Chalcogen Bonded Directly To Diazine Ring Carbon Patents (Class 544/354)
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Publication number: 20130274265Abstract: Compounds of Formula (I): where R1, R2, R5, a, and b are disclosed herein, and pharmaceutically acceptable derivatives thereof (a “Substituted-Quinoxaline-Type Bridged-Piperidine Compound”), compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound.Type: ApplicationFiled: June 11, 2013Publication date: October 17, 2013Inventors: Kouki FUCHINO, Naoki TSUNO, John W.F. WHITEHEAD, Jiangchao YAO
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Publication number: 20130253186Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 10, 2013Publication date: September 26, 2013Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
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Patent number: 8524714Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, R1, R2, R3, R4, R5, R6 and X have defined meanings.Type: GrantFiled: March 14, 2011Date of Patent: September 3, 2013Assignee: Janssen Pharmaceutica, NVInventors: Dominique Jean-Pierre Mabire, Jerome Emile Georges Guillemont, Jacobus Alphonsus Josephus van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20130197001Abstract: The present invention relates to compounds that are late sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein R1, R2, R3, and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: November 14, 2012Publication date: August 1, 2013Applicant: GILEAD SCIENCES, INC.Inventor: GILEAD SCIENCES, INC.
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Publication number: 20130158003Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: May 26, 2011Publication date: June 20, 2013Applicant: SUNOVION PHARMACEUTICALS INCInventors: John Emmerson Campbell, Michael Charles Hewitt, Philip Jones, Linghong Xie
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Patent number: 8450486Abstract: The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.Type: GrantFiled: October 28, 2011Date of Patent: May 28, 2013Assignee: Janssen Pharmaceutica, NVInventors: Dominique Jean-Pierre Mabire, Jérôme Emile Georges Guillemont, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Patent number: 8445678Abstract: Disclosed are 2-quinoxalinol salen compounds and in particular 2-quinoxalinol salen Schiff-base ligands. The disclosed 2-quinoxalinol salen compounds may be utilized as ligands for forming complexes with cations, and further, the formed complexes may be utilized as catalysts for oxidation reactions. The disclosed 2-quinoxalinol salen compounds also may be conjugated to solid supports and utilized in methods for selective solid-phase extraction or detection of cations.Type: GrantFiled: October 11, 2011Date of Patent: May 21, 2013Assignee: Auburn UniversityInventors: Anne E. V. Gorden, Xianghong Wu
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Publication number: 20130085138Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.Type: ApplicationFiled: September 26, 2012Publication date: April 4, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130065905Abstract: The present invention provides a nitrogen-containing heterocyclic compound or a pharmaceutically acceptable salt thereof having an inhibitory effect on the production of kynurenine, represented by formula (I): (wherein R6 and R7 may be the same or different and each represent a hydrogen atom or the like, R8, R9, R19, and R11 may be the same or different and each represent a hydrogen atom or the like, R1 represents lower alkyl which may be substituted with cycloalkyl, or the like, and R3 represents optionally substituted aryl or an optionally substituted heterocyclic group).Type: ApplicationFiled: May 9, 2011Publication date: March 14, 2013Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Yuichi Fukuda, Toshimi Kanai, Yoshisuke Nakasato, Keisuke Kimpara
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Publication number: 20130053384Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of using these chemical entities, e.g., for treatment of cancer are described.Type: ApplicationFiled: August 24, 2012Publication date: February 28, 2013Applicant: NeuPharma, Inc.Inventors: Yong-Liang Zhu, Xiangping Qian
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Publication number: 20130018052Abstract: The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.Type: ApplicationFiled: July 13, 2012Publication date: January 17, 2013Applicant: SK CHEMICALS CO., LTD.Inventors: Ju Young LEE, Keun-Ho RYU, Jae-Sun KIM, Yong-Hyuk KIM, Dong Chul SHIN, Bong-yong LEE, Sang-hwan KANG, Hyun-Jung LEE, Hoechul JUNG, Young Ah SHIN, Euisun PARK, Jaeseung AHN
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Patent number: 8349826Abstract: The invention relates to compounds of Formula (I) wherein U, V, W, R1, R1b, A and G are as defined in the description, to pharmaceutically acceptable salts of such compounds and to the use of these compounds in the manufacture of a medicament for the prevention or treatment of a bacterial infection.Type: GrantFiled: February 20, 2009Date of Patent: January 8, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, John-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 8329694Abstract: A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.Type: GrantFiled: June 22, 2006Date of Patent: December 11, 2012Assignees: Toyama Chemical Co., Ltd., Taisho Pharmaceutical Co., Ltd.Inventors: Taro Kiyoto, Tadashi Tanaka, Yasuhiro Tsutsui, Junichi Ando, Mai Motono, Yasuko Kawaguchi, Toshiya Noguchi, Yasunobu Ushiki, Fumihito Ushiyama, Hiroki Urabe
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Patent number: 8329698Abstract: The present invention relates to compounds of formula (I) wherein X, Y, Z, R1, R2, R3 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diabetes, metabolic syndrome, obesity, cancer, inflammation.Type: GrantFiled: May 19, 2009Date of Patent: December 11, 2012Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Daniel Cravo, Sophie Hallakou-Bozec, Franck Lepifre
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Patent number: 8314100Abstract: The present invention related to a novel urea derivative for formula (I): which is useful as an anti-cancer agent, its pharmaceutically acceptable acid addition salt or stereoisomer, and to a process for preparing the urea derivative and an anti-cancer composition comprising the same as an active ingredient.Type: GrantFiled: October 18, 2005Date of Patent: November 20, 2012Assignees: Rexahn Pharmaceuticals, Inc., Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Moon-Kook Jeon, Dong-Su Kim, Jae Yang Kong, Gun-Do Kim, Chang-Ho Ahn, Young Bok Lee
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Patent number: 8293769Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.Type: GrantFiled: May 20, 2008Date of Patent: October 23, 2012Assignee: Novartis AGInventors: Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton, Allan S. Wagman, Marion Wiesmann
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Publication number: 20120264760Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: ApplicationFiled: June 6, 2012Publication date: October 18, 2012Applicants: University of Georgia Research Foundation, Inc., Brandeis UniversityInventors: Lizbeth K. Hedstrom, Boris Striepen
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Publication number: 20120245352Abstract: The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use.Type: ApplicationFiled: March 23, 2012Publication date: September 27, 2012Applicant: Southern Methodist UniversityInventors: Edward A. Biehl, Haribabu Ankati, Sukanta Kamila
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Publication number: 20120232194Abstract: Provided is a phthalocyanine compound which is halogen-free and which has a green hue, excellent resistance to organic solvents and acids, and high chroma. Also provided are a metal-free phthalocyanine compound or a metal phthalocyanine compound represented by specified general formula (1-1) or (1-2) and having a N,N?-disubstituted imidazolone structure or piperazinedione structure introduced therein, and a coloring composition including the compound and a synthetic resin. The phthalocyanine compound of the present invention exhibits a clear green color and is halogen-free, and is thus useful as a clear green pigment for coloring materials such as a coating material, plastic, a printing ink, rubber, leather, textile printing, a color filter, a jet ink, a heat transfer ink, etc.Type: ApplicationFiled: August 6, 2010Publication date: September 13, 2012Inventors: Hitoshi Kondou, Yoshiyuki Sano, Yutaka Tachikawa
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Publication number: 20120214990Abstract: A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.Type: ApplicationFiled: May 3, 2012Publication date: August 23, 2012Applicants: TAISHO PHARMACEUTICAL CO., LTD., TOYAMA CHEMICAL CO., LTD.Inventors: Taro KIYOTO, Tadashi Tanaka, Yasuhiro Tsutsui, Junichi Ando, Mai Motono, Yasuko Kawaguchi, Toshiya Noguchi, Yasunobu Ushiki, Fumihito Ushiyama, Hiroki Urabe
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Patent number: 8211890Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy (notably methoxy); R2 represents H or F; each of R3, R4, R5 and R6 represents independently H or D; V represents CH and W represents CH or N, or V represents N and W represents CH; Y represents CH or N; Z represents O, S or CH2; and A represents CH2, CH2CH2 or CD2CD2; and salts of such compounds.Type: GrantFiled: December 11, 2009Date of Patent: July 3, 2012Assignee: Actelion PharmaceuticalsInventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20120165335Abstract: The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer.Type: ApplicationFiled: June 23, 2011Publication date: June 28, 2012Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
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Patent number: 8193199Abstract: Substituted bicyclic heteroaryls having the structures: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid LeukemiType: GrantFiled: March 24, 2008Date of Patent: June 5, 2012Assignee: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20120126184Abstract: The invention relates to a compound comprising a chromophore of formula (II), wherein m is an integer from 1 to 4, preferably 1 or 2; Q2 is a residue of carbon black or of a chromophore which comprises at least one group of the formula (I) or a cis/trans isomer thereof, wherein Z1 and Z2 are each independently of the other O or N—, each C. is independently of all others C.Type: ApplicationFiled: June 15, 2010Publication date: May 24, 2012Applicant: BASF SEInventors: Celine Vairon, Marc Maurer, Ulrich Veith, Sascha Gysin
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Publication number: 20120122837Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: September 23, 2011Publication date: May 17, 2012Inventors: CLIFFORD CHENG, GERALD W. SHIPPS, JR., XIAOHUA HUANG, YING HUANG, NING SHAO, ASHWIN RAO, ANANDAN PALANI, PETER ORTH, JOHANNES H. VOIGT, ROBERT J. HERR, LANA MICHELE ROSSITER, QI ZENG, XIANFENG SUN
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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
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Patent number: 8148376Abstract: The present invention discloses 3,4-dihydroquinoxalin-2(1H)-ones for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.Type: GrantFiled: April 26, 2010Date of Patent: April 3, 2012Assignee: Gilead Sciences, Inc.Inventors: Jeffrey Chisholm, Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrey Glushkov, Natalya Vasilevich, Timur Zilbershtein, Alexey Ivanov
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Publication number: 20120040989Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy; each of U and V represents CH and W represents CH or N, or U represents N, V represents CH and W represents N, or each of U and V represents N and W represents CH; R2 represents hydrogen or fluorine when W represents CH or R2 represents hydrogen when W represents N; A represents O or CH2; Y represents CH or N; Q represents O or S; and n represents 0 or 1; and salts of such compounds.Type: ApplicationFiled: April 8, 2010Publication date: February 16, 2012Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
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Patent number: 8114867Abstract: The invention relates to antibacterial compounds of formula I wherein R1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y1 and Y2 each represent CH, one or two of U, V, W and X represent(s) N and the remaining each represent CH or, in the case of X, may also represent CRa, Ra being halogen, and, in the case of W, may also represent CRb, or each of U, V, W, X, Y1 and Y2 represents CH, or each of U, V, W, X and Y1 represents CH and Y2 represents N, or also one or, provided R1 is hydrogen, two of U, V, W, X, Y1 and Y2 represent(s) CRC and the remaining each represent CH, Rb being alkoxy, alkoxycarbonyl or alkoxyalkoxy and Rc being, each time it occurs, independently represents hydroxy or alkoxy; A-B-D represents a chain of 4 to 6 atoms, which 4 to 6 atoms are selected from carbon, oxygen and nitrogen and may be substituted; E is one of the following groups: in which Z is CH or N and Q is O or S, or E is a phenyl group which is substituted once or twice in the meta and/or para position(s); and to saltsType: GrantFiled: April 10, 2008Date of Patent: February 14, 2012Assignee: Actelion Pharmaceuticals LtdInventors: Markus Gude, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 8110602Abstract: The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.Type: GrantFiled: July 15, 2009Date of Patent: February 7, 2012Assignee: Purdue Pharma L.P.Inventors: Kevin C. Brown, R. Richard Goehring, Yoshiyasu Baba, Naoki Tsuno
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Publication number: 20120028362Abstract: Disclosed are 2-quinoxalinol salen compounds and in particular 2-quinoxalinol salen Schiff-base ligands. The disclosed 2-quinoxalinol salen compounds may be utilized as ligands for forming complexes with cations, and further, the formed complexes may be utilized as catalysts for oxidation reactions. The disclosed 2-quinoxalinol salen compounds also may be conjugated to solid supports and utilized in methods for selective solid-phase extraction or detection of cations.Type: ApplicationFiled: October 11, 2011Publication date: February 2, 2012Applicant: AUBURN UNIVERSITYInventors: Anne E. V. Gorden, Xianghong Wu
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Publication number: 20120028800Abstract: Compounds of Formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: January 25, 2010Publication date: February 2, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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Publication number: 20120021912Abstract: Compounds of Formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: January 18, 2010Publication date: January 26, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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Publication number: 20120021909Abstract: Compounds of Formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: January 25, 2010Publication date: January 26, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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Publication number: 20120021907Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: January 6, 2010Publication date: January 26, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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Publication number: 20110301149Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.Type: ApplicationFiled: October 12, 2009Publication date: December 8, 2011Applicant: VM DISCOVERY INC.Inventor: Jay Jie-Qiang Wu
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Publication number: 20110294793Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.Type: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
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Patent number: 8058269Abstract: There is provided compounds of the formula wherein R6, V, W, X, Y, Q and n are as described. The compounds exhibit activity as anticancer agents.Type: GrantFiled: September 17, 2007Date of Patent: November 15, 2011Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Song Yang, Jing Zhang, Zhuming Zhang
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Publication number: 20110251200Abstract: The invention provides to a family of aryl guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.Type: ApplicationFiled: September 11, 2009Publication date: October 13, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Gary D. Glick, Peter Toogood, Gina Ney
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Publication number: 20110245259Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy (notably methoxy); R2 represents H or F; each of R3, R4, R5 and R6 represents independently H or D; V represents CH and W represents CH or N, or V represents N and W represents CH; Y represents CH or N; Z represents O, S or CH2; and A represents CH2, CH2CH2 or CD2CD2; and salts of such compounds.Type: ApplicationFiled: December 11, 2009Publication date: October 6, 2011Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110230491Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, R1, R2, R3, R4 and X have defined meanings.Type: ApplicationFiled: December 17, 2010Publication date: September 22, 2011Inventors: Dominique Jean-Pierre Mabire, Jerome Emile Georges Guillemont, Jacobus Alphonsus Josephus van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20110207198Abstract: The present invention relates to agents that find use in the treatment, management, and/or study of cancer. In particular, the present invention relates to agents (e.g., small molecules, nucleic acids) that affect MMSET expression or activity.Type: ApplicationFiled: February 11, 2011Publication date: August 25, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Arul M. Chinnaiyan, Sooryanaryana Lnu, Qi Cao, Irfan Asangani
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Publication number: 20110190262Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.Type: ApplicationFiled: November 14, 2008Publication date: August 4, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
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Publication number: 20110178090Abstract: Compounds of Formula (I): where R1, R2, R5, a, and b are disclosed herein, and pharmaceutically acceptable derivatives thereof (a “Substituted-Quinoxaline-Type Bridged-Piperidine Compound”), compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound.Type: ApplicationFiled: January 20, 2011Publication date: July 21, 2011Inventors: Kouki FUCHINO, Naoki Tsuno, John W.F. Whitehead, Jiangchao Yao
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Publication number: 20110166151Abstract: The object aims to find a novel pharmacological activity of a novel 1,2,3,4-tetrahydroquinoxaline derivative which contains, as a substituent, a phenyl group having a sulfonic acid ester structure introduced therein. A compound represented by general formula (1) or a salt thereof is useful as a glucocorticoid receptor agonist, particularly as a therapeutic agent for diseases against which a glucocorticoid receptor agonist (e.g., a steroid) is believed to be effective, such as inflammatory bone/joint diseases, inflammatory ophthalmic diseases (inflammatory ophthalmic diseases in the anterior or posterior segment of an eye).Type: ApplicationFiled: September 11, 2009Publication date: July 7, 2011Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Masatomo Kato, Miwa Takai, Takahiro Matsuyama, Tatsuji Kurose, Yumi Hagiwara, Kenji Oki, Mamoru Matsuda, Toshiyuki Mori
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Publication number: 20110145970Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.Type: ApplicationFiled: August 26, 2009Publication date: June 23, 2011Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Michael Krohn, Holger Zinke
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Publication number: 20110143939Abstract: Compounds of the formula (I) and salts thereof in which X, R1, R2, Y and n have the meanings indicated in the description, are suitable for use as safeners for crop plants or useful plants against the phytotoxic actions of agrochemicals such as pesticides in these plants.Type: ApplicationFiled: February 21, 2011Publication date: June 16, 2011Applicant: Bayer CropScience AGInventors: Wolfgang Schaper, Lothar Willms, Christopher Rosinger, Erwin Hacker, Eckhard Rose, Dirk Schmutzler
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Publication number: 20110136800Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: ApplicationFiled: November 5, 2010Publication date: June 9, 2011Inventors: Matthias Eckhardt, Stefan Peters, Herbert Nar, Frank Himmelsbach, Linghang Zhuang
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Publication number: 20110136788Abstract: [Problem] The present invention aims to provide an agent for the prophylaxis or treatment of irritable bowel syndrome. [Solving Means] An agent for the prophylaxis or treatment of irritable bowel syndrome, containing a compound having a TGR5 receptor agonist activity, a fused ring compound represented by the formula wherein ring A is an optionally substituted aromatic ring, and ring B? is a 5- to 9-membered ring having one or more substituents, or a salt thereof as an active ingredient.Type: ApplicationFiled: August 6, 2009Publication date: June 9, 2011Inventor: Minoru Maruyama
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Publication number: 20110130404Abstract: The present invention relates to compounds of formula (I) wherein X, Y, Z, R1, R2, R3 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diabetes, metabolic syndrome, obesity, cancer, inflammation.Type: ApplicationFiled: May 19, 2009Publication date: June 2, 2011Applicant: Merck Patent GmbHInventors: Daniel Cravo, Sophie Hallakou-Bozec, Franck Lepifre