Asymmetrical (e.g., 1, 2, 4-triazines, Etc.) Patents (Class 544/182)
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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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Patent number: 8076334Abstract: 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 diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.Type: GrantFiled: September 2, 2008Date of Patent: December 13, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Nancy-Ellen Haynes, Nathan Scott, Jefferson Wright Tilley
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Patent number: 8053573Abstract: The invention relates to the use of 5,6-diphenyl-1,2,4-triazinic compounds of general formula (I), wherein cycle penetrating bonds display an ortho, meta or para indifferent substitution position, identical or different R1 and R2 represent a hydrogen, fluoride, chloride or bromine atom, C1 to C12 linear or branched alkyl, C1 A C18 linear or branched hydroxy, alkoxy poly(ethoxy)-alkoxy with a C1 to C4 alkyl fragment and an ethoxy number ranging from 1 to 4, amino or mono or di-alkylamino with a C1 to C4 alkyl fragment group, R3 represents a chlorine atom, a hydroxy, amino, a phenyl possibly 1 to 3 times substituted by a hydroxy radical situated at least in a para or phenyl position possibly 1 to 3 times substituted in an ortho, meta or para position by a C1 to C12 alkoxy or cyano or alkymino group with a C1 to C7 alkyl fragment in the form of active sun filters or light-protective agents and to cosmetic composition containing said compounds.Type: GrantFiled: May 4, 2005Date of Patent: November 8, 2011Assignee: Pierre Fabre Dermo-CosmetiqueInventors: Jérôme Rey, Pascal Bordat, Roger Tarroux
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Publication number: 20110269712Abstract: This invention is directed to compounds of Formula (1) including all geometric and stereoisomers, N oxides, and agriculturally suitable salts thereof, agricultural compositions containing them and their use as fungicides, (1) provided that the compound of Formula 1 is other than 2-[1-[(2-chlorophenyl)acetyl]-4-piperidinyl]-N-methyl-N-[(1R)-1-phenylethyl]-4-thiazolecarboxamide and R1 is other than 4-fluorophenyl; wherein R1, R2, A, G, Q, W1, W2, X and n are otherwise as defined in the disclosure, Also disclosed are compositions containing the a compound having a formula corresponding to Formula (1) where the provisos are both omitted; and methods for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound having a formula corresponding to Formula (1) where the provisos are both omitted.Type: ApplicationFiled: July 26, 2006Publication date: November 3, 2011Inventors: John Joseph Bisaha, Patrick Ryan Kovacs, Renne M. Lett, Jeffrey Keith Long, Robert James Pasteris, Boris Abramovich Klyashchitsky, Bruce Lawrence Finkelstein, Brenton Todd Smith
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Publication number: 20110269709Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
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Publication number: 20110269760Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Applicant: Cytopia Research Pty LtdInventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
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Publication number: 20110269722Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
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Publication number: 20110245156Abstract: Compounds are disclosed. Compositions that include the compounds are disclosed. Methods of making and using the compounds are also disclosed.Type: ApplicationFiled: December 9, 2009Publication date: October 6, 2011Applicant: CYTOKINE PHARMASCIENCES, INC.Inventor: Thais M. Sielecki-Dzurdz
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MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Publication number: 20110245251Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: December 7, 2009Publication date: October 6, 2011Applicant: Arena Pharmaceuticals, Inc.Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou -
Patent number: 8022221Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: February 12, 2009Date of Patent: September 20, 2011Assignee: Amgen Inc.Inventors: Victor J. Cee, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
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Publication number: 20110212966Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.Type: ApplicationFiled: May 4, 2011Publication date: September 1, 2011Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
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Publication number: 20110212949Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests, including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: July 4, 2009Publication date: September 1, 2011Inventors: Thomas Bretschneider, Eva-Maria Franken, Ulrich Görgens, Martin Füßlein, Achim Hense, Joachim Kluth, Hans-Georg Schwarz, Adeline Köhler, Olga Malsam, Arnd Voerste, Angela Becker
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Patent number: 8008278Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, Ar1, Ar2, E, a, b, c and z are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: September 27, 2010Date of Patent: August 30, 2011Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes
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Patent number: 8003806Abstract: The invention relates to compounds of the Formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1.Type: GrantFiled: November 9, 2005Date of Patent: August 23, 2011Assignee: OSI Pharmaceuticals, LLCInventors: Jason Bloxham, Gary V. Borzillo, Eric William Collington, Shazia Sadiq, Colin Peter Sambrook Smith, Chris L. Waller, Graham M. Wynne
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Publication number: 20110190496Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.Type: ApplicationFiled: April 13, 2011Publication date: August 4, 2011Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A.R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Quinghua Weng, James David Beard
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Publication number: 20110190495Abstract: Disclosed are N-{1-[3-(2-ethoxy-5-(4-ethylpiperazinyl)sulfonylphenyl)-4,5-dihydro-5-oxo-1,2,4-triazin-6-yl]ethyl}butyramide (which is represented by formula III), its preparation method, intermediates during preparation procedure, preparation method for such intermediates and a method for preparing vardenafil from the compound. In the method for preparing vardenafil, a chloro-sulfonation reaction carries out in the early stage of the preparation procedure.Type: ApplicationFiled: December 28, 2007Publication date: August 4, 2011Applicant: Topharman Shanghai Co., Ltd.Inventors: Guanghui Tian, Zheng Liu, Jin Zheng, Jingshan Shen
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Publication number: 20110178087Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.Type: ApplicationFiled: March 30, 2011Publication date: July 21, 2011Applicant: Compass Pharmaceuticals LLC.Inventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
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Publication number: 20110178293Abstract: Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.Type: ApplicationFiled: September 22, 2009Publication date: July 21, 2011Applicant: LEGOCHEM BIOSCIENCE LTD.Inventors: Young Lag Cho, Sang Eun Chae, Sung Yoon Baek, Yeon Ok Kim, Seong Jin Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
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Patent number: 7977331Abstract: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: GrantFiled: December 21, 2007Date of Patent: July 12, 2011Assignee: Japan Tobacco Inc.Inventors: Takahiro Oka, Kazutaka Ikegashira, Shintaro Hirashima, Hiroshi Yamanaka, Satoru Noji, Yasushi Niwa, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yukihiro Nomura
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Publication number: 20110166142Abstract: 2-Substituted isoflavonoid compounds and pharmaceutical compositions containing same are useful as anti-inflammatory agents and antioxidants and for the treatment of related diseases and conditions.Type: ApplicationFiled: June 30, 2008Publication date: July 7, 2011Inventors: Eleanor Eiffe, Andrew Heaton, Catherine Walker, Alan James Husband
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Publication number: 20110166143Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: October 12, 2010Publication date: July 7, 2011Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria Franken, Arnd Voerste
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Publication number: 20110160212Abstract: Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.Type: ApplicationFiled: December 28, 2010Publication date: June 30, 2011Inventors: Weibo Wang, Tongshuang Li
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Publication number: 20110130403Abstract: The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors.Type: ApplicationFiled: March 13, 2008Publication date: June 2, 2011Applicant: RANBAXY LABORATORIES LIMITEDInventors: Sonali Rudra, Nidhi Gupta, Lalit Kumar Baregama, Ritu Agarwal, Mandadapu Raghuramaiah, Vinayak Vasantrao Khairnar, Venkata P. Palle, Sarala Balachandran, Abhijit Ray, Sunada G. Dastidar, Lalitha Vijaykrishnan
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Publication number: 20110123489Abstract: Compounds having the formula I wherein wherein R1, R2 and R3 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors with improved bioavailability. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: November 19, 2010Publication date: May 26, 2011Applicant: Roche Palo Alto LLCInventor: Joshua Paul Gergely Taygerly
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Publication number: 20110118266Abstract: The present invention relates to derivatives of general formula I wherein: —W represents nitrogen, —R1 represents: •a hydrogen or a linear or branched C1-C5 alkyl radical or, •a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, •a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, •a C6 2-oxocycloalkyl radical—R2 represents a methyl or heptyl, —m, n are equal to 1, —V represents CH2, —X—Y represents —N— (C?O)—, —CH—O—, —Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.Type: ApplicationFiled: July 7, 2009Publication date: May 19, 2011Applicant: PIERRE FABRE MEDICAMENTInventors: Isabelle Leroy, Elisabeth Dupont-Passelaigue, Karine Valeille, Yves Rival, Didier Junquero
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Patent number: 7943614Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 6-membered aromatic heterocyclic group optionally fused with a benzene ring, two or more ring constitutional atoms of the heterocyclic group are a nitrogen atom, and the heterocyclic group may be substituted with at least one group selected from the group consisting of a C1-C3 alkyl group etc.], and a plant disease controlling agent comprising this as an active ingredient.Type: GrantFiled: July 12, 2006Date of Patent: May 17, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Sadayuki Arimori, Yoshiharu Kinoshita
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Publication number: 20110112083Abstract: The present invention relates to novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.Type: ApplicationFiled: June 5, 2009Publication date: May 12, 2011Applicant: LEGOCHEM BIOSCIENCE LTD.Inventors: Ho Young Song, Young Lag Cho, Dae Yon Lee, Hee Sock Park, Sung Yoon Baek, Sang Eun Chae, Sang Hui Jo, Yeon Ok Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
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Publication number: 20110086818Abstract: The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.Type: ApplicationFiled: March 11, 2009Publication date: April 14, 2011Applicants: Presidents and Fellows of Harvard College, The General Hospital CorporationInventors: Bruce P. Bean, Clifford J. Woolf
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Patent number: 7923554Abstract: The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(?O)pR6; —NH—S(?O)pR6; —C(?O)R6; —NHC(?O)H; —C(?O)NHNH2; NHC(?O)R6; C(?NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14; —C(?O)—NHR13; —C(?O)—NR13R1Type: GrantFiled: August 10, 2005Date of Patent: April 12, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Georges Joseph Cornelius Hoornaert, Amuri Kilonda, Jan Heeres, Paulus Joannes Lewi, Marc René de Jonge, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Lucien Maria Henricus Koymans, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
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Publication number: 20110059974Abstract: Retinoic acid metabolism blocking agents (RAMBAs). The RAMBAs may be used for treatment of cancer, including breast and prostate cancers. Methods for preparing novel retinamide RAMBAs. The methods include reacting RAMBAs with terminal polar carboxylic acid group with a variety of amines in the presence of suitable coupling reagents. The retinamide RAMBAs are potent inhibitors of the growth of prostate and breast cancer cells and may be useful for the treatment of these diseases in humans.Type: ApplicationFiled: May 7, 2009Publication date: March 10, 2011Applicant: UNIVERSITY OF MARYLAND, BALTIMOREInventors: Vincent C. O. Njar, Lalji K. Gediya, Aakanksha Khandelwal
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Publication number: 20110059973Abstract: The present invention relates to novel pyrazole compounds of the formulae I and II, to their salts and their N-oxides which can be used for combating or controlling invertebrate pests, in particular arthropod pests. The invention also relates to a method for controlling invertebrate pests by using these compounds. The present invention also relates to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a pyrazole radical of the formulae A1, A2 or A3 # denotes the binding site to the remainder of formulae I or II; X1 is S, O or NR1a; X2 is OR2a, NR2bR2c, S(O)mR2d; X3 is a lone pair or oxygen; R1, R2 and R3 are, inter alia, hydrogen, and wherein R41, R42, R43, R51, R52, R53, R61, R62, R63, are as defined in claim 1.Type: ApplicationFiled: August 26, 2008Publication date: March 10, 2011Applicant: BASF SEInventors: Steffen Gross, Delphine Breuninger, Henricus Maria Martinus Bastiaans, Wolfgang von Deyn, Michael Puhl, Karsten Koerber, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi
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Publication number: 20110045974Abstract: The present invention relates to triazinylmethyl sulfonamides of formula I wherein T, R1, R2, R3, A, Y and D are as defined in the claims and to the N-oxides, and salts thereof and their use for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to processes and intermediates for preparing these compounds.Type: ApplicationFiled: March 11, 2009Publication date: February 24, 2011Applicant: BASF SEInventors: Jochen Dietz, Thomas Grote, Wassilios Grammenos, Bernd Mueller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Marianna Vrettou, Alice Glaettli
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Publication number: 20110034450Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: April 6, 2009Publication date: February 10, 2011Applicant: BAYER SCHERING PHARMA AKTIEGESELLSCHAFTInventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
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Patent number: 7880000Abstract: The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other poliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.Type: GrantFiled: May 9, 2005Date of Patent: February 1, 2011Assignee: Amgen Inc.Inventors: Stephanie D. Geuns-Meyer, Brian L. Hodous, Stuart C. Chaffee, Paul A. Tempest, Philip R. Olivieri, Rebecca E. Johnson, Brian K. Albrecht, Vinod F. Patel, Victor J. Cee, Joseph L. Kim, Steven Bellon, Xiaotian Zhu, Yuan Cheng, Ning Xi, Karina Romero, Hanh Nho Nguyen, Holly L. Deak
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Publication number: 20110009413Abstract: Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ?NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflType: ApplicationFiled: January 16, 2009Publication date: January 13, 2011Applicant: UNIVERSITY OF GREENWICHInventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann
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Patent number: 7867629Abstract: A specific derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising the compound. An organic electroluminescence device comprising at least one of organic compound layers including a light emitting layer sandwiched between an anode and a cathode, wherein said at least one of the organic compound layers comprises the derivative of the heterocyclic compound having nitrogen atom as a sole component or as mixed component. The organic electroluminescence device achieves elevation of luminance and excellent efficiency of light emission, and also achieves long lifetime by an improvement of an electrode adhesion.Type: GrantFiled: September 26, 2003Date of Patent: January 11, 2011Assignee: Idemitsu Kosan Co., Ltd.Inventors: Hiroshi Yamamoto, Masahide Matsuura, Hidetsugu Ikeda, Mineyuki Kubota, Masahiro Kawamura
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Publication number: 20100317851Abstract: There is described novel organo-platinum luminophores comprising a complex of formula (I). The luminophores have application as the emissive component in organic light emitting diodes.Type: ApplicationFiled: September 29, 2008Publication date: December 16, 2010Applicant: UNIVERSITY OF YORKInventors: Duncan W. Bruce, Valey Kozhevnikov
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Publication number: 20100311755Abstract: The invention relates to compounds of the formula I: wherein A is a saturated or unsaturated hydrocarbon chain having a chain length of 4 to 6 carbon atoms, the hydrocarbon chain being unsubstituted or substituted by 1, 2 or 3 methyl groups; R1 is selected from the group consisting of hydrogen, C1-C3 alkyl and fluorinated C1-C3 alkyl; R2 is hydrogen, halogen, cyano, C1-C3 alkyl, C1-C3 alkoxy, fluorinated C1-C3 alkyl or fluorinated C1-C3 alkoxy; R3 is selected from the group consisting of branched C4-C6 alkyl and C3-C6 cycloalkyl, and R4 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C3-alkyl and fluorinated C3-C6 cycloalkyl. and the physiologically tolerated salts of these compounds and the N-oxides thereof.Type: ApplicationFiled: October 31, 2008Publication date: December 9, 2010Applicant: ABBOTT GMBH & CO. KGInventors: Wilfried Braje, Sean Colm Turner, Andreas Haupt, Udo Lange, Herve' Geneste, Karla Drescher, Liliane Unger, Ana Lucia Jongen-Relo, Anton Bespalov
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Publication number: 20100303905Abstract: The compositions of the present invention composition comprise a therapeutically effective amount of particles comprising lamotrigine, in combination with granules comprising a disintegrant, and a sugar alcohol and/or a saccharide. These compositions are useful in treating epilepsy and bipolar disorder, particularly for patients with dysphagia, and to improve compliance with bipolar patients.Type: ApplicationFiled: December 1, 2009Publication date: December 2, 2010Inventors: Gopi M. Venkatesh, Nehal H. Vyas, Michael Gosselin, Jin-Wang Lai
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Publication number: 20100305078Abstract: The presently disclosed subject matter is directed to metallo-oxidoreductase inhibitors having metal binding moities linked to a targeting moiety through a linking group or a direct bond, methods for screening for metallo-oxidoreductase inhibitors, and methods of treating an oxidoreductase related disorder by administering a metallo-oxidoreductase inhibitor to a subject in need of treatment thereof.Type: ApplicationFiled: November 21, 2007Publication date: December 2, 2010Applicant: Viamet Pharmaceuticals, Inc.Inventors: Robert J. Schotzinger, William J. Hoekstra
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Publication number: 20100298331Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: March 24, 2008Publication date: November 25, 2010Inventors: Chi-Wan Lee, Teresa Przewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
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Patent number: 7834178Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein.Type: GrantFiled: February 28, 2007Date of Patent: November 16, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Jun Li, Jeffrey A. Robl, Lawrence J. Kennedy
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Patent number: 7816520Abstract: The invention relates to 5,6-diphenyl-1,2,4-triazinic compounds of general formula (I), wherein identical or different R1, R2, R3 and R4 represent a hydrogen, fluoride, chloride or bromine atom, C1 to C12 linear or branched alkyl, C1 A C18 linear or branched hydroxy, alkoxy poly(ethoxy)-alkoxy with a C1 to C4 alkyl fragment and an ethoxy number ranging from 1 to 4, amino or mono or di-alkylamino with a C1 to C4 alkyl fragment group, X is ortho-, meta- or paraphenylene, 4,4?-biphenylene, 2,4- or 2,6- or 3,4- or 3,5-pyridinylene, 2,2?-bipyridinylene, meta- or paraphenylenediamino, ethylenediamine, 2,2?-piperazinylene, diacyl of formula -(R4CO)2-, wherein r represents a phenyl radical, a 3 to 10 carbon, phenanthrene or anthracene atoms alkyl chain except 1,4-bis(5,6-diphenyl-1,2,4-triazin-3-yl)benzene of 2,4-bis(5,6-diphenyl-1,2,4-triazin-3-yl)pyridine and of 2,6-bis(5,6-diphenyl-1,2,4-triazin-3-yl)pyridine, to cosmetic compositions containing said compounds and to the use thereof in the form of sun filters or lType: GrantFiled: May 4, 2005Date of Patent: October 19, 2010Assignees: Pierre Fabre Dermo-Cosmetique, Centre National de la Recherche Scientifique (CNRS), Universite Claude Bernard Lyon 1Inventors: Willy Picoul, Marco Ciufolini, Pascal Bordat, Roger Tarroux
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Patent number: 7807674Abstract: 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 diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.Type: GrantFiled: August 20, 2008Date of Patent: October 5, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Nancy Ellen Haynes, Denis J. Kertesz, Sherrie Lynn Pietranico-Cole, Yimin Qian, Nathan Robert Scott, Sung-Sau So, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley
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Publication number: 20100240661Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; p is an integer ranging from 0 to 5; R1 is halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R6; and when p is an integer ranging from 2 to 5, each R1 may be the same or different; R2 is hydrogen or C1-4alkyl; n is 3, 4, 5 or 6; R6 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such R6 group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R4 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, C3-7 cycloalkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanType: ApplicationFiled: October 1, 2008Publication date: September 23, 2010Inventors: Barbara Bertani, Susanna Cremonesi, Stefano Fontana, Alessandra Pasquarello
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Publication number: 20100234254Abstract: Provided is an additive for lubricating oils which enhances frictional characteristics of slide parts in internal combustion engines and driving system transmission engines and which exhibit an excellent fuel consumption reducing effect. The above additive for lubricating oils comprises a heterocyclic compound having a heterocyclic skeleton originating in a compound selected from pyridines, pyrroles, pyrimidines, pyrazoles, pyridazines, indazoles, pyrazines, triazines, triazoles, tetrazoles, oxazoles, oxadiazoles, thiazoles, thiadiazoles, furans, dioxanes, pyrans and thiophenes. A lubricating oil composition containing the above additive for lubricating oils is effectively used for various low friction slide members, antifriction bearings and slide bearings.Type: ApplicationFiled: March 16, 2007Publication date: September 16, 2010Applicant: Idemitsu Kosan Co., Ltd.Inventors: Hiroaki Koshima, Hideki Kamano
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Publication number: 20100168114Abstract: Methods for determining invertebrate- and insect-specific, such as mosquito-specific, residues of acetylcholinesterases are provided herein. The methods can be used to design pesticides and insecticides that are specific for the invertebrate or insect (e.g., mosquito) enzymes, resulting in reduced toxicity concerns for mammals. Compositions for inhibiting invertebrate and insect (e.g., mosquito) acetylcholinesterases and methods for preparing the same are also provided.Type: ApplicationFiled: December 18, 2009Publication date: July 1, 2010Inventor: Yuan-Ping Pang
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Publication number: 20100168113Abstract: This invention relates to novel substituted nitrocatechol derivatives, their use in the treatment of some central and peripheral nervous system disorders and pharmaceutical compositions containing them.Type: ApplicationFiled: April 10, 2007Publication date: July 1, 2010Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto Dos Santos Ferreira, Patricio Manuel Vieira Soares da Silva
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Publication number: 20100160328Abstract: The present invention relates to the novel compounds of the general formula (I) possessing dipeptidyl peptidase IV enzyme inhibitory activity, pharmaceutical compositions thereof, methods of using said compounds, processes for their preparation and intermediates of the general formulae (II), (IV), (V), (VII), (VIII) and (IX).Type: ApplicationFiled: December 14, 2009Publication date: June 24, 2010Applicant: SANOFI-AVENTISInventors: Peter Aranyi, Imre BATA, Sandor Batori, Eva BORONKAY, Philippe BOVY, Zoltan Kapui, Edit SUSAN, Tibor SZABO, Katalin Urban-Szabo, Marton VARGA
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Publication number: 20100144733Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-14 or encompassed by formulas I-XII) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: ApplicationFiled: November 16, 2009Publication date: June 10, 2010Inventors: Kevin James Doyle, Graham Peter Jones, Michael Geoffrey Neil Russell, Sebastian Bruckner, Jacqueline Anne Macritchie, Joanne Peach