HRP20000315A2 - Novel 19-nor steroids substitured in position 11beta, preparation method and intermediates, application as medicines and pharmaceutical compositions containing them - Google Patents
Novel 19-nor steroids substitured in position 11beta, preparation method and intermediates, application as medicines and pharmaceutical compositions containing them Download PDFInfo
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- HRP20000315A2 HRP20000315A2 HR20000315A HRP20000315A HRP20000315A2 HR P20000315 A2 HRP20000315 A2 HR P20000315A2 HR 20000315 A HR20000315 A HR 20000315A HR P20000315 A HRP20000315 A HR P20000315A HR P20000315 A2 HRP20000315 A2 HR P20000315A2
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- Prior art keywords
- formula
- phenyl
- estra
- propyl
- action
- Prior art date
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- 238000002360 preparation method Methods 0.000 title claims description 14
- 239000003814 drug Substances 0.000 title claims description 10
- 229940079593 drug Drugs 0.000 title claims description 9
- 239000000543 intermediate Substances 0.000 title claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 title description 4
- 150000001875 compounds Chemical class 0.000 claims description 117
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 67
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 58
- 230000009471 action Effects 0.000 claims description 53
- 150000003839 salts Chemical class 0.000 claims description 32
- 125000004432 carbon atom Chemical group C* 0.000 claims description 30
- 239000002253 acid Substances 0.000 claims description 23
- 150000007513 acids Chemical class 0.000 claims description 21
- 125000003118 aryl group Chemical group 0.000 claims description 18
- 239000000460 chlorine Substances 0.000 claims description 18
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 18
- 125000004043 oxo group Chemical group O=* 0.000 claims description 18
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 17
- 125000003342 alkenyl group Chemical group 0.000 claims description 16
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- 238000006243 chemical reaction Methods 0.000 claims description 15
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- 229910052799 carbon Inorganic materials 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 14
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- IWVMCIAPBOORJL-UHFFFAOYSA-N thieno[2,3-b]furan Chemical compound C1=CSC2=C1C=CO2 IWVMCIAPBOORJL-UHFFFAOYSA-N 0.000 description 1
- 238000001890 transfection Methods 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- KPZSTOVTJYRDIO-UHFFFAOYSA-K trichlorocerium;heptahydrate Chemical compound O.O.O.O.O.O.O.Cl[Ce](Cl)Cl KPZSTOVTJYRDIO-UHFFFAOYSA-K 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- BZVJOYBTLHNRDW-UHFFFAOYSA-N triphenylmethanamine Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(N)C1=CC=CC=C1 BZVJOYBTLHNRDW-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000002485 urinary effect Effects 0.000 description 1
- 239000006216 vaginal suppository Substances 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 125000001834 xanthenyl group Chemical group C1=CC=CC=2OC3=CC=CC=C3C(C12)* 0.000 description 1
- 125000004933 β-carbolinyl group Chemical group C1(=NC=CC=2C3=CC=CC=C3NC12)* 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- 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
-
- 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
-
- 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
- C07J41/0077—Normal 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
- C07J41/0083—Normal 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Rheumatology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9714357A FR2771096B1 (fr) | 1997-11-17 | 1997-11-17 | Nouveaux 19-nor steroides, substitues en position 11beta, procede et intermediaires de preparation, application comme medicaments et compositions pharmaceutiques les renfermant |
| PCT/FR1998/002437 WO1999025725A1 (fr) | 1997-11-17 | 1998-11-16 | NOUVEAUX 19-NOR STEROÏDES SUBSTITUES EN POSITION 11β, PROCEDE ET INTERMEDIAIRES DE PREPARATION, APPLICATION COMME MEDICAMENTS ET COMPOSITIONS PHARMACEUTIQUES LES RENFERMANT |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20000315A2 true HRP20000315A2 (en) | 2000-10-31 |
Family
ID=9513422
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20000315A HRP20000315A2 (en) | 1997-11-17 | 2000-05-17 | Novel 19-nor steroids substitured in position 11beta, preparation method and intermediates, application as medicines and pharmaceutical compositions containing them |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US6479476B1 (es) |
| EP (1) | EP1032584B1 (es) |
| JP (1) | JP4476480B2 (es) |
| KR (1) | KR20010032127A (es) |
| CN (1) | CN1286694A (es) |
| AR (1) | AR016012A1 (es) |
| AT (1) | ATE232542T1 (es) |
| AU (1) | AU754846B2 (es) |
| BR (1) | BR9814201A (es) |
| CA (1) | CA2309242A1 (es) |
| CZ (1) | CZ20001799A3 (es) |
| DE (1) | DE69811393T2 (es) |
| EA (1) | EA003133B1 (es) |
| ES (1) | ES2192341T3 (es) |
| FR (1) | FR2771096B1 (es) |
| HR (1) | HRP20000315A2 (es) |
| HU (1) | HUP0100210A3 (es) |
| ID (1) | ID24236A (es) |
| IL (1) | IL136148A0 (es) |
| NO (1) | NO20002483L (es) |
| PL (1) | PL340381A1 (es) |
| SK (1) | SK7052000A3 (es) |
| TR (1) | TR200001405T2 (es) |
| WO (1) | WO1999025725A1 (es) |
| ZA (1) | ZA9810358B (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2757519B1 (fr) * | 1996-12-23 | 1999-06-11 | Hoechst Marion Roussel Inc | Steroides substitues en position 11, leur procede de preparation, leur application comme medicament et les compositions pharmaceutiques les renfermant |
| FR2780060B1 (fr) * | 1998-06-23 | 2000-08-04 | Hoechst Marion Roussel Inc | Nouveaux 19-nor steroides 17-halogenes, procede et intermediaires de preparation, application comme medicaments et compositions pharmaceutiques les renfermant |
| DE19929715A1 (de) * | 1999-06-24 | 2000-12-28 | Schering Ag | 11ß-langkettig-substituierte Estratriene, Verfahren zur Herstellung , pharmazeutische Präparate, die diese 11ß-langkettig-substituierten Estratriene enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln |
| FR2826004B1 (fr) | 2001-06-13 | 2008-03-28 | Aventis Pharma Sa | Procede de preparation de derives estrogenes |
| FR2854402B1 (fr) * | 2003-04-29 | 2008-07-04 | Aventis Pharma Sa | Nouveau procede et intermediaires de preparation de composes 19-nor-steroides |
| FR2854403B1 (fr) * | 2003-04-29 | 2008-07-11 | Aventis Pharma Sa | Nouveau procede et intermediaires de preparation de composes 19-nor-steroides 17-halogenes |
| JP6608929B2 (ja) * | 2014-11-26 | 2019-11-20 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | エストロゲン受容体調節薬 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4978657A (en) * | 1981-01-09 | 1990-12-18 | Roussel Uclaf | Novel 11β-substituted-19-nor-steroids |
| FR2640977A2 (en) * | 1982-06-11 | 1990-06-29 | Roussel Uclaf | New position-11 substituted 19-norsteroids and their application as medicinal products. |
| FR2643638B1 (fr) * | 1989-02-24 | 1991-06-14 | Roussel Uclaf | Nouveaux 19-nor steroides ayant en position 11beta une chaine carbonee comportant une fonction amide ou carbamate, leur procede de preparation et les intermediaires de ce procede, leur application comme medicaments et les compositions pharmaceutiques les contenant |
-
1997
- 1997-11-17 FR FR9714357A patent/FR2771096B1/fr not_active Expired - Fee Related
-
1998
- 1998-11-12 ZA ZA9810358A patent/ZA9810358B/xx unknown
- 1998-11-16 WO PCT/FR1998/002437 patent/WO1999025725A1/fr not_active Application Discontinuation
- 1998-11-16 AU AU12426/99A patent/AU754846B2/en not_active Ceased
- 1998-11-16 JP JP2000521105A patent/JP4476480B2/ja not_active Expired - Fee Related
- 1998-11-16 IL IL13614898A patent/IL136148A0/xx unknown
- 1998-11-16 ID IDW20000928A patent/ID24236A/id unknown
- 1998-11-16 SK SK705-2000A patent/SK7052000A3/sk unknown
- 1998-11-16 AT AT98955663T patent/ATE232542T1/de not_active IP Right Cessation
- 1998-11-16 CZ CZ20001799A patent/CZ20001799A3/cs unknown
- 1998-11-16 US US09/554,783 patent/US6479476B1/en not_active Expired - Lifetime
- 1998-11-16 HU HU0100210A patent/HUP0100210A3/hu unknown
- 1998-11-16 ES ES98955663T patent/ES2192341T3/es not_active Expired - Lifetime
- 1998-11-16 EA EA200000530A patent/EA003133B1/ru not_active IP Right Cessation
- 1998-11-16 KR KR1020007005314A patent/KR20010032127A/ko not_active Application Discontinuation
- 1998-11-16 TR TR2000/01405T patent/TR200001405T2/xx unknown
- 1998-11-16 EP EP98955663A patent/EP1032584B1/fr not_active Expired - Lifetime
- 1998-11-16 BR BR9814201-1A patent/BR9814201A/pt not_active IP Right Cessation
- 1998-11-16 CN CN98813160A patent/CN1286694A/zh active Pending
- 1998-11-16 DE DE69811393T patent/DE69811393T2/de not_active Expired - Lifetime
- 1998-11-16 PL PL98340381A patent/PL340381A1/xx unknown
- 1998-11-16 CA CA002309242A patent/CA2309242A1/fr not_active Abandoned
- 1998-11-17 AR ARP980105822A patent/AR016012A1/es unknown
-
2000
- 2000-05-12 NO NO20002483A patent/NO20002483L/no not_active Application Discontinuation
- 2000-05-17 HR HR20000315A patent/HRP20000315A2/hr not_active Application Discontinuation
-
2002
- 2002-04-10 US US10/119,903 patent/US6693090B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| ATE232542T1 (de) | 2003-02-15 |
| NO20002483L (no) | 2000-07-17 |
| HUP0100210A3 (en) | 2001-12-28 |
| EA003133B1 (ru) | 2003-02-27 |
| NO20002483D0 (no) | 2000-05-12 |
| WO1999025725A1 (fr) | 1999-05-27 |
| KR20010032127A (ko) | 2001-04-16 |
| AU754846B2 (en) | 2002-11-28 |
| AU1242699A (en) | 1999-06-07 |
| HUP0100210A1 (hu) | 2001-08-28 |
| US6693090B2 (en) | 2004-02-17 |
| US6479476B1 (en) | 2002-11-12 |
| PL340381A1 (en) | 2001-01-29 |
| CZ20001799A3 (cs) | 2001-11-14 |
| ZA9810358B (en) | 1999-11-12 |
| TR200001405T2 (tr) | 2001-05-21 |
| JP2001523687A (ja) | 2001-11-27 |
| US20030073675A1 (en) | 2003-04-17 |
| CA2309242A1 (fr) | 1999-05-27 |
| ID24236A (id) | 2000-07-13 |
| CN1286694A (zh) | 2001-03-07 |
| DE69811393T2 (de) | 2003-08-28 |
| JP4476480B2 (ja) | 2010-06-09 |
| FR2771096B1 (fr) | 2000-08-11 |
| ES2192341T3 (es) | 2003-10-01 |
| EA200000530A1 (ru) | 2000-10-30 |
| EP1032584A1 (fr) | 2000-09-06 |
| AR016012A1 (es) | 2001-05-30 |
| FR2771096A1 (fr) | 1999-05-21 |
| BR9814201A (pt) | 2000-09-26 |
| IL136148A0 (en) | 2001-05-20 |
| EP1032584B1 (fr) | 2003-02-12 |
| DE69811393D1 (de) | 2003-03-20 |
| SK7052000A3 (en) | 2000-12-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A1OB | Publication of a patent application | ||
| ARAI | Request for the grant of a patent on the basis of the submitted results of a substantive examination of a patent application | ||
| ODRP | Renewal fee for the maintenance of a patent |
Payment date: 20021105 Year of fee payment: 5 |
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| PNAN | Change of the applicant name, address/residence |
Owner name: AVENTIS PHARMA S.A., FR |
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| OBST | Application withdrawn |