摘要:
1,4-Dihydropyridines have been found to counter several processes which play a role in the development of atherosclerotic vascular lesions, such as myocytes proliferation and migration, cholesterol metabolism in macrophages and oxidative modification of low density lipoproteins. They are therefore useful in the manufacture of medicaments for preventing, arresting and reversing atherosclerotic degradation in the arterial walls of humans. The preferred 1,4-dihydropyridines for this purpose are lercanidipine, (S)-lercanidipine and (R)-lercanidipine.
摘要:
A process for the preparation of methyl 1,1,N-trimethyl-N-(3,3-diphenyl-propyl)-2-aminoethyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-pyridine-3,5-dicarboxylate (lercanidipine) of formula I comprises reacting an acid halide of 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid with 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol in an aprotic solvent. The product can be isolated by industrially applicable crystallization techniques and is obtained in high yield as its anhydrous hydrochloride, a form which possesses high stability and low hygroscopicity.
摘要:
Disclosed are compositions and dosage forms containing moguisteine and having controlled release properties, methods for using such compositions and dosage forms and methods for making them.
摘要:
There are disclosed compounds of the general formula
The heteroatom X is preferably oxygen, but may have other values. The group W is preferably a carbonyl group, but may have other values. The preferred heterocyclic ring is thus a 4-oxo-4H-1-benzopyran ring. This may have a wide range of R₂, R₃, R₆ and R₇ substituents. Y is a linking group, chosen from a wide range, but including -COO- , -CONH- , -O- , -SO₂- and -SO₂NH-. Z is an alkylene chain, and B is a complex amine. These compounds and their prodrugs, enantiomers, diastereoisomers, N-oxides and pharmaceutically acceptable salts are useful for the treatment of hypertension and urinary tract troubles associated with benign prostatic hypertrophy, and for the treatment of other diseases.
摘要:
The present invention provides inhalable microparticles comprising cysteamine hyaluronate salt. Also a preparation method and a pharmaceutical composition thereof are provided.
摘要:
This invention relates to a method for the preparation of sertraline hydrochloride, (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphtalenamine hydrochloride, in its crystalline form II.
摘要:
Described is the use in the treatment of either male or female sexual dysfunction of selective antagonists of the alpha1B-adrenergic receptor and the pharmaceutical compositions containing them as compounds capable of helping the sexual act avoiding at the same time excessive side effects due to acute hypotension.
摘要:
Compounds of formula (I) are thus useful for treating disorders of the urinary tract. In the compounds I, R1 = one or more substituents selected from H, halogen, OH, alkyl, haloalkyl, alkoxy, haloalkoxy, NO2, nitro, phenyl, substituted phenyl, heterocycle, substituted heterocycle, NR3R4(R3 and R4 being H, alkyl, acyl or alkoxycarbonyl); R2 = one or two substituents selected from H, alkyl; Y = CH2 or a bond; Q = CO, CS or SO2; A = alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, heterocyclic, alkylamino, dialkylamino, arylamino or arylalkylamino, each of which is optionally substituted; n is 1 or 2; X = an amino moiety selected from formula (a), (b) and -N(R5)-CH2-(R5 = H, methyl, benzyl group; W = bond, N, CH, CH2, C(CN) C(OH) or C(COCH3) (when W represents a nitrogen atom or a CH, C(CN) C(OH) or C(COCH3) group, the group Z-B attaches to the W ring atom); when X is (a) or (b), Z = bond, O, S, CH2, CH2CH2, CO, CHOH, OCH2, NH, NHCO or NHCONHCH2, but when X is -N(R5)-CH2-group, Z represents a CH2CH2 or CH2O group or Z and B together represent a 2,3-dihydro-benzo[1,4]dioxin-2-yl group; and B is a monocyclic or bicyclic aryl group or a monocyclic or bicyclic heterocycle, each of which is optionally substituted.