Abstract: A process ethynylates 16-methylene-17-keto steroids to the corresponding 16-methylene-17?-ethynyl-17?-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the preparation of several pharmaceutically active agents, such as e.g. Nestorone® or melengestrol acetate.
Type:
Grant
Filed:
December 19, 2012
Date of Patent:
March 29, 2016
Assignees:
Crystal Pharma, S.A.U., Population Council Inc.
Inventors:
Luis Gerardo Gutiérrez Fuentes, Celso Miguel Sandoval Rodriguez
Abstract: A process ethynylates 16-methylene-17-keto steroids to the corresponding 16-methylene-17?-ethynyl-17?-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the preparation of several pharmaceutically active agents, such as e.g. Nestorone® or melengestrol acetate.
Type:
Application
Filed:
December 19, 2012
Publication date:
January 1, 2015
Applicants:
CRYSTAL PHARMA, S.A.U., THE POPULATION COUNCIL INC.
Inventors:
Luis Gerardo Gutiérrez Fuentes, Celso Miguel Sandoval Rodríguez
Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect peptidyl-dipeptidase A; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a peptidyl-dipeptidase A in a reaction system in which the peptidyl-dipeptidase A contacts with a test substance, and the like.
Type:
Application
Filed:
June 23, 2006
Publication date:
October 11, 2012
Applicant:
SUMITOMO CHEMICAL COMPANY, LIMITED
Inventors:
Yasutaka Shimokawatoko, Marc Van De Craen, Irene Nooren, Sandra Turconi, Yann Naudet, Guy Nys, Jurgen Debaveye
Abstract: The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.
Abstract: Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.
Type:
Grant
Filed:
December 24, 1997
Date of Patent:
April 25, 2000
Assignee:
SRI International
Inventors:
Masato Tanabe, Richard H. Peters, Wan-Ru Chao, Ling Jong
Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
Type:
Grant
Filed:
January 28, 1999
Date of Patent:
November 16, 1999
Assignee:
Schering AG
Inventors:
Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Kunzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
Abstract: The invention provides new androstene derivatives having anti-inflammatory activity, pharmaceutical compositions containing them, and methods of administering them to warm-blooded animals in the treatment of inflammation. The active compounds are alkyl 17.alpha.-dichloroacetoxy-11.beta.-hydroxyandrosta-1,4-dien-3-one-17.beta. -carboxylates and related androstenes.
Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
Type:
Grant
Filed:
August 20, 1997
Date of Patent:
February 2, 1999
Assignee:
Schering AG
Inventors:
Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Kunzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
Abstract: Non-linear optical materials using a 16-benzalandrosta-1,4-diene-3,17-dione compound represented by the formula [I] ##STR1## wherein R is hydrogen, alkyl or other specified substituents, have a high non-linear optical constant, and can provide a non-linear optical device having excellent properties.
Abstract: A method for decreasing the adrenal secretion of glucocorticoids, especially cortisol, in male livestock without substantially suppressing the animal's immune system by oral or other administration of effective doses of melengesterol acetate (MGA) or derivatives thereof. Ideally, the MGA may be used in admixture with the subject animal feed, although it is understood that the compound may be administered separately.
Type:
Grant
Filed:
March 29, 1991
Date of Patent:
October 12, 1993
Assignee:
The United States of America as represented by the Secretary of Agriculture
Abstract: Novel compounds for the inhibition of sex steroid activity for the treatment of both androgen-related and estrogen-related diseases include for example 15- and 16-halo substituted compounds such as: ##STR1## The compounds are characterized by an estrogenic nucleus substituted with a substituent of the formula --R.sup.1 [B--R.sup.2 --].sub.x L--G whereinat least one of L and G is a polar moiety distanced from a ring carbon of the estrogenic nucleus by a least three intervening atoms:x is an integer from 0-6;R.sup.1 and R.sup.2 are independently either absent or selected from the group consisting of straight- or branched-chain alkylene, straight- or branched-chain alkynylene, straight- or branched-chain alkenylene, phenylene, and fluoro-substituted analogs of the foregoing; andB is either absent or selected from the group consisting of --O--, --Se--, --SO--, --SO.sub.2 --, --NR.sup.3 --, --SiR.sup.3.sub.2, --CR.sup.3 OR.sup.3 --, NR.sup.3 CO--, NR.sup.3 CS--, --CONR.sup.3 --, CSNR.sup.
Abstract: New 9.alpha.-hydroxy-17-methylene steroids are prepared by the introduction of a substituted 17-methylene group in 9.alpha.-hydroxyandrost-4-ene-3, 17-dione.The resulting compounds are useful starting compounds in the synthesis of corticosteroids.
Abstract: Compounds of the formula: ##STR1## are useful as anti-cancer, anti-obesity, anti-diabetic, anti-coronary agents, anti-aging agents, anti-hypolipidemic agents and anti-autoimmune agents.