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公开(公告)号：US20160031899A1
公开(公告)日：2016-02-04
申请号：US14772731
申请日：2014-02-27
Applicant: AQUINOX PHARMACEUTICALS (Canada) INC.
Inventor： Lloyd F. Mackenzie , Thomas B. MacRury , Curtis Harwig , David Bogucki , Jeffery R. Raymond , Jeremy D. Pettigrew
IPC: C07D493/10 , C07D211/58 , C07C255/30 , C07D213/75 , C07C275/22 , C07C335/10 , C07D231/54 , C07D215/227 , C07D221/16 , C07C215/38 , C07D307/52 , C07D333/20 , C07D213/38 , C07D277/28 , C07D231/56 , C07D261/20 , C07D277/64 , C07C35/21 , C07C35/23 , C07D307/42 , C07C233/23 , C07D213/82
CPC classification number: C07D493/10 , A61K31/416 , C07C35/21 , C07C35/23 , C07C215/26 , C07C215/38 , C07C233/23 , C07C255/30 , C07C275/22 , C07C335/10 , C07C2601/14 , C07C2602/24 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/75 , C07D213/82 , C07D215/227 , C07D221/16 , C07D221/18 , C07D231/54 , C07D231/56 , C07D261/20 , C07D277/24 , C07D277/28 , C07D277/64 , C07D307/42 , C07D307/52 , C07D333/16 , C07D333/20
Abstract: Compounds of formula (II): wherein A, R1, R2, R5 and R13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
Abstract translation: 本文描述了其中A，R 1，R 2，R 5和R 13或其立体异构体，对映异构体或互变异构体或其混合物或其药学上可接受的盐或溶剂化物的式（II）化合物，以及其它 化合物。 这些化合物具有作为SHIP1调节剂的活性，因此可用于治疗将受益于SHIP1调节的各种疾病，病症或病症。 还公开了包含本发明化合物的组合物，以及通过将这些化合物施用于有需要的动物的SHIP1调节方法。
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2.发明授权
公开(公告)号：US5387709A
公开(公告)日：1995-02-07
申请号：US134731
申请日：1993-10-12
Applicant: Claude Lardy , Daniel Guerrier , Gilles Chavernac , Francois Collonges
Inventor： Claude Lardy , Daniel Guerrier , Gilles Chavernac , Francois Collonges
IPC: A61K31/18 , A61K31/195 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/35 , A61K31/351 , A61K31/396 , A61K31/397 , A61K31/415 , A61K31/47 , A61K31/66 , A61K31/665 , A61K31/675 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/08 , A61P43/00 , C07C211/17 , C07C211/35 , C07C215/38 , C07C217/52 , C07C229/34 , C07C255/46 , C07C303/36 , C07C303/38 , C07C311/16 , C07C311/17 , C07C311/19 , C07C311/20 , C07C311/29 , C07C317/14 , C07C323/67 , C07D203/26 , C07D205/04 , C07D215/36 , C07D233/54 , C07D233/84 , C07D237/04 , C07D257/04 , C07D307/14 , C07D307/64 , C07D309/04 , C07D333/34 , C07F9/38 , C07C255/00
CPC classification number: C07D257/04 , C07C211/17 , C07C211/35 , C07C255/46 , C07C311/16 , C07C311/19 , C07C311/20 , C07C311/29 , C07C317/14 , C07C323/67 , C07D215/36 , C07D233/84 , C07D237/04 , C07D307/64 , C07D309/04 , C07D333/34 , C07F9/3882 , C40B50/14 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14
Abstract: The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts possibly in the form of complexes, esters and amides thereof, represented by the formula: ##STR1##
Abstract translation: 本发明涉及新的取代磺酰胺和可能以其复合物，酯和酰胺形式的生理上可接受的盐，由下式表示：
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3.发明授权
公开(公告)号：US5354781A
公开(公告)日：1994-10-11
申请号：US707229
申请日：1991-05-24
Applicant: Jean-Claude Breliere , Pierre Casellas , Serge Lavastre , Raymond Paul
Inventor： Jean-Claude Breliere , Pierre Casellas , Serge Lavastre , Raymond Paul
IPC: A61K31/135 , A61P37/06 , C07C209/68 , C07C209/70 , C07C209/74 , C07C211/27 , C07C211/28 , C07C211/29 , C07C211/35 , C07C213/00 , C07C215/28 , C07C215/30 , C07C215/38 , C07C221/00 , C07C225/16 , C07C225/18 , C07C211/40 , A61K31/44
CPC classification number: C07C225/18 , C07C211/35 , C07C215/38 , C07C2101/14
Abstract: The present invention relates to compounds of the formula ##STR1## in which: p1 R.sub.1 is hydrogen or a halogen atom; R.sub.2 is a cyclohexyl or a phenyl;R.sub.3 is a (C.sub.3 -C.sub.6) cycloalkyl;R.sub.4 is hydrogen, (C.sub.1 -C.sub.6) alkyl or (C.sub.3 -C.sub.6)cycloalkyl;A is --CO--CH.sub.2 --, --CH(CI)--CH.sub.2 --, --CH(OH)--CH.sub.2 --, CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- and --C.tbd.C--, or their addition salt with mineral or organic acids. These compounds are active on the immune system. The present invention further relates to a method of preparing said compounds and to the pharmaceutical compounds in which they are present.
Abstract translation: 本发明涉及式（I）的化合物，其中：p1R1是氢或卤素原子; R2是环己基或苯基; R3是（C3-C6）环烷基; R4是氢，（C1-C6）烷基或（C3-C6）环烷基; A是-CO-CH 2 - ， - CH（C 1）-CH 2 - ， - CH（OH）-CH 2 - ，CH 2 -CH 2 - ， - CH = CH-和-C 有机酸。 这些化合物在免疫系统上是有活性的。 本发明还涉及制备所述化合物的方法及其存在于其中的药物化合物。
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公开(公告)号：US5047432A
公开(公告)日：1991-09-10
申请号：US541174
申请日：1990-06-20
Applicant: John R. Housley , James E. Jeffery , David N. Johnston , Bruce J. Sargent
Inventor： John R. Housley , James E. Jeffery , David N. Johnston , Bruce J. Sargent
IPC: C07D307/52 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/22 , A61K31/33 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P25/24 , A61P25/26 , C07C45/63 , C07C49/567 , C07C67/00 , C07C213/00 , C07C215/38 , C07C217/48 , C07C217/74 , C07C219/22 , C07C225/18 , C07C231/00 , C07C231/12 , C07C235/06 , C07C313/00 , C07C317/28 , C07C323/29 , C07D211/14 , C07D211/30 , C07D211/70 , C07D213/30 , C07D295/073 , C07D295/08 , C07D295/084 , C07D295/10 , C07D295/13 , C07D295/145 , C07D295/185 , C07D317/28 , C07D319/06
CPC classification number: C07D213/30 , C07C45/63 , C07C49/567 , C07D211/70 , C07D295/073 , C07D295/092 , C07D295/13 , C07D295/145 , C07D295/185 , C07D317/28
Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof; in which R.sub.1 and R.sub.2, which are the same or different, are H or an optionally substituted hydrocarbon group or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring;R.sub.3 is an optionally substituted aromatic hydrocarbon group; andR.sub.4 is a hydrocarbon group containing at least one substituent selected from the group consisting of hydroxy and acylated derivatives thereof, optionally substituted alkoxy groups, optionally substituted cycloalkyloxy groups, optionally substituted alkylenedioxy groups, oxo and groups of formula S(O).sub.p R.sub.5 in which p is 0, 1 or 2 and R.sub.5 is an alkyl group, said hydrocarbon group being optionally substituted by additional substituents,are useful in the treatment of depression.
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5.发明授权Pharmaceutical use of laevorotatory basic derivative of 9,10-ethanoanthracene 失效药物使用9,10-乙炔蒽的lavoorotatory碱性衍生物
公开(公告)号：US5004755A
公开(公告)日：1991-04-02
申请号：US100145
申请日：1987-08-28
Applicant: Angelo Storni
Inventor： Angelo Storni
IPC: A61K31/135 , A61P25/24 , A61P25/26 , C07C213/02 , C07C213/04 , C07C213/08 , C07C215/38 , C07D263/04
CPC classification number: C07D263/04
Abstract: The present invention relates to a new laevorotatory basic derivative of 9,10-ethanoanthracene, namely R-(-)-.alpha.-[(methylamino)methyl]-9,10-ethanoanthracene-9(10H)-ethanol of the formula I ##STR1## and the acid addition salts thereof, to pharmaceutical compositions containing these new substances and to a method for treating dysphoric conditions, psychovegetative or psychosomatic disorders.
Abstract translation: 本发明涉及式I的R 10 - （ - ） - α - [（甲基氨基）甲基] -9,10-乙炔基-9（10H） - 乙醇的新型laivorotatory碱性衍生物， IMAGE>（I）及其酸加成盐用于含有这些新物质的药物组合物，以及治疗焦虑症状，精神心理障碍或心身疾病的方法。
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Patent Agency Ranking
公开(公告)号：US4925879A
公开(公告)日：1990-05-15
申请号：US227869
申请日：1988-08-01
Applicant: John R. Housley , James E. Jeffery , David N. Johnston , Bruce J. Sargent
Inventor： John R. Housley , James E. Jeffery , David N. Johnston , Bruce J. Sargent
IPC: C07D307/52 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/215 , A61K31/22 , A61K31/33 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P25/24 , A61P25/26 , C07C45/63 , C07C49/567 , C07C67/00 , C07C213/00 , C07C215/38 , C07C217/48 , C07C217/74 , C07C219/22 , C07C225/18 , C07C231/00 , C07C231/12 , C07C235/06 , C07C313/00 , C07C317/28 , C07C323/29 , C07D211/14 , C07D211/30 , C07D211/70 , C07D213/30 , C07D295/073 , C07D295/08 , C07D295/084 , C07D295/10 , C07D295/13 , C07D295/145 , C07D295/185 , C07D317/28 , C07D319/06
CPC classification number: C07D213/30 , C07C45/63 , C07C49/567 , C07D211/70 , C07D295/073 , C07D295/092 , C07D295/13 , C07D295/145 , C07D295/185 , C07D317/28
Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof; in which R.sub.1 and R.sub.2, which are the same or different, are H or an optionally substituted hydrocarbon group or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring;R.sub.3 is an optionally substituted aromatic hydrocarbon group; andR.sub.4 is a hydrocarbon group containing at least one substituent selected from the group consisting of hydroxy and acylated derivatives thereof, optionally substituted alkoxy groups, optionally substituted cycloalkyloxy groups, optionally substituted alkylenedioxy groups, oxo and groups of formula S(O).sub.p R.sub.5 in which p is 0, 1 or 2 and R.sub.5 is an alkyl group, said hydrocarbon group being optionally substituted by additional substituents,are useful in the treatment of depression.
Abstract translation: 式I化合物及其药学上可接受的盐; 其中相同或不同的R 1和R 2为H或任选取代的烃基或R 1和R 2与它们所连接的氮原子一起形成任选取代的杂环; R3是任选取代的芳族烃基; 并且R 4是含有至少一个选自羟基和其酰化衍生物，任选取代的烷氧基，任选取代的环烷氧基，任选取代的亚烷基二氧基，氧代和式S（O）p R 5基团的取代基的烃基，其中 p为0,1或2，R5为烷基，所述烃基任选被其它取代基取代，可用于治疗抑郁症。
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7.发明授权10,11-dihydro-5H-dibenzo[a,d]cycloheptadiene derivatives in a method for treating cardiac arrhythmia 失效10,11-二氢-5H-二苯并[a，d]环庚二烯衍生物在治疗心律失常的方法中的用途
公开(公告)号：US4670435A
公开(公告)日：1987-06-02
申请号：US803576
申请日：1985-12-02
Applicant: Albrecht Franke, deceased , Claus D. Mueller , Dieter Lenke
Inventor： Albrecht Franke, deceased , Claus D. Mueller , Dieter Lenke
IPC: A61K31/135 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P9/06 , C07C67/00 , C07C213/00 , C07C215/38 , C07C217/08 , C07D295/08 , C07D295/084
CPC classification number: C07D295/084
Abstract: 10,11-Dihydro-5H-dibenzo[a,d]cycloheptadiene derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 have the meanings stated in the description, and their preparation are described. The novel substances are useful for the treatment of disorders.
Abstract translation: 10,11-二氢-5H-二苯并[a，d]环庚二烯衍生物，其中R1和R2具有说明书中所述的含义，并描述了它们的制备方法。 新物质可用于治疗疾病。
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公开(公告)号：US09765085B2
公开(公告)日：2017-09-19
申请号：US14772731
申请日：2014-02-27
Applicant: Aquinox Pharmaceuticals (Canada) Inc.
Inventor： Lloyd F. Mackenzie , Thomas B. MacRury , Curtis Harwig , David Bogucki , Jeffery R. Raymond , Jeremy D. Pettigrew
IPC: C07D231/54 , A61K31/416 , C07D493/10 , C07D213/75 , C07D213/82 , C07D215/227 , C07C275/22 , C07D221/18 , C07C215/26 , C07C215/38 , C07C335/10 , C07C233/23 , C07D261/20 , C07D277/24 , C07D277/28 , C07C255/30 , C07D211/58 , C07D213/30 , C07D307/42 , C07D333/16 , C07D231/56 , C07D277/64 , C07C35/21 , C07C35/23 , C07D213/38 , C07D221/16 , C07D307/52 , C07D333/20
CPC classification number: C07D493/10 , A61K31/416 , C07C35/21 , C07C35/23 , C07C215/26 , C07C215/38 , C07C233/23 , C07C255/30 , C07C275/22 , C07C335/10 , C07C2601/14 , C07C2602/24 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/75 , C07D213/82 , C07D215/227 , C07D221/16 , C07D221/18 , C07D231/54 , C07D231/56 , C07D261/20 , C07D277/24 , C07D277/28 , C07D277/64 , C07D307/42 , C07D307/52 , C07D333/16 , C07D333/20
Abstract: Compounds of formula (II): wherein A, R1, R2, R5 and R13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
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公开(公告)号：US20170247389A2
公开(公告)日：2017-08-31
申请号：US14772731
申请日：2014-02-27
Applicant: Aquinox Pharmaceuticals (Canada) Inc.
Inventor： Lloyd F. Mackenzie , Thomas B. MacRury , Curtis Harwig , David Bogucki , Jeffery R. Raymond , Jeremy D. Pettigrew
IPC: C07D493/10 , C07D211/58 , C07C255/30 , C07D213/75 , C07C275/22 , C07C335/10 , C07D231/54 , C07D215/227 , C07D221/16 , C07C215/38 , C07D307/52 , C07D333/20 , C07D213/38 , C07D277/28 , C07D231/56 , C07D261/20 , C07D277/64 , C07C35/21 , C07C35/23 , C07D307/42 , C07C233/23 , C07D213/82
CPC classification number: C07D493/10 , A61K31/416 , C07C35/21 , C07C35/23 , C07C215/26 , C07C215/38 , C07C233/23 , C07C255/30 , C07C275/22 , C07C335/10 , C07C2601/14 , C07C2602/24 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/75 , C07D213/82 , C07D215/227 , C07D221/16 , C07D221/18 , C07D231/54 , C07D231/56 , C07D261/20 , C07D277/24 , C07D277/28 , C07D277/64 , C07D307/42 , C07D307/52 , C07D333/16 , C07D333/20
Abstract: Compounds of formula (II): wherein R1, R2, R5 and R13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
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公开(公告)号：US20120041039A1
公开(公告)日：2012-02-16
申请号：US13278925
申请日：2011-10-21
Applicant: Ian L. Scott , Vladimir A. Kuksa , Mark W. Orme , Feng Hong , Thomas L. Little, JR. , Ryo Kubota
Inventor： Ian L. Scott , Vladimir A. Kuksa , Mark W. Orme , Feng Hong , Thomas L. Little, JR. , Ryo Kubota
IPC: A61K31/4406 , A61K31/137 , C07C215/28 , C07C217/48 , C07C217/70 , A61K31/138 , C07C217/74 , C07D335/02 , A61K31/382 , C07C215/38 , C07D213/38 , A61K31/4402 , C07D333/20 , A61K31/381 , C07C237/20 , A61K31/165 , C07D309/06 , A61K31/351 , C12N5/071 , C12N5/079 , A61P27/02 , A61P29/00 , C07C211/27
CPC classification number: A61K31/382 , A61K31/138 , A61K31/165 , A61K31/351 , C07C211/27 , C07C213/00 , C07C215/20 , C07C215/28 , C07C215/30 , C07C215/42 , C07C217/16 , C07C217/48 , C07C217/54 , C07C217/72 , C07C217/74 , C07C219/22 , C07C225/16 , C07C225/18 , C07C233/18 , C07C235/34 , C07C235/54 , C07C237/20 , C07C237/38 , C07C237/40 , C07C257/14 , C07C279/08 , C07C317/28 , C07C323/25 , C07C323/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D213/30 , C07D213/38 , C07D309/06 , C07D333/16 , C07D333/20 , C07D335/02
Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
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