KR930702269A - 포스포리파제 a2저해 물질 - Google Patents

포스포리파제 a2저해 물질

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Publication number
KR930702269A
KR930702269A KR1019930700634A KR930700634A KR930702269A KR 930702269 A KR930702269 A KR 930702269A KR 1019930700634 A KR1019930700634 A KR 1019930700634A KR 930700634 A KR930700634 A KR 930700634A KR 930702269 A KR930702269 A KR 930702269A
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KR
South Korea
Prior art keywords
single bond
independently
hydrogen
halogen
hydroxy
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KR1019930700634A
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English (en)
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KR100233343B1 (ko
Inventor
미쓰아끼 오따니
시게루 마쓰다니
다다시 요시다
가즈시게 다나까
야스히꼬 후지이
가즈히로 시라하세
Original Assignee
시오노 요시히꼬
시오노기 세이야꾸 가부시끼가이샤
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Publication of KR930702269A publication Critical patent/KR930702269A/ko
Application granted granted Critical
Publication of KR100233343B1 publication Critical patent/KR100233343B1/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • 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
    • 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
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C229/36—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/62—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C07C69/84—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring
    • C07C69/90—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with esterified hydroxyl and carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C07C69/84—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring
    • C07C69/92—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with etherified hydroxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/34—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D309/36—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • C07D309/38—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms one oxygen atom in position 2 or 4, e.g. pyrones

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

본 발명은 포스포리파제 A2억제 활성을 나타내는 하기 일반식의 신규 틸로신 유도체 또는 그의 염에 관한 것이다.
상기식에서 R1,R2,R3,R4,R5,R6,R7및 R8은 독립적으로 수소, 저급 알킬, 저급 알콕시, 하이드록시 또는 할로겐이고: E1및 E2는 독립적으로 수소 또는 에스테르 잔기이고 m및 n은 독립적으로 0내지 4의 정수이고; -Y-는 하기 라디칼들로 이루어진 그룹중에서 선택된 2가 그룹이다.

Description

포스포리파제 A2저해 물질
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 하기 일반식의 틸로신 유도체 또는 그의 염.
  3. 상기식에서 R1,R2,R3,R4,R5,R6,R7및 R8은 독립적으로 수소, 저급 알킬, 저급 알콕시, 하이드록시 또는 할로겐이고: E1및 E2는 독립적으로 수소 또는 에스테르 잔기이고 m및 n은 독립적으로 0내지 4의 정수이고; -Y-는 하기 라디칼들로 이루어진 그룹중에서 선택된 2가 그룹이고;
  6. X는 단일결합, CH2,O,S,SO 또는 SO2이고; R9및 R10은 독립적으로 단일결합, 수소, 저급알킬, 저급알콕시, 하이드록시 또는 할로겐이거나, 또는 R9및 R10이 함께 결합되어 메틸렌, 에테르, 설파이드, 설피닐 또는 설폰을 형성할 수있고; R9및 R10는 독립적으로 단일결합, 수소, 저급알킬, 저급알콕시, 하이드록시 또는 할로겐이거나, 또는 R9및 R10가 함께 결합되어 메틸렌, 에테르, 설파이드, 설피닐 또는 설폰을 형성할 수 있고; R11은 수소 또는 저급 알킬이고; R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30및 R31은 독립적으로 단일결합, 수소 저급알킬, 저급알콕시, 하이드록시 또는 할로겐이지만, 단, R9, R15, R16, R17및 R8중의 하나, R10, R12, R13및 R14중의 하나, R9', R23, R24, R25및 R26중의 하나, R10', R19, R20, R21및 R22중의 하나, R27, R28, R29, R30및 R31중의 하나는 단일 결합이며; R32, R33, R34, R35및 R36은 독립적으로 수소, 저급알킬, 저급알콕시, 하이드록시, 할로겐 또는 Z이고;R37은 수소 또는 아미노-보호 그룹이고; Z는 단일결합 또는 일반식의 2가 그룹이고; R36, R39, R40, R41및 R42는 독립적으로 단일결합, 수소, 저급알킬, 저급알콕시 하이드록시 또는 할로겐이지만, 단, R32, R33, R34, R35및 R36중의 하나는 항상 Z이고; Z가 단일결합이 아닌 경우, R38, R39, R40, R41및 R42중의 하나가 단일결합이거나, 또는 R32, R33, R34, R35및 R36중의 2개이상이 Z인 경우, Z, R39, R40, R41및 R42중의 단 하나만이 단일 결합이다.
  7. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930700634A 1991-07-03 1992-06-24 포스포리파제 a2 저해물질 KR100233343B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP91-162847 1991-07-03
JP16284791 1991-07-03
PCT/JP1992/000802 WO1993001157A1 (en) 1991-07-03 1992-06-24 Phospholipase a2 inhibitor

Publications (2)

Publication Number Publication Date
KR930702269A true KR930702269A (ko) 1993-09-08
KR100233343B1 KR100233343B1 (ko) 1999-12-01

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ID=15762376

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Application Number Title Priority Date Filing Date
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EP (1) EP0547231B1 (ko)
JP (1) JP3403404B2 (ko)
KR (1) KR100233343B1 (ko)
AT (1) ATE141909T1 (ko)
CA (1) CA2090434A1 (ko)
DE (1) DE69213184T2 (ko)
DK (1) DK0547231T3 (ko)
ES (1) ES2093838T3 (ko)
GR (1) GR3020898T3 (ko)
WO (1) WO1993001157A1 (ko)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2100640A1 (en) * 1992-07-23 1994-01-24 Shigeru Matsutani Substitute benzoate derivatives
US5534533A (en) * 1993-10-01 1996-07-09 Shionogi & Co., Ltd. Carboxylate derivatives exhibiting phospholipase A2 inhibitory activity
US5612053A (en) * 1995-04-07 1997-03-18 Edward Mendell Co., Inc. Controlled release insufflation carrier for medicaments
JP7065951B2 (ja) 2017-09-22 2022-05-12 ジュビラント エピパッド エルエルシー Ｐａｄ阻害剤としての複素環式化合物
CA3076476A1 (en) 2017-10-18 2019-04-25 Jubilant Epipad LLC Imidazo-pyridine compounds as pad inhibitors
CA3080677A1 (en) 2017-11-06 2019-05-09 Jubilant Prodel LLC Pyrimidine derivatives as inhibitors of pd1/pd-l1 activation
MX2020005363A (es) 2017-11-24 2020-10-01 Jubilant Episcribe Llc Compuestos heterociclicos como inhibidores de prmt5.
MX2020009517A (es) 2018-03-13 2021-01-20 Jubilant Prodel LLC Compuestos biciclicos como inhibidores de la interaccion/activacio n de pdl/pd-l1.

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1271779A (en) * 1971-01-14 1972-04-26 Celanese Corp Purification of aromatic carboxylic acids
DE2205932A1 (de) * 1972-02-09 1973-08-16 Hoechst Ag Verfahren zur herstellung von methylestern mehrkerniger, aromatischer carbonsaeuren
JP2842613B2 (ja) * 1989-04-28 1999-01-06 塩野義製薬株式会社 フォスフォリパーゼａ▲下２▼阻害物質
JPH04117346A (ja) * 1990-09-04 1992-04-17 Shionogi & Co Ltd ホスホリパーゼａ↓２阻害物質
JPH04159251A (ja) * 1990-10-22 1992-06-02 Shionogi & Co Ltd ホスホリパーゼａ↓２阻害物質

Also Published As

Publication number Publication date
DE69213184D1 (en) 1996-10-02
CA2090434A1 (en) 1993-01-04
DE69213184T2 (de) 1997-01-09
EP0547231B1 (en) 1996-08-28
KR100233343B1 (ko) 1999-12-01
JP3403404B2 (ja) 2003-05-06
ATE141909T1 (de) 1996-09-15
WO1993001157A1 (en) 1993-01-21
ES2093838T3 (es) 1997-01-01
EP0547231A4 (en) 1994-06-08
DK0547231T3 (da) 1996-09-16
GR3020898T3 (en) 1996-11-30
EP0547231A1 (en) 1993-06-23

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