Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/210.21)
  • Bicyclic compound
    Patent number: 8703758
    Abstract: The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: April 22, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tohru Yamashita, Makoto Kamata, Hideki Hirose, Masataka Murakami, Takuya Fujimoto, Zenichi Ikeda, Tsuneo Yasuma, Ikuo Fujimori, Ryo Mizojiri, Tomoya Yukawa
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 8703759
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: April 22, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
  • HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt
    Publication number: 20140107097
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Taraneh Mirzadegan, Kelly Ganamet
  • METHYLENE LINKED QUINOLINYL MODULATORS OF RORyt
    Publication number: 20140107094
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Joan Pierce, Steven Goldberg, Anne Fourie, Xiaohua Xue
  • HETEROARYL LINKED QUINOLINYL MODULATORS OF RORyt
    Publication number: 20140107096
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 17, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: KRISTI A. LEONARD, KENT BARBAY, JAMES P. EDWARDS, KEVIN D. KREUTTER, DAVID A. KUMMER, UMAR MAHAROOF, RACHEL NISHIMURA, MAUD URBANSKI, HARIHARAN VENKATESAN, AIHUA WANG, RONALD L. WOLIN, CRAIG R. WOODS, ANNE FOURIE, XIAOHUA XUE
  • IMIDAZOLO-, OXAZOLO-, AND THIAZOLOPYRIMIDINE MODULATORS OF TRPV1
    Publication number: 20140107098
    Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
  • PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS
    Publication number: 20140107099
    Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 17, 2014
    Applicant: Genentech, Inc.
    Inventors: Jeffrey Blaney, Paul A. Gibbons, Emily Hanan, Joseph P. Lyssikatos, Steven R. Magnuson, Richard Pastor, Thomas E. Rawson, Aihe Zhou, Bing-Yan Zhu
  • Chemical compounds
    Patent number: 8697685
    Abstract: The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1-R4 are defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: April 15, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Jeffrey Michael Axten, Charles William Blackledge, Jr., Gerald Patrick Brady, Jr., Yanhong Feng, Seth W. Grant, Jesus Raul Medina, William H. Miller, Stuart P. Romeril
  • Methods of Using PI3K and MEK Modulators
    Publication number: 20140100215
    Abstract: The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
    Type: Application
    Filed: December 7, 2013
    Publication date: April 10, 2014
    Applicant: Exelixis, Inc.
    Inventors: Dana T. Aftab, A. Douglas Laird, Peter Lamb, Jean-Francois A. Martini
  • Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
    Patent number: 8691807
    Abstract: The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: April 8, 2014
    Assignee: Incyte Corporation
    Inventors: Wenqing Yao, David M. Burns, Jincong Zhuo
  • IMIDAZOPYRIDINE COMPOUNDS
    Publication number: 20140088080
    Abstract: [Problem] An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. [Means for Solution] It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 27, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Yuji KOGA, Kyoichi MAENO, Ippei SATO, Yoshimasa IMAMURA, Takeshi HANAZAWA, Maiko IIDA, Kazuhiko OHNE, Kenichiro IMAMURA, Tsubasa WATANABE, Eisuke NOZAWA, Hiroshi SHIBATA
  • Amino-Heterocyclic Compounds
    Publication number: 20140088081
    Abstract: The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, A, and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: Pfizer Inc.
    Inventors: Michelle Marie Claffey, Christopher John Helal, Patrick Robert Verhoest
  • Fused pyridine derivatives
    Patent number: 8680089
    Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: March 25, 2014
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
  • Sulfonyl containing benzothiazole inhibitors of endothelial lipase
    Patent number: 8680090
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: March 25, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
  • 2,3-DIHYDRO-1H-INDEN-1-YL-2,7-DIAZASPIRO[3.5]NONANE DERIVATIVES
    Publication number: 20140080756
    Abstract: The present invention provides a compound of Formula (I) a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.
    Type: Application
    Filed: November 18, 2013
    Publication date: March 20, 2014
    Applicant: Pfizer Inc.
    Inventors: Samit K. Bhattacharya, Kimberly O. Cameron, Dilinie P. Fernando, Kim F. McClure, Daniel W. Kung, Allyn T. Londregan, Suvi T.M. Orr
  • SUBSTITUTED INDAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
    Publication number: 20140080807
    Abstract: The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 20, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi
  • PYRAZOLO[3,4-D]PYRIMIDINE COMPOUNDS AND THEIR USE AS PDE2 INHIBITORS AND/OR CYP3A4 INHIBITORS
    Publication number: 20140080806
    Abstract: The present invention provides, inter alia, compounds of Formula (I) and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal. The present invention further provides compounds of Formula (Id) and pharmaceutically acceptable salts thereof as CYP3A4 selective inhibitors.
    Type: Application
    Filed: May 24, 2012
    Publication date: March 20, 2014
    Inventors: Christopher John Helal, Thomas Allen Chappie, John Michael Humphrey
  • Substituted indazole derivatives active as kinase inhibitors
    Patent number: 8673893
    Abstract: Substituted indazole 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 associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: March 18, 2014
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • BENZOXAZEPINES ASN INHIBITORS OF P13K/M TOR AND METHODS OF THEIR USE AND MANUFACTURE
    Publication number: 20140073628
    Abstract: The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural formula I and pharmaceutically acceptable salts thereof, wherein the variables are as defined herein.
    Type: Application
    Filed: November 23, 2011
    Publication date: March 13, 2014
    Inventor: Kenneth D. Rice
  • IMIDAZOLE CARBONYL COMPOUND
    Publication number: 20140073622
    Abstract: To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 13, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Tsuyoshi Soneda, Hiroshi Takeshita, Yoshiko Kagoshima, Yuko Yamamoto, Takafumi Hosokawa, Toshiyuki Konosu, Nobuhisa Masuda, Takuya Uchida, Issei Achiwa, Junichi Kuroyanagi, Tetsunori Fujisawa, Aki Yokomizo, Tetsuji Noguchi
  • DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) FOR USE IN TREATMENT OF DISEASES ASSOCIATED WITH A PTEN DEFICIENCY
    Publication number: 20140066429
    Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions associated with a PTEN deficiency that are ameliorated by the inhibition of PARP activity.
    Type: Application
    Filed: August 21, 2013
    Publication date: March 6, 2014
    Applicant: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel Chu, Bing Wang, Ying Feng, Yuqiao Shen, Leonard Edwin Post
  • 6,7,8,9-Tetrahydro-5H-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
    Publication number: 20140066428
    Abstract: The present invention relates to compounds defined by formula I wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.
    Type: Application
    Filed: November 5, 2013
    Publication date: March 6, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephan-Georg MUELLER, Christopher John BROWN, Alexander HEIFETZ, Bernd NOSSE, Juergen PRESTLE, Natacha PREVOST, Klaus RUDOLF, Stefan SCHEUERER, Marcus SCHINDLER, Dirk STENKAMP, Leo THOMAS, Heather TYE
  • AURORA KINASE MODULATORS AND METHOD OF USE
    Publication number: 20140066430
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Application
    Filed: October 3, 2013
    Publication date: March 6, 2014
    Applicant: Amgen Inc.
    Inventors: Victor J. CEE, Holly L. DEAK, Bingfan DU, Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Hanh Nho NGUYEN, Philip R. Olivieri, Vinod F. Patel, Karina ROMERO, Laurie Schenkel
  • PYRAZOLOPYRIDINE AND PYRAZOLOPYRIMIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS
    Publication number: 20140057894
    Abstract: Disclosed herein is a compound of Formula I: wherein X, R1, R2, and R3 are as defend herein, or a pharmaceutically acceptable salt thereof to allow the drug to penetrate the cell membrane; or a prodrug, or the compound is labeled with a detectable label or an affinity tag thereof. Also disclosed is a pharmaceutical composition, a method of treating a disorder mediated by melanocortin-4 receptors, and a method of treating obesity using the compounds described.
    Type: Application
    Filed: January 26, 2012
    Publication date: February 27, 2014
    Applicant: Universite De Montreal
    Inventors: Michel Bouvier, Anne Marinier, Rejean Ruel, Patricia René, Yves Chantigny, Philippe Dagneau, Stéphane Gingras
  • PYRIDONE AND AZA-PYRIDONE COMPOUNDS AND METHODS OF USE
    Publication number: 20140057896
    Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: October 22, 2013
    Publication date: February 27, 2014
    Inventors: Antonio J.M. BARBOSA, Peter A. BLOMGREN, Kevin S. CURRIE, Ravi KRISHNAMOORTHY, Jeffrey E. KROPF, Seung H. LEE, Scott A. MITCHELL, Daniel ORTWINE, Aaron C. SCHMITT, Xiaojing WANG, Jianjun XU, Wendy YOUNG, Honglu ZHANG, Zhongdong ZHAO, Pavel E. ZHICHKIN
  • INDAZOLE- AND PYRROLOPYRIDINE-DERIVATIVE AND PHARMACEUTICAL USE THEREOF
    Publication number: 20140057895
    Abstract: The present invention relates to a novel indazole- or pyrrolopyridine-derivative comprising a 5 membered heterocyclic substituent at 1 position thereof which has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same.
    Type: Application
    Filed: June 6, 2012
    Publication date: February 27, 2014
    Inventors: Kazuhiro Mizuno, Junya Ikeda, Takanori Nakamura, Masato Iwata, Hiromichi Otaka, Nana Goto
  • Histone Deacetylase Inhibitors
    Publication number: 20140051680
    Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: February 28, 2012
    Publication date: February 20, 2014
    Applicant: REPLIGEN CORPORATION
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • MODULATORS OF CELLULAR ADHESION
    Publication number: 20140051675
    Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
    Type: Application
    Filed: August 19, 2013
    Publication date: February 20, 2014
    Applicant: SARcode Bioscience Inc.
    Inventors: Wang SHEN, Kenneth BARR, Johan D. OSLOB, Min ZHONG
  • KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
    Publication number: 20140051679
    Abstract: The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
    Type: Application
    Filed: October 12, 2012
    Publication date: February 20, 2014
    Applicant: UNIVERISTY HEALTH NETWORKS
    Inventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter B. Sampson, Miklos Feher, Donald E. Awrey
  • N-substituted saturated heterocyclic sulfone compounds with CB2 receptor agonistic activity
    Patent number: 8653063
    Abstract: This invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3, R4, R5, R6, R7, k, m, n, p, q, r and s are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: February 18, 2014
    Assignee: RaQualia Pharma Inc.
    Inventors: Kazuo Ando, Yasuhiro Iwata
  • INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/BETA-CATENIN SIGNALING PATHWAY INHIBITORS
    Publication number: 20140045815
    Abstract: Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Application
    Filed: September 5, 2013
    Publication date: February 13, 2014
    Applicant: Samumed, LLC
    Inventors: John Hood, Sunil Kumar KC
  • 5-CYANO-4- (PYRROLO [2,3B] PYRIDINE-3-YL) -PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS
    Publication number: 20140045812
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: August 7, 2013
    Publication date: February 13, 2014
    Inventors: Michael Mortimore, Stephen Clinton Young, Simon Robert Lorrie Everitt, Ronald Knegtel, Joanne Louise Pinder, Alistair Peter Rutherford, Steven Durrant, Guy Brenchley, Jean-Damien Charrier, Michael O'Donnell
  • ALDOSTERONE SYNTHASE INHIBITORS
    Publication number: 20140045819
    Abstract: This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.
    Type: Application
    Filed: April 20, 2012
    Publication date: February 13, 2014
    Applicants: ElexoPharm GmbH, SCHERING CORPORATION
    Inventors: Scott B. Hoyt, Whitney Lane Petrilli, Clare London, Yusheng Xiong, Jerry Andrew Taylor, Amjad Ali, Michael Man-Chu Lo, Timothy J. Henderson, Qingzhong Hu, Rolf Hartmann, Lina Yin, Ralf Heim, Emmanuel Bey, Rohit Saxena, Swapan Kumar Samanta, Bheemashankar A. Kulkarni
  • BENZOTHIAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USE
    Publication number: 20140045818
    Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.
    Type: Application
    Filed: April 20, 2012
    Publication date: February 13, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Michael L. Mitchell, Paul A. Roethle, Lianhong Xu, Hong Yang, Ryan McFadden, Kerim Babaoglu
  • Cyclopropyl Fused Indolobenzazepine HCV NS5B Inhibitors
    Publication number: 20140045816
    Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 13, 2014
    Inventors: John A. Bender, Min Ding, Robert G. Gentles, Piyasena Hewawasam
  • TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS
    Publication number: 20140045817
    Abstract: Provided herein is a method of treating a PIM-1 and/or PIM-2 and/or PIM-3 kinase-mediated condition in a mammal, which comprises administering to said mammal a therapeutically effective amount of a compound of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Applicant: Array BioPharma Inc.
    Inventors: Shelley Allen, Laura L. Celeste, T. Gregg Davis, Robert Kirk DeLisle, Julie Marie Hicks, Stefan D. Gross, Erik James Hicken, Leila J. Jackson, Nicholas C. Kallan, Joseph P. Lyssikatos, Fredrik P. Marmsater, Mark C. Munson, Jed Pheneger, Bryson Rast, John E. Robinson, Stephen T. Schlachter, George T. Topalov, A. Dale Wright, Qian Zhao
  • RING-FUSED HETEROCYCLIC DERIVATIVE
    Publication number: 20140038941
    Abstract: A ring-fused heterocyclic derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof having a T-type calcium channel regulatory effect and useful as a pruritus therapeutic and/or preventive agent, and the like are provided. In the general formula (I), R1 represents optionally substituted lower alkyl, and the like; R2 represents an optionally substituted cycloalkyl, and the like; Q represents a hydrogen atom, and the like; R3 represents —C(?O)NR8R9 (wherein R8 and R9 may be the same or different, and each represents a hydrogen atom, and the like), and the like; L1 represents —CR11AR11B— (wherein R11A and R11B may be the same or different, and each represents a hydrogen atom, and the like), and the like; and W1 and W2 may be the same or different, and each represents C—R12 (wherein R12 represents a hydrogen atom, and the like), and the like.
    Type: Application
    Filed: February 1, 2012
    Publication date: February 6, 2014
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Takashi Sawada, Tomohiro Danjo, Keiichi Motosawa, Takayuki Furuta, Maki Ichioka, Masamori Sugawara, Noriaki Uesaka
  • SEROTONIN RECEPTOR MODULATOR
    Publication number: 20140038943
    Abstract: Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
    Type: Application
    Filed: October 10, 2013
    Publication date: February 6, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Nicholas I. Carruthers, Wenying Chai, Jill A. Jablonowski, Chandravadan R. Shah, Brock T. Shireman, Devin M. Swanson, Vi Tran, Victoria Wong
  • RORgammaT INHIBITORS
    Publication number: 20140038942
    Abstract: The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.
    Type: Application
    Filed: February 10, 2012
    Publication date: February 6, 2014
    Applicants: Merck Sharp & Dohme B.V., Merck Sharp & Dohme Corp.
    Inventors: Willem Frederik Johan Karstens, Mario Van Der Stelt, Jos Cals, Rita Corte Real Goncalves Azevedo, Kenneth Jay Barr, Hongjun Zhang, Richard Thomas Beresis, Dongshan Zhang, Xiaobang Duan
  • DIHYDRODIAZEPINES USEFUL AS INHIBITORS OF PROTEIN KINASES
    Publication number: 20140038935
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: January 21, 2013
    Publication date: February 6, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: Vertex Pharmaceuticals Incorporated
  • ISOINDOLINONE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
    Publication number: 20140038936
    Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. 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: May 7, 2013
    Publication date: February 6, 2014
    Inventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Anne-Laure Grillot, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Jingrong Cao, Upul Keerthi Bandarage, Suganthini S. Nanthakumar
  • NOVEL EGFR MODULATORS AND USES THEREOF
    Publication number: 20140038940
    Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.
    Type: Application
    Filed: March 15, 2013
    Publication date: February 6, 2014
    Inventors: Xiao XU, Xiaobo Wang, Long Mao, Li Zhao, Biao Xi
  • Method of using PI3K and MEK modulators
    Patent number: 8642584
    Abstract: The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
    Type: Grant
    Filed: August 7, 2012
    Date of Patent: February 4, 2014
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, A. Douglas Laird, Peter Lamb, Jean-Francois A. Martini
  • COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
    Publication number: 20140031333
    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: Application
    Filed: September 19, 2013
    Publication date: January 30, 2014
    Applicant: IRM LLC
    Inventors: Valentina MOLENTI, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh
  • AZOLOTRIAZINONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
    Publication number: 20140031337
    Abstract: The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein the variables are defined herein.
    Type: Application
    Filed: September 30, 2013
    Publication date: January 30, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Pratik Devasthale, William N. Washburn, Kishore V. Renduchintala, Radhakrishan Sridhar
  • Methods for inhibiting allograft rejection
    Patent number: 8637038
    Abstract: Disclosed herein are methods for treating or inhibiting allograft rejection in a transplant recipient. In some embodiments, the methods include administering to the transplant recipient a first amount of a JAK1/3 inhibitor comprising 5-(2-(4-fluoro-3-methoxy-5-methylphenylamino)-5-methylpyrimidin-4-ylamino)benzo[d]oxazol-2(3H)-one (Compound I) or a prodrug thereof and administering to the transplant recipient a second amount of a non-JAK1/3 inhibitor immunosuppressant, wherein the combined effect of the first amount and the second amount is greater than the effect of the first amount or the second amount individually, wherein the JAK1/3 inhibitor acts in combination with the non-JAK1/3 inhibitor immunosuppressant to inhibit or treat allograft rejection. In some embodiments at least one of the first amount or the second amount is individually a suboptimal dose for inhibiting or treating allograft rejection.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: January 28, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Vanessa Taylor, Esteban Masuda
  • Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1
    Patent number: 8637527
    Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: January 28, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
  • INDAZOLES
    Publication number: 20140024634
    Abstract: A method of treating a disease or condition for which a JAK inhibitor is indicated in a subject in need of such treatment, comprising administering to the subject a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, and particularly, a method for the treatment of various inflammatory diseases, particularly psoriasis, asthma and COPD.
    Type: Application
    Filed: September 30, 2013
    Publication date: January 23, 2014
    Inventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Steven Wade Kortum, Yogesh Anil Sabnis, Florian Michel Wakenhut, Gavin Alistair Whitlock
  • AZAINDOLE DERIVATIVES
    Publication number: 20140018344
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.
    Type: Application
    Filed: July 8, 2013
    Publication date: January 16, 2014
    Inventors: Edcon Chang, Wolfgang Reinhard Ludwig Notz, Michael B. Wallace
  • INHIBITION OF ENZYMES
    Publication number: 20140018345
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R5, R6, A1, A2, A3, A4 assume meanings as defined in formula (I) are inhibitors of neutrophil elastase.
    Type: Application
    Filed: July 12, 2013
    Publication date: January 16, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A
    Inventors: Carmelida Capaldi, Robert Andrew Heald, Nicholas Charles Ray, Jonathan Mark Sutton