KR880007562A - 레닌 억제제iii - Google Patents

레닌 억제제iii Download PDF

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Publication number
KR880007562A
KR880007562A KR870014292A KR870014292A KR880007562A KR 880007562 A KR880007562 A KR 880007562A KR 870014292 A KR870014292 A KR 870014292A KR 870014292 A KR870014292 A KR 870014292A KR 880007562 A KR880007562 A KR 880007562A
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KR
South Korea
Prior art keywords
nhch
dnma
peptide
reacting
sta
Prior art date
Application number
KR870014292A
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English (en)
Inventor
페리 허드스페드 제임스
스탠리 칼텐브론 제임스
토마스 리파인 조셉
하워드 로악 윌리암
앤드류 스티어 마이클
Original Assignee
크리스틴 에이.트라우트웨인
워너 람버트 컴퍼니
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
Priority claimed from US06/941,966 external-priority patent/US4735933A/en
Application filed by 크리스틴 에이.트라우트웨인, 워너 람버트 컴퍼니 filed Critical 크리스틴 에이.트라우트웨인
Publication of KR880007562A publication Critical patent/KR880007562A/ko

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/14—Angiotensins: Related peptides
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • 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
    • 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
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S530/00—Chemistry: natural resins or derivatives; peptides or proteins; lignins or reaction products thereof
    • Y10S530/86—Renin inhibitors

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Vascular Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

내용 없음.

Description

레닌 억제제Ⅲ
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 다음 일반식의 펩티드 및 이의 제약학적으로 허용가능한 산 부가염.
    식중, ACYL은 DNMA, R이 C1-6의 직쇄 또는 분지된 저급알킬 이거나 수소인
    X는 HIS, HOMOHIS.PHE, HOMOPHE, ILE, LEU, NLE, N-MeHIS, N-MeLEU, 또는; Y는 STA, CYSTA, 또는 PHSTA ; W는 ACYL이 DNMA일 경우 LEU, lLE, N-MeLEU, N-MeILE, VAL이고 그이외에는 존재하지 않는다 ; U는 -NHCH2CH(CH3)CH2CH3, -NHCH2Ph,, -NHCH2CH(OH)CH2SCH(CH3)2, -NHCH2CH(OH)CH2SOCH(CH3)2, -NHCH2CH(OH)CH2SO2CH(CH3)2.
  2. 제1항에 있어서 U가
    -NHCH2CH=CH2, -NHCH2CH(OH)CH2SCH(CH3)2, -NHCH2CH(OH)CH2SOCH(CH3)2, -NHCH2CH(OH)CH2SO2CH(CH3)2,또는 -NHCH2CH(CH3)CH2CH3인 팹티드
  3. 제1항에 있어서, 펩티드가 DNMA-HIS-STA-LEU-NHCH2Ph,
    DNMA-(D-HIS)-STA-LEU-NHCH2Ph, DNMA-HIS-STA-(D-LEU)-NHCH2Ph, DNMA-(N-MeHIS)-STA-LEU-NHCH2Ph, DNMA-HIS-STA-(N-MeLEU)-NHCH2Ph, DNMA-HIS-CYSTA-LEU-NHCH2Ph,
    로 구성된 그룹으로 부터 선택된 펩티드.
  4. DNMA-HIS-STA-NHCH2CH(OH)CH2SO2CH(CH3)2.로 지정된 화합물.
  5. 제1항에 있어서, (a) 보호된 -NH-치환된-1-알켄과 에폭시화제를 반응시켜 당해 에폭사이드를 만들고 (b) 이 에폭사이드를 머캅탄과 반응시켜 당해 보호된 티오에테르를 형성시킨 뒤 (c) 보호그룹을 제거하여 당해 유리 아미노 말단을 갖는 화합물을 만들어 (d) 아민을 아미노산과 반응시키거나 또는 유리된 말단 카복실그룹을 갖는 펩티드와 반응시켜 티오가 함유된 아미드 부분을 갖는 당해 펩티드를 형성하는 것으로 구성되며 만일 원한다면 펩티드를 제약학적으로 허용가능한 산 부가염으로 전환시키는, 티오가 함유된 아미드 부분을 갖는 펩티드의 제조방법.
  6. 제1항에 있어서, (a) 보호된 -NH-치환된-1-알켄과 에폭시화제를 반응시켜 당해 에폭사이드를 만들고 (b) 이 에폭사이드를 머캅탄과 반응시켜 당해 보호된 티오에테르를 형성하고 (c) 이 티오에테르를 산화시켜 당해 설폰으로 만든뒤 (d) 설폰이 함유된 화합물을 HCl과 반응시켜 유리 아미노 말단기를 생산하고 (e) 아민을 유리 말단카복실 그룹을 갖는 펩티드 또는 아미노산과 반응시켜 설폰일을 함유하는 아미드 부분을 갖는 펩티드를 형성하는 것으로 구성되며 만일 원한다면 펩티드를 제약학적으로 허용 가능한 산 부가 염으로 전환시키는 것으로 구성된 펩티드 제조방법.
  7. 레닌을 억제하는 효과적인 양의 제1항에서의 화합물과 제약학적으로 허용가능한 담체로 구성된 제약학적 조성물.
  8. 레닌을 억제하는 효과적이 양의 제4항에서의 화합물과 제약학적으로 허용가능한 담체로 구성된 제약학적 조성물.
  9. 제7항의 제약학적 조성물을 포유동물에 투여 하는 것으로 구성된 레닌에 의한 고혈압증을 치료하는 방법.
  10. 제8항의 제약학적 조성물을 포유동물에 투여하는 것으로 구성된 레닌에 의한 고혈압증을 치료하는 방법.
  11. 과알도스테론증을 억제하는 효과적인양의 제1항에서의 화합물과 제약학적으로 허용가능한 담체로 구성된 제약학적 조성물.
  12. 제11항의 제약학적 조성물을 포유동물에 투여하는 것으로 구성된 과알도스테론증의 치료방법.
  13. 혈압을 낮추는 복용량의 단일투약으로 제1항의 펩티드를 환자에 투약하고 환자의 헐압을 조사하는 것으로 구성된 레닌에 의한 고혈압 환자를 구별하는 방법.
  14. 울혈성 심부전을 치료하기에 효과적인 양의 제1항의 화합물과 제약학적으로 허용가능한 담체로 구성된 제약학적 조성물.
  15. 제14항의 제약학적 조성물을 포유동물에 투여하는 것으로 구성된 울혈성 심 부전증의 치료방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR870014292A 1986-12-15 1987-12-15 레닌 억제제iii KR880007562A (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US941966 1986-12-15
US06/941,966 US4735933A (en) 1986-12-15 1986-12-15 Renin inhibitors III
US07/113,277 US4895834A (en) 1986-12-15 1987-11-02 Renin inhibitors III
US113277 1987-11-02

Publications (1)

Publication Number Publication Date
KR880007562A true KR880007562A (ko) 1988-08-27

Family

ID=26810874

Family Applications (1)

Application Number Title Priority Date Filing Date
KR870014292A KR880007562A (ko) 1986-12-15 1987-12-15 레닌 억제제iii

Country Status (10)

Country Link
US (1) US4895834A (ko)
EP (1) EP0271862A3 (ko)
KR (1) KR880007562A (ko)
AU (1) AU605212B2 (ko)
DK (1) DK651087A (ko)
FI (1) FI875455A (ko)
NO (1) NO875199L (ko)
NZ (1) NZ222754A (ko)
PH (2) PH23734A (ko)
PT (1) PT86374B (ko)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4921855A (en) * 1987-06-22 1990-05-01 Fujisawa Pharmaceutical Co., Ltd. New Histidyl amino acid derivatives, and pharmaceutical composition comprising the same
ATE107658T1 (de) * 1988-01-26 1994-07-15 Sankyo Co Renin inhibierende polypeptide, ihre herstellung und anwendung.
DE3915755A1 (de) * 1989-05-13 1990-11-29 Bayer Ag Fungizide mittel sowie substituierte aminosaeureamid-derivate und deren herstellung
ES2097208T3 (es) 1990-05-11 1997-04-01 Pfizer Composiciones y procedimientos terapeuticos y sinergicos.
US5821232A (en) * 1990-05-11 1998-10-13 Pfizer Inc. Synergistic therapeutic compositions and methods
US5244910A (en) * 1990-08-15 1993-09-14 Abbott Laboratories Renin inhibitors
US5258362A (en) * 1991-06-11 1993-11-02 Abbott Laboratories Renin inhibiting compounds
US5212185A (en) * 1992-08-14 1993-05-18 G. D. Searle & Co. Piperidinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
US5780494A (en) * 1994-11-14 1998-07-14 G. D. Searle & Co. Piperidinyl-terminated alkylamino ethynl alanine amino diol compounds for treatment of hypertension
EP1723962A1 (en) * 2005-05-19 2006-11-22 IMBA-Institut für Molekulare Biotechnologie GmbH Use of inhibitors of the renin-angiotensin system for the treatment of lung injuries

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0114993B1 (en) * 1982-12-27 1990-05-16 Merck & Co. Inc. Renin inhibitory tripeptides
EP0173481A3 (en) * 1984-08-06 1988-12-21 The Upjohn Company Peptides
SU1676454A3 (ru) * 1984-11-30 1991-09-07 Санкио Компани Лимитед (Фирма) Способ получени пептидов или их фармацевтически приемлемых солей
KR870005013A (ko) * 1985-11-29 1987-06-04 가와무라 요시부미 레닌-억제 올리고펩티드, 그의 제조방법 및 용도
US4735933A (en) * 1986-12-15 1988-04-05 Warner-Lambert Company Renin inhibitors III
NZ222755A (en) * 1986-12-23 1989-11-28 Warner Lambert Co Renin inhibiting acyl peptide derivatives containing two to four amino acid residues, and pharmaceutical compositions
FI89058C (fi) * 1987-02-27 1993-08-10 Yamanouchi Pharma Co Ltd Foerfarande foer framstaellning av som remin-inhibitorer anvaenda 2-(l-alanyl-l-histidylamino)-butanol-derivat
DK523288A (da) * 1987-10-06 1989-04-07 Hoffmann La Roche Aminosyrederivater

Also Published As

Publication number Publication date
NO875199L (no) 1988-06-16
EP0271862A2 (en) 1988-06-22
PH24655A (en) 1990-09-07
AU8207287A (en) 1988-06-30
PH23734A (en) 1989-11-03
PT86374B (pt) 1990-11-20
NZ222754A (en) 1989-12-21
EP0271862A3 (en) 1990-11-14
US4895834A (en) 1990-01-23
AU605212B2 (en) 1991-01-10
FI875455A0 (fi) 1987-12-11
NO875199D0 (no) 1987-12-14
DK651087D0 (da) 1987-12-11
DK651087A (da) 1988-06-16
PT86374A (en) 1988-01-01
FI875455A (fi) 1988-06-16

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