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1. 发明申请

US20130053386A1 DIARYL ETHER DERIVATIVES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS 有权
标题翻译： DIARYL醚衍生物作为Notch SPARING GAMMA秘密酶抑制剂
公开(公告)号：US20130053386A1
公开(公告)日：2013-02-28
申请号：US13501628
申请日：2010-10-05
申请人： William Colby Brown , Richard W. Heidebrecht , Jason Brubaker , Christian Fischer , John T. Hendrix , Elizabeth H. Kelley , Rachel N. MacCoss , Joey L. Methot , Thomas Miller , Karin M. Otte , Phieng Siliphaivanh , Thomas Reger , Peter D. Williams , Catherine M. Wiscount
发明人： William Colby Brown , Richard W. Heidebrecht , Jason Brubaker , Christian Fischer , John T. Hendrix , Elizabeth H. Kelley , Rachel N. MacCoss , Joey L. Methot , Thomas Miller , Karin M. Otte , Phieng Siliphaivanh , Thomas Reger , Peter D. Williams , Catherine M. Wiscount
IPC分类号： C07D231/20 , C07D403/12 , A61K31/4155 , C07D401/12 , A61K31/4439 , A61K31/454 , A61K31/506 , C07D401/04 , C07D405/12 , C07D413/12 , A61K31/4245 , A61K31/422 , A61K31/5377 , C07D491/113 , A61K31/438 , A61K31/496 , C07D413/14 , A61P25/28 , A61K31/415
CPC分类号： C07D231/22 , C07D231/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/113
摘要： The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明包括一类新的二芳基醚衍生物，其抑制通过推定的γ-分泌酶处理APP，同时保留Notch信号通路，因此可用于治疗或预防阿尔茨海默病而不发展Notch抑制介导的胃肠道问题。还包括药物组合物和使用方法。

2. 发明授权

US08871796B2 Diaryl ether derivatives as notch sparing gamma secretase inhibitors 有权
标题翻译：二芳基醚衍生物作为缺口保留的γ分泌酶抑制剂
公开(公告)号：US08871796B2
公开(公告)日：2014-10-28
申请号：US13501628
申请日：2010-10-05
申请人： William Colby Brown , Jason Brubaker , Christian Fischer , Richard W. Heidebrecht , John T. Hendrix , Elizabeth H. Kelley , Rachel N. MacCoss , Joey L. Methot , Thomas Miller , Karin M. Otte , Phieng Siliphaivanh , Thomas Reger , Peter D. Williams , Catherine M. Wiscount
发明人： William Colby Brown , Jason Brubaker , Christian Fischer , Richard W. Heidebrecht , John T. Hendrix , Elizabeth H. Kelley , Rachel N. MacCoss , Joey L. Methot , Thomas Miller , Karin M. Otte , Phieng Siliphaivanh , Thomas Reger , Peter D. Williams , Catherine M. Wiscount
IPC分类号： A61K31/415 , C07D401/00 , C07D421/00 , C07D405/10 , C07D413/12 , C07D409/12 , C07D417/12 , C07D231/22 , C07D413/14 , C07D491/113 , C07D405/12 , C07D401/04 , C07D405/14 , C07D401/12
CPC分类号： C07D231/22 , C07D231/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/113
摘要： The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明包括一类新的二芳基醚衍生物，其抑制通过推定的γ-分泌酶处理APP，同时保留Notch信号通路，因此可用于治疗或预防阿尔茨海默病而不发展Notch抑制介导的胃肠道问题。还包括药物组合物和使用方法。

3. 发明授权

US09315475B2 HIV protease inhibitors 有权
标题翻译： HIV蛋白酶抑制剂
公开(公告)号：US09315475B2
公开(公告)日：2016-04-19
申请号：US14021930
申请日：2013-09-09
申请人： Christian Beaulieu , David J. Bennett , Christopher J. Bungard , Ronald K. Chang , Sheldon Crane , Thomas J. Greshock , Li Hao , Kate Holloway , Jesse J. Manikowski , John A. McCauley , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Philippe G. Nantermet , Christian Nadeau , Satyanarayana Tummanapalli , William Shipe , Sanjay Kumar Singh , Vouy Linh Truong , Sivalenka Vijayasaradhi , Peter D. Williams , Catherine M. Wiscount
发明人： Christian Beaulieu , David J. Bennett , Christopher J. Bungard , Ronald K. Chang , Sheldon Crane , Thomas J. Greshock , Li Hao , Kate Holloway , Jesse J. Manikowski , John A. McCauley , Daniel McKay , Carmela Molinaro , Oscar Miguel Moradei , Philippe G. Nantermet , Christian Nadeau , Satyanarayana Tummanapalli , William Shipe , Sanjay Kumar Singh , Vouy Linh Truong , Sivalenka Vijayasaradhi , Peter D. Williams , Catherine M. Wiscount
IPC分类号： C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D265/30 , C07D487/04 , C07D493/04 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07F7/08
CPC分类号： C07D265/30 , A61K31/5375 , A61K31/5377 , A61K31/695 , A61K45/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D487/04 , C07D493/04 , C07F7/0814
摘要： The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：式I所包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

4. 发明授权

US06515011B2 Thrombin inhibitors 失效
标题翻译：凝血酶抑制剂
公开(公告)号：US06515011B2
公开(公告)日：2003-02-04
申请号：US10023776
申请日：2001-12-18
申请人： Harold G. Selnick , James C. Barrow , Philippe G. Nantermet , Peter D. Williams , Kenneth J. Stauffer , Philip E. Sanderson , Kenneth E. Rittle , Matthew M. Morrissette , Catherine M. Wiscount , Lekhanh O. Tran , Terry A. Lyle , Donnette D. Staas
发明人： Harold G. Selnick , James C. Barrow , Philippe G. Nantermet , Peter D. Williams , Kenneth J. Stauffer , Philip E. Sanderson , Kenneth E. Rittle , Matthew M. Morrissette , Catherine M. Wiscount , Lekhanh O. Tran , Terry A. Lyle , Donnette D. Staas
IPC分类号： A61K3140
CPC分类号： C07D401/06 , A61K38/00 , C07D205/04 , C07D207/16 , C07D403/12 , C07K5/06 , C07K5/06034 , C07K5/06078 , C07K5/06139 , C07K5/06191
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. where R3 is —CH2NH2, —CH2CH2NH2, or —CH2NHC(O)OC(CH3)3.
摘要翻译：本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓闭塞：或其药学上可接受的盐，例如，其中R 3是-CH 2 NH 2，-CH 2 CH 2 NH 2或-CH 2 NHC（O）OC（CH 3）3。

5. 发明申请

US20100056516A1 1-HYDROXY NAPHTHYRIDINE COMPOUNDS AS ANTI-HIV AGENTS 审中-公开
标题翻译： 1-羟基萘啶化合物作为抗HIV药物
公开(公告)号：US20100056516A1
公开(公告)日：2010-03-04
申请号：US12373907
申请日：2007-07-13
申请人： Peter D. Williams , Shankar Venkatraman , H. Marie Langford , Boyoung Kim , Theresa M. Booth , Jay A. Grobler , Donnette Staas , Rowena D. Ruzek , Mark W. Embrey , Catherine M. Wiscount , Terry A. Lyle
发明人： Peter D. Williams , Shankar Venkatraman , H. Marie Langford , Boyoung Kim , Theresa M. Booth , Jay A. Grobler , Donnette Staas , Rowena D. Ruzek , Mark W. Embrey , Catherine M. Wiscount , Terry A. Lyle
IPC分类号： A61K31/4375 , C07D471/04 , C07D413/14 , A61K31/5377 , A61P31/18
CPC分类号： C07D471/04
摘要： 1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.
摘要翻译：式I的1-羟基萘啶化合物（例如，1-羟基萘啶-2（1H） - 酮化合物是HIV整合酶和/或HIV核糖核酸酶H和HIV复制抑制剂的抑制剂：（I）其中X和R 1 -R 6是这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防，延迟发作和治疗。该化合物用于抗艾滋病毒感染和艾滋病作为化合物本身或以其形式化合物及其盐可用作药物组合物中的成分，任选地与其它抗HIV剂如HIV抗病毒剂，免疫调节剂，抗生素和疫苗组合使用。

6. 发明授权

US06528503B2 Thrombin inhibitors 失效
标题翻译：凝血酶抑制剂
公开(公告)号：US06528503B2
公开(公告)日：2003-03-04
申请号：US10171708
申请日：2002-06-14
申请人： Peter D. Williams , Terry A. Lyle , Matthew M. Morrissette , Lekhanh O. Tran , Donnette D. Staas
发明人： Peter D. Williams , Terry A. Lyle , Matthew M. Morrissette , Lekhanh O. Tran , Donnette D. Staas
IPC分类号： A61K31397
CPC分类号： C07D401/06 , A61K38/00 , C07D205/04 , C07D207/16 , C07D403/12 , C07K5/06078 , C07K5/06139 , C07K5/06191
摘要： Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, e.g. 1-(3(S)-Cyclopropyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide, and 1-(3-Cyclopropyl-3-methyl-2(R)-hydroxybutanoyl)azetidine-2(S)-N-(2-aminomethyl-5-chlorobenzyl)carboxamide.
摘要翻译：本发明的化合物可用于抑制具有以下结构的凝血酶和相关的血栓闭塞：或其药学上可接受的盐，例如， 1-（3-（S） - 环丙基-2（R） - 羟基丁酰基）氮杂环丁烷-2（S）-N-（2-氨基甲基-5-氯苄基）甲酰胺和1-（3-环丙基-3-甲基-2 （R） - 羟基丁酰基）氮杂环丁烷-2（S）-N-（2-氨基甲基-5-氯苄基）甲酰胺。

7. 发明授权

US6087373A Thrombin inhibitors 失效
标题翻译：凝血酶抑制剂
公开(公告)号：US6087373A
公开(公告)日：2000-07-11
申请号：US157964
申请日：1998-09-21
申请人： Craig Coburn , Joseph P. Vacca , Peter D. Williams
发明人： Craig Coburn , Joseph P. Vacca , Peter D. Williams
IPC分类号： A61P9/10 , C07D471/04 , A61K31/4375
CPC分类号： C07D471/04
摘要： A compound which inhibits human thrombin and which has the general structure ##STR1##
摘要翻译：一种抑制人凝血酶并具有一般结构的化合物

8. 发明授权

US5670509A Tocolytic oxytocin receptor antagonists 失效
标题翻译：溶血性催产素受体拮抗剂
公开(公告)号：US5670509A
公开(公告)日：1997-09-23
申请号：US411619
申请日：1995-04-05
申请人： Ben E. Evans , Douglas W. Hobbs , Joseph M. Pawluczyk , Douglas J. Pettibone , Kenneth E. Rittle , Peter D. Williams
发明人： Ben E. Evans , Douglas W. Hobbs , Joseph M. Pawluczyk , Douglas J. Pettibone , Kenneth E. Rittle , Peter D. Williams
IPC分类号： C07D221/20 , C07D401/12 , C07D405/06 , A61K31/44 , C07D471/10
CPC分类号： C07D221/20 , C07D401/12 , C07D405/06
摘要： Compounds of the formula X-Y-Z-R.sup.1 wherein: X is ##STR1## Y is --CO-- or --SO.sub.2 --; Z is an optional substituent selected from --NH--, --O--, --CHR--, --CH.dbd.CH--, --CH.dbd., --(CH.sub.2).sub.m -- or--CHCHOH--; and R.sup.1 is --CH.sub.3 --, --CH(CH.sub.3).sub.2, or substituted phenyl are tocolytic oxytocin antagonists useful in the treatment of pre-term labor, stripping labor preparatory to Caesarean delivery and dysmenorrhea.
摘要翻译： PCT No.PCT / US93 / 09152 Sec。 371日期1995年04月5日 102（e）1995年4月5日PCT PCT 1993年9月27日PCT公布。出版物WO94 / 07496 日期：1994年4月14日，式X-Y-Z-R 1的化合物其中：X为-CO-或-SO 2 - ; Z是选自-NH-，-O-，-CHR-，-CH = CH - ， - CH =， - （CH 2）m - 或-CHCHOH-的任选取代基; R1为-CH3-，-CH（CH3）2或取代苯基为溶解性催产素拮抗剂，可用于治疗前期劳动，剥夺预备剖宫产和痛经的劳动者。

9. 发明申请

US20170217986A1 HIV PROTEASE INHIBITORS 有权
公开(公告)号：US20170217986A1
公开(公告)日：2017-08-03
申请号：US15123111
申请日：2015-03-02
申请人： John A. MCCAULEY , David Johathan BENNETT , Christopher J. BUNGARD , Thomas J. GRESHOCK , M. Katharine HOLLOWAY , Peter D. WILLIAMS , Christian BEAULIEU , Sheldon CRANE , Stephanie LESSARD , Daniel MCKAY , Carmela MOLINARO , Oscar Miguel MORADEI , Vijayasaradhi SIVALENKA , Vouy Linh TRUONG , Satyanarayana TUMMANAPALLI , Merck Canada Inc.
发明人： John A. McCauley , David Jonathan Bennett , Christopher J. Bungard , Thomas J. Greshock , M. Katharine Holloway , Peter D. Williams , Christian Beaulieu , Sheldon Crane , Stephanie Lessard , Daniel Mckay , Carmela Molinaro , Oscar Miguel Moradei , Vijayasaradhi Sivalenka , Vouy Linh Truong , Satyanarayana Tummanapalli
IPC分类号： C07D498/10 , A61K31/5375 , C07D413/12 , A61K31/5377 , C07D417/14 , A61K45/06 , C07D487/04 , C07D471/04 , C07D413/06 , C07D265/36 , A61K31/5386 , C07D265/30 , C07D413/14
CPC分类号： C07D498/10 , A61K31/5375 , A61K31/5377 , A61K31/5386 , A61K45/06 , C07D265/30 , C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

10. 发明申请

US20090312335A1 Hiv Integrase Inhibitors 审中-公开
标题翻译： Hiv整合酶抑制剂
公开(公告)号：US20090312335A1
公开(公告)日：2009-12-17
申请号：US12084158
申请日：2006-10-23
申请人： John S Wai , Peter D. Williams , Terry A. Lyle
发明人： John S Wai , Peter D. Williams , Terry A. Lyle
IPC分类号： A61K31/495 , C07D471/04
CPC分类号： C07D487/04
摘要： Substituted hydroxytetrahydropyrrolopyrazinone and substituted hydroxytetrahydro-pyrazolopyrazinone compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein R1, R2, R3, R4; R5, X, ring A, and Q are as defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：取代的羟基四氢吡咯并吡嗪酮和式（I）的取代的羟基四氢吡唑并吡嗪酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂：（I）其中R1，R2，R3，R4; R5，X，环A和Q如本文所定义。这些化合物可用于预防和治疗艾滋病毒感染以及预防，延迟艾滋病的发病和治疗。这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

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