http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-096788-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/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-048 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-052 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-06 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/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-18 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-052 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-048 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-343 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-436 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-352 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 |
| filingDate | 2014-07-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1b0ded2f394d2e436849b4c5a9254931 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d982712b97db415897ba03e68dc23558 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e65d0e1f066f7c4be625a6cca1b908db http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1624fde26f145a4bea9ab518460dbecb |
| publicationDate | 2016-02-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-096788-A1 |
| titleOfInvention | TRICYCLIC CARBOXAMIDE COMPOUNDS AS POWERFUL ROCK INHIBITORS |
| abstract | Claim 1: A compound characterized by the formula (1), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof, wherein: A¹, A² are CR¹; A³ is independently selected from N and CR¹; B is independently selected from -O-, -CR³R⁴O-, -OCR³R⁴-, -NRᵃ-, -C (O) O-, -OC (O) -, -C (O) NRᵃ-, -NRᵃC (O) - and -S-; L is independently selected from - (CR⁶R⁷) q, - (CR⁶R⁷) ₛNR⁵ (CR⁶R⁷) q-, - (CR⁶R⁷) ₛO (CR⁶R⁷) q- and - (CR⁶R⁷) ₛC (O) (CR⁶R⁷) q-; R¹ is independently selected from H, F, Cl, Br, CN, NRᵃRᵃ, -OC₁₋₄ alkyl substituted with 0-3 Rᵉ, C₁₋₄ alkyl substituted with 0-3 Rᵉ, - (CH₂) ʳORᵇ, (CH₂) ʳS (O) ₚRᶜ, - (CH₂) ʳC (= O) Rᵇ, - (CH₂) ʳNRᵃRᵃ, - (CH₂) ʳC (= O) NRᵃRᵃ, - (CH₂) ʳC (= O) (CH₂) ʳNRᵃRᵃ, (CH₂) ʳCN, - (CH₂) ʳNRᵃC (= O) Rᵇ, - (CH₂) ʳNRᵃC (= O) ORᵇ, - (CH₂) ʳOC (= O) NRᵃRᵃ, - (CH₂) ʳNRᵃC (= O) NRᵃRᵃ, - (CH₂) ʳC (= O) ORᵇ, - (CH₂) ʳS (O) ₚNRᵃRᵃ, - (CH₂) ʳNRᵃS (O) ₚNRᵃRᵃ, - (CH₂) ʳNRᵃS (O) ₚRᶜ, (CH₂) ʳ-C₃₋₆ carbocyclyl substituted with 0 - 3 Rᵉ and - (CH₂) ʳ-heterocyclyl substituted with 0-3 Rᵉ; R², is independently selected from H, F, Cl, Br, CN, NRᵃRᵃ, -OC₁₋₄ alkyl substituted with 0-3 Rᵉ, C₁₋₄ alkyl substituted with 0-3 Rᵉ, - (CH₂) ʳORᵇ; R³ and R⁴ are independently selected from H, F, OH, CN, NRᵃRᵃ, C₁₋₄ alkyl substituted with 0-3 Rᵉ, C₁₋₄ alkenyl substituted with 0-3 Rᵉ, and C₁₋₄ alkynyl substituted with 0-3 Rᵉ , - (CH₂) ʳORᵇ, (CH₂) ʳS (O) ₚRᶜ, - (CH₂) ʳC (= O) Rᵇ, - (CH₂) ʳNRᵃRᵃ, - (CH₂) ʳC (= O) NRᵃRᵃ, - (CH₂) ʳC ( = O) (CH₂) ʳNRᵃRᵃ, (CH₂) ʳCN, - (CH₂) ʳNRᵃC (= O) Rᵇ, - (CH₂) ʳNRᵃC (= O) ORᵇ, - (CH₂) ʳOC (= O) NRᵃRᵃ, - (CH₂) ʳNRᵃC (= O) NRᵃRᵃ, - (CH₂) ʳC (= O) ORᵇ, - (CH₂) ʳS (O) ₚNRᵃRᵃ, - (CH₂) ʳNRᵃS (O) ₚNRᵃRᵃ, - (CH₂) ʳNRᵃS (O) ₚRᶜ, (CH₂ ) ʳ-C₃₋₆ carbocyclyl substituted with 0-3 Rᵉ, and - (CH₂) ʳ-heterocyclyl substituted with 0-3 Rᵉ; and - (CH₂) ʳ-heterocyclyl substituted with 0-3 Rᵉ; R⁵ is independently selected from H and C₁₋₄ alkyl optionally substituted with F, Cl, Br, CN, -ORᵇ, -S (O) ₚRᶜ, -C (= O) Rᵇ, -NRᵃRᵃ, -C (= O) NRᵃRᵃ , -C (= O) (CH₂) ʳNRᵃRᵃ, CN, -NRᵃC (= O) Rᵇ, -NRᵃC (= O) ORᵇ, -OC (= O) NRᵃRᵃ, -NRᵃC (= O) NRᵃRᵃ, -C (= O) ORᵇ, -S (O) ₚNRᵃRᵃ, -NRᵃS (O) ₚNRᵃRᵃ, and -NRᵃS (O) ₚRᶜ, - (CH₂) ʳ-C₃₋₁₀carbocyclyl substituted with 0 - 5 Rᵉ, and - (CH₂) ʳ-heterocyclyl substituted with 0-5 Rᵉ; R⁶ and R⁷ are independently selected from H, C₁₋₄ alkyl substituted with 0-4 Rᵉ, - (CH₂) ʳORᵇ, - (CH₂) ʳS (O) ₚRᶜ, - (CH₂) ʳC (= O) Rᵇ, - (CH₂ ) ʳNRᵃRᵃ, - (CH₂) ʳC (= O) (CH₂) ʳNRᵃRᵃ, - (CH₂) ʳNRᵃC (= O) Rᵇ, - (CH₂) ʳNRᵃC (= O) ORᵇ, - (CH₂) ʳOC (= O) NRᵃRᵃ, - (CH₂) ʳNRᵃC (= O) NRᵃRᵃ, - (CH₂) ʳC (= O) ORᵇ, - (CH₂) ʳS (O) ₚNRᵃRᵃ - (CH₂) ʳNRᵃS (O) ₚNRᵃRᵃ, - (CH₂) ʳNRᵃS (O) ₚRᶜ , (CH₂) ʳ-C₃₋₆ carbocyclyl substituted with 0-3 Rᵉ and - (CH₂) ʳ-heterocyclyl substituted with 0-3 Rᵉ; alternatively, R⁶ and R⁷, together with the carbon atom to which they are attached, form a cycloalkyl or heterocyclyl, each substituted with 0-5 Rᵉ; alternatively, when q is 2 or 3, two adjacent groups R⁶ form a cycloalkyl or heterocyclyl, each substituted with 0-5 Rᵉ; R⁸ is selected from C₃₋₁₀ carbocyclyl and heterocyclyl, each substituted with 0-5 Rᵉ; R⁹ is independently selected from F, Cl, Br, C₁₋₄ alkyl substituted with 0-5 Rᵉ, C₂₋₄ alkenyl substituted with 0-5 Rᵉ, C₂₋₄ alkynyl substituted with 0-5 Rᵉ, = O, nitro, - (CHRᵈ) ʳS (O) ₚRᶜ, - (CHRᵈ) ʳS (O) ₚNRᵃRᵃ, - (CHRᵈ) ʳNRᵃS (O) ₚRᶜ, - (CHRᵈ) ʳORᵇ, - (CHRᵈ) ʳCN, - (CHRᵈ) ʳNRᵃRᵃ, - (CHRᵈ ) ʳNRᵃC (= O) Rᵇ, - (CHRᵈ) ʳNRᵃC (= O) NRᵃRᵃ, - (CHRᵈ) ʳC (= O) ORᵇ, - (CHRᵈ) ʳC (= O) Rᵇ, - (CHRᵈ) ʳOC (= O) Rᵇ, - (CHRᵈ) ʳC (= O) NRᵃRᵃ, - (CHRᵈ) ʳ-cycloalkyl, - (CHRᵈ) ʳ-heterocyclyl, - (CHRᵈ) ʳ-aryl and - (CHRᵈ) ʳ-heteroaryl, where the alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl are substituted with 0-4 Rᵉ; alternatively, two adjacent R⁹ groups combine to form a carbocyclic or heterocyclic ring comprising carbon atoms and 1-3 heteroatoms selected from N, O and S (O) ₚ, wherein the carbocyclic and heterocyclic rings are substituted with 0-4 Rᵉ; Rᵃ, in each case, is independently selected from H, C₁₋₆ alkyl substituted with 0-5 Rᵉ, C₂₋₆ alkenyl substituted with 0-5 Rᵉ, C₂₋₆ alkynyl substituted with 0-5 Rᵉ, - (CH₂) ʳ -C₃₋₁₀ carbocyclyl substituted with 0-5 Rᵉ and - (CH₂) ʳ-heterocyclyl substituted with 0-5 Rᵉ; or Rᵃ and Rᵃ, together with the nitrogen atom to which both are attached, form a heterocyclic ring substituted with 0-5 Rᵉ; Rᵇ, in each case, is independently selected from H, C₁₋₆ alkyl substituted with 0-5 Rᵉ, C₂₋₆ alkenyl substituted with 0-5 Rᵉ, C₂₋₆ alkynyl substituted with 0-5 Rᵉ, - (CH₂) ʳ -C₃₋₁₀ carbocyclyl substituted with 0-5 Rᵉ and - (CH₂) ʳ-heterocyclyl substituted with 0-5 Rᵉ; Rᶜ, in each case, C₁₋₆ alkyl substituted with 0-5 Rᵉ, C₂₋₆ alkenyl substituted with 0-5 Rᵉ, C₂₋₆ alkynyl substituted with 0-5 Rᵉ, C₃₋₆ carbocyclyl and heterocyclyl is independently selected; Rᵈ, in each case, is independently selected from H and C₁₋₆ alkyl substituted with 0-5 Rᵉ; Rᵉ, in each case, C₁₋₆ alkyl is selected independently (optionally substituted with F, Cl, and Br, OH), C₂₋₆ alkenyl, C₂₋₆ alkynyl, - (CH₂) ʳ-C₃₋₁₀ carbocyclyl, - ( CH₂) ʳ-heterocyclyl, F, Cl, Br, CN, NO₂, = O, CO₂H, CO₂C₁₋₆ alkyl, - (CH₂) ʳOC₁₋₅ alkyl, - (CH₂) ʳOH, - (CH₂) ʳNRᶠRᶠ, - (CH₂ ) ʳNRᶠRᶠC (= O) C₁₋₄ alkyl, -C (= O) NRᶠRᶠ, -C (= O) Rᶠ, S (O) ₚNRᶠRᶠ, -NRᶠRᶠS (O) ₚC₁₋₄ alkyl and S (O) ₚC₁₋₄ I rent; Rᶠ, in each case, is independently selected from H, F, Cl, Br, C₁₋₅ alkyl, C₃₋₆ cycloalkyl; or Rᶠ and Rᶠ, together with the nitrogen atom to which they are attached, form a heterocyclic ring; p, in each case, is independently selected from 0, 1 and 2; q, in each case, is independently selected from 0, 1, 2 and 3; r, in each case, is independently selected from 0, 1, 2, 3 and 4; s, in each case, is independently selected from 1 and 2; provided that s and q are in the same term, s + q £ 3. |
| priorityDate | 2013-07-02-04:00^^<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: 50.