Day: October 26, 2022

On August 13, 2020, Genung, Nathan; Guckian, Kevin M.; Vessels, Jeffrey; Zhang, Lei; Gianatassio, Ryan; Lin, Edward Yin Shiang; Xin, Zhili published a patent.Quality Control of 3-Chloro-6-fluorobenzo[d]isoxazole The title of the patent was Preparation of heteroaryloxypyrrolidinylmethylthiazolylacetamide derivatives and analogs for use as O-GlcNAcase inhibitors. And the patent contained the following:

Title compounds I [R1 = halo, alkyl, haloalkyl, or alkoxy; R3 = H or alkyl; R4 = H, alkyl, haloalkyl, or cycloalkyl; or R3 and R4 are taken together with their intervening atoms to form an (un)substituted heterocyclyl; R5 = (un)substituted bicyclic aryl, bicyclic heteroaryl, bicyclic cycloaliphatic, or bicyclic heterocyclyl; each Y independently = CH, C(halo), N, etc. wherein at least one is N; Z = C(O), CH2C(O), (CH2)2, etc.; n = 0 to 8; p = 0 or 1; with provisions], and their pharmaceutically acceptable salts, are prepared and disclosed as O-glycoprotein-2-acetamido-2-deoxy-3-D-glucopyranosidase (O-GlcNAcase) inhibitors. Thus, e.g., II was prepared by a multistep procedure (preparation given). I were evaluated in OGA enzyme inhibition biochem. assays, e.g., II demonstrated an IC50 value of <1.0 nM. The experimental process involved the reaction of 3-Chloro-6-fluorobenzo[d]isoxazole(cas: 374554-89-9).Quality Control of 3-Chloro-6-fluorobenzo[d]isoxazole

The Article related to thiazolylacetamide heteroaryloxypyrrolidinylmethyl preparation oglcnacase oga inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Quality Control of 3-Chloro-6-fluorobenzo[d]isoxazole

Referemce:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

On June 28, 2012, Boss, Christoph; Brotschi, Christine; Heidmann, Bibia; Sifferlen, Thierry; Williams, Jodi T. published a patent.Computed Properties of 374554-89-9 The title of the patent was 3,8-Diazabicyclo[4.2.0]octane derivatives as orexin receptor antagonists and their preparation and use for the treatment of diseases. And the patent contained the following:

The invention relates to 3,8-Diazabicyclo[4.2.0]octane derivatives of formula cis-I, which are orexin receptor antagonists and which are useful in the treatment of diseases. Compounds of formula cis-I wherein Ar1is substituted Ph and substituted 5- to 6-membered heteroaryl; Ar2 is substituted 5- to 6-membered heteroaryl and substituted 8- to 10-membered bicyclic heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound cis-II was prepared by multistep procedure (procedure given). All the invention compounds were evaluated for their orexin receptor antagonistic activity. From the assay, it was determined that compound cis-II exhibited IC50 values of 1 nM and 5 nM towards OX1 and OX2, resp. The experimental process involved the reaction of 3-Chloro-6-fluorobenzo[d]isoxazole(cas: 374554-89-9).Computed Properties of 374554-89-9

The Article related to diazabicyclooctane preparation orexin receptor antagonist treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Computed Properties of 374554-89-9

Referemce:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

On November 22, 2001, Yamada, Akira; Spears, Glen; Hayashida, Hisashi; Tomishima, Masaki; Ito, Kiyotaka; Imanishi, Masashi published a patent.Reference of 3-Chloro-6-fluorobenzo[d]isoxazole The title of the patent was Preparation of N-imidazolylphenyl-5,6-dihydrobenzo[h]quinazolin-4-amines and other N-containing heterocyclic amines as 5-hydroxytryptamine antagonists for treatment of CNS disorders. And the patent contained the following:

Title compounds AMQNHZ [I; wherein A = H, (un)substituted, unsaturated, N-containing heterocyclic group, or C(NH)NHR; R = (un)substituted aryl or heterocyclic group; M = (CH2)n, (CH2)nO(CH2)m, or (CH2)nNH(CH2)m; n and m = independently 0-2; Q = (un)substituted cycloalkylene group, arylene, or divalent heterocyclic group; Z = (un)substituted, unsaturated, mono-, di-, tri-, or tetra-cyclic, N-containing heterocyclic group which may contain addnl. N, O, and S atoms as the ring member(s), e.g. indeno[1,2,3-de]phthalazinyl or 5,6-dihydrobenzo[h]quinazolinyl; and the prodrugs or pharmaceutically acceptable salts thereof] were prepared For example, a mixture of 4-chloro-5,6-dihydrobenzo[h]quinazoline, 3-(1,2-dimethyl-1H-imidazol-5-yl)aniline, and 1,3-dimethyl-2-imidazolidinone was heated for an hour at 200°C, cooled, treated with 1N aqueous NaOH and water, and worked up to give II. I are 5-hydroxytryptamine (5-HT) antagonists useful for the prevention and/or treatment of central nervous system (CNS) disorders, such as anxiety, depression, obsessive compulsive disorders, migraine, anorexia, Alzheimer’s disease, sleep disorders, bulimia, panic attacks, withdrawal from drug abuse, schizophrenia, and disorders associated with spinal trauma and/or head injury (no data). The experimental process involved the reaction of 3-Chloro-6-fluorobenzo[d]isoxazole(cas: 374554-89-9).Reference of 3-Chloro-6-fluorobenzo[d]isoxazole

The Article related to imidazolylphenyl benzoquinazolinamine preparation hydroxytryptamine antagonist, benzoquinazolinamine imidazolylphenyl preparation central nervous system disorder treatment and other aspects.Reference of 3-Chloro-6-fluorobenzo[d]isoxazole

Referemce:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics