http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-044516-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 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/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-517 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-84 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-84 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-02 |
| filingDate | 2004-04-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_860303ddb1a7c6992a4c20931f0c1289 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0ac56f022e1f12f3103957e041628e9b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b07ba79f85f967da025030bdaf1ee900 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_87319e35619b3108ce5c462631e535b6 |
| publicationDate | 2005-09-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-044516-A1 |
| titleOfInvention | DERIVATIVES OF QUINAZOLINE, COMPOSITIONS THAT CONTAIN THEM, PREPARATION AND USES OF THE SAME AS INHIBITORS OF THE P38 PROTEINQUINASE |
| abstract | Method of preparation and pharmaceutical compositions containing them. Claim 1: A compound having the formula (1), or a pharmaceutically acceptable isomer, prodrug, or salt thereof, wherein, Q is -C (R1R2R3); R 1 is selected from hydrogen, C 1-8 alkyl, C 1-8 hydroxylalkyl, and C 1-8 alkoxyC 1-8 alkyl; R2 and R3 are selected from: (i) independently of: (a) hydrogen, since if R1 is hydrogen, only one of R2 and R3 can be selected from hydrogen; (b) C1-8 alkyl; (c) C1-8 alkyl substituted with one, two, or three of halogen, cyano, -OR8, -SR8, -C (= O) R8, -C (O) 2R8, -C (= O) NR8R9, - S (O) pR10, -C (O) 2NR8R9, -S (O) 2NR8R9, and / or -NR8R9; (d) -OR8, -SR8, -C (= O) R8, -C (O) 2R8, -C (= O) NR8R9, -S (O) pR10, -C (O) 2NR8R9, and -S ( O) 2NR8R9; (e) C3-7 cycloalkyl, substituted C3-7 cycloalkyl, heterocycle, substituted heterocycle, C3-7 cycloalkyl C1-8 alkyl, C3-7 cycloalkyl C1-8 alkyl substituted, C1-8 heterocycloalkyl, and substituted C1-8 heterocycloalkyl; or alternatively, (ii) R2 and R3 are taken together to form an optionally substituted C3-7 cycloalkyl or heterocycle ring; R4 and R5 are independently selected from hydrogen, halogen, cyano, C1-8 haloalkyl, and C1-8 haloalkoxy, since R4 and R5 are not both hydrogen; R6 may be attached to the C5, C7, and / or C8 carbon atoms of the quinazoline ring, and when attached to the C5 carbon atom is C1-4 alkyl and when attached to C7 and / or C8 is independently selected from C1-8 alkyl, halogen, cyano, nitro, hydroxy, C1-8 alkoxy, C1-8 haloalkoxy, amino, C1-8 alkylamino, and C1-8 alkyl substituted with one or two of halogen, cyano, nitro, hydroxy, alkoxy C1-8, C1-8 haloalkoxy, amino, and / or C1-8 alkylamino; R7 is attached to any available carbon atom of the phenyl ring and in each case is independently selected from C1-8 alkyl, substituted C1-8 alkyl, halogen, cyano, nitro, hydroxy, C1-8 alkoxy, C1-8 haloalkoxy, amino , and C1-8 alkylamino; R8 and R9 are (i) independently selected from hydrogen, C1-8 alkyl, C1-8 haloalkyl, C1-8 hydroxyalkyl, C1-8 alkoxy C1-8 alkyl, substituted C3-7 cycloalkyl, substituted C3-7 cycloalkyl, heterocycle, and heterocycle replaced; or (ii) when R8 and R9 are attached to the same nitrogen atom (such as in -C (O) 2NR8R9, -S (O) 2NR8R9, and -NR8R9), R8 and R9 can be taken together to form a heterocycle ring optionally substituted; R 10 is C 1-8 alkyl, C 1-8 hydroxyalkyl, C 1-8 alkoxyC 1-8 alkyl, C 3-7 cycloalkyl, substituted C 3-7 cycloalkyl, heterocycle, or substituted heterocycle; m is 0, 1, 2 or 3; n is 0, 1 or 2; and p is 1 or 2; wherein the term "substituted cycloalkyl" is a cycloalkyl group with one, two or three substituents independently selected from the group consisting of halo, C1-8 haloalkyl, C1-8 haloalkoxy, cyano, nitro, -Y-Rs, -Y-cycloalkyl C3-7, -Y-heterocyclyl, -Y-ORs, -Y-NRsRt, -YC (= O) Rs, -YC (O) 2Rs, -YC (= O) NRsRt, -YC (O) 2NRSRt, - YS (O) 0-2Rs, -Y-NRS (O) 2Rs, -Y- S (O) 2NRsRt, and / or -Y-NRC (= O) NRsRt, where Y is absent or is an alkylene group, R is hydrogen, C1-4 alkyl, or C1-4 hydroxylalkyl, and Rs and Rt are independently selected from hydrogen, C1-8 alkyl, C3-7 cycloalkyl, and heterocycle, except when said substituent is -YS (O) 1- 2Rs or -Y-NRS (O) 2Rs, then Rs in these cases is not hydrogen, and in each case, each of Rs and / or Rt in turn is optionally substituted with one or two of C1-4 alkyl, halo , cyano, hydroxy, C1-8 alkoxy, amino, C1-8 alkylamino, C1-8 haloalkyl, C1-8 haloalkoxy, C1-8 hydroxyalkyl, C1-8 alkoxy C1-8 alkyl, C1-8 aminoalkyl, C1-8 alkylamino C1-8 alkyl, -SO2 (C1-8 alkyl), CO2H, CO2 (C1-8 alkyl), C (= O) H, and / or C (= O) C1-8 alkyl; the term "aryl" indicates a monovalent, monocyclic or bicyclic fraction of 6 to 10 atoms in the ring in which at least one of the rings is an aromatic, carbocyclic portion, understanding, however, that the point of attachment will be in the ring aromatic; the term "substituted aryl" is an aryl group as defined above, with one or more substituents independently selected from the group consisting of halo, C1-8 haloalkyl, C1-8 haloalkoxy, cyano, nitro, -Y-Rp, -Y - aryl, -Y-heteroaryl, -Y-C3-7 cycloalkyl, -Y-heterocyclyl, -Y-ORp, -Y-NRpRq, -YC (= O) Rp, -YC (O) 2Rp, -YC (= O) NRpRq, -YC (O) 2NRpRq, -YS (O) 0-2Rp, -Y-NRS (O) 2Rq, -YS (O) 2NRpRq, and / or -Y-NRC (= O) NRpRq, in where Y is absent or a C1-4 alkylene group, R is hydrogen, C1-4 alkyl, or C1-4 hydroxylalkyl, and Rp and Rq are independently selected from hydrogen, C1-8 alkyl, aryl, heteroaryl, C3-7 cycloalkyl , and heterocycle, except when said substituent is -YS (O) 1-2Rp or -Y-NRS (O) 2Rp, then Rp in these cases is not hydrogen, and in each case, each of Rp and / or Rq a in turn it is optionally substituted with one or two of C1-8 alkyl, halo, cyano, hydroxy, C1-8 alkoxy, amino, C1-8 alkylamino, C1-8 haloalkyl, C1-8 haloalkoxy, hydroxyalkyl C1-8, C1-8 alkoxy C1-8 alkyl, C1-8 aminoalkyl, C1-8 alkylamino C1-8 alkyl, -SO2 (C1-8 alkyl), CO2H, CO2 (C1-8 alkyl), C (= O) H , and / or C (= O) C1-8 alkyl; the term "heterocycle" "heterocyclyl" or "heterocyclic" indicates a saturated or partially unsaturated non-aromatic monocyclic or bicyclic fraction of 3 to 10 ring atoms, in which one or two ring atoms are heteroatoms selected from N, O, or S (O) n (where n is an integer from 0 to 2), the remaining atoms in the ring are carbon atoms, and in addition, one or two carbon atoms can be replaced by a carbonyl group, and in the case of a bicyclic heterocycle, one of the two rings may be a non-aromatic carbocyclic with the point of attachment, being in the heterocyclic ring; the term "substituted heterocycle" indicates a heterocycle group with one, two or three substituents selected from the group consisting of halo, C1-8 haloalkyl, C1-8 haloalkoxy, cyano, nitro, -Y-Rs, -Y- C3-7 cycloalkyl , -Y-heterocyclyl, -Y-ORs, -Y-NRsRt, -YC (= O) Rs, -YC (O) 2Rs, -YC (= O) NRsRt, -YC (O) 2NRsRt, -YS (O ) 0-2Rs, -Y-NRS (O) 2Rs, -YS (O) 2NRsRt, and / or -Y-NRC (= O) NRsRt, where Y, R, Rs and Rt are as defined above for substituted cycloalkyl groups, such that Rs and Rt are, in turn, in each case independently optionally substituted with one to two additional groups as recited above in the definition for substituted cycloalkyl; the term "heteroaryl" indicates a monovalent, monocyclic aromatic fraction of 5 to 10 ring atoms containing one, two, three or four ring heteroatoms, each independently selected from N, O, or S, the ring atoms being remaining carbon, and this also includes such rings with a second ring fused thereto of five or six ring atoms, wherein the second fused ring can be aromatic or non-aromatic and can be carbocyclic, heterocyclic, or a heteroaryl ring, meaning, however, that in such cases the point of attachment will be in the aromatic ring containing at least one heteroatom; the term "substituted heteroaryl" is a heteroaryl ring as defined above having one, two or three substituents selected from the group consisting of halo, C1-8 haloalkyl, C1-8 haloalkoxy, cyano, nitro, -Y-Rp, -Y -aryl, -Y-heteroaryl, -Y-C3-7 cycloalkyl, -Y-heterocyclyl, -Y-ORp, -Y-NRpRq, -YC (= O) Rp, - YC (O) 2Rp, -YC (= O) NRpRq, -YC (O) 2NRpRq, -YS (O) 0-2Rp, -Y-NRS (O) 2Rp, -YS (O) 2NRpRq, and / or -Y-NRC (= O) NRpRq, in where Y, R, Rp and Rq are as defined above for substituted aryl groups, such as Rp and Rq are, in turn, in each case independently optionally substituted with one to two additional substituents as referred to above in the definition of substituted aryls; the term "substituted alkyl" indicates a C1-8 alkyl group with one, two, three or four substituents, independently selected from the group consisting of halo, C1-8 haloalkoxy, trifluoromethyl, cyano, nitro, -ORa, -SRa, -S (O) Rc, -S (O) 2Rc, -C (= O) Ra, -C (= O) NRaRb, -C (O) 2Ra, -C (O) 2NRaRb, -S (O) 2NRaRb, - NRaRb, aryl, substituted aryl, heteroaryl, substituted heteroaryl, C3-7 cycloalkyl, substituted C3-7 cycloalkyl, heterocycle, and / or substituted heterocycle, wherein Ra and Rb are independently selected from hydrogen, C1-6 alkyl, aryl, heteroaryl , C3-7 cycloalkyl, and heterocycle, and Rc is selected from C1-6 alkyl, aryl, heteroaryl, C3-7 cycloalkyl, and heterocycle, and each of Ra, Rb, and Rc in turn is optionally substituted with one two or three of C1-8 alkyl, halo, C1-8 haloalkyl, hydroxy, C1-8 alkoxy, C1-8 haloalkoxy, cyano, amino, C1-8 alkylamino, SO2 (C1-8 alkyl), CO2H, CO2 (C1 alkyl -8), C (= O) H, and / or C (= O) C1-8 alkyl, and / or a C1-4 alkyl substitute gone with one to two halo, hydroxy, C1-8 alkoxy, C1-8 haloalkoxy, cyano, amino, C1-8 alkylamino, -SO2 (C1-8 alkyl), CO2H, CO2 (C1-8 alkyl), C ( = O) H, and / or C (= O) C1-8 alkyl; the term "heteroalkyl" indicates an alkyl fraction, wherein one, two or three hydrogen atoms have been replaced with a substituent independently selected from the group consisting of -ORd, -NRdRe, and S (O) nRd (where n is a number integer from 0 to 2), understanding that the point of attachment of the heteroalkyl fraction is through a carbon atom, where Rd and Re are selected from hydrogen, C1-8 alkyl, substituted C1-8 alkyl (but not including arylalkyl or heteroarylalkyl), C3-7 cycloalkyl, substituted C3-7 cycloalkyl, heterocycle, and substituted heterocycle, except when Rd is attached to S (O) nRd and n is 1 or 2, then Rd is not hydrogen, and when Rd and Re they are attached to the same nitrogen atom, these can be taken together to form an optionally substituted heterocyclyl or heteroaryl ring. |
| priorityDate | 2003-04-16-04:00^^<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: 45.