CN114502535A - 一种RORγ调节剂的酸加成盐 - Google Patents

一种RORγ调节剂的酸加成盐 Download PDF

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CN114502535A
CN114502535A CN202080069974.9A CN202080069974A CN114502535A CN 114502535 A CN114502535 A CN 114502535A CN 202080069974 A CN202080069974 A CN 202080069974A CN 114502535 A CN114502535 A CN 114502535A
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formula
compound
acid addition
addition salt
pharmaceutically acceptable
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CN202080069974.9A
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CN114502535B (zh
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周先强
杜振兴
王捷
王林
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

一种RORγ的调节剂的酸加成盐。具体而言，涉及式II化合物的酸加成盐。更具体地，涉及式II化合物的苯甲酸盐、草酸盐、甲磺酸盐、马来酸盐、氢溴酸盐、盐酸盐、乙酸盐，以及式II化合物的苯甲酸盐晶型、苯甲酸盐无定型、草酸盐晶型、草酸盐无定型、甲磺酸盐无定型、马来酸盐B晶型、马来酸盐C晶型、马来酸盐D晶型、氢溴酸盐I晶型、盐酸盐α晶型、盐酸盐β晶型、盐酸盐γ晶型、乙酸盐晶型。

Description

PCT国内申请，说明书已公开。

Claims (27)

  1. PCT国内申请，权利要求书已公开。
CN202080069974.9A 2019-10-31 2020-10-30 一种RORγ调节剂的酸加成盐 Active CN114502535B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2019110499305 2019-10-31
CN201911049930 2019-10-31
PCT/CN2020/125125 WO2021083311A1 (zh) 2019-10-31 2020-10-30 一种RORγ调节剂的酸加成盐

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CN114502535A true CN114502535A (zh) 2022-05-13
CN114502535B CN114502535B (zh) 2024-04-12

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US (1) US20220411380A1 (zh)
EP (1) EP4053109A4 (zh)
JP (1) JP2023500291A (zh)
KR (1) KR20220093340A (zh)
CN (1) CN114502535B (zh)
AU (1) AU2020377114A1 (zh)
BR (1) BR112022008293A2 (zh)
CA (1) CA3156332A1 (zh)
MX (1) MX2022005260A (zh)
TW (1) TW202118751A (zh)
WO (1) WO2021083311A1 (zh)

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Publication number Priority date Publication date Assignee Title
WO2023232870A1 (en) 2022-05-31 2023-12-07 Immunic Ag Rorg/rorgt modulators for the treatment of virus infections like covid-19

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001016097A1 (en) * 1999-08-27 2001-03-08 Sugen, Inc. Phosphate mimics and methods of treatment using phosphatase inhibitors
US20070259936A1 (en) * 2006-05-03 2007-11-08 Player Mark R Benzimidazole Modulators of VR1
CN102906074A (zh) * 2010-05-24 2013-01-30 东亚荣养株式会社 稠合咪唑衍生物
CN104603118A (zh) * 2012-05-31 2015-05-06 菲尼克斯药品股份公司 作为孤儿核受体RORγ调节物的经甲酰胺或磺酰胺取代的噻唑及相关衍生物
CN105209453A (zh) * 2012-10-16 2015-12-30 詹森药业有限公司 ROR-γ-T的亚甲基连接的喹啉基调节剂
CN105829316A (zh) * 2013-12-19 2016-08-03 默克专利股份公司 作为RORγ抑制剂的四氢-四唑并[1，5-a]吡嗪
CN109071509A (zh) * 2016-01-29 2018-12-21 生命医药公司 作为ROR-γ的调节剂的苯并咪唑衍生物
CN109485595A (zh) * 2017-09-12 2019-03-19 江苏恒瑞医药股份有限公司 亲水性基团取代的吲哚甲酰胺类衍生物、其制备方法及其在医药上的应用

Family Cites Families (5)

* 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
PT3131902T (pt) 2014-04-14 2019-09-17 Boehringer Ingelheim Int Compostos como moduladores de ror gama
US9771374B2 (en) * 2014-07-25 2017-09-26 Innov17 Llc Benzimidazole retinoic acid receptor-related orphan receptor modulators and uses thereof
PL3781161T3 (pl) * 2018-05-03 2023-10-09 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Pochodne benzimidazolu jako modulatory receptora sierocego gamma związanego z retinoidami (rory) oraz ich zastosowania farmaceutyczne

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001016097A1 (en) * 1999-08-27 2001-03-08 Sugen, Inc. Phosphate mimics and methods of treatment using phosphatase inhibitors
US20070259936A1 (en) * 2006-05-03 2007-11-08 Player Mark R Benzimidazole Modulators of VR1
CN102906074A (zh) * 2010-05-24 2013-01-30 东亚荣养株式会社 稠合咪唑衍生物
CN104603118A (zh) * 2012-05-31 2015-05-06 菲尼克斯药品股份公司 作为孤儿核受体RORγ调节物的经甲酰胺或磺酰胺取代的噻唑及相关衍生物
CN105209453A (zh) * 2012-10-16 2015-12-30 詹森药业有限公司 ROR-γ-T的亚甲基连接的喹啉基调节剂
CN105829316A (zh) * 2013-12-19 2016-08-03 默克专利股份公司 作为RORγ抑制剂的四氢-四唑并[1，5-a]吡嗪
CN109071509A (zh) * 2016-01-29 2018-12-21 生命医药公司 作为ROR-γ的调节剂的苯并咪唑衍生物
CN109485595A (zh) * 2017-09-12 2019-03-19 江苏恒瑞医药股份有限公司 亲水性基团取代的吲哚甲酰胺类衍生物、其制备方法及其在医药上的应用

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Publication number Publication date
EP4053109A1 (en) 2022-09-07
WO2021083311A1 (zh) 2021-05-06
AU2020377114A1 (en) 2022-06-16
BR112022008293A2 (pt) 2022-07-26
EP4053109A4 (en) 2022-12-21
KR20220093340A (ko) 2022-07-05
JP2023500291A (ja) 2023-01-05
MX2022005260A (es) 2022-06-09
TW202118751A (zh) 2021-05-16
US20220411380A1 (en) 2022-12-29
CA3156332A1 (en) 2021-05-06
CN114502535B (zh) 2024-04-12

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