KR970701044A - 콜린에스테라제 활성제 - Google Patents

콜린에스테라제 활성제 Download PDF

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Publication number
KR970701044A
KR970701044A KR1019960704350A KR19960704350A KR970701044A KR 970701044 A KR970701044 A KR 970701044A KR 1019960704350 A KR1019960704350 A KR 1019960704350A KR 19960704350 A KR19960704350 A KR 19960704350A KR 970701044 A KR970701044 A KR 970701044A
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South Korea
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group
cholinesterase
general formula
compound represented
action
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KR1019960704350A
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요시아키 다나카
나오미 고바야시
나오키 나카타
이타루 야마구치
타다시 모리
Original Assignee
이베 사치아키
제리아 신야쿠 고교 가부시키가이샤
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Publication of KR970701044A publication Critical patent/KR970701044A/ko

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    • 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
    • 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
    • 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
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • 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
    • A61P25/28—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Organic Chemistry (AREA)
  • Neurology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

본 발명은 하기 일반식(I)
{식 중, A는 페닐기 또는 인다닐기와 같은 기를 나타내고, B는 프롤릴기 또는 티오프롤릴기를 나타내며, m은 0~5의 점수를 나타낸다.} 표시되는 화합물을 유효성분으로 함유하는 콜린에스테라제 활성제에 관한 것이다.
본 발명에 따른 콜린에스테라제 활성화제는 강력한 콜린에스테라제 활성작용, 특히 선택적으로 말초콜린에스테라제를 활성화 작용을 가지며, 또한 안정성이 높기 때문에, 중추성 콜린에스테라제의 저해제의 부작용, 특히 간장해의 예방, 치료제 및 각종약제의 콜린에스테라제 저해작용으로 인한 부작용 예방, 치료제로서도 유용하다.

Description

콜린에스테라제 활성제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (5)

  1. 하기 일반식(I)
    {식 중, A는
    (여기에서, R1및 R2은 같거나 다르며, 수소원자, 알킬기, 알콕시기,아미노기, 또는 할로겐 원자를 나타내고, R3는 수소원자 또는 히드록시기를 나타내고, B는 다음 식
    (여기서, R4는 수소원자, 포르밀기, 시아노기, 디알콕시메틸기, 카르복시기, 알콕시카르보닐기, 또는 히드록시메틸기를 나타내고, X는 메틸렌기, 에틸렌기, 산소원자, 유황원자, 술포닐기, 술포닐기 또는 -CH2-S-를 나타내고, Y는 메틸렌기, 에틸렌기, -CH2-S- , 유황원자, 술포닐기 또는 술포닐기를 나타내고, m은 0~5의 정수를 나타낸다. } 로 표시되는 화합물을 유효성분으로 함유하는 콜린에스테라제 활성제.
  2. 제1항의 일반식(I)로 표시되는 화합물을 유효성분으로 함유하는 콜린에스테라제 작용저하로 인한 질환의 예방 및 치료제.
  3. 제1항의 일반식(I)로 표시되는 화합물의 콜린에스테라제 활성화제로의 사용.
  4. 콜린에스테라제 작용저하로 인한 질환의 예방 및 치료제를 위한 제1항의 일반식(I)로 표시되는 화합물의 사용.
  5. 제1항의 일반식(I)로 표시되는 화합물을 유효량을 투여함을 특징으로 하는 콜린에스테라제 작용저하로 인한 질환의 치료방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960704350A 1994-02-17 1995-02-17 콜린에스테라제 활성제 KR970701044A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP6041714A JPH07228529A (ja) 1994-02-17 1994-02-17 コリンエステラーゼ賦活剤
JP41714/1994 1994-02-17
PCT/JP1995/000229 WO1995022326A1 (fr) 1994-02-17 1995-02-17 Activateur de la cholinesterase

Publications (1)

Publication Number Publication Date
KR970701044A true KR970701044A (ko) 1997-03-17

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ID=12616097

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Application Number Title Priority Date Filing Date
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Country Link
US (1) US6017929A (ko)
EP (1) EP0754454A4 (ko)
JP (1) JPH07228529A (ko)
KR (1) KR970701044A (ko)
AU (1) AU681251B2 (ko)
CA (1) CA2182882A1 (ko)
WO (1) WO1995022326A1 (ko)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE122010000020I1 (de) * 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
KR100688740B1 (ko) * 1999-03-15 2007-02-28 액시스 파마슈티컬스 인코포레이티드 프로테아제 억제제로서의 ｎ-시아노메틸 아미드
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
JP2004523506A (ja) 2000-12-22 2004-08-05 アクシス・ファーマシューティカルズ・インコーポレイテッド カテプシン阻害剤としての新規な化合物と組成物
EP1436255A1 (en) 2001-09-14 2004-07-14 Aventis Pharmaceuticals, Inc. Novel compounds and compositions as cathepsin inhibitors
KR20050044497A (ko) 2001-11-14 2005-05-12 아벤티스 파마슈티칼스 인크. 올리고펩티드 및 카텝신 ｓ 억제제로서 이를 포함하는조성물
EA200702208A1 (ru) * 2005-04-22 2008-04-28 Алантос Фармасьютиклз Холдинг, Инк. Ингибиторы дипептидилпептидазы-iv
EP1760076A1 (en) 2005-09-02 2007-03-07 Ferring B.V. FAP Inhibitors
TW200803883A (en) * 2005-09-22 2008-01-16 Veritron Ltd Enhancer of cholinesterase activity
CN101190330A (zh) * 2006-11-30 2008-06-04 深圳市鼎兴生物医药技术开发有限公司 胆碱酯酶在拮抗速激肽药物中的应用
EP2889306B1 (en) 2012-08-24 2018-09-19 Ajinomoto Co., Inc. Acyl dipeptide derivative

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Publication number Priority date Publication date Assignee Title
US3928594A (en) * 1974-06-24 1975-12-23 Albert W Cook Method of alleviating symptoms of multiple scleroisis
US5120843A (en) * 1987-04-27 1992-06-09 Upjohn Pharmaceutically active amines
US4857524A (en) * 1987-08-08 1989-08-15 Kissei Pharmaceutical Co., Ltd. Thiazolidine compounds and therapeutic method
CA2084412C (en) * 1990-06-04 2000-05-09 W. Stephen Faraci Pyrrolidine and thiazolidine amides
JPH04261151A (ja) * 1991-02-13 1992-09-17 Zeria Pharmaceut Co Ltd アミノアルコール誘導体及びそれを含有する医薬
AU6983894A (en) * 1993-06-30 1995-01-24 Zeria Pharmaceutical Co., Ltd. Thiazolidine derivative and medicine containing the same

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Publication number Publication date
AU1718195A (en) 1995-09-04
WO1995022326A1 (fr) 1995-08-24
JPH07228529A (ja) 1995-08-29
EP0754454A1 (en) 1997-01-22
US6017929A (en) 2000-01-25
CA2182882A1 (en) 1995-08-24
AU681251B2 (en) 1997-08-21
EP0754454A4 (en) 1998-08-05

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