JPS5946299A - 11β及び2位が置換されている新規な19―ノルステロイド、それらの製造方法及びこれらを含有する組成物 - Google Patents

11β及び2位が置換されている新規な19―ノルステロイド、それらの製造方法及びこれらを含有する組成物

Info

Publication number
JPS5946299A
JPS5946299A JP58102979A JP10297983A JPS5946299A JP S5946299 A JPS5946299 A JP S5946299A JP 58102979 A JP58102979 A JP 58102979A JP 10297983 A JP10297983 A JP 10297983A JP S5946299 A JPS5946299 A JP S5946299A
Authority
JP
Japan
Prior art keywords
group
compound
formula
carbon atoms
estra
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.)
Granted
Application number
JP58102979A
Other languages
English (en)
Japanese (ja)
Other versions
JPH0443077B2 (oth
Inventor
ジヤン・ジヨルジユ・トウ−チ
ベスペルト・トレリ
ロジエ・ドラエ
ダニエル・フイリベ−ル
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.)
Sanofi Aventis France
Original Assignee
Roussel Uclaf SA
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 Roussel Uclaf SA filed Critical Roussel Uclaf SA
Publication of JPS5946299A publication Critical patent/JPS5946299A/ja
Publication of JPH0443077B2 publication Critical patent/JPH0443077B2/ja
Granted legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0081Substituted in position 17 alfa and 17 beta
    • C07J1/0088Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0059Estrane derivatives substituted in position 17 by a keto group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005Ketals
    • C07J21/006Ketals at position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036Nitrogen-containing hetero ring
    • C07J71/0057Nitrogen and oxygen
    • C07J71/0063Nitrogen and oxygen at position 2(3)

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Toxicology (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP58102979A 1982-06-11 1983-06-10 11β及び2位が置換されている新規な19―ノルステロイド、それらの製造方法及びこれらを含有する組成物 Granted JPS5946299A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR82-10205 1982-06-11
FR8210205A FR2528434B1 (fr) 1982-06-11 1982-06-11 Nouveaux 19-nor steroides substitues en 11b et eventuellement en 2, leur procede de preparation et leur application comme medicament

Publications (2)

Publication Number Publication Date
JPS5946299A true JPS5946299A (ja) 1984-03-15
JPH0443077B2 JPH0443077B2 (oth) 1992-07-15

Family

ID=9274893

Family Applications (1)

Application Number Title Priority Date Filing Date
JP58102979A Granted JPS5946299A (ja) 1982-06-11 1983-06-10 11β及び2位が置換されている新規な19―ノルステロイド、それらの製造方法及びこれらを含有する組成物

Country Status (7)

Country Link
US (2) US4547493A (oth)
EP (2) EP0097572B1 (oth)
JP (1) JPS5946299A (oth)
AT (1) ATE46702T1 (oth)
CA (1) CA1220780A (oth)
DE (1) DE3367396D1 (oth)
FR (1) FR2528434B1 (oth)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59157099A (ja) * 1983-02-18 1984-09-06 シエ−リング・アクチエンゲゼルシヤフト 11β―アリール―エストラジエン及びその製法
JPS6118798A (ja) * 1984-06-29 1986-01-27 ルセル‐ユクラフ 新規の11β位置換ステロイド誘導体、それらの製造方法及びそれらの薬剤としての使用
JP2002518516A (ja) * 1998-06-23 2002-06-25 ヘキスト・マリオン・ルセル 新規の17−ハロゲン化−19−ノルステロイド、それらの製造方法及び中間体、それらの医薬としての使用並びにそれらを含有する製薬組成物
JP2006524671A (ja) * 2003-04-29 2006-11-02 アベンティス ファルマ ソシエテ アノニム 19−ノルステロイド化合物の新製造方法及び中間体
JP2006525290A (ja) * 2003-04-29 2006-11-09 アベンティス ファルマ ソシエテ アノニム 17−ハロゲン化19−ノルステロイド化合物の新製造方法及び中間体
JP2012533578A (ja) * 2009-07-21 2012-12-27 バイエル ファーマ アクチエンゲゼルシャフト 17−ヒドロキシ−17−ペンタフルオロエチルエストラ−4,9−(10)−ジエン−11−アリール誘導体、その調製方法、その誘導体を利用した諸疾患の治療

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4978657A (en) * 1981-01-09 1990-12-18 Roussel Uclaf Novel 11β-substituted-19-nor-steroids
EP0116974B1 (de) * 1983-02-18 1986-10-29 Schering Aktiengesellschaft 11-Beta-Aryl-Estradiene, Verfahren zu deren Herstellung und diese enthaltende pharmazeutische Präparate
FR2573657B1 (fr) * 1984-11-29 1989-05-12 Roussel Uclaf Produit comprenant une substance antiprogestomimetique et une substance uterotonique
FR2596395B1 (fr) * 1986-03-26 1989-05-26 Roussel Uclaf Nouveaux steroides comportant un cycle spirannique en position 17, leur procede de preparation, leur application comme medicaments et les compositions les renfermant
DE3625315A1 (de) * 1986-07-25 1988-01-28 Schering Ag 11ss-(4-isopropenylphenyl)-estra-4,9-diene, deren herstellung und diese enthaltende pharmazeutische praeparate
FR2610933B1 (fr) * 1987-02-18 1989-06-09 Roussel Uclaf Nouveaux 19-nor steroides substitues en position 7, leur preparation, leur application comme medicaments, les compositions pharmaceutiques les renfermant
FR2620707B1 (fr) * 1987-09-18 1989-12-08 Roussel Uclaf Nouveaux steroides comportant un cycle spirannique a 3, 4 ou 6 chainons en position 17, leur procede et des intermediaires de preparation, leur application comme medicaments et les compositions pharmaceutiques les renfermant
JP2785023B2 (ja) * 1987-12-30 1998-08-13 ルセル―ユクラフ 17α位置を置換された17β―OH―19―ノルステロイドの新誘導体、その製造方法、その薬剤としての使用及びそれを含有する製薬組成物
US5686465A (en) * 1988-10-31 1997-11-11 Endorecherche Inc. Sex steroid activity inhibitors
US5395842A (en) * 1988-10-31 1995-03-07 Endorecherche Inc. Anti-estrogenic compounds and compositions
US5204337A (en) * 1988-10-31 1993-04-20 Endorecherche Inc. Estrogen nucleus derivatives for use in inhibition of sex steroid activity
US6790971B1 (en) * 1989-02-24 2004-09-14 Aventis Pharma S.A. 19-Nor-steroids
US5364847A (en) * 1989-03-10 1994-11-15 Endorecherche Inhibitors of sex steroid biosynthesis and methods for their production and use
DE3921059A1 (de) * 1989-06-23 1991-01-10 Schering Ag 11(beta)-aryl-4-estrene, verfahren zu ihrer herstellung sowie deren verwendung als arzneimittel
WO1991000732A1 (en) * 1989-07-07 1991-01-24 Endorecherche Inc. Androgen derivatives for use in the inhibition of sex steroid activity
HUT60139A (en) * 1989-07-07 1992-08-28 Endorecherche Inc Process for producing pharmaceutical composition suitable for treating prostate cancer connected with androgen
DE59010853D1 (de) * 1989-08-04 1998-12-03 Schering Ag 11 Beta-Aryl-gona-4,9-dien-3-one
FR2651435A1 (fr) * 1989-09-07 1991-03-08 Roussel Uclaf Nouvelle utilisation de composes anti-progestomimetiques.
FR2654337B1 (fr) * 1989-11-15 1994-08-05 Roussel Uclaf Nouvelles microspheres injectables biodegradables procede de preparation et suspensions injectables les renfermant.
DE4008584A1 (de) * 1990-03-15 1991-09-26 Schering Ag Verfahren zur herstellung von zwischenprodukten fuer die antigestagensynthese (onapristonsynthese)
US5407928A (en) * 1990-08-15 1995-04-18 Schering Aktiengesellschaft 11β-aryl-gona-4,9-dien-3-ones
ZA924811B (en) * 1991-06-28 1993-12-29 Endorecherche Inc Controlled release systems and low dose androgens
DE4132182A1 (de) * 1991-09-24 1993-03-25 Schering Ag 11(beta)-substituierte 14, 17-ethanoestratriene, verfahren zur herstellung dieser verbindungen, sowie ihre verwendung zur herstellung von arzneimitteln
US6060503A (en) * 1991-12-02 2000-05-09 Endorecherche, Inc. Benzopyran-containing compounds and method for their use
FR2685332A1 (fr) * 1991-12-20 1993-06-25 Roussel Uclaf Nouveaux 19-nor sterouides ayant en position 11beta une chaine thiocarbonee, leur procede de preparation et les intermediaires et leur application a titre de medicaments.
JPH07506575A (ja) * 1992-05-21 1995-07-20 アンドルシェルシュ・インコーポレイテッド テストステロン5α−レダクターゼ活性の阻害剤
FR2706454B1 (fr) * 1993-06-17 1995-09-15 Roussel Uclaf Nouveaux 19-Nor stéroïdes, procédé et intermédiaires de préparation, application comme médicaments et compositions pharmaceutiques les contenant.
US5679788A (en) * 1993-06-17 1997-10-21 Roussel Uclaf 11 beta-substituted-19 nor-steroids
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
EP0683172B1 (en) * 1994-05-19 1997-08-13 Akzo Nobel N.V. 11,21-Bisphenyl-19-norpregnane derivatives
US5929262A (en) * 1995-03-30 1999-07-27 The United States Of America As Represented By The Department Of Health And Human Services Method for preparing 17α-acetoxy-11β-(4-N, N-dimethylaminophyl)-19-Norpregna-4,9-diene-3, 20-dione, intermediates useful in the method, and methods for the preparation of such intermediates
FR2757399B1 (fr) * 1996-12-23 1999-12-17 Hoechst Marion Roussel Inc Application de composes steroides substitues en 11 pour la fabrication de medicaments ayant une activite estrogene dissociee
GB9910934D0 (en) * 1999-05-11 1999-07-14 Res Inst Medicine Chem Chemical compounds
FR2826004B1 (fr) 2001-06-13 2008-03-28 Aventis Pharma Sa Procede de preparation de derives estrogenes
WO2004112720A2 (en) * 2003-06-20 2004-12-29 Viral Genomix, Inc. Antiviral compositions and methods of using the same
ATE453660T1 (de) * 2006-02-17 2010-01-15 Janssen Pharmaceutica Nv 17-phosphor-steroid-derivate als progesteron- rezeptormodulatoren
WO2011150209A1 (en) 2010-05-26 2011-12-01 Corcept Therapeutics, Inc. Treatment of muscular dystrophy
AU2016226451B2 (en) 2015-03-02 2019-12-19 Corcept Therapeutics, Inc. Use of glucocorticoid receptor antagonist and somatostatin analogues to treat ACTH-secreting tumors
US10610534B2 (en) 2015-03-30 2020-04-07 Corcept Therapeutics, Inc. Use of glucocorticoid receptor antagonists in combination with glucocorticoids to treat adrenal insufficiency
KR20180052120A (ko) 2015-08-13 2018-05-17 코어셉트 쎄라퓨틱스, 잉크. Acth-의존성 쿠싱 증후군을 감별 진단하는 방법
WO2017112904A1 (en) * 2015-12-23 2017-06-29 Oric Pharmaceuticals, Inc. Inhibitors of glucocorticoid receptor
EP3394078A4 (en) 2015-12-23 2019-11-27 Oric Pharmaceuticals, Inc. INHIBITORS OF THE GLUCOCORTICIDE RECEPTOR
JP6995757B2 (ja) 2015-12-23 2022-01-17 オリック ファーマシューティカルズ,インク. グルココルチコイド受容体の阻害剤
JP6765443B2 (ja) 2016-01-19 2020-10-07 コーセプト セラピューティクス, インコーポレイテッド 異所性クッシング症候群の鑑別診断
US10913811B2 (en) 2016-03-18 2021-02-09 Basf Se Finely divided aqueous multistage polymer dispersion, method for the production thereof, and use thereof as a binder
NZ753142A (en) 2016-10-07 2020-08-28 Oric Pharmaceuticals Inc Inhibitors of glucocorticoid receptor
MX2019011543A (es) 2017-03-31 2019-12-16 Corcept Therapeutics Inc Moduladores del receptor de glucocorticoides para el tratamiento de cancer cervical.
WO2018236749A2 (en) 2017-06-20 2018-12-27 Corcept Therapeutics, Inc. Methods of treating neuroepithelial tumors using selective glucocorticoid receptor modulators
EP4653047A3 (en) 2019-03-18 2026-02-18 Nieman, Lynnette K. Mifepristone for use in improving insulin sensitivity
JP2024500748A (ja) 2020-12-18 2024-01-10 インスティル バイオ (ユーケイ) リミテッド 腫瘍浸潤リンパ球の処理

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2377419A1 (fr) * 1977-01-13 1978-08-11 Roussel Uclaf Nouveaux derives steroides 11b-substitues 1,3,5 (10) trieniques, leur procede de preparation et leur application comme medicament
FR2377418A1 (fr) * 1977-01-13 1978-08-11 Roussel Uclaf Nouveaux derives steroides 4,9-dieniques 11b-substitues, leur procede de preparation et leur application comme medicaments
NL7701384A (nl) * 1977-02-10 1978-08-14 Akzo Nv Werkwijze voor het bereiden van nieuwe steroiden van de oestraanreeks.
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

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59157099A (ja) * 1983-02-18 1984-09-06 シエ−リング・アクチエンゲゼルシヤフト 11β―アリール―エストラジエン及びその製法
JPS6118798A (ja) * 1984-06-29 1986-01-27 ルセル‐ユクラフ 新規の11β位置換ステロイド誘導体、それらの製造方法及びそれらの薬剤としての使用
JP2002518516A (ja) * 1998-06-23 2002-06-25 ヘキスト・マリオン・ルセル 新規の17−ハロゲン化−19−ノルステロイド、それらの製造方法及び中間体、それらの医薬としての使用並びにそれらを含有する製薬組成物
JP2006524671A (ja) * 2003-04-29 2006-11-02 アベンティス ファルマ ソシエテ アノニム 19−ノルステロイド化合物の新製造方法及び中間体
JP2006525290A (ja) * 2003-04-29 2006-11-09 アベンティス ファルマ ソシエテ アノニム 17−ハロゲン化19−ノルステロイド化合物の新製造方法及び中間体
JP4755083B2 (ja) * 2003-04-29 2011-08-24 アベンティス・ファーマ・ソシエテ・アノニム 19−ノルステロイド化合物の新製造方法及び中間体
JP2012533578A (ja) * 2009-07-21 2012-12-27 バイエル ファーマ アクチエンゲゼルシャフト 17−ヒドロキシ−17−ペンタフルオロエチルエストラ−4,9−(10)−ジエン−11−アリール誘導体、その調製方法、その誘導体を利用した諸疾患の治療

Also Published As

Publication number Publication date
FR2528434B1 (fr) 1985-07-19
FR2528434A1 (fr) 1983-12-16
ATE46702T1 (de) 1989-10-15
EP0097572A1 (fr) 1984-01-04
EP0196707B1 (fr) 1989-09-27
US4547493A (en) 1985-10-15
CA1220780A (fr) 1987-04-21
DE3367396D1 (en) 1986-12-11
EP0196707A1 (fr) 1986-10-08
US4634696A (en) 1987-01-06
EP0097572B1 (fr) 1986-11-05
JPH0443077B2 (oth) 1992-07-15

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