Abstract: The present invention relates to novel compounds of the general formula I ##STR1## which can be used for treating medical disorders resulting from a deficiency in growth hormone.

Abstract: Diketopiperazines of formula (A): ##STR1## wherein each of R.sub.1 to R.sub.8 is H or an organic radical as described herein and the pharmaceutically acceptable salts thereof have activity as inhibitors of plasminogen activator inhibitor.

Abstract: Diketopiperazines of the formula ##STR1## where one or both of R.sub.1 and R.sub.2, which are different, are chosen from X and a phenyl group substituted by X, C(O)X, OC(O)CH.sub.2 X, OCH.sub.2 CH.sub.2 X, CH.sub.2 X, CONH(CH.sub.2).sub.n X, O(CH.sub.2).sub.n CH(OH)(CH.sub.2).sub.n X ##STR2## and, where appropriate, the other of R.sub.1 and R.sub.2 is a phenyl group optionally substituted by one or more groups selected from halogen, nitro, methoxy, NHC(O)R.sub.12, CO.sub.2 H, O(CH.sub.2).sub.n N(R.sub.12 R.sub.13), C.sub.1 -C.sub.4 alkyl and (CH.sub.2).sub.n C(O)OR.sub.12 ; X is a five- or six-membered heterocyclic ring selected from the group consisting of pyridyl, imidazolyl, furyl, pyrrolyl, pyrrolidinyl, thienyl, piperazinyl, piperidinyl, morpholinyl, quinolyl, isoquinotyl and indolyl, the heteroatom(s) of the said heterocyclic ring, when nitrogen, being optionally substituted by hydrogen, methyl, oxygen, tertiary-butyloxycarbonyl, or SO.sub.

Abstract: The present invention relates to a 2,3-diketopiperazine derivative or a salt thereof, which has inhibitory effect on platelet aggregation because of glycoprotein IIb/IIIa receptor antagonism and hence is useful as a prophylactic and therapeutic agent for diseases associated with platelet aggregation. General formula: ##STR1## wherein R.sup.1 represents a protected or unprotected amidino group; R.sup.2 represents a hydrogen atom or a carboxyl-protecting group; A represents a substituted or unsubstituted lower alkylene group; B represents --O--, --CONH--, --NHCO--or --SO.sub.2 NH--; Y represents a substituted or unsubstituted lower alkylene group; and the broken line represents a single bond or a double bond.

Abstract: Weatherable polycarbonate compositions (formulations or blends) comprise at least one of a piperazinone and piperazine dione based HALS, and at least one of a benzotriazole, benzophenone, triazine, oxanilide, and cyanoacrylate based UVA. The combination of these HALS and UVA exhibits a synergy that results in enhanced protection of the polycarbonate compositions by imparting photostability to the polycarbonate formulations, thereby reducing yellowing or other forms of light induced degradation.

Abstract: Piperazine derivatives of the formula ##STR1## their esters and salts are useful as modulators of multiple drug resistance.

Abstract: The instant invention relates to weatherable polycarbonate compositions (formulations or blends) comprising piperazinone or piperazine dione based HALS. These piperazinone or piperazine dione based HALS impart photostability to the polycarbonate formulations, thereby reducing yellowing or other forms of light induced degradation.

Abstract: Piperazine derivatives of formula (A): ##STR1## wherein .sub.-------- denotes an optional bond, provided that either .sub.----.sup.a.sub.---- and .sub.----.sup.c.sub.---- are both bonds and .sub.----.sup.b.sub.---- and .sub.----.sup.d.sub.---- are not bonds, or .sub.----.sup.b.sub.---- and .sub.----.sup.d.sub.---- are both bonds and .sub.----.sup.a.sub.---- and .sub.----.sup.c.sub.---- are not bonds; each of R.sub.14 and R.sub.15 is independently selected from hydrogen and C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by an organic functional group; and each of R.sub.1 to R.sub.10, which may be the same or different, is independently hydrogen or an organic functional group; and the pharmaceutically acceptable salts and esters thereof have utility as modulators of multiple drug resistance (MDR).

Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: A diketopiperazine of formula (I): ##STR1## wherein each of R.sub.7 and R.sub.8 which may be the same or different; is hydrogen or a nitro group;Y is ##STR2## --O-- or --S--, wherein each of R.sub.9 and R.sub.10 which may be the same or different, is hydrogen or a nitro group;n is 0, 1 or 2;m is an integer of 1 to 6;each R.sub.6, which may be the same or different, is a C.sub.1 -C.sub.6 alkyl group; andX is selected from(i) a phenyl group of the following formula ##STR3## and the salts and esters thereof; have activity as inhibitors of plasminogen activator inhibitor.

Abstract: The present invention relates to a farnesyltransferase inhibitor and an antitumor agent comprising, as an active ingredient, a piperazinedione derivative represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 independently represent lower alkyl, lower alkoxyalkyl, substituted or unsubstituted aryl, or aralkyl; R.sup.3 and R.sup.4 independently represent mercapto, lower alkanoylthio, aroylthio, lower alkoxycarbonylthio, or aryloxycarbonylthio, or alternatively R.sup.3 and R.sup.4 are combined together to form disulfide; and R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, lower alkoxyalkyl, hydroxyalkyl, lower alkanoyloxyalkyl, aroyloxyalkyl, aralkyloxyalkyl, or aralkyl.

Abstract: The use of glycine anhydride dimethylol, also known as 1,4-bis(hydroxymethyl)-2,5-piperazinedione, comprising the formula ##STR1## to kill microorganisms present in or on a host substance and to preserve products susceptible to contamination by a variety of microorganisms is disclosed.

Abstract: Diketopiperazines of the formula: ##STR1## where each of R.sub.1 to R.sub.10, which may be the same or different, is independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by one or more halogen atoms, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, halogen, hydroxy, nitro, phenyl, -cyano, --CH.sub.2 OH, --CH.sub.2 COOH, --CO.sub.2 R.sup.11, --NHCOR.sup.11, --NHSO.sub.2 R.sup.13, --SO.sub.2 R.sup.13, --CON(R.sup.11 R.sup.12), --SOR.sup.13, --SO.sub.2 N(R.sup.11 R.sup.12), --N(R.sup.11 R.sup.12), and --O(CH.sub.2).sub.n N(R.sup.11 R.sup.12), --O(CH.sub.2).sub.n CO.sub.2 R.sup.11, --OCOR.sup.11, --CH.sub.2 OCOR.sup.11, --CH.sub.2 NHCOR.sup.11, --CH.sub.2 NHCOOR.sup.13, --CH.sub.2 SR.sup.11, --CH.sub.2 SCOR.sup.11, --CH.sub.2 S(O).sub.m R.sup.13 wherein m is 1 or 2, --CH.sub.2 NHCO(CH.sub.2).sub.n CO.sub.2 R.sup.11, --N(R.sup.11)COR.sup.12, --NHCOCF.sub.3, --NHCO(CH.sub.2).sub.n CO.sub.2 R.sup.11, --NHCO(CH.sub.2).sub.n OCOR.sup.11 and --NHCO(CH.

Abstract: A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl;Y is a direct bond or lower alkylene; andR.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein. The compounds are advantageously used as Tachykinin antagonists in the treatment of respiratory diseases, ophthalmic diseases and inflammatory diseases, for example.

Abstract: The invention is directed to a series of novel piperazinylcamphorsulfonyl compounds where the camphor ring is substituted by amides, amines, alkanes, alkenes, alkylamines, halogens, hydroxy, carboxy, alkoxycarbonyl and heterocyclic tings. Such compounds are oxytocin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery.

Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.

Abstract: Piperazine compounds and salts thereof having inhibitory effect against superoxide radicals (O.sub.2.sup.-). The piperazine compounds have the general formula: ##STR1## wherein R.sup.1 is a lower alkyl group;R.sup.2 is a phenyl-lower alkyl group which may have 1 to 3 substituents, on the phenyl ring, selected from the group consisting of a hydroxyl group, a phenyl-lower alkoxy group, a lower alkyl group, a lower alkoxy group and a halogen atom;R.sup.3 is a hydrogen atom, a lower alkyl group or a phenyl-lower alkyl group; andR.sup.4 is a hydroxyl group, a phenyl-lower alkoxy group or a tetrahydropyranyloxy group.

Abstract: New nonionic radiographic contrast agents having the formula ##STR1## wherein Y is a single bond, ##STR2## R.sub.1, R.sub.1 ' and R.sub.2 are the same or different and are hydrogen, alkyl or hydroxyalkyl.Hydroxyalkyl refers to such alkyl groups having 1 or more hydroxy groups. Preferred hydroxyalkyl groups include: ##STR3## R.sub.3 and R.sub.4 are the same or different and are hydrogen, methyl or --CH.sub.2 CH.sub.2 OH; R.sub.5 is hydrogen, alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH or OH and R.sub.6 is alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH, OH or hydrogen and may be the same or different than R.sub.5 and m is zero or one, with the proviso that no methylene or methine carbon atom of the heterocyclic ring is attached to both a nitrogen and an oxygen atom with the additional proviso that when Y is a single bond, m is not zero. These new contrast agents are water soluble and have desirable low osmolality and anticoagulant properties.

Abstract: Dicitrate cyclic diester (dicitrate) is a novel compound which is found in patients who do not exhibit symptoms or predisposition to idiopathic renal calculous disease. Dicitrate can be isolated and detected by novel chromatographic methods. Further, treating patients prophylactically and therapeutically with dicitrate cyclic diester can prevent or reduce the effects of calcification-related disease, including some types of kidney stones, or other disease or condition associated with the presence of metal ions. The metal ion complexing properties exhibited by dicitrate are also applicable to the use of the subject compounds as chelating agents and methods of binding, and thereby reducing, the amounts of metal ions in a substance.

Abstract: A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor.

Abstract: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R.sup.1 represents a hydrogen atom or a halogen atom or a group selected from C.sub.1-6 alkyl and C.sub.1-6 alkoxy;R.sup.2 represents a phenyl group substituted by a group selected from ##STR2## and optionally further substituted by one or two substituents selected from halogen atoms, C.sub.1-6 alkoxy, hydroxy, and C.sub.1-6 alkyl;R.sup.3 represents the group ##STR3## R.sup.4 and R.sup.5, which may be the same or different each independently represent a hydrogen atom or a halogen atom or a group selected from hydroxy, C.sub.1-6 alkoxy and C.sub.1-6 alkyl;R.sup.6 represents a hydrogen atom or a group selected from --NR.sup.9 R.sup.10 and a C.sub.1-6 alkyl group optionally substituted by one or two substituents selected from C.sub.1-6 alkoxy, hydroxy, C.sub.1-6 acyloxy and --SO.sub.2 R.sup.11 ;R.sup.7, R.sup.8 and R.sup.

Abstract: Compounds characterized generally as ethynyl alanine amino diol compounds having a piperazinyl-terminated or a piperazinyl-alkylamino-terminated group and derivatives thereof are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein G is a piperazinyl group or is a piperazinyl-containing group of Formula II: ##STR2## wherein B is a piperazinyl group or a alkylene-bridged-piperazinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR3## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.

Abstract: A method of preparing .alpha.-APM derivatives without using an expensive L-phenylalanine is provided, wherein 2,5-dioxopiperazine-3-acetamide is reacted with acetic anhydride to give N,N'-diacetyl-6-cyanomethyl-2,5-dioxopiperazine, which is then reacted with benzaldehyde in the presence of a strong base to give 1-acetyl-3-benzylidene-6-cyanomethyl-2,5-dioxopiperazine. This is treated with hydrazine to give 3-benzylidene-6-cyanomethyl-2,5-dioxopiperazine, which is then reduced to prepare 3-benzyl-6-cyanomethyl-2,5-dioxopiperazine, which is converted by reaction with methanol in the presence of a strong acid to an .alpha.-APM derivative for use as a sweetener.

Abstract: The use of glycine anhydride dimethylol, also known as 1,4-bis(hydroxymethyl)-2,5-piperazinedione, comprising the formula ##STR1## to kill microorganisms present in or on a host substance and to preserve products susceptible to contamination by a variety of microorganisms is disclosed.

Abstract: Compounds of the formulae ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1 and Y.sup.1 have the stated meanings, processes for their preparation and their use.

Abstract: Disclosed is a process for preparation of an amino acid, such as phenylalanine, with a high degree of optical purity. The process makes use of the same amino acid as a chiral template.

Abstract: Ergoline derivatives of the formula I: ##STR1## wherein R represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.1 represents hydrogen, chlorine, bromine or methyl; either R.sub.2 and R.sub.3 both represent hydrogen or together represent a chemical bond; R.sub.4 represents a C.sub.1 -C.sub.4 hydrocarbon group; each of R.sub.5, R.sub.6, R.sub.8 and R.sub.9 independently represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.7 represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or C.sub.3 -C.sub.7 cycloalkyl and n is 0, 1 or 2; are prepared by reaction between compounds of the formulae II and III: ##STR2## and subsequent cyclization of the resultant compounds. The compounds of the formula I are known useful anxiolytic, antipsychotic and anti-parkinson agents.

Abstract: A renin inhibiting compound of the formula ##STR1## wherein X is N, O or CH; R.sub.1 is absent or a functional group; A and L are independently selected from absent, C.dbd.O, SO.sub.2 and CH.sub.2 ; D is C.dbd.O, SO.sub.2 or CH.sub.2 ; Y is N or CH; R.sub.2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R.sub.3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.

Abstract: Disclosed is a process for synthesis of a dipeptide such as N-acetyl-L-.alpha.-aspartyl-L-phenylalanine methyl ester wherein one amino acid serves as a chiral template which allows for synthesis of a second amino acid residue to form said dipeptide. The process involves several novel steps such as a nucleophile addition step. In addition, several novel intermediates are described.

Abstract: The invention relates to novel intermediate compounds for preparation of novel amino acid derivatives having renin inhibiting activity.

Abstract: Compounds of the formula ##STR1## wherein Ar, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and n have the meanings mentioned in the description, processes and intermediates for their preparation, pharmaceutical compositions which contain them and their use in therapy in the treatment of cardiovascular diseases.

Abstract: A process for producing a chlorohenylhydrazine compound is disclosed, which comprises chlorinating at least one hydrogen atom on the phenyl nucleus in a beta-imidated phenylhydrazine compound and subsequently hydrolyzing the chlorinated compound. Said chlorophenylhydrazine compound is useful as starting material for the production of herbicide, insecticide and photographic coupler is produced in high yield and low cost.

Abstract: Compounds of formula (I):A--M--B-- (I)(in which: M represents a saturated heterocyclic group having from 5 to 7 ring atoms of which 2 are nitrogen atoms, said group being unsubstituted or being substituted at any of its carbon atoms by C.sub.1 -C.sub.6 alkyl and/or oxo substituents: A represents a halo-substituted benzhydryl substituent; and B represents certain specific substituted alkyl groups) and salts thereof are valuable for the treatment and prophylaxis of disorders arising from circulatory problems, especially those affecting the brain. They may be prepared by reacting a compound of formula A--M--H with a halo or acyloxy derivative corresponding to the alkyl substituent B which it is desired to introduce.

Abstract: Disclosed is a process for preparation of an amino acid, such as phenylalanine, with a high degree of optical purity. The process makes use of the same amino acid as a chiral template.

Abstract: A new compound called N,N'-carbonyl-bis-(4-ethyl-2,3-dioxo)-piperazine of Formula I ##STR1## A process for the preparation thereof based on the reaction of 4-ethyl-2,3-dioxo-piperazine or a trimethylsilyl derivative thereof with carbonyl chloride or a derivative thereof.The use of the compound of Formula I as an intermediate in the preparation of compounds of Formula II ##STR2## where R is a radical, substituted in alpha position, of a molecule of an acid selected from the group formed by phenylacetic acid, p-hydroxy phenylacetic acid, a 6-(phenylacetamido)-penicillanic acid and a 7-(phenylacetamido)-cephalosporanic acid.

Abstract: A sulfonamide compound represented by the following formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are identical or different, and each represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; R.sup.4 represents a hydrogen atom, a lower alkyl group, or a substituted or unsubstituted aralykyl group; R.sup.5 represents a substituted or unsubstituted aryl group or a substituted or unsubstituted aralkyl group; R.sup.6 and R.sup.7 are identical or different and each represents a hydrogen atom, a lower alkyl group or a lower alkoxy group; and n is an integer of 1 to 8,and an acid addition salt thereof. The compounds of formula (I) provided by this invention have some useful biological activities such as the spasmolytic activity on the vascular smooth muscles and anti-platelet aggregatory activity and are useful as drugs for treating cardiovascular disorders such as angina pectoris, cerebral circulation disorder and thrombosis.

Abstract: Diseases caused by platelet activating factor are prevented and treated by administration to a subject of a therapeutically effective amount of a piperazine compound of the formula: ##STR1## wherein R.sup.1 to R.sup.4 are as defined in the specification.

Abstract: The invention relates to a PAF-antagonist pharmaceutical composition comprising a compound of the formula: ##STR1## wherein R.sup.1 is pyridyl(lower)alkyl or thiazolyl(lower)alkyl,R.sup.2 is N-lower alkylindolyl(lower)alkyl which may have lower alkyl or halogen on the indole ring, andR.sup.3 and R.sup.4 are each hydrogen or lower alkyl; or pharmaceutically acceptable salt thereof.

Abstract: Compounds of the formula:Ar.sub.1 -X-Ar-Z-(R).sub.n'and salts thereof, whereinAr.sub.1 is a nitrogen, sulfur or oxygen heterocyclic ring;Ar is a phenyl ring or a nitrogen, oxygen or sulfur heterocyclic ring;Ar and Ar.sub.1 may be fully substituted or less than fully substituted with H, CH.sub.3, lower alkyl, aryl, aralkyl, halo, hydroxy, lower alkoxy, CF.sub.

Abstract: The compound (S)(+)-4,4'-(1-methyl-1,2-ethanediyl)-bis(2,6-piperazinedione) is prepared by treating propylenediamine tetraacetic tetraamide in a dipolar aprotic solvent with an alkali metal derivative of dimethyl sulfoxide to form a dialkali metal salt of (S)(+)-4,4'-(1-methyl-1,2-ethanediyl)-bis(2,6-piperazinedione); and neutralizing the dialkali metal salt.

Abstract: The invention is a process for the preparation of halohydroxyalkyl carbamates which comprises contacting an epihalohydrin carbonate with a secondary amine-containing compound, wherein the secondary amine has a pKa at which the secondary amine will react with the epihalohydrin carbonate and which does not catalyze the formation of unwanted by-products in the further presence of an acid scavenger capable of forming a salt with the hydrogen halide by-product formed, in an amount sufficient to prevent the formation of unwanted by-products, in a polar organic solvent under conditions such that a halohydroxyalkyl carbamate, wherein the carbamate nitrogen is tertiary, is prepared.

Abstract: Disclosed are novel bis-dioxopiperazine derivatives, process for their preparation, antitumor agents comprising them and compositions containing them.The bis-dioxopiperazine derivatives are represented by the following general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms; R.sub.2 represents a hydrogen atom or a group of ##STR2## R.sub.3 and R.sub.4, which are respectively independent and are the same or different, represent respectively a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms or a heterocyclic radical selected from the group consisting of substituted or unsubstituted piperidino, substituted or unsubstituted piperazino, substituted or unsubstituted morpholino and substituted or unsubstituted thiomorpholino, or R.sub.3 and R.sub.

Abstract: The compound of the formula ##STR1## and non-toxic, pharmacologically acceptable acid addition salts thereof. The compound as well as its salts are useful as analgesics.

Abstract: The novel compound 1,4-diisopropyl-2,5-diketopiperazine can be hydrolytically cleaved to prepare N-isopropylglycine, which can be reacted with formaldehyde and prosphorous acid to produce N-isopropyl-N-phosphonomethylglycine. The latter compound can be dealkylated in the presence of base to produce N-phosphonomethylglycine, a well known herbicide.

Abstract: Substituted and unsubstituted 2,5-diketopiperazines can be prepared by a process which comprises bringing together a substituted or unsubstituted glycinamide and a haloacetyl halide, optionally in the presence of a non-nucleophilic base, and thereafter adding a stronger base.

Abstract: A method for converting .beta.-aspartylphenylalanine derivative (1) to .alpha.-aspartylphenylalanine derivatives (2) and (3), said derivatives having the following structures: ##STR1## which comprises: reacting said .beta.-aspartylphenylalanine derivative (1) at a temperature of from 0.degree. to 200.degree. C. for a time period of from 30 minutes to 80 hours, in a C.sub.1 to C.sub.4 alcohol solvent with or without stirring, wherein R and R' represent hydrogen or an alkyl group having from 1 to 4 carbon atoms.

Abstract: The invention includes novel dicarboxylic acids derived from alkylene or arylene diaminetetraacetec acid corresponding to the formula ##STR1## These dicarboxylic acids derived from alkylene or arylene diaminetetraacetic acid are useful in the preparation of polyamides.Another aspect of the invention is a polymer prepared from between about 1 and 100 mole percent of the diamine salt of the compound represented by formula (I) ##STR2## These polymers are useful in preparing molded articles.

Abstract: A compound of the formula: ##STR1## wherein u represents hydrogen, carboxamido, N-hydroxycarboxamido, carboxy, azido, an aryl, an acylamino, a protected carboxy or an N-alkoxycarboxamido, or, together with v, can represent --S-- or --CH.sub.2 S--; v represents hydrogen, halogen, cyano or an alkylthio, or, together with u, can represent --S-- or --CH.sub.2 S--, or, together with w, can represent --(CH.sub.2).sub.3 CO--; w represents hydrogen, carboamoyl, cyano, carboxy, an N-alkylcarbamoyl, an alkyl, an aryl, a protected carboxy or a heterocycle, or, together with v, can represents --(CH.sub.2).sub.

Abstract: 2-Acyl-1,3,4,6,7,11b-hexahydro-2H-pyrazino-[2,1-a]-4-isoquinoleinones having anthelmintic activity of the formula ##STR1## are prepared from 4-acyl-2,6-dioxopierazines by reaction with a phenethyl halide, selective reduction of one of the oxo groups and cyclization, by the novel intermediates of formula ##STR2## in which Y represents O or H, OH.