Patent classifications
C07D213/71
METHOD FOR PRODUCING PENTAFLUOROSULFANYL GROUP-CONTAINING ARYL COMPOUND
The present invention provides a production method capable of efficiently synthesizing an SF.sub.5 group-containing compound, or the like. The present invention is a method for synthesizing an SF.sub.5 group-containing compound represented by the general formula (1) from a thioaryl compound represented by the general formula (2) [A.sup.1 is an aryl group or a heteroaryl group; G.sup.1 is SH, SCN, SF.sub.3, SSR.sup.1, SCOR.sup.2, SR.sup.3, SF.sub.2R.sup.4, SSi(R.sup.5).sub.3, SPO(R.sup.6).sub.2, (N-phthalimidyl)thio group, or a thianthrenium group (R.sup.1 is an aryl group or a heteroaryl group; R.sup.2 and R.sup.5 are an aryl group, a heteroaryl group, an alkyl group, or an alkenyl group; R.sup.3 and R.sup.4 are an alkyl group or an alkenyl group, R.sup.6 is an aryloxy group, a heteroaryloxy group, an alkyloxy group, or an alkenyloxy group)].
[Chemical Formula 1]
A.sup.1G.sup.1(2)
A.sup.1SF.sub.5(1)
METHOD FOR PRODUCING PENTAFLUOROSULFANYL GROUP-CONTAINING ARYL COMPOUND
The present invention provides a production method capable of efficiently synthesizing an SF.sub.5 group-containing compound, or the like. The present invention is a method for synthesizing an SF.sub.5 group-containing compound represented by the general formula (1) from a thioaryl compound represented by the general formula (2) [A.sup.1 is an aryl group or a heteroaryl group; G.sup.1 is SH, SCN, SF.sub.3, SSR.sup.1, SCOR.sup.2, SR.sup.3, SF.sub.2R.sup.4, SSi(R.sup.5).sub.3, SPO(R.sup.6).sub.2, (N-phthalimidyl)thio group, or a thianthrenium group (R.sup.1 is an aryl group or a heteroaryl group; R.sup.2 and R.sup.5 are an aryl group, a heteroaryl group, an alkyl group, or an alkenyl group; R.sup.3 and R.sup.4 are an alkyl group or an alkenyl group, R.sup.6 is an aryloxy group, a heteroaryloxy group, an alkyloxy group, or an alkenyloxy group)].
[Chemical Formula 1]
A.sup.1G.sup.1(2)
A.sup.1SF.sub.5(1)
BIVALENT LINKERS AND CONJUGATES THEREOF
Bivalent linkers to be included in or for preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates are described.
BIVALENT LINKERS AND CONJUGATES THEREOF
Bivalent linkers to be included in or for preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates are described.
BENZAMIDE COMPOUND AND PREPARATION METHOD, USE, AND PHARMACEUTICAL COMPOSITION THEREOF
The present invention relates to a benzamide compound and a preparation method, use and pharmaceutical composition thereof. The benzamide compound represented by formula (I) is a STAT3 inhibitor, and can be used to prevent and/or treat a disease related to STAT3 activity, such as a tumor, autoimmune disease, renal disease, cardiovascular disease, inflammation, metabolic/endocrine dysfunction, and neurological disease.
##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##
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##
Charged ion channel blockers and methods for use
The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: ##STR00001##
The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:
##STR00001## or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
COMPOSITIONS AND METHODS OF MODULATING 15-PGDH ACTIVITY
Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.