C07D401/06

Novel Heterocyclic Derivatives with Cardiomyocyte Proliferation Activity for Treatment of Heart Diseases

Provided are novel heterocyclic derivatives with cardiomyocyte proliferation activity for treatment of heart diseases. Specifically, provided are the compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, preparation method thereof, application thereof and pharmaceutical composition useful for treatment of heart diseases.

HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

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HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

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Benzimidazole Derivatives

The invention relates to a compound of formula (I) wherein R.sup.1-R.sup.3 are as defined in the description and in the claims The compound of formula (I) can be used as a medicament.

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Benzimidazole Derivatives

The invention relates to a compound of formula (I) wherein R.sup.1-R.sup.3 are as defined in the description and in the claims The compound of formula (I) can be used as a medicament.

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AZASPIROCYCLES AS MONOACYLGLYCEROL LIPASE MODULATORS

Azaspirocycle compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions:

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wherein X, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, m, n, o, and p are defined herein.

AZASPIROCYCLES AS MONOACYLGLYCEROL LIPASE MODULATORS

Azaspirocycle compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions:

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wherein X, R.sup.1, R.sup.2a, R.sup.2b, R.sup.3, m, n, o, and p are defined herein.

Indole compounds and analogues thereof

Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula I, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity. ##STR00001##

Indole compounds and analogues thereof

Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula I, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity. ##STR00001##

METHODS AND COMPOSITIONS OF INHIBITING DCN1-UBC12 INTERACTION

In one aspect, the invention relates to substituted 1-phenyl-3-(piperidin-4-yl)urea analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the DCN1-UBC12 interaction inhibitors of DCN1-mediated cullin-RING ligase activity, methods of making same, pharmaceutical compositions comprising same, methods of treating disorders using the disclosed compounds and compositions, methods of treating disorders associated with a DCN1-UBC12 interaction dysfunction, methods of treating disorders associated with a DCN1-mediated cullin-RING ligase activity dysfunction, methods of male contraception comprising the disclosed compounds and compositions, and kits comprising the disclosed compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.