WO1991012206A3 - Steroides inhibiteurs de l'aromatase - Google Patents

Steroides inhibiteurs de l'aromatase Download PDF

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Publication number
WO1991012206A3
WO1991012206A3 PCT/CA1991/000033 CA9100033W WO9112206A3 WO 1991012206 A3 WO1991012206 A3 WO 1991012206A3 CA 9100033 W CA9100033 W CA 9100033W WO 9112206 A3 WO9112206 A3 WO 9112206A3
Authority
WO
WIPO (PCT)
Prior art keywords
aromatase
compounds
inhibiting steroids
steroids
inhibiting
Prior art date
Application number
PCT/CA1991/000033
Other languages
English (en)
Other versions
WO1991012206A2 (fr
Inventor
Fernand Labrie
Yves Merand
Original Assignee
Endorecherche Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Endorecherche Inc filed Critical Endorecherche Inc
Publication of WO1991012206A2 publication Critical patent/WO1991012206A2/fr
Publication of WO1991012206A3 publication Critical patent/WO1991012206A3/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/003—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by oxygen as hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

De nouveaux inhibiteurs de l'aromatase sont utiles dans des préparations thérapeutiques de traitement de maladies provoquées par l'÷strogène. Ces composés sont des dérivés spécifiques d'androstanedione et d'androstènedione substitué en position α ayant un effet fortement inhibiteur de l'aromatase. L'invention concerne la synthèse de ces composés et des compositions pharmaceutiques les contenant.
PCT/CA1991/000033 1990-02-08 1991-02-04 Steroides inhibiteurs de l'aromatase WO1991012206A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US477,024 1990-02-08
US07/477,024 US5227375A (en) 1990-02-08 1990-02-08 Aromatase inhibitors

Publications (2)

Publication Number Publication Date
WO1991012206A2 WO1991012206A2 (fr) 1991-08-22
WO1991012206A3 true WO1991012206A3 (fr) 1991-11-28

Family

ID=23894189

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CA1991/000033 WO1991012206A2 (fr) 1990-02-08 1991-02-04 Steroides inhibiteurs de l'aromatase

Country Status (10)

Country Link
US (1) US5227375A (fr)
AU (1) AU7150991A (fr)
GR (1) GR910100067A (fr)
IE (1) IE65269B1 (fr)
IL (1) IL97122A (fr)
MY (1) MY105479A (fr)
NZ (1) NZ236966A (fr)
TW (1) TW221418B (fr)
WO (1) WO1991012206A2 (fr)
ZA (1) ZA91604B (fr)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR0180008B1 (ko) * 1991-03-28 1999-04-01 야마구찌 다까시 신규 옥사-또는 아자스테로이드 유체
ATE179179T1 (de) * 1992-09-30 1999-05-15 Teikoku Hormone Mfg Co Ltd 7-substituierte oxa-steroid verbindung
US6407082B1 (en) * 1996-09-13 2002-06-18 New Life Pharmaceuticals Inc. Prevention of ovarian cancer by administration of a vitamin D compound
US5593987A (en) * 1993-12-21 1997-01-14 Eli Lilly And Company Methods of inhibiting breast disorders
US6765002B2 (en) 2000-03-21 2004-07-20 Gustavo Rodriguez Prevention of ovarian cancer by administration of products that induce transforming growth factor-β and/or apoptosis in the ovarian epithelium
US6028064A (en) 1996-09-13 2000-02-22 New Life Pharmaceuticals Inc. Prevention of ovarian cancer by administration of progestin products
US6511970B1 (en) 1996-09-13 2003-01-28 New Life Pharmaceuticals Inc. Prevention of ovarian cancer by administration of products that induce transforming growth factor-beta and/or apoptosis in the ovarian epithelium
US6034074A (en) 1996-09-13 2000-03-07 New Life Pharmaceuticals Inc. Prevention of ovarian cancer by administration of a Vitamin D compound
AU8779898A (en) * 1997-08-11 1999-03-01 Weider Nutrition International, Inc. Compositions and treatments to reduce side effects of administration of androgenic testosterone precursors
BR9908592A (pt) 1998-03-11 2001-04-24 Endorech Inc Processo para inibir a atividade de 17ß-hidroxiesteróide desidrogenase tipo 5, composição farmacêutica, inibidor de 17ß-hidroxiesteróide desidrogenase tipo 5, processo para inibir 17ß-hidroxiesteróide desidrogenase tipo 3, inibidor de 17ß-hidroxiesteróide desidrogenase tipo 3, processos para tratar, ou reduzir o risco de desenvolver, câncer da próstata, hiperplasia prostática benigna, acne, seborréia, hirsutismo ou alopécia androgênica, sìndrome de ovário policìstico, câncer de mama, endometriose ou leiomioma, para inibir as secreções hormonais testiculares, para tratar puberdade precoce, e, kit
WO2001014406A1 (fr) * 1999-08-23 2001-03-01 Chugai Seiyaku Kabushiki Kaisha Agents anti-androgènes
US20010044431A1 (en) * 2000-03-21 2001-11-22 Rodriguez Gustavo C. Prevention of ovarian cancer by administration of products that induce biologic effects in the ovarian epithelium
CA2480151A1 (fr) * 2002-03-22 2003-10-09 Pharmacia Corporation Spirolactonisation c-17 et oxydation 6,7 de steroides
MXPA05004024A (es) * 2002-11-07 2005-06-08 Pharmacia & Upjohn Co Llc Procedimientos para preparar esteroides c-7 sustituidos.
US8183401B2 (en) * 2004-01-16 2012-05-22 Cedarburg Pharmaceuticals, Inc. Exemestane and its intermediates and methods of making the same
AU2011256088B2 (en) * 2010-05-20 2015-03-26 University Of Saskatchewan Use of aromatase inhibitors for synchronizing ovulation, inducing superovulation or double ovulation and improving twinning and fertility in a mammal
WO2014169395A1 (fr) 2013-04-19 2014-10-23 University Of Saskatchewan Dispositif intravaginal libérant un inhibiteur de l'aromatase

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2558088A1 (de) * 1975-12-19 1977-07-07 Schering Ag Verfahren zur herstellung von 4-androsten-3,17-dion-derivaten
US4596797A (en) * 1981-05-22 1986-06-24 Schering Aktiengesellschaft Use of aromatase-inhibitors for prophylaxis and/or treatment of benign prostatic hyperplasia
DE3612632A1 (de) * 1986-04-11 1987-10-22 Schering Ag Verfahren zur herstellung von 7(alpha)-propylsteroiden
US4822528A (en) * 1986-09-17 1989-04-18 Farmitalia Carlo Erba S.R.L. 4-substituted 6-alkylidenandrosteine-3,17-dione derivatives and process for their preparation
US4824830A (en) * 1986-07-14 1989-04-25 Farmitalia Carlo Erba S.R.L. 6- or 7-methylenandrosta-1,4-diene-3,17-dione derivatives and process for their preparation

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL125069C (fr) * 1963-12-24
US3380886A (en) * 1965-04-07 1968-04-30 Upjohn Co 7alpha-methyl-3beta-hydroxy-5-androstenes
US3591607A (en) * 1966-04-19 1971-07-06 Hoffmann La Roche Retrosteroid a-ring formation
US3766213A (en) * 1966-04-19 1973-10-16 Hoffmann La Roche Retrosteroid a ring formation
US3485828A (en) * 1967-04-10 1969-12-23 Syntex Corp 6,7-ethylene and 6,7-substituted ethylene derivatives of the pregnane series
US3952018A (en) * 1972-01-14 1976-04-20 Hoffmann-La Roche Inc. 15-Oxasteroids
US4451404A (en) * 1983-02-09 1984-05-29 The Upjohn Company 16β-Methyl steroid process
US4596796A (en) * 1983-09-12 1986-06-24 Sumitomo Chemical Company, Limited Dithiolphosphoric acid ester as a soil pesticide

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2558088A1 (de) * 1975-12-19 1977-07-07 Schering Ag Verfahren zur herstellung von 4-androsten-3,17-dion-derivaten
US4596797A (en) * 1981-05-22 1986-06-24 Schering Aktiengesellschaft Use of aromatase-inhibitors for prophylaxis and/or treatment of benign prostatic hyperplasia
DE3612632A1 (de) * 1986-04-11 1987-10-22 Schering Ag Verfahren zur herstellung von 7(alpha)-propylsteroiden
US4824830A (en) * 1986-07-14 1989-04-25 Farmitalia Carlo Erba S.R.L. 6- or 7-methylenandrosta-1,4-diene-3,17-dione derivatives and process for their preparation
US4822528A (en) * 1986-09-17 1989-04-18 Farmitalia Carlo Erba S.R.L. 4-substituted 6-alkylidenandrosteine-3,17-dione derivatives and process for their preparation

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Proceedings/Annual meeting of the American association for cancer research, vol. 30, March, 1989,page 303, col. 1206, "Endocrinology". *
Steroids, Vol. 40, No. 6, December 1982 Alan J. Solo et al.: "7 -alkyltestosterone derivatives: synthesis and activity as androgens and as aromatase inhibitors ", *

Also Published As

Publication number Publication date
ZA91604B (en) 1992-09-30
WO1991012206A2 (fr) 1991-08-22
IE910263A1 (en) 1991-08-14
IL97122A0 (en) 1992-05-25
GR910100067A (el) 1992-06-30
AU7150991A (en) 1991-09-03
US5227375A (en) 1993-07-13
MY105479A (en) 1994-10-31
IE65269B1 (en) 1995-10-18
IL97122A (en) 1996-06-18
TW221418B (fr) 1994-03-01
NZ236966A (en) 1993-11-25

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