The Diazine Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/115)
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Patent number: 7893049Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R6 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: April 5, 2007Date of Patent: February 22, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Darryl McConnell, Bodo Betzemeier, Thomas Gerstberger, Maria Impagnatiello, Steffen Steurer, Lars van der Veen, Ulrike Weyer-Czernilofsky
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Publication number: 20110021511Abstract: The invention relates to compounds of general formula 1 to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts and/or solvates which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as inductors of apoptosis in the case of non-solid malignant tumors of the hematopoietic system, in particular in the case of leukemias and lymphomas, more particularly in the case of leukemic B lymphocytes.Type: ApplicationFiled: December 21, 2007Publication date: January 27, 2011Applicant: THE MEDICINES COMPANY (LEIPZIG) GMBHInventors: Claudia Reichelt, Alexander Schulze, Mohammed Daghish, Friedrich-Alexander Ludwig, Jochen Heinicke, Konrad Herrmann, Maj Schuster, Sven Letschert, Kenneth Mugridge, Joseph DeAngelo
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Publication number: 20110021519Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: June 8, 2010Publication date: January 27, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, David Kay, Ronald Knegtel
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Publication number: 20110021493Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.Type: ApplicationFiled: September 2, 2008Publication date: January 27, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Hartmut Schirok, Ying Li-Sommer, Michael Brands, Mario Lobell, Adrian Tersteegen, Herbert Himmel, Karl-Heinz Schlemmer, Dieter Lang, Kirsten Petersen, Matthias Renz, Dominik Mumberg, Jens Hoffman, Gerhard Siemeister, Ulf Bömer
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Publication number: 20110003786Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.Type: ApplicationFiled: July 2, 2010Publication date: January 6, 2011Inventors: Robin Alec FAIRHURST, Marc GERSPACHER, Robert MAH
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Patent number: 7851472Abstract: The compounds of formula I in which R1 and R2 have the meanings as given in the description are novel effective PDE2 inhibitors.Type: GrantFiled: August 31, 2005Date of Patent: December 14, 2010Assignee: NYCOMED GmbHInventors: Beate Schmidt, Steffen Weinbrenner, Dieter Flockerzi, Raimund Kuelzer, Hermann Tenor, Hans-Peter Kley
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Publication number: 20100298302Abstract: The invention provides compounds that inhibit selected kinases (Pim, Flt and/or CK2 kinases) and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain infections and immunological disorders.Type: ApplicationFiled: May 20, 2010Publication date: November 25, 2010Inventors: Fabrice PIERRE, Mustapha Haddach, Peter C. Chua
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Publication number: 20100298287Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: ApplicationFiled: January 21, 2009Publication date: November 25, 2010Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
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Publication number: 20100298297Abstract: This invention relates to compounds of Formula (I), wherein the variables are as disclosed in the specification, to pharmaceutical compositions containing them, to methods of making the compounds and pharmaceutical compositions, and to methods of using the compounds and pharmaceutical compositions for treating or preventing disorders, in particular cancer.Type: ApplicationFiled: March 20, 2007Publication date: November 25, 2010Applicant: BAYER HEALTHCARE AGInventors: Chengzhi Zhang, Kanwar Sidhu, Mario Lobell, Gaeten Ladouceur, Qian Zhao, Zheng Liu, Kristen Allegue, Chetan Darne, Jason Newcom
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Publication number: 20100280026Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: February 26, 2010Publication date: November 4, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Jeremy Green, Huai Gao, Young-Choon Moon, Guy Brenchley, Ronald Knegtel, Francoise Pierard
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Publication number: 20100261714Abstract: Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: April 8, 2010Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Claudio STURINO, Patrick DEROY, Martin DUPLESSIS, Paul J. EDWARDS, Anne-Marie FAUCHER, Teddy HALMOS, Clint JAMES, Jean-Eric LACOSTE, Eric MALENFANT, Joannie MINVILLE, Louis MORENCY, Sebastien MORIN, Martin TREMBLAY, Christiane YOAKIM
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Publication number: 20100249110Abstract: The present invention relates to substituted pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: March 31, 2010Publication date: September 30, 2010Applicant: ArQule, Inc.Inventors: Manish Tandon, Jianqiang Wang, Nivedita Namdev
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Publication number: 20100239525Abstract: The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 30, 2009Publication date: September 23, 2010Applicant: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Sudharshan Eathiraj, Eugene Kelleher, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Rocio Palma, Manish Tandon, David Vensel, Neil Westlund, Hui Wu, Rui-Yang Yang
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Publication number: 20100239526Abstract: The present invention relates to substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 30, 2009Publication date: September 23, 2010Applicant: ArQule, Inc.Inventors: Syed M. Ali, Mark Ashwell, Chris Brassard, Audra Dalton, Anton Filikov, Jason Hill, Nivedita Namdev, Rocio Palma, Manish Tandon, David Vensel, Jianqiang Wang, Neil Westlund
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Publication number: 20100210639Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain tricyclic compounds (referred to herein as TC compounds), and especially certain 9H-pyrimido[4,5-b]indole, 9H-pyrido[4?,3?:4,5]pyrrolo[2,3-d]pyridine, and 9H-1,3,6,9-tetraaza-fluorene compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: ApplicationFiled: July 1, 2008Publication date: August 19, 2010Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Charles Reader, Suki Klair, Jane Scanlon, Glynn Addison, Michael Cherry
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Publication number: 20100189658Abstract: The present invention relates to molecular probes of the formula (I) {L1-R1-L}n-A-CO—NH—R2-L2??(I) as defined herein that allow for the observation of the catalytic activity of a selected cathepsin in in vitro assays, in cells or in multicellular organisms, a method for their preparation and the use thereof.Type: ApplicationFiled: August 27, 2009Publication date: July 29, 2010Applicant: SANOFI-AVENTISInventors: Karl-Ulrich WENDT, Maik KINDERMANN, Anja GLOBISCH
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Patent number: 7763725Abstract: The invention relates to novel pyrimido-benzimidazole derivatives. Said products exhibit a good affinity for certain melanocortin receptor sub-types, in particular MC4 receptors. Said products represent a particular interest for treating pathological disorders and diseases associated with one or several melanocortin receptors. Pharmaceutical compositions containing said products and the use thereof for a drug preparation are also disclosed.Type: GrantFiled: June 22, 2005Date of Patent: July 27, 2010Assignee: Ipsen Pharma S.A.S.Inventors: Lydie Poitout, Carole Sackur, Valerie Brault, Pierre Roubert, Pascale Plas
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Publication number: 20100173906Abstract: Substituted 3,4,6,7-tetrahydro-5H-1,2a,4a,8-tetraazacyclopenta[cd]phenalene-9-amines, pharmaceutical compositions containing the compounds or salts thereof, intermediates, methods of making the compounds or salts thereof, and methods of use of these compounds or salts thereof or pharmaceutical compositions as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: September 6, 2007Publication date: July 8, 2010Inventor: George W. Griesgraber
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Patent number: 7749996Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: GrantFiled: November 20, 2007Date of Patent: July 6, 2010Assignee: Alantos Pharmaceutical Holdings, Inc.Inventors: Christian Gege, Carine Chevrier, Matthias Schneider, Harald Bluhm, Matthias Hochgürtel, Hongbo Deng, Brian M. Gallagher, Jr., Irving Sucholeiki, Arthur Taveras
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Publication number: 20100168416Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: March 9, 2010Publication date: July 1, 2010Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
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Publication number: 20100160310Abstract: The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z1 and Z2 represent NH; Y represents —C3-9alkyl-, —C3-9alkenyl-, —C1-5alkyl-NR6—C1-5alkyl-, —C1-5alkyl-NR7—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-6alkyl-NH—CO—, —C1-2alkyl-CO-Het10-CO—, —C1-3alkyl-NH—CO-Het3-, -Het4-C1-3alkyl-CO—NH—C1-3alkyl-, —C1-2alkyl-NH—CO-L1-NH—, —NH—CO-L2-NH—, —C1-2alkyl-CO—NH-L3-CO—, —C1-2alkyl-NH—CO-L1-NH—CO—C1-3alkyl-, —C1-2alkyl-CO—NH-L3-CO—NH—C1-3alkyl-, —C1-2alkyl-NR11—CH2—CO—NH—C1-3alkyl-, Het5-CO—C1-2alkyl-, (C1-5alkyl-CO—NH—C1-3alkyl-CO—NH, —C1-5alkyl-NR13—CO—C1-3alkyl-NH—, —C1-3alkyl-NH—CO-Het27-CO—, or —C1-3alkyl-CO-Het28-CO—NH—; X1 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR16—C1-2alkyl-, —CO—NR17—, Het23-C1-2alkyl- or C1-2alkyl; X2 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR18—C1-2alkyl-, —CO—NR19—, Het24—C1-2alkyl- or C1-2alkyl; R1 and R5 each independenType: ApplicationFiled: December 8, 2005Publication date: June 24, 2010Inventors: Eddy Jean Edgard Freyne, Marc Willems, Werner Constant Johan Embrechts, Kristof Van Emelen, Sven Franciscus Anna Van Brandt, Frederik Jan Rita Rombouts
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Publication number: 20100152180Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.Type: ApplicationFiled: August 6, 2007Publication date: June 17, 2010Inventors: Philip Jones, Uwe Koch, Jesus Maria Ontoria Ontoria, Rita Scarpelli, Carsten Schultz-Fademrecht
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Publication number: 20100145041Abstract: Disclosed are thiazolyl-dihydro-quinazolines of general formula (I) wherein the groups R1 to R4 have the meanings given in the claims and specification, the isomers thereof, and processes for preparing these compounds and their use as pharmaceutical compositions.Type: ApplicationFiled: February 17, 2010Publication date: June 10, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Trixi BRANDL, Udo MAIER, Matthias HOFFMANN, Stefan SCHEUERER, Anne T. JOERGENSEN, Alexander PAUTSCH, Steffen BREITFELDER, Matthias GRAUERT, Christoph HOENKE, Klaus ERB, Michael PIEPER, Ingo PRAGST
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Publication number: 20100130489Abstract: The invention relates to Imidazolo-heteroaryl derivatives of formula (I). The compounds inhibit the activity of the Dlta enzyme of Gram-positive bacteria and are useful to treat Gram-positive bacterial infections. Furthermore the application discloses method for assessing the Dlta inhibitory activity of tested molecules and a method for measuring the efficacy of molecules in inhibiting bacteria proliferation in vitro.Type: ApplicationFiled: March 21, 2008Publication date: May 27, 2010Applicant: MUTABILIS SAInventors: Sonia Escaich, Alexis Denis, Vincent Gerusz, Francois Moreau, Mayalen Oxoby, Yannick Bonvin
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Patent number: 7723330Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: March 6, 2007Date of Patent: May 25, 2010Assignees: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Publication number: 20100105668Abstract: The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CO NR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —O—N?CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-Type: ApplicationFiled: November 24, 2009Publication date: April 29, 2010Inventors: Eddy Jean Edgard Freyne, Timothy Pietro Suren Perera, Peter Jacobus Johannes Antonius Buijnsters, Marc Willems, Gaston Stanislas Marcella Diels, Werner Constant Johan Embrechts, Peter ten Holte, Frederik Jan Rita Rombouts, Carsten Schultz-Fademrecht
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Publication number: 20100087420Abstract: The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: ApplicationFiled: December 4, 2009Publication date: April 8, 2010Applicant: ALANTOS PHARMACEUTICALS HOLDINGS, INC.Inventors: Christian Gege, Carine Chevrier, Matthias Schneider, Harald Bluhm, Matthias Hochgürtel, Hongbo Deng, Brian M. Gallagher, JR., Irving Sucholeiki, Arthur G. Taveras
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Publication number: 20100063046Abstract: The present invention provides tetracyclic imidazole analogs which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing these compounds, and methods of using the same.Type: ApplicationFiled: May 17, 2007Publication date: March 11, 2010Inventors: Jeffrey P. Whitten, Michael Schwaebe
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Patent number: 7671050Abstract: The compounds of formula (I) in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors.Type: GrantFiled: January 4, 2006Date of Patent: March 2, 2010Assignee: NYCOMED GmbHInventors: Beate Schmidt, Steffen Weinbrenner, Dieter Flockerzi, Raimund Külzer, Hermann Tenor, Hans-Peter Kley
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Publication number: 20090318421Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.Type: ApplicationFiled: April 28, 2006Publication date: December 24, 2009Inventors: Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Patent number: 7629460Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: August 15, 2008Date of Patent: December 8, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Matthias Hoffmann
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Publication number: 20090270388Abstract: The present invention relates to novel fused azolepyriimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-? inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-? activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis.Type: ApplicationFiled: March 30, 2009Publication date: October 29, 2009Applicant: Bayer Pharmaceuticals CorporationInventors: Mitsuyuki Shimada, Toshiki Murata, Kinji Fuchikami, Hideki Tsujishita, Naoki Omori, Issei Kato, Mami Miura, Klaus Urbahns, Florian Gantner, Kevin Bacon
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Publication number: 20090227575Abstract: A 7H-pyrrolo[2,3-h]quinazoline compound of the formula I wherein Ar, R1, R2, R7, R8, R9, R10, R11, R12, and n are as defined in the specification, and methods for making same.Type: ApplicationFiled: March 4, 2009Publication date: September 10, 2009Applicant: WyethInventors: Aranapakam Mudumbai Venkatesan, Zecheng Chen, Osvaldo Dos Santos, Natasja Brooijmans, Ariamala Gopalsamy
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Publication number: 20090215741Abstract: The disclosure concerns compounds of general formula (I): wherein n, X, Y, R1 and R2 are as defined herein. The disclosure also concerns a method for preparing the compounds and their therapeutic use.Type: ApplicationFiled: May 6, 2009Publication date: August 27, 2009Applicant: SANOFI-AVENTISInventors: Jacques FROISSANT, Frank MARGUET, Anne OLIVIER-BANDINI, Frederic PUECH
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Publication number: 20090209531Abstract: The invention relates to novel pyrimido-benzimidazole derivatives. Said products exhibit a good affinity for certain melanocortin receptor sub-types, in particular MC4 receptors. Said products represent a particular interest for treating pathological disorders and diseases associated with one or several melanocortin receptors. Pharmaceutical compositions containing said products and the use thereof for a drug preparation are also disclosed.Type: ApplicationFiled: June 22, 2005Publication date: August 20, 2009Inventors: Lydie Poitout, Carole Sackur, Valerie Brault, Pierre Roubert, Pascale Plas
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Patent number: 7569567Abstract: A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4) alkyl or (C1-C4) alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.Type: GrantFiled: June 17, 2008Date of Patent: August 4, 2009Assignee: sanofi-aventisInventors: Philippe Burnier, Jacques Froissant, Benoit Marabout, Frank Marguet, Frederic Puech
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Patent number: 7566713Abstract: Compounds of formula (I) are CD80 inhibitors, and of value for immunomodulation, e.g. in rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis: wherein Y is —CH2—, —CH2CH2—, or CH2CH2CH2—; R1 represents H; F; methyl, trifuoromethyl, methoxy or triflioromethoxy; R3 represents H; F; CI; Br; NO2; CN; C1C6 alkyl optionally substituted by F or Cl; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(?O) NR6R7—NR7C(?O)R6, NR7C(?O)OR6, NHC(?O) or NHC(?S)NR7R6 wherein R6 and R7 are as defined in the specification and X represents a bond or a divalent radical as defined in the specification.Type: GrantFiled: April 26, 2005Date of Patent: July 28, 2009Assignee: Medigene LimitedInventor: Ian Richard Mathews
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Publication number: 20090186887Abstract: The invention relates to novel pyrimidothienoindazoles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.Type: ApplicationFiled: March 30, 2009Publication date: July 23, 2009Applicant: Bayer Pharmaceuticals CorporationInventors: Chengzhi Zhang, Roger A. Smith, Gan Wang, Sharad K. Verma, Qingming Zhu
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Publication number: 20090185975Abstract: The invention provides a probe compound useful for early diagnosis of conformation disease, a composition and a kit comprising it for diagnosis for conformation disease, and a medical composition for treatment and/or prevention of conformation disease.Type: ApplicationFiled: December 25, 2006Publication date: July 23, 2009Applicant: TOHOKU UNIVERSITYInventors: Yukitsuka Kudo, Hiroyuki Arai, Nobuyuki Okamura, Masahiro Maruyama, Syozo Furumoto, Katsumi Doh-Ura
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Publication number: 20090143361Abstract: The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical compositions which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating central nervous system disorders, obesity, and metabolic disorders.Type: ApplicationFiled: November 25, 2008Publication date: June 4, 2009Applicants: ELBION GMBH, WYETHInventors: Michael S. Malamas, Yike Ni, James Joseph Erdei, Hans Stange, Rudolf Schindler, Norbert Hofgen, Ute Egerland, Barbara Langen
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Publication number: 20090143367Abstract: The invention relates to imidazo[1,5-a]pyrazine derivatives, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.Type: ApplicationFiled: November 25, 2008Publication date: June 4, 2009Applicants: ELBION GMBH, WYETHInventors: Michael S. Malamas, Yike Ni, James Joseph Erdei, Norbert Hofgen, Hans Stange, Rudolf Schindler, Ute Egerland, Barbara Langen
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Publication number: 20090131424Abstract: Disclosed are compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.Type: ApplicationFiled: January 9, 2009Publication date: May 21, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Trixi BRANDL, Udo MAIER, Christoph HOENKE, Anne T. JOERGENSEN, Alexander PAUTSCH, Steffen BREITFELDER, Matthias GRAUERT, Matthias HOFFMANN, Stefan SCHEUERER, Klaus ERB, Michael PIEPER, Ingo PRAGST
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Publication number: 20090124605Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: October 31, 2008Publication date: May 14, 2009Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gabriella Traquandi, Maria Gabriella Brasca, Roberto D'Alessio, Paolo Polucci, Fulvia Roletto, Anna Vulpetti, Paolo Pevarello, Achille Panzeri, Francesca Quartieri, Ron Ferguson, Paola Vianello, Daniele Fancelli
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Publication number: 20090118271Abstract: Preventive or therapeutic agents for pancreatic cancer, ovarian cancer, or liver cancer of the present invention comprise a water-soluble prodrug represented by formula 1 described below, or a pharmaceutically acceptable salt, or a hydrate or solvate of the prodrug or pharmaceutically acceptable salt, (wherein, R1 represents a hydrogen atom, or a C1-C6 alkyl group; W represents a divalent group comprising a tertiary amino group or a divalent group comprising a sulfonyl group, and Y represents a residue of a compound represented by Y—OH comprising an alcoholic hydroxyl group, wherein said Y—OH is a camptothecin, a taxane, or an anticancer nucleotide).Type: ApplicationFiled: October 19, 2006Publication date: May 7, 2009Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Isao Umeda, Jun Ohwada, Sawako Ozawa, Mika Endo, Masako Ura
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Publication number: 20090099168Abstract: Pyridopyrazine- and pyrimidopyrazine-dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dihydroxypyridine carboxamides are of Formula I: wherein G, Q, bond a, R5, R6 and R7 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: December 9, 2008Publication date: April 16, 2009Inventors: Monica Donghi, Cristina Gardelli
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Publication number: 20090098218Abstract: The present invention describes tetracyclic compounds of formula (IA) or (IB), wherein the symbols R, X, A, Y, R2, R3 and D are as defined in the specification, their use in the treatment of certain diseases, e.g. depending on MK-2 or TNF activity, and ways of manufacturing them.Type: ApplicationFiled: July 16, 2008Publication date: April 16, 2009Inventors: Achim Schlapbach, Laszlo Revesz, Guido Koch
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Publication number: 20090099165Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.Type: ApplicationFiled: April 13, 2007Publication date: April 16, 2009Applicants: Arizona Board of Regents on Behalf of The University of Arizona, Montigen Pharmaceuticals, Inc.Inventors: Laurence H. Hurley, Daruka Mahadevan, Haiyong Han, David J. Bearss, Hariprasad Vankayalapati, Sridevi Bashyam, Ruben M. Munoz, Steven L. Warner, Kimiko Della Croce, Daniel D. Von Hoff, Cory L. Grand, James Welsh
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Publication number: 20090093476Abstract: The present invention provides new compounds displaying high affinity for adenosine A3 receptors. It also provides modulators of adenosine A3 receptors. It further provides compounds for the treatment and/or prophylaxis of conditions and diseases where adenosine A3 receptor plays a role. Pharmaceutical compositions for the treatment and/or prophylaxis of conditions and diseases where adenosine A3 receptors play a role are also described.Type: ApplicationFiled: December 19, 2006Publication date: April 9, 2009Applicant: FAUST PHARMACEUTICALSInventors: Stephan Schann, Stanislas Mayer, Sophie Gardan
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Publication number: 20090082336Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.Type: ApplicationFiled: November 4, 2008Publication date: March 26, 2009Inventors: Julius J. Matasi, Deen Tulshian, Duane A. Burnett, Wen-Lian Wu, Peter Korakas, Lisa S. Silverman, Thavalakulamgara K. Sasikumar, Li Qiang, Martin S. Donalski
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Publication number: 20090029985Abstract: The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.Type: ApplicationFiled: May 12, 2008Publication date: January 29, 2009Inventors: Martin Watterson, Linda Van El Dik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Valeniza, Wenhui Hu, Magdena Zasadzki