Additional Hetero Ring Patents (Class 514/444)
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Patent number: 5639772Abstract: 3-amino-5-aryl- and 5-heteroarylchromans, as well as enantiomers and salts thereof are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.Type: GrantFiled: May 30, 1995Date of Patent: June 17, 1997Assignee: Astra AktiebolagInventors: Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
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Patent number: 5639784Abstract: A method is disclosed for the treatment of migraine by the administration of 3-amino-5-carbamoyl-chromans and 8-fluoro-3-amino-5-carbamoylchromans or enantiomers or salts thereof.Type: GrantFiled: May 30, 1995Date of Patent: June 17, 1997Assignee: Astra AktiebolagInventors: Eva Maria Hammarberg, Lars George Johansson, Lars-Gunnar Larsson, Rolf Noreen, Lucy Anna Renyi, Svante Bertil Ross, Daniel Dungan Sohn, Bjorn Eric Svensson, Seth-Olov Thorberg
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Patent number: 5635531Abstract: The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.Type: GrantFiled: July 8, 1996Date of Patent: June 3, 1997Assignee: Bristol-Myers Squibb CompanyInventor: Shu-Hui Chen
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Patent number: 5635527Abstract: A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.Type: GrantFiled: February 6, 1996Date of Patent: June 3, 1997Assignee: The Green Cross CorporationInventors: Shinichiro Ono, Tomohiro Yoshida, Atsuyuki Ashimori, Keigo Kosaka, Takehiro Okada, Kazuhiro Maeda, Masahiro Eda, Fumio Mori, Yoshihisa Inoue, Hajime Ebisu, Teruaki Imada, Ruriko Ikegawa, Feng Wang, Norifumi Nakamura
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Patent number: 5627198Abstract: The invention relates to heterocyclic amides of the formula ##STR1## in which the radicals A, Z, A.sub.1, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, to a process for the preparation of these amides and to their use as active substances for the curing and amelioration of disorders and diseases which can be treated by exerting influence on potassium channels.Type: GrantFiled: December 4, 1995Date of Patent: May 6, 1997Assignee: Hafslund Nycomed Pharma AktiengesellschaftInventors: Peter Esch, Robertson Towart, Franz Rovenszky
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Patent number: 5624940Abstract: The present invention provides aqueous inclusion complexes of certain known benzothiophene compounds, particularly Raloxifene, and water soluble cyclodextrins. Also provided are pharmaceutical compositions of such inclusion complexes, and methods of using these complexes for inhibiting bone loss and reducing serum cholesterol in mammals.Type: GrantFiled: June 30, 1995Date of Patent: April 29, 1997Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, George J. Cullinan, Paul C. Francis, David E. Magee, Stephanie A. Sweetana, Arvind L. Thakkar
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Patent number: 5618835Abstract: A compound having the structure: ##STR1## pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: April 8, 1997Assignee: The Procter & Gamble CompanyInventors: Laurence I. Wu, John M. Janusz
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Patent number: 5618836Abstract: Compounds of Formula 1 ##STR1## where R.sub.1 -R.sub.7 are hydrogen, lower alkyl of 1-6 carbons, or halogen;Y is phenyl, pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl;A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds;B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.14, CR.sub.14 (OR.sub.12).sub.2, or CR.sub.14 OR.sub.13 O, where R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.Type: GrantFiled: April 10, 1995Date of Patent: April 8, 1997Assignee: AllerganInventors: Roshantha A. Chandraratna, Richard L. Beard
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Patent number: 5612355Abstract: This invention relates to phenyl amidine alkanoic acids and lactones 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 amidine derivatives.Type: GrantFiled: May 26, 1995Date of Patent: March 18, 1997Assignee: G. D. Searle & Co.Inventors: Norman A. Abood, Robert E. Manning, Masateru Miyano
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Patent number: 5612351Abstract: The present invention relates to a novel method for treating a mammal suffering from urinary bladder dysfunctions.Type: GrantFiled: November 8, 1994Date of Patent: March 18, 1997Assignee: Novo Nordisk A/SInventors: Mark A. Muhlhauser, Harlan E. Shannon, Karl B. Thor
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Patent number: 5607939Abstract: The compound ##STR1## wherein ring A represents a benzene ring; Ar represents an aromatic group; R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group; m represents an integer of 1 to 6; n represents an integer of 2 to 3; ----- represents a single bond or a double bond; X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where ----- is a single bond or .dbd.N-- where ----- is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.Type: GrantFiled: April 25, 1995Date of Patent: March 4, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato, Yasuo Nagai
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Patent number: 5605924Abstract: The present invention relates to compounds of the formula ##STR1## where X is a bond or --CH2--;R.sup.2 is pyrrolidino;R is OH, --OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3 or ##STR2## R.sup.1 is hydrogen, OH, fluoro, chloro, --OSO.sub.2 --(CH.sub.2).sub.n --CH.sub.3 or ##STR3## each R.sup.3 is independently C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, unsubstituted or substituted phenyl where the substituent is fluoro, chloro, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy;each n is independently 3, 4 or 5; and pharmaceutically acceptable salts and solvates thereof; provided that at least one of R and R.sup.1 is ##STR4## The invention also relates to methods of use of the compounds of formula I and pharmaceutical compositions which comprise compounds of formula I.Type: GrantFiled: January 17, 1996Date of Patent: February 25, 1997Assignee: Eli Lilly and CompanyInventors: Larry J. Black, Henry U. Bryant, George J. Cullinan
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Patent number: 5604182Abstract: Compounds of formula (I): ##STR1## and salts and esters thereof have valuable anthelmintic, acaricidal and insecticidal activities. Methods of preparing the compounds are also provided.Type: GrantFiled: July 11, 1994Date of Patent: February 18, 1997Assignee: Sankyo Company LimitedInventors: Yasuhiro Morisawa, Akio Saito, Toshimitsu Toyama, Susumu Kaneko
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Patent number: 5602170Abstract: A method of treating inflammation including administering to a subject an effective amount of a compound of the following formula: ##STR1## wherein m is 1-4; and each of A and B, independently, is H, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, (CH.sub.2).sub.n CHO, (CH.sub.2).sub.o COOH, C.sub.1-7 alkoxy, C.sub.2-7 alkoxyalkyl, C.sub.1-7 hydroxyalkyl, CN, NO.sub.2, halogen, CH(OR.sup.1).sub.2, CO.R.sup.1, NR.sup.2 R.sup.3 or its acid salt, CO.NR.sup.2 R.sup.3, CHR.sup.1 NR.sup.2 R.sup.3 or its acid salt, CH=NR.sup.2, C.tbd.CR.sup.4, CR.sup.1 =CR.sup.5 R.sup.6, CO.CH.dbd.CHR.sup.7, CH.dbd.CHR.sup.8, or COOR.sup.9 ; in which each of n and o, independently, is 0-4; R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 acyl; each of R.sup.2 and R.sup.3, independently is H, C.sub.1-4 alkyl, or C.sub.1-4 hydroxyalkyl; R.sup.4 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, COR.sup.2, COOR.sup.10, C.sub.1-4 hydroxyalkyl or its acid ester or 2-tetrahydropyranyl ether, C.sub.Type: GrantFiled: September 8, 1994Date of Patent: February 11, 1997Assignee: Industrial Technology Research InstituteInventors: Ching-Te Chang, Kuo-Mou Chen, Wann-Huang Liu, Fen-Lan Lin, Rong-Tsun Wu
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Patent number: 5602104Abstract: A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis. In the formula,X represents --CH.dbd.CH--, O or S,R.sub.1 represents hydrogen, branched alkyl having 3-15 carbon atoms, alkoxy having 1-6 carbon atoms or 1-adamantyl, R.sub.2 represents hydroxy, hydrogen, linear or branched alkyl having 1-15 carbon atoms Or alkoxy having 1-6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, or R.sub.1 and R.sub.2 together with the adjacent carbon atoms of the naphthalene ring form a 5 or 6 chain ring optionally substituted by at least one lower alkyl radical, or interrupted by an oxygen atom,R.sub.3 represents --CH.sub.2 OH or --COR.sub.4, or --CH.sub.3 when R.sub.1 and R.sub.2 taken together form a 5 or 6 chain ring,R.sub.4 represents --OR.sub.5 or ##STR2## R.sub.Type: GrantFiled: April 13, 1995Date of Patent: February 11, 1997Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Braham Shroot, Jacques Eustache, Oliver Watts, Jean-Michel Bernardon, Philippe Nedoncelle
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Patent number: 5602130Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O, or NR' where R' is hydrogen or lower alkyl; R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-4; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 14, 1994Date of Patent: February 11, 1997Assignee: AllerganInventor: Roshantha A. Chandraratna
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Anti-tumor compounds, pharmaceutical compositions, methods for preparation thereof and for treatment
Patent number: 5599820Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.Type: GrantFiled: June 5, 1995Date of Patent: February 4, 1997Assignees: The Research Foundation of State University of New York, Indena SpA Gruppo Inverni Della BeffaInventors: Iwao Ojima, Ezio Bombardelli -
Patent number: 5596014Abstract: A pharmaceutical composition containing a compound and an excipient, the compound having the formula: ##STR1## in which n is 2, 3 or 4; R is H, --CH(R.sup.1).cndot.OR.sup.2, --CH(O--Z).sub.2, or --COR.sup.3 ; R.sup.1 is H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, OH, C.sub.1-6 hydroxyalkyl, or COOH; R.sup.2 is H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, tetrahydropyranyl, phenyl, benzoyl, C.sub.1-6 acyl, tosyl, or --CO--Y--COOH; and R.sup.3 is H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, OH, C.sub.1-6 hydroxyalkyl, or COOH; wherein Z is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, or C.sub.1-6 acyl; and Y is C.sub.1-6 alkylidene, C.sub.2-6 alkenylidene, phenylene, or deleted; or an ester or a salt thereof.Type: GrantFiled: June 5, 1995Date of Patent: January 21, 1997Assignee: Industrial Technology Research InstituteInventors: Ching-Te Chang, Rong-Tsun Wu
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Patent number: 5591727Abstract: The invention relates to an insecticidal composition which comprises at least one pyrethroid, at least one UV absorbing agent and at least one antioxidant from the group consisting of tocopherol derivatives and citric acid esters. This insecticidal composition can in particular be used as an emulsion or on a powdery carrier for the control of flying and crawling insects such as flies and cockroaches.Type: GrantFiled: February 7, 1995Date of Patent: January 7, 1997Assignees: Perycut-Chemie AG, Franz BencsitsInventor: Franz Bencsits
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Patent number: 5589501Abstract: A pharmaceutical compound of the formula ##STR1## in which m is 0, 1 or 2, n and q are each 0 or 1 to 5, and p is 0 or 1, X is --CO.sub.2 H or tetrazolyl,Y is --CH.dbd.CH--, andZ is(i) phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(ii) --CHR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(iii) .dbd.CR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, or(iv) ##STR2## where r is 0 or 1 to 3 and the phenyl rings are optionally substituted; provided that when Z is phenyl and m is 1, p is 1; and salts and esters thereof.Type: GrantFiled: November 22, 1994Date of Patent: December 31, 1996Assignees: Eli Lilly and Company, Universite Louis Pasteur, Lilly, S.A.Inventors: Jesus E. Carrera, Almudena R. Esteban, Andr e Mann, Ang ele Schoenfelder, Darryle D. Schoepp, Concepcion P. Tercero, Camille-Georges Wermuth
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Patent number: 5578636Abstract: Novel polythiophene compounds useful as anti-tumor agents are described. Preferred compounds of the formula: ##STR1## wherein n is 0-2 and R.sub.2 and R.sub.3 are optionally substituted 2-thienyl or 3-thienyl have been found to exhibit selective cytotoxic activity against transformed human cells. Pharmaceutical compositions containing the described polythiophene compounds are expected to exhibit good chemotherapeutic activity against slow growing tumors based on tumor cell line assays. A method for treating patients having tumors utilizing the disclosed polythiophene compounds is also described.Type: GrantFiled: April 8, 1994Date of Patent: November 26, 1996Assignees: Purdue Research Foundation, International Technology Research InstituteInventors: Ching T. Chang, Ching-Jer Chang, Chen-Tao Lee, Fen-Lan Lin, Jih-Dar Tsai, Curtis L. Ashendel, Thomas C. K. Chan, Robert L. Geahlen, David J. Waters
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Patent number: 5576338Abstract: Compounds having the Formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.Type: GrantFiled: February 15, 1995Date of Patent: November 19, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Richard Friesen, Yves Ducharme, Daniel Dube', Carole Lepine, Daniel Delorme, Pierre Hamel
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Patent number: 5576317Abstract: The present invention relates to a method of treating or preventing emesis in a mammal, including a human, by administering to the mammal a 5HT.sub.3 receptor antagonist and an NK-1 receptor antagonist (e.g., a substance P receptor antagonist). It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a 5HT.sub.3 receptor antagonist and an NK-1 receptor antagonist.Type: GrantFiled: December 9, 1994Date of Patent: November 19, 1996Assignee: Pfizer Inc.Inventor: Susan F. Gonsalves
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Patent number: 5571825Abstract: The present invention provides a method of selectively inhibiting prostaglandin G/H synthase-2 that comprises administering to a patient in need of such inhibition an inhibiting amount of a compound having the Formula I, II or III ##STR1## wherein the R groups and heterocycles are defined in the disclosure.Type: GrantFiled: March 31, 1995Date of Patent: November 5, 1996Assignee: Warner-Lambert CompanyInventors: Diane H. Boschelli, David T. Connor, Richard D. Dyer, Sonya S. Khatana, James B. Kramer, William H. Roark
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Patent number: 5567717Abstract: A compound of the formula ##STR1## wherein Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in the specification.Type: GrantFiled: June 5, 1995Date of Patent: October 22, 1996Assignee: Sterling Winthrop, Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Theodore J. Nitz
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Patent number: 5556877Abstract: This invention relates to taxoids of general formula (I), their preparation and the pharmaceutical compositions which contain them. The products of general formula (I) have notable antitumoral properties. In the general formula (I),Ar represents an aryl radical,R represents a hydrogen atom or an acetyl or alkoxyacetyl radical,R.sub.1 represents a benzoyl radical or a radical R.sub.2 --O--CO-- in which R.sub.2 represents an alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical, andR.sub.3 represents an alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted aryl (with the exception of unsubstituted phenyl) or heterocyclyl radical.Type: GrantFiled: March 2, 1994Date of Patent: September 17, 1996Assignee: Rhone-Poulenc Rorer S.A.Inventors: Herv e Bouchard, Jean-Dominique Bourzat, Alain Commer.cedilla.on, Jean-Pierre Pulicani
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Patent number: 5556876Abstract: A method of lowering serum cholesterol levels comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R is hydrogen; hydroxy; C.sub.1 -C.sub.6 alkoxy; a group of the formula --O--C(O)--R.sup.a, wherein R.sup.a is hydrogen, C.sub.1 -C.sub.6 alkyl optionally substituted with amino, halo, carbonyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.7 alkanoyloxy, carbamoyl and/or aryl; or R.sup.a is C.sub.1 -C.sub.6 alkenyl optionally substituted with aryl; or R.sup.a is a C.sub.3 -C.sub.7 cycloalkyl; or R.sup.a is aryl optionally substituted with hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, and/or halo; or R.sup.a is --O-aryl;or R is a group of the formula --O--C(O)R.sup.c --O--(C.sub.1 -C.sub.6 alkyl) wherein R.sup.c is a bond or C.sub.1 -C.sub.6 alkanediyl;R.sup.1 is halo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.7 alkyl substituted with C.sub.1 -C.sub.6 alkyl, substituted or unsubstituted C.sub.3 -C.sub.Type: GrantFiled: August 15, 1995Date of Patent: September 17, 1996Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Timothy A. Grese
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Patent number: 5554607Abstract: A method for increasing the HDL cholesterol concentration in the blood of a mammal in need of increased HDL cholesterol blood concentration, which comprises administering to said mammal, orally or parenterally, a compound of formula I: ##STR1## wherein R is alkyl; a substituted or unsubstituted aromatic N, O or S heterocycle; substituted or unsubstituted aryl, arylalkyl, benzhydryl or indanyl, in which the substituents are one to three members independently selected from the group consisting of alkyl, alkoxy, alkylthio, alkenyl, alkynyl, halo, perfluoroalkyl, perfluoroalkyl or hydroxy; and R.sup.1 is aryl, alkyl, alkenyl, alkynyl or substituted aryl where the substituents are one to three members independently selected from the group consisting of alkyl, alkoxy, alkylthio, alkenyl, alkynyl, halo, perfluoroalkyl, perfluoroalkoxy or hydroxy.Type: GrantFiled: November 28, 1995Date of Patent: September 10, 1996Assignee: American Home Products CorporationInventors: Hassan M. Elokdah, Sie-Yearl Chai, Theodore S. Sulkowski, Donald P. Strike
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Patent number: 5552435Abstract: 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: January 9, 1995Date of Patent: September 3, 1996Assignee: Pfizer Inc.Inventor: Kevin Koch
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Patent number: 5541199Abstract: Compounds of the formula: ##STR1## in which n is one of the integers 1, 2, 3,or 4; m is one of the integers 0 or 1; R is ##STR2## or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.Type: GrantFiled: June 2, 1995Date of Patent: July 30, 1996Assignee: American Home Products CorporationInventor: Richard E. Mewshaw
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Patent number: 5538969Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: May 26, 1995Date of Patent: July 23, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talam as, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fern andez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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Patent number: 5530010Abstract: A method of inhibiting demyelinating or dysmyelinating diseases or their symptoms comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.Type: GrantFiled: February 2, 1995Date of Patent: June 25, 1996Assignee: Eli Lilly and CompanyInventor: Andrew L. Glasebrook
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Patent number: 5527829Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: May 23, 1994Date of Patent: June 18, 1996Assignee: Agouron Pharmaceuticals, Inc.Inventor: Vincent J. Kalish
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Patent number: 5525602Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: February 18, 1994Date of Patent: June 11, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: John W. Patterson, David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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Patent number: 5523296Abstract: Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is 0 and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5, R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, CH.sub.2 NR.sub.5 COR.sub.7, CHO, CH(OR.sub.8).sub.2, CHOR.sub.9 O, --COR.sub.10, CR.sub.10 (OR.sub.8).sub.2, or CR.sub.10 OR.sub.9 O, where R.sub.4 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.Type: GrantFiled: November 28, 1994Date of Patent: June 4, 1996Assignee: Allergan, Inc.Inventors: Robert M. Burk, David F. Woodward
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Patent number: 5523312Abstract: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: September 27, 1994Date of Patent: June 4, 1996Assignee: Sterling Winthrop Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman
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Patent number: 5512568Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: February 18, 1994Date of Patent: April 30, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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Patent number: 5506257Abstract: The present invention provides methods for blocking sodium channels in cardiac or neuronal tissue using aminocyclohexylamides. This invention also provides kits including aminocyclohexylamides and instructions for the use of the compounds for the treatment of arrhythmia or for the inducement of local anaesthesia.Type: GrantFiled: February 15, 1994Date of Patent: April 9, 1996Assignee: University of British ColumbiaInventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
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Patent number: 5500425Abstract: Compounds of the formula I ##STR1## processes for their preparation, pharmaceutical preparations, use of and method of treatment of disorders in CNS by using compounds of formula I.Type: GrantFiled: September 9, 1994Date of Patent: March 19, 1996Assignee: Aktiebolaget AstraInventors: Lars-Gunnar Larsson, Lucy A. Renyl, Svante B. Ross, Daniel D. Sohn, Seth-Olov Thorberg
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Patent number: 5494929Abstract: A method of inhibiting effects of growth hormone comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically accepatable salt of solvate thereof.Type: GrantFiled: January 12, 1995Date of Patent: February 27, 1996Assignee: Eli Lilly and CompanyInventor: Timothy A. Grese
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Patent number: 5492927Abstract: This invention encompasses methods for the treatment or prevention of a physiological disorder associated with an excess of tachykinins, said disorder being an allergy which method comprises administering to a mammal in need of said treatment an effective amount of a compound of Formula I ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamthylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.Type: GrantFiled: December 21, 1993Date of Patent: February 20, 1996Assignee: Eli Lilly and CompanyInventors: Bruce D. Gitter, William H. W. Lunn
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Patent number: 5488062Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or the alkali metal salt of a heterocyclic carboxylic acid.Type: GrantFiled: August 9, 1994Date of Patent: January 30, 1996Assignee: Sterling Winthrop Inc.Inventors: Richard P. Dunlap, Dennis J. Hlasta, Ranjit C. Desai, Lee H. Latimer, Chakrapani Subramanyam, John J. Court, Malcolm R. Bell, Virendra Kumar
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Patent number: 5484810Abstract: This invention relates to alkylated sulfonium alkylene derivatives of certain 2H-1-benzopyrans, to the intermediates and processes useful for their preparation, to their free-radical scavenger and cardioprotective properties and to their end-use application as therapeutic agents.Type: GrantFiled: February 28, 1995Date of Patent: January 16, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
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Patent number: 5484805Abstract: The invention concerns a heterocyclene derivative of the formula I ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a 9- or 10-membered bicyclic heterocyclic moiety;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar.sup.2 is optionally substituted 5-membered heterocyclene moiety;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sub.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: July 8, 1994Date of Patent: January 16, 1996Assignees: Imperial Chemical Industries PLC, ICI PharmaInventor: Thomas G. C. Bird
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Patent number: 5482942Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.Type: GrantFiled: June 28, 1994Date of Patent: January 9, 1996Assignee: American Home Products CorporationInventors: Richard M. Soll, Paul J. Dollings
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Patent number: 5482967Abstract: Novel compound represented by the formula: ##STR1## such as 6-Chloro-N-(2,6-diethoxyphenyl)-4-(2-methylphenyl-2-oxo-2H-1-benzopyran-3- acetamide: ##STR2## or a salt thereof. The compound has an excellent activity of inhibiting ACAT, lowering the cholesterol in blood and inhibiting tachykinin receptor. The present invention also relates to the production and use of the disclosed compound.Type: GrantFiled: September 2, 1993Date of Patent: January 9, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Hitoshi Ikeda, Takenori Ishimaru, Takayuki Doi
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Patent number: 5482966Abstract: The invention concerns oxime derivatives of the formula I ##STR1## wherein R.sup.4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and (1-4C)alkyl;R.sup.5 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4C)alkyl and hydroxy-(2-4C)alkyl;Ar.sup.1 is phenylene or a heteroaryl diradical;A.sup.1 is a direct link to X.sup.1, or A.sup.1 is (1-4C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is phenylene or a heteroaryl diradical;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which together with the carbon atom to which A.sup.2 and A.sup.3 are attached define a ring having 5 or 6 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.Type: GrantFiled: June 13, 1994Date of Patent: January 9, 1996Assignees: Zeneca Limited, Zeneca Pharma S.A.Inventors: Thomas G. C. Bird, Patrick Ple
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Patent number: 5478854Abstract: R.sup.g is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Further provided by this invention are pharmaceutical formulations and intermediates for the the preparation of deoxy taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.Type: GrantFiled: March 10, 1994Date of Patent: December 26, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Vittorio Farina, Shu-Hui Chen, David Langley, Mark D. Wittman, Joydeep Kant, Dolatrai M. Vyas
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Patent number: 5474995Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases, ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: January 10, 1994Date of Patent: December 12, 1995Assignee: Merck Frosst Canada, Inc.Inventors: Yves Ducharme, Jacques Y. Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
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Anti-tumor compounds, pharmaceutical compositions, methods for preparation thereof and for treatment
Patent number: 5475011Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and method for treatment of certain cancers with these new compounds.Type: GrantFiled: March 26, 1993Date of Patent: December 12, 1995Assignee: The Research Foundation of State University of New YorkInventors: Iwao Ojima, Ezio Bombardelli