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filingDate 2001-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5d67d2241c9d4421316ac7115979dc64
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b60b3fa1862b1839d744cc28bee49453
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_43fc2f620a8d6e43da4a1b664e2b7247
publicationDate 2004-07-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-035723-A1
titleOfInvention COMPOSITE DERIVED FROM 1,5 BENZOTIAZEPIN, PROCEDURE FOR PREPARATION, PHARMACEUTICAL COMPOSITION, AND, COMBINATION THAT UNDERSTAND IT AND ITS USE IN THE MANUFACTURE OF A MEDICINAL PRODUCT
abstract A compound derived from 1.5 benzothiazepine of formula (1): where: Rv and Rw are independently selected from hydrogen or C1-6 alkyl; R1 and R2 are independently selected from hydrogen and C1-6 alkyl; Rx and Ry are independently selected from hydrogen or C1-6 alkyl, or one of Rx and Ry is hydrogen or C1-6 alkyl and the other is hydroxy or C1-6 alkoxy; Rz is selected from halo, nitro, cyano, hydroxyl, amino, carboxy, carbamoyl, mercapto, sulfamoyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 alkanoylo, C1- alkanoyloxy 6, N- (C1-6 alkyl) amino, N, N- (C1-6 alkyl) 2amino, C1-6 alkanoylamino, N- (C1-6 alkyl) carbamoyl, N, N- (C1-6 alkyl) 2carbamoyl , C1-6S alkyl (O) where a is 0 to 2; C1-6 alkoxycarbonyl, C1-6 alkoxycarbonylamino, ureido, N '- (C1-6 alkyl) ureido, N- (C1-6 alkyl) ureido, N', N '- (C1-6 alkyl) 2ureido, N'- (C1-6 alkyl) -N- (C1-6 alkyl) ureido, N ', N' - (C1-6 alkyl) 2-N- (C1-6 alkyl) ureido, N- (C1-6 alkyl) sulfamoyl and N, N- (C1-6 alkyl) 2sulfamoyl; v is 0-5; one of R4 and R5 is a group of formula (2): where R3 and R6 and the other of R4 and R5 are independently selected from hydrogen, halo, nitro, cyano, hydroxyl, amino, carboxy, carbamoyl, mercapto, sulfamoyl, alkyl C1-4, C2-4 alkenyl, C2-4 alkynyl, C1-4 alkoxy, C1-4 alkanoyl, C1-4 alkanoyloxy, N- (C1-4 alkyl) amino, N, N- (C1-4 alkyl) 2amino , C1-4 alkanoylamino, N- (C1-4 alkyl) carbamoyl, N, N-C1-4 alkyl) 2carbamoyl, C1-4S alkyl (O) where a is between 0 and 2, C1-4 alkoxycarbonyl, N- (C1-4 alkyl) sulfamoyl and N, N- (C1-4 alkyl) 2sulfamoyl; where R3 and R6 and the other of R4 and R5 may optionally be substituted on a carbon by one or more R16; D is -O-; -N (Ra) -, -S (O) b- or -CH (Ra) -; where Ra is hydrogen or C1-6 alkyl and b is 0-2; ring A is aryl or heteroaryl; wherein ring A is optionally substituted by one or more substituents selected from R17; R7 is hydrogen, C1-4 alkyl, carbocyclyl or heterocyclyl; where R7 is optionally substituted by one or more substituents selected from R18; R8 is hydrogen or C1-4 alkyl; R9 is hydrogen or C1-4 alkyl; R 10 is hydrogen, C 1-4 alkyl, carbocyclyl or heterocyclyl; where R10 is optionally substituted by one or more substituents selected from R19; R11 is carboxy, sulfo, sulfino, phosphono, tetrazolyl, -P (O) (ORc) (ORd), -P (O) (OH) (ORc), -P (O) (OH) (Rd) or -P (O) (ORc) (Rd) where Rc and Rd are independently selected from C1-6 alkyl; or R11 is a group of formula (3) where: X is -N (Rq) -, -N (Rq) C (O) -, -O-, and -S (O) a-; where a is 0-2 and Rq is hydrogen or C1-4 alkyl; R12 is hydrogen or C1-4 alkyl; R13 and R14 are independently selected from hydrogen, C1-4 alkyl, carbocyclyl, heterocyclyl or R23; wherein said C1-4 alkyl, carbocyclyl or heterocyclyl can be independently and optionally substituted by one or more substituents selected from R20; R15 is carboxy, sulfo, sulfine, phosphono, tetrazolyl, -P (O) (ORe) (ORf), -P (O) (OH) (ORe), -P (O) (OH) (Re) or -P (O) (ORe) (Rf) where Re and Rf are independently selected from C1-6 alkyl; or R15 is a group of formula (4): where: R24 is selected from hydrogen or C1-4 alkyl; R25 are selected from hydrogen, C1-4 alkyl, carbocyclyl, heterocyclyl or R27; wherein said C1-4 alkyl, carbocyclyl or heterocyclyl can be optionally substituted independently by one or more substituents selected from R28; R26 is selected from carboxy, sulfo, sulfine, phosphono, tetrazolyl, -P (O) (ORg) (ORh), P (O) (OH) (ORg), -P (O) (OH) (Rg) or - P (O) (ORg) (Rh) where Rg and Rh are independently selected from C1-6 alkyl; p is 1-3; where the values of R13 may be the same or different; q is 0-1; r is 0-3; where the values of R14 may be the same or different; m is 0-2; where the values of R10 may be the same or different; n is 1-3; where the values of R7 can be the same or different; z is 0-3; where the R25 values may be the same or different; R16, R17 and R18 are independently selected from halo, nitro, cyano, hydroxyl, amino, carboxy, carbamoyl, mercapto, sulfamoyl, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1-4 alkoxy, C1- alkanoyl 4, C1-4 alkanoyloxy; N- (C1-4 alkyl) amino, N, N- (C1-4 alkyl) 2amino, C1-4 alkanoylamino, N- (C1-4 alkyl) carbamoyl, NN- (C1-4 alkyl) 2carbamoyl, C1- alkyl 4S (O) where a is between 0 and 2; C1-4 alkoxycarbonyl, N- (C1-4 alkyl) sulfamoyl and N, N- (C1-4 alkyl) 2sulfamoyl; where R16, R17 and R18 can be independently and optionally substituted on a carbon by one or more R21; R19, R20, R23, R27 and R28 are independently selected from halo, nitro, cyano, hydroxy, amino, carboxy, carbamoyl, mercapto, sulfamoyl, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1-4 alkoxy , C1-4 alkanoyl, C1-4 alkanoyloxy, N- (C1-4 alkyl) amino, N, N- (C1-4 alkyl) 2amino, C1-4 alkanoylamino, N- (C1-4 alkyl) carbamoyl, NN- (C1-4 alkyl) 2carbamoyl, C1-4S alkyl (O) where a is between 0 and 2, C1-4 alkoxycarbonyl, N- (C1-4 alkyl) sulfamoyl and N, N- (C1-4 alkyl) 2sulfamoyl ; carbocyclyl, heterocyclyl, sulfo, sulfino, amidino, phosphono, -P (O) (ORa) (ORb), -P (O) (OH) (ORa), -P (O) (OH) (Ra) or -P (O) (ORa) (Rb), where Ra and Rb are independently selected from C1-6 alkyl; where R19, R20, R23, R27 and R28 can be independently and optionally substituted by one or more R22; R21 and R22 are independently selected from halo, hydroxy, cyano, carbamoyl, ureido, amino, nitro, carboxy, carbamoyl, mercapto, sulfamoyl, trifluoromethyl, trifluoromethoxy, methyl, ethyl, methoxy, ethoxy, vinyl, allyl, ethynyl, methoxycarbonyl, formyl , acetyl, formamide, acetylamino, acetoxy, methylamino, dimethylamino, N-methylcarbamoyl, N, N-dimethylcarbamoyl, methylthio, methylsulfinyl, mesyl, N-methylsulfamoyl and N, N-dimethylsulfamoyl; or a salt, solvate, solvate of said salt or prodrug acceptable for pharmaceutical use thereof. These compounds are used as inhibitors of ileal bile acid transport (IBAT) for the treatment of hyperlipidemia. It also describes the processes for its manufacture and the pharmaceutical compositions and combinations that contain them.
priorityDate 2000-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 85.