摘要:
A process is described for the preparation of a compound of formula (I) or a stereoisomeric compound thereof, in which the 1,2-position is saturated or is a double bond; X and X are each independently hydrogen or halogen; R is hydrogen or acyl; R is hydroxyl, acyloxy or oxo; and R is alkyl, by reacting a compound of formula (II) with an aldehyde R CHO in either phosphoric acid or about 60 % to about 75 % w/w sulphuric acid. Compounds of formula (I) are either pharmacologically active steroids or are intermediates in the synthesis of pharmacologically active steroids.
摘要:
The invention is related to a solution formulation of Cyclosporin A in 1,1,1,2,3,3,3-heptafluoropropane which is suitable for administration to a patient by inhalation using any standard medicinal aerosol device. Standard excipients normally used in medicinal aerosol formulations to aid valve lubrication or improve flavour may also be added. Other medicaments in solution or suspension may be used in addition to Cyclosporin A and other propellants in addition to 1,1,1,2,3,3,3-heptafluoropropane may be used.
摘要:
An inhaler for inhalation of a medicament from a pierced capsule has a swirling or emptying chamber (29) where the capsule is emptied by inhalation action of an operator. A rotary magazine (23) for a multi-unit dose inhaler is also disclosed, which holds a number of capsules containing a medicament in a number of recesses arranged around the periphery of the magazine. The capsules are held in place by pins (101) or plugs at both ends. Either the capsules are pierced before being loaded into the magazine (23) or they are pierced by the pins (101) when they are loaded into the magazine (23). In either case a seal may be provided around the ends of the capsules near the holes which are plugged to keep them fresh. When a recess is rotated to a particular position (41) within the magazine (23) then it releases its capsule. Contents of a capsule are drawn out during inhalation when the capsule is in the swirling chamber (29). A motor can be used to operate the magazine.
摘要:
Compounds of formula (I) are described, wherein: R1 is CN, CH¿2?CN, CH=CHCN, CHO, or CH=CHCO2H; R?2¿ is aryl lower alkoxy, heteroaryl lower alkoxy, aryl lower alkylthio or heteroaryl lower alkylthio in which each of the aryl and heteroaryl moieties is optionally substituted; R3 is halogen; R4 is optionally substituted aryl or optionally substituted heteroaryl; R5 is carboxy or an acid isostere; X is oxygen or sulphur; and n is zero or 1; and their N-oxides and prodrugs, and pharmaceutically acceptable salts thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.
摘要:
This invention is directed to compounds of formula (I), wherein R1 is an optionally substituted lower alkyl group; R2 is an optionally substituted oxaaliphatic group; R3 is an optionally substituted aryl group or an optionally substituted heteroaryl group; Q?1, Q2 and Q3¿ are independently nitrogen, CX or CH; Z1 is oxygen or sulfur; Z2 is -CH=CH-, -C C-, -CH¿2?-CZ-, -CZCH2-, -CZ-CZ-, -CH2-NH-, -CH2-O-, -CH2-S-, -CX2-O-, -CZNH-, -NH-CH2-, -O-CH2_, -SCH2-, -SOCH2-, -SO2CH2-, -O-CX2-, -O-CZ-, -NH-CZ-, -N=N-, -NH-SO2-, -SO2-NH-, -CZ-CZ-NH-, -NH-CO-O-, -O-CO-NH- or -NH-CO-NH-; Z is oxygen or sulfur; and X is halo; or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which possess useful pharmaceutical properties. They are especially useful for inhibiting the production or physiological effects of TNF and inhibit cyclic AMP. The present invention is also directed to their pharmaceutical use, pharmaceutical compositions containing the compounds, and methods for their preparation.
摘要:
This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
摘要:
Dérivés de benzanilide de la formule (I) où R1 représente alkyle, éventuellement interrompu par un hétéroatome ou plus, X1 représente oxygène, soufre ou -NR5-, où R5 représente hydrogène ou alkyle ou alcanoyle éventuellement substitué par de l'halogène, R2 représente hydrogène ou alkyle, R3 représente alkyle, alcoxy, alkylthio, diméthylamino ou un groupe hétérocyclo contenant au moins un atome d'azote et lié par cet atome d'azote au reste de la molécule, ou un atome d'halogène, et R4 représente un alkyle contenant jusqu'à 10 atomes de carbone, contenant facultativement une ou plusieurs double(s) ou triple(s) liaison(s) carbone-carbone, et facultativement interrompu par un ou plusieurs hétéroatome(s).
摘要:
Un inhalateur permettant l'inhalation d'un médicament pulvérulent à partir de l'intérieur d'une capsule comprend une chambre (24) dans laquelle la capsule est positionnée avec son axe longitudinal dans le plan médian de la chambre et ainsi parallèlement aux parois avant (29) et arrière (30) de ladite chambre, l'espace entre lesdites parois avant et arrière étant légèrement supérieur au diamètre de la capsule, et le diamètre de ladite chambre est supérieur à la longueur de la capsule. Le dispositif comprend des aiguilles (21) servant de moyen d'ouverture pour percer les extrémités de la capsule lorsqu'elle se trouve dans un évidement (25). Des admissions d'air (26), une chambre (24) et un embout (27) ont une relation spatiale créant un mouvement tourbillonnaire de l'écoulement d'air permettant un bon vidage de la capsule et une fine dispersion des poudres. Les parois intérieures de la chambre et de l'embout peuvent être en matière antistatique.