The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumors, wherein the definition of each substituent group in general formula (I) is the same as that in the description.

##STR00001##

The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumors, wherein the definition of each substituent group in general formula (I) is the same as that in the description.

##STR00001##

The present invention relates to a Palladium (II)-catalyzed C(sp.sup.3)H alkynylation of amines using picolinamide as directing group. The developed alkynylation strategy is simple, efficient, and tolerant of various ring size including five to eight member cyclic, quaternary amines, and N-heterocyclic motifs.

The present invention relates to a Palladium (II)-catalyzed C(sp.sup.3)H alkynylation of amines using picolinamide as directing group. The developed alkynylation strategy is simple, efficient, and tolerant of various ring size including five to eight member cyclic, quaternary amines, and N-heterocyclic motifs.

The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT.sub.2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT.sub.2C inverse agonistic action comprising Compound (1):

##STR00001## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-6 alkyl etc.; R.sup.5 is C.sub.4-7 alkyl or (CR.sup.8R.sup.9).sub.r-E; R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently hydrogen, fluorine or C.sub.1-6 alkyl; A is C.sub.6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C.sub.3-8 cycloalkyl or C.sub.6-10 aryl etc.; L is oxygen, sulfur or NR.sup.10; n is 1, 2 or 3; R.sup.10 is hydrogen or C.sub.1-6 alkyl etc.; and X is hydrogen or halogen etc.

The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT.sub.2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT.sub.2C inverse agonistic action comprising Compound (1):

##STR00001## or a pharmaceutically acceptable salt thereof wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-6 alkyl etc.; R.sup.5 is C.sub.4-7 alkyl or (CR.sup.8R.sup.9).sub.r-E; R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently hydrogen, fluorine or C.sub.1-6 alkyl; A is C.sub.6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C.sub.3-8 cycloalkyl or C.sub.6-10 aryl etc.; L is oxygen, sulfur or NR.sup.10; n is 1, 2 or 3; R.sup.10 is hydrogen or C.sub.1-6 alkyl etc.; and X is hydrogen or halogen etc.

The present invention relates to a Palladium (II)-catalyzed C(sp.sup.3)-H alkynylation of amines using picolinamide as directing group. The developed alkynylation strategy is simple, efficient, and tolerant of various ring size including five to eight member cyclic, quaternary amines, and N-heterocyclic motifs.

The present invention relates to a Palladium (II)-catalyzed C(sp.sup.3)-H alkynylation of amines using picolinamide as directing group. The developed alkynylation strategy is simple, efficient, and tolerant of various ring size including five to eight member cyclic, quaternary amines, and N-heterocyclic motifs.

The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumors, wherein the definition of each substituent group in general formula (I) is the same as that in the description. ##STR00001##

The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumors, wherein the definition of each substituent group in general formula (I) is the same as that in the description. ##STR00001##