JP2016505042A5 - - Google Patents
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- Publication number
- JP2016505042A5 JP2016505042A5 JP2015553839A JP2015553839A JP2016505042A5 JP 2016505042 A5 JP2016505042 A5 JP 2016505042A5 JP 2015553839 A JP2015553839 A JP 2015553839A JP 2015553839 A JP2015553839 A JP 2015553839A JP 2016505042 A5 JP2016505042 A5 JP 2016505042A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heterocycle
- carbocycle
- nhco
- substituted
- 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
Links
- 125000000217 alkyl group Chemical group 0.000 claims 279
- 125000000623 heterocyclic group Chemical group 0.000 claims 107
- 125000003545 alkoxy group Chemical group 0.000 claims 48
- 229910052799 carbon Inorganic materials 0.000 claims 39
- 229910052757 nitrogen Inorganic materials 0.000 claims 33
- 229910052739 hydrogen Inorganic materials 0.000 claims 32
- 229910052736 halogen Inorganic materials 0.000 claims 27
- 150000002367 halogens Chemical class 0.000 claims 27
- 229910052760 oxygen Inorganic materials 0.000 claims 27
- 229910052717 sulfur Inorganic materials 0.000 claims 22
- 229910004013 NO 2 Inorganic materials 0.000 claims 16
- 125000002947 alkylene group Chemical group 0.000 claims 16
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 14
- 125000005842 heteroatom Chemical group 0.000 claims 13
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 11
- 125000004432 carbon atom Chemical group C* 0.000 claims 10
- 150000001721 carbon Chemical group 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 7
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 5
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 125000002837 carbocyclic group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 102000000568 rho-Associated Kinases Human genes 0.000 claims 3
- 108010041788 rho-Associated Kinases Proteins 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 210000002460 smooth muscle Anatomy 0.000 claims 2
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- -1 Kill Chemical group 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000031481 Pathologic Constriction Diseases 0.000 claims 1
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 206010047163 Vasospasm Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 208000026106 cerebrovascular disease Diseases 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000030603 inherited susceptibility to asthma Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000002981 neuropathic effect Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 208000037804 stenosis Diseases 0.000 claims 1
- 230000036262 stenosis Effects 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361754007P | 2013-01-18 | 2013-01-18 | |
| US61/754,007 | 2013-01-18 | ||
| PCT/US2014/011957 WO2014113620A2 (en) | 2013-01-18 | 2014-01-17 | Phthalazinones and isoquinolinones as rock inhibitors |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018242013A Division JP6770053B2 (ja) | 2013-01-18 | 2018-12-26 | Ｒｏｃｋ阻害剤としてのフタラジノンおよびイソキノリノン |
| JP2018242012A Division JP6622378B2 (ja) | 2013-01-18 | 2018-12-26 | Ｒｏｃｋ阻害剤としてのフタラジノンおよびイソキノリノン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016505042A JP2016505042A (ja) | 2016-02-18 |
| JP2016505042A5 true JP2016505042A5 (enExample) | 2017-02-16 |
| JP6488239B2 JP6488239B2 (ja) | 2019-03-20 |
Family
ID=50031626
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015553839A Expired - Fee Related JP6488239B2 (ja) | 2013-01-18 | 2014-01-17 | Ｒｏｃｋ阻害剤としてのフタラジノンおよびイソキノリノン |
| JP2018242012A Expired - Fee Related JP6622378B2 (ja) | 2013-01-18 | 2018-12-26 | Ｒｏｃｋ阻害剤としてのフタラジノンおよびイソキノリノン |
| JP2018242013A Expired - Fee Related JP6770053B2 (ja) | 2013-01-18 | 2018-12-26 | Ｒｏｃｋ阻害剤としてのフタラジノンおよびイソキノリノン |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018242012A Expired - Fee Related JP6622378B2 (ja) | 2013-01-18 | 2018-12-26 | Ｒｏｃｋ阻害剤としてのフタラジノンおよびイソキノリノン |
| JP2018242013A Expired - Fee Related JP6770053B2 (ja) | 2013-01-18 | 2018-12-26 | Ｒｏｃｋ阻害剤としてのフタラジノンおよびイソキノリノン |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US9221767B2 (enExample) |
| EP (3) | EP3252050B1 (enExample) |
| JP (3) | JP6488239B2 (enExample) |
| CN (1) | CN105073741B (enExample) |
| BR (1) | BR112015017008A2 (enExample) |
| CA (1) | CA2898440A1 (enExample) |
| EA (3) | EA034395B1 (enExample) |
| ES (2) | ES2684776T3 (enExample) |
| HK (1) | HK1212979A1 (enExample) |
| MX (1) | MX2015008741A (enExample) |
| TW (1) | TW201443023A (enExample) |
| WO (1) | WO2014113620A2 (enExample) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9221767B2 (en) | 2013-01-18 | 2015-12-29 | Bristol-Myers Squibb Company | Substituted phthalazinones as rock inhibitors |
| AR094929A1 (es) | 2013-02-28 | 2015-09-09 | Bristol Myers Squibb Co | Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2 |
| US9828345B2 (en) | 2013-02-28 | 2017-11-28 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent ROCK1 and ROCK2 inhibitors |
| US9902702B2 (en) | 2014-07-15 | 2018-02-27 | Bristol-Myers Squibb Company | Spirocycloheptanes as inhibitors of rock |
| 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 |
| ES2815681T3 (es) | 2015-01-09 | 2021-03-30 | Bristol Myers Squibb Co | Ureas cíclicas como inhibidores de ROCK |
| WO2016138533A2 (en) | 2015-02-27 | 2016-09-01 | The Regents Of The University Of California | Small molecules that enable cartilage rejuvanation |
| TW201706265A (zh) | 2015-03-09 | 2017-02-16 | 必治妥美雅史谷比公司 | 做為Ｒｈｏ激酶（ＲＯＣＫ）抑制劑之內醯胺 |
| US11046670B2 (en) | 2015-10-19 | 2021-06-29 | Board Of Regents, The University Of Texas System | Piperazinyl norbenzomorphan compounds and methods for using the same |
| CN105232542B (zh) * | 2015-11-10 | 2016-03-30 | 王秀珍 | 一种治疗小儿肺炎的药物组合物 |
| CN106928252B (zh) * | 2015-12-31 | 2019-09-27 | 成都先导药物开发股份有限公司 | 一种抑制rock的化合物及其制备方法与应用 |
| UY37073A (es) | 2016-01-13 | 2017-07-31 | Bristol-Myers Squibb Company Una Corporación Del Estado De Delaware | Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock, y las composiciones que los contienen |
| IL293496B2 (en) | 2016-03-28 | 2023-05-01 | Incyte Corp | Pyrrolotriazine compounds as TAM inhibitors |
| AU2017257153A1 (en) * | 2016-04-29 | 2018-11-22 | Board Of Regents, The University Of Texas System | Sigma receptor binders |
| US10562887B2 (en) | 2016-05-27 | 2020-02-18 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of ROCK |
| JP6903731B2 (ja) * | 2016-07-07 | 2021-07-14 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 強力で選択的なｒｏｃｋ阻害剤としてのラクタム、環状尿素、およびカルバメート、およびトリアゾロン誘導体 |
| KR102491994B1 (ko) | 2016-07-07 | 2023-01-25 | 브리스톨-마이어스 스큅 컴퍼니 | Rock의 억제제로서의 스피로락탐 |
| US10787450B2 (en) | 2016-07-07 | 2020-09-29 | Bristol-Myers Squibb Company | Spiro-fused cyclic ureas as inhibitors of rock |
| US10654860B2 (en) | 2016-11-30 | 2020-05-19 | Bristol-Myers Squibb Company | Tricyclic rho kinase inhibitors |
| US12060341B2 (en) | 2017-07-12 | 2024-08-13 | Bristol-Myers Squibb Company | Spiroheptanyl hydantoins as ROCK inhibitors |
| 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 |
| ES2894128T3 (es) | 2017-07-12 | 2022-02-11 | Bristol Myers Squibb Co | Inhibidores aminoheterocíclicos de cinco miembros y aminoheterocíclicos bicíclicos de 5,6 o 6,6 miembros de ROCK para el tratamiento de la insuficiencia cardíaca |
| EP3652164B1 (en) | 2017-07-12 | 2023-06-21 | Bristol-Myers Squibb Company | Phenylacetamides as inhibitors of rock |
| CN110914257B (zh) | 2017-07-12 | 2023-05-26 | 百时美施贵宝公司 | 作为rock抑制剂的螺庚基乙内酰脲 |
| WO2019089868A1 (en) | 2017-11-03 | 2019-05-09 | Bristol-Myers Squibb Company | Diazaspiro rock inhibitors |
| SG11202100531RA (en) | 2018-09-17 | 2021-02-25 | Yungjin Pharm Co Ltd | Novel thiazole derivatives and pharmaceutically acceptable salts thereof |
| WO2020228436A1 (zh) * | 2019-05-10 | 2020-11-19 | 浙江海正药业股份有限公司 | 芳环或杂芳环类衍生物及其制备方法和用途 |
| CN110041328A (zh) * | 2019-05-22 | 2019-07-23 | 南京合巨药业有限公司 | 一种5-氟-1H-吡咯并[2,3-b]吡啶-3-羧酸的制备方法 |
| KR102682428B1 (ko) * | 2020-05-08 | 2024-07-05 | 주식회사 티씨노바이오사이언스 | 엑토뉴클레오티드 피로포스파타아제-포스포디에스터라아제의 저해 활성을 갖는 신규한 프탈라진 유도체 및 이들의 용도 |
| WO2022003610A1 (en) | 2020-07-02 | 2022-01-06 | Pi Industries Ltd. | 2-(4,5-dihydroisoxazol-3-yl)isoindoline-5-carboxamide derivatives and similar compounds as pesticides for crop protection |
| US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
| US20230391739A1 (en) * | 2020-11-24 | 2023-12-07 | Katholieke Universiteit Leuven | Aryl derivatives for treating trpm3 mediated disorders |
| CN114106211A (zh) * | 2021-08-31 | 2022-03-01 | 海南医学院 | 一种云南鸡油菌多糖及其分离纯化方法 |
| UY39932A (es) | 2021-09-08 | 2023-03-31 | Pi Industries Ltd | Compuestos de isoxazolina y su uso como agentes de control de plagas. |
| 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 |
| AR129420A1 (es) * | 2022-05-25 | 2024-08-21 | Univ Leuven Kath | Nuevos derivados para tratar trastornos mediados por trpm3 |
| TW202413357A (zh) * | 2022-05-25 | 2024-04-01 | 天主教魯汶大學 | 用於治療ＴＲＰＭ３介導之病症的吡唑并［１，５－ａ］吡啶衍生物 |
| WO2024216197A2 (en) * | 2023-04-13 | 2024-10-17 | Acelot, Inc. | Compounds and methods for treating protein aggregation diseases |
| CN119528827A (zh) * | 2023-08-31 | 2025-02-28 | 北京五和博澳药业股份有限公司 | 一种酞嗪酮类化合物及其制备方法、药物组合物及用途 |
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| US9221767B2 (en) | 2013-01-18 | 2015-12-29 | Bristol-Myers Squibb Company | Substituted phthalazinones as rock inhibitors |
| CN103242647B (zh) | 2013-04-27 | 2015-06-17 | 大连理工大学 | 一种阻燃耐热聚氨酯泡沫塑料及其制备方法 |
-
2014
- 2014-01-17 US US14/157,564 patent/US9221767B2/en active Active
- 2014-01-17 EP EP17176983.9A patent/EP3252050B1/en active Active
- 2014-01-17 HK HK16100934.1A patent/HK1212979A1/zh unknown
- 2014-01-17 EA EA201891501A patent/EA034395B1/ru not_active IP Right Cessation
- 2014-01-17 EA EA201790202A patent/EA033220B1/ru not_active IP Right Cessation
- 2014-01-17 WO PCT/US2014/011957 patent/WO2014113620A2/en not_active Ceased
- 2014-01-17 EP EP14702408.7A patent/EP2945943B1/en active Active
- 2014-01-17 EP EP17176975.5A patent/EP3252049A1/en not_active Withdrawn
- 2014-01-17 ES ES14702408.7T patent/ES2684776T3/es active Active
- 2014-01-17 CA CA2898440A patent/CA2898440A1/en not_active Abandoned
- 2014-01-17 CN CN201480016485.1A patent/CN105073741B/zh not_active Expired - Fee Related
- 2014-01-17 TW TW103101887A patent/TW201443023A/zh unknown
- 2014-01-17 US US14/759,495 patent/US9926282B2/en active Active
- 2014-01-17 JP JP2015553839A patent/JP6488239B2/ja not_active Expired - Fee Related
- 2014-01-17 BR BR112015017008A patent/BR112015017008A2/pt not_active Application Discontinuation
- 2014-01-17 EA EA201591296A patent/EA027138B1/ru not_active IP Right Cessation
- 2014-01-17 MX MX2015008741A patent/MX2015008741A/es active IP Right Grant
- 2014-01-17 ES ES17176983T patent/ES2785498T3/es active Active
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2018
- 2018-02-07 US US15/890,436 patent/US10385026B2/en active Active
- 2018-12-26 JP JP2018242012A patent/JP6622378B2/ja not_active Expired - Fee Related
- 2018-12-26 JP JP2018242013A patent/JP6770053B2/ja not_active Expired - Fee Related