The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/127)
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Publication number: 20140288064Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.Type: ApplicationFiled: June 6, 2014Publication date: September 25, 2014Applicant: WOCKHARDT LIMITEDInventors: Sachin BHAGWAT, Prasad Keshav DESHPANDE, Satish BHAWSAR, Vijaykumar Jagdishwar PATIL, Ravikumar TADIPARTHI, Shivaji Sampatrao PAWAR, Sunil Bhaginath JADHAV, Sanjay Kisan DABHADE, Vikas Vitthalrao DESHMUKH, Bharat DHOND, Satish BIRAJDAR, Mohammad Usman SHAIKH, Deepak DEKHANE, Piyush Ambalal PATEL
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Publication number: 20140288051Abstract: New bicyclic compounds, their preparation, and their use as antibacterial agents, either alone or in combination with an antibiotic for the treatment of infections caused by ?-lactamase-producing pathogenic bacteria, are described.Type: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Inventors: Samarendra N. MAlTI, Dai NGUYEN, Jehangir KHAN, Rong LING
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Publication number: 20140288043Abstract: A first aspect of the invention relates to a compound of formula (1A) or (1B), or a pharmaceutically acceptable salt thereof, Wherein R1 is a group selected from alkyl, monocyclic heterocycloalkyl, bicyclic heterocycloalkyl and cycloalkyl, each of which is optionally substituted, and wherein X1, X2, X3 and X4 are as defined herein. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (1A) and (1B).Type: ApplicationFiled: March 19, 2013Publication date: September 25, 2014Applicant: Genentech, Inc.Inventors: Bryan Chan, Anthony Estrada, Daniel Shore, Zachary Sweeney
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Patent number: 8841456Abstract: A 1,5-naphthyridine derivative represented by Formula [1] (in which R1, R2, R3, R4 and R5 represent a hydrogen atom, -L-Z (in which Z represents a non-aromatic heterocyclic group or the like; and L represents a single bond or the like), or the like, R6 represents -L-Z or the like, R7 and R8 represent a hydrogen atom or the like, and Q represents an oxygen atom or the like), or a salt thereof has an excellent inhibitory activity with respect to the PI3K-AKT pathway and the Ras-Raf-MEK-ERK pathway, and is useful for treatments such as prophylactic treatments and therapeutic treatments of diseases in which the PI3K-AKT pathway and the Ras-Raf-MEK-ERK pathway are involved.Type: GrantFiled: January 28, 2014Date of Patent: September 23, 2014Assignee: FUJIFILM CorporationInventors: Hidetomo Furuyama, Hideki Kurihara, Kentarou Furuya, Takahiro Terao, Shinichirou Sekine, Daisuke Nakagawa
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Publication number: 20140275061Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.Type: ApplicationFiled: October 12, 2012Publication date: September 18, 2014Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
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Publication number: 20140275026Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, and R5 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Inventors: Le Wang, John Pratt, Lisa A. Hasvold, Dachun Liu, Yujia Dai, Steven D. Fidanze, James H. Holms, Robert A. Mantei, Keith F. McDaniel, George S. Sheppard, William J. McClellan
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Publication number: 20140274926Abstract: The present invention provides compounds of Formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: IRM LLCInventors: Arnab Kumar CHATTERJEE, Fang LIANG, Casey Jacob Nelson MATHISON, Pranab Kumar MISHRA, Valentina MOLTENI, Advait Suresh NAGLE, Frantisek SUPEK, Liying Jocelyn TAN, Agnes VIDAL
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Publication number: 20140275018Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicant: WOCKHARDT LIMITEDInventors: Mahesh Vithalbhai PATEL, Prasad Keshav Deshpande, Satish Bhawasar, Sachin Bhagwat, Mohammad Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Snjeev Joshi
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Publication number: 20140275013Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicants: UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR COMMERCIALIZATION, IRM LLCInventors: Arnab Kumar CHATTERJEE, Fang LIANG, Casey Jacob Nelson MATHISON, Pranab Kumar MISHRA, Valentina MOLTENI, Advait Suresh Nagle, Frantisek SUPEK, Liying Jocelyn TAN, Agnes VIDAL, Michael Herman GELB, Frederick Simmons BUCKNER, Hari Babu TATIPAKA, Neil Richard NORCROSS, John Robert GILLESPIE
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Publication number: 20140275027Abstract: Disclosed are compounds of Formula (IIIa), wherein R1, R2, R3, X1, X2, X3, X4, X5, have any of the values defined therefore in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIIa).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Jianchun Gong, Zhi-Fu Tao, Thomas D. Penning, Andrew J. Souers, Yunsong Tong, Guidong Zhu
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Publication number: 20140275063Abstract: Compounds of formula (I) are inhibitors of Semicarbazide-sensitive amine oxidase R1—X—R2??(I) wherein R1, X and R2 are as defined in the claims.Type: ApplicationFiled: September 13, 2012Publication date: September 18, 2014Applicant: PROXIMAGEN LIMITEDInventors: Allison Carley, Iain Simpson
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Publication number: 20140275011Abstract: Disclosed are compound of Formula (Ia), wherein R2, R12, R16, J, Q, X, Y and Z are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (Ia).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: AbbVie Inc.Inventors: Anthony Mastracchio, Milan Bruncko, Chunqiu Lai, Julie M. Miyashiro, Zhi-Fu Tao, Keith W. Woods, Thomas D. Penning, Andrew J. Souers
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Publication number: 20140275040Abstract: The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Proximagen LimitedInventors: Max Espensen, Lee Patient, David Evans, Edward Savory, Iain Simpson
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Patent number: 8835431Abstract: Compounds of formula (I): wherein R2, W, A, Y, and R1 are as defined in the specification, and pharmaceutically acceptable salts thereof, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: GrantFiled: December 7, 2012Date of Patent: September 16, 2014Assignee: Chiesi Farmaceutici S.p.A.Inventors: Monique Bodil Van Niel, Nicholas Charles Ray, Andrew Peter Cridland, Christopher Hurley, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani
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Publication number: 20140256705Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: March 11, 2014Publication date: September 11, 2014Inventors: Lisa A. Hasvold, Dachun Liu, Keith F. McDaniel, John Pratt, George S. Sheppard, Carol K. Wada, Kevin R. Woller
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Publication number: 20140256658Abstract: The present invention describes antibiotic conjugates. These single drug entities are formed connecting one antibiotic with another antibiotic. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
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Publication number: 20140256704Abstract: The present invention relates to compounds according to Formulas I, IA or IB: to pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes.Type: ApplicationFiled: December 9, 2013Publication date: September 11, 2014Applicant: ARRIEN PHARMACEUTICALS LLCInventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy, Venu Babu Ganipisetty, Sureshkumar Talluri, Rajendra P. Appalaneni
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Publication number: 20140256713Abstract: The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: February 21, 2014Publication date: September 11, 2014Applicants: Shionogi & Co., Ltd., ViiV Healthcare CompanyInventors: Brian Alvin JOHNS, Eric Eugene BOROS, Takashi KAWASUJI, Cecilia S. KOBLE, Noriyuki KUROSE, Hitoshi MURAI, Ronald George SHERRILL, Jason Gordon WEATHERHEAD
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Publication number: 20140249148Abstract: Provided herein are inhibitors of HDAC3, as well as methods of treatment comprising administering those compounds to a subject in need thereof.Type: ApplicationFiled: January 31, 2014Publication date: September 4, 2014Inventors: John H. van Duzer, Ralph Mazitschek
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Publication number: 20140248240Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.Type: ApplicationFiled: September 2, 2011Publication date: September 4, 2014Inventors: Kenneth W. Bair, Timm Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Judith D. Kuntz, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
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Publication number: 20140243520Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: May 6, 2014Publication date: August 28, 2014Applicant: Array BioPharma Inc.Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
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Publication number: 20140243302Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.Type: ApplicationFiled: June 26, 2012Publication date: August 28, 2014Applicants: MERCK SHARP & DOHME CORPORATION, KYORIN PHARMACEUTICAL CO., LTD.Inventors: Yasumichi Fukuda, David E. Kaelin, JR., Sheo B. Singh
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Patent number: 8815854Abstract: The present invention relates to substituted imidazopyridinyl compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: June 21, 2012Date of Patent: August 26, 2014Assignee: 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, Takeshi Isoyama
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PYRROLO[2,3-b]PYRIDIN-4-YL-AMINES AND PYRROLO[2,3-b]PYRIMIDIN-5-YL-AMINES AS JANUS KINASE INHIBITORS
Publication number: 20140228346Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.Type: ApplicationFiled: April 17, 2014Publication date: August 14, 2014Applicant: Incyte CorporationInventors: James D. Rodgers, Haisheng Wang, Andrew P. Combs, Richard B. Sparks -
Publication number: 20140221341Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: ApplicationFiled: April 15, 2014Publication date: August 7, 2014Applicant: NAEJA PHARMACEUTICAL INC.Inventors: Samarendra N. MAITI, Dai NGUYEN, Jehangir KHAN, Rong LING
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Patent number: 8796257Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: GrantFiled: November 30, 2012Date of Patent: August 5, 2014Assignee: Naeja Pharmaceutical Inc.Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
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Publication number: 20140213554Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.Type: ApplicationFiled: December 20, 2013Publication date: July 31, 2014Inventors: Guoxian Wu, Katrina Chan, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Marika Nespi, Wayne Spevak, Ying Zhang
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Patent number: 8791113Abstract: The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.Type: GrantFiled: May 31, 2011Date of Patent: July 29, 2014Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Patent number: 8791256Abstract: There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R3, R4, R5, R6, Q, W, X, m, n and p are as described in the specification, process for preparing them, and their use as pharmaceuticals.Type: GrantFiled: June 5, 2013Date of Patent: July 29, 2014Assignee: Novartis AGInventors: Kamlesh Jagdis Bala, Catherine Leblanc, David Andrew Sandham, Katharine Louise Turner, Simon James Watson, Lyndon Nigel Brown, Brian Cox
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Publication number: 20140206679Abstract: The present invention relates to a heterocyclic pyridone compound represented by General Formula (I), where the heterocyclic pyridone compound is used as a tyrosine kinase inhibitor, and particularly a c-Met inhibitor. The present invention also relates to intermediates for preparing heterocyclic pyridone compound and a preparation method. The present invention further relates to a pharmaceutical composition containing the heterocyclic pyridone compound as an active ingredient, and a use of the pharmaceutical composition in treatment of diseases associated with tyrosine kinase c-Met, especially cancer associated with c-Met, as a medicament.Type: ApplicationFiled: May 28, 2012Publication date: July 24, 2014Applicant: SHANGHAI HUILUN LIFE SCIENCE & TECHNOLOGY CO., LTDInventors: Jianjun Cheng, Jihong Qin, Bin Ye
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Publication number: 20140206682Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of PDGFR (PDGFR?, PDGFR?) kinases or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.Type: ApplicationFiled: August 31, 2012Publication date: July 24, 2014Applicants: NOVARTIS PHARMACEUTICALS UK LIMITED, IRM LLCInventors: Fang Liang, Michael Gibney, Vince Yeh, Xiaolin Li, Valentina Molteni, Duncan Shaw, Ashley Mitchell Berman, Sarah Lewis, Jon Loren, Vikki Furminger
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Patent number: 8778977Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.Type: GrantFiled: July 2, 2007Date of Patent: July 15, 2014Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
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Publication number: 20140194420Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by formula: or a pharmaceutically acceptable salt thereof, wherein R4 is hydrogen, or substituted or unsubstituted alkyl, R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl or the like, with the proviso that R1, R2 and R3 are not simultaneously hydrogen, X is a single bond, —S—, —O—, —NR5—, —C(?O)— or the like, R5 is hydrogen, or substituted or unsubstituted alkyl, Y is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heterocyclyl or the like.Type: ApplicationFiled: July 13, 2012Publication date: July 10, 2014Applicant: Shionogi & Co., Ltd.Inventors: Eiichi Kojima, Keisuke Tonogaki, Nobuyuki Tanaka, Manabu Katou, Akira Ino, Masafumi Iwatsu, Masahiko Fujioka, Yu Hinata, Naoki Ohyabu
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Publication number: 20140187551Abstract: Compounds of the formula (I) in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed treatment of tumours.Type: ApplicationFiled: May 29, 2012Publication date: July 3, 2014Applicant: MERCK PATENT GMBHInventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
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Publication number: 20140187535Abstract: The disclosure relates to Substituted Benzimidazole-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable salts or solvates thereof, e.g., a pharmaceutically acceptable salt or solvate, wherein R1, R2, R3, Qa, W, U, A, B, Z, a, and the dashed lines are as defined herein, compositions comprising an effective amount of a Substituted Benzimidazole-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted Benzimidazole-Type Piperidine Compound.Type: ApplicationFiled: December 23, 2013Publication date: July 3, 2014Applicants: Shionogi & Co., Ltd., Purdue Pharma L.P.Inventors: Nobuyuki TANAKA, Kenji YAMAWAKI, Jiangchao YAO, Jianming YU, Xiaoming ZHOU
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Patent number: 8765743Abstract: The invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: GrantFiled: June 3, 2009Date of Patent: July 1, 2014Assignee: Glaxosmithkline Intellectual Property Development LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Patent number: 8765746Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A 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: GrantFiled: October 13, 2011Date of Patent: July 1, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
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Patent number: 8765747Abstract: The present application relates to therapeutic organic compounds of formula (I), wherein Q, R1, R2, R3, and R4 are defined herein. The invention also relates to pharmaceutical compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease such as cancer comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.Type: GrantFiled: June 14, 2010Date of Patent: July 1, 2014Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Hwan Geun Choi, Taebo Sim, Nathanael Gray, Wenjun Zhou, Jae Won Chang, Jianming Zhang, Ellen Weisberg
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Publication number: 20140179680Abstract: The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.Type: ApplicationFiled: December 18, 2013Publication date: June 26, 2014Inventors: Matthew P. Christopher, Francesc Xavier Fradera Llinas, Michelle Machacek, Michelle Martinez, Michael Hale Reutershan, Manami Shizuka, Binyuan Sun, Christopher Francis Thompson, B. Wesley Trotter, Matthew E. Voss, Michael D. Altman, Stephane L. Bogen, Ronald J. Doll
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Publication number: 20140179672Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations 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 for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: November 1, 2013Publication date: June 26, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Alexandros VAKALOPOULOS, Markus FOLLMANN, Ingo HARTUNG, Philipp BUCHGRABER, Rolf JAUTELAT, Jorma HAßFELD, Niels LINDNER, Alexey GROMOV, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva Maria BECKER-PELSTER, Andreas KNORR
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Publication number: 20140171429Abstract: The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, Formula (1) wherein R1, R2, R3, X, Y, Z, A, B, G1, m, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.Type: ApplicationFiled: January 20, 2012Publication date: June 19, 2014Applicant: ABBVIE INC.Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Zhongqiang Zhao, Dikun Chai, Leifu Yang, Yingxiang Gao, Marina Pliushchev
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Publication number: 20140171405Abstract: The present invention relates to fused pyrazole derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.Type: ApplicationFiled: December 18, 2013Publication date: June 19, 2014Applicant: Incyte CorporationInventors: Jincong Zhuo, Meizhong Xu, Ding-Quan Qian
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Publication number: 20140162971Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: March 14, 2013Publication date: June 12, 2014Inventors: Le WANG, John K PRATT, Keith F. McDANIEL, Yujia DAI, Steven D FIDANZE, Lisa HASVOLD, John H. Holms, Warren M. KATI, Dachun LIU, Robert A Mantei, William J. McCLELLAN, George S. SHEPPARD, Carol K. Wada
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Publication number: 20140155387Abstract: The present invention refers to: a compound having the general formula (I), wherein n is 0, 1, 2 or; m is 0, 1, 2 or 3; o is 0, 1, 2 or 3; W, X, Y and Z are independently selected from CH, N or N-oxide; A is NR4, C?O, C?S, OP(O)(O), P?O, CH2, or a heteroarly selected from the group consisting of (a), (b), (c), (d), (e), (f), (g); V is C?O, O, S, CH2, or NR5; as well as its use in treating inflammatory diseases such as asthma, COPD, inflammation post infection, arthritis, atherosclerosis, pain and dermatitis.Type: ApplicationFiled: April 20, 2012Publication date: June 5, 2014Applicants: QURIENT, CO. LTD., INSTITUT PASTEUR KOREAInventors: Zaesung No, Jaeseung Kim, Sung-Jun Han, Jung Hwan Kim, Young Sam Park, Sangchul Lee, Kiyean Nam, Jeongjun Kim, Jinhwa Lee, Sunhee Kang, Min Jung Seo, Saeyeon Lee, Gahee Choi
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Publication number: 20140155395Abstract: 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 4, 2014Publication date: June 5, 2014Applicant: Janssen Pharmaceutica, NVInventors: Mark R. Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
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Publication number: 20140155379Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.Type: ApplicationFiled: December 20, 2013Publication date: June 5, 2014Applicant: Ligand Pharmaceuticals IncorporatedInventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
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Publication number: 20140155393Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: ApplicationFiled: November 8, 2011Publication date: June 5, 2014Applicant: Janssen Pharmaceuticals, Inc.Inventors: José Maria Cid-Núñez, Andrés Avelino Trabanco-Suárez, Juan Antonio Vega Ramiro, Daniel Oehlrich, Gary John Tresadern, Gregor James Macdonald
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Publication number: 20140155375Abstract: The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase enzymes.Type: ApplicationFiled: June 8, 2012Publication date: June 5, 2014Applicant: GlaxoSmithKline Interllectual Property LimitedInventors: Deborah W. Chen, Sarah Duncan, Nigel Paul King, Kiew Ching Lee, Sing Yeung Mak, Dean Andrew Rivers
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Publication number: 20140155398Abstract: The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A? B, D, R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.Type: ApplicationFiled: November 22, 2013Publication date: June 5, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Ashwani Kumar Verma, Kumaragurubaran Nagaswamy, Lalima Sharma, Soma Ghosh, Balkrishna Ramchandra Kale, Aniruddha Mondal, Punit Kumar Srivastava, Sunanda Ghosh Dastidar, Rijwan Jaffer Momin, Pradip Balu Wagh, Sonali Nanasaheb Pansare, Pramod Raosaheb Markad, Yogesh Balasaheb Khairnar, Rie Miyauchi, Takeshi Murata, Masayuki Ishizaki, Masatoshi Nagamochi, Shin Iimura
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Publication number: 20140155594Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.Type: ApplicationFiled: April 24, 2013Publication date: June 5, 2014Applicant: Cancer Research Technology LimitedInventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Stanway