Abstract: Compounds having opioid characteristics are provided that can be used for various therapeutic methods including the treatment of pain and opioid use disorders, and compounds having opioid antagonist properties that can be used to treat opioid overdoses. These compounds include agonists and antagonists having selective activity toward more one or more opioid receptors. Such compounds can be full or partial agonists, or can be antagonists lacking agonist properties toward delta and kappa opioid receptors. The partial agonists can diminish side effects associated with traditional opioid medications, and the antagonists can overcome respiratory depression caused by potent narcotics. Structurally these compounds include constrained piperidines with alkenyl or cyanoalkyl groups, as well as other substituents providing desired properties.

Abstract: The present disclosure is directed to isolated recombinant antibodies, or antigen-binding fragments thereof, that bind to fentanyl or fentanyl analogs. The novel antibodies or antigen-binding fragments thereof can be used to detect, diagnose, treat, and/or prevent opioid use disorder.

Abstract: Described is the preparation of novel fentanyl haptens of Formula (1) through (6) and their use in the preparation of effective fentanyl vaccines.

Abstract: The present disclosure is directed to isolated recombinant antibodies, or antigen-binding fragments thereof, that bind to fentanyl or fentanyl analogs. The novel antibodies or antigen-binding fragments thereof can be used to detect, diagnose, treat, and/or prevent opioid use disorder.

Abstract: The present invention is directed to a compound having Formula (I) and its enantiomer: wherein the definitions of n, R, X, Y and Y3, and Z are provided in the disclosure. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use as opioid-like agonists in the treatment of pain.

Abstract: The present invention is directed to a compound having Formula (I) and its enantiomer: wherein the definitions of n, R, X, Y and Y3, and Z are provided in the disclosure. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use as opioid-like agonists in the treatment of pain.

Abstract: In this application is described a composition and method for inducing in a subject anti-hapten antibodies without inducing antibodies to the carrier protein. Kits for designing and making compositions with desired haptens are also described.

Abstract: In this application Is described a composition and method for Inducing In a subject anti-hapten antibodies without Inducing antibodies to the carrier protein. Kits for designing and making compositions with desired haptens are also described. In this application Is disclosed a synthetic liposome composition comprising liposomes (L) containing monophosphoryl lipid A (MPLA) [L(MPLA)] and an immunoconjugate comprising a carrier and a hapten. In one embodiment, the carrier is a 23 amino acid hydrophobic membrane proximal external region peptide (MPER) derived from the gp41 transmembrane protein of HIV-1 that spontaneously associates with the outer surface of bilayers of liposomes containing MPLA during liposome formation.

Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders, convulsions and parkinsonism. Compounds of particular interest are of the formula ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.

Abstract: Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of an N-(1-thienylcycloalkyl)alkenylamine compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula ##STR1## wherein R.sup.1 is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl and alkoxy; wherein each of R.sup.2 is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl, oxo and alkoxy; wherein R.sup.

Abstract: Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of an N-(1-thienylcycloalkyl)alkenylamine compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.5 are defined in specification.

Abstract: This invention is in the field of clinical neurology and relates specifically to compounds, compositions and methods for treatment of patients with generalized epilepsy or partial (symptomatic) epilepsy using compounds of the formula: ##STR1## This invention also relates to compounds, compositions and methods of treatment for drug craving in patients addicted to cocaine.

Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders and convulsions. Compounds of particular interest are of the formula ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms, and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.

Abstract: A derivative of phencyclidine (1) bearing an isothiocyanate moiety on the meta position of the aromatic ring (3; Metaphit as methanesulfonate and HCl salt) has been synthesized and identified as a rapid and specific site-directed acylating agent of the [.sup.3 H]-phencyclidine binding site in rat brain homogenates. Additional related compounds to Metaphit are Thiophit (oxalate salt), Ethylphit (HCl salt), and Isopropylphit (HCl salt).

Abstract: A derivative of phencyclidine (1) bearing an isothiocyanate moiety of the meta position of the aromatic ring (2; Metaphit) has been synthesized and identified as a rapid and specific site-directed acylating agent of the [.sup.3 H]-phencyclidine binding site in rat brain homogenates.

Abstract: 6-Keto-hydroxymorphinans having at the 4 position a substituent which is R.sub.1 =H, O lower alkyl, or O lower acyl, and N may be substituted by R.sub.2, which for agonist properties may be lower alkyl, lower alkenyl, cyclopropylmethyl, or phenyl lower alkyl, etc. Additionally, the nitrogen may be substituted by R.sub.2, which is allyl, cyclopropylmethyl, cyclobutylmethyl, dimethylallyl, etc., which function as antagonists to the morphine-like activity of the compound. Such activity is known as antinociceptive.

Abstract: This patent application describes the preparation and properties of novel and highly potent morphinan analgesics. The compounds include narcotic agnoists as well as narcotic antagonists and are represented by the following formula: ##STR1## R.sub.1 =OCH.sub.3, OCOCH.sub.3, H R.sub.2 =CH.sub.3, CH.sub.2 --CH.dbd.CH.sub.2, ##STR2## CH.sub.2 CH.sub.2 C.sub.6 H.sub.