Category: 64987-16-2

On January 9, 2020, Franch, Luigi; Ghosh, Shomir; Glick, Gary; Katz, Jason; Opipari, Anthony William, Jr.; Roush, William R.; Seidel, Hans Martin; Shen, Dong-Ming; Venkatraman, Shankar; Winkler, David Guenther published a patent.Related Products of 64987-16-2 The title of the patent was Heteroaryl compounds as NLRP modulators and their preparation. And the patent contained the following:

The invention relates to heteroaryl compounds of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt thereof, and are useful to treat connected to the modulation of NLRP3. Compounds of formula I wherein n is 0 and 1; o is 0, 1, 2 and 3; q is 1 and 2; A and E are independently 5- to 10-membered heteroaryl and C6-10 aryl; R1a is (un)substituted C1-6 alkyl and SONH2 and derivatives; R1b is substituted C1-6 alkyl, SO2NH2 and derivatives, OH and derivatives, etc.; R2 is C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, etc.; R6 and R7 are independently C1-6 alkyl, C1-6 alkoxy, halo, CN, NO2, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 2,2,2-trichloroethyl N-[2-azatricyclo[7.3.0.0[3,7]]dodeca-1,3(7),8-trien-8-yl]carbamate with 3-(hydroxymethyl)-N1-methylbenzene-1,4-disulfonamide. The invention compounds were evaluated for their NLRP3 modulatory activity. From the assay, it was determined that compound II exhibited IC50 value in the range of ≥ 0.2μM to < 1μM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Related Products of 64987-16-2

The Article related to heteroaryl preparation nlrp3 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Related Products of 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On January 9, 2020, Glick, Gary; Roush, William; Venkatraman, Shankar; Shen, Dong-Ming; Ghosh, Shomir; Seidel, Hans Martin; Franchi, Luigi; Winkler, David Guenther; Opipari, Anthony William, Jr.; Katz, Jason published a patent.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Aryl and heteroaryl compounds as NLRP modulators and their preparation. And the patent contained the following:

The invention relates to heteroaryl compounds of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt thereof, and are useful to treat connected to the modulation of NLRP3. Compounds of formula I wherein n is 0 and 1; o is 0, 1, 2 and 3; q is 1 and 2; A and E are independently 5- to 10-membered heteroaryl and C6-10 aryl; R1a is (un)substituted C1-6 alkyl, SONR11R12 and CR11R12NR11R12; R1b is substituted C1-6 alkyl, SO2NH2 and derivatives, OH and derivatives, etc.; R2 is C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, etc.; R6 and R7 are independently C1-6 alkyl, C1-6 alkoxy, halo, CN, NO2, etc.; R11 and R12 are independently H and (un)substituted C1-6 alkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by chlorination of 2-[4-[(cyclopentyloxy)methyl]-2,6-bis(propan-2-yl)phenyl]acetic acid; the resulting 2-[4-[(cyclopentyloxy)methyl]-2,6-bis(propan-2-yl)phenyl]acetyl chloride underwent amidation with 3-(hydroxymethyl)-N1-methylbenzene-1,4-disulfonamide to give compound II. The invention compounds were evaluated for their NLRP3 modulatory activity. From the assay, it was determined that compound II exhibited IC50 value in the range of ≥ 0.04μM to < 0.2μM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to heteroaryl preparation nlrp3 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On January 24, 1985, there was a patent about blood platelet.Application of 64987-16-2 The title of the patent was Alkyl 2-substituted amino-4-thiazolylacetates. And the patent contained the following:

The title esters I [R, R1 = 5-(1-imidazolyl)pentyl, Me; cyclohexylamino, Me; EtNH, Et] were prepared by reaction of II with the corresponding carboxylic acids or isocyanates. I had platelet aggregation inhibitory activity at 5-25 mg/kg-day. Thus, a mixture of 6-(1-imidazolyl)hexanoic acid 0.9, 1-hydroxybenzotriazole 0.7, and DCC 1 g in DMF was stirred 30 min at 40-50°, 0.9 g II (R1 = Me) in DMF added, and the whole stirred 1 h at 40-50% to give I [R = 5-(1-imidazolyl)pentyl, R1 = Me]. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Application of 64987-16-2

The Article related to aminothiazolylacetate blood platelet aggregation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Application of 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On May 21, 2008, Zhao, Hongfu; Liu, Gang; Zheng, Gengxiu; Sun, Bin; Guo, Fangshui; Wang, Guangzheng published a patent.Electric Literature of 64987-16-2 The title of the patent was Method for preparing 2-(2-butoxycarbonylaminothiazol-4-yl)-2-pentenoate. And the patent contained the following:

The title method comprises: (1) carrying out reaction of alkyl 2-(2-aminothiazol-4-yl)acetate 1.0 mol and di-tert-Bu dicarbonate 1.0-1.5 mol in the presence of 4-N,N-dimethylaminopyridine as catalyst at 0-80°C to obtain alkyl 2-(2-butoxycarbonylaminothiazol-4-yl)acetate, and (2) cooling alkyl 2-(2-butoxycarbonylaminothiazol-4-yl)acetate to -60-0°C, adding alkali, adding propionaldehyde, heating to room temperature, and carrying out reaction to obtain the final product. The method has the advantages of shortening reaction time, reducing usage of di-tert-Bu dicarbonate, and enhancing yield. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Electric Literature of 64987-16-2

The Article related to aminothiazolylpentenoate butoxycarbonyl preparation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Electric Literature of 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On January 31, 2014, Praveen, Aletti S.; Yathirajan, Hemmige S.; Narayana, Badiadka; Sarojini, Balladka K. published an article.Name: Methyl 2-(2-aminothiazol-4-yl)acetate The title of the article was Synthesis, characterization and antimicrobial studies of a few novel thiazole derivatives. And the article contained the following:

A series of novel N-[4-(substituted)-1,3-thiazol-2-yl]-2-(substituted)acetamides and Me 2-(2-(2-(substituted)acetamido)thiazol-4-yl)acetates were synthesized. All compounds were screened for their in vitro antibacterial activity against S. aureus, E. coli, P. aeruginosa, and K. pneumonia by disk diffusion and for antifungal activity against P. marneffei, T. mentagrophytes, A. flavus, and A. fumigatus by serial plate dilution Some of the compounds exhibited growth inhibition against all the tested bacterial strains, with MIC of 12.5-6.25 μg/mL. Among the compounds tested for antifungal activity, several of them showed a wide range of activity against all the tested strains. Most of the newly synthesized compounds were effective against fungal strains rather than bacterial strains. However, some of the compounds showed selective sensitivity against some of the bacterial strains, whereas they were unable to sustain the growth of other strains. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Name: Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to thiazole amide preparation antibacterial antifungal, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Name: Methyl 2-(2-aminothiazol-4-yl)acetate

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On February 26, 1986, Onoue, Hiroshi; Takahashi, Hiromi published a patent.Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Thiazolylpentenedioic acids. And the patent contained the following:

Esters I (R1 = NH2, protected amino; R2 = standard alc. residue; R3 = H, cyano, esterified CO2H; R4 = H, cyano, esterified CO2H) were prepared Thiazoleacetate ester II was treated with MeOCH:C(CO2Me)2; the product underwent elimination reaction to yield I (R1 = NHCO2CH2Ph, R2 = Me, R3 = R4 = CO2H), and the latter was subjected to hydrolysis-decarboxylation to give I (R1 = NHCO2CH2Ph, R2 = R3 = H, R4 = CO2H). The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to thiazolylpentenedioic acid, glutaconic acid thiazolyl, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On June 5, 2019, there was a patent about acute b-cell leukemia.Electric Literature of 64987-16-2 The title of the patent was Preparation of substituted sulfonamidothiazoles as CTRS1 inhibitors. And the patent contained the following:

The invention relates to compounds of formula I (wherein R1 is (un)substituted C1-5 alkyl and C0-2 alkyleneC3-5 cycloalkyl; R3 is H, halo, CH3, etc.; R4 and R5 are independently H, halo, C1-6 alkyl, etc.; R6 is H and C1-3 alkyl, etc.; Ar1 is 6-membered aryl and heteroaryl; Ar2 is 6-membered aryl and heteroaryl; R10 is H, halo, C1-3 alkyl, etc.; R11 is H, F, Cl, Me, etc.; R12 is H, halo, C1-4 alkyl, etc.; R13 is H, halo, Me and OMe;) and salts, solvates thereof and derivatives thereof, their preparation and use as CTR synthase 1 inhibitors for the treatment of disorders associated with cell proliferation. Example compound II was prepared by cross-coupling of N-(4-bromophenyl)-2-(2-(cyclopropanesulfonamido)thiazol-4-yl)-2-methylpropanamide with pyrimidin-5-ylboronic acid. The invention compounds were evaluated for their CTRS1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of ≤ 1μM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Electric Literature of 64987-16-2

The Article related to sulfonamidothiazole preparation ctrs1 inhibitor treatment cell proliferation, acute b-cell leukemia and other aspects.Electric Literature of 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On February 15, 2007, Srinivas, Akella Satya Surya Visweswara; Mathiyazhagan, Kasinathan; Sharada, Duddu Savaraiah; Ponpandian, Thanasekaran; Revathy, Kulasekharan; Reddy, Gaddam Om; Kamaraj, Mani; Rajagopal, Sriram published a patent.Name: Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of heterocyclic compounds as inhibitors of histone deacetylase for treatment of cancer. And the patent contained the following:

The title heterocyclic compounds with general formula of A-(CH2)m-O-C(=X)-NH-(CH2)n-E-(CH2)p-C(=Y)-N(R1)R2 [wherein A and E = independently (hetero)aryl, arylalkyl, or benzo-fused heteroaryl, etc.; X and Y = independently O, S, or (un)substituted NH; R1 and R2 = independently H, OH, alkoxy, arylalkyl, etc.; or R1 and R2 form a ring; m, n, and p = independently 0-2], or derivatives, analogs, stereoisomers, and pharmaceutically acceptable salts thereof were prepared as inhibitors of histone deacetylase (HDAC) for treatment of cancer. For example, I was prepared in a multi-step synthesis. I showed inhibitory activity with IC50 of 0.021 μM against HDAC. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Name: Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to preparation heterocyclic compound thiazole inhibitor histone deacetylase treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Name: Methyl 2-(2-aminothiazol-4-yl)acetate

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On December 31, 2012, Zhang, Lei; Chen, Xiaojie; Liu, Jun; Zhu, Qingzhang; Leng, Ying; Luo, Xiaomin; Jiang, Hualiang; Liu, Hong published an article.SDS of cas: 64987-16-2 The title of the article was Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. And the article contained the following:

Dual-target-directed agents simultaneously inhibiting glycogen phosphorylase (GP) and activating glucokinase (GK) could decelerate the inflow of glucose from glycogenolysis and accelerate the outflow of glucose in the liver, and therefore allow for better control over hyperglycemia in a synergetic manner. A series of hybrid compounds were designed by structure-assisted and ligand-based strategies. In vitro bioassays found two novel compounds I and II worthy of further optimization on balance of dual action to GP and GK. In addition, for single-target activity, two compounds exhibited more potent GP inhibitory activity and four compounds showed better GK activation than their corresponding references The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).SDS of cas: 64987-16-2

The Article related to heteroaryl amide preparation glycogen phosphorylase inhibition glucokinase activation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.SDS of cas: 64987-16-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On January 3, 2014, Srinivas, Akella Satya Surya Visweswara; Mathiyazhagan, Kasinathan; Reddy, Gaddam Om published a patent.Recommanded Product: Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of heterocyclic compounds as inhibitors of histone deacetylase for treatment of cancer. And the patent contained the following:

The title heterocyclic compounds with general formula of A-(CH2)m-O-C(=X)-NH-(CH2)n-E-(CH2)p-C(=Y)-N(R1)R2 [wherein A and E = independently (hetero)aryl, arylalkyl, or benzo-fused heteroaryl, etc.; X and Y = independently O, S, or (un)substituted NH; R1 and R2 = independently H, OH, alkoxy, arylalkyl, etc.; or R1 and R2 form a ring; m, n, and p = independently 0-2], or derivatives, analogs, stereoisomers, and pharmaceutically acceptable salts thereof were prepared as inhibitors of histone deacetylase (HDAC) for treatment of cancer. For example, I was prepared in a multi-step synthesis. I showed inhibitory activity with IC50 of 0.021 μM against HDAC. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Recommanded Product: Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to preparation heterocycle thiazole inhibitor histone deacetylase treatment cancer, antitumor agents, cytotoxic agents, neoplasm, proliferative disorders, psoriasis and other aspects.Recommanded Product: Methyl 2-(2-aminothiazol-4-yl)acetate

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica