HRP20230208T1 - MEZILATNA SOL AMINO-LUPANSKOG SPOJA S INHIBITORSKOM AKTIVNOŠĆU SAZRIJEVANJA HIV-a - Google Patents
MEZILATNA SOL AMINO-LUPANSKOG SPOJA S INHIBITORSKOM AKTIVNOŠĆU SAZRIJEVANJA HIV-a Download PDFInfo
- Publication number
- HRP20230208T1 HRP20230208T1 HRP20230208TT HRP20230208T HRP20230208T1 HR P20230208 T1 HRP20230208 T1 HR P20230208T1 HR P20230208T T HRP20230208T T HR P20230208TT HR P20230208 T HRP20230208 T HR P20230208T HR P20230208 T1 HRP20230208 T1 HR P20230208T1
- Authority
- HR
- Croatia
- Prior art keywords
- inhibitors
- hiv
- mesylate salt
- crystalline form
- tablet
- Prior art date
Links
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 title claims 7
- 230000035800 maturation Effects 0.000 title claims 2
- 230000002401 inhibitory effect Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- 208000031886 HIV Infections Diseases 0.000 claims 2
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 claims 2
- 208000037357 HIV infectious disease Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 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
- 150000003839 salts Chemical class 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
- 102100031650 C-X-C chemokine receptor type 4 Human genes 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- 102000004163 DNA-directed RNA polymerases Human genes 0.000 claims 1
- 108090000626 DNA-directed RNA polymerases Proteins 0.000 claims 1
- 229940099797 HIV integrase inhibitor Drugs 0.000 claims 1
- 101000922348 Homo sapiens C-X-C chemokine receptor type 4 Proteins 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 1
- 229950004159 bictegravir Drugs 0.000 claims 1
- SOLUWJRYJLAZCX-LYOVBCGYSA-N bictegravir Chemical compound C([C@H]1O[C@@H]2CC[C@@H](C2)N1C(=O)C1=C(C2=O)O)N1C=C2C(=O)NCC1=C(F)C=C(F)C=C1F SOLUWJRYJLAZCX-LYOVBCGYSA-N 0.000 claims 1
- 229950005928 cabotegravir Drugs 0.000 claims 1
- WCWSTNLSLKSJPK-LKFCYVNXSA-N cabotegravir Chemical compound C([C@H]1OC[C@@H](N1C(=O)C1=C(O)C2=O)C)N1C=C2C(=O)NCC1=CC=C(F)C=C1F WCWSTNLSLKSJPK-LKFCYVNXSA-N 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 230000034303 cell budding Effects 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 229960002542 dolutegravir Drugs 0.000 claims 1
- RHWKPHLQXYSBKR-BMIGLBTASA-N dolutegravir Chemical compound C([C@@H]1OCC[C@H](N1C(=O)C1=C(O)C2=O)C)N1C=C2C(=O)NCC1=CC=C(F)C=C1F RHWKPHLQXYSBKR-BMIGLBTASA-N 0.000 claims 1
- 239000007888 film coating Substances 0.000 claims 1
- 238000009501 film coating Methods 0.000 claims 1
- 239000002835 hiv fusion inhibitor Substances 0.000 claims 1
- 239000003084 hiv integrase inhibitor Substances 0.000 claims 1
- 239000004030 hiv protease inhibitor Substances 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- 229940057948 magnesium stearate Drugs 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 229960001855 mannitol Drugs 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 229940069328 povidone Drugs 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 229940079832 sodium starch glycolate Drugs 0.000 claims 1
- 229920003109 sodium starch glycolate Polymers 0.000 claims 1
- 239000008109 sodium starch glycolate Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
- C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (15)
1. Mezilatna sol spoja
[image]
2. Kristalni oblik mezilatne soli prema zahtjevu 1.
3. Bezvodni kristalni oblik mezilatne soli prema zahtjevu 1.
4. Bezvodni kristalni oblik mezilatne soli prema zahtjevu 1, naznačen time što daje XRPD uzorak uglavnom u skladu sa slikom 1.
5. Bezvodni kristalni oblik mezilatne soli prema zahtjevu 1, naznačen time što daje XRPD uzorak uglavnom kako je navedeno u Tablici 2
[image]
6. Bezvodni kristalni oblik mezilatne soli prema zahtjevu 1 naznačen je XRPD uzorkom koji ima reprezentativne difrakcijske vrhove, u o2ө: 7.6±3.0, 9.5±0.3, 11.4±0.3, 11.7±0.3, 12.3±0.3, i 13.1±0.3.
7. Farmaceutski pripravak sadrži sol u skladu s bilo kojim od zahtjeva 1-6.
8. Farmaceutski pripravak u skladu sa zahtjevom 7 nadalje sadrži farmaceutski prihvatljivu pomoćnu tvar.
9. Farmaceutski pripravak prema zahtjevu 8 naznačen time što je navedeni pripravak u obliku tablete, kapsule, ili obliku pogodnom za injekciju.
10. Tableta u skladu sa zahtjevom 9, nadalje sadrži najmanje jedan farmaceutski prihvatljiv ekscipijent odabran iz skupine koju čine mikrokristalna celuloza, manitol, natrijev škrobni glikolat, povidon, i magnezijev stearat.
11. Tableta u skladu sa zahtjevom 10 naznačena time što je navedena tableta obložena filmskom prevlakom na bazi polimera.
12. Farmaceutski pripravak u skladu s bilo kojim od zahtjeva 7-11 za uporabu u liječenju HIV infekcije kod ljudi.
13. Farmaceutski pripravak za uporabu u skladu sa zahtjevom 12, naznačen time što uporaba nadalje sadrži davanje čovjeku najmanje jedno drugo sredstvo koje se koristi za liječenje HIV infekcije odabrano iz skupine koja se sastoji od nukleozida inhibitora HIV reverzne transkriptaze, ne-nukleozidni inhibitori HIV reverzne transkriptaze, inhibitori HIV proteaze, inhibitori HIV fuzije, inhibitori vezanja HIV-a, inhibitori CCR5, inhibitori CXCR4, inhibitori pupanja ili sazrijevanja HIV-a, i inhibitori HIV integraze.
14. Farmaceutski pripravak za uporabu u skladu sa zahtjevom 12 naznačen time što je navedeno drugo sredstvo odabrano iz skupine koja se sastoji od dolutegravira, biktegravira, i kabotegravira.
15. Sol kako je definirana u bilo kojem od zahtjeva 1-6 za uporabu u terapiji.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862777432P | 2018-12-10 | 2018-12-10 | |
| US201962874557P | 2019-07-16 | 2019-07-16 | |
| PCT/IB2019/060564 WO2020121161A1 (en) | 2018-12-10 | 2019-12-09 | Mesylate salt of an amino-lupane compound with hiv maturation inhibitory activity |
| EP19823817.2A EP3894424B1 (en) | 2018-12-10 | 2019-12-09 | Mesylate salt of an amino-lupane compound with hiv maturation inhibitory activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20230208T1 true HRP20230208T1 (hr) | 2023-04-14 |
Family
ID=68944386
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20230208TT HRP20230208T1 (hr) | 2018-12-10 | 2019-12-09 | MEZILATNA SOL AMINO-LUPANSKOG SPOJA S INHIBITORSKOM AKTIVNOŠĆU SAZRIJEVANJA HIV-a |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20220024970A1 (hr) |
| EP (1) | EP3894424B1 (hr) |
| JP (1) | JP2022510475A (hr) |
| DK (1) | DK3894424T3 (hr) |
| ES (1) | ES2938486T3 (hr) |
| FI (1) | FI3894424T3 (hr) |
| HR (1) | HRP20230208T1 (hr) |
| HU (1) | HUE061184T2 (hr) |
| LT (1) | LT3894424T (hr) |
| PL (1) | PL3894424T3 (hr) |
| PT (1) | PT3894424T (hr) |
| RS (1) | RS64113B1 (hr) |
| SI (1) | SI3894424T1 (hr) |
| WO (1) | WO2020121161A1 (hr) |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014184553A1 (en) * | 2013-05-15 | 2014-11-20 | Cipla Limited | Pharmaceutical antiretroviral compositions |
| CR20160472A (es) | 2014-04-11 | 2017-03-10 | Viiv Healthcare Uk (No 4) Ltd | Triterpenoides con actividad inhibidora de la maduración del vih |
-
2019
- 2019-12-09 EP EP19823817.2A patent/EP3894424B1/en active Active
- 2019-12-09 SI SI201930452T patent/SI3894424T1/sl unknown
- 2019-12-09 WO PCT/IB2019/060564 patent/WO2020121161A1/en unknown
- 2019-12-09 US US17/296,627 patent/US20220024970A1/en not_active Abandoned
- 2019-12-09 LT LTEPPCT/IB2019/060564T patent/LT3894424T/lt unknown
- 2019-12-09 PT PT198238172T patent/PT3894424T/pt unknown
- 2019-12-09 PL PL19823817.2T patent/PL3894424T3/pl unknown
- 2019-12-09 HR HRP20230208TT patent/HRP20230208T1/hr unknown
- 2019-12-09 ES ES19823817T patent/ES2938486T3/es active Active
- 2019-12-09 DK DK19823817.2T patent/DK3894424T3/da active
- 2019-12-09 JP JP2021532391A patent/JP2022510475A/ja active Pending
- 2019-12-09 HU HUE19823817A patent/HUE061184T2/hu unknown
- 2019-12-09 FI FIEP19823817.2T patent/FI3894424T3/fi active
- 2019-12-09 RS RS20230264A patent/RS64113B1/sr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2020121161A1 (en) | 2020-06-18 |
| EP3894424A1 (en) | 2021-10-20 |
| JP2022510475A (ja) | 2022-01-26 |
| ES2938486T3 (es) | 2023-04-11 |
| SI3894424T1 (sl) | 2023-04-28 |
| EP3894424B1 (en) | 2023-01-25 |
| RS64113B1 (sr) | 2023-04-28 |
| PL3894424T3 (pl) | 2023-05-02 |
| LT3894424T (lt) | 2023-03-10 |
| US20220024970A1 (en) | 2022-01-27 |
| DK3894424T3 (da) | 2023-03-06 |
| HUE061184T2 (hu) | 2023-05-28 |
| PT3894424T (pt) | 2023-02-28 |
| FI3894424T3 (fi) | 2023-04-25 |
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