申请人:Matier L. William
公开号:US20070254950A1
公开(公告)日:2007-11-01
Compounds of the following formula are disclosed: wherein R
1
and R
2
are each independently H, W, or a phenoxyl protecting group; and R
4
is H or W, provided that at least one of R
1
, R
2
, and R
4
is W; R
3
is hydrogen, straight chain or branched C
1
-C
10
alkyl, cycloalkyl, amino, C
1
-C
10
alkoxy, —NHC(═O)Ra, or —C(═O)N(H)R
a
; R
a
is alkyl, aryl, or heterocyclyl; Z is -0-, —O(C═O)—, or NH(C═O)—, wherein when Z is -0-, R
5
is H, straight chain or branched C
1
-C
10
alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C
1
-C
10
alkyl, CI—Clo alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolsdinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with CI—Clo alkyl, C
1
-C
10
alkoxy, or halo; and W is: wherein each R
6
is independently H, straight chain or branched C
1
-C
10
alkyl, or straight chain or branched C
1
-C
10
alkoxyalkyl; and R
7
is alkyl, cycloalkyl, aryl, or aralkyl; and wherein when Z is —O(C═O)—, R
5
is straight chain or branched C
1
-C
10
alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C
1
-C
10
alkyl, CI—CIO alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, dioxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolidinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with C
1
-C
10
alkyl, C
1
-C
10
alkoxy, or halo; and W is:, wherein each R6 is independently H, straight chain or branched CI—C to alkyl, or straight chain or branched C,—C to alkoxyalkyl; and R7 is alkyl, cycloalkyl, aryl, or aralkyl; and wherein when Z is —NH(C═O)—, R5 is straight chain or branched C
1
-C
10
alkyl, cycloalkyl, cycloalkyl substituted with at least one straight or branched C
1
-C
10
alkyl, CI—CIO alkoxyalkyl, amino, benzyl, tetrahydrofuranyl, dihydrofuranyl, furanyl, morpholinyl, piperidinyl, tetrahydropyranyl, & oxolanyl, 2,2-dimethyl dioxolanyl, dioxanyl, pyrrolyl, pyrrolidinyl, tetrahydrooxazolyl, dihydrooxazolyl, phenyl, or phenyl substituted with C
1
-C
10
alkyl, C
1
-C
10
alkoxy, or halo; and W is: wherein each R6 is independently H, straight chain or branched C1-C to alkyl, or straight chain or branched C,—Clo alkoxyalkyl. Methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating patients by administration of the pharmaceutical compositions, are also disclosed.
公开了以下式子的化合物:其中R1和R2分别独立地为H,W或
苯氧基保护基;而R4为H或W,但至少其中之一为W;R3为
氢,直链或支链C1-C10烷基,
环烷基,
氨基,C1-C10烷
氧基,—NHC(═O)Ra,或—C(═O)N(H)Ra;Ra为烷基,芳基或杂环基;Z为-0-,—O(C═O)—或NH(C═O)—,其中当Z为-0-时,R5为H,直链或支链C1-C10烷基,
环烷基,至少有一个直链或支链C1-C10烷基替代的
环烷基,CI-Clo烷
氧基烷基,
氨基,
苄基,
四氢呋喃基,二
氢呋喃基,
呋喃基,
吗啉基,
哌啶基,
四氢吡喃基,二
氢二
氧杂环基,
2,2-二
甲基二
氧杂环基,二
氧杂环基,
吡咯基,
吡咯啉基,四
氢噁唑基,二
氢噁唑基,
苯基,或带有CI-Clo烷基,C1-C10烷
氧基或卤素替代的
苯基;W为:其中每个R6独立地为H,直链或支链C1-C10烷基或直链或支链C1-C10烷
氧基烷基;而R7为烷基,
环烷基,芳基或芳基烷基;当Z为—O(C═O)—时,R5为直链或支链C1-C10烷基,
环烷基,至少有一个直链或支链C1-C10烷基替代的
环烷基,CI-Clo烷
氧基烷基,
氨基,
苄基,
四氢呋喃基,二
氢呋喃基,
呋喃基,
吗啉基,
哌啶基,
四氢吡喃基,二
氢二
氧杂环基,
2,2-二
甲基二
氧杂环基,二
氧杂环基,
吡咯基,
吡咯啉基,四
氢噁唑基,二
氢噁唑基,
苯基,或带有C1-C10烷基,C1-C10烷
氧基或卤素替代的
苯基;W为:其中每个R6独立地为H,直链或支链C1-C10烷基或直链或支链C1-C10烷
氧基烷基;而R7为烷基,
环烷基,芳基或芳基烷基;当Z为—NH(C═O)—时,R5为直链或支链C1-C10烷基,
环烷基,至少有一个直链或支链C1-C10烷基替代的
环烷基,CI-Clo烷
氧基烷基,
氨基,
苄基,
四氢呋喃基,二
氢呋喃基,
呋喃基,
吗啉基,
哌啶基,
四氢吡喃基,二
氢二
氧杂环基,
2,2-二
甲基二
氧杂环基,二
氧杂环基,
吡咯基,
吡咯啉基,四
氢噁唑基,二
氢噁唑基,
苯基,或带有C1-C10烷基,C1-C10烷
氧基或卤素替代的
苯基;W为:其中每个R6独立地为H,直链或支链C1-C10烷基或直链或支链C1-C10烷
氧基烷基。还公开了制备这些化合物的方法,包括这些化合物的制药组合物以及通过给药这些制药组合物治疗患者的方法。