CN111148747A - 吡啶并嘧啶类化合物的盐型和晶型及其制备方法 - Google Patents

吡啶并嘧啶类化合物的盐型和晶型及其制备方法 Download PDF

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Publication number
CN111148747A
CN111148747A CN201880061016.XA CN201880061016A CN111148747A CN 111148747 A CN111148747 A CN 111148747A CN 201880061016 A CN201880061016 A CN 201880061016A CN 111148747 A CN111148747 A CN 111148747A
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degrees
compound
crystalline form
formula
ray powder
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CN111148747B (zh
Inventor
沈竞康
孟韬
于霆
马兰萍
王昕�
陈驎
张永良
唐伟
杨文谦
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Shanghai Institute of Materia Medica of CAS
Shandong Luoxin Pharmaceutical Group Co Ltd
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Shanghai Institute of Materia Medica of CAS
Shandong Luoxin 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
    • A61K31/535—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
    • 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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

提供一种吡啶并嘧啶类化合物的盐型和晶型及其制备方法，具体公开了式(I)的化合物的游离碱、硫酸盐、其晶型及其制备方法，还包括这些盐型和晶型在制备用于治疗由PI3K‑Akt‑mTOR信号通路功能失调而导致的疾病或病症的药物中的应用。

Description

PCT国内申请，说明书已公开。

Claims (10)

  1. PCT国内申请，权利要求书已公开。
CN201880061016.XA 2017-11-07 2018-11-07 吡啶并嘧啶类化合物的盐型和晶型及其制备方法 Active CN111148747B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2017110851757 2017-11-07
CN201711085175 2017-11-07
PCT/CN2018/114354 WO2019091400A1 (zh) 2017-11-07 2018-11-07 吡啶并嘧啶类化合物的盐型和晶型及其制备方法

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CN111148747A true CN111148747A (zh) 2020-05-12
CN111148747B CN111148747B (zh) 2023-04-04

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102887895A (zh) * 2011-07-22 2013-01-23 山东轩竹医药科技有限公司 吡啶并嘧啶类mTOR抑制剂
CN103588792A (zh) * 2013-03-04 2014-02-19 中国科学院上海药物研究所 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途
WO2016150396A1 (zh) * 2015-03-25 2016-09-29 中国科学院上海药物研究所 取代吡啶并嘧啶类化合物的合成工艺

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102887895A (zh) * 2011-07-22 2013-01-23 山东轩竹医药科技有限公司 吡啶并嘧啶类mTOR抑制剂
CN103588792A (zh) * 2013-03-04 2014-02-19 中国科学院上海药物研究所 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途
WO2016150396A1 (zh) * 2015-03-25 2016-09-29 中国科学院上海药物研究所 取代吡啶并嘧啶类化合物的合成工艺

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
A.JOHN BLACKER ET AL.: "《Pharmaceutical Process Development Current Chemical and Engineering Challenges》", 31 December 2011, THE ROYAL SOCIETY OF CHEMISTRY *
赵桂森等主编: "《新药设计与开发基础》", 30 November 2015, 山东大学出版社 *

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WO2019091400A1 (zh) 2019-05-16
CN111148747B (zh) 2023-04-04

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