C07C275/16

Heterodimers of Glutamic Acid
20230095637 · 2023-03-30 ·

Compounds of Formula (Ia)

##STR00001##

wherein R is a C.sub.6-C.sub.12 substituted or unsubstituted aryl, a C.sub.6-C.sub.12 substituted or unsubstituted heteroaryl, a C.sub.1-C.sub.6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O).sub.2, C(O).sub.2 (CH2)p Y is C(O), O, NR′, S, S(O).sub.2, C(O).sub.2, (CH2)p Z is H or C.sub.1-C.sub.4 alkyl, R′ is H, C(O), S(O).sub.2, C(O).sub.2, a C.sub.6-C.sub.12 substituted or unsubstituted aryl, a C.sub.6-C.sub.12 substituted or unsubstituted heteroaryl or a C.sub.1-C.sub.6 substituted of unsubstituted when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C.sub.6-C.sub.12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition, Radiolabels can be incorporated into the structure through a variety of prosthetic, groups attached at the X amino acid side chain via a carbon or hetero atom linkage.

Heterodimers of Glutamic Acid
20230095637 · 2023-03-30 ·

Compounds of Formula (Ia)

##STR00001##

wherein R is a C.sub.6-C.sub.12 substituted or unsubstituted aryl, a C.sub.6-C.sub.12 substituted or unsubstituted heteroaryl, a C.sub.1-C.sub.6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O).sub.2, C(O).sub.2 (CH2)p Y is C(O), O, NR′, S, S(O).sub.2, C(O).sub.2, (CH2)p Z is H or C.sub.1-C.sub.4 alkyl, R′ is H, C(O), S(O).sub.2, C(O).sub.2, a C.sub.6-C.sub.12 substituted or unsubstituted aryl, a C.sub.6-C.sub.12 substituted or unsubstituted heteroaryl or a C.sub.1-C.sub.6 substituted of unsubstituted when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C.sub.6-C.sub.12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition, Radiolabels can be incorporated into the structure through a variety of prosthetic, groups attached at the X amino acid side chain via a carbon or hetero atom linkage.

UREA COMPOUND FOR ANTAGONIZING LPA1 RECEPTOR

The present invention provides a compound represented by formula (I) or a pharmaceutically acceptable salt thereof which has the effect of antagonizing the LPA1 receptor.

UREA COMPOUND FOR ANTAGONIZING LPA1 RECEPTOR

The present invention provides a compound represented by formula (I) or a pharmaceutically acceptable salt thereof which has the effect of antagonizing the LPA1 receptor.

CALPAIN-2 INHIBITOR COMPOUNDS AND METHODS OF TREATMENT
20230091121 · 2023-03-23 ·

Compounds of Formula (I) or (X) are provided including for treatment of disorders such as a disorder or symptom associated with neuronal cell death. In one aspect, compounds which are selective inhibitors of calpain-2 are provided. Preferred compounds can be useful to treat acute neurodegeneration.

LABELING PRECURSORS WITH SQUARIC ACID COUPLING

The invention relates to a marking precursor incorporating a chelator or fluorination group for radiolabelling with .sup.44Sc, .sup.47Sc, .sup.55Co, .sup.62Cu, .sup.64Cu, .sup.67Cu, .sup.66Ga, .sup.67Ga, .sup.68Ga, .sup.89Zr, .sup.86Y, .sup.90Y, .sup.90Nb, .sup.99mTc, .sup.111In, .sup.135Sm, .sup.140Pr, .sup.159Gd, .sup.149Tb, .sup.160Tb, .sup.161Tb, .sup.165Er, .sup.166Dy, .sup.166Ho, .sup.175Yb, .sup.177Lu, .sup.186Re, .sup.188Re, .sup.213Bi and .sup.225Ac or with .sup.18F, .sup.131I or .sup.211At, and one or two biological targeting vectors which are coupled to the chelator or fluorinating group via one or more squaric acid groups.

Inhibitors of integrin alpha 2 beta 1 and methods of use

Disclosed herein, inter alia, are inhibitors of integrin alpha 2 beta 1 and methods of using the same.

Linkers for antibody drug conjugates

In one aspect, the present disclosure provides compounds of the formula (I): wherein the variables are as defined herein. In another aspect, the present disclosure provides compounds of the formula (V): wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure provides antibody drug conjugates comprising compounds of the present disclosure. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds and anti-body drug conjugates disclosed herein. ##STR00001##

Inhibitors of alpha 2 beta 1 integrin and methods of use thereof

Disclosed herein, inter alia, are inhibitors of alpha 2 beta 1 integrin and methods of using the same.

DOUBLE TARGETED CONSTRUCTS TO AFFECT TUMOR KILL

The present technology is directed to compounds, compositions, medicaments, and methods related to the treatment of cancers expressing PSMA. The compounds are of Formulas I & II

##STR00001##

or pharmaceutically acceptable salts thereof. The present technology is especially well-suited for use in treating prostate cancer.