KR880012637A - Ⅱ-아릴에스트란 및 ⅱ-아릴프레그난 유도체 - Google Patents
Ⅱ-아릴에스트란 및 ⅱ-아릴프레그난 유도체 Download PDFInfo
- Publication number
- KR880012637A KR880012637A KR1019880004653A KR880004653A KR880012637A KR 880012637 A KR880012637 A KR 880012637A KR 1019880004653 A KR1019880004653 A KR 1019880004653A KR 880004653 A KR880004653 A KR 880004653A KR 880012637 A KR880012637 A KR 880012637A
- Authority
- KR
- South Korea
- Prior art keywords
- group
- compound
- hydroxyl
- compound according
- acyloxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 239000004215 Carbon black (E152) Substances 0.000 claims 3
- 125000004423 acyloxy group Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 229930195733 hydrocarbon Natural products 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- -1 aminophenyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 1
- 230000018044 dehydration Effects 0.000 claims 1
- 238000006297 dehydration reaction Methods 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 230000007062 hydrolysis Effects 0.000 claims 1
- 238000006460 hydrolysis reaction Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002560 nitrile group Chemical group 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000004417 unsaturated alkyl group Chemical group 0.000 claims 1
- 229930195735 unsaturated hydrocarbon Natural products 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/005—Ketals
- C07J21/006—Ketals at position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/005—Ketals
- C07J21/008—Ketals at position 17
-
- 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
- C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
- C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (9)
- 하기 구조식을 가지는 것을 특징으로 하는 11-아릴에스트란 및 11-아릴프레그난유도체.식중, R1은 치환체 X 및 Y가 각각 H 또는 (1-4)C 탄화수소 라디칼이거나 (2-6)C 탄화수소라디칼인를 가진 아릴기이고, R2는 (1-4)C를 함유하는 알킬기이고, R3은 H, OH, (1-8)C를 함유하고 적어도 히드록실, 옥소, 할로겐, 아지도 또는 니트릴기를 포함하는 포화 또는 불포화탄화수소, 또는 아실옥시 또는 알콕시기이고, R4는 히드록실, 아실옥시 또는 알콕시기, 또는 히드록실, 알콕시, 아실옥시 또는 할로겐기로 임의 치환된 아실기이고, 또는 R3과 R4가 함께 고리를 형성하고, R5는 (1-4)C를 함유하는 탄화수소라디칼이다.
- 제 1항에 있어서, R1이 하기구조식을 가지는 아미노페닐기인것을 특징으로 하는 화합물.식중, X 및 Y는 각각 (1-4)C 함유알킬이다.
- 제 1항 또는 제 2항에 있어서, R2가 메틸인것을 특징으로 하는 화합물.
- 제 1항 내지 제 3항에 있어서, R3가 (1-4)C 및 1또는 2개의히드록실기를 함유하는 불포화 알킬기인 것을 특징으로하는 화합물.
- 제 1항 내지 제 3항에 있어서, R3및 R4가 함께 고리를 형성하는 것을 특징으로하는 화합물.
- 제 1항 내지 제 4항에 있어서, R4가 히드록실기인 것을 특징으로 하는 화합물.
- 제 1항 내지 제 6항에 있어서, R5가 (1-4)C 함유 알킬기인 것을 특징으로 하는 화합물.
- 하기구조식의 화합물을 탈수 및 가수분해하여 제조하는 것을 특징으로 하는 제 1항의 화합물의 제조방법.식중, R1, R2, R3, R4및 R5는 제 1항에서의 정의와 동일하고, R3및/또는 R4가 산소함유기인 경우에는 R3및/또는 R4는 산소원자가 가수분해성기에 의해 보호된 산소 함유기일수도 있고, R6및 R7은 (1-4)C 함유 알킬기이거나 R6과 R7이 함께 (2-5)C 함유 알킬렌기를 형성한다.
- 적어도 하나의 제 1항의 화합물을 포함하는 약학조성물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
NL8700970 | 1987-04-24 | ||
NL8700970 | 1987-04-24 | ||
NL87.00970 | 1987-04-24 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR880012637A true KR880012637A (ko) | 1988-11-28 |
KR970005318B1 KR970005318B1 (ko) | 1997-04-15 |
Family
ID=19849909
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019880004653A KR970005318B1 (ko) | 1987-04-24 | 1988-04-23 | 11-아릴에스트란 및 11-아릴프레그난 유도체 |
Country Status (17)
Country | Link |
---|---|
US (1) | US4871724A (ko) |
EP (1) | EP0289073B1 (ko) |
JP (1) | JP2655676B2 (ko) |
KR (1) | KR970005318B1 (ko) |
CN (1) | CN1019978C (ko) |
AT (1) | ATE69820T1 (ko) |
AU (1) | AU608831B2 (ko) |
CA (1) | CA1297472C (ko) |
DE (1) | DE3866410D1 (ko) |
DK (1) | DK168294B1 (ko) |
ES (1) | ES2045082T3 (ko) |
FI (1) | FI88396C (ko) |
GR (1) | GR3003363T3 (ko) |
IE (1) | IE60783B1 (ko) |
NZ (1) | NZ224355A (ko) |
PT (1) | PT87322B (ko) |
ZA (1) | ZA882643B (ko) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE59010853D1 (de) * | 1989-08-04 | 1998-12-03 | Schering Ag | 11 Beta-Aryl-gona-4,9-dien-3-one |
US5407928A (en) * | 1990-08-15 | 1995-04-18 | Schering Aktiengesellschaft | 11β-aryl-gona-4,9-dien-3-ones |
ZA929315B (en) * | 1991-12-20 | 1993-05-24 | Akzo Nv | 17-spirofuran-3'-ylidene steroids. |
CA2100514C (en) * | 1992-07-29 | 2005-03-29 | Johannes A. M. Hamersma | 17-spiromethylene steroids |
DE4332283A1 (de) * | 1993-09-20 | 1995-04-13 | Jenapharm Gmbh | Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
DE4434488A1 (de) | 1994-09-14 | 1996-03-21 | Schering Ag | Steroidester und -amide, Verfahren zu ihrer Herstellung und ihre pharmazeutische Verwendung |
US5576310A (en) * | 1994-09-20 | 1996-11-19 | Jenapharm Gmbh | 11-benzaldoxime-17β-methoxy-17α-methoxymethyl-estrasdiene derivatives, methods for their production and pharmaceuticals containing such compounds |
ZA9510926B (en) | 1994-12-23 | 1996-07-03 | Schering Ag | Compounds with progesterone-antagonistic and antiestrogenic action to be used together for female contraception |
US6020328A (en) * | 1998-03-06 | 2000-02-01 | Research Triangle Institute | 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties |
US6262042B1 (en) | 1998-05-29 | 2001-07-17 | Research Triangle Institute | 17β-amino and hydroxylamino-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties |
US5962444A (en) * | 1998-05-29 | 1999-10-05 | Research Triangle Institute | 17β-nitro-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties |
CN1117759C (zh) * | 1999-09-02 | 2003-08-13 | 上海中西药业股份有限公司 | 甾体化合物,其制备方法和其药物组合物及其应用 |
TW200531977A (en) | 2004-03-25 | 2005-10-01 | Akzo Nobel Nv | Progesterone receptor modulators |
EP3693376A1 (en) | 2006-10-24 | 2020-08-12 | Allergan Pharmaceuticals International Limited | Compositions for suppressing endometrial proliferation |
TWI539953B (zh) | 2008-04-28 | 2016-07-01 | 瑞波若斯治療學公司 | 用於治療乳癌之組成物和方法 |
WO2011119194A1 (en) | 2010-03-22 | 2011-09-29 | Repros Therapeutics Inc. | Compositions and methods for non-toxic delivery of antiprogestins |
US9096641B2 (en) | 2013-06-05 | 2015-08-04 | Evestra, Inc. | Imidazolyl progesterone antagonists |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3424769A (en) * | 1966-04-04 | 1969-01-28 | Syntex Corp | Process for the preparation of novel 6alpha-methyl-delta4,9(10)- diene steroids |
ZA8231B (en) * | 1981-01-09 | 1982-11-24 | Roussel Uclaf | New 11 -substituted steroid derivatives, their preparation, their use as medicaments, the compositions containing them and the new intermediates thus obtained |
EP0116974B1 (de) * | 1983-02-18 | 1986-10-29 | Schering Aktiengesellschaft | 11-Beta-Aryl-Estradiene, Verfahren zu deren Herstellung und diese enthaltende pharmazeutische Präparate |
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 |
AU580843B2 (en) * | 1985-02-07 | 1989-02-02 | Schering Aktiengesellschaft | 11``-phenyl-gonanes, their manufacture and pharmaceutical preparations containing them |
US4678282A (en) * | 1985-02-19 | 1987-07-07 | Ovonic Imaging Systems, Inc. | Active display matrix addressable without crossed lines on any one substrate and method of using the same |
GB8513723D0 (en) * | 1985-05-31 | 1985-07-03 | Erba Farmitalia | 11-beta substituted steroids |
-
1988
- 1988-04-12 EP EP88200689A patent/EP0289073B1/en not_active Expired - Lifetime
- 1988-04-12 ES ES88200689T patent/ES2045082T3/es not_active Expired - Lifetime
- 1988-04-12 AT AT88200689T patent/ATE69820T1/de not_active IP Right Cessation
- 1988-04-12 DE DE8888200689T patent/DE3866410D1/de not_active Expired - Fee Related
- 1988-04-14 IE IE113188A patent/IE60783B1/en not_active IP Right Cessation
- 1988-04-14 ZA ZA882643A patent/ZA882643B/xx unknown
- 1988-04-19 FI FI881826A patent/FI88396C/fi not_active IP Right Cessation
- 1988-04-20 US US07/183,851 patent/US4871724A/en not_active Expired - Fee Related
- 1988-04-20 CA CA000564606A patent/CA1297472C/en not_active Expired - Fee Related
- 1988-04-22 NZ NZ224355A patent/NZ224355A/xx unknown
- 1988-04-22 AU AU15072/88A patent/AU608831B2/en not_active Ceased
- 1988-04-22 JP JP63100010A patent/JP2655676B2/ja not_active Expired - Lifetime
- 1988-04-22 PT PT87322A patent/PT87322B/pt not_active IP Right Cessation
- 1988-04-22 DK DK221888A patent/DK168294B1/da active IP Right Grant
- 1988-04-23 KR KR1019880004653A patent/KR970005318B1/ko not_active IP Right Cessation
- 1988-04-23 CN CN88102416A patent/CN1019978C/zh not_active Expired - Fee Related
-
1991
- 1991-12-17 GR GR91402004T patent/GR3003363T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
KR970005318B1 (ko) | 1997-04-15 |
EP0289073A1 (en) | 1988-11-02 |
GR3003363T3 (en) | 1993-02-17 |
NZ224355A (en) | 1990-03-27 |
FI881826A0 (fi) | 1988-04-19 |
PT87322B (pt) | 1992-08-31 |
ES2045082T3 (es) | 1994-01-16 |
FI88396C (fi) | 1993-05-10 |
ZA882643B (en) | 1988-10-04 |
JP2655676B2 (ja) | 1997-09-24 |
AU1507288A (en) | 1988-10-27 |
IE60783B1 (en) | 1994-08-10 |
DE3866410D1 (de) | 1992-01-09 |
DK221888A (da) | 1988-10-25 |
EP0289073B1 (en) | 1991-11-27 |
PT87322A (pt) | 1988-05-01 |
AU608831B2 (en) | 1991-04-18 |
ATE69820T1 (de) | 1991-12-15 |
IE881131L (en) | 1988-10-24 |
CA1297472C (en) | 1992-03-17 |
DK221888D0 (da) | 1988-04-22 |
FI881826A (fi) | 1988-10-25 |
CN1019978C (zh) | 1993-03-03 |
US4871724A (en) | 1989-10-03 |
CN88102416A (zh) | 1988-12-14 |
DK168294B1 (da) | 1994-03-07 |
JPS63280097A (ja) | 1988-11-17 |
FI88396B (fi) | 1993-01-29 |
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