Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula I: (I) wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyper-proliferative disorders, also are disclosed.

Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula I: (I) wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyper-proliferative disorders, also are disclosed.

Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula I: (I) wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.

Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula I: (I) wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.

Abstract: A new group of fluorescent organic compounds having a variety of uses are described. They are especially useful as dye compounds in dye laser systems, and as photochemical agents in the treatment of diseased tissues using photodynamic therapy techniques. The compounds include a tri-cyclic compound having the following structure: ##STR1## Preferably R.sub.1 -R.sub.5 .dbd.R.sub.9 -R.sub.12 .dbd.C; R.sub.7 .dbd.B; R.sub.6 and R.sub.8 .dbd.N; R.sub.14 .dbd.lower n-alkyl or an electron withdrawing group such as CN.sup.- ; R.sub.16 and R.sub.19 are independently selected from the group consisting of lower n-alkyl, a sulfate or an acid or salt thereof, or hydrogen; and R.sub.20 .dbd.R.sub.21 .dbd.F.

Abstract: A method is disclosed for predicting response of a tumor patient to therapy, and selecting appropriate therapy for malignant neoplasms such as breast, ovarian and gastrointestinal cancer. A sample of tumor cells is cultured in the presence of 10 .mu.g/ml estradiol, and inhibition of cell growth in the culture paradoxically indicates an estrogen dependent tumor that will respond to antiestrogenic therapy. Another sample of tumor cells is cultured in the presence of a chemotherapeutic agent which predicts response of the tumor to in vivo administration of a cytotoxic agent. The chemotherapeutic agent is preferably a cytotoxic drug, or a drug having both cytotoxic and antiestrogenic mechanisms of action. A particularly suitable substance having both mechanisms of action is: ##STR1## wherein R.sup.1 H, OH, OOC(CH.sub.2).sub.2 CO.sub.2 H or CH.sub.3 COO; R.sup.2 is C.sub.6 H.sub.4 OH, C.sub.6 H.sub.4 OCOCH.sub.3, C.sub.6 H.sub.4 OOC(CH.sub.2)CO.sub.2 H, or C.sub.6 H.sub.5 ; and X is C.sub.6 H.sub.3 -2,4(NO.sub.2).

Abstract: A new group of fluorescent organic materials having a variety of uses are described. They are especially useful as dye compounds in dye laser systems, and as photochemical agents in the treatment of sensitive diseased tissues using photodynamic therapy techniques.

Abstract: Apparatus for in situ radiotherapy has a flexible catheter having a proximal end for receiving a radioisotope and a distal end for positioning the flexible catheter within a patient to be treated. An anchor, which is permanently connectable to tissues deep inside the patient, has a sealing collar connected to it which seals the distal end of the catheter. The catheter also includes a plug near the distal end which seals the distal end in addititon to the seal provided by the sealing collar. The anchor has a penetration point connected to it to assist a surgeon in implanting the catheter within a tumor. A threaded fastener on the anchor is screwed into the catheter. The flexible catheter can be released remotely from the anchor by unscrewing it. A suture eye is connected to the anchor. The suture eye may be sutured to healthy tissue within the patient when the apparatus is implanted to secure the anchor to the patient.

Abstract: Apparatus for in situ radiotherapy has a flexible catheter having a proximal end for receiving a radiosotope and a distal end for positioning the flexible catheter within a patient to be treated. An anchor, which is permanently connectable to tissues deep inside the patient, has a sealing collar connected to it which seals the distal end of the catheter. The anchor has a penetration point connected to it to assist a surgeon in implanting the catheter within a tumor. A threaded fastener is connected to the anchor and screwed into the catheter. The flexible catheter can be released remotely from the anchor by unscrewing it. A suture eye is connected to the anchor. The suture eye may be sutured to healthy tissue within the patient when the apparatus is implanted to secure the anchor to the patient.

Abstract: A new group of fluorescent organic materials having a variety of uses are described. They are especially useful as dye compounds in dye laser systems, and as photochemical agents in the treatment of diseased tissues using photodynamic therapy techniques. The materials involve a tri-cyclic compound having the following structure: ##STR1## In this structure, R.sub.1 -R.sub.21 represent a variety of organic and inorganic groups.

Abstract: Dermal inflammations which are induced and propagated by leukotrienes are treated by topically applying to the inflamed dermis the following compound: ##STR1## wherein R.sup.3 is H or a thiol; n is 1 to 12; p is 0 to 12; X is a substituted carbonyl, such as an ester or a carboxylic acid; and Y is an aliphatic or branched hydrocarbon, aromatic ring, carbonyl or substituted amide.

Abstract: Azido-, 4-nitro and 2,4-dinitrophenylhydrazones as well as 4,4'-dihydroxybenzophenone-hydrazone and other hydrazones are disclosed which have antiestrogenic activity useful in treating estrogen-requiring tumor cells. The described hydrazones bind to estrogen receptors in the cytoplasm of tumor cells. The azido-, 4-nitro- and 2,4-dinitro-phenyl branches of the molecules appear to bind to the receptors and prevent translocation of estrogenic information into the nucleus, thereby blocking the synthesis of necessary macromolecules such as proteins. Absence of geometric isomerization from antiestrogenic to estrogenic forms of the drug minimizes estrogenic side-effects.

Abstract: A method of treating chemical ulcers caused by leukotriene production, the method comprising the step of applying to the ulcer a compound that interferes with leukotriene production, the compound being selected from the group consisting of N,N'-diacetylcystine, N-acetylhomocysteine and N-acetylcysteine.

Abstract: A method of treating herpes, comprising the step of applying to the herpes lesions a compound that interferes with leukotriene production, the compound being selected from the group consisting of N,N'-diacetylcystine, N-acetylhomocysteine and N-acetylcysteine.