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The new pyridazine containing iron complexes, [N,N,N?,N?-tetrakis(3-pyridazylmethyl)propylenediamine]iron(II)(PF6)2 (1) and [N,N?-bis(2-pyridazylmethyl)-N,N?-bis(2-pyridylmethyl)propylenediamine]iron(II) (PF6)2 (2) were synthesized and their reactivity towards protonation was compared to that of the analogous tetrapyridine complex [N,N,N?,N?-tetrakis(2-pyridylmethyl)propylenediamine]iron(II)(PF6)2 (3). The solution and solid-state structures were confirmed by NMR and X-ray crystallographic studies. For 1?3, the ligands bind in a hexadentate fashion giving similar octahedral structures with an N6 coordination environment. Across the series, the increasing number of pyridazines has only modest effects on the spectroscopic and electrochemical properties of the metal. Nevertheless, their reactivity towards protonation is drastically different. While 2 and 3 decompose in the presence of strong acids, 1 is able to be stably protonated as a result of cooperative second sphere interactions.

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Substituted 1 H-imidazo[4,5-b]pyridin-2(3H)-ones as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity.

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New thioamide derivatives of 2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide (29) and related compounds (in which the tetrahydrothiophene ring was replaced by tetrahydrothiopyran, tetrahydrofuran, 1,3-dithiane, or 1,3-oxathiane and where the pyridine ring was repleaced by other nitrogen heterocycles) were synthesized and tested for their antisecretory and antiulcer activities.These thioamides were prepared according to one of the following methods: (i) reaction of an isothiocyanate with the carbanion of the corresponding cyclic precursor (for secondary thioamides); (ii) reaction of ammonia or an amine with the dithio ester prepared from the same precursor (for primary, secondary, and tertiary thioamides).These thioamides were evaluated by the Shay method to measure their antisecretory activity and by the stress-induced-ulcer method to test their antiulcer activity.Structure-activity relationships are discussed.N-Methyl-2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide (R.P. 40749,30) exhibited activities that were at least 10 times higher than those reported for cimetidine.

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 27349-66-2, name is 3-(Chloromethyl)pyridazine hydrochloride, introducing its new discovery. Recommanded Product: 3-(Chloromethyl)pyridazine hydrochloride

The new pyridazine containing iron complexes, [N,N,N?,N?-tetrakis(3-pyridazylmethyl)propylenediamine]iron(II)(PF6)2 (1) and [N,N?-bis(2-pyridazylmethyl)-N,N?-bis(2-pyridylmethyl)propylenediamine]iron(II) (PF6)2 (2) were synthesized and their reactivity towards protonation was compared to that of the analogous tetrapyridine complex [N,N,N?,N?-tetrakis(2-pyridylmethyl)propylenediamine]iron(II)(PF6)2 (3). The solution and solid-state structures were confirmed by NMR and X-ray crystallographic studies. For 1?3, the ligands bind in a hexadentate fashion giving similar octahedral structures with an N6 coordination environment. Across the series, the increasing number of pyridazines has only modest effects on the spectroscopic and electrochemical properties of the metal. Nevertheless, their reactivity towards protonation is drastically different. While 2 and 3 decompose in the presence of strong acids, 1 is able to be stably protonated as a result of cooperative second sphere interactions.

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Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: STR1 in which: B represents a –S, –SO–, or –SO2 — group, R1 and R2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen such as chlorine, bromine or iodine, A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical in which the hydroxy is optionally substituted by a lower alkyl radical, Ar represents a group STR2 R4 denotes hydrogen or an alkyl radical and Cy represents a cyclic group.

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New thioamide derivatives of 2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide (29) and related compounds (in which the tetrahydrothiophene ring was replaced by tetrahydrothiopyran, tetrahydrofuran, 1,3-dithiane, or 1,3-oxathiane and where the pyridine ring was repleaced by other nitrogen heterocycles) were synthesized and tested for their antisecretory and antiulcer activities.These thioamides were prepared according to one of the following methods: (i) reaction of an isothiocyanate with the carbanion of the corresponding cyclic precursor (for secondary thioamides); (ii) reaction of ammonia or an amine with the dithio ester prepared from the same precursor (for primary, secondary, and tertiary thioamides).These thioamides were evaluated by the Shay method to measure their antisecretory activity and by the stress-induced-ulcer method to test their antiulcer activity.Structure-activity relationships are discussed.N-Methyl-2-(2-pyridyl)tetrahydrothiophene-2-carbothioamide (R.P. 40749,30) exhibited activities that were at least 10 times higher than those reported for cimetidine.

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Alkyl- or aryl-aminoalkoxy-benzene-sulfonyl indoles

The present invention relates to aminoalkoxyphenyl derivatives of formula: STR1 and its N-oxide and pharmaceutically acceptable salts, in which: B represents a–S–, –SO– or –SO2 — group, R1 and R2, which are identical or different, each denote hydrogen, a methyl or ethyl radial or a halogen atom, A denotes a straight-or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radial in which the hydroxy is optionally substituted by a lower alkyl radical, R3 denotes an alkkyl radical or a radical of formula: in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and Ar denotes a pyridyl, phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl group or lower alkoxy groups, R11 denotes hydrogen or a lower alkyl, phenyl, diphenylmethyl, benzyl or halogenobenzyl radical, R4 denotes hydrogen or an alkyl radical, or R3 and R4 when taken together denote an alkylene or alkenylene radical having from 3 to 6 carbon atoms and optionally substituted with a phenyl radical or optionally interrupted by STR2 R represent hydrogen, an alkyl radical, a cycloalkyl radical, a benzyl radical or a phenyl radical optionally substituted with one or more substituents, which may be identical or different, selected from halogen atoms and from lower alkyl, lower alkoxy or nitro groups, are described. The compounds of the invention possess exceptional pharmacological properties, especially calcium transport inhibitory properties, as well as bradycardic, hypotensive and antiadrenergic properties.

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Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction

Compounds of the formulae (IA) and (IB): wherein R1 is C1 to C3 alkyl optionally substituted with phenyl, Het or a N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group is optionally substituted by one or more substitutents selected from C1 to C4 alkoxy; halo; CN; CF3; OCF3 or C1 to C4 alkyl wherein said C1 to C4 alkyl group is optionally substituted by C1 to C4 haloalkyl or haloalkoxy either of which is substituted by one or more halo atoms; R2 is C1 to C6 alkyl and R13 is OR3 or NR5R6, or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity are potent and selective inhibitors of type 5 cyclic guanosine 3?,5?-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).

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Use of aminoalkoxyphenyl derivatives for reducing and/or controlling excessive intraocular pressure

The present invention is directed to the use of aminoalkoxyphenyl derivatives for reducing and/or controlling excessive intraocular pressure and compositions suitable for this case.

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Aminoalkoxyphenyl derivatives, process of preparation and compositions containing the same

An aminoalkoxyphenyl compound of formula STR1 as well as a pharmaceutically acceptable salt of this compound.

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