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KR950701922A - 치환된 트리아졸의 설페이트 염, 이를 포함하는 약제학적 조성물 및 치료요법에서의 이의 용도(The sulphate salt of a substituted triazole, pharmaceutical compositions thereof and their use in therapy) - Google Patents

치환된 트리아졸의 설페이트 염, 이를 포함하는 약제학적 조성물 및 치료요법에서의 이의 용도(The sulphate salt of a substituted triazole, pharmaceutical compositions thereof and their use in therapy)

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Publication number
KR950701922A
KR950701922A KR1019940704402A KR19940704402A KR950701922A KR 950701922 A KR950701922 A KR 950701922A KR 1019940704402 A KR1019940704402 A KR 1019940704402A KR 19940704402 A KR19940704402 A KR 19940704402A KR 950701922 A KR950701922 A KR 950701922A
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KR
South Korea
Prior art keywords
salt
pharmaceutically acceptable
composition
solvate
salts
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Granted
Application number
KR1019940704402A
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English (en)
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KR100286411B1 (ko
Inventor
베이커 레이몬드
귈리오 마타샤 빅터
올리브 캐롤
조지 피트 켄달
에드워드 스토레이 데이비드
조셉 스트리트 레슬리
리챠드 귀블린 알렉산더
Original Assignee
더블유. 지. 콜
머크 샤프 앤드 돔 리미티드(Merck Sharp & Dohme Limited)
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Priority claimed from GB929211903A external-priority patent/GB9211903D0/en
Priority claimed from GB939307306A external-priority patent/GB9307306D0/en
Application filed by 더블유. 지. 콜, 머크 샤프 앤드 돔 리미티드(Merck Sharp & Dohme Limited) filed Critical 더블유. 지. 콜
Publication of KR950701922A publication Critical patent/KR950701922A/ko
Application granted granted Critical
Publication of KR100286411B1 publication Critical patent/KR100286411B1/ko
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms

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

Abstract

본 발명은, 5-HT1-유사 수용체의 선택적 작용제인 N,N-디메틸-2-〔5-(12,4-트리아졸-1-일메틸)-1H-인돌-3-일)에틸아민의 설페이트 염에 관한 것이며, 이는 이들 수용체의 선택적 작용제와 관련된, 특히 편두통 및 관련질환의 임상질환을 치료하는데 유용하다.

Description

치환된 트리아졸의 설페이트 염, 이를 포함하는 약제학적 조성물 및 치료요법에서의 이의 용도(The sulphate salt of a substituted triazole, pharmaceutical compositions thereof and their use in therapy)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (20)

  1. N,N-디메틸-2-〔5-(1,2,4-트리아졸-1-일메틸)-1H-인돌-3-일〕에틸아민의 설페이트 염.
  2. 구조식(Ⅰ)의 N,N-디메틸-2-〔5-(1,2,4-트리아졸-1-일메틸)-1H-인돌-3-일〕에틸아민 설페이트 염(2:1) 및 약제학적으로 허용되는 이의 용매화물.
  3. 제2항에서 청구된 바와 같은 염의 수화물.
  4. 제2항에서 청구된 바와 같은 염의 0.7수화물
  5. 하나 이상의 약제학적으로 허용되는 담체와 함께, 제1항 또는 제2항에서 청구된 바와 같은 염 또는 약제학적으로 허용되는 이의 용매화물을 포함하는 약제학적 조성물.
  6. 제1항 또는 제2항에서 청구된 바와 같은 염 또는 약제학적으로 허용되는 이의 용매화물, 투여함에 따라 구강에 7.5이상의 pH를 부여할 수 있는 하나 이상의 약제학적으로 허용되는 완충제 및 하나 이상의 약제학적으로 허용되는 부형제를 포함하는, 설하 투여용으로 적합한 고형물 형태의 약제학적 조성물.
  7. 하나 이상의 약제학적으로 허용되는 담체와 함께, 제1항 또는 제2항에서 청구된 바와 같은 염 또는 약재학적으로 허용되는 이의 용매화물을 포함하는, 비강 투여용으로 적합한 약제학적 조성물.
  8. 제7항에 있어서, 수용제 형태로 존재하는 조성물.
  9. 제8항에 있어서, 무균성, 발열원-무함유 수중의 용제 형태로 존재하는 조성물.
  10. 제8항 또는 제9항에 있어서, 염을 1㎎/㎖ 내지 200㎎/㎖의 농도로 함유하는 조성물.
  11. 제10항에 있어서, 염을 10㎎/㎖ 내지 190㎎/㎖의 농도로 함유하는 조성물.
  12. 제11항에 있어서, 염을 약 189㎎/㎖의 농도로 함유하는 조성물.
  13. 제7항 내지 제12항 중 어느 한 항에 있어서, 단위 투여량 형태로 존재하고 활성성분을 0.1㎎ 내지 100㎎의 양으로 함유하는 조성물.
  14. 제13항에 있어서, 단위 투여용적이 50 내지 200㎕인 조성물.
  15. (A) 구조식(Ⅱ)의 N,N-디메틸-2-(5-(1,2,4-트리아졸-1-일메틸)-1H-인돌-3-일〕에틸아민을 적절한 용매중에서 약 0.5몰 당량의 황산과 반응시키거나, (B) 제2항에서 정의한 구조식(Ⅰ)의 설페이트 염(2:1) 이외의 상기 구조식(Ⅱ)의 화합물의 염을 적절한 설페이트 염으로 처리함을 포함하여, 제1항 또는 제2항에서 청구된 바와 같은 염 또는 이의 용매화물을 제조하는 방법.
  16. 제1항 또는 제2항에서 청구된 바와 같은 염 또는 약제학적으로 허용되는 이의 용매화물을 약제학적으로 허용되는 담체와 혼합함을 포함하여, 제5항 내지 제14항중 어느 한 항에서 청구된 바와 같은 약제학적 조성물을 제조하는 방법.
  17. (A) 제1항 또는 제2항에서 청구된 바와 같은 염 또는 약제학적으로 허용되는 이의 용매화물을 수중에 용해시키거나, (B) 제15항에서 정의된 바와 같은 1몰 당량의 구조식(Ⅱ)의 화합물을 수중 0.5 내지 0.7몰 당량의 농 황산과 혼합함을 포함하여, 제8항 내지 제14항중 어느 한 항에서 청구된 바와 같은 약제학적 조성물을 제조하는 방법.
  18. 치료 요법에 사용하기 위한 제1항 또는 제2항에서 청구된 바와 같은 염 또는 이의 용매화물.
  19. 치료를 필요로 하는 환자에게 유효량의 제1항 또는 제2항에서 청구된 바와 같은 염 또는 약제학적으로 허용되는 이의 용매화물을 투여함을 포함하여, 5-HT1-유사 수용체의 선택적 작용제와 관련된 임상질환을 치료하고/하거나 예방하는 방법.
  20. 5-HT1-유사 수용체의 선택적 작용제와 관련된 임상질환의 치료용 및/또는 예방용 약제의 제조를 위한, 제1항 또는 제2항에서 청구된 바와같은 염 또는 약제학적으로 허용되는 이의 용매화물의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940704402A 1992-06-05 1993-05-28 치환된 트리아졸의 설페이트 염, 이의 제조방법 및 이를 포함하는 약제학적 조성물 Expired - Fee Related KR100286411B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB9211903.1 1992-06-05
GB929211903A GB9211903D0 (en) 1992-06-05 1992-06-05 Pharmaceutical composition
GB939307306A GB9307306D0 (en) 1993-04-07 1993-04-07 Therapeutic agents
GB9307306.2 1993-04-07
PCT/GB1993/001132 WO1993025547A1 (en) 1992-06-05 1993-05-28 The sulphate salt of a substituted triazole, pharmaceutical compositions thereof, and their use in therapy

Publications (2)

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KR950701922A true KR950701922A (ko) 1995-05-17
KR100286411B1 KR100286411B1 (ko) 2001-04-16

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KR1019940704402A Expired - Fee Related KR100286411B1 (ko) 1992-06-05 1993-05-28 치환된 트리아졸의 설페이트 염, 이의 제조방법 및 이를 포함하는 약제학적 조성물

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US (1) US5527817A (ko)
EP (1) EP0573221B1 (ko)
JP (2) JP2619197B2 (ko)
KR (1) KR100286411B1 (ko)
CN (1) CN1043532C (ko)
AT (1) ATE165602T1 (ko)
AU (2) AU659311B2 (ko)
BG (1) BG61976B1 (ko)
CA (1) CA2097208C (ko)
CZ (1) CZ282060B6 (ko)
DE (1) DE69318212T2 (ko)
DK (1) DK0573221T3 (ko)
ES (1) ES2116411T3 (ko)
FI (3) FI106201B (ko)
HK (1) HK1010050A1 (ko)
HU (1) HUT71403A (ko)
IL (1) IL105847A (ko)
LV (1) LV12210B (ko)
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RO (1) RO114326B1 (ko)
RU (1) RU2130022C1 (ko)
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UA27908C2 (uk) 2000-10-16
NO944656D0 (no) 1994-12-02
CZ304494A3 (en) 1995-09-13
RO114326B1 (ro) 1999-03-30
FI20001776A7 (fi) 2000-08-10
US5527817A (en) 1996-06-18
LV12210B (en) 1999-03-20
SK147994A3 (en) 1995-07-11
AU4337293A (en) 1994-01-04
BG99132A (bg) 1995-07-28
JP2972150B2 (ja) 1999-11-08
KR100286411B1 (ko) 2001-04-16
BG61976B1 (bg) 1998-11-30
SG50406A1 (en) 1998-07-20
CN1089263A (zh) 1994-07-13
JPH09176155A (ja) 1997-07-08
RU2130022C1 (ru) 1999-05-10
ES2116411T3 (es) 1998-07-16
FI20001777A7 (fi) 2000-08-10
NZ253210A (en) 1995-09-26
EP0573221B1 (en) 1998-04-29
HK1010050A1 (en) 1999-06-11
IL105847A0 (en) 1993-09-22
LV12210A (lv) 1999-01-20
HU9403478D0 (en) 1995-02-28
NO944656L (no) 1994-12-02
DK0573221T3 (da) 1998-10-07
CA2097208A1 (en) 1993-12-06
MX9303373A (es) 1995-01-31
DE69318212D1 (de) 1998-06-04
AU3987593A (en) 1993-12-09
SK279211B6 (sk) 1998-08-05
FI945694A0 (fi) 1994-12-02
WO1993025547A1 (en) 1993-12-23
CZ282060B6 (cs) 1997-05-14
NO307420B1 (no) 2000-04-03
DE69318212T2 (de) 1998-11-19
EP0573221A1 (en) 1993-12-08
FI106201B (fi) 2000-12-15
FI20001776L (fi) 2000-08-10
AU659311B2 (en) 1995-05-11
FI20001777L (fi) 2000-08-10
RU94046380A (ru) 1996-12-10
HUT71403A (en) 1995-11-28
JPH0641121A (ja) 1994-02-15
CN1043532C (zh) 1999-06-02
JP2619197B2 (ja) 1997-06-11
FI945694L (fi) 1994-12-02
CA2097208C (en) 2005-02-08
IL105847A (en) 1998-09-24
ATE165602T1 (de) 1998-05-15

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