Abstract: The invention relates to (among other things) oligomer-PTK inhibitor conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over PTK inhibitor compounds lacking a water-soluble, non-peptidic oligomer.
Abstract: A polymerizable yellow dye which is used to block or lower the intensity of blue light transmitted through ophthalmic lenses and is represented by the following formula (I): wherein R1 is hydrogen or —NHCOCH3; R2 is hydrogen or C1-C3 alkyl groups; R3 and R4 are independently hydrogen or —OCO—R5, wherein R5 is isopropenyl group or a substituted isopropenyl group represented as —R6—(R7O)n—COC(CH3)CH2, R6 is NH or R7 is C1-C5 alkylene groups and n is an integer of 1-40.
Abstract: The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a -amino- -biphenyl- -methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
Type:
Grant
Filed:
August 22, 2011
Date of Patent:
July 21, 2015
Assignee:
Novartis AG
Inventors:
David Hook, Bernhard Riss, Jianguang Zhou, Yunzhong Li, Erhard Bappert
Abstract: The present invention describes a method to generate new chemical entities (NCEs) that have well-defined activities such as, but not limited to, anti-bacterial, antifungal and anthelmintic effects. The NCEs are generated through adaptive evolution of one microbe (the producer) against another organism or cell type (the target). The producer is made to compete against the target over time by co-culturing the two together and serially passing the producer organism until the producer adaptively evolves by synthesizing an NCE(s) that inhibits growth of or kills the target. The molecular structure of the chemical entity (or entities) is then elucidated using tools from genomics, molecular biology, computational biology, analytical chemistry, organic chemistry and related fields.
Type:
Grant
Filed:
October 28, 2011
Date of Patent:
July 14, 2015
Assignee:
The Regents of the University of California
Abstract: The present invention relates to nitrogenous associative molecules comprising at least one unit rendering them capable of associating with one another or with a filler by noncovalent bonds, and comprising a function capable of reacting with a polymer containing unsaturations so as to form a covalent bond with said polymer.
Type:
Grant
Filed:
July 12, 2011
Date of Patent:
July 7, 2015
Assignee:
ARKEMA FRANCE
Inventors:
Nicolas Seeboth, Serguey Ivanov, Jean-Luc Couturier, Manuel Hidalgo
Abstract: In a process for oxidizing a hydrocarbon to a product comprising at least one of the corresponding hydroperoxide, alcohol, ketone, carboxylic acid and dicarboxylic acid, the hydrocarbon is contacted with an oxygen-containing compound in at least one oxidation zone in the presence of a catalyst comprising a cyclic imide having an imide group of formula (I): wherein X represents an oxygen atom, a hydroxyl group, or an acyloxy group and wherein the oxygen-containing compound supplied to said at least one oxidation zone has a water content of less than or equal to 0.6% by weight of the oxygen-containing compound.
Type:
Grant
Filed:
August 16, 2011
Date of Patent:
July 7, 2015
Assignee:
ExxonMobil Chemical Patents Inc.
Inventors:
Christopher L. Becker, Jihad M. Dakka, Francisco M. Benitez, Edmund J. Mozeleski
Abstract: Disclosed is a compound of formula (I), wherein Z, m and R1-R6 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogs, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogs. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
Abstract: The invention described herein pertains to substituted dibenzonaphthyridine compounds, pharmaceutical compositions, and formulations comprising the dibenzonaphthyridine compounds, their synthesis, and methods for their use in the treatment and/or prevention of cancer.
Abstract: The present invention relates to substituted pyrrole compounds and compositions comprising substituted pyrrole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted pyrrole compound of the invention, or a pharmaceutical composition comprising such a compound.
Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.
Abstract: (R)-Nifuratel is disclosed together with its use as bactericide and bacteriostatic agent as well as the pharmaceutical compositions containing the same; (R)-nifuratel has been surprisingly found to possess a better antimicrobial profile than either nifuratel racemate or (S)-nifuratel. A new procedure for the synthesis of both (R)-Nifuratel and (S)-Nifuratel is also disclosed.
Type:
Grant
Filed:
January 28, 2015
Date of Patent:
June 30, 2015
Assignee:
POLICHEM SA
Inventors:
Stefania Gagliardi, Alessandra Consonni, Federico Mailland, Anna Bulgheroni
Abstract: The present invention disclosed a preparation method of parylene AF4, which provides a reactant and a reducing agent with the use of catalyst or exposure to UV light with photo-initiator, to shorten the reaction time as a result of minimized the byproduct(s) formation, and obtain high purity (>99.0%) of parylene AF4 product under high concentrated reaction mixture.
Abstract: A process for producing a charge control agent comprising an azo-based iron complex salt compound as an effective component, comprises: synthesizing a monoazo compound through diazotization coupling; and ironing the monoazo compound by using an ironizing agent such as ferric chloride to produce an azo-based iron complex salt compound represented by the following formula. The ironization reaction of the monoazo compound is carried out while pH is kept at 7.0 to 8.0. Since the above azo-based iron complex salt compound having high purity can be obtained at a high yield, it can be used as a charge control agent directly and a special purification step can be eliminated, thereby making it possible to greatly cut the production cost.
Abstract: The present invention disclosed a preparation method of parylene AF4, which provides a reactant and a reducing agent with the use of catalyst or exposure to UV light with photo-initiator, to shorten the reaction time as a result of minimized the byproduct(s) formation, and obtain high purity (>99.0%) of parylene AF4 product under high concentrated reaction mixture.
Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.
Type:
Grant
Filed:
May 19, 2014
Date of Patent:
June 9, 2015
Assignee:
ASTEX THERAPEUTICS, LTD.
Inventors:
Valerio Berdini, Michael Alistair O'Brien, Maria Grazia Carr, Theresa Rachel Early, Adrian Liam Gill, Gary Trewartha, Alison Jo-Anne Woolford, Andrew James Woodhead, Paul Graham Wyatt
Abstract: The present invention relates to novel bipyridyl derivatives 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:
July 29, 2014
Date of Patent:
June 9, 2015
Assignee:
Merck Patent GmbH
Inventors:
Guenter Hoelzemann, Dieter Dorsch, Alfred Jonczyk, Christiane Amendt, Frank Zenke
Abstract: The present invention describes compounds of formula (I) Wherein: R1 is selected from C1-C6 alkyl, CF3, Phenyl & 2-thienyl R2 is selected from C1-C6 alkyl, phenyl & CF3 R3 is selected from H, C1-C6 alkyl, halo, NO2, NH2, haloalkyl R4 is selected from H, C1-C6 alkyl, halo, NO2, NH2, haloalkyl R5 is selected from H, C1-C6 alkyl, halo, NO2, NH2, haloalkyl R6 is selected from H, —(CH2)nC(O)OR7 & C(O)C6H4—R7 R7 is selected from C1-C6 alkyl, phenyl optionally substituted by 1-3 substituents selected from CF3, NO2 and halo. n is 0-6 These compounds have been identified as novel anticancer agents.
Type:
Grant
Filed:
November 8, 2013
Date of Patent:
June 9, 2015
Assignee:
UNITED ARAB EMIRATES UNIVERSITY
Inventors:
Ibrahim Mahmoud Abdou, Alaa ElDin Abdel Aziz Salem, Abdu Adem, Hussein F. Zhodi, Hany Abdel Aziz El Deab
Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.
Abstract: The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
Type:
Grant
Filed:
September 14, 2012
Date of Patent:
June 2, 2015
Assignee:
Merck Sharp & Dohme B.V.
Inventors:
Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Cristian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik