Assignee: Pfizer Inc.Inventors: Ian T. Barnish, Keith James
-
Patent number: 5360909Abstract: Disclosed are phenoxyacetic acid compounds of formula (I): ##STR1## where X is a hydrogen atom, a lower alkyl group or a halogen atom;R1 is a carboxyl group or a lower alkoxycarbonyl group;Y is an oxygen atom, ##STR2## n is an integer of from 0 to 5; Z is ##STR3## R2 is a hydrogen atom or a lower alkyl group; and m is 0 or 1.The compounds and their physiologically acceptable salts are used as thromboxane A2 antagonistic agents, leukotriene antagonistic agents and/or anti-allergic agents.Type: GrantFiled: March 22, 1993Date of Patent: November 1, 1994Assignee: Terumo Kabushiki KaishaInventors: Azuma Igarashi, Sachiko Maeda, Katuyoshi Sugizaki, Takashi Shizawa, Atsumi Tajima, Kenichi Abe, Shinji Ozawa
-
Patent number: 5359135Abstract: The present invention relates to monoclonal antibodies that are distinguished by a high degree of selectivity and affinity towards triasulfurone and that are therefore outstandingly suitable for use in an immunoassay for the rapid and effective detection of triasulfurone. The present invention relates also to hybridoma cell lines that produce the said monoclonal antibodies and to immunological methods for the detection of triasulfurone in soil, water or air samples using the said monoclonal antibodies and to test kits that may be used in those detection methods.Type: GrantFiled: November 29, 1993Date of Patent: October 25, 1994Assignee: Ciba-Geigy CorporationInventors: Jean-Marc Schlaeppi, Klaus Ramsteiner, Willy Meyer
-
Patent number: 5358956Abstract: Novel fibrinogen receptor antagonists of the formula: ##STR1## are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.Type: GrantFiled: October 14, 1992Date of Patent: October 25, 1994Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Wasyl Halczenko
-
Patent number: 5336800Abstract: Oxamides useful as dye intermediates have the formula ##STR1## where R.sup.1 and R.sup.2 are independently of each other hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,X is hydroxyl, nitro or a radical of the formula --NR.sup.3 R.sup.4, where R.sup.3 is hydrogen or C.sub.1 -C.sub.4 -alkanoyl and R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,Z is C.sub.2 -C.sub.8 -alkylene, substituted or unsubstituted phenylene or substituted or unsubstituted naphthylene, or X--Z and R.sup.1 are, together with the nitrogen atom joining them together, the radical of the formula ##STR2## where R.sup.3 is as defined above,L is a bridge member andY is vinyl or a radical of the formula --C.sub.2 H.sub.4 --A, where A is hydroxyl or a group which is detachable under alkaline reaction conditions.Type: GrantFiled: January 4, 1993Date of Patent: August 9, 1994Assignee: BASF AktiengesellschaftInventors: Bernd Siegel, Manfred Patsch, Knut Kessel
-
Patent number: 5328932Abstract: The present invention provides new thrombin inhibiting bisamidines derivatives, their pharmaceutically acceptable salts and hydrates, methods for their preparation, pharmaceutical composition, a process for their preparation, and use of the compounds in treatment of thrombosis, ischemia and stroke.Type: GrantFiled: June 17, 1993Date of Patent: July 12, 1994Assignee: Bristol-Myers Squibb CompanyInventors: Neelakantan Balasubramanian, William Teh-Wei Han
-
Patent number: 5324747Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, n, m, o, p and q are as hereinafter set forth, and, when R.sub.2 is hydrogen, pharmaceutically acceptable salts thereof with bases, are described. The compounds of formula 1 are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.Type: GrantFiled: July 15, 1992Date of Patent: June 28, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Mathew Carson, Ru-Jen L. Han, Ronald A. LeMahieu, Vincent S. Madison
-
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
-
Patent number: 5302739Abstract: Compounds of the formula ##STR1## as intermediates for the preparation of pyrimidine or triazine herbicides.Type: GrantFiled: October 29, 1992Date of Patent: April 12, 1994Assignees: Kumiai Chemical Industry Co., Ihara Chemical Industry Co., Ltd.Inventors: Masatoshi Tamaru, Norihiro Kawamura, Masahiro Sato, Fumiaki Takabe, Shigehiko Tachikawa, Ryo Yoshida
-
Patent number: 5292933Abstract: The invention relates to a novel process for the resolution of an acid mixture (hereinafter: threo acid mixture) containing (+)-threo-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)-propionic acid [hereinafter: (+)-threo acid]and (-)-threo-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)-propionic acid [hereinafter: (-)-threo acid].Type: GrantFiled: April 9, 1991Date of Patent: March 8, 1994Assignee: Richter Gedeon Vegyeszeti Gyar RTInventors: Kalman Harsanyi, Elemer Fogassy, Maria cs, Tibor Gizur, Zsuzsanna Aracs nee Tischler, Katalin Berki, Laszlo Toke, Zsuzsanna Martonffy nee Jaszay
-
Patent number: 5290773Abstract: A sulfonyl compound of the formula ##STR1## The above illuminated formula (I) undergo bimolecular condensation by the condensing agents and easily form simple metal salts especially metal complexes which act as combatting viruses and inhibiting tissue growth.Type: GrantFiled: March 21, 1990Date of Patent: March 1, 1994Inventor: Takeo Takayanagi
-
Patent number: 5280043Abstract: Phenylalkanoic acids containing a sulphonamido group, and their use in a method of treatment of thromboxane-A.sub.2 mediated diseases are disclosed. A compound of the invention is 4-[4-(phenyl-sulphonamido)phenyl]butyric acid.Type: GrantFiled: April 2, 1992Date of Patent: January 18, 1994Assignee: Smith Kline & French Laboratories Ltd.Inventors: David G. Cooper, Andrew D. Gribble
-
Patent number: 5264457Abstract: This invention relates to compounds having the following formula ##STR1## which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine sulfones derivatives.Type: GrantFiled: February 14, 1992Date of Patent: November 23, 1993Assignee: G. D. Searle & Co.Inventors: Steven P. Adams, Joseph G. Rico, Masateru Miyano
-
Patent number: 5262564Abstract: The subject invention provides for novel anti-tumor and anti-retroviral compounds. More specifically, the invention relates to the sulfinic acid adducts of therapeutic C-nitroso compounds. The formation of the adducts increases the stability and more solubility of the C-nitroso compounds. These compounds include the L-cysteinesulfinic acid adducts of 6-nitroso-1,2-benzopyrone and 3-nitrosobenzamide. The invention also provides for compositions containing one or more of the compounds, and for methods of treating retroviral infections, cancer, infectious virus concentration with the subject compounds and compositions.Type: GrantFiled: October 30, 1992Date of Patent: November 16, 1993Assignee: Octamer, Inc.Inventors: Ernest Kun, Jerome Mendeleyev
-
Patent number: 5258398Abstract: This invention relates to novel diaminoalkanoic acid derivatives that inhibit platelet aggregation and thrombus formation in mammalian blood thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease and disseminated intravascular coagulation, to pharmaceutical compositions including such compounds, and to their use in inhibiting thrombus formation and platelet aggregation in mammals.Type: GrantFiled: December 16, 1991Date of Patent: November 2, 1993Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Scott I. Klein, Bruce F. Molino
-
Patent number: 5256812Abstract: Novel carboxamides and sulfonamides are described having of the formulaR.sup.1 --A--(W).sub.a --X--(CH.sub.2).sub.b --(Y).sub.c --B--Z--COOR(I),in which R.sup.1, A, W, X, Y, B, Z, R, a, b and c are as provided in the description. These compounds are useful in the treatment of thromboses, apoplexy, myocardial infarct, inflammations, arteriosclerosis as well as in the treatment and prevention of tumors. These novel compounds are prepared by eliminating the protective groups in corresponding compounds with protected amidino or guanidino groups.Type: GrantFiled: September 6, 1991Date of Patent: October 26, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
-
Patent number: 5256657Abstract: Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH.sub.2 R.sup.1 has the R-configuration, the carbon atom bearing CH.sub.2 R.sup.2 has the S-configuration, R.sup.1 is isopropyl, R.sup.2 is 3-indolyl, m is 2, n is 0, p is 2 and R.sup.3 and R.sup.4 taken alone are each methyl or R.sup.3 and R.sup.4 taken together with N are morpholino and pharmaceutically acceptable acid addition salts or solvates or acid addition salts-solvates thereof, which are matrix-metalloprotease inhibitors useful in treatment of disease in which matrix-metalloprotease promoted connective tissue remodelling is a causative factor, for example, rheumatoid arthritis and cancer, and a method of preparation and method of use thereof and methods of preparation of intermediates therefor are disclosed.Type: GrantFiled: August 19, 1991Date of Patent: October 26, 1993Assignee: Sterling Winthrop, Inc.Inventors: Jasbir Singh, Barry A. Morgan, James A. Gainor, Thomas D. Gordon, Robert C. Wahl
-
Patent number: 5250725Abstract: The present invention relates to novel cephalosporin derivatives with improved pharmacokinetics, corresponding to the formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3 represent a hydrogen atom, or R.sub.1 and R.sub.2 represent a hydrogen atom or a methyl group and R.sub.3 represents a carboxyl group, or ##STR2## form a cyclobutyl group and R.sub.3 represents a carboxyl group; and A and B are different and occupy the meta and para positions of the benzene ring, one representing a hydroxyl group and the other being selected from the groups ##STR3## and --NH--SO.sub.2 --Alk--NH.sub.2 in which Alk denotes a C.sub.2 -C.sub.4 lower alkylene group and also to the pharmaceutically acceptable salts and esters of the said derivatives.It further relates to a process for the preparation of such cephalosporins and to pharmaceutical compositions in which they are present.Type: GrantFiled: September 3, 1991Date of Patent: October 5, 1993Assignee: Elf SanofiInventors: Dominique Olliero, Bernard Labeeuw, Gilles Roche, Ali Salhi
-
Patent number: 5239113Abstract: Novel substituted .beta. amino acid derivatives are provided which inhibit platelet aggregation and intermediates thereof. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.Type: GrantFiled: April 10, 1992Date of Patent: August 24, 1993Assignees: Monsanto Company, G. D. Searle & Co.Inventors: Phillipe R. Bovy, Joseph G. Rico, Thomas E. Rogers, Foe S. Tjoeng, Jeffery A. Zablocki
-
Patent number: 5225595Abstract: Sulfonyl compounds of the formula ##STR1## where Ar is the radical of a benzene or naphthalene ring,R.sup.1 and R.sup.2 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, cyano, halogen or hydroxysulfonyl,R.sup.3 is nitro, amino, C.sub.1 -C.sub.4 -alkanoylamino or benzoylamino, andR.sup.4 is a radical of the formula ##STR2## where X.sup.1, X.sup.2 and X.sup.3 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl or substituted or unsubstituted phenyl, andX.sup.4 is a group which is detachable under alkaline conditions,either in the free form or in the form of their salts, are useful for synthesizing reactive dyes.Type: GrantFiled: November 4, 1992Date of Patent: July 6, 1993Assignee: BASF AktiengesellschaftInventors: Bernd Siegel, Claus Marschner, Manfred Patsch
-
Patent number: 5214201Abstract: This invention relates to certain salts of leukotriene antagonists and the use of a particular amine to form these salts as a means for selectively crystallizing optical isomers of the leukotriene antagonists disclosed herein.Type: GrantFiled: December 12, 1991Date of Patent: May 25, 1993Assignee: SmithKline Beecham CorporationInventor: Robert J. Mills
-
Patent number: 5210290Abstract: Fluorobenzenensulfonamides of Formula I ##STR1## wherein m means the number 0, 1, 2, 3, or 4,n means the number 0 or 1, andY means the residue of an aminocarboxylic or aminosulfonic acid,with the proviso that m and n are not to stand simultaneously for the number 0 and, if desired, the acid groups are present in the form of their amides or in the form of salts with organic or inorganic bases, are suitable for use as NMR diagnostic aids.Type: GrantFiled: March 12, 1991Date of Patent: May 11, 1993Assignee: Schering AktiengesellschaftInventors: Heinz Gries, Ulrich Niedballa, Hanns-Joachim Weinmann, Hans Bauer
-
Patent number: 5210257Abstract: Novel aryl ethers, containing both a carboxylic acid and a sulfonic acid functionality; and a process for making them are described. These difunctional aryl compounds comprise:i) a carboxylic acid group or its derivative,ii) a first aromatic group bonded to the carboxylic acid or its derivative,iii) a second aromatic group linked to the first aromatic group by a non-electron-withdrawing moiety,iv) a third aromatic group linked to the second aromatic group by a non-electron-withdrawing moiety, andv) a sulfonyl group or its derivative bonded to the third aromatic group.Type: GrantFiled: April 12, 1991Date of Patent: May 11, 1993Assignee: The Dow Chemical CompanyInventor: William J. Harris
-
Patent number: 5208236Abstract: Novel glutarylamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of the formula ##STR1## wherein: R.sup.1 and R.sup.3 are independently hydroxy, lower alkoxy, aryllower alkoxy, amino, lower alkylamino and di-(lower alkyl)amino;R.sup.2 is H or hydroxy;R.sup.4 is aryl, substituted aryl, heteroaryl or substituted heteroaryl;R.sup.6 is H or R.sup.7 --(CH.sub.2).sub.3 --, wherein R.sup.7 is amino or (aryllower alkoxy)carbonylamino;Q is --C(O)-- or --SO.sub.2 --;Y is lower alkyl, lower alkoxy, aryllower alkoxy, amino, lower alkylamino, di-(lower alkyl)amino, or a group of the formula ##STR2## wherein A is a bond, --N(R.sup.5)--, or --O--; and R.sup.5 is H or lower alkyl;B is H or Z--(CH.sub.2).sub.m --Z is amino, lower alkylamino, di-(lower alkyl)amino, (aryllower alkoxy)carbonylamino, 1-pyrrolidino or 1-piperidino;m=1,2,3,4 or 5; and n=1,2 or 3; oror a pharmaceutically acceptable addition salt thereof; useful in the treatment of cardiovascular disorders, are disclosed.Type: GrantFiled: September 23, 1992Date of Patent: May 4, 1993Assignee: Schering CorporationInventor: Bernard R. Neustadt
-
Patent number: 5206403Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime either derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COR6, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.Type: GrantFiled: November 5, 1990Date of Patent: April 27, 1993Assignee: Eisai Co., Ltd.Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
-
Patent number: 5202470Abstract: The invention provides a compound of the formula[NH.sub.2 NH.sub.2 ].sub.a [C.sub.6 H.sub.3 (COOH) (SO.sub.3 H) (OH)].sub.bwhereina is 1 andb is from 1 to 2.The compound is useful for stabilizing tin (II) compounds against oxidation, in particular in the electrolytic coloring of aluminium or aluminium alloys.Type: GrantFiled: November 19, 1990Date of Patent: April 13, 1993Inventor: Erich Ruf
-
Patent number: 5198566Abstract: Disclosed herein are N-substituted-3-(substituted hydrazino)benzenesulfonamide derivatives of the formula (I): ##STR1## wherein R.sup.1 and CF.sub.3, COOH or CCl=CClCOOH, R.sup.2 is H, Cl, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.4 alkoxycarbonyl; Z is CH or N; X.sup.1 is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxyl or Cl; and X.sup.2 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxyl, a process for the preparation thereof, and herbicidal compositions containing the N-substituted-3-(substituted hydrazino)benzenesulfonamide derivatives as active ingredients.Type: GrantFiled: June 3, 1992Date of Patent: March 30, 1993Assignee: Kureha Kagaku Kogyo K.K.Inventors: Hideo Arabori, Shiro Yamazaki, Masato Arahira, Aiko Murakami
-
Patent number: 5192803Abstract: Novel substituted 2-phenoxyphenoxyethylcarbamic esters of the formula I ##STR1## where R.sub.1 is C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.4 alkenyl, R.sub.2 is C.sub.1 -C.sub.4 alkyl or a radical of the formula ##STR2## --C(CH.sub.3).sub.2 --CN or --N(R.sub.9)--COO--C.sub.1 -C.sub.4 alkyl, R.sub.3 and R.sub.4 independently of one another are hydrogen or methyl, R.sub.5 is fluorine or chlorine, R.sub.6 is either identical to the substituents given in the case of R.sub.5 or is hydrogen, R.sub.7 and R.sub.8 independently of one another are hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or nitro, R.sub.9 is C.sub.1 -C.sub.4 alkyl and n is zero, one or two, their preparation, their use in pest control, and pesticides containing these carbamic esters as active substance, are described. The preferred field of application is the control of pests on animals and plants, in partcular of eggs and larvae of phytophagous harmful insects and harmful mites.Type: GrantFiled: June 24, 1991Date of Patent: March 9, 1993Assignee: Ciba-Geigy CorporationInventor: Friedrich Karrer
-
Patent number: 5189211Abstract: A sulfonamide derivative represented by the Formula: ##STR1## wherein A, B, X, Y, R, m and n are as defined in the specification, and a salt thereof have thromboxane A.sub.2 antagonism, therefore they are useful, for example, as blood platelet aggregation inhibiting agents.Type: GrantFiled: July 26, 1991Date of Patent: February 23, 1993Assignees: Taisho Pharmaceutical Co., Ltd., Nippon Suisan Kaisha, Ltd.Inventors: Masakazu Sato, Yutaka Kawashima, Jun Goto, Yoshiyuki Chiba, Mikio Satake, Chuzo Iwata, Takeshi Imanishi