http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CO-5011121-A1
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c76ecadad74a1a35270b3e3a34d60f37 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D249-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C33-46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C327-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D231-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D233-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D275-03 |
classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-00 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-454 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C323-60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K45-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-427 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C327-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-425 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C211-45 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P13-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C327-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D275-03 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D275-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D521-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C33-46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 |
filingDate | 1999-06-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1b41f851d28cc0849bb9fa03f0b7ff74 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0e53f1a04d2c5ca445e2088cbf2b7fbb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0c2f0be474b1416b00f0f61c871819f4 |
publicationDate | 2001-02-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CO-5011121-A1 |
titleOfInvention | USEFUL ISOTIAZOL DERIVATIVES AS ANTI-TARGET AGENTS |
abstract | A compound of the formula: or a pharmaceutically acceptable salt, prodrug or solvate thereof in which X1 is O or S; R1 is H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, -C (O) (C1-C10 alkyl), - (CH2) -C6 -C10 aryl), - (CH2) t (heterocycle of 4-10 links), -C (O) (CH2) (C6-C10 aryl), or -C (O) (CH2) (5-10 link heterocycle), in which t is an integer in the range from 0 to 5; said alkyl group optionally includes 1 or 2 heteroradicals selected from O, S and -N (R6) - with the proviso that two O atoms, two S atoms or an O and S atom are not directly linked to each other , said aryl, heterocyclic R1 groups are optionally fused to a C6-C10 aryl group, a C5-C8 saturated cyclic group, or a 5-10 link heterocyclic group; 1 or 2 carbon atoms in the above heterocyclic radicals are optionally substituted with an oxy radical (= O); the radicals - (CH2) t - of the above R1 groups optionally include a double or triple carbon-carbon bond in which t is an integer from 2 to 5; and the above R1 groups, except H are optionally substituted with 1 to 3 R4 groups; R2 is selected from the list of substituents provided in the definition of R1, -SO2 (CH2) t (C6-C10 aryl), -SO2 (CH2) t (5-10 link heterocycle), and -OR5, t is a integer in the range of 0 to 5, the radical - (CH2) t - of the above R2 groups optionally include a double or triple carbon-carbon bond in which t is an integer from 2 to 5, and the above groups R2 are optionally substituted with 1 to 3 R4 groups; or R1 and R2 can be joined with the nitrogen to which they are attached to form a 4-10 link monocyclic or poly-saturated ring or a 5-10 link heteroaryl ring, wherein said saturated and heteroaryl rings optionally include 1 or 2 heteroatoms selected from O, S and -N (R6) - in addition to the nitrogen to which R1 and R2 are attached, said -N (R6) - is optionally = N- or -N = in which R1 and R2 are together as said heteroaryl group, said optionally saturated ring may be partially unsaturated including 1 or 2 double carbon-carbon bonds, and said saturated and heteroaryl rings, which include the R6 group of said -N (R6) - is optionally substituted with 1 to 3 groups R4; R3 is H, C1 AND # 8209 alkyl; C10, C2 alkenyl # 8209; C10, C2 alkynyl # 8209; C10, AND # 8209; (CH2) t (aryl C6 AND # 8209; C10), or AND # 8209; (CH2) t (5-10 link heterocycle), in which t is an integer between 0 and 5; said alkyl group optionally includes 1 or 2 heteroradicals selected from O, S and AND # 8209; N (R6) AND # 8209; with the proviso that two atoms of O, two atoms of S or one atom of O and S, are not directly linked to each other; said aryl and heterocyclic groups R3 are optionally fused to an aryl group C6 AND # 8209; C10, a saturated cyclic group C5 AND # 8209; C8 or a heterocyclic group of 5AND # 8209; 10 links; 1 or 2 carbon atoms in the above heterocyclic heterocyclics are optionally substituted with an oxo radical (= O); the radicals AND # 8209; (CH2) t of the interior R3 groups optionally include a carbonAND bond # 8209; double or triple carbon in which t is an integer from 2 to 5, and the above groups R3 are optionally substituted with 1 to 5 R4 groups; each R4 is independently selected from C1 alkyl AND # 8209; C10, C2-C10 alkenyl, C2-C10 alkynyl, halo, cyano, nitro, trifluoromethyl, trifluoromethoxy, azido, AND # 8209; OR5, AND # 8209; C (O) R5, AND # 8209; C (O) OR5, -NR6 C (O) OR5, -OC (O) R5, AND # 8209; NR6 SO2 R5, -SO2 NR5 R6, -NR6 C (O) R5, AND # 8209; C (O) NR5 R6, AND # 8209; NR5 R6, AND # 8209; S (O) j R7 in which j is an integer in the range of 0 to 2, AND # 8209; SO3 H, AND # 8209; NR5 (CR6 R7) j OR6, AND # 8209; (CH2) t (aryl C6-C10), AND # 8209; SO2 (CH2) t (aryl C6 -C10), AND # 8209; S (CH2) t (aryl C6 AND # 8209; C10), AND # 8209; O (CH2) t (5-10 link heterocycle), and - (CR6 R7) m OR6, where m is an integer in the range of 1 to 5 and t is an integer in the range of 0 to 5; said alkyl group optionally contains 1 or 2 heteroradicals selected from O, S and AND # 8209; N (R6) AND # 8209; with the proviso that two atoms of O, two atoms of S or one atom of O and S, are not directly linked to each other; said aryl and heterocyclic groups R4 are optionally fused to an aryl group C6 AND # 8209; C10, a saturated cyclic group C5 AND # 8209; C8 or a heterocyclic group of 5AND # 8209; 10 links; 1 or 2 carbon atoms in the above heterocyclic heterocyclics are optionally substituted with an oxo radical (= O); and the alkyl, aryl and heterocyclic radicals of the above R4 groups are optionally substituted with 1 to 3 substituents independently selected from halo, cyano, nitro, trifluoromethyl, trifluoromethoxy, azido, AND # 8209; NR6 SO2 R5, AND # 8209; SO2 NR5 R6, AND # 8209; C (O) R5, AND # 8209; C (O) OR5, -OC (O) R5, AND # 8209; NR6 C (O) R5, AND # 8209; C (O) NR5 R6 , AND # 8209; NR5 R6, AND # 8209; (CR6 R7) m OR6 in which m is an integer from 1 to 5, AND # 8209; OR5 and the substituents listed in the definition of R5; each R5 is independently selected from H, C1 alkyl AND # 8209; C10, AND # 8209; (CH2) t (C6-C10 aryl), and AND # 8209; (CH2) t (5AND heterocycle # 8209; 10 links) , in which t is an integer from 0 to 5; said alkyl group optionally includes 1 or 2 heteroradicals selected from O, S and AND # 8209; N (R6) AND # 8209; with the proviso that two atoms of O, two atoms of S or one atom of O and S, are not directly linked to each other; said aryl and heterocyclic groups R5 are optionally fused to an aryl group C6 AND # 8209; C10, a saturated cyclic group C5 AND # 8209; C8 or a heterocyclic group of 5AND # 8209; 10 links; and the above substituents R5, except H, are optionally substituted with 1 to 3 substituents independently selected from halo, cyano, nitro, trifluoromethyl, trifluoromethoxy, azido, AND # 8209; C (O) R6, AND # 8209; C (O) OR6, AND # 8209; CO (O) R6, AND # 8209; NR6 C (O) R7, AND # 8209; C (O) NR7 R7, AND # 8209; NR6 R7, hydroxy, C1 alkyl AND # 8209; C6 and C1 AND # 8209 alkoxy; C6; and, each R6 and R7 are independently H or C1 AND # 8209 alkyl; C6; with the proviso that said compound of formula 1AND # 8209; do not be 1AND # 8209; methylAND # 8209; 3AND # 8209; (4AND # 8209; carbamoilAND # 8209; 3AND # 8209; ethoxyAND # 8209; 5AND # 8209; isothiazole) urea, 1,1AND # 8209; dimethylAND # 8209; 3AND # 8209; (4AND # 8209; carbamoilAND # 8209; 3AND # 8209; ethoxyAND # 8209; 5AND # 8209; isothiazole) urea, 1AND # 8209; methylAND # 8209; 3AND # 8209; (4AND # 8209; carbamoilAND # 8209; 3AND # 8209; PropoxyAND # 8209; 5AND # 8209; isothiazol) urea, 1AND # 8209; methylAND # 8209; 3AND # 8209; (4AND # 8209; carbamoilAND # 8209; 3AND # 8209; (methylthio) AND # 8209; 5AND # 8209 ; isothiazole) urea, 1AND # 8209; methylAND # 8209; 3AND # 8209; (4AND # 8209; carbamoilAND # 8209; 3AND # 8209; (ethylthio) AND # 8209; 5AND # 8209; isothiazole) urea, 1,1AND # 8209 ; dimethylAND # 8209; 3AND # 8209; (4AND # 8209; carbamoilAND # 8209; 3AND # 8209; (eiltio) AND # 8209; 5AND # 8209; isothia-zol) urea, 1AND # 8209; methylAND # 8209; 3AND # 8209 ; (4AND # 8209; carbamoilAND # 8209; 3AND # 8209; (propylthio) AND # 8209; 5AND # 8209; isothiazole) urea, 1,1AND # 8209; dimethylAND # 8209; 3AND # 8209; (4AND # 8209; carbamoilAND # 8209; 3AND # 8209; (propylthio) AND # 8209; 5AND # 8209; isothiazole) urea or 1AND # 8209; methylAND # 8209; 3AND # 8209; (4AND # 8209; carbamoilAND # 8209; 3AND # 8209; (isopropylthio) AND # 8209; 5AND # 8209; isothiazole) urea. |
priorityDate | 1998-06-04-04:00^^<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: 64.