Nitrogen Or C(=x), Wherein X Is Chalcogen, Attached Indirectly To The Seven-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 514/217.12)
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Patent number: 7141560Abstract: The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.Type: GrantFiled: January 17, 2002Date of Patent: November 28, 2006Assignee: Akzo Nobel N.V.Inventors: Niall Morton Hamilton, David Jonathan Bennett
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Patent number: 6992081Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: September 21, 2001Date of Patent: January 31, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Fang
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Patent number: 6967196Abstract: In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the sulfur atom and nitrogen atom of the sulfonamide group include substituted or unsubstituted hydrocarbyl moieties, substituted or unsubstituted heterocycle moieties, polycyclic moieties, halogen, alkoxy, ether, ester, amide, sulfonyl, sulfonamidyl, sulfide, carbamate, and the like. Invention compounds are capable of a wide variety of uses. For example sulfonamide compounds can act to modulate production of amyloid ? protein and are useful in the prevention or treatment of a variety of diseases. Pharmaceutical compositions containing invention compounds are also provided. Such compositions have wide utility for the prevention or treatment of a variety of diseases.Type: GrantFiled: February 22, 2000Date of Patent: November 22, 2005Assignees: Bristol-Myers Squibb Company, Merck & Co. Inc.Inventors: David W. Smith, Benito Munoz, Kumar Srinivasan, Carl P. Bergstrom, Prasad V. Chaturvedula, Milind S. Deshpande, Daniel J. Keavy, Wai Yu Lau, Michael F. Parker, Charles P. Sloan, Owen B. Wallace, Henry Hui Wang
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Patent number: 6953789Abstract: The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1 may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2, etc., X1 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group or —NR3—, etc, X2 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group, —NR4—, —O— or —S(O)p— (wherein p is 0, 1 or 2), each Y may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, a halogen atom, a carboxyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR5, an oxo group, a thioxo group, an optionally substituted imino group, a nitro group, a cyano group, etc.Type: GrantFiled: January 13, 2004Date of Patent: October 11, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Toshiro Yamashita, Hiroshi Nara, Masayuki Takizawa, Koji Yoshimura
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Patent number: 6906059Abstract: The use of benzazepin-N-acetic acid derivatives which contain an oxo group in the a position to the nitrogen atom and are substituted in the 3 position by a 1-(carboxyalkyl)-cyclopentyl-carbonyl-amino radical, and of their salts and biolabile esters, for the prophylaxis and/or treatment of heart damage caused by cardiotoxic doses of medicaments or chemicals, in larger mammals and in particular humans. The invention is particularly applicable to the prophylaxis and/or treatment of heart damage, in particular to the myocardium, which may occur during cytostatic chemotherapy. The invention also includes the use of the afore-mentioned benzazepin-N-acetic acid derivatives for adjuvant treatment in therapies in which medicaments having oxidative-toxic side-effects are used, and the preparation of medicaments suitable for this prophylaxis and/or treatment or adjuvant treatment.Type: GrantFiled: January 14, 2002Date of Patent: June 14, 2005Assignee: Solvay PharmaceuticalsInventors: Zsuzsanna Lonovics, Julius Gy. Papp, Dirk Thormaehlen, Harald Waldeck, Zsuzsanna Rozsa
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Publication number: 20040266731Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.Type: ApplicationFiled: June 27, 2003Publication date: December 30, 2004Inventors: Roger D. Tung, Scott L. Harbeson, David D. Deininger, Mark A. Murcko, Govinda R. Bhisetti, Luc J. Farmer
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Publication number: 20040254166Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1Type: ApplicationFiled: April 1, 2004Publication date: December 16, 2004Inventors: Kevin D. Kreutter, Lily Lee, Tianbao Lu, Venkatraman Mohan, Sharmila Patel, Hui Huang, Guozhang Xu, Mark Fitzgerald
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Publication number: 20040248876Abstract: Methods and compositions which are useful in the treatment of amyloidosis. In particular, methods and compositions are provided for inhibiting, preventing and treating amyloid deposition, e.g., in pancreatic islets, wherein the amyloidotic deposits are islet amyloid polypeptide (IAPP)-associated amyloid deposition or deposits. The methods of the invention involve administering to a subject a therapeutic compound which inhibits IAPP-associated amyloid deposits. Accordingly, the compositions and methods of the invention are useful for inhibiting IAPP-associated amyloidosis in disorders in which such amyloid deposition occurs, such as diabetes.Type: ApplicationFiled: May 2, 2003Publication date: December 9, 2004Applicant: Queen's University at Kingston and Neurochem, Inc.Inventors: Walter A. Szarek, Donald F. Weaver, Xianqi Kong, Ajay Gupta, David Migneault
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Publication number: 20040235896Abstract: Compounds of the formula (I) wherein R represents OH or NHOH; R1 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl, or acyl derived from a carboxylic acid, from a carbonic acid, from a carbamic acid of from a sulfonic acid; R2 represents biarylsulfonyl or aryloxyarylsufonyl; R3 represents hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, cycloalkyl-lower alkyl or acyl derived from a carboxylic acid, from a carbonic acid or form a carbamic acid; R4 and R5 represent independently hydrogen, lower alkyl, lower alkoxycarbonyl, aryl-lower alkyl or cycloalkyl-lower alkyl; m is zero, 1, 2 or 3; pharmaceutically acceptable prodrug derivatives thereof; pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; and their use for inhibiting matrix degrading metalloproteinases and preventing or treating matrix metalloproteinase dependent conditions in mammals.Type: ApplicationFiled: May 13, 2004Publication date: November 25, 2004Inventors: Roger Aki Fujimoto, Leslie Wighton McQuire, Lauren G. Monovich, Philippe Nantermet, David Thomas Parker, Leslie Ann Robinson, Jerry W. Skiles, Ruben alberto Tommasi
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Patent number: 6821965Abstract: The invention concerns amide derivatives of the Formula (I) wherein R3 is (1-6C)alkyl or halogeno; Q is aryl or heteroaryl which optionally bears 1, 2, 3 or 4 substituents such as hydroxy, halogeno, trifluoromethyl, cyano, (1-6C)alkyl, (1-6C)alkoxy, halogeno(1-6C)alkyl, hydroxy-(1-6C)alkyl, di-[(1-6C)alklyl]amino-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, (1-6)alkoxy-(2-6C)alkoxy, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, amino-2(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, aryl-(1-6C)alkoxy, heteroaryl, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyl-(1-6C)alkyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; p is 0-2 and R2 is a substituent such as hydroxy and halogeno; q is 0-4; and R4 includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseaseType: GrantFiled: February 2, 2001Date of Patent: November 23, 2004Assignee: AsterZeneca ABInventors: Dearg S Brown, George R Brown
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Patent number: 6821963Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.Type: GrantFiled: June 4, 2002Date of Patent: November 23, 2004Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
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Publication number: 20040229858Abstract: Compounds that selectively inhibit the binding of ligands to &agr;4&bgr;1 integrin (VLA-4) and methods for their preparation are disclosed.Type: ApplicationFiled: February 26, 2004Publication date: November 18, 2004Applicants: Daiichi Pharmaceutical Co., LTD., Pharmacopeia Drug Discovery, Inc.Inventors: John J. Baldwin, Edward McDonald, Kevin Joseph Moriarty, Christopher Ronald Sarko, Nobuo Machinaga, Atsushi Nakayama, Jun Chiba, Shin Iimura, Yoshiyuki Yoneda
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Publication number: 20040229864Abstract: The present invention relates to sulfone derivatives of formula (I):Type: ApplicationFiled: May 14, 2004Publication date: November 18, 2004Inventors: Sylvie Bourrain, Peter Alan Hunt, Ian Thomas Huscroft, Janusz Jozef Kulagowski, Clare London, Elizabeth Mary Naylor, Piotr Antoni Raubo, Eileen Mary Seward
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Patent number: 6818765Abstract: Benzene-sulphonamide derivatives complying with the general formula (I): in which the different symbols have different meanings, their optical isomers and the salts pharmacologically acceptable of these derivatives, as well as their uses for drug manufacture and as radiolabelled pharmacological tools of the thromboxan A2 receptors.Type: GrantFiled: October 16, 2001Date of Patent: November 16, 2004Assignee: Universite de LiegeInventors: Jacques Delarge, Jean-Michel Dogne, Bernard Masereel
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Publication number: 20040224907Abstract: The present invention relates to sigma-1 receptor ligands, to uses of sigma-1 receptor ligands in treating drug resistance, methods of using sigma-1 receptor ligands in regulating P-glycoprotein expression, methods of screening for compositions (e.g., agonists) that activate the sigma-1 receptor, regulate P-glycoprotein expression and/or have tolerance reducing activity.Type: ApplicationFiled: April 19, 2004Publication date: November 11, 2004Inventors: Gavril W. Pasternak, Claire Neilan
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Publication number: 20040220224Abstract: The invention features a method of treating irritable bowel syndrome (IBS) by administering quarternary ammonium compounds of formulae I-V, described herein.Type: ApplicationFiled: April 13, 2004Publication date: November 4, 2004Applicant: Pfizer IncInventors: Ivan Michael Richards, Karen Patrice Kolbasa
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Publication number: 20040220169Abstract: The present invention relates to new substituted carboxylic acid amides of general formula 1Type: ApplicationFiled: December 19, 2003Publication date: November 4, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: James Gillard, Sandra Ruth Handschuh, Herbert Nar, Roland Pfau, Henning Priepke, Wolfgang Wienen, Annette Mario Schuler-Metz, Eckhart Bauer, Georg Dahmann, Kai Gerlach
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Publication number: 20040186088Abstract: The present invention relates to compounds that inhibit TACE, compositions thereof, and methods of using those compounds and compositions for treating diseases.Type: ApplicationFiled: December 19, 2003Publication date: September 23, 2004Inventors: Upul Bandarage, Jon H. Come, Emanuele Perola, Govinda Rao Bhisetti, Jeffrey O. Saundres
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Publication number: 20040186097Abstract: The present application describes modulators of CCR3 of formula (I): 1Type: ApplicationFiled: March 25, 2004Publication date: September 23, 2004Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, Dean A. Wacker
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Publication number: 20040186098Abstract: The present invention relates generally to methods for preventing and/or treating injury or degeneration of cochlear hair cells and spiral ganglion neurons by administering sensorineurotrophic compounds described below. The invention relates more specifically to methods for treating sensorineural hearing loss as well as vestibular disorders and tinnitus.Type: ApplicationFiled: March 29, 2004Publication date: September 23, 2004Applicant: Amgen Inc.Inventor: Ella Magal
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Publication number: 20040180876Abstract: The present invention relates to novel compounds of Formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.Type: ApplicationFiled: February 9, 2004Publication date: September 16, 2004Inventors: Keith Biggadike, Diane Mary Coe, Dean David Edney, Stephen Barry Guntrip, Abigail Halton, Brian Edgar Looker, Michael John Monteith, Rajnikant Patel, Panayiotis Alexandrou Procopiou
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Publication number: 20040180871Abstract: The present invention provides compositions and their use in the treatment of inflammatory diseases caused by T-cell proliferation such as sepsis, inflammatory bowel diseases, autoimmune encephalomyelitis, or lupus.Type: ApplicationFiled: December 23, 2003Publication date: September 16, 2004Applicant: Genzyme CorporationInventors: Mark M. Staveski, Robert J. Miller, Sharon R. Nahill
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Publication number: 20040176347Abstract: A pharmaceutical composition for the treatment and/or prevention of cerebral ischemic diseases, which comprises two components, i.e.Type: ApplicationFiled: January 14, 2004Publication date: September 9, 2004Inventors: Kaneyoshi Honjo, Narito Tateishi, Nobuo Katsube
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Publication number: 20040142980Abstract: The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseases.Type: ApplicationFiled: June 30, 2003Publication date: July 22, 2004Inventors: Barry Craig Finzel, Hua Gao, Meredith L. Greene, Rebecca J. Gross, Richard Allen Nugent, Jeffrey A. Pfefferkorn
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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: 20040127488Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: July 2, 2003Publication date: July 1, 2004Applicant: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald George Sherrill, Andrew Spaltenstein, Eric Steven Furfine, Francois Maltais, Clarence Webster Andrews, John Franklin Miller, Vicente Samano
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Publication number: 20040122000Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: October 21, 2003Publication date: June 24, 2004Applicant: Vertex Pharmaceuticals Incorporated.Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
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Publication number: 20040110736Abstract: The present application describes modulators of MCP-1 of formula (I): 1Type: ApplicationFiled: November 12, 2003Publication date: June 10, 2004Inventor: Robert Cherney
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Publication number: 20040102437Abstract: Compounds having an Rho kinase inhibitory activity. These compounds include the compound of general formula (I): Het-X-Z, pharmaceutically acceptable salts thereof and solvates of the same, wherein Het represents a monocyclic or dicyclic heterocycle group containing at least one nitrogen atom (for example, pyridyl, phthalimido); X represents (i) an —NH—C(═O)—NH-Q1- group, (ii) an —NH—C(═O)-Q2- group, etc. (wherein Q1 and Q2 represent each a bond, alkylene or alkenylene); and Z represents hydrogen, halogeno, a monocyclic, dicyclic ortricyclic carbon cycle or heterocycle, etc. (for example, optionally substituted phenyl).Type: ApplicationFiled: May 19, 2003Publication date: May 27, 2004Inventors: Atsuya Takami, Hiroshi Iijima, Masayuki Iwakubo, Yuji Okada
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Publication number: 20040092497Abstract: The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the &agr;&ngr;&bgr;3 and/or the &agr;&ngr;&bgr;5 integrin without significantly antagonizing the IIb/IIIa integrin.Type: ApplicationFiled: September 5, 2003Publication date: May 13, 2004Inventors: Srinivasan Raj Nagarajan, Ish Kumar Khanna, Michael B. Tollefson, Scott B, Mohler, Barbara B. Chen, Mark Russell, Balekudru Devadas, Thomas D. Penning, Lori A. Schretzman, Dale P. Spangler, Mark L. Boys, Nizal S. Chandrakumar, Hwang-Fun Lu
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Publication number: 20040087573Abstract: Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: ApplicationFiled: October 23, 2003Publication date: May 6, 2004Inventors: Richard L. Apodaca, Curt A. Dvorak, Chandravadan R. Shah, Wei Xiao
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Publication number: 20040082569Abstract: An amide of the formula I 1Type: ApplicationFiled: October 20, 2003Publication date: April 29, 2004Applicant: Abbott GmbH & Co., KGInventors: Wilfried Lubisch, Achim Moller, Hans-Jorg Treiber, Monika Knopp
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Publication number: 20040072821Abstract: The present invention relates N-substituted glycine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: October 2, 2003Publication date: April 15, 2004Inventors: David Lauffer, Brian Ledford, Michael Mullican
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Publication number: 20040067927Abstract: The invention relates to novel compounds which are substituted alkyldiamino derivatives of formula (I). The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of formula (I) and especially their use as inhibitors of the plasmodium falciparum protease plasmepsin II or related aspartic proteases.Type: ApplicationFiled: November 7, 2003Publication date: April 8, 2004Inventors: Christoph Boss, Walter Fischli, Solange Meyer, Sylvia Richard-Bildstein, Thomas Weller
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Publication number: 20040067935Abstract: The present application describes modulators of chemokine receptors of formula (I): 1Type: ApplicationFiled: September 25, 2003Publication date: April 8, 2004Inventor: Douglas G. Batt
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Publication number: 20040063680Abstract: The present invention provides a method of treating stroke in a patient comprising administering to said patient an effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 5, 2003Publication date: April 1, 2004Inventors: James Allen Clemens, David Lodge
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Publication number: 20040063649Abstract: The invention is directed to a method of treating cancer or a bacterial or protozoal infection in a mammalian subject in need of such treatment. The method comprises the adjunctive administration of pharmaceutically effective amounts of a macrolide antibiotic and a Substance P antagonist. The invention also encompasses a method of preventing or treating emesis associated with macrolide antibiotic administration. The invention further encompasses novel compositions comprising a macrolide antibiotic and a Substance P antagonist.Type: ApplicationFiled: September 18, 2003Publication date: April 1, 2004Applicant: Pfizer IncInventors: Dennis M. Godek, Richard Todd Darrington, Elizabeth Fraering Illyes
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Publication number: 20040053908Abstract: Compounds represented by the following general formula: 1Type: ApplicationFiled: April 18, 2003Publication date: March 18, 2004Inventors: Yasuhiro Funahashi, Akihiko Tsuruoka, Masayuki Matsukura, Toru Haneda, Yoshio Fukuda, Junichi Kamata, Keiko Takahashi, Tomohiro Matsushima, Kazuki Miyazaki, Ken-ichi Nomoto, Tatsuo Watanabe, Hiroshi Obaishi, Atsumi Yamaguchi, Sachi Suzuki, Katsuji Nakamura, Fusayo Mimura, Yuji Yamamoto, Junji Matsui, Kenji Matsui, Takako Yoshiba, Yasuyuki Suzuki, Itaru Arimoto
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Publication number: 20040048852Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical.Type: ApplicationFiled: January 7, 2003Publication date: March 11, 2004Inventors: Thomas E. Barta, Daniel P. Becker, Terri L. Boehm, Gary A. DeCrezcenzo, John N. Freskos, Daniel P. Getman, Joseph J. McDonald, Clara I. Villamil, Louis John Bedell, Jeffery N. Carroll, Theresa R. Fletcher, Susan Landis Hockerman, Stephen A. Kolodziej, Madeleine H. Li, Deborah A. Mischke, Patrick B. Mullins, Carol Pearcy Howard, Joseph Gerace Rico, Nathan W. Stehle
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Publication number: 20040038966Abstract: A composition for use as an antiobestic agent and preventive or therapeutic agent for diabetes, containing a compound of the formula (I): 1Type: ApplicationFiled: November 25, 2002Publication date: February 26, 2004Inventors: Toshisada Yano, Isako Sakaguchi, Goro Katsuura, Naoki Yoshikawa
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Publication number: 20040023944Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.Type: ApplicationFiled: May 21, 2003Publication date: February 5, 2004Applicant: Beacon Laboratories, Inc.Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman
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Publication number: 20040023938Abstract: The present invention relates to microbicides for agricultural or horticultural use containing sulfonamide derivative of, for example, a formula (I): 1Type: ApplicationFiled: March 19, 2003Publication date: February 5, 2004Inventors: Takanori Tabuchi, Tetsuhiro Yamamoto, Masaharu Nakayama
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Publication number: 20040019038Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: ApplicationFiled: July 21, 2003Publication date: January 29, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John Robert Proudfoot, Alan D. Swinamer, Hidenori Takahashi, Thomas A. Gilmore, Rajiv Sharma
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Publication number: 20030232811Abstract: The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.Type: ApplicationFiled: January 31, 2003Publication date: December 18, 2003Applicant: TEIJIN LIMITEDInventors: Naoki Tsuchiya, Susumu Takeuchi, Takumi Takeyasu, Naoki Hase, Takao Yamori, Takashi Tsuruo
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Publication number: 20030232806Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification).Type: ApplicationFiled: May 6, 2003Publication date: December 18, 2003Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Takuya Seko, Masashi Kato
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Publication number: 20030229072Abstract: Disclosed are cyclic and acyclic amidines, pharmaceutical compositions containing such amidines, and their use in treating or preventing progesterone receptor mediated diseases or conditions, such as osteopenia and osteoporosis.Type: ApplicationFiled: March 3, 2003Publication date: December 11, 2003Inventors: William H Bullock, Harold C E Kluender, William L Collibee, Robert Dally, Martha E Rodriguez, Ming Wang
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Publication number: 20030216383Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het 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: October 1, 2002Publication date: November 20, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Weimin Liu, Denice M. Spero, David S. Thomson, Yancey D. Ward, Erick R.R. Young
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Patent number: 6642224Abstract: To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-METHYL-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4′-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.Type: GrantFiled: October 2, 2002Date of Patent: November 4, 2003Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Fukushi Hirayama, Hiroyuki Koshio, Tsukasa Ishihara, Norio Seki, Shunichiro Hachiya, Keizo Sugasawa, Ryota Shiraki, Yuji Koga, Yuzo Matsumoto, Takeshi Shigenaga, Souichirou Kawazoe
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Publication number: 20030195191Abstract: Compounds of formula (I): wherein R1 is bicyclyl or heterobicyclyl, R2 and R3 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, (C1-6)alkylthio, (C2-6)alkenylthio, (C2-6)alkynylthio, aryloxy, arylthio, heterocyclyloxy, heterocyclythio, (C1-6)alkoxy, (C1-6)alkenyloxy, aryl(C1-6)alkoxy, aryl(C1-6)alkylthio, amino, mono- or di-(C1-6)alkylamino, acylamino, sulfonylamino, cycloalkyl, cycloalkenyl, carboxylic acid (C1-6) ester, hydroxy, halogen, carboxamide: CONR8R9 where R8 and R9 are independently selected from the group consisting of hydrogen, alkyl, aryl, arylalkyl and heterocyclyl and includes R8 and R9 as part of a heterocyclyl group, or R2 and R3 together form a cyclic alkyl or alkenyl; R4 and R5 are each independently aryl, heteroaryl, heterocyclyl, alkoxy, alkyl, hydroxy or optionally substituted amino; R6 and R7 are each hydrogen or together form a fused aryl ring; and m and n are each independently from 0 to 2; with the proviso that when n=1 neither R4 nor RType: ApplicationFiled: May 12, 2003Publication date: October 16, 2003Inventors: Gordon Burton, Barry Sidney Orlek
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Publication number: 20030171347Abstract: The present invention relates to novel sigma receptor antagonist compounds that have anti-cocaine properties. These sigma receptor antagonists are useful in the treatment of cocaine overdose and addiction as well as movement disorders. The sigma receptor antagonists of the present invention may also be used in the treatment of neurological, psychiatric, gastrointestinal, cardiovascular, endocrine and immune system disorders as well as for imaging procedures. The present invention also relates to novel pharmaceutical compounds incorporating sigma receptor antagonists which can be used to treat overdose and addiction resulting from the use of cocaine and/or other drugs of abuse.Type: ApplicationFiled: June 21, 2002Publication date: September 11, 2003Inventor: Rae R. Matsumoto