Category: 142327-44-4

On April 9, 2015, Andrews, Mark D.; af Forselles, Kerry; Beaumont, Kevin; Galan, Sebastien R. G.; Glossop, Paul A.; Grenie, Mathilde; Jessiman, Alan; Kenyon, Amy S.; Lunn, Graham; Maw, Graham; Owen, Robert M.; Pryde, David C.; Roberts, Dannielle; Tran, Thien Duc published an article.Product Details of 142327-44-4 The title of the article was Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain. And the article contained the following:

The transient receptor potential (TRP) family of ion channels comprises nonselective cation channels that respond to a wide range of chem. and thermal stimuli. TRPM8, a member of the melastatin subfamily, is activated by cold temperatures (<28°), and antagonists of this channel have the potential to treat cold induced allodynia and hyperalgesia. However, TRPM8 has also been implicated in mammalian thermoregulation and antagonists have the potential to induce hypothermia in patients. The authors report herein the identification and optimization of a series of TRPM8 antagonists that ultimately led to the discovery of I (PF-05105679). The clin. finding with this compound will be discussed, including both efficacy and its ability to affect thermoregulation processes in humans. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Product Details of 142327-44-4

The Article related to trpm antagonist cold pain analgesic, pf-05105679, trp channel, trpm8, clinical tool, hypothermia, ion channel, pain, thermoregulation, Pharmacology: Structure-Activity and other aspects.Product Details of 142327-44-4

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

On November 13, 2008, Bonnert, Roger Victor; McInally, Thomas; Thom, Stephen published a patent.Product Details of 142327-44-4 The title of the patent was Preparation of imidazoquinolines as TLR7 immunomodulators. And the patent contained the following:

Title compounds I [R1 = (un)substituted alkyl; Z1 = alkylene or cycloalkylene; X1 = NR5, NCOR5, CONR5, NR5CO, SO2NR5, etc.; Y1 = single bond or alkylene; each R2 independently = halo, CN, OH, thiol, alkyl, etc.; R3 = (un)substituted alkyl; each Ra independently = halo, CN, OH, thiol, alkyl, hydroxyalkyl, etc.; R5 = H, 3- to 8-membered saturated heterocyclic ring, (un)substituted alkyl or cycloalkyl; or R5 = alkylene which may be linked to a carbon atom within a alkylene group Z1 so as to form a saturated 4- to 7-membered nitrogen containing ring; with the proviso; m, n, p and q independently = 0-2; A = monocyclic or bicyclic aryl or monocyclic or bicyclic heteroaryl], and their pharmaceutically acceptable salts, are prepared and disclosed as toll-like receptors (TLR7) modulators. Thus, e.g., II was prepared in 8 steps starting from 4-hydroxyquinoline. II exhibited pEC50 value of 6.5 in human TLR7 assay. Having immuno-modulating properties via TLR7, I are useful in the treatment of viral or allergic diseases and cancers, etc. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Product Details of 142327-44-4

The Article related to imidazoquinoline preparation tlr7 immunomodulator allergy antiviral antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Product Details of 142327-44-4

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

On June 21, 2012, McInally, Thomas; Pimm, Austen published a patent.Electric Literature of 142327-44-4 The title of the patent was Imidazo[4,5-c]quinolin-1-yl derivative useful in therapy, and preparation thereof. And the patent contained the following:

The invention provides the compound of formula I and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound in therapy. Compound I is useful in the treatment of asthma, COPD, allergic rhinitis, allergic conjunctivitis, atopic dermatitis, cancer, hepatitis B, hepatitis C, HIV, HPV, bacterial infections, actinic keratosis or pre-cancerous skin lesions. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Electric Literature of 142327-44-4

The Article related to imidazoquinoline preparation asthma copd cancer hepatitis allergic rhinitis treatment, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Electric Literature of 142327-44-4

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

On October 10, 2013, Ahn, Kay; Boehm, Markus; Cabral, Shawn; Carpino, Philip A.; Futatsugi, Kentaro; Hepworth, David; Kung, Daniel W.; Orr, Suvi; Wang, Jian published a patent.Electric Literature of 142327-44-4 The title of the patent was Preparation of pyrrolidinylimidazopyridinylpiperidinylmethanone derivatives and analogs for use as diacylglycerol acyltransferase 2 inhibitors. And the patent contained the following:

Title compounds I [A = CH2, O, S, etc.; B = bond, CH2, oxetanyl, (un)substituted cyclopropyl, etc.; C and D independently = N, CH, CF, or C(CH3), wherein only one is N; R1 = (un)substituted C(O)heterocyclyl, C(O)NH2, or heteroaryl; R2 = (un)substituted alkyl, alkoxy, cycloalkyl, aryl, etc.; R3 = OH, F, (un)substituted alkyl, or cycloalkyl; n = 0 to 2], and their pharmaceutically acceptable salts, are prepared and disclosed as diacylglycerol acyltransferase 2 (DGAT2) inhibitors. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated in DGAT2 inhibition assays, e.g., II demonstrated an IC50 value of 1.7 nM. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Electric Literature of 142327-44-4

The Article related to imidazopyridinylpiperidinylmethanone pyrrolidinyl derivative preparation diacylglycerol acyltransferase dgat2 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Electric Literature of 142327-44-4

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

On September 16, 2004, Constan, Alexander Angelo; Keshary, Prakash Raj; MacLean, David Burton; Paralkar, Vishwas Madhav; Roman, Doina Cosma; Thompson, David Duane; Wright, Timothy Michael published a patent.Recommanded Product: 142327-44-4 The title of the patent was Use of EP2 selective receptor agonists in medical treatment of pulmonary hypertension and other conditions. And the patent contained the following:

The invention discloses methods for treating pulmonary hypertension, facilitating joint fusion, facilitating tendon and ligament repair, reducing the occurrence of secondary fracture, treating avascular necrosis, facilitating cartilage repair, facilitating bone healing after limb transplantation, facilitating liver regeneration, facilitating wound healing, reducing the occurrence of gastric ulceration, treating hypertension, facilitating the growth of tooth enamel or finger or toe nails, treating glaucoma, treating ocular hypertension, and repairing damage caused by metastatic bone disease using an EP2 selective receptor agonist. Preparation of compounds, e.g. 7-[(4-butylbenzyl)-(pyridine-3-sulfonyl)amino]heptanoic acid, is described. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Recommanded Product: 142327-44-4

The Article related to ep2 receptor agonist therapeutic, pulmonary hypertension treatment ep2 receptor agonist, heptanoate derivative preparation ep2 receptor agonist therapeutic, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Recommanded Product: 142327-44-4

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

On June 16, 2005, Collini, Michael D.; Singhaus, Robert R.; Hu, Baihua; Jetter, James W.; Morris, Robert L.; Kaufman, David H.; Miller, Christopher P.; Ullrich, John W.; Unwalla, Rayomand J.; Wrobel, Jay E.; Quinet, Elaine; Nambi, Ponnal; Bernotas, Ronald C.; Elloso, Merle published a patent.Electric Literature of 142327-44-4 The title of the patent was Preparation of quinolines useful in treating LXR (liver X receptor)-mediated diseases. And the patent contained the following:

This invention provides quinolines of formula I (R1 = H or C1-C3 alkyl; X1 = a bond or an appropriate group to link R2 which is an optionally substituted heterocycle; X2 = a bond or CH2; R3 = optionally substituted Ph, naphthyl, or heterocycle; R4, R5, and R6 = H or F, R7 = H, C1-C4 alkyl, C1-C4 perfluoroalkyl, halogen, NO2, CN, optionally substituted phenyl) that are useful in the treatment or inhibition of LXR mediated diseases (no data). The LXR mediated diseases specifically claimed are, for example, atherosclerosis, Alzheimer’s disease, dementia, diabetes, multiple sclerosis, and thyroiditis. Pharmaceutical compositions containing the compounds of the invention and synthetic procedures for preparing them are also claimed. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Electric Literature of 142327-44-4

The Article related to quinoline preparation liver x receptor mediated disease treatment, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Electric Literature of 142327-44-4

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

On May 3, 2007, Hurt, Clarence Ray; Pennell, Andrewm. K.; Wright, John Jessen; Wang, Qiang; Leleti, Manmohan Reddy; Thomas, William D.; Li, Yandong; Dragoli, Dean R. published a patent.Formula: C10H10O3 The title of the patent was Substituted dihydropyridines as C5a receptor modulators and their preparation, pharmaceutical compositions and use in the treatment of diseases. And the patent contained the following:

Compounds of formula I are provided that are modulators of the C5a receptor. Compounds of formula I wherein A is N or C; B is halo, CN, NO2, CO2H and derivatives, CONH2 and derivatives, NH and derivatives, etc.; R1 is H, amino, (un)substituted C1-8 (di)alkylamino, (un)substituted C1-8 alkoxy, (un)substituted C1-8 (halo)alkyl, etc.; C1 and C2 are independently (un)substituted (hetero)aryl, (un)substituted (hetero)aryl-C1-4 alkyl, (un)substituted (hetero)cycloalkyl, and (un)substituted (hetero)cycloalkyl-C1-4 alkyl; L1 is bond, (un)substituted C1-8 (hetero)alkylene, (un)substituted C1-8 alkenylene, (un)substituted C2-8 alkynylene, S, SO, SO2, O, NH and derivatives; R2 is OH and derivatives, NH2 and derivatives, C1-8 (halo)alkyl, C3-6 cycloalkyl, C2-8 alkenyl, (hetero)aryl, etc.; R3 is H, C1-6 (halo)alkyl, C1-6 acyl, C3-8 cycloalkyl, (hetero)aryl, etc.; D is O, S, and NOH and derivatives; and their pharmaceutically acceptable salts thereof, are claimed. The compounds are substituted dihydropyridines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathol. activation of C5a receptors. Example compound II was prepared by condensation of 4-methylbenzaldehyde with acetone; the resulting (E)-4-(4-methylphenyl)-3-buten-2-one underwent cyclization with di-Et malonate followed by decarboxylation to give 4-(4-methylphenyl)cyclohexane-1,3-dione, which underwent cyclization with 3-hydroxybenzaldehyde, cyclopentyl acetoacetate and ammonium acetate to give compound II. All the invention compounds were evaluated for their C5a receptor modulatory activity. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Formula: C10H10O3

The Article related to dihydropyridine preparation c5a receptor modulator treatment disease, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Formula: C10H10O3

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

On October 26, 2021, Duan, Wenhu; Shen, Xu; Wang, Wei; Wang, Jiaying; Cao, Sufen; Lv, Jianlu; Xu, Xu published a patent.Application In Synthesis of Methyl 2-(3-formylphenyl)acetate The title of the patent was Preparation of compounds with AMPK agonistic activity and prodrugs thereof and their application in medicine. And the patent contained the following:

The invention discloses the preparation method of the compounds with AMPK agonistic activity with general formula I, [wherein X = H or halogen; M = N or CH, R1 = substituted or unsubstituted 6-10 membered aryl, substituted or unsubstituted 3-10 membered heteroaryl containing 1-3 heteroatoms selected from N, O and S; R2 = hydroxyl, carboxyl, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted 6-10 membered aryl and substituted or unsubstituted 3-10 membered heteroaryl containing 1-3 heteroatoms selected from N, O and S], which has the advantages of preparing and treating diseases related to abnormal energy metabolism, neurodegenerative diseases and inflammation related diseases; cardiovascular and cerebrovascular diseases, tumor drug. For example, 2-(3-(7-chloro-6-(4-(1- hydroxycyclobutyl) phenyl)-2-oxo-1,2- dihydroquinoline-3-yl) phenyl) acetic acid was prepared via Suzuki-coupling with 1-(4- bromophenyl) cyclobutanol and bis(pinacolato)diboron, hydrolysis of di-Et isophthalate, followed by acylation with 2-amino-5-bromo-4-chlorobenzaldehyde, followed by Knoevenagel reaction, followed by Suzuki coupling with 1-[4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl] cyclobutanol, and followed by hydrolysis. The compounds with AMPK agonistic activity can be used as therapeutic agents for diseases related to abnormal energy metabolism, neurodegenerative diseases, neurol. and mitochondrial dysfunction and disorder diseases, inflammation related diseases, cardiovascular and cerebrovascular diseases and tumors. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Application In Synthesis of Methyl 2-(3-formylphenyl)acetate

The Article related to ampk agonist quinoline condensation suzuki coupling hydrolysis human, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application In Synthesis of Methyl 2-(3-formylphenyl)acetate

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

On April 22, 1992, Kulagowski, Janusz J.; Rowley, Michael; Leeson, Paul D.; Mawer, Ian Michael published a patent.Recommanded Product: Methyl 2-(3-formylphenyl)acetate The title of the patent was Preparation of 3-aryl-4-hydroxy-2-quinolones as NMDA and AMPA antagonists. And the patent contained the following:

Title compounds (I; R1-R6 = H, hydrocarbyl, heterocyclyl, halo, cyano, CF3, NO2, OR7, SR7, SOR7, SO2R7, SO2NR7R8, NR7R8, etc.; R1R2 = atoms to form a hetero- or carbocycle; R7, R8 = H, hydrocarbyl, heterocyclyl), were prepared Thus, 3-methoxyphenylacetyl chloride and Me 2-amino-4-chlorobenzoate were refluxed 18 h in CH2Cl2 to give Me 4-chloro-3-(3-methoxyphenyl)acetamidobenzoate. The latter was stirred with KN(SiMe3)2 in THF/PhMe to give title compound II. All I prepared displaced 3H-trans-3-carboxy-5,7-dichloro-4-(phenylaminocarbonylamino)-1,2,3,4-tetrahydroquinoline from strychnine-insensitive sites of NMDA receptors in rat forebrain membranes with IC50 < 50 μM. Dosage forms were prepared containing several specific I. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Recommanded Product: Methyl 2-(3-formylphenyl)acetate

The Article related to arylhydroxyquinolone preparation nmda antagonist, ampa antagonist arylhydroxyquinolone antagonist, quinolone arylhydroxy arylhydroxyquinolone antagonist, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Recommanded Product: Methyl 2-(3-formylphenyl)acetate

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

On December 1, 2005, Epple, Robert; Russo, Ross; Azimioara, Mihai; Xie, Yongping published a patent.Safety of Methyl 2-(3-formylphenyl)acetate The title of the patent was Isoxazole compounds as PPAR modulators, their preparation, pharmaceutical compositions, and use in therapy. And the patent contained the following:

The invention relates to isoxazole compounds of formula I, which are modulators of peroxisome proliferator-activated receptors (PPAR), particularly PPARδ. In compounds I, R1 is selected from (un)substituted C1-6 alkyl, (un)substituted C3-12 cycloalkyl, (un)substituted C3-8 heterocyclyl, (un)substituted C6-10 aryl, and (un)substituted C5-10 heteroaryl; R2 is selected from (CH2)nO(CH2)nOR5, (CH2)nOR5, CO2R5, C(O)N(R4)2, C(O)N(R4)(CH2)nOR4, CO2(CH2)nOR5, C(O)(CH2)nOR5, C(O)N(R4)(CH2)nOR5, C(O)N(R4)(R5), and C(O)N(R4)(CH2)nR5, where n is 0-4, R4 is H or C1-6 alkyl, and R5 is C1-6 alkyl, C3-12 cycloalkyl, C3-8 heterocyclyl, C6-10 aryl, or C5-10 heteroaryl, or R4 and R5, together with the nitrogen atom to which they are attached, form C3-8 heterocyclyl or C5-10 heteroaryl; and R3 is selected from (un)substituted C3-12 cycloalkyl, (un)substituted C3-8 heterocyclyl, (un)substituted C6-10 aryl, and (un)substituted C5-10 heteroaryl; including pharmaceutically acceptable salts, hydrates, solvates, isomers, and prodrugs thereof. The invention also relates to the preparation of I, pharmaceutical compositions comprising a therapeutically effective amount of compound I in combination with one or more pharmaceutically acceptable excipients, as well as to the use of the compositions to treat or prevent diseases or disorders associated with PPAR activity. Esterification of 3-bromophenylacetic acid followed by coupling with cyanide, reduction of the nitrile to an aldehyde, condensation with hydroxylamine, and chlorination gave chlorooxime II. N-Boc-2-bromoethylamine was substituted with 2,4-dichlorophenol followed by deprotection, amidation with Et benzoylacetate to give benzoylacetamide III, which underwent cyclocondensation with chlorooxime II and ester hydrolysis, resulting in the formation of isoxazole IV. Most preferred compounds of the invention express an EC50 value for PPARδ of less than 100 nM. The compounds of the invention are at least 100-fold selective for PPARδ over PPARγ. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Safety of Methyl 2-(3-formylphenyl)acetate

The Article related to isoxazole preparation selective ppar delta modulator, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.Safety of Methyl 2-(3-formylphenyl)acetate

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