Patent classifications
C07C255/42
HIGHLY WATER-SOLUBLE SALTS OF A SHORT ACTING PHENYLALKYLAMINE CALCIUM CHANNEL BLOCKER AND USES THEREOF
The present invention includes surprisingly water-soluble salts of a phenylalkylamine compound that are potent antagonists of L-type calcium channels. Aqueous solutions including salts of the instant invention are formulated for nasal administration and provide a novel therapeutic platform for the treatment of stable angina, migraine, and cardiac arrhythmia, such as paroxysmal supraventricular tachycardia.
HIGHLY WATER-SOLUBLE SALTS OF A SHORT ACTING PHENYLALKYLAMINE CALCIUM CHANNEL BLOCKER AND USES THEREOF
The present invention includes surprisingly water-soluble salts of a phenylalkylamine compound that are potent antagonists of L-type calcium channels. Aqueous solutions including salts of the instant invention are formulated for nasal administration and provide a novel therapeutic platform for the treatment of stable angina, migraine, and cardiac arrhythmia, such as paroxysmal supraventricular tachycardia.
Method for producing pyrrole compound
The present invention provides a production method of a 3-cyanopyrrole compound possibly useful as an intermediate for pharmaceutical products. A production method of compound (II) including subjecting compound (I) to a reduction reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. A production method of compound (III) including subjecting compound (I) to a reduction reaction followed by a cyclization reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. ##STR00001##
Method for producing pyrrole compound
The present invention provides a production method of a 3-cyanopyrrole compound possibly useful as an intermediate for pharmaceutical products. A production method of compound (II) including subjecting compound (I) to a reduction reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. A production method of compound (III) including subjecting compound (I) to a reduction reaction followed by a cyclization reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. ##STR00001##
Method of High-Pressure Purification of [F-18]FEONM
A method is provided to purify [F-18]FEONM under a high pressure. The synthesis processes of [F-18]FEONM are integrated. An isolation process of non-toxic radio-high performance liquid chromatography (radio-HPLC) is used to purify the crude product. The method integrates a convention [F-18]FDG synthesizer and a novel radio-HPLC system together in a heat chamber. After radiofluorinating the precursor, the reaction product is purified with an alumina solid-phase column in advance to obtain the crude product while fluorine-18 is removed. Then, diphenyl semipreparative HPLC column is used for a final purification. A non-toxic solvent is used for mobile-phase eluting to remove the unreacted precursor and the phase-transfer solvent. The radiofluorination has a reaction yield about 50 percent (%). The method has an uncorrected radiochemical yield of 10˜20%. Both of the radio-HPLC and the radio-thin layer chromatography (radio-TLC) have radiochemical purity higher than 95%.
Method of High-Pressure Purification of [F-18]FEONM
A method is provided to purify [F-18]FEONM under a high pressure. The synthesis processes of [F-18]FEONM are integrated. An isolation process of non-toxic radio-high performance liquid chromatography (radio-HPLC) is used to purify the crude product. The method integrates a convention [F-18]FDG synthesizer and a novel radio-HPLC system together in a heat chamber. After radiofluorinating the precursor, the reaction product is purified with an alumina solid-phase column in advance to obtain the crude product while fluorine-18 is removed. Then, diphenyl semipreparative HPLC column is used for a final purification. A non-toxic solvent is used for mobile-phase eluting to remove the unreacted precursor and the phase-transfer solvent. The radiofluorination has a reaction yield about 50 percent (%). The method has an uncorrected radiochemical yield of 10˜20%. Both of the radio-HPLC and the radio-thin layer chromatography (radio-TLC) have radiochemical purity higher than 95%.
Stilbene Derivatives for the Treatment of CNS and Other Disorders
The present application discloses stilbene derivative compounds and compositions, and methods for treating ocular diseases, neurological disorders and protein aggregation-related disorders in patients using the compounds and compositions as disclosed herein.
CHIRAL PLATINUM COMPLEX, METHOD FOR PREPARING THE SAME, AND METHOD FOR USING THE SAME
A chiral platinum complex having a chemical formula (I):
##STR00001##
A method for synthesizing the chiral platinum complex (I), includes: dissolving 0.700 g of Pt(DMSO).sub.2(NO.sub.3).sub.2 in 30 mL of dichloromethane as a solvent to yield a solution; adding 0.450 g of 1,4-(4R)-diphenyl-2-oxazolinyl benzene to the solution, and reflux a resulting mixture for reaction for 48 hrs, and stopping the reaction; filtrating reaction products; and adding dichloromethane and petroleum ether, and naturally volatilizing to yield a binuclear platinum complex single crystal. A method for condensation of benzophenone imine and trimethylsilitrile by using the chiral platinum complex as a catalyst. A method for treating cancer includes administering the chiral platinum complex to a patient in need thereof. The cancer includes: lung cancer (A549), nasopharyngeal carcinoma (KB), anti-drug-resistant nasopharyngeal carcinoma (KB-VIn), and human breast cancer (MCF-7).
CHIRAL PLATINUM COMPLEX, METHOD FOR PREPARING THE SAME, AND METHOD FOR USING THE SAME
A chiral platinum complex having a chemical formula (I):
##STR00001##
A method for synthesizing the chiral platinum complex (I), includes: dissolving 0.700 g of Pt(DMSO).sub.2(NO.sub.3).sub.2 in 30 mL of dichloromethane as a solvent to yield a solution; adding 0.450 g of 1,4-(4R)-diphenyl-2-oxazolinyl benzene to the solution, and reflux a resulting mixture for reaction for 48 hrs, and stopping the reaction; filtrating reaction products; and adding dichloromethane and petroleum ether, and naturally volatilizing to yield a binuclear platinum complex single crystal. A method for condensation of benzophenone imine and trimethylsilitrile by using the chiral platinum complex as a catalyst. A method for treating cancer includes administering the chiral platinum complex to a patient in need thereof. The cancer includes: lung cancer (A549), nasopharyngeal carcinoma (KB), anti-drug-resistant nasopharyngeal carcinoma (KB-VIn), and human breast cancer (MCF-7).
SHORT ACTING PHENYLALKYLAMINE CALCIUM CHANNEL BLOCKERS AND USES THEREOF
The present invention relates to the use of a pharmaceutically effective amount of an short-acting calcium channel blocking compound to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension before, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.