Enantiomerically purified gper agonist for use in treating disease states and conditions
OwnerChristopher NATALE, Patrick T. MOONEY +2inventors
InventorsChristopher NATALE, Patrick T. MOONEY, Tina GARYANTES, Wayne LUKE
Life of this patent
Estimating the term…
Abstract
The present disclosure provides 1) an enantiomerically purified compound SRR G-1, or a derivative thereof, including specific crystal forms, salts and co-crystals that modulates G protein-coupled estrogen receptor activity, 2) pharmaceutical and cosmetic compositions comprising an enantiomerically purified SRR G-1, or a derivative thereof, and 3) methods of treating or preventing disease states and conditions and cosmetic conditions mediated through these receptors and related methods thereof in humans and animals.
Claims13
A method of treating a disease or disorder in a subject in need thereof, comprising:
- a) administering to the subject a therapeutically effective amount of a compound of the formula:
- 1-((3aS,4R,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethan-1-one
- SRR G-1
- or a pharmaceutically acceptable salt thereof,
- wherein the compound comprises a crystalline Form A characterized by an XRPD pattern having peaks expressed in degrees 2θ (±0.20) at about 5.75, about 20.54, about 20.71, about 21.25, and about 21.86, wherein the crystalline Form A has a melt onset of about 176° C., wherein the crystalline Form A is anhydrous, wherein the crystalline Form A exhibits low hygroscopicity, and wherein the crystalline Form A exhibits a calculated density of about 1.485 g cm−3, and
- b) alleviating one or more symptoms associated with the disease or disorder in the subject.
A method of treating type 2 diabetes in a subject in need thereof, comprising:
- a) administering to the subject a therapeutically effective amount of a compound of the formula:
- 1-((3aS,4R,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethan-1-one
- SRR G-1
- or a pharmaceutically acceptable salt thereof,
- wherein the compound comprises a crystalline Form A characterized by an XRPD pattern having peaks expressed in degrees 2θ (±0.20) at about 5.75, about 20.54, about 20.71, about 21.25, and about 21.86, wherein the crystalline Form A has a melt onset of about 176° C., wherein the crystalline Form A is anhydrous, wherein the crystalline Form A exhibits low hygroscopicity, and wherein the crystalline Form A exhibits a calculated density of about 1.485 g cm−3;
- and
- b) alleviating one or more symptoms of type 2 diabetes in the subject.
A method of increasing or preventing loss of skin pigmentation in a subject in need thereof, comprising:
- a) administering to the subject a therapeutically effective amount of a compound of the formula:
- 1-((3aS,4R,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethan-1-one
- SRR G-1
- or a pharmaceutically acceptable salt thereof,
- wherein the compound comprises a crystalline Form A characterized by an XRPD pattern having peaks expressed in degrees 2θ (±0.20) at about 5.75, about 20.54, about 20.71, about 21.25, and about 21.86, wherein the crystalline Form A has a melt onset of about 176° C., wherein the crystalline Form A is anhydrous, wherein the crystalline Form A exhibits low hygroscopicity, and wherein the crystalline Form A exhibits a calculated density of about 1.485 g cm−3;
- and
- increasing or preventing loss of skin pigmentation in the subject.
A method of skin protection in a subject in need thereof comprising:
- a) administering to a subject a therapeutically effective amount of a compound of the formula:
- 1-((3aS,4R,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethan-1-one
- SRR G-1
- or a pharmaceutically acceptable salt thereof,
- wherein the compound comprises a crystalline Form A characterized by an XRPD pattern having peaks expressed in degrees 2θ (±0.20) at about 5.75, about 20.54, about 20.71, about 21.25, and about 21.86, wherein the crystalline Form A has a melt onset of about 176° C., wherein the crystalline Form A is anhydrous, wherein the crystalline Form A exhibits low hygroscopicity, and wherein the crystalline Form A exhibits a calculated density of about 1.485 g cm−3;
- and
- b) increasing skin pigmentation in the subject.
A method of treating cancer in a subject in need thereof comprising:
- administering to a subject a therapeutically effective amount of a compound of the formula:
- 1-((3aS,4R,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethan-1-one
- SRR G-1
- or a pharmaceutically acceptable salt thereof,
- wherein the compound comprises a crystalline Form A characterized by an XRPD pattern having peaks expressed in degrees 2θ (±0.20) at about 5.75, about 20.54, about 20.71, about 21.25, and about 21.86, wherein the crystalline Form A has a melt onset of about 176° C., wherein the crystalline Form A is anhydrous, wherein the crystalline Form A exhibits low hygroscopicity, and wherein the crystalline Form A exhibits a calculated density of about 1.485 g cm−3;
- and
- b) alleviating one or more symptoms associated with the cancer in the subject.
Dependencies are inferred from the claim text.