- Stable carteolol hydrochloride, preparation method thereof and eye medicine combination
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The invention relates to stable carteolol hydrochloride, a preparation method thereof and an eye medicine combination, in particular to a method for preparing carteolol hydrochloride. The method comprises the following steps of preparing 3-amino-2-cyclohexenone, tetrahydro-2,5(1H, 6H)-quinolinone, 5-hydroxy-3,4-dihydro-2(1H)-carbostyril and 5-(2,3-epoxypropoxy)-3,4-dihydro-2(1H)-carbostyril, and then the carteolol hydrochloride is obtained. Furthermore, the invention provides the carteolol hydrochloride crude medicine obtained according to the method, the eye medicine combination prepared by using the obtained carteolol hydrochloride as the crude medicine, and applications of the obtained carteolol hydrochloride to preparation of drugs for treating or preventing glaucoma or ocular hypertension. The method has excellent pharmaceutical characteristics, for example, the obtained crude medicine and a preparation has excellent stability.
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Paragraph 0120-0121; 0129; 0141; 0152; 0163; 0173-0174; 0185
(2017/12/06)
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- Compounds enhancing antitumor activity of other cytotoxic agents
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This invention relates to certain heterocyclic compounds and their pharmaceutically acceptable salts, which are useful for sensitizing multidrug-resistant tumor cells to anticancer agents and multidrug resistant forms of malaria, tuberculosis, leishmania and amoebic dysentery to chemotherapeutants. The compounds and their pharmaceutically acceptable salts are also inhibitors of the active drug transport capability of P-glycoprotein which is encoded by the human MDR1 gene, as well as of certain other related ATP-binding-cassette transporters from eukaryotic and prokaryotic organisms (e.g., pfmdr from Plasmodium falciprum, and murine mdr1 and mdr3 gene products).
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- Carbostyril compounds connected via an oxyalkyl group with a piperidine ring and having pharmaceutical utility
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Carbostyril derivatives of Formula I: STR1 wherein: m is 0, 1, or 2; n is 0, 1, or 2; R1 is hydrogen or lower alkyl; R2 is hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, aralkoxy, or acyloxy; R3 is hydrogen, halogen, lower alkyl, or lower alkoxy; R4 is hydrogen, hydroxy, lower alkyl, acyloxy, provided that when R4 is hydroxy or acyloxy, m and n are both 1; R5 is hydrogen or lower alkyl; and R6 is alkyl, hydroxyalkyl, alkoxyalkyl, or (dialkylamino)alkyl; and the pharmaceutically acceptable acid addition salts and N-oxides (at the carbostyril nitrogen) thereof, and compositions containing them, are useful in treating cardiovascular diseases, particularly arrhythmias. Methods of preparing intermediates, the compounds, their formulations and methods of treatment therewith are also disclosed.
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- Carbostyril derivatives, and antihistaminic agents containing the same
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Novel carbostyril derivatives and their salts having antihistaminic effects and are useful as antihistaminic agents, represented by the general formula (1), STR1 wherein R1 is a hydrogen atom, a lower alkenyl group, a lower alkynyl group or a l
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- CARBAMYLPIPERAZINE COMPOUNDS
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4-(3-Aryloxy-2-hydroxypropyl)piperazines bearing a carbamyl group in the 1-position are β-adrenergic blockers. A typical example is 1-carbamyl-4-{3-2-allyl-3-(2-carbethoxyaminoethyl)phenoxy!-2-hydroxypropyl} piperazine.
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- 3,4-DIHYDROCARBOSTYRIL DERIVATIVES AND PROCESS FOR PRODUCING THE SAME
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Novel compounds represented by the formula STR1 wherein R. sup.1, R. sup.2, and R' and R" are defined as hereinafter, having a blocking activity on β-adrenergic nerves, novel intermediates useful for synthesis thereof and processes for preparing the same are disclosed. When substitution is at the 5-position and R 1 and R 2 are hydrogen, R' and R" are not simultaneously hydrogen and a 1 to 4 carbon atom alkyl group in the claimed compound. "
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- 5-[2-Hydroxy-3-(3,4-dimethoxy phenethylamino)]-propoxy-3,4-dihydro carbostyril and pharmaceutically acceptable salts thereof
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A group of β-blockers represented by the formula STR1 wherein R is STR2 or STR3 and the physiologically compatible acid addition salts thereof. These β-blockers are β-adrenergic receptor blocking agents which are useful in the treatment of angina pectoris
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