Patent classifications
C07D277/62
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.
METHOD OF CONTROLLING SOYBEAN RUST FUNGUS HAVING RESISTANCE TO QoI FUNGICIDE
A method for controlling a soybean rust fungus having an amino acid substitution of F129L in a mitochondrial cytochrome b protein. A compound of formula (I) can be used for controlling a soybean rust fungus having an amino acid substitution of F129L in a mitochondrial cytochrome b protein,
##STR00001##
wherein: R.sup.1 represents a C1-C4 alkyl group or the like; n represents 0, 1, or 2; Q represents the group of Q1 or the like;
##STR00002##
represents the binding site to the rest of molecule; X.sup.1 represents —C(H)═ or the like; X.sup.2 represents -C(O)OCH.sub.3 or the like; J represents the group represented by J1 or the like;
##STR00003##
# represents the binding position to E; Y.sup.1 represents an oxygen atom or the like; Y.sup.2 represents ═C(R.sup.6)— or the like; R.sup.6 represents a C1-C4 alkyl group or the like; and E represents a C1-C6 chain hydrocarbon group or the like.
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.
Ferroportin inhibitors and methods of use
The subject matter described herein is directed to Ferroportin inhibitor compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis. The compounds of Formula I and pharmaceutical salts thereof have the following structure: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Y.sup.1, Y.sup.2, and Y.sup.3 are as described herein.
Ferroportin inhibitors and methods of use
The subject matter described herein is directed to Ferroportin inhibitor compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis. The compounds of Formula I and pharmaceutical salts thereof have the following structure: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Y.sup.1, Y.sup.2, and Y.sup.3 are as described herein.
EBNA1 Inhibitors and Methods Using Same
The present invention provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by EBNA1 activity, such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The present invention further provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection and/or lytic EBV infection.
EBNA1 Inhibitors and Methods Using Same
The present invention provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by EBNA1 activity, such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The present invention further provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection and/or lytic EBV infection.
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.
SUCCINATE AND FUMARATE ACID ADDITION SALTS OF PIPERAZINE DERIVATIVES
The invention relates to succinic acid addition salts or fumaric acid addition salts of piperazine derivatives of formula (I), as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and, in particular, as glucosidase inhibitors.
##STR00001##
Compounds and compositions for inhibition of FASN
The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below: ##STR00001##