JP2013527136A5 - - Google Patents
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- JP2013527136A5 JP2013527136A5 JP2012555446A JP2012555446A JP2013527136A5 JP 2013527136 A5 JP2013527136 A5 JP 2013527136A5 JP 2012555446 A JP2012555446 A JP 2012555446A JP 2012555446 A JP2012555446 A JP 2012555446A JP 2013527136 A5 JP2013527136 A5 JP 2013527136A5
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- JP
- Japan
- Prior art keywords
- alkyl
- het
- group
- substituted
- independently
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 165
- 125000001424 substituent group Chemical group 0.000 claims 68
- 229910052739 hydrogen Inorganic materials 0.000 claims 40
- 239000001257 hydrogen Substances 0.000 claims 40
- 125000003342 alkenyl group Chemical group 0.000 claims 26
- 125000001072 heteroaryl group Chemical group 0.000 claims 25
- 229910052799 carbon Inorganic materials 0.000 claims 23
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 19
- 150000002431 hydrogen Chemical class 0.000 claims 19
- 125000000623 heterocyclic group Chemical group 0.000 claims 17
- -1 hydrate Substances 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 12
- 125000005843 halogen group Chemical group 0.000 claims 11
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 150000002829 nitrogen Chemical group 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000003107 substituted aryl group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 125000005740 oxycarbonyl group Chemical group [*:1]OC([*:2])=O 0.000 claims 5
- 125000006647 (C3-C15) cycloalkyl group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 125000005418 aryl aryl group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000001544 thienyl group Chemical group 0.000 claims 4
- 208000009745 Eye Disease Diseases 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- IGERFAHWSHDDHX-UHFFFAOYSA-N 1,3-dioxanyl Chemical group [CH]1OCCCO1 IGERFAHWSHDDHX-UHFFFAOYSA-N 0.000 claims 2
- 208000010412 Glaucoma Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 201000005794 allergic hypersensitivity disease Diseases 0.000 claims 2
- 125000000319 biphenyl-4-yl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 208000003432 Bone Disease Diseases 0.000 claims 1
- 208000008787 Cardiovascular Disease Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000007906 Intestinal Disease Diseases 0.000 claims 1
- 208000001083 Kidney Disease Diseases 0.000 claims 1
- 208000002780 Macular Degeneration Diseases 0.000 claims 1
- 210000000329 Myocytes, Smooth Muscle Anatomy 0.000 claims 1
- 206010053643 Neurodegenerative disease Diseases 0.000 claims 1
- 206010029331 Neuropathy peripheral Diseases 0.000 claims 1
- 208000008760 Optic Nerve Disease Diseases 0.000 claims 1
- 206010061323 Optic neuropathy Diseases 0.000 claims 1
- 208000001218 Otorhinolaryngologic Disease Diseases 0.000 claims 1
- 208000003561 Respiratory Tract Disease Diseases 0.000 claims 1
- 208000007014 Retinitis Pigmentosa Diseases 0.000 claims 1
- 206010038932 Retinopathy Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 208000006641 Skin Disease Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 208000005918 Urinary Bladder Disease Diseases 0.000 claims 1
- 229930002945 all-trans-retinaldehyde Natural products 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 230000005549 barrier dysfunction Effects 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004619 benzopyranyl group Chemical group O1C(C=CC2=C1C=CC=C2)* 0.000 claims 1
- 201000008848 bladder disease Diseases 0.000 claims 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 1
- 230000003915 cell function Effects 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 230000001684 chronic Effects 0.000 claims 1
- 230000036461 convulsion Effects 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 150000002148 esters Chemical group 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000002757 inflammatory Effects 0.000 claims 1
- 200000000018 inflammatory disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000000414 obstructive Effects 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000002062 proliferating Effects 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 150000003254 radicals Chemical class 0.000 claims 1
- 238000007634 remodeling Methods 0.000 claims 1
- 230000002207 retinal Effects 0.000 claims 1
- 235000020945 retinal Nutrition 0.000 claims 1
- 239000011604 retinal Substances 0.000 claims 1
- 239000011435 rock Substances 0.000 claims 1
- 201000001880 sexual dysfunction Diseases 0.000 claims 1
- 231100000872 sexual dysfunction Toxicity 0.000 claims 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 0 Cc1ccc(*(*)C(O2)=O)c2c1 Chemical compound Cc1ccc(*(*)C(O2)=O)c2c1 0.000 description 8
- KMCGEYKRTBLDNR-UHFFFAOYSA-N CC(C1)c2ccccc2OC1=O Chemical compound CC(C1)c2ccccc2OC1=O KMCGEYKRTBLDNR-UHFFFAOYSA-N 0.000 description 1
- RUOJZAUFBMNUDX-UHFFFAOYSA-N CC(CO1)OC1=O Chemical compound CC(CO1)OC1=O RUOJZAUFBMNUDX-UHFFFAOYSA-N 0.000 description 1
- VKACUMNDDKMYEC-UHFFFAOYSA-N CC(Cc(cccc1)c1O1)C1=O Chemical compound CC(Cc(cccc1)c1O1)C1=O VKACUMNDDKMYEC-UHFFFAOYSA-N 0.000 description 1
- ULVAFTSBGFLYID-UHFFFAOYSA-N CC(O1)=C(N)OC1=O Chemical compound CC(O1)=C(N)OC1=O ULVAFTSBGFLYID-UHFFFAOYSA-N 0.000 description 1
- SYDXAGKNQBZUSM-UHFFFAOYSA-N NC(C1)OC1O Chemical compound NC(C1)OC1O SYDXAGKNQBZUSM-UHFFFAOYSA-N 0.000 description 1
- YZEVBZBPMBVPSU-UHFFFAOYSA-N NC(CCC1)OC1=O Chemical compound NC(CCC1)OC1=O YZEVBZBPMBVPSU-UHFFFAOYSA-N 0.000 description 1
- BBGZTSZVGWIYER-UHFFFAOYSA-N NC(CCCO1)C1=O Chemical compound NC(CCCO1)C1=O BBGZTSZVGWIYER-UHFFFAOYSA-N 0.000 description 1
- QJPWUUJVYOJNMH-UHFFFAOYSA-N NC(CCO1)C1=O Chemical compound NC(CCO1)C1=O QJPWUUJVYOJNMH-UHFFFAOYSA-N 0.000 description 1
- MFBFZXUSFVXOQA-UHFFFAOYSA-N NC(CO1)OC1=O Chemical compound NC(CO1)OC1=O MFBFZXUSFVXOQA-UHFFFAOYSA-N 0.000 description 1
- CEZBCWUICWDAJI-UHFFFAOYSA-N NC1Oc(cccc2)c2OC1 Chemical compound NC1Oc(cccc2)c2OC1 CEZBCWUICWDAJI-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB201018996A GB201018996D0 (en) | 2010-11-10 | 2010-11-10 | Novel ROCK inhibitors |
| GB1018996.7 | 2010-11-10 | ||
| PCT/EP2011/053343 WO2011107608A1 (en) | 2010-03-02 | 2011-03-04 | Heterocyclic amides as rock inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013527136A JP2013527136A (ja) | 2013-06-27 |
| JP2013527136A5 true JP2013527136A5 (ru) | 2014-02-13 |
| JP5710650B2 JP5710650B2 (ja) | 2015-04-30 |
Family
ID=43414658
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012555446A Expired - Fee Related JP5710650B2 (ja) | 2010-11-10 | 2011-03-04 | Ｒｏｃｋ阻害剤としての複素環アミド |
Country Status (3)
| Country | Link |
|---|---|
| JP (1) | JP5710650B2 (ru) |
| CN (2) | CN102884049B (ru) |
| GB (1) | GB201018996D0 (ru) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2846752A1 (en) * | 2011-08-31 | 2013-03-07 | Amakem Nv | Biphenylcarboxamides as rock kinase inhibitors |
| CN108191820A (zh) * | 2017-12-31 | 2018-06-22 | 佛山市赛维斯医药科技有限公司 | 一种含异丙胺和噻吩酰胺类结构的化合物 |
| CN108047195A (zh) * | 2017-12-31 | 2018-05-18 | 佛山市赛维斯医药科技有限公司 | 一种含丙二醇腈基噻吩酰胺类化合物及其用途 |
| CN107935986A (zh) * | 2017-12-31 | 2018-04-20 | 佛山市赛维斯医药科技有限公司 | 异丙胺和卤代噻吩酰胺类结构化合物、其制备方法及用途 |
| CN108047194A (zh) * | 2017-12-31 | 2018-05-18 | 佛山市赛维斯医药科技有限公司 | 含甲基萘和丙二醇噻吩酰胺类化合物、制备方法及其用途 |
| CN107915717A (zh) * | 2017-12-31 | 2018-04-17 | 佛山市赛维斯医药科技有限公司 | 一类含异丙基萘和丙二醇噻吩酰胺类化合物及其用途 |
| CN108101885A (zh) * | 2017-12-31 | 2018-06-01 | 佛山市赛维斯医药科技有限公司 | 含异丙胺和硝基噻吩酰胺类结构化合物、其制备方法及用途 |
| CN108129452A (zh) * | 2017-12-31 | 2018-06-08 | 佛山市赛维斯医药科技有限公司 | 一种含异丙基萘和丙二醇硝基噻吩酰胺类化合物及其用途 |
| CN108047193A (zh) * | 2017-12-31 | 2018-05-18 | 佛山市赛维斯医药科技有限公司 | 烷氧噻吩酰胺类rock抑制剂、制备方法及其用途 |
| CN107935987A (zh) * | 2017-12-31 | 2018-04-20 | 佛山市赛维斯医药科技有限公司 | 含甲基萘和噻吩酰胺结构的rock抑制剂、制备方法及其用途 |
| CN108191821A (zh) * | 2017-12-31 | 2018-06-22 | 佛山市赛维斯医药科技有限公司 | 一种含甲基萘和腈基噻吩酰胺类结构的rock抑制剂及用途 |
| CN114956977B (zh) * | 2022-06-09 | 2024-03-26 | 朗捷睿(苏州)生物科技有限公司 | 一种联苯类化合物、药物组合物及其制备方法和应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101248046A (zh) * | 2005-07-11 | 2008-08-20 | 德福根有限公司 | 作为激酶抑制剂的酰胺衍生物 |
| JP2009500437A (ja) * | 2005-07-11 | 2009-01-08 | デブジェン エヌブイ | キナーゼ阻害剤としてのアミド誘導体 |
| US20090233960A1 (en) * | 2005-10-13 | 2009-09-17 | Devgen Nv | Kinase Inhibitors |
| US8058271B2 (en) * | 2006-05-12 | 2011-11-15 | Vertex Pharmaceuticals Incorporated | Selective inhibitors of rock protein kinase and uses thereof |
| US8445686B2 (en) * | 2007-08-27 | 2013-05-21 | Abbvie Inc. | 4-(4-pyridinyl)-benzamides and their use as rock activity modulators |
| WO2010032875A2 (en) * | 2008-09-18 | 2010-03-25 | Astellas Pharma Inc. | Heterocyclic carboxamide compounds |
-
2010
- 2010-11-10 GB GB201018996A patent/GB201018996D0/en not_active Ceased
-
2011
- 2011-03-04 JP JP2012555446A patent/JP5710650B2/ja not_active Expired - Fee Related
- 2011-03-04 CN CN201180011949.6A patent/CN102884049B/zh not_active Expired - Fee Related
- 2011-03-04 CN CN2013102026660A patent/CN103316000A/zh active Pending
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