Category: 1209459-32-4

On May 25, 2018, Woodring, Jennifer L.; Bachovchin, Kelly A.; Brady, Kimberly G.; Gallerstein, Mitchell F.; Erath, Jessey; Tanghe, Scott; Leed, Susan E.; Rodriguez, Ana; Mensa-Wilmot, Kojo; Sciotti, Richard J.; Pollastri, Michael P. published an article.Category: pyrimidines The title of the article was Corrigendum to “Optimization of physicochemical properties for 4-Anilinoquinazoline inhibitors of trypanosome proliferation” [Eur. J. Med. Chem. 141 (2017) 446-459] [Erratum to document cited in CA167:595582]. And the article contained the following:

In the original publication, the acknowledgments section has information omitted; the correction is provided here. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Category: pyrimidines

The Article related to anilinoquinazoline trypanosome inhibitor antimalarial malaria trypanosomiasis trypanosomicide erratum, Placeholder for records without volume info and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 25, 2014, Chan, Bryan; Estrada, Anthony; Shore, Daniel; Sweeney, Zachary published a patent.Formula: C8H10BrN3O The title of the patent was Preparation of pyrazolopyridine compounds as LRRK2 inhibitors. And the patent contained the following:

The invention relates to pyrazolopyridine compounds of formula I and II, or pharmaceutically acceptable salts thereof that are useful for the treatment of the diseases associated with LRRK2. Compounds of formula I and II wherein R1 is (un)substituted alkyl, heterocycloalkyl, cycloalkyl, etc.; for formula I, one, two, or three of X1-X4 are N and the remainder are each independently CR2; or X1-X4 are independently CR2; for formula II, X4 is C or N; and one or two of X1-X3 are independently N or NR8, and the remainder are each independently CR2; each R2 is independently H, alkyl, cyano, halo, heteroaryl, OR4, CONR5R6, SO2R7, etc.; each R8 is independently H or (un)substituted alkyl; R4-R7 are independently H or alkyl; R5 and R6 together with nitrogen to which they are attached are linked to form a ring; are claimed. Example compound III was prepared by cyclocondensation of compound IV with hydrazine hydrate, followed by deprotection in 25% yield over two steps. The invention compounds were evaluated for the LRRK2 inhibitory activity and compound III shows 0.0005 μM of Ki. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Formula: C8H10BrN3O

The Article related to pyrazolopyridine preparation lrrk2 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Formula: C8H10BrN3O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 26, 2013, Chan, Bryan; Estrada, Anthony; Shore, Daniel; Sweeney, Zachary published a patent.Recommanded Product: 4-(2-Bromopyrimidin-4-yl)morpholine The title of the patent was Preparation of pyrazolopyridines for treatment of Parkinsons disease. And the patent contained the following:

The title compounds I or II [R1 = (un)substituted alkyl, monocyclic heterocycloalkyl, bicyclic heterocycloalkyl, cycloalkyl; for I: 1-3 of X1-X4 = N, and the remainder are each CR2; for II: X4 = C or N, and 1-2 of X1-X3 = N and NR8, and the remainder = CR2, such that X1-X4 and N form a heteroaryl; R2 = H, alkyl, CN, halo, etc.; R8 = H, (un)substituted alkyl; with the proviso], useful for the prevention or treatment of a disorder caused by, associated with or accompanied by abnormal kinase activity, preferably abnormal LRRK2 activity, were prepared E.g., a multi-step synthesis of III, starting from 4-chloro-3-iodo-1H-pyrazolo[4,3-c]pyridine, was described. Exemplified compounds I and II were tested for their LRRK2 activity (data given). Pharmaceutical compositions comprising compound I or II, alone or in combination with other therapeutic agent, were disclosed. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Recommanded Product: 4-(2-Bromopyrimidin-4-yl)morpholine

The Article related to pyrazolopyridine preparation lrrk2 inhibitor antiparkinsonian combination chemotherapy, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Recommanded Product: 4-(2-Bromopyrimidin-4-yl)morpholine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On May 25, 2018, Woodring, Jennifer L.; Bachovchin, Kelly A.; Brady, Kimberly G.; Gallerstein, Mitchell F.; Erath, Jessey; Tanghe, Scott; Leed, Susan E.; Rodriguez, Ana; Mensa-Wilmot, Kojo; Sciotti, Richard J.; Pollastri, Michael P. published an article.Category: pyrimidines The title of the article was Corrigendum to “Optimization of physicochemical properties for 4-Anilinoquinazoline inhibitors of trypanosome proliferation” [Eur. J. Med. Chem. 141 (2017) 446-459] [Erratum to document cited in CA167:595582]. And the article contained the following:

In the original publication, the acknowledgments section has information omitted; the correction is provided here. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Category: pyrimidines

The Article related to anilinoquinazoline trypanosome inhibitor antimalarial malaria trypanosomiasis trypanosomicide erratum, Placeholder for records without volume info and other aspects.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 25, 2014, Chan, Bryan; Estrada, Anthony; Shore, Daniel; Sweeney, Zachary published a patent.Formula: C8H10BrN3O The title of the patent was Preparation of pyrazolopyridine compounds as LRRK2 inhibitors. And the patent contained the following:

The invention relates to pyrazolopyridine compounds of formula I and II, or pharmaceutically acceptable salts thereof that are useful for the treatment of the diseases associated with LRRK2. Compounds of formula I and II wherein R1 is (un)substituted alkyl, heterocycloalkyl, cycloalkyl, etc.; for formula I, one, two, or three of X1-X4 are N and the remainder are each independently CR2; or X1-X4 are independently CR2; for formula II, X4 is C or N; and one or two of X1-X3 are independently N or NR8, and the remainder are each independently CR2; each R2 is independently H, alkyl, cyano, halo, heteroaryl, OR4, CONR5R6, SO2R7, etc.; each R8 is independently H or (un)substituted alkyl; R4-R7 are independently H or alkyl; R5 and R6 together with nitrogen to which they are attached are linked to form a ring; are claimed. Example compound III was prepared by cyclocondensation of compound IV with hydrazine hydrate, followed by deprotection in 25% yield over two steps. The invention compounds were evaluated for the LRRK2 inhibitory activity and compound III shows 0.0005 μM of Ki. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Formula: C8H10BrN3O

The Article related to pyrazolopyridine preparation lrrk2 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Formula: C8H10BrN3O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On September 26, 2013, Chan, Bryan; Estrada, Anthony; Shore, Daniel; Sweeney, Zachary published a patent.Recommanded Product: 4-(2-Bromopyrimidin-4-yl)morpholine The title of the patent was Preparation of pyrazolopyridines for treatment of Parkinsons disease. And the patent contained the following:

The title compounds I or II [R1 = (un)substituted alkyl, monocyclic heterocycloalkyl, bicyclic heterocycloalkyl, cycloalkyl; for I: 1-3 of X1-X4 = N, and the remainder are each CR2; for II: X4 = C or N, and 1-2 of X1-X3 = N and NR8, and the remainder = CR2, such that X1-X4 and N form a heteroaryl; R2 = H, alkyl, CN, halo, etc.; R8 = H, (un)substituted alkyl; with the proviso], useful for the prevention or treatment of a disorder caused by, associated with or accompanied by abnormal kinase activity, preferably abnormal LRRK2 activity, were prepared E.g., a multi-step synthesis of III, starting from 4-chloro-3-iodo-1H-pyrazolo[4,3-c]pyridine, was described. Exemplified compounds I and II were tested for their LRRK2 activity (data given). Pharmaceutical compositions comprising compound I or II, alone or in combination with other therapeutic agent, were disclosed. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Recommanded Product: 4-(2-Bromopyrimidin-4-yl)morpholine

The Article related to pyrazolopyridine preparation lrrk2 inhibitor antiparkinsonian combination chemotherapy, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Recommanded Product: 4-(2-Bromopyrimidin-4-yl)morpholine

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 September 8, 2017, Al-Awar, Rima; Zepeda-Velazquez, Carlos Armando; Poda, Gennady; Isaac, Methvin; Uehling, David; Wilson, Brian; Joseph, Babu; Liu, Yong; Subramanian, Pandiaraju; Mamai, Ahmed; Prakesch, Michael; Stille, Julia Kathleen published a patent.Quality Control of 4-(2-Bromopyrimidin-4-yl)morpholine The title of the patent was Preparation of N-aryl heteroarylcarboxamides and arylcarboxamides as inhibitors of WDR5 protein-protein binding. And the patent contained the following:

The application is directed to compounds of formula I and their uses, for example as medicaments for the treatment of diseases, disorders or conditions mediated or treatable by inhibition of binding between WDR5 protein and its binding partners. Compounds of formula I wherein R1 is (un)substituted heterocycloalkyl; R2 is (un)substituted C6-10 aryl and (un)substituted heteroaryl; R3 is (un)substituted C6-10 aryl, (un)substituted heteroaryl and (un)substituted heterocycloalkyl; X1 and X2 are independently CR17 and N; R17 is H, F, C1-6 alkyl and C1-6 fluoroalkyl; A is F, (fluoro)alkyl and (fluoro)alkylene; and pharmaceutically acceptable salts and solvates thereof, are claimed. Example compound II was prepared by multistep procedure (procedure given). The invention compounds were evaluated for their WDR5 protein binding affinity. From the assay, it was determined that compound II exhibited KD value of 0.084 μM. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Quality Control of 4-(2-Bromopyrimidin-4-yl)morpholine

The Article related to aryl heteroarylcarboxamide arylcarboxamide preparation wdr5 protein binding inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Quality Control of 4-(2-Bromopyrimidin-4-yl)morpholine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On April 4, 2019, Duvey, Guillaume; Celanire, Sylvain published a patent.Formula: C8H10BrN3O The title of the patent was Preparation of novel heterocyclic compounds 1-oxo-5,6,7,8-tetrahydro-2H-phthalazine derivatives and analogs, as mGluR7 modulators. And the patent contained the following:

The invention is related to the preparation of compounds I [G = N, CR7; E = N, CR8; provided that at least one of G or E is N; Y = CR9, N; X = (CR5R6)n; R1-9 = independently H, halo, CN, CF3, etc.; wherein any two radicals R1 and R2, R3 and R4, and R5 and R6 may be taken together to form an oxo; wherein optionally any two radicals selected from R1-9 may be taken together to form an (un)substituted 3 to 10-membered non aromatic carbocyclic or heterocyclic ring or a 5 to 10-membered aromatic heterocyclic ring; n = 0-1; Ar1, Ar2 = (un)substituted aryl or heteroaryl], their N-oxide forms , their pharmaceutically acceptable salts and solvates, their optical isomers, racemates, diastereoisomers, enantiomers and tautomers which are modulators of the metabotropic glutamate receptors (mGluR), preferably of the metabotropic glutamate receptor subtype 7 (mGluR7), to pharmaceutical composition comprising such compound and to their use for the treatment of prevention of disorders associated with glutamate dysfunction. Thus, II was prepared by a multi-step synthesis from 1-bromo-2,4-dimethylbenzene and 1,4-dioxaspiro[4.5]decan-8-one. Compounds I are antagonists or neg. allosteric modulators of the mGluR7 as they reduce or inhibit the mGluR7 response induced by glutamate or a mGluR7 agonist, such as L-AP4 as shown in an inositol monophosphate production assay. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).Formula: C8H10BrN3O

The Article related to oxotetrahydrophthalazine cyclopentapyridazinone pyridopyrimidinone preparation metabotropic glutamate receptor mglur7 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Formula: C8H10BrN3O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

On March 27, 2019, Duvey, Guillaume; Celanire, Sylvain published a patent.SDS of cas: 1209459-32-4 The title of the patent was Preparation of novel heterocyclic compounds 1-oxo-5,6,7,8-tetrahydro-2H-phthalazine derivatives and analogs, as mGluR7 modulators. And the patent contained the following:

The invention is related to the preparation of compounds I [G = N, CR7; E = N, CR8; provided that at least one of G or E is N; Y = CR9, N; X = (CR5R6)n; R1-9 = independently H, halo, CN, CF3, etc.; wherein any two radicals R1 and R2, R3 and R4, and R5 and R6 may be taken together to form an oxo; wherein optionally any two radicals selected from R1-9 may be taken together to form an (un)substituted 3 to 10-membered non aromatic carbocyclic or heterocyclic ring or a 5 to 10-membered aromatic heterocyclic ring; n = 0-1; Ar1, Ar2 = (un)substituted aryl or heteroaryl], their N-oxide forms , their pharmaceutically acceptable salts and solvates, their optical isomers, racemates, diastereoisomers, enantiomers and tautomers which are modulators of the metabotropic glutamate receptors (mGluR), preferably of the metabotropic glutamate receptor subtype 7 (mGluR7), to pharmaceutical composition comprising such compound and to their use for the treatment of prevention of disorders associated with glutamate dysfunction. Thus, II was prepared by a multi-step synthesis from 1-bromo-2,4-dimethylbenzene and 1,4-dioxaspiro[4.5]decan-8-one. Compounds I are antagonists or neg. modulators of the mGluR7 as they reduce or inhibit the mGluR7 response induced by glutamate or a mGluR7 agonist, such as L-AP4 as shown in an inositol monophosphate production assay. The experimental process involved the reaction of 4-(2-Bromopyrimidin-4-yl)morpholine(cas: 1209459-32-4).SDS of cas: 1209459-32-4

The Article related to oxotetrahydrophthalazine cyclopentapyridazinone pyridopyrimidinone preparation metabotropic glutamate receptor mglur7 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.SDS of cas: 1209459-32-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia