Isoquinolines (including Hydrogenated) Patents (Class 514/253.05)
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Patent number: 7763614Abstract: The present invention relates to compounds of structural formula I: I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: September 22, 2004Date of Patent: July 27, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Isaacs, Christopher J. Dinsmore, B. Wesley Trotter, Nigel Liverton, Douglas C. Beshore, Nathan R. Kett, Charles J. McIntyre, Kausik K. Nanda, David A. Claremon
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Publication number: 20100184650Abstract: Patients are subject to a post-seizure treatment regime to separately inhibitor consecutive targets of an epileptogenic cascade comprising neurotransmitter receptor signaling, kinase/phosphatase activity, protein translation, and apoptosis or inflammation.Type: ApplicationFiled: January 17, 2010Publication date: July 22, 2010Inventors: Frances E. Jensen, Sanjay N. Rakhade
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Publication number: 20100184750Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: January 18, 2010Publication date: July 22, 2010Applicant: ABBOTT LABORATORIESInventors: Laura A. Hexamer, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Michael D. Wendt
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Patent number: 7759351Abstract: The invention provides new oxazolidinone compounds of formula (I) wherein A is certain heterocycles optionally substituted; R1, R2, R3 and R4 are independently selected from —H and halogen; X is selected from O, S, NR9 and CR9R10; R9 and R10 having different meanings; Y is selected from O, S, SO, SO2, NO, NR12 and CR12R13; R12 and R13 having different meanings. It also provides different processes for the preparation of such compounds. Oxazolidinone compounds of formula (I) are active against Gram-positive and some Gram-negative human and veterinary pathogens with a weak monoamine oxidase (MAO) inhibitory activity. They are useful for the treatment of bacterial infections.Type: GrantFiled: June 26, 2006Date of Patent: July 20, 2010Assignee: Ferrer Internacional, S.A.Inventors: Montserrat Cano, Albert Palomer, Antonio Guglietta
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Patent number: 7754721Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, X, Y, Z, Ar, R1, R2, R3, R4, R5, R6 and R7 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: August 17, 2007Date of Patent: July 13, 2010Assignee: Roche Palo Alto LLCInventors: David Scott Carter, Ryan Craig Schoenfeld, Robert James Weikert
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Publication number: 20100144616Abstract: One aspect of the present application relates to a method for limiting damage to neuronal cells by ischemic or epoxic conditions, e.g., such as may be manifest by a reduction in brain infarct volume, by administering to an individual a hedgehog therapeutic or ptc therapeutic in an amount effective for reducing cerebral infarct volume.Type: ApplicationFiled: July 28, 2008Publication date: June 10, 2010Applicant: Curis, Inc.Inventor: Nagesh K. Mahanthappa
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Publication number: 20100137331Abstract: The present invention relates to compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: February 2, 2010Publication date: June 3, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Andreas Termin, Dean Wilson, Pramod Joshi
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Publication number: 20100137329Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.Type: ApplicationFiled: February 8, 2010Publication date: June 3, 2010Applicant: SANOFI-EVENTISInventors: Ahmed ABOUABDELLAH, Antonio Almario Garcia, Christian Hoornaert, Adrien Tak Li
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Publication number: 20100130469Abstract: The present invention relates to novel organic compounds comprising a naphthyridine which may be mediators of a selective subset of kinases belonging to the AGC kinase family, such as for example PKC, PKD, PKN-1/2, CDK-9, MRCK-beat, PASK, PRKX, ROCK-I/II or mediators of other kinases, the selectivity of which would be depending on the structural variation thereof.Type: ApplicationFiled: April 4, 2008Publication date: May 27, 2010Inventors: Maurice van Eis, Walter Schuler, Anette Von Matt, Nicolas Soldermann, Lauren G. Monovich, Christoph Gaul
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Publication number: 20100120769Abstract: The present invention relates to compounds of formula I wherein s, R1a and R1 to R3 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: January 20, 2010Publication date: May 13, 2010Inventors: Matthias Nettekoven, Jean-Marc ` Plancher, Olivier Roche, Tadakatsu Takahashi, Sven Taylor
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Publication number: 20100120759Abstract: The present invention provides a novel class of azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: January 21, 2010Publication date: May 13, 2010Applicant: Corcept Therapeutics, Inc.Inventors: Robin D. CLARK, Nicholas C. RAY, Paul BLANEY, Christopher HURLEY, Hazel HUNT, David CLARK, Karen WILLIAMS
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Publication number: 20100099676Abstract: A compound represented by the general formula (I): wherein R1 is wherein R26 and R28 are each independently lower alkyloxy and the like; n1 is an integer of 0 to 3; Z is a optionally substituted C1-C5 alkynylene which may be interrupted with a substituent selected from Substituent group a and the like; A is a group represented by the formula: wherein R6 and R7 are each independently lower alkyl and the like; m and n are each independently 0, 1, or 2; R2 is a hydrogen atom and the like; R3 is optionally substituted lower alkyl and the like; R4 is a hydrogen atom; or R3 and R4 may be taken together with an adjacent carbon atom to from a ring; R5 is hydroxyl and the like, or an optically active isomer, a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: October 31, 2007Publication date: April 22, 2010Applicant: SHIONOGI & CO., LTD.Inventors: Takeshi Endoh, Yasuhiko Fujii, Eiichi Kojima, Genta Tadano, Naoko Yamaguchi, Yo Adachi, Sachie Tagashira, Yuki Tachibana, Naohiro Onodera
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Publication number: 20100099665Abstract: The present invention relates to isoquinolinone derivatives of formula (I): wherein are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: October 1, 2009Publication date: April 22, 2010Applicant: AstraZeneca ABInventors: Stephen John BROUGH, Timothy Jon Luker, Bryan Glyn Roberts, Stephen Anthony St-Gallay
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Publication number: 20100099659Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y1, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.Type: ApplicationFiled: December 11, 2009Publication date: April 22, 2010Inventors: Joshua Kennedy-Smith, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel Mclntosh, Timothy D. Owens, Michael Soth, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
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Patent number: 7687503Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.Type: GrantFiled: June 22, 2006Date of Patent: March 30, 2010Assignee: Sanofi-AventisInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Adrien Tak Li
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Patent number: 7683066Abstract: The present invention relates to compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: May 15, 2006Date of Patent: March 23, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Andreas Termin, Dean Wilson, Pramod Joshi
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Publication number: 20100063060Abstract: A combination of a Rho kinase inhibitor and a prostaglandin as a therapeutic agent for treating glaucoma. The actions of reducing intraocular pressure are complemented and/or enhanced by combining a Rho kinase inhibitor with a prostaglandin. Each of the Rho kinase inhibitor and the prostaglandin can be administered in combination or in a mixture.Type: ApplicationFiled: October 16, 2009Publication date: March 11, 2010Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Tadashi Nakajima, Takeshi Matsugi, Hideaki Hara
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Publication number: 20100056518Abstract: The invention relates to 6-substituted isoquinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: ApplicationFiled: June 18, 2009Publication date: March 4, 2010Applicant: SANOFI-AVENTISInventors: Oliver PLETTENBURG, Armin HOFMEISTER, Katrin LORENZ, Joachim BRENDEL, Matthias Löhn, John Weston
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Publication number: 20100041671Abstract: A method for treating glaucoma comprising administering to a patient pharmaceutically effective amounts of a Rho kinase inhibitor and a prostaglandin.Type: ApplicationFiled: October 16, 2009Publication date: February 18, 2010Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Tadashi Nakajima, Takeshi Matsugi, Hideaki Hara
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Publication number: 20090306041Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables R, X, Y1, Y2, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.Type: ApplicationFiled: February 5, 2009Publication date: December 10, 2009Inventors: Nolan James Dewdney, Joshua Kennedy-Smith, Rama K. Kondru, Bradley E. Loc, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
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Publication number: 20090275537Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: August 11, 2008Publication date: November 5, 2009Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Bing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, JR.
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Publication number: 20090275514Abstract: Provided are compositions and methods of treating inflammation of the heart of a subject diagnosed with inflammation of the heart, comprising administering to the subject an effective amount of an inhibitor of Calmodulin Kinase II, whereby the administration of the inhibitor treats inflammation of the heart in the subject. Also provided are compositions and methods of preventing inflammation of the heart of a subject, comprising administering to the subject an effective amount of an inhibitor of Calmodulin Kinase II, whereby the administration of the inhibitor prevents inflammation of the heart in the subject.Type: ApplicationFiled: April 30, 2009Publication date: November 5, 2009Inventors: Mark E. Anderson, Madhu V. Singh
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Publication number: 20090238761Abstract: This invention provides novel aryl piperazine derivatives having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, D2-like and 5-HT2 receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders incl. schizophrenia.Type: ApplicationFiled: January 2, 2006Publication date: September 24, 2009Applicant: Universita Degli Studi Di SienaInventors: Giuseppe Campiani, Stefania Butini, Caterina Fattorusso, Francesco Trotta, Silvia Franceschini, Meri De Angelis, Karin Sandager Nielsen
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Publication number: 20090220570Abstract: Regenerative growth of an adult mammalian central nervous system neuron axon subject to growth inhibition by endogenous, myelin growth repulsion factors is promoted by delivering to the axon a therapeutically effective amount of a specific inhibitor of protein kinase C, whereby regenerative growth of the axon is promoted and a resultant promotion of the regenerative growth of the axon is detected.Type: ApplicationFiled: May 18, 2009Publication date: September 3, 2009Inventors: Zhigang He, Vuk Koprivica, Rajeev Sivasankanan
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Patent number: 7582638Abstract: The present invention provides kinase inhibitors of Formula (I) wherein R1, R2, and X are as described herein, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 23, 2006Date of Patent: September 1, 2009Assignee: Eli Lilly and CompanyInventors: Alfonso De Dios, Cristina Garcia-Paredes, Beatriz López de Uralde Garmendia, Mary Margaret Mader, Mark Andrew Pobanz, Chuan Shih, Boyu Zhong
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Publication number: 20090176798Abstract: The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.Type: ApplicationFiled: December 5, 2008Publication date: July 9, 2009Applicant: Biovitrum ABInventors: Joseph W. Boyd, Giles A. Brown, Michael Higginbottom
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Publication number: 20090143402Abstract: Isoquinolone derivatives of the general formula are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia.Type: ApplicationFiled: April 11, 2008Publication date: June 4, 2009Applicant: H. LUNDBECK A/SInventors: Klaus Baek Simonsen, Jan Kehler, Karsten Juhl, Nikolay Khanzhin, Soren Moller Nielsen
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Patent number: 7541357Abstract: 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 optiType: GrantFiled: July 15, 2005Date of Patent: June 2, 2009Assignee: AMR Technology, Inc.Inventors: Bruce F. Molino, Shuang Liu, Peter R. Guzzo, James P. Beck
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Publication number: 20090131451Abstract: The present application features the use of the somatostatin subtype 3 receptor (SST3) as a target for affecting insulin secretion and for diagnosing diabetes related disorders. Glucose stimulated insulin secretion was found to be stimulated by knocking down expression of SST3 and through the use of a SST3 selective antagonist.Type: ApplicationFiled: November 17, 2006Publication date: May 21, 2009Inventors: Yun-Ping Zhou, Jing Li, Weizhen Wu, Jin Shang, John R. Thompson, Nancy A. Thornberry
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Publication number: 20090118299Abstract: There is Provided an Agent for Prevention of glaucoma or an agent for prevention or treatment of ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. An agent for prevention or treatment of glaucoma comprising a Rho kinase inhibitor and a carbonic anhydrase inhibitor in combination.Type: ApplicationFiled: July 11, 2006Publication date: May 7, 2009Applicant: KOWA CO., LTD.Inventors: Ken Mizuno, Jiro Matsumoto
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Publication number: 20090099158Abstract: Certain substituted tetrahydroisoquinoline compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: ApplicationFiled: February 28, 2008Publication date: April 16, 2009Inventors: Cheryl A. Grice, Michael A. Letavic, Alejandro Santillan, JR., Kimberly L. Schwarz
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Publication number: 20090088429Abstract: The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: ApplicationFiled: December 20, 2007Publication date: April 2, 2009Applicant: SANOFI-AVENTISInventors: Oliver PLETTENBURG, Armin HOFMEISTER, Dieter KADEREIT, Stefan PEUKERT, Sven RUF, Kurt RITTER, Matthias LOEHN, Yuri IVASHCHENKO, Peter MONECKE, Matthias DREYER, Aimo KANNT
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Publication number: 20090082338Abstract: There is provided a preventive for glaucoma or a preventive or a remedy for ocular hypertension, with a potent ocular hypotensive effect and prolonged duration thereof. A preventive or a remedy for glaucoma comprising a Rho kinase inhibitor and an ?1 blocker in combination.Type: ApplicationFiled: June 20, 2006Publication date: March 26, 2009Applicant: Kowa Co., Ltd.Inventors: Ken Mizuno, Jiro Matsumoto
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Publication number: 20090075988Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides a process for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: ApplicationFiled: September 11, 2008Publication date: March 19, 2009Applicant: H. Lundbeck A/SInventors: Jan Kehler, Jacob Nielsen, Morten Langgaard
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Patent number: 7504395Abstract: A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans and the symptoms associated therewith, inattentiveness, and hyperactivity with impulsivity, using eltoprazine and related compounds is provided.Type: GrantFiled: July 19, 2002Date of Patent: March 17, 2009Assignee: Psychogenics, Inc.Inventors: Daniela Brunner, Daniel W. Goodman
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Publication number: 20090068144Abstract: The present invention provides a compound selected from compounds of formula I as ligand binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy. Compounds of formula (I) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events, heart valvular degenerative disease Moreover, compounds of formula (I) can be used to decrease the side effects from cytotoxic cancer agents and to treat viral infections.Type: ApplicationFiled: March 17, 2006Publication date: March 12, 2009Inventors: Lutz Weber, Vladimir Khazak, Gunther Ross, Cotic Kalinski, Chritoph Burdack
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Patent number: 7501412Abstract: The present invention relates to an isoquinoline compound represented by the following formula (I) or (II), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction.Type: GrantFiled: November 21, 2003Date of Patent: March 10, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masakazu Fujio, Hiroyuki Satoh, Shinya Inoue, Toshifumi Matsumoto, Yasuhiro Egi, Taichi Takahashi
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Publication number: 20090054434Abstract: The present invention is directed to certain isoquinolin-1(2H)-one compounds, useful as PDE10 inhibitors, having the formula: where R1, R2, R3, R4 and R5 are as defined herein, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: August 22, 2008Publication date: February 26, 2009Applicants: Amgen Inc., Memory Pharmaceuticals Corp.Inventors: Essa Hu, Roxanne Kunz, Ning Chen, Ruiping Liu
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Publication number: 20090054453Abstract: The present invention relates to new compounds of formula I, or salts, solvates or solvated salts thereof, wherein Q, R1, R2, R3, R4 and n are defined as in claim 1, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.Type: ApplicationFiled: March 15, 2007Publication date: February 26, 2009Inventors: Lilian Alcaraz, Gunnar Nordvall, Didier Rotticci, Daniel Sohn
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Publication number: 20090048223Abstract: A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; G3 represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkoxycarbonyl group, an acyl group, an acyloxy group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Y represents a single bond, or —C(R3)(R4)— (R3 and R4 represent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); G4 represents hydroType: ApplicationFiled: February 27, 2008Publication date: February 19, 2009Applicant: Asahi Kasei Pharma CorporationInventors: Koki Matsubara, Atsushi Iesato, Akifumi Oomura, Koh Kawasaki, Rintaro Yamada, Minoru Seto
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Publication number: 20090036465Abstract: Methods for treatment of pulmonary hypertension include administration of a first amount of treprostinil and administration of a second amount of a Rho kinase inhibitor such that the first amount and the second amount form together an amount effective for pulmonary hypertension treatment. Kits for treatment pulmonary hypertension are also disclosed.Type: ApplicationFiled: October 17, 2007Publication date: February 5, 2009Inventors: Robert ROSCIGNO, Eugene SULLIVAN
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Publication number: 20090029987Abstract: The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.Type: ApplicationFiled: July 28, 2006Publication date: January 29, 2009Applicant: RESVERLOGIX CORP.Inventors: Norman C.W. Wong, Henrik C. Hansen, Fabrizio S. Chiacchia, Jan O. Johansson
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Publication number: 20090023746Abstract: The present invention relates to isoquinolinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: April 4, 2008Publication date: January 22, 2009Applicant: AstraZeneca ABInventors: Matthew Hallam, Barrie Martin, Piotr Raubo, Bryan Roberts, Stephen St-Gallay, Paul Willis
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Patent number: 7476671Abstract: The present invention relates to 2-amino-imidazo[4,5-d]pyridazin-4-ones and 2-amino-imidazo[4,5-c]pyridin-4-ones of general formula wherein R1 to R4 and X are defined as in claims 1 to 6, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: December 12, 2006Date of Patent: January 13, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Norbert Hauel, Mohammad Tadayyon, Leo Thomas
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Publication number: 20080318948Abstract: The present invention provides compounds of the formula which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, type 2 diabetes and obesity.Type: ApplicationFiled: September 28, 2006Publication date: December 25, 2008Inventor: Gregory Raymond Bebernitz
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Patent number: 7449477Abstract: The present invention relates to compounds Formula (I) as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.Type: GrantFiled: November 22, 2004Date of Patent: November 11, 2008Assignee: Eli Lilly and CompanyInventors: David Anthony Barda, Kenneth James Henry, Jr., Jianping Huang, Sajan Joseph, Ho-Shen Lin, Michael Enrico Richett
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Publication number: 20080275056Abstract: The present invention provides kinase inhibitors of Formula (I) wherein R1, R2, and X are as described herein, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 23, 2006Publication date: November 6, 2008Inventors: Alfonso De Dios, Cristina Garcia-Paredes, Beatriz Lopez Uralde Garmendia, Mary Margaret Mader, Mark Andrew Pobanz, Chuan Shih, Boyu Zhong
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Publication number: 20080269243Abstract: The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: ApplicationFiled: March 19, 2008Publication date: October 30, 2008Applicant: Amgen Inc.Inventors: Holger Monenschein, G. Erich Wohlhieter, Qingping Zeng
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Publication number: 20080267870Abstract: Racemic mixtures and enantiomerically pure forms of novel 1-[(2?-substituted)-piperazin-1?-yl]-isoquinolines are norepinephrine (NE) transporter (NET) inhibitor compounds. Compounds of the invention are considered therapeutic agents for central nervous system (CNS) diseases and disorders, without limitation, including neurodegeneration, anxiety, depression, attention deficit disorders, drug dependency, and post traumatic stress disorder. Examples of the chemical syntheses of the compounds of the invention are provided. The isoquinoline compounds of the invention competitively bind at NET at nanomolar concentrations. The isoquinoline agents of the invention bind selectively to NET over other competitive transporter targets and receptor binding sites, including those of serotonin and dopamine, amongst others. The chemical syntheses of the invention are suitable for labeling with radionuclide atoms.Type: ApplicationFiled: March 21, 2008Publication date: October 30, 2008Inventors: John M. Gerdes, David B. Bolstad, Michael R. Braden, August W. Barany
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Patent number: 7442710Abstract: The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R? and R1, R2,R3, R4, R5, and R6 are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used for the treatment of diseases related to the glycine transporter inhibitor, such as schizophrenia and Alzheimer's disease.Type: GrantFiled: January 24, 2006Date of Patent: October 28, 2008Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard