Day: November 2, 2022

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

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