CN113816952A - 吗啉衍生物的盐及其晶型、其制备方法及药物组合物、用途 - Google Patents

吗啉衍生物的盐及其晶型、其制备方法及药物组合物、用途 Download PDF

Info

Publication number
CN113816952A
CN113816952A CN202110801274.0A CN202110801274A CN113816952A CN 113816952 A CN113816952 A CN 113816952A CN 202110801274 A CN202110801274 A CN 202110801274A CN 113816952 A CN113816952 A CN 113816952A
Authority
CN
China
Prior art keywords
morpholine derivative
pharmaceutical composition
morpholine
degrees
malate
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN202110801274.0A
Other languages
English (en)
Chinese (zh)
Inventor
夏广新
谢建树
贾国慧
韩建生
上田直子
饭嶋彻
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shanghai Pharmaceuticals Holding Co Ltd
Original Assignee
Shanghai Pharmaceuticals Holding Co Ltd
Mitsubishi Tanabe Pharma Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Shanghai Pharmaceuticals Holding Co Ltd, Mitsubishi Tanabe Pharma Corp filed Critical Shanghai Pharmaceuticals Holding Co Ltd
Publication of CN113816952A publication Critical patent/CN113816952A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/33—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems
    • C07C309/34—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems formed by two rings
    • C07C309/35—Naphthalene sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/42—Separation; Purification; Stabilisation; Use of additives
    • C07C51/43—Separation; Purification; Stabilisation; Use of additives by change of the physical state, e.g. crystallisation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/08—Acetic acid
    • C07C53/10—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/255—Tartaric acid
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN202110801274.0A 2015-12-29 2016-12-29 吗啉衍生物的盐及其晶型、其制备方法及药物组合物、用途 Pending CN113816952A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2015110167833 2015-12-29
CN201511016783 2015-12-29
CN201611246909.0A CN106928218B (zh) 2015-12-29 2016-12-29 吗啉衍生物的盐及其晶型、其制备方法及药物组合物、用途

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201611246909.0A Division CN106928218B (zh) 2015-12-29 2016-12-29 吗啉衍生物的盐及其晶型、其制备方法及药物组合物、用途

Publications (1)

Publication Number Publication Date
CN113816952A true CN113816952A (zh) 2021-12-21

Family

ID=59224612

Family Applications (3)

Application Number Title Priority Date Filing Date
CN202110801274.0A Pending CN113816952A (zh) 2015-12-29 2016-12-29 吗啉衍生物的盐及其晶型、其制备方法及药物组合物、用途
CN202110794158.0A Active CN113816951B (zh) 2015-12-29 2016-12-29 吗啉衍生物的盐及其晶型、其制备方法及药物组合物、用途
CN201611246909.0A Active CN106928218B (zh) 2015-12-29 2016-12-29 吗啉衍生物的盐及其晶型、其制备方法及药物组合物、用途

Family Applications After (2)

Application Number Title Priority Date Filing Date
CN202110794158.0A Active CN113816951B (zh) 2015-12-29 2016-12-29 吗啉衍生物的盐及其晶型、其制备方法及药物组合物、用途
CN201611246909.0A Active CN106928218B (zh) 2015-12-29 2016-12-29 吗啉衍生物的盐及其晶型、其制备方法及药物组合物、用途

Country Status (11)

Country Link
US (1) US10519150B2 (https=)
EP (1) EP3398946B1 (https=)
JP (1) JP6818031B2 (https=)
CN (3) CN113816952A (https=)
DK (1) DK3398946T3 (https=)
ES (1) ES2918674T3 (https=)
HU (1) HUE059444T2 (https=)
PL (1) PL3398946T3 (https=)
PT (1) PT3398946T (https=)
TW (1) TWI705065B (https=)
WO (1) WO2017114456A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4209218A4 (en) * 2020-09-04 2024-09-11 Shanghai Pharmaceuticals Holding Co., Ltd. Application of nitrogen-containing saturated heterocyclic compound
WO2022047730A1 (en) * 2020-09-04 2022-03-10 Shanghai Pharmaceuticals Holding Co., Ltd. Methods to treat inflammatory bowel disease
CN116425677B (zh) * 2022-01-11 2026-04-14 苏州恩华生物医药科技有限公司 氨基环丁烷衍生物的盐、其晶型及其制备方法和应用

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1248869A2 (en) * 2000-01-07 2002-10-16 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
WO2012124775A1 (ja) * 2011-03-16 2012-09-20 田辺三菱製薬株式会社 含窒素飽和複素環化合物
WO2014042263A1 (ja) * 2012-09-14 2014-03-20 田辺三菱製薬株式会社 新規レニン阻害薬
JP5764628B2 (ja) * 2012-09-14 2015-08-19 田辺三菱製薬株式会社 医薬組成物

Also Published As

Publication number Publication date
EP3398946A4 (en) 2019-08-28
CN106928218B (zh) 2021-08-03
ES2918674T3 (es) 2022-07-19
JP6818031B2 (ja) 2021-01-20
CN113816951A (zh) 2021-12-21
EP3398946A1 (en) 2018-11-07
EP3398946B1 (en) 2022-05-04
JP2019500385A (ja) 2019-01-10
WO2017114456A1 (zh) 2017-07-06
PL3398946T3 (pl) 2022-10-10
US10519150B2 (en) 2019-12-31
DK3398946T3 (da) 2022-08-08
TW201722950A (zh) 2017-07-01
PT3398946T (pt) 2022-08-09
TWI705065B (zh) 2020-09-21
US20190016718A1 (en) 2019-01-17
CN113816951B (zh) 2022-09-27
HUE059444T2 (hu) 2022-11-28
CN106928218A (zh) 2017-07-07

Similar Documents

Publication Publication Date Title
TWI624447B (zh) 吡咯衍生物的結晶及其製造方法
CN105175473A (zh) 一种奥贝胆酸晶型i及其制备方法、药物组合物和用途
EP3205653A1 (en) Crystal form of bisulfate of jak inhibitor and preparation method therefor
WO2015014315A1 (zh) 一种抑制剂的晶型及其制备方法和用途
CN113816951B (zh) 吗啉衍生物的盐及其晶型、其制备方法及药物组合物、用途
KR20240000540A (ko) (s)-n-(3-(2-(((r)-1-하이드록시프로판-2-일)아미노)-6-모르폴리노피리딘-4-일)-4-메틸페닐)-3-(2,2,2-트리플루오로에틸)피롤리딘-1-카르복스아미드 및 이의 염의 고체 상태 형태
CN106279126B (zh) 阿法替尼酸加成盐及其晶型、其制备方法及药物组合物
WO2023137966A1 (zh) 一种徳拉沙星葡甲胺盐新晶型及其制备方法
AU2012283277B2 (en) Polymorphs of 6-(piperidin-4-yloxy)-2H-isoquinolin-1-one hydrochloride
AU2005261580A1 (en) S-tenatoprazole sodium monohydrate salt and the use thereof in the form of a proton pump inhibitor
EP3517529B1 (en) Salt of quinazoline derivative, preparation method therefor and application thereof
CN103819461B (zh) N-[3-氯-4-(3-氟苄氧基)苯基]-6-[5-[[2-(甲亚磺酰基)乙基]氨基]甲基]-2-呋喃基]-4-喹唑啉胺多晶型物及其制备方法
TW202611037A (zh) 替戈拉生富馬酸單乙酯、其製備方法、藥物組合物及用途
WO2025232904A1 (zh) 替戈拉生富马酸单乙酯、其制备方法、药物组合物及应用
WO2025167588A1 (zh) Zipalertinib的晶型及其制备方法和用途
WO2023061437A1 (zh) 抗肿瘤药物的盐及其晶型
WO2024169896A1 (zh) 一种苯并氮杂芳环衍生物的盐、晶型及其在医药上的应用
CN121627657A (zh) 呋喹替尼的晶型及其制备方法
CN105732596A (zh) N-[3-氯-4-(3-氟苄氧基)苯基]-6-[5-[[2-(甲亚磺酰基)乙基]氨基]甲基]-2-呋喃基]-4-喹唑啉胺多晶型物及其制备方法
US20060270685A1 (en) Anhydrous ziprasidone mesylate and a process for its preparation

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
TA01 Transfer of patent application right

Effective date of registration: 20250620

Address after: 201203 Pudong New Area Zhangjiang Road, Shanghai, No. 92

Applicant after: SHANGHAI PHARMACEUTICALS HOLDING Co.,Ltd.

Country or region after: China

Address before: 201203 Pudong New Area Zhangjiang Road, Shanghai, No. 92

Applicant before: SHANGHAI PHARMACEUTICALS HOLDING Co.,Ltd.

Country or region before: China

Applicant before: MITSUBISHI TANABE PHARMA Corp.

Country or region before: Japan

TA01 Transfer of patent application right