The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/253)
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Patent number: 7163942Abstract: The present invention relates to compounds of the Formula I wherein R1, R2, R3, m, and n are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating disorders and diseases, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.Type: GrantFiled: March 11, 2005Date of Patent: January 16, 2007Assignee: Pfizer Inc.Inventors: Michael A. Brodney, Karen J. Coffman
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Patent number: 7153972Abstract: A method for producing a compound represented by the formula: wherein the ring A is a benzene ring which may be substituted in addition to the R? group; R1 is hydrogen or an optionally substituted hydrocarbon residue; X is a direct bond or a spacer having an atomic length or two or less between the phenylene group and the phenyl group; Y is —O—, —S(O)m- or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; R? is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or a group convertible thereinto; n is an integer of 1 or 2; or a salt thereof, which comprises deprotecting a compound represented by the formula: wherein R is triphenylmethyl, 2-tetrahydropyranyl, methoxymethyl or ethoxy methyl, the other symbols as defined above; or a salt thereof.Type: GrantFiled: November 19, 2004Date of Patent: December 26, 2006Assignee: Takeda Pharmaceutical Company, LimitedInventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Patent number: 7138414Abstract: The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives. Compounds are described of the formula I where the radicals are defined as specified, and also their pharmaceutically acceptable salts and processes for their preparation. The compounds are suitable, for example, for treating type 2 diabetes.Type: GrantFiled: July 11, 2003Date of Patent: November 21, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Karl Schoenafinger, Elisabeth Defossa, Dieter Kadereit, Erich Von Roedern, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt
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Patent number: 7119090Abstract: The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: February 25, 2002Date of Patent: October 10, 2006Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 7115749Abstract: The present invention provides compounds of formula I wherein X and R1–R7 are as defined herein.Type: GrantFiled: October 26, 2005Date of Patent: October 3, 2006Assignee: Schering CorporationInventors: Gerald W. Shipps, Jr., Tong Wang, Kristin E. Rosner, Patrick J. Curran, Alan B. Cooper, Viyyoor M. Girijavallabhan
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Patent number: 7112600Abstract: The present invention provides a fused ring compound of the following formula [I] ? wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. The compound of the present invention shows an anti-hepatitis C virus (HCV) action based on the HCV polymerase inhibitory activity, and is useful as a therapeutic agent or prophylactic agent for hepatitis C.Type: GrantFiled: June 26, 2002Date of Patent: September 26, 2006Assignee: Japan Tobacco Inc.Inventors: Hiromasa Hashimoto, Kenji Mizutani, Atsuhito Yoshida
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Patent number: 7109223Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.Type: GrantFiled: August 25, 2003Date of Patent: September 19, 2006Assignee: Merck & Co. Inc.Inventors: Yongxin Han, John Colucci, Xavier Billot, Marie-Claire Wilson, Robert Young
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Patent number: 7105557Abstract: Provided are crystalline and amorphous form of valsartan, and processes for their preparation.Type: GrantFiled: May 27, 2005Date of Patent: September 12, 2006Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Igor Rukhman, Evgeni Flyaks, Tamas Koltai, Judith Aronhime
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Patent number: 7087631Abstract: The present invention relates to 5-Aryltetrazole Compounds, compositions comprising an effective amount of a 5-Aryltetrazole Compound, and methods for treating an inflammation disease, a reperfusion disease, or hyperuricemia in an animal in need thereof comprising administering to the animal an effective amount of a 5-Aryltetrazole compound.Type: GrantFiled: July 17, 2003Date of Patent: August 8, 2006Assignee: Inotek Pharmaceuticals CorporationInventors: Alex Nivorozhkin, John Van Duzer, Garry Southan, Siya Ram, Qi Zeng
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Patent number: 7078423Abstract: The present invention relates to 5-Aryltetrazole compounds, compositions comprising a 5-Aryltetrazole compound, and methods for treating an inflammation disease, a reperfusion disease, hyperuricemia, gout, or tumor-lysis syndrome in an animal in need thereof comprising administering to the animal an effective amount of a 5-Aryltetrazole compound.Type: GrantFiled: July 18, 2002Date of Patent: July 18, 2006Assignee: Inotek Pharmaceuticals CorporationInventors: Alex Nivorozhkin, John Van Duzer, Andrew Salzman, Garry Southan, Siya Ram, Qi Zeng, Csaba Szabo
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Patent number: 7067546Abstract: A process for producing crystals of 2-ethoxy-1-[[2?-(1H-tetrazol-5-yl) biphenyl-4-yl]methyl]-1H-benzimdazole-7-carboxylic acid (compound (I)), characterized by dissolving or suspending the compound (I) or a salt thereof in a solvent comprising an aprotic polar solvent and crystallizing it. By the process, the contaminants which are contained in the compound (I) or its salt and are difficult to remove, such as tin compounds, analogues of the compound (I), and a residual organic solvent, can be easily removed. Crystals of the compound (I) can be efficiently and easily mass-produced in high yield on an industrial scale.Type: GrantFiled: August 1, 2002Date of Patent: June 27, 2006Assignee: Takeda Pharmaceutical CompanyInventors: Hideo Hashimoto, Hideaki Maruyama
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Patent number: 7063928Abstract: This invention relates to a novel organophotoreceptor that includes: (a) a charge transport material comprising a fluorenone hydrazone having a) least two fluorenone alkylsulfonylphenylhydrazone groups, b) at least two fluorenone pyrrolylhydrazone groups, c) at least two fluorenone benzotriazolylhydrazone groups, d) at least two fluorenone sulfolanylhydrazone groups, e) at least two fluorenone pyrazolylhydrazone groups, f) at least two fluorenone naphthylhydrazone groups, g) at least two fluorenone tetrazolylhydrazone groups, h) at least two fluorenone stilbenylhydrazone groups, or i) at least two fluorenone (9H-fluoren-9-ylidene)benzylhydrazone groups. Some of these fluoreneones may be represented by the formula where n is an integer between 2 and 6, inclusive; R1 is hydrogen, alkyl, or aryl; R2 is alkylsulfonylphenyl or one of its derivatives; X is a linking group having the formula —(CH2)m—, branched or linear.Type: GrantFiled: November 5, 2004Date of Patent: June 20, 2006Assignee: Samsung Electronics Co Ltd.Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katritzky, Ritu Jain, Rexiat Maimait
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Patent number: 7038060Abstract: Provided is a novel method of making 2-butyl-3-[[2?(1-trityl-1H-tetrazol-5-yl)biphen-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.Type: GrantFiled: February 5, 2004Date of Patent: May 2, 2006Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Ben-Zion Dolitzky, Julia Kaftanov, Boris Pertsikov, Igor Rukhman, Gennady Nisnevich
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Patent number: 7008959Abstract: The invention relates to a novel crystalline form of irbesartan to pharmaceutical compositions containing it, to processes for preparing it, and to a method for treating cardiovascular diseases utilizing it.Type: GrantFiled: September 9, 2004Date of Patent: March 7, 2006Assignee: Sanofi-AventisInventors: Bruno Franc, Christian Hoff, San Kiang, Mark D. Lindrud, Olivier Monnier, Chenkou Wei
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Patent number: 7005442Abstract: The present invention provides a compound represented by the general formula I; wherein A, Ar, X, Z, n, x, y, R and R3 are as defined in the specification.Type: GrantFiled: September 1, 2004Date of Patent: February 28, 2006Assignee: Allergan, Inc.Inventors: David W. Old, Thang D. Dinh, Robert M. Burk
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Patent number: 6949575Abstract: The present invention provides compounds of Formula (I) and a method of treating Alzheimer's disease using a compound of Formula (I), wherein: R1 and R2 include alkyl and phenylalkyl; R3 is hydrogen or alkyl; and R4 and R5 include alkyl, alkoxy, carboxyl, alkoxycarbonyl, and nitro. Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of Formula (I) and a method of imaging amyloid deposits using compounds of Formula (I).Type: GrantFiled: April 25, 2001Date of Patent: September 27, 2005Assignee: Pfizer Inc.Inventors: Nancy Sue Barta, Christopher Franklin Bigge
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Patent number: 6949570Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: May 7, 2002Date of Patent: September 27, 2005Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Susan Ashwell, Reinhardt Bernhard Baudy, Michael A. Pleiss, Dimitrios Sarantakis, Eugene D. Thorsett
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Patent number: 6949640Abstract: 2-Chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.Type: GrantFiled: February 16, 2001Date of Patent: September 27, 2005Assignee: Southern Research InstituteInventors: John A. Montgomery, Anita T. Fowler, John A. Secrist, III
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Patent number: 6939967Abstract: Process for production of non-proteinogenic L-amino acids by direct fermentation of a microorganism strain known per se having a deregulated cysteine metabolism in a manner known per se, which comprises adding, during the fermentation, a nucleophilic compound to the fermentation batch in a manner such that this leads to the production of non-proteinogenic L-amino acids by the microorganism strain.Type: GrantFiled: April 28, 2004Date of Patent: September 6, 2005Assignee: Consortium für elektrochemische Industrie GmbHInventor: Thomas Maier
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Patent number: 6916831Abstract: Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(?O)R6, —O(C?O)OR6; and —O(C?O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.Type: GrantFiled: February 24, 2003Date of Patent: July 12, 2005Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Kenneth F. Bastow, Sheng-Chu Kuo
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Patent number: 6911416Abstract: The present invention relates to new substituted N-benzoyl-N?-(tetrazolylphenyl)-ureas of the formula (I) in which R1, R2, R3, R4 and n are as stated in the description, to processes for their preparation, and to their use as pesticides.Type: GrantFiled: May 2, 2001Date of Patent: June 28, 2005Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Christoph Erdelen
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Patent number: 6900207Abstract: An N-containing five-membered ring compound of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation systems disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.Type: GrantFiled: January 25, 2001Date of Patent: May 31, 2005Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Patent number: 6881727Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.Type: GrantFiled: July 3, 2002Date of Patent: April 19, 2005Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Watanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
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Patent number: 6875776Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: October 24, 2002Date of Patent: April 5, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, Cheryl McArdle Clark, George V. DeLucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 6875787Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein the dashed line indicates the presence or absence of a bond, the hatched wedge indicates the ? (down) configuration, and the solid triangle indicates the ? (up) configuration; B is a single, double, or triple covalent bond; n is 0-6; X is CH2, S or O; Y is any pharmaceutically acceptable salt of CO2H, or CO2R, CONR2, NHCH2CH2OH, N(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, or R is H, C1-6 alkyl or C2-6 alkenyl; R2 and R3 are C1-6 linear alkyl which may be the same or different, and may be bonded to each other such that they form a ring incorporating the carbon to which they are commonly attached; R4 is hydrogen, R, C(?O)R, or any group that is easily removed under physiological conditions such that R4 is effectively hydrogen; R5 is hydrogenType: GrantFiled: February 11, 2003Date of Patent: April 5, 2005Assignee: Allergan, Inc.Inventor: Yariv Donde
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Patent number: 6875760Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.Type: GrantFiled: August 30, 2002Date of Patent: April 5, 2005Assignee: Novo Nordisk A/SInventors: Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Inge Thøger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thøgersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Anker Steen Jøgensen, Janos Tibor Kodra, Shenghua Shi
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Patent number: 6875884Abstract: Urea and thiourea derivatives inhibit cell function of the chemokine receptor CCR-3. These compounds offer an effective means for treating a range of diseases thought to be mediated by the CCR-3 receptor. A variety of useful urea and thiourea derivatives can be synthesized using liquid and solid phase synthesis protocols.Type: GrantFiled: July 28, 2000Date of Patent: April 5, 2005Assignee: Kirin Beer Kabushiki KaishaInventors: Janak Padia, Michael Hocker, Tsuyoshi Nishitoba, Hirohi Ohashi, Eiji Sawa
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Patent number: 6869970Abstract: The invention relates to new forms of salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt.Type: GrantFiled: January 29, 2003Date of Patent: March 22, 2005Assignee: Novartis AGInventor: Erwin Ernst Marti
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Patent number: 6858740Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives and a process for preparing them and their uses. The invention also concerns a process for preparing ?-ethyl-2-oxo-1-pyrrolidine acetamide derivatives from unsaturated 2-oxo-1-pyrrolidine derivatives. Particularly the invention concerns novel intermediates and their use in methods for the preparation of S-?-ethyl-2-oxo-1-pyrrolidine acetamide.Type: GrantFiled: July 1, 2003Date of Patent: February 22, 2005Assignee: UCB Farchim S.A.Inventors: John Surtees, Violeta Marmon, Edmond Differding, Vincent Zimmermann
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Patent number: 6849626Abstract: The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.Type: GrantFiled: August 21, 2001Date of Patent: February 1, 2005Assignee: Merck Patent GmbHInventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleiltz, Christopher Barnes
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Patent number: 6844443Abstract: A method for producing a compound represented by the formula: wherein the ring A is a benzene ring which may be substituted in addition to the R? group; R1 is hydrogen or an optionally substituted hydrocarbon residue; X is a direct bond or a spacer having an atomic length or two or less between the phenylene group and the phenyl group; Y is —O—, —S(O)m- or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; R? is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or a group convertible thereinto; n is an integer of 1 or 2; or a salt thereof, which comprises deprotecting a compound represented by the formula: wherein R is triphenylmethyl, 2-tetrahydropyranyl, methoxymethyl or ethoxy methyl, the other symbols as defined above; or a salt thereof.Type: GrantFiled: July 7, 2003Date of Patent: January 18, 2005Assignee: Takeda Pharmaceutical Company, Ltd.Inventors: Takehiko Naka, Kohei Nishikawa, Takeshi Kato
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Patent number: 6838565Abstract: Carboxylic acid amides of general formula having an antithrombotic activity and a factor Xa-inhibiting activity. Exemplary are: (a) N-[1-(3-amidino-phenyl)-2-(1H-tetrazol-5-yl)-ethyl]-4-(2,5-dihydro-pyrrol-1-yl-carbonyl)-3-methyl-benzamide, (b) N-[1-(3-amidino-phenyl)-2-(1H-tetrazol-5-yl)-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide, (c) N-[1-(5-amidino-2-hydroxy-phenyl)-2-phenyl-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide, and (d) N-[1-(5-amidino-2-hydroxy-phenyl)-2-(pyridin-3-yl)-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide.Type: GrantFiled: July 21, 2003Date of Patent: January 4, 2005Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Uwe Ries, Henning Priepke, Wolfgang Wienen, Herbert Nar, Sandra Handschuh
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Publication number: 20040259921Abstract: This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I, 1Type: ApplicationFiled: September 23, 2003Publication date: December 23, 2004Applicant: Pfizer IncInventors: Kimberly O. Cameron, Bruce A. Lefker
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Publication number: 20040254373Abstract: The invention provides compounds of Formula I: 1Type: ApplicationFiled: June 30, 2004Publication date: December 16, 2004Applicant: Pfizer IncInventors: David W. Piotrowski, Bruce N. Rogers, William W. McWhorter, Daniel Patrick Walker, Jeffrey W. Corbett, Vincent E. Groppi, Daniel G. Rudmann
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Publication number: 20040249150Abstract: The invention provides compounds of Formula I: 1Type: ApplicationFiled: June 29, 2004Publication date: December 9, 2004Applicant: Pfizer IncInventors: David W. Piotrowski, Bruce N. Rogers, William W. McWhorter, Daniel Patrick Walker, Jeffrey W. Corbett, Vincent E. Groppi, Daniel G. Rudmann
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Publication number: 20040242895Abstract: The invention relates to novel tetrazolinone derivatives of general formula (I) wherein R1 represents halogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylsulfonyl, C1-4 alkylsulfonyloxy, C2-5 alkoxycarbonyl, C2-6 alkoxyalkyl, C2-6 alkylthioalkyl, nitro or cyano, R2 represents a hydrogen atom, C1-6 alkyl, C3-6 cycloalkyl which may be optionally substituted with halogen or C1-3 alkyl, C1-4 haloalkyl, or phenyl which may be optionally substituted with halogen, C1-3 alkyl, C1-3 haloalkyl or nitro, m represents 0, 1 or 2, n represents 0 or 1, Q represents one of the groups which are mentioned in the description. The invention further relates to their use as herbicides and a process together with the intermediates for their preparation.Type: ApplicationFiled: June 21, 2004Publication date: December 2, 2004Inventors: Akihiko Yanagi, Shinichi Narabu, Toshio Goto, Seishi Ito, Chieko Ueno
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Patent number: 6821960Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.Type: GrantFiled: November 16, 2001Date of Patent: November 23, 2004Assignee: Noyo Nordisk Pharmaceuticals, Inc.Inventors: Anker Steen Jørgensen, Peter Madsen
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Patent number: 6812240Abstract: The present invention provides a compound represented by the general formula I; wherein A, Ar, X, Z, n, x, y, R and R3 are as defined in the specification.Type: GrantFiled: January 26, 2004Date of Patent: November 2, 2004Assignee: Allergan, Inc.Inventors: David W. Old, Thang D. Dinh, Robert M. Burk
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Patent number: 6812237Abstract: Compounds of the formula (I), wherein R1 is aryl or biaryl; R2 is aryl-lower alkyl, biaryl-lower alkyl, benzo-fused cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; Y is O, S, SO, SO2, CO or NR6; R3 is hydrogen or lower alkyl; or R2 and R3 combined are C2-C7-alkylene or C2-C7-alkylene interrupted by Y; R4 is hydrogen or lower alkyl; R5 is hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, biaryl-lower alkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C2-C7-alkyl in which C2-C7-alkyl is interrupted by Y; R6 is hydrogen, lower alkyl or aryl-lower alkyl; and pharmaceutically acceptable salts thereof, which are useful as cysteine cathepsin inhibitorsType: GrantFiled: November 7, 2002Date of Patent: November 2, 2004Assignee: Novartis AGInventors: Scott Douglas Cowen, Paul David Greenspan, Leslie Wighton McQuire, Ruben Alberto Tommasi, John Henry Van Duzer
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Publication number: 20040215023Abstract: A process for producing crystals of 2-ethoxy-1-[[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H-benzimdazole-7-carboxylic acid (compound (I)), characterized by dissolving or suspending the compound (I) or a salt thereof in a solvent comprising an aprotic polar solvent and crystallizing it. By the process, the contaminants which are contained in the compound (I) or its salt and are difficult to remove, such as tin compounds, analogues of the compound (I), and a residual organic solvent, can be easily removed. Crystals of the compound (I) can be efficiently and easily mass-produced in high yield on an industrial scale.Type: ApplicationFiled: February 2, 2004Publication date: October 28, 2004Inventors: Hideo Hashimoto, Hideaki Maruyama
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Patent number: 6809113Abstract: Compounds which are antagonists of MCP-1 function and are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection; pharmaceutical compositions comprising these compounds; and the use of these compounds and compositions in the prevention or treatment of such diseases.Type: GrantFiled: February 27, 2002Date of Patent: October 26, 2004Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
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Publication number: 20040209928Abstract: Compounds of formula (I) 1Type: ApplicationFiled: December 23, 2003Publication date: October 21, 2004Inventors: Ravi Kurukulasuriya, James T. Link, Jyoti R. Patel, Bryan K. Sorensen
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Patent number: 6806365Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: April 5, 2002Date of Patent: October 19, 2004Assignee: Hoffmann-La Rocher Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achytharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Publication number: 20040204406Abstract: The present invention is directed to a compound of formula I, 1Type: ApplicationFiled: December 23, 2003Publication date: October 14, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Marc Nazare, Volkmar Wehner, David W. Will, Hans Matter
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Patent number: 6800761Abstract: The invention relates to a novel crystalline form of irbesartan, to pharmaceutical compositions containing it, to processes for preparing it, and to a method for treating cardiovascular diseases utilizing it.Type: GrantFiled: March 12, 2001Date of Patent: October 5, 2004Assignee: Sanofi-SynthelaboInventors: Bruno Franc, Christian Hoff, San Kiang, Mark D. Lindrud, Olivier Monnier, Chenkou Wei
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Publication number: 20040192747Abstract: The present invention relates to new substituted N-benzoyl-N′-(tetrazolylphenyl)-ureas of the formula (I) 1Type: ApplicationFiled: April 14, 2004Publication date: September 30, 2004Inventors: Fritz Maurer, Christoph Erdelen
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Patent number: 6794404Abstract: A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (CType: GrantFiled: September 10, 2002Date of Patent: September 21, 2004Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
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Publication number: 20040181075Abstract: This invention is a novel methods of manufacturing chalcones that includes reacting a carbon-linked heteroaryl or heterocyclic substituted benzaldehyde with an acetophenone in a solvent or mixture of solvents in the presence of LiOMe. Also provided are new chalcones for the treatment of medical conditions.Type: ApplicationFiled: December 19, 2003Publication date: September 16, 2004Inventors: M. David Weingarten, Liming Ni, Charles Q. Meng, Kimberly J. Worsencroft, James A. Sikorski
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Patent number: 6790978Abstract: Compounds of the present invention of the formula are thyromimetic agents which can be used to prevent and/or treat diseases associated with an imbalance of thyroid hormones, such as hypo- and hyper-thyroidism, obesity, osteoporosis and depression. The compounds of the invention are, in particular, hypolipedemic agents which enhance the clearance of cholesterol from circulation, particularly the clearance of cholesterol in the form of low density lipoproteins (LDL). The compounds are useful for reducing total cholesterol plasma levels in mammals, in particular for reducing levels of LDL-cholesterol. Furthermore, such compounds also lower elevated lipoprotein (a) [Lp(a)] levels, an independent cardiovascular risk factor, in mammals.Type: GrantFiled: September 28, 2001Date of Patent: September 14, 2004Assignee: Novartis AGInventor: Paivi Jaana Kukkola
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Patent number: 6784195Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1, R2, T and Ht are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: October 5, 2001Date of Patent: August 31, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Hale, James Janetka, Francois Maltais, Jingrong Cao