Chalcogen Attached Indirectly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/252)
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Patent number: 5846986Abstract: Compounds of the formula ##STR1## wherein Azo is alkyltetrazolyl or is chosen from the group consisting of oxadiazolyl, imidazolyl, pyrazolyl, triazolyl, oxazolyl, triazinyl, thiazolyl, isothiazolyl or any of these substituted with a member of the group consisting of alkyl, alkylthio, alkoxy, hydroxy, halo, cyano, nitro, hydroxyalkyl, alkoxyalkyl, alkoxycarbonyl, alkanoyl, fluoroalkyl or the N-oxide of any of the preceding;Y is an alkylene bridge of 3-9 carbon atoms;R.sub.1 and R.sub.2 are each individually chosen from hydrogen, halo, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluoromethyl or cyano;R.sub.Type: GrantFiled: November 25, 1997Date of Patent: December 8, 1998Assignee: SanofiInventors: David J. Aldous, Thomas R. Bailey, Guy Dominic Diana, Theodore J. Nitz, Gee-Hong Kuo
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Patent number: 5840758Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein Y is selected from halogen, alkyl, and haloalkyl; n is 0, 1, 2, or 3; A is selected from (a) optionally substituted alkylene, (b) optionally substituted cycloalkylene, (c) optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, (d) optionally substituted alkenylene and (e) ##STR2## X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from --OR.sup.4, --NR.sup.6 R.sup.7, and a pharmaceutically acceptable metabolically cleavable group, (c) --OR.sup.2, (d) tetrazolyl, (e) --CH(OR.sup.2)--CH.sub.2 OR.sup.8, (f) --CH(OR.sup.2)--CH.sub.2 --CH.sub.2 OR.sup.8, (g) --CH(OR.sup.2)--CH(OR.sup.8)--CH.sub.2 OR.sup.9, and (h).dbd.N--OR.sup.2 ; and R.sup.Type: GrantFiled: June 6, 1996Date of Patent: November 24, 1998Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Teodozyj Kolasa, Wendy Lee, Andrew O. Stewart
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Patent number: 5837702Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)-- where R.sup.8 is hydrogen, alkyl, haloalkyl, aryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl, and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.Type: GrantFiled: August 30, 1994Date of Patent: November 17, 1998Assignee: Bristol-Myers Squibb Co.Inventors: George C. Rovnyak, Karnail S. Atwal, Dinos P. Santafianos, Charles Z. Ding
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Patent number: 5827863Abstract: Compounds of general formula I and their salts and solvates are angiotensin II receptor antagonists and as such are useful in the treatment of hypertension, congestive heart failure and elevated intraocular pressure. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.Type: GrantFiled: June 20, 1996Date of Patent: October 27, 1998Assignee: J. Uriach & Cia, S.A.Inventors: Carmen Almansa, Concepcion Gonzalez, M. Carmen Torres, Elena Carceller, Javier Batroli
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Patent number: 5821256Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and X have the meaning indicated in claim 1, and their salts exhibit endothelin receptor-antagonistic properties.Type: GrantFiled: August 15, 1996Date of Patent: October 13, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Dieter Dorsch, Mathias Osswald, Werner Mederski, Claudia Wilm, Claus J. Schmitges, Maria Christadler
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Patent number: 5821250Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisiting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; and(e) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: October 13, 1998Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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Patent number: 5817683Abstract: Naphthoic derivatives of the Formula (I) ##STR1## wherein the variables are defined herein; and pharmaceutical compositions containing these compounds, and their use as endothelin receptor antagonists are disclosed.Type: GrantFiled: April 8, 1996Date of Patent: October 6, 1998Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Jia-Ning Xiang
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Patent number: 5777128Abstract: The present invention relates to a process for preparing compounds of structure (I), and the intermediate compound of formula (II).Type: GrantFiled: November 21, 1996Date of Patent: July 7, 1998Assignee: SmithKline Beecham p.l.c.Inventors: John David Hayler, Trevor John Grinter, Vance Novak, Norman John Lewis
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Patent number: 5770598Abstract: The present invention relates to heterocyclic compounds which have been found to have anti-tumour activity. More specifically, the invention concerns Pyrrolo ?3,2-b! carbazoles, 1H-Benzofuro ?3,2-.function.! indoles and 1H-?1! Benzothieno ?2,3-.function.! indoles, methods for their preparation, pharmaceutical formulations containing them and their use as anti-tumour agents.Type: GrantFiled: April 10, 1997Date of Patent: June 23, 1998Assignee: University College Cardiff Consultants LimitedInventors: David D. Miller, Paul Barraclough, Sadie Vile, Ann L. Walker, Patrick V. R. Shannon, Laddawan Chunchatprasert, Pierre P. M. Debont, Alan T. Hudson
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Patent number: 5767141Abstract: Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseasesPropane derivatives of the formula I ##STR1## in which the radicals have the meanings stated in the description, a process for the preparation of these compounds, their use as pharmaceuticals, and pharmaceutical products are described. Also described are novel intermediates for preparing the compounds of the formula I.Type: GrantFiled: March 8, 1995Date of Patent: June 16, 1998Assignee: Hoechst AktiengesellschaftInventors: Gerrit Schubert, Horst Hemmerle, Peter Below, Andreas Herling, Hans-Jorg Burger
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Patent number: 5763618Abstract: A method of manufacturing a sulfide comprises the steps of (a) dissolving a thiol in a solvent to form a solution; (b) oxidizing the thiol to a disulfide in the presence of a first oxidizing agent in the solution; (c) reacting the disulfide with a coupler in the presence of a base and a second oxidizing agent, without isolation of said disulfide from the solution, to form a reaction mixture in which the sulfide is produced; and (d) obtaining said sulfide.Type: GrantFiled: April 29, 1996Date of Patent: June 9, 1998Assignee: Konica CorporationInventors: Ryuzou Watanabe, Shinri Tanaka, Katsuji Ota, Michiko Nagato, Tomio Horiuchi
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Patent number: 5763619Abstract: Disclosed is a method for removing a protective group of an N-protected tetrazolyl compound which comprises reacting said N-protected tetrazolyl compound with a mineral acid under substantially anhydrous conditions in the presence of an alcohol, insuring a high reaction yield of the object tetrazolyl compound.Type: GrantFiled: August 16, 1996Date of Patent: June 9, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Yasushi Shida, Kokichi Yoshida
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Patent number: 5763616Abstract: The present invention provides an indazolesulfonylurea derivative represented by the general formula: ##STR1## ?wherein R.sup.1 is a hydrogen atom or an alkyl group, etc., R.sup.2 and R.sup.3 are the same or different and represent a hydrogen atom, a halogen atom, an alkyl group, the formula --COR.sup.4 (wherein R.sup.4 represents an alkoxy group, etc.), an alkoxy group, a haloalkoxy group or a cyano group, etc., X is an oxygen atom or a sulfur atom, Y is a hydrogen atom or an alkyl group, etc., A and B are the same or different and represent a halogen atom, an alkoxy group or an alkyl group, etc., and Z represents a nitrogen atom or a methine group!, as well as a herbicide containing it as an active ingredient and an intermediate for its production.The compound of the present invention exhibits excellent herbicidal effects over a wide range from the preemergence stage to the growing stage of various weeds which are problematic in agricultural fields.Type: GrantFiled: January 7, 1997Date of Patent: June 9, 1998Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Chiharu Suzuki, Katsumi Masuda, Masatoshi Tamaru, Masahito Inamori, Nobuo Takefuji, Katsutada Yanagisawa, Yasunori Ogawa
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Patent number: 5760037Abstract: These compounds correspond to the following general formula: ##STR1## where: n is 0, 1, or 2,m is are 1, 2, or 3,R, R.sub.1, R.sub.2, and R.sub.3, whether identical or different, represent an atom of hydrogen or a linear or branched alkyl radical at C.sub.1 -C.sub.4,R.sub.1 and R.sub.2, or R.sub.2 and R.sub.3 taken together can form a 5- or 6-group cycle,X and Y, whether identical or different, represent a nitrogenous aromatic heterocycle in position 2,Z.sub.1, Z.sub.2, and Z.sub.3, whether identical or different, represent an atom of hydrogen, a linear or branched alkyl radical at C.sub.1 -C.sub.4, the radical --OR.sub.4 or --NR.sub.4 R'.sub.4,R.sub.4 and R'.sub.4 represent an atom of hydrogen or a linear or branched alkyl radical at C.sub.1 -C.sub.4,and the metallic salts and complexes thereof.Use in pharmaceutical and cosmetic compositions to protect the organism from oxidizing stress situations linked to certain pathological states.Type: GrantFiled: July 23, 1996Date of Patent: June 2, 1998Assignee: L'OrealInventors: Jean-Baptiste Galey, Jacqueline Dumats
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Patent number: 5756804Abstract: A process for preparing polycyclic aromatic compounds, which comprises reactinga) an aromatic boron compound withb) an aromatic halogen compound or an aromatic perfluoroalkylsulfonate in the presence ofc) a base,d) a nickel or palladium catalyst,e) a phosphorus-containing ligand andf) a polyhydric alcohol, a sulfoxide or sulfone.The process gives high yields, in particular also in the coupling of chloroaromatics.Type: GrantFiled: July 24, 1996Date of Patent: May 26, 1998Assignee: Hoechst AktiengesellschaftInventors: Steffen Haber, Hans-Jerg Kleiner
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Patent number: 5750549Abstract: The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, Q, W, X, Y, Z and n are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.Type: GrantFiled: October 15, 1996Date of Patent: May 12, 1998Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Ping Chen, Philippe L. Durette, Paul Finke, Jeffrey Hale, Edward Holson, Ihor Kopka, Malcolm MacCoss, Laura Meurer, Sander G. Mills, Albert Robichaud
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Patent number: 5750543Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: May 12, 1998Assignee: The Procter & Gamble CompanyInventors: Laurence Ichih Wu, John Michael Janusz
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Patent number: 5750558Abstract: Described herein are compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein L is selected from the group consisting of ##STR2## R.sup.2 is selected from (a) ##STR3## R.sup.3 is selected from optionally substituted phenyl, and optionally substituted pyridyl; Y is selected from halogen, alkyl, haloalkyl, alkoxy, pyridylmethoxy, thiazolylmethoxy, benzothiazolylmethoxy, quinolylmethoxy, and optionally substituted quinolylmethoxy; W is selected from hydrogen, alkyl, hydroxyalkyl, and hydroxy; A is absent or is selected from optionally substituted alkylene optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, and ##STR4## and X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from (b-1) a pharmaceutically acceptable metabolically cleavable group, (b-2)--OR.sup.10,(b-3)--O(CH.sub.2).sub.w --CH(OR.sup.Type: GrantFiled: June 6, 1996Date of Patent: May 12, 1998Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Teodozyj Kolasa, Wendy Lee, Andrew O. Stewart
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Patent number: 5739374Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5736559Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: August 1, 1996Date of Patent: April 7, 1998Assignee: Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5725806Abstract: A method of stabilizing non-halogen containing 3-isothiazolone microbicides against chemical degradation by the introduction of aromatic disulfide compounds (except 2,2'-dithiobisbenzoic acid) is disclosed.Type: GrantFiled: November 8, 1996Date of Patent: March 10, 1998Assignee: Rohm and Haas CompanyInventor: Tirthankar Ghosh
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Patent number: 5718845Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.Type: GrantFiled: January 18, 1995Date of Patent: February 17, 1998Assignee: Enichem S.p.A.Inventors: Kevin J. Drost, Pushkara Rao Varanasi, Kwan-Yue Alex Jen, Michael Anthony Drzewinski
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Patent number: 5719290Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof. These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure ##STR1## in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L-Ala, L-Ile, L-Phe, L-Try, L-Thr, or an amide such as NHCH.sub.2 C.sub.6 H.sub.5 or NH(CH.sub.2).sub.2 C.sub.6 H.sub.5.Type: GrantFiled: November 4, 1996Date of Patent: February 17, 1998Assignee: G. D. Searle & Co.Inventors: Sean T. Nugent, Richard A. Mueller
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Patent number: 5708016Abstract: A compound of formula (I): ##STR1## in which: R.sub.1 represents an indolyl, naphthyl, tetrahydronaphthyl, thienyl, phenyl, optionally substituted, or (C.sub.3 -C.sub.7)cycloalkyl group,n represents an integer such that 1.ltoreq.n.ltoreq.8,m represents an integer such that 1.ltoreq.m.ltoreq.4,R.sub.2 represents an unsubstituted or substituted benzyl group, an unsubstituted or substituted phenyl group or a linear or branched (C.sub.1 -C.sub.6)alkyl group, its enantiomers, diastereoisomers and epimers as well as its addition salts with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful as substance P antagonists.Type: GrantFiled: February 14, 1997Date of Patent: January 13, 1998Assignee: Adir et CompagnieInventors: Jean-Luc Fauchere, Nathalie Kucharczyk-Gentric, Emmanuel Canet, Michel Lonchampt
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Patent number: 5703108Abstract: Methods for the treatment of bone disorders utilizing certain prostaglandin agonists/antagonists.Type: GrantFiled: February 20, 1997Date of Patent: December 30, 1997Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Paul A. Dasilva-Jardine, Robert L. Rosati
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Patent number: 5686478Abstract: Novel derivatives of the general structural Formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, complications of diabetes, migraine, bone resorption, and inflammatory diseases, including Raynaud's disease and asthma.Type: GrantFiled: July 7, 1994Date of Patent: November 11, 1997Assignee: Merck & Co. Inc.Inventors: William J. Greenlee, Thomas F. Walsh
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Patent number: 5684046Abstract: Described herein are Benzopyran and other benzo-fused leukotriene B.sub.4 antagonists have the formula ##STR1## wherein R.sup.1 is a phenyl or substituted phenyl group, and A, n, R.sup.2 and R.sup.3 are as defined herein.Type: GrantFiled: May 3, 1996Date of Patent: November 4, 1997Assignee: Pfizer IncInventor: Kevin Koch
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Patent number: 5677324Abstract: The present invention relates to compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein the dashed line represents an optional covalent bond; X is O, NH, S or a direct link; R.sup.3 is hydroxy when the dashed line does not represent a covalent bond and R.sup.3 is absent when the dashed line represents a covalent bond; R.sup.4 is (a), when X is O, a group of formula (i), (b), when X is O, NH or S, optionally substituted hydroxyphenyl, (c) an optionally substituted 4- to 7-membered heterocyclic ring, or (d), when X is NH, a group of formula (ii). The compounds are useful for the treatment of disease associated with the altered tone or motility of smooth muscle.Type: GrantFiled: August 4, 1995Date of Patent: October 14, 1997Assignee: Pfizer Inc.Inventors: Alexander Roderick Mackenzie, Sandra Marina Monaghan
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Patent number: 5674879Abstract: Conformationally restricted compounds are described which are therapeutically effective as angiotensin II antagonists for the treatment of circulatory disorders.Type: GrantFiled: March 3, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Robert E. Manning, Horng-Chih Huang
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Patent number: 5675024Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: November 22, 1995Date of Patent: October 7, 1997Assignee: AllerganInventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5672583Abstract: Novel Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.Type: GrantFiled: May 17, 1995Date of Patent: September 30, 1997Assignee: Merck & Co., Inc.Inventors: Kevin Chapman, William Hagmann, Philippe Durette, Craig Esser, Ihor Kopka, Charles Caldwell
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Patent number: 5663053Abstract: Coenzyme A-independent transacylase is required for the release of free arachidonic acid, and the production of arachidonic acid metabolites and platelet activation factor. Blocking of this enzyme inhibits the production of these inflammatory mediators and will be of therapeutic utility in a broad range of allergic and inflammatory diseases and disorders. Compounds are described herein which inhibit the action of CoA-IT and are therefore useful in the treatment of disease states caused thereby.Type: GrantFiled: November 30, 1994Date of Patent: September 2, 1997Assignees: SmithKline Beecham Corporation, The Johns Hopkins UniversityInventors: James David Winkler, Deirdre Mary Bernadette Hickey, Floyd Harold Chilton, III
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Patent number: 5656619Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5648372Abstract: A compound represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 denote a halogen atom or hydrogen atom; R.sup.3 means a hydrogen atom or lower alkyl group; l, r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic ring, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for --S--, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmacetical composition suitable for use as an antifungal agent.Type: GrantFiled: February 1, 1995Date of Patent: July 15, 1997Assignee: Eisai Co., Ltd.Inventors: Toshihiko Naito, Katsura Hata, Yumiko Kaku, Akihiko Tsuruoka, Itaru Tsukada, Manabu Yanagisawa, Toshio Toyosawa, Kazumasa Nara
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Patent number: 5648354Abstract: Novel 1,2-dithiin compounds useful as antifungal or anti-infective agents, as well as methods for their use as such, are described.Type: GrantFiled: February 28, 1995Date of Patent: July 15, 1997Assignee: Shaman Pharmaceuticals, Inc.Inventors: Donald E. Bierer, Jeffrey M. Dener, Joane Litvak, Larisa G. Dubenko
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Patent number: 5646295Abstract: The invention concerns diazapentalene derivatives of formula I ##STR1## in which X and Y represent leaving groups which are less nucleophilic than thiol compounds, as thiol-specific fluorochromes for the detection of compounds containing thiol groups, in particular in cells.Type: GrantFiled: January 31, 1996Date of Patent: July 8, 1997Assignee: Boehringer Mannheim GmbHInventors: Rudolf Gompper, Manfred Kubbies, Axel Schmidt, Bernhard Virnekas
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Patent number: 5643946Abstract: Compounds of the formula ##STR1## wherein the substituents are as defined herein, are disclosed. Pharmaceutical compositions and methods of treating allergic and inflammatory diseases are also taught.Type: GrantFiled: May 18, 1995Date of Patent: July 1, 1997Assignee: SmithKline Beecham CorporationInventor: Siegfried Benjamin Christensen, IV
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Patent number: 5641798Abstract: This invention provides novel bicyclic compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides intermediates useful in the synthesis of excitatory amino acid antagonists.Type: GrantFiled: June 1, 1995Date of Patent: June 24, 1997Assignee: Eli Lilly and CompanyInventor: James A. Monn
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Patent number: 5633273Abstract: 6-Heterocyclic-4-amino-l,2,2a,3,4,5-hexahydrobenz-[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.Type: GrantFiled: June 2, 1995Date of Patent: May 27, 1997Assignee: Eli Lilly and CompanyInventors: Richard N. Booher, David E. Lawhorn, Michael J. Martinelli, Charles J. Paget, Jr., John M. Schaus
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Patent number: 5633371Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: September 15, 1995Date of Patent: May 27, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
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Patent number: 5625067Abstract: The invention relates to cyclopentane ether derivatives of Formula I ##STR1## their salts with physiologically compatible bases, as well as the .alpha.-, .beta.- or .gamma.-cyclodextrin clathrates, and also the liposome-encapsulated compounds of Formula I, processes for their production, and their pharmaceutical usage.Type: GrantFiled: December 14, 1994Date of Patent: April 29, 1997Assignee: Schering AktiengesellschaftInventors: Hartmut Rehwinkel, Ulrich Klar, Helmut Vorbruggen, Karl-Heinz Thierauch, Peter Verhallen
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Patent number: 5620998Abstract: The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## wherein Y.sub.1 is O, S or N(R) and R is hydrogen or C.sub.1 -C.sub.7 alkyl;X.sub.1 is --CO-- or --S(O).sub.m -- and the index m is 0, 1 or 2;one of the variables X.sub.2 and X.sub.4 is C.sub.1 -C.sub.4 alkylene and the other of the variables X.sub.2 and X.sub.4 is a bond; or each of the variables X.sub.2 and X.sub.4 is a bond;X.sub.3 is C.sub.3 -C.sub.7 cycloalkylidene or the structural element --C(X.sub.a)(X.sub.b)-- and X.sub.a is hydrogen or C.sub.1 -C.sub.7 alkyl and X.sub.b is C.sub.1 -C.sub.7 alkyl;and the rings A, B and C, with the exception of the substituents indicated in the formula, and also aromatic substituents are, independently of one another, unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of halogen, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.7 alkoxy, C.sub.2 -C.sub.7 alkenyloxy, phenoxy, benzyloxy, trifluoromethyl and S(O).sub.Type: GrantFiled: June 7, 1995Date of Patent: April 15, 1997Assignee: Ciba-Geigy CorporationInventors: Tibur Schmidlin, Paul Zbinden, Peter B uhlmayer
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Patent number: 5616591Abstract: Compounds of the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.Type: GrantFiled: March 27, 1992Date of Patent: April 1, 1997Assignee: E.R. Squibb & Sons, Inc.Inventor: Michael A. Poss
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Patent number: 5614540Abstract: Novel compounds of Formula (I) ##STR1## where X.sub.4 is a substituted cyclohexane or cyclohexane group and the other radicals are defined herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. The compounds of the present invention are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.Type: GrantFiled: May 18, 1995Date of Patent: March 25, 1997Assignee: SmithKline Beecham CorporationInventor: Siegfried B. Christensen, IV
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Patent number: 5614519Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-[(2-n-propyl-4-methyl-6-(1-(2-N-morpholinoethyl)-imidazol-4-yl)-benzimi dazol-1-yl)-methyl]-biphenyl-2-carboxylic acid.Type: GrantFiled: June 1, 1995Date of Patent: March 25, 1997Assignee: Karl Thomae GmbHInventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. Antonius van Meel, Wolfgang Wienen, Michael Entzeroth
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Patent number: 5607955Abstract: A tricyclic compound represented by the following formula (I): ##STR1## exhibits antagonism to angiotensin II receptors.Type: GrantFiled: May 1, 1995Date of Patent: March 4, 1997Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Fumihiko Kanai, Hideyuki Sato, Hiroyuki Obase, Toshiaki Kumazawa, Shiho Takahara, Tetsuji Ohno, Tomoko Ishikawa, Koji Yamada
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Patent number: 5608075Abstract: Polymorphic forms of Losartan (Formula I) ##STR1## and a process for the preparation of Form II of Losartan. Losartan is known to be useful in the treatment of hypertension.Type: GrantFiled: January 12, 1995Date of Patent: March 4, 1997Assignees: Merck & Co., Inc., E. I. Du Pont de Nemours & Company, The DuPont Merck Pharmaceutical CompanyInventors: Gordon C. Campbell, Jr., Anil M. Dwivedi, Dorothy A. Levorse, James A. McCauley, Krishnaswamy S. Raghavan
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Patent number: 5602127Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo [1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-[(2-n-propyl-4-methyl-6-(butanesultam-1-yl)benzimidazol-1-yl)-methyl]-b iphenyl-2-carboxylic acid.Type: GrantFiled: June 1, 1995Date of Patent: February 11, 1997Assignee: Karl Thomae GmbHInventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
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Patent number: 5602157Abstract: Novel compounds or formula (I) are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. The compounds or the present invention are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition therefore.Type: GrantFiled: May 18, 1995Date of Patent: February 11, 1997Assignee: SmithKline Beecham CorporationInventor: Siegfried B. Christensen, IV
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Patent number: 5599943Abstract: Disclosed are a compound of the formula (R).sub.3 SnN.sub.3, wherein R is a C.sub.7-18 alkyl, and a process for producing a tetrazolylbenzene compound which comprises reacting a cyanobenzene compound with a (R).sub.3 SnN.sub.3. This process is useful for a safe and commercially profitable production of the tetrazolylbenzene compound which is employed for producing a tetrazole derivative having a hypotensive action based on angiotensin II-antagonizing activity or a production intermediate thereof.Type: GrantFiled: August 28, 1995Date of Patent: February 4, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Takeshi Kato, Yasushi Shida