KR950016738A - 알쯔하이머 질병의 억제 방법 - Google Patents

알쯔하이머 질병의 억제 방법 Download PDF

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KR950016738A
KR950016738A KR1019940034929A KR19940034929A KR950016738A KR 950016738 A KR950016738 A KR 950016738A KR 1019940034929 A KR1019940034929 A KR 1019940034929A KR 19940034929 A KR19940034929 A KR 19940034929A KR 950016738 A KR950016738 A KR 950016738A
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formula
compound
disease
alzheimer
pyrrolidino
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코넬리어스 메이 패트릭
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피터 지. 스트링거
일라이 릴리 앤드 캄파니
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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

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Abstract

본 발명은 유효량의 하기 일반식( I )의 화합물, 또는 그의 약학적으로 허용가능한 염 또는 용매화물을 알쯔하이머 질병의 치료를 필요로 하는 인간에게 투여함을 포함하는, 상기 질환의 억제방법을 포함한다:
상기식에서,
Rl및 R3는 독립적으로 수소,(여기에서, Ar은 임의로 치환된 페닐이다)이고; R2는 피롤리디노, 헥사메틸렌이미노 및 피페리디노로 이루어진 그룹중에서 선택된다.
본 발명은 또한 뇌에서 TGF-β 발현의 중가를 필요로 하는 인간에게 유효량의 일반식(I) 화합물을 투여함을 포함하는, 상기 발현의 증가 방법을 제공한다.
본 발명은 또한 알쯔하이머 질병(AD)과 관련된 염증 반응 또는 β-아밀로이드 펩티드 매개된 신경독성의 억제를 필요로 하는 인간에게 유효랑의 일반식(I) 화합물을 투여함을 특징으로 포함하는, 상기 억제 방법을 제공한다.

Description

알쯔하이머 질병의 억제 방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (8)

  1. 알쯔하이머 질병의 억제에 사용하기 위한 하기 일반식( 1 )의 화합물을 또는 그의 약학적으로 허용가능한 염 또는 용매화물:
    상기식에서,
    R1및 R3는 독립적으로 수소,(여기에서, Ar은 임의로 치환된 페닐이다)이고; R2는 피롤리디노 및 피페리디노로 이루어진 그룹중에서 선택된다.
  2. 제1항에 있어서, 하기 구조식을 갖는 화합물 또는 그의 염산염:
  3. 뇌에서의 TGF-β 발현의 증가에 사용하기 위한 하기 일반식( I )의 화합물 또는 그의 약학적으로 허용가능한 염 또는 용매화물:
    상기식에서,
    R1및 R3는 독립적으로 수소,(여기에서, Ar은 임의로 치환된 페닐이다)이고; R2는 피롤리디노 및 피페리디노로 이루어진 그룹중에서 선택된다.
  4. 제3항에 있어서, 하기 구조식을 갖는 화합물 또는 그의 염산염:
  5. 알쯔하이머 질병과 관련된 염증 반응의 억제에 사용하기 위한 하기 일반식( l )의 화합물 또는 그의 약학적으로 허용가능한 염 또는 용매화물:
    상기식에서,
    R1및 R3는 독립적으로 수소,(여기에서, Ar은 임의로 치환된 페닐이다)이고; R2는 피롤리디노 및 피페리디노로 이루어진 그룹중에서 선택된다.
  6. 제5항에 있어서, 하기 구조식을 갖는 화합물 또는 그와 염산염:
  7. β-아밀로이드 펩티드 매개된 신경독성의 억제에 사용하기 위한 일반식( I )의 화합물 또는 그의 약학적으로 허용가능한 염 또는 용매화물:
    상기식에서,
    R1및 R3는 독립적으로 수소,(여기에서, Ar은 임의로 치환된 페닐이다)이고; R2는 피롤리디노 및 피페리디노로 이루어진 그룹중에서 선택된다.
  8. 제7항에 있어서, 하기 구조식을 갖는 화합물 또는 그의 염산염:
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940034929A 1993-12-21 1994-12-19 알쯔하이머 질병의 억제 방법 KR950016738A (ko)

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US08/171,387 US5552415A (en) 1993-12-21 1993-12-21 Method of inhibiting Alzheimer's Disease
US08/171,387 1993-12-21

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EP (1) EP0659418A1 (ko)
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AU (1) AU688815B2 (ko)
CA (1) CA2138495A1 (ko)
CZ (1) CZ288984B6 (ko)
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CZ288984B6 (cs) 2001-10-17
US5652259A (en) 1997-07-29
JPH07215854A (ja) 1995-08-15
IL112050A (en) 1999-03-12
CN1294913A (zh) 2001-05-16
RU2128992C1 (ru) 1999-04-20
CN1108098A (zh) 1995-09-13
EP0659418A1 (en) 1995-06-28
AU688815B2 (en) 1998-03-19
US5552415A (en) 1996-09-03
US5686476A (en) 1997-11-11
RU94045155A (ru) 1996-11-10
CA2138495A1 (en) 1995-06-22
NO944928D0 (no) 1994-12-19
CN1087937C (zh) 2002-07-24
NO944928L (no) 1995-06-22
IL112050A0 (en) 1995-03-15
HU9403668D0 (en) 1995-02-28
ZA9410095B (en) 1996-06-19
AU8154694A (en) 1995-06-29
HUT71465A (en) 1995-11-28
NZ270177A (en) 1997-08-22
CZ322094A3 (en) 1995-09-13

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