http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-066143-A2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a7f82940e47ba7a1188f8e2ffca55e0f |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-7052 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-455 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-74 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-337 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-397 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-655 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P7-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-74 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-655 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-337 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7052 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D205-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-455 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-397 |
| filingDate | 2008-02-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2009-07-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-066143-A2 |
| titleOfInvention | COMPOSITIONS AND THERAPEUTIC COMBINATIONS OF STEROL ABSORPTION (ES) WITH CARDIOVASCULAR AGENT (S) AND THE USE OF THE SAME FOR THE PREPARATION OF MEDICINES FOR THE TREATMENT OF VASCULAR AFFECTIONS |
| abstract | Claim 1: A composition characterized in that it comprises, (i) at least one sterol absorption inhibitor or its acceptable for pharmaceutical use; and (ii) at least one cardiovascular agent for the treatment of cardiovascular conditions that is different from at least one sterol absorption inhibitor; wherein the at least one sterol absorption inhibitor represented by (a) formula (1) or its isomers, or salts or solvates acceptable for pharmaceutical use of the compounds of the formula (1) or its isomers, or prodrugs of the compounds of the formula (1) or its isomers, salts or solvates, in which, in the above formula (1): Ar1 is R3-substituted aryl; Ar2 is R4-substituted aryl; Ar3 is R5-substituted aryl; Y and Z are independently selected from the group consisting of -CH2-, -CH (lower alkyl) - and -C- (lower dialkyl) -A is selected from -O-, -S-. -S (O) - or -S (O) 2; R1 is selected from the group consisting of -O (CO) R6, -O (CO) OR9 and -O (CO) NR6R7; R2 is selected from the group consisting of hydrogen, lower alkyl, and aryl; or R1 and R2 together are = O; q is 1, 2, or 3; p is 0, 1, 2, 3 or 4; R5 is substituents 1-3 that are independently selected from the group consisting of -OR6, -O (CO) R6, -O (CO) OR9, -O (CH2) 1-5OR9, -O (CO) NR6R7, -NR6R7, -NR6 (CO) R7, -NR6 (CO) OR9, -NR6 (CO) NR7R8, -NR6SO2-lower alkyl, NR6SO2-aryl-, -CONR6R7, -COR6, -SO2NR6R7, S (O) 0-2aryl, -O (CH2) 1-10-COOR6, -O (CH2) 1-10CONR6R7, o-halogen, m-halogen, o-lower alkyl, m-lower alkyl, - (lower alkylene) -COOR6, and -CH = CH-COOR6; R3 and R4 are independently substituents 1-3 that are independently selected from the group consisting of hydrogen, p-lower alkyl, aryl, -NO2, -CF3 and p-halogen; R6, R7 and R8 are independently selected from the group consisting of hydrogen, lower alkyl, aryl and lower aryl-substituted alkyl; and R9 is lower alkyl, aryl or lower aryl-substituted alkyl; (b) formula (2) or isomers of the compounds of the formula (2), or salts or solvates that are acceptable for pharmaceutical use of the compounds of the formula (2) or of the isomers of the compounds of the formula (2) ), or prodrugs of the compounds of the formula (2) or of the isomers, salts or solvates of the compounds of the formula (2), in which, in the above formula (2): A is selected from the group to be it is formed by R2-substituted heterocycloalkyl, R2-substituted heteroaryl, R2-substituted benzofused heterocycloalkyl, and R2-substituted benzofused heteroaryl; Ar1 is R3-substituted aryl; Ar2 is R4-substituted aryl; Q is a bond or, with the position ring carbon 3 of azetidinone, forms the spiro group of formula (3); and R1 is selected from the group consisting of: (CH2) q, in which q is from 2 to 6, provided that when Q forms a spiro ring, q can also be zero or 1; - (CH2) eG- (CH2) r-, in which G is -O-, -C (O) -, phenylene, -NR8 or S (O) 0-2, e is 0-5 and r is 0- 5, provided that the sum of eyr is 1-6; - (C2-6 alkenylene) and - (CH2) fV- (CH2) g- in which V is C3-6 cycloalkylene, f is 1-5 and g is 0-5, provided that the sum of fyg is 1-6 ; R5 is selected from:> CH-,> C- (C1-6 alkyl) -,> CF-,> C (OH) -,> C (C6H4-R9) -,> N-, or s + NO-- ; R6 and R7 are independently selected from the group consisting of -CH2, -CH (C1-6 alkyl) -, -C (di- C1-6 alkyl) -, -CH = CH- and -C (alkyl C1-6) = CH-; or R5 together with adjacent R6, or R5 together with an adjacent R7, form a group -CH = CH- or a -CH = C (C1-6 alkyl) -: a and b are independently 0, 1, 2, or 3 , provided that the two are not zero; provided that when R6 is -CH = CH- or -C (C1-6 alkyl) = CH-, a is 1; provided that when R7 is -CH = CH- or -C (C1-6 alkyl) = CH-, b is 1; provided that when it is 2 or 3, the R6 may be the same or different; and provided that when b is 2 or 3, R7 may be the same or different; and when Q is a link, R1 can also be selected from -M-Yd- (CR10R11) -Zh, -Xm- (CR12R13) s-Yn- (CR10R11) t-Zp- or -Xj- (CR10R11) v- Yk-S (O) 0-2-; where M is -O-, -S-, -S (O) - or -S (O) 2-; X, Y and Z are independently selected from the group consisting of -CH2-, -CH (C1-6 alkyl) - and -C (di-C1-6 alkyl); R10 and R12 are independently selected from the group consisting of -OR14, -O (CO) R14, -O (CO) OR15 and -O (CO) NR14R15; R11 and R13 are independently selected from the group consisting of hydrogen, (C1-6) alkyl and aryl; or R10 and R11 together are = O, or R12 and R13 together are = O; d is 1, 2 or 3; h is 0, 1, 2, 3 or 4; s is 0 or 1; t is 0 or 1; m, n and p are independently 0-4; provided that at least one of s and t is 1; and the sum of m, n, p, s and t is 1-6; provided that when p is 0 and t is 1, the sum of m, s and n is 1-5; and provided that when p is 0 and s is 1, the sum of m, t and n is 1-5; v is 0 or 1; j and k are independently 1-5, provided that the sum of j, k and v is 1-5; R2 is substituents 1-3 in the ring carbon atoms that are selected from the group consisting of hydrogen, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkenyl, R17-substituted aryl, R17-substituted benzyl, R17-substituted benzyloxy, R17-substituted aryloxy, halogen, -NR14R15, NR14R15 (C1-6 alkylene) -, NR14R15C (O) (C1-6 alkylene) -, -NHC (CO ) R16, OH, C1-6 alkoxy, -OC (O) R16, -COR14, hydroxy-C1-6 alkyl, C1-6 alkoxy C1-6 alkyl, NO2, S (O) 0-2R16, -SO2NR14R15 and - ( C1-6 alkylene) COOR14 when R2 is a substituent on a heterocycloalkyl ring, R2 is as defined, or is = O or a moiety of formula (4); and, wherein R2 is a substituent in a substitutable ring nitrogen, is hydrogen, C1-6 alkyl, aryl, C1-6 alkoxy, aryloxy, C1-6 alkylcarbonyl, arylcarbonyl, hydroxy, - (CH2) 1-6CONR18R18, or a remainder of the formula group (5); in which J is -O-, -NH-, -NR18- or -CH2; R3 and R4 are independently selected from the group consisting of substituents 1-3 that are independently selected from the group consisting of C1-6 alkyl, -OR14, -O (CO) R14, -O ( CO) OR16, -O (CH2) 1-5OR14, -O (CO) NR14R15, -NR14R15, -NR14 (CO) R15-NR14 (CO) OR16, -NR14 (CO) NR15R19, -NR14SO2R16, -COOR14, - CONR14R15, -COR14, -SO2NR14R15, S (O) 0-2R16, -O (CH2) 1-10-COOR14, -O (CH2) 1-10CONR14R15, - (C1-6 alkylene) -COOR14, -CH = CH -COOR14, -CF3, -CN, -NO2 and halogen; R8 is hydrogen, C1-6 alkyl, aryl C1-6 alkyl, -C (O) R14 or COOR14; R9 and R17 are independently groups 1-3 that are independently selected from the group consisting of hydrogen, C1-6 alkyl, C1-6 alkoxy, COOH, NO2, NR14R15, OH and halogen; R14 and R15 are independently selected from the group consisting of hydrogen, C1-6 alkyl, aryl and aryl-substituted C1-6 alkyl; R16 is C1-6 alkyl, aryl, or R17-substituted aryl; R18 is hydrogen or C1-6 alkyl; and R19 is hydrogen, hydroxy or C1-6 alkoxy; (c) formula (6) or its isomers, or salts or solvates that are acceptable for pharmaceutical use of the compounds of the formula (6) or their isomers, or prodrugs of the compounds of the formula (6) or their isomers , salts or solvates in which, in the above formula (6): Ar1 is aryl, R10-substituted aryl or heteroaryl; Ar2 is aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X and Y are independently selected from the group consisting of -CH2-, -CH (lower alkyl) - and -C- (lower dialkyl) -; R is -OR6, -O (O) R6, or -O (CO) OR9 or -O (CO) NR6R7; R1 is hydrogen, lower alkyl or aryl; or R and R1 together are = O; q is 0 or 1; r is = 0, 1 or 2; m and n are independently 0, 1, 2, 3, or 5; provided that the sum of m, n and q is 1, 2, 3, 4, or 5; R4 is substituents 1-5 that are independently selected from the group consisting of lower alkyl, -OR6, -O (CO) R6, -O (CO) OR9, -O (CH2) 1-5OR6, -O (CO) NR6R7, -NR6R7, NR6 (CO) R7, -NR6 (CO) OR9, -NR6 (CO) NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S (O) 0-2R9 , -O (CH2) 1-10-COOR6, O (CH2) 1-1OCONR6R7, - (lower alkylene) COOR6, -CH = CH-COOR6; R5 is substituents 1-5 that are independently selected from the group consisting of -OR6, -O (CO) R6, -O (CO) OR9, -O (CH2) 1-5OR6, -O (CO) NR6R7, -NR6R7, -NR6 (CO) R7, -NR6 (CO) OR9, -NR6 (CO) NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S (O) 0-2R9, - O (CH2) 1-10-COOR6, -O (CH2) 1-10CONR6R7, -CF3, -CN, -NO2, halogen, - (lower alkylene) COOR6 and -CH = CH-COOR6; R6, R7 and R8 are independently selected from the group consisting of hydrogen, lower alkyl, aryl, and substituted lower alkyl of aryl; and R9 is lower alkyl, aryl or substituted lower alkyl of aryl. R10 is substituents 1-5 which are independently selected from the group consisting of lower alkyl, -OR6, -O (CO) R6, -O (CO) OR9, -O (CH2) 1-5OR6, -O (CO) NR6R7, -NR6R7, -NR6 (CO) R7, -NR6 (CO) OR9,.-NR6 (CO) NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, -S (O) 0-2R9, -O (CH2) 1-10-COOR6, -O (CH2) 1-10CONR6R7, -CF3, -CN, -NO2 and halogen; (d) formula (7) or isomers of the compounds of the formula (7), or salts or solvates that are acceptable for pharmaceutical use of the compounds of the formula (7) or of the isomers of the compounds of the formula (7 ), or prodrugs of the compounds of the formula (7) or of the isomers, salts or solvates of the compounds of the formula (7), in which: R1 is> CH-,> C (lower alkyl) -,> CF-,> C (OH) -. > C (C6H5) -,> C (C6H4-R15) -,> N- or s + NO--; R2 and R3 are independently selected from the group consisting of: -CH2-, -CH (lower alkyl) -, -C (lower dialkyl) -, -CH = CH- and -C (lower alkyl) = CH -; or R1 together with an adjacent R2, or R1 together with an adjacent R3, form a group -CH = CH- or one -CH = C (lower alkyl) -; u and v are independently 0, 1, 2, or 3, provided that both are not zero; |
| priorityDate | 2001-01-26-04:00^^<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: 60.