DE60208366T2 - Substituierte azabicyclische einheiten zur krankheitsbehandlung (nikotinische acetylcholinrezeptor-antagonisten) - Google Patents
Substituierte azabicyclische einheiten zur krankheitsbehandlung (nikotinische acetylcholinrezeptor-antagonisten) Download PDFInfo
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- DE60208366T2 DE60208366T2 DE60208366T DE60208366T DE60208366T2 DE 60208366 T2 DE60208366 T2 DE 60208366T2 DE 60208366 T DE60208366 T DE 60208366T DE 60208366 T DE60208366 T DE 60208366T DE 60208366 T2 DE60208366 T2 DE 60208366T2
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- Prior art keywords
- azabicyclo
- chlorobenzamide
- mmol
- mixture
- int
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- YFTHZRPMJXBUME-UHFFFAOYSA-N tripropylamine Chemical compound CCCN(CCC)CCC YFTHZRPMJXBUME-UHFFFAOYSA-N 0.000 description 1
- 125000005500 uronium group Chemical group 0.000 description 1
- 239000003981 vehicle Substances 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
- 238000010626 work up procedure Methods 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- 229960000607 ziprasidone Drugs 0.000 description 1
- MVWVFYHBGMAFLY-UHFFFAOYSA-N ziprasidone Chemical compound C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 MVWVFYHBGMAFLY-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged 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
-
- 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
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
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)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28495001P | 2001-04-19 | 2001-04-19 | |
| US284950P | 2001-04-19 | ||
| US34890401P | 2001-10-26 | 2001-10-26 | |
| US348904P | 2001-10-26 | ||
| PCT/US2002/008268 WO2002085901A1 (en) | 2001-04-19 | 2002-04-18 | Substituted azabicyclic moieties for the treatment of disease (nicotinic acethylcholine receptor agonists) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60208366D1 DE60208366D1 (de) | 2006-02-02 |
| DE60208366T2 true DE60208366T2 (de) | 2006-07-06 |
Family
ID=26962909
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60208366T Expired - Fee Related DE60208366T2 (de) | 2001-04-19 | 2002-04-18 | Substituierte azabicyclische einheiten zur krankheitsbehandlung (nikotinische acetylcholinrezeptor-antagonisten) |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US6869946B2 (https=) |
| EP (1) | EP1389208B1 (https=) |
| JP (1) | JP2004526788A (https=) |
| AR (1) | AR035817A1 (https=) |
| AT (1) | ATE314367T1 (https=) |
| CA (1) | CA2439960A1 (https=) |
| DE (1) | DE60208366T2 (https=) |
| ES (1) | ES2254723T3 (https=) |
| MX (1) | MXPA03009644A (https=) |
| PE (1) | PE20021019A1 (https=) |
| WO (1) | WO2002085901A1 (https=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10164139A1 (de) | 2001-12-27 | 2003-07-10 | Bayer Ag | 2-Heteroarylcarbonsäureamide |
| EP1480977A2 (en) * | 2002-02-15 | 2004-12-01 | PHARMACIA & UPJOHN COMPANY | Substituted aryl compounds for treatment of disease |
| CA2476681A1 (en) | 2002-02-19 | 2003-08-28 | Bruce N. Rogers | Fused bicyclic-n-bridged-heteroaromatic carboxamides for the treatment of disease |
| GB0220581D0 (en) | 2002-09-04 | 2002-10-09 | Novartis Ag | Organic Compound |
| MXPA05003317A (es) | 2002-09-25 | 2005-07-05 | Memory Pharm Corp | Indazoles, benzotiazoles y benzoisotiazoles asi como preparacion y usos de los mismos. |
| WO2004052889A1 (en) * | 2002-12-06 | 2004-06-24 | Pharmacia & Upjohn Company Llc | Compounds as radioligands for the diagnosis of disease |
| EP1587511A2 (en) * | 2003-01-22 | 2005-10-26 | Pharmacia & Upjohn Company LLC | Treatment of diseases with alpha-7 nach receptor full agonists |
| GB0310867D0 (en) * | 2003-05-12 | 2003-06-18 | Novartis Ag | Organic compounds |
| RU2389729C2 (ru) | 2003-12-22 | 2010-05-20 | Мемори Фармасьютиклз Корпорейшн | 1н-индазолы, 1, 2-бензизоксазолы и 1, 2-бензизотиазолы, их получение и применение |
| EP1735306A2 (en) | 2004-03-25 | 2006-12-27 | Memory Pharmaceuticals Corporation | Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and uses thereof |
| US20070155780A1 (en) * | 2004-04-15 | 2007-07-05 | Hitoshi Nakata | Stabilized composition containing 4-amino-5-chloro-n-[(1r, 3r, 5s)-8-methyl-8-azabicyclo[3.2.1]oct-3-y1]-2-[1-methylbut-2-ynyloxy]benzamide |
| CA2567977A1 (en) * | 2004-04-22 | 2006-01-05 | Memory Pharmaceutical Corporation | Indoles, 1h-indazoles, 1,2-benzisoxazoles, 1,2-benzoisothiazoles, and preparation and uses thereof |
| NZ551712A (en) | 2004-05-07 | 2010-07-30 | Memory Pharm Corp | 1H-indazoles, benzothiazoles, 1,2-benzoisoxazoles, 1,2-benzoisothiazoles, and chromones and preparations and uses thereof |
| AR049401A1 (es) | 2004-06-18 | 2006-07-26 | Novartis Ag | Aza-biciclononanos |
| GB0415746D0 (en) | 2004-07-14 | 2004-08-18 | Novartis Ag | Organic compounds |
| GB0424564D0 (en) * | 2004-11-05 | 2004-12-08 | Novartis Ag | Organic compounds |
| CA2591817A1 (en) | 2004-12-22 | 2006-06-29 | Memory Pharmaceuticals Corporation | Nicotinic alpha-7 receptor ligands and preparation and uses thereof |
| US7732607B2 (en) * | 2005-08-22 | 2010-06-08 | Anatoly Mazurov | Heteroaryl-substituted diazatricycloalkanes and methods of use thereof |
| US8106066B2 (en) | 2005-09-23 | 2012-01-31 | Memory Pharmaceuticals Corporation | Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof |
| GB0521508D0 (en) | 2005-10-21 | 2005-11-30 | Novartis Ag | Organic compounds |
| GB0525673D0 (en) | 2005-12-16 | 2006-01-25 | Novartis Ag | Organic compounds |
| GB0525672D0 (en) | 2005-12-16 | 2006-01-25 | Novartis Ag | Organic compounds |
| JP5172124B2 (ja) * | 2006-09-29 | 2013-03-27 | 関東化学株式会社 | ２位に置換基を有する光学活性キヌクリジノール類の製造方法 |
| JP5232374B2 (ja) * | 2006-09-29 | 2013-07-10 | 関東化学株式会社 | ２位に置換基を有する光学活性キヌクリジノール類の製造方法 |
| WO2009146031A1 (en) | 2008-03-31 | 2009-12-03 | University Of South Florida | Methods of treating disease-induced ataxia and non-ataxic imbalance |
| JP2011520964A (ja) * | 2008-05-23 | 2011-07-21 | ユニバーシティ・オブ・サウス・フロリダ | ニコチン性アセチルコリン受容体活性を有する化合物を用いる末梢感覚神経喪失の治療方法 |
| TW201031664A (en) * | 2009-01-26 | 2010-09-01 | Targacept Inc | Preparation and therapeutic applications of (2S,3R)-N-2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)-3,5-difluorobenzamide |
| PE20170923A1 (es) | 2010-05-17 | 2017-07-12 | Forum Pharmaceuticals Inc | Una forma cristalina de clorhidrato de (r)-7-cloro-n-(quinuclidin-3-il)benzo[b]tiofeno-2-carboxamida monohidratado |
| WO2012177263A1 (en) * | 2011-06-24 | 2012-12-27 | Intra-Cellular Therapies, Inc. | Compounds and methods of prophylaxis and treatment regarding nictonic receptor antagonists |
| EP3461481A1 (en) | 2012-05-08 | 2019-04-03 | Forum Pharmaceuticals Inc. | Methods of maintaining, treating or improving cognitive function |
| EP3623371A1 (en) * | 2014-12-16 | 2020-03-18 | Axovant Sciences GmbH | Geminal substituted quinuclidine amide compounds as agonists of alpha-7 nicotinic acetylcholine receptors |
| CN109320510B (zh) * | 2018-11-27 | 2021-04-27 | 江苏慧聚药业有限公司 | 一种马罗匹坦游离碱的制备方法 |
| CN111793017B (zh) * | 2019-04-04 | 2024-01-16 | 广东东阳光药业股份有限公司 | 一种内酰胺化合物的制备方法 |
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| US3702324A (en) | 1970-06-24 | 1972-11-07 | Stanford Research Inst | 3,4,5-trimethoxybenzamides of substituted anilines and of alkylpiperidines |
| NL7611713A (nl) | 1975-11-03 | 1977-05-05 | Thomae Gmbh Dr K | Werkwijze voor de bereiding van verbindingen en preparaten met waardevolle farmacologische eigen- schappen. |
| FR2529548A1 (fr) | 1982-07-02 | 1984-01-06 | Delalande Sa | Nouveaux derives de l'amino-3 quinuclidine, leur procede et leur application en therapeutique |
| US5175173A (en) | 1983-12-22 | 1992-12-29 | Sun Jung Hui | Carboxamides useful as antiemetic or antipsychotic agents |
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| US4820715A (en) | 1984-06-28 | 1989-04-11 | Bristol-Myers Company | Anti-emetic quinuclidinyl benzamides |
| US4870181A (en) | 1985-02-04 | 1989-09-26 | A. H. Robins Company, Incorporated | Process for the preparation of 2-alkoxy-N-(1-azabicyclo[2.2.2])octan-3-yl)aminobenzamides |
| US4605652A (en) | 1985-02-04 | 1986-08-12 | A. H. Robins Company, Inc. | Method of enhancing memory or correcting memory deficiency with arylamido (and arylthioamido)-azabicycloalkanes |
| EP0201165B1 (en) | 1985-03-14 | 1994-07-20 | Beecham Group Plc | Medicaments for the treatment of emesis |
| GB8520616D0 (en) | 1985-08-16 | 1985-09-25 | Beecham Group Plc | Compounds |
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| EP0235878A3 (en) | 1986-01-16 | 1989-06-14 | Beecham Group Plc | Novel compounds |
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| HU895334D0 (en) | 1986-07-30 | 1990-01-28 | Sandoz Ag | Process for the preparation of nasal pharmaceutical compositions |
| DE3780276T2 (de) | 1986-12-16 | 1993-02-25 | Robins Co Inc A H | Angstloesende n-(1-azabicyclo(2.2.2)oct-3-yl)benzamide und -thiobenzamide. |
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| US4835162A (en) | 1987-02-12 | 1989-05-30 | Abood Leo G | Agonists and antagonists to nicotine as smoking deterents |
| DE3822792C2 (de) | 1987-07-11 | 1997-11-27 | Sandoz Ag | Neue Verwendung von 5HT¶3¶-Antagonisten |
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| AU611976B2 (en) | 1987-12-24 | 1991-06-27 | John Wyeth & Brother Limited | Aroyl urea and carbamic acid derivatives of azabicyclo compounds |
| FR2625678B1 (fr) | 1988-01-13 | 1991-06-07 | Delalande Sa | Agents anorexigenes a base de n-(quinuclidin-3-yl)-benzamides ou thiobenzamides |
| US4863919A (en) | 1988-02-01 | 1989-09-05 | A. H. Robins Company, Incorporated | Method of enhancing memory or correcting memory deficiency with arylamido(and arylthiomido)-azabicycloalkanes |
| DE3810552A1 (de) | 1988-03-29 | 1989-10-19 | Sandoz Ag | Ester und amide von indol-, benzo(b)thiopen-, benzo(b)furancarbonsaeuren oder 4-amino-2-methoxy-benzolsaeuren mit n-heterocyclischen oder n-heterobicyclischen alkoholen oder aminen, verfahren zu deren herstellung sie enthaltende pharmazeutische zusammensetzungen sowie applikator zur verabreichung derselben |
| EP0353371A1 (en) | 1988-08-04 | 1990-02-07 | Synthelabo | Memory enhancing-R-N-(1-azabicyclo[2.2.2] oct-3-yl) benzamides and thiobenzamides |
| DE3878235T2 (de) | 1988-08-04 | 1993-06-03 | Synthelabo | Antischizophren-wirksame s-n-(1-azabicyclo (2.2.2.)oct-3-yl)benzamide und thiobenzamide. |
| US4920227A (en) | 1988-11-29 | 1990-04-24 | Rorer Pharmaceutical Corp. | Benzobicyclic carboxamide 5-HT3 antagonists |
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| GB8928837D0 (en) | 1989-12-21 | 1990-02-28 | Beecham Group Plc | Pharmaceuticals |
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| US5070095A (en) | 1990-12-12 | 1991-12-03 | A. H. Robins Company, Incorporated | Substituted 4-(amidino)benzamides of 1-azabicyclo[2.2.2]octan-3- and -4-amine as gastric prokinetic, antiemetic, and anxiolytic agents |
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| US5723103A (en) | 1994-12-09 | 1998-03-03 | Vanderbilt University | Substituted benzamides and radioligand analogs and methods of use |
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| SE9600683D0 (sv) | 1996-02-23 | 1996-02-23 | Astra Ab | Azabicyclic esters of carbamic acids useful in therapy |
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| AU4980200A (en) | 1999-05-27 | 2000-12-18 | Pharmacia & Upjohn Company | Methods and compositions for measuring ion channel conductance |
| SE9903760D0 (sv) | 1999-10-18 | 1999-10-18 | Astra Ab | New compounds |
| SE9904176D0 (sv) | 1999-11-18 | 1999-11-18 | Astra Ab | New use |
| SE0000540D0 (sv) | 2000-02-18 | 2000-02-18 | Astrazeneca Ab | New compounds |
| GB0010955D0 (en) | 2000-05-05 | 2000-06-28 | Novartis Ag | Organic compounds |
-
2002
- 2002-04-05 PE PE2002000274A patent/PE20021019A1/es not_active Application Discontinuation
- 2002-04-09 AR ARP020101299A patent/AR035817A1/es unknown
- 2002-04-17 US US10/124,145 patent/US6869946B2/en not_active Expired - Fee Related
- 2002-04-18 JP JP2002583428A patent/JP2004526788A/ja not_active Withdrawn
- 2002-04-18 WO PCT/US2002/008268 patent/WO2002085901A1/en not_active Ceased
- 2002-04-18 AT AT02764140T patent/ATE314367T1/de not_active IP Right Cessation
- 2002-04-18 DE DE60208366T patent/DE60208366T2/de not_active Expired - Fee Related
- 2002-04-18 CA CA002439960A patent/CA2439960A1/en not_active Abandoned
- 2002-04-18 MX MXPA03009644A patent/MXPA03009644A/es unknown
- 2002-04-18 ES ES02764140T patent/ES2254723T3/es not_active Expired - Lifetime
- 2002-04-18 EP EP02764140A patent/EP1389208B1/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| WO2002085901A1 (en) | 2002-10-31 |
| US6869946B2 (en) | 2005-03-22 |
| CA2439960A1 (en) | 2002-10-31 |
| ES2254723T3 (es) | 2006-06-16 |
| MXPA03009644A (es) | 2004-01-29 |
| US20030055043A1 (en) | 2003-03-20 |
| AR035817A1 (es) | 2004-07-14 |
| WO2002085901A8 (en) | 2003-12-24 |
| EP1389208A1 (en) | 2004-02-18 |
| PE20021019A1 (es) | 2002-11-13 |
| JP2004526788A (ja) | 2004-09-02 |
| ATE314367T1 (de) | 2006-01-15 |
| EP1389208B1 (en) | 2005-12-28 |
| DE60208366D1 (de) | 2006-02-02 |
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| 8364 | No opposition during term of opposition | ||
| 8339 | Ceased/non-payment of the annual fee |