Hetero Ring In The Polycyclo Ring System Patents (Class 514/320)
-
Publication number: 20110230463Abstract: [Object] Provided is a compound which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient for an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells. [Means for Solution] According to the present invention, a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient of an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells can be provided. The 2H-chromene compound and a derivative thereof which are the compounds of the present invention have an S1P1 agonist action, and can be used particularly for prevention and/or treatment of a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.Type: ApplicationFiled: December 4, 2009Publication date: September 22, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Hironori Harada, Kazuyuki Hattori, Kazuya Fujita, Sunao Imada, Tatsuaki Morokata
-
Publication number: 20110224228Abstract: Novel derivatives of enfumafungin are disclosed herein, along with' their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and method of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: ApplicationFiled: August 10, 2009Publication date: September 15, 2011Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: Mark L Greenlee, Robert Wilkening, James Apgar, Donald Sperbeck, Kenneth J. Wildonger, Dongfang Meng, Dann L. Parker, JR., Ahmed Mamai
-
Publication number: 20110218201Abstract: The compounds of Formula (I), are novel effective inhibitors of the type 4 phosphodiesterase.Type: ApplicationFiled: November 12, 2009Publication date: September 8, 2011Applicant: NYCOMED GMBHInventors: Imre Schlemminger, Beate Schmidt, Dieter Flockerzi, Hermann Tenor, Christof Zitt, Armin Hatzelmann, Degenhard Marx, Clemens Braun, Raimund Külzer, Anke Heuser, Hans-Peter Kley, Geert Jan Sterk
-
Publication number: 20110217335Abstract: Disclosed are macrocyclic compounds of formulae I, I?, II, II?, III, III?, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.Type: ApplicationFiled: January 15, 2009Publication date: September 8, 2011Applicant: UNIVERSITE DE STRASBOURGInventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
-
Publication number: 20110189175Abstract: Provided herein are methods for identifying a subject afflicted with chronic lymphocytic leukemia who is responsive to treatment with a chemotherapeutic agent by detecting the presence or absence of at least one APOE4 allele in the subject, the presence of an APOE4 allele identifying the subject as responsive to the treatment. Also provided are methods of treating a subject afflicted with chronic lymphocytic leukemia, including administering an estrogenic agent, an androgen withdrawal agent, an apoE4 peptide or mimetic thereof, and/or a chemotherapeutic agent in an amount effective to treat said chronic lymphocytic leukemia. Methods of determining a prognosis for a patient diagnosed with chronic lymphocytic leukemia are also provided. In addition, methods for stratifying a subject into a subgroup of a clinical trial and methods for identifying a patient in a clinical trial of a treatment for chronic lymphocytic leukemia are herein provided.Type: ApplicationFiled: January 20, 2011Publication date: August 4, 2011Inventors: J. Brice Weinberg, Warren J. Strittmatter
-
Publication number: 20110178061Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.Type: ApplicationFiled: December 17, 2010Publication date: July 21, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Andreas P. Termin, Esther Ann Martinborough, Nicole Hilgraf, Charles J. Cohen, Corey Anderson
-
Publication number: 20110172226Abstract: The present invention relates to compounds of formula I or salts thereof, wherein, R1 is selected from the group consisting of hydrogen and R4; R2 is selected from the group consisting of hydrogen, acetyl and R4; R3 is selected from the group consisting of alkyl, —O-alkyl, —NH-alkyl, aryl and heterocyclyl; R4 represents a moiety (A) wherein, X is selected from the group consisting of a single bond, alkylene, alkenylene, alkynylene, arylene or a heterocyclylene moiety; R5 and R6 are same or different and are independently selected from hydrogen, alkyl, aryl or heterocyclyl; or R5 and R6 may form together with the nitrogen atom to which they are attached a heterocyclyl ring system.Type: ApplicationFiled: February 12, 2009Publication date: July 14, 2011Applicant: Sun Pharma Advanced Research Company Ltd.Inventors: Jiten Ranchhodbhai Patel, Gopalkumar Chimanlal Patel, Gaurav Sanjivkumar Sheth, Trinadha Rao Chitturi, Rajamannar Thennati
-
Publication number: 20110172244Abstract: The invention provides compounds, of Formula I: pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: February 20, 2009Publication date: July 14, 2011Applicant: IRM LLCInventors: Phillip B. Alper, Robert Epple, Pierre-Yves Michellys, Daniel Mutnick, Victor Nikulin
-
Publication number: 20110172225Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: ApplicationFiled: September 25, 2008Publication date: July 14, 2011Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
-
Publication number: 20110165225Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.Type: ApplicationFiled: May 26, 2009Publication date: July 7, 2011Inventors: Peter Cullis, Marcel Bally
-
Publication number: 20110144159Abstract: The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or 6-membered heteroaryl moiety, or a benzisoxazole, pyrrolopyridine, or benzotriazole group; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, including pain, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.Type: ApplicationFiled: April 9, 2009Publication date: June 16, 2011Inventors: Lorraine Kathleen Fay, Douglas Scott Johnson, Marvin Jay Meyers, Atli Thorarensen, Lijuan Jane Wang
-
Patent number: 7951822Abstract: The object is to provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. The solving means is a 1,3-dihydroisobenzofuran derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: GrantFiled: March 30, 2009Date of Patent: May 31, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Koichi Yamazaki, Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
-
Publication number: 20110124674Abstract: Disclosed are a compound of a formula (I) and its pharmaceutically-acceptable salt: wherein Q is CH or N; R1a, R1b, R1c and R1d are independently a C1-6 alkyl, a halo-C1-6 alkyl, etc.; R2 is a hydrogen atom, etc.; R3 is independently a hydrogen atom, a C1-6 alkyl, etc., or two R3's, taken together, form a bridge such as methylene, etc.; R4a and R4b are independently a hydrogen atom, a C1-6 alkyl, etc.; Z is a bicyclic aromatic hetero ring, etc.; Ar is a benzene ring, etc.; m1 and m2 are independently 0, 1 or 2; n is an integer of from 1 to 4. The compound and its salt act as a melanin concentrating hormone receptor antagonist, and are useful as a preventive or remedy for central system disorders, cardiovascular disorders, metabolic disorders, etc.Type: ApplicationFiled: July 14, 2009Publication date: May 26, 2011Inventors: Hiroyuki Kishino, Nagaaki Sato, Takao Suzuki
-
Publication number: 20110118312Abstract: Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R1 represents a hydrogen atom or a methyl group; R2 is a group bound in a p- or m-position relative to a methylene group and represents a chlorine atom bound in a p-position, a bromine atom bound in a p-position, a methyl group bound in a p-position, a chlorine atom bound in a m-position or a bromine atom bound to in a m-position; X represents a methylene or an oxygen atom; and n represents an integer of 1 to 3.Type: ApplicationFiled: January 20, 2011Publication date: May 19, 2011Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Tomohiro TOYODA, Hidefumi YOSHINAGA
-
Publication number: 20110118262Abstract: Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same.Type: ApplicationFiled: June 24, 2009Publication date: May 19, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin Bentzien, Stephen James Boyer, Jennifer Burke, Anne Bettina Eldrup, Xin Guo, John David Huber, Thomas Martin Kirrane, Fariba Soleymanzadeh, Alan David Swinamer
-
Publication number: 20110111057Abstract: The present invention provides a method for treating cancer in a mammal comprising contacting the cancer cells with a compound which is a apogossypol, derivative.Type: ApplicationFiled: October 7, 2010Publication date: May 12, 2011Inventors: John C. Reed, Maurizio Pellecchia
-
Publication number: 20110105475Abstract: The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).Type: ApplicationFiled: March 30, 2009Publication date: May 5, 2011Applicant: MERXCK PATENT GESELLSCHAFTInventors: Didier Roche, Giséle Mautino, Ingo Kober, Francis Contard, Serge Christmann-Franck, Saumitra Sengupta, Ramesh Sistla, Gummadi Venkateshwar Rao
-
Publication number: 20110105506Abstract: Diaminoalkanes of Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.Type: ApplicationFiled: May 28, 2010Publication date: May 5, 2011Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
-
Publication number: 20110105463Abstract: Compounds of Formula (I): in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: ApplicationFiled: June 24, 2009Publication date: May 5, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff
-
Patent number: 7935714Abstract: Provided herein is a composition that contains an effective amount of one or more compounds for treating, preventing, or ameliorating a disorder such as insomnia or another sleeping disorder and using the composition.Type: GrantFiled: May 13, 2005Date of Patent: May 3, 2011Assignee: Bright Future Pharmaceutical LaboratoriesInventors: Hsiao Chang Chan, Yu Lin Gou, Dewi Kenneth Rowlands, Yiu Wa Chung
-
Patent number: 7928125Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: October 29, 2007Date of Patent: April 19, 2011Assignee: SmithKline Beecham LimitedInventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
-
Publication number: 20110082098Abstract: Novobiocin analogues are useful in methods of treating, inhibiting, and/or preventing cyst formation in autosomal dominant polycystic kidney disease (ADPKD) in a subject. The disclosure provides methods of treating ADPKD comprising administering a therapeutically effective amount of a coumarin-3-carboxamide novobiocin analogue. Accordingly, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of mTOR pathway phosphoproteins P-mTOR, P-Akt and P-S6K, or combinations thereof. Further, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of Hsp-90 client proteins CFTR, ErbB2, c-Raf and Cdk4, or combinations thereof.Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Applicant: UNIVERSITY OF KANSASInventors: James P. Calvet, Brian S.J. Blagg, Shirin V. Sundar, Brenda S. Magenheimer
-
Patent number: 7919508Abstract: The present invention provides compounds of formula I: a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, X and n are defined as defined herein. Additionally, a method for treating dopamine-related neurological disorders selected form the group consisting of neurological, psychological, cardiovascular, cognitive or attention disorders, substance abuse and addictive behavior, or a combination thereof, comprising administering to a patient in need of such treatment a therapeutically effective amount of compounds of formula I.Type: GrantFiled: October 24, 2006Date of Patent: April 5, 2011Assignee: Aventis Pharmaceuticals Inc.Inventors: Gregory Shutske, Keith J. Harris, Kenneth J. Bordeau, Michael R. Angelastro, Stanly John, Joseph T. Klein, Jinqi Lu, Catherine Bomont
-
Patent number: 7919509Abstract: To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: GrantFiled: February 27, 2009Date of Patent: April 5, 2011Assignee: Kowa Company, Ltd.Inventors: Ayumu Okuda, Takayuki Matsuda, Toru Miura, Hidefumi Ozawa, Ayako Tosaka, Koichi Yamazaki, Yuki Yamaguchi, Sayaka Kurobuchi, Yuichiro Watanabe, Kimiyuki Shibuya
-
Publication number: 20110065743Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.Type: ApplicationFiled: October 25, 2010Publication date: March 17, 2011Applicant: Research Triangle InstituteInventors: Frank Ivy CARROLL, Hernan A. Navarro, Lawrence E. Brieaddy, Scott P. Runyon, James B. Thomas
-
Publication number: 20110065707Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof, wherein A1, A2, R1, R2, R3, R4, R5 and R6 have the significance given herein.Type: ApplicationFiled: September 3, 2010Publication date: March 17, 2011Inventors: Jean Ackermann, Aurelia Conte, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
-
Publication number: 20110059913Abstract: The present invention relates to identification of Oroxylum indicum, Indian medicinal plant as a rich source for flavanoid compounds. Mucoprotective and antigastric ulcer properties in the flavone class of compounds isolated therefrom have been identified along with a flavanoids mixture in substantial yields from hexane and acetone extracts. The hexane extract was fractionated, purified and the compounds identified as Oroxylin A, Chrysin and Baicalein. The acetone extract was purified and the compounds obtained identified as methoxy chrysin, Oroxyloside methyl ester and chrysin-7-O-methyl glycoside.Type: ApplicationFiled: November 12, 2010Publication date: March 10, 2011Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Janaswamy Madusudana RAO, Suresh Babu KATRAGADDA, Hari Babu TATIPAKA, Manjulatha KHANAPUR, Muralidhar Gurachar PUROHIT, Venkata Srinivas PULLELA, Jhillu Singh YADAV
-
Publication number: 20110059945Abstract: 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: ApplicationFiled: November 12, 2010Publication date: March 10, 2011Applicant: 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
-
Patent number: 7902253Abstract: An isoflavone derivative of tectorigenin compound as shown in formula (II), its preparation method and the antiviral medicine containing it as an effective constituent. The compound structure is shown as follows: Where:: R1 is H, NH2 or SO3M; R2 is OR?; R3 is H or —CH2NR?; where R? is H, —CH2COONa or —CH2CH2NMe2; NR? is or —NMe2; M is H, Na, K or N+H (CH2CH2OH)3.Type: GrantFiled: May 14, 2004Date of Patent: March 8, 2011Assignees: Chengdu Dikang Pharmaceutical Institute, Sichuan Dikang Sci-Tech Pharmaceutical Co., Ltd.Inventors: Xuemin Xu, Chongjun Yuan, Jia Wang, Shangbin Qi, Hai Yin, Yanming Zeng
-
Patent number: 7893090Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: October 30, 2007Date of Patent: February 22, 2011Assignee: SmithKline Beecham LimitedInventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
-
Patent number: 7888510Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.Type: GrantFiled: July 29, 2004Date of Patent: February 15, 2011Assignee: Laboratorios del Dr. Esteve S.A.Inventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
-
Publication number: 20110015185Abstract: The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.Type: ApplicationFiled: September 28, 2010Publication date: January 20, 2011Applicant: BIOVITRUM ABInventors: Gary Johansson, Peter Brandt, Björn M. Nilsson
-
Patent number: 7872002Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: June 6, 2008Date of Patent: January 18, 2011Assignee: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W. F. Wasley
-
Publication number: 20110009396Abstract: The present invention provides compounds represented by formula 1: wherein, R1 R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.Type: ApplicationFiled: July 25, 2008Publication date: January 13, 2011Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Rada Dalal, Sapna Parikh, Aditi Amol Tannu
-
Patent number: 7863266Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: June 6, 2008Date of Patent: January 4, 2011Assignee: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta
-
Publication number: 20100331298Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: ApplicationFiled: December 10, 2008Publication date: December 30, 2010Applicant: CytoPathfinder, Inc.Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
-
Patent number: 7858614Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: June 6, 2008Date of Patent: December 28, 2010Assignee: Helicon Therapeutics, Inc.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
-
Patent number: 7855193Abstract: 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: GrantFiled: July 24, 2006Date of Patent: December 21, 2010Assignee: 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
-
Patent number: 7855200Abstract: The present invention relates to methods of using Oroxylum indicum as a rich source for flavanoid compounds having mucoprotective and antigastric ulcer properties, and containing Oroxylin A, Chrysin and Baicalein.Type: GrantFiled: January 9, 2007Date of Patent: December 21, 2010Assignee: Council of Scientific and Industrial ResearchInventors: Janaswamy Madusudana Rao, Suresh Babu Katragadda, Hari Babu Tatipaka, Manjulatha Khanapur, Muralidhar Gurachar Purohit, Venkata Srinivas Pullela, Jhillu Singh Yadav
-
Patent number: 7842716Abstract: The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins.Type: GrantFiled: March 29, 2004Date of Patent: November 30, 2010Assignee: HeartDrug Research, LLCInventor: Victor L. Serebruany
-
Patent number: 7842704Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: December 11, 2007Date of Patent: November 30, 2010Assignee: Theravance, Inc.Inventors: Mathai Mammen, Sarah Dunham
-
Patent number: 7838535Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: December 11, 2007Date of Patent: November 23, 2010Assignee: Theravance, Inc.Inventors: Mathai Mammen, Sarah Dunham
-
Publication number: 20100292218Abstract: 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: ApplicationFiled: December 4, 2009Publication date: November 18, 2010Inventors: Ruihong CHEN, Allan E. Rubenstein, Jin-Chen Yu, Nicolas Winssinger, Sofia Barluenga
-
Publication number: 20100286124Abstract: The present invention relates to new prop-2-yn-1-amine inhibitors of monoamine oxidase type B activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 9, 2010Publication date: November 11, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
-
Publication number: 20100286201Abstract: New polymorphic forms of (S)-2-((4-benzofuranyl)carbonylamino methyl)-1-((4-(2-methyl-5-(4-fluorophenyl))thiazolyl)carbonyl)piperidine, methods for their preparation and use in medicine.Type: ApplicationFiled: September 11, 2008Publication date: November 11, 2010Inventor: Leanda Jane Kindon
-
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
-
Patent number: 7812034Abstract: Liposarcomas are treated using HIV protease inhibitors, particularly nelfinavir. The protease inhibitors may be used alone or in combination with traditional cancer treatments, such as chemotherapy, radiotherapy, or surgery.Type: GrantFiled: November 2, 2004Date of Patent: October 12, 2010Assignee: City of HopeInventors: Warren Chow, Chu-Chih Shih
-
Patent number: 7812019Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.Type: GrantFiled: November 22, 2005Date of Patent: October 12, 2010Assignee: Abbott LaboratoriesInventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, Jr., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
-
Publication number: 20100256142Abstract: A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.Type: ApplicationFiled: September 25, 2009Publication date: October 7, 2010Inventors: Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski
-
Publication number: 20100249094Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: March 10, 2010Publication date: September 30, 2010Inventors: Kap-Sun Yeung, Kyle E. Parcella, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, John F. Kadow, Andrew Nickel