http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-078550-A1

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filingDate 2010-10-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2011-11-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-078550-A1
titleOfInvention DERIVATIVES OF AZETIDINE AND PIPERIDINE, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM AND THEIR USE FOR THE TREATMENT OF AFFECTIONS MEDIATED BY THE MODULATION OF GPR119
abstract Heterocyclic compounds, pharmaceutical compositions comprising these compounds, and the use of such compounds, in order to treat or prevent the diseases or disorders associated with the activity of GPR119. Claim 1: A compound selected from formula (1), wherein: n is selected from 0, 1, 2, 3 and 4; R1 is selected from -X1S (O) 0-2X2R4a, -X1C (O) OX2R4a, -X1C (O) X2R4a, X1S (O) 0-2X2OR4a, -X1C (O) NR4bX2R4a, -X1S (O) 0 -2X2C (O) R4a, -X1S (O) 0-2X2C (O) OR4a, -X1S (O) 0-2X2OC (O) R4a and -X1S (O) 0-2NR4aR4b; wherein X1 is selected from a bond, O, NR5aR5b and C1-4 alkylene; X2 is selected from a bond and C1-4 alkylene; R4a is selected from hydrogen, halogen, hydroxyl, C1-6 alkyl, C1-6 alkyl substituted by halogen, C1-6 alkyl substituted by hydroxyl, C2-6 alkenyl, C6-10 aryl, heteroaryl, C3-8 heterocycloalkyl, and C3-8 cycloalkyl; wherein this aryl, heteroaryl, cycloalkyl and heterocycloalkyl of R4a is optionally substituted with 1 to 3 radicals independently selected from hydroxyl, halogen, C1-6 alkyl, C1-6 alkyl substituted by halogen, C1-6 alkyl substituted by hydroxyl, C1-6 alkyl substituted by cyano, C1-6 alkoxy, C1-6 alkoxy substituted by halogen, C6-10 aryl-C1-4 alkoxy, and -X3C (O) OX4R5c; wherein R4b is selected from hydrogen and C1-6 alkyl; and R5a and R5b are independently selected from hydrogen and C1-6 alkyl; wherein X3 and X4 are independently selected from a bond and C1-4 alkylene; R5c is selected from hydrogen and C1-6 alkyl; R2 is independently selected from hydrogen, halogen, hydroxyl, C1-6 alkyl, C1-6 alkyl substituted by halogen, C1-6 alkyl substituted by hydroxyl, C1-6 alkoxy, C1-6 alkoxy substituted by halogen, -C ( O) R6, and -C (O) OR6; wherein R6 is selected from hydrogen and C1-6 alkyl; R20 is selected from hydrogen and methyl; W1 and W2 are independently selected from CR7 and N; wherein R7 is selected from hydrogen, halogen, cyano, C1-6 alkyl, and -C (O) OR8; wherein R8 is selected from hydrogen and C1-6 alkyl; Y1 is selected from CH2 and C (O); or Y1 and W2 taken together can form a double bond, where W2 is C, and Y1 is CH; Y2, Y3, Y6 and Y7 are independently selected from N and CR9, where at least two of Y2, Y3, Y6 and Y7 are CR9 where R9 is selected from hydrogen, halogen, hydroxyl, C1-6 alkyl , C1-6 alkyl substituted by halogen, C1-6 alkyl substituted by hydroxyl, C1-6 alkoxy, C1-6 alkoxy substituted by halogen, -C (O) R10, and -C (O) OR10; wherein R10 is selected from hydrogen and C1-6 alkyl; Y4 is selected from O, CR11aR11b, NR11a and S (O) 0-2; each R11a and R11b is independently selected from hydrogen and C1-6 alkyl; wherein the alkyl of R11a or R11b is optionally substituted with hydroxyl, C1-4 alkyl, halogen, C1-4 alkyl substituted by halogen, C1-4 alkoxy, C1-4 alkoxy substituted by halogen, and -NR12aR12b; wherein R12a and R12b are independently selected from hydrogen and C1-4 alkyl; Y5 is selected from (CR13aR13b) 1-3; wherein R13a and R13b are independently selected from hydrogen, halogen, and C1-6 alkyl; wherein the alkyl of R13a or R13b is optionally substituted with 1 to 5 substituents independently selected from hydroxyl, C1-4 alkyl, halogen, C1-4 alkyl substituted by halogen, C1-4 alkoxy, and C1-4 alkoxy substituted by halogen; or R13a and R3, together with the atoms with which they are attached, form oxetan-3-yl; R3 is selected from C6-10 aryl, and heteroaryl; wherein this aryl or heteroaryl of R3 is optionally substituted with 1 to 4 radicals R14; wherein each R14 is independently selected from hydrogen, C1-6 alkyl, halogen, cyano, C1-6 alkoxy, halogen substituted C1-6 alkyl, halogen substituted C1-6 alkoxy, C3-8 cycloalkyl and C1- heterocycloalkyl 10; wherein the alkyl, cycloalkyl, heterocycloalkyl and alkoxy of R14 is optionally substituted by 1 to 3 groups selected from C1-6 alkyl, halogen, C1-6 alkoxy, halogen substituted C1-6 alkyl, and substituted C1-6 alkoxy by halogen; and pharmaceutically acceptable salts thereof.
priorityDate 2009-10-09-04:00^^<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: 48.