http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-113947-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_9008466a40998f8be8e54cd3aceb10a2 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-0078 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-0075 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-541 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 |
| filingDate | 2018-12-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0e852e77a5d13c2c86afa419ff76e57d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_476f3208b271a3eefa83cfd1ab098ec2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0d2eb3616a4260b3cd3ca4a573481539 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_376a0fef23a58668bbdab424496c314a |
| publicationDate | 2020-07-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-113947-A1 |
| titleOfInvention | DERIVATIVES OF AZAINDOL AS RHO-KINASE INHIBITORS |
| abstract | Rho-kinase inhibitor compounds of formula (1), which are derived from tyrosine analogues, processes for preparing said compounds, pharmaceutical compositions containing them and the therapeutic use of the same. Such compounds may be useful in the treatment of numerous disorders associated with ROCK enzyme-related mechanisms, such as lung diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF), and pulmonary arterial hypertension (PAH). . Claim 1: A compound characterized in that it is of formula (1) where: X¹ is a carbon or nitrogen atom; p is zero or an integer between 1 and 3; each R, when present, is H or halogen; R¹ is -H, -CN, or C₁₋₆ alkyl; B is C₃₋₈ heterocycloalkyl, or B is a group of formula R²R³N-C₁₋₆ alkyl, optionally substituted with one or more substituents selected from hydroxyl, C₁₋₆ alkyl, C₁₋₆ hydroxyalkyl, C₁₋₆ alkoxycarbonyl, C₃₋₁₀ cycloalkoxycarbonyl, aryl-C₁₋₆ alkoxycarbonyl; where R² and R³, the same or different, are selected from the group consisting of -H, C₁₋₆ alkyl, C₁₋₆ hydroxyalkyl, C₃₋₈ heterocycloalkyl, further optionally substituted with one or more C₁₋₆ alkyl; or B is a group of formula R²R³N-C₁₋₆ alkyl, optionally substituted with one or more substituents selected from hydroxyl, C₁₋₆ alkyl, C₁₋₆ hydroxyalkyl, C₁₋₆ alkoxycarbonyl, C₃₋₁₀ cycloalkoxycarbonyl, aryl-C₁₋₆ alkoxycarbonyl; where R² and R³, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring, preferably a 4- to 6-membered saturated monocyclic heterocyclic ring, where at least one additional ring carbon atom is optionally replaced by al less one additional group independently selected from N, NH, S or O and / or may have a substituent group -oxo (= O), wherein said heterocyclic ring further optionally includes spiro distribution; and said heterocyclic ring in turn is further optionally substituted with one or more substituents selected from hydroxyl, C₁₋₆ alkyl, C₁₋₆ hydroxyalkyl, C₁₋₆ alkoxycarbonyl, C₃₋₁₀ cycloalkoxycarbonyl, aryl-C₁₋₆ alkoxycarbonyl; or B is a group of formula R²R³N-C₁₋₆ alkyl, optionally substituted with one or more substituents selected from hydroxyl, C₁₋₆ alkyl, C₁₋₆ hydroxyalkyl, C₁₋₆ alkoxycarbonyl, C₃₋₁₀ cycloalkoxycarbonyl, aryl-C₁₋₆ alkoxycarbonyl; where R³ is selected from the group consisting of -H, C₁₋₆ alkyl, C₁₋₆ hydroxyalkyl, C₃₋₈ heterocycloalkyl, further optionally substituted with one or more C₁₋₆ alkyl; R² is a divalent group - (CH₂) q-, where q is an integer between 1 and 3; wherein said divalent group is connected to the ortho carbon atom of the adjacent phenyl ring to form a heterocyclic ring, preferably a 4- to 10-membered heterocyclic ring fused to the phenyl ring; wherein said heterocyclic ring in turn is further optionally substituted with one or more groups selected from C₁₋₆ alkyl, C₁₋₆ hydroxyalkyl; or B is a divalent group - (CH₂) ₛ-, where s is an integer between 2 and 8, where said divalent group is connected to the adjacent carbon ortho to the phenyl ring to form a fused ring; preferably a 4- to 10-membered monocyclic ring fused to the phenyl ring; wherein said ring is further substituted with one or more -NH₂; and their pharmaceutically acceptable salts and solvates. |
| priorityDate | 2017-12-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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