http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-054189-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_12a9e9ce63eb0bbf3658453fb50a6d9b |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D307-83 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-404 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D209-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 |
| filingDate | 2006-04-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_03d849d4b4d05cc85816ab3ca0cc2292 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_876f71c40c23d9c163db215b57e27e3b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bb1a09688321304e1b385916bf7973e3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dd76d91e59f050b72b1a4207503330b7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2208c3960da42c400f5ecf15f5cff747 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e34c1df699948bd3e375fd169e1de257 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a3993ecc7d5bd336875c73fb3953f244 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d30236edc7593824a23bcfd87eb061a3 |
| publicationDate | 2007-06-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-054189-A1 |
| titleOfInvention | DERIVATIVES OF INDOL FOR THE TREATMENT OF INFLAMMATORY DISEASES |
| abstract | They are suitable for the treatment of gastrointestinal or respiratory tract disorders or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or carcinogenic diseases, as well as pharmaceutical compositions containing these compounds. Claim 1: Compound of the formula (1), wherein they mean: A is CO, C = NH, C1-6 alkylene or C3-8 cycloalkylene; B1 is phenyl or an aromatic or non-aromatic ring, which may eventually contain one, two or three heteroatoms selected from the oxygen, sulfur and nitrogen group and which may eventually be mono- or polysubstituted with one or more radicals selected from the OH, O- group. C 1-6 alkyl, C 1-6 haloalkyl, halogen, C 1-6 alkyl and C 1-6 haloalkyl; B2 is phenyl or a heteroaryl, which may contain one, two or three heteroatoms selected from the oxygen, sulfur and nitrogen group; X is O, S, NR5 or CR6R7; n is 0, 1, 2 or 3; R1 is H, C1-6 alkyl, C1-6 haloalkyl, COR1.1, COOR1.1, CH2COOR1.1; R1.1 is H or C1-6 alkyl; R2 is H, C1-6 alkyl or haloalkyl; or R1 and R2 together with nitrogen form a non-aromatic heterocycle, which may contain one, two or three heteroatoms selected from the oxygen and nitrogen group; or R2, N, A and B1 together form a bicyclic group of the formula (2), wherein they mean: A is CO, C = NH or C1-3 alkyl; m is 1, 2 or 3; and R3 is H or a radical selected from the group consisting of OH, C1-6 haloalkyl, a C6-10 aryl, a C5-10 heteroaryl and a C3-10 heterocycle, wherein the C3-10 heterocycle and the C5-10 heteroaryl they may contain one, two or three heteroatoms selected from the oxygen, sulfur and nitrogen group, which may be optionally substituted with one or more radicals selected from the group consisting of C1-6 alkyl, C6-10 aryl, optionally C3-8 cycloalkyl by bridge and C1-6 haloalkyl, which may be optionally substituted with a radical of the group consisting of C1-6 alkyl, C1-6 haloalkyl, OH, halogen and C6-10 aryl; R3 is C1-6 alkyl, which may be optionally substituted with one or more radicals selected from the group consisting of hydrogen, OH, CN, CNH2, CNH-C1-6 alkyl, CON (C1-6 alkyl) 2, COOH, COO-C1- alkyl 6, COH, CO-C1-6 alkyl, CO-C6-10 aryl, OH, O-C1-6 alkyl, O-haloC1-6 alkyl, halogen, SH, S-C1-6 alkyl, S-haloC1-6 alkyl, SO2-alkanol C1- 6; SO2-C1-6 alkyl, SO2-haloC1-6 alkyl, SO2-NH2, SO2-NH-C1-6 alkyl, SO2-N (C1-6 alkyl) 2, NO2, NH2, NH1-6 alkyl and N (C1-6 alkyl) 2; or R3 is a radical selected from the group consisting of C3-8 cycloalkyl, C5-8 cycloalkenyl, C1-6 alkyl and alkanol, which may be optionally substituted with one or more radicals selected from the group consisting of C6-10 aryl, C3- cycloalkyl 8, a C5-10 heteroaryl and a C3-10 heterocycle, may optionally be substituted with one or more radicals of the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, CN, CONH2, CONH-C1-6 alkyl, CON (C1-6 alkyl) 2, COOH, COO-C1-6 alkyl, COH, CO1-6 alkyl, COaryl, OH, O-C1-6 alkyl, O-haloC1-6 alkyl, halogen, SH, S-C1-6 alkyl, S-haloC1-6 alkyl, SO2-alkanol C1-6, SO2- C1-6 alkyl, SO2-haloC1-6 alkyl, SO2-NH2, SO2-NH-C1-6 alkyl, SO2-N (C1- alkyl) 6) 2, NO2, NH2, NH2-C1-6 alkyl, N (C1-6 alkyl) 2, a C5-10 heteroaryl and a C3-10 heterocycle, wherein the C5-10 heteroaryl and the C3-10 heterocycle may optionally be substituted with a radical selected from oxo, hydroxyl, halogen, C1-6 alkyl and C1-6 haloalkyl; or R3 is a radical selected from a group consisting of C6-10 aryl, a C6-10 heteroaryl and a C3-10 heterocycle, which may be substituted with one or more radicals selected from the group consisting of aryl, C1-6 alkyl, alkenyl C2-6, C2-6 alkynyl, C1-6 haloalkyl, CO-NH2, CONH-C1-6 alkyl, CON (C1-6 alkyl) 2, COOH, COO-C1-6 alkyl, COH, CO-C1-6 alkyl, CO- C6-10 alkyl, OH, O-C1-6 alkyl, O-haloC1-6 alkyl, halogen, SH, S-C1-6 alkyl, S-haloC1-6 alkyl, SO2-C1-6 alkyl, SO2-alkanol C1-6, SO2-haloalkylC1- 6, SO2-NH2, SO2-NH-C1-6 alkyl, SO2-N (C1-6 alkyl) 2, NO2, NH2, NH-C1-6 alkyl, N (C1-6 alkyl) 2 and N- (SO2- C1-6 alkyl ) (R3.4; or R3 is a radical selected from the group consisting of C1-6 alkyl, C6-10 arylC1-6 alkyl, C5-10 heteroarylC1-6 heteroaryl, C3-7 cycloalkyl, C6-10 aryl, a C5 heteroaryl -10 and a C3-10 heterocycle, which may eventually be substituted with one or more radicals of the group consisting of B, halogen, OH, C1-6 alkyl and oxo; wherein B is a com position of the formula (3), wherein Z1 means H, OH, halogen, C1-6 alkyl, C1-6 alkanol, O (C1-6 alkyl), C6-10 aryl, O-C6-10 aryl, NH2, NHC1- alkyl 6, N (C1-6 alkyl) 2 or C3-7 cycloalkyl; and Z2 means OH, NH2, NH1-6alkyl, N (C1-6alkyl) 2, C1-6alkyl, C3-7mono- or bicyclic cycloalkyl, C3-10mono- or bicyclic heterocycle, C5-10 mono- or bicyclic heteroaryl or C6-10 aryl ; or R3 is a radical selected from the group consisting of C6-10 aryl and a C5-10 heteroaryl, which may eventually be substituted with C1-6 alkyl, which may eventually be substituted with a radical selected from the group consisting of COOR3.3, NR3 .3R3.4, NHCO3.3, NHCOOR3.3, phenyl, wherein the phenyl may optionally be substituted with a radical selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, CN, C1 haloalkyl -6, CONH2, CONH- C1-6 alkyl, CON (C1-6 alkyl) 2, COOH, COO- C1-6 alkyl, COH, CO1-6 alkyl, OH, O-C1-6 alkyl, C1-6 haloalkyl, halogen , SH, S-C1-6 alkyl, S-haloC1-6 alkyl, SO2-C1-6 alkyl, SO2-haloC1-6 alkyl, SO2-NH2, SO2-NH-C1-6 alkyl, SO2-N (C1-6 alkyl) 2, NO2 , NH2, NH1-6 alkyl and N (C1-6 alkyl) 2, a C3-10 heterocycle and a C510 heteroaryl, wherein the C3-10 heterocycle and the C5-10 heteroaryl may be optionally substituted with an oxo group or a methyl group; wherein: R3.3 is H or C1-6 alkyl; R3.4 is H, C1-6 alkyl or C7-11 aralkyl, C5-10 heteroaryl-C1-6 alkylene; or R3 is a radical selected from a group consisting of C6-10 aryl and a C5-10 heteroaryl, which may be optionally substituted with NR3.1R3.2; wherein: R3.1 is H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 haloalkyl, COR3.1.1, COOR3.1.1, CONR3.1.1R3.1.2 or SO2-R3.1.1; and R3.1.1 is H, C1-6 alkyl, C1-6 haloalkyl, C3-6 cycloalkyl or C6-10 aryl; and R3.1.2 is H, C1-6 alkyl, C1-6 haloalkyl, C3-6 cycloalkyl or C6-10 aryl; and R3.2 is H or a radical selected from the group consisting of C1-6 alkyl, C3-6 cycloalkyl and C1-6 haloalkyl, which may be optionally substituted with one or more radicals selected from the group consisting of NH2, NH1-6 alkyl, N (C1-6 alkyl) 2, oxo and a non-aromatic C3-10 heterocycle, which may be substituted with one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, where the non-aromatic C3-10 heterocycle may eventually be substituted with C1-4 alkyl; or R3 is a radical selected from a group consisting of C6-10 aryl and a C5-10 heteroaryl, which is substituted with a C3-10 heterocycle, which may be optionally substituted with one or more radicals selected from the group consisting of C6- aryl. 10, C1-6 alkyl, C3-6 cycloalkyl, CN, C1-6 haloalkyl, CONH2, CONH-C1-6 alkyl, CON (C1-6 alkyl) 2, COOH, COO-C1-6 alkyl, COH, CO-C1-6 alkyl , oxo, OH, O-C1-6 alkyl, halogen, SH, S- C1-6 alkyl, NH2, NH1-6 alkyl and N (C1-6 alkyl) 2; or R3 is benzimidazolyl, which may be optionally substituted with a radical selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl and C3-6 cycloalkyl; and R4 is C1-6 alkyl, C3-8 cycloalkyl, C1-6 haloalkyl, OR4.1, NR4.1R4.2, CN, or halogen; where they mean: R4.1 is H, C1-6 alkyl, C3-8 cycloalkyl or C1-6 haloalkyl; R4.2 is H, C1-6 alkyl, C3-8 cycloalkyl or C1-6 haloalkyl; and R5 is C1-6 alkyl, C3-8 cycloalkyl, C1-6 haloalkyl, COR5.1, CONHR5.1, CON (R5.1) 2, SO2-C1-6 alkyl, SO2-haloC1-6 alkyl, SO2-aryl or a radical selected from the group consisting of R5.2, SO2-C1-6-R5.2 alkyl, and C1-6-R5.2 alkyl, which may be optionally substituted with one or more radicals selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, CN, C1-6 haloalkyl, CONH2, CONH-C1-6 alkyl, CON (C1-6 alkyl) 2, COOH, COO-C1-6 alkyl, COH, CO-C1-6 alkyl, O -C3-6cycloalkyl, O-haloC1-6 alkyl, O-C1-6 alkyl, halogen, SO2-C1-6 alkyl, SO2-NH2, SO2-NH-C1-6 alkyl, SO2-N (C1-6 alkyl) 2, NO2, NH2 , NH-C1-6 alkyl and N (C1-6 alkyl) 2; where they mean: R5.1 is C 1-6 alkyl, C 5-10 heteroaryl-C 1-6 alkylene or C 1-6 aryl-C 1-6 alkylene; and R5.2 is C6-10 aryl or a C5-10 heteroaryl; and R6 is H, C1-6 alkyl or C1-6 haloalkyl; R7 is H, C1-6 alkyl or C1-6 haloalkyl; or R6 and R7 together form a 3-6 member carbocycle; possibly in the form of their racemates, enantiomers, diastereoisomers and eventually in the form of their salts by the addition of pharmacologically tolerable acids, solvates or hydrates, as well as their deuterated forms. |
| priorityDate | 2005-04-28-04:00^^<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: 61.