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CN109963836A - 氘原子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 - Google Patents

氘原子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 Download PDF

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Publication number
CN109963836A
CN109963836A CN201880004431.1A CN201880004431A CN109963836A CN 109963836 A CN109963836 A CN 109963836A CN 201880004431 A CN201880004431 A CN 201880004431A CN 109963836 A CN109963836 A CN 109963836A
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medicine
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atom replaces
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CN109963836B (zh
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刘�东
陈磊
陆标
刘苏星
张儒民
贺峰
陶维康
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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
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • 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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Indole Compounds (AREA)

Abstract

一种涉及氘原子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。特别地，涉及通式(I)所示的氘原子取代的吲哚甲酰胺类衍生物、其制备方法、含有该衍生物的药物组合物，其作为ROR激动剂的用途以及其用于预防和/或治疗肿瘤或癌症的用途，其中通式(I)中的各取代基与说明书中的定义相同。

Description

PCT国内申请，说明书已公开。

Claims (22)

  1. PCT国内申请，权利要求书已公开。
CN201880004431.1A 2017-09-12 2018-09-11 氘原子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 Active CN109963836B (zh)

Applications Claiming Priority (3)

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CN2017108171401 2017-09-12
CN201710817140 2017-09-12
PCT/CN2018/105008 WO2019052440A1 (zh) 2017-09-12 2018-09-11 氘原子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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CN109963836A true CN109963836A (zh) 2019-07-02
CN109963836B CN109963836B (zh) 2022-11-22

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US (1) US20200277278A1 (zh)
EP (1) EP3683206A4 (zh)
JP (1) JP2020533337A (zh)
CN (1) CN109963836B (zh)
AU (1) AU2018331125A1 (zh)
BR (1) BR112020004611A2 (zh)
CA (1) CA3075324A1 (zh)
TW (1) TW201912627A (zh)
WO (1) WO2019052440A1 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020140960A1 (zh) * 2019-01-04 2020-07-09 江苏恒瑞医药股份有限公司 吲哚甲酰胺类衍生物的晶型及其制备方法
TW202100513A (zh) * 2019-03-11 2021-01-01 大陸商江蘇恒瑞醫藥股份有限公司 氘原子取代的吲哚甲酰胺類衍生物的晶型及其製備方法
CN112745268B (zh) * 2019-10-31 2022-09-16 江苏恒瑞医药股份有限公司 苯并咪唑衍生物的晶型及制备方法

Citations (4)

* Cited by examiner, † Cited by third party
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US20160122318A1 (en) * 2014-11-05 2016-05-05 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ror-gamma
WO2017024018A1 (en) * 2015-08-05 2017-02-09 Vitae Pharmaceuticals, Inc. Modulators of ror-gamma
WO2017157332A1 (zh) * 2016-03-18 2017-09-21 江苏恒瑞医药股份有限公司 芳香酰胺类衍生物、其制备方法及其在医药上的应用
CN109952298A (zh) * 2017-07-06 2019-06-28 江苏恒瑞医药股份有限公司 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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DE19847943A1 (de) 1998-10-09 2000-04-13 Deutsche Telekom Ag Verfahren zum Generieren von digitalen Wasserzeichen für elekronische Dokumente
FR2863266B1 (fr) 2003-12-08 2006-01-27 Galderma Res & Dev NOUVEAUX LIGANDS ACTIVATEURS DES RECEPTEURS RARs, UTILISATION EN MEDECINES HUMAINE AINSI QU'EN COSMETIQUE
ATE414689T1 (de) 2003-12-08 2008-12-15 Galderma Res & Dev Biphenylderivate, die sich als rar-rezeptor- aktivierende liganden eignen, verfahren zu deren herstellung und deren verwendung in der humanmedizin und in kosmetika
US7476673B2 (en) 2003-12-30 2009-01-13 Allergan, Inc. Disubstituted chalcone oximes as selective agonists of RARγ retinoid receptors
FR2894960B1 (fr) 2005-12-15 2008-02-29 Galderma Res & Dev Derives biphenyliques agonistes selectifs du recepteurs rar-gamma
FR2894959B1 (fr) 2005-12-15 2008-02-29 Galderma Res & Dev Derives biphenyliques agonistes selectifs du recepteur rar-gamma
TW200815384A (en) 2006-08-25 2008-04-01 Viropharma Inc Combination therapy method for treating hepatitis C virus infection and pharmaceutical compositions for use therein
FR2915993B1 (fr) 2007-05-11 2009-07-03 Galderma Res & Dev Nouveaux ligands agonistes des recepteurs pars, utilisation en medecine humaine ainsi qu'en cosmetique.
JP2011037803A (ja) 2009-08-18 2011-02-24 Central Glass Co Ltd ホルミル基置換芳香族化合物の製造方法
EP2722329A1 (en) 2012-10-18 2014-04-23 F. Hoffmann-La Roche AG Indol-amide compounds as beta-amyloid inhbitors
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US20160122318A1 (en) * 2014-11-05 2016-05-05 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ror-gamma
WO2017024018A1 (en) * 2015-08-05 2017-02-09 Vitae Pharmaceuticals, Inc. Modulators of ror-gamma
WO2017157332A1 (zh) * 2016-03-18 2017-09-21 江苏恒瑞医药股份有限公司 芳香酰胺类衍生物、其制备方法及其在医药上的应用
CN109952298A (zh) * 2017-07-06 2019-06-28 江苏恒瑞医药股份有限公司 吲哚甲酰胺类衍生物、其制备方法及其在医药上的应用

Also Published As

Publication number Publication date
JP2020533337A (ja) 2020-11-19
EP3683206A4 (en) 2021-01-13
TW201912627A (zh) 2019-04-01
WO2019052440A1 (zh) 2019-03-21
AU2018331125A1 (en) 2020-03-05
EP3683206A1 (en) 2020-07-22
CA3075324A1 (en) 2019-03-21
BR112020004611A2 (pt) 2020-09-24
CN109963836B (zh) 2022-11-22
US20200277278A1 (en) 2020-09-03

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