Month: November 2022

On August 11, 2016, Moussy, Alain; Benjahad, Abdellah; Pez, Didier; Sandrinelli, Franck; Martin, Jason; Picoul, Willy; Chevenier, Emmanuel published a patent.Computed Properties of 215610-30-3 The title of the patent was Preparation of phenylamino-oxazole or phenylamino-thiazole compounds with antitumor activity. And the patent contained the following:

The invention relates to compounds of formula I and pharmaceutical compositions thereof, useful to destroy, inhibit, or prevent the growth or spread of cells, especially malignant cells, into surrounding tissues implicated in a variety of human and animal diseases. I [wherein A = an optionally substituted heterocyclyl; B = aryl or heteroaryl; X = N, C-R6; R1, R2, R4, R5, and R6 independently = H, CN, CF3, etc.; R3 = H] or a pharmaceutically acceptable salt thereof, which are claimed and exemplified. Reaction of N-(5-methoxy-2-methylphenyl)acetamide with 5-[6-(1H-pyrazol-1-yl)pyridin-3-yl]-2-chlorooxazole provided example compound II in 68% yield. Candidate compounds of I were evaluated for antitumor activity in solid and hematol. tumor cells using CellTiter-Blue cell-based survival proliferation assay (data given). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Computed Properties of 215610-30-3

The Article related to phenylaminothiazole phenylaminooxazle antitumor malignancy, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Computed Properties of 215610-30-3

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

On November 13, 2003, Venkatesan, Aranapakam Mudumbai; Mansour, Tarek Suhayl; Abe, Takao; Yamamura, Itsuki; Takasaki, Tsuyoshi; Agarwal, Atul; Dos Santos, Osvaldo; Sum, Fuk-Wah; Lin, Yang-I. published a patent.Name: Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate The title of the patent was Preparation of bicyclic 6-alkylidene-penems as β-lactamase inhibitors for use against bacterial infections or diseases. And the patent contained the following:

The present invention provides bicyclic 6-alkylidene-penems (shown as I; variables defined below; e.g. II), pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. IC50 values for inhibition of β-lactamase from 4 sources are tabulated for >30 examples of I; in vitro minimal inhibitory concentrations against 9 types of bacteria are tabulated for >30 examples of I; ED50 values for protective effects of >30 examples of I (sometimes combined with piperacillin) in mice are tabulated. For I: one of A and B is H and the other is an (un)substituted fused bicyclic heteroaryl group; X is O or S; R5 is H, C1-C6 alkyl, C5-C6 cycloalkyl, or CHR3OCOC1-C6alkyl; and R3 is H, C1-C6 alkyl, C5-C6 cycloalkyl, (un)substituted aryl, or (un)substituted heteroaryl. The compounds I when combined with β-lactam antibiotics will provide an effective treatment against life threatening bacterial infections. Forty example preparations of I are included. For example, II was prepared in 5 steps (25, 91, 76, 40, 18 % yields, resp.) starting from 1-benzoyl-4-piperidone and Et mercaptoacetate and involving intermediates Et 5-benzoyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carboxylate, (5-benzyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl)methanol, 2-formyl-5-benzyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine and 4-nitrobenzyl 6-[(acetyloxy)(5-benzyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl)methyl]-6-bromo-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate. 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).Name: Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate

The Article related to bicyclic alkylidene penem beta lactamase inhibitor antibacterial, beta lactam antibiotic codrug bicyclic alkylidene penem preparation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Name: Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate

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

On December 6, 2007, Blom, Petra; Defert, Olivier; Kaletta, Titus; Leysen, Dirk Casimir Maria published a patent.Name: 5-Methoxy-1H-pyrazole The title of the patent was Preparation of thiazole and pyridinyl carboxamides and related heterocyclic analogs that interact with ion channels. And the patent contained the following:

Title compounds I [X = substituted thiazole, pyridine, oxopiperidine, etc.; R1 = H, halo, OH, NO2, alkyl, etc.; L1 = alkylene, cycloalkylene, pyrrolidinlenealkylene, etc.; m = 0-4], and their pharmaceutically acceptable salts, are prepared and disclosed as being capable of interacting with ion channels, in particular ion channels from the kv family. Thus, e.g., II was prepared by coupling of the corresponding 4-bromothiazole derivative (preparation given) with Ph boronic acid. Inhibition assays of the kv4.3 ion channel are described, e.g., II provided above 50% inhibition. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Name: 5-Methoxy-1H-pyrazole

The Article related to thiazole carboxamide derivative preparation ion channel modulator kv, pyridine carboxamide derivative preparation ion channel modulator kv, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Name: 5-Methoxy-1H-pyrazole

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

On August 21, 2019, Lancellotti, Patrizio; Oury, Cecile; Pirotte, Bernard published a patent.Safety of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine The title of the patent was Preparation of pyrimidine derivatives for use as antibacterial agents. And the patent contained the following:

Title compounds I [each X independently = N, CH, C(alkyl), etc.; Y = O or S; R1 and R2 independently = (un)substituted alkyl, alkenyl, aryl, etc.; each R3 independently = H, halo, OH, NO2, etc.; with provisions], and their pharmaceutically acceptable salts, are prepared and disclosed as antibacterial agents. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated for antibacterial effects on S. epidermidis (ATCC25904), e.g., II demonstrated a minimal inhibitory concentration of 20-25 μM. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Safety of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

The Article related to pyrimidine preparation antibacterial agent, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

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

On August 22, 2019, Lancellotti, Patrizio; Oury, Cecile; Pirotte, Bernard published a patent.Application of 85426-79-5 The title of the patent was Preparation of pyrimidine derivatives for use as antibacterial agents. And the patent contained the following:

Title compounds I [each X independently = N, CH, C(alkyl), etc.; Y = O or S; R1 and R2 independently = (un)substituted alkyl, alkenyl, aryl, etc.; each R3 independently = H, halo, OH, NO2, etc.; with provisions], and their pharmaceutically acceptable salts, are prepared and disclosed as antibacterial agents. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated for antibacterial effects on S. epidermidis (ATCC25904), e.g., II demonstrated a minimal inhibitory concentration of 20-25 μM. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Application of 85426-79-5

The Article related to pyrimidine preparation antibacterial agent, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 85426-79-5

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

On July 8, 2004, Abe, Takao; Matsunaga, Hiroshi; Mihira, Ado; Sato, Chisato; Ushirogochi, Hideki; Sato, Koichi; Takasaki, Tsuyoshi; Venkatesan, Aranapakam Mudumbai; Mansour, Tarek Suhayl published a patent.Product Details of 153597-59-2 The title of the patent was Process for preparing 6-alkylidene penem derivatives. And the patent contained the following:

The present invention provides a process of making compounds of formula I (R = H, C1-6 alkyl, C5-6 cycloalkyl, or substituted ester; A, B = H, heteroaryl, fused bicycles, fused tricycles, etc.) which are useful for the treatment of bacterial infection or disease. Thus, sodium (5R),(6Z)-6-(2,3-dihydroimidazo[2,1-b]thiazol-6-ylmethylene)penem-3-carboxylate (II) was prepared via a multistep synthetic sequence which started from 6-aminopenicillanic acid. 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).Product Details of 153597-59-2

The Article related to alkylidene penem derivative antibacterial preparation, Biomolecules and Their Synthetic Analogs: Other Bacterial and Fungal Metabolites and other aspects.Product Details of 153597-59-2

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

On February 1, 2007, Oslob, Johan D.; Yu, Chul Hyun published a patent.Reference of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol The title of the patent was Pyrazolopyrimidines useful as Aurora kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of Aurora kinase mediated diseases. And the patent contained the following:

The invention provides compounds having the formula I, which are useful as inhibitors of protein kinase (e.g., Aurora), and thus are useful, for example, for the treatment of Aurora mediated diseases. Compounds of formula I wherein dotted line is double bond as valency permits; R2 is H, halo, CN, NO2, (hetero)aliphatic, (hetero)alicyclic and (hetero)aromatic moiety; R4 is absent, H, (hetero)aliphatic, (hetero)alicyclic, and (hetero)aromatic moiety; if R4 is absent, X1 and X2 are independently NH and derivatives and CR1 proviso that only one of X1 and X2 are CR1; if R4 is present X1 and X2 are independently N and derivatives, and CR1, proviso that only one of X1 and X2 is CR1; R1 is H, halo, CN, No2, (hetero)aliphatic, etc.; L1 is 2-8 atom heteroaliph. linker; L2 is 1-6 atom heteroaliph. linker; Y is (hetero)alicyclic, and (hetero)aromatic moiety; Z is (hetero)alicyclic, (hetero)aliphatic, and (hetero)aromatic moiety; are claimed. Example compound II was prepared by amination of 4-chloro-5-methylpyrazolopyrimidine derivative with 2-[2-(3-trifluoromethylphenylurido)thiazol-2-yl]ethylamine. All the invention compounds were evaluated for their Aurora kinase inhibitory activity. The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Reference of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol

The Article related to pyrazolo pyrimidine preparation aurora kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol

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

On June 30, 2015, Kamal, Raj; Kumar, Vipan; Bhardwaj, Vikas; Kumar, Vikas; Aneja, Kamal Rai published an article.Computed Properties of 36640-53-6 The title of the article was Synthesis, characterization and in vitro antimicrobial evaluation of some novel hydrazone derivatives bearing pyrimidinyl and pyrazolyl moieties as a promising heterocycles. And the article contained the following:

In the present investigation, ten new 2-((3-aryl-1-phenyl-1H-pyrazol-4-yl)methylene)-1-(4,6-dimethylpyrimidin-2-yl)hydrazines [I; Ar = (un)substituted Ph, 2-naphthyl] having pyrimidinyl and pyrazolyl moieties were synthesized. Structures of all compounds were confirmed by their spectral and elemental data. Most of the tested compounds were found to be significantly more effective against bacterial strains Staphylococcus aureus, Bacillus subtilis and Pseudomonas aeruginosa than the reference drug ciprofloxacin. All the newly synthesized compounds were found to be more potent antifungal agents than reference drug against Candida albicans, whereas except I (Ar = 4-nitrophenyl) all other compounds also shown good activity against Saccharomyces cerevisiae. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Computed Properties of 36640-53-6

The Article related to pyrimidinyl pyrazolyl hydrazone preparation bactericide fungicide, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 36640-53-6

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

On June 25, 2020, Brenneman, Jehrod Burnett; Krall, Elsa Beyer; Schlabach, Michael; Wylie, Andrew Alistair published a patent.Recommanded Product: 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine The title of the patent was Preparation of substituted pyrazolopyrimidines and substituted purines and their use as ubiquitin-specific-processing protease 1 (USP1) inhibitors. And the patent contained the following:

The present disclosure provides compounds having formula I and the pharmaceutically acceptable salts and solvates thereof, wherein X1, X2 is independently N and CR2; R1 and R2 are independently H, halo, cyano, (un)substituted alkyl, etc.; R3 is (un)substituted Ph, pyridinyl, pyrazolyl, etc.; X11 and X12 is independently N and CH; R5′ is H, (un)substituted C1-6alkyl, (un)substituted C1-6alkoxy, etc.; R5 is (un)substituted C1-6alkyl, (un)substituted C2-6alkenyl, C1-6haloalkyl, etc.; R6 and R7 is independently H, halo, CN, (un)substituted alkenyl, etc. The present disclosure is also directed to the use of compounds of Formula I to inhibit a USP1 protein and to treat a disorder responsive to the inhibition of USP1 proteins and USP1 activity. Example compound II was prepared via a multistep procedure (procedure given). From the assay, it was determined that example compound II exhibited IC50 value of > 200 nM towards USP1. The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).Recommanded Product: 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine

The Article related to pyrazolopyrimidines purine preparation usp1 inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine

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

On August 18, 2016, Gray, Nathanael S.; Hatcher, John; Choi, Hwan Geun published a patent.Name: 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine The title of the patent was LRRK2 inhibitors and methods of making and using the same. And the patent contained the following:

The invention relates to compounds of formula I, II, and III as LRRK2 inhibitors; their preparation and use in the treatment of neurodegenerative diseases, such as Parkinson’s disease. Compounds of formula I wherein Rx is NRARB, substituted piperidinylmethanone, substituted morpholinomethanone, etc.; RA and RB are independently (un)substituted C1-6 alkyl and COR7; R7 is (un)substituted C1-6 alkyl, (un)substituted C2-6 alkenyl, (un)substituted C2-6 alkynyl; X1, X2 and X3 are independently N, NH and derivatives, substituted C; Rn is H and (un)substituted C1-6 alkyl; each R1 is independently (un)substituted C1-6 alkyl, (un)substituted C1-6 alkoxy and halo; m = 0 – 3; R2 is H, alkoxy, halo, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound IV was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their LRRK2 inhibitory activity (some data given). The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).Name: 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine

The Article related to pyrrolopyrimidine preparation lrrk2 inhibitor treatment neurodegenerative disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine

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