At 4- Or 6-position Patents (Class 544/326)
  • Patent number: 10342796
    Abstract: 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: Grant
    Filed: December 30, 2016
    Date of Patent: July 9, 2019
    Assignee: Ancureall Pharmaceutical (Shanghai) Co., Ltd.
    Inventors: Jutong Si, Guan Wang, Zhihe Yang, Meifeng Jiang, Benpo Xu, Chentao Zhou
  • Patent number: 10028961
    Abstract: 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: Grant
    Filed: April 7, 2016
    Date of Patent: July 24, 2018
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Zenon D. Konteatis, Janeta Popovici-Muller, Jeremy M. Travins, Robert Zahler, Zhenwei Cai, Ding Zhou
  • Patent number: 9725418
    Abstract: 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: Grant
    Filed: March 16, 2015
    Date of Patent: August 8, 2017
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Hideki Uneme, Ganesh Balkrishna Salunke
  • Patent number: 9695154
    Abstract: 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: Grant
    Filed: July 1, 2014
    Date of Patent: July 4, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Matthew O. Duffey, Dylan B. England, Zhigen Hu, Mitsuhiro Ito, Steven P. Langston, Charles McIntyre, Hirotake Mizutani, He Xu
  • Patent number: 9586940
    Abstract: 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: Grant
    Filed: July 16, 2015
    Date of Patent: March 7, 2017
    Assignee: KADMON CORORATION, LLC
    Inventors: Samuel Waksal, Lillian Chiang
  • Patent number: 9296704
    Abstract: The present invention provides 4,6-diaminopyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: June 4, 2014
    Date of Patent: March 29, 2016
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
  • Patent number: 9260415
    Abstract: 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: Grant
    Filed: December 4, 2014
    Date of Patent: February 16, 2016
    Assignee: Genentech, Inc.
    Inventors: James John Crawford, BinQing Wei, Wendy B. Young
  • Patent number: 9006249
    Abstract: 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: Grant
    Filed: June 7, 2012
    Date of Patent: April 14, 2015
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Patent number: 8993757
    Abstract: 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: Grant
    Filed: September 14, 2012
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Ines Huisman, Marcelis Van Der Stelt, Wouter Wiedenhof, Charles Anthony Graham Baker-Glenn, Wesley Peter Blackaby, Naimisha Trivedi
  • Patent number: 8980871
    Abstract: 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: Grant
    Filed: September 19, 2008
    Date of Patent: March 17, 2015
    Assignees: Wake Forest University Health Sciences, The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Daniel B. Kim-Shapiro, S. Bruce King, Daniel A. Sweeney, Mark T. Gladwin
  • Patent number: 8975249
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: March 10, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Matthew F. Baevsky, Juswinder Singh
  • Patent number: 8962641
    Abstract: 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: Grant
    Filed: April 7, 2014
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Annekatrin Heimann, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Patent number: 8933090
    Abstract: 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: Grant
    Filed: October 19, 2010
    Date of Patent: January 13, 2015
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
  • Patent number: 8906914
    Abstract: 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: Grant
    Filed: August 17, 2010
    Date of Patent: December 9, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Natalie A. Hawryluk, J. Guy Breitenbucher, William M. Jones, Alison L. Chambers, John M. Keith, Mark Seierstad
  • Publication number: 20140350251
    Abstract: 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: Application
    Filed: August 8, 2014
    Publication date: November 27, 2014
    Inventors: DAVID ALAN CLARK, BRUCE LAWRENCE FINKELSTEIN, GREGORY RUSSELL ARMEL, VERNON ARIE WITTENBACH
  • Patent number: 8883785
    Abstract: 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: Grant
    Filed: January 20, 2011
    Date of Patent: November 11, 2014
    Assignee: CHDI Foundation, Inc.
    Inventors: Celia Dominguez, Leticia M. Toledo-Sherman, Dirk Winkler, Frederick Brookfield, Paula C. De Aguiar Pena
  • Publication number: 20140329795
    Abstract: 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: Application
    Filed: August 28, 2012
    Publication date: November 6, 2014
    Inventors: 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
  • Patent number: 8877745
    Abstract: 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: Grant
    Filed: May 10, 2011
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
  • Publication number: 20140291646
    Abstract: A pyrene-based compound and an organic light-emitting diode including the same, the pyrene-based compound being represented by Formula 1, below:
    Type: Application
    Filed: March 25, 2014
    Publication date: October 2, 2014
    Applicant: Samsung Display Co., Ltd.
    Inventors: Dong-Woo SHIN, O-Hyun KWON, Mie-Hwa PARK, Seul-Ong KIM, Byoung-Ki CHOI
  • Publication number: 20140288067
    Abstract: 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: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • Publication number: 20140275123
    Abstract: 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-alkox
    Type: Application
    Filed: May 28, 2014
    Publication date: September 18, 2014
    Inventors: Francis Tisdell, JR., James M. Renga, David H. Young, George E. Davis, William C. Lo, Maurice C.H. Yap
  • Publication number: 20140275536
    Abstract: 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: Application
    Filed: December 22, 2010
    Publication date: September 18, 2014
    Applicant: Galderma Research & Development
    Inventor: Cédric Poinsard
  • Patent number: 8796284
    Abstract: 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: Grant
    Filed: March 29, 2011
    Date of Patent: August 5, 2014
    Assignee: Palobiofarma, S.L.
    Inventors: Juan Alberto Camacho Gomez, Julio Cesar Castro-Palomino Laria
  • Patent number: 8796283
    Abstract: 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: Grant
    Filed: October 14, 2010
    Date of Patent: August 5, 2014
    Assignee: Proximagen Limited
    Inventors: Kevin Dinnell, Andrew Lightfoot, Gillian Elizabeth Lunniss
  • Patent number: 8785630
    Abstract: 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: Grant
    Filed: February 6, 2013
    Date of Patent: July 22, 2014
    Assignee: Vestaron Corporation
    Inventors: Robert M. Kennedy, Bruce A. Steinbaugh
  • Patent number: 8765749
    Abstract: 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: Grant
    Filed: October 20, 2010
    Date of Patent: July 1, 2014
    Assignee: Korea Institute of Science and Technology
    Inventors: Tae Bo Sim, Young Jin Ham, Kyung Ho Yoo, Chang Hyun Oh, Jung Mi Hah, Hwan Geun Choi, Hwan Kim, Eun Jin Jun
  • Patent number: 8765949
    Abstract: 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: Grant
    Filed: December 16, 2010
    Date of Patent: July 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heiner Ebel, Sara Frattini, Kai Gerlach, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Marco Santagostino, Stefan Scheuerer, Christofer Tautermann, Thomas Trieselmann
  • Patent number: 8759356
    Abstract: 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-alkox
    Type: Grant
    Filed: May 3, 2010
    Date of Patent: June 24, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Francis E. Tisdell, James M. Renga, William C. Lo, Maurice C. H. Yap, David H. Young, George E. Davis
  • Patent number: 8748606
    Abstract: The present invention provides 4,6-diaminopyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: June 10, 2014
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
  • Patent number: 8686143
    Abstract: 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: Grant
    Filed: October 25, 2011
    Date of Patent: April 1, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: 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
  • Publication number: 20140080848
    Abstract: 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: Application
    Filed: September 13, 2013
    Publication date: March 20, 2014
    Applicants: National Taiwan University, National Yang-Ming University
    Inventors: Chung-Wai SHIAU, Kuen-Feng CHEN
  • Publication number: 20140057911
    Abstract: Certain 4,6-disubstituted aminopyrimidine derivatives having both aromatic and halogenic substituents.
    Type: Application
    Filed: August 23, 2013
    Publication date: February 27, 2014
    Inventors: Franco Lori, James Chafouleas, Davide De Forni, Antonio Solinas, Zoltán Varga, Zoltán Greff, László Örfi, György Kéri
  • Publication number: 20140031355
    Abstract: 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: Application
    Filed: November 4, 2011
    Publication date: January 30, 2014
    Applicant: Amgen Inc.
    Inventor: Amy Kaizerman
  • Patent number: 8618111
    Abstract: 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: Grant
    Filed: January 24, 2011
    Date of Patent: December 31, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Siegfried Schneider, Dirk Kessler, Lars van der Veen, Tobias Wunberg
  • Patent number: 8586505
    Abstract: 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: Grant
    Filed: July 15, 2010
    Date of Patent: November 19, 2013
    Assignee: SDS Biotech K. K.
    Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Ryutaro Katsuki, Tomoko Muraki
  • Patent number: 8575338
    Abstract: 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: Grant
    Filed: April 8, 2009
    Date of Patent: November 5, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Yasuyuki Tsuzuki, Miki Hirai
  • Patent number: 8563715
    Abstract: [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: Grant
    Filed: March 31, 2009
    Date of Patent: October 22, 2013
    Assignee: Zenyaku Kogyo Kabushikikaisha
    Inventors: Takeshi Nagata, Toshiaki Suzuki, Akira Yoshimura, Naoto Tadano, Toshiyuki Matsuno, Hideki Satoh, Kenichi Saitoh, Soichi Ohta
  • Patent number: 8524710
    Abstract: 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: Grant
    Filed: October 24, 2011
    Date of Patent: September 3, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Banner, Uwe Grether, Wolfgang Haap, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
  • Publication number: 20130217688
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: May 2, 2013
    Publication date: August 22, 2013
    Applicant: Celgene Avilomics Research, Inc.
    Inventor: Celgene Avilomics Research, Inc.
  • Patent number: 8445498
    Abstract: The present invention provides 4,6-disubstituted pyrimidine compound useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: February 1, 2011
    Date of Patent: May 21, 2013
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
  • Publication number: 20130123270
    Abstract: 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: Application
    Filed: March 26, 2012
    Publication date: May 16, 2013
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Kenneth G. Carson, Prakash Raman, Francois Soucy, Qing Ye, Shomir Ghosh
  • Patent number: 8431580
    Abstract: 4-Aminopyrimidine derivatives of formula (I) that are useful as histamine H4 receptor antagonists.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: April 30, 2013
    Assignee: Palau Pharma, S.A.
    Inventors: Elena Carceller González, Eva Maria Medina Fuentes, Robert Soliva Soliva, Marina Virgili Bernadó, Josep Martí Via
  • Patent number: 8431573
    Abstract: 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: Grant
    Filed: May 2, 2011
    Date of Patent: April 30, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Hendrix, Lars Bärfacker, Heike Heckroth, Dagmar Karthaus, Adrian Tersteegen
  • Publication number: 20130102782
    Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of Janus kinases (JAK).
    Type: Application
    Filed: July 3, 2012
    Publication date: April 25, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Gerald J. Tanoury, Young Chun Jung, Derek Magdziak, Adam Looker, Billie J. Kline, Václav Jurcík, Beatriz Dominguez Olmo
  • Patent number: 8426433
    Abstract: 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: Grant
    Filed: June 27, 2008
    Date of Patent: April 23, 2013
    Assignee: 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
  • Publication number: 20130090338
    Abstract: 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: Application
    Filed: May 10, 2011
    Publication date: April 11, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
  • Patent number: 8389521
    Abstract: 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: Grant
    Filed: April 24, 2008
    Date of Patent: March 5, 2013
    Assignee: Ingenium Pharmaceuticals GmbH
    Inventors: Heike Schauerte, Hans Allgeier, Michael A. Pleiss, Martin Augustin, Gisela Peraus, Gabriele Stumm, Philipp Wabnitz
  • Patent number: 8367825
    Abstract: 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: Grant
    Filed: February 28, 2012
    Date of Patent: February 5, 2013
    Assignee: 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
  • Publication number: 20130030171
    Abstract: The invention relates to heteroaryl aryl ureas of the formula IA, wherein the radicals and symbols have the meanings as defined herein, the use of such compounds in the treatment of protein kinase dependent diseases; to pharmaceutical preparations comprising said heteroaryl aryl ureas, to processes for the manufacture of such novel compounds and to methods of treatment comprising the use of such heteroaryl aryl ureas.
    Type: Application
    Filed: September 21, 2012
    Publication date: January 31, 2013
    Applicant: Novartis AG
    Inventor: Novartis AG
  • Patent number: 8343990
    Abstract: Substituted cyclopropyl compounds of formula (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: January 1, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harold B. Wood, Jason W. Szewczyk, Yong Huang, Alan D. Adams