Day: October 26, 2022

On April 3, 2014, Eskildsen, Joergen published a patent.Recommanded Product: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Preparation of indolylalkylamide derivatives for use as positive allosteric modulators of nicotinic acetylcholine receptor. And the patent contained the following:

Title compounds I [R1, R2, R4, and R5 independently = H, F, CN, (un)substituted alkyl, alkenyl, or alkynyl; R3 = H, CN, (un)substituted alkyl, alkenyl, or alkynyl; R6 = H or Me; Q = substituted isoxazolyl, isothiazolyl, or pyrazolyl], and their pharmaceutically acceptable salts, are prepared and disclosed as pos. allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor. Thus, e.g., II was prepared by a multistep procedure (preparation given). I were evaluated in α7 NNR receptor PAM flux activity assays, e.g., II demonstrated an EC50 value of 2200 nM. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Recommanded Product: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

The Article related to indolylalkylamide preparation pos allosteric modulators nicotinic acetylcholine receptor, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

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

On August 7, 2014, Okura, Hironari; Kitajima, Kazuki; Kawahara, Atsuko; Wakita, Takeo; Kawase, Ayumi; Nomura, Michikazu published a patent.Electric Literature of 1014631-89-0 The title of the patent was Preparation of heterocyclic compounds as pest control agents. And the patent contained the following:

Disclosed are compounds I [G1 = nitrogen, carbon atom or CH; R1 = H, halo, cyano, etc.; m = 1-3; n = 0 or 1; Hy = 5- or 6-membered aromatic ring represented by Q1 (*2 is connection position to G2); A1 = carbon or nitrogen atom; A2 = carbon or sulfur atom; A3 = carbon or nitrogen atom; A4 = carbon or nitrogen atom; with a proviso that A1 and A2 cannot be carbon atom simultaneously; p = 0-2; q = 0 or 1; R2 = H, halo, alkyl, etc.; G2 = Q2 (*1 is connection position to Hy); Q = oxygen atom or NR5; R5 = H, alkyl, cycloalkyl, etc.; R3 = H, alkyl, cycloalkyl, etc.; R4 = alkyl, cycloalkyl, alkenyl, etc.; or salts thereof]. For example, compound II was prepared via reaction of thionicotinamide with chloroacetylacetone, condensation reaction with NH2OH and carbamoylation with ethylisocyanate. The invention compounds, e.g., II, showed ≥70% pesticidal activities for Laodelphax striatellus and Myzus persicae. The experimental process involved the reaction of 1-(Pyridin-3-yl)-1H-pyrazole-4-carboxylic acid(cas: 1014631-89-0).Electric Literature of 1014631-89-0

The Article related to heterocycle preparation pest control agent, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 1014631-89-0

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

On January 17, 2019, Hoffman, Thomas James; Stierli, Daniel; Pitterna, Thomas; Rajan, Ramya published a patent.Application of 215610-30-3 The title of the patent was Preparation of oxadiazole derivatives as microbicides. And the patent contained the following:

Compounds of the formula I useful as pesticides, especially as fungicides. Compounds of formula I wherein Z is substituted pyrazolyl; R1, R2, R3 and R4 are independently H and F, provided that 0 – 2 of R1 – R4 are F; R5 and R6 are independently H and Me; and salts and N-oxides thereof, are claimed. Example compound II was prepared by amidation of 1-[[4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]pyrazole-4-carboxylic acid with N-cyclopropylethylamine. The invention compounds were evaluated for their fungicidal activity (data given). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Application of 215610-30-3

The Article related to oxadiazole preparation fungicide microbicide, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Application of 215610-30-3

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

On September 6, 2019, Tang, Haifeng; Boyce, Sarah; Hanson, Michael; Nie, Zhe published a patent.Name: 5-Methoxy-1H-pyrazole The title of the patent was Compounds and compositions for treating conditions associated with APJ receptor activity. And the patent contained the following:

The invention relates to substituted triazoles of formula I and pharmaceutically acceptable salts thereof (wherein R1 is (Y1)0-1Y2; Y1 is (un)substituted C1-6 alkylene; Y2 is (un)substituted C3-10 cycloalkyl, (un)substituted C6-10 aryl, (un)substituted heteroaryl, etc.; R2 is (un)substituted C6-10 aryl, (un)substituted heteroaryl; R3 is (Y3)0-1Y4; Y3 is (un)substituted C1-6 alkylene; Y4 is (un)substituted C3-6 cycloalkyl, (un)substituted C6-10 aryl, (un)substituted 5- to 10-membered heteroaryl; R4 is H and C1-3 alkyl;) as apelin receptor modulators; their preparation and use in the treatment of pulmonary arterial hypertension. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their APJ modulatory activities. From the assay, it was determined that compound II exhibited EC50 value of less than 1 nM. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Name: 5-Methoxy-1H-pyrazole

The Article related to triazole preparation apj receptor modulator treatment pulmonary arterial hypertension, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Name: 5-Methoxy-1H-pyrazole

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

Kamal, Raj; Kumar, Vipan; Kumar, Ravinder; Kumar, Vikas; Sharma, Prabodh C.; Bansal, Kushal K. published an article in 2019, the title of the article was Chloramine-T Mediated Facile One Pot Synthesis of Pyrazolyltriazolobenzothiazole Hybrids as Potent Anti-Infective Agents.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde And the article contains the following content:

An expedient and facile one pot synthesis of 3-(3-aryl-1-phenyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[3,4-b]-1,3-benzothiazole derivatives I (R = 4-methoxyphenyl, 3-nitrophenyl, 2-naphthyl, etc.) through in situ oxidative cyclization of corresponding N-heteroarylhydrazone promoted by environmentally benign chloramines-T trihydrate at room temperature has been accomplished. All synthesized pyrazolyltriazolobenzothiazole hybrids I were also evaluated for their antibacterial and anthelmintic potentials and found to be moderate to significant anti-infective agents. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to pyrazolyl triazolobenzothiazole preparation green chem antibacterial anthelmintic activity, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Reference of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

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

Vlasenko, Yulia A.; Kuczmera, Thomas J.; Antonkin, Nikita S.; Postnikov, Pavel S.; Nachtsheim, Boris J. published an article in 2022, the title of the article was Site selective nucleophilic aromatic substitutions of azole-ligated diaryliodonium salts.SDS of cas: 57446-04-5 And the article contains the following content:

Herein the application of azole-stabilized diaryliodonium salts with addnl. thiophen-2-yl-ligands as substrates for metal-free nucleophilic arylations was presented. Besides their synthesis, their application in chemoselective nitrations, oxygenations, aminations as well as thiolations under umpolung conditions was demonstrated. Convenient one-pot procedures that are based on their in situ formation are also discussed. The experimental process involved the reaction of Methyl 3-(2-nitrophenyl)-1H-pyrazole-5-carboxylate(cas: 57446-04-5).SDS of cas: 57446-04-5

The Article related to diaryliodonium triflate regioselective nucleophilic aromatic nitration reaction, nitro biaryle preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.SDS of cas: 57446-04-5

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

On March 17, 2022, Yang, Shengyong; Li, Linli published a patent.Electric Literature of 1187582-58-6 The title of the patent was Preparation of 5-substituted indole-3-amide derivatives for disease treatments targeting RIPK1. And the patent contained the following:

Provided are a 5-substituted indole 3-amide derivative, a preparation method and a use thereof, belonging to the field of medicine. A compound represented by formula I [wherein X1 and X3 = independently N or (un)substituted CH; X2 = (un)substituted NH or CH=CH; R2B = -R2-B; R2 = (un)substituted alkylene,; B = (un)substituted aryl, cycloalkyl, heteroaryl, etc.; R3 = H or (un)substituted alkyl; R4 and R5 = independently H, alkyl, CN, OH, CO2H, etc.; A = (un)substituted aryl or heteroaryl] or a pharmaceutically acceptable salt thereof is provided. For example, II was prepared in a multi-step synthesis. This type of compound can significantly inhibit the activity of RIPK1 kinase, has high selectivity and excellent safety, serves as a RIPK1 kinase inhibitor, and can be used as a potential therapeutic drug for inflammation, immune diseases, tumors and neurodegenerative diseases. TNFα-induced SIRS model experiments proved that the compound can inhibit a RIPK1 kinase in vivo. Pharmacokinetic results showed that this series of compounds has excellent pharmacokinetic properties, thus providing a novel strategy and means for disease treatments targeting RIPK1. The experimental process involved the reaction of 5-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazole(cas: 1187582-58-6).Electric Literature of 1187582-58-6

The Article related to preparation indole amide disease treatment ripk1 human, inflammation immune tumor neurodegenerative disease, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 1187582-58-6

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

On March 29, 2012, Bartolozzi, Alessandra; Bosanac, Todd; Chen, Zhidong; De Lombaert, Stephane; Huber, John D.; Liu, Weimin; Lo, Ho Yin; Loke, Pui Leng; Riether, Doris; Tye, Heather; Wu, Lifen; Zindell, Renee M. published a patent.Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid The title of the patent was Preparation of oxadiazole inhibitors of leukotriene production. And the patent contained the following:

The title compounds I [R1, R2 = H, alkyl, carboxyxlice (with the proviso that both R1 and R2 are not hydrogen); R3 = (un)substituted 5-11 membered heteroaryl ring containing 1-3 heteroatoms selected from N, O and S; R4 = H, halo, alkyl, nitrile; R5 = (un)substituted alkyl, C3-10 carbocycle, 5-11 membered heterocycle, etc.], useful in treating a leukotriene-mediated disorders, were prepared Thus, reacting compound II (preparation given) with the pyrimidine derivative III afforded the title compound IV. Biol. testing showed that compounds I are effective inhibitors of 5-lipoxygenase activating protein (FLAP) and thus inhibit leukotriene production (IC50 values were given). The invention also relates to pharmaceutical compositions comprising compounds I, methods of I in the treatment of various diseases and disorders, processes for preparing I and intermediates useful in these processes. The experimental process involved the reaction of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid(cas: 1340372-11-3).Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

The Article related to oxadiazole preparation leukotriene production ltb4 inhibitor, lipoxygenase activating protein flap inhibitor oxadiazole preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Quality Control of 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid

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

On August 29, 2019, Walters, W. Patrick; Lescarbeau, Andre; Kelley, Elizabeth H.; Shortsleeves, Kelley C.; Taylor, Alexander M.; Pierce, Levi Charles Thomas; Murcko, Mark Andrew; Giordanetto, Fabrizio; Greisman, Jack Benjamin; Maragakis, Paul; Bhat, Sathesh; Konze, Kyle; Dahlgren, Markus Kristofer; Therrien, Eric published a patent.Quality Control of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine The title of the patent was Preparation of heterocyclic compounds as SHP2 phosphatase inhibitors. And the patent contained the following:

The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure. Example compound I•formate was prepared by cyclocondensation of tert-Bu (1-(5-amino-1,3,4-thiadiazol-2-yl)-3-methylpiperidin-3-yl)carbamate with 2,3-dichlorobenzaldehyde and 2-isocyano-2,4,4-trimethylpentane followed by deprotection. The invention compounds were evaluated for their SHP2 phosphatase inhibitory activity. From the assay, it was determined that compound I•formate exhibited IC50 value less than 5 μM. The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).Quality Control of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine

The Article related to heterocycle preparation shp2 phosphatase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Quality Control of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine

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

On September 26, 2019, Xie, Yinong; Babiss, Lee E. published a patent.Category: pyrazoles-derivatives The title of the patent was Preparation of SHP2 inhibitors and uses thereof. And the patent contained the following:

The invention relates to compounds of formula I and their preparation, useful as inhibitors of protein tyrosine phosphatase SHP2 in the treatment of diseases such as cancer. Compounds of formula I are claimed, in which ring A is (un)substituted aryl, heteroaryl, and bicyclic ring system; X is S, O, NRa, CHRa, S(O), SO2, C(O), or bond; Ra is H and C1-6 hydrocarbyl; ring B is (un)substituted mono-, bi-, tri-, or tetracyclic heterocyclic ring system containing heteroaryl and at least two ring N atoms; and pharmaceutically acceptable salts thereof. Example compound II was prepared via a multistep process with key step of coupling tert-Bu ((1-(5-chloro-4-cyano-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)-4-methylpiperidin-4-yl)methyl)carbamate with 2,3-dichlorophenylboronic acid followed by deprotection. Invention compounds were evaluated for their SHP2 inhibitory activity (data given). The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).Category: pyrazoles-derivatives

The Article related to shp2 inhibition treatment cancer, heteroaromatic preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: pyrazoles-derivatives

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