C07D253/06

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.

Substituted pyridazines and 1,2,4-triazines as prostacyclin receptor modulators

Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. ##STR00001##
Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

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.

6-MEMBERED HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

A compound represented by Formula (I):

Chemical Formula 1

##STR00001##

wherein
Chemical Formula 2

##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
Chemical Formula 3

##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 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):

Chemical Formula 1

##STR00001##

wherein
Chemical Formula 2

##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
Chemical Formula 3

##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 is an integer from 0 to 3,
or a pharmaceutically acceptable salt thereof.

Inhibitors of creatine transport and uses thereof
10717704 · 2020-07-21 · ·

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

Inhibitors of creatine transport and uses thereof
10717704 · 2020-07-21 · ·

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

Heterocyclic compound

Provided is a heterocyclic compound that may have a GCN2 inhibitory action, and is expected to be useful for the prophylaxis or treatment of GCN2 associated diseases including cancer and the like. A compound represented by the formula (I): ##STR00001##
wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

Heterocyclic compound

Provided is a heterocyclic compound that may have a GCN2 inhibitory action, and is expected to be useful for the prophylaxis or treatment of GCN2 associated diseases including cancer and the like. A compound represented by the formula (I): ##STR00001##
wherein each symbol is as described in the DESCRIPTION, or a salt thereof.