Abstract: A method for synthesizing of thioesters by using a compound as a catalyst is disclosed. The compound is represented by formula I below: In formula I, R5 represents H, a substituted or unsubstituted alkyl, a substituted or unsubstituted aryl, or a substituted or unsubstituted heteroaryl; X and Y each independently represents one of H, C1-10 alkyl, C5-10 aryl, C1-10 alkyl alcohol, thiohydroxy, carbonyl, sulfonyl, sulfamoyl, carbamoyl, C1-10 alkoxycarbonyl, C1-10 alkoxycarbamoyl, C1-10 alkylamino, C1-10 alkylsulfonyl, C1-10 haloalkylsulfonyl, ureido, amido, and C1-10 alkoxylcarbamoyl; and n is 0, 1, 2, 3, 4 or 5.
Abstract: The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
Abstract: The present invention relates to a cosmetic process for treating keratin materials, which can give them, especially in a long-lasting and reversible manner, interesting cosmetic properties; this process comprising the application to said materials: in a first stage, of a cosmetic composition comprising at least one graftable species, comprising at least one unit of formula (Ia): and in a second stage, of a cosmetic composition comprising at least one cosmetic active agent bearing at least one unit of formula (Ia): The invention also relates to a kit comprising said compositions.
Type:
Grant
Filed:
June 12, 2015
Date of Patent:
February 7, 2017
Assignee:
L'OREAL
Inventors:
Anne-Claude Dublanchet, Christian Blaise
Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
Type:
Grant
Filed:
March 15, 2016
Date of Patent:
January 31, 2017
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf Lotz, Mohammad Tadayyon
Abstract: A process for synthesis of enatiomerically pure or enatiomerically enriched or racemic mixture of (+ and/or ?) epicatechin and its intermediates, comprising the steps of: (i) obtaining penta-protected quercetin; (ii) reducing the penta-protected quercetin obtained from step (i); (iii) optionally deprotecting the compound of step (ii); (iv) reducing the compound obtained from step (ii) or step (iii) in the presence of a chiral/achiral reducing agent to obtain a chiral intermediate; (v) deprotecting and/or hydrogenation of the chiral intermediate obtained from step (iv) to obtain (?)-epicatechin; (vi) optionally simultaneously deprotecting and by drogenation of the compound obtained from step (ii) to obtain racemic epicatechin.
Abstract: The present invention discloses novel chemical compounds obtained by causing a covalent attachment of a modifying agent of the structure provided for formula 1, to a functional group or a heteroatom of a heterocyclic ring system in chemical compound with improved chemical and biological properties. Wherein: Y is DRUG-CO; DRUG-OCO; DRUG-NRCO, and X is selected from.
Type:
Grant
Filed:
October 7, 2013
Date of Patent:
January 31, 2017
Assignee:
SPHAERA PHARMA PTE LTD.
Inventors:
Sundeep Dugar, Frank Peter Hollinger, Dinesh Mahajan, Rhushikesh Chandrabhan Deokar
Abstract: Provided herein are compounds of Formula I: in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, which are DP2 receptor modulators useful in the treatment of immunologic diseases.
Type:
Grant
Filed:
May 4, 2015
Date of Patent:
January 31, 2017
Assignee:
Array BioPharma Inc.
Inventors:
Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff, Ganghyeok Kim
Abstract: The present invention relates to novel ?-lactam compounds, their preparation and use. In particular, this invention relates to novel ?-lactam compounds which are amidine substituted monobactam derivatives useful as antimicrobial agents and their preparation.
Type:
Grant
Filed:
January 23, 2013
Date of Patent:
January 31, 2017
Assignee:
AiCuris GmbH & Co. KG
Inventors:
Burkhard Klenke, Irith Wiegand, Guido Schiffer, Heike Broetz-Oesterhelt, Samarendra N. Maiti, Jehangir Khan, Andhe Reddy, Zhixiang Yang, Mostafa Hena, Guofeng Jia, Ou Ligong, Hong Liang, Judy Yip, Chuanjun Gao, Sabiha Tajammul, Rahim Mohammad, Ganguli Biswajeet
Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
Type:
Grant
Filed:
January 16, 2015
Date of Patent:
January 31, 2017
Assignee:
Massachusetts Institute of Technology
Inventors:
Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
Abstract: This invention pertains to hydroformylation catalysts containing a mixture of isomeric forms of halo-phosphorus ligands. This invention also describes a procedure for preparing isomers of certain halophosphite ligands, which contain the phosphorus atom in a macrocyclic ring.
Type:
Grant
Filed:
June 13, 2016
Date of Patent:
January 24, 2017
Assignee:
Eastman Chemical Company
Inventors:
Thomas Allen Puckette, Xiaopeng Shan, Jody Lee Rodgers, Brian E. Green
Abstract: The invention provides methods and compositions for use in treating diseases associated with excessive cellular proliferation, such as cancer.
Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.
Type:
Grant
Filed:
January 25, 2013
Date of Patent:
January 24, 2017
Assignee:
Vanda Pharmaceuticals, Inc.
Inventors:
Marlene Michelle Dressman, Louis William Licamele, Mihael H. Polymeropoulos
Abstract: A resist composition containing a compound represented by the general formula (1) or (2), a method for forming a resist pattern using the composition, a polyphenolic compound for use in the composition, and an alcoholic compound that can be derived therefrom are described.
Abstract: The present invention relates to a process for the manufacturing of pure and substantially oligomers-free 1,4:3,6-dianhydrohexitol di(alkyl carbonate)s which comprises the steps of: a) Preparing a reaction mixture consisting of at least one dianhydrohexitol, at least 2 molar equivalents with respect to the amount of dianhydrohexitol present, of at least one dialkyl carbonate of formula R—O—C(?O)—O—R, where R has the same meaning indicated above, and from 0.01 to less than 0.1 molar equivalents of a transesterification catalyst with respect to the amount of dianhydrohexitol present; and b) Heating the reaction mixture up to its reflux temperature in a reactor preferably equipped with a rectification column comprising a number of theoretical distillation plates sufficient to separate continuously from the reaction mixture by fractional distillation the alcohol obtained or the azeotrope which the alcohol forms with the dialkyl carbonate present in the reaction mixture.
Type:
Grant
Filed:
January 24, 2013
Date of Patent:
January 10, 2017
Assignee:
Fundacion Technalia Research & Innovation
Inventors:
Jose Ramon Ochoa Gomez, Silvia Gil Rio, Belen Maestro Madurga, Leire Lorenzo Ibarreta, Olga Gomez De Miranda Jimenez De Aberasturi
Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.
Type:
Grant
Filed:
April 16, 2015
Date of Patent:
January 10, 2017
Assignee:
Vanda Pharmaceuticals, Inc.
Inventors:
Marlene Michelle Dressman, John Joseph Feeney, Louis William Licamele, Mihael H. Polymeropoulos
Abstract: The present invention provides 2,6,7,8 Substituted Purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
Type:
Grant
Filed:
January 29, 2014
Date of Patent:
January 10, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Carolyn Michele Cammarano, Matthew P. Christopher, Christopher Dinsmore, Ronald J. Doll, Francesc Xavier Fradera Llinas, Chaomin Li, Michelle Machacek, Michelle Martinez, Latha G. Nair, Weidong Pan, Michael Hale Reutershan, Manami Shizuka, Dietrich P. Steinhuebel, Binyuan Sun, Christopher Francis Thompson, B. Wesley Trotter, Yaolin Wang, Liping Yang, Stephane L. Bogen, Matthew E. Voss, Jagannath Panda, Anthappan Tony Kurissery
Abstract: The present disclosure provides ?-diketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
Type:
Grant
Filed:
February 21, 2014
Date of Patent:
January 3, 2017
Assignee:
Samumed, LLC
Inventors:
Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
Abstract: Provided is a method for producing an oxime compound with satisfactory selectivity. Provide is a method for producing an oxime represented by the following formula (II): wherein R1 and R2 are respectively the same as defined below, the method including oxidizing an amine represented by the following formula (I): wherein R1 and R2 each independently represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group (provided that R1 and R2 are not simultaneously hydrogen atoms), or R1 and R2, together with the carbon atom to which R1 and R2 are attached, form an optionally substituted alicyclic hydrocarbon group having 3 to 12 carbon atoms [hereinafter sometimes referred to as the amine compound (I)], with oxygen in the presence of a layered silicate.
Type:
Grant
Filed:
December 12, 2013
Date of Patent:
January 3, 2017
Assignee:
Sumitomo Chemical Company, Limited
Inventors:
Masahiro Hoshino, Yuta Kikuchi, Sho Tsujiuchi
Abstract: The present patent discloses a one step process for the synthesis of THF and related ring hydrogenated products form furfural using Palladium metal based carbon supported catalyst with high selectivity and 100% conversion in both batch and continuous modes.
Type:
Grant
Filed:
January 30, 2014
Date of Patent:
December 27, 2016
Assignee:
Council of Scientific & Industrial Research