Abstract: (4-Piperidinylmethyl and -hetero)purines having antihistaminic properties and being useful agents in the treatment of allergic diseases.

Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.

Abstract: Histamine H.sub.1 antagonists of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl of 1 to 6 carbon atoms; ##STR2## and the other is hydrogen or alkyl of 1 to 6 carbon atoms, where ##STR3## in which X is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano or a nitro substituent on one of the available carbon atoms; andn is one of the integers 2, 3 or 4;or a pharmaceutically acceptable salt thereof.

Abstract: Histamine H.sub.1 -receptor antagonists of the formula: ##STR1## where R.sup.1 is hydrogen or alkyl; one of R.sub.2 and R.sup.3 is alkyl and the other is ##STR2## where R.sup.4 is pyridin-2-yl, pyridin-4-yl, thienyl, or phenyl, any of which is optionally substituted by a halo, alkyl of 1 to 6 carbon atoms, nitro, trifluoromethyl, hydroxy or alkoxy of 1 to 6 carbon atoms substituent; and R.sup.5 is pyridin-2-yl, pyridin-4-yl or phenyl, any of which is optionally substituted by a halo, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, nitro or trifluoromethyl substituent.

Abstract: N-Theophyllin-7-ylalkylene-N.sup.1 -(bis-p-fluorophenyl)methyl-piperazine derivatives as histamine H.sub.1 -antagonists.

Abstract: Certain functionalized cogeners of 1,3-dialkylxanthine exhibit high potency and selectivity as antagonists for A.sub.1 - and A.sub.2 -adenosine receptors and are suitable for attachment to probes, drug carriers, or solid supports. These derivatives are characterized by the presence of a phenyl at the 8 position para-substituted with a functionalized chain to provide high water solubility and high receptor affinity. Some of these analogs, containing a distal amino- or carboxylic-functionalized chain, are suitable for synthesis of amino acid conjugates. The compounds of this invention are suitable for use as antiallergenic, antiasthmatic, or cardiotonic drugs, central nervous system stimulants, and diuretics.

Abstract: New derivatives of theophylline having the formula ##STR1## wherein R is hydrogen or a hydroxy group, and n is an integer of 0.ltoreq.n.ltoreq.3 and/or the pharmaceutically acceptable, acid addition salts thereof, exhibit in addition to other properties, histamine-serotinine- bradykynine- antagonistic, anti-anaphylactic and .beta.-adrenergic stimulating effects.

Abstract: Polymeric, single-stranded DNA molecule which is labeled with a plurality of labels, the labels being bonded, via linking groups, to adenine and cytosine bases of the DNA molecule in substantially equal numbers, the labels being bonded to essentially none of the guanine or thymine bases of the DNA molecule, the DNA molecule being adapted for use as a probe in a nucleic acid hybridization assay.

Abstract: 1.4;3.6-Dianhydrohexitol nitrates substituted by purine bases, namely, adenyl-desoxy-1.4;3.6-dianhydrohexitol nitrates of the general formula Ia as well as theophyllinyl-desoxy-1.4;3.6-dianhydrohexitol nitrates of the general formula Ib, ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and, independently of one another signify(a) a hydrogen atom,(b) a straight-chained or branched alkyl group with 1 to 7 C-atoms,(c) an .omega.-phenylalkyl group, whereby the alkyl group has 1 to 7 C-atoms and whereby the phenyl ring can be halogen-substituted in the p-position, or wherein(d) R.sup.1 signifies one of the residues given under (a) to (c) and R.sup.2 an acyl radical or an aliphatic, possibly methyl-substituted monocarboxylic acid with 2 to 7 C-atoms, or wherein(e) R.sup.1 and R.sup.

Abstract: Certain functionalized congeners of 1,3-dialkylxanthine exhibit high potency and selectivity as antagonists for A.sub.1 - and A.sub.2 -adenosine receptors and are suitable for attachment to probes, drug carriers, or solid supports. These derivatives are characterized by the presence of a phenyl at the 8 position para-substituted with a functionalized chain to provide high water solubility and high receptor affinity to such an extent that these compounds are suitable for use as antiallergenic, antiasthmatic, or cardiotonic drugs, central nervous system stimulants, and diuretics.

Abstract: New derivatives of theophylline having the formula ##STR1## in which R denotes hydrogen or OH, n the numbers 0 or 1, X either >CH-- or >N--, Y either --O-- or --CO-- and R a five membered or six membered aryl ring or hetero-aryl ring, that is substituted in given cases with halogen, short chain alkyl groups, alkoxy groups or halogen-alkyl, and exhibit in addition to other properties, histamine-, serotinine- bradykynine- antagonistic, anti-anaphylactic and -adrenergic stimulating effects.

Abstract: Xanthine compounds of the formula: ##STR1## in which: R.sub.1 is hydrogen or (C.sub.1 -C.sub.5) alkyl;R.sub.2 is hydrogen, (C.sub.1 -C.sub.5) alkyl optionally having a double bond, or benzyl;R.sub.3 is hydrogen or methyl;A is (CH.sub.2).sub.n, in which n is an integer from 1 to 4, optionally substituted, when n is higher than 1, by hydroxy;X is nitrogen or ##STR2## and the substituents R are each (C.sub.1 -C.sub.5) alkyl or they form together a polymethylene chain from C.sub.4 to C.sub.6, optionally containing an oxygen or a sulfur atom.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of migraine and asthenia.

Abstract: Derivatives of theophylline substituted at the 7 position with various substituents containing a homopiperazine nucleus. The compounds can be prepared reacting theophylline or reactive intermediate containing same with a homopiperazine compound. The compounds exhibit antihistaminic activity and vasodilating activity.

Abstract: The new compound 3-(1,2,3,6-tetrahydro-1,3-dimethyl-2,6-Dioxopurine-7-acetyl-8-(2-phenyleth yl)-1-oxa-3,8-diazaspiro-(4,5)decan-2-one and the process of preparation are described.

Abstract: A new therapeutic agent with anti-platelet aggregant activity is described, with the chemical formula of 7-(1-methyl-5-p-methylbenzoylpyrrole-2-acetamidoethyl)-theophylline: ##STR1##

Abstract: Antitussive compounds of the formula I ##STR1## or physiologically acceptable acid addition salts thereof are disclosed, where A stands for straight or branched chain C.sub.1-5 alkylene or ##STR2## R.sub.1 stands for straight or branched chain C.sub.1-10 alkyl, halogenoalkyl, hydroxyalkyl, C.sub.5-6 cycloalkyl, vinyl, 2-ethoxyethyl, carbonylalkyl or aminoalkyl of the formula ##STR3## wherein R stands for hydrogen or methyl, n is 0 to 3,R.sub.2 stands for hydrogen or straight or branched chain alkyl,R.sub.3 stands for hydrogen or straight or branched chain alkyl or,R.sub.2 and R.sub.3 together with the nitrogen atom may form a 5-6 membered ring, which ring can optionally contain an oxygen or a second nitrogen atom, the latter, optionally substituted by methyl or,R.sub.1 can stand for a phenyl group of the formulaR.sub.4 R.sub.5 C.sub.6 H.sub.3whereinR.sub.4 and R.sub.5 represent independently hydrogen, chlorine, hydroxy, methoxy, ethoxy, methyl or amino or,R.sub.

Abstract: A novel compound has the following formula: ##STR1## in which R.sub.1 and R.sub.2 are methyl or a group having the formula: ##STR2## provided that one of R.sub.1 and R.sub.2 is methyl and the other is said group, wherein R stands for a hydrogen atom or a lower alkyl group, Z stands for a group ##STR3## in which X.sub.1 and X.sub.2, which may be the same or different, stand for a hydrogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group or a halogen atom, or a pyridyl group or a group ##STR4## in which Y.sub.1 and Y.sub.2, which may be the same or different stand for a hydrogen atom, a lower alkyl group, a lower alkoxy group, a trifluoromethyl group or a halogen atom, X stands for a nitrogen or carbon atom, and n is an integer of from 2 to 10, provided that when R.sub.2 is the group having the formula II, X is not carbon and Z is not pyridyl.

Abstract: New xanthine compounds of the formula: ##STR1## in which: R.sub.1 is hydrogen or alkyl from C.sub.1 to C.sub.5 inclusive;R.sub.2 is a hydrocarbon radical up to C.sub.6 having optionally a double bond, phenyl or benzyl;R.sub.3 is hydrogen, alkyl, hydroxyalkyl or dihydroxyalkyl each from C.sub.1 to C.sub.5R.sub.4 represents: ##STR2## in which: Y is hydrogen, halogen, alkyl or alkoxy from C.sub.1 to C.sub.5 or hydroxyl;Z is methylene or a straight or branched hydrocarbon radical from C.sub.2 to C.sub.5 optionally substituted by hydroxyl; andA is an amino group of the formula: ##STR3## p being 2 or 3; ##STR4## in which q is 1 or 2, and X is a single bond, oxygen or ##STR5## in which R.sub.5 is hydrogen, alkyl or alkylene up to C.sub.5, or ##STR6## in which m is an integer from 2 to 6 and R.sub.6 is alkyl from C.sub.1 to C.sub.5.

Abstract: There are disclosed theobromine derivatives wherein theobromine is substituted at the 1 position with substituted piperazino, homopiperazino and piperidino groups, and pharmacologically acceptable acid addition salts thereof. The compounds exhibit vasodilating and psychotropic and analgesic activities.

Abstract: Intermediates in the preparation of 9-position derivatives of theophylline useful in synthesizing theophylline immunogens and labeled conjugates. The labeled conjugates and the antibodies produced against the immunogens are particularly useful in homogeneous nonradioisotopic immunoassay for measuring theophylline in biological fluids such as serum.

Abstract: Compounds useful as tracers in the radioimmunoassay of xanthine derivatives such as theophylline and pharmacologically related drugs: ##STR1## wherein at least one R.sub.1, R.sub.3, R.sub.7 or R.sub.8 is a radioiodinated radical and wherein, if not substituted by a radioiodinated radical, the remaining R.sub.1, R.sub.3, R.sub.7 or R.sub.8 groups are otherwise identical to the substituents at these positions in the xanthine derivative to be assayed. Ordinarily, R.sub.1 is hydrogen, acetate or methyl; R.sub.3 is methyl; R.sub.7 is hydrogen, acetate or methyl; and R.sub.8 is hydrogen. The tracers are made by linking radioiodinatable or preradioiodinated radicals to the xanthine derivative which is to be assayed. The tracers may be employed in known radioimmunoassay techniques.

Abstract: Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, phenyl, or substituted phenyl having one or more substituents each of which is selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, chloro and dialkylamino wherein the alkyl portions, which can be the same or different, each have 1 to 5 carbon atoms, with the proviso that when R.sub.1 is alkoxy or alkylthio, then R.sub.2 cannot be alkoxy or alkylthio; X and X', which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.6 alkoxycarbonyl, halo, C.sub.1 -C.sub.

Abstract: Compounds useful as tracers in the radioimmunoassay of xanthine derivatives such as theophylline and pharmacologically related drugs: ##STR1## Wherein at least one R.sub.1, R.sub.3, R.sub.7 or R.sub.8 is a radioiodinated radical and wherein, if not substituted by a radioiodinated radical, the remaining R.sub.1, R.sub.3, R.sub.7 or R.sub.8 groups are otherwise identical to the substituents at these positions in the xanthine derivative to be assayed. Ordinarily, R.sub.1 is hydrogen, acetate or methyl; R.sub.3 is methyl; R.sub.7 is hydrogen, acetate or methyl; and R.sub.8 is hydrogen. The tracers are made by linking radioiodinatable or preradioiodinated radicals to the xanthine derivative which is to be assayed. The tracers may be employed in known radioimmunoassay techniques.

Abstract: The salts of N-unsubstituted, N-monosubstituted and N,N-disubstituted 7-(3-amino-2-hydroxypropyl)theophylline and 5-methylisoxazole-3-carboxylic acid are hypolipidaemic agents. The compounds, of which the 7-[3-(N-methyl-N-2-hydroxyethyl)amino-2-hydroxypropyl]-theophylline salt of 5-methylisoxazole-3-carboxylic acid is a representative embodiment, are prepared by allowing the isoxazole acid and the amine to react.