Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
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Publication number: 20120149710Abstract: Bacterial infections, including Methicillin resistant Staphylococcus aureus (MRSA) infections are a major health problem that has created a pressing need for new antibiotics. Pyridazinone, rhodanine, and pyrazolethione compounds effective inhibit the enzymatic activity of sortase A (srtA) found in gram positive bacteria are disclosed. A structure activity relationship (SAR) analysis led to the identification of several pyridazinone and pyrazolethione analogs that inhibit SrtA with IC50 values in the sub-micromolar range. Compounds that inhibit the S. aureus SrtA sortase may function as potent anti-infective agents as this enzyme attaches virulence factors to the cell wall. Many of these molecules also inhibit the sortase enzyme from B. anthracis suggesting that they may be generalized sortase inhibitors. The novel compounds, compositions, uses, formulations, medicaments, articles of manufacture provide improved materials, uses, and treatments useful in combating infectious disorders.Type: ApplicationFiled: August 23, 2010Publication date: June 14, 2012Inventors: Michael E. Jung, Robert T. Clubb, Sung Wook Yi, Nutee Suree, Jeremy Justin Clemens
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Publication number: 20120129779Abstract: The present invention relates to novel cytotoxic molecules and their use for the treatment of cancer and other diseases.Type: ApplicationFiled: May 9, 2008Publication date: May 24, 2012Applicant: R&D-BIOPHARMACEUTICALS GMBHInventor: Wolfgang Richter
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Publication number: 20120128742Abstract: The present disclosure relates to crystalline form of (S)-N-((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluoro-benzoyl)-thiazol-2-yl]-pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide, salts and hydrates thereof. This disclosure also relates to solid oral formulation of (S)-N-((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluoro-benzoyl)-thiazol-2-yl]-pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide, pharmaceutically acceptable salts, solvates (including hydrates) thereof, as well as methods of treatment using the same.Type: ApplicationFiled: August 11, 2010Publication date: May 24, 2012Inventors: Jeewan Thakur, Dong Yang, Lili Feng
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Patent number: 8178522Abstract: The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. 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: May 15, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20120115868Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The 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 pharmaceuticals.Type: ApplicationFiled: November 2, 2011Publication date: May 10, 2012Inventors: Stephen Deems Gabriel, Andrew Thomas
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Patent number: 8168631Abstract: Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: February 3, 2009Date of Patent: May 1, 2012Assignee: Allergan, Inc.Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Rong Yang, Cédric Chauvignac
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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
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Patent number: 8163746Abstract: Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.Type: GrantFiled: April 19, 2007Date of Patent: April 24, 2012Assignee: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Matsuzawa, Ryushi Seo, Hironori Harada, Akira Suga, Tomoaki Abe, Hidenori Azami, Shunichiro Matsumoto, Takashi Shin, Masayuki Tanahashi, Toru Watanabe
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Publication number: 20120094971Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.Type: ApplicationFiled: September 3, 2009Publication date: April 19, 2012Applicant: REPLIGEN CORPORATIONInventors: James R. Rusche, Norton P. Peet, Allen T. Hopper
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Patent number: 8158825Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: June 21, 2006Date of Patent: April 17, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Patent number: 8153800Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7 or —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitType: GrantFiled: August 3, 2011Date of Patent: April 10, 2012Assignees: Tibotec Pharmaceuticals Ltd., Medivar ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Karl Magnus Nilsson, Bengt Bertril Samuelsson, Asa Annica Kristina Rosenquist
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Patent number: 8148411Abstract: The present invention relates to 2-hetarylthiazole-4-carboxamide derivatives of the formula (I), the use thereof as medicament for the treatment of various disorders, and processes for the preparation thereofType: GrantFiled: December 9, 2008Date of Patent: April 3, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Ulrich Bothe, Arne Von Bonin, Duy Nguyen, Ulf Bomer, Judith Guenther
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Publication number: 20120077855Abstract: The disclosure features crystalline tripeptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions.Type: ApplicationFiled: September 20, 2011Publication date: March 29, 2012Inventors: Pasit Phiasivongsa, Louis C. Sehl
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Publication number: 20120065206Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: ApplicationFiled: December 1, 2009Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Publication number: 20120058986Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.Type: ApplicationFiled: September 2, 2011Publication date: March 8, 2012Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
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Publication number: 20120040962Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.Type: ApplicationFiled: March 25, 2010Publication date: February 16, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20120028995Abstract: The invention relates to compounds of general formula (I) as set forth in the claims as well as to the use of the compounds of the general formula (1) in the medical field, specifically for use in the suppression of DNA synthesis and inflammatory cytokine production as well as in the stimulation of anti-inflammatory cytokine production in vitro and in vivo. This abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.Type: ApplicationFiled: July 19, 2011Publication date: February 2, 2012Applicant: IMTM GMBHInventors: Siegfried ANSORGE, Ute BANK, Anke HEIMBURG, Heiko JULIUS, Karsten NORDHOFF, Michael TAEGER
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Patent number: 8106215Abstract: The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists.Type: GrantFiled: July 2, 2008Date of Patent: January 31, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Publication number: 20120022059Abstract: The present invention relates to novel substituted furancarboxamides, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.Type: ApplicationFiled: June 16, 2011Publication date: January 26, 2012Applicant: AiCuris GmbH & Co. KGInventors: Kai THEDE, Susanne Greschat, Steffen Wildum, Daniela Paulsen
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Publication number: 20120014914Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt, or mixtures thereof, that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.Type: ApplicationFiled: September 21, 2011Publication date: January 19, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Luc J. Farmer, Robert B. Perni, Govinda Rao Bhisetti, Keith P. Wilson
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Publication number: 20120009141Abstract: A compound of Formula 1: or a salt thereof, and methods for the use thereof, especially as an IAP inhibitor, as well as related compounds, compositions, and methods.Type: ApplicationFiled: August 7, 2009Publication date: January 12, 2012Applicant: PHARMASCIENCE INC.Inventors: Alain Laurent, Melanie Proulx, James B. Jaquith, Irina Denissova
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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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Patent number: 8088804Abstract: Described herein are N-hydroxyamide antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical compositions compound of Formula (I): or a salt, solvate ti hydrate thereof, wherein A is (a) each indicates a point of attachment.Type: GrantFiled: December 4, 2006Date of Patent: January 3, 2012Assignee: Pfizer Inc.Inventors: Rakesh Kumar Jain, Mikhail Fedorovich Gordeev, Jason Gustaf Lewis, Charles Francavilla
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Publication number: 20110318359Abstract: The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor.Type: ApplicationFiled: December 2, 2009Publication date: December 29, 2011Inventors: Edward P. Feener, Allen Clermont
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Publication number: 20110312953Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, Qx, A, Qy and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and to a plurality of processes for their preparation.Type: ApplicationFiled: June 14, 2011Publication date: December 22, 2011Applicant: BAYER CROPSCIENCE AGInventors: Rùdiger FISCHER, Christoph GRONDAL, Markus HEIL, Heinz-Juergen WROBLOWSKY, Ernst Rudolf GESING, Arnd VOERSTE, Ulrich GÖGENS
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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: 20110306646Abstract: The present invention relates to a N-(Phenylcycloalkyl)carboxamide or N-(Benzylcycloalkyl)carboxamide or its thiocarboxamide derivative of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, substituted or non-substituted 5-membered heterocyclyl group, T represents an oxygen or a sulphur atom, B represents a non aromatic carbocycle that can be substituted by one to four C1-C8-alkyl groups, and X, Z1, Z2 and Z3 represent various substituents; their process of preparation; the preparation of intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: February 16, 2010Publication date: December 15, 2011Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Marie-Claire Cournoyer, Philippe Rinolfi, Ulrike Wachendorff-Neumann
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Publication number: 20110295012Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7 or —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from niType: ApplicationFiled: August 3, 2011Publication date: December 1, 2011Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominque Louis Nestor Ghislai Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Vladimir Ivanov, Michael Pelcman, Anna Karin Gertrud Linnea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
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Patent number: 8067638Abstract: The present invention is to provide a compound represented by the general formula (1) exhibiting a high insecticidal effect and an insecticide comprising the compound as an active ingredient. The compound represented by the general formula (1) and an insecticide comprising the compound as an active ingredient, wherein, in the formula, A1, A2, A3 and A4 each represent a carbon atom or the like; R1 and R2 each represent a hydrogen atom or the like; G1 and G2 represent an oxygen atom or the like; Xs each represent a hydrogen atom, a halogen atom or the like; n represents an integer of 0 to 4; Q1 represents a substituted phenyl group, a substituted heterocyclic group or the like; Q2 represents a substituted phenyl group, a substituted heterocyclic group or the like.Type: GrantFiled: June 20, 2006Date of Patent: November 29, 2011Assignee: Mitsui Chemicals, Inc.Inventors: Akiyoshi Kai, Takeo Wakita, Hiroyuki Katsuta, Kei Yoshida, Hidetaka Tsukada, Yusuke Takahashi, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido
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Publication number: 20110281875Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: July 8, 2011Publication date: November 17, 2011Inventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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Publication number: 20110269753Abstract: Compounds of the formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, N-oxides, metabolites and prodrugs thereof. These compounds are phosphodiesterase type 4 (PDE4) inhibitors. They are useful in the treatment of a variety of allergic or inflammatory diseases including asthma, COPD, chronic bronchitis, atopic dermatitis, allergic rhinitis, allergic conjunctivitis, vernal conjunctivitis, psoriasis, rheumatoid arthritis, ulcerative colitis, Crohn's disease, uveitis, NASH and lupus.Type: ApplicationFiled: January 21, 2010Publication date: November 3, 2011Applicant: ORCHID RESEARCH LABORATORIES LTD.Inventors: Gopalan Balasubramanian, Sukunath Narayanan, Ganapavarapu Veera Raghava Sharma, Lavanya Andiappan, Shridhar Narayanan, Sanjeev Saxena, Sridharan Rajagopal, Santosh Lolaknath Vishwakarma, Saravanan Thirunavukkarasu
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Publication number: 20110263626Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: August 28, 2008Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-metz, Rainer Walter
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Publication number: 20110263486Abstract: The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y is —NRaRb, —NRc?ONRaRb, —NRcC?SNRaRb, —NRcC?NRdNaRb, heterocycle, —C?ONRaRb, heterocycle, or aryl; n is 0 to 8; m is 0, or 1; r is 0 to 3; t is 0 to 3; X is O or N; Z is CH2, C?O, C?S or a single bond; Z1 is CO—R2, CS—R2, (CH2)t—R2 or the side-chain of a naturally occurring amino acid; Z2 is CO—R2, CS—R2 or (CH2)t—R3 or the side-chain of a naturally occurring amino acid; Z3 is CO—R2, CS—R2 or (CH2)t—R4 or the side-chain of a naturally occurring amino acid; Z4 is H, alkyl, alkoxy, or cycloalkyl; R1, R2, R3, and R4 are independently from each other H, OH, SH, NH2, CN, NO2, alkyl, cycloalkyl, heterocycloalkyl, haloalkyl, alkylthio, haloalkyloxy, hydroxyalkyl, hydroxyalkylamino, alkylamino, alkylaryl, alkylsulfinyl, alkylsulfonyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxyalkyl, alkoxy, aryloxy, heteroaryl, aryl, or halogen.Type: ApplicationFiled: March 11, 2011Publication date: October 27, 2011Applicant: 4SC AGInventors: Johann LEBAN, Martin KRALIK
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Publication number: 20110263662Abstract: The invention relates to 1,2-diamido-ethylene derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: August 14, 2008Publication date: October 27, 2011Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
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Publication number: 20110257174Abstract: 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: September 29, 2009Publication date: October 20, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Christopher Oalmann, Robert B. Perni, Chi B. Vu
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Publication number: 20110257196Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.Type: ApplicationFiled: December 29, 2010Publication date: October 20, 2011Inventors: Yan Lu, Chien-Ming Li, Zhao Wang, Jianjun Chen, Wei Li, James T. Dalton, Duane D. Miller, Charles Duke, Sunjoo Ahn
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Patent number: 8039495Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: GrantFiled: October 15, 2010Date of Patent: October 18, 2011Assignee: Hoffman-La Roche Inc.Inventors: David Robert Bolin, Yimin Qian, Kshitij Chhabilbhai Thakkar, Lin Yi, Weiya Yun
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Publication number: 20110245239Abstract: Novel isoxazoline compounds and compositions containing the compounds are disclosed. The compounds have pesticidal properties and are suitable for use on non-human animals.Type: ApplicationFiled: December 17, 2009Publication date: October 6, 2011Inventors: Steve Nanchen, Noëlle Gauvry, Thomas Goebel
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Patent number: 8030495Abstract: The present invention is directed to cyclopropyl proline bis-amide 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: GrantFiled: May 19, 2008Date of Patent: October 4, 2011Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
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Patent number: 8030339Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: GrantFiled: October 12, 2006Date of Patent: October 4, 2011Assignee: Neurosearch A/SInventors: William Dalby Brown, Janus S. Larsen, Lene Teuber, David Tristram Brown, Philip K. Ahring, Naheed Mirza, Elsebet Østergaard Nielsen
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Patent number: 8022096Abstract: Pyrrolidine compounds described herein and methods for using them to inhibit dipeptidyl peptidase IV and treat Type II diabetes.Type: GrantFiled: February 25, 2009Date of Patent: September 20, 2011Assignee: National Health Research InstitutesInventors: Weir-Torn Jiaang, Yu-Sheng Chao, Ting-Yueh Tsai, Tsu Hsu
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Patent number: 8017788Abstract: N-Substituted heteroaryl (substituted)alkyl sulfoximines are effective at controlling insects.Type: GrantFiled: March 12, 2010Date of Patent: September 13, 2011Assignee: Dow AgroSciences LLCInventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Gregory T. Whiteker, Nneka T. Breaux, John F. Daeuble
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Patent number: 8017771Abstract: Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-type coupling reactions between peptidic compounds having a hydroxyproline moiety of the following formula: and halogenated or sulfonated bromoquinoline compounds.Type: GrantFiled: January 16, 2009Date of Patent: September 13, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Carl Alan Busacca, Rogelio Perez Frutos, Nizar Haddad, Suresh R. Kapadia, Jon Charles Lorenz, Anjan Saha, Chris Hugh Senanayake, Xudong Wei
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Patent number: 8008502Abstract: The present invention relates to novel thiazoline acids and derivatives thereof useful as chelators of trivalent metals in therapeutic applications. For example, the thiazoline acid derivatives are useful in diagnosing and treating pathological conditions associated with an excess of trivalent metals in humans and animals.Type: GrantFiled: March 27, 2009Date of Patent: August 30, 2011Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron
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Publication number: 20110207771Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: June 6, 2007Publication date: August 25, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Daniel Stierli, John J. Taylor, Harald Walter, Paul Anthony Worthington, Ramya Rajan
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Publication number: 20110207767Abstract: This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.Type: ApplicationFiled: November 3, 2009Publication date: August 25, 2011Inventors: Patrick Henry Beusker, Rudy Gerardus Elisabeth Coumans, Ronald Christiaan Elgrtsma, Wiro Michaël Petrus Bernardus Menge, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker, Franciscus Marinus Hendrikus De Groot
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Publication number: 20110178063Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: June 3, 2009Publication date: July 21, 2011Applicant: GLAXO GROUP LIMITEDInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
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Publication number: 20110178101Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: January 18, 2011Publication date: July 21, 2011Inventors: Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20110172207Abstract: The present invention relates to novel substituted pyrazolamides, methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of retroviral diseases, in humans and/or animals.Type: ApplicationFiled: September 16, 2010Publication date: July 14, 2011Applicant: AiCuris Gmbh & Co. KGInventors: Rudolf SCHOHE-LOOP, Reinhold Welker, Arnold Paessens, Marcus Bauser, Friederike Stoll, Frank Dittmer, Kerstin Henninger, Daniela Paulsen, Dieter Lang