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KR900006342A - 1,4-디아제핀 유도체 및 그의 약학적 이용 - Google Patents

1,4-디아제핀 유도체 및 그의 약학적 이용 Download PDF

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KR900006342A
KR900006342A KR1019890015723A KR890015723A KR900006342A KR 900006342 A KR900006342 A KR 900006342A KR 1019890015723 A KR1019890015723 A KR 1019890015723A KR 890015723 A KR890015723 A KR 890015723A KR 900006342 A KR900006342 A KR 900006342A
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group
compound
compounds
hydrogen
cycloalkyl
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KR910009332B1 (ko
Inventor
가즈오 오가노
스헤이 미야자와
스테펜 존 클라크 리차드
신야 아베
데쯔야 가와하라
나오유끼 시모무라
오사무 아사노
히로유끼 요시무라
미쯔아끼 미야모또
요시노리 사꾸마
겐조 무라모또
히로시 오바이시
고우기찌 하라다
하지메 쯔노다
사또시 가따야마
고우지 야마다
시게루 소우다
요시마사 마찌다
고우이찌 가따야마
이사오 야마쯔
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나이또오 하루오
에자이 가부시끼가이샤
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Publication of KR900006342A publication Critical patent/KR900006342A/ko
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • 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
    • 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
    • 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
    • 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
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

내용없음

Description

1,4-디아제핀 유도체 및 그의 약학적 이용
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (21)

  1. 하기 주어진 식의 트리아졸로-1,4-디아제핀 화합물 및 그의 약리학적으로 허용가능한 염.
    상기식에서, R1과 R2는 동일 또는 상이하며 수소원자 또는 저급알킬기를 나타내고, R3은 수소 원자 또는 할로겐원자를 나타내며, R4는 수소원자 또는 저급알킬기를 나타낸다. X는 (a)식의 기, (b) 식 의 기(식중 R5는 수소원자 또는 저급알킬기를 나타낸다), (c) 식의 기, (d) 식의 기(식중 R6은 저급알킬기를 나타낸다.) (e) 식의 기를 나타내며 n은 0 또는 1의 정수이고, Y는 (1) 치환기(들)를 가질 수 있는 시클로알킬기, (2) 시클로 알킬알킬, (3) 알키닐기, (4) 식의 기(식중 R7은 수소 또는 메틸이며 r은 0,1 또는 2이다. (5) 식 NC-(CH2)p-의 기(식중 p는 1 내지 6의 정수이다), (6) 식 A-(CH2)q-의 기 (A는 피리딜기, 피라닐기 및 모르폴리노기로부터 선택된 기를 나타내며 q는 0 내지 6의 정수이다. (7) 1내지 6탄소원자를 가지고 있는 알키닐기(이때에 페닐기 또는 시클로알킬기가 어는 한 탄소원자에 결합된다), (8) 식의 기, (9) 식의 기(식중 R8과 R9는 동일 또는 상이한 것으로, 수소원자, 저급알킬기, 피리딜메틸기 또는 시클로알킬기를 나타내며 또는 R8과 R9는 질소원자와 함께 결합하여 고리를 형성할 수 있고, B는 페닐렌기 또는 1내지 3탄소원자를 가지는 저급알킬렌 기를 나타낸다), (10) 식의 기, (11) 식CH2-C≡C-CH2-의 기, (12) 식의 기, (13) 식의 기, (14) 식의 기, (15) 저급알킬기, 또는 (16) 시클로알킬알케닐기, (17)(CH2)s- (s는 1 또는 2이다.) (18)(t는 1 또는 2이다), (19)(20) 아릴알킬, (21) 아릴알케닐, (22)(E)u- (R10은 수소 또는 페닐이며, R11은 수소 또는 저급알킬이고, E는 알케닐렌이며 u는 0 또는 1이다.), 또는 (23)(식중 G는 알케닐렌 또는 -J-(CH2)k-이고, 이때에 J는 산소 또는 황이며, k는 0,1 또는 2이다)를 나타내며, 단, X가 (a)(b)(c), 또는 (e)인 경우 Y는 (1) 내지 (14)에서 선택된 기이고, X가 (d)인 경우, Y는 (15)의 기이며, n이 0일때 Y는 (3)의 알키닐기이다.
  2. 제1항에 있어서, X가 (a), (b) 또는 (c)인 것을 특징으로 하는 화합물 및 염.
  3. 제1항에 있어서, X가 (c) -CO-인 것을 특징으로 하는 화합물 및 염.
  4. 제1항에 있어서, Y가 (1) 내지 (16)중의 하나인 것을 특징으로 하는 화합물 및 염.
  5. 제1항에 있어서, X가 (c) -CO-이고 n이 1인 것을 특징으로 하는 화합물 및 염.
  6. 제1항에 있어서, X가 (a) -COO-이고 n이 1인 것을 특징으로 하는 화합물 및 염.
  7. 제1항에 있어서, X가 (b) -NR5-CO-이고 n이 1인 것을 특징으로 하는 화합물 및 염.
  8. 제1항 내지 제7항중 어느 하나에 있어서, Y가 시클로알킬인 것을 특징으로 하는 화합물 및 염.
  9. 제1항 내지 제7항중 어느 하나에 있어서, Y가 3내지 7탄소원자를 가지는 시클로알킬인 것을 특징으로 하는 화합물 및 염.
  10. 제1항 내지 제7항중 어느 하나에 있어서, Y가 시클로프로필인 것을 특징으로 하는 화합물 및 염.
  11. 제1항 내지 제7항중 어느 하나에 있어서, R1이 수소이고 R2가 메틸인 것을 특징으로 하는 화합물 및 염.
  12. 제1항 내지 제7항중 어느 하나에 있어서, R1이 수소이고 R2가 메틸이며 Y가 시클로알킬인 것을 특징으로 하는 화합물 및 염.
  13. 제1항에 있어서, Y가 (4),(3),(16) 및 (2) 중의 하나인 것을 특징으로 하는 화합물 및 염.
  14. 제1항에 있어서, Y가 HC≡C-C(CH3)2-인 것을 특징으로 하는 화합물 및 염.
  15. 제1항에 있어서, R3이 염소이고, R1이 수소이며, R4는 메틸이고, n은 1이며, Y-X-및 R2은 다음 조합중의 어느 하나로 규정되는 것을 특징으로 하는 화합물 및 염.
  16. 다음식의 트리아졸로-1,4-디아제핀 화합물 및 그의 약리학적으로 허용가능한 염.
    (상기식에서, Y, X, n, R1, R2, R3, R4는 제1항에서와 동일하게 규정된다.)
  17. 다음식의 트리아졸로-1,4-디아제핀 화합물 및 그의 약리학적으로 허용가능한 염.
    (상기식에서, Y, X, n, R1, R2, R3, R4는 제1항에서와 같이 규정된다.)
  18. 제1항에 규정된 화합물 또는 그의 염의 약리학적 유효량과 약리학적으로 허용가능한 담체로 이루어지는 약학조성물.
  19. 제1항에서 규정된 화합물 또는 그의 염의 약리학적 유효량을 투여하는 것으로 이루어지는, 항-PAF 활성이 효과적으로 대항하는 질병의 치료방법.
  20. 제19항에 있어서, 질병이 알레르기성 질병인 것을 특징으로 하는 방법.
  21. 제19항에 있어서, 질병이 천식인 것을 특징으로 하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890015723A 1988-10-31 1989-10-31 1,4-디아제핀 유도체 및 그의 약학적 이용 Expired KR910009332B1 (ko)

Applications Claiming Priority (12)

Application Number Priority Date Filing Date Title
JP27546088 1988-10-31
JP63-275460 1988-10-31
JP275460 1988-10-31
JP297068 1988-11-24
JP63-297,068 1988-11-24
JP29706888 1988-11-24
JP63-318,016 1988-12-16
JP318016 1988-12-16
JP31801688 1988-12-16
JP63-331,622 1988-12-28
JP33162288 1988-12-28
JP331622 1988-12-28

Publications (2)

Publication Number Publication Date
KR900006342A true KR900006342A (ko) 1990-05-08
KR910009332B1 KR910009332B1 (ko) 1991-11-11

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EP (3) EP0677524B1 (ko)
JP (1) JP2756004B2 (ko)
KR (1) KR910009332B1 (ko)
CN (1) CN1036520C (ko)
AT (3) ATE234306T1 (ko)
AU (1) AU621413B2 (ko)
CA (1) CA2000985C (ko)
DE (3) DE68929049T2 (ko)
DK (1) DK540689A (ko)
FI (1) FI95708C (ko)
HU (1) HU217127B (ko)
NO (1) NO175259C (ko)
NZ (1) NZ231188A (ko)
PH (1) PH27461A (ko)
PT (1) PT92153B (ko)

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FI894867A0 (fi) 1989-10-13
PT92153A (pt) 1990-05-31
CA2000985A1 (en) 1990-04-30
CN1036520C (zh) 1997-11-26
NO175259B (no) 1994-06-13
NO894287D0 (no) 1989-10-27
JPH02256682A (ja) 1990-10-17
JP2756004B2 (ja) 1998-05-25
HUT53106A (en) 1990-09-28
NO175259C (no) 1994-09-21
ATE234306T1 (de) 2003-03-15
CA2000985C (en) 2000-01-18
EP0606103A1 (en) 1994-07-13
CN1121076A (zh) 1996-04-24
KR910009332B1 (ko) 1991-11-11
NO894287L (no) 1990-05-02
FI95708C (fi) 1996-03-11
DE68929455T2 (de) 2004-01-08
DE68929455D1 (de) 2003-04-17
AU621413B2 (en) 1992-03-12
EP0677524B1 (en) 2002-02-13
PH27461A (en) 1993-07-09
EP0367110B1 (en) 1999-08-11
PT92153B (pt) 1995-06-30
DK540689A (da) 1990-05-01
EP0677524A1 (en) 1995-10-18
AU4376189A (en) 1990-05-03
HU217127B (hu) 1999-11-29
DE68929049T2 (de) 2000-01-27
EP0367110A1 (en) 1990-05-09
FI95708B (fi) 1995-11-30
HU895609D0 (en) 1990-01-28
DE68929372D1 (de) 2002-03-21
EP0606103B1 (en) 2003-03-12
ATE213247T1 (de) 2002-02-15
DK540689D0 (da) 1989-10-30
DE68929372T2 (de) 2002-10-02
NZ231188A (en) 1991-06-25
ATE183187T1 (de) 1999-08-15
DE68929049D1 (de) 1999-09-16

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