Patents Examined by Hong Liu
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Patent number: 6159966Abstract: A compound of formula (I) ##STR1## its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates, wherein R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are the same or different; R.sup.1 and R.sup.2 together represent along with carbon atoms to which they are attached an aromatic cyclic structure containing 5-6 ring atoms which may optionally be substituted; X represents a heteroatom selected from oxygen or sulfur; R.sup.7 represents hydrogen atom, hydroxy, alkoxy, halogen, lower alkyl group or optionally substituted aralkyl group or forms a bond together with R.sup.8 ; R.sup.8 represents hydrogen atom, hydroxy, alkoxy, halogen, lower alkyl group or optionally substituted aralkyl or R.sup.8 forms a bond together with R.sup.Type: GrantFiled: August 14, 1998Date of Patent: December 12, 2000Assignees: Reddy-Cheminor Inc., Dr. Reddy's Research FoundationInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Ashok Chennaveerappa Bajji, Shivaramayya Kalchar, Sekar Reddy Alla, Rajagopalan Ramanujam, Reeba Kannimel Vikramadithyan
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Patent number: 6156757Abstract: The present invention concerns the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R.sup.1 is independently hydrogen, halogen, C.sub.1-6 alkyl, nitro, hydroxy or C.sub.1-4 alkyloxy; Alk is C.sub.1-6 alkanediyl; n is 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central .alpha..sub.2 -adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.Type: GrantFiled: October 4, 1999Date of Patent: December 5, 2000Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo Edmond Josephine Kennis, Christopher John Love, Paul Fran.cedilla.ois Bischoff
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Patent number: 6156930Abstract: The present invention provides a method for producing trifluoromethanesulfonyl chloride. This method includes the step of reacting trifluoromethanesulfonic acid with phosphorous trichloride and chlorine. With this method, trifluoromethanesulfonyl chloride can be easily and highly selectively produced at high yield. The reaction may be carried out at about atmospheric pressure. Furthermore, the reaction may be carried out in the presence of phosphorus oxychloride either under a pressurized condition or at about atmospheric pressure.Type: GrantFiled: December 28, 1999Date of Patent: December 5, 2000Assignee: Central Glass Company, LimitedInventors: Kaoru Mori, Takanori Hamana, Shigenori Sakai, Tadayuki Kawashima
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Patent number: 6150360Abstract: This invention concerns the use of the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR.sup.4 or N; n is 0, 1, 2, 3 or 4; R.sup.1 and R.sup.2 are each independently selected from hydrogen, hydroxy, C.sub.1-12 alkyl, C.sub.1-12 alkyloxy, C.sub.1-12 alkylcarbonyl, C.sub.1-12 -alkyloxycarbonyl, aryl, amino, mono- or di(C.sub.1-12 alkyl)amino, mono- or di(C.sub.1-12 alkyl)aminocarbonyl wherein each of the aforementioned C.sub.1-12 alkyl groups may optionally and each individually be substituted; or R.sup.1 and R.sup.2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C.sub.1-12 alkyl)aminoC.sub.1-4 alkylidene; R.sup.3 is hydrogen, aryl, C.sub.1-6 alkylcarbonyl, optionally substituted C.sub.1-6 alkyl; and each R.sup.4 independently is hydroxy, halo, C.sub.1-6 alkyl, C.sub.1-6 -alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is --X--R.Type: GrantFiled: March 25, 1999Date of Patent: November 21, 2000Assignee: Janssen Pharmaceutica N.V.Inventors: Frederik Frans Desire Daeyaert, Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici
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Patent number: 6150352Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions in both men and women.Type: GrantFiled: November 12, 1998Date of Patent: November 21, 2000Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Eric E Allen, Matthew J. Wyvratt, Jr., Jinlong Jiang, Richard B. Toupence, Thomas F Walsh, Feroze Ujjainwalla, Jonathan R Young, Robert J. Devita
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Patent number: 6143743Abstract: Corticotropin releasing factor (CRF) antagonists of formula (I): ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.Type: GrantFiled: July 2, 1998Date of Patent: November 7, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Richard Gerald Wilde, Rajagopal Bakthavatchalam, James Peter Beck, Argyrios Georgious Arvanitis
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Patent number: 6133255Abstract: Tricyclic pyridin-2-one analogues which are ligands for GABA.sub.Type: GrantFiled: September 27, 1999Date of Patent: October 17, 2000Assignee: Merck Sharp & Dohme LimitedInventors: Timothy Harrison, Richard Thomas Lewis, Christopher Richard Moyes, Alan Nadin, Andrew Pate Owens
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Patent number: 6127365Abstract: The present invention is directed to compounds of the formula (I): ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9a, R.sup.9b, m and n are as defined herein) which are tachykinin antagonists and which are particularly useful in the treatment of pain, inflammation, migraine, emesis and postherpetic neuralgia.Type: GrantFiled: August 13, 1998Date of Patent: October 3, 2000Assignee: Merck Sharp & Dohme Ltd.Inventors: Jason Matthew Elliott, Fintan Kelleher, Christopher John Swain
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Patent number: 6127374Abstract: This invention provides irreversible inhibitors of tyrosine kinases having for formula ##STR1## which compounds are useful for treating cancer, restenosis, atherosclerosis, endometriosis and psoriasis.Type: GrantFiled: March 25, 1999Date of Patent: October 3, 2000Assignee: Warner-Lambert CompanyInventor: Alexander James Bridges
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Patent number: 6124283Abstract: New piperidinyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula ##STR1## wherein X is N or CH;Y is NR.sub.2 CH.sub.2, CH.sub.2 --NR.sub.2, NR.sub.2 --CO, CO--NR.sub.2 or NR.sub.2 SO.sub.2 ;R.sub.1 is H, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl;R.sub.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or (CH.sub.2).sub.n -aryl,where aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted;n is 0-4;as (R)-enantiomer, (S)-enantiomer or a racemate in the form of the free base or a pharmaceutically acceptable salt or hydrate thereof; a pharmaceutical formulation containing the compounds, use of the compounds in the treatment of 5-hydroxytryptamine mediated disorders, processes for the preparation of the compounds and intermediates for the preparation of the compounds.Type: GrantFiled: April 25, 1997Date of Patent: September 26, 2000Assignee: Astra AktiebolagInventors: Stefan Berg, Lennart Florvall, Svante Ross, Seth-Olov Thorberg
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Patent number: 6117869Abstract: The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds ##STR1## More particularly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurysm, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, osteoporosis, rheumatoid or osteoarthritis, renal disease, left ventricular dilatation, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: July 26, 1999Date of Patent: September 12, 2000Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Bruce David Roth, Drago Robert Sliskovic
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Patent number: 6110915Abstract: A class of substituted 7,8-ring fused 1,2,4-triazolo[4,3-b]pyridazine derivatives, as shown in Formula I, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-position, are selective ligands for GABA.sub.A receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of emesis.Type: GrantFiled: December 8, 1998Date of Patent: August 29, 2000Assignee: Merck & Co., Inc.Inventors: Jose Luis Castro Pineiro, Frederick David Tattersall
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Patent number: 6107294Abstract: The present invention describes novel thiazolo[4,5-d]pyrimidines of formula: ##STR1## wherein R.sup.3 is a substituted aromatic or heteroaromatic group, or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.Type: GrantFiled: March 31, 1999Date of Patent: August 22, 2000Assignee: Dupont PharmaceuticalsInventor: James Peter Beck
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Patent number: 6080738Abstract: A heterocyclic amide compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and a pharmaceutical use thereof. The heterocyclic amide compound and a pharmacologically acceptable salt thereof of the present invention have superior inhibitory action on chymase group in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be used for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.Type: GrantFiled: April 22, 1999Date of Patent: June 27, 2000Assignee: Yoshitomi Pharmaceuticals Industries, Ltd.Inventors: Fumihiko Akahoshi, Atsuyuki Ashimori, Takuya Yoshimura, Masahiro Eda, Hiroshi Sakashita, Masahide Nakajima, Teruaki Imada
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Patent number: 6075019Abstract: The invention relates to novel S-aryl-dithiazine dioxides, to processes for their preparation and to the use in crop protection and in the protection of materials.Type: GrantFiled: June 23, 1999Date of Patent: June 13, 2000Assignee: Bayer AktiengesellschaftInventors: Hermann Uhr, Martin Kugler, Peter Wachtler
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Patent number: 6071909Abstract: The present patent application discloses compounds having formula (I) ##STR1## or a pharmaceutically acceptable salt thereof or an oxide thereof, wherein R.sup.3 is (II), ##STR2## wherein A, B and D each is CH, or one or two of A, B and D is N and the others are CH; R.sub.11 is phenyl, benzimidazolyl, or monocyclic heteroaryl all of which may be substituted one or more times with substituents selected from alkyl, alkoxy, phenyl, halogen, CF.sub.3, amino, nitro, cyano, acyl, acylamino, phenyl and monocyclic heteroaryl; and one of R.sup.6 and R.sup.7 is hydrogen and the other is furanyl or isoxazolyl each of which may be substituted one or more times with substituents selected from halogen, alkyl, alkoxy and phenyl. The compounds are useful for the treatment of various central nervous system disorders such as epilepsy and other convulsive disorders, anxiety, sleep disorders and memory disorders.Type: GrantFiled: July 20, 1999Date of Patent: June 6, 2000Assignee: Merck Sharpe & Dohme Ltd.Inventors: Timothy Harrison, Timothy Jason Sparey, Martin Richard Teall
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Patent number: 6063784Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the application and its non-toxic, pharmaceutically acceptable acid addition salts which are useful for treating hypertension.Type: GrantFiled: March 10, 1999Date of Patent: May 16, 2000Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S. )Inventors: Dennis Bigg, Marie-Odile Galcera
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Patent number: 6057326Abstract: Novel and known bicyclic 4-aralkylaminopyrimidine derivatives of formula (I) wherein A is a benzene or imidazole ring; B is a benzene, tetralin, indane or 2-oxindole ring R is (C.sub.1 -C.sub.4)perfluoroalkyl, phenyl, phenyl-(C.sub.1 -C.sub.4)alkyl, hydroxy-(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy-(C.sub.1 -C.sub.4)alkyl, (C.sub.2 -C.sub.4)acyloxy-(C.sub.1 -C.sub.4)alkyl, halobenzoyloxy-(C.sub.1 -C.sub.4)alkyl, carboxy, carbamoyl, (C.sub.1 -C.sub.4)alkoxycarbonyl, cyano, (C.sub.1 -C.sub.4)alkylcarbonyl, carboxy-(C.sub.1 -C.sub.4)alkyl, carbamoyl-(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxycarbonyl-(C.sub.1 -C.sub.4)alkyl, halo-(C.sub.1 -C.sub.4)alkyl, amino-(C.sub.1 -C.sub.4)alkyl, mono- or di-(C.sub.1 -C.sub.4)alkylamino-(C.sub.1 -C.sub.4)alkyl, sulfo-(C.sub.1 -C.sub.4)alkyl or sulfamido-(C.sub.1 -C.sub.4)alkyl; each of R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen or --NR.sub.5 R.sub.6 in which each of R.sub.Type: GrantFiled: February 6, 1998Date of Patent: May 2, 2000Assignee: Pharmacia & Upjohn S.p.AInventors: Maria Gabriella Brasca, Dario Ballinari, Antonio Longo, Franco Buzzetti
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Patent number: 6046135Abstract: 1,3-Oxazin-4-one derivatives of formula (I): ##STR1## wherein Q represents --C(.dbd.O)--, --CH(OH)-- or --C(OR.sup.11)(OR.sup.11)--, in which R.sup.11 represents lower alkyl; or the two groups --OR.sup.11, together with the carbon atom to which they are attached, form a five or six membered cyclic ketal group; and their use as herbicides.Type: GrantFiled: September 2, 1998Date of Patent: April 4, 2000Assignees: Rhone-Poulenc Agriculture Ltd, Mitsubishi Chemical CorporationInventors: Michael Colin Cramp, Yoshihiro Usui, Sachio Kudo