JP2014507421A5 - - Google Patents
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- 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 (2) | 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 (2) |
| EP (2) | EP2668180B1 (2) |
| JP (1) | JP5998152B2 (2) |
| KR (1) | KR101762724B1 (2) |
| CN (1) | CN103562202B (2) |
| AU (1) | AU2012209295B2 (2) |
| CA (1) | CA2825306C (2) |
| ES (1) | ES2693107T3 (2) |
| SG (1) | SG192126A1 (2) |
| WO (1) | WO2012103059A2 (2) |
| ZA (1) | ZA201305571B (2) |
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3689886A1 (en) * | 2013-01-16 | 2020-08-05 | The Regents of The University of Michigan | Bcl-2/bcl-xl inhibitors and their use in the treatment of cancer |
| RU2015149680A (ru) | 2013-04-21 | 2017-05-24 | Йеда Ресеарч Энд Девелопмент Ко. Лтд. | Агенты для подавления активности и/или снижения количества bcl-xl и/или 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 |
| IL286427B2 (en) | 2014-01-28 | 2024-08-01 | Mayo Found Medical Education & Res | Inhibitors bcl-2 anti-apoptotic protein family members for treatment of non cancer pulmonary disease or an opthalmic disease |
| 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 |
| 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 |
| CN105753814A (zh) * | 2015-01-01 | 2016-07-13 | 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 |
| BR112018002550A2 (en) | 2015-08-10 | 2018-09-18 | Dana-Farber Cancer Institute, Inc. | inhibitor resistance mechanism |
| CN109152933B (zh) * | 2016-04-21 | 2022-12-02 | 生物风险投资有限责任公司 | 诱导抗细胞凋亡bcl-2家族蛋白的降解的化合物及其用途 |
| 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 |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| US20200354336A9 (en) * | 2017-08-11 | 2020-11-12 | Unity Biotechnology, Inc. | Treatment of Lung Diseases Using Pharmaceutical Agents that Eliminate Senescent Cells |
| WO2019033119A1 (en) * | 2017-08-11 | 2019-02-14 | Unity Biotechnology, Inc. | TREATMENT OF OPHTHALMIC CONDITIONS SUCH AS MACULAR DEGENERATION, GLAUCOMA AND 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 |
| 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 |
| KR20200108301A (ko) | 2018-01-10 | 2020-09-17 | 리커리엄 아이피 홀딩스, 엘엘씨 | 벤즈아미드 화합물 |
| 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 |
| CR20200347A (es) | 2018-02-13 | 2020-09-23 | Gilead Sciences Inc | Inhibidores pd-1/pd-l1 |
| TWI712412B (zh) | 2018-04-19 | 2020-12-11 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
| SG11202009933WA (en) * | 2018-04-29 | 2020-11-27 | Beigene Ltd | Bcl-2 INHIBITORS |
| 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 |
| CN117866015A (zh) | 2018-04-30 | 2024-04-12 | 联合生物科技公司 | 一种临床管理中使用的化合物及其用途 |
| 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 |
| SG11202012425QA (en) | 2018-07-13 | 2021-01-28 | Gilead Sciences Inc | Pd-1/pd-l1 inhibitors |
| TW202019421A (zh) * | 2018-07-31 | 2020-06-01 | 大陸商蘇州亞盛藥業有限公司 | Bcl-2/Bcl-xL抑制劑與化療藥物的組合及其應用 |
| US11554127B2 (en) | 2018-07-31 | 2023-01-17 | 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 |
| CA3095699A1 (en) | 2018-07-31 | 2020-02-06 | Ascentage Pharma (Suzhou) Co., Ltd. | Combination product of bcl-2 inhibitor and chemotherapeutic agent and use thereof in the prevention and/or treatment of diseases |
| 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 |
| US11903950B2 (en) | 2018-08-22 | 2024-02-20 | Newave Pharmaceutical Inc. | BCL-2 inhibitors |
| KR20210047320A (ko) * | 2018-08-22 | 2021-04-29 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 피롤로-아미노-피리다지논 화합물 및 이의 중간체의 제조 방법 |
| WO2020086556A1 (en) | 2018-10-24 | 2020-04-30 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| WO2020140005A2 (en) | 2018-12-29 | 2020-07-02 | Newave Pharmaceutical Inc. | Bcl-2 inhibitors |
| 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 |
| US20220372042A1 (en) | 2019-10-03 | 2022-11-24 | Newave Pharmaceutical Inc. | Condensed heterocycles as bcl-2 inhibitors |
| WO2021083135A1 (en) | 2019-10-28 | 2021-05-06 | Beigene, Ltd. | Bcl-2 INHIBITORS |
| WO2021110102A1 (en) * | 2019-12-02 | 2021-06-10 | Beigene, Ltd. | Methods of cancer treatment using bcl-2 inhibitor |
| WO2021133862A1 (en) * | 2019-12-24 | 2021-07-01 | The Regents Of The University Of California | Targeting the intrinsic apoptotic machinery in glioblastoma |
| US12552784B2 (en) | 2019-12-27 | 2026-02-17 | Newave Pharmaceutical Inc. | 1H-pyrrolo[2,3-b]pyridine derivatives as BCL-2 inhibitors for the treatment of neoplastic and autoimmune diseases |
| WO2021204060A1 (en) * | 2020-04-10 | 2021-10-14 | Ascentage Pharma (Suzhou) Co., Ltd. | Combinations of bcl-2/bcl-xl inhibitors and related uses |
| IL296582A (en) | 2020-04-15 | 2022-11-01 | Beigene Ltd | bcl-2 inhibitor |
| US20230159527A1 (en) * | 2020-05-08 | 2023-05-25 | Fochon Pharmaceuticals, Ltd. | 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 |
| EP4396180A4 (en) * | 2021-08-31 | 2025-07-09 | Beigene Ltd | SOLID FORMS OF BCL-2 INHIBITORS, PROCESS FOR THEIR PREPARATION AND USE THEREOF |
| 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 |
| EP4719408A1 (en) * | 2023-05-30 | 2026-04-08 | Ascentage Pharma (Suzhou) Co., Ltd. | Bcl-2/bcl-xl protein degrader and use thereof |
| CN117756811A (zh) * | 2023-12-29 | 2024-03-26 | 贵州民族大学 | 一种合成多取代基吡咯化合物的方法 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20010098982A (ko) * | 1999-02-09 | 2001-11-08 | 3-디멘져널 파마슈티칼즈 인코오포레이티드 | 프로테아제 억제제로서의 헤테로아릴 아미딘, 메틸아미딘및 구아니딘 |
| US7432304B2 (en) | 2001-05-30 | 2008-10-07 | The Regents Of The University Of Michigan | Small molecule antagonists of Bcl-2 family proteins |
| CA2551909C (en) * | 2004-02-12 | 2011-10-11 | Transtech Pharma, Inc. | Substituted azole derivatives, compositions, and methods of use |
| WO2005090297A1 (en) * | 2004-03-19 | 2005-09-29 | Biotie Therapies Corporation | Sulphonamide derivatives |
| AU2005277223C1 (en) * | 2004-08-20 | 2009-05-21 | The Regents Of The University Of Michigan | Small molecule inhibitors of anti-apoptotic Bcl-2 family members and the uses thereof |
| EP1778206A4 (en) * | 2004-08-20 | 2009-08-05 | Univ Michigan | SMALL MOLECULE INHIBITORS FROM MEMBERS OF THE ANTIOPTOTIC BCL-2 FAMILY AND USES THEREOF |
| PL1888550T3 (pl) | 2005-05-12 | 2014-12-31 | Abbvie Bahamas Ltd | Promotory apoptozy |
| 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 |
| EP1948614A2 (en) * | 2005-11-18 | 2008-07-30 | Takeda San Diego, Inc. | Glucokinase activators |
| TW200806641A (en) * | 2006-01-25 | 2008-02-01 | 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 |
| JP5461197B2 (ja) * | 2007-02-02 | 2014-04-02 | ベイラー カレッジ オブ メディスン | 代謝障害を処置するための組成物および方法 |
| 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 |
| PT2324008E (pt) * | 2008-07-24 | 2012-06-25 | Nerviano Medical Sciences Srl | 3,4-diarilpirazoles como inibidores da proteína quinase |
| US20110319392A1 (en) * | 2009-03-12 | 2011-12-29 | George Adjabeng | Thiazole Sulfonamide And Oxazole Sulfonamide Kinase Inhibitors |
| US20100278921A1 (en) | 2009-04-30 | 2010-11-04 | Fischer Cristina M | Solid oral formulation of abt-263 |
| CA2772989A1 (en) * | 2009-09-10 | 2011-03-17 | Novartis Ag | Sulfonamides as inhibitors of bcl-2 family proteins for the treatment of cancer |
-
2012
- 2012-01-24 EP EP12739376.7A patent/EP2668180B1/en active Active
- 2012-01-24 AU AU2012209295A patent/AU2012209295B2/en active Active
- 2012-01-24 CN CN201280017060.3A patent/CN103562202B/zh active Active
- 2012-01-24 EP EP18186324.2A patent/EP3459945A1/en not_active Withdrawn
- 2012-01-24 US US13/356,763 patent/US8691184B2/en active Active
- 2012-01-24 WO PCT/US2012/022315 patent/WO2012103059A2/en not_active Ceased
- 2012-01-24 CA CA2825306A patent/CA2825306C/en active Active
- 2012-01-24 JP JP2013551282A patent/JP5998152B2/ja active Active
- 2012-01-24 ES ES12739376.7T patent/ES2693107T3/es active Active
- 2012-01-24 SG SG2013056544A patent/SG192126A1/en unknown
- 2012-01-24 KR KR1020137021901A patent/KR101762724B1/ko active Active
-
2013
- 2013-07-23 ZA ZA2013/05571A patent/ZA201305571B/en unknown
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