C07D207/335

Pyrrole derivatives as PLK1 inhibitors

The invention provides compounds of the formula (3): ##STR00001##
or a pharmaceutically acceptable salt or tautomer thereof, wherein:
Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O;
ring X is a benzene or pyridine ring;
ring Y is a benzene, pyridine, thiophene or furan ring;
Ar.sup.1 is an optionally substituted benzene, pyridine, thiophene or furan ring;
m is 0, 1 or 2;
n is 0, 1 or 2;
R.sup.1 is selected from various substituents:
R.sup.2 is selected from hydrogen and a C.sub.1-4 hydrocarbon group;
R.sup.3 is selected from hydrogen and a C.sub.1-4 hydrocarbon group;
R.sup.4 is selected from various substituents;
R.sup.5 is selected from various substituents;
Ar.sup.2 is an optionally substituted phenyl, pyridyl or pyridone group;
R.sup.6 is a group Q.sup.1-R.sup.a—R.sup.b;
Q.sup.1 is absent or is a C.sub.1-3 saturated hydrocarbon linker;
R.sup.a is selected from O; C(O); C(O)O; CONR.sup.c; N(R.sup.c)CO; N(R.sup.c)CONR.sup.c, NR.sup.c; and SO.sub.2NR.sup.c;
R.sup.b is selected from hydrogen and various substituents;
and R.sup.7 is selected from R.sup.4. The compounds are useful in the treatment of cancers.

Method of treating or preventing Ras-mediated diseases

Disclosed are compounds, for example, a compound of formula I, ##STR00001##
wherein R, R.sub.0, R.sub.1-R.sub.8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition for example, cancer, mediated by the ras gene.

Method of treating or preventing Ras-mediated diseases

Disclosed are compounds, for example, a compound of formula I, ##STR00001##
wherein R, R.sub.0, R.sub.1-R.sub.8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition for example, cancer, mediated by the ras gene.

POLYMORPHS OF PHENYL PYRROLE AMINOGUANDIUM SALTS

The present disclosure relates to crystalline forms of N-{3-[1-(2-nitrophenyl)-1H-pyrrol-2-yl]-allylidene}-aminoguanidinium salts having high solubility. The disclosure also relates to use of said crystalline forms in medicine.

POLYMORPHS OF PHENYL PYRROLE AMINOGUANDIUM SALTS

The present disclosure relates to crystalline forms of N-{3-[1-(2-nitrophenyl)-1H-pyrrol-2-yl]-allylidene}-aminoguanidinium salts having high solubility. The disclosure also relates to use of said crystalline forms in medicine.

Pyrrole compound, method of making same, and aroma composition, food, drink and cosmetics containing same

A compound represented by the following formula (1): ##STR00001## wherein, R.sub.1 is a linear or branched alkyl group having 1 to 3 carbon atoms or a hydroxyl group; and R.sub.2 is a 1-pyrrolyl group, a 2-pyrrolyl group, or a 3-pyrrolyl group. The present invention can provide a means highly effective in contributing to savory roasting flavor and capable of imparting fragrance with natural feeling.

Pyrrole compound, method of making same, and aroma composition, food, drink and cosmetics containing same

A compound represented by the following formula (1): ##STR00001## wherein, R.sub.1 is a linear or branched alkyl group having 1 to 3 carbon atoms or a hydroxyl group; and R.sub.2 is a 1-pyrrolyl group, a 2-pyrrolyl group, or a 3-pyrrolyl group. The present invention can provide a means highly effective in contributing to savory roasting flavor and capable of imparting fragrance with natural feeling.

PYRROLE DERIVATIVES AS PLK1 INHIBITORS

The invention provides compounds of the formula (3):

##STR00001## or a pharmaceutically acceptable salt or tautomer thereof, wherein: Z is a 5-membered heteroaryl ring containing one or two nitrogen ring members and optionally one further heteroatom ring member selected from N and O; ring X is a benzene or pyridine ring; ring Y is a benzene, pyridine, thiophene or furan ring; Ar.sup.1 is an optionally substituted benzene, pyridine, thiophene or furan ring; m is 0, 1 or 2; n is 0, 1 or 2; R.sup.1 is selected from various substituents: R.sup.2 is selected from hydrogen and a C.sub.1-4 hydrocarbon group; R.sup.3 is selected from hydrogen and a C.sub.1-4 hydrocarbon group; R.sup.4 is selected from various substituents; R.sup.5 is selected from various substituents; Ar.sup.2 is an optionally substituted phenyl, pyridyl or pyridone group; R.sup.6 is a group Q.sup.1-R.sup.a—R.sup.b; Q.sup.1 is absent or is a C.sub.1-3 saturated hydrocarbon linker; R.sup.a is selected from O; C(O); C(O)O; CONR.sup.c; N(R.sup.c)CO; N(R.sup.c)CONR.sup.c, NR.sup.c; and SO.sub.2NR.sup.c; R.sup.b is selected from hydrogen and various substituents; and R.sup.b is selected from R.sup.4. The compounds are useful in the treatment of cancers.

Compound used as autophagy regulator, and preparation method therefor and uses thereof

It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators. ##STR00001##

MMPL3 INHIBITORS, COMPOSITIONS AND USES THEREOF
20220017492 · 2022-01-20 ·

The present disclosure relates generally to inhibitors of mycobacterial membrane protein MmpL3, compositions comprising the inhibitors, and methods of preparation and use thereof.