CN111295372A - 硝羟喹啉前药及其用途 - Google Patents
硝羟喹啉前药及其用途 Download PDFInfo
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/60—Quinoline or hydrogenated quinoline ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic 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
- C07D215/16—Heterocyclic 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
- C07D215/20—Oxygen atoms
- C07D215/24—Oxygen atoms attached in position 8
- C07D215/26—Alcohols; Ethers thereof
- C07D215/28—Alcohols; Ethers thereof with halogen atoms or nitro radicals in positions 5, 6 or 7
-
- 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
-
- 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
- A61K31/535—Heterocyclic 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic 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
- C07D215/16—Heterocyclic 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
- C07D215/20—Oxygen atoms
- C07D215/24—Oxygen atoms attached in position 8
- C07D215/26—Alcohols; Ethers thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic 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
- C07D215/16—Heterocyclic 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
- C07D215/20—Oxygen atoms
- C07D215/24—Oxygen atoms attached in position 8
- C07D215/26—Alcohols; Ethers thereof
- C07D215/32—Esters
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic 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
- C07D215/16—Heterocyclic 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
- C07D215/20—Oxygen atoms
- C07D215/24—Oxygen atoms attached in position 8
- C07D215/26—Alcohols; Ethers thereof
- C07D215/32—Esters
- C07D215/34—Carbamates
-
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic 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
- C07D413/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/58—Pyridine 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)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
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 |
Publications (2)
Publication Number | Publication Date |
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CN111295372A true CN111295372A (zh) | 2020-06-16 |
CN111295372B CN111295372B (zh) | 2021-03-09 |
Family
ID=69953367
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CN201980004913.1A Active CN111295372B (zh) | 2018-09-29 | 2019-09-27 | 硝羟喹啉前药及其用途 |
Country Status (11)
Country | Link |
---|---|
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)
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)
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 |
Citations (17)
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2019
- 2019-09-27 EP EP19864911.3A patent/EP3858814A4/en active Pending
- 2019-09-27 KR KR1020217012529A patent/KR20210070320A/ko active Search and Examination
- 2019-09-27 BR BR112021005941-5A patent/BR112021005941A2/pt unknown
- 2019-09-27 CA CA3113463A patent/CA3113463A1/en active Pending
- 2019-09-27 WO PCT/CN2019/108419 patent/WO2020063824A1/zh active Application Filing
- 2019-09-27 AU AU2019351494A patent/AU2019351494A1/en active Pending
- 2019-09-27 SG SG11202103134TA patent/SG11202103134TA/en unknown
- 2019-09-27 US US17/280,999 patent/US20210363165A1/en active Pending
- 2019-09-27 MX MX2021003724A patent/MX2021003724A/es unknown
- 2019-09-27 JP JP2021542249A patent/JP2022502510A/ja active Pending
- 2019-09-27 CN CN201980004913.1A patent/CN111295372B/zh active Active
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Cited By (6)
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 |
Also Published As
Publication number | Publication date |
---|---|
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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