Abstract: The present invention provides methods of treatment utilizing pharmaceutical compositions comprising an effective nicotine agonist amount of epibatidine (1) or a synthetic 7-azabicyclo[2.2.1]-heptane or heptene derivative thereof, and a pharmaceutically acceptable earner, excipient or diluent.

Abstract: 7-Azabicyclo[2.2.1]-heptane and -heptene derivatives with analgesic or anti-inflammatory activity are disclosed that can be administered to a mammal, including a human, to treat pain and inflammatory disorders. A method for the treatment of pain or inflammatory disorders is also presented that includes administering an effective amount of the compound or its pharmaceutically acceptable salt or derivative, or mixtures thereof, to a host in need of analgesic anti-inflammatory therapy, optionally in a pharmaceutically acceptable carrier or diluent.

Abstract: This invention relates to the treatment of conditions that can be treated with a nicotinic agonist by administering to a patient an effective amount of a 7-azabicyclo[2.2.1]-heptane or heptene.

Abstract: Indene derivatives have been found to have potent and specific PAF (Platelet-Activating-Factor) antagonistic activities and are thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, and adult respiratory distress syndrome.

Abstract: Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared.These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.

Abstract: The invention disclosed herein relates to novel 1-deoxyglycosides, preferably 1-deoxy-D-mannopyranosides and 1-deoxy-L-rhamnopyranosides, having in the 1-position of the pyranose ring an aralkylthio/aralkenylthio, aralkyloxy/aralkenyloxy or aralkanoylamino/aralkenoylamino substituent; and to novel processes for preparing these 1-substituted-1-deoxyglycosides starting with the corresponding tetra-O-acetylglycopyranosyl bromide or amine. The 6-hydroxy group of 1-substituted-1 deoxyglycopyranosides can also be replaced by other functional groups. These aralkylthio/aralkenylthio, aralkyloxy/aralkenyloxy and aralkanoylamino/aralkenoylamino 1-deoxyglycosides are potent inhibitors of antigen-specific T-cell proliferation and are also useful as inhibitors of delayed-type hypersensitivity reactions.

Abstract: Mercaptoalkylpyridines carrying an ethenyl or ethynyl substituent are prepared from known pyridine compounds, principally pyridoxine, by known chemical procedures, and are useful in the treatment of rheumatoid arthritis and related inflammatory diseases.

Abstract: Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared.These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.

Abstract: Phosphatidyl inositol analogs are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These phosphatidyl inositol analogs are prepared by condensation of a protected inositol with a substituted phosphonic or phosphorous acid followed by removal of protecting groups.

Abstract: Fluorescein esters and ethers including the dioleyl derivative of fluorescein are disclosed. These compounds have the useful property of being fluorescent under the influence of the proper frequency of electromagnetic irradiation. Further, dioleyl fluorescein is readily incorporated into low-density lipoproteins which can then become part of the cell matter; the compounds retain their fluorescent properties during this procedure. The fluorescence allows cells to be indentified and separated. The fluorescein esters and ethers are prepared from fluorescein and the novel reagent O-alkenyl-N,N'-dialkylisourea.

Abstract: Tricyclic derivatives of substituted pyrrole acids, e.g., substituted 4,10-dihydro-10-oxo-1H-[1]benzoxepino[4,3-b]pyrrole-2-acetic acids or the 5-thia analogs thereof have been prepared via hydrolysis of a precursor or decarboxylation of a precursor-diacid. These tricyclic compounds are found to have high analgesic and anti-inflammatory activities but low ulcerogenic side effects.

Abstract: This invention relates to ophthalmic preparations which include 5-fluoro-2-methyl-1-(p-methylthiobenzylidene)-3-indenylacetic acid or ophthalmologically acceptable salts thereof as the active entity for reducing or controlling inflammation of the eye.

Abstract: 2-Amino-2-deoxy-.beta.-D-glucopyranosyl-(1-4)-2-amino-2-deoxy-D-glucoses of the general structural formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl (1-7C), substituted alkyl (1-7C), phenyl, substituted phenyl, benzyl, or substituted benzyl;R.sub.2 is alkyl, substituted alky, phenyl, or substituted phenyl and each R.sub.2 may be the same group or a different group;R.sub.3 is H or ##STR2## wherein R.sub.8 is H or lower alkyl (1-10C), and provided at least one of R.sub.3 is not H,R.sub.9 is H, or R.sub.9 -R.sub.10 together is --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R.sub.10 is H, alkyl (L-7C), hydroxymethyl, mercaptomethyl, benzyl, or substituted benzyl;R.sub.11 and R.sub.12 each is carboxyl, esterified carboxyl (1-7C), amidated carboxyl, or mono- or di-alkyl- (1-3C) amidated carboxyl;R.sub.4 and R.sub.5 are the same or different and are H, aliphatic or aromatic acyl (2-21C) or substituted acyl (2-21C);when R.sub.8 is lower alkyl, the stereochemistry at asymmetric center I can be either D or L;when R.sub.

Abstract: Cell-specific ligands comprising conjugates of saccharides and amino acids or peptides are synthesized from amino acids such as ornithine, lysine, peptides such as dilysine, diornithine or oligolysine and selected saccharides having reactive functional groups protected by appropriate blocking groups. Such glycopeptides are useful as tissue specific substances, which when coupled with bioactive materials through metabolizable or hydrolyzable linkages, deliver such bioactive materials to the selected site. In this manner, antiinflammatory drugs such as dexamethasone are linked through a metabolizable or hydrolyzable linkage and on administration to an animal suffering from inflammatory disease carries the drug to the site of inflammation for intracellular release. Other examples include the macrophage ligand N.sup.2 -N.sup.2, N.sup.6 -Bis-[3-(.alpha.-D-mannopyranosylthio)propionyl]-6-lysyl-N.sup.6 -[3-(.alpha.-D-mannopyranosylthio)propionyl]-L-lysine, 5, which when coupled to .beta.

Abstract: 2-Amino-2-deoxy-glycoses of the general structural formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl (1-7C), substituted alkyl (1-7C), phenyl, substituted phenyl, benzyl, or substituted benzyl;R.sub.2 is alkyl, substituted alkyl, phenyl, or substituted phenyl;R.sub.3 is H or lower alkyl (1-10C) with the proviso that when the aminoglycose has the 2-amino-2-deoxy-D-glucose configuration, R.sub.3 cannot be H;R.sub.4 and R.sub.5 are same or different and are H, aliphatic or aromatic acyl (2-21C) or substituted acyl (2-21C);R.sub.6 is H, or R.sub.6 -R.sub.7 together is --CH.sub.2 --CH.sub.2 --CH.sub.2 --,R.sub.7 is H, alkyl (1-7C), hydroxymethyl, mercaptomethyl, benzyl, or substituted benzyl;R.sub.8 and R.sub.9 each is carboxyl, esterified carboxyl (1-7C), amidated carboxyl, or mono- or di-alkyl-(1-3C)-amidated carboxyl;provided that when R.sub.

Abstract: Immunologically active compounds of the formula: ##STR1## wherein: R.sub.1 is C.sub.1-7 alkyl; substituted C.sub.1-7 alkyl; phenyl; or substituted phenyl;R.sub.2 is hydrogen; C.sub.1-7 alkyl; substituted C.sub.1-7 alkyl; phenyl; substituted phenyl; phenyl C.sub.1-4 alkyl; or substituted phenyl C.sub.1-4 alkyl;R.sub.3 and R.sub.4 may be the same or different and are each independently hydrogen, provided that R.sub.3 and R.sub.4 may not both be hydrogen; or ##STR2## where X is --O--; --S--; or ##STR3## R.sub.10 is hydrogen; C.sub.1-30 alkyl; C.sub.2-30 alkenyl; C.sub.1-30 alkoxy; phenyl; C.sub.1-20 alkylsulfonyl; or cholesteryl;R.sub.11, R.sub.12, R.sub.13, R.sub.14, and R.sub.15 may be the same or different and are each independently hydrogen; C.sub.1-20 alkyl; C.sub.1-20 alkylcarbonyloxy; amino; benzyl; C.sub.1-20 alkoxymethyl; C.sub.1-20 alkylamido; or ##STR4## r is 0 or 1; s is 0 or 1; and t is 0 to 20; provided that s may only be 0 when both r and t are greater than 0 or when r is 0 and R.sub.

Abstract: Mercaptoalkylpyridines carrying an ethenyl or ethynyl substituent are prepared from known pyridine compounds, principally pyridoxine, by known chemical procedures, and are useful in the treatment of rheumatoid arthritis and related inflammatory diseases.

Abstract: Lipid vesicles comprising a lipid bilayer which includes analogs of cell-surface receptors such as dicetyl phosphate; stearylamine; 6-(5-cholesten-3.beta.-yloxy) hexyl 1-thio-.beta.-L-fucopyranoside; 6-(5-cholesten-3.beta.-yloxy) hexyl 1-thio-.beta.-D-galactopyranoside; 6-(5-cholesten-3.beta.-yloxy)hexyl 1-thio-.alpha.-D-mannopyranoside; 6-(5-cholesten-3-yloxy)hexyl 2-acetamido-2-deoxy-1-thio-.beta.-D-galactopyranoside; 6-(5-cholesten-3.beta.-yloxy)hexyl 6-amino-6-deoxy-1-thio-.beta.-D-galactopyranoside; or 6-(5-cholesten-3.beta.-yloxy)hexyl 6-amino-6-deoxy-1-thio-.alpha.-D-mannopyranoside; cholesterol and distearoyl phospatidylcholine, and an effective amount of physiologically compatible radioactive tracer, cytotoxic or therapeutic agent as a part of the vesicles. The vesicles of this invention can be administered to the human host and have been found to release the contents of the vesicles in a predetermined manner, i.e.

Abstract: Fluorescein esters and ethers including the dioleyl derivative of fluorescein are disclosed. These compounds have the useful property of being fluorescent under the influence of the proper frequency of electromagnetic irradiation. Further, dioleyl fluorescein is readily incorporated into low-density lipoproteins which can then become part of the cell matter; the compounds retain their fluorescent properties during this procedure. The fluorescence allows cells to be identified and separated. The fluorescein esters and ethers are prepared from fluorescein and the novel reagent O-alkenyl-N,N'-dialkylisourea.

Abstract: Certain novel acyl cyanoguanidines, their preparation, pharmaceutical compositions and novel methods of treating inflammation and autoimmune diseases such as rheumatoid arthritis are disclosed.