Asymmetrical (e.g., 1, 2, 4-triazines, Etc.) Patents (Class 544/182)
  • Publication number: 20090023730
    Abstract: 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: Application
    Filed: February 25, 2008
    Publication date: January 22, 2009
    Applicant: ACHILLION PHARMACEUTICALS
    Inventors: Avinash Phadke, Dawei Chen, Milind Deshpande, Andrew Thurkauf, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
  • Publication number: 20090012092
    Abstract: 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 R1
    Type: Application
    Filed: August 10, 2005
    Publication date: January 8, 2009
    Inventors: 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
  • Patent number: 7473669
    Abstract: 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: Grant
    Filed: May 3, 2006
    Date of Patent: January 6, 2009
    Assignee: Dow AgroSciences LLC
    Inventors: 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
  • Publication number: 20090005383
    Abstract: 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: Application
    Filed: August 20, 2008
    Publication date: January 1, 2009
    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
  • Publication number: 20090005346
    Abstract: 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: Application
    Filed: December 8, 2006
    Publication date: January 1, 2009
    Applicants: K.U.Leuven Research & Development, Institute of Organic Chemistry and Biochemistry Academy of Sciences of the Czech Republic
    Inventors: Antonin Holy, Marcela Krecmerova, Alois Piskala, Graciela Andrei, Erik De Clercq, Robert Snoeck, Johan Neyts, Lieve Naesens
  • Patent number: 7470688
    Abstract: 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: Grant
    Filed: October 17, 2006
    Date of Patent: December 30, 2008
    Assignee: Maybridge Limited
    Inventors: 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
  • Publication number: 20080312238
    Abstract: 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: Application
    Filed: September 1, 2005
    Publication date: December 18, 2008
    Applicant: 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
  • Patent number: 7462614
    Abstract: 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: Grant
    Filed: March 29, 2004
    Date of Patent: December 9, 2008
    Assignee: Smithkline Beecham Corporation
    Inventors: Mui Cheung, Nigel Paul King, Kevin Wayne Kuntz, Robert Anthony Mook, Jr., Mark Andrew Pobanz, James Michael Salovich, Brian John Wilson
  • Publication number: 20080299055
    Abstract: 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: Application
    Filed: May 4, 2005
    Publication date: December 4, 2008
    Applicant: Pierre Fabre Dermo-Cosmetique
    Inventors: Jerome Rey, Pascal Bordat, Roger Tarroux
  • Publication number: 20080287444
    Abstract: 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: Application
    Filed: April 25, 2008
    Publication date: November 20, 2008
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
  • Patent number: 7452882
    Abstract: 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: Grant
    Filed: July 18, 2006
    Date of Patent: November 18, 2008
    Assignee: 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
  • Publication number: 20080267892
    Abstract: 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 l
    Type: Application
    Filed: May 4, 2005
    Publication date: October 30, 2008
    Applicant: Pierre Fabre Dermo-Cosmetique
    Inventors: Willy Picoul, Marco Ciufolini, Pascal Bordat, Roger Tarroux
  • Publication number: 20080261971
    Abstract: 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: Application
    Filed: July 29, 2005
    Publication date: October 23, 2008
    Inventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
  • Patent number: 7429590
    Abstract: 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: Grant
    Filed: December 6, 2004
    Date of Patent: September 30, 2008
    Assignee: Merck & Co. Inc.
    Inventors: Tesfaye Biftu, Matthew J. Wyvratt, Louis L. Zuegner, III, legal representative, Michael H. Fisher
  • Patent number: 7410968
    Abstract: 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: Grant
    Filed: August 26, 2005
    Date of Patent: August 12, 2008
    Assignee: PARION SCIENCES, Inc.
    Inventors: Michael R. Johnson, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
  • Patent number: 7407956
    Abstract: 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: Grant
    Filed: January 8, 2007
    Date of Patent: August 5, 2008
    Assignee: Pfizer, Inc.
    Inventors: Mark A. Dombrowski, Allen J. Duplantier
  • Patent number: 7405217
    Abstract: This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: July 29, 2008
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Clive Leslie Branch, Christopher Norbert Johnson, David John Nash, Geoffrey Stemp
  • Publication number: 20080167313
    Abstract: 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; n
    Type: Application
    Filed: March 2, 2006
    Publication date: July 10, 2008
    Applicant: Pierre Fabre Medicament
    Inventors: Elisabeth Dupont-Passelaigue, Isabelle Leroy, Jean-Francois Patoiseau, Didier Junquero, Yves Rival, Andre Delhon
  • Patent number: 7390807
    Abstract: 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: Grant
    Filed: January 31, 2005
    Date of Patent: June 24, 2008
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Nissim Garti, Yana Berkovich, Ben-Zion Dolitzky, Judith Aronhime, Claude Singer, Anita Liebermann, Neomi Gershon
  • Patent number: 7390899
    Abstract: 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: Grant
    Filed: September 18, 2003
    Date of Patent: June 24, 2008
    Assignee: Richter Gedeon Vegyeszeti Gyar. RT.
    Inventors: Jozsef Neu, Tibor Gizur, Jozsef Törley, Janos Csabai, Ferenc Vegh, Peter Kalvin, Gabor Tarkanyi
  • Publication number: 20080146544
    Abstract: 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: Application
    Filed: February 25, 2008
    Publication date: June 19, 2008
    Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
  • Publication number: 20080138283
    Abstract: 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: Application
    Filed: June 28, 2007
    Publication date: June 12, 2008
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Joseph John Mann, J.S. Dileep Kumar
  • Publication number: 20080139808
    Abstract: 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: Application
    Filed: January 30, 2008
    Publication date: June 12, 2008
    Inventors: Nissim Garti, Yana Berkovich, Ben-Zion Dolitzky, Judith Aronhime, Claude Singer, Anita Liebermann, Neomi Gershon
  • Publication number: 20080113990
    Abstract: Biphenyl derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.
    Type: Application
    Filed: October 12, 2006
    Publication date: May 15, 2008
    Inventors: Esther Martinborough, Danielle Lehsten, Timothy Neubert, Aarti Sameer Kawatkar, Nicole Zimmermann, Andreas Termin
  • Patent number: 7371750
    Abstract: 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: Grant
    Filed: July 29, 2004
    Date of Patent: May 13, 2008
    Assignee: IRM LLC
    Inventors: 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
  • Patent number: 7368569
    Abstract: This invention relates to a process for making spirolactone compounds analogous to formula I
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: May 6, 2008
    Assignees: 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
  • Publication number: 20080064872
    Abstract: 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: Application
    Filed: September 6, 2007
    Publication date: March 13, 2008
    Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Xiaoxia Liu
  • Patent number: 7326706
    Abstract: 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: Grant
    Filed: August 12, 2004
    Date of Patent: February 5, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bruce A. Ellsworth, Chongqing Sun, Annapurna Pendri
  • Patent number: 7304072
    Abstract: 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: Grant
    Filed: August 23, 2004
    Date of Patent: December 4, 2007
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takehiro Fukami, Akio Kanatani, Akane Ishihara, Yasuyuki Ishii, Toshiyuki Takahashi, Yuji Haga, Toshihiro Sakamoto, Takahiro Itoh, Masato Chiba
  • Patent number: 7304063
    Abstract: 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: Grant
    Filed: April 20, 2004
    Date of Patent: December 4, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Craig W. Lindsley, Zhijian Zhao
  • Patent number: 7271167
    Abstract: 1,2,4-Triazin-5-ones useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
    Type: Grant
    Filed: October 9, 2003
    Date of Patent: September 18, 2007
    Assignee: Cytokinetics, Inc.
    Inventors: Xiangping Qian, Gustave Bergnes, David J. Morgans, Jr.
  • Patent number: 7262200
    Abstract: 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: Grant
    Filed: October 27, 2003
    Date of Patent: August 28, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Alex Aronov, David J. Lauffer, Huan Qui Li, Ronald Charles Tomlinson, Pan Li
  • Patent number: 7259163
    Abstract: 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: Grant
    Filed: October 30, 2002
    Date of Patent: August 21, 2007
    Assignee: Glaxo Group Limited
    Inventors: 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
  • Publication number: 20070185113
    Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 29, 2007
    Publication date: August 9, 2007
    Inventors: Christoph Faeh, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Philippe Pflieger
  • Patent number: 7235657
    Abstract: 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: Grant
    Filed: June 27, 2005
    Date of Patent: June 26, 2007
    Assignee: Pfizer Inc.
    Inventor: Zhengong Bryan Li
  • Patent number: 7230100
    Abstract: 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: Grant
    Filed: April 7, 2006
    Date of Patent: June 12, 2007
    Assignee: Shire BioChem., Inc.
    Inventor: Qing Yu
  • Patent number: 7223759
    Abstract: 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: Grant
    Filed: September 15, 2004
    Date of Patent: May 29, 2007
    Assignee: 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
  • Patent number: 7220783
    Abstract: 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: Grant
    Filed: November 12, 2003
    Date of Patent: May 22, 2007
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenji Kawada, Mitsuaki Ohtani, Ryuji Suzuki, Akinori Arimura
  • Patent number: 7214677
    Abstract: 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: Grant
    Filed: November 12, 2002
    Date of Patent: May 8, 2007
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventors: Allen J. Duplantier, Chakrapani Subramanyam
  • Patent number: 7192959
    Abstract: 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: Grant
    Filed: April 21, 2004
    Date of Patent: March 20, 2007
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 7189719
    Abstract: 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: Grant
    Filed: April 21, 2004
    Date of Patent: March 13, 2007
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 7176202
    Abstract: 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: Grant
    Filed: October 27, 2005
    Date of Patent: February 13, 2007
    Assignee: Pfizer Inc.
    Inventors: Mark A. Dombroski, Allen J. Duplantier
  • Patent number: 7160886
    Abstract: 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: Grant
    Filed: February 27, 2004
    Date of Patent: January 9, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, Liangqin Guo, Qingmei Hong, Ravi P. Nargund, Patrick G. Pollard, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye
  • Patent number: 7157464
    Abstract: 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: Grant
    Filed: June 11, 2003
    Date of Patent: January 2, 2007
    Assignee: Chemocentryx, Inc.
    Inventors: Andrew M. K. Pennell, James B. Aggen, J.J. Kim Wright, Subrabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
  • Patent number: 7135471
    Abstract: 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 AIDS
    Type: Grant
    Filed: May 16, 2003
    Date of Patent: November 14, 2006
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Norbert Beier, Pierre Schelling, Michael Wolf
  • Patent number: 7129241
    Abstract: 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 AIDS
    Type: Grant
    Filed: May 12, 2003
    Date of Patent: October 31, 2006
    Assignee: Merck Patent Gesellschaft
    Inventors: Hans-Michael Eggenweiler, Michael Wolf
  • Patent number: 7109334
    Abstract: 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: Grant
    Filed: June 14, 2002
    Date of Patent: September 19, 2006
    Assignee: Shire BioChem, Inc.
    Inventor: Qing Yu
  • Patent number: 7101915
    Abstract: 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: Grant
    Filed: July 30, 1997
    Date of Patent: September 5, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenji Kawada, Mitsuaki Ohtani, Ryuji Suzuki, Akinori Arimura
  • Patent number: 7078403
    Abstract: 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: Grant
    Filed: June 16, 2000
    Date of Patent: July 18, 2006
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Wen-Yang Wu, Keith Watson, Darryl McConnell, Betty Jin, Guy Krippner
  • Patent number: 7074836
    Abstract: 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: Grant
    Filed: November 12, 2003
    Date of Patent: July 11, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenji Kawada, Mitsuaki Ohtani, Ryuji Suzuki, Akinori Arimura