Category: 1427433-22-4

On January 14, 2021, Garofalo, Albert W.; De Lombaert, Stephane; Schwarz, Jacob Bradley; Andreotti, Daniele; Sabbatini, Fabio Maria; Serra, Elena; Bernardi, Silvia; Migliore, Marco; Budassi, Federica; Beato, Claudia published a patent.Related Products of 1427433-22-4 The title of the patent was Indazoles and azaindazoles as LRRK2 inhibitors in the treatment of CNS disorders and their preparation. And the patent contained the following:

The invention relates compounds of formula I, their preparation and their use as inhibitors of LRRK2 in the treatment of CNS disorders. Compound I, wherein A is halo, (un)subsititued C1-6 alkyl, (un)subsititued C2-6 alkenyl, etc.; ring B is Ph and 5- to 10-membered heteroaryl wherein said 5- to 10-membered heteroaryl comprises 1, 2 and 3 ring-forming heteroatoms independently864 selected from N, O and S; X2 is N and CR2; X3 is N and CR3; X4 is N and CR4; no more than two of X2, X3 and X4 are simultaneously N; R1 is independently H, halo, C1-6 alkyl, etc.; R2 and R4 are independently H, halo, C2-6 alkenyl, etc.; R3 is H, halo, C1-6 haloalkyl, etc.; n is 0, 1, 2, and 3; and pharmaceutically acceptable salts thereof, are claimed. Compound II was prepared by reacting 3-bromo-1H-indazol-5-amine with 3-furanylboronic acid yielding 3-(furan-3-yl)-1H-indazole-5-amine, then 5-cyano-3-fluoropyridine-2-carboxylic acid underwent amidation with 3-(furan-3-yl)-1H-indazole-5-amine to yield compound II. Compound II was evaluated for LRRK2 inhibitory activity resulting in a wild type LRRK2 and G2019S LRRK2 IC50 of ≤ 100 nM for both. Compounds of the invention were evaluated for their LRRK2 inhibitory activity (data given). The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methyl-benzoic acid(cas: 1427433-22-4).Related Products of 1427433-22-4

The Article related to indazole azaindazole preparation lrrk2 inhibitor cns disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 1427433-22-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 21, 2022, Garofalo, Albert W.; Schwarz, Jacob Bradley; Sabbatini, Fabio Maria; Migliore, Marco; Bernardi, Silvia; Budassi, Federica published a patent.Related Products of 1427433-22-4 The title of the patent was Preparation of indazoles and azaindazoles as LRRK2 inhibitors. And the patent contained the following:

The present invention is directed to indazole and azaindazole derivatives I and II [A = (un)substituted aryl, cycloalkyl, 5-14 membered heteroaryl, etc.; L = O or NH; ring B = Ph or 6-membered heteroaryl; ring C = Ph or 6-membered heteroaryl, wherein ring C is fused to ring D; X2 = N or CR2; X3 = N or CR3; X4 = N or CR4; wherein not more than two of X2, X3, and X4 are simultaneously N; each R1 and R5 = (independently) H, halo, alkyl, etc.; R2-R4 = (independently) H, halo, alkyl, etc.; n = 0-3; m = 0-1; p = 0-3; wherein in I: when ring B = Ph, then n = 1-3 and R1 = group other than H] or pharmaceutically acceptable salts thereof which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders such as Parkinson’s disease. E.g., a multi-step synthesis of III, starting from 6-bromo-1H-indazole and 1-cyclopropyl-4-iodopyrazole, was described. Exemplified compounds I and II were tested in the LRRK2 kinase activity assay (data given). Pharmaceutical composition comprising compound I or II was disclosed. The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methyl-benzoic acid(cas: 1427433-22-4).Related Products of 1427433-22-4

The Article related to indazole azaindazole preparation lrrk2 inhibitor cns disorder parkinson disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 1427433-22-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On May 21, 2021, Weis, Erik; Hayes, Martin A.; Johansson, Magnus J.; Martin-Matute, Belen published an article.Application of 1427433-22-4 The title of the article was Iridium-catalyzed C-H methylation and d3-methylation of benzoic acids with application to late-stage functionalizations. And the article contained the following:

An iridium-catalyzed carboxylate-directed ortho C-H methylation and d3-methylation of benzoic acids was reported. The method used com. available reagents and precatalyst and requires no inert atm. or exclusion of moisture. Substrates bearing electron-rich and electron-poor groups were successfully methylated, including compounds with competing directing/coordinating groups. The method was also applied to the LSF of several marketed drugs, forming analogs with increased metabolic stability compared with the parent drug. The experimental process involved the reaction of 3-Bromo-2-fluoro-6-methyl-benzoic acid(cas: 1427433-22-4).Application of 1427433-22-4

The Article related to benzoic acid potassium methyltrifluoroborate iridium catalyst regioselective methylation, methylbenzoic acid preparation, applied chemistry, chemistry, green chemistry, organic chemistry and other aspects.Application of 1427433-22-4

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary