CN113166061A - 含有磺酰基结构的RORγ抑制剂 - Google Patents

含有磺酰基结构的RORγ抑制剂 Download PDF

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CN113166061A
CN113166061A CN201980076661.3A CN201980076661A CN113166061A CN 113166061 A CN113166061 A CN 113166061A CN 201980076661 A CN201980076661 A CN 201980076661A CN 113166061 A CN113166061 A CN 113166061A
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substituted
alkyl
amino
compound
pharmaceutically acceptable
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CN113166061B (zh
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王小龙
阳安乐
姜洪建
蒋晓龙
陈磊
周建
徐宏江
宋伟
王晓金
耿晓函
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Nanjing Gearpharma Technology Co ltd
Chia Tai Tianqing Pharmaceutical Group Co Ltd
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Nanjing Gearpharma Technology Co ltd
Chia Tai Tianqing Pharmaceutical Group Co Ltd
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • 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
    • C07D211/72—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 hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D261/04—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
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    • C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D307/30—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/32—Oxygen atoms
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    • C07D333/46—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom
    • C07D333/48—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom by oxygen atoms
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    • C07D405/02—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 two hetero rings

Abstract

一类含有磺酰基结构的RORγ抑制剂，其制备方法，以及含有这些化合物的药物组合物。所述抑制剂具有式(I)或式(V)所示结构，式(I)化合物和式(V)化合物具有良好的RORγ抑制活性，有望用于治疗哺乳动物由RORγ受体介导的疾病。

Description

PCT国内申请，说明书已公开。

Claims (32)

  1. PCT国内申请，权利要求书已公开。
CN201980076661.3A 2018-11-27 2019-11-27 含有磺酰基结构的RORγ抑制剂 Active CN113166061B (zh)

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CN202311636222.8A CN117800904A (zh) 2018-11-27 2019-11-27 含有磺酰基结构的RORγ抑制剂

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CN2018114260604 2018-11-27
CN201811426060 2018-11-27
CN2019102435551 2019-03-28
CN201910243579 2019-03-28
CN201910243555 2019-03-28
CN2019102435797 2019-03-28
PCT/CN2019/121306 WO2020108538A1 (zh) 2018-11-27 2019-11-27 含有磺酰基结构的RORγ抑制剂

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Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4273135A1 (en) * 2020-12-31 2023-11-08 Scinnohub Pharmaceutical Co., Ltd Plasmin inhibitor, and preparation method therefor and application thereof
CN115557913A (zh) * 2021-07-02 2023-01-03 广东东阳光药业有限公司 苯并氮杂环类化合物及其在药物中的应用
CN113461608B (zh) * 2021-07-12 2023-03-17 江苏弘和药物研发有限公司 一种6-甲酰基烟酸甲酯的合成方法

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012027965A1 (en) * 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
WO2013029338A1 (en) * 2011-09-01 2013-03-07 Glaxo Group Limited Novel compounds
WO2013169864A2 (en) * 2012-05-08 2013-11-14 Lycera Corporation TETRAHYDRO[1,8]NAPHTHYRIDINE SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORƴ AND THE TREATMENT OF DISEASE
CN104379559A (zh) * 2012-04-27 2015-02-25 葛兰素集团有限公司 新化合物
CN104812393A (zh) * 2012-05-08 2015-07-29 默沙东公司 用于抑制RORγ活性和治疗疾病的四氢萘啶和相关双环化合物
CN106458991A (zh) * 2014-05-23 2017-02-22 豪夫迈·罗氏有限公司 苯磺酰胺衍生物和它们作为 rorc 调节剂的用途
WO2018116285A1 (en) * 2016-12-23 2018-06-28 Glenmark Pharmaceuticals S.A. Substituted morpholine derivatives as ror gamma modulators
CN108430974A (zh) * 2015-06-05 2018-08-21 领先制药控股公司 RORγ调节剂
CN108463458A (zh) * 2015-11-20 2018-08-28 生命医药公司 ROR-γ的调节剂
CN111094267A (zh) * 2017-09-30 2020-05-01 正大天晴药业集团股份有限公司 作为RORγ抑制剂的磺酰基取代的双环化合物

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012027965A1 (en) * 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
WO2013029338A1 (en) * 2011-09-01 2013-03-07 Glaxo Group Limited Novel compounds
CN104379559A (zh) * 2012-04-27 2015-02-25 葛兰素集团有限公司 新化合物
WO2013169864A2 (en) * 2012-05-08 2013-11-14 Lycera Corporation TETRAHYDRO[1,8]NAPHTHYRIDINE SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORƴ AND THE TREATMENT OF DISEASE
CN104812393A (zh) * 2012-05-08 2015-07-29 默沙东公司 用于抑制RORγ活性和治疗疾病的四氢萘啶和相关双环化合物
CN106458991A (zh) * 2014-05-23 2017-02-22 豪夫迈·罗氏有限公司 苯磺酰胺衍生物和它们作为 rorc 调节剂的用途
CN108430974A (zh) * 2015-06-05 2018-08-21 领先制药控股公司 RORγ调节剂
CN108463458A (zh) * 2015-11-20 2018-08-28 生命医药公司 ROR-γ的调节剂
WO2018116285A1 (en) * 2016-12-23 2018-06-28 Glenmark Pharmaceuticals S.A. Substituted morpholine derivatives as ror gamma modulators
CN111094267A (zh) * 2017-09-30 2020-05-01 正大天晴药业集团股份有限公司 作为RORγ抑制剂的磺酰基取代的双环化合物

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