JP2014507421A5 - - Google Patents
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- Publication number
- JP2014507421A5 JP2014507421A5 JP2013551282A JP2013551282A JP2014507421A5 JP 2014507421 A5 JP2014507421 A5 JP 2014507421A5 JP 2013551282 A JP2013551282 A JP 2013551282A JP 2013551282 A JP2013551282 A JP 2013551282A JP 2014507421 A5 JP2014507421 A5 JP 2014507421A5
- Authority
- JP
- Japan
- Prior art keywords
- conr
- alkyl
- cycloalkyl
- ring
- 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 9
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 5
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 5
- 102100021569 Apoptosis regulator Bcl-2 Human genes 0.000 claims 2
- 102100026596 Bcl-2-like protein 1 Human genes 0.000 claims 2
- 101000971171 Homo sapiens Apoptosis regulator Bcl-2 Proteins 0.000 claims 2
- 230000009286 beneficial effect Effects 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- -1 CF 3 Chemical group 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- CKUAXEQHGKSLHN-UHFFFAOYSA-N [C].[N] Chemical group [C].[N] CKUAXEQHGKSLHN-UHFFFAOYSA-N 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 238000010276 construction Methods 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000011287 therapeutic dose Methods 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161436077P | 2011-01-25 | 2011-01-25 | |
| US61/436,077 | 2011-01-25 | ||
| PCT/US2012/022315 WO2012103059A2 (en) | 2011-01-25 | 2012-01-24 | Bcl-2/bcl-xl inhibitors and therapeutic methods using the same |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014507421A JP2014507421A (ja) | 2014-03-27 |
| JP2014507421A5 true JP2014507421A5 (enExample) | 2016-01-28 |
| JP5998152B2 JP5998152B2 (ja) | 2016-09-28 |
Family
ID=46544312
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013551282A Active JP5998152B2 (ja) | 2011-01-25 | 2012-01-24 | Ｂｃｌ−２／ｂｃｌ−ｘｌ阻害剤およびそれを使用する治療方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8691184B2 (enExample) |
| EP (2) | EP2668180B1 (enExample) |
| JP (1) | JP5998152B2 (enExample) |
| KR (1) | KR101762724B1 (enExample) |
| CN (1) | CN103562202B (enExample) |
| AU (1) | AU2012209295B2 (enExample) |
| CA (1) | CA2825306C (enExample) |
| ES (1) | ES2693107T3 (enExample) |
| SG (1) | SG192126A1 (enExample) |
| WO (1) | WO2012103059A2 (enExample) |
| ZA (1) | ZA201305571B (enExample) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6347793B2 (ja) * | 2013-01-16 | 2018-06-27 | ザ リージェンツ オブ ザ ユニバーシティー オブ ミシガン | Ｂｃｌ−２／Ｂｃｌ−ｘＬ阻害薬およびそれを使用した治療方法 |
| US20160122758A1 (en) * | 2013-04-21 | 2016-05-05 | Yeda Research And Development Co. Ltd. | Agents for downregulation of the activity and/or amount of bcl-xl and/or bcl-w |
| US20190269675A1 (en) | 2014-01-28 | 2019-09-05 | Buck Institute for Research and Aging | Treatment of parkinson's disease and other conditions caused or mediated by senescent astrocytes using small molecule senolytic agents |
| 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 |
| IL311537A (en) | 2014-01-28 | 2024-05-01 | Mayo Found Medical Education & Res | Methods and preparations for killing aging cells and for the treatment of diseases and disorders related to aging |
| 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 |
| WO2016107603A1 (zh) * | 2015-01-01 | 2016-07-07 | 成都贝斯凯瑞生物科技有限公司 | 取代氮杂环衍生物及其应用 |
| WO2016127135A1 (en) * | 2015-02-06 | 2016-08-11 | Unity Biotechnology, Inc. | Compounds and uses in treatment of senescence-associated conditons |
| WO2016135732A1 (en) | 2015-02-26 | 2016-09-01 | Yeda Research And Development Co. Ltd. | Method of promoting hair growth |
| EP3334725B1 (en) | 2015-08-10 | 2025-04-23 | Dana-Farber Cancer Institute, Inc. | Bromodomain and extra terminal (bet) inhibitor and a protein phosphatase 2a (pp2a) activator for treating bet inhibitor resistant cancer |
| US10807977B2 (en) * | 2016-04-21 | 2020-10-20 | Bioventures, Llc | Compounds that induce degradation of anti-apoptotic Bcl-2 family proteins and the uses thereof |
| CN106177955B (zh) * | 2016-08-18 | 2018-03-16 | 广州威溶特医药科技有限公司 | Bcl‑xL抑制剂和溶瘤病毒在制备抗肿瘤药物中的应用 |
| EP3441069B1 (en) * | 2017-08-11 | 2023-04-05 | Unity Biotechnology, Inc. | Treatment of diabetic retinopathy using pharmaceutical agents that eliminate senescent cells |
| WO2019033122A1 (en) * | 2017-08-11 | 2019-02-14 | Unity Biotechnology, Inc. | TREATMENT OF PULMONARY DISEASES USING PHARMACEUTICAL AGENTS THAT ELIMINATE SENESCENT CELLS |
| US20200354336A9 (en) * | 2017-08-11 | 2020-11-12 | Unity Biotechnology, Inc. | Treatment of Lung Diseases Using Pharmaceutical Agents that Eliminate Senescent Cells |
| CN107573256B (zh) * | 2017-09-26 | 2020-02-21 | 安徽国星生物化学有限公司 | 一种对氯苯肼盐酸盐连续化生产方法及其装置 |
| CN109718377B (zh) * | 2017-10-31 | 2021-03-26 | 中国科学院脑科学与智能技术卓越创新中心 | KPNB1抑制剂和Bcl-xL抑制剂在制备抗肿瘤药物中的应用 |
| US10588916B2 (en) | 2017-10-31 | 2020-03-17 | Unity Biotechnology, Inc. | Technology to inhibit vascular changes that lead to vision loss in the eye |
| AU2018357829B2 (en) | 2017-12-30 | 2019-09-26 | Unity Biotechnology, Inc. | Peptide-based proteasome inhibitors for treating conditions mediated by senescent cells and for treating cancer |
| SG11202005785XA (en) | 2018-01-10 | 2020-07-29 | Recurium Ip Holdings Llc | Benzamide compounds |
| US10111873B1 (en) | 2018-01-17 | 2018-10-30 | King Saud University | Dihydropyrimidinone derivatives |
| ES3041854T3 (en) | 2018-01-22 | 2025-11-17 | Bioventures Llc | Bcl-2 proteins degraders for cancer treatment |
| SI3752501T1 (sl) | 2018-02-13 | 2023-08-31 | Gilead Sciences, Inc. | Inhibitorji pd-1/pd-l1 |
| CA3093130C (en) | 2018-04-19 | 2023-10-17 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| HUE071493T2 (hu) * | 2018-04-29 | 2025-09-28 | Beigene Switzerland Gmbh | Bcl-2 inhibitorok |
| CN112513057B (zh) | 2018-04-30 | 2024-01-05 | 联合生物科技公司 | 供在由衰老细胞引起或介导的状况的临床管理中使用和用于治疗癌症的作为Bcl家族拮抗剂的酰基氨基膦酸酯和酰基苄胺 |
| US10738042B2 (en) | 2018-04-30 | 2020-08-11 | Unity Biotechnology, Inc. | Phosphonamidates that are Bcl family antagonists for use in clinical management of conditions caused or mediated by senescent cells and for treating cancer |
| CA3056878C (en) | 2018-04-30 | 2021-03-30 | Unity Biotechnology | Phospholidines that are bcl family antagonists for use in clinical management of conditions caused or mediated by senescent cells and for treating cancer |
| US10717722B2 (en) | 2018-06-13 | 2020-07-21 | Unity Biotechnology, Inc. | Acyl sulfonamides that are Bcl family antagonists for use in clinical management of conditions caused or mediated by senescent cells and for treating cancer |
| SI3820572T1 (sl) | 2018-07-13 | 2023-12-29 | Gilead Sciences, Inc. | Inhibitorji pd-1/pd-l1 |
| CN110776507B (zh) | 2018-07-31 | 2020-12-18 | 苏州亚盛药业有限公司 | Bcl-2抑制剂与化疗药的组合产品及其在预防和/或治疗疾病中的用途 |
| EP3672591B1 (en) | 2018-07-31 | 2024-02-14 | Ascentage Pharma (Suzhou) Co., Ltd. | Synergistic antitumor effect of bcl-2 inhibitor combined with rituximab and/or bendamustine or bcl-2 inhibitor combined with chop |
| US12083136B2 (en) * | 2018-07-31 | 2024-09-10 | Ascentage Pharma (Suzhou) Co., Ltd | Combination of BCL-2/BCL-XL inhibitors and chemotherapeutic agent and use thereof |
| CN114522167A (zh) * | 2018-07-31 | 2022-05-24 | 苏州亚盛药业有限公司 | Bcl-2抑制剂或Bcl-2/Bcl-xL抑制剂与BTK抑制剂的组合产品及其用途 |
| BR112020018978A2 (pt) | 2018-07-31 | 2021-03-02 | Ascentage Pharma (Suzhou) Co., Ltd. | produto de combinação que compreende um inibidor de bcl-2 e um inibidor de mdm2 e uso dos ditos inibidores na prevenção e/ou tratamento de câncer |
| EP3842426A4 (en) * | 2018-08-22 | 2022-05-18 | Jiangsu Hengrui Medicine Co., Ltd. | PREPARATION PROCESS OF PYRROLO-AMINO-PYRIDAZINONE COMPOUNDS AND INTERMEDIATE THEREOF |
| US12220419B2 (en) | 2018-08-22 | 2025-02-11 | Newave Pharmaceutical Inc. | BCL-2 inhibitors |
| JP7158577B2 (ja) | 2018-10-24 | 2022-10-21 | ギリアード サイエンシーズ， インコーポレイテッド | Ｐｄ－１／ｐｄ－ｌ１阻害剤 |
| TWI729662B (zh) * | 2019-01-04 | 2021-06-01 | 大陸商蘇州亞盛藥業有限公司 | 一種磺胺類化合物及製備磺胺類化合物的製程 |
| EP3906235B1 (en) * | 2019-01-04 | 2023-03-15 | Ascentage Pharma (Suzhou) Co., Ltd. | Method for preparing sulfonamides drugs |
| TWI770503B (zh) * | 2019-05-13 | 2022-07-11 | 大陸商蘇州亞盛藥業有限公司 | 用於預測bcl-2/bcl-xl抑制劑對癌症的功效的方法和組合物 |
| WO2021066873A1 (en) | 2019-10-03 | 2021-04-08 | Newave Pharmaceutical Inc. | Condensed heterocycles as bcl-2 inhibitors |
| WO2021110102A1 (en) * | 2019-12-02 | 2021-06-10 | Beigene, Ltd. | Methods of cancer treatment using bcl-2 inhibitor |
| US20230040125A1 (en) * | 2019-12-24 | 2023-02-09 | The Regents Of The University Of California | Targeting the intrinsic apoptotic machinery in glioblastoma |
| EP3914257B1 (en) * | 2020-04-10 | 2023-12-27 | Ascentage Pharma (Suzhou) Co., Ltd. | Combination of a bcl-2/bcl-xl inhibitor with osimertinib |
| BR112022019525A2 (pt) | 2020-04-15 | 2023-11-14 | Beigene Ltd | Composto, composição farmacêutica e método para tratar doenças apoptóticas desreguladas |
| CA3177906A1 (en) * | 2020-05-08 | 2021-11-11 | Weipeng Zhang | Compounds as bcl-2 inhibitors |
| WO2022216942A1 (en) | 2021-04-07 | 2022-10-13 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for the treatment of cancer |
| MX2024002465A (es) * | 2021-08-31 | 2024-04-29 | Beigene Ltd | Formas solidas de inhibidores de bcl-2, metodo de preparacion y sus usos. |
| WO2023122000A1 (en) * | 2021-12-20 | 2023-06-29 | Newave Pharmaceutical Inc. | Bcl-2 inhibitors |
| WO2024051741A1 (zh) * | 2022-09-06 | 2024-03-14 | 西藏海思科制药有限公司 | 一种抑制Bcl-2或Bcl-xL的化合物及其在医药上的应用 |
| CN115557846B (zh) * | 2022-10-17 | 2023-11-10 | 成都道合尔医药技术有限公司 | 8-氨基辛酸的合成方法 |
| WO2024245312A1 (en) * | 2023-05-30 | 2024-12-05 | Ascentage Pharma (Suzhou) Co., Ltd. | Bcl-2/bcl-xl protein degrader and use thereof |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA200100882A1 (ru) * | 1999-02-09 | 2002-04-25 | 3-Дименшенл Фамэсьютикэлс, Инк. | Гетероарильные производные амидина, метиламидина и гуанидина (варианты), способ их получения, фармацевтическая композиция (варианты), способ ингибирования протеазы (варианты) и способ лечения различных заболеваний (варианты) |
| US7432304B2 (en) | 2001-05-30 | 2008-10-07 | The Regents Of The University Of Michigan | Small molecule antagonists of Bcl-2 family proteins |
| EP1730118A1 (en) * | 2004-02-12 | 2006-12-13 | Transtech Pharma, Inc. | Substituted azole derivatives, compositions, and methods of use |
| WO2005090297A1 (en) * | 2004-03-19 | 2005-09-29 | Biotie Therapies Corporation | Sulphonamide derivatives |
| CA2577752A1 (en) | 2004-08-20 | 2006-03-02 | The Regents Of The University Of Michigan | Small molecule inhibitors of anti-apoptotic bcl-2 family members and the uses thereof |
| CN101039662A (zh) * | 2004-08-20 | 2007-09-19 | 密执安州立大学董事会 | 抗－细胞凋亡bcl－2家族成员的小分子抑制剂及其应用 |
| TWI337608B (en) * | 2005-05-12 | 2011-02-21 | Abbott Lab | Apoptosis promoters |
| JP5193861B2 (ja) * | 2005-07-07 | 2013-05-08 | アボット・ラボラトリーズ | アポトーシス促進剤 |
| US20070197532A1 (en) * | 2005-11-18 | 2007-08-23 | Cao Sheldon X | Glucokinase activators |
| CA2640090A1 (en) * | 2006-01-25 | 2007-08-02 | Synta Pharmaceuticals Corp. | Substituted aromatic compounds for inflammation and immune-related uses |
| WO2008010934A2 (en) * | 2006-07-14 | 2008-01-24 | Chemocentryx, Inc. | Triazolyl phenyl benzenesulfonamides |
| PE20080948A1 (es) * | 2006-07-25 | 2008-09-10 | Irm Llc | Derivados de imidazol como moduladores de la senda de hedgehog |
| CA2677264C (en) * | 2007-02-02 | 2021-11-30 | Baylor College Of Medicine | Compositions and methods for the treatment of metabolic disorders |
| US7776877B2 (en) * | 2007-06-22 | 2010-08-17 | Chemocentryx, Inc. | N-(2-(hetaryl)aryl) arylsulfonamides and N-(2-(hetaryl) hetaryl arylsulfonamides |
| UA103319C2 (en) * | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| JP5385382B2 (ja) * | 2008-07-24 | 2014-01-08 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | プロテインキナーゼ阻害剤としての３，４−ジアリールピラゾール |
| WO2010104899A1 (en) * | 2009-03-12 | 2010-09-16 | Glaxosmithkline Llc | Thiazole sulfonamide and oxazole sulfonamide kinase inhibitors |
| US20100278921A1 (en) | 2009-04-30 | 2010-11-04 | Fischer Cristina M | Solid oral formulation of abt-263 |
| AU2010294292B2 (en) * | 2009-09-10 | 2013-07-18 | Novartis Ag | Sulfonamides as inhibitors of Bcl-2 family proteins for the treatment of cancer |
-
2012
- 2012-01-24 SG SG2013056544A patent/SG192126A1/en unknown
- 2012-01-24 KR KR1020137021901A patent/KR101762724B1/ko active Active
- 2012-01-24 WO PCT/US2012/022315 patent/WO2012103059A2/en not_active Ceased
- 2012-01-24 AU AU2012209295A patent/AU2012209295B2/en active Active
- 2012-01-24 US US13/356,763 patent/US8691184B2/en active Active
- 2012-01-24 EP EP12739376.7A patent/EP2668180B1/en active Active
- 2012-01-24 CN CN201280017060.3A patent/CN103562202B/zh active Active
- 2012-01-24 JP JP2013551282A patent/JP5998152B2/ja active Active
- 2012-01-24 CA CA2825306A patent/CA2825306C/en active Active
- 2012-01-24 EP EP18186324.2A patent/EP3459945A1/en not_active Withdrawn
- 2012-01-24 ES ES12739376.7T patent/ES2693107T3/es active Active
-
2013
- 2013-07-23 ZA ZA2013/05571A patent/ZA201305571B/en unknown
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