Category: pyrimidines

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 September 18, 2014, Chesworth, Richard; Moradei, Oscar Miguel; Shapiro, Gideon; Jin, Lei; Babine, Robert E. published a patent.Name: 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride The title of the patent was 1-Amino-3-(aryloxy)propanol derivatives as CARM1 inhibitors and uses thereof. And the patent contained the following:

Provided herein are compounds of formula I and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; and their use for inhibiting CARM1 activity and for treating CARM1-mediated disorders. Compounds of formula I wherein X is O, S and CH2; R1 is H and (un)substituted C1-4 alkyl; R1a is H; each R2 are independently H, halo, CN, NO2, acyl, etc.; HET is 6-membered monocyclic nitrogen-containing heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their CARM1 inhibitory activity (data given). The experimental process involved the reaction of 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride(cas: 1187830-46-1).Name: 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride

The Article related to amino aryloxypropanol preparation carm1 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 6,7-Dihydro-5H-pyrrolo[3,4-d]pyrimidine hydrochloride

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

On January 18, 2018, Bartels, Bjoern; Jakob-Roetne, Roland; Limberg, Anja; Neidhart, Werner; Ratni, Hasane; Reutlinger, Michael; Steiner, Sandra published a patent.Safety of 5-Bromo-2,4,6-trichloropyrimidine The title of the patent was Preparation of fused pyrimidine derivatives as γ-secretase inhibitors. And the patent contained the following:

The present invention relates to a compound of formula I wherein R1 is Ph, lower alkyl, C3-6-cycloalkyl, -CH2-C3-6-cycloalkyl or bridged C4-6-cycloalkyl, substituted by one, two or three halogen atoms, or by lower alkyl or lower alkyl substituted by halogen;R2 is a five or six membered heteroaryl group, selected from or wherein R6 is hydrogen, lower alkyl, halogen or lower alkoxy; and R7 is hydrogen, lower alkoxy or halogen; R3 is lower alkyl or lower alkyl substituted by hydroxy: R4 is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; n is 1 or 2; -( )n- is -CH2- or -CH2CH2- for n being 1 or 2; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or optical isomer and/or stereoisomer 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. 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 (1R,5S,8S)-3-(6-methylpyrimidin-4-yl)-3-azabicyclo[3.2.1]octan-8-amine. The invention compounds were evaluated for their γ-secretase inhibitory activity. From the assay, it was determined that compound II exhibited EC50 value of 14 nM. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Safety of 5-Bromo-2,4,6-trichloropyrimidine

The Article related to pyrimidine preparation gamma secretase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 5-Bromo-2,4,6-trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 16, 2019, Blake, James F.; Burgess, Laurence E.; Chicarelli, Mark Joseph; Christensen, James Gail; Cook, Adam; Fell, Jay Bradford; Fischer, John P.; Marx, Matthew Arnold; Mejia, Macedonio J.; Savechenkov, Pavel; Vigers, Guy P.A.; Smith, Christopher Ronald; Rodriguez, Martha E. published a patent.Electric Literature of 175357-98-9 The title of the patent was 5,6,7,8-Tetrahydropyrido[3,4-d]pyrimidine derivatives as KRas G12C inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formula I that inhibit KRas G12C. The invention relates to compounds of formula I that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor. Compounds of formula I wherein L is a bond, CO and C1-3 alkylene; ring X is a 4- to 12-membered (mono/spiro)cyclic or bridged ring; Y is a bond, O, S and NH and derivatives; R1 is (un)substituted alkenoyl, (un)substituted alkynoyl, (un)substituted ethenylsulfonyl, etc.; R2 is H, alkyl, hydroxyalkyl, aryl, etc.; R3 is C1-3 alkyl, oxo, haloalkyl, etc.; R4 is H, cycloalkyl, aryl, etc.; n is 0, 1 and 2; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their KRas G12C inhibitory activity. From the assay, it was determined that compound II exhibited > 25 % inhibition at 5 μM concentration The experimental process involved the reaction of 4-Chloro-6-fluoropyrido[3,4-d]pyrimidine(cas: 175357-98-9).Electric Literature of 175357-98-9

The Article related to pyridopyrimidine preparation kras g12c inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 175357-98-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On February 26, 2015, Blaquiere, Nicole; Burch, Jason; Castanedo, Georgette; Feng, Jianwen A.; Hu, Baihua; Lin, Xingyu; Staben, Steven; Wu, Guosheng; Yuen, Po-Wai published a patent.Quality Control of Methyl 6-amino-2-chloropyrimidine-4-carboxylate The title of the patent was Alkynyl alcohols as NIK kinase inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formula I and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed Compounds of formula I wherein ring A is monocycle and bicycle; A1 is N and CR1; A2 is N, NR2 and CR2; A3 is N, NR3 and CR3; A4 is N and CH; provided that one, two or three of A1 – A4 are N; one of A5 – A8 is N and the remaining are CR6 or all A5 – A8 are CR6; R1 is H, halo, OH, amino, C1-3 alkyl, etc.; R2 is H, OH, amino, C1-6 alkyl, etc.; R3 is H, (un)substituted C1-6 alkyl, C1-6 alkoxy, etc.; R1R2 or R2R3 can be taken together to form a C3-7 cycloalkyl, Ph and 3- to 11-membered heterocyclyl; R4 is C1-6 alkyl, CH2F and CH2OH; R5 is (un)substituted 3- to 11-membered heterocycle; R4R5 can be taken together to form (un)substituted C3-11 cycloalkyl and 3- to 11-membered heterocyclyl; each R6 is independently H, F, Cl, NH2, OH, etc.; and stereoisomers, and salts thereof, are claimed. Example compound II was prepared by cross-coupling of 2-chloropyrimidine-4-carboxamide with potassium (S)-trifluoro(3-((3-hydroxy-1-methyl-2-oxopyrrolidin-3-yl)ethynyl)phenyl)borate. The invention compounds were evaluated for their NIK inhibitory activity (data given). The experimental process involved the reaction of Methyl 6-amino-2-chloropyrimidine-4-carboxylate(cas: 944129-00-4).Quality Control of Methyl 6-amino-2-chloropyrimidine-4-carboxylate

The Article related to alkynyl alc preparation nik inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of Methyl 6-amino-2-chloropyrimidine-4-carboxylate

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia