KR960034200A - 항편두통성 인돌릴알킬-피리딘일 및 피리미딘일피페라진의 1,2,5-티아디아졸 유도체 - Google Patents

항편두통성 인돌릴알킬-피리딘일 및 피리미딘일피페라진의 1,2,5-티아디아졸 유도체 Download PDF

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Publication number
KR960034200A
KR960034200A KR1019960005354A KR19960005354A KR960034200A KR 960034200 A KR960034200 A KR 960034200A KR 1019960005354 A KR1019960005354 A KR 1019960005354A KR 19960005354 A KR19960005354 A KR 19960005354A KR 960034200 A KR960034200 A KR 960034200A
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South Korea
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compound
vascular headache
administered
hydrogen
effective amount
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KR1019960005354A
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English (en)
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알. 크렌쇼 로니
에이치. 뤼디거 에드워드
더블유. 스미쓰 데이비드
솔로몬 카롤라
예비치 조셉
Original Assignee
니콜라스 피 · 말라테스티닉
브리스톨-마이어즈 스퀴브 컴페니
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Application filed by 니콜라스 피 · 말라테스티닉, 브리스톨-마이어즈 스퀴브 컴페니 filed Critical 니콜라스 피 · 말라테스티닉
Publication of KR960034200A publication Critical patent/KR960034200A/ko

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

식(Ⅰ)의 인돌린알킬피페라진일 피리딘 및 피리미딘의 일련의 신규 5-(3,4-디아미노-1,2,5-티아디아졸 S-옥사이드) 유도체가 혈관성 두통의 완화에 사용되는 것이 목적이다.
식 (Ⅰ)에서 X는 S, SO 및 SO2중에서 선택된다.

Description

항편두통의 인돌릴알킬-피리딘일 및 피리미딘일피페라진의 1,2,5-티아디아졸 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (14)

  1. 식 (Ⅰ)의 화합물 또는 약리학적으로 허용되는 산부가염 및/또는 그의 용매화물:
    상기 식에서 R1은 수소, 할로겐, 저급 알킬 및 저급 알콕시 중에서 선택되고; R2,R3및 R5는 각각 수소 및 저급 알킬 중에서 선택되고; R4는 저급 알콕시; R5는아미노, 저급 알킬아미노, 디-저급 알킬아미노 및 저급 알콕시이며; X는 S, So 및 SO2중에서 선택되고, Y 및 Z는 각각 Y 및 Z가 모두 다 동시에 CH일 수 없다는 조건하에 N 및 CH중에서 선택되며; m은 제로 및 1~3의 정수 중에서 선택되고; n은 1~5 정수 중에서 선택된다.
  2. 제1항에 있어서, Y 및 Z가 N인 화합물.
  3. 제1항에 있어서, X가 SO인 화합물.
  4. 제3항에 있어서, R1,R2,R3및 R5가 수소인 화합물.
  5. 제3항에 있어서, m이 제로이고 n이 3인 화합물.
  6. 제3항에 있어서, R4가 메톡시인 화합물.
  7. 제3항에 있어서, R1,R2,R3및 R5가 수소이고, R4가 메톡시이고; Y 및 Z가 N이고; m이 제로이며 n이 3인 화합물.
  8. 제7항에 있어서, R5가 아미노 메틸아미노, 디메틸아미노, 및 메톡시인 화합물 중에서 선택된 화합물.
  9. 혈관성 두통에 걸린 사람에게 제1항의 화합물의 치료 유효량을 투여하는 혈관성 두통의 치료방법.
  10. 혈관성 두통에 걸린 사람에게 제3항의 화합물의 치료 유효량을 투여하는 혈관성 두통의 치료방법.
  11. 초기의 혈관성 두통에 걸린 사람에게 제1항의 화합물의 예방 유효량을 투여하는 혈관성 두통의 중지방법.
  12. 초기의 혈관성 두통에 걸린 사람에게 제3항의 화합물의 예방 유효량을 투여하는 혈관성 두통의 중지방법.
  13. 혈관성 두통의 위험이 있거나 혈관성 두통에 걸린 사람에게 전신 투여에 적합한 단위 투여랑 형태의 약제 조성물로서, 조성물이 약제 부형제와 제1항의 화합물 약 1~500㎎로 이루어진 약제 조성물.
  14. 혈관성 두통의 위험이 있거나 혈관성 두통에 걸린 사람에게 전신 투여에 적합한 단위 투여랑 형태의 약제 조성물로서, 조성물이 약제 부형제와 제3항의 화합물 약 1~500㎎로 이루어진 약제 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960005354A 1995-03-02 1996-02-29 항편두통성 인돌릴알킬-피리딘일 및 피리미딘일피페라진의 1,2,5-티아디아졸 유도체 KR960034200A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/396,825 1995-03-02
US08/396,825 US5618816A (en) 1995-03-02 1995-03-02 Antimigraine 1,2,5-thiadiazole derivatives of indolylalkyl-pyridnyl and pyrimidinylpiperazines

Publications (1)

Publication Number Publication Date
KR960034200A true KR960034200A (ko) 1996-10-22

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KR1019960005354A KR960034200A (ko) 1995-03-02 1996-02-29 항편두통성 인돌릴알킬-피리딘일 및 피리미딘일피페라진의 1,2,5-티아디아졸 유도체

Country Status (17)

Country Link
US (1) US5618816A (ko)
EP (1) EP0729958A2 (ko)
JP (1) JPH08253479A (ko)
KR (1) KR960034200A (ko)
CN (1) CN1063177C (ko)
AR (1) AR002281A1 (ko)
AU (1) AU707770B2 (ko)
CA (1) CA2169804A1 (ko)
CZ (1) CZ46896A3 (ko)
HU (1) HUP9600498A3 (ko)
IL (1) IL117224A (ko)
NO (1) NO305248B1 (ko)
NZ (1) NZ286090A (ko)
PL (1) PL313022A1 (ko)
RU (1) RU2165420C2 (ko)
TW (1) TW331558B (ko)
ZA (1) ZA961392B (ko)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU694226B2 (en) * 1994-05-19 1998-07-16 Merck Sharp & Dohme Limited Piperazine, piperidine and tetrahydropyridine derivatives ofindol-3-ylalkyl as 5-HT1D-alpha agonists
GB9415575D0 (en) * 1994-08-02 1994-09-21 Merck Sharp & Dohme Therapeutic agents
GB9501865D0 (en) * 1995-01-31 1995-03-22 Merck Sharp & Dohme Therapeutic agents
US8022095B2 (en) 1996-08-16 2011-09-20 Pozen, Inc. Methods of treating headaches using 5-HT agonists in combination with long-acting NSAIDs
US5872145A (en) * 1996-08-16 1999-02-16 Pozen, Inc. Formulation of 5-HT agonist and NSAID for treatment of migraine
US6586458B1 (en) 1996-08-16 2003-07-01 Pozen Inc. Methods of treating headaches using 5-HT agonists in combination with long-acting NSAIDs
US7189753B1 (en) 1997-11-06 2007-03-13 Cady Roger K Preemptive prophylaxis of migraine
JP4616009B2 (ja) * 2002-12-26 2011-01-19 ポーゼン インコーポレイテッド NSAIDsおよびトリプタンを含有する多層剤型
US20070184109A1 (en) * 2003-06-06 2007-08-09 Floyd Alison G Compositions comprising triptans and nsaids
WO2015014256A1 (en) 2013-07-29 2015-02-05 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use thereof
WO2016192657A1 (en) 2015-06-03 2016-12-08 Sunshine Lake Pharma Co., Ltd. Substituted piperazine compounds and methods of use and use thereof

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3468882A (en) * 1966-10-07 1969-09-23 Sterling Drug Inc Phenylhydrazone derivatives as intermediates for preparing indoles
NL189197C (nl) * 1979-09-04 1993-02-01 Bristol Myers Squibb Co 3,4-digesubstitueerde-1,2,5-thiadiazool-1-oxiden en 1,1-dioxiden, bereiding daarvan alsmede farmaceutische preparaten.
US4600779A (en) * 1982-03-29 1986-07-15 Bristol-Myers Company Substituted 3,4-diamino-1,2,5-thiadiazoles having histamine H2 -receptor antagonist activity
IT1170387B (it) * 1982-06-07 1987-06-03 Glaxo Group Ltd Composti eterociclici, procedimento per prepararli e composizioni farmaceutiche che li contengono
US4440933A (en) * 1983-03-16 1984-04-03 Bristol-Myers Company Process for preparing 1,2,5-thiadiazoles
GB2162522B (en) * 1984-08-01 1988-02-24 Glaxo Group Ltd An indole derivative
US4954502A (en) * 1988-06-10 1990-09-04 Bristol-Myers Squibb Company 1-indolyalkyl-4-(substituted-pyridinyl)piperazines
FR2635104B1 (fr) * 1988-08-03 1992-04-30 Synthelabo Derives d'indolone, leur preparation et leur application en therapeutique
FR2672052B1 (fr) * 1991-01-28 1995-05-24 Esteve Labor Dr Derives d'aryl (ou heteroaryl)-piperazinyl-alkyl-azoles, leur preparation et leur application en tant que medicaments.
US5077293A (en) * 1990-06-29 1991-12-31 Bristol-Myers Squibb Co. 1-indolyalkyl-4-(alkoxypyrimidinyl)piperazines
CA2043709C (en) * 1990-06-29 2002-01-22 David W. Smith Antimigraine alkoxypyrimidine derivatives
DE4101686A1 (de) * 1991-01-22 1992-07-23 Merck Patent Gmbh Indolderivate
CA2084531A1 (en) * 1991-12-19 1993-06-20 David W. Smith Antimigraine 4-pyrimidinyl and pyridinyl derivatives of indol-3yl-alkyl piperazines
CA2130078A1 (en) * 1993-09-16 1995-03-17 Jonas A. Gylys Antimigraine cyclobutenedione derivatives of indolylalkyl-pyridinyl and pyrimidinylpiperazines
GB9410031D0 (en) * 1994-05-19 1994-07-06 Merck Sharp & Dohme Therapeutic agents
AU694226B2 (en) * 1994-05-19 1998-07-16 Merck Sharp & Dohme Limited Piperazine, piperidine and tetrahydropyridine derivatives ofindol-3-ylalkyl as 5-HT1D-alpha agonists
GB9415575D0 (en) * 1994-08-02 1994-09-21 Merck Sharp & Dohme Therapeutic agents

Also Published As

Publication number Publication date
CN1138042A (zh) 1996-12-18
EP0729958A3 (ko) 1996-10-02
JPH08253479A (ja) 1996-10-01
NO960699L (no) 1996-09-03
IL117224A (en) 2000-06-29
CA2169804A1 (en) 1996-09-03
ZA961392B (en) 1997-08-21
IL117224A0 (en) 1996-06-18
TW331558B (en) 1998-05-11
NZ286090A (en) 1997-12-19
HUP9600498A3 (en) 1998-10-28
AU707770B2 (en) 1999-07-22
EP0729958A2 (en) 1996-09-04
CN1063177C (zh) 2001-03-14
RU2165420C2 (ru) 2001-04-20
CZ46896A3 (en) 1996-09-11
NO305248B1 (no) 1999-04-26
PL313022A1 (en) 1996-09-16
HU9600498D0 (en) 1996-04-29
HUP9600498A2 (en) 1997-10-28
NO960699D0 (no) 1996-02-22
US5618816A (en) 1997-04-08
AR002281A1 (es) 1998-03-11
AU4581996A (en) 1996-09-12

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