Tag: 200-300

On June 25, 2009, Goldfarb, David Scott published a patent.Quality Control of 5-Phenylpyrimidine-2-carboxylic acid The title of the patent was Method using lifespan-altering compounds for altering the lifespan of eukaryotic organisms, and screening for such compounds. And the patent contained the following:

The invention discloses a method for altering the lifespan of a eukaryotic organism. The method comprises the steps of providing a lifespan-altering compound, and administering an effective amount of the compound to a eukaryotic organism, such that the lifespan of the organism is altered. In one embodiment, the compound is identified using the DeaD assay. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Quality Control of 5-Phenylpyrimidine-2-carboxylic acid

The Article related to lifespan alteration compound screening dead assay, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Quality Control of 5-Phenylpyrimidine-2-carboxylic acid

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On August 31, 2017, Wakiyama, Yoshinari; Kumura, Ko; Umemura, Eijiro; Ueda, Kazutaka; Watanabe, Takashi; Yamada, Keiko; Okutomi, Takafumi; Ajito, Keiichi published an article.Application of 160377-42-4 The title of the article was Synthesis and structure-activity relationships of novel lincomycin derivatives. Part 4: synthesis of novel lincomycin analogs modified at the 6- and 7-positions and their potent antibacterial activities. And the article contained the following:

To modify lincomycin (LCM) at the C-6 and the C-7 positions, we firstly prepared various substituted proline intermediates (7, 11-15 and 17). These proline intermediates were coupled with Me 1-thio-α-lincosamide and tetrakis-O-trimethylsilylation followed by selective deprotection of the TMS group at the 7-position gave a wide variety of key intermediates (23-27, 47 and 50). Then, we synthesized a variety of novel LCM analogs modified at the 7-position in application of the Mitsunobu reaction, an SN2 reaction, and a Pd-catalyzed cross-coupling reaction. Compounds 34 and 35 (1′-NH derivatives) exhibited enhanced antibacterial activities against resistant pathogens with erm gene compared with the corresponding 1′-N-Me derivatives (3 and 37). On the basis of reported SAR, we modified the 4′-position of LCM derivatives possessing a 5-(2-nitrophenyl)-1,3,4-thiadiazol-2-yl group at the C-7 position. Compound 56 showed significantly potent antibacterial activities against S. pneumoniae and S. pyogenes with erm gene, and its activities against S. pneumoniae with erm gene were improved compared with those of 34 and 57. Although we synthesized novel analogs by transformation of a C-7 substituent focusing on the 1′-demethyl framework to prepare very potent analogs 73 and 75, it was impossible to generate novel derivatives exhibiting stronger antibacterial activities against S. pneumoniae with erm gene compared with 56. The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).Application of 160377-42-4

The Article related to lincomycin derivative analog antibacterial activity, Microbial, Algal, and Fungal Biochemistry: Antimicrobial Sensitivity and other aspects.Application of 160377-42-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 31, 2017, Wakiyama, Yoshinari; Kumura, Ko; Umemura, Eijiro; Masaki, Satomi; Ueda, Kazutaka; Sato, Yasuo; Watanabe, Takashi; Hirai, Yoko; Ajito, Keiichi published an article.Category: pyrimidines The title of the article was Synthesis and structure-activity relationships of novel lincomycin derivatives part 3: discovery of the 4-(pyrimidin-5-yl)phenyl group in synthesis of 7(S)-thiolincomycin analogs. And the article contained the following:

Novel lincomycin derivatives possessing an aryl Ph group or a heteroaryl Ph group at the C-7 position via sulfur atom were synthesized by Pd-catalyzed cross-coupling reactions of 7(S)-7-deoxy-7-thiolincomycin with various aryl halides. This reaction is the most useful method to synthesize a variety of 7(S)-7-deoxy-7-thiolincomycin derivatives On the basis of anal. of structure-activity relationships of these novel lincomycin derivatives, the authors found that (a) the location of basicity in the C-7 side chain was an important factor to enhance antibacterial activities, and (b) compounds 22, 36, 42, 43 and 44 had potent antibacterial activities against a variety of Streptococcus pneumoniae with erm gene, which cause severe respiratory infections, even compared with the authors’ C-7-modified lincomycin analogs (1-4) reported previously. Furthermore, 7(S)-configuration was found to be necessary for enhancing antibacterial activities from comparison of configurations at the 7-position of 36 (S-configuration) and 41 (R-configuration). The experimental process involved the reaction of 5-(4-Bromophenyl)pyrimidine(cas: 160377-42-4).Category: pyrimidines

The Article related to structure activity lincomycin derivative, Microbial, Algal, and Fungal Biochemistry: Antimicrobial Sensitivity and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 11, 2017, Gaufreteau, Delphine; Kolczewski, Sabine; Plancher, Jean-Marc; Stoll, Theodor published a patent.Related Products of 1209459-32-4 The title of the patent was Preparation of 6-(pyrimidin-2-yl)indolin-2-one derivatives useful in the treatment of CNS-related disorders. And the patent contained the following:

The invention is concerned with indolin-2-one derivatives of formula I that are useful in the treatment of CNS-related diseases. Compounds of formula I wherein A is Ph, pyrazinyl, pyridazinyl, pyrimidinyl, pyridinyl, etc.; R1 and R2 are independently H, lower acyl. cycloalkyl, lower alkyl, etc.; R1R2 may be taken together to form morpholinyl, oxopyrrolidinyl, substituted piperidinyl, etc.; R3 is H and lower alkyl; and pharmaceutically acceptable salts, racemic mixtures, enantiomers, optical isomer and stereoisomers thereof, are claimed. Example compound II was prepared by N-arylation of 3,3-dimethyl-6-(2-methylpyrimidin-5-yl)indolin-2-one with 4-(6-bromopyrazin-2-yl)morpholine. The invention compounds were evaluated for their ENT1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 0.0390 μM. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Related Products of 1209459-32-4

The Article related to pyrimidinylindolinone preparation treatment cns disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Related Products of 1209459-32-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 31, 2019, Bartels, Bjoern; Cook, Xinlan Aloise Ford; Ratni, Hasane; Reutlinger, Michael; Vifian, Walter published a patent.Product Details of 63931-21-5 The title of the patent was Preparation of pyrimidine derivatives as Aβ42 inhibitor. And the patent contained the following:

The invention provides pyrimidine compounds with formula I as Aβ24 inhibitor. Compounds of formula I wherein each R1 is independently H and halo; R2 is H and methyl; R3 is five membered heteroaryl group; n is 1, 2 and 3; X is N and C; A is is a (un)substitued bicyclo[1.1.1]pentane or (un)stituted bicyclo[2.2.2]octane; and a pharmaceutically acceptable salt thereof; are claimed. Example compound II was prepared by N-alkylation of 3-(4-methylimidazol-1-yl)bicyclo[1.1.1]pentan-1-amine with 2-chloro-7-(4-fluorophenyl)-N,5,5-trimethyl-6H-pyrrolo[2,3-d]pyrimidin-4-amine. The compounds of formula I were evaluated for their Aβ24 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 of 0.032 μM. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Product Details of 63931-21-5

The Article related to pyrimidine derivative preparation protein inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Product Details of 63931-21-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 2, 2020, Kanouni, Toufike; Arnold, Lee D.; Kaldor, Stephen W.; Murphy, Eric A.; Tyhonas, John published a patent.Recommanded Product: 785777-98-2 The title of the patent was Inhibitors of cyclin-dependent kinases. And the patent contained the following:

Provided herein are inhibitors of cyclin-dependent kinases (CDKs), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases. The experimental process involved the reaction of 2,5-Dichloro-4-(trifluoromethyl)pyrimidine(cas: 785777-98-2).Recommanded Product: 785777-98-2

The Article related to cyclin dependent kinase cdk12 inhibitor preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 785777-98-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On April 30, 1993, Oleynik, I. V.; Zagulyaeva, O. A. published an article.Formula: C11H8N2O2 The title of the article was Chemical properties of ylidene derivatives of azines. 7. Transformations of 5-methyl(phenyl)-substituted 1,2-dihydro-2-pyrimidinylidenemalononitriles by action of nitric acid. And the article contained the following:

Reaction of title compounds I (R = Me, Ph) with HNO3, depending on the conditions, gave either the corresponding 2-pyrimidinecarboxylic acids or acetonitrile derivatives, e.g., II. The experimental process involved the reaction of 5-Phenylpyrimidine-2-carboxylic acid(cas: 85386-20-5).Formula: C11H8N2O2

The Article related to malononitrile pyrimidinylidene reaction nitric acid, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C11H8N2O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On July 12, 1973, Narr, Berthold; Woitun, Eberhard published a patent.HPLC of Formula: 42518-42-3 The title of the patent was Thrombocyte aggregation-inhibiting thieno[2,3-d]pyrimidines. And the patent contained the following:

Twenty-seven thienopyrimidines [I; R, R1 = H or Me; X = NH(CH2)2NH2 or NH(CH2)5NH2; X, Y = 1-pyrrolidinyl, 1-piperazinyl, 4-methyl-1-piperazinyl, piperidino, morpholino, 2-methylmorpholino, or thiomorpholino and its S-oxide or S,S-dioxide] were prepared by reaction of I (X, Y = Cl, SO2Me, SO2Et, or X or Y one of above substituents) with XH and(or) YH. I have a thrombocyte aggregation-inhibiting effect. Thus, KOCN in H2O was added to Et 2-amino-4,5-dimethyl-3-thiophenecarboxylate at 33.5.degree. and the mixture stirred 10 hr at room temperature to give 70% 5,6-dimethyl-2,4-dihydroxythieno[2,3-d]pyrimidine (II). II in POCl3 was heated 6 hr at 180° in a bomb tube to give 81% I (R = R1 = Me, X = Y = Cl) (III). III and morpholine were refluxed 2 hr to give 72% I (R = R1 = Me, X = Y = morpholino). The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).HPLC of Formula: 42518-42-3

The Article related to thienopyrimidine thrombocyte aggregation inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 42518-42-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 5, 2022, Hallur, Gurulingappa; Madhyastha, Naveena; Stephen, Michael Rajesh; Roth, Bruce; Pandey, Anjali; Saxton, Tracy; Rajagopal, Sridharan; Sadhu M., Naveen published a patent.COA of Formula: C4BrCl3N2 The title of the patent was Pyrimidine compounds, compositions, and medicinal applications thereof. And the patent contained the following:

The disclosure relates to a class of pyrimidine compounds of formula I (wherein X is NH and O; R1 is (C(R4)2)nR5; n = 0 – 3; each R4 is independently H, halo, OH, etc.; R5 is C4-10 cycloalkyl, aryl and heteroaryl; R2 is aryl, heteroaryl, cycloalkyl, etc.; R3 is substituted heteroaryl) and pharmaceutically acceptable salts, and stereoisomers thereof as EGFR inhibitors; their preparation and use to treat cancer. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their anticancer activities (some data given). The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).COA of Formula: C4BrCl3N2

The Article related to pyrimidine preparation egfr inhibitor anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C4BrCl3N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On January 11, 2018, Bartels, Bjoern; Jakob-Roetne, Roland; Limberg, Anja; Neidhart, Werner; Ratni, Hasane; Steiner, Sandra; Reutlinger, Michael published a patent.Recommanded Product: 63931-21-5 The title of the patent was Fused pyrimidine derivatives as γ-secretase inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formula I, or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. The compounds may be used for the treatment of Alzheimer’s disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome. Compounds of formula I wherein R1 is Ph, lower alkyl, C3-6 cycloalkyl, etc.; R2is H, halo, lower alkyl, etc.; R3 is 5-membered heteroaryl; R4 is (un)substituted lower alkyl; R5 and R5′ are independently H and lower alkyl; A is CH2 and CH2CH2; X is CH and N; and pharmaceutically active acid addition salts, racemic mixtures, enantiomers, optical isomers and stereoisomers thereof, are claimed. Example compound II was prepared by amination of 2-chloro-7-(4-fluorophenyl)-N,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-amine with 3-methoxy-4-(3-methyl-1H-1,2,4-triazol-1-yl)aniline. The invention compounds were evaluated for their γ-secretase inhibitory activity. From the assay, it was determined that compound II exhibited EC50 value of 5 nM. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Recommanded Product: 63931-21-5

The Article related to pyrimidine preparation gamma secretase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 63931-21-5

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia