http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-045047-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_96b882006e755dfc56fcabfc5fb019f6 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-52 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-50 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-52 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-513 |
filingDate | 2004-07-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2005-10-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | AR-045047-A1 |
titleOfInvention | ARILO AND HETEROARILO DERIVATIVES TRISUSTITUIDOS AS MODULATORS OF METABOLISM AND PROFILAXIS AND TREATMENT OF DISORDERS RELATED TO THEMSELVES |
abstract | The compounds herein are useful in the prophylaxis or treatment of metabolic disorders and complications thereof such as diabetes and obesity. Claim 1: A compound of formula (1) or a salt, hydrate or solvate or N-oxide thereof, in which: A and B are each C1-3 alkylene optionally substituted with 1 to 4 substituents selected from the group consisting in C1-3 alkyl, C1-4 alkoxy, carboxy, cyano, C1-3 haloalkyl and halogen; D is O, S, S (O), S (O) 2, CR2R3 or N-R2; E is N, C or CR4; the double line (from points up and continues down) is a single link when E is N or CR4, or a double link when E is C; V1 is selected from the group consisting of C1-3 alkylene, ethynylene and C1-2 heteroalkylene optionally substituted with 1 to 4 substituents selected from the group consisting of C1-3 alkyl, C1-4 alkoxy, carboxy, cyano, C1-3 haloalkyl and halogen; or V1 is a link; V2 is C3-6 cycloalkylene or C1-3 alkylene where each is optionally substituted with 1 to 4 substituents selected from the group consisting of C1-3 alkyl, C1-4 alkoxy, carboxy, cyano, C1-3 haloalkyl and halogen; or V2 is a link; W is NR5, O, S, S (O), or S (O) 2; or W is absent; Q is NR6, O, S, S (O) or S (O) 2; X is N or CR7; Y is N or CR8; Z is selected from the group consisting of C1-5 acyl, C1-5 alkoxy, C2-6 alkenyl, C1-4 alkoxy, C1-8 alkyl, C1-4 alkylcarboxamide, C2-6 alkynyl, C1-4 alkylthiocarboxamide, C1 alkylsulfonamide -4, alkylsulfinyl 1-4, alkylsulfonyl C1-4, alkylthio C1-4, alkylthioureyl C1-4, alkylureyl C1-4, amino, alkylamino C1-2, dialkylamino C2-4, carbamimidoyl, carbo-alkoxy C1-6, carboxamide , carboxy, cyano, C3-7 cycloalkyl, C4-8 diacylamino, C2-6 dialkylcarboxamide, C2-6 dialkylthiocarboxamide, C2-6 dialkylsulfonamide, C2-6 dialkylsulfonylamino, formyl, C1-4 haloalkoxy. C1-4 haloalkyl, C1-4 haloalkylcarboxamide, C1-4 haloalkylsulfinyl, C1-4 haloalkylsulfonyl, C1-4 haloalkylthio, halogen, aryl, heterocyclic, heteroaryl, hydroxyl, hydroxycarbamimidoyl, hydroxylamino, nitro and tetrazolyl, where C1-8 alkyl, cycloalkyl C3-7, and heterocyclic are each optionally substituted with 1, 2, 3 or 4 groups selected from the group consisting of C1-5 acyl, C1-5 acyloxy, C1-4 alkoxy, C1-7 alkyl, C1-4 alkylcarboxamide , C 1-4 alkylsulfonamide, C 1-4 alkylsulfinyl, C 1-4 alkylsulfonyl, C 1-4 alkylthio, C 1-4 alkylureyl, amino, C 1-2 alkylamino, C 2-4 dialkylamino, C 1-6 carbo alkoxy, carboxyamide, carboxy, cyano, formyl, C1-4 haloalkoxy, C1-4 haloalkylsulfinyl, C1-4 haloalkylsulfonyl, C1-4 haloalkylthio, halogen, hydroxyl, hydroxylamino and nitro, and wherein said C1-7 alkyl is optionally substituted with amino; or Z is a group of the formula (A); wherein R9 is H, C1-8 alkyl or C3-7 cycloalkyl; and R10 is H, nitro or nitrile; Ar1 is aryl or heteroaryl each optionally substituted with R11, R12, R13, R14, and R15; where R11 is selected from the group consisting of C1-5 acyl, C1-6 acylsulfonamide, C1-5 acyloxy, C2-6 alkenyl, C1-4 alkoxy, C1-8 alkyl, C1-4 alkylamino, C1-6 alkylcarboxamide, alkylthiocarboxamide C1-4, C2-6 alkynyl, C1-4 alkylsulfonamide, C1-4 alkylsulfinyl, C1-4 alkylsulfonyl, C1-4 alkylthio, C1-4 alkylthioureyl, C1-4 alkylureyl, amino, arylsulfonyl, carbamimidoyl, C1- carboxy alkoxy 6, carboxamide, carboxy, cyano, C3-7 cycloalkyl, C3-7 cycloalkyloxy, C2-6 dialkylamino, C2-6 dialkylcarboxamide, C2-6 dialkylthiocarboxamide, guanidinyl, halogen, C1-4 haloalkoxy, C1-4 haloalkyl, C1- haloalkylsulfinyl 4, C1-4 haloalkylsulfonyl, C1-4 haloalkylthio, heterocyclic, heterocyclic-oxy, heterocyclic-sulfonyl, heterocyclic-carbonyl, heteroaryl, heteroarylcarbonyl, hydroxyl, nitro, oxo-cycloalkyl C4-7, phenyl, sulfonamide, sulfonic acid and thiol, and wherein C1-5 acyl, C1-6 acylsulfonamide, C1-4 alkoxy, C1-8 alkyl, C1-4 alkylamino, alkylsulfonam C 1-6, C 1-4 alkylsulfonyl, C 1-4 alkylthio, arylsulfonyl, carbamimidoyl, C 2-6 dialkylamino, heterocyclic, heterocyclic-carbonyl, heteroaryl, phenoxy and phenyl are optionally substituted with 1 to 5 substituents independently selected from the group consisting of C1-5 acyl, C1-5 acyloxy, C2-6 alkenyl, C1-4 alkoxy, C1-7 alkyl, C1-4 alkylamino, C1-4 alkylcarboxamide, C2-6 alkynyl, C1-4 alkylsulfonamide, C1-4 alkylsulfinyl, C 1-4 alkylsulfonyl, C 1-4 alkylthio, C 1-4 alkylureyl, C 1-6 carboxy alkoxy, carboxamide, carboxy, cyano, C 3-7 cycloalkyl, C 3-7 cycloalkyloxy, C 2-6 dialkylamino, C 2-6 dialkylcarboxamide, halogen, C1-4 haloalkoxy, C1-4 haloalkyl, C1-4 haloalkylsulfinyl, C1-4 haloalkylsulfonyl, C1-4 haloalkylthio, heteroaryl, heterocyclic, hydroxyl, nitro, phenyl, and phosphonooxy, wherein said C1-7 alkyl and C1-4 alkylcarboxamide are each optionally substituted with 1 to 5 substituents selected from the group consisting of alkoxy C1-4 and hydroxy, or R11 is a group of formula (B), in which "p" and "r" are each independently 0.1, 2 or 3; and R16 is H, C1-5 acyl, C2-6 alkenyl, C1-8 alkyl, C1-4 alkylcarboxamide, C2-6 alkynyl, C1-4 alkylsulfonamide, C1-6 carboxy-alkoxy, carboxamide, carboxy, cyano, C3 cycloalkyl -7, C2-6 dialkylcarboxamide, halogen, heteroaryl or phenyl, and where the heteroaryl or phenyl are optionally substituted with 1 to 5 substituents independently selected from the group consisting of C1-4 alkoxy, amino, alkylamino, C1-4, C2 alkynyl -6, C2-8 dialkylamino, halogen, C1-4 haloalkoxy, C1-4 haloalkyl and hydroxyl; and R12, R13, R14 and R15 are each independently selected from the group consisting of C1-5 acyl, C1-5 alkoxy, C2-6 alkenyl, C1-4 alkoxy, C1-8 alkyl, C1-4 alkylcarboxamide, C2 alkynyl -6, C1-4 alkylsulfonamide, C1-4 alkylsulfinyl, C1-4 alkylsulfonyl, C1-4 alkylthio, C1-4 alkylureyl, C1-6 carbo alkoxy, carboxamide, carboxy, cyano, C3-7 cycloalkyl, C2-6 dialkylcarboxamide , halogen, C1-4 haloalkoxy, C1-4 haloalkyl, C1-4 haloalkylsulfinyl, C1-4 haloalkylsulfonyl, C1-4 haloalkylthio, hydroxyl and nitro; or two adjacent groups selected from the group consisting of R12, R13, R14 and R15 together with the atoms to which they are attached form a 5, 6 or 7 membered cycloalkyl, cycloalkenyl or heterocyclic group that is fused with Ar1, where the group 5, 6 or 7 members is optionally substituted with halogen; R1, R7 and R8 are each independently selected from the group consisting of H, C1-5 alkoxy, C2-6 alkenyl, C1-4 alkoxy, C1-8 alkyl, C1-4 alkylcarboxamide, C2-6 alkynyl, C1- alkylsulfonamide 4, C1-4 alkylsulfinyl, C1-4 alkylsulfonyl, C1-4 alkylthio, C1-4 alkylureyl, amino, C1-4 alkylamino, C2-8 dialkylamino, carboxamide, cyano, C3-7 cycloalkyl, C2-6 dialkylcarboxamide, C2 dialkylsulfonamide -6, halogen, C1-4 haloalkoxy, C1-4 haloalkyl, C1-4 haloalkylsulfinyl, C1-4 haloalkylsulfonyl, C1-4 haloalkylthio and hydroxyl; R2 is selected from the group consisting of C1-8 alkyl, amino, aryl, carboxamide, carboxy, cyano, C3-6 cycloalkyl, C1-4 haloalkoxy, C1-4 haloalkyl, halogen, heteroaryl and hydroxyl; and wherein C1-8 alkyl, aryl or heteroaryl are optionally substituted with 1 to 5 substituents selected from the group consisting of C1-5 acyl, C1-5 acyloxy, C1-4 alkoxy, C1-8 alkyl, C1-4 alkylamino, alkylcarboxamide C1-4, C 1-4 alkylthiocarboxamide, C 1-4 alkylsulfonamide, C 1-4 alkylsulfinyl, C 1-4 alkylsulfonyl, C 1-4 alkylthio, C 1-4 alkylthioureyl, C 1-4 alkylureyl, amino, carboxyC 1-6 alkoxy, carboxamide, carboxy, cyano, C3-6 cycloalkyl, C3-6 cycloalkyl C1-3 heteroalkylene, C2-8 dialkylamino, C2-6 dialkylcarboxamide, C2-6 dialkylthiocarboxamide, C2-6 dialkylsulfonamide, C1-4 alkylthioureyl, haloC 1-4 haloalkoxy C1-4, C1-4 haloalkylsulfinyl, C1-4 haloalkylsulfonyl, C1-4 haloalkyl, C1-4 haloalkylthio, halogen, heterocyclic, hydroxy, hydroxylamino and nitro; or R2 is -Ar2-Ar3 where Ar2 and r3 are each independently aryl or heteroaryl optionally substituted with 1 to 5 substituents selected from the group consisting of H, C1-5 acyl, C1-5 acyloxy, C1-4 alkoxy, C1 alkyl -8, C 1-4 alkylcarboxamide, C 1-4 alkylthiocarboxamide, C 1-4 alkylsulfinyl, C 1-4 alkylsulfonyl, C 1-4 alkylthio, amino, C 1-4 alkylamino, C 1-6 carbo-alkoxy, carboxamide, carboxy, cyano, C3 cycloalkyl -6, C2-8 dialkylamino, C2-6 dialkylcarboxamide, C1-4 haloalkoxy, C1-4 haloalkyl, halogen, hydroxyl and nitro; or R2 is a group of formula (C); in which: R17 is H, C1-8 alkyl, C3-7 cycloalkyl, aryl, heteroaryl or OR19; and R18 is F, Cl, Br, CN, or NR20R21; where R19 is H, C1-8 alkyl or C3-7 cycloalkyl, and R20 and R21 are each independently H, C1-8 alkyl, C3-7 cycloalkyl, aryl or heteroaryl; or R2 is a group of the formula (D); in which G is i) -C (O) -, - C (O) NR23-, -C (O) O-, -OC (O) NR23-, -NR23C (O) O-, -OC (O ) -, - C (S) -, -C (S) NR23-, -C (S) O-, -OC (S) -, -CR23R24-, -O-, -S-, -S (O) - or S (O) 2- when D is CR2R3, or ii) -CR23R24C (O) -, -C (O) -, -CR23R24C (O) NR25-, -C (O) NR23-, -C (O ) O-, -C (S) -, -C (S) NR23-, -C (S) O-, -CR23R24-, -S (O) 2-, or a link when D is NR2, where R23, R24 and R25 are each independently H or C1-8 alkyl, and R22 is H, C1-8 alkyl, C2-6 alkynyl, C3-7 cycloalkyl, phenyl, heteroaryl, or heterocyclic each optionally substituted with 1 to 5 selected substituents from the group consisting of C1-5 acyl, C1-5 acyloxy, C2-6 alkenyl, C1-4 alkoxy, C1-7 alkyl, C1-4 alkylamino, C1-4 alkylcarboxamide, C1-4 alkylthiocarboxamide, C1-4 alkylsulfonamide, C 1-4 alkylsulfinyl, C 1-4 alkylsulfonyl, C 1-4 alkylthio, C 1-4 alkylthioureyl, C 1-4 alkylureyl, amino, C 1-6 carboxy alkoxy, carboxamide, carboxy, cyano, C 3-7 cycloalkyl, C 2-8 dialkylamino, C2-6 dialkylcarboxamide, C2 dialkylthiocarboxamide -6, C2-6 dialkylsulfonamide, C1-4 alkylthioureyl, C1-4 haloalkoxy, C1-4 haloalkyl, C1-4 haloalkylsulfinyl, C1-4 haloalkylsulfonyl, haloa |
priorityDate | 2003-07-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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