KR880003939A - 피페리딘 화합물과 이의 제조방법 및 용도 - Google Patents
피페리딘 화합물과 이의 제조방법 및 용도 Download PDFInfo
- 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
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic 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
- C07D413/04—Heterocyclic 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
-
- 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
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic 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
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (5)
- 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.
- 제1항에 있어서, 1-메틸-3-(3-사이클로프로필-1,2,4-옥사디아졸-5-일)-1,2,5,6-테트라하이드로피리딘인 화합물.
- (a)하기 일반식(Ⅱ)의 화합물의 반응성 유도체를 하기 일반식(Ⅲ)의 화합물과 반응시켜 R3,R4및 R5중의 하나가R'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 하나가R'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.
- 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.
- 제4항에 있어서, 1 내지 100mg의 활성 화합물을 함유하는 경구 복용 단위의 형태인 약제학적 조성물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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)
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)
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 |
-
1987
- 1987-07-21 IL IL8327587A patent/IL83275A/en unknown
- 1987-08-06 PH PH35635A patent/PH23584A/en unknown
- 1987-08-07 EP EP87111470A patent/EP0259621B1/en not_active Expired - Lifetime
- 1987-08-07 ES ES87111470T patent/ES2043624T3/es not_active Expired - Lifetime
- 1987-08-07 DE DE8787111470T patent/DE3782785T2/de not_active Expired - Fee Related
- 1987-08-07 AT AT87111470T patent/ATE82751T1/de not_active IP Right Cessation
- 1987-08-14 IE IE217387A patent/IE62485B1/en not_active IP Right Cessation
- 1987-08-26 US US07/089,747 patent/US4837241A/en not_active Expired - Lifetime
- 1987-09-02 FI FI873809A patent/FI86424C/fi not_active IP Right Cessation
- 1987-09-03 PT PT85650A patent/PT85650B/pt not_active IP Right Cessation
- 1987-09-04 NZ NZ221672A patent/NZ221672A/xx unknown
- 1987-09-07 NO NO873731A patent/NO169285C/no not_active IP Right Cessation
- 1987-09-08 AU AU78165/87A patent/AU603603B2/en not_active Ceased
- 1987-09-08 JP JP62223199A patent/JPH0662616B2/ja not_active Expired - Lifetime
- 1987-09-08 KR KR1019870009915A patent/KR950009366B1/ko not_active IP Right Cessation
- 1987-09-08 CA CA000546359A patent/CA1340937C/en not_active Expired - Fee Related
-
1988
- 1988-08-25 US US07/236,550 patent/US4933353A/en not_active Expired - Fee Related
-
1993
- 1993-02-11 GR GR930400285T patent/GR3007053T3/el unknown
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 |
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