Abstract: Polyamine compounds, method of synthesis and method of use for anti-cancer purposes, and for enhancing the activity of existing anti-cancer drugs are provided. This disclosure has identified certain polyamine motifs that can be attached to toxic agents to facilitate their access to cancer cells as well as polyamine compounds of surprising cytotoxicity and selectivity in killing cancer cells. It includes an illustrative conjugate system with examples of a triamine or a tetraamine appended to a cytotoxic agent. There are five method schemes illustrative of the synthesis of the compounds of the invention. Included is a general strategy to enhance cell uptake by attaching a polyamine vectoring system with an example of a triamine vector attached to an existing anti-cancer drug to improve its chemotherapeutic potency. There is an illustration of using the triamine vector to improve the selectivity of an anthracenylmethyl amine cytotoxic agent (e.g.

Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.

Abstract: Cytotoxic polyamine analogues are provided that are useful for treating diseases where it is desired to inhibit cell growth and/or proliferation, for example cancer and post-angioplasty injury.

Abstract: Chiral hydroxyethylamine, hydroxyethylurea or hydroxyethylsulfonamide isostere containing retroviral protease and renin inhibitors can be prepared by multi-step syntheses that utilize key chiral amine intermediates. This invention is a cost effective method of obtaining such key chiral amine intermediates enantiomerically, diastereomerically and chemically pure. The method is suitable for large scale (multikilogram) productions. This invention also encompasses organic acid and inorganic acid salts of the amine intermediates.

Abstract: Novel polyamines, their synthesis and use in pharmacological, cosmetic or agricultural applications are provided. The polyamines induce antizyme production which in turn down regulates both the production of polyamines by omithine decarboxylase (ODC) and the transport of polyamines by its corresponding polyamine transporter. These compounds will preferably enter the cell independent of the polyamine transporter. As drugs, these compounds are used to treat any disease associated with cellular proliferation including but not limited to cancer.

Abstract: The invention provides triamine derivative melanocortin receptor ligands of the formula: wherein R1 to R8 and n have the meanings provided herein. The invention further provides methods of using the ligands to alter or regulate the activity of a melanocortin receptor.

Abstract: Methods and compositions for treating disease caused by microorganisms, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders 1

Abstract: Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.

Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: The present invention provides a convergent method for the synthesis of ubiquinones and ubiquinone analogues. Also provided are precursors of ubiquinones and their analogues that are useful in the methods of the invention.

Abstract: (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine (sertraline) may be prepared by hydrogenating of N-[4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenylidene]methanamine in the presence of a dehalogenation inhibitor, e.g., triphenylphosphite or trimethylphosphite and a catalyst.

Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Abstract: An improved detergent for use in hydrocarbon fuels comprising the composition produced by mixing (1) the Mannich reaction product of a polyisobutene-substituted phenol, (preferably, where the polyisobutene from which the substituted phenol is derived contains at least 70% terminal olefinic double bonds of the vinylidene type); an aldehyde; and an amine, preferably, ethylene diamine; and (2) a compound selected from the group consisting of an alkylbenzene sulfonic acid, an alkylnapthalene sulfonic acid, acetylaetone and mixtures thereof. Preferably, the alkylbenzene and alkylnapthalene sulfonic acid is selected to be a (C6 to C18) alkylbenzene sulfonic acid/napthalene sulfonic acid, especially preferred being dodecylbenzene sulfonic acid.

Abstract: Estrogen receptor modulators, compositions comprising the compounds and methods relating to the use thereof are described. The compounds may be used in inhibiting the proliferation of and/or induces apoptosis in human breast cancer cells.

Abstract: Polyamines having the formula: wherein R1 and R2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; and a and b may be the same or different and are integers from 1 to 8; or a salt thereof with a pharmaceutically acceptable acid. Anti-neoplastic, anti-diarrheal, anti-peristaltic, gastro-intestinal anti-spasmodic, anti-viral, anti-retroviral, anti-psoriasis and insecticidal compositions comprising biologically effective amounts of the above-described amines and biologically acceptable carriers therefor are also disclosed, as well as methods of treatment, administration or application of biologically effective amounts of the polyamines of the invention. Also disclosed are methods for preparing the polyamines of the invention.

Abstract: Anti-diarrheal, anti-secretory, nitric oxide agonist, nitric oxide synthase activating or gastrointestinal anti-spasmodic compounds of the formula:  R1—N1H—(CH2)3—N2H—(C2)3—N3H—(CH2)4—N4H—(CH2)3—N5H—(CH2)3—N6H—R6  (II); or wherein: R1 and R6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms; R2-R5 may be the same or different and are H, R1 or R6; R7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms; m is an integer from 3 to 6, inclusive; and n is an integer from 3 to 6, inclusive; or (IV) a salt thereof with a pharmaceutically acceptable acid; and a pharmaceutically acceptable carrier therefor. Methods of treatment utilizing the composition are also disclosed.

Abstract: The invention provides N-aminopropylated toluenediamines, processes for synthesizing them, compositions containing them and methods for using them to cure epoxy resins. In preferred embodiments, the N-aminopropylated toluenediamines are represented by the following formula: where the nitrogen atoms are ortho or meta to each other on the aromatic ring.

Abstract: The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as dermal and topical anesthetics in mammals, including man, as well as compositions containing said compounds.

Abstract: Novel compounds having the formula: wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.

Abstract: Chiral hydroxyethylamine, hydroxyethylurea or hydroxyethylsulfonamide isostere containing retroviral protease and renin inhibitors can be prepared by multi-step syntheses that utilize key chiral amine intermediates. This invention is a cost effective method of obtaining such key chiral amine intermediates enantiomerically, diastereomerically and chemically pure. The method is suitable for large scale (multikilogram) productions. This invention also encompasses organic acid and inorganic acid salts of the amine intermediates.

Abstract: Reaction products of i) a compound containing at least one primary or secondary amine group and at least one hydroxyl group; ii) a polyamine containing at least two amine groups wherein at least one of the amine groups is a primary or secondary amine, and wherein component ii) is different from i); iii) an alkyl-substituted hydroxyaromatic compound, and iv) an aldehyde, provide improved detergency as well as improved lubricity to hydrocarbon fuels. Compositions comprising a hydrocarbon fuel and the reaction products are also disclosed.

Abstract: A compound having the formula: ##STR1## wherein: R.sub.1 -R.sub.6 may be the same or different and are H, alkyl or aralkyl having from1 to 12 carbon atoms;m is an integer from 3 to 6, inclusive;n is an integer from 3 to 6, inclusive;excluding those compounds of formula (I) wherein all of R.sub.1 -R.sub.6 are H and further excluding those compounds of formula (I) wherein:1) m is 3, n is 4, R.sub.1, R.sub.2, R.sub.5 and R.sub.6 are all H, and R.sub.3 and R.sub.4 are methyl;2) m is 3, n is 4, R.sub.1 and R.sub.6 are methyl or ethyl, and R.sub.2 -R.sub.5 are all H;3) m is 3, n is 4, and R.sub.1 -R.sub.6 are all methyl, ethyl or propyl;4) m and n are 3, R.sub.1, R.sub.2, R.sub.5 and R.sub.6 are all H, and R.sub.3 and R.sub.4 are methyl;5) m and n are 3 and R.sub.1 -R.sub.6 are all methyl;6) m and n are 3, R.sub.1 and R.sub.6 are H, and R.sub.2 -R.sub.5 are all methyl;7) m and n are 3, R.sub.1 and R.sub.6 are methyl, and R.sub.2 -R.sub.5 are all H;8) m and n are 3, R.sub.1 and are R.sub.6 are hydrogen, R.sub.

Abstract: A diaminoalkane of general formula (I) in which R.sub.1 to R.sub.10 stand independently of each other for hydrogen, a (C.sub.1 -C.sub.4)-alkyl group, a hydroxy-(C.sub.2 -C.sub.3)-alkyl group, a (C.sub.1 -C.sub.4)-alkoxy-(C.sub.2 -C.sub.3) alkyl group, an amino- (C.sub.2 -C.sub.3) alkyl group or a 2,3-dihydroxypropyl group and n is a number from 1 to 6 with the proviso that the --NR.sub.1 R.sub.2 and --NR.sub.7 R.sub.8 groups are either in positions 4 and 4' or in positions 5 and 5'. Salts of the diaminoalkane which are physiologically compatible with inorganic and organic acids. Method of coloring keratin fiber.

Abstract: A purified acid addition salt of a (2S, 3S, 5S)-2,5-diamino-1,6-diphenyl-3-hydroxyhexane, e.g., (2S, 3S, 5S)-2-tert-butoxycarbonylamino-3-hydroxy-5-amino-1,6-diphenylhexane, is obtained from its mixture, in an arbitrary ratio, with its (2S, 3S, 5R) stereoisomer in the presence of an inorganic or organic acid. The desired (2S, 3S, 5S) acid addition salt may be recovered from the mixture by, for example, recrystallization. These purified acid addition salts are useful as intermediates in the synthesis of medicines such as retrovirus protease inhibitors including human immunodeficiency virus (HIV) protease inhibitors.

Abstract: The invention provides methods for preparing a 2-isoxazoline compound represented by formula (1) and a 2,5-diamino-1,6-diphenyl-3-hydroxyhexane compound obtainable by reducing the 2-isoxazoline compound and represented by formula (6): ##STR1## wherein Ph is phenyl; and each of R.sup.1 and R.sup.2 independently represents hydrogen, acyl, alkyloxycarbonyl, arylalkyloxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylalkylaminocarbonyl, arylaminocarbonyl, alkyl, arylalkyl, aryl, alkylsulfonyl, acylalkylsulfonyl, or arylsulfonyl, or R.sup.1 and R.sup.2 are linked to each other to form divalent acyl. These compounds are useful as intermediates in the synthesis of medicines such as retrovirus protease inhibitors including human immunodeficiency virus (HIV) protease inhibitors.

Abstract: Reaction products of polyolefins having predominantly a terminal double bond and a number average molecular weight of from 250 to 10,000, which possess an aliphatic hydrocarbon skeleton which is straight-chain or carries C.sub.1 -C.sub.4 -alkyl side chains, with from 1 to 10 mol, per equivalent of double bond, of one or more vinyl esters I ##STR1## are obtainable by reacting the stated polyolefins with the vinyl esters I in the presence of a free radical initiator at from 80 to 200.degree. C., it being possible for these reaction products subsequently to have been hydrolyzed to the corresponding alcohols or converted into the corresponding amines by reductive amination with amines II ##STR2## .

Abstract: A process for preparing a compound of formula (I) or an addition salt thereof and/or a solvate thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are each independently C.sub.1-4 alkoxy and R.sup.3 is C.sub.1-6 alkyl, which process comprises reacting an arylamine of formula (II): ##STR2## wherein R.sup.4 and R.sup.5 are as defined in relation to formula (I) with a .beta.-aminoaldehyde of formula (III): ##STR3## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in relation to formula (I); and thereafter reducing the intermediate so formed and, optionally, forming an addition salt of the compound of formula (I) and/or a solvate thereof.

Abstract: The present invention provides a compound of formula: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a and R.sup.6b are defined herein or a pharmaceutically acceptable salt thereof, a process for its preparation, intermediates and its use as a tachykinin antagonist.

Abstract: Novel nitrobenzene compounds of the nitroparaphenylene-diamine type substituted by sulphur in the 5-position are disclosed. These compounds are intended especially for the dyeing of keratin fibers and in particular human hair. A process for their preparation, dyeing compositions in which these compounds are present and a dyeing process in which these compositions are used are also disclosed.

Abstract: A compound according to the formula: ##STR1## and conjugates thereof.

Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.

Abstract: Isoprene derivatives of formula (I) ##STR1## wherein m is an integer of 0 to 3,n is an integer of 5 to 12,A is cyclo(C.sub.3 -C.sub.6)alkylene, phenylene, fluorenylene, pyrrolidinylene, piperazinylene, 9-aza-3-oxabicyclo?3.3.1!-nonylene,R.sub.1 and R.sub.2 are each independently benzyl, of which a phenyl ring may be substituted by 1 to 5 substituents selected from the group consisting of hydroxy, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and halogen,X is a single bond or a divalent radical of --(CH.sub.2).sub.p NH--,p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof. Those compounds are useful as multidrug resistance inhibitors for overcoming multidrug resistance of cancer and agents for enhancing an activity of anti-cancer agents.

Abstract: The invention relates to cyclohexenyl antibacterial compounds of the formula I: ##STR1## and pharmaceutical compositions containing the compounds, methods for their production and use.

Abstract: This invention relates to certain polyamine derivatives, to the methods and intermediates useful for their preparation, and to their use in treating diseases caused by infestation with a variety of parasitic protozoa.

Abstract: The invention relates to compounds of the formula ##STR1## in which: m is 2 or 3;Ar and Ar' independently are a thienyl group; a substituted or unsubstituted phenyl group; or an imidazolyl group; it also being possible for Ar' to be a benzothienyl group which is unsubstituted or substituted by a halogen; a naphthyl group which is unsubstituted or substituted by a halogen; a biphenyl group; or a substituted or unsubstituted indolyl;X is hydrogen;X' is hydrogen or a hydroxyl group or is joined to X" below to form a carbon-carbon bond, or X and X' together form an oxo group or a dialkylaminoalkoxyimino group of the formula .dbd.N--O--(CH.sub.2).sub.p --Am, in which p is 2 or 3 and Am is a dialkylamino group;Y is a nitrogen atom or a group C(X"), in which X" is hydrogen or forms a carbon-carbon bond with X';Q is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aminoalkyl group of the formula --(CH.sub.2).sub.

Abstract: Polyamines having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are alkyl, aralkyl or aryl having up to 10 carbon atoms; anda and b may be the same or different and are integers from 1 to 8; or a salt thereof with a pharmaceutically acceptable acid. Anti-neoplastic, anti-diarrheal, anti-peristaltic, gastrointestinal anti-spasmodic, anti-viral, anti-retroviral, anti-psoriasis and insecticidal compositions comprising biologically effective amounts of the above-described amines and biologically acceptable carriers therefor are also disclosed, as well as methods of treatment, administration or application of biologically effective amounts of the polyamines of the invention. Also disclosed are methods for preparing the polyamines of the invention.

Abstract: Compounds of formula ##STR1## wherein R, R', R", R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X, Y, m, n and p have the meanings reported in the description;and their pharmaceutically acceptable salts are described.The compounds of formula I are useful in the treatment of arterial hypertension and congestive heart failure, of renal failure, of peripheral arteriopathies, of cerebrovascular insufficiencies and of ischemic cardiopathy.

Abstract: A process for preparing substituted aromatic azo compounds is provided which comprises contacting a nucleophilic compound and an azo containing compound in the presence of a suitable solvent system, and reacting the nucleophilic compound and the azo containing compound in the presence of a suitable base and a controlled amount of protic material at a temperature of about 10.degree. C. to about 150.degree. C. in a confined reaction zone wherein the molar ratio of protic material to base is 0:1 to about 5:1. In another embodiment, the substituted aromatic azo compounds are further reacted with a nucleophilic compound in the presence of a suitable solvent system, a suitable base and a controlled amount of protic material at a temperature of about 70.degree. C. to about 200.degree. C. in a confined reaction zone wherein the molar ratio of protic material to base is 0:1 to about 5:1 to produce a substituted aromatic amine.

Abstract: A process for preparing substituted aromatic amines which comprises contacting a nucleophilic compound and a substituted aromatic azo compound in the presence of a suitable solvent system, and reacting the nucleophilic compound and the substituted aromatic azo compound in the presence of a suitable base and a controlled amount of protic material at a temperature of about 70.degree. C. to about 200.degree. C. in a confined reaction zone wherein the molar ratio of protic material to base is 0:1 to about 5:1. In another embodiment, the substituted aromatic amines of the invention are reductively alkylated to produce alkylated diamines or substituted derivatives thereof.

Abstract: Curing components containing amino groups for curing epoxy resins are obtained by the reaction of alkylated polyhydroxy aromatics (A) with polyamines (B) and aldehydes (C) by the mechanism of the Mannich reaction. The preparation of curable mixtures and varnish formulations is also disclosed. The curing components and curable mixtures can also be employed at a low temperature.

Abstract: Curing components containing amino groups for curing epoxy resins are obtained by the reaction of alkylated polyhydroxy aromatics (A) with polyamines (B) and aldehydes (C) by the mechanism of the Mannich reaction. The preparation of curable mixtures and varnish formulations is also disclosed. The curing components and curable mixtures can also be employed at a low temperature.

Abstract: A process of reforming an alkyleneamine feedstock or a mixture of such feedstocks to an alkyleneamine or a mixture of alkyleneamines which is different from the feedstock or feedstock mixture. The process is catalyzed by one of the following: Group VB metal oxides, Group VB metal phosphates, Group IIA metal silicates, and tungsten oxides. For example, ethylenediamine is contacted with a catalyst of niobic acid or magnesium silicate to yield predominantly diethylenetriamine and non-cyclic triethylenetetramines; whereas high molecular weight polyethylenepolyamines are cracked by the same catalysts to mixtures of lower molecular weight linear and cyclic materials.

Abstract: The invention relates to a disinfectant concentrate which contains amine and alcohol wherein the alcohol component includes at least one glycol ether of limited miscibility with water and the amine component includes at least one secondary and/or tertiary alkyl amine free from hydroxyl groups. It also relates to a disinfectant producabile from the disinfectant concentrate, the use of the disinfectant concentrate and of the disinfectant as bactericide, in particular mycobactericide, fungicide or virucide.

Abstract: The present invention relates to novel acyclic ethylenediamine derivatives of nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined as in the specification. It also relates to novel intermediates used in the synthesis of such derivatives.Compounds of the formula I and their pharmaceutically acceptable salts are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: A tertiary amino alcohol, being useful as an emulsifier, is defined by the formula (1) or (2): ##STR1## where R is a C.sub.2 to C.sub.24 straight-chain or branched alkylene group, an alicyclic alkylene group, an aralkylene group or --CH.sub.2 CH.sub.2 O).sub.p (CH.sub.2 CH.sub.2).sub.q (where p is 0 or a positive integer and q is a positive integer), R' is a C.sub.1 to C.sub.24 straight-chain or branched alkyl group or an aralkyl group and n is a positive integer of 2 to 50.

Abstract: Anti-diarrheal, anti-secretory, nitric oxide agonist, nitric oxide synthase activating or gastrointestinal anti-spasmodic compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.6 may be the same or different and are H, alkyl or aralkyl having from 1 to 12 carbon atoms;R.sub.2 -R.sub.5 may be the same or different and are H, R.sub.1 or R.sub.6 ;R.sub.7 is H, alkyl, aryl or aralkyl having from 1 to 12 carbon atoms;m is an integer from 3 to 6, inclusive; andn is an integer from 3 to 6, inclusive; or(IV) a salt thereof with a pharmaceutically acceptable acid; and a pharmaceutically acceptable carrier therefor. Methods of treatment utilizing the composition are also disclosed.

Abstract: Ashless dispersants are formed using polymers of propylene characterized in that they are liquid substantially linear polymers, they have stereo-irregularity in the polymer chain, at least 60 mol percent of the polymer has a terminal vinylidene group and, optionally, the polymer contains up to 25 mol percent of ethylene or a C.sub.4 to C.sub.10 monoolefin polymerized into the polymer chains.

Abstract: The present invention relates to anti-neoplastic and anti-psoriasis pharmaceutical compositions and methods of treatment and to insecticidal compositions and methods of controlling the growth of insects.