- 2-OXO-2,3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-4-METHYLBENZAMIDE DERIVATIVES AND SIMILAR COMPOUNDS AS RIPK2 INHIBITORS FOR TREATING E.G. AUTOIMMUNE DISEASES
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Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein α, β, R2, R3, R4, R5, R8, R9, X1, X6, and X7 are defined in the specification. The compounds of formula 1 are receptor-interacting protein kinase 2 (RIPK2) inhibitors for treating e.g. type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer and non-malignant proliferative disorders, such as e.g. allergic rhinitis, asthma, atopic dermatitis, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, lupus nephritis, psoriasis, immune thrombocytopenic purpura, inflammatory bowel disease, chronic obstructive pulmonary disease, Sjogren's syndrome, ankylosing spondylitis, Behcet's disease, graft versus host disease, pemphigus vulgaris, idiopathic plasmacytic lymphadenopathy, atherosclerosis, myocardial infarction and thrombosis. The present description discloses the preparation of exemplary compounds as well as pharmacological data thereof (e.g. pages 107 to 208; examples 1 to 109; table 1). An exemplary compound is e.g. N-cyclopropyl-2-fluoro-5-(l-(2-fluoroethyl)-3-(l-hydroxy-2-methylpropan-2-yl)-2-oxo-2,3-dihydro-lH-imidazo[4,5-b]pyridin-6-yl)-4-methylbenzamide (example 1).
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Paragraph 0424-0426
(2020/10/20)
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- Preparation method for o-tolylacetic acid aryl formic acid derivative
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The invention discloses a preparation method for an o-tolylacetic acid aryl formic acid derivative. According to the method, new C-C bonds can be formed, the organic o-tolylacetic acid aryl formic acid derivative is obtained, the good functional group tolerance is achieved, and the o-tolylacetic acid aryl formic acid derivative which cannot be easily obtained by adopting other methods can be synthesized; according to the method, adopted raw materials are easy to obtain, the yield is high, the reaction conditions are mild, the substrate range is wide, and after-treatment is simple and green.
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Paragraph 0088-0091
(2019/07/16)
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- Palladium-Catalyzed ortho-C-H Methylation of Benzoic Acids
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A palladium-catalyzed methylation of C-H bonds of benzoic acids with di-tert-butyl peroxide as the methylating reagent under an external oxidant and ligand-free conditions has been achieved. The reaction is found to be directed by a weakly coordinating carboxyl group, offering a facile route for the synthesis of highly functionalized ortho-methyl benzoic acids.
- Lv, Weiwei,Wen, Si,Liu, Jing,Cheng, Guolin
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p. 9786 - 9791
(2019/08/26)
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- PHENYL mTORC INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 00364; 00490; 00497; 00521; 00551
(2018/05/27)
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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 1643; 1644
(2018/10/21)
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- SUBSTITUTED BENZENE COMPOUNDS
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The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
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Page/Page column 318
(2012/11/06)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure
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Page/Page column 42
(2010/11/18)
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- Synthesis of Sterically Hindered 1,3-Connected Polyarylmethanes
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Sterically hindered 1,3-connected polyarylmethanes were prepared by repetitive additions of aryllithiums to carbonyl compounds.Synthetic routes with various degree of convergence were used.Variable temperature NMR spectroscopy, in conjunction with other t
- Rajca, Andrzej,Janicki, Slawomir
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p. 7099 - 7107
(2007/10/02)
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