KR900001675A - 기관지확장 작용을 갖는 화합물 - Google Patents

기관지확장 작용을 갖는 화합물 Download PDF

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KR900001675A
KR900001675A KR1019890009472A KR890009472A KR900001675A KR 900001675 A KR900001675 A KR 900001675A KR 1019890009472 A KR1019890009472 A KR 1019890009472A KR 890009472 A KR890009472 A KR 890009472A KR 900001675 A KR900001675 A KR 900001675A
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alkyl
compound
pharmaceutically acceptable
halogen
independently
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KR1019890009472A
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토마스 로간 로버트
레드패쓰 제임스
맥가리 죠지
깁슨 로이 로버트
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에이.쥐.제이.베르메렌, 에프.쥐.엠.헤르만스
악조 엔.브이.
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Publication of KR900001675A publication Critical patent/KR900001675A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/58—Radicals substituted by nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/15—Oximes (>C=N—O—); Hydrazines (>N—N<); Hydrazones (>N—N=) ; Imines (C—N=C)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • C07C259/12—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 with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines
    • C07C259/16—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 with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxamidine groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/81—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans 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 carbon atoms of the hetero ring
    • C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D307/85—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D333/70—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Furan Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

내용 없음

Description

기관지확장 작용을 갖는 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기식(I)로서 표시되는 화합물 및 약학적으로 허용되는 그의 염의 기관지확장 작용을 갖는 약제의 제조에 있어서의 용도.
    상기식에서, R1,R2,R3및 R4는 각각 독립적으로 H,C1-4알킬, 할로겐으로 치환된 C1-4알킬, OH, C1-4알콕시, 할로겐으로 치환된 C1-4알콕시, NO2,CN,할로겐, 비치환된 또는 C1-4알킬로 치환된 아미노기이거나, 또는 R1,R2,R3및 R4중 2개의 인접한 기들의 함께 메틸렌 디옥시를 형성하고; X는 S,O또는 (CH2)M(m=1또는 2)이며; R5는H 또는 C1-4알킬이고; R6는 H,NH2또는 C1-4알킬이며; R7는 H,C1-4알킬 또는 OR8로서 R8은 H,C1-4알킬 또는 C1-4아실이다.
  2. 제1 항에 있어서, R1,R2,R3및 R4중 적어도 2개가 독립적으로 OH,C1-4알콕시이거나, 또는 함께 메틸렌 디옥시기를 형성하고, 나머지 기들중 1 개 또는 2개는 독립적으로 H, NO2아미노,,C1-4알킬로 치환된 아미노 또는 할로겐이며, R5가 H 또는 CH3이고, R6는 H,NH2또는 CH3이며, R7는 OH인 화합물 및 약학적으로 허용되는 이들의 염의, 기관지확장 작용을 갖는 약제의 제조에 있어서의 용도.
  3. 제 1 항에 있어서, R1,R2,R3및 R4중 적어도 2개가 독립적으로 OH,OCH3또는 OC2H5이고, 나머지 기들중 1개 또는 2개는 독립적으로 H,NO2,F 또는 C1이며, X는 S,0 또는 (CH2)2이고, R5는 H이며, R6은 H 또는 NH2이고 및 R7이 OH인 화합물 또는 약학적으로 허용되는 이들의 염의, 기관지확장 작용을 갖는 약제의 제조에 있어서의 용도.
  4. 제 1 항에 있어서, R2와 R3가 OCH3이고, R5과 R4가 H,F 또는 C1이며, X는 S,0 또는 (CH2)2이고, R5는 H이며, R6은 NH2이고 및 R7이 OH인 화합물 또는 약학적으로 허용되는 이들의 염의, 기관지확장 작용을 갖는 약제의 제조에 있어서의 용도.
  5. 제 4 항에 있어서, R1과 R4가수소인 화합물의 용도.
  6. 하기식으로 표시되는 화합물.
    상기식에서, 옥심기는 자체의 E-이성질체로부터 완전히 유리된 기하학적 Z-이성질체로 구성되고, R1,R2,R3,R4,R5,R8및 X는 제 1 항에서 정의한 바와같으며, R6은 H또는 C1-4알킬이다.
  7. 하기식으로 표시되는 화합물.
    상기식에서, 옥시기는 자체의 Z-이성질체로부터 완전히 유리된 기하학적 E-이성질체로 구성되고,R1,R2,R3,R4,R5,R8및 X는 제 1 항에서 정의한 바와같으며, R6은 H또는 C1-4알킬로서, 단 R6가 C2-4알킬인 경우 R1-R5및 R8기들중 적어도 1개는 H가 아니다.
  8. 제 6 항 또는 제 7 항에 있어서,R1,R2,R3,R4,R5및R8이 H이고,R2와 R3,가 OCH3이며, 및 X가 S인 화합물.
  9. ,R1,R2,R3및 R4가 할로겐으로 치환된 C1-4알콕시이고,R6가NH2이며, 및 R5,R7,R과 X는 제 1 항에서 정의한 바와 같은 식(I)의 화합물 및 약학적으로 허용되는 그의 염.
  10. 활성성분으로서의 제 6 항 내지 제10항중 어느 한 항에서 정의한 1가지 이상의 화합물과 약학적으로 허용되는 담체를 함유하는 약학제제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890009472A 1988-07-05 1989-07-04 기관지확장 작용을 갖는 화합물 KR900001675A (ko)

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NL88306121.0 1988-07-05
EP88306121 1988-07-05

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US (1) US5026724A (ko)
EP (1) EP0352832B1 (ko)
JP (1) JPH0285241A (ko)
KR (1) KR900001675A (ko)
AU (1) AU619567B2 (ko)
DE (1) DE68901424D1 (ko)
DK (1) DK332489A (ko)
ES (1) ES2051986T3 (ko)
FI (1) FI893248A (ko)
GR (1) GR3005347T3 (ko)
IE (1) IE60969B1 (ko)
NZ (1) NZ229773A (ko)
PT (1) PT91057B (ko)
ZA (1) ZA894880B (ko)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE913683A1 (en) * 1990-10-26 1992-05-22 Akzo Nv USE OF A BENZO[b]THIOPHENE-2-CARBOXIMIDAMIDE DERIVATIVE
US5276052A (en) * 1990-10-26 1994-01-04 Akzo N.V. Use of a benzo[b]thiopene-2-carboximidamide derivative
US5340833A (en) * 1992-05-01 1994-08-23 Eisai Co., Ltd. Urokinase inhibitors
DE4321444A1 (de) * 1993-06-28 1995-01-05 Bernd Prof Dr Clement Pharmazeutische Zubereitung
US5955495A (en) * 1996-05-03 1999-09-21 Hoffmann-La Roche Inc. Method of treating diseases of the CNS
US6291514B1 (en) 1998-02-09 2001-09-18 3-Dimensional Pharmaceuticals, Inc. Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
CN101212967A (zh) 2005-05-10 2008-07-02 因塞特公司 吲哚胺2,3-双加氧酶调节剂及其用法
CA2634198C (en) 2005-12-20 2014-06-03 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
CL2007002650A1 (es) 2006-09-19 2008-02-08 Incyte Corp Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras.
CA2663057C (en) 2006-09-19 2015-12-08 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
AU2009268739B2 (en) 2008-07-08 2014-05-08 Incyte Holdings Corporation 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
HUE049337T2 (hu) 2013-11-08 2020-09-28 Incyte Holdings Corp Eljárás indolamin-2,3-dioxigenáz inhibitor elõállítására

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1231170A (ko) * 1967-12-15 1971-05-12
US3910955A (en) * 1970-12-21 1975-10-07 Aspro Nicholas Ltd Benzothiophene-ethylamines
US4158015A (en) * 1978-08-16 1979-06-12 Mobil Oil Corporation Process for the stereoselective synthesis of the E isomer of aryl alkyl oximes
US4737519A (en) * 1983-12-14 1988-04-12 The Upjohn Company Substituted naphthalenes, indoles, benzofurans, and benzothiophenes as lipoxygenase inhibitors
GB8406906D0 (en) * 1984-03-16 1984-04-18 Akzo Nv Benzo-thiazole and benzothiophene derivatives
GB8508588D0 (en) * 1985-04-02 1985-05-09 Akzo Nv Indene & napthalene derivatives

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NZ229773A (en) 1991-12-23
DK332489A (da) 1990-01-06
FI893248A (fi) 1990-01-06
DE68901424D1 (de) 1992-06-11
AU3783789A (en) 1990-01-11
US5026724A (en) 1991-06-25
GR3005347T3 (ko) 1993-05-24
AU619567B2 (en) 1992-01-30
DK332489D0 (da) 1989-07-04
ZA894880B (en) 1990-03-28
EP0352832B1 (en) 1992-05-06
IE892038L (en) 1990-01-05
EP0352832A1 (en) 1990-01-31
PT91057B (pt) 1994-12-30
ES2051986T3 (es) 1994-07-01
PT91057A (pt) 1990-02-08
JPH0285241A (ja) 1990-03-26
IE60969B1 (en) 1994-09-07
FI893248A0 (fi) 1989-07-04

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