Additional Hetero Ring Attached Directly Or Indirectly To The Four-membered Hetero Ring By Nonionic Bonding Patents (Class 514/210.18)
  • NAMPT INHIBITORS
    Publication number: 20130303511
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Applicant: AbbVie Inc.
    Inventors: Richard F. Clark, Bryan Sorensen, Augustine T. Osuma, Robin Frey, Kenton Longenecker, George Doherty, Michael L. Curtin, Michael R. Michaelides, Ramzi F. Sweis, Marina A. Pliushchev, Andy Judd, Todd M. Hansen, Howard R. Heyman
  • NOVEL TRIAZINE COMPOUNDS
    Publication number: 20130303516
    Abstract: The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.
    Type: Application
    Filed: January 25, 2012
    Publication date: November 14, 2013
    Inventors: Sundeep Dugar, Dinesh Mahajan, Chandraban Rhushikesh Deokar, Peter Frank Hollinger, Kamal Kishore Kapoor
  • 2-METHOXY-PYRIDIN-4-YL-DERIVATIVES
    Publication number: 20130303514
    Abstract: The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, and R4 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
    Type: Application
    Filed: January 18, 2012
    Publication date: November 14, 2013
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Martin Bolli, Cyrille Lescop, Boris Mathys, Keith Morrison, Claus Mueller, Oliver Nayler, Beat Steiner
  • QUINOXALINES AND AZA-QUINOXALINES AS CRTH2 RECEPTOR MODULATORS
    Publication number: 20130303517
    Abstract: The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Application
    Filed: December 19, 2011
    Publication date: November 14, 2013
    Inventors: Christopher W. Boyce, Sylvia Joanna Degrado, Xiao Chen, Jun Qin, Robert D. Mazzola, JR., Younong Yu, Kevin D. McCormick, Anandan Palani, Dong Xiao, Robert George Aslanian, Jie Wu, Ashwin Umesh Rao, Phieng Siliphaivanh, Joey L. Methot, Hongjun Zhang, Elizabeth Helen Kelley, William Colby Brown, Qin Jiang, Jolicia Polivina Gauuan, Andrew J. Leyhane, Purakkattle Johny Biju, Pawan K. Dhondi, Li Dong, Salem Fevrier, Xianhai Huang, Henry M. Vaccaro
  • NOVEL AZETIDINE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS
    Publication number: 20130303513
    Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: June 28, 2013
    Publication date: November 14, 2013
    Applicant: Allergan, Inc.
    Inventors: Wenkui K. Fang, Evelyn G. Corpuz, Wha-Bin Im, Ken Chow, Liming Wang
  • NAMPT INHIBITORS
    Publication number: 20130303509
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Applicant: ABBVIE INC.
    Inventors: Todd M. Hansen, Kenton Longenecker, Howard R. Heyman, Michael L. Curtin, Richard F. Clark, Bryan Sorensen, Zhiqin Ji, Kevin Woller, George Doherty, Robin Frey
  • NAMPT INHIBITORS
    Publication number: 20130303508
    Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
    Type: Application
    Filed: May 10, 2013
    Publication date: November 14, 2013
    Applicant: ABBVIE INC.
    Inventors: Richard F. Clark, Bryan Sorensen, Augustine T. Osuma, Robin Frey, Kenton Longenecker, George Doherty, Michael L. Curtin, Michael R. Michaelides, Ramzi F. Sweis, Marina A. Pliushchev, Andy Judd, Todd M. Hansen, Howard R. Heyman
  • QUINOLINES AND AZA-QUINOLINES AS CRTH2 RECEPTOR MODULATORS
    Publication number: 20130296300
    Abstract: The invention provides certain quinolines and aza-quinolines of the Formula (I), and their pharmaceutically acceptable salts, wherein E, J1, Ja, Jb, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Application
    Filed: December 19, 2011
    Publication date: November 7, 2013
    Inventors: Christopher W. Boyce, Salem Fevrier, Kevin D. McCormick, Anandan Palani, Robert G. Aslanian, Phieng Siliphaivanh, Joey L. Methot, William Colby Brown, Henry Vaccaro
  • HETEROAROMATIC AND AROMATIC PIPERAZINYL AZETIDINYL AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
    Publication number: 20130296297
    Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, W and are defined herein.
    Type: Application
    Filed: March 19, 2013
    Publication date: November 7, 2013
    Inventors: Chris Flores, Marina Nelen, Erica Nulton, Stephen Prouty, Matthew Todd, Sui-Po Zhang
  • 2-Carboxamide-7-Piperazinyl-Benzofuran Derivatives
    Publication number: 20130296296
    Abstract: The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted; R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocyclyl, C1-4alkylheterocyclyl, heterocyclyl-heteroaryl, aryl-heterocyclyl, carbocyclyl-heteroaryl, heterocyclyl-aryl, optionally substituted; R3 is hydrogen or C1-4alkyl, or R2 and R3 may together with the nitrogen atom, form a saturated ring system containing 4, 5 or 6 ring forming atoms, and optionally substituted; R4 is hydrogen, halogen, methyl or methoxy; to pharmaceutical composition containing said compounds and to the use of said compounds in therapy, for instance in treating cognitive disorders. The present invention further relates to new intermediates useful in the preparation thereof.
    Type: Application
    Filed: February 4, 2013
    Publication date: November 7, 2013
    Inventor: ASTRAZENECA AB
  • LINKED DIBENZIMIDAZOLE ANTIVIRALS
    Publication number: 20130295049
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: October 30, 2012
    Publication date: November 7, 2013
    Applicant: ENANTA PHARMACEUTICALS, INC
    Inventor: ENANTA PHARMACEUTICALS, INC
  • COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
    Publication number: 20130296318
    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 kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
    Type: Application
    Filed: June 28, 2013
    Publication date: November 7, 2013
    Inventors: Shenlin Huang, Xianming Jin, Zuosheng Liu, Daniel Poon, John Tellew, Yongqin Wan, Xing Wang, Yongping Xie
  • TRIAZOLOPYRIDAZINE COMPOUNDS, USE AS INHIBITORS OF THE KINASE LRRK2, AND METHODS FOR PREPARATION THEREOF
    Publication number: 20130296298
    Abstract: The present invention provides novel LRRK2 kinase inhibitors and methods of treating disease states using these inhibitors.
    Type: Application
    Filed: May 2, 2013
    Publication date: November 7, 2013
    Applicants: THE UAB RESEARCH FOUNDATION, Southern Research Institute
    Inventors: Robert A. Galemmo, JR., Andrew B. West, Joseph A. Maddry, Subramaniam Ananthan, Ashish Kumar Pathak, Jacob Valiyaveettil
  • PYRROLO[2,3-b]PYRIDIN-4-YL-AMINES AND PYRROLO[2,3-b]PYRIMIDIN-5-YL-AMINES AS JANUS KINASE INHIBITORS
    Publication number: 20130296299
    Abstract: 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: Application
    Filed: May 8, 2013
    Publication date: November 7, 2013
    Inventors: James D. Rodgers, Haisheng Wang, Andrew P. Combs, Richard B. Sparks
  • Amino-pyrrolidine-azetidine diamides as monoacylglycerol lipase inhibitors
    Patent number: 8575363
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R1, and R2 are defined herein.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: November 5, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Yue-Mei Zhang, Peter J. Connolly, Shu-Chen Lin, Mark J. MacIelag
  • Combination therapy in treatment of oncological and fibrotic diseases
    Publication number: 20130289014
    Abstract: The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of a cell signalling and/or angiogenesis inhibitor in conjunction with an Aurora kinase inhibitor.
    Type: Application
    Filed: June 28, 2013
    Publication date: October 31, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Flavio SOLCA, Ulrich GUERTLER, Ulrike TONTSCH-GRUNT
  • N-CONTAINING HETEROARYL DERIVATIVES AS JAK3 KINASE INHIBITORS
    Publication number: 20130289015
    Abstract: N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors.
    Type: Application
    Filed: June 28, 2013
    Publication date: October 31, 2013
    Inventors: Carmen Almansa Rosales, Jorge Salas Solana, Robert Soliva Soliva, Sergio Rodriguez Escrich, Maria Cristina Sicre Gonzalez
  • Carboxamide compounds and their use
    Patent number: 8569282
    Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I-A) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: October 29, 2013
    Assignee: CytoPathfinder, Inc.
    Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
  • Inhibitors of flaviviridae viruses
    Patent number: 8569302
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: October 29, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Mertzman, Philip A. Morganelli, William J. Watkins, Hong Ye
  • Compounds and compositions as c-Kit kinase inhibitors
    Patent number: 8569283
    Abstract: 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 c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: October 29, 2013
    Inventors: Valentina Molteni, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh
  • Amino-Indolyl-Substituted Imidazolyl-Pyrimidines and Their Use as Medicaments
    Publication number: 20130281430
    Abstract: The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula 1 wherein R1, R2, R3, R4 and R5 are defined as in claim 1 and pharmaceutically acceptable salts thereof and the use of these compounds for the preparation of a medicament for treating a disease selected from asthma, COPD, rheumatoid arthritis, specific lymphomas and specific diseases of the nervous system.
    Type: Application
    Filed: April 17, 2013
    Publication date: October 24, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Georg DAHMANN, Horst DOLLINGER, Christian GNAMM, Dennis FIEGEN, Matthias HOFFMANN, Jasna KLICIC, David James LAMB, Andreas SCHNAPP
  • 2,4-DIAMINO-PYRIMIDINES AS AURORA INHIBITORS
    Publication number: 20130281429
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
    Type: Application
    Filed: March 26, 2013
    Publication date: October 24, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephan Karl ZAHN, Guido BOEHMELT, Andreas MANTOULIDIS, Ulrich REISER, Matthias TREU, Ulrich GUERTLER, Andreas SCHOOP, Flavio SOLCA, Ulrike TONTSCH-GRUNT, Ralph BRUECKNER, Charlotte REITHER, Lars HERFURTH, Oliver KRAEMER, Heinz STADTMUELLER, Harald ENGELHARDT
  • COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES
    Publication number: 20130281403
    Abstract: The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.
    Type: Application
    Filed: June 7, 2013
    Publication date: October 24, 2013
    Inventors: Arnab K. Chatterjee, Advait S. Nagle, Tao Wu, David C. Tully, Kelli L. Kuhen
  • DNA-PK INHIBITORS
    Publication number: 20130281431
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: April 23, 2013
    Publication date: October 24, 2013
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Pyridone Derivatives
    Publication number: 20130281428
    Abstract: Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.
    Type: Application
    Filed: January 30, 2013
    Publication date: October 24, 2013
    Inventors: Hitoshi Ohki, Masahiro Ota, Kosuke Takeuchi, Hideaki Watanabe, Akitake Yamaguchi, Yoshihiro Shibata, Yuichi Tominaga, Takeshi Jimbo, Keijiro Kobayashi, Katsuhiro Kobayashi, Daisuke Fukatsu
  • TREATMENT OF DISEASES BY EPIGENETIC REGULATION
    Publication number: 20130281399
    Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 24, 2013
    Applicant: RVX Therapeutics Inc.
    Inventors: Kevin G. McLure, Peter R. Young
  • VIRAL POLYMERASE INHIBITORS
    Publication number: 20130274179
    Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.
    Type: Application
    Filed: April 11, 2013
    Publication date: October 17, 2013
    Applicant: Biota Scientific Management Pty Ltd
    Inventors: Silas Bond, Rosliana Halim, Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding
  • COMPOUNDS AND METHODS FOR ANTIVIRAL TREATMENT
    Publication number: 20130273037
    Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Application
    Filed: April 17, 2013
    Publication date: October 17, 2013
    Inventors: Dustin Siegel, David Sperandio, Hai Yang, Michael Sangi, Jay P. Parrish, Hon Chung Hui
  • INDAZOLYL TRIAZOL DERIVATIVES
    Publication number: 20130274241
    Abstract: Compounds of Formula (I) are used for the treatment of inflammation and autoimmune disorders.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 17, 2013
    Applicant: MERCK SERONO S.A. - INTELLECTUAL PROPERTY
    Inventors: Catherine Jorand-Lebrun, Stefano Crosignani, Jerome Dorbais, Tania Grippi-Vallotton, Adeline Pretre
  • FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF
    Publication number: 20130274240
    Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.
    Type: Application
    Filed: November 5, 2012
    Publication date: October 17, 2013
    Inventor: JAPAN TOBACCO INC.
  • VIRAL POLYMERASE INHIBITORS
    Publication number: 20130274218
    Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.
    Type: Application
    Filed: April 11, 2013
    Publication date: October 17, 2013
    Applicant: Biota Scientific Management Pty Ltd
    Inventors: Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding, Silas Bond, Rosliana Halim
  • Amide derivative
    Patent number: 8557802
    Abstract: Provided are a compound having an excellent hypoglycemic action, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: October 15, 2013
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Shigeo Yamanoi, Hidenori Namiki, Takahiro Katagiri, Mayuko Akiu, Katsuji Kagechika, Takeshi Honda, Koji Matsumoto, Ryutaro Nakashima
  • Purinone derivative
    Patent number: 8557803
    Abstract: Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: October 15, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Shingo Yamamoto, Toshio Yoshizawa
  • Compounds and compositions useful for the treatment of parasitic diseases
    Patent number: 8557801
    Abstract: The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.
    Type: Grant
    Filed: July 9, 2010
    Date of Patent: October 15, 2013
    Assignee: IRM LLC
    Inventors: Arnab K. Chatterjee, Advait S. Nagle, Tao Wu, David C. Tully, Kelli L. Kuhen
  • 1,4-OXAZEPANE DERIVATIVES
    Publication number: 20130267494
    Abstract: Provided is a compound having a monoamine reuptake inhibitory activity, which is represented by the formula (I) wherein ring A is an optionally substituted 6-membered aromatic ring, ring B is the substituents on ring A are optionally bonded to form, together with ring A, an optionally substituted 9- or 10-membered aromatic fused ring, and other symbols are as defined in the specification, or a salt thereof.
    Type: Application
    Filed: October 5, 2011
    Publication date: October 10, 2013
    Inventors: Yuji Ishichi, Masami Yamada, Taku Kamei, Ikuo Fujimori, Yoshihisa Nakada, Tomoya Yukawa, Nobuki Sakauchi, Yusuke Ohba, Tetsuya Tsukamoto
  • INDOLE AND INDAZOLE COMPOUNDS THAT ACTIVATE AMPK
    Publication number: 20130267493
    Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 10, 2013
    Applicant: PFIZER INC.
    Inventors: Samit Bhattacharya, Kimberly Cameron, Matthew Dowling, Dilinie Fernando, David Ebner, Kevin Filipski, Daniel Kung, Esther Lee, Aaron Smith, Meihua Tu
  • BICYCLIC AZAHETEROCYCLOBENZYLAMINES AS PI3K INHIBITORS
    Publication number: 20130261101
    Abstract: The present invention provides bicyclic azaheterocyclobenzylamines of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: April 1, 2013
    Publication date: October 3, 2013
    Inventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr.
  • Pyrrolopyridines as kinase inhibitors
    Patent number: 8545897
    Abstract: 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: Grant
    Filed: March 20, 2012
    Date of Patent: October 1, 2013
    Assignee: Array BioPharma Inc.
    Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunwardana, Pete Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
  • (3-(4-(aminomethyl)phenoxy or phenylthio)azetidin-1-yl)(5-phenyl-1,3,4-oxadiazol-2-yl)methanone compounds
    Patent number: 8546375
    Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: October 1, 2013
    Assignee: AstraZeneca AB
    Inventors: Susanne Doris Margit Bökman-Winiwarter, Marlene Fredenwall, Carl Anders Hogner, Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Björn Christian Ingvar Löfberg, Sverker Von Unge
  • PYRAZOLOPYRIDAZINES AND METHODS FOR TREATING RETINAL-DEGENERATIVE DISEASES AND HEARING LOSS ASSOCIATED WITH USHER SYNDROME
    Publication number: 20130252936
    Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.
    Type: Application
    Filed: March 8, 2013
    Publication date: September 26, 2013
    Applicant: Usher III Initiative
    Inventors: Roland Werner BÜRLI, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E. Harte
  • FUSED TRICYCLIC COMPOUNDS AS ADENOSINE RECEPTOR ANTAGONIST
    Publication number: 20130252885
    Abstract: The present disclosure relates to fused tricyclic compounds of formula (I) or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2A adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2A receptor.
    Type: Application
    Filed: September 22, 2011
    Publication date: September 26, 2013
    Applicant: Advinus Therapeutics Limited
    Inventors: Barawkar Dinesh, Basu Sujay, Ramdas Vidya, Naykodi Minakshi, Patel Meena, Shejul Yogesh, Thorat Sachin, Panmand Anil
  • BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION
    Publication number: 20130244996
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: March 5, 2013
    Publication date: September 19, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael J. BURKE, Suresh R. KAPADIA, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Hossein RAZAVI, Sonia RODRIGUEZ, Anjan SAHA, Robert SIBLEY, Lana Louise SMITH-KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, Jiang-Ping WU, Erick Richard Roush YOUNG, Qiang ZHANG, Qing ZHANG, Renee M. ZINDELL
  • PIPERIDIN-4-YL-AZETIDINE DIAMIDES AS MONOACYLGLCEROL LIPASE INHIBITORS
    Publication number: 20130244998
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R are defined herein.
    Type: Application
    Filed: May 2, 2013
    Publication date: September 19, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Peter J. Connolly, Haiyan Bian, Xun Li, Li Liu, Mark J. Macielag, Mark E. McDonnell
  • AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
    Publication number: 20130244997
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Application
    Filed: May 1, 2013
    Publication date: September 19, 2013
    Applicant: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J. Connolly, Christopher M. Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark J. Macielag, Mark E. McDonnell, Philip M. Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • BICYCLIC GPR119 MODULATORS
    Publication number: 20130245000
    Abstract: The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).
    Type: Application
    Filed: November 24, 2011
    Publication date: September 19, 2013
    Applicant: LUPIN LIMITED
    Inventors: Rajesh Thotapally, Onkar Gangaram Kachi, Atish Harishchandra Rodge, Ashok Bhau Pathak, Bhavana Shrirang Kardile, Milind Dattatraya Sindkhedkar, Venkata P. Palle, Rajender Kumar Kamboj
  • Substituted Heterocyclic Compounds
    Publication number: 20130244999
    Abstract: The present invention relates to substituted heterocyclic compounds of Formula I: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.
    Type: Application
    Filed: May 6, 2013
    Publication date: September 19, 2013
    Applicant: Incyte Corporation
    Inventors: Colin Zhang, Ding-quan Qian, Jincong Zhuo, Wenqing Yao
  • AZAINDOLES USEFUL AS INHIBITORS OF JANUS KINASES
    Publication number: 20130237516
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: April 25, 2013
    Publication date: September 12, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Luc Farmer, Gabriel Martinez-Botella, Albert Pierce, Francesco Salituro, Jian Wang, Wannamaker W. Wannamaker, Tiansheng Wang
  • NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
    Publication number: 20130237518
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).
    Type: Application
    Filed: October 24, 2011
    Publication date: September 12, 2013
    Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, JR.
  • AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
    Publication number: 20130237517
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Application
    Filed: April 29, 2013
    Publication date: September 12, 2013
    Applicant: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J. Connolly, Christopher M. Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark J. Macielag, Mark E. McDonnell, Philip M. Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Indole modulators of S1P receptors
    Patent number: 8530462
    Abstract: The present invention relates to novel indole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: September 10, 2013
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, Michael E. Garst, Wha Bin Im