TWI855062B - Bcl-2抑制劑 - Google Patents

Bcl-2抑制劑 Download PDF

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Publication number
TWI855062B
TWI855062B TW109114185A TW109114185A TWI855062B TW I855062 B TWI855062 B TW I855062B TW 109114185 A TW109114185 A TW 109114185A TW 109114185 A TW109114185 A TW 109114185A TW I855062 B TWI855062 B TW I855062B
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Taiwan
Prior art keywords
methyl
amino
oxy
azaspiro
benzamide
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TW109114185A
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English (en)
Chinese (zh)
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TW202043217A (zh
Inventor
薛海
郭運行
志偉 王
孫漢資
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英屬開曼群島商百濟神州有限公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyrrole Compounds (AREA)
TW109114185A 2018-04-29 2020-04-28 Bcl-2抑制劑 TWI855062B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN2018085217 2018-04-29
CN2018107134 2018-09-21
WOPCT/CN2019/085001 2019-04-29
PCT/CN2019/085001 WO2019210828A1 (en) 2018-04-29 2019-04-29 Bcl-2 INHIBITORS

Publications (2)

Publication Number Publication Date
TW202043217A TW202043217A (zh) 2020-12-01
TWI855062B true TWI855062B (zh) 2024-09-11

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TW109114185A TWI855062B (zh) 2018-04-29 2020-04-28 Bcl-2抑制劑

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US (3) US11420968B2 (enExample)
EP (2) EP4545515A1 (enExample)
JP (4) JP2021521138A (enExample)
KR (1) KR102738032B1 (enExample)
CN (3) CN112437772B (enExample)
AU (1) AU2019264475C1 (enExample)
BR (1) BR112020022092A2 (enExample)
CA (1) CA3098348A1 (enExample)
DK (1) DK3788042T3 (enExample)
ES (1) ES3018793T3 (enExample)
FI (1) FI3788042T3 (enExample)
HR (1) HRP20250392T1 (enExample)
HU (1) HUE071493T2 (enExample)
IL (1) IL278366B2 (enExample)
LT (1) LT3788042T (enExample)
MX (2) MX2020011495A (enExample)
PL (1) PL3788042T3 (enExample)
PT (1) PT3788042T (enExample)
SG (1) SG11202009933WA (enExample)
SI (1) SI3788042T1 (enExample)
TW (1) TWI855062B (enExample)
WO (1) WO2019210828A1 (enExample)

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BR112022012283A2 (pt) 2019-12-20 2022-08-30 Recurium Ip Holdings Llc Combinações
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JP7765790B2 (ja) * 2021-12-06 2025-11-07 杭州和正医薬有限公司 抗アポトーシスタンパク質bcl-2阻害剤、医薬組成物及びその使用
TW202400163A (zh) 2022-05-12 2024-01-01 英屬開曼群島商百濟神州有限公司 使用bcl-2抑制劑治療髓性惡性腫瘤之方法
WO2023231777A1 (en) * 2022-06-01 2023-12-07 Fochon Pharmaceuticals, Ltd. Compounds as bcl-2 inhibitors
KR20250079128A (ko) * 2022-07-21 2025-06-04 베이진 스위찰랜드 게엠베하 Bcl-2 저해제를 사용한 다발성 골수종의 치료 방법
WO2024140678A1 (en) * 2022-12-27 2024-07-04 Beigene (Suzhou) Co., Ltd. A ketal protected intermediate for sonrotoclax and preparation method thereof
WO2024140692A1 (en) * 2022-12-27 2024-07-04 Beigene (Suzhou) Co., Ltd. Salts and solid forms of sonrotoclax intermediate
WO2024140690A1 (en) * 2022-12-27 2024-07-04 Beigene (Suzhou) Co., Ltd. Intermediates of sonrotoclax and the method of preparing the same
TW202604488A (zh) 2024-06-26 2026-02-01 瑞士商百濟神州I有限責任公司 包含索托克拉固體分散體之醫藥調配物及其製備方法
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HUE071493T2 (hu) 2025-09-28
IL278366B1 (en) 2025-05-01
AU2019264475B2 (en) 2024-09-26
SI3788042T1 (sl) 2025-06-30
AU2019264475A1 (en) 2020-11-12
JP2025119001A (ja) 2025-08-13
IL278366A (enExample) 2020-12-31
CN112437772A (zh) 2021-03-02
MX2020011495A (es) 2021-01-15
JP7688210B2 (ja) 2025-06-03
HRP20250392T1 (hr) 2025-05-23
ES3018793T3 (en) 2025-05-19
EP3788042A1 (en) 2021-03-10
EP3788042A4 (en) 2022-01-26
DK3788042T3 (en) 2025-04-07
EP3788042B1 (en) 2025-02-12
US12077536B2 (en) 2024-09-03
CN117683029A (zh) 2024-03-12
JP2024161475A (ja) 2024-11-19
PL3788042T3 (pl) 2025-06-02
US11420968B2 (en) 2022-08-23
EP4545515A1 (en) 2025-04-30
MX2023001689A (es) 2023-02-22
FI3788042T3 (fi) 2025-04-07
PT3788042T (pt) 2025-04-15
KR102738032B1 (ko) 2024-12-05
KR20210005677A (ko) 2021-01-14
JP2021521138A (ja) 2021-08-26
TW202043217A (zh) 2020-12-01
CA3098348A1 (en) 2019-11-07
CN112437772B (zh) 2023-11-21
US20210269433A1 (en) 2021-09-02
JP7540113B1 (ja) 2024-08-26
WO2019210828A1 (en) 2019-11-07
US20240376104A1 (en) 2024-11-14
BR112020022092A2 (pt) 2021-02-02
JP2024119916A (ja) 2024-09-03
US20220402915A1 (en) 2022-12-22
SG11202009933WA (en) 2020-11-27
AU2019264475C1 (en) 2025-01-30
CN117430601A (zh) 2024-01-23
LT3788042T (lt) 2025-03-25

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