Ring Nitrogen In The Bicyclo Ring System Patents (Class 514/235.2)
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Publication number: 20130158031Abstract: This invention relates to novel alkyne-bridged hetero-aromatics as described in the specification which are PDE10A inhibitors and useful for the treatment of neurological, psychiatric disorder, metabolic disorders, such as Schizophrenia, Parkinson's disease, Huntington's disease, Alzheimer's disease, learning memory disorder, drug addiction (abuse), sleeping disorder, depression, obesity, non-insulin dependent diabetes, bipolar disorder, obsessive compulsive disorder, or pain; to process for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.Type: ApplicationFiled: December 18, 2012Publication date: June 20, 2013Applicant: SU ZHOU JING HONG BIOTECH CO., LTD.Inventors: Zhen-Wei CAI, Ding ZHOU, Yougang LIN, Ping CHEN
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Publication number: 20130158029Abstract: The invention refers to compounds of general formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: May 26, 2011Publication date: June 20, 2013Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia López, Antoni Torrens Jover, José Luis Diaz Fernández, Ana Maria Caamaño Moure
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Publication number: 20130158006Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: ApplicationFiled: November 28, 2012Publication date: June 20, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Patent number: 8466148Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.Type: GrantFiled: November 7, 2011Date of Patent: June 18, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20130150363Abstract: The present invention relates to a method of treating cancer in a patient comprising administering to the patient therapeutically effective amounts of: a) a compound of formula A: or a pharmaceutically acceptable salt thereof, wherein R1-R4, p, and q are as defined; and (b) an erbB inhibitor that inhibits erbB-1 or erbB-2 or erbB-3 receptor or a combination thereof. The method of the present invention addresses a need in the art with the discovery of a combination therapy that shows evidence of being a more effective therapy than previously disclosed therapies.Type: ApplicationFiled: January 29, 2013Publication date: June 13, 2013Applicant: GlaxoSmithKlineInventor: GlaxoSmithKline
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Publication number: 20130150339Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: ApplicationFiled: December 6, 2012Publication date: June 13, 2013Applicant: Amgen Inc.Inventor: Amgen Inc.
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Publication number: 20130143867Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.Type: ApplicationFiled: January 18, 2013Publication date: June 6, 2013Applicant: SYCHRONEURON INC.Inventor: SYCHRONEURON INC.
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Publication number: 20130143881Abstract: This invention relates crystalline hydrates of N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, Compound (I). The invention provides methods for treatment of cancer by exploiting the modulation of protein kinase activity. The invention also provides pharmaceutical compositions containing a crystalline hydrate of Compound (I) and a pharmaceutically acceptable excipient.Type: ApplicationFiled: March 11, 2011Publication date: June 6, 2013Applicant: Exelixis, Inc.Inventors: Hilary Cannon, Feirong Kang, Frederick G. Vogt
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Publication number: 20130143860Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.Type: ApplicationFiled: January 31, 2013Publication date: June 6, 2013Applicant: Astellas Pharma Inc.Inventor: Astellas Pharma Inc.
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Publication number: 20130142790Abstract: The present invention relates to a method of treating cancer in a patient comprising administering to the patient therapeutically effective amounts of: a) a compound of formula A: or a pharmaceutically acceptable salt thereof, wherein R1—R4, p, and q are as defined; and (b) an erbB inhibitor that inhibits erbB-1 or erbB-2 or erbB-3 receptor or a combination thereof. The method of the present invention addresses a need in the art with the discovery of a combination therapy that shows evidence of being a more effective therapy than previously disclosed therapies.Type: ApplicationFiled: January 29, 2013Publication date: June 6, 2013Applicant: GlaxoSmithKlineInventor: GlaxoSmithKline
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Publication number: 20130143882Abstract: Compounds having the structure which are selective inhibitors of P13K (phosphatidylinositol 3-kinase-delta), 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.Type: ApplicationFiled: June 30, 2011Publication date: June 6, 2013Applicant: Amgen Inc.Inventor: Paul John Dransfield
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Publication number: 20130143866Abstract: Compositions of matter including ?-tocotrienol and SU11274 are disclosed herein. A variety of Met kinase inhibitors may be used in conjunction with tocotrienols in the treatment or prevention of cancer. Combinations of ?-tocotrienol and SU11274 inhibit the cell growth of +SA mammary tumor cells.Type: ApplicationFiled: December 2, 2012Publication date: June 6, 2013Inventor: Paul W. Sylvester
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Publication number: 20130143863Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, A1, A2, A3, A4, A5 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful, for example, as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.Type: ApplicationFiled: November 29, 2012Publication date: June 6, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130137686Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: November 5, 2012Publication date: May 30, 2013Inventor: Esanex, Inc.
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Publication number: 20130137678Abstract: Described herein are Compounds, compositions comprising such Compounds, and the use of such Compounds and compositions as anti-viral agents. In one aspect, provided herein are methods of inhibiting viral replication using Compounds described herein or compositions thereof. In another aspect, provided herein are methods for preventing a symptom of a viral infection using a Compound, or a composition thereof. In another aspect, provided herein are methods of treating and/or managing viral infection using a compound or a composition thereof.Type: ApplicationFiled: May 31, 2011Publication date: May 30, 2013Applicant: MOUNT SINAI SCHOOL OF MEDICINEInventors: Megan Shaw, Hans-Heinrich Hoffmann, Adolfo Garcia-Sastre, Peter Palese
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Patent number: 8450348Abstract: The present invention provides derivatives of squaric acid, in particular derivatives of 3,4-diamino-cyclobut-3-ene-1,2-dione and tautomers and isomers thereof, as a single stereoisomer or a mixture of stereoisomers, or as a pharmaceutically acceptable salt thereof. These compounds show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: GrantFiled: February 21, 2007Date of Patent: May 28, 2013Assignee: Forma TM, LLCInventors: Krishna K. Murthi, Roland Köstler, Chase Smith, Tilman Brandstetter, Arthur F. Kluge
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Publication number: 20130131060Abstract: The present invention relates to a compound of formula (I) wherein R1, R2 and R3 are as defined in the description and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula I and of the salts thereof. The compounds of formula I are suitable for treating tumors.Type: ApplicationFiled: December 10, 2010Publication date: May 23, 2013Applicant: Johannes Gutenberg-Universität MainzInventors: Gerd Dannhardt, Jan-Peter Kramb, Stanislav Plutizki
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Publication number: 20130131061Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R5 and R6 are as defined in the specification.Type: ApplicationFiled: January 11, 2013Publication date: May 23, 2013Applicant: KARO BIO ABInventors: Patrik Rhonnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstal, Aiping Cheng
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Publication number: 20130123258Abstract: Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of a Plasmodium infection in the recipient subject, or to reduce the likelihood of the onset or establishment of a Plasmodium infection if administered prior to the parasite contacting the subject. The therapeutic compositions can be formulated to provide an effective single dose amount of an antimalarial compound or multiple doses for administering over a period of time.Type: ApplicationFiled: October 26, 2012Publication date: May 16, 2013Inventors: Roman Manetsch, Richard Matthew Cross, Niranjan Kumar Namelikonda, Dennis Edward Kyle, Tina Susanna Mutka, Alexis Nichole LaCrue, Jordany Richarlson Maignan, Fabian Ernesto Saenz
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Publication number: 20130123259Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: December 20, 2012Publication date: May 16, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
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Publication number: 20130123344Abstract: Disclosed are compounds and pharmaceutical compositions containing compounds that inhibit JMJD2 proteins, including those of the formula (I): wherein R1, R2, R3, R4, and R5 are as defined herein or pharmaceutically acceptable salts thereof. Also disclosed is a method of preventing or treating a viral infection of a host, comprising administering to the host an effective amount of an inhibitor of the JMJD2 family of histone demethylases, for example, a compound of the formula (I). The viral infection may be a primary infection, reactivation of a virus after latency in a host, or may be in a mammal that has undergone, is undergoing, or will undergo immunosuppressive therapy.Type: ApplicationFiled: January 22, 2013Publication date: May 16, 2013Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human ServicesInventor: The United States of America, as Represented by the Secretary, Department of Health and Human Services
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Publication number: 20130116231Abstract: The present invention relates to 1,4-dihydropyridazinone derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: July 7, 2011Publication date: May 9, 2013Inventors: Kevin Wilson, Michael Altman, Kathryn Lipford, Catherine White, Matthew Daniels
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Publication number: 20130116229Abstract: The present invention relates to compounds 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: November 8, 2012Publication date: May 9, 2013Applicants: AbbVie Inc., Abbott GmbH & Co. KGInventors: Abbott GmbH & Co.KG, AbbVie Inc.
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Publication number: 20130116234Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.Type: ApplicationFiled: November 1, 2012Publication date: May 9, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130109653Abstract: The present invention provides a substituted pyridine compound or a pharmacologically acceptable salt thereof which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a compound represented by a general formula (I), wherein R1 is H, optionally substituted alkyl, OH, optionally substituted alkoxy, alkylsulfonyl, optionally substituted amino, carboxy, optionally substituted carbonyl, CN, halogeno, optionally substituted phenyl, optionally substituted aromatic heterocyclyl, optionally substituted saturated heterocyclyl, optionally substituted saturated heterocyclyloxy or optionally substituted saturated heterocyclylcarbonyl, etc., and the like.Type: ApplicationFiled: July 8, 2011Publication date: May 2, 2013Applicants: UBE INDUSTRIES, LTD., DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsuyoshi Nakamura, Hidenori Namiki, Naoki Terasaka, Akiko Shima, Masahiko Hagihara, Noriaki Iwase, Katsunori Takata, Osamu Kikuchi, Kazunari Tsuboike, Hiroyuki Setoguchi, Kenji Yoneda, Hidetoshi Sunamoto, Koji Ito
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Publication number: 20130102604Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1. The compound may be used, for example, for the treatment or prophylaxis of obesity, hyperglycemia, dyslipidemia, and type 1 or type 2 diabetes.Type: ApplicationFiled: December 10, 2012Publication date: April 25, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8426406Abstract: The present invention is related to glucocorticoid receptor agonists comprised of a compound represented by formula (1) which is 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivative or a salt thereof and novel pharmacological effects of the glucocorticoid receptor agonists. In the formula (1), R1 represents formula (2a), (3a), (4a) or (5a); R2 represents —(CO)—R8, —(CO)O—R9, or the like; R2—O— is substituted at the 4- or -5-position of benzene ring A; R3 represents a lower alkyl group; R4, R5, R6 or R7 represents a halogen atom, a lower alkyl group which may have a substituent, or the like; m, n, p or q represents 0, 1 or the like; R8, R9 or the like represents a lower alkyl group which may have a substituent, a lower alkenyl group, or the like.Type: GrantFiled: May 12, 2009Date of Patent: April 23, 2013Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Masatomo Kato, Miwa Takai, Takahiro Matsuyama, Tatsuji Kurose, Yumi Hagiwara, Mamoru Matsuda, Toshiyuki Mori, Kenji Imoto, Atsuyoshi Dota
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Publication number: 20130096119Abstract: The invention relates to isoquinolin-3-ylurea derivatives of formula (I) wherein R1 represents (C1-C3)alkyl, (C1-C3)haloalkyl or cyclopropyl, R4 represents H and the substituents R2 and R3 and R5 have the meanings disclosed in the specification; and to the salts of such compounds. These compounds are useful for the prevention or the treatment of bacterial infections.Type: ApplicationFiled: March 30, 2011Publication date: April 18, 2013Inventors: Daniel Bur, Markus Gude, Christian Hubschwerlen, Philippe Panchaud
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Publication number: 20130096089Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.Type: ApplicationFiled: September 7, 2012Publication date: April 18, 2013Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
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Publication number: 20130096120Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: ApplicationFiled: October 11, 2012Publication date: April 18, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Publication number: 20130096118Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.Type: ApplicationFiled: June 16, 2011Publication date: April 18, 2013Inventors: Chunjian Liu, James Lin, George V. DeLucca, Batt G. Douglas, Qingjie Liu
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Publication number: 20130096083Abstract: The use of isoquinolones for preparing drugs, including novel isoquinolones as well as their synthesis method. In particular, isoquinolone derivatives used in the treatment of pathological angiogenesis, and more particularly of cancer.Type: ApplicationFiled: March 1, 2011Publication date: April 18, 2013Applicants: UNIVERSITE JOSEPH FOURIER, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Andrei Popov, Aurelie Juhem, Jean-Claude Florent, Chi-Hung N'Guyen
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Publication number: 20130096121Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bc1-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bc1-xL protein.Type: ApplicationFiled: October 11, 2012Publication date: April 18, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Publication number: 20130096122Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.Type: ApplicationFiled: December 6, 2012Publication date: April 18, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Patent number: 8420637Abstract: The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I wherein Y, Q, Z, R, R1 and R2 are as defined in the specification. The present invention further comprises pharmaceutical compositions, e.g. ophthalmic compositions, including said compound of formula I.Type: GrantFiled: September 22, 2009Date of Patent: April 16, 2013Assignee: Allergan, Inc.Inventors: June Chen, Simon Pettit, Hans Fliri
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Patent number: 8420638Abstract: The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.Type: GrantFiled: June 29, 2011Date of Patent: April 16, 2013Assignee: Gemin X Pharmaceuticals Canada Inc.Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrance W. Deyle
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Publication number: 20130090323Abstract: 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 11, 2013Applicant: Amgen Inc.Inventors: Paul John Dransfield, Felix Gonzalez Lopez De Turiso, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
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Publication number: 20130089518Abstract: The invention provides novel pyrimidine derivatives of formula I, to methods of preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for using such compounds in treatment of diseases including cancer; wherein R1, R2, R3, R4, R5, L, A, D, E, Z, and Y are as defined in the specification.Type: ApplicationFiled: May 20, 2011Publication date: April 11, 2013Applicant: CHEMILIA ABInventors: Marita Högberg, Tommy Johansson, Emma Dahlstedt, Olof Smitt
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Patent number: 8415349Abstract: The invention provides derivatives of azabicyclo alkane having formula (ID), and the method for making them, wherein each substitute in formula (ID) is same as defined in the description.Type: GrantFiled: September 14, 2012Date of Patent: April 9, 2013Assignee: Jiangsu Hansoh Pharmaceuticals Co., Ltd.Inventors: Peng Cho Tang, Zhigang Lin, Hejun Lü, Fuqiang Zhao, Li Li, Fanglong Yang, Jianghong Fu, Lin Wang, Guangyuan Shen, Dongliang Guan
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Publication number: 20130085131Abstract: 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 pi 110? 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 LympType: ApplicationFiled: June 30, 2011Publication date: April 4, 2013Applicant: Amgen Inc.Inventors: Minna Bui, Benjamin Fisher, Xiaolin Hao, Brian Lucas
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Publication number: 20130084275Abstract: The present invention relates generally to methods and compositions for reducing Interleukin-4 or Interleukin-13 signaling, in particular to treat asthma and atopic dermatitis. The inventors have found that Rac/PAK mediated endocytosis of the ligand bound type I (IL-4R with the chains IL-4Ra and IL-2-Rg) and/or type II receptor (IL-13R with the chains IL-4Ra and IL-13Ra1) is needed for the IL-4 and/or IL-13 mediated activation of downstream signalling events including phosphorylation of Stat family transcrition factors. These discoveries enable new methods of screening compounds that modulate Interleukin-4 and Interleukin-13 signalling, as well as new methods for treating conditions characterized by increased Interleukin-4 and Interleukin-13 levels. These conditions include inflammatory conditions, asthma bronchiale, atopic dermatitis, allergies, atopic syndromes, allergic rhinitis, and th2-induced conditions.Type: ApplicationFiled: April 26, 2012Publication date: April 4, 2013Applicant: Technische Universitat DresdenInventors: Christian Bôkel, Thomas Weidemann
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Patent number: 8410087Abstract: The purpose of the present invention is to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein R1 is a hydrogen atom or a halogen atom; R2 is a group represented by wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof.Type: GrantFiled: October 18, 2007Date of Patent: April 2, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Yasuma, Osamu Ujikawa, Masahiro Itoh, Kazuko Aoki
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Publication number: 20130079342Abstract: Substituted bicyclic heteroaryls of the following formulae 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 LeukemiaType: ApplicationFiled: June 30, 2011Publication date: March 28, 2013Inventors: Paul John Dransfield, Felix Gonzalez Lopez De Turiso, Vatee Pattaropong, Jillian L. Simard
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Publication number: 20130079343Abstract: Disclosed are a 1,3,6-substituted indole compound having inhibitory activity for protein kinases, a pharmaceutically acceptable thereof, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth including the compound as an active ingredient. Since the novel indole compound exhibits superior inhibitory activity for various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.Type: ApplicationFiled: November 24, 2012Publication date: March 28, 2013Applicant: Korea Institute of Science and TechnologyInventor: Korea Institute of Science and Technology
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Patent number: 8404683Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.Type: GrantFiled: November 3, 2010Date of Patent: March 26, 2013Assignee: Janssen Pharmaceutical N.V.Inventors: Jean Ferand Armand Lacrampe, Christophe Meyer, Yannick Aimè Eddy Ligny, Imre Christian Francis Csoka, Luc Van Hijfte, Janine Arts, Bruno Schoentjes, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert
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Publication number: 20130072485Abstract: The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.Type: ApplicationFiled: November 6, 2012Publication date: March 21, 2013Applicants: Dana-Farber Cancer Institute, Inc., Whitehead Institute for Biomedical ResearchInventors: Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc.
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Publication number: 20130065890Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, T, U, V, X, Y, Z, G, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder, e.g., cancer or age-related macular degeneration, with such a compound.Type: ApplicationFiled: November 8, 2012Publication date: March 14, 2013Inventor: Hutchison Medipharma Enterprises Limited
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Publication number: 20130065897Abstract: The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.Type: ApplicationFiled: December 22, 2010Publication date: March 14, 2013Applicant: PETER MACCALLUM CANCER INSTITUTEInventors: Julie Ann Spicer, Kristiina Maria Huttunen, Dani Michelle Lyons, Joseph Albert Trapani, Mark John Smyth, William Alexander Denny
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Publication number: 20130059851Abstract: A method of identifying a subject having cancer who is likely to benefit from treatment with a combination therapy with a RAF inhibitor and a second inhibitor is provided. A method of treating cancer in a subject in need thereof is also provided and includes administering to the subject an effective amount of a RAF inhibitor and an effective amount of a second inhibitor, wherein the second inhibitor is a MEK inhibitor, a CRAF inhibitor, a CrkL inhibitor or a TPL2/COT inhibitor. A method of identifying a kinase target that confers resistance to a first inhibitor is also provided.Type: ApplicationFiled: March 9, 2011Publication date: March 7, 2013Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Levi A. Garraway, Cory M. Johannessen
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Patent number: 8389720Abstract: The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S 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 the neuropeptide S receptor is involved.Type: GrantFiled: November 3, 2009Date of Patent: March 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Mark T. Bilodeau, Christopher D. Cox, John C. Hartnett, Nathan R. Kett, Yiwei Li, Peter J. Manley, Jeffrey Melamed, William D. Shipe, B. Wesley Trotter, Amy Zartman