C07D253/06

1,2,4-TRIAZIN-3(2H)-ONE COMPOUNDS FOR THE TREATMENT OF HYPERPROLIFERATIVE DISEASES

The present invention includes name compounds of general formula (I): (I) in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, methods for their preparation, pharmaceutical compositions and combinations comprising said compounds, and their use for the treatment of hyperproliferative diseases.

##STR00001##

CYANOTRIAZINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF
20230312527 · 2023-10-05 ·

A compound represented by structural formula (I) and a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt thereof, can be used for treating diseases such as obesity, hyperlipidemia, hypercholesterolemia, and diabetes and also for treating other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other related disorders and diseases

##STR00001##

Saturated-ring-fused dihydropyrimidinone or dihydrotriazinone compounds and pharmaceutical use thereof

The present invention relates to saturated-ring-fused dihydropyrimidinone or dihydrotriazinone compounds, or pharmaceutically acceptable salts having RORγ antagonist activity, pharmaceutical compositions comprising the same, and pharmaceutical use thereof. A compound of Formula [I] or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and pharmaceutical use thereof are provided: ##STR00001## wherein each substituent is defined as defined in the description.

Compositions and methods for stabilizing benzothiazole luciferin analogs

Disclosed herein are compositions and methods for stabilizing a benzothiazole luciferin analog such as D-luciferin and 6-amino-D-luciferin. The compositions may include the benzothiazole luciferin analog, a thionucleobase compound of formula (I), and a liquid medium, in which the thionucleobase is present in an amount effective to stabilize the luminogenic composition against decomposition. The methods provided herein may stabilize the benzothiazole luciferin analog against decomposition by contacting the benzothiazole luciferin analog with an effective amount of the thionucleobase compound in the presence of a liquid medium. Also provided herein is a kit containing the composition.

Compositions and methods for stabilizing benzothiazole luciferin analogs

Disclosed herein are compositions and methods for stabilizing a benzothiazole luciferin analog such as D-luciferin and 6-amino-D-luciferin. The compositions may include the benzothiazole luciferin analog, a thionucleobase compound of formula (I), and a liquid medium, in which the thionucleobase is present in an amount effective to stabilize the luminogenic composition against decomposition. The methods provided herein may stabilize the benzothiazole luciferin analog against decomposition by contacting the benzothiazole luciferin analog with an effective amount of the thionucleobase compound in the presence of a liquid medium. Also provided herein is a kit containing the composition.

6-MEMBERED HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

A compound represented by Formula (I):

##STR00001##

wherein

##STR00002##

or the like
Y.sup.1 is O or the like; Z.sup.1 is C(R.sup.4) or N; Z.sup.2a is C(R.sup.5a) or the like; Z.sup.3a is C(R.sup.6) or the like; R.sup.4, R.sup.5a and R.sup.6 are each independently a hydrogen atom or the like; R.sup.1 is substituted or unsubstituted aromatic carbocyclyl or the like; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are each independently a hydrogen atom or the like; X is N(R.sup.7a) or the like; R.sup.7a is a hydrogen atom or the like; R.sup.3 is

##STR00003##

or the like
Ring B is a 6-membered aromatic carbocycle or the like; R.sup.9a and R.sup.10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p 1 is an integer from 0 to 3,
or a pharmaceutically acceptable salt thereof.

6-MEMBERED HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

A compound represented by Formula (I):

##STR00001##

wherein

##STR00002##

or the like
Y.sup.1 is O or the like; Z.sup.1 is C(R.sup.4) or N; Z.sup.2a is C(R.sup.5a) or the like; Z.sup.3a is C(R.sup.6) or the like; R.sup.4, R.sup.5a and R.sup.6 are each independently a hydrogen atom or the like; R.sup.1 is substituted or unsubstituted aromatic carbocyclyl or the like; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are each independently a hydrogen atom or the like; X is N(R.sup.7a) or the like; R.sup.7a is a hydrogen atom or the like; R.sup.3 is

##STR00003##

or the like
Ring B is a 6-membered aromatic carbocycle or the like; R.sup.9a and R.sup.10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p 1 is an integer from 0 to 3,
or a pharmaceutically acceptable salt thereof.

6-membered heterocyclic derivatives and pharmaceutical composition comprising the same

A compound represented by Formula (I): ##STR00001##
wherein ##STR00002##
or the like,
Y.sup.1 is O or the like; Z.sup.1 is C(R.sup.4) or N; Z.sup.2a is C(R.sup.5a) or the like; Z.sup.3a is C(R.sup.6) or the like; R.sup.4, R.sup.5a and R.sup.6 are each independently a hydrogen atom or the like; R.sup.1 is substituted or unsubstituted aromatic carbocyclyl or the like; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are each independently a hydrogen atom or the like; X is N(R.sup.7a) or the like; R.sup.7a is a hydrogen atom or the like; R.sup.3 is ##STR00003##
or the like,
Ring B is a 6-membered aromatic carbocycle or the like; R.sup.9a and R.sup.10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p1 is an integer from 0 to 3,
or a pharmaceutically acceptable salt thereof.

6-membered heterocyclic derivatives and pharmaceutical composition comprising the same

A compound represented by Formula (I): ##STR00001##
wherein ##STR00002##
or the like,
Y.sup.1 is O or the like; Z.sup.1 is C(R.sup.4) or N; Z.sup.2a is C(R.sup.5a) or the like; Z.sup.3a is C(R.sup.6) or the like; R.sup.4, R.sup.5a and R.sup.6 are each independently a hydrogen atom or the like; R.sup.1 is substituted or unsubstituted aromatic carbocyclyl or the like; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are each independently a hydrogen atom or the like; X is N(R.sup.7a) or the like; R.sup.7a is a hydrogen atom or the like; R.sup.3 is ##STR00003##
or the like,
Ring B is a 6-membered aromatic carbocycle or the like; R.sup.9a and R.sup.10a are each independently halogen or the like; n is an integer from 1 to 5; m is an integer from 0 to 4; and p1 is an integer from 0 to 3,
or a pharmaceutically acceptable salt thereof.

SULFONYL-STRUCTURE-CONTAINING TRIAZINONE DERIVATIVES, THEIR PREPARATION METHODS AND THEIR USES IN INSECT KILLING AND/OR BACTERIUM KILLING

The present invention belongs to the technical field of pesticides, particularly relates to sulfonyl-structure-containing triazinone derivatives, their preparation methods, and their uses in insect killing and/or bacterium killing. The sulfonyl-structure-containing triazinone derivatives are compounds represented by formula (I.sub.a) or (I.sub.b). The sulfonyl-structure-containing triazinone derivatives provided in the present invention exhibit outstanding insecticidal activity as well as bactericidal activity.