A61K31/4747

THERAPEUTIC COMPOUNDS AND USES THEREOF

Provided herein are compounds of formula I:

##STR00001##

and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.

THERAPEUTIC COMPOUNDS AND USES THEREOF

Provided herein are compounds of formula I:

##STR00001##

and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.

COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF HIF2-alpha AND THEIR METHODS OF USE

The present invention relates to compounds of formula (I)

##STR00001##

or a pharmaceutically acceptable salt form thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of disease.

COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF HIF2-alpha AND THEIR METHODS OF USE

The present invention relates to compounds of formula (I)

##STR00001##

or a pharmaceutically acceptable salt form thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of disease.

Tetrahydroisoquinoline derivatives

Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

TRICYCLIC AKR1C3 DEPENDENT KARS INHIBITORS

The present invention relates to novel tricyclic compounds that are AKR1C3 dependent KARS inhibitor, processes for their preparation, pharmaceutical compositions, and medicaments containing them, and their use in diseases and disorders mediated by an AKR1C3 dependent KARS inhibitor.

TRICYCLIC AKR1C3 DEPENDENT KARS INHIBITORS

The present invention relates to novel tricyclic compounds that are AKR1C3 dependent KARS inhibitor, processes for their preparation, pharmaceutical compositions, and medicaments containing them, and their use in diseases and disorders mediated by an AKR1C3 dependent KARS inhibitor.

DIHYDRO-SPIRO[INDOLINE-3:1'-iSOQUINOLIN]-2-ONES AS ANTIMALARIAL AGENTS

The present invention is directed to the antimalarial activity of various 3′,4′-dihydro-2′H-spiro[indoline-3:1′-isoquinolin]-2-ones and related compounds. The present invention is also directed to the use of these compounds as antimalarial agents, in the treatment of malaria. In addition, the invention relates to pharmaceutical compositions comprising one or more of these compounds alone or in combination with other therapeutic agents for the treatment and/or radical cure of severe acute malaria. The invention is also directed to the use of these agents alone and in combination with other agents in malaria prophylaxis, for example, by inhibiting and/or reducing the likelihood of a malaria infection.

DIHYDRO-SPIRO[INDOLINE-3:1'-iSOQUINOLIN]-2-ONES AS ANTIMALARIAL AGENTS

The present invention is directed to the antimalarial activity of various 3′,4′-dihydro-2′H-spiro[indoline-3:1′-isoquinolin]-2-ones and related compounds. The present invention is also directed to the use of these compounds as antimalarial agents, in the treatment of malaria. In addition, the invention relates to pharmaceutical compositions comprising one or more of these compounds alone or in combination with other therapeutic agents for the treatment and/or radical cure of severe acute malaria. The invention is also directed to the use of these agents alone and in combination with other agents in malaria prophylaxis, for example, by inhibiting and/or reducing the likelihood of a malaria infection.

DIHYDRO-SPIRO[INDOLINE-3:1'-iSOQUINOLIN]-2-ONES AS ANTIMALARIAL AGENTS

The present invention is directed to the antimalarial activity of various 3′,4′-dihydro-2′H-spiro[indoline-3:1′-isoquinolin]-2-ones and related compounds. The present invention is also directed to the use of these compounds as antimalarial agents, in the treatment of malaria. In addition, the invention relates to pharmaceutical compositions comprising one or more of these compounds alone or in combination with other therapeutic agents for the treatment and/or radical cure of severe acute malaria. The invention is also directed to the use of these agents alone and in combination with other agents in malaria prophylaxis, for example, by inhibiting and/or reducing the likelihood of a malaria infection.