The Carbon Is Double Bonded Directly At The 16-position Patents (Class 552/528)
  • Patent number: 9296780
    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
  • Publication number: 20150005518
    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
  • Publication number: 20120258929
    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
  • Publication number: 20110098260
    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.
    Type: Application
    Filed: December 1, 2010
    Publication date: April 28, 2011
    Applicant: Harbor BioSciences, Inc.
    Inventor: James M. Frincke
  • Patent number: 6054446
    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
  • Patent number: 5986115
    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
  • Patent number: 5981517
    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.
    Type: Grant
    Filed: April 24, 1997
    Date of Patent: November 9, 1999
    Assignee: Soft Drugs, Inc.
    Inventor: Nicholas S. Bodor
  • Patent number: 5866560
    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
  • Patent number: 5262090
    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.
    Type: Grant
    Filed: March 4, 1992
    Date of Patent: November 16, 1993
    Assignee: Hitachi Chemical Company, Ltd.
    Inventor: Makoto Kaji
  • Patent number: 5252564
    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
    Inventor: Michael T. Zavy
  • Patent number: 5204337
    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.
    Type: Grant
    Filed: July 21, 1992
    Date of Patent: April 20, 1993
    Assignee: Endorecherche Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5194602
    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.
    Type: Grant
    Filed: December 12, 1990
    Date of Patent: March 16, 1993
    Assignee: Gist-Brocades N.V.
    Inventors: Jacobus N. M. Batisi, Arthur F. Marx
  • Patent number: 5001119
    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.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: March 19, 1991
    Inventors: Arthur G. Schwartz, Marvin L. Lewbart