http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-082391-A1
Outgoing Links
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| filingDate | 2011-07-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2012-12-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-082391-A1 |
| titleOfInvention | BICYCLE INHIBITORS OF ACETIL-COA AND USES OF THE SAME |
| abstract | This provides a method for the preparation of the compounds of the formula (1), their therapeutic uses, combinations with other pharmacologically active agents, and pharmaceutical compositions. Claim 1: A compound of the formula (1), or a salt pharmaceutically acceptable thereof, wherein ring A is a bicyclic ring system selected from the group of formulas (2) where the wavy line indicates that the point of attachment of L1 is on ring A '; and wherein R1 can replace a hydrogen atom of any CH bond in ring A; X1, for each presentation, is independently CH or N; X2 is NR19, O, or S; X3, for each presentation, is independently NR9, CH2, O, or S; r is 1 or 2; Ring B is cyclohexyl or phenyl; with the understanding that, when ring B is phenyl, ring A is of formula (3) wherein R1a is hydrogen, phenyl, phenyl-amino, or a 5-10 membered heteroaryl, where R1a can be optionally substituted on one or more carbon atoms with one or more independently selected R13; and wherein, when R1a is a heteroaryl comprising one or more -NH-, the hydrogen of each group -NH- can be optionally replaced with R22; Q is selected from the group of formulas (4) where the wavy line indicates the point of attachment with the ring B; X4 is -NR4- or -O-; q and n are each independently 0, 1, 2, 3 or 4; L1 is -NHSO2-, -SO2NH-, -NHSO2NH- or -NHC (O) NH-; R1 can replace a hydrogen atom of any CH bond in ring A and, for each presentation, is independently deuterium, hydroxyl, nitro, halogen, cyano, carboxyl, formyl, C1-7 alkyl, C3-8 carbocyclyl, alkenyl C2-7, C2-7 alkynyl, C1-7 alkoxy, C1-7 thioalkyl, C3-8 cycloalkoxy, C6-10 aryl, C6-10 aryl-C1-4 alkyl, C6-10 aryloxy, amino, N-C1 alkyl -7-amino, N, N-di- (C1-7 alkyl) -amino, C6-10-amino N-aryl, 3-10 membered heterocyclyl, N- (3-10 membered heterocyclyl) -amino, ( 3 to 10 membered heterocyclyl) -oxy, 5 to 10 membered heteroaryl, (5 to 10 membered heteroaryl) -C 1-4 alkyl, N- (5 to 10 membered heteroaryl) -amino, (5 to 10 heteroaryl members) -oxy, C 1-7 alkanoyl, C 1-7 alkoxycarbonyl, C 1-7 alkanoyloxy, C 1-7 alkyl-amido, C 6-10 -amido aryl, (3-10 membered heterocyclyl) -amido, carbamoyl, N -C 1-7 alkylcarbamoyl, N, N-di- (C 1-7 alkyl) -carbamoyl, C 1-7 alkoxy, C 1-7 alkyl ureido, and aryl C6-10-ureido, wherein R1 is optionally substituted on one or more carbon atoms with one or more independently selected R13; and wherein, when R1 comprises a heterocyclyl or a heteroaryl comprising one or more -NH-, the hydrogen of each group -NH- can be independently optionally replaced with R22; or two R1 on the same carbon atom, can together form an oxo; or two R1 on the same carbon atom, together with the carbon atom with which they are attached, form a spiro-carbocyclyl of 3 to 8 carbon atoms; or two R1 on adjacent carbon atoms, together with the carbon atoms with which they are attached, can form a carbocyclyl of 3 to 8 fused carbon atoms or phenyl, which may be optionally substituted with one or more R13; and R2, for each presentation, is independently selected from the group consisting of hydroxyl, cyano, C1-7 alkyl, C1-7 alkoxy, C2-7 alkenyl, amino, C1-7-amino alkyl, di- (C1 alkyl -7) -amino, C 1-7 alkyl-amido, C 1-7 alkoxy-amido; wherein R2, for each presentation, can be independently optionally substituted with one or more halogens; or two or more R2 groups on non-adjacent carbon atoms together form a C1-4 alkylene bridge; or two or more R2 groups on adjacent carbon atoms, can form a fused C3-8 carbocyclyl; R3 is selected from the group consisting of a C1-7 alkyl, C3-8 carbocyclyl, C3-8 carbocyclyl-C1-4 alkyl, C6-10 aryl, C6-10 aryl-C1-4 alkyl, a heteroaryl of 5 10-membered, a (5-10 membered heteroaryl) -C 1-4 alkyl, a 3-10 membered heterocyclyl, and a (3-10 membered heterocyclyl) -C 1-4 alkyl, wherein R 3 is optionally substituted on one or more carbon atoms with one or more R14; and wherein, when R3 comprises a heteroaryl or heterocyclyl, which comprises one or more -NH-, the hydrogen of each group -NH- can be independently optionally replaced with a C1-7 alkyl; R4 is hydrogen, C1-7 alkyl, or C1-4 alkoxy-C1-4 alkyl; or R3 and R4, together with the nitrogen atom with which they are attached, form a 3- to 7-membered heterocyclyl, wherein the heterocyclyl may be optionally substituted on one or more carbon atoms with one or more R15; and wherein, when the heterocyclyl comprises one or more -NH-, the hydrogen of each group -NH- can be independently optionally replaced with R16; R13, for each presentation, is independently deuterium, nitro, halogen, cyano, hydroxyl, carboxyl, C1-7 alkyl, C3-8 cycloalkyl, C1-7 alkoxy, C6-10 aryl, C6-10 aryloxy, heterocyclyl 3-10 members, 5-10 membered heteroaryl, amino, C1-7-amino alkyl, di- (C1-7 alkyl) -amino, C1-7 alkanoyl, C1-7 alkoxycarbonyl, C1-7 alkanoyloxy, C1-7 alkyl -amido, C1-7 alkoxy-amido, carbamoyl, N-C1-7-carbamoyl, N, N-di- (C1-7 alkyl) -carbamoyl, C1-7-sulfonyl alkyl, C1-7-sulfonyloxy alkyl, C1-7-sulfonamido alkyl, sulfamoyl, N-C1-7-sulfamoyl alkyl, or N, N-di- (C1-7 alkyl) sulfamoyl, wherein R13 is optionally substituted on one or more carbon atoms with one or more R17 independently selected; and wherein, when R13 is a heterocyclyl or a heteroaryl comprising one or more -NH-, the hydrogen of each group -NH- can be independently optionally replaced with R20; or two R13 on the same carbon atom, can together form an oxo or a C3-8 spirocarbocyclyl; or two R13 on adjacent carbon atoms, together with the carbon atoms with which they are attached, can form a 3- to 7-membered heterocyclyl, which may be optionally substituted on one or more carbon atoms with one or more R17, and if the heterocyclyl comprises one or more groups -NH-, the hydrogen of each group -NH- can be independently optionally replaced with R20; R14, for each presentation, is independently halogen, hydroxyl, carboxyl, C1-7 alkoxycarbonyl, C1-7 alkyl, C1-7 alkoxy, C3-8 cycloalkyl, C6-10 aryl, or 5-10 membered heteroaryl, in where R14 may be optionally substituted on one or more carbon atoms with one or more independently selected R24; or two R14 on the same carbon atom, can together form an oxo, a C3-8 spiro carbocyclyl, or a 3 to 7 membered spiro-heterocyclyl; or two R14 on adjacent carbon atoms, together with the carbon atoms with which they are attached, can form a phenyl, which may be optionally substituted on one or more carbon atoms with one or more R24; R15, for each presentation, is independently selected from the group consisting of hydroxyl, carboxyl, C1-7 alkyl, C1-7 alkoxy, C3-8 carbocyclyl, phenyl, and C1-7 alkoxycarbonyl; wherein R15 may be optionally substituted on one or more carbon atoms with one or more substituents independently selected from halogen, hydroxyl, C1-4 alkoxy; or two R15s on the same carbon atom together form an oxo, or together with the carbon atom with which they are attached, form a C2-8 cycloalkyl, or a 3-10 membered heterocyclyl; or two R15 on adjacent carbon atoms, together with the carbon atoms with which they are attached, can form a fused phenyl; R16, for each presentation, is independently selected from the group consisting of C1-7 alkyl, C3-8 carbocyclyl, C1-7 alkanoyl, C1-7 alkoxycarbonyl, or 5-10 membered heteroaryl; R17, for each presentation, is independently selected from cyano, halogen, hydroxyl, carboxyl, C1-7 alkyl, C1-7 alkoxy, amino, C1-7-amino alkyl, di (C1-7 alkyl) -amino, aryl C6-10-amino, C6-10 aryl-C 1-4 alkyl-amino, C 1-7 alkoxycarbonyl, C 1-7 alkanoyloxy, 3- to 10-membered heterocyclyl, wherein R 17 may be optionally substituted on one or more atoms of carbon with one or more of the following independently selected: halogen, amino, C 1-7 alkyl, C 1-7 alkoxy, halo C 1-7 alkyl, carboxyl, or C 1-7 alkoxycarbonyl; and wherein, when R17 is a heterocyclyl, which comprises one or more -NH-, the hydrogen of each group -NH- can be independently optionally replaced with R23; or two R17 on the same carbon atom, can together form an oxo; R18 is a C1-7 alkyl, C3-8 cycloalkyl, phenyl or a C1-7 alkoxy-C1-7 alkyl; R19, for each presentation, is independently hydrogen, C1-7 alkyl, C1-7 alkanoyl, tri- (C1-7 alkyl) -silyl, C3-8 cycloalkyl, C1-7 alkoxycarbonyl, C3-8cycloalkoxycarbonyl, carbamoyl, N-C 1-7 alkyl-carbamoyl, N, N-di- (C 1-7 alkyl) -carbamoyl, or C 6-10 aryl-C 1-4 alkyl; wherein R19 is optionally substituted on one or more carbon atoms with one or more R21; R20, R21, R22, and R23, for each presentation, are independently deuterium, halogen, carboxyl, C1-7 alkyl, C1-7 alkoxy, C6-10 aryloxy, C6-10 aryl-C1-4 alkoxy, or C1- alkoxy 7-carbonyl; and R24, for each presentation, is independently hydroxy, halogen, carboxyl, C 1-7 alkyl, halo C 1-7 alkyl, C 1-7 alkoxy, amino, N-C 1-7 alkyl, N, N-di (alkyl C1-7) -amino, C1-7 alkoxycarbonyl, C1-7 alkanoyloxy, phosphono-oxyl, C1-7 alkoxy- (hydroxy) -phosphoryloxy or di- (C1-7 alkoxy) -phosphoryloxy; wherein R24 may be optionally substituted on one or more carbon atoms with a group independently selected from amino, N-al |
| priorityDate | 2010-07-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 91.