FI92707B - Förfarande för framställning av nya terapeutiskt användbara estramustinestrar - Google Patents
Förfarande för framställning av nya terapeutiskt användbara estramustinestrar Download PDFInfo
- Publication number
- FI92707B FI92707B FI893130A FI893130A FI92707B FI 92707 B FI92707 B FI 92707B FI 893130 A FI893130 A FI 893130A FI 893130 A FI893130 A FI 893130A FI 92707 B FI92707 B FI 92707B
- Authority
- FI
- Finland
- Prior art keywords
- estramustine
- general formula
- compound
- aminoacetate
- methylaminoacetate
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/40—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
- C07C271/42—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/46—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by halogen atoms or by nitro or nitroso groups
-
- 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
- C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Cephalosporin Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Claims (6)
1. Förfarande för framställning av terapeutiskt användbara nya estramustinestrar med den allmänna formeln 5
0 R1 R2 Ä H I / O-C-CH-(CH-) -N rtS v 10 och2ch?x 0 |Υγν C1CH2CH2<^ N C I där R1, R2 och R3 är väte eller lägre alkyl med 1-4 kol-15 atomer, och där R2 och R3 även kan bilda med N-atomen en ring med 2-5 kolatomer, och där n är 0, 1 eller 2, och för framställning av farmaceutiskt godtagbara salter där-av, kännetecknat därav, att a) estramustin förestras med en syra med en reaktiv sub-20 stituent för erhällande av en förening med den allmänna formeln
0 R1 O-fi-CH-(CH^) -R4 CH.J 2 n 25 cich,ch,v o 2 z\ u ^ N-C-0II C1CH2CH2 30 där R4 är en reaktiv substituent, och föreningen II omsätts därefter med en amin med den allmänna formeln HNRZR3, eller b) estramustin förestras med en aminosyra med den allmänna formeln
35 HOOC-CH- (CH2 )n-R2R5 R1 I!: 17 92707 där R5 är R3 eller en skyddsgrupp, för erhallande av en mellanprodukt med den allmänna formeln II, där R4 är -NRZR5, frän vilken skyddsgruppen efterät avlägsnas för erhällande av en förening med den allmänna formeln I. 5
2. Förfarande enligt patentkravet 1, känne-te c k n a t därav, att n är 0.
3. Förfarande enligt patentkravet 1 eller 2, kännetecknat därav, att R1 är väte.
4. Förfarande enligt patentkraven 1-3, k ä n n e-10 tecknat därav, att R2 och R3 är lika eller olika och är väte, metyl eller etyl.
5. Förfarande enligt patentkravet 1, känne-te c k n a t därav, att den framställda föreningen är 17-estramustin-N,N-dietylaminoacetat, 15 17-estramustin-4-(N,N-dimetylamino)butyrat, 17-estramustin-N-metylaminoacetat, 17-estramustinaminoacetat, 17-estramustin-2-aminopropionat, 17-estramustin-N-etylaminoacetat, 20 17-estramustin-N-(2-propyl)aminoacetat, 17-estramustin-3-aminopropionat eller 17-estramustin-N-(1-propyl)aminoacetat.
6. Förfarande enligt patentkravet 1, känne-te c k n a t därav, att den framställda föreningen är * 25 17-estramustin-N-metylaminoacetat-hydroklorid, 17-estramustinaminoacetat-hydroklorid, 17-estramustin-N-metylaminoacetat-metansulfonat, 17-estramustinaminoacetat-metansulfonat, 17-estramustin-N-metylaminoacetat-etansulfonat eller 30 17-estramustinaminoacetat-etansulfonat. * »
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE8802402 | 1988-06-28 | ||
| SE8802402A SE8802402D0 (sv) | 1988-06-28 | 1988-06-28 | Novel esters |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| FI893130A0 FI893130A0 (sv) | 1989-06-27 |
| FI893130A FI893130A (sv) | 1989-12-29 |
| FI92707B true FI92707B (sv) | 1994-09-15 |
| FI92707C FI92707C (sv) | 1994-12-27 |
Family
ID=20372746
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FI893130A FI92707C (sv) | 1988-06-28 | 1989-06-27 | Förfarande för framställning av nya terapeutiskt användbara estramustinestrar |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US5036062A (sv) |
| EP (1) | EP0351561B1 (sv) |
| JP (1) | JP2563587B2 (sv) |
| KR (1) | KR910000607A (sv) |
| CN (1) | CN1031060C (sv) |
| AT (1) | ATE96446T1 (sv) |
| CA (1) | CA1317587C (sv) |
| DD (1) | DD284026A5 (sv) |
| DE (1) | DE68910211T2 (sv) |
| DK (1) | DK318989A (sv) |
| ES (1) | ES2059626T3 (sv) |
| FI (1) | FI92707C (sv) |
| HU (1) | HU203766B (sv) |
| IE (1) | IE62462B1 (sv) |
| IL (1) | IL90724A0 (sv) |
| LT (1) | LT3548B (sv) |
| LV (1) | LV10235B (sv) |
| MD (1) | MD940402A (sv) |
| NO (1) | NO172939C (sv) |
| NZ (1) | NZ229649A (sv) |
| PH (1) | PH30437A (sv) |
| PT (1) | PT90986B (sv) |
| RU (1) | RU2036929C1 (sv) |
| SE (1) | SE8802402D0 (sv) |
| ZA (1) | ZA894716B (sv) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5209926A (en) * | 1990-06-12 | 1993-05-11 | Insite Vision Incorporated | Aminosteroids for ophthalmic use |
| US5252319A (en) * | 1990-06-12 | 1993-10-12 | Insite Vision Incorporated | Aminosteroids for ophthalmic use |
| US5256408A (en) * | 1990-06-12 | 1993-10-26 | Insite Vision Incorporated | Aminosteroids for ophthalmic use |
| US5124154A (en) * | 1990-06-12 | 1992-06-23 | Insite Vision Incorporated | Aminosteroids for ophthalmic use |
| JP2520074B2 (ja) * | 1992-06-11 | 1996-07-31 | 呉羽化学工業株式会社 | 新規なエストラジオ―ル誘導体−クロラムブチル結合体、その製造方法、及び医薬製剤 |
| JPH07101977A (ja) * | 1993-10-05 | 1995-04-18 | Kureha Chem Ind Co Ltd | ホルモン作用を軽減した新規なエストラジオール誘導体及びその増殖因子阻害剤 |
| FR2717690B1 (fr) * | 1994-03-24 | 1996-04-26 | Roussel Uclaf | Application de stéroïdes aromatiques 3 substitués par un aminoalcoxy substitué à l'obtention d'un médicament pour contrôler la stérilité, notamment masculine. |
| GB9419153D0 (en) * | 1994-09-22 | 1994-11-09 | Erba Carlo Spa | Estramustine formulations with improved pharmaceutical properties |
| US20030108764A1 (en) * | 2001-12-04 | 2003-06-12 | Neill John Thomas | Method for improving bonding of circuit board substrates to metal surfaces and the articles formed thereby |
| CN101463295B (zh) * | 2008-11-28 | 2011-08-17 | 江苏海迅实业集团股份有限公司 | 半导体工业用清洗剂 |
| EP3019172B1 (en) | 2013-07-11 | 2019-09-25 | Evestra, Inc. | Pro-drug forming compounds |
| WO2019078983A1 (en) | 2017-10-19 | 2019-04-25 | Evestra, Inc. | CONTRACEPTIVES OF PROGESTINE PRODRANT WITH EXTENDED ACTION |
| CN112979744B (zh) * | 2021-02-18 | 2022-02-15 | 齐齐哈尔医学院 | 具有抗肿瘤活性的薯蓣皂苷元拼合氮芥衍生物及其制备方法和用途 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1126386B (de) * | 1959-11-14 | 1962-03-29 | Hoechst Ag | Verfahren zur Herstellung von Steroid-21-aminosaeureestern |
| US3299104A (en) * | 1963-04-09 | 1967-01-17 | Leo Ab | Certain steroid nu-bis-(haloethyl)-carbamates |
| US4443440A (en) * | 1982-08-30 | 1984-04-17 | The Upjohn Company | Amine containing ester prodrugs of corticosteroids |
| US4615835A (en) * | 1983-11-17 | 1986-10-07 | Stiftung Deutsches Krebsforschungs Zentrum | Steroid esters of N-(2-halogenethyl)-N-nitroso-carbamoylamino and acids and peptides therefore, as well as method for preparing them |
| JPS617292A (ja) * | 1984-06-20 | 1986-01-13 | Japan Atom Energy Res Inst | 制癌剤を結合させたエストラサイト系化合物を製造する方法 |
-
1988
- 1988-06-28 SE SE8802402A patent/SE8802402D0/sv unknown
-
1989
- 1989-06-13 IE IE190889A patent/IE62462B1/en not_active IP Right Cessation
- 1989-06-13 US US07/365,436 patent/US5036062A/en not_active Expired - Fee Related
- 1989-06-16 CA CA000603014A patent/CA1317587C/en not_active Expired - Fee Related
- 1989-06-19 EP EP89111062A patent/EP0351561B1/en not_active Expired - Lifetime
- 1989-06-19 DE DE89111062T patent/DE68910211T2/de not_active Expired - Fee Related
- 1989-06-19 ES ES89111062T patent/ES2059626T3/es not_active Expired - Lifetime
- 1989-06-19 AT AT89111062T patent/ATE96446T1/de not_active IP Right Cessation
- 1989-06-21 NZ NZ229649A patent/NZ229649A/en unknown
- 1989-06-21 ZA ZA894716A patent/ZA894716B/xx unknown
- 1989-06-23 IL IL90724A patent/IL90724A0/xx not_active IP Right Cessation
- 1989-06-27 RU SU894614513A patent/RU2036929C1/ru active
- 1989-06-27 FI FI893130A patent/FI92707C/sv not_active IP Right Cessation
- 1989-06-27 NO NO892672A patent/NO172939C/no unknown
- 1989-06-27 DD DD89330011A patent/DD284026A5/de not_active IP Right Cessation
- 1989-06-27 HU HU893235A patent/HU203766B/hu not_active IP Right Cessation
- 1989-06-27 DK DK318989A patent/DK318989A/da not_active Application Discontinuation
- 1989-06-27 CN CN89104490A patent/CN1031060C/zh not_active Expired - Fee Related
- 1989-06-27 PT PT90986A patent/PT90986B/pt not_active IP Right Cessation
- 1989-06-27 JP JP1162850A patent/JP2563587B2/ja not_active Expired - Lifetime
- 1989-06-27 PH PH38864A patent/PH30437A/en unknown
- 1989-06-28 KR KR1019890009004A patent/KR910000607A/ko active IP Right Grant
-
1993
- 1993-06-02 LT LTIP603A patent/LT3548B/lt not_active IP Right Cessation
- 1993-06-08 LV LVP-93-514A patent/LV10235B/xx unknown
-
1994
- 1994-07-14 MD MD94-0402A patent/MD940402A/ro unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Patent granted |
Owner name: PHARMACIA AB |
|
| BB | Publication of examined application | ||
| PC | Transfer of assignment of patent |
Owner name: PHARMACIA AB |
|
| MM | Patent lapsed | ||
| MM | Patent lapsed |
Owner name: PHARMACIA AB |