JP2011524912A5 - - Google Patents
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- Publication number
- JP2011524912A5 JP2011524912A5 JP2011514714A JP2011514714A JP2011524912A5 JP 2011524912 A5 JP2011524912 A5 JP 2011524912A5 JP 2011514714 A JP2011514714 A JP 2011514714A JP 2011514714 A JP2011514714 A JP 2011514714A JP 2011524912 A5 JP2011524912 A5 JP 2011524912A5
- Authority
- JP
- Japan
- Prior art keywords
- heterocycle
- alkyl
- alkynyl
- alkenyl
- arylalkyl
- 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- Withdrawn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
- 125000000623 heterocyclic group Chemical group 0.000 claims 60
- 125000000217 alkyl group Chemical group 0.000 claims 38
- 125000003342 alkenyl group Chemical group 0.000 claims 35
- 125000000304 alkynyl group Chemical group 0.000 claims 35
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 19
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims 19
- 125000005356 cycloalkylalkenyl group Chemical group 0.000 claims 19
- 125000005357 cycloalkylalkynyl group Chemical group 0.000 claims 19
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 125000001424 substituent group Chemical group 0.000 claims 19
- 125000005018 aryl alkenyl group Chemical group 0.000 claims 15
- 125000003710 aryl alkyl group Chemical group 0.000 claims 15
- 125000005015 aryl alkynyl group Chemical group 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 15
- 125000004447 heteroarylalkenyl group Chemical group 0.000 claims 15
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 15
- 125000005312 heteroarylalkynyl group Chemical group 0.000 claims 15
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 239000003112 inhibitor Substances 0.000 claims 11
- 229920000728 polyester Polymers 0.000 claims 11
- 239000011435 rock Substances 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 239000007951 isotonicity adjuster Substances 0.000 claims 10
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 239000000825 pharmaceutical preparation Substances 0.000 claims 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 7
- 239000002736 nonionic surfactant Substances 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 230000003204 osmotic effect Effects 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 239000004094 surface-active agent Substances 0.000 claims 4
- 239000000872 buffer Substances 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerol group Chemical group OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000004434 sulfur atom Chemical group 0.000 claims 3
- 239000012929 tonicity agent Substances 0.000 claims 3
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims 2
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 2
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 2
- 229920002675 Polyoxyl Polymers 0.000 claims 2
- 125000002015 acyclic group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 229960000502 poloxamer Drugs 0.000 claims 2
- 229920001983 poloxamer Polymers 0.000 claims 2
- 229920000136 polysorbate Polymers 0.000 claims 2
- 229950008882 polysorbate Drugs 0.000 claims 2
- HRCKLYFDWWYCLS-LJQANCHMSA-N 2-[3-[[(3r)-3-(isoquinolin-5-ylamino)pyrrolidin-1-yl]methyl]phenoxy]ethanol Chemical group OCCOC1=CC=CC(CN2C[C@@H](CC2)NC=2C3=CC=NC=C3C=CC=2)=C1 HRCKLYFDWWYCLS-LJQANCHMSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 239000004359 castor oil Substances 0.000 claims 1
- 235000019438 castor oil Nutrition 0.000 claims 1
- 239000002738 chelating agent Substances 0.000 claims 1
- 239000007979 citrate buffer Substances 0.000 claims 1
- 239000008121 dextrose Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims 1
- 229940075507 glyceryl monostearate Drugs 0.000 claims 1
- 230000004410 intraocular pressure Effects 0.000 claims 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims 1
- DSSHWWLYALEYJS-HXUWFJFHSA-N n-[3-[[(3r)-3-(1h-indazol-5-ylamino)piperidin-1-yl]methyl]phenyl]ethanesulfonamide Chemical group CCS(=O)(=O)NC1=CC=CC(CN2C[C@@H](CCC2)NC=2C=C3C=NNC3=CC=2)=C1 DSSHWWLYALEYJS-HXUWFJFHSA-N 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- 239000008363 phosphate buffer Substances 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 239000003755 preservative agent Substances 0.000 claims 1
- 230000002335 preservative effect Effects 0.000 claims 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 1
- VLPFTAMPNXLGLX-UHFFFAOYSA-N trioctanoin Chemical compound CCCCCCCC(=O)OCC(OC(=O)CCCCCCC)COC(=O)CCCCCCC VLPFTAMPNXLGLX-UHFFFAOYSA-N 0.000 claims 1
- 229920001664 tyloxapol Polymers 0.000 claims 1
- MDYZKJNTKZIUSK-UHFFFAOYSA-N tyloxapol Chemical compound O=C.C1CO1.CC(C)(C)CC(C)(C)C1=CC=C(O)C=C1 MDYZKJNTKZIUSK-UHFFFAOYSA-N 0.000 claims 1
- 229960004224 tyloxapol Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7351908P | 2008-06-18 | 2008-06-18 | |
| US61/073,519 | 2008-06-18 | ||
| PCT/US2009/047108 WO2009155209A1 (en) | 2008-06-18 | 2009-06-11 | Ophthalmic formulation of rho kinase inhibitor compound |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011524912A JP2011524912A (ja) | 2011-09-08 |
| JP2011524912A5 true JP2011524912A5 (https=) | 2012-06-07 |
Family
ID=41434400
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011514714A Withdrawn JP2011524912A (ja) | 2008-06-18 | 2009-06-11 | Ｒｈｏキナーゼ阻害化合物の眼科用製剤 |
Country Status (3)
| Country | Link |
|---|---|
| EP (1) | EP2299820A4 (https=) |
| JP (1) | JP2011524912A (https=) |
| WO (1) | WO2009155209A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20130095263A (ko) * | 2010-07-27 | 2013-08-27 | 인스파이어 파마슈티컬스 인코퍼레이티드 | 전구약물 형태의 키나아제 저해제 화합물을 사용하여 안질환을 치료하는 방법 |
| CN107109410B (zh) | 2014-08-22 | 2021-11-02 | 奥克兰联合服务有限公司 | 通道调节剂 |
| EP3843845B1 (en) | 2018-08-29 | 2026-03-11 | University Of Massachusetts | Inhibition of protein kinases to treat friedreich ataxia |
| WO2020072456A1 (en) * | 2018-10-02 | 2020-04-09 | Case Western Reserve University | Compounds for treating myelin related disorders |
| CN120457109A (zh) | 2022-12-30 | 2025-08-08 | 阿维森纳生物科学公司 | 氮杂吲哚rock抑制剂 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7217722B2 (en) * | 2000-02-01 | 2007-05-15 | Kirin Beer Kabushiki Kaisha | Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same |
| EP1550660A1 (en) * | 2002-09-12 | 2005-07-06 | Kirin Beer Kabushiki Kaisha | Isoquinoline derivatives having kinasae inhibitory activity and drugs containing the same |
| EP2468729B1 (en) * | 2003-10-15 | 2013-12-25 | Ube Industries, Ltd. | Novel indazole derivative |
| US20050272851A1 (en) * | 2004-06-04 | 2005-12-08 | Xerox Corporation | Wax emulsion for emulsion aggregation toner |
| EP1962853A1 (en) * | 2005-12-22 | 2008-09-03 | Alcon Research, Ltd. | (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)- pyrazines for treating rho kinase-mediated diseases and conditions |
-
2009
- 2009-06-11 WO PCT/US2009/047108 patent/WO2009155209A1/en not_active Ceased
- 2009-06-11 EP EP09767519A patent/EP2299820A4/en not_active Withdrawn
- 2009-06-11 JP JP2011514714A patent/JP2011524912A/ja not_active Withdrawn
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