http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-108175-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c1698cffb4f39e393843f352b342bb5a |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D277-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-6539 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 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/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-426 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-65583 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-662 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-426 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F9-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-662 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F9-44 |
| filingDate | 2017-04-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_664101689708d0457f2416bfa1a06178 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bc04a9f124411757c22566de8d6c5152 |
| publicationDate | 2018-07-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-108175-A1 |
| titleOfInvention | TIAZOL ACETAMIDA ANTIVÍRICOS COMPOUNDS |
| abstract | To a process for their preparation and their use as medicaments, in particular as antiviral medicaments. Claim 1: A compound represented by formula (1), an enantiomer, diastereomer, tautomer, N-oxide, solvate, formulation and pharmaceutically acceptable salt thereof, wherein X is selected from the compounds of the group of formulas (2 ); R¹ is selected from H, halogen, C₁₋₆ alkyl, halo-C₁₋₆ alkyl, C₃₋₆ cycloalkyl, halo-C₃₋₆ cycloalkyl, -O-C₁₋₆ alkyl, -O-halo-C₁₋₆ alkyl, and -NH-C₁₋₆ alkyl; provided that in case X is one of the residues of the group of formulas (3), then R¹ is not hydrogen (H); R² is selected from H, -CN, -NO₂, C₁₋₁₀ alkyl, C₂₋₁₀ alkenyl, C₂₋₁₀ alkynyl, C₀₋₁₀-alkylene-C₃₋₁₀-cycloalkyl, C₀₋₁₀-alkylene-C₃₋-heterocycloalkyl, ₁₀-(5 to 10 membered heteroaryl), C₀₋₁₀ alkylene-(6 to 10 membered aryl), C₀₋₁₀ alkylene-(6 to 10 membered heteroaryl), C₀₋₁₀ alkylene-OR¹¹, C₀₋₁₀ alkylene -CO₂R¹¹, C₀₋₁₀-C(=O)NR¹¹R¹²-alkylene, C₀₋₁₀-C(=S)NR¹¹R¹²-alkylene, C₀₋₁₀-C(=O)NR¹¹SO₂R¹³-alkylene, C₀₋₹-C(R)SO₹NR¹₀-C₀₋₹-C(=S)NR¹₀-alkylene , C₀₋₁₀-C alkylene (= O) R¹¹, C₀₋₁₀-C alkylene (= S) R¹¹, C₀₋₁₀-SR¹¹ alkylene, C₀₋₁₀-SOˣR¹³ alkylene, C₀₋₁₀-SO₃R¹¹ alkylene, C₀₋₁₀ alkylene -So₂nr¹¹R¹², C₀₋₁₀-NR¹¹C alkylene (= O) R¹¹, C₀₋₁₀-NR¹¹C alkylene (= S) R¹¹, C₀₋₁₀-NR¹¹SO₂R¹³ alkylene, c₀₋₁₀-nr¹¹c alkylene (= O) nr¹¹r¹², c₀₋₁₀ alkylene -NR¹¹C(=S)NR¹¹R¹², C₀₋₁₀ alkylene-NR¹¹SO₂NR¹¹R¹², C₀₋₁₀ alkylene-NR¹¹R¹², where alkyl, alkenyl, alkynyl, alkylene, cycloalkyl, heterocycloalkyl, aryl and heteroaryl are unsubstituted or substituted with 1 to 7 entities independently selected from the group consisting of oxo, CN, -NO₂, OR¹¹, O-C₂₋₆-OR¹¹-alkylene, C₁₋₆-alkyl, halo-C₁₋₆-alkyl, halogen, CO₂R¹¹, C(=O)NR¹¹R¹², C (= O) NR¹¹SO₂R¹¹, C (= O) R¹¹, SR¹¹, SOˣR¹¹, SO₃R¹¹, P (= O) (OR¹¹ )², SO₂NR¹¹R¹², NR¹¹CO₂R¹³, NR¹¹SO₂R¹³, NR¹¹C (= O) NR¹¹R¹², NR¹¹SO₂NR¹¹R¹², C₃₋₁₀-cycloalkyl, O-C₃₋₁₀-cycloalkyl, C₃₋₁₀-heterocycloalkyl, O-C₃₋₁₀-heterocycloalkyl and NR¹¹R¹²; R³ is selected from H, C₁₋₆ alkyl, C₁₋₆ halo-alkyl, -O-C₁₋₆ alkyl, -O-C₁₋₆ halo-alkyl, C₃₋₆ cycloalkyl, and C₃₋₆ heterocycloalkyl, where alkyl, cycloalkyl and heterocycloalkyl are optionally substituted with 1 to 5 substituents independently selected from halogen, -CN, OH, oxo, C₁₋₃ alkyl, halo-C₁₋₃ alkyl, O-C₁₋₃ alkyl, O-halo-C₁₋₃ alkyl , SO₂-C₁₋₃ alkyl, CO₂H; o R² and R³, when taken together with the nitrogen to which they are attached, complete a 3 to 8 membered ring containing carbon atoms and optionally containing 1 or 2 heteroatoms selected from O, S or N, where the ring is unsubstituted or substituted with 1 to 4 substituents independently selected from the group consisting of halogen, -CN, -NO₂, OH, oxo, C₁₋₃ alkyl, halo-C₁₋₃ alkyl, O-C₁₋₃ alkyl, O- halo-C₁₋₃ alkyl, SO₂-C₁₋₃ alkyl, CO₂H; R⁴ is selected from H, C₁₋₆ alkyl, C₁₋₆ acyl, C₂₋₆ alkenyl, C₃₋₈ cycloalkyl and C₃₋₈ heterocycloalkyl, where alkyl, acyl, alkenyl, cycloalkyl and heterocycloalkyl are optionally substituted with 1 to 5 substituents independently selected from halogen, -CN, OH, oxo, C₁₋₃-alkyl, C₁₋₃-halo-alkyl, O-C₁₋₃-alkyl, O-C₁₋₃-halo-alkyl; R⁵ and R⁶ and R⁵' and R⁶' are independently selected from H, halogen, C₁₋₆-alkyl, NH₂, NH-C₁₋₆-alkyl, N(C₁₋₆-alkyl)₂, C₀₋₆-C(=O)-alkylene NH₂; or R⁵ and R⁶ and R⁵' and R⁶', independently, when taken together with the carbon to which they are attached, complete a 3 to 8 membered ring containing carbon atoms and optionally containing 1 or 2 heteroatoms selected from O, S or N, where the ring is unsubstituted or substituted with 1 to 4 substituents independently selected from the group consisting of halogen, -CN, -NO₂, OH, oxo, C₁₋₃ alkyl, halo-C₁₋₃ alkyl, O -C₁₋₃-alkyl, O-halo-C₁₋₃-alkyl, SO₂-C₁₋₃-alkyl, CO₂H; or R⁵ and R⁵' and R⁶ and R⁶', independently, when taken together with the two adjacent carbons to which they are attached, complete a 3 to 8 membered ring containing carbon atoms and optionally containing 1 or 2 selected heteroatoms from O, S, or N, where the ring is unsubstituted or substituted with 1 to 4 substituents independently selected from the group consisting of halogen, -CN, -NO₂, OH, oxo, C₁₋₃ alkyl, halo-C₁₋ alkyl ₃, O-C₁₋₃ alkyl, O-halo-C₁₋₃ alkyl, SO₂-C₁₋₃ alkyl, CO₂H; R⁷ is selected from 6-membered aryl and 5- or 6-membered heteroaryl, where aryl and heteroaryl are optionally substituted with 1 to 4 substituents independently selected from halogen, -CN, -NO₂, OH, C₁₋₆ alkyl, O -C₁₋₆-alkyl, C₃₋₆-cycloalkyl, O-C₃₋₆-cycloalkyl, C₃₋₆-heterocycloalkyl, O-C₃₋₆-heterocycloalkyl, SOʸ-C₁₋₆-alkyl, CO₂H, C(=O)O-C₁₋₆-alkyl , 6- to 10-membered aryl, 5- or 10-membered heteroaryl, O-(6- to 10-membered aryl), and O-(5- or 10-membered heteroaryl), wherein alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl are optionally substituted with 1 to 5 substituents independently selected from halogen, -CN, -NO₂, OH, R¹³, OR¹³, CO₂R¹¹, NR¹¹R¹², C(=O)R¹¹, C(=S)R¹¹, C(=O)NR¹¹R¹², NR¹¹C (=O)NR¹¹R¹², NR¹¹C(=O)OR¹³, OC(=O)NR¹¹R¹², C(=S)NR¹¹R¹², NR¹¹C(=S)NR¹¹R¹², NR¹¹C(=O)OR¹³, OC(=O)NR¹¹R¹², C( =S)NR¹¹R¹², NR¹¹C(=S)NR¹¹R¹², NR¹¹C(=S)OR¹³, OC(=S)NR¹¹R¹², SOʸ-C₁₋₆-alkyl, SOʸ-halo-C₁₋₆-alkyl, SR¹¹, SOˣ R¹³, SO₃R¹¹, SO₂NR¹¹R¹², NR¹¹SO₂R¹³, NR¹¹SO₂NR¹¹R¹²; R⁸ is selected from H, -CN, -NO₂, C₁₋₁₀ alkyl, C₂₋₁₀ alkenyl, C₂₋₁₀ alkynyl, C₀₋₁₀-alkylene-C₃₋₁₀-cycloalkyl, C₀₋₁₀-alkylene-C₁₁₋-heterocycloalkyl, ₁₀-(5 to 10 membered heteroaryl), C₀₋₁₀ alkylene-(6 to 10 membered aryl), C₀₋₁₀ alkylene-(6 to 10 membered heteroaryl), C₀₋₁₀ alkylene-OR¹¹, C₀₋₁₀ alkylene -CO₂R¹¹, C₀₋₁₀-C(=O)NR¹¹R¹²-alkylene, C₀₋₁₀-C(=S)NR¹¹R¹²-alkylene, C₀₋₁₀-C(=O)NR¹¹SO₂R¹³-alkylene, C₀₋₹-C(R)SO₹NR¹₀-C₀₋₹-C(=S)NR¹₀-alkylene , C₀₋₁₀-C(=O)R¹¹-alkylene, C₀₋₁₀-C(=S)R¹¹-alkylene, C₀₋₁₀-SR¹¹-alkylene, C₀₋₁₀-SOˣ-R¹³-alkylene, C₀₋₁₀-SO₹-R¹³-alkylene, C₀₋₁₀-SR¹¹-alkylene ₋₁₀-SO₂NR¹¹R¹², alkylene C₀₋₁₀-NR¹¹C (= O) R¹¹, C₀₋₁₀-NR¹¹C alkylene (= S) R¹¹, C₀₋₁₀-NR¹¹SO₂R¹¹ alkylene (= O) NR¹¹R¹², C₀ alkylene ₋₁₀-NR¹¹C(=S)NR¹¹R¹², alkylene C₀₋₁₀-NR¹¹-SO₂-NR¹¹R¹², alkylene C₀₋₁₀-NR¹¹R¹², where alkyl, alkenyl, alkynyl, alkylene, cycloalkyl, heterocycloalkyl, aryl and heteroaryl are synsubstituted or substituted with 1 to 7 substitutes tunts independently selected from the group consisting of oxo, CN, -NO₂, OR¹¹, O-C₂₋₆-OR¹¹-alkylene, C₁₋₆-alkyl, halo-C₁₋₆-alkyl, halogen, CO₂R¹¹, CONR¹¹R¹², CONR¹¹SO₂R¹¹, COR¹¹, COR¹¹ , So₃H, PO (OH) ₂, SO₂NR¹¹R¹², NR¹¹COR¹¹, NR¹¹SO₂R¹¹,, NR¹¹R¹², C₃₋₁₀ C₃₋₁₀, O-cycloalkyl c₃₋₁₀, heterocycloalkyl c₃₋₁₀, o-heterocycloalkyl C₃₋₁₀ and NR¹¹R¹² ; R⁹ is selected from C₁₋₁₀ alkyl, C₋₁₀₋₁₀ alkyl, C₋₁₀₋₁₀ alkynyl, C₀₋₁₀ C₀₋₁₀-cycloalkyl alkylene, C₀₋₁₀-heterocycloalkyl alkylene, C₀₋₁₀- alkylene (5 to 10 heteroaryl membered), C₀₋₁₀-alkylene-(6- to 10-membered aryl), C₀₋₁₀-alkylene-(6- to 10-membered heteroaryl), C₀₋₁₀-OR¹¹ alkylene, C₀₋₁₀-CO₂R¹¹ alkylene, C₀₁₀- C(=O)NR¹¹R¹², C₀₋₁₀-C(=S)NR¹¹R¹² alkylene, C₀₋₁₀-C(=O)NR¹¹SO₂R¹³ alkylene, C₀₋₁₀-C(=S)NR¹¹SO₂R¹-C₀ alkylene, = O) R¹¹, C₀₋₁₀-C alkylene (= S) R¹¹, C₀₋₁₀-SR¹¹ alkylene, C₀₋₁₀-SOˣR¹³ alkylene, alkylene C₀₋₁₀-SO₃R¹¹, alkylene C₀₋₁₀-SO₂NR¹¹R¹², alkylene c₀₋₁₀- NR¹¹C (= O) R¹¹, alkylene C₀₋₁₀-NR¹¹C (= S) R¹¹, alkylene C₀₋₁₀-NR¹¹SO₂R¹³, alkylene C₀₋₁₀-NR¹¹C (= O) NR¹¹R¹², C₀₋₁₀-NR¹¹C alkylene (= S) NR¹¹R¹², C₀₋₁₀-NR¹¹SO₂NR¹¹R¹² alkylene, C₀₋₁₀-NR¹¹R¹² alkylene, wherein alkyl, alkenyl, alkynyl, alkylene, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl are unsubstituted or substituted with 1 to 7 select substituents. independently from the group consisting of oxo, CN, -NO₂, OR¹¹, O-C₂₋₆-OR¹¹-alkylene, C₁₋₆-alkyl, halo-C₁₋₆-alkyl, halogen, CO₂R¹¹, C(=O)NR¹¹R¹², C (= O) NR¹¹so₂R¹¹, C (= O) R¹¹, SR¹¹, SOˣR¹¹, SO₃R¹¹, P (= O) (OR¹¹) ₂, SO₂NR¹¹R¹², NR¹¹C (= O) R¹¹, NR¹¹SO₂R¹³, NR¹¹C (= O) NR¹¹R¹²², NR¹¹SO₂NR¹¹R¹², Cycloalkyl C₃₋₁₀, O-C₃₋₁₀-cycloalkyl, C₃₋₁₀-heterocycloalkyl, O-C₃₋₁₀-heterocycloalkyl and NR¹¹R¹²; R¹⁰ is selected from -CN, OH, and -NO₂; R¹¹ is independently selected from H, C₁₋₆ alkyl, C₀₋₆ alkylene-C₃₋₁₀ cycloalkyl, and C₀₋₆ alkylene-C₃₋₁₀ heterocycloalkyl, where alkyl, alkylene, cycloalkyl, and heterocycloalkyl are unsubstituted or substituted with 1 to 6 substituents independently selected from the group consisting of halogen, -CN, OH, oxo, C₁₋₃ alkyl, halo-C₁₋₃ alkyl, O-C₁₋₃ alkyl, O-halo-C₁₋₃ alkyl, NH₂, NH( C₁₋₃-alkyl), N(C₁₋₃-alkyl)₂, C₃₋₆-heterocycloalkyl, C₃₋₆-cycloalkyl, SO₂-NH-C₁₋₃-alkyl, SO₂-N(C₁₋₃-alkyl)₂, and SO₂-C₁₋-alkyl ₃, where cycloalkyl and heterocycloalkyl are unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of F, OH, oxo, CH₃, CHF₂, and CF₃; R¹² is independently selected from H, C₁₋₆ alkyl, C₁₋₆ halo-alkyl, and C₃₋₆ cycloalkyl; or R¹¹ and R¹², when taken together with the nitrogen to which they are attached, complete a 3 to 8 membered ring containing carbon atoms and optionally containing 1 or 2 heteroatoms selected from O, S or N, where the ring is unsubstituted or substituted with 1 to 4 substituents independently selected from the group consisting of halogen, -CN, -NO₂, OH, oxo, C₁₋₃ alkyl, halo-C₁₋₃ alkyl, O-C₁₋₃ alkyl, O- halo-C₁₋₃ alkyl, SO₂-C₁₋₃ alkyl, CO₂H; R¹³ is independently selected from C₁₋₆ alkyl, C₀₋₆ alkylene-C₃₋₁₀ cycloalkyl, and C₀₋₆ alkylene-C₃₋₁₀ heterocycloalkyl, where alkyl, alkylene, cycloalkyl, and heterocycloalkyl are unsubstituted or substituted with 1 to 6 selected substituents independently from the group consisting of halogen, -CN, OH, oxo, C₁₋₃-alkyl, halo-C₁₋₃-alkyl, O-C₁₋₃-alkyl, O-halo-C₁₋₃-alkyl, NH₂, NH(C₁-alkyl ₋₃,), N(C₁₋₃ alkyl)₂, C₃₋₆ heterocycloalkyl, C₃₋₆ cycloalkyl, SO₂-NH-C₁₋₃ alkyl, SO₂-N(C₁₋₃ alkyl)₂ and SO₂-C₁₋₃ alkyl , wherein cycloalkyl and heterocycloalkyl are unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of F, OH, oxo, CH₃, CHF₂, and CF₃; n is selected between 0 and 1; x is independently selected from 1 and 2; y is independently selected from 0, 1 and 2; and where R¹ is optionally connected to a residue selected from R², R³, R⁸, R⁹, R¹⁰ or R¹² to form a 5 to 8 membered heterocycle, which is optionally substituted with 1 to 4 substituents independently selected from the group consisting of halogen , -CN, -NO₂, OH, oxo, C₁₋₃-alkyl, C₁₋₃-halo-alkyl, O-C₁₋₃-alkyl, O-C₁₋₃-halo-alkyl, SO₂-C₁₋₃-alkyl, CO₂H. |
| priorityDate | 2016-04-06-04:00^^<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: 45.