PE20091208A1 - DERIVATIVES OF LYSINE SULFONAMIDE AS INHIBITORS OF HIV PROTEASE - Google Patents
DERIVATIVES OF LYSINE SULFONAMIDE AS INHIBITORS OF HIV PROTEASEInfo
- Publication number
- PE20091208A1 PE20091208A1 PE2008001964A PE2008001964A PE20091208A1 PE 20091208 A1 PE20091208 A1 PE 20091208A1 PE 2008001964 A PE2008001964 A PE 2008001964A PE 2008001964 A PE2008001964 A PE 2008001964A PE 20091208 A1 PE20091208 A1 PE 20091208A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- cycloalkyl
- fluoroalkyl
- amino
- hiv protease
- Prior art date
Links
- -1 OF LYSINE SULFONAMIDE Chemical class 0.000 title abstract 4
- 108091005804 Peptidases Proteins 0.000 title abstract 2
- 239000004365 Protease Substances 0.000 title abstract 2
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 229940124530 sulfonamide Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- GTCAXTIRRLKXRU-UHFFFAOYSA-N methyl carbamate Chemical compound COC(N)=O GTCAXTIRRLKXRU-UHFFFAOYSA-N 0.000 abstract 2
- HFFXLYHRNRKAPM-UHFFFAOYSA-N 2,4,5-trichloro-n-(5-methyl-1,2-oxazol-3-yl)benzenesulfonamide Chemical compound O1C(C)=CC(NS(=O)(=O)C=2C(=CC(Cl)=C(Cl)C=2)Cl)=N1 HFFXLYHRNRKAPM-UHFFFAOYSA-N 0.000 abstract 1
- 208000030507 AIDS Diseases 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 208000037357 HIV infectious disease Diseases 0.000 abstract 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 abstract 1
- 239000004472 Lysine Substances 0.000 abstract 1
- UKJLNMAFNRKWGR-UHFFFAOYSA-N cyclohexatrienamine Chemical compound NC1=CC=C=C[CH]1 UKJLNMAFNRKWGR-UHFFFAOYSA-N 0.000 abstract 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Landscapes
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
REFERIDA A UN DERIVADO DE LISINA SULFONAMIDA DE FORMULA (A), DONDE R1 ES ALQUILO C1-C6 O ALQUILO C1-C6 SUSTITUIDO CON CICLOALQUILO C3-C6; R2 ES CH(RJ)-Z; Z ES OH, NH2 O ORP; RJ ES H, ALQUILO C1-C6, FLUOROALQUILO C1-C6, ALQUILO C1-C6 SUSTITUIDO CON CICLOALQUILO C3-C5; RP ES P(O)(OH)2, P(O)(OM)2 O C(O)RQ; M ES UN METAL ALCALINO O ALCALINO TERREO; RQ ES ALQUILO C1-C6, CICLOALQUILO C3-C6, ENTRE OTROS; R3 Y R4 SON H, ALQUILO C1-C6, FLUOROALQUILO C1-C6 O ALQUILO C1-C6 SUSTITUIDO CON CICLOALQUILO C3-C5; R5 ES H, ALQUILO C1-C6, FLUOROALQUILO C1-C6, CICLOALQUILO C3-C5 O ALQUILO C1-C6 SUSTITUIDO CON CICLOALQUILO C3-C5; R5A ES H O ALQUILO C1-C6; XA ES ALQUILO C1-C6, CICLOALQUILO C3-C6, HALOALQUILO C1-C6, ENTRE OTROS; k, m Y n SON UN ENTERO DE 0 A 3; R6 ES (i), (ii), (iii), ENTRE OTROS; XB Y XC SON ALQUILO C1-C6, CICLOALQUILO C3-C6, HALOALQUILO C1-C6, ENTRE OTROS; EL SIMBOLO ASTERISCO REPRESENTA EL PUNTO DE UNION AL RESTO DEL COMPUESTO; R7 ES H, ALQUILO C1-C6, CICLOALQUILO C3-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-{(1S,5S)-5-[[4-AMINOFENIL)SULFONIL](ISOPROPIL)AMINO]-6-HIDROXI-1-METILHEXIL}-NALFA-(METOXICARBONIL)-BETA-FENIL-L-FENILALNINAMIDA, [(1S)-2-({(5S)-5-[[4-AMINOFENIL)SULFONIL]-((3S)-3-ETILBUTIL)AMINO]-6-HIDROXI-1-METILHEXIL)AMINO)-1-(DIFENILMETIL)-2-OXOETIL]CARBAMATO DE METILO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INIHIBIDORES DE LA PROTEASA DEL VIH Y SON UTILES EN EL TRATAMIENTO DE INFECCION POR VIH Y DEL SIDAREFERRED TO A LYSINE SULFONAMIDE DERIVATIVE OF FORMULA (A), WHERE R1 IS C1-C6 ALKYL OR C1-C6 ALKYL SUBSTITUTED WITH C3-C6 CYCLOALKYL; R2 IS CH (RJ) -Z; Z IS OH, NH2 OR ORP; RJ IS H, C1-C6 ALKYL, C1-C6 FLUOROALKYL, C1-C6 ALKYL REPLACED WITH C3-C5 CYCLOALKYL; RP ES P (O) (OH) 2, P (O) (OM) 2 O C (O) RQ; M IS AN ALKALINE METAL OR EARTH ALKALINE; RQ IS C1-C6 ALKYL, C3-C6 CYCLOALKYL, AMONG OTHERS; R3 AND R4 ARE H, C1-C6 ALKYL, C1-C6 FLUOROALKYL OR C1-C6 ALKYL SUBSTITUTED WITH C3-C5 CYCLOALKYL; R5 IS H, C1-C6 ALKYL, C1-C6 FLUOROALKYL, C3-C5 CYCLOALKYL OR C1-C6 ALKYL SUBSTITUTED WITH C3-C5 CYCLOALKYL; R5A IS H OR C1-C6 ALKYL; XA IS C1-C6 ALKYL, C3-C6 CYCLOALKYL, C1-C6 HALOALKYL, AMONG OTHERS; k, m AND n ARE AN INTEGER FROM 0 TO 3; R6 IS (i), (ii), (iii), AMONG OTHERS; XB AND XC ARE C1-C6 ALKYL, C3-C6 CYCLOALKYL, C1-C6 HALOALKYL, AMONG OTHERS; THE ASTERISK SYMBOL REPRESENTS THE POINT OF JOINT TO THE REST OF THE COMPOUND; R7 IS H, C1-C6 ALKYL, C3-C6 CYCLOALKYL, AMONG OTHERS. PREFERRED COMPOUNDS ARE: N - {(1S, 5S) -5 - [[4-AMINOPHENIL) SULFONIL] (ISOPROPYL) AMINO] -6-HYDROXY-1-METHYLHEXYL} -NALFA- (METOXYCARBONYL) -BETA-PHENYL-L- PHENYLALNINAMIDE, [(1S) -2 - ({(5S) -5 - [[4-AMINOPHENYL) SULFONIL] - ((3S) -3-ETHYLBUTYL) AMINO] -6-HYDROXY-1-METHYLHEXYL) AMINO) -1 - (DIPHENYLMETIL) -2-OXOETHYL] METHYL CARBAMATE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INIHIBITORS OF HIV PROTEASE AND ARE USEFUL IN THE TREATMENT OF HIV INFECTION AND AIDS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18872008P | 2008-08-12 | 2008-08-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20091208A1 true PE20091208A1 (en) | 2009-08-28 |
Family
ID=41665383
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001964A PE20091208A1 (en) | 2008-08-12 | 2008-11-24 | DERIVATIVES OF LYSINE SULFONAMIDE AS INHIBITORS OF HIV PROTEASE |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR071258A1 (en) |
| CL (1) | CL2008003492A1 (en) |
| PE (1) | PE20091208A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12083099B2 (en) | 2020-10-28 | 2024-09-10 | Accencio LLC | Methods of treating symptoms of coronavirus infection with viral protease inhibitors |
-
2008
- 2008-11-21 AR ARP080105074 patent/AR071258A1/en unknown
- 2008-11-24 PE PE2008001964A patent/PE20091208A1/en not_active Application Discontinuation
- 2008-11-24 CL CL2008003492A patent/CL2008003492A1/en unknown
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12083099B2 (en) | 2020-10-28 | 2024-09-10 | Accencio LLC | Methods of treating symptoms of coronavirus infection with viral protease inhibitors |
| US12453717B1 (en) | 2020-10-28 | 2025-10-28 | Accencio LC | Methods of treating symptoms of coronavirus infection with viral protease inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| AR071258A1 (en) | 2010-06-09 |
| CL2008003492A1 (en) | 2009-10-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |