Exactly Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/303)
  • Patent number: 10071086
    Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.
    Type: Grant
    Filed: January 31, 2017
    Date of Patent: September 11, 2018
    Assignee: Samumed, LLC
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Patent number: 10065954
    Abstract: Specific compounds of formula (Ia): and pharmaceutically acceptable salts thereof. Pharmaceutical compositions of the specific compounds of formula (Ia) and pharmaceutically acceptable salts thereof. A method for inhibiting tumor growth in a subject that includes administering to the subject an effective amount of a compound selected from the specific compounds of formula (Ia) and pharmaceutically acceptable salts thereof. A method for modulating semicarbazide-sensitive amine oxidase activity in a subject that includes administering to the subject an effective amount of a compound selected from the specific compounds of formula (Ia) and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: September 4, 2018
    Assignee: PROXIMAGEN LIMITED
    Inventors: Max Espensen, Lee Patient, Edward Savory
  • Patent number: 10034861
    Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: July 31, 2018
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Karsten Juhl, Mauro Marigo, Paulo Jorge Vieira Vital, Mikkel Jessing, Morten Langgård, Lars Kyhn Rasmussen, Carl Martin Sebastian Clementson
  • Patent number: 10016362
    Abstract: Apixaban liquid formulation is provided. Also provided is a method of administering an apixaban liquid formulation.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: July 10, 2018
    Assignees: BRISTOL-MYERS SQUIBB COMPANY, PFIZER INC.
    Inventors: Sherif Ibrahim Farag Badawy, Susan Lum
  • Patent number: 10016406
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: July 10, 2018
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Patent number: 10011586
    Abstract: The present invention relates to a heterocyclic compound having a novel structure that can be used in the prevention or treatment of diseases caused by abnormality in a PRS (prolyl-tRNA synthetase) activity, a method for preparing the same, and a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: July 3, 2018
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Joon Seok Park, Youn Jung Yoon, Min Jae Cho, Ho Bin Lee, Ja Kyung Yoo, Bong Yong Lee
  • Patent number: 10000771
    Abstract: Isolated peptides comprising nuclear targeting activity or being capable of preventing endogenous nuclear targeting activity are disclosed. Polynucleotides encoding same, pharmaceutical compositions comprising same, as well as uses thereof are also disclosed.
    Type: Grant
    Filed: April 13, 2016
    Date of Patent: June 19, 2018
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: Rony Seger, Dana Chuderland
  • Patent number: 10000466
    Abstract: 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: Grant
    Filed: July 7, 2017
    Date of Patent: June 19, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael J. Orwat, Donald J. P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
  • Patent number: 9994563
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease 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: Grant
    Filed: November 12, 2015
    Date of Patent: June 12, 2018
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Patent number: 9981994
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
    Type: Grant
    Filed: January 17, 2017
    Date of Patent: May 29, 2018
    Assignee: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Craig C. Beeson, Christopher C. Lindsey, Yuri K. Peterson, Baerbel Rohrer
  • Patent number: 9975893
    Abstract: Disclosed are a compound of formula (I), a tautomer, an optical isomer or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the above-mentioned compounds. The above-mentioned compounds have the activity of inhibiting Xa factor positive effect, and can be used for the preparation of a medicament for preventing and/or treating diseases inhibiting Xa factor positive effect in case of low bleeding risk.
    Type: Grant
    Filed: September 2, 2015
    Date of Patent: May 22, 2018
    Assignee: CSPC ZHONGQI PHARMACEUTICAL TECHNOLOGY (SHIJIAZHUANG) CO., LTD.
    Inventors: Ying Shi, Qingzhi Gao, Yi Mi, Xuliang Wang
  • Patent number: 9944638
    Abstract: Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: April 17, 2018
    Assignee: JANSSEN SCIENCES IRELAND US
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Patent number: 9925226
    Abstract: A method for manufacturing water-soluble medical amber causes that original great molecular groups of medical amber crystals are decomposed into hydrophilic extracted liquid plentiful of water and having small molecular groups, which can be directly coated on skin without mixing with water and added with grease or oil. The method original performs disinfecting and sterilizing treatment for natural medical amber crystals; after a polishing and cleaning step, they are placed in a bottle with treatment liquid therein for a predetermined time period so that the mixture in the bottle ferments and decomposes into small pieces which presents as cream-like liquid. Then paddies are added into the bottle. The bottle is retained through several months so that the medical amber crystals ferment quickly to form as a liquid composite. Then the bottle is evaporated several hours so that the liquid composite is distilled out of the bottle.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: March 27, 2018
    Inventor: Huei Chen Yang
  • Patent number: 9914910
    Abstract: Methods of preserving and/or protecting pancreatic beta cells by inhibiting NOX-1. In a further aspect, NOX-1 inhibitors are administered to a subject in order to preserve and/or protect beta cells in the prevention or treatment of diabetes. NOX-1 inhibitors are also disclosed.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: March 13, 2018
    Assignee: Eastern Virginia Medical School
    Inventor: David Taylor-Fishwick
  • Patent number: 9889140
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, 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: Grant
    Filed: September 16, 2016
    Date of Patent: February 13, 2018
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 9890178
    Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: February 13, 2018
    Assignee: Janssen Sciences Ireland UC
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Patent number: 9873695
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example as modulators of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
    Type: Grant
    Filed: August 5, 2015
    Date of Patent: January 23, 2018
    Assignee: RaQualia Pharma Inc.
    Inventors: Yasuhiro Iwata, Kiyoshi Kawamura, Masaki Sudo, Kaoru Shimada, Shinichi Koizumi, Nobuyuki Takahashi, Keiko Obata, Makiko Kuroda
  • Patent number: 9855272
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Grant
    Filed: August 23, 2016
    Date of Patent: January 2, 2018
    Assignee: Samumed, LLC
    Inventors: John Hood, Sunil Kumar Kc, David Mark Wallace
  • Patent number: 9844536
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, 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: Grant
    Filed: November 29, 2016
    Date of Patent: December 19, 2017
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 9820976
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterized by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.
    Type: Grant
    Filed: September 1, 2016
    Date of Patent: November 21, 2017
    Assignees: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
    Inventors: Caroline Joy Springer, Ion Niculescu-Duvaz, Richard Marais, Dan Niculescu-Duvaz, Alfonso Zambon, Delphine Menard
  • Patent number: 9815854
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, 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: Grant
    Filed: November 21, 2016
    Date of Patent: November 14, 2017
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar K C, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 9809592
    Abstract: The present invention provides a compound of the Formula (I) below: Wherein R1 is selected from the group consisting of H, CH3, CN, CH2CN, C(CH3)2CN, and F; R2 is selected from the group consisting of H, O(C1-C3alkyl)R5, CH2CN, and CN; R3 is selected from the group consisting of H, OCH3, CN, C(CH3)2CN, and CH2CN; R4 is selected from the group consisting of H and CH3; R5 is selected from the group consisting of H, CN, C(CH3)2CN, OCH3, S(O)2CH3, and C(CH3)2OH; provided that at least one selected from the group consisting of R1, R2, R3 and R4 is H; or a pharmaceutically acceptable salt thereof, methods of treating diabetes using the compound and a process for preparing the compound.
    Type: Grant
    Filed: January 6, 2015
    Date of Patent: November 7, 2017
    Assignee: Eli Lilly and Company
    Inventors: Chafiq Hamdouchi, Pranab Maiti, Anne Reifel Miller
  • Patent number: 9771362
    Abstract: 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: Grant
    Filed: June 20, 2016
    Date of Patent: September 26, 2017
    Assignee: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Stanway
  • Patent number: 9763927
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: June 16, 2016
    Date of Patent: September 19, 2017
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar Kc
  • Patent number: 9725435
    Abstract: 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: Grant
    Filed: June 15, 2016
    Date of Patent: August 8, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael J. Orwat, Donald J. P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
  • Patent number: 9725446
    Abstract: Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.
    Type: Grant
    Filed: January 5, 2016
    Date of Patent: August 8, 2017
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Christian Sirrenberg, Thomas J. J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
  • Patent number: 9675593
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: June 13, 2017
    Assignee: INTERMUNE, Inc.
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
  • Patent number: 9624243
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: April 18, 2017
    Assignee: NOVARTIS AG
    Inventors: Thomas David McCarthy, Alan Naylor
  • Patent number: 9603846
    Abstract: A crystalline Form N-1 of apixaban substantially free from one or more of: 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid; 7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-1-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide; or methyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate, relative to apixaban by area percentage of HPLC and having a mean particle size equal to or greater than 100 ?m.
    Type: Grant
    Filed: November 24, 2015
    Date of Patent: March 28, 2017
    Assignee: Cadila Healthcare Limited
    Inventors: Brij Khera, Kumar Kamlesh Singh, Santosh Devidas Diwakar, Sunil Dnyaneshwar Narode, Hiteshkumar Natwarlal Suthar
  • Patent number: 9598397
    Abstract: The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: March 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yang Cao, Donald R. Gauthier, Jr., Guy R. Humphrey, Tetsuji Itoh, Michel Journet, Gang Qian, Benjamin D. Sherry, David M. Tschaen
  • Patent number: 9586977
    Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.
    Type: Grant
    Filed: December 8, 2015
    Date of Patent: March 7, 2017
    Assignee: Samumed, LLC
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Patent number: 9572799
    Abstract: The invention relates to the use of compounds corresponding to formula (I), or a pharmaceutically acceptable salt thereof, for preparing a medicament for the treatment of bladder cancer.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: February 21, 2017
    Assignee: SANOFI
    Inventor: Chantal Alcouffe
  • Patent number: 9567332
    Abstract: The present invention provides a process for the preparation and purification of apixaban.
    Type: Grant
    Filed: January 15, 2014
    Date of Patent: February 14, 2017
    Assignee: GLENMARK PHARMACEUTICALS LIMITED
    Inventors: Shekhar Bhaskar Bhirud, Sushanta Mishra, Suresh Babu Narayanan, Sachin Bhagwan Naykodi, Samir Naik, Sachin Srivastava, Pramod Vitthal Patil
  • Patent number: 9546185
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, 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: Grant
    Filed: September 8, 2015
    Date of Patent: January 17, 2017
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar K C, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 9540398
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, 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: Grant
    Filed: September 8, 2015
    Date of Patent: January 10, 2017
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 9534017
    Abstract: This application describes a family of compounds acting as ?-arrestin effectors. Such compounds may provide significant therapeutic benefit in the treatment of chronic and acute cardiovascular diseases.
    Type: Grant
    Filed: August 15, 2014
    Date of Patent: January 3, 2017
    Assignee: Trevena, Inc.
    Inventors: Dennis Yamashita, Xiao-Tao Chen
  • Patent number: 9527853
    Abstract: The present invention provides fused bicyclic triazole derivatives of Formula (I) useful as gamma secretase modulators (GSM), for the treatment of Alzheimer's disease and related diseases.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: December 27, 2016
    Assignee: Ares Trading S.A.
    Inventors: Ben Whittaker, Chris Steele, David Hardick, Dale Mitchell, Vincent Pomel, Anna Quattropani, Dirk Beher
  • Patent number: 9499543
    Abstract: The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: November 22, 2016
    Assignee: RaQualia Pharma Inc.
    Inventors: Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi, Toyoharu Numata
  • Patent number: 9447071
    Abstract: Disclosed are crystalline free base ansolvate forms of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1), such as the free base Form I, Form II and Material N. Also disclosed are crystalline free base solvates of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1).
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: September 20, 2016
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Stephan D. Parent, Travis Houston
  • Patent number: 9446035
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Grant
    Filed: May 21, 2015
    Date of Patent: September 20, 2016
    Assignee: Samumed, LLC
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Patent number: 9447096
    Abstract: The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: September 20, 2016
    Assignee: RaQualia Pharma Inc.
    Inventors: Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi, Toyoharu Numata
  • Patent number: 9439893
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.
    Type: Grant
    Filed: July 30, 2015
    Date of Patent: September 13, 2016
    Assignees: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
    Inventors: Caroline Springer, Ion Niculescu-Duvaz, Richard Marais, Dan Niculescu-Duvaz, Alfonso Zambon, Delphine Menard
  • Patent number: 9434700
    Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
    Type: Grant
    Filed: October 23, 2014
    Date of Patent: September 6, 2016
    Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
  • Patent number: 9434732
    Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I 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 JAK kinase activity in a patient are disclosed.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: September 6, 2016
    Assignee: Genentech, Inc.
    Inventors: Bing-Yan Zhu, Michael Siu, Steven R. Magnuson, Richard Pastor, He Haiying, Xiao Yisong, Zheng Jifu, Xu Xing, Zhao Junping, Christopher Hurley, Jun Liang, Wendy Liu, Joseph P. Lyssikatos
  • Patent number: 9394301
    Abstract: 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: Grant
    Filed: March 16, 2015
    Date of Patent: July 19, 2016
    Assignee: Cancer Research Technology Limited
    Inventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Stanway
  • Patent number: 9381195
    Abstract: The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; for use in the treatment of pain.
    Type: Grant
    Filed: July 29, 2013
    Date of Patent: July 5, 2016
    Assignee: PIERRE FABRE MEDICAMENT
    Inventors: Pierre Sokoloff, Frédéric Cachoux
  • Patent number: 9359330
    Abstract: The present disclosure provides substituted piperidines or pyrrolidines having Formula IA: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R6, A, X, m and n are defined as set forth in the specification. In certain embodiments, Compounds of the present disclosure are useful for treating pain. The present disclosure is also directed to the use of Compounds of the present disclosure to treat a disorder responsive to blockade of one or more sodium channels.
    Type: Grant
    Filed: August 26, 2014
    Date of Patent: June 7, 2016
    Assignee: Purdue Pharma L.P.
    Inventors: Laykea Tafesse, Jae Hyun Park
  • Patent number: 9359329
    Abstract: The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt: in which n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X represents a group —CH2, —CH(R?)—, —NH(R?)— or a heteroatom chosen from O and S, it being understood that R? represents a group —(C1-C5)alkyl, —(C1-C5)alkoxy, —CH2-aryl, —C(O)R5 or —COOR5; R1 represents an oxo group, —COOR5, —W—OH or —W—NR5R6; R2 represents an H atom or a group chosen from the groups (i) —(C1-C5)alkyl, (ii) —(C1-C5)alkoxy, (iii) —COOR5, (iv) —NR5R6, (v) —C(O)—NR5R6, (vi) —SO2—NR3R4, (vii) heteroaryl optionally substituted with a group —(C1-C5)alkyl, (viii) —W-aryl, (ix) —W-heteroaryl, (x) —O—W-aryl, (xi) —O—W-heteroaryl and (xii) —O—W—NR5R6; it being understood that R3 and R4, (i) which may be identical or different, represent, independently of each other, an H atom, a group —(C1-C5)alkyl, —(C3-C6)cycloalkyl, aryl, heteroaryl, —CH2-heteroaryl, —(C1-C5)alkyl-NR5R6, —W—OH or —W—NR5R6; or
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: June 7, 2016
    Assignee: SANOFI
    Inventors: Jean-Michel Altenberger, Valerie Fossey, Geraldine Manette
  • Patent number: 9339494
    Abstract: Azaindoles having inhibitory activity on RSV replication and having the formula I compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: May 5, 2015
    Date of Patent: May 17, 2016
    Assignee: Janssen Sciences Ireland UC
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Patent number: 9340514
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Grant
    Filed: April 2, 2015
    Date of Patent: May 17, 2016
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Neil Bifulco, Jr., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu