Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperazine Ring Patents (Class 514/255.01)
-
Publication number: 20120230943Abstract: The present invention relates to agents, and methods for identifying compounds, which agents and compounds are effective in the treatment, and more particularly, that inhibit cachexia, and its associated or related disorders and conditions. In addition, the invention relates to compositions and methods for the use thereof in treating conditions that are characterized by cachexia, and its associated or related disorders and conditions and/or cachexia, and its associated or related disorders and conditions, such as for example, cancer cachexia and cachexia associated with AIDS, autoimmune disorders, drug addiction, alcoholism, chronic inflammatory disorders, cirrhosis of the liver, anorexia and neurodegenerative disease. In particular, the diagnostic marker and drug target of the invention is the ATGL Lipase, which can be inhibited by e.g. siRNAs and compounds with any of the following structures (I).Type: ApplicationFiled: March 31, 2010Publication date: September 13, 2012Inventors: Robert Zimmerman, Rudolf Zechner, Günther Haemmerle, Gerald Höfler, Suman Das, Achim Lass
-
Publication number: 20120225890Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: ApplicationFiled: March 6, 2012Publication date: September 6, 2012Inventors: Alan D. Snow, Beth Nguyen, Gerardo Castillo, Virginia Sanders, Thomas Lake, Lesley Larsen, Rex T. Weavers, Stephen Lorimer, David Larsen, David L. Coffen, Charlotte Coffen
-
Patent number: 8258140Abstract: The invention concerns bicyclic compounds of Formula I wherein , R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.Type: GrantFiled: February 9, 2010Date of Patent: September 4, 2012Assignee: Astrazeneca ABInventors: Robert Hugh Bradbury, Gregory Richard Carr, Alfred Arthur Rabow, Srinivasa Rao Korupoju, Harikrishna Tumma
-
Publication number: 20120220605Abstract: Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel actrvrh, particularly Nav1.7, Nav 1.8, or Cav 3.2 channel activity are disclosed. More specifically, compounds for use in the treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's disease, depression, schizophrenia, psychosis, and tinnitus are disclosed.Type: ApplicationFiled: September 3, 2010Publication date: August 30, 2012Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Yanbing Ding
-
Patent number: 8252801Abstract: The invention relates to a method of administering histamine H3 antagonist and an antipsychotic therapeutic agent, compositions comprising a histamine H3 antagonist and an antipsychotic therapeutic agent, and a related article of manufacture.Type: GrantFiled: June 3, 2010Date of Patent: August 28, 2012Assignee: Abbott LaboratoriesInventors: Lynne E. Rueter, Kaitlin E. Browman, Jorge D. Brioni, Marlon D. Cowart, Timothy A. Esbenshade, Gerard B. Fox
-
Patent number: 8252786Abstract: The invention relates to a compound (I) wherein R is a heterocyclyl radical; R1 and R2 are independently H or alkyl; R3 is H, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl; R4 and R5 are independently H or alkyl; q is a number selected from 0 and 1; and the salts, solvates, prodrugs or stereoisomers thereof having inhibitory activity for UBC13-UEV interactions and which can be used in the production of pharmaceutical compositions intended for antitumor therapy or the treatment and/or prophylaxis of diseases associated to metabolic pathways involving the UBC13 enzyme, metabolic pathways involving transcriptional factor NF-?B, or pathways involving PCNA or RAD6.Type: GrantFiled: March 7, 2007Date of Patent: August 28, 2012Assignee: Consejo Superior de Investigaciones CientificasInventors: Timothy Thomson Okatsu, Johanna Scheper Sigmund, Ángel Messeguer Peypoch, Ángel Ramírez Ortiz, María Luz Ortiz Melguizo, legal representative, Ma Carmen Fabrega Claveria, legal representative, Gloria Sanclimens Pérez de Rozas, Isabel Masip Masip, Alejandra Moure Fernández, Domingo González Ruiz, Antonio Morreale de León
-
Publication number: 20120214769Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.Type: ApplicationFiled: April 8, 2011Publication date: August 23, 2012Applicant: METABASIS THERAPEUTICS, INC.Inventors: Jorge E. Gomez-Galeno, K. Raja Reddy, Paul D. van Poelje, Robert Huerta Lemus, Thanh Huu Nguyen, Matthew P. Grote, Qun Dang, Scott J. Hecker, Venkat Reddy Mali, Mingwei Chen, Zhili Sun, Serge Henri Boyer, Haiqing Li, William Craigo
-
Publication number: 20120214785Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerald Juergen ROTH, Martin FLECK, Niklas HEINE, Joerg KLEY, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
-
Patent number: 8242175Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.Type: GrantFiled: December 7, 2010Date of Patent: August 14, 2012Assignee: DAC S.R.L.Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
-
Publication number: 20120196824Abstract: The invention provides a therapeutic drug for ischemic stroke. The therapeutic drug has the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof, as an active ingredient.Type: ApplicationFiled: October 8, 2010Publication date: August 2, 2012Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Tomofumi Setsuta, Maki Seki, Hiroshi Iwasaki, Minoru Tanaka
-
Publication number: 20120184520Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.Type: ApplicationFiled: September 15, 2010Publication date: July 19, 2012Applicant: Astellas Pharma Inc.Inventors: Kousei Yoshihara, Daisuke Suzuki, Susumu Yamaki, Yuji Koga, Norio Seki, Jiro Fujiyasu, Masahiro Neya
-
Patent number: 8217046Abstract: The present invention relates to compounds of general formula (I): wherein: R1 represents: halogen, CN or NO2; R2 represents: hydrogen or halogen; n represents: 1 or 2; R3 represents: phenyl substituted by one or more halogens or C1-C6 alkyls; or a cyclohexyl; as well as the therapeutically-acceptable salts or solvates thereof. These compounds are useful as protease-activated receptor-1 (PAR-1) antagonists, particularly in the treatment of thrombosis.Type: GrantFiled: June 19, 2007Date of Patent: July 10, 2012Assignee: Pierre Fabre MedicamentInventors: Michel Perez, Marie Lamothe, Bruno Le Grand, Robert Letienne
-
Publication number: 20120172375Abstract: A method of promoting the differentiation of an oligodendrocyte precursor cell. The method includes administering to the oligodendrocyte precursor cell an effective amount of a compound capable of promoting oligodendrocyte precursor cell differentiation.Type: ApplicationFiled: November 9, 2009Publication date: July 5, 2012Inventors: Bruce Trapp, Wendy B. MacKlin, Carlos E. Pedraza, Elena K. Muratova, Victor V. Sokolov
-
Publication number: 20120171133Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ active agents that modulate dynein expression in the skin. Also provided are methods for screening for substances which modulate dynein expression levels and the methods of using active agents identified by the screening protocol in the treatment of skin.Type: ApplicationFiled: November 29, 2011Publication date: July 5, 2012Applicant: AVON PRODUCTS, INC.Inventors: Qian ZHENG, John W. LYGA, Russell J. WYBORSKI
-
Publication number: 20120165324Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: December 29, 2011Publication date: June 28, 2012Inventors: Francesco G. Salituro, Jeffrey Saunders
-
Patent number: 8198277Abstract: Pharmaceutical compositions of L malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.Type: GrantFiled: December 18, 2008Date of Patent: June 12, 2012Assignee: Sunovion Pharmaceuticals Inc.Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousau
-
Patent number: 8198278Abstract: Besylate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl) carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided.Type: GrantFiled: December 18, 2008Date of Patent: June 12, 2012Assignee: Sunovion Pharmaceuticals Inc.Inventors: Richard Hsia, H. Scott Wilkinson, Tushar Misra, Kostas Saranteas, Patrick Mousaw
-
Publication number: 20120142698Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: ApplicationFiled: August 6, 2010Publication date: June 7, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
-
Publication number: 20120135918Abstract: The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15-A16-A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —C(O)C1-C20alky or a di-aminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.Type: ApplicationFiled: May 12, 2010Publication date: May 31, 2012Applicants: MCGILL UNIVERSITY, THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUNDInventors: Cyril Y. Bowers, David H. Coy, Simon J. Hocart, Gloria S. Tannenbaum
-
Publication number: 20120136006Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.Type: ApplicationFiled: February 6, 2012Publication date: May 31, 2012Inventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
-
Publication number: 20120136002Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.Type: ApplicationFiled: May 18, 2010Publication date: May 31, 2012Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
-
Patent number: 8188090Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein X, Q and R1-R3 are defined in the detailed description and claims. The invention is also concerned with the compounds of formula Z: and pharmaceutically acceptable salts and esters thereof, wherein R1-R3 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I and Z as well as pharmaceutical compositions containing such compounds. The compounds of formula I and Z are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.Type: GrantFiled: November 9, 2009Date of Patent: May 29, 2012Assignee: Hoffman-La Roche Inc.Inventors: Fariborz Firooznia, Tai-An Lin, Sung-Sau So, Baoxia Wang, HongYing Yun
-
Publication number: 20120122870Abstract: Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment.Type: ApplicationFiled: May 10, 2010Publication date: May 17, 2012Applicants: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT, APOGEE BIOTECHNOLOGY CORPORATIONInventors: Charles D. Smith, Zhi Zhong, Lynn W. Maines
-
Publication number: 20120115841Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: ApplicationFiled: May 17, 2010Publication date: May 10, 2012Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
-
Publication number: 20120107273Abstract: The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof and an anti-HCV agent and an HCV polymerase inhibitor containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: ApplicationFiled: April 25, 2011Publication date: May 3, 2012Applicant: Japan Tobacco Inc.Inventors: Hiroyuki Abe, Masahiro Tanaka, Kazuyuki Sugimoto, Akira Suma, Masahiro Yokota, Makoto Shiozaki, Kiyosei Ilo, Kazuhito Ueyama, Dai Motoda, Toru Noguchi, Tsuyoshi Adachi, Junichiro Tsuruha, Satoki Doi
-
Publication number: 20120107276Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.Type: ApplicationFiled: December 28, 2011Publication date: May 3, 2012Applicant: Siga Technologies, Inc.Inventors: Dennis E. Hruby, Tove C. Bolken, Dongcheng Dai
-
Publication number: 20120108603Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: December 30, 2011Publication date: May 3, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Hans Louis Jos De Winter, Alexy Borisovich Dyatkin, Marc Gustaal Celine Verdonck, Lieven Meerpoel, Jimmy Arnold Viviane Van heusden
-
PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF SALICYLANILIDES FOR TREATMENT OF HEPATITIS VIRUSES
Publication number: 20120108592Abstract: A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Inventors: J. Edward Semple, Jean-Francois Rossignol -
Publication number: 20120101087Abstract: The present invention relates to, in part, novel bisphenol compounds useful for the recognition, attachment and growth of unwanted biologics on natural and manmade surfaces. Another aspect of the invention relates to combinatorial libraries for producing the same. Another aspect of the invention relates to pharmaceutical formulations comprising the same.Type: ApplicationFiled: December 12, 2008Publication date: April 26, 2012Inventors: Randall S. Alberte, Robert D. Smith
-
Publication number: 20120101080Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.Type: ApplicationFiled: June 25, 2010Publication date: April 26, 2012Applicant: BioVersys AGInventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
-
Publication number: 20120101082Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.Type: ApplicationFiled: December 19, 2011Publication date: April 26, 2012Inventors: ANDRZEJ ROMAN BATT, MARTIN LEE STOCKLEY, MICHAEL BRYAN ROE, CELINE Marguerite Simone HEENEY, ANDREW JOHN BAXTER, PETER HUDSON, RACHEL HANDY
-
Publication number: 20120094973Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetes and ischemia, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.Type: ApplicationFiled: December 21, 2011Publication date: April 19, 2012Applicant: NATIONAL TAIWAN UNIVERSITYInventors: Yueh-Hsiung Kuo, Ming-Jai Su
-
Publication number: 20120095003Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Applicant: XenoPort, Inc.Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
-
Publication number: 20120094964Abstract: The present invention relates to sulfamoyl benzoic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.Type: ApplicationFiled: May 6, 2010Publication date: April 19, 2012Inventors: Tadashi Inoue, Masashi Ohmi, Kiyoshi Kawamura, Kazuo Ando, Yuji Shishido
-
Patent number: 8148422Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: GrantFiled: December 15, 2009Date of Patent: April 3, 2012Assignee: Janssen Pharmaceutica, NVInventors: Mark J. Macielag, James J. McNally
-
Patent number: 8148414Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.Type: GrantFiled: August 19, 2009Date of Patent: April 3, 2012Assignee: XenoPort, Inc.Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
-
Patent number: 8143259Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 are defined herein.Type: GrantFiled: August 11, 2009Date of Patent: March 27, 2012Assignee: Janssen Pharmaceutica, NVInventors: Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Donald W. Ludovici, Jay M. Matthews, Mingde Xia, Xiaoqing Xu, Mark A. Youngman, Bin Zhu
-
Patent number: 8138190Abstract: Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R5, R6, R7, R8, R9, R10, m, Q, X, and Y are set forth in the description.Type: GrantFiled: March 17, 2009Date of Patent: March 20, 2012Assignee: Amgen Inc.Inventors: Jay P. Powers, Daqing Sun, Xuelei Yan
-
Publication number: 20120065193Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Inventors: James Arnold, Andrew Todd Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
-
Publication number: 20120058998Abstract: A method of inhibiting the inflammatory process, the method comprising administering to a mammal suffering from inflammation a therapeutically effective amount of a pharmaceutical composition comprising a compound where: R is a C1-C10 alkylene group, in which, when the number of carbon atoms is at least 2, there are optionally 1 or 2 non-adjacent double bonds; 1 to 3 non-adjacent methylene groups are optionally replaced by NR1 (where R1 is H, alkyl, or acyl), O, or S; and 1 or 2 methylene groups are optionally replaced by a carbonyl or hydroxymethylene group and pharmaceutically acceptable esters or salts of the compounds and wherein the inflammatory process results from a disease selected from the group consisting of ulcerative colitis, endotoxic shock, rheumatoid arthritis, juvenile arthritis, osteoarthritis, psoriasis, Crohn's disease, inflammatory bowel disease, multiple sclerosis, insulin dependent diabetes mellitus, gout, psoriatic arthritis, reactive arthritis, vital or post-viral arthritis and anType: ApplicationFiled: October 7, 2011Publication date: March 8, 2012Inventors: Virginia Sanders, Joel Cummings, Alan D. Snow
-
Publication number: 20120052019Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.Type: ApplicationFiled: August 22, 2011Publication date: March 1, 2012Inventors: Xiangping Qian, Yong-Liang Zhu
-
Publication number: 20120046293Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: October 10, 2011Publication date: February 23, 2012Applicant: Merck Frosst Canada Ltd.Inventors: CHRISTOPHER I. BAYLY, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
-
Publication number: 20120046292Abstract: [Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.Type: ApplicationFiled: April 19, 2010Publication date: February 23, 2012Applicant: ASTELLAS PHARMA INC.Inventors: Tomoaki Kawano, Yasuhiro Yonetoku, Takeshi Hanazawa, Takahiro Nigawara, Hiroki Fukudome, Hiroshi Moritani
-
Patent number: 8119633Abstract: Substituted sulfonamide compounds corresponding to formula I pharmaceutical compositions comprising them, a process for preparing them, and the use of such compounds to treat or inhibit pain and other disorders or disease states.Type: GrantFiled: April 30, 2008Date of Patent: February 21, 2012Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Stefan Oberboersch, Melanie Reich, Bernd Sundermann, Werner Englberger, Timo Struenker, Ruth Jostock, Sabine Hees, Edward Bijsterveld, Fritz Theil, Heinz Graubaum
-
Publication number: 20120040986Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: August 11, 2011Publication date: February 16, 2012Inventors: Bernd RIEDL, Jacques DUMAS, Uday KHIRE, Timothy B. LOWINGER, William J. SCOTT, Roger A. SMITH, Jill E. WOOD, Mary-Katherine MONAHAN, Reina NATERO, Joel RENICK, Robert N. SIBLEY
-
Patent number: 8114880Abstract: The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.Type: GrantFiled: October 22, 2007Date of Patent: February 14, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Joannes Theodorus Maria Linders, Libuse Jaroskova, Marcel Viellevoye, Leo Jacobus Jozef Backx, Didier Jean-Claude Berthelot, Guuske Frederike Busscher
-
Patent number: 8106058Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.Type: GrantFiled: January 31, 2007Date of Patent: January 31, 2012Assignee: Siga Technologies, Inc.Inventors: Dennis E. Hruby, Tove C. Bolken, Dongcheng Dai
-
Publication number: 20120022080Abstract: The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity.Type: ApplicationFiled: March 31, 2010Publication date: January 26, 2012Applicant: RENASCIENCE CO., LTD.Inventors: Toshio Miyata, Kenji Murano, Nagahisa Yamaoka, Akihisa Maeda
-
Publication number: 20120015960Abstract: Provided are compounds for inhibiting Snail-p53 binding and therapeutic agents for cancer including the compounds as an effective component. The Snail-p53 binding inhibitors induce expression of p53 in K-Ras mutant cell lines, thereby enabling effective treatment or prevention of K-Ras mutant cancer, such as, pancreatic cancer, lung cancer, cholangioma, and colon cancer, of which diagnosis or treatment is not easy.Type: ApplicationFiled: November 23, 2009Publication date: January 19, 2012Applicants: The Industry & Academic Cooperation in Chungnam National University, Pusan National University Industry-University Cooperation FoundationInventors: Bum Joon Park, Nam Chul Ha, Sun Hye Lee, Gyu Yong Song, Jee Hyun Lee
-
Publication number: 20120015928Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang