JP2008508248A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2008508248A5 JP2008508248A5 JP2007523161A JP2007523161A JP2008508248A5 JP 2008508248 A5 JP2008508248 A5 JP 2008508248A5 JP 2007523161 A JP2007523161 A JP 2007523161A JP 2007523161 A JP2007523161 A JP 2007523161A JP 2008508248 A5 JP2008508248 A5 JP 2008508248A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- indole
- carboxamidine
- benzyl
- pain
- 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.)
- Withdrawn
Links
- NUNZGJKXTJMXGY-UHFFFAOYSA-N 1H-indole-2-carboximidamide Chemical class C1=CC=C2NC(C(=N)N)=CC2=C1 NUNZGJKXTJMXGY-UHFFFAOYSA-N 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 6
- 241000725303 Human immunodeficiency virus Species 0.000 claims 4
- 208000002193 Pain Diseases 0.000 claims 4
- 150000001450 anions Chemical class 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 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 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 208000015122 neurodegenerative disease Diseases 0.000 claims 4
- 208000024891 symptom Diseases 0.000 claims 4
- 239000000654 additive Substances 0.000 claims 3
- 150000003974 aralkylamines Chemical class 0.000 claims 3
- 239000000969 carrier Substances 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000019901 Anxiety disease Diseases 0.000 claims 2
- 206010058019 Cancer Pain Diseases 0.000 claims 2
- 208000000094 Chronic Pain Diseases 0.000 claims 2
- 206010011878 Deafness Diseases 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 208000010412 Glaucoma Diseases 0.000 claims 2
- 241000282412 Homo Species 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- 208000013016 Hypoglycemia Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 208000019695 Migraine disease Diseases 0.000 claims 2
- 208000007101 Muscle Cramp Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 208000028017 Psychotic disease Diseases 0.000 claims 2
- 208000005392 Spasm Diseases 0.000 claims 2
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims 2
- 208000009205 Tinnitus Diseases 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 229940126574 aminoglycoside antibiotic Drugs 0.000 claims 2
- 239000002647 aminoglycoside antibiotic agent Substances 0.000 claims 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- 230000036506 anxiety Effects 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 210000004556 brain Anatomy 0.000 claims 2
- 208000015114 central nervous system disease Diseases 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 229960003920 cocaine Drugs 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003995 emulsifying agent Substances 0.000 claims 2
- 206010015037 epilepsy Diseases 0.000 claims 2
- 239000000796 flavoring agent Substances 0.000 claims 2
- 235000013355 food flavoring agent Nutrition 0.000 claims 2
- 239000003205 fragrance Substances 0.000 claims 2
- 230000010370 hearing loss Effects 0.000 claims 2
- 231100000888 hearing loss Toxicity 0.000 claims 2
- 208000016354 hearing loss disease Diseases 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 230000002218 hypoglycaemic effect Effects 0.000 claims 2
- 208000014674 injury Diseases 0.000 claims 2
- 230000000302 ischemic effect Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 206010027599 migraine Diseases 0.000 claims 2
- 208000004296 neuralgia Diseases 0.000 claims 2
- 231100000878 neurological injury Toxicity 0.000 claims 2
- 208000021722 neuropathic pain Diseases 0.000 claims 2
- 230000003287 optical effect Effects 0.000 claims 2
- 230000003204 osmotic effect Effects 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 210000001525 retina Anatomy 0.000 claims 2
- 210000000278 spinal cord Anatomy 0.000 claims 2
- 239000003381 stabilizer Substances 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 231100000886 tinnitus Toxicity 0.000 claims 2
- 230000008736 traumatic injury Effects 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical group C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 1
- VAVCHKDWTHPHIZ-UHFFFAOYSA-N 5-methoxy-N'-[(3-methoxyphenyl)methyl]-1H-indole-2-carboximidamide Chemical compound COC1=CC=CC(CNC(=N)C=2NC3=CC=C(OC)C=C3C=2)=C1 VAVCHKDWTHPHIZ-UHFFFAOYSA-N 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 102100022630 Glutamate receptor ionotropic, NMDA 2B Human genes 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- YFSGCLWMVKOPCV-UHFFFAOYSA-N N'-[(2-ethoxyphenyl)methyl]-1H-indole-2-carboximidamide Chemical compound CCOC1=CC=CC=C1CNC(=N)C1=CC2=CC=CC=C2N1 YFSGCLWMVKOPCV-UHFFFAOYSA-N 0.000 claims 1
- AHWVUKXCVFZVQZ-UHFFFAOYSA-N N'-[(2-ethoxyphenyl)methyl]-5-fluoro-1H-indole-2-carboximidamide Chemical compound CCOC1=CC=CC=C1CNC(=N)C1=CC2=CC(F)=CC=C2N1 AHWVUKXCVFZVQZ-UHFFFAOYSA-N 0.000 claims 1
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 claims 1
- 102000014649 NMDA glutamate receptor activity proteins Human genes 0.000 claims 1
- -1 Preparations Substances 0.000 claims 1
- 108010038912 Retinoid X Receptors Proteins 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 125000005907 alkyl ester group Chemical group 0.000 claims 1
- 230000003042 antagnostic effect Effects 0.000 claims 1
- XRFJTMWLAFLVMZ-UHFFFAOYSA-N chembl1187939 Chemical compound COC1=CC=CC(OC)=C1CNC(=N)C1=CC2=CC=CC=C2N1 XRFJTMWLAFLVMZ-UHFFFAOYSA-N 0.000 claims 1
- AZFIMJORKKWWAI-UHFFFAOYSA-N chembl1188722 Chemical compound COC1=CC=CC(OC)=C1CNC(=N)C1=CC2=CC(Cl)=CC=C2N1 AZFIMJORKKWWAI-UHFFFAOYSA-N 0.000 claims 1
- ORNVTLQUTGQFPT-UHFFFAOYSA-N chembl1189498 Chemical compound COC1=CC=CC(OC)=C1CNC(=N)C1=CC2=CC(F)=CC=C2N1 ORNVTLQUTGQFPT-UHFFFAOYSA-N 0.000 claims 1
- SGCBSFBLWDLENT-UHFFFAOYSA-N chembl1197001 Chemical compound C=1C2=CC(OC)=CC=C2NC=1C(=N)NCC1=C(OC)C=CC=C1OC SGCBSFBLWDLENT-UHFFFAOYSA-N 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000000945 filler Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 239000008194 pharmaceutical composition 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
- 238000002360 preparation method Methods 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 238000009736 wetting Methods 0.000 claims 1
- 239000000080 wetting agent Substances 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HU0401523A HUP0401523A3 (en) | 2004-07-29 | 2004-07-29 | Indole-2-carboxamide derivatives, pharmaceutical compositions containing them and process for producing them |
| PCT/HU2005/000078 WO2006010965A1 (en) | 2004-07-29 | 2005-07-21 | Indole-2 -carboxamidine derivatives as nmda receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008508248A JP2008508248A (ja) | 2008-03-21 |
| JP2008508248A5 true JP2008508248A5 (enExample) | 2008-05-15 |
Family
ID=89985408
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007523161A Withdrawn JP2008508248A (ja) | 2004-07-29 | 2005-07-21 | Ｎｍｄａ受容体アンタゴニストとしてのインドール−２−カルボキサミジン誘導体 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US20090048303A1 (enExample) |
| EP (1) | EP1773770B1 (enExample) |
| JP (1) | JP2008508248A (enExample) |
| KR (1) | KR20070038502A (enExample) |
| CN (1) | CN1989103A (enExample) |
| AP (1) | AP2006003840A0 (enExample) |
| AT (1) | ATE427299T1 (enExample) |
| AU (1) | AU2005266160A1 (enExample) |
| BR (1) | BRPI0513932A (enExample) |
| CA (1) | CA2574155A1 (enExample) |
| DE (1) | DE602005013675D1 (enExample) |
| EA (1) | EA009981B1 (enExample) |
| GE (1) | GEP20094606B (enExample) |
| HU (1) | HUP0401523A3 (enExample) |
| IL (1) | IL179485A0 (enExample) |
| MA (1) | MA28815B1 (enExample) |
| MX (1) | MX2007001052A (enExample) |
| NO (1) | NO20071109L (enExample) |
| TN (1) | TNSN07016A1 (enExample) |
| WO (1) | WO2006010965A1 (enExample) |
| ZA (1) | ZA200700325B (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7732162B2 (en) | 2003-05-05 | 2010-06-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases |
| US8278345B2 (en) | 2006-11-09 | 2012-10-02 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| ATE554085T1 (de) | 2006-11-30 | 2012-05-15 | Probiodrug Ag | Neue inhibitoren von glutaminylcyclase |
| JP5930573B2 (ja) | 2007-03-01 | 2016-06-15 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤の新規使用 |
| EP2142514B1 (en) | 2007-04-18 | 2014-12-24 | Probiodrug AG | Thiourea derivatives as glutaminyl cyclase inhibitors |
| JP5934645B2 (ja) | 2009-09-11 | 2016-06-15 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体 |
| CA2788656A1 (en) | 2010-02-16 | 2011-08-25 | Pfizer Inc. | (r)-4-((4-((4-(tetrahydrofuran-3-yloxy)benzo[d]isoxazol-3-yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2h-pyran-4-ol, a partial agonist of 5-ht4 receptors |
| JP6026284B2 (ja) | 2010-03-03 | 2016-11-16 | プロビオドルグ エージー | グルタミニルシクラーゼの阻害剤 |
| NZ602312A (en) | 2010-03-10 | 2014-02-28 | Probiodrug Ag | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
| WO2011131748A2 (en) | 2010-04-21 | 2011-10-27 | Probiodrug Ag | Novel inhibitors |
| SG10201510402WA (en) * | 2010-11-18 | 2016-01-28 | Univ Yale | Bifunctional molecules with antibody-recruiting and entry inhibitory activity against the human immunodeficiency virus |
| EP2686313B1 (en) | 2011-03-16 | 2016-02-03 | Probiodrug AG | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
| EP2852588B8 (en) * | 2012-05-22 | 2018-01-10 | Autifony Therapeutics Limited | Hydantoin derivatives as kv3 inhibitors |
| JO3579B1 (ar) | 2014-09-26 | 2020-07-05 | Luc Therapeutics Inc | مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول |
| JP7114594B2 (ja) | 2017-07-28 | 2022-08-08 | 武田薬品工業株式会社 | 複素環化合物 |
| ES2812698T3 (es) | 2017-09-29 | 2021-03-18 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
| JP2021050161A (ja) | 2019-09-25 | 2021-04-01 | 武田薬品工業株式会社 | 複素環化合物及びその用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9726388D0 (en) * | 1997-12-12 | 1998-02-11 | Cerebrus Ltd | Chemical compounds |
| US6376530B1 (en) * | 1999-05-10 | 2002-04-23 | Merck & Co., Inc. | Cyclic amidines useful as NMDA NR2B antagonists |
| US6319944B1 (en) * | 1999-05-10 | 2001-11-20 | Merck & Co., Inc. | Aryl amidines, compositions containing such compounds and methods of use |
| GB0015488D0 (en) * | 2000-06-23 | 2000-08-16 | Merck Sharp & Dohme | Therapeutic agents |
| HU227197B1 (en) * | 2000-10-24 | 2010-10-28 | Richter Gedeon Nyrt | Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them |
| JP2004253425A (ja) * | 2003-02-18 | 2004-09-09 | Tdk Corp | 積層コンデンサ |
-
2004
- 2004-07-29 HU HU0401523A patent/HUP0401523A3/hu unknown
-
2005
- 2005-07-21 EP EP05764412A patent/EP1773770B1/en not_active Expired - Lifetime
- 2005-07-21 DE DE602005013675T patent/DE602005013675D1/de not_active Expired - Fee Related
- 2005-07-21 US US11/658,787 patent/US20090048303A1/en not_active Abandoned
- 2005-07-21 CA CA002574155A patent/CA2574155A1/en not_active Abandoned
- 2005-07-21 CN CNA2005800247658A patent/CN1989103A/zh active Pending
- 2005-07-21 BR BRPI0513932-5A patent/BRPI0513932A/pt not_active IP Right Cessation
- 2005-07-21 EA EA200700365A patent/EA009981B1/ru not_active IP Right Cessation
- 2005-07-21 GE GEAP20059893A patent/GEP20094606B/en unknown
- 2005-07-21 AU AU2005266160A patent/AU2005266160A1/en not_active Abandoned
- 2005-07-21 WO PCT/HU2005/000078 patent/WO2006010965A1/en not_active Ceased
- 2005-07-21 JP JP2007523161A patent/JP2008508248A/ja not_active Withdrawn
- 2005-07-21 KR KR1020077000263A patent/KR20070038502A/ko not_active Withdrawn
- 2005-07-21 AP AP2006003840A patent/AP2006003840A0/xx unknown
- 2005-07-21 MX MX2007001052A patent/MX2007001052A/es active IP Right Grant
- 2005-07-21 AT AT05764412T patent/ATE427299T1/de not_active IP Right Cessation
-
2006
- 2006-11-22 IL IL179485A patent/IL179485A0/en unknown
-
2007
- 2007-01-11 ZA ZA200700325A patent/ZA200700325B/en unknown
- 2007-01-17 TN TNP2007000016A patent/TNSN07016A1/en unknown
- 2007-02-22 MA MA29702A patent/MA28815B1/fr unknown
- 2007-02-27 NO NO20071109A patent/NO20071109L/no not_active Application Discontinuation
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2008508248A5 (enExample) | ||
| DE602005002930T2 (de) | Sulfonamidderivate zur behandlung von krankheiten | |
| JP5612610B2 (ja) | ホスホジエステラーゼ阻害剤としての安息香酸（１−フェニル−２−ピリジン−４−イル）エチルエステル | |
| DE602005001929T2 (de) | Sulfonamidderivate zur behandlung von krankheiten | |
| RU2003115490A (ru) | Амидные производные в качестве антагонистов nmda рецептора | |
| EA017530B1 (ru) | Производные 1-фенил-2-пиридинилалкиловых спиртов в качестве ингибиторов фосфодиэстераз | |
| JP5822840B2 (ja) | 眼疾患処置薬 | |
| JP2008508247A5 (enExample) | ||
| CA2438991A1 (en) | Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists | |
| KR102568464B1 (ko) | 피롤로[2,3-d]피리미딘 화합물의 제조 방법, 이의 중간체, 및 이의 용도 | |
| JP6628252B2 (ja) | 虚血性眼疾患の処置用の医薬組成物 | |
| JP2006526604A (ja) | β−２アドレナリン受容体アゴニストとしての２−アミノ−ピリジン誘導体 | |
| TW201425311A (zh) | 新穎之雙環吡啶酮 | |
| JP2019513745A (ja) | ピロロ［１，２−ａ］ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用 | |
| JP2008508251A5 (enExample) | ||
| JP2007529499A (ja) | β２受容体アゴニストとしてのフェニルアミノエタノール誘導体 | |
| JP2016525142A5 (enExample) | ||
| JP2022512652A (ja) | Ｐ２ｘ３拮抗薬での皮膚掻痒症の治療 | |
| EP4313951A1 (en) | 1,3-substituted cyclobutyl derivatives and uses thereof | |
| JP2008508250A5 (enExample) | ||
| JP2020502063A5 (enExample) | ||
| JP2008508249A5 (enExample) | ||
| JP2006523674A (ja) | 慢性閉塞性肺疾患（ｃｏｐｄ）のための組合せ治療法 | |
| RU2005136431A (ru) | 4-, 6-или 7-гидроксииндолы с n-оксидными группами и их применение в качестве терапевтических средств | |
| HK40047992A (en) | Manufacturing process and intermediates for a pyrrolo[2,3- d]pyrimidine compound and use thereof |