Ring Chalcogen In The Bicyclo Ring System Patents (Class 514/260.1)
  • Publication number: 20140206703
    Abstract: The present invention relates to thienopyrimidine compounds which are potassium channel inhibitors. Pharmaceutical compositions comprising the compounds and their use in the treatment of arrhythmia are also described.
    Type: Application
    Filed: March 29, 2012
    Publication date: July 24, 2014
    Applicant: XENTION LIMITED
    Inventors: John Ford, Derek Edward John
  • Publication number: 20140206684
    Abstract: Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Applicant: INTELLIKINE LLC
    Inventors: Pingda REN, Yi LIU, Troy Edward WILSON, Katrina CHAN, Christian ROMMEL, Liansheng LI
  • Patent number: 8765771
    Abstract: The present invention relates to provision of a novel compound that has an activity of promoting insulin secretion from pancreatic ? cells and thus is useful as a prophylaxis and/or therapeutic agent for diseases caused by hyperglycemia such as diabetes mellitus, and the compound represented by the following formula (1): wherein one of A and B represents a nitrogen atom and the other represents a nitrogen atom or CR10, X represents an oxygen atom, a sulfur atom or —(CH2)n-N(R12)—, Y represents an oxygen atom, a sulfur atom or —N(R13)—, and R1 to R9 each represent a hydrogen atom or another substituent, or a salt thereof, or a solvate of the compound or the salt.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: July 1, 2014
    Assignee: Kowa Co., Ltd.
    Inventors: Toshiharu Morimoto, Tomoaki Koshizawa, Gen Watanabe, Tadaaki Ohgiya, Nao Yamasaki, Noriyuki Inoue
  • Patent number: 8765755
    Abstract: 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: Grant
    Filed: December 5, 2012
    Date of Patent: July 1, 2014
    Assignee: YM Biosciences Australia Pty Ltd.
    Inventors: David Gerard Bourke, Christopher John Burns, Anthony Nicholas Cuzzupe, John Thomas Feutrill, Marcel Robert Kling, Tracy Leah Nero
  • Patent number: 8765757
    Abstract: 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: Grant
    Filed: November 13, 2008
    Date of Patent: July 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
  • Patent number: 8759361
    Abstract: 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: Grant
    Filed: August 22, 2011
    Date of Patent: June 24, 2014
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
  • Publication number: 20140171408
    Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.
    Type: Application
    Filed: February 20, 2014
    Publication date: June 19, 2014
    Applicant: Genentech, Inc.
    Inventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum MacLeod, Steven R. Magnuson, Vickie Hsiao-Wei Tsui, Karen Williams, Birong Zhang
  • Publication number: 20140170162
    Abstract: The invention relates to treatment and/or prevention of nerve injury. In one embodiment, the present invention provides a method of preserving the neuromuscular junction (NMJ) in an individual by administering a therapeutically effective dosage of a composition comprising an inhibitor of Wnt3a, and an inhibitor of MMP3 to the individual. In another embodiment, the present invention provides a method of stabilizing NMJ after nerve injury by inhibiting the WNT and beta-catenin signaling pathway and preserving agrin.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventor: Ranjan Gupta
  • Publication number: 20140171428
    Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, traumatic nerve injury, and depression. This invention is useful for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.
    Type: Application
    Filed: November 13, 2013
    Publication date: June 19, 2014
    Applicant: NEURONASCENT, INC.
    Inventor: Judith KELLEHER-ANDERSSON
  • Patent number: 8754073
    Abstract: Piperidinodihydrothienopyrimidines of formula 1 wherein X is SO or SO2 (preferably SO), and R1, R2, R3, and R4 may have the meanings given in the disclosure and claims, pharmacologically acceptable salts thereof, and pharmaceutical compositions containing these compounds. These piperidinodihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system, or cancers.
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: June 17, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pascale Pouzet, Ralf Anderskewitz, Horst Dollinger, Dennis Fiegen, Thomas Fox, Rolf Goeggel, Christoph Hoenke, Domnic Martyres, Peter Nickolaus, Klaus Klinder
  • Patent number: 8754079
    Abstract: 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: Grant
    Filed: February 25, 2011
    Date of Patent: June 17, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Joerg Kley, Elke Langkopf, Norbert Redemann, Achim Sauer, Leo Thomas, Dieter Wiedenmayer, Matthias Austen, John Danilewicz, Martin Schneider, Kay Schreiter, Phillip Black, Wesley Blackaby, Ian Linney
  • Patent number: 8748436
    Abstract: The invention relates to oxazolopyrimidine compounds of formula (I), where A, R1, R2, R3, R4 and X are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: June 10, 2014
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Andreas Gille, Katrin Hiss
  • Patent number: 8748437
    Abstract: The invention provides a crystal of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid (which has the chemical structure shown below) and a mixed crystal comprising such a crystal. The invention also provides methods of producing such crystals, pharmaceutical compositions comprising such crystals, and methods of modulating phosphodiesterase-9 activity and treating disorders such as overactive bladder syndrome by administration of an effective amount of the crystals.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: June 10, 2014
    Assignee: ASKA Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Hayashi, Takayoshi Nakagawa, Koichi Miyazaki
  • Publication number: 20140155386
    Abstract: 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: Application
    Filed: December 2, 2013
    Publication date: June 5, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak
  • Publication number: 20140148433
    Abstract: The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: August 31, 2011
    Publication date: May 29, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Lars Bärfacker, Stefan Weigand
  • Patent number: 8735402
    Abstract: The present invention relates to cycloalkyloxycarboxylic acid derivatives of the formula I in which A, R1, R2a, R2b, R2c, R3 and X are as defined in the claims. The compounds of the formula I are suitable, for example, for wound healing.
    Type: Grant
    Filed: June 25, 2012
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Thomas Huebschle, Katrin Hiss, Silke Haag-Diergarten
  • Patent number: 8735387
    Abstract: The present invention relates to oxazolopyrimidine compounds of the formula I in which A, R1, R2 and R3 are defined as indicated in the claims. The compounds of the formula I modulate the activity of the Edg-1 receptor and in particular are agonists of this receptor, and are useful for the treatment of diseases such as atherosclerosis, heart failure or peripheral arterial occlusive disease, for example. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Werngard Czechtizky
  • Patent number: 8735401
    Abstract: 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: Grant
    Filed: September 23, 2011
    Date of Patent: May 27, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nobuo Cho, Takashi Imada, Takenori Hitaka, Kazuhiro Miwa, Masami Kusuka, Nobuhiro Suzuki
  • Publication number: 20140134178
    Abstract: Phosphorylation of histones was observed at certain tyrosine residues which have not been associated with epigenetic modification. These sites include H2B Tyr37, H4 Tyr88 and Tyr51 and H3 Tyr99. Kinases responsible for the phosphorylation as well as downstream genes regulated by such phosphorylation were also identified. Antibodies that are specific to such phosphorylated histones have been generated, which are useful for detecting the phosphorylation and related events. With such findings, the present disclosure provides compositions and methods for disease diagnosis, prognosis and therapy selection, in particular for cancer, obesity and diabetes.
    Type: Application
    Filed: January 4, 2013
    Publication date: May 15, 2014
    Applicant: H. LEE MOFFIT CANCER CENTER AND RESEARCH INSTITUTE
    Inventors: Kiran Mahajan, Nupam P. Mahajan
  • Publication number: 20140128388
    Abstract: Drug candidates for inhibition of HIV-1 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-1 viral replication in vitro.
    Type: Application
    Filed: July 31, 2013
    Publication date: May 8, 2014
    Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education
    Inventors: Lori Emert-Sedlak, Toshiaki Kodama, Billy W. Day, Weixiang Dai, Ronald P. Trible, Thomas E. Smithgall
  • Patent number: 8716297
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, A, B, and n are defined in the description. The present invention relates also to compositions containing compounds of formula (I) which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: May 6, 2014
    Assignee: AbbVie Inc.
    Inventors: Keith W. Woods, Chunqui Lai, Thomas D. Penning, Julie M. Miyashiro
  • Publication number: 20140113877
    Abstract: The compounds of formula (1) in which A, X, R1, R2, R3 and R7 have the meanings as given in the description, are novel effective inhibitors of type 4 and type 5 phosphodiesterase.
    Type: Application
    Filed: June 12, 2012
    Publication date: April 24, 2014
    Applicant: Takeda GmbH
    Inventors: Dieter Flockerzi, Alexander Mann, Thomas Stengel, Harald Ohmer, Ulrich Kautz, Steffen Weinbrenner, Stefan Fischer, Hermann Tenor, Christof Zitt, Armin Hatzelmann, Torsten Dunkern, Christian Hesslinger, Clemens Braun, Ewald Benediktus, Andreas Pahl, Raimund Kuelzer, Degenhard Marx
  • Patent number: 8703777
    Abstract: Provided herein are substituted bicyclic compounds, e.g., compounds of Formula IV, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for inhibiting phosphatidyl inositol-3 kinase (PI3 kinase), e.g., for the treatment of various diseases and conditions associated with PI3 kinase activity, including but not limited to, cancer, inflammatory disease, immune disease, and respiratory disease.
    Type: Grant
    Filed: January 5, 2009
    Date of Patent: April 22, 2014
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Katrina Chan, Christian Rommel, Liansheng Li
  • Publication number: 20140107113
    Abstract: The present patent application relates to a pharmaceutical composition comprising a transient receptor potential ankyrin-1 receptor (“TRPA1”) antagonist and a beta-2 adrenergic receptor agonist (“beta-2 agonist”).
    Type: Application
    Filed: June 21, 2012
    Publication date: April 17, 2014
    Applicant: GLENMARK PHARMACEUTICALS S.A.
    Inventors: Neelima Khairatkar-Joshi, Abhay Kulkarni, Dinesh Pradeep Wale, Anil Hari Kadam, Thamil Selvan Vaiyapuri
  • Publication number: 20140107098
    Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
  • Patent number: 8697708
    Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: April 15, 2014
    Assignee: F. Hoffmann-La Roche AG
    Inventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven R. Magnuson, Vickie H. Tsui, Karen Williams, Birong Zhang
  • Patent number: 8691828
    Abstract: The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: April 8, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yuya Oguro, Osamu Kurasawa
  • Patent number: 8691829
    Abstract: The invention provides methods to treat certain liver disorders by administering a compound that inhibits PD K isoforms, particularly the delta isoform. It further provides specific compounds useful for these methods and ways to identify subjects who are particularly suitable for receiving these treatments.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: April 8, 2014
    Assignee: Gilead Calistoga LLC
    Inventor: Roger G. Ulrich
  • Patent number: 8686184
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: April 1, 2014
    Assignee: Theravance, Inc.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Publication number: 20140088088
    Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, Formulas (I), (II), (III) and (IV) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent proliferative disorders and their use to manufacture a medicine to treat or prevent proliferative disorders, particularly cancer such as leukemia. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent proliferative disorders. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of proliferative disorders and pathologic conditions such as, but not limited to, cancer such as leukemia.
    Type: Application
    Filed: September 8, 2011
    Publication date: March 27, 2014
    Applicant: Katholieke Universiteit Leuven, K.U. Leuven R&D
    Inventors: Jean Herman, Thierry Louat
  • Patent number: 8653260
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
  • Publication number: 20140045865
    Abstract: The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). 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 TRPA1.
    Type: Application
    Filed: October 21, 2013
    Publication date: February 13, 2014
    Applicant: Glenmark Pharmaceuticals, S.A.
    Inventors: Sukeerthi Kumar, Abraham Thomas, Sachin Sundarlal Chaudhari, Bipin Parsottam Kansagra, Venkata Ramana Yemireddy, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay, Girish Gudi
  • Patent number: 8648068
    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: Grant
    Filed: February 25, 2011
    Date of Patent: February 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: 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
  • Publication number: 20140038959
    Abstract: The present invention relates to a method of treating tumors wherein PAK1 is over-expressed or amplified by co-administering a PAK1 inhibitor and a second anti-hyper-proliferative agent
    Type: Application
    Filed: May 9, 2013
    Publication date: February 6, 2014
    Applicant: Genentech, Inc.
    Inventor: Genentech, Inc.
  • Publication number: 20140037647
    Abstract: Disclosed herein are new prognostic molecular markers for prostate cancer. More specifically, the invention has identified that overexpression or amplification of at least one of AURKA or MYCN define a distinct subgroup of prostate cancer that is predisposed to the development of lethal NEPC, who will benefit from early intervention.
    Type: Application
    Filed: March 28, 2012
    Publication date: February 6, 2014
    Applicant: CORNELL UNIVERSITY
    Inventors: Mark A. Rubin, Himisha Beltran
  • Patent number: 8642594
    Abstract: Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk? and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO2—, —C(?O)O—, —C(?O)NRA—, —C(?S)NRA—, —SO2NRA—, —NRAC(?O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.
    Type: Grant
    Filed: January 21, 2010
    Date of Patent: February 4, 2014
    Assignees: Vernalis (R&D) Limited, Cancer Research Technology Ltd., The Institute of Cancer Research
    Inventors: Brian William Dymock, Martin James Drysdale, Christofe Fromont, Allan Jordan, Xavier Barril-Alonso
  • Patent number: 8637527
    Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: January 28, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
  • Publication number: 20140024661
    Abstract: A group of fused two ring pyrimidine compounds having a heterocycles substituent at the 2 position and a substituted amine at the 4 position as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine and other ring are disclosed. In addition a group of quinazoline compounds having similar substituents at the 2 and 4 positions as well as at other positions are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity.
    Type: Application
    Filed: July 19, 2013
    Publication date: January 23, 2014
    Applicant: Cleave Biosciences, Inc.
    Inventors: Han-Jie Zhou, Francesco Parlati
  • Publication number: 20140024662
    Abstract: The present invention features compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods for treating diseases and conditions associate with cellular necrosis. Screening assays for identifying compounds useful for treating these conditions are also described.
    Type: Application
    Filed: September 25, 2013
    Publication date: January 23, 2014
    Applicants: Shanghai Institute of Organic Chemistry, President and Fellows of Harvard College
    Inventors: Junying YUAN, Chengye Yuan, Alexei Degterev
  • Patent number: 8633201
    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: Grant
    Filed: April 10, 2007
    Date of Patent: January 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Babette Aicher, Thomas Stephen Coulter, Stefan Jaekel, Arndt-René Kelter, Stephen Murfin, Tanja Reuter, Steven Taylor
  • Publication number: 20140018361
    Abstract: The present invention provides furano- and pyrrolo-pyrimidine and pyridine compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: July 11, 2013
    Publication date: January 16, 2014
    Inventors: Geraldine C. Harriman, Donna L. Romero, Craig E. Masse, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
  • Publication number: 20140011818
    Abstract: The present invention discloses novel enantiomeric antifungal compounds of Formula (1a) and Formula (1b) containing thieno-[2,3-d]Jpyrimidin-4(3H)-one moiety and pharmaceutically acceptable salts thereof, method of preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these compounds.
    Type: Application
    Filed: May 31, 2011
    Publication date: January 9, 2014
    Applicants: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH, FDC LIMITED
    Inventors: Hanumant Bapurao Borate, Suleman Riyajsaheb Maujan, Sangmeshwer Prabhkara Sawargave, Subhash Prataprao Chavan, Mohan Anand Chandavarkar, Ramkrishnan Ramachandran Iyer, Vikas Vasanat Nawathye, Gajanan Jalindar Chavan, Amit Chandrakant Tawte, Deepali Damodar Rao
  • Patent number: 8618116
    Abstract: The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives and pharmaceutically acceptable salts and methods of use thereof for the treatment of pulmonary arterial hypertension, pulmonary hypertension associated with chronic obstructive pulmonary disease (COPD), asthma, cystic fibrosis, hypertension, ischemic stroke, angina pectoris, congestive heart failure, arrhythmia, arterial fibrillation, Alzheimer's disease, cognition impairment, memory decline, and schizophrenia, and depression.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: December 31, 2013
    Inventor: Daljit Singh Dhanoa
  • Patent number: 8618115
    Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: December 31, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: William N. Washburn, Mark C. Manfredi, Jeffrey A. Robl, Andres S. Hernandez
  • Publication number: 20130345192
    Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.
    Type: Application
    Filed: October 28, 2011
    Publication date: December 26, 2013
    Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.
    Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
  • Publication number: 20130345219
    Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: August 28, 2013
    Publication date: December 26, 2013
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Chi-Wan Lee, Teresa Prezewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
  • Publication number: 20130338095
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: December 19, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
  • Patent number: 8609840
    Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, traumatic nerve injury, and depression. This invention is useful for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: December 17, 2013
    Assignee: Neuronascent, Inc.
    Inventor: Judith Kelleher-Andersson
  • Patent number: 8609670
    Abstract: The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: December 17, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pascale A. J. Pouzet, Peter Nickolaus, Ulrike Werthmann, Rogelio Perez Frutos, Bing-Shiou Yang, Soojin Kim, Jason Alan Mulder, Nitinchandra D. Patel, Chris Hugh Sananayake, Thomas Gabriel Tampone, Xudong Wei
  • Patent number: 8609650
    Abstract: 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: Grant
    Filed: July 26, 2011
    Date of Patent: December 17, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak