KR960030938A - 나프틸 화합물, 중간체, 조성물 및 방법 - Google Patents
나프틸 화합물, 중간체, 조성물 및 방법 Download PDFInfo
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- KR960030938A KR960030938A KR1019960004619A KR19960004619A KR960030938A KR 960030938 A KR960030938 A KR 960030938A KR 1019960004619 A KR1019960004619 A KR 1019960004619A KR 19960004619 A KR19960004619 A KR 19960004619A KR 960030938 A KR960030938 A KR 960030938A
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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- 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
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- A—HUMAN NECESSITIES
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- 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
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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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- 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
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- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C43/00—Ethers; Compounds having groups, groups or groups
- C07C43/02—Ethers
- C07C43/257—Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings
- C07C43/295—Ethers having an ether-oxygen atom bound to carbon atoms both belonging to six-membered aromatic rings containing hydroxy or O-metal groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
- C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
- C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
- C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
- C07C45/70—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form
- C07C45/71—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C47/00—Compounds having —CHO groups
- C07C47/52—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings
- C07C47/575—Compounds having —CHO groups bound to carbon atoms of six—membered aromatic rings containing ether groups, groups, groups, or groups
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
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- Physical Education & Sports Medicine (AREA)
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- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
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- Orthopedic Medicine & Surgery (AREA)
- Diabetes (AREA)
- Vascular Medicine (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)
- Pyrrole Compounds (AREA)
- Steroid Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
본 발명은 하기 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허용되는 염을 제공한다:
상기 식에서, R1은 -H, -OH, -O(C1-C4알킬), -OCOC6H5, -OCO(C1-C6알킬), 또는 -OSO2(C2-C6알킬)이고; R2는 -H, -OH, -O(C1-C4알킬), -OCOC6H5, -OCO(C1-C5알킬), -CSO2(C2-C6알킬) 또는 할로이고; R3는 1-페피리디닐, 1-피롤리디닐, 메틸-1-피롤리디닐, 디메틸-1-피롤리디노, 4-모르폴리노, 디메틸아미노, 디에틸아미노, 디이소프로필아미노, 또는 1-헥사메틸렌이미노이고, n은 2 또는 3이다.
또한 본 발명은 하기 일반식(III)의 화합물 또는 그의 약학적으로 허용되는 염을 제공한다:
상기 식에서, Rla는 -H 또는 -OR5이고, 이때 R5는 하이드록시 보호기이고, R2a는 -H, 할로, 또는 -OR6이고, 이때 R6은 하이드록시 보호기이고, R4는 -OH 또는 -CHO이다.
더욱더 본 발명은 일반식(Ⅰ)의 화합물의 약학 조성물 및 그 중에서도 특히 폐경기후 증후군의 증상 및 호르몬에 의존하는 암, 특히 유방암을 완화시키는데 일반식(Ⅰ)의 화합물을 사용하는 방법을 제공한다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (3)
- 하기 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허용되는 염:상기 식에서, R1은 -H, -OH, -O(C1-C4알킬), -OCOC6H5, -OCO(C1-C6알킬), 또는 -OSO2(C2-C6알킬)이고; R2는 -H, -OH, -O(C1-C4알킬), -OCOC6H5, -OCO(C1-C6알킬), -OSO2(C2-C6알킬) 또는 할로이고; R3는 1-피페리디닐, 1-피롤리디닐, 메틸-1-피롤리디닐, 디메틸-1-피롤리디노, 4-모르폴리노, 디메틸아미노, 디에틸아미노, 디이소프로필아미노, 또는 1-헥사메틸렌이미노이고, n은 2 또는 3이다.
- 제1항에 있어서, R1이 -OH이고, R2가 -OH이고, R3가 1-피페리디닐이고, n이 2인 화합물 또는 그의 약학적으로 허용되는 염.
- 활성 성분으로 제1 또는 제2항에 청구된 화합물과 임의로, 에스트로겐 또는 프로게스틴을 그에 대해 약학적으로 허용되는 하나 이상의 담체, 부형제, 또는 희석제와 함께 포함하는 약학 제형.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/395,950 US5998401A (en) | 1995-02-28 | 1995-02-28 | Naphthyl compounds, intermediates, compositions, and methods |
US08/395,950 | 1995-02-28 |
Publications (1)
Publication Number | Publication Date |
---|---|
KR960030938A true KR960030938A (ko) | 1996-09-17 |
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ID=23565221
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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KR1019960004619A KR960030938A (ko) | 1995-02-28 | 1996-02-26 | 나프틸 화합물, 중간체, 조성물 및 방법 |
Country Status (32)
Country | Link |
---|---|
US (5) | US5998401A (ko) |
EP (1) | EP0729951B1 (ko) |
JP (1) | JPH08268881A (ko) |
KR (1) | KR960030938A (ko) |
CN (2) | CN1053886C (ko) |
AR (2) | AR001036A1 (ko) |
AT (1) | ATE180776T1 (ko) |
AU (1) | AU694837B2 (ko) |
BR (1) | BR9600821A (ko) |
CA (1) | CA2170337A1 (ko) |
CO (1) | CO4700421A1 (ko) |
CY (1) | CY2178B1 (ko) |
CZ (1) | CZ288213B6 (ko) |
DE (1) | DE69602638T2 (ko) |
DK (1) | DK0729951T3 (ko) |
ES (1) | ES2132841T3 (ko) |
FI (1) | FI115524B (ko) |
GR (1) | GR3030407T3 (ko) |
IL (1) | IL117168A (ko) |
IN (1) | IN182138B (ko) |
MX (1) | MX9600743A (ko) |
MY (1) | MY113232A (ko) |
NO (1) | NO305833B1 (ko) |
NZ (1) | NZ286072A (ko) |
PE (1) | PE28497A1 (ko) |
PL (1) | PL183578B1 (ko) |
RU (1) | RU2167849C2 (ko) |
SG (1) | SG55098A1 (ko) |
TR (1) | TR199600126A1 (ko) |
TW (1) | TW349946B (ko) |
YU (1) | YU11496A (ko) |
ZA (1) | ZA961291B (ko) |
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CA2214931A1 (en) * | 1996-09-26 | 1998-03-26 | Henry Uhlman Bryant | Tetrahydrobenzo-a-fluorene compounds and method of use |
CA2214929A1 (en) * | 1996-09-26 | 1998-03-26 | Charles Willis Lugar, Iii | Naphthofluorene compounds, intermediates, compositions and methods |
CA2214935A1 (en) * | 1996-09-26 | 1998-03-26 | Henry Uhlman Bryant | Benzofluorene compounds, intermediates, compositions, and methods |
CA2217810A1 (en) * | 1996-10-10 | 1998-04-10 | Eli Lilly And Company | 2-aryl-3-aminoaryloxynaphthyl compounds, intermediates, compositions and methods |
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ZA982877B (en) * | 1997-04-09 | 1999-10-04 | Lilly Co Eli | Treatment of central nervous system disorders with selective estrogen receptor modulators. |
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EP1173164A2 (en) * | 1999-04-16 | 2002-01-23 | AstraZeneca AB | Estrogen receptor-beta ligands |
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KR100370597B1 (ko) * | 2000-06-22 | 2003-02-05 | 박정일 | 산형매립초로부터 분리한 신규한 나프탈렌계 화합물 및이를 유효성분으로 하는 약학적 조성물 |
WO2002044119A2 (en) * | 2000-11-28 | 2002-06-06 | Eli Lilly And Company | Synthesis of 2-aryl-1-naphthol derivatives via a tandem palladium catalyzed arylation and dehydrogenation |
JP2004531559A (ja) * | 2001-05-22 | 2004-10-14 | イーライ・リリー・アンド・カンパニー | エストロゲン欠乏または内因性エストロゲンに対する異常な生理反応に関連する疾患を抑制するためのテトラヒドロキノリン誘導体 |
WO2002094788A1 (en) | 2001-05-22 | 2002-11-28 | Eli Lilly And Company | 2-substituted 1,2,3,4-tetrahydroquinolines and derivatives thereof, compositions and methods |
US6914074B2 (en) | 2001-12-13 | 2005-07-05 | Wyeth | Substituted phenyl naphthalenes as estrogenic agents |
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US9315539B2 (en) * | 2002-10-01 | 2016-04-19 | Yale University | 11 beta-short chain substituted estradiol analogs and their use in the treatment of menopausal symptoms and estrogen sensitive cancer |
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-
1995
- 1995-02-28 US US08/395,950 patent/US5998401A/en not_active Expired - Fee Related
- 1995-06-06 US US08/469,971 patent/US5567712A/en not_active Expired - Fee Related
- 1995-06-06 US US08/466,954 patent/US6268361B1/en not_active Expired - Fee Related
- 1995-06-06 US US08/465,844 patent/US5574190A/en not_active Expired - Fee Related
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1996
- 1996-02-09 ES ES96300877T patent/ES2132841T3/es not_active Expired - Lifetime
- 1996-02-09 EP EP96300877A patent/EP0729951B1/en not_active Expired - Lifetime
- 1996-02-09 DK DK96300877T patent/DK0729951T3/da active
- 1996-02-09 AT AT96300877T patent/ATE180776T1/de not_active IP Right Cessation
- 1996-02-09 DE DE69602638T patent/DE69602638T2/de not_active Expired - Fee Related
- 1996-02-15 PL PL96312829A patent/PL183578B1/pl unknown
- 1996-02-15 TW TW085101903A patent/TW349946B/zh active
- 1996-02-16 TR TR96/00126A patent/TR199600126A1/xx unknown
- 1996-02-19 ZA ZA9601291A patent/ZA961291B/xx unknown
- 1996-02-19 IL IL11716896A patent/IL117168A/en not_active IP Right Cessation
- 1996-02-22 IN IN321CA1996 patent/IN182138B/en unknown
- 1996-02-26 CZ CZ1996581A patent/CZ288213B6/cs not_active IP Right Cessation
- 1996-02-26 AU AU45732/96A patent/AU694837B2/en not_active Ceased
- 1996-02-26 KR KR1019960004619A patent/KR960030938A/ko not_active Application Discontinuation
- 1996-02-26 PE PE1996000130A patent/PE28497A1/es not_active Application Discontinuation
- 1996-02-26 BR BR9600821A patent/BR9600821A/pt not_active Application Discontinuation
- 1996-02-26 AR ARP960101524A patent/AR001036A1/es active IP Right Grant
- 1996-02-26 MX MX9600743A patent/MX9600743A/es not_active IP Right Cessation
- 1996-02-26 NO NO960772A patent/NO305833B1/no not_active IP Right Cessation
- 1996-02-26 CO CO96008862A patent/CO4700421A1/es unknown
- 1996-02-26 CN CN96105727A patent/CN1053886C/zh not_active Expired - Fee Related
- 1996-02-26 AR ARP960101525A patent/AR002964A1/es unknown
- 1996-02-26 FI FI960889A patent/FI115524B/fi active IP Right Grant
- 1996-02-26 CA CA002170337A patent/CA2170337A1/en not_active Abandoned
- 1996-02-26 RU RU96103632/04A patent/RU2167849C2/ru active
- 1996-02-26 YU YU11496A patent/YU11496A/sh unknown
- 1996-02-26 NZ NZ286072A patent/NZ286072A/en unknown
- 1996-02-26 JP JP8037970A patent/JPH08268881A/ja active Pending
- 1996-02-27 MY MYPI96000686A patent/MY113232A/en unknown
- 1996-02-27 SG SG1996006121A patent/SG55098A1/en unknown
-
1999
- 1999-06-03 GR GR990401445T patent/GR3030407T3/el unknown
- 1999-11-05 CN CNB99123572XA patent/CN1152683C/zh not_active Expired - Fee Related
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2000
- 2000-05-03 US US09/563,282 patent/US6355632B1/en not_active Expired - Fee Related
- 2000-08-02 CY CY0000035A patent/CY2178B1/xx unknown
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