Abstract: This invention relates to compounds of formula II: wherein R1, R2, ProtSH, and ProtNH are as defined, to processes for the synthesis of ecteinascidins of formula I from compounds of formula II, and to processes for the synthesis of compounds of formula II.
Type:
Grant
Filed:
May 24, 2011
Date of Patent:
August 30, 2016
Assignee:
PHARMA MAR, S.A.
Inventors:
Ma Jesús Martin López, Andrés Francesch Solloso, Maria del Carmen Cuevas Marchante
Abstract: Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1, R2, R4, R5, R6 and R7 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
Type:
Grant
Filed:
March 15, 2013
Date of Patent:
August 30, 2016
Assignee:
Janssen Sciences Ireland UC
Inventors:
Sandrine Marie Helene Vendeville, Pierre Jean-Marie Bernard Raboisson, Tse-I Lin, Abdellah Tahri, Katie Ingrid Eduard Amssoms
Abstract: The present invention provides synthetic processes for preparing racemic and/or optically pure epicatechin, epigallocatechin and related polyphenols as such or as their variously functionalized derivatives. A principle objective of the disclosure is to provide a new and useful method of synthesis to obtain polyphenols in isomerically pure and/or racemic forms.
Type:
Grant
Filed:
January 24, 2012
Date of Patent:
August 30, 2016
Assignee:
SPHAERA PHARMA PTE. LTD.
Inventors:
Sundeep Dugar, Dinesh Mahajan, Peter Giannousis Pantelis, Vijay Singh, Kamal Kishore Kapoor
Abstract: Disclosed herein are 6-substituted 13-demethyl-estradiol derivatives as selective ER? agonists. Also disclosed is a method for treating pain by administering these 6-substituted 13-demethyl-estradiol derivatives.
Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis. The invention also provides processes for preparing compounds of the invention.
Type:
Grant
Filed:
October 31, 2013
Date of Patent:
August 23, 2016
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis, Harmon J. Zuccola
Abstract: The present invention relates to compounds suitable for use in electronic devices, and to electronic devices, especially organic electroluminescent devices, comprising these compounds.
Type:
Grant
Filed:
February 28, 2013
Date of Patent:
August 23, 2016
Assignee:
Merck Patent GmbH
Inventors:
Philipp Stoessel, Elvira Montenegro, Arne Buesing, Teresa Mujica-Fernaud, Joachim Kaiser
Abstract: The present invention relates to compounds of the following general formula (I), or to a pharmaceutically acceptable salt thereof, as well as to the uses thereof as a drug, in particular in the treatment of cancerous or precancerous hyperproliferative conditions, and to the pharmaceutical compositions containing same.
Type:
Grant
Filed:
August 1, 2013
Date of Patent:
August 16, 2016
Assignee:
PIERRE FABRE MEDICAMENT
Inventors:
Frédéric Marion, Frédéric Lieby-Muller, Serge Grisoni, Nicolas Rahier, Michel Perez, Isabelle Sartori
Abstract: The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1-propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.
Type:
Grant
Filed:
November 17, 2014
Date of Patent:
August 16, 2016
Assignee:
MannKind Corporation
Inventors:
John J. Freeman, Adrienne Stamper, Melissa Heitmann
Abstract: This disclosure relates to new azepino[4,5-b]indole compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new 1,2,3,4,5,6-tetrahydroazepino[4,5-b]indoles. Pharmaceutical compositions are also provided.
Type:
Grant
Filed:
March 8, 2013
Date of Patent:
August 9, 2016
Assignee:
Medivation Technologies, Inc.
Inventors:
David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sarvajit Chakravarty
Abstract: The present invention relates to Bridged Bicyclic Piperidine Derivatives, compositions comprising a Bridged Bi-cyclic Piperidine Derivative, and methods of using the Bridged Bicyclic Piperidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
Type:
Grant
Filed:
October 28, 2010
Date of Patent:
August 9, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Joel M. Harris, Andrew Stamford, William J. Greenlee, Santhosh Francis Neelamkavil
Abstract: The present invention relates to a method for the preparation of sitagliptin phosphate and sitagliptin phosphate anhydrous of Formula (I?) and monohydrate of Formula (I),
Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.
Type:
Grant
Filed:
April 22, 2015
Date of Patent:
August 2, 2016
Assignee:
Cancer Research Technology Limited
Inventors:
Ian Collins, Michael Lainchbury, Thomas Peter Matthews, John Charles Reader
Abstract: Pyrazolo[1,5-a]pyrimidine-based compounds of the formula: are disclosed, wherein R1, R2 and R3 are defined herein. Compositions comprising the compounds and methods of their use to treat, manage and/or prevent diseases and disorders mediated by adaptor associated kinase 1 activity are also disclosed.
Type:
Grant
Filed:
September 11, 2014
Date of Patent:
August 2, 2016
Assignee:
Lexicon Pharmaceuticals, Inc.
Inventors:
Yingzhi Bi, Kenneth Gordon Carson, Giovanni Cianchetta, Michael Alan Green, Godwin Kumi, Alan Main, Yulian Zhang, Glenn Gregory Zipp
Abstract: A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.
Abstract: A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.
Abstract: Hydrocarbon feedstocks are desulfurized by conversion of organosulfur compounds in a mixture of hydrocarbons into sulfoxides and/or sulfones. The oxidant used to promote oxidation of organosulfur-compounds is electrosynthesized in-situ.
Abstract: This invention relates to a method of preparing an ester compound, including adding carboxylic acid to a mixture of glycerol and acetone in the presence of a sulfuric acid catalyst and applying an ultrasonic wave to induce an esterification reaction, and to an ester compound prepared thereby.
Type:
Grant
Filed:
December 1, 2014
Date of Patent:
July 19, 2016
Assignee:
LG Chem, Ltd.
Inventors:
Myungjin Kong, Won Jae Lee, Yong-Jin Choe
Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of asthma and allergy may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of respiratory diseases, respiratory disorders, COPD, bronchitis, brain injury, inflammation, inflammatory skin diseases, asthma, allergic reactions, infections due to acute allergy, bronchospasm, respiratory distress, acute asthma, leukotrienes over activity, 5-LO enzyme activity and cancer.
Abstract: A method for making the compound is set forth utilizing the starting material
Type:
Grant
Filed:
October 17, 2014
Date of Patent:
July 19, 2016
Assignee:
Bristol-Myers Squibb Company
Inventors:
Martin D. Eastgate, Michael S. Bultman, Ke Chen, Dayne Dustan Fanfair, Richard J. Fox, Thomas E. La Cruz, Boguslaw M. Mudryk, Christina Ann Risatti, James H Simpson, Maxime C. Soumeillant, Jonathan Clive Tripp, Yi Xiao
Abstract: The present invention relates to pharmaceutically acceptable acid addition salts of sitagliptin, in particular anti-oxidant acid addition salts of sitagliptin and a process for its preparation. The present invention also provides a pharmaceutical composition using the pharmaceutically acceptable acid addition salts of sitagliptin.