RU2002131886A - Азабициклические карбаматы и их применение в качестве агонистов альфа-7 никотинового ацетилхолинового рецептора - Google Patents
Азабициклические карбаматы и их применение в качестве агонистов альфа-7 никотинового ацетилхолинового рецептора Download PDFInfo
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- RU2002131886A RU2002131886A RU2002131886/04A RU2002131886A RU2002131886A RU 2002131886 A RU2002131886 A RU 2002131886A RU 2002131886/04 A RU2002131886/04 A RU 2002131886/04A RU 2002131886 A RU2002131886 A RU 2002131886A RU 2002131886 A RU2002131886 A RU 2002131886A
- Authority
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- Prior art keywords
- free base
- acid addition
- addition salt
- compound
- formula
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- POPPVIRYGJQIOF-UHFFFAOYSA-N 2-acetyloxyethyl(trimethyl)azanium;3-(1-methylpyrrolidin-2-yl)pyridine Chemical compound CC(=O)OCC[N+](C)(C)C.CN1CCCC1C1=CC=CN=C1 POPPVIRYGJQIOF-UHFFFAOYSA-N 0.000 title 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 title 1
- 108010009685 Cholinergic Receptors Proteins 0.000 title 1
- 102000034337 acetylcholine receptors Human genes 0.000 title 1
- 239000000556 agonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 14
- 239000002253 acid Substances 0.000 claims 12
- 239000012458 free base Substances 0.000 claims 12
- 208000028017 Psychotic disease Diseases 0.000 claims 4
- 230000004770 neurodegeneration Effects 0.000 claims 4
- 208000015122 neurodegenerative disease Diseases 0.000 claims 4
- -1 1- (2-fluorophenyl) ethyl Chemical group 0.000 claims 3
- FZCCWBIUMZOAMX-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-3-ylcarbamic acid Chemical compound C1CC2C(NC(=O)O)CN1CC2 FZCCWBIUMZOAMX-UHFFFAOYSA-N 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- PFKFTWBEEFSNDU-UHFFFAOYSA-N carbonyldiimidazole Chemical compound C1=CN=CN1C(=O)N1C=CN=C1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 238000002844 melting Methods 0.000 claims 2
- 230000008018 melting Effects 0.000 claims 2
- 239000008177 pharmaceutical agent Substances 0.000 claims 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- PFYXSUNOLOJMDX-UHFFFAOYSA-N bis(2,5-dioxopyrrolidin-1-yl) carbonate Chemical compound O=C1CCC(=O)N1OC(=O)ON1C(=O)CCC1=O PFYXSUNOLOJMDX-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000008024 pharmaceutical diluent Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Classifications
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0010955.3 | 2000-05-05 | ||
| GBGB0010955.3A GB0010955D0 (en) | 2000-05-05 | 2000-05-05 | Organic compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2002131886A true RU2002131886A (ru) | 2004-04-10 |
Family
ID=9891092
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2002131886/04A RU2002131886A (ru) | 2000-05-05 | 2001-05-03 | Азабициклические карбаматы и их применение в качестве агонистов альфа-7 никотинового ацетилхолинового рецептора |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US6780861B2 (https=) |
| EP (1) | EP1282620B1 (https=) |
| JP (1) | JP4898062B2 (https=) |
| KR (1) | KR20020093974A (https=) |
| CN (1) | CN1167703C (https=) |
| AR (1) | AR028073A1 (https=) |
| AT (1) | ATE263167T1 (https=) |
| AU (2) | AU2001262257B2 (https=) |
| BR (1) | BR0110521A (https=) |
| CA (1) | CA2407972C (https=) |
| CZ (1) | CZ20023622A3 (https=) |
| DE (1) | DE60102581T2 (https=) |
| DK (1) | DK1282620T3 (https=) |
| ES (1) | ES2218418T3 (https=) |
| GB (1) | GB0010955D0 (https=) |
| HK (1) | HK1054223B (https=) |
| HU (1) | HUP0301866A2 (https=) |
| IL (1) | IL152417A0 (https=) |
| MX (1) | MXPA02010892A (https=) |
| NO (1) | NO20025280D0 (https=) |
| NZ (1) | NZ522226A (https=) |
| PE (1) | PE20020221A1 (https=) |
| PL (1) | PL357435A1 (https=) |
| PT (1) | PT1282620E (https=) |
| RU (1) | RU2002131886A (https=) |
| SK (1) | SK15612002A3 (https=) |
| TR (1) | TR200401007T4 (https=) |
| WO (1) | WO2001085727A1 (https=) |
| ZA (1) | ZA200208969B (https=) |
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| PE20021019A1 (es) * | 2001-04-19 | 2002-11-13 | Upjohn Co | Grupos azabiciclicos sustituidos |
| MXPA04003524A (es) * | 2001-11-02 | 2004-07-23 | Searle Llc | Compuestos de benzotiepina monofluorados y difluorados novedosos como inhibidores de transporte de acido biliar co-dependiente de sodio apical (asbt) y captacion de taurocolato. |
| DE10164139A1 (de) | 2001-12-27 | 2003-07-10 | Bayer Ag | 2-Heteroarylcarbonsäureamide |
| US6852716B2 (en) * | 2002-02-15 | 2005-02-08 | Pfizer Inc | Substituted-aryl compounds for treatment of disease |
| AU2003217275A1 (en) * | 2002-02-19 | 2003-09-09 | Pharmacia And Upjohn Company | Azabicyclic compounds for the treatment of disease |
| DE10234424A1 (de) * | 2002-07-29 | 2004-02-12 | Bayer Ag | Benzothiophen-, Benzofuran- und Indolharnstoffe |
| 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. |
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| WO2004085433A2 (en) * | 2003-03-28 | 2004-10-07 | Pharmacia & Upjohn Company Llc | Positive allosteric modulators of the nicotinic acetylcholine receptor |
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| US20050170360A1 (en) * | 2004-01-30 | 2005-08-04 | Papke Roger L. | Variant neuronal nicotinic alpha-7 receptor and methods of use |
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| WO2006001894A1 (en) * | 2004-04-22 | 2006-01-05 | Memory Pharmaceutical Corporation | Indoles, 1h-indazoles, 1,2-benzisoxazoles, 1,2-benzoisothiazoles, and preparation and uses thereof |
| JP2007538011A (ja) * | 2004-05-07 | 2007-12-27 | メモリー・ファーマシューティカルズ・コーポレイション | １ｈ−インダゾール、ベンゾチアゾール、１，２−ベンゾイソキサゾール、１，２−ベンゾイソチアゾール、およびクロモン、ならびにそれらの調製および使用 |
| PE20060437A1 (es) | 2004-06-18 | 2006-06-08 | Novartis Ag | COMPUESTOS AZA-BICICLONONANOS COMO LIGANDOS COLINERGICOS DE nAChR |
| GB0415746D0 (en) | 2004-07-14 | 2004-08-18 | Novartis Ag | Organic compounds |
| GB0424564D0 (en) * | 2004-11-05 | 2004-12-08 | Novartis Ag | Organic compounds |
| RU2418797C2 (ru) | 2004-12-22 | 2011-05-20 | Мемори Фармасьютиклз Корпорейшн | Лиганды никотинового рецептора альфа-7, их получение и применение |
| US8106066B2 (en) | 2005-09-23 | 2012-01-31 | Memory Pharmaceuticals Corporation | Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof |
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| GB0525672D0 (en) | 2005-12-16 | 2006-01-25 | Novartis Ag | Organic compounds |
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| KR20180011888A (ko) | 2008-11-19 | 2018-02-02 | 포럼 파마슈티칼즈 인크. | (ｒ)-７-클로로-ｎ-(퀴누클리딘-３-일)벤조［ｂ］티오펜-２-카르복사미드 및 그 약학적으로 허용가능한 염을 이용한 인지 장애의 치료 |
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| SE9600683D0 (sv) | 1996-02-23 | 1996-02-23 | Astra Ab | Azabicyclic esters of carbamic acids useful in therapy |
| DE69727679T2 (de) * | 1996-06-05 | 2004-07-22 | Lindner, Wolfgang, Prof. Dr. | Auf cinchonan basierte chirale selektoren zur trennung von stereoisomeren |
| US6624173B1 (en) * | 1997-06-30 | 2003-09-23 | Targacept, Inc. | Pharmaceutical compositions for treating and/or preventing CNS disorders |
| US6525065B1 (en) * | 1997-06-30 | 2003-02-25 | Targacept, Inc. | Pharmaceutical compositions and methods for effecting dopamine release |
| US5988429A (en) * | 1997-10-14 | 1999-11-23 | Pharmadesign, Inc. | Blister pack pill dispenser |
| ES2252063T3 (es) * | 1999-09-28 | 2006-05-16 | Eisai Co., Ltd. | Compuesto de quinuclidina y medicamento que comprende el compuesto como principio activo. |
| US6479510B2 (en) * | 2000-08-18 | 2002-11-12 | Pharmacia & Upjohn Company | Quinuclidine-substituted aryl compounds for treatment of disease |
| GB0109871D0 (en) * | 2001-04-20 | 2001-06-13 | Glaxo Group Ltd | Metering method for particulate material |
-
2000
- 2000-05-05 GB GBGB0010955.3A patent/GB0010955D0/en not_active Ceased
-
2001
- 2001-05-03 BR BR0110521-3A patent/BR0110521A/pt not_active Application Discontinuation
- 2001-05-03 HK HK03104830.3A patent/HK1054223B/en not_active IP Right Cessation
- 2001-05-03 PT PT01936319T patent/PT1282620E/pt unknown
- 2001-05-03 US US10/258,920 patent/US6780861B2/en not_active Expired - Fee Related
- 2001-05-03 RU RU2002131886/04A patent/RU2002131886A/ru not_active Application Discontinuation
- 2001-05-03 WO PCT/EP2001/005008 patent/WO2001085727A1/en not_active Ceased
- 2001-05-03 EP EP01936319A patent/EP1282620B1/en not_active Expired - Lifetime
- 2001-05-03 MX MXPA02010892A patent/MXPA02010892A/es unknown
- 2001-05-03 JP JP2001582328A patent/JP4898062B2/ja not_active Expired - Fee Related
- 2001-05-03 KR KR1020027014760A patent/KR20020093974A/ko not_active Withdrawn
- 2001-05-03 AR ARP010102089A patent/AR028073A1/es not_active Application Discontinuation
- 2001-05-03 DE DE60102581T patent/DE60102581T2/de not_active Expired - Lifetime
- 2001-05-03 PE PE2001000399A patent/PE20020221A1/es not_active Application Discontinuation
- 2001-05-03 PL PL01357435A patent/PL357435A1/xx not_active Application Discontinuation
- 2001-05-03 CZ CZ20023622A patent/CZ20023622A3/cs unknown
- 2001-05-03 ES ES01936319T patent/ES2218418T3/es not_active Expired - Lifetime
- 2001-05-03 AU AU2001262257A patent/AU2001262257B2/en not_active Ceased
- 2001-05-03 SK SK1561-2002A patent/SK15612002A3/sk unknown
- 2001-05-03 NZ NZ522226A patent/NZ522226A/en unknown
- 2001-05-03 CN CNB01808821XA patent/CN1167703C/zh not_active Expired - Fee Related
- 2001-05-03 TR TR2004/01007T patent/TR200401007T4/xx unknown
- 2001-05-03 HU HU0301866A patent/HUP0301866A2/hu unknown
- 2001-05-03 AT AT01936319T patent/ATE263167T1/de active
- 2001-05-03 AU AU6225701A patent/AU6225701A/xx active Pending
- 2001-05-03 DK DK01936319T patent/DK1282620T3/da active
- 2001-05-03 CA CA002407972A patent/CA2407972C/en not_active Expired - Fee Related
- 2001-05-03 IL IL15241701A patent/IL152417A0/xx unknown
-
2002
- 2002-11-04 NO NO20025280A patent/NO20025280D0/no not_active Application Discontinuation
- 2002-11-05 ZA ZA200208969A patent/ZA200208969B/en unknown
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| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
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