Abstract: The invention provides compounds, compositions, and methods for treating pain.

Abstract: The invention provides compounds, compositions, and methods for treating pain.

Abstract: and salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using a compound of formula I.

Abstract: and salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using a compound of formula I.

Abstract: The present invention relates to conjugates and vaccine compositions for treatment of opioid addiction, and methods of use of these conjugates and compositions.

Abstract: The invention provides a compound of formula (I) or a salt thereof, as well as compositions comprising such compounds. The compounds and compositions are useful as analgesics.

Abstract: The invention provides a compound of formula (I) or a salt thereof, as well as compositions comprising such compounds. The compounds and compositions are useful as analgesics.

Abstract: The present invention relates generally to analgesic compounds having a mu opioid receptor agonist linked to a delta opioid receptor antagonist, and to methods for producing analgesia using such compounds. As compared to opioids such as morphine, these compounds can cause less tolerance, physical dependence, and/or constipation. These compounds are also more potent than morphine and are able to cross the blood brain barrier, thereby allowing for peripheral (e.g., IV) administration.

Abstract: The invention provides kappa receptor agonists of formula (I) and delta receptor antagonists of formula (II), wherein R1–R6 X and n have any of the meanings given in the specification, as well as compositions comprising them, methods for their use, and synthetic procedures and intermediates useful for their preparation.

Abstract: The invention provides kappa receptor agonists of formula (I) and delta receptor antagonists of formula (II), wherein R1-R6 X and n have any of the meanings given in the specification, as well as compositions comprising them, methods for their use, and synthetic procedures and intermediates useful for their preparation.

Abstract: Compounds of the formula: are provided, which are selective kappa opioid receptor antagonists, wherein R1 is (C1-C5)alkyl, C3-C6(cycloalkyl)alkyl, C5-C7(cycloalkenyl)alkyl, (C6-C12)aryl, (C6-C12)aralkyl, trans(C4-C5)alkenyl, allyl or furan-2-ylalkyl, R2 is H, OH or O2C(C1-C5)alkyl; R3 is H, (C6-C10)aralkyl, (C1-C5)alkyl or (C1-C5)alkylCO; X is O, S or NY, wherein Y is H or (C1-C5) alkyl; R4 is CH2 (methylene) or C═O (carbonyl), R5 is CH2, C═O or C═NH (imino) and R6 is (C1-C4)alkyl or NH(C1-C4)alkyl, optionally substituted by a non-terminal (C1-C2)alkyl group or by N(R7)(R8) wherein R7 and R8 are individually H or (C1-C3)alkyl, with the proviso that one of R4 or R5 is CH2, and the pharmaceutically acceptable salts thereof.

Abstract: The invention provides kappa receptor antagonists of formula (I), wherein R1-R6 X and Y have any of the meanings given in the specification, as well as compositions comprising them, and methods for their use.

Abstract: A delta-selective opioid receptor antagonist is provided of the formula: wherein R1 is (C1-C3)alkyl, C3-C6(cycloalkyl)alkyl, C5-C7(cycloalkenyl)alkyl, aryl, aralkyl, trans-(C4-C5)alkenyl, allyl or furan-2-ylalkyl, R2 is H, OH or O2C(C1-C5)alkyl; R3 is H, (C1-C5)alkyl; or ((C1-C5)alkyl)-C═O; and R4 and R5 are individually H, F, Cl, Br, NH2, NO2, (C1-C5)alkyl or (C1-C5)alkoxy, or R4 and R5 together are benzo or dioxymethylene; and the pharmaceutically acceptable salts thereof.

Abstract: The invention provides certain amino acid conjugates of substituted 2-phenyl-N-?1-(phenyl)-2-(1-heterocycloalkyl- or heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid receptors in mammalian tissue.

Abstract: A therapeutic method is provided to elevate a depressed mammalian autologous mixed lymphocyte response and to alleviate the diseases associated therewith by the administration of an effective amount of certain selective delta opioid receptor antagonists to a mammal such as a human patient in need of such treatment.

Abstract: Compounds are provided of the formula: ##STR1## wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.6 -C.sub.12)aralkyl, trans(C.sub.4 -C.sub.5)alkenyl, allyl or furan-2-ylalkyl, R.sup.2 is H, OH or O.sub.2 C(C.sub.1 -C.sub.5)alkyl; R.sup.3 is H, (C.sub.6 -C.sub.10)aralkyl, (C.sub.1 -C.sub.5)alky or (C.sub.1 -C.sub.5)alkylCO; X is O, S or NY, wherein Y is H, benzyl or (C.sub.1 -C.sub.5)alkyl; R is CH(Z)CO.sub.2 Y, wherein Z is H, CH.sub.2 CO.sub.2 Y or (CH.sub.2).sub.n N(R.sup.4)(R.sup.5), wherein n is 1-5 and R.sup.4 and R.sup.5 are individually H, (C.sub.1 -C.sub.4)alkyl, phenyl, (C.dbd.NH)NH.sub.2, benzyloxycarbonyl or (C.dbd.NHNO.sub.2); and the pharmaceutically acceptable salts thereof.

Abstract: A therapeutic method is provided to elevate a depressed mammalian autologous mixed lymphocyte response and to alleviate the diseases associated therewith by the administration of an effective amount of certain selective delta opioid receptor antagonists to a mammal such as a human patient in need of such treatment.

Abstract: Compounds of the formula: ##STR1## are provided, which are selective kappa opioid receptor antagonists, wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.6 -C.sub.12)aralkyl, trans (C.sub.4 -C.sub.5) alkenyl, allyl or furan-2-ylalkyl; R.sup.2 is H, OH or O.sub.2 C(C.sub.1 -C.sub.5)alkyl; R.sup.3 is H, (C.sub.6 -C.sub.10)aralkyl, (C.sub.1 -C.sub.5)alkyl or (C.sub.1 -C.sub.5)alkylCO; X is O, S or NY, wherein Y is H or (C.sub.1 -C.sub.5)alkyl; R.sup.4 is CH.sub.2 (methylene) or C.dbd.O (carbonyl), R.sup.5 is CH.sub.2, C.dbd.O or C.dbd.NH (imino) and R.sup.6 is (C.sub.1 -C.sub.4)alkyl or NH(C.sub.1 -C.sub.4)alkyl, optionally substituted by a non-terminal (C.sub.1 -C.sub.2)alkyl group or by N(R.sup.7) (R.sup.8) wherein R.sup.7 and R.sup.8 are individually H or (C.sub.1 -C.sub.3) alkyl, with the proviso that one of R.sup.4 or R.sup.5 is CH.sub.2, and the pharmaceutically acceptable salts thereof.

Abstract: A therapeutic method is provided to inhibit the use of cocaine by the administration of an effective amount of certain selective delta opioid receptor antagonists to a human patient in need of such treatment.

Abstract: A motion provided to alleviate the tolerance to, or dependence on, an opiate analgesic, by the administration of an effective amount of a selective delta opioid receptor antagonist to a human patient in need of such treatment.