Patent classifications
C07D233/46
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.
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.
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##
Substituted pyrazoles as inhibitors of fibroblast growth factor receptor
An indole derivative as expressed by Formula (I), a preparation method thereof, a pharmaceutical salt, and use thereof as a therapeutic agent, especially as a FGFR inhibitor. Each substituent in Formula (I) has identical definition as specified in the specification. ##STR00001##
Substituted pyrazoles as inhibitors of fibroblast growth factor receptor
An indole derivative as expressed by Formula (I), a preparation method thereof, a pharmaceutical salt, and use thereof as a therapeutic agent, especially as a FGFR inhibitor. Each substituent in Formula (I) has identical definition as specified in the specification. ##STR00001##
Bis-cyclic guanidines as antibacterial agents
Provided are novel bis-cyclic guanidine compounds, and the use thereof for treating bacterial infection.