Abstract: The present invention relates to polymorphic forms of the compound of Formula I (i.e., ethyl 2-cyano-3,12-dioxoIeana-1,9(11)-dien-28-oate (CDDO ethyl ester)) and methods of using them for treating a variety of disease states such as cancer and condisitons associated with inflammation.
Type:
Grant
Filed:
December 6, 2012
Date of Patent:
May 23, 2017
Assignee:
Applied Pharmaceutical Science, Inc.
Inventors:
Xiaohong Zhang, Lu Song, Wendong Sun, Kaiyang Liu, Chunlei Han
Abstract: The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, which has a superior peripheral blood lymphocyte decreasing action, and is useful for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of transplantation of organ or tissue; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases.
Abstract: The invention relates to compounds of Formula A: or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
Abstract: A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by dissolving an isopropanol-solvated crystal of ulipristal acetate in a mixed solvent containing ethanol and water, and crystallizing an ulipristal acetate from the solution without addition of a seed crystal to the solution.
Abstract: A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by crystallization or transition in association with a specified solvent. The solvent comprises at least one member selected from the group consisting of water, an aliphatic hydrocarbon, an aromatic hydrocarbon, a halogenated hydrocarbon, a linear alcohol, an alkyl ether, an acetate ester, an alkyl ketone, an N-alkylacylamide, and an alkanenitrile.
Abstract: The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.
Type:
Grant
Filed:
December 26, 2013
Date of Patent:
May 2, 2017
Assignee:
HETERO RESEARCH FOUNDATION
Inventors:
Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Lanka Vl Subrahmanyam, Gazula Levi David Krupadanam, Mukkera Venkati, Neela Sudhakar, Kallem Srinivas Reddy
Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.
Type:
Grant
Filed:
June 5, 2015
Date of Patent:
May 2, 2017
Assignee:
Kythera Biopharmaceuticals, Inc.
Inventors:
Robert M. Moriarty, Nathaniel E. David, Nadir Ahmeduddin Mahmood
Abstract: The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1, R2, R3, R4, R5, and R6 are as described herein. The present invention relates generally to selective FXR agonists and to methods of making and using them.
Abstract: The present invention provides novel substituted quinoline compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
Type:
Grant
Filed:
August 12, 2015
Date of Patent:
March 21, 2017
Assignees:
CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
Abstract: The present invention relates to a novel geranyl flavonoid derivative with improved water-solubility or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a method for treating cancer using the same. Particularly, the novel geranyl flavonoid derivative of the present invention inhibits the expression of STAT3 target protein by suppressing the phosphorylation of STAT3 (Signal Transducers and Activators of Transcription 3) protein, suggesting that it has cancer cell growth inhibiting effect in various cancer cell lines. Also, the compound of the invention has the effect of reducing the size and weight of a tumor significantly in vivo, so that the geranyl flavonoid derivative or the pharmaceutically acceptable salt thereof can be efficiently used for the treatment of cancer.
Type:
Grant
Filed:
June 5, 2015
Date of Patent:
February 28, 2017
Assignee:
Korea Research Institute of Bioscience and Biotechnology
Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
Type:
Grant
Filed:
December 3, 2015
Date of Patent:
February 28, 2017
Assignee:
Duke University
Inventors:
Mitchell A. deLong, John M. McIver, Robert S. Youngquist
Abstract: The present invention provides triterpenoids produced from natural compounds such as oleanolic acid, ursolic acid, betulinic acid, and hederagenin.
Type:
Grant
Filed:
September 25, 2014
Date of Patent:
January 10, 2017
Assignee:
Trustees of Dartmouth College
Inventors:
Gordon W. Gribble, Liangfeng Fu, Michael B. Sporn, Karen T. Liby
Abstract: The invention relates to compounds of Formula A: or a salt, solvate, or hydrate thereof. The compounds of formula A are TGR5 modulators useful for the treatment of disease.
Abstract: The present invention pertains, at least in part, to novel substituted etracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.
Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.
Type:
Grant
Filed:
September 30, 2014
Date of Patent:
December 20, 2016
Assignee:
KYTHERA BIOPHARMACEUTICALS, INC.
Inventors:
Robert M. Moriarty, Nathaniel E. David, Nadir Ahmeduddin Mahmood
Abstract: This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.
Type:
Grant
Filed:
August 23, 2013
Date of Patent:
December 13, 2016
Assignees:
RESEARCH TRIANGLE INSTITUTE, The United States of America, as represented by the Secretary, Department of Health and Human Services
Inventors:
Scott P Runyon, Michael Rogawski, Edgar Cook, John Kepler, Hernan Navarro, Rafal Kaminski, Matthew Orr
Abstract: The present invention relates to a pure polymorph of Nor-UDCA or Bis-nor-UDCA, or of a pharmaceutically acceptable salt thereof. The invention further provides a pharmaceutical composition comprising the polymorph of the invention, and a method for preparing the polymorph. The invention includes the pharmaceutical use of the polymorph or of the pharmaceutical composition of the invention.
Type:
Grant
Filed:
November 30, 2011
Date of Patent:
December 6, 2016
Assignee:
Dr. Falk Pharma GmbH
Inventors:
Rudolf Wilhelm, Markus Proels, Erik Fischer, Heidi Waenerlund Poulsen
Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.
Type:
Grant
Filed:
November 16, 2011
Date of Patent:
December 6, 2016
Assignee:
TEXAS HEART INSTITUTE
Inventors:
Ronald J. Biediger, William C. Gundlach, IV, Robert V. Market, Michael M. Savage, Peter Vanderslice
Abstract: Disclosed herein are compositions and methods for the treatment or prophylaxis of a subject having or susceptible to a kidney disease. The method includes the step of administering to the subject a compound of formula (I) in a dose of about 1 to 10 mg/Kg to improve the glomerular filtration rate (GFR) of the subject for at least 4 folds as compared to the GFR of the subject before treatment, The method further includes the step of administering to the subject an effective amount of lucidenic acid C (LAC), lucidenic acid N (LAN), lucidenic acid E2 (LAE2), lucidenic acid A (LAA), and lucidenic acid D2 (LAD2).
Type:
Grant
Filed:
June 9, 2014
Date of Patent:
December 6, 2016
Inventors:
Cheng-Po Huang, Teng-Hai Chen, Kuang Dee Chen, Chun-Tao Su
Abstract: Disclosed herein are cocrystals of progesterone and a coformer containing a six-membered aromatic ring having at least one substituent possessing a carbonyl functionality. Cocrystals of progesterone and a coformer selected from vanillic acid, benzoic acid, salicylic acid, cinnamic acid, or vanillin are also disclosed herein.
Type:
Grant
Filed:
September 4, 2013
Date of Patent:
December 6, 2016
Assignee:
AMRI SSCI, LLC
Inventors:
Ekaterina Albert, Patricia Andres, Melanie Janelle Bevill, Jared Smit, Jennifer Nelson