http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-094929-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/A61P27-06 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/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D217-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D231-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D231-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D407-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D241-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D231-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4155 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D317-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 |
| filingDate | 2014-02-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d982712b97db415897ba03e68dc23558 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1624fde26f145a4bea9ab518460dbecb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e65d0e1f066f7c4be625a6cca1b908db http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a7ab844cc4739314ee7ac74aa5d0bf66 |
| publicationDate | 2015-09-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-094929-A1 |
| titleOfInvention | DERIVATIVES OF PHENYLPIRAZOL AS POWERFUL INHIBITORS OF ROCK1 AND ROCK2 |
| abstract | These compounds are selective ROCK inhibitors. Also, pharmaceutical compositions comprising these compounds and methods for treating cardiovascular disorders, disorders related to smooth muscle, oncological disorders, neuropathological disorders, autoimmune disorders, fibrotic disorders and / or inflammatory disorders by use. Claim 1: A compound characterized in that it has the formula (1), or an enantiomer, diastereomer, stereoisomer, salt of that pharmaceutically acceptable, wherein R¹ is independently selected from H, F, Cl, Br, OH, CN, NRᵃRᵃ, -O-C₁₋₄ alkyl substituted with 0-3 Rᵉ and C₁₋₄ alkyl substituted with 0-3 Rᵉ; R² is independently selected from H, - (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, C₁₋₄ alkyl substituted with 0-3 Rᵉ, (CH₂) ʳ-carbocyclyl C₃₋₆ substituted with 0-3 Rᵉ and - (CH₂) ʳ-heterocyclyl substituted with 0-3 Rᵉ; R³ is independently selected from F, Cl, Br, CN, 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-carbocyclyl C₃₋₆ substituted with 0 - 3 Rᵉ and - (CH₂) ʳ-heterocyclyl substituted with 0 - 3 Rᵉ; R⁴ is independently selected from H, F, Cl, Br, OH, CN, O-C₁₋₄ alkyl substituted with 0-3 Rᵉ and C₁₋₄ alkyl substituted with 0-3 Rᵉ; R⁵ is independently selected from H and C₁₋₄ alkyl substituted with 0-3 Rᵉ; R⁶ and R⁷ are independently selected from H, CN, C₁₋₆ alkyl substituted with 0-4 Rᵉ, C₂₋₄ alkenyl 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) 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-carbocyclyl C₃₋₆ 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 both are attached, form a cycloalkyl substituted with 0-5 Rᵉ; alternatively, two adjacent R⁶ groups form a cycloalkyl substituted with 0-5 Rᵉ, where n is greater than 1; R⁸ is selected from aryl and heteroaryl, each substituted with 0-5 Rᵉ; R⁹ is independently selected from F, Cl, Br, CN, = O, C₁₋₄ alkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, 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 (ORR) ) NRᵃRᵃ, - (CHRᵈ) ʳC (= O) ORᵇ, - (CHRᵈ) ʳC (= O) Rᵇ, - (CHRᵈ) OC (= O) Rᵇ, - (CHRᵈ) ʳC (= O) NRᵃRᵃ, - (CHRᵈ ) ʳ-cycloalkyl, - (CHRᵈ) ʳ-heterocyclyl, - (CHRᵈ) ʳ-aryl and - (CHRᵈ) ʳ-heteroaryl, wherein 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, CN, 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-carbocyclyl C₃₋₁₀ 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 -Cbo -carbocyclyl substituted with 0-5 Rᵉ and - (CH₂) ʳ-heterocyclyl substituted with 0-5Rᵉ; Rᶜ, in each case, is independently selected from C₁₋₆ alkyl substituted with 0-5 Rᵉ, C₂₋₆ alkenyl substituted with 0-5 Rᵉ, C₃₋₆ alkynyl substituted with 0-5 Rᵉ; C₃₋₆ carbocyclyl and heterocyclyl; Rᵈ, in each case, is independently selected from H and C₁₋₄ alkyl substituted with 0-5 Rᵉ; Rᵉ, in each case, is independently selected from C₁₋₆ alkyl substituted with 0-5 Rᶠ, C₂₋₆ alkenyl, C₂₋₆ alkynyl, - (CH₂) ʳ -C₃₋₆ cycloalkyl, F, Cₗ, Bʳ, CN, NO₂, = O, CO₂H, - (CH₂) ʳO-C₁₋₅ alkyl, - (CH₂) ʳORᶠ, S (O) ₚRᶠ, C (= O) NRᶠRᶠ, S (O) ₚNRᶠRᶠ and - (CH₂) ʳNRᶠRᶠ; Rᶠ, in each case, is independently selected from H, C₁₋₅ alkyl, C₃₋₆ cycloalkyl and phenyl, or Rᶠ and Rᶠ, together with the nitrogen atom to which both are attached, form a heterocyclic ring optionally substituted with C₁ alkyl ₋₄; n, in each case, is independently selected from 1, 2 and 3; p, in each case, is independently selected from 0, 1 and 2; and r, in each case, is independently selected from 0, 1, 2, 3 and 4. |
| priorityDate | 2013-02-28-04:00^^<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: 70.