KR880013902A - 아미노산 유도체 - Google Patents

아미노산 유도체 Download PDF

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KR880013902A
KR880013902A KR1019880006097A KR880006097A KR880013902A KR 880013902 A KR880013902 A KR 880013902A KR 1019880006097 A KR1019880006097 A KR 1019880006097A KR 880006097 A KR880006097 A KR 880006097A KR 880013902 A KR880013902 A KR 880013902A
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amino
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methyl
carbon atoms
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라다쯔 페터
좀브로에크 요하네스
간데 요아힘
제어 슈미트게스 클라우스
오토 민크 클라우스
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나우만,호이만
메르크 파텐트 게젤샤프트 미트 베슈랭크터 하프퉁
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    • 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
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0227—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the (partial) peptide sequence -Phe-His-NH-(X)2-C(=0)-, e.g. Renin-inhibitors with n = 2 - 6; for n > 6 see C07K5/06 - C07K5/10

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
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  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Cardiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Crystallography & Structural Chemistry (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

내용 없음

Description

아미노산 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 일반식(Ⅰ)의 아미노산 유도체 및 이의 염.
    X-VCHR2-CHOH-Z-(CH2)a-CO-NR3-CHR4-CR5-(CHR6)n-CO-E-Q-Y (Ⅰ)
    상기식에서, X는 H,R1,R1-O-Cm-H2m-CO-, R1-CmH2-O-CO,R1-CmH2m-CO-,R1-SO2-,(R1-CmH2m)-,L(R7-CpH2p)-CrH2-CO-, R1-(NHCH2CH2)m-,NH-CH2CO, 9-플루오텐일-CmH2m-O-CO-,또는 (R1-CmH2m-(T)X-CO-CrH2r)-L(R7-CpH2p)-CyH2y-CO-이고 V는 -CH2-,O-또는 -NR8-이고, Z는 -CH2,-CH=CH-, -C=C-, -CH2-O-, -CH2-NR9-또는 -CH2-S-이고, E는 펩티트 형태로 상호 결합된 0내지 2의 아미노산 라디칼이고 AbU, Ala, Cal, His, Ile, Leu, Met, Nle, Phe, Trp, Tyr 및 Val를 포함하는 그룹에서 선택되고, Q및 T는 각각 0또는 NH 이고, Y는 -CtH2t-R10또는 -CwH2w-(CR11)s-CtH2t-R10이고, R1, R2, R4, R7및 R10은 각기 H, A, Ar-알킬, Het 또는 Het-알킬, 또는 각기 비치완 또는 A, AO 및/또는 Hal로 일치환 또는 다치환된 탄소수 3내지 7의 시클로알킬, 탄소수 4내지 11의 시클로알킬알킬, 각기 탄소수 7내지 14의 비시클로알킬 또는 트리시클로알킬 또는 각기 탄소수 8내지 18의 비시클로알킬알킬 또는 트리시클로알킬알킬이고, R3, R6, R8및 R9은 각기 H또는 A이고, R5및 R11은 각기 (H, OH), (H, NH2)또는=0이고, L는 CH 또는 N이고, a,m,p,r,t,w및 y는 각기 0,1,2,3,4,5,6,7,8,9 또는 10이고, n 및 s는 각기 1또는 2이고, X는 0또는 1이고 Ar는 비치환 또는 A, AO, Hal, CF3, HO, H2NCO, HANCO, A2NCO, H2NSO2, HANSO2, A2NSO2, 탄소수 1내지 8의 히드록시알킬, H2N 및/또는 탄소수 1내지 8의 아미노알킬로 일치환 또는 다치환된 페닐, 또는 비치환된 나프틸이고, Het는 1내지 4의 N, O 및/또는 S 원자를 갖는 포화 또는 불포화된 5-원 또는 6-원 헤테로시클릭라디칼로서 벤젠링과 융합할 수 있고/있거나, A, AO, Hal, CF3, HO, O2N, 카보닐 산소, H2N, HAN, A2N, AcNH, AS, ASO, ASO2, AOOC, CN, H2NCO, NOOC, H2NSO2, ASO2NH, Ar 또는 Ar-알케닐, 각기 탄소수 1내지 8의 히드록시 알킬 및/ 또는 S 헤테로원자는 또한 산화될 수 있고, Hal은 F, Cl, Br 또는 1이고, Ac는 A-CO-, Ar-CO-또는 A-NH-CO-이고,A는 탄소수 1내지 8의 알킬이며, 또한 여기에서 하나 또는 그이상의 -NH-CO-그룹은 하나 또 그 이상의 -NA-CO-그룹으로 치환될 수도 있다.
  2. a)N-(3-티아-5-히드록시-6S-BOC-아미노-7-페닐-헵타노일)-모체-Ile-(N-3-피리딜-메틸-아미드) ; b)N-(4-히드록시-5-BOC-아미노-6-페닐-헥사노일)-AHCP-Ile-(N-2-아미노-5, 6-디메틸-3-피라지닐-메틸-아미드) ; c)N-(3-티아-5-히드록시-6S-BOC-아미노-7-페닐-헵타노일)-AHCP-Ile-(N-2-아미노-5, 6-디메틸-3-피리지닐-메틸-아미드) ; d)N-(3-티아-5-히드록시-6S-BOC-아미노-7-페닐-헵타노일)-AHCP-Ile-(N-4-아미노-2-메틸-5-피리미디닐-메틸-아미드) ; e)N-(4-히드록시-5-BOC-아미노-6-페닐-헥사노일)-AHCP-Ile-(N-4-아미노-2-메틸-5-피리미디닐-메틸-아미드).
  3. 일반식(I) 및 이들 임의 아미노산 유도체를 제조하는 방법에 있어서, 그의기능성 유도체중의 하나를 가용매 분해제 또는 가수소분해제로 처리하여 유리하거나, 또는 일반식(Ⅱ)의 카복실산 또는 이의 반응 유도체중의 하나를 일반식(Ⅲ)의 화합물 또는 이의 반응 유도체중의 하나와 반응시키거나, 또는 일반식(Ⅳ)의 화합물을 환원제로 처리하고/하거나, 필요하다면, 일반식(Ⅰ)의 화합물에 있어서, 기능적으로 변형된 아미노 그룹 및/또는 히드록실 그룹을 가용매 분해제 또는 가수소분해제로 처리하여 유리하고/하거나, 유리아미노 그룹 또는 히드록실 그룹을 아실화 하고/하거나, 케토 그룹을 CHOH그룹으로 환원하거나 CH(NH2)그룹으로 환원적으로 아미노화 하고/하거나, 일반식(Ⅰ)화합물을 산으로 처리하여 이의 임중 하나로 전환시키는 것을 특징으로 하는, 일반식(Ⅰ) 및 이의 염의 아미노산 유도체의 제조방법.
    X-V-CHR2-CHOH-Z-(CH2)a-G1-OH (Ⅱ)
    H-G2(Ⅲ)
    X-V-CHR2-CO-Z-(CH2)a-CO-W-E-Q-Y (Ⅸ)
    상기식에서, G1은 (a)-CO (b)-CO-2 (c)-CO-W-E1-또는 (d)-CO-W-E-이고 W는 -NR3-CHR4-CR5-(CHR6)n-CO-이고, G2는 (a)-W-E-Q-Y, (b)-E-Q-Y, (c)-E2-Q-Y 또는 (d)-Q-Y이고 E1및 E2는 모두 E이다.
  4. 일반식(Ⅰ)의 화합물 및/또는 이의 생리학적으로 허용가능한 염중 하나를 고체, 액체 또는 반-액체 부형제 또는 보조제의 적어도 1종과 함께 필요하다면 1종 또는 그 이상의 다른 활성화합물과 조합하여 적합한 투여형태로 전환시키는 것을 특징으로 하는 약학적 제형의 제조방법.
  5. 일반식(Ⅰ)의 화합물을 적어도 1종 및/또는 이의 생리학적으로 허용가능한 염중 하나를 함유함을 특징으로 하는 약학제 제형.
  6. 일반식(Ⅰ)의 화합물 또는 이의 생리학적으로 허용가능한 염의 레닌-의존형 고혈압 또는 과알도스테론증 치료에 있어서의 용도.
  7. 일반식(Ⅰ)의 화합물 또는 이의 생리학적으로 허용가능한 염의 레닌-의존형 고혈압 또는 과알도스테론중 치료용 의약품의 제조를 위한 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880006097A 1987-05-25 1988-05-25 아미노산 유도체 Withdrawn KR880013902A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DEP3717631.5 1987-05-25
DE19873717631 DE3717631A1 (de) 1987-05-26 1987-05-26 Aminosaeurederivate

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KR880013902A true KR880013902A (ko) 1988-12-22

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EP (1) EP0292800A3 (ko)
JP (1) JPH01163164A (ko)
KR (1) KR880013902A (ko)
AU (1) AU610588B2 (ko)
DE (1) DE3717631A1 (ko)
HU (1) HU205951B (ko)
ZA (1) ZA883782B (ko)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1340588C (en) * 1988-06-13 1999-06-08 Balraj Krishan Handa Amino acid derivatives
CA2010531A1 (en) * 1989-03-06 1990-09-06 Werner Neidhart Amino acid derivatives
DE3913290A1 (de) * 1989-04-22 1990-10-25 Hoechst Ag Renin-hemmende di- und tripeptide, verfahren zu deren herstellung, diese enthaltende mittel und ihre verwendung
DE4033062A1 (de) * 1990-10-18 1992-04-23 Merck Patent Gmbh Aminosaeurederivate
GB8927913D0 (en) * 1989-12-11 1990-02-14 Hoffmann La Roche Amino acid derivatives
DE4021512A1 (de) * 1990-07-05 1992-01-16 Merck Patent Gmbh Aminosaeurederivate

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2561733B1 (fr) * 1984-03-20 1986-08-22 Peugeot Barre de torsion tubulaire
DE3418491A1 (de) * 1984-05-18 1985-11-21 Merck Patent Gmbh, 6100 Darmstadt Diaminosaeurederivate
EP0163237A3 (en) * 1984-05-29 1988-04-27 Merck & Co. Inc. Di- and tri-peptidal renin inhibitors
DE3438545A1 (de) * 1984-10-20 1986-04-24 Merck Patent Gmbh, 6100 Darmstadt Peptide
DE3538749A1 (de) * 1985-10-31 1987-05-07 Merck Patent Gmbh Peptide
DE3540495A1 (de) * 1985-11-15 1987-05-21 Merck Patent Gmbh Aminosaeurederivate
EP0249096B1 (de) * 1986-06-10 1995-01-11 Merck Patent Gmbh Reninhemmende Aminosäurederivate.
DE3635907A1 (de) * 1986-10-22 1988-04-28 Merck Patent Gmbh Hydroxy-aminosaeurederivate
DE3804793A1 (de) * 1988-02-16 1989-08-24 Hoechst Ag Renin-hemmende aminosaeurederivate
DE3809145A1 (de) * 1988-03-18 1989-09-28 Merck Patent Gmbh Aminosaeurederivate
DE3812328A1 (de) * 1988-04-14 1989-10-26 Merck Patent Gmbh Aminosaeurederivate

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HU205951B (en) 1992-07-28
ZA883782B (en) 1989-01-25
DE3717631A1 (de) 1988-12-15
EP0292800A3 (de) 1990-11-22
AU610588B2 (en) 1991-05-23
HUT49148A (en) 1989-08-28
AU1630088A (en) 1989-02-16
EP0292800A2 (de) 1988-11-30
JPH01163164A (ja) 1989-06-27

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