200064-13-7Relevant articles and documents
A facile and efficient synthesis of 3-amino-5-bromopyridine derivatives using microwave irradiation
Dandu, Reddeppa Reddy,Rose, Adam C.,Hudkins, Robert L.
, p. 875 - 881 (2011)
A facile and general synthetic strategy was developed to synthesize 3-amino-5-bromopyridine derivatives under microwave heating conditions. The strategy involved reacting 3,5-dibromopyridine with an excess of an aliphatic amine using microwave heating, without the need to use either metal-mediated, base-promoted or harsh long thermal reaction times. The microwave approach enabled the rapid synthesis of 3-amino-5-bromopyridine derivatives in multi-gram quantities from commercially available starting materials.
Amination of Aryl Halides Mediated by Electrogenerated Nickel from Sacrificial Anode
Daili, Farah,Sengmany, Stéphane,Léonel, Eric
, p. 2462 - 2469 (2021/06/28)
Electrochemical C(sp2)?N couplings mediated by nickel salts generated from the sacrificial anode has been described for the first time. In this approach, the sacrificial nickel anode is employed as the sole source of nickel and the process, operationally simple to set up, enables the preparation of functionalized arylamine derivatives with moderate to good yields, under mild reaction conditions and without additional ligand. A cooperative process between the two electrodes is involved in the proposed mechanism.
CHROMENOPYRIDINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS
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Paragraph 0460, (2019/07/13)
The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula (I); where A1, A2, G, R1, R2, R3, R4, and W are described herein.
METHODS OF USING INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS
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Paragraph 0293; 0294; 0295; 0296, (2018/05/16)
This disclosure features the use of one or more indazole-3-carboxamide compounds or salts or analogs thereof, in the treatment of one or more diseases or conditions independently selected from the group consisting of a tendinopathy, dermatitis, psoriasis, morphea, ichthyosis, Raynaud's syndrome, and Darier's disease; and/or for promoting wound healing. The methods include administering to a subject (e.g., a subject in need thereof) a therapeutically effective amount of one or more indazole-3-carboxamide compounds or salts or analogs thereof as described anywhere herein.
PRMT5 INHIBITORS AND USES THEREOF
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Paragraph 00230, (2014/07/08)
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
ALDOSTERONE SYNTHASE INHIBITORS
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Paragraph 0542, (2014/11/11)
The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, R7, W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Regioselective reactions of 3,4-pyridynes enabled by the aryne distortion model
Goetz, Adam E.,Garg, Neil K.
, p. 54 - 60 (2013/02/23)
The pyridine heterocycle continues to play a vital role in the development of human medicines. More than 100 currently marketed drugs contain this privileged unit, which remains highly sought after synthetically. We report an efficient means to access di- and trisubstituted pyridines in an efficient and highly controlled manner using transient 3,4-pyridyne intermediates. Previous efforts to employ 3,4-pyridynes for the construction of substituted pyridines were hampered by a lack of regiocontrol or the inability to later manipulate an adjacent directing group. The strategy relies on the use of proximal halide or sulfamate substituents to perturb pyridyne distortion, which in turn governs regioselectivities in nucleophilic addition and cycloaddition reactions. After trapping of the pyridynes generated in situ, the neighbouring directing groups may be removed or exploited using versatile metal-catalysed cross-coupling reactions. This methodology now renders 3,4-pyridynes as useful synthetic building blocks for the creation of highly decorated derivatives of the medicinally privileged pyridine heterocycle.
INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF
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Paragraph 0438-0439, (2013/10/22)
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt path
Novel Compounds for the Treatment of Diseases Associated with Amyloid or Amyloid-like Proteins
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Page/Page column 21, (2011/10/31)
The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like prote
Novel compounds for the treatment of diseases associated with amyloid or amyloid-like proteins
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Page/Page column 27, (2011/11/01)
The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like prote
