Patent classifications
C07D241/36
INHIBITORS OF HEPATITIS C VIRUS
- Kyla Bjornson ,
- Eda Canales ,
- Jeromy J. Cottell ,
- Kapil K. Karki ,
- Ashley A. Katana ,
- Darryl Kato ,
- Tetsuya Kobayashi ,
- John O. Link ,
- Ruben Martinez ,
- Barton W. Phillips ,
- Hyung-Jung Pyun ,
- Michael Sangi ,
- Adam J. Schrier ,
- Dustin Siegel ,
- James G. Taylor ,
- Chinh V. Tran ,
- Teresa A. Trejo Martin ,
- Randall W. Vivian ,
- Zheng-Yu Yang ,
- Jeff Zablocki ,
- Sheila Zipfel
Compounds of Formula I are disclosed
##STR00001##
As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.
IRIDIUM (III) COMPLEXES WITH CYCLIC QUINOXALINE-FUSED LIGANDS AND ORGANIC LIGHT-EMITTING DIODES USING THE SAME
An iridium (III) complex compound with cyclic quinoxaline-fused dibenzosuberene ligand is shown in General Formula (1),
##STR00001## wherein m is 1 or 2, n is 1 or 2, and m+n is 3; A is a bridging atom represented by General Formula (2) or General Formula (3),
##STR00002## wherein R.sub.1 is a hydrogen atom, alkyl or tert-butyl group, R.sub.2 to R.sub.14 are independently selected from the group consisting of hydrogen atom, halogen atom, cyano group, alkyl group, cycloalkyl group, aryl group, alkoxy group, amino group, thioalkyl group, silyl group and alkenyl group.
IRIDIUM (III) COMPLEXES WITH CYCLIC QUINOXALINE-FUSED LIGANDS AND ORGANIC LIGHT-EMITTING DIODES USING THE SAME
An iridium (III) complex compound with cyclic quinoxaline-fused dibenzosuberene ligand is shown in General Formula (1),
##STR00001## wherein m is 1 or 2, n is 1 or 2, and m+n is 3; A is a bridging atom represented by General Formula (2) or General Formula (3),
##STR00002## wherein R.sub.1 is a hydrogen atom, alkyl or tert-butyl group, R.sub.2 to R.sub.14 are independently selected from the group consisting of hydrogen atom, halogen atom, cyano group, alkyl group, cycloalkyl group, aryl group, alkoxy group, amino group, thioalkyl group, silyl group and alkenyl group.
PHENAZINE DERIVATIVES AS ANTIMICROBIAL AGENTS
The present invention provides novel phenazine derivatives, such as compounds of Formula (I) (e.g., Formula (I)), (II), and (III), and pharmaceutically acceptable salts thereof. The compounds of the invention are expected to be antimicrobial agents and may act by a microbial warfare strategy (e.g., a reactive oxygen species (ROS)-based competition strategy). The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the compounds of the invention and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection or mycobacterial infection) in a subject, inhibiting the mycobacterium), inhibiting the formation and/or growth of a biofilm, reducing or clearing a biofilm, and/or disinfecting a surface.
HYDROPHILIC SELF-IMMOLATIVE LINKERS AND CONJUGATES THEREOF
The present disclosure provides compounds with a hydrophilic self-immolative linker, which is cleavable under appropriate conditions and incorporates a hydrophilic group to provide better solubility of the compound. The compounds of the present disclosure comprise a drug moiety, a targeting moiety capable of targeting a selected cell population, and a linker which contains an acyl unit, an optional spacer unit for providing distance between the drug moiety and the targeting moiety, a peptide linker which can be cleavable under appropriate conditions, a hydrophilic self-immolative linker, and an optional second self-immolative spacer or cyclization self-elimination linker.
HYDROPHILIC SELF-IMMOLATIVE LINKERS AND CONJUGATES THEREOF
The present disclosure provides compounds with a hydrophilic self-immolative linker, which is cleavable under appropriate conditions and incorporates a hydrophilic group to provide better solubility of the compound. The compounds of the present disclosure comprise a drug moiety, a targeting moiety capable of targeting a selected cell population, and a linker which contains an acyl unit, an optional spacer unit for providing distance between the drug moiety and the targeting moiety, a peptide linker which can be cleavable under appropriate conditions, a hydrophilic self-immolative linker, and an optional second self-immolative spacer or cyclization self-elimination linker.
Method for treating depression and/or depression status with substituted quinoxaline compounds
A heterocyclic compound represented by the general formula (1) or a salt thereof: ##STR00001## wherein m, l, and n respectively represent an integer of 1 or 2; X represents O or CH.sub.2; R.sup.1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R.sup.2 and R.sup.3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R.sub.2 and R.sub.3 are bonded to form a cyclo-C3-C8 alkyl group; and R.sup.4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
Hydrophilic self-immolative linkers and conjugates thereof
The present disclosure provides compounds with a hydrophilic self-immolative linker, which is cleavable under appropriate conditions and incorporates a hydrophilic group to provide better solubility of the compound. The compounds of the present disclosure comprise a drug moiety, a targeting moiety capable of targeting a selected cell population, and a linker which contains an acyl unit, an optional spacer unit for providing distance between the drug moiety and the targeting moiety, a peptide linker which can be cleavable under appropriate conditions, a hydrophilic self-immolative linker, and an optional second self-immolative spacer or cyclization self-elimination linker.
Hydrophilic self-immolative linkers and conjugates thereof
The present disclosure provides compounds with a hydrophilic self-immolative linker, which is cleavable under appropriate conditions and incorporates a hydrophilic group to provide better solubility of the compound. The compounds of the present disclosure comprise a drug moiety, a targeting moiety capable of targeting a selected cell population, and a linker which contains an acyl unit, an optional spacer unit for providing distance between the drug moiety and the targeting moiety, a peptide linker which can be cleavable under appropriate conditions, a hydrophilic self-immolative linker, and an optional second self-immolative spacer or cyclization self-elimination linker.
Pyruvate kinase activators for use in treating blood disorders
Described herein are compounds that activate pyruvate kinase, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I) wherein R.sup.1, R.sup.2, R.sup.a, R.sup.b, R.sup.j, R.sup.k, and Q are as defined herein. ##STR00001##