HRP20110527T1 - Nukleozid-fosfonatni konjugati kao sredstva protiv hiv-a - Google Patents
Nukleozid-fosfonatni konjugati kao sredstva protiv hiv-a Download PDFInfo
- Publication number
- HRP20110527T1 HRP20110527T1 HR20110527T HRP20110527T HRP20110527T1 HR P20110527 T1 HRP20110527 T1 HR P20110527T1 HR 20110527 T HR20110527 T HR 20110527T HR P20110527 T HRP20110527 T HR P20110527T HR P20110527 T1 HRP20110527 T1 HR P20110527T1
- Authority
- HR
- Croatia
- Prior art keywords
- ester
- compound
- combination
- sulfate
- image
- Prior art date
Links
- -1 Nucleoside phosphonate Chemical class 0.000 title claims 16
- 239000002259 anti human immunodeficiency virus agent Substances 0.000 title 1
- 229940124411 anti-hiv antiviral agent Drugs 0.000 title 1
- 239000002777 nucleoside Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 9
- XQSPYNMVSIKCOC-NTSWFWBYSA-N Emtricitabine Chemical compound C1=C(F)C(N)=NC(=O)N1[C@H]1O[C@@H](CO)SC1 XQSPYNMVSIKCOC-NTSWFWBYSA-N 0.000 claims 6
- 230000000840 anti-viral effect Effects 0.000 claims 5
- 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 claims 4
- 229960000531 abacavir sulfate Drugs 0.000 claims 3
- 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 3
- XPOQHMRABVBWPR-ZDUSSCGKSA-N efavirenz Chemical compound C([C@]1(C2=CC(Cl)=CC=C2NC(=O)O1)C(F)(F)F)#CC1CC1 XPOQHMRABVBWPR-ZDUSSCGKSA-N 0.000 claims 3
- 229960000366 emtricitabine Drugs 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 239000004615 ingredient Substances 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 229960004693 tenofovir disoproxil fumarate Drugs 0.000 claims 3
- CWVMWSZEMZOUPC-JUAXIXHSSA-N (3s,5s,8r,9s,10s,13s,14s,16r)-16-bromo-3-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,14,15,16-tetradecahydrocyclopenta[a]phenanthren-17-one Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H]3CC[C@](C)(C([C@H](Br)C4)=O)[C@@H]4[C@@H]3CC[C@H]21 CWVMWSZEMZOUPC-JUAXIXHSSA-N 0.000 claims 2
- LHCOVOKZWQYODM-CPEOKENHSA-N 4-amino-1-[(2r,5s)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one;1-[(2r,4s,5s)-4-azido-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidine-2,4-dione Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1.O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](N=[N+]=[N-])C1 LHCOVOKZWQYODM-CPEOKENHSA-N 0.000 claims 2
- BXZVVICBKDXVGW-NKWVEPMBSA-N Didanosine Chemical compound O1[C@H](CO)CC[C@@H]1N1C(NC=NC2=O)=C2N=C1 BXZVVICBKDXVGW-NKWVEPMBSA-N 0.000 claims 2
- XPOQHMRABVBWPR-UHFFFAOYSA-N Efavirenz Natural products O1C(=O)NC2=CC=C(Cl)C=C2C1(C(F)(F)F)C#CC1CC1 XPOQHMRABVBWPR-UHFFFAOYSA-N 0.000 claims 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 2
- 125000003412 L-alanyl group Chemical group [H]N([H])[C@@](C([H])([H])[H])(C(=O)[*])[H] 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 229960001830 amprenavir Drugs 0.000 claims 2
- YMARZQAQMVYCKC-OEMFJLHTSA-N amprenavir Chemical compound C([C@@H]([C@H](O)CN(CC(C)C)S(=O)(=O)C=1C=CC(N)=CC=1)NC(=O)O[C@@H]1COCC1)C1=CC=CC=C1 YMARZQAQMVYCKC-OEMFJLHTSA-N 0.000 claims 2
- 229960002656 didanosine Drugs 0.000 claims 2
- 229960003804 efavirenz Drugs 0.000 claims 2
- 229960003586 elvitegravir Drugs 0.000 claims 2
- JUZYLCPPVHEVSV-LJQANCHMSA-N elvitegravir Chemical compound COC1=CC=2N([C@H](CO)C(C)C)C=C(C(O)=O)C(=O)C=2C=C1CC1=CC=CC(Cl)=C1F JUZYLCPPVHEVSV-LJQANCHMSA-N 0.000 claims 2
- 229960001627 lamivudine Drugs 0.000 claims 2
- JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 claims 2
- 229940033984 lamivudine / zidovudine Drugs 0.000 claims 2
- 238000013160 medical therapy Methods 0.000 claims 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- NQDJXKOVJZTUJA-UHFFFAOYSA-N nevirapine Chemical compound C12=NC=CC=C2C(=O)NC=2C(C)=CC=NC=2N1C1CC1 NQDJXKOVJZTUJA-UHFFFAOYSA-N 0.000 claims 2
- 229960000523 zalcitabine Drugs 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
- NKPHEWJJTGPRSL-OCCSQVGLSA-N 1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea Chemical compound CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O NKPHEWJJTGPRSL-OCCSQVGLSA-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
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- ILAYIAGXTHKHNT-UHFFFAOYSA-N 4-[4-(2,4,6-trimethyl-phenylamino)-pyrimidin-2-ylamino]-benzonitrile Chemical compound CC1=CC(C)=CC(C)=C1NC1=CC=NC(NC=2C=CC(=CC=2)C#N)=N1 ILAYIAGXTHKHNT-UHFFFAOYSA-N 0.000 claims 1
- HSBKFSPNDWWPSL-CAHLUQPWSA-N 4-amino-5-fluoro-1-[(2r,5s)-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]pyrimidin-2-one Chemical compound C1=C(F)C(N)=NC(=O)N1[C@H]1C=C[C@@H](CO)O1 HSBKFSPNDWWPSL-CAHLUQPWSA-N 0.000 claims 1
- HSBKFSPNDWWPSL-VDTYLAMSSA-N 4-amino-5-fluoro-1-[(2s,5r)-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]pyrimidin-2-one Chemical compound C1=C(F)C(N)=NC(=O)N1[C@@H]1C=C[C@H](CO)O1 HSBKFSPNDWWPSL-VDTYLAMSSA-N 0.000 claims 1
- ZGDKVKUWTCGYOA-BXVZCJGGSA-N Ancriviroc Chemical compound C=1C=C(Br)C=CC=1C(=N/OCC)/C(CC1)CCN1C(CC1)(C)CCN1C(=O)C1=C(C)C=C[N+]([O-])=C1C ZGDKVKUWTCGYOA-BXVZCJGGSA-N 0.000 claims 1
- 108010019625 Atazanavir Sulfate Proteins 0.000 claims 1
- 239000004156 Azodicarbonamide Substances 0.000 claims 1
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims 1
- 229920000858 Cyclodextrin Polymers 0.000 claims 1
- QNAYBMKLOCPYGJ-UHFFFAOYSA-N D-alpha-Ala Natural products CC([NH3+])C([O-])=O QNAYBMKLOCPYGJ-UHFFFAOYSA-N 0.000 claims 1
- 108010032976 Enfuvirtide Proteins 0.000 claims 1
- 239000001116 FEMA 4028 Substances 0.000 claims 1
- KJHKTHWMRKYKJE-SUGCFTRWSA-N Kaletra Chemical compound N1([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=2C=CC=CC=2)NC(=O)COC=2C(=CC=CC=2C)C)CC=2C=CC=CC=2)CCCNC1=O KJHKTHWMRKYKJE-SUGCFTRWSA-N 0.000 claims 1
- OFFWOVJBSQMVPI-RMLGOCCBSA-N Kaletra Chemical compound N1([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=2C=CC=CC=2)NC(=O)COC=2C(=CC=CC=2C)C)CC=2C=CC=CC=2)CCCNC1=O.N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 OFFWOVJBSQMVPI-RMLGOCCBSA-N 0.000 claims 1
- QNAYBMKLOCPYGJ-UWTATZPHSA-N L-Alanine Natural products C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 claims 1
- FFEARJCKVFRZRR-UHFFFAOYSA-N L-Methionine Natural products CSCCC(N)C(O)=O FFEARJCKVFRZRR-UHFFFAOYSA-N 0.000 claims 1
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 1
- QWCKQJZIFLGMSD-VKHMYHEASA-N L-alpha-aminobutyric acid Chemical group CC[C@H](N)C(O)=O QWCKQJZIFLGMSD-VKHMYHEASA-N 0.000 claims 1
- 229930195722 L-methionine Natural products 0.000 claims 1
- 125000000393 L-methionino group Chemical group [H]OC(=O)[C@@]([H])(N([H])[*])C([H])([H])C(SC([H])([H])[H])([H])[H] 0.000 claims 1
- 229930182821 L-proline Natural products 0.000 claims 1
- 102000007999 Nuclear Proteins Human genes 0.000 claims 1
- 108010089610 Nuclear Proteins Proteins 0.000 claims 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 1
- NCDNCNXCDXHOMX-UHFFFAOYSA-N Ritonavir Natural products C=1C=CC=CC=1CC(NC(=O)OCC=1SC=NC=1)C(O)CC(CC=1C=CC=CC=1)NC(=O)C(C(C)C)NC(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-UHFFFAOYSA-N 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
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 1
- XNKLLVCARDGLGL-JGVFFNPUSA-N Stavudine Chemical compound O=C1NC(=O)C(C)=CN1[C@H]1C=C[C@@H](CO)O1 XNKLLVCARDGLGL-JGVFFNPUSA-N 0.000 claims 1
- SUJUHGSWHZTSEU-UHFFFAOYSA-N Tipranavir Natural products C1C(O)=C(C(CC)C=2C=C(NS(=O)(=O)C=3N=CC(=CC=3)C(F)(F)F)C=CC=2)C(=O)OC1(CCC)CCC1=CC=CC=C1 SUJUHGSWHZTSEU-UHFFFAOYSA-N 0.000 claims 1
- WREGKURFCTUGRC-POYBYMJQSA-N Zalcitabine Chemical compound O=C1N=C(N)C=CN1[C@@H]1O[C@H](CO)CC1 WREGKURFCTUGRC-POYBYMJQSA-N 0.000 claims 1
- QAGMBTAACMQRSS-MTULOOOASA-N [(2r,3s)-3,5-diacetyloxyoxolan-2-yl]methyl acetate Chemical compound CC(=O)OC[C@H]1OC(OC(C)=O)C[C@@H]1OC(C)=O QAGMBTAACMQRSS-MTULOOOASA-N 0.000 claims 1
- 229950001146 adargileukin alfa Drugs 0.000 claims 1
- WOZSCQDILHKSGG-UHFFFAOYSA-N adefovir depivoxil Chemical compound N1=CN=C2N(CCOCP(=O)(OCOC(=O)C(C)(C)C)OCOC(=O)C(C)(C)C)C=NC2=C1N WOZSCQDILHKSGG-UHFFFAOYSA-N 0.000 claims 1
- 229960003205 adefovir dipivoxil Drugs 0.000 claims 1
- 229960003767 alanine Drugs 0.000 claims 1
- 229960005310 aldesleukin Drugs 0.000 claims 1
- 108700025316 aldesleukin Proteins 0.000 claims 1
- 229940024606 amino acid Drugs 0.000 claims 1
- 229950007215 ancriviroc Drugs 0.000 claims 1
- 229960003796 atazanavir sulfate Drugs 0.000 claims 1
- XOZUGNYVDXMRKW-AATRIKPKSA-N azodicarbonamide Chemical compound NC(=O)\N=N\C(N)=O XOZUGNYVDXMRKW-AATRIKPKSA-N 0.000 claims 1
- 235000019399 azodicarbonamide Nutrition 0.000 claims 1
- 229960004853 betadex Drugs 0.000 claims 1
- PMDQGYMGQKTCSX-HQROKSDRSA-L calcium;[(2r,3s)-1-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-[[(3s)-oxolan-3-yl]oxycarbonylamino]-4-phenylbutan-2-yl] phosphate Chemical compound [Ca+2].C([C@@H]([C@H](OP([O-])([O-])=O)CN(CC(C)C)S(=O)(=O)C=1C=CC(N)=CC=1)NC(=O)O[C@@H]1COCC1)C1=CC=CC=C1 PMDQGYMGQKTCSX-HQROKSDRSA-L 0.000 claims 1
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims 1
- HJZLEGIHUQOJBA-UHFFFAOYSA-N cyclohexane propionic acid Chemical compound OC(=O)CCC1CCCCC1 HJZLEGIHUQOJBA-UHFFFAOYSA-N 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 229950006497 dapivirine Drugs 0.000 claims 1
- 229960005107 darunavir Drugs 0.000 claims 1
- CJBJHOAVZSMMDJ-HEXNFIEUSA-N darunavir Chemical compound C([C@@H]([C@H](O)CN(CC(C)C)S(=O)(=O)C=1C=CC(N)=CC=1)NC(=O)O[C@@H]1[C@@H]2CCO[C@@H]2OC1)C1=CC=CC=C1 CJBJHOAVZSMMDJ-HEXNFIEUSA-N 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
- 229950006528 elvucitabine Drugs 0.000 claims 1
- 229940001018 emtriva Drugs 0.000 claims 1
- PEASPLKKXBYDKL-FXEVSJAOSA-N enfuvirtide Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(C)=O)[C@@H](C)O)[C@@H](C)CC)C1=CN=CN1 PEASPLKKXBYDKL-FXEVSJAOSA-N 0.000 claims 1
- 229960002062 enfuvirtide Drugs 0.000 claims 1
- 125000004494 ethyl ester group Chemical group 0.000 claims 1
- 229960002049 etravirine Drugs 0.000 claims 1
- PYGWGZALEOIKDF-UHFFFAOYSA-N etravirine Chemical compound CC1=CC(C#N)=CC(C)=C1OC1=NC(NC=2C=CC(=CC=2)C#N)=NC(N)=C1Br PYGWGZALEOIKDF-UHFFFAOYSA-N 0.000 claims 1
- 229960002933 fosamprenavir calcium Drugs 0.000 claims 1
- 229960000848 foscarnet sodium Drugs 0.000 claims 1
- DMEGYFMYUHOHGS-UHFFFAOYSA-N heptamethylene Natural products C1CCCCCC1 DMEGYFMYUHOHGS-UHFFFAOYSA-N 0.000 claims 1
- 229960004243 indinavir sulfate Drugs 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 229960004525 lopinavir Drugs 0.000 claims 1
- 229940113983 lopinavir / ritonavir Drugs 0.000 claims 1
- 229960004710 maraviroc Drugs 0.000 claims 1
- GSNHKUDZZFZSJB-QYOOZWMWSA-N maraviroc Chemical compound CC(C)C1=NN=C(C)N1[C@@H]1C[C@H](N2CC[C@H](NC(=O)C3CCC(F)(F)CC3)C=3C=CC=CC=3)CC[C@H]2C1 GSNHKUDZZFZSJB-QYOOZWMWSA-N 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 229960004452 methionine Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 150000004702 methyl esters Chemical class 0.000 claims 1
- BDJAEZRIGNCQBZ-UHFFFAOYSA-N methyl-cyclobutane Natural products CC1CCC1 BDJAEZRIGNCQBZ-UHFFFAOYSA-N 0.000 claims 1
- AARXZCZYLAFQQU-UHFFFAOYSA-N motexafin gadolinium Chemical compound [Gd].CC(O)=O.CC(O)=O.C1=C([N-]2)C(CC)=C(CC)C2=CC(C(=C2C)CCCO)=NC2=CN=C2C=C(OCCOCCOCCOC)C(OCCOCCOCCOC)=CC2=NC=C2C(C)=C(CCCO)C1=N2 AARXZCZYLAFQQU-UHFFFAOYSA-N 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 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
- 229960000689 nevirapine Drugs 0.000 claims 1
- RGSFGYAAUTVSQA-UHFFFAOYSA-N pentamethylene Natural products C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229940124531 pharmaceutical excipient Drugs 0.000 claims 1
- 239000011574 phosphorus Substances 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 229960002429 proline Drugs 0.000 claims 1
- 229960002814 rilpivirine Drugs 0.000 claims 1
- YIBOMRUWOWDFLG-ONEGZZNKSA-N rilpivirine Chemical compound CC1=CC(\C=C\C#N)=CC(C)=C1NC1=CC=NC(NC=2C=CC(=CC=2)C#N)=N1 YIBOMRUWOWDFLG-ONEGZZNKSA-N 0.000 claims 1
- 229960000311 ritonavir Drugs 0.000 claims 1
- NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229960003542 saquinavir mesylate Drugs 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229940054565 sustiva Drugs 0.000 claims 1
- 229960001355 tenofovir disoproxil Drugs 0.000 claims 1
- BCQMBFHBDZVHKU-UHFFFAOYSA-N terbumeton Chemical compound CCNC1=NC(NC(C)(C)C)=NC(OC)=N1 BCQMBFHBDZVHKU-UHFFFAOYSA-N 0.000 claims 1
- 230000002992 thymic effect Effects 0.000 claims 1
- 229960000838 tipranavir Drugs 0.000 claims 1
- SUJUHGSWHZTSEU-FYBSXPHGSA-N tipranavir Chemical compound C([C@@]1(CCC)OC(=O)C([C@H](CC)C=2C=C(NS(=O)(=O)C=3N=CC(=CC=3)C(F)(F)F)C=CC=2)=C(O)C1)CC1=CC=CC=C1 SUJUHGSWHZTSEU-FYBSXPHGSA-N 0.000 claims 1
- DFHAXXVZCFXGOQ-UHFFFAOYSA-K trisodium phosphonoformate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)P([O-])([O-])=O DFHAXXVZCFXGOQ-UHFFFAOYSA-K 0.000 claims 1
- 229940008349 truvada Drugs 0.000 claims 1
- 241001430294 unidentified retrovirus Species 0.000 claims 1
- 229960002555 zidovudine Drugs 0.000 claims 1
- HBOMLICNUCNMMY-XLPZGREQSA-N zidovudine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](N=[N+]=[N-])C1 HBOMLICNUCNMMY-XLPZGREQSA-N 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 System
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se)
-
- 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
- A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
-
- 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
- C07H19/16—Purine 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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- 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
- A61K31/7076—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 containing purines, e.g. adenosine, adenylic acid
-
- 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
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se)
- C07F9/40—Esters thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids, i.e. RP(=X)(XH)2 (X = S, Se)
- C07F9/44—Amides thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
-
- 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
-
- 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
- C07H19/16—Purine radicals
- C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
Abstract
Spoj sa slijedećom formulomnaznačen time, što se R1 i R2 biraju iz slijedeće tablice:
Claims (12)
1. Spoj sa slijedećom formulom
[image]
naznačen time, što se R1 i R2 biraju iz slijedeće tablice:
[image]
[image]
gdje Ala predstavlja L-alanin, Phe predstavlja L-fenilalanin, Met predstavlja L-metionin, ABA predstavlja (S)-2-aminobuternu kiselinu, Pro predstavlja L-prolin, CHA predstavlja 2-amino-3-(S)cikloheksil-propionsku kiselinu, Gly predstavlja glicin;
R1 ili R2 aminokiselinske karboksilne grupe esterificirane su kako je navedeno u koloni estera, gdje
cPent je ciklopentan ester; Et je etil ester, 3-furan-4H je (R) tetrahidrofuran-3-il ester; cBut je ciklobutan ester; sBu(S) je (S) secButil ester; sBu(R) je (R) secButil ester; iBu je izobutil ester; CH2cPr je metilciklopropan ester, nBu je n-butil ester; CH2cBu je metilciklobutan ester; 3-pent je 3-pentil ester; nPent je nPentil ester; iPr je izopropil ester, nPr je nPropil ester; alil je alil ester; Me je metil ester; Bn je benzil ester; i
gdje A ili B u zagradi označavaju jedan stereoizomer na fosforu, gdje je manje polarni izomer označenim kao (A), a polarniji kao (B),
ili njegova farmakološki prihvatljiva sol ili solvat.
2. Spoj iz zahtjeva 1, naznačen time, što ima formulu XX:
[image]
3. Spoj iz zahtjeva 1, naznačen time, što ima formulu XXX:
[image]
4. Farmaceutska smjesa, naznačena time, što sadrži farmaceutski ekscipijent i protiv virusa efikasnu količinu spoja iz bilo kojeg od zahtjeva 1 do 3.
5. Farmaceutska smjesa iz zahtjeva 4, naznačena time, što dalje sadrži drugi aktivni sastojak.
6. Kombinacija, naznačena time, što sadrži spoj iz bilo kojeg od zahtjeva 1 do 3 i jedan ili više sastojaka sa antivirusnom aktivnošću.
7. Kombinacija iz zahtjeva 6, naznačena time, što se jedan ili više sastojaka sa antivirusnom aktivnošću biraju iz grupe koja sadrži nikavir, aldesleukin, gadolinijev teksafirin. enfuvirtid, emapimod-hidroklorid, elvucitabin, cijanovirin N, azodikarbonamid, tenofovir dizoproksil fumarat, antikort, reverset, sampidin, imunitin, inaktivin, racivir, celulosa-sulfat, dapivirin, lamivudin/zidovudin/abakavir sulfat, etravirin, adargileukin alfa, gliminoks. natrijev-dodecil sulfat, ankrivirok, O-(2-hidroksipropil)-beta-ciklodekstrin, darunavir, maravirok, dermavir, sulfonizirani esperidin, V-I imunitor, rilpivirin, metabolit X, MIV-150/karagard, tenofovir dizoproksil fumarat/emtricitabin/efavirenz, timusni nukleusni protein, GS-9137 (elvitegravir) i celuloza-acetat-ftalat.
8. Kombinacija iz zahtjeva 6, naznačena time, što se jedan od sastojaka sa antivirusnom aktivnošću bira iz grupe koja sadrži:
abakavir sulfat
abakavir sulfat/lamivudin
adefovir dipivoksil
amprenavir
atazanavir sulfat
delavirdin mezilat
dideoksicitidin; zalcitabin
dideoksiinozin; didanozin
efavirenz
emtricitabin
fosamprenavir kalcij
foskarnet natrij
indinavir sulfat
lamivudin
lamivudin/zidovudin
lopinavir
lopinavir/ritonavir
nelfinavir mezilat
nevirapin
ritonavir
sakvinavir mezilat
stavudin
tenofovir dizoproksil fumarat/emtricitabin
tipranavir
zidovudin.
9. Kombinacija iz zahtjeva 6, naznačena time, što se jedan od aktivnih sastojaka bira iz grupe koja sadrži antivirusne spojeve: truvada, viread, emtriva, d4T, sustiva ili amprenavir.
10. Farmaceutska smjesa iz zahtjeva 4 ili 5 ili kombinacija iz bilo kojeg od zahtjeva 6 do 9, naznačena time, što se koristi u medicinskoj terapiji.
11. Spoj iz bilo kojeg od zahtjeva 1 do 3 ili kombinacija iz bilo kojeg od zahtjeva 6 do 9, naznačeni time, što se koriste u medicinskoj terapiji, u liječenju od retrovirusa ili od hepadna virusa.
12. Spoj iz bilo kojeg od zahtjeva 1 do 3 ili kombinacija iz bilo kojeg od zahtjeva 6 do 9, naznačeni time, što se upotrebljavaju u metodi liječenja od HIV-a ili HIV-u pridruženih poremećaja.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US59181104P | 2004-07-27 | 2004-07-27 | |
PCT/US2005/026504 WO2006110157A2 (en) | 2004-07-27 | 2005-07-26 | Nucleoside phosphonate conjugates as anti hiv agents |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20110527T1 true HRP20110527T1 (hr) | 2011-08-31 |
Family
ID=35502668
Family Applications (4)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20070079A HRP20070079A2 (hr) | 2004-07-27 | 2007-02-27 | Fosfonatni analozi spojeva koji inhibiraju hiv |
HR20070078A HRP20070078A2 (hr) | 2004-07-27 | 2007-02-27 | Fosfonatni analozi spojeva koji inhibiraju hiv |
HR20110527T HRP20110527T1 (hr) | 2004-07-27 | 2011-07-13 | Nukleozid-fosfonatni konjugati kao sredstva protiv hiv-a |
HRP20190712TT HRP20190712T1 (hr) | 2004-07-27 | 2019-04-16 | Fosfonatni analozi spojeva hiv inhibitora |
Family Applications Before (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20070079A HRP20070079A2 (hr) | 2004-07-27 | 2007-02-27 | Fosfonatni analozi spojeva koji inhibiraju hiv |
HR20070078A HRP20070078A2 (hr) | 2004-07-27 | 2007-02-27 | Fosfonatni analozi spojeva koji inhibiraju hiv |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20190712TT HRP20190712T1 (hr) | 2004-07-27 | 2019-04-16 | Fosfonatni analozi spojeva hiv inhibitora |
Country Status (36)
Country | Link |
---|---|
US (11) | US8318701B2 (hr) |
EP (4) | EP3539546A1 (hr) |
JP (3) | JP2008508291A (hr) |
KR (2) | KR101233824B1 (hr) |
CN (4) | CN101027062A (hr) |
AP (2) | AP2412A (hr) |
AR (1) | AR051922A1 (hr) |
AT (2) | ATE505196T1 (hr) |
AU (2) | AU2005330489B2 (hr) |
BR (2) | BRPI0512690A (hr) |
CA (2) | CA2574514A1 (hr) |
CY (2) | CY1111709T1 (hr) |
DE (2) | DE602005027466D1 (hr) |
DK (2) | DK2258376T3 (hr) |
EA (2) | EA019419B1 (hr) |
ES (3) | ES2363160T3 (hr) |
HK (2) | HK1103648A1 (hr) |
HR (4) | HRP20070079A2 (hr) |
HU (1) | HUE043207T2 (hr) |
IL (2) | IL180758A (hr) |
IS (2) | IS2840B (hr) |
LT (1) | LT2258376T (hr) |
ME (2) | ME01945B (hr) |
MX (2) | MX2007001053A (hr) |
NO (5) | NO339222B1 (hr) |
NZ (2) | NZ553405A (hr) |
PL (4) | PL2258376T3 (hr) |
PT (2) | PT1778251E (hr) |
RS (2) | RS51799B (hr) |
SG (1) | SG155164A1 (hr) |
SI (2) | SI2258376T1 (hr) |
TR (1) | TR201906416T4 (hr) |
TW (1) | TWI362934B (hr) |
UA (2) | UA88313C2 (hr) |
WO (2) | WO2006110157A2 (hr) |
ZA (2) | ZA200701466B (hr) |
Families Citing this family (142)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MY164523A (en) | 2000-05-23 | 2017-12-29 | Univ Degli Studi Cagliari | Methods and compositions for treating hepatitis c virus |
EP1576138B1 (en) | 2002-11-15 | 2017-02-01 | Idenix Pharmaceuticals LLC. | 2'-methyl nucleosides in combination with interferon and flaviviridae mutation |
WO2004096286A2 (en) | 2003-04-25 | 2004-11-11 | Gilead Sciences, Inc. | Antiviral phosphonate analogs |
DK2258376T3 (en) * | 2004-07-27 | 2019-04-15 | Gilead Sciences Inc | Phosphonate analogues of HIV inhibitor compounds |
CA2616314A1 (en) * | 2005-07-27 | 2007-02-01 | Gilead Sciences, Inc. | Antiviral phosphonate conjugates for inhibition of hiv |
US8895531B2 (en) | 2006-03-23 | 2014-11-25 | Rfs Pharma Llc | 2′-fluoronucleoside phosphonates as antiviral agents |
WO2008100447A2 (en) * | 2007-02-09 | 2008-08-21 | Gilead Sciences, Inc. | Nucleoside analogs for antiviral treatment |
WO2008098374A1 (en) * | 2007-02-16 | 2008-08-21 | Affinium Pharmaceuticals, Inc. | Salts, prodrugs and polymorphs of fab i inhibitors |
US7964580B2 (en) | 2007-03-30 | 2011-06-21 | Pharmasset, Inc. | Nucleoside phosphoramidate prodrugs |
US8173621B2 (en) | 2008-06-11 | 2012-05-08 | Gilead Pharmasset Llc | Nucleoside cyclicphosphates |
EP2307435B1 (en) * | 2008-07-08 | 2012-06-13 | Gilead Sciences, Inc. | Salts of hiv inhibitor compounds |
CN102325783A (zh) | 2008-12-23 | 2012-01-18 | 法莫赛特股份有限公司 | 嘌呤核苷的合成 |
TWI576352B (zh) | 2009-05-20 | 2017-04-01 | 基利法瑪席特有限責任公司 | 核苷磷醯胺 |
US8618076B2 (en) | 2009-05-20 | 2013-12-31 | Gilead Pharmasset Llc | Nucleoside phosphoramidates |
SG184323A1 (en) | 2010-03-31 | 2012-11-29 | Gilead Pharmasett Llc | Stereoselective synthesis of phosphorus containing actives |
US8563530B2 (en) | 2010-03-31 | 2013-10-22 | Gilead Pharmassel LLC | Purine nucleoside phosphoramidate |
CA2818853A1 (en) | 2010-11-30 | 2012-06-07 | Gilead Pharmasset Llc | 2'-spirocyclo-nucleosides for use in therapy of hcv or dengue virus |
CA2843324A1 (en) | 2011-03-31 | 2012-11-15 | Idenix Pharmaceuticals, Inc. | Compounds and pharmaceutical compositions for the treatment of viral infections |
PT2710019T (pt) | 2011-05-19 | 2017-07-21 | Gilead Sciences Inc | Processos e intermediários para preparar agentes anti-hiv |
JP6205354B2 (ja) | 2011-07-06 | 2017-09-27 | ギリアード サイエンシーズ, インコーポレイテッド | Hivの処置のための化合物 |
EP2567961A1 (en) | 2011-09-08 | 2013-03-13 | Straitmark Holding AG | Method for the manufacture of compounds containing an alpha-oxyphosphorus group by using an activator |
AR088441A1 (es) | 2011-09-12 | 2014-06-11 | Idenix Pharmaceuticals Inc | Compuestos de carboniloximetilfosforamidato sustituido y composiciones farmaceuticas para el tratamiento de infecciones virales |
MX354958B (es) | 2011-09-16 | 2018-03-27 | Gilead Pharmasset Llc | Metodos para el tratamiento de vhc. |
EP3333173B1 (en) * | 2011-10-07 | 2019-06-26 | Gilead Sciences, Inc. | Methods for preparing anti-viral nucleotide analogs |
AR089650A1 (es) | 2011-10-14 | 2014-09-10 | Idenix Pharmaceuticals Inc | Fosfatos 3,5-ciclicos sustituidos de compuestos de nucleotido de purina y composiciones farmaceuticas para el tratamiento de infecciones virales |
US8889159B2 (en) | 2011-11-29 | 2014-11-18 | Gilead Pharmasset Llc | Compositions and methods for treating hepatitis C virus |
WO2013082476A1 (en) | 2011-11-30 | 2013-06-06 | Emory University | Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections |
PE20150132A1 (es) | 2012-05-22 | 2015-02-14 | Idenix Pharmaceuticals Inc | Compuestos d-aminoacidos para enfermedad hepatica |
WO2013177188A1 (en) | 2012-05-22 | 2013-11-28 | Idenix Pharmaceuticals, Inc. | 3',5'-cyclic phosphoramidate prodrugs for hcv infection |
US9296778B2 (en) | 2012-05-22 | 2016-03-29 | Idenix Pharmaceuticals, Inc. | 3′,5′-cyclic phosphate prodrugs for HCV infection |
CA2871547C (en) | 2012-05-25 | 2021-05-25 | Janssen R&D Ireland | Uracyl spirooxetane nucleosides |
WO2014052638A1 (en) | 2012-09-27 | 2014-04-03 | Idenix Pharmaceuticals, Inc. | Esters and malonates of sate prodrugs |
AP2015008384A0 (en) | 2012-10-08 | 2015-04-30 | Univ Montpellier Ct Nat De La Rech Scient | 2'-Chloro nucleoside analogs for hcv infection |
WO2014066239A1 (en) | 2012-10-22 | 2014-05-01 | Idenix Pharmaceuticals, Inc. | 2',4'-bridged nucleosides for hcv infection |
US9211300B2 (en) | 2012-12-19 | 2015-12-15 | Idenix Pharmaceuticals Llc | 4′-fluoro nucleosides for the treatment of HCV |
US20140187501A1 (en) * | 2012-12-28 | 2014-07-03 | Blend Therapeutics, Inc. | Targeted Conjugates Encapsulated in Particles and Formulations Thereof |
PL2950786T3 (pl) | 2013-01-31 | 2020-05-18 | Gilead Pharmasset Llc | Formulacja skojarzona dwóch związków przeciwwirusowych |
US9309275B2 (en) | 2013-03-04 | 2016-04-12 | Idenix Pharmaceuticals Llc | 3′-deoxy nucleosides for the treatment of HCV |
WO2014137930A1 (en) | 2013-03-04 | 2014-09-12 | Idenix Pharmaceuticals, Inc. | Thiophosphate nucleosides for the treatment of hcv |
WO2014160484A1 (en) | 2013-03-13 | 2014-10-02 | Idenix Pharmaceuticals, Inc. | Amino acid phosphoramidate pronucleotides of 2'-cyano, azido and amino nucleosides for the treatment of hcv |
WO2014165542A1 (en) | 2013-04-01 | 2014-10-09 | Idenix Pharmaceuticals, Inc. | 2',4'-fluoro nucleosides for the treatment of hcv |
EP3004130B1 (en) | 2013-06-05 | 2019-08-07 | Idenix Pharmaceuticals LLC. | 1',4'-thio nucleosides for the treatment of hcv |
WO2015017713A1 (en) | 2013-08-01 | 2015-02-05 | Idenix Pharmaceuticals, Inc. | D-amino acid phosphoramidate pronucleotides of halogeno pyrimidine compounds for liver disease |
PL3038601T3 (pl) | 2013-08-27 | 2020-08-24 | Gilead Pharmasset Llc | Formulacja złożona dwóch związków przeciwwirusowych |
WO2015161137A1 (en) | 2014-04-16 | 2015-10-22 | Idenix Pharmaceuticals, Inc. | 3'-substituted methyl or alkynyl nucleosides for the treatment of hcv |
EP3273028B1 (en) * | 2014-05-28 | 2019-07-10 | Volvo Truck Corporation | A turbocompound unit |
TW201613936A (en) | 2014-06-20 | 2016-04-16 | Gilead Sciences Inc | Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide |
NO2717902T3 (hr) | 2014-06-20 | 2018-06-23 | ||
WO2016030863A1 (en) | 2014-08-29 | 2016-03-03 | Glaxosmithkline Intellectual Property Development Limited | Compounds and methods for treating viral infections |
WO2016036759A1 (en) | 2014-09-04 | 2016-03-10 | Gilead Sciences, Inc. | Methods of treating or preventing hiv in patients using a combination of tenofovir alafenamide and dolutegravir |
TWI738321B (zh) | 2014-12-23 | 2021-09-01 | 美商基利科學股份有限公司 | 多環胺甲醯基吡啶酮化合物及其醫藥用途 |
SG11201705192PA (en) | 2014-12-24 | 2017-07-28 | Gilead Sciences Inc | Fused pyrimidine compounds for the treatment of hiv |
TW202237569A (zh) | 2014-12-24 | 2022-10-01 | 美商基利科學股份有限公司 | 喹唑啉化合物 |
CN107428693B (zh) | 2014-12-24 | 2020-05-29 | 吉利德科学公司 | 用于hiv治疗的异喹啉化合物 |
HRP20211456T1 (hr) | 2014-12-26 | 2021-12-24 | Emory University | Protuvirusni derivati n4-hidroksicitidina |
US9670205B2 (en) | 2015-03-04 | 2017-06-06 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
CA2980362C (en) | 2015-04-02 | 2020-02-25 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
JP2018525412A (ja) | 2015-08-26 | 2018-09-06 | ギリアード サイエンシーズ, インコーポレイテッド | 重水素化トール様受容体調節因子 |
JP2018529714A (ja) | 2015-09-30 | 2018-10-11 | ギリアード サイエンシーズ, インコーポレイテッド | Hivの処置のための化合物および組合せ物 |
CN114848812A (zh) | 2015-12-15 | 2022-08-05 | 吉利德科学公司 | 人免疫缺陷病毒中和抗体 |
TWI740910B (zh) * | 2016-03-09 | 2021-10-01 | 美商艾洛斯生物製藥公司 | 非環抗病毒劑 |
EP3454856A4 (en) | 2016-05-10 | 2019-12-25 | C4 Therapeutics, Inc. | HETEROCYCLIC DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
CN109562113A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的螺环降解决定子体 |
EP3347352B1 (en) | 2016-08-19 | 2019-07-03 | Gilead Sciences, Inc. | Therapeutic compounds useful for the prophylactic or therapeutic treatment of an hiv virus infection |
WO2018042331A1 (en) | 2016-08-31 | 2018-03-08 | Glaxosmithkline Intellectual Property (No.2) Limited | Combinations and uses and treatments thereof |
WO2018042332A1 (en) | 2016-08-31 | 2018-03-08 | Glaxosmithkline Intellectual Property (No.2) Limited | Combinations and uses and treatments thereof |
WO2018045150A1 (en) | 2016-09-02 | 2018-03-08 | Gilead Sciences, Inc. | 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators |
WO2018045144A1 (en) | 2016-09-02 | 2018-03-08 | Gilead Sciences, Inc. | Toll like receptor modulator compounds |
WO2018051250A1 (en) | 2016-09-14 | 2018-03-22 | Viiv Healthcare Company | Combination comprising tenofovir alafenamide, bictegravir and 3tc |
EP3518935A1 (en) * | 2016-09-27 | 2019-08-07 | Gilead Sciences, Inc. | Therapeutic compositions for treatment of human immunodeficiency virus |
WO2018064080A1 (en) | 2016-09-28 | 2018-04-05 | Gilead Sciences, Inc. | Benzothiazol-6-yl acetic acid derivatives and their use for treating hiv infection |
WO2018081292A1 (en) | 2016-10-27 | 2018-05-03 | Gilead Sciences, Inc. | Crystalline forms of darunavir free base, hydrate, solvates and salts |
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 |
JOP20180009A1 (ar) | 2017-02-06 | 2019-01-30 | Gilead Sciences Inc | مركبات مثبط فيروس hiv |
RU2647576C1 (ru) * | 2017-02-28 | 2018-03-16 | Васильевич Иващенко Александр | Циклобутил (S)-2-[[[(R)-2-(6-аминопурин-9-ил)-1-метил-этокси]метил-фенокси-фосфорил]амино]-пропаноаты, способ их получения и применения |
WO2018237148A1 (en) | 2017-06-21 | 2018-12-27 | Gilead Sciences, Inc. | MULTISPECIFIC ANTIBODIES TARGETING HIV GP120 AND CD3 |
ES2892402T3 (es) | 2017-08-01 | 2022-02-04 | Gilead Sciences Inc | Formas cristalinas de ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-il)-4-fluoro-2,5-dihidrofuran-2-il)oxi)metil)(fenoxi)fosforil)-L-alaninato de etilo para tratar infecciones virales |
TW202024061A (zh) | 2017-08-17 | 2020-07-01 | 美商基利科學股份有限公司 | Hiv蛋白質膜抑制劑之固體形式 |
AR112412A1 (es) | 2017-08-17 | 2019-10-23 | Gilead Sciences Inc | Formas de sal de colina de un inhibidor de la cápside del vih |
JOP20180092A1 (ar) | 2017-10-13 | 2019-04-13 | Gilead Sciences Inc | مثبطات hiv بروتياز |
EP3700573A1 (en) | 2017-10-24 | 2020-09-02 | Gilead Sciences, Inc. | Methods of treating patients co-infected with a virus and tuberculosis |
US11331331B2 (en) | 2017-12-07 | 2022-05-17 | Emory University | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
KR102492187B1 (ko) | 2017-12-20 | 2023-01-27 | 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. | Sting 어댑터 단백질을 활성화하는 포스포네이트 결합을 가진 3'3' 사이클릭 다이뉴클레오티드 |
AU2018392212B9 (en) | 2017-12-20 | 2021-03-18 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein |
US10836746B2 (en) | 2018-02-15 | 2020-11-17 | Gilead Sciences, Inc. | Therapeutic compounds |
EP4253366A3 (en) | 2018-02-16 | 2023-11-29 | Gilead Sciences, Inc. | Methods and intermediates for preparing a therapeutic compound useful in the treatment of retroviridae viral infection |
KR20200140867A (ko) | 2018-04-06 | 2020-12-16 | 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. | 3'3'-사이클릭 다이뉴클레오티드 |
TWI818007B (zh) | 2018-04-06 | 2023-10-11 | 捷克科學院有機化學與生物化學研究所 | 2'3'-環二核苷酸 |
TW202005654A (zh) | 2018-04-06 | 2020-02-01 | 捷克科學院有機化學與生物化學研究所 | 2,2,─環二核苷酸 |
US20190359645A1 (en) | 2018-05-03 | 2019-11-28 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotides comprising carbocyclic nucleotide |
US11168130B2 (en) | 2018-07-03 | 2021-11-09 | Gilead Sciences, Inc. | Antibodies that target HIV GP120 and methods of use |
CN112423750A (zh) | 2018-07-16 | 2021-02-26 | 吉利德科学公司 | 用于治疗hiv的衣壳抑制剂 |
TWI766172B (zh) | 2018-07-30 | 2022-06-01 | 美商基利科學股份有限公司 | 抗hiv化合物 |
WO2020072656A1 (en) | 2018-10-03 | 2020-04-09 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
MX2021005047A (es) | 2018-10-31 | 2021-09-08 | Gilead Sciences Inc | Compuestos de 6-azabenzimidazol sustituidos como inhibidores de hpk1. |
WO2020092528A1 (en) | 2018-10-31 | 2020-05-07 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity |
WO2020176510A1 (en) | 2019-02-25 | 2020-09-03 | Gilead Sciences, Inc. | Protein kinase c agonists |
WO2020176505A1 (en) | 2019-02-25 | 2020-09-03 | Gilead Sciences, Inc. | Protein kinase c agonists |
CN113543851A (zh) | 2019-03-07 | 2021-10-22 | 捷克共和国有机化学与生物化学研究所 | 2’3’-环二核苷酸及其前药 |
EP3935066A1 (en) | 2019-03-07 | 2022-01-12 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 3'3'-cyclic dinucleotides and prodrugs thereof |
US11766447B2 (en) | 2019-03-07 | 2023-09-26 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3′3′-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator |
US11084832B2 (en) | 2019-03-22 | 2021-08-10 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use |
TW202210480A (zh) | 2019-04-17 | 2022-03-16 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
TWI751517B (zh) | 2019-04-17 | 2022-01-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
WO2020214647A1 (en) | 2019-04-17 | 2020-10-22 | Gilead Sciences, Inc. | Solid forms of an hiv protease inhibitor |
TW202104210A (zh) | 2019-04-17 | 2021-02-01 | 美商基利科學股份有限公司 | Hiv蛋白酶抑制劑 |
TW202231277A (zh) | 2019-05-21 | 2022-08-16 | 美商基利科學股份有限公司 | 鑑別對使用gp120 v3聚醣導向之抗體的治療敏感之hiv病患的方法 |
EP3972695A1 (en) | 2019-05-23 | 2022-03-30 | Gilead Sciences, Inc. | Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors |
RU2717101C1 (ru) | 2019-06-03 | 2020-03-18 | Андрей Александрович Иващенко | Анелированные 9-гидрокси-1,8-диоксо-1,3,4,8-тетрагидро-2Н-пиридо[1,2-a]пиразин-7-карбоксамиды - ингибиторы интегразы ВИЧ, способы их получения и применения |
WO2020255038A1 (en) | 2019-06-18 | 2020-12-24 | Janssen Sciences Ireland Unlimited Company | Combination of hepatitis b virus (hbv) vaccines and pyridopyrimidine derivatives |
CN114245807A (zh) | 2019-06-25 | 2022-03-25 | 吉利德科学公司 | Flt3l-fc融合蛋白和使用方法 |
KR20220047277A (ko) | 2019-07-16 | 2022-04-15 | 길리애드 사이언시즈, 인코포레이티드 | Hiv 백신, 및 이의 제조 및 사용 방법 |
US20220257619A1 (en) | 2019-07-18 | 2022-08-18 | Gilead Sciences, Inc. | Long-acting formulations of tenofovir alafenamide |
EP4017476A1 (en) | 2019-08-19 | 2022-06-29 | Gilead Sciences, Inc. | Pharmaceutical formulations of tenofovir alafenamide |
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 |
AU2020412875A1 (en) | 2019-12-24 | 2022-06-23 | Carna Biosciences, Inc. | Diacylglycerol kinase modulating compounds |
CN115151545A (zh) | 2020-02-24 | 2022-10-04 | 吉利德科学公司 | 用于治疗hiv感染的四环化合物 |
JP2023518433A (ja) | 2020-03-20 | 2023-05-01 | ギリアード サイエンシーズ, インコーポレイテッド | 4’-c-置換-2-ハロ-2’-デオキシアデノシンヌクレオシドのプロドラッグ並びにその製造法及び使用法 |
EP4153181A1 (en) | 2020-05-21 | 2023-03-29 | Gilead Sciences, Inc. | Pharmaceutical compositions comprising bictegravir |
EP4172157A1 (en) | 2020-06-25 | 2023-05-03 | Gilead Sciences, Inc. | Capsid inhibitors for the treatment of hiv |
CR20230071A (es) | 2020-08-07 | 2023-04-11 | Gilead Sciences Inc | Profármacos de análogos de nucleótidos de fosfonamida y su uso farmacéutico |
EP4228656A2 (en) * | 2020-08-18 | 2023-08-23 | Yeda Research and Development Co. Ltd | Anti-viral and anti-tumoral compounds |
CN114262348A (zh) * | 2020-09-16 | 2022-04-01 | 上海本仁科技有限公司 | 环状核苷磷酸酯类化合物及其应用 |
AU2021351491A1 (en) | 2020-09-30 | 2023-05-04 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and uses thereof |
TWI815194B (zh) | 2020-10-22 | 2023-09-11 | 美商基利科學股份有限公司 | 介白素2-Fc融合蛋白及使用方法 |
US20220144923A1 (en) | 2020-11-11 | 2022-05-12 | Gilead Sciences, Inc. | METHODS OF IDENTIFYING HIV PATIENTS SENSITIVE TO THERAPY WITH gp120 CD4 BINDING SITE-DIRECTED ANTIBODIES |
LT4196479T (lt) | 2021-01-19 | 2023-12-11 | Gilead Sciences, Inc. | Pakeistieji piridotriazino junginiai ir jų panaudojimo būdai |
WO2022245814A1 (en) * | 2021-05-17 | 2022-11-24 | Rome Therapeutics, Inc. | Methods of treating medical conditions and inhibiting line1 reverse transcriptase using a substituted 4-fluoro-2,5-dihydrofuranyl phosphonic acid or related compound |
TW202313094A (zh) | 2021-05-18 | 2023-04-01 | 美商基利科學股份有限公司 | 使用FLT3L—Fc融合蛋白之方法 |
WO2022271684A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
EP4359411A1 (en) | 2021-06-23 | 2024-05-01 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
CN117396478A (zh) | 2021-06-23 | 2024-01-12 | 吉利德科学公司 | 二酰基甘油激酶调节化合物 |
IL309378A (en) | 2021-06-23 | 2024-02-01 | Gilead Sciences Inc | DIACYLGLYERCOL KINASE MODULATING COMPOUNDS |
TW202337439A (zh) | 2021-12-03 | 2023-10-01 | 美商基利科學股份有限公司 | 用於hiv病毒感染之治療性化合物 |
WO2023102523A1 (en) | 2021-12-03 | 2023-06-08 | Gilead Sciences, Inc. | Therapeutic compounds for hiv virus infection |
US20230203071A1 (en) | 2021-12-03 | 2023-06-29 | Zhimin Du | Therapeutic compounds for hiv virus infection |
TW202400172A (zh) | 2022-04-06 | 2024-01-01 | 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 |
WO2024015741A1 (en) | 2022-07-12 | 2024-01-18 | Gilead Sciences, Inc. | Hiv immunogenic polypeptides and vaccines and uses thereof |
WO2024044477A1 (en) | 2022-08-26 | 2024-02-29 | Gilead Sciences, Inc. | Dosing and scheduling regimen for broadly neutralizing antibodies |
WO2024076915A1 (en) | 2022-10-04 | 2024-04-11 | Gilead Sciences, Inc. | 4'-thionucleoside analogues and their pharmaceutical use |
Family Cites Families (184)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4276351A (en) | 1980-06-30 | 1981-06-30 | E. I. Du Pont De Nemours And Company | Polyvinyl butyral plasticized with tetraethyleneglycol di-2-ethylhexanoate |
US4816570A (en) | 1982-11-30 | 1989-03-28 | The Board Of Regents Of The University Of Texas System | Biologically reversible phosphate and phosphonate protective groups |
US4649041A (en) | 1983-07-20 | 1987-03-10 | Warner-Lambert Company | Magnesium trisilicate suitable for preparation of medicament adsorbates of antinauseants |
DK159431C (da) | 1984-05-10 | 1991-03-18 | Byk Gulden Lomberg Chem Fab | 6-phenyl-3(2h)-pyridazinoner, fremgangsmaade til fremstilling deraf, laegemidler indeholdende disse samt anvendelse af forbindelserne til fremstilling af laegemidler |
US4724232A (en) | 1985-03-16 | 1988-02-09 | Burroughs Wellcome Co. | Treatment of human viral infections |
CS263952B1 (en) | 1985-04-25 | 1989-05-12 | Holy Antonin | Remedy with antiviral effect |
JPH035439Y2 (hr) | 1985-06-04 | 1991-02-12 | ||
AU570853B2 (en) | 1985-08-26 | 1988-03-24 | United States of America, as represented by the Secretary, U.S. Department of Commerce, The | Inhibition of infectivity and cytopathic effect of htlv-111/ lav by purine bases |
US6492352B1 (en) | 1985-10-31 | 2002-12-10 | Astra Lakemedel Aktiebolag | Method for the control and treatment of acquired immunodeficiency syndrome (AIDS) |
US4968788A (en) | 1986-04-04 | 1990-11-06 | Board Of Regents, The University Of Texas System | Biologically reversible phosphate and phosphonate protective gruops |
US5455339A (en) * | 1986-05-01 | 1995-10-03 | University Of Georgia Research Foundation, Inc. | Method for the preparation of 2',3'-dideoxy and 2',3'-dideoxydide-hydro nucleosides |
IE63869B1 (en) | 1986-11-06 | 1995-06-14 | Res Dev Foundation | Aerosols containing liposomes and method for their preparation |
US4978655A (en) | 1986-12-17 | 1990-12-18 | Yale University | Use of 3'-deoxythymidin-2'-ene (3'deoxy-2',3'-didehydrothymidine) in treating patients infected with retroviruses |
FR2611203B1 (fr) | 1987-02-20 | 1989-06-09 | Sturtz Georges | Analogues gem-diphosphoniques d'amethopterine (methotrexate) et de derives deaza-n-10 amethopterine. leur preparation et les compositions pharmaceutiques qui les contiennent |
US5028595A (en) | 1987-09-18 | 1991-07-02 | Hoffmann-La Roche Inc. | Method for preventing AIDS in a subject or treating a subject infected with the AIDS virus |
US5631370A (en) | 1988-01-20 | 1997-05-20 | Regents Of The University Of Minnesota | Optically-active isomers of dideoxycarbocyclic nucleosides |
US5466793A (en) * | 1988-03-01 | 1995-11-14 | Ajinomoto Co., Inc. | Process for preparing 2', 3'- dideoxyinosine |
US5047407A (en) | 1989-02-08 | 1991-09-10 | Iaf Biochem International, Inc. | 2-substituted-5-substituted-1,3-oxathiolanes with antiviral properties |
ZA894534B (en) | 1988-06-20 | 1990-03-28 | Merrell Dow Pharma | Novel neplanocin derivatives |
GB8815265D0 (en) | 1988-06-27 | 1988-08-03 | Wellcome Found | Therapeutic nucleosides |
US5744600A (en) * | 1988-11-14 | 1998-04-28 | Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic | Phosphonomethoxy carbocyclic nucleosides and nucleotides |
CA2001715C (en) | 1988-11-14 | 1999-12-28 | Muzammil M. Mansuri | Carbocyclic nucleosides and nucleotides |
US5202128A (en) | 1989-01-06 | 1993-04-13 | F. H. Faulding & Co. Limited | Sustained release pharmaceutical composition |
US5366972A (en) | 1989-04-20 | 1994-11-22 | Boehringer Ingelheim Pharmaceuticals, Inc. | 5,11-dihydro-6H-dipyrido(3,2-B:2',3'-E)(1,4)diazepines and their use in the prevention or treatment of HIV infection |
CA2479846C (en) * | 1989-05-15 | 2007-07-24 | Institute Of Organic Chemistry And Biochemistry Of The Academy Of Scienc Es Of The Czech Republic | Phosphonomethoxymethylpurine/pyrimidine derivatives |
US5552558A (en) | 1989-05-23 | 1996-09-03 | Abbott Laboratories | Retroviral protease inhibiting compounds |
JP2722673B2 (ja) | 1989-05-31 | 1998-03-04 | 住友化学工業株式会社 | 光学活性なアシルビフェニル誘導体の製造法 |
GB8927913D0 (en) | 1989-12-11 | 1990-02-14 | Hoffmann La Roche | Amino acid derivatives |
GB8927915D0 (en) | 1989-12-11 | 1990-02-14 | Hoffmann La Roche | Novel alcohols |
US5563142A (en) | 1989-12-28 | 1996-10-08 | The Upjohn Company | Diaromatic substituted compounds as anti-HIV-1 agents |
US5204466A (en) | 1990-02-01 | 1993-04-20 | Emory University | Method and compositions for the synthesis of bch-189 and related compounds |
US5914331A (en) | 1990-02-01 | 1999-06-22 | Emory University | Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane |
DE4003574A1 (de) | 1990-02-07 | 1991-08-08 | Bayer Ag | Neue dipeptide, verfahren zu ihrer herstellung und ihre verwendung als renininhibitoren in arzneimitteln |
CA2083386C (en) | 1990-06-13 | 1999-02-16 | Arnold Glazier | Phosphorous prodrugs |
DE69116750T2 (de) | 1990-07-04 | 1996-11-14 | Merrell Dow Pharma | 9-Purinyl-Phosphonsäurederivate |
US5177064A (en) | 1990-07-13 | 1993-01-05 | University Of Florida | Targeted drug delivery via phosphonate derivatives |
EP0468119A1 (en) | 1990-07-24 | 1992-01-29 | Merrell Dow Pharmaceuticals Inc. | Novel carbocyclic analogs of certain nucleosides |
US5223618A (en) | 1990-08-13 | 1993-06-29 | Isis Pharmaceuticals, Inc. | 4'-desmethyl nucleoside analog compounds |
DE69129650T2 (de) | 1990-09-14 | 1999-03-25 | Acad Of Science Czech Republic | Wirkstoffvorläufer von Phosphonaten |
US5672697A (en) * | 1991-02-08 | 1997-09-30 | Gilead Sciences, Inc. | Nucleoside 5'-methylene phosphonates |
DE4111730A1 (de) | 1991-04-10 | 1992-10-15 | Knoll Ag | Neue cytarabin-derivate, ihre herstellung und verwendung |
JP2648897B2 (ja) | 1991-07-01 | 1997-09-03 | 塩野義製薬株式会社 | ピリミジン誘導体 |
EP0531597A1 (en) | 1991-09-12 | 1993-03-17 | Merrell Dow Pharmaceuticals Inc. | Novel unsaturated acyclic phosphonate derivatives of purine and pyrimidine |
US5610294A (en) | 1991-10-11 | 1997-03-11 | The Du Pont Merck Pharmaceutical Company | Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors |
US5413999A (en) | 1991-11-08 | 1995-05-09 | Merck & Co., Inc. | HIV protease inhibitors useful for the treatment of AIDS |
DE4138584A1 (de) | 1991-11-23 | 1993-05-27 | Hoechst Ag | Carbocyclische phosphonat-nucleotidanaloge, deren herstellung und verwendung |
GB9126144D0 (en) | 1991-12-10 | 1992-02-12 | British Bio Technology | Compounds |
FR2692265B1 (fr) | 1992-05-25 | 1996-11-08 | Centre Nat Rech Scient | Composes biologiquement actifs de type phosphotriesters. |
US5519021A (en) | 1992-08-07 | 1996-05-21 | Merck & Co., Inc. | Benzoxazinones as inhibitors of HIV reverse transcriptase |
IS2334B (is) | 1992-09-08 | 2008-02-15 | Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) | Aspartyl próteasi hemjari af nýjum flokki súlfonamíða |
US5484926A (en) | 1993-10-07 | 1996-01-16 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
DE4308096A1 (de) | 1993-03-13 | 1994-09-15 | Hoechst Ag | Prodrug-Derivate von Enzyminhibitoren mit Hydroxylgruppen, Verfahren zu deren Herstellung und ihre Verwendung |
US5654286A (en) | 1993-05-12 | 1997-08-05 | Hostetler; Karl Y. | Nucleotides for topical treatment of psoriasis, and methods for using same |
EP0632048B1 (en) | 1993-06-29 | 2001-03-21 | Mitsubishi Chemical Corporation | Phosphonate-nucleotide ester derivatives |
AU7491694A (en) | 1993-07-14 | 1995-02-13 | Ciba-Geigy Ag | Cyclic hydrazine compounds |
US5656745A (en) | 1993-09-17 | 1997-08-12 | Gilead Sciences, Inc. | Nucleotide analogs |
WO1995007920A1 (en) | 1993-09-17 | 1995-03-23 | Gilead Sciences, Inc. | Nucleotide analogs |
US5446137B1 (en) | 1993-12-09 | 1998-10-06 | Behringwerke Ag | Oligonucleotides containing 4'-substituted nucleotides |
US5493030A (en) | 1994-02-18 | 1996-02-20 | Syntex (U.S.A.) Inc. | 5-substituted derivatives of mycophenolic acid |
US5854227A (en) | 1994-03-04 | 1998-12-29 | Hartmann; John F. | Therapeutic derivatives of diphosphonates |
WO1997011092A1 (fr) | 1994-04-07 | 1997-03-27 | Nippon Shinyaku Co., Ltd. | Derives de phosphates de cyclosporine et composition medicinale |
ATE255564T1 (de) | 1994-09-26 | 2003-12-15 | Shionogi & Co | Imidazolderivat |
CA2203570A1 (en) | 1994-11-04 | 1996-05-17 | Lawrence R. Mcgee | Thiepane compounds inhibiting and detecting hiv protease |
US5543523A (en) | 1994-11-15 | 1996-08-06 | Regents Of The University Of Minnesota | Method and intermediates for the synthesis of korupensamines |
ES2097703B1 (es) | 1995-04-12 | 1997-12-01 | Decox S L | Una nueva composicion estimulante de la actividad cerebral basada en alcaloides de nucleo de eburnamenina, y sus metodos de preparacion. |
US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
EP0836604A1 (en) | 1995-06-29 | 1998-04-22 | Novo Nordisk A/S | Novel substituted azabicyclic compounds |
US5750493A (en) | 1995-08-30 | 1998-05-12 | Raymond F. Schinazi | Method to improve the biological and antiviral activity of protease inhibitors |
US5646180A (en) | 1995-12-05 | 1997-07-08 | Vertex Pharmaceuticals Incorporated | Treatment of the CNS effects of HIV |
US5914332A (en) | 1995-12-13 | 1999-06-22 | Abbott Laboratories | Retroviral protease inhibiting compounds |
RU2106353C1 (ru) | 1996-03-19 | 1998-03-10 | Корпорация "С энд Ти Сайенс энд Текнолоджи Инк." | Соли 5'-н-фосфоната 3'- азидо-3'-дезокситимидина, являющиеся специфическими ингибиторами продукции вируса иммунодефицита человека вич-1 и вич-2 |
US5874577A (en) | 1996-04-03 | 1999-02-23 | Medichem Research, Inc. | Method for the preparing 9-12-(Diethoxyphosphonomethoxy)ethyl!adenine and analogues thereof |
US5849911A (en) | 1996-04-22 | 1998-12-15 | Novartis Finance Corporation | Antivirally active heterocyclic azahexane derivatives |
US5795909A (en) | 1996-05-22 | 1998-08-18 | Neuromedica, Inc. | DHA-pharmaceutical agent conjugates of taxanes |
WO1998004569A1 (en) | 1996-07-26 | 1998-02-05 | Gilead Sciences, Inc. | Nucleotide analogs |
EP0919562B1 (en) | 1996-08-13 | 2002-11-06 | Mitsubishi Chemical Corporation | Phosphonate nucleotide compounds |
EP0948341A4 (en) | 1996-09-17 | 2003-05-21 | Supergen Inc | DERIVATIVES OF PHOSPHOLIPIDIC DRUGS |
EP0934325B1 (en) | 1996-10-09 | 2004-07-14 | Pharmasset, Ltd. | Mycophenolic bisphosphonate compounds |
EP0994106B1 (en) | 1996-12-26 | 2004-03-17 | Shionogi & Co., Ltd. | Process for the preparation of carbamoylated imidazole derivatives |
AU1810399A (en) * | 1997-12-10 | 1999-06-28 | Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The | Method for synthesizing |
US6436989B1 (en) | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
US6312662B1 (en) | 1998-03-06 | 2001-11-06 | Metabasis Therapeutics, Inc. | Prodrugs phosphorus-containing compounds |
US6174888B1 (en) | 1998-05-28 | 2001-01-16 | Novartis Ag | 2-amino-7-(1-substituted-2-hydroxyethyl)-3,5-dihydropyrrolo[3,2-D]pyrimidin-4-ones |
AU4125099A (en) | 1998-06-01 | 1999-12-20 | S & T Science And Technology Inc. | Antiviral phosphorus derivatives of 4'-thio-5-ethyl-2'-deoxyuridine |
GB9815567D0 (en) | 1998-07-18 | 1998-09-16 | Glaxo Group Ltd | Antiviral compound |
CO5261510A1 (es) | 1999-02-12 | 2003-03-31 | Vertex Pharma | Inhibidores de aspartil proteasa |
US6761903B2 (en) | 1999-06-30 | 2004-07-13 | Lipocine, Inc. | Clear oil-containing pharmaceutical compositions containing a therapeutic agent |
CN1321999C (zh) | 1999-03-05 | 2007-06-20 | 症变治疗公司 | 新的含磷前药 |
DE19912636A1 (de) | 1999-03-20 | 2000-09-21 | Aventis Cropscience Gmbh | Bicyclische Heterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Herbizide und pharmazeutische Mittel |
US6258831B1 (en) | 1999-03-31 | 2001-07-10 | The Procter & Gamble Company | Viral treatment |
US6608027B1 (en) | 1999-04-06 | 2003-08-19 | Boehringer Ingelheim (Canada) Ltd | Macrocyclic peptides active against the hepatitis C virus |
DE19927689A1 (de) | 1999-06-17 | 2000-12-21 | Gruenenthal Gmbh | Orale Darreichungsformen zur Verabreichung einer fixen Kombination von Tramadol und Diclofenac |
DE60005017T2 (de) | 1999-06-25 | 2004-06-09 | Vertex Pharmaceuticals Inc., Cambridge | Prodrugs von impdh-inhibierenden carbamaten |
US6581606B2 (en) | 1999-07-06 | 2003-06-24 | The Rx Files Corporation | Method, apparatus and system for use in treating patient with a drug having an antineoplastic effect to optimize therapy and prevent an adverse drug response |
WO2001013957A2 (en) | 1999-08-24 | 2001-03-01 | Cellgate, Inc. | Enhancing drug delivery across and into epithelial tissues using oligo arginine moieties |
GB9920872D0 (en) | 1999-09-04 | 1999-11-10 | Glaxo Group Ltd | Benzophenones as inhibitors of reverse transcriptase |
IL131887A0 (en) | 1999-09-14 | 2001-03-19 | Dpharm Ltd | Phospholipid prodrugs of anti-proliferative drugs |
JP4993649B2 (ja) | 1999-12-03 | 2012-08-08 | ザ レジェンツ オブ ザ ユニバーシティー オブ カリフォルニア サン ディエゴ | ホスホネート化合物 |
AU2335801A (en) | 1999-12-22 | 2001-07-03 | Merck Frosst Canada & Co. | Aromatic phosphonates as protein tyrosine phosphatase 1b (ptp-1b) inhibitors |
US6767900B2 (en) | 2000-02-29 | 2004-07-27 | Mitsubishi Pharma Corporation | Phosphonate nucleotide compound |
MY164523A (en) * | 2000-05-23 | 2017-12-29 | Univ Degli Studi Cagliari | Methods and compositions for treating hepatitis c virus |
MXPA02012160A (es) | 2000-06-13 | 2003-04-25 | Shionogi & Co | Composiciones medicinales las cuales contienen derivados de propenona. |
FR2810322B1 (fr) | 2000-06-14 | 2006-11-10 | Pasteur Institut | PRODUCTION COMBINATOIRE D'ANALOGUES DE NUCLEOTIDES ET NUCLEOTIDES (XiTP) |
UA72612C2 (en) | 2000-07-06 | 2005-03-15 | Pyrido[2.3-d]pyrimidine and pyrimido[4.5-d]pyrimidine nucleoside analogues, prodrugs and method for inhibiting growth of neoplastic cells | |
US6617310B2 (en) | 2000-07-19 | 2003-09-09 | Bristol-Myers Squibb Pharma Company | Phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines |
AP1466A (en) | 2000-07-21 | 2005-09-22 | Gilead Sciences Inc | Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same. |
US6420586B1 (en) | 2000-08-15 | 2002-07-16 | University Of Kansas | Amino acid-derived cyclic phosphonamides and methods of synthesizing the same |
DE60124117T8 (de) | 2000-09-08 | 2007-05-31 | Zeria Pharmaceutical Co., Ltd. | Aminothiazol-derivate enthaltende pharmazeutische zusammensetzungen zur behandlung von motorischen störungen des kolons |
RU2188203C2 (ru) | 2000-10-05 | 2002-08-27 | Государственный научный центр вирусологии и биотехнологии "Вектор" | 2',3'-дидегидро-2',3'-дидезокситимидин-5'[(этоксикарбонил)(этил)фосфонат]- ингибитор репродукции вируса иммунодефицита человека |
GB0028429D0 (en) | 2000-11-22 | 2001-01-10 | Astrazeneca Ab | Therapy |
AU2002232660A1 (en) | 2000-12-15 | 2002-06-24 | Pharmasset Ltd. | Antiviral agents for treatment of flaviviridae infections |
NZ526715A (en) | 2000-12-28 | 2005-02-25 | Kissei Pharmaceutical | Glucopyranosyloxypyrazole derivatives and use thereof in medicines |
EP1707571B1 (en) | 2001-01-22 | 2011-09-28 | Merck Sharp & Dohme Corp. | Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase |
EP1377568A1 (en) | 2001-01-31 | 2004-01-07 | Warner-Lambert Company LLC | Method for carbamoylating alcohols |
WO2002064543A2 (en) | 2001-02-12 | 2002-08-22 | Wyeth | Novel succinate salt of o-desmethyl-venlafaxine |
DE60225374T2 (de) | 2001-05-31 | 2009-03-26 | Sumitomo Chemical Co., Ltd. | Verfahren zur Herstellung eines aktivierten Aluminiumoxid-Formkörpers |
GB0114286D0 (en) | 2001-06-12 | 2001-08-01 | Hoffmann La Roche | Nucleoside Derivatives |
ES2571945T3 (es) | 2001-06-20 | 2016-05-27 | Nuevolution As | Moléculas y métodos con plantilla para el uso de tales moléculas |
KR20020097384A (ko) | 2001-06-20 | 2002-12-31 | 미쯔비시 도꾜 세이야꾸 가부시끼가이샤 | 기존의 약제에 내성변이를 가지는 바이러스에 유효한 약제 |
DK1408984T3 (da) | 2001-07-20 | 2009-02-09 | Bioagency Ag | Organofosforforbindelser til aktivering af gamma/delta T celler |
CA2457575C (en) * | 2001-08-17 | 2010-12-21 | Sankyo Agro Company, Limited | 3-phenoxy-4-pyridazinol derivatives and herbicidal composition containing the same |
JP2005508924A (ja) | 2001-08-30 | 2005-04-07 | 三菱ウェルファーマ株式会社 | 抗ウイルス剤 |
ES2258652T3 (es) | 2001-11-29 | 2006-09-01 | Pfizer Products Inc. | Sales de succinato de 5,8,14-triazatetraciclo(10.3.1.02,11.04,9)-hexadeca-2(11),3,5,7,9-pentaeno y composiciones farmaceuticas de los mismos. |
CN1617877A (zh) | 2001-12-07 | 2005-05-18 | 三菱制药株式会社 | 膦酸酯核苷酸类似物在治疗乙肝病毒感染方面的用途 |
UA75482C2 (en) | 2001-12-12 | 2006-04-17 | Pfizer Prod Inc | Salts of e-2-methoxy-n-(3-{4-[3-methyl-4-(6-methylpyridine-3-yloxy)phenylamino]quinozaline -6-yl}alyl)acetamide, a method for the preparation and use thereof for the treatment of cancer |
KR100937162B1 (ko) | 2001-12-21 | 2010-01-15 | 에이자이 아이엔씨. | 알콜 및 페놀의 수용성 포스포노옥시메틸 유도체를제조하는 방법 |
US20030198666A1 (en) | 2002-01-07 | 2003-10-23 | Richat Abbas | Oral insulin therapy |
IL162734A0 (en) | 2002-02-01 | 2005-11-20 | Ariad Gene Therapeutics Inc | Phosphorus-containing compounds & uses thereof |
ATE433961T1 (de) | 2002-02-08 | 2009-07-15 | Conforma Therapeutics Corp | Ansamycine mit verbesserten pharmakologischen und biologischen eigenschaften |
US7927613B2 (en) | 2002-02-15 | 2011-04-19 | University Of South Florida | Pharmaceutical co-crystal compositions |
WO2003080078A1 (en) | 2002-03-18 | 2003-10-02 | Mitsubishi Pharma Corporation | Treatment of pre-core hepatitis b virus mutant infections |
US6958349B2 (en) * | 2002-04-10 | 2005-10-25 | Ortho-Mcneil Pharmaceuticals, Inc. | Heteroaryl alkylamide derivatives useful as bradykinin receptor modulators |
CA2481285A1 (en) | 2002-04-26 | 2003-11-06 | Gilead Sciences, Inc. | Non nucleoside reverse transcriptase inhibitors |
US20050239054A1 (en) | 2002-04-26 | 2005-10-27 | Arimilli Murty N | Method and compositions for identifying anti-HIV therapeutic compounds |
US6872827B2 (en) | 2002-04-26 | 2005-03-29 | Chembridge Research Laboratories, Inc. | Somatostatin analogue compounds |
EP1826205A1 (en) | 2002-09-30 | 2007-08-29 | A/S GEA Farmaceutisk Fabrik | Novel raloxifene succinic acid addition salts and/or solvates thereof, and pharmaceutical compositions comprising these |
US20040157793A1 (en) * | 2002-11-12 | 2004-08-12 | Stuyver Lieven J. | Modified nucleosides as antiviral agents |
MXPA05008736A (es) | 2003-02-19 | 2005-10-05 | Univ Yale | Analogos de nucleosido antivirales y metodos para tratar infecciones virales, especialmente infecciones por vih. |
US7300924B2 (en) | 2003-04-25 | 2007-11-27 | Gilead Sciences, Inc. | Anti-infective phosphonate analogs |
EP1617848A2 (en) * | 2003-04-25 | 2006-01-25 | Gilead Sciences, Inc. | Anti-cancer phosphonate conjugates |
EA200501676A1 (ru) | 2003-04-25 | 2006-04-28 | Джилид Сайэнс, Инк. | Фосфонатсодержащие ингибиторы киназы (варианты), способ их получения, фармацевтическая композиция, лекарственная форма на их основе и способ ингибирования киназы у млекопитающего (варианты) |
US7452901B2 (en) * | 2003-04-25 | 2008-11-18 | Gilead Sciences, Inc. | Anti-cancer phosphonate analogs |
US7470724B2 (en) | 2003-04-25 | 2008-12-30 | Gilead Sciences, Inc. | Phosphonate compounds having immuno-modulatory activity |
WO2005002626A2 (en) | 2003-04-25 | 2005-01-13 | Gilead Sciences, Inc. | Therapeutic phosphonate compounds |
MXPA05011294A (es) | 2003-04-25 | 2006-03-15 | Gilead Sciences Inc | Compuestos de fosfonato anti-inflamatorios. |
CN101410120A (zh) | 2003-04-25 | 2009-04-15 | 吉里德科学公司 | 抗炎的膦酸酯化合物 |
WO2004096287A2 (en) | 2003-04-25 | 2004-11-11 | Gilead Sciences, Inc. | Inosine monophosphate dehydrogenase inhibitory phosphonate compounds |
US7432261B2 (en) | 2003-04-25 | 2008-10-07 | Gilead Sciences, Inc. | Anti-inflammatory phosphonate compounds |
MXPA05011287A (es) * | 2003-04-25 | 2006-01-24 | Gilead Sciences Inc | Analogos de fosfonato anti-cancer. |
WO2004096237A2 (en) | 2003-04-25 | 2004-11-11 | Gilead Sciences, Inc. | Phosphonate analogs for treating metabolic diseases |
MXPA05011289A (es) | 2003-04-25 | 2006-01-24 | Gilead Sciences Inc | Compuestos de fosfato que tienen actividad inmunomoduladora. |
WO2004096286A2 (en) * | 2003-04-25 | 2004-11-11 | Gilead Sciences, Inc. | Antiviral phosphonate analogs |
WO2004096233A2 (en) | 2003-04-25 | 2004-11-11 | Gilead Sciences, Inc. | Nucleoside phosphonate conjugates |
US7407965B2 (en) | 2003-04-25 | 2008-08-05 | Gilead Sciences, Inc. | Phosphonate analogs for treating metabolic diseases |
JP2007502329A (ja) | 2003-05-23 | 2007-02-08 | トランスフォーム・ファーマシューティカルズ・インコーポレイテッド | セルトラリン組成物 |
EP1634882A4 (en) * | 2003-06-16 | 2008-01-09 | Ajinomoto Kk | INOSIN DERIVATIVE AND METHOD FOR THE PRODUCTION THEREOF |
JP2007500727A (ja) * | 2003-07-30 | 2007-01-18 | 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核酸塩基ホスホネートアナログ |
BRPI0413555A (pt) | 2003-08-18 | 2006-10-17 | Lundbeck & Co As H | composto ou sal do mesmo, composição farmacêutica, uso de um composto ou sal, e, método para o tratamento de uma doença, para a fabricação de um composto e para a preparação de composto |
AU2004286238A1 (en) | 2003-10-24 | 2005-05-12 | Gilead Sciences, Inc. | Methods and compositions for identifying therapeutic compounds |
US7432273B2 (en) | 2003-10-24 | 2008-10-07 | Gilead Sciences, Inc. | Phosphonate analogs of antimetabolites |
WO2005044279A1 (en) | 2003-10-24 | 2005-05-19 | Gilead Sciences, Inc. | Purine nucleoside phosphonate conjugates |
CA2548951A1 (en) | 2003-12-22 | 2005-07-14 | Gilead Sciences, Inc. | Kinase inhibitor phosphonate conjugates |
CA2548753A1 (en) * | 2003-12-22 | 2005-07-14 | Gilead Sciences, Inc. | 4-substituted carbovir and abacavir-derivatives as well as related compounds with hiv and hcv antiviral activity |
US20050171126A1 (en) * | 2003-12-26 | 2005-08-04 | Ajinomoto Co., Inc. | Process for the production of purine nucleoside compounds |
US7404949B2 (en) | 2004-03-15 | 2008-07-29 | Unilever Home & Personal Care Usa, Division Of Conopco, Inc. | Methods and compositions useful to prevent in-grown hair arising from shaving |
US20090035315A1 (en) | 2004-06-17 | 2009-02-05 | Stephan Christgau | Method of Improving Treatments in Rheumatic and Arthritic Diseases |
DK2258376T3 (en) * | 2004-07-27 | 2019-04-15 | Gilead Sciences Inc | Phosphonate analogues of HIV inhibitor compounds |
WO2006015262A2 (en) | 2004-07-29 | 2006-02-09 | Coherix, Inc. | Method for processing multiwavelength interferometric imaging data |
US20060069060A1 (en) | 2004-09-27 | 2006-03-30 | Sanjeev Redkar | Salts of decitabine |
US7154505B2 (en) | 2004-11-11 | 2006-12-26 | Stonecube Limited | Method of and apparatus for generating a representation of an object |
KR20060080817A (ko) | 2005-01-06 | 2006-07-11 | 씨제이 주식회사 | 시부트라민의 디카복실산염 |
MY148074A (en) | 2005-05-10 | 2013-02-28 | Novartis Ag | Pharmaceutical compositions comprising imatinib and a release retardant |
CA2617327A1 (en) | 2005-08-04 | 2007-02-15 | Novartis Ag | Salts of vildagliptin |
DE102005041860A1 (de) | 2005-09-02 | 2007-03-08 | Schering Ag | Nanopartikulärer Einschluss- und Ladungskomplex für pharmazeutische Formulierungen |
JP2009519952A (ja) | 2005-12-16 | 2009-05-21 | ワイス | トリアゾロピリミジン化合物の凍結乾燥組成物 |
US20060223820A1 (en) | 2006-03-21 | 2006-10-05 | Chemagis Ltd. | Crystalline aripiprazole salts and processes for preparation and purification thereof |
US8895531B2 (en) * | 2006-03-23 | 2014-11-25 | Rfs Pharma Llc | 2′-fluoronucleoside phosphonates as antiviral agents |
LT3150586T (lt) * | 2007-02-23 | 2020-03-10 | Gilead Sciences, Inc. | Terapinių agentų farmakokinetinių savybių moduliatoriai |
US20090163449A1 (en) | 2007-12-20 | 2009-06-25 | Eastman Chemical Company | Sulfo-polymer powder and sulfo-polymer powder blends with carriers and/or additives |
EP2307435B1 (en) | 2008-07-08 | 2012-06-13 | Gilead Sciences, Inc. | Salts of hiv inhibitor compounds |
JP4330086B1 (ja) | 2009-02-09 | 2009-09-09 | 株式会社テクネス | 非酸化物セラミックス製品の製造方法 |
EP2305680A3 (en) | 2009-09-30 | 2011-05-18 | Aurobindo Pharma Limited | Novel salts of (1S,4R)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol |
US20140094609A1 (en) | 2012-10-03 | 2014-04-03 | Gilead Sciences, Inc. | Process for the preparation of an hiv integrase inhibitor |
US20140094485A1 (en) | 2012-10-03 | 2014-04-03 | Gilead Sciences, Inc. | Solid state forms of hiv inhibitor |
-
2005
- 2005-07-26 DK DK10178348.8T patent/DK2258376T3/en active
- 2005-07-26 RS RSP20110303 patent/RS51799B/en unknown
- 2005-07-26 AT AT05857701T patent/ATE505196T1/de active
- 2005-07-26 NZ NZ553405A patent/NZ553405A/xx unknown
- 2005-07-26 MX MX2007001053A patent/MX2007001053A/es not_active Application Discontinuation
- 2005-07-26 DK DK05857701.6T patent/DK1778251T3/da active
- 2005-07-26 CN CNA2005800325676A patent/CN101027062A/zh active Pending
- 2005-07-26 KR KR1020077004805A patent/KR101233824B1/ko active IP Right Grant
- 2005-07-26 EA EA200700363A patent/EA019419B1/ru not_active IP Right Cessation
- 2005-07-26 LT LTEP10178348.8T patent/LT2258376T/lt unknown
- 2005-07-26 CA CA002574514A patent/CA2574514A1/en not_active Abandoned
- 2005-07-26 PL PL10178348T patent/PL2258376T3/pl unknown
- 2005-07-26 UA UAA200701987A patent/UA88313C2/ru unknown
- 2005-07-26 JP JP2007523730A patent/JP2008508291A/ja active Pending
- 2005-07-26 HU HUE10178348A patent/HUE043207T2/hu unknown
- 2005-07-26 ME MEP-2011-303A patent/ME01945B/me unknown
- 2005-07-26 PT PT05857701T patent/PT1778251E/pt unknown
- 2005-07-26 SI SI200532247T patent/SI2258376T1/sl unknown
- 2005-07-26 AU AU2005330489A patent/AU2005330489B2/en active Active
- 2005-07-26 AR ARP050103101 patent/AR051922A1/es active IP Right Grant
- 2005-07-26 US US11/658,419 patent/US8318701B2/en active Active
- 2005-07-26 BR BRPI0512690-8A patent/BRPI0512690A/pt not_active IP Right Cessation
- 2005-07-26 PL PL382846A patent/PL216369B1/pl not_active IP Right Cessation
- 2005-07-26 AP AP2007003912A patent/AP2412A/xx active
- 2005-07-26 EP EP19155831.1A patent/EP3539546A1/en not_active Withdrawn
- 2005-07-26 TR TR2019/06416T patent/TR201906416T4/tr unknown
- 2005-07-26 WO PCT/US2005/026504 patent/WO2006110157A2/en active Application Filing
- 2005-07-26 DE DE602005027466T patent/DE602005027466D1/de active Active
- 2005-07-26 US US11/190,225 patent/US7871991B2/en active Active
- 2005-07-26 EP EP10178348.8A patent/EP2258376B1/en active Active
- 2005-07-26 PL PL05857701T patent/PL1778251T3/pl unknown
- 2005-07-26 SI SI200531308T patent/SI1778251T1/sl unknown
- 2005-07-26 PT PT10178348T patent/PT2258376T/pt unknown
- 2005-07-26 RS RS20190476A patent/RS58600B1/sr unknown
- 2005-07-26 ES ES05857701T patent/ES2363160T3/es active Active
- 2005-07-26 ES ES10178348T patent/ES2720618T3/es active Active
- 2005-07-26 EP EP05857701A patent/EP1778251B1/en active Active
- 2005-07-26 ME MEP-2019-115A patent/ME03423B/me unknown
- 2005-07-27 AT AT05777315T patent/ATE469163T1/de not_active IP Right Cessation
- 2005-07-27 SG SG200905022-0A patent/SG155164A1/en unknown
- 2005-07-27 TW TW94125503A patent/TWI362934B/zh active
- 2005-07-27 NZ NZ553406A patent/NZ553406A/en unknown
- 2005-07-27 US US11/658,628 patent/US8329926B2/en active Active
- 2005-07-27 EA EA200700362A patent/EA019559B1/ru not_active IP Right Cessation
- 2005-07-27 EP EP05777315A patent/EP1778249B1/en active Active
- 2005-07-27 CN CN2010102437749A patent/CN101914124B/zh active Active
- 2005-07-27 WO PCT/US2005/027088 patent/WO2006015261A2/en active Application Filing
- 2005-07-27 AU AU2005267800A patent/AU2005267800B2/en active Active
- 2005-07-27 AP AP2007003899A patent/AP2629A/xx active
- 2005-07-27 CN CN2010102437734A patent/CN101935333A/zh active Pending
- 2005-07-27 KR KR1020077004803A patent/KR101233823B1/ko active IP Right Grant
- 2005-07-27 JP JP2007523866A patent/JP4954877B2/ja active Active
- 2005-07-27 MX MX2007001059A patent/MX2007001059A/es active IP Right Grant
- 2005-07-27 PL PL382843A patent/PL230036B1/pl unknown
- 2005-07-27 ES ES05777315T patent/ES2346454T3/es active Active
- 2005-07-27 BR BRPI0512683-5A patent/BRPI0512683A/pt active Search and Examination
- 2005-07-27 DE DE602005021506T patent/DE602005021506D1/de active Active
- 2005-07-27 CN CN2005800325568A patent/CN101031306B/zh active Active
- 2005-07-27 CA CA2574121A patent/CA2574121C/en active Active
- 2005-07-27 UA UAA200701991A patent/UA91688C2/ru unknown
-
2007
- 2007-01-17 IL IL180758A patent/IL180758A/en active IP Right Grant
- 2007-01-18 IL IL180781A patent/IL180781A/en active IP Right Grant
- 2007-01-23 IS IS8594A patent/IS2840B/is unknown
- 2007-01-23 IS IS8595A patent/IS8595A/is unknown
- 2007-02-20 ZA ZA2007/01466A patent/ZA200701466B/en unknown
- 2007-02-20 ZA ZA200701465A patent/ZA200701465B/xx unknown
- 2007-02-26 NO NO20071077A patent/NO339222B1/no unknown
- 2007-02-26 NO NO20071078A patent/NO339020B1/no unknown
- 2007-02-27 HR HR20070079A patent/HRP20070079A2/hr not_active Application Discontinuation
- 2007-02-27 HR HR20070078A patent/HRP20070078A2/hr not_active Application Discontinuation
- 2007-11-02 HK HK07111940.1A patent/HK1103648A1/xx unknown
- 2007-11-02 HK HK07111941.0A patent/HK1103649A1/xx unknown
-
2011
- 2011-06-03 JP JP2011125822A patent/JP2011201911A/ja not_active Withdrawn
- 2011-07-06 CY CY20111100662T patent/CY1111709T1/el unknown
- 2011-07-13 HR HR20110527T patent/HRP20110527T1/hr unknown
-
2012
- 2012-09-25 US US13/626,687 patent/US8697861B2/en active Active
- 2012-10-17 US US13/653,982 patent/US9579332B2/en active Active
-
2014
- 2014-02-11 US US14/178,237 patent/US9457035B2/en active Active
-
2016
- 2016-09-01 US US15/254,684 patent/US20170088576A1/en not_active Abandoned
- 2016-09-23 NO NO20161521A patent/NO342132B1/no unknown
- 2016-10-07 NO NO20161612A patent/NO342571B1/no unknown
-
2017
- 2017-01-10 US US15/402,857 patent/US20170210770A1/en not_active Abandoned
- 2017-07-06 US US15/643,168 patent/US20180086784A1/en not_active Abandoned
-
2018
- 2018-02-16 NO NO20180243A patent/NO20180243A1/no not_active Application Discontinuation
- 2018-11-19 US US16/195,152 patent/US20190315785A1/en not_active Abandoned
- 2018-11-20 US US16/196,075 patent/US20190345190A1/en not_active Abandoned
-
2019
- 2019-04-16 HR HRP20190712TT patent/HRP20190712T1/hr unknown
- 2019-05-14 CY CY20191100518T patent/CY1121623T1/el unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20110527T1 (hr) | Nukleozid-fosfonatni konjugati kao sredstva protiv hiv-a | |
KR102626210B1 (ko) | N4-하이드록시사이티딘 및 유도체 및 이와 관련된 항-바이러스 용도 | |
TWI332956B (en) | Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds | |
AU2018236826B2 (en) | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use | |
ES2892123T3 (es) | Derivados antivíricos de N4-hidroxicitidina | |
ES2452718T3 (es) | Profármacos a base de lisina de inhibidores de la aspartil proteasa y procesos para su preparación | |
ES2488922T3 (es) | Fosfoindoles enantiómeramente puros como inhibidores del HIV | |
EP3762372A1 (en) | 4'-halogen containing nucleotide and nucleoside therapeutic compositions and uses related thereto | |
EA019749B1 (ru) | Противовирусные соединения | |
CN111454273A (zh) | 多环碳酰基吡啶酮化合物及其药物用途 | |
Zakharova et al. | Tyrosine-based 1-(S)-[3-hydroxy-2-(phosphonomethoxy) propyl] cytosine and-adenine ((S)-HPMPC and (S)-HPMPA) prodrugs: Synthesis, stability, antiviral activity, and in vivo transport studies | |
CN112533609A (zh) | 抗hiv化合物 | |
NO154751B (no) | Analogifremgangsmaate for fremstilling av terapeutisk virksomme hydroksykarbonylfosfonsyreestere. | |
JP2023531524A (ja) | 1’-シアノヌクレオシド類似体及びその使用 | |
JP5584865B2 (ja) | 抗ウイルス薬のための前駆体分子としての新規なヌクレオチド類似体 | |
Eriksson et al. | Serine peptide phosphoester prodrugs of cyclic cidofovir: synthesis, transport, and antiviral activity | |
WO1995012605A1 (en) | Novel amino acid derivatives | |
CA3186054A1 (en) | Prodrugs of phosphonamide nucleotide analogues and their pharmaceutical use | |
EP4040965A2 (en) | 4'-halogen containing nucleotide and nucleoside therapeutic compositions and uses related thereto | |
NO883468L (no) | Fremgangsmaate til fremstilling av farmasoeytiske blandinger inneholdende cyklopeptider som reserpsjonsbefordrere vedapplikasjon paa slimhuden. | |
NO784332L (no) | Amidderivater, farmasoeytiske preparater og fremgangsmaate til bekjempelse av virusinfeksjoner | |
Eriksson | Synthesis and biological evaluation of novel cidofovir prodrugs targeting hPEPT1 | |
Peterson | Peptidomimetic prodrugs of cidofovir: Design, synthesis, transport, mechanism of activation, and antiviral activity | |
Williams | Nucleoside Phosphonate Prodrugs: Synthesis and Antiviral Activity | |
Krylov et al. | Enzymatically activated phosphate and phosphonate prodrugs |