Polycyclo Heterocyclic Ring System Containing Ring Nitrogen Patents (Class 548/181)
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Patent number: 7119104Abstract: A compound represented by the formula (I) or a salt of the compound, and a PPAR-? activator which contains the compound or salt as the active ingredient: (wherein A represents O or S; B1 represents N, etc.; B2 represents O, etc.; each of X1 and X2 represents O, S, a bond, etc.; Y represents C1-8 alkylene chain; Z represents O or S; R1 represents aryl, etc. which can have substituents; R2 represents C1-8 alkyl, etc.; R3 represents C1-8 alkyl, C2-8 alkenyl, etc.; each of R4 and R5 represents hydrogen, C1-8 alkyl, etc.; and R6 represents hydrogen, etc.; provided that each of Z and R3 is attached to the benzene ring, and X2 is not attached to the benzene ring).Type: GrantFiled: October 9, 2002Date of Patent: October 10, 2006Assignee: Nippon Chemiphar, Co., Ltd.Inventors: Shogo Sakuma, Tomio Yamakawa, Takashi Kanda, Seiichiro Masui
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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: 7115644Abstract: Disclosed are benzimidazolone compounds of formulas (I) & (II): wherein R1, R2, R3, R4, R5, X, L, m, n and t are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease.Type: GrantFiled: September 3, 2003Date of Patent: October 3, 2006Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Antonio Jose del Moral Barbosa, Jr., Daniel R. Goldberg, Abdelhakim Hammach, Pingrong Liu, Neil Moss, Mark Stephen Ralph, Gregory Paul Roth, Christopher Ronald Sarko, Fariba Soleymanzadeh, Andre White
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Patent number: 7112600Abstract: The present invention provides a fused ring compound of the following formula [I] ? wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. The compound of the present invention shows an anti-hepatitis C virus (HCV) action based on the HCV polymerase inhibitory activity, and is useful as a therapeutic agent or prophylactic agent for hepatitis C.Type: GrantFiled: June 26, 2002Date of Patent: September 26, 2006Assignee: Japan Tobacco Inc.Inventors: Hiromasa Hashimoto, Kenji Mizutani, Atsuhito Yoshida
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Patent number: 7094794Abstract: Substituted thiazole-benzoisothiazole dioxide derivatives, process for their preparation and their use. The invention relates to compounds of the formula I in which the radicals have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example as medicaments for lowering the blood glucose and for the prevention and treatment of diabetes.Type: GrantFiled: July 27, 2004Date of Patent: August 22, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Stefan Petry, Karl-Heinz Baringhaus, Norbert Tennagels, Guenter Mueller
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Patent number: 7087576Abstract: Novel dipeptide ethers are effective for lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyceride levels. The dipeptide ethers are also useful for the treatment and/or prophylaxis of diabetes, obesity, inflammation and autoimmune diseases such as multiple sclerosis and rheumatoid arthritis.Type: GrantFiled: October 7, 2003Date of Patent: August 8, 2006Assignee: Bexel Pharmaceuticals, Inc.Inventors: Bishwajit Nag, Abhijeet Nag, Debendranath Dey, Partha Neogi, Shiv Kumar Agarwal, Surendra Kumar Pandey
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Patent number: 7053221Abstract: A method is provided for carrying out depolymerization of a polymer containing electrophilic linkages in the presence of a catalyst and a nucleophilic reagent, wherein production of undesirable byproducts resulting from polymer degradation is minimized. The reaction can be carried out at a temperature of 80° C. or less, and generally involves the use of an organic, nonmetallic catalyst, thereby ensuring that the depolymerization product(s) are substantially free of metal contaminants. In an exemplary depolymerization method, the catalyst is a carbene compound such as an N-heterocyclic carbene, or is a precursor to a carbene compound. The method provides an important alternative to current recycling techniques such as those used in the degradation of polyesters, polyamides, and the like.Type: GrantFiled: January 30, 2003Date of Patent: May 30, 2006Assignee: International Business Machines CorporationInventors: James Lupton Hedrick, Gregory Walker Nyce, Robert M. Waymouth
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Patent number: 7045544Abstract: The invention relates to compounds of formula (I), to a method for the production thereof, and to the use of the same as pharmaceuticals for the treatment of diseases in humans and/or animalsType: GrantFiled: September 16, 2002Date of Patent: May 16, 2006Assignee: Bayer HealthCare AGInventors: Jens-Kerim Ergüden, Thomas Krahn, Christian Schröder, Johannes-Peter Stasch, Stefan Weigand, Hanno Wild, Michael Brands
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Patent number: 7026316Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: March 22, 2002Date of Patent: April 11, 2006Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Charles G. Caldwell, Hyun O. Ok, Emma R. Parmee, Ann E. Weber
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Patent number: 6995262Abstract: The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae (a) to (n) given in the claims. The polymethine dyes according to the invention are suitable for use as dyes and/or labels, in particular for staining or labeling biomolecules.Type: GrantFiled: July 24, 2000Date of Patent: February 7, 2006Assignee: Bayer CropScience AGInventors: Geert Deroover, Michael Missfeldt, Lydia Simon
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Patent number: 6984652Abstract: Compounds comprising an indazolyl group and a thiazolyl group, preferably 7-substituted 3-(thiazol-2-yl)-1H-indazole compounds in which the indazolyl group and a thiazolyl group are each independently optionally substituted, are useful for the treatment or prophylaxis of bacterial infections in mammals. The compounds are believed to function by inhibiting gyrase B.Type: GrantFiled: May 17, 2004Date of Patent: January 10, 2006Assignee: Warner-Lambert Company LLCInventors: Kraig Yager, Shaosong Chu, Krzysztof Appelt, Xiaoming Li
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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: 6960591Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: GrantFiled: July 4, 2001Date of Patent: November 1, 2005Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
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Patent number: 6949543Abstract: The invention relates to a novel amide derivative which is an N-({[4-(substituted thiazol-4-yl)phenyl]carbamoyl}methyl)amide derivative having a characteristic in that an aryl or heteroaryl group as an aromatic ring group is directly substituted on the N atom of amido group. Since said amide derivative has excellent anti-herpesvirus action, it is useful as medicaments and antiviral agents, particularly as preventive or therapeutic agents for various diseases accompanied by Herpesviridae virus infections, illustratively, varicella (chickenpox) accompanied by varicella zoster virus infection, shingles accompanied by the recurrent infection of latent varicella zoster virus, labial herpes and herpes encephalitis accompanied by HSV-1 infection, genital herpes accompanied by HSV-2 and the like various herpesvirus infections.Type: GrantFiled: November 8, 2001Date of Patent: September 27, 2005Assignees: Yamanouchi Pharmaceutical Co., Ltd., Rational Drug Design LaboratoriesInventors: Toru Kontani, Junji Miyata, Wataru Hamaguchi, Yoji Miyazaki, Hiroshi Suzuki, Eiichi Nakai, Shunji Kageyama
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Patent number: 6924297Abstract: Compounds of formula (I) and pharmaceutically acceptable derivatives thereof bind with high affinity to the EP4 receptor and are of use in the treatment or prevention of conditions such as a pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.Type: GrantFiled: December 20, 2001Date of Patent: August 2, 2005Assignee: SmithKline Beecham CorporationInventors: Gerard Martin Paul Giblin, Haydn Terence Jones, Andrew McMurtrie Mason, Neil Derek Miller, Susan Roomans, Stephen Edward Shanahan, Ann Louise Walker
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Patent number: 6916819Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: GrantFiled: December 21, 2001Date of Patent: July 12, 2005Assignee: Neurogen CorporationInventors: Guiying Li, John M. Peterson, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, Vinod Singh, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu
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Patent number: 6911463Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.Type: GrantFiled: August 6, 2002Date of Patent: June 28, 2005Assignee: Eli Lilly and CompanyInventors: Daniel Jon Sall, Jolie Anne Bastian, Cynthia Darshini Jesudason, Theo Schotten, Gerd Reuhter, Don Richard Finley, Freddie Craig Stevens, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, John Xiaoqiang He, John Arnold Werner, William George Trankle, Andrew Michael Ratz
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Patent number: 6852716Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: February 10, 2003Date of Patent: February 8, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Jason K. Myers, Vincent E. Groppi, Jr.
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Patent number: 6849631Abstract: The present invention relates to the synthesis of a new class of indeno [1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.Type: GrantFiled: December 7, 2001Date of Patent: February 1, 2005Assignee: Bristol Myers Squibb Pharma CompanyInventor: David J. Carini
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Patent number: 6841566Abstract: An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: wherein R1 is selected from: H, haloalkyl, (C1-6)alkyl, (C2-6)alkenyl, (C3-7)cycloalkyl, (C2-6)alkynyl, (C5-7)cycloalkenyl, 6 or 10-membered aryl, Het all optionally substituted; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C6-10)bicycloalkyl, 6- or 10-membered aryl, or Het all optionally substituted; B is N or CR5, wherein R5 is H, halogen, haloalkyl, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; X is N or CR5; D is N or CR5; each of Y1 and Y2 is independently O or S; Z is O, N, or NRZ wherein RZ is H, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; R3 and R4 are each independently H, (C1-6)alkyl, first (C3-7)cycloalkyl or 6- or 10-membered aryl, Het (C1-6)alkyl-6- or 10-membered aryl, (C1-6)alkyl-Het; or each R3 and R4 are independently covalently bonded together to form second (C3-7)cycloalkyl, or heterocycle, all optionally substituted; or when Z is N, either R3 or R4Type: GrantFiled: July 18, 2002Date of Patent: January 11, 2005Assignee: Boehringer Ingelheim, Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos
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Publication number: 20040267023Abstract: A novel process for the preparation of compounds of formula I 1Type: ApplicationFiled: June 21, 2004Publication date: December 30, 2004Inventors: Wolfgang Goehring, Ursula Hoffmann, Michelangelo Scalone, Helmut Stahr, Shaoning Wang
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Publication number: 20040259922Abstract: The present invention relates to epothilon derivatives, processes for their production and their use in the manufacture of medicaments and plant protection agents.Type: ApplicationFiled: February 17, 2004Publication date: December 23, 2004Inventors: Gerhard Hoefle, Thomas Leibold
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Publication number: 20040260098Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.Type: ApplicationFiled: March 28, 2003Publication date: December 23, 2004Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J. Sorensen, Aaron Balog, Kenneth A. Savin
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Publication number: 20040259923Abstract: A compound of the formula (I): R1—NH—X—Y-Z (I) wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a mammal, and the like.Type: ApplicationFiled: January 27, 2004Publication date: December 23, 2004Applicant: Fujisawa Pharmaceutical Co. Ltd.Inventors: Takayuki Inoue, Takashi Tojo, Masataka Morita, Mitsuru Ohkubo, Kousei Yoshihara, Akira Nagashima
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Publication number: 20040242593Abstract: 1′-substituted cannabinoid derivatives of delta-8-tetrahydrocannabinol, delta-9-tetrahydrocannabinol, and delta-6a-10a-tetrahydrocannabinol that have affinity for the cannabinoid receptor type-1 (CB-1) and/or cannabinoid receptor type-2 (CB-2). Compounds having activity as either agonists or antagonists of the CB-1 and/or CB-2 receptors can be used for treating CB-1 or CB-2 mediated conditions.Type: ApplicationFiled: May 20, 2004Publication date: December 2, 2004Inventors: Bob M. Moore, Antonio M. Ferreira, Mathangi Krishnamurthy
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Publication number: 20040242602Abstract: The present invention relates to modulators of the calcium sensing receptor having the formula I 1Type: ApplicationFiled: February 10, 2004Publication date: December 2, 2004Inventors: Timur Gungor, John K. Dickson
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Publication number: 20040235914Abstract: The present invention relates to the use of compounds of the general Formula (XIII): 1Type: ApplicationFiled: May 6, 2004Publication date: November 25, 2004Applicant: 4 SC AGInventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
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Publication number: 20040235833Abstract: The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: ApplicationFiled: March 12, 2004Publication date: November 25, 2004Applicant: Pfizer IncInventors: Alan Daniel Brown, Justin Stephen Bryans, Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Simon John Mantell
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Publication number: 20040235916Abstract: The invention relates to the novel compounds of formula (I), to a method for producing the same and to their use as drugs, especially as antiviral drugs.Type: ApplicationFiled: December 19, 2003Publication date: November 25, 2004Inventors: Rudolf Schohe-Loop, Ulrich Betz, Rudiger Fischer, Martin Hendrix, Gerald Kleymann, Judith Baumeister, Wolfgang Bender, Peter Eckenberg, Gabriele Handke-Erguden, Kerstin Henninger, Axel Jensen, Jorg Keldenich, Udo Schneider, Olaf Weber
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Patent number: 6821964Abstract: Chemokine receptor antagonists, in particular, bicyclic diamine compounds of Formula (I) that act as antagonists of chemokine CCR2 and CCR3 receptors including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leucocyte accumulation are described herein.Type: GrantFiled: March 6, 2002Date of Patent: November 23, 2004Assignee: Pfizer IncInventors: Roberto Colon-Cruz, Mary T. Didiuk, Erin M. Duffy, Ravi Garigipati, Wan F. Lau, Wayne S. McDonald
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Publication number: 20040229926Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: 1Type: ApplicationFiled: June 22, 2004Publication date: November 18, 2004Applicant: TANABE SEIYAKU CO., LTD.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Publication number: 20040224994Abstract: Insecticidal (dihalopropenyl) phenylalkyl substituted dihydrobenzofuran and dihydrobenzopyran derivatives of Formula I are disclosed. These compounds provide unexpected insecticidal activity across a spectrum of insect pests combined with desirable physical properties including improved photostability.Type: ApplicationFiled: April 27, 2004Publication date: November 11, 2004Inventors: George Theodoridis, Edward J. Barron, Dominic P. Suarez, Y. Larry Zhang, Ping Ding, David M. Roush, Stephen F. Donovan, Frank J. Zawacki, Walter H. Yeager, John W. Lyga, Daniel H. Cohen
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Publication number: 20040220183Abstract: The invention relates to new hydroxyindoles of the Formula, 1Type: ApplicationFiled: May 27, 2004Publication date: November 4, 2004Inventors: Norbert Hofgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelenyi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
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Patent number: 6809098Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicament, a method of therapeutic treatment using such a compound and processes for producing the compounds.Type: GrantFiled: August 21, 2002Date of Patent: October 26, 2004Assignee: AstraZeneca ABInventors: Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
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Publication number: 20040209929Abstract: Fused heteroarylcarboxylic acids of formula (I): 1Type: ApplicationFiled: February 19, 2004Publication date: October 21, 2004Applicant: Agouron Pharmaceuticals, Inc.Inventors: Donald Skalitzky, Wei-Guo Su, Luke Raymond Zehnder
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Publication number: 20040209889Abstract: Compounds represented by Formula (I): (I)or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: ApplicationFiled: July 29, 2003Publication date: October 21, 2004Inventors: Christopher F Claiborne, David A Claremon, Brian E Libby, John W Butcher, John A McCauley, Nigel J Liverton, Peter M Munson, Kevin T Nguyen, Brian Phillips, Wayne Thompson
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Publication number: 20040209867Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: ApplicationFiled: April 20, 2004Publication date: October 21, 2004Applicant: WyethInventors: Derek Cecil Cole, Joseph Raymond Stock, William Joseph Lennox, Ping Zhou
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Publication number: 20040204588Abstract: A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.Type: ApplicationFiled: February 11, 2003Publication date: October 14, 2004Inventors: Hector F. DeLuca, Pawel K. Grzywacz, Rafal R. Sicinski
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Patent number: 6797708Abstract: This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.Type: GrantFiled: November 22, 2002Date of Patent: September 28, 2004Assignee: WyethInventors: John C. McKew, Steven Y. Tam, Katherine L. Lee, Lihren Chen, Paresh Thakker, Fuk-Wah Sum, Mark Behnke, Baihua Hu, James D. Clark
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Patent number: 6794406Abstract: The invention relates to new indole derivatives, processes for their preparation, and their use in medicaments.Type: GrantFiled: December 21, 2001Date of Patent: September 21, 2004Assignee: Bayer AktiengesellschaftInventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Christiane Faeste
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Patent number: 6794404Abstract: A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (CType: GrantFiled: September 10, 2002Date of Patent: September 21, 2004Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
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Publication number: 20040180885Abstract: Indole derivatives represented by formula (I): 1Type: ApplicationFiled: March 8, 2004Publication date: September 16, 2004Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Kazuhiko Torisu, Kaoru Kobayashi, Fumio Nambu
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Publication number: 20040180881Abstract: Compounds which are oxazolyl-pyrazole derivatives, as defined in the specification, and pharmaceutically acceptable salts thereof; are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.Type: ApplicationFiled: April 15, 2004Publication date: September 16, 2004Inventors: Daniela Berta, Eduard Felder, Anna Vulpetti, Marzia Villa
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Publication number: 20040181062Abstract: This invention provides a compound of the following formula: 1Type: ApplicationFiled: February 5, 2004Publication date: September 16, 2004Applicant: Pfizer IncInventors: Yoshiyuki Okumura, Yoshinori Murata, Takashi Mano
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Publication number: 20040180925Abstract: A compound represented by general formula (I):Type: ApplicationFiled: November 10, 2003Publication date: September 16, 2004Inventors: Kenji Matsuno, Kimihisa Ueno, Yasuhiro Iwata, Yuichi Matsumoto, Satoshi Nakanishi, Kotaro Tasaki, Hideaki Kusaka, Yuji Nomoto, Akira Ogawa
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Publication number: 20040176428Abstract: Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (Formula I) are inhibitors of the dipep tidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent diabetes mellitus.Type: ApplicationFiled: December 18, 2003Publication date: September 9, 2004Inventors: Scott D. Edmondson, Emma Parmee, Ann E. Weber, Jinyou Xu
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Publication number: 20040176429Abstract: A microbial method for the preparation of an epothilone containing a terminal hydroxyalkyl group, comprising contacting at least one epothilone having a terminal alkyl group with an enzyme or microorganism capable of catalyzing the selective hydroxylation of said alkyl group to a hydroxyalkyl group, and effecting said hydroxylation.Type: ApplicationFiled: March 23, 2004Publication date: September 9, 2004Inventors: Wenying Li, James A. Matson, Xiaohua Huang, Kin Sing Lam, Grace A. McClure
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Publication number: 20040176431Abstract: Aminothiazole compounds substituted with sulfur-containing groups are represented by the Formula (I), and their pharmaceutically acceptable salts, prodrugs, active metabolites, and pharmaceutically acceptable salts of said metabolites are described.Type: ApplicationFiled: February 11, 2004Publication date: September 9, 2004Applicant: Pfizer, Inc.Inventors: Wesley K.M. Chong, Shao Song Chu, Rohit K. Duvadie, James Na, Lana Schaffer, Yi Yang, Lin Li
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Patent number: 6787561Abstract: A benzimidazole compound or a salt thereof which has an inhibitory action of forming of macrophages and is useful as an active ingredient of an orally available medicament for preventive and/or therapeutic treatment of arteriosclerosis, which is represented by the formula (I): wherein, R1 represents one or more functional groups on the benzene ring selected from the group consisting of hydrogen atom, a halogen atom, a lower alkyl group and a lower alkoxy group; R2 represents hydrogen atom, an alkyl group or an acyl group; L represents a C4-C8 alkylene group or an ethyleneoxy linking group represented as (CH2CH2O)nCH2CH2 wherein n represents 1 or 2; X represents O or NH; Y represents S or a single bond; and Q represents a 5- or 6-membered heterocyclic group which may have a functional group on the ring.Type: GrantFiled: June 5, 2002Date of Patent: September 7, 2004Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Aoki, Kazuhiro Aikawa, Masayuki Kawakami, Yongzhe Yan
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Patent number: 6787651Abstract: Disclosed are substituted indoles, pharmaceutical compositions containing such indoles, and their use in treating or preventing PPAR-&ggr; mediated diseases or conditions, such as osteopenia, osteoporosis, cancer, diabetes and atherosclerosis.Type: GrantFiled: October 9, 2001Date of Patent: September 7, 2004Assignee: SmithKline Beecham CorporationInventors: Andreas Stolle, Jacques P. Dumas, William Carley, Philip D. G. Coish, Steven R. Magnuson, Yamin Wang, Dhanapalan Nagarathnam, Derek B. Lowe, Ning Su, William H. Bullock, Ann-Marie Campbell, Ning Qi, Jeremy L. Baryza, James H. Cook