Patent classifications
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
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
6-MEMBERED URACIL ISOSTERES
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
NOVEL COMPOUND AS PROTEIN KINASE INHIBITORS
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
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
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##