CN1035615C - 作为新的乙酰胆碱酯酶抑制剂的芳香杂环胺类的制备方法 - Google Patents

作为新的乙酰胆碱酯酶抑制剂的芳香杂环胺类的制备方法 Download PDF

Info

Publication number
CN1035615C
CN1035615C CN92112079A CN92112079A CN1035615C CN 1035615 C CN1035615 C CN 1035615C CN 92112079 A CN92112079 A CN 92112079A CN 92112079 A CN92112079 A CN 92112079A CN 1035615 C CN1035615 C CN 1035615C
Authority
CN
China
Prior art keywords
formula
compound
reaction
piperidinyl
phenylmethyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CN92112079A
Other languages
English (en)
Chinese (zh)
Other versions
CN1071166A (zh
Inventor
梁玉凭
A·A·内格尔
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Inc
Original Assignee
Pfizer Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer Inc filed Critical Pfizer Inc
Publication of CN1071166A publication Critical patent/CN1071166A/zh
Application granted granted Critical
Publication of CN1035615C publication Critical patent/CN1035615C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/06—Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D409/06—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 only aliphatic carbon atoms
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Control Of Indicators Other Than Cathode Ray Tubes (AREA)
  • Control Of El Displays (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN92112079A 1991-10-03 1992-09-30 作为新的乙酰胆碱酯酶抑制剂的芳香杂环胺类的制备方法 Expired - Fee Related CN1035615C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US77128391A 1991-10-03 1991-10-03
US771.283 1991-10-03

Publications (2)

Publication Number Publication Date
CN1071166A CN1071166A (zh) 1993-04-21
CN1035615C true CN1035615C (zh) 1997-08-13

Family

ID=25091318

Family Applications (1)

Application Number Title Priority Date Filing Date
CN92112079A Expired - Fee Related CN1035615C (zh) 1991-10-03 1992-09-30 作为新的乙酰胆碱酯酶抑制剂的芳香杂环胺类的制备方法

Country Status (36)

Country Link
US (4) US5574046A (enExample)
EP (1) EP0606248B1 (enExample)
JP (1) JP2546785B2 (enExample)
KR (1) KR0170458B1 (enExample)
CN (1) CN1035615C (enExample)
AP (1) AP314A (enExample)
AT (1) ATE235490T1 (enExample)
AU (1) AU667053B2 (enExample)
BG (1) BG61727B1 (enExample)
BR (1) BR9206577A (enExample)
CA (1) CA2119647C (enExample)
CZ (1) CZ290807B6 (enExample)
DE (2) DE69232976T2 (enExample)
DK (1) DK0606248T3 (enExample)
EG (1) EG21481A (enExample)
ES (1) ES2193137T3 (enExample)
FI (1) FI116939B (enExample)
HU (1) HU225049B1 (enExample)
IL (1) IL103274A (enExample)
IS (1) IS1745B (enExample)
MA (1) MA22672A1 (enExample)
MX (1) MX9205678A (enExample)
NO (1) NO308533B1 (enExample)
NZ (1) NZ244601A (enExample)
OA (1) OA09895A (enExample)
PH (1) PH31290A (enExample)
PL (3) PL171984B1 (enExample)
PT (1) PT100917B (enExample)
RO (1) RO112868B1 (enExample)
RU (1) RU2100357C1 (enExample)
SG (1) SG52618A1 (enExample)
TW (1) TW263504B (enExample)
UA (1) UA41290C2 (enExample)
UY (1) UY23484A1 (enExample)
WO (1) WO1993007140A1 (enExample)
ZA (1) ZA927589B (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5620973A (en) * 1993-11-30 1997-04-15 Takeda Chemical Industries, Ltd. Tetracyclic condensed heterocyclic compounds and their use
EP0976404A3 (en) * 1998-07-30 2001-06-27 Pfizer Products Inc. A pharmaceutical composition for the prevention and treatment of diseases of cognitive dysfunction in a mammal
US6218383B1 (en) 1998-08-07 2001-04-17 Targacept, Inc. Pharmaceutical compositions for the prevention and treatment of central nervous system disorders
HUP0104493A3 (en) 1998-09-30 2002-12-28 Takeda Pharmaceutical Drugs for improving vesical excretory strength
SE9902268D0 (sv) * 1999-06-16 1999-06-16 Astra Ab Pharmaceutically active compounds
CN1317276C (zh) * 2000-09-29 2007-05-23 中国科学院上海药物研究所 一类吲哚基哌啶类化合物及其制备方法和用途
KR100823908B1 (ko) * 2000-10-20 2008-04-21 바이오비트럼 에이비(피유비엘) 2-, 3-, 4-, 또는 5-치환-n1-(벤젠술포닐)인돌 및 이의치료 용도
JP2006505571A (ja) * 2002-10-15 2006-02-16 リゲル ファーマシューテイカルズ、インコーポレイテッド 置換されたインドール及びhcv阻害剤としてのその使用
US20060014801A1 (en) * 2002-11-22 2006-01-19 The Johns Hopkins University Prevention and treatment of cognitive impairment using (R)-(-)-5-methyl-1-nicotynoyl-2-pyrazoline (MNP) and analogs
CA2566204A1 (en) * 2004-05-14 2005-12-01 The Johns Hopkins University Method for improving cognitive function by co-administration of a gabab receptor antagonist and an acetylcholinesterase inhibitor
EP1600447A1 (en) * 2004-05-28 2005-11-30 Neuropharma S.A.U. Butyrylcholinesterase selective inhibitors
DK1753764T3 (da) 2004-06-09 2009-02-16 Glaxo Group Ltd Pyrrolopyridin-derivater
EP2425846A1 (en) * 2004-12-23 2012-03-07 Voyager Pharmaceutical Corporation Acetylcholinesterase Inhibitors and leuprolide acetate for the treatment of Alzheimer's disease
CN1808106B (zh) * 2005-01-21 2010-11-24 中国科学院上海药物研究所 一种用核磁共振筛选乙酰胆碱酯酶抑制剂的方法
KR20160127181A (ko) 2008-08-12 2016-11-02 진판델 파마슈티컬스 인코포레이티드 질환 위험 인자의 식별 방법
US8846315B2 (en) 2008-08-12 2014-09-30 Zinfandel Pharmaceuticals, Inc. Disease risk factors and methods of use
CN101503414B (zh) * 2009-03-04 2013-10-30 沈阳药科大学 噻唑并[3,2-b]-1,2,4-三嗪衍生物及其应用
CN103772312B (zh) 2009-10-02 2016-08-17 埃维克辛公司 抗炎症的2-羰基噻唑和2-羰基恶唑
EP2533645B1 (en) 2010-02-09 2016-07-27 The Johns Hopkins University Methods and compositions for improving cognitive function
CN107362165A (zh) 2011-01-10 2017-11-21 金帆德尔制药股份有限公司 用于治疗阿尔茨海默病的方法和药物产品
US10154988B2 (en) 2012-11-14 2018-12-18 The Johns Hopkins University Methods and compositions for treating schizophrenia
US20150376161A1 (en) 2013-01-29 2015-12-31 Avexxin As Antiiflammatory and antitumor 2-oxothiazoles abd 2-oxothiophenes compounds
CA2904767C (en) 2013-03-15 2022-06-21 Agenebio, Inc. Methods and compositions for improving cognitive function
US10806717B2 (en) 2013-03-15 2020-10-20 The Johns Hopkins University Methods and compositions for improving cognitive function
CN103333163A (zh) * 2013-07-09 2013-10-02 广州中医药大学 一种苯并呋喃类衍生物及其制备方法和应用
GB201413695D0 (en) 2014-08-01 2014-09-17 Avexxin As Compound
EA034167B8 (ru) 2015-05-22 2021-04-27 Эйджинбайо, Инк. Фармацевтические композиции леветирацетама пролонгированного высвобождения
GB201604318D0 (en) 2016-03-14 2016-04-27 Avexxin As Combination therapy
CN107141266B (zh) * 2017-06-28 2019-04-09 佳木斯大学附属第一医院 一种用于治疗阿尔茨海默病的杂环化合物及其制备方法
CN115466211B (zh) * 2022-06-09 2024-02-23 中国人民解放军空军军医大学 一种n-苯基喹啉-4-胺类化合物及其应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0288563A1 (en) * 1986-09-30 1988-11-02 Eisai Co., Ltd. Cyclic amine derivatives
EP0351282A1 (fr) * 1988-07-12 1990-01-17 Synthelabo Dérivés de (hydroxy-1 pipéridinyl-2 alkyl)indolones-2, quinoléinones-2, benzo[b]azépinones-2, benzimidazolones-2 et quinazolinones-2, leur préparation et leur application en thérapeutique
EP0441517A2 (en) * 1990-02-08 1991-08-14 Pfizer Inc. Tricyclic amines as novel cholinesterase inhibitors
EP0487071A1 (en) * 1990-11-22 1992-05-27 Takeda Chemical Industries, Ltd. Condensed heterocyclic compounds, their production and use

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1068259B (enExample) * 1954-04-28 1959-11-05
FR2334358A1 (fr) * 1975-12-12 1977-07-08 Sogeras Nouveaux medicaments derives de l'indole
US4122265A (en) * 1976-05-21 1978-10-24 Hoffmann-La Roche Inc. Derivatives of 3-phenylisoindole-1-carboxylic acid
ZA815541B (en) * 1980-08-12 1983-03-30 Glaxo Group Ltd Heterocyclic compounds
GB8615562D0 (en) * 1986-06-25 1986-07-30 Maggioni Farma Aminoalcohols
FI95572C (fi) * 1987-06-22 1996-02-26 Eisai Co Ltd Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi
IT1226100B (it) * 1988-07-07 1990-12-10 Dompe Farmaceutici Spa Derivati benzimidazolici farmacologicamente attivi.
US4908372A (en) * 1988-10-13 1990-03-13 Merrell Dow Pharmaceuticals Inc. Antihistaminic piperidinyl benzimidazoles
JP2969359B2 (ja) * 1989-01-13 1999-11-02 武田薬品工業株式会社 環状アミン化合物
US5064840A (en) * 1989-08-03 1991-11-12 Merrell Dow Pharmaceuticals Anti-psychotic piperidylbenzimidazole compounds
US5116846A (en) * 1990-03-28 1992-05-26 Du Pont Merck Pharmaceutical Company N-aralkyl piperidine derivatives as psychotropic drugs
NZ243065A (en) * 1991-06-13 1995-07-26 Lundbeck & Co As H Piperidine derivatives and pharmaceutical compositions
DE69330823T2 (de) * 1992-02-13 2002-05-02 Merrell Pharmaceuticals Inc., Cincinnati Thiacyclische piperidinylderivate
CA2092112A1 (en) * 1992-03-23 1993-09-24 Nobuyoshi Iwata Indole and indazole derivatives, for the treatment and prophylaxis of cerebral disorders, their preparation and their use

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0288563A1 (en) * 1986-09-30 1988-11-02 Eisai Co., Ltd. Cyclic amine derivatives
EP0351282A1 (fr) * 1988-07-12 1990-01-17 Synthelabo Dérivés de (hydroxy-1 pipéridinyl-2 alkyl)indolones-2, quinoléinones-2, benzo[b]azépinones-2, benzimidazolones-2 et quinazolinones-2, leur préparation et leur application en thérapeutique
EP0441517A2 (en) * 1990-02-08 1991-08-14 Pfizer Inc. Tricyclic amines as novel cholinesterase inhibitors
EP0487071A1 (en) * 1990-11-22 1992-05-27 Takeda Chemical Industries, Ltd. Condensed heterocyclic compounds, their production and use

Also Published As

Publication number Publication date
RU2100357C1 (ru) 1997-12-27
RO112868B1 (ro) 1998-01-30
JPH06510788A (ja) 1994-12-01
DE9290112U1 (de) 1994-06-01
OA09895A (en) 1995-09-15
CA2119647C (en) 1998-08-04
IL103274A (en) 1996-11-14
UA41290C2 (uk) 2001-09-17
BG98689A (bg) 1995-03-31
DE69232976D1 (de) 2003-04-30
PL171984B1 (pl) 1997-07-31
JP2546785B2 (ja) 1996-10-23
BR9206577A (pt) 1995-10-10
IS1745B (is) 2000-05-18
ZA927589B (en) 1994-04-05
NO308533B1 (no) 2000-09-25
US6303633B1 (en) 2001-10-16
CZ290807B6 (cs) 2002-10-16
DE69232976T2 (de) 2003-10-02
BG61727B1 (bg) 1998-04-30
US20020049210A1 (en) 2002-04-25
FI116939B (fi) 2006-04-13
DK0606248T3 (da) 2003-06-23
AU667053B2 (en) 1996-03-07
AP9200421A0 (en) 1992-10-31
HU225049B1 (en) 2006-05-29
US5574046A (en) 1996-11-12
EP0606248B1 (en) 2003-03-26
MX9205678A (es) 1993-04-01
WO1993007140A1 (en) 1993-04-15
MA22672A1 (fr) 1993-07-01
AU2519692A (en) 1993-05-03
SG52618A1 (en) 1998-09-28
PT100917A (pt) 1993-11-30
KR0170458B1 (ko) 1999-02-18
HU9400952D0 (en) 1994-06-28
US6124321A (en) 2000-09-26
NO941179D0 (no) 1994-03-30
FI941518A0 (fi) 1994-03-31
PT100917B (pt) 1999-07-30
PL171693B1 (pl) 1997-06-30
CZ78594A3 (en) 1995-07-12
HUT70544A (en) 1995-10-30
NZ244601A (en) 1995-03-28
CA2119647A1 (en) 1993-04-15
PL171669B1 (en) 1997-06-30
FI941518L (fi) 1994-03-31
IL103274A0 (en) 1993-02-21
ES2193137T3 (es) 2003-11-01
NO941179L (no) 1994-03-30
TW263504B (enExample) 1995-11-21
PH31290A (en) 1998-07-06
CN1071166A (zh) 1993-04-21
AP314A (en) 1994-02-04
EP0606248A1 (en) 1994-07-20
IS3919A (is) 1993-04-04
ATE235490T1 (de) 2003-04-15
EG21481A (en) 2001-11-28
UY23484A1 (es) 1993-03-11

Similar Documents

Publication Publication Date Title
CN1071166A (zh) 作为新的乙酰胆碱酯酶抑制剂的芳香杂环胺类
CN1273451C (zh) 哌啶mch拮抗剂及其治疗肥胖症的用途
CN1249051C (zh) 毒蕈碱性激动剂
CN1176651C (zh) N-(3-苯并呋喃基)脲衍生物
CN1098098A (zh) 哌嗪衍生物
CN1221417A (zh) 具有抗糖尿病、降低血脂、抗高血压性能的噻唑烷二酮化合物,其制备方法及其药物组合物
CN1094726A (zh) 噻唑烷二酮衍生物,它们的制备方法和用途
CN1023602C (zh) 制备抑制精神的3-哌嗪基苯并唑类衍生物的方法
CN1092766A (zh) 药物
CN1142162C (zh) 作为抗菌剂的新的双环噁唑烷酮
CN100338074C (zh) 杂环化合物和以其为有效成分的脑机能改善剂
CN1071665A (zh) 唑烷酮衍生物
CN1054600A (zh) 新的胆碱酯酶抑制剂三环—环胺
CN1017901B (zh) 抗精神病药稠环吡啶基哌嗪衍生物的制备方法
CN100335464C (zh) 芳烷基-四氢-吡啶,其制备方法及含有它们的药物组合物
CN1121715A (zh) 4-芳基-4-羟基-四氢吡喃类化合物和3-芳基-3-羟基-四氢呋喃类化合物作为5-脂氧合酶抑制剂
CN1179962C (zh) 氮杂吲哚嗪酮衍生物和以其为有效成分的脑功能改善剂
CN1311785A (zh) 作为甘氨酸拮抗剂的四氢喹啉衍生物
CN1111634A (zh) 噻吩并噻嗪衍生物
CN1823054A (zh) 咪唑衍生物ⅲ
CN1572791A (zh) 新的苯并噻嗪和苯并噻二嗪化合物,其制备方法以及包含所述化合物的药物组合物
CN1154693A (zh) 具有多巴胺能活性的苯并咪唑衍生物
CN86108467A (zh) 三环哒嗪并吡啶酮衍生物
CN1381456A (zh) 新型嘧啶-4-酮化合物、其制备方法和含有它们的药物组合物
CN1286833C (zh) 吲哚和2,3-二氢吲哚衍生物、它们的制备及用途

Legal Events

Date Code Title Description
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C06 Publication
PB01 Publication
C14 Grant of patent or utility model
GR01 Patent grant
C15 Extension of patent right duration from 15 to 20 years for appl. with date before 31.12.1992 and still valid on 11.12.2001 (patent law change 1993)
OR01 Other related matters
C19 Lapse of patent right due to non-payment of the annual fee
CF01 Termination of patent right due to non-payment of annual fee