Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/278)
-
Publication number: 20110281874Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: July 27, 2011Publication date: November 17, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas D. AICHER, Steven Armen BOYD, Mark Joseph CHICARELLI, Kevin Ronald CONDROSKI, Ronald Jay HINKLIN, Ajay SINGH
-
Patent number: 8058280Abstract: The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a hydroxy group, (3?) a C1-4 alkyl and (4?) a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1?) a halogen, (2?) a C1-4 alkoxy-C1-4 alkyl, (3?) a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4?) a C1-4 alkoxy and (5?) a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.Type: GrantFiled: August 31, 2007Date of Patent: November 15, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Nobuo Cho, Takashi Imada, Takenori Hitaka, Kazuhiro Miwa, Masami Kusaka, Nobuhiro Suzuki
-
Publication number: 20110275645Abstract: The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity.Type: ApplicationFiled: May 5, 2010Publication date: November 10, 2011Inventors: Renee Desai, Ketan Desai
-
Publication number: 20110269773Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula (I): Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: July 5, 2007Publication date: November 3, 2011Inventors: Ian S. Mitchell, James F. Blake, Rul Xu, Nicholas C. Kallan, Dengming Xiao, Keith Lee Spencer, Jose R. Bencsik
-
Publication number: 20110269772Abstract: Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Applicant: SUPERGEN, INC.Inventors: David J. BEARSS, Hariprasad VANKAYALAPATI, Yong XU
-
Publication number: 20110263532Abstract: The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications.Type: ApplicationFiled: August 11, 2009Publication date: October 27, 2011Applicant: President and Fellows of Harvard CollegeInventors: Tracy Keller, Ralph Mazitschek, Malcolm Whitman, Jinbo Lee
-
Publication number: 20110251216Abstract: The present invention relates to therapeutic targets for cancer. In particular, the present invention relates to small molecules and nucleic acids that target EZH2 expression in cancer (e.g., prostate cancer, breast cancer, other solid tumors, multiple myeloma).Type: ApplicationFiled: February 10, 2011Publication date: October 13, 2011Applicant: The Regents of The University of MichiganInventors: Arul M. Chinnaiyan, Sooryanaryana Lnu, Qi Cao
-
Publication number: 20110230476Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: September 9, 2010Publication date: September 22, 2011Applicant: AVILA THERAPEUTICS, INC.Inventors: DEQIANG NIU, RUSSELL C. PETTER, JUSWINDER SINGH, ARTHUR F. KLUGE, HORMOZ MAZDIYASNI, ZHENDONG ZHU, LIXIN QIAO, KEVIN KUNTZ
-
Patent number: 8022076Abstract: This invention relates to novel compound of formula (I) or pharmaceutically acceptable salts thereof. The invention is also directed to the uses of compounds having formula (I) in the treatment or prevention of diseases or disorders which requires potassium channel inhibition to an animal, mammal or human in need thereof. The invention is also directed to the use of compounds having formula (I) in the treatment or prevention of arrhythmia to an animal, mammal or human in need thereof.Type: GrantFiled: June 10, 2004Date of Patent: September 20, 2011Assignee: Xention LimitedInventors: John Ford, Nicholas John Palmer, John Frederick Atherall, David John Madge, Brad Sherborne, Mark Bushfield, Edward Benedict Stevens
-
Publication number: 20110224155Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.Type: ApplicationFiled: June 3, 2008Publication date: September 15, 2011Applicant: SENOMYX INC.Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
-
Publication number: 20110224197Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, such as inhibitors of GSK-3. The invention provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. The invention provides processes for preparing compounds of the invention. The invention provides methods of identifying compounds useful for treatment of diabetes, diabetic neuropathy, osteoporosis, Alzheimer's disease, Huntington's disease, Parkinson's disease, AIDS-associated dementia, bipolar disorder, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, leukocytopenia, cardiomyocyte hypertrophy, stroke, post-stroke, spinal cord injury, traumatic brain injury, Charcot-Marie-Tooth, peripheral nerve regeneration, and rheumatoid arthritis.Type: ApplicationFiled: September 9, 2010Publication date: September 15, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Gregory William Henkel, Michael Liu, Timothy Neuberger
-
Publication number: 20110217311Abstract: The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use 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: February 25, 2011Publication date: September 8, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten LEHMANN-LINTZ, Armin HECKEL, Joerg KLEY, Elke LANGKOPF, Nobert REDEMANN, Achim SAUER, Leo THOMAS, Dieter WIEDENMAYER, Matthias AUSTEN, John DANILEWICZ, Martin SCHNEIDER, Kay SCHREITER, Phillip BLACK, Wesley BLACKABY, Ian LINNEY
-
Publication number: 20110218338Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritus.Type: ApplicationFiled: April 11, 2011Publication date: September 8, 2011Inventors: Hui Cai, Frank Chavez, James P. Edwards, Anne E. Fitzgerald, Jing Liu, Neelakandha S. Mani, Danielle K. Neff, Michele C. Rizzolio, Brad M. Savall, Deborah M. Smith, Jennifer D. Venable, Jianmei Wei, Ronald L. Wolin
-
Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
Patent number: 8012965Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: December 28, 2007Date of Patent: September 6, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20110212937Abstract: 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: ApplicationFiled: July 28, 2010Publication date: September 1, 2011Inventors: 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
-
Publication number: 20110212103Abstract: The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use 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: February 25, 2011Publication date: September 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Armin HECKEL, Frank HIMMELSBACH, Joerg KLEY, Thorsten LEHMANN-LINTZ, Norbert REDEMANN, Achim SAUER, Leo THOMAS, Dieter WIEDENMAYER, Phillip BLACK, Wesley BLACKABY, Ian LINNEY, Matthias AUSTEN, John DANILEWICZ, Martin SCHNEIDER, Kay SCHREITER
-
Publication number: 20110212102Abstract: 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: February 25, 2011Publication date: September 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten LEHMANN-LINTZ, Joerg KLEY, Norbert REDEMANN, Achim SAUER, Leo THOMAS, Dieter WIEDENMAYER, Matthias AUSTEN, John DANILEWICZ, Martin SCHNEIDER, Kay SCHREITER, Phillip BLACK, Wesley BLACKABY, Ian LINNEY
-
Patent number: 8008487Abstract: The present invention provides compounds of formula (I), thieno[2,3-d]pyrimidines, having fungicidal activity.Type: GrantFiled: October 21, 2005Date of Patent: August 30, 2011Assignee: Dow AgroSciences LLCInventors: William Kirkland Brewster, Carla Jean Rasmussen Klittich, Terry William Balko, Nneka Tuere Breaux, William Randal Erickson, James Edward Hunter, Christian Thomas Lowe, Michael John Ricks, Thomas Lyman Siddall, Carla Nanette Yerkes, Yuanming Zhu
-
Patent number: 8003656Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: GrantFiled: August 22, 2007Date of Patent: August 23, 2011Assignee: Neurogen CorporationInventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
-
Publication number: 20110201628Abstract: The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer.Type: ApplicationFiled: September 29, 2009Publication date: August 18, 2011Inventors: Claudio Edmundo Chuaqui, Shan Huang, Stephanos Ioannidis, Jie Shi, Mei Su, Qibin Su
-
Publication number: 20110190241Abstract: Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro.Type: ApplicationFiled: May 14, 2009Publication date: August 4, 2011Inventors: Lori Emert-Sedlak, Toshiaki Kodama, Billy W. Day, Weixiang Dai, Ronald P. Trible, Thomas E. Smithgall
-
Patent number: 7989445Abstract: The present invention relates to a compound represented by the formula: wherein Ar is an optionally substituted ring; A is a spacer having a main chain of 1 to 4 atoms; B is a bond, a C1-10 alkylene group or an oxygen atom; R3 and R5 are each independently a hydrogen atom or a substituent; R4 is an optionally substituted cyclic group or an optionally substituted C1-10 alkyl group; and R1 and R2 are each independently a hydrogen atom or a substituent, or R1 and R2 or R1 and B are bonded to form an optionally substituted nitrogen-containing heterocycle, or R1 and Ar are bonded to form an optionally substituted nitrogen-containing fused heterocycle, or a salt thereof. The thienopyrimidone compound of the present invention has a superior melanin-concentrating hormone receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of obesity and the like.Type: GrantFiled: April 27, 2006Date of Patent: August 2, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Toshiki Murata, Shingo Makino
-
Patent number: 7989433Abstract: The present invention provides compounds having the following Formula IA and IB, which are useful as MCHR1 antagonists, and includes prodrugs and pharmaceutically acceptable salts thereof:Type: GrantFiled: May 28, 2009Date of Patent: August 2, 2011Assignee: Bristol-Myers Squibb CompanyInventors: William N. Washburn, Pratik Devasthale, Jeffrey A. Robl
-
Publication number: 20110183992Abstract: Provided are therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof; therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity, which has an affinity for the adenosine A2A receptor 10 times or higher than that for the adenosine A1 receptor, or a pharmaceutically acceptable salt thereof; and the like.Type: ApplicationFiled: July 23, 2009Publication date: July 28, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Junichi Ikeda, Shunji Ichikawa, Masako Kurokawa, Tomoyuki Kanda
-
Publication number: 20110178294Abstract: Carboxylic acid derivatives where R—R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: ApplicationFiled: December 3, 2010Publication date: July 21, 2011Applicant: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Vogelbacher, Wolfgang Wernet, Andrea Hager-Wernet, Liliane Unger, Manfred Raschack
-
Publication number: 20110172249Abstract: The present invention provides a method for improving absorbability of the active ingredient of an enteric polymer coated preparation, which includes using an organic acid.Type: ApplicationFiled: September 2, 2009Publication date: July 14, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMTEDInventors: Kazuhisa Kamikawa, Takayuki Okabe, Miho Nakamura
-
Publication number: 20110166116Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.Type: ApplicationFiled: June 23, 2010Publication date: July 7, 2011Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, NEUROCRINE BIOSCIENCES, INC.Inventors: Brian DYCK, Joe A. TRAN, Junko TAMIYA, Florence JOVIC, Troy VICKERS, Chen CHEN, Nicole HARRIOTT, Timothy COON, Neil J. ASHWEEK
-
Publication number: 20110165183Abstract: The invention provides a compound of formula (I): wherein W is a bicyclic heteroaromatic group; or a salt thereof. The compounds and salts thereof have beneficial therapeutic properties (e.g. immunosuppressant properties).Type: ApplicationFiled: July 31, 2009Publication date: July 7, 2011Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin L. Kotian, V. Satish Kumar
-
Publication number: 20110166163Abstract: The present application relates to novel substituted furopyrimidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular diseases.Type: ApplicationFiled: June 3, 2008Publication date: July 7, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Thomas Lampe, Raimund Kast, Mario Jeske, Friederike Stoll, Joachim Schuhmacher, Eva-Maria Becker, Hartmut Beck
-
Publication number: 20110165118Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: November 13, 2008Publication date: July 7, 2011Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
-
Publication number: 20110166121Abstract: The present invention relates to a fused heterocyclic compound having the Formula 1, which is useful as a platelet aggregation inhibitor, a method for preparing the same, and a pharmaceutical composition for inhibiting platelet aggregation comprising the same.Type: ApplicationFiled: September 8, 2009Publication date: July 7, 2011Applicant: LG LIFE SCIENCES LTD.Inventors: Chang Seok Lee, Tae Hee Lee, Sook Kyung Yoon, Jeung Soon Choi, Yong Jin Jang, Sung Wook Kim, Hye Kyung Chang, Mi Jeong Park, Tae Hun Kim, Young Ha Ahn, Hee Dong Park, Hyun Jung Park, Dong Chul Lim, Joo Youn Lee, Sung Hack Lee, Wan Su Park, Yeong Soo Oh
-
Publication number: 20110160207Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: March 2, 2011Publication date: June 30, 2011Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
-
Patent number: 7968536Abstract: The present invention provides compounds useful as inhibitors of protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: GrantFiled: June 30, 2008Date of Patent: June 28, 2011Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.Inventors: Jennifer Cossrow, Bing Guan, Alexey Ishchenko, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
-
Publication number: 20110152259Abstract: The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: and L is selected from the group consisting of: pharmaceutically compositions comprising one or more compounds of formula (I), and methods of using the compounds of formula (I).Type: ApplicationFiled: February 24, 2011Publication date: June 23, 2011Inventors: Anandan Palani, Jing Su, Dong Xiao, Xianhai Huang, Ashwin U. Rao, Xiao Chen, Haiqun Tang, Jun Qin, Ying R. Huang, Robert G. Aslanian, Brain A. McKittrick, Syliva J. Degrado
-
Publication number: 20110152242Abstract: A compound of formula (I), wherein W is formula (1); A is a benzene ring, a fÊve-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; n is zero, one, two or three; when n is zero or one, V is CH2; when n is two or three, V is CH2, O or NR5; when V is CH2, the bond formed by V and an adjacent carbon ring atom is optionally fused to a phenyl ring, a five-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; the ring being optionally substituted by one or more R1 groups; and R7 and R8 are independently hydrogen, hydroxy, halogen or C1-4alkyl; Z is a phenyl ring, a five-membered heteroaromatic ring containing one, two, three or four heteroatoms independently chosen from O, N or S, atType: ApplicationFiled: March 21, 2006Publication date: June 23, 2011Inventors: Tracy Bayliss, Rebecca Elizabeth Brown, Gregory John Hollingworth, Brian A. Jones, Christopher Richard Moyes, Lauren Rogers
-
Publication number: 20110144321Abstract: The invention provides novel synthetic intermediates and processes that can be used to prepare compounds of formula (I), wherein R1 has any of the values described herein and R2 is a nucleoside sugar group.Type: ApplicationFiled: July 22, 2009Publication date: June 16, 2011Applicant: BIOCRYST PHARMACEUTICALS, INC.Inventors: Pooran Chand, Minwan Wu, Pravin L. Kotian, V. Satish Kumar, Tsu-Hsing Lin
-
Patent number: 7960382Abstract: Novel compounds and their uses are disclosed herein.Type: GrantFiled: April 13, 2009Date of Patent: June 14, 2011Assignee: Allergan, Inc.Inventors: Stephen Ruckmick, Robert Cain, Milton J. Abreo, Massoud Fahid, Brent A. Johnson
-
Publication number: 20110130563Abstract: The present invention relates to an improved process for the preparation of dihydrothieno[3,2-d]pyrimidine diols, and similar pyrimidine diols, that is efficient, high-yielding, and does not require expensive and potentially unstable intermediates. The diols are used as intermediates in the synthesis of pyrimidine compounds which inhibit PDE4, and are thus useful in the treatment of respiratory or gastrointestinal diseases and complaints, peripheral or central nervous system diseases and disorders, inflammatory conditions, and cancers.Type: ApplicationFiled: May 7, 2009Publication date: June 2, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Rogelio Perez Frutos, Thomas G. Tampone, Jason Alan Mulder, Dhileepkumar Krishnamurthy, Chris Hugh Senanayake
-
Patent number: 7951812Abstract: The present invention is directed to antifolate compounds having the structure wherein: X is CHR9 or NR9; Y1, Y2, and Y3 independently are O or S; V1 and V2 independently are O, S, or NZ; Z is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, or alkaryl; R1 and R2 independently are H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, or alkaryl; R3 is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, hydroxyl, or halo; and R4, R5, R6, R7, R8, and R9 independently are H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, acyl, —C(O)-alkyl, —C(O)-alkenyl, or —C(O)—alkynyl; as well as pharmaceutically acceptable esters, amides, salts, solvates, and prodrugs thereof.Type: GrantFiled: January 18, 2008Date of Patent: May 31, 2011Assignee: Chelsea Therapeutics, Inc.Inventors: Michael J. Roberts, Simon Pedder
-
Publication number: 20110124665Abstract: The present application relates to novel, cyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.Type: ApplicationFiled: December 8, 2006Publication date: May 26, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Thomas Lampe, Eva-Maria Becker, Raimund Kast, Hartmut Beck, Mario Jeske, Joachim Schuhmacher, Friederike Stoll, Martina Klein, Metin Akbaba, Andreas Knorr, Johannes-Peter Stasch, Lars Bärfacker, Alexander Hillisch, Gunter Karig, Mark Meininghaus, Karl-Heinz Schlemmer, Rudolf Schohe-Loop
-
Patent number: 7947691Abstract: Acrylic n-hydroxy imides and their use in pharmaceutical compositions and in the inhibition of flap endonuclease are disclosed.Type: GrantFiled: July 20, 2005Date of Patent: May 24, 2011Assignee: Athersys, Inc.Inventors: Lawrence N. Tumey, Youssef Bennani, Bayard Huck, David C. Bom
-
Patent number: 7947690Abstract: The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, —O-(lower alkyl), halogen atom, carboxyl, —CO2-(lower alkyl), and carbamoyl, R1 represents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and R2 represents a group represented by formula (II) or an optionally substituted cyclic amino: wherein R21 and R22 may be identical or different and each represents —H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or —O-(lower alkyl), each of which is optionally substituted.Type: GrantFiled: October 17, 2005Date of Patent: May 24, 2011Assignee: Astellas Pharma Inc.Inventors: Yasuhiro Yonetoku, Kenji Negoro, Kenichi Onda, Masahiko Hayakawa, Daisuke Sasuga, Takahiro Nigawara, Kazuhiko Iikubo, Hiroyuki Moritomo, Shigeru Yoshida, Takahide Ohishi
-
Publication number: 20110118284Abstract: Compounds of formula (I) are A2B receptor antagonists, wherein R1 is optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; R2 and R3 are independently selected from hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl-(C1-C6)-alkyl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C1-C6 alkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or R2 and R3 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R4 is C1-C3 alkyl, C2-C3 alkenyl, —N(—R5)—R6, or optionally substituted heteroarylmethylamino; and R5 and R6 are independently selected from hydrogen or C1-C3 alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated ring.Type: ApplicationFiled: September 19, 2008Publication date: May 19, 2011Applicant: VERNALIS (R&D) LTD.Inventors: Allan Jordan, Simon Bedford, Klenke Burkhard, Ian Yule, Karine Poullennec
-
Publication number: 20110104109Abstract: The present invention relates to Tetracyclic Indole Derivatives, compositions comprising at least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Frank Bennett, Qingbei Zeng, Srikanth Venkatraman, Mousumi Sannigrahi, Kevin X. Chen, Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
-
Publication number: 20110092499Abstract: The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: November 14, 2008Publication date: April 21, 2011Applicant: YM BIOSCIENCES AUSTRALIA PTY LTDInventors: David Gerard Bourke, Christopher John Burns, Antony Nicholas Cuzzupe, John Thomas Feutrill, Marcel Robert Kling, Tracy Leah Nero
-
Patent number: 7928111Abstract: The present invention provides compounds including substituted thienopyrimidinone derivatives of Formula (IIc) as ligands for modulating chemosensory receptors: These compounds are useful as sweet taste enhancers in comestible or medicinal compositions. The present invention also provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.Type: GrantFiled: August 8, 2007Date of Patent: April 19, 2011Assignee: Senomyx, Inc.Inventors: Catherine Tachdjian, Xiao-Qing Tang, Sara Werner, Marketa Rinnova, Qing Chen, Guy Servant, Xiaodong Li, Feng Zhang, Haitian Liu, Albert Zlotnik, Mark Zoller, Boris Klebansky, Richard Fine, Xinshan Kang
-
Publication number: 20110086865Abstract: The invention relates to molecules ANT-ligands having a substituted nitrogeneous heterocycle A wherein —A is a substituted pyrazinone of formula I wherein R1 is —(CH2)n —CO—OH; —(CH2)n —CO—OR; —(CH2)n —CO—NHR; —(CH2)n —CO—N(R, R?); —(CH2)n —OH; —(CH2)n —OR; —(CH2)n —OAr; —(CH2)n —C(R,R?) —(CH2)n —OH, R and R?, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het.Type: ApplicationFiled: May 29, 2009Publication date: April 14, 2011Applicant: MITOLOGICSInventors: Annie Borgne-Sanchez, Etienne Jacotot, Catherine Brenner
-
Publication number: 20110082158Abstract: Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula II: These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase and/or other folate metabolizing enzymes in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.Type: ApplicationFiled: October 12, 2010Publication date: April 7, 2011Inventors: Aleem Gangjee, Larry H. Matherly
-
Publication number: 20110082157Abstract: The invention relates to 5-HT receptor antagonists. Novel piperidinylamino-thieno [2,3-d] pyrimidine compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include central nervous system disorders such as pulmonary arterial hypertension, migraine, hypertension, disorders of the gastrointestinal tract, restenosis, asthma, obstructive airway disease, prostatic hyperplasia and priapism, anxiety, depression, schizophrenia, neural injury and stroke. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also provided.Type: ApplicationFiled: June 8, 2010Publication date: April 7, 2011Inventors: Dale S. Dhanoa, Oren Becker, Silvia Noiman, Sekar A. Reddy, Srinivasa Rao Cheruku, Rosa E. Mele'ndez, Anurag Sharadendu, Dongli Chen, Yael Marantz, Sharon Shacham, Alexander Heifetz, Boaz Inbal, Venkitasamy Kesavan, Shay Bar-Haim
-
Patent number: 7915267Abstract: The present invention provides a novel amide compound represented by the following formula, which has a matrix metalloproteinase inhibitory activity and is useful as a pharmaceutical agent. wherein each symbol is as defined in the specification.Type: GrantFiled: October 27, 2006Date of Patent: March 29, 2011Assignee: Takeda Pharmaceutical Company LimitedInventors: Hiroshi Nara, Akira Kaieda, Kenjiro Sato, Jun Terauchi