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

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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
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Taiwan
Prior art keywords
morpholine derivative
morpholine
patent application
scope
tartrate
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TW105143910A
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English (en)
Chinese (zh)
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TW201722950A (zh
Inventor
夏廣新
謝建樹
賈國慧
韓建生
上田直子
飯嶋徹
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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
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (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 2015-12-29
CN201511016783.3 2015-12-29

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

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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

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US (1) US10519150B2 (cg-RX-API-DMAC10.html)
EP (1) EP3398946B1 (cg-RX-API-DMAC10.html)
JP (1) JP6818031B2 (cg-RX-API-DMAC10.html)
CN (3) CN113816951B (cg-RX-API-DMAC10.html)
DK (1) DK3398946T3 (cg-RX-API-DMAC10.html)
ES (1) ES2918674T3 (cg-RX-API-DMAC10.html)
HU (1) HUE059444T2 (cg-RX-API-DMAC10.html)
PL (1) PL3398946T3 (cg-RX-API-DMAC10.html)
PT (1) PT3398946T (cg-RX-API-DMAC10.html)
TW (1) TWI705065B (cg-RX-API-DMAC10.html)
WO (1) WO2017114456A1 (cg-RX-API-DMAC10.html)

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Publication number Priority date Publication date Assignee Title
WO2022047730A1 (en) * 2020-09-04 2022-03-10 Shanghai Pharmaceuticals Holding Co., Ltd. Methods to treat inflammatory bowel disease
KR102898913B1 (ko) * 2020-09-04 2025-12-10 상하이 파마슈티컬스 홀딩 컴퍼니 리미티드 질소 함유 포화 헤테로사이클릭 화합물의 응용
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

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

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL150524A0 (en) * 2000-01-07 2003-02-12 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

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

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