The disclosure relates to a method for treating cancer comprising administering a therapeutically effective amount of an EZH2 inhibitor to a subject in need thereof, wherein the cancer is characterized by at least one cancer cell originating from a stem cell, a progenitor cell, or an immature cell and wherein the at least one cancer cell comprises one or more genetic lesion(s) that confer(s) dependence of the cancer cell on an EZH2 function. In certain embodiments, the EZH2 inhibitor of the disclosure is tazemetostat or a pharmaceutically acceptable salt thereof.

The present invention relates to a 6-(isooxazolidin-2-yl)-N-phenylpyrimidin-4-amine derivative, and a pharmaceutical composition for preventing or treating cancer comprising the compound as an effective component. The compound exhibits high inhibitory activity against an epidermal growth factor receptor (EGFR) variant, or wild-type or variants of one or more of ERBB2 and ERBB4, and thus may be usefully used in the treatment of cancers in which same are expressed. In particular, the compound exhibits excellent inhibitory activity on proliferation of lung cancer cell lines, and thus can be usefully used in the treatment of lung cancer.

The invention relates to the novel products of formula (I): ##STR00001##
with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH.sub.2).sub.m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO.sub.2—Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)═N—ORc, —CO.sub.2Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF.sub.3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH.sub.3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is ##STR00002##
and the isomer of configuration R,R ##STR00003##
these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.

The invention relates to the novel products of formula (I): ##STR00001##
with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH.sub.2).sub.m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO.sub.2—Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)═N—ORc, —CO.sub.2Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF.sub.3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH.sub.3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is ##STR00002##
and the isomer of configuration R,R ##STR00003##
these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.

The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).

The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).

Methods for treating chronic obstructive pulmonary disease (COPD) in a patient are disclosed. In the methods, a patient having COPD is selected for treatment based on the patient's peak inspiratory flow rate (PIFR) and percent predicted force expiratory volume in one second (FEV.sub.1); and a bronchodilator is administered to the selected patient using a nebulizer. Administration of a bronchodilator to patients having low PIFR and a percent predicted FEV.sub.1 less than 50 percent using a nebulizer as the inhalation delivery device provides significantly greater improvements in trough FEV.sub.1 and trough forced vital capacity (FVC) compared to administration of a bronchodilator to such patients using a dry powder inhaler.

Compositions and methods for treating depression, anxiety and/or circadian rhythm sleep disorders using deuterium oxide and various compounds thereof.

Compositions and methods for treating depression, anxiety and/or circadian rhythm sleep disorders using deuterium oxide and various compounds thereof.

The present invention is relates to a compound of formula (I),

##STR00001##

wherein
X.sup.1, X.sup.2 and X.sup.3 are, independently of each other, N or CH; with the proviso that at least two of X.sup.1, X.sup.2 and X.sup.3 are N;
Y is N or CH;
R.sup.1 and R.sup.2 are independently of each other (iii) a morpholinyl of formula (II)

##STR00002##

wherein the arrow denotes the bond in formula (I); and
wherein R.sup.3 and R.sup.4 are independently of each other H, C.sub.1-C.sub.3alkyl optionally substituted with one or two OH, C.sub.1-C.sub.2fluoroalkyl, C.sub.1-C.sub.2alkoxy, C.sub.1-C.sub.2alkoxyC.sub.1-C.sub.3alkyl, CN, or C(O)O—C.sub.1-C.sub.2alkyl; or R.sup.3 and R.sup.4 form together a bivalent residue —R.sup.5R.sup.6— selected from C.sub.1-C.sub.3alkylene optionally substituted with 1 to 4 F, —CH.sub.2—O—CH.sub.2—, —CH.sub.2—NH—CH.sub.2—, or any of the structures

##STR00003##

wherein the arrows denote the bonds in formula (II); or (iv) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R.sup.7; wherein R.sup.7 is independently at each occurrence C.sub.1-C.sub.3alkyl optionally substituted with one or two OH, C.sub.1-C.sub.2fluoroalkyl, C.sub.1-C.sub.2alkoxyC.sub.1-C.sub.3alkyl, C.sub.3-C.sub.6cycloalkyl; or two R.sup.7 substituents form together a bivalent residue —R.sup.8R.sup.9— selected from C.sub.1-C.sub.3alkylene optionally substituted with 1 to 4 F, —CH.sub.2—O—CH.sub.2— or —O—CH.sub.2CH.sub.2—O—;
with the proviso that at least one of R.sup.1 and R.sup.2 is a morpholinyl of formula II;
and prodrugs, metabolites, tautomers, solvates and pharmaceutically acceptable salts thereof, for use in the prevention or treatment of a neurological disorder in a subject.