Abstract: The present invention provides two new microorganism strains of Saccharothrix, designated as YS-44442 and YS-45494, a process of producing pravastatin using the strains, and an improved process for isolation of (HMG)-CoA reductase inhibitors.

Abstract: The present invention synthesizes a series of novel indole analogs of 1-benzyl-3-(5?-hydroxymethyl-2?-furyl)indazole (YC-1), and their anti-platelet activity.

Abstract: The present invention provides pharmaceutically acceptable salts having local anesthetic and anti-inflammatory activities. The preferred pharmaceutically acceptable salt is a diclofenac salt of lidocaine. Diclofenac is a non-steroidal anti-inflammatory drug (“NSAID”). Lidocaine is a local anesthetic. Other NSAID (except the salicylic acid derivatives of NSAID) can be used to replace diclofenac and/or other local anesthetics can be used to replace lidocaine. The pharmaceutically acceptable salts are crystalline compounds, which are distinctively different from either the NSAID alone or the local anesthetic alone, as indicated by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), High Performance Liquid Chromatography (HPLC) and Fourier-Transformed Infrared Spectroscopy (FTIR) analyses.

Abstract: A method for treating an angiogenesis-related disorder. The method includes administrating to a subject in need thereof an effective amount of a compound of the formula: Each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR?, (CH2)mOR, (CH2)mSR, (CH2)mNRR?, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH?NOR, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R?, independently, is H or C1˜C6 alkyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.

Abstract: This invention features a method for enhancing bone growth or inhibiting bone resportion. The method includes administering to a subject in need thereof a compound of the following formula: A is H, R, or each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is H, halogen, R, C(O)OH, C(O)OR, C(O)SH, C(O)SR, C(O)NH2, C(O)NHR, C(O)NRR?, ROH, ROR?, RSH, RSR?, NHR, NRR?, RNHR?, or RNR?R?; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are ORO; wherein each of R, R?, and R?, independently is C1˜C6 alkyl; and n is 1, 2, or 3.

Abstract: The present invention provides a topical formulation containing NSAID, particularly diclofenac. The topical formulation is particularly useful for alleviating pain/inflammation associated with infection caused by herpes virus, especially herpes simplex virus (HSV) and varicella-zoster virus (VZV). Similar relief can be achieved where diclofenac is replaced with another non-steroidal anti-inflammatory drug (NSAID), which includes, without limitation, etodolac, ketorolac, bromfenac, diflunisal, ibuprofen, fenoprofen, ketoprofen, naproxen, suprofen, meclofenamate, mefenamic acid, piroxicam, meloxicam, indomethacin, sulindac, phenylbutazone, oxyphenbutazone, and tolmetin. The topical formulation is further characterized by its fast relief on pain and/or inflammation associated with infection caused by herpes virus, i.e., a complete relief in no more than seven (7) days after the application of the topical formulation on skins of patients.

Abstract: The present invention provides an injectable pharmaceutical composition containing, as an active ingredient, paclitaxel, an anti-cancer agent. The injectable pharmaceutical composition comprises an effective amount of paclitaxel, which is dissolved in polyoxyethylated castor oil, alcohol, and an injectable aqueous solution. A sufficient amount of CO2 is added to stabilize paclitaxel in the injectable pharmaceutical composition to make the injectable pharmaceutical composition to a pH about 5.0.

Abstract: Novel compounds of 2-(substituted arylmethyl)-3-(substituted phenyl)-2H-indazoles and 1-(substituted arylmethyl)-3-(substituted phenyl)-1H-indazoles are synthesized, and useful as anti-angiogenic agents.

Abstract: The present invention synthesizes a series of novel indole analogs of 1-benzyl-3-(5?-hydroxymethyl-2?-furyl)indazole (YC-1), and their anti-platelet activity.

Abstract: A fused pyrazolyl compound of the following formula: wherein A, Ar1, Ar2, R1, R2, R3, and R4, are as defined herein. Also disclosed is a pharmaceutical composition containing an effective amount of the above-described fused pyrazolyl compound.

Abstract: A method for preferentially inhibiting release of pro-inflammatory cytokines over release of anti-inflammatory cytokines using a fused pyrazolyl compound of formula (I): A is R or in which R is H, alkyl, aryl, cyclyl, heteroaryl, or heterocyclyl; each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is R?, nitro, halogen, —C(O)—OR?, —C(O)—SR?, —C(O)—NR?R?, —(CH2)mOR?, —(CH2)mSR?, —(CH2)mNR?R?, —(CH2)mCN, —(CH2)mC(O)—OR?, —(CH2)mC(O)H, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are —O(CH2)nO—, in which each of R? and R?, independently, is H, alkyl, cyclyl, aryl, heteroaryl, heterocyclyl; and m is 0, 1, 2, 3, 4, 5, or 6; and n is 1, 2, or 3. This invention also covers a method of inhibiting activity of NF-?B with such a compound.

Abstract: This invention relates to a method for treating cancer including administrating to a subject in need thereof an effective amount of a compound of the formula: wherein, A is H or each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR?, (CH2)mOR, (CH2)mSR, (CH2)mNRR?, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH?NOR, (CH2)mC(O)N(OR)R?, N(OR)R?, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R?, independently, is H or C1˜C6 alkyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.

Abstract: The present invention features a method for treating sepsis. The method includes administrating to a subject in need thereof an effective amount of a fused pyrazolyl compound of formula (I): A is H, C1˜C6 alkyl, or in which n is 0, 1, 2, or 3; each of Ar1, Ar2, and Ar3, independently, is phenyl, pyridinyl, thienyl, furyl, or pyrrolyl; and each of R1, R2, R3, R4, R5, and R6, independently, is XYZ; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)1-6O; in which X is a bond or C1˜C6 alkylene, Y is a bond, O, S, OC(O), OC(O)(CH2)1-6C(O)O, C(O)O, C(O)S, C(O)NH, C(O)NC1˜C6 alkyl, NH, or NC1˜C6 alkyl, and Z is H, halogen, CN, NO2, or C1˜C6 alkyl; and provided that one of R3 and R4 is not H.

Abstract: The present invention features a method for treating sepsis. The method includes administrating to a subject in need thereof an effective amount of a fused pyrazolyl compound of formula (I): A is H, C1˜C6 alkyl, or in which n is 0, 1, 2, or 3; each of Ar1, Ar2, and Ar3, independently, is phenyl, pyridinyl, thienyl, furyl, or pyrrolyl; and each of R1, R2, R3, R4, R5, and R6, independently, is XYZ; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)1-6O; in which X is a bond or C1˜C6 alkylene, Y is a bond, O, S, OC(O), OC(O)(CH2)1-6C(O)O, C(O)O, C(O)S, C(O)NH, C(O)NC1˜C6 alkyl, NH, or NC1˜C6 alkyl, and Z is H, halogen, CN, NO2, or C1˜C6 alkyl; and provided that one of R3 and R4 is not H.

Abstract: This invention features a method for enhancing bone growth or inhibiting bone resportion. The method includes administering to a subject in need thereof a compound of the following formula: A is H, R, or each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, or pyrrolyl; each of R1, R2, R3, R4, R5, and R6, independently, is H, halogen, R, C(O)OH, C(O)OR, C(O)SH, C(O)SR, C(O)NH2, C(O)NHR, C(O)NRR?, ROH, ROR?, RSH, RSR?, NHR, NRR?, RNHR?, or RNR?R?; or R1 and R2 together, R3 and R4 together, or R5 and R6 together are ORO; wherein each of R, R?, and R?, independently is C1˜C6 alkyl; and n is 1, 2, or 3.

Abstract: The present invention provides oral pharmaceutical compositions for acetic acid class of non-steroidal anti-inflammatory drug (NSAID), particularly ketorolac. The pharmaceutical composition contains a core, a drug layer (which comprises the drug, a binder, and a disintegrant), a protecting layer, and an enteric coating layer. The oral pharmaceutical compositons are particularly useful for treating patients with moderate to acute pain. The present invention also provides a method for making the pharmaceutical compositions and a method for using the pharmaceutical compositions.

Abstract: A method for inhibiting cell proliferation, cell migration, or tube formation induced by an angiogenic factor. The method includes administrating to a subject in need thereof an effective amount of a compound of the formula: wherein A is H or in which n is 0, 1, 2, or 3; each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR?, (CH2)mOR, (CH2)mSR, (CH2)mNRR?, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH?NOR, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R?, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.

Abstract: Fused tri-heterocyclic compounds of formula: R1 is H or alkyl; R2 is H, alkyl, alkenyl, aryl, heteroaryl, cyclyl, or heterocyclyl; R3 and R4, independently, is H, alkyl, alkenyl, aryl, heteroaryl, cyclyl, heterocyclyl, or (CRaRb)mX(CRcRd)nY; in which X is a bond, O, S, or NRe; Y is alkoxy, aryloxy, heteroaryloxy, OC(O)Re, C(O)Re, N(ReRe?), NReC(O)Re?, S(O)2Re, or SRe; each of m and n, independently, is 1, 2, 3, 4, or 5; each of Ra, Rb, Rc, Rd, Re, and Re?, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; and R5 is H or halogen.

Abstract: The present invention provides two new microorganism strains of Saccharothrix, designated as YS-44442 and YS-45494, a process of producing pravastatin using the strains, and an improved process for isolation of (HMG)-CoA reductase inhibitors.

Abstract: The present invention provides a topical formulation containing NSAID, particularly diclofenac. The topical formulation is particularly useful for alleviating pain/inflammation associated with infection caused by herpes virus, especially herpes simplex virus (HSV) and varicella-zoster virus (VZV). Similar relief can be achieved where diclofenac is replaced with another non-steroidal anti-inflammatory drug (NSAID), which includes, without limitation, etodolac, ketorolac, bromfenac, diflunisal, ibuprofen, fenoprofen, ketoprofen, naproxen, suprofen, meclofenamate, mefenamic acid, piroxicam, meloxicam, indomethacin, sulindac, phenylbutazone, oxyphenbutazone, and tolmetin. The topical formulation is further characterized by its fast relief on pain and/or inflammation associated with infection caused by herpes virus, i.e., a complete relief in no more than seven (7) days after the application of the topical formulation on skins of patients.