{"id":10568,"date":"2022-10-26T02:53:05","date_gmt":"2022-10-25T18:53:05","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10568"},"modified":"2022-10-26T02:53:05","modified_gmt":"2022-10-25T18:53:05","slug":"higashino-takeo-et-al-published-their-patent-in-1992-cas-143803-93-4","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10568","title":{"rendered":"Higashino, Takeo et al. published their patent in 1992 |CAS: 143803-93-4"},"content":{"rendered":"<p>On May 6, 1992, Higashino, Takeo; Suzuki, Yukio; Sasahara, Takehiko; Saito, Tetsu; Mochizuki, Daisuke published a patent.<a href=\"https:\/\/www.ambeed.com\/products\/143803-93-4.html\">COA of Formula: C9H8N2O2<\/a> The title of the patent was Preparation of pyrazolo[1,5-a]pyridine-3-carboxylic acid as serotonin 3-receptor binding antagonists. And the patent contained the following:<\/p>\n<p>The title compounds (I; R1, R2 = H, alkyl; R3 = azabicyclo groups Q, Q1; Y = O, NH; Z = alkyl; n = 2, 3) or their salts, useful as antianxietics and antiemetics, especially for reducing nausea and vomiting due to side effects of an carcinostatic agent, were prepared, e.g., by amidation of pyrazolo[1,5-a]pyridinecarboxylic acids by azabicycloalkanamines. Thus, 7-methyl-3-pyrazolo[1,5-a]pyridinecarboxylic acid [J. Organic Chem. 33(5), 2062-4 (1968)] was refluxed in SOCl2 for 30 min., distilled, and the residue refluxed for 24 h with endo-8-methyl-8-azabicyclo[3.2.1]oct-3-yl-7-methylpyrazolo[1,5-a]pyridine-3-carboxamide (II). The latter in a 3H-quipazine binding assay in vitro had IC50 = 19.1 nM. II at 0.1 mg\/kg i.v. in beagles prevented vomiting following administration of 3 mg\/kg i.v. cisplatin. The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).<a href=\"https:\/\/www.ambeed.com\/products\/143803-93-4.html\">COA of Formula: C9H8N2O2<\/a><\/p>\n<p>The Article related to pyrazolopyridine preparation antiemetic antianxietic, nausea cisplatin prevention pyrazolopyridine preparation, vomiting cisplatin prevention pyrazolopyridine preparation and other aspects.<a href=\"https:\/\/www.ambeed.com\/products\/143803-93-4.html\">COA of Formula: C9H8N2O2<\/a><\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">Pyrazole &#8211; Wikipedia<\/a>,<br \/><a href=\"https:\/\/www.sciencedirect.com\/topics\/chemistry\/pyrazoles\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>The Article related to pyrazolopyridine preparation antiemetic antianxietic, nausea cisplatin prevention pyrazolopyridine preparation, vomiting cisplatin prevention pyrazolopyridine preparation and other aspects.<a href=\"https:\/\/www.ambeed.com\/products\/143803-93-4.html\">COA of Formula: C9H8N2O2<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[759,131],"tags":[128],"class_list":["post-10568","post","type-post","status-publish","format-standard","hentry","category-143803-93-4","category-pyrazoles-derivatives","tag-100-200"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Higashino, Takeo et al. published their patent in 1992 |CAS: 143803-93-4 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"On May 6, 1992, Higashino, Takeo; Suzuki, Yukio; Sasahara, Takehiko; Saito, Tetsu; Mochizuki, Daisuke published a patent.COA of Formula: C9H8N2O2 The title of the patent was Preparation of pyrazolo[1,5-a]pyridine-3-carboxylic acid as serotonin 3-receptor binding antagonists. 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