Category: 142327-44-4

On October 26, 2012, Almstetter, Michael; Thormann, Michael; Treml, Andreas; Traube, Nadine published a patent.Product Details of 142327-44-4 The title of the patent was Pyrazolo[4,3-d]pyrimidines useful as kinase inhibitors and their preparation. And the patent contained the following:

The invention relates to pyrazolo[4,3-d]pyrimidine compounds of formula I that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. Compounds of formula I wherein A is NH, O, S, CO, etc.; R1 is alkyl, alkenyl, alkynyl, aryl, etc.; R2 is alkyl, alkenyl, alkynyl, heteroaryl, etc.; R3 is H, halo, NO2, N3, etc.; and pharmaceutically acceptable salts, solvates, hydrates, and pharmaceutically acceptable formulations thereof, are claimed. Example compound II was prepared by amination of 7-chloro-2-(4-methoxybenzyl)-5-phenyl-2H-pyrazolo[4,3-d]pyrimidine with 1H-indazol-5-amine followed by debenzylation. All the invention compounds were evaluated for their kinase inhibitory activity. From the assay, it was determined that compound II exhibited Ki value of less than 10 nM towards SYK, and an IC50 value in the range of 100 nM to 1000 nM towards LRRK2. 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 pyrazolopyrimidine preparation kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 142327-44-4

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

On March 29, 2007, Hashimoto, Kazuki; Nakamura, Tomoaki; Nakamura, Kei; Tojo, Shingo; Kurimoto, Ayumu; Isobe, Yoshiaki; Wada, Hiroki; Bonnert, Roger published a patent.Electric Literature of 142327-44-4 The title of the patent was Preparation of adenine derivatives as TLR7 agonists. And the patent contained the following:

Title compounds I [R1 = halo, (un)substituted alkyl, (un)substituted alkenyl, etc.; R2 = H, (un)substituted alkyl, (un)substituted alkenyl, etc.; X = O, S, NR4, etc.; with the proviso that if R1 is halo, X is a single bond; R4 = H, alkyl; A1 = (un)substituted, (un)saturated nitrogenous heterocycle containing hetero atoms selected from N, O and S; A2 = (un)substituted aromatic carbocycle, (un)substituted aromatic heterocycle; L3 = (un)substituted alkylene, single bond; L1, L2 = alkylene (1-3 methylene in alkylene may be replaced with O, S, NR5, etc.), single bond; R5 = H, (un)substituted alkyl, (un)substituted cycloalkyl, etc.] or their pharmaceutically acceptable salts were prepared For example, de-tert-butoxycarbonylation of 2-butoxy-9-[(1-[3-[N-(tert-butoxycarbonyl)-N-methylamino]propyl]piperidin-4-yl)methyl]-8-methoxyadenine, e.g., prepared from 4-hydroxymethylpiperidine-1-carboxylic acid tert-Bu ester in 3 steps, followed by reductive amination with 3-formylphenylacetic acid Me ester and treatment with sulfuric acid afforded compound II. In toll-like receptor 7 (TLR7) binding assays, the EC50 value of compound III was 74.5 nM. Compounds I are claimed useful for the treatment of asthma, COPD, etc. 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 adenine preparation tlr7 agonist, asthma copd treatment adenine preparation tlr7 agonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 142327-44-4

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

On October 6, 2005, Kurimoto, Ayumu; Hashimoto, Kazuki; Isobe, Yoshiaki; Brough, Stephen; Millichip, Ian; Wada, Hiroki; Bonnert, Roger; McInally, Thomas published a patent.Formula: C10H10O3 The title of the patent was Preparation of 8-oxoadenine compounds as immunomodulators. And the patent contained the following:

Title compounds I [ring A = aromatic carbocycle, etc.; R = halo, etc.; n = 0-2; Z1 = (un)substituted alkylene, etc.; X2 = O, etc.; Y1, Y2, Y3 = alkylene, etc.; X1 = O, etc.; R2 = H, (un)substituted alkyl, etc.; R1 = H, OH, etc.] were prepared For example, bromination of 2-butoxy-9-[2-(3-methoxycarbonylphenoxy)ethyl]adenine, e.g., prepared from Me 3-hydroxybenzoate in 2 steps, using Br2 followed by treatment with NaOH afforded compound II. In interferon induction assays (in vitro), the min. effective concentration of compound II was 0.3 nM. Compounds I are claimed useful for the treatment of cancer, allergy, etc. Formulation is given. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Formula: C10H10O3

The Article related to oxoadenine preparation immunomodulator, antitumor antiallergic agent oxoadenine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C10H10O3

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

On July 30, 1993, Tomioka, Hideo; Taketsuji, Kohji published an article.COA of Formula: C10H10O3 The title of the article was Formation of heptafulvene in reactions of [(methoxycarbonyl)methyl]phenylcarbene in the gas phases. And the article contained the following:

Flash vacuum pyrolysis of [[(methoxycarbonyl)methyl]phenyl]diazomethane (I) produced 1-(methoxycarbonyl)benzocyclobutene (II), as a result of intramol. C-H insertion in the ortho isomer of [[(methoxycarbonyl)methyl]phenyl]carbene (III) generated by carbene-carbene rearrangement, and 8-(methoxycarbonyl)heptafulvene (IV), presumably formed by intramol. H migration in the seven-membered ring intermediates involved in the rearrangement. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).COA of Formula: C10H10O3

The Article related to heptafulvene, methoxycarbonylmethylphenylcarbene rearrangement gas mechanism, Physical Organic Chemistry: Rearrangements, Including Isomerization and Tautomerization and other aspects.COA of Formula: C10H10O3

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

On August 18, 1994, Maier, Franz Karl; Ebert, Wolfgang; Lee-Vaupel, Mary; Gries, Heinz; Conrad, Juergen published a patent.Name: Methyl 2-(3-formylphenyl)acetate The title of the patent was Preparation of meso-tetraphenylporphyrin complexes as diagnostic and therapeutic agents. And the patent contained the following:

Title complexes comprising I [R1 = VCOA, VSO2A, VP(O)A2, NECH2COA; A = OH, OR4, NR5R6; E = acyl, alkylsulfonyl, carboxyalkyl, etc.; R2 = groups cited for R1 and R3; R3 = H, halo, alky; R4 = alkyl, CH2Ph; R5,R6 = H, hydrocarbyl, aryl(alkyl); NR5R6 = heterocyclyl; V = (un)substituted alkylene] and an ion of elements having Z = 21-32, 38, 39, 42-51, and 58-83 were prepared Thus, Mn3+ {5,10,15,20-tetrakis[4-(carboxymethoxy)phenyl]porphyrin} chloride was prepared in 3 steps from 5,10,15,20-tetrakis(4-hydroxyphenyl)porphyrin. Physiol. compatibility and relaxivity data for 2 I were given. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Name: Methyl 2-(3-formylphenyl)acetate

The Article related to mesotetraphenylporphyrin complex preparation diagnostic therapeutic, Physical Organic Chemistry: Oxidation-Reduction, Including Dehydrogenation and Hydrogenolysis and other aspects.Name: Methyl 2-(3-formylphenyl)acetate

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

On May 13, 1994, Kulagowski, Janusz J.; Baker, Raymond; Curtis, Neil R.; Mawer, Ian M.; Moseley, Angela M.; Ridgill, Mark P.; Rowley, Michael; Stansfield, Ian; Leeson, Paul D. published an article.HPLC of Formula: 142327-44-4 The title of the article was 3′-(Arylmethyl)- and 3′-(Aryloxy)-3-phenyl-4-hydroxyquinolin- 2(1H)-ones: Orally Active Antagonists of the Glycine Site on the NMDA Receptor. And the article contained the following:

Antagonists acting at the glycine site of the N-methyl-D-aspartate (NMDA) receptor are expected to have considerable therapeutic potential in a variety of disorders of the central nervous system. However in vivo studies with currently available compounds are severely compromised by the poor activities observed following systemic administration. The authors have previously followed a strategy of carboxyl replacement in known antagonists to provide 7-chloro-4-hydroxy-3-phenylquinolin-2(1H)-one (I). The authors now show that optimization of I by substitution of the 3-Ph with selected hydrophobic 3′-substituents yields a 100-fold improvement of in vitro affinity (IC50 values for displacement of [3H]L-689,560 binding and Kb values in cortical slice), combined with potent systemic anticonvulsant activity in the DBA/2 mouse audiogenic seizure model (ED50 values obtained after i.p. (i.p.) and oral (p.o.) administration). The following 3′-derivatives of I were identified: 3′-(4-methoxybenzyl)- (L-703,717), IC50 4.5 nM, Kb 25 nM, ED50 0.7 mg/kg i.p. and 0.9 mg/kg p.o.; 3′-(4-(1-methoxy)methoxybenzyl)- (L-708,541), IC50 2.2 nM, Kb 3.2 nM, ED50 0.5 mg/kg i.p. and 0.9 mg/kg p.o.; 3′-phenoxy- (L-701,324), IC50 2.8 nM, Kb 28 nM, ED50 0.9 mg/kg i.p. and 0.9 mg/kg p.o.; and 3′-(3-thienyloxy)- (L-705,022), IC50 1.4 nM, Kb 5.0 nM< ED50 0.8 mg/kg i.p. and 0.8 mg/kg p.o. These new glycine antagonists are the most potent yet described, both in vitro and in vivo, and are the first with oral activity. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).HPLC of Formula: 142327-44-4

The Article related to nmda receptor glycine site antagonist hydroxyphenylquinolone, anticonvulsant phenylhydroxyquinolone preparation, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.HPLC of Formula: 142327-44-4

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

On December 24, 2014, Madanahalli Ranganath Rao, Jagannath; Gurram Ranga, Madhavan; Pachiyappan, Shanmugam published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of spirooxindole derivatives for use as AMPK activators. And the patent contained the following:

Title compounds I [A = bond, (un)substituted aryl, or heteroaryl; B = (un)substituted cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; C = (un)substituted aryl or heteroaryl; X = N or CR3; Y = H, OH, (un)substituted heteroaryl, etc.; Z = bond or a linking moiety; R1 and R2 independently = H or (un)substituted alkyl; R3 and R5 independently = H, halo, CN, NO2, etc.; R4 = H, F, Cl, Br, or I; R6 and R7 independently = H or (un)substituted alkyl; n = 0 to 2], and their pharmaceutically acceptable salts, are prepared and disclosed as AMPK activators. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated in AMPK biol. activity assays, e.g., II demonstrated 166% activation of beta 1 at 10 μM. The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Category: esters-buliding-blocks

The Article related to spirooxindole preparation ampk activator, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Category: esters-buliding-blocks

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

On July 2, 1998, Cameron, Kimberly O’Keefe; Ke, Hua Zhu; Lefker, Bruce Allen; Rosati, Robert Louis; Thompson, David Duane published a patent.Recommanded Product: Methyl 2-(3-formylphenyl)acetate The title of the patent was Preparation of alkylsulfonylaminocarboxylic acid as prostaglandin agonists. And the patent contained the following:

Title compounds AB(KM)QZ [I; A = acyl, alkylsulfonyl, cycloalkylsulfonyl, etc.; B = N, CH; K = electron pare, alkylene, thioalkylene, oxyalkylene, etc.; M = cyclic, heterocyclic, etc.; Q = alkylene, alkylenethioalkylene, etc.; Z = COOH, alkoxycarbonyl, tetrazolyl, oxadiazolyl, etc.], and pharmaceutically acceptable salts are prepared as prostaglandin agonists useful for the treatment of bone disorders including osteoporosis. 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 alkylsulfonylaminocarboxyli acid preparation prostaglandin agonist osteoporosis, Aliphatic Compounds: Carboxylic Acids and Peroxycarboxylic Acids and Their Sulfur-Containing Analogs and Salts and other aspects.Recommanded Product: Methyl 2-(3-formylphenyl)acetate

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

On February 22, 2000, Cameron, Kimberly O’Keefe; Lefker, Bruce Allen published a patent.Related Products of 142327-44-4 The title of the patent was Preparation of therapeutic chemicals for glaucoma treatment. And the patent contained the following:

Title compounds AB(KM)QZ [A = alkylsulfonyl, cycloalkylsulfonyl; Q = alkylene, alkylenethioalkylene, alkylenesulfonylalkylene; Z = COOH, CO2R, R = alkyl; B = N; K = alkylene, thioalkylene; M = aryl, heterocyclic], pharmaceutical acceptable salts, and delivery systems are prepared and tested as prostaglandin agonist for lowering internal pressure of mammalian eyes and for treating glaucoma. Thus, the title compound 7-[(4-butylbenzyl)methanesulfonylamino]heptanoic acid was prepared The experimental process involved the reaction of Methyl 2-(3-formylphenyl)acetate(cas: 142327-44-4).Related Products of 142327-44-4

The Article related to prostaglandin agonist preparation antiglaucoma agent, organic acid preparation glaucoma treatment, Aliphatic Compounds: Carboxylic Acids and Peroxycarboxylic Acids and Their Sulfur-Containing Analogs and Salts and other aspects.Related Products of 142327-44-4

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

On April 22, 1999, Cameron, Kimberly O’Keefe; Lefker, Bruce Allen; Rosati, Robert Louis published a patent.Electric Literature of 142327-44-4 The title of the patent was Preparation of prostaglandin agonists and their use to treat bone disorders. And the patent contained the following:

Title prostaglandin agonists GAB(KM)QZ [A is SO2, CO; G is Ar, alkylene, ArCONHalkylene, amino, oxyalkylene, etc.; B is N, CH; Q is alkylene, alkyl, alkylene-W-alkylene, alkylene-W-X-alkylene; W is oxy, thio, sulfino, sulfonyl, aminosulfonyl, etc.; X is aryl; K is a bond, alkylene, thioalkylene, alkylenethioalkylene, etc.; M is Ar, ArSar, ArSOAr, ArSO2Ar, ArOAr], prodrugs thereof and the pharmaceutically acceptable salts of said compounds and said prodrugs are prepared as well as methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists are discussed. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis. 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 arylsulfonylaminoaliphaticcaboxylic acid preparation prostaglandin agonist, arylsulfonylaminoaromaticcaboxylic acid preparation prostaglandin agonist, Aliphatic Compounds: Carboxylic Acids and Peroxycarboxylic Acids and Their Sulfur-Containing Analogs and Salts and other aspects.Electric Literature of 142327-44-4

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