Abstract: A beta-adrenergic blocking compound according to the present teachings include compounds having the following structural formula: wherein n is 0 or 1, or a pharmaceutically acceptable salt thereof.

Abstract: An ursolic acid derivative can have the following structural formula: The ursolic acid derivative exhibits potent selective calcium channel blocker activities and may be used to treat a disease or condition for which calcium channel regulation is useful.

Abstract: The sulindac derivatives are compounds of the formula: wherein R is one of twenty-five substituted or unsubstituted phenyl substituents; and pharmaceutically acceptable salts thereof. The sulindac derivatives are synthesized by refluxing sulindac hydrazide with appropriately substituted benzaldehydes in the presence of ethanol and catalytic amounts of glacial acetic acid. The sulindac derivatives may be used as active ingredients in pharmaceutical compositions for the treatment of inflammation or inflammatory diseases. The sulindac derivatives may also be used as analgesic and/or gastric sparing agents.

Abstract: The naphthyridinyl hydrazine derivatives as potent peripheral analgesic agents are (E)-2-(substituted benzylidene)-1-(2,7-dialkyl-1,8-naphthyridinyl) hydrazines that provide effective peripheral analgesic activity, as demonstrated using the mouse writhing test. The new target compounds include at least one compound that demonstrates higher potency in providing analgesic relief in mice (Protection (%)=81.44) compared to the reference drug acetyl salicylic acid (Protection (%)=78.47). These results demonstrated that the target compound exerts acute analgesic action, suggesting that it may represent an alternative in the development of new therapeutic strategies. Preferably, the (E)-2-(substituted benzylidene)-1-(2,7-dialkyl naphthyridinyl) hydrazine has the formula: wherein R1 and R2 are alkyl, R3 is hydrogen, and R4 is NO2.

Abstract: The naphthyridinyl hydrazine derivatives as potent peripheral analgesic agents are (E)-2-(substituted benzylidene)-1-(2,7-dialkyl-1,8-naphthyridinyl) hydrazines that provide effective peripheral analgesic activity, as demonstrated using the mouse writhing test. The new target compounds include at least one compound that demonstrates higher potency in providing analgesic relief in mice (Protection (%)=81.44) compared to the reference drug acetyl salicylic acid (Protection (%)=78.47). These results demonstrated that the target compound exerts acute analgesic action, suggesting that it may represent an alternative in the development of new therapeutic strategies. Preferably, the (E)-2-(substituted benzylidene)-1-(2,7-dialkyl naphthyridinyl) hydrazine has the formula: wherein R1 and R2 are alkyl, R3 is hydrogen, and R4 is NO2.

Abstract: The sulfonylurea derivatives of oleanolic acid include compounds replacing the 5-chloro-2-methoxybenzoic acid moiety found in glibenclamide with oleanolic acid. The resulting triterpenoidal sulfonylurea derivatives are compounds having the following formula: or a pharmaceutically acceptable salt thereof. The derivatives are synthesized by condensation of 3-oxo-Olean-12-en-28-oic acid with 4-(2-aminoethyl)benzenesulfonamide to form an intermediate product, followed by reaction with cyclohexyl isocyanate or 4-methylcyclohexyl isocyanate to give 3a or 3b, respectively. The sulfonylurea derivative compounds were screened for their oral hypoglycemic activity in vivo using the alloxan-induced diabetic mouse model and proved more potent than either glibenclamide or oleanolic acid.

Abstract: The pyrido[2,3-d]pyrimidine derivatives as anticancer agents include 5-(substituted-phenyl)-2-(3-methyl-5-oxo-2H-pyrazol-1(5H)-yl)-7-(pyridin-3-yl)pyrido[2,3-d]pyrimidin-4(3H)-one derivatives having the formula: where R is hydrogen; 2-halo, 3-halo, or 4-halo (Cl, Br, or F); 2-methoxy, 3-methoxy, or 4-methoxy (OCH3); 2-nitro, 3-nitro, or 4-nitro (NO2); 4-isopropyl, 4-methyl, or 4-cyano (CN); 2-hydroxy or 3-hydroxy (OH), 3-chloro and 5-chloro; 2-methoxy and 5-methoxy, 3-methoxy and 5-methoxy, or 3-methoxy and 4-methoxy; 3,4,5-trimethoxy; or 2-hydroxy and 4-hydroxy; or a pharmaceutically acceptable salt thereof. The derivatives may be useful in treating various cancers, including hepatic, colon, prostate, breast, and lung cancer.

Abstract: The abietic acid derivatives as anti-tumor agents are derivatives of abietic acid in which the hydroxyl entity (—OH) of the carboxyl entity is replaced by an electronegative substituent, which may be C6H5-O—, C6H5-S—, or C6H5-NH—, and a hydrogen atom on one of the rings is replaced by a hydroxyl (—OH) substituents, the derivatives having the formula: wherein X is O, S, or NH. The derivatives are formed by formation of an intermediate lactone from abietic acid, followed by reaction of the lactone with phenol, thiophenol, or aniline. All of the derivatives exhibited potent 5?-reductase inhibitor activity, both in vitro and in vivo, and anti-tumor activity with regard to two prostate cancer cell lines—LNCaP and PC-3. The intermediate lactones are also derivatives of abietic acid that exhibit anti-tumor activity.

Abstract: A dihydropyrimidinone derivative includes a compound having a chemical structure according to Formula 1: Z is selected from O, S and N; Y is N X is selected from O and S; and R represents aryl, substituted aryl, heteroaryl, or substituted heteroaryl, wherein the substituted aryl or substituted heteroaryl have one or more substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, hydroxyl, alkylthio, alkylamino, heteroaryl, aryloxy, haloaryloxy, arylthio, arylamino, and pharmaceutically acceptable salts thereof.

Abstract: A substituted pyrazole derivative includes a compound of the formula: or a pharmaceutically acceptable salt thereof.

Abstract: A pentacyclic triterpenoidal derivative can include 3,11-dioxo-24(phenyl)-urs-12-en-24-one (4), 24-norurs-12-en-24(phenyl)-3,11-dione (5), 3,11-dioxo-24(Phenyl)-urs-1,12-diene-24-one (6), or 24-nor-urs-1,12-diene-24(phenyl)-3,11-dione (7). The pentacyclic triterpenoidal derivative demonstrates highly potent 5-lipoxygenase inhibition activity.

Abstract: Oleanolic acid methyl ester derivatives demonstrate potent anti-diabetic activities. In in vitro anti-diabetic testing, the derivatives showed more potency regarding dipeptidyl peptidase-4 (DPP-IV) inhibitor activity, peroxisome proliferator-activated receptors (PPARs) agonist activity, and ?-Glucosidase inhibitors activity, as compared to reference standards oleanolic acid and acarbose. In in vivo oral hypoglycemic testing, both acute and sub-acute studies demonstrated that the derivatives had high potency and long duration of action compared to the reference standards pioglitazone, acarbose and oleanolic acid.

Abstract: The glycyrrhetic acid derivatives can include: The glycyrrhetic acid derivatives can be used to treat inflammation and/or ulcers.

Abstract: The substituted naphthyridinyl hydrazine compounds as anti-liver cancer agents are anti-liver cancer agents that inhibit proliferative pathways of cancer cells, thereby exhibiting potent in vitro and in vivo anticancer activity. The compounds have the formula: wherein R1 and R2 each are selected independently from hydrogen, mercapto, and C1-C5-alkyl, preferably methyl, ethyl, propyl, isopropyl or halogen; R3 and R4 each are selected independently from hydrogen, alkyl or halogen; and R5 is selected from substituted or unsubstituted aryl, more preferably from substituted phenyl, naphthyl, and substituted or unsubstituted heteroaryl, more preferably from furyl, pyrrolyl, thienyl, imidazolyl, thiadiazolyl, pyridinyl, pyridazinyl, pyrimidinyl, benzothiazolyl, oxadiazolyl or sugar moities. These agents exert their action through topoisomerase II inhibition.

Abstract: Cyclooxygenase inhibitors include compounds of the formula: where R represents phenyl, nitrophenyl, 2-nitrophenyl, 3-nitrophenyl, 4-nitrophenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 3,4-dimethoxyphenyl, 2-methoxyphenyl, 4-hydroxyphenyl, dimethylaminophenyl, 3-methoxyphenyl, 4-ethoxyphenyl, 2,4,5-trimethoxyphenyl, 3,4,5-trimethoxyphenyl, 2,4,6-trimethoxyphenyl, and 2,4-dimethoxyphenyl, 3-hydroxyphenyl, 4-dimethylaminophenyl, or 2,3,4-trimethoxyphenyl.

Abstract: The present invention relates to a compound of formula 1 and addition salts thereof, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as neuro-muscular blocker or skeletal muscle relaxant; wherein each symbol is as defined in the Specification.

Abstract: The present invention relates to a compound represented by formula 1 or an addition salt thereof, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as an hypnotic agent or anesthetic agent: wherein each symbol is as defined in the Specification.

Abstract: The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as hypnotic agent or anesthetic agent.

Abstract: The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as neuromuscular blocker or skeletal muscle relaxant.