The Five-membered Nitrogen Hetero Ring Has Chalcogen As A Ring Member Patents (Class 514/253.1)
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Publication number: 20130203730Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: March 13, 2013Publication date: August 8, 2013Applicant: AstraZeneca ABInventor: AstraZeneca AB
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Publication number: 20130196964Abstract: The present application relates to novel aryl compounds with heterocyclic substituents, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: October 31, 2009Publication date: August 1, 2013Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Berhörster, Susanne Greschat, Karl-Heinz Thierauch, Frank Süssmeier
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Publication number: 20130190286Abstract: The present invention encompasses compounds of general formula (1) where in the groups R0to R3 and L are defined as in claim 1, which are suitable for the 5 treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: ApplicationFiled: March 25, 2011Publication date: July 25, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Patent number: 8492545Abstract: The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula I: which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit and bcr-abl inhibitors. The groups R1 and R2, identical or different, represent each a hydrogen, halogen atom, an alkyl, an alkoxy, a trifluoromethyl, an amino, an alkylamino, a dialkylamino, a solubilising group; m is 0-5 and n is 0-4; the group R3 represents an aryl or an heteroaryl group as described in claims herein.Type: GrantFiled: March 8, 2012Date of Patent: July 23, 2013Assignee: AB ScienceInventors: Alain Moussy, Philippe Reginault, Francois Bellamy, Anne Lermet
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Patent number: 8486931Abstract: The present invention relates to compounds of the general formula (I) in which A, B, R1, R2 and Het have the meaning given in claim 1; Y is a bivalent group of the formula in which D is C1-C3-alkylene, where D may have a substituent R5; R3 is hydrogen, C1-C8-alkyl or together with R4 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, and R4 is hydrogen, C1-C8-alkyl or together with R3 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, where R5 together with R5a, where present, are a bond or C1-C3-alkylene; and where one of the following conditions is satisfied: R3 together with R4 is C1-C3-alkylene which may have a radical R5a; or R3 together with R5 is C1-C3-alkylene; or R4 together with R5 is C1-C3-alkylene where the radical A is different from phenyl when the radical B is phenyl or naphthyl; and medicaments which comprise such compounds and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/oType: GrantFiled: February 29, 2008Date of Patent: July 16, 2013Assignee: Abbott GmbH & Co. KGInventors: Herve Genesle, Thorsten Oost, Charles W. Hutchins, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch, Astrid Netz, Alfred Hahn
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Publication number: 20130172326Abstract: The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(?O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.Type: ApplicationFiled: November 23, 2011Publication date: July 4, 2013Applicant: PIERRE FABRE MEDICAMENTInventors: Elisabeth Dupont-Passelaigue, Isabelle Le Roy, Christophe Pignier
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Publication number: 20130172362Abstract: Compounds that inhibit interaction between murine double minute 2 (Mdm2) protein and p53 protein and that exhibit anti-tumor activity are provided. Compounds provided by the present disclosure include imidazothiazole derivatives that inhibit interaction between Mdm2 protein and p53 protein and exhibit anti-tumor activity.Type: ApplicationFiled: January 31, 2013Publication date: July 4, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: DAIICHI SANKYO COMPANY, LIMITED
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Patent number: 8476249Abstract: Invented is a method of treating thrombocytopenia in a human, in need thereof which comprises the in vivo administration of a therapeutically effective amount of a peptide or a non-peptide TPO receptor agonist and an anti-clotting agent or agents, and optional further active ingredients, to such human.Type: GrantFiled: May 6, 2010Date of Patent: July 2, 2013Assignee: GlaxoSmithKline LLCInventors: Connie L. Erickson-Miller, Michael Arning
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Patent number: 8476278Abstract: The present invention relates to novel Thiazole Derivatives, compositions comprising the Thiazole Derivatives, and methods for using the Thiazole Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.Type: GrantFiled: October 27, 2008Date of Patent: July 2, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Panduranga Adulla P. Reddy, Tzu T. Wong, Lianyun Zhao, Shuyi Tang, Marc A. Labroli, Timothy J. Guzi, M. Arshad Siddiqui
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Patent number: 8476277Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: April 25, 2008Date of Patent: July 2, 2013Assignee: Purdue Pharma L.P.Inventor: Laykea Tafesse
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Publication number: 20130164259Abstract: The present invention relates to 1,4-Substituted Piperazine Derivatives, compositions comprising one or more 1,4-Substituted Piperazine Derivatives, and methods of using the 1,4-Substituted Piperazine Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: December 20, 2010Publication date: June 27, 2013Inventors: Cliff C. Cheng, Xiaohua Huang, Gerald W. Shipps, JR.
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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: 20130137703Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: January 9, 2013Publication date: May 30, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130123239Abstract: The invention relates to compounds of Formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: June 22, 2011Publication date: May 16, 2013Inventor: Noriyuki Kurose
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Publication number: 20130115194Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: November 2, 2012Publication date: May 9, 2013Inventors: Daniel D. LONG, Robert Murray MCKINNELL, Lan JIANG, Mandy LOO, Kassandra LEPACK, Lori Jean VAN ORDEN, Gavin OGAWA, Xiaojun HUANG, Weijiang ZHANG
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Patent number: 8435976Abstract: The invention relates to compounds of formula (I) which are useful as kinase inhibitors, more specifically useful as PIM kinase inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same, either alone or in combination, to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: GrantFiled: September 8, 2010Date of Patent: May 7, 2013Assignee: F. Hoffmann-La RocheInventors: Xiaojing Wang, Allen J. Ebens, Jr.
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Publication number: 20130109675Abstract: A series of oxazole and thiazole compounds are shown herein to be small molecule inhibitors of the Wnt pathway that specifically target the activity of the stabilized pool of ?-cat oxazole and thiazole 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, cancer, and others.Type: ApplicationFiled: August 27, 2012Publication date: May 2, 2013Inventors: Ramanuj Dasgupta, Foster Gonsalves
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Publication number: 20130102592Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: December 5, 2012Publication date: April 25, 2013Applicant: SAREUM LIMITEDInventor: Sareum Limited
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Publication number: 20130096117Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: October 2, 2012Publication date: April 18, 2013Inventors: Julie Nicole HAMBLIN, Paul Spencer JONES, Suzanne Elaine KEELING, Joelle LE, Nigel James PARR
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Patent number: 8420658Abstract: Method and composition of Carboxyamidotriazole orotate for treating age-related macular degeneration and other angiogenesis-dependent diseases.Type: GrantFiled: May 24, 2010Date of Patent: April 16, 2013Assignee: Tactical Therapeutics IncInventor: Rashida A Karmali
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Publication number: 20130090309Abstract: The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: April 30, 2012Publication date: April 11, 2013Inventors: Eric Thomas Romeo, Michelle R. Machacek, Benjamin Wesley Trotter, Thomas Allen Miller, Brian Michael Andresen, Neville John Anthony, Brandon M. Taoka, Yuan Liu
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Patent number: 8410090Abstract: The invention relates to heterocyclylamide-substituted thiazoles, pyrroles and thiophenes and processes for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, in particular for the use as antiviral agents, especially against cytomegaloviruses.Type: GrantFiled: July 1, 2006Date of Patent: April 2, 2013Assignee: AiCuris GmbH & Co. KGInventors: Holger Zimmermann, David Brueckner, Kerstin Henninger, Martin Hendrix, Martin Radtke
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Publication number: 20130079351Abstract: A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.Type: ApplicationFiled: November 15, 2012Publication date: March 28, 2013Applicant: ASTELLAS PHARMA, INC.Inventor: ASTELLAS PHARMA, INC.
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Publication number: 20130079325Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: November 14, 2012Publication date: March 28, 2013Inventors: Jennifer R. Allen, Biswas Kaustav, Frank Chavez, Ning Chen, Frenel Fils De Morin, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Guomin Yao
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Publication number: 20130079340Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings, having histamine H3 antagonistic activity can be used in pharmaceutical compositions.Type: ApplicationFiled: October 25, 2012Publication date: March 28, 2013Inventors: Florencio Zaragoza Dorwald, Rolf Hohlweg, Inge Thoger Christensen, Jane Marie Lundbeck, Knud Erik Andersen
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Patent number: 8404691Abstract: There is provided compounds that inhibit interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. Compounds include imidazothiazole derivatives that can inhibit interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity.Type: GrantFiled: July 15, 2011Date of Patent: March 26, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Kouichi Uoto, Yuuichi Sugimoto, Hiroyuki Naito, Masaki Miyazaki, Keisuke Yoshida, Masashi Aonuma
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Publication number: 20130072474Abstract: The present invention relates to the use of masitinib or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of dementia of Alzheimer's type, at appropriate dosage regimen.Type: ApplicationFiled: March 9, 2011Publication date: March 21, 2013Applicant: AB SCIENCEInventors: Jean-Pierre Kinet, Alain Moussy, Colin Field
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Publication number: 20130072467Abstract: The present invention provides a novel compound having a superior activity as an ERR-? modulator and useful as an agent for the prophylaxis or treatment of ERR-? associated diseases. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: August 3, 2012Publication date: March 21, 2013Inventors: Shigemitsu MATSUMOTO, Koji Ono, Yusuke Tominari, Taisuke Katoh, Kazuhiro Miwa, Atsushi Hasuoka, Shinichi Imamura
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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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PYRIDYLTHIAZOLE-BASED UREAS AS INHIBITORS OF RHO ASSOCIATED PROTEIN KINASE (ROCK) AND METHODS OF USE
Publication number: 20130059839Abstract: Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.Type: ApplicationFiled: April 18, 2011Publication date: March 7, 2013Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.Inventors: Nicholas J. Lawrence, Roberta Pireddu, Said M. Sebti -
Patent number: 8389516Abstract: 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 or CH, or CF; R2 and R3 are as defined in the description.Type: GrantFiled: June 7, 2011Date of Patent: March 5, 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: 20130053345Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: ApplicationFiled: May 4, 2011Publication date: February 28, 2013Inventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl, Ying Wang
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Publication number: 20130053361Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: ApplicationFiled: July 5, 2012Publication date: February 28, 2013Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
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Publication number: 20130040930Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Patent number: 8362249Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R6, 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: GrantFiled: April 21, 2010Date of Patent: January 29, 2013Assignee: Boehringer Ingelheim International GmbHInventors: John David Ginn, Daniel Richard Marshall, Anthony S. Prokopowicz, Sabine Schlyer, Robert Sibley, Michael Robert Turner, Di Wu, Frank Wu
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Publication number: 20130023522Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R8, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: July 17, 2012Publication date: January 24, 2013Applicant: MERCK PATENT GMBHInventors: Henry YU, Jiezhen LI, Thomas E. RICHARDSON, Pandi BHARATHI, Brian H. HEASLEY, Andreas GOUTOPOULOS
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Publication number: 20130018048Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: ApplicationFiled: April 4, 2011Publication date: January 17, 2013Applicant: Merck Sharp & Dohme Corp.Inventors: ZhiQiang Yang, Philippe G. Nantermet, Constantine Kreatsoulas, Keith P. Moore, Evan Foster Shalen
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Patent number: 8354401Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof.Type: GrantFiled: October 27, 2009Date of Patent: January 15, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Seigo Ishibuchi, Hidemasa Hikawa, Akiko Tarao, Jun-ichi Endoh, Kunitomo Adachi, Kazuhiro Maeda, Kaoru Tashiro
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Publication number: 20130005701Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: ApplicationFiled: January 27, 2012Publication date: January 3, 2013Applicant: Bayer Pharma AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Röhrig, Elisabeth Perzborn, Karl-Heinz Schlemmer, Joseph Pernerstorfer
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Publication number: 20130005710Abstract: The present invention provides a novel aminopyridine derivative that is excellent in pharmaceutical effects such as a neuroprotective effect, a neurogenesis or nerve regeneration promoting effect, and a cognitive function improving effect and, preferably, is low toxic and delivered at a high rate to the central nervous system.Type: ApplicationFiled: November 17, 2010Publication date: January 3, 2013Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Norihito Tokunaga, Yuhei Miyanohana
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Publication number: 20120328691Abstract: The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 29, 2007Publication date: December 27, 2012Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Tzu T. Wong, Praveen K. Tadikonda, M. Arshad Siddiqui, Marc A. Labroli, Cory Poker, Timothy J. Guzi
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Publication number: 20120321622Abstract: The present invention relates to novel thiazole-substituted indolin-2-ones as inhibitors of CSCPK and related kinases; to methods of inhibiting cancer stem cells by using a kinase inhibitor; to pharmaceutical compositions containing such compounds; and to methods of using such compounds in the treatment of a protein kinase related disorder in a mammal; and to processes of making such compounds and intermediates thereof.Type: ApplicationFiled: August 27, 2012Publication date: December 20, 2012Applicant: Boston Biomedical, Inc.Inventors: Chiang Jia Li, Ji-Feng Liu, Youzhi Li, Wei Li, Harry Rogoff
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Patent number: 8334290Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: GrantFiled: October 30, 2006Date of Patent: December 18, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
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Publication number: 20120316162Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumours.Type: ApplicationFiled: August 22, 2012Publication date: December 13, 2012Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Kai SCHIEMANN, Melanie SCHULTZ, Andree BLAUKAT, Ingo KOBER
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Publication number: 20120302579Abstract: Invented is a method of treating cancer and pre-cancerous syndromes in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal.Type: ApplicationFiled: June 4, 2012Publication date: November 29, 2012Inventor: Connie Erickson-Miller
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Publication number: 20120302577Abstract: The present invention relates to the use of masitinib or a pharmaceutically acceptable salt thereof, and in particular of masitinib mesylate, for the preparation of a medicament for the treatment of GIST, to the use of this therapy for the treatment of GIST, and a method of treating mammals, including humans, suffering from GIST by administering to said mammal in need of such treatment an effective dose of masitinib, and in particular masitinib mesylate.Type: ApplicationFiled: January 28, 2011Publication date: November 29, 2012Applicant: AB SCIENCEInventors: Alain Moussy, Jean-Pierre Kinet
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Patent number: 8318735Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.Type: GrantFiled: October 29, 2007Date of Patent: November 27, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Gerald W. Shipps, Jr., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Lianyun Zhao, Shuyi Tang, Tzu T. Wong, Praveen K. Tadikonda, Luis E. Torres, M. Arshad Siddiqui, Michael P. Dwyer, Kartik M. Keertikar, Timothy J. Guzi
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Publication number: 20120295918Abstract: Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human.Type: ApplicationFiled: June 4, 2012Publication date: November 22, 2012Inventor: Connie Erickson-Miller
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Publication number: 20120289495Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, Y, Q, X, B and L are as defined herein, and methods of making and using the same.Type: ApplicationFiled: January 13, 2011Publication date: November 15, 2012Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
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Publication number: 20120283242Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].Type: ApplicationFiled: January 28, 2011Publication date: November 8, 2012Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida