Month: November 2022

On September 13, 2007, Blake, James F.; Boyd, Steven Armen; Cohen, Frederick; De Meese, Jason; Fong, Kin Chiu; Gaudino, John J.; Kaplan, Tomas; Marlow, Allison L.; Seo, Jeongbeob; Thomas, Allen A.; Tian, Hongqi; Young, Wendy B. published a patent.Related Products of 924909-16-0 The title of the patent was Heterobicyclic pyrazole compounds as Met tyrosine kinase inhibitors and their preparation and use. And the patent contained the following:

The invention is related to the preparation of I and II [X = O, S, NH and derivatives; Z2, Z3 = independently CH and derivatives, N, wherein none or one of Z2, and Z3 = N; R1 = H, (un)substituted alk(en/yn)yl, (hetero)aryl, etc.; R2 = H, CF3, CN, SH and derivatives, SO2NH2 and derivatives, etc.; R3 = (un)substituted carbocyclyl, heterocyclyl, (hetero)/aryl] and their pharmaceutically acceptable salts which are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds I and II and their stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathol. conditions are disclosed. Thus, pyrazolopyridine III was prepared by a multi-step synthesis via 1-(4-methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol intermediate which was obtained from 1-(4-methoxybenzyl)-1H-pyrazol-5-amine and Meldrum’s acid. Certain I and II had IC50’s < 1 μM in a c-Met enzyme assay. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Related Products of 924909-16-0

The Article related to heterobicyclic pyrazole preparation tyrosine kinase inhibitor antiproliferative, pyrazolopyridine preparation met kinase inhibitor antitumor hyperproliferative disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Related Products of 924909-16-0

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

On March 3, 2022, Grall-Ulsemer, Sandra; Guba, Wolfgang; Lerner, Christian; Li, Mingming; Liu, Yongqiang; Rudolph, Markus; Schmitt, Sebastien; Urner, Lorenz; Wang, Yongguang; Wang, Min; Wang, Jianhua; Yang, Song; Zhou, Chengang; Mattei, Patrizio published a patent.Formula: C4H6N2O The title of the patent was Imidazole-pyrazole derivatives as antibacterials and their preparation. And the patent contained the following:

The invention provides imidazole-pyrazole derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases. Compounds of formula I wherein R1R2 are taken together to form substituted nitrogen-containing heterocyclyl; R1 is (un)substituted 3- to 14-membered heterocyclyl, (un)substituted 3- to 14-membered heterocyclyl-CO and (un)substituted 3- to 14-membered heterocyclyl-C1-6 alkyl; R2 is H and C1-6 alkyl; R3 is H, halo, C1-6 alkyl and C1-6 alkoxy; R4 and R6 are independently H, C1-6 alkyl, C1-6 alkoxy, CN, etc.; R5a, R5b and R5c are independently H, halo, OH, C1-6 alkyl, C1-6 alkoxy, etc.; R7 is H, C1-6 alkyl and C1-6 haloalkyl; A is 5- to 14-membered heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by methylation of N-(3-chloro-4-(4-(piperidine-4-carbonyl)piperazine-1-carbonyl)phenyl)-5-(1-(5-methoxypyridin-2-yl)-3-(trifluoromethyl)-pyrazol-4-yl)-1-methyl-imidazole-2-carboxamide with Me iodide. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 0.095μM. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Formula: C4H6N2O

The Article related to imidazole pyrazole preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Formula: C4H6N2O

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

On March 10, 2022, Lerner, Christian; Li, Mingming; Liu, Yongqiang; Schmitt, Sebastien; Wang, Jianhua; Wang, Min; Wang, Yongguang; Yang, Song; Zhou, Chengang published a patent.COA of Formula: C4H6N2O The title of the patent was Preparation of imidazole-pyrazole derivatives with anti-bacterial properties. And the patent contained the following:

The invention provides imidazole pyrazole derivatives having formula I, and pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases. Compounds of formula I wherein R1R2 may be taken together to form substituted nitrogen-containing heterocycle; R1 is C1-6 alkyl, amino-C1-6 alkyl, amino-C1-6 alkoxy-C1-6 alkyl, etc.; R2 is H and C1-6 alkyl; R3 is H, halo, C1-6 alkyl and C1-6 alkoxy; R4 and R6 are independently H, C1-6 alkyl, C1-6 alkoxy, CN, etc.; R5a, R5b and R5c are H, halo, OH, C1-6 alkyl, C1-6 alkoxy, etc.; A is 5- to 14- membered heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II•HCO2H was prepared by arylation of tert-Bu 4-(4-(2-chloro-4-(1-methyl-5-(3-(trifluoromethyl)-1H-pyrazol-4-yl)-imidazole-2-carboxamido)benzoyl)piperazine-1-carbonyl)piperidine-1-carboxylate with 2-chloropyrimidine; the resulting tert-Bu 4-(4-(2-chloro-4-(1-methyl-5-(1-(pyrimidin-2-yl)-3-(trifluoromethyl)-pyrazol-4-yl)-imidazole-2-carboxamido)benzoyl)piperazine-1- carbonyl)piperidine-1-carboxylate underwent hydrolysis to give compound II•HCO2H. The invention compounds were evaluated for their antibacterial activity. From the assay, it was determined that compound II exhibited IC90 value of 0.69μM. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).COA of Formula: C4H6N2O

The Article related to imidazole pyrazole preparation antibacterial, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.COA of Formula: C4H6N2O

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

On January 13, 2022, Barrett, Matthew; Cockerill, George Stuart; Good, James; Avery, Craig Alex; Cochrane, Edward James; Jones, Stefan Paul; Onions, Stuart Thomas; Warner, Andrew Joseph published a patent.Recommanded Product: Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate The title of the patent was Synthesis of Benzodiazepines useful in treating a respiratory syncytial virus infection. And the patent contained the following:

The synthesis of benzodiazepines, I, wherein: one of R1 or R2 can be II such that the other group is selected from H, cycloalkyl, halo, amino, benzyl, Ph, 4- to 10-membered heterocyclic or heteroaryl groups; R3 can be H or halo; and the ring A can be a 5- or 6-membered heterocyclic ring system containing a variety of N, O or C atoms are prepared as pharmaceutically acceptable salt RSV inhibitors used to treat or prevent an RSV infection. Of note, II was synthesized and displayed an RSV A2 plaque EC50 of 33 nM and cell cytotoxicity of greater than 25,000 nM CC50 and presented in aqueous formulations. Further, some I derivatives were tested in vitro pharmacokinetics to investigate liver microsomal stability. 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).Recommanded Product: Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate

The Article related to benzodiazepine preparation antiviral rsv infection, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Recommanded Product: Ethyl 6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxylate

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

On April 12, 2012, Biggadike, Keith; Birault, Veronique; Champigny, Aurelie Cecile; Coe, Diane Mary; Hughes, Owen Rhys; Needham, Deborah; Tape, Daniel Terence published a patent.Synthetic Route of 143803-93-4 The title of the patent was Imidazo[1,2-a]pyridine and pyrazolo[1,5-a]pyridine derivatives as TRPV1 antagonists and their preparation and use for the treatment of TRPV1-mediated diseases. And the patent contained the following:

The invention relates to imidazopyridine and pyrazolopyridine derivatives of formula I, which are TRPV1 antagonists and which are useful in the treatment of TRPV1-mediated diseases. Compounds of formula I wherein A is single bond, CH2 and CH(CH3); X1 is H, F and Me; X2 is H, F, Me and CH2OH; X3 is H, F and Ch2OH; provided that at least two of X1, X2 and X3 are H; Y is C when Z is N, and Y is N when Z is C; R1 is halo, C1-4 alkyl, CF3 and OCF3; R2 and R3 are independently H, halo, C1-4 alkyl, CF3 and OCF3; and pharmaceutically acceptable salts and solvates, are claimed. Example compound II was prepared by a amidation of imidazo[1,2-a]pyridine-3-carboxylic acid with (2-{[4-(1,1-dimethylethyl)phenyl]oxy}ethyl)amine. All the invention compounds were evaluated for their TRPV1 antagonistic activity. From the assay, it was determined that all compounds exhibited a pIC50 value greater than 5.2. The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).Synthetic Route of 143803-93-4

The Article related to imidazopyridine preparation trpv1 antagonist treatment disease, pyrazolopyridine preparation trpv1 antagonist treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Synthetic Route of 143803-93-4

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

On March 28, 2013, Wilson, Timothy R.; Koeppen, Hartmut; Merchant, Mark; Settleman, Jeffrey published a patent.SDS of cas: 924909-16-0 The title of the patent was Combinations comprising c-Met antagonists and B-raf antagonists for treatment of cancer. And the patent contained the following:

The invention provides combination therapies for treating a pathol. condition, such as cancer, wherein a c-met antagonist (e.g. crizotinib, tivantinib, anti-HGF antibody, onartuzumab) is combined with a B-raf antagonist (e.g. vemurafenib), thereby providing significant antitumor activity. C-met expression was inversely correlated with sensitivity to vemurafenib treatment. In one aspect, provided are methods for treating a cancer patient who has increased likelihood of developing resistance to B-raf antagonist comprising administering an effective amount (in combination) of B-raf antagonist and c-met antagonist. In addition, patients with B-raf mutant melanoma who had higher levels of circulating hepatocyte growth factor (HGF) showed substantially reduced progression free survival and overall survival when treated with B-raf antagonist, relative to patients with lower circulating HGF levels treated with B-raf antagonist. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).SDS of cas: 924909-16-0

The Article related to combination chemotherapy cmet antagonist braf inhibitor cancer treatment, gdc0712 preparation antitumor combination chemotherapy cmet braf drug target, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.SDS of cas: 924909-16-0

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

On August 13, 2009, Hirokawa, Takatsugu; Takemura, Shunji; Shibazaki, Manabu; Ishiwatari, Hiroyuki published a patent.Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the patent was 3-naphthylpyrazole compounds, histamine H4 receptor antagonists containing them, their use for treatment for inflammatory disorders, and pharmaceutical compositions containing them. And the patent contained the following:

Claimed are title compounds I [ring A = C6-10 aryl; X = (CH2)n (n = 1-6), CH:N; Y = O, S, NR8; Z = direct bond, CHR7; R1-R7 = H, halo, OH, NO2, carboxy, carbamoyl, C1-6 alkyl, C2-6 acyl, C6-10-aryl-C1-6 alkyl, C5-10-heteroaryl-C2-6 alkenyl, etc.; R8 = H, OH, C1-6 alkyloxy], their salts, or their solvates [exclusive of (E)-2-[[3-(2-Naphthyl)-1-phenyl-1H-pyrazol-4-yl]methylene]hydrazinecarboxamide] and histamine H4 receptor antagonists containing I, their salts, or their solvates. Also claimed are prophylactic and/or therapeutic agents and pharmaceutical compositions containing I, their salts, or their solvates. Thus, (S)-2-amino-N-[[3-(2-naphthyl)-1-phenyl-1H-pyrazol-4-yl]methyl]-3-phenylpropanamide at 10 μM (preparation given) showed 86% inhibition against histamine binding to human recombinant H4 receptor expressed on CHO cells. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to naphthylpyrazole compound preparation histamine h4 receptor antagonist inflammation inhibitor, Pharmacology: Effects Of Inflammation Inhibitors and Immune Agents and other aspects.Quality Control of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

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

On February 11, 1983, Cottam, Howard B.; Revankar, Ganapathi R.; Robins, Roland K. published an article.HPLC of Formula: 85426-79-5 The title of the article was A convenient synthesis of 6-amino-1-β-D-ribofuranosylpyrazolo[3,4-d]pyrimidin-4-one and related 4,6-disubstituted pyrazolopyrimidine nucleosides. And the article contained the following:

The glycosylation of 4,6-dichloropyrazolo[3,4-d]pyrimidine and 4-chloro-6-methylthiopyrazolo[3,4-d]pyrimidine via the corresponding trimethylsilyl intermediate and tetra-O-acetyl-β-D-ribofuranose in the presence of trimethylsilyl triflate as a catalyst, gave selective glycosylation at N-1 as the only nucleoside product. The intermediates 4,6-dichloro-1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)pyrazolo[3,4-d]pyrimidine and 4-chloro-6-methylthio-1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)pyrazolo[3,4-d]pyrimidine gave new and convenient synthetic routes to the inosine analog I, the guanosine analog II, the adenosine analog III, and the isoguanosine analog IV. Glycosylation of the trimethylsilyl derivative of 6-chloropyrazolo[3,4-d]pyrimidin-4-one unexpectedly gave the N-2 glycosyl isomer as the major product. A number of new 4,6-disubstituted pyrazolo[3,4-d]pyrimidine nucleosides were prepared from these glycosyl intermediates. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).HPLC of Formula: 85426-79-5

The Article related to pyrazolopyrimidine nucleoside, ribofuranosylpyrazolopyrimidinone, glycosylation pyrazolopyrimidine ribofuranose, Carbohydrates: Nucleosides and Nucleotides, Cobalamins, Riboflavin and other aspects.HPLC of Formula: 85426-79-5

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

Seela, Frank; Menkhoff, Sabine published an article in 1986, the title of the article was 2′-Deoxyribofuranosides of 6-oxoallopurinol and of related 4,6-disubstituted pyrazolo[3,4-d]pyrimidines.Computed Properties of 98138-75-1 And the article contains the following content:

Deoxypentofuranosylpyrazolopyrimidine I (R = OMe) was aminated to I (R = NH2) and demethylated to pyrimidinones II and III. I (R = OMe) was prepared by phase-transfer glycosidation of methoxylated or chlorinated pyrimidine base. The experimental process involved the reaction of 6-Chloro-4-methoxy-1H-pyrazolo[3,4-d]pyrimidine(cas: 98138-75-1).Computed Properties of 98138-75-1

The Article related to pentofuranosylpyrazolopyrimidinedione, pyrazolopyrimidine deoxypentofuranosyl glycosidation, methoxypyrazolopyrimidinylpentofuranose preparation hydrolysis, Carbohydrates: Nucleosides and Nucleotides, Cobalamins, Riboflavin and other aspects.Computed Properties of 98138-75-1

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

On June 7, 2012, Crew, Andrew P.; Dong, Hanqing; Ferraro, Caterina; Sherman, Dan; Siu, Kam W. published a patent.Recommanded Product: 215610-30-3 The title of the patent was Macrocyclic phosphonates and phosphinates, fused with five- and six-membered nitrogen heterocycles as specific focal adhesion kinase inhibitors in cancer therapy. And the patent contained the following:

Macrocyclic phosphonates or phosphinates I, II [1, X = N, CH; A1 = C6H4, heteroarylene; A3 = heteroarylene, preferably, A3 = pyrazolediyl, triazolediyl, imidazolediyl; L2 = O, bond; L3 = C2-6 alkylene; L4 = C1-2 alkylene; Q1-Q4 = N, N-oxide, optionally substituted CH, Q1-Q4 may form a fused (hetero)cycle; R1-R3 = H, organyl, preferably, R1 = Cl, CN, NO2, CF3; R4 = OH, C1-4 alkyl, C3-6 cycloalkyl, C4-6 heterocyclyl, alkoxy], including resolved enantiomers thereof, and a pharmaceutically acceptable salts thereof, useful as selective focal adhesion kinase (FAK) inhibitors, beneficial in therapy of aggressive tumors, were prepared by intramol. esterification of acyclic phosphonate or phosphinate group with OH-containing linker A3 or by Suzuki coupling of pinacolboronate-containing linker A3 with halo-substituted (hetero)aryl ring. The prepared compounds 1 were tested for inhibition of phospho-FAK Y397 in the presence of human plasma, showing IC50 values, in general, less than 0.4 μM. In an example, the phosphonate II (1a, X = N, R1 = CF3, R2 = R3 = H, R4 = Et, R5 = OMe; L3 = (CH2)3, X1+X2 = CH2NMeCO) was prepared by esterification of 0.07 mmol of the acyclic phosphonate, sodium Et [4-[4-[[7-[1-(3-hydroxypropyl)-1H-pyrazol-4-yl]-2-methyl-3-oxo-2,3-dihydro-1H-isoindol-4-yl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-3-methoxybenzylphosphonate in the presence of 0.3684 mmol of PYBOP and 0.4 mmol of DIPEA in 50 mL of 1,2-dichloroethane and 10 mL of DMF for 3 h at 20° with a 12% yield. In another example, the phosphonate 1a exhibited inhibitory activity towards phospho-FAK Y397 at a concentration <0.4 μM both in the plasma-free conditions and in the presence of human or murine plasma. The experimental process involved the reaction of 5-Methoxy-1H-pyrazole(cas: 215610-30-3).Recommanded Product: 215610-30-3

The Article related to phosphonate cyclic macrocyclic preparation focal adhesion kinase inhibition, antitumor agent macrocyclic phosphonate phosphinate focal adhesion kinase inhibition, Organometallic and Organometalloidal Compounds: Phosphorus Compounds and other aspects.Recommanded Product: 215610-30-3

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