Ring Sulfur In The Bicyclo Ring System Patents (Class 514/301)
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Patent number: 8524906Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: August 17, 2011Date of Patent: September 3, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, Upul Keerthi Bandarage, Kevin Michael Cottrell, Robert J. Davies, Elaine B. Krueger, Mark Willem Ledeboer, Brian Ledford, Arnaud Le Tiran, David Messersmith, Tiansheng Wang, Jinwang Xu, Yusheng Liao
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Publication number: 20130224259Abstract: The present disclosure provides DDAH modulators. Thus, the present disclosure provides a method of treating a patient suffering from a disorder characterized by excessive NO production and/or elevated DDAH activity, the method comprising administering to said patient an effective amount of a compound of one of formulae I-X. The present disclosure also provides a pharmaceutical composition comprising a compound of one of formulae I-X.Type: ApplicationFiled: February 13, 2013Publication date: August 29, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventor: The Board of Trustees of the Leland Stanford Junior University
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Publication number: 20130225581Abstract: The present invention provides a nitrogen-containing aromatic heterocyclic derivative represented by formula (I): [wherein W represents CR3 (wherein R3 represents a hydrogen atom or the like) or the like, R4 represents a hydrogen atom or the like, R5 represents a hydrogen atom or the like, R9 represents substituted imidazolyl, R12 and R13 may be the same or different, each represent a hydrogen atom or the like, R22 and R23 may be the same or different, each represent a hydrogen atom or the like, R24 represents a hydrogen atom or the like, Y represents C—R25 (wherein R25 represents a hydrogen atom or the like) or the like] or a pharmaceutically acceptable salt thereof and a FGFR inhibitor comprising, as an active ingredient, the nitrogen-containing aromatic heterocyclic derivative or the pharmaceutically acceptable salt thereof, or the like.Type: ApplicationFiled: July 15, 2011Publication date: August 29, 2013Applicant: KYOWA HAKKO KIRIN CO., LTDInventors: Takayuki Furuta, Kazuo Kubo, Toshiyuki Atsumi, Maasa Yamanouchi
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Publication number: 20130225567Abstract: 5-alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification.Type: ApplicationFiled: February 19, 2013Publication date: August 29, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Ulrich REISER, Gerd BADER, Walter SPEVAK, Andreas STEFFEN, Alastair L. PARKES
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Publication number: 20130224255Abstract: Embodiments of the present invention include methods for the treatment, prevention, or amelioration of vascular disease in diabetic patients. The methods include both implantation of a stent including a first drug. Some embodiments include additional therapy, such as the co-administration of another drug. Some embodiments involve different stent selection for a diabetic patient compared to a non-diabetic patient.Type: ApplicationFiled: February 23, 2012Publication date: August 29, 2013Applicant: Abbott Cardiovascular Systems Inc.Inventors: Syed F.A. Hossainy, Paul M. Consigny
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Publication number: 20130217699Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.Type: ApplicationFiled: May 8, 2012Publication date: August 22, 2013Applicant: ELI LILLY AND COMPANYInventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
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Patent number: 8513278Abstract: Described herein are ways to solubilize clopidogrel for parenteral administration containing clopidogrel and D50W, which is useful in the prevention of platelet aggregation in acute coronary syndrome, acute myocardial infarction or to prevent platelet facilitated thrombosis following coronary angioplasty and/or coronary stenting.Type: GrantFiled: November 26, 2012Date of Patent: August 20, 2013Assignee: Academic Pharmaceuticals, Inc.Inventor: John C Somberg
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Publication number: 20130210719Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of heart failure, as well as to a method for treating heart failure, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said heart failure. The invention further relates to a treatment programme for treating heart failure, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating heart failure or the symptoms thereof.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: HEART METABOLICS LIMITEDInventor: Heart Metabolics Limited
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Publication number: 20130210720Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of heart failure, as well as to a method for treating heart failure, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said heart failure. The invention further relates to a treatment programme for treating heart failure, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating heart failure or the symptoms thereof.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: HEART METABOLICS LIMITEDInventor: HEART METABOLICS LIMITED
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Publication number: 20130210768Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is 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, such as schizophrenia.Type: ApplicationFiled: June 6, 2011Publication date: August 15, 2013Inventors: Kenneth L. Arrington, Vadim Dudkin, Mark E. Layton, Joseph E. Pero, Alexander J. Reif
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Publication number: 20130203737Abstract: The present invention relates to a fused heterocyclic derivative of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl, each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl optionally substituted with one or more fluoro atoms, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, dimethylamino, and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, and phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, Z is a linking group —W—(Cn-alkylene)-T- wherein W is attached to R1 and selType: ApplicationFiled: July 8, 2011Publication date: August 8, 2013Applicant: ABBVIE B.V.Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Leonardus A.J.M. Sliedregt, Maria J.P. van Dongen, Jacobus A.J. den Hartog
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Publication number: 20130203703Abstract: The present invention relates to compounds which are 1,2-dihydro-4-hydroxy-2-oxo-quinoline-3-carboxanilides, their thieno-pyridone analogs, and prodrugs thereof. This invention specifically relates to such derivatives containing an N-hydrogen in the carboxanilide moiety and which exhibit modulating activity towards the aromatic hydrocarbon receptor (AhR), and, specifically, also to prodrugs thereof. The present invention also relates to use of said compounds as a medicament, and for the treatment of cancer, autoimmune disorders and other disorders with an immunological component, and a pharmaceutical composition comprising one or more of said compounds and a method of treatment.Type: ApplicationFiled: October 11, 2011Publication date: August 8, 2013Applicant: Immunahr ABInventor: Lars Pettersson
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Patent number: 8501955Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: GrantFiled: October 7, 2008Date of Patent: August 6, 2013Assignee: Advinus Therapeutics Private LimitedInventors: Debnath Bhuniya, Sandeep Bhausaheb Bhosale, Gobind Sing Kapkoti, Venkata Poornapragnacharyulu Palle, Siddhartha De, Kasim A. Mookhtiar, Bhavesh Dave, Anil Deshpande, Santosh Kurhade, Balasaheb Kobal, Keshav Naik, Sachin Kandalkar
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Patent number: 8501769Abstract: The present invention discloses fused thienopyridyl compounds of general formula (I) wherein X1-X6, R5-R7, Z1 and L are as defined in the description. The resent invention also discloses a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain, urinary incontinence, bladder overactivity, and inflammatory thermal hyperalgesia in mammals, and pharmaceutical compositions including those compounds.Type: GrantFiled: December 15, 2010Date of Patent: August 6, 2013Assignee: AbbVie Inc.Inventors: Sean T Turner, Tammie K Jinkerson, Arthur R. Gomtsyan, Chih-hung Lee
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Patent number: 8497283Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: GrantFiled: September 14, 2012Date of Patent: July 30, 2013Assignee: Merck Patent GmbHInventors: Melanie Schultz, Kai Schiemann, Jr., Wolfgang Staehle
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Publication number: 20130189342Abstract: The present invention comprises compositions, methods and kits for delivering drugs. The invention provides an implantable device for delivery of a pharmaceutical substance to a patient, comprising a core comprising a core polymeric material optionally containing a core pharmaceutical substance, surrounded by a first layer comprising a first-layer pharmaceutical substance and a first-layer polymeric material, optionally surrounded by one or more additional layers comprising an additional pharmaceutical substance and an additional polymeric material, where the core, first, and optional additional polymeric materials may be the same or different, and where the optional core pharmaceutical substance, first-layer pharmaceutical substance, and optional additional pharmaceutical substances are the same or different. Implantation of the device allows a controlled release of drug for an extended period of time. The device may be implanted subcutaneously in an individual in need of continuous treatment with a drug.Type: ApplicationFiled: March 16, 2011Publication date: July 25, 2013Applicant: TITAN PHARMACEUTICALS, INC.Inventors: Rajesh A. Patel, Sunil R. Bhonsle
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Patent number: 8492401Abstract: Provided herein are novel sirtuin-modulating compounds of Structural Formula (Ia) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: November 15, 2012Date of Patent: July 23, 2013Assignee: GlaxoSmithKline LLCInventors: Christopher Oalmann, Jeremy S Disch, Pui Yee Ng, Robert B Perni
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Publication number: 20130184308Abstract: An object of the present invention is to provide an activated blood coagulation factor X (FXa) inhibitor that reduces the risk of bleeding caused by the treatment of thromboembolism. The present invention provides an oral anticoagulant agent comprising a compound represented by the following formula (1): or a pharmacologically acceptable salt thereof, or a hydrate thereof, as an active ingredient, wherein (A) a factor involved in the risk of bleeding caused by the anticoagulant agent is selected as a dose determinant; (B) a reference value of the dose determinant is set; (C) the dose determinant of a patient in need of administration is measured; and (D) the dose of the anticoagulant agent is selected with the reference value as an index.Type: ApplicationFiled: January 11, 2013Publication date: July 18, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: DAIICHI SANKYO COMPANY, LIMITED
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Patent number: 8487101Abstract: A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.Type: GrantFiled: July 20, 2010Date of Patent: July 16, 2013Assignee: UCB Pharma S.A.Inventors: Daniel Christopher Brookings, Martin Clive Hutchings, Barry John Langham
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Patent number: 8481572Abstract: Provided is a pharmaceutical composition including as an active component a compound of formula (I): wherein X and (R1)n are as defined, and a physiological acceptable carrier. Also provided is a method for treating cancer including administering to an individual in need of such treatment an effective amount of the presently described pharmaceutical composition.Type: GrantFiled: August 10, 2008Date of Patent: July 9, 2013Assignee: Urifer Ltd.Inventors: Uri Nir, Sally Shpungin, Etai Yaffe, Moshe Cohen
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Patent number: 8481544Abstract: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, —S(O)NR6—, —C(?O)O— or —S(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N; R2 and R3 are as defined in the description.Type: GrantFiled: June 7, 2011Date of Patent: July 9, 2013Assignee: Biota Europe LimitedInventors: David John Haydon, Lloyd George Czaplewski, Nicholas John Palmer, Dale Robert Mitchell, John Frederick Atherall, Christopher Richard Steele, Tamara Ladduwahetty
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Publication number: 20130172327Abstract: Disclosed are N-1-cyano-2-(phenyl)ethyl)-2-azabicyclo[2.2.1]heptane-3-carboxamides of formula I and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory diseases.Type: ApplicationFiled: September 14, 2012Publication date: July 4, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Doris RIETHER, Wolfgang WIENEN
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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: 20130165476Abstract: Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.Type: ApplicationFiled: January 28, 2011Publication date: June 27, 2013Applicant: JIANGSU VCARE PHARMATECH CO., LTD.Inventors: Hongbin Sun, Jiaqi Shan, Boyu Zhang, Fang Yuan
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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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Publication number: 20130158069Abstract: It is intended to provide a highly safe, orally administrable preventive and/or therapeutic agent for thrombosis and/or embolism that can be applied to a thrombosis and/or embolism patient with severe renal impairment. The present inventors have found that even for a thrombosis and/or embolism patient with severe renal impairment, use of edoxaban at a dose of 15 mg once a day can effectively prevent thrombosis and/or embolism while avoiding the risk of bleeding. The present inventors have also found that even for a thrombosis and/or embolism patient with severe renal impairment, edoxaban at a dose of 15 mg once a day can effectively prevent thrombosis and/or embolism with safety over a long period.Type: ApplicationFiled: July 20, 2012Publication date: June 20, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tetsuya Kimura, Tomohiko Kumakura, Masaya Tachibana, Chiaki Matsumoto, Kenji Abe
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Patent number: 8466171Abstract: Disclosed are fused heterocyclic compounds of Formula (I): or pharmaceutically-acceptable salts or stereoisomers thereof. Also disclosed are methods of using such compounds in the treatment of at least one androgen receptor-associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: GrantFiled: October 31, 2008Date of Patent: June 18, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Weifang Shan, James Aaron Balog, Ashvinikumar V. Gavai, Yufen Zhao
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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: 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: 20130143861Abstract: The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering budiodarone to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of budiodarone and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of budiodarone may also be treated. Some methods provide for prevention of atrial remodeling and others provide for the reversal of atrial remodeling, including methods to quantify the reversal of atrial remodeling.Type: ApplicationFiled: February 4, 2013Publication date: June 6, 2013Applicant: ARMETHEON, INC.Inventor: Armetheon, Inc.
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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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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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Publication number: 20130137716Abstract: Described herein are ways to solubilize clopidogrel for parenteral administration containing clopidogrel and D50W, which is useful in the prevention of platelet aggregation in acute coronary syndrome, acute myocardial infarction or to prevent platelet facilitated thrombosis following coronary angioplasty and/or coronary stenting.Type: ApplicationFiled: November 26, 2012Publication date: May 30, 2013Applicant: ACADEMIC PHARMACEUTICALS INCORPORATEDInventor: Academic Pharmaceuticals Incorporated
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Publication number: 20130136804Abstract: N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea free base and crystallines form thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.Type: ApplicationFiled: December 17, 2012Publication date: May 30, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Publication number: 20130131021Abstract: This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of a phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol.Type: ApplicationFiled: January 7, 2013Publication date: May 23, 2013Applicant: CONCERT PHARMACEUTICALS INC.Inventor: CONCERT PHARMACEUTICALS INC.
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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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Publication number: 20130129700Abstract: The present invention provides compositions containing clopidogrel, present as a free base or a pharmaceutically acceptable salt thereof, and sulfoalkyl ether cyclodextrin (SAE-CD). The compositions can be liquid, suspension or solid compositions. They can be adapted for oral, peroral or parenteral administration. The SAE-CD serves to aid in dissolution and stabilization of the clopidogrel in aqueous media. The stability of clopidogrel against hydrolytic degradation, thermal degradation, and photolytic degradation are improved. SAE-CD provides improved results over other cyclodextrin derivatives. The SAE-CD-containing composition of clopidogrel can be provided in liquid form, solid form or as a reconstitutable powder. Both ready-to-use and concentrated liquid compositions can be prepared. The liquid composition is optionally available as a clear solution.Type: ApplicationFiled: November 30, 2012Publication date: May 23, 2013Applicant: Cydex Pharmaceuticals, Inc.Inventor: Cydex Pharmaceuticals, 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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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: 20130102617Abstract: Phenylacetamide compounds of the formula having sulfonyl group and cycloalkyl group on the phenyl group and having heteroaryl group on the nitrogen atom in the amide have an excellent glucokinase activation action. The compound of the present invention is useful as an agent for treating diabetes, in particular, type II diabetes, as well as metabolic syndrome and obesity.Type: ApplicationFiled: April 18, 2012Publication date: April 25, 2013Applicant: ASTELLAS PHARMA INC.Inventors: Masahiko Hayakawa, Yoshiyuki Kido, Takahiro Nigawara, Mitsuaki Okumura, Akira Kanai, Keisuke Maki, Nobuaki Amino
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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.