http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2691084-T3

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filingDate 2014-08-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2018-11-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_609b2c2edc727d61aa7a58dcdbc6368d
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bee7f163f285e5e8ceab1396828e5035
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publicationDate 2018-11-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2691084-T3
titleOfInvention Bicyclic Calicrein Plasma Inhibitors
abstract A compound of formula (I), ** Formula ** wherein W is selected from CH and N; X is selected from CH, CH2-CH2, CH> = CH, N and NH; Y is selected from CH2, CH, N, NH and O; wherein the bond between X and Y ("---") is saturated, unsaturated, or aromatic; B is selected from i) a radical of formula II ** Formula ** and ii) a 6.5- or 6,6-heteroaromatic fused bicyclic ring, containing N and, optionally, one or two additional heteroatoms independently selected from N , O and S, which is optionally mono, di or trisubstituted with a substituent selected from alkyl, alkoxy, OH, halo, CN, COOR8, CONR8R9, CF3 and NR8R9; P is H and Q is -C (R20) (R21) NH2, or P is -C (R20) (R21) NH2 and Q is H; U and V are independently selected from C and N such that the aromatic ring containing U and V is phenyl, pyridine or pyridazine; R1 is absent when U is N; R2 is absent when V is N; or, when present, R1 and R2 are independently selected from H, alkyl, alkoxy, CN, halo and CF3; R3 is selected from H, alkyl, alkoxy, CN, halo and CF3; A is selected from phenyl substituted heteroaryl; and - (CH2) 0-3 phenyl optionally substituted with heteroaryl, - (CH2) 1-3-heteroaryl or - (CH2) 1-3-NR14R15; R8 and R9 are independently selected from H and alkyl; R20 and R21 are independently selected from H and alkyl, or can together form a cycloalkyl ring or a cyclic ether; alkyl is a linear saturated hydrocarbon having up to 10 carbon atoms (C1-C10) or a branched saturated hydrocarbon having between 3 and 10 carbon atoms (C3-C10); Alkyl can be optionally substituted with 1 or 2 substituents independently selected from (C1-C6) alkoxy, OH, CN, CF3, COOR10, CONR10R11, fluoro and NR10R11; cycloalkyl is a monocyclic saturated hydrocarbon of 3 to 7 carbon atoms; a cyclic ether is a monocyclic saturated hydrocarbon of 4 to 7 carbon atoms, in which one of the carbons in the ring is replaced by an oxygen atom; alkoxy is a linear O-linked hydrocarbon of 1 to 6 carbon atoms (C1-C6) or a branched O-linked hydrocarbon of 3 to 6 carbon atoms (C3-C6); alkoxy can be optionally substituted with 1 or 2 sub-constituents independently selected from OH, CN, CF3, COOR10, CONR10R11, fluoro and NR10R11; aryl is phenyl, biphenyl, or naphthyl; aryl can be optionally substituted with 1, 2 or 3 substituents independently selected from alkyl, alkoxy, methylenedioxy, ethylenedioxy, OH, halo, CN, morpholinyl, piperidinyl, heteroaryl, - (CH2) 0-3 -O-heteroaryl, arilob, - O-arilob, - (CH2) 1-3 -arylob, - (CH2) 1-3 -heteroaryl, - COOR10, -CONR10R11, - (CH2) 1-3 -NR14R15, CF3 and -NR10R11; arilob is phenyl, biphenyl or naphthyl, which can be optionally substituted with 1, 2 or 3 substituents independently selected from alkyl, alkoxy, OH, halo, CN, morpholinyl, piperidinyl, -COOR10, -CONR10R11, CF3 and NR10R11; Heteroaryl is a 5-, 6-, 9-, or 10-membered mono or bicyclic aromatic ring containing, where possible, 1, 2, or 3 ring members independently selected from N, NR8, S, and O; Heteroaryl can be optionally substituted with 1, 2 or 3 substituents independently selected from alkyl, alkoxy, OH, halo, CN, aryl, morpholinyl, piperidinyl, - (CH2) 1-3 -aryl, heteroarylob, -COOR10, -CONR10R11, CF3 and -NR10R11; Heteroaryl is a 5-, 6-, 9-, or 10-membered mono or bicyclic aromatic ring, containing, where possible, 1, 2, or 3 ring members independently selected from N, NR8, S, and O; wherein heteroarylob can be optionally substituted with 1, 2 or 3 substituents independently selected from alkyl, alkoxy, OH, halo, CN, morpholinyl, piperidinyl, aryl, - (CH2) 1-3 -aryl, -COOR10, -CONR10R11, CF3 and NR10R11; R10 and R11 are independently selected from H and alkyl; or R10 and R11 together with the nitrogen to which they are attached form a 4-, 5-, 6- or 7-membered heterocyclic ring which may be saturated or unsaturated with 1 or 2 double bonds; R14 and R15 are independently selected from alkyl, arilob, and heteroarylob; or R14 and R15 together with the nitrogen to which they are attached form a 4-, 5-, 6-, or 7-membered heterocyclic ring that may be saturated or unsaturated with 1 or 2 double bonds, and optionally may be oxo-substituted; and tautomers, stereoisomers (including enantiomers, diastereoisomers, and racemic and squamous mixtures thereof), pharmaceutically acceptable salts and solvates thereof.
priorityDate 2013-08-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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