http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-046258-A1

Outgoing Links

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filingDate 2004-07-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cacd718e9f105804d12e275353852bd8
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5050c137a78dbd92791cd90b2bcd4c16
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publicationDate 2005-11-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-046258-A1
titleOfInvention COMPOUNDS DERIVED FROM PIPERIDINE OR 8-AZA-BICYCLE [3.2.1] OCT-E-IL
abstract Useful compounds for the modulation of the activity of the CCR5 receptor. Process for its preparation. Claim 1: A compound characterized in that it is of the formula (1) wherein: A is absent or is (CH2) 2; R1 is C (O) NR10R11, C (O) 2R12, NR13C (O) R14, NR15C (O) NR16R17, NR18C (O) 2R19, heterocyclyl, aryl or heteroaryl, R10, R13, R15, R16 and R18 are H or C1-6 alkyl; R11, R12, R14, R17 and R19 are C1-8 alkyl (optionally substituted by halo, hydroxy, C1-6 alkoxy, C1-6 haloalkoxy, C3-6 cycloalkyl (optionally substituted by halo), C5-6 cycloalkenyl, S ( C1-4 alkyl), S (O) (C1-4 alkyl), S (O) 2 (C1-4 alkyl), heteroaryl, aryl, heteroaryloxy or aryloxy), aryl, heteroaryl, C3-7 cycloalkyl (optionally substituted by halo or C1-4 alkyl), C4-7 cycloalkyl fused to a phenyl ring, C5-7 cycloalkenyl or heterocyclyl (the same optionally substituted by oxo, C (O) (C1-6 alkyl), S (O) k (C1 -6 alkyl), halo or C1-4 alkyl; or R11, R12, R14 and R17 can also be H; or R10 and R11, and / or R16 and R17 can be joined to form a 4, 5 or 6 membered ring which optionally includes an atom of N, O or S, said ring is optionally substituted by C1-6 alkyl, S (O) 1 (C1-6 alkyl) or C (O) (C1-6 alkyl); R2 is phenyl , heteroaryl or C3-7 cycloalkyl; R3 is H or C1-4 alkyl; R4 is heterocyclyl; n is 1, 2 or 3; the aryl, phenyl and h moieties Eteroaryl is optionally independently substituted by one or more halo, cyano, nitro, hydroxy, OC (O) NR20R21, NR22R23, NR24C (O) R25, NR26C (O) NR27R28, S (O) 2NR29R30, NR31S (O) 2R32, C (O) NR33R34, CO2R36, NR37CO2R31, S (O) qR39, OS (O) 2R49, C1-6alkyl (optionally mono-substituted by S (O) 2R50 or C (O) NR51R52), C2-6 alkenyl, C2 -6 alkynyl, C3-10 cycloalkyl, C1-6haloalkyl, C1-6alkoxy (C1-6) alkyl, C1-6 alkoxy, C1-6haloalkoxy, phenyl, phenyl (C1-4) alkyl, phenoxy, phenylthio, phenylS (O) , phenylS (O) 2, phenyl (C1-4) alkoxy, heteroaryl, heteroaryl (C1-4) alkyl, heteroaryloxy or heteroaryl (C1-4) alkoxy, where any of the above-mentioned phenyl and heteroaryl portions are optionally substituted with halo , hydroxy, nitro, S (C1-4 alkyl), S (O) (C1-4 alkyl), S (O) 2 (C1-4 alkyl), S (O) 2NH2, S (O) 2NH (C1- 4 alkyl), S (O) 2N (C1-4 alkyl) 2, cyano, C1-4 alkyl, C1-4 alkoxy, C (O) NH2, C (O) NH (C1-4 alkyl), C (O ) N (C1-4 alkyl) 2, CO2H, CO2 (C1-4 alkyl), NHC (O) (C1-4 alkyl), NHS (O) 2 (C1-4 al chyl), CF3 or OCF3; unless otherwise stated heterocyclyl is optionally substituted by C1-6 alkyl [optionally substituted by phenyl {it optionally substituted by halo, C1-4 alkyl, C1-4 alkoxy, cyano, nitro, CF3, OCF3, (C1- 4 alkyl) C (O) NH, S (O) 2NH2, C1-4 alkylthio, S (O) (C1-4 alkyl) or S (O) 2 (C1-4 alkyl)} or heteroaryl {the same optionally substituted by halo, C1-4 alkyl, C1-4 alkoxy, cyano, nitro, CF3, (C1-4 alkyl) C (O) NH, S (O) 2NH2, C1-4 alkylthio, S (O) (C1-4 alkyl) or S (O) 2 (C1-4 alkyl)}], phenyl {optionally substituted by halo, C1-4 alkyl, C1-4 alkoxy, cyano, nitro, CF3, OCF3, (C1-4 alkyl) C ( O) NH, S (O) 2NH2, C1-4 alkylthio, S (O) (C1-4 alkyl) or S (O) 2 (C1-4 alkyl)}, heteroaryl {optionally substituted by halo, C1-4 alkyl , C1-4 alkoxy, cyano, nitro, CF3, (C1-4 alkyl) C (O) NH, S (O) 2NH2, C1-4 alkylthio, S (O) (C1-4 alkyl) or S (O) 2 (C1-4 alkyl)}, S (O) 2NR40R41, C (O) R42, C (O) 2 (C1-6 alkyl) (such as tert-butoxycarbonyl), C (O) 2 (phenyl (C1- 2 alkyl) (such as benc iloxycarbonyl), C (O) NHR43, S (O) 2R4, NHS (O) 2, NHR45, NHC (O) R46, NHC (O) NHR47 or NHS (O) 2R48, with the condition that none of the latter Four substituents are linked to an N in the ring. K, l and q are, independently, 0, 1 or 2; R20, R22, R24, R26, R27, R29, R31, R33, R37, R40 and R51 are independently H or C1-6 alkyl; R21, R23, R25, R28, R30, R32, R34, R36, R38, R39, R41, R42, R43, R44, R45, R46, R47, R48, R49, R50 and R52 are independently C1-6 alkyl ( optionally substituted by halo, hydroxy, C1-6 alkoxy, C1-6 haloalkoxy, C3-6 cycloalkyl, C5-6 cycloalkenyl, S (C1-4 alkyl), S (O) (C1-4 alkyl), S (O) 2 (C1-4 alkyl), heteroaryl, phenyl, heteroaryloxy or phenyloxy), C3-7 cycloalkyl, phenyl or heteroaryl; wherein any of the above-mentioned phenyl and heteroaryl moieties are optionally substituted with halo, hydroxy, nitro, S (C1-4 alkyl), S (O) (C1-4 alkyl), S (O) 2 (C1-4 alkyl) , S (O) 2NH2, S (O) 2NH (C1-4 alkyl), S (O) 2N (C1-4 alkyl) 2, cyano, C1-4 alkyl, C1-4 alkoxy, C (O) NH2, C (O) NH (C1-4 alkyl), C (O) N (C1-4 alkyl) 2, CO2H, CO2 (C1-4 alkyl), NHC (O) (C1-4 alkyl), NHS (O) 2 (C1-4 alkyl), C (O) (C1-4 alkyl), CF3 or OCF3; R21R23, R25R28, R30R34R35; R36, R41, R42, R43, R45, R46, R47 and R52 may additionally be H; or a salt acceptable for pharmaceutical use thereof or a solvate thereof.
priorityDate 2003-07-16-04:00^^<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: 63.