Category: 64987-16-2

On August 26, 2003, Bizzarro, Fred Thomas; Corbett, Wendy Lea; Grippo, Joseph Francis; Haynes, Nancy-Ellen; Holland, George William; Kester, Robert Francis; Mahaney, Paige Erin; Sarabu, Ramakanth published a patent.Application In Synthesis of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of cycloalkylheteroaryl propionamides as glucokinase activators for treatment of type II diabetes. And the patent contained the following:

Title compounds [I; R1, R2 = H, halo, amino, hydroxyamino, NO2, cyano, sulfonamido, perfluoroalkyl, alkylthio, alkylsulfonyl, alkylsulfinyl, etc.; R3 = alkyl, cycloalkyl; R4 = certain un- or monosubstituted 5- and 6-membered heteroaromatic rings connected by a ring C atom; R4 (claims) = un- or monosubstituted triazine, pyrazine, or pyridazine; and their pharmaceutical acceptable salts], were prepared via amidation, for use as glucokinase activators for treatment of type II diabetes. Thus, the invention compound N-(5-chlorothiazol-2-yl)-3-cyclopentyl-2(R)-[4-(methanesulfonyl)phenyl]propionamide (II) was prepared by addition of 3-cyclopentyl-2(R)-[4-(methanesulfonyl)phenyl]propionic acid (preparation given) to a stirred mixture of triphenylphosphine and N-bromosuccinimide in methylene chloride at 0°, followed by stirring at room temperature for 30 min, addition of a solution of 2-amino-5-chlorothiazole hydrochloride and pyridine in methylene chloride, and stirring at 25° overnight. All of the exemplified compounds I activated glucokinase in vitro, exhibiting an SC1.5 ≤ 30 μM. Selected invention compounds exhibited glucokinase activator activity in vivo when administered orally to mice. Thus, I are expected to increase insulin secretion in the treatment of type II diabetes. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Application In Synthesis of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to cycloalkylheteroaryl propionamide preparation thiazolyl glucokinase activator diabetes, antidiabetic thiazole pyrazine pyridazine pyridine pyrimidine glucokinase activator preparation and other aspects.Application In Synthesis of Methyl 2-(2-aminothiazol-4-yl)acetate

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

On October 5, 2000, Bizzarro, Fred Thomas; Corbett, Wendy Lea; Focella, Antonino; Grippo, Joseph Francis; Haynes, Nancy-ellen; Holland, George William; Kester, Robert Francis; Mahaney, Paige E.; Sarabu, Ramakanth published a patent.HPLC of Formula: 64987-16-2 The title of the patent was Preparation of arylcycloalkylpropionamides as glucokinase activators.. And the patent contained the following:

Title compounds [I; R1, R2 = H, halo, amino, hydroxyamino, NO2, cyano, sulfonamido, perfluoroalkyl, alkylthio, alkylsulfonyl, alkylsulfinyl, etc.; R3 = alkyl, cycloalkyl; R4 = CONHR40, (substituted) 5-6 membered heteroaryl; R40 = H, alkyl, alkenyl, hydroxyalkyl, haloalkyl, etc.], were prepared for treatment of type II diabetes. Thus, 3-cyclopentyl-2-(3,4-dichlorophenyl)propionic acid (preparation given), benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate, and 2-aminothiazole in CH2Cl2 was treated with Et3N followed by 14 h stirring to give 3-cyclopentyl-2-(3,4-dichlorophenyl)-N-thiazol-2-ylpropionamide. I activated glucokinase in vitro with SC1.5≤30 μM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).HPLC of Formula: 64987-16-2

The Article related to arylcycloalkylpropionamide preparation glucokinase activator, cyclopentylphenylthiazolylpropionamide preparation glucokinase activator, diabetes type ii treatment arylcycloalkylpropionamide preparation and other aspects.HPLC of Formula: 64987-16-2

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

On March 31, 2008, Rao, V. Rajeswar; Reddy, V. Ravinder published an article.HPLC of Formula: 64987-16-2 The title of the article was Synthesis of some new types of 3-coumarinyl-substituted pyrazolopyrimidines and imidazothiazoles. And the article contained the following:

The treatment of 3-[3-(dimethylamino)-1-oxo-2-propenyl]chromen-2-ones with 3-amino-4-cyanopyrazole gave 7-(2-oxo-2H-chromen-3-yl)pyrazolo[1,5-a]pyrimidine-3-carbonitriles. The reaction of 3-(2-bromoacetyl)coumarins with 2-amino-4-(methoxycarbonylmethyl)thiazole and 2-amino-4-methylthiazole gives Me 2-(6-(2-oxo-2H-chromen-3-yl)imidazo[2,1-b]thiazol-3-yl)acetate and 3-(2-methylimidazo[2,1-b]thiazol-6-yl)-2H-chromen-2-ones, resp. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).HPLC of Formula: 64987-16-2

The Article related to aminopropenonyl chromenone cyclocondensation aminocyanopyrazole, bromoacetyl chromenone cyclocondensation aminothiazole, coumarinyl pyrazolopyrimidine preparation imidazothiazole, imidazothiazole coumarinyl preparation and other aspects.HPLC of Formula: 64987-16-2

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

On February 15, 2007, Nunes, Joseph J.; Milne, Jill; Bemis, Jean; Xie, Roger; Vu, Chi B.; Ng, Pui Yee; Disch, Jeremy S.; Salzmann, Thomas; Armistead, David published a patent.Computed Properties of 64987-16-2 The title of the patent was Preparation of benzothiazoles and thiazolopyridines as sirtuin modulators. And the patent contained the following:

The title compounds I [X7-X10 = N, CR20 or CR11 (wherein R20 = H or solubilizing group; R11 = H, (un)substituted alkyl); R19 = phenylene, pyridylene, etc.; R21 = (un)substituted NHCO, NHSO2, NHCONH, etc.; R31 = (un)substituted monocyclic or bicyclic (hetero)aryl; with proviso] and their analogs which are novel sirtuin-modulating compounds useful for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity, were prepared E.g., a multi-step synthesis of II, starting from 4-aminopyridin-3-yl diisopropylcarbamodithioate and 3-nitrobenzoyl chloride, was given. Exemplified compounds I were tested for sirtuin modulating activity (data given). Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Computed Properties of 64987-16-2

The Article related to benzimidazole preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor, benzothiazole preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor and other aspects.Computed Properties of 64987-16-2

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

On January 1, 2017, Tomasic, Tihomir; Mirt, Matic; Barancokova, Michaela; Ilas, Janez; Zidar, Nace; Tammela, Paivi; Kikelj, Danijel published an article.SDS of cas: 64987-16-2 The title of the article was Design, synthesis and biological evaluation of 4,5-dibromo-N-(thiazol-2-yl)-1H-pyrrole-2-carboxamide derivatives as novel DNA gyrase inhibitors. And the article contained the following:

Two new series of Escherichia coli DNA gyrase inhibitors bearing the 4,5-dibromopyrrolamide moiety was designed and synthesized. 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazole-2,6-diamine derivatives inhibited E. coli DNA gyrase in the submicromolar to low micromolar range (IC50 values between 0.891 and 10.4 μM). Their “ring-opened” analogs, based on the 2-(2-aminothiazol-4-yl)acetic acid scaffold, displayed weaker DNA gyrase inhibition with IC50 values between 15.9 and 169 μM. Mol. docking experiments were conducted to study the binding modes of inhibitors. 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 amido tetrahydrobenzothiazolyl pyrrolylcarboxamide preparation sar dna gyrase mol docking, phenyl acetamidothiazolyl pyrrolylcarboxamide preparation sar dna gyrase mol docking, antibacterial, dna gyrase, docking, inhibitor, thiazole and other aspects.SDS of cas: 64987-16-2

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

On July 10, 2003, Lau, Jesper; Kodra, Janos Tibor; Guzel, Mustafa; Santosh, Kalpathy Chidambareswaran; Mjalli, Adnan M. M.; Andrews, Robert Carl; Polisetti, Dharma Rao published a patent.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of N-aryl amide derivatives as glucokinase (GK) activators. And the patent contained the following:

Amides and ureas, such as R3-X-A(R1)-L1-G-NR4R5 [A = N, C(R2); G = SO2, CO; L1 = bond or linking alkylene, etc.; X = bond, O, S, SO, SO2, N(R6), alkylene, etc.; R1, R3 = H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, etc.; R2 = H, alkyl; R1R2 = cycloalkyl or heterocyclic ring; R4 = H, alkyl; R5 = aryl, heteroaryl; R6 = H, alkyl], were prepared as GK activators for therapeutic use in the treatment of diseases or conditions where increasing glucokinase activity is beneficial, such as impaired glucose tolerance (IGT), Syndrome X, type 2 diabetes, type 1 diabetes, dyslipidemia, hyperlipidemia, hypertension, and obesity. Thus, amide I was prepared via formation of 2-(3,4-dichlorophenoxy)hexanoic acid in 55% yield by reacting Et 2-hydroxyhexanoate with 3,4-dichlorophenol using Ph3P and diisopropyl azodicarboxylate in THF followed by formation of I in 72% by an amidation reaction of 2-(3,4-dichlorophenoxy)hexanoic acid with 2-aminothiazole using TFFH and DIEA in THF. The prepared amides were assayed for human liver GK activation activity. 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 heterocyclic amide preparation glucokinase activator, impaired glucose tolerance treatment heterocyclyl amide preparation, syndrome x treatment heterocyclyl amide preparation, diabetes treatment heterocyclyl amide preparation, dyslipidemia treatment heterocyclyl amide preparation, hyperlipidemia treatment heterocyclyl amide preparation and other aspects.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

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

On February 15, 2007, Nunes, Joseph J.; Milne, Jill; Bemis, Jean; Xie, Roger; Vu, Chi B.; Ng, Pui Yee; Disch, Jeremy S. published a patent.HPLC of Formula: 64987-16-2 The title of the patent was Preparation of imidazo[2,1-b]thiazole derivatives as sirtuin modulators. And the patent contained the following:

The title compounds I [R19 = 1,2-phenylene, 5-6 membered 1,2-heteroarylene; R20 = H or solubilizing group; R21 = (un)substituted NHCO, NHSO2, NHCONH, etc.; R31 = (un)substituted monocyclic or bicyclic (hetero)aryl; with provisos] and their analogs which are novel sirtuin-modulating compounds useful for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity, were prepared E.g., a 3-step synthesis of II, starting from 2-aminothiazole and 2-bromo-2′-nitroacetophenone, was given. Exemplified compounds I were tested for sirtuin modulating activity (data given). Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).HPLC of Formula: 64987-16-2

The Article related to benzimidazole preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor, thiazolopyridine preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor, oxazolopyridine preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor and other aspects.HPLC of Formula: 64987-16-2

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

On February 15, 2007, Nunes, Joseph J.; Milne, Jill; Bemis, Jean; Xie, Roger; Vu, Chi B.; Ng, Pui Yee; Disch, Jeremy S. published a patent.Computed Properties of 64987-16-2 The title of the patent was Preparation of imidazopyridine derivatives as sirtuin modulators. And the patent contained the following:

The title compounds I [R23, R24 = H, Me or solubilizing agent; R25 = H or solubilizing agent; R19 = 1,2-phenylene, 5-membered heteroarylene; R21 = (un)substituted NHCO, NHSO2, NHCONH, etc.; R31 = (un)substituted monocyclic or bicyclic (hetero)aryl; with provisos] and their analogs which are novel sirtuin-modulating compounds useful for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity, were prepared E.g., a 3-step synthesis of II, starting from 2-bromo-2′-nitroacetophenone and 2-aminopyridine, was given. Exemplified compounds I were tested for sirtuin modulating activity (data given). Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Computed Properties of 64987-16-2

The Article related to benzimidazole preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor, thiazolopyridine preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor, oxazolopyridine preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor and other aspects.Computed Properties of 64987-16-2

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

On February 15, 2007, Nunes, Joseph J.; Milne, Jill; Bemis, Jean; Xie, Roger; Vu, Chi B.; Ng, Pui Yee; Disch, Jeremy S.; Salzmann, Thomas; Armistead, David published a patent.Reference of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of oxazolopyridine derivatives as sirtuin modulators. And the patent contained the following:

The title compounds I [X7-X10 = N, CR20, CR22 (wherein R20 = H or solubilizing group; R22 = H, (un)substituted alkyl; one of X7-X10 = N and the others = CR20 or CR22; zero to one R20 is solubilizing group); R19 = 1,2-phenylene, pyridylene, 5-6 membered (hetero)arylene; R21 = (un)substituted NHCO, NHSO2, NHCONH, etc.; R31 = (un)substituted monocyclic or bicyclic (hetero)aryl; with provisos] and their analogs which are novel sirtuin-modulating compounds useful for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity, were prepared E.g., a 3-step synthesis of II, starting from 2-chloropyridin-3-amine and 3-nitrobenzoyl chloride, was given. Exemplified compounds I were tested for sirtuin modulating activity (data given). Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Reference of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to benzimidazole preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor, thiazolopyridine preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor, oxazolopyridine preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor and other aspects.Reference of Methyl 2-(2-aminothiazol-4-yl)acetate

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

On February 15, 2007, Nunes, Joseph J.; Milne, Jill; Bemis, Jean; Xie, Roger; Vu, Chi B.; Ng, Pui Yee; Disch, Jeremy S. published a patent.Application In Synthesis of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of benzimidazole derivatives as sirtuin modulators. And the patent contained the following:

The title compounds I [R1, R4, R6 = H or (un)substituted alkyl; R2 = (un)substituted NHCO, NHSO2, NHCONH, etc.; R3 = (un)substituted monocyclic or bicyclic (hetero)aryl; R5, R7 = H or solubilizing group; with provisos] and their analogs which are novel sirtuin-modulating compounds useful for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity, were prepared E.g., a 2-step synthesis of II, starting from 1,2-diaminobenzene and 6-aminopyridine-2-carboxylic acid, was given. Exemplified compounds I were tested for sirtuin modulating activity (data given). Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Application In Synthesis of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to benzimidazole preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor, thiazolopyridine preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor, oxazolopyridine preparation sirtuin modulator antidiabetic antiobesity cardiovascular antiinflammatory antitumor and other aspects.Application In Synthesis of Methyl 2-(2-aminothiazol-4-yl)acetate

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