JP2022502393A - Ｎ−（１−（（２−（ジメチルアミノ）エチル）アミノ）−２−メチル−１−オキソプロパン−２−イル）−４−（４−（２−メチル−５−（（２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）−３，４，５−トリヒドロキシ−６−（メチルチオ）テトラヒドロ−２ｈ−ピラン−２−イル）ベンジル）フェニル）ブタンアミドの結晶形態及びそれらの合成方法 - Google Patents

Ｎ−（１−（（２−（ジメチルアミノ）エチル）アミノ）−２−メチル−１−オキソプロパン−２−イル）−４−（４−（２−メチル−５−（（２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）−３，４，５−トリヒドロキシ−６−（メチルチオ）テトラヒドロ−２ｈ−ピラン−２−イル）ベンジル）フェニル）ブタンアミドの結晶形態及びそれらの合成方法 Download PDF

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JP2022502393A
JP2022502393A JP2021516806A JP2021516806A JP2022502393A JP 2022502393 A JP2022502393 A JP 2022502393A JP 2021516806 A JP2021516806 A JP 2021516806A JP 2021516806 A JP2021516806 A JP 2021516806A JP 2022502393 A JP2022502393 A JP 2022502393A
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compound
methyl
degrees
pyran
tetrahydro
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JP2022502393A5 (https=
JPWO2020068661A5 (https=
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マーク スティーブン ベドナーズ
クアンチュ ダイ
ジェフリー マニング エッカート
ギャプ−キー リム
ローレン シロイス
ウェンシュエ ウー
マシュー マンジュ ジャオ
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レクシコン ファーマシューティカルズ インコーポレイテッド
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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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D207/10—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 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/10—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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)
  • Diabetes (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Obesity (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2021516806A 2018-09-26 2019-09-23 Ｎ−（１−（（２−（ジメチルアミノ）エチル）アミノ）−２−メチル−１−オキソプロパン−２−イル）−４−（４−（２−メチル−５−（（２ｓ，３ｒ，４ｒ，５ｓ，６ｒ）−３，４，５−トリヒドロキシ−６−（メチルチオ）テトラヒドロ−２ｈ−ピラン−２−イル）ベンジル）フェニル）ブタンアミドの結晶形態及びそれらの合成方法 Pending JP2022502393A (ja)

Applications Claiming Priority (3)

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US201862736871P 2018-09-26 2018-09-26
US62/736,871 2018-09-26
PCT/US2019/052414 WO2020068661A1 (en) 2018-09-26 2019-09-23 Crystalline forms of n-(1 -((2-(dimethylamino)ethyl)amino)-2-m ethyl-1 -oopropan-2-yl)-4-(4-(2-methyl-5- (2s,3r,4r,5s,6r)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2h-pyran-2-yl)benzyl) phenl)butanamide and methods of their synthesis

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JP2022502393A true JP2022502393A (ja) 2022-01-11
JP2022502393A5 JP2022502393A5 (https=) 2022-03-07
JPWO2020068661A5 JPWO2020068661A5 (https=) 2022-03-07

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US (1) US10968192B2 (https=)
EP (1) EP3856714A1 (https=)
JP (1) JP2022502393A (https=)
KR (1) KR20210065974A (https=)
CN (1) CN113039176A (https=)
AU (1) AU2019346497A1 (https=)
BR (1) BR112021004839A2 (https=)
CA (1) CA3113037A1 (https=)
CO (1) CO2021005141A2 (https=)
IL (1) IL281728A (https=)
MX (1) MX2021003545A (https=)
SG (1) SG11202102498UA (https=)
WO (1) WO2020068661A1 (https=)

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WO2021227439A1 (zh) * 2020-05-15 2021-11-18 上海喆邺生物科技有限公司 一种芳基葡糖苷衍生物
ES3040243T3 (en) * 2020-05-15 2025-10-29 Shanghai Zheye Biotechnology Co Ltd Aryl glucoside derivative and use thereof in drug
CN117018204A (zh) 2020-07-06 2023-11-10 诺未科技（北京）有限公司 一种治疗癌症的组合物及其应用和药物
WO2025101731A1 (en) 2023-11-10 2025-05-15 Lexicon Pharmaceuticals, Inc. Sglt1 inhibitors for use in the treatment of hepatic encephalopathy

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