TWI705065B - 嗎啉衍生物的鹽及其晶型、其製備方法及藥物組成物、用途 - Google Patents

嗎啉衍生物的鹽及其晶型、其製備方法及藥物組成物、用途 Download PDF

Info

Publication number
TWI705065B
TWI705065B TW105143910A TW105143910A TWI705065B TW I705065 B TWI705065 B TW I705065B TW 105143910 A TW105143910 A TW 105143910A TW 105143910 A TW105143910 A TW 105143910A TW I705065 B TWI705065 B TW I705065B
Authority
TW
Taiwan
Prior art keywords
morpholine derivative
morpholine
patent application
scope
tartrate
Prior art date
Application number
TW105143910A
Other languages
English (en)
Chinese (zh)
Other versions
TW201722950A (zh
Inventor
夏廣新
謝建樹
賈國慧
韓建生
上田直子
飯嶋徹
Original Assignee
大陸商上海醫藥集團股份有限公司
日商田邊三菱製藥股份有限公司
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 大陸商上海醫藥集團股份有限公司, 日商田邊三菱製藥股份有限公司 filed Critical 大陸商上海醫藥集團股份有限公司
Publication of TW201722950A publication Critical patent/TW201722950A/zh
Application granted granted Critical
Publication of TWI705065B publication Critical patent/TWI705065B/zh

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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
TW105143910A 2015-12-29 2016-12-29 嗎啉衍生物的鹽及其晶型、其製備方法及藥物組成物、用途 TWI705065B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201511016783.3 2015-12-29
CN201511016783 2015-12-29

Publications (2)

Publication Number Publication Date
TW201722950A TW201722950A (zh) 2017-07-01
TWI705065B true TWI705065B (zh) 2020-09-21

Family

ID=59224612

Family Applications (1)

Application Number Title Priority Date Filing Date
TW105143910A TWI705065B (zh) 2015-12-29 2016-12-29 嗎啉衍生物的鹽及其晶型、其製備方法及藥物組成物、用途

Country Status (11)

Country Link
US (1) US10519150B2 (OSRAM)
EP (1) EP3398946B1 (OSRAM)
JP (1) JP6818031B2 (OSRAM)
CN (3) CN106928218B (OSRAM)
DK (1) DK3398946T3 (OSRAM)
ES (1) ES2918674T3 (OSRAM)
HU (1) HUE059444T2 (OSRAM)
PL (1) PL3398946T3 (OSRAM)
PT (1) PT3398946T (OSRAM)
TW (1) TWI705065B (OSRAM)
WO (1) WO2017114456A1 (OSRAM)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022048614A1 (zh) 2020-09-04 2022-03-10 上海医药集团股份有限公司 一种含氮的饱和杂环化合物的应用
WO2022047730A1 (en) * 2020-09-04 2022-03-10 Shanghai Pharmaceuticals Holding Co., Ltd. Methods to treat inflammatory bowel disease
CN116425677A (zh) * 2022-01-11 2023-07-14 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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201242955A (en) * 2011-03-16 2012-11-01 Mitsubishi Tanabe Pharma Corp Nitrogen-containing heterocyclic compound

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2930501A (en) * 2000-01-07 2001-07-24 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
JP5764628B2 (ja) * 2012-09-14 2015-08-19 田辺三菱製薬株式会社 医薬組成物
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201242955A (en) * 2011-03-16 2012-11-01 Mitsubishi Tanabe Pharma Corp Nitrogen-containing heterocyclic compound

Also Published As

Publication number Publication date
EP3398946B1 (en) 2022-05-04
JP6818031B2 (ja) 2021-01-20
PT3398946T (pt) 2022-08-09
DK3398946T3 (da) 2022-08-08
TW201722950A (zh) 2017-07-01
EP3398946A4 (en) 2019-08-28
JP2019500385A (ja) 2019-01-10
HUE059444T2 (hu) 2022-11-28
CN113816951B (zh) 2022-09-27
CN106928218A (zh) 2017-07-07
ES2918674T3 (es) 2022-07-19
CN106928218B (zh) 2021-08-03
EP3398946A1 (en) 2018-11-07
US20190016718A1 (en) 2019-01-17
CN113816951A (zh) 2021-12-21
CN113816952A (zh) 2021-12-21
WO2017114456A1 (zh) 2017-07-06
US10519150B2 (en) 2019-12-31
PL3398946T3 (pl) 2022-10-10

Similar Documents

Publication Publication Date Title
JP7407740B2 (ja) Ｔｌｒ７／ｔｌｒ８阻害剤の結晶形態
AU2014239995B2 (en) Salt of omecamtiv mecarbil and process for preparing salt
JP2020183408A (ja) ｛［５−（３−クロロフェニル）−３−ヒドロキシピリジン−２−カルボニル］アミノ｝酢酸の固体形態、組成物、及びその使用
JP2020100624A (ja) Ｌ−オルニチンフェニルアセテートおよびその製造方法
JP2003531173A (ja) ゾルピデムヘミタートレイト
KR20170057441A (ko) Jak 억제제의 바이설페이트의 결정형 및 이의 제조방법
WO2015014315A1 (zh) 一种抑制剂的晶型及其制备方法和用途
TWI705065B (zh) 嗎啉衍生物的鹽及其晶型、其製備方法及藥物組成物、用途
JP2024517431A (ja) （ｓ）－ｎ－（３－（２－（（（ｒ）－１－ヒドロキシプロパン－２－イル）アミノ）－６－モルホリノピリジン－４－イル）－４－メチルフェニル）－３－（２，２，２－トリフルオロエチル）ピロリジン－１－カルボキサミドおよびその塩の固体状態での形態
TW200900392A (en) Novel crystalline bepotastine metal salt hydrate, method for preparing same, and pharmaceutical composition comprising same
WO2025241792A1 (zh) 艾拉司群二盐酸盐的新晶型及其制备方法和用途
WO2020065667A1 (en) Novel polymorphs of acalabrutinib, a bruton's tyrosine kinase inhibitor
WO2023137966A1 (zh) 一种徳拉沙星葡甲胺盐新晶型及其制备方法
JP6317358B2 (ja) Ｌ‐リジンを含む（３ｓ，３ｓ’）４，４’‐ジスルファンジイルビス（３‐アミノブタン１‐スルホン酸）の新規結晶相
CN101981004B (zh) 晶体形式
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
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
EP3517529B1 (en) Salt of quinazoline derivative, preparation method therefor and application thereof
CN120058671A (zh) 沃诺拉赞半富马酸盐及其制备方法
WO2023061437A1 (zh) 抗肿瘤药物的盐及其晶型
WO2024027013A1 (zh) 一种依洛西巴特晶型ii及其制备方法
WO2022224269A1 (en) Co-crystals, salts and solid forms of niraparib
US20060270685A1 (en) Anhydrous ziprasidone mesylate and a process for its preparation
WO2015113314A1 (zh) 3-(4-氨基-1,3-二氢-1-氧代-2h-异吲哚-2-基)-2,6-哌啶二酮新晶型及其制备方法