Patent classifications
C07D311/22
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.
SYNTHESIS OF INTERMEDIATES FOR THE PREPARATION OF ALPHA-TOCOPHEROL
The present invention relates to a novel synthetic pathway for alpha-tocopherol. The invention discloses different reactions yielding some new intermediates in a very high yield and stereoselectivity.
SYNTHESIS OF INTERMEDIATES FOR THE PREPARATION OF ALPHA-TOCOPHEROL
The present invention relates to a novel synthetic pathway for alpha-tocopherol. The invention discloses different reactions yielding some new intermediates in a very high yield and stereoselectivity.
Alvocidib Prodrugs Having Increased Bioavailability
Compounds having the following structure (I):
##STR00001##
or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of R.sup.1, R.sup.2 or R.sup.3 is —P(═O)(OH).sub.2, and the other two of R.sup.1, R.sup.2 and R.sup.3 are each H, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided.
BRAG2 INHIBITORS AND APPLICATIONS THEREOF
The present invention relates to molecules having the following chemical structure (I). The present invention concerns molecules, in particular active as BRAG2 inhibitors and applications thereof. In particular, the invention concerns BRAG2 inhibitors in the treatment of a cancer or angiogenesis.
##STR00001##
BRAG2 INHIBITORS AND APPLICATIONS THEREOF
The present invention relates to molecules having the following chemical structure (I). The present invention concerns molecules, in particular active as BRAG2 inhibitors and applications thereof. In particular, the invention concerns BRAG2 inhibitors in the treatment of a cancer or angiogenesis.
##STR00001##
ROR-gamma modulators and uses thereof
The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.
ROR-gamma modulators and uses thereof
The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.
BIHETEROCYCLIC COMPOUND
The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter
##STR00001##
wherein R.sup.1-L- is R.sup.1—OC(O)—, or the like, R.sup.1 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R.sup.2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R.sup.3 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like, the part of X, Y, and Z is X═Y—Z, X—Y═Z, or X—Y—Z, X is nitrogen atom, NR.sup.4 (R.sup.4 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.
BIHETEROCYCLIC COMPOUND
The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter
##STR00001##
wherein R.sup.1-L- is R.sup.1—OC(O)—, or the like, R.sup.1 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R.sup.2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R.sup.3 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like, the part of X, Y, and Z is X═Y—Z, X—Y═Z, or X—Y—Z, X is nitrogen atom, NR.sup.4 (R.sup.4 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.