1,2 Diazine Attached Directly Or Indirectly To An Additional Hetero Ring By Nonionic Bonding Patents (Class 514/252.01)
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Patent number: 11135220Abstract: This disclosure provides, among other things, formulated oltipraz compositions comprising stabilized oltipraz crystals, for use in treating a patient who has a viral infection or is at risk of incurring a viral infection. Such viral infections can include a viral infection caused by a coronavirus such as one associated with MERS or SARS, e.g., SARS-CoV-2.Type: GrantFiled: April 9, 2020Date of Patent: October 5, 2021Assignee: ST IP Holding AGInventors: Bomi Framroze, Jeffrey A. Gelfand
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Patent number: 11103493Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.Type: GrantFiled: July 30, 2018Date of Patent: August 31, 2021Assignee: Merck Sharp & Dohme Corp.Inventors: Hua Zhou, Xavier Fradera, Yongxin Han, Meredeth A. McGowan, Nunzio Sciammetta, Catherine White, Wensheng Yu
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Patent number: 10647714Abstract: Disclosed herein are 5 or 8-substituted imidazo[1,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo[1,5-a]pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8-substituted imidazo[1,5-a]pyridines that can be useful for inhibiting indoleamine 2,3-dioxygenase and/or tryptophane 2,3-dioxygenase and for treating diseases or disorders mediated thereby.Type: GrantFiled: March 27, 2019Date of Patent: May 12, 2020Assignee: BEIGENE, LTD.Inventors: Hexiang Wang, Guoliang Zhang, Yunhang Guo, Bo Ren, Zhiwei Wang, Changyou Zhou
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Patent number: 10583088Abstract: Disclosed herein are compositions comprising a drug such as a triptan (e.g. rizatriptan) and/or an NSAID (e.g. meloxicam) in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability, solubility, or pharmacokinetics of the drug for the treatment of conditions such as pain.Type: GrantFiled: June 7, 2018Date of Patent: March 10, 2020Assignee: AXSOME THERAPEUTICS, INC.Inventor: Herriot Tabuteau
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Patent number: 10561726Abstract: Described herein are methods, formulations and kits for treating a patient with cancer with anti-VEGF antibodies and albumin-bound chemotherapeutic/anti-VEGF antibody nanoparticle complexes.Type: GrantFiled: April 6, 2016Date of Patent: February 18, 2020Assignees: Vavotar Life Sciences LLC, Mayo Foundation for Medical Education and ResearchInventors: Gerald F. Swiss, Svetomir N. Markovic, Wendy K. Nevala
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Patent number: 10471068Abstract: Disclosed herein are compositions comprising a drug such as a triptan (e.g. rizatriptan) and/or an NSAID (e.g. meloxicam) in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the drug for the treatment of conditions such as pain.Type: GrantFiled: May 10, 2018Date of Patent: November 12, 2019Assignee: AXSOME THERAPEUTICS, INC.Inventor: Herriot Tabuteau
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Patent number: 10471014Abstract: Disclosed herein are compositions comprising a drug such as a triptan (e.g. rizatriptan) and/or an NSAID (e.g. meloxicam) in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability, solubility, or pharmacokinetics of the drug for the treatment of conditions such as pain.Type: GrantFiled: June 6, 2018Date of Patent: November 12, 2019Assignee: AXSOME THERAPEUTICS, INC.Inventor: Herriot Tabuteau
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Patent number: 10357035Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, and especially fungicides.Type: GrantFiled: November 3, 2016Date of Patent: July 23, 2019Assignee: Syngenta Participations AGInventors: Werner Zambach, Clemens Lamberth, Martin Pouliot, Stefano Rendine, Mathias Blum
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Patent number: 10266544Abstract: The invention relates to aryl substituted aminomethyl spectinomycin analogs, derivatives thereof, and related compounds, which are useful as anti-bacterial agents; methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating anti-bacterial infections using the compounds and compositions.Type: GrantFiled: September 29, 2014Date of Patent: April 23, 2019Assignee: St. Jude Children's Research Hospital, Inc.Inventors: Richard E. Lee, Samanthi L. Waidyarachchi, David F. Bruhn, Jiuyu Liu, Zhong Zheng, Jason W. Rosch
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Patent number: 10266497Abstract: Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of monoacylglycerol lipase (MAGL). Furthermore, the subject compounds and compositions are useful for the treatment of pain.Type: GrantFiled: May 22, 2018Date of Patent: April 23, 2019Assignee: ABIDE THERAPEUTICS, INC.Inventors: Cheryl A. Grice, John J. M. Wiener, Olivia D. Weber, Katharine K. Duncan
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Patent number: 10143696Abstract: Disclosed in certain embodiments is a method of decreasing gastric emptying comprising administering to a subject an effective amount of a sodium-channel blocker to decrease gastric emptying.Type: GrantFiled: August 18, 2017Date of Patent: December 4, 2018Assignee: Purdue Pharma L.P.Inventors: Michele Hummel, Donald J. Kyle, Garth Whiteside, Nathan Lautermilch
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Patent number: 10125111Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus, (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: February 17, 2016Date of Patent: November 13, 2018Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Zhiwei Yin, Zhongxing Zhang, John F. Kadow
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Patent number: 10053469Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: September 30, 2016Date of Patent: August 21, 2018Assignees: GILEAD CONNECTICUT, INC., GENENTECH INC.Inventors: Antonio J. M. Barbosa, Peter A. Blomgren, Kevin S. Currie, Ravi Krishnamoorthy, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Daniel Ortwine, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Wendy Young, Honglu Zhang, Zhongdong Zhao, Pavel E. Zhichkin
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Patent number: 10043656Abstract: Methods and apparatuses for selectively depositing silicon-containing dielectric or metal-containing dielectric material on silicon or metal surfaces selective to silicon oxide or silicon nitride materials are provided herein. Methods involve exposing the substrate to an acyl chloride which is reactive with the silicon oxide or silicon nitride material where deposition is not desired to form a ketone structure that blocks deposition on the silicon oxide or silicon nitride material. Exposure to the acyl chloride is performed prior to deposition of the desired silicon-containing dielectric material or metal-containing dielectric material.Type: GrantFiled: March 10, 2017Date of Patent: August 7, 2018Assignee: Lam Research CorporationInventors: David Charles Smith, Dennis M. Hausmann
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Patent number: 10004782Abstract: The present invention relates to pharmaceutical compositions comprising {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid (FRI-1) in combination with an anti-diabetic drug selected from the group consisting of metformin, sitagliptin or exenatide. The present invention also relates to the use of the pharmaceutical compositions in restoring insulin sensitivity and treating type II diabetes, including reducing body weight in subjects undergoing type II diabetes treatment.Type: GrantFiled: November 5, 2013Date of Patent: June 26, 2018Assignee: vTv Therapeutics LLCInventors: Maria Carmen Valcarce Lopez, Tung Fong
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Patent number: 9943522Abstract: The present invention relates to the use of cathepsin K and/or cathepsin S inhibitors in a method for the treatment and/or prophylaxis of pulmonary hypertension and/or heart failure.Type: GrantFiled: May 11, 2012Date of Patent: April 17, 2018Assignee: BAYER INTELLECTUAL PROPERTY GMBHInventors: Stefan Golz, Martina Delbeck, Heinrich Meier, Andreas Geerts, Thomas Mondritzki, Hubert Trübel
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Patent number: 9738653Abstract: The disclosure provides compounds of formula I or II, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: March 12, 2014Date of Patent: August 22, 2017Assignee: Bristol-Myers Squibb CompanyInventors: Kap-Sun Yeung, Kyle J. Eastman, Kyle E. Parcella
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Patent number: 9717728Abstract: A pharmaceutical combination comprising (a) a B-Raf inhibitor and (b) a histone deacetylase inhibitor; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.Type: GrantFiled: November 8, 2013Date of Patent: August 1, 2017Assignee: Novartis AGInventors: Stuart John Gallagher, Peter Hersey
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Patent number: 9598399Abstract: Provided is a compound represented by formula (1-0): wherein in formula (1-0), R represents —O(CH2)n—, —O(CH2)nOC2H4—, —CH2O(CH2)n— or —CH2O(CH2)nOC2H4—; n represents an integer from 1 to 5; and Q1 represents F or —OCH3.Type: GrantFiled: August 22, 2013Date of Patent: March 21, 2017Assignee: HAMAMATSU PHOTONICS K.K.Inventors: Shingo Nishiyama, Norihiro Harada, Hideo Tsukada
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Patent number: 9556139Abstract: Provided herein are compounds of Formula I: in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, which are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: GrantFiled: May 4, 2015Date of Patent: January 31, 2017Assignee: Array BioPharma Inc.Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff, Ganghyeok Kim
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Patent number: 9505785Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: October 22, 2013Date of Patent: November 29, 2016Assignees: Gilead Connecticut, Inc., Genentech, Inc.Inventors: Antonio J. M. Barbosa, Peter A. Blomgren, Kevin S. Currie, Ravi Krishnamoorthy, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Daniel Ortwine, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Wendy Young, Honglu Zhang, Zhongdong Zhao, Pavel E. Zhichkin
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Patent number: 9475811Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.Type: GrantFiled: December 3, 2014Date of Patent: October 25, 2016Assignee: Novartis AGInventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas Troxler, Konstanze Hurth, Mathias Frederiksen
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Patent number: 9399645Abstract: Compounds of formula (I) and pharmaceutical compositions thereof: wherein A1 A2 and A3 are each independently selected from the group consisting of N and CR3, wherein R1 is an optionally substituted heterocyclyl or an optionally substituted —(C1-6)alkyl-heterocyclyl, R2 is an optionally substituted aryl or an optionally subsisted heteroaryl, R4 is an optionally substituted aryl, an optionally substituted heterocyclyl or an optionally substituted heteroaryl, useful as an inhibitor of HIV replication.Type: GrantFiled: December 19, 2012Date of Patent: July 26, 2016Assignee: Boehringer Ingelheim International GmbHInventors: Claudio Sturino, Pierre Beaulieu, Patrick Deroy, Martin Duplessis, Clint James, Jean-Eric Lacoste, Joannie Minville, Louis Morency, Sébastien Morin, Bruno Simoneau, Martin Tremblay
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Patent number: 9353060Abstract: 4,6-Dibromo-3-hydroxypicolinate esters are prepared from furan-2-yl aminoacetates in one chemical step by use of a bromination-rearrangement reaction.Type: GrantFiled: July 7, 2015Date of Patent: May 31, 2016Assignee: Dow AgroSciences LLCInventor: James M. Renga
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Patent number: 9249152Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth.Type: GrantFiled: March 20, 2015Date of Patent: February 2, 2016Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Kyle J. Eastman, Zhongxing Zhang, Kyle E. Parcella, Zhiwei Yin, John F. Kadow
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Patent number: 9206181Abstract: The present invention related to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5, R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: (Ia) in free base or acid addition salt form, to processes for their production, to pharmaceutical compositions comprising them and their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and neurodegenerative disorders.Type: GrantFiled: May 23, 2014Date of Patent: December 8, 2015Assignee: Novartis AGInventors: Mathias Frederiksen, Dominik Feuerbach, Konstanze Hurth, Manuel Koller, Bernard Lucien Roy
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Patent number: 9115152Abstract: Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating cancer mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of cancer in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: December 11, 2014Date of Patent: August 25, 2015Assignee: GENENTECH, INC.Inventors: James John Crawford, Wendy B. Young
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Patent number: 9096567Abstract: Provided herein is a method of treating an allergic inflammatory disease selected from asthma, dermatitis, allergic rhinitis, urticaria, anaphylaxis, angioedemea, allergies, contact hypersensitivity, drug hypersensitivity, and allergic conjunctivitis in a mammal, comprising administering a therapeutically effective amount of a compound of Formula I or a pharmaceutically acceptable salt thereof, to said mammal in need thereof, wherein A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 are as defined herein.Type: GrantFiled: March 31, 2014Date of Patent: August 4, 2015Assignee: Array BioPharma Inc.Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff, Ganghyeok Kim
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Patent number: 9028876Abstract: Rate-controlled particles, comprising compounds of the formula as a solid dispersion.Type: GrantFiled: March 14, 2012Date of Patent: May 12, 2015Assignee: Janssen R&D IrelandInventors: Thomas Hantke, Bettina Rehbock, Jörg Rosenberg, Jörg Breitenbach
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Patent number: 8987272Abstract: The invention relates to a compound of Formulae I and/or II: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof; X is selected from Se, N—OH, NH, NO2, CN, N—CN, N?O, O or S, and the remaining substituents are described herein; and a composition thereof. The invention also relates to a method of administration thereof; and use thereof to treat HIV.Type: GrantFiled: April 1, 2011Date of Patent: March 24, 2015Assignee: Critical Outcome Technologies Inc.Inventors: Wayne Danter, Clinton Threlfall, Sylvain Guizzetti, Julien Marin
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Patent number: 8975296Abstract: The instant invention relates to pharmaceutical compositions containing cathespin K inhibitors. Also disclosed are processes for making said pharmaceutical compositions.Type: GrantFiled: March 20, 2013Date of Patent: March 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Haihong Fan, Majid Mahjour, Justin Moser, Bhagwant Rege
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Publication number: 20150065500Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: September 11, 2014Publication date: March 5, 2015Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
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Publication number: 20150057281Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.Type: ApplicationFiled: October 29, 2014Publication date: February 26, 2015Inventors: Johnson LAU, Jiann-Jyh HUANG
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Patent number: 8946225Abstract: The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: —R1 represents one or more groups such as: trifluoromethyl, halogen such as F, Cl, —when n=m=1, W represents CH then Y represents oxygen, —U represents: •either —(C?O)CH2NH— and is branched at position 4 of pyridazinone, then R2 represents H, •or —(C?O)NH— and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, —R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enzyme inhibitors for the treatment of obesity, type-2 diabetes and lipid disorders.Type: GrantFiled: August 5, 2010Date of Patent: February 3, 2015Assignee: Pierre Fabre MedicamentInventors: Elisabeth Dupont-Passelaigue, Samuel Mialhe, Jean-Pierre Rieu, Didier Junquero, Karine Valeille
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Publication number: 20150030704Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 21, 2012Publication date: January 29, 2015Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: William Farnaby, Charlotte Fieldhouse, Katherine Hazel, Catrina Kerr, Natasha Kinsella, David Livermore, Kevin Merchant, David Miller
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Patent number: 8940774Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.Type: GrantFiled: November 26, 2013Date of Patent: January 27, 2015Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Patent number: 8933079Abstract: Pyridone and pyridazinone derivatives that are active against the melanin-concentrating hormone (MCH) and useful as anti-obesity pharmaceuticals.Type: GrantFiled: February 28, 2013Date of Patent: January 13, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Thorsten Oost, Ralf Lotz, Dirk Stenkamp
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Publication number: 20140371230Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: June 25, 2014Publication date: December 18, 2014Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear
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Patent number: 8877747Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.Type: GrantFiled: October 21, 2009Date of Patent: November 4, 2014Assignee: Korea Research Institute of Chemical TechnologyInventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
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Patent number: 8853213Abstract: The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.Type: GrantFiled: December 29, 2011Date of Patent: October 7, 2014Assignee: Hanmi Pharm. Co., LtdInventors: Jung Beom Son, Nam Du Kim, Young Kil Chang, Hee Cheol Kim, Ji Sook Kim, Young Hee Jung
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Patent number: 8853211Abstract: Compounds of the formula (I) in which D, R1, R2, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: December 10, 2009Date of Patent: October 7, 2014Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
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Patent number: 8841449Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: GrantFiled: November 9, 2012Date of Patent: September 23, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven John Durrant, Ronald Knegtel
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Patent number: 8829199Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.Type: GrantFiled: August 5, 2010Date of Patent: September 9, 2014Assignees: Chugai Seiyaku Kabushiki Kaisha, F. Hoffmann-La Roche AGInventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
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Publication number: 20140249155Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.Type: ApplicationFiled: March 23, 2014Publication date: September 4, 2014Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONInventors: Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, VNR Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
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Publication number: 20140243349Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.Type: ApplicationFiled: February 21, 2014Publication date: August 28, 2014Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
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Patent number: 8815864Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: GrantFiled: November 25, 2013Date of Patent: August 26, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Elke Langkopf, Holger Wagner
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Publication number: 20140227302Abstract: Disclosed herein are compounds of Formula (I) (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.Type: ApplicationFiled: September 4, 2012Publication date: August 14, 2014Inventors: Wen-Lian Wu, Duane A. Burnett
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Publication number: 20140221376Abstract: Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.Type: ApplicationFiled: April 9, 2014Publication date: August 7, 2014Applicant: Xcovery Holding Company, LLCInventors: Congxin Liang, Zhigang Li
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Patent number: 8796271Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: August 11, 2011Date of Patent: August 5, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Patent number: 8785445Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.Type: GrantFiled: December 18, 2009Date of Patent: July 22, 2014Assignee: Array BioPharma Inc.Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess