ECSP013947A - Compuestos estrogénicos - Google Patents

Compuestos estrogénicos

Info

Publication number
ECSP013947A
ECSP013947A EC2001003947A ECSP013947A ECSP013947A EC SP013947 A ECSP013947 A EC SP013947A EC 2001003947 A EC2001003947 A EC 2001003947A EC SP013947 A ECSP013947 A EC SP013947A EC SP013947 A ECSP013947 A EC SP013947A
Authority
EC
Ecuador
Prior art keywords
alkyl
alkynyl
acyl
alkenyl
halogen
Prior art date
Application number
EC2001003947A
Other languages
English (en)
Inventor
Hubert Jan Jozef Loozen
Gerrit Herman Veeneman
Wilhelmus Gerardus Eduardus Joseph Schoonen
Original Assignee
Akzo Nobel Nv
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 Akzo Nobel Nv filed Critical Akzo Nobel Nv
Publication of ECSP013947A publication Critical patent/ECSP013947A/es

Links

Classifications

    • 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
    • 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
    • C07J1/0051—Estrane derivatives
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens
    • 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
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • 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
    • C07J1/0051—Estrane derivatives
    • C07J1/0081—Substituted in position 17 alfa and 17 beta
    • C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
    • C07J1/0096—Alkynyl derivatives
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presentación es novedosa, una clase de estrógenos selectivos que tiene un esqueleto esteroide con un anillo A no aromático u un grupo hidróxilo libre o extremo en el átomo de carbono No. 3. Los estrógenos satisfacen la fórmula general I, en la cual R1 es H, (C1-C3)alquilo o (C2-C3)acilo; R2 es Hm a-(C1-C4)alquilo, a-(C2-C4)alquenilo o (C2-C4)alquinilo; R3 es H o (C1-C4)alquilo, (C2-C4)alquenilo o (C2-C4)alquinilo, cada uno en la ubicación 15 o 16 del esqueleto, del esteroide; R4 es H o (C1-C5)alquilo, (C2-C5) alquelino o (C2-C5)alquinilo, cada uno opcionalmente sustituido por un halógeno; de preferencia etinilo; R5 es H, (C1-C3)alquilo o (C2-C3)acilo; R6 es (C1-C5)alquilo, (C2-C5)aquenilo, (C2-C5)alquinilo o (C1-C5) alquiloideno, cada uno opcionalmente sustituido por un halógeno o (C1-C3)alquiloxy; Los enlaces punteados representan enlaces dobles opcionales.
EC2001003947A 1999-09-06 2001-02-22 Compuestos estrogénicos ECSP013947A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP99202900 1999-09-06
PCT/EP2000/008406 WO2001018027A1 (en) 1999-09-06 2000-08-28 Non-aromatic estrogenic steroids with a hydrocarbon substituent in position 11

Publications (1)

Publication Number Publication Date
ECSP013947A true ECSP013947A (es) 2002-09-27

Family

ID=8240610

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2001003947A ECSP013947A (es) 1999-09-06 2001-02-22 Compuestos estrogénicos

Country Status (24)

Country Link
US (1) US6677329B1 (es)
EP (1) EP1224204B1 (es)
JP (1) JP2003508541A (es)
KR (1) KR20020092907A (es)
CN (2) CN1185249C (es)
AT (1) ATE295851T1 (es)
AU (1) AU770331B2 (es)
BR (1) BR0013769A (es)
CA (1) CA2382489C (es)
CZ (1) CZ2002831A3 (es)
DE (1) DE60020260T2 (es)
EC (1) ECSP013947A (es)
ES (1) ES2241657T3 (es)
HU (1) HUP0202595A3 (es)
IL (2) IL148116A0 (es)
MX (1) MXPA02001831A (es)
NO (1) NO20021079L (es)
NZ (1) NZ517281A (es)
PL (1) PL353826A1 (es)
RU (1) RU2245886C2 (es)
SK (1) SK3282002A3 (es)
TR (1) TR200200575T2 (es)
WO (1) WO2001018027A1 (es)
ZA (1) ZA200201250B (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2204613T3 (es) * 1999-04-06 2004-05-01 Akzo Nobel N.V. Androgenos 7-alfa alquilo oralmente activos.
IL148116A0 (en) * 1999-09-06 2002-09-12 Akzo Nobel Nv Non-aromatic estrogenic steroids with a hydrocarbon substituent in position 11
WO2001098322A1 (en) * 2000-06-22 2001-12-27 Northeastern University Novel steroidal antiestrogens and antiandrogens and uses thereof
US8173628B2 (en) * 2000-06-22 2012-05-08 Northeastern University Steroidal antiestrogens and antiandrogens and uses thereof
BR0112791A (pt) * 2000-07-28 2003-06-24 Akzo Nobel Nv Composto esteroidal 16alfa-substituido, uso do mesmo, métodos de tratamento para ativação seletiva de receptores de estrogênio do subtipo alfa, e para terapia de reposição hormonal ou contracepção, e, composição farmacêutica
UA89964C2 (ru) 2004-09-08 2010-03-25 Н.В. Органон 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ
HUE055367T2 (hu) * 2016-03-03 2021-11-29 Crystal Pharma Sau Eljárás új intermedierek 11-metilén-szteroidok elõállítására
CN114249789B (zh) * 2020-09-23 2023-06-02 湖南普尔生物医药有限公司 一种7α-甲基-3,3-二甲氧基-5(10)-雄烯-17-酮的制备方法
CN114409717B (zh) * 2021-12-17 2023-03-17 湖南科益新生物医药有限公司 替勃龙中间体醚化物和替勃龙的制备方法
CN114230627B (zh) * 2021-12-31 2023-09-15 湖南新合新生物医药有限公司 一种倍他米松环氧水解物中间体的制备方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3092645A (en) 1961-12-28 1963-06-04 Searle & Co Esters of 17alpha-alkynylester-5(10)-ene-3beta, 17beta-diols
GB1112840A (en) 1964-04-07 1968-05-08 Res Inst Medicine Chem Steroids having pro-oestrogenic activity
US3465010A (en) * 1966-11-22 1969-09-02 Searle & Co 17 - (unsaturated hydrocarbon - substituted) 11,13beta - dialkylgon -4 - ene - 3,17beta-diols and esters thereof
US3377366A (en) 1966-12-02 1968-04-09 Searle & Co 17alpha-alkynyl/alkenyl-11, 13beta-dialkylgon-5(10)-en-3-ones and esters thereof
US3652606A (en) 1970-08-07 1972-03-28 Searle & Co 3-oxygenated 11beta-methylestr-4-en-17beta-ol and esters thereof
AU572589B2 (en) * 1983-12-14 1988-05-12 Upjohn Company, The 11(alpha)-difluoromethyl and (e)-and (z)-11-fluoromethylene steroids
ZA94715B (en) * 1993-02-08 1994-10-24 Akzo Nv Steroids for treating menopausal complaints
ATE180669T1 (de) * 1993-03-05 1999-06-15 Akzo Nobel Nv Verwendung von pregnanderivaten zur behandlung von tumoren
KR20010041698A (ko) 1998-03-09 2001-05-25 악조 노벨 엔.브이. 신규 피임 키트
IL148116A0 (en) * 1999-09-06 2002-09-12 Akzo Nobel Nv Non-aromatic estrogenic steroids with a hydrocarbon substituent in position 11

Also Published As

Publication number Publication date
DE60020260D1 (de) 2005-06-23
CZ2002831A3 (cs) 2002-05-15
CN1185249C (zh) 2005-01-19
NZ517281A (en) 2003-09-26
RU2245886C2 (ru) 2005-02-10
ATE295851T1 (de) 2005-06-15
DE60020260T2 (de) 2006-01-19
KR20020092907A (ko) 2002-12-12
NO20021079L (no) 2002-04-29
AU770331B2 (en) 2004-02-19
ZA200201250B (en) 2003-07-30
WO2001018027A1 (en) 2001-03-15
BR0013769A (pt) 2002-04-30
CA2382489A1 (en) 2001-03-15
IL148116A (en) 2006-10-31
CA2382489C (en) 2008-03-11
IL148116A0 (en) 2002-09-12
NO20021079D0 (no) 2002-03-05
EP1224204A1 (en) 2002-07-24
EP1224204B1 (en) 2005-05-18
CN1637016A (zh) 2005-07-13
PL353826A1 (en) 2003-12-01
US6677329B1 (en) 2004-01-13
CN1372565A (zh) 2002-10-02
AU7511700A (en) 2001-04-10
HUP0202595A2 (hu) 2002-12-28
MXPA02001831A (es) 2002-10-23
CN100354299C (zh) 2007-12-12
TR200200575T2 (tr) 2002-06-21
ES2241657T3 (es) 2005-11-01
HUP0202595A3 (en) 2004-06-28
JP2003508541A (ja) 2003-03-04
SK3282002A3 (en) 2002-06-04

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