Plural Double Bonds Between The Ring Members Of The Oxazole Ring Patents (Class 548/235)
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Patent number: 7825155Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.Type: GrantFiled: September 13, 2006Date of Patent: November 2, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Patent number: 7816385Abstract: A novel class of dicarboxylic acid derivatives, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator -Activated Receptors (PPAR).Type: GrantFiled: December 12, 2003Date of Patent: October 19, 2010Assignee: High Point Pharmaceuticals, LLCInventors: Per Sauerberg, Lone Jeppesen, Zdenek Polivka, Karel Sindelar
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Publication number: 20100256923Abstract: One embodiment includes a material exhibiting an optical response signature for neutrons that is different than an optical response signature for gamma rays, said material exhibiting performance comparable to or superior to stilbene in terms of distinguishing neutrons from gamma rays, wherein the material is not stilbene. Another embodiment includes a substantially pure crystal exhibiting an optical response signature for neutrons that is different than an optical response signature for gamma rays, the substantially pure crystal comprising a material selected from a group consisting of: 1-1-4-4-tetraphenyl-1-3-butadiene; 2-fluorobiphenyl-4-carboxylic acid; 4-biphenylcarboxylic acid; 9-10-diphenylanthracene; 9-phenylanthracene; 1-3-5-triphenylbenzene; m-terphenyl; bis-MSB; p-terphenyl; diphenylacetylene; 2-5-diphenyoxazole; 4-benzylbiphenyl; biphenyl; 4-methoxybiphenyl; n-phenylanthranilic acid; and 1-4-diphenyl-1-3-butadiene.Type: ApplicationFiled: April 3, 2009Publication date: October 7, 2010Inventors: Stephen A. Payne, Wolfgang Stoeffl, Natalia P. Zaitseva, Nerine J. Cherepy, M. Leslie Carman
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Patent number: 7803825Abstract: The present invention provides a compound of formula Ia: and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.Type: GrantFiled: July 15, 2008Date of Patent: September 28, 2010Assignee: Wyeth LLCInventors: Jonathan Laird Gross, Albert Jean Robichaud, Marla Jean Williams, Alessandro Mazzacani
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Publication number: 20100240708Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, methods for using the compounds and processes for making the compounds. More specifically, the disclosure relates to alpha-(N-benzenesulfonamido)cycloalkyl compounds that may inhibit one or both of: (i) the functioning of a ?-secretase enzyme; or (ii) the production of ?-amyloid. Such compounds may be beneficial in the treatment of Alzheimer's disease and other conditions. Representative compounds have the following formula I: wherein: A, R1, and R2 are described herein.Type: ApplicationFiled: March 17, 2010Publication date: September 23, 2010Inventors: Dalton King, Zhaoxing Meng, Ivar M. McDonald, Richard E. Olson, John E. Macor
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Publication number: 20100234364Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 10, 2007Publication date: September 16, 2010Inventors: Arindrajit Basak, Jeff Jin, Jimmie Moore, Andrew M.K. Pennell, Sreenlvas Punna, Solomon Ungashe, Zheng Wei
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Patent number: 7795287Abstract: A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: August 30, 2007Date of Patent: September 14, 2010Assignee: Allergan, Inc.Inventor: David W. Old
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Patent number: 7795291Abstract: Compounds are provided which have the structure of Formula (I): wherein R1 is halogen; and X is hydrogen or halogen, and salts thereof, which compounds are useful as anti-atherosclerotic, anti-dyslipidemic, anti-diabetic, and anti-obesity agents.Type: GrantFiled: July 5, 2007Date of Patent: September 14, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Joseph A. Tino, Peter T. W. Cheng, Yan Shi, Jun Li, Ranjan Mukherjee
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Patent number: 7790728Abstract: The present disclosure relates to a compound of formula (I) wherein: A is an optionally substituted monocyclic or polycyclic aryl or heteroaryl group; B is an optionally substituted monocyclic nitrogen-containing heteroaryl group; and either a) R1 and R2 are chosen from a hydrogen atom and specified substituents, or b) R2, R1 and the —NH— group to which R1 is attached, form a moiety chosen from the moiety of formulae (IIa) and (IIb): or a pharmaceutically acceptable salt thereof, or a N-oxide thereof. The present disclosure also relates to a method for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor.Type: GrantFiled: July 25, 2006Date of Patent: September 7, 2010Assignee: Laboratorios Almirall, S.A.Inventors: Bernat Vidal Juan, Christina Esteve Trias, Lidia Soca Pueyo, Paul Robert Eastwood
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Publication number: 20100222580Abstract: The invention relates to a process for the preparation of onium alkylsulfates by reaction of an onium halide with a symmetrically substituted dialkyl sulfate, in which the alkyl group can have 1 to 14 C atoms, with an asymmetrically substituted dialkyl sulfate, in which one alkyl group can have 4 to 20 C atoms and the second alkyl group denotes methyl or ethyl, with an alkyl trialkylsilyl sulfate, with an alkyl acyl sulfate or with an alkyl sulfonyl sulfate, where the reaction with a dialkyl sulfate is carried out at room temperature.Type: ApplicationFiled: November 18, 2005Publication date: September 2, 2010Applicant: MERCK PATENT GMBHInventors: Nikolai Ignatyev, Urs Welz-Biermann, Andriy Kucheryna, Helge Willner
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Patent number: 7786110Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: GrantFiled: November 8, 2007Date of Patent: August 31, 2010Assignee: Roche Palo Alto LLCInventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
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Publication number: 20100215616Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: February 8, 2010Publication date: August 26, 2010Inventors: Jeffrey Lee Romine, Denis R. St. Laurent, Makonen Belema, Lawrence B. Snyder, Lawrence G. Hamann, John F. Kadow, Jayne Kapur, Andrew C. Good, Omar D. Lopez, Rico Lavoie, John A. Bender
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Publication number: 20100210849Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.Type: ApplicationFiled: February 10, 2010Publication date: August 19, 2010Applicant: DIVERGENCE, INC.Inventors: Urszula Slomczynska, Matt W. Dimmic, William P. Haakenson, JR., Al Wideman
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Patent number: 7759374Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).Type: GrantFiled: October 12, 2006Date of Patent: July 20, 2010Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Alexey Rivkin, Fumikiko Yoshimura, Ting-Chao Chou, Ana E. Gabarda, Huajin Dong
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Patent number: 7754747Abstract: The present invention relates to oxazolo-naphthyl acids of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.Type: GrantFiled: August 22, 2005Date of Patent: July 13, 2010Assignee: Wyeth LLCInventors: Thomas J. Commons, Richard P. Woodworth, Jr.
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Patent number: 7745470Abstract: There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.Type: GrantFiled: March 8, 2006Date of Patent: June 29, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Lorin A. Thompson, III, Kenneth M. Boy, Jianliang Shi, John E. Macor
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Patent number: 7737140Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein J1, J2, U1, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: April 21, 2009Date of Patent: June 15, 2010Assignee: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20100137280Abstract: The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl, is a single or double bond; X1 and X2 are N, CRx1, NRx2, or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.Type: ApplicationFiled: March 20, 2008Publication date: June 3, 2010Applicant: ABBOTT GMBH & CO. KGInventors: Thomas Schultz, SR., Wilfried Braje, Sean Colm Turner, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Matthias Mayrer
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Publication number: 20100130495Abstract: The present invention relates to novel compounds of formula I and therapeutically acceptable salts thereof, their pharmaceutical compositions, processes for making them and their use as therapeutic methods for treatment and/or prevention of various diseases.Type: ApplicationFiled: November 6, 2009Publication date: May 27, 2010Applicant: ASTRAZENECA ABInventors: Rickard FORSBLOM, Kim PAULSEN, Didier ROTTICCI, Ellen SANTANGELO, Magnus WALDMAN
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Publication number: 20100130555Abstract: A method for treating or preventing injury of a biological material exposed to hypoxic or ischemic conditions comprising contacting the biological material with an effective amount of a compound is disclosed. The compound has the following structure (I): R1—(S)n—R2 ??(I) or a stereoisomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, and n are as defined herein. Compounds, methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: October 16, 2009Publication date: May 27, 2010Applicant: Ikaria, Inc.Inventors: Edward A. Wintner, Fuqiang Ruan
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Patent number: 7713968Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, and B are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: April 22, 2009Date of Patent: May 11, 2010Assignee: Allergan, Inc.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Publication number: 20100113540Abstract: Compounds of formula (I) are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiratory tract diseases: wherein (i) R1 is C1-C6-alkyl or hydrogen; and R2 is hydrogen or a group —R7, —Z—Y—R7, —Z—NR9R10; —Z—CO—NR9R10, —Z—NR9—[AE11]C(O)O—R7, or —Z—C(O)—R7; and R3 is a lone pair, or C1C6-alkyl; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring and R2 is a lone pair or a group —R7, —Z—Y—R7, —Z—NR9R10, —Z—CO—NR9R10, —Z—NR9—[AE12]C(O)O—R7; or; —Z—C(O)—R7; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group —Y—R7, —Z—Y—R7, —Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—[AE13]C(O)O—R7; or; —Z—C(O)—R7; and R3 is a lone pair, or C1-C6-alkyl; R4 and R5 are independently selected from the group consisting of aryl, ary-tfused-heterocycloalkyl, heteroaryl, C1-C6-alkyl, cycloalkyl; R6 is —OH, C1-C6-alkyl, C1-C6-alkoxy, hydroxy-C1-C6-alkyl, nitrile, a gType: ApplicationFiled: August 8, 2006Publication date: May 6, 2010Applicant: ARGENTA DISCOVERY LIMITEDInventors: Nicholas Charles Ray, Richard James Bull, Harry Finch, Marco van den Heuvel, Jose Antonio Bravo
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Patent number: 7709509Abstract: The invention relates to oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing peroxisome proliferator activator receptor (PPAR) delta agonist activity comprising compounds of formula I, in which the R1-R7 substituents as well as the U, V, W, X Y and z radicals are as defined herein, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved; neurodegenerative diseases and/or demyelinating disorders of the central and peripheral nervous systems and/or neurological diseases involving neuro-inflammatory processes and/or other peripheral neuropathies.Type: GrantFiled: June 5, 2008Date of Patent: May 4, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Stefanie Keil, Wolfgang Wendler, Maike Glien, Jochen Goerlitzer, Karen Chandross, Daniel G. McGarry, Jean Merrill, Patrick Bernardelli, Baptiste Ronan, Corinne Terrier
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Patent number: 7709654Abstract: Process for the preparation of oxazole, imidazole, and pyraxole boryl compounds. The compounds are intermediates to functionalized compounds, both natural and synthetic which are cytotoxic, anticancer and antiviral agents.Type: GrantFiled: September 11, 2007Date of Patent: May 4, 2010Assignee: Board of Trustees of Michigan State UniversityInventors: Milton R. Smith, III, Robert E. Maleczka, Jr., Venkata A. Kallepalli, Edith Onyeozili
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Patent number: 7700637Abstract: Compounds of the formula provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the present invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases (IBDs), ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.Type: GrantFiled: September 16, 2004Date of Patent: April 20, 2010Assignee: Novartis AGInventors: Robert Edson Damon, Thalaththani Ralalage Vedananda
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Patent number: 7700607Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: GrantFiled: July 18, 2007Date of Patent: April 20, 2010Inventors: Essa Hu, Jason Brooks Human, Roxanne Kunz, Andrew Tasker, Ryan White
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Publication number: 20100093816Abstract: The invention provides [2-(4-chloro-benzyloxy)-ethyl]-[2-((R)-cyclohexyl-hydroxy-phenyl-methyl)-oxazol-5-yl-methyl]-dimethyl-ammonium napadisylate, pharmaceutical compositions containing it, and its use in therapy.Type: ApplicationFiled: February 6, 2008Publication date: April 15, 2010Applicants: ARGENTA DISCOVERY LTD., ASTRAZENECA ABInventors: Barbara Giuseppina Avitabile, David O'Sullivan, James Richard Bull
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Patent number: 7683182Abstract: The present invention is directed to monohydrate and anhydrate crystal forms of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol, an estrogenic receptor modulator useful in the treatment of, for example, diseases related to abnormal levels of estrogen.Type: GrantFiled: March 6, 2006Date of Patent: March 23, 2010Assignee: Wyeth LLCInventors: Abdolsamad Tadayon, Silvio Iera, Hong Wen, Marc S. Tesconi, Mannching Sherry Ku
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Publication number: 20100048895Abstract: The present invention relates to a novel process, useful for preparing key intermediates of formula (I) in the synthesis of various compounds, among them compounds which are potent and specific antagonists of D3 receptors, in which X may be Nitrogen or Sulfur; Het means aryl or heteroaryl; each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl C1-C6 alkoxy, halo C1-C6 alkyl C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —C(O)R1, nitro, hydroxy, —NR2R3, cyano or a group Z; R1 is a C1-C4 alkyl —OR3 or —NR3R4; R2 is hydrogen or C1-C6 alkyl; R3 is hydrogen or C1-C6 alkyl; R is H, C1-C6 alkyl aryl, benzyl; each of which may be substituted by 1 to 4 groups J; according to the following Scheme 1: in which step a means a reaction in basic conditions of compounds (IIA) with 3-thiosemicarbazide derivatives, followed by a treatment with an inorganic base and n-propane phosphonic cyclic anhydride and final pH adjustement with inorganic acids to give compounds of forType: ApplicationFiled: October 29, 2009Publication date: February 25, 2010Inventor: Sergio Bacchi
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Publication number: 20100041896Abstract: This patent mainly provides a new macrolide compound named FW-04-806, which contains bis-oxazoly in molecule. FW-04-806, a bis-oxazolyl macrolide compound extracted and separated from the ferment liquid of streptomyces FIM-04-806, has anti-tumor activities and provides a chemical research basis for natural drugs and the lead compound for the research and development of new anti-tumor drugs. Anti-tumor in vitro experiment shows that minimal median inhibitory concentration IC50 is 12.36 ug/ml to K562 cell (human chronic mydogenous leukemia leap clone).Type: ApplicationFiled: August 12, 2008Publication date: February 18, 2010Inventors: Zheng WEI, Zhentai Cheng, Tian-en Wei, Yuanrong Cheng, Yunyang Lian, Wei Hung
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Patent number: 7662971Abstract: Improved competitive inhibitors of FAAH employ an ?-keto heterocyclic pharmacophore and a binding subunit having a ?-unsaturation. The ?-keto heterocyclic pharmacophore and a binding subunit are attached to one another, preferably by a hydrocarbon chain. The improvement lies in the use of a heterocyclic pharmacophore selected from oxazoles, oxadiazoles, thiazoles, and thiadiazoles that have alkyl or aryl substituents at their 4 and/or 5 positions. The improved competitive inhibitors of FAAH display enhanced activity over conventional competitive inhibitors of FAAH.Type: GrantFiled: October 8, 2003Date of Patent: February 16, 2010Assignee: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20100035944Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating G protein-coupled receptor 20 (GPR20), and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated GPR20.Type: ApplicationFiled: January 8, 2008Publication date: February 11, 2010Applicant: IRM LLCInventors: Robert Epple, Mihal Azimioara, Christopher Cow, Ross Russo, Victor Nikulin, Gerald Lelais
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Patent number: 7652020Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.Type: GrantFiled: June 1, 2005Date of Patent: January 26, 2010Assignee: Schering CorporationInventors: Zhuyan Guo, Peter Orth, Zhaoning Zhu, Robert D. Mazzola, Tin-Yau Chan, Henry A. Vaccaro, Brian McKittrick, Joseph A. Kozlowski, Brian J. Lavey, Guowei Zhou, Sunil Paliwal, Shing-Chun Wong, Neng-Yang Shih, Pauline C. Ting, Kristin E. Rosner, Gerald W. Shipps, Jr., M. Arshad Siddiqui, David B. Belanger, Chaoyang Dai, Dansu Li, Vinay M. Girijavallabhan, Janeta Popovici-Muller, Wensheng Yu, Lianyun Zhao
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Patent number: 7652061Abstract: Compounds of the formula provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis, Crohn's disease, and conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.Type: GrantFiled: May 19, 2004Date of Patent: January 26, 2010Assignee: Novartis A.G.Inventors: Gary Michael Ksander, Thalaththani Ralalage Vedananda
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Patent number: 7649006Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).Type: GrantFiled: May 9, 2003Date of Patent: January 19, 2010Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Samuel J. Danishefsky, Alexey Rivkin, Yoshimura Fumikiko, Ting-Chao Chou, Ana E. Gabarda, Huajin Dong
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Publication number: 20100009991Abstract: The present invention relates to a novel compound or a salt thereof, which is useful as a CRTH2 antagonist, especially as a medicament for disorder that participates eosinophil, for example, allergic disorder such as asthma, allergic rhinitis, allergic dermatitis, conjunctival inflammation, hives, eosinophilic bronchitis, food allergy, inflammation of the nasal sinuses, multiple sclerosis, angiitis, or chronic obstructive pulmonary disease (COPD) and the like.Type: ApplicationFiled: December 13, 2007Publication date: January 14, 2010Applicant: Astellas Pharma Inc.Inventors: Tadashi Terasaka, Tatsuya Zenkoh, Hisashi Hayashida, Hiroshi Matsuda, Junji Sato, Yoshimasa Imamura, Hiroshi Nagata, Norio Seki, Yoshiyuki Tenda, Mamoru Tasaki, Masahiro Takeda, Seiichiro Tabuchi, Minoru Yasuda, Kazunori Tsubaki
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Publication number: 20090324544Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: June 11, 2009Publication date: December 31, 2009Inventors: Yao-Ling Qiu, Ce Wang, Jiang Long, Lu Ying, Yat Sun Or
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Patent number: 7638513Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, aggrecanase, ADMP, LpxC, ADAMs, TACE, TNF-? or combinations thereof.Type: GrantFiled: December 1, 2005Date of Patent: December 29, 2009Assignee: Schering CorporationInventors: M. Arshad Siddiqui, Umar Faruk Mansoor, Panduranga A. Reddy, Vincent S. Madison
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Patent number: 7638637Abstract: The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure (I) wherein R11 is C5-C18 alkyl or C5-C18 alkenyl; Q is selected from the group consisting of C3-C6 optionally substituted cycloalkyl, C3-C6 optionally substituted heterocyclic, C3-C6 optionally substituted aryl C3-C6 optionally substituted heteroaryl and; R2 is selected from the group consisting of H, C1-C4 alkyl, (C1-C4 alkyl)OH and (C1-C4 alkyl)NH2; R23 is H or C1-C4 alkyl, and R15 is a phosphonate ester or a phosphate ester or a pharmaceutically acceptable salt or tautomer thereof.Type: GrantFiled: November 3, 2004Date of Patent: December 29, 2009Assignee: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald
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Publication number: 20090318514Abstract: The invention provides the use of compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, for the manufacture of a medicament for the treatment or prophylaxis of a condition that may be treated with a thyroid receptor agonist or partial agonist wherein R1, R2, R3, R4, Y, W and R5 are as defined in the specification. The invention also provides compounds of formula (Ia) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, formula (Ia) wherein R1, R2, R3, R4, Y, W and R5 are as defined in the specification.Type: ApplicationFiled: May 3, 2007Publication date: December 24, 2009Inventors: Ana Maria Garcia Collazo, Eva Kristina Koch, Anton Joakim Löfstedt, Aiping Cheng, Sandra Gordon, Tomas Fredrik Hansson
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Patent number: 7628938Abstract: The present invention provides a photochromic compound that is colored when irradiated with visible light and quickly faded when set in a dark place. The photochromic compound according to the present invention is expressed by the following general formula (I): where each of A1, A2 and A3 is a five-member rings forming a 6?-electron system, the three rings being identical, partially identical or totally different from each other, and each ring may have a substituent; B1 and B2 are functional groups, each having an atomic number of five or larger, including a ring compound, and bonded to the 2-carbon of each of A2 and A3, respectively; and R1, R2 and R3 are substituents identical to or different from each other. This compound is highly colorable and durable even when it is dispersed into plastic macromolecular materials. Therefore, it is suitable as a dye material for sunglasses or similar products.Type: GrantFiled: March 21, 2007Date of Patent: December 8, 2009Assignee: National University Corporation Nara Institute of Science and TechnologyInventors: Tsuyoshi Kawai, Takuya Nakajima, Shigekazu Kawai
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Publication number: 20090298854Abstract: This invention is directed to indole acetic acid derivatives and their use in pharmaceutical compositions for the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic disease. The invention is also directed to intermediates useful in preparation of indole acetic derivatives and to methods of preparation.Type: ApplicationFiled: July 23, 2009Publication date: December 3, 2009Inventors: Xin Ma, Louis-David Cantin, Soongyu Choi, Roger Clark, Martin Hentemann, Joachim Rudolph, Rico Lavoie, Zhonghua Zhang
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Publication number: 20090291970Abstract: The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: July 27, 2009Publication date: November 26, 2009Inventors: James P. Beck, Matthew Drowns, Martha A. Warpehoski
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Patent number: 7618991Abstract: The invention concerns compounds of formula (I): Wherein X, Y, R1, R2, R3 and R4 are as described herein. The invention also concerns a method for preparing same and the therapeutic use thereof.Type: GrantFiled: May 23, 2008Date of Patent: November 17, 2009Assignee: Sanofi-AventisInventors: Francis Barth, Murielle Rinaldi-Carmona
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Patent number: 7608721Abstract: The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein R1 to R6, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: GrantFiled: May 8, 2007Date of Patent: October 27, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
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Publication number: 20090264485Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: August 7, 2006Publication date: October 22, 2009Inventors: Hans-Willi Krell, Joerg Middeldorff, Ulrike Reiff, Thomas von Hirschheydt, Edgar Voss
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Publication number: 20090253758Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, and or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, and intermediates useful in the preparation of same.Type: ApplicationFiled: February 19, 2009Publication date: October 8, 2009Inventor: Chris P. Miller
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Publication number: 20090253699Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.Type: ApplicationFiled: October 13, 2005Publication date: October 8, 2009Applicant: PCT Therapeutics, Inc.Inventors: Neil G. Almstead, Guangming Chen, Gary M. Karp, Ellen Welch, Richard Wilde, Jeffrey A. Campbell
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Patent number: 7598281Abstract: The present invention comprises compounds and compositions for the treatment of metabolic disorders and more particularly, those insulin-related metabolic disorders of the blood such as hyperlipidemia, diabetes, insulin-resistence and the like comprising acetic acid derivatives with arylcycloalkyl-substituted alkanoic acid derivatives and their salts. Known as peroxisome proliferator-activated receptors (PPAR) agonists/antagonists, the invention relates to compounds of the formula I wherein the various substituent R-groups are more specifically defined herein.Type: GrantFiled: February 7, 2007Date of Patent: October 6, 2009Assignee: Sanofi-Aventis Deutschland GmbHInventors: Heiner Glombik, Christian Stapper, Eugen Falk, Stefanie Keil, Hans-Ludwig Schaefer, Wolfgang Wendler, Stephanie Knieps
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Patent number: 7598245Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: April 13, 2007Date of Patent: October 6, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael J. Arnost, Guy W. Bemis, Robert J. Davies, Cornelia J. Forster, Ronald Grey, Jr., Mark W. Ledeboer, Brian Ledford, Craig Marhefka, David Messersmith, Albert C. Pierce, Francesco G. Salituro, Jian Wang