Publication number: 20110144101
Abstract: The present invention provides methods for the use of compounds having formula (I) in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis, wherein R1-R11, t, X, Y, Z, and n are as defined herein.
Type:
Application
Filed:
July 20, 2010
Publication date:
June 16, 2011
Applicant:
EISAI CO., LTD.
Inventors:
Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-André Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
Publication number: 20110112071
Abstract: A compound represented by formula (I?): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q? represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.
Type:
Application
Filed:
January 18, 2011
Publication date:
May 12, 2011
Applicant:
MOCHIDA PHARMACEUTICAL CO., LTD.
Inventors:
Hideharu UCHIDA, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
Publication number: 20110059945
Abstract: The present invention relates to compounds of the general formula (I) 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 may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
Type:
Application
Filed:
November 12, 2010
Publication date:
March 10, 2011
Applicant:
EPIX PHARMACEUTICALS, INC.
Inventors:
Ashis K. Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa Cheruku, Pini Orbach, Anurag Sharadendu, Robert Christian Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker
Publication number: 20100322928
Abstract: A method of treating systemic lupus erythematosus (SLE) in a subject are provided. The method comprise altering in cells of the subject activity and/or expression of at least one gene selected from the group consisting of Mpo, Ltf, Lcn, Camp, Ngp, Slfn, Ctsg, Thbs1, S100a8, 1190003K14Rik, Prtn3, S100a9, Tfpi, Fzd6, Nid1, 5830484A20Rik, 5830484A20 LOC 545340, Tnfsf4, IPstpip2, Pigr, 270022B06Rik, L5R-alpha, A130040M12Rik, Gpr132, Cd8b1, Dhx9, Cyp11a1, Lmo7, Rnf184, Pstpip2, Hdgfrp3, Ass1 and Zbtb20, thereby treating SLE. Also provided are methods of diagnosing SLE and monitoring treatment of SLE.
Type:
Application
Filed:
January 17, 2008
Publication date:
December 23, 2010
Applicant:
Yeda Research and Development Co., Ltd.
Inventor:
Edna Mozes
Patent number: 7855193
Abstract: The present invention relates to compounds of the general formula (I) 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 may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
Type:
Grant
Filed:
July 24, 2006
Date of Patent:
December 21, 2010
Assignee:
EPIX Pharmaceuticals, Inc.
Inventors:
Ashis K. Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa R. Cheruku, Pini Orbach, Anurag Sharadendu, Robert Christian Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker
Publication number: 20100292218
Abstract: The present invention provides compounds of formulae Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va and the therapeutic use thereof. The present invention also includes methods of treating NF2-deficient or NF1-deficient cells or neurodegenerative diseases with radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va. Furthermore, the present invention is directed to methods of inhibiting the growth of NF2-deficient or NF1-deficient tumors. The methods comprise contacting NF2-deficient or NF1-deficient tumor cells with radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va. The present invention is also directed to the combinational use of radicicol or its derivatives, such as one or more compounds of formula I, II, III, IV, V, Ia, Ia?, IIa, IIa?, IIIa, IIIa?, IVa, or Va with at least one additional active agent, such as one or more HSP90 inhibitors.
Type:
Application
Filed:
December 4, 2009
Publication date:
November 18, 2010
Inventors:
Ruihong CHEN, Allan E. Rubenstein, Jin-Chen Yu, Nicolas Winssinger, Sofia Barluenga
Publication number: 20100179109
Abstract: Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
Type:
Application
Filed:
April 4, 2008
Publication date:
July 15, 2010
Inventors:
Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, Damiano Ghirlanda, Alexey V. Ishchenko, Lara S. Kallander, Brian Lawhorn, Colin A. Leach, Qing Lu, Gerard McGeehan, Jaclyn R. Patterson, Robert D. Simpson, Suresh B. Singh, Patrick Stoy, Lamont R. Terrell, Colin Tice, Zhenrong Xu, Jing Yuan, Catherine C. K. Yuan, Jing Zhang, Wei Zhao