http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-106314-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/A61P39-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D209-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4545 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4162 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 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/A61P37-06 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-438 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4427 |
| filingDate | 2016-10-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ee0a21d60dda2dea73637c262bdd24dc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_28564f09a64f7809c841e4ac7ba0be51 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4c69d735bba7eba6e72f9530e3010de9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3d334d25cd7d8871c2b3c9d6789cf45c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9051f154f2f0f0a32d855947928f4c46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6e82754ccf3225a92d5e88ccf9047219 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9a532074c849019827c7bd68c87448a2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_67f981d2eb0424f08c01cf1f66ef3b60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d42292ee5c05b2352b7f9ed64cf01077 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7270222fa9569a56c35c949a4ce09fd5 |
| publicationDate | 2018-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-106314-A1 |
| titleOfInvention | SPIRO[3H-INDOL-3,2’-PYRROLIDIN]-2(1H)-ONE AND DERIVATIVES AS MDM2 INHIBITORS - p53 |
| abstract | The present application discloses compounds as inhibitors of the interaction between MDM2 and p53, pharmaceutical compositions containing compounds of this type, their use as medicaments, especially as agents for the treatment and / or prevention of oncological diseases and synthetic intermediates. Claim 1: A compound characterized by the formula (1), wherein R¹ is a group optionally substituted with one or more Rᵇ¹ and / or Rᶜ¹, identical or different, selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl and 3 to 10 membered heterocyclyl; each Rᵇ¹ is independently selected from -ORᶜ¹, -NRᶜ¹Rᶜ¹, halogen, -CN, -C (O) Rᶜ¹, -C (O) ORᶜ¹, -C (O) NRᶜ¹Rᶜ¹, -S (O) ₂Rᶜ¹, -S (O) ₂NRᶜ¹Rᶜ¹, -NHC (O) Rᶜ¹, -N (C₁₋₄ alkyl) C (O) Rᶜ¹ and the bivalent substituent = O, while = O may only be a substituent in non-aromatic ring systems; each Rᶜ¹, independently of one another, indicates hydrogen or a group optionally substituted with one or more Rᵈ¹ and / or Rᵉ¹, identical or different, selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; each Rᵈ¹ is independently selected from -ORᵉ¹, -NRᵉ¹Rᵉ¹, halogen, -CN, -C (O) Rᵉ¹, -C (O) ORᵉ¹, -C (O) NRᵉ¹Rᵉ¹, -S (O) ₂Rᵉ¹, -S (O) ₂NRᵉ¹Rᵉ¹, -NHC (O) Rᵉ¹, -N (C₁₋₄ alkyl) C (O) Rᵉ¹ and the bivalent substituent = O, while = O may only be a substituent in non-aromatic ring systems; each Rᵉ¹, independently of one another, indicates hydrogen or a group optionally substituted with one or more Rᶠ¹ and / or Rᵍ¹, identical or different, selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; each Rᶠ¹ is independently selected from -ORᵍ¹, -NRᵍ¹Rᵍ¹, halogen, -CN, -C (O) Rᵍ¹, -C (O) ORᵍ¹, -C (O) NRᵍ¹Rᵍ¹, -S (O) ₂Rᵍ¹, -S (O) ₂NRᵍ¹Rᵍ¹, -NHC (O) Rᵍ¹, -N (C₁₋₄ alkyl) C (O) Rᵍ¹ and the bivalent substituent = O, while = O may only be a substituent in non-aromatic ring systems; each Rᵍ¹ is independently selected from hydrogen, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, C₆₋₁₀ aryl, heteroaryl of 5 to 10 members and 3 to 10 membered heterocyclyl; R² and R³, each independently, is selected from hydrogen, C₆₋₁₀ aryl, 5 to 10 membered heteroaryl and 3 to 10 membered heterocyclyl, wherein C₆₋₁₀ aryl, 5 to 10 membered heteroaryl and 3 to heterocyclyl 10 members are optionally substituted with one or more identical or different R y² and / or Rᶜ²; each Rᵇ² is independently selected from -ORᶜ², -NRᶜ²Rᶜ², halogen, -CN, -C (O) Rᶜ², -C (O) ORᶜ², -C (O) NRᶜ²Rᶜ², -S (O) ₂Rᶜ², -S (O) ₂NRᶜ²Rᶜ², -NHC (O) Rᶜ², -N (C₁₋₄ alkyl) C (O) Rᶜ² and the bivalent substituent = O, while = O may only be a substituent in non-aromatic ring systems; each Rᶜ², independently of one another, indicates hydrogen or a group optionally substituted with one or more identical or different Rᵈ² and / or Rᵉ² selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋ ₆ cycloalkyl, C₄₋₆ cycloalkenyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; each Rᵈ² is independently selected from -ORᵉ², -NRᵉ²Rᵉ², halogen, -CN, -C (O) Rᵉ², -C (O) ORᵉ², -C (O) NRᵉ²Rᵉ², -S (O) ₂Rᵉ², -S (O) ₂NRᵉ²Rᵉ², -NHC (O) Rᵉ², -N (C₁₋₄ alkyl) C (O) Rᵉ² and the bivalent substituent = O, while = O may only be a substituent in non-aromatic ring systems; each Rᵉ², independently of one another, indicates hydrogen or a group selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₆ cycloalkyl, C₄₋₆ cycloalkenyl, C₆₋₁₀ aryl, heteroaryl 5 to 10 members and heterocyclyl 3 to 10 members; A is selected from 5 to 6 membered phenyl and heteroaryl if F is carbon or A is 5 to 6 membered heteroaryl containing nitrogen if F is nitrogen; each R⁴ is independently selected from Rᵃ⁴ and Rᵇ⁴; each Rᵃ⁴, independently of one another, is a group optionally substituted with one or more Rᵇ⁴ and / or Rᶜ⁴, identical or different, selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋ ₇ cycloalkyl, C₄₋₇ cycloalkenyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; each Rᵇ⁴ is independently selected from -ORᶜ⁴, -NRᶜ⁴Rᶜ⁴, halogen, -CN, -C (O) Rᶜ⁴, -C (O) ORᶜ⁴, -C (O) NRᶜ⁴Rᶜ⁴, -C (O) NRᵍ⁴ORᶜ⁴, -S (O) ₂Rᶜ⁴, -S (O) ₂NRᶜ⁴Rᶜ⁴, -NHSO₂Rᶜ⁴, -N (C₁₋₄ alkyl) SO₂Rᶜ⁴, -NHC (O) Rᶜ⁴ and -N (C₁₋₄ alkyl) C (O) Rᶜ⁴; each Rᶜ⁴, independently of one another, indicates hydrogen or a group optionally substituted with one or more Rᵈ⁴ and / or Rᵉ⁴, identical or different, selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; each Rᵈ⁴ is independently selected from -ORᵉ⁴, -NRᵉ⁴Rᵉ⁴, halogen, -CN, -C (O) Rᵉ⁴, -C (O) ORᵉ⁴, -C (O) NRᵉ⁴Rᵉ⁴, -C (O) NRᵍ⁴ORᵉ⁴, -S (O) ₂Rᵉ⁴, -S (O) ₂NRᵉ⁴Rᵉ⁴, -NHC (O) Rᵉ⁴ and -N (C₁₋₄ alkyl) C (O) Rᵉ⁴; each Rᵉ⁴, independently of one another, indicates hydrogen or a group optionally substituted with one or more Rᶠ⁴ and / or Rᵍ⁴, identical or different, selected from C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, C₆₋₁₀ aryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; each Rᶠ⁴ is independently selected from -ORᵍ⁴, -NRᵍ⁴Rᵍ⁴, halogen, -CN, -C (O) Rᵍ⁴, -C (O) ORᵍ⁴, -C (O) NRᵍ⁴Rᵍ⁴, -C (O) NRᵍ⁴ORᵍ⁴, -S (O) ₂Rᵍ⁴, -S (O) ₂NRᵍ⁴Rᵍ⁴, -NHC (O) Rᵍ⁴ and -N (C₁₋₄ alkyl) C (O) Rᵍ⁴; each Rᵍ⁴ is independently selected from hydrogen, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₃₋₇ cycloalkyl, C₄₋₇ cycloalkenyl, C₆₋₁₀ aryl, heteroaryl of 5 to 10 members and 3 to 10 membered heterocyclyl; r indicates the number 0, 1, 2 or 3; n indicates the number 1, 2 or 3; each R⁷ is independently selected from halogen, C₁₋₄ alkyl, -CN, C₁₋₄ haloalkyl, -OC₁₋₄ alkyl and -OC₁₋₄ haloalkyl; q indicates the number 0, 1, 2 or 3; W, X and Y are each independently selected from -N = and -CH = provided that the hydrogen in each -CH = can be replaced by a substituent R⁷ if present and that a maximum of two W, X and Y they can be -N =; V is oxygen or sulfur; D is nitrogen, E is carbon and F is carbon; or D is carbon, E is nitrogen and F is carbon; or D is carbon, E is carbon and F is nitrogen; or a salt of that. Claim 16: Synthetic intermediates characterized by the formula (2), wherein R², R³, R⁴, R⁷, A, V, W, X, Y, r and q are as defined in any of claims 1 to 14. |
| priorityDate | 2015-10-09-04:00^^<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: 63.