http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2330863-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_fd47318319f20f7f99d9fef1fd3e511b |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-02 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-42 |
| filingDate | 2005-01-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2009-12-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dab28ab93ba90681c0ed906c9b2e3fe5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_951fd09857e9b5108c9c6d9dcdcee0d3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_da27a5ab909885a650d7d936ab8c6bb2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_566ebd57e6585ab6d1f02793b2f17056 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5e081f38c6b97ef7a76d1b51252191e6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_725556dd3343532f7879ba2ed7da6feb |
| publicationDate | 2009-12-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2330863-T3 |
| titleOfInvention | 4-ARILPIRAMIDINAS 2- (AMINO-SUBSTITUTES) AND RELATED COMPOUNDS OF UTILITY FOR THE TREATMENT OF INFLAMMATORY DISEASES. |
| abstract | A compound of the formula I: ** (See formula) ** or a pharmaceutically acceptable salt thereof, in which: R1 and R2 are each, independently, H, C1-3 alkyl or C3-5 cycloalkyl; R3 is H or F; R4 is H, F, -ORA, -C (O) RA, -C (O) ORA or -N (RA) 2 or R3 and R4 together with the carbon atom to which they are attached, form a carbonyl group; wherein each occurrence of RA is, independently, H, C1-3 alkyl or C3-5 cycloalkyl; Ring A is optionally substituted with 1 or 2 independent appearances of R5, where each R5 is independently selected from halo, C1-4 aliphatic, -CN, -ORB, -SRC, -N (RB) 2, -NRBC (O) RB, -NRBC (O) N (RB) 2, -NRBCO2RC, -CO2RB, -C (O) RB, -C (O) N (RB) 2, -OC (O) N (RB ) 2, -S (O) RC, -SO2N (RB) 2, -S (O) RC, -NRBSO2N (RB) 2, -NRBSO2RC or C1-4 aliphatic optionally substituted with halo, -CN, -ORB, - SRC, -N (RB) 2, -NRBC (O) B, -NRBC (O) N (RB) 2, -NRBCO2RC, -CO2RB, -C (O) RB, -C (O) N (RB) 2 , -OC (O) N (RB) 2, -S (O) 2RC, -SO2N (RB) 2, -S (O) RC, NRBSO2N (RB) 2 or -NRBSO2RC, where each occurrence of RB is, independently, H or C1-4 aliphatic; or two RBs in the same nitrogen atom together with the nitrogen atom form a 5-8-membered aromatic or non-aromatic ring which has, in addition to the nitrogen atom, 0-2 ring heteroatoms selected from N, O or S; and each occurrence of RC is, independently, C1-4 aliphatic; Cy1 is selected from: a) a phenyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl or triazinyl ring substituted with an appearance of W in the meta or para position of the ring; or b) a triazolyl, imidazolyl, pyrazolyl, pyrrolyl, thiazolyl, isothiazolyl, thienyl, thiadiazolyl, isoxazolyl, oxazolyl, furanyl or oxadiazolyl ring substituted with an occurrence of W; wherein Cy1 is also optionally substituted with one to three independent occurrences of R6, where each occurrence of R6 is independently selected from -halo, aliphatic C1-8, -CN, -ORB, -SRD, -N (RE) 2, -NREC (O) RB, -NREC (O) N (RE) 2, -NRECO2RD, -CO2RB, -C (O) RB, -C (O) N (RE) 2, -OC ( O) N (RE) 2 -S (O) 2RD, -SO2N (RE) 2, -S (O) RD, -NRESO2N (RE) 2, -NRESO2RD, -C (= NH) -N (RE) 2 or C1-8 aliphatic optionally substituted with halo, -CN, ORB, -SRD, -N (RE) 2, -NREC (O) RB, -NREC (O) N (RE) 2, -NRECO2RD, -CO2RB, - C (O) RB, -C (O) N (RE) 2, -OC (O) N (RE) 2, -S (O) 2RD, -SO2N (RE) 2, -S (O) RD, - NRESO2N (RE) 2, -NRESO2RD or -C (= NH) -N (RE) 2, where each occurrence of RD is aliphatic C1-6 and each occurrence of RE is, independently, H, aliphatic C1-6 , -C (= O) RB, -C (O) ORB or -SO2RB; or two REs in the same nitrogen atom together with the nitrogen atom form a 5-8-membered aromatic or non-aromatic ring which has, in addition to the nitrogen atom, 0-2 ring heteroatoms selected from N, O or S; W is selected from one of: i) -L1-V-L2-R7, where L1 is -CHR13-, where R13 is C1-3 alkyl, OH or OMe, V is NRE, L2 is - (CH2) n- , where n is 1-3 and R7 is -N (RF) 2, NRECOORG, NRECORG, NRESO2RG, an optionally substituted 5-6 membered aryl or heteroaryl group or an optionally substituted 3-8 membered heterocyclyl group, in which RF is, independently, H, C1-6 aliphatic, C6-10 aryl, 3-14 membered heterocyclyl, 5-14 membered heteroaryl, -C (= O) RB, -C (O) ORB or -SO2RB ; or two RFs in the same nitrogen atom together with the nitrogen atom form an optionally substituted 5-8-membered aromatic or non-aromatic ring which has, in addition to the nitrogen atom, 0-2 ring heteroatoms selected from N, O or S; and each occurrence of RG is C1-6 aliphatic, C6-10 aryl, 3-14 membered heterocyclyl or 5-14 membered heteroaryl and wherein R7 is optionally substituted at one or more carbon atoms with 1, 2 or 3 occurrences independent of R11 and in one or several nitrogen atoms substitutable with R12, in which each occurrence of R11 is independently selected from C1-6 aliphatic, 6-10 membered aryl, 5-10 membered heteroaryl, - N (RB) 2, = O, halo, NO2, CN, -ORB, -C (O) RA, -CO2RA, -SRC, -S (O) RC, -S (O) 2RC, -OS (O) 2RC-, N (RB) C (O) RA, -N (RB) CO2RA, -N (RB) SO2RA, -C (O) N (RB) 2, -SON (RB) 2, -N (RB) C (O) N (RB) 2 or -OC (O) RA and each occurrence of R12 is independently selected from H, aliphatic C1-6, 6-10 membered aryl, 5-10 membered heteroaryl, -C (= O) RB or -SO2RB; ii) -V-R8, wherein V is NH- and R8 is an optionally substituted group selected from piperidinyl, azetidinyl or pyrrolidinyl; V is -O- or -COO- and R8 is C1-6 alkyl; or V is -CH2 or SO2 and R8 is an optionally substituted group selected from: ** (See formula) ** in which R8 is optionally substituted in one or two carbon atoms with one or two occurrences of C1-4 alkyl, phenyl, 5-14 membered heteroaryl, halo, -COOH, -COO (C1-4 alkyl), -CONH2, -CONH (C1-4 alkyl), -CON (C1-4 alkyl) 2, -CONH (heteroaryl of 5-14 members), -CN, -NH2, -OH, -O (C1-4 alkyl), -NH (C1-4 alkyl), -N (C1-4 alkyl) 2, = O or C1-4 alkyl substituted with one or two independent appearances of phenyl, 5-14 membered heteroaryl, halo, -COON, -COO (C1-4 alkyl), -CONH2, -CONH (C1-4 alkyl), -CON (C1-4 alkyl ) 2, -CONH (5-14 membered heteroaryl), -CN, -NH2, -OH, -O (C1-4 alkyl), -NH (C1-4 alkyl) or -N (C1-4 alkyl) 2 and R8 is optionally substituted on a nitrogen atom with -C 1-4 alkyl, -COO (C 1-4 alkyl) or -SO 2 (C 1-4 alkyl); or iii) -L1-V-R8, wherein L1 is -CH2-, V is -NRC- or NRECO- and R8 is an optionally substituted group selected from C1-6 alkyl or a 5-6 membered heteroaryl group or a 3-7 membered heterocyclyl group, wherein R8 is unsubstituted or R8 is substituted at one or two carbon atoms with one or two occurrences of C1-4 alkyl, phenyl, 5-14 membered heteroaryl, halo, -COON , -COO (C1-4 alkyl), -CONH2, -CONH (C1-4 alkyl), -CON (C1-4 alkyl) 2, -CONH (5-14 membered heteroaryl), -CN, -NH2, - OH, -O (C1-4 alkyl), -NH (C1-4 alkyl), -N (C1-4 alkyl) 2, = O or C1-4 alkyl substituted with one or two independent occurrences of phenyl, heteroaryl of 5 -14 members, halo, -COON, -COO (C1-4 alkyl), -CONH2, -CONH (C1-4 alkyl), -CON (C1-4 alkyl) 2, -CONH (5-14 member heteroaryl) , -CN, -NH2, -OH, -O (C1-4 alkyl), -NH (C1-4 alkyl) or -N (C1-4 alkyl) 2 and R8 is optionally substituted on a nitrogen atom with -alkyl C1-4 or -COO (C1-4 alkyl), -SO2 (C1-4 alkyl), b encyl or CH2 (5-14 membered heteroaryl); Q is a bond, CH2 or C (= O); Cy2 is a C6-10 aryl, a 5-10 membered heteroaryl ring or a 5-10 membered heterocyclyl ring, in which each ring is optionally substituted with one to three independent occurrences of R9 and an occurrence of R10, where each occurrence of R9 is independently selected from aliphatic C1-4, -N (RB) 2, halo, NO2, -CN, -ORB, C (O) RA, -CO2RA, -SRC, -S (O ) RC, -S (O) 2RC, -OS (O) 2RC-, N (RB) C (O) RA, -N (RB) CO2RA, -N (RB) SO2RA, -C (O) N (RB ) 2, -SO2N (RB) 2, -N (RB) C (O) N (RB) 2, -OC (O) RA or C1-4 aliphatic optionally substituted with -N (RB) 2, halo, NO2, -CN, -ORB, -C (O) RA, -CO2RA, -SRC, -S (O) RC, -OS (O) 2RC, -S (O) 2RC, -N (RB) C (O) RA , -N (RB) CO2RA, -N (RB) SO2RA, -C (O) N (RB) 2, -SO2N (RB) 2, -N (RB) C (O) N (RB) 2 or -OC (O) RA and R10 is selected from phenyl or a 5-6 membered heterocyclyl or heteroaryl ring, with the proviso that: 1) when Cy1 is phenyl substituted at the meta position with W, then: a) when W is - OMe, R1, R2, R3 and R4 are each hydrogen and Q is a bond, ent times when ring A is further substituted with R5, R5 is a group other than -CF3; and b) when W is -OMe, R1, R2, R3 and R4 are each hydrogen and Q is -CH2-, then Cy2 is different from 1Hbenzimidazol-1-yl; 2) when Cy1 is phenyl substituted at the position for with W and R1, R2, R3 and R4 are each hydrogen, then a) when Q is a bond, W is different from -OMe; b) when Q is -CH2-, W is different from -OMe. |
| priorityDate | 2004-01-08-04:00^^<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: 1237.