Quinoline Or Isoquinoline (including Hydrogenated) Patents (Class 544/128)
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Publication number: 20110039828Abstract: A novel compound of the formula (I): wherein R1 is alkoxycarbonyl or the like, R2 is alkyl or the like; R3 is hydrogen or the like; R4 is alkylene or the like; R5 is optionally substituted heterocyclic group; R6, R7, R8 and R9 are independently hydrogen; alkyl, alkoxy, or the like; R10 is optionally substituted aromatic ring, or the like; or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP).Type: ApplicationFiled: October 25, 2010Publication date: February 17, 2011Inventors: Hitoshi KUBOTA, Masakatsu Sugahara, Mariko Furukawa, Mayumi Takano, Daisuke Motomura
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Publication number: 20110034439Abstract: To provide an antitumor agent which exhibits excellent c-Met inhibitory effect and mitigates side effects by virtue of selectively affecting to tumor cells in which c-Met is specifically expressed.Type: ApplicationFiled: April 9, 2009Publication date: February 10, 2011Applicant: Taiho Pharmaceutical Co., Ltd.Inventors: Yoshimitsu Suda, Kosuke Egami, Hidenori Fujita
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Patent number: 7879856Abstract: Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: December 21, 2007Date of Patent: February 1, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland
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Patent number: 7868003Abstract: The invention relates to substituted 4-phenyltetrahydroisoquinolines of formula I wherein R1-R8, N, W, X and Z are defined herein. These compounds and pharmaceutical compositions comprising them are useful in the treatment of respiratory disorders, sleep apnea, kidney disorders, high blood pressure, hypertension, disorders of the central nervous system and the like.Type: GrantFiled: July 11, 2007Date of Patent: January 11, 2011Assignee: Sanofi-AventisInventors: Uwe Heinelt, Hans-Jochen Lang, Klaus Wirth, Thomas Licher, Armin Hofmeister
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Publication number: 20100331293Abstract: 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, Sjogren'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 25, 2010Publication date: December 30, 2010Applicant: AMGEN INC.Inventors: Timothy D. Cushing, Paul John Dransfield, Felix Gonzalez Lopez De Turiso, Michael G. Johnson, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
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Substituted tetrahydroisochinolines as MMP inhibitors, related production method and use as medicine
Patent number: 7858619Abstract: The present invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, A, L and n are as defined herein, its pharmaceutical composition, preparation and uses as a MMP inhibitor.Type: GrantFiled: September 27, 2007Date of Patent: December 28, 2010Assignee: sanofi-aventisInventors: Armin Hofmeister, Manfred Schudok, Hans Matter, Kristin Breitschopf, Antonio Ugolini -
Patent number: 7858620Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides a process for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: September 11, 2008Date of Patent: December 28, 2010Assignee: H. Lundbeck A/SInventors: Jan Kehler, Jacob Nielsen, Morten Langgaard
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Publication number: 20100324043Abstract: Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.Type: ApplicationFiled: June 16, 2010Publication date: December 23, 2010Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
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Publication number: 20100324042Abstract: The present invention relates to a heterocyclic compound of the general formula (I) and their use and preparation, methods of making the compounds, compositions containing at least one of said compounds, and methods of treatment using at least one compound.Type: ApplicationFiled: October 19, 2007Publication date: December 23, 2010Applicant: Abbott GmbH & Co. KG.Inventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Kent D. Stewart
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Publication number: 20100317624Abstract: Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: June 7, 2010Publication date: December 16, 2010Inventors: Allison Laura CHOY, Ann EAKIN, Olga QUIROGA, Brian SHERER
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Patent number: 7846930Abstract: Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.Type: GrantFiled: May 13, 2008Date of Patent: December 7, 2010Assignee: Janssen Pharmaceutica NVInventor: John M. Keith
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Publication number: 20100292235Abstract: Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: March 16, 2007Publication date: November 18, 2010Inventors: Michael G. Kelly, John Kincaid, Yunfeng Fang, Jianhua He, Yeyu Cao, Carl Kaub, Sumithra Gowlugari, Zhan Wang
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Patent number: 7833999Abstract: The invention relates to tetrahydroisoquinoline sulfonamide compounds (of formula (1) as defined in the specification), 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: November 15, 2006Date of Patent: November 16, 2010Assignee: sanofi-aventisInventors: Juan Antonio Diaz Martin, Maria Dolores Jimenez Bargueno
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Publication number: 20100267696Abstract: 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: ApplicationFiled: December 11, 2008Publication date: October 21, 2010Applicant: 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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Patent number: 7816352Abstract: The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.Type: GrantFiled: March 10, 2006Date of Patent: October 19, 2010Assignee: The Regents of The University of CaliforniaInventors: Dennis A. Carson, Howard B. Cottam, Sylvie Barchéchath, Mary Patricia Corr
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Publication number: 20100261705Abstract: The present invention provides a carbostyril compound represented by General Formula (1) or a salt thereof, wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; R4 and R5 each represent a hydrogen atom; the bond between the 3 and 4 positions of the carbostyril skeleton is a single bond or a double bond; R1 is a hydrogen atom, etc; R2 is a hydrogen atom, etc; and R3 is a hydrogen atom, etc. The carbostyril compound or salt thereof of the present invention induces the production of TFF, and thus is usable for the treatment and/or prevention of disorders such as alimentary tract diseases, oral diseases, upper respiratory tract diseases, respiratory tract diseases, eye diseases, cancers, and wounds.Type: ApplicationFiled: November 3, 2009Publication date: October 14, 2010Inventors: Takeshi Kuroda, Takahito Yamauchi, Tomoichi Shinohara, Kunio Oshima, Chiharu Kitajima, Hitoshi Nagao, Tae Fukushima, Takahiro Tomoyasu, Hironobu Ishiyama, Ohta Kazuhide, Masaaki Takano, Takumi Sumida
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Publication number: 20100261701Abstract: 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: ApplicationFiled: October 1, 2009Publication date: October 14, 2010Applicant: ASAHI KASEI PHARMA CORPORATIONInventors: Shunsuke Kaneko, Kenichiro Sato, Daisuke Shikanai, Rintaro Yamada, Katsuhiko Sakurada
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Publication number: 20100256113Abstract: As a result of extensive studies on NAD(P)H oxidase inhibitors, the present inventors found that a quinolone derivative having, at the 2-position, an alkyl group substituted with a heteroatom or the like has an excellent NAD(P)H oxidase inhibitory activity, and accomplished the present invention. The compound of the present invention has a reactive oxygen species production inhibitory activity based on the NAD(P)H oxidase inhibitory activity, and therefore can be used as an agent for preventing and/or treating diabetes, impaired glucose tolerance, hyperlipidemia, fatty liver, diabetic complications and the like.Type: ApplicationFiled: September 25, 2008Publication date: October 7, 2010Applicant: Astellas Pharma Inc.Inventors: Kenichi Onda, Kenichiro Imamura, Fumie Sato, Hiroyuki Moritomo, Yasuharu Urano, Yuki Sawada, Naoki Ishibashi, Keita Nakanishi, Kazuhiro Yokoyama, Shigetada Furukawa, Kazuhiro Momose
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Patent number: 7803791Abstract: The present invention is directed to a Gyrase inhibitor-protein conjugate; in particular a Gyrase inhibitor-albumin conjugate. The present invention further provides methods of the treatment of inflammatory conditions and tumors. Methods of making and producing a Gyrase inhibitor-protein conjugate are also disclosed.Type: GrantFiled: January 20, 2006Date of Patent: September 28, 2010Assignee: Albupharm Heidelberg GmbH & Co. KGInventors: Hannsjörg Sinn, Marcel Mülbaier
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Publication number: 20100239496Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.Type: ApplicationFiled: March 23, 2010Publication date: September 23, 2010Applicant: Siemens Medical Solutions USA, Inc.Inventors: Umesh B. Gangadharmath, Hartmuth C. Kolb, Peter J.H. Scott, Joseph C. Walsh, Wei Zhang, Anna Katrin Szardenings, Anjana Sinha, Gang Chen, Eric Wang, Vani P. Mocharia, Chul Yu, Changhui Liu, Daniel Kurt Cashion, Dhanalakshmi Kasi
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Publication number: 20100240644Abstract: The present invention provides a morpholine derivative of the formula [I]; wherein R1 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, a cycloalkyl group or an alkyl group; R2 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, an optionally substituted alkylcarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted heterocyclo-substituted carbonyl group or a cycloalkylcarbonyl group; T is a methylene group or a carbonyl group; R3, R4, R5 and R6 are the same or different and a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group; or pharmaceutically acceptable salts thereof. These compounds are useful as a renin inhibitor.Type: ApplicationFiled: June 16, 2008Publication date: September 23, 2010Inventors: Hidenori Akatsuka, Hiroshi Sugama, Nobumasa Awai, Takayuki Kawaguchi, Yoichi Takahashi, Toru Iijima, Jingkang Shen, Guangxin Xia, Jianshu Xie
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Publication number: 20100234350Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 14, 2009Publication date: September 16, 2010Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire, Hans-Michael Jantzen, David M. Sedlock
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Publication number: 20100234344Abstract: The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims.Type: ApplicationFiled: March 22, 2008Publication date: September 16, 2010Applicant: JERINI AGInventors: Christoph Gibson, Thomas Tradler, Karsten Schinatbaum, Jochen Pfeifer, Elsa Locardi, Dirk Scharn, Mathias Paschke, Ulf Reimer, Uwe Richter, Gerd Hummel, Ulrich Reineke
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Publication number: 20100234372Abstract: The invention relates to substituted 2-mercaptoquinoline-3-carboxamides, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: ApplicationFiled: March 10, 2010Publication date: September 16, 2010Applicant: GRUNENTHAL GMBHInventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder
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Publication number: 20100222346Abstract: The present invention relates to 4-benzylaminoquinolines of the formula (I) or physiologically tolerated salts thereof. The invention relates to pharmaceutical compositions comprising such quinolines, and the use of such quinolines for therapeutic purposes. The quinolines are GIyTI inhibitors.Type: ApplicationFiled: August 22, 2008Publication date: September 2, 2010Inventors: Wilhelm Amberg, Michael Ochse, Wilfried Braje, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
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Publication number: 20100222349Abstract: The present invention relates to compounds of formula (I) and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.Type: ApplicationFiled: October 15, 2008Publication date: September 2, 2010Applicant: Glaxo Group LimitedInventors: Paul Martin Gore, Ashley Paul Hancock, Simon Teanby Hodgson, Michael Joachim Kranz, Panayiotis Alexandrou Procopiou, Sadie Vile
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Publication number: 20100222325Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-III: wherein, variables Q, R, X, X?, Y1, Y2, Y2?, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.Type: ApplicationFiled: February 24, 2010Publication date: September 2, 2010Inventors: Steven Berthel, Fariborz Firooznia, Daniel Fishlock, Jun-Bae Hong, Yan Lou, Matthew Lucas, Timothy D. Owens, Keshab Sarma, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
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Publication number: 20100222347Abstract: Disclosed is a low-molecular-weight compound having an EPO production-promoting activity and/or a hemoglobin expression-enhancing activity. Specifically disclosed is an EPO production promoter and/or a hemoglobin expression enhancer comprising a 1-acyl-4-(phenoxy, benzyloxy or phenylamino)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by the general formula (1); [wherein R1, R2, R2?, R3 and R3? independently represent a hydrogen atom, a C1-6 alkyl group, or the like; R4, R5, R6, R7, R8, R9 and R10 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or the like; A represents N—R11 or an oxygen atom; R11 represents a hydrogen atom, a C1-6 alkyl group, or the like; and n represents an integer of 0 or 1], a salt of the tetrahydroquinoline compound, or a solvate of the tetrahydroquinoline compound or the salt.Type: ApplicationFiled: September 29, 2008Publication date: September 2, 2010Applicant: KOWA COMPANY, LTD.Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
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Publication number: 20100222348Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, Z and n have defined meanings, the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary ammonium salts and the stereochemically isomeric forms thereof, and their use for the treatment of PARP-mediated disorders.Type: ApplicationFiled: October 22, 2008Publication date: September 2, 2010Inventors: Patrick René Angibaud, Laurence Francoise Bernadette Marconnet-Decrane, Jorge Eduardo Vialard, Laurence Anne Mevellec, Christophe Meyer, Pierre-Henri Storck
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Patent number: 7786116Abstract: The present invention is directed to novel 2-amino-quinoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD), mild cognitive impairment, senility and/or dementia. The compounds of the present invention are inhibitors of ?-secretase, also known as ?-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2.Type: GrantFiled: January 29, 2009Date of Patent: August 31, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Ellen Baxter, Christopher J. Creighton, Chih Yung Ho, Yifang Huang, Tianbao Lu, Chi Luo, Allen B. Reitz, Charles H. Reynolds, Tina Morgan Ross, Ellen Sieber-McMaster
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Patent number: 7786115Abstract: The invention concerns a compound of the Formula I wherein m is 0-2 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is halogeno, trifluoromethyl or (1-6C)alkyl; R3 is hydrogen, halogeno or (1-6C)alkyl; and R4 is (3-6C)cycloalkyl;or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: GrantFiled: December 22, 2005Date of Patent: August 31, 2010Assignee: AstraZeneca ABInventors: Ian Alun Nash, Kenneth Mark Page, Paul Allen Bethel
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Publication number: 20100216786Abstract: The present invention relates to the adenosine A3 receptor ligands of the general formula (I), within them favourably to the antagonists, to their salts, solvates, N-oxides and isomers, to the pharmaceutical compositions containing the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the use of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, to the preparation of the compounds of the general formula (I), their salts, solvates, N-oxides and isomers, as well as to the new intermediates of the general formula (II), (VI), (XI), (XII) and (XV), and to the preparation thereof.Type: ApplicationFiled: December 4, 2009Publication date: August 26, 2010Applicant: SANOFI-AVENTISInventors: Edit SUSAN, Kinga BOER, Zoltan KAPUI, Geza TIMARI, Sandor BATORI, Endre MIKUS, Judit VARGANE SZEREDI, Michel FINET, Katalin URBAN-SZABO, Tibor SZABO
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Publication number: 20100210836Abstract: The present invention relates to lymphoid tyrosine phosphatase inhibitors and autoimmunity. More specifically, the invention relates to the identification of lymphoid tyrosine phosphatase inhibitors and the analysis of the structure-activity relationship.Type: ApplicationFiled: February 12, 2010Publication date: August 19, 2010Applicant: University of Southern CaliforniaInventors: Nunzio BOTTINI, Nouri Neamati
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Publication number: 20100210622Abstract: In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: ApplicationFiled: December 17, 2009Publication date: August 19, 2010Inventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Peter Czabotar, Danette A. Dudley, Wayne J. Fairbrother, John A, Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Lisa A. Hasvold, Andrew M. Petros, Andrew J. Souers, Zhi-Fu Tao, Le Wang, Xilu Wang, Kurt Deshayes
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Publication number: 20100197909Abstract: To provide a novel mutilin derivative having a substitution at the 14-position, which is a novel mutilin analogue exhibiting a potent and broad antimicrobial action against Gram-positive bacteria and Gram-negative bacteria including various drug-resistant bacteria, and which is expected to be useful as an agent for treating infectious diseases. A mutilin derivative represented by the following general formula (1): or a pharmaceutically acceptable addition salt thereof.Type: ApplicationFiled: May 23, 2008Publication date: August 5, 2010Inventors: Yasumichi Fukuda, Masanori Takadoi, Yoshikazu Asahina, Taro Sato, Haruaki Kurasaki, Hiroyuki Ebisu, Masaya Takei, Hideyuki Fukuda
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Publication number: 20100197688Abstract: The present invention is directed to compounds of generic formula (I) which are inhibitors of ephrin A4. 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 regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.Type: ApplicationFiled: May 28, 2009Publication date: August 5, 2010Inventors: Philippe G. Nantermet, Hamaka A. Rajapakse, Takeshi Sagara, John M. Sanders, Hong Zhu
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Publication number: 20100190766Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.Type: ApplicationFiled: December 10, 2009Publication date: July 29, 2010Applicant: Achaogen, Inc.Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
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Publication number: 20100190782Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: ApplicationFiled: December 17, 2009Publication date: July 29, 2010Inventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Carl Steven Rye, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Andrew M. Petros, Andrew J. Souers
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Publication number: 20100190745Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: June 3, 2009Publication date: July 29, 2010Applicant: AstraZeneca ABInventors: Allison Laura Choy, Pamela Hill, John Irvin Manchester, Brian Sherer
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Patent number: 7763614Abstract: The present invention relates to compounds of structural formula I: I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: September 22, 2004Date of Patent: July 27, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Isaacs, Christopher J. Dinsmore, B. Wesley Trotter, Nigel Liverton, Douglas C. Beshore, Nathan R. Kett, Charles J. McIntyre, Kausik K. Nanda, David A. Claremon
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Publication number: 20100184763Abstract: This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HW molecule.Type: ApplicationFiled: February 10, 2010Publication date: July 22, 2010Inventors: Jennifer R. Allen, Kaustav Biswas, Roland Burli, Jennifer Dao, Michael J. Frohn, Jennifer E. Golden, Randall W. Hungate, Robert Kurzeja, Stephanie J. Mercede, Kristine M. Muller, Susana C. Neira, Tanya A. N. Peterkin, Christopher M. Tegley, Violeta Yu
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Publication number: 20100184739Abstract: 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: December 11, 2009Publication date: July 22, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Urvi Sheth, Lev T.D. Fanning, Mehdi Michael Djamel Numa, Hayley Binch, Dennis Hurley, Jinglan Zhou, Sara S. Hadida Ruah, Anna Hazlewood, Alina Silina, Rajendran Vairagoundar, Fredrick van Goor, Peter D.J. Grootenhuis, Martyn Botfield
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Publication number: 20100168100Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: ApplicationFiled: May 16, 2008Publication date: July 1, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Nicholas D. Adams, Amita M. Chaudhari
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Publication number: 20100168065Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, n, m and X have defined meanings.Type: ApplicationFiled: March 7, 2008Publication date: July 1, 2010Applicant: Janssen Pharmaceutica NVInventors: Jorge Eduardo Vialard, Patrick René Angibaud, Laurence Anne Mevellec, Christophe Meyer, Eddy Jean Edgard Freyne, Isabelle Noëlle Pilatte, Bruno Roux, Elisabeth Thérèse Jeanne Pasquier, Xavier Marc Bourdrez, Christophe Denis Adelinet, Laurence Francoise Bernadette Marconnet-Decrane, Jacqueline Anne Macritchie, James Edward Stewart Duffy, Andrew Pate Owens, Pierre-Henri Storck, Virginie Sophie Poncelet
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Publication number: 20100168099Abstract: The invention provides new 1H-quinolin-4-one compounds of formula (I), wherein R1, R2, R3, R4 and R5 have different meanings, and pharmaceutically acceptable salts and hydrates thereof. Compounds of formula (I) are useful for treating or preventing diseases associated with GABAA receptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds.Type: ApplicationFiled: August 9, 2007Publication date: July 1, 2010Applicant: FERRER INTERNACIONAL, S.A.Inventors: José Luis Falcö, Albert Palomer, Antonio Guglietta
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Patent number: 7745451Abstract: Fused heterocyclic compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4?, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.Type: GrantFiled: May 4, 2006Date of Patent: June 29, 2010Assignee: Renovis, Inc.Inventors: Michael G. Kelly, John Kincaid, Carl J. Kaub
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Publication number: 20100160312Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A0-3 and R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: February 23, 2010Publication date: June 24, 2010Applicant: AMGEN INC.Inventors: Essa HU, Jason Brooks Human, Roxanne Kunz, Andrew Tasker, Ryan White
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Patent number: 7741322Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: September 17, 2004Date of Patent: June 22, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Charles J. McIntyre, Richard Isaacs, David A. Claremon
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Publication number: 20100152112Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: ApplicationFiled: May 16, 2008Publication date: June 17, 2010Inventors: Nicholas D. Adams, Joelle Lorraine Burgess, Michael Gerard Darcy, Carla A. Donatelli, Steven David Knight
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Publication number: 20100152185Abstract: The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: December 7, 2009Publication date: June 17, 2010Inventors: Lin Chu, Mark T. Goulet, Feroze Ujjainwalla, Linda Chang, Richard Frenette, Yves Girard, Michel Therien, Dwight MacDonald, John H. Hutchinson