The Hetero Ring Is Five-membered, Consisting Of One Oxygen And Four Carbons, And Shares The Spiro Atom With A Six-membered Oxygen Containing Hetero Ring (e.g., Sapogenins, Etc.) Patents (Class 540/17)
Abstract: The present invention pertains to the field of pharmaceutical chemistry, and relates to compounds having cyclopentanoperhydrophenanthrene skeletons and preparation methods therefore. The compounds have some physiological activity, and are useful as synthons/intermediates for further synthesizing some compounds having specific structures. These compounds and salts thereof are useful as lead compounds for synthesizing pharmaceuticals, pesticides and new materials. From this, further screen and preparation by chemical, biological and medical means offer new compounds that are more valuable and have important applications, achieving the object of inventing and creating new drugs.
Abstract: The present invention relates to the fields of chemistry and pharmacy and, in particular, to the production of novel molecular entities: esterane derivatives fused with spirostanes rings, acting upon the Central Nervous Systems (CNS). From diosgenin, a naturally occurring sapogenin, with some subsequent transformations thereof, spirosteroid derivatives of the I-IV general formula can be obtained, with a cyclopentaneperhydrophenantrene nucleus fused to a 25R-spirostanes nucleus. Such molecular entities have an anti-inflammatory and anti-glutamatergic actions that can be used to treat inflammatory, cerebrovascular, neurodegenerative, neuropsychiatric, and neurologic diseases.
Type:
Application
Filed:
December 27, 2012
Publication date:
May 21, 2015
Inventors:
Laura Garcia Pupo, Yanier Nuñez Figueredo, Juan Enrique Tacoronte Morales, Yamila Verdecia Reyes, Estael Ochoa Rodriguez, Zaldo Castro Armando
Abstract: Provided herein are timosaponin compounds of Formula I, II, III, I?, II? and III?, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are uses of said timosaponin compounds for preparing medicament for the treatment of diseases associated with beta-amyloid in hosts or subjects in need thereof.
Abstract: In the present invention, different strategies are used to improve the bioavailability of triterpene glycosides and triterpenes including, for example, (a) a covalent approach involving modification with polyethylene glycol and (b) a formulation approach involving non-covalent encapsulation in antibody targeted pol(DL-lactic acid) nanoparticles.
Type:
Application
Filed:
January 17, 2014
Publication date:
July 17, 2014
Applicant:
Research Foundation of the City University of New York
Abstract: One or more agent selected from A/B-cis furostane, furostene, spirostane and spirostene steroidal sapogenins and ester, ether, ketone or glycosylated forms thereof, including E and/or F ring opened derivatives thereof, is used to treat or prevent L-DOPA, dopamine agonist and/or dopamine enhancer induced disorders, such as L-DOPA induced dyskinesia (LID), which is a side effect of L-DOPA, dopamine agonist and/or dopamine enhancer therapies, e.g., for Parkinson's disease. The agent according to the invention may be administered in association with the therapeutic agent for the treatment of the Parkinson's disease or another dopamine-responsive disorder.
Abstract: An agent selected from A/B-cis furostane, furostene, spirostane and spirostene steroidal sapogenins and ester, ether, ketone and glycosylated forms thereof is used to induce self-regulated homeostasis of neurotrophic factors (NFs), for example BDNF and/or GDNF, NFs with limited and manageable side effects in a subject, by modulating NFs in a non-toxic manner under homeostatic control. An effective amount of at least one such agent is administered to the subject, particularly in the treatment or prevention of a range of NF-mediated disorders, particularly neurological, psychiatric, inflammatory, allergic, immune and neoplastic disorders, and in the restoration or normalisation of neuronal and other function in or in relation to any damaged or abnormal tissue, including when assisting tissue (for example, skin, bone, eye and muscle) healing and general skin, bone, eye and muscle health.
Type:
Application
Filed:
January 22, 2010
Publication date:
February 9, 2012
Inventors:
Daryl Rees, Antonia Orsi, Patrick Howson, Zongqin Xia, Yaer Hu
Abstract: A non-aqueous electrolyte solution is provided that realizes a large capacity, exhibits high storage characteristics and cycle characteristics, and is capable of inhibiting gas generation.
Abstract: The invention discloses therapeutic methods and uses of certain steroidal sapogenins, related compounds and derivatives thereof, in the treatment of non-cognitive neurodegeneration, non-cognitive neuromuscular degeneration, motor-sensory neurodegeneration or receptor dysfunction or loss in the absence of cognitive, neural and neuromuscular impairment.
Type:
Application
Filed:
April 12, 2011
Publication date:
August 4, 2011
Applicant:
PHYTOPHARM PLC
Inventors:
Daryl REES, Phil Gunning, Antonia Orsi, Zongqin Xia, Yaer Hu
Abstract: The invention provides smilagenin in novel amorphous, crystalline, hydrated and solvated forms, and the use thereof in manufacturing pharmaceutical or edible grade smilagenin and its derivatives.
Abstract: The present invention is based on the discovery that certain chemical compounds isolated from Chinese medicinal herbs are useful as anti-microbial agents, e.g., anti-bacterial agents, anti-fungal agents, and the like. In particular, the present invention provides compositions useful for treating microbial infections such as, for example, oral microbial infections, including periodontal disease and dental caries.
Type:
Grant
Filed:
March 4, 2004
Date of Patent:
January 25, 2011
Assignee:
The Regents of the University of California
Inventors:
Wenyuan Shi, Li Chen, Qing-yi Lu, David Heber, Maxwell H. Anderson
Abstract: A method to stereospecifically prepare a steroidal sapogenin or a derivative thereof by reducing a 3-keto,5?-H steroidal sapogenin with a hindered organoborane or an organo-aluminium hydride. A 3?-hydroxy,5?-H steroidal sapogenin or derivative thereof may be prepared by reducing the 3-keto,5?-H steroidal sapogenin using as reducing agent a relatively highly hindered organoborane reagent or by SN 2 inversion of a 3?-hydroxy,5?-H steroidal sapogenin or derivative thereof. The organo-aluminium hydride may be used to prepare a 3?,5?-H steroidal sapogenin or derivative thereof. The invention provides a convenient route to useful steroidal sapogenins such as sarsasapogenin, episarsasapogenin, smilagenin, epismilagenin and esters thereof, from readily available or easily preparable starting materials (e.g. diosgenone, preparable from diosgenin).
Type:
Grant
Filed:
April 28, 2003
Date of Patent:
May 18, 2010
Assignee:
Phytopharm PLC
Inventors:
Philip James Gunning, Peter David Tiffin
Abstract: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
Type:
Application
Filed:
April 20, 2009
Publication date:
February 25, 2010
Inventors:
Eric Anderson, Gary L. Bolton, Deborah A. Ferguson, Xin Jiang, Robert M. Kral, JR., Patrick M. O'Brien, Melean Visnick
Abstract: The invention provides sarsasapogenin in novel amorphous, crystalline, solvated and hydrated forms, and the use thereof in manufacturing pharmaceutical or edible grade sarsasapogenin and its derivatives.
Abstract: A process for the synthesis of peracyl-1-O-steroidal-.beta.-cellobiosides that provides excellent .beta.-anomeric selectivity without the use of a metal salt promoter. The process comprises reacting heptaacyl-.beta.-D-cellobiosyl-1-fluoride and a trisubstituted silyl-3-O-steroid, wherein the steroid is tigogenin, hecogenin, 11-ketotigogenin or diosgenin in the absence of a metal salt under suitable conditions.
Type:
Grant
Filed:
December 20, 1994
Date of Patent:
October 8, 1996
Assignee:
Pfizer Inc.
Inventors:
Kathleen D. Goggin, John F. Lambert, Stanley W. Walinsky
Abstract: Steroid compounds active on the cardiovascular system of formula ##STR1## wherein X, n, R, R.sub.1 and R.sub.2 have the meanings mentioned in the description are described.
Type:
Grant
Filed:
February 12, 1992
Date of Patent:
June 20, 1995
Assignee:
Zambon Group S.p.A.
Inventors:
Giorgio Bertolini, Cesare Casagrande, Stefania Montanari, Gabriele Norcini, Francesco Santangelo
Abstract: The present invention is directed toward a process for extracting compounds from plant material, comprisinga) contacting hydrolyzed plant material with a supercritical fluid and optionally with a co-solvent and p1 b) recovering the compound from the supercritical fluid.In another embodiment, the present invention is directed toward a process for removing a compound from plant material, comprising contacting the plant material with an acid, a supercritical fluid and a co-solvent, and recovering the compound from the supercritical fluid. The sterols, diosgenin and sarsapogenin, are efficiently extracted from barbasco root and Yucca seed, respectively.
Type:
Grant
Filed:
October 23, 1991
Date of Patent:
October 12, 1993
Assignee:
Schering Corporation
Inventors:
Michelle A. De Crosta, Peter Kabasakalian, Frederick J. F. Honold, Sr.
Abstract: The invention relates to new 11-arylsteroid compounds, having a strong antiprogestin and a weak or nonexistent antiglucocorticoid activity, to processes for preparing said compounds and also to pharmaceutical preparations which contain these derivatives as active constituent, characterized in that said steroids have the following formula: ##STR1## in which R.sub.1 is an aryl group with a ##STR2## group as substituent, X and Y each being separately H or a (1-4 C) hydrocarbyl group or together a (2-C) hydrocarbyl group which forms a 3- to 7-membered ring together with the nitrogen atom;R.sub.2 is hydrogen, hydroxyl, an acyloxy or an alkoxy group or a saturated or unsaturated hydrocarbyl group containing 1-8 carbon atoms, which hydrocarbyl group is provided with at least one hydroxyl, oxo, azido, cyano and/or halogen group;R.sub.3 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally substituted by a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.2 and R.sub.
Type:
Grant
Filed:
December 8, 1988
Date of Patent:
May 1, 1990
Assignee:
Akzo N.V.
Inventors:
Hendrick Paul de Jongh, Nicolaas P. van Vliet
Abstract: The present invention is concerned with 11-aryloestrane and 11-arylpregnane derivatives, characterized in that these derivatives have the following structure: ##STR1## wherein R.sub.1 is an aryl group with an ##STR2## group as substituent,X and Y each being separately H or a (1-4 C) hydrocarbon radical or together a (2-6 C) hydrocarbon radical;R.sub.2 is an alkyl group containing 1-4 carbon atoms;R.sub.3 is H, OH, a saturated or unsaturated hydrocarbon radical containing 1-8 carbon atoms, at least provided with a hydroxyl, oxo, halogen, azido or nitrile group; an acyloxy or an alkoxy group;R.sub.4 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally provided with a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.3 and R.sub.4 together form a ring system; andR.sub.5 is a hydrocarbon group containing 1-4 carbon atoms, and further with processes for the preparation of these compounds and with pharmaceutical preparations comprising these compounds.