Compounds and methods for the treatment of dermal and ocular disorders
AssigneeAzura Ophthalmics Ltd.
InventorsIan HOLMES, Yair ALSTER, Charles BOSWORTH, Omer RAFAELI, Marc GLEESON, Luba LITINETSKY
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AssigneeAzura Ophthalmics Ltd.
InventorsIan HOLMES, Yair ALSTER, Charles BOSWORTH, Omer RAFAELI, Marc GLEESON, Luba LITINETSKY
Estimating the term…
Described herein are compositions and methods for the treatment or prevention of dermal or ocular surface disorders, such as those associated with bacterial and/or parasitic infections. Bacterial and/or parasitic infections include mites (e.g., demodex), worms, protozoa (e.g., amoeba (e.g., acanthamoeba or cryptosporidiosis)), giardia, trichomonas, or chlamydia. Said compositions and methods comprise compounds which demonstrate immunological, keratolytic, anti-histamine, anti-inflammatory, and/or other desirable activities. Topical administration of said compositions to the eyelid margin or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.
A compound having a structure represented by Formula (I):
The compound of any one of the preceding claims, wherein the H1 antagonist is an ethylenediamine (H1 antagonist), ethanolamine (H1 antagonist), alkylamine (H1 antagonist), piperazine (H1 antagonist), tricyclic (H1 antagonist), or tetracyclic (H1 antagonist).
The compound of any one of the preceding claims, wherein the H1 antagonist is a piperazine (H1 antagonist) or a tricyclic (H1 antagonist).
The compound of any one of the preceding claims, wherein the H1 antagonist comprises two aromatic rings (e.g., connected to a (central) carbon, nitrogen, or CO).
The compound of any one of the preceding claims, wherein the H1 antagonist comprises an amine (e.g., amine substituted with alkyl, such as methyl).
The compound of any one of the preceding claims, wherein the H1 antagonist comprises a spacer (e.g., between the amine and the (central) carbon, nitrogen, or CO).
The compound of any one of the preceding claims, wherein the H1 antagonist is selected from the group consisting of olopatadine, cetirizine, acrivastine, bilastine, fexofenadine, levocabastine, hydroxyzine, periciazine, and quetiapine.
The compound of any one of the preceding claims, wherein the H1 antagonist is selected from the group consisting of olopatadine, cetirizine, acrivastine, bilastine, fexofenadine, and levocabastine.
The compound of any one of the preceding claims, wherein the H1 antagonist is olopatadine or cetirizine.
A topical pharmaceutical composition (e.g., peridermal or periocular) comprising a compound having a structure represented by Formula (II):
The topical pharmaceutical composition or compound of any one of the preceding claims, wherein each linker (e.g., L or LA) is independently a bond, substituted or unsubstituted (e.g., branched or straight) alkyl (alkylenyl), or substituted or unsubstituted (e.g., branched or straight) heteroalkyl (heteroalkylenyl).
The topical pharmaceutical composition or compound of any one of the preceding claims, wherein each linker (e.g., L or LA) is independently a bond or substituted or unsubstituted (e.g., branched or straight) alkyl (alkylenyl) (e.g., >C(═O)).
The topical pharmaceutical composition or compound of any one of the preceding claims, wherein the linker (e.g., L or LA) is a bond.
A compound having a structure represented by Formula (II-A):
Use of a compound of Formula (A) for treating a (e.g., keratolytic) dermal or ocular disease or disorder (e.g., the disease or disorder being associated with keratin production and/or buildup) in an individual (e.g., in need thereof), the compound having a structure represented by Formula (A):
A compound having the structure:
A compound having the structure:
The topical pharmaceutical composition or compound of any one of the preceding claims, wherein the linker is a non-hydrolyzable linker.
The topical pharmaceutical composition or compound of any one of the preceding claims, wherein the compound (e.g., the linker of the compound) is enzymatically stable.
The topical pharmaceutical composition or compound of any one of the preceding claims, wherein the compound (e.g., the linker of the compound) is not cleavable by enzymes, such as enzymes of the skin and/or eye (e.g., esterases, hydrolases, or reductases).
The topical pharmaceutical composition or compound of any one of the preceding claims, wherein the compound (e.g., the linker of the compound) is stable in an aqueous environment, such as a biological environment and/or a buffered solution).
The topical pharmaceutical composition or compound of any one of the preceding claims, wherein the compound has anti-parasitic activity.
The topical pharmaceutical composition or compound of any one of the preceding claims, wherein the compound has keratolytic activity.
The topical pharmaceutical composition or compound of any one of the preceding claims, wherein the compound has antihistamine activity.
A pharmaceutical composition comprising a compound of any one of the preceding claims, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.
A method of treating a dermal or an ocular disease or disorder in an individual, comprising administering to the individual a compound or composition of any one of the preceding claims.
Dependencies are inferred from the claim text.