Abstract: This invention discloses 2-methylene-19,26,27-trinor-(20S)-vitamin D analogs, and specifically 2-methylene-19,26,27-trinor-(20S)-1?-hydroxyvitamin D3 and pharmaceutical uses therefor. This compound exhibits 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. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
Type:
Grant
Filed:
July 9, 2007
Date of Patent:
May 11, 2010
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Hector F. DeLuca, Lori A. Plum, Pawel K. Grzywacz, Margaret Clagett-Dame
Abstract: This invention discloses 2-methylene-19-nor-17-ene vitamin D analogs, and specifically 2-methylene-19-nor-1?-hydroxy-17-ene-homopregnacalciferol and pharmaceutical uses therefor. This compound exhibits 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. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders and inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
Type:
Grant
Filed:
July 9, 2007
Date of Patent:
April 27, 2010
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
Abstract: Compounds of formula I are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
Type:
Grant
Filed:
April 6, 2007
Date of Patent:
April 27, 2010
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki
Abstract: The present invention provides a pyrazole derivative of the general formula (1), which has an excellent efficacy as an active component for a herbicide, an intermediate for the production thereof, processes for the production thereof, and a herbicide containing the derivative as an active ingredient.
Type:
Grant
Filed:
February 19, 2002
Date of Patent:
April 20, 2010
Assignees:
Sagami Chemical Research Center, Kaken Pharmaceutical Co., Ltd.
Abstract: Novel vitamin D analogs, markedly active in the fields of cell proliferation and differentiation, are selected from among (4E,6E)-7-{3-[2-(3,4-bis-hydroxymethylphenyl)-ethyl]phenyl}-3-ethylnona-4,6-dien-3-ol, (E)-6-[3-(3,4-bis-hydroxymethylbenzyloxy)phenyl]1,1,1-trifluoro-2-trifluoromethyloct-5-en-3-yn-2-ol, (3E,5E)-6-[3-(3,4-bis-hydroxymethylbenzyloxy)-phenyl]-1,1,1-trifluoro-2-trifluoromethylocta-3,5-dien-2-ol, (E)-6-{3-[2-(3,4-bis-hydroxymethylphenyl)ethyl]phenyl}-1,1,1-trifluoro-2-trifluoromethyloct-5-en-3-yn-2-ol, and (3E,5E)-6-{3-[2-(3,4-bis-hydroxymethylphenyl)-ethyl]phenyl-1,1,1-trifluoro-2-trifluoromethylocta-3,5-dien-2-ol, and the geometric isomers thereof and these compounds in which one or more of the hydroxyl functions are protected by a protective group —(C?O)—R, in which R is a linear or branched alkyl radical having from 1 to 6 carbon atoms, an aryl radical having from 6 to 10 carbon atoms, or an aralkyl radical having from 7 to 11 carbon atoms, the aryl radical or the aralkyl radical optional
Abstract: The invention relates to novel substituted benzoylcyclohexenones of the formula (I) in which Q, R1, R2, R3, R4, R5, Y and Z have one of the meanings given in the disclosure, to processes for their preparation, and to their use.
Type:
Grant
Filed:
May 3, 2002
Date of Patent:
March 2, 2010
Assignee:
Bayer CropScience AG
Inventors:
Hans-Georg Schwarz, Klaus-Helmut Muller, Stefan Herrmann, Dorothee Hoischen, Kristian Kather, Stefan Lehr, Otto Schallner, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen, Shinichi Narabu, Akihiko Yanagi, Shinichi Shirakura, Toshio Goto, Yoshihiro Yamaguchi
Abstract: The invention relates to a method of preparing urethane-protected N-carboxyanhydrides of alpha amino acids. The inventive method enables the synthesis of urethane-protected N-carboxyanhydrides of alpha amino acids in the presence of a catalytic quantity of triethylene diamine without the addition of a tertiary amine-type base.
Type:
Grant
Filed:
August 17, 2004
Date of Patent:
February 23, 2010
Assignee:
ISOCHEM
Inventors:
Hervé Lhermitte, Julien Grima, Antoine Paris
Abstract: Compounds of the formula in which A is an unsubstituted or mono- to tetrasubstituted, aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, where one to two of the substituents of A can be selected from the group consisting of halo-C1-C3alkyl, cyclopropyl, halocyclopropyl, C2-C3alkenyl, C2-C3alkynyl, halo-C2-C3alkenyl, halo-C2-C3alkynyl, halo-C1-C3alkoxy, C1-C3alkylthio, halo-C1-C3alkylthio, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro, and one to four of the substituents of A can be selected from the group consisting of C1-C3alkyl, C1-C3alkoxy and halogen; R is hydrogen, C1-C6alkyl, phenyl-C1-C4alkyl, C3-C6cycloalkyl, C2-C6alkenyl or C2-C6alkynyl; and X is N—NO2 or N—CN, and, if appropriate, tautomers thereof, in each case in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
Abstract: Pharmaceutical compositions containing organic compounds or salts thereof that serve as modulators for the SDF-1 or I-TAC chemokines are disclosed. The compounds and compositions are useful in the treatment of cancer, especially in the inhibition of cancer proliferation, growth, and metastasis. Methods of interfering with SDF-1 and/or I-TAC binding to the CCXCKR2 receptor and treating cancer using the compounds and pharmaceutical compositions of the present invention are also disclosed.
Type:
Grant
Filed:
December 22, 2003
Date of Patent:
January 19, 2010
Assignee:
Chemocentryx, Inc.
Inventors:
Anita Melikian, Jennifer Burns, Brian E. McMaster, Thomas Schall, J. J. Wright
Abstract: 19-nor-vitamin D analogs having an additional dihydrofuran ring connecting the 3?-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit selective in vitro and in vivo activities, making them therapeutic agents for the treatment or prophylaxis of autoimmune diseases, some types of cancers, metabolic bone diseases, osteomalacia, osteopenia, secondary hyperparathyroidism, psoriasis, or other skin diseases.
Type:
Grant
Filed:
July 10, 2008
Date of Patent:
January 19, 2010
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Hector F. DeLuca, Agnieszka Glebocka, Katarzyna Sokolowska, Rafal R. Sicinski, Lori A. Plum, Margaret Clagett-Dame
Abstract: Compounds of formula I are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
Type:
Grant
Filed:
April 6, 2007
Date of Patent:
January 19, 2010
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki
Abstract: Compounds of formula I are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
Type:
Grant
Filed:
April 6, 2007
Date of Patent:
January 19, 2010
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki
Abstract: The present invention relates to a cosmetic process for treating wrinkled skin, in particular the skin of the face and/or of the forehead, through a dermo-decontracting effect, comprising the topical application to said skin of a composition comprising, in a physiologically acceptable medium, at least one piperidine derivative chosen from the compounds of formula (I). These compounds make it possible to combat expression wrinkles according to a mechanism of dermo-decontraction.
Abstract: Methods and kits for lanthionizing keratin fibers to achieve relaxation of the keratin fibers, and methods and kits for re-waving keratin fibers comprising applying to keratin fibers a pretreatment composition comprising at least one reducing agent chosen from thiols, sulfites, and derivatives thereof, applying to the pretreated keratin fibers a composition comprising at least one hydroxide compound, and heating the keratin fibers.
Abstract: A process for the preparation of [1,4,5]-oxadiazepine derivatives by reaction of N,N?-diacyl-hydrazines with 2,2?-disubstituted diethyl ethers to form 4,5-diacyl-[1,4,5]-oxadiazepines and reaction of the latter compounds with a hydrohalic acid.
Abstract: A composition of matter is disclosed that comprises a compound of the formula: wherein R1 is selected from the group consisting of unsubstituted and substituted biphenyl moieties, unsubstituted and substituted fluorenyl moieties, unsubstituted and substituted carbazolyl moieties, and unsubstituted and substituted pyridyl moieties; and R2 is hydrogen or alkyl. The compositions are useful as insecticides, acaricides, and fungicides.
Type:
Grant
Filed:
March 3, 2005
Date of Patent:
September 22, 2009
Assignee:
Crompton Corporation
Inventors:
Mark A. Dekeyser, Sheldon B. Park, Paul T. McDonald
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:
May 6, 2005
Date of Patent:
January 20, 2009
Assignee:
Laboratoires Serono SA
Inventors:
Gerardo Burton, Carlos P. Lantos, Adriana Silvia Veleiro
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: The present invention involves intermediates, including a 7?-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent.
Abstract: A process for producing a monoalkylation aromatic product, such as ethylbenzene and cumene, utilizing an alkylation reactor zone and a transalkylation zone in series or a combined alkylation and transkylation reactor zone.