http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-089207-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_96ec3985e3ce9b24614fb87bf51a4f12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f52c68e4149a6c462b850d4e7cc2b2f9 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-53 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5355 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-541 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-53 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
| filingDate | 2012-12-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c19a51031f4b047d29f52ee53a69f5b8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8a4f5a9b0889e099985574ff756cbe65 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0fbccbb9b44f7361dab649f5ea329fd9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_49714099b0904090d4aed5bbee95d9f6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c380ad2947ad117da53e087521786905 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3f30973191c4520808ec7aa077508ad9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_090a186c0c2f394c7ba41555c9bbad1e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_75115899f69221f04330c0303f6849eb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_537b3e2a9d67b8fc93ec4fbcf2ef8dd5 |
| publicationDate | 2014-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-089207-A1 |
| titleOfInvention | BENZOTIENILO-PIRROLOTRIAZINAS DISUSTITUIDAS AND ITS USES |
| abstract | They have inhibitory activities of the protein tyrosine kinase, to methods of preparing these compounds, to pharmaceutical compositions containing these compounds, and to the use of these compounds and compositions to treat proliferative disorders, in particular cancer and tumor diseases. Claim 1: A compound of formula (1) wherein R¹ is hydrogen, chlorine, methyl or methoxy, R² is hydrogen or methoxy, provided that at least one of R¹ and R² is different from hydrogen; G¹ represents chlorine, C₁₋₄ alkyl, C₁₋₄ alkoxycarbonyl, 5-membered aza-heteroaryl, or the group -CH₂-OR³, -CH₂-NR⁴R⁵ or -C (= O) -NR⁴R⁶, in which R³ is hydrogen, C₁₋₄ alkyl or C₃₋₆ cycloalkyl or phenyl, (i) said C₁₋₄ alkyl is optionally substituted with hydroxy, C₁₋₄ alkoxy, hydroxycarbonyl, C₁₋₄ alkoxycarbonyl, amino, aminocarbonyl, monoC₁₋₄-aminocarbonyl alkyl , di-C₁₋₄-aminocarbonyl, C ciclo cycloalkyl or up to three fluorine atom, and (ii) said C₃₋₆ cycloalkyl is optionally substituted with one or two substituents independently selected from the group consisting of C₁₋₄ alkyl, hydroxy and amino, and (iii) said phenyl is optionally substituted with one or two substituents independently selected from the group consisting of fluorine, chlorine, bromine, cyano, trifluoromethyl, trifluoromethoxy, C₁₋₄ alkyl and C₁₋₄ alkoxy; R⁴ is hydrogen or C₁₋₄ alkyl; R⁵ is hydrogen, C₁₋₄ alkyl, C₁₋₄ alkylcarbonyl, C₃₋₆ cycloalkyl or 4-6 membered heterocycloalkyl, wherein (i) said C₁₋₄ alkyl is optionally substituted with hydroxy, C₁₋₄ alkoxy, hydroxycarbonyl, C₁₋₄ alkoxycarbonyl, aminocarbonyl, mono-C₁₋₄-aminocarbonyl alkyl, di-C₁₋₄-aminocarbonyl alkyl, or C₃₋₆ cycloalkyl, and (ii) said C₃₋₆ cycloalkyl is optionally substituted with one or two independently selected substituents from the group consisting of C₁₋₄ alkyl, hydroxy and amino, and (iii) said 4- to 6-membered heterocycloalkyl is optionally substituted with one or two substituents independently selected from the group consisting of C₁₋₄ alkyl, hydroxy, oxo and amino ; R⁶ is hydrogen, C₁₋₄ alkyl, C₃₋₆ cycloalkyl or 4-6 membered heterocycloalkyl, wherein (i) said C₁₋₄ alkyl is optionally substituted with hydroxy, C₁₋₄ alkoxy, hydroxycarbonyl, C₁₋₄ alkoxycarbonyl, amino, aminocarbonyl, mono-C₁₋₄-aminocarbonyl alkyl, di-C₁₋₄-aminocarbonyl, or C₃₋₆ cycloalkyl, and (ii) said C₃₋₆ cycloalkyl is optionally substituted with one or two substituents independently selected from the group which consists of C₁₋₄ alkyl, hydroxy and amino, and (iii) said 4- to 6-membered heterocycloalkyl is optionally substituted with one or two substituents independently selected from the group consisting of C₁₋₄ alkyl, hydroxy, oxo and amino, or R⁴ and R⁵, or R⁴ and R⁶, respectively, bind and, taken together with the nitrogen atom to which they are attached, form a monocyclic, saturated 4- to 7-membered heterocycloalkyl ring which may contain ner a second ring heteroatom selected from N (R⁷) and O, and which may be substituted on the ring carbon atoms with one or two substituents independently selected from the group consisting of C₁₋₄ alkyl, oxo, hydroxy, amino and aminocarbonyl, and wherein R⁷ is hydrogen, C₁₋₄ alkyl, formyl or C₁₋₄ alkylcarbonyl, and G² represents chloro, cyano, C₁₋₄ alkyl, or the group -CR⁸AR⁸BOH, -CH₂-NR⁹R¹⁰, -C (= O) -NR¹¹R¹² or -CH₂-OR¹⁵, wherein R⁸A and R⁸B are independently selected from the group consisting of hydrogen, C₁₋₄ alkyl, cyclopropyl and cyclobutyl; R⁹ is hydrogen or C₁₋₄ alkyl; R¹⁰ is hydrogen, C₁₋₄ alkyl, C₁₋₄ alkylcarbonyl, C₃₋₆ cycloalkyl or 4-6 membered heterocycloalkyl, in which (i) said C₁₋₄ alkyl is optionally substituted with hydroxy, amino, aminocarbonyl, mono-alkyl C₁₋₄-aminocarbonyl, or di-C₁₋₄-aminocarbonyl alkyl, and (ii) said C₃₋₆ cycloalkyl is optionally substituted with one or two substituents independently selected from the group consisting of C₁₋₄ alkyl, hydroxy and amino, and (iii) said 4- to 6-membered heterocycloalkyl is optionally substituted with one or two substituents independently selected from the group consisting of C₁₋₄ alkyl, hydroxy, oxo and amino; R¹¹ is hydrogen or C₁₋₄ alkyl; R¹² is hydrogen, C₁₋₄ alkyl, C₃₋₆ cycloalkyl or 4-6 membered heterocycloalkyl, wherein (i) said C₁₋₄ alkyl is optionally substituted with hydroxy, amino, aminocarbonyl, mono-C₁₋₄-aminocarbonyl alkyl , or di-C₁₋₄-aminocarbonyl alkyl, and (ii) said C₃₋₆ cycloalkyl is optionally substituted with one or two substituents independently selected from the group consisting of C₁₋₄ alkyl, hydroxy and amino, and (iii) said heterocycloalkyl 4 to 6 members is optionally substituted with one or two substituents independently selected from the group consisting of C₁₋₄ alkyl, hydroxy, oxo and amino, or R⁹ and R¹⁰, or R¹¹ and R¹², respectively, are joined and, taken together with the nitrogen atom to which they are attached, form a monocyclic, saturated 4- to 7-membered heterocycloalkyl ring which may contain a second ring heteroatom selected from N (R (³), O, S and S (O) ₂, and the which may be substituted on the ring carbon atoms with up to three substituents independently selected from the group consisting of fluorine, C₁₋₄ alkyl, oxo, hydroxy, amino and aminocarbonyl, and wherein R¹³ is hydrogen, C₁₋₄ alkyl or C₃₋₆ cycloalkyl, formyl or C₁₋₄ alkylcarbonyl; and R¹⁵ is C₁₋₄ alkyl; provided that G¹ is not chlorine when G² is chlorine or cyano; or a salt, hydrate and / or solvate thereof acceptable for pharmaceutical use. |
| priorityDate | 2011-12-15-04:00^^<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: 56.