http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-066910-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f2d3599fb8f8f479dba95ca9bb504884 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D209-46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 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/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 |
| filingDate | 2008-06-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2009-09-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-066910-A1 |
| titleOfInvention | UROTENSIN II RECEIVER ANTAGONISTS |
| abstract | Use as antagonists of the urotensin II receptor, and pharmaceutical compositions. Claim 1: A compound of the formula (1) in which, A is a bond or is selected from the group consisting of a-1, a-2 optionally unsaturated, a-3, a-4, a-5 optionally unsaturated and optionally unsaturated a-6, in which the lower portion of A is attached, relative to the nitrogen atom of the formula (1), to position 3 or 4 in the benzene ring portion of the formula (1 ) in which, when A is present, then G is hydrogen, or a substituent selected from C1-8 alkyl, C2-8 alkenyl, C3-14 cycloalkyl or a portion -C [(R1) (R11)] - LD, remainder of formula (3), or two C1-4 alkyl substituents, both attached to the common nitrogen atom of the ring of formula (1), thereby forming a quaternary ammonium salt; R1 is selected from the group consisting of hydrogen, C1-8 alkyl, C2-8 alkenyl, and C2-8 alkynyl; R11 is selected from the group consisting of hydrogen, C1-8 alkyl and cyclopropyl; L is absent or is C1-4 alkyl; D is aryl, C3-14 cycloalkyl, C5-14 cycloalkenyl, heterocyclyl, or heteroaryl, in which aryl and heteroaryl is optionally substituted with one, two, three or four substituents independently selected from the group consisting of C1 alkyl -3, C1-3 alkoxy, C2-8 alkenyl, C2-3 alkenyloxy, hydroxy, C1-3 alkylthio, fluorine, chloro, cyano, C1-3 alkylcarbonyl, (C1-3 alkylcarbonyl) amino, (C1-3 alkyl) amino, di (C1-3 alkyl) amino and C2-14 cycloalkyl, in which C3-14 cycloalkyl is optionally substituted with one, two, three or four C1-3 alkyl substituents; R4 is hydrogen or C1-8 alkyl; L2 is -C (R2) (R5) - (CR6R7) r-, in which r is 0, 1 or 2; and in which R5, R6, and R7 are independently hydrogen or C1-3 alkyl; R2 is selected from the group consisting of heteroaryl, phenyl, heterocyclyl and C1-6 alkyl, in which phenyl is optionally substituted with [(R200-C1-6 alkyl) (Ra)] amino, [(R200-sulfonyl) (Ra)] amino or [(hydroxysulfonyl) (Ra)] amino, in which heterocyclyl is optionally substituted with C1-4 alkyl, aryl, heteroaryl, R200-C1-6 alkyl or R200-sulfonyl, and in which C1-6 alkyl is optionally substituted with carboxy, hydroxy, R200, NRaRb, C1-6 alkoxy, R200-C1-6 alkoxy, R200-oxy, R200-thio, aminocarbonyl, C1-6 carboxy-alkoxy, aminocarbonyl-alkoxy C1-6, (C1-6 alkyl) aminocarbonyl, di (C1-6 alkyl) aminocarbonyl, [(R200-C1-6 alkyl) (Ra)] amino, (R200-C1-6 alkyl) 2-amino, (alkyl C1-6-carbonyl) amino, (trihalo-C1-4 alkyl-carbonyl) amino, (R200-C1-6-alkylcarbonyl) amino, (C1-6-alkoxycarbonyl) amino, (R200-C1-6 alkoxy- carbonyl) amino, (C1-6 alkoxy-C1-6 alkylcarbonyl) amino, (R200-carbonyl) amino, (amino- C1-6 alkylcarbonyl) amino, [(C1-6 alkyl) amino-C1-alkyl 4-carbon il] amino, [di (C1-6 alkyl) amino-C1-6 alkyl) amino-C1-6-carbonyl] amino, (C1-6 alkyl-carbonyl-acetonitrile-carbonyl) amino, ureido, thioureido, acetamidino, guanidino, ({[(R200) (Ra)] aminocarbonyl} (Ra)) amino, [(R200-oxycarbonyl) (Ra)] amino, [(R200) (Ra)] aminocarbonyloxy, aminosulfonyl, C1-6 alkyl sulfonyl, hydroxysulfonyl , (C1-6 alkyl sulfonyl) amino, (R200-C1-6 alkyl sulfonyl) amino, (R200-C2-6 alkenyl sulfonyl) amino, (C1-6 alkyl sulfonyl-C1-6 alkyl sulfonyl) amino, R200- sulfonyloxy, aminosulfonyloxy, (C1-6 alkyl) aminosulfonyloxy, di (C1-6 alkyl) aminosulfonyloxy, [(aminosulfonyl) (Ra)] amino, {[(C1-6 alkyl) aminosulfonyl] (Ra)} amino, {[di (C1-6 alkyl) aminosulfonyl] (Ra)} amino, [(hydroxysulfonyl) (Ra)] amino, [(R200-oxysulfonyl) (Ra)] amino, [(R200-sulfonyl) (Ra)] amino, [( R200) (Ra)] aminosulfonyloxy, or ({[(R200) (Ra)] aminosulfonyl} (Rc)) amino; Ra is selected from the group consisting of hydrogen, C1-6 alkyl, C1-6 alkylcarbonyl and C3-8 cycloalkyl; Rb is selected from the group consisting of hydrogen, C1-6 alkyl or R201, R200 is C6-10 aryl, heteroaryl, C3-8 cycloalkyl or heterocyclyl, each optionally substituted with one, two or three independently selected substituents between the group consisting of C1-4 alkyl, trihalo-C1-4 alkyl, C1-4 alkoxy, trihalo-C1-4 alkoxy, C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, amino, C1-6 alkyl amino, C 1-6 dialkyl, (C 1-6 alkylcarbonyl) amino, C 1-6 alkyl sulfonyl, hydroxysulfonyl, aminosulfonyl, chlorine, fluorine, bromine and R202, in which C 3-8 cycloalkyl or heterocyclyl is substituted by optionally with one, two or three oxo substituents on available elements of the carbon atom ring in which heteroaryl having a nitrogen atom ring element is optionally substituted on the ring nitrogen atom with an oxy substituent forming thus an oxide; R201 is C6-10 aryl, heteroaryl, C3-8 cycloalkyl or heterocyclyl, in which aryl, heteroaryl, C3-8 cycloalkyl or heterocyclyl are each optionally substituted with one, two or three substituents independently selected from the group consisting of C1-4 alkyl, trihalo-C1-4 alkyl, C1-4 alkoxy, trihalo-C1-4 alkoxy, amino, C1-6-amino alkyl, C1-6-dialkyl amino, C1-6 alkylcarbonyl, C 1-6 alkoxycarbonyl, (C 1-6 alkylcarbonyl) amino, C 1-6 alkyl sulfonyl, hydroxysulfonyl, aminosulfonyl, chlorine, fluorine, bromine, aryl, heteroaryl, arylC 1-6 alkyl, aryl sulfonyl and heteroaryl -sulfonyl, in which C3-8 cycloalkyl or heterocyclyl is optionally substituted with one, two or three oxo substituents on available elements of the carbon atom ring in which heteroaryl having a nitrogen atom ring element is substituted optionally in the ring nitrogen atom with an oxy substituent thereby forming a n oxide; R202 is aryl, heteroaryl, arylC 1-6 alkyl, [(arylC 1-6 alkyl) (Ra)] amino, hydroxysulfonyl, aryl sulfonyl, heteroaryl sulfonyl or [(heteroaryl sulfonyl) (Ra)] amino, wherein each aryl and heteroaryl is optionally substituted with one, two or three C1-4 alkyl substituents; B is C6-10 aryl, tetralinyl, indanyl, or a heteroaryl selected from the group consisting of pyridin-2-yl, pyridin-4-yl, pyrazol-4-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrazin-2-yl, imidazol-1-yl, thien-2-yl, isoquinolinyl, indolyl, quinolinyl, and thiazol-5-yl, in which B is optionally substituted with one, two or three substituents selected in form independent of the group consisting of C1-4 alkyl, C1-4 alkoxy, fluorinated C1-4 alkoxy, halogen, cyano, hydroxy, aminocarbonyl, C1-4 alkylcarbonyl, C1-4 dialkyl aminocarbonyl, aminosulfonyl, C1-4 alkyl -aminosulfonyl, dialkyl C1-4-aminosulfonyl, hydroxysulfonyl, aminosulfonylamino, alkyl C1-4-aminosulfonylamino, dialkyl C1-4-aminosulfonylamino, aminosulfonyloxy, alkyl C1-4-aminosulfonyloxy, and dialkyl C1-4-aminosulfonyloxy, provided that when B is select from the group consisting of C6-10 aryl, tetralinyl, indanyl, thien-2-yl, and indolyl, then B is independently substituted With two to three substituents selected from the group consisting of C1-3 alkoxy and hydroxy, provided that, when B is phenyl substituted at positions 3,4-, 3,5- or 4,5- with a C1- alkoxy substituent 3 unbranched in each position, then phenyl can be optionally further substituted in a remaining 3-, 4-, or 5- open position with an additional C1-3 alkoxy or a hydroxy substituent; E is hydrogen, halogen, cyano, C1-3 alkyl, C1-3 alkoxy, C2-5 alkenyl, amino, C1-3-alkyl or di-C1-3-alkyl; X is O or S and enantiomers, diastereomers, tautomers, solvates, and salts acceptable for pharmaceutical use. |
| priorityDate | 2007-06-07-04:00^^<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: 77.