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BR0013769A - Esteróides estrogênicos não aromáticos, composição farmacêutica, e, uso de um composto esteróide - Google Patents

Esteróides estrogênicos não aromáticos, composição farmacêutica, e, uso de um composto esteróide

Info

Publication number
BR0013769A
BR0013769A BR0013769-3A BR0013769A BR0013769A BR 0013769 A BR0013769 A BR 0013769A BR 0013769 A BR0013769 A BR 0013769A BR 0013769 A BR0013769 A BR 0013769A
Authority
BR
Brazil
Prior art keywords
alkyl
alkynyl
alkenyl
aromatic
pharmaceutical composition
Prior art date
Application number
BR0013769-3A
Other languages
English (en)
Inventor
Hubert Jan Jozef Loozen
Gerrit Herman Veeneman
Wilhelmus Gerardus Ed 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 BR0013769A publication Critical patent/BR0013769A/pt

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

"ESTERóIDES ESTROGêNICOS NãO AROMáTICOS, COMPOSIçãO FARMACêUTICA, E, USO DE UM COMPOSTO ESTERóIDE". Divulgados são os novos estrogênio seletivos do tipo tendo um esqueleto de esteróide com um anel A não aromático e um grupo hidroxila livre ou revestido no átomo de carbono n.N<0> 3. Os estrogênios satisfazem a fórmula geral (I), em que R^ 1^ é H, (C~ 1~-C~ 3~) alquila ou (C~ 2~-C~ 3~)acila; R^ 2^ é H, <244>-(C~ 1~-C~ 4~)alquila, <244>-(C~ 2~-C~ 4~)alquenila ou <244>-(C~ 2~-C~ 4~)alquinila; R^ 3^ é H ou (C~ 1~-C~ 4~)alquila, (C~ 2~-C~ 4~)alquenila ou (C~ 2~-C~ 4~)alquinila, cada um na localização 15 ou 16 do esqueleto de esteróide; R^ 4^ é H ou (C~ 1~-C~ 5~)alquila, (C~ 2~-C~ 5~)alquenila ou (C~ 2~-C~ 5~)alquinila, cada um opcionalmente substituído por halógeno; preferido é etinila; R^ 5^ é H, (C~ 1~-C~ 3~)alquila ou (C~ 2~-C~ 3~)acila; R^ 6^ é (C~ 1~-C~ 5~)alquila, (C~ 2~-C~ 5~)alquenila, (C~ 2~-C~ 5~)alquinila ou (C~ 1~-C~ 5~)alquilideno, cada um opcionalmente substituído por halógeno ou (C~ 1~-C~ 3~)alquilóxi; as ligações tracejadas representam ligações duplas opcionais.
BR0013769-3A 1999-09-06 2000-08-28 Esteróides estrogênicos não aromáticos, composição farmacêutica, e, uso de um composto esteróide BR0013769A (pt)

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
BR0013769A true BR0013769A (pt) 2002-04-30

Family

ID=8240610

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0013769-3A BR0013769A (pt) 1999-09-06 2000-08-28 Esteróides estrogênicos não aromáticos, composição farmacêutica, e, uso de um composto esteróide

Country Status (24)

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

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6756366B1 (en) * 1999-04-06 2004-06-29 Akzo Nobel N.V. Orally active androgens
DE60020260T2 (de) * 1999-09-06 2006-01-19 Akzo Nobel N.V. Nicht-aromatische estrogenische steroide mit einem 11-hydrocarbyl substituent
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
AU8201601A (en) * 2000-07-28 2002-02-13 Akzo Nobel Nv 16alpha-methyl or ethyl substituted estrogens
UA89964C2 (ru) 2004-09-08 2010-03-25 Н.В. Органон 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ
US11034716B2 (en) * 2016-03-03 2021-06-15 Crystal Pharma, S.A.U. Process and new intermediates for the preparation of 11-methylene steroids
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
CN1292702A (zh) 1998-03-09 2001-04-25 阿克佐诺贝尔公司 新型避孕药盒
DE60020260T2 (de) * 1999-09-06 2006-01-19 Akzo Nobel N.V. Nicht-aromatische estrogenische steroide mit einem 11-hydrocarbyl substituent

Also Published As

Publication number Publication date
CN1372565A (zh) 2002-10-02
AU7511700A (en) 2001-04-10
NZ517281A (en) 2003-09-26
JP2003508541A (ja) 2003-03-04
AU770331B2 (en) 2004-02-19
ES2241657T3 (es) 2005-11-01
CN100354299C (zh) 2007-12-12
ATE295851T1 (de) 2005-06-15
HUP0202595A3 (en) 2004-06-28
WO2001018027A1 (en) 2001-03-15
KR20020092907A (ko) 2002-12-12
RU2245886C2 (ru) 2005-02-10
US6677329B1 (en) 2004-01-13
CN1637016A (zh) 2005-07-13
EP1224204B1 (en) 2005-05-18
PL353826A1 (en) 2003-12-01
MXPA02001831A (es) 2002-10-23
EP1224204A1 (en) 2002-07-24
HUP0202595A2 (hu) 2002-12-28
IL148116A (en) 2006-10-31
IL148116A0 (en) 2002-09-12
CZ2002831A3 (cs) 2002-05-15
CA2382489A1 (en) 2001-03-15
NO20021079L (no) 2002-04-29
CA2382489C (en) 2008-03-11
ECSP013947A (es) 2002-09-27
ZA200201250B (en) 2003-07-30
NO20021079D0 (no) 2002-03-05
DE60020260T2 (de) 2006-01-19
TR200200575T2 (tr) 2002-06-21
DE60020260D1 (de) 2005-06-23
CN1185249C (zh) 2005-01-19
SK3282002A3 (en) 2002-06-04

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 12A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2166 DE 10/07/2012.