Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
Perimidine (including hydrogenated) (Class 514/268)
  • FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY
    Publication number: 20120232086
    Abstract: The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D are as herein described. The present invention also provides compositions comprising at least one Fused Tricyclic Compound, and use of such compounds in the treatment of central nervous system diseases or disorders such as Parkinson's disease.
    Type: Application
    Filed: November 12, 2010
    Publication date: September 13, 2012
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew W. Stampford
  • Substituted Thienol[2,3-d] pyrimidines as HIV Inhibitors
    Publication number: 20120225894
    Abstract: This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.
    Type: Application
    Filed: May 11, 2012
    Publication date: September 6, 2012
    Applicant: Ardea Biosciences, Inc.
    Inventors: Jean-Luc GIRARDET, Zhi HONG, Stephanie SHAW, Yung-hyo KOH
  • COMPOUNDS FOR DISEASES AND DISORDERS
    Publication number: 20120225845
    Abstract: The invention provides novel compounds useful for the treatment of disorders associated with a defect in vesicular transport (e.g., axonal transport). The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Application
    Filed: May 4, 2012
    Publication date: September 6, 2012
    Applicant: Myrexis, Inc.
    Inventors: Christine Klein, Andrew D. Gassman, Leena Bhoite, John Manfredi
  • Antimicrobial Compounds and Methods of Making and Using the Same
    Publication number: 20120220566
    Abstract: 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: Application
    Filed: October 15, 2010
    Publication date: August 30, 2012
    Applicant: 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
  • QUINAZOLINE COMPOUNDS
    Publication number: 20120220588
    Abstract: 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: Application
    Filed: November 1, 2010
    Publication date: August 30, 2012
    Inventors: Lara S. Kallander, Brian Griffin Lawhorn, Joanne Philp
  • TRICYCLIC INHIBITORS OF KINASES
    Publication number: 20120220572
    Abstract: 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: Application
    Filed: February 28, 2012
    Publication date: August 30, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Yunsong Tong, Thomas D. Penning, Alan S. Florjancic, Julie Miyashiro, Keith W. Woods
  • THIENO- ADN FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR
    Publication number: 20120214792
    Abstract: 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: Application
    Filed: April 25, 2012
    Publication date: August 23, 2012
    Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
  • PAR-1 Antagonists for Use in the Treatment or Prevention of Influenza Virus Type A Infections
    Publication number: 20120213802
    Abstract: 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: Application
    Filed: November 15, 2010
    Publication date: August 23, 2012
    Inventors: Béatrice Riteau, Khaled Khoufache
  • THIENO- AND FURO-PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR
    Publication number: 20120208793
    Abstract: 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: Application
    Filed: April 25, 2012
    Publication date: August 16, 2012
    Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
  • Azole Derivatives as WTN Pathway Inhibitors
    Publication number: 20120208828
    Abstract: 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: Application
    Filed: June 7, 2010
    Publication date: August 16, 2012
    Applicant: OSLO UNIVERSITY HOSPITAL HF
    Inventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss
  • Derivatives of pyrimido[6,1-A]isoquinolin-4-one
    Patent number: 8242127
    Abstract: 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: Grant
    Filed: April 24, 2008
    Date of Patent: August 14, 2012
    Assignee: Verona Pharma plc
    Inventors: Alexander William Oxford, David Jack
  • TRICYCLIC PYRAZOLOPYRIMIDINE DERIVATIVES
    Publication number: 20120202833
    Abstract: 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: Application
    Filed: April 20, 2012
    Publication date: August 9, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Hitoshi Ohki, Tooru Okayama, Masahiro Ikeda, Masahiro Ota, Yoshihiro Shibata, Toshiyuki Nakanishi, Yasusi Ueda, Nobuyuki Suzuki, Shinji Matuura
  • Anti-viral compounds
    Patent number: 8236950
    Abstract: 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: Grant
    Filed: December 19, 2007
    Date of Patent: August 7, 2012
    Assignee: Abbott Laboratories
    Inventors: 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
  • Tricyclic pyrazolopyrimidine derivatives
    Patent number: 8236813
    Abstract: 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: Grant
    Filed: October 29, 2010
    Date of Patent: August 7, 2012
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Hitoshi Ohki, Tooru Okayama, Masahiro Ikeda, Masahiro Ota, Yoshihiro Shibata, Toshiyuki Nakanishi, Yasusi Ueda, Nobuyuki Suzuki, Shinji Matuura
  • PYRAZOLYL AND PYRIMIDINYL TRICYCLIC ENONES AS ANTIOXIDANT INFLAMMATION MODULATORS
    Publication number: 20120196880
    Abstract: 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: Application
    Filed: December 19, 2011
    Publication date: August 2, 2012
    Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
  • Inhibitors of PI3-kinases
    Patent number: 8232286
    Abstract: 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: Grant
    Filed: February 5, 2009
    Date of Patent: July 31, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: 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
  • SUBSTITUTED PYRAZOLO-QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20120190678
    Abstract: 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: Application
    Filed: December 16, 2011
    Publication date: July 26, 2012
    Inventors: Francesco Casuscelli, Claudia Piutti, Antonella Ermoli, Daniela Faiardi
  • NOVEL BICYCLIC UREA COMPOUNDS
    Publication number: 20120190654
    Abstract: 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: Application
    Filed: July 28, 2010
    Publication date: July 26, 2012
    Applicant: MERCK PATENT GMBH
    Inventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
  • [1,2,4]TRIAZOLO [1,5-C]PYRIMIDINE DERIVATIVES AS HSP90 MODULATORS
    Publication number: 20120184546
    Abstract: 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: Application
    Filed: September 3, 2010
    Publication date: July 19, 2012
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L
    Inventors: Elena Casale, Francesco Casuscelli, Claudio Dalvit, Paolo Polucci, Fabio Zuccotto
  • COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES
    Publication number: 20120183577
    Abstract: 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: Application
    Filed: August 8, 2011
    Publication date: July 19, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Juan-Miguel Jimenez, Jeremy Green, Huai Gao, Young-Choon Moon, Guy Brenchley, Ronald Knegtel, Francoise Pierard
  • 1,2,4-triazolo[4,3-c]pyrimidin-3-one and pyrazolo[4,3-e]-1,2,4-triazolo[4,3-c]pyrimidin-3-one compounds for use as adenosine Areceptor antagonists
    Patent number: 8222259
    Abstract: 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: Grant
    Filed: March 3, 2009
    Date of Patent: July 17, 2012
    Assignee: Schering Corporation
    Inventors: Joel M. Harris, Bernard R. Neustadt, Jinsong Hao, Andrew W. Stamford
  • Six-membered -heterocyclic carbene-based catalysts for asymmetric reactions
    Patent number: 8222265
    Abstract: 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: Grant
    Filed: August 30, 2010
    Date of Patent: July 17, 2012
    Assignee: Florida State University Research Foundation
    Inventors: D. Tyler McQuade, Jin Kyoon Park, Matthew D. Rexford, Hershel H. Lackey
  • FUSED TRICYCLIC COMPOUNDS AS NOVEL mTOR INHIBITORS
    Publication number: 20120178744
    Abstract: 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: Application
    Filed: June 30, 2010
    Publication date: July 12, 2012
    Inventors: 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
  • NOVEL COMPOUNDS FOR INHIBITING EEF-2 KINASE ACTIVITY
    Publication number: 20120178769
    Abstract: The present invention discloses novel compounds for inhibiting eEF2 kinase and methods of use thereof.
    Type: Application
    Filed: July 15, 2010
    Publication date: July 12, 2012
    Applicant: The University of Medicine and Dentistry
    Inventor: Alexey G. Ryazanov
  • Tricyclic Compounds as Modulators of TNF-alpha Synthesis and as PDE4 Inhibitors
    Publication number: 20120172381
    Abstract: 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: Application
    Filed: March 2, 2012
    Publication date: July 5, 2012
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel
  • Substituted pyrimido isoquinoline derivatives
    Patent number: 8211903
    Abstract: 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: Grant
    Filed: December 15, 2010
    Date of Patent: July 3, 2012
    Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-Aventis
    Inventors: Alistair Lochead, Mourad Saady, Philippe Yaiche
  • Substituted dihydro, trihydro and tetrahydro cycloalkyloxazolopyrimidinones, preparation and use thereof
    Patent number: 8207181
    Abstract: 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: Grant
    Filed: September 3, 2010
    Date of Patent: June 26, 2012
    Assignee: Sanofi
    Inventors: Raymond Walter Kosley, Jr., Rosy Sher
  • Tricyclic indoles and (4,5-dihydro) indoles
    Patent number: 8207180
    Abstract: 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: Grant
    Filed: November 23, 2007
    Date of Patent: June 26, 2012
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Ermes Vanotti, Marina Caldarelli, Francesco Casuscelli, Barbara Forte, Maria Menichincheri, Alessandra Scolaro, Gabriella Traquandi, Paola Vianello
  • RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20120157453
    Abstract: 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: Application
    Filed: August 27, 2010
    Publication date: June 21, 2012
    Applicants: GENENTECH, INC., ARRAY BIOPHARMA INC.
    Inventors: Ignacio Aliagas, Stefan Gradl, Janet Gunzner, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Steven Mark Wenglowsky
  • TRICYCLIC PYRIMIDINE DERIVATIVES AS WNT ANTAGONISTS
    Publication number: 20120157481
    Abstract: 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: Application
    Filed: June 25, 2010
    Publication date: June 21, 2012
    Inventors: Florian Fuchs, Daniel Gilbert, Corinna Koch, Rajendra-Prasad Maskey, Sandra Steinbrink, Michael Boutros
  • BICYCLIC AND TRICYCLIC DERIVATIVES AS THROMBIN RECEPTOR ANTAGONISTS
    Publication number: 20120157403
    Abstract: 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: Application
    Filed: February 24, 2012
    Publication date: June 21, 2012
    Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
  • PYRANYL ARYL METHYL BENZOQUINAZOLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20120157438
    Abstract: 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: Application
    Filed: August 26, 2010
    Publication date: June 21, 2012
    Applicant: Merck Sharp & Dohme Corp
    Inventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
  • PLATELET ADP RECEPTOR INHIBITORS
    Publication number: 20120149688
    Abstract: 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: Application
    Filed: October 10, 2011
    Publication date: June 14, 2012
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-Maguire
  • METHODS AND COMPOSITIONS FOR THE TREATMENT OF CANCERS AND PATHOGENIC INFECTIONS
    Publication number: 20120141491
    Abstract: 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: Application
    Filed: August 9, 2010
    Publication date: June 7, 2012
    Applicant: University of Florida Research Foundation Inc.
    Inventors: William A. Dunn, Debra Everton Akin, Brian Keith Law
  • Thieno- and furo-pyrimidine modulators of the histamine Hreceptor
    Patent number: 8193178
    Abstract: 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: Grant
    Filed: September 12, 2008
    Date of Patent: June 5, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
  • METHODS AND COMPOSITIONS FOR THE TREATMENT OF SICKLE CELL DISEASE
    Publication number: 20120134979
    Abstract: 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: Application
    Filed: November 22, 2011
    Publication date: May 31, 2012
    Inventors: Yang Xia, Rodney E. Kellems, Yujin Zhang, Harinder S. Juneja
  • POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS
    Publication number: 20120129868
    Abstract: 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: Application
    Filed: July 29, 2010
    Publication date: May 24, 2012
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Jason W. Brown, Anthony R. Gangloff, Andre A. Kiryanov
  • TREATMENT OF LUNG CANCER WITH A NITROBENZAMIDE COMPOUND IN COMBINATION WITH A GROWTH FACTOR INHIBITOR
    Publication number: 20120130144
    Abstract: 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: Application
    Filed: February 4, 2010
    Publication date: May 24, 2012
    Applicant: BiPar Sciences, Inc.
    Inventors: Barry M. Sherman, Charles Bradley, Valeria S. Ossovskaya
  • DEUTERATED SERINE-THREONINE PROTEIN KINASE MODULATORS
    Publication number: 20120129849
    Abstract: 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: Application
    Filed: September 23, 2011
    Publication date: May 24, 2012
    Applicant: CYLENE PHARMACEUTICALS, INC.
    Inventors: Mustapha HADDACH, David M. Ryckman
  • THIENOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS
    Publication number: 20120128686
    Abstract: 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: Application
    Filed: August 24, 2009
    Publication date: May 24, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias Austen, Phillip Black, Wesley Blackaby, John Danilewicz, Ian Linney, Kay Schreiter, Martin Schneider
  • Potent PARP inhibitors
    Patent number: 8183250
    Abstract: 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: Grant
    Filed: June 2, 2009
    Date of Patent: May 22, 2012
    Assignee: Abbott Laboratories
    Inventors: Thomas D. Penning, Sheela A. Thomas, Philip J. Hajduk, Daryl R. Sauer, Kathy Sarris, Vincent L. Giranda
  • SMALL MOLECULE INHIBITORS OF NECROPTOSIS
    Publication number: 20120122889
    Abstract: 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: Application
    Filed: December 23, 2009
    Publication date: May 17, 2012
    Applicant: President and Fellows of Harvard College
    Inventors: Junying Yuan, Emily S. Hsu
  • TRICYCLIC N-HETEROARYL-CARBOXAMIDE DERIVATIVES CONTAINING A BENZIMIDAZOLE UNIT, METHOD FOR PREPARING SAME AND THEIR THERAPEUTIC USE
    Publication number: 20120122852
    Abstract: 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: Application
    Filed: January 24, 2012
    Publication date: May 17, 2012
    Applicant: SANOFI-AVENTIS
    Inventors: Laurent DUBOIS, Yannick EVANNO, Luc EVEN, Catherine GILLE, Andre MALANDA, David MACHNIK, Nathalie RAKOTOARISOA
  • FUSED PYRIMIDINEONE COMPOUNDS AS TRPV3 MODULATORS
    Publication number: 20120115886
    Abstract: 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: Application
    Filed: January 11, 2012
    Publication date: May 10, 2012
    Inventors: V. S. Prasada Rao LINGAM, Sachin Sundarial CHAUDHARI, Abraham THOMAS, Neelima KHAIRATKAR-JOSHI, Vidya Ganpati KATTIGE
  • Aspartyl protease inhibitors
    Patent number: 8168641
    Abstract: 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: Grant
    Filed: June 7, 2007
    Date of Patent: May 1, 2012
    Assignee: Schering Corporation
    Inventors: Yusheng Wu, Ulrich Iserloh, Jared N. Cumming, Xiaoxiang Liu, Robert D. Mazzola, Zhong-Yue Sun, Ying Huang, Andrew Stamford, Brian McKittrick, Zhaoning Zhu
  • Heterotricyclic compounds as serotonergic and/or dopaminergic agents and uses thereof
    Patent number: 8168639
    Abstract: 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: Grant
    Filed: September 24, 2007
    Date of Patent: May 1, 2012
    Assignee: ATIR Holding S.A.
    Inventor: Vladimir Kogan
  • TREATMENT OF PULMONARY HYPERTENSION
    Publication number: 20120095006
    Abstract: 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: Application
    Filed: December 16, 2011
    Publication date: April 19, 2012
    Inventors: Ghazwan Saleem Butrous, Timothy Michael Lukas, Ian Machin
  • Pyrazolopyrimidine derivative
    Patent number: 8158638
    Abstract: 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: Grant
    Filed: September 14, 2007
    Date of Patent: April 17, 2012
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Satoru Ohsuki, Atsushi Tengeiji, Masahiro Ikeda, Yoshihiro Shibata, Chikahiro Nagata, Takashi Shimada
  • 2,4 (4,6) pyrimidine derivatives
    Patent number: 8148388
    Abstract: 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: Grant
    Filed: December 8, 2005
    Date of Patent: April 3, 2012
    Assignee: 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
  • Substituted thieno[3,2-d]pyrimidine PIM kinase inhibitors as cancer chemotherapeutics
    Patent number: 8148384
    Abstract: 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: Grant
    Filed: December 6, 2007
    Date of Patent: April 3, 2012
    Assignee: Abbott Laboratories
    Inventors: Thomas D. Penning, Lisa A. Hasvold, Laura A. Hexamer, Vincent L. Giranda, Nan-horng Lin, Zhi-Fu Tao, Le Wang