A Negishi cross-coupling of alkylpyridinium salts and alkylzinc halides has been developed. This is the first example of alkyl–alkyl bond formation via cross-coupling of an alkyl amine derivative w...

/pdf/harnessing-alkylpyridinium-salts-as-electrophiles-in-12hiu93u67.pdf

Harnessing Alkylpyridinium Salts as Electrophiles in Deaminative Alkyl–Alkyl Cross-Couplings

The invention relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis. The method comprises administering to a subject in need of treatment a therapeutically effective amount of a compound that has 5-HT3 receptor antagonist activity and NorAdrenaline Reuptake Inhibitor (NARI) activity. The invention further relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of urinary frequency, urinary urgency, urinary urge incontinence, nocturia and enuresis, comprising coadministering to said subject a first amount of a 5­HT3 antagonist and a second amount of a NARI, wherein the first and second amounts together comprise a therapeutically effective amount or are each present in a therapeutically effective amount.

Method of treating lower urinary tract disorders

This invention relates to a compound of the Formula I: ##STR1## as a racemic mixture and its individual enantiomers, in particular the (R)-enantiomer, and their pharmaceutically acceptable salts. These compounds are useful as sodium channel blockers, and are particularly useful for the alleviation of neuropathic pain.

Treatment of neuropathic pain

Disclosed are compounds of the formula: wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substitutents which may together form ring structutes; m is zero, one or two; and R5 and R6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.

Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives; new classes of dopamine receptor subtype specific ligands

The compounds of formula I ##STR1## where R1, R2 and R have various significances, and physiologically acceptable hydrolyzable derivatives thereof having the hydroxy group in the 2 position of the 3-aminopropoxy side chain in esterified form, are useful as cardiotonic, anti-arrhythmic, α- and β-adrenoceptor blocking agents.

3-Aminopropoxyaryl derivatives, their preparation and pharmaceutical compositions containing them

Neue substituierte 2-phenylamino-imidazoline-(2), deren saeureadditionssalze, diese enthaltende arzneimittel und verfahren zur herstellung derselben

The compounds are 1-phenoxy-2-hydroxy-3-alkylamino-propanes and non-toxic acid addition salts thereof, useful as beta -adrenolytics and hypotensives in warm-blooded animals.

1-phenoxy-2-hydroxy-3-sec. alkylamino-propanes

Compounds of the formula ##EQU1## wherein R is hydrogen or alkyl of 1 to 3 carbon atoms, and R 1 is hydrogen or methyl, And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anticonvulsives and antiarrhythmics in warmblooded animals.

1-(2',6'-Dimethyl-phenoxy)-2-amino-alkanes and salts thereof

Compounds of the formula ##STR1## wherein R 1 and R 2 , which may be identical to or different from each other, are each hydrogen, chlorine, bromine or alkyl of 1 to 3 carbon atoms, R 3 is hydrogen, furfuryl, hydroxyethyl, β-hydroxy-phenethyl, monochlorophenyl-ethyl, dichlorophenyl-ethyl, N-ethyl-piperidyl or --A--NR 6 R 7 , where A is alkylene of 1 to 5 carbon atoms, and R 6 and R 7 are alkyl of 1 to 2 carbon atoms or, together with each other and the nitrogen atom to which they are attached, form a heterocycle selected from the group consisting of pyrrolidino, morpholino, piperazino or N'-dimethylphenyl-piperazino, R 4 is hydrogen or, together with R 3 and the nitrogen to which they are attached, forms a heterocycle selected from the group consisting of piperidino, morpholino, dimethyl-morpholino or N'-methyl-piperazino, R 5 is hydrogen, alkyl of 1 to 3 carbon atoms, hydroxy-ethyl, diethylamino-ethyl or furfuryl, Provided, however, that R 1 and R 2 are other than both hydrogen or both alkyl at the same time and that R 3 and R 5 are other than both hydrogen at the same time, or a non-toxic, pharmacologically acceptable acid addition salt thereof; the compounds as well as the salt are useful as hypotensives, platelet aggregation inhibitors and antiarrhythmics.

2-Amino-4-phenyl-2-imidazolines and salts thereof

Compounds of the formula ##EQU1## wherein R1 is allyl, allyloxy or chlorine, R2 is hydrogen or methyl, R3 is hydrogen, alkyl of 1 to 5 carbon atoms or benzyl, and n is an integer from 2 to 6, inclusive, Provided, however, that when R1 is allyl or allyloxy, R2 is hydrogen; and their non-toxic, pharmacologically acceptable acid addition salts; the compounds as well as their salts are useful as β-adrenergic blocking agents and hypotensives.

N,N'bis-(3-phenoxy-2-hydroxy-propyl)-alkylenediamines and salts thereof

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