Double Bonded Divalent Chalcogen Containing Patents (Class 544/131)
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Publication number: 20120101064Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.Type: ApplicationFiled: April 30, 2010Publication date: April 26, 2012Applicants: Astex Therapeutics Limited, Novartis AGInventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Grialdes, Michael Joseph Luzzio, Lawrence Blas Perez
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Publication number: 20120101100Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: February 25, 2009Publication date: April 26, 2012Inventors: Shanta Bist, Brian Dangel, Brian Sherer
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Patent number: 8163728Abstract: The present invention is concerned with isoxazole-pyrazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutics. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: April 28, 2010Date of Patent: April 24, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20120094980Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Inventors: Janet L. Gunzner, Daniel P. Sutherlin, Mark S. Stanley, Liang Bao, Georgette Castanedo, Rebecca Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina, Michael F.T. Koehler
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Publication number: 20120094996Abstract: There is provided compounds of formula (I): wherein R1, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K) is desired and/or required, and particularly in the treatment of cancer.Type: ApplicationFiled: April 1, 2010Publication date: April 19, 2012Applicant: Centro Nacional de Investigaciones Oncologicas (CNIO)Inventors: Joaquin Pastor Fernández, Guido Kurz, Sonia Martinez Gonzalez
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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
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Publication number: 20120077794Abstract: The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.Type: ApplicationFiled: June 2, 2010Publication date: March 29, 2012Applicant: GLAXSMITHKLINE LLCInventors: Siegfried Benjamin Christensen, IV, Donghui Qin, Shenglin Chen, Xing Huang, Di Li, Fei Li, Xiaojuan Lin, Shi Lu, Maoyun Lv, Chengde Wu, Weiliang Xu, Gang Yan, Jianxing Yuan, Weina Zhang, Zhiliu Zhang
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Publication number: 20120077807Abstract: Disclosed are 6-(morpholinoalkyl)-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications.Type: ApplicationFiled: June 24, 2011Publication date: March 29, 2012Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-sen Lai, Daniel P. O'Connell, Wengen Wu, Christopher P. Kiritsy
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Publication number: 20120077801Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.Type: ApplicationFiled: August 3, 2011Publication date: March 29, 2012Inventors: Roger Victor Bonnert, Rhona Jane Cox, Simon De Sousa, Mark Dickinson, Simon Fraser Hunt, Austen Pimm, Hitesh Jayantilal Sanganee, Frank Burkamp, Premji Meghani
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Publication number: 20120077806Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.Type: ApplicationFiled: September 23, 2011Publication date: March 29, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey W. Perry, Roderick J. Sorenson, Mary X. O'Riordan, Yafei Jin
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Publication number: 20120077808Abstract: Disclosed are heterocyclylalkyl-substituted and heteroaralkyl-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications.Type: ApplicationFiled: June 24, 2011Publication date: March 29, 2012Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-sen Lai, Daniel P. O'Connell, Wengen Wu, Christopher P. Kiritsy
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Patent number: 8143246Abstract: The invention relates to 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, (C1-3)alkyloxy, (C1-3)alkyloxycarbonyl, halogen or CN), (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each cycloalkyl ring optionally comprising a heteroatom selected from O and S; R2 and R3 are independently H or (C1-3)alkyl; or R2 and R3 form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R4 is H or 1 to 3 F substituents; R5 is H or 1 to 4 F substituents; R6 and R7 are independently H or F; X represents R8, OR8, NR8R9, R8 is (C5-7)cycloalkyl optionally comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; R10 represents 1-3 substituents independently selected from H, (C1-3)alkyl, halogen, oxo, CN and CF3; Y is CF2, O, S, SO or SO2; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said 1-(4Type: GrantFiled: February 15, 2010Date of Patent: March 27, 2012Assignee: MSD OSS B.V.Inventors: Marcelis van der Stelt, Joseph Maria Gerardus Barbara Cals, Johannes Petrus Gerardus Klomp
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Publication number: 20120071473Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.Type: ApplicationFiled: September 23, 2011Publication date: March 22, 2012Inventors: Vlad Edward Gregor, Nelson Levy
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Publication number: 20120065064Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: December 12, 2009Publication date: March 15, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: John Benjamin Taylor, Jeffrey Steven Wailes, Stephane André Marie Jeanmart, Mangala Govenkar
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Publication number: 20120065191Abstract: The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.Type: ApplicationFiled: December 23, 2009Publication date: March 15, 2012Applicant: BIAL - PORTELA & Cª, S.A.Inventors: Laszlo Erno Kiss, David Alexander Learmonth, Carla Patrícia da Costa Pereira Rosa, Rita Gusmão de Noronha, Pedro Nuno Leal Palma, Patrício Manuel Vieira Araújo Soares da Silva, Alexander Beliaev
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Publication number: 20120059004Abstract: 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: February 16, 2011Publication date: March 8, 2012Applicant: CANTHERA THERAPEUTICS, INC.Inventors: PETER ELLIOTT, ANNA MANDINOVA, MICHAEL ANDREW FOLEY, ROBERT GOULD, SAM LEE
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Publication number: 20120058988Abstract: The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.Type: ApplicationFiled: December 17, 2009Publication date: March 8, 2012Inventors: Ashok Vinayak Purandare, Douglas G. Batt, Qingjie Liu, Harold Mastalerz, Kurt Zimmermann
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Publication number: 20120053166Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: March 5, 2010Publication date: March 1, 2012Inventors: Julie Nicole Hamblin, Zoe Alicia Harrison, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Christopher James Lunniss, Nigel James Parr
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Patent number: 8124605Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.Type: GrantFiled: July 7, 2008Date of Patent: February 28, 2012Assignee: Kinex Pharmaceuticals, LLCInventor: David G. Hangauer, Jr.
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Publication number: 20120046286Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: April 28, 2010Publication date: February 23, 2012Inventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr
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Publication number: 20120046285Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: ApplicationFiled: August 17, 2011Publication date: February 23, 2012Applicants: ASTELLAS PHARMA INC., ALCON RESEARCH, LTD.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
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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
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Publication number: 20120035174Abstract: Salts of N-[6-(cis-2,6-dimethylmorpholin-4-yl)pyridine-3-yl]-2-methyl-4?-(trifluoromethoxy)[1,1?-biphenyl]-3-carboxamide are prepared and characterized.Type: ApplicationFiled: October 13, 2011Publication date: February 9, 2012Applicant: NOVARTIS AGInventors: Joginder Singh Bajwa, Marilyn De La Cruz, Stephanie Kay Dodd, Liladhar Murlidhar Waykole, Raeann Wu
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Publication number: 20120035163Abstract: The present invention provides an agent for the prophylaxis or treatment of diabetes, obesity and the like, a glucokinase activator, containing a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.Type: ApplicationFiled: December 28, 2009Publication date: February 9, 2012Inventors: Tsuneo Yasuma, Nobuyuki Takakura, Yasufumi Miyamoto
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Publication number: 20120035157Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R4, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Applicant: AstraZeneca ABInventors: Marjana Andersson, Peter Hansen, Hans Lönn, Antonios Nikitidis, Petter Sjölin
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Publication number: 20120035175Abstract: The present invention relates to a salt selected from the group comprising the N-methyl-D-glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2-hydroxyethyl)morpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.Type: ApplicationFiled: July 1, 2011Publication date: February 9, 2012Applicant: 4SC AGInventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT
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Publication number: 20120022255Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
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Publication number: 20120014997Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: September 26, 2011Publication date: January 19, 2012Inventors: Solomon Ungashe, J.J. Wright, Andrew Pennell, Zheng Wei, Anita Melikan
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Publication number: 20120015942Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: July 18, 2011Publication date: January 19, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
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Patent number: 8097624Abstract: The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2R5N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups.Type: GrantFiled: May 9, 2008Date of Patent: January 17, 2012Assignee: Apotex Inc.Inventors: Tim Fat Tam, Michael Spino, Wanren Li, Yingsheng Wang, Yanqing Zhao, Birenkumar Hasmukhbhai Shah
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Publication number: 20120010181Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.Type: ApplicationFiled: November 9, 2009Publication date: January 12, 2012Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K.C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
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Publication number: 20120010172Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.Type: ApplicationFiled: August 31, 2009Publication date: January 12, 2012Applicant: McDERMOTT WILL & EMERY LLPInventors: Mette Knak Christensen, Fredrik Bjorkling
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Publication number: 20120010185Abstract: The present invention relates to compounds of general formula I wherein the groups and radicals B, k, L, U, V, W, X, Y, Z, R1, R2, have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one compound according to the invention. By virtue of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.Type: ApplicationFiled: September 22, 2011Publication date: January 12, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk STENKAMP, Stephan Georg MUELLER, Gerald Juergen ROTH, Joerg KLEY, Klaus RUDOLF, Armin HECKEL, Marcus SCHINDLER, Ralf LOTZ, Thorsten LEHMANN-LINTZ
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Publication number: 20120010190Abstract: This invention relates to novel 1-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R10 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may be used as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: July 12, 2011Publication date: January 12, 2012Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
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Publication number: 20120004227Abstract: The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)?(C(?O)N(R1), C(?O)N(R2)), (C(?O)N(R1), imidazole-1,3-diyl), (N(R1), C(?O)N(R2)), (O, C(?O)N(R2)), (C(R3)(R4), N(R2)) or (a single bond, C(?O)N(R2)); R1, R2 and R3 are independently hydrogen or substituted or unsubstituted alkyl; R5 is substituted or unsubstituted aryl or heterocyclyl; R6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.Type: ApplicationFiled: March 5, 2010Publication date: January 5, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Hiroshi Yoshida, Keisuke Tonogaki, Masahiro Sakagami, Kenji Takaya
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Publication number: 20120004228Abstract: There is provided compounds of formula I, wherein Y, ring A, Da, Db, D2, D3, L1, Y1, L2, Y2, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.Type: ApplicationFiled: March 12, 2010Publication date: January 5, 2012Applicant: BIOLIPOX ABInventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics
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Publication number: 20110319411Abstract: 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: December 8, 2009Publication date: December 29, 2011Applicant: Sirtis Pharmaceuticals, Inc.Inventors: Chi B. Vu, Lauren Mcpherson, Pui Yee Ng, Charles Blum
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Patent number: 8084615Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: GrantFiled: October 30, 2007Date of Patent: December 27, 2011Assignees: University of Washington, Novartis Vaccines and Diagnostics, Inc.Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
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Publication number: 20110312939Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 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 in such a treatment.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20110312961Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).Type: ApplicationFiled: October 15, 2009Publication date: December 22, 2011Inventors: Christopher D. Cox, Paul J. Coleman, Broc Flores, John D. Schreier
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Publication number: 20110312935Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.Type: ApplicationFiled: September 25, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Henning Priepke, Dirk Stenkamp
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Publication number: 20110312962Abstract: The present application discloses novel 2-morpholino-3-amido-pyhcline derivatives and their use as modulators of the voltage gated Kv7 (KCNQ) potassium ion channels in the treatment of pain, neurodegenerative disorders, urinary incontinence, etc. . . . . In other aspects the application discloses the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: November 26, 2009Publication date: December 22, 2011Applicant: NEUROSEARCH A/SInventors: William Dalby Brown, Carsten Jessen, Dorte Strøbaek
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Publication number: 20110312963Abstract: The present disclosure relates to compounds of formula (I): which are inhibitors of p38 mitogen-activated protein kinase enzymes, particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPDType: ApplicationFiled: December 11, 2009Publication date: December 22, 2011Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Kevin Joly, Catherine Elisabeth Charron
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Publication number: 20110306611Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: August 3, 2009Publication date: December 15, 2011Applicant: Paratek Pharmaceuticals, Inc.Inventors: Michael N. Alekshun, Victor Amoo, Oak K. Kim, Atul K. Verma
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Publication number: 20110306614Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Publication number: 20110306597Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the treatment of allergic and respiratory conditions.Type: ApplicationFiled: June 12, 2009Publication date: December 15, 2011Inventors: James Michael Crawforth, Paul Alan Glossop, Bruce Cameron Hamper, Wei Huang, Bradley Elwood Neal, Simon John Mantell, Kirk Olson, Atli Thorarensen, Steve Ronald Turner
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Publication number: 20110306590Abstract: Aryl- and heteroaryl-nitrogen heterocyclic 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 9, 2011Publication date: December 15, 2011Inventors: Jennifer R. Allen, Kristin L. Andrews, Michael J. Frohn, Paul E. Harrington, Alexander J. Pickrell, Robert M. Rzasa
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Patent number: 8076332Abstract: The present invention relates to a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of a pharmacological effect of the derivative. A compound represented by the general formula (1) or a salt thereof has an effect of cellular morphological change on trabecular meshwork cells and is effective in the prevention and/or treatment of a disease considered to be related to intraocular pressure. In the formula, R1 and R2 represent a hydrogen atom, a lower alkyl group, or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, or the like; R4 and R5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group, or the like; l and m represent 0, 1, 2, or the like.Type: GrantFiled: December 26, 2007Date of Patent: December 13, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Publication number: 20110301140Abstract: The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: August 4, 2011Publication date: December 8, 2011Inventors: Jeffrey M. Bergman, Paul J. Coleman, Mark E. Fraley, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker, Justin T. Steen
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Publication number: 20110294812Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, which are inhibitors of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.Type: ApplicationFiled: December 11, 2009Publication date: December 1, 2011Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Simon Christopher Hirst, David Michel Adrien Taddei, Catherine Elisabeth Charron