The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/362)
  • Publication number: 20110312959
    Abstract: 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: Application
    Filed: February 12, 2010
    Publication date: December 22, 2011
    Inventors: Abdelaziz Yasri, Gwénaël Cheve, Cédric Bories, Louis Delon
  • Patent number: 8080547
    Abstract: 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: Grant
    Filed: October 6, 2009
    Date of Patent: December 20, 2011
    Assignee: Sanofi-Aventis
    Inventors: Luc Even, Christian Hoornaert
  • Patent number: 8080546
    Abstract: 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: Grant
    Filed: October 24, 2008
    Date of Patent: December 20, 2011
    Assignee: Amgen Inc.
    Inventors: Liping H. Pettus, Andrew Tasker, Shimin Xu, Ryan Wurz
  • Publication number: 20110306609
    Abstract: 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: Application
    Filed: December 18, 2009
    Publication date: December 15, 2011
    Inventors: Christopher Oalmann, Jeremy S. Disch, Pui Yee Ng, Robert Perni
  • Patent number: 8071600
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Grant
    Filed: August 31, 2006
    Date of Patent: December 6, 2011
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
  • Patent number: 8071593
    Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.
    Type: Grant
    Filed: May 8, 2008
    Date of Patent: December 6, 2011
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
  • Patent number: 8071588
    Abstract: The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: December 6, 2011
    Assignee: Glaxo Group Limited
    Inventors: James Francis Callahan, Guoliang Lin, Zehong Wan, Hongxing Yan
  • Publication number: 20110294790
    Abstract: 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: Application
    Filed: November 19, 2009
    Publication date: December 1, 2011
    Applicant: 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: 20110294779
    Abstract: 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: Application
    Filed: June 2, 2011
    Publication date: December 1, 2011
    Inventors: DANIELA ALBERATI, RUBÉN ALVAREZ SÁNCHEZ, KONRAD BLEICHER, ALEXANDER FLOHR, KATRIN GROEBKE ZBINDEN, MATTHIAS KOERNER, BERND KUHN, JENS-UWE PETERS, MARKUS RUDOLPH
  • Publication number: 20110294777
    Abstract: Substituted bicyclic beta-lactams of Formula I: (I), are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.
    Type: Application
    Filed: January 15, 2009
    Publication date: December 1, 2011
    Inventors: Timothy A. Blizzard, Helen Chen, Candido Gude, Jeffrey D. Hermes, Jason Imbriglio, Seongkon Kim, Jane Y. Wu, Sookhee Ha, Christopher J. Mortko, Ian Mangion, Nelo Rivera, Rebecca T. Ruck, Michael Shevlin
  • Publication number: 20110294809
    Abstract: 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: Application
    Filed: October 27, 2009
    Publication date: December 1, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Alain Jean Braun, Olivier Crespin, Eric Nicolai, Cecile Pascal, Olivier Venier
  • Publication number: 20110294805
    Abstract: 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: Application
    Filed: August 3, 2011
    Publication date: December 1, 2011
    Applicant: Amgen Inc.
    Inventors: Liping H. PETTUS, Andrew Tasker, Shimin Xu, Ryan Wurz
  • Patent number: 8067408
    Abstract: The present invention is directed to novel compounds of Formula (I), pharmaceutical compositions and their use in therapy, for example as inhibitors of phosphodiesterase type IV (PDE4) and as antagonists of muscarinic acetylcholine receptors (mAChRs), in the treatment of/and or prophylaxis of respiratory diseases, including antiinflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: November 29, 2011
    Assignee: Glaxo Group Limited
    Inventors: James Francis Callahan, Guoliang Lin, Zehong Wan, Hongxing Yan
  • Publication number: 20110288074
    Abstract: 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: Application
    Filed: January 25, 2010
    Publication date: November 24, 2011
    Applicant: DOMAIN THERAPEUTICS
    Inventors: Stephan Schann, Stanislas Mayer
  • Publication number: 20110288054
    Abstract: 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: Application
    Filed: September 22, 2009
    Publication date: November 24, 2011
    Applicant: Schering Corporation
    Inventors: 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: 20110288077
    Abstract: This invention relates to compounds of the Formula (I)-(IX):, as defined 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-? combinations thereof.
    Type: Application
    Filed: September 22, 2009
    Publication date: November 24, 2011
    Applicant: SCHERING CORPORATION
    Inventors: Michael K.C. Wong, Wensheng Yu, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Joseph A. Kozlowski, Seong Heon Kim, Guowei Zhou, De-Yi Yang, Razia K. Rizvi, Lei Chen, Aneta Maria Kosinski, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Publication number: 20110281842
    Abstract: 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: Application
    Filed: May 12, 2011
    Publication date: November 17, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Michael R. Michaelides, Andrew S. Judd, Shannon R. Fix-Stenzel, Richard F. Clark, Bryan K. Sorensen, Zhiqin Ji
  • Publication number: 20110281888
    Abstract: Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.
    Type: Application
    Filed: May 16, 2011
    Publication date: November 17, 2011
    Inventors: Mark J. Mulvihill, Amo G. Steinig, Andrew Philip Crew, Meizhong Jin, Andrew Kleinberg, An-Hu Li, Jing Wang
  • Publication number: 20110275803
    Abstract: The invention provides a method for the synthesis of dehydrogenated lactam drugs of Formula I:
    Type: Application
    Filed: May 4, 2011
    Publication date: November 10, 2011
    Applicant: Alkermes, Inc.
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Publication number: 20110269768
    Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.
    Type: Application
    Filed: July 14, 2011
    Publication date: November 3, 2011
    Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
  • Publication number: 20110269746
    Abstract: Compounds exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof: wherein A is selected from among a 3- to 10-membered heterocyclyl group, B is selected from among an amino group, and X is selected from N and CH.
    Type: Application
    Filed: July 14, 2011
    Publication date: November 3, 2011
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Daigo Asano
  • Publication number: 20110269757
    Abstract: 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: Application
    Filed: September 22, 2009
    Publication date: November 3, 2011
    Applicant: GENKYOTEX SA
    Inventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
  • Patent number: 8048879
    Abstract: 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 methods
    Type: Grant
    Filed: April 5, 2006
    Date of Patent: November 1, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Corinna Sundermann, Bernd Sundermann, Jörg Holenz, HagenHeinrich Hennies
  • Publication number: 20110263592
    Abstract: Imidazo[1,2-?]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia, dyssomnia, parasomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Application
    Filed: August 14, 2008
    Publication date: October 27, 2011
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Yifeng Xiong, Konrad Feichtinger, Albert S. Ren, Brett Ullman
  • Publication number: 20110263610
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).
    Type: Application
    Filed: March 30, 2009
    Publication date: October 27, 2011
    Applicant: IRM LLC
    Inventors: Yongqin Wan, Shifeng Pan, Guobao Zhang, Xia Wang, Yun Feng Xie, Jiqing Jiang, Dean Phillips, Yang Yang
  • Publication number: 20110257156
    Abstract: 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: Application
    Filed: November 5, 2009
    Publication date: October 20, 2011
    Inventors: 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: 20110257175
    Abstract: The invention provides new compounds and compositions thereof. The invention also provides methods for treating ophthalmic diseases, disorders and conditions.
    Type: Application
    Filed: April 8, 2011
    Publication date: October 20, 2011
    Inventors: Stëphane Raeppel, Lijie Zhan, Stephen William Claridge, Franck Raeppel, Frëdëric Gaudette, Arkadii Vaisburg
  • Publication number: 20110257100
    Abstract: 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: Application
    Filed: April 8, 2011
    Publication date: October 20, 2011
    Inventors: Stëphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frëdëric Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
  • Publication number: 20110251212
    Abstract: A compound which specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist is provided. It has been found out that a piperazine derivative represented by the formula (I) binds specifically to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein R1 is each independently C1-C3 alkyl or the like, m is an integer of 0 to 4, X is —N(R4)—C(?O)—C(?O)—, —N(R4)—(CR5R6)p—C(?O)—, —N(R4)—C(?O)—(CR7R8)q— or —C(?O)—N(R4)—(CR7R8)q—, p and q are each independently an integer of 1 to 3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or lower alkyl, A1 is benzoxazolinone or the like, and A2 is optionally substituted phenyl or the like, or a pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: August 19, 2008
    Publication date: October 13, 2011
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Moriyasu Masui, Minoru Tomida, Naotake Kobayashi, Kousuke Anan, Aya Tazawa, Kayoko Hata
  • Publication number: 20110245267
    Abstract: The present invention relates to novel Piperidine and piperazine Derivatives, pharmaceutical compositions comprising the Piperidine and piperazine Derivatives and the use of these compounds of formula (I) for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Application
    Filed: December 18, 2009
    Publication date: October 6, 2011
    Applicant: Schering Plough Corporation
    Inventors: Dong Xiao, Anandan Palani, Robert G. Aslanian
  • Patent number: 8030311
    Abstract: The invention relates to compounds of the formula (I) wherein the moieties R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof, as well as their use, methods of use for them and method of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases.
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: October 4, 2011
    Assignee: Novartis AG
    Inventors: Guido Bold, Pascal Furet, Vito Guagnano, Clive McCarthy, Andrea Vaupel
  • Publication number: 20110237565
    Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
    Type: Application
    Filed: March 10, 2011
    Publication date: September 29, 2011
    Applicant: KALYPSYS, INC.
    Inventors: Allen Borchardt, Robert Davis, Stewart A. Noble
  • Patent number: 8022206
    Abstract: 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: Grant
    Filed: February 6, 2009
    Date of Patent: September 20, 2011
    Assignee: OSI Pharmaceuticals, LLC
    Inventors: 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: 20110224191
    Abstract: 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: Application
    Filed: November 19, 2009
    Publication date: September 15, 2011
    Inventors: Xin Chen, Melzhong Jin, Andrew Kleinberg, An-Hu Li, Mark J. Mulvihill, Arno G. Steinig, Jing Wang
  • Patent number: 8012956
    Abstract: 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: Grant
    Filed: October 27, 2008
    Date of Patent: September 6, 2011
    Assignee: 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: 20110212930
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Application
    Filed: May 5, 2011
    Publication date: September 1, 2011
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
  • Publication number: 20110207711
    Abstract: 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: Application
    Filed: July 27, 2009
    Publication date: August 25, 2011
    Inventors: Jason Katz, James Jewell, Joon Jung, Solomon Kattar, Yongquan Hou, Rachel MacCoss, Satoru Ito
  • Publication number: 20110207732
    Abstract: 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: Application
    Filed: September 24, 2009
    Publication date: August 25, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Timo Heinrich, Hannes Koolman
  • Publication number: 20110201608
    Abstract: 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 fr
    Type: Application
    Filed: July 23, 2009
    Publication date: August 18, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: 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
  • Patent number: 7998963
    Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein Ar is indolyl, indazolyl or dihydroindolyl, and R1, R2, R3 and R4 are as defined herein. Also provided are pharmaceutical compositions, methods of using the compounds in the treatment of depressive, anxiolytic and other disorders associated with inhibition of the reuptake of norepinephrine, serotonin, and dopamine, and methods of preparing the compounds.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: August 16, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: David Scott Carter, Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
  • Publication number: 20110195933
    Abstract: The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: July 27, 2009
    Publication date: August 11, 2011
    Inventors: Jason D. Katz, Sandra L. Knowles, James P. Jewell, David L. Sloman, Matthew G. Stanton, Njamkou Noucti
  • Patent number: 7994173
    Abstract: The present invention is concerned with novel compounds of formula (I) having fundic relaxating activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
    Type: Grant
    Filed: January 24, 2008
    Date of Patent: August 9, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans Eduard Janssens, Jerome Emile Georges Guillemont, Francois Maria Sommen, Jean-Francois Bonfanti
  • Publication number: 20110190260
    Abstract: [1,2,4]Triazolo[1,5-a]pyridine compounds are disclosed that have a formula represented by the formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.
    Type: Application
    Filed: July 24, 2009
    Publication date: August 4, 2011
    Inventors: Christel Jeanne Marie Menet, Nolwenn Jouannigot, Javier Blanc, Luc Juliaan Corina Van Rompaey, Stephen Robert Fletcher, Alastair James Hodges, Koen Kurt Smits
  • Publication number: 20110190290
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Application
    Filed: December 15, 2010
    Publication date: August 4, 2011
    Applicant: EPITHERIX, LLC
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Publication number: 20110178083
    Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.
    Type: Application
    Filed: July 9, 2009
    Publication date: July 21, 2011
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Publication number: 20110178082
    Abstract: 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: Application
    Filed: September 22, 2009
    Publication date: July 21, 2011
    Applicant: Genkyotex SA
    Inventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
  • Publication number: 20110178070
    Abstract: The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: June 23, 2009
    Publication date: July 21, 2011
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Xianchang Gong, Bohan Jin, Massaki Hirose, Feng Zhou, Qing Dong
  • Publication number: 20110178081
    Abstract: 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: Application
    Filed: September 22, 2009
    Publication date: July 21, 2011
    Applicant: Genkyotex SA
    Inventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
  • Publication number: 20110172203
    Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: December 29, 2010
    Publication date: July 14, 2011
    Applicant: ArQule, Inc.
    Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Yuko Yamamoto
  • Publication number: 20110172415
    Abstract: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.
    Type: Application
    Filed: March 17, 2011
    Publication date: July 14, 2011
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Moriyasu Masui, Makoto Adachi, Hidenori Mikamiyama, Akira Matsumura, Naoki Tsuno