-ent-19-norprogesterone, compositions and uses thereof to treat traumatic brain injury (TBI), including concussions-
AssigneeOragenics, Inc.
InventorDaniel E. Levy
Life of this patent
Estimating the term…
Abstract
The present invention relates to ent-19-Norprogesterone, compositions and methods of use thereof to treat, minimize and/or prevent traumatic brain injury (TBI), including severe TBI, moderate TBI and mild TBI, including concussions.
Claims20
An intranasal method for treating a human diagnosed with traumatic brain injury (TBI) wherein the subject needs TBI treatment, said method comprising:
- administering to the human a nasal pharmaceutical composition to treat the TBI, wherein the nasal pharmaceutical composition comprises ent-19-norprogesterone, or a pharmaceutically acceptable salt, ester, prodrug or co-crystal thereof, and a pharmaceutically acceptable excipient in an amount effective to treat the TBI, wherein said administration route is intranasally, and wherein the ent-19-norprogesterone has the following chemical structure
The intranasal method according to claim 85, wherein the TBI is a concussion.
The method according to claim 85, wherein the pharmaceutical composition further comprises an additional therapeutic agent selected from a group of additional therapeutic agents consisting of a neuroprotective agent, an anti-inflammatory agent, an anti-amyloid agent, and an anti-Tau agent.
The method according to claim 85, wherein the nasal pharmaceutical composition is powder.
The method according to claim 86, wherein the human is in a military.
The method according to claim 86, wherein the human is an athlete.
The method according to claim 102, wherein the human athlete is a football player.
A method of treating a human who is concussed, wherein the concussed human needs concussion treatment, said method comprising
- administering ent-19-norprogesterone, or a pharmaceutically acceptable salt, ester, prodrug or co-crystal thereof, to the concussed human for providing a neuroprotective effect in the brain of the concussed human, wherein said administration is intranasal administration, wherein the neuroprotective effect includes reducing cell death, brain swelling, and/or inflammation, wherein said administration step includes administering the ent-19-norprogesterone in an amount effective to provide the neuroprotective effect, and wherein the ent-19-norprogesterone has the following chemical structure
A compound having a structure comprising:
- or a pharmaceutically acceptable salt, ester, prodrug or co-crystal thereof, wherein said compound is
- or a pharmaceutically acceptable salt, ester, prodrug or co-crystal thereof, and
- wherein, X is O, N or S;
- Y is O, N or S;
- or, YR8R10 is absent;
- R1, R2, R5, and R6 are independently H, C1-C6 alkyl, halogen, OR12, NR13R14, SR15, SOR16 or S02R17;
- R4 is H or C1-C6 alkyl;
- R4 together with R3 and X forms an optionally substituted 5-6 membered heterocycle containing 1-2 nitrogen, oxygen or sulfur atoms;
- or R4 and R7 together form a double bond;
- R3 is H or C1-C6 alkyl;
- R3 together with R4 and X forms an optionally substituted 5-6 membered heterocycle containing 1-2 nitrogen, oxygen or sulfur atoms, or R3 is absent;
- R7 is absent, H, C(O)—C1-C6 alkyl, C1-C6 alkyl;
- or R7 and R4 together form a double bond;
- R8 is H, C(O)—C1-C6 alkyl, C1-C6 alkyl;
- R8 together with R9 and Y forms an optionally substituted 5-6 membered heterocycle containing 1-2 nitrogen, oxygen or sulfur atoms, or R8 is absent;
- R9 is H or C1-C6 alkyl;
- R9 together with R8 and Y forms an optionally substituted 5-6 membered heterocycle containing 1-2 nitrogen, oxygen or sulfur atoms;
- R9 and R11 together form a double bond;
- R10 is absent, H, C(O)—C1-C6 alkyl, C1-C6 alkyl;
- or R10 and R11 together form a double bond;
- R11 is H or C1-C6 alkyl;
- or R11 and R—10 together form a double bond;
- R11 and R9 together form a double bond;
- R12, R13, R14, R15, R16 and R17 are independently H, C(O)—C1-C6 alkyl, C1-C6 alkyl;
- and the dotted line indicates the presence of either a single or a double bond wherein the valences of a single bond are completed by hydrogens.
Dependencies are inferred from the claim text.