ME02612B - Tenofovir alafenamid hemifumarat - Google Patents
Tenofovir alafenamid hemifumaratInfo
- Publication number
- ME02612B ME02612B MEP-2016-273A MEP2016273A ME02612B ME 02612 B ME02612 B ME 02612B ME P2016273 A MEP2016273 A ME P2016273A ME 02612 B ME02612 B ME 02612B
- Authority
- ME
- Montenegro
- Prior art keywords
- tenofovir alafenamide
- hemifumarate
- fumaric acid
- hiv
- pharmaceutical composition
- Prior art date
Links
- 229960004556 tenofovir Drugs 0.000 title 1
- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical compound OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 title 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 10
- SVUJNSGGPUCLQZ-FQQAACOVSA-N tenofovir alafenamide fumarate Chemical compound OC(=O)\C=C\C(O)=O.O([P@@](=O)(CO[C@H](C)CN1C2=NC=NC(N)=C2N=C1)N[C@@H](C)C(=O)OC(C)C)C1=CC=CC=C1.O([P@@](=O)(CO[C@H](C)CN1C2=NC=NC(N)=C2N=C1)N[C@@H](C)C(=O)OC(C)C)C1=CC=CC=C1 SVUJNSGGPUCLQZ-FQQAACOVSA-N 0.000 claims 8
- 239000001530 fumaric acid Substances 0.000 claims 5
- LDEKQSIMHVQZJK-CAQYMETFSA-N tenofovir alafenamide Chemical compound O([P@@](=O)(CO[C@H](C)CN1C2=NC=NC(N)=C2N=C1)N[C@@H](C)C(=O)OC(C)C)C1=CC=CC=C1 LDEKQSIMHVQZJK-CAQYMETFSA-N 0.000 claims 5
- 229960004946 tenofovir alafenamide Drugs 0.000 claims 5
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 208000031886 HIV Infections Diseases 0.000 claims 2
- 208000037357 HIV infectious disease Diseases 0.000 claims 2
- 241000725303 Human immunodeficiency virus Species 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000002777 nucleoside Substances 0.000 claims 2
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 230000000069 prophylactic effect Effects 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- 102100035875 C-C chemokine receptor type 5 Human genes 0.000 claims 1
- 101710149870 C-C chemokine receptor type 5 Proteins 0.000 claims 1
- 229940099797 HIV integrase inhibitor Drugs 0.000 claims 1
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 claims 1
- 238000002441 X-ray diffraction Methods 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 239000003084 hiv integrase inhibitor Substances 0.000 claims 1
- 238000013160 medical therapy Methods 0.000 claims 1
- 239000002773 nucleotide Substances 0.000 claims 1
- 125000003729 nucleotide group Chemical group 0.000 claims 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 claims 1
Classifications
-
- 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 Table
- 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
-
- 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 Table
- 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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- 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
- A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
- A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Molecular Biology (AREA)
- Virology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Peptides Or Proteins (AREA)
Claims (15)
1. Tenofovir alafenamid hemifumarat.
2. Tenofovir alafenamid hemifumarat prema patentnom zahtevu 1, u kome je odnos fumarinske kiseline prema tenofovir alafenamidu: 0,5 ± 0,1.
3. Tenofovir alafenamid hemifumarat prema patentnom zahtevu 2, u kome je odnos fumarinske kiseline prema tenofovir alafenamidu: 0,5 ± 0,05.
4. Tenofovir alafenamid hemifumarat prema patentnom zahtevu 2, u kome je odnos fumarinske kiseline prema tenofovir alafenamidu: 0,5 ± 0,01.
5. Tenofovir alafenamid hemifumarat prema patentnom zahtevu 1, u kome uzorak na rendgenskom difraktogramu (XRPD) uključuje 2θ vrednosti 6,9 ± 0,2° i 8,6 ± 0,2°, kada je mereno koristeći zračenje koje ima talasnu dužinu 1,5406 Å.
6. Tenofovir alafenamid hemifumarat prema patentnom zahtevu 5, u kome uzorak na rendgenskom difraktogramu (XRPD) uključuje 2θ vrednosti 6,9 ± 0,2°, 8,6 ± 0,2°, 11,0 ± 0,2°, 15,9 ± 0,2° i 20,2 ± 0,2°, kada je mereno koristeći zračenje koje ima talasnu dužinu 1,5406 Å.
7. Hemifumarat prema patentnom zahtevu 1, koji, na diferencijalnom skenirajućem kalorimetru (DSC), ima početak endotermne reakcije na: 131 ± 2°C.
8. Hemifumarat prema patentnom zahtevu 7, koji, na diferencijalnom skenirajućem kalorimetru (DSC), ima početak endotermne reakcije na 131 ± 1°C.
9. Farmaceutska kompoziija koja uključuje hemifumarat prema bilo kom od patentnih zahteva od 1 do 8 i farmaceutski prihvatljiv ekscipijent.
10. Farmaceutska kompozicija prema patentnom zahtevu 9, koja, dalje, uključuje dodatni terapijski agens; opciono, gde je dodatni terapijski agens izabran iz grupe koja se sastoji od jedinjenja inhibitora proteaze virusa humane imunodeficijencije (HIV), nenukleozidnih inhibitora HIV reverzne transkriptaze, nukleozidnih inhibitora HIV reverzne transkriptaze, nukleotidnih inhibitora HIV reverzne transkriptaze, inhibitora HIV integraze i CCR5 inhibitora.
11. Metoda za pripremu farmaceutske kompozicije, koja uključuje kombinovanje hemifumarata, prema bilo kom od patentnih zahteva od 1 do 8, i farmaceutski prihvatljivog ekscipijenta, da bi se dobila ta farmaceutska kompozicija.
12. Metoda za pripremu tenofovir alafenamid hemifumarata koja uključuje podvrgavanje rastvora, koji sadrži: a) odgovarajući rastvarač; b) fumarinsku kiselinu; c) tenofovir alafenamid; i d) jedno ili više zrna tenofovir alafenamid hemifumarata, uslovima koji obezbeđuju kristalizaciju fumarinske kiseline i tenofovir alafenamida; opciono, gde rastvarač uključuje acetonitril; i/ili rastvor je podvrgnut temperaturama u opsegu od oko 0°C do oko 75°C.
13. Hemifumarat prema bilo kom od patentnih zahteva od 1 do 8, ili kompozicija iz bilo kog od patentnih zahteva od 9 do 10, za upotrebu u medicinskoj terapiji.
14. Hemifumarat prema bilo kom od patentnih zahteva od 1 do 8, ili kompozicija prema bilo kom od patentnih zahteva od 9 do 10, za upotrebu u: profilaktičkom ili terapijskom tretmanu HIV infekcije; opcionio, naznačeno time što je HIV infekcija kod ljudi.
15. Hemifumarat prema bilo kom od patentnih zahteva od 1 do 8, ili kompozicija prema bilo kom od patentnih zahteva od 9 do 10, za upotrebu u: profilaktičkom ili terapijskom tretmanu HBV infekcije; opciono, naznačeno time što je HBV infekcija kod ljudi. 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161524224P | 2011-08-16 | 2011-08-16 | |
| EP12753867.6A EP2744810B2 (en) | 2011-08-16 | 2012-08-15 | Tenofovir alafenamide hemifumarate |
| PCT/US2012/050920 WO2013025788A1 (en) | 2011-08-16 | 2012-08-15 | Tenofovir alafenamide hemifumarate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02612B true ME02612B (me) | 2017-06-20 |
Family
ID=46785793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-273A ME02612B (me) | 2011-08-16 | 2012-08-15 | Tenofovir alafenamid hemifumarat |
Country Status (41)
Families Citing this family (96)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110343135A (zh) | 2011-08-16 | 2019-10-18 | 吉利德科学公司 | 替诺福韦艾拉酚胺(tenofovir alafenamide)半反丁烯二酸盐 |
| TWI613211B (zh) | 2011-10-07 | 2018-02-01 | 基利科學股份有限公司 | 抗病毒核苷酸類似物的製備方法 |
| MD20140091A2 (ro) * | 2012-02-03 | 2015-01-31 | Gilead Sciences, Inc. | Terapie combinată cuprinzând hemifumarat tenofovir alafenamidă şi cobicistat pentru utilizare în tratamentul infecţiilor virale |
| WO2015040640A2 (en) * | 2013-09-20 | 2015-03-26 | Laurus Labs Private Limited | An improved process for the preparation of tenofovir alafenamide or pharmaceutically acceptable salts thereof |
| TWI660965B (zh) * | 2014-01-15 | 2019-06-01 | 美商基利科學股份有限公司 | 泰諾福韋之固體形式 |
| WO2015120057A1 (en) | 2014-02-05 | 2015-08-13 | Gilead Sciences, Inc. | Pharmaceutical combinations against co-infection with hiv and tuberculosis |
| CN105085571A (zh) * | 2014-05-20 | 2015-11-25 | 四川海思科制药有限公司 | 替诺福韦艾拉酚胺复合物及其制备方法和用途 |
| HRP20220651T1 (hr) | 2014-09-15 | 2022-08-19 | The Regents Of The University Of California | Nukleotidni analozi |
| CN105646584B (zh) * | 2014-11-12 | 2018-09-28 | 四川海思科制药有限公司 | 替诺福韦艾拉酚胺富马酸盐晶型及其制备方法和用途 |
| CN105237571B (zh) * | 2014-11-28 | 2018-03-09 | 成都苑东生物制药股份有限公司 | 9‑[(r)‑2‑[[(s)‑[[(s)‑1‑(异丙氧基羰基)乙基]氨基]苯氧基氧膦基]甲氧基]丙基]腺嘌呤的盐 |
| CN104558036A (zh) * | 2014-12-11 | 2015-04-29 | 杭州和泽医药科技有限公司 | 一种替诺福韦艾拉酚胺半反丁烯二酸盐晶型及其制备方法 |
| IL296496B2 (en) | 2014-12-26 | 2024-10-01 | Univ Emory | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| EP3240793A1 (en) * | 2015-01-03 | 2017-11-08 | Mylan Laboratories Ltd. | Processes for the preparation of amorphous tenofovir alafenamide hemifumarate and a premix thereof |
| CN105669751B (zh) * | 2015-03-05 | 2018-09-21 | 洛阳聚慧医药科技有限公司 | 非环核苷酸磷酰胺类化合物及其盐的制备以及在抗病毒方面的应用 |
| GB201509431D0 (en) * | 2015-06-01 | 2015-07-15 | Equigerminal Sa | Antiviral composition |
| CZ2015384A3 (cs) | 2015-06-05 | 2016-12-14 | Zentiva, K.S. | Pevné formy Tenofovir alafenamidu |
| AU2016277859B2 (en) * | 2015-06-17 | 2019-08-01 | Gilead Sciences, Inc. | Co-crystals, salts and solid forms of tenofovir alafenamide |
| EA201792592A1 (ru) | 2015-06-30 | 2018-06-29 | Джилид Сайэнс, Инк. | Фармацевтические препараты, содержащие тенофовир и эмтрицитабин |
| WO2017007701A1 (en) * | 2015-07-07 | 2017-01-12 | Merck Sharp & Dohme Corp. | Antiviral phosphodiamide compounds |
| TWI639598B (zh) | 2015-08-10 | 2018-11-01 | 美商默沙東藥廠 | 抗病毒β－胺基酸酯磷酸二醯胺化合物 |
| WO2017037608A1 (en) * | 2015-08-28 | 2017-03-09 | Laurus Labs Private Limited | Solid forms of tenofovir alafenamide and salts thereof, processes for its preparation and pharmaceutical compositions thereof |
| SI3346995T1 (sl) | 2015-11-09 | 2019-11-29 | Gilead Sciences Inc | Terapevtski sestavek za zdravljenje virusa človeške imunske pomanjkljivosti |
| CN106699812A (zh) * | 2015-11-12 | 2017-05-24 | 江苏豪森药业集团有限公司 | 替诺福韦前药的制备和纯化方法 |
| US10745428B2 (en) | 2015-12-10 | 2020-08-18 | Idenix Pharmaceuticals Llc | Antiviral phosphodiamide prodrugs of tenofovir |
| US10450335B2 (en) | 2015-12-15 | 2019-10-22 | Merck Sharp & Dohme Corp. | Antiviral oxime phosphoramide compounds |
| WO2017134089A1 (en) | 2016-02-02 | 2017-08-10 | Sandoz Ag | Crystalline forms of tenofovir alafenamide monofumarate |
| CN107226826A (zh) * | 2016-03-25 | 2017-10-03 | 江苏奥赛康药业股份有限公司 | 替诺福韦艾拉酚胺富马酸盐化合物及其药物组合物 |
| WO2017203395A1 (en) * | 2016-05-21 | 2017-11-30 | Shilpa Medicare Limited | Crystalline forms of tenofovir alafenamide hemi fumarate |
| CN109476689B (zh) * | 2016-06-05 | 2021-09-03 | 上海诚妙医药科技有限公司 | 富马酸替诺福韦艾拉酚胺盐的新晶型、制备方法及其用途 |
| TW202138365A (zh) | 2016-08-19 | 2021-10-16 | 美商基利科學股份有限公司 | 治療性化合物 |
| EP3503895B1 (en) | 2016-08-25 | 2021-09-15 | Merck Sharp & Dohme Corp. | Antiviral prodrugs of tenofovir |
| CN107793451A (zh) * | 2016-08-30 | 2018-03-13 | 江苏奥赛康药业股份有限公司 | 替诺福韦艾拉酚胺半富马酸盐化合物及其药物组合物 |
| WO2018044822A1 (en) * | 2016-08-31 | 2018-03-08 | Viiv Healthcare Company | Combinations and uses and treatments thereof |
| WO2018051250A1 (en) | 2016-09-14 | 2018-03-22 | Viiv Healthcare Company | Combination comprising tenofovir alafenamide, bictegravir and 3tc |
| WO2018080903A1 (en) | 2016-10-26 | 2018-05-03 | Merck Sharp & Dohme Corp. | Antiviral aryl-amide phosphodiamide compounds |
| CN113072583A (zh) * | 2016-11-28 | 2021-07-06 | 正大天晴药业集团股份有限公司 | 一种替诺福韦艾拉酚胺半富马酸盐的结晶及其制备方法 |
| CN108129514A (zh) * | 2016-12-01 | 2018-06-08 | 北京美倍他药物研究有限公司 | 磷酸/膦酸衍生物的单一异构体及其医药用途 |
| CN108070003A (zh) * | 2016-12-02 | 2018-05-25 | 上海博志研新药物技术有限公司 | 替诺福韦艾拉酚胺半反丁烯二酸盐晶型及制备方法和应用 |
| MA47131A (fr) | 2016-12-22 | 2021-05-12 | Idenix Pharmaceuticals Llc | Composés benzyl-amide phosphodiamide antiviraux |
| KR20190100250A (ko) | 2016-12-22 | 2019-08-28 | 머크 샤프 앤드 돔 코포레이션 | 테노포비르의 항바이러스 지방족 에스테르 전구약물 |
| AU2017378959B2 (en) | 2016-12-23 | 2021-09-09 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Nucleoside phosphate compound and preparation method and use thereof |
| WO2018115046A1 (en) | 2016-12-23 | 2018-06-28 | Sandoz Ag | Crystalline solid forms of tenofovir alafenamide |
| AR110768A1 (es) * | 2017-01-31 | 2019-05-02 | Gilead Sciences Inc | Formas cristalinas de tenofovir alafenamida |
| WO2018153977A1 (en) | 2017-02-24 | 2018-08-30 | Hexal Ag | Stable composition of tenofovir alafenamide |
| RU2659388C1 (ru) | 2017-02-28 | 2018-07-02 | Васильевич Иващенко Александр | Нуклеотиды, включающие N-[(S)-1-циклобутоксикарбонил]фосфорамидатный фрагмент, их аналоги и их применение |
| CN108794530A (zh) * | 2017-04-26 | 2018-11-13 | 上海医药工业研究院 | 一种替诺福韦丙酚酰胺盐晶型及其制备方法和用途 |
| CN107445994A (zh) * | 2017-05-31 | 2017-12-08 | 北京阜康仁生物制药科技有限公司 | 替诺福韦艾拉酚胺半富马酸盐新晶型 |
| RU2662160C9 (ru) | 2017-07-03 | 2018-10-22 | Александрович Иващенко Андрей | Комбинированный лекарственный препарат для терапии вирусных инфекций |
| AR112412A1 (es) | 2017-08-17 | 2019-10-23 | Gilead Sciences Inc | Formas de sal de colina de un inhibidor de la cápside del vih |
| CN107522743A (zh) * | 2017-09-30 | 2017-12-29 | 深圳科兴生物工程有限公司 | 一种半富马酸替诺福韦艾拉酚胺工业化连续生产方法 |
| CN107865874A (zh) * | 2017-10-23 | 2018-04-03 | 上海博悦生物科技有限公司 | 一种替诺福韦艾拉酚胺的药物组合物及其制备方法 |
| US20190151307A1 (en) | 2017-10-24 | 2019-05-23 | Gilead Sciences, Inc. | Methods of treating patients co-infected with a virus and tuberculosis |
| KR102626210B1 (ko) | 2017-12-07 | 2024-01-18 | 에모리 유니버시티 | N4-하이드록시사이티딘 및 유도체 및 이와 관련된 항-바이러스 용도 |
| US20200407382A1 (en) | 2017-12-30 | 2020-12-31 | Cipla Limited | Polymorphic forms of (9-[(r)-2-[[(s)-[[(s)-1-(isopropoxycarbonyl)ethyl]amino]phenoxy phosphinyl]methoxy]propyl] adenine and pharmaceutically acceptable salts thereof |
| CN111836805B (zh) | 2018-02-15 | 2023-07-14 | 吉利德科学公司 | 吡啶衍生物及其用于治疗hiv感染的用途 |
| TWI745652B (zh) | 2018-02-16 | 2021-11-11 | 美商基利科學股份有限公司 | 用於製備有療效化合物之方法及中間物 |
| CN108440596B (zh) * | 2018-03-22 | 2020-07-03 | 科兴生物制药股份有限公司 | 一种半富马酸替诺福韦艾拉酚胺的新型制备工艺 |
| JP2021528363A (ja) | 2018-06-12 | 2021-10-21 | シチュアン ケルン−バイオテック バイオファーマシューティカル カンパニー リミテッド | ホスホンアミドエステル化合物、その塩、その関連する結晶体、その製造方法及びその使用 |
| US11944611B2 (en) | 2018-07-16 | 2024-04-02 | Gilead Sciences, Inc. | Capsid inhibitors for the treatment of HIV |
| EP3823629B1 (en) | 2018-07-19 | 2024-12-25 | Merck Sharp & Dohme LLC | Phosphinic amide prodrugs of tenofovir |
| KR20250161656A (ko) | 2018-09-19 | 2025-11-17 | 길리애드 사이언시즈, 인코포레이티드 | Hiv 예방용 인테그라제 억제제 |
| IL286328B1 (en) | 2019-03-22 | 2026-04-01 | Gilead Sciences Inc | Tricyclic bridging compounds of carbamoylpyridone and their pharmaceutical use |
| KR102054104B1 (ko) * | 2019-04-30 | 2019-12-09 | 유니셀랩 주식회사 | 신규한 테노포비어 알라펜아미드 염 및 이의 제조방법 |
| WO2021011891A1 (en) | 2019-07-18 | 2021-01-21 | Gilead Sciences, Inc. | Long-acting formulations of tenofovir alafenamide |
| WO2021034804A1 (en) * | 2019-08-19 | 2021-02-25 | Gilead Sciences, Inc. | Pharmaceutical formulations of tenofovir alafenamide |
| CN110452268A (zh) * | 2019-08-21 | 2019-11-15 | 天地恒一制药股份有限公司 | 一种丙酚替诺福韦半富马酸单晶的制备方法 |
| EP4643882A3 (en) | 2019-11-26 | 2026-01-14 | Gilead Sciences, Inc. | Capsid inhibitors for the prevention of hiv |
| EP4085062A1 (en) * | 2020-02-20 | 2022-11-09 | Cipla Limited | Novel salts and/or co-crystals of tenofovir alafenamide |
| CA3169348A1 (en) | 2020-03-20 | 2021-09-23 | Gilead Sciences, Inc. | Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same |
| KR20210125298A (ko) | 2020-04-08 | 2021-10-18 | 주식회사 파마코스텍 | 테노포비어 알라펜아미드 헤미타르트레이트의 신규한 제조방법 |
| JP7520162B2 (ja) | 2020-06-25 | 2024-07-22 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｉｖの治療のためのカプシド阻害剤 |
| JP7659628B2 (ja) | 2020-11-11 | 2025-04-09 | ギリアード サイエンシーズ， インコーポレイテッド | ｇｐ１２０ ＣＤ４結合部位指向性抗体による治療に感受性のＨＩＶ患者を特定する方法 |
| US11667656B2 (en) | 2021-01-27 | 2023-06-06 | Apotex Inc. | Crystalline forms of Tenofovir alafenamide |
| KR20220141457A (ko) | 2021-04-13 | 2022-10-20 | 경동제약 주식회사 | 신규 결정형의 테노포비어 알라펜아미드 말레산염 및 이를 포함하는 약제학적 조성물 |
| JP7765637B2 (ja) | 2021-12-03 | 2025-11-06 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｉｖウイルス感染症のための治療化合物 |
| WO2023102523A1 (en) | 2021-12-03 | 2023-06-08 | Gilead Sciences, Inc. | Therapeutic compounds for hiv virus infection |
| PT4440702T (pt) | 2021-12-03 | 2025-08-13 | Gilead Sciences Inc | Compostos terapêuticos para a infecção pelo vírus do hiv |
| TWI856796B (zh) | 2022-04-06 | 2024-09-21 | 美商基利科學股份有限公司 | 橋聯三環胺甲醯基吡啶酮化合物及其用途 |
| EP4547659A1 (en) | 2022-07-01 | 2025-05-07 | Gilead Sciences, Inc. | Therapeutic compounds useful for the prophylactic or therapeutic treatment of an hiv virus infection |
| JP2025526212A (ja) | 2022-07-21 | 2025-08-13 | アンティバ バイオサイエンシズ インコーポレイテッド | Ｈｐｖ感染症及びｈｐｖ誘発性新生物の治療用の組成物及び剤形 |
| WO2024044477A1 (en) | 2022-08-26 | 2024-02-29 | Gilead Sciences, Inc. | Dosing and scheduling regimen for broadly neutralizing antibodies |
| EP4598934A1 (en) | 2022-10-04 | 2025-08-13 | Gilead Sciences, Inc. | 4'-thionucleoside analogues and their pharmaceutical use |
| AR132464A1 (es) | 2023-04-19 | 2025-07-02 | Gilead Sciences Inc | Régimen de dosificación de inhibidor de la cápside |
| EP4719608A1 (en) | 2023-05-31 | 2026-04-08 | Gilead Sciences, Inc. | Quinazolinyl-indazole derivatives as therapeutic compounds for hiv |
| AU2024281548A1 (en) | 2023-05-31 | 2025-11-13 | Gilead Sciences, Inc. | Solid forms of compounds useful in the treatment of hiv |
| KR20260046169A (ko) | 2023-07-28 | 2026-04-06 | 길리애드 사이언시즈, 인코포레이티드 | Hiv의 치료 및 예방을 위한 레나카파비르 주간 투여 레지먼 |
| WO2025042394A1 (en) | 2023-08-23 | 2025-02-27 | Gilead Sciences, Inc. | Dosing regimen of hiv capsid inhibitor |
| AU2024360779A1 (en) | 2023-10-11 | 2026-04-16 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and uses thereof |
| CN122055369A (zh) | 2023-10-11 | 2026-05-15 | 吉利德科学公司 | 桥连三环氨基甲酰基吡啶酮化合物及其用途 |
| TW202515549A (zh) | 2023-10-11 | 2025-04-16 | 美商基利科學股份有限公司 | 橋聯三環胺甲醯基吡啶酮化合物及其用途 |
| US20250230163A1 (en) | 2023-12-22 | 2025-07-17 | Gilead Sciences, Inc. | Solid forms of hiv integrase inhibitors |
| US20250296932A1 (en) | 2024-03-01 | 2025-09-25 | Gilead Sciences, Inc. | Pharmaceutical compositions comprising hiv integrase inhibitors |
| US20250333424A1 (en) | 2024-03-01 | 2025-10-30 | Gilead Sciences, Inc. | Antiviral compounds |
| US20250289822A1 (en) | 2024-03-01 | 2025-09-18 | Gilead Sciences, Inc. | Solid forms of hiv integrase inhibitors |
| US20260007683A1 (en) | 2024-06-14 | 2026-01-08 | Gilead Sciences, Inc. | Pharmaceutical compositions comprising hiv integrase inhibitors |
| WO2026076265A1 (en) | 2024-10-03 | 2026-04-09 | Gilead Sciences, Inc. | Combination therapy comprising bridged tricyclic carbamoylpyridone compounds and p-glycoprotein inhibitors |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5302585A (en) * | 1990-04-20 | 1994-04-12 | Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic | Use of chiral 2-(phosphonomethoxy)propyl guanines as antiviral agents |
| EP0481214B1 (en) | 1990-09-14 | 1998-06-24 | Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic | Prodrugs of phosphonates |
| US5798340A (en) | 1993-09-17 | 1998-08-25 | Gilead Sciences, Inc. | Nucleotide analogs |
| US5468768A (en) | 1994-01-06 | 1995-11-21 | Bristol-Myers Squibb Company | Antimigraine derivatives of indolylcycloalkanylamines |
| WO1998004569A1 (en) | 1996-07-26 | 1998-02-05 | Gilead Sciences, Inc. | Nucleotide analogs |
| PT915894E (pt) | 1996-07-26 | 2003-10-31 | Gilead Sciences Inc | Analogos de nucleotidos |
| US5922695A (en) | 1996-07-26 | 1999-07-13 | Gilead Sciences, Inc. | Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability |
| ATE305009T1 (de) | 1997-07-25 | 2005-10-15 | Gilead Sciences Inc | Nukleotid-analog zusamensetzung und synthese verfahren |
| CN1291994C (zh) * | 2000-07-21 | 2006-12-27 | 吉里德科学公司 | 核苷酸膦酸酯类似物前药及其筛选和制备方法 |
| TWI275392B (en) | 2002-04-08 | 2007-03-11 | Bristol Myers Squibb Co | Low dose liquid entecavir formulations and use |
| US7642277B2 (en) | 2002-12-04 | 2010-01-05 | Boehringer Ingelheim International Gmbh | Non-nucleoside reverse transcriptase inhibitors |
| JP2004288898A (ja) * | 2003-03-24 | 2004-10-14 | Canon Inc | 太陽電池モジュールの製造方法 |
| ECSP045074A (es) | 2004-04-22 | 2004-05-28 | Inhibidores hidroxipirimidinona carboxamida n-sustituida de integrasa de vih | |
| EP2229945A1 (en) | 2004-05-21 | 2010-09-22 | Japan Tobacco, Inc. | Combinations comprising a 4-isoquinolone derivative and anti-HIV agents |
| WO2007013086A1 (en) | 2005-07-26 | 2007-02-01 | Hetero Drugs Limited | Novel polymorphs of tenofovir disoproxil fumarate |
| SI2049506T2 (sl) | 2006-07-07 | 2024-07-31 | Gilead Sciences, Inc. | Modulatorji farmakokinetičnih lastnosti terapevtikov |
| WO2008007392A2 (en) | 2006-07-12 | 2008-01-17 | Matrix Laboratories Limited | Process for the preparation of tenofovir |
| EP4403221A3 (en) | 2007-02-23 | 2024-10-09 | Gilead Sciences, Inc. | Modulators of pharmacokinetic properties of therapeutics |
| WO2008143500A1 (en) | 2007-05-22 | 2008-11-27 | Ultimorphix Technologies B.V. | Tenofovir disoproxil hemi-fumaric acid co-crystal |
| CN103479584A (zh) | 2008-05-02 | 2014-01-01 | 吉里德科学公司 | 固体载体颗粒在改善药物制剂加工性中的应用 |
| CN102307573B (zh) | 2009-02-06 | 2013-09-11 | 吉里德科学公司 | 用于联合治疗的片剂 |
| US7973013B2 (en) | 2009-09-21 | 2011-07-05 | Gilead Sciences, Inc. | 2'-fluoro substituted carba-nucleoside analogs for antiviral treatment |
| TWI556840B (zh) | 2010-11-19 | 2016-11-11 | 吉李德科學股份有限公司 | 治療用組成物 |
| CN110343135A (zh) | 2011-08-16 | 2019-10-18 | 吉利德科学公司 | 替诺福韦艾拉酚胺(tenofovir alafenamide)半反丁烯二酸盐 |
| TWI613211B (zh) | 2011-10-07 | 2018-02-01 | 基利科學股份有限公司 | 抗病毒核苷酸類似物的製備方法 |
| MD20140091A2 (ro) † | 2012-02-03 | 2015-01-31 | Gilead Sciences, Inc. | Terapie combinată cuprinzând hemifumarat tenofovir alafenamidă şi cobicistat pentru utilizare în tratamentul infecţiilor virale |
-
2012
- 2012-08-15 CN CN201910647566.6A patent/CN110343135A/zh active Pending
- 2012-08-15 US US13/586,358 patent/US8754065B2/en active Active
- 2012-08-15 PL PL12753867.6T patent/PL2744810T5/pl unknown
- 2012-08-15 DK DK12753867.6T patent/DK2744810T4/da active
- 2012-08-15 HU HUE12753867A patent/HUE031253T2/en unknown
- 2012-08-15 PE PE2014000206A patent/PE20141328A1/es active IP Right Grant
- 2012-08-15 AU AU2012296622A patent/AU2012296622C1/en active Active
- 2012-08-15 SM SM20160476T patent/SMT201600476T1/it unknown
- 2012-08-15 SI SI201230807T patent/SI2744810T2/sl unknown
- 2012-08-15 EP EP16153076.1A patent/EP3070088A1/en not_active Withdrawn
- 2012-08-15 EP EP12753867.6A patent/EP2744810B2/en active Active
- 2012-08-15 UA UAA201401084A patent/UA115311C2/uk unknown
- 2012-08-15 FI FIEP12753867.6T patent/FI2744810T4/fi active
- 2012-08-15 KR KR1020147003886A patent/KR101612642B1/ko active Active
- 2012-08-15 SG SG2014011548A patent/SG2014011548A/en unknown
- 2012-08-15 PT PT127538676T patent/PT2744810T/pt unknown
- 2012-08-15 CN CN201280039891.0A patent/CN103732594A/zh active Pending
- 2012-08-15 AR ARP120102988A patent/AR087546A1/es not_active Application Discontinuation
- 2012-08-15 WO PCT/US2012/050920 patent/WO2013025788A1/en not_active Ceased
- 2012-08-15 PH PH1/2014/500349A patent/PH12014500349A1/en unknown
- 2012-08-15 EP EP20206486.1A patent/EP3831832A1/en active Pending
- 2012-08-15 LT LTEP12753867.6T patent/LT2744810T/lt unknown
- 2012-08-15 IN IN1012DEN2014 patent/IN2014DN01012A/en unknown
- 2012-08-15 BR BR112014003420-6A patent/BR112014003420B1/pt active IP Right Grant
- 2012-08-15 UY UY0001034262A patent/UY34262A/es active IP Right Grant
- 2012-08-15 TW TW101129542A patent/TWI516499B/zh active
- 2012-08-15 ME MEP-2016-273A patent/ME02612B/me unknown
- 2012-08-15 HR HRP20161696TT patent/HRP20161696T4/hr unknown
- 2012-08-15 RS RS20161018A patent/RS55353B2/sr unknown
- 2012-08-15 MD MDA20140011A patent/MD4508C1/ro active IP Right Grant
- 2012-08-15 AP AP2014007437A patent/AP3639A/xx active
- 2012-08-15 CA CA2845553A patent/CA2845553C/en active Active
- 2012-08-15 MX MX2014001549A patent/MX336627B/es unknown
- 2012-08-15 EA EA201490208A patent/EA027768B1/ru active Protection Beyond IP Right Term
- 2012-08-15 JP JP2014526164A patent/JP5651275B2/ja active Active
- 2012-08-15 ES ES12753867T patent/ES2608871T5/es active Active
-
2014
- 2014-01-24 ZA ZA2014/00582A patent/ZA201400582B/en unknown
- 2014-02-12 CR CR20140072A patent/CR20140072A/es unknown
- 2014-02-12 MA MA36754A patent/MA35350B1/fr unknown
- 2014-02-12 CO CO14029801A patent/CO6880063A2/es unknown
- 2014-02-13 IL IL230949A patent/IL230949A/en active IP Right Grant
- 2014-02-13 CL CL2014000370A patent/CL2014000370A1/es unknown
- 2014-02-13 EC ECSP14013206 patent/ECSP14013206A/es unknown
- 2014-03-05 US US14/197,873 patent/US9296769B2/en active Active
- 2014-11-14 JP JP2014231819A patent/JP5956537B2/ja active Active
-
2015
- 2015-08-18 IL IL240649A patent/IL240649A0/en unknown
-
2016
- 2016-06-16 JP JP2016120153A patent/JP6280162B2/ja active Active
- 2016-12-22 CY CY20161101331T patent/CY1118385T1/el unknown
- 2016-12-28 SM SM201600476T patent/SMT201600476B/it unknown
-
2018
- 2018-01-18 JP JP2018006107A patent/JP2018065870A/ja not_active Withdrawn
-
2019
- 2019-11-21 JP JP2019210196A patent/JP2020040972A/ja active Pending
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20161696T1 (hr) | Tenofovir alafenamid hemifumarat | |
| EP3752495B1 (en) | Pyridine derivatives and their use for treating hiv infection | |
| JP6804790B1 (ja) | Ｎ４−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 | |
| ES2705709T3 (es) | Compuestos de isoquinolina para el tratamiento del VIH | |
| AU2015371198B2 (en) | Quinazoline derivatives used to treat HIV | |
| JP6606692B2 (ja) | （２Ｒ，５Ｓ，１３ＡＲ）−８−ヒドロキシ−７，９−ジオキソ−Ｎ−（２，４，６−トリフルオロベンジル）−２，３，４，５，７，９，１３，１３Ａ−オクタヒドロ−２，５−メタノピリド［１’，２’：４，５］ピラジノ［２，１−ｂ］［１，３］オキサゼピン−１０−カルボキサミドの結晶形 | |
| JP2015038149A5 (me) | ||
| KR101985122B1 (ko) | Hiv의 치료를 위한 융합된 피리미딘 화합물 | |
| JP2018115191A5 (me) | ||
| ES2351958T3 (es) | 5-cloro-3-(4-metanosulfonilfenil)-6'-metil-[2,3'] bipiridinil en forma cristalina pura y procedimiento de síntesis. | |
| EP3986561A1 (en) | Pyrido[2,3-d]pyrimidine derivatives as inhibitors of human immunodeficiency virus replication | |
| CA2950307A1 (en) | Sodium (2r,5s,13ar)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate | |
| EP3853228A1 (en) | Inhibitors of human immunodeficiency virus replication | |
| JP2014510139A (ja) | 固体形態のｈｉｖ阻害剤 | |
| EP4135702A1 (en) | Inhibitors of human immunodeficiency virus replication | |
| CA3204255A1 (en) | Combination therapy for hiv with adenosine derivative and capsid inhibitors | |
| EP3962603A1 (en) | Inhibitors of human immunodeficiency virus replication | |
| IL296182A (en) | Inhibitors of human immunodeficiency virus replication | |
| CA2952526A1 (en) | Bet-protein inhibiting 3,4-dihydropyrido[2,3-b]pyrazinones with meta-substituted aromatic amino- or ether groups | |
| JP2011528030A5 (me) | ||
| TW201127826A (en) | Solid dispersion comprising an anti-HIV agent | |
| HK40076424A (en) | Co-crystals and salts of 8-chloro-n-(4-(trifluoromethoxy)phenyl)quinolin-2-amine | |
| CN104803981A (zh) | 一种哌啶-4-胺基二芳基嘧啶衍生物及其制备方法和用途 | |
| OA18583A (en) | Quinazoline derivatives used to treat HIV | |
| HK40043125A (en) | Pyridine derivatives and their use for treating hiv infection |