The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/362)
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Patent number: 7977338Abstract: Compounds of formula wherein the residues R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, salts thereof; their use, methods of their use, processes for their production, pharmaceutical compositions comprising them, their combinations with second drug substances and the use thereof and the like. The compounds are protein kinase inhibitors and can be used for the treatment of diseases mediated by protein kinase inhibitors, e.g. for the treatment of various proliferative diseases.Type: GrantFiled: October 15, 2007Date of Patent: July 12, 2011Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano
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Patent number: 7977325Abstract: This invention relates to compounds of general formula I in which R1 and R2 are described in this application, the use of the compounds of general formula I as inhibitors of protein tyrosine kinases for treatment of various diseases as well as the compounds of general formulas II and III as intermediate compounds for the production of compounds of general formula I, wherein X, R1a and R2a have the meaning that is described in general formulas II and III.Type: GrantFiled: December 14, 2005Date of Patent: July 12, 2011Assignee: Bayer Schering Pharma AGInventors: Wolfgang Schwede, Hermann Kuenzer, Antonius Ter Laak, Benjamin Bader, Roman Hillig, Ursula Moenning, Arndt Schmitz, Dieter Zopf
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Patent number: 7977352Abstract: Novel triazolopyridine 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, ECM degradation, joint degradation and/or inflammation, and others.Type: GrantFiled: November 30, 2007Date of Patent: July 12, 2011Assignee: Galapagos NVInventors: Paul John Edwards, Wolfgang Schmidt, Veronique Birault, Friedrich Erich Karl Kroll, Andrew Burritt, Xueliang Tao, Martin James Inglis Andrews, Sébastien Laurent Xavier Martina
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Publication number: 20110166123Abstract: Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.Type: ApplicationFiled: January 7, 2009Publication date: July 7, 2011Applicant: AARDEA BIOSCIENCES, INC.Inventors: Huanming Chen, Jianlin Song, Jean-Michel Vernier, Anthony B. Pinkerton, Johnny Y. Nagasawa
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Publication number: 20110160204Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L1, R1, R2, R3, R4, R5, R6, and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.Type: ApplicationFiled: February 25, 2011Publication date: June 30, 2011Applicant: CEPHALON, INC.Inventors: Bruce D. Dorsey, Karen L. Milkiewicz, Douglas A. Pippin, Jay P. Theroff, Ted Underiner, Linda Weinberg, Craig A. Zificsak
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Patent number: 7964606Abstract: The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions comprising an effective amount of a Phenylene Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Phenylene Compound.Type: GrantFiled: July 29, 2010Date of Patent: June 21, 2011Assignee: Purdue Pharma L.P.Inventor: Qun Sun
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Publication number: 20110144104Abstract: The present invention relates to pyrrolidinyl-alkyl-amide derivatives of formula (I) or (IA) wherein the variables are as defined herein, to their preparation and to their therapeutic use as CCR3 receptor ligands.Type: ApplicationFiled: January 26, 2011Publication date: June 16, 2011Applicant: SANOFI-AVENTISInventors: Agnes BEHR, Sandor BATORI, Veronika BARTANE BODOR, Zoltan SZLAVIK, Imre BATA, Katalin URBAN-SZABO, Zoltan KAPUI, Endre MIKUS
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Publication number: 20110144121Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: ApplicationFiled: June 16, 2010Publication date: June 16, 2011Applicant: CARA THERAPEUTICS, INC.Inventor: Robert Zhiyong Luo
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Patent number: 7960388Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are 3-imidazoyl-pyrazolo[3,4-b]pyridine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: November 12, 2009Date of Patent: June 14, 2011Assignee: ChemoCentryx, Inc.Inventors: Lianfa Li, Andrew M.K. Pennell, Penglie Zhang
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Publication number: 20110130286Abstract: Piperazine compounds of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the piperazine compounds of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one piperazine compound of the formula I to act on plants, their seed and/or their habitat.Type: ApplicationFiled: July 23, 2009Publication date: June 2, 2011Applicant: BASF SEInventors: Liliana Parra Rapado, Eike Hupe, Matthias Witschel, Thomas Seitz, Anja Simon, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt, Trevor William Newton, Frank Stelzer, Tao Qu, William Karl Moberg, Dschun Song, Michael Rack, Timo Frassetto, Klaus Kreuz, Julia Major
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Publication number: 20110124628Abstract: 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: November 22, 2010Publication date: May 26, 2011Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert Mantei, Todd M. Hansen
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Patent number: 7947686Abstract: Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, 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 dysregulated protein kinase activity, like cancer.Type: GrantFiled: December 6, 2006Date of Patent: May 24, 2011Assignee: Nerviano Medical Sciences S.r.l.Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Paolo Polucci, Manuela Villa, Marcella Nesi, Mauro Angiolini, Mario Varasi
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Patent number: 7947677Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B1, B2, B3, B4, D1, D2, E1, E2, E3, E4, E5, G1, G2, J, K, T, U, V, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: November 14, 2006Date of Patent: May 24, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Steven N. Gallicchio, C. Blair Zartman, Harold G. Selnick
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Publication number: 20110118246Abstract: The invention is directed to to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: June 3, 2009Publication date: May 19, 2011Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Publication number: 20110118278Abstract: There are provided bicyclic carbonylamino-pyrazoles of formula (I), wherein the variables are as specified in the claims, for use as medicament, in particular for the treatment of diseases due to the malfunctioning of protein kinases (PKs), such as cancer, pharmaceutical compositions comprising such carbamoyl derivatives, and their use as prodrugs of therapeutically active agents. Method of treatment and some new bicyclic carbonylamino-pyrazoles are also object of the present invention.Type: ApplicationFiled: May 14, 2009Publication date: May 19, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Paolo Polucci
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Patent number: 7943768Abstract: A compound of formula (I) P—W—C(?X)-L-Q??(I) wherein P is an optionally substituted aryl or heteroaryl group; W is an optionally substituted 6 or 7-membered aliphatic ring comprising ring atoms Y1 and Y2 independently selected from Oxygen and Nitrogen, X is selected from Oxygen, Nitrogen and Sulphur; L is an optional C1-4 linker; and Q is an optionally substituted 4-7 membered aliphatic ring: for use in the treatment of chemokine mediated diseases or disorders.Type: GrantFiled: December 18, 2006Date of Patent: May 17, 2011Assignee: AstraZeneca ABInventors: Justin Fairfield Bower, Peter Wedderburn Kenny, Jeffrey Philip Poyser
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Publication number: 20110110889Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs 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: ApplicationFiled: February 27, 2009Publication date: May 12, 2011Applicants: Array Bio Pharma Inc., Grenentech ,Inc.Inventors: Kateri A. Ahrendt et al., Alexander J. Buckmelter, Jonas Grina, Joshua D. Hansen, Ellen R. Laird, David Moreno, Brad Newhouse, Li Ren, Steven M. Wenglowsky, Bainian Feng, Janet Gunzner, Kim Malesky, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Wendy B. Young
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Publication number: 20110112077Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: January 15, 2009Publication date: May 12, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. KUDUK, Ronald K, CHANG
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Patent number: 7939527Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: GrantFiled: April 9, 2009Date of Patent: May 10, 2011Assignee: Janssen Pharmaceutica NVInventors: Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
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Publication number: 20110105497Abstract: Compounds for treating, preventing or managing cancer are disclosed. Also provided are methods for using the compounds in treatment of various cancers. Also provided are methods of treatment using the compounds together with another chemotherapy, radiation therapy, hormonal therapy, biological therapy, or immunotherapy. Pharmaceutical compositions suitable for use in the methods are also disclosed.Type: ApplicationFiled: October 26, 2010Publication date: May 5, 2011Inventor: Anantha Sudhakar
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Publication number: 20110105498Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R4, R5, R6 and Z are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: April 24, 2008Publication date: May 5, 2011Applicant: Amgen Inc.Inventors: Liping H. Pettus, Andrew Tasker, Shimin Xu, Ryan Wurz
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Publication number: 20110098293Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.Type: ApplicationFiled: February 27, 2009Publication date: April 28, 2011Inventors: Michael Mannion, Stephane Raeppel, Stephen William Claridge, Frederic Gaudette, Lijie Zhan, Ljubomir Isakovic, Oscar Mario Saavedra, Tetsuyuki Uno, Masashi Kishida, Arkadii Vaisburg
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Publication number: 20110098291Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary diseases and disorders.Type: ApplicationFiled: May 4, 2010Publication date: April 28, 2011Applicant: Alla Chem Inc.Inventors: Alexander KHVAT, Sergey TKACHENKO, Ilya OKUN, Borys V. ROGOVOY, Nikolay SAVCHUK, John MAY, Patrick O'CONNOR, William RIPKA, Jean-Michel VERNIER, David MATTHEWS
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Publication number: 20110098308Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: July 1, 2010Publication date: April 28, 2011Applicant: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M.K. Pennell, John J. Kim Wright, Wei Chen, Manmohan R. Leleti, Yandong Li, Lianfa Li, Yuan Xu, Mark M. Gleason, Yibin Zeng, Kevin Lloyd Greenman
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Patent number: 7932251Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.Type: GrantFiled: July 15, 2008Date of Patent: April 26, 2011Assignee: N.V. OrganonInventors: Jiaqiang Cai, Zoran Rankovic, Philip Stephen Jones, David Jonathan Bennett, Xavier Fradera
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Publication number: 20110092479Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs 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: ApplicationFiled: February 27, 2009Publication date: April 21, 2011Applicants: Array BioPharma Inc., Genentech, Inc.Inventors: Kateri A. Ahrendt, Alexandre J. Buckmelter, Jason De Meese, Jonas Grina, Joshua D. Hansen, Ellen R. Laird, Paul Lunghofer, David Moreno, Brad Newhouse, Li Ren, Jeongbeob Seo, Hongqi Tian, Steven M. Wenglowsky, Bainian Feng, Janet Gunzner, Kim Malesky, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Wendy B. Young
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Publication number: 20110092505Abstract: The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.Type: ApplicationFiled: June 12, 2009Publication date: April 21, 2011Inventors: Robin Burgis, Michael Paul Capparelli, Lucian Dipietro, Gabriel G. Gamber, Charles Francis Jewell, JR., Erik Meredith, Karl Miranda, Lauren G. Monovich, Chang Rao, Nicolas Soldermann, Taeyoung Yoon, Qingming Zhu
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Publication number: 20110082138Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: November 24, 2010Publication date: April 7, 2011Applicant: Daiichi Sankyo Company, LimitedInventors: Masami Ohtsuka, Noriyasu Haginoya, Masanori Ichikawa, Hironori Matsunaga, Hironao Saito, Yoshihiro Shibata, Tomoyuki Tsunemi
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Publication number: 20110082130Abstract: Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).Type: ApplicationFiled: August 23, 2010Publication date: April 7, 2011Applicant: LIGAND PHARMACEUTICALS, INC.Inventors: Yang Gao, Bingsong Han, Yuelian Xu, Timothy M Caldwell, Linghong Xie
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Publication number: 20110071160Abstract: The subject matter of the present invention are compounds corresponding to formula (I): in which: X is an unsubstituted or substituted divalent (C1-C5)alkylene radical; R1 is an —NR8R9 group; or an unsubstituted or substituted piperidin-3-yl or piperidin-4-yl radical; R2 is a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R3 is a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R4 is a hydrogen atom, a halogen atom, an Alk group, a hydroxyl or an OAlk group; and R5 is a hydrogen atom, a halogen atom, an Alk group, a hydroxyl or an OAlk group.Type: ApplicationFiled: October 15, 2010Publication date: March 24, 2011Applicant: SANOFI-AVENTISInventors: Cedric COUTURIER, Loic FOULON, Claudine SERRADEIL-LE GAL, Gerard VALETTE
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Publication number: 20110071161Abstract: The invention relates to the triazolopyridine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.Type: ApplicationFiled: November 30, 2010Publication date: March 24, 2011Applicant: SANOFI-AVENTISInventor: Christian HOORNAERT
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Publication number: 20110071128Abstract: The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.Type: ApplicationFiled: September 21, 2010Publication date: March 24, 2011Inventors: Daniela Alberati, Rubén Alvarez Sánchez, Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
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Publication number: 20110059941Abstract: Compounds of Formula (I), wherein R1-R10, A and X1 to X3 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: ApplicationFiled: May 19, 2006Publication date: March 10, 2011Inventors: Peter William Rodney Caulkett, Darren McKerrecher, Nicholas John Newcombe, Kurt Gordon Pike, Michael James Waring
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Publication number: 20110059982Abstract: Azaindole derivative compounds are described. The compounds have an optionally substituted azaindole core linked to a carbocyclic ring having at least one nitrogen atom and further bound to an optionally substituted aryl ring. A process for preparing these compounds, compositions comprising them, and methods of using them to treat disorders of the central nervous system are described.Type: ApplicationFiled: February 14, 2009Publication date: March 10, 2011Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Timo Heinrich, Michael Katzer
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Publication number: 20110059946Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: September 10, 2010Publication date: March 10, 2011Applicant: Morphochem Aktiengesellschaft fuer Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin
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Patent number: 7902356Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein w, R1, q, p, R2, t, Ar1, L1, R3 and R4 are as defined, or a pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.Type: GrantFiled: December 16, 2005Date of Patent: March 8, 2011Assignee: Eli Lilly and CompanyInventors: Albert Kudzovi Amegadzie, James Peter Beck, Kevin Matthew Gardinier, Erik James Hembre, James Craig Ruble, Kenneth Allen Savin, Brian David Wakefield
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Publication number: 20110053953Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8 and n are defined in the specification, methods for using said compounds, methods for making said compounds and pharmaceutical compositions containing said compounds.Type: ApplicationFiled: January 31, 2008Publication date: March 3, 2011Inventors: Abdelmalik Slassi, Methvin Isaac, Joshua Clayton, Ian Egle, Babu Joseph, Fupeng Ma
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Publication number: 20110039822Abstract: The present invention provides a compound having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases, inflammatory diseases, and allergic diseases. As a result of studies on a novel condensed heterocyclic derivative, the inventors have found that a compound having a cross-linked structure has an excellent JAK3 inhibition activity, and have completed the present invention. In other words, it is verified that the compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g.Type: ApplicationFiled: October 28, 2010Publication date: February 17, 2011Applicant: Astellas Pharma Inc.Inventors: Takayuki INOUE, Akira Tanaka, Kazuo Nakai, Hiroshi Sasaki, Fumie Takahashi, Shohei Shirakami, Keiko Hatanaka, Yutaka Nakajima, Koichiro Mukoyoshi, Hisao Hamaguchi, Shigeki Kunikawa, Yasuyuki Higashi
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Publication number: 20110039823Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.Type: ApplicationFiled: April 11, 2008Publication date: February 17, 2011Applicant: Actelion Pharmaceuticals LtdInventors: Daniel Bur, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110039861Abstract: The present invention relates to cyclic azaindole-3-carboxamides of the formula I, wherein A, R, R10, R20, R30, R40, Y1, Y2, Y3, Y4, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: July 28, 2010Publication date: February 17, 2011Applicant: SANOFI-AVENTISInventors: Henning STEINHAGEN, Bodo SCHEIPER, Hans MATTER, Gary MCCORT
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Publication number: 20110034457Abstract: The use of compounds of formula (I) in therapy, particularly for the treatment of a disorder mediated by excessive or inappropriate HSP90 activity formula (I), wherein R2 is a group of formula (IA): —(Ar1)m-(Alk1)p-(Z)r-(Alk2)S-Q??(IA) Ar1, Alk1, Z, Alk2 and Q being as defined in the specification; m, p, r and s are independently 0 or 1; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group; or a salt, N-oxide, hydrate, or solvate thereof.Type: ApplicationFiled: October 21, 2010Publication date: February 10, 2011Applicant: VERNALIS (CAMBRIDGE) LIMITED.Inventors: Martin James Drysdale, Brian William Dymock, Xavier Barril-Alonso
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Publication number: 20110028717Abstract: The present invention creates an azaindole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further providing a therapeutic agent for treating allergic diseases. A compound of the general formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; the formula of —X1?X2—X3?X4— is a formula of —C(R1)?C(R2)—C(R3)?N— etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is optionally substituted C1-C6 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is optionally substituted C1-C6 alky etc.; R9 is carboxy etc.; M is sulfonyl etc.; Y is a single bond etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.Type: ApplicationFiled: October 14, 2010Publication date: February 3, 2011Inventors: Akira Kugimiya, Itsuo Makino, Naohiro Onodera
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Patent number: 7879844Abstract: The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia).Type: GrantFiled: December 25, 2006Date of Patent: February 1, 2011Assignee: Astellas Pharma Inc.Inventors: Takayuki Inoue, Akira Tanaka, Kazuo Nakai, Hiroshi Sasaki, Fumie Takahashi, Shohei Shirakami, Keiko Hatanaka, Yutaka Nakajima, Koichiro Mukoyoshi, Hisao Hamaguchi, Shigeki Kunikawa, Yasuyuki Higashi
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Publication number: 20110021497Abstract: The invention relates to compounds of formula (I) wherein X, T1 and R1 to R3 have the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.Type: ApplicationFiled: November 21, 2008Publication date: January 27, 2011Inventors: Nigel Ramsden, Kathryn Bell, Andrew David Cansfield, Jess Taylor, Mihiro Sunose, David Middlemiss, Gitte Neubauer
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Publication number: 20110021494Abstract: The compounds of formula (I), wherein ring D and ring E together form a fused ring system selected from formula (II), (III), (IV), (V), (VI), (VII), and the salts of these compounds are novel, effective inhibitors of histone deacetylases.Type: ApplicationFiled: September 19, 2008Publication date: January 27, 2011Applicant: 4SC AGInventors: Thomas Maier, Thomas Beckers, Thomas Baer, Matthias Vennemann, Volker Gekeler, Astrid Zimmermann, Petra Gimmnich, Kamlesh Padiya, Hemant Joshi, Uday Joshi, Mahindra Makhija, Dipak Harel
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Publication number: 20110009390Abstract: The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: R1, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.Type: ApplicationFiled: May 21, 2008Publication date: January 13, 2011Applicant: F2G LIMITEDInventors: Lloyd James Payne, Robert Downham, Graham Edward Morris Sibley, Philip Edwards, Gareth Morse Davies
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Publication number: 20110008288Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). 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 the compounds of the present invention.Type: ApplicationFiled: June 15, 2010Publication date: January 13, 2011Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Datong Tang, Ce Wang, Yao-Ling Qiu
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Publication number: 20110009381Abstract: Provided herein are novel sirtuin-modulating compounds Structural Formula (I): and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: November 7, 2008Publication date: January 13, 2011Applicant: Sirtis Pharmaceuticals, Inc.Inventors: Chi B. Vu, Christopher Oalmann, Robert B. Perni, Jeremy S. Disch, Bruce Szczepankiewicz, Giovanna Gualtieri, Rebecca L. Casaubon
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Patent number: 7868007Abstract: The invention relates to the triazolopyridine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.Type: GrantFiled: October 6, 2009Date of Patent: January 11, 2011Assignee: sanofi-aventisInventor: Christian Hoornaert
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Publication number: 20110003808Abstract: This invention relates to novel octahydroquinolizines for treatment or prevention of diabetes mellitus and its complications, for treatment or prevention of hyperlipidemia, for treatment of diabetic dyslipidemia, for treatment or prevention of the metabolic syndrome, for treatment of diseases related to metabolic dysfunction, for treatment of obesity or obesity-related diseases. The invention also includes pharmaceutical compositions and kits comprising these compounds alone or in combination with other drugs or compounds aiming towards an improved treatment or prevention of the aforementioned diseases or syndromes in humans or animals.Type: ApplicationFiled: December 17, 2008Publication date: January 6, 2011Applicant: 55PHARMA DRUG DISCOVERY & DEVELOPMENT AGInventors: Immanuel Adorjan, Leonhardt Bauer, Klaus Frobel, Clemens Fuernsinn