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KR870700067A - 피리도(2,3-d)-피리미딘 유도체 - Google Patents

피리도(2,3-d)-피리미딘 유도체

Info

Publication number
KR870700067A
KR870700067A KR1019860700771A KR860700771A KR870700067A KR 870700067 A KR870700067 A KR 870700067A KR 1019860700771 A KR1019860700771 A KR 1019860700771A KR 860700771 A KR860700771 A KR 860700771A KR 870700067 A KR870700067 A KR 870700067A
Authority
KR
South Korea
Prior art keywords
compound
amino
glutamic acid
pyrimidin
benzoyl
Prior art date
Application number
KR1019860700771A
Other languages
English (en)
Other versions
KR940002952B1 (ko
Inventor
에드워드 씨 테일러
죠오지 피터 베어드스레이
피터 쥬니어 해링톤
스테펜 알 플레처
Original Assignee
원본미기재
더 트러스 티스 어브 프린스톤 유니버시티
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by 원본미기재, 더 트러스 티스 어브 프린스톤 유니버시티 filed Critical 원본미기재
Publication of KR870700067A publication Critical patent/KR870700067A/ko
Application granted granted Critical
Publication of KR940002952B1 publication Critical patent/KR940002952B1/ko

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Cosmetics (AREA)

Abstract

내용 없음.

Description

피리도(2,3-d)피리미딘 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (20)

  1. 다음일반식(IA)의 피리도[2,3-d] 피리미딘; 다음일반식(IB)의 5,6,7,8-테트라하이드로피리도[2,3-d)피리미딘; 이들의 토우토머 이성체; 와 이들의 약제학적으로 허용되는 알카리금속, 알카리토금속, 비독성금속, 암모늄 및 치환된 암모늄염으로 구성되는 군으로부터 선정된 화합물.
    상기식에서, R1은 아미노 또는 하이드록시; R3는 수소, 메틸 또는 에틸; * 로 표시된 탄소원자에 대한 배열이 L배열이다.
  2. 제1항에 있어서, R1이 아미노 또는 하이드록시; 또 R3가 수소, 메틸 또는 에틸인 다음일반식(IB)의 5,6,7,8-테트라하이드로피리도(2,3-d)피리미딘 화합물.
  3. 제2항에 있어서, R3가 수소인 화합물.
  4. 제3항에 있어서, R1이 하이드록시인 화합물.
  5. 제1항에 있어서, N-(4-[2-아미노-(2-4-하이드록시-5, 6, 7, 8-테트라하이드로피리도[2, 3-d]피리미딘-6-일)에틸]벤조일)-L-글루탐산화합물.
  6. 제1항에 있어서, N-(4-[1-(2-아미노-4-하이드록시-5, 6, 7, 8-테트라하이드로피리도[2, 3-d]피리미딘-6-일)프로프-2-일)벤조일-L-글루탐산 화합물.
  7. 제1항에 있어서, N-(4-[1-(2-아미노-4-하이드록시-5, 6, 7, 8-테트라하이드로피리도[2, 3-d]피리미딘-6-일)부트-2-일)벤조일)-L-글루탐산화합물.
  8. 제2항에 있어서, R1이 아미노인 화합물.
  9. 제1항에 있어서, N-(4-[2-(2, 4-디아미노-5, 6, 7, 8-테트라하이드로피리도[2, 3d)피리미딘-6-일)에틸]벤조일-L-글루탐산 화합물.
  10. 제1항에 있어서, N-(4-[1-(2, 4-디아미노-5, 6, 7, 8-테트라하이드로피리도[2, 3-d)피리미딘-6일)프로프-2-일[벤조일)-L-글루탐산 화합물.
  11. 제1항에 있어서, N-(4-[1-(2, 4-디아미노-5, 6, 7, 8-테트라하이드록시피리도[2, 3-d]피리미딘-6-일)부트-2-일]벤조일)-L-글루탐산 화합물.
  12. 제1항에 있어서, N-(4-[2-(2-아미노-4-하이드록시피리도[2, 3-d]피리미딘-6-일)에틸]벤조일)-L-글루탐산 화합물.
  13. 제1항에 있어서, N-(4-[1-(2-아미노-4-하이드록시피리도[2, 3-d]피리미딘-6-일)프로프-2-일]벤조일)-L-글루탐산 화합물.
  14. 제1항에 있어서, N-(4-[1-2-아미노-4-하이드록시피리도[2, 3-d]피리미딘-6-일)부트-2-일]벤조일)-L-글루탐산 화합물.
  15. 효과량 만큼의 제1항에 따른 화합물을 단위투여량 또는 배수 투여량 형태로 포유동물에 투여함으로서 포유동물내의 신생종양 성장을 퇴치하는 방법.
  16. 효과량만큼의 제5항에 따른 화합물을 단위투여량 또는 배수 투여량형태로 포유동물에 투여함으로서 포유동물내의 신생종양 성장을 퇴치하는 방법.
  17. 포유동물의 단위투여량 또는 배수투여량 형태로 투여해서 신생종양 성장퇴치에 효과가 있는 제1항의 따른 화합물 일정량과 약제학적으로 허용되는 담체를 결합시켜 제조되는 포유동물내의 신생종양성장퇴치용 약제조성물.
  18. 포유동물에 단위투여량 또는 배수투여량 형태로 투여해서, 신생종양 성장퇴치에 효과가 있는 제5항에 따른 화합물 일정량과 약제학적으로 허용되는 담체를 결합시켜 제조되는 포유동물내의 신생종양성장퇴치용 약제조성물.
  19. 다음 일반식(Ⅱ)의 글루탐산유도체를 가수분해 도는 가수소분해 시켜서 제1항에 따른 화합물을 제조하는 방법.
    상기식에서, R1은 상기 규정한 바와같고; R3은 수소, 메틸 또는 에틸이며; R4는
    R5및 R6는 같거나 서로 다른 카르복실산 보호기이며; 그리고 R7은 수소, 또는 아미노 보호기임.
  20. 다음 일반식(XI)의 화합물.
    상기 식에서, R1은 아미노 또는 하이드록시이고; R3은 수소, 메틸, 또는 에틸이고; 그리고 Z는 하이드록시, 알콕시, 또는 -NH-C+H(COOX)-CH2CH2COOX로서 이때 X는 수소 또는 알킬이고 “+” 표시의 탄소원자에 대한 배열은 L 배열이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019860700771A 1985-03-08 1986-02-24 피리도[2,3-d]피리미딘 유도체의 제조방법 KR940002952B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US70962285A 1985-03-08 1985-03-08
US709.622 1985-03-08
US709622 1985-03-08
PCT/US1986/000368 WO1986005181A1 (en) 1985-03-08 1986-02-24 PYRIDO AD2,3-d BDPYRIMIDIN DERIVATIVES

Publications (2)

Publication Number Publication Date
KR870700067A true KR870700067A (ko) 1987-02-28
KR940002952B1 KR940002952B1 (ko) 1994-04-09

Family

ID=24850641

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019860700771A KR940002952B1 (ko) 1985-03-08 1986-02-24 피리도[2,3-d]피리미딘 유도체의 제조방법

Country Status (22)

Country Link
EP (1) EP0215063B1 (ko)
JP (2) JPH0822860B2 (ko)
KR (1) KR940002952B1 (ko)
CN (1) CN1016174B (ko)
AT (1) ATE96790T1 (ko)
AU (1) AU578813B2 (ko)
CA (1) CA1276637C (ko)
DE (1) DE3689250T2 (ko)
DK (1) DK168666B1 (ko)
EG (1) EG18371A (ko)
ES (2) ES8704167A1 (ko)
GR (1) GR860592B (ko)
HU (1) HU196202B (ko)
IE (1) IE63653B1 (ko)
IL (1) IL78059A (ko)
MX (1) MX9203357A (ko)
NZ (1) NZ215404A (ko)
PH (1) PH23136A (ko)
PT (1) PT82149B (ko)
SU (1) SU1676449A3 (ko)
WO (1) WO1986005181A1 (ko)
ZA (1) ZA861235B (ko)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ219971A (en) * 1986-06-06 1989-08-29 Univ Princeton Tetrahydropyrido (2,3-d pyrimidine derivatives and pharmaceutical compositions
IE60038B1 (en) * 1986-06-30 1994-05-18 Univ Princeton 4(3H)-oxo-5, 6, 7, 8-tetrahydropyrido-[2, 3-d]pyrimidine derivatives
US4818819A (en) * 1986-10-20 1989-04-04 The Trustees Of Princeton University Process for the preparation of fused pyridine compounds
GB8702758D0 (en) * 1987-02-06 1987-03-11 Wellcome Found Treatment of disease
EP0278686A1 (en) * 1987-02-07 1988-08-17 The Wellcome Foundation Limited Pyridopyrimidines methods for their preparation and pharmaceutical formulations thereof
EP0305667A3 (en) * 1987-09-03 1989-10-25 American Cyanamid Company Improved process for producing 5,10-dideaza-(5,6,7,8)-tetrahydrofolic acid
US4895946A (en) * 1987-10-26 1990-01-23 The Trustees Of Princeton University Process for the preparation of fused pyridine compounds
US4889859A (en) * 1988-02-05 1989-12-26 The Trustees Of Princeton University Pyrido[2,3-d]pyrimidine derivatives
DK172753B1 (da) * 1988-05-25 1999-06-28 Lilly Co Eli N-(5,6,7,8-tetrahydropyrido[2,3--d]pyrimidin-6-yl-alkanoyl)-glutaminsyrederivater, deres anvendelse, farmaceutiske præparat
JPH03173890A (ja) * 1989-09-21 1991-07-29 Takeda Chem Ind Ltd ピロロ［２，３―ｄ］ピリミジン誘導体，その製造法，用途及び中間体
CA2066898A1 (en) * 1991-04-29 1992-10-30 Chuan Shih Pharmaceutical compounds
US5196424A (en) * 1992-03-24 1993-03-23 Eli Lilly And Company N-[2-amino-4-substituted[[(pyrrollo or pyrido)[2,3-d]pyrimidinyl]-alkyl]benzoyl]-L-glutamic acids
WO1993020075A1 (en) * 1992-04-01 1993-10-14 The University Of Sydney 8-substituted-n5-deazapterins as antifolates
ZA932731B (en) * 1992-04-23 1994-10-19 Lilly Co Eli Method of treating gar-transformylase-dependent tumors
JPH07506369A (ja) * 1992-04-29 1995-07-13 エス・アール・アイ・インターナシヨナル 炎症を処置するためのデアザアミノプテリン
US5594139A (en) * 1993-01-29 1997-01-14 Agouron Pharmaceuticals, Inc. Processes for preparing antiproliferative garft-inhibiting compounds
SG49234A1 (en) * 1993-01-29 1998-05-18 Agouron Pharma Condensed heterocyclic glutamic acid derivatives as antiproliferative agents
JP3473956B2 (ja) * 1994-07-28 2003-12-08 アグーロン ファーマシューティカルズ，インコーポレーテッド 抗増殖剤およびｇａｒｆｔ阻害剤として有用な化合物
CN1053448C (zh) * 1994-07-28 2000-06-14 阿格罗尼制药公司 用作抗增殖药物及garft抑制剂的化合物
US5831100A (en) * 1995-06-07 1998-11-03 Agouron Pharmaceuticals, Inc. Syntheses of optically pure compounds useful as GARFT inhibitors and their intermediates
HUP0201333A3 (en) 1999-05-24 2004-11-29 Sankyo Company Ltd Chuo Ku Medicinal compositions containing anti-fas antibody
EP2349274A4 (en) 2008-09-17 2014-12-17 Endocyte Inc CONJUGATES OF ANTIFOLATES BINDING THE FOLATE RECEPTOR
CN116333411B (zh) * 2023-05-29 2023-08-11 石家庄启宏新材料制品有限公司 一种阻燃eva保温材料及其制备方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4512992A (en) * 1980-06-13 1985-04-23 Burroughs Wellcome Co. Treatment with dialkoxy pyridopyrimidine compounds
US4431805A (en) * 1981-09-25 1984-02-14 Southern Research Institute Pyrido[2,3-d]-pyrimidines
US4526964A (en) * 1982-01-11 1985-07-02 Southern Research Institute 2,4-Diamino-6-(hydroxymethyl)pyrido[2,3-d]pyrimidine
US4536575A (en) * 1982-01-11 1985-08-20 Southern Research Institute 2-Amino-4(3H)-oxopyrido[2,3-d]pyrimidino
US4460591A (en) * 1982-08-26 1984-07-17 Sri International 8,10-Dideazaminopterins
US4532241A (en) * 1982-08-26 1985-07-30 Sri International 8,10-Dideazaminopterins
US4432981A (en) * 1982-11-05 1984-02-21 Sterling Drug Inc. 2-(Pyridinyl or hydroxyphenyl)-8-substituted pyrido[2,3-d]pyrimidin-5(8H)-ones
WO1985002844A1 (en) * 1983-12-27 1985-07-04 Sri International 8,10-dideazaminopterins

Also Published As

Publication number Publication date
CA1276637C (en) 1990-11-20
CN1016174B (zh) 1992-04-08
IL78059A0 (en) 1986-07-31
IE860561L (en) 1986-09-08
AU578813B2 (en) 1988-11-03
ATE96790T1 (de) 1993-11-15
PT82149A (en) 1986-04-01
ES8801268A1 (es) 1987-12-16
PH23136A (en) 1989-05-11
JPH08193084A (ja) 1996-07-30
DK472186D0 (da) 1986-10-02
DK472186A (da) 1986-12-19
EP0215063B1 (en) 1993-11-03
JPS62502535A (ja) 1987-10-01
IE63653B1 (en) 1995-05-31
DE3689250T2 (de) 1994-03-03
MX9203357A (es) 1992-07-01
IL78059A (en) 1989-06-30
AU5510886A (en) 1986-09-24
SU1676449A3 (ru) 1991-09-07
CN86101475A (zh) 1987-01-21
GR860592B (en) 1986-06-26
NZ215404A (en) 1990-03-27
ES8704167A1 (es) 1987-03-16
ES557174A0 (es) 1987-12-16
EP0215063A4 (en) 1987-11-23
HUT41785A (en) 1987-05-28
DE3689250D1 (de) 1993-12-09
WO1986005181A1 (en) 1986-09-12
PT82149B (pt) 1988-04-21
KR940002952B1 (ko) 1994-04-09
DK168666B1 (da) 1994-05-16
EG18371A (en) 1993-04-30
HU196202B (en) 1988-10-28
EP0215063A1 (en) 1987-03-25
ZA861235B (en) 1986-10-29
JPH0822860B2 (ja) 1996-03-06
ES552684A0 (es) 1987-03-16

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