CN110536884B - Mcl-1抑制剂的合成 - Google Patents

Mcl-1抑制剂的合成 Download PDF

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Publication number
CN110536884B
CN110536884B CN201880021146.0A CN201880021146A CN110536884B CN 110536884 B CN110536884 B CN 110536884B CN 201880021146 A CN201880021146 A CN 201880021146A CN 110536884 B CN110536884 B CN 110536884B
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methyl
mol
dimethyl
pyrazol
solvent
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Chinese (zh)
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CN110536884A (zh
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C.斯图尔特
S.哈迪
A.斯塔克
A.赫德
Q.叶
郑晓兰
C.费拉
J.克克
D.哈斯拉
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AstraZeneca AB
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AstraZeneca AB
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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)
  • Lubricants (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201880021146.0A 2017-03-31 2018-03-29 Mcl-1抑制剂的合成 Active CN110536884B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762479493P 2017-03-31 2017-03-31
US62/479493 2017-03-31
PCT/EP2018/058056 WO2018178227A1 (en) 2017-03-31 2018-03-29 Synthesis of mcl-1 inhibitor

Publications (2)

Publication Number Publication Date
CN110536884A CN110536884A (zh) 2019-12-03
CN110536884B true CN110536884B (zh) 2023-05-02

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

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3781570A4 (en) * 2018-11-22 2021-06-02 Ascentage Pharma (Suzhou) Co., Ltd. MACROCYCLIC INDOLES SERVING AS MCL-1 INHIBITORS
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
EP4061819A1 (en) 2019-11-21 2022-09-28 Janssen Pharmaceutica NV Macrocyclic indole derivatives as mcl-1 inhibitors
WO2021099580A1 (en) 2019-11-21 2021-05-27 Janssen Pharmaceutica Nv Macrocyclic sulfonyl derivatives as mcl-1 inhibitors
EP4107161A1 (en) 2020-02-21 2022-12-28 Janssen Pharmaceutica NV Macrocyclic indole derivatives as inhibitors of mcl-1
JP2023526985A (ja) 2020-05-29 2023-06-26 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７－ピラゾール－５－イル－インドール誘導体
WO2021255258A1 (en) 2020-06-19 2021-12-23 Janssen Pharmaceutica Nv N-linked macrocyclic 4-(pyrazol-5-yl)-indole derivatives as inhibitors of mcl-1
BR112022025674A2 (pt) 2020-06-19 2023-01-17 Janssen Pharmaceutica Nv Derivados de 7-(pirazol-5-il)-indol macrocíclico n-ligado como inibidores de mcl-1
BR112023000212A2 (pt) 2020-07-08 2023-01-31 Janssen Pharmaceutica Nv Éter macrocíclico contendo derivados de indol como inibidores de mcl-1
WO2022032284A1 (en) * 2020-08-07 2022-02-10 Zeno Management, Inc. Macrocyclic compounds
CA3200758A1 (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
TWI910028B (zh) 2021-06-11 2025-12-21 美商基利科學股份有限公司 Mcl-1抑制劑與抗癌劑之組合
US11931424B2 (en) 2021-06-11 2024-03-19 Gilead Sciences, Inc. Combination MCL-1 inhibitors with anti-body drug conjugates

Citations (4)

* 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
CN105061315A (zh) * 2015-08-06 2015-11-18 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
CN106478606A (zh) * 2016-09-21 2017-03-08 沈阳药科大学 N‑取代吲哚类衍生物及其应用
CN109071566A (zh) * 2016-04-22 2018-12-21 阿斯利康(瑞典)有限公司 用于治疗癌症的大环mcl-1抑制剂

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9949965B2 (en) * 2014-10-17 2018-04-24 Vanderbilt University Tricyclic indole Mcl-1 inhibitors and uses thereof

Patent Citations (4)

* 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
CN105061315A (zh) * 2015-08-06 2015-11-18 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
CN109071566A (zh) * 2016-04-22 2018-12-21 阿斯利康(瑞典)有限公司 用于治疗癌症的大环mcl-1抑制剂
CN106478606A (zh) * 2016-09-21 2017-03-08 沈阳药科大学 N‑取代吲哚类衍生物及其应用

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Publication number Publication date
TWI781996B (zh) 2022-11-01
JP2020515557A (ja) 2020-05-28
CN110536884A (zh) 2019-12-03
IL269410B2 (en) 2023-03-01
KR102604876B1 (ko) 2023-11-22
BR112019019686A2 (pt) 2020-04-14
JP7032428B2 (ja) 2022-03-08
US20210122735A1 (en) 2021-04-29
US11149024B2 (en) 2021-10-19
MX2019011468A (es) 2019-11-01
IL269410B (en) 2022-11-01
AU2018244180B2 (en) 2021-03-04
WO2018178227A1 (en) 2018-10-04
ES2909751T3 (es) 2022-05-10
ZA201905645B (en) 2020-05-27
EP3601230B1 (en) 2022-01-26
KR20190136039A (ko) 2019-12-09
MX387814B (es) 2025-03-04
CA3056712A1 (en) 2018-10-04
EA038226B1 (ru) 2021-07-27
AU2018244180A1 (en) 2019-11-07
TW201902868A (zh) 2019-01-16
EA201992235A1 (ru) 2020-02-10
IL269410A (en) 2019-11-28
AR111304A1 (es) 2019-06-26
CO2019010035A2 (es) 2019-09-30
EP3601230A1 (en) 2020-02-05

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