Abstract:
Compounds for the treatment of estrogen-receptor related maladies are provided. Compounds with anti-androgenic properties also are provided. In particular, the invention provides compounds that are tetrahydroquinoline phenylamide derivatives and are useful for the treatment of breast and prostate cancer, and osteoporosis.
Abstract:
A family of substituted chiral allosteric effectors of hemoglobin is useful for delivering more oxygen to hypoxic and ischemic tissues by reducing the oxygen affinity of hemoglobin in whole blood.
Abstract:
Chemical structures have been identified which allosterically modify pyrvate kinase and either inhibit or activate enzymatic activity. These compounds can be used as pharmaceuticals in the treatment of a wide variety of diseases and disorders where influencing metabolic processes is beneficial, such as the glycolytic pathway, all pathways which use ATP as an energy source, and all pathways which involve 2,3-diphosphoglycerate.
Abstract:
A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The effect has particular application in a wide variety of treatments including hypoxia, hypothermia, ischemia, stroke, ARDS, COPD, surgical blood loss, acute nonvolemic hemodilutions, wounds, diabetic ulcers, chronic leg ulcers, pressure sores, tissue transplants, and sepsis. The compounds are capable of acting on hemoglobin in whole blood.
Abstract:
Compounds of the general structural formula: ##STR1## wherein X, Y and Z may each be CH.sub.2, NH, or O, R.sub.2-6 are either hydrogen, halogen, or a substituted or unsubstituted C.sub.1, C.sub.2, or C.sub.3 alkyl group and these moieties maybe the same or different, or alkyl moieties of aliphatic or aromatic rings incorporating two of the R.sub.2-6 sites, R.sub.7-8 are hydrogen, methyl, or ethyl groups and these moieties may be the same or different, or alkyl moieties as part of an aliphatic ring connecting R.sub.7 and R.sub.8, and R.sub.9 is a hydrogen, loweralkyl such as methyl, ethyl or propyl, or a salt cation such as sodium, potassium, or ammonium are useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.
Abstract:
A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.
Abstract:
Chemical compounds which interact inside the central water cavity of hemoglobin and bridge between the two .alpha. subunits can be used to allosterically modify hemoglobin towards tense and relaxed states. The functional groups employed are aldehydes and carboxylic acids, wherein the aldehydes form covalent bonds (schiff base) with amino acid residues of hemoglobin and the carboxylic acids form ionic bonds with amino acid residues of hemoglobin. Particularly useful compounds within the practice of this invention bond to the n-terminal valine of one .alpha. subunit of hemoglobin, and the lysine 99 and/or arginine 141 of the other .alpha. subunit.
Abstract:
A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.
Abstract:
The present invention describes novel tritium labelled nitrogen mustard type compounds, and their aziridinium type analog, and a process for the production of same. The compounds are of value in medical research and development and also as active ingredients of pharmaceutical compositions. The compounds can be used to develop analogs of human disease states and can also be used to evaluate the mechanism of neurotransmitter regulation and function, both in vitro and in vivo.
Abstract:
The present invention is directed to a method of treating a person for sickle cell anemia comprising administering to the person a therapeutically effective dosage of a compound of the general formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: R=ethyl, propyl or isopropyl; and ##STR2##