Plural Ring Nitrogens In The Additional Hetero Ring (e.g., Imidazole, Pyrazine, Etc.) Patents (Class 514/235.8)
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Patent number: 7888351Abstract: The present invention relates to compounds of the formula; and their use in therapy.Type: GrantFiled: April 10, 2007Date of Patent: February 15, 2011Assignee: Novartis AGInventors: Daniel Kaspar Baeschlin, Garry Fenton, Kenji Namoto, Nils Ostermann, Richard Sedrani, Finton Sirockin
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Publication number: 20110034435Abstract: A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R1 is independently halogen, cyano, etc., each of X1, X2 and X3 is CR2 or nitrogen, R2 is independently hydrogens, etc., n is 0, 1, 2, 3 or 4; -D-Y is —O—CH2COOH, etc, and G is a substituted amino, a substituted heterocyclic group, etc, or a pharmaceutical acceptable salt thereof, has activities of opening BK channels.Type: ApplicationFiled: April 8, 2009Publication date: February 10, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Yasuyuki Tsuzuki, Miki Hirai
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Publication number: 20110034454Abstract: A compound of formula (I) or a salt, ester or prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme.Type: ApplicationFiled: January 8, 2007Publication date: February 10, 2011Inventors: Allan Paul Dishington, Shaun Michael Fillery, Maurice Raymond Verschoyle Finlay, Kurt Gordon Pike
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Publication number: 20110034449Abstract: N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.Type: ApplicationFiled: September 17, 2010Publication date: February 10, 2011Applicant: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpAInventors: Benedetta Crescenzi, Cristina Gardelli, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, Alessia Petrocchi, Marco Poma, Michael Rowley, Rita Scarpelli, Vincenzo Summa
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Publication number: 20110034433Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: December 9, 2008Publication date: February 10, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Jens Schamberger
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Patent number: 7884098Abstract: The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof; wherein R1, R1? R2, R3, R4, R5, r and s are as defined herein. Compounds of the present invention are useful in the treatment of diseases associated with Aurora kinase activity such as cancer.Type: GrantFiled: January 25, 2008Date of Patent: February 8, 2011Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Deborah L. Bryan, David Harold Drewry, Thomas H Faitg, Timothy Francis Gallagher, Neil W Johnson, Jiri Kasparec, Jeffrey M Ralph, Domingos J. Silva
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Patent number: 7879898Abstract: Methods are provided for treating chronic obstructive pulmonary diseases such as emphysema using compounds that activate the signaling pathways of hepatocyte growth factor.Type: GrantFiled: February 12, 2007Date of Patent: February 1, 2011Assignee: Angion Biomedica Corp.Inventor: Yanchun He
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Patent number: 7879853Abstract: The invention relates to novel pyrimidine derivatives of Formula (1) which are efficacious inhibitors of protein kinases, in particular of one or more isoforms of the protein kinase B/Akt.Type: GrantFiled: June 28, 2005Date of Patent: February 1, 2011Assignee: Bayer Schering Pharma AGInventors: Josef Stadlwieser, Thomas Baer, Thomas Maier, Thomas Beckers, Thomas Ciossek, Armin Zuelch, Ulrich Graedler
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Publication number: 20110021520Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.Type: ApplicationFiled: July 23, 2010Publication date: January 27, 2011Inventors: Sangamesh BADIGER, Murali CHEBROLU, Mathias FREDERIKSEN, Philipp HOLZER, Konstanze HURTH, Rainer Martin LUEOEND, Rainer MACHAUER, Henrik MOEBITZ, Ulf NEUMANN, Rita RAMOS, Heinrich RUEEGER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
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Publication number: 20110021505Abstract: The present invention relates to the use of sulfonyl-substituted 2-sulfonylaminobenzoic acid N-phenylamides of the formula I, wherein A and R1 to R6 have the meanings indicated in the claims, for treating pain and for manufacturing a medicament for the treatment of pain.Type: ApplicationFiled: March 30, 2010Publication date: January 27, 2011Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Karl RUDOLPHI, Martin MICHAELIS, Hans GUEHRING
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Publication number: 20110021525Abstract: The invention provides compounds and methods for inhibition of kinases, more specifically p70S6 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration, chemoinvasion and metabolism. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.Type: ApplicationFiled: July 20, 2010Publication date: January 27, 2011Applicant: EXELIXIS, INC.Inventors: Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew Tsuhako, John M. Nuss, Wei Xu
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Publication number: 20110021524Abstract: This invention provides a combination of ATP-competitive BCR-ABL inhibitor and a non-ATP competitive BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with BCR-ABL.Type: ApplicationFiled: December 18, 2008Publication date: January 27, 2011Applicant: IRM LLCInventors: Francisco Adrian, Christine Dierks, Nathanael S. Gray, Markus Warmuth
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Publication number: 20110020338Abstract: The invention relates to the use of compounds of formula (I) or (II) in the treatment of mammalian target of VEGF-driven angiogenic diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical preparations comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.Type: ApplicationFiled: March 24, 2009Publication date: January 27, 2011Inventor: Carlos Garcia-Echeverria
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Patent number: 7875610Abstract: The present invention relates to new dopamine D3 and D2 ligands of formula (I): wherein R1, R2 and Q are as described herein, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes for preparing the same, to compositions containing the same and to their use in the treatment and/or prevention of conditions which requires modulation of dopamine receptors.Type: GrantFiled: December 3, 2008Date of Patent: January 25, 2011Assignee: Richter Gedeon Nyrt.Inventors: Gizella Bartane Szalai, Eva Againe Csongor, Gyorgy Domany, Istvan Gyertyan, Bela Kiss, Judit Laszy, Katalin Saghy, Eva Schmidt, Sandor Farkas, Zsolt Komlodi
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Patent number: 7872005Abstract: This invention relates to compounds of formula (I): or pharmaceutically acceptable salts, solvate, clathrates hydrates or polymorphs thereof, their compositions and methods of use and methods of making thereof. The compounds (and compositions) are useful in modulating IL-12 production and processes mediated by IL-12.Type: GrantFiled: July 1, 2005Date of Patent: January 18, 2011Assignee: Synta Pharmaceuticals CorporationInventors: Lijun Sun, Zachary Demko, Yumiko Wada, Shijie Zhang
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Publication number: 20110009408Abstract: The invention concerns the generation of a three dimensional model of the six helix bundle (6HB) complexed with an inhibitor and the use of that model to identify, screen and/or develop inhibitors against viruses that use a class I fusion protein. Such inhibitors of viruses that use a class I fusion protein may be effective for treating, for example, respiratory infections by Respiratory Syncytial Virus (RSV).Type: ApplicationFiled: February 26, 2009Publication date: January 13, 2011Inventors: Dirk André Emmy Roymans, Hendrik Leon Augusta Jozef De Bondt, Eric Pierre Alexandre Arnoult, Herman Van Vlijmen, Jean-François Bonfanti
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Publication number: 20110005947Abstract: The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity.Type: ApplicationFiled: May 6, 2010Publication date: January 13, 2011Applicant: Portola Pharmaceuticals, Inc.Inventors: Shawn M. Bauer, Jack W. Rose, Yonghong Song, Qing Xu, Mukund Mehrotra, Wolin Huang, Anjali Pandey
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Publication number: 20110003813Abstract: Substituted biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: February 15, 2010Publication date: January 6, 2011Inventors: Charles A. Blum, Harry Brielmann, Bertrand L. Chenard, Xiaozhang Zheng
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Publication number: 20110003812Abstract: Magnesium salts/complexes of compounds useful for inhibiting the ADAM-IO protein and methods of making and purifying them are provided. Further provided are compositions comprising magnesium salts/complexes of the compounds in combination with a pharmaceutically acceptable carrier. The compounds well as such compositions comprising them are useful for the treatment of cancer, arthritis, diseases related to angiogenesis, such as renal diseases, heart diseases, such as heart failure, atherosclerosis, and stroke, inflammation, ulcer, infertility, scleroderma, endometriosis, mesothelioma, and diabetes. In addition, methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role are provided.Type: ApplicationFiled: October 15, 2008Publication date: January 6, 2011Applicant: SYMPHONY EVOLUTION, INC.Inventors: Sriram Naganathan, JoAnn Wilson, Daniel Dickman
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Publication number: 20110003814Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: September 8, 2010Publication date: January 6, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Dean Mitchell Wilson, Esther Martinborough, Timothy Donald Neubert, Andreas Peter Termin, Jesus E. Gonzalez, III, Nicole Zimmerman
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Publication number: 20100331328Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicyclylaryl-aryl-amines compounds of the following formula (referred to herein as BCAA compounds), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc.Type: ApplicationFiled: February 19, 2009Publication date: December 30, 2010Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Charles Reader, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Michael Cherry
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Publication number: 20100331329Abstract: The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Applicant: ASTRAZENECA ABInventors: Elaine Sophie Elizabeth Stokes, Craig Anthony Roberts, Michael James Waring
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Publication number: 20100329998Abstract: Described are novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are useful in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; ARDS; psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever. More particularly these compounds are useful as PDE4 inhibitors and are useful for treating PDE4 mediated diseases.Type: ApplicationFiled: January 30, 2009Publication date: December 30, 2010Inventors: Visweswara Akella Satya Surya Srinivas, Ravikumar Tadiparthi, Ganapavarapu Veera Raghava Sharma, Thirunavukkarasu Sappanimuthu, Durairaj Peter Bhakiaraj, Virendra Kachhadia, Kilambi Narasimhan, Sathya Narayana Thara, Sriram Rajagopal, Om Gaddam, Nishikanth Reddy Gaddam, Sukunath Narayanan, Venkatesan Parameswaran, Venkatesan Janarthanam, Maruthikumar Narayanam, Sathyanarayana Gadde, Uma Ramachandran, Gopalan Balasubramanian, Narayanan Surendran, Shridhar Narayanan, Lolaknath Santosh Vishwakarma, Sanjeev Saxena
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Publication number: 20100324032Abstract: Novel compounds, compositions, and kits are provided. Methods of modulating A? levels, and methods of treating a disease associated with aberrant A? levels are also provided.Type: ApplicationFiled: August 23, 2010Publication date: December 23, 2010Inventors: Soan Cheng, Daniel D. Comer, Long Mao, Guity P. Balow, David Pleynet
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Publication number: 20100322980Abstract: The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.Type: ApplicationFiled: August 25, 2010Publication date: December 23, 2010Inventors: Tai-wei Ly, Yuji Koriyama, Takashi Yoshino, Hiroki Sato, Kazuho Tanaka, Hiromi Sugimoto, Yoshihisa Manabe, Kevin Bacon, Klaus Urbahns, Masanori Seki, Takuya Shintani
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Publication number: 20100323020Abstract: A liquid pharmaceutical composition comprises an aqueous medium having suspended therein a solid particulate Bc1-2 family protein inhibitory compound such as ABT-263, having a D90 particle size not greater than about 3 ?m; wherein the aqueous medium further comprises at least one pharmaceutically acceptable surfactant and at least one pharmaceutically acceptable basifying agent such as sodium bicarbonate in amounts that are effective together to inhibit particle size increase. The composition is suitable for oral or parenteral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bc1-2 family proteins, for example cancer.Type: ApplicationFiled: June 17, 2010Publication date: December 23, 2010Applicant: ABBOTT LABORATORIESInventors: Rajeev Gokhale, Kennan C. Marsh, Yi Shi
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Publication number: 20100324045Abstract: This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih)1 (Ij), (Ik), (Il1-3). (Im1-3), (In1-3), (Io1-2), (Ip1-6), (Iq1-6), (Ir1-6) and (Is1-2), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.Type: ApplicationFiled: November 7, 2008Publication date: December 23, 2010Inventors: David A. Claremon, Linghang Zhuang, Colin M. Tice, Yuanjie Ye, Wei He, Suresh B. Singh, Zhenrong Xu, Salvacion Cacatian, Wei Zhao
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Patent number: 7855205Abstract: The present invention provides pyrimidinyl substituted fused-pyrrolyl compounds of Formula (I) and pharmaceutical compositions comprising the compounds and methods of synthesis and use thereof. The compounds are kinase inhibitors useful in treating or ameliorating a kinase mediated, angiogenesis-mediated or hyperproliferative disorder. The invention thus also provides a therapeutic or prophylactic method of use for the compounds and/or pharmaceutical compositions to treat such disorders.Type: GrantFiled: October 28, 2005Date of Patent: December 21, 2010Assignee: Janssen Pharmaceutica NVInventors: Shenlin Huang, Ronghua Li, Peter J. Connolly, Stuart L. Emanuel, Steven A. Middleton
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Patent number: 7851471Abstract: The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: GrantFiled: December 5, 2008Date of Patent: December 14, 2010Assignee: AstraZeneca AB (PUBL)Inventors: Joseph W. Boyd, Giles A. Brown, Michael Higginbottom
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Patent number: 7851466Abstract: This invention features pyrimidine compounds of formula (I): aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.Type: GrantFiled: November 18, 2005Date of Patent: December 14, 2010Assignee: Synta Pharmaceuticals Corp.Inventors: Yumiko Wada, Rongzhen Lu, Albert Y. Hsia
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Publication number: 20100311748Abstract: The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R2 or R3 is (Z).Type: ApplicationFiled: August 29, 2008Publication date: December 9, 2010Applicant: ASTRAZENECA ABInventors: Leslie Dakin, Benjamin Fauber, Alexander Hird, James Janetka, Daniel John Russell, Qibin Su, Bin Yang, Xiaolan Zheng
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Publication number: 20100311751Abstract: A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound, e.g., ABT-263, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.Type: ApplicationFiled: June 8, 2010Publication date: December 9, 2010Applicant: ABBOTT LABORATORIESInventors: Eric A. Schmitt, Ping Tong, Katherine Heemstra, Cristina M. Fischer, Huailiang Wu, Jonathan Mark Miller, Yanxia Li, Justin S. Lafountaine
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Publication number: 20100311749Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: A is C1-6alkyl, C3-6cycloalkyl, —CH2—R6, —CHMe-R7, —CMe2-R7, or optionally substituted aryl; wherein, when A is optionally substituted aryl, said aryl group is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of halogen, C1-6alkyl, —CF3, C1-4alkoxy, C1fluoroalkoxy, cyano, NR8R9, and pyridyl wherein the pyridyl is optionally substituted by one methyl; R1 is chlorine, fluorine, —CF3, cyano or C1-6alkyl; R2, R3 and R5 independently are hydrogen, fluorine, chlorine, —CF3, cyano or C1-6alkyl, such that at least one of R2, R3 and R5 is other than hydrogen; R4 is hydrogen. These compounds and salts are thought to be P2X7 receptor antagonists. The invention also provides for the treatment of pain, inflammation, rheumatoid arthritis, osteoarthritis, or a neurodegenerative disease.Type: ApplicationFiled: October 24, 2008Publication date: December 9, 2010Inventors: Laura Jane Chambers, Katharine Laura Collis, David Kenneth Dean, Jorge Munoz-Muriedas, Jon Graham Anthony Steadman, Daryl Simon Walter
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Publication number: 20100310563Abstract: Methods are provided for treating a subject with a cellular proliferative disorder that include administering to the subject a therapeutically effective amount of a JAK2 inhibitor and a therapeutically effective amount of a TNF-alpha inhibitor. In addition, methods are provided herein for determining if a subject with a cellular proliferative disorder would benefit from treatment with an agent that inhibits tumor necrosis factor (TNF)-alpha. Methods are also provided for identifying an agent of use in treating a subject with a cellular proliferative disorder or with a predisposition for cellular proliferative disorder. The methods include contacting an isolated cell expressing an activating mutation in the JAK2 protein with a test agent, and detecting the amount of tumor necrosis factor (TNF)-alpha produced by the cell.Type: ApplicationFiled: November 28, 2008Publication date: December 9, 2010Inventors: Thomas G.P. Bumm, Michael W.N. Deininger
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Publication number: 20100311730Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds of formula (I), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionisi?q radiation.Type: ApplicationFiled: October 6, 2008Publication date: December 9, 2010Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Charles Reader, Thomas Peter Matthews, Kwai Ming Cheung, Nicolas Proisy, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Glynn Jonathan Addison, Michael Cherry
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Publication number: 20100311750Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: ApplicationFiled: December 1, 2008Publication date: December 9, 2010Inventors: Muneto Mogi, Toshio Kawanami, Ken Yamada, Kayo Yasoshima, Hidetomo Imase, Takahiro Miyake, Osamu Ohmori
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Publication number: 20100305128Abstract: The present invention provides novel pyrimidinyl-thiophene kinase modulators and methods of using the novel pyrimidinyl-thiophene kinase modulators to treat diseases mediated by kinase activity.Type: ApplicationFiled: August 6, 2010Publication date: December 2, 2010Inventors: William D. Arnold, Chixu Chen, Stefan N. Gradl, Stephanie A. Hopkins, Ruo W. Steensma, Masaki Tomimoto, Mark E. Wilson
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Publication number: 20100305088Abstract: This invention is directed to a 3-(amido or sulphamido)-4-(4-substituted-azinyl)benzamide or benzsulphonamide compound as defined herein. The 3-(amido or sulphamido)-(4-substituted-azinyl)benzamide or benzsulphonamide compound is useful as a inhibitor of the chemokine receptor CxCR3, and for preventing or treating a CxCR3 chemokine receptor mediated disease or condition related thereto in a patient in need of such.Type: ApplicationFiled: August 6, 2010Publication date: December 2, 2010Applicant: SANOFI-AVENTISInventors: David S. Thorpe, Martin Smrcina, Dagmar D. Cabel
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Publication number: 20100305125Abstract: ABT-263 bis-HCl and crystalline polymorphs thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.Type: ApplicationFiled: April 29, 2010Publication date: December 2, 2010Inventors: Thomas Borchardt, Paul Brackemeyer, Nathaniel Catron, Rodger Henry, Xiaochun Lou, Matthew Ravn, Geoff G.Z. Zhang, Deliang Zhou
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Publication number: 20100305126Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G1, R2, R3, R4, R5, n, p, q, Ar1, and Ar2 are defined in the description. The present invention relates also to methods of making said compounds, and compositions comprising said compounds which are useful for inhibiting kinases such as IGF-1R.Type: ApplicationFiled: May 26, 2010Publication date: December 2, 2010Applicant: ABBOTT LABORATORIESInventors: Richard F. Clark, Randy L. Bell, Nwe Y. Ba-maung, Scott A. Erickson, Steve D. Fidanze, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang, Jieyi Wang
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Publication number: 20100305127Abstract: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.Type: ApplicationFiled: August 4, 2010Publication date: December 2, 2010Applicant: GLAXO GROUP LIMITEDInventors: Alan David Borthwick, Deirdre Mary Bernadette Hickey, John Liddle, Andrew McMurtrie Mason
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Patent number: 7842693Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: December 9, 2003Date of Patent: November 30, 2010Assignee: ChemoCentryx, Inc.Inventors: Andrew M. K. Pennell, James B. Aggen, J. J. Kim Wright, Subhabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi, Valeri V. Martichonok
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Publication number: 20100298323Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: June 3, 2010Publication date: November 25, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
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Publication number: 20100298326Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a? and I-A.a? in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: December 28, 2007Publication date: November 25, 2010Inventors: Andreas Kling, Wilfried Hornberger, Helmut Mack, Achim Moeller, Volker Nimmrich, Dietmar Seemann, Wilfried Lubisch
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Publication number: 20100298312Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.Type: ApplicationFiled: September 3, 2008Publication date: November 25, 2010Applicant: The Scripps Research InstituteInventors: Theodore M. Kamenecka, Rong Jiang, Xinyi Song, Philip LoGrasso, Michael D. Cameron, Derek R. Duckett
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Publication number: 20100298299Abstract: The present invention relates to new non-peptide derivatives of formula (I), wherein R1-R5, Q and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.Type: ApplicationFiled: October 27, 2007Publication date: November 25, 2010Inventors: Istvan Vago, Sandor Farkas, Katalin Hornok, Gyula Beke, Eva Bozo, Monika Vastag, Eva Szentirmay, Gyorgy Keseru, Eva Schmidt
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Publication number: 20100297194Abstract: An orally deliverable pharmaceutical composition comprises as a sole or first active ingredient a compound of Formula I defined herein or a pharmaceutically acceptable salt thereof, for example ABT-263 free base or ABT-263 bis-HCl salt, dispersed, in a free base equivalent amount of at least about 2.5% by weight of the composition, in a pharmaceutically acceptable carrier; wherein said active ingredient is in solid-state form and/or the composition further comprises, dispersed in the carrier, a pharmaceutically acceptable heavier-chalcogen antioxidant in an amount effective to inhibit oxidation of the active ingredient at a thioether linkage thereof. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.Type: ApplicationFiled: April 29, 2010Publication date: November 25, 2010Inventors: Nathaniel Catron, Michael G. Fickes, Cristina M. Fischer, Rajeev Gokhale, Anthony R. Haight, Katherine Heemstra, David Hill, Martin Knobloch, Drazen Kostelac, Justin S. Lafountaine, Yanxia Li, Bernd Liepold, Kennan Marsh, Jonathan M. Miller, Claudia Packhaeuser, Yeshwant D. Sanzgiri, Eric A. Schmitt, Yi Shi, Norbert Steiger, Ping Tong, Huailiang Wu, Geoff G.Z. Zhang, Deliang Zhou
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Patent number: 7838525Abstract: The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.Type: GrantFiled: November 21, 2006Date of Patent: November 23, 2010Assignee: Arena Pharmaceuticals, Inc.Inventors: Robert M. Jones, Graem Semple, Yifeng Xiong, Young-Jun Shin, Albert S. Ren, Imelda Calderon, Beatriz Fioravanti, Jin Sun Karoline Choi, Juerg Lehmann, Marc A. Bruce
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Patent number: 7838522Abstract: The present invention is related to macrogol glyceride pharmaceutical formulations containing benzothiazole derivatives. In particular, the invention is related to benzothiazole stearoyl macrogol pharmaceutical formulations, method of preparation and use thereof.Type: GrantFiled: November 16, 2005Date of Patent: November 23, 2010Assignee: Ares Trading S.A.Inventors: Pierandrea Esposito, Daniela Chicco, Luca Donati, Andrea Leonardi, Stefania Bertero, Jean-Pierre Gotteland, Pascale Gaillard, Isabelle Jeanclaude-Etter, Simone Grandolini, Mario Maio
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Patent number: 7838524Abstract: The present invention relates to compounds of formula (I), pharmaceutical compositions which contain them and methods for treating cancer using compounds of formula (I).Type: GrantFiled: May 2, 2005Date of Patent: November 23, 2010Assignee: Bayer Healthcare LLCInventors: Wendy Lee, Gaetan Ladouceur, Jacques Dumas, Roger Smith, Shihong Ying, Gan Wang, Zhi Chen, Qingjie Liu, Holia Hatoum Mokdad