http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-113965-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42e94091a4fc81b8d0237117707cc7ee |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 |
| 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/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4192 |
| filingDate | 2018-12-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f5fc60542d2c480a923e401fc3881725 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a28e4230fa1667a4b6c44fb85af3f8aa http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5f985ec0008e7f70eb58359e7fbb23d0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c801cc2003c37f445802e07788db7747 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f4ee67145e738aea5694aa6c8529f312 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3eb950f5b4529a233c95b938d25e6bb4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_17aeb8a3e4760049350fa8cf7c93d2b9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d897af154e921f7f101261dcd61e61ab http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0ac4ea15456903dde6d8fee700abf6f8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4e0420a3d3eb67058df2522fad505598 |
| publicationDate | 2020-07-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-113965-A1 |
| titleOfInvention | TRIAZOLE AZOLES CYCLOHEXYL ACIDS AS ANTAGONISTS OF LPA |
| abstract | Compounds of formula (1), or a pharmaceutically acceptable stereoisomer, tautomer or solvate or salt thereof, wherein all variables are as defined herein. These compounds are selective inhibitors of the LPA receptor. Claim 1: A compound characterized by the formula (1), or a stereoisomer, a tautomer, a solvate or a salt of those acceptable from the pharmaceutical point of view, wherein X¹, X², X³ and X⁴ are each independently, CR⁵ or N; provided that no more than two of X¹, X², X³ or X⁴ are N; one of Q¹, Q² and Q³ is NR⁶, and the other two are N; and the dashed circle indicates optional bonds that form an aromatic ring; L is a covalent bond or C₁₋₄ alkylene substituted with 0 to 4 R⁷; Z is CHR⁸ᵃ, NR⁸ᵇ, or O; ring Y is a 5-membered heteroaryl or 5-membered heterocyclyl, each independently containing a nitrogen atom and at least one additional heteroatom selected from nitrogen, oxygen and sulfur; R¹ is (-CH₂) ₐR⁹; a is an integer of 0 or 1; R² is each independently halo, cyano, hydroxyl, amino, C₁₋₆ alkyl, C₃₋₆ cycloalkyl, 4- to 6-membered heterocyclyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, alkoxyalkyl, haloalkoxyalkyl or haloalkoxy; n is an integer of 0, 1, or 2; R³ is halo, cyano, hydroxyl, amino, oxo, -ORᵃ, -SRᵃ, = S, -NRᶜRᶜ, = NH, = N-OH, = NRᵃ, = N-ORᵃ, -NO₂, -S (O) ₂Rᵃ, -S (O) ₂NHRᵇ, -S (O) ₂NRᶜRᶜ, -S (O) ₂ORᵇ, -OS (O) ₂Rᵇ, -OS (O) ₂ORᵇ, -P (O) (ORᵇ) (ORᵇ), -C ( O) Rᵇ, C (NRᵇ) Rᵇ, -C (O) ORᵇ, -C (O) NRᶜRᶜ, -C (NRᵇ) NRᶜRᶜ, -OC (O) Rᵇ, -NRᵇC (O) Rᵇ, -OC (O) ORᵇ, -NRᵇC (O) ORᵇ, -OC (O) NRᶜRᶜ, -NRᵇC (O) NRᶜRᶜ, -NRᵇC (NRᵇ) Rᵇ, -NRᵇC (NRᵇ) NRᶜRᶜ, C₁₋₆ alkyl, C₁₋₆ deuterated alkyl (deuterated from partially or fully), C₂₋₆ alkenyl, C₁₋₆ haloalkyl, C₁₋₆ heteroalkyl, 6 to 10 membered aryl, arylalkyl, 5 to 10 membered heteroaryl, heteroarylalkyl, 3 to 8 membered carbocyclyl substituted with 0 to 1 = CH₂, carbocyclylalkyl, 4- to 8-membered heterocyclyl, or heterocyclylalkyl; wherein alkyl, heteroalkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl and Rᵃ, by themselves or as part of another group, are each independently substituted with 0 to 5 Rᵈ; Rᵃ is selected from C₁₋₆ alkyl, C₁₋₆ deuterated alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, carbocyclyl, carbocyclylalkyl, heterocyclyl, and heterocyclylalkyl; Rᵇ is, each independently, hydrogen or Rᵃ; Rᶜ is, each independently, Rᵇ; or, alternatively, two Rᶜ, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclyl; Rᵈ is each independently selected from Rᵃ, alkoxy, haloalkoxy, alkylamino, cycloalkylamino, heterocyclylamino, haloalkyl, hydroxyalkyl, aminoalkyl, cycloalkoxy, heterocyclyloxy, haloalkoxy, alkoxyalkoxy, haloalkylamino, alkoxyalkylamino, haloalkoxyalkylamino, arkylaminoalkylamino, haloalkoxyalkylamino, arkylaminoalkylamino, haloalkoxyalkylamino, arkylaminoralkylamino, haloalkoxyalkylamino, arkylaminoalkyl, , heteroarylalkyloxy, alkylthio, halo, cyano, hydroxyl, amino, oxo, -ORᵃ, -SRᵃ, = S, -NRᶜRᶜ, = NH, = N-OH, = NRᵃ, = N-ORᵃ, -NO₂, -S (O ) ₂Rᵃ, -S (O) ₂NHRᵇ, -S (O) ₂NRᶜRᶜ, -S (O) ₂ORᵇ, -OS (O) ₂Rᵇ, -OS (O) ₂ORᵇ, -P (O) (ORᵇ) (ORᵇ), -C (O) Rᵇ, -C (NRᵇ) Rᵇ, -C (O) ORᵇ, -C (O) NRᶜRᶜ, -C (NRᵇ) NRᶜRᶜ, -OC (O) Rᵇ, -NRᵇC (O) Rᵇ, - OC (O) ORᵇ, -NRᵇC (O) ORᵇ, -NRᵇC (O) NRᶜRᶜ, -NRᵇC (NRᵇ) Rᵇ and -NRᵇC (NRᵇ) NRᶜRᶜ; or, alternatively, one or two Rᵈ in alkyl, heteroalkyl, aryl, heteroaryl, carbocyclyl or heterocyclyl, together with the atoms to which they are attached, form a bridging or cyclic moiety; R⁴ is, each independently, halo, hydroxyl, amino, cyano, -C (O) NH₂, -C (O) NR¹²ᵃR¹²ᵇ, C (O) OR¹²ᵃ, C₁₋₄ alkyl, C₁₋₄ haloalkyl, C₂₋₆ alkoxyalkyl, C₁₋₄ alkoxy, oxo (= O) or imino (= NH); or, alternatively, R³ and R⁴, together with the atoms to which they are attached, form a carbocyclyl or heterocyclyl moiety; m is an integer of 0, 1, or 2; R⁵ is hydrogen, halo, cyano, hydroxyl, amino, C₁₋₆ alkyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy or haloalkoxy; R⁶ is hydrogen, C₁₋₆ alkyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy; R⁷ is halo, oxo, cyano, hydroxyl, amino, C₁₋₆ alkyl, C₃₋₆ cycloalkyl, 4- to 6-membered heterocyclyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy or haloalkoxy; R⁸ᵃ is hydrogen, halo, cyano, or C₁₋₄ alkyl; R⁸ᵇ is hydrogen or C₁₋₄ alkyl; R⁹ is selected from -CN, -C (O) OR¹⁰, -C (O) NR¹¹ᵃR¹¹ᵇ, or a moiety selected from the group of formulas (2); Rᵉ is C₁₋₆ alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, or haloalkoxyalkyl; R¹⁰ is hydrogen or C₁₋₁₀ alkyl; R¹¹ᵃ and R¹¹ᵇ are each independently hydrogen, C₁₋₆ alkyl, C₃₋₆ cycloalkyl, 4- to 6-membered heterocyclyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy; R¹²ᵃ is C₁₋₄ alkyl; and R¹²ᵇ is hydrogen or C₁₋₄ alkyl. |
| priorityDate | 2017-12-19-04:00^^<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: 48.