Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Diazine Ring Patents (Class 544/406)
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Patent number: 7642263Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and prodrugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: GrantFiled: September 2, 2008Date of Patent: January 5, 2010Assignee: AstraZeneca ABInventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20090324540Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: ApplicationFiled: June 10, 2009Publication date: December 31, 2009Applicant: Emisphere Technologies, Inc.Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
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Publication number: 20090318473Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.Type: ApplicationFiled: February 11, 2009Publication date: December 24, 2009Inventors: Jean-Michel Altenburger, Valerie Fossey, Gilbert Lassalle, Frederic Petit, Jean Claude Vernieres, Philip Janiak
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Patent number: 7629346Abstract: The present invention relates to compounds of the formula I: wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.Type: GrantFiled: May 30, 2007Date of Patent: December 8, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Paul Hebeisen, Hans Iding, Matthias Heinrich Nettekoven, Ulrike Obst Sander, Stephan Roever, Urs Weiss, Beat Wirz
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Publication number: 20090298853Abstract: DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is ?O; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or —O—; Y2 is —(CH2)r— wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or —O—; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.Type: ApplicationFiled: December 19, 2008Publication date: December 3, 2009Applicant: AstraZeneca ABInventors: Udo Andreas Bauer, Jonas Gunnar Barlind, Petra Johannesson, Jan Magnus Johansson, Alexander Tobias Noeske, Annika Ulrika Petersson, Alan Martin Birch, Roger John Butlin, Clive Green, Andrew Leach, Ragnar Hovland
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Patent number: 7622468Abstract: The present invention relates to tetrahydropyridine compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: December 16, 2003Date of Patent: November 24, 2009Assignee: Merck & Co. Inc.Inventors: Mark E. Fraley, Robert M. Garbaccio
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Publication number: 20090281069Abstract: The present invention relates to compounds of the formula; and their use in therapy.Type: ApplicationFiled: April 10, 2007Publication date: November 12, 2009Inventors: Daniel Kaspar Baeschlin, Garry Fenton, Kenji Namoto, Nils Ostermann, Richard Sedrani, Finton Sirockin
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Publication number: 20090281118Abstract: The present application describes selective ligands of formula (I) for neuronal nicotinic receptors (NNRs), more specifically for the ?4?2 NNR subtype, compositions thereof, and methods of using the same, wherein X, R1, X, R2, R3, L1, m, n, p, and q are defined in the specification.Type: ApplicationFiled: April 27, 2009Publication date: November 12, 2009Applicant: Abbott LaboratoriesInventors: William H. Bunnelle, Lei Shi, Marc J.C. Scanio
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Publication number: 20090270421Abstract: Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having Ki's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an ?-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other ?-unsaturation corresponding to the arachidonyl ?8,9/?11,12 and/or oleyl ?9,10 positions. A preferred ?-keto heterocylic head group is ?-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).Type: ApplicationFiled: April 24, 2009Publication date: October 29, 2009Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20090270417Abstract: Novel 3,4-di-, 3,3,4-di-, 3,4,4,-tri- and 3,3,4,4-tetra-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described.Type: ApplicationFiled: June 11, 2007Publication date: October 29, 2009Applicant: NOVARTIS AGInventors: Juergen Klaus Maibaum, Edwige Liliane Jeanne Lorthiois, Peter Buehimayer
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Patent number: 7608618Abstract: Compounds of the formula wherein: Y? is O or S, W? is optionally substituted, Z? is selected from the group consisting of wherein Q? is OR7 and R7 is C1-3alkyleneC3-8heterocycloalkyl useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division also are disclosed.Type: GrantFiled: April 27, 2005Date of Patent: October 27, 2009Assignee: Icos CorporationInventors: Edward A. Kesicki, John Joseph Gaudino, Adam Wade Cook, Scott Douglas Cowen, Laurence Edward Burgess
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Patent number: 7598241Abstract: Novel compounds of the formula (I) in which R1, D, X, W, Y and T have the meaning indicated in Patent Claim (1), e.g. (II), are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.Type: GrantFiled: January 8, 2004Date of Patent: October 6, 2009Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christoph van Amsterdam
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Patent number: 7598236Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: December 15, 2007Date of Patent: October 6, 2009Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20090247550Abstract: The present invention relates to pyrazine derivatives of the formula and pharmaceutically acceptable salts thereof, wherein R1 to R8 are as defined in the description and claims for use as HDL-cholesterol raising agents in the treatment and/or prophylaxis of diseases or disorders that can be treated with such agents such as dyslipidemia.Type: ApplicationFiled: March 16, 2009Publication date: October 1, 2009Inventors: Paul Hebeisen, Constantinos G. Panousis, Stephan Roever, Matthew Wright
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Patent number: 7595321Abstract: The present invention relates to new compounds of formula (I) wherein Z is N; Y is CONR5, NR5CO, SO2NR5, NR5SO2, CH2NR5, NR5, NR5CONR5, CH2CO, CO, O or CH2O; X is CH or N; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S and said phenyl ring or 5 or 6 membered heteroaromatic ring may optionally be fused with a 5 or 6 membered saturated, partially saturated or unsaturated ring containing one or more atoms selected from C, N, O or S; Q is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, such as provide compounds having a selective inhibiting effect at GSK3.Type: GrantFiled: December 15, 2003Date of Patent: September 29, 2009Assignee: AstraZeneca ABInventors: Stefan Berg, Sven Hellberg
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Patent number: 7585853Abstract: The present invention relates to new compounds of formula (I) wherein: Z is N and X is CH or N; Y is CONR5; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S; Q is phenyl or a 5 or 6 membered aromatic heterocyclic ring containing one or more nitrogen atoms; R is C1-6alkylNR10R11 or C1-6alkylazetidine; R10 is hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C0-6alkylC3-6cycloalkyl, C0-6alkylaryl, C0-61alkylheteroaryl or C1-6alkylNR8R9; R11 is C1-6alkylNR8R9, C0-6alkylC3-6cycloalkyl or C0-6alkylheterocycloalkyl; as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.Type: GrantFiled: December 15, 2003Date of Patent: September 8, 2009Assignee: AstraZeneca ABInventors: Stefan Berg, Sven Hellberg, Peter Soderman
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Publication number: 20090192172Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: ApplicationFiled: December 8, 2005Publication date: July 30, 2009Applicant: Bayer Cropscience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Herbert Gayer, Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Patent number: 7560462Abstract: Substituted urea compounds useful in the treatment of diseases and C1-3alkyleneOR3 conditions related to DNA damage or lesions in DNA replication are disclosed formula (I), wherein X1 is null, —O—, —S—, —CH2—, or —N(R1)—; X2 is —O—, . -£>. -, or —N(R1)—,—. . Y xs 0 or S; or =y represents two hydrogen atoms attached to a common carbon atom, —W is selected from the group consisting of heteroaryl, aryl, heterocycloalkyl, cycloalkyl, and C1-6alkyl substituted with a heteroaryl. or aryl group; R6 is —C?C—R7 or heteroaryl; R8, R9, and R10, independently, are selected from the group consisting of halo, optionally substituted C1-6alkyl, C2-6alkenyl, C2-6alkynyl, OCP3, CF3, NO2, CN, NC, N(R3)2, OR3, CO2R3, C(O)N (R3)2, C(O)R3, N(R1)COR3, N(R1)C(O)OR3, N(R8)C(O)OR3, N(R1)C(O)C1-3alkyleneC(O)R3, N(R1)C(O)C1 -3alkyleneC(O)OR3, N(R1)C(O)C1-3alkyleneOR3, N(R1)C(O)C1-3alkyleneNHC(O)OR3, N(R1)C(O)C1-3alkyleneSO2.Type: GrantFiled: July 1, 2005Date of Patent: July 14, 2009Assignee: ICOS CorporationInventors: John Joseph Gaudino, Adam Wade Cook
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Publication number: 20090156616Abstract: The present invention relates to compounds of formula (I) and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: July 17, 2006Publication date: June 18, 2009Inventors: Jonas Bostrom, Leifeng Cheng, Roine Olsson
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Publication number: 20090143409Abstract: The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in the description.Type: ApplicationFiled: February 6, 2009Publication date: June 4, 2009Inventors: Mirjana Andjelkovic, Agnes Benardeau, Evelyne Chaput, Paul Hebeisen, Matthias Nettekoven, Ulrike Obst Sander, Constantinos G. Panousis, Stephan Roever
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Patent number: 7524957Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).Type: GrantFiled: February 1, 2008Date of Patent: April 28, 2009Assignee: AstraZeneca ABInventors: Scott Boyd, Peter William Rodney Caulkett, Rodney Brian Hargreaves, Suzanne Saxon Bowker, Roger James, Clifford David Jones, Darren McKerrecher, Michael Howard Block, Craig Johnstone
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Publication number: 20090076032Abstract: The present invention relates to novel derivatives of 18?-glycyrrhetinic acid and methods of synthesising the derivatives. Also included within the scope of the present invention are pharmaceutical compositions comprising the derivatives of the present invention and medical uses of the derivatives, including their use in inhibiting enzymes such as retinol dehydrogenases. The present invention also relates to methods of treating diseases, such as hyperproliferative diseases, neoplasms, cancers and photoageing.Type: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Inventors: Simon Ward, Alice Macgowan, Stanley Roberts, Jenny Littlechild, Kirsty Line, Ed Irving, Sam Donnelly
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Publication number: 20090076031Abstract: The present application describes deuterium-enriched bortezomib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090022688Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt, or mixtures thereof, that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are useful as antiviral agents. The invention further relates to pharmaceutically acceptable compositions comprising said compounds either for ex vivo use or for administration to a patient suffering from HCV infection and processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a pharmaceutical composition comprising a compound of this invention.Type: ApplicationFiled: July 8, 2008Publication date: January 22, 2009Inventors: Luc J. Farmer, Robert B. Perni, Govinda Rao Bhisetti, Keith P. Wilson
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Publication number: 20080293717Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 2, 2008Publication date: November 27, 2008Applicant: CHEMOCENTRYX, INC.Inventors: SOLOMON UGASHE, Zheng Wei, J.J. Wright, Andrew Pennell
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Publication number: 20080280873Abstract: Biaryl substituted pyrazinone compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: March 25, 2005Publication date: November 13, 2008Inventors: Jun Liang, Prasun K. Chakravarty, Deborah E. Pan, William H. Parsons, Pengcheng P. Shao, Feng Yee, Bishan Zhou
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Publication number: 20080262230Abstract: Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.Type: ApplicationFiled: March 29, 2006Publication date: October 23, 2008Applicant: Nippon Zoki Pharmaceutical Co., LTD.Inventors: Kunihiko Higashiura, Takashi Ogino, Kazuhito Furukawa
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Publication number: 20080255095Abstract: A compound of the formula (I): wherein R1 is C1-C6 alkyl, amino, (C1-C6 alkyl)amino, di(C1-C6 alkyl)amino or a nitrogen-containing saturated heterocyclic; R2 and R3 are hydrogen or C1-C6 alkyl; Arom is phenyl, idenyl, napthyl, phenanthrenyl, furyl, thiolyl, pyrrolyl, azepinyl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, 1,2,3 oxadiazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or quinolyl; A is C1-C6 alkylene; Ra is hydrogen, C1-C6 alkyl or C2-C6 alkenyl; E is a single bond, oxygen, sulfur or —NR4—, wherein R4 is hydrogen or C1-C7 alkanoyl; X1 and X2 are oxygen or sulfur; or a pharmacologically acceptable salt or ester thereof.Type: ApplicationFiled: June 18, 2007Publication date: October 16, 2008Applicant: BTG INTERNATIONAL LIMITEDInventors: Kazuo Koyama, Shinji Marumoto, Narihiro Toda, Hiroshi Kogen, Keiko Suzuki
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Publication number: 20080207638Abstract: The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis.Type: ApplicationFiled: July 17, 2006Publication date: August 28, 2008Inventors: Rachael Ann Ancliff, Mark James Bamford, Simon Teanby Hodgson, Christopher Allan Parr, Panayiotis Alexandrou Procopiou, David Matthew Wilson, Michael Woodrow
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Publication number: 20080200476Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: April 7, 2008Publication date: August 21, 2008Applicant: PARION SCIENCES, Inc.Inventor: Michael R. JOHNSON
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Publication number: 20080194585Abstract: Compounds of Formula 1, and their N-oxides and agriculturally suitable salts, are disclosed as useful as fungicides (INSERT FORMULA I HERE) wherein R1 is NR4R5, N?CR19R21, OR6, G1 or G2; or C1-C8 alkyl, C2-C8 alkenyl, each optionally substituted; A is O, S or NR7; R2 is cyano, NR8 N?CR9R10, NC(?O)R30; or a 5- or 6-membered heteroaromatic ring, each ring or ring system optionally substituted; R?3? is H, halogen, cyano, C1-C6 alkyl; J is C1-C8 alkyl or phenyl, optionally substituted; and R4, R5, R6, R7, R8, R9, R10, R19, R21, R30, G and G2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula 1.Type: ApplicationFiled: February 14, 2006Publication date: August 14, 2008Inventors: Paula Louise Sharpe, Thomas Martin Stevenson, James Francis Bereznak, Ritesh Sheth, Andrew Edmund Taggi, Chip-Ping Tseng, Wenming Zhang
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Publication number: 20080176863Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: March 17, 2008Publication date: July 24, 2008Applicant: PARION SCIENCES, Inc.Inventors: Michael R. JOHNSON, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
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Publication number: 20080161325Abstract: The present invention relates to compounds of formula (AA) (I) and (X): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: November 13, 2007Publication date: July 3, 2008Inventors: Yvette M. Fobian, John N. Freskos, Barbara Jagodzinska
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Publication number: 20080153843Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: September 28, 2007Publication date: June 26, 2008Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie REICH, Stefan SCHUNK, Sabine HEES, Ruth JOSTOCK, Michael Franz-Martin ENGELS, Achim KLESS, Thomas CHRISTOPH, Klaus SCHIENE, Tieno GERMANN, Edward BIJSTERVELD
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Patent number: 7388008Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.Type: GrantFiled: August 2, 2004Date of Patent: June 17, 2008Assignee: Ambrilia Biopharma Inc.Inventors: Brent Richard Stranix, Valérie Perron
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Publication number: 20080132507Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.Type: ApplicationFiled: October 13, 2005Publication date: June 5, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Richard Clark, Shinsuke Hirota, Hiroshi Azuma, Kazunobu Kira, Nobuhisa Watanabe, Tadashi Nagakura, Tatsuo Horizoe
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Patent number: 7378421Abstract: Novel compounds of the formula I in which R1, R2, R3 and Het are as defined herein, which are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.Type: GrantFiled: April 28, 2004Date of Patent: May 27, 2008Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Teresa Mujica-Fernaud, Herwig Buchholz, Wilfried Rautenberg, Christian Sirrenberg
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Publication number: 20080108632Abstract: This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat hepatitis C virus infection.Type: ApplicationFiled: November 2, 2007Publication date: May 8, 2008Applicant: TaiGen Biotechnology Co., Ltd.Inventors: Chu-chung Lin, Pei-chin Cheng, Yo-chin Liu, Chen-fu Liu, Chi-Hsin Richard King
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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: 7342019Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, in which R1 and R2 independently represent: a C1-6alkyl group; an optionally substituted (amino)C1-4alkyl-group; an optionally substituted non-aromatic C3-15carbocyclic group; a (C3-12cycloalkyl)C1-3alkyl-group; a group —(CH2)r(phenyl)s in which r is 0, 1, 2, 3 or 4, s is 1 when r is 0 otherwise s is 1 or 2 and the phenyl groups are optionally independently substituted by Z; naphthyl; anthracenyl; an optionally substituted saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following: oxygen, sulphur or an additional nitrogen; 1-adamantylmethyl; a group —(CH2)t Het in which t is 0, 1, 2, 3 or 4, and the alkylene chain is optionally substituted and Het represents an optionally substituted aromatic heterocycle; or R1 represents H and R2 is as defined above; or R1 and R2 together with the nitrogen atom to which they are attaType: GrantFiled: December 18, 2002Date of Patent: March 11, 2008Assignee: AstraZeneca ABInventors: Anna Ingrid Kristina Berggren, Stig Jonas Boström, Stig Thomas Elebring, Peter Greasley, Emma Terricabras, Johan Michael Wilstermann
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Publication number: 20080051578Abstract: The present invention relates to compounds of general formula (I) wherein A, B, L, R1, R2, R3a and R3b are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: August 24, 2006Publication date: February 28, 2008Inventors: Georg Dahmann, Kai Gerlach, Roland Pfau, Henning Priepke, Wolfgang Wienen, Annette Schuler-Metz, Herbert Nar
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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: 7319100Abstract: Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): Such compounds are particularly useful as CRF receptor ligands, and hence, in the treatment of various neurologically-related disorders such as affective disorder, anxiety and depression.Type: GrantFiled: February 14, 2007Date of Patent: January 15, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Argyrios G. Arvanitis, Paul J. Gilligan, Richard A. Hartz
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Publication number: 20070293509Abstract: The present invention relates to compounds of the formula I: wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.Type: ApplicationFiled: May 30, 2007Publication date: December 20, 2007Inventors: Paul Hebeisen, Hans Iding, Matthias Heinrich Nettekoven, Ulrike Obst Sander, Stephan Roever, Urs Weiss, Beat Wirz
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Publication number: 20070254895Abstract: Provided is a crystalline IPA solvate of 2(R)-(3-Chloro-4-methanesulfonyl-phenyl)-3-((R)-3-oxo-cyclopentyl)-N-pyrazin-2-yl-propionamide as a glucokinase activator which increases insulin secretion in the treatment of, for example, type II diabetes.Type: ApplicationFiled: April 11, 2007Publication date: November 1, 2007Inventors: Duk Soon Choi, Hitesh Parmendra Chokshi, Ahmad Waseem Malick, Roumen Nikolaev Radinov
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Publication number: 20070244129Abstract: Provided is a process for the preparation of 2(R)-(3-Chloro-4-methanesulfonyl-phenyl)-3-((R)-3-oxo-cyclopentyl)-N-pyrazin-2-yl-propionamide and its isopropanol solvate as a glucokinase activator which increases insulin secretion in the treatment of, for example, type II diabetes.Type: ApplicationFiled: April 11, 2007Publication date: October 18, 2007Inventors: Andrzej Robert Daniewski, Wen Liu, Roumen Nikolaev Radinov
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Patent number: 7282502Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: March 28, 2006Date of Patent: October 16, 2007Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C. B. Harriman, Zhan Shi, Chen Shaowu
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Patent number: 7273868Abstract: 1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ?CH— or ?N—, Y is —NH—, —NR4—, —S—, —O—, —CH?N—, —N?CH—, —N?N—, —CH?CH—, etc., R1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R3 and a substituent in Y may be combined to form a lactone ring.Type: GrantFiled: November 4, 2003Date of Patent: September 25, 2007Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
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Patent number: 7273946Abstract: Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.Type: GrantFiled: January 5, 2005Date of Patent: September 25, 2007Assignee: Nicox S.A.Inventors: Eninnio Ongini, Valerio Chiroli, Francesca Benedini, Piero Del Soldato