摘要:
The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR3 or a direct bond; R1 is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C1-6alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R2 is aryl, Het1, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C1-4alkyl; R4 and R5 independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6akylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6 or NR7R8; R6 is substituted sulfonyl or sulfinyl; R7 and R8 are hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R9 and R10 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, carboxyl, C1-4alkyloxycarbonyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R12 and R13 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl and R6; aryl is optionally substituted phenyl; Het1, Het2 and Het3 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
摘要翻译:本发明涉及配制N-氧化物的化合物,其药学上可接受的加成盐及其立体化学异构形式,p和q分别为0,1,2,3或4,q也为5; X是O,S,NR 3或直接键; R 1是氢,羟基,卤素,任选取代的氨基,任选取代的C 1-6烷基,C 1-6烷氧基,C 3-7环烷基或芳基; R 2是芳基,Het 1,C 3-7环烷基,任选取代的C 1-6烷基; 并且如果X是O,S或NR 3,则R 2也可以是羰基或硫代羰基连接的取代基; R 3是氢或C 1-4烷基; R 4和R 5独立地是任选取代的C 1-6烷基,卤素,羟基,巯基,C 1-6烷氧基,C 1-6烷硫基,C 1-6烷基羰基氧基,芳基,氰基,硝基,Het 3, 或NR 7 R 8; R 6是取代的磺酰基或亚磺酰基; R 7和R 8是氢,任选取代的C 1-4烷基,芳基,羰基或硫代羰基连接的取代基,C 3-7环烷基,Het 3和R 6; R 9和R 10各自独立地选自氢,任选取代的C 1-4烷基,苯基,羰基或硫代羰基连接的取代基,C 3-7环烷基,Het 3和R 6; R 11是羟基,巯基,氰基,硝基,卤素,三卤代甲基,C 1-4烷氧基,羧基,C 1-4烷氧基羰基,三卤代C 1-4烷基磺酰氧基,R 6,NR 7 R 8,C(= O) NR 7 R 8,芳基,芳氧基,芳基羰基,C 3-7环烷基,C 3-7环烷氧基,邻苯二甲酰亚胺-2-基,Het 3和C(= O)Het 3; R 12和R 13各自独立地选自氢,任选取代的C 1-4烷基,苯基,羰基或硫代羰基连接的取代基,C 3-7环烷基和R 6; 芳基是任选取代的苯基; Het <1>,Het <
摘要:
A unique PVP-iodide solid solution is prepared by drying a solution of PVP and iodide wherein the PVP:I ratio is preferably in the range of about 2:1 to 6:1, which dried product may then be mechanically blended with elemental iodine at ambient temperature to rapidly form a stabilized PVP-iodide-iodine complex, characterized in that the resulting product comprises a single solid phase.
摘要:
A composition and method for controlling cortisol levels in mammals is provided in which a mixture of a member from the group whole bee venom and mellitin and partially hydrolyzed cocoa butter is topically applied to the mammal being treated.
摘要:
Disclosed a process for making greater use of female gametes in herbivorous mannals. The techniques include methods of obtaining ova from donor, preparation of recipients, detection of oestrus, and transplant techniques. Also disclosed are methods of making greater desired use of ova of these mammals. Among those are techniques by sex determination, for freezing and thawing eggs, for tissue culture of eggs and for clonal production of like embroyos utilized for transplantation to achieve a greater number of clonal differentiated cellular bodies having like genetic characteristics.
摘要:
A PHARMACEUTICAL PREPARATION SUITABLE FOR ORAL ADMINISTRATION COMPRISES AN ACTIVE THEREAPEUTIC INGREDIENT IS SILID SOLUTION WITH A STEROIDAL LIPID, TOGETHER WITH A PHARMACEUTICALLY ACCEPTABLE CARRIER FOR SAID MIXTURE. THE THEREPEUTIC INGREDIENT MAY BE, FOR EXAMPLE, A NATURAL STEROID HORMONE, AND THE LIPID MAY BE A STEROL. THE PREPARATION MAY BE PROVIDED IN UNIT DOSAGE FORMS SUCH AS TABLETS, LOZENGES, CAPSULES, AND THE LIKE.
摘要:
A HORMONE-LIKE SUBSTANCE OF POLYEPTIDE TYPE HAVING SERUM CALCIUM REDUCING PROPERTY IN MAMMALS, WHICH IS ISOLATED FROM AN EEL, GENUS ANGUILLA, BY EXTRACTING HEART, PARTICUALRLY PERICARDIAL MEMBRANE AND/OR A TISSURE COMPRISING VENA CAVA ATTACHED TO OESOPHAGUS NEAR THE HEART WITH AN EXTRACTION SOLVENT, I.E. WATER, DILUTE ORGANIC ACID, DILUTE MINERAL ACID OR A MIXTURE OF WATER, HYDROPHILLIC ORGANIC SOLVENT AND AT LEAST ONE OF THE DILUTE ACIDS, AND REMOVING CONTAMINATING PROTEINS FROM THE RESULTING EXTRACT OR FROM AN EXTRACT LIQUID OBTAINED BY REMOVING SOLID FROM SAID EXTRACT. THE SUBSTANCE IS USEFUL FOR TREATMENT OF VARIOUS METABOLIC OSTEOLOGICAL DISEASE, FOR EXPAMPLE, OSTEOPETROSIS AND GERONOTOLOGICAL DISEASES. THE EELS USED ARE PREFERABLY THOSE BRED IN SEA WATER OR AN AQUEOUS SODIUM CHLORIDE SOLUTION SIMILAR IN COMPOSITION THERETO.
摘要:
DISCLOSED HEREIN IS A PROCESS FOR THE FRACTIONATION OF SNAKE VENOM AND THE UTILIZATION OF CERTAIN OF THE RESULTANT FRACTIONS AS ANGIOTENSIN CONVERTING ENZYME INHIBITORS.
摘要:
A therapeutic composition of methionine with 2dimethylaminoethanol in aqueous media. A method of extending life span in animals and the survival time of cells, tissues and organs in vitro by treatment with a mixture of methionine and 2dimethylaminoethanol or materials which form 2-dimethylaminoethanol in aqueous media.
摘要:
THERE HAVE BEEN PREPARED THE NEW 17-BUTYRATES, 21ESTERS OF 6A,9A-DIFLUOROPREDNISOLONE USEFUL AN ANTI-INFLAMMATORY AGENTS. THEY MAY BE MIXED WITH SUITABLE PHARMACEUTICAL CARRIERS TO OBTAIN PHARMACEUTICAL COMPOSITIONS FOR THE SYSTEMIC AND LOCAL TREATMENT OF INFLAMMATORY CONDITIONS AND DISEASES.
摘要:
ENCHANCEMENT OF THE GROWTH RATE OF FEMALE RUMINANT ANIMALS BY PARENTERALLY ADMINSTERING TO SAID ANIMALS, IN A SINGLE DOSE, A GROWTH-ENCHANCING AMOUNT OF A SELECTED DERIVATIVE OF CERTAIN HALOGENATED 16A, 17A-DIHYDROXYSTEROIDS OF THE PREGNANE SERIES.