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公开(公告)号：US10568968B2
公开(公告)日：2020-02-25
申请号：US15803516
申请日：2017-11-03
发明人： Martin Oft , Catherine Sheppard , John Brian Mumm , Lingling Wu
IPC分类号： A61K47/60 , A61K38/20 , C07K16/30 , A61K45/06 , A61K39/395
摘要： Provided are methods of treatment for tumors. In particular, methods are provided for use of a chemically modified IL-10 to treat tumors.
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公开(公告)号：US09181262B2
公开(公告)日：2015-11-10
申请号：US14507001
申请日：2014-10-06
发明人： Itzia Z. Arroyo , Davida Krueger , Ping Chen , Aaron J. Moment , Tesfaye Biftu , Faye Sheen , Yanfeng Zhang
IPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/4985 , A61K31/513
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/4985 , A61K31/513 , C07B2200/13 , Y02P20/55
摘要： Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
摘要翻译： （2R，3S，5R）-2-（2,5-二氟苯基）-5- [2-（甲基磺酰基）-2,6-二氢吡咯并[3,4-c]吡唑-5（4H） - 吡啶-3-基]四氢-2H-吡喃-3-胺是二肽基肽酶-IV的有效抑制剂，可用于治疗非胰岛素依赖型（2型）糖尿病。 本发明还涉及含有这些新型形式的药物组合物，制备这些形式的方法及其药物组合物及其用于治疗2型糖尿病的用途。
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公开(公告)号：US08895603B2
公开(公告)日：2014-11-25
申请号：US14118998
申请日：2012-06-25
申请人： Itzia Arroyo , Davida Krueger , Ping Chen , Aaron Moment , Tesfaye Biftu , Faye Sheen , Yanfeng Zhang
发明人： Itzia Arroyo , Davida Krueger , Ping Chen , Aaron Moment , Tesfaye Biftu , Faye Sheen , Yanfeng Zhang
IPC分类号： A61K31/4162 , C07D231/00 , C07D487/04 , A61K31/4439 , A61K31/4985 , A61K31/513
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/4985 , A61K31/513 , C07B2200/13 , Y02P20/55
摘要： Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
摘要翻译： （2R，3S，5R）-2-（2,5-二氟苯基）-5- [2-（甲基磺酰基）-2,6-二氢吡咯并[3,4-c]吡唑-5（4H） - 吡啶-3-基]四氢-2H-吡喃-3-胺是二肽基肽酶-IV的有效抑制剂，可用于治疗非胰岛素依赖型（2型）糖尿病。 本发明还涉及含有这些新型形式的药物组合物，制备这些形式的方法及其药物组合物及其用于治疗2型糖尿病的用途。
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4.发明授权(4, 5, 6, 7-tetrahydro-1-H-indol-7-yl) acetic acid derivatives for treatment of Alzheimer's disease 失效（4,5,6,7-四氢-1H-吲哚-7-基）乙酸衍生物，用于治疗阿尔茨海默病公开(公告)号：US07728022B2
公开(公告)日：2010-06-01
申请号：US11587779
申请日：2005-05-06
申请人： Michela Bettati , Ian Churcher , Victoria Alexandra Doughty , Timothy Harrison , Emmanuela Nizi , Adam Smith
发明人： Michela Bettati , Ian Churcher , Victoria Alexandra Doughty , Timothy Harrison , Emmanuela Nizi , Adam Smith
IPC分类号： A61K31/41 , A61K31/403 , C07D403/06 , C07D209/12
CPC分类号： C07D209/08 , C07D209/02 , C07D209/10 , C07D231/56 , C07D409/04
摘要： Compounds of formula I: are disclosed. The compounds are useful in treating or preventing diseases associated with deposition of Aβ in the brain.
摘要翻译： 公开了式I化合物。 该化合物可用于治疗或预防与A＆Bgr沉积相关的疾病; 在大脑中
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公开(公告)号：US07468393B2
公开(公告)日：2008-12-23
申请号：US11796389
申请日：2007-04-27
申请人： Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alan Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
发明人： Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alan Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
IPC分类号： A61K31/10 , C07C317/24 , C07C317/32
CPC分类号： C07C317/28 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/36 , C07C317/42 , C07C317/44 , C07D205/04 , C07D207/10 , C07D211/38 , C07D211/72 , C07D213/34 , C07D213/71 , C07D217/24 , C07D231/12 , C07D233/64 , C07D241/08 , C07D249/08 , C07D261/08 , C07D271/10 , C07D277/26 , C07D295/096 , C07D317/62 , C07D319/18
摘要： Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.
摘要翻译： 式I化合物是人5-HT 2A受体的有效和选择性拮抗剂，因此可用于治疗CNS的多种不利条件。
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6.发明授权Indazol-3-ones and analogues and derivatives thereof which modulate the function of the vanilloid-1 receptor (VR1) 失效吲哚-3-酮及其类似物和衍生物，其调节香草素-1受体（VR1）的功能公开(公告)号：US07449585B2
公开(公告)日：2008-11-11
申请号：US10579355
申请日：2004-11-12
IPC分类号： C07D231/56 , C07D471/02 , C07D487/00 , A61K31/415 , A61K31/44 , A61K241/36 , A61K31/495
CPC分类号： C07D231/56 , C07D401/04 , C07D471/04
摘要： Compounds of formula (I), which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
摘要翻译： 可用作治疗化合物的式（I）化合物，特别是用于治疗通过调节香草素-1受体（VR1）的功能而改善的疼痛和其它病症。
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7.发明授权公开(公告)号：US07411088B2
公开(公告)日：2008-08-12
申请号：US10589098
申请日：2005-02-16
申请人： Karel Marie Joseph Brands , Sarah Elizabeth Brewer , Antony John Davies , Ulf H. Dolling , Deborah Camille Hammond , David Ross Lieberman , Jeremy Peter Scott
发明人： Karel Marie Joseph Brands , Sarah Elizabeth Brewer , Antony John Davies , Ulf H. Dolling , Deborah Camille Hammond , David Ross Lieberman , Jeremy Peter Scott
IPC分类号： C07C315/00
CPC分类号： C07C57/62 , C07B2200/09 , C07C51/60 , C07C59/56 , C07C315/02 , C07C319/14 , C07C319/16 , C07C2601/14 , C07C2601/16 , C07C63/68 , C07C317/44 , C07C323/61
摘要： There is provided stereoselective route to a compound of formula I: wherein R represents H or an alkali metal, Ar1 represents 4-chlorophenyl and Ar2 represents 2,5-difluorophenyl.
摘要翻译： 提供了式I化合物的立体选择性途径：其中R表示H或碱金属，Ar 1表示4-氯苯基，Ar 2表示2,5-二氟苯基 。
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公开(公告)号：US07410964B2
公开(公告)日：2008-08-12
申请号：US10555034
申请日：2004-05-07
申请人： Kevin Dinnell , Karl Richard Gibson , Timothy Harrison , Richard Alexander Jelley , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Brian John Williams
发明人： Kevin Dinnell , Karl Richard Gibson , Timothy Harrison , Richard Alexander Jelley , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Brian John Williams
IPC分类号： C07D285/22 , A61K31/5415
CPC分类号： C07D279/02
摘要： Compounds of formula I: inhibit gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译： 式I化合物：抑制γ-分泌酶，因此可用于治疗或预防阿尔茨海默氏病。
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公开(公告)号：US07381725B2
公开(公告)日：2008-06-03
申请号：US10524006
申请日：2003-08-04
IPC分类号： A61K31/501 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D237/14 , C07D237/20 , A61P25/28
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D409/04 , C07D471/04
摘要： A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译： 一类由任选取代的杂芳环在4-位取代的哒嗪衍生物是GABA A受体的选择性配体，特别是对α2和/或α3和/或其α5亚基具有高亲和力，因此有益于 治疗和/或预防中枢神经系统的不良状况，包括焦虑，抽搐和认知障碍。
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公开(公告)号：US07365196B2
公开(公告)日：2008-04-29
申请号：US10239233
申请日：2001-03-15
申请人： Patrice Charles Belanger , Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Edward Giles McIver , Alan John Nadin , Joseph George Neduvelil , Mark Steven Shearman , Adrian Leonard Smith , Timothy Jason Sparey , Graeme Irvine Stevenson , Martin Richard Teall
发明人： Patrice Charles Belanger , Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Edward Giles McIver , Alan John Nadin , Joseph George Neduvelil , Mark Steven Shearman , Adrian Leonard Smith , Timothy Jason Sparey , Graeme Irvine Stevenson , Martin Richard Teall
IPC分类号： C07D413/14 , C07D413/12 , C07D213/71 , C07D213/52 , C07D333/34 , C07D409/14 , C07D409/12 , C07D249/12 , C07D233/84 , C07D207/48 , C07D277/16 , C07D307/64 , A61P25/28
CPC分类号： C07D213/30 , A61K31/18 , A61K31/40 , C07C311/07 , C07C311/09 , C07C311/11 , C07C311/14 , C07C311/20 , C07C311/24 , C07C323/67 , C07C2601/08 , C07C2601/14 , C07C2602/44 , C07C2602/46 , C07C2603/72 , C07C2603/78 , C07D207/36 , C07D211/14 , C07D211/18 , C07D213/71 , C07D213/81 , C07D215/12 , C07D223/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D271/107 , C07D277/36 , C07D285/14 , C07D285/16 , C07D295/088 , C07D295/135 , C07D295/26 , C07D307/64 , C07D307/81 , C07D319/18 , C07D333/34 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10 , C07D513/10
摘要： A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
摘要翻译： 公开了一类化合物，其包含磺酰氨基取代的桥连双环烷基结构。 这些化合物是γ-分泌酶的抑制剂，因此可用于治疗和/或预防阿尔茨海默氏病。
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