CN1033033C - 具有孕甾酮拮抗活性的11β，19桥接甾族化合物的制备方法 - Google Patents

具有孕甾酮拮抗活性的11β，19桥接甾族化合物的制备方法 Download PDF

Info

Publication number
CN1033033C
CN1033033C CN88102162A CN88102162A CN1033033C CN 1033033 C CN1033033 C CN 1033033C CN 88102162 A CN88102162 A CN 88102162A CN 88102162 A CN88102162 A CN 88102162A CN 1033033 C CN1033033 C CN 1033033C
Authority
CN
China
Prior art keywords
compound
phenylene
group
hydroxy
prop
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN88102162A
Other languages
English (en)
Chinese (zh)
Other versions
CN88102162A (zh
Inventor
埃卡德·奥托
鲁道夫·维歇特
根特·尼夫
聚比尔·拜雅
沃尔特·埃尔格
戴维·安德鲁·亨德逊
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharma AG
Merck Sharp and Dohme LLC
Original Assignee
Schering AG
Schering Corp
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 Schering AG, Schering Corp filed Critical Schering AG
Publication of CN88102162A publication Critical patent/CN88102162A/zh
Application granted granted Critical
Publication of CN1033033C publication Critical patent/CN1033033C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0057—Nitrogen and oxygen
    • C07J71/0063—Nitrogen and oxygen at position 2(3)
    • 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
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/006—Ketals at position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0038—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an androstane skeleton, including 18- or 19-substituted derivatives, 18-nor derivatives and also derivatives where position 17-beta is substituted by a carbon atom not directly bonded to a further carbon atom and not being part of an amide group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C07J53/002—Carbocyclic rings fused
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0047—Nitrogen only at position 2(3)

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • External Artificial Organs (AREA)
  • Separation By Low-Temperature Treatments (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN88102162A 1987-03-18 1988-03-18 具有孕甾酮拮抗活性的11β，19桥接甾族化合物的制备方法 Expired - Fee Related CN1033033C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DEP3708942.0 1987-03-18
DE19873708942 DE3708942A1 (de) 1987-03-18 1987-03-18 19,11ss-ueberbrueckte steroide, deren herstellung und diese enthaltende pharmazeutische praeparate

Related Child Applications (2)

Application Number Title Priority Date Filing Date
CN96100917A Division CN1057770C (zh) 1987-03-18 1996-01-17 19,11β－桥甾族化合物在制药中的应用
CN96102566A Division CN1080267C (zh) 1987-03-18 1996-02-01 １９，１１β－桥甾族化合物的中间体的制备

Publications (2)

Publication Number Publication Date
CN88102162A CN88102162A (zh) 1988-11-23
CN1033033C true CN1033033C (zh) 1996-10-16

Family

ID=6323462

Family Applications (3)

Application Number Title Priority Date Filing Date
CN88102162A Expired - Fee Related CN1033033C (zh) 1987-03-18 1988-03-18 具有孕甾酮拮抗活性的11β，19桥接甾族化合物的制备方法
CN96100917A Expired - Fee Related CN1057770C (zh) 1987-03-18 1996-01-17 19,11β－桥甾族化合物在制药中的应用
CN96102566A Expired - Fee Related CN1080267C (zh) 1987-03-18 1996-02-01 １９，１１β－桥甾族化合物的中间体的制备

Family Applications After (2)

Application Number Title Priority Date Filing Date
CN96100917A Expired - Fee Related CN1057770C (zh) 1987-03-18 1996-01-17 19,11β－桥甾族化合物在制药中的应用
CN96102566A Expired - Fee Related CN1080267C (zh) 1987-03-18 1996-02-01 １９，１１β－桥甾族化合物的中间体的制备

Country Status (19)

Country Link
US (1) US5095129A (OSRAM)
EP (1) EP0283428B1 (OSRAM)
JP (1) JP2588267B2 (OSRAM)
CN (3) CN1033033C (OSRAM)
AT (1) ATE69055T1 (OSRAM)
AU (1) AU628015B2 (OSRAM)
CA (1) CA1326015C (OSRAM)
DD (1) DD273262A5 (OSRAM)
DE (2) DE3708942A1 (OSRAM)
ES (1) ES2040373T3 (OSRAM)
FI (1) FI101883B (OSRAM)
GR (1) GR3003362T3 (OSRAM)
HU (2) HU206368B (OSRAM)
IE (1) IE62480B1 (OSRAM)
IL (1) IL85773A (OSRAM)
NZ (1) NZ223924A (OSRAM)
PT (1) PT87007B (OSRAM)
WO (1) WO1988007051A1 (OSRAM)
ZA (1) ZA881962B (OSRAM)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5446178A (en) * 1987-03-18 1995-08-29 Schering Aktiengesellschaft Process for preparing 19,11β-bridged steroids
DE3832303A1 (de) * 1988-09-20 1990-04-12 Schering Ag 11ss-phenyl-14ssh-steroide
DE3917274A1 (de) * 1989-05-24 1990-11-29 Schering Ag 9(alpha)-hydroxy-19, 11(beta)-ueberbrueckte steroide, deren herstellung und diese enthaltende pharmazeutische praeparate
DE3921059A1 (de) * 1989-06-23 1991-01-10 Schering Ag 11(beta)-aryl-4-estrene, verfahren zu ihrer herstellung sowie deren verwendung als arzneimittel
DD289541A5 (de) * 1989-08-04 1991-05-02 ��@�K@�������������@�K@��������������@��������k�� Verfahren zur herstellung von 11beta-aryl-16 alpha, 17 alph-cyclohexanoestra-4,9-dienen
DE4038128A1 (de) * 1990-11-27 1992-06-04 Schering Ag 8-en-19, 11(beta)-ueberbrueckte steroide, deren herstellung und diese enthaltende pharmazeutische praeparate
US5439913A (en) * 1992-05-12 1995-08-08 Schering Aktiengesellschaft Contraception method using competitive progesterone antagonists and novel compounds useful therein
DE4235220A1 (de) * 1992-10-13 1994-06-16 Schering Ag Gestagen wirksame 19,11ß-überbrückte 4-Estrene
DE4413184A1 (de) * 1994-04-12 1995-10-19 Schering Ag 10,11-C¶3¶-überbrückte Steroide
DE4413185A1 (de) * 1994-04-12 1995-10-19 Schering Ag 11beta,19-überbrückte 13alpha-Alkylsteroide
DE4417880A1 (de) * 1994-05-18 1995-11-23 Schering Ag 19,11beta-Überbrückte 18-Nor-Steroide, Verfahren zu ihrer Herstellung, diese Steroide enthaltende Arzneimittel sowie deren Verwendung zur Herstellung von Arzneimitteln
US5780220A (en) * 1994-05-19 1998-07-14 Trustees Of The University Of Pennsylvania Methods and compositions for inhibiting HIV replication
US5639598A (en) * 1994-05-19 1997-06-17 The Trustees Of The University Of Pennsylvania Method and kit for identification of antiviral agents capable of abrogating HIV Vpr-Rip-1 binding interactions
DE4424222C1 (de) * 1994-07-09 1995-09-14 Metallgesellschaft Ag Gelöstes Methyllithium enthaltendes Synthesemittel sowie Verfahren zu deren Herstellung
DE4434488A1 (de) * 1994-09-14 1996-03-21 Schering Ag Steroidester und -amide, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung
US5521166A (en) * 1994-12-19 1996-05-28 Ortho Pharmaceitical Corporation Antiprogestin cyclophasic hormonal regimen
ZA9510926B (en) 1994-12-23 1996-07-03 Schering Ag Compounds with progesterone-antagonistic and antiestrogenic action to be used together for female contraception
IL118974A (en) * 1995-08-17 2001-09-13 Akzo Nobel Nv History 11 - (Transformed Phenyl) - Astra - 4, 9 - Diane, their preparation and pharmaceutical preparations containing them
DE19652408C2 (de) * 1996-12-06 2002-04-18 Schering Ag Steroidester, Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung von Arzneimitteln
US6090798A (en) * 1997-12-19 2000-07-18 Alcon Laboratories, Inc. Treatment of GLC1A glaucoma with glucocorticoid antagonists
GB0000313D0 (en) 2000-01-10 2000-03-01 Astrazeneca Uk Ltd Formulation
PT3263112T (pt) 2006-10-24 2020-08-25 Allergan Pharmaceuticals Int Ltd Composições e métodos para supressão de proliferações do endométrio
TWI539953B (zh) 2008-04-28 2016-07-01 瑞波若斯治療學公司 用於治療乳癌之組成物和方法
CN107260745A (zh) 2010-03-22 2017-10-20 利普生物药剂公司 用于抗孕酮的非毒性递送的组合物和方法
ES2762243T3 (es) 2010-05-26 2020-05-22 Corcept Therapeutics Inc Tratamiento de distrofia muscular
CN103555806B (zh) * 2013-11-16 2015-05-13 江南大学 一种高效利用亚麻刺盘孢霉合成7α-羟基-雄甾烯酮的方法
CN107530435A (zh) 2015-03-02 2018-01-02 科赛普特治疗学股份有限公司 使用糖皮质激素受体拮抗剂和生长抑素治疗acth分泌型肿瘤
MX383353B (es) 2015-03-30 2025-03-13 Corcept Therapeutics Inc Uso de antagonistas de receptores de glucocorticoides en combinacion con glucocorticoides para tratar la insuficiencia adrenal.
MX383318B (es) 2015-08-13 2025-03-13 Corcept Therapeutics Inc Metodo para diagnosticar de manera diferencial el sindrome de cushing dependiente de la corticotropina.
EP3405101B1 (en) 2016-01-19 2020-12-23 Corcept Therapeutics, Inc. Differential diagnosis of ectopic cushing's syndrome
MX2019011543A (es) 2017-03-31 2019-12-16 Corcept Therapeutics Inc Moduladores del receptor de glucocorticoides para el tratamiento de cancer cervical.
MX393313B (es) 2017-06-20 2025-03-24 Corcept Therapeutics Inc Metodos de tratamiento de tumores neuroepiteliales usando moduladores selectivos del receptor de glucocorticoide.
AU2021400069A1 (en) 2020-12-18 2023-07-06 Instil Bio (Uk) Limited Processing of tumor infiltrating lymphocytes

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA8231B (en) * 1981-01-09 1982-11-24 Roussel Uclaf New 11 -substituted steroid derivatives, their preparation, their use as medicaments, the compositions containing them and the new intermediates thus obtained
FR2522328B1 (fr) * 1982-03-01 1986-02-14 Roussel Uclaf Nouveaux produits derives de la structure 3-ceto 4,9 19-nor steroides, leur procede de preparation et leur application comme medicaments
FR2576025B1 (fr) * 1985-01-14 1987-01-23 Roussel Uclaf Nouveaux steroides substitues en position 10, leur procede et les intermediaires de preparation, leur application comme medicaments, les compositions pharmaceutiques les contenant

Also Published As

Publication number Publication date
NZ223924A (en) 1991-12-23
HU210532A9 (en) 1995-04-28
EP0283428A1 (de) 1988-09-21
DE3865863D1 (OSRAM) 1991-12-05
PT87007B (pt) 1992-06-30
JPH02503194A (ja) 1990-10-04
EP0283428B1 (de) 1991-10-30
ES2040373T3 (es) 1993-10-16
IE880793L (en) 1988-09-18
IE62480B1 (en) 1995-02-08
IL85773A (en) 1994-01-01
CN1135488A (zh) 1996-11-13
PT87007A (pt) 1988-04-01
HU206368B (en) 1992-10-28
CN88102162A (zh) 1988-11-23
WO1988007051A1 (fr) 1988-09-22
CA1326015C (en) 1994-01-11
FI894364A0 (fi) 1989-09-15
GR3003362T3 (en) 1993-02-17
ZA881962B (en) 1988-09-08
HU911518D0 (en) 1991-11-28
CN1080267C (zh) 2002-03-06
IL85773A0 (en) 1988-09-30
ATE69055T1 (de) 1991-11-15
DD273262A5 (de) 1989-11-08
CN1141926A (zh) 1997-02-05
JP2588267B2 (ja) 1997-03-05
AU628015B2 (en) 1992-09-10
US5095129A (en) 1992-03-10
CN1057770C (zh) 2000-10-25
AU1420988A (en) 1988-10-10
FI101883B1 (fi) 1998-09-15
FI101883B (fi) 1998-09-15
DE3708942A1 (de) 1988-09-29

Similar Documents

Publication Publication Date Title
CN1033033C (zh) 具有孕甾酮拮抗活性的11β，19桥接甾族化合物的制备方法
CN1036342C (zh) 9，11-脱氢甾类化合物及9-α-羟基-16，17-脱氢甾类化合物的制备方法
CN1131235C (zh) 11β－卤素－7α－经取代的雌三烯、制备包含所述11β－卤素－7α－经取代的雌三烯的药物制剂的方法以及该物质在制备药物中的应用
CN1048499C (zh) 11β－芳基－4－雌烯药物组合物的制备方法
CN1214039C (zh) 3－氮－6,7－二氧甾族化合物及其应用
CN1026236C (zh) 甾类5-α-还原酶抑制剂的制备方法
CN1026324C (zh) 11β-(4-异丙烯基苯基)-4，9-雌二烯，其制法及含此化合物的药剂
CN1158297C (zh) 用于治疗的具有c-17烷基侧链和芳香a-环的甾族化合物
CN1231670A (zh) 7α－(ξ－氨基烷基)－雌三烯、其制备方法、含有7α－(ξ－氨基烷基)－雌三烯的药剂及其用于制备药物的应用
CN86104664A (zh) 取代的雄-1，4-二烯-3，17-二酮类化合物的制法
CN1085562A (zh) 新的7β-取代-4-氮杂-5α-胆甾烷酮作5α-还原酶抑制剂
CN1084857A (zh) 17-螺亚甲基甾族化合物
CN1491230A (zh) 用于改进抗炎治疗的细胞靶向的免疫细胞特异性大环内酯化合物与抗炎化合物的共轭物
HK1046145A1 (zh) 作為選擇性雌激素的16-羥基雌三烯
CN1095383A (zh) 取代的6-氮杂雄甾烯酮
CN1066271A (zh) 14β-H-14-和15-烯键-11β-芳基-4-雌烯
CN1653081A (zh) 甾族化合物的c－17螺甾内酯化和6,7氧化
CN1065070A (zh) 6,7-变性的11β-芳基-4-雌烯
HUT64363A (en) Process for producing 8-ene-19,11-beta-bridged steroides and pharmaceutical preparatives containing them
CN1185249C (zh) 在11位带有烃取代基的非芳香族雌激素甾族化合物
CN85106995A (zh) 在十位以含有双键或三键的基团取代的新的甾体化合物的制备方法
CN1059529A (zh) 抗雄激素的[3，2-C]吡唑基和[3，2-d]三唑基类甾醇
CN101061132A (zh) 用于制备17－羟基－6β,7β;15β,16β－双亚甲基－17α－孕甾4－烯－3－酮－21－羧酸γ－内酯的方法和用于该方法的关键中间体
CN101061133A (zh) 制备17－羟基－6β,7β;15β,16β－双亚甲基－3－氧代－17α－孕甾－4－烯－21－羧酸γ－内酯的工业方法和用于该方法的关键中间体
CN1305890C (zh) 17α－氟烷基甾体、其制备方法以及包含这些化合物的药物组合物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
C15 Extension of patent right duration from 15 to 20 years for appl. with date before 31.12.1992 and still valid on 11.12.2001 (patent law change 1993)
OR01 Other related matters
C19 Lapse of patent right due to non-payment of the annual fee
CF01 Termination of patent right due to non-payment of annual fee