KR890008155A - 신규인 유도체, 그 제조방법 및 의약에서의 사용 - Google Patents

신규인 유도체, 그 제조방법 및 의약에서의 사용 Download PDF

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KR890008155A
KR890008155A KR1019880014928A KR880014928A KR890008155A KR 890008155 A KR890008155 A KR 890008155A KR 1019880014928 A KR1019880014928 A KR 1019880014928A KR 880014928 A KR880014928 A KR 880014928A KR 890008155 A KR890008155 A KR 890008155A
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South Korea
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compound
formula
hydrogen
alkyl
hydrate
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KR1019880014928A
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제임즈 헌터 데이빗
에드워드 마아크웰 로저
윌리엄 워드 로버트
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원본미기재
비이참 그루우프 피일엘시이
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Publication of KR890008155A publication Critical patent/KR890008155A/ko

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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006—Esters of acyclic acids which can have further substituents on alkyl
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Steroid Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

내용 없음

Description

신규인 유도체, 그 제조방법 및 의약에서의 사용
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (16)

  1. 하기 일반식(I)의 화합물, 또는 그 염, 용매화합물 또는 수화물 :
    상기식에서 R1은 수소 또는 히드록시이고 ; R2는 수소 또는 알킬이고 ; R3는 C3-6알킬이고 ; R4는 수소, 알킬, Z가 임의로 치환된 페닐 또는 헤테로 아릴인 -CH2-Z이거나, R4는 R8가 수소, 알킬 또는 -CH2-Ph(여기서 Ph는 임의로 치환된 페닐임)이고 R9가 수소 또는 알킬인이고 ; R5는 수소 또는 알킬이다.
  2. 제1항에 있어서, R1이 히드록시인 화합물.
  3. 제1항 또는 제2항에 있어서, R2가 수소, 메틸, 에틸 또는 이소프로필인 화합물.
  4. 제1항 내지 제3항중 어느 한 항에 있어서, R3이 n-부틸, 이소-부틸 또는 이차-부틸인 화합물.
  5. 제1항 내지 제4항중 어느 한 항에 있어서, R4가 벤질, 4-히드록시벤질, 4-메톡시벤질 또는 3-인돌릴메틸인 화합물.
  6. 제1항 내지 제5항중 어느 한 항에 있어서, R5가 메틸 또는 에틸인 화합물.
  7. 제1항 내지 제6항중 어느 한 항에 있어서, R1이 히드록시이고 ; R2가 메틸 또는 에틸이고 ; R3가 이소-부틸이고 ; R4가 4-메톡시벤질 또는 3-인돌릴메틸이고 ; R5가 메틸인 화합물.
  8. 제1항 내지 제7항중 어느 한 항에 있어서, 일반식(I)에서 별표로 표시된 키랄 중심이 S-배치를 갖는 화합물.
  9. 하기 화합물들로부터 선택된 화합물 : N-[N-(1-포스포노에틸-로이실]-N,0-디메틸-L-티로신아미드 ; N-[N-(포스포노메틸)-로이실-N,O-디메틸-L-티로신아미드 ;N-[N-(1-포스포노프로필)-로이실]-N,O-디메틸-L-티로신아미드 ; N-[N-(1-포스포노-2-메틸프로필)-로이실]-N,O-디메틸-L-티로신아미드 ; 및 N-[N-(1-포스포노에틸)-로이실]-N-메틸-L-트립토판아미드.
  10. 제1항 내지 제9항중 어느 한 항에 따른 화합물의 제약학적으로 허용가능한 염, 용매 화합물 또는 수화물.
  11. 하기 일반식(II)의 화합물로부터 R10기를 분리시키고 필요하다면 R1'를 R1으로 전환시키는 것을 포함하는, 제1항에서 정의한 일반식(I)의 화합물의 제조방법 :
    상기식에서 R10은 알킬 또는 임의로 치환된 벤질이고 R1'은 R1이거나 R1으로 전환될 수 있는 기이고 R2, R3, R4및 R5는 일반식(I)에서 정의된 바와 같다.
  12. 제11항에서 정의한 일반식(II)의 화합물.
  13. 제1항에서 정의한 일반식(I)의 화합물, 또는 제약학적으로 허용가능한 그 염, 용매화합물 또는 수화물 및 제약학적으로 허용가능한 담체를 포함하는 제약학적 조성물.
  14. 활성 치료 물질로서 사용하기 위한, 제1항에서 정의한 일반식(I)의 화합물, 또는 제약학적으로 허용가능한 그 염, 용매화합물 또는 수화물.
  15. 포유동물의 콜라겐 분해 상태의 치료시 사용하기 위한, 제1항에서 정의한 일반식(I)의 화합물, 또는 제약학적으로 허용가능한 그 염, 용매 화합물 또는 수화물.
  16. 포유동물의 콜라겐 분해 상태의 치료를 위한 의약품의 제조시, 제1항에서 정의한 일반식(I)의 화합물, 또는 제약학적으로 허용가능한 그 염, 용매화합물 또는 수화물의 사용.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880014928A 1987-11-14 1988-11-12 신규인 유도체, 그 제조방법 및 의약에서의 사용 KR890008155A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB878726714A GB8726714D0 (en) 1987-11-14 1987-11-14 Compounds
GB8726714 1987-11-14

Publications (1)

Publication Number Publication Date
KR890008155A true KR890008155A (ko) 1989-07-10

Family

ID=10626975

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Application Number Title Priority Date Filing Date
KR1019880014928A KR890008155A (ko) 1987-11-14 1988-11-12 신규인 유도체, 그 제조방법 및 의약에서의 사용

Country Status (15)

Country Link
US (1) US4935404A (ko)
EP (1) EP0320118B1 (ko)
JP (1) JPH01160992A (ko)
KR (1) KR890008155A (ko)
AT (1) ATE90107T1 (ko)
AU (1) AU609900B2 (ko)
CA (1) CA1322076C (ko)
DE (1) DE3881489T2 (ko)
DK (1) DK633088A (ko)
ES (1) ES2054826T3 (ko)
GB (1) GB8726714D0 (ko)
IE (1) IE883391L (ko)
NZ (1) NZ226930A (ko)
PT (1) PT88992B (ko)
ZA (1) ZA888448B (ko)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0401963A1 (en) * 1989-04-13 1990-12-12 Beecham Group p.l.c. Phosphonopeptides with collagenase inhibiting activity
US5212163A (en) * 1989-04-13 1993-05-18 Beecham Group P.L.C. Compounds
GB8921326D0 (en) * 1989-09-21 1989-11-08 Beecham Group Plc Novel treatment
FR2654430B1 (fr) * 1989-11-15 1995-01-06 Commissariat Energie Atomique Nouveaux derives de peptides, utilisables comme inhibiteurs des collagenases bacteriennes.
GB9008065D0 (en) * 1990-04-10 1990-06-06 Beecham Group Plc Novel compounds
GB9008078D0 (en) * 1990-04-10 1990-06-06 Beecham Group Plc Novel compounds
US5294632A (en) * 1991-05-01 1994-03-15 Ciba-Geigy Corporation Phosphono/biaryl substituted dipetide derivatives
US5155100A (en) * 1991-05-01 1992-10-13 Ciba-Geigy Corporation Phosphono/biaryl substituted dipeptide derivatives
EP0520573A1 (en) * 1991-06-27 1992-12-30 Glaxo Inc. Cyclic imide derivatives
US5250522A (en) * 1992-10-09 1993-10-05 Ciba-Geigy Corporation Phosphono/biaryl substituted amino acid derivatives
GB9122859D0 (en) * 1991-10-28 1991-12-11 Smithkline Beecham Plc Novel compounds
JPH05148277A (ja) * 1991-11-05 1993-06-15 Banyu Pharmaceut Co Ltd アミノホスホン酸誘導体
US5504070A (en) * 1991-12-05 1996-04-02 Berlex Laboratories, Inc. Inhibitors of the conversion of big endothelin to endothelin
US5270365A (en) * 1991-12-17 1993-12-14 Merck & Co., Inc. Prevention and treatment of periodontal disease with alendronate
CA2126687A1 (en) * 1992-01-15 1993-07-22 Charles G. Caldwell Substituted phosphinic acid-containing peptidyl derivatives as antidegenerative agents
EP0639982A1 (en) * 1992-05-01 1995-03-01 British Biotech Pharmaceuticals Limited Use of mmp inhibitors
US5326760A (en) * 1992-06-29 1994-07-05 Glaxo, Inc. Aminobutanoic acid compounds having metalloprotease inhibiting properties
WO1994007481A1 (en) * 1992-10-02 1994-04-14 Merck & Co., Inc. N-(mercaptoacyl)peptidyl derivatives as antidegenerative agents
US6090785A (en) * 1992-10-15 2000-07-18 Merck & Co., Inc. Substituted N-carboxyalkylpeptidyl derivatives as antidegenerative agents
US5672583A (en) * 1992-11-25 1997-09-30 Merck & Co., Inc. Carboxy-peptidyl derivatives as antidegenerative active agents
EP0618224A1 (en) * 1993-03-30 1994-10-05 Merrell Dow Pharmaceuticals Inc. Phosphonomethyldipeptides
US5608078A (en) * 1993-03-30 1997-03-04 Merrell Pharmaceuticals Inc. Phosphonomethyldipeptides and process for preparation thereof
JPH08511509A (ja) * 1993-04-07 1996-12-03 グリコメド・インコーポレイテッド 合成マトリックスメタロプロテアーゼ阻害剤およびその用途
US5840698A (en) * 1994-10-27 1998-11-24 Affymax Technologies N.V. Inhibitors of collagenase-1 and stormelysin-I metalloproteases, pharmaceutical compositions comprising same and methods of their use
US5831004A (en) 1994-10-27 1998-11-03 Affymax Technologies N.V. Inhibitors of metalloproteases, pharmaceutical compositions comprising same and methods of their use
US6953788B1 (en) 1996-09-19 2005-10-11 Aventis Pharmaceuticals Inc. 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase
WO1998054123A1 (en) * 1997-05-30 1998-12-03 Warner-Lambert Company Substituted peptidylamine calcium channel blockers
EP0922702A1 (de) * 1997-12-13 1999-06-16 Roche Diagnostics GmbH Neue Azulenderivate und diese enthaltende Arzneimittel
PE20010659A1 (es) 1999-10-01 2001-06-20 Hoffmann La Roche Derivados de las pirimidin-2,4,6-trionas como inhibidores de metaloproteasas
US6716845B2 (en) 2001-03-30 2004-04-06 Hoffmann-La Roche Inc. Barbituric acid derivatives
US7420000B2 (en) * 2003-09-10 2008-09-02 University Of Southern California Amino phosphonate and amino bis-phosphonate derivatives

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US3950402A (en) * 1972-05-31 1976-04-13 Monsanto Company Process for producing N-phosphonomethyl glycine
IL48835A (en) * 1975-01-27 1979-05-31 Sparamedica Ag Amino acyl and peptidyl derivatives of phophonic acids, their preparation and pharmaceutical compositions containingthem
EP0002039A1 (en) * 1977-11-19 1979-05-30 Ciba-Geigy Ag Phosphonous acid derivatives, processes for their preparation and their use in combating microorganisms
US4331591A (en) * 1978-10-05 1982-05-25 Ciba-Geigy Corporation Chemical process for the production of α-aminophosphonic acids and peptide derivatives
US4389349A (en) * 1982-01-25 1983-06-21 Cho Hung H Process for preparing of N-phosphenomethyl glycine
US4661298A (en) * 1983-08-31 1987-04-28 Stauffer Chemical Company Process for the formation of phosphonoalkylated amino acids
US4804500A (en) * 1985-04-22 1989-02-14 Monsanto Company Amine dealkylation process

Also Published As

Publication number Publication date
EP0320118A3 (en) 1990-07-04
EP0320118B1 (en) 1993-06-02
JPH01160992A (ja) 1989-06-23
EP0320118A2 (en) 1989-06-14
GB8726714D0 (en) 1987-12-16
DK633088D0 (da) 1988-11-11
ATE90107T1 (de) 1993-06-15
DE3881489D1 (de) 1993-07-08
NZ226930A (en) 1991-07-26
IE883391L (en) 1989-05-14
US4935404A (en) 1990-06-19
PT88992A (pt) 1988-12-01
ES2054826T3 (es) 1994-08-16
AU609900B2 (en) 1991-05-09
PT88992B (pt) 1993-02-26
ZA888448B (en) 1989-10-25
DE3881489T2 (de) 1993-09-16
AU2507088A (en) 1989-05-25
DK633088A (da) 1989-05-15
CA1322076C (en) 1993-09-07

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