Phthalazines (including Hydrogenated) Patents (Class 544/237)
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Publication number: 20090270617Abstract: 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A.Type: ApplicationFiled: July 10, 2009Publication date: October 29, 2009Applicant: KUDOS PHARMACEUTICALS LIMITEDInventors: Keith Allan Menear, Anthony Peter Ottridge, Derek John Londesbrough, Michael Raymond Hallett, Keith Raymond Mulholland, John David Pittam, David Dermot Patrick Laffan, Ian Woodward Ashworth, Martin Francis Jones, Janette Helen Cherryman
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Publication number: 20090264434Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: March 9, 2009Publication date: October 22, 2009Inventors: Steven Joseph Berthel, Nancy-Ellen Haynes, Robert Francis Kester, Lee Apostle McDermott, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Jefferson Wright Tilley
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Publication number: 20090253705Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: April 2, 2009Publication date: October 8, 2009Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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Publication number: 20090253906Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optType: ApplicationFiled: April 2, 2009Publication date: October 8, 2009Applicant: AMR TECHNOLOGY, INC.Inventors: Bruce F. MOLINO, Shuang LIU, Peter R. GUZZO, James P. BECK
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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: 20090239872Abstract: The present invention relates to a method of treating a warm-blooded animal, especially a human, having mesothelioma, especially malignant mesothelioma, comprising administering to said animal a therapeutically effective amount of a 4-pyridylmethyl-phthalazine derivative.Type: ApplicationFiled: April 29, 2009Publication date: September 24, 2009Inventor: John Arthur Hohneker
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Publication number: 20090221529Abstract: This invention relates to the design, synthesis and use of synthetic vitamin D and other steroidal analogs. It further relates to the therapeutic use of such analogs and their manufacture.Type: ApplicationFiled: December 12, 2006Publication date: September 3, 2009Applicant: Women's & Infants Hospital of Rhode IslandInventors: Laurent Brard, Satyan Kalkunde, Rakesh Kumar Singh
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Patent number: 7569574Abstract: The invention relates to new purine derivatives of general formula wherein R1 to R4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV), the preparation thereof, the use thereof for the prevention or treatment of diseases or conditions associated with an increased DPP-IV activity or capable of being prevented or alleviated by reducing the DPP-IV activity, particularly type I or type II diabetes mellitus, the pharmaceutical compositions containing a compound of general formula (I) or a physiologically acceptable salt thereof as well as processes for the preparation thereof.Type: GrantFiled: August 4, 2003Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Roland Maier, Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf, Michael Mark, Ralf R. H. Lotz
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Publication number: 20090192156Abstract: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; X and Y are selected from CH and CH, CF and CH, CH and CF and N and CH respectively; RC is selected from H, C1-4 alkyl; and R1 is selected from C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl, which groups are optionally substituted; or RC and R1 together with the carbon and oxygen atoms to which they are attached form a spiro-C5-7 oxygen-containing heterocyclic group, which is optionally substituted or fused to a C5-7 aromatic ring.Type: ApplicationFiled: January 22, 2009Publication date: July 30, 2009Inventors: Keith Allan MENEAR, Muhammad Hashim Javaid, Sylvie Gomez, Marc Geoffrey Hummersone, Carlos Fenandez Lence, Niall Morrison Barr Martin, David Alan Rudge, Craig Anthony Roberts, Kevin Blades
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Publication number: 20090186897Abstract: A compound of the formula (I): wherein RH represents one or more optional substituents on the fused cyclohexene ring; R1 is selected from H and halo; RN is selected from H and optionally substituted C1-10 alkyl; and 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-fused C5-7 carbocylic or heterocyclic ring.Type: ApplicationFiled: September 12, 2008Publication date: July 23, 2009Inventors: Muhammad Hashim JAVAID, Keith Allan Menear, Niall Morrison Barr Martin
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Publication number: 20090186155Abstract: An ink for ink-jet recording includes a luminescence marker which emits light by oxidization. It may be determined whether the ink for ink-jet recording is used for recording the ink-jet recorded object with a simple method such as an evaluation of luminescence by oxidation, without requiring a special equipment.Type: ApplicationFiled: January 21, 2009Publication date: July 23, 2009Applicant: BROTHER KOGYO KABUSHIKI KAISHAInventor: Michiko Aoyama
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Publication number: 20090187018Abstract: The present invention provides an improved process of preparing hydralazine hydrochloride, which involves the preparation of 1-chlorophthalazine salt and further reacting with hydrazine followed by purification of hydralazine hydrochloride, which is free of phosphate, does not contain any individual impurities more than 0.05%, total impurities less than 0.5%, and a hydrazine content of not more than 0.001 %, and preferably less than 0.0003%. One benefit of improved purity is enhanced storage stability.Type: ApplicationFiled: April 3, 2009Publication date: July 23, 2009Applicant: Navinta LLCInventors: Christopher N. Jobdevairakkam, Jayaraman Kannappan, Jagadeesh B. Rangisetty
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Patent number: 7560450Abstract: The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: November 18, 2003Date of Patent: July 14, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Roland Maier, Michael Mark, Mohammad Tadayyon
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Patent number: 7560551Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R1-8 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.Type: GrantFiled: January 18, 2007Date of Patent: July 14, 2009Assignee: Amgen Inc.Inventors: Victor J. Cee, Hanh Nho Nguyen, Karina Romero
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Publication number: 20090163501Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: ApplicationFiled: February 12, 2009Publication date: June 25, 2009Applicant: Amgen Inc.Inventors: Victor J. Cee, Holly L. Deak, Bingfan Du, Stephanie D. Genus-Meyer, Brain L. Hodous, Han Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
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Publication number: 20090163477Abstract: A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, wherein: A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X?NRX then n is 1 or 2 and if X?CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or when X is CRXRY, RC1, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; R1 is selected from H and halo; and Het is selected from: where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N, where only one or two of Y1, Y2 and Y3 can be N;Type: ApplicationFiled: June 20, 2008Publication date: June 25, 2009Inventors: Muhammad Hashim Javaid, Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Sylvie Gomez, Vincent Junior Ming-lai Loh, Xiao-Ling Fan Cockcroft, Stefano Forte, Keith Allan Menear, Ian Timothy William Matthews, Frank Kerrigan
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Publication number: 20090131444Abstract: The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans.Type: ApplicationFiled: May 23, 2006Publication date: May 21, 2009Applicant: ASTRAZENECA ABInventors: Folkert Reck, Marshall Morningstar, Hajnalka Hartl
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Publication number: 20090124625Abstract: The present invention relates to novel compounds of formula (I) wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.Type: ApplicationFiled: June 17, 2005Publication date: May 14, 2009Applicant: Addex Pharmaceuticals SAInventors: Anne-Sophie Bessis, Christelle Bolea, Beatrice Bonnet, Mark Epping-Jordan, Nicolas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
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Publication number: 20090124624Abstract: The invention concerns 1-amino-phthalazine derivatives of general formula (I): Wherein A, B, L, R, R1, R2, R3, R4, R5 and R7 are as defined herein. The invention also concerns the preparation of said compounds and their therapeutic use.Type: ApplicationFiled: April 7, 2008Publication date: May 14, 2009Applicant: SANOFI-AVENTISInventors: Jean Michel AUGEREAU, Gilles COURTEMANCHE, Michel GESLIN, Laurence SERVA
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Patent number: 7531653Abstract: The present invention provides an improved process of preparing hydralazine hydrochloride, which involves the preparation of 1-chlorophthalazine salt and further reacting with hydrazine followed by purification of hydralazine hydrochloride, which is free of phosphate, does not contain any individual impurities more than 0.05%, total impurities less than 0.5%, and a hydrazine content of not more than 0.001%, and preferably less than 0.0003%. One benefit of improved purity is enhanced storage stability.Type: GrantFiled: December 7, 2005Date of Patent: May 12, 2009Assignee: Navinta LLCInventors: Jagadeesh B. Rangisetty, Christopher N. Jobdevairakkam, Jayaraman Kannappan
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Patent number: 7531540Abstract: The compounds of formula I in which the given substituents have the meanings as given in the description, are novel effective PDE4 inhibitors.Type: GrantFiled: December 29, 2006Date of Patent: May 12, 2009Assignee: Nycomed GmbHInventors: Gerhard Grundler, Beate Schmidt, Geert Jan Sterk
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Publication number: 20090099175Abstract: The present invention if directed to certain cinnoline compounds that are PDE10 inhibitors, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDE10 enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: February 28, 2007Publication date: April 16, 2009Inventors: Mark P. Arrington, Allen T. Hopper, Richard D. Conticello, Truc M. Nguyen, Hans-Jurgen E. Hess, Carla Maria Gauss, Stephen A. Hitchcock
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Patent number: 7517983Abstract: The present invention describes a process to form hydrazides from the reaction of a hydrazine and a dicarboxylic, using a Lewis acid as a main reagent of the reaction. The reaction occurs in a safe reactional environment, utilizing smooth conditions, neither involving high temperatures nor high pressures, producing the desired products with high yields, between 90-95%. The invention also describes a kit for utilization of chemiluminescent substances, comprised of two solutions.Type: GrantFiled: November 25, 2004Date of Patent: April 14, 2009Assignee: Universidade Federal Do Rio De Janeiro-UFRGInventors: Cláudio Cerqueira Lopes, Rosângela Sabattini Capella Lopes, Jarí Nobrega Cardoso, Jacqueline Alves da Silva, Letícia Gomes Ferreira
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Publication number: 20090091240Abstract: Provided is a condensed ring-containing compound having a condensed dicyclic group having a specific structure and carbazolyl groups and/or indolyl groups, and further provided is an organic electroluminescent device in which an organic thin film layer comprising a single layer or plural layers having at least a light emitting layer is interposed between a cathode and an anode, wherein at least one layer in the above organic thin film layer contains the condensed ring-containing compound described above in the form of a single component or a mixed component, whereby a current efficiency and a heat resistance are high, and a lifetime is very long.Type: ApplicationFiled: October 19, 2005Publication date: April 9, 2009Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Kiyoshi Ikeda, Mitsunori Ito, Takashi Arakane
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Publication number: 20090076003Abstract: The invention relates to new phthalazine derivatives, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof alone or in combination with one or more other pharmaceutically active compounds for the treatment of a disease, especially of a disease that responds to the inhibition of tyrosine kinases, more especially the inhibition of the vascular endothelial growth factor (VEGF) receptor kinase, preferably the treatment of a proliferative disease, such as a tumour disease.Type: ApplicationFiled: June 18, 2008Publication date: March 19, 2009Inventors: Guido Bold, Paul William Manley
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Publication number: 20090069303Abstract: 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.Type: ApplicationFiled: November 14, 2008Publication date: March 12, 2009Applicant: 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: 20090069297Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D?, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.Type: ApplicationFiled: April 3, 2008Publication date: March 12, 2009Applicant: Amgen Inc.Inventors: Victor Cee, Holly Deak, Bingfan Du, Stephanie Geuns-Meyer, Brian L. Hodous, Zihao Hua, Mathew Martin, Isaac Marx, Hanh Nho Nguyen, Philip Olivieri, Kathleen Panter, Karina Romero, Laurie Schenkel, Ryan White
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Publication number: 20090048259Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer.Type: ApplicationFiled: June 23, 2008Publication date: February 19, 2009Applicant: Amgen Inc.Inventors: Richard J. Austin, Jacob Kaizerman, Brian Lucas, Dustin L. McMinn, Jay Powers
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Publication number: 20090048226Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1? converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), or interferon-?-(“IFN-?”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-? production and methods for treating interleukin-1, apoptosis-, and interferon-?-mediated diseases using the compounds and compositions of this invention.Type: ApplicationFiled: January 22, 2008Publication date: February 19, 2009Inventors: Marion W. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
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Publication number: 20090048443Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optType: ApplicationFiled: October 16, 2008Publication date: February 19, 2009Applicant: AMR TECHNOLOGY, INC.Inventors: Bruce F. MOLINO, Shuang LIU, Peter R. GUZZO, James P. BECK
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Patent number: 7491821Abstract: Compounds of formula 1 are modulators of P2X3 useful for the treatment of pain and genitourinary, gastrointestinal, and respiratory disorders: wherein R1 is —C(?S)CH3, pyridyl, pyrimidinyl, pyrazinyl, thiazolyl, furyl, furylcarbonyl, acetyl, or carbamoyl; R2a and R2b are independently H, methyl, or ethyl; R3 is H or methyl; Y is a bond, —(CR4R5)n— or —CR4?CR5—; wherein R4 and R5 are each independently H or methyl and n is 1 or 2; X is N or CH; A is phenyl, 5-membered heterocyclyl, or 6-membered heterocyclyl; R6, R7 and R8 are each independently H, halo, lower alkyl, cycloalkyl, alkylthio, alkylthio-lower alkyl, alkylsulfonyl-lower alkyl, di(lower alkyl)amino-lower alkyl, morpholinyl-lower alkyl, 4-methyl-piperazinyl-methyl, trifluoromethyl, pyridyl, tetrazolyl, thiophenyl, phenyl, biphenyl, or benzyl (where thiophenyl, phenyl and benzyl are substituted with 0-3 lower alkyl, halo, sulfonamido, trifluoromethyl, lower alkoxy or lower alkylthio) or R6 and R7 together form a 5-membered or 6-membered carbocyclType: GrantFiled: August 11, 2006Date of Patent: February 17, 2009Assignee: Roche Palo Alto LLCInventors: Christine E. Brotherton-Pleiss, Michael Patrick Dillon, Shelley K. Gleason, Clara Jeou Jen Lin, Ryan Craig Schoenfeld, Marzia Villa, Yansheng Zhai
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Publication number: 20090042879Abstract: The present invention provides a novel compound having an excellent PDE4 inhibitory activity and TNF-? production-suppressing activity, and also provides a preventive and therapeutic agent for atopic dermatitis or the like. The present invention includes a novel phthalazinone derivative of the following general structural formula [1] or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising it as an active ingredient. In the structural formula [1], the partial structure bridging the 6-position and the 7-position represents a single bond or a double bond; R1 and R2 are the same or different and each represents alkyl or the like; Y represents phenylene or the like; Z represents alkylene or the like; and R3 represents a mono- to tri-cyclic saturated or unsaturated cyclic amino group or the like optionally substituted with R31 and R32, wherein R31 and R32 represent alkyl or the like.Type: ApplicationFiled: April 21, 2006Publication date: February 12, 2009Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Kohei Kagayama, Xin Zhang
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Publication number: 20090035267Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof, which can inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.Type: ApplicationFiled: July 31, 2007Publication date: February 5, 2009Inventors: Joel D. Moore, Datong Tang, Yat Sun Or, Zhe Wang
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Patent number: 7485641Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.Type: GrantFiled: June 18, 2007Date of Patent: February 3, 2009Assignee: Pfizer, Inc.Inventors: David W. Piotrowski, Yu Hui, John W. Benbow
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Publication number: 20090023740Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.Type: ApplicationFiled: July 14, 2008Publication date: January 22, 2009Applicant: IcagenInventors: Alan Bradley Fulp, Matthew Scott Johnson, Christopher John Markworth, Brian Edward Marron, Darrick Conway Seconi, Christopher William West, Xiaodong Wang, Shulan Zhou
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Publication number: 20090023738Abstract: The present invention relates to diaminopyrimidines of the general formula I, process for their preparation, and the use thereof for the manufacture of pharmaceutical compositions for the treatment of disorders and indications connected with the EP2 receptor.Type: ApplicationFiled: June 19, 2008Publication date: January 22, 2009Inventors: Nico Braeuer, Bernd Buchmann, Marcus Koppitz, Antonius Ter Laak, Gernot Langer, Bernhard Lindenthal, Olaf Peters, Tim Wintermantel
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Publication number: 20090023727Abstract: A compound of the formula (I): wherein: R represents one or more optional substituents on the fused cyclohexene ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; if X=NRX, then RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted ester, optionally substituted acyl, and optionally substituted sulfonyl groups; if X=CRXRY then RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted sulfonamino, optionally substituted ether, optionally substituted ester, optionally substituted acyl, optionally substituted acylamido, and optionally substituted sulfonyl groups and RY is selected from H, hydroxy, optType: ApplicationFiled: July 3, 2008Publication date: January 22, 2009Inventors: Muhammad Hashim Javaid, Keith Allan Menear, Niall Morrison Barr Martin, Graeme Cameron Murray Smith, David Alan Rudge, Craig Anthony Roberts
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Patent number: 7476763Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I: methods for their production, pharmaceutical formulations containing these compounds, methods of producing such pharmaceutical formulations and related methods of treating or inhibiting certain diseases or conditions.Type: GrantFiled: November 9, 2006Date of Patent: January 13, 2009Assignee: Gruenenthal GmbHInventors: Corinna Sundermann, Bernd Sundermann
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Publication number: 20080318960Abstract: The present invention relates to compounds, and uses thereof, having the chemical formula: or a pharmaceutically acceptable salt or prodrug thereof, wherein the compound modulates the activity of PAR2 or a PAR2 subtype and thereby may be used to treat or prevent diseases involving abnormal PAR2 or PAR2 subtype activity.Type: ApplicationFiled: May 16, 2006Publication date: December 25, 2008Inventors: Ethan Burstein, Anne Eeg Knapp
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Publication number: 20080300243Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 24, 2006Publication date: December 4, 2008Inventors: Michael G. Kelly, John Kincaid, Matthew Duncton, Kiran Sahasrabudhe, Satyanarayana Janagani, Ravindra B. Upasani, Guoxian Wu, YunFeng Fang, Zhi-Liang Wei, Carl Kaub, Jianhua He
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Patent number: 7459564Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: GrantFiled: January 12, 2006Date of Patent: December 2, 2008Assignee: Bristol-Myers Squibb CompanyInventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. Pinto
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Patent number: 7456195Abstract: The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, Y, Z, R7, R8, R9, and R11 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: GrantFiled: June 22, 2006Date of Patent: November 25, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Xiaojun Zhang, Alexandra A. Nirschl, Yan Zou, Eldon Scott Priestley
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Publication number: 20080280909Abstract: Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning ?4 integrin in which ?4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection. wherein R1 is a methyl group and R2 is a methoxy group.Type: ApplicationFiled: June 25, 2007Publication date: November 13, 2008Applicant: Ajinomoto Co., Inc.Inventors: Tatsuya Okuzumi, Kazuyuki Sagi, Toshihiko Yoshimura, Yuji Tanaka, Eiji Nakanishi, Miho Ono, Masahiro Murata
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Publication number: 20080280910Abstract: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring or an optionally substituted, fused cyclohexene ring; D is selected from: where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N and Y4 is selected from CH and N; where Y1 is selected from CH and N and Y2 is selected from CH and N; where Q is O or S; and where Q is O or S; and RD is an optionally substituted C5-20 aryl group, bound to D by a carbon-carbon bond.Type: ApplicationFiled: March 19, 2008Publication date: November 13, 2008Inventors: Keith Allan Menear, Marc Geoffrey Hummersone, Sylvie Gomez, Muhammad Hashim Javaid, Niall Morrison Barr Martin, Frank Kerrigan
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Patent number: 7449464Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.Type: GrantFiled: June 24, 2004Date of Patent: November 11, 2008Assignees: Kudos Pharmaceuticals Limited, Maybridge LimitedInventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
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Publication number: 20080269234Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.Type: ApplicationFiled: June 12, 2008Publication date: October 30, 2008Applicant: ABBOTT LABORATORIESInventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
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Publication number: 20080261941Abstract: The present invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity.Type: ApplicationFiled: October 18, 2007Publication date: October 23, 2008Inventors: Lorraine Kathleen FAY, Douglas S. Johnson, Suzanne Ross Kesten, Scott E. Lazerwith, Mark Anthony Morris, Cory Michael Stiff, Marvin Jay Meyers, Lijuan Jane Wang
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Publication number: 20080261947Abstract: Fused pyridazine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof (wherein each symbol has the meaning as defined in the specification.). Because of inhibiting poly(ADP-ribose)polymerase, the compounds represented by formula (I) are useful as preventives and/or remedies for various ischemic diseases (in brain, cord, heart, digestive tract, skeletal muscle, retina, etc.), inflammatory diseases (inflammatory bowel disease, multiple cerebrosclerosis, arthritis, etc.), neurodegenerative diseases (extrapyramidal disorder, Alzheimer's disease, muscular dystrophy, lumbar spinal canal stenosis, etc.), diabetes, shock, head trauma, renal failure, hyperalgesia, etc. Moreover, these compounds are useful as agents against retroviruses (HIV etc.), sensitizers in treating cancer and immunosuppressants.Type: ApplicationFiled: June 11, 2008Publication date: October 23, 2008Inventors: Takuya Seko, Jun Takeuchi, Shinya Takahashi, Yoshihisa Kamanaka, Wataru Kamoshima
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Publication number: 20080255128Abstract: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; X is selected from H and F; R1 and R2 are independently selected from H and methyl; RN1 is selected from H and optionally substituted C1-7 alkyl; RN2 is selected from H, optionally substituted C1-7 alkyl, C3-7 heterocyclyl and C5-6 aryl; or RN1 and RN2 and the nitrogen atom to which they are bound form an optionally substituted nitrogen containing C5-7 heterocyclic group.Type: ApplicationFiled: April 10, 2008Publication date: October 16, 2008Inventors: Muhammad Hashim Javaid, Marc Geoffrey Hummersone, Keith Allan Menear, Sylvie Gomez, Niall Morrison Barr Martin
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Patent number: RE40793Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R1 and R2 taken together form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, —Alk—Y—C(?O)—R9, or —Alk—Y—C (?O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, or a heterocyclic ring-system; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, or a heterocyclic ringsystem; X is O, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, or C1-6alkyl; R11 and R12 each independType: GrantFiled: October 26, 2005Date of Patent: June 23, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean-Paul Renë Marie Andrë Bosmans, Michel Anna Jozef DeCleyn, Michel Surkyn