http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-098991-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42e94091a4fc81b8d0237117707cc7ee |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-52 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-66 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-455 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-65616 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-437 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 |
| filingDate | 2014-12-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5044f7fee6fd64e936a8e512175c3047 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c0412516cd0cdc26dea0335ba1ea9983 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_40d7c18fc0ce811d620f8019949f7e8f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_97768f6cfa9bfdb06f11a6a6ed0c4070 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_663445a1d761b808d72aea2505f7daf7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c420cd30cdc35d83a5a4ce9269220216 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_28f86f1796bddfe66a047bcf701e10ec http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d91788d13d1a21b8e8743cc518b6668a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_06b38d5d9d0337e9ce2044c4e257e373 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6b3aed1592c09be182932148e5231ea4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f707abe022090f79774509014ead0270 |
| publicationDate | 2016-06-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-098991-A1 |
| titleOfInvention | NICOTINAMIDE COMPOUNDS REPLACED WITH HETEROARILE |
| abstract | The use of such compounds as IRAK4 modulators, and pharmaceutical compositions comprising such compounds are also described. These compounds are useful for treating, preventing or slowing inflammatory and autoimmune diseases. Claim 1: A compound characterized by the formula (1) or a salt thereof, wherein: HET is a heteroaryl selected from pyrazolyl, indolyl, pyrrolo [2,3-b] pyridinyl, pyrrolo [2,3-d] pyrimidinyl , pyrazolo [3,4-b] pyridinyl, pyrazolo [3,4-d] pyrimidinyl, 2,3-dihydro-1H-pyrrolo [2,3-b] pyridinyl, imidazo [4,5-b] pyridinyl and purinyl , wherein the heteroaryl is substituted with Rᵃ and Rᵇ; Rᵃ is H, F, Cl, Br, -CN, -OH, C₁₋₄ alkyl, C₁₋₄ fluoroalkyl, C₁₋₄ hydroxyalkyl, C₁₋₄ alkoxy, -NH₂, -NH (C₁₋₄ alkyl), -N (C₁₋₄ alkyl) ₂, -NH (C₁₋₄ hydroxyalkyl), -NH (C₁₋₄ fluoroalkyl), -NH (C₁₋₆ hydroxy-fluoroalkyl), -C (O) NH₂, -CH₂NHC (O) ( C₁₋₆ alkyl), -CH₂NHC (O) (C₁₋₆ hydroxyalkyl), -CH₂NHC (O) NH (C₁₋₆ alkyl), -CH₂NHC (O) NHCH₂ (phenyl), -CH₂NHC (O) N (C₁₋ ₄ alkyl) ₂, -CH₂NHC (O) O (C₁₋₄ alkyl), -CH₂NHC (O) (C₃₋₈ cycloalkyl), -CH₂NHC (O) (tetrahydrofuranyl), -CH₂NHC (O) CH₂ (C₃₋₆ cycloalkyl ), -CH₂NHC (O) CH₂ (tetrahydropyranyl), -CH₂NHC (O) CH₂ (phenyl), -NHC (O) (C₁₋₄ alkyl), pyrrolidinyl, hydroxypyrrolidinyl or pyridazinyl; Rᵇ is H or -NH₂; R¹ is: (i) C₁₋₆ alkyl, C₁₋₆ fluoroalkyl, C₁₋₆ hydroxyalkyl, C₁₋₈ hydroxy-fluoroalkyl, - (C₁₋₆ alkylenyl) O (C₁₋₄ alkyl), - (C₁₋₆ alkylenyl) O (C₁₋₄ fluoroalkyl), - (C₁₋₆ fluoroalkylene) O (C₁₋₄ alkyl), - (C₁₋₆ fluoroalkylene) O (C₁₋₄ deuteroalkyl), - (C₁₋₆ fluoroalkylene) O (C₁₋₄ fluoroalkyl), - (C₁₋₄ fluoroalkylene) C (C₃₋₆cycloalkyl) ₂ (OH), - (C₁₋₄ alkyleneyl) NHC (O) (C₁₋₄ alkyleneyl) OC (O) (C₁₋₃ alkyl), - (C₁₋₆ alkylenyl) NHS (O) ₂ (C₁₋₄ alkyl), - (C₁₋₆ alkyleneyl) P (O) (C₁₋₄ alkoxy) ₂, - (C₁₋₆ fluoroalkylene) NH (C₁₋₄ alkyl), - (C₁₋₆ alkylenyl) C (O) NH (C₁₋₄ alkyl), - (C₁₋₆ fluoroalkylene) C (O) NH (C₁₋₄ alkyl), - (C₁₋₆ fluoroalkylene) C ( O) NH (C₁₋₄ hydroxyalkyl) or - (C₁₋₆ fluoroalkylene) OP (O) (OH) ₂; (ii) - (C₁₋₃, alkylenyl) Rˣ, - (C₁₋₃ fluoroalkylene) Rˣ, - (C₁₋₃ alkyleneyl) C (O) Rˣ, - (C₁₋₃ alkyleneyl) C (O) NHRˣ, - ( C₁₋₃, fluoroalkylenyl) C (O) Rˣ or CH₂CF = (tetrahydropyranyl), wherein Rˣ is a cyclic group selected from C₃₋₆ cycloalkyl, tetrazolyl, 1,1-dioxidotetrahydrothiophenyl, 1,1-dioxidothiomorpholinyl, oxadiazolyl, piperidinyl, piperazinyl, pyrrolidinyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, pyridinyl, imidazolyl, morpholinyl, phenyl and triazinyl, wherein each cyclic group is substituted with 0 to 3 substituents independently selected from F, -OH, -CH₃, -C (CH₂) ₂OH, -OCH₃, -C (O) CH₂CN, -S (O) ₂CH₃, -S (O) ₂NH₂, -NHC (O) CH₃, -N (S (O) ₂CH₃) ₂, -CH₂CH₂ (acetamidophenyl), -CH₂CH₂ (methoxyphenyl), -CH₂CH₂ (sulfamoylphenyl), oxetanyl, benzyl and morpholinyl; (iii) C₃₋₆ cycloalkyl or C₄₋₆ cycloalkenyl, each substituted with 0 to 3 substituents independently selected from F, -OH, -CN, C₁₋₃ alkyl, C₁₋₃ alkoxy, -S (C₁₋₃ alkyl) , -NO₂, -S (O) ₂ (C₁₋₃ alkyl), C₁₋₄ hydroxyalkyl, -C (C₁₋₃ alkyl) (OH) (C₃₋₆ cycloalkyl), -CH₂C (O) NH (C₁₋₃ alkyl), -NHC (O) (C₁₋₃ alkyl), -NHC (O) (C₁₋₄ hydroxyalkyl), -C (O) NH (C₁₋₃ alkyl), -C (O) NH (C₁₋₃ deuteroalkyl), -C (O) NH (C₃₋₆ cycloalkyl), -NHC (O) O (C₁₋₃ alkyl), -NHS (O) ₂ (C₁₋₃ alkyl), pyridinyl, imidazolyl, pyrazolyl, methylimidazolyl, methylpyrazolyl and thiazolyl; (iv) tetrahydropyranyl, piperidinyl, pyrazolyl, phenyl, pyridinyl or pyrimidinyl, each substituted with 0 to 1 substituent selected from -OH, C₁₋₃ alkyl, C₁₋₃ fluoroalkyl, C₁₋₄ hydroxyalkyl, C₁₋₃ alkoxy, -C (O) (C₁₋₄ alkyl), -S (O) ₂ (C₁₋₄ alkyl), -S (O) ₂NH (C₁₋₄ alkyl), -NH (C₁₋₃ alkyl), -N (C₁₋ ₃ alkyl) ₂, -O (C₁₋₃ alkylenyl) N (C₁₋₃ alkyl) ₂, -CH₂ (morpholinyl), acetidinyl, oxetanyl, tetrahydropyranyl, morpholinyl, piperazinyl, piperidinyl, methylpiperazinyl, methoxypiperidinyl, pyridinyl, pyrimidinyl, pyrimidinyl and -C (O) (methylsulfonyl acetidinyl); or (v) pyrrolo [2,3-c] pyridinyl, bicyclo [2.2.1] heptan-1-ol, tetrahydrobenzo [d] thiazol-2-amine or 1,3-diazaspiro [4.5] decan-2,4- diona; and R² is (i) C₁₋₇ alkyl or C₂₋₆ alkenyl, each substituted with 0 to 3 substituents independently selected from F, -OH and -CN; - (C₁₋₄-alkylene) O (C₁₋₄-alkyl), - (C₁₋₄-alkylene) O (C₁₋₄-fluoroalkyl), - (C₁₋₆-alkyleneyl) NH₂, - (C₁₋₆-alkyleneyl) S (O) ₂ (C₁₋₃ alkyl), - (C₁₋₆ fluoroalkylene) NH (C₁₋₃ alkyl) or - (C₁₋₆ alkyleneyl) NHC (O) (C₁₋₄ fluoroalkyl); (ii) - (C₁₋₄ alkylenyl) Rʸ, wherein Rʸ is C₃₋₆ cycloalkyl, acetidinyl, oxetanyl, oxazolyl, pyridinyl, tetrahydropyranyl or morpholinyl, each substituted with or 2 substituents independently selected from F, OH and C₁₋₃ I rent; (iii) C₃₋₆ cycloalkyl, acetidinyl, oxetanyl, furanyl, tetrahydrofuranyl, pyrrolidinyl, piperidinyl or tetrahydropyranyl, each substituted with 0 to 3 substituents independently selected from F, -OH, C₁₋₃ alkyl, C₁₋₃, hydroxyalkyl, - C (O) (C₁₋₃ alkyl), -C (O) (C₁₋₃ fluoroalkyl), -C (O) (C₁₋₃ cyanoalkyl), -C (O) O (C₁₋₃ alkyl), -C (O) NH₂, -C (O) NH (C₁₋₃ alkyl), -C (O) (difluorophenyl), -NH₂, -NH (C₁₋₃ alkyl), -NH (C₁₋₃ fluoroalkyl), -NH (oxetanyl), -NHC (O) (C₁₋₃ alkyl), -NHC (O) (C₁₋₃ fluoroalkyl), -NHC (O) (C₃₋₆ cycloalkyl), -NHC (O) (fluorophenyl), - S (O) ₂ (C₁₋₃ alkyl), imidazolyl, phenyl, pyrimidinyl, fluoropyrimidinyl, chloropyrimidinyl and methoxypyrimidinyl; (iv) adamantanil, hydroxyamantanyl, benzo [d] imidazolyl, benzo [d] oxazolyl, benzo [d] triazolyl, benzothiazolyl, bicyclo [1.1.1] pentanyl or hydroxybicyclo [2.2.1] heptanyl; or (v) phenyl, pyrazolyl, thiazolyl, thiadiazolyl or indazolyl, each substituted with 0 to 2 substituents independently selected from F, Cl, -OH, -CN, C₁₋₄ alkyl, C₁₋₄ hydroxyalkyl, C₁₋₄ fluoroalkyl, C₁₋₄ cyanoalkyl, C₁₋₃ alkoxy, C₃₋₆ cycloalkyl, - (C₁₋₃ alkylenyl) O (C₁₋₃ alkyl), - (C₁₋₃ alkylenyl) O (C₁₋₃ fluoroalkyl), -C (O) NH₂, -C (O) NH (C₁₋₃ alkyl), -NHC (O) (C₁₋₃ alkyl), -NHC (O) S (O) ₂ (C₁₋₃ alkyl), -S (O) ₂NH₂ , -S (O) ₂ (C₁₋₃ alkyl), pyrazolyl, methylpyrazolyl, imidazolyl, triazolyl, methyltetrazolyl, ethyltetrazolyl, phenyl, pyrimidinyl, fluoropyrimidinyl and tetrahydropyranyl. |
| priorityDate | 2014-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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