KR880002829A - 디하이드로피리딘 항알러지제 및 소염제 - Google Patents

디하이드로피리딘 항알러지제 및 소염제 Download PDF

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KR880002829A
KR880002829A KR870009443A KR870009443A KR880002829A KR 880002829 A KR880002829 A KR 880002829A KR 870009443 A KR870009443 A KR 870009443A KR 870009443 A KR870009443 A KR 870009443A KR 880002829 A KR880002829 A KR 880002829A
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alkyl
compound
substituted
aryl
formula
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KR870009443A
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쿠퍼 켈빈
존 패리 마이클
에드워드 크로스 피터
리챠드슨 케네스
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알렌 제이. 스피겔
화이자 인코포레이티드
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Publication of KR880002829A publication Critical patent/KR880002829A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/82—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
    • C07D211/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D417/14—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 three or more hetero rings

Abstract

내용 없음

Description

디하이드로피리딘 항알러지제 및 소염제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 하기 일반식(Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 염.
    상기식에서, R은 페닐이거나 니트로, 할로, C1-C4알킬, C1-C4알콕시, 아릴(C1-C4알콕시), C1-C4알칼티오, C1-C4알킬설포닐, 하이드록시, 트리플루오로메틸 및 시아노로부터 선택된 1개 이상의 치환제에 의해 치환된 페닐이며, R1및 R2는 각각 독립적으로 수소 또는 C1-C6알킬이거나, 두 그룹은 이들이 부착된 질소원자와 함께 결합하여 피롤리디닐, 피페리디노, 모르폴리노, 피페라지닐 또는 N-(치환된)-피페라지닐 그룹[여기서, 치환체는 C1-C4알킬, C2-C4알카노일 또는 피리딜이다]을 형성할 수 있거나, R2는 수소 또는 C1-C4알킬이고, R1은 C3-C7사이클로알킬, 아릴, 인다닐 또는 헤테로 아릴, 또는 C3-C7사이클로알킬, C1-C4알콕시카보닐, 아릴 및 헤테로아릴로부터 선택된 1개 이상의 치환체에 의해 치환된 C1-C4알킬그룹이며, R3는 C1-C6알킬이고, Y는, X를 산소원자에 연결시키는 쇄중에 적어도 2개의 탄소원자를 갖는 직쇄 또는 측쇄일 수 있는 탄소수 2내지 8의 알킬렌 그룹이며, X는 C1-C4알킬 그룹 또는 할로원자일 수 있는 1 내지 3개의 치환체로 임의 치환되거나, 4 및 5위치가 -(CH2)p-[여기서, p는 3 또는 4이다]에 의해 연결될 수 있는 1-이미다졸릴이다.
  2. 제1항에 있어서, R이 2-클로로페닐인 화합물.
  3. 제1항 또는 2항에 있어서, Y가 -(CH2)2-인 화합물.
  4. 제1항에 있어서, R4가 에틸인 화합물.
  5. 제1항에 있어서, X가 2,4,5-트로메틸-1-이미다졸린인 화합물.
  6. 제1항에 있어서, R2가 수소이고, R1이 3급-부틸인 화합물.
  7. 제1항에 있어서, Rx가 수소이고, R1이 헤테로아릴로서, 임의로 벤조융합될 수 있거나, C1-C4알킬, C1-C4알콕시 또는 할로에 의해 치환될 수 있는 피리딜, 티에닐, 리파졸릴, 티아졸릴, 티아디아졸릴, 또는 옥사졸릴인 화합물.
  8. 제7항에 있어서, R1이 피리드-2-일, 6-메틸-피리드-2-일, 티아졸-2-일 또는 벤조티아졸-2-일인 화합물.
  9. 제1항에 있어서, 4-(2-클로롤페닐)-3-에톡시카보닐-6-메틸-5-(N-3급-부틸가바모일)-2-[2-(2,4,5-트리메틸이미다졸-1-일)에톡시메틸]-1,4-디하이드로피리딘 또는 4-(2-클로로페닐)-3-에톡시카보닐-6-메틸-5-[N-(6-메틸-피리드-2-일)카바모일]-2-[2-(2,4,5-트리메틸이미다졸-1-일)에톡시메틸]-1,4-디하이드로피리딘인 화합물.
  10. (a) 일반식(Ⅱ)의 화합물, 일반식(Ⅴ)의 알데하이드 및 일반식(Ⅲ)의 화합물을 함께 반응시키거나, (b) 일반식(Ⅳ)의 아민을 일반식의 디온과 반응시킨 다음, 이어서 일반식 R5CH(NH2)2의 아민알 또는 이의 삼량체를 부가시키고, 각 경우에 임의로, 생성물의 약제학적으로 허용되는 염을 형성시킴을 특징으로 하여 일반식(Ⅰ)의 화합물 및 약제학적으로 허용되는 이의 염을 제조하는 방법.
    상기식에서 R은 페닐이거나 니트로, 할로, C1-C4알킬, C1-C4알콕시, 아릴(C1-C4알콕시), C1-C4알킬티오, C1-C4알킬설포닐 하이드록시, 트리플루오로메틸 및 시아노로부터 선택된 1개 이상의 치환체에 의해 치환된 페닐이며, R1및 R2는 각각 독립적으로 수소 또는 C1-C6알킬이거나, 두 그룹은 이들이 부착된 질소원자와 함께 결합하여 피롤리디닐, 피페리디노, 모르폴리노, 피페라지닐 또는 N-(치환된)-피페라지닐 그룹[여기서, 치환체는 C1-C4알킬, C2-C4알카노일 또는 피리딜이다]을 형성할 수 있거나, R2는 수소 또는 C1-C4알킬이고, R1은 C3-C7사이클로알킬, 아릴, 안다닐 또는 헤테로아릴, 또는 C3-C7사이클로알킬, C1-C4알콕시카보닐, 아릴 및 헤테로아릴로부터 선택된 1개 이상의 치환체에 의해 치환된 C1-C4알킬그룹이며, R3는 C1-C6알킬이고, R4및 R5는 각각 C1-C4알킬이며, Y는 X를 산소원자에 연결시키는 쇄중에 적어도 2개의 탄소원자를 갖는 직쇄 또는 측쇄일 수 있는 탄소수 2 내지 8의 알킬렌 그룹이고, X는 C1-C4알킬그룹 또는 할로원자일 수 있는 1 내지 3개의 치환체로 임의 치환되거나, 4 및 5위치가-(CH2)p-[여기서, p는 3 또는 4이다]에 의해 연결될 수 있는 1-이미다졸릴이다.
  11. 제 1 항 내지 9항중의 어느 하나에서 청구한 일반식(I)의 화합물 또는 약제학적으로 허용되는 이의염과 함게 약제학적으로 허용되는 희석제 또는 담체를 함유함을 특징으로 하는 약제학적 조성물.
  12. 의약품으로서, 특히 인간의 알러지, 염증 및 과다분비 상태의 치료시에 사용하기 위한, 제1항 내지 9항 중의 어느 하나에서 청구한 일반식(I)의 화합물 또는 약제학적으로 허용되는 이의 염.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR870009443A 1986-08-29 1987-08-28 디하이드로피리딘 항알러지제 및 소염제 KR880002829A (ko)

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GB868620880A GB8620880D0 (en) 1986-08-29 1986-08-29 Therapeutic agents
GB8620880 1986-08-29

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US (1) US4788205A (ko)
EP (1) EP0258033B1 (ko)
JP (1) JPS6363661A (ko)
KR (1) KR880002829A (ko)
CN (1) CN87106032A (ko)
AT (1) ATE92486T1 (ko)
AU (1) AU7767887A (ko)
DD (1) DD262023A5 (ko)
DK (1) DK450687A (ko)
FI (1) FI873725A (ko)
GB (1) GB8620880D0 (ko)
HU (1) HUT45047A (ko)
IE (1) IE872317L (ko)
IL (1) IL83681A0 (ko)
NO (1) NO873650L (ko)
PL (1) PL267485A1 (ko)
PT (1) PT85607B (ko)
ZA (1) ZA876437B (ko)

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GB8803963D0 (en) * 1988-02-19 1988-03-23 Pfizer Ltd Therapeutic agents
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US5478848A (en) * 1994-01-26 1995-12-26 Bayer Corporation Inhibition of arthritis by L-type calcium channel antagonists nimodipine, nisoldipine and nifedipine
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US6566359B1 (en) 2002-05-20 2003-05-20 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College 2,4,6-trimethyl-1,4-dihydro-pyridine-3,5-dicarboxylic acid esters as neuroprotective drugs
PL1889198T3 (pl) 2005-04-28 2015-04-30 Proteus Digital Health Inc System farmakologiczno-informatyczny
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ES2919563T3 (es) 2009-02-20 2022-07-27 Enhanx Biopharm Inc Sistema de administración de medicamentos a base de glutatión
JP2012526144A (ja) 2009-05-06 2012-10-25 ラボラトリー スキン ケア インコーポレイテッド 活性物質−リン酸カルシウム粒子複合体を含む経皮送達組成物およびその使用方法
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EP0174131A3 (en) * 1984-09-01 1989-06-07 FISONS plc Dihydropyridines, processes and intermediates for their production, and pharmaceutical formulations containing them

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EP0258033A2 (en) 1988-03-02
US4788205A (en) 1988-11-29
AU7767887A (en) 1988-03-10
JPS6363661A (ja) 1988-03-22
PL267485A1 (en) 1988-09-01
HUT45047A (en) 1988-05-30
NO873650L (no) 1988-03-01
FI873725A (fi) 1988-03-01
PT85607B (pt) 1990-05-31
EP0258033A3 (en) 1990-11-07
IE872317L (en) 1988-02-29
PT85607A (en) 1987-09-01
ZA876437B (en) 1989-03-29
GB8620880D0 (en) 1986-10-08
CN87106032A (zh) 1988-03-23
ATE92486T1 (de) 1993-08-15
EP0258033B1 (en) 1993-08-04
DD262023A5 (de) 1988-11-16
IL83681A0 (en) 1988-01-31
DK450687A (da) 1988-03-01
FI873725A0 (fi) 1987-08-27
DK450687D0 (da) 1987-08-28
NO873650D0 (no) 1987-08-28

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