Ring Sulfur In The Bicyclo Ring System Patents (Class 546/114)
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Publication number: 20130165477Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: February 14, 2013Publication date: June 27, 2013Applicant: METHYLGENE INC.Inventor: MethylGene Inc.
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Publication number: 20130165657Abstract: The problem to be solved is to produce, at high yields with high purity, anhydrous crystals of a compound represented by formula (1) that is an important intermediate for preparation of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof. The solution thereto is an industrial preparation process that provides, with high purity, anhydrous crystals of a compound represented by the following formula (1), which is an intermediate for the production of FXa inhibitor compound (X) or a pharmacologically acceptable salt thereof, or a hydrate thereof, wherein Boc represents a tert-butoxycarbonyl group.Type: ApplicationFiled: January 2, 2013Publication date: June 27, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Koutarou Kawanami, Hideaki Ishikawa, Masahiro Shoji
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Patent number: 8470821Abstract: Compounds active on phosphodiesterase PDE4B are provided. Also provided herewith are compositions useful for treatment of PDE4B-mediated diseases or conditions, and methods for the use thereof.Type: GrantFiled: July 20, 2009Date of Patent: June 25, 2013Assignee: Plexxikon Inc.Inventors: Prabha N. Ibrahim, Hanna Cho, Bruce England, Sam Gillette, Dean R. Artis, Rebecca Zuckerman, Chao Zhang
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Patent number: 8470850Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.Type: GrantFiled: May 6, 2010Date of Patent: June 25, 2013Assignee: MethylGene Inc.Inventors: Arkadii Vaisburg, Stephen William Claridge, Franck Raeppel, Oscar Mario Saavedra, Noemy Berstein, Marie-Claude Granger, Lijie Zhan, Amal Wahhab, David Liewellyn
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Publication number: 20130158002Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: February 28, 2011Publication date: June 20, 2013Inventors: Mark E. Layton, Michael J. Kelly, Timothy J. Hartingh
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Publication number: 20130157941Abstract: The present invention relates to azolopyridin-3-one derivatives of the general formula (I) with the meanings specified in the description, to their pharmaceutically usable salts and to their use as drug substances.Type: ApplicationFiled: June 17, 2011Publication date: June 20, 2013Applicant: SanofiInventors: Stefan Petry, Norbert Tennagels, Karl-Heinz Baringhaus
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Patent number: 8466289Abstract: The present invention relates to compounds of Formula I where R1a, R1b, X, R2a, R2b, W, R3, R4, and R5 are as defined herein as well as pharmaceutically acceptable salts thereof. The compounds have been shown to act as MEK inhibitors which may be useful in the treatment of hyperproliferative diseases, like cancer and inflammation.Type: GrantFiled: November 3, 2010Date of Patent: June 18, 2013Assignee: Novartis AGInventors: Mark G. Bock, Dinesh Chikkanna, Clive McCarthy, Henrik Moebitz, Chetan Pandit
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Publication number: 20130150573Abstract: Novel processes for the preparation of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety and intermediates thereto are provided. The compounds prepared by the present processes may be useful, for example, as selective inhibitors of human MEK (MAPKK) enzymes, and are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.Type: ApplicationFiled: February 6, 2013Publication date: June 13, 2013Applicant: UCB Pharma S.A.Inventor: UCB Pharma S.A.
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Publication number: 20130150366Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: February 5, 2013Publication date: June 13, 2013Applicant: ASTRAZENECA, INTELLECTUAL PROPERTYInventor: AstraZeneca, Intellectual Property
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Publication number: 20130150347Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
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Publication number: 20130150341Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 3, 2012Publication date: June 13, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
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Publication number: 20130144061Abstract: The present invention provides a novel process for preparing a substituted aromatic compound such as an aromatic halo compound or a salt thereof through a transformation reaction of an aromatic diazonium salt from an aromatic amino compound at stable high yields utilizing a novel Sandmeyer-like reaction using a nitroxide radical compound as a reaction catalyst.Type: ApplicationFiled: February 1, 2013Publication date: June 6, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: DAIICHI SANKYO COMPANY, LIMITED
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Patent number: 8455512Abstract: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefore in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGF?-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.Type: GrantFiled: May 20, 2011Date of Patent: June 4, 2013Assignee: Medicis Pharmaceutical CorporationInventors: Stephen D. Barrett, James B. Kramer, Mark L. Boys, Huifen Chen
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Patent number: 8455484Abstract: The invention provides new compounds and compositions thereof. The invention also provides methods for treating ophthalmic diseases, disorders and conditions.Type: GrantFiled: April 8, 2011Date of Patent: June 4, 2013Assignee: MethylGene Inc.Inventors: Stéphane Raeppel, Lijie Zhan, Stephen William Claridge, Franck Raeppel, Frédéric Gaudette, Arkadii Vaisburg
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Publication number: 20130129677Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: December 7, 2012Publication date: May 23, 2013Applicant: Siga Technologies, Inc.Inventor: Siga Technologies, Inc.
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Patent number: 8445680Abstract: The present invention relates to tetrahydrothienopyridine compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: GrantFiled: February 11, 2009Date of Patent: May 21, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: John S. Debenham, Jeffrey J. Hale, Christina B. Madsen-Duggan, Thomas F. Walsh
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Patent number: 8440830Abstract: The compounds of formula (I), wherein ring D and ring E together form a fused ring system selected from formula (II), (III), (IV), (V), (VI), (VII), and the salts of these compounds are novel, effective inhibitors of histone deacetylases.Type: GrantFiled: September 19, 2008Date of Patent: May 14, 2013Assignee: 4SC AGInventors: Thomas Maier, Thomas Beckers, Thomas Baer, Matthias Vennemann, Volker Gekeler, Astrid Zimmermann, Petra Gimmnich, Kamlesh Padiya, Hemant Joshi, Uday Joshi, Mahindra Makhija, Dipak Harel
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Patent number: 8440652Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.Type: GrantFiled: March 2, 2012Date of Patent: May 14, 2013Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David John Augeri, Jeffrey Thomas Bagdanoff, Simon David Peter Baugh, Marianne Carlsen, Kenneth Gordon Carson, John Anthony Gilleran, Wei He, Tamas Oravecz, Konstantin Salojin, Leonard Sung
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Publication number: 20130116233Abstract: The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: October 29, 2012Publication date: May 9, 2013Applicants: AbbVie Inc., Abbott GmbH & Co. KGInventors: Abbott GmbH & Co. KG, AbbVie Inc.
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Publication number: 20130116430Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.Type: ApplicationFiled: December 28, 2012Publication date: May 9, 2013Applicant: FUJIFILM CORPORATIONInventors: Hideyasu FUJIWARA, Kimihiko SATO, Shinsuke MIZUMOTO, Yuichiro SATO, Hideki KURIHARA, Yohei KUBO, Hiyoku NAKATA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Shinji HAGIWARA, Mari YAMAMOTO
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Patent number: 8436179Abstract: 4-Amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide which inhibits protein kinases such as Aurora-kinases and the VEGFR and PDGFR families of kinases, with an improved aqueous solubility profile, compositions containing 4-amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide and methods of treating diseases using 4-amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide are disclosed.Type: GrantFiled: July 18, 2012Date of Patent: May 7, 2013Assignee: AbbVie Inc.Inventors: Michael R. Michaelides, Michael L. Curtin, James H. Holms, Douglas H. Steinman
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Publication number: 20130109656Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: August 15, 2012Publication date: May 2, 2013Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robinson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtli
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Publication number: 20130096135Abstract: The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.Type: ApplicationFiled: September 27, 2012Publication date: April 18, 2013Applicant: METHYLGENE INC.Inventor: MethylGene Inc.
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Publication number: 20130095057Abstract: Disclosed are compounds of formula (I): or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof, which are of use in the treatment of infection with, and diseases caused by, Clostridium difficile.Type: ApplicationFiled: November 30, 2012Publication date: April 18, 2013Inventor: Summit Corporation Plc
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Publication number: 20130096088Abstract: The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.Type: ApplicationFiled: September 27, 2012Publication date: April 18, 2013Applicant: METHYLGENE INC.Inventor: METHYLGENE INC.
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Publication number: 20130096136Abstract: The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.Type: ApplicationFiled: September 27, 2012Publication date: April 18, 2013Applicant: METHYLGENE INC.Inventor: METHYLGENE INC.
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Patent number: 8420636Abstract: The present invention relates to pyrrolidinyl-alkyl-amide derivatives of formula (I) or (IA) wherein the variables are as defined herein, to their preparation and to their therapeutic use as CCR3 receptor ligands.Type: GrantFiled: January 26, 2011Date of Patent: April 16, 2013Assignee: SanofiInventors: Agnes Behr, Sandor Batori, Veronika Bartane Bodor, Zoltan Szlavik, Imre Bata, Katalin Urban-Szabo, Zoltan Kapui, Endre Mikus
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Publication number: 20130090327Abstract: The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.Type: ApplicationFiled: September 27, 2012Publication date: April 11, 2013Applicant: METHYLGENE INC.Inventor: METHYLGENE INC.
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Publication number: 20130085151Abstract: 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, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: ApplicationFiled: June 30, 2011Publication date: April 4, 2013Applicant: Amgen IncInventor: Brian Lucas
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Publication number: 20130085154Abstract: Salts of prasugrel were prepared including, for example, crystalline forms of prasugrel hydrobromide. These salts are useful, for example, in medicaments that inhibit the aggregation of platelets.Type: ApplicationFiled: April 7, 2011Publication date: April 4, 2013Inventors: Mihaela Tuksar, Tomislav Biljan, Miroslav Zegarac
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Patent number: 8410272Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention have use as therapeutic agents, e.g., they demonstrate anti-proliferative, anti-inflammatory, anti-angiogenic, anti-migration activities. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of, e.g., anti-inflammatory, renal, and hyperproliferative disorders. The compounds of the invention are pyrazolylbenzothiazole derivatives of the following formula (1) wherein X, R1, R2, R3 and R4 are described herein.Type: GrantFiled: October 22, 2010Date of Patent: April 2, 2013Assignee: Dermira (Canada), Inc.Inventors: Zaihui Zhang, Timothy S Daynard, Shisen Wang, Xinyao Du, Gregory B Chopiuk, Jun Yan, Jianxin Chen, Serguei V Sviridov
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Patent number: 8404847Abstract: The present invention provides a method for producing a compound represented by formula (A), the method comprising the steps of: (a) mixing a compound represented by formula (B) with p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate at less than 1 molar equivalent with respect to the compound represented by formula (B) in a solvent under heating; (b) adding additional p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate to the mixed solution under cooling, wherein the additional p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate is added in such an amount that the total molar equivalent thereof with the p-toluenesulfonic acid or p-toluenesulfonic acid monohydrate of step (a) is 1 molar equivalent or more with respect to the compound represented by formula (B) of step (a); and (c) subsequently allowing the mixed solution to crystallize to obtain the compound represented by formula (A).Type: GrantFiled: June 17, 2011Date of Patent: March 26, 2013Assignee: Daiichi Sankyo Company, LimitedInventor: Takeo Koyama
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Patent number: 8404846Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: August 29, 2008Date of Patent: March 26, 2013Assignee: MethylGene Inc.Inventors: Stephen William Claridge, Ljubomir Isakovic, Michael Mannion, Stéphane Raeppel, Oscar Mario Saavedra, Frédéric Gaudette, Lijie Zhan, Arkadii Vaisburg
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Publication number: 20130072473Abstract: The present invention is directed to compounds of Formulae (I), (IIa-IIh), (IIIa-IIIe), (IVa-IVc), (Va-V1), (VIa-VII), (VII), (VIII) and (IX), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.Type: ApplicationFiled: May 9, 2012Publication date: March 21, 2013Inventors: Bradley Tait, Noel A. Powell, Matthew Cullen
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Publication number: 20130072449Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: August 14, 2012Publication date: March 21, 2013Applicant: InterMune, Inc.Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
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Publication number: 20130072482Abstract: The present invention is for the anti-inflammatory compounds that have an inhibitory activity against protein tyrosine kinases and their pharmaceutical composition(s) containing the compound as the active ingredient. Since the compounds of the present invention can inhibit multiple protein kinases associated with inflammatory diseases and immune disorders, they are useful for their prevention or treatment.Type: ApplicationFiled: May 26, 2011Publication date: March 21, 2013Inventors: Beom-Seok Yang, Yong-Zu Kim, Tae-Kyo Park, Sung-Ho Woo, Hyang-Sook Lee, Sun-Young Kim, Jong-Un Cho, Hong-Bum Lee
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Publication number: 20130072520Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)— or ?N—; R1 is hydrogen or an optional substituent and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2—, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(?O)—, —O—(C?O)—, —C(?O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, or —N(CH2CH3)—; and Q is hydrogen, halogen, nitType: ApplicationFiled: November 28, 2011Publication date: March 21, 2013Applicant: Biota Scientific Management Pty LtdInventors: David BROWN, Ian COLLINS, Lloyd CZAPLEWSKI, David HAYDON
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Publication number: 20130072521Abstract: A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation.Type: ApplicationFiled: November 12, 2012Publication date: March 21, 2013Applicant: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCHInventor: Tianjin Institute of Pharmaceutical Research
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Patent number: 8399479Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: November 23, 2009Date of Patent: March 19, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Peter D.J. Grootenhuis, Sara S. Hadida Ruah, Jinglan Zhou
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Patent number: 8399449Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.Type: GrantFiled: February 25, 2009Date of Patent: March 19, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Nobuhiro Fujii, Yuya Oguro, Satoshi Sasaki, Shigeru Kondo
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Publication number: 20130065901Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: November 5, 2012Publication date: March 14, 2013Applicant: ARRAY BIOPHARMA INC.Inventor: Array BioPharma Inc.
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Patent number: 8394821Abstract: An object of the present invention is to provide a novel salt form of a compound that exhibits an inhibitory effect on activated blood coagulation factor X, and is useful as a preventive and/or therapeutic drug for thrombotic diseases, and crystals thereof. The present invention provides N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide tartrate and crystals thereof, as a novel salt form of N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide and crystals thereof.Type: GrantFiled: July 13, 2011Date of Patent: March 12, 2013Assignee: Daiichi Sankyo Company, LimitedInventor: Makoto Ono
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Patent number: 8394993Abstract: The invention relates to a process for the preparation of cyclopropyl benzyl ketone compounds of formula (II) wherein R1 represents fluorine or chlorine atom or C1-4 alkoxy group, by the reaction of a Grignard reagent, obtained from the reaction of compound of formula (V), wherein X represents chlorine or fluorine atom, with the compound of formula (IV), wherein R2 represents C1-4 alkyl group, having a straight or branched chain. The process can be applied preferably on industrial scale. Compound of formula (II), wherein R represents a fluorine atom in position 2 is an intermediate of the preparation process of prasugrel, which is a platelet inhibitor used in the therapy.Type: GrantFiled: November 27, 2008Date of Patent: March 12, 2013Assignee: Egis Gyogyszergyar Nyilvanosan Mukodo ReszvenytarsasagInventors: Tibor Mezei, Gyula Lukács, Enikó Molnár, József Barkóczy, Balázs Volk, Márta Porcs-Makkay, János Szulágyi, Mária Vajjon
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Patent number: 8389541Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: December 30, 2011Date of Patent: March 5, 2013Assignee: MethylGene Inc.Inventors: Stephen William Claridge, Ljubomir Isakovic, Michael Mannion, Stephane Raeppel, Oscar Mario Saavedra, Frederic Gaudette, Lijie Zhan, Arkadii Vaisburg
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Publication number: 20130053569Abstract: The present invention relates to process for the preparation of Prasugrel HCl having formula (I).Type: ApplicationFiled: March 17, 2011Publication date: February 28, 2013Inventors: Jayaraman Venkat Raman, Samir Patel, Abhijit Kadam, Vijay Patel, Jignesh Patel
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Publication number: 20130053375Abstract: Disclosed are quinoline compounds having the formula: wherein R1, R2 and A are as defined herein, and methods of making and using the same.Type: ApplicationFiled: May 6, 2011Publication date: February 28, 2013Inventors: Michael Jonathan Bury, Linda N. Casillas, Adam Kenneth Charnley, Michael P. DeMartino, Xiaoyang Dong, Patrick Eidam, Pamela A. Haile, Philip Anthony Harris, Ami Lakdawala Shah, Bryan W. King, Robert W. Marquis, JR., John F. Mehlmann, Joseph J. Romano, Clark A. Sehon
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Publication number: 20130053401Abstract: The invention relates to compounds that are direct activators of AMPK (AMP-activated protein kinase) and their use in the treatment of disorders regulated by activation of AMPK. For instance, compounds according to the invention are useful for the treatment of diabetes, metabolic syndrome, obesity, inflammation, cancer and cardiovascular diseases.Type: ApplicationFiled: December 28, 2010Publication date: February 28, 2013Inventors: Daniel Cravo, Sophie Hallakou-Bozec, Sébastien Bolze, Franck Lepifre, Laurent Faveriel, Jean-Denis Durand, Christine Charon
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Publication number: 20130046093Abstract: A pharmaceutical composition for preventing or treating a degenerative brain disease, and a method of screening a material for preventing or treating a degenerative brain disease. The method may effectively screen a prophylactic or therapeutic candidate material for preventing or treating a degenerative brain disease. A variety of degenerative brain diseases may be effectively prevented or treated using the pharmaceutical composition including a screened material for preventing or treating a degenerative brain disease.Type: ApplicationFiled: August 17, 2012Publication date: February 21, 2013Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Changjoon Justin LEE, Seonmi Jo, Boeun Yoon, Hyunah Choo, Ji Yoon Kim, Daesoo Kim
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Publication number: 20130045973Abstract: Compounds are disclosed that have a formula represented by the following: 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, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: April 20, 2012Publication date: February 21, 2013Inventors: Matthew Duncton, Donogh John Roger O'Mahony, Matthew Cox, Maria De Los Angeles Estiarte-Martinez
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Patent number: 8372315Abstract: A donor-acceptor (DA) ?-conjugated polymer with high charge transfer mobility has a plurality of D1kAD1k portions, where k is 1 or 2, D1 is a donor unit having at least one solubilizing side chain, and A is an acceptor unit, and the donor-acceptor (DA) ?-conjugated polymer has a plurality of D2m spacer sequences situated between the D1kAD1k portions, where m is 1 to 6 and D2 is a second donor unit where all atoms of the unit are coplanar in at least one conformation that the unit can assume. The DA ?-conjugated polymer can reflect a blue tinted green, deep green, or yellow tinted green color. The DA ?-conjugated polymers have space-charge limited (SCL) zero field hole mobilities of at least 1×10?6 cm2V?1s?1.Type: GrantFiled: May 26, 2010Date of Patent: February 12, 2013Assignee: University of Florida Research Foundation, Inc.Inventors: Pierre Marc Beaujuge, John R. Reynolds, Stefan Martin Ellinger