Abstract: wherein: R1 is a moiety selected from: R2 is CH2CH2CONH2 or CH2CH2OH; R3 and R4 are independent substituents selected from the group including H, —N(CH3)2, or —OCH3; or pharmaceutically acceptable salts thereof.

Abstract: The present invention provides compounds of the general formula: wherein W is O or NH, optionally substituted, as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.

Abstract: The present invention relates to pharmaceutical compositions containing benzo[a]carbazoles or indenoindoles, which are useful as tissue selective estrogenic agents, having the general structures below: ##STR1## and one or more estrogens and methods of treatment utilizing these formulations.

Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below: ##STR1##

Abstract: The present invention relates to new substituted benzo[a]carbazoles and indenoindoles which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, having the general structures below.

Abstract: The present invention provides compounds of the general formula: ##STR1## wherein W is O or NH, optionally substituted, as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.

Abstract: The present invention relates to new substituted benzo[a]carbozoles and indenoindoles which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, having the general structures below.

Abstract: The present invention provides compounds represented by the general formula (1) whereinR.sub.1 is selected from H, OH, OR.sub.2 or halogen (F, Cl, Br, I);R.sub.2 is lower alkyl (C.sub.1 to C.sub.6);n is selected from 0, 1 or 2;X is CH or CH.sub.2 ;m is selected from 2, 3 or 4;Y is N or CH.sub.2 ;Ar is aryl or heteroaryl, both optionally substituted;or pharmaceutically acceptable salts thereof, as well as methods and pharmaceutical compositions utilizing these compounds for the inhibition of serotonin uptake and the treatment of CNS disorders, particularly depression.

Abstract: This invention relates to a process for the preparation of the formula I compound [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid, a NMDA antagonist useful as an anticonvulsant and neuroprotectant in situations involving excess release of excitatory amino acids. ##STR1## In the process of the present invention, 3-aminopropyl carbamic acid 1,1-dimethyl-ethyl ester is reacted with a dialkyl vinylphosphonate to obtain N-[3-(t-butyloxycarbonyl-amino)propyl ]-2-aminoethylphosphonic acid dialkyl ester (d) in 80% yield Reaction of (d) with a 3,4-dialkoxycyclobut-3-en-1,2-dione gives [3-[[2-(dialkoxyphosphoryl)ethyl ]-(2-alkoxy-3,4-dioxo-1,2-cyclobuten-1-yl)amino]propyl] carbamic acid 1,1-dimethylethyl ester (e) in 96% yield. Deprotection and cyclization of (e) in trifluoroacetic acid gives [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]prosphonic acid dialkyl ester (c) in 58% yield.

Abstract: The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are, independently, selected from H; C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are independently selected from H, halogen, --NO.sub.2, alkyl, alkoxy, C.sub.1 -C.sub.6 perfluorinated alkyl, OH or the C.sub.1 -C.sub.4 esters or alkyl ethers thereof, --CN, --O--R.sup.1, --O--Ar, --S--R.sup.1, --S--Ar, --SO--R.sup.1, --SO--Ar, --SO.sub.2 --R.sup.1, --SO.sub.2 --Ar, --CO--R.sup.1, --CO--Ar, --CO.sub.2 --R.sup.1, or --CO.sub.2 --Ar; and Y is selected from a) the moiety: ##STR2## wherein R.sub.7 and R.sub.8 are independently selected from the group of H, C.sub.1 -C.sub.

Abstract: The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below: ##STR1##

Abstract: This invention relates to a process for the preparation of the formula I compound [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid, a NMDA antagonist useful as an anticonvulsant and neuroprotectant in situations involving excess release of excitatory amino acids. ##STR1## In the process of the present invention, 3-aminopropyl carbamic acid 1,1-dimethylethyl ester is reacted with a dialkyl vinylphosphonate to obtain N-[3-(t-butyloxycarbonyl-amino)propyl]-2-aminoethylphosphonic acid dialkyl ester (d) in 80% yield. Reaction of (d) with a 3,4-dialkoxycyclobut-3-en-1,2-dione gives [3-[[2-(dialkoxyphosphoryl)ethyl]-(2-alkoxy-3,4-dioxo-1,2-cyclobuten-1-yl) amino]propyl] carbamic acid 1,1-dimethylethyl ester (e) in 96% yield. Deprotection and cyclization of (e) in trifluoroacetic acid gives [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid dialkyl ester (c) in 58% yield.

Abstract: The present invention provides improved devices for inserting solid materials under a tissue, the devices particularly containing a penetration guide means designed to facilitate the implantation by limiting the insertion of the implants to positions under and substantially parallel to the plane of the tissue.

Abstract: The present invention relates to new 3-[4-(2-Phenyl-Indole-1-ylmethyl)-Phenyl]-Acrylamide compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, the compounds having the following general structure.

Abstract: Tricyclic diazepines of the formula: wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.

Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.

Abstract: This invention discloses organoleptically acceptable formulations containing non-solubilized S(+) 1,8-diethyl-1,3,4,9-tetrahydropyrano?3,4-b!indole-1-acetic acid, preferably with an acidic component, also known as S(+)etodolic acid or S(+)etodolac.

Abstract: This invention relates to 2- or 3-(substituted aminoalkoxyphenyl)quinazolin-4-ones which are partial estrogen agonists and are useful in treating osteoporosis, prostatic hypertrophy, breast cancer and endometrial cancer.