KR970701708A - 9-데옥소탁산 화합물(9-Deoxotaxane compounds) - Google Patents
9-데옥소탁산 화합물(9-Deoxotaxane compounds)Info
- Publication number
- KR970701708A KR970701708A KR1019960705045A KR19960705045A KR970701708A KR 970701708 A KR970701708 A KR 970701708A KR 1019960705045 A KR1019960705045 A KR 1019960705045A KR 19960705045 A KR19960705045 A KR 19960705045A KR 970701708 A KR970701708 A KR 970701708A
- Authority
- KR
- South Korea
- Prior art keywords
- iii
- compound
- hydrogen
- deoxy
- acetyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/06—Peri-condensed systems
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
- C07D305/14—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
Abstract
본 발명은 하기 화학식 (2)의 화합물, 이의 제조방법, 이 화합물을 함유하는 약제학적 조성물 및 종양 성장을 억제하기 위해 이들을 사용하는 방법에 관한 것이다.
위의 화학식 (2)에서, -OR1은 알카노일 또일 파클리탁셀의 C-13 측쇄이고, R2, R3및 R6은 다양한 조합으로 탈산소화되거나 수소일 수 있으며, R4및 R5는 아실 그룹이다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (11)
- 하기 화학식 (2)의 화합물 또는 이의 프로드럭(prodrug).위의 화학식 (2)에서, R1은 알카노일 또는 식의 라디칼(여기서, R7은 수소, 알킬, 페닐, 치환된 페닐, 알콕시, 치환된 알콕시, 아미노, 치환된 아미노, 페녹시 및 치환된 페녹시로 이루어진 그룹으로부터 선택되고, R8은 수소, 알킬, 하이드록시알킬, 알콕시알킬, 아미노알킬, 페닐, 치환된 페닐, α-나프틸, β-나프틸 및 헤테로아릴로 이루어진 그룹으로부터 선택되며, R9는 수소, 알카노일, 치환된 알카노일 및 아미노알카노일로 이루어진 그룹으로부터 선택된다)이고, R2, R3및 R6은 독립적으로 수소, 하이드록시, 알콕시, 아미노알카노일 및 알카노일옥시로 이루어진 그룹으로부터 선택되며, R4는 알킬, 알카노일, 아미노알카노일 및 아로일로 이루어진 그룹으로부터 선택되고, R5는 알킬, 알카노일, 아미노알카노일 및 아로일로 이루어진 그룹으로부터 선택된다.
- 제1항에 있어서, R1이 식또는의 라디칼인 화합물.
- 제1항에 있어서, R2가 수소인 화합물.
- 제2항에 있어서, R2가 수소인 화합물.
- 제1항에 있어서, R3이 수소인 화합물.
- 제2항에 있어서, R3이 수소인 화합물.
- 제2항에 있어서, R2와 R3이 둘다 수소인 화합물.
- 제2항에 있어서, R2와 R3이 둘다 수소인 화합물.
- 제1항에 있어서, R1과 R4가 아세틸이고 R2가 아세톡시이며 R5가 하이드록시인 화합물.
- 제1항에 있어서, 13-아세틸-9-데옥소바카틴 Ⅲ, 9-데옥소파클리탁셀, 13-아세틸-7-데옥시-9-데옥소바카틴 Ⅲ, 7-데옥시-9-데옥소파클리탁셀, 13-아세틸-10-데스아세톡시-7-데옥시-9-데옥소바카틴 Ⅲ 및 10-데스아세톡시-7-데옥시-9-데옥소파클리탁셀로 이루어진 그룹으로부터 선택되는 화합물.
- 메틸 13-아세틸-9-디하이드로바카틴 Ⅲ 9-O-크산테이트, 9-데옥소바카틴 Ⅲ, 13-{(2R,3S)-N-벤질옥시카보닐-N,O-(1-메틸에틸리덴)-3-페닐이소세린}-9-데옥소바카틴 Ⅲ, 7-O-트리에틸실실-9-데옥소바카틴 Ⅲ, 13-아세틸-9-데옥소바카틴 Ⅲ 7-티오카보닐이미다졸리드, 7-데옥시-9-데옥소바카틴 Ⅲ, 13-{(2R,3S)-N-벤질옥시카보닐-N,O-(1-메틸에틸리덴)-3-페닐이소세린}-7-데옥시-9-데옥소바카틴 Ⅲ, 7-데옥시-9-데옥소바카틴 Ⅲ 10-티오카보닐이미다졸리드, 10-데스아세톡시-7-데옥시-9-데옥소바카틴 Ⅲ 및 13-{(2R,3S)-N-벤질옥시카보닐-N,O-(1-메틸에틸리덴)-3-페닐이소세린}-10-데스아세톡시-7-데옥시-9-데옥소바카틴 Ⅲ으로 이루어진 그룹으로부터 선택되는 중간체.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/208,509 US5440056A (en) | 1992-04-17 | 1994-03-09 | 9-deoxotaxane compounds |
US08/208,509 | 1994-03-09 | ||
PCT/US1995/002524 WO1995024402A1 (en) | 1994-03-09 | 1995-03-01 | 9-deoxotaxane compounds |
Publications (1)
Publication Number | Publication Date |
---|---|
KR970701708A true KR970701708A (ko) | 1997-04-12 |
Family
ID=22774850
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019960705045A KR970701708A (ko) | 1994-03-09 | 1995-03-01 | 9-데옥소탁산 화합물(9-Deoxotaxane compounds) |
Country Status (15)
Country | Link |
---|---|
US (2) | US5440056A (ko) |
EP (1) | EP0749432B1 (ko) |
JP (1) | JPH09511235A (ko) |
KR (1) | KR970701708A (ko) |
AT (1) | ATE201019T1 (ko) |
AU (1) | AU688946B2 (ko) |
CA (1) | CA2182103A1 (ko) |
DE (1) | DE69520880T2 (ko) |
DK (1) | DK0749432T3 (ko) |
ES (1) | ES2158093T3 (ko) |
GR (1) | GR3036286T3 (ko) |
IL (1) | IL112880A0 (ko) |
PH (1) | PH31271A (ko) |
PT (1) | PT749432E (ko) |
WO (1) | WO1995024402A1 (ko) |
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-
1994
- 1994-03-09 US US08/208,509 patent/US5440056A/en not_active Expired - Fee Related
-
1995
- 1995-03-01 DK DK95912007T patent/DK0749432T3/da active
- 1995-03-01 KR KR1019960705045A patent/KR970701708A/ko not_active Application Discontinuation
- 1995-03-01 JP JP7523511A patent/JPH09511235A/ja not_active Withdrawn
- 1995-03-01 ES ES95912007T patent/ES2158093T3/es not_active Expired - Lifetime
- 1995-03-01 PT PT95912007T patent/PT749432E/pt unknown
- 1995-03-01 AT AT95912007T patent/ATE201019T1/de not_active IP Right Cessation
- 1995-03-01 AU AU31047/95A patent/AU688946B2/en not_active Ceased
- 1995-03-01 EP EP95912007A patent/EP0749432B1/en not_active Expired - Lifetime
- 1995-03-01 WO PCT/US1995/002524 patent/WO1995024402A1/en active IP Right Grant
- 1995-03-01 CA CA002182103A patent/CA2182103A1/en not_active Abandoned
- 1995-03-01 DE DE69520880T patent/DE69520880T2/de not_active Expired - Fee Related
- 1995-03-05 IL IL11288095A patent/IL112880A0/xx unknown
- 1995-03-09 PH PH50096A patent/PH31271A/en unknown
- 1995-05-11 US US08/439,334 patent/US5616740A/en not_active Expired - Fee Related
-
2001
- 2001-07-26 GR GR20010401136T patent/GR3036286T3/el not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
WO1995024402A1 (en) | 1995-09-14 |
DK0749432T3 (da) | 2001-07-30 |
PH31271A (en) | 1998-06-18 |
CA2182103A1 (en) | 1995-09-14 |
EP0749432B1 (en) | 2001-05-09 |
MX9603891A (es) | 1997-07-31 |
ES2158093T3 (es) | 2001-09-01 |
US5440056A (en) | 1995-08-08 |
DE69520880T2 (de) | 2001-12-20 |
DE69520880D1 (de) | 2001-06-13 |
ATE201019T1 (de) | 2001-05-15 |
JPH09511235A (ja) | 1997-11-11 |
PT749432E (pt) | 2001-09-28 |
AU688946B2 (en) | 1998-03-19 |
AU3104795A (en) | 1995-09-25 |
GR3036286T3 (en) | 2001-10-31 |
US5616740A (en) | 1997-04-01 |
IL112880A0 (en) | 1995-06-29 |
EP0749432A1 (en) | 1996-12-27 |
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