http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-079026-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_bcff13f8573db698307f919e6385d5c4 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-675 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P39-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-6561 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-454 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D495-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-407 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-107 |
| filingDate | 2010-11-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2011-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-079026-A1 |
| titleOfInvention | ANTIGONISTAS DE ESPIRO -OXINDOL OF MDM2 |
| abstract | The compounds and compositions provided herein refer to spiro-oxindoles that function as antagonists of the interaction between p53 and MDM2, and their use as therapeutic agents for the treatment of cancer and other diseases. Claim 1: A compound having Formula (1): wherein: R1a, R1b, R1c and R1d are independently selected from the group consisting of hydrogen, halogen, hydroxy, amino, nitro, cyano, alkoxy, aryloxy, alkyl optionally substituted, haloalkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted cycloalkenyl, optionally substituted aryl, optionally substituted heteroaryl, carboxamido and sulfonamido; R2 is selected from the group consisting of optionally substituted aryl and optionally substituted heteroaryl; R3 is selected from the group consisting of optionally substituted alkyl, (cycloalkyl) optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted cycloalkenyl, optionally substituted aryl and optionally substituted heteroaryl; R4 is selected from the group consisting of hydrogen and optionally substituted C1-6 alkyl; R5 is selected from group (2): in which: each R6 and R6b is independently selected from the group consisting of hydrogen and optionally substituted C1-6 alkyl; R7 is selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl and optionally substituted cycloalkyl; each of R8a and R8b is independently selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl and optionally substituted cycloalkyl; or R8a and R8b taken together with the carbon to which they are attached form an optionally substituted cycloalkyl of 3 to 8 members; W1 is selected from the group consisting of -OR9a and -NR9bR9c; R9a is hydrogen; R9b is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, -SO2R9d and -CONR9eR9f; R9c is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl and optionally substituted heteroaryl; or R9b and R9c taken together with the nitrogen atom to which they are attached form an optionally substituted 4 to 8 membered heterocycle; R9d is selected from the group consisting of optionally substituted alkyl and optionally substituted cycloalkyl; each of R9e and R9f is independently selected from the group consisting of hydrogen, optionally substituted alkyl and optionally substituted cycloalkyl; or R9e and R9f taken together with the nitrogen atom to which they are attached form an optionally substituted 4 to 8 membered heterocycle; W2 is selected from the group consisting of -OR10 and -NR11aR11b; R10 is hydrogen; or one of R9a and R10 is hydrogen and the other is a metabolically cleavable group; with the proviso that when W1 is -OR9a and W2 is -OR10 then at least one of R7, R8a and R8b is different from hydrogen; R11a is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, -SO2R11c and -CONR11dR11e; Rb is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl and optionally substituted heteroaryl; or R11a and R11b taken together with the nitrogen atom to which they are attached form an optionally substituted 4 to 8 membered heterocycle; R11c is selected from the group consisting of optionally substituted alkyl and optionally substituted cycloalkyl; each of R11d and R11e is independently selected from the group consisting of hydrogen, optionally substituted alkyl and optionally substituted cycloalkyl; or R11d and R11e together with the nitrogen atom to which they are attached form an optionally substituted 4 to 8 membered heterocycle; n is 1, 2, 3, 4 or 5; each R12a, R12b, R12c and R12d is independently selected from the group consisting of hydrogen and optionally substituted C1-6 alkyl; R13 is selected from the group consisting of hydrogen and optionally substituted C1-6 alkyl; R14 is selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl and optionally substituted cycloalkyl; Z is selected from the group consisting of -OR15 and -NR16aR16b; or Z and R14 taken together form a carbonyl group; R15 is selected from the group consisting of hydrogen and a metabolically cleavable group; R16b is selected from the group consisting of -SO2R16c and -CONR16dR16e; R16b is selected from the group consisting of hydrogen and optionally substituted alkyl; R16c is selected from the group consisting of optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl and optionally substituted heteroaryl; each of R16d and R16e is independently selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl and optionally substituted heteroaryl; or R16d and R16e taken together with the nitrogen atom to which they are attached form a 4- to 8-membered heterocycle; or is 1, 2 or 3; p is 0, 1, 2 or 3; each R17a, R17b, R17c and R17d is independently selected from the group consisting of hydrogen and optionally substituted C1-6 alkyl; R18 is selected from the group consisting of hydrogen and optionally substituted C1-6 alkyl; R19 is selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl and optionally substituted cycloalkyl; R20 is selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl and optionally substituted cycloalkyl; each of R21a and R21b is hydrogen; or one of R21a and R21b is hydrogen and the other is a metabolically cleavable group; q is 0, 1, 2 or 3; r is 1, 2 or 3; X is selected from the group consisting of O, S and NR '; And it is selected from the group consisting of O, S and NRö; R 'is selected from the group consisting of hydrogen, optionally substituted alkyl, aralkyl and optionally substituted cycloalkyl; Rö is selected from the group consisting of hydrogen, optionally substituted alkyl, aralkyl and optionally substituted cycloalkyl; and --- represents a single bond or a double bond, or a pharmaceutically acceptable salt, solvate or prodrug thereof. |
| priorityDate | 2009-11-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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