Day: October 26, 2022

On March 12, 2009, Demeese, Jason; Gaudino, John; Neitzel, Alicia Tarin; Lunghofer, Paul; Jeongbeob, Seo; Hongqi, Tian; Young, Wendy B.; Sutherlin, Daniel P. published a patent.HPLC of Formula: 924909-16-0 The title of the patent was Preparation of pyrazolopyridines as tyrosine kinase inhibitors. And the patent contained the following:

Title compounds[I, II; X = O, S, NR10; W = O, S, SO, SO2; R1 = H, alkyl, alkenyl, alkynyl, CONR10R11, (substituted) carbocyclyl, heterocyclyl, aryl, heteroaryl, etc.; R2 = H, CF3, cyano, NR10R11, (substituted) alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, etc.; R3 = (substituted) carbocyclyl, heterocyclyl, aryl, heteroaryl; R4 = H, F, Cl, Br, CF3, cyano, NR10R11, OR10, etc.; R10, R11 = H, (substituted) alkyl, alkenyl, alkynyl, carbocyclyl, heteroaryl, etc.], were prepared as c-MET kinase inhibitors (no data). Thus, title compound (III) was prepared in 13 steps from 2,2-dimethyl-1,3-dioxane-4,6-dione, 1-(4-methoxybenzyl)-1H-pyrazol-5-amine, 1,2-difluoro-4-nitrobenzene, 1-(4-fluorophenyl)hydrazine hydrochloride, 1,3-dioxane-4,6-dione, and tert-Bu 4-hydroxypiperidine-1-carboxylate. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).HPLC of Formula: 924909-16-0

The Article related to pyrazolopyridine preparation tyrosine kinase inhibitor, cmet kinase inhibitor piperidinyloxypyrazolopyridine preparation, cancer stroke diabetes hepatomegaly alzheimers treatment phenoxypyrazolopyridine preparation and other aspects.HPLC of Formula: 924909-16-0

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

Nicolaou, K. C.; Rhoades, Derek; Wang, Yanping; Totokotsopoulos, Sotirios; Bai, Ruoli; Hamel, Ernest published an article in 2015, the title of the article was Synthesis and Biological Evaluation of Novel Epothilone B Side Chain Analogues.Formula: C8H11BrN2O And the article contains the following content:

The design, synthesis, and biol. evaluation of a series of epothilone analogs with novel side chains equipped with an amino group are described. Their design facilitates potential conjugation to selective drug delivery systems such as antibodies. Their synthesis proceeded efficiently via Stille coupling of a readily available vinyl iodide and heterocyclic stannanes. Cytotoxicity studies and tubulin binding assays revealed two of these analogs, I (R = CF3, F), to be more potent than epothilones A-D and the anticancer agent ixabepilone, currently in clin. use. The experimental process involved the reaction of 5-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazole(cas: 1187582-58-6).Formula: C8H11BrN2O

The Article related to epothilone b side chain analog preparation antitumor structure activity, tubulin binding epothilone b side chain analog, antibody-drug conjugates, anticancer agents, epothilones, organic synthesis, tubulin binding agents and other aspects.Formula: C8H11BrN2O

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

On September 23, 2021, Lancellotti, Patrizio; Oury, Cecile; Pirotte, Bernard; Musumeci, Lucia; Jacques, Nicolas; Goffin, Eric published a patent.Product Details of 85426-79-5 The title of the patent was Preparation of pyrimidine derivatives for prevention and treatment of Gram-negative bacterial infection, contamination and fouling. And the patent contained the following:

This invention relates to new pyrimidine derivatives I [X1 and X2 = (independently) N, (un)substituted CH (with the exception that if one of X1 or X2 is N, then the remaining of X1 or X2 = (un)substituted CH); Y = O or S; R1 and R2 = (independently) alkyl, cycloalkyl, aryl, etc.; R3-R7 = (independently) H, halo, alkyl, etc.] or pharmaceutically acceptable acid addition salts, together with a membrane penetrating agent, optionally with a detectable isotope and pharmaceutical composition for use in treatment or prevention of Gram-neg. bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of Gram-neg. biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. E.g., a multi-step synthesis of (1R,2S)-II, starting from 4,6-dichloro-2-(propylthio)pyrimidin-5-amine and methylamine, was disclosed. Antibacterial effects of representative compounds I together with Polymyxin B Nonapeptide (membrane penetrating agent) on Escherichia coli were examined (data given). A method of diagnosing or prognosing a Gram-neg. bacterial infection in a host mammal comprising using the pyrimidine derivatives I together with a membrane penetrating agent, was disclosed. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Product Details of 85426-79-5

The Article related to pyrimidine derivative pyrrolopyrimidinamine phenylcyclopropyl preparation gram neg bacterial infection, antibacterial combination chemotherapy membrane penetrating agent pyrrolopyrimidinamine phenylcyclopropyl preparation and other aspects.Product Details of 85426-79-5

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

Seela, Frank; Jawalekar, Anup M.; Sun, Lijuan; Leonard, Peter published an article in 2005, the title of the article was Oligonucleotides Containing Pyrazolo[3,4-d]Pyrimidines: 8-Aza-7-deazaadenines With Bulky Substituents in the 2- or 7-Position.Product Details of 85426-79-5 And the article contains the following content:

The synthesis of the 2′-deoxyadenosine analogs, e.g. I, modified at the 7- and/or 2-position is described. The effect of 7-chloro and 2-methylthio groups on the duplex stability is evaluated. For that, the nucleosides, e.g. I, were converted to the corresponding phosphoramidites, which were employed in the solid-phase oligonucleotide synthesis. In oligonucleotide duplexes, compound I forms stable base pairs with dT, of which the separated I-dT base pairs contribute stronger than that of the consecutive base pairs. Nucleoside II shows universal base pairing properties while its N8 isomer forms duplexes with lower stability. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Product Details of 85426-79-5

The Article related to structure property thermodn thermal stability dna duplex synthesis, dna duplex synthesis thermal stability thermodn, oligonucleotide pyrazolopyrimidine azadeazaadenine synthesis dna duplex stability nucleoside phosphoramidite and other aspects.Product Details of 85426-79-5

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

On April 1, 2021, Richards, Nicole; Lewis, Richard; Hamilton, Matthew; Ray, William; Alvarez, Fernando; Pfaffinger, Dana; Reyna, Naphtali; Cross, Jason; Ramaswamy, Suyambu Kesava Vijayan; Bardenhagen, Jennifer; Lightfoot, Yaima Luzardo; Acton, Paul; Goodwani, Sunil published a patent.Reference of 5-Methoxy-1H-pyrazole The title of the patent was Preparation of 1-[(4,5-dihydro-1H-pyrazol-1-yl)carbonyl]bicyclo[1.1.1]pentane derivatives as inhibitors of receptor interacting protein kinase for the treatment of disease. And the patent contained the following:

The is invention is related to the preparation of compounds I [X = a bond, carbamoyl, carbonyl, (un)substituted alkylene; R1a, R1b = independently H, (un)substituted alkyl; or R1aNR1b= (un)substituted heterocycloalkyl or heteroaryl; R2 = H, OH, CN, halo, NH2, etc.] or salts thereof which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer. Thus, Wittig reaction between 3,5-difluorobenzaldehyde and 2-(triphenylphosphoranylidene)acetaldehyde, cyclization of (E)-3-(3,5-difluorophenyl)-2-propenal with NH2NH2 and reaction of 5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazole with 3-(methoxycarbonyl)bicyclo[1.1.1]pentane-1-carboxylic acid gave II. Exemplified compounds I were tested for their RIPK1 activity (data given for representative compounds I). The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Reference of 5-Methoxy-1H-pyrazole

The Article related to dihydropyrazolylcarbonylbicyclopentane derivative preparation receptor interacting protein kinase 1 inhibitor, ripk1 inhibitor dihydropyrazolylcarbonylbicyclopentane derivative preparation antiinflammatory anticancer neurodegenerative disorder and other aspects.Reference of 5-Methoxy-1H-pyrazole

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

Rajashakar, V.; Saisree, K.; Sikender, M.; Naveen, S.; Madhava Reddy, B.; Harinadha Babu, V. published an article in 2016, the title of the article was Synthesis of pyrazolyl thiobarbituric acids and their cytotoxic and antimicrobial evaluation.HPLC of Formula: 36640-53-6 And the article contains the following content:

Synthesis, cytotoxic and anti-microbial screening of novel thiobarbituric acid incorporated pyrazole derivatives I [Ar = Ph, 4-H3CC6H4, 4-HOC6H4, 4-ClC6H4 and 2-naphthyl] were performed. Vilsmeier-Haack reaction of different Ph hydrazones afforded pyrazole-4-carbaldehydes in good yields. Knoevenagel condensation of compounds with thiobarbituric acid gave a series of 5-ylidene derivatives I in reasonable yields. The synthesized compounds were characterized with the help of IR, 1H-NMR and mass spectral data. The compounds were tested for cytotoxic activity against Vero, MCF-7 and HCT-116 cell lines. Among the tested compounds, compound I [Ar = 4-HOC6H4] was found to be most active mol. with the activity against both MCF-7 and HCT-116 cell lines with IC50 values of 14.0 μM and 18.12 μM. In anti-microbial screening, none of the compounds exhibited anti-bacterial activity. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).HPLC of Formula: 36640-53-6

The Article related to arylethylideneamino aniline preparation vilsmeir haack reaction, aryl phenylpyrazolyl carboxaldehyde preparation thiobarbituric acid knoevenagel condensation, phenyl arylpyrazolylmethylene thioxopyrimidine dione preparation antibacterial antitumor activity sar and other aspects.HPLC of Formula: 36640-53-6

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

On March 31, 2007, Jagadhani, S. G.; Kale, S. B.; Chaudhari, C. S.; Sangle, M. D.; Randhavane, P. V.; Karale, B. K. published an article.SDS of cas: 36640-53-6 The title of the article was Knoevenagel reactions of 3-formyl chromones and 4-formyl pyrazoles with pyrazolone by conventional and non-conventional methods. And the article contained the following:

3-Formyl chromones when heated with 1,2-dihydro-1-phenyl-3-propylpyrazol-5-one (I) in presence of acetic acid afforded the compounds 4-(4-oxo-4H-chromon-3-yl)methylene-1-phenyl-3-propyl-1H-pyrazol-5-(4H)-ones. 4-Formyl pyrazoles on treatment with compound I in presence of acetic acid gave compounds (4)-1-phenyl-4-((1-phenyl-1H-pyrazol-4-yl)methylene)-3-propyl-1H-pyrazol-5-(4H)-ones. These compounds are synthesized by traditional, microwave, and ultrasonic irradiations. 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 formyl chromone condensation pyrazolone microwave ultrasonic irradiation, pyrazole formyl condensation pyrazolone microwave ultrasonic irradiation, chromonyl methylene pyrazolone preparation microwave ultrasonic irradiation, pyrazolyl methylene pyrazolone preparation and other aspects.SDS of cas: 36640-53-6

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

On April 13, 2017, Aiguade Bosch, Jose; Connolly, Stephen; Eastwood, Paul Robert; Gomez Castillo, Elena; Moreno Mollo, Immaculada Montserrat; Roberts, Richard Spurring; Sevilla Gomez, Sara published a patent.Application of 314021-93-7 The title of the patent was Preparation of bicyclic fused pyrimidinone and triazinone derivatives as new TRPA1 antagonists. And the patent contained the following:

The present invention relates to compounds of Formula I [G1 = C or N atom; G2, G3, G4, G5 = each independently C(Ra), N(Rb), or N; G6 = N, G7 = C atom, G8 = N atom, G9 = O atom; Ra = H, linear or branched C1-4 alkyl, halogen atom, linear or branched C1-4 alkoxy, linear or branched C1-4 haloalkyl, linear or branched C1-4 haloalkoxy, oxo, C3-7 cycloalkyl, cyano, amino, mono – or di(C1-4 alkyl)amino, or hydroxy; Rb = H or linear or branched C1-4 alkyl; L = (un)substituted linear or branched C2-4 alkylene, C(Rb):C(Rb), C3-7 cycloalkylene, (CH2)2-3-O, (CH2)1-2-C(O), (CH2)1-2-S, (CH2)1-2-S(O), CONH, CF2O, or 4- to 6-membered N-containing heterocyclylene, wherein at least one nitrogen atom is linked the G7 group; Q = each (un)substituted monocyclic or bicyclic C6-14 aryl or monocyclic or bicyclic 5- to 14-membered heteroaryl containing at least one heteroatom selected from N, O and S; or when Q = Ph, L together with Q form a 5- to 7-membered N-containing heterocyclyl fused to the Ph group; n = 0-1; the solid/dashed line = single or a double bond], pharmaceutically acceptable salts, solvates, N-oxides, tautomers, stereoisomers, or isotopically-labeled derivatives thereof:. These compounds are used in the treatment of a pathol. condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism. The pathol. condition or disease is selected from acute and/or chronic pruritus, acute and/or chronic pain, inflammatory dermatol. diseases, respiratory disorders, gastrointestinal inflammatory disorders, and urinary tract disorders. Thus, a suspension of 0.040 g 5-methylquinazolin-4(3H)-one and 0.069 g potassium carbonate in 1.0 mL DMF was stirred at room temperature for 10 min, followed by adding a solution of 0.071 g 5-(chloromethyl)-3-[2-(4-chlorophenyl)ethyl]-1,2,4-oxadiazole in 0. 5 mL DMF, and the resulting mixture of was stirred for 3 h to give, after workup and flash chromatog., 72% 3-[[3-[2-(4-chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-5-methylquinazolin-4(3H)-one (II). II and 3-[[3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-5-methylimidazo[5,1-f]-[1,2,4]triazin-4(3H)-one (III) inhibited the tetracycline-inducible human TRPA1 expression in CHO cells in a calcium flux assay with IC50 of 100-1,000 and <100 nM, resp. The experimental process involved the reaction of 1-Methyl-1H-pyrazolo[4,3-d]pyrimidin-7-ol(cas: 314021-93-7).Application of 314021-93-7

The Article related to fused pyrimidinone preparation trpa1 antagonist, bicyclic fused triazinone preparation trpa1 antagonist, transient receptor potential cation channel trpa trpa1 antagonist, acute chronic pruritus treatment bicyclic heterocycle, chronic acute pain treatment bicyclic heterocycle and other aspects.Application of 314021-93-7

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

On September 18, 2014, Nazare, Marc; Halland, Nis; Schmidt, Friedemann; Kleemann, Heinz-Werner; Weiss, Tilo; Saas, Joachim; Struebing, Carsten published a patent.Synthetic Route of 98138-75-1 The title of the patent was Preparation of N-[4-(azaindazol-6-yl)-phenyl]-sulfonamides as SGK1 inhibitors. And the patent contained the following:

The title compounds I [Ar = (un)substituted Ph, 5-6 membered monocyclic, aromatic, heterocyclic group which comprises 1-3 identical or different ring heteroatoms selected from the series consisting of N, O and S, and is bonded via a ring C atom; n = 0-2; X = N, CH; Z = a bond, O, S, (un)substituted NH; R1 = H, (un)substituted NH2, NHC(O)NH2, etc.; R2 = halo, alkyl, alkoxy, CN; R3 = H, alkyl, -alkyl-R (R = (un)substituted 3-12 membered, monocyclic or bicyclic, saturated, partially unsaturated or aromatic, cyclic group which comprises 0-3 identical or different ring heteroatoms selected from N, O and S)] which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism, were prepared E.g., a multi-step synthesis of II, starting from 2,5-dichlorobenzenesulfonyl chloride and 4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenylamine, was described. Exemplified compounds I were tested for serum and glucocorticoid-regulated kinase 1 (SGK-1) inhibitory activity (data given). The invention furthermore relates to processes for the preparation of compounds I, their use as pharmaceuticals, and pharmaceutical compositions comprising them. The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).Synthetic Route of 98138-75-1

The Article related to azaindazolylphenyl sulfonamide preparation sgk1 inhibitor antiinflammatory antirheumatic antiarthritic, degenerative joint disorder osteoarthritis treatment azaindazolylphenyl sulfonamide preparation, serum glucocorticoid regulated kinase sgk inhibitor azaindazolylphenyl sulfonamide preparation and other aspects.Synthetic Route of 98138-75-1

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

On December 7, 2006, Mansour, Tarek Suhayl; Venkatesan, Aranapakam Mudumbai published a patent.HPLC of Formula: 153597-59-2 The title of the patent was Bicyclic 6-alkylidene-penems as class-D β-lactamase inhibitors. And the patent contained the following:

Penems, such as I [R = H, alkali metal, C1-6 alkyl, C5-6 cycloalkyl, or substituted ester; A, B = H, heteroaryl, fused bicycles, fused tricycles, etc.], were prepared for use in pharmaceutical compositions as inhibitors of β-lactamases which are class-D enzymes that hydrolyze β-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present invention when combined with β-lactam antibiotics will provide an effective treatment against life threatening bacterial infections. Thus, (5R,6Z)-6-(7-methyl-5,6,7,8-tetrahydroimidazo[1,2-a]pyrazin-2-ylmethylene)-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid sodium salt (II) was prepared via a coupling reaction of 7-methyl-5,6,7,8-tetrahydroimidazo[1,2-a]pyrazine-2-carboxaldehyde with (5R,6S)-6-bromo-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid 4-nitrobenzyl ester. The prepared penems were assayed for microbial susceptibility against E. coli GC 2883, a class-D producing organism. 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).HPLC of Formula: 153597-59-2

The Article related to alkylidene penem derivative preparation beta lactamase inhibitor, beta lactam antibiotic alkylidene penem derivative preparation, antibacterial agent alkylidene penem derivative preparation beta lactamase inhibitor, bacterial infection treatment alkylidene penem preparation beta lactamase inhibitor and other aspects.HPLC of Formula: 153597-59-2

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