Tag: 200-300

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 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 April 20, 2017, Nicolaou, Kyriacos C.; Rhoades, Derek; Wang, Yanping; Totokotsopoulos, Sotirios published a patent.Category: pyrazoles-derivatives The title of the patent was Methods of synthesis, methods of treatment with, and drug conjugates of epothilone analogs. And the patent contained the following:

In one aspect, the present disclosure provides epothilone analogs I [wherein: X1 is absent, O or NRa; Ra is H, C≤8-alkyl, C≤8-cycloalkyl,(C≤6-alkyldiyl)-(C≤8-cycloalkyl), or a substituted version of either of these groups; provided that when X1 is absent, that the atoms to which it is attached are a part of a double bond;]. [X2, X3 and X4 are each independently O or NRb; wherein, Rb is H or C≤8-alkyl, C≤8-cycloalkyl, (C≤6-alkanediyl)-(C≤8-cycloalkyl), C≤b-aralkyl, or a substituted version of either of these groups;]. [Y1 and Y2 are each independently NH2, OH, or C≤8-alkoxy, C≤8-aralkoxy, C≤8-acyloxy, (C≤8-alkyl)amino, di(C≤8-alkyl)amino, C≤8-amido, or a substituted version of any of these groups, or ORc, wherein Rc is a hydroxy protecting group;]. [R1, R3, R4, R5, R6 and R7 are each independently H or C≤12-alkyl, C≤12-cycloalkyl, C≤12-alkenyl, C≤12-alkynyl, C≤12-aryl, or a substituted version of any of these groups; and,]. [R2 is C≤12-heteroaryl, C≤8-heteroarenediyl-Rd, or a substituted version of either of these groups; wherein Rd is C≤12-alkyl, C≤12-aryl, C≤12-aralkyl, C≤12-heteroaryl, C≤12-heteroaralkyl, or a substituted version of either of these groups;]. [Provided that R2 is not 2-methylthiazolyl, 2-(hydroxymethyl)thiazolyl, N-2-methyl-3- (methylthio)pyrazolyl or 2-(methylthio)thiazolyl;], or a pharmaceutically acceptable salt thereof. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Addnl., drug conjugates with cell targeting moieties of the compounds are also provided. Thus, epothilone B pyrazole analog II was prepared and tested for pharmacol. activity [EC50 = 19 μM for induction of tubulin assembly; GI50 = 14 nM vs. MCF-7 cell line; GI50 = 38 nM vs. OVCAR-8 cell line]. The experimental process involved the reaction of 5-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazole(cas: 1187582-58-6).Category: pyrazoles-derivatives

The Article related to epothilone analogs preparation antitumor, antibody epothilone analog conjugate preparation cancer cell targeting, Biomolecules and Their Synthetic Analogs: Other Bacterial and Fungal Metabolites and other aspects.Category: pyrazoles-derivatives

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 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 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

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

On October 14, 2013, Jung, Chan Seong; Kim, Dong Jin; Park, Gi Deok; Kim, Yun Gyeong; Pyo, Jeong In; Kim, Hyeon Tae; Hwang, On Yu; Azam, Sharif Mohammed Shafioul; Song, Chi Man; Kim, Yeong Su published a patent.Application of 85426-79-5 The title of the patent was Preparation of pyrazolopyrimidine derivatives for inhibiting nitric oxide generation. And the patent contained the following:

Disclosed are pyrazolopyrimidine derivatives, e.g., I [R1 = H, (un)substituted alkyl, (un)substituted aryl, etc.; R2 = H, halo, (un)substituted alkoxy, etc.; X1 = H, halo or (un)substituted aryl; or pharmaceutically acceptable salts thereof]. For example, compound II was prepared by following general procedure: reaction of 4-chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine with an amine (1.1 equiv) [dioxane, reflux temperature, 8 h]. Compound II [NR2 = piperidn-1-ylethylamino] showed 102±6% inhibition at 20 μM for NO generation. Title compounds are claimed useful for the treatment of Parkinson disease, Alzheimer disease, Hungtinton disease, etc. 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 pyrazolopyrimidine preparation nitric oxide generation inhibition, cerebral nerve disease treatment pyrazolopyrimidine nitric oxide generation inhibition, 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 October 15, 2009, Chen, Bei; Jiang, Tao; Marsilje, Thomas H.; Michellys, Pierre-Yves; Nguyen, Truc Ngoc; Pei, Wei; Wu, Baogen; Gao, Zhaobo; Ge, Yonghui; Huang, Chen; Li, Yuncheng published a patent.Computed Properties of 85426-79-5 The title of the patent was Preparation of pyrimidine derivatives as protein kinase inhibitors for treating proliferative disorders, immune disorders, and infections. And the patent contained the following:

The invention relates to pyrimidine derivatives having Formula I or II (wherein R1 and R2 are H, C1-6 alkyl or halo-substituted C1-6 alkyl; R3 is halo, C1-6 alkyl, or a halo-substituted C1-6 alkyl; R4 is H; alternatively, R3 and R4 together form part of a ring; R5, R6 and R8 are independently C1-6 alkyl, C1-6 alkoxy, C2-6 alkenyl or C2-6 alkynyl, each optionally substituted; R7 is sulfamoyl, carbamoyl, etc.; R9 is -L-S(O)2R18, -L-S(O)2NRR17, etc.; R is H or C1-6alkyl; R17 and R18 are independently C1-6 alkyl, halo-substituted C1-6 alkyl, etc.; L is (CR2)1-4 or a bond; n = 1-2) and methods for using such compounds as kinase inhibitors for disease treatment. For example, the compounds of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-IR), and/or insulin receptor (InsR) kinase activity or a combination thereof. Synthetic procedures for preparing the pyrimidines of the invention are claimed as are compositions containing them. Example compound III, prepared in a multistep synthesis that culminated in the reaction of corresponding pipieridine intermediate with dimethylamino acetyl halide, had an IC50 of 0.026 μM in an ALK assay. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Computed Properties of 85426-79-5

The Article related to preparation pyrimidine derivative therapeutic kinase inhibitor, pyrimidine derivative treatment proliferative disorder immune disorder infection, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 85426-79-5

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

On January 7, 2016, Chen, Wei; Wang, Longcheng; Yan, Shunqi; Loury, David J.; Jia, Zhaozhong J.; Frye, Leah Lynn; Greenwood, Jeremy Robert; Shelley, Mee Yoo; Atallah, Gordana Babic; Zanaletti, Riccardo; Catalani, Maria Pia; Raveglia, Luca Francesco published a patent.Recommanded Product: 924909-16-0 The title of the patent was Preparation of substituted pyrazolopyridines as inhibitors of Bruton’s tyrosine kinase. And the patent contained the following:

The title compounds I [one of W1 and W2 = C(R9), or N; and the other C(R9); Z = C(R9) or N; L1 = N(R5), O, S or alkyl; T1 = O, N(R5), S, alkylene, or a single bond; Cy1 = substituted aryl or heteroaryl; Cy2 = (un)substituted heterocycloalkyl, aryl, cycloalkyl, or heteroaryl; R1 = H, halo, alkyl, etc; R5 = H, alkyl, heteroalkyl; or when each of L1 and T1 = (independently) N(R5), then the two R5 may join together to form (un)substituted heterocycle; each R9 = (independently) H, halo, CN, etc.] that inhibit Bruton’s tyrosine kinase (Btk), were prepared and formulated. E.g., a multi-step synthesis of 3-hydrazinylpropanenitrile, was described. The Btk IC50 of compounds I was determined in both a cellular kinase assay and in a cellular functional assay of BCR-induced calcium flux (data given). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds I. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Recommanded Product: 924909-16-0

The Article related to pyrazolopyridine preparation bruton’s tyrosine kinase btk inhibitor antitumor antiinflammatory, lymphoma autoimmune heteroimmune disease treatment pyrazolopyridine preparation btk inhibitor and other aspects.Recommanded Product: 924909-16-0

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