SI9500295B - 17-desoxy-corticosteroid-21-/O/-carboxy acid esters, process for their preparation and medicaments containing them - Google Patents
17-desoxy-corticosteroid-21-/O/-carboxy acid esters, process for their preparation and medicaments containing them Download PDFInfo
- Publication number
- SI9500295B SI9500295B SI9500295A SI9500295A SI9500295B SI 9500295 B SI9500295 B SI 9500295B SI 9500295 A SI9500295 A SI 9500295A SI 9500295 A SI9500295 A SI 9500295A SI 9500295 B SI9500295 B SI 9500295B
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- Slovenia
- Prior art keywords
- formula
- methyl
- hydrogen
- compound
- salt
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
- C07J5/0007—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa
- C07J5/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa not substituted in position 16
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J33/00—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J33/002—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- 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
- C07J41/005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
-
- 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
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (5)
1 Patentni zahtevki 1. 17-Deoksikortikoid-21-dikarboksilni ester s formulo I o i 21 CH2—O — C—X —R(l)
R(2) v kateri je: A CHOH, CH2 ali C=0; X (C2-C4) alifatski ogljikovodik, enkrat ali več kot enkrat nenasičen; Y vodik, fluor ali klor; Z vodik, fluor ali metil: R(l) v danem primeru substituiran ali pripojen aril ali hetanl; in R(2) vodik ali α-metil ali β-metil.
2. 17-Deoksikortikoid-21-karboksilni ester po zahtevku 1, označen s tem, da v njem pomenijo: R(l) je definiran kot v zahtevku 1; A CHOH kot β konfiguriran; Y F; Z vodik; R(2) a-metil. 2
3. Postopek za pripravo spojine s formulo I, kot je zahtevana v zahtevku 1, ki obsega: a) presnovo spojine s formulo II 21 CH2—R(4) II co
v kateri je R(4) enak OH in so preostali substituenti kot so definirani v zahtevku 1, al) z aktivirano karboksilno kislino s formulo III, prednostno halidom ali anhidridom ali azolidom R(5)—CO—X-R(l) III pri čemer sta X in R(l) kot sta definirana v zahtevku 1, in je R(5) Cl, Br, 0[—CO—X—R(l)]- ali —OC—(0)CF3 ali drug aktiviran kislinski radikal, ali a2) s samo karboksilno kislino s formulo III, v kateri je R(5) OH in so nadaljnji substituenti navedeni pri formuli III; v prisotnosti reagentov, ki odcepljajo vodo, kot je DCC1 in podobni, ali 3
v kateri je R(4) Br, J ali sulfonska aril esterska skupina ali sulfonska alkil esterska skupina, in so drugi substituenti kot so definirani v zahtevku 1, presnovimo s soljo, prednostno K- ali Na-soljo ali trialkilamonijevo soljo, karboksilne kisline s formulo III R(5)-CO—X—R(l) III v kateri je R(5) —[OMe+] in imajo nadaljnji substituenti pri formuli III podane pomene, pri čemer je Me+ prednostno kation alkalijske soli ali trialkilamonijeve soli.
4. Farmacevtski sestavek, ki obsega učinkovito količino spojine s formulo I, kot je zahtevana v zahtevku 1, skupaj s farmacevtsko sprejemljivim nosilcem.
5. Uporaba spojine I po zahtevku 1 za pripravo zdravila za zdravljenje dermatoz.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4433374A DE4433374A1 (de) | 1994-09-20 | 1994-09-20 | 17-Desoxi-corticosteroid-21-/O/-Carbonsäure- ester, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| SI9500295A SI9500295A (en) | 1996-04-30 |
| SI9500295B true SI9500295B (en) | 2001-12-31 |
Family
ID=6528610
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI9500295A SI9500295B (en) | 1994-09-20 | 1995-09-20 | 17-desoxy-corticosteroid-21-/O/-carboxy acid esters, process for their preparation and medicaments containing them |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US5824670A (sl) |
| EP (1) | EP0708111B1 (sl) |
| JP (1) | JP3902255B2 (sl) |
| KR (1) | KR100406627B1 (sl) |
| CN (1) | CN1056151C (sl) |
| AT (1) | ATE188480T1 (sl) |
| AU (1) | AU695710B2 (sl) |
| CA (1) | CA2158610C (sl) |
| CZ (1) | CZ288297B6 (sl) |
| DE (2) | DE4433374A1 (sl) |
| DK (1) | DK0708111T3 (sl) |
| ES (1) | ES2140596T3 (sl) |
| FI (1) | FI114708B (sl) |
| GR (1) | GR3032688T3 (sl) |
| HU (1) | HU217438B (sl) |
| IL (1) | IL115331A (sl) |
| NO (1) | NO305210B1 (sl) |
| NZ (1) | NZ280038A (sl) |
| PL (1) | PL186071B1 (sl) |
| PT (1) | PT708111E (sl) |
| RU (1) | RU2161624C2 (sl) |
| SI (1) | SI9500295B (sl) |
| TW (1) | TW424094B (sl) |
| ZA (1) | ZA957877B (sl) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2596007B1 (en) | 2010-07-20 | 2016-01-06 | Taro Pharmaceutical Industries Ltd | Process for the preparation of 17-desoxy-corticosteroids |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2755292A (en) * | 1952-01-21 | 1956-07-17 | Organon Labor Ltd | Phenyl propionate of testosterone |
| US2783226A (en) * | 1955-02-03 | 1957-02-26 | Schering Corp | Esters of cortical hormones |
| ES229413A1 (es) * | 1956-06-22 | 1956-11-01 | Francisco Vismara S P A | UN PROCEDIMIENTO PARA LA PREPARACIoN DE COMPUESTOS ESTEROIDALES QUE CONTENGAN UN GRUPO CEToLICO EN LA CADENA LATERAL |
| DE1131668B (de) * | 1959-07-16 | 1962-06-20 | Leo Ab | Verfahren zur Herstellung von Estern von Corticosteroid-Hormonen |
| CH495969A (de) * | 1965-11-09 | 1970-09-15 | Schering Ag | Verfahren zur Herstellung neuer 21-Ester von 16a-Methyl-21-hydroxy- 1,4-steroiden |
| DE2047105C3 (de) * | 1970-09-18 | 1979-02-15 | Schering Ag, 1000 Berlin Und 4619 Bergkamen | 17-Chlorsteroide und Verfahren zu ihrer Herstellung |
| US3956349A (en) * | 1975-02-18 | 1976-05-11 | Syntex (U.S.A.) Inc. | Process for preparing 3-enol ethers of 11β-hydroxy-Δ4 -pregnene-3-ones and derivatives thereof |
| FR2342738A1 (fr) * | 1976-03-02 | 1977-09-30 | Roussel Uclaf | Nouveaux derives halogenes de la serie du 16a-methyl pregnane |
| DE2617655C2 (de) * | 1976-04-21 | 1984-11-08 | F. Hoffmann-La Roche & Co Ag, Basel | Kortikoide, Verfahren zu deren Herstellung und diese enthaltende pharmazeutische Präparate |
| DE2645104C2 (de) * | 1976-10-04 | 1986-04-24 | Schering AG, 1000 Berlin und 4709 Bergkamen | 11β-Hydroxy-1,4,8-pregnatrien-3,20-dion-Derivate und Verfahren zu ihrer Herstellung |
| FR2381065A2 (fr) * | 1977-02-22 | 1978-09-15 | Roussel Uclaf | Nouveaux derives halogenes de la serie du 16 a-methyl pregnane |
| US4086254A (en) * | 1977-04-13 | 1978-04-25 | The Upjohn Company | Photocleavable steroids |
| LU77457A1 (sl) * | 1977-05-31 | 1979-01-19 | ||
| US4377573A (en) * | 1978-01-06 | 1983-03-22 | Leveen Harry H | Method of control of gastrointestinal bleeding |
| DE2817988A1 (de) * | 1978-04-25 | 1979-11-08 | Hoechst Ag | Corticoid 17-alkylcarbonate und verfahren zu deren herstellung |
| DE2920726A1 (de) * | 1979-05-18 | 1980-11-27 | Schering Ag | Neue kortikoide, ihre herstellung und verwendung |
| CY1359A (en) * | 1981-02-02 | 1987-08-07 | Schering Corp | Aromatic heterocyclic esters of steroids, their preparation and pharmaceutical compositions containing them |
| SE8303031D0 (sv) * | 1983-05-30 | 1983-05-30 | Leo Ab | Improved steroid esters preparation |
| US4910191A (en) * | 1988-06-28 | 1990-03-20 | Merrell Dow Pharmaceuticals Inc. | 19-substituted progesterone derivatives useful as 19-hydroxylase inhibitors |
| US4920114A (en) * | 1988-06-28 | 1990-04-24 | Merrell Dow Pharmaceuticals Inc. | 19-fluoro- or cyano-21-hydroxyprogesterone derivatives useful as 19-hydroxylase inhibitors |
| NZ237559A (en) * | 1990-04-02 | 1993-04-28 | Merrell Dow Pharma | Halogenoethyl steroid derivatives and pharmaceutical compositions |
-
1994
- 1994-09-20 DE DE4433374A patent/DE4433374A1/de not_active Withdrawn
-
1995
- 1995-09-08 TW TW084109384A patent/TW424094B/zh not_active IP Right Cessation
- 1995-09-15 AT AT95114511T patent/ATE188480T1/de active
- 1995-09-15 ES ES95114511T patent/ES2140596T3/es not_active Expired - Lifetime
- 1995-09-15 DE DE59507565T patent/DE59507565D1/de not_active Expired - Lifetime
- 1995-09-15 DK DK95114511T patent/DK0708111T3/da active
- 1995-09-15 PT PT95114511T patent/PT708111E/pt unknown
- 1995-09-15 EP EP95114511A patent/EP0708111B1/de not_active Expired - Lifetime
- 1995-09-18 CZ CZ19952425A patent/CZ288297B6/cs not_active IP Right Cessation
- 1995-09-18 US US08/529,668 patent/US5824670A/en not_active Expired - Lifetime
- 1995-09-18 CN CN95116294A patent/CN1056151C/zh not_active Expired - Fee Related
- 1995-09-18 AU AU31728/95A patent/AU695710B2/en not_active Ceased
- 1995-09-18 NZ NZ280038A patent/NZ280038A/en not_active IP Right Cessation
- 1995-09-18 FI FI954394A patent/FI114708B/fi not_active IP Right Cessation
- 1995-09-18 IL IL11533195A patent/IL115331A/en not_active IP Right Cessation
- 1995-09-19 JP JP23939895A patent/JP3902255B2/ja not_active Expired - Fee Related
- 1995-09-19 HU HU9502735A patent/HU217438B/hu not_active IP Right Cessation
- 1995-09-19 ZA ZA957877A patent/ZA957877B/xx unknown
- 1995-09-19 RU RU95116371/04A patent/RU2161624C2/ru not_active IP Right Cessation
- 1995-09-19 CA CA002158610A patent/CA2158610C/en not_active Expired - Fee Related
- 1995-09-19 NO NO953695A patent/NO305210B1/no not_active IP Right Cessation
- 1995-09-19 PL PL95310544A patent/PL186071B1/pl not_active IP Right Cessation
- 1995-09-20 SI SI9500295A patent/SI9500295B/sl unknown
- 1995-09-20 KR KR1019950030850A patent/KR100406627B1/ko not_active IP Right Cessation
-
2000
- 2000-02-18 GR GR20000400386T patent/GR3032688T3/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| IF | Valid on the event date |