Abstract: Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

Abstract: Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapuetics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and nuerodegenerative disease. As cancer therapuetics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.

Abstract: The invention is directed to aza-bridged-bicyclic compounds having Formula (I): 1

Abstract: UCF116 derivatives represented by formula (I): wherein Q represents and R represents hydrogen, C(═O)R1a (wherein R1a represents methyl, ethyl, propyl, isopropyl, 2,2-dimethylpropyl, pentyl, alkyl having 6 to 10 carbon atoms, 1-propenyl, isopropenyl, 2-methyl-1-propenyl, substituted or unsubstituted alicyclic alkyl having 3 to 5 carbon atoms, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aralkyloxy, or substituted lower alkyl), C(═X)NHR1b (wherein X represents an oxygen or sulfur atom, and R1b represents substituted or unsubstituted lower alkyl, substituted or unsubstituted alicyclic alkyl, substituted or unsubstituted lower alkoxycarbonyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, or a substituted or unsubstituted heterocyclic group), or SO2R1c (wherein R1c represents substituted or unsubstituted lower alkyl, substituted or uns

Abstract: An essentially pure noribogaine compound having the formula: wherein R is hydrogen or a hydrolyzable group of the formula: wherein X is an unsubstituted C1-C12 group or a C1-C12 group substituted by lower alkyl or lower alkoxy groups, wherein the noribogaine compound having the hydrolyzable group hydrolyzes in vivo to form 12-hydroxy ibogamine.

Abstract: This invention is directed to novel tricyclic ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions of such tricyclic compounds, plus the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, and for the prevention of ischemic injury.

Abstract: Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

Abstract: This invention relates to certain squalene synthetase inhibitors useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, anti-Alzheimer's agents or anti-acne agents.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of phenyl derivatives of imidazolone compounds of Formula I. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: The presently claimed process provides a method for preparing compounds of the formula ##STR1## phosphorous (III) compound and a diester of azodicarboxylate.

Abstract: The subject invention concerns a process for preparing a compound of formula (3) ##STR1## in enantio-enriched form, comprising reducing a compound of formula (4) ##STR2## using an asymmetric enantiospecific reductant, wherein A.sup.1 .dbd.A.sup.2 .dbd.H or A.sup.1, A.sup.2 .dbd.O; B.sup.1 .dbd.B.sup.2 .dbd.H or B.sup.1, B.sup.2 .dbd.O; Z.dbd.H, C.sub.1-20 alkyl or a precursor thereof, or a removable protecting group for nitrogen, e.g, acyl or alkyloxycarbonyl; Y.dbd.H or a substituent; R.sup.1 .dbd.C.sub.1-20 alkyl; and R is an optional, additional substituent.

Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole, and triazoles, in particular those including a cycloheptane structure, that are useful as serine protease inhibitors, including inhibitors for human neutrophil elastase. Compounds of the invention are useful in treating conditions such as adult respiratory distress syndrome, septic shock, and multiple organ failure.

Abstract: This invention is directed to novel tricyclic ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions of such tricyclic compounds, plus the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, and for the prevention of ischemic injury.

Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.

Abstract: Disclosed are methods of preparing azepines by a multistep synthesis including a Diels-Alder reaction. Also disclosed are methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment an azepine which has high binding to the NMDA glycine site.

Abstract: Compounds having the formula ##STR1## methods for using such compounds to inhibit protein kinase C in animals, including man are useful as inhibitors of protein kinase C. Also disclosed are pharmaceutical compositions including such compounds and compounds having the formula.

Abstract: The method for assaying the SOD (super oxide dismutase) activity in liquid medium is based on the activation of self-oxidization, by SOD activity, of a reactive agent having the general formula (I) wherein either n is 1 or 2, R.sup.1 is --OR.sup.4 or --NR.sup.5 R.sup.6 ; R.sup.2 is H, --OR.sup.4, alkyl (1-6C), --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --, to form a ring by binding to the phenyl substituent, at meta with respect to R.sup.1 ; and R.sup.3 is H, alkyl (1-6C) or --OR.sup.4 (if R.sup.2 is different from --OR.sup.4); with R.sup.4 being H or alkyl (1-6C); R.sup.5 being H, alkyl (1-6C), --CH.sub.2 COOH, --C.sub.6 H.sub.5 COOH or --C.sub.6 H.sub.5 SO.sub.3 H; and R.sup.6 is H, alkyl (1-6C) or --CH.sub.2 COOH; or n is 1, R.sup.1 is --OR.sup.4, R.sup.2 is --CH.sub.2 --O--, in order to form a ring by bonding of O with the phenyl substituent, at meta with respect to R.sup.1 ; and R.sup.3 is H or --OR.sup.4.

Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide derivatives which are useful as inhibitors of enkephalinase and ACE.

Abstract: The present invention relates to novel aminoacetylmercapto derivatives useful as inhibitors of enkephalinase and ACE.

Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## are useful as ACE and NEP inhibitors and those wherein A is ##STR3## are useful as ACE inhibitors. Methods of preparation and intermediates are also disclosed.

Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide tricyclic derivatives which are useful as inhibitors of Enkephalise.

Abstract: The present invention relates to novel 2-substitited indane-2-mercaptoacetylamide tricyclic derivatives which are useful as inhibitors of Enkephalise.

Abstract: The present invention relates to novel 2-substituted indane-2-mercaptoacetylamide derivatives which are useful as inhibitors of enkephalinase and ACE.

Abstract: The present invention relates to novel 2-substitited indane-2-mercaptoacetylamide tricyclic derivatives which are useful as inhibitors of Enkephalise.

Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a 3-azabicyclo[3.2.2]-nonanyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.

Abstract: The present invention is directed toward anionic polymerization initiators which are soluble in hydrocarbon solvents. The initiators include a lithio amine having the general formula ALi. The component A is a dialkyl or dicycloalkyl amine radical or a cyclic amine. The invention is also directed toward polymers and other products made using the initiator, and methods therefor. Further, the invention contemplates a polymer, a polymer composition and products therefrom, which include a functional group from the reaction product of an amine and an organolithium compound. The resulting polymers may be terminated with a terminating, coupling or linking agent, which may provide the polymer with a multifunctionality.

Abstract: The invention provides novel 2,3,6 substituted quinazolinones having the formula: ##STR1## wherein R.sup.6, R and X are as described in the specification, which have activity as angiotensin II (AII) antagonists.

Abstract: Pharmacologically active compounds corresponding to the general formula I ##STR1## in which R.sup.1 represents hydrogen, a lower alkyl or cycloalkyl-alkyl group or an optionally substituted phenyl-lower alkyl group,R.sup.2 denotes hydrogen or a lower alkyl group optionally substituted in the .alpha.-position to the nitrogen atom by lower alkoxy,R.sup.3 denotes hydrogen, lower alkyl, lower alkoxy, halogen or hydroxyl,n represents 1 or, if the --(CH.sub.2).sub.n -- chain is in the 4-position of the ring structure, also represents 2,R.sup.4 denotes hydrogen, lower alkyl, cycloalkyl, cycloalkyl-lower alkyl or an optionally substituted phenyl-lower alkyl group, andR.sup.5 denotes hydrogen, lower alkyl, cycloalkyl, cycloalkyl-lower alkyl or an optionally substituted phenyl-lower alkyl group, orR.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, form a heterocycle andD represents a bond, or, if R.sup.4 and R.sup.5 do not denote hydrogen, also represents the --N.dbd.

Abstract: A series of bridged bicyclic imide compounds having a 4-(4-[2-pyrimidinyl]-1-piperazinyl)butyl group attached to the imide nitrogen are useful for alleviating the symptoms of anxiety and depression in human subjects.

Abstract: A process for synthesizing polyoxa tetracyclics which involves the ozonolysis of a single-ring-structure vinyl silane with resulting direct formation of the desired multiple ring material. The polyoxa tetracyclic compounds have the formula ##STR1## The vinyl silanes have the structure ##STR2## The vinyl silanes are new chemical compounds as are corresponding primary ozonide and dioxetane intermediates. In a preferred embodiment, this invention provides a total synthesis of the antimalarial artemisinin.

Abstract: The compounds ##STR1## in which Z is ##STR2## where R.sup.4 is -H or alkyl; q is one of the integers 0, 1 or 2; Y is H.sub.2 or O; or Z, taken with R.sup.1 forms ##STR3## R.sup.1 is hydrogen or alkyl or combined with Z as described above; R.sup.2 and R.sup.3 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, carbamoyl or sulfonamido or R.sup.2 and R.sup.3, taken together are methylenedioxy, ethylenedioxy or propylenedioxy; m is one of the integers 1, 2 or 3; n is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are antipsychotic, antidepressant and anxiolytic agents useful in relieving the symptoms of these disease states.

Abstract: The compounds ##STR1## in which Z is ##STR2## where R.sup.4 is --H or alkyl; q is one of the integers 0, 1 or 2; Y is H.sub.2 or O; or Z, taken with R.sup.1 forms ##STR3## R.sup.1 is hydrogen or alkyl or combined with Z as described above; R.sup.2 and R.sup.3 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, carbamoyl or sulfonamido or R.sup.2 and R.sup.3, taken together are methylenedioxy, ethylenedioxy or propylenedioxy; m is one of the integers 1, 2 or 3; n is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are antipsychotic, antidepressant and anxiolytic agents useful in relieving the symptoms of these disease states.

Abstract: The present invention is directed to 5-HT.sub.3 receptor antagonist compounds of formula I: ##STR1## in which the dashed line denotes an optional double bond;n is 1, 2 or 3;p is 0, 1, 2 or 3;q is 0, 1 or 2;each R.sup.1 is independently selected from halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, amino carbonyl, (lower alkyl)amino, di(lower alkyl)amino, and (lower alkanoyl)amino;each R.sup.2 is lower alkyl; andR.sup.3 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## in which u is 0 or 1;z is 1, 2 or 3; andR.sup.4 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sup.5 where t is 1 or 2 and R.sup.5 is thienyl, pyrrolyl, or furyl, each optionally further substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.

Abstract: Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture.

Abstract: Disclosed herein are novel benzisothiazole derivatives having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of a variety of central nervous system disorders.

Abstract: A process for synthesizing polyoxa tetracyclics which involves the ozonolysis of a single-ring-structure vinyl silane with resulting direct formation of the desired multiple ring matrial. The polyoxa tetracyclic compounds have the formula ##STR1## The vinyl silanes have the structure ##STR2## The vinyl silanes are new chemical compounds as are corresponding primary ozonide and dioxetane intermediates. In a preferred embodiment, this invention provides a total synthesis of the antimalarial artemisinin.

Abstract: The synthesis of ring-fused thienopyrimidinedione derivatives is described. The novel ring-fused thienopyrimidinedione derivatives are generally vasodilating agents and antihypertensive agents and as such are useful as cardiovascular agents.

Abstract: The invention relates to new anellated indole derivatives of general formula 2, ##STR1## wherein p1 R.sub.0 is alkyl or alkoxy having 1-4 C-atoms, phenylalkoxy having 1-3 C-atoms in the alkoxy group, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, or a group R.sub.7 S(O).sub.p, wherein R.sub.7 is alkyl having 1-4 C-atoms and p has the value 0, 1 or 2, or R.sub.0 is a group R.sub.8 R.sub.9 N, R.sub.8 R.sub.9 N--CO--CH.sub.2 -- or R.sub.8 R.sub.9 --N--CO wherein R.sub.8 and R.sub.9 are hydrogen or alkyl having 1-4 C-atoms or R.sub.8 R.sub.9 N forms a saturated 5- or 6-membered ring and n has the value 0, 1 or 2, Z together with the carbon atom and nitrogen atom to which Z is bound and the intermediate carbon atom, forms a heterocyclic group consisting of 5-8 ring atoms, in which, in addition to the nitrogen atom already present, a --CO--group or a second hetero atom from the group N, O, S, S-O or SO.sub.

Abstract: This invention relates to a selective process for preparing bicyclic lactam-lactone compounds wherein the rings are fused, i.e. the rings share at least two carbon atoms, or are isolated. In particular, the present invention provides a process for selectively reacting novel 1-hydrocarbylamino (or heteroatom-substituted hydrocarbylamino); 1,1-dicarboxylic acid, alkylesters; 1-alkanolactonyl or hydrocarbyl (or heteroatom-substituted hydrocarbyl) alkanonylactonyl methane, as the salt of an acid having a pKa of 0 or more, to provide bicyclic lactam-lactone compounds. The selectively of the reaction to either fused or isolated bicyclic compounds is controlled by cyclizing the novel salts, in the absence of a base, a cyclizing said novel salts, in the presence of an amount of base substantially equivalent to said acid, respectively.

Abstract: 1,2,4-Triazolo[4,3-d]-4-azatricyclo[4.3.1.1.sup.3,8 ]-undecane and 3-derivatives and intermediates thereof are described. The compounds are useful and antiinflammatory and antihypoxia agents.

Abstract: Novel phenylserine derivatives of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions, and a process for preparing the compounds are disclosed. The phenylserine derivatives and pharmaceutically acceptable acid addition salts are capable of inhibiting the biosynthesis of leucotrienes and/or antagonistic activity against SRS-A and hence are useful for prophylaxis and treatment of various allergic diseases (e.g. bronchial asthma, allergic nasitis, urticaria), ischemic heart diseases, ischemic encephalopathy, inflammation, or the like.

Abstract: Zwitterionic bicyclic compounds are disclosed which are useful as anti-allergic, anti-inflammatory and/or cytoprotective agents. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.

Abstract: Microbicidally active novel 1-heteroaryl-4-aryl-pyrazolin-5-ones of the formula ##STR1## in which R represents hydrogen or alkyl,R.sup.1 represents halogen, hydroxyl, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted phenoxy, a radical --S(O).sub.p -- alkyl which is optionally substituted in the alkyl part, nitro, optionally substituted amino or a fused-on carbocyclic or heterocyclic radical,p represents an integer 0, 1 or 2,R.sup.2 represents halogen or optionally substituted alkyl, or represents alkoxy, alkylmercapto, nitro, cyano, carboxamide or a fused-on carbocyclic radical,m represents an integer from 0 to 5,n represents an integer from 0 to 4, it being possible for the substituents to be identical or different when m and/or n represent a number greater than 1, andX, Y and Z are identical or different and represent a nitrogen atom or the radical .dbd.CH or ##STR2## wherein R.sup.