JP2021091683A - ２−（（４−（（Ｓ）−２−（５−クロロピリジン−２−イル）−２−メチルベンゾ［ｄ］［１，３］ジオキソール−４−イル）ピペリジン−１−イル）メチル）−１−（（（Ｓ）−オキセタン−２−イル）メチル）−１Ｈ−ベンゾ［ｄ］イミダゾール−６−カルボン酸の１，３−ジヒドロキシ−２−（ヒドロキシメチル）プロパン−２−アミン塩の固体形態 - Google Patents

２−（（４−（（Ｓ）−２−（５−クロロピリジン−２−イル）−２−メチルベンゾ［ｄ］［１，３］ジオキソール−４−イル）ピペリジン−１−イル）メチル）−１−（（（Ｓ）−オキセタン−２−イル）メチル）−１Ｈ−ベンゾ［ｄ］イミダゾール−６−カルボン酸の１，３−ジヒドロキシ−２−（ヒドロキシメチル）プロパン−２−アミン塩の固体形態 Download PDF

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JP2021091683A
JP2021091683A JP2020202383A JP2020202383A JP2021091683A JP 2021091683 A JP2021091683 A JP 2021091683A JP 2020202383 A JP2020202383 A JP 2020202383A JP 2020202383 A JP2020202383 A JP 2020202383A JP 2021091683 A JP2021091683 A JP 2021091683A
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disease
compound
methyl
tris salt
salt
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JP2021091683A5 (https=
Inventor
ギャリー・イー・アスプネス
E Aspnes Gary
スコット・ダブリュー・バグリー
W Bagley Scott
ウェスリー・デウィット・クラーク
Dewitt Clark Wesley
ジョン・エム・カート
M Curto John
デビッド・ジェームズ・エドモンズ
James Edmonds David
マーク・イー・フラナガン
e flanagan Mark
建太郎 二木
Kentaro Futatsugi
建太郎 二木
デビッド・アンドリュー・グリフィス
Andrew Griffith David
キム・ウアード
Kim Huard
ヤジン・リアン
Yajing Lian
クリス・リンベラキス
Limberakis Chris
アリン・ティー・ロンドレーガン
T Londregan Allyn
アラン・エム・マシオウェツ
M Mathiowetz Alan
デビッド・ウォルター・ピオトロウスキー
Walter Piotrowski David
ロジャー・ビー・ラッゲリ
B Ruggeri Roger
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Pfizer Inc
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Pfizer Inc
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Publication of JP2021091683A5 publication Critical patent/JP2021091683A5/ja
Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/10—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2020202383A 2019-12-10 2020-12-07 ２−（（４−（（Ｓ）−２−（５−クロロピリジン−２−イル）−２−メチルベンゾ［ｄ］［１，３］ジオキソール−４−イル）ピペリジン−１−イル）メチル）−１−（（（Ｓ）−オキセタン−２−イル）メチル）−１Ｈ−ベンゾ［ｄ］イミダゾール−６−カルボン酸の１，３−ジヒドロキシ−２−（ヒドロキシメチル）プロパン−２−アミン塩の固体形態 Withdrawn JP2021091683A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962946084P 2019-12-10 2019-12-10
US62/946,084 2019-12-10

Publications (2)

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JP2021091683A true JP2021091683A (ja) 2021-06-17
JP2021091683A5 JP2021091683A5 (https=) 2023-08-10

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JP2020202383A Withdrawn JP2021091683A (ja) 2019-12-10 2020-12-07 ２−（（４−（（Ｓ）−２−（５−クロロピリジン−２−イル）−２−メチルベンゾ［ｄ］［１，３］ジオキソール−４−イル）ピペリジン−１−イル）メチル）−１−（（（Ｓ）−オキセタン−２−イル）メチル）−１Ｈ−ベンゾ［ｄ］イミダゾール−６−カルボン酸の１，３−ジヒドロキシ−２−（ヒドロキシメチル）プロパン−２−アミン塩の固体形態

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Country Link
US (1) US20230045419A1 (https=)
EP (1) EP4073028A1 (https=)
JP (1) JP2021091683A (https=)
KR (1) KR20220112811A (https=)
CN (1) CN115175893A (https=)
AR (1) AR120703A1 (https=)
AU (1) AU2020402177A1 (https=)
BR (1) BR112022010599A2 (https=)
CA (1) CA3163979A1 (https=)
MX (1) MX2022007105A (https=)
TW (1) TWI809334B (https=)
WO (1) WO2021116874A1 (https=)
ZA (1) ZA202207589B (https=)

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MA54555A (fr) 2018-11-22 2021-09-29 Qilu Regor Therapeutics Inc Agonistes de glp-1r et leurs utilisations
EP3953344A4 (en) 2019-04-12 2023-08-09 Qilu Regor Therapeutics Inc. GLP-IR AGONISTS AND THEIR USES
US12065434B2 (en) 2020-12-15 2024-08-20 Pfizer Inc. Metabolites of GLP1R agonists
US20220193063A1 (en) * 2020-12-15 2022-06-23 Pfizer Inc. Metabolites of glp1r agonists
PT4408840T (pt) 2021-09-27 2025-10-07 Terns Pharmaceuticals Inc Ácidos benzimidazolocarboxílicos como agonistas de glp-1r
US20250115612A1 (en) 2021-10-05 2025-04-10 Astrazeneca Ab Certain 2,5-diazabicyclo[4.2.0]octanes and octahydrofuro[3,4-b]pyrazines as glp-1 receptor modulators
MX2024004131A (es) 2021-10-05 2024-04-22 Astrazeneca Ab Ciertos 2,5-diazabiciclo[4.2.0]octanos como moduladores del receptor de glp-1.
WO2023057414A1 (en) 2021-10-05 2023-04-13 Astrazeneca Ab Certain octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators
CN118401519A (zh) 2021-10-25 2024-07-26 拓臻制药公司 作为glp-1r激动剂的化合物
US20250042882A1 (en) 2021-12-16 2025-02-06 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
WO2023111144A1 (en) 2021-12-16 2023-06-22 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
CN119095843A (zh) 2022-02-23 2024-12-06 拓臻制药公司 作为glp-1r激动剂的化合物
US20250214968A1 (en) * 2022-03-25 2025-07-03 Ildong Pharmaceutical Co., Ltd. Novel Salt of GLP-1 Receptor Agonist Compound, Preparation Method Thereof and Pharmaceutical Composition Comprising Thereof
WO2023228023A1 (en) 2022-05-23 2023-11-30 Pfizer Inc. Treatment of type 2 diabetes or weight management control with 2-((4-((s)-2-(5-chloropyridin-2-yl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-benzo[d]imidazole-6-carboxylic acid or a pharmaceutically salt thereof
CN117362282B (zh) * 2022-07-07 2026-04-21 杭州德睿智药科技有限公司 Glp-1r激动剂的盐及其制备方法和应用
CN116217522B (zh) * 2023-02-22 2025-06-24 广东莱佛士制药技术有限公司 Glp-1受体激动剂关键中间体的手性纯化方法
EP4568664B1 (en) 2023-04-07 2026-04-01 Terns Pharmaceuticals, Inc. Combination comprising a thr-beta agonist and a glp-1r agonist for use in treating obesity
CN118812522A (zh) * 2023-04-21 2024-10-22 苏州闻泰医药科技有限公司 一种glp-1r受体激动剂化合物盐、其晶型、其制备方法和应用
CN120981457A (zh) 2023-09-14 2025-11-18 歌礼制药(中国)有限公司 Glp-1r激动剂及其治疗方法
TW202521534A (zh) 2023-11-24 2025-06-01 香港商歌禮製藥(中國)有限公司 Glp-1r 激動劑及其治療方法

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US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
US5013556A (en) 1989-10-20 1991-05-07 Liposome Technology, Inc. Liposomes with enhanced circulation time
WO2008012623A1 (en) * 2006-07-25 2008-01-31 Pfizer Products Inc. Benzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
HRP20161178T1 (hr) 2010-09-30 2016-11-04 Pfizer Inc. N1-PIRAZOLOSPIROKETONSKI INHIBITORI ACETIL-CoA-KARBOKSILAZE
CU24152B1 (es) 2010-12-20 2016-02-29 Irm Llc 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr
SI3397631T1 (sl) 2015-12-29 2022-01-31 Pfizer Inc. Substituirani 3-azabiciklo(3.1.0)heksani kot zaviralci ketoheksokinaze
AR109179A1 (es) 2016-08-19 2018-11-07 Pfizer Inhibidores de diacilglicerol aciltransferasa 2
KR102314286B1 (ko) * 2016-12-16 2021-10-21 화이자 인코포레이티드 Glp-1 수용체 작용제 및 이의 용도
US10934279B2 (en) * 2018-06-13 2021-03-02 Pfizer Inc. GLP-1 receptor agonists and uses thereof
WO2020234726A1 (en) * 2019-05-20 2020-11-26 Pfizer Inc. Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases

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TWI809334B (zh) 2023-07-21
CA3163979A1 (en) 2021-06-17
AR120703A1 (es) 2022-03-09
TW202136247A (zh) 2021-10-01
AU2020402177A1 (en) 2022-06-16
BR112022010599A2 (pt) 2022-08-16
WO2021116874A1 (en) 2021-06-17
EP4073028A1 (en) 2022-10-19
CN115175893A (zh) 2022-10-11
ZA202207589B (en) 2023-04-26
MX2022007105A (es) 2022-07-11
KR20220112811A (ko) 2022-08-11
US20230045419A1 (en) 2023-02-09

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