Patent classifications
C07D213/82
Process of making CFTR modulators
- Paul Angell ,
- John E. Cochran ,
- Benjamin J. Littler ,
- David Siesel ,
- Armando Urbina ,
- Corey Don ANDERSON ,
- Jeremy J. Clemens ,
- Thomas Cleveland ,
- Timothy Richard Coon ,
- Bryan Frieman ,
- Peter Grootenhuis ,
- Sara Sabina Hadida Ruah ,
- Jason McCartney ,
- Mark Thomas Miller ,
- Prasuna Paraselli ,
- Fabrice Pierre ,
- Sara E. Swift ,
- Jinglan Zhou
The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof. ##STR00001##
Process of making CFTR modulators
- Paul Angell ,
- John E. Cochran ,
- Benjamin J. Littler ,
- David Siesel ,
- Armando Urbina ,
- Corey Don ANDERSON ,
- Jeremy J. Clemens ,
- Thomas Cleveland ,
- Timothy Richard Coon ,
- Bryan Frieman ,
- Peter Grootenhuis ,
- Sara Sabina Hadida Ruah ,
- Jason McCartney ,
- Mark Thomas Miller ,
- Prasuna Paraselli ,
- Fabrice Pierre ,
- Sara E. Swift ,
- Jinglan Zhou
The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof. ##STR00001##
TRIARYL COMPOUNDS FOR TREATMENT OF PD-L1 DISEASES
Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I)
##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.3, R.sup.3a, R.sup.4, R.sup.6, R.sup.7, R.sup.8, A, Z, X.sup.1 and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
SMYD Inhibitors
The present disclosure provides carboxamides and sulfonamides having Formula (I); and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.
##STR00001##
SMYD Inhibitors
The present disclosure provides carboxamides and sulfonamides having Formula (I); and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.
##STR00001##
MODULATORS OF HSD17B13 AND METHODS OF USE THEREOF
The disclosure relates to compounds and pharmaceutical compositions capable of modulating the hydroxysteroid 17-beta dehydrogenase (HSD17B) family member proteins including inhibiting the HSD17B member proteins, e.g. HSD17B13. The disclosure further relates to methods of treating liver diseases, disorders, or conditions with the compounds and pharmaceutical compositions disclosed herein, in which the HSD17B family member protein plays a role.
MODULATORS OF HSD17B13 AND METHODS OF USE THEREOF
The disclosure relates to compounds and pharmaceutical compositions capable of modulating the hydroxysteroid 17-beta dehydrogenase (HSD17B) family member proteins including inhibiting the HSD17B member proteins, e.g. HSD17B13. The disclosure further relates to methods of treating liver diseases, disorders, or conditions with the compounds and pharmaceutical compositions disclosed herein, in which the HSD17B family member protein plays a role.
COMPOUND AND COMPOSITION AS PDGF RECEPTOR KINASE INHIBITOR
An object of the present invention is to provide a compound having a PDGF receptor kinase inhibitory activity.
Examples of the present invention may include, for example, a compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof.
##STR00001##
The compound of the present invention has an inhibitory activity against the PDGF receptor kinase. In addition, since the compound of the present invention has an inhibitory activity against the PDGF receptor kinase, it is useful as a therapeutic agent for respiratory diseases, cancers, smooth muscle proliferative diseases, vasoproliferative diseases, autoimmune/inflammatory diseases, metabolic diseases, vasoocclusive diseases, and the like.
COMPOUND AND COMPOSITION AS PDGF RECEPTOR KINASE INHIBITOR
An object of the present invention is to provide a compound having a PDGF receptor kinase inhibitory activity.
Examples of the present invention may include, for example, a compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof.
##STR00001##
The compound of the present invention has an inhibitory activity against the PDGF receptor kinase. In addition, since the compound of the present invention has an inhibitory activity against the PDGF receptor kinase, it is useful as a therapeutic agent for respiratory diseases, cancers, smooth muscle proliferative diseases, vasoproliferative diseases, autoimmune/inflammatory diseases, metabolic diseases, vasoocclusive diseases, and the like.
METHODS OF TREATING ELEVATED PLASMA CHOLESTEROL
The present invention relates to compounds of Formula I, pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I increase significantly low density lipoprotein receptor and are useful for preventing and treating of elevated cholesterol.