Tag: 100-200

On May 16, 2013, Harriman, Geraldine C.; Masse, Craig E.; Harwood, James; Bhat, Sathesh; Greenwood, Jeremy Robert published a patent.Application of 64987-16-2 The title of the patent was Preparation of thienopyrimidinedione derivatives as ACC inhibitors. And the patent contained the following:

The present invention provides compounds, specifically thienopyrimidine derivatives I [X = O, S, or NR; R1 = H, (un)substituted alkyl; R2 = halo, R, OR, etc.; or R1 and R2 are taken together to form (un)substituted 4-7 membered partially unsaturated carbocyclo-, or heterocyclo-, benzo-, or 5-6 membered heteroaryl- fused ring; R = H, (un)substituted alkyl, Ph, etc.; L1, L2 = a bond, alkylene, cyclobutylenyl, etc.; R3 = H, halo, CN, etc.; R4 = H, (un)substituted 3-8 membered monocyclic saturated or partially unsaturated carbocyclic ring, etc.; with the provisos], useful as inhibitors of Acetyl CoA Carboxylase (ACC), pharmaceutical compositions thereof, and methods of using the same for treating ACC-mediated disorders such as obesity, dyslipidemia, hyperlipidemia, fungal, parasitic or bacterial infections in a subject. The invention further provides a method of inhibiting ACC in a plant comprising contacting the plant with the inhibitor compound I. Over three-hundred compounds I were prepared E.g., a multi-step synthesis of (2S)-II, starting from Et 3-oxobutanoate and Et 2-cyanoacetate, was described. Exemplified compounds I were tested in in vitro ACC1 and ACC2 inhibition assays (data given). 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 thienopyrimidinedione preparation acetyl coa carboxylase acc inhibitor metabolic disorder, antiobesity fungicide antiparasitic antibacterial thienopyrimidinedione preparation acc inhibitor, dyslipidemia hyperiipidemia treatment thienopyrimidinedione preparation acc inhibitor, thienopyrimidine preparation acetyl coa carboxylase acc inhibitor metabolic disorder and other aspects.Application of 64987-16-2

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

On November 2, 2020, Zhang, KaiYue; Li, Jing; Wang, KaiXuan; An, Xiaoying; Wang, LanZhi published an article.Formula: C5H5NOS The title of the article was Atom-economical Approaches to 1,5-Benzodiazepines Containing Indole Ring via Fe3O4@SiO2-PTSA-catalyzed Multi-component Domino Reactions. And the article contained the following:

Four novel atom-economical approaches for synthesis of 1,5-dihydrospiro[benzo[b][1,4]diazepine-2,3′-indole] compounds, e.g., I via three-component or four-component domino reactions was developed in presence of a catalytic amount of magnetic nanoparticles (Fe3O4@SiO2-PTSA) in ethanol, which provided an efficient one-pot synthesis of 1,5-benzodiazepines with multi-ring system and functional groups containing indole, aryl, ester, acyl and alkyl groups in excellent yields. In a one-pot operation, two new nitrogen heterocycle (indole and diazepine) rings and four new chem. bonds (one C-C, two C-N and one C=C) were constructed by series of domino reactions. Furthermore, plausible catalytic synthesis reaction mechanisms had been proposed. The advantages of these methods were green reaction process, recyclable magnetic catalyst, mild reaction conditions, short reaction time and high yields of products. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Formula: C5H5NOS

The Article related to iron oxide silica supported toluenesulfonic acid nanoparticle catalyst preparation, dihydrospiro benzodiazepine indole chemoselective regioselective green preparation atom economy, phenylenediamine ketone indole multicomponent domino magnetic nanoparticle catalyst, ketone phenylenediamine indole dmf dimethylacetal multicomponent domino magnetic nanocatalyst and other aspects.Formula: C5H5NOS

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

On August 16, 2001, Fotouhi, Nader; Gillespie, Paul; Guthrie, Robert William; Pietranico-Cole, Sherrie Lynn; Yun, Weiya published a patent.Synthetic Route of 19989-66-3 The title of the patent was Preparation of N-aroyldehydroamino acids as lymphocyte function associated antigen-1 antagonists.. And the patent contained the following:

Title compounds [I; R1 = H, OH, amino, halo; R2 = H, OH, halo; R3 = H; R2R3 = atoms to form Ph, pyrrole, pyrroline, pyrazole, triazole, imidazole, etc., rings; A = CH2CH2CH(OH), CH2CH2CO, CH2NHCO, etc.; R4, R5 = H, Me, Et; B = H, alkyl, (substituted) (bicyclic) (hetero)aryl, etc.; R6 = CO2H, CO2R7, CH2OH, etc.; R7 = alkyl, dimethylaminoalkyl, pyrrolidinylalkyl, etc.], were prepared Thus, Me (Z)-3-(1H-benzotriazol-5-yl)-2-[[2-chloro-4-[[(3-hydroxybenzyl)amino]carbonyl]-6-methylbenzoyl]amino]propenoate (preparation given) was stirred 125 h with LiOH in MeOH/THF/H2O to give 61% (Z)-3-(1H-benzotriazol-5-yl)-2-[[2-chloro-4-[[(3-hydroxybenzyl)amino]carbonyl]-6-methylbenzoyl]amino]propenoic acid. The latter inhibited LFA-1 binding to immobilized ICAM-1 with IC50 = 0.4 nM. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Synthetic Route of 19989-66-3

The Article related to aroyldehydroamino acid preparation lymphocyte function associated antigen antagonist, propenoate aroylamino preparation lfa1 antagonist, amino acid dehydro aroyl lymphocyte function associated antigen antagonist, t cell activation inhibitor aroylaminopropenoate preparation, psoriasis graft rejection dermatitis asthma arthritis treatment aroylaminopropenoate and other aspects.Synthetic Route of 19989-66-3

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

On September 4, 1997, Jeon, Yoon T.; Gluchowski, Charles published a patent.SDS of cas: 70202-00-5 The title of the patent was Preparation of novel indoles and benzothiazoles for cloned human alpha 2 receptors. And the patent contained the following:

The title compounds [I-IV; R1-R3 = H, C1-7 alkyl, C2-7 alkenyl, alkynyl; R4-R6 = H, halo, Oh, etc.; R7 = H, NH, C1-7 alkyl, etc.; R8 = H, C1-7 alkyl, C2-7 alkenyl, etc.; R9 = H, Ph, C1-7 alkyl, etc.; X = CH2, O, NH, S] which are selective for cloned human alpha 2 receptors and therefore useful for lowering intraocular pressure, for treating presbyopia, migraine, hypertension, alc. withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal congestion, urinary incontinence as well as for use as analgesics, sedatives, anesthetics, cognition enhancers and ocular vasoconstriction agents, were prepared Thus, reaction of 7-bromo-5-aminoindole with 2-imidazoline-2-sulfonic acid (ISA) afforded 46% I [R1-R5 = H; R6 = Br; R7-R9 = H; X = N] which showed pEC50 of 9.36 at alpha 2 receptor. The experimental process involved the reaction of 7-chloro-benzothiazol-6-ylamine(cas: 70202-00-5).SDS of cas: 70202-00-5

The Article related to adrenoceptor agonist indole benzothiazole preparation, anesthetic indole benzothiazole preparation, sedative indole benzothiazole preparation, vasoconstriction ocular indole benzothiazole preparation, antiglaucoma agent indole benzothiazole preparation, migraine indole benzothiazole preparation, antihypertensive indole benzothiazole preparation and other aspects.SDS of cas: 70202-00-5

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

On December 31, 2021, Stevanovic, Nevena; Mazzeo, Paolo Pio; Bacchi, Alessia; Matic, Ivana Z.; Djordjic Crnogorac, Marija; Stanojkovic, Tatjana; Vujcic, Miroslava; Novakovic, Irena; Radanovic, Dusanka; Sumar-Ristovic, Maja; Sladic, Dusan; Cobeljic, Bofzidar; Andjelkovic, Katarina published an article.Name: 2-Acetylthiazole The title of the article was Synthesis, characterization, antimicrobial and cytotoxic activity and DNA-binding properties of d-metal complexes with hydrazones of Girard’s T and P reagents. And the article contained the following:

In this work synthesis, characterization and crystal structures of 1, Zn(II) complex ([ZnL1(NCS)2]), with (E)-1-(2-oxo-2-(2-(quinolin-2-ylmethylene)hydrazinyl)ethyl)pyridin-1-ium chloride (HL1Cl) and 2, Bi(III) complex ([BiHL2Cl4]x1/2CH3OH), with (E)-N,N,N-trimethyl-2-oxo-2-(2-(1-(thiazol-2-yl)ethylidene)hydrazinyl)ethan-1-aminium chloride (HL2Cl), have been reported. Zn(II) complex possesses a distorted trigonal bipyramidal geometry while surroundings around Bi(III) ion are extended pentagonal bipyramidal. Antimicrobial activity, brine shrimp assay and DPPH radical scavenging activity of both complexes, including previously synthesized complexes with HL2Cl ligand (Zn(II) and Ni(II)) and complexes with (E)-N,N,N-trimethyl-2-oxo-2-(2-(1-(pyridin-2-yl)ethylidene)hydrazinyl)ethan-1-aminium chloride (HL3Cl) (Zn(II), Cu(II), Cd(II), Co(II), Fe(III), Ni(II)), were evaluated. For the most active complexes, cytotoxic activity against five malignant cancer cell lines (HeLa, A375, MCF7, PC-3 and A549) and normal cell line HaCaT, as well as generation of reactive oxygen species (ROS), was tested. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Name: 2-Acetylthiazole

The Article related to quinolinylmethylene hydrazinylpyridinium zinc thiocyanide complex preparation crystal mol structure, thiazolylethylidene hydrazinylethylaminium bismuth complex preparation crystal mol structure antimicrobial, cytotoxic dna complexation metal hydrazone girard t p reagent, antimicrobial activity, cytotoxic activity, dna-binding experiments and other aspects.Name: 2-Acetylthiazole

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

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.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. 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 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