OA10691A - Treatment of the cns effects of hiv with vx-478 alone or in combination with azt or 3tc - Google Patents

Treatment of the cns effects of hiv with vx-478 alone or in combination with azt or 3tc Download PDF

Info

Publication number: OA10691A
Authority: OA; OAPI
Prior art keywords: hiv; compound; formula; cns; viral
Prior art date: 1995-12-05

Application number

OA9800067A

Other languages

English (en)

Inventor

Pravin Ramsewak Chaturvedi

Original Assignee

Vertex Pharma

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1995-12-05

Filing date

1998-05-29

Publication date

2001-05-04

1998-05-29 Application filed by Vertex Pharma filed Critical Vertex Pharma

2001-05-04 Publication of OA10691A publication Critical patent/OA10691A/en

Links

230000000694 effects Effects 0.000 title claims abstract description 17
238000011282 treatment Methods 0.000 title claims description 12
150000001875 compounds Chemical class 0.000 claims description 44
239000008194 pharmaceutical composition Substances 0.000 claims description 12
108010017640 Aspartic Acid Proteases Proteins 0.000 claims description 9
102000004580 Aspartic Acid Proteases Human genes 0.000 claims description 9
208000015181 infectious disease Diseases 0.000 claims description 7
210000002845 virion Anatomy 0.000 claims description 7
241000700605 Viruses Species 0.000 claims description 6
238000004519 manufacturing process Methods 0.000 claims description 5
230000005764 inhibitory process Effects 0.000 claims description 3
230000002458 infectious effect Effects 0.000 claims 2
238000000034 method Methods 0.000 abstract description 19
239000000203 mixture Substances 0.000 abstract description 17
206010065040 AIDS dementia complex Diseases 0.000 abstract description 3
210000003169 central nervous system Anatomy 0.000 abstract 2
241000725303 Human immunodeficiency virus Species 0.000 description 21
-1 amine ketone Chemical class 0.000 description 18
239000003795 chemical substances by application Substances 0.000 description 16
RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 10
208000030507 AIDS Diseases 0.000 description 9
QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 9
206010011416 Croup infectious Diseases 0.000 description 8
201000010549 croup Diseases 0.000 description 8
230000003612 virological effect Effects 0.000 description 8
108091005804 Peptidases Proteins 0.000 description 7
239000004365 Protease Substances 0.000 description 7
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 7
239000003112 inhibitor Substances 0.000 description 7
239000002243 precursor Substances 0.000 description 7
208000031886 HIV Infections Diseases 0.000 description 6
208000037357 HIV infectious disease Diseases 0.000 description 6
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 6
210000004556 brain Anatomy 0.000 description 6
238000006243 chemical reaction Methods 0.000 description 6
208000033519 human immunodeficiency virus infectious disease Diseases 0.000 description 6
239000002904 solvent Substances 0.000 description 6
241000894007 species Species 0.000 description 6
150000001412 amines Chemical class 0.000 description 5
235000001014 amino acid Nutrition 0.000 description 5
150000001413 amino acids Chemical class 0.000 description 5
201000010099 disease Diseases 0.000 description 5
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 5
230000002401 inhibitory effect Effects 0.000 description 5
239000000243 solution Substances 0.000 description 5
208000024891 symptom Diseases 0.000 description 5
102100031780 Endonuclease Human genes 0.000 description 4
102000035195 Peptidases Human genes 0.000 description 4
108010092799 RNA-directed DNA polymerase Proteins 0.000 description 4
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 4
239000002253 acid Substances 0.000 description 4
239000002671 adjuvant Substances 0.000 description 4
239000003443 antiviral agent Substances 0.000 description 4
230000000707 stereoselective effect Effects 0.000 description 4
239000000725 suspension Substances 0.000 description 4
230000009385 viral infection Effects 0.000 description 4
XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 3
102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 description 3
YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 3
208000036142 Viral infection Diseases 0.000 description 3
150000001370 alpha-amino acid derivatives Chemical class 0.000 description 3
235000008206 alpha-amino acids Nutrition 0.000 description 3
150000001414 amino alcohols Chemical class 0.000 description 3
239000003696 aspartic proteinase inhibitor Substances 0.000 description 3
239000002585 base Substances 0.000 description 3
239000000969 carrier Substances 0.000 description 3
210000004027 cell Anatomy 0.000 description 3
239000003153 chemical reaction reagent Substances 0.000 description 3
239000001257 hydrogen Substances 0.000 description 3
229910052739 hydrogen Inorganic materials 0.000 description 3
125000002887 hydroxy group Chemical group [H]O* 0.000 description 3
125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 description 3
239000003921 oil Substances 0.000 description 3
235000019198 oils Nutrition 0.000 description 3
239000000137 peptide hydrolase inhibitor Substances 0.000 description 3
125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 3
125000006239 protecting group Chemical group 0.000 description 3
108090000623 proteins and genes Proteins 0.000 description 3
229940124530 sulfonamide Drugs 0.000 description 3
150000003456 sulfonamides Chemical class 0.000 description 3
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 description 2
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
229920002261 Corn starch Polymers 0.000 description 2
229920000858 Cyclodextrin Polymers 0.000 description 2
DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
102000006992 Interferon-alpha Human genes 0.000 description 2
108010047761 Interferon-alpha Proteins 0.000 description 2
KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 description 2
NBIIXXVUZAFLBC-UHFFFAOYSA-L Phosphate ion(2-) Chemical compound OP([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-L 0.000 description 2
ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 2
UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
210000001744 T-lymphocyte Anatomy 0.000 description 2
150000007513 acids Chemical class 0.000 description 2
230000009471 action Effects 0.000 description 2
230000001154 acute effect Effects 0.000 description 2
HIGRAKVNKLCVCA-UHFFFAOYSA-N alumine Chemical class C1=CC=[Al]C=C1 HIGRAKVNKLCVCA-UHFFFAOYSA-N 0.000 description 2
239000002259 anti human immunodeficiency virus agent Substances 0.000 description 2
229940124411 anti-hiv antiviral agent Drugs 0.000 description 2
230000000840 anti-viral effect Effects 0.000 description 2
229940124522 antiretrovirals Drugs 0.000 description 2
239000003903 antiretrovirus agent Substances 0.000 description 2
230000004888 barrier function Effects 0.000 description 2
235000013405 beer Nutrition 0.000 description 2
210000004369 blood Anatomy 0.000 description 2
239000008280 blood Substances 0.000 description 2
230000037396 body weight Effects 0.000 description 2
UORVGPXVDQYIDP-UHFFFAOYSA-N borane Chemical compound B UORVGPXVDQYIDP-UHFFFAOYSA-N 0.000 description 2
239000000872 buffer Substances 0.000 description 2
229910052799 carbon Inorganic materials 0.000 description 2
108091092356 cellular DNA Proteins 0.000 description 2
239000008120 corn starch Substances 0.000 description 2
WHBIGIKBNXZKFE-UHFFFAOYSA-N delavirdine Chemical compound 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 description 2
235000014113 dietary fatty acids Nutrition 0.000 description 2
229940042399 direct acting antivirals protease inhibitors Drugs 0.000 description 2
239000002270 dispersing agent Substances 0.000 description 2
238000009826 distribution Methods 0.000 description 2
239000003937 drug carrier Substances 0.000 description 2
239000000194 fatty acid Substances 0.000 description 2
229930195729 fatty acid Natural products 0.000 description 2
150000004665 fatty acids Chemical class 0.000 description 2
238000009472 formulation Methods 0.000 description 2
150000004820 halides Chemical class 0.000 description 2
239000004030 hiv protease inhibitor Substances 0.000 description 2
150000002431 hydrogen Chemical class 0.000 description 2
239000012442 inert solvent Substances 0.000 description 2
230000002452 interceptive effect Effects 0.000 description 2
125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 2
239000008101 lactose Substances 0.000 description 2
210000000653 nervous system Anatomy 0.000 description 2
NQDJXKOVJZTUJA-UHFFFAOYSA-N nevirapine Chemical compound C12=NC=CC=C2C(=O)NC=2C(C)=CC=NC=2N1C1CC1 NQDJXKOVJZTUJA-UHFFFAOYSA-N 0.000 description 2
229910052700 potassium Inorganic materials 0.000 description 2
239000011591 potassium Substances 0.000 description 2
230000000069 prophylactic effect Effects 0.000 description 2
230000001681 protective effect Effects 0.000 description 2
235000018102 proteins Nutrition 0.000 description 2
102000004169 proteins and genes Human genes 0.000 description 2
108010043277 recombinant soluble CD4 Proteins 0.000 description 2
230000002829 reductive effect Effects 0.000 description 2
229960000311 ritonavir Drugs 0.000 description 2
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 description 2
QWAXKHKRTORLEM-UGJKXSETSA-N saquinavir Chemical compound 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 QWAXKHKRTORLEM-UGJKXSETSA-N 0.000 description 2
229920006395 saturated elastomer Polymers 0.000 description 2
239000011780 sodium chloride Substances 0.000 description 2
239000000126 substance Substances 0.000 description 2
125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 2
150000003461 sulfonyl halides Chemical class 0.000 description 2
239000000829 suppository Substances 0.000 description 2
239000000375 suspending agent Substances 0.000 description 2
208000011580 syndromic disease Diseases 0.000 description 2
230000001225 therapeutic effect Effects 0.000 description 2
238000002560 therapeutic procedure Methods 0.000 description 2
230000000699 topical effect Effects 0.000 description 2
231100000419 toxicity Toxicity 0.000 description 2
230000001988 toxicity Effects 0.000 description 2
241001430294 unidentified retrovirus Species 0.000 description 2
WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 1
WSLDOOZREJYCGB-UHFFFAOYSA-N 1,2-Dichloroethane Chemical compound ClCCCl WSLDOOZREJYCGB-UHFFFAOYSA-N 0.000 description 1
ASOKPJOREAFHNY-UHFFFAOYSA-N 1-Hydroxybenzotriazole Chemical group C1=CC=C2N(O)N=NC2=C1 ASOKPJOREAFHNY-UHFFFAOYSA-N 0.000 description 1
IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
CHHHXKFHOYLYRE-UHFFFAOYSA-M 2,4-Hexadienoic acid, potassium salt (1:1), (2E,4E)- Chemical compound [K+].CC=CC=CC([O-])=O CHHHXKFHOYLYRE-UHFFFAOYSA-M 0.000 description 1
LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 1
JXRGUPLJCCDGKG-UHFFFAOYSA-N 4-nitrobenzenesulfonyl chloride Chemical compound [O-][N+](=O)C1=CC=C(S(Cl)(=O)=O)C=C1 JXRGUPLJCCDGKG-UHFFFAOYSA-N 0.000 description 1
BTJIUGUIPKRLHP-UHFFFAOYSA-N 4-nitrophenol Chemical compound OC1=CC=C([N+]([O-])=O)C=C1 BTJIUGUIPKRLHP-UHFFFAOYSA-N 0.000 description 1
QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 1
206010001513 AIDS related complex Diseases 0.000 description 1
101710110426 Aspartyl protease inhibitor Proteins 0.000 description 1
CIUUIPMOFZIWIZ-UHFFFAOYSA-N Bropirimine Chemical compound NC1=NC(O)=C(Br)C(C=2C=CC=CC=2)=N1 CIUUIPMOFZIWIZ-UHFFFAOYSA-N 0.000 description 1
101710132601 Capsid protein Proteins 0.000 description 1
101710205625 Capsid protein p24 Proteins 0.000 description 1
BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 1
XFXPMWWXUTWYJX-UHFFFAOYSA-N Cyanide Chemical compound N#[C-] XFXPMWWXUTWYJX-UHFFFAOYSA-N 0.000 description 1
108020004414 DNA Proteins 0.000 description 1
102000004163 DNA-directed RNA polymerases Human genes 0.000 description 1
108090000626 DNA-directed RNA polymerases Proteins 0.000 description 1
206010012289 Dementia Diseases 0.000 description 1
241000255581 Drosophila <fruit fly, genus> Species 0.000 description 1
108010042407 Endonucleases Proteins 0.000 description 1
VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 1
239000005977 Ethylene Substances 0.000 description 1
244000182067 Fraxinus ornus Species 0.000 description 1
239000004471 Glycine Substances 0.000 description 1
108010017213 Granulocyte-Macrophage Colony-Stimulating Factor Proteins 0.000 description 1
102000004457 Granulocyte-Macrophage Colony-Stimulating Factor Human genes 0.000 description 1
108010010369 HIV Protease Proteins 0.000 description 1
229940122440 HIV protease inhibitor Drugs 0.000 description 1
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
206010061598 Immunodeficiency Diseases 0.000 description 1
208000029462 Immunodeficiency disease Diseases 0.000 description 1
102000014150 Interferons Human genes 0.000 description 1
108010050904 Interferons Proteins 0.000 description 1
108010002350 Interleukin-2 Proteins 0.000 description 1
102000000588 Interleukin-2 Human genes 0.000 description 1
OWYWGLHRNBIFJP-UHFFFAOYSA-N Ipazine Chemical compound CCN(CC)C1=NC(Cl)=NC(NC(C)C)=N1 OWYWGLHRNBIFJP-UHFFFAOYSA-N 0.000 description 1
208000008771 Lymphadenopathy Diseases 0.000 description 1
FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
241000124008 Mammalia Species 0.000 description 1
AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 description 1
NQTADLQHYWFPDB-UHFFFAOYSA-N N-Hydroxysuccinimide Chemical compound ON1C(=O)CCC1=O NQTADLQHYWFPDB-UHFFFAOYSA-N 0.000 description 1
239000005642 Oleic acid Substances 0.000 description 1
ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 description 1
208000001388 Opportunistic Infections Diseases 0.000 description 1
101710177166 Phosphoprotein Proteins 0.000 description 1
239000004698 Polyethylene Substances 0.000 description 1
229920001214 Polysorbate 60 Polymers 0.000 description 1
229940124158 Protease/peptidase inhibitor Drugs 0.000 description 1
206010037660 Pyrexia Diseases 0.000 description 1
108090000783 Renin Proteins 0.000 description 1
102100028255 Renin Human genes 0.000 description 1
IWUCXVSUMQZMFG-AFCXAGJDSA-N Ribavirin Chemical compound N1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 IWUCXVSUMQZMFG-AFCXAGJDSA-N 0.000 description 1
235000004443 Ricinus communis Nutrition 0.000 description 1
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
241000713311 Simian immunodeficiency virus Species 0.000 description 1
241000714229 Simian retrovirus 1 Species 0.000 description 1
101710149279 Small delta antigen Proteins 0.000 description 1
KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 1
HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 description 1
108060008682 Tumor Necrosis Factor Proteins 0.000 description 1
108700010756 Viral Polyproteins Proteins 0.000 description 1
108700022715 Viral Proteases Proteins 0.000 description 1
229940124532 absorption promoter Drugs 0.000 description 1
DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
229960004150 aciclovir Drugs 0.000 description 1
MKUXAQIIEYXACX-UHFFFAOYSA-N aciclovir Chemical compound N1C(N)=NC(=O)C2=C1N(COCCO)C=N2 MKUXAQIIEYXACX-UHFFFAOYSA-N 0.000 description 1
230000003213 activating effect Effects 0.000 description 1
230000004913 activation Effects 0.000 description 1
239000000654 additive Substances 0.000 description 1
230000000996 additive effect Effects 0.000 description 1
239000003513 alkali Substances 0.000 description 1
150000001350 alkyl halides Chemical class 0.000 description 1
150000008052 alkyl sulfonates Chemical class 0.000 description 1
230000029936 alkylation Effects 0.000 description 1
238000005804 alkylation reaction Methods 0.000 description 1
HFHDHCJBZVLPGP-RWMJIURBSA-N alpha-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO HFHDHCJBZVLPGP-RWMJIURBSA-N 0.000 description 1
XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
229910052782 aluminium Inorganic materials 0.000 description 1
230000000798 anti-retroviral effect Effects 0.000 description 1
238000002832 anti-viral assay Methods 0.000 description 1
239000000427 antigen Substances 0.000 description 1
108091007433 antigens Proteins 0.000 description 1
102000036639 antigens Human genes 0.000 description 1
229940006133 antiglaucoma drug and miotics carbonic anhydrase inhibitors Drugs 0.000 description 1
239000007900 aqueous suspension Substances 0.000 description 1
238000003556 assay Methods 0.000 description 1
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
235000013871 bee wax Nutrition 0.000 description 1
239000012166 beeswax Substances 0.000 description 1
WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 description 1
229960004853 betadex Drugs 0.000 description 1
230000004071 biological effect Effects 0.000 description 1
230000015572 biosynthetic process Effects 0.000 description 1
229910000085 borane Inorganic materials 0.000 description 1
210000005013 brain tissue Anatomy 0.000 description 1
229950009494 bropirimine Drugs 0.000 description 1
239000002775 capsule Substances 0.000 description 1
150000004657 carbamic acid derivatives Chemical class 0.000 description 1
239000003489 carbonate dehydratase inhibitor Substances 0.000 description 1
150000004649 carbonic acid derivatives Chemical class 0.000 description 1
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
239000001768 carboxy methyl cellulose Substances 0.000 description 1
230000003197 catalytic effect Effects 0.000 description 1
230000007541 cellular toxicity Effects 0.000 description 1
239000001913 cellulose Substances 0.000 description 1
229920002678 cellulose Polymers 0.000 description 1
239000012069 chiral reagent Substances 0.000 description 1
AOGYCOYQMAVAFD-UHFFFAOYSA-N chlorocarbonic acid Chemical class OC(Cl)=O AOGYCOYQMAVAFD-UHFFFAOYSA-N 0.000 description 1
101150087654 chrnd gene Proteins 0.000 description 1
230000001684 chronic effect Effects 0.000 description 1
238000003776 cleavage reaction Methods 0.000 description 1
101150093710 clec-87 gene Proteins 0.000 description 1
238000011260 co-administration Methods 0.000 description 1
229940110456 cocoa butter Drugs 0.000 description 1
235000019868 cocoa butter Nutrition 0.000 description 1
239000008119 colloidal silica Substances 0.000 description 1
239000003086 colorant Substances 0.000 description 1
238000010276 construction Methods 0.000 description 1
230000008878 coupling Effects 0.000 description 1
238000010168 coupling process Methods 0.000 description 1
238000005859 coupling reaction Methods 0.000 description 1
JJCFRYNCJDLXIK-UHFFFAOYSA-N cyproheptadine Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2C=CC2=CC=CC=C21 JJCFRYNCJDLXIK-UHFFFAOYSA-N 0.000 description 1
230000006378 damage Effects 0.000 description 1
229960005319 delavirdine Drugs 0.000 description 1
235000005911 diet Nutrition 0.000 description 1
230000037213 diet Effects 0.000 description 1
239000003085 diluting agent Substances 0.000 description 1
231100000676 disease causative agent Toxicity 0.000 description 1
239000002552 dosage form Substances 0.000 description 1
239000003792 electrolyte Substances 0.000 description 1
239000003995 emulsifying agent Substances 0.000 description 1
230000001804 emulsifying effect Effects 0.000 description 1
239000008387 emulsifying waxe Substances 0.000 description 1
150000002118 epoxides Chemical class 0.000 description 1
BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
235000019197 fats Nutrition 0.000 description 1
GDSRMADSINPKSL-HSEONFRVSA-N gamma-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO GDSRMADSINPKSL-HSEONFRVSA-N 0.000 description 1
229940080345 gamma-cyclodextrin Drugs 0.000 description 1
210000001035 gastrointestinal tract Anatomy 0.000 description 1
150000004676 glycans Chemical class 0.000 description 1
125000005456 glyceride group Chemical group 0.000 description 1
229960002449 glycine Drugs 0.000 description 1
230000003862 health status Effects 0.000 description 1
125000005842 heteroatom Chemical group 0.000 description 1
150000004678 hydrides Chemical class 0.000 description 1
XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 description 1
150000004679 hydroxides Chemical class 0.000 description 1
NPZTUJOABDZTLV-UHFFFAOYSA-N hydroxybenzotriazole Substances O=C1C=CC=C2NNN=C12 NPZTUJOABDZTLV-UHFFFAOYSA-N 0.000 description 1
210000000987 immune system Anatomy 0.000 description 1
230000007813 immunodeficiency Effects 0.000 description 1
239000002955 immunomodulating agent Substances 0.000 description 1
229940121354 immunomodulator Drugs 0.000 description 1
230000006872 improvement Effects 0.000 description 1
238000011065 in-situ storage Methods 0.000 description 1
229940102223 injectable solution Drugs 0.000 description 1
238000002347 injection Methods 0.000 description 1
239000007924 injection Substances 0.000 description 1
229940079322 interferon Drugs 0.000 description 1
238000007917 intracranial administration Methods 0.000 description 1
238000007919 intrasynovial administration Methods 0.000 description 1
INQOMBQAUSQDDS-UHFFFAOYSA-N iodomethane Chemical compound IC INQOMBQAUSQDDS-UHFFFAOYSA-N 0.000 description 1
150000002500 ions Chemical class 0.000 description 1
QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 1
239000000787 lecithin Substances 0.000 description 1
235000010445 lecithin Nutrition 0.000 description 1
229940067606 lecithin Drugs 0.000 description 1
208000032839 leukemia Diseases 0.000 description 1
239000003446 ligand Substances 0.000 description 1
230000000670 limiting effect Effects 0.000 description 1
230000007774 longterm Effects 0.000 description 1
239000006210 lotion Substances 0.000 description 1
239000000314 lubricant Substances 0.000 description 1
210000004324 lymphatic system Anatomy 0.000 description 1
239000003550 marker Substances 0.000 description 1
230000004060 metabolic process Effects 0.000 description 1
238000002156 mixing Methods 0.000 description 1
230000004048 modification Effects 0.000 description 1
238000012986 modification Methods 0.000 description 1
230000035772 mutation Effects 0.000 description 1
DQCKKXVULJGBQN-XFWGSAIBSA-N naltrexone Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=O)O)CC1)O)CC1CC1 DQCKKXVULJGBQN-XFWGSAIBSA-N 0.000 description 1
229960003086 naltrexone Drugs 0.000 description 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 description 1
229960000689 nevirapine Drugs 0.000 description 1
150000002828 nitro derivatives Chemical class 0.000 description 1
229910052757 nitrogen Inorganic materials 0.000 description 1
LYGJENNIWJXYER-UHFFFAOYSA-N nitromethane Chemical compound C[N+]([O-])=O LYGJENNIWJXYER-UHFFFAOYSA-N 0.000 description 1
231100000344 non-irritating Toxicity 0.000 description 1
231100000252 nontoxic Toxicity 0.000 description 1
230000003000 nontoxic effect Effects 0.000 description 1
239000000346 nonvolatile oil Substances 0.000 description 1
239000002777 nucleoside Substances 0.000 description 1
150000003833 nucleoside derivatives Chemical class 0.000 description 1
229940060184 oil ingredients Drugs 0.000 description 1
ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
239000004006 olive oil Substances 0.000 description 1
235000008390 olive oil Nutrition 0.000 description 1
239000001301 oxygen Substances 0.000 description 1
229910052760 oxygen Inorganic materials 0.000 description 1
230000036961 partial effect Effects 0.000 description 1
230000001575 pathological effect Effects 0.000 description 1
XDRYMKDFEDOLFX-UHFFFAOYSA-N pentamidine Chemical compound C1=CC(C(=N)N)=CC=C1OCCCCCOC1=CC=C(C(N)=N)C=C1 XDRYMKDFEDOLFX-UHFFFAOYSA-N 0.000 description 1
229960004448 pentamidine Drugs 0.000 description 1
239000003208 petroleum Substances 0.000 description 1
108010089520 pol Gene Products Proteins 0.000 description 1
108700004029 pol Genes Proteins 0.000 description 1
101150088264 pol gene Proteins 0.000 description 1
239000002798 polar solvent Substances 0.000 description 1
229920000573 polyethylene Polymers 0.000 description 1
229920001223 polyethylene glycol Polymers 0.000 description 1
229920000642 polymer Polymers 0.000 description 1
235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 1
235000010989 polyoxyethylene sorbitan monostearate Nutrition 0.000 description 1
229920001184 polypeptide Polymers 0.000 description 1
229920001451 polypropylene glycol Polymers 0.000 description 1
229920001282 polysaccharide Polymers 0.000 description 1
239000005017 polysaccharide Substances 0.000 description 1
229940113124 polysorbate 60 Drugs 0.000 description 1
229920000053 polysorbate 80 Polymers 0.000 description 1
239000004302 potassium sorbate Substances 0.000 description 1
235000010241 potassium sorbate Nutrition 0.000 description 1
229940069338 potassium sorbate Drugs 0.000 description 1
230000003389 potentiating effect Effects 0.000 description 1
239000003755 preservative agent Substances 0.000 description 1
150000003141 primary amines Chemical class 0.000 description 1
230000008569 process Effects 0.000 description 1
102000004196 processed proteins & peptides Human genes 0.000 description 1
108090000765 processed proteins & peptides Proteins 0.000 description 1
229940002612 prodrug Drugs 0.000 description 1
239000000651 prodrug Substances 0.000 description 1
QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 description 1
125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 1
230000002797 proteolythic effect Effects 0.000 description 1
WTTIBCHOELPGFK-LBPRGKRZSA-N r82150 Chemical compound C1N(CC=C(C)C)[C@@H](C)CN2C(=S)NC3=CC=CC1=C32 WTTIBCHOELPGFK-LBPRGKRZSA-N 0.000 description 1
230000000717 retained effect Effects 0.000 description 1
230000001177 retroviral effect Effects 0.000 description 1
230000002441 reversible effect Effects 0.000 description 1
229960000329 ribavirin Drugs 0.000 description 1
HZCAHMRRMINHDJ-DBRKOABJSA-N ribavirin Natural products O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1N=CN=C1 HZCAHMRRMINHDJ-DBRKOABJSA-N 0.000 description 1
239000003419 rna directed dna polymerase inhibitor Substances 0.000 description 1
150000003839 salts Chemical class 0.000 description 1
229960001852 saquinavir Drugs 0.000 description 1
230000007017 scission Effects 0.000 description 1
150000003335 secondary amines Chemical class 0.000 description 1
238000009097 single-agent therapy Methods 0.000 description 1
235000017557 sodium bicarbonate Nutrition 0.000 description 1
229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
229910000033 sodium borohydride Inorganic materials 0.000 description 1
239000012279 sodium borohydride Substances 0.000 description 1
235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
229910000104 sodium hydride Inorganic materials 0.000 description 1
239000012312 sodium hydride Substances 0.000 description 1
239000007787 solid Substances 0.000 description 1
239000004334 sorbic acid Substances 0.000 description 1
235000010199 sorbic acid Nutrition 0.000 description 1
229940075582 sorbic acid Drugs 0.000 description 1
239000001587 sorbitan monostearate Substances 0.000 description 1
235000011076 sorbitan monostearate Nutrition 0.000 description 1
229940035048 sorbitan monostearate Drugs 0.000 description 1
239000007921 spray Substances 0.000 description 1
KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
238000006277 sulfonation reaction Methods 0.000 description 1
230000002195 synergetic effect Effects 0.000 description 1
238000003786 synthesis reaction Methods 0.000 description 1
230000008685 targeting Effects 0.000 description 1
MHXBHWLGRWOABW-UHFFFAOYSA-N tetradecyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCCCCCCCCCCCCC MHXBHWLGRWOABW-UHFFFAOYSA-N 0.000 description 1
YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
231100001274 therapeutic index Toxicity 0.000 description 1
231100000331 toxic Toxicity 0.000 description 1
230000002588 toxic effect Effects 0.000 description 1
238000011269 treatment regimen Methods 0.000 description 1
125000004665 trialkylsilyl group Chemical group 0.000 description 1
VOITXYVAKOUIBA-UHFFFAOYSA-N triethylaluminium Chemical compound CC[Al](CC)CC VOITXYVAKOUIBA-UHFFFAOYSA-N 0.000 description 1
125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
102000003390 tumor necrosis factor Human genes 0.000 description 1
235000013311 vegetables Nutrition 0.000 description 1
239000003981 vehicle Substances 0.000 description 1
230000017613 viral reproduction Effects 0.000 description 1
239000001993 wax Substances 0.000 description 1
239000000080 wetting agent Substances 0.000 description 1
210000002268 wool Anatomy 0.000 description 1
150000003751 zinc Chemical class 0.000 description 1

Classifications

- 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
- 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
- A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
- A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV

Landscapes

Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Chemical & Material Sciences (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Epidemiology (AREA)
General Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Virology (AREA)
Molecular Biology (AREA)
Communicable Diseases (AREA)
Oncology (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Tropical Medicine & Parasitology (AREA)
AIDS & HIV (AREA)
Hospice & Palliative Care (AREA)
Psychiatry (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Peptides Or Proteins (AREA)

OA9800067A 1995-12-05 1998-05-29 Treatment of the cns effects of hiv with vx-478 alone or in combination with azt or 3tc OA10691A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US08/567,199 US5646180A (en)	1995-12-05	1995-12-05	Treatment of the CNS effects of HIV

Publications (1)

Publication Number	Publication Date
OA10691A true OA10691A (en)	2001-05-04

Family

ID=24266147

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
OA9800067A OA10691A (en)	1995-12-05	1998-05-29	Treatment of the cns effects of hiv with vx-478 alone or in combination with azt or 3tc

Country Status (23)

Country	Link
US (1)	US5646180A (pl)
EP (1)	EP0866696B1 (pl)
JP (1)	JP2000501713A (pl)
KR (1)	KR19990071750A (pl)
CN (1)	CN1203530A (pl)
AP (1)	AP864A (pl)
AT (1)	ATE279922T1 (pl)
AU (1)	AU722850B2 (pl)
BR (1)	BR9611861A (pl)
CA (1)	CA2238471A1 (pl)
CZ (1)	CZ291994B6 (pl)
DE (1)	DE69633680T2 (pl)
ES (1)	ES2231828T3 (pl)
HU (1)	HUP9903673A3 (pl)
NO (1)	NO317837B1 (pl)
NZ (1)	NZ324603A (pl)
OA (1)	OA10691A (pl)
PL (1)	PL187747B1 (pl)
PT (1)	PT866696E (pl)
RU (1)	RU2203658C2 (pl)
UA (1)	UA61902C2 (pl)
WO (1)	WO1997020554A1 (pl)
ZA (1)	ZA9610139B (pl)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US6107499A (en) *	1988-02-26	2000-08-22	Neuromedica, Inc.	Dopamine analog amide
US5942253A (en)	1995-10-12	1999-08-24	Immunex Corporation	Prolonged release of GM-CSF
US6576636B2 (en)	1996-05-22	2003-06-10	Protarga, Inc.	Method of treating a liver disorder with fatty acid-antiviral agent conjugates
US5795909A (en) *	1996-05-22	1998-08-18	Neuromedica, Inc.	DHA-pharmaceutical agent conjugates of taxanes
AU727983B2 (en) *	1996-06-25	2001-01-04	Glaxo Group Limited	Combinations comprising VX478, zidovudine, FTC and/or 3TC for use in the treatment of HIV
DE69718168T2 (de) *	1996-06-25	2003-10-23	Glaxo Group Ltd., Greenford	Zusammensetzungen enthaltend vx478, zidovudine und 159u89 für die verwendung in der behandlung von hiv
US6232333B1 (en)	1996-11-21	2001-05-15	Abbott Laboratories	Pharmaceutical composition
ZA9710071B (en) *	1996-11-21	1998-05-25	Abbott Lab	Pharmaceutical composition.
JP2001525840A (ja) *	1997-05-17	2001-12-11	グラクソ、グループ、リミテッド	炭素環式ヌクレオシド１５９２ｕ８９を含有する抗ウイルス的組合せ
WO1998057648A1 (en) *	1997-06-16	1998-12-23	Vertex Pharmaceuticals Incorporated	Methods of increasing the bioavailability of stable crystal polymorphs of a compound
US6576231B2 (en) *	1997-09-12	2003-06-10	Schering Ag	Methods for treating HIV-Infected Patients by the Administration of GM-CSF and a protease inhibitor
US5955459A (en) *	1997-11-26	1999-09-21	Neuromedica, Inc.	Fatty acid-antipsychotic compositions and uses thereof
US5977174A (en) *	1997-11-26	1999-11-02	Neuromedica, Inc.	Cholinergic compositions and uses thereof
US6197764B1 (en)	1997-11-26	2001-03-06	Protarga, Inc.	Clozapine compositions and uses thereof
US6153653A (en) *	1997-11-26	2000-11-28	Protarga, Inc.	Choline compositions and uses thereof
US6436989B1 (en) *	1997-12-24	2002-08-20	Vertex Pharmaceuticals, Incorporated	Prodrugs of aspartyl protease inhibitors
US6309632B1 (en) *	1998-04-28	2001-10-30	Immunex Corporation	Methods for treating HIV-infected patients by administering GM-CSF
US6875773B1 (en) *	1998-05-29	2005-04-05	Ben M. Dunn	Combination therapy for treatment of FIV infection
US20090197827A1 (en) *	1998-05-29	2009-08-06	Dunn Ben M	Combination Therapy for Treatment of FIV Infection
US6331537B1 (en)	1998-06-03	2001-12-18	Gpi Nil Holdings, Inc.	Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds
US7235583B1 (en) *	1999-03-09	2007-06-26	Luitpold Pharmaceuticals, Inc.,	Fatty acid-anticancer conjugates and uses thereof
US7253169B2 (en)	1999-11-12	2007-08-07	Gliamed, Inc.	Aza compounds, pharmaceutical compositions and methods of use
US6417189B1 (en)	1999-11-12	2002-07-09	Gpi Nil Holdings, Inc.	AZA compounds, pharmaceutical compositions and methods of use
MXPA02006134A (es)	1999-12-21	2002-12-13	Guilford Pharm Inc	Compuestos derivados de hidantoina, composiciones farmaceuticas y metodos de uso de los mismos.
ATE300255T1 (de) *	2000-10-16	2005-08-15	Conor Medsystems Inc	Expandierbare medizinische vorrichtung zum zuführen eines heilmittels
EP1423107B1 (en) *	2001-03-23	2012-05-09	Luitpold Pharmaceuticals, Inc.	Fatty alcohol drug conjugates
JP2005500988A (ja)	2001-03-23	2005-01-13	ルイトポルド・ファーマシューティカルズ・インコーポレーテッド	脂肪族アミン薬物複合体
EP2316468A1 (en)	2002-02-22	2011-05-04	Shire LLC	Delivery system and methods for protecting and administering dextroamphetamine
DE602005027466D1 (de)	2004-07-27	2011-05-26	Gilead Sciences Inc	Nukleosid phosphonat konjugate als anti hiv mittel
US20080269161A1 (en) *	2005-01-20	2008-10-30	Seth Perry	Compositions and Methods Relating to Mitochondrial Hyperpolarization in Neurological Disease
US20090081318A1 (en) *	2005-12-23	2009-03-26	Gelbard Harris A	Treatment of neuroads using inhibitors of glycogen synthase kinase (gsk)-3
BRPI0710177A2 (pt) *	2006-04-19	2012-05-29	Abbott Gmbh & Co Kg	arilsulfonas heterocìclicas adequadas para tratar distúrbios que respondem à modulação do receptor 5ht6 de serotonina
DK2364314T3 (da)	2008-12-09	2014-05-12	Gilead Sciences Inc	Modulatorer af toll-lignende receptorer
US20110223131A1 (en)	2010-02-24	2011-09-15	Gilead Sciences, Inc.	Antiviral compounds
CN106232073B (zh)	2014-02-28	2020-11-03	阿坦斯医疗保健产品公司	具有多层折叠吸收芯的吸收性用品
WO2016001907A1 (en)	2014-07-02	2016-01-07	Prendergast Patrick T	Mogroside iv and mogroside v as agonist/stimulator/un-blocking agent for toll-like receptor 4 and adjuvant for use in human/animal vaccine and to stimulate immunity against disease agents.
TWI733652B (zh)	2014-07-11	2021-07-21	美商基利科學股份有限公司	用於治療ＨＩＶ之ｔｏｌｌ樣受體調節劑
WO2017048727A1 (en)	2015-09-15	2017-03-23	Gilead Sciences, Inc.	Modulators of toll-like recptors for the treatment of hiv
US12303369B2 (en)	2016-12-14	2025-05-20	Attends Healthcare Products, Inc.	Absorbent laminates, absorbent cores and disposable articles utilizing the absorbent laminates, and related methods
US11744748B2 (en)	2018-05-28	2023-09-05	Attends Healthcare Products, Inc.	Dryness layer laminate for absorbent articles

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP0428849A3 (en) *	1989-09-28	1991-07-31	Hoechst Aktiengesellschaft	Retroviral protease inhibitors
IS2334B (is) *	1992-09-08	2008-02-15	Vertex Pharmaceuticals Inc., (A Massachusetts Corporation)	Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
AU5748194A (en) *	1992-12-11	1994-07-04	Vertex Pharmaceuticals Incorporated	Mannitol derivatives and their use as inhibitors of aspartyl protease

1995
- 1995-12-05 US US08/567,199 patent/US5646180A/en not_active Expired - Lifetime
1996
- 1996-05-12 UA UA98073527A patent/UA61902C2/uk unknown
- 1996-12-03 ZA ZA9610139A patent/ZA9610139B/xx unknown
- 1996-12-05 AT AT96942917T patent/ATE279922T1/de not_active IP Right Cessation
- 1996-12-05 HU HU9903673A patent/HUP9903673A3/hu unknown
- 1996-12-05 CN CN96198816A patent/CN1203530A/zh active Pending
- 1996-12-05 KR KR1019980704028A patent/KR19990071750A/ko not_active Withdrawn
- 1996-12-05 WO PCT/US1996/019447 patent/WO1997020554A1/en not_active Ceased
- 1996-12-05 AP APAP/P/1998/001340A patent/AP864A/en active
- 1996-12-05 ES ES96942917T patent/ES2231828T3/es not_active Expired - Lifetime
- 1996-12-05 NZ NZ324603A patent/NZ324603A/xx unknown
- 1996-12-05 EP EP96942917A patent/EP0866696B1/en not_active Expired - Lifetime
- 1996-12-05 DE DE69633680T patent/DE69633680T2/de not_active Expired - Fee Related
- 1996-12-05 PT PT96942917T patent/PT866696E/pt unknown
- 1996-12-05 AU AU11486/97A patent/AU722850B2/en not_active Ceased
- 1996-12-05 RU RU98112594/14A patent/RU2203658C2/ru not_active IP Right Cessation
- 1996-12-05 CZ CZ19981708A patent/CZ291994B6/cs not_active IP Right Cessation
- 1996-12-05 JP JP9521449A patent/JP2000501713A/ja active Pending
- 1996-12-05 PL PL96327061A patent/PL187747B1/pl not_active IP Right Cessation
- 1996-12-05 BR BR9611861A patent/BR9611861A/pt not_active Application Discontinuation
- 1996-12-05 CA CA002238471A patent/CA2238471A1/en not_active Abandoned
1998
- 1998-05-29 OA OA9800067A patent/OA10691A/en unknown
- 1998-06-04 NO NO19982556A patent/NO317837B1/no unknown

Also Published As

Publication number	Publication date
AP864A (en)	2000-08-11
DE69633680T2 (de)	2006-02-23
NO982556L (no)	1998-06-04
BR9611861A (pt)	1999-05-18
US5646180A (en)	1997-07-08
KR19990071750A (ko)	1999-09-27
AU722850B2 (en)	2000-08-10
JP2000501713A (ja)	2000-02-15
HUP9903673A3 (en)	2000-08-28
DE69633680D1 (de)	2004-11-25
RU2203658C2 (ru)	2003-05-10
AU1148697A (en)	1997-06-27
CZ170898A3 (cs)	1998-09-16
WO1997020554A1 (en)	1997-06-12
HUP9903673A2 (hu)	2000-03-28
UA61902C2 (en)	2003-12-15
ES2231828T3 (es)	2005-05-16
CN1203530A (zh)	1998-12-30
ATE279922T1 (de)	2004-11-15
CZ291994B6 (cs)	2003-07-16
EP0866696A1 (en)	1998-09-30
AP9801340A0 (en)	1998-09-30
NO317837B1 (no)	2004-12-20
EP0866696B1 (en)	2004-10-20
CA2238471A1 (en)	1997-06-12
PT866696E (pt)	2005-03-31
NO982556D0 (no)	1998-06-04
NZ324603A (en)	2000-08-25
ZA9610139B (en)	1997-06-17
PL327061A1 (en)	1998-11-23
PL187747B1 (pl)	2004-09-30

Publication	Publication Date	Title
OA10691A (en)	2001-05-04	Treatment of the cns effects of hiv with vx-478 alone or in combination with azt or 3tc
EP1637528B1 (en)	2010-09-01	Oxygenated-heterocycle containing sulfonamide inhibitors of aspartyl protease
JP3046357B2 (ja)	2000-05-29	アスパルチルプロテアーゼ阻害因子であるｔｈｆ含有スルホンアミド類
WO1994013629A1 (en)	1994-06-23	Mannitol derivatives and their use as inhibitors of aspartyl protease
HK1092791B (en)	2011-07-08	Oxygenated-heterocycle containing sulfonamide inhibitors of aspartyl protease
MXPA97008055A (en)	1998-01-01	Consistent aspartile protease inhibitors ensulfonamide containing oxygen heterocicle
HK1042892A1 (en)	2002-08-30	Oxygenated-heterocycle containing sulfonamide inhibitors of aspartyl protease
MXPA00006315A (en)	2001-07-03	Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors
HK1009811B (en)	2002-12-20	Oxygenated-heterocycle containing sulfonamide inhibitors of aspartyl protease
CA2302144A1 (en)	2000-09-30	Hydroxyphenyl derivatives with hiv integrase inhibitory properties