The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/127)
-
Publication number: 20110319407Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: June 21, 2011Publication date: December 29, 2011Inventors: Wenge Xie, Brian Herbert, Richard A. Schumacher, Truc Minh Nguyen, Jianguo Ma, Carla Maria Gauss, Ashok Tehim
-
Publication number: 20110312957Abstract: The invention provides compounds of formula A or B which are useful in the treatment of a subject infected with HIV.Type: ApplicationFiled: September 15, 2009Publication date: December 22, 2011Applicant: CSIRInventors: Moira Leanne Bode, Amanda Louise Rousseau, David Gravestock, Simon Sana Moleele, Christiaan Wynand Van Der Westhuyzen
-
Publication number: 20110312959Abstract: The present invention relates to compounds of general formula I and use thereof as inhibitors of protein kinases AbI and Src and the method of production thereof. The present invention also relates to pharmaceutical compositions and medici-nal products comprising these compounds.Type: ApplicationFiled: February 12, 2010Publication date: December 22, 2011Inventors: Abdelaziz Yasri, Gwénaël Cheve, Cédric Bories, Louis Delon
-
Publication number: 20110311458Abstract: The present invention relates to alkaloid aminoester compounds which act as muscarinic receptor antagonists, processes for their preparation, compositions comprising them, and therapeutic uses thereof.Type: ApplicationFiled: June 22, 2011Publication date: December 22, 2011Applicant: Chiesi Farmaceutici S.p.A.Inventors: Gabriele AMARI, Mauro Riccaboni, Stefano Bossolo
-
Patent number: 8080547Abstract: The invention relates to the triazolopyridine carboxamide derivative and trizolopyrimidine carboxamide derivative of general Formula (I): Wherein X, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.Type: GrantFiled: October 6, 2009Date of Patent: December 20, 2011Assignee: Sanofi-AventisInventors: Luc Even, Christian Hoornaert
-
Patent number: 8080546Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, and in particular, p38 activity mediated inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, A5, R1, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of inflammatory diseases including rheumatoid arthritis, psoriasis and other disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: October 24, 2008Date of Patent: December 20, 2011Assignee: Amgen Inc.Inventors: Liping H. Pettus, Andrew Tasker, Shimin Xu, Ryan Wurz
-
Publication number: 20110306609Abstract: Provided herein are novel sirtuin-modulating compounds of Structural Formula (Ia) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: December 18, 2009Publication date: December 15, 2011Inventors: Christopher Oalmann, Jeremy S. Disch, Pui Yee Ng, Robert Perni
-
Publication number: 20110294806Abstract: This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: December 11, 2009Publication date: December 1, 2011Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Jiwei Qi, Yihan Wang, Feng Li, William C. Shakespeare, Anna Kohlmann, David C. Dalgarno, Xiaotian Zhu
-
Publication number: 20110294805Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R4, R5, R6 and Z are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: August 3, 2011Publication date: December 1, 2011Applicant: Amgen Inc.Inventors: Liping H. PETTUS, Andrew Tasker, Shimin Xu, Ryan Wurz
-
Publication number: 20110294779Abstract: The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.Type: ApplicationFiled: June 2, 2011Publication date: December 1, 2011Inventors: DANIELA ALBERATI, RUBÉN ALVAREZ SÁNCHEZ, KONRAD BLEICHER, ALEXANDER FLOHR, KATRIN GROEBKE ZBINDEN, MATTHIAS KOERNER, BERND KUHN, JENS-UWE PETERS, MARKUS RUDOLPH
-
Publication number: 20110294790Abstract: Bicyclic pyrazole and isoxazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases mediated by HSP90 protein, like cancer and neurodegenerative disorders.Type: ApplicationFiled: November 19, 2009Publication date: December 1, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Sergio Mantegani, Maria Gabriella Brasca, Francesco Casuscelli, Ron Ferguson, Helena Posteri, Carlo Visco, Elena Casale, Fabio Zuccotto
-
Publication number: 20110294809Abstract: The invention relates to tropane urea derivatives of general formula (I) and to the application thereof as modulators of the activity of 11?-hydroxysteroid dehydrogenose type 1 (11?HSD1).Type: ApplicationFiled: October 27, 2009Publication date: December 1, 2011Applicant: SANOFI-AVENTISInventors: Alain Jean Braun, Olivier Crespin, Eric Nicolai, Cecile Pascal, Olivier Venier
-
Publication number: 20110288090Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: January 25, 2010Publication date: November 24, 2011Inventors: Donna J. Armstrong, Yasuhiro Goto, Takashi Hashihayata, Tetsuya Kato, Michael J. Kelly, III, Mark E. Layton, Craig W. Lindsley, Yoshio Ogino, Yu Onozaki, Kenvin J. Rodzinak, Michael A. Rossi, Philip E. Sanderson, Jiabing Wang, Melissa M. Yaroschak
-
Publication number: 20110287937Abstract: Provided are 2-pyridone derivatives which have excellent herbicidal activity and exhibit high safety to useful crops and so on; salts thereof; and herbicides containing same. In more detail, 2-pyridone derivatives represented by general formula [I] or agrochemically acceptable salts thereof, and herbicides containing these compounds are provided. In general formula [I], X1 is an oxygen atom or a sulfur atom; X2, X3, and X4 are to each CH or N(O)m; m is an integer of 0 or 1; R1 is a hydrogen atom, a C1-12 alkyl group, or the like; R2 is a halogen atom, a cyano group, or the like; n is an integer of 0 to 4; R3 is a hydroxyl group, a halogen atom, or the like; A1 is C(R11R12); A2 is C(R13R14) or C?O; A3 is C(R15R16); and R11, R12, R13, R14, R15, and R16 are each independently a hydrogen atom or a C1-6 alkyl group.Type: ApplicationFiled: February 2, 2010Publication date: November 24, 2011Applicants: IHARA CHEMICAL INDUSTRY CO., LTD., KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Fumiaki Takabe, Yuuki Hirano, Akira Funyu, Masami Kobayashi, Takashi Mitsunari
-
Publication number: 20110288085Abstract: A compound of Formula (I) or Formula (II) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) or Formula (II), and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: June 18, 2009Publication date: November 24, 2011Inventors: John Hynes, George V. De Lucca, Hong Wu
-
Publication number: 20110288074Abstract: The present invention provides new compounds with high affinity for adenosine A2A receptors. It also provides antagonists of adenosine A2A receptors and their use as medicaments for the treatment and/or prophylaxis of diseases and disorders where the partial or total inactivation of adenosine A2A receptors signalling pathways could be beneficial such as Alzheimer's disease, Parkinson's disease, attention deficit and hyperactivity disorders (ADHD), Huntington's disease, neuroprotection, schizophrenia, anxiety and pain.Type: ApplicationFiled: January 25, 2010Publication date: November 24, 2011Applicant: DOMAIN THERAPEUTICSInventors: Stephan Schann, Stanislas Mayer
-
Publication number: 20110288054Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: September 22, 2009Publication date: November 24, 2011Applicant: Schering CorporationInventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K.C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
-
Publication number: 20110282056Abstract: Disclosed are compounds according to Formula I: wherein the variables are described herein.Type: ApplicationFiled: January 20, 2009Publication date: November 17, 2011Applicant: MERCK PATENT GMBHInventors: Benny C. Askew, Nadia Brugger, Ruoxi Lan, Amanda E. Sutton
-
Publication number: 20110281842Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, B, R1, R2, R3, R4a, R5, and Z are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora.Type: ApplicationFiled: May 12, 2011Publication date: November 17, 2011Applicant: ABBOTT LABORATORIESInventors: Michael R. Michaelides, Andrew S. Judd, Shannon R. Fix-Stenzel, Richard F. Clark, Bryan K. Sorensen, Zhiqin Ji
-
Publication number: 20110275595Abstract: The present invention relates to compounds defined by formula I wherein the groups R1, Y1 to Y4, V, W, and X are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: ApplicationFiled: October 22, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach
-
Publication number: 20110275628Abstract: Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HT2B receptor. The compound and salt are useful for treatment or prevention of various diseases and conditions associated with a 5-HT2B receptor.Type: ApplicationFiled: November 24, 2009Publication date: November 10, 2011Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Tadashi Inoue, Yuji Shishido, Hiroaki Ito
-
Publication number: 20110275627Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salt thereof, wherein X1 to X4, R1 to R4, A, B, D and m are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: August 25, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Todd Bosanac, Stephane De Lombaert, Ho Yin Lo, Peter Allen Nemoto, Alan Olague
-
Publication number: 20110269758Abstract: Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed Aurora kinases such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.Type: ApplicationFiled: June 29, 2009Publication date: November 3, 2011Applicant: MERCK PATENT GMBHInventors: Yufang Xiao, Bayard R. Huck, Amanda E. Sutton, Xiaoling Chen, Srinivasa R. Karra, Andreas Goutopoulos
-
Publication number: 20110269741Abstract: 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: March 28, 2011Publication date: November 3, 2011Applicant: Ardea Biosciences, Inc.Inventors: Huanming CHEN, Jianlin SONG, Jean-Michel VERNIER, Anthony B. PINKERTON, Johnny Y. NAGASAWA
-
Publication number: 20110269757Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: September 22, 2009Publication date: November 3, 2011Applicant: GENKYOTEX SAInventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
-
Patent number: 8048879Abstract: The present invention relates to substituted 4,5,6,7-tetrahydro-isoxazolo[4,5-c]pyridine compound corresponding to formula I, methods for producing them, to medicaments containing these compounds, the use of these compounds for producing medicaments and related treatment methodsType: GrantFiled: April 5, 2006Date of Patent: November 1, 2011Assignee: Gruenenthal GmbHInventors: Corinna Sundermann, Bernd Sundermann, Jörg Holenz, HagenHeinrich Hennies
-
Publication number: 20110263564Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: October 29, 2009Publication date: October 27, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Radha Narayan, Jeremy S. Disch, Robert B. Perni, Chi B. Vu
-
Publication number: 20110263594Abstract: The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.Type: ApplicationFiled: July 16, 2009Publication date: October 27, 2011Applicant: SANOFI-AVENTISInventors: Eric Bacque, Dominique Damour, Conception Nemecek, Patrick Nemecek, Sylvie Wentzler
-
Publication number: 20110257152Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.Type: ApplicationFiled: April 14, 2011Publication date: October 20, 2011Applicant: ABBOTT LABORATORIESInventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Yunsong Tong, Alan S. Florjancic
-
Publication number: 20110257156Abstract: In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: October 20, 2011Inventors: Zhaoning Zhu, William J. Greenlee, David James Cole, Dmitri A. Pissarnitski, Gioconda V. Gallo, Hongmei Li, Hubert B. Josien, Jun Qin, Chad E. Knutson, Mihirbaran Mandal, Monica L. Vicarel, Murali Rajagopalan, Pawan Kumar Dhondi, Ruo Xu, Zhong-Yue Sun, Thomas A. Bara, Xianhai Huang, Xiaohong Zhu, Zhiqiang Zhao, John W. Clader, Anandan Palani, Theodros Asberom, Troy McCracken, Chad E. Bennett
-
Publication number: 20110257171Abstract: The invention relates to the novel products of formula (I): in which: Ra is H, Hal, aryl or heteroaryl, which are optionally substituted; Rb is H, Rc, —COORc-CO-Rc or —CO—NRcRd; where Rc is alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd is H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.Type: ApplicationFiled: July 16, 2009Publication date: October 20, 2011Applicant: SANOFI-AVENTISInventors: Dominique Damour, Conception Nemecek, Patrick Nemecek, Sylvie Wentzler
-
Publication number: 20110257100Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.Type: ApplicationFiled: April 8, 2011Publication date: October 20, 2011Inventors: Stëphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frëdëric Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
-
Publication number: 20110257175Abstract: The invention provides new compounds and compositions thereof. The invention also provides methods for treating ophthalmic diseases, disorders and conditions.Type: ApplicationFiled: April 8, 2011Publication date: October 20, 2011Inventors: Stëphane Raeppel, Lijie Zhan, Stephen William Claridge, Franck Raeppel, Frëdëric Gaudette, Arkadii Vaisburg
-
Publication number: 20110251194Abstract: The disclosure concerns heterobicyclic compounds of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as enantiomers, diastereoisomers and mixtures thereof. Methods for preparing the compounds, pharmaceutical compositions, and methods of treatment also are disclosed.Type: ApplicationFiled: January 7, 2011Publication date: October 13, 2011Applicant: SANOFI-AVENTISInventors: Claude BERNHART, Gary MCCORT, Samir JEGHAM, Jean Marc HERBERT, Pierre CASELLAS, Monsif BOUABOULA, Olivier DUCLOS
-
Publication number: 20110251192Abstract: The present invention pertains to the field of pharmaceutical chemistry and discloses 8-(3-aminopropyl)-3-exo-8-azabicyclo[3.2.1]octane-3-amino amide compounds represented by formula I, the pharmaceutical compositions, the preparation method and the use thereof. Such compounds or pharmaceutically acceptable salts thereof can be used as an antagonist of CCR5 in preparing medicaments for treating diseases mediated by CCR5, particularly HIV infection, asthma, rheumatoid arthritis, autoimmune diseases and chronic obstructive pulmonary diseases (COPD).Type: ApplicationFiled: September 18, 2009Publication date: October 13, 2011Applicants: SHANGHAI TARGETDRUG CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Yaqiu Long, Xing Fan, Dongzhi Feng, Li Chen, Renhai Chen
-
Publication number: 20110245243Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.Type: ApplicationFiled: June 16, 2011Publication date: October 6, 2011Inventors: Hong LIU, David C. TULLY, Arnab CHATTERJEE, Phillip B. ALPER, David H. WOODMANSEE, Daniel MUTNICK
-
Publication number: 20110237580Abstract: The present invention is concerned with novel substituted bicyclic imidazole derivatives of Formula (I) wherein R0, R1, R3, R4, X, A1, A2, A3, A4, Y1, Y2 and Y3 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said novel compound as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: December 16, 2009Publication date: September 29, 2011Inventors: Henricus Jacobus Maria Gijsen, Gregor James MacDonald, François Paul Bischoff, Gary John Tresadern, Andrés Avelino Trabanco-Suárez, Sven Franciscus Anna Van Brandt, Didier Jean-Claude Berthelot
-
Patent number: 8026236Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: GrantFiled: January 13, 2010Date of Patent: September 27, 2011Assignee: N.V. OrganonInventors: John Stephen Robinson, Philip Stephen Jones, Jiaqiang Cai, David Jonathan Bennett
-
Patent number: 8022059Abstract: A compound of the formula: wherein ring X is benzene or pyridine; R1 is substituted alkyl; R2 is optionally substituted aryl or optionally substituted heterocyclic group; R3 is hydrogen or alkyl; R4 is hydrogen, halogen or alkyl; R5 is hydrogen or alkyl; R6 and R7 are the same or different and each hydrogen or halogen, or a pharmaceutically acceptable salt thereof, which is useful as IKur blocker effective for preventing or treating cardiac arrhythmia such as atrial fibrillation.Type: GrantFiled: September 26, 2008Date of Patent: September 20, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Tetsuo Yamaguchi, Hiroyuki Kawanishi, Hideki Ushirogochi, Tatsuyuki Takahashi, Tohru Takebe
-
Patent number: 8022206Abstract: Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET.Type: GrantFiled: February 6, 2009Date of Patent: September 20, 2011Assignee: OSI Pharmaceuticals, LLCInventors: An-Hu Li, Arno G. Steinig, Andrew Kleinberg, Qinghua Weng, Mark J. Mulvihill, Jing Wang, Xin Chen, Ti Wang, Hanqing Dong, Meizhong Jin
-
Publication number: 20110224191Abstract: Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Xin Chen, Melzhong Jin, Andrew Kleinberg, An-Hu Li, Mark J. Mulvihill, Arno G. Steinig, Jing Wang
-
Patent number: 8017605Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, 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: GrantFiled: June 10, 2009Date of Patent: September 13, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Soumya P. Sahoo, Meng-Hsin Chen, Kevin D. Dykstra, Hiroo Koyama, Peter T. Meinke, Stephen J. O'Keefe, Ginger Xu-qiang Yang
-
Publication number: 20110218197Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: ApplicationFiled: February 25, 2011Publication date: September 8, 2011Inventors: Mark R. PLAYER, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
-
Patent number: 8012966Abstract: The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8X, Y and have the meaning cited in the specification. Also disclosed are the pharmaceutical compositions containing the foregoing compounds, methods for the preparation and pharmaceutical use thereof, particularly as protein kinase inhibitors. Formula (I).Type: GrantFiled: January 24, 2007Date of Patent: September 6, 2011Assignee: Shanghai Hengrui Pharmaceutical Co., Ltd.Inventors: Peng Cho Tang, Yidong Su, Lei Zhang, Lu Xiao
-
Patent number: 8012956Abstract: A compound according to Formula I or II: wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: October 27, 2008Date of Patent: September 6, 2011Assignee: Exelixis, Inc.Inventors: Kenneth D. Rice, Naing Aay, Neel Kumar Anand, Arlyn Arcalas, Tae-Gon Baik, Charles M. Blazey, Owen Joseph Bowles, Chris A. Buhr, Joerg Bussenius, Simona Costanzo, Jeffrey Kimo Curtis, Steven Charles Defina, Larisa Dubenko, Abigail R. Kennedy, Angie Inyoung Kim, Katherine Lara, Sunghoon Ma, Jean-Claire Limun Manalo, Csaba J. Peto, Tsze H. Tsang, Longcheng Wang
-
Publication number: 20110212957Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: May 9, 2011Publication date: September 1, 2011Inventors: Wenge Xie, Brian Herbert, Truc Nguyen, Carla Gauss, Ashok Tehim
-
Publication number: 20110207711Abstract: The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.Type: ApplicationFiled: July 27, 2009Publication date: August 25, 2011Inventors: Jason Katz, James Jewell, Joon Jung, Solomon Kattar, Yongquan Hou, Rachel MacCoss, Satoru Ito
-
Publication number: 20110207732Abstract: Compounds of the formula (I), in which X1, X2, X3, X4, R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: September 24, 2009Publication date: August 25, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Timo Heinrich, Hannes Koolman
-
Publication number: 20110201608Abstract: The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 denotes a group A selected from among —O—R3, —NR3R4, —CR3R4R5, -(ethyne)-R3, —S—R3, —SO—R3 and SO2—R3 or R1 denotes a group B selected from among C6-10-aryl, five- to ten-membered, mono- or bicyclic heteroaryl with 1-3 heteroatoms selected independently of one another from among N, O and S; while this heteroaryl is linked to the structure according to formula 1 via either a C atom or an N atom, three- to ten-membered, mono- or bicyclic, saturated or partially saturated heterocyclic group with 1-3 heteroatoms selected independently of one another from among N, O and S, while this heterocyclic group is linked to the structure according to formula 1 via either a C atom or an N atom, and 5- to 11-membered spiro group which may optionally contain 1, 2 or 3 heteroatoms selected independently of one another frType: ApplicationFiled: July 23, 2009Publication date: August 18, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Hoffmann, Thierry Bouyssou, Georg Dahamnn, Harald Engelhardt, Dennis Fiegen, Sandra Handschum, Silke Hobbie, Takeshi Kono, Ulrich Reiser, Yayoi Sato, Andreas Schnapp, Annette Schuler-Metz
-
Publication number: 20110201604Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.Type: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Adnan M. M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta