The present invention relates to pyrimidone compounds used as Lp-PLA.sub.2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R.sub.1, R.sub.2, R.sub.3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA.sub.2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA.sub.2 enzyme.

##STR00001##

The present invention relates to pyrimidone compounds used as Lp-PLA.sub.2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R.sub.1, R.sub.2, R.sub.3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA.sub.2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA.sub.2 enzyme.

##STR00001##

The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I]

##STR00001##

wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.

The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I]

##STR00001##

wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.

A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, and a heterocyclic ring, wherein ring A is selected from the group consisting of a benzene ring, a naphthalene ring, a quinoxaline ring, a thiophene ring, an indole ring, a benzothiophene ring, an imidazole ring, a quinoline ring, a quinazoline ring, and a pyridine ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A, wherein R.sup.1 and R.sup.2 are bonded to adjacent ring atoms of ring A; m represents an integer of 1 or 2; X is a halogen atom, and when m is 2, each X is the same or different; R.sup.1 and R.sup.2 are the same or different; R.sup.1 and R.sup.2 independently represent a group represented from the following groups:

—(CH.sub.2).sub.n—Y—R.sup.4

wherein Y is selected from the group consisting of O, S, SO, SO.sub.2, and Se, n represents an integer of 1 to 8, R.sup.4 represents

##STR00001##

wherein R.sup.41, R.sup.42 and R.sup.47 are the same and are a hydrogen atom

##STR00002##

A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, and a heterocyclic ring, wherein ring A is selected from the group consisting of a benzene ring, a naphthalene ring, a quinoxaline ring, a thiophene ring, an indole ring, a benzothiophene ring, an imidazole ring, a quinoline ring, a quinazoline ring, and a pyridine ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A, wherein R.sup.1 and R.sup.2 are bonded to adjacent ring atoms of ring A; m represents an integer of 1 or 2; X is a halogen atom, and when m is 2, each X is the same or different; R.sup.1 and R.sup.2 are the same or different; R.sup.1 and R.sup.2 independently represent a group represented from the following groups:

—(CH.sub.2).sub.n—Y—R.sup.4

wherein Y is selected from the group consisting of O, S, SO, SO.sub.2, and Se, n represents an integer of 1 to 8, R.sup.4 represents

##STR00001##

wherein R.sup.41, R.sup.42 and R.sup.47 are the same and are a hydrogen atom

##STR00002##

The present disclosure encompasses solid state forms of Mavacamten, in embodiments crystalline polymorphs of Mavacamten, processes for preparation thereof, and pharmaceutical compositions thereof.

Disclosed are a compound and a pharmaceutically acceptable salt thereof, which can be used, by means of a chemical small molecule which targets both UHFR1 and HDAC1, or a pharmaceutically acceptable salt thereof, as corresponding inhibitors or drugs for treating diseases, and are used for treating myelodysplastic syndrome, psoriasis, scar hyperplasia, prostate or breast hyperplasia, hematologic neoplasms and solid cancers alone or combined with other methods. Same have a good therapeutic effect.

Disclosed are a compound and a pharmaceutically acceptable salt thereof, which can be used, by means of a chemical small molecule which targets both UHFR1 and HDAC1, or a pharmaceutically acceptable salt thereof, as corresponding inhibitors or drugs for treating diseases, and are used for treating myelodysplastic syndrome, psoriasis, scar hyperplasia, prostate or breast hyperplasia, hematologic neoplasms and solid cancers alone or combined with other methods. Same have a good therapeutic effect.

The invention relates to the field of pesticide technology, and in particular a type of carboxylic acid derivative-substituted iminoaryl compound, preparation method, herbicidal composition and use thereof. The compound, as shown in general formula I:

##STR00001## wherein, Q represents

##STR00002##

Y represents halogen, haloalkyl or cyano; Z represents halogen; M represents CH or N; W represents OX.sub.5, SX.sub.5 or N(X.sub.5).sub.2; X represents —CX.sub.1X.sub.2-(alkyl).sub.n-, -alkyl-CX.sub.1X.sub.2-(alkyl).sub.n- or —(CH.sub.2).sub.r—; X.sub.3 and X.sub.4 each independently represent O, S, NH or N-alkyl, etc. The compound has excellent herbicidal activity against gramineous weeds, broadleaf weeds, cyperaceae weeds and so on even at low application rates, and has high selectivity for crops.