-
1.
公开(公告)号:US20220259156A1
公开(公告)日:2022-08-18
申请号:US17681634
申请日:2022-02-25
申请人: Lupin Inc.
发明人: Richard John Holl , Kurt Nielsen , James Garegnani
IPC分类号: C07D233/94 , A61K31/4164 , A61K31/57 , A61K31/565
摘要: The present invention is related to deuterated secnidazole, a prodrug thereof, a hydrate thereof, a solvate thereof, a polymorph thereof, or a pharmaceutically acceptable salt thereof and its use for the treatment of bacterial vaginosis or trichomoniasis in a subject in need thereof. The present invention is also related to pharmaceutical compositions and methods and uses of treating bacterial vaginosis, trichomoniasis, amoebiasis, giardiasis, or a combination thereof.
-
公开(公告)号:US11000508B2
公开(公告)日:2021-05-11
申请号:US16901739
申请日:2020-06-15
申请人: LUPIN INC.
发明人: Helen S. Pentikis , David Palling , Carol J. Braun , Richard Holl
IPC分类号: A61K31/4164 , A61K45/06 , C07D233/94 , A61K31/565 , A61K31/567 , A61K9/00 , A61K9/16 , A61K9/50
摘要: Method of treating trichomoniasis in a subject in need thereof involving administering to the subject a therapeutically effective amount of secnidazole in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules having a volume-weighted particle size distribution within a microgranule population, wherein the volume-weighted particle size distribution as measured from a representative sample of the microgranule population comprises (a) at least 10% of the microgranule population having a volume-weighted particle size about no less than 470 micrometers; or (b) 50% of the microgranule population having a volume-weighted particle size between about no less than 640 micrometers and about no more than 810 micrometers; or (c) 90% of the microgranule population having a volume-weighted particle size about no more than 1170 micrometers; or (d) a combination thereof, which can include some or all of (a) through (c) above.
-
公开(公告)号:US20200022958A1
公开(公告)日:2020-01-23
申请号:US16586339
申请日:2019-09-27
发明人: Helen S. PENTIKIS , David PALLING , Carol J. BRAUN
IPC分类号: A61K31/4164 , A61K45/06 , C07D233/94 , A61K31/565 , A61K31/567 , A61K9/00 , A61K9/16 , A61K9/50
摘要: Embodiments are directed to a secnidazole formulations and the use of a secnidazole formulation for the treatment of bacterial vaginosis (BV).
-
公开(公告)号:US20180311214A1
公开(公告)日:2018-11-01
申请号:US15973939
申请日:2018-05-08
IPC分类号: A61K31/4164 , A61K9/00 , C07D233/94 , A61K45/06
CPC分类号: A61K31/4164 , A61K9/0014 , A61K45/06 , C07D233/94
摘要: This invention relates to the medical use of an antimicrobial agent, racemic Ornidazole, its (R) and (S) enantiomers, or pharmaceutically acceptable salts or esters thereof, and to methods of treatment which involve treating a subject with Ornidazole. The racemic (rac)-ornidazole, its enantiomers, or pharmaceutically acceptable salts or esters thereof, may be used in combination with other actives. The invention also relates to pharmaceutical formulations and compositions comprising (rac)-ornidazole, (R)-ornidazole, (S)-ornidazole, or pharmaceutically acceptable salts or esters thereof, and/or other actives as well as methods to stereoselectively manufacture the enantiomers.
-
公开(公告)号:US09233932B2
公开(公告)日:2016-01-12
申请号:US14477606
申请日:2014-09-04
申请人: NEKTAR THERAPEUTICS
IPC分类号: A61K31/41 , C07D233/94 , A61K47/48
CPC分类号: C07D233/94 , A61K47/48215 , A61K47/60
摘要: The invention provides (among other things) small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer.
摘要翻译: 本发明提供了(尤其是)通过共价连接水溶性低聚物化学改性的小分子药物。
-
公开(公告)号:US20130217740A1
公开(公告)日:2013-08-22
申请号:US13806719
申请日:2011-06-29
IPC分类号: C07D233/94
CPC分类号: C07D233/94 , A61K9/0014 , A61K31/4164
摘要: A compound of formula (I): is described, as well as enantiomers, pharmaceutically acceptable salts thereof, and uses thereof.
摘要翻译: 描述了式(I)的化合物,以及对映异构体,其药学上可接受的盐及其用途。
-
公开(公告)号:US20130197048A1
公开(公告)日:2013-08-01
申请号:US13807167
申请日:2011-06-29
IPC分类号: C07D233/94
CPC分类号: C07D233/94 , A61K9/0014 , A61K31/4164
摘要: A compound of formula (I): is described, as well as pharmaceutically acceptable salts thereof, and its use as a medicament.
摘要翻译: 描述了式(I)的化合物,以及其药学上可接受的盐及其作为药物的用途。
-
公开(公告)号:US20120219500A1
公开(公告)日:2012-08-30
申请号:US13504318
申请日:2010-10-25
申请人: Kazuhisa Sakurai , Akio Nagano
发明人: Kazuhisa Sakurai , Akio Nagano
IPC分类号: A61K51/04 , G01N33/569 , C07F5/00 , C07D233/91 , C07D233/95 , C07D233/94 , A61K49/00
CPC分类号: G01N33/52 , A61K51/0453 , A61K51/0455 , A61K51/0463 , C12Q1/025 , C12Q1/18 , G01N33/569 , G01N2333/205 , G01N2333/35
摘要: A diagnostic agent for infectious diseases which is capable of distinguishing among different kinds of bacterial species and which allows simple and non-invasive measurement and/or imaging in a short period of time is provided; and a screening method for a therapeutic agent for infectious diseases caused by microorganisms are provided.A diagnostic agent for infectious diseases caused by nitroimidazole susceptible microorganisms, containing an imidazole derivative or a fused imidazole derivative having at least one nitro group on an imidazole ring, or a labeled form thereof as an active ingredient is provided.
摘要翻译: 提供能够区分不同种类的细菌种类并且允许在短时间内进行简单和非侵入性测量和/或成像的感染性疾病诊断剂; 并提供了由微生物引起的感染性疾病的治疗剂的筛选方法。 提供了由咪唑衍生物或咪唑环上具有至少一个硝基的稠合咪唑衍生物或其标记形式作为有效成分的由硝基咪唑易感微生物引起的感染性疾病的诊断剂。
-
公开(公告)号:US20120202756A1
公开(公告)日:2012-08-09
申请号:US13253677
申请日:2011-10-05
IPC分类号: A61K31/7056 , C07H15/14 , C07C229/22 , C07C229/60 , C07D211/46 , C07D211/22 , C07D417/12 , C07D403/12 , A61K31/4164 , A61K31/225 , A61K31/24 , A61K31/445 , A61K31/554 , A61K31/506 , A61P31/04 , A61P9/06 , A61P25/28 , A61P19/02 , A61P25/24 , A61P35/00 , A61P19/10 , A61P31/12 , A61P3/10 , C07D233/94
CPC分类号: C07C279/26 , A61K31/4375 , C07C233/47 , C07C233/54 , C07C2601/14 , C07D211/32 , C07D211/46 , C07D233/94 , C07D285/135 , C07D307/20 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07D501/60 , C07F9/3873 , C07H15/04
摘要: The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.
摘要翻译: 本发明涉及各种药物的前药和含有这些前药的药物组合物。 还提供了用于使局部介导的(来自肠内腔)最小化与未发病药物相关的不良胃肠道事件和用上述前药增加血浆药物水平的维持的方法。 因此,本发明涉及广泛多样的药物(阿片样物质除外)的前体药物使用以使其短暂失活,并因此降低在给予母体化合物后通常明显的局部介导的不良胃肠道(GI)副作用。 此外,这样的前药可以赋予改善的药代动力学。
-
公开(公告)号:US5459144A
公开(公告)日:1995-10-17
申请号:US169809
申请日:1993-12-17
IPC分类号: C07D213/30 , C07D213/69 , C07D213/70 , C07D233/54 , C07D233/70 , C07D233/90 , C07D233/94 , C07D235/06 , C07D235/26 , C07D235/28 , C07D239/54 , C07D257/04 , C07D257/06 , C07D277/36 , C07D295/092 , C07D307/20 , C07D401/06 , C07D405/06 , C07D413/06 , C07D413/12 , C07D471/04 , C07D473/00 , C07D473/32 , C07D473/34 , C07D487/04 , C07D493/04 , C07D521/00 , A61K31/505 , A61K31/415 , A61K31/425 , A61K31/44 , C07D211/70 , C07D405/12 , C07D471/02 , C07D487/00
CPC分类号: C07D213/30 , C07D213/69 , C07D213/70 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/70 , C07D233/90 , C07D233/94 , C07D235/06 , C07D235/26 , C07D235/28 , C07D239/54 , C07D249/08 , C07D257/04 , C07D257/06 , C07D277/36 , C07D295/088 , C07D307/20 , C07D401/06 , C07D405/06 , C07D413/06 , C07D413/10 , C07D471/04 , C07D473/00 , C07D473/32 , C07D473/34 , C07D487/04 , C07D493/04
摘要: The invention relates to compounds of the formula ##STR1## wherein Z, X, Q, Y, W, and W' are as described herein. These compounds have antiviral activity, and certain of these compounds have antiinflammatory activity and are PAF inhibitors.
摘要翻译: 本发明涉及下式化合物:其中Z,X,Q,Y,W和W'如本文所述。 这些化合物具有抗病毒活性,并且这些化合物中的某些具有抗炎活性并且是PAF抑制剂。
-
-
-
-
-
-
-
-
-