The present disclosure provides a tyrosine kinase inhibitor having the general formula (I).

##STR00001## R1 is C.sub.1-C.sub.6 alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, mono-substituted phenyl, poly-substituted phenyl, trifluoromethyl, 2,2,2-trifluoroethyl, CH.sub.3O(CH.sub.2)n-,

##STR00002##

R being methyl, ethyl, isopropyl, trifluoromethyl, 2,2,2-trifluoroethyl, cyclopropyl, acetyl or acryloyl, and n being an integer from 1 to 6. R2 and R3 are respectively halogen, hydrogen, amino, substituted amino, cyano, hydroxyl, sulfonic acid group, sulfonamide, trifluoromethyl, 2,2,2-trifluoroethyl, methyl, methoxy or ethynyl. R2 and R3 are in an ortho, para or meta position. Y is NH, O, S or Z—N, where Z is methyl, ethyl, isopropyl, trifluoromethyl, 2,2,2-trifluoroethyl or cyclopropyl. X is Cl, Br or F.

The present disclosure provides a tyrosine kinase inhibitor having the general formula (I).

##STR00001## R1 is C.sub.1-C.sub.6 alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, mono-substituted phenyl, poly-substituted phenyl, trifluoromethyl, 2,2,2-trifluoroethyl, CH.sub.3O(CH.sub.2)n-,

##STR00002##

R being methyl, ethyl, isopropyl, trifluoromethyl, 2,2,2-trifluoroethyl, cyclopropyl, acetyl or acryloyl, and n being an integer from 1 to 6. R2 and R3 are respectively halogen, hydrogen, amino, substituted amino, cyano, hydroxyl, sulfonic acid group, sulfonamide, trifluoromethyl, 2,2,2-trifluoroethyl, methyl, methoxy or ethynyl. R2 and R3 are in an ortho, para or meta position. Y is NH, O, S or Z—N, where Z is methyl, ethyl, isopropyl, trifluoromethyl, 2,2,2-trifluoroethyl or cyclopropyl. X is Cl, Br or F.

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, ##STR00001##
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, ##STR00001##
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

The present invention relates to compounds of Formulae (I) and (II) as defined herein, and salts and solvates thereof. ##STR00001##
The present invention also relates to pharmaceutical compositions comprising compounds of Formulae (I) and (II), and to the use of compounds of Formulae (I) and (II) in the treatment or prevention of filarial worm infection, as well as other diseases or conditions in which filarial worm infection is implicated.

The present invention relates to compounds of Formulae (I) and (II) as defined herein, and salts and solvates thereof. ##STR00001##
The present invention also relates to pharmaceutical compositions comprising compounds of Formulae (I) and (II), and to the use of compounds of Formulae (I) and (II) in the treatment or prevention of filarial worm infection, as well as other diseases or conditions in which filarial worm infection is implicated.

The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H-pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one(ibrutinib) and its synthesis intermediates.

##STR00001##

The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof. ##STR00001##