DK169162B1 - Anvendelse af antigestagener til fremstilling af lægemidler til terapi og profylakse af dysmenoréisk besvær samt til behandling af forstyrrelser og besvær fremkaldt af endometriose - Google Patents
Anvendelse af antigestagener til fremstilling af lægemidler til terapi og profylakse af dysmenoréisk besvær samt til behandling af forstyrrelser og besvær fremkaldt af endometriose Download PDFInfo
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- DK169162B1 DK169162B1 DK487287A DK487287A DK169162B1 DK 169162 B1 DK169162 B1 DK 169162B1 DK 487287 A DK487287 A DK 487287A DK 487287 A DK487287 A DK 487287A DK 169162 B1 DK169162 B1 DK 169162B1
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- Prior art keywords
- hydroxy
- disorders
- dimethylamino
- phenyl
- dysmenorrhea
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- 239000003418 antiprogestin Substances 0.000 title claims abstract description 9
- 239000003814 drug Substances 0.000 title claims abstract description 6
- 229940079593 drug Drugs 0.000 title claims abstract description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims description 10
- 208000035475 disorder Diseases 0.000 title claims description 10
- 208000005171 Dysmenorrhea Diseases 0.000 title claims description 9
- 206010013935 Dysmenorrhoea Diseases 0.000 title claims description 9
- 238000004519 manufacturing process Methods 0.000 title claims description 7
- 238000002560 therapeutic procedure Methods 0.000 title claims description 6
- 238000011282 treatment Methods 0.000 title claims description 6
- 201000009273 Endometriosis Diseases 0.000 title claims description 4
- 238000011321 prophylaxis Methods 0.000 title claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 17
- 108091007433 antigens Proteins 0.000 claims description 14
- 239000000427 antigen Substances 0.000 claims description 13
- 102000036639 antigens Human genes 0.000 claims description 13
- 150000003180 prostaglandins Chemical class 0.000 abstract description 13
- 230000015572 biosynthetic process Effects 0.000 abstract description 3
- 238000003786 synthesis reaction Methods 0.000 abstract description 2
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 12
- 229940094443 oxytocics prostaglandins Drugs 0.000 description 10
- 229960003387 progesterone Drugs 0.000 description 6
- 239000000186 progesterone Substances 0.000 description 6
- 230000005764 inhibitory process Effects 0.000 description 5
- SESFRYSPDFLNCH-UHFFFAOYSA-N benzyl benzoate Chemical compound C=1C=CC=CC=1C(=O)OCC1=CC=CC=C1 SESFRYSPDFLNCH-UHFFFAOYSA-N 0.000 description 4
- 210000002966 serum Anatomy 0.000 description 4
- 230000000890 antigenic effect Effects 0.000 description 3
- 235000013405 beer Nutrition 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 230000005906 menstruation Effects 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- QOXOZONBQWIKDA-UHFFFAOYSA-N 3-hydroxypropyl Chemical group [CH2]CCO QOXOZONBQWIKDA-UHFFFAOYSA-N 0.000 description 2
- 241000700198 Cavia Species 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 229960002903 benzyl benzoate Drugs 0.000 description 2
- 239000004359 castor oil Substances 0.000 description 2
- 235000019438 castor oil Nutrition 0.000 description 2
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 210000000056 organ Anatomy 0.000 description 2
- 230000035935 pregnancy Effects 0.000 description 2
- 239000000583 progesterone congener Substances 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 150000003431 steroids Chemical class 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 210000004291 uterus Anatomy 0.000 description 2
- 229910002012 Aerosil® Inorganic materials 0.000 description 1
- 101500021169 Aplysia californica Myomodulin-G Proteins 0.000 description 1
- VNGFJSASHMIDOP-IGPMMVRKSA-N C1CC2=CC(=O)CCC2=C2[C@@H]1[C@@H]1CC(CCCO)C[C@]1(C)CC2 Chemical compound C1CC2=CC(=O)CCC2=C2[C@@H]1[C@@H]1CC(CCCO)C[C@]1(C)CC2 VNGFJSASHMIDOP-IGPMMVRKSA-N 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 206010028347 Muscle twitching Diseases 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 208000036029 Uterine contractions during pregnancy Diseases 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 230000036770 blood supply Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 230000008602 contraction Effects 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 210000004246 corpus luteum Anatomy 0.000 description 1
- 239000007933 dermal patch Substances 0.000 description 1
- 230000001627 detrimental effect Effects 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 210000004696 endometrium Anatomy 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 230000029849 luteinization Effects 0.000 description 1
- 230000029860 luteolysis Effects 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000000044 progesterone antagonist Substances 0.000 description 1
- 102000003998 progesterone receptors Human genes 0.000 description 1
- 108090000468 progesterone receptors Proteins 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 239000000003 vaginal tablet Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Description
DK 169162 B1
Opfindelsen angår anvendelse af antigestagener til fremstilling af lægemidler til terapi og profylakse af dysmenoréisk besvær samt til behandling af forstyrrelser og besvær fremkaldt af endometriose.
5 Virksomme antigestagener er f.eks. kendt fra europæisk patentskrift 0 057 115 (Roussel-Uclaf).
Særligt indgående blev undersøgt den som RU 486 betegnede ll|3r-[ (4-N,N-dimethylamino) phenyl] -17&-hydroxy-17a-propinyl-4,9 (10) -østradien-3-on. Angivelser om virkningsmekanismen af RU 486 10 findes i "Human Reproduction", bind 1 (1986), 107 - 110. Ifølge denne bevirker antigestagenet en blokering af progesteron-aktiviteten og en stigning i prostaglandindannelsen, hvorved prostaglandinet stimulerer uteruskontraktiliteten. Med RU 486 er der allerede udført kliniske undersøgelser til afslutning af 15 et svangerskab.
Det har nu vist sig, at modsat den hidtidige antagelse hæmmer antigestagener den uterine produktion af prostaglandiner (PG).
Denne virkning blev iagttaget på ikke-gravide marsvin.
Den af uterine PG ved afslutningen af den ca. 16 dages cyklus 20 følgende luteolyse blev blokeret af antigestagener. Der fremkom et forløb af serum-progesteronværdien, som ellers kun haves under graviditet. En skadelig indvirkning på det normale cyklusforløb gennem hæmmet PG-produktion efter antigestagen-indgivelse forventes imidlertid ikke hos mennesker, da leve-25 tiden af corpus luteum (går til grunde ved cyklusafslutningen) hos kvinder ikke styres af uterus. Man må derimod forvente, at med en hæmning af den uterine PG-frigørelse er en dæmpning af uterusmotorikken, når der foreligger en dysmenoré, mulig.
Fordelen ved denne terapimulighed består i, at et ønskeligt 30 mål af hæmning opnås, uden at PG-funktionen i andre organer berøres.
DK 169162 B1 2
Der opnås en høj grad af organselektivitet ved terapi af dysmenoré med antigestagener.
Antigestagener kan anvendes ved begyndelsen af dysmenoréisk besvær såsom "trækninger i underlivet". Det er ofte menings-5 fuldt at lægge begyndelsen af terapien på noget tidligere faser af lutealfasen for at opnå en tilstrækkelig grad af hæmning.
I en foretrukken udførelsesform foretages antigestagenbehandlingen i reglen gennem 1 - 6, fortrinsvis 1-4 dage, begyndende på menstruationstidspunktet.
Antigestagenerne anvendes ifølge den foreliggende opfindelse i mængder på almindeligvis 2 - 50 mg, fortrinsvis 5 - 20 mg 11β-[ (4-N,N-dimethylamino) phenyl] -17ct-hydroxy-17f3- (3-hydroxypropyl) -13a-methyl-4,9(10)-gonadien-3-on pr. dag eller en biologisk ækvi-25 valent mængde af et andet antigestagen.
Som antigestagener kan der være tale om alle forbindelser, der har en stærk affinitet til gestagenreceptoren (progesteron-receptoren) og derved ikke udviser nogen egen gestagenaktivitet. Som kompetitive progesteron-antagonister kan der 20 f.eks. være tale om følgende steroider: 113- [ (4-N,N-dimethylamino) phenyl] -17f3-hydroxy-l7a-propinyl-4,9(10)-østradien~3-on, 113-[(4-N,N-dimethylamino) phenyl]-173-hydroxy-18-methyl-17a-propinyl-4,9(10)-østradien-3-on og 25 113”[(4-N,N-dimethylamino)phenyl]-17a3~hydroxy-17aa-propinyl-D- homo-4,9(10)-16-østratrien-3-on DK 169162 B1 3 (europæisk patentansøgning 82 400025.1 - offentliggørelses-nummer 0 057 115), 110-methoxyphenyl-170-hydroxy-17a-ethinyl-4,9 (10)-østradien- 3-on 5 (Steroids 37 (1981) 361 - 382), 110-((4-N,N-dimethylamino) phenyl]-173-hydroxy-17a-(hydroxyprop-1-(Z)-enyl)-4,9(10)-østradien-3-on (europæisk patentansøgning 84 7300147.0 - offentliggørelses-nummer 0 147 361), 10 110- t (4-N,N-dimethylamino) phenyl] -17<x-hydroxy-170- (3-hydroxy- propyl)-13a-methyl-4,9(10)-gonadien-3-on (europæisk patentansøgning 84 730062.1 - offentliggørelsesnummer 0 129 499).
Antigestagenerne kan f.eks. indgives lokalt, topisk, enteralt 15 eller parenteralt.
Til den foretrukne orale applikation kan der især være tale om tabletter, drageer, kapsler, piller, suspensioner eller opløsninger, der kan fremstilles på sædvanlig måde med de i galenik-ken sædvanlige tilsætninger og bærerstoffer. Til den lokale 20 eller topiske anvendelse kan der f.eks. være tale om vaginaltabletter eller transdermale systemer såsom hudplastre.
En doseringsenhed indeholder ca. 2 - 50 mg 110-[(4-N,N-dimethylamino) phenyl] -17a-hydroxy-170-(3-hydroxypropyl)-13a-methyl-4,9(10)-gonadien-3-on eller en biologisk ækvivalent mængde af 25 et andet antigestagen.
De følgende eksempler skal belyse den galeniske sammensætning af antigestagener.
DK 169162 B1 4 EKSEMPEL 1.
Sammensætning af en tablet med 10 mg 11β- [ (4-N,N-dimethylamino) -phenyl] -17a-hydroxy-17f3- (3-hydroxypropyl) -13a-methyl-4,9 (10) -gonadien-3-on til oral applikation.
10,0 mg 11β-[(4-N,N-dimethylamino)phenyl]-17a-hydroxy-17£-5 (3-hydroxypropyl)-13a-methyl-4,9(10)-gonadien-3-on 140,5 mg lactose 69,5 mg maj'sstivelse 2,5 mg polyvinylpyrrolidon 25 2,0 mg Aerosil 10 0,5 mg magniumstearat 225,0 mg samlet vægt EKSEMPEL 2.
Sammensætning af en olieagtig opløsning med 50 mg 11β-[(4-Ν,Ν-dimethylamino)phenyl]-17α-hydroxy-17β-(3-hydroxypropyl)-13a-15 methyl-4,9(10)-gonadien-3-on til parenteral applikation- I 1 ml ricinusolie/benzylbenzoat i rumfangsforholdet 6:4 opløses 50 mg af antigestagenet.
Farmakologiske iagttagelser.
Ikke-gravide marsvin fik daglig fra den 8. til den 16. dag i 20 den ca. 16 dages cyklus 10 mg 110-[(4-N,N-dimethylamino)phenyl]-17α-1^^1τοχγ-17β- (3-hydroxypropyl) -l3a-methyl-4,9 (10) -gonadien- 3-on.
DK 169162 B1 5
Prøvestoffet blev opløst i 1 ml benzylbenzoat/ricinusolie (1:2) og injiceret subkutant. Progesteronindholdet i serum blev bestemt daglig.
Af følgende tabel kan ses, at serum-progesteronværdien hos de 5 med antigestagenet behandlede dyr stiger, medens serum-progesteronværdien for de med opløsningsmiddel behandlede kontroller falder stærkt henimod cyklusafslutningen.
Tilsvarende konstateringer fremkom dosisafhængigt for dette stof og også andre antigestagener ved analoge forsøg.
10 Stigningen af progesteron i blodet hos dyr, der blev behandlet med antigestagenet, afspejlede en hæmning af den uterine PG-frigørelse.
Prostaglandiner har en nøglerolle for den normale og patologiske menstruation: 15 Det ses i forbindelse med forandringer i uterusslimhindens blodforsyning og de ve-agtige kontraktioner af uterus under menstruationen. En forøget PG-frigørelse og forøgede uterus-kontraktioner, der kan føles yderst smertefulde, udgør karakteregenskaberne ved en dysmenoré. En hæmning af den uterine PG 20 med antigestagener fjerner eller formindsker i det mindste tydeligt det besvær, der hænger sammen med en dysmenoré. Da den uterine PG-syntese ganske væsentligt finder sted i endometrium, kan det også forventes, at forstyrrelser og besvær, der følger af endometriose, ligeledes kan påvirkes gunstigt 25 med antigestagener.
DK 169162 B1 6
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Claims (4)
1. Anvendelse af antigestagener til fremstilling af lægemidler til terapi og profylakse af dysmenoréisk besvær.
2. Anvendelse af antigestagener til fremstilling af lægemidler til behandling af forstyrrelser og besvær fremkaldt af endo-metriose.
3. Anvendelse af 11β-[ (4-N, N-dimethy lamino) phenyl] -178-hydroxy-17a-propinyl-4,9(10)-østradien-3-on, 11β- [ (4-N,N-dimethylamino) phenyl] -173-hydroxy-18-methyl-17a- 10 propinyl-4,9(10)-østradien-3-on, 11β- [ (4-N,N-dimethylamino) phenyl] -17 a8-hydroxy-17aa-propiny 1-D-homo-4,9(10)-16-Østratrien-3-on, ll(3-methoxyphenyl-173-hydroxy-17a-ethinyl-4,9 (10) -østradien-15 3-on, 11β- [ (4-N, N-dimethy lamino) phenyl] -17p-hydroxy-17a- (hydroxyprop-1-(Z)-enyl)-4,9(10)-østradien-3-on eller 11β- [ (4-N, N-dimethy lamino) phenyl] -17ot-hydroxy-17£- (3-hydroxy-20 Propyl)-13a-methyl-4,9(10)-gonadien-3-on som antigestagener ifølge krav 1 eller 2.
4. Anvendelse af 2 - 50 mg 11/3- [ (4-N, N-dimethylamino) phenyl] -17o;-hydroxy-17j8- (3-hydroxypropyl) -13a!-methyl-4,9 (10) -gonadien- 3-on til fremstilling af et lægemiddel til terapi og profylakse af dysmenoréisk besvær ifølge krav 1 eller til behandling 25 af forstyrrelser og besvær fremkaldt af endometriose ifølge krav 2.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19863633244 DE3633244A1 (de) | 1986-09-26 | 1986-09-26 | Antigestagene zur hemmung der uterinen prostaglandinsynthese |
| DE3633244 | 1986-09-26 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| DK487287D0 DK487287D0 (da) | 1987-09-16 |
| DK487287A DK487287A (da) | 1988-03-27 |
| DK169162B1 true DK169162B1 (da) | 1994-09-05 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK487287A DK169162B1 (da) | 1986-09-26 | 1987-09-16 | Anvendelse af antigestagener til fremstilling af lægemidler til terapi og profylakse af dysmenoréisk besvær samt til behandling af forstyrrelser og besvær fremkaldt af endometriose |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US5744464A (da) |
| EP (1) | EP0266303B1 (da) |
| JP (1) | JP2582088B2 (da) |
| AT (1) | ATE78690T1 (da) |
| AU (1) | AU605177B2 (da) |
| DE (2) | DE3633244A1 (da) |
| DK (1) | DK169162B1 (da) |
| ES (1) | ES2051766T3 (da) |
| GR (1) | GR3005467T3 (da) |
| IE (1) | IE66196B1 (da) |
| IL (1) | IL83967A (da) |
| ZA (1) | ZA877247B (da) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3733478A1 (de) * | 1987-10-01 | 1989-04-13 | Schering Ag | Antigestagen- und antioestrogenwirksame verbindungen zur geburtseinleitung und zum schwangerschaftsabbruch sowie zur behandlung gynaekologischer stoerungen und hormonabhaengiger tumore |
| FR2651435A1 (fr) * | 1989-09-07 | 1991-03-08 | Roussel Uclaf | Nouvelle utilisation de composes anti-progestomimetiques. |
| FR2654337B1 (fr) * | 1989-11-15 | 1994-08-05 | Roussel Uclaf | Nouvelles microspheres injectables biodegradables procede de preparation et suspensions injectables les renfermant. |
| DE19652408C2 (de) * | 1996-12-06 | 2002-04-18 | Schering Ag | Steroidester, Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung von Arzneimitteln |
| ES2295050T3 (es) | 1999-08-31 | 2008-04-16 | Bayer Schering Pharma Aktiengesellschaft | Mesoprogestinas para el tratamiento y la prevencion de trastornos ginecologicos benignos dependientes de hormonas. |
| US20100249125A1 (en) * | 2009-03-31 | 2010-09-30 | The Texas A&M University System | Inhibition of prostglandin e2 receptors for the treatment of endometriosis |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3077437A (en) * | 1957-07-29 | 1963-02-12 | George P Heckel | Pregnanediol for treatment of premenstrual syndrome |
| US3666858A (en) * | 1967-06-29 | 1972-05-30 | Gordon Alan Hughes | Utilization of gon-4-ene therapy in treatment of females and in growth stimulation |
| US4780461A (en) * | 1983-06-15 | 1988-10-25 | Schering Aktiengesellschaft | 13α-alkyl-gonanes, their production, and pharmaceutical preparations containing same |
| DE3337450A1 (de) * | 1983-10-12 | 1985-04-25 | Schering AG, 1000 Berlin und 4709 Bergkamen | Prostaglandine und antigestagene fuer den schwangerschaftsabbruch |
| DE3347126A1 (de) * | 1983-12-22 | 1985-07-11 | Schering AG, 1000 Berlin und 4709 Bergkamen | 11ss-aryl-estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3625315A1 (de) * | 1986-07-25 | 1988-01-28 | Schering Ag | 11ss-(4-isopropenylphenyl)-estra-4,9-diene, deren herstellung und diese enthaltende pharmazeutische praeparate |
| DE3702383A1 (de) * | 1987-01-23 | 1988-08-04 | Schering Ag | 11ss-alkinylestrene und -estradiene, deren herstellung und diese enthaltende pharmazeutische praeparate |
-
1986
- 1986-09-26 DE DE19863633244 patent/DE3633244A1/de not_active Withdrawn
-
1987
- 1987-09-15 ES ES87730107T patent/ES2051766T3/es not_active Expired - Lifetime
- 1987-09-15 EP EP87730107A patent/EP0266303B1/de not_active Expired - Lifetime
- 1987-09-15 DE DE8787730107T patent/DE3780757D1/de not_active Expired - Lifetime
- 1987-09-15 AT AT87730107T patent/ATE78690T1/de not_active IP Right Cessation
- 1987-09-16 DK DK487287A patent/DK169162B1/da not_active IP Right Cessation
- 1987-09-21 IL IL83967A patent/IL83967A/xx not_active IP Right Cessation
- 1987-09-22 JP JP62236403A patent/JP2582088B2/ja not_active Expired - Lifetime
- 1987-09-23 AU AU78950/87A patent/AU605177B2/en not_active Ceased
- 1987-09-25 ZA ZA877247A patent/ZA877247B/xx unknown
- 1987-09-25 IE IE257887A patent/IE66196B1/en not_active IP Right Cessation
-
1992
- 1992-08-20 GR GR920401791T patent/GR3005467T3/el unknown
-
1993
- 1993-07-26 US US08/096,360 patent/US5744464A/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| DK487287D0 (da) | 1987-09-16 |
| IE66196B1 (en) | 1995-12-13 |
| US5744464A (en) | 1998-04-28 |
| DE3780757D1 (de) | 1992-09-03 |
| JPS63101326A (ja) | 1988-05-06 |
| ES2051766T3 (es) | 1994-07-01 |
| ZA877247B (en) | 1988-03-28 |
| AU605177B2 (en) | 1991-01-10 |
| AU7895087A (en) | 1988-03-31 |
| DE3633244A1 (de) | 1988-03-31 |
| IE872578L (en) | 1988-03-26 |
| GR3005467T3 (da) | 1993-05-24 |
| EP0266303A3 (en) | 1989-12-20 |
| IL83967A (en) | 1992-11-15 |
| JP2582088B2 (ja) | 1997-02-19 |
| EP0266303B1 (de) | 1992-07-29 |
| ATE78690T1 (de) | 1992-08-15 |
| DK487287A (da) | 1988-03-27 |
| IL83967A0 (en) | 1988-02-29 |
| EP0266303A2 (de) | 1988-05-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B1 | Patent granted (law 1993) | ||
| PBP | Patent lapsed |
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