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BRPI0519034A2 - compostos inibidores de aspartil protease heterocÍclicos, composiÇÕes e referidos usos - Google Patents

compostos inibidores de aspartil protease heterocÍclicos, composiÇÕes e referidos usos

Info

Publication number
BRPI0519034A2
BRPI0519034A2 BRPI0519034-7A BRPI0519034A BRPI0519034A2 BR PI0519034 A2 BRPI0519034 A2 BR PI0519034A2 BR PI0519034 A BRPI0519034 A BR PI0519034A BR PI0519034 A2 BRPI0519034 A2 BR PI0519034A2
Authority
BR
Brazil
Prior art keywords
compositions
compounds
bond
formula
aspartyl protease
Prior art date
Application number
BRPI0519034-7A
Other languages
English (en)
Inventor
Zhaoning Zhu
Brian Mckittrick
Zhong-Yue Sun
Yuanzan C Ye
Johannes H Voigt
Corey Strickland
Elizabeth M Smith
Andrew Stamford
William J Greenlee
Robert Mazzola
John Caldwell
Jared Cumming
Lingyan Wang
Yusheng Wu
Ulrich Iserloh
Tao Guo
Thuy X H Le
Kurt W Saionz
Suresh D Babu
Rachael C Hunter
Michelle L Morris
Huizhong Gu
Dawit Tadesse
Gang Qian
Original Assignee
Schering Corp
Pharmacopeia Inc
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.)
Filing date
Publication date
Application filed by Schering Corp, Pharmacopeia Inc filed Critical Schering Corp
Publication of BRPI0519034A2 publication Critical patent/BRPI0519034A2/pt

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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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    • A61K31/41—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
    • A61K31/4178—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
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    • 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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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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Abstract

COMPOSTOS INIBIDORES DE ASPARTIL PROTEASE HETEROCICLICOS, COMPOSIÇÕES E REFERIDOS USOS. São descritos os compostos da fórmula I ou um estereoisômero, tautômero, ou sal farmaceuticamente aceitável ou solvato deste, onde w é uma ligação, -C(=S)-, -S(0)-, -S(O)~ 2~-, -C(=O)-, -O-, -C(R^ 6^) (R^ 7^)-, -N(R^ 5^)- ou C(=N(R^ 5^))-; X é -O-, -N(R^ 5^)- or -C(R^ 6^)(R^ 7^)-; contanto que quando X for -O-, U não seja -O-, -S(O)-, -S(O)~ 2~-, -C(=O)- ou -C(NR^ 5^)-; U é uma ligação, -S(O)-, -S(O)~ 2~-, -C(O)-, -O-, -P(O)(OR^ 15^)-, -C (=NR^ 5^)-, -(C(R^ 6^)(R^ 7^))~ b~- ou -N(R^ 5^)-; onde b é 1 ou 2; contanto que quando W for -S(O)-, -S(O)~ 2~-, -O-, ou -N(R^ 5^)-, U não seja -S(O)-, -S(O)~ 2~-, -O-, ou - N(R^ 5^)-; contanto que quando X for -N(R^ 5^)- e W for -S(O)-, -S(O)~ 2~-, -O-, ou - N(R^ 5^)-, então U não seja uma ligação; e R¹, R², Rü R^ 4^, R^ 5^, R^ 6^, e R^ 7^ são como definido na especificação; e composições farmacêuticas compreendendo os compostos de fórmula (1). É também descrito o método de inibição de aspartil protease, e em particular, os métodos de tratar doenças cardiovasculares, doenças cognitivas e neurodegenerativas, e os métodos de inibição do Vírus da Imuno-deficiência Humana, plasmepinas, catepsina D e enzimas protozoárias. São também descritos métodos de tratar doenças cognitivas ou neurodegenerativas empregando-se os compostos de fórmula I, em combinação com um inibidor de colinesterase ou um agonista m~ 1~ ou antagonista m~ 2~ muscarínico.
BRPI0519034-7A 2004-12-13 2005-06-09 compostos inibidores de aspartil protease heterocÍclicos, composiÇÕes e referidos usos BRPI0519034A2 (pt)

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