http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-091272-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
| filingDate | 2013-06-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2015-01-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-091272-A1 |
| titleOfInvention | PIRAZOLOPIRIMIDONA AND PIRAZOLOPIRIDONA AS TANQUIRASA INHIBITORS |
| abstract | The compounds of formula (1) are useful in the treatment of cancer. Claim 1: Compound of the formula (1) wherein: Q and X are, independently at each occurrence, N or CH; R¹ is selected from the group consisting of hydrogen, C₁₋₆ alkyl, C₁₋₆ hydroxyalkyl, dihydroxy-C₁₋₆ alkyl, 1,1-dioxothian-4-yl or tetrahydropyran-4-yl; R² is a remainder of formula (2) or (3); Y is selected from the group consisting of CR⁴R⁴ or NR⁴, in which R⁵ is hydrogen, C₁₋₆ alkyl, -OH or -CN; R³ is selected from the group consisting of: (i) hydrogen, (ii) C₁₋₆ alkyl, (iii) C₁₋₆ haloalkyl, (iv) halogen, (v) C₁₋₆ alkoxy, (vi) S ( O) ₂R³ᵃ in which R³ᵃ is C₁₋₆ alkyl, C ciclo cycloalkyl, C₁₋₃ alkyl-C₃₋₆ cycloalkyl or NH₂ or (vii) CONR³ᵇR³ᶜ in which R³ᵇ and R³ᶜ are independently hydrogen, C₁₋₃ or R³ᵇ alkyl and R³ᶜ together with the nitrogen to which they are attached form a cyclic amine; R⁴ is selected from the group consisting of: (i) hydrogen, (ii) C₁₋₆ alkyl, (iii) C₁₋₆ haloalkyl optionally substituted with hydroxyl, (iv) C₃₋₇ cycloalkyl, (v) C₃₋ cycloalkyl ₇-C₁₋₃ alkyl, (vi) C₅₋₁₀ bicycloalkyl, (vii) the remainder of formula (4) in which R⁶ is independently selected from the group consisting of: (a) C₁₋₆ alkyl, (b ) C₁₋₆ haloalkyl optionally substituted with hydroxyl, (c) C₁₋₆ hydroxyalkyl, (d) dihydroxy-C alquilo alkyl, (e) C₁₋₃ alkoxy-C alquilo alkyl, (f) C₃₋₇ cycloalkyl, ( g) C₁₋₆ acyl, (h) halo, (i) cyano, (j) NO₂, (k) carboxyl, (l) alkoxycarbonyl C₁₋₆, (m) CONR⁴ᵇR⁴ᶜ in which R⁴ᵇ and R⁴ᶜ are independently hydrogen, alkyl C₁₋₆ or R⁴ᵇ and R⁴ᶜ together with the nitrogen atom to which they are attached form a cyclic amine, (n) -S (O) ₂R⁴ᵃ in which R⁴ᵃ is C₁₋₆ alkyl, c Clo-icloalkyl, C₁₋₃-C₃₋₆ -alkyl or NH₂ alkyl, (o) NR⁴ᵇR⁴ᶜ, in which R⁴ᵇ and R⁴ᶜ are independently C₁₋₆ alkyl or hydrogen, (p) OR⁴ᵈ in which R⁴ᵈ is selected from the group consisting of: (i) hydrogen, (ii) C₁₋₆ alkyl, (iii) C₁₋₃ alkoxy-C₁₋₃ alkyl, (iv) C₁₋₆ hydroxyalkyl, also optionally replacing said hydroxyalkyl with halogen, (v) dihydroxy-C₁₋₆ alkyl, (vi) (alkyl) ₂₋₆NR⁴ᵉCR⁴ᶠ in which R⁴ᵉ and R⁴ᶠ are independently hydrogen or C₁₋₆ or R⁴ᵉ alkyl and R⁴ᶠ together with the nitrogen to which they are attached form a cyclic amine which optionally contains another heteroatom selected from NR⁴ᵍ, O or S (O) ₀₋₂ in which R⁴ᵍ is hydrogen or C₁₋₃ alkyl, (vii) oxetanyl, (viii) tetrahydropyranyl, (ix) 1,1-dioxothianyl, (x) (1-Oxothiethan-3-yl) methyl and (xi) (alkyl) ₂₋₆OR⁴ʰ in the that R⁴ʰ is C (O) CH (NH₂) R⁴ⁱ in which R⁴ⁱ is C₁₋₆ alkyl or P (= O) (OH) ₂, (q) heterocyclyl-C alquilo alkyl in which said heterocycle is piperidine, morpholine , piperazine or 4-methylpiperazine; r) 1H-tetrazol-5-yl, and (s) 1,1-dioxothiollan-3-yl, (viii) heteroaryl, (ix) heteroaryl-C₁₋₃ alkyl, (x) heterocyclyl, (xi) heterocyclyl-alkyl C₁₋₃, (xii) -S (O) ₂R⁴ᵃ in which R⁴ᵃ is C₁₋₆ alkyl, C₃₋₆ cycloalkyl, C₁₋₃ alkyl C₃₋₆-cycloalkyl or NH₂, (xiii) 1,1-dioxothiollan-3 -ilo; wherein: each of said cycloalkyl is optionally substituted with one to three hydroxyls or C₁₋₃-C₁₋₆ alkoxy; each of said heteroaryls is optionally further substituted with C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₃ hydroxyalkyl, C₁₋₆ haloalkyl, halogen, CN, pyrazinyl or C₁₋₆ alkylsulfonyl; each of said heterocycles is selected from tetrahydropyran-4-yl, tetrahydrofuran-2-yl, oxethan-3-yl, 1,1-dioxo-tetrahydrothiophenyl, 1,1-dioxothiollan-3-yl, 1-Boc-piperidinyl , piperidin-4-yl, 1-methyl-piperidin-4-yl, 1 -Boc-piperazin-4-yl, 1-methyl-piperazin-4-yl or piperazin-4-yl; or a pharmaceutically acceptable salt thereof. |
| priorityDate | 2012-06-07-04:00^^<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: 40.