Abstract: The present invention involves intermediates, including a 7?-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.
Abstract: Methods of using 7?,11?-dimethyl-17?-hydroxyestra-4,14-dien-3-one (III) and 17 esters thereof for various hormonal therapies, oral and parenteral dosage forms comprising these actives, and processes for their preparation.
Type:
Grant
Filed:
October 28, 2002
Date of Patent:
March 27, 2007
Assignee:
The United States of America as represented by the Department of Health and Human Services
Inventors:
Richard P. Blye, Hyun K. Kim, Pemmaraju Narasimha Rao, Carmie Kirk Acosta
Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: wherein the variables are defined in the specification.
Type:
Grant
Filed:
August 24, 2001
Date of Patent:
November 14, 2006
Assignee:
Entremed, Inc.
Inventors:
Gregory E. Agoston, Jamshed H. Shah, Kimberly A. Hunsucker, Victor S. Pribluda, Theresa M. LaVallee, Shawn J. Green, Christopher J. Herbstritt, Xiaoguo H. Zhan, Anthony M. Treston
Abstract: This invention relates to novel oxathiinecarboxamides of the formula (I) in which R, R1 and m are as defined in the disclosure, to a plurality of processes for preparing these substances and to their use for controlling unwanted micro-organisms.
Abstract: The invention relates to vitamin D derivatives of general formula I, process for their production, intermediate products of the process as well as the use for the production of pharmaceutical agents.
Type:
Grant
Filed:
November 26, 2002
Date of Patent:
October 3, 2006
Assignee:
Schering AG
Inventors:
Andreas Steinmeyer, Katica Schwarz, Claudia Giesen, Martin Haberey, Marianne Fähnrich
Abstract: The invention relates to insecticidal mixtures comprising the compound of the formula (I) and at least one further known active compound selected from the group consisting of abamectin, emamectin or emamectin benzoate, methiocarb, ?-cyfluthrin and lambda-cyhalothrin, and to the use of these mixtures for protecting plants against attack by pests.
Type:
Grant
Filed:
January 20, 2003
Date of Patent:
August 29, 2006
Assignee:
Bayer Cropscience AG
Inventors:
Wolfram Andersch, Angelika Lubos-Erdelen, legal representative, Peter Jeschke, Christoph Erdelen, deceased
Abstract: This invention provides a novel class of vitamin D related compounds, namely, the 2-alkylidene-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula: where Y1 and Y2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R6 and R8, which may be the same or different, are each selected from hydrogen, alkyl, hydroxyalkyl and fluoroalkyl, or when taken together represent the group —(CH2)x— where x is an integer from 2 to 5, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds are characterized by relatively high intestinal calcium transport activity and relatively high bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of diseases where bone formation is desired, particularly low bone turnover osteoporosis.
Abstract: The present invention relates to the use of substituted aryl- and heteroarylpropargylamines of the formula (I) where a) R1 is heteroaryl or aryl, unsubstituted or mono- or polysubstituted by identical or different radicals, b) A is a group CR4R5 or C?O, where R4 is hydrogen, halogen or alkyl; R5 is hydrogen, halogen or a substituted or unsubstituted hydrocarbon radical; c) R2 and R3 together with the nitrogen atom to which they are attached form N-heteroaryl or N-heterocyclyl, unsubstituted or mono- or polysubstituted by identical or different radicals, if appropriate also as N-oxide or salt, as pesticide against arthropods and helminths for protecting plants and animals.
Type:
Grant
Filed:
August 22, 2002
Date of Patent:
August 1, 2006
Assignee:
Bayer Cropscience S.A.
Inventors:
Harald Jakobi, Susan Mary Cramp, Joachim Dickhaut, Stephen Lindell, Jörg Tiebes, Maria Asuncion Canales, Daniela Jans, Waltraud Hempel, Reed Nathan Royalty, Susan Marie McComb, Maria-Theresia Thönessen, Jutta Maria Waibel, Vincent Lee Salgado
Abstract: Fungicidal mixtures, comprising A) the compound of the formula I and B) the compound of the formula II in a synergistically effective amount, methods for controlling harmful fungi using mixtures of the compounds I and II and the use of the compounds I and II for preparing such mixtures are described.
Type:
Grant
Filed:
June 30, 2003
Date of Patent:
July 11, 2006
Assignee:
BASF Aktiengesellschaft
Inventors:
Eberhard Ammermann, Reinhard Stierl, Ulrich Schöfl, Klaus Schelberger, Maria Scherer, Michael Henningsen, Randall Even Gold
Abstract: The invention relates to a reducing composition for the permanent deformation of the hair comprising an N-substituted formamidinesulphinic acid derivative as reducing agent and to a process for the permanent deformation of the hair employing this reducing composition.
Type:
Grant
Filed:
November 17, 2000
Date of Patent:
July 4, 2006
Inventors:
Nathalie Garnier, Gérard Malle, Henri Samain
Abstract: This invention discloses (20S)-1?-hydroxy-2?-methyl-19-nor-vitamin D3 and (20S)-1?-hydroxy-2?-methyl-19-nor-vitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.
Type:
Grant
Filed:
January 22, 2004
Date of Patent:
June 20, 2006
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Hector F. DeLuca, Rafal R. Sicinski, Pawel K. Grzywacz
Abstract: A treatment for obesity and overweight comprises administering a vitamin D analog. The analog effectively inhibits an increase in body fat to animals at risk and decreases the basal fat content of animals. The treatment has a positive effect on the lean body component such that while there is an overall decrease in body weight, there is also a decrease in percent body fat. This decrease can be proportionally greater than the overall decrease in body weight. In addition, the treatment has a positive effect on bone turnover and osteogenesis making the vitamin D analog a beneficial treatment for the symptoms of menopause. Various exemplary embodiments of the treatment use the 2-alkylidene derivatives of vitamin D3, such as the 2-alkylidene-19-nor derivatives in both the R and S configurations at carbon-20.
Type:
Grant
Filed:
November 24, 2004
Date of Patent:
May 30, 2006
Inventors:
Hector F. DeLuca, Lori A. Plum, Hau Zhe Ke, Thomas A. Brown
Abstract: The present invention is related to novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues, their use as antiglucocorticoids for the treatment and/or prophylaxis of disease associated to an excess of glucocorticoids. In particular, the invention relates to the use of novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues for treating Cushing's syndrome, iatrogenic hypercortisolism or depression. Also the present invention is related to methods of preparing the novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues.
Type:
Grant
Filed:
September 17, 2001
Date of Patent:
May 30, 2006
Assignee:
Applied Research Systems ARS Holding N.V.
Inventors:
Gerardo Burton, Carlos P. Lantos, Adriana Silvia Veleiro
Abstract: Disclosed are improved pharmaceutical formulations comprising dehydroepiandrosterone (DHEA), enriched in selected polymorphic forms, for therapeutic applications. In one embodiment, the formulation comprises, in solid form, DHEA, at least 85% of which is present as a single polymorph selected from the form I polymorph or the form II polymorph, and at least one pharmaceutical excipient. Methods for making and using such compositions are also disclosed.
Type:
Grant
Filed:
March 16, 2000
Date of Patent:
May 16, 2006
Assignee:
Genelabs Technologies, Inc.
Inventors:
Jagdish Parasrampuria, Maxine B. Yonker, Kenneth E. Schwartz, Marc J. Gurwith
Abstract: An estrogen/antiestrogen-porphyrin conjugate, their composition and methods for their use are claimed. The active compounds of the invention are conjugates consisting of an estrogen or anti estrogen portion, tether or linker portion and a porphyrin portion. The method of invention exploits an active process that involves strong and specific interactions between nuclear receptor and its cognate ligand.
Type:
Grant
Filed:
April 12, 2001
Date of Patent:
May 2, 2006
Assignee:
The Trustees of Boston University
Inventors:
Rahul Ray, Scott C. Mohr, Narasimha Swamy
Abstract: The invention relates to a composition useful for the breaking of rest in deciduous fruit species such as apple species and grape species comprising an organic nitrogen-containing compound having a molecular weight of 60 to 300 with the exception of urea and dinitro-ortho-cresol, an inorganic nitrate rest-breaking agent, and a surfactant. Preferably, the organic nitrogen-containing compound is a choline salt such as choline chloride, the inorganic nitrate rest-breaking agent is selected from the group consisting of potassium nitrate, calcium nitrate, ammonium nitrate, calcium ammonium nitrate, urea ammonium nitrate, zinc ammonium nitrate, and mixtures thereof, and the surfactant is an alkoxylated amine such as Armoblen ®*, and Berol®* compound or an alkoxylated quaternary ammonium compound.
Abstract: This invention concerns new biocidal compounds of formula (I) wherein R is H or CH3. Of particular interest are two isomers that are named malayamycin A and desmethylmalayamycin A. These isomers, which may be prepared by growing under controlled conditions a previously unknown strain of micro-organism from the species Streptomyces malaysiensis, are characterised by nmr and mass spectroscopic data. They have biocidal activity, including anti-fungal, anti-viral and anti-cancer activity, and are of special interest for use in agriculture, horticulture, animal and human health.
Type:
Grant
Filed:
January 10, 2003
Date of Patent:
April 11, 2006
Assignee:
Syngenta Crop Protection, Inc.
Inventors:
Jill Patricia Benner, Bettina Gertrud Henriette Boehlendorf, Martin Richard Kipps, Nicolas Eugene Paul Lambert, Riet Luck, Louis-Pierre Molleyres, Snezana Neff, Traugott Christoph Schuez, Paul David Stanley