KR950011443A - 갈란타민 유도체, 이의 제조방법 및 약제로서의 이의 용도 - Google Patents
갈란타민 유도체, 이의 제조방법 및 약제로서의 이의 용도 Download PDFInfo
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- KR950011443A KR950011443A KR1019940026303A KR19940026303A KR950011443A KR 950011443 A KR950011443 A KR 950011443A KR 1019940026303 A KR1019940026303 A KR 1019940026303A KR 19940026303 A KR19940026303 A KR 19940026303A KR 950011443 A KR950011443 A KR 950011443A
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- hydrogen
- compound
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- alkylcarbonyloxy
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
-
- 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
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/06—Peri-condensed systems
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Psychiatry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
본 출원은 콜린성 기능 감퇴에 의해 특징지워지는 기억 기능 장애를 치료하는데 유용한 하기 일반식(I)의 화합물, 당해 화합물을 함유하는 약제학적 조성물 및 당해 화합물의 제조 및 사용방법에 관한 것이다.
상기식에서, R1, R2, R3및 R4는 본 명세서에서 정의한 바와 같다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (9)
- 일반식(I)의 화합물 및 이의 모든 기하이성체, 광학이성체 및 입체이성체, 또는 약제학적으로 허용되는 이의 부가염.상기식에서, R1은 수소, (C1-C12)알킬카보닐, (C1-C12)알콕시카보닐, 모노(C1-C12)알킬아미노카보닐 또는 디(C1-C8)알킬아미노카보닐이고, R2는 수소, (C3-C12)알케닐카보닐옥시, (C3-C12)사이클로 알킬카보닐옥시, (C3-C12)사이클로알킬아미노카보닐옥시, (C3-C12)알키닐카보닐옥시, (C3-C12)사이클로알킬(C1-C12)알킬카보닐옥시, 산소 함유 헤테로사이클릴옥시, 산소 함유 헤테로사이클릴카보닐옥시, 황 함유 헤테로사이클릴옥시, 황 함유 헤테로사이클릴카보닐옥시, 질소 함유 헤테로 사이클릴옥시, 질소 함유 헤테로사이클릴카보닐옥시, 할로알킬설포닐옥시 또는 (C1-C6)알킬실릴옥시이며, R3은 수소, 할로 또는 (C1-C4)알킬이고, R4는 수소 또는 (C1-C6)알킬이며, 단 R3및 R4가 수소인 경우, R1및 R2는 둘 다 수소가 아니다.
- 제1항에 있어서, R1이 수소, (C1-C12)알킬카보닐 또는 (C1-C12)알콜시카보닐이고, R2가 수소, (C3-C12)알케닐카보닐옥시, (C3-C12)알키닐카보닐옥시, (C3-C12)사이클로알킬카보닐옥시, (C3-C12)사이클로알킬아미노카보닐옥시, (C3-C12)사이클로알킬 (C1-C12)알킬카보닐옥시, 할로(C1-C6)알킬설포닐옥시, (C1-C6)알킬실릴옥시, 피리딜옥시, 티오모르폴리노카보닐옥시, 푸라닐카보닐옥시, 티에닐카보닐옥시, 테트라하이드로푸라닐카보닐옥시, 푸라닐옥시, 티에닐옥시, 피를리디닐카보닐옥시, 테트라하이드로푸라닐옥시, 피페리디닐카보닐옥시, 아제핀카보닐옥시, 모르폴리노카보닐옥시 또는 테트라하이드로이소퀴놀리닐카보닐옥시이며, R3이 수소 또는 할로이고, R4가 수소 또는 (C1-C6)알킬이며, 단 R3및 R4가 수소인 경우 R1및 R2는 둘 다 수소가 아닌 일반식(I)의 화합물 및 이의 모든 기하이성체, 광학이성체 및 입체이성체, 또는 약제학적으로 허용되는 이의 부가염.
- 제1항에 있어서, R1이 수소, (C1-C12)알킬카보닐 또는 (C1-C12)알콕시카보닐옥시, R2가 (C3-C12)알케닐카보닐옥시, (C3-C12)알키닐카보닐옥시, (C3-C12)사이클로알킬카보닐옥시, (C3-C12)사이클로알킬(C1-C12)알킬카보닐옥시, 피리딜옥시, 푸라노일옥시, 모르폴리노카보닐옥시 또는 테트라하이드로이소퀴놀릴카보닐옥시이며, R3이 수소 또는 브롬이고, R4가 수소 또는 메틸인 일반식(I)의 화합물.
- 제3항에 있어서, R1이 수소인 일반식(I)의 화합물.
- 제4항에 있어서, R3및 R4가 수소인 일반식(I)의 화합물.
- 제항에 있어서, R2가 사이클로프로필카보닐옥시, 사이클로부틸카보닐옥시, 사이클로헥실카보닐옥시, 메틸사이클로헥실카보닐옥시, 아다만틸카보닐옥시, 아다만틸메틸카보닐옥시, 2-메틸프로페닐카보닐옥시, 2-프로피닐카보닐옥시, 사이클로헵틸아미노카보닐옥시, 사이클로헥실아미노카보닐옥시, 모르폴리노카보닐옥시 또는 테트라하이드로이소퀴놀리닐카보닐옥시인 일반식(I)의 화합물.
- 제1항에 있어서, (6-0-데메틸)-6-0-(1,2,3,4-테트라하이드로이소퀴놀린-2-일)카보닐)갈란타민 또는 약제학적으로 허용되는 이의 산 부가염인 화합물.
- 제1항에서 정의한 일반식(I)의 화합물 및 약제학적으로 허용되는 이의 산 부가염을 포함하는 약제학적 조성물.
- 콜린성 기능 감퇴에 의해 특징지워지는 기억 기능 장애의 치료에 사용하기에 유용한 약제를 제조하기 위한, 제1항에서 정의한 일반식(I)의 화합물의 용도.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US8/137,440 | 1993-10-15 | ||
US08/137,440 | 1993-10-15 | ||
US08/137,440 US6323195B1 (en) | 1993-10-15 | 1993-10-15 | Galanthamine derivatives as acetylcholinesterase inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
KR950011443A true KR950011443A (ko) | 1995-05-15 |
KR0169114B1 KR0169114B1 (ko) | 1999-01-15 |
Family
ID=22477446
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019940026303A KR0169114B1 (ko) | 1993-10-15 | 1994-10-14 | 갈라타민 유도체 및 이를 포함하는 약제학적 조성물 |
Country Status (23)
Country | Link |
---|---|
US (2) | US6323195B1 (ko) |
EP (2) | EP0653427B1 (ko) |
JP (1) | JP2664344B2 (ko) |
KR (1) | KR0169114B1 (ko) |
CN (1) | CN1039911C (ko) |
AT (1) | ATE212348T1 (ko) |
AU (1) | AU696249B2 (ko) |
CA (1) | CA2118174C (ko) |
CZ (1) | CZ287071B6 (ko) |
DE (1) | DE69429708T2 (ko) |
DK (1) | DK0653427T3 (ko) |
EG (1) | EG20472A (ko) |
ES (1) | ES2171428T3 (ko) |
FI (1) | FI108723B (ko) |
IL (1) | IL111274A (ko) |
NO (1) | NO310415B1 (ko) |
NZ (1) | NZ264683A (ko) |
PL (1) | PL177730B1 (ko) |
PT (1) | PT653427E (ko) |
RO (1) | RO114133B1 (ko) |
RU (1) | RU2114850C1 (ko) |
TW (1) | TW363969B (ko) |
ZA (1) | ZA948062B (ko) |
Families Citing this family (26)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9514821D0 (en) * | 1995-07-19 | 1995-09-20 | Sod Conseils Rech Applic | Galanthamine derivatives |
AT403803B (de) * | 1996-04-19 | 1998-05-25 | Sanochemia Ltd | Neue benzazepinderivate, diese enthaltende arzneimittel und verwendung derselben zum herstellen von arzneimitteln |
JP5558648B2 (ja) | 1998-11-23 | 2014-07-23 | デイビス、ボニー | アセチルコリンエステラーゼ阻害剤のための投与製剤 |
PT1140105E (pt) | 1998-12-24 | 2004-03-31 | Janssen Pharmaceutica Nv | Composicao de galantamina de libertacao controlada |
US8603546B2 (en) * | 1999-01-11 | 2013-12-10 | Herbaceuticals Inc. | Herbal supplement for increased muscle strength and endurance for athletes |
ATE355066T1 (de) * | 1999-01-11 | 2006-03-15 | Atanas Russinov Djananov | Nahrungszusatz aus kräutern zur steigerung der muskulären kraft und ausdauer von athleten |
WO2000059544A1 (fr) * | 1999-03-31 | 2000-10-12 | Eisai Co., Ltd. | Compositions stabilisees contenant des medicaments nootropes |
KR100502391B1 (ko) * | 1999-10-26 | 2005-07-19 | 얀센 파마슈티카 엔.브이. | 갈란타민 및 감미제를 함유하는 경구 용액 |
CA2393301A1 (en) * | 1999-12-10 | 2001-06-21 | Bonnie Davis | Analogs of galanthamine and lycoramine as modulators of nicotinic receptors |
EP1181294B1 (de) | 2000-03-31 | 2004-03-31 | Sanochemia Pharmazeutika Aktiengesellschaft | Neue derivate und analoga von galanthamin |
US20030162770A1 (en) * | 2002-02-22 | 2003-08-28 | Davis Bonnie M. | Use of modulators of nicotinic receptors for treatment of cognitive dysfunction |
US20050143350A1 (en) * | 2003-11-19 | 2005-06-30 | Seed John C. | Combination drug therapy to treat obesity |
WO2005065661A2 (en) * | 2003-12-31 | 2005-07-21 | Actavis Group Hf | Immediate, controlled and sustained release formulations of galanthamine |
WO2005065662A1 (en) * | 2003-12-31 | 2005-07-21 | Actavis Group Hf | Solid dosage formulations of galantamine |
WO2006004201A1 (ja) * | 2004-07-01 | 2006-01-12 | Eisai R & D Management Co., Ltd. | 神経再生促進剤 |
EP2316437B1 (en) * | 2005-05-13 | 2014-07-30 | Alza Corporation | Multilayer drug delivery system with barrier against reservoir material flow |
US20080188510A1 (en) * | 2005-05-23 | 2008-08-07 | Eisai R & D Management Co., Ltd. | Novel methods using zonisamide |
JP2009508903A (ja) * | 2005-09-22 | 2009-03-05 | ガラントス ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング | 認知障害を伴う疾患の治療に用いるための脳血液関門透過性が改善されたコリン作用増強剤 |
US20090253654A1 (en) | 2005-09-22 | 2009-10-08 | Galantos Pharma Gmbh | Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment |
EP1777222A1 (en) | 2005-09-22 | 2007-04-25 | Galantos Pharma GmbH | Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment |
WO2007035941A2 (en) * | 2005-09-23 | 2007-03-29 | Alza Corporation | Transdermal galantamine delivery system |
ES2463715T3 (es) | 2008-04-14 | 2014-05-29 | Neurodyn Life Sciences Inc. | Derivados de galantamina como profármacos para el tratamiento de enfermedades del cerebro humano |
MX2012000939A (es) * | 2009-07-23 | 2012-06-08 | Shire Llc | Profarmacos de peptidos y aminoacidos de galantamina y usos de los mismos. |
WO2013160728A1 (en) | 2012-04-26 | 2013-10-31 | Alma Mater Studiorum - Universita' Di Bologna | Dual targeting compounds for the treatment of alzheimer's disease |
EP3628315A1 (en) | 2018-09-28 | 2020-04-01 | Université de Caen Normandie | Combination of acetylcholinesterase inhibitor and 5-ht4 receptor agonist as neuroprotective agent in the treatment of neurodegenerative diseases |
CN113292420A (zh) * | 2021-05-27 | 2021-08-24 | 神隆医药(常熟)有限公司 | 加兰他敏中间体原料2-溴-5-羟基-4-甲氧基苯甲酸回收方法 |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
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PL122665B1 (en) | 1978-11-21 | 1982-08-31 | Edinen Zentar Chim | Process for preparing novel dienones of narvedine type and their derivatives |
US4663318A (en) | 1986-01-15 | 1987-05-05 | Bonnie Davis | Method of treating Alzheimer's disease |
US6150354A (en) * | 1987-01-15 | 2000-11-21 | Bonnie Davis | Compounds for the treatment of Alzheimer's disease |
AU632458B2 (en) * | 1987-05-04 | 1993-01-07 | Bonnie Davis | Compounds for the treatment of alzheimer's disease |
NL8800350A (nl) | 1988-02-12 | 1989-09-01 | Stichting Biomedical Research | Synthetische galanthamine-derivaten, werkwijze voor het bereiden daarvan, en farmaceutische samenstellingen. |
DK0584185T3 (da) | 1991-05-14 | 2000-02-07 | Ernir Snorrason | Behandling af træthedssyndrom med cholinesteraseinhibitorer |
US5231093A (en) * | 1991-10-01 | 1993-07-27 | Hoechst-Roussel Pharmaceuticals Incorporated | Carbamate derivatives of 4-amino-3-isoxazolidinones, 3-amino-1-hydroxypyrrolidin-2-ones and 1-amino-1-cyclopropanecarboxylic acid analogs |
US5153193A (en) | 1991-10-01 | 1992-10-06 | Hoechst-Roussel Pharmaceuticals Incorporated | Carbamate derivatives of 4-amino-3-isoxazolidinones, 3-amino-1-hydroxypyrrolidin-2-ones and 1-amino-1-cyclopropanecarboxylic acid analogs |
-
1993
- 1993-10-15 US US08/137,440 patent/US6323195B1/en not_active Expired - Lifetime
-
1994
- 1994-10-10 DE DE69429708T patent/DE69429708T2/de not_active Expired - Lifetime
- 1994-10-10 DK DK94115959T patent/DK0653427T3/da active
- 1994-10-10 EP EP94115959A patent/EP0653427B1/en not_active Expired - Lifetime
- 1994-10-10 AT AT94115959T patent/ATE212348T1/de active
- 1994-10-10 EP EP00107570A patent/EP1020470A3/en not_active Withdrawn
- 1994-10-10 PT PT94115959T patent/PT653427E/pt unknown
- 1994-10-10 ES ES94115959T patent/ES2171428T3/es not_active Expired - Lifetime
- 1994-10-13 NZ NZ264683A patent/NZ264683A/en not_active IP Right Cessation
- 1994-10-13 EG EG64194A patent/EG20472A/xx active
- 1994-10-13 IL IL11127494A patent/IL111274A/xx not_active IP Right Cessation
- 1994-10-13 RU RU94036448A patent/RU2114850C1/ru active
- 1994-10-13 FI FI944821A patent/FI108723B/fi not_active IP Right Cessation
- 1994-10-14 RO RO94-01669A patent/RO114133B1/ro unknown
- 1994-10-14 CA CA002118174A patent/CA2118174C/en not_active Expired - Lifetime
- 1994-10-14 ZA ZA948062A patent/ZA948062B/xx unknown
- 1994-10-14 NO NO19943893A patent/NO310415B1/no not_active IP Right Cessation
- 1994-10-14 PL PL94305456A patent/PL177730B1/pl unknown
- 1994-10-14 CN CN94117060A patent/CN1039911C/zh not_active Expired - Lifetime
- 1994-10-14 AU AU75814/94A patent/AU696249B2/en not_active Expired
- 1994-10-14 CZ CZ19942546A patent/CZ287071B6/cs not_active IP Right Cessation
- 1994-10-14 TW TW083109526A patent/TW363969B/zh not_active IP Right Cessation
- 1994-10-14 KR KR1019940026303A patent/KR0169114B1/ko active IP Right Grant
- 1994-10-17 JP JP6250778A patent/JP2664344B2/ja not_active Expired - Fee Related
-
1995
- 1995-05-22 US US08/445,921 patent/US5777108A/en not_active Expired - Fee Related
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