James W. Simpkins - Gainesville FL Douglas F. Covey - Ballwin MO
Assignee:
University of Florida Resarch Foundation, Inc. - Gainesville FL Washington University - St. Louis MO
International Classification:
A61K 3156
US Classification:
514182, 514179, 514180, 514181
Abstract:
The present invention in various embodiments provides methods of treating stroke and conferring protection on a population of cells associated with ischemia in a subject following an ischemic event, comprising: (a) providing an estrogen compound; and (b) administering the effective amount of the compound over a course that includes at least one dose within a time that is effectively proximate to the ischemic event, so as to confer protection on the population of cells. Novel methods are provided for the delivery of an estrogen compound. Examples of ischemic events treatable according to the invention are cerebrovascular disease or stroke, subarachnoid subhemorrhage, myocardial infarct, surgery and trauma. A method of treating ischemic damage utilizing hormones that are non-sex hormones is also provided. A method of treating stroke with ent-17-estradiol, and a method of synthesis, and compounds produced from the synthesis are provided.
Lactam And Thiolactam Derivatives As Anesthetic And Conscious Sedation Agents
James A. Ferrendelli - Houston TX Douglas F. Covey - Ballwin MO
Assignee:
Board of Regents, The University of Texas System - Austin TX Washington University - St. Louis MO
International Classification:
A61K 3140
US Classification:
514327, 514424
Abstract:
This invention relates to lactam and thiolactam derivatives having useful anesthetic and conscious sedation activity. Particularly useful compounds include the diethyl lactams such as 3,3-diethyl-2-pyrrolidinone. Methods for using these compounds and pharmaceutical compositions containing these compounds are provided.
Modified, Hydroxy-Substituted Aromatic Structures Having Cytoprotective Activity
The present invention is directed to modified, hydroxy-bearing aromatic ring structures having cytoprotective activity. More specifically, in a first embodiment the present invention is directed to phenolic compounds, and in particular steriods (e. g. , estrogens), wherein a non-fused polycyclic, hydrophobic substituent is attached to the hydroxy-substituted A-ring thereof. The present invention is further directed to a process for conferring cytoprotection to a population of cells involving the administration of the compound.
Neuroactive 13, 24-Cyclo-18, 21-Dinorcholanes And Structurally Related Pentacyclic Steriods
Douglas F. Covey - Ballwin MO, US Xin Jiang - Baltimore MD, US
Assignee:
Washington University - St. Louis MO
International Classification:
A61K 31/56 A61K 31/58 C07J 53/00 C07J 71/00
US Classification:
514179, 514172, 514173, 540 15, 540 76, 552510
Abstract:
Novel pentacyclic steroids and pentacyclic D-homosteroids comprising: (i) the tetracyclic steroid ring system or tetracyclic D-homosteroid ring system, respectively; (ii) a C(3) substituent selected from the group consisting of (a) a hydroxyl or carboxyl in the α-configuration and (b) a sulfate or other negatively charged moiety; and (iii) a fused fifth ring, the fused fifth ring comprising a hydrogen bond acceptor, and (a) in the case of the pentacyclic steroid the C(13) and C(17) carbons, or (b) in the case of the pentacyclic D-homosteroid the C(13) and C(17a) carbons, having utility as anesthetics and in the treatment of disorders relating to GABA function and activity.
The present invention is generally directed to novel enantiomeric estrogen derivatives, some of which may have one or more unsaturated bonds in conjugation with the terminal or A-ring of the structure, which have cytoprotective activity. The present invention is further directed to a process for conferring cytoprotection to a population of cells, of a subject in need thereof, involving the administration of an effective dose of the compound.
Methods Of Prevention And Treatment Of Ischemic Damage
James Simpkins - Fort Worth TX, US Douglas Covey - Ballwin MO, US
International Classification:
A61K031/56
US Classification:
514/182000
Abstract:
The present invention in various embodiments provides methods of treating stroke and conferring protection on a population of cells associated with ischemia in a subject following an ischemic event, comprising: (a) providing an estrogen compound; and (b) administering the effective amount of the compound over a course that includes at least one dose within a time that is effectively proximate to the ischemic event, so as to confer protection on the population of cells. Novel methods are provided for the delivery of an estrogen compound. Examples of ischemic events treatable according to the invention are cerebrovascular disease or stroke, subarachnoid subhemorrhage, myocardial infarct, surgery and trauma. A method of treating ischemic damage utilizing hormones that are non-sex hormones is also provided. A method of treating stroke with ent-17-estradiol, and a method of synthesis, and compounds produced from the synthesis are provided.
Modified, Hydroxy-Substituted Aromatic Structures Having Cytoprotective Activity
The present invention is directed to a process for conferring cytoprotection on a population of cells which comprises administering to that population of cells a compound comprising a hydroxy-substituted aromatic ring structure and a non-fused polycyclic, hydrophobic substituent attached thereto. In particular, the present invention is directed to such a process wherein the administered compound is phenolic, such as a steriod (e.g., estrogen), and has a non-fused polycyclic, hydrophobic substituent attached to the hydroxy-substituted A-ring thereof.
Neuroactive 13,24-Cyclo-18,21-Dinorcholanes And Structurally Related Pentacylic Steroids
Novel pentacyclic steroids and pentacyclic D-homosteroids comprising: (i) the tetracyclic steroid ring system or tetracyclic D-homosteroid ring system, respectively; (ii) a C(3) substituent selected from the group consisting of (a) a hydroxyl or carboxyl in the α-configuration and (b) a sulfate or other negatively charged moiety; and (iii) a fused fifth ring, the fused fifth ring comprising a hydrogen bond acceptor, and (a) in the case of the pentacyclic steroid the C(13) and C(17) carbons, or (b) in the case of the pentacyclic D-homosteroid the C(13) and C(17a) carbons, having utility as anesthetics and in the treatment of disorders relating to GABA function and activity.