CN110023291B - 三环rho激酶抑制剂 - Google Patents

三环rho激酶抑制剂 Download PDF

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CN110023291B
CN110023291B CN201780073847.4A CN201780073847A CN110023291B CN 110023291 B CN110023291 B CN 110023291B CN 201780073847 A CN201780073847 A CN 201780073847A CN 110023291 B CN110023291 B CN 110023291B
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CN110023291A (zh
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杨武
P·W·格伦茨
R·S·布海德
K·蒂亚加拉扬
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Bristol Myers Squibb Co
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    • C07—ORGANIC CHEMISTRY
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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom

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  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Ophthalmology & Optometry (AREA)
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CN201780073847.4A 2016-11-30 2017-11-29 三环rho激酶抑制剂 Active CN110023291B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662427875P 2016-11-30 2016-11-30
US62/427,875 2016-11-30
PCT/US2017/063554 WO2018102325A1 (en) 2016-11-30 2017-11-29 Tricyclic rho kinase inhibitors

Publications (2)

Publication Number Publication Date
CN110023291A CN110023291A (zh) 2019-07-16
CN110023291B true CN110023291B (zh) 2023-07-18

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US (1) US10654860B2 (enExample)
EP (1) EP3548468B1 (enExample)
JP (1) JP7191826B2 (enExample)
KR (1) KR102511441B1 (enExample)
CN (1) CN110023291B (enExample)
ES (1) ES2829400T3 (enExample)
WO (1) WO2018102325A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR107354A1 (es) 2016-01-13 2018-04-18 Bristol Myers Squibb Co Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock
JP6987792B2 (ja) 2016-05-27 2022-01-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Ｒｏｃｋ阻害剤としてのトリアゾロンおよびテトラゾロン
ES2829550T3 (es) 2016-07-07 2021-06-01 Bristol Myers Squibb Co Ureas cíclicas espiro-condensadas como inhibidores de 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
ES2821877T3 (es) 2016-07-07 2021-04-28 Bristol Myers Squibb Co Espirolactamas como inhibidores de ROCK
KR102511441B1 (ko) 2016-11-30 2023-03-16 브리스톨-마이어스 스큅 컴퍼니 트리시클릭 Rho 키나제 억제제
JP7206253B2 (ja) 2017-07-12 2023-01-17 ブリストル－マイヤーズ スクイブ カンパニー Ｒｏｃｋ阻害剤としてのフェニルアセトアミド
TW201908293A (zh) 2017-07-12 2019-03-01 美商必治妥美雅史谷比公司 作為rock抑制劑之5員及雙環雜環醯胺
US12060341B2 (en) 2017-07-12 2024-08-13 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as ROCK inhibitors
JP7313331B2 (ja) 2017-07-12 2023-07-24 ブリストル－マイヤーズ スクイブ カンパニー Ｒｏｃｋ阻害剤としてのスピロヘプタニルヒダントイン
KR102680160B1 (ko) 2017-07-12 2024-06-28 브리스톨-마이어스 스큅 컴퍼니 심부전의 치료를 위한 rock의 5원-아미노헤테로사이클 및 5,6- 또는 6,6-원 비시클릭 아미노헤테로시클릭 억제제
WO2019089868A1 (en) 2017-11-03 2019-05-09 Bristol-Myers Squibb Company Diazaspiro rock inhibitors
WO2023085369A1 (ja) 2021-11-11 2023-05-19 学校法人同志社 角膜内皮細胞の凍結保存製剤およびその製造法

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1418870A (zh) * 2001-10-10 2003-05-21 第一制糖株式会社 作为环加氧酶－2的高选择性抑制剂的3，4－二氢－1h－萘类衍生物
CN1893943A (zh) * 2003-10-03 2007-01-10 3M创新有限公司 吡唑并吡啶和其类似物
CN102977095A (zh) * 2012-12-03 2013-03-20 华东理工大学 吡唑并喹啉类化合物及其用途
CN105102448A (zh) * 2013-02-28 2015-11-25 百时美施贵宝公司 作为强效rock1和rock2抑制剂的苯基吡唑衍生物
CN105358547A (zh) * 2013-02-28 2016-02-24 百时美施贵宝公司 作为强效rock1和rock2抑制剂的苯基吡唑衍生物
CN105492444A (zh) * 2013-07-02 2016-04-13 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
CN105518005A (zh) * 2013-07-02 2016-04-20 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
CN107406426A (zh) * 2015-01-09 2017-11-28 百时美施贵宝公司 作为rock抑制剂的环状脲类

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090075980A1 (en) * 2003-10-03 2009-03-19 Coley Pharmaceutical Group, Inc. Pyrazolopyridines and Analogs Thereof
EP1713775A4 (en) 2004-01-30 2009-08-12 Smithkline Beecham Corp CHEMICAL COMPOUNDS
WO2006107771A2 (en) * 2005-04-01 2006-10-12 Coley Pharmaceutical Group, Inc. PYRAZOLO[3,4-c]QUINOLINES, PYRAZOLO[3,4-c]NAPHTHYRIDINES, ANALOGS THEREOF, AND METHODS
CA2898440A1 (en) 2013-01-18 2014-07-24 Bristol-Myers Squibb Company Phthalazinones and isoquinolinones as rock inhibitors
US9902702B2 (en) 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
JP6633618B2 (ja) 2014-08-21 2020-01-22 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 強力なｒｏｃｋ阻害剤としてのタイドバックのベンズアミド誘導体
WO2016144936A1 (en) 2015-03-09 2016-09-15 Bristol-Myers Squibb Company Lactams as inhibitors of rock
AR107354A1 (es) 2016-01-13 2018-04-18 Bristol Myers Squibb Co Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock
JP6987792B2 (ja) 2016-05-27 2022-01-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Ｒｏｃｋ阻害剤としてのトリアゾロンおよびテトラゾロン
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
ES2829550T3 (es) 2016-07-07 2021-06-01 Bristol Myers Squibb Co Ureas cíclicas espiro-condensadas como inhibidores de ROCK
ES2821877T3 (es) 2016-07-07 2021-04-28 Bristol Myers Squibb Co Espirolactamas como inhibidores de ROCK
KR102511441B1 (ko) 2016-11-30 2023-03-16 브리스톨-마이어스 스큅 컴퍼니 트리시클릭 Rho 키나제 억제제
TW201908293A (zh) 2017-07-12 2019-03-01 美商必治妥美雅史谷比公司 作為rock抑制劑之5員及雙環雜環醯胺
KR102680160B1 (ko) 2017-07-12 2024-06-28 브리스톨-마이어스 스큅 컴퍼니 심부전의 치료를 위한 rock의 5원-아미노헤테로사이클 및 5,6- 또는 6,6-원 비시클릭 아미노헤테로시클릭 억제제
JP7313331B2 (ja) 2017-07-12 2023-07-24 ブリストル－マイヤーズ スクイブ カンパニー Ｒｏｃｋ阻害剤としてのスピロヘプタニルヒダントイン
JP7206253B2 (ja) 2017-07-12 2023-01-17 ブリストル－マイヤーズ スクイブ カンパニー Ｒｏｃｋ阻害剤としてのフェニルアセトアミド
WO2019089868A1 (en) 2017-11-03 2019-05-09 Bristol-Myers Squibb Company Diazaspiro rock inhibitors

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1418870A (zh) * 2001-10-10 2003-05-21 第一制糖株式会社 作为环加氧酶－2的高选择性抑制剂的3，4－二氢－1h－萘类衍生物
CN1893943A (zh) * 2003-10-03 2007-01-10 3M创新有限公司 吡唑并吡啶和其类似物
CN102977095A (zh) * 2012-12-03 2013-03-20 华东理工大学 吡唑并喹啉类化合物及其用途
CN105102448A (zh) * 2013-02-28 2015-11-25 百时美施贵宝公司 作为强效rock1和rock2抑制剂的苯基吡唑衍生物
CN105358547A (zh) * 2013-02-28 2016-02-24 百时美施贵宝公司 作为强效rock1和rock2抑制剂的苯基吡唑衍生物
CN105492444A (zh) * 2013-07-02 2016-04-13 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
CN105518005A (zh) * 2013-07-02 2016-04-20 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
CN107406426A (zh) * 2015-01-09 2017-11-28 百时美施贵宝公司 作为rock抑制剂的环状脲类

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
《Discovery of potent and selective urea-based ROCK inhibitors:Exploring the inhibitor’s potency and ROCK2/PKA selectivity by 3D-QSAR, molecular docking and molecular dynamics simulations》;Ding Mei等;《Bioorganic & Medicinal Chemistry》;20150325(第23期);全文 *

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