Patent classifications
C07D213/26
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.
PROCESS FOR THE PREPARATION OF RUTHENIUM COMPLEXES
A process for the preparation of a complex of formula (I): the process comprising the step of reacting a complex of formula (II) or a complex of formula RuX.sub.3.H.sub.2O (IV) with a bidentate ligand of formula (III) wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, A, B, and X are described in the specification; the molar ratio of the complex of formula (II): the bidentate ligand of formula (III) is about 1:6 to about 1:8 or the molar ratio of the complex of formula (IV): the bidentate ligand of formula (III) is about 1:3 to about 1:4; and the process is carried out in water or a water-based solvent, wherein the water-based solvent comprises at least 60% water (by volume) and an organic solvent, at one or more temperatures in the range of about 80° C. to 110° C.
##STR00001##
BISAMIDE COMPOUND AND APPLICATION THEREOF
This disclosure provides a bisamide compound and an application thereof, where the compound has a structure as shown by general formula I:
##STR00001##
the definition of each substituent in the formula is shown in the specification. The specification also discloses use thereof as an insecticide and an animal parasite control agent.
BISAMIDE COMPOUND AND APPLICATION THEREOF
This disclosure provides a bisamide compound and an application thereof, where the compound has a structure as shown by general formula I:
##STR00001##
the definition of each substituent in the formula is shown in the specification. The specification also discloses use thereof as an insecticide and an animal parasite control agent.
Tetralin and tetrahydroquinoline compounds as inhibitors of HIF-2α
- Joel Worley BEATTY ,
- Samuel Lawrie DREW ,
- Matthew Epplin ,
- Jeremy Thomas Andre FOURNIER ,
- Balint GAL ,
- Tezcan GUNEY ,
- Karl T. Haelsig ,
- Clayton HARDMAN ,
- Steven Donald JACOB ,
- Jenna Leigh JEFFREY ,
- Jaroslaw KALISIAK ,
- Kenneth Victor LAWSON ,
- Manmohan Reddy LELETI ,
- Erick Allen LINDSEY ,
- Artur Karenovich MAILYAN ,
- Debashis MANDAL ,
- Guillaume MATA ,
- Hyunyoung Moon ,
- Jay Patrick Powers ,
- Brandon Reid ROSEN ,
- Yongli Su ,
- Anh Thu TRAN ,
- Zhang Wang ,
- Xuelei Yan ,
- Kai YU
Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.
NOVEL SULFONEUREA COMPOUNDS
The present invention relates to compounds of formula (I): wherein A, B, X, Y, R.sup.1, R.sup.4 and R.sup.7 are as defined in the specification. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3.
##STR00001##
SUBSTITUTED AMIDE COMPOUNDS USEFUL AS FARNESOID X RECEPTOR MODULATORS
Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, when Q is: (i) halo, cyano, hydroxyl, NR.sup.xR.sup.x, C(O)OH, C(O)NH.sub.2, C.sub.1-6 alkyl substiuted with zero to 6 R.sup.1a, or P(O)R.sup.1cR.sup.1c, or (ii) L R.sup.1; and A, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Z.sup.1, Z.sup.2, R.sup.1, R.sup.1a, R.sup.1c, R.sup.2, R.sup.3a, R.sup.3b, R.sup.x, L, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
##STR00001##
SUBSTITUTED AMIDE COMPOUNDS USEFUL AS FARNESOID X RECEPTOR MODULATORS
Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, when Q is: (i) halo, cyano, hydroxyl, NR.sup.xR.sup.x, C(O)OH, C(O)NH.sub.2, C.sub.1-6 alkyl substiuted with zero to 6 R.sup.1a, or P(O)R.sup.1cR.sup.1c, or (ii) L R.sup.1; and A, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Z.sup.1, Z.sup.2, R.sup.1, R.sup.1a, R.sup.1c, R.sup.2, R.sup.3a, R.sup.3b, R.sup.x, L, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
##STR00001##
TETRALIN AND TETRAHYDROQUINOLINE COMPOUNDS AS INHIBITORS OF HIF-2ALPHA
- Joel Worley BEATTY ,
- Samuel Lawrie DREW ,
- Matthew Epplin ,
- Jeremy Thomas Andre FOURNIER ,
- Balint GAL ,
- Tezcan GUNEY ,
- Karl T. Haelsig ,
- Clayton HARDMAN ,
- Steven Donald JACOB ,
- Jenna Leigh JEFFREY ,
- Jaroslaw KALISIAK ,
- Kenneth Victor LAWSON ,
- Manmohan Reddy LELETI ,
- Erick Allen LINDSEY ,
- Artur Karenovich MAILYAN ,
- Debashis MANDAL ,
- Guillaume MATA ,
- Hyunyoung Moon ,
- Jay Patrick Powers ,
- Brandon Reid ROSEN ,
- Yongli Su ,
- Anh Thu TRAN ,
- Zhang Wang ,
- Xuelei Yan ,
- Kai YU
Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.
NOVEL COMPOUNDS
The invention relates to compounds of formula (I) and to their use in treating or preventing an inflammatory disease or a disease associated with an undesirable immune response:
##STR00001## wherein A, L, R.sup.A1, R.sup.A2, R.sup.C and R.sup.D are as defined herein.