The present invention relates to N-(2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-5-yl)-4-quinazolinamine and N-(2,3-dihydro-1H-indol-5-yl)-4-quinazolinamine derivatives of Formula (I) ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and A have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors of PERK. The invention further relates to processes for preparing such compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

The present invention relates to N-(2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-5-yl)-4-quinazolinamine and N-(2,3-dihydro-1H-indol-5-yl)-4-quinazolinamine derivatives of Formula (I) ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and A have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors of PERK. The invention further relates to processes for preparing such compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

The present invention relates to a graphene nanoribbon, comprising a repeating unit which comprises at least one modification, wherein the modification is selected from a heteroatomic substitution, a vacancy, a sp.sup.3 hybridization, a Stone-Wales defect, an inverse Stone-Wales defect, a hexagonal sp.sup.2 hybridized carbon network ring size modification, and any combination thereof.

The present invention relates to a graphene nanoribbon, comprising a repeating unit which comprises at least one modification, wherein the modification is selected from a heteroatomic substitution, a vacancy, a sp.sup.3 hybridization, a Stone-Wales defect, an inverse Stone-Wales defect, a hexagonal sp.sup.2 hybridized carbon network ring size modification, and any combination thereof.

Disclosed are small molecule antagonists of 47 integrin, and methods of using them to treat a number of specific diseases or conditions.

ANT-ligands having a substituted nitrogeneous heterocycle A wherein A is a substituted pyrimidinone of formula I ##STR00001##
wherein R1 is (CH2)n-COOH; (CH2)n-COOR; (CH2)n-CONHR; (CH2)n-CON(R, R); (CH2)n-OH; (CH2)n-OR; (CH2)n-OAr; (CH2)n-C(R,R)(CH2)n-OH, R and R, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het. representing an heterocyclic radical with one or several hetero atoms selected between N, S and O, said phenyl or heterocycle being optionally substituted by one or several atoms, groups or radicals selected from halogen atoms such as Cl, Br, I, or halogenated groups such as CCl3 or CF3; one or several OH, OR, COOH or COOR groups; a phenyl; a linear or branched C1-C12 alkyl radical; NHCOR; or CN; said groups occupying the same or different positions on the phenyl or heterocyclic radical; a linear or branched C1-C12 alkyl radical; a linear or branched C2-C12 alkylene radical; (CH2)n-C3-C6 cycloalkyl radical; (CH2)n Ar or (CH2)n-Het.; (CH2)n-NHCOR; (CH2)n-NH2; (CH2)n-N(R,R); (CH2)n-NHCOOH; (CH2)n-NHCOOR; NH(CH2)n-COOH; NH(CH2)n-COOR; R2 is (CH2)n-Ar, Ar being such as above defined and being optionally substituted such as above defined; a linear or branched C1-C12 alkyl or C2-C12 alkenyl radical, (CH2)n-OH; (CH2)n-OR; (CH2)n-CO-Het; (CH2)n-NHCOR; (CH2)n-NH2; (CH2)n-N(R,R); (CH2)n-COOH; (CH2)n-COOR; a linear or branched C1-C12 alkyl radical; (CH2)n-C(R)CHC(R)CH2; R3 forms a phenyl or an heterocyclic condensed group with the two adjacent carbons of the pyrazinone residue, said condensed group being optionally substituted such as above defined for Ar and Het.; and/or condensed to a cyclohexyl or oxanyl group, in turn optionally substituted such as above defined for Ar; n is 0 or an integer from 1 to 5; or A is a substituted pyrimidine of formula II ##STR00002##
wherein R4 is a CONHAr radical, optionally substituted such as above defined; R5 forms a phenyl or heterocyclic group condensed to the two adjacent carbon groups of the pyrazine residue, said phenyl or heterocyclic group being optionally substituted such as above defined, and
Ar being such as above defined with respect to formula I
or A is a substituted pyridine group of formula III ##STR00003##
wherein,
Ar and R2 are as above defined with respect to formula I.

Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Provided are prophylactic and therapeutic methods of treatment of subjects for the purpose of inhibiting vaso-occlusive events, including embolism, by administering agents, including anagrelide and anagrelide derivatives, which reduce the number of circulating platelets to low normal or to below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.

Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Provided are novel compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are inhibitors of CD73 and are useful in the treatment of cancer.