Exactly Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/303)
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Patent number: 10071086Abstract: 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: GrantFiled: January 31, 2017Date of Patent: September 11, 2018Assignee: Samumed, LLCInventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Patent number: 10065954Abstract: 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: GrantFiled: September 17, 2015Date of Patent: September 4, 2018Assignee: PROXIMAGEN LIMITEDInventors: Max Espensen, Lee Patient, Edward Savory
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Patent number: 10034861Abstract: 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: GrantFiled: June 29, 2017Date of Patent: July 31, 2018Assignee: H. Lundbeck A/SInventors: Jan Kehler, Karsten Juhl, Mauro Marigo, Paulo Jorge Vieira Vital, Mikkel Jessing, Morten Langgård, Lars Kyhn Rasmussen, Carl Martin Sebastian Clementson
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Patent number: 10016362Abstract: Apixaban liquid formulation is provided. Also provided is a method of administering an apixaban liquid formulation.Type: GrantFiled: May 24, 2016Date of Patent: July 10, 2018Assignees: BRISTOL-MYERS SQUIBB COMPANY, PFIZER INC.Inventors: Sherif Ibrahim Farag Badawy, Susan Lum
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Patent number: 10016406Abstract: 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: GrantFiled: August 18, 2017Date of Patent: July 10, 2018Assignee: Samumed, LLCInventors: John Hood, David Mark Wallace, Sunil Kumar KC
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Patent number: 10011586Abstract: 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: GrantFiled: June 7, 2016Date of Patent: July 3, 2018Assignee: Daewoong Pharmaceutical Co., Ltd.Inventors: Joon Seok Park, Youn Jung Yoon, Min Jae Cho, Ho Bin Lee, Ja Kyung Yoo, Bong Yong Lee
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Patent number: 10000771Abstract: 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: GrantFiled: April 13, 2016Date of Patent: June 19, 2018Assignee: Yeda Research and Development Co. Ltd.Inventors: Rony Seger, Dana Chuderland
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Patent number: 10000466Abstract: 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: GrantFiled: July 7, 2017Date of Patent: June 19, 2018Assignee: Bristol-Myers Squibb CompanyInventors: Michael J. Orwat, Donald J. P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
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Patent number: 9994563Abstract: 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: GrantFiled: November 12, 2015Date of Patent: June 12, 2018Assignee: Samumed, LLCInventors: John Hood, David Mark Wallace, Sunil Kumar KC
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Patent number: 9981994Abstract: 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: GrantFiled: January 17, 2017Date of Patent: May 29, 2018Assignee: MUSC FOUNDATION FOR RESEARCH DEVELOPMENTInventors: Craig C. Beeson, Christopher C. Lindsey, Yuri K. Peterson, Baerbel Rohrer
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Patent number: 9975893Abstract: 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: GrantFiled: September 2, 2015Date of Patent: May 22, 2018Assignee: CSPC ZHONGQI PHARMACEUTICAL TECHNOLOGY (SHIJIAZHUANG) CO., LTD.Inventors: Ying Shi, Qingzhi Gao, Yi Mi, Xuliang Wang
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Patent number: 9944638Abstract: 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: GrantFiled: April 22, 2016Date of Patent: April 17, 2018Assignee: JANSSEN SCIENCES IRELAND USInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Patent number: 9925226Abstract: 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: GrantFiled: July 11, 2014Date of Patent: March 27, 2018Inventor: Huei Chen Yang
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Patent number: 9914910Abstract: 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: GrantFiled: March 31, 2017Date of Patent: March 13, 2018Assignee: Eastern Virginia Medical SchoolInventor: David Taylor-Fishwick
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Patent number: 9889140Abstract: 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: GrantFiled: September 16, 2016Date of Patent: February 13, 2018Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 9890178Abstract: 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: GrantFiled: April 22, 2016Date of Patent: February 13, 2018Assignee: Janssen Sciences Ireland UCInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Patent number: 9873695Abstract: 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: GrantFiled: August 5, 2015Date of Patent: January 23, 2018Assignee: RaQualia Pharma Inc.Inventors: Yasuhiro Iwata, Kiyoshi Kawamura, Masaki Sudo, Kaoru Shimada, Shinichi Koizumi, Nobuyuki Takahashi, Keiko Obata, Makiko Kuroda
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Patent number: 9855272Abstract: 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: GrantFiled: August 23, 2016Date of Patent: January 2, 2018Assignee: Samumed, LLCInventors: John Hood, Sunil Kumar Kc, David Mark Wallace
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Patent number: 9844536Abstract: 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: GrantFiled: November 29, 2016Date of Patent: December 19, 2017Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 9820976Abstract: 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: GrantFiled: September 1, 2016Date of Patent: November 21, 2017Assignees: 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
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Patent number: 9815854Abstract: 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: GrantFiled: November 21, 2016Date of Patent: November 14, 2017Assignee: Samumed, LLCInventors: Sunil Kumar K C, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 9809592Abstract: 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: GrantFiled: January 6, 2015Date of Patent: November 7, 2017Assignee: Eli Lilly and CompanyInventors: Chafiq Hamdouchi, Pranab Maiti, Anne Reifel Miller
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Patent number: 9771362Abstract: 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: GrantFiled: June 20, 2016Date of Patent: September 26, 2017Assignee: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Stanway
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Patent number: 9763927Abstract: 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: GrantFiled: June 16, 2016Date of Patent: September 19, 2017Assignee: Samumed, LLCInventors: John Hood, David Mark Wallace, Sunil Kumar Kc
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Patent number: 9725435Abstract: 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: GrantFiled: June 15, 2016Date of Patent: August 8, 2017Assignee: Bristol-Myers Squibb CompanyInventors: Michael J. Orwat, Donald J. P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
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Patent number: 9725446Abstract: 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: GrantFiled: January 5, 2016Date of Patent: August 8, 2017Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Christian Sirrenberg, Thomas J. J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
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Patent number: 9675593Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.Type: GrantFiled: May 23, 2016Date of Patent: June 13, 2017Assignee: INTERMUNE, Inc.Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
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Patent number: 9624243Abstract: 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: GrantFiled: January 4, 2013Date of Patent: April 18, 2017Assignee: NOVARTIS AGInventors: Thomas David McCarthy, Alan Naylor
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Patent number: 9603846Abstract: 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: GrantFiled: November 24, 2015Date of Patent: March 28, 2017Assignee: Cadila Healthcare LimitedInventors: Brij Khera, Kumar Kamlesh Singh, Santosh Devidas Diwakar, Sunil Dnyaneshwar Narode, Hiteshkumar Natwarlal Suthar
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Patent number: 9598397Abstract: 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: GrantFiled: December 2, 2014Date of Patent: March 21, 2017Assignee: 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
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Patent number: 9586977Abstract: 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: GrantFiled: December 8, 2015Date of Patent: March 7, 2017Assignee: Samumed, LLCInventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Patent number: 9572799Abstract: 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: GrantFiled: June 13, 2014Date of Patent: February 21, 2017Assignee: SANOFIInventor: Chantal Alcouffe
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Patent number: 9567332Abstract: The present invention provides a process for the preparation and purification of apixaban.Type: GrantFiled: January 15, 2014Date of Patent: February 14, 2017Assignee: GLENMARK PHARMACEUTICALS LIMITEDInventors: Shekhar Bhaskar Bhirud, Sushanta Mishra, Suresh Babu Narayanan, Sachin Bhagwan Naykodi, Samir Naik, Sachin Srivastava, Pramod Vitthal Patil
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Patent number: 9546185Abstract: 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: GrantFiled: September 8, 2015Date of Patent: January 17, 2017Assignee: Samumed, LLCInventors: Sunil Kumar K C, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 9540398Abstract: 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: GrantFiled: September 8, 2015Date of Patent: January 10, 2017Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 9534017Abstract: 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: GrantFiled: August 15, 2014Date of Patent: January 3, 2017Assignee: Trevena, Inc.Inventors: Dennis Yamashita, Xiao-Tao Chen
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Patent number: 9527853Abstract: 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: GrantFiled: June 14, 2013Date of Patent: December 27, 2016Assignee: Ares Trading S.A.Inventors: Ben Whittaker, Chris Steele, David Hardick, Dale Mitchell, Vincent Pomel, Anna Quattropani, Dirk Beher
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Patent number: 9499543Abstract: 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: GrantFiled: May 28, 2014Date of Patent: November 22, 2016Assignee: RaQualia Pharma Inc.Inventors: Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi, Toyoharu Numata
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Patent number: 9447071Abstract: 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: GrantFiled: February 6, 2015Date of Patent: September 20, 2016Assignee: Global Blood Therapeutics, Inc.Inventors: Zhe Li, Stephan D. Parent, Travis Houston
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Patent number: 9446035Abstract: 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: GrantFiled: May 21, 2015Date of Patent: September 20, 2016Assignee: Samumed, LLCInventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Patent number: 9447096Abstract: 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: GrantFiled: May 28, 2014Date of Patent: September 20, 2016Assignee: RaQualia Pharma Inc.Inventors: Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi, Toyoharu Numata
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Patent number: 9439893Abstract: 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: GrantFiled: July 30, 2015Date of Patent: September 13, 2016Assignees: 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
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Patent number: 9434700Abstract: Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.Type: GrantFiled: October 23, 2014Date of Patent: September 6, 2016Inventors: Neil Bifulco, Jr., Lucian V. DiPietro, Brian L. Hodous, Chandrasekhar V. Miduturu
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Patent number: 9434732Abstract: 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: GrantFiled: October 9, 2013Date of Patent: September 6, 2016Assignee: 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
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Patent number: 9394301Abstract: 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: GrantFiled: March 16, 2015Date of Patent: July 19, 2016Assignee: Cancer Research Technology LimitedInventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Stanway
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Patent number: 9381195Abstract: 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: GrantFiled: July 29, 2013Date of Patent: July 5, 2016Assignee: PIERRE FABRE MEDICAMENTInventors: Pierre Sokoloff, Frédéric Cachoux
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Patent number: 9359330Abstract: 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: GrantFiled: August 26, 2014Date of Patent: June 7, 2016Assignee: Purdue Pharma L.P.Inventors: Laykea Tafesse, Jae Hyun Park
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Patent number: 9359329Abstract: 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; orType: GrantFiled: March 7, 2014Date of Patent: June 7, 2016Assignee: SANOFIInventors: Jean-Michel Altenberger, Valerie Fossey, Geraldine Manette
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Patent number: 9339494Abstract: 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: GrantFiled: May 5, 2015Date of Patent: May 17, 2016Assignee: Janssen Sciences Ireland UCInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Patent number: 9340514Abstract: 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: GrantFiled: April 2, 2015Date of Patent: May 17, 2016Assignee: BLUEPRINT MEDICINES CORPORATIONInventors: Neil Bifulco, Jr., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu