摘要:
This invention is directed to a pharmacologically acceptable composition for inhibiting nitric oxide synthase in a mammal, which includes a mercapto or seleno derivative and a pharmaceutically acceptable carrier. The invention also concerns a method of inhibiting nitric oxide synthase, selectively inhibiting the inducible isoform of nitric oxide synthase, and treating various conditions where there is an advantage in inhibiting nitric oxide biosynthesis. The method includes the step of administering to a mammal a mercapto or seleno derivative in pure form or in a pharmaceutically acceptable carrier.
摘要:
In the production of spherulitic nitroguanidine having a high bulk and tap ensity nitroguanidine is dissolved in dipolar, aprotic solvents, e.g. DMF, DMSO, NMP, etc., by heating to above the saturation temperature t.sub.s and the supersaturated solution is cooled with a controlled temperature gradient (.degree.C./min), crystallization being assisted by the addition of particulate, spherulitic material. In order to obtain spherical nitroguanidine with high yield in a continuous process and with mother liquor reuse, during the heating to above the saturation temperature t.sub.s, spherical control particles with a diameter of 5 to 500 .mu.m are regularly added to the solution in a quantity of 0.05 to 5.00 mass %. The particle size is chosen in such a way that, as a function of the solution behaviour of the nitroguanidine used and its concentration, on dropping below the saturation temperature spherical control particles are still present in the indicated quantity in the supersaturated solution.
摘要:
Compounds of formula (I): ##STR1## (wherein: R.sup.0 is hydrogen, methyl or hydroxymethyl; R.sup.1 is substituted alkyl; R.sup.2 and R.sup.3 are each hydrogen, halogen, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkyl, nitro, haloalkyl, or substituted alkyl; X is oxygen or sulfur; and Ar optionally substituted phenyl or naphthyl); and pharmaceutically acceptable salts thereof have a variety of valuable pharmaceutical activities, including anti-diabetic and anti-obesity activities; in addition, they are capable of treating or preventing hyperlipemia and hyperglycemia and, by inhibiting the action of aldose reductase, they can also be effective in the treatment and prevention of complications of diabetes.
摘要翻译:式(I)化合物:其中:R 0是氢,甲基或羟甲基; R 1是取代的烷基; R 2和R 3各自是氢,卤素,羟基,烷氧基,羧基,烷氧基羰基,烷基,硝基, 卤代烷基或取代烷基; X为氧或硫; Ar为任选取代的苯基或萘基); 和其药学上可接受的盐具有多种有价值的药物活性,包括抗糖尿病和抗肥胖活性; 此外,它们能够治疗或预防高脂血症和高血糖,并且通过抑制醛糖还原酶的作用,它们也可有效治疗和预防糖尿病并发症。
摘要:
The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
摘要:
Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.
摘要:
A continuous process for forming spheroidal high bulk density nitroguanid crystals from an aqueous solution of nitroguanidine which contains methylcellulose and partially hydrolyzed poly(vinyl alcohol) as crystal habit modifiers. A saturated aqueous solution of nitroguanidine is formed at a temperature T.sub.1 where 70.degree. C..ltoreq.T.sub.1 .ltoreq.100.degree. C. and crystallization occurs at a lower temperature T.sub.2 where 20.degree. C..ltoreq.T.sub.1 -T.sub.2 .ltoreq.50.degree. C.
摘要:
Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.
摘要:
The invention relates to compounds of the general formula AB, which may be a salt or an amide, wherein:A represents a cyclooxygenase inhibitor having an accessible acidic function andB represents the L-form of arginine analogues of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 represent various substituents, process for the preparation of such compounds and pharmaceutical composition thereof.
摘要:
Novel substituted nitroguanidine derivatives and salts thereof having the following formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted heterocyclic group; R.sup.2 is a group attached through a sulfur atom, a group attached through a phosphorus atom, cyano, --CO--OR.sup.6 wherein R.sup.6 is a substituted or unsubstituted hydrocarbon group or a substituted or unsubstituted heterocyclic group, or --CO--NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8, which are the same or different, are each independently hydrogen, a substituted or unsubstituted hydrocarbon group or a substituted or unsubstituted heterocyclic group, or R.sup.7 and R.sup.8, taken together with the nitrogen atom to which they are attached are a cyclic amino group; R.sup.3 is hydrogen, a substituted or unsubstituted hydrocarbon group (except for one substituted with an oxo group at the binding site), a group attached through a sulfur atom, a group attached through a phosphorus atom, cyano, --CO--R.sup.9 wherein R.sup.9 is hydrogen, a substituted or unsubstituted hydrocarbon group or a substituted or unsubstituted heterocyclic group, --CO--OR.sup.10 wherein R.sup.10 is a substituted or unsubstituted hydrocarbon group or a substituted or unsubstituted heterocyclic group, or --CO--NR.sup.11 R.sup.12 wherein R.sup.11 and R.sup.12, which are the same or different, are each independently hydrogen, a substituted or unsubstituted hydrocarbon group or a substituted or unsubstituted heterocyclic group, or R.sup.11 and R.sup.12, taken together with the nitrogen atom to which they are attached are a cyclic amino group; and R.sup.4 is hydrogen or a lower alkyl group; which have unexpectedly potent pesticidal activity and very low toxicity.
摘要:
A process of preparing spherical high bulk density nitroguanidine by dissing low bulk density nitroguanidine in N-methyl pyrrolidone at elevated temperatures and then cooling the solution to lower temperatures as a liquid characterized as a nonsolvent for the nitroguanidine is provided. The process is enhanced by inclusion in the solution of from about 1 ppm up to about 250 ppm of a metal salt such as nickel nitrate, zinc nitrate or chromium nitrate, preferably from about 20 to about 50 ppm.