Disclosed am compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and am useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

Disclosed am compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and am useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.

This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).

The presently-disclosed subject matter includes azetidine-substituted fluorescent compounds, where the compounds may be used as probes, dyes, tags, and the like. The presently-disclosed subject matter also includes kits comprising the same as well as methods for using the same to detect a target substance.

The presently-disclosed subject matter includes azetidine-substituted fluorescent compounds, where the compounds may be used as probes, dyes, tags, and the like. The presently-disclosed subject matter also includes kits comprising the same as well as methods for using the same to detect a target substance.

The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof: (I), wherein R1 and R2 represent hydrogen or deuterium; R3 represents hydrogen, COOH or OH; R3 and R3 represent hydrogen, methyl, methoxy, chlorine, fluorine or cyano; R4 and R4 represent hydrogen or fluorine; R5 represents hydrogen, fluorine or (C.sub.1-C.sub.3)alkyl; R6 represents phenyl, fused phenyl, bicyclic group comprising 5 to 12 carbon atoms, heteroaryl group comprising 2 to 9 carbon atoms and comprising from 1 to 3 heteroatoms, cycloalkyl group comprising 3 to 7 carbon atoms, (C.sub.3-C.sub.6)cycloalkyl(C.sub.1-C.sub.3)alkyl group, 4 to 7 membered-heterocycloalkyl group comprising 1 or 2 heteroatoms, (C.sub.1-C.sub.6)alkyl, and phenyl(C.sub.1-C.sub.2)alkyl group; X represents CH.sub.2, O or S; Y represents CH, N or CR, wherein R represents (C.sub.1-C.sub.3)alkyl, halogen, cyano, or (C.sub.1-C.sub.3)fluoroalkyl; R7 represents (C.sub.1-C.sub.3)alkyl, halogen atom, cyano, or (C.sub.1-C.sub.3)fluoroalkyl; R8 represents hydrogen or fluorine; R9 represents hydrogen, (C.sub.1-C.sub.3)alkyl or a cyclopropyl; n is 0, 1 or 2; and m is 0 or 1. Further disclosed are process for preparing the same, pharmaceutical compositions comprising them as well as said compounds of formula (I) for use as an inhibitor and degrader of estrogen receptors, in particular in the treatment of ovulatory dysfunction, cancer, endometriosis, osteoporosis, benign prostatic hypertrophy or inflammation.

##STR00001##

The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof: (I), wherein R1 and R2 represent hydrogen or deuterium; R3 represents hydrogen, COOH or OH; R3 and R3 represent hydrogen, methyl, methoxy, chlorine, fluorine or cyano; R4 and R4 represent hydrogen or fluorine; R5 represents hydrogen, fluorine or (C.sub.1-C.sub.3)alkyl; R6 represents phenyl, fused phenyl, bicyclic group comprising 5 to 12 carbon atoms, heteroaryl group comprising 2 to 9 carbon atoms and comprising from 1 to 3 heteroatoms, cycloalkyl group comprising 3 to 7 carbon atoms, (C.sub.3-C.sub.6)cycloalkyl(C.sub.1-C.sub.3)alkyl group, 4 to 7 membered-heterocycloalkyl group comprising 1 or 2 heteroatoms, (C.sub.1-C.sub.6)alkyl, and phenyl(C.sub.1-C.sub.2)alkyl group; X represents CH.sub.2, O or S; Y represents CH, N or CR, wherein R represents (C.sub.1-C.sub.3)alkyl, halogen, cyano, or (C.sub.1-C.sub.3)fluoroalkyl; R7 represents (C.sub.1-C.sub.3)alkyl, halogen atom, cyano, or (C.sub.1-C.sub.3)fluoroalkyl; R8 represents hydrogen or fluorine; R9 represents hydrogen, (C.sub.1-C.sub.3)alkyl or a cyclopropyl; n is 0, 1 or 2; and m is 0 or 1. Further disclosed are process for preparing the same, pharmaceutical compositions comprising them as well as said compounds of formula (I) for use as an inhibitor and degrader of estrogen receptors, in particular in the treatment of ovulatory dysfunction, cancer, endometriosis, osteoporosis, benign prostatic hypertrophy or inflammation.

##STR00001##

A method for preparing an ophthalmic device for slowing, inhibiting or preventing myopia progression involves (a) soaking an ophthalmic device in one or more first solvent solutions to swell the ophthalmic device; (b) soaking the swelled ophthalmic device in one or more second solvents solutions comprising one or more red-light blocking compounds blocking greater than about 5% to about 25% of red-light transmission through the ophthalmic device at a wavelength of from about 550 nanometers (nm) to about 800 nm to de-swell the swelled ophthalmic device and entrap the one or more red-light blocking compounds in the de-swelled ophthalmic device; and (c) sterilizing the de-swelled ophthalmic device.

A method for preparing an ophthalmic device for slowing, inhibiting or preventing myopia progression involves (a) soaking an ophthalmic device in one or more first solvent solutions to swell the ophthalmic device; (b) soaking the swelled ophthalmic device in one or more second solvents solutions comprising one or more red-light blocking compounds blocking greater than about 5% to about 25% of red-light transmission through the ophthalmic device at a wavelength of from about 550 nanometers (nm) to about 800 nm to de-swell the swelled ophthalmic device and entrap the one or more red-light blocking compounds in the de-swelled ophthalmic device; and (c) sterilizing the de-swelled ophthalmic device.