IL96695A - 2,19-methyleneoxy and 2,19-methylenethio bridged steroids as aromatase and 19-hydroxylase inhibitors - Google Patents
2,19-methyleneoxy and 2,19-methylenethio bridged steroids as aromatase and 19-hydroxylase inhibitorsInfo
- Publication number
- IL96695A IL96695A IL9669590A IL9669590A IL96695A IL 96695 A IL96695 A IL 96695A IL 9669590 A IL9669590 A IL 9669590A IL 9669590 A IL9669590 A IL 9669590A IL 96695 A IL96695 A IL 96695A
- Authority
- IL
- Israel
- Prior art keywords
- compound
- formula
- alkanoyl
- double bond
- aromatase
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title description 14
- 150000003431 steroids Chemical class 0.000 title description 11
- 102000014654 Aromatase Human genes 0.000 title description 9
- 108010078554 Aromatase Proteins 0.000 title description 9
- 150000001875 compounds Chemical class 0.000 claims description 70
- 239000000203 mixture Substances 0.000 claims description 22
- -1 X = =0 Chemical group 0.000 claims description 12
- UAOMVDZJSHZZME-UHFFFAOYSA-N diisopropylamine Chemical compound CC(C)NC(C)C UAOMVDZJSHZZME-UHFFFAOYSA-N 0.000 claims description 12
- 229940011871 estrogen Drugs 0.000 claims description 10
- 239000000262 estrogen Substances 0.000 claims description 10
- ZCSHNCUQKCANBX-UHFFFAOYSA-N lithium diisopropylamide Chemical compound [Li+].CC(C)[N-]C(C)C ZCSHNCUQKCANBX-UHFFFAOYSA-N 0.000 claims description 6
- XJGUKDJAOUXADK-UHFFFAOYSA-N [difluoro(naphthalen-2-yl)methyl]phosphonic acid Chemical compound C1=CC=CC2=CC(C(F)(F)P(O)(=O)O)=CC=C21 XJGUKDJAOUXADK-UHFFFAOYSA-N 0.000 claims description 5
- 206010020772 Hypertension Diseases 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 4
- 229940043279 diisopropylamine Drugs 0.000 claims description 4
- 230000001631 hypertensive effect Effects 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 125000001589 carboacyl group Chemical group 0.000 claims 9
- 230000003509 anti-fertility effect Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000000350 glycoloyl group Chemical group O=C([*])C([H])([H])O[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 42
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- 239000000243 solution Substances 0.000 description 29
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- 238000006243 chemical reaction Methods 0.000 description 14
- KQTAMTBUQUXVAK-MFDYCWBWSA-N 2,19-moaed Chemical compound C1OC[C@]23[C@H]4CC[C@](C)(C(CC5)=O)[C@@H]5[C@@H]4CCC3=CC(=O)[C@@H]1C2 KQTAMTBUQUXVAK-MFDYCWBWSA-N 0.000 description 13
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- 235000011152 sodium sulphate Nutrition 0.000 description 5
- XGUHPTGEXRHMQQ-BGJMDTOESA-N 19-hydroxyandrost-4-ene-3,17-dione Chemical compound O=C1CC[C@]2(CO)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 XGUHPTGEXRHMQQ-BGJMDTOESA-N 0.000 description 4
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Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0073—Sulfur-containing hetero ring
- C07J71/0078—Sulfur-containing hetero ring containing only sulfur
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45344189A | 1989-12-20 | 1989-12-20 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL96695A0 IL96695A0 (en) | 1991-09-16 |
| IL96695A true IL96695A (en) | 1996-08-04 |
Family
ID=23800602
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL9669590A IL96695A (en) | 1989-12-20 | 1990-12-17 | 2,19-methyleneoxy and 2,19-methylenethio bridged steroids as aromatase and 19-hydroxylase inhibitors |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP0434020B1 (da) |
| JP (1) | JP2922653B2 (da) |
| KR (1) | KR100187781B1 (da) |
| CN (1) | CN1035768C (da) |
| AR (1) | AR248410A1 (da) |
| AT (1) | ATE124417T1 (da) |
| AU (1) | AU630008B2 (da) |
| CA (1) | CA2032311C (da) |
| DE (1) | DE69020520T2 (da) |
| DK (1) | DK0434020T3 (da) |
| ES (1) | ES2076286T3 (da) |
| FI (1) | FI107925B (da) |
| GR (1) | GR3017136T3 (da) |
| HU (1) | HU208024B (da) |
| IE (1) | IE67557B1 (da) |
| IL (1) | IL96695A (da) |
| NO (1) | NO177676C (da) |
| NZ (1) | NZ236473A (da) |
| PT (1) | PT96258B (da) |
| ZA (1) | ZA9010082B (da) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5491136A (en) * | 1989-12-20 | 1996-02-13 | Merrell Dow Pharmaceuticals Inc. | 2,19-methyleneoxy and 2,19-methylenethio bridged steroids as aromatase, 19-hydroxylaser inhibitors and methods of their use in the treatment of estrogen mediated disorders |
| US5126488A (en) * | 1990-11-30 | 1992-06-30 | Merrell Dow Pharmaceuticals Inc. | 2β,19-methyleneamino bridged steroids as aromatase inhibitors |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3627756A (en) * | 1970-04-23 | 1971-12-14 | Searle & Co | N-dialkylaminoalkyl-n-(2{62 ,19-epoxy-5{60 -androstan-17{62 -yl)amines/formamides and 3{60 -halo derivatives thereof |
| US3954980A (en) * | 1971-10-19 | 1976-05-04 | Derek Harold Richard Barton | Chemical compounds |
| US4814324A (en) * | 1987-03-06 | 1989-03-21 | Merck & Co., Inc. | Sterol inhibitors of testosterone 5α-reductase |
-
1990
- 1990-12-14 ZA ZA9010082A patent/ZA9010082B/xx unknown
- 1990-12-14 CA CA002032311A patent/CA2032311C/en not_active Expired - Fee Related
- 1990-12-14 NZ NZ236473A patent/NZ236473A/xx unknown
- 1990-12-14 AU AU68083/90A patent/AU630008B2/en not_active Ceased
- 1990-12-17 IL IL9669590A patent/IL96695A/en not_active IP Right Cessation
- 1990-12-17 HU HU908299A patent/HU208024B/hu not_active IP Right Cessation
- 1990-12-18 KR KR1019900020871A patent/KR100187781B1/ko not_active Expired - Fee Related
- 1990-12-19 JP JP2411707A patent/JP2922653B2/ja not_active Expired - Fee Related
- 1990-12-19 EP EP90124739A patent/EP0434020B1/en not_active Expired - Lifetime
- 1990-12-19 IE IE459790A patent/IE67557B1/en not_active IP Right Cessation
- 1990-12-19 CN CN90110133A patent/CN1035768C/zh not_active Expired - Fee Related
- 1990-12-19 DE DE69020520T patent/DE69020520T2/de not_active Expired - Fee Related
- 1990-12-19 DK DK90124739.5T patent/DK0434020T3/da active
- 1990-12-19 PT PT96258A patent/PT96258B/pt not_active IP Right Cessation
- 1990-12-19 ES ES90124739T patent/ES2076286T3/es not_active Expired - Lifetime
- 1990-12-19 AT AT90124739T patent/ATE124417T1/de not_active IP Right Cessation
- 1990-12-19 NO NO905494A patent/NO177676C/no not_active IP Right Cessation
- 1990-12-19 FI FI906269A patent/FI107925B/fi not_active IP Right Cessation
- 1990-12-20 AR AR90318689A patent/AR248410A1/es active
-
1995
- 1995-08-16 GR GR950402256T patent/GR3017136T3/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed | ||
| KB | Patent renewed | ||
| MM9K | Patent not in force due to non-payment of renewal fees |