http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-095198-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_7c5e77c181522ee1fd44df1ae5ac2196 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4725 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4725 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 |
| filingDate | 2014-03-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2015-09-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-095198-A1 |
| titleOfInvention | DERIVATIVES OF TRIAZOLONA DE PIRIDINILO AND PIRIDINILO FUSIONADO |
| abstract | The pharmaceutical compositions of the compound are useful for autoimmune diseases; inflammatory disorders, cancer, non-malignant proliferative disorders; and other conditions associated with BTK. Claim 1: A compound of formula (1), a tautomer thereof or a pharmaceutically acceptable salt of the compound or tautomer, wherein: R¹ is selected from hydrogen, halo, -CN, C₁₋₄ alkyl, C₁₋₄ haloalkyl, and -OR¹⁴; R² and R³ are each independently selected from hydrogen, halo, -CN, R⁶, and R⁷, or R² and R³, together with carbon atoms to which they are attached, form a benzene ring or a pyridine ring where the Benzene ring is optionally substituted with one to four substituents independently selected from halo, -CN, R⁶, and R⁷, and the pyridine ring is optionally substituted with one to three substituents independently selected from halo, -CN, R⁶, and R⁷; R⁴ has the formula (2), where the wavy line indicates a point of attachment; L is selected from -O-, -CH₂O-, and -N (R⁴ᵉ) -; R⁴ᵃ is selected from -CH₂R⁵ and ethenyl optionally substituted with one to three substituents independently selected from halo, cyano, and R⁷; and (a) R⁴ᶜ is hydrogen, R⁴ᵉ is selected from hydrogen and C₁₋₄ alkyl when L is -N (R⁴ᵉ) -, and R⁴ᵇ and R⁴ᵈ, together with a nitrogen atom and carbon atoms at which R⁴ᵇ, R⁴ᶜ, and R⁴ᵈ are respectively attached, form a pyrrolidine ring or a piperidine ring, each ring optionally substituted with one to six substituents independently selected from halo, C₁₋₄ alkyl, and C₁₋₄ haloalkyl; or (b) R⁴ᵇ is selected from hydrogen and C₁₋₄ alkyl, R⁴ᵈ is hydrogen, L is -N (R⁴ᵉ) -, and R⁴ᶜ and R⁴ᵉ, together with the carbon atoms and a nitrogen atom at which R⁴ᶜ, R⁴ᵈ , and R⁴ᵉ are respectively attached, form a pyrrolidine ring or a piperidine ring, each ring optionally substituted with one to six substituents independently selected from halo, C₁₋₄ alkyl, and C₁₋₄ haloalkyl; or (c) R⁴ᵈ is hydrogen, R⁴ᵉ is selected from hydrogen and C₁₋₄ alkyl when L is -N (R⁴ᵉ) -, and R⁴ᵇ and R⁴ᶜ, together with the nitrogen and carbon atoms to which R⁴ᵇ and R⁴ᶜ are respectively attached , they form a pyrrolidine ring or a piperidine ring, each ring optionally substituted with one to six substituents independently selected from halo, C₁₋₄ alkyl, and C₁₋₄ haloalkyl; R⁵ is selected from hydrogen, halo, and C₁₋₄ alkyl; each R⁶ is independently selected from -OR⁸, -N (R⁸) R⁹, -NR⁸C (O) R⁹, -NHC (O) NR⁸R⁹, -NR⁸C (O) NHR⁹, -C (O) R⁸, -C (O ) OR⁸, -C (O) N (R⁸) R⁹, -C (O) N (R⁸) OR⁹, -C (O) N (R⁸) S (O) ₂R⁷, -N (R⁸) S (O) ₂R⁷ , -SR⁸, -S (O) R⁷, -S (O) ₂R⁷, and S (O) ₂N (R⁸) R⁹; each R⁷ is independently selected from (a) C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl, each optionally substituted with one to five substituents independently selected from halo, oxo, -CN, and R¹⁰; and (b) C₃₋₁₀- (CH₂) ₘ- cycloalkyl, C₆₋₁₄- (CH₂) ₘ- aryl, C₂₋₆- (CH₂) ₘ- heterocyclyl, and C₁₋₉- (CH₂) ₘ- heteroaryl, each one optionally substituted with one to five substituents independently selected from halo, oxo, -CN, R¹⁰, and C₁₋₆ alkyl optionally substituted with one to five substituents independently selected from halo, oxo, -CN, and R¹⁰; each R⁸ and R⁹ is independently selected from (a) hydrogen; (b) C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl, each optionally substituted with one to five substituents independently selected from halo, oxo, -CN, and R¹⁰; and (c) C₃₋₁₀- (CH₂) ₘ- cycloalkyl, C₆₋₁₄- (CH₂) ₘ- aryl, C₂₋₆- (CH₂) ₘ- heterocyclyl, and C₁₋₉- (CH₂) ₘ- heteroaryl, each one optionally substituted with one to five substituents independently selected from halo, oxo, -CN, R¹⁰, and C₁₋₆ alkyl optionally substituted with one to five substituents independently selected from halo, oxo, -CN, and R¹⁰; each R¹⁰ is independently selected from -OR¹¹, -N (R¹¹) R¹², -N (R¹¹) C (O) R¹², -NHC (O) NR¹¹R¹², -NR¹¹C (O) NHR¹², -C (O) R¹¹, -C (O) OR¹¹, -C (O) N (R¹¹) R¹², -C (O) N (R¹¹) OR¹², -C (O) N (R¹¹) S (O) ₂R¹³, -NR¹¹S (O) ₂R¹³ , -SR¹¹, -S (O) R¹³, -S (O) ₂R¹³, and -S (O) ₂N (R¹¹) R¹²; each R¹¹ and R¹² is independently selected from (a) hydrogen; and (b) C₁₋₆ alkyl and C₃₋₁₀- (CH₂) ₘ- cycloalkyl, each optionally substituted with one to five substituents independently selected from halo, oxo, -CN, -OH, and -NH₂; each R¹³ is independently selected from C₁₋₆ alkyl and C₃₋₁₀- (CH₂) cycloalkyl, each optionally substituted with one to five substituents independently selected from halo, oxo, -CN, -OH, and-NH₂ ; each R¹⁴ is independently selected from hydrogen, C₁₋₄ alkyl, and C₁₋₄ haloalkyl; and each m is independently selected from 0, 1, 2, 3, and 4; wherein each heteroaryl and heterocyclyl of R⁷, R⁸, and R⁹ independently has one to four heteroatoms, each of the heteroatoms independently selected from N, O, and S. |
| priorityDate | 2013-03-11-04:00^^<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: 38.