http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2886650-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42e94091a4fc81b8d0237117707cc7ee |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-498 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4985 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4709 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5383 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5355 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-404 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-04 |
| filingDate | 2017-11-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2021-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_63e6b621fb3bd45b75d4b6b5c3fdb74c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e7236afc4ef2e990c332af7ffba4e7a5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3d189664fce5357a5da7b361b69a9459 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e6880bf0c37bf4077ae4985b31bb6586 |
| publicationDate | 2021-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2886650-T3 |
| titleOfInvention | Indazole derivatives as alphaV integrin antagonists |
| abstract | A compound of Formulas (Ia) or (Ib): **(See formula)** where A, E, G and J are independently N, C or CH; provided that at least one of A, E, G and J is C bonded to Y; L1 and L2 are each independently C1-4alkylene; X is C1-4 alkylene substituted with 0, 1 or 2 R8a; Y is a covalent bond, O, S, NH, -O-(C1-3 alkylene)-, -S-(C1-3 alkylene)-, or -NH-(C1-3 alkylene)-, in where the C1-3 alkylene is each independently substituted with 0, 1 or 2 R8b; m is an integer of 1 or 2; r is an integer of 0, 1, 2, or 3; R1 is an arginine mimetic moiety selected from the group consisting of **(See formula)** wherein one of the asterisks on each of the arginine mimetic moieties is an X attachment point and the other two asterisks are hydrogen ; R2 is hydrogen, halo, or C1-6 alkyl; R3 is hydrogen, C1-6 alkyl, 3 to 10 membered carbocyclyl, carbocyclylalkyl, 6 to 10 membered aryl, arylalkyl, 3 to 14 membered heterocyclyl, heterocyclylalkyl, 5 to 14 membered heteroaryl, heteroarylalkyl, where alkyl, carbocyclyl, heterocyclyl, aryl and heteroaryl, alone or as part of another group, are each independently substituted with 0, 1, 2 or 3 R6; R3a is hydrogen; or R3a and R3, together with the atom(s) to which they are attached, form a 3- to 6-membered carbocyclic or heterocyclic ring that is optionally substituted with one or more groups independently selected from halo, cyano, hydroxyl, amino, alkyl C1-6, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, haloalkoxy, amido, carbamate, and sulfonamide; R4 is hydrogen, C1-6 alkyl, 3 to 10 membered carbocyclyl, carbocyclylalkyl, 3 to 10 membered heterocyclyl, heterocyclylalkyl, 6 to 10 membered aryl, arylalkyl, 5 to 14 membered heteroaryl, heteroarylalkyl, -S(O )mR7, -C(O)NRaRb, -NHC(O)ORa, -NHC(O)NRaRb, -NHC(O)R7, -OC(O)NRaRb, -OC(O)R7, -NHS(O) mNRaRb, or -NHS(O)mR7; wherein alkyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl, by themselves or as part of another group, are each independently substituted with 0, 1, 2, or 3 R9; R5 is hydrogen, R5a, or a moiety selected from **(See formula)** R5a and R5b are each independently C1-6 alkyl, phenyl, benzyl or 5 to 7 membered heterocyclyl; wherein alkyl, phenyl, and heterocyclyl are each independently substituted with 0 to 3 R5d; R5c is C1-6 alkyl or 5 to 7 membered carbocyclyl; wherein C1-6 alkyl, phenyl, and heterocyclyl are each independently substituted with 0 to 3 R5d; and R5d, at each occurrence, is independently halo, OH, alkoxy, oxo, or alkyl; or alternatively, two adjacent R5d, together with the atoms to which they are attached, form a carbocyclyl moiety; R6 is halo, cyano, hydroxyl, amino, oxo, nitro, -S(O)mR12, C1-6 alkyl, alkoxy, haloalkyl, haloalkoxy, haloaminoalkyl, hydroxyalkyl, aminoalkyl, alkoxycarbonyl, 6- to 10-membered aryl, aryloxy, arylalkoxy, 5 to 10 membered heteroaryl, 3 to 6 membered carbocyclyl, or 3 to 7 membered heterocyclyl; wherein alkyl, aryl, heteroaryl, carbocyclyl, or heterocyclyl, alone or as part of another group, are each independently substituted with 0, 1, or 2 R10; R7 is each independently C1-6 alkyl, C1-6 alkoxy, C1-6 aminoalkyl, C1-6 haloalkyl, 6 to 10 membered aryl, arylalkyl, 5 to 10 membered heteroaryl, cycloalkyl, or heterocycloalkyl; wherein alkyl, aryl, heteroaryl, cycloalkyl, and heterocycloalkyl, alone or as part of another group, are each independently substituted with 0, 1, 2, or 3 R11; R8a and R8b, at each occurrence, are independently halo, cyano, hydroxyl, amino, oxo, C1-6alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, or haloalkoxy; R9 is each independently halo, cyano, hydroxyl, amino, oxo, nitro, C1-6alkyl, alkoxy, haloalkyl, haloalkoxy, haloaminoalkyl, hydroxyalkyl, aminoalkyl, alkoxycarbonyl, 6- to 10-membered aryl, aryloxy, arylalkoxy, heteroaryl, 5 to 10 heteroaryl, 3 to 6 membered carbocyclyl, or 3 to 7 membered heterocyclyl; wherein alkyl, aryl, heteroaryl, carbocyclyl, or heterocyclyl, alone or as part of another group, are each independently substituted with 0, 1, or 2 R13; R10 is halo, cyano, hydroxyl, amino, oxo, C1-6 alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, haloalkoxy, amido, carbamate, or sulfonamide; R11, each occurrence, is independently halo, cyano, hydroxyl, amino, oxo, C1-6alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, or haloalkoxy; R12 is -N(RxRy), C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 hydroxyalkyl, or C1-6 aminoalkyl; R13 is halo, cyano, hydroxyl, amino, oxo, C1-6 alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, haloalkoxy, amido, carbamate, or sulfonamide; Ra and Rb, at each occurrence, are independently hydrogen, C1-6 alkyl, C1-6 haloalkyl, C3-6 cycloalkyl, 6 to 10 membered aryl, 5 to 10 membered heteroaryl, cycloalkylalkyl, arylalkyl, heteroarylalkyl, or alkoxyalkyl; or alternatively, Ra and Rb, taken together with the atoms to which they are attached, form a 3- to 8-membered carbocyclic or heterocyclic ring; wherein aryl and heteroaryl, alone or as part of another group, are each independently substituted with one or more groups independently selected from halo, cyano, hydroxyl, amino, C1-6alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy , haloalkoxy, amido, carbamate and sulfonamide; and carbocyclyl and heterocyclyl, alone or as part of another group, are each independently substituted with one or more groups independently selected from halo, cyano, hydroxyl, amino, oxo, C1-6 alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy , haloalkoxy, amido, carbamate and sulfonamide; Re is OH, amino, amido, carbamate, sulfonamide, C1-4alkyl, halo, C1-4haloalkyl, or C3-6cycloalkyl; Rf is H, CH3, CH2CH3 or C(O)OCH2CH3; Rg is selected from CH3, CH2CCl3, phenyl, 4-fluorophenyl, 4-methoxyphenyl, benzyl; Rx and Ry are each independently hydrogen or C1-6 alkyl; or a pharmaceutically acceptable salt thereof. |
| priorityDate | 2016-11-08-04:00^^<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: 567.