KR970706261A - 치료법에 유용한 퀴녹살린 유도체(quinoxaline derivatives useful in therapy) - Google Patents

치료법에 유용한 퀴녹살린 유도체(quinoxaline derivatives useful in therapy) Download PDF

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KR970706261A
KR970706261A KR1019970701887A KR19970701887A KR970706261A KR 970706261 A KR970706261 A KR 970706261A KR 1019970701887 A KR1019970701887 A KR 1019970701887A KR 19970701887 A KR19970701887 A KR 19970701887A KR 970706261 A KR970706261 A KR 970706261A
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alkyl
compound
formula
pharmaceutically acceptable
acceptable salt
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KR1019970701887A
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마이클 조나단 프레이
찰스 에릭 모우브레이
알란 스토비에
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무어 제임스 더블유
화이자 리서치 앤드 디벨롭먼트 캄파니 엔브이/에스에이
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Publication of KR970706261A publication Critical patent/KR970706261A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines 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
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

화학식(I)의 화합물 및 약학적으로 허용가능한 이의 유도체는 특히 신경변성 장애의 치료에 유용하다:
상기 식에서, A는 N 또는 CH이고; R1및 R2은 독립적으로 C1-4알킬, 할로 또는 CF3이고; R3은 C1-4알킬(임의로 치환됨), C3-7사이클로알킬, CF3또는 아릴이고; R4는 H, C3-7사이클로알킬 또는 C1-6알킬(임의로 치환됨)이다.

Description

치료법에 유용한 퀴녹살린 유도체(QUINOXALINE DERIVATIVES USEFUL IN THERAPY)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (17)

  1. 화학식(I)의 화합물 또는 약학적으로 허용가능한 이의 염 :
    상기 식에서, A는 N또는 CH이고; R1및 R2은 독립적으로 C1-4알킬, 할로 또는 CF3이고; R3은 C1-4알킬(임의로 C3-7사이클로알킬 또는 아릴에 의해 치환됨), C3-7사이클로알킬, CF3또는 아릴이고; R4는 H, C3-7사이클로알킬 또는 C1-6알킬[임의로 OH, C1-4알콕시, 아릴(임의로 C1-4알킬, C1-4알콕시, 할로 및 CF3로 부터 독립적으로 선택된 3개까지의 치환체에 의해 치환됨), 헤테로사이클릴(임의로 C1-4알킬, C1-4알콕시, OH, 할로, CF3및 옥소로부터 독립적으로 선택된 3개까지의 치환체에 의해 치환되고, 임의로 벤조-융합됨), C2-6알케닐, C2-6알키닐, C2-6알카노일, CO2H, C1-4알콕시카보닐, NH2, C1-4알킬아미노, 디(C1-4알킬)아미노, NHSO2CF3, CONR5R6, NHCONR5R6또는 O(CH2)nNR5R6에 의해 치환됨]이고; R5및 R6은 독립적으로 H또는 C1-4알킬이거나, 또는 이들이 부착된 질소 원자와 함께 피롤리디노, 피페리디노 또는 모폴리노그룹을 형성하고; n은 2,3 또는 4이다.
  2. 제1항에 있어서, A가 N인 화합물.
  3. 제1 또는 제2항에 있어서, R1이 할로 또는 C1-4알킬인 화합물.
  4. 제1항 내지 제3항 중 어느 한 항에 있어서, R2가 할로 또는 C1-4알킬인 화합물.
  5. 제1항 내지 제4항 중 어느 한 항에 있어서, R3가 C1-4알킬인 화합물.
  6. 제5항에 있어서, R3가 메틸인 화합물.
  7. 제1항 내지 제6항중 어느 한 항에 있어서, R4가 OH 또는 CO2H에 의해 치환된 C1-6알킬인 화합물.
  8. 제7항에 있어서, R4가 CH2CH2OH또는 CH2CO2H인 화합물.
  9. 제2항에 있어서, 질소 원자간의 결합의 키랄설이 A에 의해 대표되고, 1,4-디하이드로-2,3-디옥소퀴녹살린 환이 하기 화학식(IA)와 같은 화합물:
    (여기서 R1-4는 제1항에서 정의된 바와 같다)
  10. 제1항 내지 제9항 중 어느 한 항에 있어서, (R)-N-(1,4-디하이드로-6,7-디클로로-2,3-디옥소퀴녹살린-5-일)-N-(2-하이드록시에틸)메탄술폰아미드인 화합물.
  11. 제1항 내지 제9항 중 어느 한 항에 있어서, (R)-N-(카복시메틸)-N-(1,4-디하이드로-6,7-디클로로-2,3-디옥소퀴녹살린-5-일)메탄술폰아미드인 화합물.
  12. 제1항에서 정의된 바와 같은 화학식(I)의 화합물 또는 약학적으로 허용가능한 이의 염을 약학적으로 허용가능한 보조제, 희석제 또는 담체와 함께 포함하는 약학적 제형물.
  13. 제1항에 있어서, 약학제로서 사용하기 위한 화학식(I)의 화합물 또는 약학적으로 혀용가능한 이의 염.
  14. 불안완화성, 항경련성, 마취성 또는 신경보호성 약제의 제조에 있어서, 제1항에서 정의된 바와 같은 화학식(I)의 화합물 또는 약학적으로 허용가능한 이의 염의 용도.
  15. 제1항에서 정의된 바와 같은 화학식(I)의 화합물 또는 약학적으로 허용가능한 이의 염을 불안완화성, 항경련성, 마취성 또는 신경보호성의 치료가 요구되는 환자에게 투여함을 포함하는, 불안완화성, 항경련성, 마취성 또는 신경보호성 치료방법.
  16. 하기 화학식(Ⅱ)의 화합물로부터 보호 그룹을 제거하고, 원하거나 필요할 경우 생성된 화합물을 약학적으로 허용가능한 염 또는 이의 역으로 전환시킴을 포함하는, 화학식(I)의 화합물 또는 약학적으로 허용가능한 이의 염의 제조 방법:
    여기서, A 및 R1-4는 제1항에서 정의된 바와 같고, P및 P는 하이드록시 보호 그룹이다)
  17. 제16항에 정의된 화학식(Ⅱ)의 화합물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019970701887A 1994-09-24 1995-09-08 치료법에 유용한 퀴녹살린 유도체(quinoxaline derivatives useful in therapy) KR970706261A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB9419318.2 1994-09-24
GB9419318A GB9419318D0 (en) 1994-09-24 1994-09-24 Therapeutic agents
PCT/EP1995/003559 WO1996009295A1 (en) 1994-09-24 1995-09-08 Quinoxaline derivatives useful in therapy

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KR970706261A true KR970706261A (ko) 1997-11-03

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US (1) US5852016A (ko)
EP (1) EP0783495B1 (ko)
JP (1) JP2986920B2 (ko)
KR (1) KR970706261A (ko)
CN (1) CN1158610A (ko)
AT (1) ATE213731T1 (ko)
AU (1) AU688591B2 (ko)
BR (1) BR9504132A (ko)
CA (1) CA2200742C (ko)
CO (1) CO4410336A1 (ko)
CZ (1) CZ85797A3 (ko)
DE (1) DE69525633T2 (ko)
DK (1) DK0783495T3 (ko)
ES (1) ES2171553T3 (ko)
FI (1) FI971193A (ko)
GB (1) GB9419318D0 (ko)
HU (1) HUT77734A (ko)
IL (2) IL115334A0 (ko)
MX (1) MX9702259A (ko)
NO (1) NO971261L (ko)
NZ (1) NZ292922A (ko)
PE (1) PE47596A1 (ko)
PL (1) PL319405A1 (ko)
PT (1) PT783495E (ko)
RU (1) RU2135484C1 (ko)
TR (1) TR199501158A2 (ko)
WO (1) WO1996009295A1 (ko)
ZA (1) ZA958023B (ko)

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MY132385A (en) * 1995-08-31 2007-10-31 Novartis Ag 2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives
DK0784973T3 (da) * 1995-10-10 2002-03-18 Pfizer Quinoxalinderivater til behandling af tinnitus
GB9604400D0 (en) * 1996-03-01 1996-05-01 Pfizer Ltd Compounds useful in therapy
AU3133697A (en) 1996-06-05 1998-01-05 Warner-Lambert Company Amide derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists
US5721256A (en) * 1997-02-12 1998-02-24 Gpi Nil Holdings, Inc. Method of using neurotrophic sulfonamide compounds
AU722616B2 (en) * 1997-02-18 2000-08-10 American Home Products Corporation 5-aminoalkoxy-1,4-dihydroquinoxaline-2,3-diones being dopamine agonists
US5922715A (en) * 1997-02-18 1999-07-13 American Home Products Corporation 5-aminoalkoxy-1, 4-dihydroquinoxaline-2, 3-diones
TW526195B (en) 1997-06-10 2003-04-01 Novartis Ag Crystal modifications of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide and their use
GB0310881D0 (en) * 2003-05-12 2003-06-18 Merck Sharp & Dohme Pharmaceutical formulation
US10208000B2 (en) 2015-12-16 2019-02-19 University Of Kentucky Research Foundation Eis inhibitors

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DK146787A (da) * 1987-03-23 1988-09-24 Ferrosan Heterocykliske forbindelser, deres fremstilling og anvendelse
DK715888D0 (da) * 1988-12-22 1988-12-22 Ferrosan As Quinoxalinforbindelser, deres fremstilling og anvendelse
DE69132340T2 (de) * 1990-11-06 2001-02-08 Yamanouchi Pharma Co Ltd Kondensiertes pyrazinderivat
DE4123106A1 (de) * 1991-07-09 1993-01-14 Schering Ag Arzneimittel zur behandlung von entzugssymptomen
PT101004B (pt) * 1991-10-26 1999-10-29 Schering Ag Derivados da quinoxalina, processo para a sua preparacao e composicoes farmaceuticas que os contem
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IL109397A0 (en) * 1993-04-28 1994-07-31 Schering Ag Quinoxalinedione derivatives, processes for the preparation thereof and pharmaceutical compositions containing the same
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Publication number Publication date
AU688591B2 (en) 1998-03-12
NO971261D0 (no) 1997-03-19
CA2200742C (en) 2001-09-11
NO971261L (no) 1997-05-05
MX9702259A (es) 1997-06-28
ES2171553T3 (es) 2002-09-16
ZA958023B (en) 1997-03-24
JPH09511526A (ja) 1997-11-18
CA2200742A1 (en) 1996-03-28
EP0783495A1 (en) 1997-07-16
CN1158610A (zh) 1997-09-03
ATE213731T1 (de) 2002-03-15
TR199501158A2 (tr) 1997-02-21
RU2135484C1 (ru) 1999-08-27
PT783495E (pt) 2002-07-31
DE69525633D1 (de) 2002-04-04
IL126104A0 (en) 1999-05-09
EP0783495B1 (en) 2002-02-27
BR9504132A (pt) 1996-08-06
WO1996009295A1 (en) 1996-03-28
JP2986920B2 (ja) 1999-12-06
CZ85797A3 (cs) 1998-09-16
PE47596A1 (es) 1996-11-12
DK0783495T3 (da) 2002-04-22
IL115334A0 (en) 1995-12-31
NZ292922A (en) 1998-07-28
US5852016A (en) 1998-12-22
AU3523295A (en) 1996-04-09
FI971193A0 (fi) 1997-03-21
GB9419318D0 (en) 1994-11-09
HUT77734A (hu) 1998-07-28
DE69525633T2 (de) 2002-08-08
FI971193A (fi) 1997-05-21
PL319405A1 (en) 1997-08-04
CO4410336A1 (es) 1997-01-09

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