摘要:
The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
摘要:
The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
摘要:
1,2,8,8a-Tetrahydrocyclopropa[3]pyrrolo(3,2-e)indol-4(5H)-ones, and related compounds of formulas I and intermediate therefor II ##STR1## wherein R.sub.2, R.sub.2 ', R.sub.3, R.sub.5, R.sub.50 and X are as defined in the specification, e.g., (7bR,8aS)-1,2,8,8a-tetrahydro-7-methyl-2-[[5-(((1H-indol-2-yl)carbonyl)amino)-1H-indol-2-yl]carbonyl]cyclopropa[pyrrolo[3,2-e]indol-4(5H)-one (U-71,184), as purified, and its racemic form (U-68,415), and related compounds, are useful as ultraviolet light absorbers and as antibacterials. The lead compounds are useful as antitumor drug compounds in standard laboratory animal tests.
摘要:
Compounds which are 3-amino-pyrazole derivatives represented by formula (I) wherein R is C3–C6 cycloalkyl group optionally substituted by a straight or branched C1–C6 alkyl or arylalkyl group; R1 is a straight or branched C1–C6 alkyl, C2–C4 alkenyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl or arylalkenyl group, each of which may be optionally further substituted as indicated in the description; or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
摘要:
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof. Such compounds may be incorporated into pharmaceutical compositions which can inhibit various enzymes from the matrix metalloproteinase family.
摘要:
A compound of formula I or pharmaceutical acceptable salts thereof, ##STR1## wherein R.sub.1 is isopropyl, 2-methylbut-2yl, phenyl, benzyl, or 1H-indol-3ylmethyl; R.sub.2 is n-octyl, phenyl, or phenyl substituted with methoxy, fluoro, or bromo, are matrix metalloproteinase inhibitors.
摘要:
Compounds which are 3-amino-pyrazole derivatives represented by formula (I): where R is a C3-C6 cycloalkyl group, which may optionally be substituted by a straight or branched C1-C6 alkyl group, and R1 is a straight or branched C1-C6 alkyl group or a C2-C4 alkenyl, cycloalkyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl and arylalkenyl, which may be optionally substituted; or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
摘要:
1,2,8,8a-Tetrahydrocyclopropa[3]pyrrolo(3,2-e)indol-4(5H)-ones, and related compounds of formulas I and intermediate therefor II ##STR1## wherein R.sub.2, R.sub.2 ', R.sub.3, R.sub.5, R.sub.50 and X are as defined in the specification, e.g., (7bR,8aS)-1,2,8,8a -tetrahydro-7-methyl-2-[[5-(((1H-indol-2-yl)carbonyl)amino)-1H-indol-2-yl]carbonyl]cyclopropa[pyrrolo[3,2-e]indol-4(5H)-one (U-71,184), as purified, and its racemic form (U-68,415), and related compounds, are useful as ultraviolet light absorbers and as antibacterials. The lead compounds are useful as antitumor drug compounds in standard laboratory animal tests.
摘要:
An improved process for preparing sulfonylated indoline compounds of the formula ##STR1## via reduction of a nitrodiol of the formula ##STR2## where R.sub.1 and R.sub.3 are defined in the specification, to obtain the corresponding aminodiol ##STR3## and then the aminodiol (III) is sulfonylated and cyclized in situ to obtain the sulfonylated indoline compound (I). The substituted indoline compounds (I) are useful in overall processes for making 1,2,8,8a-cyclopropa[c]benzo[1,2-b:4,3-b']dipyrrol-4(5H)-ones which have useful light absorber, anti-bacterial and anti-tumor pharmaceutical use properties.
摘要:
The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.