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CN111194309A - 吲哚胺-2,3-双加氧酶抑制剂盐及其制备方法 - Google Patents

吲哚胺-2,3-双加氧酶抑制剂盐及其制备方法 Download PDF

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CN111194309A
CN111194309A CN201880061367.0A CN201880061367A CN111194309A CN 111194309 A CN111194309 A CN 111194309A CN 201880061367 A CN201880061367 A CN 201880061367A CN 111194309 A CN111194309 A CN 111194309A
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compound
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formula
acid
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王召印
胡新波
郭巍
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Shanghai Institute of Organic Chemistry of CAS
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Shanghai Institute of Organic Chemistry of CAS
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/08—1,2,5-Oxadiazoles; Hydrogenated 1,2,5-oxadiazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4245—Oxadiazoles
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明涉及吲哚胺‑2,3‑双加氧酶抑制剂盐及其制备方法。具体地，本发明涉及式I化合物的盐及其多种无定形物和多晶型物，其中各基团的定义如说明书中所述。所述盐结构稳定，具有良好的光稳定性、热稳定性、非吸湿性和药代动力学性质，溶解性能良好，纯度和生物利用度显著提高，特别适合用于开发和生产高质量的IDO酶抑制剂。

Description

PCT国内申请，说明书已公开。

Claims (10)

  1. PCT国内申请，权利要求书已公开。
CN201880061367.0A 2017-10-18 2018-10-17 吲哚胺-2,3-双加氧酶抑制剂盐及其制备方法 Pending CN111194309A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201710971186.9A CN109678813A (zh) 2017-10-18 2017-10-18 吲哚胺-2,3-双加氧酶抑制剂盐及其制备方法
CN2017109711869 2017-10-18
PCT/CN2018/110682 WO2019076324A1 (zh) 2017-10-18 2018-10-17 吲哚胺-2,3-双加氧酶抑制剂盐及其制备方法

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CN111194309A true CN111194309A (zh) 2020-05-22

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CN201880061367.0A Pending CN111194309A (zh) 2017-10-18 2018-10-17 吲哚胺-2,3-双加氧酶抑制剂盐及其制备方法

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WO (1) WO2019076324A1 (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
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CN114539111A (zh) * 2020-11-19 2022-05-27 深圳信立泰药业股份有限公司 奥当卡替的盐及其制备方法和医药用途

Citations (10)

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WO2008036652A2 (en) * 2006-09-19 2008-03-27 Incyte Corporation Amidines as modulators of indoleamine 2,3-dioxygenase
CN103130735A (zh) * 2005-05-10 2013-06-05 因塞特公司 吲哚胺2,3-双加氧酶调节剂及其用法
CN105481789A (zh) * 2014-09-15 2016-04-13 中国科学院上海有机化学研究所 一种吲哚胺-2,3-双加氧酶抑制剂及其制备方法
CN105646389A (zh) * 2016-01-28 2016-06-08 中国科学院上海有机化学研究所 一种作为吲哚胺-2,3-双加氧酶抑制剂的氨基磺酸脂及其制备方法和用途
WO2017101884A1 (zh) * 2015-12-15 2017-06-22 江苏豪森药业集团有限公司 吲哚胺2,3-双加氧酶抑制剂及其制备方法与应用
WO2017143874A1 (zh) * 2016-02-25 2017-08-31 深圳市塔吉瑞生物医药有限公司 一种取代的恶二唑类化合物及包含该化合物的组合物及其用途
CN107176933A (zh) * 2016-03-09 2017-09-19 中国科学院上海有机化学研究所 一种含氮烷基化和芳基化亚砜亚胺的吲哚胺-2,3-双加氧酶抑制剂
CN107304191A (zh) * 2016-04-20 2017-10-31 上海翰森生物医药科技有限公司 吲哚胺2,3‑双加氧酶抑制剂及其制备方法与应用
WO2018072697A1 (zh) * 2016-10-17 2018-04-26 上海医药集团股份有限公司 含噁二唑环化合物、制备方法、中间体、组合物及应用
WO2018095432A1 (en) * 2016-11-28 2018-05-31 Shanghai Fochon Pharmaceutical Co., Ltd. Sulfoximine, sulfonimidamide, sulfondiimine and diimidosulfonamide compounds as inhibitors of indoleamine 2, 3-dioxygenase

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CN103130735A (zh) * 2005-05-10 2013-06-05 因塞特公司 吲哚胺2,3-双加氧酶调节剂及其用法
WO2008036652A2 (en) * 2006-09-19 2008-03-27 Incyte Corporation Amidines as modulators of indoleamine 2,3-dioxygenase
CN105481789A (zh) * 2014-09-15 2016-04-13 中国科学院上海有机化学研究所 一种吲哚胺-2,3-双加氧酶抑制剂及其制备方法
WO2017101884A1 (zh) * 2015-12-15 2017-06-22 江苏豪森药业集团有限公司 吲哚胺2,3-双加氧酶抑制剂及其制备方法与应用
CN105646389A (zh) * 2016-01-28 2016-06-08 中国科学院上海有机化学研究所 一种作为吲哚胺-2,3-双加氧酶抑制剂的氨基磺酸脂及其制备方法和用途
WO2017143874A1 (zh) * 2016-02-25 2017-08-31 深圳市塔吉瑞生物医药有限公司 一种取代的恶二唑类化合物及包含该化合物的组合物及其用途
CN107176933A (zh) * 2016-03-09 2017-09-19 中国科学院上海有机化学研究所 一种含氮烷基化和芳基化亚砜亚胺的吲哚胺-2,3-双加氧酶抑制剂
CN107304191A (zh) * 2016-04-20 2017-10-31 上海翰森生物医药科技有限公司 吲哚胺2,3‑双加氧酶抑制剂及其制备方法与应用
WO2018072697A1 (zh) * 2016-10-17 2018-04-26 上海医药集团股份有限公司 含噁二唑环化合物、制备方法、中间体、组合物及应用
WO2018095432A1 (en) * 2016-11-28 2018-05-31 Shanghai Fochon Pharmaceutical Co., Ltd. Sulfoximine, sulfonimidamide, sulfondiimine and diimidosulfonamide compounds as inhibitors of indoleamine 2, 3-dioxygenase

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* Cited by examiner, † Cited by third party
Title
HOLLY K. KOBLISH ET AL.: "Hydroxyamidine Inhibitors of Indoleamine-2,3-dioxygenase Potently Suppress Systemic Tryptophan Catabolism and the Growth of IDO-Expressing Tumors", 《MOLECULAR CANCER THERAPEUTICS》 *
刘燕玲 等: "色氨酸2,3-双加氧酶2的生物学特征及其在免疫调节与肿瘤治疗中的作用", 《细胞与分子免疫学杂志》 *
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