CN111032644A - 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物 - Google Patents

用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物 Download PDF

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CN111032644A
CN111032644A CN201880055633.9A CN201880055633A CN111032644A CN 111032644 A CN111032644 A CN 111032644A CN 201880055633 A CN201880055633 A CN 201880055633A CN 111032644 A CN111032644 A CN 111032644A
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compound
alkyl
formula
hydroxy
pharmaceutically acceptable
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CN111032644B (zh
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沈春莉
吴成德
陈胜林
陈曙辉
张喜全
田心
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
Medshine Discovery Inc
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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
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    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
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    • C07D401/14—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 three or more hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

本申请属于医药领域，具体而言涉及用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物或其药学上可接受的盐、其制备方法、含有该化合物的药物组合物、以及其在治疗雄激素介导的细胞增殖性疾病中的用途。本申请的化合物具有良好的雄激素受体拮抗作用，表现出优异的抗肿瘤效果。

Description

PCT国内申请，说明书已公开。

Claims (85)

  1. PCT国内申请，权利要求书已公开。
CN201880055633.9A 2017-08-07 2018-08-07 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物 Active CN111032644B (zh)

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CN202110900404.6A CN113582977B (zh) 2017-08-07 2018-08-07 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物
CN202110901351.XA CN113563311A (zh) 2017-08-07 2018-08-07 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物

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CN2017106678604 2017-08-07
CN201710667860 2017-08-07
CN201810333652 2018-04-13
CN2018103336525 2018-04-13
PCT/CN2018/099161 WO2019029521A1 (zh) 2017-08-07 2018-08-07 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物

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CN202110900404.6A Division CN113582977B (zh) 2017-08-07 2018-08-07 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物

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CN111032644B (zh) 2017-08-07 2021-08-10 正大天晴药业集团股份有限公司 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物
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CN110452166A (zh) * 2019-09-06 2019-11-15 浙江朗华制药有限公司 一种5-异硫氰酰基-3-三氟甲基-2-氰基吡啶的制备方法
WO2021143925A1 (zh) * 2020-01-19 2021-07-22 正大天晴药业集团股份有限公司 作为ar拮抗剂的二芳基硫代乙内酰脲化合物
WO2024088395A1 (zh) * 2022-10-28 2024-05-02 南京明德新药研发有限公司 桥环类化合物及其在药学上的应用

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109422737A (zh) * 2017-08-22 2019-03-05 上海时莱生物技术有限公司 咪唑酮类雄激素受体拮抗剂、其制备方法和用途
CN109422737B (zh) * 2017-08-22 2021-07-30 上海时莱生物技术有限公司 咪唑酮类雄激素受体拮抗剂、其制备方法和用途

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US11332465B2 (en) 2022-05-17
AU2018314980B2 (en) 2022-05-19
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CN111032644B (zh) 2021-08-10
WO2019029521A1 (zh) 2019-02-14
CA3072269A1 (en) 2019-02-14
US20230035184A1 (en) 2023-02-02
KR102658095B1 (ko) 2024-04-19
CN113582977B (zh) 2023-04-14
JP2020530490A (ja) 2020-10-22
EP3666772A1 (en) 2020-06-17
US20200277290A1 (en) 2020-09-03
CN113582977A (zh) 2021-11-02
JP7285838B2 (ja) 2023-06-02
KR20200043407A (ko) 2020-04-27
AU2018314980A1 (en) 2020-03-05
CN113563311A (zh) 2021-10-29

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