Unsaturated Ring Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/144)
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Publication number: 20110003850Abstract: This invention provides a compound of formula IA where X=0 or S; Y is 0 or S; q=1 or 0; and other substituents are defined herein. Such compounds can affect the opening of, or otherwise modulate, voltage-gated potassium channels. Such compounds useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.Type: ApplicationFiled: February 1, 2010Publication date: January 6, 2011Applicant: Valeant Pharmaceuticals International, Inc.Inventors: Jean-Michel Vernier, Martha Alicia De La Rosa, Huanming Chen, Jim Zhen Wu, Gary Lee Larson, Ian Wayne Cheney
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Publication number: 20100331303Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: ApplicationFiled: August 20, 2010Publication date: December 30, 2010Inventors: Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
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Publication number: 20100311773Abstract: Disclosed are novel anabaseine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.Type: ApplicationFiled: December 30, 2009Publication date: December 9, 2010Applicant: Cornerstone Therapeutic, Inc.Inventors: Gregory J. Habgood, Daniel Elbaum
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Publication number: 20100305092Abstract: The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, X have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: ApplicationFiled: December 17, 2008Publication date: December 2, 2010Applicant: MERCK SERONO SAInventors: Anna Quattropani, Christophe Cleva, Eric Sebille, Matthias Schwarz, Delphine Marin
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Publication number: 20100305067Abstract: Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, or —C(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N? or —CH?Z2 is —N? or —C(R1)?; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2Jalkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic raType: ApplicationFiled: December 12, 2008Publication date: December 2, 2010Applicant: BIOTA EUROPE LTDInventors: David John Haydon, Lloyd George Czaplewski
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Publication number: 20100292242Abstract: Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Shuang Liu, Bruce F. Molino, Kassoum Nacro
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Publication number: 20100286198Abstract: Anti-infective and biofilm-inhibiting activities of aryl isoquinoline-derivatives of the general formulae 1 to 3 are described.Type: ApplicationFiled: September 27, 2007Publication date: November 11, 2010Inventors: Gerhard Bringmann, Tanja Gulder, Ute Hentschel, Frank Meyer, Heidrun Moll, Joachim Morschhäuser, Alicia Ponte-Sucre De Vanegas, Wilma Ziebuhr, August Stich, Reto Brun, Werner E.G. Müller, Virima Mudogo
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Publication number: 20100267945Abstract: A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, where R1 is optionally substituted lower alkyl, Y is —S(O)2—, R2 is hydrogen or optionally substituted lower alkyl, R7 is hydrogen or optionally substituted lower alkyl, X is a group of the formula: where R5 and R6 are each independently hydrogen, a group of the formula: is optionally substituted cycloalkylene, p is 0, and q is 1 or 2, Z is optionally substituted carbocyclyl or optionally substituted heterocyclyl, and provided that a compound wherein Z is fused heterocyclyl consisting of three rings or optionally substituted pyrimidinyl is excluded.Type: ApplicationFiled: June 25, 2010Publication date: October 21, 2010Applicant: Shionogi & Co., Ltd.Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
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Publication number: 20100261728Abstract: Tetrahydroisoquinoline compounds of formula (I), and compositions containing them, for the treatment of acute, inflammatory and neurophatic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, 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, inflammatory pain and associated hyperalgesia and allodynia, neurophatic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceratType: ApplicationFiled: December 4, 2008Publication date: October 14, 2010Applicant: Amgen Inc.Inventors: Mark H. Norman, Yunxin Y. Bo, Vijay K. Gore, Daniel Horne, Matthew Kaller, Vu Van Ma, Holger Monenschein, Thomas Nguyen, Nobuko Nishimura, Nuria Tamayo
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Publication number: 20100256165Abstract: A large conductance calcium-activated K channel opener comprising as an active ingredient a nitrogen-containing 5-membered heterocyclic compound represented by the following formula (I): wherein X represents N—R4, O or S, R1 and R2 each independently represent hydrogen, halogen, carboxyl, amino, lower alkyl, lower alkoxycarbonyl, lower alkenyl, cyclo-lower alkyl, carbamoyl, aryl, heterocyclic or heterocyclic-substituted carbonyl group, R3 represents aryl, heterocyclic or lower alkyl group, and R4 represents hydrogen or lower alkyl group, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 7, 2010Publication date: October 7, 2010Inventors: Mitsuya Hongu, Toshihiro Hosaka, Toshihiko Kashiwagi, Rikako Kono, Hiroyuki Kobayashi
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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: 20100187978Abstract: The present invention relates to a material for an organic electro-optical device and an organic electro-optical device including the same. More particularly, the present invention relates to a material having thermal stability of a glass transition temperature of 120° C. or more and a thermal decomposition temperature of 450° C. or more, and being capable of providing an organic electro-optical device having high efficiency and a long life-span due to less crystallization and improved amorphous properties in a material for an organic electro-optical device. The material for an organic electro-optical device can be used singularly or as a host material in combination with a dopant, and includes an asymmetric fluorene derivative compound. An organic electro-optical device including the material for an organic electro-optical device is also provided.Type: ApplicationFiled: May 28, 2008Publication date: July 29, 2010Applicant: CHEIL INDUSTRIES INC.Inventors: Eun Sun Yu, Nam Soo Kim, Young Hoon Kim, Mi Young Chae
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Publication number: 20100152234Abstract: The invention relates to substituted tetrahydroisoquinolinyl-4-oxobutyric acid amides, methods for the preparation thereof, medicinal products containing these compounds and the use of these compounds for the preparation of medicinal products.Type: ApplicationFiled: December 11, 2009Publication date: June 17, 2010Applicant: GRUNENTHAL GMBHInventors: Sven Kühnert, Gregor Bahrenberg, Beatrix Merla, Klaus Schiene, Wolfgang Schröder
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Publication number: 20100152450Abstract: The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand.Type: ApplicationFiled: October 13, 2009Publication date: June 17, 2010Applicants: PSYCHOGENICS, INC., The Board of Trustees of the University of IllinoisInventors: Jayaraman Chandrasekhar, Alan P. Kozikowski, Jianhua Liu, Werner Tueckmantel, Joel R. Walker, Po-wai Yuen
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Publication number: 20100130545Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
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Patent number: 7718671Abstract: Substituted arylthiourea compounds of Formula I, and the pharmaceutically acceptable salts of such compounds, useful as antiviral agents, are provided herein. Certain substituted arylthioureas disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions containing one or more substituted arylthiourea compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Such pharmaceutical compositions may contain a substituted arylthiourea as the only active agent or may contain a combination of a substituted arylthiourea derivative and one or more other pharmaceutically active agents. Methods of treating Hepatitis C viral infections in mammals are also provided herein.Type: GrantFiled: July 8, 2004Date of Patent: May 18, 2010Assignee: Achillion Pharmaceuticals, Inc.Inventors: Avinash Phadke, Jesse Quinn, Junko Ohkanda, Andrew Thurkauf, Yiping Shen, Cuixian Liu, Dawei Chen, Shouming Li, Xiangzhu Wang
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Publication number: 20100121062Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T ??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.Type: ApplicationFiled: September 25, 2009Publication date: May 13, 2010Applicant: The Board of Trustees of the University of IllinoisInventors: Martin D. Burke, David M. Knapp, Eric P. Gillis
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Patent number: 7700620Abstract: The present invention provides novel C-linked cyclic compounds and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.Type: GrantFiled: June 26, 2006Date of Patent: April 20, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James C. Sutton, Jennifer X. Qiao, Carl Thibeault, Rejean Ruel
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Patent number: 7683066Abstract: The present invention relates to compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: May 15, 2006Date of Patent: March 23, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Andreas Termin, Dean Wilson, Pramod Joshi
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Publication number: 20100022583Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.Type: ApplicationFiled: June 5, 2009Publication date: January 28, 2010Inventor: Tianbao Lu
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Publication number: 20090306390Abstract: A novel class of chiral ligands represented by a structure of Formula (I): wherein R1, R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy, C(O)R6, C(O)NHR6, Si(R6)3, benzyl and aryl; X is selected from the group consisting of OH, OR7, O-Prot and P(R7)2 where Prot represents a protecting group; and R6 and R7 are selected from the group consisting of hydrogen, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy, phenyl, and aryl is disclosed herein.Type: ApplicationFiled: March 2, 2007Publication date: December 10, 2009Applicant: Chao-Jun LiInventors: Chao-Jun Li, Patricia MacLeod, Zhiping Li, Jianqing Feng
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Publication number: 20090288707Abstract: The present invention relates to novel compounds for electronic material, and organic electroluminescent devices or organic solar cells comprising the same. Specifically, the compounds for electronic material according to the invention are characterized in that they are represented by Chemical Formula (1): Since the compounds for electronic material, when being applied to an organic electroluminescent device, show good luminous efficiency and excellent life property of material, OLED's having very good operation life can be manufactured therefrom.Type: ApplicationFiled: April 17, 2009Publication date: November 26, 2009Applicant: Gracel Display Inc.Inventors: Mi Ae Lee, Young Jun Cho, Hyuck Joo Kwon, Bong Ok Kim, Sung Min Kim, Seung Soo Yoon
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Patent number: 7612090Abstract: Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being aryl or heteroaryl Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine or dopamine.Type: GrantFiled: April 29, 2003Date of Patent: November 3, 2009Assignee: Albany Molecular Research, Inc.Inventors: James P. Beck, Matt A. Curry, Mark A. Smith
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Publication number: 20090253906Abstract: 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: April 2, 2009Publication date: October 8, 2009Applicant: AMR TECHNOLOGY, INC.Inventors: Bruce F. MOLINO, Shuang LIU, Peter R. GUZZO, James P. BECK
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Publication number: 20090239841Abstract: Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.Type: ApplicationFiled: October 24, 2005Publication date: September 24, 2009Inventors: Alan J. Hutchison, Jun Yuan
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Publication number: 20090197862Abstract: 2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.Type: ApplicationFiled: February 4, 2009Publication date: August 6, 2009Inventors: Arno G. Steinig, Mark J. Mulvihill, Jing Wang, Douglas S. Werner, Qinghua Weng, Julie Kan, Heather Coate, Xin Chen
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Publication number: 20090176822Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.Type: ApplicationFiled: April 17, 2008Publication date: July 9, 2009Applicant: Genentech, Inc.Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare
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Publication number: 20090166670Abstract: Provided are an anthracene-based compound represented by Formula 1 or 2 and an organic light emitting device employing the same: where R is a hydrogen atom, a halogen atom, a cyano group, a hydroxyl group, a substituted or unsubstituted C1-C20 alkyl group, a substituted or unsubstituted C3-C20 cycloalkyl group, a substituted or unsubstituted C5-C30 heterocycloalkyl group, a substituted or unsubstituted C1-C20 alkoxy group, a substituted or unsubstituted C6-C30 aryl group, a substituted or unsubstituted C6-C30 aralkyl group or a substituted or unsubstituted C2-C30 heteroaryl group, L is a bivalent linking group and a substituted or unsubstituted C6-C30 arylene group or a substituted or unsubstituted C2-C30 heteroarylene group, and m is an integer of 0 to 3.Type: ApplicationFiled: December 19, 2008Publication date: July 2, 2009Inventors: Sang-hoon Park, O-hyun Kwon, Seung-gak Yang, Yu-jin Kim, Yu-ri Choi, Kwan-hee Lee
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Patent number: 7550481Abstract: The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: December 15, 2004Date of Patent: June 23, 2009Assignee: Merck & Co., Inc.Inventors: James C. Barrow, Craig A. Coburn, Philippe G. Nantermet, Harold G. Selnick, Shawn J. Stachel, Matthew G. Stanton, Shaun R. Stauffer, Linghang Zhuang, Jennifer R. Davis
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Publication number: 20090108746Abstract: Provided are an anthracene-based compound represented by Formula 1 or 2 and an organic light emitting device employing the same: where R is a hydrogen atom, a halogen atom, a cyano group, a hydroxyl group, a substituted or unsubstituted C1-C20 alkyl group, a substituted or unsubstituted C3-C20 cycloalkyl group, a substituted or unsubstituted C5-C30 heterocycloalkyl group, a substituted or unsubstituted C1-C20 alkoxy group, a substituted or unsubstituted C6-C30 aryl group, a substituted or unsubstituted C6-C30 aralkyl group or a substituted or unsubstituted C2-C30 heteroaryl group, L is a bivalent linking group and a substituted or unsubstituted C6-C30 arylene group or a substituted or unsubstituted C2-C30 heteroarylene group, and m is an integer of 0 to 3.Type: ApplicationFiled: September 29, 2008Publication date: April 30, 2009Inventors: Sang-hoon Park, O-hyun Kwon, Seung-gak Yang, Yu-jin Kim, Yu-ri Choi
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Publication number: 20090105474Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.Type: ApplicationFiled: March 14, 2006Publication date: April 23, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Yoichi Taniguchi, Eiji Hara, Hitoshi Akitsu, Hidehiko Tanaka, Shuzo Anzai
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Publication number: 20090099133Abstract: Compounds of the formula (I) were synthesized. They were found to down-regulate or inhibit the expression or function of the IGF-1 receptor.Type: ApplicationFiled: September 8, 2006Publication date: April 16, 2009Inventors: Jan Gunzinger, Kurt Leander
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Publication number: 20090079331Abstract: There are provided a compound represented by the general formula (1) and an organic light-emitting device which comprises the compound and has an optical output with remarkably high efficiency and high luminance.Type: ApplicationFiled: December 8, 2006Publication date: March 26, 2009Applicant: CANON KABUSHIKI KAISHAInventors: Satoshi Igawa, Shinjiro Okada, Takao Takiguchi, Keiji Okinaka, Naoki Yamada, Masashi Hashimoto
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Publication number: 20090074791Abstract: The present invention relates to substituted phenylisoquinoline and phenylquinazoline derivatives and to their pharmaceutical uses in preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.Type: ApplicationFiled: September 2, 2008Publication date: March 19, 2009Inventor: Rene Beerli
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Publication number: 20090054650Abstract: The present invention relates to a new method of cross-coupling aryl moieties comprising reacting an arylhalide with an arylboronic acid in the presence of a palladium compound and a compound comprising a di-alkylphosphine moiety.Type: ApplicationFiled: October 3, 2008Publication date: February 26, 2009Inventor: Alex Sergey IONKIN
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Publication number: 20090048443Abstract: 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: October 16, 2008Publication date: February 19, 2009Applicant: AMR TECHNOLOGY, INC.Inventors: Bruce F. MOLINO, Shuang LIU, Peter R. GUZZO, James P. BECK
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Publication number: 20090029987Abstract: The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.Type: ApplicationFiled: July 28, 2006Publication date: January 29, 2009Applicant: RESVERLOGIX CORP.Inventors: Norman C.W. Wong, Henrik C. Hansen, Fabrizio S. Chiacchia, Jan O. Johansson
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Publication number: 20080318952Abstract: 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: ApplicationFiled: May 13, 2008Publication date: December 25, 2008Inventor: John M. Keith
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Publication number: 20080318979Abstract: This invention provides potassium channel modulators which are compounds of formula I where at least one of W and Z is N; where the moiety is one of Groups A or B below A where Ar is a 1,2-fused, six membered ring aromatic group, bearing substituents R1 and R2 as defined below, and containing zero or one ring nitrogen atom; and where other substituents are defined herein. The invention also provides a composition comprising a pharmaceutically acceptable carrier and at least one of the following: i) a pharmaceutically effective amount of a compound of formula I and ii) a pharmaceutically acceptable salt, ester, or prodrug thereof. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt, ester, or prodrug thereof.Type: ApplicationFiled: June 12, 2008Publication date: December 25, 2008Applicant: VALEANT PHARMACEUTICALS INTERNATIONALInventors: Jean-Michel VERNIER, Samedy OUK, Martha A. DE LA ROSA
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Publication number: 20080275242Abstract: The invention provides compounds which exert excellent fungicidal activities against various plant diseases and are useful as active ingredients of pesticides permitting the control of rice blast and so on even in low dosages. Compounds represented by the general formulae (1a) to (1d) or salts thereof: (1a) (1b) (1c) (or) (1d) wherein R1 and R2 are each C1-6 alkyl or the like; R3 and R4 are each hydrogen, halogeno, or the like; R5 is hydrogen, C1-6 alkyl, or the like; X is halogeno, C1-6 alkyl, or the like; Y is halogeno, C1-6 alkyl, or the like; n is an integer of 0 to 4; and m is an integer of 0 to 6.Type: ApplicationFiled: January 21, 2005Publication date: November 6, 2008Inventors: Hiroyuki Ito, Kota Fujiwara, Munetsugu Morimoto, Harukazu Tanaka, Yasushi Tamagawa, Hiroyuki Komai
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Patent number: 7439363Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): R2 is selected from the group consisting of —C1-8alkyl-Z, —C2-8alkenyl-Z and —C2-8alkynyl-Z; wherein the —C1-8alkyl-Z, —C2-8alkenyl-Z and —C2-8alkynyl-Z and Z is a 5 to 6 member aromatic monocyclic heteroaryl ring having from 2 to 4 heteroatoms. These compounds are useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.Type: GrantFiled: June 1, 2004Date of Patent: October 21, 2008Assignee: Janssen Parmaceutica N.V.Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, Hong Ye
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Publication number: 20080234266Abstract: Compounds of the formula (I), in which R, X, X? and R2, R2?, R2?, R3?, R2?? and R7 have the meanings indicated in claim 1, are inhibitors of CHK1 CHK2 and SGK kinases and can be employed, inter alia, for the treatment of cancer.Type: ApplicationFiled: June 30, 2006Publication date: September 25, 2008Inventors: Werner Mederski, Ulrich Emde, Gerhard Barnickel, Frank Zenke, Hartmut Greiner, Frank Stieber
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Publication number: 20080221094Abstract: The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-13 inhibiting compounds with a squaramide moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13 inhibitors.Type: ApplicationFiled: March 7, 2008Publication date: September 11, 2008Inventors: Harald Bluhm, Christian Gege, Matthias Hochgurtel, Arthur Taveras
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Patent number: 7423049Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: May 8, 2006Date of Patent: September 9, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
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Publication number: 20080207607Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: ApplicationFiled: November 20, 2007Publication date: August 28, 2008Inventors: Christian Gege, Carine Chevrier, Matthias Schneider, Harald Bluhm, Matthias Hochgurtel, Hongbo Deng, Brian M. Gallagher, Irving Sucholeiki, Arthur Taveras
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Publication number: 20080194621Abstract: The present invention relates to substituted 4-phenyltetrahydroisoquinoline compounds and pharmaceutical compositions comprising them which are excellent inhibitors of the sodium-hydrogen exchanger (NHE), in particular of the sodium-hydrogen exchanger of subtype 3 (NHE-3). As such these compounds are useful in the treatment of various disorders of the renal and respiratory systems such as acute or chronic renal failure, pulmonary complications, biliary function disorders, respiratory disorders such as snoring or sleep apneas and cardiovascular/central nervous system disorders such as stroke. More specifically, the present invention relates to substituted 4-phenyl-tetrahydroisoquinolines defined by the formula I in which R1-R8 are defined herein.Type: ApplicationFiled: March 12, 2008Publication date: August 14, 2008Applicant: SANOFI-AVENTISInventor: Hans-Jochen Lang
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Publication number: 20080161345Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.Type: ApplicationFiled: May 12, 2005Publication date: July 3, 2008Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
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Publication number: 20080161346Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as VEGF 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: ApplicationFiled: December 19, 2007Publication date: July 3, 2008Applicant: Amgen Inc.Inventors: Yuan Cheng, Deborah Choquette, Jean-Christophe Harmange, Andrew Tasker
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Publication number: 20080139610Abstract: This invention provides a compound of formula IA where X?O or S; Y is O or S; q=1 or 0; and other substituents are defined herein. Such compounds can affect the opening of, or otherwise modulate, voltage-gated potassium channels. They are potentially useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.Type: ApplicationFiled: August 22, 2007Publication date: June 12, 2008Applicant: Valeant Pharmaceuticals North AmericaInventors: Jean-Michel Vernier, Martha Alicia De La Rosa, Huanming Chen, Jim Zhen Wu, Gary Lee Larson, Ian Wayne Cheney
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Publication number: 20080125416Abstract: The invention relates to compounds of 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: August 29, 2005Publication date: May 29, 2008Inventors: Christian Laggner, Maria Rosa Cuberes-Altisent, Joerg Holenz, Juana Maria Berrocal-Romero, Maria Montserrat Contijoch-Llobet