31402-54-7

Usage

Uses

Used in Pharmaceutical Industry:
5-BROMO-2-(METHYLAMINO)PYRIMIDINE is used as a building block for the synthesis of pharmaceuticals, contributing to the development of new drugs and therapeutic agents. Its unique structure and reactivity allow for the creation of diverse bioactive molecules with potential medicinal applications.
Used in Agrochemical Industry:
5-BROMO-2-(METHYLAMINO)PYRIMIDINE is utilized as a key component in the synthesis of agrochemicals, such as pesticides and herbicides. Its incorporation into these compounds can enhance their effectiveness in controlling pests and weeds, thereby improving crop yields and agricultural productivity.
Used in Chemical Research:
5-BROMO-2-(METHYLAMINO)PYRIMIDINE serves as a valuable research tool in chemical studies. Its versatile reactivity and potential for functionalization make it an ideal candidate for exploring new chemical reactions and mechanisms, furthering our understanding of organic chemistry.
Used in Bioactive Molecule Development:
5-BROMO-2-(METHYLAMINO)PYRIMIDINE is employed in the development of bioactive molecules, which have the potential to interact with biological systems and exhibit therapeutic or other beneficial effects. Its unique structure and properties can be leveraged to design and synthesize novel compounds with specific biological activities.

InChI:InChI=1/C5H6BrN3/c6-4-2-8-5(1-7)9-3-4/h2-3H,1,7H2

Upstream product

• 931-61-3 N-methylpyrimidin-2-amine 
• 593-51-1 methylamine hydrochloride 
• 32779-36-5 5-Bromo-2-chloropyrimidine 
• 7752-82-1 5-bromo-2-aminopyrimidine 
• 74-88-4 methyl iodide 
• 74-89-5 methylamine 

Downstream Products

• 904326-88-1 methyl[5-(4,4,5,5-tetramethyl(1,3,2-dioxaborolan-2-yl))pyrimidin-2-yl]amine 
• 1172612-45-1 N-methyl-5-(m-tolylethynyl)pyrimidin-2-amine 
• 1172612-43-9 methyl-(5-phenylethynyl-pyrimidin-2-yl)-amine 
• 884603-50-3 5-ethynyl-N-methylpyrimidin-2-amine 
• 1407999-88-5 C₂₈H₃₀F₃N₉O 
• 1594728-81-0 5-(3-aminophenyl)-N-methylpyrimidin-2-amine 
• 1581701-20-3 methyl 2-(methylamino)pyrimidine-5-carboxylate 
• 5388-21-6 2-(methylamino)pyrimidine-5-carboxylic acid 
• 1581701-26-9 N-(2-methyl-5-((4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)carbamoyl)phenyl)-2-(methylamino)pyrimidine-5-carboxamide 
• 1360552-10-8 C₁₇H₁₈N₄ 
• 1257628-58-2 4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-(2-(2-(methylamino)pyrimidin-5-yl)ethynyl)benzamide 
• 1360551-14-9 2-[4-(3-{(R)-1-cyclopropyl-1-[4-(2-methylamino-pyrimidin-5-yl)-phenyl]-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide 

Relevant academic research and scientific papers

NOVEL COMPOUNDS

Described herein are compounds that are inhibitors of p21-activated kinases (PAKS). In particular, the compounds described herein are demonstrated to be selective PAK4 inhibitors. The compounds described herein are also demonstrated to reduce the expression of key immune checkpoint molecules, such as PD-1 and CHEK2. Also described herein are pharmaceutical compositions containing such compounds, methods for using such compounds in the treatment of cancers, more specifically, the treatment of pancreatic and lung cancers, and to related uses.

PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH ZINC BINDING MOIETY

PROBLEM TO BE SOLVED: To provide phosphoinositide 3-kinase inhibitors with a zinc binding moiety. SOLUTION: There is provided a compound represented by formula (I) in the figure. (X is S, O or the like; Y is CH, N or the like; G1 is optionally substituted N or the like; R1 and R2 are each independently H or the like; C is a substituted heterocycle or the like; B is a linear alkyl or the like; Ra and Rb together with the nitrogen atom coupled to them are morpholino or the like; G2 is an indazole ring or the like; q, r and s are independently from 0 to 1, provided that at least one of them is 1; t is from 0 to 1; n is from 0 to 4; and p is from 0 to 2.) COPYRIGHT: (C)2016,JPOandINPIT

TREATMENT OF CANCERS HAVING K-RAS MUTATIONS

The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.

METHOD OF INHIBITING HAMARTOMA TUMOR CELLS

Dimorpholinopyrimidines are useful for inhibiting growth or proliferation of hamartoma tumor cells. Because the Dimorpholinopyrimidines inhibit the growth and proliferation of hamartoma tumor cells they are also useful in treating PTEN hamartoma tumor syndromes. The therapeutic and prophylactic treatments provided by this invention are practiced by administering to a patient in need thereof an amount of a compound of dimorpholinopyrimidine derivative that is effective to inhibit growth or proliferation of the hamartoma tumor cells.

Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl) benzamide derivatives as potent pan Bcr-Abl inhibitors including the threonine315←isoleucine315 mutant

A series of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives were designed and synthesized as new Bcr-Abl inhibitors by using combinational strategies of bioisosteric replacement, scaffold hopping, and conformational constraint. The compounds displayed significant inhibition against a broad spectrum of Bcr-Abl mutants including the gatekeeper T315I and p-loop mutations, which are associated with disease progression in CML. The most potent compounds 6q and 6qo strongly inhibited the kinase activities of Bcr-AblWT and Bcr-AblT315I with IC50 values of 0.60, 0.36 and 1.12, 0.98 nM, respectively. They also potently suppressed the proliferation of K562, KU812 human CML cells, and a panel of murine Ba/F3 cells ectopically expressing either Bcr-AblWT or any of a panel of other Bcr-Abl mutants that have been shown to contribute to clinical acquired resistance, including Bcr-AblT315I, with IC50 values in low nanomolar ranges. These compounds may serve as lead compounds for further development of new Bcr-Abl inhibitors capable of overcoming clinical acquired resistance against imatinib.

TREATMENT OF CANCERS HAVING K-RAS MUTATIONS

The present invention provides a method of treating a cancer associated with a K- ras mutation in a subject in need thereof. The method comprises the steps of (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) adminsiterign to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.

Synthesis and in vitro and in vivo evaluation of phosphoinositide-3-kinase inhibitors

Phospoinositide-3-kinases (PI3K) are important oncology targets due to the deregulation of this signaling pathway in a wide variety of human cancers. A series of 2-morpholino, 4-substituted, 6-(3-hydroxyphenyl) pyrimidines have been reported as potent inh

MORPHOLINOPURINE DERIVATIVES

There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: wherein R1, R2, R3, R4, Ra, Rb, Rc, and X each have the same meaning as defined in the specification.

NEW COMPOUNDS

The present invention encompasses compounds of general formula (1), wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use

TRIAZINE COMPOUNDS AS KINASE INHIBITORS

The present invention relates to triazine compounds that are useful as kinase inhibitors. More particularly, the present invention relates to morpholino substituted triazines, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with mTOR kinases or PI3 kinases. The compounds are of the formula (I)