Nitrogen Bonded Directly To The 3-position Of The Oxazole Ring Patents (Class 548/246)
  • Publication number: 20150110809
    Abstract: Embodiments of the invention are directed to compounds that inhibit an activity of EP AC proteins and methods of using the same. The inventors have developed a sensitive and robust high throughput screening (HTS) assay for the purpose of identifying EPAC specific inhibitors (Tsalkova et al. (2012) PLOS ONE 7 (1):e30441).
    Type: Application
    Filed: February 8, 2013
    Publication date: April 23, 2015
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Xiaodong Cheng, Jia Zhou, Tamara Tsalkova, Fang Mei, Haijun Chen
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Patent number: 8969587
    Abstract: Compounds, compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: March 3, 2015
    Assignee: Ambit Biosciences Corporation
    Inventors: Sunny Abraham, Shripad S. Bhagwat, Brian T. Campbell, Qi Chao, Raffaella Faraoni, Mark W. Holladay, Andiliy G. Lai, Martin W. Rowbottom, Eduardo Setti, Kelly G. Sprankle
  • Patent number: 8957063
    Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: February 17, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Monika Ermann, Innocent Mushi
  • Patent number: 8927551
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: January 6, 2015
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Publication number: 20140357655
    Abstract: Spiroindoline derivatives, process for their preparation and pharmaceutical compositions thereof, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially sex-hormone-related diseases in both men and women, in particularly those selected from the group of endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasia such as cancers of the prostate, breast and ovary, gonadotrope pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hypertrophy, contraception and infertility (e.g., assisted reproductive therapy such as in vitro fertilization). The present application relates in particular to spiroindoline derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists.
    Type: Application
    Filed: January 15, 2013
    Publication date: December 4, 2014
    Inventors: Olaf Panknin, Stefan Bäurle, Sven Ring, Wolfgang Schwede, Wilhelm Bone, Katrin Nowak-Reppel, Eckhard Bender, Reinhard Nubbemeyer, Mark Jean Gnoth
  • Publication number: 20140315933
    Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or pharmaceutically acceptable salts thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes and to methods of treatment; wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.
    Type: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Applicant: PFIZER LIMITED
    Inventors: Robert McKenzie Owen, Robert Ian Storer
  • Publication number: 20140296245
    Abstract: This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: October 2, 2014
    Inventors: Shaoyi Sun, Alla Yurevna Zenova, Mikhail Chafeev, Qi Jia, Zaihui Zhang, Renata Marcella Oballa
  • Patent number: 8829034
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: September 9, 2014
    Assignee: Boehringer Ingerlheim International GmbH
    Inventors: Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Parke, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
  • Patent number: 8822462
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: September 2, 2014
    Assignee: Emory University
    Inventors: Stephen F. Traynelis, Dennis C. Liotta, Rose M. Santangelo, Ethel C. Garnier
  • Publication number: 20140206676
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: January 12, 2013
    Publication date: July 24, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Patent number: 8772288
    Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: July 8, 2014
    Assignee: Almirall, S.A.
    Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
  • Publication number: 20140142149
    Abstract: Methods of administering and pharmaceutical compositions of a biphenyl sulfonamide compound which is a dual angiotensin and endothelin receptor antagonist are disclosed for treating diseases.
    Type: Application
    Filed: December 19, 2012
    Publication date: May 22, 2014
    Applicant: Ligand Pharmaceuticals Inc.
    Inventors: Jinkun Zhang, Zofia E. Dziewanowska, Rene Belder, Ian Henderson, Joseph B. Bogardus, Zhaoying Zhang
  • Patent number: 8716492
    Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: May 6, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
  • Patent number: 8709700
    Abstract: The present invention relates to a fluorine-free photoacid generator (PAG) and a photoresist composition containing the same. The PAG is characterized by the presence of an onium cationic component and a fluorine-free fused ring heteroaromatic sulfonate anionic component containing one or more electron withdrawing substituents. The onium cationic component of the PAG is preferably a sulfonium or an iodonium cation. The photoresist composition further contains an acid sensitive imaging polymer. The photoresist composition is especially useful for forming material patterns on a semiconductor substrate using 193 nm (ArF) lithography.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: April 29, 2014
    Assignee: International Business Machines Corporation
    Inventors: Sen Liu, Pushkara R. Varanasi
  • Publication number: 20140066466
    Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.
    Type: Application
    Filed: March 12, 2012
    Publication date: March 6, 2014
    Applicant: President and Fellows of Harvard College
    Inventor: Junying Yuan
  • Patent number: 8653127
    Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: February 18, 2014
    Assignee: Cara Therapeutics, Inc.
    Inventor: Robert Zhiyong Luo
  • Patent number: 8629157
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain (I).
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: January 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khor, Doris Riether, Lifen Wu, Renee M. Zindell
  • Publication number: 20130345120
    Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
    Type: Application
    Filed: March 9, 2012
    Publication date: December 26, 2013
    Applicant: Glaxosmithkline LLC
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
  • Publication number: 20130324536
    Abstract: The invention provides pyrazolyl guanidine compounds that inhibit F1Fo-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: December 5, 2013
    Applicant: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Clarke B. Taylor, Chad A. Van Huis
  • Publication number: 20130324557
    Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
    Type: Application
    Filed: November 4, 2011
    Publication date: December 5, 2013
    Applicant: SENOMYX, INC.
    Inventors: Chad Priest, Alain Noncovich, Andrew Patron, Jane Ung
  • Patent number: 8592470
    Abstract: A compound represented by formula (1-1) or (1-2), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of sitaxentan and has an improved CYP inhibitory effect: wherein R1 is a halogen atom, etc., R2 is a methyl group, etc., R3 is a C1-6 alkyl group, etc., and M is a group represented by: etc.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: November 26, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Keigo Tanaka, Tomoki Nishioka
  • Publication number: 20130296559
    Abstract: A substituted alkenylbenzene compound of formula (4): wherein X1 is selected from the group consisting of a halogen atom, —SF5, C1-C6haloalkyl, hydroxy C1-C6haloalkyl, C1-C6alkoxy C1-C6haloalkyl, C3-C8halocycloalkyl, C1-C6haloalkoxy, C1-C3haloalkoxy C1-C3haloalkoxy, C1-C6haloalkylthio, C1-C6haloalkylsulfinyl and C1-C6haloalkylsulfonyl; X3 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy and C1-C6alkylthio; X4 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, C1-C4alkyl, C1-C4alkoxy and C1-C4haloalkoxy; R3 is —C(R3a)(R3b)R3c, where R3a and R3b independently of each other are a halogen atom, or R3a and R3b together form 3- to 6-membered ring together with the carbon atom bonding them by forming a C2-C5haloalkylene chain, and R3c is selected from the group consisting of a hydrogen atom, halogen atom.
    Type: Application
    Filed: March 25, 2013
    Publication date: November 7, 2013
    Inventors: Takeshi MITA, Takamase Kikuchi, Takashi Mizukoshi, Manabu Yaosaka, Mitsuaki Komoda
  • Publication number: 20130237531
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: April 19, 2013
    Publication date: September 12, 2013
    Inventors: Guoxian Wu, Jiazhong Zhang, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, James Tsai
  • Publication number: 20130210773
    Abstract: In one aspect, the invention relates to indole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 21, 2011
    Publication date: August 15, 2013
    Inventor: Craig W. Lindsley
  • Patent number: 8507541
    Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: August 13, 2013
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Brian M. Glass, Richard B. Sparks, Eddy Wai Tsun Yue
  • Publication number: 20130197045
    Abstract: A compound represented by formula (1-1) or (1-2), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of sitaxentan and has an improved CYP inhibitory effect: wherein R1 is a halogen atom, etc., R2 is a methyl group, etc., R3 is a C1-6 alkyl group, etc., and M is a group represented by: etc.
    Type: Application
    Filed: January 29, 2013
    Publication date: August 1, 2013
    Applicant: Eisai R&D Management Co., Ltd.
    Inventor: Eisai R&D Management Co., Ltd.
  • Publication number: 20130184315
    Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: July 18, 2011
    Publication date: July 18, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbH
    Inventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
  • Publication number: 20130165412
    Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.
    Type: Application
    Filed: September 14, 2012
    Publication date: June 27, 2013
    Inventors: Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
  • Publication number: 20130165452
    Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.
    Type: Application
    Filed: February 22, 2013
    Publication date: June 27, 2013
    Applicant: PFIZER INC.
    Inventor: Pfizer Inc.
  • Patent number: 8466182
    Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: June 18, 2013
    Assignees: The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University of Maryland, Baltimore
    Inventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
  • Publication number: 20130039856
    Abstract: The present invention concerns medicaments for slowing ageing. The medicaments can include an inhibitor of microbial folate biosynthesis as well as agents capable of reducing folate uptake by an animal. Examples of such medicaments include inhibitors that reduce the activity of an enzyme in the folate biosynthesis pathway, such as sulfonamides including sulfamethoxazole. The invention also concerns a food supplement, additive, functional food, or nutraceutial comprising the inhibitor or agent or composition as discussed above, as well as methods for screening for an agent for use as a medicament for slowing ageing comprising determining whether a test agent inhibits microbial folate biosynthesis, or whether the test agent reduces folate uptake by a non-human animal.
    Type: Application
    Filed: February 25, 2011
    Publication date: February 14, 2013
    Applicant: University of Durham
    Inventor: David Weinkove
  • Publication number: 20120322800
    Abstract: Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).
    Type: Application
    Filed: October 14, 2010
    Publication date: December 20, 2012
    Inventor: Julian Blagg
  • Publication number: 20120309673
    Abstract: Compounds of Formula II wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4? is C1-C6alkyl, C1-C6haloalkyl or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
    Type: Application
    Filed: December 10, 2010
    Publication date: December 6, 2012
    Applicant: Medivir UK Ltd
    Inventors: Susana Ayesa, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jönsson, Pia Kahnberg, Björn Klasson, Peter Lind, Stina Lundgren, Lourdes Odén, Kevin Parkes, Daniel Wiktelius
  • Patent number: 8299103
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: October 30, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether
  • Publication number: 20120225880
    Abstract: A compound of formula (I): wherein A, B, D, X, Y, R1, R2, R3, m, p, and q are defined herein. Also disclosed is a method for inhibiting FMS-like tyrosine kinase 3, aurora kinase, or vascular endothelial growth factor receptor.
    Type: Application
    Filed: March 1, 2012
    Publication date: September 6, 2012
    Applicant: National Health Research Institutes
    Inventors: Weir-Torn Jiaang, Tsu-An Hsu, Wen-Hsing Lin, Yu-Sheng Chao
  • Patent number: 8236822
    Abstract: Cannabinoid receptor ligands of formula (I) wherein Ring A and R1 are as defined in the specification. Compositions including such compounds, and methods of treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: August 7, 2012
    Assignee: Abbott Laboratories
    Inventors: Xueqing Wang, Michael J. Dart, Bo Liu
  • Patent number: 8211926
    Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Grant
    Filed: June 16, 2010
    Date of Patent: July 3, 2012
    Assignee: Cara Therapeutics, Inc.
    Inventor: Robert Zhiyong Luo
  • Publication number: 20120165339
    Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.
    Type: Application
    Filed: December 20, 2011
    Publication date: June 28, 2012
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
  • Publication number: 20120149706
    Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: February 21, 2012
    Publication date: June 14, 2012
    Inventors: Jacques DUMAS, Uday KHIRE, Timothy B. Lowinger, Holger PAULSEN, Bernd RIEDL, Willian J. SCOTT, Roger A. SMITH, Jill WOOD, Holia HATOUM-MOKDAD, Wendy LEE, Aniko REDMAN, Jeffrey JOHNSON, Robert SIBLEY
  • Publication number: 20120142677
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: December 15, 2009
    Publication date: June 7, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khok, Doris Riether, Lifen Wu, Renee M. Zindell
  • Patent number: 8178568
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: May 15, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John Regan, Doris Riether
  • Publication number: 20120115841
    Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
    Type: Application
    Filed: May 17, 2010
    Publication date: May 10, 2012
    Applicant: ACTELION PHARMACEUTICALS LTD.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Patent number: 8158825
    Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: April 17, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
  • Publication number: 20120028977
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
    Type: Application
    Filed: January 28, 2010
    Publication date: February 2, 2012
    Applicant: EMORY UNIVERSITY
    Inventors: Stephen F. Traynelis, Dennis C. Liotta, Rose M. Santangelo, Ethel C. Garnier
  • Publication number: 20120010186
    Abstract: Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.
    Type: Application
    Filed: March 18, 2010
    Publication date: January 12, 2012
    Applicant: MERCK FROSST CANADA LTD.
    Inventors: Nicolas Lachance, Serge Leger, Renata M. Oballa, David Powell, Geoffrey K. Tranmer, Evelyn Martins, Yves Gareau
  • Publication number: 20110269804
    Abstract: A compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: July 24, 2009
    Publication date: November 3, 2011
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Jérôme Yves Cassayre, Peter Renold, Thomas Pitterna, Vladimir Bobosik, Myriem El Qacemi, Anne Jacqueline Dalencon, Werner Zambach, Christopher Richard Ayles Godfrey, Pierre Joseph Marcel Jung, Jagadish Pabba
  • Publication number: 20110251216
    Abstract: 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: Application
    Filed: February 10, 2011
    Publication date: October 13, 2011
    Applicant: The Regents of The University of Michigan
    Inventors: Arul M. Chinnaiyan, Sooryanaryana Lnu, Qi Cao
  • Publication number: 20110230445
    Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.
    Type: Application
    Filed: May 26, 2011
    Publication date: September 22, 2011
    Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
  • Publication number: 20110201609
    Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.
    Type: Application
    Filed: June 30, 2009
    Publication date: August 18, 2011
    Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South Florida
    Inventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida