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1. 发明申请

US20140162942A1 INHIBITION OF CYP3A DRUG METABOLISM 审中-公开
标题翻译： CYP3A药物代谢的抑制作用
公开(公告)号：US20140162942A1
公开(公告)日：2014-06-12
申请号：US13812221
申请日：2011-07-25
申请人： Anima Ghosal , Samir Gupta , Narendra Kishnani , Claudia Kasserra , Edward O'Mara
发明人： Anima Ghosal , Samir Gupta , Narendra Kishnani , Claudia Kasserra , Edward O'Mara
IPC分类号： A61K38/06 , A61K45/06
CPC分类号： A61K38/06 , A61K38/07 , A61K45/06 , A61K2300/00
摘要： The present invention provides methods, pharmaceutical compositions, medicaments, and pharmaceutical kits that employ the use of boceprevir as a CYP3A4/5 inhibitor to improve the pharmacokinetics of therapeutic compounds metabolized by cytochrome P450 3A4/5 (CYP3A4/5) enzymes.
摘要翻译：本发明提供使用波普瑞韦作为CYP3A4 / 5抑制剂来改善由细胞色素P450 3A4 / 5（CYP3A4 / 5）酶代谢的治疗性化合物的药代动力学的方法，药物组合物，药物和药物试剂盒。

2. 发明申请

US20050215534A9 3-Nitrogen-6, 7-dioxygen steroids and uses related thereto 失效
标题翻译： 3-氮-6,7-二氧类固醇及其相关用途
公开(公告)号：US20050215534A9
公开(公告)日：2005-09-29
申请号：US10624946
申请日：2003-07-21
申请人： Jeffery Raymond , Claudia Kasserra , Yaping Shen
发明人： Jeffery Raymond , Claudia Kasserra , Yaping Shen
IPC分类号： A61K31/56 , A61K31/566 , A61K31/57 , A61K31/58 , A61P9/06 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/02 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/08 , A61P43/00 , C07J41/00 , C07J43/00 , C07J71/00
CPC分类号： C07J41/00 , C07J41/0005 , C07J41/0011 , C07J43/00 , C07J71/0047 , C07J71/0063 , Y02P20/55
摘要： A compound of the formula and pharmaceutically acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein, independently at each occurrence: R1 and R2 are selected from hydrogen, oxygen so as to form nitro or oxime, amino, sulfate, and sulfonic acid, and organic groups having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen, phosphorous, silicon, and sulfur, where R1 and R2 may, together with the N to which they are both bonded, form a heterocyclic structure that may be part of an organic group having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen and silicon, and where R1 may be a 2, or 3 atom chain to numeral 2 so that —N—R1— forms part of a fused bicyclic structure to ring A; R3 and R4 are selected from direct bonds to 6 and 7 respectively so as to form carbonyl groups, hydrogen, or a protecting group such that R3 and/or R4 is part of hydroxyl or carbonyl protecting group; numerals 1 through 17 each represent a carbon having substitution as described. The compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias.
摘要翻译： R 1和R 2各自独立地是分别地或以混合物形式的式及其药学上可接受的盐，溶剂合物，立体异构体和前药的化合物，其中每次出现：R 1和选自氢，氧，以形成硝基或肟，氨基，硫酸根和磺酸，以及具有1-30个碳原子并且任选地含有1-6个选自氮，氧，磷，硅和硫的杂原子的有机基团，其中 R 1和R 2可以与它们都键合的N一起形成可以是具有1-30个碳的有机基团的一部分的杂环结构，以及任选地含有1-6个选自氮，氧和硅的杂原子，并且其中R 1可以是2或3个原子链至2，使得-NR 1 - 形成环A的稠合双环结构的一部分; R 3和R 4分别选自6和7的直接键，以便形成羰基，氢或保护基，使得R 3，和/或R 4是羟基或羰基保护基的一部分; 数字1至17各自表示如上所述具有取代的碳。化合物可以配制成药物组合物，并用于治疗和/或预防各种病症，包括炎症，哮喘，过敏性疾病，慢性阻塞性肺病，特应性皮炎，实体瘤，AIDS，局部缺血和心律失常。

3. 发明申请

US20070060553A1 3-Nitrogen-6,7-dioxygen steroids and uses related thereto 审中-公开
标题翻译： 3-氮-6,7-二氧类固醇及其相关用途
公开(公告)号：US20070060553A1
公开(公告)日：2007-03-15
申请号：US11496052
申请日：2006-07-28
申请人： Jeffery Raymond , Claudia Kasserra , Yaping Shen
发明人： Jeffery Raymond , Claudia Kasserra , Yaping Shen
IPC分类号： C07J43/00 , C07J41/00 , A61K31/58 , A61K31/56
CPC分类号： C07J41/00 , C07J41/0005 , C07J41/0011 , C07J43/00 , C07J71/0047 , C07J71/0063 , Y02P20/55
摘要： A compound of the formula and pharmaceutically acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein, independently at each occurrence: R1 and R2 are selected from hydrogen, oxygen so as to form nitro or oxime, amino, sulfate, and sulfonic acid, and organic groups having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen, phosphorous, silicon, and sulfur, where R1 and R2 may, together with the N to which they are both bonded, form a heterocyclic structure that may be part of an organic group having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen and silicon, and where R1 may be a 2, or 3 atom chain to numeral 2 so that —N—R1— forms part of a fused bicyclic structure to ring A; R3 and R4 are selected from direct bonds to 6 and 7 respectively so as to form carbonyl groups, hydrogen, or a protecting group such that R3 and/or R4 is part of hydroxyl or carbonyl protecting group; numerals 1 through 17 each represent a carbon having substitution as described. The compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias.
摘要翻译： R 1和R 2各自独立地是分别地或以混合物形式的式及其药学上可接受的盐，溶剂合物，立体异构体和前药的化合物，其中每次出现：R 1和选自氢，氧，以形成硝基或肟，氨基，硫酸根和磺酸，以及具有1-30个碳原子并且任选地含有1-6个选自氮，氧，磷，硅和硫的杂原子的有机基团，其中 R 1和R 2可以与它们都键合的N一起形成可以是具有1-30个碳的有机基团的一部分的杂环结构，以及任选地含有1-6个选自氮，氧和硅的杂原子，并且其中R 1可以是2或3个原子链至2，使得-NR 1 - 形成环A的稠合双环结构的一部分; R 3和R 4分别选自6和7的直接键，以便形成羰基，氢或保护基，使得R 3，和/或R 4是羟基或羰基保护基的一部分; 数字1至17各自表示如上所述具有取代的碳。化合物可以配制成药物组合物，并用于治疗和/或预防各种病症，包括炎症，哮喘，过敏性疾病，慢性阻塞性肺病，特应性皮炎，实体瘤，AIDS，局部缺血和心律失常。

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