JP2005525385A5 - - Google Patents
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- Publication number
- JP2005525385A5 JP2005525385A5 JP2003577874A JP2003577874A JP2005525385A5 JP 2005525385 A5 JP2005525385 A5 JP 2005525385A5 JP 2003577874 A JP2003577874 A JP 2003577874A JP 2003577874 A JP2003577874 A JP 2003577874A JP 2005525385 A5 JP2005525385 A5 JP 2005525385A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrochloride
- azabicyclo
- exo
- octane
- group
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 208000002193 Pain Diseases 0.000 claims description 7
- 150000001875 compounds Chemical class 0.000 claims description 6
- 206010013663 drug dependence Diseases 0.000 claims description 6
- 208000011117 substance-related disease Diseases 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 230000004770 neurodegeneration Effects 0.000 claims description 5
- 208000030507 AIDS Diseases 0.000 claims description 3
- 208000024827 Alzheimer disease Diseases 0.000 claims description 3
- 208000019901 Anxiety disease Diseases 0.000 claims description 3
- 208000000094 Chronic Pain Diseases 0.000 claims description 3
- 208000020406 Creutzfeldt Jacob disease Diseases 0.000 claims description 3
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 claims description 3
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 claims description 3
- 206010059866 Drug resistance Diseases 0.000 claims description 3
- 208000012661 Dyskinesia Diseases 0.000 claims description 3
- 208000010412 Glaucoma Diseases 0.000 claims description 3
- 208000023105 Huntington disease Diseases 0.000 claims description 3
- 208000013016 Hypoglycemia Diseases 0.000 claims description 3
- 206010021143 Hypoxia Diseases 0.000 claims description 3
- 208000006264 Korsakoff syndrome Diseases 0.000 claims description 3
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims description 3
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims description 3
- 208000026072 Motor neurone disease Diseases 0.000 claims description 3
- 208000008238 Muscle Spasticity Diseases 0.000 claims description 3
- 208000018737 Parkinson disease Diseases 0.000 claims description 3
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims description 3
- 208000009205 Tinnitus Diseases 0.000 claims description 3
- 208000000323 Tourette Syndrome Diseases 0.000 claims description 3
- 208000016620 Tourette disease Diseases 0.000 claims description 3
- 201000004810 Vascular dementia Diseases 0.000 claims description 3
- 208000005298 acute pain Diseases 0.000 claims description 3
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 3
- 230000036506 anxiety Effects 0.000 claims description 3
- 210000003169 central nervous system Anatomy 0.000 claims description 3
- 230000001684 chronic effect Effects 0.000 claims description 3
- 206010015037 epilepsy Diseases 0.000 claims description 3
- 230000003492 excitotoxic effect Effects 0.000 claims description 3
- 231100000063 excitotoxicity Toxicity 0.000 claims description 3
- 208000007386 hepatic encephalopathy Diseases 0.000 claims description 3
- 230000002218 hypoglycaemic effect Effects 0.000 claims description 3
- 230000007954 hypoxia Effects 0.000 claims description 3
- 208000014674 injury Diseases 0.000 claims description 3
- 230000007774 longterm Effects 0.000 claims description 3
- 238000000034 method Methods 0.000 claims description 3
- 230000004065 mitochondrial dysfunction Effects 0.000 claims description 3
- 201000006417 multiple sclerosis Diseases 0.000 claims description 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 3
- 201000000980 schizophrenia Diseases 0.000 claims description 3
- 208000018198 spasticity Diseases 0.000 claims description 3
- 231100000886 tinnitus Toxicity 0.000 claims description 3
- 230000008733 trauma Effects 0.000 claims description 3
- 229910052739 hydrogen Inorganic materials 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 12
- 229940099433 NMDA receptor antagonist Drugs 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 239000003703 n methyl dextro aspartic acid receptor blocking agent Substances 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- UBAYTMLUKJFWKU-UHFFFAOYSA-N 1,3,3,5,6-pentamethyl-6-azabicyclo[3.2.1]octane Chemical compound C1C2(C)N(C)CC1(C)CC(C)(C)C2 UBAYTMLUKJFWKU-UHFFFAOYSA-N 0.000 claims 1
- KJNPYCPXGWCVRN-UHFFFAOYSA-N 1,3,3,5-tetramethyl-6-azabicyclo[3.2.1]octane Chemical compound C1C2(C)NCC1(C)CC(C)(C)C2 KJNPYCPXGWCVRN-UHFFFAOYSA-N 0.000 claims 1
- NTHBANFYFGMKNN-UHFFFAOYSA-N 5-ethyl-1,3,3-trimethyl-6-azabicyclo[3.2.1]octane Chemical compound C1C2(C)CNC1(CC)CC(C)(C)C2 NTHBANFYFGMKNN-UHFFFAOYSA-N 0.000 claims 1
- YIVWYYZYBLLGIR-UHFFFAOYSA-N 7,7,9,9-tetramethyl-1-azaspiro[4.5]decane Chemical compound C1C(C)(C)CC(C)(C)CC11NCCC1 YIVWYYZYBLLGIR-UHFFFAOYSA-N 0.000 claims 1
- AFRVUEQFUFKBNX-UHFFFAOYSA-N 8,10,10-trimethyl-6-azatricyclo[6.3.1.01,6]dodecane Chemical compound C1N2CCCCC22CC1(C)CC(C)(C)C2 AFRVUEQFUFKBNX-UHFFFAOYSA-N 0.000 claims 1
- GDSLUJLJBCXFRY-UHFFFAOYSA-N 8,8,10,10-tetramethyl-1-azaspiro[5.5]undecane Chemical compound C1C(C)(C)CC(C)(C)CC11NCCCC1 GDSLUJLJBCXFRY-UHFFFAOYSA-N 0.000 claims 1
- 201000006474 Brain Ischemia Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000001089 Multiple system atrophy Diseases 0.000 claims 1
- 229940127523 NMDA Receptor Antagonists Drugs 0.000 claims 1
- 201000008485 Wernicke-Korsakoff syndrome Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 1
- 208000031237 olivopontocerebellar atrophy Diseases 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 4
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 description 2
- 206010008027 Cerebellar atrophy Diseases 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 description 2
- 240000007817 Olea europaea Species 0.000 description 2
- 229940049706 benzodiazepine Drugs 0.000 description 2
- 150000001557 benzodiazepines Chemical class 0.000 description 2
- 229960003920 cocaine Drugs 0.000 description 2
- 208000028867 ischemia Diseases 0.000 description 2
- 208000005264 motor neuron disease Diseases 0.000 description 2
- 229960002715 nicotine Drugs 0.000 description 2
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 description 2
- 229940005483 opioid analgesics Drugs 0.000 description 2
- 229920006395 saturated elastomer Polymers 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36638602P | 2002-03-21 | 2002-03-21 | |
| PCT/GB2003/001236 WO2003080046A1 (en) | 2002-03-21 | 2003-03-21 | Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexane nmda, 5ht3, and neuronal nicotinic receptor antagoni sts |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005525385A JP2005525385A (ja) | 2005-08-25 |
| JP2005525385A5 true JP2005525385A5 (https=) | 2009-01-15 |
| JP4262606B2 JP4262606B2 (ja) | 2009-05-13 |
Family
ID=28454794
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003577874A Expired - Fee Related JP4262606B2 (ja) | 2002-03-21 | 2003-03-21 | Nmda、5ht3及び神経性ニコチンレセプターアンタゴニストとしてのアミノシクロヘキサンのアザ二環状、アザ三環状及びアザスピロ環状誘導体 |
Country Status (19)
| Country | Link |
|---|---|
| US (4) | US7022729B2 (https=) |
| EP (1) | EP1485086A1 (https=) |
| JP (1) | JP4262606B2 (https=) |
| KR (1) | KR100741257B1 (https=) |
| CN (1) | CN1638762A (https=) |
| AR (1) | AR039008A1 (https=) |
| AU (1) | AU2003216855B2 (https=) |
| CA (1) | CA2474637A1 (https=) |
| CO (1) | CO5611104A2 (https=) |
| EA (1) | EA007098B1 (https=) |
| GE (1) | GEP20063954B (https=) |
| IL (1) | IL164041A0 (https=) |
| MX (1) | MXPA04007755A (https=) |
| NO (1) | NO20044481L (https=) |
| PL (1) | PL372701A1 (https=) |
| TW (1) | TW200306189A (https=) |
| UA (1) | UA77778C2 (https=) |
| WO (1) | WO2003080046A1 (https=) |
| ZA (1) | ZA200406940B (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2483126T3 (es) | 2004-06-17 | 2014-08-05 | Merz Pharma Gmbh & Co. Kgaa | Formulaciones de formas de dosificación de neramexano |
| US20060205822A1 (en) * | 2004-12-22 | 2006-09-14 | Forest Laboratories, Inc. | 1-Aminocyclohexane derivatives for the treatment of multiple sclerosis, emotional lability and pseudobulbar affect |
| EP2111858A1 (en) | 2008-04-25 | 2009-10-28 | EPFL Ecole Polytechnique Fédérale de Lausanne | Novel treatment for alzheimer's disease |
| US20090275597A1 (en) * | 2008-05-02 | 2009-11-05 | Forest Laboratories Holdings Limited | Methods of treating cns disorders |
| PE20130775A1 (es) * | 2010-05-27 | 2013-07-21 | Targacept Inc | Antagonistas no competitivos de receptores nicotinicos |
| RU2014122338A (ru) * | 2011-11-03 | 2015-12-10 | Таргасепт, Инк. | Неконкурентные модуляторы никотиновых рецепторов |
| JP6095122B2 (ja) * | 2012-01-25 | 2017-03-15 | 国立大学法人東北大学 | 脳機能改善剤 |
| PE20151727A1 (es) | 2013-03-14 | 2015-12-17 | Boehringer Ingelheim Int | Acido 2-aza-biciclo[2.2.1]heptano-3-carboxilico (bencil-ciano-metil)-amidas sustituidas inhibidores de catepsina c |
| KR102510588B1 (ko) | 2014-09-12 | 2023-03-17 | 베링거 인겔하임 인터내셔날 게엠베하 | 카텝신 c의 스피로사이클릭 억제제 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1153973A (en) * | 1966-03-14 | 1969-06-04 | Upjohn Co | alpha,alpha-Diphenyl-beta-Methyl-1-Azaspiro[4,5]Decane (and [4,4]Nonane)-1-Propanols |
| GB1472334A (en) * | 1973-07-14 | 1977-05-04 | Tanabe Seiyaku Co | 1-3-hydroxyphenyl-6-azabicyclo-3,2,1-octane derivatives and their use in pharmaceutical preparations |
| FR2451368A1 (fr) * | 1979-03-12 | 1980-10-10 | Lilly Co Eli | Phenylmorphanes, intermediaires et procedes de synthese, et leur utilisation therapeutique |
| DE3132020A1 (de) * | 1981-08-13 | 1983-03-03 | Basf Ag, 6700 Ludwigshafen | N-benzoyl-n'-phenylharnstoffe, verfahren zu ihrer herstellung und ihre verwendung zur bekaempfung von insekten und spinnentieren |
| JPS62297848A (ja) * | 1986-06-17 | 1987-12-25 | Konica Corp | ハロゲン化銀写真感光材料 |
| AU1161292A (en) | 1991-01-09 | 1992-08-17 | Smithkline Beecham Plc | Azabicydic and azatricydic derivatives, process and intermediates for their preparation and pharmaceutical compositions containing them |
| JP3134952B2 (ja) * | 1991-09-18 | 2001-02-13 | 東洋紡績株式会社 | 難撚性ポリエステル樹脂組成物の製造方法 |
| FR2693462B1 (fr) * | 1992-07-08 | 1994-09-30 | Cepbepe | Préparation de nouveaux dérivés amido-alcools et leurs applications en thérapeutique. |
| WO1994008964A1 (fr) * | 1992-10-16 | 1994-04-28 | Asahi Kasei Kogyo Kabushiki Kaisha | Derive de n-phenethylazepine et son utilisation |
| KR100224961B1 (ko) | 1994-08-18 | 1999-10-15 | 디. 제이. 우드 | 신경보호성 3-(피페리디닐-1)-크로만-4,7-디올 및 1-(4-하이드로페닐)-2-(피페리디닐-1)-알칸올 유도체 |
| JPH11512444A (ja) * | 1995-09-22 | 1999-10-26 | ノボ ノルディスク アクティーゼルスカブ | 新規置換アザ環式またはアザ二環式化合物 |
| US5900227A (en) * | 1996-06-17 | 1999-05-04 | Oklahoma Medical Research Foundation | Multicyclic nitrone spin trapping compositions |
| JP2002531456A (ja) * | 1998-11-27 | 2002-09-24 | ニューロサーチ、アクティーゼルスカブ | 8−アザビシクロ〔3.2.1〕オクト−2−エン及び−オクタン誘導体 |
| TW593223B (en) | 2000-06-20 | 2004-06-21 | Merz Pharma Gmbh & Co Kgaa | 1-amino-alkylcyclohexanes as 5-HT3 and neuronal nicotinic receptor antagonists |
| US6951961B2 (en) * | 2002-05-17 | 2005-10-04 | Marina Nikolaevna Protopopova | Methods of use and compositions for the diagnosis and treatment of infectious disease |
-
2003
- 2003-03-17 TW TW092105796A patent/TW200306189A/zh unknown
- 2003-03-18 AR ARP030100948A patent/AR039008A1/es unknown
- 2003-03-21 GE GEAP8454A patent/GEP20063954B/en unknown
- 2003-03-21 AU AU2003216855A patent/AU2003216855B2/en not_active Ceased
- 2003-03-21 MX MXPA04007755A patent/MXPA04007755A/es not_active Application Discontinuation
- 2003-03-21 UA UA20041008550A patent/UA77778C2/uk unknown
- 2003-03-21 JP JP2003577874A patent/JP4262606B2/ja not_active Expired - Fee Related
- 2003-03-21 US US10/394,670 patent/US7022729B2/en not_active Expired - Fee Related
- 2003-03-21 EP EP03712394A patent/EP1485086A1/en not_active Withdrawn
- 2003-03-21 CN CNA038044900A patent/CN1638762A/zh active Pending
- 2003-03-21 PL PL03372701A patent/PL372701A1/xx not_active Application Discontinuation
- 2003-03-21 KR KR1020047011982A patent/KR100741257B1/ko not_active Expired - Fee Related
- 2003-03-21 WO PCT/GB2003/001236 patent/WO2003080046A1/en not_active Ceased
- 2003-03-21 IL IL16404103A patent/IL164041A0/xx unknown
- 2003-03-21 CA CA002474637A patent/CA2474637A1/en not_active Abandoned
- 2003-03-21 EA EA200401230A patent/EA007098B1/ru unknown
-
2004
- 2004-08-31 ZA ZA200406940A patent/ZA200406940B/en unknown
- 2004-08-31 CO CO04085290A patent/CO5611104A2/es not_active Application Discontinuation
- 2004-10-20 NO NO20044481A patent/NO20044481L/no not_active Application Discontinuation
-
2005
- 2005-08-11 US US11/202,012 patent/US7238703B2/en not_active Expired - Fee Related
- 2005-08-11 US US11/202,115 patent/US20060019983A1/en not_active Abandoned
-
2007
- 2007-04-04 US US11/732,764 patent/US20070185151A1/en not_active Abandoned
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