Quinoline Or Isoquinoline (including Hydrogenated) Patents (Class 544/128)
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Publication number: 20130053348Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: September 12, 2012Publication date: February 28, 2013Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Sing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, JR.
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Patent number: 8383094Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: September 29, 2009Date of Patent: February 26, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Makonen Belema, Van N. Nguyen, Michael Serrano-Wu, Denis R. St. Laurent, Yuping Qiu, Min Ding, Nicholas A. Meanwell, Lawrence B. Snyder
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Publication number: 20130045975Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.Type: ApplicationFiled: February 10, 2012Publication date: February 21, 2013Applicant: KALYPSYS, INC.Inventors: Steven P. Govek, Clay Beauregard, Daniel A. Gamache, Mark R. Hellberg, Stewart A. Noble, Andrew K. Shiau, David J. Thomas, John M. Yanni
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Publication number: 20130041046Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Applicant: SENOMYX, INC.Inventors: Catherine TACHDJIAN, Xiao Qing TANG, Donald S. KARANEWSKY, Guy SERVANT, Xiaodong LI, Feng ZHANG, Qing CHEN, Hong ZHANG, Timothy James DAVIS, Vincent DARMOHUSODO, Melissa Sue WONG, Victor SELCHAU
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Publication number: 20130040931Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).Type: ApplicationFiled: January 14, 2011Publication date: February 14, 2013Applicant: Amgen Inc.Inventors: Nick A. Paras, James Brown, Yuan Cheng, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Ana Elena Minatti, Thomas Nixey, Timothy Powers, Christopher M. Tegley, Qiufen Xue, Bryant Yang, Wenge Zhong
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Publication number: 20130035327Abstract: 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: ApplicationFiled: October 8, 2012Publication date: February 7, 2013Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Publication number: 20130030172Abstract: Methods of preparing compounds of formula i(1): or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 join together with the nitrogen atom to which they are attached to form a 6 membered heterocycloalkyl group; X1 is H, Br, Cl or F; X2 is H, Br, Cl or F; s is 2-6; n1 is 0-2; and n2 is 0-2.Type: ApplicationFiled: December 4, 2009Publication date: January 31, 2013Applicant: Exelixis, Inc.Inventors: Jo Ann Wilson, Sharique Zuberi, Erick Goldman, James Kanter
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Publication number: 20130028989Abstract: Targeting uncontrolled cell proliferation and resistance to DNA damaging chemotherapeutics with at least one reagent has significant potential in cancer treatment. Replication Protein A, the eukaryotic single-strand (ss) DNA binding protein, is essential for genomic maintenance and stability via roles in both DNA replication and repair. Reported herein are small molecules that inhibits the in vitro, in vivo, and cellular ssDNA binding activity of RPA, thereby disrupting the eukaryotic cell cycle, inducing cytotoxicity and increasing the efficacy of chemotherapeutic agents damage DNA, and/or disrupt its replication and/or function. These results provide new insights into the mechanism of RPA-ssDNA interactions in chromosome maintenance and stability. This represents a molecularly targeted eukaryotic DNA binding inhibitor and demonstrates the utility of targeting a protein-DNA interaction as a means of studying the cell cycle and providing a therapeutic strategy for cancer treatment.Type: ApplicationFiled: February 5, 2011Publication date: January 31, 2013Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: John J. Turchi, Sarah Shuck
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Publication number: 20130029949Abstract: Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.Type: ApplicationFiled: July 20, 2012Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias HOFFMANN, Daniel BISCHOFF, Georg DAHMANN, Jasna KLICIC, Gerhard SCHAENZLE, Stefan Ludwig Michael WOLLIN, Serge Gaston CONVERS-REIGNIER, Stephen Peter EAST, Frederic Jacques MARLIN, Clive McCARTHY, John SCOTT
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Patent number: 8362250Abstract: The present invention provides dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes provided in this invention can comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been substituted with specific groups to provide beneficial properties.Type: GrantFiled: September 21, 2009Date of Patent: January 29, 2013Assignee: Enzo Biochem, Inc.Inventors: Praveen Pande, Hilary J. Cox, Yuejun Xiang, Wayne Forrest Patton
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Patent number: 8362008Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.Type: GrantFiled: December 11, 2008Date of Patent: January 29, 2013Assignee: The University Of EdinburghInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Publication number: 20130023518Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R5 have the significance given in claim 1, can be used as a medicament.Type: ApplicationFiled: September 28, 2012Publication date: January 24, 2013Applicant: Hoffmann-La Roche IncInventor: Hoffmann-La Roche Inc.
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Publication number: 20130018043Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.Type: ApplicationFiled: July 11, 2012Publication date: January 17, 2013Inventors: Joseph A. Bilotta, Adrian Wai-Hing Cheung, Fariborz Firooznia, Kevin Richard Guertin, Stuart Hayden, Nancy-Ellen Haynes, Christine M. Lukacs-Lesburg, Nicholas Marcopulos, Eric Mertz, Lida Qi, Yimin Qian, Sung-Sau So, Jenny Tan, Kshitij C. Thakkar
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Publication number: 20130012499Abstract: The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.Type: ApplicationFiled: March 23, 2011Publication date: January 10, 2013Applicant: GlaxoSmithKline LLCInventors: Carl A. Brooks, Mui Cheung, S. Eidam Hilary, Ryan M. Fox, Mark A. Hilfiker, Eric S. Manas
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Patent number: 8350028Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein R1 and R2 are as described herein and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonists, useful for the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.Type: GrantFiled: March 5, 2009Date of Patent: January 8, 2013Assignee: Hofmann-La Roche Inc.Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Patent number: 8349830Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: October 26, 2010Date of Patent: January 8, 2013Assignee: Merck Sharp & DohmeInventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
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Publication number: 20130005965Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optType: ApplicationFiled: July 2, 2012Publication date: January 3, 2013Applicants: BRISTOL-MYERS SQUIBB COMPANY, ALBANY MOLECULAR RESEARCH, INC.Inventors: Bruce F. MOLINO, Shuang LIU, Peter R. GUZZO, James P. BECK
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Publication number: 20130004509Abstract: The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of BRAF. In particular embodiments, the invention concerns mutations in a BRAF sequence that confer resistance to a BRAF inhibitor. Identification of such mutations in a BRAF sequence allows the identification and design of second-generation BRAF inhibitors. Methods and kits for detecting the presence of a mutant BRAF sequence in a sample are also provided.Type: ApplicationFiled: February 22, 2011Publication date: January 3, 2013Inventor: Levi Garraway
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Publication number: 20130005705Abstract: The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling 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: June 27, 2012Publication date: January 3, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Hervé Geneste, Michael Ochse, Karla Drescher, Berthold Behl, Loic Laplanche, Jürgen Dinges, Clarissa Jakob
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Patent number: 8344137Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R5 have the significance given in claim 1, can be used as a medicament.Type: GrantFiled: April 7, 2011Date of Patent: January 1, 2013Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Jim Zhen Wu, Mingwei Zhou
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Publication number: 20120329796Abstract: The present invention relates to compound (I) wherein: means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a —CN group, a hydroxyl group, a —COOR1 group, a (C1-C3)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, a —NO2 group, a —NRiR2 group, a (C1-C4)alkoxy group, a phenoxy group and a (C1-C3)alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n? is 1 or 2, R? is a hydrogen atom, a halogen atom or a group chosen among a (Ci-C3)alkyl group, a hydroxyl group, a —COOR1 group, a —NO2 group, a —NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (Ci-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a —CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating pathological or nonpathological conditions linked with premature aging.Type: ApplicationFiled: June 14, 2010Publication date: December 27, 2012Applicants: SOCIETE SPLICOS, UNIVERSITE MONTPELLIER 2, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Jamal Tazi, Florence Mahuteau, Romain Najman, Didier Scherrer, Julien Santo
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Publication number: 20120323003Abstract: The disclosure relates to tetrahydroisoquinoline sulfonamide compounds of formula I: wherein R1, R2, n and B are as defined in the disclosure, their preparation and their use in therapies for the treatment of central nervous system diseases such as vigilance and sleep disorders, narcolepsy, Alzheimer's disease and other dementias, Parkinson's disease, attention disorders in hyperkinetic children, memory and learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness and travel sickness.Type: ApplicationFiled: August 24, 2012Publication date: December 20, 2012Applicant: SANOFIInventors: Juan Antonio DIAZ MARTIN, Maria Dolores JIMENEZ BARGUENO
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Publication number: 20120322785Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.Type: ApplicationFiled: December 14, 2011Publication date: December 20, 2012Applicant: Genentech, Inc.Inventors: Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel Kintz, Hans Edward Purkey
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Publication number: 20120316168Abstract: The present invention provides a quinolone compound represented by General Formula (1) or a salt thereof, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a phenyl group optionally being substituted with one or more substituents, etc.; R4 represents a halogen atom; R5 represents a hydrogen atom or halogen atom; R6 represents a hydrogen atom; and R7 represents a hydroxyl group, etc. The quinolone compound have a functional improvement effect, which suppresses progression of neurological dysfunction by inhibiting the chronic progression of Parkinson's disease or protecting dopamine neurons from the disease etiology, thereby prolonging the period before first administration begins.Type: ApplicationFiled: August 21, 2012Publication date: December 13, 2012Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji OTSUBO, Yuji OCHI, Masami NAKAI, Atsushi MORI
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Publication number: 20120316167Abstract: The present invention provides new secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. Many of these compounds are active against Candida species such as Candida Albicans and Candida Glabrata.Type: ApplicationFiled: December 28, 2010Publication date: December 13, 2012Applicant: Polichem SAInventors: Stefania Gagliardi, Simone Del Sordo, Federico Mailland, Michela Legora
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Publication number: 20120309758Abstract: 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: ApplicationFiled: June 8, 2012Publication date: December 6, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Urvi Sheth, Lev T.D. Fanning, Mehdi Numa, Hayley Binch, Dennis James Hurley, Jinglan Zhou, Sara S. Hadida Ruah, Anna R. Hazlewood, Alina Silina, Rajendran Vairagoundar, Fredrick F. Van Goor, Peter Diederik Jan Grootenhuis, Martyn C. Botfield
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Publication number: 20120309751Abstract: New tertiary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. These compounds are also active against Candida species such as Candida Albicans and Candida Glabrata.Type: ApplicationFiled: December 28, 2010Publication date: December 6, 2012Applicant: POLICHEM SAInventors: Stefania Gagliardi, Simone Del Sordo, Federico Mailland, Michela Legora
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Publication number: 20120301427Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HW).Type: ApplicationFiled: January 25, 2012Publication date: November 29, 2012Inventors: Gary BRIDGER, Al KALLER, Curtis HARWIG, Renato SKERLJ, David BOGUCKI, Trevor R. WILSON, Jason CRAWFORD, Ernest J. MCEACHERN, Bem ATSMA, Siqiao NAN, Yuanxi ZHOU, Dominique SCHOLS, Christopher D. SMITH, Maria R. DI FLURI
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Patent number: 8314087Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: February 15, 2008Date of Patent: November 20, 2012Assignee: Amgen Inc.Inventors: Brian K. Albrecht, Steven Bellon, Shon Booker, Alan C. Cheng, Derin D'Amico, Noel D'Angelo, Jean-Christophe Harmange, Tae-Seong Kim, Longbin Liu, Mark H. Norman, Aaron C. Siegmund, Markian Stec, Ning Xi, Kevin Yang
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Patent number: 8314232Abstract: The present invention relates to a process of preparing a compound of the following formula III: wherein R1-R4 are as defined herein. The present invention also relates to the preparation of intermediates used to prepare the compound of formula III.Type: GrantFiled: September 25, 2009Date of Patent: November 20, 2012Assignee: GlaxoSmithKline LLCInventors: Nicole Marie Deschamps, Michael Tolar Martin, Michael John Monteith, Xiaoming Zhou
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Publication number: 20120283256Abstract: The present invention relates to compounds having the following Formula (I) for use in the prevention and/or the treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs.Type: ApplicationFiled: December 16, 2010Publication date: November 8, 2012Inventors: Andre Delacourte, Patricia Melnyk, Stephane Burlet, Nicolas Lefur
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Publication number: 20120277231Abstract: The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.Type: ApplicationFiled: October 16, 2010Publication date: November 1, 2012Inventors: Axel Ullrich, Robert Torku, Yixiang Zhang, György Kéri, László Örfi, István Szabadkai
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Publication number: 20120277216Abstract: The present invention relates to novel 1,2-dihydro-2-oxoquinoline compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The compounds of the present invention are useful in the treatment/prevention of various disorders that are mediated by 5-HT4 receptor activity.Type: ApplicationFiled: December 29, 2009Publication date: November 1, 2012Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Ishtiyaque Ahmad, Pradeep Jayarajan, Nagaraj Vishwottam Kandikere, Anil Karbhari Shinde, Rama Sastri Kambhampati, Gopinadh Bhyrapuneni, Jyothsna Ravula, Sriramachandra Murthy Patnala, Venkateswarlu Jasti
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Publication number: 20120277230Abstract: The present invention relates to compound (I) wherein: means a pyridazine, a pyrimidine or a pyrazine group, R independently represent a hydrogen atom, a halogen atom or a group chosen among a CN group, a hydroxyl group, a COOR1 group, a (C1-C3)fluoroalkyl group, a (C1-C3)fluoroalkoxy group, a NO2 group, a NR1R2 group, a (C1-C4)alkoxy group, a phenoxy group and a (C1-C3)alkyl group, said alkyl being optionally mono-substituted by a hydroxyl group, n is 1, 2 or 3, n is 1 or 2, R is a hydrogen atom, a halogen atom or a group chosen among a (C1-C3)alkyl group, a hydroxyl group, a COOR1 group, a NO2 group, a NR1R2 group, a morpholinyl or a morpholino group, a N-methylpiperazinyl group, a (C1-C3)fluoroalkyl group, a (C1-C4)alkoxy group and a CN group, Z is N or C, Y is N or C, X is N or C, W is N or C, T is N or C, U is N or C, for use as an agent for preventing, inhibiting or treating cancer. Some of said compounds are new and also form part of the invention.Type: ApplicationFiled: June 14, 2010Publication date: November 1, 2012Applicants: SOCIETE SPLICOS, UNIVERSITE MONTPELLIER 2, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Pierre Roux, Florence Mahuteau, Romain Najman, Jamal Tazi, Gilles Gadea, Didier Scherrer, Carsten Brock, Nathalie Cahuzac
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Patent number: 8299055Abstract: The present invention relates to a compound represented by the following formula (1): wherein D1, A1, D2, R1, D3, and R2 each have the same meaning as defined in the present specification or a salt thereof. The compound represented by the formula (1) or a salt thereof has an IKK? inhibiting activity and the like and is useful for the prevention and/or treatment of IKK?-associated diseases or symptoms and the like.Type: GrantFiled: October 1, 2009Date of Patent: October 30, 2012Assignee: Asahi Kasei Pharma CorporationInventors: Shunsuke Kaneko, Kenichiro Sato, Daisuke Shikanai, Rintaro Yamada, Katsuhiko Sakurada
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Publication number: 20120270858Abstract: The invention provides isoquinoline, quinoline, and quinazoline derivatives to treat a variety of disorders, diseases and pathologic conditions, and more specifically to the use of isoquinoline, quinoline, and quinazoline derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds to the treatment of hyperproliferative diseases and pathologic angiogenesis.Type: ApplicationFiled: June 9, 2010Publication date: October 25, 2012Applicant: CALIFORNIA CAPITAL EQUITY, LLCInventors: Chunlin Tao, Xiaowen Sun, Hongna Han, Lukasz Koroniak, Neil Desai
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Publication number: 20120270872Abstract: This invention relates to three crystalline forms 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), designated as Form A, Form B, and Form C. 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 form of Compound (I) and a pharmaceutically acceptable excipient.Type: ApplicationFiled: July 16, 2010Publication date: October 25, 2012Applicant: Exelixis, Inc.Inventors: Hilary Cannon, David Igo, Tri Tran
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Patent number: 8293732Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.Type: GrantFiled: December 4, 2007Date of Patent: October 23, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Ismet Dorange, Magali Madeleine Simone Motte, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
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Patent number: 8293897Abstract: The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter—and/or intra—cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: GrantFiled: October 9, 2009Date of Patent: October 23, 2012Assignees: Sunshine Lake Pharma Co., Ltd.Inventor: Ning Xi
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Patent number: 8293729Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.Type: GrantFiled: June 23, 2010Date of Patent: October 23, 2012Assignees: Boehringer Ingelheim International GmbH, Neurocrine Biosciences Inc.Inventors: Brian Dyck, Joe A. Tran, Junko Tamiya, Florence Jovic, Troy Vickers, Chen Chen, Nicole Harriott, Timothy Coon, Neil J. Ashweek
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Publication number: 20120264739Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.Type: ApplicationFiled: December 30, 2010Publication date: October 18, 2012Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
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Publication number: 20120252808Abstract: The present invention is directed to quinoline amide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: December 13, 2010Publication date: October 4, 2012Inventors: Scott D. Kuduk, Kelly-Ann S. Schlegel, Zhi-Qiang Yang
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Patent number: 8273733Abstract: The disclosure relates to tetrahydroisoquinoline sulfonamide compounds of formula I: wherein R1, R2, n and B are as defined in the disclosure, their preparation and their use in therapies for the treatment of central nervous system diseases such as vigilance and sleep disorders, narcolepsy, Alzheimer's disease and other dementias, Parkinson's disease, attention disorders in hyperkinetic children, memory and learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness and travel sickness.Type: GrantFiled: October 8, 2010Date of Patent: September 25, 2012Assignee: SanofiInventors: Juan Antonio Diaz Martin, Maria Dolores Jimenez Bargueno
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Publication number: 20120232265Abstract: 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: ApplicationFiled: November 7, 2011Publication date: September 13, 2012Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20120225874Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.Type: ApplicationFiled: May 17, 2012Publication date: September 6, 2012Applicant: NOVARTIS AGInventors: Masashi KISHIDA, Naoko MATSUURA, Hidetomo IMASE, Yuki IWAKI, Ichiro UMEMURA, Osamu OHMORI, Eiji KAWAHARA
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Publication number: 20120214991Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.Type: ApplicationFiled: October 21, 2009Publication date: August 23, 2012Applicant: Korea Research Institute of Chemical TechnologyInventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
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Publication number: 20120208798Abstract: Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: November 3, 2010Publication date: August 16, 2012Inventors: Emmanuel Hubert Demont, Neil Stuart Garton, Romain Luc Marie Gosmini, Thomas George Christopher Hayhow, Jonathan Seal, David Matthew Wilson, Michael David Woodrow
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Publication number: 20120208814Abstract: Tetrahydroquinoline compounds of formula (I) or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicted.Type: ApplicationFiled: November 3, 2010Publication date: August 16, 2012Inventors: Emmanuel Hubert Demont, Romain Luc Marie Gosmini
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Publication number: 20120202996Abstract: The present invention relates to tetrahydroquinoline derivatives having general formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y—X is C(O)—O, S(O)2-O, NHC(O)—O, NHC(S)—O, OC(O)—O, bond-O, C(O)—NH, S(O)2-NH, NHC(O)—NH, NHC(S)—NH, OC(O)—NH, bond-NH, NH—C(O), O—C(O), NH—S(O)2, or O—S(O)2 or Y—X is a bond; R6 is H, trifluoromethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8,R9-aminocarbonyl(1-4C)alkyl, R8,R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro, hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4CType: ApplicationFiled: October 7, 2011Publication date: August 9, 2012Applicant: N.V. OrganonInventors: Nicole Corine Renée Van Straten, Rudolf Gijsbertus Van Someren, Jurgen Schulz
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Patent number: 8236796Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle oType: GrantFiled: April 2, 2009Date of Patent: August 7, 2012Assignees: Albany Molecular Research, Inc., Bristol-Myers Squibb CompanyInventors: Bruce F. Molino, Shuang Liu, Peter R. Guzzo, James P. Beck