KR890701579A - Malic acid derivatives containing renin inhibitory peptides - Google Patents

Malic acid derivatives containing renin inhibitory peptides

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Publication number
KR890701579A
KR890701579A KR1019890700388A KR890700388A KR890701579A KR 890701579 A KR890701579 A KR 890701579A KR 1019890700388 A KR1019890700388 A KR 1019890700388A KR 890700388 A KR890700388 A KR 890700388A KR 890701579 A KR890701579 A KR 890701579A
Authority
KR
South Korea
Prior art keywords
alkyl
hydroxy
het
aryl
amino
Prior art date
Application number
KR1019890700388A
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Korean (ko)
Inventor
차이스리봉스 슈비트
Original Assignee
로버어트 에이 아미테이지
디 엎존 캄파니
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.)
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Application filed by 로버어트 에이 아미테이지, 디 엎존 캄파니 filed Critical 로버어트 에이 아미테이지
Publication of KR890701579A publication Critical patent/KR890701579A/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • 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
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

내용 없음No content

Description

레닌 억제 펩타이드를 함유하는 말산 유도체Malic acid derivatives containing renin inhibitory peptides

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (5)

하기 일반식 Ⅰ의 레닌 억제 펩타이드 또는 제약적으로 허용가능한 이들의 산 또는 염기 부가염류; Z-C(O)-CH(OH)-CH(CH2R1)-C(O)-N(R2)CH(CH2R3)-(C(O))-NH-CH(CH2R4)-X-C(R5)(R2)-C(O)-Y-ZRenin inhibitory peptides of Formula I or pharmaceutically acceptable acid or base addition salts thereof; ZC (O) -CH (OH) -CH (CH 2 R 1 ) -C (O) -N (R 2 ) CH (CH 2 R 3 )-(C (O))-NH-CH (CH 2 R 4 ) -XC (R 5 ) (R 2 ) -C (O) -YZ 상기식에서, X는Where X is (a) -CH(OH)- : (f) -CH(NH2)-CH2;(a) -CH (OH)-: (f) -CH (NH 2 ) -CH 2 ; (b) -CH(NH2); (g) -C(O)-CH2;(b) -CH (NH 2 ); (g) -C (O) -CH 2 ; (c) -C(O)- ; (h) -CH2-NH- ;(c) -C (O)-; (h) -CH 2 -NH-; (d) -CH(OH)-CH(OH)-; (i) -CH2-O- ; 또는(d) -CH (OH) -CH (OH)-; (i) -CH 2 -O-; or (e) -CH(OH)-CH2- ; (j) -P(O)(A)(B)-(여기에서,(e) -CH (OH) -CH 2- ; (j) -P (O) (A) (B)-(where A는 (a) -OH 또는 (b) -NH2;A is (a) -OH or (b) -NH 2 ; B는 (a) 없음; (c) -NH- ; 또는B is (a) absent; (c) -NH-; or (b) -O- ; (d) -CH2-임 이고 ;(b) -O-; (d) -CH 2- ; 상기식에서, Y는Where Y is (a) 없거나 (b) -NHCH(R5)C(O)-이고;(a) absent or (b) -NHCH (R 5 ) C (O)-; 상기식에서, Z는 (a) -O-R4; (b) -N(R2)R6; 또는 (c) 질소 원자를 통해 결합한 Het 이고 ; 상기식에서, R1은Wherein Z is (a) -OR 4 ; (b) -N (R 2 ) R 6 ; Or (c) Het bonded via a nitrogen atom; Wherein R 1 is (a) 수소 ; (d) -(CH2)p-Het;(a) hydrogen; (d)-(CH 2 ) p-Het; (b) C1-C5알킬 ; (e) -(CH2)p-(C3-C7) 시클로알킬;(b) C 1 -C 5 alkyl; (e)-(CH 2 ) p- (C 3 -C 7 ) cycloalkyl; (c) -(CH2)p-아릴; (f) -(CH2)-S-아릴;(c)-(CH 2 ) p -aryl; (f)-(CH 2 ) -S-aryl; (g) -(CH2)p-S-Het; (i) -(CH2)-S-(C3-C7(시클로알킬));(g)-(CH 2 ) p -S-Het; (i)-(CH 2 ) -S- (C 3 -C 7 (cycloalkyl)); (h) -(CH2)p-S-(C1-C5) 알킬; 또는 (h) - (CH 2) p -S- (C 1 -C 5) alkyl; or 상기식에서, R2는 (a) 수소; 또는 (b) C1-C5알킬;Wherein R 2 is (a) hydrogen; Or (b) C 1 -C 5 alkyl; 상기식에서, R3는Wherein R 3 is (a) 수소; (f) -(CH2)p-NH-C(NH2)=NH;(a) hydrogen; (f)-(CH 2 ) p -NH-C (NH 2 ) = NH; (b) C1-C5알킬; (g) -(CH2)p-아릴;(b) C 1 -C 5 alkyl; (g)-(CH 2 ) p -aryl; (c) -(CH2)p-OH; (h) -(CH2)p-Het ; 또는(c)-(CH 2 ) p -OH; (h)-(CH 2 ) p -Het; or (d) -(CH2)p-CO2H ; (i) -(CH2)-(C3-C7) 시클로알킬;(d)-(CH 2 ) p -CO 2 H; (i)-(CH 2 )-(C 3 -C 7 ) cycloalkyl; (e) -(CH2)p-NH2;(e)-(CH 2 ) p -NH 2 ; 상기식에서, R4는Wherein R 4 is (a) 수소 ; (e) Het(a) hydrogen; (e) Het (b) C1-C5알킬; (f) -(CH2)p-OH; 또는(b) C 1 -C 5 alkyl; (f)-(CH 2 ) p -OH; or (c) C3-C7시클로알킬; (g) -(CH2)p-NH3;(c) C 3 -C 7 cycloalkyl; (g)-(CH 2 ) p -NH 3 ; (d) 아릴;(d) aryl; 상기식에서 R5는,In which R 5 is (a) 수소;(a) hydrogen; (b) C1-C5알킬; (d) -(CH)-p-Het; 또는(b) C 1 -C 5 alkyl; (d)-(CH) -p-Het; or (c) -(CH2)p-아릴; (e) -(CH2)-p-(C3-C7)시클로알킬;(c)-(CH 2 ) p -aryl; (e) - (CH 2) - p - (C 3 -C 7) cycloalkyl; 상기식에서, R6는Wherein R 6 is (a) 수소; (d) -C1-C10알킬;(a) hydrogen; (d) -C 1 -C 10 alkyl; (b)아릴; (e) -(CH2)p-(C3-C7) 시클로알킬 ; 또는(b) aryl; (e)-(CH 2 ) p- (C 3 -C 7 ) cycloalkyl; or (c) Het (f) -(CH2)p-R7;(c) Het (f)-(CH 2 ) p -R 7 ; 상기식에서 R7은,In formula, R 7 is (a) 아릴 ; (e) 폴리 히드록실화된 알킬;(a) aryl; (e) poly hydroxylated alkyl; (b) Het; (f)-COOH;(b) Het; (f) -COOH; (c) 히드록시; (g) 구아니딜; 또는(c) hydroxy; (g) guanidyl; or (d) 아미노; (h) -SO3H;(d) amino; (h) -SO 3 H; 상기식에서, p는 0내지 5(5포함) ;Wherein p is 0 to 5 (including 5); 상기식에서, n은 1내지 5(5포함) ;Wherein n is 1 to 5 (including 5); 상기식에서, 아릴은Wherein aryl is (a) C1-C3알킬; (h) -CH2H;(a) C 1 -C 3 alkyl; (h) -CH 2 H; (b) 히드록시; (i) -CH2(C1-C3) 알킬;(b) hydroxy; (i) -CH 2 (C 1 -C 3 ) alkyl; (c) C1-C3알콕시; (j) -CONH2;(c) C 1 -C 3 alkoxy; (j) -CONH 2 ; (d) 할로겐; (k) -CONH-(C1-C3)알킬;(d) halogen; (k) -CONH- (C 1 -C 3) alkyl; (e) 아미노; (l) 니트로;(e) amino; (l) nitro; (f) 모노 또는 디(C1-C3)알킬아미노; (m) 머캅토;(f) mono or di (C 1 -C 3 ) alkylamino; (m) mercapto; (g) -CHO; (n) C1-C3알킬티오;(g) -CHO; (n) C 1 -C 3 alkylthio; (o) -SO3H (q) -CN(o) -SO 3 H (q) -CN (p) -SO2NH2; 또는(p) -SO 2 NH 2 ; or 중 0 내지 3개로 치환된 나프틸 또는 페닐; 상기식에서, Het 는 1-3개의 헤테로원자(질소, 산소, 황)를 함유하고 임의로 이환식 기(여기에서, 임의의 상기 헤테로시크릭 고리는 벤젠 고리 또는 다른 헤테로사이클에 융합됨)를 포함하는, 6 또는 6-구성원 포화 또는 불포화 고리이고: 화합적으로 실행가능하다면, 장소 및 황원자는 산화된 형태로 있을 수 있고: 단, X가Naphthyl or phenyl substituted with 0 to 3 of them; Wherein Het contains 1-3 heteroatoms (nitrogen, oxygen, sulfur) and optionally comprises a bicyclic group, where any of said heterocyclic ring is fused to a benzene ring or other heterocycle, Is a 6 or 6-membered saturated or unsaturated ring: if it is feasible in practice, the moiety and sulfur atoms may be in oxidized form provided that X is (a) -CH(OH)-; (c) -(C(O)o-인 경우,(a) -CH (OH)-; (c)-(C (O) o-, (b) -CH(NH2) ; 및(b) -CH (NH 2 ); And R2및 R5가 함께 결합하여 -F2; -Cl2-; -FH- 또는 -C1H-, 또는 카르복시-, 아미노- 또는 이들의 다른 반응선기 보호 형태를 형성할 수 있다.R 2 and R 5 are bonded together to form —F 2 ; -Cl 2- ; -FH- or -C1H-, or carboxy-, amino- or other reactive group protective forms thereof. 제1항에 있어서, 3S-히드록시-4-모노폴리노-2R-벤질숙시노일-Nim-토실-L-히스티딜-5S-아미노-4S-히드록시-2S-이소프로필-7-메틸옥타노일-L-이소푸실-2-피리딜메틸아민인 화합물.The compound of claim 1, wherein the 3S-hydroxy-4-monofolino-2R-benzylsuccinoyl-N im -tosyl-L-histidyl-5S-amino-4S-hydroxy-2S-isopropyl-7-methylocta Noyl-L-isofusyl-2-pyridylmethylamine. 제1항에 있어서, 3S-히드록시-4-모르폴리노-2R-(1'-나프틸메틸)숙시노일-Nim-토실-L-히스티딜-5S-아미노-4S-히드록시-2S-이소프로필-7-메틸옥타노일-L-이소루실-2-피리딜 메틸아민인 화합물.The compound of claim 1, wherein the 3S-hydroxy-4-morpholino-2R- (1′-naphthylmethyl) succinoyl-N im -tosyl-L-histidyl-5S-amino-4S-hydroxy-2S Isopropyl-7-methyloctanoyl-L-isosilyl-2-pyridyl methylamine. 제1항에 있어서. 3S-히드록시-4-모르폴리노-2R-벤질숙시노일-L-히스티딜-5S-아미노-4S-히드록시-2S-이소프로필-7-메틸옥타노일-L-이소루실-2-피리딜 메틸아민인 화합물.The method of claim 1. 3S-hydroxy-4-morpholino-2R-benzylsuccinoyl-L-histidyl-5S-amino-4S-hydroxy-2S-isopropyl-7-methyloctanoyl-L-isosilyl-2-pyri A compound that is diyl methylamine. 제2항에 있어서, 3S-히드록시-4-모르폴리노-2R-(1'-나프틸메틸)숙시노일-L-히스티딜-5S-아미노-4S-히드록시-2S-이소프로필-7-메틸옥타노일-L-이소루실-2-피리딜 메틸아민인 화합물.The compound of claim 2, wherein the 3S-hydroxy-4-morpholino-2R- (1′-naphthylmethyl) succinoyl-L-histidyl-5S-amino-4S-hydroxy-2S-isopropyl-7 -Methyloctanoyl-L-isosilyl-2-pyridyl methylamine. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019890700388A 1987-06-29 1988-05-13 Malic acid derivatives containing renin inhibitory peptides KR890701579A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US6809587A 1987-06-29 1987-06-29
US068095 1987-06-29
PCT/US1988/001535 WO1989000161A1 (en) 1987-06-29 1988-05-13 Malic acid derivative containing renin inhibiting peptides

Publications (1)

Publication Number Publication Date
KR890701579A true KR890701579A (en) 1989-12-21

Family

ID=22080381

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019890700388A KR890701579A (en) 1987-06-29 1988-05-13 Malic acid derivatives containing renin inhibitory peptides

Country Status (5)

Country Link
EP (1) EP0366669A1 (en)
JP (1) JPH02504143A (en)
KR (1) KR890701579A (en)
AU (1) AU1780588A (en)
WO (1) WO1989000161A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2086341T3 (en) * 1989-09-12 1996-07-01 Hoechst Ag DERIVATIVES OF AMINO ACIDS WITH RENINE INHIBITING PROPERTIES, PROCEDURE FOR THEIR PREPARATION, AGENTS CONTAINING THEM AND THEIR USE.

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU573735B2 (en) * 1983-02-07 1988-06-23 Aktiebolaget Hassle Peptide analogue enzyme inhibitors
DE3438545A1 (en) * 1984-10-20 1986-04-24 Merck Patent Gmbh, 6100 Darmstadt PEPTIDE
KR870005013A (en) * 1985-11-29 1987-06-04 가와무라 요시부미 Lenin-inhibiting oligopeptides, methods of making and uses thereof

Also Published As

Publication number Publication date
AU1780588A (en) 1989-01-30
EP0366669A1 (en) 1990-05-09
WO1989000161A1 (en) 1989-01-12
JPH02504143A (en) 1990-11-29

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