C07D235/14

Small molecule CD4 mimetics and uses thereof

The invention provides for compounds of formula I: wherein Z is absent or (CR.sub.AR.sub.B).sub.nW; each RA and RB is independently (i) H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, haloalkyl, each of which may be optionally substituted; (ii) OH, ORc, NH2, NHR.sub.c, NR.sub.cR.sub.c, SH, S(O).sub.mR.sub.c; or (iii) R.sub.A and R.sub.B together form C(O); W is absent, C(O), C(O)O, C(O)NR.sub.cR.sub.c, O, S(O).sub.m, or NR.sub.cR.sub.c; Y is an optionally substituted heterocyclic, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted aryl, or NR.sub.XR.sub.Y; wherein R.sub.x and R.sub.y are each independently H, alkyl or aryl; X.sup.1 is selected from the group consisting of halogen, methyl, and hydroxyl; X2 is a halogen; each R.sub.c is independently alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, each of which may be optionally substituted; m is O, 1, or 2; and n is 1, 2, 3, 4, 5, or 6; and pharmaceutically acceptable salts thereof. ##STR00001##

Small molecule CD4 mimetics and uses thereof

The invention provides for compounds of formula I: wherein Z is absent or (CR.sub.AR.sub.B).sub.nW; each RA and RB is independently (i) H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, haloalkyl, each of which may be optionally substituted; (ii) OH, ORc, NH2, NHR.sub.c, NR.sub.cR.sub.c, SH, S(O).sub.mR.sub.c; or (iii) R.sub.A and R.sub.B together form C(O); W is absent, C(O), C(O)O, C(O)NR.sub.cR.sub.c, O, S(O).sub.m, or NR.sub.cR.sub.c; Y is an optionally substituted heterocyclic, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted aryl, or NR.sub.XR.sub.Y; wherein R.sub.x and R.sub.y are each independently H, alkyl or aryl; X.sup.1 is selected from the group consisting of halogen, methyl, and hydroxyl; X2 is a halogen; each R.sub.c is independently alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, each of which may be optionally substituted; m is O, 1, or 2; and n is 1, 2, 3, 4, 5, or 6; and pharmaceutically acceptable salts thereof. ##STR00001##

SPECIFIC INHIBITORS OF METHIONYL-TRNA SYNTHETASE

The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS.

SPECIFIC INHIBITORS OF METHIONYL-TRNA SYNTHETASE

The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS.

Benzenesulfonyl-Asymmetric Ureas and Medical Uses Thereof
20170275301 · 2017-09-28 ·

Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.

Benzenesulfonyl-Asymmetric Ureas and Medical Uses Thereof
20170275301 · 2017-09-28 ·

Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.

Alpha-cinnamide compounds and compositions as HDAC8 inhibitors

The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.

Alpha-cinnamide compounds and compositions as HDAC8 inhibitors

The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.

Analgesic compounds

Disclosed herein are compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It), methods of synthesizing compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It), and methods of using compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It) as an analgesic.

Analgesic compounds

Disclosed herein are compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It), methods of synthesizing compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It), and methods of using compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It) as an analgesic.