Abstract: The invention provides a method for treating sexual dysfunction in male mammals using a compound of the formula[E--DHC] (I)or a non-toxic pharmaceutically acceptable salt thereof, wherein [E] is an estrogen and [DHC] is the reduced, biooxidizable, blood-brain barrier-penetrating, lipoidal form of a dihydropridine.revreaction.pyridinium salt redox carrier. Compositions for use in the subject method are also disclosed. A preferred compound for use in the method and compositions is an estradiol derivative, namely, 17.beta.-[(1-methyl-1,4-dihydro-3-pyridinyl)carbonyloxy]estra-1,3,5(10)-tr ien-3-ol.

Abstract: The invention provides compounds of the formulaD--DHC].sub.n (I)and the nontoxic pharmaceutically acceptable salt thereof, wherein D is the residue of a centrally acting drug containing at least one reactive functional group selected from the group consisting of amino, hydroxyl, mercapto, carboxyl, amide and imide, said residue being characterized by the absence of a hydrogen atom from at least one of said reactive functional groups in said drug; n is a positive integer equal to the number of said functional groups from which a hydrogen atom is absent; and [DHC] is the reduced, biooxidizable, blood-brain barrier penetratring lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier, said carrier comprising a bivalent radical of the formula ##STR1## wherein the alkylene group can be straight or branched and can contain 1 to 3 carbon atoms; R.sub.

Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.

Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are:(a) compounds of the formula[D--DHC] (I)wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier, with the proviso that when [DHC] is ##STR1## wherein R is lower alkyl or benzyl and [D] is a drug species containing a single NH.sub.2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH.sub.

Abstract: The present invention relates to pharmaceutical compositions and methods for the treatment of metabolic disorders and to certain inositol-nicotinate dichloroacetate derivatives as the active ingredients therein.

Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## X.sup.-, wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.

Abstract: A brain-specific dopaminergic response is elicited in a patient in need of such treatment, e.g., a patient afflicted with Parkinson's disease of hyperprolactinemia, by administering thereto a therapeutically effective amount of preferably catechol protected dopamine tethered to a reduced, blood-brain barrier penetrating lipoidal form [D-DHC] of a dihydropyridine.revreaction.pyridinium salt type redox carrier, e.g., 1,4-dihydrotrigonelline. Oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt type dopamine/carrier entity [D-QC].sup.+ prevents elimination thereof from the brain, while elimination from the general circulation is accelerated, resulting in significant and prolongedly sustained brain-specific dopaminergic activity.

Abstract: Novel soft steroid anti-inflammatory agents, said agents being esters or thioesters of 17.alpha.-alkoxy-11.beta.-hydroxyandrost-4-en-3-one-17.beta.-carboxylic acids, pharmaceutical compositions containing said agents, novel chemical intermediates useful in the preparation of said agents and methods of administering same to mammals in the treatment of inflammation. Preferred compounds are the haloalkyl esters of 17.alpha.-alkoxy-11.beta.-hydroxyandrost-4-en-3-one-17.beta.-carboxylic acids.

Abstract: The invention provides novel orally active salts of the formula ##STR1## in which .circle. is the skeleton of a polyol, n is the number of OH's in the polyol (3 to 24); p is .gtoreq.3 and .ltoreq.n; r is the available valence of the heparin unit and .gtoreq.3 and .ltoreq.7; sr is equal to pv; and R.sup.+ is ##STR2## in which R.sup.iv is C.sub.1 -C.sub.3 alkyl; R' and R" are C.sub.1 -C.sub.7 alkyl, the same or different, or combined so that --NR'R" represents the residue of a saturated monocyclic secondary amine; R"' is identical to the corresponding portion of a natural amino acid; the alkylene groups contain 1 to 3 carbon atoms; and R.sup.v is H, --CONH.sub.2 or --COO(C.sub.1 -C.sub.7 alkyl). The salts are stable lipoidal "ion pairs" or complexes which can be absorbed through the gastrointestional wall and which slowly release heparinic acid to achieve long-lasting anticoagulant activity. Novel quaternary salts which are intermediates to the heparin salts of the invention are also disclosed.

Abstract: Anticholinesterase and antihypercholesterolemic pyridine derivatives of the formula (I) ##STR1## are provided as well as processes for preparing same, and composition and methods of treatment employing such pyridine derivatives as the active drug components thereof.

Abstract: Testicularly acting drug species are site-specifically/sustainedly delivered to the testes by administering to a male in need of such treatment a pharmacologically effective amount of the target drug species [D] tethered to a reduced, blood-testis barrier penetrating lipoidal form [D--DHC] of a dihydropyridine.revreaction.pyridinium salt type redox carrier, e.g. 1,4-dihydrotrigonelline. Oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt type drug/carrier entity [D--QC].sup.+ prevents elimination thereof from the testes, while elimination from the general circulation is accelerated, resulting in significant and prolongedly sustained testicular-specific drug activity, whether ascribable to the cleavage of the [D--QC].sup.+ entity and sustained release of the drug [D] in the testes and/or to [D--QC].sup.+ itself.

Abstract: The invention provides a method for controlling mammalian body weight using a compound of the formula[E--DHC] (I)or a non-toxic pharmaceutically acceptable salt thereof, wherein [E] is an estrogen and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating, lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier. Novel compositions for weight control comprising a compound of formula (I) or its salt are also disclosed. A preferred compound for use in the subject method and compositions is an estradiol derivative, namely, 17 .beta.-[(1-methyl-1,4-dihydro-3-pyridinyl)carbonyloxy]estra-1,3,5(10)-trie n-3-ol.

Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are:(a) compounds of the formula[D-DHC] (I)wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine .revreaction. pyridinium salt redox carrier, with the proviso that when [DHC] is ##STR1## wherein R is lower alkyl or benzyl and [D] is a drug species containing a single NH.sub.2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH.sub.

Abstract: Compounds the structural formula ##STR1## or their pharmaceutically acceptable salts, wherein X is H or CH.sub.3, Z is NH.sub.2 or OR.sub.6, R.sub.1 is a C.sub.1-8 alkyl, C.sub.3-6 -cycloalkylmethyl, or phenyl-C.sub.1-2 alkyl group,R.sub.2 is hydrogen, hydroxy, chloro or fluoro,R.sub.3 is hydrogen, hydroxy, methoxy, --OCO--(C.sub.1-6 -alkyl) or morpholinoethoxy,R.sub.4 and R.sub.5 may be the same or different and are H or C.sub.1-6 alkyl,R.sub.6 is H, C.sub.1-4 alkyl, C.sub.3-5 alkenyl, C.sub.3-7 cycloalkyl phenyl, or phenyl substituted by one to three alkyl groups with a total of 4 carbon atoms are useful opiod antagonists.

Abstract: Centrally acting drug species are site-specifically/sustainedly delivered to the brain by administering to a patient in need of such treatment a therapeutically effective amount of the target drug species [D] tethered to a reduced, blood-brain barrier penetrating lipoidal form [D-DHC] of a dihydropyridine.revreaction.pyridinium salt type redox carrier. Oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt type drug/carrier entity [D-QC].sup.+ prevents elimination thereof from the brain, while elimination from the general circulation is accelerated, and subsequent cleavage of the quaternary carrier/drug species results in sustained delivery of the drug [D] in the brain and facile elimination of the carrier moiety [QC].sup.+.

Abstract: Novel, transient prodrug forms of biologically active agents containing mercapto groups have (i) the structural formula (I): ##STR1## wherein X is O, S, or NR.sup.5 ;R.sup.1 S is the residue of any biologically active agent R.sup.1 SH;R.sup.

Abstract: Novel, transient inotropic prodrug forms of the N-(2-phenylethyl)-.omega.-phenylalkylamines, notably of dobutamine, have (i) the structural formula (I): ##STR1## with the proviso that at least one R.sup.1, R.sup.2 or OR.sup.1, when R.sup.7 and/or R.sup.10 is OR.sup.1, must be R.sup.3 COXCH(R.sup.4)-- or R.sup.3 COXCH(R.sup.4)O--, respectively.

Abstract: Novel, transient prodrug forms of the phenolic dihydroxy sympathomimetic amines have (i) the structural formula (I): ##STR1## wherein X is O, S or NR.sup.5 ; n is 1 or 2; R.sup.1 is the monodehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 1, and the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 2; R.sup.

Abstract: Novel, transient prodrug forms of dopa and dopamine have (i) the structural formula (I): ##STR1## wherein each R is independently selected from the group consisting of hydrogen, R.sup.3 -CO- and ##STR2## wherein X is O, S or NR.sup.6 ; R.sup.1 is hydrogen or --COOR.sup.8 ; R.sup.2 is hydrogen or OR; R.sup.

Abstract: Novel 3,2'-spiro(1',3'-thiazolidine) compounds which are transient prodrug forms of known 6- and/or 9-haloglucocorticosteroids are described. The subject prodrugs provide improved delivery of the prior art steroids for therapeutic purposes, particularly in alleviating inflammation, and can be prepared by known methods, for example, by reacting the corresponding 3-keto steroids with a thiazolidine forming reagent such as an L-cysteine alkyl ester.