CN113660937A - 治疗剂和治疗方法 - Google Patents

治疗剂和治疗方法 Download PDF

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Publication number
CN113660937A
CN113660937A CN202080027337.5A CN202080027337A CN113660937A CN 113660937 A CN113660937 A CN 113660937A CN 202080027337 A CN202080027337 A CN 202080027337A CN 113660937 A CN113660937 A CN 113660937A
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China
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
independently
methyl
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Pending
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CN202080027337.5A
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English (en)
Chinese (zh)
Inventor
郑广荣
D·周
P·帕尔
X·刘
D·图姆穆里亚
W·胡
P·张
D·吕
Y·袁
X·张
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University of Florida Research Foundation Inc
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University of Florida Research Foundation Inc
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Publication of CN113660937A publication Critical patent/CN113660937A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202080027337.5A 2019-02-08 2020-02-07 治疗剂和治疗方法 Pending CN113660937A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962803299P 2019-02-08 2019-02-08
US62/803,299 2019-02-08
PCT/US2020/017364 WO2020163823A2 (en) 2019-02-08 2020-02-07 Therapeutic agents and methods of treatment

Publications (1)

Publication Number Publication Date
CN113660937A true CN113660937A (zh) 2021-11-16

Family

ID=71948254

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202080027337.5A Pending CN113660937A (zh) 2019-02-08 2020-02-07 治疗剂和治疗方法

Country Status (8)

Country Link
US (1) US20220169628A1 (https=)
EP (1) EP3920923A4 (https=)
JP (1) JP2022520061A (https=)
KR (1) KR20210137025A (https=)
CN (1) CN113660937A (https=)
AU (1) AU2020218367A1 (https=)
CA (1) CA3127501A1 (https=)
WO (1) WO2020163823A2 (https=)

Cited By (5)

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CN115028679A (zh) * 2022-08-11 2022-09-09 深圳湾实验室 一种具有Cyclophilin A降解活性的PROTAC化合物及其制备方法与应用
WO2023131118A1 (zh) * 2022-01-04 2023-07-13 上海科技大学 基于bcl-2家族蛋白配体化合物开发的蛋白降解剂及它们的应用
WO2024078581A1 (en) * 2022-10-12 2024-04-18 Appicine Therapeutics (Hk) Limited Selective bcl-xl protac compounds and uses thereof
WO2024153185A1 (zh) * 2023-01-18 2024-07-25 苏州宜联生物医药有限公司 包含bcl-2家族蛋白降解剂的抗体药物偶联物及其制备方法和用途
WO2024169976A1 (zh) * 2023-02-17 2024-08-22 正大天晴药业集团股份有限公司 含有三氟甲磺酰基的化合物

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AU2021207672A1 (en) 2020-01-15 2022-07-14 University Of Florida Research Foundation, Incorporated Therapeutic agents and methods of treatment
WO2022072094A2 (en) * 2020-08-28 2022-04-07 University Of Florida Research Foundation, Incorporated Modulators of nuclear receptor subfamily 4 group a member 1 (nr4a1) and uses thereof
CN117794929A (zh) 2021-02-02 2024-03-29 法国施维雅药厂 选择性bcl-xl protac化合物及使用方法
CA3231175A1 (en) 2021-09-01 2023-03-09 Xizang Haisco Pharmaceutical Co., Ltd. Compound for degradation of bcl-2 family proteins and medical application thereof
US20240398764A1 (en) * 2021-10-12 2024-12-05 University Of Florida Research Foundation, Incorporated Methods of treating diseases associated with senescent cell accumulation
WO2023107606A1 (en) 2021-12-09 2023-06-15 University Of Florida Research Foundation, Incorporated Bcl-xl/bcl-2 dual degraders for treatment of cancers
AU2022424178A1 (en) 2021-12-30 2024-07-11 Beone Medicines I Gmbh Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
US20250282771A1 (en) 2022-05-06 2025-09-11 Treeline Biosciences, Inc. Tetrahydroisoquinoline heterobifunctional bcl-xl degraders
PE20250007A1 (es) 2022-05-06 2025-01-07 Treeline Biosciences Inc Degradadores bcl-xl-heterobifuncionales de tetrahidroisoquinolina
JP2025516359A (ja) 2022-05-06 2025-05-27 ツリーライン バイオサイエンシズ インコーポレイテッド テトラヒドロイソキノリンヘテロ二官能性ｂｃｌ－ｘｌ分解剤
JP2025533820A (ja) * 2022-10-03 2025-10-09 ユニバーシティ オブ フロリダ リサーチ ファウンデーション，インコーポレイティド セレブロン動員性Ｂｃｌ－ｘＬ／Ｂｃｌ－２二重分解剤
WO2025101571A1 (en) 2023-11-07 2025-05-15 Treeline Biosciences, Inc. Tetrahydroisoquinoline heterobifunctional bcl-x l degraders
WO2025101575A1 (en) 2023-11-07 2025-05-15 Treeline Biosciences, Inc. Tetrahydroisoquinoline heterobifunctional bcl-x l degraders
TW202527930A (zh) 2023-11-07 2025-07-16 美商樹線生物科學公司 四氫異喹啉異雙功能ｂｃｌ－ｘｌ降解劑
WO2026015489A1 (en) * 2024-07-08 2026-01-15 University Of Florida Research Foundation, Incorporated Bcl-xl/bcl-2 dual degraders and uses thereof

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US20160272639A1 (en) * 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2017024317A2 (en) * 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2017184995A1 (en) * 2016-04-21 2017-10-26 Bioventures, Llc Compounds that induce degradation of anti-apoptotic bcl-2 family proteins and the uses thereof

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EP3337476A4 (en) * 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
EP4491236A3 (en) * 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
JP2020514252A (ja) * 2016-12-08 2020-05-21 アイカーン スクール オブ メディスン アット マウント シナイ Ｃｄｋ４／６媒介性がんを治療するための組成物および方法
US20240398764A1 (en) * 2021-10-12 2024-12-05 University Of Florida Research Foundation, Incorporated Methods of treating diseases associated with senescent cell accumulation
WO2023107606A1 (en) * 2021-12-09 2023-06-15 University Of Florida Research Foundation, Incorporated Bcl-xl/bcl-2 dual degraders for treatment of cancers

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US20160272639A1 (en) * 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2017024317A2 (en) * 2015-08-06 2017-02-09 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
WO2017184995A1 (en) * 2016-04-21 2017-10-26 Bioventures, Llc Compounds that induce degradation of anti-apoptotic bcl-2 family proteins and the uses thereof
CN109152933A (zh) * 2016-04-21 2019-01-04 生物风险投资有限责任公司 诱导抗细胞凋亡bcl-2家族蛋白的降解的化合物及其用途

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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023131118A1 (zh) * 2022-01-04 2023-07-13 上海科技大学 基于bcl-2家族蛋白配体化合物开发的蛋白降解剂及它们的应用
CN115028679A (zh) * 2022-08-11 2022-09-09 深圳湾实验室 一种具有Cyclophilin A降解活性的PROTAC化合物及其制备方法与应用
WO2024078581A1 (en) * 2022-10-12 2024-04-18 Appicine Therapeutics (Hk) Limited Selective bcl-xl protac compounds and uses thereof
WO2024153185A1 (zh) * 2023-01-18 2024-07-25 苏州宜联生物医药有限公司 包含bcl-2家族蛋白降解剂的抗体药物偶联物及其制备方法和用途
WO2024169976A1 (zh) * 2023-02-17 2024-08-22 正大天晴药业集团股份有限公司 含有三氟甲磺酰基的化合物

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Publication number Publication date
AU2020218367A1 (en) 2021-08-12
WO2020163823A8 (en) 2020-10-01
EP3920923A2 (en) 2021-12-15
US20220169628A1 (en) 2022-06-02
WO2020163823A3 (en) 2020-10-29
JP2022520061A (ja) 2022-03-28
EP3920923A4 (en) 2022-10-26
KR20210137025A (ko) 2021-11-17
CA3127501A1 (en) 2020-08-13
WO2020163823A2 (en) 2020-08-13

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