Four Or More Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/118)
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Publication number: 20100311721Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: March 4, 2008Publication date: December 9, 2010Applicant: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Guido Boehmelt, Harald Engelhardt, Ulrich Hirt, Otmar Schaaf, Irene Waizenegger
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Publication number: 20100305117Abstract: The invention provides 4,6-di- and 2,4,6-tri-substituted pteridine derivatives with a specific substitution pattern which exhibit a significant and selective activity against certain types of viral infections, in particular selectively inhibit replication of Flaviridae such as the hepatitis C virus, and are useful for the prevention and treatment of such viral infections.Type: ApplicationFiled: July 20, 2007Publication date: December 2, 2010Applicant: Gilead Sciences, Inc.Inventors: Piet André Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe, William John Watkins, Lee Shun Chong
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Publication number: 20100298300Abstract: Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.Type: ApplicationFiled: March 8, 2009Publication date: November 25, 2010Inventors: Martin James Inglis Andrews, Paul Edwards, Mark Stuart Chambers, Wolfgang Schmidt, Juha Andrew Clase, Gregory Bar, Kim Louise Hirst, Angus MacLeod
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Publication number: 20100298557Abstract: Disclosed is a novel compound having Syk and/or Abl inhibitory activities, which is useful for prevention/treatment of allergic diseases, autoimmune diseases, arthritides and cancers. Specifically disclosed is a pyrazolopyrimidine compound represented by the formula [I] or [III] below, a tautomer thereof, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a solvent of any of them.Type: ApplicationFiled: December 28, 2007Publication date: November 25, 2010Applicant: Taisho Pharmaceutical Co., LtdInventors: Makoto Yagi, Hiroki Umemiya, Hajime Asanuma, Yusuke Oka, Rie Nishikawa, Keisi Hayashi, Takumi Okada, Takanori Shimizu, Shigetada Sasako
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Publication number: 20100298319Abstract: The present invention relates to purine compounds that are useful as kinase inhibitors. More particularly, the present invention relates to purine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative conditions or disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative conditions or disorders including tumours and cancers as well as other disorders or conditions related to or associated with PI3 and/or mTOR kinases.Type: ApplicationFiled: October 3, 2008Publication date: November 25, 2010Applicant: S*BIO Pte Ltd.Inventors: Harish Kumar Mysore Nagaraj, Meredith Williams
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Publication number: 20100298315Abstract: The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.Type: ApplicationFiled: January 26, 2010Publication date: November 25, 2010Applicant: sanofi-aventisInventors: Eva ALBERT, Eric BACQUE, Conception NEMECEK, Antonio UGOLINI, Sylvie WENTZLER
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Publication number: 20100286126Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: ApplicationFiled: April 19, 2007Publication date: November 11, 2010Applicant: NOVARTIS AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20100273757Abstract: The present invention provides a compound of formula (I) wherein: A represents an optionally substituted monocyclic or polycyclic aryl or heteroaryl group B represents an optionally substituted monocyclic nitrogen-containing heteroaryl group; and either a) R1 and R2 represent hydrogen or specified substituents, or b) R2, R1 and the —NH— group to which R1 is attached, form a moiety selected from the moiety of formulae (IIa) and (IIb): (IIa) These compounds are useful as antagonists of the A2B receptor, for instance in the treatment of asthma.Type: ApplicationFiled: June 4, 2010Publication date: October 28, 2010Inventors: Bernat Vidal Juan, Cristina Esteve Trias, Lidia Soca Pueyo, Paul Robert Eastwood
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Publication number: 20100273780Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: ApplicationFiled: April 19, 2010Publication date: October 28, 2010Applicant: PGXHEALTH, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Patent number: 7816350Abstract: The present invention relates to a compound of formula I, or a pharmaceutically acceptable acid salt thereof. The invention further relates to the use of such compounds in the treatment of hyperproliferative skin disorders, viral infections, cancer, rheumatoid arthritis, lupus, type I diabetes, multiple sclerosis, restenosis, polycystic kidney disease, graft rejection, graft versus host disease and gout, or for psoriasis, parasitoses such as those caused by fungi or protists, or Alzheimer's disease. Further aspects of the invention relate to the use of such compounds in the inhibition of cell proliferation, in the induction of apoptosis, to modulate the activity of adrenergic and/or purinergic receptors or to suppress immunostimulation. The invention also relates to the use of 2,6,9-trisubstituted 8-azapurines in maintaining mammalian ooctyes at the germinal vesicle stage.Type: GrantFiled: February 4, 2005Date of Patent: October 19, 2010Assignees: Institute of Experimental Botany ASCR, Univerzita Palackeho v OlomouciInventors: Kveta Fuksova, Libor Havlicek, Vladimir Krystof, Rene Lenobel, Miroslav Strnad
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Publication number: 20100256118Abstract: A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.Type: ApplicationFiled: June 3, 2010Publication date: October 7, 2010Applicant: Dainippon Sumitomo Pharma Co.,Ltd.Inventors: Yoshiaki ISOBE, Haruo Takaku, Haruhisa Ogita, Masanori Tobe, Ayumu Kurimoto, Tetsuhiro Ogino, Hitoshi Fujita
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Publication number: 20100249067Abstract: The invention relates to compounds of Formula (I), a polymorph, an enantiomer, a stereoisomer, a solvate, an N-oxide derivative, or a pharmaceutically acceptable salt thereof: Formula (I), which have inhibitory effect on one or more protein kinases that are involved in cell mitosis.Type: ApplicationFiled: January 30, 2008Publication date: September 30, 2010Applicant: Biogen Idec MA Inc.Inventors: Srinivas Rao Kasibhatla, Kevin Hong, Lin Zhang, Marcus F. Boehm, Junhua Fan, Jean-Yves LeBrazidec
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Publication number: 20100249099Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.Type: ApplicationFiled: March 26, 2010Publication date: September 30, 2010Applicant: Pathway Therapeutics LimitedInventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
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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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Patent number: 7799781Abstract: The present invention relates to compounds that inhibit HSP90 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as for treatment of solid tumors.Type: GrantFiled: January 31, 2008Date of Patent: September 21, 2010Assignee: AstraZeneca ABInventor: Thorsten Nowak
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Patent number: 7786299Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.Type: GrantFiled: September 6, 2005Date of Patent: August 31, 2010Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Matthias Hoffmann, Matthias Grauert, Martin Steegmaier, Anke Baum, Jens Jurgen Quant, Flavio Solca, Florian Colbatzky
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Publication number: 20100216781Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: ApplicationFiled: October 26, 2009Publication date: August 26, 2010Inventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Lida Tehrani, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Weiming Xu, Loui Madakamutil, Kimberly Fultz, Rama K. Narla, Sabita Sankar, Jan Elsner
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Publication number: 20100216788Abstract: The present invention provides a compound represented by the formula: wherein R1a is a hydrogen atom, R2a is a C1-6 alkyl group substituted by a group represented by —NR6a—CO—(CH2)n—SO2— optionally halogenated C1-4 alkyl wherein n is an integer of 1 to 4, R6a is a hydrogen atom or a C1-4 alkyl group, and —(CH2)n— is optionally substituted by C1-4 alkyl, R3a is a hydrogen atom or a C1-6 alkyl group, R4a is a halogen atom or a C1-6 alkyl group, R5a is a halogen atom or a C1-6 alkyl group, and Xa is a hydrogen atom or a halogen atom, or a salt thereof. The compound of the present invention has a superior tyrosine kinase inhibitory action, is highly safe, and is sufficiently satisfactory as a pharmaceutical product.Type: ApplicationFiled: December 1, 2006Publication date: August 26, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Tomoyasu Ishikawa, Kazuhiro Miwa, Masaki Seto, Hiroshi Banno, Youichi Kawakita
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Patent number: 7781432Abstract: Analogs or derivatives of nitrobenzylthioinosine corresponding to formula I: in which R represents an unsubstituted or mono- or polysubstituted phenyl, benzyl or heteroaryl group or a phenyl group condensed with heteroaryl, and R? represents an unsubstituted or mono- or polysubstituted NH—C1-6-alkyl, NH-aryl, NH-heteroaryl, NH—C3-8-cycloalkyl, NH—C1-3-alkyl-aryl, NH—C1-3-alkyl-heteroaryl, N(C1-6-alkyl)2, N(C1-3-alkyl-aryl)2, N(C1-3-alkyl-heteroaryl)2, piperidine, piperazine, morpholine or pyrrolidine group; pharmaceutical compositions comprising such analogs or derivatives, and the use of such analogs or derivatives for treating pain and/or various other diseases.Type: GrantFiled: December 29, 2006Date of Patent: August 24, 2010Assignees: Gruenenthal GmbH, Leiden UniversityInventors: Adriaan Pieter Ijzermann, Reynier Tromp
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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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Patent number: 7772231Abstract: Compounds of formula (25) that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: GrantFiled: December 28, 2006Date of Patent: August 10, 2010Assignee: Abbott LaboratoriesInventors: George S. Sheppard, Gary T. Wang, Fabio Palazzo, Randy L Bell, Robert A. Mantei, Jieyi Wang, Robert D. Hubbard, Megumi Kawai, Scott A. Erickson, Nwe BaMaung, Steve D. Fidanze
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Publication number: 20100197683Abstract: Provided is a novel compound represented by the following formula Wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor ? agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.Type: ApplicationFiled: January 29, 2010Publication date: August 5, 2010Inventors: Tsuyoshi Maekawa, Hideyuki Igawa
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Publication number: 20100197684Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: February 9, 2010Publication date: August 5, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
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Publication number: 20100190784Abstract: A compound of formula (I), or stereoisomers or pharmaceutically acceptable salts thereof, wherein, R1a, R1b, R2a, R2b, U1, U2, X1, X2 and L are as defined herein.Type: ApplicationFiled: April 19, 2007Publication date: July 29, 2010Inventors: Robin Alec Fairhurst, Roger John Taylor
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Publication number: 20100190774Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.Type: ApplicationFiled: April 8, 2010Publication date: July 29, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: David J. Lauffer, Alexander Aronov, Pan Li, David D. Deininger, Kira McGinty, Dean Stamos, Jon H. Come, Michelle Stewart
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Publication number: 20100190749Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.Type: ApplicationFiled: September 17, 2009Publication date: July 29, 2010Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
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Publication number: 20100190787Abstract: The invention relates to compounds of Formula (I), a prodrug, a polymorph, a tautomer, an enantiomer, a stereoisomer, a solvate, an N-oxide, or a pharmaceutically acceptable salt thereof: (formula should be inserted here) which have inhibitory effect on one or more protein kinases that are involved in cell mitosis.Type: ApplicationFiled: January 30, 2008Publication date: July 29, 2010Inventors: Srinivas Rao Kasibhatla, Kevin Hong, Lin Zhang, Marcus F. Boehm, Junhua Fan, Jean-Yves LeBrazidec
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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: 20100184760Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.Type: ApplicationFiled: September 17, 2009Publication date: July 22, 2010Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
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Patent number: 7759485Abstract: Disclosed are processes for preparing dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and in the specification.Type: GrantFiled: August 4, 2005Date of Patent: July 20, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Guenter Linz, Gerd F. Kraemer, Ludwig Gutschera, Geert Asche
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Publication number: 20100179128Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficialType: ApplicationFiled: August 8, 2006Publication date: July 15, 2010Inventors: Richard Jonathan Daniel Hatley, Jag Paul Heer, John Liddle, Andrew McMurtrie Mason, Ivan Leo Pinto, Shahzad Sharooq Rahman, Ian Edward David Smith
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Patent number: 7754728Abstract: A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.Type: GrantFiled: September 26, 2003Date of Patent: July 13, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Yoshiaki Isobe, Haruo Takaku, Haruhisa Ogita, Masanori Tobe, Ayumu Kurimoto, Tetsuhiro Ogino, Hitoshi Fujita
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Publication number: 20100160313Abstract: The present invention relates in general to anti-cancer drug design. More specifically, the invention provides methods of mapping and screening for anti-cancer agents using pharmacophore models. The invention demonstrates that, conformational sampling of a small lead molecule, followed by representative pharmacophore model development, is an efficient approach for rational design of novel anticancer agents with similar or better potency than the original lead but with different physicochemical properties.Type: ApplicationFiled: October 22, 2009Publication date: June 24, 2010Applicant: University of Southern CaliforniaInventors: Nouri NEAMATI, Jinxia Deng
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Publication number: 20100160311Abstract: The present invention relates to azolopyrimidines of the formula I in which the substituents are defined according to the description, to processes and intermediates for preparing these compounds, to compositions comprising them and to their use for controlling phytopathogenic harmful fungi.Type: ApplicationFiled: July 5, 2007Publication date: June 24, 2010Applicant: BASF SEInventors: Jochen Dietz, Wassilios Grammenos, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Marianna Vrettou
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Publication number: 20100143301Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: December 7, 2009Publication date: June 10, 2010Applicant: Gilead Sciences, Inc.Inventors: Manoj C. Desai, Randall L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan Mc Fadden, Paul A. Roethle, Hong Yang
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Publication number: 20100144663Abstract: The present invention provides 2,6-dinitrogen-containing substituted purine compounds of formula (A) or salts or solvates thereof or the solvates of salts thereof, as well as pharmaceutical compositions containing such compounds. The compounds of the present invention have the characteristics of lower toxicity, broad anticancer spectrum, higher anticancer activity, good stability and the like. The compounds are useful for the manufacture of an antitumor medicament. The present invention also provides a process for preparing these compounds.Type: ApplicationFiled: April 17, 2008Publication date: June 10, 2010Inventors: Zhanggui Wu, Weidong Ye, Jianyong Yuan, Gang Chen
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Publication number: 20100144705Abstract: Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same.Type: ApplicationFiled: December 5, 2008Publication date: June 10, 2010Applicant: Principia Biopharma Inc.Inventor: Richard MILLER
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Publication number: 20100137585Abstract: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.Type: ApplicationFiled: January 15, 2010Publication date: June 3, 2010Inventors: Masahiko Hayakawa, Hiroyuki Kaizawa, Hiroyuki Moritomo, Ken-Ichi Kawaguchi, Tomonobu Koizumi, Mayumi Yamano, Koyo Matsuda, Minoru Okada, Mitsuaki Ohta
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Publication number: 20100130492Abstract: There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: wherein R1, R2, R3, R4, Ra, Rb, Rc, and X each have the same meaning as defined in the specification.Type: ApplicationFiled: October 14, 2009Publication date: May 27, 2010Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kiyoshi Nakayama, Kazuyuki Sugita, Masaki Setoguchi, Yuichi Tominaga, Masanori Saitou, Takashi Odagiri
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Publication number: 20100130491Abstract: The present invention provides compounds of formula (I) wherein R1, Y1, X1, L and R2 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: March 19, 2008Publication date: May 27, 2010Inventors: Roger Victor Bonnert, Thomas Mcinally, Stephen Thom
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Patent number: 7723319Abstract: The present invention relates to an acyclic nucleoside phosphonate derivative which is useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable salts, stereoisomers, and a process for the preparation thereof.Type: GrantFiled: September 9, 2009Date of Patent: May 25, 2010Assignee: LG Life Sciences Ltd.Inventors: Dong-Gyu Cho, Jae-Hong Lim, Jae-Taeg Hwang, Woo-Young Cho, Hyun-Sook Jang, Chang-Ho Lee, Tae-Saeng Choi, Chung-Mi Kim, Yong-Zu Kim, Tae-Kyun Kim, Seung-Joo Cho, Gyoung-Won Kim, Jong-Ryoo Choi, Jeong-Min Kim, Kee-Yoon Roh
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Patent number: 7718654Abstract: The invention relates to new pteridine compounds of formula 1 wherein R1, R2 , R3 and R4 have the meanings given herein, which are useful 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. The invention further relates to pharmaceutical compositions which contain these compounds.Type: GrantFiled: November 18, 2005Date of Patent: May 18, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Domnic Martyres, Horst Dollinger, Birgit Jung, Peter Nickolaus
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Publication number: 20100120739Abstract: The present disclosure relates to triazolopyridazine protein kinase modulators of Formula (I), methods of using these compounds to treat diseases mediated by kinase activity.Type: ApplicationFiled: October 18, 2007Publication date: May 13, 2010Inventors: Christopher Ronald Smith, Pierre- Yves Bounaud, Elizabeth Anne Jefferson, Patrick S. Lee, Eduardo Torres
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Publication number: 20100120765Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: ApplicationFiled: July 22, 2009Publication date: May 13, 2010Applicant: PGXHEALTH, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Publication number: 20100113441Abstract: The invention relates to substituted imidazopyrimidines and triazolopyrimidines, to methods for the production thereof, and to the use of same for producing medicaments for the treatment and/or prophylaxis of diseases, especially haematological diseases, preferably leucopenia and neutropenia.Type: ApplicationFiled: March 4, 2008Publication date: May 6, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Stephan Siegel, Andreas Wilmen, Susanne Röhrig, Niels Svenstrup, Mark Jean Gnoth, Stefan Heitmeier, Ulrich Rester, Dmitry Zubov, Jochen Strayle, Michael Sperzel
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Patent number: 7700768Abstract: Novel substituted pyrimido[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: GrantFiled: October 11, 2007Date of Patent: April 20, 2010Assignee: GlaxoSmithKline LLCInventors: Jerry L. Adams, Jeffrey C. Boehm, John J. Taggart, Ralph F. Hall
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Publication number: 20100069369Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.Type: ApplicationFiled: September 1, 2009Publication date: March 18, 2010Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
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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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Patent number: 7674789Abstract: The present invention is directed to compounds of formula (I), (Ia),(Ic) and (Id), compositions, and uses thereof as an inhibitor of the p38 kinase, and wherein, inter alia R1 is C(Z)N(R10?)(CR10R20)vRb, C(Z)O(CR10R20)vRb, N(R10?)C(Z)(CR10R20)vRb; N(R10?)C(Z)N(R10?)(CR10R20)vRb; or N(R10?)OC(Z)(CR10R20)vRb; R3 is C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroarylC1-10 alkyl, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted; X is R2, OR2?, S(O)mR2?, (CH2)n?N(R10?)S(O)mR2?, (CH2)n?N(R10?)C(O)R2?, (CH2)n?NR4R14, (CH2)n?N(R2 ?)(R2?), or N(R10?)—Rh—NH—C(?N—CN)NRqRq?; and R2 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic, or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties, excluding hydrogen, may be optionally substituted; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 24, 2006Date of Patent: March 9, 2010Assignee: Glaxo Group LimitedInventors: James F. Callahan, Zehong Wan, Hongxing Yan, Xichen Lin