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1. 发明授权

US08759337B2 Gamma secretase modulators 有权
标题翻译：伽玛分泌酶调节剂
公开(公告)号：US08759337B2
公开(公告)日：2014-06-24
申请号：US13140987
申请日：2009-12-18
申请人： Theodros Asberom , Xianhai Huang , Zhaoning Zhu , John W. Clader , Dmitri A. Pissarnitski , Hubert B. Josien , Hongmei Li
发明人： Theodros Asberom , Xianhai Huang , Zhaoning Zhu , John W. Clader , Dmitri A. Pissarnitski , Hubert B. Josien , Hongmei Li
IPC分类号： A61K31/553 , C07D498/04
CPC分类号： C07D498/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
摘要翻译：本发明提供了作为γ分泌酶调节剂的新型化合物。这些化合物具有式（化学式应该插在这里，如纸上所示）。还公开了使用式（I）化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。

2. 发明授权

US08114879B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
公开(公告)号：US08114879B2
公开(公告)日：2012-02-14
申请号：US12055900
申请日：2008-03-26
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
IPC分类号： A61K31/497 , C07D403/00
CPC分类号： C07D401/06 , A61K31/496 , A61K45/06 , C07D211/58 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R1是氢或烷基; R 2是取代的苯基，取代的杂芳基，芴基，二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R4，R5和R7是氢或烷基; R6是氢，烷基或烯基; 公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

3. 发明授权

US08067621B2 Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors 有权
标题翻译：苯磺酰基 - 苯并二氢吡喃，二氢苯并噻喃，四氢萘和相关的γ分泌酶抑制剂
公开(公告)号：US08067621B2
公开(公告)日：2011-11-29
申请号：US11654821
申请日：2007-01-18
申请人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Ann Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： C07D493/00 , A61K31/35
CPC分类号： C07D311/22 , C07C317/14 , C07C317/20 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06 , C07D405/12 , C07D409/12 , C07D491/04 , C07D493/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译：本发明公开了具有下式的新型γ分泌酶抑制剂：R2和R3，或R2和R4，或R3和R4与它们所连接的原子一起可以形成稠合的环烷基或稠合的杂环烷基环。环烷基环或杂环烷基环可任选被一个或多个取代基取代。一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如，治疗阿尔茨海默病。

4. 发明申请

US20110236400A1 TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS 有权
标题翻译：四氢吡喃葡萄糖消炎酶抑制剂
公开(公告)号：US20110236400A1
公开(公告)日：2011-09-29
申请号：US12665580
申请日：2008-07-01
申请人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul E. McNamara
发明人： Wen-Lian Wu , Thomas A. Bara , Duane A. Burnett , John W. Clader , Martin S. Domalski , Yan Jin , Hubert B. Josien , Hongmei Li , Xian Liang , Dmitri A. Pissarnitski , Thavalakulamgara K. Sasikumar , Jesse K. Wong , Ruo Xu , Zhiqiang Zhao , Paul E. McNamara
IPC分类号： A61K39/395 , C07D493/04 , C07D311/80 , C07D407/12 , A61K31/35 , A61K31/352 , A61K31/381 , A61P25/28 , A61P29/00 , A61P31/00 , C07C201/12 , C07C67/343
CPC分类号： C07D493/04 , C07D311/78 , C07D407/12
摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.
摘要翻译：公开了下式的新型γ-分泌酶抑制剂。还公开了抑制γ-分泌酶，治疗神经变性疾病的方法和治疗阿尔茨海默氏病的方法。还公开了在一个反应步骤中使用醛（或酮）和被两个吸电子基团取代的烷基的混合物制备烯烃的方法，并使该混合物与：（a）磺酰卤（例如磺酰氯）和（b）磺酰基酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱式叔胺，或（d）芳基-C（O） - （O） - 芳基和碱式叔胺，或（e）杂芳基-C（O） - 卤化物和碱式叔胺，或（f）杂芳基-C（O）-O-C（O ） - 杂芳基和碱性叔胺。

5. 发明申请

US20100087425A1 Substituted N-Arylsulfonylheterocyclic Amines As Gamma-Secretase Inhibitors 审中-公开
标题翻译：取代的N-芳基磺酰基杂环胺作为γ-分泌酶抑制剂
公开(公告)号：US20100087425A1
公开(公告)日：2010-04-08
申请号：US12633286
申请日：2009-12-08
申请人： Hubert B. Josien , John W. Clader , Thomas A. Bara , Ruo Xu , Hongmei Li , Dmitri A. Pissarnitaki , Zhiqiang Zhao
发明人： Hubert B. Josien , John W. Clader , Thomas A. Bara , Ruo Xu , Hongmei Li , Dmitri A. Pissarnitaki , Zhiqiang Zhao
IPC分类号： A61K31/5377 , C07D413/14 , C07D413/12 , C07D417/12 , C07D417/14 , A61K31/541 , A61P25/00 , A61P25/28
CPC分类号： C07D265/30 , C07D413/12 , C07D451/02 , C07D487/08
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: L is —O—, —N(R6)—, —S—, —S(O)—, or —S(O2)—; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, —C(O)—Y, —X—C(O)—Y, -alkylene-X—C(O)—Y, -alkylene-C(O)—Y, -alkylene-cycloalkylene-X—C(O)—Y, -alkylene-cycloalkylene-C(O)—Y, -cycloalkylene-alkylene-X—C(O)—Y, -cycloalkylene-alkylene-C(O)—Y, -cycloalkylene-X—C(O)—Y, -cycloalkylene-C(O)—Y, -alkylene-cycloalkylene-alkylene-X—C(O)—Y, -alkylene-cycloalkylene-alkylene-C(O)—Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of —NR8R9, —N(R6)—(CH2)b—NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and aryl heterocycloalkyl; or Y is selected from the group consisting of: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译：本发明公开了下式的新型γ-分泌酶抑制剂：其中：L是-O - ， - N（R6） - ， - S - ， - S（O） - 或-S（O 2） - ; R 1选自芳基和杂芳基; R 2选自烷基，-C（O）-Y，-X-C（O）-Y， - 亚烷基-X-C（O）-Y， - 亚烷基-C（O）-Y， - 亚烷基 - 亚环烷基-X-C（O）-Y-亚烷基 - 亚环烷基-C（O）-Y-亚烷基 - 亚烷基-X-C（O）-Y-亚烷基 - 亚烷基-C（O）（O）-Y-亚烷基-C（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-X-C（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-C（O ）-Y，芳基和杂芳基; R 3选自芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基和烷氧基烷基; 每个R 4和R 5独立地选自H和烷基; 并且Y选自-NR8R9，-N（R6） - （CH2）b-NR8R9，芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基和芳基杂环烷基; 或Y选自：一种或多种式I化合物或包含该化合物的制剂可用于，例如，治疗阿尔茨海默病。

6. 发明授权

US07452891B2 MCH antagonists and their use in the treatment of obesity 失效
标题翻译： MCH拮抗剂及其在治疗肥胖中的应用
公开(公告)号：US07452891B2
公开(公告)日：2008-11-18
申请号：US11045713
申请日：2005-01-28
申请人： John W. Clader , Hubert B. Josien , Anandan Palani , Tin Yau Chan
发明人： John W. Clader , Hubert B. Josien , Anandan Palani , Tin Yau Chan
IPC分类号： A61K31/495 , C07D295/15 , A61K31/444 , A61K31/451 , A61K31/5375 , C07D401/06 , C07D401/10 , C07D405/06
CPC分类号： C07D295/215 , A61K45/06 , C07D211/26 , C07D211/28 , C07D211/34 , C07D211/58 , C07D211/96 , C07D211/98 , C07D295/155 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D405/14
摘要： The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
摘要翻译：本发明公开了作为黑色素浓缩激素（MCH）的新型拮抗剂的化合物以及这些化合物的制备方法。在另一个实施方案中，本发明公开了包含这样的MCH拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

7. 发明授权

US07368457B2 Bridged N-arylsulfonylpiperidines as gamma-secretase inhibitors 失效
标题翻译：桥连的N-芳基磺酰基哌啶作为γ-分泌酶抑制剂
公开(公告)号：US07368457B2
公开(公告)日：2008-05-06
申请号：US10842783
申请日：2004-05-11
申请人： Hubert B. Josien
发明人： Hubert B. Josien
IPC分类号： A61K31/44 , C07D221/02
CPC分类号： C07D451/02 , C07D451/14 , C07D487/08
摘要： In an embodiment, this invention discloses novel gamma secretase inhibitors of Formulae I: wherein the various moieties are described herein. Also disclosed is a method of treating Alzheimer's disease using a compound of Formula I or a composition comprising the compound of Formula I.
摘要翻译：在一个实施方案中，本发明公开了式I的新型γ分泌酶抑制剂：其中本文描述了各种部分。还公开了使用式I化合物或包含式I化合物的组合物治疗阿尔茨海默病的方法。

8. 发明授权

US06689765B2 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：可用作CCR5拮抗剂的哌嗪衍生物
公开(公告)号：US06689765B2
公开(公告)日：2004-02-10
申请号：US10061011
申请日：2002-01-30
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin , Eric Gilbert , Marc A. Labroli
IPC分类号： A61K31695
CPC分类号： C07D401/06 , A61K31/496 , A61K45/06 , C07D211/58 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v, host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，苯基烷基，萘基，萘基烷基，杂芳基或杂芳基烷基; R 4，R 5，R 5和R 5独立地选自氢，烷基，烷氧基烷基，环烷基，环烷基烷基或任选取代的苯基， R 7为氢或烷基; R 6为氢，烷基或烯基;用于治疗HIV，实体器官移植排斥，移植物v，宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎，公开了牛皮癣，哮喘，过敏或多发性硬化，以及新化合物，包含它们的药物组合物，以及本发明的CCR5拮抗剂与用于治疗可用于治疗炎性疾病的HIV或药物。

9. 发明授权

US06683091B2 Gamma Secretase inhibitors 失效
标题翻译： Gamma分泌酶抑制剂
公开(公告)号：US06683091B2
公开(公告)日：2004-01-27
申请号：US10210829
申请日：2002-08-01
申请人： Theodoros Asberom , Henry S. Guzik , Hubert B. Josien , Dmitri A Pissarnitski
发明人： Theodoros Asberom , Henry S. Guzik , Hubert B. Josien , Dmitri A Pissarnitski
IPC分类号： C07D21560
CPC分类号： C07D231/12 , C07D215/58 , C07D233/56 , C07D249/08 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, —(CR32)1-4X(CO)Y; each R3A is independently H or alkyl; X is —O—, —NH, or —N-alkyl; and Y is —NR6R7, or —N(R3)(CH2)2-6NR6R7. Also disclosed is a method of treating Alzheimer's Disease.
摘要翻译：本发明公开了下式的新型γ分泌酶抑制剂：其中：R 1是取代的芳基或取代的杂芳基; R 2是R 1基团，烷基，-X（CO）Y， - （CR 3）2 1-4X（CO）Y; 每个R 3A独立地是H或烷基; X是-O-，-NH或-N-烷基; 并且Y是-NR 6 R 7或-N（R 3）（CH 2）2-6 NR 6 R 7。还公开了治疗阿尔茨海默病的方法。

10. 发明授权

US08569521B2 Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors 有权
标题翻译：苯磺酰基 - 苯并二氢吡喃，二氢苯并噻喃，四氢萘和相关的γ分泌酶抑制剂
公开(公告)号：US08569521B2
公开(公告)日：2013-10-29
申请号：US13267324
申请日：2011-10-06
申请人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Anne Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
发明人： Theodros Asberom , Thomas A. Bara , Chad E. Bennett , Duane A. Burnett , Mary Anne Caplen , John W. Clader , David J. Cole , Martin S. Domalski , Hubert B. Josien , Chad E. Knutson , Hongmei Li , Mark D. McBriar , Dmitri A. Pissarnitski , Li Qiang , Murali Rajagopalan , Thavalakulamgara K. Sasikumar , Jing Su , Haiqun Tang , Wen-Lian Wu , Ruo Xu , Zhiqiang Zhao
IPC分类号： C07D493/00
CPC分类号： C07D311/22 , C07C317/14 , C07C317/20 , C07C317/44 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D311/80 , C07D311/92 , C07D311/94 , C07D313/08 , C07D335/06 , C07D405/12 , C07D409/12 , C07D491/04 , C07D493/04
摘要： This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译：本发明公开了具有下式的新型γ分泌酶抑制剂：R2和R3，或R2和R4，或R3和R4与它们所连接的原子一起可以形成稠合的环烷基或稠合的杂环烷基环。环烷基环或杂环烷基环可任选被一个或多个取代基取代。一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如，治疗阿尔茨海默病。

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