AR050160A1 - Inhibisores heterociclicos de aspartil proteasa - Google Patents
Inhibisores heterociclicos de aspartil proteasaInfo
- Publication number
- AR050160A1 AR050160A1 ARP050102405A AR050160A1 AR 050160 A1 AR050160 A1 AR 050160A1 AR P050102405 A ARP050102405 A AR P050102405A AR 050160 A1 AR050160 A1 AR 050160A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- methods
- aspartil
- proteasa
- heterociclic
- Prior art date
Links
Classifications
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- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/88—Nitrogen atoms, e.g. allantoin
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
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- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A61K31/47—Quinolines; Isoquinolines
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Abstract
Se revelan compuestos de formula (1), o su estereoisomero, tautomero, o sal o solvato aceptable para uso farmacéutico, en la cual W es un enlace, -C(=S)-, -S(O)-, -S(O)2-, -C(=O)-, -O-, -C(R6)(R7)-, -N(R5)- o -C(=N(R5))-; X es -O-, -N(R5)- o - C(R6)(R7)-; siempre que cuando X sea -O-, U no sea -O-, -S(O)-, -S(O)2-, -C(=O)- o -C(=NR5)-; U es un enlace, -S(O)-, -S(O)2-, -C(O)-, -O-, -P(O)(OR15)-, -C(=NR5)-, -(C(R6)(R7)b- o -N(R5)-; donde b es 1 o 2; siempre que cuando W sea -S(O)-, -S(O)2-, -O-, o -N(R5)-, U no sea -S(O)-, -S(O)2-, -O-, o -N(R5)-; siempre que cuando X es -N(R5)- y W es -S(O)-, -S(O)2-, -O-, o -N(R5)-, entonces U no es un enlace; y R1, R2, R3, R4, R5, R6, y R7 son segun se definieron en la memoria descriptiva; y composiciones farmacéuticas que comprenden los compuesto de formula (1). Además se revela el método para inhibir la aspartil proteasa, y en particular, los métodos para tratar enfermedades cardiovasculares, enfermedades cognitivas y neurodegenerativas, y los métodos para inhibir el Virus de Inmunodeficiencia Humana, plasmepinas, catepsina D y enzimas protozoales. Además se revelan métodos para tratar enfermedades cognitivas y neurodegenerativas que utilizan los compuestos de formula (1) en combinacion con un inhibidor de colinesterasa o un agonista m1 o antagonista m2 muscarínico.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US11/010,772 US7592348B2 (en) | 2003-12-15 | 2004-12-13 | Heterocyclic aspartyl protease inhibitors |
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AR050160A1 true AR050160A1 (es) | 2006-10-04 |
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ARP050102405 AR050160A1 (es) | 2004-12-13 | 2005-06-13 | Inhibisores heterociclicos de aspartil proteasa |
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US (4) | US7592348B2 (es) |
EP (1) | EP1838304B1 (es) |
JP (1) | JP4968845B2 (es) |
KR (1) | KR20070106689A (es) |
CN (2) | CN101115482A (es) |
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AT (1) | ATE439835T1 (es) |
AU (1) | AU2005317204B2 (es) |
BR (1) | BRPI0519034A2 (es) |
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DE (1) | DE602005016159D1 (es) |
ES (1) | ES2330124T3 (es) |
HK (1) | HK1106430A1 (es) |
IL (1) | IL183826A0 (es) |
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