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公开(公告)号:US09944644B2
公开(公告)日:2018-04-17
申请号:US14775565
申请日:2014-03-13
申请人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Nicoleta Dobri , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
发明人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Nicoleta Dobri , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
IPC分类号: C07D487/04 , C07D498/04 , C07D471/04 , C07D519/00 , C07D403/04 , C07D403/12 , C07D401/12 , C07D403/06 , C07D209/52
CPC分类号: C07D487/04 , C07D209/52 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D471/04 , C07D498/04 , C07D519/00
摘要: The present invention provides compounds comprising variously substituted octahydropyrrolopyrroles, their synthesis, methods of making, methods of using, compositions and formulations thereof.
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公开(公告)号:US20180030060A1
公开(公告)日:2018-02-01
申请号:US15722760
申请日:2017-10-02
申请人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Rando Allikmets , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
发明人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Rando Allikmets , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
IPC分类号: C07D487/04 , C07D471/04
CPC分类号: C07D487/04 , C07D471/04
摘要: The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof.
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公开(公告)号:US09434727B2
公开(公告)日:2016-09-06
申请号:US14699672
申请日:2015-04-29
申请人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Rando Allikmets , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
发明人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Rando Allikmets , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
IPC分类号: C07D211/06 , C07D295/00 , C07D471/04 , C07D487/04
CPC分类号: C07D487/04 , C07D471/04
摘要: The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明提供具有以下结构的化合物:其中R 1,R 2,R 3,R 4和R 5各自独立地为H,卤素,CF 3或C 1 -C 4烷基,其中R 1,R 2,R 3,R 4或R 5中的两个或多个 不是H; R6是H,OH或卤素; B是取代或未取代的杂双环,其中当R1是CF3时,R2是H,R3是F,R4是H,R5是H,或R1是H,R2是CF3,R3是H,R4是CF3, R5是H,或R1是Cl,R2是H,R3是H,R4是F,R5是H,或R1是CF3,R2是H,R3是F,R4是H,R5是H,或R1 为CF 3,R 2为F,R 3为H,R 4为H,R 5为H或R 1为Cl,R 2为F,R 3为H,R 4为H,R 5为H,则B为 其可接受的盐。
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公开(公告)号:US20150315197A1
公开(公告)日:2015-11-05
申请号:US14699672
申请日:2015-04-29
申请人: Konstantin PETRUKHIN , Christopher CIOFFI , Graham JOHNSON , Rando ALLIKMETS , Emily FREEMAN , Ping CHEN , Michael CONLON , Lei ZHU
发明人: Konstantin PETRUKHIN , Christopher CIOFFI , Graham JOHNSON , Rando ALLIKMETS , Emily FREEMAN , Ping CHEN , Michael CONLON , Lei ZHU
IPC分类号: C07D487/04 , C07D471/04
CPC分类号: C07D487/04 , C07D471/04
摘要: The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明提供具有以下结构的化合物:其中R 1,R 2,R 3,R 4和R 5各自独立地为H,卤素,CF 3或C 1 -C 4烷基,其中R 1,R 2,R 3,R 4或R 5中的两个或多个 不是H; R6是H,OH或卤素; B是取代或未取代的杂双环,其中当R1是CF3时,R2是H,R3是F,R4是H,R5是H,或R1是H,R2是CF3,R3是H,R4是CF3, R5是H,或R1是Cl,R2是H,R3是H,R4是F,R5是H,或R1是CF3,R2是H,R3是F,R4是H,R5是H,或R1 为CF 3,R 2为F,R 3为H,R 4为H,R 5为H或R 1为Cl,R 2为F,R 3为H,R 4为H,R 5为H,B为 其可接受的盐。
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公开(公告)号:USD664673S1
公开(公告)日:2012-07-31
申请号:US29410621
申请日:2012-01-10
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公开(公告)号:US20180298012A1
公开(公告)日:2018-10-18
申请号:US15950528
申请日:2018-04-11
申请人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Nicoleta Dobri , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
发明人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Nicoleta Dobri , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
IPC分类号: C07D487/04 , C07D519/00 , C07D209/52 , C07D498/04 , C07D403/04 , C07D403/06 , C07D401/12 , C07D403/12 , C07D471/04
摘要: The present invention provides compounds comprising variously substituted octahydropyrrolopyrroles, their synthesis, methods of making, methods of using, compositions and formulations thereof.
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公开(公告)号:US09777010B2
公开(公告)日:2017-10-03
申请号:US15254966
申请日:2016-09-01
申请人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Rando Allikmets , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
发明人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Rando Allikmets , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
IPC分类号: C07D211/06 , C07D487/04 , C07D471/04
CPC分类号: C07D487/04 , C07D471/04
摘要: The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof.
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公开(公告)号:US20170247327A1
公开(公告)日:2017-08-31
申请号:US15457821
申请日:2017-03-13
申请人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Nicoleta Dobri , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
发明人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Nicoleta Dobri , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
IPC分类号: C07D209/52 , C07D471/04 , C07D498/04 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D403/06 , C07D487/04
CPC分类号: C07D209/52 , A61K31/454 , C07D209/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D471/04 , C07D487/04 , C07D498/04
摘要: The present invention provides Octahydrocyclopentapyrrole compounds having the structure: (structurally represented) wherein psi is absent or present, and when present is a bond; R1, R2, R3, R4, and R5 are each independently H, halogen, CF, or C1-C4 alkyl; R6 is absent or present, and when present is H, OH, or halogen; A is absent or present, and when present is C(O) or C(O)NH; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is C(O); and when psi is present, then R6 is absent and when psi is absent, then R6 is present, or a pharmaceutically acceptable salt thereof, for treatment of diseases characterized by excessive lipofuscin accumulation in the retina.
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公开(公告)号:US09637450B2
公开(公告)日:2017-05-02
申请号:US14775540
申请日:2014-03-13
申请人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Nicoleta Dobri , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
发明人: Konstantin Petrukhin , Christopher Cioffi , Graham Johnson , Nicoleta Dobri , Emily Freeman , Ping Chen , Michael Conlon , Lei Zhu
IPC分类号: C07D209/02 , A61K31/454 , C07D403/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D471/04 , C07D487/04 , C07D498/04 , C07D209/52
CPC分类号: C07D209/52 , A61K31/454 , C07D209/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D471/04 , C07D487/04 , C07D498/04
摘要: The present invention provides Octahydrocyclopentapyrrole compounds having the structure: (structurally represented) wherein psi is absent or present, and when present is a bond; R1, R2, R3, R4, and R5 are each independently H, halogen, CF, or C1-C4 alkyl; R6 is absent or present, and when present is H, OH, or halogen; A is absent or present, and when present is C(O) or C(O)NH; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is C(O); and when psi is present, then R6 is absent and when psi is absent, then R6 is present, or a pharmaceutically acceptable salt thereof, for treatment of diseases characterized by excessive lipofuscin accumulation in the retina.
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公开(公告)号:US20160046649A1
公开(公告)日:2016-02-18
申请号:US14775546
申请日:2014-03-13
申请人: Konstantin PETRUKHIN , Christopher CIOFFI , Graham JOHNSON , Nicoleta DOBRI , Emily FREEMAN , Ping CHEN , Michael CONLON , Lei ZHU
发明人: Konstantin PETRUKHIN , Christopher CIOFFI , Graham JOHNSON , Nicoleta DOBRI , Emily FREEMAN , Ping CHEN , Michael CONLON , Lei ZHU
IPC分类号: C07D498/04 , C07D249/04 , C07D487/04 , C07D213/79 , C07D239/28 , C07D237/24 , C07D471/04 , C07C233/56
CPC分类号: C07D498/04 , C07C233/56 , C07D213/79 , C07D213/80 , C07D231/56 , C07D237/24 , C07D239/28 , C07D249/04 , C07D471/04 , C07D487/04 , C07D491/052
摘要: The present invention provides a compound having the structure: (structurally represented) wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl; R6 is alkyl; A is absent or present, and when present is —C(O)— or —C(O)NH—; B is substituted or unsubstituted monocycle, bicycle, heteromonocycle, heterobicycle, benzyl, CO2H or (C1-C4 alkyl)-CO2H, wherein when B is CO2H, then A is present and is —C(O)—, or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明提供具有以下结构的化合物:(结构上表示)其中R 1,R 2,R 3,R 4和R 5各自独立地为H,卤素,CF 3或C 1 -C 4烷基; R6是烷基; A不存在或存在,当存在时为-C(O) - 或-C(O)NH-; B是取代或未取代的单环,自由基,杂单环,杂双环,苄基,CO 2 H或(C 1 -C 4烷基)-CO 2 H,其中当B是CO 2 H时,则A存在且为-C(O) - 或其药学上可接受的盐 其中。
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