Polycyclo Ring System Having The 1,3-diazole Ring As One Of The Cyclos Patents (Class 546/273.1)
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Publication number: 20100298287Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: ApplicationFiled: January 21, 2009Publication date: November 25, 2010Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
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Patent number: 7825115Abstract: The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.Type: GrantFiled: January 10, 2008Date of Patent: November 2, 2010Assignee: Aventis Pharma S.A.Inventors: Marcel Patek, Anil Nair, Augustin Hittinger, Conception Nemecek, Daniel Bond, Greg Harlow, Herve Bouchard, Jacques Mauger, Jean-Luc Malleron, Mark Palermo, Fahad Al-Obeidi, Thomas Faitg, Hartmut Strobel, Sven Ruf, Kurt Ritter, Youssef El-Ahmad, Dominique Lesuisse, Didier Bénard
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Patent number: 7666879Abstract: The present invention provides compounds that are inhibitors of VEGF-R2 of the formula: (I) and methods of using these compounds.Type: GrantFiled: February 23, 2006Date of Patent: February 23, 2010Assignee: Eli Lilly and CompanyInventors: David Anthony Barda, Timothy Paul Burkholder, Joshua Ryan Clayton, Yan Hao, James Robert Henry, John Monte Knobeloch, Johnathan Alexander McLean, David Mendel, Mark Edward Rempala, Zhao-Qing Wang, Yvonne Yee Mai Yip, Boyu Zhong
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Publication number: 20090318499Abstract: The compounds shown by their structural formulas in the specification have analgesic and or immunostimulant activity in mammals.Type: ApplicationFiled: January 25, 2006Publication date: December 24, 2009Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
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Patent number: 7632578Abstract: An emitting compound for an organic electroluminescent device, and an organic electroluminescent device using the same, supply an effective luminance, an efficient driving voltage, and color purity. The emitting compound has an imidazo-pyridine frame represented as in the following Formula 1: where R1 to R14, each of which is independent, refer to the functional groups recited herein.Type: GrantFiled: February 4, 2004Date of Patent: December 15, 2009Assignee: Samsung Mobile Display Co., Ltd.Inventors: Seok-Jong Lee, Yong-Joong Choi
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Publication number: 20090291968Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: March 21, 2007Publication date: November 26, 2009Inventors: Guy Georges, Bernhard Goller, Anja Limberg, Petra Rueger, Matthias Rueth, Christine Schuell, Mark Stahl
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Publication number: 20090286772Abstract: The invention encompasses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.Type: ApplicationFiled: February 22, 2007Publication date: November 19, 2009Inventors: Anh Chau, Bernard Cote, Yves Ducharme, Richard Frenette, Richard Friesen, Marc Gagnon, Andre Giroux, Evelyn Martins, Hongping Yu, Pierre Hamel
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Publication number: 20090278115Abstract: A novel nitrogen-containing heterocyclic derivative having a specific structure and an organic electroluminescence device comprising an anode, a cathode and an organic thin film layer which comprises a single layer or a plurality of layers comprising at least a light emitting layer and is disposed between the anode and the cathode, wherein at least one layer in the organic thin film layer comprises the above nitrogen-containing heterocyclic derivative singly or as a component of a mixture. The organic electroluminescence device exhibits a great luminance of emitted light and a great efficiency of light emission even under application of a low voltage.Type: ApplicationFiled: May 10, 2006Publication date: November 12, 2009Applicant: Idemitsu Kosan Co., Ltd.Inventors: Chishio Hosokawa, Hiroshi Yamamoto, Takashi Arakane
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Patent number: 7589114Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-sulfonyl]-azetidine-carboxylic acids, esters and amides which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: April 4, 2006Date of Patent: September 15, 2009Assignee: Boehringer Ingelheim International GmbHInventor: Steven Richard Brunette
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Publication number: 20090209571Abstract: The invention encompasses novel compounds of Formula or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.Type: ApplicationFiled: May 15, 2007Publication date: August 20, 2009Inventors: Bernard Cote, Yves Ducharme, Richard Frenette, Richard Friesen, Andre Giroux, Evelyn Martins, Pierre Hamel
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Publication number: 20090209540Abstract: Disclosed are biaryl benzoimidazole derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, stroke, bladder hypersensitivity, irritable bowel syndrome, a respiratory disorder such as cough, asthma, and chronic obstructive pulmonary disease, burning, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases.Type: ApplicationFiled: July 11, 2007Publication date: August 20, 2009Applicant: DAEWOONG PHARMACEUTICAL CO., LTD.Inventors: Ji Duck Kim, Hong-Chul Yoon, In Woo Kim, Hyae Jung Hyun
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Publication number: 20090176838Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: January 15, 2007Publication date: July 9, 2009Applicant: Purdue Pharma L.P.Inventor: Xiaoming Zhou
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Publication number: 20090105266Abstract: The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the formula (I): in which the substitutents are as defined in claim 1 and salts, solvates, hydrates and N-oxides thereof.Type: ApplicationFiled: April 18, 2008Publication date: April 23, 2009Inventors: Ralf Glatthar, David Carcache
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Patent number: 7517897Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: May 12, 2006Date of Patent: April 14, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Magnus Carl Arne Eriksson, Rene Marc Lemieux
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Patent number: 7498354Abstract: or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors and cancers.Type: GrantFiled: March 30, 2006Date of Patent: March 3, 2009Assignee: OSI Pharmaceuticals, Inc.Inventors: Andrew Philip Crew, Bijoy Panicker, Han-Qing Dong
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Publication number: 20090042854Abstract: The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: ApplicationFiled: January 19, 2007Publication date: February 12, 2009Inventors: Jianming Bao, Robert J. DeVita, Huagang Lu, Sander G. Mills, Gregori J. Morriello
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Publication number: 20090042873Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: ApplicationFiled: August 1, 2008Publication date: February 12, 2009Applicant: SANOFI-AVENTISInventors: Laurent DUBOIS, Yannick EVANNO, Luc EVEN, Catherine GILLE, Andre MALANDA, David MACHNIK, Nathalie RAKOTOARISOA
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Derivatives of [6,7-dihydro-5-imidazo[1,2-]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide
Patent number: 7462637Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: October 20, 2004Date of Patent: December 9, 2008Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence A. Kelly, Jin Mi Kim, René Marc Lemieux, Matt Aaron Tschantz -
Patent number: 7442716Abstract: The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.Type: GrantFiled: November 23, 2005Date of Patent: October 28, 2008Assignee: Merck Frosst Canada Ltd.Inventors: Anh Chau, Bernard Cote, Yves Ducharme, Richard Frenette, Richard Friesen, Marc Gagnon, Andre Giroux, Evelyn Martins, Hongping Yu, Tom Wu
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Patent number: 7414066Abstract: The present invention provides to a novel compound having an ACAT inhibiting activity.Type: GrantFiled: November 9, 2004Date of Patent: August 19, 2008Assignee: Kowa Company Ltd.Inventors: Kimiyuki Shibuya, Toru Miura, Katsumi Kawamine, Yukihiro Sato, Tadaaki Ohgiya, Takahiro Kitamura, Chiyoka Ozaki, Toshiyuki Edano, Mitsuteru Hirata
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Patent number: 7414046Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: May 23, 2003Date of Patent: August 19, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
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Publication number: 20080171769Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.Type: ApplicationFiled: August 10, 2007Publication date: July 17, 2008Inventors: Vlad E. Gregor, Yahua Liu, Alexey Anikin, Danny Peter Claude McGee, Charles Mikel, Douglas Eric McGrath, Goverdhan Reddy Vavilala, Jason C. Pickens, Alexander Kadushkin, Luyong Jiang, Mohan Santhanam Thiruvazhi, Sergey Zozulya, Rajendran Vairagoundar, Tong Zhu, Alexander Chucholowski, Thomas Webb, Vidyasagar Reddy Gantla, Zheng Yan
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Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Patent number: 7244746Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: February 4, 2004Date of Patent: July 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Xiaojun Han, Gene M. Dubowchik, John E. Macor
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Patent number: 7211669Abstract: The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.Type: GrantFiled: January 29, 2004Date of Patent: May 1, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Dmitry Zuev, Bireshwar Dasgupta
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Patent number: 7205406Abstract: An azomethine dye represented by the following Formula 1: wherein Y represents a substituent of 0.2??p?0.9, Z1 and Z2 each represent —CR1?, where R1 represents a hydrogen atom or a substituent, or —N?, L represents the group represented by the following Formula 1a, X represents an unsubstituted or substituted di-alkylamino group, R represents an unsubstituted or substituted alkyl group, and n represents an integer more than 0. wherein B represents a group of non-metallic atoms which are necessary to form a heterocyclic ring.Type: GrantFiled: July 1, 2005Date of Patent: April 17, 2007Assignee: Konica Minolta Holdings, Inc.Inventors: Emiko Kataoka, Takatugu Suzuki, Dai Ikemizu
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Patent number: 7169793Abstract: A process of preparation of optically pure or optically enriched isomers of omeprazole and structurally related sulfoxides is provided. Also provided are an amorphous form of esomeprazole, as well a pharmaceutical composition containing it and a method of using it for treatment of gastric disorders.Type: GrantFiled: June 27, 2003Date of Patent: January 30, 2007Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Manne Satyanarayana Reddy, Muppa Kishore Kumar, Kikkuru Srirami Reddy, Koilkonda Purandhar, Keshaboina Sreenath
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Patent number: 7160920Abstract: Disclosed are (i) compounds of a steroid, a ?-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, ?-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO?), or as the neutral species, nitric oxide (NO.) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.Type: GrantFiled: May 5, 2003Date of Patent: January 9, 2007Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Stewart K. Richardson
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Patent number: 7057042Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherein A, L, D and B1 are as described in the specification.Type: GrantFiled: May 23, 2003Date of Patent: June 6, 2006Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Steven P. Latshaw, Sherry L. Nelson, Andrew O. Stewart
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Patent number: 6974823Abstract: The present invention relates generally to novel hydantoin derivative compounds, pharmaceutical compositions containing such compounds, and methods for their use in preventing and/or treating neurological disorders, including physically damaged nerves and neurodegenerative diseases; for treating alopecia and promoting hair growth; for treating vision disorders and/or improving vision; for treating memory impairment and/or enhancing memory performance; and for treating sensorineural hearing loss by administering such compounds.Type: GrantFiled: December 21, 2000Date of Patent: December 13, 2005Assignee: GPI NIL Holdindgs, Inc.Inventor: Gregory S. Hamilton
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Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6897225Abstract: The present invention relates to a compound of the following formula: or a pharmaceutically acceptable salt thereof. Also disclosed are compositions containing the compound and methods of preparing and using the compounds. The compounds of the invention are useful in treating ?L?2 adhesion mediated conditions in a mammal.Type: GrantFiled: October 19, 2000Date of Patent: May 24, 2005Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Ila Sircar, Marshall Morningstar, Paul Furth, Nicholas Smith, Bradley R. Teegarden, Ronald C. Griffith
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Patent number: 6861434Abstract: Compounds of the formula: useful for treatment of disorders of the dopaminergic system, such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.Type: GrantFiled: April 23, 2002Date of Patent: March 1, 2005Assignee: WyethInventor: Gary P. Stack
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Patent number: 6858630Abstract: Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected substituted naphthimidazole derivative.Type: GrantFiled: December 6, 2000Date of Patent: February 22, 2005Assignee: SmithKline Beecham CorporationInventors: Juan I. Luengo, Kevin J. Duffy, Alan T. Price, Lihua Zhang
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Patent number: 6852748Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: October 15, 2003Date of Patent: February 8, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence Alfred Kelly, Jin Mi Kim, René Marc Lemieux, Matt Aaron Tschantz
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Patent number: 6803368Abstract: Compounds of the formula useful for treatment of disorders of the dopaminergic system, such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.Type: GrantFiled: April 23, 2002Date of Patent: October 12, 2004Assignee: WyethInventors: Gary P. Stack, James A. Nelson
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Patent number: 6770639Abstract: Disclosed are novel compounds of formula (I): wherein Ar1, Ra, R4, R5, X and Y are defined below, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases associated with such kinases, for example, diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are processes for preparing these compounds, novel intermediates useful in these processes and compositions comprising compounds of the formula (I).Type: GrantFiled: November 12, 2002Date of Patent: August 3, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Roger John Snow, Mario Cardozo, Daniel Goldberg, Abdelhakim Hammach, Tina Morwick, Neil Moss, Usha R. Patel, Anthony S. Prokopowicz, III, Hidenori Takahashi, Matt Aaron Tschantz, Xiao-Jun Wang
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Publication number: 20040116426Abstract: Compounds of the formula I 1Type: ApplicationFiled: September 25, 2003Publication date: June 17, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Jiang-Ping Wu, Terence Alfred Kelly, Rene M. Lemieux, Daniel R. Goldberg, Jonathan Emilian Emeigh, Ronald John Sorcek
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Patent number: 6734203Abstract: This invention relates to medicaments, particularly novel fused imidazolium derivatives useful for the treatment of cancers and novel synthetic intermediate compounds thereof. The novel imidazolium derivatives fused with an aryl or heteroaryl ring, characterized in that the 1- and/or 3-position is substituted by an alkyl group etc. having a substituent selected from the group consisting of —ORa, —SRa and the like, have excellent anti-tumor activity and low toxicity and are useful as anticancer agents having wide margins of safety.Type: GrantFiled: July 1, 2002Date of Patent: May 11, 2004Inventors: Akira Matsuhisa, Isao Kinoyama, Akira Toyoshima, Takahito Nakahara, Masahiro Takeuchi, Minoru Okada
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Patent number: 6696441Abstract: The present invention provides compounds that act to suppress p53 activity in mammalian cells, and a method to effectively suppress p53 activity in the cells of a mammal subject to a stress or pathology that is ameliorated by such suppression.Type: GrantFiled: August 11, 2000Date of Patent: February 24, 2004Assignee: The Regents of the University of CaliforniaInventors: Howard B. Cottam, Lorenzo M. Leoni, Dennis A. Carson
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Publication number: 20030232817Abstract: Compounds of the formula I 1Type: ApplicationFiled: February 24, 2003Publication date: December 18, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventor: Roman Wolfgang Fleck
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Patent number: 6657064Abstract: A novel bicyclic imidazo-5-yl-amine derivative of Formula I, wherein X denotes CR5, N or S, and Y in the case where X denotes S, denotes CR6 or N and in all other cases denotes N, and methods for preparation thereof are disclosed. Also disclosed are methods for treating pain using the compound of Formula I, and pharmaceutical compositions comprising the compound of Formula I.Type: GrantFiled: April 8, 2002Date of Patent: December 2, 2003Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul
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Patent number: 6632809Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: December 12, 2001Date of Patent: October 14, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
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Publication number: 20030186960Abstract: The present invention relates to cyclized amino acid 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: January 3, 2002Publication date: October 2, 2003Inventors: David Lauffer, Brian Ledford
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Patent number: 6608098Abstract: This invention relates to compounds represented by the general formula [I] wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.Type: GrantFiled: February 25, 2002Date of Patent: August 19, 2003Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Toshio Nagase, Tomoharu Iino, Yoshiyuki Sato, Teruyuki Nishimura, Jun-ichi Eiki
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Patent number: 6573283Abstract: Compounds of the formula: are useful for the treatment of depression and other diseases such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction, eating disorders, obesity, addictive disorders caused by ethanol or cocaine abuse and related illnesses.Type: GrantFiled: April 23, 2002Date of Patent: June 3, 2003Assignee: WyethInventor: Gary P. Stack
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Publication number: 20030045526Abstract: Compounds of the formula: 1Type: ApplicationFiled: April 23, 2002Publication date: March 6, 2003Applicant: WyethInventor: Gary P. Stack
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Patent number: 6506769Abstract: Disclosed are novel compounds of formula (I): wherein Ar1, Ra, R4, R5, X and Y are defined below, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases associated with such kinases, for example, diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are processes for preparing these compounds, novel intermediates useful in these processes and compositions comprising compounds of the formula (I).Type: GrantFiled: August 2, 2001Date of Patent: January 14, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Roger John Snow, Mario Cardozo, Daniel Goldberg, Abdelhakim Hammach, Tina Morwick, Neil Moss, Usha R. Patel, Anthony S. Prokopowicz, III, Hidenori Takahashi, Matt Aaron Tschantz, Xiao-Jun Wang
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Publication number: 20030008848Abstract: Compound of the formula I, II, III or IV 1Type: ApplicationFiled: December 5, 2001Publication date: January 9, 2003Inventors: Roman Wolfgang Fleck, Terence Alfred Kelly, Jin Mi Kim, Jinbo Lee, Rene Marc Lemieux, Ronald John Sorcek, Jiang-Ping Wu
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Patent number: RE40245Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: April 28, 2004Date of Patent: April 15, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul S. Charifson, Dean Stamos, Yusheng Liao, Michael C. Badia, Martin Trudeau