CN102971312A - 吡咯取代的2-二氢吲哚酮衍生物、其制备方法及用途 - Google Patents

吡咯取代的2-二氢吲哚酮衍生物、其制备方法及用途 Download PDF

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CN102971312A
CN102971312A CN2011800278539A CN201180027853A CN102971312A CN 102971312 A CN102971312 A CN 102971312A CN 2011800278539 A CN2011800278539 A CN 2011800278539A CN 201180027853 A CN201180027853 A CN 201180027853A CN 102971312 A CN102971312 A CN 102971312A
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pyrroles
bases
dihydro
dimethyl
oxos
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CN102971312B (zh
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王晶翼
范传文
张龙
许柏岩
严守升
郭宗儒
张明会
林栋�
张占涛
周豪杰
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Qilu Pharmaceutical Co Ltd
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Qilu 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
    • A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/14—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
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

提供了式I所示的吡咯基取代的2-二氢吲哚酮衍生物、其药学上可接受的盐、溶剂合物或者所述盐的溶剂合物，它们是有效的酪氨酸激酶抑制剂。还提供了上述化合物的制备方法、含有这些化合物的药物组合物以及这些化合物在制备用于在哺乳动物(包括人类)中治疗或者辅助治疗由酪氨酸激酶介导的肿瘤或者酪氨酸激酶驱动的肿瘤细胞的增殖或迁移的药物的用途。

Description

PCT国内申请，说明书已公开。

Claims (1)

  1. PCT国内申请，权利要求书已公开。
CN201180027853.9A 2010-06-08 2011-03-31 吡咯取代的2-二氢吲哚酮衍生物、其制备方法及用途 Active CN102971312B (zh)

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CN201180027853.9A CN102971312B (zh) 2010-06-08 2011-03-31 吡咯取代的2-二氢吲哚酮衍生物、其制备方法及用途

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CN201010194609.9 2010-06-08
CN2010101946099A CN102276584A (zh) 2010-06-08 2010-06-08 吡咯取代的2-二氢吲哚酮衍生物、其制备方法及用途
PCT/CN2011/000561 WO2011153814A1 (zh) 2010-06-08 2011-03-31 吡咯取代的2-二氢吲哚酮衍生物、其制备方法及用途
CN201180027853.9A CN102971312B (zh) 2010-06-08 2011-03-31 吡咯取代的2-二氢吲哚酮衍生物、其制备方法及用途

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CN201180027853.9A Active CN102971312B (zh) 2010-06-08 2011-03-31 吡咯取代的2-二氢吲哚酮衍生物、其制备方法及用途

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US (1) US8637681B2 (zh)
EP (1) EP2581371B1 (zh)
JP (1) JP5938400B2 (zh)
KR (1) KR101760651B1 (zh)
CN (2) CN102276584A (zh)
CA (1) CA2801939C (zh)
WO (1) WO2011153814A1 (zh)

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EP2499133A2 (en) * 2009-11-12 2012-09-19 Ranbaxy Laboratories Limited Process for the preparation of crystalline form i of l-malic acid salt of sunitinib
CN104119321B (zh) * 2013-04-28 2017-09-08 齐鲁制药有限公司 二氢吲哚酮衍生物的二马来酸盐及其多晶型物
CN104829596B (zh) * 2014-02-10 2017-02-01 石家庄以岭药业股份有限公司 吡咯取代吲哚酮类衍生物、其制备方法、包含该衍生物的组合物、及其用途
CN105566302B (zh) * 2014-10-08 2018-08-14 齐鲁制药有限公司 二氢吲哚酮化合物及其盐的结晶
CN104387370A (zh) * 2014-10-22 2015-03-04 齐鲁制药有限公司 一种小分子酪氨酸激酶抑制剂的制备方法
CN112321568B (zh) * 2020-09-22 2023-02-17 南京中医药大学 4-甲基吡咯取代的吲哚酮衍生物、其制备方法及其医药用途
CN113133999B (zh) * 2021-04-28 2022-07-05 广州医科大学 蛇床子素及其衍生物在抑制醛酮还原酶中的应用
CN114213396B (zh) * 2022-01-27 2023-03-24 深圳市乐土生物医药有限公司 一种吲哚-2-酮类化合物及其制备方法与用途
WO2023168246A2 (en) * 2022-03-01 2023-09-07 Purdue Research Foundation Selective g protein-coupled receptor kinase 5 inhibitors, compositions, and methods of use

Citations (2)

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US20030069297A1 (en) * 2000-12-20 2003-04-10 Sugen, Inc. 4-aryl substituted indolinones
WO2007085205A1 (fr) * 2006-01-27 2007-08-02 Shanghai Hengrui Pharmaceutical Co.Ltd. Dérivés de 2-indolinone à substitution pyrolle, leurs procédés de préparation et leurs utilisations médicales

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
US20030069297A1 (en) * 2000-12-20 2003-04-10 Sugen, Inc. 4-aryl substituted indolinones
WO2007085205A1 (fr) * 2006-01-27 2007-08-02 Shanghai Hengrui Pharmaceutical Co.Ltd. Dérivés de 2-indolinone à substitution pyrolle, leurs procédés de préparation et leurs utilisations médicales

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
肖锋，等: "3-取代吲哚酮类化合物的合成及抗癌活性研究", 《有机化学》, vol. 29, no. 3, 31 December 2009 (2009-12-31), pages 459 - 461 *

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EP2581371A1 (en) 2013-04-17
EP2581371A4 (en) 2013-10-30
US20130158030A1 (en) 2013-06-20
CN102276584A (zh) 2011-12-14
WO2011153814A1 (zh) 2011-12-15
JP5938400B2 (ja) 2016-06-22
KR20130092541A (ko) 2013-08-20
EP2581371B1 (en) 2017-06-07
JP2013529220A (ja) 2013-07-18
CN102971312B (zh) 2014-10-29
US8637681B2 (en) 2014-01-28
CA2801939A1 (en) 2011-12-15
KR101760651B1 (ko) 2017-07-24
CA2801939C (en) 2015-11-24

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