Abstract: Phenoxy acetic acids and phenyl propionic acids and their use in treating type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, or obesity are provided herein. The present compounds are activators of PPAR? and may be useful for treating conditions mediated by the same.
Type:
Grant
Filed:
September 3, 2013
Date of Patent:
May 30, 2017
Assignee:
vTv Therapeutics LLC
Inventors:
Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
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.
Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
Type:
Grant
Filed:
September 6, 2016
Date of Patent:
May 23, 2017
Assignee:
Genentech, Inc.
Inventors:
Steven P. Govek, Mehmet Kahraman, Nicholas D. Smith, Jeffrey H. Hager, Edna Chow Maneval
Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
Type:
Grant
Filed:
September 29, 2014
Date of Patent:
May 23, 2017
Assignee:
ALLERGAN, INC.
Inventors:
Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
Abstract: The present invention is directed to an improved process for the preparation of compounds of Formula (II) and Formula (III), which are useful in the inhibition of PDE10. In particular, the present invention is directed to an improved process for the preparation of 1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, which is useful in the inhibition of PDE10.
Type:
Grant
Filed:
April 24, 2015
Date of Patent:
May 16, 2017
Assignee:
Omeros Corporation
Inventors:
Neil S. Cutshall, Jennifer Lynn Gage, Thomas L. Little, Wayne Douglas Luke, Elisabeth C. A. Brot, Marco Jonas, Michael James McDermott, Karl E. Reineke
Abstract: The present invention relates to molecules which function as selective modulators (i.e., inhibitors and agonists, preferably inhibitors) of the Ras-homologous (Rho) family of small GTPases, in particular, Cdc42 GTPase and their use to treat diseases, for example cancers, including metastatic cancer, where Cdc42 GTPase is overexpressed or hyperactivated, genetic and acquired diseases where activation of Cdc42 GTPase plays a pivotal role (e.g., neurodegenerative diseases), rheumatoid arthritis, atherosclerosis, diabetes type I, autosomal polycystic kidney diease, cystic kidney disease, precystic kidney disease and microbial infections. Additionally, compounds according to the present invention may be used to inhibit rejection (graft host response) in transplant patients (pursuant to transplantation), to promote immunosuppression, anti-inflammatory response and to mobilize stem cell (migration) in patients in need, among others.
Type:
Grant
Filed:
April 22, 2013
Date of Patent:
May 9, 2017
Assignees:
STC.UNM, UNIVERSITY OF KANSAS
Inventors:
Angela Wandinger-Ness, Larry Sklar, Zurab Surviladze, Tudor Oprea, Laurie Hudson, Jeffrey Aube, Jennifer E. Golden, Chad E. Schroeder, Denise S. Simpson, Julica J. Noth
Abstract: The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.
Type:
Grant
Filed:
August 18, 2015
Date of Patent:
May 9, 2017
Assignee:
CORSAIR PHARMA, INC.
Inventors:
Xiaoming Zhang, Meenakshi S. Venkatraman, Cyrus K. Becker
Abstract: The present invention provides new stable crystalline N-iodoamides-1-iodo-3,5,5-trimethylhydantoin (1-ITMH) and 3-iodo-4,4-dimethyl-2-oxazolidinone (IDMO). The present invention further provides a process for the preparation of organic iodides using N-iodoamides of this invention and recovery of the amide co-products from waste water.
Type:
Grant
Filed:
November 5, 2014
Date of Patent:
May 2, 2017
Assignee:
Technion Research & Development Foundation Limited
Inventors:
Gennady Nisnevich, Kseniya Kulbitski, Mark Gandelman, Alexander Artaryan
Abstract: Disclosed herein are compounds of the formula: compositions thereof, and methods for the treatment of glaucoma, reducing intraocular pressure, and other prostaglandin EP2 mediated disease and disorders.
Abstract: A bisoxime ester photoinitiator as represented by general formula (I). By introducing a bisoxime ester group and a cycloalkylalkyl group into the chemical structure, this photoinitiator not only has excellent performance in aspects of storage stability, photosensitivity, developability, pattern integrity, and the like, but also exhibits obviously improved photosensitivity and thermal stability compared to similar photoinitiators.
Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
February 18, 2016
Date of Patent:
May 2, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
Abstract: Disclosed herein are compounds comprising a polymer conjugated with a pH-sensitive prodrug of beta-lapachone, wherein the compound is capable of forming a micelle, and wherein the pH-sensitive prodrug comprises a pH-sensitive linker selected from the group consisting of: an aryl imine and an aliphatic imine. Also provided are micelles comprised of such polymer-prodrug conjugates. Further provided are methods for treating cancer with the micelles.
Type:
Grant
Filed:
August 11, 2011
Date of Patent:
April 25, 2017
Assignee:
The Board of Regents of the University of Texas System
Inventors:
Jinming Gao, David Boothman, Yinjian Zhou, Erik Bey
Abstract: This present invention discloses a nitro-containing bisoxime ester photoinitiator having a structure represented by general formula (I). This photoinitiator has excellent application performances in terms of storage stability, photosensitivity, developability, pattern integrity, etc., and it has good adaptability to single-wavelength UV-LED light sources and exhibits a photosensitive property, which is obviously superior to those of existing photoinitiators, under the irradiation of UV-LEDs.
Abstract: The present invention provides a novel amorphous Form of azilsartan acid, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides novel crystalline Forms of azilsartan medoxomil, processes for their preparations and pharmaceutical compositions comprising them. The present invention further provides a novel amorphous Form of azilsartan medoxomil potassium, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a novel process for the preparation of azilsartan medoxomil potassium crystalline Form II.
Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
Type:
Grant
Filed:
June 30, 2015
Date of Patent:
April 18, 2017
Assignee:
AMIRA PHARMACEUTICALS, INC.
Inventors:
Thomas J. Seiders, Lucy Zhao, Jeannie Arruda, Bowei Wang, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Ryan Clark, Heather Renee Coate, Nicholas Simon Stock, Deborah Volkots
Abstract: Disclosed are compounds of the Formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and m are as described herein, as modulators of the nicotinic acetylcholine receptors, particularly the ?7 subtype, their tautomeric forms, stereoisomers, and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and combinations thereof with suitable other medicaments. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and/or treatment of disorders such as Alzheimer's disease, mild cognitive impairment, and senile dementia.
Abstract: Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and m are as described herein, as a modulator of nicotinic acetylcholine receptors particularly ?7 subtype, its tautomeric forms, its stereoisomers, its pharmaceutically acceptable salts, its pharmaceutical composition, and its combinations with suitable medicaments. 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 present invention relates to new imidazo[2,1-b]thiazole derivatives having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
Type:
Grant
Filed:
July 4, 2013
Date of Patent:
April 11, 2017
Assignee:
LABORATORIES DEL DR. ESTEVE S.A.
Inventors:
María de las Ermitas Alcalde-Pais, José Luís Diaz Fernández, María de les Neus Mesquida-Estevez, Laura Paloma-Romeu
Abstract: The present invention is directed to compounds and pharmaceutical formulations comprising these compounds which are useful as O-linked N-acetylglucosaminidase (O-GlcNAcase) inhibitors, and thus may be useful for the treatment of certain disorders such as Alzheimer's disease including reducing NFTs and/or hyperphosphorylated tau. The invention is also directed to use of the compounds as O-GlcNAcase imaging agents.
Inventors:
Harold G. Selnick, Wenping Li, Eric Hostetler, Kun Liu, Ernest J. McEachern, Yuanxi Zhou, Zhongyong Wei, Changwei Mu, Yaode Wang, Jiang Chang