Polycyclo Ring System Having One Of The Two Rings Which Form The Spiro As One Of The Cyclos Patents (Class 546/17)
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Publication number: 20110124671Abstract: The present invention relates to a compound of the following formula: or a pharmaceutically acceptable salt thereof; where R1-R5, Y, m, n, and p are defined herein. Compounds and compositions of the present invention are useful the treatment of atherosclerosis.Type: ApplicationFiled: August 14, 2008Publication date: May 26, 2011Inventors: Brian W. Budzik, Michael Jonathan Bury, Minghua Gu, Ronggang Liu, Feng Ren, Clark A. Sehon, Gren Z. Wang, Jing Zhang
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Publication number: 20110124613Abstract: The present invention provides a pharmaceutical product comprising, in combination of, (a) a (therapeutically effective) dose of a first active ingredient, which is a compound of formula (I) or a pharmaceutically acceptable salt thereof; and (b) a (therapeutically effective) dose of a second active ingredient, which is a glucocorticoid receptor agonist; and optionally, (c) a (therapeutically effective) dose of a third active ingredient, which is a ?2-agonist. The invention further relates to pharmaceutical compositions comprising said combination and to methods of treating treatment of airway diseases, especially chronic obstructive pulmonary disease (COPD) and asthma in mammals by administrating said combination. The invention further relates to a kit comprising the combination and use of said kit in treatment of airway diseases such as COPD and asthma.Type: ApplicationFiled: February 21, 2008Publication date: May 26, 2011Inventors: Tomas Eriksson, Johan Hansson, Marguerite Mensonides-Harsema, John Mo
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Publication number: 20110118251Abstract: An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described.Type: ApplicationFiled: November 10, 2010Publication date: May 19, 2011Applicant: ELI LILLY AND COMPANYInventors: Ana Belen BENITO COLLADO, Nuria DIAZ BUEZO, Alma Maria JIMENEZ-AGUADO, Celia LAFUENTE BLANCO, Maria Angeles MARTINEZ-GRAU, Concepcion PEDREGAL-TERCERO, Miguel Angel TOLEDO ESCRIBANO
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Publication number: 20110111046Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: ApplicationFiled: November 8, 2010Publication date: May 12, 2011Inventors: SCOTT WILLIAM BAGLEY, DAVID ANDREW GRIFFITH, DANIEL WEI-SHUNG KUNG
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Publication number: 20110092529Abstract: The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).Type: ApplicationFiled: January 6, 2006Publication date: April 21, 2011Inventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
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Publication number: 20110092531Abstract: A compound of the formula: or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition, and a method for treating diabetes.Type: ApplicationFiled: October 11, 2010Publication date: April 21, 2011Applicant: ELI LILLY AND COMPANYInventors: Chafiq Hamdouchi, Jayana Pankaj Lineswala, Pranab Maiti
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Publication number: 20110071131Abstract: The present invention provides compounds of Formula (I): their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceuticals compositions thereof.Type: ApplicationFiled: July 29, 2010Publication date: March 24, 2011Applicants: CEPHALON, INC., PHARMACOPEIA, INC.Inventors: Edward R. Bacon, Nadine C. Becknell, Reddeppa reddy Dandu, Lisa Guise-Zawacki, Tao Guo, Chia-yu Huang, Robert L. Hudkins, Babu G. Sundar, Ming Tao, Minglang Wu, Allison L. Zulli
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Publication number: 20110053936Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 3, 2009Publication date: March 3, 2011Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernat Vidal Juan, Nuria Aguilar Izquierdo
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Patent number: 7897765Abstract: Compounds of formula (I) are described herein The compounds can be used, for example, to modulate growth hormone secretagogue receptor (GHS-R). In some instances, the compounds can be used to treat obesity.Type: GrantFiled: February 9, 2009Date of Patent: March 1, 2011Assignee: Elixir Pharmaceuticals, Inc.Inventors: Peter Distefano, Andrew Napper, Rory Curtis, Jay Luly, Manuel A. Navia, Russell J. Thomas, Jean-Francois Pons, Jeffrey O. Saunders
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Publication number: 20110039840Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C?R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.Type: ApplicationFiled: April 14, 2009Publication date: February 17, 2011Applicant: DAC S.R.L.Inventors: Mario Varasi, Florian Thaler, Agnese Abate, Giacomo Carenzi, Ciro Mercurio, Saverio Minucci
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Publication number: 20110034499Abstract: The present invention relates to a compound of the following formula: where R1-R6, R10, Y, n, m, p, and q are as defined herein. Compounds and compositions of the present invention are useful for the treatment of diseases associated with the overexpression of CCR2.Type: ApplicationFiled: June 20, 2008Publication date: February 10, 2011Inventors: Brian W. Budzik, Hilary Schenck Eidam, Ryan Michael Fox, Krista B. Goodman, Dimitar B. Gotchev, Pamela A. Haile, Terry Vincent Hughes, Ronggang Liu, Nathan A. Miller, Tamara Ann Miskowski, Clark A. Sehon, Andrew Q. Viet, Gren Z. Wang, Jing Zhang
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Publication number: 20110034455Abstract: This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.Type: ApplicationFiled: August 24, 2007Publication date: February 10, 2011Inventors: David A. Claremon, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Salvacion Cacatian, Wei He, Robert Simpson, Zhenrong Xu, Wei Zhao
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Patent number: 7884099Abstract: The compounds include substituted rifamycin derivatives in which a quinolone carboxylic acid pharmacophore is covalently bonded to a benzoxazinorifamycin or a spiropiperidinorifamycin. The rifamycin derivatives are useful as antimicrobial agents and are effective against a number of human and veterinary Gram positive and Gram negative pathogens. The advantage of the inventive compounds is that both the rifamycin and quinolone antibacterial pharmacophores are co-delivered with matched pharmacokinetics to the targeted pathogens of interests. Delivery of multiple antibacterial pharmacophores simultaneously to the targeted pathogens has the maximum chance of achieving synergy and minimizing the development of resistance to the antibiotics given.Type: GrantFiled: November 12, 2008Date of Patent: February 8, 2011Assignee: Cumbre IP Ventures, L.P.Inventors: Charles Z. Ding, Yafei Jin, Keith Combrink, In Ho Kim
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Publication number: 20110028390Abstract: The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of acetyl-CoA carboxylase enzyme(s) in an animal.Type: ApplicationFiled: May 18, 2009Publication date: February 3, 2011Applicant: PFIZER, INC.Inventors: Jeffrey W. Corbett, Richard Elliott, Kevin Freeman-Cook, David A. Griffith, Dennis P. Phillion
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Publication number: 20110021549Abstract: The present invention relates to substituted benzofused derivatives, which can he used as vanilloid receptor ligands, method of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.Type: ApplicationFiled: July 21, 2010Publication date: January 27, 2011Applicant: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant Atmaram GHARAT, Uday Mukund JOSHI, Neelima KHAIRATKAR JOSHI
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Publication number: 20110015198Abstract: [Problem] To provide a melanin-concentrating hormone receptor antagonist useful as a pharmaceutical agent for central diseases, circulatory diseases, and metabolic diseases. [Means for Resolution] Provided is a diarylmethylamide derivative represented by formula (I): Wherein R1a, R1b, R2a, R2b, R3a, and R3b independently represent a hydrogen atom or the like, R4 represents a hydrogen atom, C1-6 alkyl, or the like, R5 represents a hydrogen atom or the like, Z represents C1-6 alkyl or the like, or R4 and Z together form a 4- to 6-membered nitrogen-containing hetero ring, Y1 represents H or the like, Y2 represents H, or Y1 and Y2 together form —O—CH2—, W represents C, SO, or the like, Ar1 represents 6-membered aryl or the like, Ar2 represents 6-membered aryl or the like, and ring A represents a benzene ring, a pyridine ring, or the like.Type: ApplicationFiled: March 26, 2009Publication date: January 20, 2011Inventors: Kaori Kamijo, Minoru Moriya, Takao Suzuki, Akihiro Takezawa
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Publication number: 20110009443Abstract: The invention provides compounds of Formula (1) or a pharmaceutically acceptable salt of said compound, wherein R1, R2, and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating mammals suffering from the condition of being overweight.Type: ApplicationFiled: May 18, 2009Publication date: January 13, 2011Inventors: Kevin Daniel Freeman-Cook, Brian Matthew Samas
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Publication number: 20110009399Abstract: The application relates to trisubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R1, R2?, X, U, W, m and n have the meanings explained in the description, a process for their preparation and the use of these compounds as medicines, especially as renin inhibitors.Type: ApplicationFiled: December 12, 2008Publication date: January 13, 2011Inventors: Peter Herold, Stjepan Jelakovic, Robert Mah, Dirk Behnke, Stefan Stutz, Vincenzo Tschinke, Nathalie Jotterand
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Publication number: 20100329978Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.Type: ApplicationFiled: May 21, 2010Publication date: December 30, 2010Applicants: University of Mississippi, I'Universite catholique de LouvainInventors: Christopher R. McCurdy, Christophe Mesangeau, Rae Reiko Matsumoto, Jacques Henri Poupaert, Bonnie Ann Avery, Ahmed Hassan Amin Abdelazeem
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Patent number: 7858635Abstract: The present invention relates to spiro compounds of formula XX as modulators of muscarinic receptors, wherein R1, R2, R3, Z1, Z2, L, G, n, m, t and p are defined herein. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: December 22, 2006Date of Patent: December 28, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis J. Hurley, Ioana Drutu, Gabriel Raffai, Daniele M. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
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Publication number: 20100324024Abstract: The present invention is directed to compounds of formula (I) (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: February 3, 2009Publication date: December 23, 2010Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
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Patent number: 7855293Abstract: The invention concerns sterically shielded, stabilized fluorescent dyes based on symmetrical or unsymmetrical 3-spirocyanines and their utilization as marker-molecules in analytical procedures. The fluorescent dyes according to the invention are characterized by a strongly reduced proneness towards aggregation due to the insertion of bulky spiro-substituents and thus enable to reach a high degree of coupling to the target molecule without a significant loss of fluorescence due to self quenching effects. They therefor exhibit a high quantum yield and are thus excellently suitable as fluorescent dyes, especially as NIR-fluorescent dyes, for the coupling or binding to biological and non-biological target molecules used in analytical methods. The analytical methods comprise all methods in which fluorescence-optical methods are used to detect biological and non-biological molecules.Type: GrantFiled: September 3, 2001Date of Patent: December 21, 2010Inventors: Lutz Haalck, Erk Gedig, Hans-Juergen Hoelpert, Viola Podsadlowski
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Patent number: 7855294Abstract: Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for diseases associated with a nociceptin receptor, for example, as a reliever against tolerance to a narcotic analgesic; a reliever against dependence on or addiction to a narcotic analgesic; an analgesic enhancer; an antiobesitic or appetite suppressor; a treating or prophylactic agent for cognitive impairment and dementia/amnesia; an agent for treating developmental cognitive abnormality; a remedy for schizophrenia; an agent for treating neurodegenerative diseases; an anti-depressant or treating agent for affective disorder; a treating or prophylactic agent for diabetes insipidus; a treating or prophylactic agent for polyuria; or a remedy for hypotension.Type: GrantFiled: March 4, 2005Date of Patent: December 21, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hirobumi Takahashi, Yuichi Sugimoto, Takashi Yoshizumi, Tetsuya Kato, Masanori Asai, Hiroshi Miyazoe
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Publication number: 20100317679Abstract: Substituted Aryl-fused Spirocyclic Amines of the formula (I): are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).Type: ApplicationFiled: September 19, 2008Publication date: December 16, 2010Applicant: LIGAND PHARMACEUTICALS, INC.Inventors: Yuelian Xu, Linghong Xie
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Publication number: 20100311734Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.Type: ApplicationFiled: July 24, 2008Publication date: December 9, 2010Inventors: Maurizio Botta, Emiliano Castiglioni, Romano Di Fabio, Raffaella Spinosa, Andrea Togninelli
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Publication number: 20100311746Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: ApplicationFiled: June 4, 2010Publication date: December 9, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis J. Hurley, Ioana Drutu, Gabriel Raffai, Daniele M. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
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Publication number: 20100298368Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds that modulate the PGD2 activated chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2). Also described herein are methods of using such CRTH2 modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2 mediated conditions or diseases.Type: ApplicationFiled: October 31, 2008Publication date: November 25, 2010Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: Brian Andrew Stearns, John Howard Hutchinson
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Patent number: 7834000Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.Type: GrantFiled: June 13, 2007Date of Patent: November 16, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Corey Gutierrez, Andreas Termin, Sara Hadida-Ruah, Pramod Joshi, Daniele Bergeron, Sanghee Yoo, Hayley Binch, Jon Come, Jingrong Cao, Suganthi Nanthakumar
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Patent number: 7834008Abstract: The present invention relates to cyclopropyl derivatives of formula (I) and salt thereof. These compounds are NK3 receptor antagonists and may therefore be useful for treatment of diseases where the NK3 receptor is implicated, e.g. psychotic disorders.Type: GrantFiled: August 13, 2004Date of Patent: November 16, 2010Assignee: H. Lundbeck A/SInventors: Jan Kehler, Tore Hansen, Anders Poulsen, Berith Bjørnholm, Thomas Ruhland, Morten Bang Nørgaard, Søren Møller Nielsen
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Publication number: 20100280049Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds that antagonize the PGD2 activated chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2). Also described herein are methods of using such CRTH2 antagonists, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2 mediated conditions or diseases.Type: ApplicationFiled: October 31, 2008Publication date: November 4, 2010Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: Brian Andrew Stearns, Yen Pham Truong, John Howard Hutchinson
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Publication number: 20100280009Abstract: The present invention is directed to 3,4-substituted pyrrolidine compounds of formula (I) 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: ApplicationFiled: December 10, 2008Publication date: November 4, 2010Inventors: Shawn J. Stachel, Thomas Steele, Alessia Petrocchi
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Patent number: 7812164Abstract: The invention provides novel derivatives of cyclopamine having the following formula:Type: GrantFiled: December 27, 2007Date of Patent: October 12, 2010Assignee: Infinity Pharmaceuticals, Inc.Inventors: Brian Austad, Mark L. Behnke, Alfredo C. Castro, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Martin Tremblay
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Publication number: 20100249167Abstract: In one aspect, the invention relates to compounds which are useful as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: March 3, 2010Publication date: September 30, 2010Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
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Patent number: 7803807Abstract: The present invention relates to compounds of Formula (I) wherein A, B and C are independently methine, said methine being optionally substituted; D is nitrogen; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted and least two of T, U, V and W are said methine groups; X is —N(SO2R4)—, N(COR5)— or —CO—; Y is C(R6)(R7)—, —O— or —N(R8) and a pharmaceutically acceptable salt, ester or N-oxide derivative thereof.Type: GrantFiled: October 26, 2009Date of Patent: September 28, 2010Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Norikazu Otake, Minoru Moriya, Yoshio Ogino, Kenji Matsuda, Yoshikazu Nagae, Akio Kanatani, Takehiro Fukami
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Publication number: 20100240688Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.Type: ApplicationFiled: September 12, 2008Publication date: September 23, 2010Applicants: ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC., ADDEX PHARMA, S.A.Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald, Guillaume Albert Jacques Duvey, Robert Johannes Lutjens, Patrick Terry Finn
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Publication number: 20100234409Abstract: Compounds of the formulae (I) and (II): (wherein Q, X, E, G1, G2, R2, R3, R4, R5, R6 and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.Type: ApplicationFiled: May 20, 2005Publication date: September 16, 2010Inventors: Lihu Yang, Songnian Lin, Gregori Morriello, Liangqin Guo, Changyou Zhou
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Publication number: 20100210674Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt or ester thereof wherein X, Y, R1, R2 are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents.Type: ApplicationFiled: January 7, 2010Publication date: August 19, 2010Inventors: Jing Zhang, Zhuming Zhang
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Patent number: 7776875Abstract: There are provided compounds of the formula and pharmaceutically acceptable salts and esters and enantiomers thereof wherein W, X, X?, Y, V, V?, A, B and R are as described herein. The compounds have utility as antiproliferative agents, especially, as anticancer agents.Type: GrantFiled: November 18, 2008Date of Patent: August 17, 2010Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Xingchun Han, Yun He, Song Yang, Zhuming Zhang
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Publication number: 20100204257Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt, ester or enantiomer thereof wherein W, X, Y, V, R1 and R2 are as described herein. The compounds have utility as antiproliferative agents, especially, as anticancer agents.Type: ApplicationFiled: January 12, 2010Publication date: August 12, 2010Inventors: Li Chen, Xingchun Han, Song Yang, Zhuming Zhang
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Publication number: 20100197714Abstract: The present invention relates to compounds of formula (I) below having pharmacological activity towards the sigma (?) receptor, and more particularly to spiro-pyrano-pyrazole compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.Type: ApplicationFiled: April 16, 2008Publication date: August 5, 2010Inventors: Bernhard Wünsch, Dirk Schepmann, Torsten Schläger, Daniel Zamanillo-Castanedo
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Publication number: 20100197716Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles 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: ApplicationFiled: April 16, 2010Publication date: August 5, 2010Inventors: Jennifer Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
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Publication number: 20100190813Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to some thieno-pyrano-pyrazole derivatives, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis or pain.Type: ApplicationFiled: June 20, 2008Publication date: July 29, 2010Inventors: Christoph Oberdorf, Dirk Schepmann, Bernhard Wünsch, Daniel Zamanillo-Castanedo
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Publication number: 20100190814Abstract: There are provided compounds of the formula and pharmaceutically acceptable salts and esters and enantiomers thereof wherein X, Y, V, R1, R2 and R are as described herein. The compounds have utility as antiproliferative agents, especially, as anticancer agents.Type: ApplicationFiled: January 12, 2010Publication date: July 29, 2010Inventors: Li Chen, Xingchun Han, Lisha Wang, Min Wang, Song Yang, Zhuming Zhang
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Publication number: 20100190768Abstract: The present invention relates to a compound represented by the formula (1) which is useful as a glucocorticoid receptor function regulating agent, an anti-inflammatory agent or an antidiabetic agent, or a pharmaceutically acceptable salt thereof: wherein R1 is aralkyl, etc.; R2 is H, etc.; —W4?W5—W6?W7— is a group of the formula: —CR4?CR5—CR6?CR7— (in which R4, R5, R6 and R7 are independently a group of the formula: -E-A (E is a single bond, etc., A is H or nitro, etc.)), etc.; R8 is a group of the formula: —OR11 (R11 is H, etc.), etc.; R9 is trifluoromethyl, etc.; R10 is a group of the formula: —[C(R13)(R14)]n—R15 (R13 and R14 are independently H, etc., n is an integer of 0 to 10, R15 is a group of the formula: N(R18)R19 (R18 and R19 form a nitrogen-containing heteromonocycle together with a nitrogen atom to which they are bonded), etc.).Type: ApplicationFiled: September 29, 2006Publication date: July 29, 2010Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Toshihiko Sone, Rieko Sawaki, Tomoko Nakajima
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Publication number: 20100166819Abstract: The invention is related to compounds of formula (I) that can be used as antagonists of the TGF? family type I receptors, Alk5 and/or Alk4, compositions and methods of use. The compounds of formula (I) can be employed in the prevention and/or treatment of diseases such as fibrosis (e.g., renal fibrosis, pulmonary fibrosis, and hepatic fibrosis), progressive cancers, or other diseases for which reduction of TGF? family signaling activity is desirable.Type: ApplicationFiled: December 22, 2006Publication date: July 1, 2010Inventors: Wen-Cherng Lee, Lihong Sun, Michael Hoemann, Deqiang Niu, Dingxue Yan, Claudio Chuaqui, Russell Petter, Helen (Xiaomei) Feng
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Publication number: 20100160255Abstract: The present invention provides a compound represented by the formula (I): wherein E is an optionally substituted cyclic group; D is a carbonyl group or a sulfonyl group; A is CH or N; ring P is an optionally further substituted 5- to 7-membered ring; ring Q is an optionally further substituted 5- to 7-membered nonaromatic ring; and ring R is an optionally further substituted and optionally condensed 5- to 7-membered nonaromatic ring, or a salt thereof. The compound of the present invention has an ACC inhibitory activity, is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and has superior properties in the efficacy, duration of activity, specificity, low toxicity and the like.Type: ApplicationFiled: July 28, 2006Publication date: June 24, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Makoto Kamata, Kohji Fukatsu, Tohru Yamashita, Naoki Furuyama, Satoshi Endo
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Publication number: 20100137297Abstract: The present invention relates to spiroindalone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: ApplicationFiled: May 12, 2008Publication date: June 3, 2010Inventors: Joan M. Fletcher, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
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Patent number: 7727999Abstract: The present invention relates to optionally substituted 1,3,8-triaza-spiro[4.5]decan-2-one compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: GrantFiled: January 27, 2009Date of Patent: June 1, 2010Assignee: ACADIA Pharmaceuticals Inc.Inventor: Nathalie Schlienger
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Patent number: 7723350Abstract: The present invention relates to a compound of the following formula: where R1-R6, R10, Y, n, m, p, and q are as defined herein. Compounds and compositions of the present invention are useful for the treatment of diseases associated with the overexpression of CCR2.Type: GrantFiled: June 20, 2008Date of Patent: May 25, 2010Assignee: Glaxo Group LimitedInventors: Hilary Schenck Eidam, Pamela A. Haile, Terry Vincent Hughes, Clark A. Sehon
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Publication number: 20100120808Abstract: Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the ? opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other ? opioid receptor-mediated conditions.Type: ApplicationFiled: June 12, 2009Publication date: May 13, 2010Applicant: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec, Guo-Hua Chu