- Preparation method of pharmaceutical compound avanafil
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The invention discloses a preparation method of a pharmaceutical compound avanafil, and belongs to the technical field of synthesis of pharmaceutical compounds. The key point of the technical scheme of the invention is as follows: a synthesis route of the synthetic method of the pharmaceutical compound avanafil is shown in the specification. The synthetic method has the advantages that the yield is high, the cost is low, the method is economical and environmentally friendly and is suitable for industrialization, the product purity is high and the like, and the method is a synthetic method withindustrial production values.
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Paragraph 0014; 0043; 0050; 0053; 0054
(2019/02/10)
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- Method of preparing medical compound stendra
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The invention discloses a method of preparing a medical compound stendra and belongs to the technical field of medical compounds. The key point of the technical scheme is as follows: the synthetic route of the method of preparing the medical compound stendra is as follows: a formula as shown in the description. The method has the advantages of being high in yield, low in cost, economical and environment-friendly, suitable for industrialization, high in product impurity and the like, and is a synthetic method which has industrial production value.
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Paragraph 0014; 0031-0032; 0042-0043; 0053-0054
(2019/02/04)
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- The discovery of avanafil for the treatment of erectile dysfunction: A novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor
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Novel pyrimidine-5-carboxamide derivatives bearing a 3-chloro-4-methoxybenzylamino group at the 4-position were identified as potent and highly selective phosphodiesterase 5 inhibitors. Among them, we successfully found 10j (avanafil) which exhibited a potent relaxant effect on isolated rabbit cavernosum (EC30 = 2.1 nM) and a high isozyme selectivity.
- Sakamoto, Toshiaki,Koga, Yuichi,Hikota, Masataka,Matsuki, Kenji,Murakami, Michino,Kikkawa, Kohei,Fujishige, Kotomi,Kotera, Jun,Omori, Kenji,Morimoto, Hiroshi,Yamada, Koichiro
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p. 5460 - 5465
(2015/01/08)
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- Cyclic compounds
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1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, wherein X is ═CH— or ═N—, Y is —NH—, —NR4—, —S—, —O—, —CH═N—, —N═CH—, —N═N—, —CH═CH—, etc., R1 is a lower alkoxy group, an amino group, a heterocyclic ring containing N atom(s), or a hydroxy group substituted by a heterocyclic ring containing N atom(s) (each of which is optionally substituted), R2 is a lower alkylamino group which is optionally substituted by an aryl group, a lower alkoxy group which is optionally substituted by an aryl group, a lower alkoxy group substituted by an aromatic heterocyclic ring containing N atom(s), R3 is an aryl group, a heterocyclic ring containing N atom(s), a lower alkyl group, a lower alkoxy group, a cyclo lower alkoxy group, a hydroxy group substituted by a heterocyclic ring containing N atom(s), or an amino group (each of which is optionally substituted), and R3 and a substituent in Y may be combined to form a lactone ring. The compound of the present invention has excellent selective PDE V inhibitory activity and therefore, is useful as a therapeutic or prophylactic drug for treating various diseases due to functional disorders on cGMP-signaling.
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