CN111295372A - 硝羟喹啉前药及其用途 - Google Patents

硝羟喹啉前药及其用途 Download PDF

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CN111295372A
CN111295372A CN201980004913.1A CN201980004913A CN111295372A CN 111295372 A CN111295372 A CN 111295372A CN 201980004913 A CN201980004913 A CN 201980004913A CN 111295372 A CN111295372 A CN 111295372A
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alkyl
heterocyclyl
aryl
heteroaryl
cycloalkyl
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CN111295372B (zh
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邓一军
吴亮
潘柯
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JIANGSU YAHONG MEDICINE SCIENCE & TECHNOLOGY CO LTD
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/60Quinoline or hydrogenated quinoline ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20Oxygen atoms
    • C07D215/24Oxygen atoms attached in position 8
    • C07D215/26Alcohols; Ethers thereof
    • C07D215/28Alcohols; Ethers thereof with halogen atoms or nitro radicals in positions 5, 6 or 7
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20Oxygen atoms
    • C07D215/24Oxygen atoms attached in position 8
    • C07D215/26Alcohols; Ethers thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20Oxygen atoms
    • C07D215/24Oxygen atoms attached in position 8
    • C07D215/26Alcohols; Ethers thereof
    • C07D215/32Esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20Oxygen atoms
    • C07D215/24Oxygen atoms attached in position 8
    • C07D215/26Alcohols; Ethers thereof
    • C07D215/32Esters
    • C07D215/34Carbamates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/58Pyridine rings

Abstract

提供硝羟喹啉前药及其用途,具体地,提供式(I)化合物或其药学上可接受的盐、其制备方法、包含其的组合物、及其在制备用于抗感染和抗肿瘤药物中的用途,式(I)中各个基团的定义如说明书中所述。式(I)化合物相对于硝羟喹啉有更好的水溶性、血药浓度或半衰期等药代动力学参数。式(I)化合物可减少给药次数,同时具有在尿路领域以外的其他领域中应用的可能性。

Description

PCT国内申请,说明书已公开。

Claims (20)

  1. PCT国内申请,权利要求书已公开。
CN201980004913.1A 2018-09-29 2019-09-27 硝羟喹啉前药及其用途 Active CN111295372B (zh)

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CN2018111483140 2018-09-29
CN201811148314 2018-09-29
PCT/CN2019/108419 WO2020063824A1 (zh) 2018-09-29 2019-09-27 硝羟喹啉前药及其用途

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CN111295372A true CN111295372A (zh) 2020-06-16
CN111295372B CN111295372B (zh) 2021-03-09

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US (1) US20210363165A1 (zh)
EP (1) EP3858814A4 (zh)
JP (1) JP2022502510A (zh)
KR (1) KR20210070320A (zh)
CN (1) CN111295372B (zh)
AU (1) AU2019351494A1 (zh)
BR (1) BR112021005941A2 (zh)
CA (1) CA3113463A1 (zh)
MX (1) MX2021003724A (zh)
SG (1) SG11202103134TA (zh)
WO (1) WO2020063824A1 (zh)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111646936A (zh) * 2020-06-22 2020-09-11 江苏亚虹医药科技有限公司 芳香醚类化合物的制备方法
CN111773193A (zh) * 2020-07-03 2020-10-16 江苏亚虹医药科技有限公司 含硝羟喹啉赖氨酸盐的药物组合物及其制备方法和用途
CN115427397A (zh) * 2020-03-30 2022-12-02 江苏亚虹医药科技股份有限公司 硝羟喹啉前药的晶型、含其的药物组合物及其制备方法和应用

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112402388A (zh) * 2019-08-05 2021-02-26 江苏亚虹医药科技股份有限公司 一种用于治疗膀胱癌的口服固体制剂及其制备方法
CN111514142B (zh) * 2020-05-29 2021-04-06 江苏亚虹医药科技股份有限公司 含硝羟喹啉前药的药物组合物及其制备方法和应用
CN112745334B (zh) * 2021-02-07 2022-03-25 厦门一先药业有限公司 一种巴洛沙韦及其衍生物的前药、其制备方法和用途
WO2022253159A1 (zh) 2021-05-31 2022-12-08 江苏亚虹医药科技股份有限公司 5-硝基-8-羟基喹啉的应用

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Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115427397A (zh) * 2020-03-30 2022-12-02 江苏亚虹医药科技股份有限公司 硝羟喹啉前药的晶型、含其的药物组合物及其制备方法和应用
CN115427397B (zh) * 2020-03-30 2024-01-26 江苏亚虹医药科技股份有限公司 硝羟喹啉前药的晶型、含其的药物组合物及其制备方法和应用
CN111646936A (zh) * 2020-06-22 2020-09-11 江苏亚虹医药科技有限公司 芳香醚类化合物的制备方法
WO2021258979A1 (zh) * 2020-06-22 2021-12-30 江苏亚虹医药科技股份有限公司 芳香醚类化合物的制备方法
CN115697970A (zh) * 2020-06-22 2023-02-03 江苏亚虹医药科技股份有限公司 芳香醚类化合物的制备方法
CN111773193A (zh) * 2020-07-03 2020-10-16 江苏亚虹医药科技有限公司 含硝羟喹啉赖氨酸盐的药物组合物及其制备方法和用途

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US20210363165A1 (en) 2021-11-25
EP3858814A1 (en) 2021-08-04
WO2020063824A1 (zh) 2020-04-02
JP2022502510A (ja) 2022-01-11
BR112021005941A2 (pt) 2021-06-29
AU2019351494A1 (en) 2021-05-20
CA3113463A1 (en) 2020-04-02
SG11202103134TA (en) 2021-04-29
KR20210070320A (ko) 2021-06-14
MX2021003724A (es) 2021-05-14
CN111295372B (zh) 2021-03-09
EP3858814A4 (en) 2022-10-05

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