C07D231/54

Aromatic derivative, preparation method for same, and medical applications thereof
11279697 · 2022-03-22 · ·

An aromatic derivative as represented by formula (I), a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising same, a preparation method therefor, and uses of the aromatic derivative and the pharmaceutically acceptable salt thereof or the pharmaceutical composition comprising same in preparing a therapeutic agent, specifically an FGFR4 tyrosine kinase inhibitor, and in preparing a medicament for treating and/or preventing neoplastic and inflammatory diseases. The substituents of formula (I) are same as defined in the description. ##STR00001##

RUBBER COMPOSITION, RUBBER MATERIAL, USE OF SAME, AND ADDITIVE

The present invention provides a rubber composition that can exhibit excellent low heat build-up, tear strength, and durability; and a rubber composition having excellent low heat build-up, tear strength, and durability, by incorporating a compound represented by the following formula (1) or (2), or a salt of the compound.

##STR00001##

In the formula (1), R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are the same or different, and each represents a hydrogen atom, an alkyl group, or the like; R.sub.3 and R.sub.4 may be taken together to form an alkylidene group, and any two of R.sub.2, R.sub.3, and R.sub.4 may be taken together to form an alkylene group; and each of these groups may have one or more substituents.

##STR00002##

In the formula (2), R.sub.5, R.sub.7, and R.sub.8 are the same or different, and each represents a hydrogen atom or an amino group; and R.sub.6 represents an alkyl group or an aralkyl group; and each of these groups may have one or more substituents.

INDENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION

Compounds of formula (I): wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b and R.sup.5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

INDENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION

Compounds of formula (I): wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b and R.sup.5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

PYRAZOLE AND IMIDAZOLE COMPOUNDS FOR INHIBITION OF IL-17 AND RORGAMMA

Disclosed herein are compounds of the formula: as well as analogs thereof, wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used to modulate the activity of IL-17 and RORγ. Also provided are methods of administering compounds and composition provided herein to a patient in need thereof, for example, for the treatment or prevention of diseases or disorders associated with inflammation or for autoimmune disorders.

##STR00001##

PYRAZOLE AND IMIDAZOLE COMPOUNDS FOR INHIBITION OF IL-17 AND RORGAMMA

Disclosed herein are compounds of the formula: as well as analogs thereof, wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used to modulate the activity of IL-17 and RORγ. Also provided are methods of administering compounds and composition provided herein to a patient in need thereof, for example, for the treatment or prevention of diseases or disorders associated with inflammation or for autoimmune disorders.

##STR00001##

Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto

Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. 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). ##STR00001##

Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto

Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. 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). ##STR00001##

COMPOSITIONS AND METHODS FOR MODULATING FARNESOID X RECEPTORS

The present invention relates to compounds of Formula I,

##STR00001##

a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).

COMPOSITIONS AND METHODS FOR MODULATING FARNESOID X RECEPTORS

The present invention relates to compounds of Formula I,

##STR00001##

a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).