HRP20161696T1 - Tenofovir alafenamid hemifumarat - Google Patents
Tenofovir alafenamid hemifumarat Download PDFInfo
- Publication number
- HRP20161696T1 HRP20161696T1 HRP20161696TT HRP20161696T HRP20161696T1 HR P20161696 T1 HRP20161696 T1 HR P20161696T1 HR P20161696T T HRP20161696T T HR P20161696TT HR P20161696 T HRP20161696 T HR P20161696T HR P20161696 T1 HRP20161696 T1 HR P20161696T1
- Authority
- HR
- Croatia
- Prior art keywords
- tenofovir alafenamide
- hemifumarate
- fumaric acid
- hiv
- inhibitors
- Prior art date
Links
- 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 title claims 9
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 10
- 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
- 239000003112 inhibitor Substances 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
- 238000002441 X-ray diffraction Methods 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
- 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
- 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
- 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
- 239000003419 rna directed dna polymerase inhibitor 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 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)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Virology (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Biochemistry (AREA)
- Tropical Medicine & Parasitology (AREA)
- Biotechnology (AREA)
- Engineering & Computer Science (AREA)
- AIDS & HIV (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)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
Claims (15)
1. Tenofovir alafenamid hemifumarat.
2. Tenofovir alafenamid hemifumarat prema patentnom zahtjevu 1, u kome je odnos fumarinske kiseline prema tenofovir alafenamidu: 0,5 ± 0,1.
3. Tenofovir alafenamid hemifumarat prema patentnom zahtjevu 2, u kome je odnos fumarinske kiseline prema tenofovir alafenamidu: 0,5 ± 0,05.
4. Tenofovir alafenamid hemifumarat prema patentnom zahtjevu 2, u kome je odnos fumarinske kiseline prema tenofovir alafenamidu: 0,5 ± 0,01.
5. Tenofovir alafenamid hemifumarat prema patentnom zahtjevu 1, u kome uzorak na rendgenskom difraktogramu (XRPD) uključuje 2θ vrijednosti 6,9 ± 0,2° i 8,6 ± 0,2°, kada je mjereno koristeći zračenje koje ima valnu dužinu 1,5406 Å.
6. Tenofovir alafenamid hemifumarat prema patentnom zahtjevu 5, u kome uzorak na rendgenskom difraktogramu (XRPD) uključuje 2θ vrijednosti 6,9 ± 0,2°, 8,6 ± 0,2°, 11,0 ± 0,2°, 15,9 ± 0,2° i 20,2 ± 0,2°, kada je mjereno koristeći zračenje koje ima valnu dužinu 1,5406 Å.
7. Hemifumarat prema patentnom zahtjevu 1, koji, na diferencijalnom skenirajućem kalorimetru (DSC), ima početak endotermne reakcije na: 131 ± 2°C.
8. Hemifumarat prema patentnom zahtjevu 7, koji, na diferencijalnom skenirajućem kalorimetru (DSC), ima početak endotermne reakcije na 131 ± 1°C.
9. Farmaceutski sastav koji sadrži hemifumarat prema bilo kojem od patentnih zahtjeva od 1 do 8 i farmaceutski prihvatljiv ekscipijens.
10. Farmaceutski sastav prema patentnom zahtjevu 9, koji nadalje, sadrži dodatni terapijski agens; opcionalno, gdje je dodatni terapijski agens izabran iz grupe koja se sastoji od spojeva 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 farmaceutskog sastava, koja uključuje kombiniranje hemifumarata, prema bilo kojem od patentnih zahtjeva od 1 do 8, i farmaceutski prihvatljivog ekscipijensa, da bi se dobio farmaceutski sastav.
12. Metoda za pripremu tenofovir alafenamid hemifumarata koja uključuje podvrgavanje rastvora, koji sadrži: a) odgovarajuće otapalo; b) fumarinsku kiselinu; c) tenofovir alafenamid; i d) jedno ili više zrna tenofovir alafenamid hemifumarata, uvjetima koji uzrokuju kristalizaciju fumarinske kiseline i tenofovir alafenamida; opcionalno, gdje otapalo sadrži acetonitril; i/ili otopina je podvrgnuta temperaturama u rasponu od oko 0°C do oko 75°C.
13. Hemifumarat prema bilo kojem od patentnih zahtjeva od 1 do 8, ili sastav iz bilo kojeg od patentnih zahtjeva od 9 do 10, za upotrebu u medicinskoj terapiji.
14. Hemifumarat prema bilo kojem od patentnih zahtjeva od 1 do 8, ili sastav prema bilo kojem od patentnih zahtjeva od 9 do 10, za upotrebu u: profilaktičkom ili terapijskom tretmanu HIV infekcije; opcionalno, naznačeno time što je HIV infekcija kod ljudi.
15. Hemifumarat prema bilo kojem od patentnih zahtjeva od 1 do 8, ili sastav prema bilo kojem od patentnih zahtjeva od 9 do 10, za upotrebu u: profilaktičkom ili terapijskom tretmanu HBV infekcije; opcionalno, naznačeno time što je HBV infekcija kod ljudi.
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 (2)
| Publication Number | Publication Date |
|---|---|
| HRP20161696T1 true HRP20161696T1 (hr) | 2017-02-24 |
| HRP20161696T4 HRP20161696T4 (hr) | 2023-10-13 |
Family
ID=46785793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20161696TT HRP20161696T4 (hr) | 2011-08-16 | 2012-08-15 | Tenofovir alafenamid hemifumarat |
Country Status (41)
| Country | Link |
|---|---|
| US (2) | US8754065B2 (hr) |
| EP (3) | EP2744810B2 (hr) |
| JP (5) | JP5651275B2 (hr) |
| KR (1) | KR101612642B1 (hr) |
| CN (2) | CN110343135A (hr) |
| AP (1) | AP3639A (hr) |
| AR (1) | AR087546A1 (hr) |
| AU (1) | AU2012296622C1 (hr) |
| BR (1) | BR112014003420B1 (hr) |
| CA (1) | CA2845553C (hr) |
| CL (1) | CL2014000370A1 (hr) |
| CO (1) | CO6880063A2 (hr) |
| CR (1) | CR20140072A (hr) |
| CY (1) | CY1118385T1 (hr) |
| DK (1) | DK2744810T4 (hr) |
| EA (1) | EA027768B1 (hr) |
| EC (1) | ECSP14013206A (hr) |
| ES (1) | ES2608871T5 (hr) |
| FI (1) | FI2744810T4 (hr) |
| HK (1) | HK1199026A1 (hr) |
| HR (1) | HRP20161696T4 (hr) |
| HU (1) | HUE031253T2 (hr) |
| IL (2) | IL230949A (hr) |
| IN (1) | IN2014DN01012A (hr) |
| LT (1) | LT2744810T (hr) |
| MA (1) | MA35350B1 (hr) |
| MD (1) | MD4508C1 (hr) |
| ME (1) | ME02612B (hr) |
| MX (1) | MX336627B (hr) |
| PE (1) | PE20141328A1 (hr) |
| PL (1) | PL2744810T5 (hr) |
| PT (1) | PT2744810T (hr) |
| RS (1) | RS55353B2 (hr) |
| SG (1) | SG2014011548A (hr) |
| SI (1) | SI2744810T2 (hr) |
| SM (1) | SMT201600476B (hr) |
| TW (1) | TWI516499B (hr) |
| UA (1) | UA115311C2 (hr) |
| UY (1) | UY34262A (hr) |
| WO (1) | WO2013025788A1 (hr) |
| ZA (1) | ZA201400582B (hr) |
Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS55353B2 (sr) | 2011-08-16 | 2023-11-30 | Gilead Sciences Inc | Tenofovir alafenamid hemifumarat |
| ES2661705T3 (es) | 2011-10-07 | 2018-04-03 | Gilead Sciences, Inc. | Métodos para la preparación de análogos de nucleótidos antivirales |
| EA026138B1 (ru) * | 2012-02-03 | 2017-03-31 | Джилид Сайэнс, Инк. | Комбинированная терапия, включающая тенофовир алафенамида гемифумарат и кобицистат, для применения для лечения вирусных инфекций |
| 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 |
| US9463194B2 (en) | 2014-02-05 | 2016-10-11 | Gilead Sciences, Inc. | Methods of treating patients co-infected 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 |
| 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 |
| KR20230130175A (ko) | 2014-12-26 | 2023-09-11 | 에모리 유니버시티 | Ｎ4-하이드록시시티딘, 이와 관련된 유도체 및 이의 항 바이러스적 용도 |
| AU2015373104B2 (en) * | 2015-01-03 | 2020-07-09 | Mylan Laboratories Limited | 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 |
| MA46677A (fr) * | 2015-06-17 | 2019-09-11 | Gilead Sciences Inc | Co-cristaux, sels et formes solides de ténofovir alafénamide |
| SI3316868T1 (sl) | 2015-06-30 | 2020-04-30 | Gilead Sciences, Inc. | Farmacevtske formulacije, ki vsebujejo tenofovir in emtricitabin |
| WO2017007701A1 (en) * | 2015-07-07 | 2017-01-12 | Merck Sharp & Dohme Corp. | Antiviral phosphodiamide compounds |
| CA2994720C (en) | 2015-08-10 | 2020-11-03 | Merck Sharp & Dohme Corp. | Antiviral beta-amino acid ester phosphodiamide compounds |
| 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 |
| PE20181207A1 (es) | 2015-11-09 | 2018-07-23 | Gilead Sciences Inc | Composiciones terapeuticas para el tratamiento del virus de inmunodeficiencia humana |
| 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 |
| WO2017106069A1 (en) * | 2015-12-15 | 2017-06-22 | Merck Sharp & Dohme Corp. | Antiviral oxime phosphoramide compounds |
| ES2806604T3 (es) | 2016-02-02 | 2021-02-18 | Sandoz Ag | Formas cristalinas de monofumarato de tenofovir alafenamida |
| 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 |
| WO2017211325A1 (zh) * | 2016-06-05 | 2017-12-14 | 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 |
| HUE045137T2 (hu) | 2016-08-19 | 2019-12-30 | Gilead Sciences Inc | HIV vírusfertõzés megelõzõ vagy terápiás kezelésére alkalmas terápiás vegyületek |
| 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 |
| CN108117570A (zh) * | 2016-11-28 | 2018-06-05 | 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 |
| CA3046029A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Antiviral benzyl-amine phosphodiamide compounds |
| KR20190100250A (ko) | 2016-12-22 | 2019-08-28 | 머크 샤프 앤드 돔 코포레이션 | 테노포비르의 항바이러스 지방족 에스테르 전구약물 |
| EP3560943A4 (en) | 2016-12-23 | 2020-09-02 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | NUCLEOSIDIC PHOSPHATE COMPOUND, PROCESS FOR PREPARATION AND USE |
| WO2018115046A1 (en) | 2016-12-23 | 2018-06-28 | Sandoz Ag | Crystalline solid forms of tenofovir alafenamide |
| TWI784370B (zh) | 2017-01-31 | 2022-11-21 | 美商基利科學股份有限公司 | 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型 |
| 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 |
| EP3700573A1 (en) | 2017-10-24 | 2020-09-02 | Gilead Sciences, Inc. | Methods of treating patients co-infected with a virus and tuberculosis |
| BR122022008466B1 (pt) | 2017-12-07 | 2023-12-05 | Emory University | Uso de um composto |
| WO2019130354A1 (en) * | 2017-12-30 | 2019-07-04 | Cipla Limited | Polymorphic forms of (9-[(r)-2-[[(s)-[[(s)-1- (isopropoxycarbonyl)ethyl]amino]phenoxy phosphinyl]methoxy]propyl] adenine and pharmaceutically acceptable salts thereof |
| US10836746B2 (en) | 2018-02-15 | 2020-11-17 | Gilead Sciences, Inc. | Therapeutic compounds |
| TWI823164B (zh) | 2018-02-16 | 2023-11-21 | 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 |
| AU2019307500B2 (en) | 2018-07-16 | 2022-09-29 | Gilead Sciences, Inc. | Capsid inhibitors for the treatment of HIV |
| EP3823629A4 (en) | 2018-07-19 | 2022-05-04 | Merck Sharp & Dohme Corp. | PHOSPHINAMIDE PRODRUGS OF TENOFOVIR |
| AU2019344929B2 (en) | 2018-09-19 | 2023-03-30 | Gilead Sciences, Inc. | Integrase inhibitors for the prevention of HIV |
| KR102054104B1 (ko) * | 2019-04-30 | 2019-12-09 | 유니셀랩 주식회사 | 신규한 테노포비어 알라펜아미드 염 및 이의 제조방법 |
| US20220257619A1 (en) | 2019-07-18 | 2022-08-18 | Gilead Sciences, Inc. | Long-acting 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 |
| JP2023502530A (ja) | 2019-11-26 | 2023-01-24 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｉｖ予防のためのカプシド阻害剤 |
| WO2021165995A1 (en) * | 2020-02-20 | 2021-08-26 | Cipla Limited | Novel salts and/or co-crystals of tenofovir alafenamide |
| TWI845826B (zh) | 2020-03-20 | 2024-06-21 | 美商基利科學股份有限公司 | 4'-c-經取代-2-鹵基-2'-去氧腺苷核苷之前藥及其製造與使用方法 |
| KR20210125298A (ko) | 2020-04-08 | 2021-10-18 | 주식회사 파마코스텍 | 테노포비어 알라펜아미드 헤미타르트레이트의 신규한 제조방법 |
| US11680064B2 (en) | 2020-06-25 | 2023-06-20 | Gilead Sciences, Inc. | Capsid inhibitors for the treatment of HIV |
| AU2021377614A1 (en) | 2020-11-11 | 2023-06-22 | Gilead Sciences, Inc. | METHODS OF IDENTIFYING HIV PATIENTS SENSITIVE TO THERAPY WITH gp120 CD4 BINDING SITE-DIRECTED ANTIBODIES |
| 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 |
| CA3235937A1 (en) | 2021-12-03 | 2023-06-08 | Gilead Sciences, Inc. | Therapeutic compounds for hiv virus infection |
| KR20240117588A (ko) | 2021-12-03 | 2024-08-01 | 길리애드 사이언시즈, 인코포레이티드 | Hiv 바이러스 감염 치료용 화합물 |
| CN118369316A (zh) | 2021-12-03 | 2024-07-19 | 吉利德科学公司 | Hiv病毒感染的治疗性化合物 |
| TWI843506B (zh) | 2022-04-06 | 2024-05-21 | 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 |
| WO2024006982A1 (en) | 2022-07-01 | 2024-01-04 | Gilead Sciences, Inc. | Therapeutic compounds useful for the prophylactic or therapeutic treatment of an hiv virus infection |
| US20240083984A1 (en) | 2022-08-26 | 2024-03-14 | Gilead Sciences, Inc. | Dosing and scheduling regimen for broadly neutralizing antibodies |
| US20240226130A1 (en) | 2022-10-04 | 2024-07-11 | Gilead Sciences, Inc. | 4'-thionucleoside analogues and their pharmaceutical use |
| WO2024220624A1 (en) | 2023-04-19 | 2024-10-24 | Gilead Sciences, Inc. | Dosing regimen of capsid inhibitor |
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 |
| DE10399025I2 (de) | 1990-09-14 | 2007-11-08 | Acad Of Science Czech Republic | Wirkstoffvorläufer von Phosphonaten |
| 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 |
| US5922695A (en) | 1996-07-26 | 1999-07-13 | Gilead Sciences, Inc. | Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability |
| DE69722004T2 (de) | 1996-07-26 | 2004-04-01 | Gilead Sciences, Inc., Foster City | Nukleotidanaloga |
| SG106656A1 (en) | 1997-07-25 | 2004-10-29 | Gilead Sciences Inc | Nucleotide analog composition and synthesis method |
| NZ536942A (en) * | 2000-07-21 | 2006-03-31 | Gilead Sciences Inc | Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same |
| MY131488A (en) | 2002-04-08 | 2007-08-30 | 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 | |
| US8633219B2 (en) | 2004-05-21 | 2014-01-21 | Japan Tobacco Inc. | Combination therapy |
| WO2007013086A1 (en) | 2005-07-26 | 2007-02-01 | Hetero Drugs Limited | Novel polymorphs of tenofovir disoproxil fumarate |
| EP3112355B1 (en) | 2006-07-07 | 2020-04-29 | Gilead Sciences, Inc. | Modulators of pharmacokinetic properties of therapeutics |
| EP2046792B1 (en) | 2006-07-12 | 2015-02-25 | Mylan Laboratories Limited | Process for the preparation of tenofovir |
| HUE029842T2 (en) | 2007-02-23 | 2017-04-28 | Gilead Sciences Inc | Modulation of pharmacokinetic parameters of therapeutic agents |
| US20090270352A1 (en) | 2007-05-22 | 2009-10-29 | Ultimorphix Technologies B.V. | Tenofovir Disoproxil Hemi-Fumaric Acid Co-Crystal |
| MX342377B (es) | 2008-05-02 | 2016-09-27 | Gilead Sciences Inc | Uso de particulas trasportadoras solidas para mejorar la capacidad de procesamiento de un agente farmaceutico. |
| WO2010091197A2 (en) | 2009-02-06 | 2010-08-12 | Gilead Sciences, Inc. | Tablets for combination therapy |
| US7973013B2 (en) | 2009-09-21 | 2011-07-05 | Gilead Sciences, Inc. | 2'-fluoro substituted carba-nucleoside analogs for antiviral treatment |
| EA025852B1 (ru) | 2010-11-19 | 2017-02-28 | Джилид Сайэнс, Инк. | ТЕРАПЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ РИЛПИВИРИН HCl И ТЕНОФОВИРА ДИЗОПРОКСИЛФУМАРАТ |
| RS55353B2 (sr) | 2011-08-16 | 2023-11-30 | Gilead Sciences Inc | Tenofovir alafenamid hemifumarat |
| ES2661705T3 (es) | 2011-10-07 | 2018-04-03 | Gilead Sciences, Inc. | Métodos para la preparación de análogos de nucleótidos antivirales |
| EA026138B1 (ru) | 2012-02-03 | 2017-03-31 | Джилид Сайэнс, Инк. | Комбинированная терапия, включающая тенофовир алафенамида гемифумарат и кобицистат, для применения для лечения вирусных инфекций |
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