http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-095310-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_b8726f713a6d86892687edccfa03d886 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cf32b60391b469c41e86c353437f5751 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02A50-30 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P33-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-107 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-08 |
| filingDate | 2014-03-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d27ec9e171fcbba7b57feb93db5da802 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f0c56e6f24ec39ee3dcbd0162890c197 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7dfab71eb48592bb21c96d3ead6d2137 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0dc7018c027b82f92e48bcb2cfef5f26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_050baae98dce131771a59289850e7172 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_208bc010b830d5520b6700604a8741b1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e6566e63c8913bdcdfd3a2e5cf3e0c4d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_41b564720804a4590119be794457c1d6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cf9999377aab52db11a36e1b39483cf8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4ed3459b6a1f7fc2f26f7c7e2123e5cc |
| publicationDate | 2015-10-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-095310-A1 |
| titleOfInvention | COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITARY DISEASES |
| abstract | The present further provides pharmaceutical compositions comprising such compounds and methods of using such compounds to treat, prevent, inhibit, improve, or eradicate the pathology and / or symptomatology of a disease caused by a parasite, such as leishmaniasis, human African trypanosomiasis and Chagas disease. Claim 1: A compound of the formula (1), or a pharmaceutically acceptable salt, or stereoisomer thereof; wherein Rˣ is hydrogen or C₁₋₄ alkyl; L¹ is a bond, CH₂C (O) -, -C (O) - or -S (O) ₂-; R¹ is selected from hydrogen, nitrogen, C₁₋₄ alkyl, C₁₋₄ alkenyl, C₁₋₆ alkoxy, amino, -NR⁷ᵃR⁷ᵇ, C₃₋₆ cycloalkyl, C₄₋₇ heterocycloalkyl, C₅₋₆ heterocycloalkenyl, phenyl, benzyl and heteroaryl C₅₋₉; or -NRˣL¹R¹ is nitrogen; or R¹ and Rˣ are taken together with the atoms to which R¹ and Rˣ are linked to form a C₄₋₉ heteroaricyclic substituted by 1 or 2 oxo, wherein R⁷ᵃ is hydrogen or C₁₋₄ alkyl; R⁷ᵇ is selected from hydrogen, C₁₋₄ alkyl, C₁₋₄ haloalkyl, C₁₋₆ alkoxy, amino, C₃₋₆ cycloalkyl, C₃₋₆ cycloalkyl substituted by C₁₋₄ alkoxy, and C₅₋₆ heteroaryl, wherein the C₅₋₆ heteroaryl of R⁷ᵇ is optionally substituted by 1 to 2 substituents independently selected from halogen, C₁₋₄ alkyl, C₁₋₄ alkoxy or amino; and wherein the hydrogens available in the C₁₋₄ alkyl of R⁷ᵃ and R⁷ᵇ are optionally replaced by deuterium; C₁₋₄ alkyl, C₁₋₄ alkenyl, C₁₋₆ alkoxy, amino, C₃₋₆ cycloalkyl, C₄₋₇ heterocycloalkyl, C₅₋₆ heterocycloalkenyl, phenyl, or C₅₋₉ heteroaryl of R¹ is optionally substituted by 1 to 4 substituents independently selected from hydroxyl, halogen, cyano, oxo, C₁₋₄ alkyl, C₁₋₄ hydroxyalkyl, C₁₋₄ haloalkyl, C₁₋₆ alkoxy, C halo haloalkoxy, C₁₋₄ alkylcarbonyloxy, hydroxycarbonyl, C₁₋₄ alkylcarbonyl, C₁₋₄ alkoxycarbonyl, aminocarbonyl, amino, C₁₋₄ alkylamino, C₁₋₄ alkylcarbonylamino, C₁₋₄-N-C-alkylaminocarbonyl, C₁₋₆ alkoxycarbonylamino, C₁₋₄-N-C₁₋₄ alkylaminocarbonyl, C₁ alkylsulfonyl ₋₄, C₃₋₆ cycloalkyl substituted by C₁₋₆ alkoxy, C₃₋₆ cycloalkyl, C₄₋₆ heterocycloalkyl, phenyl, and C₅₋₆ heteroaryl; wherein the C₃₋₆ cycloalkyl, C₄₋₆ heterocycloalkyl, C₅₋₆ heterocycloalkyl, phenyl or the C₅₋₆ heteroaryl substituent is further optionally substituted by 1 to 2 substituents independently selected from halogen, C₁₋₄ alkyl, C₁ alkylamino ₋₄, or C₄₋₆ heterocycloalkyl; R³ is selected from hydrogen, halogen, cyano, C₁₋₄ alkyl and C₁₋₄ haloalkyl; R⁴ is selected from hydrogen, halogen, C₁₋₄ alkyl, C₁₋₄ haloalkyl, and -C (O) R¹⁰, wherein R¹⁰ is selected from hydroxyl, C₁₋₄ alkyl, C₁₋₄ alkoxy, amino, C₁₋₄ alkylamino, C₃₋₆ cycloalkyl and C₄₋₆ heterocycloalkyl, wherein C₁₋₄ alkyl, C₁₋₄ alkoxy, amino, C₁₋₄ alkylamino, C₃₋₆ cycloalkyl or C₄₋₆ heterocycloalkyl of R¹⁰ is optionally substituted by 1 to 2 substituents independently selected from hydroxyl, halogen and C₁₋₄ alkyl; L³ is selected from a bond, C₃₋₇ cycloalkyl, C₄₋₇ heterocycloalkyl, C₄₋₇ cycloalkenyl, C₄₋₇ heterocycloalkenyl, phenyl, and C₅₋₆ heteroaryl; R⁰ is selected from hydrogen, hydroxyl, halogen, oxo, nitrogen, -N = CHN (CH₃) ₂, C₁₋₆ alkyl, C₁₋₄ haloalkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, C₁₋₄ alkoxy, C₄₋₆ heterocycloalkyloxy, -C (O) R⁶, -NR²ᵃR²ᵇ, -NR⁵C (O) R⁶, -NR⁵S (O) ₂R⁸, -S (O) ₂R⁸, tri-C-alkylsilyl, C₃₋₆ cycloalkyl, C₄ heterocycloalkyl ₋₆, C₃₋₆ cycloalkenyl, C₄₋₆ heterocycloalkenyl, phenyl, and C₅₋₆ heteroaryl; whenever L³ is a bond, R⁰ is not hydrogen; wherein the C alquilo alkyl, C₂₋₄ alkenyl, C₂₋₄ alkynyl, or C alco alkoxy of R⁰ optionally is substituted by 1-2 substituents independently selected from hydroxyl, halogen, C₁₋₄ alkoxy, trimetrisylyl alkoxy C₁₋₄, C₁₋₄ alkoxycarbonyl, -NR¹¹ᵃR¹¹ᵇ, C₁₋₄ alkoxycarbonylamino, C₅₋₆ heterocycloalkyloxy, C₃₋₇ cycloalkyl, C₅₋₆ heterocycloalkyl, phenyl and C y heteroaryl, wherein C₃₋₇ cycloalkyl, C₅₋ heterocycloalkyl ₆, phenyl or the C₅₋₆ heteroaryl substituent is further optionally substituted by hydroxyl, halogen, C₁₋₄ alkyl or C₁₋₄ alkoxycarbonylamino, and wherein R¹¹ᵃ and R¹¹ᵇ are independently hydrogen or C₁₋₄ alkyl; C hetero heterocycloalkyloxy, C₃₋₆ cycloalkyl, C₄₋₆ heterocycloalkyl, C₄₋₆ heterocycloalkenyl, phenyl or C₅₋₆ heteroaryl of R⁰ is optionally substituted with 1 to 4 substituents independently selected from hydroxyl, halogen, oxo, C₁ alkyl ₋₄, C₁₋₄ hydroxyalkyl, C₁₋₄ haloalkyl, - (CH₂) ₀₋₄NRᵃRᵇ, C₅₋₆ aryl-C₁₋₄ alkyl, C₄₋₆ heterocycloalkyl-C₁₋₄ alkyl, C₁₋₄ alkoxy, C₁₋₄ alkoxycarbonyl , amino, C₁₋₄ alkylamino, C₁₋₄ alkylsulfonyl, C₄₋₆ heterocycloalkyl, wherein Rᵃ and Rᵇ are each independently hydrogen, C₁₋₄ alkyl or C₃₋₆ cycloalkyl; R²ᵃ is selected from hydrogen, C₁₋₄ alkyl, C₁₋₄ alkoxy-C₁₋₄ alkyl, C₁₋₄ alkylcarbonyloxy-C₁₋₄ alkyl, and a C₅₋₆ heteroaryl substituted by C₁₋₄ haloalkyl; R²ᵇ is selected from hydrogen, C₁₋₆ alkyl, C₁₋₆ haloalkyl, C₁₋₄ aminoalkyl, C₁₋₄ alkoxycarbonyl, C₃₋₆ cycloalkyl, C₄₋₆ heterocycloalkyl, C₅₋₆ heterocycloalkenyl, and C₅₋₆ heteroaryl, in wherein C₁₋₆ alkyl of R²ᵇ is optionally substituted by C₁₋₄ alkoxy, amino, C₁₋₄ alkylamino, C₄₋₆ cycloalkyl, C₄₋₆ heterocycloalkyl, phenyl or C₅₋₆ heteroaryl, wherein C₄₋₆ cycloalkyl, heterocycloalkyl C₄₋₆, phenyl or the C₅₋₆ heteroaryl substituent is optionally substituted by hydroxy, halogen, C₁₋₄ alkyl, C₁₋₄ haloalkyl, or C₁₋₄ alkyloxycarbonylamino; the C₄₋₆ heterocycloalkyl, C₅₋₆ heterocycloalkenyl or C₅₋₆ heteroaryl of R²ᵇ is optionally substituted by 1 to 2 substituents independently selected from C₁₋₄ alkyl and C₁₋₄ haloalkyl; R⁵ is hydrogen or C₁₋₄ alkyl; R⁶ is selected from hydrogen, C₁₋₆ alkyl, C₁₋₆ hydroxyalkyl, C₁₋₆ haloalkyl, C₂₋₆ alkenyl, C₁₋₄ alkoxy, C₁₋₆ haloalkoxy, cycloalkoxyl |
| priorityDate | 2013-03-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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