CN111065630A - 一种内磺酰胺化合物结晶 - Google Patents

一种内磺酰胺化合物结晶 Download PDF

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Publication number
CN111065630A
CN111065630A CN201880059881.0A CN201880059881A CN111065630A CN 111065630 A CN111065630 A CN 111065630A CN 201880059881 A CN201880059881 A CN 201880059881A CN 111065630 A CN111065630 A CN 111065630A
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formula
compound
crystalline
monohydrate
crystal
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CN201880059881.0A
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CN111065630B (zh
Inventor
张喜全
徐文卫
李明明
孔敏敏
吴叔峰
张爱明
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Centaurus Biopharma Co Ltd
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
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Centaurus Biopharma Co Ltd
Chia Tai Tianqing Pharmaceutical Group Co Ltd
Lianyungang Runzhong Pharmaceutical Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

本申请涉及一种内磺酰胺化合物结晶,具体涉及(S)‑N‑((S)‑1‑(2‑氯苯基)‑2‑((3,3‑二氟环丁基)氨基)‑2‑氧代乙基)‑2‑(4‑氰基吡啶‑2‑基)‑N‑(3‑氟苯基)‑异噻唑烷‑3‑甲酰胺1,1‑二氧化物结晶、其制备方法、其结晶组合物、药物组合物及其用途。本申请式Ⅱ的一水合物结晶的X‑射线粉末衍射光谱用2θ值表示在约14.40°、20.28°、20.94°、22.02°和24.46°处有衍射峰。本申请式Ⅱ的一水合物结晶具有较好的IDH1抑制活性,且该结晶表现出较高的稳定性,在物理性质、安全性及代谢稳定性方面具备优势,有较高的成药价值。

Description

PCT国内申请,说明书已公开。

Claims (25)

  1. PCT国内申请,权利要求书已公开。
CN201880059881.0A 2017-09-22 2018-09-21 一种内磺酰胺化合物结晶 Active CN111065630B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2017108639248 2017-09-22
CN201710863924 2017-09-22
PCT/CN2018/106889 WO2019057142A1 (zh) 2017-09-22 2018-09-21 一种内磺酰胺化合物结晶

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CN111065630A true CN111065630A (zh) 2020-04-24
CN111065630B CN111065630B (zh) 2022-12-30

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US (1) US11254665B2 (zh)
EP (1) EP3686191B1 (zh)
JP (1) JP6951562B2 (zh)
KR (1) KR102707847B1 (zh)
CN (1) CN111065630B (zh)
AU (1) AU2018337153B2 (zh)
CA (1) CA3076405A1 (zh)
FI (1) FI3686191T3 (zh)
HU (1) HUE061207T2 (zh)
PL (1) PL3686191T3 (zh)
WO (1) WO2019057142A1 (zh)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023226964A1 (en) * 2022-05-26 2023-11-30 Danatlas Pharmaceuticals Co., Ltd. Heterocyclic derivatives, compositions and uses thereof
WO2024131727A1 (zh) * 2022-12-19 2024-06-27 正大天晴药业集团股份有限公司 一种内磺酰胺化合物治疗胆道癌的用途
WO2024205311A1 (en) * 2023-03-31 2024-10-03 Avelos Therapeutics Inc. Substituted sultam compound derivatives and their pharmaceutical use

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103097340A (zh) * 2010-07-16 2013-05-08 安吉奥斯医药品有限公司 治疗活性组合物及其使用方法
WO2015010297A1 (en) * 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
CN109071471B (zh) * 2016-03-22 2021-05-07 正大天晴药业集团股份有限公司 内磺酰胺化合物及其使用方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX350432B (es) * 2012-01-19 2017-09-06 Agios Pharmaceuticals Inc Compuestos terapeuticamente activos y sus metodos de empleo.
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
JP6524119B2 (ja) * 2014-03-14 2019-06-05 アジオス ファーマシューティカルズ, インコーポレイテッド 治療活性化合物の医薬組成物

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103097340A (zh) * 2010-07-16 2013-05-08 安吉奥斯医药品有限公司 治疗活性组合物及其使用方法
WO2015010297A1 (en) * 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
CN109071471B (zh) * 2016-03-22 2021-05-07 正大天晴药业集团股份有限公司 内磺酰胺化合物及其使用方法

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CN111065630B (zh) 2022-12-30
AU2018337153B2 (en) 2022-10-20
KR20200057049A (ko) 2020-05-25
JP6951562B2 (ja) 2021-10-20
US20200291012A1 (en) 2020-09-17
HUE061207T2 (hu) 2023-05-28
EP3686191A1 (en) 2020-07-29
WO2019057142A1 (zh) 2019-03-28
JP2020534301A (ja) 2020-11-26
CA3076405A1 (en) 2019-03-28
US11254665B2 (en) 2022-02-22
PL3686191T3 (pl) 2023-03-06
KR102707847B1 (ko) 2024-09-23
EP3686191A4 (en) 2021-01-20
EP3686191B1 (en) 2022-12-14
FI3686191T3 (fi) 2023-01-31
AU2018337153A1 (en) 2020-04-09

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