JP2017510610A5 - - Google Patents
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- Publication number
- JP2017510610A5 JP2017510610A5 JP2016561754A JP2016561754A JP2017510610A5 JP 2017510610 A5 JP2017510610 A5 JP 2017510610A5 JP 2016561754 A JP2016561754 A JP 2016561754A JP 2016561754 A JP2016561754 A JP 2016561754A JP 2017510610 A5 JP2017510610 A5 JP 2017510610A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- hydrogen
- aryl
- cycloalkyl
- 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 43
- 229910052739 hydrogen Inorganic materials 0.000 claims 31
- 239000001257 hydrogen Substances 0.000 claims 31
- 125000003118 aryl group Chemical group 0.000 claims 24
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 21
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 21
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 19
- 125000004093 cyano group Chemical group *C#N 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 150000002367 halogens Chemical class 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 18
- 239000011780 sodium chloride Substances 0.000 claims 18
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 15
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 15
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 15
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 11
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 239000000543 intermediate Substances 0.000 claims 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 3
- 230000001085 cytostatic Effects 0.000 claims 3
- 239000000824 cytostatic agent Substances 0.000 claims 3
- 230000001472 cytotoxic Effects 0.000 claims 3
- 231100000433 cytotoxic Toxicity 0.000 claims 3
- 239000000126 substance Substances 0.000 claims 3
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 238000003786 synthesis reaction Methods 0.000 claims 2
- 230000002194 synthesizing Effects 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 206010003816 Autoimmune disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 102100019155 MDM2 Human genes 0.000 claims 1
- 101700032565 MDM2 Proteins 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 201000009910 diseases by infectious agent Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical group O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 229910052717 sulfur Chemical group 0.000 claims 1
- 239000011593 sulfur Chemical group 0.000 claims 1
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP14164388.2 | 2014-04-11 | ||
EP14164388 | 2014-04-11 | ||
PCT/EP2015/057839 WO2015155332A1 (en) | 2014-04-11 | 2015-04-10 | Spiro[3h-indole-3,2'-pyrrolidin]-2(1h)-one derivatives and their use as mdm2-p53 inhibitors |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2017510610A JP2017510610A (ja) | 2017-04-13 |
JP2017510610A5 true JP2017510610A5 (US07585860-20090908-C00112.png) | 2018-05-31 |
JP6577958B2 JP6577958B2 (ja) | 2019-09-18 |
Family
ID=50478306
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016561754A Active JP6577958B2 (ja) | 2014-04-11 | 2015-04-10 | スピロ[3H−インドール−3,2’−ピロリジン]−2(1H)−オン誘導体およびMDM2−p53阻害剤としてのそれらの使用 |
Country Status (4)
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP6577958B2 (ja) * | 2014-04-11 | 2019-09-18 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | スピロ[3H−インドール−3,2’−ピロリジン]−2(1H)−オン誘導体およびMDM2−p53阻害剤としてのそれらの使用 |
JP6503386B2 (ja) | 2014-07-03 | 2019-04-17 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | MDM2−p53阻害剤としての新しいスピロ[3H−インドール−3,2’−ピロリジン]−2(1H)−オン化合物および誘導体 |
HUE046057T2 (hu) * | 2014-08-21 | 2020-02-28 | Boehringer Ingelheim Int | Új spiro[3H-indol-3,2'-pirrolidin]-2(1H)-on vegyületek és származékok, mint MDM2-P53-inhibitorok |
KR20180058832A (ko) | 2015-10-09 | 2018-06-01 | 베링거 인겔하임 인터내셔날 게엠베하 | Mdm2-p53 억제제로서의 스피로[3h-인돌-3,2'-피롤리딘]-2(1h)-온 화합물 및 유도체 |
UA123786C2 (uk) * | 2016-04-06 | 2021-06-02 | Дзе Ріджентс Оф Дзе Юніверсіті Оф Мічіган | Деструктори білка mdm2 |
CN109152843A (zh) | 2016-05-20 | 2019-01-04 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
CA3057558A1 (en) | 2017-04-05 | 2018-10-11 | Boehringer Ingelheim International Gmbh | Anticancer combination therapy |
JP2021508727A (ja) * | 2017-12-29 | 2021-03-11 | 甘李薬業股▲フン▼有限公司Gan&Lee Pharmaceuticals | 腫瘍阻害剤として使用できる化合物およびその調製方法と応用 |
US20210324478A1 (en) * | 2018-07-18 | 2021-10-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for identification assessment, prevention, and treatment of ewing sarcoma using tp53 dependency biomarkers and modulators |
IL298633A (en) | 2020-06-02 | 2023-01-01 | Boehringer Ingelheim Int | Cyclic 2-amino-3-cyanothiophenes and their implications for cancer therapy |
US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
WO2023099608A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
WO2023099592A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
CN118591540A (zh) | 2021-12-01 | 2024-09-03 | 勃林格殷格翰国际有限公司 | 包含环状2-氨基-3-氰基噻吩的kras降解化合物 |
CN118574836A (zh) | 2021-12-01 | 2024-08-30 | 勃林格殷格翰国际有限公司 | 用于治疗癌症的环状2-胺基-3-氰基噻吩及衍生物 |
WO2023099624A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1999012964A2 (en) | 1997-09-12 | 1999-03-18 | Biogen, Inc. | Kay - a novel immune system protein |
AR073578A1 (es) | 2008-09-15 | 2010-11-17 | Priaxon Ag | Pirrolidin-2-onas |
US20120071499A1 (en) | 2010-09-20 | 2012-03-22 | Xin-Jie Chu | Substituted Spiro[3H-Indole-3,6'(5'H)-[1H]Pyrrolo[1,2c]Imidazole-1',2(1H,2'H)-diones |
US20130053410A1 (en) * | 2011-03-03 | 2013-02-28 | David Joseph Bartkovitz | Substituted heteroaryl 2',3',7',7a'-tetrahydrospiro[pyrrole-3,6'-pyrrolo[1,2-c]imidazole]-1',2(1h,5'h)-dione |
JP2014513699A (ja) * | 2011-05-11 | 2014-06-05 | ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン | スピロ−オキシインドールmdm2アンタゴニスト |
CN103910746B (zh) | 2014-02-28 | 2016-08-03 | 中山大学 | 一类海洋真菌来源的Berkeleyones化合物及其制备方法和应用 |
JP6577958B2 (ja) | 2014-04-11 | 2019-09-18 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | スピロ[3H−インドール−3,2’−ピロリジン]−2(1H)−オン誘導体およびMDM2−p53阻害剤としてのそれらの使用 |
JP6503386B2 (ja) | 2014-07-03 | 2019-04-17 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | MDM2−p53阻害剤としての新しいスピロ[3H−インドール−3,2’−ピロリジン]−2(1H)−オン化合物および誘導体 |
NO2721710T3 (US07585860-20090908-C00112.png) | 2014-08-21 | 2018-03-31 | ||
HUE046057T2 (hu) | 2014-08-21 | 2020-02-28 | Boehringer Ingelheim Int | Új spiro[3H-indol-3,2'-pirrolidin]-2(1H)-on vegyületek és származékok, mint MDM2-P53-inhibitorok |
KR20180058832A (ko) | 2015-10-09 | 2018-06-01 | 베링거 인겔하임 인터내셔날 게엠베하 | Mdm2-p53 억제제로서의 스피로[3h-인돌-3,2'-피롤리딘]-2(1h)-온 화합물 및 유도체 |
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2015
- 2015-04-10 JP JP2016561754A patent/JP6577958B2/ja active Active
- 2015-04-10 EP EP15716495.5A patent/EP3129380B1/en active Active
- 2015-04-10 WO PCT/EP2015/057839 patent/WO2015155332A1/en active Application Filing
- 2015-04-10 US US14/683,173 patent/US10138251B2/en active Active
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2018
- 2018-06-11 US US16/005,316 patent/US20180291030A1/en not_active Abandoned