RU2015109132A - Пролекарственная форма тенофовира и ее фармацевтические применения - Google Patents
Пролекарственная форма тенофовира и ее фармацевтические применения Download PDFInfo
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- RU2015109132A RU2015109132A RU2015109132A RU2015109132A RU2015109132A RU 2015109132 A RU2015109132 A RU 2015109132A RU 2015109132 A RU2015109132 A RU 2015109132A RU 2015109132 A RU2015109132 A RU 2015109132A RU 2015109132 A RU2015109132 A RU 2015109132A
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- compound
- pharmaceutically acceptable
- stereoisomer
- hydrate
- acceptable salt
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- 229960004556 tenofovir Drugs 0.000 title 1
- SGOIRFVFHAKUTI-ZCFIWIBFSA-N tenofovir (anhydrous) Chemical compound N1=CN=C2N(C[C@@H](C)OCP(O)(O)=O)C=NC2=C1N SGOIRFVFHAKUTI-ZCFIWIBFSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 19
- 150000003839 salts Chemical class 0.000 claims abstract 15
- 239000012453 solvate Substances 0.000 claims abstract 13
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 5
- 239000003937 drug carrier Substances 0.000 claims abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 4
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 2
- 239000001257 hydrogen Substances 0.000 claims abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 2
- 239000000203 mixture Substances 0.000 claims abstract 2
- 230000003287 optical effect Effects 0.000 claims abstract 2
- 125000004437 phosphorous atom Chemical group 0.000 claims abstract 2
- 229910052698 phosphorus Inorganic materials 0.000 claims abstract 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract 2
- 239000008215 water for injection Substances 0.000 claims abstract 2
- 241000700721 Hepatitis B virus Species 0.000 claims 2
- 241000725303 Human immunodeficiency virus Species 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 208000002672 hepatitis B Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 claims 1
- 208000037357 HIV infectious disease Diseases 0.000 claims 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 239000008176 lyophilized powder Substances 0.000 claims 1
Classifications
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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
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Abstract
1. Соединение общей формулы (I) или его стереоизомер, фармацевтически приемлемая соль, гидрат или сольват,где Rи Rпредставляют собой C-алкил соответственно, или Rи Rвместе с присоединенным атомом углерода формируют С-циклоалкил,Rпредставляет собой водород, C-алкил, замещенный или незамещенный С-арил или 6-10-членный гетероарил,Ar представляет собой замещенный или незамещенный С-арил, или 6-10-членный гетероарил.2. Соединение общей формулы (I) по п. 1 или его стереоизомер, фармацевтически приемлемая соль, гидрат или сольват, отличающееся тем, что атом фосфора является хиральным и конфигурация представляет собой S или R, или смесь R и S.3. Соединение общей формулы (I) по п. 1 или его стереоизомер, фармацевтически приемлемая соль, гидрат или сольват, отличающееся тем, что стереоизомер содержит таутомер, цис-транс изомер, конформационный изомер, мезомер или энантиомерный или диастереомерный оптический изомер.4. Соединение общей формулы (I) по п. 1 или его стереоизомер, фармацевтически приемлемая соль, гидрат или сольват, отличающееся тем, что соединение выбирают из группы, состоящей из:5. Соединение общей формулы (I) по п. 1 или его стереоизомер, фармацевтически приемлемая соль, гидрат или сольват, отличающееся тем, что соединение выбирают из группы, состоящей из:6. Соединение формулы (Iа1) или его стереоизомер, фармацевтически приемлемая соль, гидрат или сольват,7. Фармацевтическая композиция, содержащая соединение или его стереоизомер, фармацевтически приемлемую соль, гидрат или сольват по любому из пп. 1-6 и фармацевтически приемлемый носитель.8. Фармацевтическая композиция по п. 7, где фармацевтически приемлемый носитель выбирают из группы, состоящей из воды для инъекции, лиофилизированного
Claims (10)
1. Соединение общей формулы (I) или его стереоизомер, фармацевтически приемлемая соль, гидрат или сольват,
где R1 и R2 представляют собой C1-6-алкил соответственно, или R1 и R2 вместе с присоединенным атомом углерода формируют С3-7-циклоалкил,
R3 представляет собой водород, C1-6-алкил, замещенный или незамещенный С6-10-арил или 6-10-членный гетероарил,
Ar представляет собой замещенный или незамещенный С6-10-арил, или 6-10-членный гетероарил.
2. Соединение общей формулы (I) по п. 1 или его стереоизомер, фармацевтически приемлемая соль, гидрат или сольват, отличающееся тем, что атом фосфора является хиральным и конфигурация представляет собой S или R, или смесь R и S.
3. Соединение общей формулы (I) по п. 1 или его стереоизомер, фармацевтически приемлемая соль, гидрат или сольват, отличающееся тем, что стереоизомер содержит таутомер, цис-транс изомер, конформационный изомер, мезомер или энантиомерный или диастереомерный оптический изомер.
7. Фармацевтическая композиция, содержащая соединение или его стереоизомер, фармацевтически приемлемую соль, гидрат или сольват по любому из пп. 1-6 и фармацевтически приемлемый носитель.
8. Фармацевтическая композиция по п. 7, где фармацевтически приемлемый носитель выбирают из группы, состоящей из воды для инъекции, лиофилизированного порошкового эксципиента или эксципиента лекарственного препарата для перорального приема.
9. Применение соединения любому из пп. 1-6 или его стереоизомера, фармацевтически приемлемой соли, гидрата или сольвата для получения лекарственного средства для лечения вирусных инфекций, предпочтительно ВИЧ (вирус иммунодефицита человека)-инфекции, гепатита В или заболеваний, вызванных вирусом гепатита В.
10. Применение фармацевтической композиции по п. 7 или 8 для получения лекарственного средства для лечения вирусных инфекций, предпочтительно ВИЧ-инфекции, гепатита В или заболеваний, вызванных вирусом гепатита В.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
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CN201210315565 | 2012-08-30 | ||
CN201210315565.X | 2012-08-30 | ||
CN201310041647.4 | 2013-02-01 | ||
CN201310041647.4A CN103665043B (zh) | 2012-08-30 | 2013-02-01 | 一种替诺福韦前药及其在医药上的应用 |
PCT/CN2013/079123 WO2014032481A1 (zh) | 2012-08-30 | 2013-07-10 | 一种替诺福韦前药及其在医药上的应用 |
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RU2015109132A true RU2015109132A (ru) | 2016-10-20 |
RU2664534C2 RU2664534C2 (ru) | 2018-08-20 |
RU2664534C9 RU2664534C9 (ru) | 2018-09-28 |
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RU2015109132A RU2664534C9 (ru) | 2012-08-30 | 2013-07-10 | Пролекарственная форма тенофовира и ее фармацевтические применения |
Country Status (12)
Country | Link |
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US (1) | US9908908B2 (ru) |
EP (1) | EP2891658B1 (ru) |
JP (1) | JP6335172B2 (ru) |
KR (1) | KR102057751B1 (ru) |
CN (3) | CN107312039B (ru) |
AU (1) | AU2013307899B2 (ru) |
BR (1) | BR112015003778B1 (ru) |
CA (1) | CA2882201C (ru) |
ES (1) | ES2635564T3 (ru) |
RU (1) | RU2664534C9 (ru) |
TW (1) | TWI593700B (ru) |
WO (1) | WO2014032481A1 (ru) |
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WO2015161785A1 (zh) * | 2014-04-21 | 2015-10-29 | 四川海思科制药有限公司 | 氨基磷酸酯类衍生物制备方法及其中间体和中间体的制备方法 |
WO2015197006A1 (zh) * | 2014-06-25 | 2015-12-30 | 四川海思科制药有限公司 | 一种取代的氨基酸硫酯类化合物、其组合物及应用 |
CN105399771B (zh) * | 2014-07-21 | 2020-11-24 | 江苏豪森药业集团有限公司 | 替诺福韦前药晶型及其制备方法和用途 |
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