Ring Sulfur In The Bicyclo Ring System Patents (Class 514/301)
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Publication number: 20130095095Abstract: A method for treating thrombotic disorders using a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid. Also disclosed is a method of improving the efficacy of a blood thinning medication by co-administering a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid to a subject being treated with a blood thinning medication.Type: ApplicationFiled: October 13, 2011Publication date: April 18, 2013Inventor: Thomas Christian Lines
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Publication number: 20130096153Abstract: The present invention provides methods for predicting or determining a subject's response to an antiplatelet agent, and methods for determining a subject's suitability to a treatment regime or intervention for a disease associated with platelet aggregation, using analysis of genetic polymorphisms. The present invention also relates to the use of genetic polymorphisms in assessing a subject's response to an antiplatelet agent.Type: ApplicationFiled: December 12, 2012Publication date: April 18, 2013Inventors: Patrick A. Gladding, Mark W. Webster
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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: 20130095179Abstract: Methods of identifying subjects who are resistant to antiplatelet therapy, such as therapy with clopidogrel, are presented. The methods comprise determining is whether the subject is an efficient converter of medium chain polyunsaturated fatty acids to long-chain polyunsaturated fatty acids. Also provided are methods of treating resistance to antiplatelet therapy in subjects who are efficient converters of medium chain polyunsaturated fatty acids to long-chain polyunsaturated fatty acids, comprising adjunctively administering to the subject an effective amount of a composition comprising omega-3 long chain polyunsaturated fatty acids. Improved methods of antiplatelet therapy are provided, wherein the improvement comprises adjunctive administration of a composition comprising omega-3 long chain polyunsaturated fatty acids in free acid form.Type: ApplicationFiled: September 14, 2012Publication date: April 18, 2013Applicant: Omthera Pharmaceuticals, Inc.Inventors: Michael H. Davidson, Gerald L. Wisler
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Publication number: 20130096154Abstract: The present invention provides methods for predicting or determining a subject's response to an antiplatelet agent, and methods for determining a subject's suitability to a treatment regime or intervention for a disease associated with platelet aggregation, using analysis of genetic polymorphisms. The present invention also relates to the use of genetic polymorphisms in assessing a subject's response to an antiplatelet agent.Type: ApplicationFiled: December 12, 2012Publication date: April 18, 2013Inventors: Patrick A. Gladding, Marja-Liisa Dahl, Mark W. Webster
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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: 20130085155Abstract: 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: ApplicationFiled: November 15, 2012Publication date: April 4, 2013Applicant: Sirtris PharmaceuticalsInventor: Sirtris Pharmaceuticals
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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: 8404686Abstract: The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.Type: GrantFiled: June 24, 2011Date of Patent: March 26, 2013Assignee: Spinifex Pharmaceuticals Pty LtdInventors: Maree Therese Smith, Bruce Douglas Wyse
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Patent number: 8404715Abstract: Methods and pharmaceutical compositions employing a terfenadine metabolite and a leukotriene inhibitor for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof. Also included are methods and compositions employing a terfenadine metabolite, a leukotriene inhibitor, and a decongestant for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof.Type: GrantFiled: February 16, 2012Date of Patent: March 26, 2013Assignee: Sunovion Pharmaceuticals Inc.Inventor: Paul D. Rubin
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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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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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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: 20130064892Abstract: A method of making a pharmaceutical tablet comprises (a) combining (i) an aqueous networked cellulose gel with (ii) filler and (iii) an active agent to form a mixture thereof; (b) casting the mixture to form a wet tablet; (c) drying the wet tablet to form a dry pharmaceutical tablet; and then (d) optionally coating the tablet (e.g., with an enteric coating). Pharmaceutical tablets produced by such methods are also described.Type: ApplicationFiled: September 8, 2011Publication date: March 14, 2013Inventors: Raed Hashaikeh, Hatem M.N. Abushammala
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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: 8394822Abstract: 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: September 5, 2012Date of Patent: March 12, 2013Assignee: UCB Pharma, S.A.Inventors: Martin Clive Hutchings, Sarah Catherine Archibald, Daniel Christopher Brookings, Jeremy Martin Davis, James Andrew Johnson, Barry John Langham, Judi Charlotte Neuss
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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: 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: 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: 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: 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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Publication number: 20130045251Abstract: A pharmaceutical composition containing prasugrel and its pharmaceutically acceptable salts, and methods for preparing the same are disclosed. The pharmaceutical composition improves the dissolution rate of prasugrel and its salts at high pH by using solid dispersion technology, inclusion technology or adding surfactants.Type: ApplicationFiled: April 22, 2011Publication date: February 21, 2013Applicant: JIANGSU HANSOH PHARMACEUTICAL GROUP CO., LTDInventors: Junda Cen, Chun-hong Zhang, Qi Zhang, Aifeng Lü
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Publication number: 20130040916Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.Type: ApplicationFiled: October 12, 2012Publication date: February 14, 2013Applicant: ESPERION THERAPEUTICS, INC.Inventor: Esperion Therapeutics, Inc.
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Patent number: 8372980Abstract: Fused-ring, heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein ?represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: GrantFiled: July 22, 2011Date of Patent: February 12, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Mariappan V. Chelliah, Samuel Chackalamannil
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Publication number: 20130035332Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one 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: April 25, 2011Publication date: February 7, 2013Inventors: Mark E. Layton, Michael J. Kelly
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Publication number: 20130035356Abstract: An object of the present invention is to provide a novel crystal form of a compound that has an inhibitory effect on activated blood coagulation factor X and is useful as a pharmaceutical compound for prevention and/or treatment of thrombotic and/or embolic diseases. The present invention provides a novel crystal 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 p-toluenesulfonate monohydrate, and method for producing the same.Type: ApplicationFiled: September 19, 2012Publication date: February 7, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: DAIICHI SANKYO COMPANY, LIMITED
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Publication number: 20130035355Abstract: The present invention relates to Prasugrel or a pharmaceutically acceptable salt thereof, compositions containing said active ingredient as well as pharmaceutical compositions containing said active ingredient or a composition containing said active ingredient. The present invention further relates to methods for the preparation of the novel compositions.Type: ApplicationFiled: February 10, 2011Publication date: February 7, 2013Applicant: ratiopharm GmbHInventors: Sandra Brueck, Jana Paetz
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Publication number: 20130029971Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, Y and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: January 5, 2011Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
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Publication number: 20130030014Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: July 11, 2012Publication date: January 31, 2013Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
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Publication number: 20130029995Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).Type: ApplicationFiled: July 25, 2012Publication date: January 31, 2013Applicant: Gruenenthal GmbHInventors: Robert FRANK, Thomas CHRISTOPH, Bernhard LESCH, Jeewoo LEE
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Publication number: 20130029984Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. Castro, Catherine A. Evans, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20130023556Abstract: 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: ApplicationFiled: September 14, 2012Publication date: January 24, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Melanie SCHULTZ, Kai Schiemann, JR., Wolfgang Staehle
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Publication number: 20130023555Abstract: 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: ApplicationFiled: July 18, 2012Publication date: January 24, 2013Applicant: Abbott LaboratoriesInventors: Michael R. Michaelides, Michael L. Curtin, James H. Holms, Douglas H. Steinman
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Publication number: 20130022683Abstract: It is desired to provide a pharmaceutical composition containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof, which exhibits an inhibitory effect on activated blood coagulation factor X, and is useful as an agent for preventing and/or treating thrombosis, wherein the pharmaceutical composition exhibits favorable dissolution properties. The present invention provides a method for producing a pharmaceutical composition containing a compound represented by formula (I), comprising the step of mixing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof, one or more excipients selected from the group consisting of a sugar alcohol and a water-swelling additive, a disintegrant, and a binder under conditions for keeping the maximum water content of the granules during granulation at 10% or less.Type: ApplicationFiled: September 19, 2012Publication date: January 24, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: DAIICHI SANKYO COMPANY, LIMITED
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Patent number: 8357684Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: GrantFiled: March 2, 2011Date of Patent: January 22, 2013Assignee: Janssen Pharmaceutica NVInventors: Genesis M. Bacani, Eugene Y. Cheung, Christa C. Chrovian, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener
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Patent number: 8357674Abstract: 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 an 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: GrantFiled: June 29, 2012Date of Patent: January 22, 2013Assignee: CoNCERT Pharmaceuticals, Inc.Inventors: Julie F. Liu, Rose A. Persichetti
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Publication number: 20130018052Abstract: The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.Type: ApplicationFiled: July 13, 2012Publication date: January 17, 2013Applicant: SK CHEMICALS CO., LTD.Inventors: Ju Young LEE, Keun-Ho RYU, Jae-Sun KIM, Yong-Hyuk KIM, Dong Chul SHIN, Bong-yong LEE, Sang-hwan KANG, Hyun-Jung LEE, Hoechul JUNG, Young Ah SHIN, Euisun PARK, Jaeseung AHN
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Publication number: 20130018038Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: March 23, 2011Publication date: January 17, 2013Inventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Publication number: 20130012534Abstract: The present invention is directed to pharmaceutical compositions comprising prasugrel and a cyclodextrin derivative, and methods of making and using the same.Type: ApplicationFiled: July 5, 2012Publication date: January 10, 2013Inventors: Gerold L. MOSHER, Stephen G. Machatha, Daniel J. Cushing
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Publication number: 20130011473Abstract: A solid formulation of clopidogrel bisulfate and its preparation method are disclosed. The formulation comprises clopidogrel bisulfate as active ingredient, colloidal silicon dioxide as anti-adherent/coating and the carriers selected from diluent, binder, glidant, disintegrant and/or lubricant.Type: ApplicationFiled: August 6, 2012Publication date: January 10, 2013Inventors: Jifeng Lei, Ping Sha, Ronggen Jin, Yuwen Shi, Xinhua Shen