公开(公告)号：US5071853A

公开(公告)日：1991-12-10

申请号：US483482

申请日：1990-02-27

申请人： Christopher F. Bigge ,  Sheryl J. Hays ,  Graham Johnson ,  Perry M. Novak ,  Daniel F. Ortwine

发明人： Christopher F. Bigge ,  Sheryl J. Hays ,  Graham Johnson ,  Perry M. Novak ,  Daniel F. Ortwine

IPC分类号： A61K31/13 ,  A61K31/35 ,  A61K31/352 ,  A61K31/357 ,  A61K31/38 ,  A61K31/381 ,  A61K31/382 ,  A61K31/435 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/28 ,  C07C15/30 ,  C07C45/51 ,  C07C45/56 ,  C07C45/59 ,  C07C45/68 ,  C07C49/567 ,  C07C49/67 ,  C07C49/697 ,  C07C49/753 ,  C07C61/39 ,  C07C62/34 ,  C07C62/38 ,  C07C69/00 ,  C07C69/753 ,  C07C69/757 ,  C07C211/42 ,  C07C215/44 ,  C07C215/64 ,  C07C217/52 ,  C07C217/74 ,  C07C225/20 ,  C07C233/06 ,  C07C235/40 ,  C07C243/36 ,  C07C247/10 ,  C07C265/10 ,  C07C271/24 ,  C07C271/36 ,  C07C395/00 ,  C07D209/48 ,  C07D211/74 ,  C07D221/06 ,  C07D221/16 ,  C07D265/12 ,  C07D265/34 ,  C07D307/00 ,  C07D311/22 ,  C07D311/58 ,  C07D311/80 ,  C07D315/00 ,  C07D317/72 ,  C07D333/54 ,  C07D333/74 ,  C07D335/02 ,  C07D335/04 ,  C07D335/06 ,  C07D335/10 ,  C07F7/08

CPC分类号： C07D209/48 ,  C07C211/42 ,  C07C215/44 ,  C07C217/52 ,  C07C225/20 ,  C07C233/06 ,  C07C235/40 ,  C07C243/36 ,  C07C247/10 ,  C07C271/24 ,  C07C271/36 ,  C07C395/00 ,  C07C45/511 ,  C07C45/562 ,  C07C45/59 ,  C07C45/68 ,  C07C49/67 ,  C07C49/697 ,  C07C49/753 ,  C07C61/39 ,  C07C62/34 ,  C07C69/00 ,  C07D211/74 ,  C07D221/16 ,  C07D265/34 ,  C07D307/00 ,  C07D311/58 ,  C07D311/80 ,  C07D315/00 ,  C07D317/72 ,  C07D333/54 ,  C07D333/74 ,  C07D335/02 ,  C07D335/04 ,  C07D335/06 ,  C07D335/10 ,  C07F7/0812 ,  C07F7/0818 ,  C07C2101/18 ,  C07C2103/00 ,  C07C2103/10 ,  C07C2103/18 ,  C07C2103/26 ,  C07C2103/30

摘要： A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

公开(公告)号：US4755518A

公开(公告)日：1988-07-05

申请号：US929256

申请日：1986-11-10

申请人： Michael F. Rafferty ,  Graham Johnson

发明人： Michael F. Rafferty ,  Graham Johnson

IPC分类号： C07D257/04 ,  A61K31/41 ,  A61K31/415 ,  C07D223/14

CPC分类号： C07D257/04

摘要： Novel benzoic acid or benzoic acid ester derivatives, pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headaches, such as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.

摘要翻译： 新型苯甲酸或苯甲酸酯衍生物，药物组合物及其使用方法是本发明。 效用是用于治疗关节炎，哮喘，雷诺氏病，炎性肠病，三叉神经痛或疱疹性神经痛，炎症性眼病，牛皮癣，牙痛和头痛，特别是血管性头痛，如偏头痛，丛状，混合型血管综合征 作为非血管性紧张性头痛。

公开(公告)号：US4474793A

公开(公告)日：1984-10-02

申请号：US318113

申请日：1981-11-04

申请人： Barry C. Ross ,  Graham Johnson ,  Michael A. Yeomans

发明人： Barry C. Ross ,  Graham Johnson ,  Michael A. Yeomans

IPC分类号： C07D205/08 ,  A61K31/397 ,  A61K31/43 ,  A61P31/04 ,  C07D205/09 ,  C07D499/88 ,  C07D499/897 ,  C07D513/04 ,  C07F7/18 ,  C07D499/00 ,  A61K31/425

CPC分类号： C07D513/04 ,  C07D205/09 ,  C07D499/88 ,  C07F7/186

摘要： What are disclosed are compounds, useful as intermediates in the preparation of substituted penem compounds, of the formula ##STR1## methods for making such compounds from intermediates of the formula ##STR2## by reaction of the latter with a nucleophilic compound, methods for making such intermediates from compounds of the formula ##STR3## by reaction of the last-mentioned compounds with a tervalent phosphorus compound, and methods for making said last-mentioned compounds by cyclizing compounds of the formula ##STR4## with a tervalent phosphorus compound.

摘要翻译： 所公开的化合物可用作制备取代的penem化合物的中间体，其具有式IMA IMA的方法，其通过后者与亲核化合物的反应由式IMA IMA的中间体制备此类化合物的方法， 通过最后提到的化合物与三价磷化合物的反应，通过式（IMAGE）化合物的中间体，以及通过用三价磷化合物环化式“IMAGE”化合物来制备所述最后提到的化合物的方法。

公开(公告)号：US4263215A

公开(公告)日：1981-04-21

申请号：US91743

申请日：1979-11-06

申请人： Robert H. Hesse ,  Graham Johnson

发明人： Robert H. Hesse ,  Graham Johnson

IPC分类号： C07C401/00 ,  A61K31/07 ,  A61K31/59 ,  C07B41/00 ,  C07C20060101 ,  C07C67/00 ,  C07J9/00

CPC分类号： C07C401/00

摘要： 1-Hydroxy-5,6-trans vitamin D compounds are prepared by oxidizing a 5,6-trans vitamin D compound using a selenic ester which may be formed in situ using selenous acid or selenium dioxide in the presence of an alcohol.

摘要翻译： 1-羟基-5,6-反维生素D化合物是通过使用可在醇存在下使用硒酸或二氧化硒在原位形成的硒酸酯氧化5,6-反式维生素D化合物来制备的。

公开(公告)号：US10472346B2

公开(公告)日：2019-11-12

申请号：US15522969

申请日：2015-10-30

申请人： The General Hospital Coporation ,  The Regents of the University of California ,  Steven L. Wagner ,  William C. Mobley ,  Rudolph E. Tanzi ,  Graham Johnson ,  Ronald Buckle ,  Nicholas Mayhew ,  Robert Jason Herr

发明人： Steven L. Wagner ,  William C. Mobley ,  Rudolph E. Tanzi ,  Graham Johnson ,  Ronald Buckle ,  Nicholas Mayhew ,  Robert Jason Herr ,  Kevin D. Rynearson

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D487/04 ,  A61P25/28

摘要： Provided herein are compounds and methods for treating a disorder associated with aberrant A3 peptide levels, including Alzheimer's disease. Provided herein are compositions and methods for treating a disorder associated with aberrant Aβ peptide levels, including AD. Provided herein are compounds of Formula (A) or a pharmaceutically acceptable salt thereof, wherein, L′ is selected from the group consisting of C(O), C(R1)(R2), substituted or unsubstituted —C2-6 alkylene-, and substituted or unsubstituted —C3-6 cycloalkylene.

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.

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.

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.

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.

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。