- KRAS G12D INHIBITORS
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The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.
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Paragraph 01133
(2021/03/05)
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- 6-AMINOPYRIDIN-3-YL PYRAZOLES AS MODULATORS OF RORgT
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The present invention comprises compounds of Formula I. wherein: R1, Q, R3, R4, R5, R6, A1, and A2 are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
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Paragraph 0252-0253
(2020/01/08)
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- PYRIDINYL PYRAZOLES AS MODULATORS OF RORyT
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The present invention comprises compounds of Formula I. wherein: R1, R3, R4, R5, R6, and Q are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
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Paragraph 0355
(2020/01/08)
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- NAPHTHYRIDINES AS INHIBITORS OF HPK1
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Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.
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Paragraph 0935; 0936
(2018/10/21)
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- Transition-metal-free BF3-mediated regioselective direct alkylation and arylation of functionalized pyridines using grignard or organozinc reagents
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A formal regioselective cross-coupling of various pyridines with alkyl and aryl groups can be achieved by a BF3·OEt2-mediated addition of Grignard or organozinc reagents to pyridines bearing various substituents (chloro, bromo, cyano, vinyl, phenyl, carbethoxy, nitro, etc.) followed by an oxidative aromatization mediated by chloranil. Good regioselectivity and wide functional group tolerance make this method very versatile for the preparation of polyfunctional pyridines. No transition-metal catalyst is required in these coupling reactions.
- Chen, Quan,Du Jourdin, Xavier Mollat,Knochel, Paul
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supporting information
p. 4958 - 4961
(2013/05/22)
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- SYNTHESIS OF 3-HALO- AND 3-FORMYL-4-ALKYLPYRIDINES
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In the presence of a catalytic amount of cuprous iodide, the addition of Grignard reagents to the 1-phenoxycarbonyl salts of 3-halopyridines gives 4-alkyl-3-halo-1-phenoxycarbonyl-1,4-dihydropyridines.The crude dihydropyridines were aromatized with o-chloroanil to give 4-alkyl-3-halopyridines.Several 4-alkylnicotinaldehydes were synthesized in a similar manner from the cyclic acetal (1,3-dioxolane) of 3-pyridinecarboxaldehyde.After aromatization with sulfur, the crude acetals were hydrolyzed with oxalic acid to give the desired pyridinecarboxaldehydes.
- Comins, Daniel L.,Smith, Roy K.,Stroud, Eric D.
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p. 339 - 344
(2007/10/02)
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