The disclosure provides, inter alia, alpha-5 beta-1 inhibitors, pharmaceutical compositions comprising alpha-5 beta-1 inhibitors, methods for treating diseases using alpha-5 beta-1 inhibitors, and processes for making alpha-5 beta-1 inhibitors.

The disclosure provides, inter alia, alpha-5 beta-1 inhibitors, pharmaceutical compositions comprising alpha-5 beta-1 inhibitors, methods for treating diseases using alpha-5 beta-1 inhibitors, and processes for making alpha-5 beta-1 inhibitors.

An object of the present invention is to provide a compound having a PDGF receptor kinase inhibitory activity.

Examples of the present invention may include, for example, a compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof.

##STR00001##

The compound of the present invention has an inhibitory activity against the PDGF receptor kinase. In addition, since the compound of the present invention has an inhibitory activity against the PDGF receptor kinase, it is useful as a therapeutic agent for respiratory diseases, cancers, smooth muscle proliferative diseases, vasoproliferative diseases, autoimmune/inflammatory diseases, metabolic diseases, vasoocclusive diseases, and the like.

Disclosed are multivalent, integrin-receptor antagonists that are useful in a variety of therapeutic, prophylactic, and/or diagnostic imaging modalities. In illustrative embodiments, such compounds have been prepared and utilized in the imaging, detection, localization, and/or quantitation of one or more samples of biological interest. Similarly, these compounds, as well as formulations comprising them, find utility in the prevention, treatment, and/or amelioration of one or more symptoms of a disease, abnormal condition, dysfunction, etc., including, for example proliferative diseases such as cancer in affected animals. In certain embodiments, fluorescently- or radio-labeled-non-peptidic, multivalent integrin α.sub.vβ.sub.3 compounds are provided. Compositions including such compounds have been shown to have utility in detecting, localizing, quantitating, and/or imaging integrin α.sub.vβ.sub.3 receptor-expressing cells, including, for example, cancer cells in vitro, in vivo, and/or in situ.

Disclosed are multivalent, integrin-receptor antagonists that are useful in a variety of therapeutic, prophylactic, and/or diagnostic imaging modalities. In illustrative embodiments, such compounds have been prepared and utilized in the imaging, detection, localization, and/or quantitation of one or more samples of biological interest. Similarly, these compounds, as well as formulations comprising them, find utility in the prevention, treatment, and/or amelioration of one or more symptoms of a disease, abnormal condition, dysfunction, etc., including, for example proliferative diseases such as cancer in affected animals. In certain embodiments, fluorescently- or radio-labeled-non-peptidic, multivalent integrin α.sub.vβ.sub.3 compounds are provided. Compositions including such compounds have been shown to have utility in detecting, localizing, quantitating, and/or imaging integrin α.sub.vβ.sub.3 receptor-expressing cells, including, for example, cancer cells in vitro, in vivo, and/or in situ.

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

##STR00001##

Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.

##STR00001##

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.m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO.sub.2—Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)═N—ORc, —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.

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.m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO.sub.2—Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)═N—ORc, —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.

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