http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-061110-A1

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filingDate 2007-05-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2008-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-061110-A1
titleOfInvention DERIVATIVES OF PIRROLIDIN-2-CARBOXAMIDE WITH CAP INHIBITORY ACTION, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM AND THEIR USE IN THE TREATMENT OF RESPIRATORY AFFECTIONS.
abstract Derivatives of pyrrolidin-2-carboxamides and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and the use of such compounds to treat, improve or avoid a condition associated with a channel activating protease, such as respiratory conditions {including but not limited to prostasin, PRSS22, TMPRSS11 (for example, TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2); matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A or neutrophil elastase. Claim 1: A compound of the formula (1) and its salts, hydrates, solvates and stereoisomers acceptable for pharmaceutical use, wherein: J is a 5-12 membered fused monocyclic or carbocyclic ring, an aryl, heteroaryl or heterocyclic ring containing N, O and / or S; R1 is - (CR2) l-NR2, - (CR2) l-NRC (= NR) -NR2, - (CR2) lC (= NR) -NR2 or a non-aromatic, heterocyclic ring containing nitrogen, 5- 7 members; W-R2 is a substituent in any position in ring A; W is -O (CR2) k-, -S (CR2) k-, -S (O) (CR2) k-, -SO2 (CR2) k- or -OC (O) (CR2) k-; R2 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, R6, -CR9 = CR9-R6, or -CR = CanilloE, where ring E is a fused monocyclic or carbocyclic ring, or 5-7 heterocyclic optionally substituted members; or W-R2 together form C1-6 alkyl, a 5-7 membered aryl or -OC (O) NR7R8; R3 is NR7R8 or R6; R4 and R5 are independently H, C1-6 alkyl, OH, or C1-6 alkoxy; R7 and R8 are independently H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or - (CR2) l-R6; or R7 and R8 together with N can form an optionally substituted 5-7 membered fused monocyclic or heterocyclic ring; R9 is H or C1-6 alkyl; R10 is halo, C1-6 alkyl, C1-6 alkoxy, OR11 or - (CR2) l-R11; R6, R11 and X are independently an optionally substituted 5-7 membered carbocyclic ring, heterocyclic ring, aryl or heteroaryl; or R11 is H or C1-6 alkyl; each R is H, or C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, where a carbon may be optionally substituted or replaced with NR, O or S; i is 0-1; k and l are independently 0-6; m and n are independently 1-6; and p is 0-3.
priorityDate 2006-05-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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