KR910018367A - 4-[3-(4-옥소티아졸리디닐)]부티닐아민, 이의 제조방법 및 약물로서 이의 용도 - Google Patents

4-[3-(4-옥소티아졸리디닐)]부티닐아민, 이의 제조방법 및 약물로서 이의 용도 Download PDF

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KR910018367A
KR910018367A KR1019910005987A KR910005987A KR910018367A KR 910018367 A KR910018367 A KR 910018367A KR 1019910005987 A KR1019910005987 A KR 1019910005987A KR 910005987 A KR910005987 A KR 910005987A KR 910018367 A KR910018367 A KR 910018367A
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compound
pharmaceutically acceptable
oxothiazolidine
butynyl
acceptable salt
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KR0163598B1 (ko
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제이. 리브 니콜라스
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원본미기재
훽스트-러셀 파마슈티칼스 인코포레이티드
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/08—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D277/12—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
    • C07D277/14—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems

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Abstract

내용 없음

Description

4-[3-(4-옥소티아졸리디닐)]부티닐아민, 이의 제조방법 및 약물로서 이의 용도
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (22)

  1. 일반식(Ⅰ)의 화합물 및 이의 약제학적으로 허용되는 산부가염 및 적용가능한 경우 광학 및 기하 이성체 및 이의 라세미 혼합물.
  3. 상기식에서, R1및 R2는 서로 독립적으로 수소 또는 저급 알킬이거나, R1및 R2가 이들이 결합된 탄소원자와 함께 탄소수 5 내지 8의 스피로-융합된 사이클로알칸을 형성하고; R3및 R4는 서로 독립적으로 수소 또는 저급 알킬이거나, R3및 R4가 이들이 결합된 탄소원자와 함께 탄소수 5 내지 8의 스피로-융합된 사이클로알칸을 형성하며; R5및 R6는 이들이 결합된 질소원자와 함께
  6. 각 구조식중의 X는 서로 독립적으로 할로겐, 저급알킬, 하이드록시, 니트로, 아미노, 시아노, 트리플루오로메틸 또는 메톡시이고; m은 0, 1 또는 2이다.
  7. 제1항에 있어서, R1, R2, R3및 R4가 수소인 화합물.
  8. 제1항에 있어서, R1, R2및 R4가 수소이고 R3가 알킬인 화합물.
  9. 제1항에 있어서, R3및 R4가 이들이 결합된 탄소원자와 함께 탄소수 5 내지 8의 스피로-융합된 사이클로알칸을 형성하는 화합물.
  10. 제2항에 있어서, 3-〔4-(1-(2-메톡시페닐)피페라지노)-2-부티닐〕-4-옥소티아졸리딘 또는 이의 약제학적으로 허용되는 염인 화합물.
  11. 제2항에 있어서, 3-(4-(1-(2-플루오로페닐)피페라지노)-2-부티닐-4-옥소티아졸리딘 또는 이의 약제학적으로 허용되는 염인 화합물.
  12. 제2항에 있어서, 3-(4-(4-피리딜)피페라지노)-2-부티닐)-4-옥소티아졸리딘 또는 이의 약제학적으로 허용되는 염인 화합물.
  13. 제2항에 있어서, 3-(4-(1-(4-클로로벤즈히드릴)-피페라지노)-2-부티닐)-4-옥소티아졸리딘 또는 이의 약제학적으로 허용되는 염인 화합물.
  14. 제2항에 있어서, 3-(4-〔3-(4-피페리딜)-6-클로로-벤즈이속사졸〕-2-부티닐)-4-옥소티아졸리딘 또는 이의 약제학적으로 허용되는 염인 화합물.
  15. 제3항에 있어서, 2-메틸-3-(4-(4하이드록시-4-페닐피페리디노)-2-부티닐)-4-옥소티아졸리딘 또는 이의 약제학적으로 허용되는 염인 화합물.
  16. 활성 성분으로서 제1항에 정의된 바와 같은 화합물 및 이에 적합한 담체를 함유함을 특징으로 하는 약제학적 조성물.
  17. 진통 및/또는 협압 강화 활성을 갖는 약제를 제조하기 위한, 제1항에서 정의된 바와 같은 화합물의 용도.
  18. 일반식(Ⅱ)의 화합물을 촉매의 존재하에서 포름알데히드 또는 포름알데히드 등가물 및 다음 구조식의 아민중 하나와 반응시킴을 특징으로 하여, 제1항에서 정의된 바와 같은 화합물을 제조하는 방법.
  21. 상기식에서, R1, R2, R3및 R4는 제1항에 정의된 바와 같고; X는 각 식에서 서로 독립적으로 할로겐, 저급알킬, 하이드록시, 니트로, 아미노, 시아노, 트리플루오로메틸 또는 메톡시이며; m은 0, 1 또는 2이다.
  22. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910005987A 1990-04-16 1991-04-15 4-[3-(4-옥소티아졸리디닐)]부티닐아민, 이의 제조방법 및 이를 함유하는 약제학적 조성물 KR0163598B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/509,280 US5034392A (en) 1990-04-16 1990-04-16 4-(3-(4-oxothiazolidinyl)butynylamines
US509,280 1990-04-16

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KR910018367A true KR910018367A (ko) 1991-11-30
KR0163598B1 KR0163598B1 (ko) 1998-12-01

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US (1) US5034392A (ko)
EP (1) EP0452850B1 (ko)
JP (1) JPH07119223B2 (ko)
KR (1) KR0163598B1 (ko)
AR (1) AR248402A1 (ko)
AT (1) ATE163010T1 (ko)
AU (1) AU636972B2 (ko)
BG (1) BG60066A3 (ko)
CA (1) CA2040489C (ko)
CZ (1) CZ284447B6 (ko)
DE (1) DE69128845T2 (ko)
DK (1) DK0452850T3 (ko)
ES (1) ES2112844T3 (ko)
FI (1) FI94755C (ko)
GR (1) GR3026319T3 (ko)
HU (1) HUT61017A (ko)
IE (1) IE911257A1 (ko)
IL (1) IL97852A (ko)
MX (1) MX25359A (ko)
NO (1) NO300134B1 (ko)
NZ (1) NZ237811A (ko)
PL (1) PL165488B1 (ko)
PT (1) PT97371B (ko)
RO (1) RO108683B1 (ko)
RU (1) RU2001914C1 (ko)
ZA (1) ZA912783B (ko)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5273977A (en) * 1990-11-05 1993-12-28 Warner-Lambert Company Substituted tetrahydropyridines and hydroxypiperidines as central nervous system agents
US5147881A (en) * 1990-11-14 1992-09-15 Pfizer Inc 4-(1,2-benzisoxazolyl)piperidine antipsychotic agents
US5194436A (en) * 1991-01-10 1993-03-16 Hoechst-Roussel Pharmaceuticals Inc. 1-piperazinyl-2-butenes and -2-butynes
US5130315A (en) * 1991-01-10 1992-07-14 Raymond R. Wittekind 1-piperazinyl-2-butenes and -2-butynes

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3354178A (en) * 1965-04-09 1967-11-21 Sterling Drug Inc Nu-(4-amino-2-butynyl)-nu-alkylcarboxamides
ATE81123T1 (de) * 1987-11-20 1992-10-15 Hoechst Roussel Pharma 3-(4(1-substituierte-4-piperazinyl)butyl>-4thiazolidinone, verfahren zu deren herstellung und ihre anwendung als arzneimittel.

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CA2040489A1 (en) 1991-10-17
DE69128845D1 (de) 1998-03-12
DK0452850T3 (da) 1998-09-23
FI94755C (fi) 1995-10-25
NO300134B1 (no) 1997-04-14
PT97371A (pt) 1992-01-31
RU2001914C1 (ru) 1993-10-30
IL97852A (en) 1994-11-28
ES2112844T3 (es) 1998-04-16
IL97852A0 (en) 1992-06-21
FI911783A0 (fi) 1991-04-12
PL289892A1 (en) 1992-07-27
CA2040489C (en) 2003-06-10
HUT61017A (en) 1992-11-30
AR248402A1 (es) 1995-08-18
JPH04234879A (ja) 1992-08-24
MX25359A (es) 1994-05-31
EP0452850B1 (en) 1998-02-04
PT97371B (pt) 1998-08-31
AU7502891A (en) 1991-10-17
IE911257A1 (en) 1991-10-23
ZA912783B (en) 1991-12-24
KR0163598B1 (ko) 1998-12-01
US5034392A (en) 1991-07-23
AU636972B2 (en) 1993-05-13
GR3026319T3 (en) 1998-06-30
RO108683B1 (ro) 1994-07-29
NO911465D0 (no) 1991-04-15
NZ237811A (en) 1993-12-23
CS9101065A2 (en) 1991-11-12
PL165488B1 (pl) 1994-12-30
DE69128845T2 (de) 1998-07-09
NO911465L (no) 1991-10-17
JPH07119223B2 (ja) 1995-12-20
ATE163010T1 (de) 1998-02-15
FI94755B (fi) 1995-07-14
FI911783A (fi) 1991-10-17
BG60066A3 (en) 1993-09-15
CZ284447B6 (cs) 1998-11-11
EP0452850A1 (en) 1991-10-23
HU911239D0 (en) 1991-10-28

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