Month: November 2022

On October 15, 2015, Aguilar Izquierdo, Nuria; Buil Albero, Maria Antonia; Connolly, Stephen; Eastwood, Paul Robert; Roberts, Richard Spurring; Sevilla Gomez, Sara; Vidal Juan, Bernat published a patent.Product Details of 314021-93-7 The title of the patent was TRPA1 channel antagonists as therapeutic agents. And the patent contained the following:

The invention relates to compounds I, [G1= CH, N; G2= C(Ra), N; G3= C, N; G4= C, N; G5= C(Rb), N(Rc), N, O, S; G6= C(Rb), N(Rc), N, O, S; G7= C(Rb), N(Rc), N, O, S; Q= monocyclic or bicyclic C6-C14 aryl, monocyclic or bicyclic 5-14 membered heteroaryl ring, halogen, etc.; R1= H, halogen, C1-C4 alkyl, C1-C4 haloalkyl, C6-C14 aryl, CH2Ph; R2= H, halogen, C1-C4 alkyl, C1-C4 haloalkyl, C6-C14 aryl, CH2Ph; R3= H, F; R4= H, F; Ra= H, C1-C4 alkyl, halogen, C1-C4 alkoxy, etc., Rb= H, C1-C4 alkyl, halogen, C1-C4 alkoxy, etc., Rc= H, C1-C4 alkyl, C1-C4 haloalkyl, C3-C7 cycloalkyl], and the preparation and use for the treatment of a pathol. condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism. The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Product Details of 314021-93-7

The Article related to trpa1 channel antagonist preparation, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Product Details of 314021-93-7

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On June 25, 2009, Goldfarb, David Scott published a patent.Computed Properties of 314021-93-7 The title of the patent was Method using lifespan-altering compounds for altering the lifespan of eukaryotic organisms, and screening for such compounds. And the patent contained the following:

The invention discloses a method for altering the lifespan of a eukaryotic organism. The method comprises the steps of providing a lifespan-altering compound, and administering an effective amount of the compound to a eukaryotic organism, such that the lifespan of the organism is altered. In one embodiment, the compound is identified using the DeaD assay. The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Computed Properties of 314021-93-7

The Article related to lifespan alteration compound screening dead assay, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Computed Properties of 314021-93-7

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On May 15, 2019, Sun, Liangpeng; Wang, Peipei; Xu, Lili; Gao, Lixin; Li, Jia; Piao, Huri published an article.SDS of cas: 36640-53-6 The title of the article was Discovery of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups as potential PTP1B inhibitors. And the article contained the following:

Two series of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups were identified as competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors. Among the compounds studied, IIIv was found to have the best in vitro inhibition activity against PTP1B (IC50 = 0.67 ± 0.09 μM) and the best selectivity (9-fold) between PTP1B and T-cell protein tyrosine phosphatase (TCPTP). Mol. docking studies demonstrated that compounds IIIm, IIIv and IVg could occupy simultaneously at both the catalytic site and the adjacent pTyr binding site. These results provide novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).SDS of cas: 36640-53-6

The Article related to inhibition activity ptp1b inhibitor sar mol docking, 1,3-diphenyl-1h-pyrazole, ptp1b inhibitor, rhodanine-3-alkanoic acid, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.SDS of cas: 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On March 31, 2022, Lanier, Marion; Boehm, Marcus; Huang, Liming; Martinborough, Esther; Sainz, Marcos; Selfridge, Brandon; Yeager, Adam published a patent.Computed Properties of 1014631-89-0 The title of the patent was Preparation of modulators of MAS-related G-protein receptor X2 and related products and methods. And the patent contained the following:

Methods are provided for modulating MRGPR X2 generally, or for treating a MRGPR X2 or a MRGPR X2 ortholog dependent condition, more specifically, by contacting the MRGPR X2 or the MRGPR X2 ortholog by administering to a subject in need thereof, resp., an effective amount of a compound of formula I and pharmaceutically acceptable salts, isomers, hydrates, solvates and isotopes thereof. Compounds of formula I, wherein R1 is cycloalkyl, aryl, heterocyclyl;, R2, R3, R4, R5, R6 are independently H, aryl, cycloalkyl, heteroaryl, heterocyclyl, etc.; each Rx is independently H, aryl, CN, etc.; W is N and CR7 and Z is N and CR8; R7 and R8 are independently H, aryl, cycloalkyl, heteroaryl, etc.; and pharmaceutically acceptable salts, isomers, hydrates, solvates and isotopes thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their MRGPR X2 modulatory activity (some data given). The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Computed Properties of 1014631-89-0

The Article related to quinoline preparation mrgpr2 x2 modulator, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Computed Properties of 1014631-89-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On April 28, 2022, Lanier, Marion; Boehm, Marcus; Huang, Liming; Martinborough, Esther; Sainz, Marcos; Selfridge, Brandon; Yeager, Adam published a patent.Application of 1014631-89-0 The title of the patent was Modulators of mas-related g-protein receptor x2 and related products and their use. And the patent contained the following:

Methods are provided for modulating MRGPRX2 or a MRGPRX2 ortholog generally, or for treating a MRGPRX2 or a MRGPRX2 ortholog dependent condition more specifically, by contacting the MRGPRX2 or the MRGPRX2 ortholog by administering to a subject in need thereof, resp., an effective amount of a compound having structure I: or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Application of 1014631-89-0

The Article related to mrgppx2 modulator preparation treatment disease, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 1014631-89-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On April 14, 2014, Vignaroli, Giulia; Mencarelli, Martina; Sementa, Deborah; Crespan, Emmanuele; Kissova, Miroslava; Maga, Giovanni; Schenone, Silvia; Radi, Marco; Botta, Maurizio published an article.Name: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine The title of the article was Exploring the Chemical Space around the Privileged Pyrazolo[3,4-d]pyrimidine Scaffold: Toward Novel Allosteric Inhibitors of T315I-Mutated Abl. And the article contained the following:

A library of pyrazolo[3,4-d]pyrimidines, endowed with a high level of mol. diversity, has been developed applying a synthetic sequence that allowed C3, N1, C4, and C6 substitution. The enzymic screening of this “privileged scaffold”-based compound collection, validated the use of a diversity-oriented approach in a field characteristically explored by target-oriented synthesis. In fact, several compounds showed high activity against the selected kinases (i.e., Src, Abl wt, and T315I mutated-form), furthermore and interestingly a new compound has emerged as an allosteric inhibitor of the T315I mutated-form of Abl, opening up new opportunities for the development of a novel class of noncompetitive inhibitors of Abl (T315I). The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Name: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

The Article related to diversity oriented synthesis library pyrazolopyrimidine inhibitor src abl kinase, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Name: 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On March 10, 2016, Bergman, Ylva Elisabet; Foitzik, Richard Charles; Morrow, Benjamin Joseph; Camerino, Michelle Ang; Walker, Scott Raymond; Lagiakos, H. Rachel; Feutrill, John; Stevenson, Graeme Irvine; Stupple, Paul Anthony published a patent.SDS of cas: 1014631-89-0 The title of the patent was Preparation of tetrahydroisoquinoline derivatives as PRMT5 inhibitors. And the patent contained the following:

The invention relates to tetrahydroisoquinoline derivatives of formula I as PRMT5-inhibitors; their preparation and use in the treatment of cancer and hemoglobinopathy. Compounds of formula I, wherein n = 1 and 2; p is 0 and 1; R1 is halo and Me; R2a and R2b are independently F, H, Me and CH2OH; R2c and R2n are independently F, H, Me and CH2OH; R3a and R3b are independently H and Me; R4 is H and Me; R5 is H and Me; R6a and R6b are independently H and Me; A is (un)substituted Ph, (un)substituted naphthyl; and (un)substituted C5-12 heteroaryl, are claimed. Example compound II was prepared by amidation of 2-fluoro-4-(morpholine-4-carbonyl)benzoic acid with tert-Bu (S)-3-((R)-2-amino-1-hydroxyethyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate followed by BOC-deprotection. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that example II exhibited IC50 value of 0.383 μM. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).SDS of cas: 1014631-89-0

The Article related to tetrahydroisoquinoline preparation prmt5 inhibitor treatment cancer hemoglobinopathy, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.SDS of cas: 1014631-89-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On March 10, 2016, Bergman, Ylva Elisabet; Lessene, Romina; Ganame, Danny; Foitzik, Richard Charles; Morrow, Benjamin Joseph; Camerino, Michelle Ang; Walker, Scott Raymond; Lagiakos, H. Rachel; Feutrill, John; Stupple, Paul Anthony published a patent.Application of 1014631-89-0 The title of the patent was Preparation of aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5 inhibitors. And the patent contained the following:

The invention relates to compounds of formula I, II and III as PRMT5-inhibitors; their preparation and use in the treatment of cancer and hemoglobinopathy. Compounds of formula I, II and III wherein n = 1 and 2; R is H and Me; R1 is halo and Me; R2a and R2b are independently F, H, Me and CH2OH; R2c and R2n are independently F, H, Me and CH2OH; R3a and R3b are independently H and Me; R4a is OH, NH2, CONH2 and CH2OH; R4b is H and Me; R5 is H and Me; A is (un)substituted Ph, (un)substituted naphthyl; and (un)substituted C5-12 heteroaryl, are claimed. Example compound IV was prepared by acylation of 1-amino-3-((2,3-dihydro-1H-inden-2-yl)amino)propan-2-ol with 4-chlorobenzoic acid. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that example IV exhibited IC50 value of 0.792 μM. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Application of 1014631-89-0

The Article related to aminoindane aminotetrahydronaphthalene aminobenzocyclobutane preparation prmt5 inhibitor treatment cancer hemoglobinopathy, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 1014631-89-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On July 27, 2006, Venkatesan, Aranapakam M.; Agarwal, Atul; Abe, Takao; Ushirogochi, Hideki; Yamamura, Itsuka; Ado, Mihira; Tsuyoshi, Takasaki; Dos Santos, Osvaldo; Gu, Yansong; Sum, Fuk-Wah; Li, Zhong; Francisco, Gerry; Lin, Yang-I.; Petersen, Peter J.; Yang, Youjun; Kumagai, Toshio; Weiss, William J.; Shlaes, David M.; Knox, James R.; Mansour, Tarek S. published an article.COA of Formula: C9H12N2O3 The title of the article was Structure-Activity Relationship of 6-Methylidene Penems Bearing 6,5 Bicyclic Heterocycles as Broad-Spectrum β-Lactamase Inhibitors: Evidence for 1,4-Thiazepine Intermediates with C7 R Stereochemistry by Computational Methods. And the article contained the following:

The design and synthesis of a series of 6-methylidene penems containing [6,5]-fused bicycles (thiophene, imidazole, or pyrazle-fused system) as novel class A, B, and C β-lactamase inhibitors is described. These penems proved to be potent inhibitors of the TEM-1 (class A) and AmpC (class C) β-lactamases and less so against the class B metallo-β-lactamase CcrA. Their in vitro and in vivo activities in combination with piperacillin are discussed. On the basis of the crystallog. structures of a serine-bound reaction intermediate of imidazo[2,1-c]oxazine I with SHV-1 (class A) and GC1 (class C) enzymes, compounds II (R = Q, Q1, Q2, etc.) were designed and synthesized. Penems are proposed to form a seven-membered 1,4 thiazepine ring in both class A and C β-lactamases. The interaction energy calculation for the enzyme-bound intermediates favor the formation of the C7 R enantiomer over the S enantiomer of the 1,4-thiazepine in both β-lactamases, which is consistent with those obtained from the crystal structure of I with SHV-1 and GC1. The experimental process involved the reaction of Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate(cas: 153597-59-2).COA of Formula: C9H12N2O3

The Article related to methylidene penem preparation beta lactamase inhibitor structure activity, bactericide methylidene penem structure activity, Biomolecules and Their Synthetic Analogs: Beta-Lactam Fungal Metabolites and other aspects.COA of Formula: C9H12N2O3

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On October 20, 2011, Bretschneider, Thomas; Koehler, Adeline; Fischer, Reiner; Fuesslein, Martin; Jescke, Peter; Kluth, Joachim; Muehlthau, Friedrich August; Voerste, Arnd; Malsam, Olga; Goergens, Ulrich; Sato, Yoshitaka published a patent.Recommanded Product: 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Preparation of novel heterocyclic compounds as pest control agents. And the patent contained the following:

The invention relates to amides and thioamides of formula I, to a method for the producing same, and to the use thereof for treating animal pests. Compounds of formula I wherein A1 and A2 are independently H, halo, CN, NO2, alkyl, cycloalkyl and alkoxy; G1 is N and CA1; G2 is substituted thiazolyl, thiadiazolyl, and pyrazolyl; are claimed. Example compound II was prepared by reduction of 3-(4-methyl-5-nitrothiazol)pyridine; the resulting 4-methyl-2-(pyridin-3-yl)thiazol-5-amine underwent acylation with 3,3,3-trifluoropropanoyl chloride to give compound II. All the invention compounds were evaluated for their pesticidal activity (data given). The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Recommanded Product: 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid

The Article related to heterocycle preparation pesticide, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Recommanded Product: 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics