205504-06-9

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Chemical Properties

off-white to brown powder

Upstream product

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Relevant academic research and scientific papers

Azaheterocyclylmethyl derivatives of 2,3-dihydro-1,4-dioxino[2,3-f]-quinoline as 5-HT1A antagonists

Compounds of the formula useful for the treatment of disorders, such as anxiety, aggression and stress, and for the control of various physiological phenomena, such as appetite, thermoregulation, sleep and sexual behavior.

N-substituted imide derivatives with serotonergic activity

Compounds of the Formula (I) wherein R2, Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic neuron-related diseases.

NEW RENIN-INHIBITORY OLIGOPEPTIDES, THEIR PREPARATION AND THEIR USE

Oligopeptides of formula (I): STR1 where R 1-R 5 are various organic groups, and A represents a group of formula--NH--or--(CH 2) n--, in which n represents an integer of from 1 to 3, have renin-inhibitory activity and are particularly suitable for oral administration. They may be prepared by condensing their component amino acids or lower oligopeptides using conventional peptide synthesis reactions.

HETEROCYCLIC CARBOXYLIC ACID AMIDES AND ESTERS OF AZABICYCLIC COMPOUNDS AS GASTRIC PROKINETIC, ANTIEMETIC, ANXIOLYTIC AND ANTIARRHYTHMIC AGENTS

Novel 1-azabicyclo[3.2.1]octan-5-ylmethyl and 1-azabicyclo[3.3. 1] nonan-5-ylmethyl amines and alcohols are coupled with aryl carboxylic acids to obtain compounds having the formula: STR1 wherein X is--O--or--NH--and n is 1 or 2 which are useful in increasing gastric motility, in preventing emesis and emesis caused by anticancer treatments, anxiety, certain arrhythmias, and disorders caused by serotonin imbalances.

Aminoesters of rapamycin

A compound of the structure STR1 wherein R1 and R2 are each, independently, hydrogen or STR2 with the proviso that R1 and R2 are not both hydrogen; R3 is hydrogen, alkyl, aralkyl, --(CH2)q CO2 R6,--(CH2)r NR7 CO2 R8, carbamylalkyl, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxyphenyklmethyl, imidazoylmethyl or phenyl which is optionally mono-, di-, or tri-substituted with a sustituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid; R4 and R7 are each, independently, hydrogen, alkyl, or aralkyl; R5, R6, and R8 are each, indpendently, alkyl, aralkyl, fluorenylmethyl, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid; m is 0-4; n is 0-4; p is 1-2; q is 0-4; r is 0-4; wherein R3, R4, m, and n are independent in each of the STR3 subunits when p=2; or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation, and by virtue of its antifungal activity is useful in treating fungal infections.

Quinoline-3-carboxylic acid derivatives

Compounds of formula (I): STR1 (in which R1 is alkoxy, R is alkyl, haloalkyl, alkylamino, cycloalkyl or optionally substituted phenyl, X is chlorine or fluorine and Y is selected from certain specific heterocycles) have excellent antibacterial activity. They may be prepared by introducing the group represented by Y into the corresponding compound in which Y is replaced by a halogen atom.

1H-pyrazole-1-alkanamines antiarrhythmic compositions and use

N-[alkylamino)alkyl]-3,4(or 4,5)-diaryl-1H-pyrazole-1-(branched)alkanamides and pyrazole-1-alkanamines useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic acid with an appropriate diamine followed by reduction or by reacting the anion of a lower-alkyl ester of a pyrazole-1-acetic acid with an alkylating agent followed by displacement of the ester by an appropriate amine.

Substituted 3,4-dihydroxy phenylethylamino compounds

Novel compounds of the formula STR1 in which one of R30 and R40 represents a substituted phenylalkyl group, the other of R30 and R40 represents hydrogen or halogen, and R50 and R60 each independently represent hydrogen or alkyl; in addition R60 may represent a substituted alkyl chain interrupted by N. The compounds of the invention are useful for the treatment or prophylaxis of renal failure or cardiovascular disease.

Aromatic compounds

There are described compounds of formula I, STR1 in which X represents a C2 to 8 alkylene chain optionally interrupted by a double bond or by S(O)n, wherein n is 0, 1 or 2; Y represents O or NH, l and m each independently represent 2, 3 or 4, R