Abstract: A continuous process for obtaining acrolein by catalytic dehydration of glycerol or glycerin, in the presence of an acid catalyst, wherein said process comprises the concomitant regeneration of said catalyst and is carried out in a fluidized bed reactor, said reactor comprising two zones, a first zone, or lower zone, termed catalyst regeneration zone, in which a fluidization gas comprising oxygen is introduced, and a second zone, or upper zone, termed reaction zone, in which the glycerol or glycerin is introduced and converted into acrolein.
Type:
Grant
Filed:
October 26, 2011
Date of Patent:
April 19, 2016
Assignees:
ADISSEO FRANCE S.A.S., ECOLE CENTRALE DE LILLE
Abstract: Process for preparing pyrrolidine of the formula I by reacting 1,4-butanediol (BDO) of the formula II with ammonia in the presence of hydrogen and a supported, metal-containing catalyst, wherein the catalytically active mass of the catalyst, prior to its reduction with hydrogen, comprises oxygen-containing compounds of aluminum, copper, nickel and cobalt and in the range from 0.2 to 5.0% by weight of oxygen-containing compounds of tin, calculated as SnO, and the reaction is carried out in the liquid phase at an absolute pressure in the range from 160 to 220 bar, a temperature in the range from 160 to 230° C., using ammonia in a molar ratio to BDO used of from 5 to 50 and in the presence of 1.0 to 4.5% by weight of hydrogen, based on the amount of BDO used.
Type:
Grant
Filed:
July 12, 2013
Date of Patent:
April 19, 2016
Assignee:
BASF SE
Inventors:
Roland Bou Chedid, Johann-Peter Melder, Roman Dostalek, Jörg Pastre, Aik Meam Tan
Abstract: A compound of formula I, wherein the groups R1, R2, R3, X, m, and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
Abstract: This disclosure relates to reagents and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18F labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.
Abstract: The present invention relates to novel 3,4-dihydro-1H-pyrimido[1,6-a]pyrimidin-6(2H)-one compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
Type:
Grant
Filed:
January 23, 2014
Date of Patent:
March 29, 2016
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof wherein A represents a group represented by one of formulae (i)-(iii); B represents a group represented by formula (v) or (vi); and E represents a substituted or unsubstituted heterocyclic group having a cationic nitrogen atom.
Type:
Grant
Filed:
October 3, 2012
Date of Patent:
March 22, 2016
Assignee:
SHIONOGI & CO., LTD
Inventors:
Kenji Yamawaki, Masayuki Sano, Jun Sato
Abstract: There is disclosed a crystalline DMSO solvate of prothioconazole as well as amorphous prothioconazole. Methods for making these solid forms, microbicidal compositions comprising them and uses thereof are also disclosed.
Abstract: The present invention relates to novel bipyridine sulfonamide derivatives of formula (I) and their use for the treatment and/or prophylaxis of a neurodegenerative disease or condition, particularly Alzheimers disease (AD), a cardiovascular disease or a pathology involving ischemia. Additionally, processes for preparing such derivatives and pharmaceutical compositions comprising them are provided.
Type:
Grant
Filed:
November 21, 2011
Date of Patent:
March 15, 2016
Assignee:
AUBERGINE PHARMACEUTICALS LLC
Inventors:
Francisco Palomo Nicolau, Jorge Sánchez-Quesada, Javier López Ogalla, Félix Hernández Juan, Javier Villasante Prieto, Miguel Medina Padilla, Ana Fuertes Huerta, Juan Manuel Dominguez Correa, Susana Herrero Santos, Mercedes Alonso Cascón
Abstract: The invention relates to novel oxazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
Type:
Grant
Filed:
October 11, 2012
Date of Patent:
March 15, 2016
Assignee:
NOVARTIS AG
Inventors:
Konstanze Hurth, Sebastien Jacquier, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
Abstract: The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions.
Type:
Grant
Filed:
February 25, 2014
Date of Patent:
March 8, 2016
Assignee:
Chemapotheca, LLC
Inventors:
Harold Meckler, Brian Thomas Gregg, Jie Yang
Abstract: The ectopic expression of Mer receptor tyrosine kinase (Mer) has been identified as a tumor cell survival gene product in Acute Lymphoblastic Leukemia (ALL) cells and a potential cause of ALL chemoresistance. Hence, we investigated whether the development of small molecule Mer inhibitors was possible. A first aspect of the present invention is a compound (sometimes referred to as an “active compound” herein) of Formula I, IA, or IB.
Type:
Grant
Filed:
October 1, 2012
Date of Patent:
March 1, 2016
Assignee:
The University of North Carolina at Chapel Hill
Inventors:
Xiaodong Wang, Jing Liu, Weihe Zhang, Stephen Frye, Dmitri Kireev
Abstract: Provided are a crystalline dihydrate of Rivaroxaban, processes for the preparation thereof, pharmaceutical compositions containing the crystalline dihydrate and processes for preparing and storing the pharmaceutical compositions. Also provided are a crystalline formic acid solvate of Rivaroxaban, processes for the preparation of crystalline Rivaroxaban formic acid solvate and the use of the Rivaroxaban formic acid solvate in the manufacture of the crystalline dihydrate of Rivaroxaban.
Type:
Grant
Filed:
July 5, 2011
Date of Patent:
February 23, 2016
Assignee:
SANDOZ AG
Inventors:
Johannes Ludescher, Hubert Sturm, Ulrich Griesser, Robert E. Ziegert-Knepper, Arthur Pichler, Mairi Haddow
Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using the compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
Type:
Grant
Filed:
May 9, 2013
Date of Patent:
February 23, 2016
Assignee:
Karyopharm Therapeutics Inc.
Inventors:
Vincent P. Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to imidazo[1,2-a]pyridine containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities (HDAC).
Type:
Grant
Filed:
October 17, 2014
Date of Patent:
February 23, 2016
Assignee:
MEI PHARMA, INC.
Inventors:
Ken Chi Lik Lee, Eric T. Sun, Haishan Wang
Abstract: The present invention relates to compounds of formula (X) or pharmaceutically acceptable salts thereof, wherein R1-R50, a, b, d, e, f, g, h, i, j, k, l, o, p, q, r, s, t, u, y, and z are defined herein. The novel dihydropyrrolopyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
Type:
Grant
Filed:
April 2, 2015
Date of Patent:
February 16, 2016
Assignee:
PFIZER INC.
Inventors:
Ping Chen, Hengmiao Cheng, Judith Gail Deal, Gary Michael Gallego, Mehran Jalaie, John Charles Kath, Suvi Tuula Marjukka Orr, Hong Shen, Luke Raymond Zehnder
Abstract: The present invention relates to salts comprising novel aryl-alkyl-substituted imidazolium and triazolium cations and arbitrary anions. The invention further relates to methods for the chemical conversion and separation of substances, comprising the salts according to the invention as solvents, solvent additives, or extraction means, and to the use of the salts according to the invention, for example as solvents or solvent additives in chemical reactions, as extracting agents for the separation of substances, or for storing hydrogen.
Abstract: Compounds of formula (I): wherein R1, R2, J, Q, V, X, Y and Z are defined herein are disclosed. The compounds are inhibitors of the family of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha sub-type thereof, and of Syk kinase and the Src family of tyrosine kinases. The compounds may be used in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, in particular inflammatory diseases of the lung, such as asthma and COPD, as well as those of the gastrointestinal tract, such as ulcerative colitis and Crohn's disease and of the eye, such as uveitis.
Inventors:
Lorna Anne Duffy, John King-Underwood, Alistair Ian Longshaw, Peter John Murray, Stuart Thomas Onions, David Michael Adrien Taddei, Jonathan Gareth Williams, Kazuhiro Ito, Catherine Elisabeth Charron
Abstract: The invention relates to compounds of formula (I) wherein X1, X2, R1 to R4, m, and n have the meaning as cited in the description and the claims. The compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including the compounds, the preparation of such compounds as well as the use as medicaments.
Type:
Grant
Filed:
March 4, 2011
Date of Patent:
February 2, 2016
Assignee:
CELLZOME LIMITED
Inventors:
Jessica Taylor, Daniel Paul Hardy, Rosemary Lynch, Helen Sarah Niblock, Andrew David Cansfield