KR880003939A - 피페리딘 화합물과 이의 제조방법 및 용도 - Google Patents

피페리딘 화합물과 이의 제조방법 및 용도 Download PDF

Info

Publication number
KR880003939A
KR880003939A KR1019870009915A KR870009915A KR880003939A KR 880003939 A KR880003939 A KR 880003939A KR 1019870009915 A KR1019870009915 A KR 1019870009915A KR 870009915 A KR870009915 A KR 870009915A KR 880003939 A KR880003939 A KR 880003939A
Authority
KR
South Korea
Prior art keywords
compound
formula
alkyl
independently
pharmaceutical composition
Prior art date
Application number
KR1019870009915A
Other languages
English (en)
Other versions
KR950009366B1 (ko
Inventor
헬쓰 젠센 레이프
사우에르베르그 페르
봐트젠 프랑크
윌리암 킨틀레르 젠스
Original Assignee
노보 노르디스크 에이/에스
죄르겐 부스 라센
에이/에스 페로산
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
Priority claimed from DK426986A external-priority patent/DK426986D0/da
Priority claimed from DK597186A external-priority patent/DK597186D0/da
Application filed by 노보 노르디스크 에이/에스, 죄르겐 부스 라센, 에이/에스 페로산 filed Critical 노보 노르디스크 에이/에스
Publication of KR880003939A publication Critical patent/KR880003939A/ko
Application granted granted Critical
Publication of KR950009366B1 publication Critical patent/KR950009366B1/ko

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Cephalosporin Compounds (AREA)

Abstract

내용 없음

Description

피페리딘 화합물과 이의 제조방법 및 용도
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (5)

  1. 하기 일반식(I)의 피페리딘 화합물 및 이의 약제학적으로 허용되는 산과의 염.
    상기식에서, R3,R4, 및 R5중의 적어도 하나는또는이고, 다른 것은 독립적으로 H또는 C1-6-알킬이고 이때 R'는 H,C1-8-알킬, 페닐, 티에닐, 사이클로프로필, 또는 C1-3-알콕시메틸이며, R1및 R6는 독립적으로 H또는 C1-6-알킬이며,이다.
  2. 제1항에 있어서, 1-메틸-3-(3-사이클로프로필-1,2,4-옥사디아졸-5-일)-1,2,5,6-테트라하이드로피리딘인 화합물.
  3. (a)하기 일반식(Ⅱ)의 화합물의 반응성 유도체를 하기 일반식(Ⅲ)의 화합물과 반응시켜 R3,R4및 R5중의 하나가
    R'가 후술하는 바와 같은 일반식(I)의 화합물을 형성 시키거나, (b)하기 일반식(Ⅱ)의 화합물을 NH2OH와 반응시켜 R3,R4및 R5중의 하나가 C(=NOH)NH2이고 다른 것은 독립적으로 H또는 C1-6-알킬인 일반식(Ⅱ)화합물을 형성시키고, 이 화합물(Ⅱ)을 R'-COCl 또는 (R'-CO)2O와 반응시켜 R3, R4및 R5중의 하나가
    R'가 후술하는 바와 같은 일반식(I)의 화합물을 형성시킴을 특징으로 하는 제1항의 화합물의 제조방법.
    상기식에서, R1,R6및 R' 및은 제1항에서 정의한 바와 같으며, R3, R4및 R5중의 하나는 (a)단계에서는 CO2H 또는 에스테르와 같은 이의 반응성 유도체이고 (b)단계에서는 CN이며, 다른 것은 독립적으로 H 또는 C1-6-알킬이다.
  4. 사람을 포함하는 포유동물의 전뇌 및 해마의 인식 기능을 자극하며, 알쯔하이머 병을 치료하는데 유용한 약제학적 조성물에 있어서, 포유동물의 전뇌 및 해마의 자극 또는 알쯔하이머 병의 치료에 유효한 량의 제1항 또는 2항의 화합물과 함께 약제학적으로 허용되는 담체 또는 희석제를 함유하는 조성물.
  5. 제4항에 있어서, 1 내지 100mg의 활성 화합물을 함유하는 경구 복용 단위의 형태인 약제학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019870009915A 1986-09-08 1987-09-08 피페리딘 화합물과 이의 제조방법 및 용도 KR950009366B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DK426986A DK426986D0 (da) 1986-09-08 1986-09-08 Piperidine forbindelser, deres fremstilling og anvendelse
DK4269/86 1986-09-08
DK5971/86 1986-12-12
DK597186A DK597186D0 (da) 1986-12-12 1986-12-12 Heterocykliske forbindelser, deres fremstilling og anvendelse

Publications (2)

Publication Number Publication Date
KR880003939A true KR880003939A (ko) 1988-06-01
KR950009366B1 KR950009366B1 (ko) 1995-08-21

Family

ID=26067417

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019870009915A KR950009366B1 (ko) 1986-09-08 1987-09-08 피페리딘 화합물과 이의 제조방법 및 용도

Country Status (17)

Country Link
US (2) US4837241A (ko)
EP (1) EP0259621B1 (ko)
JP (1) JPH0662616B2 (ko)
KR (1) KR950009366B1 (ko)
AT (1) ATE82751T1 (ko)
AU (1) AU603603B2 (ko)
CA (1) CA1340937C (ko)
DE (1) DE3782785T2 (ko)
ES (1) ES2043624T3 (ko)
FI (1) FI86424C (ko)
GR (1) GR3007053T3 (ko)
IE (1) IE62485B1 (ko)
IL (1) IL83275A (ko)
NO (1) NO169285C (ko)
NZ (1) NZ221672A (ko)
PH (1) PH23584A (ko)
PT (1) PT85650B (ko)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ219646A (en) * 1986-03-27 1990-10-26 Merck Sharp & Dohme Oxadiazole derivatives of azacyclics for treating cns disorders
GB8714789D0 (en) * 1987-06-24 1987-07-29 Lundbeck & Co As H Heterocyclic compounds
IE63906B1 (en) * 1987-11-13 1995-06-14 Novo Nordisk As Azabicyclic compounds and their preparation and use
EP0322034A3 (en) * 1987-12-22 1991-01-02 Merck Sharp & Dohme Ltd. Methyl tetrahydropyridyl oxadiazoles
IL88846A0 (en) * 1988-01-08 1989-07-31 Merck Sharp & Dohme Lipophilic oxadiazoles,their preparation and pharmaceutical compositions containing them
DK162892C (da) * 1988-07-04 1992-05-11 Novo Nordisk As 1,2,5,6-tetrahydropyridinforbindelser, deres fremstilling og farmaceutiske praeparater indeholdende disse
US5328925A (en) * 1989-02-22 1994-07-12 Novo Nordisk A/S Piperidine compounds and their use
US5043345A (en) * 1989-02-22 1991-08-27 Novo Nordisk A/S Piperidine compounds and their preparation and use
US5264444A (en) * 1989-02-22 1993-11-23 Novo Nordisk A/S Piperidine compounds and use
US5260311A (en) * 1989-02-22 1993-11-09 Novo Nordisk A/S Piperidine compounds and their use
EP0459568A3 (en) * 1990-05-31 1992-09-30 Merck Sharp & Dohme Ltd. Substituted oxadiazoles and thiadiazoles for use in the treatment of glaucoma and novel compounds having such use
MX9100517A (es) * 1990-08-06 1992-04-01 Smith Kline French Lab Compuestos
DK198490D0 (da) * 1990-08-21 1990-08-21 Novo Nordisk As Heterocykliske forbindelser, deres fremstilling og anvendelse
ES2113939T3 (es) * 1990-11-29 1998-05-16 Allergan Inc Uso de derivados de piridina en el tratamiento de la hipertension ocular.
US5175166A (en) * 1991-08-27 1992-12-29 The University Of Toledo Muscarinic agonists
AU3171493A (en) * 1991-12-31 1993-07-28 Fujisawa Pharmaceutical Co., Ltd. Oxadiazole derivatives having acetylcholinesterase-inhibitory and muscarinic agonist activity
US5424301A (en) * 1993-02-01 1995-06-13 Warner-Lambert Company Starch stabilized o-substituted tetrahydropyridine oxime cholinergic agents
DE69418789T2 (de) * 1993-08-05 1999-12-02 Hoechst Marion Roussel, Inc. 2-(Piperidin-4-yl, Pyridin-4-yl und Tetrahydropyridin-4-yl)-benzofuran-7-carbamat Derivate, ihre Herstellung und Verwendung als Acetylcholinesterase Inhibitoren
US5753683A (en) * 1993-08-19 1998-05-19 Novo Nordisk A/S Antipsychotic method
US5605908A (en) * 1994-10-24 1997-02-25 Eli Lilly And Company Heterocyclic compounds and their use
US5665745A (en) * 1994-10-24 1997-09-09 Eli Lilly And Company Heterocyclic compounds and their preparation and use
US5998404A (en) * 1994-10-24 1999-12-07 Eli Lilly And Company Heterocyclic compounds and their use
US5574028A (en) * 1994-10-31 1996-11-12 Eli Lilly And Company Method for treating anxiety
US5726193A (en) * 1994-10-31 1998-03-10 Eli Lilly And Company Method for treating anxiety
US5488056A (en) * 1994-10-31 1996-01-30 Eli Lilly And Company Method for treating anxiety
ES2227836T3 (es) 1997-05-29 2005-04-01 H. Lundbeck A/S Tratamiento de esquizofrenia y psicosis.
AU2307899A (en) * 1997-12-23 1999-07-12 Alcon Laboratories, Inc. Muscarinic agents and use thereof to treat glaucoma, myopia and various other conditions
US6107313A (en) * 1998-10-02 2000-08-22 Combichem, Inc. Dopamine receptor antagonists
US7332508B2 (en) 2002-12-18 2008-02-19 Novo Nordisk A/S Substituted homopiperidine, piperidine or pyrrolidine derivatives
US20070185100A1 (en) * 2004-02-18 2007-08-09 Astrazeneca Ab Poly-heterocyclic compounds and their use as metabotropic glutamate receptor antagonists
CN1980929A (zh) * 2004-02-24 2007-06-13 比奥阿克松医疗技术股份有限公司 4-取代哌啶衍生物
US8084473B2 (en) 2007-04-24 2011-12-27 Solvay Pharmaceuticals B.V. Heterocyclic compounds with affinity to muscarinic receptors
JP2010525020A (ja) * 2007-04-24 2010-07-22 ソルベイ・フアーマシユーチカルズ・ベー・ブイ ムスカリン性受容体への親和性を有する複素環式化合物
EP2296471A4 (en) 2008-05-15 2012-03-14 Univ Toledo MUSCARIC ACID AGONISTS AS COGNITIVE ENHANCERS
US9549928B2 (en) 2011-04-29 2017-01-24 The University Of Toledo Muscarinic agonists as enhancers of cognitive flexibility
US10106525B2 (en) 2015-01-26 2018-10-23 BioAxone BioSciences, Inc. Rho kinase inhibitor BA-1049 (R) and active metabolites thereof
US10149856B2 (en) 2015-01-26 2018-12-11 BioAxone BioSciences, Inc. Treatment of cerebral cavernous malformations and cerebral aneurysms with rho kinase inhibitors
US10857157B2 (en) 2015-01-26 2020-12-08 BioAxone BioSciences, Inc. Treatment of cerebral cavernous malformations and cerebral aneurysms with rho kinase inhibitors
US11198680B2 (en) 2016-12-21 2021-12-14 BioAxone BioSciences, Inc. Rho kinase inhibitor BA-1049 (R) and active metabolites thereof
WO2019014322A1 (en) 2017-07-11 2019-01-17 BioAxone BioSciences, Inc. KINASE INHIBITORS FOR THE TREATMENT OF DISEASES
WO2020206410A1 (en) * 2019-04-04 2020-10-08 University Of Maryland, Baltimore Methods of using muscarinic antagonists in the treatment of depression

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3966748A (en) * 1975-05-08 1976-06-29 American Cyanamid Company Para-fluorophenyl-N-heterocyclic substituted butanes
US4518601A (en) * 1982-06-16 1985-05-21 Ciba Geigy Corporation 2-(3-Pyridyl)-1,3,4-oxadiazoles and use thereof in pest control
NZ219646A (en) * 1986-03-27 1990-10-26 Merck Sharp & Dohme Oxadiazole derivatives of azacyclics for treating cns disorders

Also Published As

Publication number Publication date
AU603603B2 (en) 1990-11-22
FI86424C (fi) 1992-08-25
FI873809A0 (fi) 1987-09-02
PT85650B (pt) 1990-05-31
CA1340937C (en) 2000-03-28
NO169285B (no) 1992-02-24
NZ221672A (en) 1990-09-26
IL83275A0 (en) 1987-12-31
US4933353A (en) 1990-06-12
GR3007053T3 (ko) 1993-07-30
EP0259621B1 (en) 1992-11-25
JPS6377877A (ja) 1988-04-08
FI86424B (fi) 1992-05-15
PT85650A (en) 1987-10-01
JPH0662616B2 (ja) 1994-08-17
AU7816587A (en) 1988-03-31
KR950009366B1 (ko) 1995-08-21
ATE82751T1 (de) 1992-12-15
DE3782785T2 (de) 1993-04-01
PH23584A (en) 1989-09-11
FI873809A (fi) 1988-03-09
EP0259621A2 (en) 1988-03-16
NO873731L (no) 1988-03-09
IE62485B1 (en) 1995-02-08
DE3782785D1 (de) 1993-01-07
IL83275A (en) 1994-02-27
US4837241A (en) 1989-06-06
IE872173L (en) 1989-03-08
NO169285C (no) 1992-06-03
NO873731D0 (no) 1987-09-07
EP0259621A3 (en) 1988-10-12
ES2043624T3 (es) 1994-01-01

Similar Documents

Publication Publication Date Title
KR880003939A (ko) 피페리딘 화합물과 이의 제조방법 및 용도
KR890008139A (ko) 아자사이클릭 화합물 및 이의 제조방법 및 용도
HK1017274A1 (en) Process for the preparation of pharmaceutical composition containing azasteroid compounds for the treatment of prostatic hypertrophy
KR880006193A (ko) 피페리딘 화합물 및 그의 제조 및 용도
DE68922408D1 (de) Neue Triazolopyrimidin- und Pyrazolopyrimidinderivate zur Behandlung von Kachexie.
KR910002802A (ko) 1,2,3,4-테트라히드로-9-아크리딘아민의 유도체
HUT46536A (en) Process for producing antianxietive pharmaceutical compositions
KR890011596A (ko) 불면증 치료용 의약품의 제조에 있어서 1,4-이치환-피페리디닐 화합물의 용도
KR900001693A (ko) 아자사이클릭 화합물, 이의 제조방법 및 이의 용도
KR910002835A (ko) 인돌 유도체
KR960017663A (ko) 결합 수용체 길항물질
EP0270046A3 (en) Pharmaceutical composition for treatment of cataract
AU608643B2 (en) Novel derivatives of the oxime of 1,2,5,6-tetrahydropyridin-3-carboxaldehyde, the process for their preparation, their use as medicaments and the compositions containing them
KR910021400A (ko) 옥사졸리디논
KR880011098A (ko) 4-페닐피페리딘 화합물, 이의 제조방법 및 용도
HUT54688A (en) Process for producing compounds utilizable for treating ulcus and pharmaceutical compositions containing them as active components
KR900009638A (ko) 신규 화합물들
ATE92461T1 (de) Gegen die zerebrale insuffizienz wirksame verbindungen.
ATE4541T1 (de) Alkyl- und cycloalkylsubstituierte 2-(2-(2hydroxy-3-tert.-butylamino-propoxy)-5-acylamino phenyl)-1,3,4-oxadiazole, verfahren zu ihrer herstellung und diese verbindungen enthaltende pharmazeutische zubereitungen.
IT1226277B (it) Lattami n-sostituiti
TH5602EX (th) สารประกอบทางเภสัชวิทยาชนิดใหม่
TH919A (th) การเตรียมอนุพันธ์ 1-แอลคิล-2-อะมิโน-เททราลิน

Legal Events

Date Code Title Description
A201 Request for examination
G160 Decision to publish patent application
E701 Decision to grant or registration of patent right
GRNT Written decision to grant
FPAY Annual fee payment

Payment date: 20000609

Year of fee payment: 6

LAPS Lapse due to unpaid annual fee