TWI781996B - 合成ｍｃｌ-１抑制劑之方法 - Google Patents

合成ｍｃｌ-１抑制劑之方法 Download PDF

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Publication number
TWI781996B
TWI781996B TW107110205A TW107110205A TWI781996B TW I781996 B TWI781996 B TW I781996B TW 107110205 A TW107110205 A TW 107110205A TW 107110205 A TW107110205 A TW 107110205A TW I781996 B TWI781996 B TW I781996B
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TW
Taiwan
Prior art keywords
methyl
mol
dimethyl
solvent
pyrazol
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TW107110205A
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English (en)
Chinese (zh)
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TW201902868A (zh
Inventor
克雷格 史都華
賽門 哈迪
安德魯 史塔克
亞歷山大 荷德
沁 葉
鄭曉蘭
迪巴席斯 哈撒
卡迪 費拉爾
珍 柯克
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瑞典商阿斯特捷利康公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C245/00—Compounds containing chains of at least two nitrogen atoms with at least one nitrogen-to-nitrogen multiple bond
    • C07C245/02—Azo compounds, i.e. compounds having the free valencies of —N=N— groups attached to different atoms, e.g. diazohydroxides
    • C07C245/06—Azo compounds, i.e. compounds having the free valencies of —N=N— groups attached to different atoms, e.g. diazohydroxides with nitrogen atoms of azo groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/72—Hydrazones
    • C07C251/74—Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C251/76—Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of a saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Lubricants (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
TW107110205A 2017-03-31 2018-03-26 合成ｍｃｌ-１抑制劑之方法 TWI781996B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762479493P 2017-03-31 2017-03-31
US62/479,493 2017-03-31

Publications (2)

Publication Number Publication Date
TW201902868A TW201902868A (zh) 2019-01-16
TWI781996B true TWI781996B (zh) 2022-11-01

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ID=61827753

Family Applications (1)

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TW107110205A TWI781996B (zh) 2017-03-31 2018-03-26 合成ｍｃｌ-１抑制劑之方法

Country Status (16)

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US (1) US11149024B2 (enExample)
EP (1) EP3601230B1 (enExample)
JP (1) JP7032428B2 (enExample)
KR (1) KR102604876B1 (enExample)
CN (1) CN110536884B (enExample)
AR (1) AR111304A1 (enExample)
AU (1) AU2018244180B2 (enExample)
CA (1) CA3056712A1 (enExample)
CO (1) CO2019010035A2 (enExample)
EA (1) EA038226B1 (enExample)
ES (1) ES2909751T3 (enExample)
IL (1) IL269410B2 (enExample)
MX (1) MX387814B (enExample)
TW (1) TWI781996B (enExample)
WO (1) WO2018178227A1 (enExample)
ZA (1) ZA201905645B (enExample)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI749404B (zh) * 2018-11-22 2021-12-11 大陸商蘇州亞盛藥業有限公司 作為mcl-1抑制劑的大環吲哚
WO2020151738A1 (en) * 2019-01-23 2020-07-30 Ascentage Pharma (Suzhou) Co., Ltd. Macrocyclic fused pyrrazoles as mcl-1 inhibitors
MA56505A (fr) 2019-06-21 2022-04-27 Janssen Pharmaceutica Nv Inhibiteurs macrocycliques de mcl-1
KR20220034136A (ko) 2019-07-09 2022-03-17 얀센 파마슈티카 엔.브이. Mcl-1 억제제로서의 거대환식 스피로사이클 유도체
WO2021092053A1 (en) * 2019-11-08 2021-05-14 Unity Biotechnology, Inc. Mcl-1 inhibitor macrocycle compounds for use in clinical management of conditions caused or mediated by senescent cells and for treating cancer
US20230021562A1 (en) 2019-11-21 2023-01-26 Janssen Pharmaceutica Nv Macrocylic indole derivatives mcl-1 inhibitors
CA3157590A1 (en) 2019-11-21 2021-05-27 Janssen Pharmaceutica Nv Macrocyclic sulfonyl derivatives as mcl-1 inhibitors
CN115151551B (zh) 2020-02-21 2024-10-25 詹森药业有限公司 作为mcl-1抑制剂的大环吲哚衍生物
EP4157852A1 (en) 2020-05-29 2023-04-05 JANSSEN Pharmaceutica NV Macrocyclic 7-pyrazol-5-yl-indole derivatives as inhibitors of mcl-1
CA3181816A1 (en) 2020-06-19 2021-12-23 Aldo Peschiulli N-linked macrocyclic 4-(pyrazol-5-yl)-indole derivatives as inhibitors of mcl-1
CN115943147A (zh) 2020-06-19 2023-04-07 詹森药业有限公司 N-连接的大环7-(吡唑-5-基)-吲哚衍生物作为mcl-1抑制剂
CA3184877A1 (en) 2020-07-08 2022-01-13 Benoit Christian Albert Ghislain De Boeck Macrocyclic ether containing indole derivatives as inhibitors of mcl-1
WO2022032284A1 (en) * 2020-08-07 2022-02-10 Zeno Management, Inc. Macrocyclic compounds
WO2022129333A1 (en) 2020-12-17 2022-06-23 Janssen Pharmaceutica Nv Branched macrocyclic 4-(pyrazol-5-yl)-indole derivatives as inhibitors of mcl-1
CN116848126A (zh) 2021-02-12 2023-10-03 詹森药业有限公司 大环1,3-桥联的6-氯-7-吡唑-4-基-1h-吲哚-2-羧酸酯和6-氯-7-嘧啶-5-基-1h-吲哚-2-羧酸酯衍生物作为mcl-1抑制剂用于治疗癌症
JP7900421B2 (ja) 2021-06-11 2026-08-04 ギリアード サイエンシーズ， インコーポレイテッド Ｍｃｌ－１阻害剤と抗がん剤との組み合わせ
TWI861509B (zh) 2021-06-11 2024-11-11 美商基利科學股份有限公司 Mcl-1抑制劑與抗體藥物接合物之組合

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160106731A1 (en) * 2014-10-17 2016-04-21 Vanderbilt University Tricyclic indole mcl-1 inhibitors and uses thereof
TW201803879A (zh) * 2016-04-22 2018-02-01 阿斯特捷利康公司 Mcl-1抑制劑及其使用方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2915811A1 (en) * 2014-03-04 2015-09-09 Centre Régional de Lutte contre le Cancer - Centre François Baclesse MCL-1 modulating compounds for cancer treatment
CN105061315B (zh) * 2015-08-06 2017-10-24 大连理工大学 一类1,5‑二苯基吡唑‑3‑羧酸类化合物及其应用
CN106478606B (zh) * 2016-09-21 2019-05-10 沈阳药科大学 N-取代吲哚类衍生物及其应用

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160106731A1 (en) * 2014-10-17 2016-04-21 Vanderbilt University Tricyclic indole mcl-1 inhibitors and uses thereof
TW201803879A (zh) * 2016-04-22 2018-02-01 阿斯特捷利康公司 Mcl-1抑制劑及其使用方法

Also Published As

Publication number Publication date
MX2019011468A (es) 2019-11-01
AU2018244180A1 (en) 2019-11-07
IL269410A (en) 2019-11-28
CN110536884A (zh) 2019-12-03
EA201992235A1 (ru) 2020-02-10
US11149024B2 (en) 2021-10-19
IL269410B (en) 2022-11-01
JP7032428B2 (ja) 2022-03-08
CO2019010035A2 (es) 2019-09-30
MX387814B (es) 2025-03-04
JP2020515557A (ja) 2020-05-28
EA038226B1 (ru) 2021-07-27
KR20190136039A (ko) 2019-12-09
ES2909751T3 (es) 2022-05-10
AR111304A1 (es) 2019-06-26
IL269410B2 (en) 2023-03-01
EP3601230B1 (en) 2022-01-26
CN110536884B (zh) 2023-05-02
WO2018178227A1 (en) 2018-10-04
EP3601230A1 (en) 2020-02-05
US20210122735A1 (en) 2021-04-29
AU2018244180B2 (en) 2021-03-04
KR102604876B1 (ko) 2023-11-22
ZA201905645B (en) 2020-05-27
CA3056712A1 (en) 2018-10-04
TW201902868A (zh) 2019-01-16
BR112019019686A2 (pt) 2020-04-14

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