HRP20211622T1 - 4'-supstituirani nukleozidni-derivati kao inhibitori hiv reverzne transkriptaze - Google Patents
4'-supstituirani nukleozidni-derivati kao inhibitori hiv reverzne transkriptaze Download PDFInfo
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- HRP20211622T1 HRP20211622T1 HRP20211622TT HRP20211622T HRP20211622T1 HR P20211622 T1 HRP20211622 T1 HR P20211622T1 HR P20211622T T HRP20211622T T HR P20211622TT HR P20211622 T HRP20211622 T HR P20211622T HR P20211622 T1 HRP20211622 T1 HR P20211622T1
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- Prior art keywords
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- pharmaceutically acceptable
- acceptable salt
- compound according
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- 108010078851 HIV Reverse Transcriptase Proteins 0.000 title claims 6
- 150000003833 nucleoside derivatives Chemical class 0.000 title claims 4
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 title claims 3
- 150000001875 compounds Chemical class 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 14
- 239000002259 anti human immunodeficiency virus agent Substances 0.000 claims 8
- 229940124411 anti-hiv antiviral agent Drugs 0.000 claims 8
- 239000000825 pharmaceutical preparation Substances 0.000 claims 7
- -1 methyl tetrahydrogen triphosphate Chemical compound 0.000 claims 6
- 239000003443 antiviral agent Substances 0.000 claims 4
- 239000002835 hiv fusion inhibitor Substances 0.000 claims 4
- 238000011321 prophylaxis Methods 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 3
- 239000002777 nucleoside Substances 0.000 claims 3
- 238000011282 treatment Methods 0.000 claims 3
- 208000030507 AIDS Diseases 0.000 claims 2
- 208000031886 HIV Infections Diseases 0.000 claims 2
- 229940126154 HIV entry inhibitor Drugs 0.000 claims 2
- 208000037357 HIV infectious disease Diseases 0.000 claims 2
- 229940126252 HIV maturation inhibitor Drugs 0.000 claims 2
- 229960005475 antiinfective agent Drugs 0.000 claims 2
- 239000004599 antimicrobial Substances 0.000 claims 2
- 239000004030 hiv protease inhibitor Substances 0.000 claims 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 2
- 239000002955 immunomodulating agent Substances 0.000 claims 2
- YSIBYEBNVMDAPN-CMDGGOBGSA-N (e)-4-oxo-4-(3-triethoxysilylpropylamino)but-2-enoic acid Chemical compound CCO[Si](OCC)(OCC)CCCNC(=O)\C=C\C(O)=O YSIBYEBNVMDAPN-CMDGGOBGSA-N 0.000 claims 1
- NUBQKPWHXMGDLP-UHFFFAOYSA-N 1-[4-benzyl-2-hydroxy-5-[(2-hydroxy-2,3-dihydro-1h-inden-1-yl)amino]-5-oxopentyl]-n-tert-butyl-4-(pyridin-3-ylmethyl)piperazine-2-carboxamide;sulfuric acid Chemical compound OS(O)(=O)=O.C1CN(CC(O)CC(CC=2C=CC=CC=2)C(=O)NC2C3=CC=CC=C3CC2O)C(C(=O)NC(C)(C)C)CN1CC1=CC=CN=C1 NUBQKPWHXMGDLP-UHFFFAOYSA-N 0.000 claims 1
- ZIAOVIPSKUPPQW-UHFFFAOYSA-N 3-chloro-5-[1-[(4-methyl-5-oxo-1h-1,2,4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethyl)pyridin-3-yl]oxybenzonitrile Chemical group N1C(=O)N(C)C(CN2C(C(OC=3C=C(C=C(Cl)C=3)C#N)=C(C=C2)C(F)(F)F)=O)=N1 ZIAOVIPSKUPPQW-UHFFFAOYSA-N 0.000 claims 1
- 108010019625 Atazanavir Sulfate Proteins 0.000 claims 1
- 108010002459 HIV Integrase Proteins 0.000 claims 1
- 229940099797 HIV integrase inhibitor Drugs 0.000 claims 1
- 229940122313 Nucleoside reverse transcriptase inhibitor Drugs 0.000 claims 1
- IRHXGOXEBNJUSN-YOXDLBRISA-N Saquinavir mesylate Chemical compound CS(O)(=O)=O.C([C@@H]([C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)C=1N=C2C=CC=CC2=CC=1)C1=CC=CC=C1 IRHXGOXEBNJUSN-YOXDLBRISA-N 0.000 claims 1
- 229960000531 abacavir sulfate Drugs 0.000 claims 1
- WMHSRBZIJNQHKT-FFKFEZPRSA-N abacavir sulfate Chemical compound OS(O)(=O)=O.C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1.C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1 WMHSRBZIJNQHKT-FFKFEZPRSA-N 0.000 claims 1
- 229940124425 anti-infective immunomodulator Drugs 0.000 claims 1
- 229960003796 atazanavir sulfate Drugs 0.000 claims 1
- 229960000475 delavirdine mesylate Drugs 0.000 claims 1
- WHBIGIKBNXZKFE-UHFFFAOYSA-N delavirdine mesylate Natural products CC(C)NC1=CC=CN=C1N1CCN(C(=O)C=2NC3=CC=C(NS(C)(=O)=O)C=C3C=2)CC1 WHBIGIKBNXZKFE-UHFFFAOYSA-N 0.000 claims 1
- MEPNHSOMXMALDZ-UHFFFAOYSA-N delavirdine mesylate Chemical compound CS(O)(=O)=O.CC(C)NC1=CC=CN=C1N1CCN(C(=O)C=2NC3=CC=C(NS(C)(=O)=O)C=C3C=2)CC1 MEPNHSOMXMALDZ-UHFFFAOYSA-N 0.000 claims 1
- 229950003141 doravirine Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003084 hiv integrase inhibitor Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 229960004243 indinavir sulfate Drugs 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000004048 modification Effects 0.000 claims 1
- 238000012986 modification Methods 0.000 claims 1
- 229960005230 nelfinavir mesylate Drugs 0.000 claims 1
- NQHXCOAXSHGTIA-SKXNDZRYSA-N nelfinavir mesylate Chemical compound CS(O)(=O)=O.CC1=C(O)C=CC=C1C(=O)N[C@H]([C@H](O)CN1[C@@H](C[C@@H]2CCCC[C@@H]2C1)C(=O)NC(C)(C)C)CSC1=CC=CC=C1 NQHXCOAXSHGTIA-SKXNDZRYSA-N 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 229960003542 saquinavir mesylate Drugs 0.000 claims 1
- 229960003560 tenofovir alafenamide fumarate Drugs 0.000 claims 1
- SVUJNSGGPUCLQZ-FQQAACOVSA-N tenofovir alafenamide fumarate Chemical group 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 1
- 229960004693 tenofovir disoproxil fumarate Drugs 0.000 claims 1
- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical group 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 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 235000011178 triphosphate Nutrition 0.000 claims 1
- 239000001226 triphosphate Substances 0.000 claims 1
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/12—Triazine radicals
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
-
- 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
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/14—Pyrrolo-pyrimidine radicals
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Gastroenterology & Hepatology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (27)
1. Spoj strukturne formule II
[image]
ili njegova farmaceutski prihvatljiva sol, gdje:
X je O;
Y je -C=CH;
R1 je -H,
[image]
ili
[image]
ili pro-lijek modifikacija mono-, di- ili trifosfata;
R2 je -H;
R3 je -H;
R4 je -NH2;
R5 je -H, -Cl, -F ili -NH2, i;
R9 je -H, -F, -Cl, -I, -Br ili CH3.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time što:
R1 je -H.
3. Spoj prema patentnom zahtjevu 1 ili patentnom zahtjevu 2 koji je:
[image]
ili njegova farmaceutski prihvatljiva sol.
4. Spoj prema bilo kojem prethodnom patentnom zahtjevu, ili njegova farmaceutski prihvatljiva sol, izabran iz grupe koja se sastoji od:
[image]
i
[image]
i njihovih farmaceutski prihvatljivih soli.
5. Spoj prema bilo kojem prethodnom patentnom zahtjevu koji je:
[image]
6. Spoj prema bilo kojem prethodnom patentnom zahtjevu koji je farmaceutski prihvatljiva sol od:
[image]
7. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4 koji je:
[image]
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4 koji je farmaceutski prihvatljiva sol od:
[image]
9. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4 koji je:
[image]
10. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4 koji je farmaceutski prihvatljiva sol od:
[image]
11. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4 koji je:
[image]
12. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4 koji je farmaceutski prihvatljiva sol od:
[image]
13. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4 izabran iz grupe koja se sastoji od:
((2R,3S,5R)-5-(4-amino-7H-pirolo[2,3-d]pirimidin-7-il)-2-etinil-3-hidroksitetrahidrofuran-2-il)metil tetrahidrogen trifosfata;
((2R,3S,5R)-5-(4-amino-5-fluoro-7H-pirolo[2,3-d]pirimidin-7-il)-2-etinil-3-hidroksitetrahidrofuran-2-il)metil tetrahidrogen trifosfata, i;
((2R,3S,5R)-5-(4-amino-2-hloro-7H-pirolo[2,3-d]pirimidin-7-il)-2-etinil-3-hidroksitetrahidrofuran-2-il)metil tetrahidrogen trifosfata.
14. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4 koji je:
((2R,3S,5R)-5-(4-amino-7H-pirolo[2,3-d]pirimidin-7-il)-2-etinil-3-hidroksitetrahidrofuran-2-il)metil tetrahidrogen trifosfat.
15. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4 koji je:
((2R,3S,5R)-5-(4-amino-5-fluoro-7H-pirolo[2,3-d]pirimidin-7-il)-2-etinil-3-hidroksitetrahidrofuran-2-il)metil tetrahidrogen trifosfat.
16. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4 koji je:
((2R,3S,5R)-5-(4-amino-2-hloro-7H-pirolo[2,3-d]pirimidin-7-il)-2-etinil-3-hidroksitetrahidrofuran-2-il)metil tetrahidrogen trifosfat.
17. Farmaceutski pripravak koji sadrži spoj ili njegovu farmaceutski prihvatljivu sol, prema bilo kojem od patentnih zahtjeva 1 do 16 i farmaceutski prihvatljiv nosač.
18. Spoj, ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od patentnih zahtjeva 1 do 16 za uporabu u terapiji.
19. Spoj, ili njegova farmaceutski prihvatljiva sol, prema bilo kojem od patentnih zahtjeva 1 do 16 za uporabu u inhibiciji HIV reverzne transkriptaze, liječenju ili profilaksi infekcije HIV-om, ili liječenje, profilaksu ili odlaganje početka SIDA-e.
20. Farmaceutski pripravak prema patentnom zahtjevu 17, koji dalje sadrži jedno ili više anti-HIV sredstava izabranih iz grupe koja se sastoji od HIV antivirusnih sredstava, imunomodulatora i anti-infektivnih sredstava.
21. Farmaceutski pripravak prema patentnom zahtjevu 20, naznačen time što anti-HIV sredstvo je izabrano od jednog ili više antivirusnih sredstava izabranih iz grupe koja se sastoji od inhibitora HIV proteaze, nukleozidnih inhibitora HIV reverzne transkriptaze, ne-nukleozidnih inhibitora HIV reverzne transkriptaze, inhibitora HIV integraze, inhibitora fuzije HIV-a, inhibitora ulaska HIV-a i inhibitora sazrijevanja HIV-a.
22. Kombinacija koja sadrži spoj ili njegovu farmaceutski prihvatljivu sol, prema bilo kojem od patentnih zahtjeva 1 do 16 i jedno ili više anti-HIV sredstava izabranih od HIV antivirusnih sredstava, anti-infektivnih sredstava i imunomodulatora za uporabu u inhibiciji HIV reverzne transkriptaze, liječenju ili profilaksi infekcije HIV-om, ili liječenju ili profilaksi, ili odlaganju početka ili napredovanja SIDA-e.
23. Kombinacija za uporabu prema patentnom zahtjevu 22, naznačena time što anti-HIV sredstvo je antivirusno sredstvo izabrano iz grupe koja se sastoji od inhibitora HIV proteaze, nukleozidnih inhibitora HIV reverzne transkriptaze, nenukleozidnih inhibitora HIV reverzne transkriptaze, inhibitora HIV integraze, inhibitora fuzija HIV-a, inhibitora ulaska HIV-a i inhibitora sazrijevanja HIV-a.
24. Farmaceutski pripravak prema patentnom zahtjevu 20 ili kombinacija za uporabu prema patentnom zahtjevu 22, naznačen time što je anti-HIV sredstvo izabrano od sljedećih
[image]
[image]
sljedeći lijekovi navedeni u tabeli su u obliku soli: abakavir sulfat, delavirdin mezilat, indinavir sulfat, atazanavir sulfat, nelfinavir mezilat i sakvinavir mezilat.
25. Farmaceutski pripravak prema patentnom zahtjevu 20 ili kombinacija za uporabu prema patentnom zahtjevu 22, naznačen time što anti-HIV sredstvo je doravirin.
26. Farmaceutski pripravak prema patentnom zahtjevu 20 ili kombinacija za uporabu prema patentnom zahtjevu 22, naznačen time što anti-HIV sredstvo je tenofovir dizoproksil fumarat.
27. Farmaceutski pripravak prema patentnom zahtjevu 20 ili kombinacija za uporabu prema patentnom zahtjevu 22, naznačen time što anti-HIV sredstvo je tenofovir alafenamid fumarat.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2014/074294 WO2015143712A1 (en) | 2014-03-28 | 2014-03-28 | 4'-substituted nucleoside reverse transcriptase inhibitors |
| PCT/US2015/022621 WO2015148746A1 (en) | 2014-03-28 | 2015-03-26 | 4'-substituted nucleoside-derivatives as hiv reverse transcriptase inhibitors |
| EP15715934.4A EP3122752B1 (en) | 2014-03-28 | 2015-03-26 | 4'-substituted nucleoside-derivatives as hiv reverse transcriptase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20211622T1 true HRP20211622T1 (hr) | 2022-03-04 |
Family
ID=52824598
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20211622TT HRP20211622T1 (hr) | 2014-03-28 | 2015-03-26 | 4'-supstituirani nukleozidni-derivati kao inhibitori hiv reverzne transkriptaze |
Country Status (41)
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MA41213A (fr) * | 2014-12-19 | 2017-10-24 | Alios Biopharma Inc | Nucléosides substitués, nucléotides et analogues de ceux-ci |
| CR20180101A (es) | 2015-08-13 | 2018-04-12 | Merck Sharp & Dohme | Compuestos di-nucleóticos cíclicos como agonistas de sting |
| US11453697B1 (en) | 2015-08-13 | 2022-09-27 | Merck Sharp & Dohme Llc | Cyclic di-nucleotide compounds as sting agonists |
| RU2720811C2 (ru) * | 2015-09-23 | 2020-05-13 | Мерк Шарп И Доум Лимитед | 4'-замещенные нуклеозидные ингибиторы обратной транскриптазы и их получение |
| JOP20170038B1 (ar) | 2016-02-12 | 2021-08-17 | Merck Sharp & Dohme | مركبات للاستخدام لعلاج عدوى بفيروس hiv والوقاية منه |
| TW201803871A (zh) | 2016-06-24 | 2018-02-01 | 英塞特公司 | 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物 |
| CN110036001B (zh) | 2016-10-04 | 2022-03-22 | 默沙东公司 | 作为STING激动剂的苯并[b]噻吩化合物 |
| JP7125714B2 (ja) * | 2016-12-13 | 2022-08-25 | ヤマサ醤油株式会社 | 抗ウイルス活性を有する２’－デオキシ－７－デアザプリンヌクレオシド誘導体 |
| EP3621624B1 (en) | 2017-05-12 | 2023-08-30 | Merck Sharp & Dohme LLC | Cyclic di-nucleotide compounds as sting agonists |
| US11312772B2 (en) | 2017-08-04 | 2022-04-26 | Merck Sharp & Dohme Corp. | Combinations of PD-1 antagonists and benzo [b] thiophene STING agonists for cancer treatment |
| CA3071538A1 (en) | 2017-08-04 | 2019-02-07 | Merck Sharp & Dohme Corp. | Benzo[b]thiophene sting agonists for cancer treatment |
| MA50172A (fr) | 2017-09-18 | 2021-04-07 | Janssen Biopharma Inc | Nucléosides substitués, nucléotides et analogues de ceux-ci |
| EP3727401A4 (en) | 2017-12-20 | 2022-04-06 | Merck Sharp & Dohme Corp. | CYCLIC DINUCLEOTIDE COMPOUNDS USED AS STING AGONISTS |
| CN111971284A (zh) * | 2017-12-27 | 2020-11-20 | 埃默里大学 | 核苷和/或nadph氧化酶(nox)抑制剂作为髓样特异性抗病毒剂的联合模式 |
| WO2019171285A1 (en) * | 2018-03-07 | 2019-09-12 | Glaxosmithkline Intellectual Property (No.2) Limited | Compounds useful in hiv therapy |
| WO2019195063A1 (en) | 2018-04-03 | 2019-10-10 | Merck Sharp & Dohme Corp. | Aza-benzothiophene compounds as sting agonists |
| BR112020020085A8 (pt) | 2018-04-03 | 2023-04-11 | Merck Sharp & Dohme | Composto, composição farmacêutica, e, métodos para induzir uma resposta imune, para induzir produção de interferons de tipo i dependentes de sting e para tratar um distúrbio de proliferação celular |
| WO2020014041A1 (en) * | 2018-07-09 | 2020-01-16 | Merck Sharp & Dohme Corp. | Enzymatic synthesis of 4'-ethynyl nucleoside analogs |
| MA53280A (fr) * | 2018-08-09 | 2021-11-17 | Glaxosmithkline Ip No 2 Ltd | Composés utiles dans la thérapie du vih |
| WO2020154656A1 (en) | 2019-01-25 | 2020-07-30 | Brown University | Compositions and methods for treating, preventing or reversing age-associated inflammation and disorders |
| EP3934760A1 (en) * | 2019-03-06 | 2022-01-12 | GlaxoSmithKline Intellectual Property (No.2) Limited | Compounds useful in hiv therapy |
| CN110054654B (zh) * | 2019-05-27 | 2022-12-27 | 武汉百科药物开发有限公司 | 一种地西他滨中间体α-取代脱氧核糖的合成方法 |
| CN114793421B (zh) * | 2019-09-11 | 2024-09-13 | 斯克里普斯研究所 | 抗病毒前体药物及其药物组合物 |
| MX2022006940A (es) * | 2019-12-09 | 2022-07-11 | Viiv Healthcare Co | Composiciones farmaceuticas. |
| TW202245800A (zh) | 2020-02-18 | 2022-12-01 | 美商基利科學股份有限公司 | 抗病毒化合物 |
| CN118598916A (zh) | 2020-02-18 | 2024-09-06 | 吉利德科学公司 | 抗病毒化合物 |
| CN112321589B (zh) * | 2020-02-18 | 2022-05-03 | 山东科巢生物制药有限公司 | 一种抗病毒药物瑞德西韦及其中间体的合成方法 |
| TW202322824A (zh) | 2020-02-18 | 2023-06-16 | 美商基利科學股份有限公司 | 抗病毒化合物 |
| WO2021188959A1 (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 |
| CN112778310A (zh) * | 2020-04-20 | 2021-05-11 | 中国科学院上海药物研究所 | 核苷类似物或含有核苷类似物的组合制剂在抗病毒中的应用 |
| CN113527303B (zh) * | 2020-04-21 | 2022-06-10 | 浙江工业大学 | 一种瑞德西韦母核中间体的制备工艺 |
| CN113637041B (zh) * | 2020-05-11 | 2024-02-27 | 上海科胜药物研发有限公司 | 一种核糖核苷的制备方法 |
| WO2022031894A1 (en) | 2020-08-07 | 2022-02-10 | Gilead Sciences, Inc. | Prodrugs of phosphonamide nucleotide analogues and their pharmaceutical use |
| WO2022074391A1 (en) | 2020-10-08 | 2022-04-14 | Storm Therapeutics Limited | Compounds inhibitors of mettl3 |
| CN112300236A (zh) * | 2020-10-21 | 2021-02-02 | 佛山科学技术学院 | 核苷酸混合氨基磷酸酯化合物、其药物组合物及其应用 |
| WO2022159877A1 (en) | 2021-01-25 | 2022-07-28 | Brii Biosciences, Inc. | Combination therapy for hiv with adenosine derivative and capsid inhibitors |
| EP4281081A1 (en) | 2021-01-25 | 2023-11-29 | Brii Biosciences, Inc. | Adenosine derivative and pharmaceutical composition comprising the same |
| WO2022221514A1 (en) | 2021-04-16 | 2022-10-20 | Gilead Sciences, Inc. | Methods of preparing carbanucleosides using amides |
| IL310854A (en) | 2021-08-20 | 2024-04-01 | Shionogi & Co | Nucleoside compounds and their drug derivatives possessing viral growth inhibitory activity |
| EP4405357A1 (en) | 2021-09-23 | 2024-07-31 | Katholieke Universiteit Leuven KU Leuven Research & Development | Ribonucleoside analogues against -sars-cov-2 |
| US20240287124A1 (en) | 2023-01-30 | 2024-08-29 | Merck Sharp & Dohme Llc | Prodrugs of 4'-substituted nucleoside reverse transcriptase inhibitors |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5681941A (en) | 1990-01-11 | 1997-10-28 | Isis Pharmaceuticals, Inc. | Substituted purines and oligonucleotide cross-linking |
| KR927003044A (ko) | 1990-01-11 | 1992-12-17 | 크리스토퍼 케이. 미라벨리 | Rna 활성과 유전자 발현을 검출하고 조절하는 조성물 및 그 방법 |
| ATE271063T1 (de) | 1996-10-16 | 2004-07-15 | Icn Pharmaceuticals | Purin-l-nukleoside, deren analoga und verwendungen |
| DE60005501T2 (de) | 1999-05-12 | 2004-06-24 | Yamasa Corp., Choshi | 4'-c-ethynyl-pyrimidine nukleoside |
| US6831069B2 (en) | 1999-08-27 | 2004-12-14 | Ribapharm Inc. | Pyrrolo[2,3-d]pyrimidine nucleoside analogs |
| WO2003062256A1 (en) | 2002-01-17 | 2003-07-31 | Ribapharm Inc. | 2'-beta-modified-6-substituted adenosine analogs and their use as antiviral agents |
| WO2003099840A1 (en) | 2002-05-24 | 2003-12-04 | Isis Pharmaceuticals, Inc. | Oligonucleotides having modified nucleoside units |
| US20040229839A1 (en) | 2003-05-14 | 2004-11-18 | Biocryst Pharmaceuticals, Inc. | Substituted nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases |
| WO2004106356A1 (en) | 2003-05-27 | 2004-12-09 | Syddansk Universitet | Functionalized nucleotide derivatives |
| WO2005003047A1 (en) | 2003-07-03 | 2005-01-13 | Philips Intellectual Property & Standards Gmbh | Pane which can be heated by means of invisible light |
| CA2502109C (en) | 2004-03-24 | 2010-02-23 | Yamasa Corporation | 4'-c-substituted-2-haloadenosine derivative |
| WO2007095269A2 (en) | 2006-02-14 | 2007-08-23 | Merck & Co., Inc. | Nucleoside aryl phosphoramidates for the treatment of rna-dependent rna viral infection |
| US7960569B2 (en) | 2006-10-17 | 2011-06-14 | Bristol-Myers Squibb Company | Indole antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions |
| US20080261913A1 (en) | 2006-12-28 | 2008-10-23 | Idenix Pharmaceuticals, Inc. | Compounds and pharmaceutical compositions for the treatment of liver disorders |
| CN101003550B (zh) * | 2006-12-30 | 2010-05-19 | 河南省分析测试研究中心 | 8-卤代腺嘌呤类核苷化合物、合成方法和其药物用途 |
| MX2009007333A (es) | 2007-01-12 | 2009-08-31 | Biocryst Pharm Inc | Analogos de nucleosidos antivirales. |
| CN100532388C (zh) * | 2007-07-16 | 2009-08-26 | 郑州大学 | 2’-氟-4’-取代-核苷类似物、其制备方法及应用 |
| US20090318380A1 (en) | 2007-11-20 | 2009-12-24 | Pharmasset, Inc. | 2',4'-substituted nucleosides as antiviral agents |
| MX2010011659A (es) | 2008-04-23 | 2010-11-30 | Gilead Sciences Inc | Analogos de carba-nucleosido para tratamiento antiviral. |
| WO2010036407A2 (en) | 2008-05-15 | 2010-04-01 | Biocryst Pharmaceuticals, Inc. | Antiviral nucleoside analogs |
| EP2313102A2 (en) | 2008-07-03 | 2011-04-27 | Biota Scientific Management | Bycyclic nucleosides and nucleotides as therapeutic agents |
| GB0815968D0 (en) | 2008-09-03 | 2008-10-08 | Angeletti P Ist Richerche Bio | Antiviral agents |
| CN102216316A (zh) | 2008-09-05 | 2011-10-12 | 寿制药株式会社 | 取代胺衍生物及以其为有效成分的药物组合物 |
| EA201100851A1 (ru) | 2008-12-23 | 2012-04-30 | Фармассет, Инк. | Аналоги нуклеозидов |
| CL2009002207A1 (es) | 2008-12-23 | 2011-02-18 | Gilead Pharmasset Llc | Compuestos derivados de 3-hidroxi-5-(9h-purin-9-il)tetrahidrofuran-2-il, inhibidor de la replicacion de arn viral dependiente de arn; composicion farmaceutica; uso para el tratamiento de hepatitis c. |
| DE102009000180A1 (de) | 2009-01-13 | 2010-07-15 | Evonik Degussa Gmbh | Verfahren zur Herstellung von mehrschichtig beschichteten Gummipartikeln und mehrschichtig beschichtete Gummipartikel |
| GB0900914D0 (en) | 2009-01-20 | 2009-03-04 | Angeletti P Ist Richerche Bio | Antiviral agents |
| CN102421293A (zh) | 2009-03-20 | 2012-04-18 | 艾丽奥斯生物制药有限公司 | 取代的核苷和核苷酸类似物 |
| WO2011005860A2 (en) | 2009-07-07 | 2011-01-13 | Alnylam Pharmaceuticals, Inc. | 5' phosphate mimics |
| CA2782889C (en) | 2009-12-17 | 2014-08-05 | Merck Canada Inc. | Aminopyrimidines as syk inhibitors |
| MX2012013824A (es) | 2010-05-28 | 2013-03-12 | Biocryst Pharm Inc | Compuestos heterociclicos como inhibidores de cinasa janus. |
| ES2524356T3 (es) | 2010-07-22 | 2014-12-05 | Gilead Sciences, Inc. | Métodos y compuestos para tratar infecciones provocadas por virus Paramyxoviridae |
| TW201305185A (zh) | 2010-09-13 | 2013-02-01 | Gilead Sciences Inc | 用於抗病毒治療之２’－氟取代之碳－核苷類似物 |
| JP6242378B2 (ja) * | 2012-03-13 | 2017-12-06 | ギリアード サイエンシーズ， インコーポレイテッド | 抗ウイルス処置のための２’−置換カルバヌクレオシド類似体 |
| UA119050C2 (uk) * | 2013-11-11 | 2019-04-25 | Ґілеад Саєнсиз, Інк. | ПІРОЛО[1.2-f][1.2.4]ТРИАЗИНИ, ЯКІ ВИКОРИСТОВУЮТЬСЯ ДЛЯ ЛІКУВАННЯ РЕСПІРАТОРНО-СИНЦИТІАЛЬНИХ ВІРУСНИХ ІНФЕКЦІЙ |
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