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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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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Publication of TW201902868A publication Critical patent/TW201902868A/zh
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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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Lubricants (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (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
US11691989B2 (en) 2018-11-22 2023-07-04 Ascentage Pharma (Suzhou) Co., Ltd. Macrocyclic indoles as Mcl-1 inhibitors
US12319703B2 (en) 2019-01-23 2025-06-03 Ascentage Pharma (Suzhou) Co., Ltd. Macrocyclic fused pyrazoles as Mcl-1 inhibitors
KR20220024694A (ko) 2019-06-21 2022-03-03 얀센 파마슈티카 엔.브이. Mcl-1의 거대환식 억제제
WO2021005043A1 (en) 2019-07-09 2021-01-14 Janssen Pharmaceutica Nv Macrocyclic spirocycle derivatives as mcl-1 inhibitors
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
WO2021099579A1 (en) 2019-11-21 2021-05-27 Janssen Pharmaceutica Nv Macrocyclic indole derivatives as mcl-1 inhibitors
MX2022006180A (es) 2019-11-21 2022-06-14 Janssen Pharmaceutica Nv Derivados macrociclicos de sulfonilo como inhibidores de mcl-1.
JP2023514364A (ja) 2020-02-21 2023-04-05 ヤンセン ファーマシューティカ エヌ．ベー． Ｍｃｌ－１の阻害剤としての大環状インドール誘導体
EP4157852A1 (en) 2020-05-29 2023-04-05 JANSSEN Pharmaceutica NV Macrocyclic 7-pyrazol-5-yl-indole derivatives as inhibitors of mcl-1
MX2022015998A (es) * 2020-06-19 2023-04-12 Janssen Pharmaceutica Nv Derivados de 4-(pirazol-5-il)-indol macrocíclico unidos a n como inhibidores de mcl-1.
WO2021255257A1 (en) 2020-06-19 2021-12-23 Janssen Pharmaceutica Nv N-linked macrocyclic 7-(pyrazol-5-yl)-indole derivatives as inhibitors of mcl-1
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
JP2023553719A (ja) 2020-12-17 2023-12-25 ヤンセン ファーマシューティカ エヌ．ベー． Ｍｃｌ－１阻害剤としての分岐大環状４－（ピラゾール－５－イル）－インドール誘導体
JP2024506648A (ja) 2021-02-12 2024-02-14 ヤンセン ファーマシューティカ エヌ．ベー． がんの治療のためのｍｃｌ－１阻害剤としての大環状１，３－架橋６－クロロ－７－ピラゾール－４－イル－１ｈ－インドール－２－カルボキシレート及び６－クロロ－７－ピリミジン－５－イル－１ｈ－インドール－２－カルボキシレート誘導体
US11931424B2 (en) 2021-06-11 2024-03-19 Gilead Sciences, Inc. Combination MCL-1 inhibitors with anti-body drug conjugates
WO2022261301A1 (en) 2021-06-11 2022-12-15 Gilead Sciences, Inc. Combination mcl-1 inhibitors with anti-cancer agents

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

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