Abstract: Peptoid compounds of Formula I and Formula II are disclosed The compounds are useful in the treatment of matrix metalloproteinase-mediated disorders.

Abstract: Compounds of Formula I: E—NH—D—NH—B—A—B—NH—D—NH—E  (I) wherein A is C2-C6 alkene, C3-C6 cycloalkyl, cycloalkenyl, or cycloaryl; B is independently a single bond, C1-C6 alkyl alkenyl; D is independently C1-C6 alkyl or alkenyl, or C3-C6 cycloalkyl, cycloalkenyl, or cycloaryl; and E is independently H, C3-C6 alkyl or alkenyl; and pharmaceutically-suitable salts thereof; a synthetic method therefor, pharmaceutical dosage forms containing one of more of these compounds, and use of these compounds in the treatment of neoplastic cell growth, are disclosed.

Abstract: Peptiod compounds of Formula I and Formula II are disclosed 1

Abstract: Peptoid compounds of Formula I and Formula II are disclosed The compounds are useful in the treatment of matrix metalloproteinase-mediated disorders.

Abstract: Novel 4-substituted-1,2-naphthoquinones, pharmaceutical unit dosage forms containing 4-substituted-1,2-naphthoquinones, and uses of 4-substituted-1,2-naphthoquinones to inhibit the growth of cancer cells are disclosed.

Abstract: A process for the preparation of .beta.-lapachone and dunnione derivatives of formulae I and II ##STR1## wherein, the a solution of lawsone in dimethylsufoxide at a temperature of -78.degree. C. or less is reacted with lithium hydride forming the lithium salt of lawsone; alkylating the lithium salt with an allyl halide; and cyclizing the C-alkylated lawsone derivative.

Abstract: Compounds of Formula I:E-NH-D-NH-B-A-B-NH-D-NH-E (I)wherein A is C.sub.2 -C.sub.6 alkene, C.sub.3 -C.sub.6 cycloalkyl, cycloalkenyl, or cycloaryl; B is independently a single bond, C.sub.1 -C.sub.6 alkyl alkenyl; D is independently C.sub.1 -C.sub.6 alkyl or alkenyl, or C.sub.3 -C.sub.6 cycloalkyl, cycloalkenyl, or cycloaryl; and E is independently H, C.sub.1 -C.sub.6 alkyl or alkenyl; and pharmaceutically-suitable salts thereof; a synthetic method therefor, pharmaceutical dosage forms containing one of more of these compounds, and use of these compounds in the treatment of neoplastic cell growth, are disclosed.

Abstract: Novel 4-substituted-1,2-naphthoquinones, pharmaceutical unit dosage forms containing 4-substituted-1,2-naphthoquinones, and uses of 4-substituted-1,2-naphthoquinones to inhibit the growth of cancer cells are disclosed.

Abstract: A method for identifying patients at risk of developing vascular leakage syndrome and systemic inflammatory response syndrome (SIRS) such as septic shock by determining the serum levels of metalloproteinase expression, in particular type IV collagenase expression, as well as a method of treating or preventing vascular leakage syndrome and SIRS by the administration of one or more metalloproteinase inhibitors, preferably type IV collagenase inhibitors is taught. Additionally, the therapeutic efficacy of bis(dioxopiperazine) compounds is determined on the basis of collagenase inhibiting activity, and the compounds which inhibit collagenase activity are utilized for the treatment of collagenase related disorders, e.g., vascular leakage syndrome, septic shock, stroke, cardiac disorders, angiogenesis, and arthritis.

Abstract: The invention relates to .beta.-lapachone derivatives of formula II and compositions containing said compounds: ##STR1## wherein, R.sup.5, R.sup.6 and R.sup.7 are as defined in the specification. The compounds are potent inhibitors of neoplastic cell growth and proliferation.

Abstract: 3-Substituted-.beta.-lapachone analogs and their use either alone or to augment chemotherapy or radiotherapy to induce programmed neoplastic cell death without exhibiting toxicity to surrounding normal cells are disclosed. In particular, 3-allyl-.beta.-lapachones, 3-alkyl-.beta.-lapachones and 3-halo-.beta.-lapachones were found to be Topoisomerase (Topo I) inhibitors. When these analogs are used alone there is a reversible single-strand break in the DNA of neoplastic cells causing apoptosis and cell death in some cells. However, when these analogs are combined with chemotherapy or X-irradiation, an irreversible Topo I-mediated break is achieved. A new and more efficient chemical synthesis of the compounds is also disclosed.

Abstract: The present invention relates to a method for synthesis of optically pure 4-alkenyl or 4-alkanyl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase, thus making them useful in the treatment of coronary artery diseases, especially atherosclerosis, and additionally, as inhibitors of various inflammatory cytokines, making them useful in the treatment of both acute and chronic inflammation, as well in the treatment of cachexia, rheumatoid arthritis, multiple sclerosis, Crohn's disease and ulcerative colitis. The invention further relates to pharmaceutical compositions of the instant compounds.

Abstract: The present invention relates to a method for synthesis of optically pure 4-alkenyl or 4-alkanyl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase. The invention further relates to the pharmaceutical use of such compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis.

Abstract: The present invention relates to a method for synthesis of optically pure stereogenically labile 4-aryl-2-hydroxytetronic acids from an optically pure aidehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase, and additionally as inhibitors of cyclooxygenase and 5-lipoxygenase. The invention further relates to the pharmaceutical use of such.compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis, and in the treatment of various inflammatory pathologies, especially arthritis.

Abstract: The present invention relates to a method for synthesis of optically pure stereogenically labile 4-aryl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase. the invention further relates to the pharmaceutical use of such compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis.

Abstract: The present invention relates to compounds having anti-ischaemic activity of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and Z are as defined herein. The present invention further relates to a method of preparing such compounds, as well as compositions having anti-ischaemic activity which comprise such compounds and a method of treating ischaemia.

Abstract: One aspect of the present invention relates to a process of making cyclohexane-1,2-di(O)-4,5-di(N) diastereomers which are useful as a synthons for various diastereoisomeric pharmaceutical systems. The present invention also relates to the stereoisomer compounds which are derived from retro- synthetic analysis. In another aspect, the present invention relates to novel antineoplasic Pt(II) complexes derived from the stereoisomers and the processes for making such Pt(II) complexes. Mono- and di-hydroxyl substitution on the cyclohexane ring renders the organoplatinum complex relatively more water soluble, thereby facilitating intravenous administration. The Pt(II) complexes of the present invention are less nephrotoxic than cisplatin and are readily excreted via the kidney due to their enhanced water solubility.

Abstract: The present invention relates to a method for synthesis of optically pure stereogenically labile 4-substituted-2-hydroxytetronic acids from an asymmetric .alpha.-hydroxy ester. The chiron approach of the present invention utilizes a non-nucleophilic lithium amide base under kinetically controlled Claisen conditions to produce a 4-substituted-2-pheylmethoxy precursor to the 4-substituted-2-hydroxy tetronic acid. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase. The invention further relates to the pharmaceutical use of such compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis.

Abstract: One aspect of the present invention relates to a process of making cyclohexane-1,2-di(O)-4,5-di(N) diastereomers which are useful as a synthons for various diastereoisomeric pharmaceutical systems. The present invention also relates to the stereoisomer compounds which are derived from retro-synthetic analysis. In another aspect, the present invention relates to novel antineoplastic Pt(II) complexes derived from the stereoisomers and the processes for making such Pt(II) complexes. Mono- and di-hydroxyl substitution on the cyclohexane ring renders the organoplatinum complex relatively more water soluble, thereby facilitating intravenous administration. The Pt(II) complexes of the present invention are less nephrotoxic than cisplatin and are readily excreted via the kidney due to their enhanced water solubility.

Abstract: The present invention relates to the pharmaceutical use of 3,4-dihydroxybenzopyranone compounds in the treatment of diseases caused by enveloped viruses, including herpes simplex virus (HSV) types 1 and 2.