摘要:
Disclosed is a process for the oxidation of sulphonamides of formula (I) to N-sulphonyl imines of formula (II) using chromium (IV) dioxide as the oxidant. Also disclosed is a process for the preparation of imines of formula (iii) or combinatorial libraries thereof by removal of the sulphonyl group. In the formulae (I, II, III), R1 and R2 are independently selected from the group consisting of hydrogen and organic radicals not possessing a hydrogen atom in the position beta to the nitrogen atom of the sulphonamide group; and R3 is an organic radical selected from the group consisting of alkyl, substituted alkyl, aryl, and substituted aryl groups, and optionally R1 and R2 can form a ring.
摘要:
Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.
摘要:
Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.
摘要:
The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, isoxazolidine compounds which have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the isoxazolidine compounds are also taught.
摘要:
It has been newly found out that ascochlorin, which is a publicly known fat-soluble antibiotic, and its homologs serve as a ligand of retinoid X receptor and react in vivo with the amino group of serum protein to form Schiff bases without showing any side effect of retinoid. Ascochlorin and its homologs are usable in treating and/or preventing diseases or conditions which can be relieved by the retinoid X receptor ligand-dependent gene signal transcriptional regulation (for example, diseases caused by the expression of insulin resistance, hypertension, cerebrovascular diseases, rheumatoid arthritis, autoimmune diseases, Ca metabolic error, complication of diabetes, arteriosclerosis, etc.). Moreover, they can inhibit denaturation and/or necrosis of pancreatic Langerhans islet beta -cells and, therefore, are usable in making these cells to sustain the insulin productivity.
摘要:
Disclosed are novel dihydrobenzopyran compounds useful as antiarrhythmic and antifibrillatory agents. The compounds have a structure according to formula (A), or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification. Formula (A) also includes optical isomers, diastereomers or enantiomers. Also disclosed are pharmaceutical compositions and methods of treating disorders and conditions characterized by antiarrhythmic activity using these compounds or the pharmaceutical compositions containing them.
摘要:
A chroman derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, and a medicinal use thereof, wherein R is cyano, nitro, trihalomethyl, trihalomethoxy or halogen; R is lower alkoxyalkyl, aryloxyalkyl or dialkoxyalkyl; R is lower alkoxyalkyl or aryloxyalkyl; R is hydroxy, formyloxy or lower alkanoyloxy; X is N-H which may be substituted by lower alkyl, oxygen, sulfur or a single bond; Y is a residue of an aromatic or heterocyclic ring which may be substituted. The compound and pharmaceutically acceptable salt thereof have a prominent selective coronary vasodilator activity while having a minimized hypotensive effect. Therefore, they can selectively increase the coronary blood flow volume without the fear of causing sudden hypotension causative of tachycardia which adversely affects the heart, and hence are useful as a coronary vasodilator, in particular, as a preventive or remedy for cardiovascular disturbance such as angina pectoris or cardiac failure.
摘要翻译:由通式(I)表示的苯并二氢吡喃衍生物,其药学上可接受的盐及其医药用途,其中R 1为氰基,硝基,三卤代甲基,三卤甲氧基或卤素; R 2是低级烷氧基烷基,芳氧基烷基或二烷氧基烷基; R 3是低级烷氧基烷基或芳氧基烷基; R 4是羟基,甲酰氧基或低级烷酰氧基; X是可被低级烷基,氧,硫或单键取代的N-H; Y是可被取代的芳族或杂环的残基。 该化合物及其药学上可接受的盐具有突出的选择性冠状动脉血管扩张剂活性,同时具有最小化的降压作用。 因此,它们可以选择性地增加冠状动脉血流量,而不用担心引起心动过速的突发性低血压,这对心脏有不利影响,因此可用作冠状血管扩张剂,特别是作为心血管疾病如心绞痛的预防或治疗方法 心脏衰竭或心脏衰竭。
摘要:
The present invention discloses a new process for preparation of Nebivolol or it's pharmaceutically acceptable salt. More particularly, the invention discloses an improved economical process for the preparation of intermediate, 6-fluoro-3,4- dihydro-2H-1-benzopyran-2-carboxaldehyde of Formula – II, converting the 6- fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxaldehyde of Formula – II into mixture of [R*(S*)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran and [R*(R*)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran of Formula-V and separation of diastereomers of (R*)-6-Fluoro-3,4-dihydro-2-((S*)-oxiran-2-yl)- 2H-benzopran by forming azeotrope.
摘要:
The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a KATP channel to reduce an intraocular pressure.
摘要:
The present invention relates to the method of preparing chiral chromanes and chromenes in high yields by intramolecular hydroarylation of chiral aryl alkynes catalysed by either a silver(I) or gold(I) salt or complex in combination of a specific acid or by a silver(I) or gold(I) metal salt or complex having specific anion. By the hydroarylation a chromene is formed which has a chiral centre in the 2 position. The corresponding chromane is obtained by hydrogenation of the chromenes.