GB1452794A - Estriol derivatives - Google Patents
Estriol derivativesInfo
- Publication number
- GB1452794A GB1452794A GB871274A GB871274A GB1452794A GB 1452794 A GB1452794 A GB 1452794A GB 871274 A GB871274 A GB 871274A GB 871274 A GB871274 A GB 871274A GB 1452794 A GB1452794 A GB 1452794A
- Authority
- GB
- United Kingdom
- Prior art keywords
- estriol
- nicotinoyl
- dinicotinate
- esterification
- feb
- 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.)
- Expired
Links
- 150000002166 estriols Chemical class 0.000 title 1
- PROQIPRRNZUXQM-UHFFFAOYSA-N (16alpha,17betaOH)-Estra-1,3,5(10)-triene-3,16,17-triol Natural products OC1=CC=C2C3CCC(C)(C(C(O)C4)O)C4C3CCC2=C1 PROQIPRRNZUXQM-UHFFFAOYSA-N 0.000 abstract 4
- 229960001348 estriol Drugs 0.000 abstract 4
- -1 Estriol nicotinates Chemical class 0.000 abstract 3
- PROQIPRRNZUXQM-ZXXIGWHRSA-N estriol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)C4)O)[C@@H]4[C@@H]3CCC2=C1 PROQIPRRNZUXQM-ZXXIGWHRSA-N 0.000 abstract 3
- 150000001204 N-oxides Chemical class 0.000 abstract 2
- 125000002252 acyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000032050 esterification Effects 0.000 abstract 2
- 238000005886 esterification reaction Methods 0.000 abstract 2
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 abstract 1
- 239000000443 aerosol Substances 0.000 abstract 1
- 125000002723 alicyclic group Chemical group 0.000 abstract 1
- 125000001931 aliphatic group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 239000000969 carrier Substances 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 230000007062 hydrolysis Effects 0.000 abstract 1
- 238000006460 hydrolysis reaction Methods 0.000 abstract 1
- 230000000055 hyoplipidemic effect Effects 0.000 abstract 1
- 125000005394 methallyl group Chemical group 0.000 abstract 1
- 235000001968 nicotinic acid Nutrition 0.000 abstract 1
- 150000004965 peroxy acids Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- ATBIAJXSKNPHEI-UHFFFAOYSA-N pyridine-3-carbonyl chloride Chemical compound ClC(=O)C1=CC=CN=C1 ATBIAJXSKNPHEI-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Obesity (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
1452794 Estriol nicotinates THERAMEX SA 26 Feb 1975 [26 Feb 1974] 8712/74 Heading C2U The invention comprises compounds of formula (wherein R is nicotinoyl or its N-oxide; and R<SP>1</SP> is C 3-7 aliphatic organic acyl; aromatic, alicyclic or heterocyclic organic acyl; or Me, Et, Pr, allyl, methallyl, cyclopentyl or dialkylaminoalkyl); and their preparation from estriol or its 3-ethers by esterification with nicotinoyl chloride or its N-oxide; or from estriol 16,17- dinicotinate or its N,N<SP>1</SP>-dioxide by esterification with an appropriate acylating agent. The nicotinoyl groups may be N-oxidized by reaction with per-acids. Estriol 16,17-dinicotinate is prepared by selective hydrolysis of the trinicotinate. Compounds I are credited with hypolipidaemic and anti-arteriosclerotic activity, and may be made up with carriers into pharmaceutical compositions for oral, parenteral, rectal and nasal (aerosol) administration.
Priority Applications (15)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB871274A GB1452794A (en) | 1974-02-26 | 1974-02-26 | Estriol derivatives |
| AR257778A AR206704A1 (en) | 1974-02-26 | 1975-01-01 | PROCEDURE FOR THE PREPARATION OF NEW DERIVATIVES OF 16,17-DI-DICOTINOIL-ESTRIOL AND ITS N-OXODES |
| FR7503357A FR2261775B1 (en) | 1974-02-26 | 1975-02-04 | |
| CH171975A CH614218A5 (en) | 1974-02-26 | 1975-02-11 | Process for the preparation of estriol derivatives |
| ES434961A ES434961A1 (en) | 1974-02-26 | 1975-02-21 | Estriol derivatives |
| IT20627/75A IT1048803B (en) | 1974-02-26 | 1975-02-25 | NICOTINIC DERIVATIVES OF ESTRIOL HAVING HYPOLIPIDEMIC AND MODULATED EXTROGEN ACTIVITY |
| SE7502107A SE419091B (en) | 1974-02-26 | 1975-02-25 | PROCEDURE FOR THE PREPARATION OF NICOTIC ACID ESTERS AND DERIVATIVES OF OSTRIOL |
| CA220,864A CA1062699A (en) | 1974-02-26 | 1975-02-25 | Nicotinic dervatives of estriol having modified hypolipidimic and estrogenic activity |
| BR1131/75A BR7501131A (en) | 1974-02-26 | 1975-02-25 | NEW STRIOL DERIVED COMPOUNDS PROCESS FOR ITS PREPARATION AND APPLICATION IN HUMAN MEDICINE FOR HYPOLIPIDEMIANT AND ANTI-ATEROESCLEROTIC ESTROGENIC TREATMENTS |
| LU71909A LU71909A1 (en) | 1974-02-26 | 1975-02-25 | |
| IE384/75A IE40689B1 (en) | 1974-02-26 | 1975-02-25 | Novel estriol derivatives |
| BE153773A BE826016A (en) | 1974-02-26 | 1975-02-26 | NEW NICOTINIC DERIVATIVES OF ESTRIOL WITH HYPOLIPIDEMITING ACTIVITIES AND MODULATED ESTROGEN |
| NLAANVRAGE7502299,A NL180108C (en) | 1974-02-26 | 1975-02-26 | PROCESS FOR PREPARING A MEDICINAL PRODUCT BASED ON A 3,16-ALFA, 17BETA TRIHYDROXY-1,3,5 (10) OESTRATRY NESTER AND METHOD FOR PREPARING THE SUITABLE COMPOUND. |
| JP50024452A JPS5842199B2 (en) | 1974-02-26 | 1975-02-26 | ESTRIO-RUUUDOUTAINO |
| US05/736,931 US4110324A (en) | 1974-02-26 | 1976-10-29 | Nicotinic derivatives of estriol |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB871274A GB1452794A (en) | 1974-02-26 | 1974-02-26 | Estriol derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| GB1452794A true GB1452794A (en) | 1976-10-13 |
Family
ID=9857798
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB871274A Expired GB1452794A (en) | 1974-02-26 | 1974-02-26 | Estriol derivatives |
Country Status (14)
| Country | Link |
|---|---|
| JP (1) | JPS5842199B2 (en) |
| AR (1) | AR206704A1 (en) |
| BE (1) | BE826016A (en) |
| BR (1) | BR7501131A (en) |
| CA (1) | CA1062699A (en) |
| CH (1) | CH614218A5 (en) |
| ES (1) | ES434961A1 (en) |
| FR (1) | FR2261775B1 (en) |
| GB (1) | GB1452794A (en) |
| IE (1) | IE40689B1 (en) |
| IT (1) | IT1048803B (en) |
| LU (1) | LU71909A1 (en) |
| NL (1) | NL180108C (en) |
| SE (1) | SE419091B (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS60258198A (en) * | 1984-06-04 | 1985-12-20 | Amano Pharmaceut Co Ltd | Triterpene alcohol organic acid ester and its preparation |
-
1974
- 1974-02-26 GB GB871274A patent/GB1452794A/en not_active Expired
-
1975
- 1975-01-01 AR AR257778A patent/AR206704A1/en active
- 1975-02-04 FR FR7503357A patent/FR2261775B1/fr not_active Expired
- 1975-02-11 CH CH171975A patent/CH614218A5/en not_active IP Right Cessation
- 1975-02-21 ES ES434961A patent/ES434961A1/en not_active Expired
- 1975-02-25 IE IE384/75A patent/IE40689B1/en unknown
- 1975-02-25 LU LU71909A patent/LU71909A1/xx unknown
- 1975-02-25 SE SE7502107A patent/SE419091B/en not_active IP Right Cessation
- 1975-02-25 BR BR1131/75A patent/BR7501131A/en unknown
- 1975-02-25 CA CA220,864A patent/CA1062699A/en not_active Expired
- 1975-02-25 IT IT20627/75A patent/IT1048803B/en active
- 1975-02-26 BE BE153773A patent/BE826016A/en unknown
- 1975-02-26 NL NLAANVRAGE7502299,A patent/NL180108C/en not_active IP Right Cessation
- 1975-02-26 JP JP50024452A patent/JPS5842199B2/en not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| NL180108C (en) | 1987-01-02 |
| IT1048803B (en) | 1980-12-20 |
| JPS50142555A (en) | 1975-11-17 |
| JPS5842199B2 (en) | 1983-09-17 |
| NL7502299A (en) | 1975-08-28 |
| FR2261775A1 (en) | 1975-09-19 |
| BR7501131A (en) | 1975-12-02 |
| SE419091B (en) | 1981-07-13 |
| SE7502107L (en) | 1975-08-27 |
| CA1062699A (en) | 1979-09-18 |
| IE40689B1 (en) | 1979-08-01 |
| NL180108B (en) | 1986-08-01 |
| ES434961A1 (en) | 1976-12-16 |
| CH614218A5 (en) | 1979-11-15 |
| LU71909A1 (en) | 1975-08-20 |
| FR2261775B1 (en) | 1980-05-16 |
| AR206704A1 (en) | 1976-08-13 |
| IE40689L (en) | 1975-08-26 |
| BE826016A (en) | 1975-06-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| IE37538B1 (en) | New 1,4-dihydropyridine carboxylic acid compounds their production and their medicinal use | |
| GB1511366A (en) | Aliphatic carboxylic acid esters of vitamin e and process for preparation thereof | |
| HUP9801828A2 (en) | Benzoic acid, quinoline and quinazoline derivatives, pharmaceutical preparations containing them and a process for their production | |
| ES472384A1 (en) | Substituted amino-pyridine derivatives, processes for their preparation and pharmaceutical compositions containing them. | |
| ES463803A1 (en) | O-[3-(4-Substituted-piperazin-1-yl)-2-hydroxypropyl]-hydroxylamines | |
| MY128642A (en) | Process for the production of anhydrous formic acid | |
| IE782084L (en) | Quinolylguanidine derivatives | |
| HUP9701660A2 (en) | 10,13,15-trioxatricyclo[9.2.1.1.9.6]pentadekanon derivatives, process for producing them, and pharmaceutical compositions containing them | |
| GB1363719A (en) | Diglycidyl derivatives of compounds containing two n-heterocyclic rings processes for the production of the derivatives and the use thereof | |
| ES458307A1 (en) | Aminopiperidines, their production and the pharmaceutical compositions incorporating them | |
| GB1452794A (en) | Estriol derivatives | |
| GB1447462A (en) | Alpha-thiolincosaminides and the preparation thereof | |
| ES8401926A1 (en) | Hydroxybenzylamino-aryl compounds, process for preparing and pharmaceutical compositions containing the same. | |
| GB1379867A (en) | Triamcinolone derivative | |
| GB1389505A (en) | 3,4-dihydropyridones their production and their medicinal use | |
| FR2333508A1 (en) | NEW DERIVATIVES OF 3-AZA-BICYCLO (3.1.0) HEXANE, THEIR PREPARATION AND THEIR APPLICATION AS MEDICINAL PRODUCTS | |
| ES8200347A1 (en) | Pyridine derivatives, process for their preparation and medicaments containing them. | |
| FR2228064A1 (en) | 4-amino-2,6-dihydroxy-(di or tri-alkoxy)-benzyl-pyrimidines - and derivs - intermediates for pharmaceuticals | |
| ES419782A1 (en) | Esters and amides of 3-aryl-1,4 benzodioxan-2-carboxylic acids | |
| GB1420533A (en) | Pyridine derivatives having juvenile hormone activity | |
| GB1471276A (en) | 5-benzylpicolinic acid deri vatives | |
| GB1444879A (en) | 3-acylamino-6-amino-3,4-dihydro-2-pyridones and their use as medicaments | |
| IE39049B1 (en) | New 1,4-dihydroquinoline derivatives their production and their medicinal use | |
| FR2216288A1 (en) | Cephalosporin acetoxymethyl esters - useful as antibacterials and cephalosporin inters | |
| IE36278B1 (en) | Pharmaceutical compositions containing benzofuran derivatives |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PS | Patent sealed [section 19, patents act 1949] | ||
| PCNP | Patent ceased through non-payment of renewal fee |