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KR930017874A - 포화 질소 헤테로사이클의 유도체 - Google Patents

포화 질소 헤테로사이클의 유도체 Download PDF

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Publication number
KR930017874A
KR930017874A KR1019930002171A KR930002171A KR930017874A KR 930017874 A KR930017874 A KR 930017874A KR 1019930002171 A KR1019930002171 A KR 1019930002171A KR 930002171 A KR930002171 A KR 930002171A KR 930017874 A KR930017874 A KR 930017874A
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South Korea
Prior art keywords
formula
compound
salt
pharmaceutically acceptable
radical
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KR1019930002171A
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English (en)
Inventor
프라이 외르그
슈타넥 야로슬라프
Original Assignee
베르너 발데그
시바-가이기 에이지
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Publication of KR930017874A publication Critical patent/KR930017874A/ko
Withdrawn legal-status Critical Current

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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
    • C07D211/06—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 no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • 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
    • C07D211/06—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 no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • 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
    • C07D211/06—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 no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—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 no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

본 발명은 일반식(I)의 화합물 및 이의 염에 관한 것이다.
상기식에서, R1은 일반식 -(CH2)n-O-NH2(Ia)의 라디칼[여기서, n은 0또는 1이다]이고, R2은 수소이거나; 또는 R1은 수소이고, R2는 일반식-(CH2)p-O-NH2(Ib)의 라디칼[여기서, P는 1또는 2이다]이고, R은 중심 피페리딘 환 시스템의 하나의 탄소원자에 부착되지만, 일반식(Ia)의 R1또는 일반식(Ib)의 R2가 부착된 동일한 탄소에 부착되지 않는 C1-C2알킬이고, m은 1또는 2이다.
본 발명은 또한 이라한 화합물들의 제조방법, 이들의 합성 도중에 수득된 중간체, 이들을 포함하는 약제학적 조성물, 및 인체 또는 동물체의 치료 및 약제학적 조성물 제조를 위한 당해 화합물들의 용도에 관한 것이다. 일반식(I)의 화합물은 오르니틴 데카복시라아제의 억제제이다.

Description

포화 질소 헤테로사이클의 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 일반식(I)의 화합물 또는 이의 염.
    상기식에서, R1은 일반식 -(CH2)n-O-NH2(Ia)의 라디칼[여기서, n은 0또는 1이다]이고, R2은 수소이거나; 또는 R1은 수소이고, R2는 일반식-(CH2)p-O-NH2(Ib)의 라디칼[여기서, P는 1또는 2이다]이고, R은 중심 피페리딘 환 시스템의 하나의 탄소원자에 부착되지만, 일반식(Ia)의 R1또는 일반식(Ib)의 R2가 부착된 동일한 탄소에 부착되지 않는 C1-C2알킬이고, m은 1또는 2이다.
  2. 제1항에 있어서, 트랜스-2-메틸-4-아미노옥시-피페리딘 또는 약제학적으로 혀용되는 이의 염인 화합물.
  3. 제1항 또는 제2항에 따르는 일반식(I)의 화합물 또는 당해 화합물의 약제학적으로 허용되는 염을 약제학적으로 허용되는 담체와 함께 포함하는 약제학적 조성물.
  4. 오르니틴 데카복실라아제 효소의 억제에 감응하는 질병을 치료하기 위한, 제1항 또는 제2항에 따르는 일반식(I)의 화합물 또는 약제학적으로 허용되는 이의 염의 용도.
  5. 오르니틴 데카복실라이제 효소의 억제에 감응하는 질병을 치료용 약제학적 조성물을 제조하기 위한, 제1항 또는 제2항에 따르는 일반식(2)의 화합물 또는 이의 염의 용도.
  6. 효소 오르니틴 데카복실라아제 억제에 감응하는 질병을 치료하기 위한, 일반식(I)의 화합물 또는 약제학적으로 허용되는 이의 염의 용도.
  7. (a)일반식(I)의 화합물로부터 아미노 보호 그룹 또는 그들을 제거하거나[여기서, 하나 이상의 아마노 그룹이 보호된다],(b)일반식(V)의 화합물 또는 염 형성 그룹이 존재하는 경우에는 이의 염을 보호된 형태로 반응에 관여하지 않는 출발물질 중의 추가의작용 그룹인W1또는W2의 치환하에 아미노 보호된 하이드록실아민과 반응시키고, 보호그룹들을 제거한 다음, 목적하는 경우, 일반식(I)의 화합물을 일반식(I)의 또다른 화합물로 전환시키고, 이성체 혼합물을 개개의 이성체로 분리시키고/시키거나 일반식(I)의 유리 화합물을 염으로 전환 시키거나 염을 일반식(I)의 유리 화합물 또는 또 다른 염으로 전환시킴을 포함하는 제1항에 따르는 일반식(I)의 화합물의 제조방법.
    상기식에서, R1은 일반식-(CH2)a-W1(Va)의 라디칼[여기서, W|1은 이탈 그룹이고, n은 0또는 1이다]이고, R2"는 수소이거나, 또는 R1"은 수소이고, R2"는 일반식-(CH2)p-W2(Vb)의 라디칼[여기서, W2는 이탈 그룹이고, P는 1또는 2이다]이며, 기타의 기호들은 일반식(I)의 화합물에 대하여 제1항에서 정의된 바와 같다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930002171A 1992-02-17 1993-02-17 포화 질소 헤테로사이클의 유도체 Withdrawn KR930017874A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH00460/92-0 1992-02-17
CH46092 1992-02-17

Publications (1)

Publication Number Publication Date
KR930017874A true KR930017874A (ko) 1993-09-20

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Country Link
US (1) US5322852A (ko)
EP (1) EP0558443A1 (ko)
JP (1) JPH069558A (ko)
KR (1) KR930017874A (ko)
AU (1) AU3298193A (ko)
CA (1) CA2089533A1 (ko)
IL (1) IL104757A0 (ko)
TW (1) TW214545B (ko)
ZA (1) ZA931064B (ko)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3979664B2 (ja) * 1995-03-15 2007-09-19 ノバルティス・アクチエンゲゼルシャフト プトレッシン、スペルミジンおよびスペルミンなどの細胞内の内因性ポリアミンレベルを低下させるピペリジニル−２−アルキル置換直鎖ポリアミン、およびその細胞増殖に対する影響
TWI220143B (en) 1998-05-13 2004-08-11 Solvay Pharm Gmbh Method for stereochemically controlled production of isomerically pure highly substituted azacyclic compounds and novel cyclic compounds, and intermediate products
CN101932325B (zh) 2007-11-30 2014-05-28 新联基因公司 Ido抑制剂
KR20110104933A (ko) * 2008-12-15 2011-09-23 타이젠 바이오테크놀러지 컴퍼니 리미티드 피페리딘 유도체의 입체선택적 합성
US8273521B2 (en) 2009-07-31 2012-09-25 Jsr Corporation Radiation-sensitive resin composition and compound

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* Cited by examiner, † Cited by third party
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NZ219646A (en) * 1986-03-27 1990-10-26 Merck Sharp & Dohme Oxadiazole derivatives of azacyclics for treating cns disorders
EP0369944A1 (de) * 1988-11-18 1990-05-23 Ciba-Geigy Ag Substituierte Oxadiaminobutane
FR2644456B1 (fr) * 1989-03-17 1991-07-05 Rhone Poulenc Sante Nouveaux derives du 1h, 3h-pyrrolo(1,2-c)thiazolecarboxamide-7, leur preparation et les compositions pharmaceutiques qui les contiennent
IL97759A0 (en) * 1990-04-11 1992-06-21 Ciba Geigy Ag Hydroxylamine compounds
EP0495750A3 (en) * 1991-01-14 1992-09-16 Ciba-Geigy Ag Heterocyclic hydroxylamine

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JPH069558A (ja) 1994-01-18
EP0558443A1 (de) 1993-09-01
IL104757A0 (en) 1993-06-10
TW214545B (ko) 1993-10-11
AU3298193A (en) 1993-08-19
US5322852A (en) 1994-06-21
CA2089533A1 (en) 1993-08-18
ZA931064B (en) 1993-08-17

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Patent event date: 19930217

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