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11. 发明授权

US07112580B2 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：US07112580B2
公开(公告)日：2006-09-26
申请号：US10624946
申请日：2003-07-21
申请人： Jeffery R Raymond , Claudia E Kasserra , Yaping Shen
发明人： Jeffery R Raymond , Claudia E Kasserra , Yaping Shen
IPC分类号： A61K31/56 , A61K31/58 , C07J41/00 , 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 R groups are as defined by the present specification. 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：下式的化合物及其药学上可接受的盐，溶剂合物，立体异构体和前药，其分离或混合，其中R基团如本说明书所定义。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。

12. 发明申请

US20050004086A1 Indene derivatives as pharmaceutical agents 有权
标题翻译：茚衍生物作为药剂
公开(公告)号：US20050004086A1
公开(公告)日：2005-01-06
申请号：US10825084
申请日：2004-04-15
申请人： Jeffery Raymond , Kang Han , Yuanlin Zhou , Yuehua He , Bradley Noren , James Yee
发明人： Jeffery Raymond , Kang Han , Yuanlin Zhou , Yuehua He , Bradley Noren , James Yee
IPC分类号： C07C35/21 , C07C35/32 , C07C69/013 , C07C69/03 , C07C311/04 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/74 , C07D233/54 , C07D233/56 , C07D295/096 , C07D307/66 , C07D317/66 , A61K31/56 , A61K31/155 , A61K31/18 , A61K31/19 , A61K31/40 , A61K31/44
CPC分类号： C07C35/32 , C07C35/14 , C07C35/21 , C07C51/083 , C07C51/347 , C07C62/34 , C07C69/013 , C07C213/00 , C07C213/08 , C07C215/42 , C07C233/18 , C07C233/21 , C07C233/72 , C07C247/14 , C07C279/08 , C07C311/04 , C07C315/00 , C07C2601/14 , C07C2602/08 , C07C2602/24 , C07D207/335 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/74 , C07D233/54 , C07D233/64 , C07D295/096 , C07D307/66 , C07D317/66 , C07D317/70 , Y10S514/825 , Y10S514/826 , Y10S514/863
摘要： Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
摘要翻译：式（Ia）化合物：其中R 1，R 2，R 3，R 4a，R 4b，R 5和R 6在本文中定义，以及其它茚衍生物在本文中公开。还公开了含有化合物的药物组合物和使用该化合物的方法。

13. 发明申请

US20040138186A1 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：US20040138186A1
公开(公告)日：2004-07-15
申请号：US10624946
申请日：2003-07-21
申请人： Inflazyme Pharmaceuticals Ltd.
发明人： Jeffery R. Raymond , Claudia E. Kasserra , Yaping Shen
IPC分类号： A61K031/56 , C07J041/00
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 1 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 nullNnullR1null 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：分离或混合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，其中独立地在每次出现时：R 1和R 2选自氢，氧，以便形成硝基或肟，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一起形成杂环结构，其可以是具有1-30个碳的有机基团的一部分，并且任选地含有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个到数字2的原子链，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，以形成羰基，氢或保护基，使得R 3和/或R 4是羟基的一部分或羰基保护基; 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。

14. 发明申请

US20080051382A1 Crystalline Forms of 3-Beta-Amino 17-Methylene Androstane-6-Alpha 7-Beta-Diol Hydrochloride 审中-公开
标题翻译： 3-β-氨基17-亚甲基雄甾烷-6-α7-β-二醇盐酸盐的结晶形式
公开(公告)号：US20080051382A1
公开(公告)日：2008-02-28
申请号：US10575689
申请日：2004-10-20
申请人： Colette Colladant , Denis Prat , Pascal Billot , Alexandre Giuliani , Hagit Elnaleh , Marc-Antoine Perrin
发明人： Colette Colladant , Denis Prat , Pascal Billot , Alexandre Giuliani , Hagit Elnaleh , Marc-Antoine Perrin
IPC分类号： A61K31/565 , A61P29/00 , C07J53/00
CPC分类号： C07J53/00
摘要： The invention relates to novel crystalline forms of 3-beta-amino-17-methylene-androstane-6-alpha,7-beta-diol hydrochloride, referred to as form A, form B and form C, a method for preparing same, the use thereof as a drug, and pharmaceutical compositions containing same.
摘要翻译：本发明涉及3-β-氨基-17-亚甲基 - 雄甾烷-6-α，7-β-二醇盐酸盐，称为A型，B型和C型的新结晶形式，其制备方法，作为药物的用途，以及含有它们的药物组合物。

15. 发明申请

US20070208181A1 BENZYLATED PDE4 INHIBITORS 失效
标题翻译：苄基PDE4抑制剂
公开(公告)号：US20070208181A1
公开(公告)日：2007-09-06
申请号：US11683534
申请日：2007-03-08
申请人： Ronald Lauener , David Burgoyne , Patrick Rebstein , Lloyd Mackenzie , Yuanlin Zhou , Yaping Shen
发明人： Ronald Lauener , David Burgoyne , Patrick Rebstein , Lloyd Mackenzie , Yuanlin Zhou , Yaping Shen
IPC分类号： C07D207/24
CPC分类号： C07D207/26 , C07C255/46 , C07C271/60 , C07D213/75 , C07D233/32 , C07D239/10 , C07D473/04 , C07D473/06
摘要： The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.
摘要翻译：本发明涉及一种减少PDE抑制剂的致吐作用的方法，更具体地涉及具有很少或不具有致吐性副作用的具有PDE4抑制活性的化合物，以及包括用于制备这些化合物的苄基化的化学方法。苄基可以连接到PDE4抑制剂的碳原子或氮原子上。合适的苄基化学方法是从PDE4抑制剂，优选用碱提取氢，然后使得到的亲核PDE4抑制剂与苄化试剂如苄基溴或其衍生物反应。

16. 发明申请

US20040157814A1 6, 7-Oxygenated steroids and uses related thereto 失效
标题翻译： 6，7-氧化类固醇及其相关用途
公开(公告)号：US20040157814A1
公开(公告)日：2004-08-12
申请号：US10703153
申请日：2003-11-06
申请人： Inflazyme Pharmaceuticals Ltd. , The University of British Columbia , The University of Alberta
发明人： David L. Burgoyne , Yaping Shen , John M. Langlands , Christine Rogers , Joseph H.L. Chau , Edward Piers , Hassan Salari
IPC分类号： C07J017/00 , A61K031/585 , A61K031/56 , C07J003/00
CPC分类号： C07J9/00 , C07J1/0007 , C07J1/0011 , C07J1/0022 , C07J3/00 , C07J7/002 , C07J13/005 , C07J13/007 , C07J17/00 , C07J21/008 , C07J31/006 , C07J41/0016 , C07J51/00 , C07J71/001 , C07J71/0026 , Y02P20/55 , Y10S514/825 , Y10S514/826
摘要： Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6null and 7null oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6null and 7null oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and null-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.
摘要翻译：公开了在类固醇核上具有各种氧取代的类固醇化合物。存在于许多类固醇化合物上的具体功能是在6和7位都是氧取代。因此，某些类固醇在C6和C7具有氧取代，并且一些具有特异性立体化学例如6α和7beta氧取代，以及α氢在5位，除了具有6alpha和7beta氧替代。还公开了具有3,4-环氧官能团的类固醇。此外，公开了具有C17吡喃和δ-内酯官能团的类固醇，其具有类固醇核的C6和C7或C15的氧取代。

17. 发明授权

US6046185A 6,7-oxygenated steroids and uses related thereto 失效
标题翻译： 6,7-氧合类固醇及其相关用途
公开(公告)号：US6046185A
公开(公告)日：2000-04-04
申请号：US893575
申请日：1997-07-10
申请人： David L. Burgoyne , Yaping Shen , John M. Langlands , Christine Rogers , Joseph H.-L. Chau , Edward Piers , Hassan Salari
发明人： David L. Burgoyne , Yaping Shen , John M. Langlands , Christine Rogers , Joseph H.-L. Chau , Edward Piers , Hassan Salari
IPC分类号： A61K31/56 , C07J1/00 , C07J3/00 , C07J7/00 , C07J9/00 , C07J13/00 , C07J17/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J51/00 , C07J71/00
CPC分类号： C07J9/00 , C07J1/0007 , C07J1/0011 , C07J1/0022 , C07J13/005 , C07J13/007 , C07J17/00 , C07J21/008 , C07J3/00 , C07J31/006 , C07J41/0016 , C07J51/00 , C07J7/002 , C07J71/001 , C07J71/0026 , Y02P20/55 , Y10S514/825 , Y10S514/826
摘要： Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6.alpha. and 7.beta. oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6.alpha. and 7.beta. oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and .delta.-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.
摘要翻译：公开了在类固醇核上具有各种氧取代的类固醇化合物。存在于许多类固醇化合物上的具体功能是位置6和7两者的氧取代。因此，某些类固醇在C6和C7具有氧取代，并且一些具有特异性立体化学例如6α和7β氧取代，除了具有6个α和7个β氧取代之外，在5位的α氢。还公开了具有3,4-环氧官能团的类固醇。此外，公开了具有C17吡喃和δ-内酯官能团的类固醇，其具有类固醇核的C6和C7或C15的氧取代。

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