KR927003521A - 펩티딜(peptidyl) 유도체 - Google Patents

펩티딜(peptidyl) 유도체 Download PDF

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KR927003521A
KR927003521A KR1019920701788A KR920701788A KR927003521A KR 927003521 A KR927003521 A KR 927003521A KR 1019920701788 A KR1019920701788 A KR 1019920701788A KR 920701788 A KR920701788 A KR 920701788A KR 927003521 A KR927003521 A KR 927003521A
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cyclohexylalanine
amide
hydroxyamino
compound
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KR1019920701788A
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죤 로버트 포터
죤 리차드 멀피
토마스 앤드류 밀리칸
니겔 로버트 아놀드 빌레이
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죤 에드워드 베리만
쎌텍크 리미티드
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Priority claimed from GB909026251A external-priority patent/GB9026251D0/en
Priority claimed from GB919110339A external-priority patent/GB9110339D0/en
Priority claimed from GB919110338A external-priority patent/GB9110338D0/en
Priority claimed from GB919112901A external-priority patent/GB9112901D0/en
Priority claimed from GB919112888A external-priority patent/GB9112888D0/en
Priority claimed from GB919115038A external-priority patent/GB9115038D0/en
Priority claimed from GB919115039A external-priority patent/GB9115039D0/en
Priority claimed from GB919115916A external-priority patent/GB9115916D0/en
Application filed by 죤 에드워드 베리만, 쎌텍크 리미티드 filed Critical 죤 에드워드 베리만
Publication of KR927003521A publication Critical patent/KR927003521A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/04—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
    • C07C259/06—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—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
    • C07D209/20—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 substituted additionally by nitrogen atoms, e.g. tryptophane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C07K5/06113—Asp- or Asn-amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Abstract

내용 없음

Description

펩티딜(peptidyl) 유도체
[도면의 간단한 설명]
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 식(I)의 화합물과 이의 염, 용매화합물 및 수화물.
    여기서 R은 -CONHOH, 카르복실(-CO2H) 또는 에스테르화 된 카르복실 그룹을 나타내고, R1은 선택적으로 치환되는 알킬, 알케닐, 알릴, 알알킬, 헤테로알알킬 또는 헤테로 알릴티오 그룹을 나타내며, R2는 선택적으로 치환되는 알킬, 알케닐, 사이클로알킬, 사이클로알킬알킬, 알릴, 알알킬, 알알콕시 또는 알킬티오그룹 또는 아미노(-NH2), 치환된 아미노, 카르복실(-CO2H) 또는 에스테르화 된 카르복실그룹을 나타내고, R3는 수소원자 또는 알킬그룹을 나타내며, R4는 수소원자 또는 알킬그룹을 나타내고, R5는 그룹-[Alk]nR6를 나타내며, 여기서 Alk는 하나 또는 그 이상의 -O- 또는 -S- 원자 또는 -N(R")- 그룹들[여기서 R7은 수소원자 또는 C1-6알킬그룹]에 의해 선택적으로 억제되는 알킬 또는 알케닐그룹이며, n은 0 또는 정수 1, 그리고 R6는 선택적으로 치환되는 사이클로알킬 또는 사이클로알케닐 그룹이며, X는 아미노(-NH2), 또는 치환된 아미노, 히드록실 또는 치환된 히드록실 그룹이다.
  2. 제l항에 있어서, R은 -CONHOH 또는 카르복실 (-CO2H) 그룹임을 특징으로 하는 화합물.
  3. 제1항 또는 재2항에 있어서, R1, R3및 R4는 각각 수소원자 임을 특징으로 하는 화합물.
  4. 제1-3항 중의 어느 한 항에 있어서, R2는 선택적으로 치환되는 알킬, 사이클로알킬, 알릴, 알알콕시 또는 알킬티오 그룹임을 특징으로 하는 화합물.
  5. 상술한 항 중의 어느 한 항에 있어서, R5는 AlkR6그룹(여기서 Alk는 C1-6알킬임)이고 R6는 사이클로알킬 또는 사이클로알케닐 그룹임을 특징으로 하는 화합물.
  6. 상술한 항 중의 어느 한 항에 있어서, X는 아미노 또는 치환된 아미노 그룹임을 특징으로 하는 화합물.
  7. 다음 구조식(Ia)의 화합물과 이의 염, 용매화합물 및 수화물.
    R은 여기서 -CONHOH, 카르복실(-CO2H) 또는 에스테르화 된 카르복실 그룹이고, R2는 선택적으로 치환 되는 알킬, 알케닐, 사이클로알킬, 사이클로알킬알킬, 알릴, 알알킬, 알알콕시 또는 알킬티오그룹 또는 아미노(-NH2), 치환된 아미노, 카르복실(-CH2H)또는 에스테르화 된 카르복실 그룹을 나타내여, R5는 -[Alk]nR6그룹을 나타내며, 여기서 Alk는 하나 또는 그 이상의 -O- 또는 -S- 또는 -N(R7)-그룹을 [여기서 R7은 수소원자, 또는 C1-6알킬그룹]에 의해 선택적으로 억제되는 알킬 또는 알케닐 그룹이며, n은 0 또는 정수 1, R6는 선택적으로 치환되는 사이클로알킬 또는 사이클로알케닐 그룹이고, X는 아미노 (-NH2) 또는 치환된 아미노, 히드록실 또는 치환된 히드록실 그룹이다.
  8. 제7항에 있어서, R은 -CONHOH 또는 -CO2H 그룹이고, R2는 선택적으로 치환되는 알킬, 알케닐, 사이클로알킬, 사이클로알킬알킬, 알릴, 알알콕시 또는 알알킬티오 그룹이며, R5는 -AlkR6그룹을 나타내며, 여기서 Alk는 C1-6알킬그룹이고, R6는 사이클로알킬 또는 사이클로알케닐 그룹이며, X는 아미노(NH2) 또는 치환된 아미노그룹임을 특징으로 하는 화합물과 이의 염, 용매화합물 및 수화물.
  9. 제8항에 있어서, R5는 사이클로헥실 C1-6알킬그룹임을 특징으로 하는 화합물.
  10. 제9항에 있어서, R5는 사이클로헥실메틸 그룹임을 특징으로 하는 화합물.
  11. 제9항 또는 제10항에 있어서, R2는 선택적으로 치환되는 페닐 C2-6알킬그룹임을 특징으로 하는 화합물.
  12. 제11항에 있어서, R2는 선택적으로 치환되는 페닐프로필 그룹임을 특징으로 하는 화합물.
  13. [4-(N-히드록시아미노)-2(R)-사이클로헥실메틸숙시닐]-L-β-사이클로헥실알라닌-N-(2-페닐에틸)아미드, [4-(N-히드록시아미노)-2R-이소부틸숙시닐-L-β-사이클로헥실알라닌-N-(2-페닐에틸)아미드, [4-(N-히드록시아미노)-2R-페닐프로필숙시닐]-L-β-사이클로헥실알라닌-N-(2-페닐에틸)아미드, [4-(N-히드록시아미노)-2R-페닐프로필숙시닐]-L-β-사이클로헥실알라닌-N-(2-아미노에틸)-N, N-디메틸아미노]아미드, [4-(N-히드록시아미노)-2R-페닐프로필숙시닐]-L-β-사이클로헥실알라닌-N-(2-(p-설폰아도드페닐)에틸]아미드, [4-(N-히드록시아미노)-2R-페닐프로필숙시닐]-L-β-사이클로헥실알라닌-N-(2-(p-설폰닐페닐)에틸]아미드, [4-(N-히드록시아미노)-2R-페닐프로필숙시닐]-L-β-사이클로헥실알라닌-N-(2-(2-아미노에틸)-피리딘]아미드, [4-(N-히드록시아미노)-2R-펜틸숙시닐]-L-β-사이클로헥실알라닌-N-(2-페닐에틸)아미드, [4-(N-히드록시아미노)-2R-이소아밀숙시닐]-L-β-사이클로헥실알라닌-N-(2-페닐에틸)아미드, [4-(N-히드록시아미노)-2R-페닐부틸숙시닐]-L-β-사이클로헥실알라닌-N-(2-페닐에틸)아미드, [4-(N-히드록시아미노)-2R-페닐프로필숙시닐]-L-β-사이클로헥실알라닌-N-(4-3-아미노프로필)-모르포린]아미드, [4-(N-히드록시아미노)-2R-페닐프로필숙시닐]-L-β-사이클로헥실알라닌-N-(2-페닐에틸)아미드, [4-(N-히드록시아미노)-2R-페닐프로필숙시닐]-L-β-사이클로헥실알라닌-N-(β-알라닌)아미드, [4-(N-히드록시아미노)-2R-이소부틸숙시닐]-L-β-사이클로헥실알라닌 아미드, [4-(N-히드록시아미노)-2R-(3-페닐프로필)숙시닐]-L-β-사이클로헥실알라닌 아미드, [4-(N-히드록시아미노-2R-(3-페닐부틸)숙시닐]-L-β-사이클로헥실알라닌 아미드, [4-(N-히드록시-2(R)-(3-페닐프로필)숙시닐]-L-β-사이클로헥실알라닌-(N-2-페닐에틸)아미드, [4-히드록시-2(R)-(3-페닐프로필)숙시닐]-L-β-사이클로헥실알라닌-β-알라닌메틸에스테르, [4-히드록시-2(R)-(3-페닐프로필)숙시닐]-L-β-사이클로헥실알라닌-β-알라닌, [4-히드록시-2(R)-(3-페닐프로필)숙시닐]-L-β-사이클로헥실알라닌-β-알라닌아미드, [4-히드록시-2(R)-이소부틸숙시닐]-L-β-사이클로헥실알라닌]-(N-2-페닐에틸)아미드, [4-히드록시-2(R)-이소아밀숙시닐]-L-β-사이클로헥실알라닌]-(N-2-페닐에틸)아미드, [4-히드록시-2(R)-[3(4-메틸페닐)프로필]숙시닐-L-β-사이클로헥실알라닌-N-(2-페닐에틸)아미드, [4-히드록시-2R-페닐프로필숙시닐]-L-β-사이클로헥실알라닌-N-(2-(O-벤질카르보닐)애틸]아미드, [4-히드록시-2R-페닐프로필숙시닐]-L-β-사이클로헥실알라닌-N-(2-(p-설폰아미도페실)에틸]아미드, [4-히드록시-2R-페닐프로필숙시닐]-L-β-사이클로헥실알라니 글라이신 메틸에스테르와 이의 염, 용매화합물 및 수화물.
  14. 제1-13항 중의 어느 한 항에 따르는 화합물과 약학적으로 받아들여 질수 있는 희석제, 담체 또는 부형제를 포함하는 약학적 조성물.
  15. 다음 (a), (b), (c)를 포함하는, 제1항에 따르는 구조식(I)의 화합물의 제조방법.
    (a)구조식(II)의 산 또는 그에 따른 활성의 또는 보호된 유도체들을 구조식(II)의 아민과 결합시키거나,
    또는,
    또는 구조식(II)의 산을 보호그룹을 제거한 후 그에 따른 보호된 유도체와 결합하고, 또는
    (b)R이 -CCO2H 그룹인 화학(I)의 화합물을 만들기 위해 구조식(IX)의 화합물에서 카르복시기를 이탈시키며, 또는,
    (c) 구조식(I)의 화합물을 상호전환 한다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임,
KR1019920701788A 1990-12-03 1991-12-03 펩티딜(peptidyl) 유도체 KR927003521A (ko)

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Application Number Priority Date Filing Date Title
GB909026251A GB9026251D0 (en) 1990-12-03 1990-12-03 Netalloproteinase inhibitors
GB9026251.0 1990-12-03
GB9110339.0 1991-05-13
GB9110338.2 1991-05-13
GB919110339A GB9110339D0 (en) 1991-05-13 1991-05-13 Metalloproteinase inhibitors
GB919110338A GB9110338D0 (en) 1991-05-13 1991-05-13 Metalloproteinase inhibitors
GB919112901A GB9112901D0 (en) 1991-06-14 1991-06-14 Metalloproteinase inhibitors
GB9112888.4 1991-06-14
GB9112901.5 1991-06-14
GB919112888A GB9112888D0 (en) 1991-06-14 1991-06-14 Metalloproteinase inhibitors
GB919115038A GB9115038D0 (en) 1991-07-11 1991-07-11 Metalloproteinase inhibitors
GB9115038.3 1991-07-11
GB9115039.1 1991-07-11
GB919115039A GB9115039D0 (en) 1991-07-11 1991-07-11 Metalloproteinase inhibitors
GB9115916.0 1991-07-23
GB919115916A GB9115916D0 (en) 1991-07-23 1991-07-23 Metalloproteinase inhibitors
PCT/GB1991/002143 WO1992009565A1 (en) 1990-12-03 1991-12-03 Peptidyl derivatives

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GB9211715D0 (en) 1992-08-26
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EP0489577A1 (en) 1992-06-10
NO922967D0 (no) 1992-07-28
ATE120182T1 (de) 1995-04-15
JPH05503719A (ja) 1993-06-17
GB9211714D0 (en) 1992-08-26
FI923495A0 (fi) 1992-08-03
NO922968L (no) 1992-09-24
HUT61973A (en) 1993-03-29
DE69108529D1 (de) 1995-05-04
ES2069833T3 (es) 1995-05-16
FI923495A (fi) 1992-08-03
HUT62263A (en) 1993-04-28
GR3015567T3 (en) 1995-06-30
KR927003520A (ko) 1992-12-18
WO1992009564A1 (en) 1992-06-11
AU9023391A (en) 1992-06-25
HU9202497D0 (en) 1992-10-28
NO922967L (no) 1992-09-24
DE69108363D1 (de) 1995-04-27
FI923494A (fi) 1992-08-03
DK0489579T3 (da) 1995-06-12
EP0489579B1 (en) 1995-03-29
US5300501A (en) 1994-04-05
AU652793B2 (en) 1994-09-08
EP0489579A1 (en) 1992-06-10
DE69108363T2 (de) 1995-08-31
GB2255340A (en) 1992-11-04
DE69108529T2 (de) 1995-11-30
AU652596B2 (en) 1994-09-01
EP0489577B1 (en) 1995-03-22
FI923494A0 (fi) 1992-08-03
GB2255339B (en) 1994-10-05
ATE120451T1 (de) 1995-04-15
GB2255339A (en) 1992-11-04
CA2073513A1 (en) 1992-06-04
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JPH05503720A (ja) 1993-06-17
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