Patent classifications
C07D217/16
PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF 2-(2,6-DICHLOROPHENYL)-1-[(1S,3R)-3-(HYDROXYMETHYL)-5-(3-HYDROXY-3-METHYLBUTYL)-1-METHYL-3,4-DIHYDROISOQUINOLIN-2(1H)-YL]ETHENONE
The embodiments of the present invention provide processes and intermediates for the preparation of D1 PAM I: Formula (I).
##STR00001##
PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF 2-(2,6-DICHLOROPHENYL)-1-[(1S,3R)-3-(HYDROXYMETHYL)-5-(3-HYDROXY-3-METHYLBUTYL)-1-METHYL-3,4-DIHYDROISOQUINOLIN-2(1H)-YL]ETHENONE
The embodiments of the present invention provide processes and intermediates for the preparation of D1 PAM I: Formula (I).
##STR00001##
MODULATORS OF THE INTEGRATED STRESS PATHWAY
Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.
MODULATORS OF THE INTEGRATED STRESS PATHWAY
Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.
MODULATORS OF CELLULAR ADHESION
The present invention provides compounds having formula (I):
##STR00001##
and pharmaceutically acceptable derivatives thereof, wherein R.sub.1-R.sub.4, n, p, A, B, D, E, L and AR.sub.1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
MODULATORS OF CELLULAR ADHESION
The present invention provides compounds having formula (I):
##STR00001##
and pharmaceutically acceptable derivatives thereof, wherein R.sub.1-R.sub.4, n, p, A, B, D, E, L and AR.sub.1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
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##
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##
3-oxa-8-azabicyclo[3.2.1]octane derivatives and their use in the treatment of cancer and hemoglobinopathies
A compound of formula Ia, Ib, Ic or Id: ##STR00001##
wherein: n is 1 or 2; R.sup.N is H or Me; R.sup.1 is optionally one or more halo or methyl groups; R.sup.2a and R.sup.2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.2c and R.sup.2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.3a and R.sup.3b are independently selected from H and Me; R.sup.4a is selected from OH, —NH.sub.2, —C(═O)NH.sub.2, and —CH.sub.2OH; R.sup.4b is either H or Me; R.sup.5 is either H or Me; m is 1 or 2; q is 0 or 1; R.sup.11a, R.sup.11b, R.sup.11c and R.sup.11d are independently selected from H, halo, C.sub.1-4 alkyl, C.sub.1-4 fluoroalkyl, C.sub.3-4 cycloalkyl, C.sub.1-4 alkyloxy, NH—C.sub.1-4 alkyl and cyano; R.sup.12a and R.sup.12b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.12c and R.sup.12d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.12e is H or Me; R.sup.13a and R.sup.13b are independently selected from H and Me; R.sup.14 is either H or Me; R.sup.16a and R.sup.16b are independently selected from H and Me; R.sup.6 is selected from H, OMe, and OEt.
3-oxa-8-azabicyclo[3.2.1]octane derivatives and their use in the treatment of cancer and hemoglobinopathies
A compound of formula Ia, Ib, Ic or Id: ##STR00001##
wherein: n is 1 or 2; R.sup.N is H or Me; R.sup.1 is optionally one or more halo or methyl groups; R.sup.2a and R.sup.2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.2c and R.sup.2d (if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.3a and R.sup.3b are independently selected from H and Me; R.sup.4a is selected from OH, —NH.sub.2, —C(═O)NH.sub.2, and —CH.sub.2OH; R.sup.4b is either H or Me; R.sup.5 is either H or Me; m is 1 or 2; q is 0 or 1; R.sup.11a, R.sup.11b, R.sup.11c and R.sup.11d are independently selected from H, halo, C.sub.1-4 alkyl, C.sub.1-4 fluoroalkyl, C.sub.3-4 cycloalkyl, C.sub.1-4 alkyloxy, NH—C.sub.1-4 alkyl and cyano; R.sup.12a and R.sup.12b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.12c and R.sup.12d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH.sub.2OH; R.sup.12e is H or Me; R.sup.13a and R.sup.13b are independently selected from H and Me; R.sup.14 is either H or Me; R.sup.16a and R.sup.16b are independently selected from H and Me; R.sup.6 is selected from H, OMe, and OEt.