Category: 85426-79-5

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 September 8, 2005, Arora, Nidhi; Billedeau, Roland Joseph; Dewdney, Nolan James; Gabriel, Tobias; Goldstein, David Michael; O’Yang, Counde; Soth, Michael published a patent.Electric Literature of 85426-79-5 The title of the patent was Preparation of fused pyrazolo pyrimidine and pyrazolo pyrimidinone derivatives as p38 kinase inhibitors. And the patent contained the following:

The title compounds I-III [R1 = (hetero)aryl, aralkyl, cycloalkyl; R2 = (hetero)aryl, cycloalkyl, alkyl, heterocyclyl; R3 = H, alkyl; R4 = H, alkyl, OH, etc.; R5 = H, alkyl, heteroalkyl, etc.; X, Y = N, or one of X and Y = N and the other = CR6 (R6 = H, alkyl, OH, etc.); Z = N, CR6; W = O, SOm, CH2, (un)substituted NH; m = 0-2; A = O, CH2, SOm, C(O), etc.; B = O, SOm, C(O), etc.; k = 0-1], useful in treating p38 mediated disorders, were prepared and formulated. E.g., a multi-step synthesis of (S)-IV, starting from 4,6-dichloro-2-(methylthio)pyrimidine and 2-chlorobenzaldehyde, was given. The compounds I were found to be inhibitors of p38 MAP kinase. IV showed a p38 IC50 of 0.004 μM. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Electric Literature of 85426-79-5

The Article related to fused pyrazolo pyrimidine pyrimidinone preparation p38 kinase inhibitor, pyrazolopyrimidine preparation p38 kinase inhibitor, pyrazolopyrimidinone preparation p38 kinase inhibitor and other aspects.Electric Literature 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 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

On May 31, 2003, Kim, Dong Chan; Lee, Yeo Ran; Yang, Beom-Seok; Shin, Kye Jung; Kim, Dong Jin; Chung, Bong Young; Yoo, Kyung Ho published an article.Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine The title of the article was Synthesis and biological evaluations of pyrazolo[3,4-d]pyrimidines as cyclin-dependent kinase 2 inhibitors. And the article contained the following:

A series of 1,4,6-trisubstituted pyrazolo[3,4-d]pyrimidines capable of selectively inhibiting CDK2 activity were synthesized by derivatization at C-4, C-6 and N-1 with various amines and lower alkyl groups. For above synthetic compounds, biol. evaluation was carried out and structure-activity relationship was examined In the series, 4-anilino compounds exhibited better CDK2 inhibitory activity and antitumor activity compared to 4-benzyl compounds Two compounds having a 3-fluoroaniline group at C-4 showed comparable or superior CDK2 inhibitory activity to those of olomoucine and roscovitine as reference compounds In general, the unsubstituted compounds at N-1 possessed higher potency than the substituted compounds for the CDK2 inhibitory activity. As for EGFR inhibitory activity, most compounds did not have a significant activity. Two compounds exhibited potent cell growth inhibitory activity against human cancer cell lines, but their CDK2 inhibitory activities were slightly poorer than olomoucine. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

The Article related to pyrazolopyrimidine preparation cyclin dependent kinase 2 inhibitor, cdk2 inhibitor pyrazolopyrimidine preparation, egfr inhibitor pyrazolopyrimidine preparation, antitumor agent pyrazolopyrimidine preparation and other aspects.Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

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