CN111954669A - Nhe3抑制剂的晶型a及其制备方法和应用 - Google Patents

Nhe3抑制剂的晶型a及其制备方法和应用 Download PDF

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Publication number
CN111954669A
CN111954669A CN201980003171.0A CN201980003171A CN111954669A CN 111954669 A CN111954669 A CN 111954669A CN 201980003171 A CN201980003171 A CN 201980003171A CN 111954669 A CN111954669 A CN 111954669A
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preparation
pharmaceutical composition
organic solvent
prepared
medicament
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CN201980003171.0A
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CN111954669B (zh
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任国宾
弋东旭
黄嘉骏
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Shenzhen Rentai Pharmaceutical Technology Co Ltd
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Shenzhen Rentai Pharmaceutical Technology Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • C07D217/16—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
    • 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

Abstract

N，N’‑(10,17‑二氧代‑3，6，21，24‑四氧杂‑9，11，16，18‑四氮杂二十六碳烷‑1，26‑二基)双(4‑(6，8‑二氯‑2‑甲基‑1，2，3，‑四氢异喹啉‑4‑基)苯磺酰胺的晶型A，该晶型具有良好的光照稳定性、高温稳定性和高湿稳定性。

Description

PCT国内申请，说明书已公开。

Claims (23)

  1. PCT国内申请，权利要求书已公开。
CN201980003171.0A 2019-03-14 2019-03-14 Nhe3抑制剂的晶型a及其制备方法和应用 Active CN111954669B (zh)

Applications Claiming Priority (1)

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PCT/CN2019/078165 WO2020181555A1 (zh) 2019-03-14 2019-03-14 Nhe3抑制剂的晶型a及其制备方法和应用

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CN111954669B CN111954669B (zh) 2023-04-07

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US (1) US20210403450A1 (zh)
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WO (1) WO2020181555A1 (zh)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103819403A (zh) * 2008-12-31 2014-05-28 阿德利克斯公司 用于治疗与体液潴留或盐超负荷有关的病症和胃肠道病症的化合物和方法
WO2018129552A1 (en) * 2017-01-09 2018-07-12 Ardelyx, Inc. Compounds useful for treating gastrointestinal tract disorders

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2983667B1 (en) * 2013-04-12 2019-03-20 Ardelyx, Inc. Nhe3-binding compounds and methods for inhibiting phosphate transport
AU2018206479B2 (en) * 2017-01-09 2022-07-14 Ardelyx, Inc. Inhibitors of NHE-mediated antiport
WO2019091503A1 (en) * 2017-11-13 2019-05-16 Zentiva K.S. Solid forms of tenapanor and method of preparation of tenapanor

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103819403A (zh) * 2008-12-31 2014-05-28 阿德利克斯公司 用于治疗与体液潴留或盐超负荷有关的病症和胃肠道病症的化合物和方法
WO2018129552A1 (en) * 2017-01-09 2018-07-12 Ardelyx, Inc. Compounds useful for treating gastrointestinal tract disorders

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
SANJEEV KOTHARI ET AL.: "Predicting the Physical Stability of Amorphous Tenapanor Hydrochloride Using Local Molecular Structure Analysis, Relaxation Time Constants, and Molecular Modeling", 《MOL. PHARNACEUTICS》 *
STEN O. NILSSON LILL ET AL.: "Elucidating an Amorphous Form Stabilization Mechanism for Tenapanor Hydrochloride:Crystal Structure Analysis Using X-ray Diffraction, NMR Crystallography, and Molecular Modeling", 《MOL. PHARNACEUTICS》 *

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WO2020181555A1 (zh) 2020-09-17
CN111954669B (zh) 2023-04-07
US20210403450A1 (en) 2021-12-30

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