Benzothiazines (including Hydrogenated) Patents (Class 544/49)
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Publication number: 20080119647Abstract: A process for purifying meloxicam form I from a crude meloxicam, which comprises: i. contacting the crude meloxicam with an amine in a non-aqueous solvent to form a meloxicam salt; ii. isolating the meloxicam salt; iii. dissolving the meloxicam salt in an aqueous solvent to form a salt solution; and iv. adding an acid to the salt solution to precipitate free meloxicam.Type: ApplicationFiled: November 15, 2007Publication date: May 22, 2008Inventors: Liam McElroy, Lillian Cromie, Mark Garret
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Patent number: 7375220Abstract: A method of treating or preventing of a disease or condition associated with an increased level of isoforms of amyloid ? peptides (A?) and/or with a changed ratio of levels of A? isoforms and/or with the formation of plaques containing amyloid ? peptide (A?) isoforms in a mammal comprising administering to said mammal an therapeutically effective amount of a compound selected from the formulas Ia, Ib wherein V, W, Y, R2, R3, R5, R6, L1 and i are defined as in claim 1.Type: GrantFiled: May 19, 2005Date of Patent: May 20, 2008Assignees: Boehringer Ingelheim Vetmedica GmbH, Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Klaus Bornemann, Guenter Trummlitz, Edward S. Lazer, Clara K. Miao, Bernd Beck, Frank Sams-Dodd, Dagmar Kugler, Klaus Klinder, Cornelia Dorner-Ciossek, Marcus Kostka
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Patent number: 7262190Abstract: The invention relates to compounds of formula (I): wherein: R1 represents hydrogen, alkyl or cycloalkyl, R2 represents hydrogen, halogen or hydroxy, A represents CR3R4 or NR3 wherein R3 and R4 are as defined in the description, Y represents an alkylene chain as described in the description, X represents NR5R6, S(O)nR7, OR8, C(O)R9, amidino or a heterocycle, their isomers, and addition salts thereof; and medicinal products containing the same which are useful in the prevention or treatment of diseases associated with AMPA flux.Type: GrantFiled: December 8, 2005Date of Patent: August 28, 2007Assignee: Les Laboratoires ServierInventors: Patrice Desos, Alexis Cordi, Pierre Lestage, Laurence Danober
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Patent number: 7232826Abstract: The present invention provides compounds of Formula I or II that are useful as anti-cancer agents and other diseases that can be treated by inhibiting tyrosine kinase enzymesType: GrantFiled: September 29, 2003Date of Patent: June 19, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Upender Velaparthi, Mark D. Wittman
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Patent number: 7199118Abstract: This invention relates to novel benzothiazine derivatives of Formula I useful as modulators of the AMPA sensitive glutamate receptors, pharmaceutical compositions comprising such compounds and their use in therapy.Type: GrantFiled: October 2, 2002Date of Patent: April 3, 2007Assignee: NeuroSearch A/SInventors: Alex Haahr Gouliaev, Morgens Larsen, Thomas Varming, Claus Mathiesen, Tina Holm Johansen, Karin Sandager Nielsen, Barbara Hartz, Jorgen Scheel-Kruger
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Patent number: 7101428Abstract: The invention is directed to a method or use of 2,9-dichloro-quinacridone as a crystal phase inhibitor during the beta-quinacridone or gamma-quinacridone crude pigment particle size reduction processes. 2,9-dichloroquinacridone is added to the milling composition of the crude gamma or crude beta quinacridone.Type: GrantFiled: November 12, 2004Date of Patent: September 5, 2006Assignee: Ciba Specialty Chemicals CorporationInventors: Yingxia He, Colin Campbell, Gordian Schilling, Rhonda Carter
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Patent number: 6967248Abstract: The invention relates to the new crystalline forms II, III and V of meloxicam; to the processes for obtaining the crystalline forms I, II, III and V; and, finally, to the interconversion processes of the forms II, III, IV and V into the form I.Type: GrantFiled: December 9, 2002Date of Patent: November 22, 2005Assignee: Esteve Quimica, SAInventors: Laura Coppi, Marti Bartra Sanmarti, Montserrat Closa Clavo
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Patent number: 6960579Abstract: Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for treating sleep disorders, depression, and other psychiatric disorders, such as, schizophrenia, anxiety, obsessive compulsive disorder, circadian rhythm disorders, and centrally and peripherally mediated hypertension. Compositions and methods for their use are also disclosed.Type: GrantFiled: May 10, 1999Date of Patent: November 1, 2005Assignee: Alcon Manufacturing, Ltd.Inventors: Jesse A. May, Thomas R. Dean, Najam A. Sharif, Hwang-Hsing Chen
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Patent number: 6894041Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recitType: GrantFiled: November 20, 2002Date of Patent: May 17, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6881840Abstract: This relates to a dye represented by Formulae II and IIA below: wherein; R1 represents a hydrogen, an aryl group containing 6 to 14 carbon atoms, or an alkyl group containing 1 to 12 carbon atoms, R2 and R3 together form an aromatic, carbocyclic or heterocyclic ring system containing 6 to 14 atoms; X represents a sulfoxide (S?O), sulfone (SO2), or dicyanovinyl (C(CN)2) group; Y represents a sulfoxide (S?O), sulfone (SO2), carbonyl (C?O) or dicyanovinyl (C(CN)2) group; L1, L2, and L3 represent methine groups, wherein the methine groups may combine to form a 5- or 6-membered ring when m is equal to or >1; m is 0, 1, 2, or 3; W is an aryl group; and D is a moiety in conjugation with the X and Y groups.Type: GrantFiled: February 8, 2002Date of Patent: April 19, 2005Assignee: Eastman Kodak CompanyInventors: Margaret J. Helber, Douglas M. Willis, John DiCillo
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Patent number: 6869945Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems reType: GrantFiled: November 20, 2002Date of Patent: March 22, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6869948Abstract: The invention relates in its first aspect to a rapidly decomposing tablet for pain therapy containing meloxicam [4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide] in the form of a salt with an inorganic or organic base providing rapid absorption of the active substance, the process of its preparation by direct tabletting, and furthermore relates in a second aspect to the crystalline meloxicam meglumin salt mono- and dihydrate and the preparation thereof.Type: GrantFiled: March 26, 1999Date of Patent: March 22, 2005Assignee: Boehringer Ingelheim Pharma KGInventors: Thomas Bock, Paul Saegmueller, Peter Sieger, Dietrich Tuerck
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Patent number: 6869974Abstract: Compounds or their salts having general formulas (I) and (II): wherein s is an integer equal to 1 or 2, A is the radical of a drug that satisfies certain pharmacological tests, C and C1 are bivalent radicals, and precursors of the radicals B and B1 satisfy certain pharmacological tests.Type: GrantFiled: April 11, 2000Date of Patent: March 22, 2005Assignee: Nicox S.A.Inventor: Piero Del Soldato
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Patent number: 6844338Abstract: A pharmaceutical compound of the formula (I) in which R1 and R2 are each hydrogen or C1-6 alkyl, R3 is —SR10, —SOR10, —SO2R10, —COR10, —CH2OH or —CONHR11, where R10 is C1-6 alkyl and R11 is hydrogen or C1-6 alkyl, R4, R5, R6 and R7 are each hydrogen or C1-6alkyl, provided that at least one of R4, R5, R6 and R7 is C1-6alkyl, R8 and R9 are each hydrogen, halo, C1-6 alkyl or cyano, n is 0 or 1 and m is 2 or 3, x is a (a) or (b), and y is (c) or (d), wherein R12 and R13 are each hydrogen, C1- alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl; and salts thereof.Type: GrantFiled: May 4, 2001Date of Patent: January 18, 2005Assignee: Eli Lilly and CompanyInventors: John Fairhurst, Peter Gallagher
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Publication number: 20040267010Abstract: Compounds possessing 5HT7 activity of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: 1Type: ApplicationFiled: July 27, 2004Publication date: December 30, 2004Inventors: Ian Thomson Forbes, Andrew Derrik Gribble
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Publication number: 20040254371Abstract: Compounds of formula (I): 1Type: ApplicationFiled: June 10, 2004Publication date: December 16, 2004Inventors: Patrice Desos, Alex Cordi, Pierre Lestage
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Publication number: 20040242571Abstract: This invention relates to novel benzothiazine derivatives of Formula I useful as modulators of the AMPA sensitive glutamate receptors, pharmaceutical compositions comprising such compounds and their use in therapy.Type: ApplicationFiled: March 15, 2004Publication date: December 2, 2004Inventors: Alex Haahr Gouliaev, Morgens Larsen, Thomas Varming, Claus Mathiesen, Tina Holm Johansen, Karin Sandager Nielsen, Barbara Hartz, Jorgen Scheel-Kruger
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Publication number: 20040230054Abstract: Compounds of formula I: 1Type: ApplicationFiled: May 14, 2004Publication date: November 18, 2004Inventors: Kevin Dinnell, Timothy Harrison, Alan John Nadin, Andrew Pate Owens, Duncan Edward Shaw, Brian John Williams
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Publication number: 20040176355Abstract: The present invention discloses compounds which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In other aspects, the invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: ApplicationFiled: February 26, 2004Publication date: September 9, 2004Applicant: Schering CorporationInventors: Thavalakulamgara K. Sasikumar, Wen-Lian Wu, Duane A. Burnett, Li Qiang
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Publication number: 20040171611Abstract: The present invention relates to a new crystalline modification of the compound 4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazin-3-carboxamide-1,1-dioxide in the form of an acetic acid solvate of formula I as well as the use thereof as a pharmaceutical composition.Type: ApplicationFiled: September 22, 2003Publication date: September 2, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Guenter Trummlitz, Rainer Soyka, Peter Sieger, Ulrike Werthmann, Peter Luger
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Publication number: 20040138211Abstract: Disclosed are the preparation and pharmaceutical use of novel noncyclic 1,3-dicarbonyl compounds of formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Y, Z, Q, Ar and n are as defined in the specification. These compounds, as peroxisome proliferator-activated receptor (PPAR) dual agonists for both RXR/PPARgamma and RXR/PPARalpha heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders.Type: ApplicationFiled: November 14, 2003Publication date: July 15, 2004Inventors: Xian-Ping Lu, Zhibin Li, Chenzhong Liao, Leming Shi, Zhende Liu, Zhiqiang Ning, Song Shan, Tuo Deng, Baoshun Ma
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Patent number: 6759406Abstract: Compounds of formula corresponding to either formula (Ia) or (Ib): wherein: M represents a molecule that can be used for the treatment or diagnosis of pathologies caused by attack on the cartilage, R1, R2 and R3 represent an alkyl group, or R1, R2 and R3, together with the nitrogen atom carrying them, form a heterocycle, X represents a (C1-C6)alkylene chain in which one or more —CH2— groups are optionally replaced by a sulphur atom, an oxygen atom, or an —NR—, —CO—, —CO—NH—, —CO2—, —SO— or —SO2— group, n represents 0 or 1, Hal represents a halogen atom, or, R4 represents an alkyl group, Hal represents a halogen atom, represents a molecule that can be used for the treatment or diagnosis of pathologies caused by attack on the cartilage, wherein the nitrogen atom may optionally be included in a saturated or unsaturated nitrogen-containing heterocyclic system, or iType: GrantFiled: March 25, 2002Date of Patent: July 6, 2004Assignees: Les Laboratoires Servier, INSERMInventors: Jean-Claude Madelmont, Isabelle Giraud, Colette Nicolas, Jean-Claude Maurizis, Maryse Rapp, Monique Ollier, Pierre Renard, Daniel-Henri Caignard
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Publication number: 20040116413Abstract: The present invention provides compounds of formula I useful as antimicrobial agents 1Type: ApplicationFiled: November 14, 2001Publication date: June 17, 2004Inventors: Michael J. Genin, Michael Robert Barbachyn, Jackson B. Hester, Paul D. Johnson, Fred L. Ciske
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Publication number: 20040063696Abstract: 1 wherein: represents a single or double bond, R1 represents a hydrogen atom or a hydroxy, alkoxy, acyloxy, alkylsulphonyloxy, arylsulphonyloxy or arylalkoxy group, R2 represents a hydrogen atom or an alkyl group, R3 and R4, which may be identical or different, each represent a hydrogen atom, a halogen atom or an alkyl, hydroxy or alkoxy group, Ak represents an alkylene chain, R5, R6 and R7, which may be identical or different, each represent an alkyl group, or R5, R6 and R7, taken together with the nitrogen atom carrying them, form a saturated or unsaturated nitrogen-containing heterocycle,Type: ApplicationFiled: June 20, 2003Publication date: April 1, 2004Inventors: Jean-Claude Madelmont, Isabelle Giraud, Aurelien Vidal, Emmanuelle Mounetou, Maryse Rapp, Jean-Claude Maurizis, Pierre Renard, Daniel-Henri Caignard, Jean-Guy Bizot-Espiard
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Patent number: 6713477Abstract: A hydroxamic acid derivative represented by formula (1) or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which has a matrix metalo-proteinase inhibitor.Type: GrantFiled: November 9, 2001Date of Patent: March 30, 2004Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Gerard Robert Scarlato, Sara Sabina Hadida Ruah, Tamiki Nishimura, Masashi Nakatsuka, Fumio Samizo, Yumiko Kamikawa, Hitoshi Houtigai
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Publication number: 20040039198Abstract: This invention relates to 2-pyridyl substituted diarylimidazoles which are inhibitors of the transforming growth factor, (“TGF”)-&bgr; signaling pathway, in particular, the phosphorylation of smad2 or smad3 by the type I or activin-like kinase (“ALK”)-5 receptor, methods for their preparation and their use in medicine.Type: ApplicationFiled: May 14, 2003Publication date: February 26, 2004Inventors: Paul E. Bender, Joelle L. Burgess, James F. Callahan
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Patent number: 6683101Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof.Type: GrantFiled: December 3, 2002Date of Patent: January 27, 2004Assignee: Warner-Lambert CompanyInventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Publication number: 20040006062Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: 1Type: ApplicationFiled: May 5, 2003Publication date: January 8, 2004Inventors: Joanne M. Smallheer, Donald J. Pinto, Shuaige Wang, Jennifer X. Qiao, Wei Han, Zilun Hu
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Publication number: 20040002491Abstract: The invention concerns compounds of formula (1): R-A-R′ wherein: A is as defined in the description; R represent a group (V), (VI), (VII), or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description, and medicaments containing the same.Type: ApplicationFiled: June 16, 2003Publication date: January 1, 2004Inventors: Daniel Lesieur, Frederique Klupsch, Gerald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renard, Philippe Delagrange
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Publication number: 20030236252Abstract: Described are bicycle-substituted cyclohexylamines of Formula (I) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's specification. disease. The substituents are defined in the specification.Type: ApplicationFiled: November 12, 2002Publication date: December 25, 2003Inventors: Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Publication number: 20030232810Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.Type: ApplicationFiled: December 3, 2002Publication date: December 18, 2003Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Patent number: 6664251Abstract: Disclosed are benzothiazine derivatives represented by the following formula (I): wherein the dashed line indicates the presence or absence of a bond; Z represents one of the following groups: in which R1 and R2 individually represent alkyl, aralkyl or the like, R3 represents H, alkyl or the like, R4 represents H, aralkyl or the like, X1, X2 and X3 individually represent O or S, and G represents substituted or unsubstituted ethylene, trimethylene or the like; Q1 and Q2 individually represent H, OH, halogen, alkoxy or the like; A represents alkylene, alkenylene or the like; Y represents CH, C═ or N; when Y is CH, m stands for 0 or 1, n stands for 1 or 2, B represents O, S, carbonyl or the like, when Y is C═, m stands for 1, n stands for 1 or 2, B represents: in which the double bond is linked to Y, R6 represents substituted or unsubstituted aryl or the like; when Y is N, m stands for 0 or 1, n stands for 2 or 3 and B represents carbonyl, sulfonylType: GrantFiled: September 19, 2001Date of Patent: December 16, 2003Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
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Patent number: 6642383Abstract: Compounds of the formula (I) wherein p is zero or 1; q and r, independently of each other, are an integer from 1 to 6; and s is a number ranging from 1 to 8; X is —O— or, when p is 1, X is also a group Rw, Rx, Ry and Rz are, independently of each other, C1-C18alkyl, C5-C12cycloalkyl or C1-C5hydroxyalkyl, especially methyl; R1 is hydrogen; C1-C18alkyl; oxyl; OH; CH2CN; C1-C18alkoxy; C5-C12cycloalkoxy; C3-C8alkenyl; C3-C8alkynyl; C7-C12phenylalkyl; C7-C15phenylalkyl, which is substituted on the phenyl ring by 1, 2 or 3 radicals selected from C1-C4alkyl and C1-C4alkoxy; C7-C15phenylalkoxy; C7-C15phenylalkoxy, which is substituted on the phenyl ring by 1, 2 or 3 radicals selected from C1-C4alkyl and C1-C4alkoxy; or R1 is C1-C8alkanoyl; C3-C5alkenoyl; C1-C18alkanoyloxy; glycidyl; or a group —CH2CH(OH)—G, in which G is hydrogen, methyl or phenyl; R2 is hydrogen, C1-C8alkyl, C5-C12cycloalkyl or C1-C4hydroxyalkyl; R3, R4, R5 independently of each otherType: GrantFiled: May 15, 2001Date of Patent: November 4, 2003Assignee: Ciba Specialty Chemicals CorporationInventors: Dario Lazzari, Graziano Zagnoni, Mirko Rossi, Alessandro Zedda, Valerio Borzatta, Stephen Mark Andrews
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Publication number: 20030195216Abstract: A compound selected from those of formula (I): 1Type: ApplicationFiled: July 12, 2002Publication date: October 16, 2003Inventors: Solo Goldstein, Guillaume Poissonnet, Jean-Gilles Parmentier, Pierre Lestage, Brian Lockhart
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Publication number: 20030139389Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:Type: ApplicationFiled: December 11, 2002Publication date: July 24, 2003Applicant: SmithKline Beecham p.l.c.Inventors: Francis David King, Laramie Mary Gaster, Keith Raymond Mulholland
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Publication number: 20030109701Abstract: The invention relates to the new crystalline forms II, III and V of meloxicam; to the processes for obtaining the crystalline forms I, II, III and V; and, finally, to the interconversion processes of the forms II, III, IV and V into the form I.Type: ApplicationFiled: December 9, 2002Publication date: June 12, 2003Inventors: Laura Coppi, Marti Bartra Sanmarti, Montserrat Closa Clavo
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Publication number: 20030087898Abstract: The subject invention provides a compound of the formula 1, 1Type: ApplicationFiled: October 22, 2002Publication date: May 8, 2003Applicant: Pfizer Inc.Inventors: Stanton F. McHardy, Spiros Liras, Steven D. Heck
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Patent number: 6559144Abstract: Compounds of the formula I in which X, Y, Z, R1, R2, R3, R4, R5, R7, R8, R11, m and n have the meanings stated in claim 1, and their physiologically acceptable salts can be used as integrin inhibitors, in particular for the prophylaxis and treatment of circulatory disorders, for thrombosis, myocardial infarct, coronary heart disease, arteriosclerosis, osteoporosis, for pathological processes maintained or propagated by angiogenesis, and in tumour therapy.Type: GrantFiled: April 26, 2001Date of Patent: May 6, 2003Assignee: Merck Patent Gesellschaft MitInventors: Beate Diefenbach, Simon L. Goodman, Joachim März, Peter Raddatz, Friedrich Rippmann, Matthias Wiesner
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Publication number: 20030078256Abstract: Disclosed are benzothiazine derivatives represented by the following formula (I): 1Type: ApplicationFiled: September 19, 2001Publication date: April 24, 2003Applicant: SUNTORY LIMITEDInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
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Patent number: 6545150Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.Type: GrantFiled: December 5, 2001Date of Patent: April 8, 2003Assignee: Warner-Lambert CompanyInventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
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Publication number: 20030055051Abstract: The present invention provides an ophthalmic aqueous pharmaceutical preparation, which is excellent in anti-inflammatory effect, which is less stimulative and which has high safety and excellent storage stability. The ophthalmic aqueous pharmaceutical preparation comprises meloxicam and trometamol.Type: ApplicationFiled: May 24, 2002Publication date: March 20, 2003Applicant: WAKAMOTO PHARMACEUTICAL CO., LTD.Inventors: Daisuke Morizono, Hidekazu Suzuki, Masanobu Takeuchi, Kenji Naito
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Publication number: 20020173506Abstract: The invention is directed to physiologically active compounds of general formula (I):Type: ApplicationFiled: October 11, 2001Publication date: November 21, 2002Inventors: David Edward Clark, Paul Robert Eastwood, Neil Victor Harris, Clive McCarthy, Andrew David Morley, Stephen Dennis Pickett
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Patent number: 6448241Abstract: Compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof, processes for preparing them and the medicaments containing them are discussed.Type: GrantFiled: May 24, 2001Date of Patent: September 10, 2002Assignee: Aventis Pharma S.A.Inventors: Jean-Claude Hardy, Jean Bouquerel, Patrick Nemecek, Jean-Claude Aloup, Serge Mignani, Jean-François Peyronel
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Patent number: 6440962Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula I The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.Type: GrantFiled: March 27, 2001Date of Patent: August 27, 2002Assignee: Warner-Lambert CompanyInventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
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Patent number: 6436927Abstract: The present invention involves certain 8-ureido and 8-thioureido, 1,2-benzothiazines, 1,2,4-benzothioxazines and 1,2,4-benzothiodiazines useful in the treatment of disease states mediated by the chemokine, Interleukin-8.Type: GrantFiled: July 7, 1999Date of Patent: August 20, 2002Assignee: SmithKline Beecham CorporationInventors: Hong Nie, Katherine L. Widdowson
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Publication number: 20020094980Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 1Type: ApplicationFiled: December 5, 2001Publication date: July 18, 2002Inventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
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Publication number: 20020019394Abstract: Novel compounds of formulae I or Ia: 1Type: ApplicationFiled: March 26, 2001Publication date: February 14, 2002Inventors: Wenhao Li, Charles K. Marlowe, Robert M. Scarborough
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Patent number: 6329366Abstract: A pharmaceutical compound of the formula in which R1 and R2 are each hydrogen, halo, cyano or methyl, the dotted line represents an optional double bond, where R4 and R5 are each hydrogen, C1-6 alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl, n is 0 or 1, and R3 is —SR6, —SOR6, —SO2R6, —COR6, —CH2OH or —CONHR7, where R6 is C1-6 alkyl and R7 is hydrogen or C1-6 alkyl; provided that when one of R1 and R2 is hydrogen and the other is fluoro, R4 and R5 are each hydrogen or C1-6 alkyl, and n is 0, then R3 is not —COR6 or —CONHR7; and salts thereof.Type: GrantFiled: November 18, 1999Date of Patent: December 11, 2001Assignee: Eli Lilly and Company LimitedInventors: John Fairhurst, Peter Thaddeus Gallagher, Martin Victor Miles
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Patent number: 6316413Abstract: The invention concerns a pseudopeptide compounds selected among the set constituted by: (i) the compounds of formula (I): in which: A1 represents a single bond, D-Arg or L-Lys; A2 represents L-Pro or trans-4-hydroxy-L-Pro (4Hyp); A3 represents L-Phe or L-thienylalanine (Thi); Y represents a hydrogen atom or a C1-C3 alkyl group; X represents a sulphur or oxygen atom; and, (ii) their additive salts. The invention also concerns the preparation and use of this compound and its additive salts in therapy.Type: GrantFiled: June 4, 1999Date of Patent: November 13, 2001Assignee: Fournier Industrie et SanteInventors: Pierre Dodey, Jean-Michel Luccarini, Jean Martinez, Muriel Amblard, Isabelle Daffix
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Publication number: 20010036944Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 1Type: ApplicationFiled: March 27, 2001Publication date: November 1, 2001Inventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean