Abstract: The present invention relates to a process for preparing trientine dihydrochloride as an active pharmaceutical ingredient (API). The present invention relates to a process for the preparation of trientine dihydrochloride with a pharmaceutical grade of purity. The invention also relates to novel intermediates used in the preparation of trientine dihydrochloride.

Abstract: Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively wherein, R1 and R2 are individually selected from hydrogen, alkyl, substituted or alkyl; n=0, 1, or 2; Y=NR3R4, OR5, or SR5, where R3 and R4 are individually selected from acyl or sulfonyl, and where R5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.

Abstract: Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively wherein, R1 and R2 are individually selected from hydrogen, alkyl, substituted or alkyl; n=0, 1, or 2; Y=NR3R4, OR5, or SR5, where R3 and R4 are individually selected from acyl or sulfonyl, and where R5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.

Abstract: Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively wherein, R1 and R2 are individually selected from hydrogen, alkyl, substituted or alkyl; n=0, 1, or 2; Y=NR3R4, OR5, or SR5, where R3 and R4 are individually selected from acyl or sulfonyl, and where R5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.

Abstract: Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively wherein, R1 and R2 are individually selected from hydrogen, alkyl, substituted or alkyl; n=0, 1, or 2; Y=NR3R4, OR5, or SR5, where R3 and R4 are individually selected from acyl or sulfonyl, and where R5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.

Abstract: Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively wherein, R1 and R2 are individually selected from hydrogen, alkyl, substituted or alkyl; n=0, 1, or 2; Y=NR3R4, OR5, or SR5, where R3 and R4 are individually selected from acyl or sulfonyl, and where R5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.

Abstract: Compounds that inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. The compounds of the invention are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the compound can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

Abstract: ?-Amino-?-Cyanoacrylates of formula I where the variables have the following meanings: R1 is n-alkyl, n-alkenyl or alkoxyalkyl; R2,R3 are alkyl, which may be partially or fully halogenated and/or may carry a substituent from the group consisting of cyano, alkoxy, haloalkoxy, alkylthio, haloalkylthio, C1-C6-alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl and haloalkylsulfonyl, are alkenyl or alkynyl; or R2 and R3 together with the carbon atom to which they are attached form a cycloalkyl ring in which one or two nonadjacent CH2 groups may be replaced by oxygen or sulfur, and where the cycloalkyl ring may be substituted by halogen or alkyl; R4 is hydrogen, halogen, cyano or alkyl, where the substituents R2, R3 and R4 or two of the radicals R2, R3 and R4 are not simultaneously methyl, and their agriculturally useful salts, processes and intermediates for their preparation; and the use of these compounds or of compositions comprising these compounds for controlling undesirable plants are described.

Abstract: Telemetry signals and biometric telemetry signals are wirelessly transmitted from an athlete, driver, or other person over an audio/video link. The measurement stream from a sensor can be modulated and then fed into a transmitter's audio input or video input. The transmitter transmits a signal containing the measurement stream as well as audio and video streams. A demodulator recovers the measurement stream output by a receiver receiving the signal. The recovered measurement signal can then be passed to an interested party. For example, a heart rate measurement can be obtained from a driver or other athlete and displayed to a television audience.

Abstract: Compounds that inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. The compounds of the invention are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the compound can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

Abstract: The invention relates to a method of treating a patient in need thereof, including a need for diagnosis or treatment, comprising the administration of a metal complex of a polypeptide construct. The construct comprises a compound of the formula (I): ##STR1## in which, "B" is a hydrocarbon backbone,"P" is a polypeptide capable of targeting particular-cells, tissues or organs of the body,"A" may be the group --NR'--NR"-- or the group --NR'--NR"--L-- in which L may be an aliphatic or aromatic linker group,R, R', and R" may be the same or different and may be hydrogen or an aliphatic group,m is an integer .gtoreq.2, provided that the groups R, R', R", L and "P" of a given chain may be the same or different from the groups R, R', R", L and "P" of another chain,n is an integer .gtoreq.0;or a pharmaceutically acceptable salt thereof. The constructs of the present invention are capable of binding a variety of metallic species.

Abstract: This invention relates to the preparation and use of novel open-chain or cyclic polypeptide constructs in which two or more polypeptide chains, in an open-chain construct, or one or more chains, in a cyclic construct, are chemically derivatized such that the resulting construct exhibits both metal-binding capability and tissue-, organ- or cell-targeting selectivity. In particular, the polypeptide constructs of the present invention comprise compounds of the formula (I): ##STR1## in which, "B" is a hydrocarbon backbone, "P" is a polypeptide capable of targeting particular cells, tissues or organs of the body, "A" may be the group --NR'--NR"-- or the group --NR'--NR"--L-- in which L may be an aliphatic or aromatic linker group, R, R', and R" may be the same or different and may be hydrogen or an aliphatic group, m is an integer.gtoreq.2, provided that the groups R, R', R", L and "P" of a given chain may be the same or different from the groups R, R', R", L and "P" of another chain, n is an integer.gtoreq.

Abstract: This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, substantial thioureas for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.

Abstract: This invention relates to the preparation and use of novel open-chain or cyclic polypeptide constructs in which two or more polypeptide chains, in an open-chain construct, or one or more chains, in a cyclic construct, are chemically derivatized such that the resulting construct exhibits both metal-binding capability and tissue-, organ- or cell-targeting selectivity. In particular, the polypeptide constructs of the present invention comprise compounds of the formula (I): ##STR1## in which, "B" is a hydrocarbon backbone, "P" is a polypeptide capable of targeting particular cells, tissues or organs of the body, "A" may be the group --NR'--NR"-- or the group --NR'-- NR"--L-- in which L may be an aliphatic or aromatic linker group, R, R', and R" may be the same or different and may be hydrogen or an aliphatic group, m is an integer.gtoreq.2, provided that the groups R, R', R", L and "P" of a given chain may be the same or different from the groups R, R', R", L and "P" of another chain, n is an integer.gtoreq.

Abstract: This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, isothiocyanate derived thiocarbonyls for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.

Abstract: A process for the purification of aminophosphonic acids under non-alkaline conditions is described. In particular, aminophosphonic acids are slurred in neutral or acidic water, heated to reflux, cooled and then filtered. Product purities approaching 100% are thus obtained.

Abstract: This invention relates to the preparation and use of novel open-chain or cyclic polypeptide constructs in which two or more polypeptide chains, in an open-chain construct, or one or more chains, in a cyclic construct, are chemically derivatized such that the resulting construct exhibits both metal-binding capability and tissue-, organ- or cell-targeting selectivity. In particular, the polypeptide constructs of the present invention comprise compounds of the formula (I): ##STR1## in which, "B" is a hydrocarbon backbone, "P" is a polypeptide capable of targeting particular cells, tissues or organs of the body, "A" may be the group --NR'--NR"-- or the group --NR'--NR"--L-- in which L may be an aliphatic or aromatic linker group, R, R' and R" may be the same or different and may be hydrogen or an aliphatic group, m is an integer .gtoreq.2, provided that the groups R, R', R', L and "P" of a given chain may be the same or different from the groups R, R', R", L and "P" of another chain, n is an integer .gtoreq.

Abstract: This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, isothiocyanate derived thiocarbonyls for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.

Abstract: Novel antineoplastic amine-containing derivatives and methods for synthesizing such derivatives of anthracycline antibiotics are disclosed. The derivatives are useful to anthracycline antibiotic conjugates which retain substantial immunospecificity of the unconjugated antibody molecule. Using the conjugates, targeted delivery of the attached antibiotics is achieved in vivo. Such conjugates are thus therapeutically effective against a variety of neoplastic cellular disorders when administered in vivo. Methods for preparing the antibody conjugates and for use of the conjugates in vivo are also disclosed.

Abstract: Disclosed herein is a novel method for preparing a DPTA tripeptide-chelator. In particular, a method for preparing GYK-DTPA is described. The method disclosed herein is an improvement over the known methods of preparation based on the cost and labor savings of the present invention. The present invention utilizes t-butyloxycarbonyl (Boc) protecting groups to facilitate the polypeptide-chelator production.