At 4- Or 6-position Patents (Class 544/326)
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Patent number: 11021475Abstract: Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition.Type: GrantFiled: November 18, 2019Date of Patent: June 1, 2021Assignee: Bristol-Myers Squibb CompanyInventors: Ryan M. Moslin, David S. Weinstein, Stephen T. Wrobleski
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Patent number: 10774090Abstract: The present invention discloses a compound comprising the formula: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CH2 or O, and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.Type: GrantFiled: January 22, 2019Date of Patent: September 15, 2020Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
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Patent number: 10342796Abstract: Disclosed in the present invention are an acrylanilide compound represented by general formula (I) and a pharmaceutically acceptable salt thereof. The acrylanilide compound and the pharmaceutically acceptable salt thereof are used for treating clinical diseases by mainly acting on EGFR family casein kinases.Type: GrantFiled: December 30, 2016Date of Patent: July 9, 2019Assignee: Ancureall Pharmaceutical (Shanghai) Co., Ltd.Inventors: Jutong Si, Guan Wang, Zhihe Yang, Meifeng Jiang, Benpo Xu, Chentao Zhou
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Patent number: 10028961Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.Type: GrantFiled: April 7, 2016Date of Patent: July 24, 2018Assignee: Agios Pharmaceuticals, Inc.Inventors: Zenon D. Konteatis, Janeta Popovici-Muller, Jeremy M. Travins, Robert Zahler, Zhenwei Cai, Ding Zhou
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Patent number: 9725418Abstract: Provided are a pyrimidine compound represented by formula (1) having excellent harmful pest-exterminating potency, a harmful pest-exterminating agent comprising the compound and an inert carrier, and a method for exterminating harmful pests whereby the effective dose of the compound is used on harmful pests or on areas where harmful pests grow.Type: GrantFiled: March 16, 2015Date of Patent: August 8, 2017Assignee: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Hideki Uneme, Ganesh Balkrishna Salunke
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Patent number: 9695154Abstract: Disclosed are compounds of formula (I); or a pharmaceutically acceptable salt thereof; wherein Y, Ra, Ra?, Rc, Rf, X2, Rd, Rd?, Re, Re?, m, and G have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry, useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular and neurodegenerative diseases or disorders.Type: GrantFiled: July 1, 2014Date of Patent: July 4, 2017Assignee: Millennium Pharmaceuticals, Inc.Inventors: Matthew O. Duffey, Dylan B. England, Zhigen Hu, Mitsuhiro Ito, Steven P. Langston, Charles McIntyre, Hirotake Mizutani, He Xu
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Patent number: 9586940Abstract: The present invention provides a method of treating breast cancer that is nonresponsive to treatment with trastuzumab, comprising administering to a subject in need of such treatment a therapeutically effective amount of compound N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 16, 2015Date of Patent: March 7, 2017Assignee: KADMON CORORATION, LLCInventors: Samuel Waksal, Lillian Chiang
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Patent number: 9296704Abstract: The present invention provides 4,6-diaminopyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: June 4, 2014Date of Patent: March 29, 2016Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Patent number: 9260415Abstract: Heteroaryl pyridone and aza-pyridone amide compounds with electrophilic functionality of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk, and for treating cancer and immune disorders such as inflammation mediated by Btk. 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: December 4, 2014Date of Patent: February 16, 2016Assignee: Genentech, Inc.Inventors: James John Crawford, BinQing Wei, Wendy B. Young
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Patent number: 9006249Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: June 7, 2012Date of Patent: April 14, 2015Assignee: Novartis AGInventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Patent number: 8993757Abstract: The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.Type: GrantFiled: September 14, 2012Date of Patent: March 31, 2015Assignee: Merck Sharp & Dohme B.V.Inventors: Ines Huisman, Marcelis Van Der Stelt, Wouter Wiedenhof, Charles Anthony Graham Baker-Glenn, Wesley Peter Blackaby, Naimisha Trivedi
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Patent number: 8980871Abstract: Provided herein are methods of treating hemolysis by administering an active compound in an amount sufficient to treat said hemolysis. It has been found that nitroxyl donors or similar compounds preferentially react with cell-free OxyHb, as compared to OxyHb encapsulated in a red blood cell, and reacts with MetHb to form iron-nitrosyl Hb or nitrite bound MetHb. It has also been found that such compounds reduce cell-free Hb and hemolysis. Active compounds are also contemplated for use in combination therapies, for example, in combination with the administration of red blood cells and/or an agent that promotes hematopoiesis, or in combination with the administration of a nitric oxide donor.Type: GrantFiled: September 19, 2008Date of Patent: March 17, 2015Assignees: Wake Forest University Health Sciences, The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Daniel B. Kim-Shapiro, S. Bruce King, Daniel A. Sweeney, Mark T. Gladwin
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Patent number: 8975249Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: October 31, 2011Date of Patent: March 10, 2015Assignee: Celgene Avilomics Research, Inc.Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Matthew F. Baevsky, Juswinder Singh
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Patent number: 8962641Abstract: The invention relates to new pyrrolidine derivatives of the formula wherein R1 to R3, Ar, L T and n are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: April 7, 2014Date of Patent: February 24, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Annekatrin Heimann, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
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Patent number: 8933090Abstract: 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: October 19, 2010Date of Patent: January 13, 2015Assignee: Novartis AGInventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
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Patent number: 8906914Abstract: Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.Type: GrantFiled: August 17, 2010Date of Patent: December 9, 2014Assignee: Janssen Pharmaceutica NVInventors: Natalie A. Hawryluk, J. Guy Breitenbucher, William M. Jones, Alison L. Chambers, John M. Keith, Mark Seierstad
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Publication number: 20140350251Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation wherein R1 is cyclopropyl optionally substituted with 1-5 R5, isopropyl optionally substituted with 1-5 R6, or phenyl optionally substituted with 1-3 R7; R2 is ((O)jC(R15)(R16))kR; R is CO2H or a herbicidally effective derivative of CO2H; R3 is halogen, cyano, nitro, OR20, SR21 or N(R22)R23; R4 is —N(R24)R25 or —NO2; j is 0 or 1; and k is 0 or 1; provided that when k is 0, then j is 0; and R5, R6, R7, R15, R16, R20, R21, R22, R23, R24 and R25 are as defined in the disclosure. Also disclosed are compositions comprising the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.Type: ApplicationFiled: August 8, 2014Publication date: November 27, 2014Inventors: DAVID ALAN CLARK, BRUCE LAWRENCE FINKELSTEIN, GREGORY RUSSELL ARMEL, VERNON ARIE WITTENBACH
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Patent number: 8883785Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: GrantFiled: January 20, 2011Date of Patent: November 11, 2014Assignee: CHDI Foundation, Inc.Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Dirk Winkler, Frederick Brookfield, Paula C. De Aguiar Pena
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Publication number: 20140329795Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: August 28, 2012Publication date: November 6, 2014Inventors: Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson, Celia Dominguez, Leticia M. Toledo-Sherman, Ignacio Munoz
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Patent number: 8877745Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.Type: GrantFiled: May 10, 2011Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
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Publication number: 20140291646Abstract: A pyrene-based compound and an organic light-emitting diode including the same, the pyrene-based compound being represented by Formula 1, below:Type: ApplicationFiled: March 25, 2014Publication date: October 2, 2014Applicant: Samsung Display Co., Ltd.Inventors: Dong-Woo SHIN, O-Hyun KWON, Mie-Hwa PARK, Seul-Ong KIM, Byoung-Ki CHOI
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Publication number: 20140288067Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: Epizyme, Inc.Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
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Publication number: 20140275123Abstract: Various aspects disclosed herein relate to aryl substituted aminopyrimidines according to Formula 1: wherein, X1 is N or C—R3; X2 is N or C—R4 provided that X1 and X2 are not both N; R1-R7 are H, CN, CHO, —SCN, NO2, F, Cl, Br, I, substituted or unsubstituted C1-C4-alkyl, substituted or unsubstituted halo-C1-C4-alkyl, substituted or unsubstituted C1-C4-alkoxy, substituted or unsubstituted halo-C1-C4-alkoxy, substituted or unsubstituted C1-C4-thioalkyl, substituted or unsubstituted halo-C1-C4-thioalkyl, substituted or unsubstituted C3-C-7-cycloalkyl, substituted or unsubstituted C2-C4-alkenyl, C2-C4-alkynyl, substituted or unsubstituted C1-C4-acylalkyl, C1-C4-acyloxy, C1-C4 alkoxycarbonyl, C1-C4-alkoxy-amino, C1-C4-alkyl-S(O)?NH, substituted or unsubstituted aryl, substituted or unsubstituted heterocycle, wherein the substituents are one or more of the following F, Cl, Br, OH, CN, NO2, CHO, —SCN, S(O)n-C1-C4-alkyl (where n=0-2), C1-C4-alkyl, halo-C1-C4-alkyl, C1-C4-alkylamine, C1-C4-alkoxy, halo-C1-C4-alkoxType: ApplicationFiled: May 28, 2014Publication date: September 18, 2014Inventors: Francis Tisdell, JR., James M. Renga, David H. Young, George E. Davis, William C. Lo, Maurice C.H. Yap
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Publication number: 20140275536Abstract: The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): or one of its pharmaceutically acceptable salts, solvates or hydrates in the preparation of a medicament to treat skin pathologies is described.Type: ApplicationFiled: December 22, 2010Publication date: September 18, 2014Applicant: Galderma Research & DevelopmentInventor: Cédric Poinsard
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Patent number: 8796283Abstract: This invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I): or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 14, 2010Date of Patent: August 5, 2014Assignee: Proximagen LimitedInventors: Kevin Dinnell, Andrew Lightfoot, Gillian Elizabeth Lunniss
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Patent number: 8796284Abstract: New 4-amino-pyrimidine derivatives as potent antagonists of the adenosine A2a receptor formula (I): (I) The invention provides as well a method for preparing such compounds, pharmaceutical compositions comprising an effective amount of these compounds and the use of such compounds in the manufacture of a medicament to treat pathological affections that can be improved by antagonism of the adenosine A2a receptor.Type: GrantFiled: March 29, 2011Date of Patent: August 5, 2014Assignee: Palobiofarma, S.L.Inventors: Juan Alberto Camacho Gomez, Julio Cesar Castro-Palomino Laria
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Patent number: 8785630Abstract: The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.Type: GrantFiled: February 6, 2013Date of Patent: July 22, 2014Assignee: Vestaron CorporationInventors: Robert M. Kennedy, Bruce A. Steinbaugh
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Patent number: 8765949Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.Type: GrantFiled: December 16, 2010Date of Patent: July 1, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Heiner Ebel, Sara Frattini, Kai Gerlach, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Marco Santagostino, Stefan Scheuerer, Christofer Tautermann, Thomas Trieselmann
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Patent number: 8765749Abstract: Disclosed are a 1,6-substituted indole compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of cancers caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel indole compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.Type: GrantFiled: October 20, 2010Date of Patent: July 1, 2014Assignee: Korea Institute of Science and TechnologyInventors: Tae Bo Sim, Young Jin Ham, Kyung Ho Yoo, Chang Hyun Oh, Jung Mi Hah, Hwan Geun Choi, Hwan Kim, Eun Jin Jun
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Patent number: 8759356Abstract: Various aspects disclosed herein relate to aryl substituted aminopyrimidines according to Formula 1: wherein, X1 is N or C—R3; X2 is N or C—R4 provided that X1 and X2 are not both N; R1-R7 are H, CN, CHO, —SCN, NO2, F, Cl, Br, I, substituted or unsubstituted C1-C4-alkyl, substituted or unsubstituted halo-C1-C4-alkyl, substituted or unsubstituted C1-C4-alkoxy, substituted or unsubstituted halo-C1-C4-alkoxy, substituted or unsubstituted C1-C4-thioalkyl, substituted or unsubstituted halo-C1-C4-thioalkyl, substituted or unsubstituted C3-C-7-cycloalkyl, substituted or unsubstituted C2-C4-alkenyl, C2-C4-alkynyl, substituted or unsubstituted C1-C4-acylalkyl, C1-C4-acyloxy, C1-C4 alkoxycarbonyl, C1-C4-alkoxy-amino, C1-C4-alkyl-S(O)?NH, substituted or unsubstituted aryl, substituted or unsubstituted heterocycle, wherein the substituents are one or more of the following F, Cl, Br, OH, CN, NO2, CHO, —SCN, S(O)n-C1-C4-alkyl (where n=0-2), C1-C4-alkyl, halo-C1-C4-alkyl, C1-C4-alkylamine, C1-C4-alkoxy, halo-C1-C4-alkoxType: GrantFiled: May 3, 2010Date of Patent: June 24, 2014Assignee: Dow AgroSciences, LLC.Inventors: Francis E. Tisdell, James M. Renga, William C. Lo, Maurice C. H. Yap, David H. Young, George E. Davis
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Patent number: 8748606Abstract: The present invention provides 4,6-diaminopyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: November 9, 2012Date of Patent: June 10, 2014Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Patent number: 8686143Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: October 25, 2011Date of Patent: April 1, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Francesco Salituro, Albert Pierce, Alex Aronov, Gabriel Martinez-Botella, Jian Wang, Luc Farmer, Mark Ledeboer, Tiansheng Wang, Randy Bethiel, Brian Ledford, Emilie Porter Huck
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Publication number: 20140080848Abstract: A series of mono- and di-substituted quinazoline and pyrimidine derivatives based on the skeleton of erlotinib (an EGFR inhibitor) were synthesized and their bioactivities against hepatocellular carcinoma and human lung adenocarcinoma were evaluated.Type: ApplicationFiled: September 13, 2013Publication date: March 20, 2014Applicants: National Taiwan University, National Yang-Ming UniversityInventors: Chung-Wai SHIAU, Kuen-Feng CHEN
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Publication number: 20140057911Abstract: Certain 4,6-disubstituted aminopyrimidine derivatives having both aromatic and halogenic substituents.Type: ApplicationFiled: August 23, 2013Publication date: February 27, 2014Inventors: Franco Lori, James Chafouleas, Davide De Forni, Antonio Solinas, Zoltán Varga, Zoltán Greff, László Örfi, György Kéri
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Publication number: 20140031355Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.Type: ApplicationFiled: November 4, 2011Publication date: January 30, 2014Applicant: Amgen Inc.Inventor: Amy Kaizerman
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Patent number: 8618111Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: January 24, 2011Date of Patent: December 31, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Siegfried Schneider, Dirk Kessler, Lars van der Veen, Tobias Wunberg
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Patent number: 8586505Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.Type: GrantFiled: July 15, 2010Date of Patent: November 19, 2013Assignee: SDS Biotech K. K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Ryutaro Katsuki, Tomoko Muraki
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Patent number: 8575338Abstract: A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R1 is independently halogen, cyano, etc., each of X1, X2 and X3 is CR2 or nitrogen, R2 is independently hydrogens, etc., n is 0, 1, 2, 3 or 4; -D-Y is —O—CH2COOH, etc, and G is a substituted amino, a substituted heterocyclic group, etc, or a pharmaceutical acceptable salt thereof, has activities of opening BK channels.Type: GrantFiled: April 8, 2009Date of Patent: November 5, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Yasuyuki Tsuzuki, Miki Hirai
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Patent number: 8563715Abstract: [Problem] To provide a prophylactic/therapeutic agent against, for example, nerve diseases and the like such as ischemic brain disease and neurodegenerative disease, or a prophylactic/therapeutic agent against diseases against which antioxidant action is effective, as a cell protecting agent, in particular as an inhibitor of brain cell damage or brain cell death.Type: GrantFiled: March 31, 2009Date of Patent: October 22, 2013Assignee: Zenyaku Kogyo KabushikikaishaInventors: Takeshi Nagata, Toshiaki Suzuki, Akira Yoshimura, Naoto Tadano, Toshiyuki Matsuno, Hideki Satoh, Kenichi Saitoh, Soichi Ohta
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Patent number: 8524710Abstract: The invention relates to a compound of formula (I) wherein A1 to A4 and R1 to R6 are defined as in the description and in the claims. The compound of formula (I) can be used, for example, as inhibitors of the cysteine protease cathepsin.Type: GrantFiled: October 24, 2011Date of Patent: September 3, 2013Assignee: Hoffmann-La Roche Inc.Inventors: David Banner, Uwe Grether, Wolfgang Haap, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
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Publication number: 20130217688Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: May 2, 2013Publication date: August 22, 2013Applicant: Celgene Avilomics Research, Inc.Inventor: Celgene Avilomics Research, Inc.
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Patent number: 8445498Abstract: The present invention provides 4,6-disubstituted pyrimidine compound useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: February 1, 2011Date of Patent: May 21, 2013Assignee: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Publication number: 20130123270Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.Type: ApplicationFiled: March 26, 2012Publication date: May 16, 2013Applicant: Millennium Pharmaceuticals, Inc.Inventors: Kenneth G. Carson, Prakash Raman, Francois Soucy, Qing Ye, Shomir Ghosh
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Patent number: 8431580Abstract: 4-Aminopyrimidine derivatives of formula (I) that are useful as histamine H4 receptor antagonists.Type: GrantFiled: December 18, 2008Date of Patent: April 30, 2013Assignee: Palau Pharma, S.A.Inventors: Elena Carceller González, Eva Maria Medina Fuentes, Robert Soliva Soliva, Marina Virgili Bernadó, Josep Martí Via
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Patent number: 8431573Abstract: The invention relates to novel cyanopyrimidinones, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory.Type: GrantFiled: May 2, 2011Date of Patent: April 30, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Martin Hendrix, Lars Bärfacker, Heike Heckroth, Dagmar Karthaus, Adrian Tersteegen
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Publication number: 20130102782Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).Type: ApplicationFiled: July 3, 2012Publication date: April 25, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Gerald J. Tanoury, Young Chun Jung, Derek Magdziak, Adam Looker, Billie J. Kline, Václav Jurcík, Beatriz Dominguez Olmo
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Patent number: 8426433Abstract: This invention relates to new chemical compounds, application of these compounds as anticoagulants, pharmaceutical compositions, and plasma-substituting solutions on their basis, and can be used for treating thromboembolic complications of diseases such as myocardial infarction, stroke, and thrombosis of deep veins or a pulmonary artery; and for preventing hypercoagulation conditions in consequence of injuries, surgeries, sepsis, various obstetric pathologies, in disaster medicine, resuscitation, and so on.Type: GrantFiled: June 27, 2008Date of Patent: April 23, 2013Assignee: Obschestvo S Ogranichennoi Otvetsttvennoctiyu “Bionika”Inventors: Elena Ivanovna Sinauridze, Fazoil Inoyatovich Ataullakhanov, Andrey Alexandrovich Butylin, Vladimir Borisovich Sulimov, Alexey Nickolayevich Romanov, Alexey Alexeevich Bogolyubov, Yury Vladimirovich Kuznetsov, Irina Vladimirovna Gribkova, Alexander Sergeevich Gorbatenko, Olga Anatolievna Kondakova
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Publication number: 20130090338Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.Type: ApplicationFiled: May 10, 2011Publication date: April 11, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
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Patent number: 8389521Abstract: The present invention provides new compounds. The compounds are useful as CDK5 inhibitors, and accordingly they can be included in pharmaceuticals compositions for treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases. formula (I).Type: GrantFiled: April 24, 2008Date of Patent: March 5, 2013Assignee: Ingenium Pharmaceuticals GmbHInventors: Heike Schauerte, Hans Allgeier, Michael A. Pleiss, Martin Augustin, Gisela Peraus, Gabriele Stumm, Philipp Wabnitz
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Patent number: 8367825Abstract: The present invention is directed to substituted pyrimidine compounds of formula (I): and forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.Type: GrantFiled: February 28, 2012Date of Patent: February 5, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Xu Guozhang, Lily Lee, Terry V. Hughes, Steven K. Wetter, Peter J. Connolly, Marta C. Abad, Stuart L. Emanuel, Prabha S. Kamachi, Steven A. Middleton, Kathleen A. Battista, Gilles C. Bignan