Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
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Publication number: 20120220588Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, and methods of making and using the same.Type: ApplicationFiled: November 1, 2010Publication date: August 30, 2012Inventors: Lara S. Kallander, Brian Griffin Lawhorn, Joanne Philp
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Publication number: 20120220566Abstract: The present invention relates generally to the field of antimicrobial compounds and to methods of making and using them. These compounds are useful for treating, preventing, and reducing the risk of microbial infections in humans and animals.Type: ApplicationFiled: October 15, 2010Publication date: August 30, 2012Applicant: Rib-X Pharmaceuticals, Inc.Inventors: Erin M. Duffy, Ashoke Bhattacharjee, Hardwin O'Dowd, Marco DeVivo, Zoltan F. Kanyo, Jacek G. Martinow, Ik-Hyeon Paik, Matthew H. Scheideman, Sandra Sinishtaj, Brian T. Wimberly, Yusheng Wu
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Publication number: 20120220572Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R3 and R4 are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: February 28, 2012Publication date: August 30, 2012Applicant: ABBOTT LABORATORIESInventors: Yunsong Tong, Thomas D. Penning, Alan S. Florjancic, Julie Miyashiro, Keith W. Woods
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Publication number: 20120213802Abstract: The present invention provides methods and compositions (such as pharmaceutical compositions) comprising PAR1 antagonists for treating or preventing influenza virus type A infections, in particular H1N1 infection. PAR1 antagonists may be combined with a PAR2 agonist.Type: ApplicationFiled: November 15, 2010Publication date: August 23, 2012Inventors: Béatrice Riteau, Khaled Khoufache
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Publication number: 20120214792Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: ApplicationFiled: April 25, 2012Publication date: August 23, 2012Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20120208828Abstract: The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas.Type: ApplicationFiled: June 7, 2010Publication date: August 16, 2012Applicant: OSLO UNIVERSITY HOSPITAL HFInventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss
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Publication number: 20120208793Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: ApplicationFiled: April 25, 2012Publication date: August 16, 2012Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Patent number: 8242127Abstract: The present invention relates to derivatives of pyrimido[6,1-a]isoquinolin-4-one and their application as inhibitors of phosphodiesterase (PDE) isoenzymes. More particularly the invention relates to derivatives of pyrimido[6,1-a]isoquinolin-4-one and their use in medicine for example as bronchodilators with anti-inflammatory properties.Type: GrantFiled: April 24, 2008Date of Patent: August 14, 2012Assignee: Verona Pharma plcInventors: Alexander William Oxford, David Jack
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Publication number: 20120202833Abstract: A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1).Type: ApplicationFiled: April 20, 2012Publication date: August 9, 2012Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Hitoshi Ohki, Tooru Okayama, Masahiro Ikeda, Masahiro Ota, Yoshihiro Shibata, Toshiyuki Nakanishi, Yasusi Ueda, Nobuyuki Suzuki, Shinji Matuura
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Patent number: 8236813Abstract: A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1).Type: GrantFiled: October 29, 2010Date of Patent: August 7, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Hitoshi Ohki, Tooru Okayama, Masahiro Ikeda, Masahiro Ota, Yoshihiro Shibata, Toshiyuki Nakanishi, Yasusi Ueda, Nobuyuki Suzuki, Shinji Matuura
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Patent number: 8236950Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.Type: GrantFiled: December 19, 2007Date of Patent: August 7, 2012Assignee: Abbott LaboratoriesInventors: David A. Betebenner, Clarence J. Maring, Todd W. Rockway, Curt S. Cooper, David D. Anderson, Rolf Wagner, Rong Zhang, Akhteruzzaman Molla, Hongmei Mo, Tami J. Pilot-Matias, Sherie V L. Masse, Robert J. Carrick, Wenping He, Liangjun Lu
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Publication number: 20120196880Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.Type: ApplicationFiled: December 19, 2011Publication date: August 2, 2012Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
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Patent number: 8232286Abstract: New compounds of formula 1 are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.Type: GrantFiled: February 5, 2009Date of Patent: July 31, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Breitfelder, Udo Maier, Trixi Brandl, Christoph Hoenke, Matthias Grauert, Alexander Pautsch, Matthias Hoffmann, Frank Kalkbrenner, Anne T. Joergensen, Gerhard Schaenze, Stefan Peters, Frank Buettner, Eckhart Bauer
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Publication number: 20120190678Abstract: The present invention relates to substituted pyrazolo[4,3-h]quinazoline compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular PIM kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: December 16, 2011Publication date: July 26, 2012Inventors: Francesco Casuscelli, Claudia Piutti, Antonella Ermoli, Daniela Faiardi
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Publication number: 20120190654Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: July 28, 2010Publication date: July 26, 2012Applicant: MERCK PATENT GMBHInventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
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Publication number: 20120183577Abstract: 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: August 8, 2011Publication date: July 19, 2012Applicant: 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: 20120184546Abstract: The present invention relates to [1,2,4]triazolo[1,5-c]pyrimidine derivatives of formula (I) which inhibit the activity of Heat Shock Protein Hsp90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, methods of treating diseases and the pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: September 3, 2010Publication date: July 19, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.LInventors: Elena Casale, Francesco Casuscelli, Claudio Dalvit, Paolo Polucci, Fabio Zuccotto
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Patent number: 8222265Abstract: The present invention provides a catalyst complex or ligand, and compositions thereof, for use in a variety of organic reactions having high reactivity and enantioselectivity. The catalyst is a N-heterocyclic carbene having three fused rings with first and second rings being six-membered rings and the third being a five-membered ring. The first ring is fused to the second and has four substituents. The second ring has two nitrogens flanking a carbene atom with one nitrogen bound to a substituent. The carbene atom may optionally be bonded to a metal. The third ring is fused to the second ring and contains two nitrogens. The third ring of the catalyst has a double bond and two substituents on adjacent non-fused carbons. A non-fused nitrogen of the third ring is partially bonded to another substituent. Methods for the synthesis and use of the catalyst embodiments of the present invention are also provided.Type: GrantFiled: August 30, 2010Date of Patent: July 17, 2012Assignee: Florida State University Research FoundationInventors: D. Tyler McQuade, Jin Kyoon Park, Matthew D. Rexford, Hershel H. Lackey
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Patent number: 8222259Abstract: Compounds of the Formula I wherein R1 and R2 together with the carbon atoms to which they are bonded optionally form a further heteroaromatic ring of the formula (II) as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.Type: GrantFiled: March 3, 2009Date of Patent: July 17, 2012Assignee: Schering CorporationInventors: Joel M. Harris, Bernard R. Neustadt, Jinsong Hao, Andrew W. Stamford
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Publication number: 20120178769Abstract: The present invention discloses novel compounds for inhibiting eEF2 kinase and methods of use thereof.Type: ApplicationFiled: July 15, 2010Publication date: July 12, 2012Applicant: The University of Medicine and DentistryInventor: Alexey G. Ryazanov
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Publication number: 20120178744Abstract: The present invention provides Fused Tricyclic Compounds of the Formula (I) wherein Q, R1, R2, R3, and R4 are as defined herein, and pharmaceutically acceptable salts of such Fused Tricyclic Compounds. The Fused Tricyclic Compounds are useful in the treatment of cancer and other proliferative disorders.Type: ApplicationFiled: June 30, 2010Publication date: July 12, 2012Inventors: Cliff C. Cheng, Hongbo Zeng, Gerald W. Shipps, JR., Yongqi Deng, Zhaoyang Meng, Lianyun Zhao, Yang Nan, Binyuan Sun, Duan Liu, Panduranga A. Reddy, M. Arshad Siddiqui
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Publication number: 20120172381Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-? or by PDE4, including but not limited to rheumatoid arthritis.Type: ApplicationFiled: March 2, 2012Publication date: July 5, 2012Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel
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Patent number: 8211903Abstract: Pyrimido isoquinoline derivatives represented by formula (I): wherein: R1, R2, R3, R4, R7, R8, R9, R10, and are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.Type: GrantFiled: December 15, 2010Date of Patent: July 3, 2012Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-AventisInventors: Alistair Lochead, Mourad Saady, Philippe Yaiche
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Patent number: 8207181Abstract: The present disclosure relates to a series of 2-substituted-di- tri or tetra-hydro-8H-cyclopentaoxazolo[3,2-a]pyrimidin-8-ones and 2-substituted-di-, tetra-, or hexa-hydro-cyclohexaoxazolo[3,2-a]pyrimidin-9-ones of formula (I): wherein p, n, A, B, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.Type: GrantFiled: September 3, 2010Date of Patent: June 26, 2012Assignee: SanofiInventors: Raymond Walter Kosley, Jr., Rosy Sher
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Patent number: 8207180Abstract: The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, means either simple or double carbon-carbon bond and R1, R2 and R3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.Type: GrantFiled: November 23, 2007Date of Patent: June 26, 2012Assignee: Nerviano Medical Sciences S.R.L.Inventors: Ermes Vanotti, Marina Caldarelli, Francesco Casuscelli, Barbara Forte, Maria Menichincheri, Alessandra Scolaro, Gabriella Traquandi, Paola Vianello
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Publication number: 20120157453Abstract: Compounds of Formula II are useful for inhibition of Raf kinases. Methods of using compounds of Formula II 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: August 27, 2010Publication date: June 21, 2012Applicants: GENENTECH, INC., ARRAY BIOPHARMA INC.Inventors: Ignacio Aliagas, Stefan Gradl, Janet Gunzner, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Steven Mark Wenglowsky
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Publication number: 20120157481Abstract: The present invention relates to compounds having the general formula (I) with the definitions of X1-X3, Y1, Y2, L1, R1 and R2 given below and/or solvates, hydrates, esters and pharmaceutically acceptable salts thereof. Furthermore, the invention relates to the use of said compounds for modulating of the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.Type: ApplicationFiled: June 25, 2010Publication date: June 21, 2012Inventors: Florian Fuchs, Daniel Gilbert, Corinna Koch, Rajendra-Prasad Maskey, Sandra Steinbrink, Michael Boutros
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Publication number: 20120157438Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone 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: August 26, 2010Publication date: June 21, 2012Applicant: Merck Sharp & Dohme CorpInventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
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Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Publication number: 20120149688Abstract: Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 10, 2011Publication date: June 14, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-Maguire
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Publication number: 20120141491Abstract: The subject application provides small compounds that are able to increase/enhance autophagy in various cells. These compounds are useful in augmenting existing treatments of various cancers, microbial/viral infections, and neurodegenerative diseases. Thus, the subject application also provides methods of treating various types of cancers, microbial/viral infections, and neurodegenerative diseases.Type: ApplicationFiled: August 9, 2010Publication date: June 7, 2012Applicant: University of Florida Research Foundation Inc.Inventors: William A. Dunn, Debra Everton Akin, Brian Keith Law
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Patent number: 8193178Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: GrantFiled: September 12, 2008Date of Patent: June 5, 2012Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20120134979Abstract: Presented are mechanism based compositions and methods for treatment of SCD and SCD associated symptoms and disorders, particularly increased RBC sickling, HbS polymerization, hemolysis, tissue congestion and disruption and organ damage or failure in a mammal. The disclosed methods feature the identification of the heretofore unknown role of adenosine levels and signaling in the development of SCD and SCD associated symptoms and disorders. This discovery has lead to the identification of compositions for use as therapies for SCD and SCD associated disorders and symptoms in a mammal.Type: ApplicationFiled: November 22, 2011Publication date: May 31, 2012Inventors: Yang Xia, Rodney E. Kellems, Yujin Zhang, Harinder S. Juneja
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Publication number: 20120130144Abstract: In one aspect, the present invention provides a method of treating lung cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor. In another aspect, the present invention provides a method of treating non-small cell lung cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor.Type: ApplicationFiled: February 4, 2010Publication date: May 24, 2012Applicant: BiPar Sciences, Inc.Inventors: Barry M. Sherman, Charles Bradley, Valeria S. Ossovskaya
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Publication number: 20120129849Abstract: The present invention provides deuterated compounds having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. The deuterated compounds of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such deuterated compounds as therapeutic agents.Type: ApplicationFiled: September 23, 2011Publication date: May 24, 2012Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Mustapha HADDACH, David M. Ryckman
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Publication number: 20120129868Abstract: Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.Type: ApplicationFiled: July 29, 2010Publication date: May 24, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Jason W. Brown, Anthony R. Gangloff, Andre A. Kiryanov
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Publication number: 20120128686Abstract: The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.Type: ApplicationFiled: August 24, 2009Publication date: May 24, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Austen, Phillip Black, Wesley Blackaby, John Danilewicz, Ian Linney, Kay Schreiter, Martin Schneider
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Patent number: 8183250Abstract: The present invention relates to 1H-benzimidazole-4-carboxamides of formula (I), their preparation, and their use as inhibitors of the enzyme poly(ADP-ribose)polymerase for the preparation of drugs.Type: GrantFiled: June 2, 2009Date of Patent: May 22, 2012Assignee: Abbott LaboratoriesInventors: Thomas D. Penning, Sheela A. Thomas, Philip J. Hajduk, Daryl R. Sauer, Kathy Sarris, Vincent L. Giranda
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Publication number: 20120122889Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (I)-(I), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: December 23, 2009Publication date: May 17, 2012Applicant: President and Fellows of Harvard CollegeInventors: Junying Yuan, Emily S. Hsu
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Publication number: 20120122852Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: ApplicationFiled: January 24, 2012Publication date: May 17, 2012Applicant: SANOFI-AVENTISInventors: Laurent DUBOIS, Yannick EVANNO, Luc EVEN, Catherine GILLE, Andre MALANDA, David MACHNIK, Nathalie RAKOTOARISOA
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Publication number: 20120115886Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: ApplicationFiled: January 11, 2012Publication date: May 10, 2012Inventors: V. S. Prasada Rao LINGAM, Sachin Sundarial CHAUDHARI, Abraham THOMAS, Neelima KHAIRATKAR-JOSHI, Vidya Ganpati KATTIGE
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Patent number: 8168641Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: June 7, 2007Date of Patent: May 1, 2012Assignee: Schering CorporationInventors: Yusheng Wu, Ulrich Iserloh, Jared N. Cumming, Xiaoxiang Liu, Robert D. Mazzola, Zhong-Yue Sun, Ying Huang, Andrew Stamford, Brian McKittrick, Zhaoning Zhu
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Patent number: 8168639Abstract: Novel heterocyclic compounds of formula I: A-B-D??Formula I or a pharmaceutically acceptable salt thereof, wherein: A is selected from the group consisting of a moiety having general Formula II and a moiety having general Formula III: B is a moiety selected from the group consisting of: D is a moiety selected from the group consisting of: ?which exhibit a dopamine receptor (preferably a D4 receptor) and/or a serotonine receptor (preferably 5HTA1 agonistic activity), processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with the dopaminergic and/or serotonergic systems (e.g., sexual disorders, dyskinesia, anxiety) are disclosed.Type: GrantFiled: September 24, 2007Date of Patent: May 1, 2012Assignee: ATIR Holding S.A.Inventor: Vladimir Kogan
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Publication number: 20120095006Abstract: This invention relates to the use of certain cyclic guanosine 3?,5?-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension.Type: ApplicationFiled: December 16, 2011Publication date: April 19, 2012Inventors: Ghazwan Saleem Butrous, Timothy Michael Lukas, Ian Machin
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Patent number: 8158638Abstract: Problem to be Solved To provide a novel compound inhibiting the effect of HSP90, in particular a novel compound inhibiting the function of HSP90 as a chaperone protein and having antitumor activity. Solution The present invention provides a pyrazolopyrimidine compound represented by the formula (1) having various substituents which inhibits the ATPase activity of HSP90 and which has antitumor activity, an HSP90 inhibitor comprising the compound represented by the formula (1), a medicament comprising the compound represented by the formula (1), an anticancer agent comprising the compound represented by the formula (1), a pharmaceutical composition comprising the compound represented by the formula (1) and a method for treating cancer using the compound represented by the formula (1).Type: GrantFiled: September 14, 2007Date of Patent: April 17, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Satoru Ohsuki, Atsushi Tengeiji, Masahiro Ikeda, Yoshihiro Shibata, Chikahiro Nagata, Takashi Shimada
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Patent number: 8148384Abstract: Compounds of formula I wherein A1, A2, and A3 are as defined herein are inhibitors of PIM kinase. The compounds of formula I are useful for the treatment of diseases such as cancer.Type: GrantFiled: December 6, 2007Date of Patent: April 3, 2012Assignee: Abbott LaboratoriesInventors: Thomas D. Penning, Lisa A. Hasvold, Laura A. Hexamer, Vincent L. Giranda, Nan-horng Lin, Zhi-Fu Tao, Le Wang
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Patent number: 8148388Abstract: The present invention is drawn to 2,4 (4,6) pyrimidine derived macrocyclcs, pharmaceutical compositions thereof, and methods of making said compounds. The compounds disclosed herein are inhibitors of EGF receptor tyrosine kinases and are useful for treating cell proliferative disorders, including atherosclerosis, restenosis, and cancer.Type: GrantFiled: December 8, 2005Date of Patent: April 3, 2012Assignee: Janssen Pharmaceutica, N.V.Inventors: 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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Patent number: 8143248Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: GrantFiled: August 1, 2008Date of Patent: March 27, 2012Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
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Patent number: 8138194Abstract: Fused bicyclic pyrimidine compounds of formula (I): wherein R1, R3, R4, X1, X2, Y, Z, A, B, C, D, n, and the two bonds are defined herein. Also disclosed are a method for inhibiting Aurora kinase activity and a method for treating cancer with these compounds.Type: GrantFiled: April 22, 2009Date of Patent: March 20, 2012Assignee: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Su-Ying Wu, Yu-Sheng Chao
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Publication number: 20120065200Abstract: Compounds are disclosed for the treatment, management and prevention of diseases and disorders affecting the bone. Particular compounds are potent inhibitors of Notum Pectinacetylesterase, and are of the formula: wherein E, G, Y, Z, R1, R2, and R3 are defined herein.Type: ApplicationFiled: September 13, 2011Publication date: March 15, 2012Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Wei HE, Victoria LOMBARDO, Praveen PABBA, James TARVER, JR.
