A61K31/4025

DIFLUOROLACTAM COMPOUNDS AS EP4 RECEPTOR-SELECTIVE AGONISTS FOR USE IN THE TREATMENT OF EP4-MEDIATED DISEASES AND CONDITIONS

Disclosed herein are compounds of formula (I)

##STR00001##

and therapeutic methods of treatment with compounds of formula (I), wherein L.sup.1, L.sup.2, L.sup.4, R.sup.1, R.sup.4, R.sup.5, R.sup.6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.

DIFLUOROLACTAM COMPOUNDS AS EP4 RECEPTOR-SELECTIVE AGONISTS FOR USE IN THE TREATMENT OF EP4-MEDIATED DISEASES AND CONDITIONS

Disclosed herein are compounds of formula (I)

##STR00001##

and therapeutic methods of treatment with compounds of formula (I), wherein L.sup.1, L.sup.2, L.sup.4, R.sup.1, R.sup.4, R.sup.5, R.sup.6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.

Repurposcins: targeted inhibitors of mitochondrial biogenesis for eradicating cancer stem cells

A therapeutic compound having intrinsic anti-mitochondrial properties may be chemically modified to target the compound to mitochondria, and the resulting “repurposcins” may have enhanced anti-cancer properties, among other advantageous properties. For example, a repurposcin may be used to treat and/or prevent tumor recurrence, metastasis, drug resistance, and/or radiotherapy resistance. Described herein are repurposcin compounds and pharmaceutical compositions that have been developed according to the present approach. Also described are methods for identifying and developing repurposcins, methods of using repurposcins to target cancer stem cells, and compositions for treating cancer containing one or more repurposcins as the active ingredient.

Repurposcins: targeted inhibitors of mitochondrial biogenesis for eradicating cancer stem cells

A therapeutic compound having intrinsic anti-mitochondrial properties may be chemically modified to target the compound to mitochondria, and the resulting “repurposcins” may have enhanced anti-cancer properties, among other advantageous properties. For example, a repurposcin may be used to treat and/or prevent tumor recurrence, metastasis, drug resistance, and/or radiotherapy resistance. Described herein are repurposcin compounds and pharmaceutical compositions that have been developed according to the present approach. Also described are methods for identifying and developing repurposcins, methods of using repurposcins to target cancer stem cells, and compositions for treating cancer containing one or more repurposcins as the active ingredient.

ANTIBODY DRUG CONJUGATES (ADCS) AND ANTIBODY PRODRUG CONJUGATES (APDCS) WITH ENZYMATICALLY CLEAVABLE GROUPS

The present invention relates to novel binder-prodrug conjugates (APDCs) where binders are conjugated with inactive precursor compounds of kinesin spindle protein inhibitors, and to antibody-drug conjugates ADCs and to processes for producing these APDCs and ADCs.

ANTIBODY DRUG CONJUGATES (ADCS) AND ANTIBODY PRODRUG CONJUGATES (APDCS) WITH ENZYMATICALLY CLEAVABLE GROUPS

The present invention relates to novel binder-prodrug conjugates (APDCs) where binders are conjugated with inactive precursor compounds of kinesin spindle protein inhibitors, and to antibody-drug conjugates ADCs and to processes for producing these APDCs and ADCs.

INHIBITORS OF HEPATITIS C VIRUS REPLICATION

The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

##STR00001##

INHIBITORS OF HEPATITIS C VIRUS REPLICATION

The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

##STR00001##

HETEROCYCLIC COMPOUND AND USE THEREOF

The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.

##STR00001##

THERAPEUTICS FOR THE TREATMENT OF GLAUCOMA

The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a K.sub.ATP channel to reduce an intraocular pressure.