Day: November 2, 2022

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 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 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 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 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 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 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 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 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 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