C07D239/14

Novel 2,3-Dihydro-1h-imidazo{1,2-a}pyrimidin-5-one and this 1,2,3,4-tetrahydropyrimido{1,2-a}pyrimidin-6-one Derivatives Comprising a Substituted Morpholine, Preparation Thereof and Pharmaceutical Use Thereof

The invention relates to the novel products of formula (I):

##STR00001##

with p, q=0, 1 or 2; R1=phenyl, pyridyl; (CH.sub.2).sub.mRa; alkylene; cycloalkyl; heterocycloalkyl; alkyl; SO.sub.2Rb; CORe; m=1 or 2; Ra=aryl, heteroaryl, CO-cycloalkyl, CO-heterocycloalkyl, CORb, C(Rb)NORc, CO.sub.2Rd, CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF.sub.3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH.sub.3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is

##STR00002##

and the isomer of configuration R,R

##STR00003##

these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.

6-MEMBERED URACIL ISOSTERES
20190270756 · 2019-09-05 ·

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

6-MEMBERED URACIL ISOSTERES
20190270756 · 2019-09-05 ·

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

NOVEL COMPOUND AS PROTEIN KINASE INHIBITORS
20240150325 · 2024-05-09 · ·

The present invention relates to a novel compound as protein kinase inhibitors.

Synthesis of cyclocreatine and analogs thereof

Provided herein is a process and intermediates for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, using cyanamide in the reaction. ##STR00001##

Synthesis of cyclocreatine and analogs thereof

Provided herein is a process and intermediates for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, using cyanamide in the reaction. ##STR00001##

Inhibitors of creatine transport and uses thereof
10308597 · 2019-06-04 · ·

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

Inhibitors of creatine transport and uses thereof
10308597 · 2019-06-04 · ·

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

2,3-dihydro-1H-imidazo{1,2-a}pyrimidin-5-one and this 1,2,3,4-tetrahydropyrimido{1,2-a}pyrimidin-6-one derivatives comprising a substituted morpholine, preparation thereof and pharmaceutical use thereof

The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; (CH.sub.2).sub.mRa; alkylene; cycloalkyl; heterocycloalkyl; alkyl; SO.sub.2 Rb; CORe; m=1 or 2; Ra=aryl, heteroaryl, CO-cycloalkyl, CO-heterocycloalkyl, CORb, C(Rb)NORc, CO 2 Rd, CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH.sub.3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments. ##STR00001##

2,3-dihydro-1H-imidazo{1,2-a}pyrimidin-5-one and this 1,2,3,4-tetrahydropyrimido{1,2-a}pyrimidin-6-one derivatives comprising a substituted morpholine, preparation thereof and pharmaceutical use thereof

The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; (CH.sub.2).sub.mRa; alkylene; cycloalkyl; heterocycloalkyl; alkyl; SO.sub.2 Rb; CORe; m=1 or 2; Ra=aryl, heteroaryl, CO-cycloalkyl, CO-heterocycloalkyl, CORb, C(Rb)NORc, CO 2 Rd, CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH.sub.3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments. ##STR00001##