Patent classifications
C07C311/20
LPXH TARGETING COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF MAKING AND USING THE SAME
LpxH targeting compounds, compositions thereof, as well as methods for for making and using the same are disclosed herein. The LpxH target compounds typically have a structure pursuant to Formula (I) and/or a salt thereof, wherein R.sub.b is selected from a single bond, C.sub.4 to C.sub.10 unsubstituted aryl, C.sub.4 to C.sub.10 substituted aryl, unsubstituted or substituted four to ten member heterocycle ring, C.sub.1 to C.sub.10 unsubstituted alkyl, and C.sub.1 to C.sub.10 substituted alkyl; R.sub.c comprises hydrogen, halogen, OH, CO.sub.2CH.sub.3, COOH, CN.sub.2CF.sub.3, CF.sub.3, C.sub.2OH, CONHOH, CCOH, C.sub.4 to C.sub.10 unsubstituted aryl, C.sub.4 to C.sub.10 substituted aryl, unsubstituted or substituted four to ten member heterocycle ring, C.sub.1 to C.sub.10 unsubstituted alkyl, or C.sub.1 to C.sub.10 substituted alkyl; and R.sub.d and R.sub.e are independently hydrogen, OH, COH, COH, COC, COOH, R.sub.f, or are taken together as an unsubstituted or substituted four to eight member nitrogen containing heterocycle ring.
COMPOSITIONS AND METHODS RELATED TO BICYCLO[2.2.1] HEPTANAMINE-CONTAINING COMPOUNDS
The present disclosure relates to compositions and methods related to bicyclo[2.2.1]heptanamine-containing compounds and salts thereof.
COMPOSITIONS AND METHODS RELATED TO BICYCLO[2.2.1] HEPTANAMINE-CONTAINING COMPOUNDS
The present disclosure relates to compositions and methods related to bicyclo[2.2.1]heptanamine-containing compounds and salts thereof.
SMALL MOLECULE FERROPTOSIS INDUCERS
The present invention provides, inter alia, a compound according to formula (I):
##STR00001##
Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for regulating GPX4 in a cell and methods for inducing ferroptosis in a cell.
Process for hydrogenating ketones in the presence of Ru(II) catalysts
The present invention relates to a process for hydrogenating a substrate including a carbon-heteroatom double bond, the process including the step of reacting the substrate with hydrogen gas in the presence of a hydrogenation catalyst, wherein the hydrogenation catalyst is a complex of formula (I): ##STR00001##
R.sub.1-10, A and Hal are as defined in the specification. The present invention also provides processes for the preparation of the complex of formula (I) and intermediates thereof.
Process for hydrogenating ketones in the presence of Ru(II) catalysts
The present invention relates to a process for hydrogenating a substrate including a carbon-heteroatom double bond, the process including the step of reacting the substrate with hydrogen gas in the presence of a hydrogenation catalyst, wherein the hydrogenation catalyst is a complex of formula (I): ##STR00001##
R.sub.1-10, A and Hal are as defined in the specification. The present invention also provides processes for the preparation of the complex of formula (I) and intermediates thereof.
ROR gamma (RORγ) modulators
Compounds according to Formula I: ##STR00001##
or a pharmaceutically acceptable salt wherein: A.sub.1 is NR.sub.1 or CR.sub.1, with R.sub.1 herein; the cyclopropyl moiety with one or more methyl and one or more F; A.sub.2-A.sub.5 are N or CR.sub.2-CR.sub.5, with no more than two of the four positions A in A.sub.2-A.sub.5 can be simultaneously N; R.sub.2-R.sub.5 are described; R.sub.6 and R.sub.7 are independently H, F, methyl, ethyl, hydroxyl or methoxy or R.sub.6 and R.sub.7 together is carbonyl, all alkyl groups, if substituted with one or more F; R.sub.8 is H or C(1-6)alkyl; A.sub.9-A.sub.12 are N or CR.sub.9-CR.sub.12, with no more than two of the four positions A in A.sub.9-A.sub.12 can be simultaneously N; R.sub.9-R.sub.12 herein; R.sub.13 and R.sub.14 herein; or R.sub.13 and R.sub.14 fused forming a ring having 5 to 7 atoms by joining R.sub.13 being C(1-6)alkyl or C(2-6)alkenyl. The ROR compounds can treat ROR mediated diseases.
ROR gamma (RORγ) modulators
Compounds according to Formula I: ##STR00001##
or a pharmaceutically acceptable salt wherein: A.sub.1 is NR.sub.1 or CR.sub.1, with R.sub.1 herein; the cyclopropyl moiety with one or more methyl and one or more F; A.sub.2-A.sub.5 are N or CR.sub.2-CR.sub.5, with no more than two of the four positions A in A.sub.2-A.sub.5 can be simultaneously N; R.sub.2-R.sub.5 are described; R.sub.6 and R.sub.7 are independently H, F, methyl, ethyl, hydroxyl or methoxy or R.sub.6 and R.sub.7 together is carbonyl, all alkyl groups, if substituted with one or more F; R.sub.8 is H or C(1-6)alkyl; A.sub.9-A.sub.12 are N or CR.sub.9-CR.sub.12, with no more than two of the four positions A in A.sub.9-A.sub.12 can be simultaneously N; R.sub.9-R.sub.12 herein; R.sub.13 and R.sub.14 herein; or R.sub.13 and R.sub.14 fused forming a ring having 5 to 7 atoms by joining R.sub.13 being C(1-6)alkyl or C(2-6)alkenyl. The ROR compounds can treat ROR mediated diseases.
SULFONAMIDES AS GPR40- AND GPR120-AGONISTS
The invention relates to compounds acting as agonists of G-protein coupled receptor 120 (GPR120) and/or 40 (GPR40), and having formula (I):
##STR00001##
Said compounds are useful in the treatment of diseases or disorders modulated by GPR120 and/or GPR40 such as diabetes (particularly type 2 diabetes), impaired oral glucose tolerance, insulin resistance, obesity, obesity related disorders, metabolic syndrome, dyslipidemia, elevated LDL, elevated triglycerides, obesity induced inflammation, osteoporosis and obesity related cardiovascular disorders.
ROR gamma (RORγ) modulators
Compounds according to Formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof wherein: A.sub.1 is NR.sub.1 or CR.sub.1, with R.sub.1 being H or methyl, with methyl, if present, optionally being substituted with one or more F; the cyclopropyl moiety can be optionally substituted with one or more methyl and one or more F; A.sub.2-A.sub.5 are N or CR.sub.2-CR.sub.5, respectively, with the proviso that no more than two of the four positions A in A.sub.2-A.sub.5 can be simultaneously N; R.sub.2-R.sub.5 are independently H, halogen, amino, C(1-3)alkoxy, (di)C(1-3)alkylamino or C(1-6)alkyl; R.sub.6 and R.sub.7 are independently H, F, methyl, ethyl, hydroxyl or methoxy or R.sub.2 and R.sub.3 together is carbonyl, all alkyl groups, if present, optionally being substituted with one or more F; R.sub.8 is H or C(1-6)alkyl; R.sub.9 is selected from the group consisting of Formula II, III, IV and V ##STR00002## The compounds can be used as inhibitors of ROR and are useful for the treatment of ROR mediated diseases.