Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
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Patent number: 10239873Abstract: Provided are 7-azaindole or 4,7-diazaindole derivatives as an IKK? (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor. The 7-azaindole or 4,7-diazaindole derivative effectively inhibits IKK? and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.Type: GrantFiled: March 24, 2016Date of Patent: March 26, 2019Assignee: GREEN CROSS CORPORATIONInventors: Soongyu Choi, Kwang-Seop Song, Hee Jeong Seo, Sang-ho Ma, Eun-Jung Park, Younggyu Kong, So Ok Park, Kisoo Park, Ickhwan Son, Min Ju Kim, Man-Young Cha, Mi-Soon Kim, Sang Mi Kang, Dong Hyuk Jang, Jangwon Hong
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Patent number: 10233195Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.Type: GrantFiled: March 31, 2015Date of Patent: March 19, 2019Assignee: INTERMUNE, INC.Inventors: Johnnie Y. Ramphal, Brad Owen Buckman, Kumaraswamy Emayan, John Beamond Nicholas, Scott D. Seiwert
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Patent number: 10227346Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.Type: GrantFiled: February 6, 2018Date of Patent: March 12, 2019Assignee: Pfizer Inc.Inventors: Mark Edward Schnute, Andrew Christopher Flick, Peter Jones, Neelu Kaila, Scot Richard Mente, John David Trzupek, Michael L. Vazquez, Goran Mattias Wennerstal, Li Xing, Edouard Zamaratski, Liying Zhang, Rayomand Jal Unwalla
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Patent number: 10226453Abstract: 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 12, 2019Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 10206917Abstract: An aqueous drug that contains the compound represented by formula (1) or a salt thereof and in which the precipitation and the chemical dissolution of the compound of formula (1) or of a salt thereof is inhibited. An aqueous drug containing: the compound represented by formula (1) or a salt thereof; and a magnesium compound. The aqueous drug has a pH of 5.8-6.9. The concentration of the compound represented by formula (1) is 3 mg/mL or more.Type: GrantFiled: June 2, 2016Date of Patent: February 19, 2019Assignee: KYORIN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Goto, Hitoshi Kozuka, Mizuho Shibata, Wataru Minagawa, Norihiro Kanayama, Chifuyu Toriumi
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Patent number: 10202380Abstract: 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: June 27, 2016Date of Patent: February 12, 2019Assignee: Syngenta Participations AGInventors: Pierre Joseph Marcel Jung, Andrew Edmunds, Michel Muehlebach
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Patent number: 10195184Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving abnormal or excessive fibrosis.Type: GrantFiled: March 19, 2017Date of Patent: February 5, 2019Assignee: ANGION BIOMEDICA CORP.Inventors: Bijoy Panicker, Rama K. Mishra, Dong Sung Lim, Lambertus J. W. M. Oehlen, Dawoon Jung
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Patent number: 10172851Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.Type: GrantFiled: January 3, 2018Date of Patent: January 8, 2019Assignee: Array BioPharma Inc.Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Tony P. Tang, Li Ren
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Patent number: 10172845Abstract: Provided herein are compounds of the Formula I: or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.Type: GrantFiled: January 3, 2018Date of Patent: January 8, 2019Assignee: Array BioPharma Inc.Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, James Collier, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Ginelle A. Ramann, Tony P. Tang, Li Ren, Shane M. Walls
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Patent number: 10154970Abstract: The present invention provides methods for modulating the immune response of a subject to a therapeutic agent, the method comprising administering an effective amount of a triphenylethylene (TRIP) compound with an effective amount of the therapeutic agent. In particular embodiments, the TRIP compound enhances the immune response of the subject to the therapeutic agent. In some embodiments, the TRIP compound is administered in different dosing schedules to provide a biphasic immunomodulation effect.Type: GrantFiled: June 15, 2017Date of Patent: December 18, 2018Assignee: The Regents of the University of CaliforniaInventor: Michael W. DeGregorio
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Patent number: 10154993Abstract: [Problem] To provide a novel pharmaceutical composition which can suppress delayed, release of the compound represented in general formula (1) or a salt thereof. [Solution] This solid pharmaceutical composition contains the compound represented in general formula (1), or a salt thereof, and a salting-out agent.Type: GrantFiled: October 23, 2015Date of Patent: December 18, 2018Assignee: KYORIN PHARMACEUTICAL CO., LTD.Inventors: Hiroshi Uchida, Masataka Hanada, Yoshikazu Miyazaki
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Patent number: 10144733Abstract: A compound of formula (I) or a salt thereof: wherein R1 represents a five-membered aromatic heterocycle selected from a N- or a C-linked mono- or di-substituted pyrazole, an N- or a C-linked optionally mono- or di-substituted triazole or an N- or a C-linked optionally mono- or di-substituted imidazole, which five-membered aromatic heterocycle may be substituted by one or two of the groups selected a methyl group, an ethyl group, a fluorine atom, a hydroxymethyl group, a 2-hydroxypropan-2-yl group, a trifluoromethyl group, a difluoromethyl group or a fluoromethyl group, except that when R1 represents an N-linked mono- or di-substituted pyrazole, R1 does not represent 3,5-Dimethyl-1H-pyrazol-1-yl, 5-Methyl-1H-pyrazol-1-yl, 5-Ethyl-3-methyl-1H-pyrazol-1-yl, 3,5-Diethyl-1H-pyrazol-1-yl, 4-Fluoro-3,5-dimethyl-1H-pyrazol-1-yl, 3-Methyl-1H-pyrazol-1-yl or 1H-pyrazol-1-yl.Type: GrantFiled: September 22, 2015Date of Patent: December 4, 2018Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Niall Andrew Anderson, Ian Baxter Campbell, Matthew Howard James Campbell-Crawford, Ashley Paul Hancock, Seble Lemma, Simon John Fawcett MacDonald, John Martin Pritchard, Panayiotis Alexandrou Procopiou
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Patent number: 10138249Abstract: The present invention is directed to [1,2,4]triazolo[4,3-a]pyridine and [1,2,4]triazolo[4,3-a]pyrazine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.Type: GrantFiled: August 7, 2017Date of Patent: November 27, 2018Assignee: Incyte CorporationInventors: Liangxing Wu, Xiaozhao Wang, Wenqing Yao, Colin Zhang
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Patent number: 10137124Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.Type: GrantFiled: January 3, 2018Date of Patent: November 27, 2018Assignee: Array BioPharma Inc.Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Tony P. Tang, Li Ren
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Patent number: 10131677Abstract: 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: August 4, 2017Date of Patent: November 20, 2018Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 10125132Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R7, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.Type: GrantFiled: May 1, 2017Date of Patent: November 13, 2018Assignee: GALAPAGOS NVInventors: Nicolas Desroy, Bertrand Heckmann, Reginald Christophe Xavier Brys, Agnès Marie Joncour, Christophe Peixoto, Xavier Marie Bock
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Patent number: 10112942Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.Type: GrantFiled: December 29, 2017Date of Patent: October 30, 2018Assignee: Array BioPharma Inc.Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Tony P. Tang, Li Ren
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Patent number: 10106538Abstract: Protein kinases are regulators of cellular signaling and their functional dysregulation is common in carcinogenesis and many other disease states or disorders. The present invention relates to novel chemical entities that have biological activity to modulate mammalian protein kinase enzymes. In particular, compounds of the invention display potent inhibition of breast tumor related kinase (BRK).Type: GrantFiled: December 29, 2017Date of Patent: October 23, 2018Assignee: Princeton Drug Discovery IncInventors: Kan He, Lining Cai
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Patent number: 10093681Abstract: The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use.Type: GrantFiled: September 23, 2016Date of Patent: October 9, 2018Assignee: Southern Methodist UniversityInventors: Edward R. Biehl, Haribabu Ankati, Sukanta Kamila
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Patent number: 10087184Abstract: 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: September 20, 2017Date of Patent: October 2, 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: 10072026Abstract: The invention provides a crystalline form of the compound of formula: that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such crystalline form and methods of using such crystalline form in mammals suffering from inflammatory bowel diseases.Type: GrantFiled: June 23, 2017Date of Patent: September 11, 2018Assignee: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Xiaojun Huang, Venkat R. Thalladi
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Imidazo[1,2-A]pyridine derivatives for use as inhibitors of human immunodeficiency virus replication
Patent number: 10065953Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: GrantFiled: August 25, 2015Date of Patent: September 4, 2018Assignee: ViiV HEALTHCARE UK (NO.5) LIMITEDInventors: Timothy P. Connolly, Kyle J. Eastman, B. Narasimhulu Naidu, Kevin Peese -
Patent number: 10059707Abstract: The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also the preparation and use of the crystalline polymorph I of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I).Type: GrantFiled: July 29, 2015Date of Patent: August 28, 2018Assignee: BAYER PHARMA AGInventors: Johannes Platzek, Gunnar Garke, Alfons Grunenberg
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Patent number: 10051864Abstract: 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: August 24, 2017Date of Patent: August 21, 2018Assignee: SYNGENTA PARTICIPATIONS AGInventors: Andre Stoller, Andre Jeanguenat, Andrew Edmunds, Pierre Joseph Marcel Jung, Daniel Emery, Michel Muehlebach, Peter Renold
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Patent number: 10047085Abstract: 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: March 10, 2017Date of Patent: August 14, 2018Assignee: Vitae Pharmaceuticals, Inc.Inventors: David A. Claremon, Lawrence Wayne Dillard, Chengguo Dong, Yi Fan, Lanqi Jia, Zhijie Liu, 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: 10023571Abstract: The present invention provides compounds of formula I, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.Type: GrantFiled: September 1, 2016Date of Patent: July 17, 2018Assignee: Nimbus Lakshimi, Inc.Inventors: Craig E. Masse, Jeremy Robert Greenwood, Donna L. Romero, Geraldine C. Harriman, Ronald T. Wester, Mee Shelley, Joshua Jahmil Kennedy-Smith, Markus Dahlgren, Sayan Mondal, Shaughnessy Robinson
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Patent number: 10016402Abstract: Embodiments of the present invention are directed to methods for treatment of melanoma using an inhibitor of dihydroorotate dehydrogenase (DHODH) and to combination therapies that involve administering to a subject an inhibitor of oncogenic BRAF (e.g. BRAF(V600E)), as well as an inhibitor of dihydroorotate dehydrogenase (DHODH). Assays for identifying compounds useful for the treatment of melanoma are also provided. The methods comprise screening for compounds or agents that inhibit neural crest progenitor formation in a zebra fish model of melanoma.Type: GrantFiled: June 8, 2015Date of Patent: July 10, 2018Assignees: CHILDREN'S MEDICAL CENTER CORPORATION, DANA-FARBER CANCER INSTITUTE, INC.Inventors: Leonard Zon, Richard M. White
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Patent number: 10016401Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. 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: August 2, 2017Date of Patent: July 10, 2018Assignee: Celgene Quanticel Research, Inc.Inventors: Young K. Chen, Michael Brennan Wallace
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Patent number: 10005776Abstract: 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: October 22, 2015Date of Patent: June 26, 2018Assignee: Janssen Pharmaceutica NVInventors: George Hynd, Patrizia Tisselli, Janusz Jozef Kulagowski, Calum Macleod, Samuel Edward Mann, Stephen Colin Price, John Gary Montana
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Patent number: 10000501Abstract: The present invention concerns a compound of formula I or a pharmaceutically acceptable salt thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.Type: GrantFiled: September 23, 2015Date of Patent: June 19, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Jiaqiang Cai, Vincent Colandrea, Alejandro Crespo, John Debenham, Xiaoxing Du, Deodialsingh Guiadeen, Ping Liu, Rongqiang Liu, Christina B. Madsen-Duggan, Joshua G. McCoy, Weiguo Quan, Christopher Sinz, Liping Wang
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Patent number: 9994566Abstract: Disclosed are a compound of the following formula (I) or a pharmaceutically acceptable salt thereof, a preparation method thereof, pharmaceutical compositions and uses thereof in the preparation of a medicine for inhibiting HIF prolyl hydroxylase or a medicine for promoting the generation of endogenous EPO, wherein in the formula (I), R1 and R2 are each independently hydrogen; R3 is hydrogen or C1-3 alkyl; and Ar is an aromatic ring or an heteroaromatic ring selected from a naphthalene ring, a pyridine ring, a thiophene ring, a furan ring and a substituted benzene ring.Type: GrantFiled: December 14, 2015Date of Patent: June 12, 2018Assignee: SHENYANG SUNSHINE PHARMACEUTICAL CO. LTD.Inventors: Yunlong Zhou, Suixiong Cai, Guangfeng Wang, Lingling Jiao, Ping Min, Yu Jing, Ming Guo
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Patent number: 9980949Abstract: The present invention relates to SNS-595 and methods of treating cancer using the same.Type: GrantFiled: August 18, 2014Date of Patent: May 29, 2018Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Michelle Arkin, Jennifer Hyde, Duncan Walker, Jasmin Wright
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Patent number: 9981974Abstract: A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: (a) a phenyl-substituted imidazole, or a pharmaceutically acceptable salt or ester thereof; or (b) a compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; R21 is an alkanediyl or a substituted alkanediyl; a is 0 or 1; c is 0 or 1; X is C or S; R22 is a moiety that includes at least one divalent amino radical; and R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containingType: GrantFiled: March 13, 2017Date of Patent: May 29, 2018Assignee: University of Pittsburgh—Of the Commonwealth System of Higher EducationInventors: Zhou Wang, Joel Byron Nelson, Minh Bao Nguyen, John S. Lazo, Paul A. Johnston, Peter Wipf
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Patent number: 9957263Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided. The compounds are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Pharmaceutical compositions comprised of one or more compounds of formula (I) are also provided.Type: GrantFiled: June 27, 2014Date of Patent: May 1, 2018Assignee: AbbVie Inc.Inventors: Yujia Dai, Steven D. Fidanze, Lisa Hasvold, James Holms, Dachun Liu, William McClellan, Keith McDaniel, Jasmina Marjanovic, George Sheppard, Le Wang
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Patent number: 9951069Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g., HDAC2).Type: GrantFiled: January 11, 2018Date of Patent: April 24, 2018Assignee: Rodin Therapeutics, Inc.Inventors: Nathan Oliver Fuller, John A. Lowe, II
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Patent number: 9920018Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein X, Y, Z, R2, R3, R4, p and q are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: December 7, 2016Date of Patent: March 20, 2018Assignee: Gilead Sciences, Inc.Inventors: Michael Graupe, Yafan Lu, Jeff Zablocki
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Patent number: 9918969Abstract: The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.Type: GrantFiled: October 24, 2016Date of Patent: March 20, 2018Assignee: Bayer Pharma AktiengesellschaftInventors: Susanne Röhrig, Alexander Hillisch, Julia Straβburger, Stefan Heitmeier, Martina Victoria Schmidt, Karl-Heinz Schlemmer, Anja Buchmüller, Christoph Gerdes, Henrik Teller, Martina Schäfer, Adrian Tersteegen
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Patent number: 9918986Abstract: The present application relates to therapeutics and pharmaceutical compositions, their use and also methods for preventing post-traumatic osteoarthritis, early or late stage, using compounds which inhibit either, or both, AMPA and KA glutamate receptors (Glu Rs).Type: GrantFiled: July 3, 2014Date of Patent: March 20, 2018Assignee: UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITEDInventors: Deborah Mason, Cleo Bonnet
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Patent number: 9868744Abstract: The present invention provides, in part, compounds of Formula (I) and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.Type: GrantFiled: April 13, 2015Date of Patent: January 16, 2018Assignee: Pfizer Inc.Inventors: David Lawrence Firman Gray, Lei Zhang, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, Chewah Lee, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Chakrapani Subramanyam
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Patent number: 9868696Abstract: The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.Type: GrantFiled: December 28, 2015Date of Patent: January 16, 2018Assignee: Bezwada Biomedial, LLCInventor: Rao S Bezwada
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Patent number: 9862718Abstract: Sodium salt of (2S,5R)-6-benzyloxy-7-oxo-1,6-diaza-bicyclo[3.2.1]octane-2-carboxylic acid and a process for its preparation is disclosed.Type: GrantFiled: October 10, 2013Date of Patent: January 9, 2018Assignee: WOCKHARDT LIMITEDInventors: Vikas Vitthalrao Deshmukh, Amit Chandra Mishra, Dattatraya Vitthal Wani, Prasad Keshav Deshpande, Satish Bhavsar, Ravindra Dattatraya Yeole, Mahesh Vithalbhai Patel
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Patent number: 9839630Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.Type: GrantFiled: March 8, 2016Date of Patent: December 12, 2017Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Rahuman, Ramar Subbiah
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Patent number: 9833449Abstract: Compounds of formula (I): wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6alkyl; A is C—R5 or N; B is C—R6 or N; D is C—R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.Type: GrantFiled: November 15, 2016Date of Patent: December 5, 2017Assignee: GLAXO GROUP LIMITEDInventors: Stephen John Atkinson, Michael David Barker, Matthew Campbell, Hawa Diallo, Clement Douault, Neil Stuart Garton, John Liddle, Robert John Sheppard, Ann Louise Walker, Christopher Wellaway, David Matthew Wilson
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Patent number: 9815849Abstract: The invention provides compositions, methods, and kits for the treatment of acute myeloid leukemia in a subject.Type: GrantFiled: July 3, 2013Date of Patent: November 14, 2017Assignees: Dana-Farber Cancer Institute, Inc., Cold Spring Harbor LaboratoryInventors: James Elliott Bradner, Johannes Zuber, Junwei Shi, Christopher R. Vakoc, Scott W. Lowe, Constantine S. Mitsiades
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Patent number: 9796710Abstract: 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: September 27, 2016Date of Patent: October 24, 2017Assignee: 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: 9796708Abstract: Disclosed are compounds of Formula (IIa), wherein R1, R2, R3A, R3B, R3C, R3D, R3E, and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIa).Type: GrantFiled: March 13, 2014Date of Patent: October 24, 2017Assignee: AbbVie Inc.Inventors: Yunsong Tong, Milan Bruncko, Richard F. Clark, Michael Curtin, Alan S. Florjancic, Robin R. Frey, Jianchun Gong, Todd M. Hansen, Zhiqin Ji, Chunqiu Lai, Anthony Mastracchio, Michael Michaelides, Juliem Miyashiro, Roberto M. Risi, Xiaohong Song, Zhi-fu Tao, Keith W. Woods, Guidong Zhu, Thomas Penning, Andrew Souers, Rajeev Goswami, Omprakash Reddy Iguturi, Madhu Babu Dabbeeru
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Patent number: 9776999Abstract: The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.Type: GrantFiled: June 23, 2016Date of Patent: October 3, 2017Assignee: MERIAL INC.Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Douglas Edward Wilkinson, Brent Christopher Beck
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Patent number: 9775353Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts 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: July 2, 2015Date of Patent: October 3, 2017Assignee: Syngenta Participations AGInventors: Andre Stoller, Andre Jeanguenat, Andrew Edmunds, Pierre Joseph Marcel Jung, Daniel Emery, Michel Muehlebach, Peter Renold
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Patent number: 9757364Abstract: The invention relates to new naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: October 31, 2016Date of Patent: September 12, 2017Assignee: ASTEX THERAPEUTICS LTDInventors: Patrick René Angibaud, Michel Obringer, Julien Jérémie Joseph Marin, Matthieu Jeanty
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Patent number: 9758531Abstract: 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: September 12, 2017Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood