JP2007519754A5 - - Google Patents
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- Publication number
- JP2007519754A5 JP2007519754A5 JP2006551626A JP2006551626A JP2007519754A5 JP 2007519754 A5 JP2007519754 A5 JP 2007519754A5 JP 2006551626 A JP2006551626 A JP 2006551626A JP 2006551626 A JP2006551626 A JP 2006551626A JP 2007519754 A5 JP2007519754 A5 JP 2007519754A5
- Authority
- JP
- Japan
- Prior art keywords
- benzamide
- pyrimidinyl
- amino
- methyl
- phenyl
- 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.)
- Pending
Links
- -1 2-amino-4-pyrimidinyl Chemical group 0.000 claims 29
- KXDAEFPNCMNJSK-UHFFFAOYSA-N benzene carboxamide Natural products NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 5
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- ZYHQGITXIJDDKC-UHFFFAOYSA-N 2-[2-(2-aminophenyl)ethyl]aniline Chemical group NC1=CC=CC=C1CCC1=CC=CC=C1N ZYHQGITXIJDDKC-UHFFFAOYSA-N 0.000 claims 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004208 3-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C([H])C(*)=C1[H] 0.000 claims 1
- OQXPFQFKBILBEF-UHFFFAOYSA-N 4-(1h-indazol-5-yl)-n-[(3-methoxyphenyl)methyl]benzamide Chemical compound COC1=CC=CC(CNC(=O)C=2C=CC(=CC=2)C=2C=C3C=NNC3=CC=2)=C1 OQXPFQFKBILBEF-UHFFFAOYSA-N 0.000 claims 1
- IRGOHKRWMGVGCR-UHFFFAOYSA-N 4-(2-aminopyrimidin-4-yl)-n-[(3-methoxyphenyl)methyl]benzamide Chemical compound COC1=CC=CC(CNC(=O)C=2C=CC(=CC=2)C=2N=C(N)N=CC=2)=C1 IRGOHKRWMGVGCR-UHFFFAOYSA-N 0.000 claims 1
- JZIIWVNIBYGBPC-UHFFFAOYSA-N 4-(2-aminopyrimidin-4-yl)-n-[(4-methoxyphenyl)methyl]benzamide Chemical compound C1=CC(OC)=CC=C1CNC(=O)C1=CC=C(C=2N=C(N)N=CC=2)C=C1 JZIIWVNIBYGBPC-UHFFFAOYSA-N 0.000 claims 1
- NAPIHYHPUPRPDF-UHFFFAOYSA-N 4-(2-chloropyridin-4-yl)-n-[(3-methoxyphenyl)methyl]benzamide Chemical compound COC1=CC=CC(CNC(=O)C=2C=CC(=CC=2)C=2C=C(Cl)N=CC=2)=C1 NAPIHYHPUPRPDF-UHFFFAOYSA-N 0.000 claims 1
- FTEKOWMGBWHZSA-UHFFFAOYSA-N 4-(6-aminopyrimidin-4-yl)-n-[(3-methoxyphenyl)methyl]benzamide Chemical compound COC1=CC=CC(CNC(=O)C=2C=CC(=CC=2)C=2N=CN=C(N)C=2)=C1 FTEKOWMGBWHZSA-UHFFFAOYSA-N 0.000 claims 1
- ATYMIQGWWSULBL-UHFFFAOYSA-N 5-(2-aminopyrimidin-4-yl)-2-benzyl-3h-isoindol-1-one Chemical compound NC1=NC=CC(C=2C=C3CN(CC=4C=CC=CC=4)C(=O)C3=CC=2)=N1 ATYMIQGWWSULBL-UHFFFAOYSA-N 0.000 claims 1
- OFDXNOMIOCNAHC-UHFFFAOYSA-N 6-(2-aminopyrimidin-4-yl)-2-benzylisoquinolin-1-one Chemical compound NC1=NC=CC(C=2C=C3C(C(N(CC=4C=CC=CC=4)C=C3)=O)=CC=2)=N1 OFDXNOMIOCNAHC-UHFFFAOYSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- VCCHIIPGONQZHJ-UHFFFAOYSA-N n-[(3-methoxyphenyl)methyl]-4-(1h-pyrazol-4-yl)benzamide Chemical compound COC1=CC=CC(CNC(=O)C=2C=CC(=CC=2)C2=CNN=C2)=C1 VCCHIIPGONQZHJ-UHFFFAOYSA-N 0.000 claims 1
- TURLOSKPJBPGOR-UHFFFAOYSA-N n-[(3-methoxyphenyl)methyl]-4-[6-(prop-2-enylamino)pyrimidin-4-yl]benzamide Chemical compound COC1=CC=CC(CNC(=O)C=2C=CC(=CC=2)C=2N=CN=C(NCC=C)C=2)=C1 TURLOSKPJBPGOR-UHFFFAOYSA-N 0.000 claims 1
- JBLPUDJLELBRHC-UHFFFAOYSA-N n-[(3-methoxyphenyl)methyl]-4-pyridin-4-ylbenzamide Chemical compound COC1=CC=CC(CNC(=O)C=2C=CC(=CC=2)C=2C=CN=CC=2)=C1 JBLPUDJLELBRHC-UHFFFAOYSA-N 0.000 claims 1
- BHWQEVXWYHXNMX-UHFFFAOYSA-N n-[(3-methoxyphenyl)methyl]-4-pyrimidin-4-ylbenzamide Chemical compound COC1=CC=CC(CNC(=O)C=2C=CC(=CC=2)C=2N=CN=CC=2)=C1 BHWQEVXWYHXNMX-UHFFFAOYSA-N 0.000 claims 1
- SYSUZXPGQXEWCZ-UHFFFAOYSA-N n-benzyl-4-pyridin-4-ylbenzamide Chemical compound C=1C=C(C=2C=CN=CC=2)C=CC=1C(=O)NCC1=CC=CC=C1 SYSUZXPGQXEWCZ-UHFFFAOYSA-N 0.000 claims 1
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US54062104P | 2004-01-30 | 2004-01-30 | |
| PCT/US2005/003479 WO2005074643A2 (en) | 2004-01-30 | 2005-01-28 | Benzamide compounds useful as rock inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007519754A JP2007519754A (ja) | 2007-07-19 |
| JP2007519754A5 true JP2007519754A5 (OSRAM) | 2008-03-13 |
Family
ID=34837407
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006551626A Pending JP2007519754A (ja) | 2004-01-30 | 2005-01-28 | 化合物 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20080275062A1 (OSRAM) |
| EP (1) | EP1713775A4 (OSRAM) |
| JP (1) | JP2007519754A (OSRAM) |
| WO (1) | WO2005074643A2 (OSRAM) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200613272A (en) * | 2004-08-13 | 2006-05-01 | Astrazeneca Ab | Isoindolone compounds and their use as metabotropic glutamate receptor potentiators |
| EP1854484A4 (en) * | 2005-02-16 | 2010-02-10 | Astellas Pharma Inc | REMEDY FOR PAIN CONTAINING INHIBITOR OF RHO-KINASE PROTEIN |
| EP1912939A1 (en) * | 2005-08-12 | 2008-04-23 | AstraZeneca AB | Metabotropic glutamate-receptor-potentiating isoindolones |
| US7868008B2 (en) | 2005-08-12 | 2011-01-11 | Astrazeneca Ab | Substituted isoindolones and their use as metabotropic glutamate receptor potentiators |
| US7807706B2 (en) | 2005-08-12 | 2010-10-05 | Astrazeneca Ab | Metabotropic glutamate-receptor-potentiating isoindolones |
| EP1922306A2 (en) | 2005-09-02 | 2008-05-21 | Astellas Pharma Inc. | Amide derivatives as rock inhibitors |
| CL2007003874A1 (es) * | 2007-01-03 | 2008-05-16 | Boehringer Ingelheim Int | Compuestos derivados de benzamida; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar enfermedades cardiovasculares, hipertension, aterosclerosis, reestenosis, ictus, insuficiencia cardiaca, lesion isquemica, hipertensio |
| TWI417100B (zh) | 2007-06-07 | 2013-12-01 | Astrazeneca Ab | 二唑衍生物及其作為代謝型麩胺酸受體增效劑-８４２之用途 |
| ES2453950T3 (es) * | 2007-08-27 | 2014-04-09 | AbbVie Deutschland GmbH & Co. KG | 4-(4-Piridinil)-benzamidas y su uso como moduladores de la actividad de ROCK |
| SA109300358B1 (ar) | 2008-06-06 | 2012-11-03 | استرازينيكا ايه بي | مقويات مستقبل جلوتامات ذي انتحاء أيضي من أيزو إندولون |
| CN105861446B (zh) | 2009-10-16 | 2021-10-01 | 斯克里普斯研究所 | 多能细胞的诱导 |
| AU2010314204B2 (en) * | 2009-11-04 | 2015-03-26 | Nerviano Medical Sciences S.R.L. | Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides |
| UY33469A (es) * | 2010-06-29 | 2012-01-31 | Irm Llc Y Novartis Ag | Composiciones y metodos para modular la via de señalizacion de wnt |
| KR20200113286A (ko) | 2010-12-22 | 2020-10-06 | 페이트 세러퓨틱스, 인코포레이티드 | 단세포 분류 및 iPSC의 증강된 재프로그래밍을 위한 세포 배양 플랫폼 |
| US8895571B2 (en) | 2011-10-14 | 2014-11-25 | Incyte Corporation | Isoindolinone and pyrrolopyridinone derivatives as Akt inhibitors |
| EP2628482A1 (en) | 2012-02-17 | 2013-08-21 | Academisch Medisch Centrum | Rho kinase inhiitors for use in the treatment of neuroblastoma |
| WO2014079850A1 (en) * | 2012-11-23 | 2014-05-30 | F. Hoffmann-La Roche Ag | Substituted heterocyclic derivatives |
| TW201444798A (zh) * | 2013-02-28 | 2014-12-01 | 必治妥美雅史谷比公司 | 作爲強效ｒｏｃｋ１及ｒｏｃｋ２抑制劑之苯基吡唑衍生物 |
| US9828345B2 (en) | 2013-02-28 | 2017-11-28 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
| CN105518005B (zh) | 2013-07-02 | 2018-07-20 | 百时美施贵宝公司 | 作为rock抑制剂的三环吡啶-甲酰胺衍生物 |
| CN105492444B (zh) | 2013-07-02 | 2018-09-07 | 百时美施贵宝公司 | 作为rock抑制剂的三环吡啶-甲酰胺衍生物 |
| SI3080103T1 (sl) * | 2013-12-11 | 2018-11-30 | Biogen Ma Inc. | Biarilne spojine, ki so uporabne za zdravljenje človeških bolezni na področju onkologije, nevrologije in imunologije |
| KR102460549B1 (ko) | 2014-03-04 | 2022-10-28 | 페이트 세러퓨틱스, 인코포레이티드 | 개선된 재프로그래밍 방법 및 세포 배양 플랫폼 |
| CN107108581B (zh) * | 2014-08-21 | 2020-06-23 | 百时美施贵宝公司 | 作为强效rock抑制剂的回接苯甲酰胺衍生物 |
| WO2016112236A1 (en) | 2015-01-09 | 2016-07-14 | Bristol-Myers Squibb Company | Cyclic ureas as inhibitors of rock |
| US10112929B2 (en) | 2015-03-09 | 2018-10-30 | Bristol-Myers Squibb Company | Lactams as inhibitors of rock |
| US12048761B2 (en) | 2015-10-13 | 2024-07-30 | Inserm (Institut National De La Santé Et De La Recherche Medicale) | Methods and pharmaceutical compositions for the treatment of retinal capillary non-perfusion |
| EP4088719A1 (en) | 2015-10-13 | 2022-11-16 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods and pharmaceutical compositions for the treatment of retinal capillary non-perfusion |
| KR20250007036A (ko) | 2015-10-16 | 2025-01-13 | 페이트 세러퓨틱스, 인코포레이티드 | 기저 상태 다능성의 유도 및 유지를 위한 플랫폼 |
| WO2017205709A1 (en) | 2016-05-27 | 2017-11-30 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of rock |
| WO2018009625A1 (en) | 2016-07-07 | 2018-01-11 | Bristol-Myers Squibb Company | Spirolactams as inhibitors of rock |
| CN110049977B (zh) | 2016-07-07 | 2022-01-18 | 百时美施贵宝公司 | 作为强效和选择性rock抑制剂的内酰胺、环状脲和氨基甲酸酯及三唑酮衍生物 |
| ES2829400T3 (es) | 2016-11-30 | 2021-05-31 | Bristol Myers Squibb Co | Inhibidores tricíclicos de Rho cinasa |
| CN108203433B (zh) * | 2016-12-16 | 2020-07-03 | 成都先导药物开发股份有限公司 | 一种rock抑制剂及其应用 |
| EP3710008A4 (en) | 2017-11-14 | 2021-08-25 | The Schepens Eye Research Institute, Inc. | RUNX1 INHIBITION FOR THE TREATMENT OF PROLIFERATIVE VITREORETINOPATHY AND DISEASES ASSOCIATED WITH EPITHELIAL-MESENCHYMAL TRANSITION |
| EP3782987B1 (en) | 2018-04-18 | 2025-04-02 | Medshine Discovery Inc. | Benzopyrazole compound used as rho kinase inhibitor |
| CA3110661A1 (en) | 2018-08-29 | 2020-03-05 | University Of Massachusetts | Inhibition of protein kinases to treat friedreich ataxia |
| WO2020193802A1 (en) | 2019-03-28 | 2020-10-01 | Fundación De La Comunidad Valenciana Centro De Investigación Príncipe Felipe | Polymeric conjugates and uses thereof |
| CN114555561B (zh) * | 2019-10-18 | 2023-08-11 | 南京明德新药研发有限公司 | 作为rho激酶抑制剂的苯并吡唑类化合物的盐型、晶型及其制备方法 |
| WO2022100614A1 (zh) * | 2020-11-11 | 2022-05-19 | 南京明德新药研发有限公司 | 苯并脲环衍生物及其制备方法和应用 |
| US20230416221A1 (en) * | 2020-11-20 | 2023-12-28 | Hefei Institutes Of Physical Science, Chinese Academy Of Sciences | Dihydroisoquinolinone and isoindolinone derivatives and uses thereof |
| WO2022150381A1 (en) * | 2021-01-06 | 2022-07-14 | Genosco Inc. | Selective inhibitors of rock1 and rock2 protein kinases and uses thereof |
| WO2025224050A1 (en) | 2024-04-22 | 2025-10-30 | Institut National de la Santé et de la Recherche Médicale | Methods of treatment of patients suffering from hypomelanosis of ito |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW440563B (en) * | 1996-05-23 | 2001-06-16 | Hoffmann La Roche | Aryl pyrimidine derivatives and a pharmaceutical composition thereof |
| CA2340100A1 (en) * | 1998-08-11 | 2000-02-24 | Daiichi Pharmaceutical Co., Ltd. | Novel sulfonyl derivatives |
| TWI243164B (en) * | 2001-02-13 | 2005-11-11 | Aventis Pharma Gmbh | Acylated indanyl amines and their use as pharmaceuticals |
| KR20100107509A (ko) * | 2001-09-14 | 2010-10-05 | 9222-9129 퀘벡 인코포레이티드 | 히스톤 데아세틸라아제의 억제제 |
| TWI319387B (en) * | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
| EP1575918A2 (en) * | 2002-12-19 | 2005-09-21 | Neurogen Corporation | Substituted biaryl-4-carboxylic acid arylamide analogues as capsaicin receptor modulators |
| TW200613272A (en) * | 2004-08-13 | 2006-05-01 | Astrazeneca Ab | Isoindolone compounds and their use as metabotropic glutamate receptor potentiators |
| AR051596A1 (es) * | 2004-10-26 | 2007-01-24 | Irm Llc | Compuestos heterociclicos condensados nitrogenados como inhibidores de la actividad del receptor canabinoide 1; composiciones farmaceuticas que los contienen y su empleo en la preparacion de medicamentos para el tratamiento de trastornos alimentarios |
-
2005
- 2005-01-28 EP EP05712794A patent/EP1713775A4/en not_active Withdrawn
- 2005-01-28 US US10/597,473 patent/US20080275062A1/en not_active Abandoned
- 2005-01-28 JP JP2006551626A patent/JP2007519754A/ja active Pending
- 2005-01-28 WO PCT/US2005/003479 patent/WO2005074643A2/en not_active Ceased
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