Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/117)
Four or more ring nitrogens in the bicyclo ring system (Class 544/118)
  • PYRIMIDINONE DERIVATIVES, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF
    Publication number: 20130289031
    Abstract: The invention relates to novel products of formula (Ia) or (Ib): these products being in all the isomeric forms and salts as drugs, notably as anticancer drugs.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 31, 2013
    Applicant: SANOFI
    Inventors: Jerome Arigon, Maurice Brollo, Jacques Clement, Romain Combet, Florence Durand, Youssef El Ahmad, Jean-Robert Labrosse, Jean-Philippe Letallec, Baptiste Ronan
  • 2,4-DIAMINO-6,7-DIHYDRO-5H-PYRROLO[2,3]PYRIMIDINE DERIVATIVES AS FAK/Pyk2 INHIBITORS
    Publication number: 20130281438
    Abstract: The invention relates to a novel class of 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as a FAK and/or Pyk2 inhibitor, to a process for their preparation, and to a composition thereof, as well as to use of the compounds for the inhibiting FAK and/or Pyk2 and method for the treatment of a FAK and/or Pyk2 mediated disorder or disease.
    Type: Application
    Filed: January 7, 2012
    Publication date: October 24, 2013
    Applicant: CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Dengming Xiao, Liang Cheng, Xijie Liu, Yuandong Hu, Xinhe Xu, Zhihua Liu, Lipeng Zhang, Wei Wu, Shulong Wang, Yu Shen, Gen Li, Yin Wang, Sheng Zhao, Chonglong Li, Jia Tang, Honghao Yu
  • Pyrazoloquinoline derivatives
    Patent number: 8563565
    Abstract: A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has a potential use of a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: October 22, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yoshihiko Norimine, Kunitoshi Takeda, Koji Hagiwara, Yuichi Suzuki, Yuki Ishihara, Nobuaki Sato
  • Pyrido[3,2-d]pyrimidine PI3K delta inhibitor compounds and methods of use
    Patent number: 8563540
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I 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: Grant
    Filed: April 1, 2013
    Date of Patent: October 22, 2013
    Assignee: Genentech, Inc.
    Inventors: Georgette Castanedo, Bryan Chan, Matthew C. Lucas, Brian Safina, Daniel P. Sutherlin, Zachary Sweeney
  • Substituted Pyrazines Having Herbicidal Activity
    Publication number: 20130274109
    Abstract: The present invention provides substituted pyrazine compounds of the formula I or N-oxides or agriculturally suitable salts thereof, wherein the variables in the formula I are defined as in the description. Substituted pyrazines of formula I are useful as herbicides.
    Type: Application
    Filed: December 23, 2011
    Publication date: October 17, 2013
    Applicant: BASF SE
    Inventors: Ruediger Reingruber, Helmut Kraus, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Gilbert Besong, Michael Rack, Andree Van Der Kloet, Thomas Seitz, Jens Lerchl, Klaus Kreuz, Klaus Grossmann, Richard Roger Evans
  • COMPOUNDS AND METHODS FOR ANTIVIRAL TREATMENT
    Publication number: 20130273037
    Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Application
    Filed: April 17, 2013
    Publication date: October 17, 2013
    Inventors: Dustin Siegel, David Sperandio, Hai Yang, Michael Sangi, Jay P. Parrish, Hon Chung Hui
  • IMIDAZOPYRAZINE SYK INHIBITORS
    Publication number: 20130267496
    Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: May 23, 2013
    Publication date: October 10, 2013
    Applicant: GILEAD CONNECTICUT, INC.
    Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J. M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
  • IMIDAZO-, PYRAZOLOPYRAZINES AND IMIDAZOTRIAZINES AND THEIR USE
    Publication number: 20130261115
    Abstract: The invention relates to substituted imidazo-, pyrazolopyrazines and imidazotriazines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of hematological disorders, preferably of leukopenias and neutropenias.
    Type: Application
    Filed: May 30, 2013
    Publication date: October 3, 2013
    Inventors: Stephan SIEGEL, Andreas WILMEN, Susanne RÖHRIG, Niels SVENSTRUP, Mark Jean GNOTH, Stefan HEITMEIER, Ulrich RESTER, Adrian TERSTEEGEN, Michael GERISCH
  • Pyrido[2,3-b]pyrazin-8-substituted compounds and their use
    Patent number: 8546387
    Abstract: The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.
    Type: Grant
    Filed: April 28, 2012
    Date of Patent: October 1, 2013
    Assignees: Cancer Research Technology Limited, Institute of Cancer Research: Royal Cancer Hospital
    Inventors: Caroline Joy Springer, Dan Niculescu-Duvaz, Ion Niculescu-Duvaz, Richard Marais, Bartholomeus Marinus Josephus Marie Suijkerbuijk, Alfonso Zambon, Arnaud Nourry, Delphine Menard
  • 7-HYDROXY-PYRAZOLO[1,5-A] PYRIMIDINE COMPOUNDS AND THEIR USE AS CCR2 RECEPTOR ANTAGONISTS
    Publication number: 20130252951
    Abstract: The compounds of formula (I) are antagonists of the CCR2 receptor Wherein R1-7 and A are as defined in the claims.
    Type: Application
    Filed: September 26, 2011
    Publication date: September 26, 2013
    Applicant: Proximagen Limited
    Inventors: Joe William Boyd, Paul Meo, Michael Higginbottom, Iain Simpson, David Mountford, Edward Daniel Savory
  • 6-(ETHYNYL)PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS
    Publication number: 20130245012
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.
    Type: Application
    Filed: June 10, 2011
    Publication date: September 19, 2013
    Applicant: AFRAXIS, INC.
    Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
  • IMIDAZOPYRIZINE SYK INHIBITORS
    Publication number: 20130231330
    Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: April 12, 2013
    Publication date: September 5, 2013
    Applicant: GILEAD CONNECTICUT, INC.
    Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD
  • Bicyclic Heteroaryl Compounds
    Publication number: 20130231337
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 5, 2013
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
  • PHARMACEUTICAL COMPOUNDS
    Publication number: 20130230585
    Abstract: Provided herein is a pharmaceutical composition that comprises a pharmaceutically acceptable carrier or diluent and, as an active ingredient, the compound 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine bismesylate.
    Type: Application
    Filed: November 5, 2012
    Publication date: September 5, 2013
    Applicant: F. HOFFMANN-LA ROCHE AG
    Inventors: Irina Chuckowree, Adrian Folkes, Tim Hancox, Stephen Shuttleworth
  • Inhibitors of Human Immunodeficiency Virus Replication
    Publication number: 20130231331
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 5, 2013
    Inventors: Annapurna Pendri, David R. Langley, Samuel Gerritz, Guo Li, Weixu Zhai, Stanley D'Andrea, Manoj Patel, B. Narasimhulu Naidu, Kevin Peese, Zhongyu Wang
  • PYRIDO[3,2-d]PYRIMIDINE PI3K DELTA INHIBITOR COMPOUNDS AND METHODS OF USE
    Publication number: 20130225557
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I 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: April 1, 2013
    Publication date: August 29, 2013
    Applicant: Genentech, Inc.
    Inventor: Genentech, Inc.
  • BICYCLIC DIAMINES AS JANUS KINASE INHIBITORS
    Publication number: 20130225577
    Abstract: The instant invention provides compounds of formula I which are Jak inhibitors, and as such are useful for the treatment of Jak-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: October 17, 2011
    Publication date: August 29, 2013
    Inventors: David Joseph Guerin, Jason D. Brubaker, Michelle Martinez, Joon O. Jung, Neville J. Anthony, Mark E. Scott, Carolyn Michele Cammarano, Dawn Marie Mampreian Hoffman, Hyun Chong Woo, Christopher J. Dinsmore, Philip Jones
  • Pyrrolopyrazine kinase inhibitors
    Patent number: 8518945
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X? and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: March 4, 2011
    Date of Patent: August 27, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen M. Lynch, Timothy D. Owens, Michael Soth
  • METHOD OF TREATMENT USING SUBSTITUTED IMIDAZO[1,2B]PYRIDAZINE COMPOUNDS
    Publication number: 20130217662
    Abstract: Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.
    Type: Application
    Filed: September 13, 2012
    Publication date: August 22, 2013
    Inventors: Steven W. Andrews, Julia Haas, Yutong Jiang, Gan Zhang
  • PYRAZOLOPYRIMIDINYL INHIBITORS OF UBIQUITIN-ACTIVATING ENZYME
    Publication number: 20130217682
    Abstract: Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 22, 2013
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventor: Millennium Pharmaceuticals, Inc.
  • Tetrahydro-imidazo[1,5-?] pyrazine derivatives, preparation process and medicinal use thereof
    Patent number: 8513411
    Abstract: Tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I), their preparation methods, pharmaceutical compositions containing the derivatives and uses thereof as medicaments, especially as dipeptidyl peptidase IV inhibitors, wherein the substituents of formula (I) are defined as same as the description.
    Type: Grant
    Filed: May 3, 2012
    Date of Patent: August 20, 2013
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Peng Cho Tang, Fanglong Yang, Jiang Fan, Hu Feng, Yang Wang, Tao Yang
  • BICYCLIC HETEROARYL KINASE INHIBITORS AND METHODS OF USE
    Publication number: 20130203755
    Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.
    Type: Application
    Filed: May 24, 2011
    Publication date: August 8, 2013
    Applicant: UNIVERSITY OF ROCHESTER
    Inventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Torsten Wiemann, Satheesh Babu Ravula, Colin J. Loweth
  • Inhibitors of Human Immunodeficiency Virus Replication
    Publication number: 20130203748
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Application
    Filed: August 9, 2012
    Publication date: August 8, 2013
    Inventors: B. Narasimhulu Naidu, Manoj Patel
  • Heterocyclic compound and use thereof
    Patent number: 8501750
    Abstract: Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: August 6, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takanobu Kuroita, Hideyuki Igawa, Hiroki Sakamoto, Kouhei Asano, Minoru Sasaki
  • HETEROCYCLIC ALKYNYL BENZENE COMPOUNDS AND MEDICAL COMPOSITIONS AND USES THEREOF
    Publication number: 20130196985
    Abstract: The heterocyclic alkynyl benzene compounds of formula (I), their pharmaceutically acceptable salts and stereoisomers thereof, as well as application in preparing drugs for preventing or treating tumors. The compounds can overcome the clinically induced resistance against Gleevec.
    Type: Application
    Filed: June 3, 2011
    Publication date: August 1, 2013
    Applicant: Guangzzhou Institute of Biomedicine and Health, Chineses Academy of Sciences
    Inventors: Ke Ding, Deping Wang, Duanqing Pei, Zhang Zhang, Mengjie Shen, Kun Luo, Yubing Feng
  • TRIAZOLOPYRAZINONES AS P2X7 RECEPTOR ANTAGONISTS
    Publication number: 20130196986
    Abstract: The invention provides certain 3,7-disubstituted-[1,2,4]triazolo[4,3-a]pyrazin-8(7H)-ones of the Formula (I), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R8, and X are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating pain or an inflammatory disease.
    Type: Application
    Filed: September 16, 2011
    Publication date: August 1, 2013
    Inventors: Marc Labroli, Michael F. Czarniecki, Cory Seth Poker
  • SUBSTITUTED QUINAZOLINE AND PYRIDO-PYRIMIDINE DERIVATIVES
    Publication number: 20130190492
    Abstract: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
    Type: Application
    Filed: March 7, 2013
    Publication date: July 25, 2013
    Applicant: Endo Pharmaceuticals Inc.
    Inventor: Endo Pharmaceuticals Inc.
  • BICYCLIC PYRIMIDINES
    Publication number: 20130184273
    Abstract: Compounds of formula (I), which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
    Type: Application
    Filed: July 11, 2011
    Publication date: July 18, 2013
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Stuart Ince, Hartmut Rehwinkel, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer
  • TETRAHYDROPYRIDO-PYRIDINE AND TETRAHYDROPYRIDO-PYRIMIDINE COMPOUNDS AND USE THEREOF AS C5A RECEPTOR MODULATORS
    Publication number: 20130184253
    Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: July 19, 2012
    Publication date: July 18, 2013
    Applicant: NOVARTIS AG
    Inventors: Christopher Michael ADAMS, Veronique DARSIGNY, Alec Nathanson FLYER, Christine Fang GELIN, Timothy Brian Hurley, Nan JI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Erik MEREDITH, Chang RAO, Michael H. SERRANO-WU, Catherine Fooks SOLOVAY
  • Compounds for the reduction of ?-amyloid production
    Patent number: 8486952
    Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: July 16, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
  • Pyrazolo[1,5-a]pyrimidines for antiviral treatment
    Patent number: 8486938
    Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Grant
    Filed: June 23, 2011
    Date of Patent: July 16, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Constantine G. Boojamra, Eugene J. Eisenberg, Hon Chung Hui, Richard L. Mackman, Jay P. Parrish, Michael Sangi, Oliver L. Saunders, Dustin Siegel, David Sperandio, Hai Yang
  • COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION
    Publication number: 20130178462
    Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 11, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • FUSED BICYCLIC mTOR INHIBITORS
    Publication number: 20130165651
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Application
    Filed: February 15, 2013
    Publication date: June 27, 2013
    Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joseph Mulvihill, Paula A.R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
  • Inhibitors of VEGF receptor and HGF receptor signalling
    Patent number: 8470850
    Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: June 25, 2013
    Assignee: MethylGene Inc.
    Inventors: Arkadii Vaisburg, Stephen William Claridge, Franck Raeppel, Oscar Mario Saavedra, Noemy Berstein, Marie-Claude Granger, Lijie Zhan, Amal Wahhab, David Liewellyn
  • NOVEL COMPOUND ACTING AS A CANNABINOID RECEPTOR-1 INHIBITOR
    Publication number: 20130158025
    Abstract: Disclosed is a novel compound acting as a cannabinoid receptor 1 inhibitor, a prodrug thereof, an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof. The novel compound or the like is useful for preventing or treating diseases mediated by the cannabinoid receptor-1.
    Type: Application
    Filed: August 31, 2011
    Publication date: June 20, 2013
    Applicant: AMOREPACIFIC CORPORATION
    Inventors: Song Seok Shin, Yong Deog Hong, Kyoung Hee Byoun, Mi Young Park, Jin Kyu Choi, Yang Hui Park, Il Hong Bae, Yung Hyup Joo, Kyung Min Lim, Young Ho Park
  • INHIBITORS OF BRUTON'S TYROSINE KINASE
    Publication number: 20130150360
    Abstract: This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 13, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
    Publication number: 20130150362
    Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.
    Type: Application
    Filed: August 22, 2011
    Publication date: June 13, 2013
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Lianyun Zhao, Duan Liu, Shuyi Tang, Amit K. Mandal, Umar Faruk Mansoor, Lalanthi Dilrukshi Vitharana, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
  • Phosphoinositide 3-kinase inhibitors with a zinc binding moiety
    Patent number: 8461157
    Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: June 11, 2013
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Changgeng Qian
  • 2-Substituted phenyl-5,7-dihydrocarbyl-3,7-dihydropyrrolo[2,3-d] pyrimidin-4-one derivatives, the preparation and the pharmaceutical use thereof
    Patent number: 8461165
    Abstract: The invention relates to the compounds of formula I, their preparation and the pharmaceutical compositions containing the compounds. The invention also relates to the use of the compounds of formula I in preparing medicines, which can treat sexual dysfunction of animals including human (male and female), especially erectile dysfunction of male and the diseases in which the function of phospholipase 5 (cGMP PDE5) is involved.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: June 11, 2013
    Assignees: Yangtze River Pharmaceutical (Group) Co., Ltd, Tianjin North Pharma Sci-Tech Co., Ltd
    Inventors: Yongfeng Wang, Kejun Zhao
  • Imidazopyrazine Syk inhibitors
    Patent number: 8455493
    Abstract: Certain imidazopyrazines of Formula (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: June 4, 2013
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford, James P. Harding, Antonio J. M. Barbosa, Jr., Zhongdong Zhao, Soumya Mitra, David M. Armistead
  • HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS
    Publication number: 20130137681
    Abstract: The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
    Type: Application
    Filed: January 30, 2013
    Publication date: May 30, 2013
    Applicant: INCYTE CORPORATION
    Inventor: INCYTE CORPORATION
  • OXOPYRAZINE DERIVATIVE AND HERBICIDE
    Publication number: 20130137577
    Abstract: The present invention is to provide an oxopyrazine derivative having an excellent herbicidal activity and besides exhibiting high safety for useful crops and the like, or a salt thereof, and a herbicide containing the same. The present invention relates to an oxopyrazine derivative represented by formula [I]: wherein X1 represents an oxygen atom or a sulfur atom; X2 represents CH or N(O)m; m represents an integer of 0 or 1; R1 represents a hydrogen atom, a C1-C12 alkyl group and the like; R2 represents a halogen atom, a cyano group and the like; R3 is a hydroxyl group, a halogen atom and the like; A1 represents C(R4R5); A2 represents C(R6R7) or C?O; A3 represents C(R8R9); R4 to R9 represent a hydrogen atom or an alkyl group, or a salt thereof, and a herbicide containing these compounds.
    Type: Application
    Filed: January 17, 2013
    Publication date: May 30, 2013
    Applicants: IHARA CHEMICAL INDUSTRY CO., LTD., KUMIAI CHEMICAL INDUSTRY CO., LTD.
    Inventors: KUMIAI CHEMICAL INDUSTRY CO., LTD., IHARA CHEMICAL INDUSTRY CO., LTD.
  • 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
    Patent number: 8450321
    Abstract: An imidazopyrazine having the structure or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: May 28, 2013
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie
  • Pyrimidopyridazine derivatives useful as P38 MAPK inhibitors
    Patent number: 8450314
    Abstract: A compound formula (IA) or (IB), or a pharmaceutically acceptable thereof; wherein the substituents are defined as in the claims, and their use as P38 MAP kinase.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: May 28, 2013
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Amanda Beswick, Bohdan Waszkowycz
  • 5,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES AS INHIBITORS OF JAK KINASES
    Publication number: 20130131039
    Abstract: Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
    Type: Application
    Filed: April 11, 2011
    Publication date: May 23, 2013
    Applicant: Array BioPharma Inc.
    Inventors: Laurence E. Burgess, Mark Laurence Boys, Robert D. Groneberg, Darren M. Harvey, Timothy Kercher, Christopher F. Kraser, Ellen Laird, Eugene Tarlton, Qian Zhao, Lily Huang
  • 2-SUBSTITUTED-8-ALKYL-7-OXO-7,8-DIHYDROPYRIDO[2,3-D] PYRIMIDINE-6-CARBONITRILES AND USES THEREOF
    Publication number: 20130131058
    Abstract: Compounds according to Formula (I), as well salts thereof: wherein R1 and R2 are as defined herein, are useful as antiproliferative agents and kinase inhibitors. Synthetic methods for preparing the compounds of Formula (I) are also provided.
    Type: Application
    Filed: July 21, 2011
    Publication date: May 23, 2013
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • NEW BICYCLIC COMPOUNDS AS PI3-K AND MTOR INHIBITORS
    Publication number: 20130131057
    Abstract: There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
    Type: Application
    Filed: May 13, 2011
    Publication date: May 23, 2013
    Applicant: CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO
    Inventors: Joaquin Pastor Fernández, Sonia Martínez Gonzalez, Antonlo Rodriguez Hergueta, Francisco Javier Ramos Lima, Rosa Maria Alvarez Escobar, Ana Isabel Higueras Hernandez
  • ACC INHIBITORS AND USES THEREOF
    Publication number: 20130123231
    Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
    Type: Application
    Filed: November 9, 2012
    Publication date: May 16, 2013
    Applicant: Nimbus Apollo, Inc.
    Inventor: Nimbus Apollo, Inc.
  • Imidazopyrazine Syk inhibitors
    Patent number: 8440667
    Abstract: Certain imidazopyrazines of Formula (I): and pharmaceutical compositions thereof are provided herein. Methods of treating patients responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity of Formula (I) effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: May 14, 2013
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford
  • Pyrido[3,2-d]pyrimidine PI3K delta inhibitor compounds and methods of use
    Patent number: 8440651
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I 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: Grant
    Filed: February 18, 2011
    Date of Patent: May 14, 2013
    Assignee: F. Hoffmann-La Roche AG
    Inventors: Georgette Castanedo, Bryan Chan, Matthew C. Lucas, Brian Safina, Daniel P. Sutherlin, Zachary Sweeney