http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-046272-A1

Outgoing Links

Predicate Object
assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0a910d33c239980f3a705e312c5bad6a
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C311-46
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-56
filingDate 2004-10-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2005-11-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-046272-A1
titleOfInvention DIPEPTIDIL PEPTIDASA IV INHIBITORS
abstract The compounds herein are valuable in the treatment of the pathological conditions associated with the activity of DPP-IV, such as diabetes mellitus. Processes for the preparation of said compounds, the intermediates used in said processes, pharmaceutical compositions containing said compounds or salts and the use of said compounds or salts are also described. Claim 1: A compound of the formula (1) or a pharmaceutically acceptable salt thereof, wherein Ar is phenyl optionally substituted with 1, 2, 3, 4 or 5 groups independently selected from R9; R9 is selected from halo, C1-6 alkyl (optionally substituted with halo 1-5), C1-6 alkoxy (optionally substituted with 1-5 halo) and cyano; R1 is selected from H and C1-6 alkyl, R2 is selected from H, C1-6 alkyl, C3-8 cycloalkyl, C5-12 cycloalkyl, C6-12 tricycloalkyl, AR1, HET1, -C1-6AR1 alkyl, -C1 alkyl -6AR2, -C1-6 alkyl-C3-8 cycloalkyl, -C1-6HET1 alkyl, -C1-6HET2 alkyl, -C1-6CO2 alkyl C1-6 alkyl, -C1-6CO2 alkylC3-8 alkyl, -C1-6CO2AR1 alkyl, -C1-6CO2HET1 alkyl, -C1-6 alkyl-C1-6 alkyl, -C1-6 alkyl-C3-8 alkylcycloalkyl, C1-6 alkyl -COCO1, -C1-6 alkyl -COHET1, -C1-6 alkyl-C1-6 alkyl, -C1-6 alkyl C3-8, -C1-6COAR1 alkyl, -C1-6COHET1 alkyl, -C1-6 alkyl NHCOC1-6 alkyl, -C1-6 alkylC3-8 alkylcycloalkyl, C1-6NHCOAR1 alkyl, -C1-6CON alkylC1 alkyl 6, -C1-6CON alkylC3-8cycloalkyl, -C1-6 alkyl-C1-6 dialkyl, -C1-6 alkylCONHAR1, -C1-6N alkylC1-6 alkyl, -C1-6N alkyl-C1-6 dialkyl, -alkyl C1-6NHAR1, -C1-6NH alkyl (HET1), -C1-6NHSO2 alkyl C1-6 alkyl, -C1-6SO2 alkylC1-6 alkyl, -C1-6SO2 alkyl, C1-6 alkyl, -SO2C1-6 alkyl and -C1 alkyl 6SO2N-d C1-6 alkyl; or R1 and R2, together with the N to which they are attached, form a ring defined by HET1 or HET3; wherein a ring comprising R1 and R2 is optionally substituted with 1 or 2 substituents independently selected from halo, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, cyano, carboxy, C1-6 carboxy alkyl, -C1-6 alkyl , -CO2C1-6 alkyl, C1-6 alkylamino, di- C1-6 alkylamino, -NHCOC1-6 alkyl, -CONC1-6 alkyl, -CONdi-C1-6 alkyl and HET1; R3 and R4 are independently selected from H, C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, C5-12 cycloalkyl, C1-6 alkyl C3-8 cycloalkyl, C1-6 alkyl C3-8 cycloalkenyl , AR1, AR2, HET1, HET2, - C1-6AR1 alkyl, - C1-6AR2 alkyl, - C1-6HET1 alkyl and - C1-6HET2 alkyl; or R3 and R4 together form a ring defined by C3-8 cycloalkyl, AR2, HET1 or HET2, R5, R6, R7 and R8 are independently selected from H and C1-6 alkyl, wherein any C1-6 alkyl group comprised in any definition of R1, R2, R3, R4, R5, R6, R7 or R8 is optionally substituted with 1 or 2 substituents independently selected from hydroxy and F; wherein any C3-8 cycloalkyl, C3-8 cycloalkenyl, C5-12 bicycloalkyl or C6-12 tricycloalkyl included in any definition of R2, R3 or R4 is optionally substituted; AR1 is optionally substituted phenyl; AR2 is an unsaturated, partially or fully saturated bicyclic carbocyclic ring of 8, 9 or 10 members, optionally substituted; HET1 is an unsaturated, partially or completely saturated monocyclic heterocyclic ring of 3, 4 or 6 members, optionally substituted containing up to 4 heteroatoms independently selected from O, N and S (although without any content of OO, OS or SS links), bound by means of a C atom, or an N atom of the ring if the ring were not quaternized and where any free C, S or N atom can oxidize; HET2 is an unsaturated, partially or fully saturated bicyclic heterocyclyl ring of 8, 9 or 10 members, optionally substituted, containing up to four heteroatoms independently selected from O, N and S (although without OO, OS or SS link content), linked by means of a C atom of the ring in any of the rings comprising the bicyclic system; HET3 is a N-linked bicyclic or tricyclic saturated ring system, containing up to 12 ring atoms, including the N-binding atom; wherein suitable optional substituents on C3-8 cycloalkyl, C5-12 bicycloalkyl, C6-12 tricycloalkyl, AR1, AR2, HET1 and HET2 are 1, 2, 3, 4 or 5 substituents independently selected from phenyl (optionally substituted with halo, trifluoromethyl , C1-4 alkyl or C1-4 alkoxy), halo, C1-6 alkyl, C1-6 haloalkyl, C1-6 dihaloalkyl, trifluoromethyl, C1-6 alkoxy, C1-6 carboxyalkyl, C1-6 carboxyalkoxy, hydroxy, amino, C1-6-amino alkyl, C1-6 dialkyl-amino, -CONH2, -CONH1-6 alkyl, -CON-C1-6 alkyl, -NHCO C1-6 alkyl, -SO2C1-6 alkyl, -S (O) 2NH2, -SO2NHalkyl C1-6, -SO2N1-6alkyl and -NHSO2C1-6alkyl.
priorityDate 2003-10-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

Incoming Links

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Total number of triples: 53.