KR927003520A - 펩티딜(peptidyl) 유도체 - Google Patents

펩티딜(peptidyl) 유도체 Download PDF

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Publication number
KR927003520A
KR927003520A KR1019920701787A KR920701787A KR927003520A KR 927003520 A KR927003520 A KR 927003520A KR 1019920701787 A KR1019920701787 A KR 1019920701787A KR 920701787 A KR920701787 A KR 920701787A KR 927003520 A KR927003520 A KR 927003520A
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KR
South Korea
Prior art keywords
group
alkyl
amino
compound
optionally substituted
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KR1019920701787A
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English (en)
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죤 로버트 포터
죤 리차드 멀피
토마스 앤드류 밀리칸
니겔 로버트 아놀드 빌레이
Original Assignee
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 GB919112888A external-priority patent/GB9112888D0/en
Priority claimed from GB919112901A external-priority patent/GB9112901D0/en
Priority claimed from GB919115039A external-priority patent/GB9115039D0/en
Priority claimed from GB919115038A external-priority patent/GB9115038D0/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 KR927003520A publication Critical patent/KR927003520A/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 (8)

  1. 식(I)의 화합물과 이의 염, 용매화합물 및 수화물,
    여기서 R은 -CONHOH, 카르복실(-CO2H) 또는 에스테르화 된 카르복실 그룹이고, R1은 선택적으로 치환되는 알킬, 알케닐, 알릴, 알알킬, 헤테로 알알킬 그룹이며, R2는 선택적으로 치환되는 페닐 에틸, 페닐프로필, 또는 페닐 부틸 그룹이고, R3는 수소원자 또는 알킬 그룹이며, R4는 수소원자 또는 알킬 그룹이고, R5는 하나 또는 그 이상의 -O- 또는 -S- 원자 또는 -N(R7)- 그룹들[여기서 R7은 수소원자 또는 C1-6알킬그룹]에 의해 선택적으로 치환되는 알킬 또는 알케닐 그룹이며, X는 아미노(-NH2), 또는 치환된 아미노, 히드록실 또는 치환된 히드록실 그룹이다.
  2. 제1항에 있어서, R은 -CONHOH 또는 카르복실 (-CO2H) 그룹임을 특징으로 하는 화합물.
  3. 제1항 또는 제2항에 있어서, R1, R3와 R4가 각각 수소원자 임을 특징으로 하는 화합물.
  4. 제1-3항 중의 어느 한 항에 있어서, R2는 선택적으로 치환된는 페닐프로필 그룹임을 특징으로 하는 화합물.
  5. 상술된 항 중의 어느 한 항에 있어서, X는 아미노 또는 치환된 아미노 그룹임을 특징으로 하는 화합물.
  6. 식(Ia)의 화합물과 이의 염, 용매화합물 및 수화물.
    여기서 R은 -CONHOH, 카르복실(-CO2H) 또는 에스테르화 된 카르복실 그룹이고, R2는 선택적으로 치환되는 페닐프로필 그룹이며, R5는 하나 또는 그 이상의 -O- 또는 -S- 원자들 또는 -N(R7)-그룹 [여기서 R7은 수소원자 또는 C1-6알킬그룹]에 의해 선택적으로 억제되는, 선택적으로 치환되는 알킬 또는 알케닐 그룹이고, X는 아미노(-NH2) 또는 치환된 아미노, 히드록실 또는 치환된 히드록실 그룹이다.
  7. 제1 내지 6항 중의 어느 한 항에 따르는 화합물과 약학적으로 받아들여질 수 있는 희석제, 담체나 또는 부형제를 포함하는 약학적 조성물.
  8. 하기 (a), (b), (c)를 포함하는, 1항에 설명된 식(I)의 화합물의 제조방법, (a)식(II) 산 또는 이의 활성인 그리고/또는 보호된 유도체들은 식(III) 아민 또는 이의 보호된 유도체와 결합시키고 보호그룹을 제거하거나,
    또는 (b)식(IX)의 화합물을 탈카르복실화시켜 R이 -CO2H기인 식(I)의 화합물을 만들고/또는 (c)식(I)의 화합물을 상호전이(interconverting)시킨다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019920701787A 1990-12-03 1991-12-03 펩티딜(peptidyl) 유도체 KR927003520A (ko)

Applications Claiming Priority (17)

Application Number Priority Date Filing Date Title
GB9026251.0 1990-12-03
GB909026251A GB9026251D0 (en) 1990-12-03 1990-12-03 Netalloproteinase inhibitors
GB919110339A GB9110339D0 (en) 1991-05-13 1991-05-13 Metalloproteinase inhibitors
GB9110338.2 1991-05-13
GB919110338A GB9110338D0 (en) 1991-05-13 1991-05-13 Metalloproteinase inhibitors
GB9110339.0 1991-05-13
GB919112888A GB9112888D0 (en) 1991-06-14 1991-06-14 Metalloproteinase inhibitors
GB919112901A GB9112901D0 (en) 1991-06-14 1991-06-14 Metalloproteinase inhibitors
GB9112901.5 1991-06-14
GB9112888.4 1991-06-14
GB9115039.1 1991-07-11
GB9115038.3 1991-07-11
GB919115039A GB9115039D0 (en) 1991-07-11 1991-07-11 Metalloproteinase inhibitors
GB919115038A GB9115038D0 (en) 1991-07-11 1991-07-11 Metalloproteinase inhibitors
GB919115916A GB9115916D0 (en) 1991-07-23 1991-07-23 Metalloproteinase inhibitors
GB9115916.0 1991-07-23
PCT/GB1991/002142 WO1992009564A1 (en) 1990-12-03 1991-12-03 Peptidyl derivatives

Publications (1)

Publication Number Publication Date
KR927003520A true KR927003520A (ko) 1992-12-18

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
KR1019920701788A KR927003521A (ko) 1990-12-03 1991-12-03 펩티딜(peptidyl) 유도체
KR1019920701787A KR927003520A (ko) 1990-12-03 1991-12-03 펩티딜(peptidyl) 유도체

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Application Number Title Priority Date Filing Date
KR1019920701788A KR927003521A (ko) 1990-12-03 1991-12-03 펩티딜(peptidyl) 유도체

Country Status (16)

Country Link
US (1) US5300501A (ko)
EP (2) EP0489579B1 (ko)
JP (2) JPH05503719A (ko)
KR (2) KR927003521A (ko)
AT (2) ATE120182T1 (ko)
AU (2) AU652793B2 (ko)
CA (2) CA2073513A1 (ko)
DE (2) DE69108363T2 (ko)
DK (1) DK0489579T3 (ko)
ES (1) ES2069833T3 (ko)
FI (2) FI923494A0 (ko)
GB (2) GB2255339B (ko)
GR (1) GR3015567T3 (ko)
HU (3) HU9202497D0 (ko)
NO (2) NO922967L (ko)
WO (2) WO1992009564A1 (ko)

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CA2073513A1 (en) 1992-06-04
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EP0489577B1 (en) 1995-03-22
DE69108363D1 (de) 1995-04-27
EP0489577A1 (en) 1992-06-10
JPH05503719A (ja) 1993-06-17
ES2069833T3 (es) 1995-05-16
FI923495A (fi) 1992-08-03
HUT61973A (en) 1993-03-29
WO1992009565A1 (en) 1992-06-11
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HUT62263A (en) 1993-04-28
GB2255340A (en) 1992-11-04
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NO922967L (no) 1992-09-24
FI923495A0 (fi) 1992-08-03
AU9017391A (en) 1992-06-25
US5300501A (en) 1994-04-05
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AU9023391A (en) 1992-06-25
NO922967D0 (no) 1992-07-28
DE69108529D1 (de) 1995-05-04
GR3015567T3 (en) 1995-06-30
KR927003521A (ko) 1992-12-18
GB2255340B (en) 1994-09-28
AU652596B2 (en) 1994-09-01
NO922968L (no) 1992-09-24
HU9202498D0 (en) 1992-10-28
ATE120182T1 (de) 1995-04-15
FI923494A0 (fi) 1992-08-03
EP0489579B1 (en) 1995-03-29
CA2073510A1 (en) 1992-06-04
ATE120451T1 (de) 1995-04-15
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NO922968D0 (no) 1992-07-28
DE69108363T2 (de) 1995-08-31
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GB2255339B (en) 1994-10-05

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