1,4-diazine As One Of The Cyclos Patents (Class 514/249)
At least three rings in the polycyclo ring system (Class 514/250)
  • Substituted-quinoxaline-type bridged-piperidine compounds as ORL-1 modulators
    Patent number: 9145408
    Abstract: Compounds of Formula (I): where R1, R2, R5, a, and b are disclosed herein, and pharmaceutically acceptable derivatives thereof (a “Substituted-Quinoxaline-Type Bridged-Piperidine Compound”), compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound.
    Type: Grant
    Filed: June 11, 2013
    Date of Patent: September 29, 2015
    Assignees: Purdue Pharma L.P., Shionogi & Co., Ltd.
    Inventors: Naoki Tsuno, John W. F. Whitehead, Jiangchao Yao
  • Substituted quinoxalines as FGFR kinase inhibitors
    Patent number: 9145394
    Abstract: The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: November 29, 2011
    Date of Patent: September 29, 2015
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Gordon Saxty, Christopher William Murray, Valerio Berdini, Gilbert Ebai Besong, Christopher Charles Frederick Hamlett, Steven John Woodhead, Yannick Aime Eddy Ligny, Patrick René Angibaud
  • Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones as protein kinase inhibitors
    Patent number: 9145418
    Abstract: The present invention relates to substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives, of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: September 29, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Francesco Casuscelli, Elena Casale, Marisa Montemartini, Claudia Piutti
  • Substituted quinoxalines as sodium channel modulators
    Patent number: 9139529
    Abstract: The invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.
    Type: Grant
    Filed: January 29, 2014
    Date of Patent: September 22, 2015
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
  • Radiolabeled PDE10A ligands
    Patent number: 9138494
    Abstract: Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by PDE10A ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as PDE10A positron emission tomography ligands. Also disclosed are pharmaceutical compositions comprising compound of formula (I), methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: September 22, 2015
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: Lawrence A. Black, Berthold Behl, Jill Wetter
  • Substituted pyrido[2,3-B]pyrazines as IP receptor agonists
    Patent number: 9132127
    Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.
    Type: Grant
    Filed: April 30, 2014
    Date of Patent: September 15, 2015
    Assignee: Novartis AG
    Inventors: Steven John Charlton, Catherine LeBlanc, Stephen Carl McKeown
  • Substituted benzopiperazines as CETP inhibitors
    Patent number: 9126976
    Abstract: Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: August 13, 2012
    Date of Patent: September 8, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Rajan Anand, Vincent J. Colandrea, Maud Reiter, Petr Vachal, Aaron Zwicker, Jonathan E. Wilson, Fengqi Zhang, Kake Zhao
  • Modulators of toll-like receptors
    Patent number: 9127006
    Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
    Type: Grant
    Filed: July 1, 2014
    Date of Patent: September 8, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Manoj C. Desai, Randall L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan McFadden, Paul A. Roethle, Hong Yang
  • Cyclic Glycyl-2-Allyl Proline improves cognitive performance in impaired animals
    Patent number: 9119851
    Abstract: Embodiments of this invention provide methods for therapeutic use of cyclic G-2-Allyl Proline to treat cognitive disorders as well as manufacture of medicaments including tablets, capsules, injectable solutions that are useful for treatment of such conditions.
    Type: Grant
    Filed: June 25, 2014
    Date of Patent: September 1, 2015
    Assignee: NEUREN PHARMACEUTICALS, LTD.
    Inventors: Michael John Bickerdike, Jian Guan
  • Substituted pyrrolo[1,2-A]pyrazin-1-ones and pyrazolo[1,5-A]pyrazin-4-ones as inhibitors of tankyrase and poly(ADP-ribose)polymerase activity
    Patent number: 9120805
    Abstract: Compounds of the formula I in which R1, X and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Grant
    Filed: March 19, 2013
    Date of Patent: September 1, 2015
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Hans-Peter Buchstaller, Gerard Moinet, Ansgar Wegener
  • Substituted pyrido[2,3-B]pyrazines as IP receptor agonists
    Patent number: 9115129
    Abstract: The present invention provides substituted pyrido[2,3-b]pyrazines which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such substituted pyride[2,3-b]pyrazines are also encompassed.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: August 25, 2015
    Assignee: Novartis AG
    Inventors: Steven John Charlton, Catherine Leblanc, Stephen Carl McKeown
  • Method of improving diastolic dysfunction
    Patent number: 9114133
    Abstract: A method of treating, preventing, reversing, or ameliorating diastolic dysfunction includes reducing S-glutathionylated myosin binding protein-C (MyBP-C) level by administering to a host in need thereof a therapeutically effective amount of tetrahydrobiopterin (BH4).
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: August 25, 2015
    Assignees: U.S. DEPT. OF VETERANS AFFAIRS, THE BOARD OF TRUSTEES OF THE UNIV. OF ILLINOIS
    Inventor: Samuel C. Dudley, Jr.
  • Coated tablets of eszopiclone
    Patent number: 9114086
    Abstract: Coated tablets of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The tablets minimize the perceived bitterness of the medicament. A method for analyzing instantaneous dissolution of sub-microgram quantities of core material is also disclosed.
    Type: Grant
    Filed: April 2, 2014
    Date of Patent: August 25, 2015
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Richard Hsia, Cai Gu Huang, Konstantinos E. Saranteas, Tushar K. Misra, Philip J. Bonasia, Jr.
  • Salts of DPP-IV inhibitor
    Patent number: 9108972
    Abstract: The present invention discloses new salts of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine i.e. gentisate, adipate and trifluoro acetic acid salts. The invention also describes the new. crystalline and amorphous forms of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine gentisate. The present invention also discloses novel crystalline salt form of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine hydrochloride and novel crystalline and amorphous salt forms of besylate and process for their preparation and isolation.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: August 18, 2015
    Assignee: Cadila Healthcare Limited
    Inventors: Bipin Pandey, Mayank Ghanshyambhai Dave, Himanshu M. Kothari, Bhavin Shriprasad Shukla
  • Aryl substituted carboxamide derivatives as calcium or sodium channel blockers
    Patent number: 9101616
    Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as NaV1.3 and NaV1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.
    Type: Grant
    Filed: May 31, 2010
    Date of Patent: August 11, 2015
    Assignee: RaQualia Pharma Inc.
    Inventors: Tadashi Inoue, Shuzo Watanabe, Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Kaoru Shimada
  • Selective HDAC3 inhibitors
    Patent number: 9096549
    Abstract: Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: August 4, 2015
    Assignee: ACETYLON PHARMACEUTICALS, INC.
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Targeting TGF-? as a therapy for Alzheimer's disease
    Patent number: 9095126
    Abstract: Described herein are compositions and methods for enhancing peripheral macrophage A? phagocytosis activity. The methods include inhibiting the TGF-? signaling pathway and activating the BMP signaling pathway in peripheral macrophages to promote central nervous system infiltration and enhance macrophage A? phagocytosis activity. Inhibition of TGF-? signaling and activation of BMP signaling in peripheral macrophages represents an advantageous anti-amyloid therapeutic approach for Alzheimer's disease.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: August 4, 2015
    Assignee: Yale University
    Inventors: Richard A. Flavell, Terrence C. Town
  • Substituted quinoxalines compounds
    Patent number: 9090572
    Abstract: A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents —O— or —CH2—; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
    Type: Grant
    Filed: September 12, 2011
    Date of Patent: July 28, 2015
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Nobuaki Ito, Hirofumi Sasaki, Kuninori Tai, Tomoichi Shinohara
  • Methods and compositions to reduce oxidative stress
    Patent number: 9089573
    Abstract: The invention relates to therapeutic applications for compositions that reduce the level of oxidative stress on cells in vivo or in vitro. The invention describes methods for improving the therapeutic properties of stem cells. The invention also provides combination therapies that are useful to balance the oxidative microenvironment of cells in vivo or in vitro.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: July 28, 2015
    Assignee: University of Massachusetts
    Inventor: Louis M. Messina
  • Cyclic urea- or lactam-substituted quinoxaline-type piperidines as ORL-1 modulators
    Patent number: 9085561
    Abstract: The disclosure relates to Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein R1, R2, Qa, Y1, Z, A, B, Qx, E, G, J, M, U, W, and a are as defined herein, compositions comprising an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: July 21, 2015
    Assignees: Purdue Pharma L.P., Shionogi & Co., Ltd.
    Inventors: Naoki Tsuno, Tatsuhiko Ueno, Xiaoming Zhou
  • Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments
    Patent number: 9079906
    Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: July 14, 2015
    Assignee: Sanofi
    Inventors: Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Karl Schoenafinger, Henning Steinhagen, Bodo Scheiper
  • Substituted quinoxaline carboxylic acid compounds for the inhibition of PASK
    Patent number: 9073902
    Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: January 5, 2012
    Date of Patent: July 7, 2015
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero
  • Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl) -phenylamino]-pyrimidin-4-yl}-1-methyl-urea and salts thereof
    Patent number: 9067896
    Abstract: The present technology provides novel anhydrous and hydrated crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea, amorphous and anhydrous crystalline polymorphs of its monophosphoric acid salt, and the hydrochloride salt, including its dihydrate. The present technology further provides methods for preparing the various forms, compositions containing them, and methods of treatment employing them.
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: June 30, 2015
    Assignee: Novartis AG
    Inventors: Joerg Berghausen, Prasad K Kapa, Joseph McKenna, Joel Slade, Raeann Wu, Zhengming Du, Frank Stowasswer
  • Pyrido [2, 3-B] pyrazine compounds and their therapeutical uses such as for inhibiting ATP consuming proteins and treating diseases associated therewith
    Patent number: 9051318
    Abstract: The present invention relates to novel pyrido[2,3-b]pyrazine compounds of formula (I): and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.
    Type: Grant
    Filed: February 13, 2012
    Date of Patent: June 9, 2015
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
  • SUBSTITUTED PYRIDINE SPLEEN TYROSINE KINASE (SYK) INHIBITORS
    Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • BICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS
    Publication number: 20150148342
    Abstract: The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Application
    Filed: November 26, 2014
    Publication date: May 28, 2015
    Applicant: INCYTE CORPORATION
    Inventors: Eddy W. Yue, Andrew P. Combs, Brent Douty
  • CARBAMATE COMPOUNDS AND OF MAKING AND USING SAME
    Publication number: 20150148330
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 28, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • QUINOLINE DERIVATIVES AS BROMODOMAIN INHIBITORS
    Publication number: 20150148344
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
  • NON-SYSTEMIC TGR5 AGONISTS
    Publication number: 20150148311
    Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.
    Type: Application
    Filed: June 20, 2014
    Publication date: May 28, 2015
    Inventors: Jason G. Lewis, Nicholas Reich, Tao Chen, Jeffrey W. Jacobs, Dominique Charmot, Marc Navre, Patricia Finn, Christopher Carreras, Andrew Spencer
  • TRIAZOLO COMPOUNDS AS PDE10 INHIBITORS
    Publication number: 20150148332
    Abstract: The present invention provides compounds of formula (Ia) and (Ib) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: November 25, 2014
    Publication date: May 28, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Bernd Kuhn, Christian Lerner, Markus Rudolph, Herve Schaffhauser
  • DRUG FOR PREVENTING/TREATING OCULAR DISEASE
    Publication number: 20150148350
    Abstract: The present invention relates to a medicament for preventing or treating an ocular disease comprising cyclo-trans-4-L-hydroxyprolyl-L-serine as an active ingredient, a medicament for preventing or treating dry eye comprising the compound as an active ingredient, and, in particular, a medicament for preventing or treating dry eye having an action of enhancing mucin secretion and an action of enhancing repair of ocular tissue damage caused by dry eye.
    Type: Application
    Filed: April 5, 2013
    Publication date: May 28, 2015
    Inventors: Taiichi Kaku, Yoshiharu Kadota, Shumpei Yamaguchi, Takahiro Nakamura, Masashi Akitsu
  • [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
    Patent number: 9040534
    Abstract: The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 26, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall
  • Alpha adrenergic receptor modulators
    Patent number: 9040532
    Abstract: Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: May 26, 2015
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Liming Wang, Wenkui K. Fang, Evelyn G. Corpuz, Santosh C. Sinha, Daniel W. Gil, Mohammad I. Dibas, John E. Donello
  • Oxime-substituted-quinoxaline-type piperidine compounds as ORL-1 modulators
    Patent number: 9040533
    Abstract: The present disclosure relates to Oxime-Substituted Quinoxaline-Type Piperidine Compounds, such as those of Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R20, R21, Q, Y1, Z, A, B, and a are as defined herein; compositions comprising an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: May 26, 2015
    Assignees: Purdue Pharma L.P., Shionogi & Co., Ltd.
    Inventors: Jeffrey Michael Marra, Naoki Tsuno, Tatsuhiko Ueno, Xiaoming Zhou
  • PESTICIDALLY ACTIVE PYRIDYL- AND PYRIMIDYL- SUBSTITUTED THIAZOLE DERIVATIVES
    Publication number: 20150141423
    Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 21, 2015
    Applicant: Syngenta Participations AG
    Inventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
  • QUINAZOLINEDIONE DERIVATIVE
    Publication number: 20150141400
    Abstract: The present invention relates to quinazolinedione derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 24, 2013
    Publication date: May 21, 2015
    Inventors: Takeshi Murata, Hatsuo Kawada, Satoshi Niizuma, Sousuke Hara, Kihito Hada, Hideaki Shimada, Hiroshi Tanaka, Toshiyuki Mio
  • BLOOD BORNE miRNA SIGNATURE FOR THE ACCURATE DIAGNOSIS OF PANCREATIC DUCTAL ADENOCARCINOMA
    Publication number: 20150141342
    Abstract: The differential expression of select miRNA in plasma and bile among patients with PDAC, chronic pancreatitis (CP), and controls were measured. Patients (n=215) with treatment-naïve PDAC (n=77), CP with bile or pancreatic duct pathology (n=67), and controls (n=71) that had been prospectively enrolled in a Pancreatobiliary Disease Biorepository at the time of endoscopic retrograde cholangiopancreatography (ERCP) or endoscopic ultrasound (EUS) were identified. Controls were patients with choledocholithiasis but normal pancreata. The sample was separated into training (n=95) and validation (n=120) cohorts to establish and then test the performance of PDAC Signature Panels in diagnosing PDAC. The training cohort (n=95) included age-matched patients with CP and controls. Panels were derived from the differential expression of 10-candidate miRNA in plasma or bile.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 21, 2015
    Inventors: Murray Korc, A. Jesse Gore, Gregory A. Cote, Stuart Sherman
  • N-Aryl Unsaturated Fused Ring Tertiary Amine Compounds, Preparation Method and Anti-Tumor Applications Thereof
    Publication number: 20150141407
    Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 21, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
  • HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
    Publication number: 20150141422
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • SUBSTITUTED 3,4-DIHYDRO-2H-PYRIDO[1,2-A]PYRAZINE-1,6-DIONE DERIVATIVES USEFUL FOR THE TREATMENT OF (INTER ALIA) ALZHEIMER'S DISEASE
    Publication number: 20150141411
    Abstract: The present invention is concerned with novel substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, R5, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 21, 2015
    Inventors: Frederik Jan Rita Rombouts, Andres Avelino Trabanco-Suarez, Henricus Jacobus Maria Gijsen, Gregor James Macdonald, Francois Paul Bischoff, Sergio-Alvar Alonso-de-Diego, Adriana Ingrid Velter, Yves Emiel Maria Van Roosbroeck
  • METHOD FOR MODULATING CANONICAL WNT PATHWAY USING FOLATE AND INOSITOL
    Publication number: 20150141430
    Abstract: The canonical Wnt signaling pathway is implicated in wound healing. Administration of a composition having myo-inositol and folic acid upregulates fibronectin and provides the greatest protection in an additive/synergistic manner against adverse Wnt/?-catenin-mediated effects on cell processes relating to cell differentiation, proliferation, and migration that relate to wound healing.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 21, 2015
    Applicant: University of South Florida
    Inventor: Kersti K. Linask
  • NOVEL SUBSTITUTED PYRAZOLO-PIPERAZINES AS CASEIN KINASE 1 D/E INHIBITORS
    Publication number: 20150133428
    Abstract: The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventors: Upender Velaparthi, Chetan Padmakar Darne, Peiying Liu, Mark D. Wittman, Bradley C. Pearce, Erika M. V. Araujo, Bireshwar Dasgupta, Jalathi Surendran Nair, Sakthi Kumaran Janakiraman, Chandrasekhar Reddy Rachamreddy, Mettu Mallikarjuna Rao, Arul Mozhi Selvan Subbiah Karuppiah, Bandreddy Subba Reddy, Pulicharla Nagalakshmi, Rajesh Onkardas Bora, Shilpa Holehatti Maheshwarappa, Selvakumar Kumaravel, Dibakar Mullick, Ramesh Sistla
  • COMPOSITIONS AND METHODS FOR IDENTIFYING AND DIAGNOSING SALT SENSITIVITY OF BLOOD PRESSURE
    Publication number: 20150133414
    Abstract: It was determined whether SNPs in SLC4A5 are associated with salt sensitivity of blood pressure (BP). Subjects consumed an isocaloric constant diet with a randomized order of 7 days low Na+ (10 mmol/d) and 7 days high Na+ (300 mmol/d) intake. Salt sensitivity was defined as a ?7 mm Hg increase in mean arterial pressure (MAP). 35 polymorphisms in 17 candidate genes were assayed. Association analyses with salt sensitivity revealed three variants that associated with salt sensitivity, two in SLC4A5 (rs7571842, rs10177833; P<0.001), and one in GRK4 (rs1801058; P=0.020). Paradoxical changes in blood pressure in response to changes in salt intake were also found associated with a SNP for DRD2 (rs6276). In conclusion, SLC4A5 variants are strongly associated with salt sensitivity of BP in Caucasian and a DRD2 SNP is a marker for paradoxical response to salt intake.
    Type: Application
    Filed: April 22, 2013
    Publication date: May 14, 2015
    Applicant: University of Virginia Patent Foundation
    Inventors: Robin A. Felder, Robert M. Carey, John E. Jones, Pedro A. Jose, Scott M. Williams
  • METHOD OF REDUCING FASTING INSULIN LEVELS IN MTHFR GENE DEFICIENT SUBJECTS WITH NORMAL TO SLIGHTLY ELEVATED HEMOGLOBIN A1C
    Publication number: 20150133397
    Abstract: A method of treatment for reducing elevated fasting insulin levels of subjects with a MTHFR gene deficiency is provided. The method includes first determining whether a subject has an MTHFR gene deficiency. Once a subject has been found to have the MTHFR gene deficiency, the fasting insulin levels of the subject are determined. If the subject has a high fasting insulin level, the subject is administered an active folate.
    Type: Application
    Filed: August 8, 2014
    Publication date: May 14, 2015
    Inventors: Jeffrey Lynn Barringer, Stephen Albert Smith, Jerry Golden
  • NANOSTRUCTURED MUCOADHESIVE MICROPARTICLES
    Publication number: 20150133454
    Abstract: Provided is a nanostructured mucoadhesive microparticle including a biocompatible polymer, the microparticle having a surface with a nanostructure formed thereon. The present nanostructured mucoadhesive microparticle having an increased retention time on the mucous as well as with a minimized irritation to the surface can be advantageously used as a drug delivery vehicle. Thus the increased bioavailability of a therapeutic agent administered by the present microparticle leads to an increased therapeutic efficacy, reduced dosage and reduced number of administration as well as significant cost savings and improved patient convenience resulted therefrom.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 14, 2015
    Applicant: SNU R&DB FOUNDATION
    Inventors: Young Bin Choy, Chun Gwon Park
  • THIENOPYRIMIDINES
    Publication number: 20150133425
    Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
  • FOLIC ACID – RAMIPRIL COMBINATION: CELL PROTECTIVE, NEUROPROTECTIVE AND RETINOPROTECTIVE OPHTALMOLIGIC COMPOSITIONS
    Publication number: 20150133455
    Abstract: The invention relates to a cellprotective, neuroprotective and retinoprotective composition. In an embodiment of the invention, said composition comprises (i) Ramipril or Ramiprilate and (ii) folic acid. The composition of the invention can be used, in particular, for the prevention of loss of vision, or even for improving visual acuity and visual field in normal subjects, as well as for treating ophthalmologic pathologies, in particular: glaucoma, diabetic retinopathy, age related macular degeneration, hereditary dystrophy of the retina, uveitis, ammetropia (myopia, presbyopia). This combination of active principles could also be used in general conditions for treating general pathologies (cancer . . . ).
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventor: Raouf REKIK
  • Triazolopyrazine
    Publication number: 20150133447
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3, X3 to X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: November 4, 2014
    Publication date: May 14, 2015
    Inventor: Harald ENGELHARDT
  • Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands
    Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Linked purine pterin HPPK inhibitors useful as antibacterial agents
    Patent number: 9029344
    Abstract: The disclosure provides linked purine pterin compounds and analogs thereof that are novel HPPK inhibitors. The HPPK inhibitors described herein are compounds and the pharmaceutically acceptable salts thereof of general Formula I The variables, e.g. A1 to A3, R1 to R4, L1, L2, B1, and B2 are described herein. Compounds and salts of Formula I bind to HPPK with high affinity and specificity. Pharmaceutical compositions containing an HPPK inhibitor of Formula I and methods of treating a bacterial infection in a patient by providing one or more HPPK inhibitors of Formula I to the patient are also provided. Processes and intermediates useful for preparing compounds of Formula I are also provided. Methods of using the disclosed compounds to guide the development of additional novel anti-bacterial agents are also provided.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: May 12, 2015
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Genbin Shi, Gary X. Shaw, Xinhua Ji