CN111065636A - 稠合杂芳基衍生物、其制备方法及其在医药上的应用 - Google Patents

稠合杂芳基衍生物、其制备方法及其在医药上的应用 Download PDF

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CN111065636A
CN111065636A CN201880058416.5A CN201880058416A CN111065636A CN 111065636 A CN111065636 A CN 111065636A CN 201880058416 A CN201880058416 A CN 201880058416A CN 111065636 A CN111065636 A CN 111065636A
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CN111065636B (zh
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张国宝
马殿强
贺峰
陶维康
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Shandong Shengdi Pharmaceutical Co ltd
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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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
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    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
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  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

提供一类稠合杂芳基衍生物、其制备方法及其在医药上的应用。具体而言，提供一种通式(I)所示的稠合杂芳基衍生物、其制备方法及含有该衍生物的药物组合物以及其作为治疗剂，特别是作为TLR7激动剂的用途，其中通式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 (26)

  1. PCT国内申请，权利要求书已公开。
CN201880058416.5A 2017-09-22 2018-09-21 稠合杂芳基衍生物、其制备方法及其在医药上的应用 Active CN111065636B (zh)

Applications Claiming Priority (3)

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CN201710866425 2017-09-22
CN2017108664254 2017-09-22
PCT/CN2018/106983 WO2019057158A1 (zh) 2017-09-22 2018-09-21 稠合杂芳基衍生物、其制备方法及其在医药上的应用

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CN111065636A true CN111065636A (zh) 2020-04-24
CN111065636B CN111065636B (zh) 2022-08-23

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TW (1) TW201915000A (zh)
WO (1) WO2019057158A1 (zh)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102272134A (zh) * 2008-12-09 2011-12-07 吉里德科学公司 Toll样受体调节剂
CN102439011A (zh) * 2009-02-11 2012-05-02 加利福尼亚大学校务委员会 Toll样受体调节剂和疾病的治疗
WO2013117615A1 (en) * 2012-02-08 2013-08-15 Janssen R&D Ireland Piperidino-pyrimidine derivatives for the treatment of viral infections
CN107074860A (zh) * 2014-09-16 2017-08-18 吉利德科学公司 制备toll样受体调节剂的方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MD20170081A2 (ro) * 2015-03-04 2018-03-31 Gilead Sciences, Inc. Compuşi 4,6-diamino-pirido[3,2-D]pirimidină modulatori ai receptorilor de tip Toll

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102272134A (zh) * 2008-12-09 2011-12-07 吉里德科学公司 Toll样受体调节剂
CN103497192A (zh) * 2008-12-09 2014-01-08 吉里德科学公司 Toll 样受体调节剂
CN102439011A (zh) * 2009-02-11 2012-05-02 加利福尼亚大学校务委员会 Toll样受体调节剂和疾病的治疗
WO2013117615A1 (en) * 2012-02-08 2013-08-15 Janssen R&D Ireland Piperidino-pyrimidine derivatives for the treatment of viral infections
CN107074860A (zh) * 2014-09-16 2017-08-18 吉利德科学公司 制备toll样受体调节剂的方法

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
EMMANUEL H. DEMONT ET AL.: "Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors", 《J. MED. CHEM》 *
PAUL BAMBOROUGH ET AL.: "Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors", 《J. MED. CHEM》 *

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CN111065636B (zh) 2022-08-23
TW201915000A (zh) 2019-04-16

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Address after: 222047 No. 7 Kunlun Shan Road, Lianyungang economic and Technological Development Zone, Jiangsu

Patentee after: JIANGSU HENGRUI MEDICINE Co.,Ltd.

Patentee after: Shandong Shengdi Pharmaceutical Co.,Ltd.

Patentee after: SHANGHAI HENGRUI PHARMACEUTICAL Co.,Ltd.

Address before: 222047 No. 7 Kunlun Shan Road, Lianyungang economic and Technological Development Zone, Jiangsu

Patentee before: JIANGSU HENGRUI MEDICINE Co.,Ltd.

Patentee before: SHANGHAI HENGRUI PHARMACEUTICAL Co.,Ltd.