Abstract: Disclosed are benztropine and CFT analogs useful for imaging of cocaine receptors and treatment of cocaine abuse. Also disclosed are analogs useful for imaging and treatment of Parkinson's disease.

Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a 3-azabicyclo[3.2.1]-oct-8-yl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.

Abstract: A benzamide derivative represented by the following formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkanoyl group; R.sup.2 represents a hydrogen atom or a halogen atom; R.sup.3 represents a lower alkoxy group; R.sup.4 represents a hydrogen atom or a lower alkyl group; R.sup.5 represents a hydrogen atom, a lower alkyl group, or a lower alkoxy group; A represents C.sub.1 -C.sub.7 alkylene group which may optionally be substituted with a lower alkyl group; X represents a methylene group, an oxygen atom, or a sulfur atom; m represents an integer of from 0 to 3; n represents an integer of from 0 to 3; and p represents an integer of from 0 to 2 and a pharmacologically acceptable salt thereof is provided. These compounds are useful since they have gastrointestinal stimulating activity, and a pharmaceutical composition comprising said compound is useful for the treatment of gastrointestinal diseases.

Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

Abstract: The present invention relates to a novel class of benzoylecgonine, ecgonine and ecgonidine derivatives which are useful for preventing and treating immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. The compounds of this invention are conveniently obtained by chemical synthesis. Accordingly, this invention also relates to methods for preparing the benzoylecgonine, ecgonine and ecgonidine derivatives and to pharmaceutical compositions containing these derivatives.

Abstract: Compounds are provided for the preparation of reagents, including labels which can be used in immunoassays of cocaine and cocaine metabolites. The compounds are derivatives of cocaine which are conjugated to antigenic proteins or polypeptides for the formation of antibodies for use in immunoassays. The compounds also may be conjugated to labels for use in immunoassays.

Abstract: The present invention is directed to a fluorescence polarization assay for benzoyl ecgonine and substituted benzoyl ecgonine compounds in biological fluids, and to a method of making reagents therefor. Specifically, tracers, immunogens and antibodies are disclosed. The tracers and the immunogens are made from substituted benzoyl ecgonine compounds. A fluorescein moiety is included in the tracer, while a poly(amino acid) forms a part of the immunogen. The assay is conducted by measuring the degree of polarization retention of plane polarized light that has been passed through a sample containing antiserum and tracer.

Abstract: Aroyl ureas and carbamic acid derivatives of formulaA--CO--NHCW--Y--Band pharmaceutically acceptable salts thereof whereinA is a specified aromatic radical including optionally substituted phenylW is O or SY is NH or S andB is a specified saturated azacyclic ring, eg tropan-3-yl or quinuclidin-3-yl,possess 5-HT.sub.3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.

Abstract: A process for the preparation of vinyl carbamates of formula I ##STR1## is described which comprises heating an .alpha.-halogeno-carbamate of formula II ##STR2## in which X is a halogen atom at a temperature between 70.degree. and 250.degree. C. for a period of time between several minutes up to several hours. R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are the same or different. The process is applicable to a great variety of products in which R.sub.1, R.sub.2, R.sub.3, and R.sub.4 have different meanings. The process permits to prepare in a simple and economical fashion, vinyl carbamates, which have industrial value and novel vinyl carbamates.

Abstract: Compounds of the formula ##STR1## wherein Ar is ##STR2## R.sub.1 is hydrogen, fluorine, bromine, methyl or methoxy; X is .dbd.CO, .dbd.CH--CN, .dbd.CH--OH, --O--, --S--, --NH--, ##STR3## and R is hydrogen, 4-fluoro, 4-chloro, 4-trifluoromethyl, 3-trifluoromethyl, 3-trifluoromethyl-4-chloro, 4-methyl or 4-methoxy;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as neuroleptics.

Abstract: The invention relates to novel nortropine-carbazate derivatives of the general formula (I), ##STR1## wherein R.sub.1 is C.sub.1-4 alkyl, phenyl or halophenyl group,R.sub.2 is hydrogen or a C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkyl, C.sub.1-4 acyl, phenoxycarbonyl or C.sub.1-4 alkoxycarbonyl group, andR.sub.3 is hydrogen of a C.sub.1-4 alkyl or C.sub.1-4 acyl group, orR.sub.2 and R.sub.3 may form together a C.sub.1-10 alkylene group attachedTo the nitrogen atom with a double bond, as well as to pharmaceutically acceptable acid addition salts of said compounds.The above compounds are new and can be applied as narcosis potentiating agents.The compounds of the general formula (I) can be prepared by reacting a compound of the general formula (II), ##STR2## wherein R.sub.1 is as defined above and Q is halogen, C.sub.1-4 alkoxy or phenoxy, with a hydrazine compound of the general formula (III), ##STR3## wherein R.sub.2 and R.sub.3 are as defined above.