JP2004524292A5 - - Google Patents
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- JP2004524292A5 JP2004524292A5 JP2002556156A JP2002556156A JP2004524292A5 JP 2004524292 A5 JP2004524292 A5 JP 2004524292A5 JP 2002556156 A JP2002556156 A JP 2002556156A JP 2002556156 A JP2002556156 A JP 2002556156A JP 2004524292 A5 JP2004524292 A5 JP 2004524292A5
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- JP
- Japan
- Prior art keywords
- compound
- formula
- pharmaceutically acceptable
- pharmaceutical formulation
- acceptable salt
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 10
- 239000011780 sodium chloride Substances 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000000825 pharmaceutical preparation Substances 0.000 claims 5
- 208000009025 Nervous System Disease Diseases 0.000 claims 4
- 206010029305 Neurological disorder Diseases 0.000 claims 4
- 206010037175 Psychiatric disease Diseases 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 229940079593 drugs Drugs 0.000 claims 3
- ZFGOYLVAXSSNIR-UHFFFAOYSA-N 1-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid;hydrochloride Chemical compound Cl.OC(=O)C1C2(N)C1CCC2C(O)=O ZFGOYLVAXSSNIR-UHFFFAOYSA-N 0.000 claims 2
- 206010002855 Anxiety Diseases 0.000 claims 2
- 206010057666 Anxiety disease Diseases 0.000 claims 2
- 206010059866 Drug resistance Diseases 0.000 claims 2
- 206010013754 Drug withdrawal syndrome Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 150000001450 anions Chemical class 0.000 claims 2
- 230000036506 anxiety Effects 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 230000002461 excitatory amino acid Effects 0.000 claims 2
- 239000003257 excitatory amino acid Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 230000001105 regulatory Effects 0.000 claims 2
- 230000005586 smoking cessation Effects 0.000 claims 2
- 230000005062 synaptic transmission Effects 0.000 claims 2
- 206010000565 Acquired immunodeficiency syndrome Diseases 0.000 claims 1
- 206010001897 Alzheimer's disease Diseases 0.000 claims 1
- 206010002026 Amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 206010003736 Attention deficit/hyperactivity disease Diseases 0.000 claims 1
- 206010004938 Bipolar disease Diseases 0.000 claims 1
- 208000006752 Brain Edema Diseases 0.000 claims 1
- 206010048962 Brain oedema Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010057668 Cognitive disease Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 208000008208 Craniocerebral Trauma Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000001187 Dyskinesias Diseases 0.000 claims 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims 1
- 102000018899 Glutamate Receptors Human genes 0.000 claims 1
- 108010027915 Glutamate Receptors Proteins 0.000 claims 1
- 201000001971 Huntington's disease Diseases 0.000 claims 1
- 206010021143 Hypoxia Diseases 0.000 claims 1
- 102000006541 Ionotropic Glutamate Receptors Human genes 0.000 claims 1
- 108010008812 Ionotropic Glutamate Receptors Proteins 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 206010027599 Migraine Diseases 0.000 claims 1
- 208000008085 Migraine Disorders Diseases 0.000 claims 1
- 206010028334 Muscle spasms Diseases 0.000 claims 1
- 206010052639 Nerve injury Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010061536 Parkinson's disease Diseases 0.000 claims 1
- 206010061920 Psychotic disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 206010038932 Retinopathy Diseases 0.000 claims 1
- 206010040984 Sleep disease Diseases 0.000 claims 1
- 208000005392 Spasm Diseases 0.000 claims 1
- 208000008513 Spinal Cord Injury Diseases 0.000 claims 1
- 208000000323 Tourette Syndrome Diseases 0.000 claims 1
- 206010044126 Tourette's disease Diseases 0.000 claims 1
- 206010046543 Urinary incontinence Diseases 0.000 claims 1
- 206010047700 Vomiting Diseases 0.000 claims 1
- 230000002378 acidificating Effects 0.000 claims 1
- -1 amino-bicyclo [3.1.0] hexane-2,6-dicarboxylic acid methanesulfonate Chemical compound 0.000 claims 1
- 201000006287 attention deficit hyperactivity disease Diseases 0.000 claims 1
- 201000006474 brain ischemia Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 230000002490 cerebral Effects 0.000 claims 1
- 230000036461 convulsion Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 231100000040 eye damage Toxicity 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 230000002218 hypoglycaemic Effects 0.000 claims 1
- 230000001146 hypoxic Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000002503 metabolic Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000008430 obsessive-compulsive disease Diseases 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
Claims (22)
- 製薬上許容されるアニオンを提供する酸を用いて作製された酸付加塩である、または、酸性部分を含有する化合物に関しては、製薬上許容されるアニオンを提供する塩基を用いて作製された塩である、請求項1に記載の式Iの化合物の製薬上許容される塩。
- (1S,2S,5R,6S)−2−[(2’S)−(2’−アミノ)−プロピオニル]アミノ−ビシクロ[3.1.0]ヘキサン−2,6−ジカルボン酸塩酸塩である、請求項2に記載の式Iの化合物の製薬上許容される塩。
- (1S,2S,5R,6S)−2−[(2’S)−(2’−アミノ)−プロピオニル]アミノ−ビシクロ[3.1.0]ヘキサン−2,6−ジカルボン酸メタンスルホン酸塩である、請求項2に記載の式Iの化合物の製薬上許容される塩。
- 製薬上許容されるキャリア、希釈剤または賦形剤と組合せて、請求項1〜4のいずれか1項に記載の式Iの化合物(またはその製薬上許容される塩)を含有する医薬製剤。
- 調節された興奮性アミノ酸神経伝達を必要とする患者におけるcAMP関連代謝チャネル型グルタミン酸受容体に影響を与えるための医薬製剤であって、請求項1〜4のいずれか1項に記載の化合物を薬学的に有効な量で含む医薬製剤。
- 興奮性アミノ酸神経伝達を調節するための医薬製剤であって、請求項1〜4のいずれか1項に記載の化合物を薬学的に有効な量で含む医薬製剤。
- 患者における神経学的な障害を治療するための医薬製剤であって、請求項1〜4のいずれか1項に記載の化合物を薬学的に有効な量で含む医薬製剤。
- 前記神経学的な障害が、心臓バイパス手術および移植の結果として生じる大脳欠損、大脳虚血、脊髄外傷、頭部外傷、アルツハイマー病、ハンティングトン舞踏病、筋萎縮性側索硬化症、AIDS誘発性痴呆、周産期低酸素症、低血糖性神経損傷、目の損傷および網膜症、認知障害、特発性および薬物誘発性パーキンソン病、筋肉痙攣、偏頭痛、尿失禁、薬物耐性、退薬症状および薬物停止、喫煙停止、嘔吐、脳浮腫、慢性疼痛、睡眠障害、痙攣、トゥーレット症候群、注意欠損障害、または遅発性ジスキネジアである、請求項9に記載の医薬製剤。
- 前記神経学的な障害が、薬物耐性、退薬症状及び薬物停止または喫煙停止である、請求項10に記載の医薬製剤。
- 患者における精神医学的障害を治療するための医薬製剤であって、請求項1〜4のいずれか1項に記載の化合物を薬学的に有効な量で含む医薬製剤。
- 前記精神医学的障害が精神分裂病、不安および関連障害、うつ病、双極性障害、精神病または強迫性障害である、請求項12に記載の医薬製剤。
- 前記精神医学的障害が不安および関連障害である、請求項13に記載の医薬製剤。
- Rmがtert−ブトキシカルボニルであり、R11がCO2R14であり、R13およびR14が両方ともメチルであり、R12が水素である、請求項15に記載の、式IVの化合物。
- 医薬としての使用のための、請求項1〜4のいずれか1つに記載の、式Iの新規な化合物またはその製薬上許容される塩。
- 神経学的または精神医学的障害の治療のための、医薬の製造用の、式Iの化合物またはその製薬上許容される塩の使用。
- 実施例に関して、明細書中に実質的に記載されている、式Iの新規な化合物。
- 哺乳動物におけるcAMP関連代謝チャネル型グルタミン酸受容体に影響を与えるための医薬製剤であって、実施例のいずれかに関して明細書中に実質的に記載されている式Iの化合物を薬学的に有効な量で含む医薬製剤。
- 実施例のいずれかに関して明細書中に実質的に記載されている、式Iの新規な化合物の製造方法。
- (1S,2S,5R,6S)−2−[(2’S)−(2’−アミノ)−プロピオニル]アミノ−ビシクロ[3.1.0]ヘキサン−2,6−ジカルボン酸塩酸塩である、化合物。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP01500007 | 2001-01-11 | ||
EP01500206 | 2001-08-02 | ||
US32978601P | 2001-10-16 | 2001-10-16 | |
EP01500263A EP1310480A1 (en) | 2001-11-07 | 2001-11-07 | Prodrugs of excitatory amino acids |
PCT/US2001/045866 WO2002055481A1 (en) | 2001-01-11 | 2001-12-21 | Prodrugs of excitatory amino acids |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2004524292A JP2004524292A (ja) | 2004-08-12 |
JP2004524292A5 true JP2004524292A5 (ja) | 2006-08-17 |
JP4064237B2 JP4064237B2 (ja) | 2008-03-19 |
Family
ID=27440162
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2002556156A Expired - Fee Related JP4064237B2 (ja) | 2001-01-11 | 2001-12-21 | 興奮性アミノ酸のプロドラッグ |
Country Status (24)
Country | Link |
---|---|
US (1) | US7256217B2 (ja) |
EP (1) | EP1368304B1 (ja) |
JP (1) | JP4064237B2 (ja) |
KR (1) | KR20030090622A (ja) |
CN (1) | CN1267407C (ja) |
AR (1) | AR036007A1 (ja) |
AT (1) | ATE356111T1 (ja) |
AU (1) | AU2002228737B2 (ja) |
BR (1) | BR0116770A (ja) |
CA (1) | CA2433667C (ja) |
CZ (1) | CZ303490B6 (ja) |
DE (1) | DE60127182T2 (ja) |
DZ (1) | DZ3461A1 (ja) |
ES (1) | ES2282315T3 (ja) |
HU (1) | HUP0400620A3 (ja) |
IL (1) | IL156364A0 (ja) |
MX (1) | MXPA03006186A (ja) |
NO (1) | NO20033166L (ja) |
NZ (1) | NZ526050A (ja) |
PE (1) | PE20020829A1 (ja) |
PL (1) | PL208413B1 (ja) |
SK (1) | SK287934B6 (ja) |
SV (1) | SV2003000836A (ja) |
WO (1) | WO2002055481A1 (ja) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1517915B1 (en) | 2002-06-11 | 2009-01-21 | Eli Lilly And Company | Prodrugs of excitatory amino acids |
WO2010111080A2 (en) | 2009-03-27 | 2010-09-30 | Eli Lilly And Company | Optimized treatment of schizophrenia |
AR079343A1 (es) * | 2009-12-21 | 2012-01-18 | Lilly Co Eli | Compuesto de acido 2-amino-4-(4h-1,2,4-triazol-3-ilsulfanil)biciclo[3.1.0]hexano-2,6-dicarboxilico, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar un trastorno psiquiatrico |
US9296710B2 (en) | 2011-06-17 | 2016-03-29 | Eli Lilly And Company | Bicyclo (3.1.0) hexane-2, 6-dicarboxylic acid derivatives as mGlu2 receptor agonist |
AR089718A1 (es) | 2012-02-01 | 2014-09-10 | Lilly Co Eli | AGONISTAS DE mGlu2/3 |
US11384061B2 (en) | 2018-04-17 | 2022-07-12 | Bayer Aktiengesellschaft | Process for preparing esters of N-acylated amino acids with acid-labile keto protective group functions |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5750566A (en) * | 1994-08-12 | 1998-05-12 | Eli Lilly And Company | Synthetic excitatory amino acids |
PL182285B1 (pl) | 1994-08-12 | 2001-12-31 | Lilly Co Eli | Syntetyczne aminokwasy oraz ich estry i srodki farmaceutyczne je zawierajace PL PL PL PL PL PL PL |
AU3364995A (en) | 1994-08-12 | 1996-03-07 | Eli Lilly And Company | Composition and method for treating anxiety |
IL118727A (en) | 1995-06-29 | 2003-01-12 | Lilly Co Eli | (-)-2-spiro-5-hydantoinbicyclo [3.1.0] hexane-6-carboxylic acid, salts thereof and use thereof for the preparation of (+)-(2) aminobicyclo [3.1.0] hexane-2,6-dicarboxylic acid |
ZA983930B (en) * | 1997-05-14 | 1999-11-08 | Lilly Co Eli | Excitatory amino acid receptor modulators. |
ES2191412T3 (es) | 1998-01-28 | 2003-09-01 | Taisho Pharmaceutical Co Ltd | Derivados de aminoacidos que contienen fluor. |
GB9815542D0 (en) | 1998-07-17 | 1998-09-16 | Lilly Co Eli | Bicyclohexane derivatives |
US6528499B1 (en) | 2000-04-27 | 2003-03-04 | Georgetown University | Ligands for metabotropic glutamate receptors and inhibitors of NAALADase |
WO2002055485A1 (en) | 2001-01-11 | 2002-07-18 | Eli Lilly And Company | Prodrugs of excitatory amino acids |
EP1423411A2 (en) | 2001-07-09 | 2004-06-02 | Eli Lilly And Company | Prodrugs of excitatory amino acids |
AU2002353845A1 (en) | 2001-11-23 | 2003-06-10 | Eli Lilly And Company | Prodrugs of excitatory amino acids |
AU2002361611A1 (en) | 2001-12-21 | 2003-07-24 | Eli Lilly And Company | Prodrugs of excitatory amino acids |
-
2001
- 2001-12-14 HU HU0400620A patent/HUP0400620A3/hu unknown
- 2001-12-14 IL IL15636401A patent/IL156364A0/xx unknown
- 2001-12-14 US US10/250,448 patent/US7256217B2/en not_active Expired - Fee Related
- 2001-12-14 CN CNB018219667A patent/CN1267407C/zh not_active Expired - Fee Related
- 2001-12-14 NZ NZ526050A patent/NZ526050A/en unknown
- 2001-12-21 PL PL361669A patent/PL208413B1/pl unknown
- 2001-12-21 BR BR0116770-7A patent/BR0116770A/pt not_active IP Right Cessation
- 2001-12-21 DE DE60127182T patent/DE60127182T2/de not_active Expired - Lifetime
- 2001-12-21 JP JP2002556156A patent/JP4064237B2/ja not_active Expired - Fee Related
- 2001-12-21 MX MXPA03006186A patent/MXPA03006186A/es active IP Right Grant
- 2001-12-21 DZ DZ013461A patent/DZ3461A1/fr active
- 2001-12-21 CZ CZ20031916A patent/CZ303490B6/cs not_active IP Right Cessation
- 2001-12-21 CA CA2433667A patent/CA2433667C/en not_active Expired - Fee Related
- 2001-12-21 ES ES01989859T patent/ES2282315T3/es not_active Expired - Lifetime
- 2001-12-21 SK SK826-2003A patent/SK287934B6/sk not_active IP Right Cessation
- 2001-12-21 EP EP01989859A patent/EP1368304B1/en not_active Expired - Lifetime
- 2001-12-21 AU AU2002228737A patent/AU2002228737B2/en not_active Ceased
- 2001-12-21 AT AT01989859T patent/ATE356111T1/de not_active IP Right Cessation
- 2001-12-21 KR KR10-2003-7009216A patent/KR20030090622A/ko not_active Application Discontinuation
- 2001-12-21 WO PCT/US2001/045866 patent/WO2002055481A1/en active IP Right Grant
-
2002
- 2002-01-10 PE PE2002000010A patent/PE20020829A1/es not_active Application Discontinuation
- 2002-01-11 SV SV2002000836A patent/SV2003000836A/es not_active Application Discontinuation
- 2002-01-11 AR ARP020100085A patent/AR036007A1/es unknown
-
2003
- 2003-07-10 NO NO20033166A patent/NO20033166L/no not_active Application Discontinuation
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