Ring Nitrogen In The Polycyclo Ring System Patents (Class 546/198)
-
Patent number: 7846934Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof (I), wherein: R3 is cyclopentyl or cyclohexyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: GrantFiled: January 8, 2009Date of Patent: December 7, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
-
Patent number: 7847101Abstract: Pharmaceutical pyrazolybenzothiazole compositions of formula (1) are provided. The compositions may be pharmaceutically acceptable salts. R1, R2 and R3 at each occurrence are independently selected from amino, aminosulfinyl, aminosulfonyl, aryl, azido, halogen, heteroalkyl, heteroaryl, hydrazinyl, hydrocarbyl, hydrogen, hydroxyl, nitro, nitroso, phosphate, phosphinate, phosphonate, phosphonium, phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfinic acid, sulfonamido, sulfonate, sulfonic acid, sulfonyl, sulfoxido, thiol, thioureido, and ureido, and R4 is selected from hydrogen, heteroalkyl, heteroaryl, and hydrocarbyl.Type: GrantFiled: July 23, 2003Date of Patent: December 7, 2010Assignee: Valocor Therapeutics, Inc.Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov
-
Publication number: 20100305073Abstract: The present invention relates to compounds that have CYP450 inhibiting properties and are therefore useful as boosters of certain drugs, i.e. they are able to increase at least one of the pharmacokinetic variables of certain drugs when co-administered. The invention further provides the use of said compounds as improvers of the bioavailability of certain drugs. Methods for the preparation of the compounds of the invention and pharmaceutical compositions are also provided.Type: ApplicationFiled: December 5, 2008Publication date: December 2, 2010Inventors: Tim Hugo Maria Jonckers, Wim Bert Griet Schepens, Geerwin Yvonne Paul Haché, Beate Sabine Hallenberger, Jennifer Chiyomi Sasaki, Judith Eva Baumeister, Gerben Albert Van 'T Klooster
-
Patent number: 7842808Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: January 5, 2007Date of Patent: November 30, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Ling Chen, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, Guanglin Luo, John E. Macor, Graham S. Poindexter, George O. Tora
-
Publication number: 20100298288Abstract: Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moietyType: ApplicationFiled: June 16, 2008Publication date: November 25, 2010Applicant: MERCK & CO., INCInventors: Julianne A. HUNT, Ramzi F. Sweis, Dooseop Kim, Florida Kallashi, Peter J. Sinclair
-
Publication number: 20100292208Abstract: Compounds with two fused bicyclic heteroaryl moieties and their pharmaceutical compositions, and methods of using them as leukotriene A4 hydrolase (LTA4H) modulators and for the treatment of diseases, disorders and conditions mediated by LTA4H.Type: ApplicationFiled: May 12, 2010Publication date: November 18, 2010Inventors: Genesis Bacani, Christa C. Chrovian, Wendy Eccles, Anne M. Fourie, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, JR., Virginia M. Tanis, John J. M. Wiener
-
Publication number: 20100292211Abstract: The present invention relates to the prediction of antipsychotic treatment efficacy based on a patient's genotype at one or more single nucleotide polymorphism (SNP) loci and to the treatment of a patient based on such prediction.Type: ApplicationFiled: September 10, 2008Publication date: November 18, 2010Inventor: Christian LAVEDAN
-
Publication number: 20100286181Abstract: 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: August 16, 2007Publication date: November 11, 2010Applicant: ASTRAZENECA ABInventors: Gregory Basarab, Pamela Hill, Kenneth Gregory Hull
-
Patent number: 7816376Abstract: The invention relates to compounds of the formula (I) and pharmaceutically usable derivatives, salts, solvates and stereoisomers and mixtures thereof, in which X, Y, Z, R1, R3, R4, R8, p, k, E, G, Z and Q are as defined in claim 1, which are employed as excitatory amino acid antagonists for combating neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's, Parkinson's or Huntington's disease, cerebral ischaemia, infarction or psychoses.Type: GrantFiled: March 5, 2003Date of Patent: October 19, 2010Assignee: Merck Patent GmbHInventors: Oliver Schadt, Joachim Leibrock, Helmut Pruecher, Christoph Seyfried
-
Publication number: 20100261687Abstract: Object of the present invention are novel substituted compounds of the formula 1, wherein A, R1, R2, R3 and R4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 19, 2010Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Marc GRUNDL, Horst DOLLINGER, Riccardo GIOVANNINI, Christoph HOENKE, Matthias HOFFMANN, Jan KRIEGL, Domnic MARTYRES, Georg RAST, Peter SEITHER
-
Publication number: 20100249163Abstract: The present invention relates to piperidinyl-based renin inhibitor compounds having the formula containing amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: November 26, 2008Publication date: September 30, 2010Inventors: Daniel Dube, Erich L. Grimm, Dwight MacDonald, Bruce MacKay
-
Patent number: 7803803Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl, or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; and R8 is C1-8-alkyl or C3-8-cycloalkyl.Type: GrantFiled: January 8, 2009Date of Patent: September 28, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
-
Publication number: 20100239551Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating chan-nel activating proteases, and methods for using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSSI1E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.Type: ApplicationFiled: January 4, 2008Publication date: September 23, 2010Applicant: IRM LLCInventors: David C. Tully, Arnab K. Chatterjee, Agnes Vidal, Badry Bursulaya
-
Publication number: 20100240889Abstract: The present invention provides compounds of formula (I): in which R1, R?1, R2, R?2, R3, Y and G have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.Type: ApplicationFiled: April 24, 2006Publication date: September 23, 2010Applicant: PROSKELIA SASInventors: Pierre DePrez, Hélène Jary, Taoues Temal
-
Patent number: 7799791Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; or R1 and R2 are both H; one of R3 and R4 is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; or R3 and R4 are joined together with the adjacent backbone carbon atom to form a spiro-C5-C6 cycloalkyl group; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl; or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; R8 is C1-8-alkyl or C3-8-cycloalkyl; R9 is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms.Type: GrantFiled: January 8, 2009Date of Patent: September 21, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
-
Publication number: 20100228008Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins and nucleic acids. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that 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 modified by the addition of charged and polar groups to provide beneficial properties.Type: ApplicationFiled: June 17, 2009Publication date: September 9, 2010Applicant: ENZO LIFE SCIENCES, INC. C/O ENZO BIOCHEM, INC.Inventors: Yuejun Xiang, Praveen Pande, Rajesh Khazanchi, Elazar Rabbani, Dakai Liu, Wei Cheng
-
Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
-
Patent number: 7790753Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.Type: GrantFiled: April 17, 2006Date of Patent: September 7, 2010Assignee: sanofi-aventisInventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Corinne Veronique
-
Publication number: 20100222366Abstract: The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.Type: ApplicationFiled: July 23, 2008Publication date: September 2, 2010Inventors: Joseph B. Santella, John Hynes, Daniel S. Gardner
-
Publication number: 20100221764Abstract: The present invention relates to an enzyme substrate for detecting nitroreductase activity of formula (I) below: in which X is S, NX1, O or NX1-CO; R1 is nothing or a substituent selected from Cl, CH3, Br, F, I, alkyl, aryl and carboxyl; R2 is nothing or a substituent selected from Cl, O—CH2—O, O—CH3, F, diethylenediamine-CH3, NR3R4, Br, I, alkyl, aryl, carboxyl, NO2 and R3 and R4 are independently H or an alkyl group containing from 1 to 4 carbon atoms; and X1 is selected from H, CH3, C2H4Ph, OH, alkyl and aryl.Type: ApplicationFiled: May 29, 2008Publication date: September 2, 2010Applicant: BIOMERIEUXInventors: Olivier Fabrega, Arthur James, Vindhya Lakshika Salwatura, Sylvain Orenga, Stephen Stanforth
-
Publication number: 20100216840Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.Type: ApplicationFiled: May 7, 2010Publication date: August 26, 2010Applicant: ACADIA PHARMACEUTICALS INC.Inventors: NICHOLAS MICHAEL KELLY, KRISTIAN NORUP KOCH, BO-RAGNAR TOLF
-
Publication number: 20100216787Abstract: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula.Type: ApplicationFiled: December 22, 2009Publication date: August 26, 2010Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Masakazu Sato, Yuko Matsunaga, Hajime Asanuma, Hideaki Amada, Takeshi Koami, Tetsuo Takayama, Tetsuya Yabuuchi, Fumiyasu Shiozawa, Hironori Katakai, Hiroki Umemiya, Akiko Ikeda
-
Patent number: 7781436Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: GrantFiled: July 25, 2006Date of Patent: August 24, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
-
Patent number: 7781430Abstract: Compounds of formulae I and II: are disclosed as 5-HT3 inhibitors. Those compounds that exhibit central activity are useful in treating CINV; those that inhibit peripheral receptors are useful to treat IBS-D.Type: GrantFiled: November 2, 2007Date of Patent: August 24, 2010Assignee: Albany Molecular Research, Inc.Inventors: David J. Fairfax, Zhicai Yang
-
Patent number: 7781431Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.Type: GrantFiled: September 7, 2004Date of Patent: August 24, 2010Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpAInventors: Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontoria, Michael Rowley
-
Publication number: 20100210688Abstract: The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4, R5, R6, R7, R7a, R7b, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: April 27, 2010Publication date: August 19, 2010Inventors: Roger Bonnert, Alice Flaherty, Garry Pairaudeau, Michael Stocks
-
Publication number: 20100210687Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.Type: ApplicationFiled: September 18, 2008Publication date: August 19, 2010Inventors: David Gwyn Cooper, Ian Thomason Forbes, Vincenzo Garzya, Dale James Johnson, Graeme Irvine Stevenson, Paul Adrian Wyman
-
Publication number: 20100204272Abstract: Compounds of formula (I) or a salt thereof are provided: wherein R4, R5, R6, Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.Type: ApplicationFiled: September 18, 2008Publication date: August 12, 2010Inventors: David Gwyn Cooper, Ian Thomson Forbes, Vincenzo Garzya, Dale James Johnson, Graeme Irvine Stevenson, Paul Adrian Wyman
-
Publication number: 20100204239Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.Type: ApplicationFiled: February 2, 2010Publication date: August 12, 2010Inventors: Zhihua Sui, Xuqing Zhang, Xiaojie Li
-
Patent number: 7772252Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: GrantFiled: April 17, 2009Date of Patent: August 10, 2010Assignee: Aventis Pharmaceuticals Inc.Inventors: James Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M Shutske, Joseph T Strupczewski, Kenneth J Bordeau, John G Jurcak, Thaddeus Nieduzak, Sharon A. Jackson, Paul Angell, James P Carey, George Lee, David Fink, Jean-Francois Sabuco, Yulin Chiang, Nicola Collar
-
Publication number: 20100184794Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like. A glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: October 17, 2007Publication date: July 22, 2010Inventors: Tsuneo Yasuma, Yasufumi Miyamoto
-
Publication number: 20100179150Abstract: 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: February 16, 2006Publication date: July 15, 2010Applicant: ASTRAZENECA ABInventors: Gregory Basarab, Brian Dangel, Paul Robert Fleming, Michael Barry Gravestock, Oluyinka Green, Sheila Irene Hauck, Pamela Hill, Kenneth Gregory Hull, George Mullen, Brian Sherer, Fei Zhou, Haihong Ni
-
Publication number: 20100179189Abstract: Compounds represented by Formula (I) or Formula (II) against cell releasing TNF?, their pharmaceutically acceptable salts or hydrates and preparation methods and uses thereof, in which A and B represent CH2, CO, SO, or SO2; D represents S, NH, or NC1-6 alkyl; R1 represents H, or one or two same or different radical(s) selected from the group consisting of F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), or N(C1-4 alkyl)2.Type: ApplicationFiled: October 16, 2007Publication date: July 15, 2010Inventor: Hesheng Zhang
-
Patent number: 7754732Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: January 5, 2007Date of Patent: July 13, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Gene M. Dubowchik, Xiang Jun J. Jiang, John E. Macor, Graham S. Poindexter, Shikha Vig
-
Publication number: 20100168167Abstract: There is provided compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, m and n have meanings given in the description, and pharmaceutically acceptable derivatives thereof, which compounds are useful in the treatment of diseases and conditions associated with inflammation.Type: ApplicationFiled: March 12, 2008Publication date: July 1, 2010Inventors: Benjamin Pelcman, Christian Krog-Jensen, Yaping Shen, James Gee Kan Yee, Lloyd F. MacKenzie, Yuanlin Zhou, Kang Han, Jeffery R. Raymond
-
Publication number: 20100152240Abstract: Compounds represented by Formula (I) or Formula (II), their pharmaceutically acceptable salts or hydrates wherein A, B and E independently represent CH2 or CO; D represents S, NH, or NC1-6 alkylhydrocarbyl; R represents H or R3; R1 represents H, or 1-2 same or different occurrences of radical(s) selected from the group consisting of F, Cl, Br, C1-4 alkylhydrocarbyl, OH, OC1-4 alkylhydrocarbyl, NO2, NHC(O)C1-4 alkylhydrocarbyl, NH2, NH(C1-4 alkylhydrocarbyl), N(C1-4 alkylhydrocarbyl)2; and R2 represents F, CF3, H or C1-4 alkylhydrocarbyl; are active inhibitors of TNF?. Provided are also preparation methods and uses thereof.Type: ApplicationFiled: October 16, 2007Publication date: June 17, 2010Inventor: Hesheng Zhang
-
Publication number: 20100152200Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of alphaviruses.Type: ApplicationFiled: November 16, 2009Publication date: June 17, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: David J. Miller, Daniel C. Peltier, Weiping Peng
-
Patent number: 7737150Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: GrantFiled: January 8, 2009Date of Patent: June 15, 2010Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
-
Patent number: 7737166Abstract: A 1,6-?-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-?-glucan synthesis inhibition. Also provided is a drug, a salt or hydrate thereof, especially an antifungal that contains the compound.Type: GrantFiled: August 16, 2006Date of Patent: June 15, 2010Assignee: Daiichi Sankyo Company, LimitedInventors: Katsuhiro Kawakami, Kazuo Kanai, Takao Horiuchi, Hiroshi Takeshita, Syozo Kobayashi, Yuichi Sugimoto, Issei Achiwa, Junichi Kuroyanagi
-
Publication number: 20100137245Abstract: Heterocyclyl-substituted thiazoles of the formula (I), in which the symbols have the meanings given in the description, and also to the agrochemically active salts thereof, and their use for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).Type: ApplicationFiled: September 29, 2009Publication date: June 3, 2010Applicant: BAYER CROPSCIENCE AGInventors: Pierre CRISTAU, Nicola Rahn, Stefan Herrmann, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann, Arnd Voerste, Jürgen Benting, Pierre Wasnaire, Sebstian Hoffmann
-
Patent number: 7700641Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: GrantFiled: April 11, 2006Date of Patent: April 20, 2010Assignee: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Nagasree Chakka, Sultan Chowdhury, Robert Fraser, Jianmin Fu, Duanjie Hou, Tom Hsieh, Rajender Kamboj, Shifeng Liu, Vandna Raina, Mehran Seid Bagherzadeh, Jianyu Sun, Shaoyi Sun, Serguei Sviridov
-
Patent number: 7691846Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4-P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: March 10, 2009Date of Patent: April 6, 2010Assignee: Bristol-Myers Squibb CompanyInventor: Donald J. P. Pinto
-
Publication number: 20100076196Abstract: A process for the preparation of crystalline 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxyphenyl]-ethanone (Iloperidone), which comprises the reaction between 3-[1-(3-chloropropyl)-4-piperidinyl]-6-fluoro-1,2-benzisoxazole and 3-methoxy-4-hydroxy-acetophenone.Type: ApplicationFiled: September 8, 2009Publication date: March 25, 2010Inventor: Miklós Vértessy
-
Patent number: 7683184Abstract: The heterocyclic compound of the present invention is represented by general formula (I) and is suitable to forming an optical recording layer in an optical recording medium to which short-wavelength light is applied for recording and playing-back.Type: GrantFiled: August 18, 2005Date of Patent: March 23, 2010Assignee: Adeka CorporationInventors: Satoshi Yanagisawa, Yusuke Kubota
-
Publication number: 20100029687Abstract: [Problem] To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. [Means for Resolution] It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).Type: ApplicationFiled: November 14, 2007Publication date: February 4, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
-
Publication number: 20100022530Abstract: Compounds of the formula (I) in which A1, A2, R1, X1, X2, X3, Y, R2, Cy and n have meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: November 22, 2007Publication date: January 28, 2010Applicant: MERCK PATENT GMBHInventors: Kai Schiemann, Dirk Finsinger, Frank Zenke
-
Publication number: 20100010044Abstract: The present invention relates to a novel crystalline form of 2-[4-(4-fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazol-6-yl)-acetamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described.Type: ApplicationFiled: July 8, 2009Publication date: January 14, 2010Applicant: Forest Laboratories Holdings LimitedInventors: Alphonso HIGUERA, Haijian ZHU, Andreas GRILL
-
Publication number: 20100010009Abstract: The present invention relates to compounds of formula (1), and pharmaceutically acceptable salts thereof, A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof (I), wherein: one of R1 and R2 is H, and the other is selected from F and Cl, or R1 and R2 are both F; R3 is selected from cyclopentyl and cyclohexyl; R4 is an optionally substituted 5- or 6-membered monocyclic or an 8- to 10-membered bicyclic aryl or heteroaryl ring which includes up to four heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: ApplicationFiled: January 8, 2009Publication date: January 14, 2010Inventors: Martin Quibell, John Paul Watts
-
Patent number: 7642274Abstract: The invention aims to provide a drug having an activity on inhibiting a decrease in pain threshold. Since a ?-opioid receptor agonist effectively inhibits the decrease in pain threshold, it is useful as an inhibitor of pain threshold decrease.Type: GrantFiled: July 2, 2004Date of Patent: January 5, 2010Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kyoichi Shimomura, Hiroyuki Aono, Yaeko Tsukahara, Taeko Hata
-
Publication number: 20090325930Abstract: The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; ??(I-1) formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R? represents 1 to 4 independent hydrogen atoms and the like; and R? represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.Type: ApplicationFiled: August 20, 2009Publication date: December 31, 2009Inventors: Shinichi Hamaoka, Noritaka Kitazawa, Kazumasa Nara, Atsushi Sasaki, Atsushi Kamada, Tadashi Okabe