Asymmetrical (e.g., 1, 2, 4-triazines, Etc.) Patents (Class 544/182)
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Publication number: 20090023730Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: February 25, 2008Publication date: January 22, 2009Applicant: ACHILLION PHARMACEUTICALSInventors: Avinash Phadke, Dawei Chen, Milind Deshpande, Andrew Thurkauf, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Publication number: 20090012092Abstract: 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)—NR13 R1Type: ApplicationFiled: August 10, 2005Publication date: January 8, 2009Inventors: Georges Joseph Cornelius Hoornaert, Amuri Kilonda, Jan Heeres, Paulus Joannes Lewi, Marc Rene de Jonge, Frederik Frans Desire Daeyaert, Hendrik Maarten Vinkers, Lucien Maria Henricus Koymans, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts
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Patent number: 7473669Abstract: This invention relates to substituted dihydrotriazinones, triazinones and related compounds, compositions comprising such compounds and an agronomically acceptable carrier, and the use thereof as broad spectrum fungicides. This invention also teaches methods of preparing these compounds as well as methods of using the compounds as fungicides.Type: GrantFiled: May 3, 2006Date of Patent: January 6, 2009Assignee: Dow AgroSciences LLCInventors: Steven Howard Shaber, Maurice Chee Hoong Yap, Kevin Gerald Meyer, Noormohamed Mohamed Niyaz, Brent Jeffrey Rieder, Michael Thomas Sullenberger, William Randal Erickson, Frisby Davis Smith
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Publication number: 20090005383Abstract: 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: ApplicationFiled: August 20, 2008Publication date: January 1, 2009Inventors: 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: 20090005346Abstract: The present invention provides 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections.Type: ApplicationFiled: December 8, 2006Publication date: January 1, 2009Applicants: K.U.Leuven Research & Development, Institute of Organic Chemistry and Biochemistry Academy of Sciences of the Czech RepublicInventors: Antonin Holy, Marcela Krecmerova, Alois Piskala, Graciela Andrei, Erik De Clercq, Robert Snoeck, Johan Neyts, Lieve Naesens
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Patent number: 7470688Abstract: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii) where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C?O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(?O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2; RC1 and RC2 are independently selected from H, R, C(?O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-Type: GrantFiled: October 17, 2006Date of Patent: December 30, 2008Assignee: Maybridge LimitedInventors: Muhammad Hashim Javaid, Keith Allan Menear, Sylvie Gomez, Marc Geoffrey Hummersone, Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Xiao-Ling Fan Cockcroft, Frank Kerrigan
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Publication number: 20080312238Abstract: A series of mono- and binuclear 4-arylazo-3,5-diamino-pyrazoles which are useful for inhibition of cyclin-dependent kinases (preferably CDK9). Hence they can be used as antimitotic-, pro-apoptotic and antiinflammatory drugs, in particular, in chemotherapy of cancer and asthma, therapy of psoriasis and parasitoses as those caused by fungi or protists, treatment of Alzheimer's disease or as anti neurodegenerative drugs, or to suppress immunostimulation. These compounds are useful in a variety of utilities, including as intermediates in the preparation of flame-retardants, diagnostic reagents and therapeutics, including antivirals and immunosuppressors.Type: ApplicationFiled: September 1, 2005Publication date: December 18, 2008Applicant: Institute of Experimental Bontany of the Academy of Sciences of the Czech Republic, v.v.i.Inventors: Petr Cankar, Iveta Frysova, Vladimir Krystof, Rene Lenobel, Jan Slouka, Miroslav Strnad, Peter Martin Fischer
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Patent number: 7462614Abstract: The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: GrantFiled: March 29, 2004Date of Patent: December 9, 2008Assignee: Smithkline Beecham CorporationInventors: Mui Cheung, Nigel Paul King, Kevin Wayne Kuntz, Robert Anthony Mook, Jr., Mark Andrew Pobanz, James Michael Salovich, Brian John Wilson
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Publication number: 20080299055Abstract: 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: ApplicationFiled: May 4, 2005Publication date: December 4, 2008Applicant: Pierre Fabre Dermo-CosmetiqueInventors: Jerome Rey, Pascal Bordat, Roger Tarroux
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Publication number: 20080287444Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: ApplicationFiled: April 25, 2008Publication date: November 20, 2008Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Patent number: 7452882Abstract: 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: July 18, 2006Date of Patent: November 18, 2008Assignee: 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: 20080267892Abstract: 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: ApplicationFiled: May 4, 2005Publication date: October 30, 2008Applicant: Pierre Fabre Dermo-CosmetiqueInventors: Willy Picoul, Marco Ciufolini, Pascal Bordat, Roger Tarroux
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Publication number: 20080261971Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, (I) wherein R1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, (II) or (III) R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl;Type: ApplicationFiled: July 29, 2005Publication date: October 23, 2008Inventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Patent number: 7429590Abstract: Compounds described by the Formula (I) or (II): or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidieal agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria. African typanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).Type: GrantFiled: December 6, 2004Date of Patent: September 30, 2008Assignee: Merck & Co. Inc.Inventors: Tesfaye Biftu, Matthew J. Wyvratt, Louis L. Zuegner, III, legal representative, Michael H. Fisher
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Patent number: 7410968Abstract: The present invention relates to compounds represented by formula (I): where the structural variables are as defined herein. The compounds are useful for promoting hydration of mucosal surfaces.Type: GrantFiled: August 26, 2005Date of Patent: August 12, 2008Assignee: PARION SCIENCES, Inc.Inventors: Michael R. Johnson, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
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Patent number: 7407956Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: January 8, 2007Date of Patent: August 5, 2008Assignee: Pfizer, Inc.Inventors: Mark A. Dombrowski, Allen J. Duplantier
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Patent number: 7405217Abstract: This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals.Type: GrantFiled: November 9, 2006Date of Patent: July 29, 2008Assignee: SmithKline Beecham p.l.c.Inventors: Clive Leslie Branch, Christopher Norbert Johnson, David John Nash, Geoffrey Stemp
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Publication number: 20080167313Abstract: The invention concerns 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a branched or linear C1-C7 alkyl or alkenyl radical, a C1-C6 alkyl radical substituted by groups such as trifluoromethyl, C5-C6 cycloalkyl, nitrile, C1-C4 alkoxycarbonylvinyl, hydroxycarbonylvinyl, C1-C4 alkoxycarbonyl, carboxylate, benzyloxy or phenyl (for which the phenyl ring is optionally substituted by one or more groups such as C1-C4 alkoyl, C1-C4 alkoxy, nitro, halogen, trifluoromethyl); YR3 represents oxygen or NR3 for which R3 represents hydrogen, a linear or branched C1-C7 alkyl or alkenyl radical, a C1-C6 alkyl radical substituted by groups such as trifluoromethyl or phenyl (for which the phenyl ring is optionally substituted by one or more groups such as C1-C4 alkoyl, C1-C4 alkoxy, nitro, halogen, trifluoromethyl); Z represents an oxygen atom or a carbon atom capable of being bound to the ortho, meta or para positions of the phenyl group of formula I; nType: ApplicationFiled: March 2, 2006Publication date: July 10, 2008Applicant: Pierre Fabre MedicamentInventors: Elisabeth Dupont-Passelaigue, Isabelle Leroy, Jean-Francois Patoiseau, Didier Junquero, Yves Rival, Andre Delhon
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Patent number: 7390807Abstract: The present invention relates to lamotrigine, a useful agent for anti-epilepsia. New crystal forms of lamotrigine containing molecules of the solvent in stoichiometric ratios are disclosed. The present invention also provides processes for preparing the new crystal forms of lamotrigine.Type: GrantFiled: January 31, 2005Date of Patent: June 24, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Nissim Garti, Yana Berkovich, Ben-Zion Dolitzky, Judith Aronhime, Claude Singer, Anita Liebermann, Neomi Gershon
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Patent number: 7390899Abstract: The present invention relates to a new process for the synthesis of high purity 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of formula (I) using 2,3-dichlorobenzoyl cyanide and an aminoguanidine salt as starting materials. 2,3-dichlorobenzoyl cyanide is reacted with 1-2 mol equivalent of aminoguanidine salt in 3-6 mol equivalent of methanesulfonic acid, then the obtained adduct of formula (IV) is transformed without isolation into the product with magnesium oxide.Type: GrantFiled: September 18, 2003Date of Patent: June 24, 2008Assignee: Richter Gedeon Vegyeszeti Gyar. RT.Inventors: Jozsef Neu, Tibor Gizur, Jozsef Törley, Janos Csabai, Ferenc Vegh, Peter Kalvin, Gabor Tarkanyi
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Publication number: 20080146544Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.Type: ApplicationFiled: February 25, 2008Publication date: June 19, 2008Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
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Publication number: 20080138283Abstract: The present invention relates to Radiolabeled Compounds and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.Type: ApplicationFiled: June 28, 2007Publication date: June 12, 2008Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Joseph John Mann, J.S. Dileep Kumar
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Publication number: 20080139808Abstract: The present invention relates to lamotrigine, a useful agent for anti-epilepsia. New crystal forms of lamotrigine containing molecules of the solvent in stoichiometric ratios are disclosed. The present invention also provides processes for preparing the new crystal forms of lamotrigine.Type: ApplicationFiled: January 30, 2008Publication date: June 12, 2008Inventors: Nissim Garti, Yana Berkovich, Ben-Zion Dolitzky, Judith Aronhime, Claude Singer, Anita Liebermann, Neomi Gershon
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Publication number: 20080113990Abstract: Biphenyl derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.Type: ApplicationFiled: October 12, 2006Publication date: May 15, 2008Inventors: Esther Martinborough, Danielle Lehsten, Timothy Neubert, Aarti Sameer Kawatkar, Nicole Zimmermann, Andreas Termin
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Patent number: 7371750Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, c-Raf, Csk, Fes, FGFR, Flt3, Ikk, IR, JNK, Lck, Mkk, PKC, PKD, Rsk, SAPK, Syk, Trk, BTK, Src, EGFR, IGF, Mek, Ros and Tie2 kinases.Type: GrantFiled: July 29, 2004Date of Patent: May 13, 2008Assignee: IRM LLCInventors: Taebo Sim, Hyun Soo Lee, Pingda Ren, Qiang Ding, Guobao Zhang, Yi Liu, Xia Wang, Tetsuo Uno, Bing Li, Lintong Li, Nathanael Schiander Gray, Shuli You
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Patent number: 7368569Abstract: This invention relates to a process for making spirolactone compounds analogous to formula IType: GrantFiled: October 14, 2003Date of Patent: May 6, 2008Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ralph P. Volante, David M. Tschaen, Steven A. Weissman, Matthew Heileman, Toshiaki Mase, Takehiko Iida, Kenji Maeda, Toshihiro Wada, Hiroki Sato, Kenichi Asakawa
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Publication number: 20080064872Abstract: A novel compound having agonist activity at the S1P3 receptor which is represented by the formula I wherein X is selected from the group consisting of CR3, N and NO; Y is selected from the group consisting of CR3, N and NO; Z is selected from the group consisting of CR3, N and NO; and at least one of X, Y and Z is N or NO; V is O or NOR4 R1 is an aryl group; R2 is an aryl group; R3 is selected from the group consisting of H and alkyl; and 2 of said R3 groups may together form a cyclic alkyl ring having from 3 to 6 carbon atoms; R4 is selected from the group consisting of H and alkyl; a is 0 or an integer of from 1 to 6; b is 0 or 1; c is 0 or 1; f is 0 or an integer of 1 or 2; x is 0 or 1; y is 0 or an integer of from 1 to 3; and z is 0 or an integer of from 1 to 3.Type: ApplicationFiled: September 6, 2007Publication date: March 13, 2008Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Xiaoxia Liu
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Patent number: 7326706Abstract: The present application describes compounds according to Formula I, wherein A, G1, G2 and R1 are described herein. Additionally, the present application describes pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents.Type: GrantFiled: August 12, 2004Date of Patent: February 5, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Bruce A. Ellsworth, Chongqing Sun, Annapurna Pendri
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Patent number: 7304072Abstract: Compounds represented by the general formula (I) wherein Ar1 represents an aryl or heteroaryl which may be substituted; n represents 0 or 1; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen; and a salt, ester or N-oxide derivative thereof. The compounds exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases, sexual and reproductive dysfunctions, gastro-intestinal disorders, respiratory disorders, inflammation or glaucoma, and the like.Type: GrantFiled: August 23, 2004Date of Patent: December 4, 2007Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh, Masato Chiba
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Patent number: 7304063Abstract: The present invention is directed to compounds which contain a heterocyclic triazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 20, 2004Date of Patent: December 4, 2007Assignee: Merck & Co., Inc.Inventors: Mark T. Bilodeau, Craig W. Lindsley, Zhijian Zhao
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Patent number: 7271167Abstract: 1,2,4-Triazin-5-ones useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: October 9, 2003Date of Patent: September 18, 2007Assignee: Cytokinetics, Inc.Inventors: Xiangping Qian, Gustave Bergnes, David J. Morgans, Jr.
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Patent number: 7262200Abstract: The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.Type: GrantFiled: October 27, 2003Date of Patent: August 28, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, David J. Lauffer, Huan Qui Li, Ronald Charles Tomlinson, Pan Li
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Patent number: 7259163Abstract: Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; C represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; D represents a saturated or unsaturated optionally substituted 6-membered heterocyclic ring; E represents hydrogen or C1-6alkyl; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof, processes for their preparation and methods of using them in HCV treatment are provided.Type: GrantFiled: October 30, 2002Date of Patent: August 21, 2007Assignee: Glaxo Group LimitedInventors: Gianpaolo Bravi, Rossella Guidetti, David Haigh, Charles David Hartley, Peter David Howes, Deborah Lynette Jackson, Victoria Lucy Helen Lovegrove, Pritom Shah, Martin John Slater, Katrina Jane Wareing
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Publication number: 20070185113Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: January 29, 2007Publication date: August 9, 2007Inventors: Christoph Faeh, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Philippe Pflieger
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Patent number: 7235657Abstract: The present invention relates to the methods for preparing compounds of the formula I: or the pharmaceutically acceptable salts thereof, wherein R1, R2, R4, R10, and R11 have any of the values defined in the specification. The compounds of the present invention are useful in the treatment of diseases, including inflammatory diseases such as rheumatoid arthritis.Type: GrantFiled: June 27, 2005Date of Patent: June 26, 2007Assignee: Pfizer Inc.Inventor: Zhengong Bryan Li
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Patent number: 7230100Abstract: A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, carbon or sulphur, comprising a coupling step of the pyrimidine base with a molecule of formula (B) described herein in a suitable coupling solvent, in the presence of catalytic amounts of an element or combination of elements of groups IB or IIB of the periodic table, a tertiary amine and a Lewis acid to obtained an intermediate of formula (D) which is deprotected in the subsequent step to generate the product of formula (A).Type: GrantFiled: April 7, 2006Date of Patent: June 12, 2007Assignee: Shire BioChem., Inc.Inventor: Qing Yu
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Patent number: 7223759Abstract: The invention relates to antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds and pharmaceutical compositions thereof. This invention also relates to a method of using such compounds in the treatment of bacterial infections in mammals, especially humans.Type: GrantFiled: September 15, 2004Date of Patent: May 29, 2007Assignee: Anadys Pharmaceuticals, Inc.Inventors: Yuefen Zhou, Dionisios Vourloumis, Vlad E. Gregor, Geoffrey C. Winters, Thomas Hermann, Benjamin Ayida, Zhongxiang Sun, Douglas Murphy, Klaus B. Simonsen
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Patent number: 7220783Abstract: The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R1–R13 are hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is —O—, —CH2—, —NR14— or —S(O)p- and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.Type: GrantFiled: November 12, 2003Date of Patent: May 22, 2007Assignee: Shionogi & Co., Ltd.Inventors: Kenji Kawada, Mitsuaki Ohtani, Ryuji Suzuki, Akinori Arimura
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Patent number: 7214677Abstract: The present invention relates to novel to P2X7 inhibitors of formula I and to processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them, and their use in therapy. The active compounds of the present invention are potent inhibitors of P2X7 and as such are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: November 12, 2002Date of Patent: May 8, 2007Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Allen J. Duplantier, Chakrapani Subramanyam
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Patent number: 7192959Abstract: The present invention relates to compounds represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are defined herein. The compounds are useful for blocking sodium channels.Type: GrantFiled: April 21, 2004Date of Patent: March 20, 2007Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
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Patent number: 7189719Abstract: The present invention relates to a compound represented by formula (I): in which at least one of R3 and R4 is a group represented by formula (A): where the structural variables are as defined herein. The compounds are useful for blocking sodium channels.Type: GrantFiled: April 21, 2004Date of Patent: March 13, 2007Assignee: Parion Sciences, Inc.Inventor: Michael R. Johnson
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Patent number: 7176202Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1–R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: October 27, 2005Date of Patent: February 13, 2007Assignee: Pfizer Inc.Inventors: Mark A. Dombroski, Allen J. Duplantier
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Patent number: 7160886Abstract: Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: February 27, 2004Date of Patent: January 9, 2007Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Liangqin Guo, Qingmei Hong, Ravi P. Nargund, Patrick G. Pollard, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye
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Patent number: 7157464Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: June 11, 2003Date of Patent: January 2, 2007Assignee: Chemocentryx, Inc.Inventors: Andrew M. K. Pennell, James B. Aggen, J.J. Kim Wright, Subrabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
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Patent number: 7135471Abstract: Aryl oxime derivatives of the formula (I), in which R1, R2, R3, X and B are as defined in claim 1, act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDSType: GrantFiled: May 16, 2003Date of Patent: November 14, 2006Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Norbert Beier, Pierre Schelling, Michael Wolf
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Patent number: 7129241Abstract: Pyridazine derivatives of the formula (I) act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDSType: GrantFiled: May 12, 2003Date of Patent: October 31, 2006Assignee: Merck Patent GesellschaftInventors: Hans-Michael Eggenweiler, Michael Wolf
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Patent number: 7109334Abstract: A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, carbon or sulphur, comprising a coupling step of the pyrimidine base with a molecule of formula (B) described herein in a suitable coupling solvent, in the presence of catalytic amounts of an element or combination of elements of groups IB or IIB of the periodic table, a tertiary amine and a Lewis acid to obtained an intermediate of formula (D) which is deprotected in the subsequent step to generate the product of formula (A).Type: GrantFiled: June 14, 2002Date of Patent: September 19, 2006Assignee: Shire BioChem, Inc.Inventor: Qing Yu
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Patent number: 7101915Abstract: The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R1–R13 are hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is —O—, CH2—, —NR14— or —S(O)p— and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.Type: GrantFiled: July 30, 1997Date of Patent: September 5, 2006Assignee: Shionogi & Co., Ltd.Inventors: Kenji Kawada, Mitsuaki Ohtani, Ryuji Suzuki, Akinori Arimura
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Patent number: 7078403Abstract: Disclosed herein are compounds of formula II: wherein Alk, Z, X1, X2, R1, —R10 and R11 are defined herein, and their salts and pharmaceutically acceptable derivatives thereof, as well as other compounds of the general formula Het-A-Alk-W-Ar-C(X2)?NO-X2 where Het, A, W and Ar are also defined herein. These compounds are useful in treating picornavirus infections in mammals. Novel intermediates of these compounds, as well as pharmaceutical compositions and methods of use, are also disclosed herein.Type: GrantFiled: June 16, 2000Date of Patent: July 18, 2006Assignee: Biota Scientific Management Pty Ltd.Inventors: Wen-Yang Wu, Keith Watson, Darryl McConnell, Betty Jin, Guy Krippner
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Patent number: 7074836Abstract: The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R1–R13 are hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is —O—, —CH2—, NR14— or —S(O)p— and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.Type: GrantFiled: November 12, 2003Date of Patent: July 11, 2006Assignee: Shionogi & Co., Ltd.Inventors: Kenji Kawada, Mitsuaki Ohtani, Ryuji Suzuki, Akinori Arimura