The Additional Hetero Ring Is Six-membered And Contains Nitrogen Patents (Class 514/217.04)
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Patent number: 7202237Abstract: The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions, disorders, or diseases involving the cholinergic system of the central nervous system, pain, inflammatory diseases, diseases caused by smooth muscle contractions and as assistance in the cessation of chemical substance abuse.Type: GrantFiled: May 19, 2004Date of Patent: April 10, 2007Assignee: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet Østergaard Nielsen
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Patent number: 7115596Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or the ?v?5 integrin without significantly inhibiting the ?v?6 integrin.Type: GrantFiled: December 19, 2003Date of Patent: October 3, 2006Assignee: Pharmacia CorporationInventors: John A. Wendt, Heather Stenmark, Hongwei Wu, Yaping Wang, Barbara B. Chen, Thomas D. Penning, Victoria L. Downs, Mark L. Boys, Mark Russell, Dale P. Spangler
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Patent number: 7115635Abstract: The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.Type: GrantFiled: April 26, 2002Date of Patent: October 3, 2006Assignee: Mitsubishi Pharma CorporationInventors: Masatoshi Kiuchi, Takanobu Kuroita, Hideo Tomozane, Shuuzou Takeda, Yoshihito Tanaka, Hidemitsu Higashi, Shigeki Kuwahara
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7071184Abstract: The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.Type: GrantFiled: March 7, 2001Date of Patent: July 4, 2006Assignee: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Jr., Daniel F. Veber, Dennis S. Yamashita
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Patent number: 7041675Abstract: The invention relates to compounds of the formula I and the tautomeric forms, possible enantiomeric and diasteromeric forms thereof, and prodrugs thereof, and use thereof as PARP inhibitors.Type: GrantFiled: January 25, 2001Date of Patent: May 9, 2006Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Michael Kock, Thomas Hoeger, Roland Grandel, Reinhold Mueller, Sabine Schult
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Patent number: 7026310Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: April 14, 2005Date of Patent: April 11, 2006Assignee: Zentaris GmbHInventors: Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
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Patent number: 7022695Abstract: Thioether-substituted benzamide compounds having the formula: are provided that exhibit exceptionally strong inhibition of Factor Xa in combination with weak hERG binding.Type: GrantFiled: October 5, 2004Date of Patent: April 4, 2006Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Erick A. Goldman, Wenrong Huang, Penglie Zhang
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Patent number: 6992092Abstract: The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1, R2, Ra, Rb, X, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.Type: GrantFiled: April 15, 2004Date of Patent: January 31, 2006Assignee: Pfizer Inc.Inventors: Donald L. Bussolotti, Ronald B. Gammill
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Patent number: 6984637Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 21, 2003Date of Patent: January 10, 2006Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Patent number: 6974870Abstract: Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the I?B kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.Type: GrantFiled: December 6, 2003Date of Patent: December 13, 2005Assignee: Boehringer Ingelheim Phamaceuticals, Inc.Inventors: Charles L. Cywin, Can Mao, Jonathan Emeigh, Roman Wolfgang Fleck, Ming-Hong Hao, Eugene Hickey, Weimin Liu, Daniel Richard Marshall, Tina Morwick, Peter Nemoto, Ronald John Sorcek, Sanxing Sun, Jiang-Ping Wu, Erick Young, Darren DiSalvo, John Ginn, Pier Cirillo
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Patent number: 6964956Abstract: Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the I?B kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.Type: GrantFiled: June 3, 2003Date of Patent: November 15, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles L. Cywin, Zhidong Chen, Roman Wolfgang Fleck, Ming-Hong Hao, Eugene Hickey, Weimin Liu, Daniel Richard Marshall, Peter Nemoto, Ronald John Sorcek, Sanxing Sun, Jiang-Ping Wu, Tina Morwick, Jonathan Emeigh
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Patent number: 6939867Abstract: Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with ?-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and cardiovascular diseasesType: GrantFiled: February 28, 2002Date of Patent: September 6, 2005Assignee: Pfizer Inc.Inventors: Robert L. Dow, Ernest S. Paight
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Patent number: 6887864Abstract: This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.Type: GrantFiled: March 6, 2003Date of Patent: May 3, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Walter-Gunar Friebe, Birgit Masjost, Ralf Schumacher
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Patent number: 6849621Abstract: Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such as, for example, allergy, allergy-induced airway responses, and congestion (e.g., nasal congestion) using the compounds of Formula I in combination with a H. receptor antagonist.Type: GrantFiled: March 11, 2002Date of Patent: February 1, 2005Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Stuart B. Rosenblum, Qingbei Zeng, Mwangi Wa Mutahi, Robert G. Aslanian, Pauline C. Ting, Neng-Yang Shih, Daniel M. Solomon, Jianhua Cao, Henry A. Vaccaro, Kevin D. McCormick, John J. Baldwin, Ge Li
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Publication number: 20040229863Abstract: The present invention provides methods which use 4-amino-azepan-3-one protease inhibitors of cathepsin S in the treatment of diseases in which cathepsin S is implicated, especially treatment or prevention of autoimmune disease; treatment or prevention of a disease state caused by the formation of atherosclerotic lesions and complications arising therefrom; and diseases requiring inhibition, for therapy, of a class II MHC-restricted immune response, inhibition of an asthmatic response, inhibition of an allergic response, inhibition of immune response against a transplanted organ or tissue, or inhibition of elastase activity in atheroma, and novel compounds for use therewith.Type: ApplicationFiled: March 10, 2004Publication date: November 18, 2004Applicant: SmithKline Beecham CorporationInventors: Maxwell D. Cummings, Robert W. Marquis, Yu Ru, Scott K. Thompson, Daniel F. Veber, Dennis S. Yamashita
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Publication number: 20040224941Abstract: Compounds represented by formula (I), prodrugs thereof and salts thereof, and pharmaceutical compositions comprising the same as an active ingredient (wherein each symbol has the meaning as defined in the specification.).Type: ApplicationFiled: November 10, 2003Publication date: November 11, 2004Inventors: Takuya Seko, Masahiko Terakado, Hiroshi Kohno, Shinya Takahashi
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Patent number: 6815451Abstract: The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists especially urotensin II antagonists.Type: GrantFiled: September 15, 2003Date of Patent: November 9, 2004Assignee: Actelion Pharmaceuticals Ltd.Inventors: Jörg Velker, Hamed Aissaoui, Christoph Binkert, Martine Clozel, Boris Mathys, Claus Mueller, Oliver Nayler, Michael Scherz, Thomas Weller
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Patent number: 6809093Abstract: Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds.Type: GrantFiled: December 19, 2000Date of Patent: October 26, 2004Assignee: H. Lee Moffitt Cancer & Research Institute, Inc.Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
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Publication number: 20040192674Abstract: The present invention provides methods which uses certain 4-amino-azepan-3-ones to inhibit cathepsin L. Consequently they are useful for preventing or treating diseases in which cathepsin L is implicated, such as rheumatoid arthritis or inhibition of positive selection of CD4+T-cells by cortical thymic epithelial cells.Type: ApplicationFiled: February 5, 2004Publication date: September 30, 2004Inventor: Robert W. Marquis
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Publication number: 20040192680Abstract: Compounds of formula (I) 1Type: ApplicationFiled: December 18, 2003Publication date: September 30, 2004Inventors: Steven N. Anderson, Pramila A. Bhatia, Teodozyj Kolasa, Masaki Nakane, Meena V. Patel, Jeffrey J. Rohde, Xia Zhiren, Henry Qing-Wei Zhang
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Publication number: 20040192673Abstract: This invention relates to N-aroyl cyclic amine derivatives of formula (I): wherein: Y represents a bond, oxygen, or a group (CH2)n, wherein n represents 1, 2 or 3 m represents 1, 2 or 3; p represents 0 or 1; X is O,SC═O, SO2, or —CH═CH; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar2 represents phenyl or a 5- or 5-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R1 represents hydrogen, optionally substituted (C1-4)alkoxy, halo, cyano, optionally substituted (C1-16)alkyl, optionally substituted 5- or 6-membered heterocyclic ring containing up to 4 heteroatoms selected from N, O and S; or a pharmaceutical accType: ApplicationFiled: April 15, 2004Publication date: September 30, 2004Inventors: Pascale Gaillard, Christopher Norbert Johnson, Riccardo Novelli, Roderick Alan Porter, Geoffrey Stemp, Kevin Michael Thewlis
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Publication number: 20040167119Abstract: A chemical genus of 2-(aminomethyl)arylamides, which are useful as analgesics, is disclosed.Type: ApplicationFiled: February 11, 2003Publication date: August 26, 2004Applicant: PHARMACOPEIA, INCInventors: Koc-Kan Ho, John J. Baldwin, Adolph C. Bohnstedt, Steven G. Kultgen, Edward McDonald, Tao Guo, John Richard Morphy, Zoran Rankovic, Robert Horlick, Kenneth C. Appell
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Publication number: 20040157828Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: ApplicationFiled: November 17, 2003Publication date: August 12, 2004Inventors: Ren Xie, Dennis S Yamashita
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Publication number: 20040157829Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.Type: ApplicationFiled: February 2, 2004Publication date: August 12, 2004Applicant: ICAgen, Inc.Inventors: Grant A. McNaughton-Smith, Michael F. Gross, Alan D. Wickenden
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Publication number: 20040152688Abstract: Aminopyridine derivatives of the following formula I which exhibit pharmacological activity at estrogen receptors alpha (ER&agr;) and beta (ER&bgr;) are described herein. The described invention also includes compositions and medicaments containing the aminopyridine derivatives as well as processes for the preparation and use of such compounds, compositions and medicaments.Type: ApplicationFiled: March 23, 2004Publication date: August 5, 2004Inventors: David Harold Drewry, Brad Richard Henke
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Publication number: 20040152692Abstract: The present invention relates to pyrrolidine sulfonamides, pharmaceutical compositions containing them and their use as urotensin II antagonists.Type: ApplicationFiled: September 26, 2003Publication date: August 5, 2004Inventors: Dashyant Dhanak, Steven D Knight, Jian Jin, Ralph A Rivero
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Publication number: 20040147507Abstract: The present invention provides a compound of formula I: 1Type: ApplicationFiled: November 3, 2003Publication date: July 29, 2004Inventors: Mark Ledeboer, Brian Ledford
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Publication number: 20040147506Abstract: This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I] 1Type: ApplicationFiled: October 20, 2003Publication date: July 29, 2004Inventors: Takeru Yamakawa, Yoshio Ogino, Yufu Sagara, Kenji Matsuda, Akira Naya, Toshifumi Kimura, Norikazu Otake
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Publication number: 20040142924Abstract: The present invention relates to 6-phenyl-pyridin-2-ylamine derivatives of the formula 1Type: ApplicationFiled: October 3, 2003Publication date: July 22, 2004Applicant: Pfizer IncInventor: Jon A. Low
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Publication number: 20040142923Abstract: The present invention relates to pyrrolidine sulfonamides, pharmaceutical compositions containing them and their use as urotensin II antagonists.Type: ApplicationFiled: September 26, 2003Publication date: July 22, 2004Inventors: Dashyant Dhanak, Steven D. Knight, Jian Jin, Ralph A. Rivero
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Publication number: 20040138205Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I 1Type: ApplicationFiled: November 18, 2003Publication date: July 15, 2004Inventors: Dawei Chen, Milind Deshpande, Andrew Thurkauf, Avinash Phadke, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Publication number: 20040132694Abstract: This invention relates to the novel use of amide squaramides in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: July 16, 2003Publication date: July 8, 2004Inventors: Michael R. Palovich, Katherine L. Widdowson
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Publication number: 20040132718Abstract: The present application describes monocyclic or bicyclic carbocycles and heterocycles and derivatives thereof of Formula I: 1Type: ApplicationFiled: December 8, 2003Publication date: July 8, 2004Inventors: Irina C. Jacobson, Ruth R. Wexler, Suanne Nakajima, Mimi L. Quan, Shuaige Wang, Joanne M. Smallheer, Jennifer X. Qiao
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Publication number: 20040121997Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 24, 2003Publication date: June 24, 2004Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
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Publication number: 20040121994Abstract: Compounds of formula (I) 1Type: ApplicationFiled: December 20, 2002Publication date: June 24, 2004Inventors: Steven N. Anderson, Pramila Bhatia, Teodozyj Kolasa, Masaki Nakane, Meena V. Patel, Jeffrey J. Rohde, Zhiren Xia, Henry Q. Zhang
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Patent number: 6743808Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7-membered ring; R8 is hydrogen or alkyl; hType: GrantFiled: April 14, 2000Date of Patent: June 1, 2004Assignee: H. Lundbeck A/SInventors: Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
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Publication number: 20040067928Abstract: Substituted propane-1,3-diamine derivatives, methods for producing such derivatives, and medicaments and pharmaceutical compositions containing such derivatives useful for the treatment or prophylaxis of pain, urinary incontinence, itching, tinitus aurium, or diarrhea are provided.Type: ApplicationFiled: August 21, 2003Publication date: April 8, 2004Applicant: Gruenenthal GmbHInventors: Bernd Sundermann, Helmut Buschmann, Babette-Yvonne Koegel, Beatrix Merla, Nikolaus Risch
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Publication number: 20040063679Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.Type: ApplicationFiled: September 27, 2002Publication date: April 1, 2004Applicant: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey D. Ward, Erick R.R. Young, Eugene R. Hickey, Weimin Liu, Usha R. Patel
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Publication number: 20040058903Abstract: The present invention relates to compounds of the formula (I) wherein R1 and R2 are each independently lower alkyl lower alkenyl, acyl, amino, lower alkoxy, lower cycloalkyloxy, aryl, aryloxy, sulfooxy, mercapto, sulfo, hydrogen, halogen, nitro, cyano or hydroxy, or may form a ring structure; Q1 is N or CH; L is optionally substituted unsaturated 3 to 10-membered heterocyclic group; X is optionally substituted monocyclic arylene or monocyclic heteroarylene; Y is -(A1)m-(A2)n-(A4)k-; Z is directbond, —CH2-, —NH— or —O—; and R is hydrogen or lower alkyl, or a salt thereof The compounds of the present invention inhibit apolipoprotein B (Apo B) secretion and are useful as a medicament for prophylactic and treatment of diseases or conditions resulting from elevated circulating levels of Apo B.Type: ApplicationFiled: September 3, 2003Publication date: March 25, 2004Inventors: Hisashi Takasugi, Takeshi Terasawa, Yoshikazu Inoue, Hideko Nakamura, Akira Nagayoshi, Hiroaki Ohtake, Yoshiro Furukawa, Masafumi Mikami, Kazumasa Hinoue, Makoto Ohtsubo
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Publication number: 20040048848Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 1Type: ApplicationFiled: February 5, 2003Publication date: March 11, 2004Applicant: Schering-Plough Corporation and Pharmacopeia, Inc.Inventors: Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
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Publication number: 20040043988Abstract: The present invention relates to a class of compounds represented by the Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula (I), and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 and/or &agr;v &bgr;5 integrin.Type: ApplicationFiled: August 21, 2003Publication date: March 4, 2004Inventors: Ish Kurmar Khanna, Michael Clare, Alan Gasiecki, Thomas Rogers, Barbara B. Chen, Mark Russell, Hwang-Fun Lu
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Publication number: 20040038965Abstract: The present invention provides C3-C6 1-amino-1-acyl cycloalkane-substituted 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: ApplicationFiled: May 22, 2003Publication date: February 26, 2004Inventors: Robert W. Marquis, Jr., Daniel F. Veber, Dennis S. Yamashita
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Publication number: 20040034013Abstract: The present invention provides methods which use 4-amino-azepan-3-one protease inhibitors of cathepsin L in the treatment of diseases in which cathepsin L is implicated, especially treatment or prevention of rheumatoid arthritis; treatment or prevention of cancer metastasis; treatment or prevention of diseases requiring inhibition of tissue destruction by macrophage, particularly lung macrophage, such as asthma, chronic obstructive pulmonary disease (COPD), and emphysema; treatment or prevention of diseases requiring, for therapy, inhibition of positive selection of CD4+ T-cells by cortical thymic epithelial cells.Type: ApplicationFiled: October 17, 2002Publication date: February 19, 2004Inventors: Maxwell D Cummings, Robert W Marquis, Yu Ru, Scott K Thompson, Daniel F Veber, Dennis S Yamashita
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Publication number: 20040029863Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: June 23, 2003Publication date: February 12, 2004Applicant: Amgen Inc.Inventors: Kevin Koch, Andreas Termin, John A. Josey
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Patent number: 6686351Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: February 27, 2002Date of Patent: February 3, 2004Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Qi Chao
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Patent number: 6683074Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: September 26, 2001Date of Patent: January 27, 2004Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Publication number: 20040014783Abstract: The present invention provides a compound of a formula (I): 1Type: ApplicationFiled: May 13, 2003Publication date: January 22, 2004Applicant: AstraZeneca AB, a Sweden corporationInventors: Aaron Rigby, Hitesh Sanganee, Brian Springthorpe, Louise Lawrence
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Patent number: 6680314Abstract: Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is aryl optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteroaryl group, or R is a monocyclic 5 to 6-membered heteroaryl group optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteraryl group, or R is a bicyclic heteroaryl group composed of a monocyclic 5 to 6-membered heteroaryl group fused to a benzene ring, optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cyType: GrantFiled: April 30, 2002Date of Patent: January 20, 2004Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
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Publication number: 20040009967Abstract: The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.Type: ApplicationFiled: July 30, 2002Publication date: January 15, 2004Applicant: Klinge Pharma GmbHInventors: Elfi Biedermann, Max Hasmann, Roland Loser, Benno Rattel, Friedemann Reiter, Barbara Schein, Klaus Seibel, Klaus Vogt