A61K31/4704

METHODS AND COMPOSITIONS RELATING TO STEROID HORMONE RECEPTOR-DEPENDENT PROLIFERATIVE DISORDERS
20230102174 · 2023-03-30 ·

Pharmaceutical compositions are provided according to aspects of the present disclosure which include a compound having chemical structural formula I:

##STR00001##

where R.sub.1 is selected from the group consisting of: an alkyl group, a heteroalkyl group, an aryl group, a heteroaryl group, an alkenyl group, a heteroalkenyl group, an alkynyl group, a heteroalkynyl group, a cycloalkyl group, a hetercycloalkyl group, an alkylcycloalkyl group, a heteroalkyl cycloalkyl group, an aralkyl group, a heteroaralkyl group, an alkoxy group, a polar group, an ester and a charged group; a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof; and/or a pharmaceutically acceptable salt thereof; where R.sub.4′ is H or an alkoxy group; where both R.sub.5 and R.sub.3′ are OH, or where one or both OH groups is optionally modified as a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof; and/or a deuterated form thereof; and/or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.

METHODS AND COMPOSITIONS RELATING TO STEROID HORMONE RECEPTOR-DEPENDENT PROLIFERATIVE DISORDERS
20230102174 · 2023-03-30 ·

Pharmaceutical compositions are provided according to aspects of the present disclosure which include a compound having chemical structural formula I:

##STR00001##

where R.sub.1 is selected from the group consisting of: an alkyl group, a heteroalkyl group, an aryl group, a heteroaryl group, an alkenyl group, a heteroalkenyl group, an alkynyl group, a heteroalkynyl group, a cycloalkyl group, a hetercycloalkyl group, an alkylcycloalkyl group, a heteroalkyl cycloalkyl group, an aralkyl group, a heteroaralkyl group, an alkoxy group, a polar group, an ester and a charged group; a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof; and/or a pharmaceutically acceptable salt thereof; where R.sub.4′ is H or an alkoxy group; where both R.sub.5 and R.sub.3′ are OH, or where one or both OH groups is optionally modified as a pharmaceutically acceptable hydrolysable, or enzymatically cleavable, prodrug form thereof; and/or a deuterated form thereof; and/or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.

Compounds for treatment of PD-L1 diseases

Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) ##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.3, R.sup.3a, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and the subscript n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Compounds for treatment of PD-L1 diseases

Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) ##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.3, R.sup.3a, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and the subscript n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

TASQUINIMOD OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF FOR USE IN COMBINATION THERAPY

A combination comprising tasquinimod, or a pharmaceutically acceptable salt thereof, and at least one further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody, for use as a in the treatment of multiple myeloma. A kit comprising tasquinimod and a package insert with instructions for using tasquinimod in combination with at least one further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody, to treat multiple myeloma in an individual. Tasquinimod for use in the treatment of multiple myeloma, in combination with a further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody.

TASQUINIMOD OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF FOR USE IN COMBINATION THERAPY

A combination comprising tasquinimod, or a pharmaceutically acceptable salt thereof, and at least one further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody, for use as a in the treatment of multiple myeloma. A kit comprising tasquinimod and a package insert with instructions for using tasquinimod in combination with at least one further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody, to treat multiple myeloma in an individual. Tasquinimod for use in the treatment of multiple myeloma, in combination with a further compound selected from a proteasome inhibitor, an immunomodulatory imide, and an antibody.

DRUGGABLE TARGET TO TREAT RETINAL DEGENERATION

This invention relates to novel method of treating or ameliorating a retinal disease or disorder or retinal degradation in a subject and a novel method of restoring retinal pigment epithelium cell compromising the administration of a one or more compounds which modulate Nox4, formation of radical oxygen species, serine protease, a dopamine receptor, NF-kB, mTOR, AMPK, RPE epithelial to mesenchymal transition, RPE dedifferentiation, or one or more Rho GTPases; and kits for administration of the methods.

Compounds for treatment of eye diseases associated with excessive vascularisation

The present invention relates to compounds for treatment of a disease or disorder associated with excessive vascularisation of the eye, such as for instance corneal neovascularisation, neovascularisation of the iris, neovascularisation of the ciliary body, corneal pannus, choroidal neovascularisation, retinal neovascularisation, wet age-related macular degeneration, proliferative diabetic retinopathy, retinopathy of prematurity, and ischemic retinopathy.

Compounds for treatment of eye diseases associated with excessive vascularisation

The present invention relates to compounds for treatment of a disease or disorder associated with excessive vascularisation of the eye, such as for instance corneal neovascularisation, neovascularisation of the iris, neovascularisation of the ciliary body, corneal pannus, choroidal neovascularisation, retinal neovascularisation, wet age-related macular degeneration, proliferative diabetic retinopathy, retinopathy of prematurity, and ischemic retinopathy.

Compounds for treatment of eye diseases associated with excessive vascularisation

The present invention relates to compounds for treatment of a disease or disorder associated with excessive vascularisation of the eye, such as for instance corneal neovascularisation, neovascularisation of the iris, neovascularisation of the ciliary body, corneal pannus, choroidal neovascularisation, retinal neovascularisation, wet age-related macular degeneration, proliferative diabetic retinopathy, retinopathy of prematurity, and ischemic retinopathy.