A series of 4,5-disubstituted cis-pyrrolidinones was investigated as inhibitors of 17beta-HSD II for the treatment of osteoporosis. Biochemical data for several compounds are given. Compound 42 was selected as the lead candidate.
The application of poloxamer in pharmaceutics used as additives or substrates in tablets, solid lipid nanoparticles, suppositories,controlled release gels, ophthalmic delivery system was summarized.
Neuraminidase is one of the most important surface glycoproteins of Influenza Virus and has been considered an attractive target for the development of new drugs for Influenza. This paper reviews the progress of inhibitors of Neuraminidase.
Objective To observe the efficarcy of a bone- fortifying compound for treating primary osteoporosis(PO);to observe its antioxidant action,and the relation of bone density(BD) with superoxide dismutase(SOD).Method 80 cases of primary osteoporosis were studied;Lumbar pain,BD,SOD,MDA were studied before and after treatment.Result In the treatment group,total efficacy rate was 95.65% ,BD rose by 3.22% .Conclusion Our bone- fortifying compound is efficacious for PO,enhancing bone formation and inhibiting bone absorption,and has antioxidant action as well,thus slowing the aging process.
Objective:To study the inhibition of Liuweidihuang Decoction, Jinguishengi Pills, Lizhong Decoction and Guizhigancao Decoction on Sister Chromatid Exchanges (SCE) induced by CPP. Methods:The bone marrow cell of pure ICR species of mouse was used as an experimental material and the SCE induced by CPP was used as an index. Results:Four kinds of prescription showed the inhibition on SCE induced by CPP. Conclusion:4 kinds of prescription have a potential prevention ation of tumor.
A method of treating a disease other than cancer, mediated by P-38 which comprises administering a compound of formula I ** ** formula wherein A is ** ** formula B is an aryl or heteroaryl to tricyclic, substituted or unsubstituted, of up to 30 carbon atoms with at least one aromatic structure containing 0-4 members 6 members group consisting of nitrogen, oxygen and sulfur, wherein if B is substituted, it is substituted by one or more substituents selected from the group consisting of halogen, up to per-halo, and Wn, where n is 0-3 and each W is independently selected from the group consisting of -CN, -CO2R7, -C (O) NR7R7, -C (O) - R7, -NO2, -OR7, -SR7, -NR7R7, -NR7C (O) OR7, -NR7C (O) R7, C1-C10 alkyl, C1-10 alkenyl, alcoxiC1-10, C3-C10 aryl, C6- C14, C24 alkaryl-C7, C3-C13 heteroaryl, C4 alk-heteroaryl-C23, C1-C10 alkyl substituted C2-10-alkenyl, substituted C1-10 alkoxy substituted C3-C10 alkyl, alk-heteroaryl substituted C4-C23 and Q-Ar; wherein if W is a substituent group substituted or estasustituido conuno independently selected from the group consisting of -CN, -CO2R7, -C (O) R7, -C (O) NR7 R7, -OR7, -SR7, - NR7R7, NO2, -NR 7 C (O) R 7, -NR 7 C (O) OR7 and halogen up to per-halo; wherein each R7se independently selected from H, C1-C10 alkyl, C2-10-alkenyl, C3-C10 aryl, C6-C14 hetaryl C3-C13, alkaryl C7-C24 alk-heteroaryl C4-C23, alkyl C1- C10 to perhalosustituido, C2-10alkenyl to perhalosustituido, C3-10 cycloalkyl to perhalosustituido, C6-C14 aryl and hetaryl to perhalosustituido C3-C13 to perhalosustituido, wherein Q is -O-, - S-, -N (R7) -, - (CH2) -m, -C (O) -, -CH (OH) -, - (CH2) mO-, -NR 7 C (O) NR7R7 '-, - NR7 C (O) -, -C (O) NR7-, - (CH2) ms-, - (CH2) mN (R7) -, -O (CH2) m-, -CHXa, -CXa2-, -S- (CH2) m- and -N (R7) (CH2) m-, m = 1-3, and X a is halogen; and Ar is an aromatic 5-10 membered structure containing 0-2 members of the group consisting of nitrogen, oxygen and sulfur, which is unsubstituted or substituted by halogen up to per-halo and optionally substituted by Zn1, wherein n1 is 0 to 3 and each Z is independently selected from group consisting of -CN, -CO2R7, -C (O) NR7R7, -C (O) -NR 7, -COR7, -NO2, -OR7, -SR7, -NR7R7, -NR7C selected (O) OR7, -NR7C (O) R7, C1-C10 alkyl, C3-C10 cycloalkyl, C6-C14 aryl, hetaryl C3-C13, alkaryl C7-C24 alk-heteroaryl C4-C23, C1-C10 substituted alkyl, C3-C10 substituted alkaryl and substituted C7-C24 alk-heteroaryl substituted C4-C23; where the substituent Z is selected from the group consisting of -CN, -CO2R7, -C (O) NR7R7, -OR7, -SR7, -NO2, -NR7R7, -NR7C (O) R7, -NR7C (O) OR7, R3 ', R4' ', R5' each independently selected from H, C1-10 alkyl, optionally substituted by halogen, up to perhalo, C1-10 -alkoxy, optionally substituted by halogen, up to perhaloalkoxy, halogen; NO2 or NH2; R6 'is H, C1-10 alkyl, C1-10 alkoxy, -NHCOR1; -NR1 COR1; NO2; ** ** Fomula one of R4 '', R5 'or R6' can be -X-Y, or 2 substituents R4 '-R6' 'together may be adjacent an aryl or hetaryl ring with 5-12 atoms, optionally substituted with C1-10 alkyl, C1-10 alkoxy, C3-10 cycloalkyl, C2-10 alkenyl, C1-10 alkanoyl, C6-12 aryl, C5-12 hetaryl or C6-12 aralkyl; R1 is C1-10 alkyl optionally substituted by halogen, up to perhalo; X is-CH2-, -S-, -N (CH3) -, -NHC (O) -, -CH2-S-, -S-CH2-, -C (O) -, or -O-; and X is additionally a single bond where Y is pyridyl; Y is phenyl, pyridyl, naphthyl, pyridone, pyrazine, benzodioxane, benzopyridine, pyrimidine or benzothiazole, each optionally substituted by C1-10 alkyl, C1-10 alkoxy, halogen, OH, -SCH3 or NO2 or, where Y is phenyl, with ** ** formula or a pharmaceutically acceptable salt thereof.