At 4- Or 6-position Patents (Class 544/319)
  • Patent number: 10316016
    Abstract: Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the lysine specific demethylase-1 inhibitor 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile. Also described are pharmaceutical compositions suitable for administration to a mammal that include the lysine specific demethylase-1 inhibitor, and methods of using the lysine specific demethylase-1 inhibitor for treating diseases or conditions that are associated with lysine specific demethylase-1 activity.
    Type: Grant
    Filed: July 10, 2018
    Date of Patent: June 11, 2019
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal, Paula Alessandra Tavares-Greco, Matthew Michael Kreilein
  • Patent number: 10207999
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: February 19, 2019
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 10106528
    Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: October 23, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Zulan Pi, Donna M. Bilder, Robert Paul Brigance, Heather Finlay, Wen Jiang, James A. Johnson, R. Michael Lawrence, Wei Meng, Michael C. Myers, Monique Phillips, George O. Tora, Xiaojun Zhang
  • Patent number: 10100209
    Abstract: Disclosed is a method of manufacturing a work function-controlled carbon nanomaterial and metal nanowire hybrid transparent conductive film, including: a first step of modifying the surface of a carbon nanomaterial to introduce a functional group to a conductive carbon nanomaterial; a second step of forming a work function-reduced carbon nanomaterial dispersed solution by mixing and reacting the carbon nanomaterial, which is functionalized in the first step, with an isocyanate-based compound and a pyrimidine-based compound; a third step of forming a single-component coating solution by hybridizing the work function-reduced carbon nanomaterial dispersed solution obtained in the second step with a metal nanowire; and a fourth step of forming a film by applying the coating solution, which is formed in the third step, on a substrate.
    Type: Grant
    Filed: March 15, 2016
    Date of Patent: October 16, 2018
    Assignee: KOREA ELECTROTECHNOLOGY RESEARCH INSTITUTE
    Inventors: Joong-tark Han, Geon-woong Lee, Kang-jun Baeg, Jong-seuk Woo, Seung-yol Jeong, Hee-jin Jeong
  • Patent number: 10047069
    Abstract: Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the lysine specific demethylase-1 inhibitor 4-[2-(4-aminopiperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydropyrimidin-4-yl]-2-fluorobenzonitrile. Also described are pharmaceutical compositions suitable for administration to a mammal that include the lysine specific demethylase-1 inhibitor, and methods of using the lysine specific demethylase-1 inhibitor for treating diseases or conditions that are associated with lysine specific demethylase-1 activity.
    Type: Grant
    Filed: October 25, 2017
    Date of Patent: August 14, 2018
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal, Paula Alessandra Tavares-Greco, Matthew Michael Kreilein
  • Patent number: 10023543
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: July 17, 2018
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9840477
    Abstract: The present disclosure relates to novel cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, the disclosure relates to novel tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer.
    Type: Grant
    Filed: June 6, 2016
    Date of Patent: December 12, 2017
    Assignee: CB THERAPEUTICS INC.
    Inventor: Deyi Zhang
  • Patent number: 9828358
    Abstract: Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the lysine specific demethylase-1 inhibitor 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile. Also described are pharmaceutical compositions suitable for administration to a mammal that include the lysine specific demethylase-1 inhibitor, and methods of using the lysine specific demethylase-1 inhibitor for treating diseases or conditions that are associated with lysine specific demethylase-1 activity.
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: November 28, 2017
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal, Paula Alessandra Tavares-Greco, Matthew Michael Kreilein
  • Patent number: 9776974
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: October 3, 2017
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9771329
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
    Type: Grant
    Filed: February 8, 2016
    Date of Patent: September 26, 2017
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9636421
    Abstract: The present invention relates to a compound comprising an alpha-end and an omega-end, the compound comprising on the alpha-end a reactive group Q1 capable of reacting with a functional group F1 present on a biomolecule and on the omega-end a target molecule, the compound further comprising a group according to formula (1) or a salt thereof: Said compound may also be referred to as a linker-conjugate. The invention also relates to a process for the preparation of a bioconjugate, the process comprising the step of reacting a reactive group Q1 of a linker-conjugate according to the invention with a functional group F1 of a biomolecule. The invention further relates to a bioconjugate obtainable by the process according to the invention.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: May 2, 2017
    Assignee: Synaffix B.V.
    Inventors: Jorge Merijn Mathieu Verkade, Maria Antonia Wijdeven, Petrus Josephus Jacobus Maria Van de Sande, Sander Sebastiaan Van Berkel, Floris Louis Van Delft
  • Patent number: 9604906
    Abstract: The present invention relates to an industrially feasible and economically viable process for the preparation of 3-aryloxy-3-phenylpropylamine and salt of formula I thereof.
    Type: Grant
    Filed: June 17, 2014
    Date of Patent: March 28, 2017
    Assignee: ZCL CHEMICALS LIMITED
    Inventors: Nand Lal Agarwal, Pranav Popatlal Mistri, Trushar Dahyabhai Patel, Pankaj Jayantilal Makasana
  • Patent number: 9556125
    Abstract: The invention relates to a process for preparing a pyrimidine intermediate, namely the compound of formula I-2 or a salt thereof, which involves the use of a liquid-liquid extraction using methyl iso-butyl ketone. Said compound of formula I-2 or its salt can be used to prepare macitentan.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: January 31, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Stefan Abele, Jacques-Alexis Funel, Ivan Schindelholz
  • Patent number: 9533959
    Abstract: The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.
    Type: Grant
    Filed: February 15, 2016
    Date of Patent: January 3, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Michael Edward O'Donnell
  • Patent number: 9359338
    Abstract: Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: June 7, 2016
    Assignee: CROWN BIOSCIENCE INC. (Taiwan)
    Inventors: Deyi Zhang, Ruihao Zhang, Boyu Zhong, Chuan Shih
  • Patent number: 9255097
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
    Type: Grant
    Filed: April 30, 2015
    Date of Patent: February 9, 2016
    Assignee: QUANTICEL PHARMACEUTICALS, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 9227941
    Abstract: The present invention relates to a carbon nanomaterial having a higher order structure by means of multiple hydrogen bonds and to a method for preparing same. One of the key technical features of the present invention is a carbon nanomaterial having a higher order structure, in which a functional group capable of multiple hydrogen bonds reacts with a conductive carbon nanomaterial, into which said functional group is introduced by a surface modification to be functionalized, thus enabling multiple hydrogen bonds between carbon nanomaterials.
    Type: Grant
    Filed: May 9, 2012
    Date of Patent: January 5, 2016
    Assignee: Korea Eletrotechnology Research Institute
    Inventors: Joong-tark Han, Geon-woong Lee, Seung-yol Jeong, Hee-jin Jeong, Bo hwa Jeong
  • Patent number: 9090594
    Abstract: PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts of the compounds as represented by Formula I. The compounds significantly inhibit the Pim kinase activity and are used to prepare drugs to treat PIM kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.
    Type: Grant
    Filed: February 10, 2014
    Date of Patent: July 28, 2015
    Assignee: JIKAI BIOSCIENCES, INC.
    Inventor: Yu Ge
  • Publication number: 20150141372
    Abstract: Compounds of formula (I), processes for their production and their use as Bub1 kinase inhibitors for the treatment of hyperproliferative diseases and/or disorders responsive to induction of cell death.
    Type: Application
    Filed: May 8, 2013
    Publication date: May 21, 2015
    Inventors: Marion Hitchcock, Christoph-Stephan Hilger, Anne Mengel, Hans Briem, Simon Holton, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernández-Montalván, Christian Stegmann, Cornelia Preuße, Mark Jean Gnoth
  • Patent number: 9034851
    Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: September 19, 2012
    Date of Patent: May 19, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Qun Dang, Changyou Zhou, Wuxin Zou, Yuxia Hua
  • Publication number: 20150126513
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
  • Publication number: 20150119412
    Abstract: A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: wherein each symbol is as defined herein, or a salt thereof, a medicament comprising the compound or a salt thereof, and use of the compound or a salt thereof as an agent the prophylaxis or treatment of diabetes mellitus are provided.
    Type: Application
    Filed: October 28, 2014
    Publication date: April 30, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo Kasai, Takashi Nakahata, Asato Kina, Hideki Hirose, Takeshi Yamasaki, Tohru Yamashita, Yoichi Nishikawa
  • Patent number: 9018200
    Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
  • Patent number: 9012635
    Abstract: Compounds useful in the treatment of mammalian cancers and especially human cancers according to Formula I are disclosed. Pharmaceutical compositions and methods of treatment employing the compounds disclosed herein are also disclosed.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: April 21, 2015
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Michael D. Kaufman
  • Publication number: 20150105549
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, X is CH or N; Y is C(O) or S(O)2; provided that when Y is S(O)2, then X is CH; A is a radical selected from the group consisting of and B1, B2, B3, T, R1, R2R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: KANU MAGANBHAI PATEL, Thomas Paul Selby, Brenton Todd Smith, Andrew Edmund Taggi, Patrick Ryan Kovacs
  • Publication number: 20150099883
    Abstract: The present invention provides an aryloxyurea compound or salt thereof, and a pest control agent including the aryloxyurea compound or salt thereof as an active ingredient. The aryloxyurea compound has a superior acaricidal and/or insecticidal activity, superior safety, and can be synthesized advantageously and industrially. The compound of the present invention includes aryloxyurea compounds represented by the following formula or salts thereof: in the formula, Cy represents an unsubstituted or X-substituted phenyl group or the like, X represents a halogen atom or the like, R1 represents an ethyl group or the like, R2 represents a hydrogen atom or the like, R3 and R4 represents a methyl group or the like, X1 represents a methylthio group or the like, m1 represents an integer of 1 to 4, X2 represents a methyl group or the like, m2 is an integer of 0 to 3.
    Type: Application
    Filed: April 8, 2013
    Publication date: April 9, 2015
    Inventors: Hironori Furukawa, Daisuke Hanai, Tetsuo Tamai, Jun Kanazawa, Katsunori Tanaka, Asaho Nagagata
  • Publication number: 20150099756
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Yun JIN, Zehong WAN, Qing ZHANG
  • Publication number: 20150099875
    Abstract: The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Jean-Damien Charrier, Michael Edward O'Donnell
  • Patent number: 9000163
    Abstract: Provided is a method for selectively demethylating a 2-methoxy group. Specifically provided is a production method of a compound represented by formula (7) below through the following reactions.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: April 7, 2015
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Masaaki Nagasawa, Kazuyasu Asami, Ryu Nakao, Nobuyuki Tanaka, Yoshiyuki Aida
  • Patent number: 8993584
    Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as procymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: March 31, 2015
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Koji Sugimoto, Hiroyuki Hayashi
  • Publication number: 20150087639
    Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
    Type: Application
    Filed: July 18, 2013
    Publication date: March 26, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Yingjun Zhang, Jiancun Zhang, Xiaojun Wang, Runfeng Lin, Shengtian Cao, Zhaohe Wang, Jing Li
  • Patent number: 8987276
    Abstract: The present invention is concerned with novel substituted triazolyl piperazine and triazolyl piperidine derivatives of Formula (I) wherein R1, R2, R3, R4a, R4b, R5, X, Y1, Y2, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: March 24, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Francois Paul Bischoff, Adriana Ingrid Velter, Sven Franciscus Anna Van Brandt, Didier Jean-Claude Berthelot
  • Publication number: 20150080568
    Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
    Type: Application
    Filed: July 28, 2014
    Publication date: March 19, 2015
    Inventors: Weirong Chen, Benjamin Lane, Hairuo Peng
  • 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: 8981091
    Abstract: Disclosed is a pest control composition having an excellent controlling effect on pests, which comprises etoxazole and fenazaquin.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: March 17, 2015
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Katsuya Natsuhara, Azusa Tanaka
  • 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: 8975261
    Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: March 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
  • Publication number: 20150057152
    Abstract: The present invention relates to novel crystalline polymorphic and amorphous forms of the compound (E)-2-{2-[6-(2-cyanophenoxy) pyrimidin-4-yloxy] phenyl}-3-methoxy-acrylate (azoxystrobin). Infrared Raman spectra, X-ray powder diffraction pattern and differential scanning calorimetry thermogram of two polymorphs “A” and “B” are provided. Further, the present invention also provides methods for preparing the novel polymorphic forms “A” and “B”, as well as processes for producing mixtures of the polymorphs, and a process for preparing amorphous azoxystrobin. Yet further, the present invention provides anti-fungal compositions comprising the novel crystalline polymorphs “A” and “B” or amorphous azoxystrobin, which are useful for controlling and combating fungi grown on agricultural and horticultural crops and up-land, and methods of using the same as pesticidal agents for combating fungi on agricultural and horticultural crops.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 26, 2015
    Inventors: Sharona Zamir, Inna Faktorovitch
  • Publication number: 20150057278
    Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein Cy1, Cy2, n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.
    Type: Application
    Filed: September 10, 2012
    Publication date: February 26, 2015
    Inventors: Dan Littman, Jun R. Huh, Ruili Huang, Wenwei Huang, Erika E. Englund
  • 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: 8962833
    Abstract: The present invention provides novel salts of raltegravir, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides crystalline sodium salt of raltegravir, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a process for the preparation of amorphous sodium salt of raltegravir. The present invention further provides a process for the preparation of raltegravir potassium crystalline form H1.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: February 24, 2015
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Kesireddy Subash Chander Reddy, Bandi Vamsi Krishna
  • Publication number: 20150051225
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 19, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Ishtiyaque Ahmad, Rajagopal Bakthavatchalam, Sivaramakrishna Battula, Henricus Jacobus, Maria Gijsen, Mark Wall
  • Publication number: 20150051209
    Abstract: The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 19, 2015
    Applicant: NOVARTIS AG
    Inventors: Mark Gary BOCK, Henrik MOEBITZ, Sunil Kumar PANIGRAHI, Ramulu PODDUTOORI, Susanta SAMAJDAR
  • Patent number: 8957062
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: February 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
  • Publication number: 20150045554
    Abstract: The present invention relates to a novel synthetic route for the preparation of raltegravir and pharmaceutically acceptable salts, starting from 2-amino-2-methylpropanenitrile and oxadiazole carbonyl chloride, through the formation of a pyrimidinone intermediate of formula (V).
    Type: Application
    Filed: December 21, 2012
    Publication date: February 12, 2015
    Inventors: Mukund Keshav Gurjar, Swapnil Panditrao Sonawane, Golakchandra Sudarshan Maikap, Gulabrao Dagadu Patil, Shivnath Bhaupatil Shinde, Pankaj Shalikrao, Samit Satish Mehta
  • Publication number: 20150045349
    Abstract: The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: February 19, 2013
    Publication date: February 12, 2015
    Inventors: Hiroyuki Nagamiya, Masato Yoshida, Masaki Seto, Shogo Marui, Tsuneo Oda, Yuji Ishichi, Hideo Suzuki, Tomokazu Kusumoto, Takatoshi Yogo, Chul Yun Rhim, Cheolhwan Yoon, Gil Nam Lee, Hyun Bin Kang, Kwang Ok Kim, Hye Sun Jeon
  • Publication number: 20150045378
    Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
    Type: Application
    Filed: February 12, 2013
    Publication date: February 12, 2015
    Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata
  • Publication number: 20150045355
    Abstract: Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.
    Type: Application
    Filed: December 31, 2011
    Publication date: February 12, 2015
    Inventors: Changyou Zhou, Shaohui Wang, Guoliang Zhang
  • Patent number: 8952024
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, X is CH or N; Y is C(O) or S(O)2; provided that when Y is S(O)2, then X is CH; A is a radical selected from the group consisting of and B1, B2, B3, T, R1, R2 R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: September 7, 2010
    Date of Patent: February 10, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: Kanu Maganbhai Patel, Thomas Paul Selby, Brenton Todd Smith, Andrew Edmund Taggi, Patrick Ryan Kovacs
  • Patent number: 8952025
    Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: February 10, 2015
    Assignee: Arizona Board of Regents, A Body Corporate of the State of Arizona Acting for and on Behalf of Arizona State University
    Inventors: Sidney Hecht, Omar Khdour, Jun Lu, Pablo Arce