At Least Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/236)
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Publication number: 20110166123Abstract: Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.Type: ApplicationFiled: January 7, 2009Publication date: July 7, 2011Applicant: AARDEA BIOSCIENCES, INC.Inventors: Huanming Chen, Jianlin Song, Jean-Michel Vernier, Anthony B. Pinkerton, Johnny Y. Nagasawa
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Publication number: 20110166133Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Ros, KDR, FMS, C-FMS, FLT3, c-Kit, JAK2, JAK3, Aurora, PDGFR, Lck, TrkA, TrkB, TrkC, IGF-IR, ALK4, ALK5 and ALK or combinations thereof.Type: ApplicationFiled: May 7, 2009Publication date: July 7, 2011Applicant: IRM LLCInventors: Pamela A. Albaugh, Ha-Soon Choi, Gregory Chopiuk, Yi Fan, Paul Vincent Rucker, Zhicheng Wang
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Publication number: 20110152240Abstract: The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds.Type: ApplicationFiled: November 15, 2010Publication date: June 23, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Mustapha Haddach, Joe A. Tran, Fabrice Pierre, Collin F. Regan, Nicholas B. Raffaele, Suchitra Ravula, David M. Ryckman
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Patent number: 7964204Abstract: Disclosed are compounds of Formula (1), including all geometric and stereoisomers, N-oxides, and salts thereof, Formula (1): wherein A1, A2, A3, A4, A5 and A6 are independently, selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3; A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2. and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfo?yl, C1-C6 alkylamino, C2-G6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: GrantFiled: December 28, 2006Date of Patent: June 21, 2011Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
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Patent number: 7960369Abstract: The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.Type: GrantFiled: November 6, 2003Date of Patent: June 14, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Kohji Fukatsu, Shinobu Sasaki, Shuji Hinuma, Yasuaki Ito, Nobuhiro Suzuki, Masataka Harada, Tsuneo Yasuma
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Publication number: 20110124642Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring Z1, R1, p, R3, and R4 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: November 18, 2010Publication date: May 26, 2011Applicant: ABBOTT LABORATORIESInventors: Brian S. Brown, Tongmei Li, Arturo Perez-Medrano, Sridhar Peddi
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Patent number: 7947709Abstract: Compounds of formula I, wherein R1, R2, R3, X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.Type: GrantFiled: June 20, 2008Date of Patent: May 24, 2011Assignee: Roche Palo Alto LLCInventors: Todd Richard Elworthy, Joan Heather Hogg, Joshua Kennedy-Smith, Counde O'Yang, Mark Smith, Zachary Kevin Sweeney, Jeffrey Wu
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Publication number: 20110117073Abstract: The invention relates to protein conjugates that contain a protein kinase containg a cysteine residue in the ATP binding site and an inhibitor that is covalently and irreversibly bonded to said cysteine residue, such that the activity of the protein kinase is irreversibly inhibited. The invention also relates to compounds that irreversibly inhibit protein kinases.Type: ApplicationFiled: September 15, 2010Publication date: May 19, 2011Applicant: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Russell Colyn Petter, Deqiang Niu, Lixin Qiao, Arthur Kluge, Roy Lobb, Shomir Ghosh, Zhendong Zhu
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Publication number: 20110118221Abstract: The present invention relates to novel 1,4-diarylpyrimido[4,5-d]pyridazine-2,5-dione 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: April 24, 2009Publication date: May 19, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Franz Von Nussbaum, Dagmar Karthaus, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
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Publication number: 20110112079Abstract: The invention related to compounds for formula I useful for inhibiting phosphodiesterase-4.Type: ApplicationFiled: January 8, 2009Publication date: May 12, 2011Inventors: Craig J. Thomas, Menghang Xia, Amanda P. Skoumbourdis, Christopher A. LeClair, Ruili Huang, Martin J. Walsh
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Publication number: 20110105430Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (A) are inhibitors N of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.Type: ApplicationFiled: June 8, 2009Publication date: May 5, 2011Inventors: Soumya P. Sahoo, Meng-Hsin Chen, Kevin D. Dykstra, Hiroo Koyama, Peter T. Meinke, Stephen J. O'keefe, Ginger Xu-Qiang Yang
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Publication number: 20110105457Abstract: The purpose of the present invention is to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prevention/treatment of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. This was achieved by providing a substituted 2-amino-5,6-nitrogenated fused ring compound shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 16, 2009Publication date: May 5, 2011Inventors: Daisuke Taniyama, Kazuya Kano, Kazuya Okamoto, Masahiko Fujioka, Yasunori Mitsuoka
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Publication number: 20110098471Abstract: The present invention provides a novel antimicrobial drug comprising an oxazolidinone derivative of the formula (I): or a pharmaceutically acceptable salt or solvate thereof; wherein ring A is ring B is a benzene ring optionally substituted with lower alkyl; ring C is an optionally substituted six-membered heterocycle containing at least one nitrogen atom and one to three double bond(s) in the ling wherein the atom at the point of attachment to ring B is a carbon atom; ring D is an optionally substituted five-membered ring containing one or two double bond(s) in the ring; A1 and A2 are independently nitrogen or carbon; m is 0 or 1; R represents H, —NHC(?O)RA, —NHC(?S)RA, —NH-het1, —O-het1, —S-het1, —S(?O)-het1, —S(?O)2-het1, het2, —CONHRA, —OH, lower alkyl, lower alkoxy or lower alkenyl; and het1 and het2 are independently a heterocyclic group; with the proviso that the fused ring C-D is notType: ApplicationFiled: June 23, 2009Publication date: April 28, 2011Inventors: Issei Katoh, Toshiaki Aoki, Hideyuki Suzuki, Iwao Utsunomiya, Norikazu Kuroda, Tsutomu Iwaki
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Publication number: 20110092498Abstract: Compounds of the formula (I), in which R1, R2, R3, R3?, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 25, 2009Publication date: April 21, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
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Patent number: 7928106Abstract: The invention is concerned with novel aza-pyridopyrimidinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, X1, X2, X3, Y, Z, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used in treating or preventing diseases which are modulated by HM74A agonists.Type: GrantFiled: March 17, 2008Date of Patent: April 19, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Aurelia Conte, Henrietta Dehmlow, Uwe Grether, Nicole A. Kratochwil, Holger Kuehne, Robert Narquizian, Constantinos G. Panousis, Jens-Uwe Peters, Fabienne Ricklin
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Publication number: 20110082138Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: November 24, 2010Publication date: April 7, 2011Applicant: Daiichi Sankyo Company, LimitedInventors: Masami Ohtsuka, Noriyasu Haginoya, Masanori Ichikawa, Hironori Matsunaga, Hironao Saito, Yoshihiro Shibata, Tomoyuki Tsunemi
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Publication number: 20110082136Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: June 8, 2009Publication date: April 7, 2011Inventors: Michelle Machacek, Gabriela de Almeida, Jonathan B. Grimm, Rachel N. MacCoss, Eric Romeo, Tony Siu, Catherine White, Kevin Wilson
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Patent number: 7915258Abstract: The invention relates to compounds having the formula (I): Wherein R1, R2, R3 and R4 are as described herein. Also disclosed are the method of preparation and their use in therapy.Type: GrantFiled: May 19, 2009Date of Patent: March 29, 2011Assignee: Sanofi-AventisInventors: Christian Congy, Victor Dos Santos, Murielle Rinaldi-Carmona, Arnaud Rouquette, Didier Van Broeck
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Publication number: 20110071115Abstract: The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, infections, and certain immunological disorders.Type: ApplicationFiled: September 10, 2010Publication date: March 24, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: MUSTAPHA HADDACH, DAVID M. RYCKMAN, NICHOLAS RAFFAELE
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Publication number: 20110065714Abstract: This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.Type: ApplicationFiled: May 13, 2009Publication date: March 17, 2011Applicant: Shire LLCInventors: Bernard Golding, Peter Cicala, Richard Franklin, Kim Hirst
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Publication number: 20110065708Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: ApplicationFiled: August 19, 2010Publication date: March 17, 2011Applicant: NOVARTIS AGInventors: Miao DAI, Xingnian FU, Feng HE, Lei JIANG, Yue LI, Fang LIANG, Lei LIU, Yuan MI, Yao-chang XU, Guoliang XUN, Xiaoxia YAN, Zhengtian YU, Ji Yue ZHANG
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Publication number: 20110065711Abstract: This invention relates to novel substituted triazolo-pyridazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?1-GABAA receptor antagonist or an ?2- and/or an ?3-GABAA receptor partial agonist.Type: ApplicationFiled: June 22, 2010Publication date: March 17, 2011Applicant: CoNCERT Pharmaceuticals, Inc.Inventors: Scott L. Harbeson, Roger D. Tung, Julie F. Liu
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Patent number: 7906512Abstract: Methods for treating an allergic or inflammatory disease or other Syk-mediated disease or Syk-mediated condition characterized by administering a composition which contains a therapeutically effective amount of a 3,6-substituted imidazol[1,2-b]pyridazine compound.Type: GrantFiled: March 10, 2010Date of Patent: March 15, 2011Assignee: Alcon, Inc.Inventors: Mark R. Hellberg, Steven T. Miller, Andrew Rusinko
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Publication number: 20110059975Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A2 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.Type: ApplicationFiled: February 18, 2010Publication date: March 10, 2011Inventors: Joshua Kennedy-Smith, Wylie Solang Palmer, Zachary Kevin Sweeney
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Publication number: 20110053915Abstract: The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins.Type: ApplicationFiled: December 12, 2008Publication date: March 3, 2011Applicant: ALLA CHEM, LLCInventors: Andrey Alexandrovich Ivaschenko, Yan Vadimovich Lavrovsky, Sergey Viktorovich Malyarchuk, Ilya Matusovich Okun, Nikolay Filippovich Savchuk, Sergey Yevgenievich Tkachenko, Alexander Viktorovich Khvat, Alexander Vasilievich Ivaschenko
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Publication number: 20110053943Abstract: This invention relates to novel compounds of the invention 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: June 1, 2010Publication date: March 3, 2011Inventors: David A. Claremon, Colin M. Tice, Linghang Zhuang, Katerina Leftheris, Yuanjie Ye, Suresh B. Singh
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Publication number: 20110053892Abstract: Disclosed are compounds and compositions of Formula (I), pharmaceutically acceptable salts and solvates thereof, and their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses:Type: ApplicationFiled: August 30, 2010Publication date: March 3, 2011Inventors: Martin Leivers, John Miller
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Publication number: 20110052534Abstract: Disclosed are compounds and compositions of Formula (I), pharmaceutically acceptable salts and solvates thereof, and their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses:Type: ApplicationFiled: August 31, 2010Publication date: March 3, 2011Inventors: Martin Leivers, John Miller
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Publication number: 20110044943Abstract: Disclosed are compounds of Formula (I), pharmaceutically acceptable salts and solvates thereof, compositions thereof, and methods for their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses.Type: ApplicationFiled: July 11, 2008Publication date: February 24, 2011Inventors: Martin Robert Leivers, Jesse Daniel Keicher, Franz Ulrich Schmitz, Roopa Rai, Ryan Lauchli, Sebastian Reinhard Johannes Liehr, Stephanie Anna Chan, Tony Loc Ton
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Publication number: 20110046127Abstract: There is provided compounds of formula (I): wherein Z, M, R1, X, R3, R4 and R5 have meanings given in the description, an pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein kinase (e.g. a PIM family kinase or PI3-K) is desired and/or required, an particularly in the treatment of cancer.Type: ApplicationFiled: November 10, 2008Publication date: February 24, 2011Inventors: Paolo Pevarello, Ana Maria Garcia Collazo, Antonio Rodriguez Hergueta, Carl-Gustaf Pierre Saluste, Francisco Javier Ramos Lima, Esther Gonzalez Cantalapiedra, Julen Oyarzabal Santamarina
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Publication number: 20110044898Abstract: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.Type: ApplicationFiled: December 2, 2008Publication date: February 24, 2011Applicant: University of SydneyInventors: Michael Kassiou, Michelle Louise James, Christopher Andrew Luus
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Publication number: 20110039831Abstract: The invention relates to compounds of formula (I) and salts thereof wherein the substituents are as defined in the specification, the application of a compound of formula (I) in a process for the treatment of the human or animal body, in particular with regard to C-Met tyrosine kinase mediated disease; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner; processes for the preparation of a compound of formula (I).Type: ApplicationFiled: August 3, 2010Publication date: February 17, 2011Inventors: Pascal Furet, Clive McCarthy, Joseph Schoepfer, Stefan Stutz
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Publication number: 20110034468Abstract: Disclosed are triazolopyridine compounds of Formula (I), including pharmaceutically acceptable salts thereof. Also, disclosed are methods of using the compound in the treatment of obesity, dyslipidemia, diabetes and atherosclerosis, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 7, 2009Publication date: February 10, 2011Inventors: Yanting Huang, Chongqing Sun, R. Michael Lawrence, William R. Ewing, Huji Turdi
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Publication number: 20110034452Abstract: The invention relates to novel compounds of formula I where X, A?, Q1, Q2 Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: SANOFI-AVENTISInventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN
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Publication number: 20110034451Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: sanofi-aventisInventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN, Bodo SCHEIPER
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Publication number: 20110034456Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, R9, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: sanofi-aventisInventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN
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Publication number: 20110034467Abstract: The invention relates to novel dihydro-pyrrolopyridine, dihydro-pyrrolopyridazine and dihydro-pyrrolopyrimidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.Type: ApplicationFiled: May 25, 2007Publication date: February 10, 2011Inventors: Susanne Röhrig, Mario Jeske, Elisabeth Perzborn, Mark Jean Gnoth
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Patent number: 7884104Abstract: The present invention is directed to novel substituted aminopiperidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: September 27, 2005Date of Patent: February 8, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Jason M. Cox, Scott D. Edmondson, Bart Harper, Ann E. Weber
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Publication number: 20110021513Abstract: The present invention relates to modulators of IRAK kinase and provides compositions comprising such modulators, as well as methods therewith for treating conditions or diseases mediated by or associated with IRAK kinase.Type: ApplicationFiled: September 7, 2007Publication date: January 27, 2011Applicant: Biogen Idec Ma Inc.Inventors: Thomas Durand-Reville, Charles Jewell, Charles Hammond, Donovan Chin
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Publication number: 20110021521Abstract: The present invention relates to compounds that are sodium channel inhibitors 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 W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: July 26, 2010Publication date: January 27, 2011Applicant: Gilead Palo Alto, Inc.Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
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Patent number: 7875612Abstract: A cell population expressing folate receptors is selectively targeted with a non-peptide folic acid analogue. The non-peptide folic acid analogue is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.Type: GrantFiled: April 24, 2002Date of Patent: January 25, 2011Assignees: Purdue Research Foundation, Endocyte, Inc.Inventors: Mark A. Green, Chun-Yen Ke, Christopher P. Leamon
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Publication number: 20110015198Abstract: [Problem] To provide a melanin-concentrating hormone receptor antagonist useful as a pharmaceutical agent for central diseases, circulatory diseases, and metabolic diseases. [Means for Resolution] Provided is a diarylmethylamide derivative represented by formula (I): Wherein R1a, R1b, R2a, R2b, R3a, and R3b independently represent a hydrogen atom or the like, R4 represents a hydrogen atom, C1-6 alkyl, or the like, R5 represents a hydrogen atom or the like, Z represents C1-6 alkyl or the like, or R4 and Z together form a 4- to 6-membered nitrogen-containing hetero ring, Y1 represents H or the like, Y2 represents H, or Y1 and Y2 together form —O—CH2—, W represents C, SO, or the like, Ar1 represents 6-membered aryl or the like, Ar2 represents 6-membered aryl or the like, and ring A represents a benzene ring, a pyridine ring, or the like.Type: ApplicationFiled: March 26, 2009Publication date: January 20, 2011Inventors: Kaori Kamijo, Minoru Moriya, Takao Suzuki, Akihiro Takezawa
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Publication number: 20110009414Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise, for example, administering to a mammal in need thereof a compound of formula (II): where x, y, A, D, E, T, Q, G, Z, J, K, L, M, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (II) are also disclosed.Type: ApplicationFiled: May 6, 2009Publication date: January 13, 2011Applicant: Xenon Pharmaceuticals Inc.Inventors: Rajender Kamboj, Jian-min Fu, Vishnumurthy Kodumuru, Shifeng Liu, Kashinath Sadalapure, Nagasree Chakka, Duanjie Hou, Shaoyi Sun
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Patent number: 7868001Abstract: A compound of Formula I: Each variable is defined in the specification. This invention relates to a method of decreasing a level of a cytokine (e.g., TNF? or interlukine such as IL-1?) in a subject with a compound of Formula I. It also relates to a method of treating a disorder mediated by an overproduction of a cytokine with such a compound.Type: GrantFiled: November 2, 2007Date of Patent: January 11, 2011Assignee: Hutchison Medipharma Enterprises LimitedInventors: Wei Deng, Wei-Guo Su, Yu Cai, Jeff Duan
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Publication number: 20110003806Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
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Publication number: 20110003807Abstract: The present invention relates to a compound represented by the formula (I) or (I?): wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Hiroshi Banno, Masaaki Hirose, Osamu Kurasawa
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Publication number: 20100331333Abstract: This invention relates generally to imidazo[1,2-b]pyridazine-based modulators of Liver X receptors (LXRs) having formula (I) and related methods: wherein R2 is C6-C10 aryl or heteroaryl including 5-10 atoms, each of which is: (i) substituted with 1 R6, and (ii) optionally substituted with from 1-5 Re; and R1, R3, R4, R5, R6 and Re are defined herein.Type: ApplicationFiled: December 19, 2008Publication date: December 30, 2010Applicant: Wyeth LLCInventor: Robert Ray Singhaus, JR.
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Publication number: 20100331310Abstract: Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. wherein Q represents ethylene, etc., R1, R2 and R3 represent hydrogen, etc., X1 represents C1-6 alkylene, etc., X2 represents C1-6 alkylene, etc., A1 represents a 5- to 6-membered heterocyclic group, etc., and A2 represents C6-14 aryl, etc.Type: ApplicationFiled: February 9, 2009Publication date: December 30, 2010Inventors: Fumihiro Ozaki, Motohiro Soejima, Tasuku Ishida, Yoshihiko Norimine, Nobuyuki Kurusu, Eriko Doi, Toshihiko Kaneko, Daiju Hasegawa, Kiyoaki Kobayashi, Noboru Yamamoto
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Publication number: 20100323994Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: February 6, 2009Publication date: December 23, 2010Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Brian E. Fink, Soong-Hoon Kim, Yufen Zhao, Ping Chen, Wayne Vaccaro, Litai Zhang, Ashvinikumar V. Gaval, Dharmpal S. Dodd, Libing Chen
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Publication number: 20100324048Abstract: The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer.Type: ApplicationFiled: June 15, 2010Publication date: December 23, 2010Applicant: ELI LILLY AND COMPANYInventors: Philip Arthur Hipskind, Bharvin Kumar Patel, Takako Wilson (nee Takakuwa)