Patent classifications
C07D237/30
DIHYDRO-CYCLOPENTA-ISOQUINOLINE SULFONAMIDES DERIVATIVES
The present invention relates to dihydro-cyclopenta-isoquinoline derivatives of formula (I): processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses, non-allergic mast cell responses or certain autoimmune responses), and in particular, disorders caused by the interaction of IgE with the Fc?RI receptor.
##STR00001##
NITROGEN CONTAINING BICYCLIC DERIVATIVES FOR TREATING PAIN AND PAIN RELATED CONDITIONS
The present invention relates to new compounds of formula (I):
##STR00001##
showing great affinity and activity towards the subunit 2 of voltage-gated calcium channels (VGCC), especially the 2-1 subunit of voltage-gated calcium channels or dual activity towards the subunit 2 of voltage-gated calcium channels (VGCC), especially the 2-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET).
NITROGEN CONTAINING BICYCLIC DERIVATIVES FOR TREATING PAIN AND PAIN RELATED CONDITIONS
The present invention relates to new compounds of formula (I):
##STR00001##
showing great affinity and activity towards the subunit 2 of voltage-gated calcium channels (VGCC), especially the 2-1 subunit of voltage-gated calcium channels or dual activity towards the subunit 2 of voltage-gated calcium channels (VGCC), especially the 2-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET).
COMPOUNDS AND USE THEREOF FOR TREATMENT OF NEURODEGENERATIVE, DEGENERATIVE AND METABOLIC DISORDERS
Provided are, inter alia, compounds having a structure of Formula (X), or a pharmaceutically acceptable salt thereof composition including the same and methods of use. Ring A, L.sup.1, L.sup.2, W, R.sup.2A, R.sup.2B, and R.sup.10 are as described herein.
##STR00001##
COMPOUNDS AND USE THEREOF FOR TREATMENT OF NEURODEGENERATIVE, DEGENERATIVE AND METABOLIC DISORDERS
Provided are, inter alia, compounds having a structure of Formula (X), or a pharmaceutically acceptable salt thereof composition including the same and methods of use. Ring A, L.sup.1, L.sup.2, W, R.sup.2A, R.sup.2B, and R.sup.10 are as described herein.
##STR00001##
HETEROAROMATIC COMPOUNDS
The specification relates to compounds of Formula (1):
##STR00001##
and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cancer.
Trans-cycloheptenes and hetero-trans-cycloheptenes for bioorthogonal coupling
A substituted trans-cycloheptene according to formula (I); wherein: a) Z and L are each selected from the group consisting of SiR.sup.1R.sup.2, CH.sub.2, CHOH, and CHR.sup.2; R.sup.1 is phenyl or CH.sub.3; R.sup.2 is phenyl, CH.sub.3, (CH.sub.2).sub.nCN, or (CH.sub.2).sub.nOH, wherein n is an integer from 1 to 5; R.sup.a and R.sup.b are each individually selected from the group consisting of H, OH, and CH.sub.3; and Z and L are not both SiR.sup.1R.sup.2; or b) Z is BocN, L is CH.sub.2, R.sup.a is H, and R.sup.b is H; or c) Z is C=0, L is CH.sub.2, R.sup.a is H, and R.sup.b is H. ##STR00001##
Trans-cycloheptenes and hetero-trans-cycloheptenes for bioorthogonal coupling
A substituted trans-cycloheptene according to formula (I); wherein: a) Z and L are each selected from the group consisting of SiR.sup.1R.sup.2, CH.sub.2, CHOH, and CHR.sup.2; R.sup.1 is phenyl or CH.sub.3; R.sup.2 is phenyl, CH.sub.3, (CH.sub.2).sub.nCN, or (CH.sub.2).sub.nOH, wherein n is an integer from 1 to 5; R.sup.a and R.sup.b are each individually selected from the group consisting of H, OH, and CH.sub.3; and Z and L are not both SiR.sup.1R.sup.2; or b) Z is BocN, L is CH.sub.2, R.sup.a is H, and R.sup.b is H; or c) Z is C=0, L is CH.sub.2, R.sup.a is H, and R.sup.b is H. ##STR00001##
CONDENSED RING DERIVATIVE, AND PREPARATION METHOD, INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND USE THEREOF
Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.
CONDENSED RING DERIVATIVE, AND PREPARATION METHOD, INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND USE THEREOF
Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.