Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/210.21)
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Patent number: 10383866Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders, cough, and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: GrantFiled: December 19, 2016Date of Patent: August 20, 2019Assignee: AMGEN INC.Inventors: Matthew Weiss, Thomas Dineen, Benjamin C. Milgram
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Patent number: 10385058Abstract: Methods for preparing the Bruton's Tyrosine Kinase (“BTK”) inhibitor compound 2-{3?-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4?]bipyridinyl-2?-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided. Methods for preparing tricyclic lactam compounds are also provided.Type: GrantFiled: December 14, 2017Date of Patent: August 20, 2019Assignee: Genentech, Inc.Inventors: Danial Beaudry, Theresa Cravillion, Francis Gosselin, Ngiap-Kie Lim, Sushant Malhotra, Qingping Tian, Haiming Zhang, Alexander Gmehling, Alec Fettes, Stephan Bachmann
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Patent number: 10378068Abstract: Provided herein are methods of treating a subject having a cancer, methods of selecting a treatment for a subject having a cancer, methods of selecting a subject having a cancer for a treatment that does not include a Trk inhibitor, methods of determining the likelihood that a subject having a cancer will have a positive response to a treatment with a Trk inhibitor, methods of predicting the efficacy of a Trk inhibitor in a subject having cancer, methods of determining a subject's risk for developing a Trk inhibitor-resistant cancer, and methods of determining the presence of a Trk inhibitor-resistant cancer in a subject, based on the detection of a cell from a sample from the subject that has at least one of the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.Type: GrantFiled: October 16, 2017Date of Patent: August 13, 2019Assignees: Loxo Oncology, Inc., Array BioPharma, Inc.Inventors: Nisha Nanda, Joshua H. Bilenker, James F. Blake, Gabrielle R. Kolakowski, Barbara J. Brandhuber, Steven W. Andrews
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Patent number: 10370387Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) 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: GrantFiled: January 18, 2018Date of Patent: August 6, 2019Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: Yun-Long Li, Wenyu Zhu, Song Mei
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Patent number: 10363249Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used in pharmaceutical compositions to treat taxane-resistant cancers. Methods are provided for treating taxane-resistant cancer in a subject. Methods are also provided for increasing the sensitivity of a cancer cell to taxanes (i.e., paclitaxel, Nab-paclitaxel docetaxel, and/or cabazitaxel) treatment.Type: GrantFiled: August 14, 2015Date of Patent: July 30, 2019Assignee: 3-V Biosciences, Inc.Inventor: Timothy Sean Heuer
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Patent number: 10344023Abstract: The present disclosure is based, in part, on the discovery that disclosed compounds can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.Type: GrantFiled: December 23, 2015Date of Patent: July 9, 2019Assignee: Proteostasis Therapeutics, Inc.Inventors: Cecilia M. Bastos, Benito Munoz, Bradley Tait
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Patent number: 10328082Abstract: The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1-C6 linear or branched chain alkyl, etc.; R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.Type: GrantFiled: May 18, 2015Date of Patent: June 25, 2019Assignee: Pfizer Inc.Inventors: Eugene Lvovich Piatnitski Chekler, Adam Matthew Gilbert, Rayomand Jal Unwalla, Patrick Robert Verhoest, James Thomas Anderson
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Patent number: 10308656Abstract: Provided herein are methods for identifying and treating subjects having conditions involving aberrant Ku70/80 activity. In particular, the invention relates to small-molecules which function as inhibitors of Ku70/80 protein and the non-homologous end-joining (NHEJ) pathway, and their use as therapeutics for the treatment of cancer and other diseases.Type: GrantFiled: August 16, 2016Date of Patent: June 4, 2019Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONAInventors: Eric Weterings, Daruka Mahadevan, Josef Vagner
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Patent number: 10301323Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).Type: GrantFiled: July 26, 2018Date of Patent: May 28, 2019Assignee: BIOMARIN PHARMACEUTICAL INC.Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
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Patent number: 10294224Abstract: A process for producing crystals of a compound represented by the following formula (I): by crystallizing the compound from an aqueous solution containing the compound and an inorganic salt, such as sodium chloride. Such crystals can be subjected to lyophilization to provide a lyophilized composition having a desirable storage stability.Type: GrantFiled: December 4, 2015Date of Patent: May 21, 2019Assignee: MEIJI SEIKA PHARMA CO., LTD.Inventors: Takaya Ogawa, Takuya Yokoyama, Shusuke Furuyama, Masato Ichiki, Kenichi Fushihara
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Patent number: 10287252Abstract: Provided is a compound for use in medicine for inhibiting tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO), which compound comprises formula (I) wherein X1, X2, and X7, may be the same or different and each is independently selected from C and N; X3, X4, X5, and X6 may be the same or different and each is independently selected from C, N, O and S wherein when X3 is N it has a double bond and wherein when X6 is N it has a double bond; the dotted line is a bond which may be present or absent; R1, R2, R3, R4, R5, R6, and R7 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that at least one of R2, R3, R4 and R6 comprises a group Y; and provided that the number of R1, R2, R3, R4, R5, R6, and R7 groups present is such that the respective valencies of X1, X2, X3, X4, X5, X6, and X7 are maintained; and wherein Y is a group having a formula selected from (II), (III), (IV), (V) whereinType: GrantFiled: November 2, 2015Date of Patent: May 14, 2019Assignee: IOmet Pharma Ltd.Inventors: Phillip M. Cowley, Alan Wise, Susan Davis, Margaret Huggett, Michael Kiczun
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Patent number: 10253018Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, ester, stereoisomer, tautomer, solvate, hydrate, or combination thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).Type: GrantFiled: May 24, 2018Date of Patent: April 9, 2019Assignee: ENANTA PHARMACEUTICALS, INC.Inventors: Guoqiang Wang, Brett Granger, Ruichao Shen, Yong He, Xuechao Xing, Jun Ma, Jiang Long, Jing He, Bin Wang, Yat Sun Or
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Patent number: 10246462Abstract: Disclosed herein, inter alia, are compounds and methods of use thereof for the modulation of chemokine receptor activity.Type: GrantFiled: September 8, 2017Date of Patent: April 2, 2019Assignee: FLX BIO, INC.Inventors: Hilary Plake Beck, Berenger Biannic, Minna Hue Thanh Bui, Dennis X. Hu, Jeffrey J. Jackson, John Michael Ketcham, Jay Patrick Powers, Maureen Kay Reilly, Omar Robles-Resendiz, Hunter Paul Shunatona, James Ross Walker, David Juergen Wustrow, Ashkaan Younai, Mikhail Zibinsky
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Patent number: 10246461Abstract: The invention relates generally to pharmaceutical tablet compositions comprising fumaric acid and the compound (S)-2-(3?-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4?-bipyridin]-2?-yl)-7,7-dimethyl-2,3,4,6,7,8-hexahydro-1H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one free base that is an inhibitor of Bruton's tyrosine kinase. The invention further relates to amorphous solid dispersions comprising at least one polymer and the Bruton's kinase inhibitor free base compound. The invention further relates to crystalline mesylate salts, crystalline chloride salts and crystalline sulfate salts of the Bruton's kinase inhibitor free base compound. In some aspects, the crystalline salts are single polymorphs.Type: GrantFiled: February 27, 2017Date of Patent: April 2, 2019Assignee: Genentech, Inc.Inventors: Chen Mao, Dawen Kou, Po-Chang Chiang
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Patent number: 10231956Abstract: 4-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 4-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: August 3, 2016Date of Patent: March 19, 2019Assignee: Samumed, LLCInventors: Sunil Kumar Kc, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 10208041Abstract: The present invention relates to compounds according to Formula (II): or a stereoisomer, tautomer or pharmaceutically acceptable salt or ester thereof, wherein A, R1 and R2 are defined herein. Also described are pharmaceutically acceptable compositions of Formula (II) compounds as well as methods for utilizing the compounds of Formula (II) and the pharmaceutically acceptable compositions of Formula (II) compounds as antibacterial agents and ?-lactamase inhibitors, useful in the treatment of infectious diseases.Type: GrantFiled: October 5, 2017Date of Patent: February 19, 2019Assignee: Hoffman-La Roche Inc.Inventors: Paul Spurr, Christelle Carl, Martin Binder, Kewei Yang, Valérie Verhoeven
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Patent number: 10160761Abstract: Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphic forms, cocrystals, and amorphous forms thereof, and pharmaceutical compositions thereof.Type: GrantFiled: September 13, 2016Date of Patent: December 25, 2018Assignee: Infinity Pharmaceuticals, Inc.Inventors: Louis Grenier, Andre Lescarbeau, Praveen Sharma, Daniel G. Genov
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Patent number: 10154995Abstract: Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: August 23, 2017Date of Patent: December 18, 2018Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Adam Cook, Indrani W. Gunawardana, Kevin W. Hunt, Michael Lyon, Andrew T. Metcalf, Peter J. Mohr, David A. Moreno, Brad Newhouse, Li Ren, Tony P. Tang, Allen A. Thomas, Jacob Schwarz, Jane Schmidt, Lewis Gazzard, Huifen Chen
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Patent number: 10155259Abstract: The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.Type: GrantFiled: July 29, 2015Date of Patent: December 18, 2018Assignee: Merck Sharp & Dohme B.V.Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik
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Patent number: 10131665Abstract: A crystalline form of a diazabicyclooctane derivative represented by the following Formula (VII), and processes for producing the same:Type: GrantFiled: October 8, 2014Date of Patent: November 20, 2018Assignee: MEIJI SEIKA PHARMA CO., LTD.Inventors: Takao Abe, Takeshi Furuuchi, Yoshiaki Sakamaki, Nakako Mitsuhashi, Yumiko Saito
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Patent number: 10131662Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.Type: GrantFiled: March 7, 2016Date of Patent: November 20, 2018Assignee: SYNGENTA PARTICIPATIONS AGInventors: Pierre Joseph Marcel Jung, Andrew Edmunds, Michel Muehlebach, Roger Graham Hall, Jerome Yves Cassayre
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Patent number: 10131664Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: GrantFiled: February 20, 2018Date of Patent: November 20, 2018Assignee: Celgene Quanticel Research, Inc.Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
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Patent number: 10092563Abstract: The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein W, B, n, m, A?, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.Type: GrantFiled: June 10, 2015Date of Patent: October 9, 2018Assignee: Gilead Sciences, Inc.Inventors: Shaopei Cai, Zhimin Du, Joshua Kaplan, Jennifer A. Loyer-Drew, Devan Naduthambi, Barton W. Phillips, Gary Phillips, Joshua Van Veldhuizen, William J. Watkins, Suet Chung Yeung
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Patent number: 10087185Abstract: Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions comprising compounds of Formula (I) and methods of using compounds of Formula (I).Type: GrantFiled: October 23, 2017Date of Patent: October 2, 2018Assignee: Janssen Pharmaceutica NVInventors: Michael K. Ameriks, Márió Gyuris, Brian Ngo Laforteza, Terry Patrick Lebold, Stephen Todd Meyer, Suchitra Ravula, Brad M. Savall, Brock T. Shireman, Warren Stanfield Wade, János Gerencsér
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Patent number: 10081622Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; 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: GrantFiled: February 22, 2017Date of Patent: September 25, 2018Assignee: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
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Patent number: 10077264Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.Type: GrantFiled: December 12, 2016Date of Patent: September 18, 2018Assignee: NOVIRA THERAPEUTICS, INC.Inventors: George D. Hartman, Scott Kuduk
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Patent number: 10071095Abstract: The present invention relates to methods of treating various central nervous system disorders using novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: GrantFiled: August 10, 2017Date of Patent: September 11, 2018Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma, S.A.Inventors: Jose Maria Cid-Nunez, Daniel Oehlrich, Andres Avelino Trabanco-Suarez, Gary John Tresadern, Juan Antonio Vega Ramiro, Gregor James MacDonold
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Patent number: 10053454Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: February 27, 2014Date of Patent: August 21, 2018Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Poss, David R. Tortolani, Ashok Vinayak Purandare, John S. Tokarski, Christopher P. Mussari, Muthoni G. Kamau, Dharmpal S. Dodd, Ashvinikumar V. Gavai, Daniel O'Malley, Tram N. Huynh, Wayne Vaccaro, Lalgudi S. Harikrishnan
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Patent number: 10053457Abstract: The invention relates to compounds of Formula (I) wherein n, X, R1 and R2 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.Type: GrantFiled: January 14, 2016Date of Patent: August 21, 2018Assignee: IDORSIA PHARMACEUTICALS LTD.Inventors: Eva Caroff, Emmanuel Meyer
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Patent number: 10045983Abstract: Heteroaryl pyridone and aza-pyridone compounds 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 heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: August 31, 2017Date of Patent: August 14, 2018Assignee: Genentech, Inc.Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
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Patent number: 10035799Abstract: The present inventions include a method of inhibiting COMT enzyme in a subject as well as compounds of formula I, or a pharmaceutically acceptable salt thereof, that are useful in the treatment of various disorders mediated by COMT, including Parkinson's disease and/or schizophrenia.Type: GrantFiled: January 29, 2016Date of Patent: July 31, 2018Assignee: LIEBER INSTITUTE FOR BRAIN DEVELOPMENTInventors: James Barrow, Glen Ernst, Yifang Huang, Ingrid Price Buchler, Daniel Weinberger
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Patent number: 10030030Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4?S,5?R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.Type: GrantFiled: February 2, 2018Date of Patent: July 24, 2018Assignee: Daiichi Sankyo Company, LimitedInventors: Shoko Yoshida, Yuuichi Sugimoto
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Patent number: 10030019Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: GrantFiled: June 2, 2016Date of Patent: July 24, 2018Assignee: FEDORA PHARMACEUTICALS INC.Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
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Patent number: 10023578Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4?S,5?R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.Type: GrantFiled: February 2, 2018Date of Patent: July 17, 2018Assignee: Daiichi Sankyo Company, LimitedInventors: Shoko Yoshida, Yuuichi Sugimoto
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Patent number: 10005773Abstract: The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-?B-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.Type: GrantFiled: September 25, 2014Date of Patent: June 26, 2018Assignee: Janssen Pharmaceutica NVInventors: George Hynd, Patrizia Tisselli, David Edward Clark, Janusz Jozef Kulagowski, Calum MacLeod, Samuel Edward Mann, Terry Aaron Panchal, Stephen Colin Price, John Gary Montana
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Patent number: 9974782Abstract: The invention provides for compounds that are phosphodiesterase inhibitors. The invention further provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention also provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.Type: GrantFiled: August 12, 2016Date of Patent: May 22, 2018Assignee: The Trustees of Columbia University in the City of New YorkInventors: Yan Feng, Ottavio Arancio, Shixian Deng, Donald W. Landry
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Patent number: 9951047Abstract: The present invention provides salts consisting of an organocarboxylic acid selected from the group consisting of succinic acid and maleic acid and a compound represented by formula (I) and crystals thereat which can be used as bulk materials for pharmaceuticals.Type: GrantFiled: August 17, 2015Date of Patent: April 24, 2018Assignee: Eisai R&D Management Co., Ltd.Inventors: Shunsuke Ozaki, Kenshi Yoshida
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Patent number: 9938283Abstract: The present invention provides a crystalline form of baricitinib characterized by an XRPD pattern substantially as depicted in FIG. 1, a process for its preparation, a pharmaceutical composition comprising it, and its use for the treatment of JAK-associated diseases.Type: GrantFiled: April 29, 2015Date of Patent: April 10, 2018Assignee: Sun Pharmaceutical Industries LimitedInventors: Gyanendra Pandey, Javeena, Kaptan Singh, Mohan Prasad
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Patent number: 9926313Abstract: A series of substituted 3H imidazo[4,5-b]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.Type: GrantFiled: December 8, 2014Date of Patent: March 27, 2018Assignee: UCB BIOPHARMA SPRLInventors: Michael Louis Robert Deligny, Jag Paul Heer, Victoria Elizabeth Jackson, Boris Kroeplien, Fabien Claude Lecomte, John Robert Porter
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Patent number: 9926282Abstract: The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.Type: GrantFiled: January 17, 2014Date of Patent: March 27, 2018Assignee: Bristol-Myers Squibb CompanyInventors: Peter W. Glunz, Yan Zou, Mimi L. Quan, Vladimir Ladziata
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Patent number: 9926301Abstract: The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) 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: GrantFiled: June 20, 2016Date of Patent: March 27, 2018Assignee: Incyte CorporationInventors: Yun-Long Li, Jincong Zhuo, Song Mei
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Patent number: 9918939Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.Type: GrantFiled: July 29, 2014Date of Patent: March 20, 2018Assignee: Gilead Connecticut, Inc.Inventors: Melissa Jean Casteel, Bei Li, Rowchanak Pakdaman, Diana Sperger, Dimitrios Stefanidis
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Patent number: 9920041Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.Type: GrantFiled: February 22, 2017Date of Patent: March 20, 2018Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
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Patent number: 9907791Abstract: Provided herein are methods for inhibiting osteolysis or treating osteoporosis in a subject in need thereof, the method including administering to the subject at least one RON inhibitor. The osteolysis may be caused by a condition selected from the group consisting of cancer, inflammation, and cyst. The condition may include a bone tumor or a tumor located in bone. The subject may have been diagnosed with bone cancer. The inhibitor may be ASLAN002. The inhibitor may be OSI-296. The inhibitor may be selective or specific for RON. The inhibitor may not depend on the function of RANKL or TGF?.Type: GrantFiled: March 13, 2015Date of Patent: March 6, 2018Assignee: University of Utah Research FoundationInventors: Alana L. Welm, Kelsi Kretschmann Andrade
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Patent number: 9884874Abstract: Provided is a novel compound having bromodomain and extra terminal domain (BET) protein inhibiting activities, and a pharmaceutical composition comprising the same which can be useful for prevention or treatment of precancerous transformation or cancer.Type: GrantFiled: April 8, 2015Date of Patent: February 6, 2018Assignee: KAINOS MEDICINE, INC.Inventors: Su-Sung Oh, Minjeong Choi
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Patent number: 9873702Abstract: The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: December 4, 2015Date of Patent: January 23, 2018Assignees: Southern Research Institute, The United States of America as Represented by the Secretary, Department of Health and Human ServicesInventors: Subramaniam Ananthan, Richard B. Rothman
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Patent number: 9868748Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR?. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.Type: GrantFiled: May 1, 2014Date of Patent: January 16, 2018Assignee: Vitae Pharmaceuticals, Inc.Inventors: David A. Claremon, Lawrence Wayne Dillard, Chengguo Dong, Yi Fan, Lanqi Jia, Stephen D. Lotesta, Andrew Marcus, Suresh B. Singh, Colin M. Tice, Jing Yuan, Wei Zhao, Yajun Zheng, Linghang Zhuang
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Patent number: 9868733Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: GrantFiled: August 19, 2013Date of Patent: January 16, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: James M. Apgar, Tesfaye Biftu, Ping Chen, Danqing Feng, Jacqueline D. Hicks, Ahmet Kekec, Kenneth J. Leavitt, Bing Li, Iyassu Sebhat, Xiaoxia Qian, Lan Wei, Robert R. Wilkening, Zhicai Wu, Ashok Arasappan
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Patent number: 9833454Abstract: The compound N2-(3-(difluoromethoxy)-4-(3-methyl-1H-1,2,4-triazol-1-yl)phenyl)-7-(4-fluorophenyl)-N4,5,5-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidine-2,4-diamine: [PLEASE INSERT CHEMICAL STRUCTURE HERE] reduces -amyloid peptide (A 42) production and has low potential for bioactivation, and may be useful in the treatment of Alzheimer's Disease and other conditions affected by -amyloid peptide (A 42) production.Type: GrantFiled: April 1, 2015Date of Patent: December 5, 2017Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Boy, Stephen E. Mercer, Richard E. Olson, Xiaoliang Zhou
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Patent number: RE47396Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.Type: GrantFiled: October 20, 2015Date of Patent: May 21, 2019Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen