http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2905755-T3

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filingDate 2017-07-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2022-04-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_675aeb1741f1849ad0a550f37d65aaec
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_82e1bfc7be9d87220b55808feff39963
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publicationDate 2022-04-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2905755-T3
titleOfInvention Piperidine derivatives
abstract A compound of formula (I) **(See formula)** in which the two piperidine ring substituents: R1-CO- and -NH-CO-Ar1-Ar2, are in relative trans configuration; Ar1 represents a 5-membered heteroarylene group selected from oxazol-diyl, isoxazol-diyl, oxadiazol-diyl or triazol-diyl, in which the group -NH-CO- and Ar2 are bound in meta arrangement with ring atoms of Ar1; wherein said 5-membered heteroarylene is unsubstituted or monosubstituted with RAr1; in which RAr1 represents methyl, methoxy, fluorine, chlorine, trifluoromethyl or trifluoromethoxy; Ar2 represents phenyl or 6-membered heteroaryl; wherein said 6-membered phenyl or heteroaryl is independently mono-, di-, or trisubstituted, wherein the substituents are independently selected from fluoro, chloro, methyl, cyano, methoxy, or fluoro(C1 ); R1 represents RN1RN2N-, where · RN1 represents -hydrogen; - (C1-6)alkyl; -(C1-6)alkyl which is monosubstituted with -hydroxy; - alkoxy (C1-3); - 2-hydroxy-ethoxy; - -CO-NH2; - -SO2-(C1-3)alkyl; - cyano; - fluoroalkoxy (C1-3); - -NRN3RN4, in which RN3 and RN4 independently represent hydrogen or (C1-4)alkyl; - (C2-6)alkynyl; - (C2-5)fluoroalkyl; - alkoxy (C1-4); - 2-(2-oxo-pyrrolidin-1-yl)-ethyl; - a -L1-Cy1 group; wherein -L1 represents a direct bond, -(C1-3)alkylene- or -(C3-5)cycloalkylene-; and - Cy1 represents (C3-6)cycloalkyl, wherein said (C3-6)cycloalkyl optionally contains a ring oxygen atom; wherein said (C3-6)cycloalkyl is independently unsubstituted; or monosubstituted with fluoro, methyl or hydroxy, -CO-(1-4C)alkoxy or cyano; or disubstituted with fluoro or trisubstituted with methyl and two fluoro; - a -L2-Ar3 group, in which -L2 represents a direct bond, -(C1-4)alkylene-; *-(C3-5)cycloalkylene-(C0-2)alkylene- wherein said (C3-5)cycloalkylene optionally contains a ring oxygen atom, wherein the asterisk indicates the bond to which Ar3 is attached; *-(C1-2)alkylene-(C3-5)cycloalkylene- wherein said (C3-5)cycloalkylene optionally contains a ring oxygen atom, wherein the asterisk indicates the bond to which Ar3 is attached; or -(C1-3)alkylene- which is monosubstituted with hydroxy, trifluoromethyl or -CO-(C1-4)alkoxy; and - Ar3 represents 5- or 6-membered phenyl or heteroaryl; wherein said independently 5- or 6-membered phenyl or heteroaryl is unsubstituted or mono- or disubstituted; wherein the substituents are independently selected from (C1-4)alkyl, (C1-4)alkoxy, halogen, hydroxy, (C1-3)fluoroalkyl or (C1-3)fluoroalkoxy; wherein, in case Ar3 represents 6-membered heteroaryl which is pyridyl or pyrimidinyl, such pyridyl or pyrimidinyl may additionally be present in the form of the respective N-oxide; and RN2 independently represents hydrogen, (C1-4)alkyl or (C2-3)fluoroalkyl; · o RN1 and RN2 together with the nitrogen atom to which they are attached form a 4 to 6 membered ring selected from -azetidinyl, pyrrolidinyl or piperidinyl; each, independently, - not substituted; - or monosubstituted with fluoro, methyl or hydroxy; - or disubstituted with fluoro; - or monosubstituted with Ar4, in which Ar4 represents 5- or 6-membered phenyl or heteroaryl; wherein said independently 5- or 6-membered phenyl or heteroaryl is unsubstituted or mono- or disubstituted; wherein the substituents are independently selected from (C1-4)alkyl, (C1-4)alkoxy, halogen, (C1-3)fluoroalkyl or (C1-3)fluoroalkoxy; o - morpholinyl; R2 represents · hydrogen; · (C1-6)alkyl; · (C2-6)alkyl that is monosubstituted with (C1-3)alkoxy or hydroxy; · alkenyl (C3-5); · cyano-methyl; · (C2-3)fluoroalkyl; · (C3-8)cycloalkyl-(C0-3)alkyl; wherein (C3-8)cycloalkyl is unsubstituted or mono- or disubstituted wherein the substituents are independently selected from (C1-3)alkyl, fluoro, hydroxy, hydroxy-(C1-3)alkyl ), (C1-3)alkoxy or (C1-3)fluoroalkyl; · thiethan-3-yl; · (C3-8)cycloalkenyl-(C1-3)alkyl; or · Ar5-CH2- in which Ar5 represents 5- or 6-membered phenyl or heteroaryl, in which the 5- or 6-membered phenyl or heteroaryl is independently unsubstituted or mono- or disubstituted in which the substituents are independently selected from (C1-4)alkyl, (C1-4)alkoxy, halogen, (C1-3)fluoroalkyl or (C1-3)fluoroalkoxy; and R3 represents hydrogen or methyl; or one of its pharmaceutically acceptable salts.
priorityDate 2016-07-28-04:00^^<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: 983.