JPWO2019213151A5 - - Google Patents
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- JPWO2019213151A5 JPWO2019213151A5 JP2020560258A JP2020560258A JPWO2019213151A5 JP WO2019213151 A5 JPWO2019213151 A5 JP WO2019213151A5 JP 2020560258 A JP2020560258 A JP 2020560258A JP 2020560258 A JP2020560258 A JP 2020560258A JP WO2019213151 A5 JPWO2019213151 A5 JP WO2019213151A5
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- JP
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- Prior art keywords
- alkyl
- substituted
- compound according
- compound
- hydrogen
- 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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- 150000001875 compounds Chemical class 0.000 claims description 98
- 125000000217 alkyl group Chemical group 0.000 claims description 70
- 229910052739 hydrogen Inorganic materials 0.000 claims description 37
- 239000001257 hydrogen Substances 0.000 claims description 34
- -1 4- (4- (3- (2- (4-chlorophenyl) -1-isopropyl-5-methyl-4- (methylsulfonyl) -1H-pyrrole-3-yl) -5-fluorophenyl) Piperazine-1-yl) phenyl Chemical group 0.000 claims description 20
- 229910052736 halogen Inorganic materials 0.000 claims description 14
- 150000002367 halogens Chemical class 0.000 claims description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 13
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 9
- 229910052760 oxygen Inorganic materials 0.000 claims description 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 5
- 229910052717 sulfur Inorganic materials 0.000 claims description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-M dihydrogenphosphate Chemical compound OP(O)([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-M 0.000 claims description 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims 5
- 125000000547 substituted alkyl group Chemical group 0.000 description 32
- 150000002431 hydrogen Chemical class 0.000 description 21
- 125000001072 heteroaryl group Chemical group 0.000 description 20
- 125000000623 heterocyclic group Chemical group 0.000 description 18
- 125000003118 aryl group Chemical group 0.000 description 12
- 230000032683 aging Effects 0.000 description 8
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 8
- 239000000203 mixture Substances 0.000 description 8
- 125000003107 substituted aryl group Chemical group 0.000 description 8
- 206010028980 Neoplasm Diseases 0.000 description 7
- 201000011510 cancer Diseases 0.000 description 7
- 125000000392 cycloalkenyl group Chemical group 0.000 description 7
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 125000005415 substituted alkoxy group Chemical group 0.000 description 6
- 125000003342 alkenyl group Chemical group 0.000 description 5
- 125000003545 alkoxy group Chemical group 0.000 description 5
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 description 5
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 5
- 125000004093 cyano group Chemical group *C#N 0.000 description 5
- 125000000753 cycloalkyl group Chemical group 0.000 description 5
- 125000004663 dialkyl amino group Chemical group 0.000 description 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 5
- 125000002373 5 membered heterocyclic group Chemical group 0.000 description 4
- 125000004070 6 membered heterocyclic group Chemical group 0.000 description 4
- 125000003282 alkyl amino group Chemical group 0.000 description 4
- 125000000304 alkynyl group Chemical group 0.000 description 4
- 229910052757 nitrogen Inorganic materials 0.000 description 4
- 125000004426 substituted alkynyl group Chemical group 0.000 description 4
- 125000005647 linker group Chemical group 0.000 description 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 125000001424 substituent group Chemical group 0.000 description 3
- 125000005017 substituted alkenyl group Chemical group 0.000 description 3
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 3
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 3
- PIGFYZPCRLYGLF-UHFFFAOYSA-N Aluminum nitride Chemical compound [Al]#N PIGFYZPCRLYGLF-UHFFFAOYSA-N 0.000 description 2
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 description 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 2
- 125000004644 alkyl sulfinyl group Chemical group 0.000 description 2
- 125000004414 alkyl thio group Chemical group 0.000 description 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 description 2
- 125000005163 aryl sulfanyl group Chemical group 0.000 description 2
- 125000004104 aryloxy group Chemical group 0.000 description 2
- 125000001589 carboacyl group Chemical group 0.000 description 2
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 230000001404 mediated effect Effects 0.000 description 2
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 125000005138 alkoxysulfonyl group Chemical group 0.000 description 1
- 125000004688 alkyl sulfonyl alkyl group Chemical group 0.000 description 1
- 125000002947 alkylene group Chemical group 0.000 description 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 description 1
- 125000003710 aryl alkyl group Chemical group 0.000 description 1
- 125000005160 aryl oxy alkyl group Chemical group 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 description 1
- 125000004181 carboxyalkyl group Chemical group 0.000 description 1
- 125000000000 cycloalkoxy group Chemical group 0.000 description 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 125000004438 haloalkoxy group Chemical group 0.000 description 1
- 125000001188 haloalkyl group Chemical group 0.000 description 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 1
- 125000005326 heteroaryloxy alkyl group Chemical group 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 125000005338 substituted cycloalkoxy group Chemical group 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 150000003512 tertiary amines Chemical class 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862664891P | 2018-04-30 | 2018-04-30 | |
| US201862664850P | 2018-04-30 | 2018-04-30 | |
| US201862664860P | 2018-04-30 | 2018-04-30 | |
| US201862664863P | 2018-04-30 | 2018-04-30 | |
| US62/664,860 | 2018-04-30 | ||
| US62/664,863 | 2018-04-30 | ||
| US62/664,850 | 2018-04-30 | ||
| US62/664,891 | 2018-04-30 | ||
| PCT/US2019/030023 WO2019213151A1 (en) | 2018-04-30 | 2019-04-30 | Phosphonamidates that are bcl family antagonists for use in clinical management of conditions caused or mediated by senescent cells and for treating cancer |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021522270A JP2021522270A (ja) | 2021-08-30 |
| JP2021522270A5 JP2021522270A5 (https=) | 2022-04-20 |
| JPWO2019213151A5 true JPWO2019213151A5 (https=) | 2022-04-20 |
| JP7080346B2 JP7080346B2 (ja) | 2022-06-03 |
Family
ID=66530472
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020560258A Active JP7080346B2 (ja) | 2018-04-30 | 2019-04-30 | 老化細胞によって引き起こされるかまたは媒介される状態の臨床管理における使用のためおよびがんを治療するための、Ｂｃｌファミリーアンタゴニストであるホスホノアミダート |
| JP2020561053A Active JP7204780B2 (ja) | 2018-04-30 | 2019-04-30 | 老化細胞によって引き起こされるかまたは媒介される状態の臨床管理における使用のためおよびがんを治療するための、Ｂｃｌファミリーアンタゴニストであるアシルホスホノアミダートおよびアシルベンジルアミン |
| JP2020561057A Expired - Fee Related JP7089062B2 (ja) | 2018-04-30 | 2019-04-30 | 老化細胞によって引き起こされるかまたは媒介される状態の臨床管理における使用のためおよびがんを治療するための、Ｂｃｌファミリーアンタゴニストであるホスホリジン |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020561053A Active JP7204780B2 (ja) | 2018-04-30 | 2019-04-30 | 老化細胞によって引き起こされるかまたは媒介される状態の臨床管理における使用のためおよびがんを治療するための、Ｂｃｌファミリーアンタゴニストであるアシルホスホノアミダートおよびアシルベンジルアミン |
| JP2020561057A Expired - Fee Related JP7089062B2 (ja) | 2018-04-30 | 2019-04-30 | 老化細胞によって引き起こされるかまたは媒介される状態の臨床管理における使用のためおよびがんを治療するための、Ｂｃｌファミリーアンタゴニストであるホスホリジン |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10703745B2 (https=) |
| EP (3) | EP3787626B1 (https=) |
| JP (3) | JP7080346B2 (https=) |
| CN (4) | CN112513057B (https=) |
| WO (3) | WO2019213160A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020140005A2 (en) | 2018-12-29 | 2020-07-02 | Newave Pharmaceutical Inc. | Bcl-2 inhibitors |
| EP3906235B1 (en) | 2019-01-04 | 2023-03-15 | Ascentage Pharma (Suzhou) Co., Ltd. | Method for preparing sulfonamides drugs |
| CN113248415B (zh) * | 2021-05-26 | 2022-08-09 | 苏州正永生物医药有限公司 | 一种abt-737关键中间体的制备方法以及abt-737的制备方法 |
| CN118717761A (zh) * | 2024-05-27 | 2024-10-01 | 复旦大学 | 瑞美吉泮在制备治疗/预防阿尔茨海默病药物中的应用 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5807846A (en) | 1996-11-14 | 1998-09-15 | Warner-Lambert Company | Phosphonamide ACAT inhibitors |
| HUP0200260A3 (en) * | 1999-03-05 | 2002-11-28 | Metabasis Therapeutics Inc San | Novel phosphorus-containing prodrugs, their preparation and their use |
| WO2003000188A2 (en) | 2001-06-21 | 2003-01-03 | Ariad Pharmaceuticals, Inc. | Novel quinazolines and uses thereof |
| EP1575591A4 (en) | 2002-12-23 | 2007-09-12 | Ariad Pharma Inc | HETEROCYCLES AND ITS USE |
| AU2006223257A1 (en) * | 2005-03-11 | 2006-09-21 | The Regents Of The University Of Michigan | Chromen-4-one inhibitors of anti-apoptotic Bcl-2 family members and the uses thereof |
| US7834023B2 (en) * | 2006-09-20 | 2010-11-16 | Portola Pharmaceuticals, Inc. | Substituted dihydroquinazolines as platelet ADP receptor inhibitors |
| WO2008100423A1 (en) * | 2007-02-09 | 2008-08-21 | Sirtris Pharmaceuticals, Inc. | Gut microsomal triglyceride transport protein inhibitors |
| US8124605B2 (en) * | 2007-07-06 | 2012-02-28 | Kinex Pharmaceuticals, Llc | Compositions and methods for modulating a kinase cascade |
| US8563735B2 (en) | 2008-12-05 | 2013-10-22 | Abbvie Inc. | Bcl-2-selective apoptosis-inducing agents for the treatment of cancer and immune diseases |
| TWI535712B (zh) | 2010-08-06 | 2016-06-01 | 阿斯特捷利康公司 | 化合物 |
| CA2822039C (en) | 2010-12-16 | 2019-05-28 | Allergan, Inc. | Sulfur derivatives as chemokine receptor modulators |
| SG192126A1 (en) | 2011-01-25 | 2013-09-30 | Univ Michigan | Bcl-2/bcl-xl inhibitors and therapeutic methods using the same |
| US20140189897A1 (en) | 2011-06-21 | 2014-07-03 | Mayo Foundation For Medical Education And Research | Transgenic animals capable of being induced to delete senescent cells |
| WO2013052943A2 (en) * | 2011-10-06 | 2013-04-11 | The Regents Of The University Of Michgian | Small molecule inhibitors of mcl-1 and uses thereof |
| US9901080B2 (en) | 2012-08-23 | 2018-02-27 | Buck Institute For Research On Aging | Transgenic mouse having a transgene that converts a prodrug into a cytotoxic compound in senescent cells |
| EP2922544B1 (en) | 2012-11-21 | 2018-08-01 | Eutropics Pharmaceuticals, Inc. | Methods and compositions useful for treating diseases involving bcl-2 family proteins with quinoline derivatives |
| KR102318204B1 (ko) | 2013-01-16 | 2021-10-26 | 더 리젠츠 오브 더 유니버시티 오브 미시간 | Bcl-2bcl-xl 억제제 및 그를 사용하는 치료 방법 |
| CN105377289A (zh) | 2013-04-21 | 2016-03-02 | 耶达研究及发展有限公司 | 用于下调Bcl-xL和/或Bcl-w的活性和/或量的试剂 |
| US10328058B2 (en) * | 2014-01-28 | 2019-06-25 | Mayo Foundation For Medical Education And Research | Treating atherosclerosis by removing senescent foam cell macrophages from atherosclerotic plaques |
| US20170216286A1 (en) | 2014-01-28 | 2017-08-03 | Mayo Foundation For Medical Education And Research | Killing senescent cells and treating senescence-associated conditions using a src inhibitor and a flavonoid |
| AU2015211021B2 (en) | 2014-01-28 | 2020-07-02 | Buck Institute For Research On Aging | Methods and compositions for killing senescent cells and for treating senescence-associated diseases and disorders |
| EP3125943B1 (en) | 2014-04-04 | 2026-04-22 | Merck Sharp & Dohme LLC | Phosphate based linkers for intracellular delivery of drug conjugates |
| EP3139942B1 (en) | 2014-05-05 | 2019-12-18 | Bioventures, Llc | COMPOSITIONS AND METHODS FOR INHIBITING ANTIAPOPTOTIC Bcl-2 PROTEINS AS ANTI-AGING AGENTS |
| US20180000816A1 (en) * | 2015-02-06 | 2018-01-04 | Unity Biotechnology, Inc. | Use of a Heterocyclic Bcl-xL Inhibitor and Related Analogs for Removing Senescent Cells in the Treatment of Eye Diseases and Other Age-Related Conditions |
| CA2981753A1 (en) * | 2015-02-06 | 2016-08-11 | Unity Biotechnology, Inc. | Compounds and uses in treatment of senescence-associated conditions |
| US10195213B2 (en) | 2015-03-13 | 2019-02-05 | Unity Biotechnology, Inc. | Chemical entities that kill senescent cells for use in treating age-related disease |
| CN107846899A (zh) | 2015-07-15 | 2018-03-27 | 拜耳农作物科学股份公司 | 取代的氧代四氢喹啉基次膦酰胺和‑膦酰胺或其盐及其提高植物中的胁迫耐受性的用途 |
| CN105646587B (zh) * | 2016-03-02 | 2018-03-23 | 云南中医学院 | 1,3,2‑氧氮磷杂环戊烷类化合物、制备方法及应用 |
| WO2019001171A1 (zh) | 2017-06-27 | 2019-01-03 | 维眸生物科技上海有限公司 | 一种含磷化合物及其制备和应用 |
| WO2019033122A1 (en) | 2017-08-11 | 2019-02-14 | Unity Biotechnology, Inc. | TREATMENT OF PULMONARY DISEASES USING PHARMACEUTICAL AGENTS THAT ELIMINATE SENESCENT CELLS |
| EP3441069B1 (en) | 2017-08-11 | 2023-04-05 | Unity Biotechnology, Inc. | Treatment of diabetic retinopathy using pharmaceutical agents that eliminate senescent cells |
-
2019
- 2019-04-30 JP JP2020560258A patent/JP7080346B2/ja active Active
- 2019-04-30 JP JP2020561053A patent/JP7204780B2/ja active Active
- 2019-04-30 EP EP19797087.4A patent/EP3787626B1/en active Active
- 2019-04-30 CN CN201980034704.1A patent/CN112513057B/zh active Active
- 2019-04-30 WO PCT/US2019/030039 patent/WO2019213160A1/en not_active Ceased
- 2019-04-30 CN CN202410023605.6A patent/CN117866015A/zh active Pending
- 2019-04-30 EP EP19723963.5A patent/EP3788054B1/en active Active
- 2019-04-30 EP EP19796304.4A patent/EP3788052A4/en not_active Withdrawn
- 2019-04-30 CN CN201980034780.2A patent/CN112469411B/zh active Active
- 2019-04-30 JP JP2020561057A patent/JP7089062B2/ja not_active Expired - Fee Related
- 2019-04-30 CN CN201980002328.8A patent/CN110662752B/zh active Active
- 2019-04-30 WO PCT/US2019/030023 patent/WO2019213151A1/en not_active Ceased
- 2019-04-30 WO PCT/US2019/030028 patent/WO2019213153A1/en not_active Ceased
- 2019-05-29 US US16/425,665 patent/US10703745B2/en active Active
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