Three Or More Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 514/228.5)
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Publication number: 20100267666Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1, R, and X are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: February 20, 2009Publication date: October 21, 2010Inventors: Joe Timothy Bamberg, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Alam Jahangir, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, David Bernard Smith, Michael Soth, Hanbiao Yang
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Publication number: 20100249120Abstract: The present invention relates to substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: March 31, 2010Publication date: September 30, 2010Applicant: ArQule, Inc.Inventors: Jason Hill, Manish Tandon, Nivedita Namdev, Rocio Palma, Neil Westlund, Anton Filikov
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Publication number: 20100249119Abstract: The present invention provides a heterocyclic compound having a strong Raf inhibitory activity, which is represented by the following formula wherein each substituent is as defined in the present specification, or a salt thereof.Type: ApplicationFiled: August 28, 2008Publication date: September 30, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masaaki Hirose, Masanori Okaniwa, Yoko Hayashi, Terufumi Takagi
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Publication number: 20100249030Abstract: The present invention relates to a method of treating cancer by pretreatment with anti-mitotic agents followed by at least one aurora kinase inhibitor. Extensive illustrations are provided for the antimitotic agents and aurora kinase inhibitors that are useful in the inventive treatment.Type: ApplicationFiled: July 28, 2008Publication date: September 30, 2010Inventor: Andrea Dawn Basso-Porcaro
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Publication number: 20100240638Abstract: The present application describes macrocyclic compounds of formula (I) with NS3 protease inhibitory activity for treating hepatitis C virus infection.Type: ApplicationFiled: February 19, 2008Publication date: September 23, 2010Inventors: Shawn D. Britt, Jiping Fu, David Thomas Parker, Michiael Patane, Parkash Raman, Branko Radetich, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng, Trixi Brand, Sylvain Cottens, Claus Ehrhardt, Stefan Andreas Randl, Pascal Rigollier, Nikolaus Schiering, Oliver Simic
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Publication number: 20100210629Abstract: The present invention provides for tricyclic compounds having the formula (I), wherein R1, R2, R5, R6, R7, and R8 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.Type: ApplicationFiled: April 23, 2010Publication date: August 19, 2010Inventors: William J. Pitts, James Kempson, Junqing Guo, Jagabandhu Das, Charles M. Langevine, Steven H. Spergel, Scott Hunter Watterson
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Patent number: 7776867Abstract: The present invention relates to furanopyrimidine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula I, methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula I.Type: GrantFiled: June 29, 2005Date of Patent: August 17, 2010Assignee: Amgen Inc.Inventors: John Laird Buchanan, William H. Buckner, Simon A. Burkitt, Erin F. DiMauro, Christopher N. Farthing, Alexander D. Frenkel, Martin J. Harrison, Frank Kayser, Jinqian Liu, Sarah E. Lively, Teresa L. Marshall, David C. McGowan, Rajiv Sharma, Stephen J. Shuttleworth, Xiaotian Zhu
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Publication number: 20100204203Abstract: The present invention provides a compound of a formula (I), wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.Type: ApplicationFiled: January 10, 2008Publication date: August 12, 2010Inventors: Roger Victor Bonnert, Frank Burkamp, Rhona Jane Cox, Simon de Sousa, Mark Dickinson, Simon Fraser Hunt, Premji Meghani, Austen Pimm, Hitesh Jayantilal Sanganee
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Publication number: 20100204187Abstract: Purine derivatives of Formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK3 kinase inhibitors.Type: ApplicationFiled: January 23, 2008Publication date: August 12, 2010Inventors: Jorge Salas Solana, Carmen Almansa Rosales, Robert Soliva Soliva, Montserrat Fontes Ustrell, Marina Virgili Bernadó, Josep Comelles Espuga, José Javier Pastor Porras
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Patent number: 7772226Abstract: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.Type: GrantFiled: August 28, 2008Date of Patent: August 10, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Seiji Yoshikawa, Eita Emori, Fumiyoshi Matsuura, Richard Clark, Hironori Ikuta, Kazunobu Kira, Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki
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Publication number: 20100196316Abstract: The present invention relates to cyclosporin analogues having antiviral activity against HCV and useful in the treatment of HCV infections. More particularly, the invention relates to novel cyclosporin analogue compounds, compositions containing such compounds and methods for using the same, as well as processes for making such compounds.Type: ApplicationFiled: January 30, 2010Publication date: August 5, 2010Inventors: Yat Sun Or, Guoqiang Wang, Jiang Long, Xuri Gao
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Publication number: 20100197674Abstract: The present invention is to provide an oxopyrazine derivative having an excellent herbicidal activity and besides exhibiting high safety for useful crops and the like, or a salt thereof, and a herbicide containing the same. The present invention relates to an oxopyrazine derivative represented by formula [I]: wherein X1 represents an oxygen atom or a sulfur atom; X2 represents CH or N(O)m; m represents an integer of 0 or 1; R1 represents a hydrogen atom, a C1-C12 alkyl group and the like; R2 represents a halogen atom, a cyano group and the like; R3 is a hydroxyl group, a halogen atom and the like; A1 represents C(R4R5); A2 represents C(R6R7) or C?O; A3 represents C(R8R9); R4 to R9 represent a hydrogen atom or an alkyl group, or a salt thereof, and a herbicide containing these compounds.Type: ApplicationFiled: July 31, 2008Publication date: August 5, 2010Applicants: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Ryuji Tamai, Minoru Ito, Masami Kobayashi, Takashi Mitsunari, Yuki Nakano
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Publication number: 20100190747Abstract: The present invention provides a compound represented by the formula: wherein the symbols are as described in the specification, or a salt thereof, which is useful for preventing/treating eicosanoid-associated diseases such as atherosclerosis, diabetes, obesity, atherothrombosis, asthma, fever, pain, cancer, rheumatism, osteoarthritis and atopic dermatitis, and which has an excellent pharmacological action, physicochemical properties, etc.Type: ApplicationFiled: January 26, 2010Publication date: July 29, 2010Inventors: Hideo Suzuki, Takuya Fujimoto, Takeshi Yamamoto
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Patent number: 7763624Abstract: The present invention relates to compounds of Formula I or a stereomer, a tautomer, a solvate, a pharmaceutically acceptable salt, or a prodrug thereof, pharmaceutical formulations containing the compounds, methods of treatments using the compounds, for example, protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders and methods of preparing medicaments comprising the compounds.Type: GrantFiled: August 18, 2006Date of Patent: July 27, 2010Assignee: Amgen Inc.Inventors: John L. Buchanan, William H. Buckner, Mario G. Cardozo, Erin F. DiMauro, Jiasheng Fu, Xiaolin Hao, Xian Yun Jiao, Frank Kayser, David J. Kopecky, Craig E. Masse, Susan A. Tomlinson, Ryan White, Xiaotian Zhu
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Publication number: 20100179125Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: September 2, 2009Publication date: July 15, 2010Applicant: Bayer HealthCare LLCInventors: Julie A. Dixon, Barton Phillips, Furahi Achebe, Harold C. E. Kluender, Jason Newcom, Kyle Parcella, Steven Magnuson, Zhenqiu Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler, Stephen O'Connor
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Publication number: 20100152174Abstract: The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-2alkyl-NR21—H2—CO—NH—C1-3alkyl- or —C1-2alkyl-NR23—CO—CR16R17—NH—; X1 represents O or —O—C1-2alkyl-; X2 represents a direct bond, C1-2alkyl, —CO—C1-2alkyl or NR12—C1-2alkyl; R1 represents hydrogen or halo; R2 represents halo, acetylene or Het1; R3 represents hydrogen or cyano; R4 represents Ar4—C1-4alkyloxy-, C1-4alkyloxy- or C1-4alkyloxy substituted with one or where possible two or more substituents selected from Het2, NR7R8, hydroxy and C1-4alkyloxy-C1-4alkyloxy-; R7 represents hydrogen or C1-4alkyl; R8 represents C1-4alkyl substituted with NR25R26 or C1-4alkylsulfonyl; R12 represents hydrogen or C1-4alkyl-; R13 represents Ar6-sulfonyl or C1-6alkyloxycarbonyl optionally substituted with phenyl; R16 and R17 represents hydrType: ApplicationFiled: December 8, 2005Publication date: June 17, 2010Inventors: Eddy Jean Edgard Freyne, Marc Willems, Peter Ten Holte, Alexandra Papanikos, Werner Constant John Embrechts, Pierre Henri Storck, Virginie Sophie Poncelet, Werner Constant Johan Embrechts, Pierre Henri Storck, Virginie Sophie Poncelet
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Patent number: 7723330Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: March 6, 2007Date of Patent: May 25, 2010Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Publication number: 20100125068Abstract: The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.Type: ApplicationFiled: January 15, 2010Publication date: May 20, 2010Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, David A. Parry
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Publication number: 20100113420Abstract: Pyrrolopyrimidine derivatives of Formula (I) that are useful as JAK3 kinase inhibitors.Type: ApplicationFiled: March 31, 2008Publication date: May 6, 2010Inventors: Jorge Salas Solana, Carmen Almansa Rosales, Robert Soliva Soliva, Montserrat Fontes Ustrell, Marc Vendrell Escobar
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Publication number: 20100113436Abstract: A compound having the formula (I) wherein ring A represents a substituted or unsubstituted monocyclic or multicyclic ring; m=any positive integer; n=0-5; X=CH and Y=—C(O)NR1R2, —NR1R2 or —S(O)2R4, where R1, R2 and R4 are each individually selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring, or any combination thereof, or R1 and R2 are linked so as to form part of a substituted or unsubstituted heterocyclic ring, or X=N and Y=—S(O)2R3 or —C(O)R3, where R3 is selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring or any combination thereof.Type: ApplicationFiled: October 1, 2007Publication date: May 6, 2010Inventors: Richard Amewu, Paul Micheal O'Neill, Andrew Stachulski, Gemma Ellis, Stephen Andrew Ward
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Patent number: 7704999Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.Type: GrantFiled: December 21, 2007Date of Patent: April 27, 2010Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Ulrich Niewöhner, Maria Niewöhner, legal representative, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jörg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski
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Publication number: 20100093714Abstract: This invention relates to a novel thieno[2,3-d]pyrimidine, A, and its therapeutic and prophylactic uses, wherein R1 and R2 are defined in the specification. Disorders treated and/or prevented include Parkinson's Disease.Type: ApplicationFiled: June 5, 2009Publication date: April 15, 2010Inventors: Devraj CHAKRAVARTY, Brian Christopher SHOOK
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Publication number: 20100093702Abstract: This invention relates to a novel thieno[2,3-d]pyrimidine, A, and its therapeutic and prophylactic uses, wherein R1 and R2 are defined in the specification. Disorders treated and/or prevented include Parkinson's Disease.Type: ApplicationFiled: June 5, 2009Publication date: April 15, 2010Inventors: J. Kent Barbay, Devraj Chakravarty, Brian Christopher Shook, Aihua Wang
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Publication number: 20100063032Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer s disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia.Type: ApplicationFiled: March 24, 2008Publication date: March 11, 2010Inventors: John S. Debenham, Christina B. Madsen-Duggan, Thomas F. Walsh
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Publication number: 20100063024Abstract: The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R2 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R3 is a hydrogen atom or a lower alkyl group; R4 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R1k)R1m; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.Type: ApplicationFiled: April 25, 2007Publication date: March 11, 2010Inventors: Toshihiro Sakamoto, Takeshi Sagara, Sachie Otsuki, Satoshi Sunami, Kenji Niiyama, Fuyuki Yamamoto, Takashi Yoshizumi, Hidetomo Furuyama, Yasuhiro Goto, Makoto Bamba, Keiji Takahashi, Hiroshi Hirai, Toshihide Nishibata
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Publication number: 20100063038Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: December 1, 2006Publication date: March 11, 2010Inventors: Julie Dixon, Barton Phillips, Furahi Achebe, Harold Kluender, Jason Newcom, Kyle Parcella, Stephen J. O'Connor, Steven Magnuson, Zhenqui Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler
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Patent number: 7674788Abstract: The invention relates to new pteridines which are suitable for treating respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system and cancers. This invention also relates to pharmaceutical compositions containing these compounds.Type: GrantFiled: May 22, 2007Date of Patent: March 9, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Horst Dollinger, Domnic Martyres, Juergen Mack, Rolf Goeggel, Birgit Jung, Peter Nickolaus
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Publication number: 20100048544Abstract: Tricyclic nitrogen-containing compounds of Formula (I) or pharmaceutically acceptable salts and/or N-oxides thereof: compositions containing them, their use in the treatment of tuberculosis, and methods for the preparation of such compounds.Type: ApplicationFiled: April 10, 2008Publication date: February 25, 2010Inventors: Lluis Ballell-Pages, David Barros-Aguirre, Julia Castro-Pichel, Modesto Jesus Remuinan-Blanco, Jose Maria Fiandor-Roman
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Patent number: 7659280Abstract: The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula I, as well as related compositions and methods for treating a variety of autoimmune diseases.Type: GrantFiled: February 16, 2007Date of Patent: February 9, 2010Assignee: Rigel Pharmaceuticals, Inc.Inventors: Jeffrey Wayne Clough, Somasekhar Bhamidipati, Rajinder Singh, Esteban Masuda, Haoran Zhao
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Publication number: 20100029619Abstract: The present invention provides a compound represented by the formula (I): wherein ring A is a ring which is optionally further substituted; R1 is a hydrogen atom or a substituent; R2 is a hydrogen atom or a substituent; R3 is a hydrogen atom or a substituent; R4 is a hydrogen atom or a substituent; R5 is a hydrogen atom or a substituent; R6 is a hydrogen atom or a substituent; X is ?N— or ?C(Z)- (Z is a hydrogen atom or a substituent); when X is ?C(Z)-, Z and R6 are optionally bonded to each other to form, together with the carbon atom bonded thereto, an optionally substituted ring, provided that when X is ?CH—, then R6 is not optionally substituted 2-piperidinyl, excluding N-imidazo[1,2-a]pyridin-2-yl-4-methyl-benzamide, N-imidazo[1,2-a]pyridin-2-yl-benzamide and N-(7-methylimidazo[1,2-a]pyridin-2-yl)-benzamide, or a salt thereof, and a pharmaceutical agent containing same.Type: ApplicationFiled: August 3, 2007Publication date: February 4, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMTEDInventors: Osamu Uchikawa, Nozomu Sakai, Yoshito Terao, Hideo Suzuki
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Publication number: 20100029627Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y represents —C3-9alkyl-, —C1-5alkyl-NR6—C1-5alkyl- or —C1-5alkyl-NR7—CO—C1-5alkyl-; X1 represents —O—; X2 represents NR5—C1-2alkyl-; R1 represents hydrogen, halo or Het3-O—; R2 represents hydrogen; R3 represents hydroxy, C1-4alkyloxy- or C1-4alkyloxy substituted with one or two substituents each independently selected from Het4, hydroxy, C1-4alkyloxy-, C1-4alkyloxy-C1-4alkyloxy and NR9R10; R5 represents hydrogen or C1-4alkyl; R6 represents hydrogen or C1-4alkyl; R7 represents hydrogen; R9 and R10 each independently represent hydrogen; C1-4alkyl-S(?O)2—C1-4alkyl-C(?O)—; C1-4alkyl or C1-4alkyl substituted with hydroxy; Het3 represents pyridinyl optionally substituted with C1-4alkyl; Het4 represents morpholinyl, piperidinyl or piperazinyl wherein said Het4 is optionally substituted with hydroxy-C1-4alkyl or C1-4alkyl-S(?O)2—C1-4alType: ApplicationFiled: July 12, 2007Publication date: February 4, 2010Inventors: Alexandra Papanikos, Freyne Eddy Jean Edgard, Peter Ten Holte, Marc Willems, Werner Constant Johan Embrechts, Laurence Anne Mevellec, Fierre-Henri Storck
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Publication number: 20100022522Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: August 27, 2009Publication date: January 28, 2010Inventors: James D. Rodgers, Stacey Shepard, Thomas P. Maduskuie, JR., Haisheng Wang, Nikoo Falahatpisheh, Maria Rafalski, Argyrios G. Arvanitis, Louis Storace, Ravikumar Jalluri, Jordan S. Fridman, Krishna Vaddi
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Publication number: 20090325945Abstract: The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc.Type: ApplicationFiled: April 26, 2007Publication date: December 31, 2009Inventors: Dan Niculescu-Duvaz, Caroline Joy Springer, Richard Malcolm Marais, Harmen Dijkstra, Delphine Menard, Ion Niculescu-Duvaz, Lawrence Davies, Arnaud Nourry
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Publication number: 20090324543Abstract: 2-amino-pyrido(3,2-d)pyrimidine derivatives with a specific substitution pattern on positions 4 and 6 of the core structure are useful in the treatment or prevention of an infection due to a virus from the Flaviviridae family, especially HCV, when administered to a patient in a therapeutically effective amount.Type: ApplicationFiled: December 24, 2007Publication date: December 31, 2009Applicant: Gilead Sciences, IncInventors: William John Watkins, Lee Shung Chong, Jennifer R. Zhang
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Publication number: 20090318425Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: June 23, 2009Publication date: December 24, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Edcon Chang, Stephen L. Gwaltney, Angie Vassar
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Patent number: 7625890Abstract: Invented are novel 1H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: GrantFiled: June 27, 2007Date of Patent: December 1, 2009Assignee: SmithKline Beecham Corp.Inventors: Dirk A. Heerding, Tammy J. Clark, Jack Dale Leber, Igor Safonov
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Patent number: 7618963Abstract: A bicyclic heteroaromatic compound according to general formula I, or a pharmaceutically acceptable salt thereof, wherein R1 is (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl or (4-13C)heteroaryl; all optionally substituted with one or more substituents; R2 is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (6-14C)aryl or (4-13C)heteroaryl; R3 is (1-8C)alkyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl or (4-13C)heteroaryl; Y is CH or N; Z is NH2 or OH; A is S, N(H), N(R), O or a bond and B is N(H), O or a bond; X1-X2 is C?C, C(O)—NH, NH—C(O), C(O)—O, O—C(O), C?N, N?C or S or O. The compounds of the invention can be used in fertility regulation therapies.Type: GrantFiled: April 23, 2007Date of Patent: November 17, 2009Assignee: N.V. OrganonInventors: Cornelis Marius Timmers, Willem Frederik Johan Karstens
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Publication number: 20090275534Abstract: The invention relates to pyrido[2,3-b]pyrazine compounds of general formulae (Ia) and (Ib), to their preparation and use, for example, for the treatment of malignant disorders and other disorders based on pathological cell proliferations.Type: ApplicationFiled: May 9, 2008Publication date: November 5, 2009Applicant: ZENTARIS GmbHInventors: Matthias Gerlach, Irene Seipelt, Eckhard Guenther, Emmanuel Polymeropoulos, Tilmann Schuster, Eckhard Claus
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Publication number: 20090275569Abstract: The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.Type: ApplicationFiled: September 9, 2008Publication date: November 5, 2009Inventors: Xianchang Gong, Kathy Barrett, Jianguo Cao, Colleen Gritzen, Glenn Noronha, John D. Hood, Chi Ching Mak, Andrew McPherson, Ved Prakash Pathak, Joel Renick, Richard M. Soll, Ute Splittgerber, Wolfgang Wrasidlo, Ningning Zhao, Elena Dneprovskaia, Binqi Zeng, Glenn Noronha
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Patent number: 7605155Abstract: In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: October 4, 2006Date of Patent: October 20, 2009Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Marc Labroli, Kartik M. Keertikar
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Publication number: 20090258857Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: ApplicationFiled: June 13, 2007Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
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Publication number: 20090258867Abstract: The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which R1 and R2 are the same or different and each an optionally substituted aryl group etc, R0 is hydrogen atom, an alkyl group etc, E is a group of the formula: —C(?O)— or —SO2—, R is a group of the following formula [i], [ii] or [iii] etc: Ring A is (a) a C3-8 cycloalkyl group optionally fused to a benzene ring or (b) a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom etc, R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group etc, one of RA and RB is an alkyl group etc, and the other is hydrogen atom, an alkyl group etc, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 4, 2007Publication date: October 15, 2009Inventors: Koichi Tanimoto, Mariko Oi, Yasunori Tsuboi, Yasunori Moritani
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Publication number: 20090239854Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: October 27, 2008Publication date: September 24, 2009Inventors: David T. HUNG, Andrew A. PROTTER, Rajendra P. JAIN, Sundeep DUGAR, Sarvajit CHAKRAVARTY, Sergey O. BACHURIN, Anatoly K. USTINOV, Bogdan K. BEZNOSKO, Elena F. SHEVTSOVA, Vladimir V. GRIGORIEV, Nadezhda Sergeevna Beznosko
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Publication number: 20090227571Abstract: Provided herein are compounds that bind to androgen receptors and modulate the activity and/or the amount of androgen receptors and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.Type: ApplicationFiled: June 30, 2006Publication date: September 10, 2009Inventors: Jon C. Loren, Todd Miller, Bijan Pedram, Charlene V. Rowley, Yixing Shen, Cornelis Arjan Van Oeveren, Lin Zhi
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Patent number: 7582627Abstract: Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R1 and R3 include alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclic, and heteroaryl; R5, R6, and R8 include H, alkyl, alkoxy, halo, NO2, CN, NH2, alkyl and dialkylamino; R7 includes hydrogen, alkyl, cycloalkyl, heterocyclic, fused heterocyclic, aryl and fused aryl; J and K are C or N; and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 13, 2006Date of Patent: September 1, 2009Assignee: Warner-Lambert CompanyInventors: Paul Bird, Edmund Lee Ellsworth, Dai Quoc Nguyen, Joseph Peter Sanchez, Howard Daniel Hollis Showalter, Rajeshwar Singh, Michael Andrew Stier, Tuan Phong Tran, Brian Morgan Watson, Judy Yip
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Publication number: 20090215746Abstract: There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.Type: ApplicationFiled: October 31, 2008Publication date: August 27, 2009Applicant: Takeda Pharmaceuticals Company LimitedInventors: Tsuneo Yasuma, Akira Mori, Masahiro Kawase, Hiroyuki Kimura, Masato Yoshida, Albert Charles Gyorkos, Scott Alan Pratt, Christopher Peter Corrette
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Publication number: 20090215750Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: February 20, 2009Publication date: August 27, 2009Inventors: Joe Timothy Bamberg, Mark Bartlett, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, Jaehyeon Park, David Bernard Smith, Michael Soth, Hanbiao Yang, Calvin Wesley Yee
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Publication number: 20090203673Abstract: The present invention encompasses compounds of general Formula (I) wherein X and R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: July 5, 2007Publication date: August 13, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald Engelhardt, Gerd Bader, Guido Boehmelt, Ralph Brueckner, Thomas Gerstberger, Maria Impagnatiello, Daniel Kuhn, Otmar Schaaf, Heinz Stadtmueller, Irene Waizenegger, Andreas Zoephel
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Publication number: 20090186875Abstract: Dihydrothienopyrimidines of formula 1 and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: ApplicationFiled: February 19, 2009Publication date: July 23, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christoph HOENKE, Birgit JUNG, Domnic MARTYRES, Peter NICKOLAUS, Pascale POUZET
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Publication number: 20090181959Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: June 12, 2008Publication date: July 16, 2009Applicant: INCYTE CORPORATIONInventors: James D. Rodgers, Stacey Shepard, Thomas P. Maduskuie, JR., Haisheng Wang, Nikoo Falahatpisheh, Maria Rafalski, Argyrios G. Arvanitis, Louis Storace, Ravi Kumar Jalluri, Jordan S. Fridman, Krishna Vaddi