Double Bonded Divalent Chalcogen Containing Patents (Class 544/131)
-
Publication number: 20120214808Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Prosidion LimitedInventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Simon Andrew Swain, Philippe Wong-Kai-In
-
Publication number: 20120214735Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Advinus Therapeutics LimitedInventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
-
Publication number: 20120214991Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.Type: ApplicationFiled: October 21, 2009Publication date: August 23, 2012Applicant: Korea Research Institute of Chemical TechnologyInventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
-
Publication number: 20120208811Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.Type: ApplicationFiled: August 5, 2010Publication date: August 16, 2012Applicants: F. HOFFMANN-LA ROCHE AG, CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
-
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: 20120202795Abstract: The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Philip M. WEINTRAUB, Paul R. EASTWOOD, Shujaath MEHDI, David W. STEFANY, Kwon Yon MUSICK, Neil MOORCROFT, Sungtaek LIM, John Z. JIANG, Hartmut RUTTEN, Stefan PEUKERT, Uwe SCHWAHN
-
Publication number: 20120202808Abstract: A compound of formula (1): wherein R1 and R2 represent hydrogen, lower alkyl, lower alkenyl, lower alkynyl or R3 represents hydroxyl, lower alkoxy, lower cycloalkyloxy, aryloxy, carboxy, lower alkoxycarbonyl, or NRaRb of the formula R4 and R5 represent halogen, lower alkyl, hydroxyl, or lower alkoxy; R6 represents halogen, lower alkyl, aryl, heterocyclic, hydroxy, lower alkoxy, mercapto, lower alkylthio, lower alkylcarbonyl, amino, nitro or cyano; R7 represents lower alkyl, hydroxyl or lower alkoxy; Ra and Rb represent hydrogen or lower alkyl; ring A represents a cyclic hydrocarbon or a heterocyclic ring; ring B represents a heterocyclic ring; X represents lower alkylene; Z represents a single bond or lower alkylene; Y represents lower alkylene and W1-W2 represents CH—CH, or represents a single bond and W1-W2 represents N—CH, CH—N or CH—CH; and 1, m, n and o represent 0, 1, 2, or 3.Type: ApplicationFiled: April 17, 2012Publication date: August 9, 2012Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
-
Publication number: 20120202817Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban
-
Patent number: 8236799Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention relates to compounds of the formula I: or a pharmaceutically acceptable salt thereof. The compounds of the invention are useful for methods of protecting against or treating hearing loss, osteoporosis, cell proliferative disorders, obesity, diabetes, eye disease, stroke, atherosclerosis, neuropathic pain or hepatitis B.Type: GrantFiled: June 3, 2011Date of Patent: August 7, 2012Assignee: Kinex Pharmaceuticals, LLCInventor: David G. Hangauer, Jr.
-
Publication number: 20120196849Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.Type: ApplicationFiled: April 10, 2012Publication date: August 2, 2012Applicant: IRM LLCInventors: Wenqi Gao, Jiqing Jiang, Yongqin Wan, Dai Cheng, Dong Han, Xu Wu, Shifeng Pan
-
Publication number: 20120196858Abstract: The invention provides a method of promoting apoptosis in tumor cells, which can result in inhibiting tumor growth, or inhibiting tumor metastasis, or promoting tumor apoptosis, or any combination thereof, by administration of an effective amount of a focal adhesion kinase (FAK) inhibitor. The inhibitor is a small molecule organic compound. Accordingly, the focal adhesion kinase inhibitor can be used in the treatment of tumors, such as malignant cancer. For example, administration of effective amounts of the FAK inhibitor PND-1186 has been found to inhibit tumor cells in murine models for breast and ovarian cancer.Type: ApplicationFiled: August 12, 2010Publication date: August 2, 2012Applicant: Poniard Pharmaceuticals ,Inc.Inventor: David Schlaepfer
-
Patent number: 8232271Abstract: Compounds having the formula I wherein R1, R2, R3a, R3b, R3c, R4, R5 and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: GrantFiled: October 30, 2009Date of Patent: July 31, 2012Assignee: Roche Palo Alto LLCInventors: Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Francisco Xavier Talamas
-
Publication number: 20120190673Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.Type: ApplicationFiled: December 19, 2011Publication date: July 26, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio BERDINI, Maria Grazia CARR, Adrian Liam GILL, Steven HOWARD, Eva Figueroa NAVARRO, Gary TREWARTHA, David Charles REES, Mladen VINKOVIC, Paul Graham WYATT
-
Publication number: 20120184549Abstract: This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, Io1, Io2, Io5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.Type: ApplicationFiled: January 11, 2012Publication date: July 19, 2012Inventor: Frank Himmelsbach
-
Publication number: 20120184553Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.Type: ApplicationFiled: September 27, 2010Publication date: July 19, 2012Inventors: Paula Louise Nichols, Andrew John Eatherton, Paul Bamborough, Karamjit Singh Jandu, Oliver James Philps, Daniele Andreotti
-
Publication number: 20120184538Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: February 10, 2012Publication date: July 19, 2012Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
-
Publication number: 20120178734Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: ApplicationFiled: May 28, 2010Publication date: July 12, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Jennifer A. Kowalski, Matt Aaron Tschantz
-
Publication number: 20120177634Abstract: This disclosure concerns novel demethylpenclomedine analogs. Also disclosed are pharmaceutical compositions and methods for using such compositions to treat hyperproliferative disorders.Type: ApplicationFiled: February 22, 2012Publication date: July 12, 2012Inventor: Lee Roy Morgan
-
Publication number: 20120172372Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: December 30, 2011Publication date: July 5, 2012Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
-
Publication number: 20120172359Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.Type: ApplicationFiled: March 7, 2012Publication date: July 5, 2012Applicant: NOVARTIS AGInventors: Sangamesh BADIGER, Murali CHEBROLU, Mathias FREDERIKSEN, Philipp HOLZER, Konstanze HURTH, Rainer Martin LUEOEND, Lei LI, Hui LIU, Rainer MACHAUER, Henrik MOEBITZ, Ulf NEUMANN, Rita RAMOS, Heinrich RUEEGER, Michael SCHAEFER, Siem Jacob VEENSTRA, Marina TINTELNOT-BLOMLEY, Markus VOEGTLE, Xin XIONG
-
Patent number: 8207164Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.Type: GrantFiled: July 23, 2010Date of Patent: June 26, 2012Assignee: Novartis AGInventors: Philipp Holzer, Rainer Machauer, Marina Tintelnot-Blomley
-
Publication number: 20120157433Abstract: The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor.Type: ApplicationFiled: September 2, 2010Publication date: June 21, 2012Inventors: Keith B. Pfister, Martin Sendzik
-
Publication number: 20120157455Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.Type: ApplicationFiled: June 17, 2011Publication date: June 21, 2012Applicant: CANTHERA THERAPEUTICS, INC.Inventors: Michael Andrew Foley, Robert Gould, Peter Elliott, Anna Mandinova, Sam Lee
-
Publication number: 20120157434Abstract: The present invention provides heterocyclic compounds of the following formula I: or pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof useful as antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: ApplicationFiled: February 29, 2008Publication date: June 21, 2012Inventors: Mikhail Fedorovich Gordeev, Zhengyu Yuan, Jinqian Liu
-
Publication number: 20120149705Abstract: N-Thio-anthranilamid compounds of formula (I) wherein A is a group selected from A1 and A2 wherein the variables and the indices are as defined per the description, processes for preparing the compounds I, pesticidal compositions comprising compounds I, use of compounds I for the control of insects, acarids or nematodes, and methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites by use of compounds of formula I.Type: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Applicant: BASF SEInventors: Thomas SCHMIDT, Michael PUHL, Joachim DICKHAUT, Henricus Maria Martinus BASTIAANS, Michael RACK, Deborah L. CULBERTSON, Douglas D. Anspaugh, Franz-Josef BRAUN, Toni BUCCI, Henry Van Tuyl COTTER, David G. KUHN, Hassan OLOUMI-SADEGHI
-
Publication number: 20120149675Abstract: The present invention is concerned with novel 1,2,3-triazole-imidazole compounds of formula (I) wherein X, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention provides a method for the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutic agents.Type: ApplicationFiled: December 2, 2011Publication date: June 14, 2012Inventor: Andrew Thomas
-
Patent number: 8198271Abstract: A compound having the following formula (1) or a salt thereof: wherein R1 and R2 represent hydrogen, a lower alkyl, a lower alkenyl, a lower alkynyl or a group having the following formula (2): (R6)n—{circle around (A)}—Z—??(2), R3 represents hydroxy, a lower alkoxy, a lower cycloalkyloxy, an aryloxy, carboxy, a lower alkoxycarbonyl, or —NRaRb having the following formula (3): (R7)o—{circle around (B)}—??(3), R4 and R5 represent halogen, a lower alkyl, hydroxy, or a lower alkoxy; R6 represents halogen, a lower alkyl, an aryl group, a heterocyclic, a hydroxy, a lower alkoxy, mercapto, a lower alkylthio, a lower alkylcarbonyl, amino, nitro or cyano; R7 represents a lower alkyl, hydroxy or a lower alkoxy; Ra and Rb represent hydrogen or a lower alkyl; the ring A represents a cyclic hydrocarbon or a heterocyclic ring; the ring B represents a heterocyclic ring having one or more heteroatoms selected from the group consisting of nitrogen and oxygen; X represents a lower alkylene; Y represents a lower alkyleType: GrantFiled: May 25, 2009Date of Patent: June 12, 2012Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
-
Publication number: 20120142691Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: ApplicationFiled: August 4, 2010Publication date: June 7, 2012Inventors: Hirohide Noguchi, Tadashi Inoue, Mikio Morita, Yoshimasa Arano
-
Publication number: 20120142686Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:Type: ApplicationFiled: October 20, 2011Publication date: June 7, 2012Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
-
Publication number: 20120142688Abstract: A 1-(substituted aryl)-5-trifluoromethyl-2-(1H)pyridone compounds and pharmaceutical acceptable salts, preparation methods and uses for preparing the drugs for treating fibrosis thereof.Type: ApplicationFiled: May 24, 2010Publication date: June 7, 2012Applicant: CENTRAL SOUTH UNIVERSITYInventors: Gaoyun Hu, Lijian Tao, Jun Chen
-
Publication number: 20120142671Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.Type: ApplicationFiled: November 1, 2011Publication date: June 7, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
-
Patent number: 8188079Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.Type: GrantFiled: August 9, 2010Date of Patent: May 29, 2012Assignees: Hoffman-La Roche Inc., Siena Biotech S.p.A.Inventors: Matteo Andreini, David Banner, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Massimiliano Travagli, Michela Valacchi, Thomas Woltering, Wolfgang Wostl
-
Publication number: 20120129859Abstract: 1-(substituted benzyl)-5-trifluoromethyl-2(1H)pyridone compounds and their pharmaceutical acceptable salts are disclosed. The preparation methods of the compounds and their salts and the use of the same for preparing the medicaments for treating fibrosis are also disclosed. New pyridine compounds and their salts are obtained from trifluoromethyl pyridone as starting material.Type: ApplicationFiled: May 24, 2010Publication date: May 24, 2012Inventors: Gaoyun Hu, Lijian Tao, Jun Chen
-
Publication number: 20120129843Abstract: This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables Rz, Q, J, R1, R3, R5, and R6 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Yan ZHANG, Brett Andrew Tounge, Aihua Wang, Michael Hawkins, Kristi Anne Leonard, Joseph Kent Barbay, Umar S.M. Maharoof
-
Publication number: 20120129844Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: January 26, 2012Publication date: May 24, 2012Inventors: David Buttar, Kevin Michael Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
-
Publication number: 20120122854Abstract: The invention is concerned with novel carbocyclyl fused cyclic amines of formula (I) wherein A, X1 to X3, Y1 to Y3, Z, R1, R2, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.Type: ApplicationFiled: January 11, 2012Publication date: May 17, 2012Inventors: Markus Boehringer, Katrin Groebke Zbinden, Wolfgang Haap, Narendra Panday, Fabienne Ricklin, Martin Stahl, Petra Schmitz
-
Publication number: 20120122839Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.Type: ApplicationFiled: January 17, 2012Publication date: May 17, 2012Applicant: Priaxon AGInventors: Christoph BURDACK, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
-
Publication number: 20120115844Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, Z, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.Type: ApplicationFiled: November 2, 2011Publication date: May 10, 2012Inventors: Maria-Clemencia Hernandez, Matthew C. Lucas, Andrew Thomas
-
Publication number: 20120116075Abstract: An acrylamide derivative represented by formula (I), pharmaceutically acceptable salts and solvates thereof, as well as a medicament containing said acrylamide derivative or its pharmaceutically acceptable salts as the active ingredient, which can be used to treat disorders associated with tyrosine kinase especially Bcr-Abl, including proliferative disorders such as cancers, and inflammation and the like are provided.Type: ApplicationFiled: April 27, 2010Publication date: May 10, 2012Applicants: BEIJING JIASHILIANBO PHARM SCI & TECH CO. LTD, BEIJING SHIQIAO BIOPHARM CO. LTDInventor: Shuping Sun
-
Publication number: 20120115867Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, 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 or C1-C6 alkyl, R3, R4 are, independently, hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl or C1-C6 haloalkoxy, and R5 and R6 are as further defined in the specification, and pharmaceutical acceptable salts thereof.Type: ApplicationFiled: May 4, 2011Publication date: May 10, 2012Applicant: DAC S.R.L.Inventors: Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Mario Varasi, Ciro Mercurio
-
Publication number: 20120114765Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.Type: ApplicationFiled: March 31, 2010Publication date: May 10, 2012Inventors: Ping Cao, Joseph Weinstock, William D. Kingsbury, Craig A. Leach, Suresh Kumar Kizhakkethil-George, Benjamin Nicholson
-
Publication number: 20120108583Abstract: The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Applicant: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant A. Gharat, Nagarajan Muthukaman, Lakshminarayana Narayana, Neelima Khairatkar-Joshi, Vidya G. Kattige
-
Publication number: 20120108572Abstract: Heteroaryloxy-substituted benzoic acid amides of general formula I wherein the groups R1 to R7 as well as X and Y are defined according to claim 1, including the tautomers, the stereoisomers, the mixtures and the salts thereof. The compounds according to the invention are suitable for the treatment of respiratory complaints, particularly COPD and asthma.Type: ApplicationFiled: August 26, 2009Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger Wagner, Elke Langkopf, Frank Himmelsbach, Rolf Goeggel, Birgit Jung
-
Publication number: 20120108585Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: August 11, 2009Publication date: May 3, 2012Applicant: Sirtris Pharmaceuticals, Inc.Inventor: Chi B. Vu
-
Publication number: 20120108567Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Darryl McCONNELL, Maria IMPAGNATIELLO, Dirk KESSLER, Oliver KRAEMER, Siegfried SCHNEIDER, Lars VAN DER VEEN, Ulrike WEYER-CZERNILOFSKY, Tobias WUNBERG
-
Publication number: 20120101078Abstract: Disclosed are a series of neuropeptide Y Y5 receptor ligands, and as such are useful to treat disorders related to mood, stress, ADHD, cognition, stress and dementia.Type: ApplicationFiled: March 19, 2010Publication date: April 26, 2012Applicant: H. Lundbrck A/SInventors: Bin Chen, James Ford Burns, Dario Doller
-
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: 20120101079Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: October 19, 2011Publication date: April 26, 2012Applicant: Grunenthal GmbHInventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
-
Publication number: 20120101091Abstract: The present application provides compounds of formula I wherein X, Y, R2, n, R5 and R6 are defined herein, useful as inhibitors of the hepatitis C virus NS5B polymerase The present application also provides pharmaceutical compositions containing said compounds, methods of using said compounds as pharmaceuticals alone or with other antiviral agent in the treatment of a hepatitis C viral infection in a mammal having or at risk of having the infection.Type: ApplicationFiled: October 1, 2009Publication date: April 26, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pierre Beaulieu, Pierre Bonneau, René Coulombe, Pasquale Forgione, James Gillard, Araz Jakalian, Jean Rancourt
-
Publication number: 20120101097Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.Type: ApplicationFiled: March 10, 2011Publication date: April 26, 2012Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell