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US 2015/0307449 A1Published application
Pyrrole sulfonamide derivative, preparation method for same, and medical application thereof
AssigneeJiangsu Hansoh Pharmaceutical Co., Ltd.
InventorsJiong LAN, Piaoyang SUN, Lei CHEN, Wei PENG, Xing LIU, Qing DONG
Life of this patent
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Abstract
The present invention relates to a pyrrole sulfonamide derivative, a preparation method for the same, and medical applications thereof. Specifically, the present invention relates to a novel pyrrole sulfonamide derivative as represented by formula (I), a preparation method for the derivative, a pharmaceutical composition comprising the derivative, and uses of the same as therapeutic agents, and particularly as gastric acid secretion inhibitors and potassium-competitive acid blockers (P-CABs), wherein each substituent of formula (I) is as defined in the description.
Claims25
A compound of formula (I), or a tautomer, mesomer, racemate, enantiomer, diastereoisomer or mixture thereof, or a pharmaceutically acceptable salt thereof:
- wherein:
- R1 is selected from the group consisting of C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl and 5 to 14-membered heteroaryl, wherein the cycloalkyl, heterocyclyl, aryl and heteroaryl are each optionally substituted by one or more groups selected from the group consisting of halogen, cyano, C1-C20 alkyl, C1-C20 haloalkyl, C1-C20 hydroxyalkyl, C3-C20 cycloalkyl, C1-C20 alkoxy, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl, 5 to 14-membered heteroaryl, carboxyl and alkoxycarbonyl;
- R2 is selected from the group consisting of hydrogen atom, C1-C20 alkyl, C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl and 5 to 14-membered heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are each optionally substituted by one or more groups selected from the group consisting of halogen, cyano, hydroxy, amino, C1-C20 alkyl, C1-C20 haloalkyl, C1-C20 hydroxyalkyl, C1-C20 alkoxy, C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl, 5 to 14-membered heteroaryl, carboxyl and alkoxycarbonyl;
- R3 is selected from the group consisting of hydrogen atom and C1-C20 alkyl;
- ring A is selected from the group consisting of 6 to 14-membered aryl and 5 to 14-membered heteroaryl, wherein the aryl and heteroaryl are each optionally substituted by one or more groups selected from the group consisting of halogen, cyano, C1-C20 alkyl, C1-C20 haloalkyl, C1-C20 hydroxyalkyl, C3-C20 cycloalkyl, C1-C20 alkoxy, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl, 5 to 14-membered heteroaryl, carboxyl and alkoxycarbonyl;
- R4 and R5 are each independently selected from the group consisting of hydrogen atom, halogen, cyano, hydroxy, C1-C20 alkyl, C1-C20 haloalkyl, C1-C20 alkoxy, C1-C20 haloalkoxy, C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl and 5 to 14-membered heteroaryl;
- or R4 and R5 are taken together to form a C3-C20 cycloalkyl or heterocyclyl containing 3 to 20 ring atoms;
- R6 and R7 are each independently selected from the group consisting of hydrogen atom, C1-C20 alkyl, C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl and 5 to 14-membered heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are each independently and optionally substituted by one or more groups selected from the group consisting of halogen, cyano, hydroxy, amino, oxo, C1-C20 alkyl, C1-C20 haloalkyl, C1-C20 hydroxyalkyl, C1-C20 alkoxy, C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl, 5 to 14-membered heteroaryl, carboxyl and alkoxycarbonyl;
- and
- n is 0, 1 or 2.
7 more elements
A compound of formula (I-A), or a tautomer, mesomer, racemate, enantiomer, diastereomer, or mixture thereof, or a pharmaceutically acceptable salt thereof:
- wherein:
- R1 is selected from the group consisting of C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl and 5 to 14-membered heteroaryl, wherein the cycloalkyl, heterocyclyl, aryl and heteroaryl is optionally substituted by one or more groups selected from the group consisting of halogen, cyano, C1-C20 alkyl, C1-C20 haloalkyl, C1-C20 hydroxyalkyl, C3-C20 cycloalkyl, C1-C20 alkoxy, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl, 5 to 14-membered heteroaryl, carboxyl and alkoxycarbonyl;
- R2 is selected from the group consisting of hydrogen atom, C1-C20 alkyl, C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl and 5 to 14-membered heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are each optionally substituted by one or more groups selected from the group consisting of halogen, cyano, hydroxy, amino, C1-C20 alkyl, C1-C20 haloalkyl, C1-C20 hydroxyalkyl, C1-C20 alkoxy, C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl, 5 to 14-membered heteroaryl, carboxyl and alkoxycarbonyl;
- ring A is selected from the group consisting of 6 to 14-membered aryl and 5 to 14-membered heteroaryl, wherein the aryl and heteroaryl are each optionally substituted by one or more groups selected from the group consisting of halogen, cyano, C1-C20 alkyl, C1-C20 haloalkyl, C1-C20 hydroxyalkyl, C3-C20 cycloalkyl, C1-C20 alkoxy, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl, 5 to 14-membered heteroaryl, carboxyl and alkoxycarbonyl;
- R4 and R5 are each independently selected from the group consisting of hydrogen atom, halogen, cyano, hydroxy, C1-C20 alkyl, C1-C20 haloalkyl, C1-C20 alkoxy, C1-C20 haloalkoxy, C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl and 5 to 14-membered heteroaryl;
- or R4 and R5 are taken together to form a C3-C20 cycloalkyl or heterocyclyl containing 3 to 20 ring atoms;
- R6 and R7 are each independently selected from the group consisting of hydrogen atom, C1-C20 alkyl, C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl and 5 to 14-membered heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are each independently and optionally substituted by one or more groups selected from the group consisting of halogen, cyano, hydroxy, amino, oxo, C1-C20 alkyl, C1-C20 haloalkyl, C1-C20 hydroxyalkyl, C1-C20 alkoxy, C3-C20 cycloalkyl, heterocyclyl containing 3 to 20 ring atoms, 6 to 14-membered aryl, 5 to 14-membered heteroaryl, carboxyl and alkoxycarbonyl;
- n is 0, 1 or 2;
- and
- PG is an amino-protecting group.
7 more elements
-16. (canceled)
Dependencies are inferred from the claim text.