KR910015568A - 신경 보호성 3-피페리디노-4-하이드록시 크로만 유도체 - Google Patents

신경 보호성 3-피페리디노-4-하이드록시 크로만 유도체 Download PDF

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KR910015568A
KR910015568A KR1019910002022A KR910002022A KR910015568A KR 910015568 A KR910015568 A KR 910015568A KR 1019910002022 A KR1019910002022 A KR 1019910002022A KR 910002022 A KR910002022 A KR 910002022A KR 910015568 A KR910015568 A KR 910015568A
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compound
separated
piperidino
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general formula
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KR930011041B1 (ko
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윌리엄 버틀러 토드
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제이. 트레보 럼
화이자 인코포레이티드
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/10Heterocyclic 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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14Heterocyclic 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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/48Oxygen atoms attached in position 4 having an acyclic carbon atom attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/52Oxygen atoms attached in position 4 having an aryl radical as the second substituent in position 4
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06Oxygen atoms

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  • Organic Chemistry (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

내용 없음

Description

신경 보호성 3-피페리디노-4-하이드록시 크로만 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (8)

  1. 하기 일반식(Ⅰ)의 화합물 또는 약제학적으로 허용가능한 그의 염.
    상기식에서, A 및 B는 함께 -CH2CH2-이거나, 서로 분리되어 각각 H이고; X는 CH2또는 O이며; X1은 H 또는 OH이고; Z는 H, F, Cl, Br 또는 OH이며; Z1은 H, F, Cl, Br 또는 (C1-C3)알킬이고; n은 0 또는 1이며; m은 0 또는 1 내지 6의 정수이다.
  2. 제1항에 있어서, 하기 일반식(Ia)의 시스 입체 화학식을 갖는 화합물.
    상기식에서, A 및 B는 서로 분리되어 있고; Z는 H, F, Cl 또는 OH이며; Z1은 H이고; m은 0.1 또는 2이며; x는 0이고; n은 1이다.
  3. 제2항에 있어서, Z가 크로만 환 시스템의 7-위치에 치환되며 OH인 화합물.
  4. 제1항에 있어서, 하기 일반식(Ib)의 트란스 입체 화학식을 갖는 화합물.
    상기식에서, A 및 B는 서로 분리되어 있고; Z는 OH이며; Z1은 H이고; m은 0.1 또는 2이며; x는 CH2이고; n은 1이다.
  5. 제4항에 있어서, Z가 테트라하이드로나프탈렌 환 시스템의 6-위치에 치환되며 OH인 화합물.
  6. 제1항에 있어서, A 및 B가 서로 분리되어 있으며, Z가 OH이고, Z1이 H이며, m이 0.1 또는 2이고, x가 CH2이며, n이 0인 화합물.
  7. 제6항에 있어서, X1이 OH이고, m이 0인 화합물.
  8. 하기 일반식(Ⅱ)의 화합물
    상기식에서, A 및 B는 함께 -CH2CH2- 이거나, A 및 B가 서로 분리되어 각각 H이고; G 및 J는 함께 O이거나, G 와 J가 서로 분리되어 G는 수소이고, J는 하이드록시이며; X는 CH2또는 O이며; X1은 H 또는 OH이며; Z1은 H, F, Cl, Br 또는 (C1-C3)알킬이고; Z3는 H, F, Cl, Br 또는 OR이며; R은 H 또는 통상의 하이드록시 보호 그룹이고; n은 0 또는 1이며; m은 0 또는 1 내지 6의 정수이고; 단, G 및 J가 분리되어 있을때 Z3는 OR1이고, R1은 통상의 하이드록시 보호그룹이다.
    하기 일반식(Ⅲ)의 화합물.
    상기식에서, A 및 B는 함께 -CH2CH2- 이거나, A 및 B가 서로 분리되어 각각 H이고; X1은 H 또는 OH이며; Z1은 H, F, Cl,Br 또는 (C1-C3)알킬이고; Z3은 H, F, Cl, Br 또는 OR이며; R은 H 또는 통상의 하이드록시 보호 그룹이고; m은 0 또는1 내지 6의 정수이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910002022A 1990-02-06 1991-02-06 신경 보호성 3-피페리디노-4-하이드록시 크로만 유도체 KR930011041B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
USPCT/US90/00674 1990-02-06
PCT/US1990/000674 WO1991012005A1 (en) 1990-02-06 1990-02-06 Neuroprotective 3-piperidino-4-hydroxychroman derivatives and analogs
US90/00674 1990-02-06

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KR910015568A true KR910015568A (ko) 1991-09-30
KR930011041B1 KR930011041B1 (ko) 1993-11-20

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US (1) US5356905A (ko)
EP (1) EP0441506B1 (ko)
JP (1) JPH0768214B2 (ko)
KR (1) KR930011041B1 (ko)
CN (1) CN1029960C (ko)
AT (1) ATE108787T1 (ko)
AU (1) AU626490B2 (ko)
BR (1) BR9100490A (ko)
CA (1) CA2035653C (ko)
CZ (1) CZ286218B6 (ko)
DE (2) DE69102893T4 (ko)
DK (1) DK0441506T3 (ko)
EG (1) EG19643A (ko)
ES (1) ES2056571T3 (ko)
FI (1) FI94957C (ko)
HU (1) HU222726B1 (ko)
IE (1) IE63836B1 (ko)
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PH (1) PH31061A (ko)
PL (1) PL164866B1 (ko)
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SK (1) SK281729B6 (ko)
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US6476041B1 (en) 1999-10-29 2002-11-05 Merck & Co., Inc. 1,4 substituted piperidinyl NMDA/NR2B antagonists
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US6489477B1 (en) 1999-10-29 2002-12-03 Merck & Co., Inc. 2-aza-bicyclo[2.2.2]octane NMDA/NR2B antigonists
US6369076B1 (en) 1999-10-29 2002-04-09 Merck & Co. Inc. 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists
US6495561B2 (en) 1999-10-29 2002-12-17 Merck & Co., Inc. 2-cyclohexyl imidazopyridine NMDA/NR2B antagonists
US6432976B1 (en) 1999-10-29 2002-08-13 Merck & Co., Inc. 8-aza-bicyclo[3.2.1]octane NMDA/NR2B antagonists
EP1235572A2 (en) 1999-10-29 2002-09-04 MERCK SHARP &amp; DOHME LTD. Method to treat pain utilizing benzimidazole nmda/nr2b antagonists
IL145209A0 (en) 2000-09-06 2002-06-30 Pfizer Prod Inc Pharmaceutical combinations for the treatment of stroke and traumatic brain injury
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CN1029960C (zh) 1995-10-11
PL164866B1 (pl) 1994-10-31
MY105293A (en) 1994-09-30
IE63836B1 (en) 1995-06-14
IL97100A (en) 1996-06-18
EG19643A (en) 1995-09-30
PL288949A1 (en) 1991-07-29
FI94957C (fi) 1995-11-27
ES2056571T3 (es) 1994-10-01
US5356905A (en) 1994-10-18
IL97100A0 (en) 1992-03-29
PT96664B (pt) 1998-07-31
DE69102893T4 (de) 1995-08-10
NO178399B (no) 1995-12-11
CZ286218B6 (cs) 2000-02-16
JPH0768214B2 (ja) 1995-07-26
NZ237025A (en) 1992-11-25
WO1991012005A1 (en) 1991-08-22
DE69102893D1 (de) 1994-08-25
FI923527A (fi) 1992-08-05
AU7029391A (en) 1991-09-05
DE69102893T2 (de) 1994-11-03
PT96664A (pt) 1991-10-31
DK0441506T3 (da) 1994-09-05
ATE108787T1 (de) 1994-08-15
EP0441506A2 (en) 1991-08-14
NO178399C (no) 1996-03-20
BR9100490A (pt) 1991-10-29
CS25091A3 (en) 1991-09-15
CN1053923A (zh) 1991-08-21
EP0441506A3 (en) 1991-11-21
EP0441506B1 (en) 1994-07-20
FI94957B (fi) 1995-08-15
NO923081D0 (no) 1992-08-05
PH31061A (en) 1998-02-05
ZA91830B (en) 1992-09-30
CA2035653A1 (en) 1991-08-07
CA2035653C (en) 1999-12-21
NO923081L (no) 1992-08-05
AU626490B2 (en) 1992-07-30
KR930011041B1 (ko) 1993-11-20
JPH04211058A (ja) 1992-08-03
RU2099339C1 (ru) 1997-12-20
FI923527A0 (fi) 1992-08-05
DE9101346U1 (de) 1991-06-06
HU222726B1 (hu) 2003-09-29
MX24433A (es) 1993-05-01
SK281729B6 (sk) 2001-07-10
IE910372A1 (en) 1991-08-14

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