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61. 发明申请

US20060194854A1 New 2-substituted - 1,3-thiazole compounds 审中-公开
标题翻译：新的2-取代-1,3-噻唑化合物
公开(公告)号：US20060194854A1
公开(公告)日：2006-08-31
申请号：US11430061
申请日：2006-05-08
申请人： Stefan Berg , Sven Hellberg
发明人： Stefan Berg , Sven Hellberg
IPC分类号： C07D277/04 , A61K31/426
CPC分类号： C07D277/58 , C07D277/42 , C07D277/48
摘要： The present invention relates to new compounds of formula I, Wherein Y is NR4CONR4, NR4CO, or NR4; R1 is nitro or COR5; R2 is hydrogen or NH2; R3 is C1-6alkyl or C0-6akylaryl wherein C0-6alkylaryl may be substituted by A; R4 is hydrogen; R5 is C1-6alkyl; A is independently selected from halo, OR6 and C1-6alkyl; R6 is C1-6alkyl; provided that the compound is not N-(4-Methoxybenzyl)-N′-(5-nitro-1,3-thiazol-2-yl)urea as a free base or a salt thereof as well as a process for their preparation, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
摘要翻译：本发明涉及新的式I化合物，其中Y是NR 4 CONR 4，NR 4 CO或NR 4 ; R 1是硝基或COR 5; R 2是氢或NH 2; R 3是C 1-6烷基或C 0-6-6烷基芳基，其中C 0-6-0烷基芳基可以是被A取代; R 4是氢; R 5是C 1-6烷基; A独立地选自卤素，OR 6和C 1-6烷基; R 6是C 1-6烷基; 条件是该化合物不是作为游离碱或其盐的N-（4-甲氧基苄基）-N' - （5-硝基-1,3-噻唑-2-基）脲及其制备方法，含有所述治疗活性化合物的药物制剂和所述活性化合物在治疗中的用途。

62. 发明授权

US07056939B2 4-(4Methoxybenzyl)-n′-(5-nitro1,3-thiazol-2-yl)urea and its use in the treatment of conditions associated with glycogen-synthase kinase-3 (gsk3) 失效
标题翻译： 4-（4-甲氧基苄基）-n' - （5-硝基-1,3-噻唑-2-基）脲及其用于治疗与糖原合成酶激酶-3（gsk3）相关的病症的用途，
公开(公告)号：US07056939B2
公开(公告)日：2006-06-06
申请号：US10481711
申请日：2002-07-03
申请人： Stefan Berg , Sven Hellberg
发明人： Stefan Berg , Sven Hellberg
IPC分类号： A61K31/427 , A61K31/426 , C07D277/56 , C07D277/58
CPC分类号： C07D277/58
摘要： The present invention relates to a new compound of formula I as a free base or a pharmaceutically acceptable salt thereof, a process for the preparation, pharmaceutical formulations containing said therapeutically active compound and to the use of said compound in therapy.
摘要翻译：本发明涉及作为游离碱或其药学上可接受的盐的新型式I化合物，制备方法，含有所述治疗活性化合物的药物制剂以及所述化合物在治疗中的用途。

63. 发明授权

US07056921B2 Substituted chroman derivatives 失效
标题翻译：取代的色原衍生物
公开(公告)号：US07056921B2
公开(公告)日：2006-06-06
申请号：US10714577
申请日：2003-11-13
申请人： Stefan Berg , Martin Nylöf , Svante Ross , Seth-Olov Thorberg
发明人： Stefan Berg , Martin Nylöf , Svante Ross , Seth-Olov Thorberg
IPC分类号： A61K31/497 , C07D403/02 , C07D243/06
CPC分类号： C07D405/12 , C07D311/58 , C07D407/12
摘要： The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1–C6 alkyl; R1 is H, C1–C6 alkyl or C3–C6 cycloalkyl; R3 is C1–C6 alkyl, C3–C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0–4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.
摘要翻译：本发明涉及新的具有式（I）的哌啶基或哌嗪基取代的二氢-2H-1-苯并吡喃衍生物化合物，其中X是N或CH; Y是NR 2 CH 2，CH 2 NR 2，NR 2 CO， CONR 2，NR 2 SO 2或NR 2 CONR 2其中R 1，R 2，R 2，R 2， 2是H或C 1 -C 6烷基; R 1是H，C 1 -C 6烷基或C 3 -C 6烷基或C 3 -C 6烷基， SUB>环烷基; R 3是C 1 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，环烷基或（CH 2 CH 2）n - 芳基，其中芳基是苯基或含有一个或两个选自N，O和S的杂原子的杂芳环，并且其可以是单 - 或被R 4和/或R 5二取代的二价基团。 n为0-4; 作为（R） - 对映异构体，（S） - 对映异构体或游离碱或其药学上可接受的盐或溶剂合物形式的外消旋体，其制备方法，含有所述治疗活性化合物的药物组合物和所述活性化合物。

64. 发明申请

US20060052396A1 Arylamines for the treatment of conditions associated with gsk-3 审中-公开
标题翻译：用于治疗与gsk-3有关的病症的芳胺
公开(公告)号：US20060052396A1
公开(公告)日：2006-03-09
申请号：US10481721
申请日：2002-07-03
申请人： Stefan Berg , Sven Hellberg
发明人： Stefan Berg , Sven Hellberg
IPC分类号： A61K31/4965 , A61K31/4439 , C07D403/02 , C07D401/02
CPC分类号： C07D213/42 , C07C233/78 , C07C311/17 , C07C311/29 , C07C311/53 , C07D207/09 , C07D207/12 , C07D207/14 , C07D213/73 , C07D213/75 , C07D213/82 , C07D233/34 , C07D241/26 , C07D243/08 , C07D295/13 , C07D295/185 , C07D295/192 , C07D295/26 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07F5/025
摘要： The present invention relates to new compounds of formula (I) wherein Z, Y, X, P, Q, R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A, m and n are defined as in any one of claims 1 to 3, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds for the treatment of conditions associated with glycogens synthase kinase-3 (GSK3).
摘要翻译：本发明涉及其中Z，Y，X，P，Q，R，R 1，R 2，R 3， R 4，R 5，R 5，R 6，R 7，R 8， R 9，R 9，R 10，R 11，R 12，A，m和n 如权利要求1至3中任一项所定义，其制备方法及其中制备的新中间体，含有所述治疗活性化合物的药物制剂以及所述活性化合物用于治疗与糖原合酶激酶-3相关的病症（GSK3

65. 发明申请

US20050153987A1 Compounds 有权
标题翻译：化合物
公开(公告)号：US20050153987A1
公开(公告)日：2005-07-14
申请号：US10509268
申请日：2003-03-28
申请人： Stefan Berg , Sven Hellberg , Martin Nylof , Yafeng Xue
发明人： Stefan Berg , Sven Hellberg , Martin Nylof , Yafeng Xue
IPC分类号： C07D213/61 , A61K31/404 , A61K31/4427 , A61K31/4439 , A61K31/4545 , A61K31/455 , A61K31/495 , A61K31/496 , A61K31/5377 , A61K31/551 , A61P3/10 , A61P9/10 , A61P15/00 , A61P15/16 , A61P17/14 , A61P21/02 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P31/18 , A61P43/00 , C07D209/34 , C07D213/68 , C07D213/71 , C07D213/81 , C07D213/89 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D43/04 , A61K31/506
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The present invention provides new compounds of formula Ia and Ib: as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
摘要翻译：本发明提供新的式Ia和Ib化合物，以及其制备方法和其中使用的新中间体，含有所述治疗活性化合物的药物制剂和所述活性化合物在治疗中的用途。

66. 发明申请

US20050102489A1 Method and apparatus for compressing VLIW instruction and sharing subinstructions 有权
公开(公告)号：US20050102489A1
公开(公告)日：2005-05-12
申请号：US11015717
申请日：2004-12-17
申请人： Donglok Kim , Stefan Berg , Weiyun Sun , Yongmin Kim
发明人： Donglok Kim , Stefan Berg , Weiyun Sun , Yongmin Kim
IPC分类号： G06F9/318 , G06F9/38 , G06F15/00 , G06F15/76
CPC分类号： G06F9/3891 , G06F9/3017 , G06F9/3853 , G06F9/3885
摘要： A VLIW instruction format is introduced having a set of control bits which identify subinstruction sharing conditions. At compilation the VLIW instruction is analyzed to identify subinstruction sharing opportunities. Such opportunities are encoded in the control bits of the instruction. Before the instruction is moved into the instruction cache, the instruction is compressed into the new format to delete select redundant occurrences of a subinstruction. Specifically, where a subinstruction is to be shared by corresponding functional processing units of respective clusters, the subinstruction need only appear in the instruction once. The redundant appearance is deleted. The control bits are decoded at instruction parsing time to route a shared subinstruction to the associated functional processing units.

67. 发明授权

US06670359B2 Substituted chroman derivatives 失效
标题翻译：取代的苯并二氢吡喃衍生物
公开(公告)号：US06670359B2
公开(公告)日：2003-12-30
申请号：US10285743
申请日：2002-11-01
申请人： Stefan Berg , Martin Nylöf , Svante Ross , Seth-Olov Thorberg
发明人： Stefan Berg , Martin Nylöf , Svante Ross , Seth-Olov Thorberg
IPC分类号： A61K31445
CPC分类号： C07D405/12 , C07D311/58 , C07D407/12
摘要： The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.
摘要翻译：本发明涉及新的具有式（I）的哌啶基或哌嗪基取代的二氢-2H-1-苯并吡喃衍生物化合物，其中X是N或CH; Y是NR2CH2，CH2NR2，NR2CO，CONR2，NR2SO2或NR2CONR2，其中R2是H 或C 1 -C 6烷基; R 1是H，C 1 -C 6烷基或C 3 -C 6环烷基; R 3是C 1 -C 6烷基，C 3 -C 6环烷基或（CH 2）n - 芳基，其中芳基是苯基或杂芳环，两个选自N，O和S的杂原子，可以被R4和/或R5单取代或二取代; n为0-4;作为（R） - 对映异构体，（S） - 对映异构体或形式的游离碱或其药学上可接受的盐或溶剂合物，其制备方法，含有所述治疗活性化合物的药物组合物和所述活性化合物的用途。

68. 发明授权

US06548498B1 Substituted indan derivatives 失效
标题翻译：取代的茚满衍生物
公开(公告)号：US06548498B1
公开(公告)日：2003-04-15
申请号：US09171575
申请日：1998-10-21
申请人： Stefan Berg , Lennart Florvall , Svante Ross , Seth-Olov Thorberg
发明人： Stefan Berg , Lennart Florvall , Svante Ross , Seth-Olov Thorberg
IPC分类号： C07D295135
CPC分类号： C07D295/135 , C07D295/155
摘要： The present invention relates to new piperidyl- or piperazinyl-substituted indan derivatives of the formula I as (R)-enantiomers, (S)-enantiomers, or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof. The present invention further relates to a process for the preparation of the compounds, to pharmaceutical compositions containing the compounds and to methods of treatment of 5-hydroxytryptamine-mediated disorders comprising administering the compounds.
摘要翻译：本发明涉及式Ias（R） - 对映异构体，（S） - 对映异构体或游离碱形式的外消旋物或其药学上可接受的盐或溶剂化物的新的哌啶基或哌嗪基取代的茚满衍生物。本发明还涉及制备所述化合物的方法，含有所述化合物的药物组合物和治疗5-羟色胺介导的病症的方法，包括给予所述化合物。

69. 发明授权

US06410532B1 Substituted 1,2,3,4-tetrahydronaphthalene derivatives 有权
公开(公告)号：US06410532B1
公开(公告)日：2002-06-25
申请号：US09902000
申请日：2001-07-10
申请人： Stefan Berg , Mats Linderberg , Svante Ross , Seth-Olov Thorberg , Bengt Ulff
发明人： Stefan Berg , Mats Linderberg , Svante Ross , Seth-Olov Thorberg , Bengt Ulff
IPC分类号： C07D295135
摘要： The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2 wherein R2 is H or C1-6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy—C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.

70. 发明授权

US06387899B1 Substituted chroman derivatives 失效
标题翻译：取代的苯并二氢吡喃衍生物
公开(公告)号：US06387899B1
公开(公告)日：2002-05-14
申请号：US09171572
申请日：1998-10-21
申请人： Stefan Berg , Mats Linderberg , Svante Ross , Seth-Olov Thorberg , Bengt Ulff
发明人： Stefan Berg , Mats Linderberg , Svante Ross , Seth-Olov Thorberg , Bengt Ulff
IPC分类号： A61K315377
CPC分类号： C07D311/58
摘要： The present invention relates to new piperidinyl- or piperazinyl-substituted-3,4-dihydro-2H-1-benzopyran derivatives having formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted; n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CONR6R7, CN, CF3, OH, C1-C6 alkoxy, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.
摘要翻译：本发明涉及具有式（I）的新的哌啶基或哌嗪基 - 取代-3,4-二氢-2H-1-苯并吡喃衍生物，其中X是N或CH; Y是NR2CH2，CH2NR2，NR2CO，CONR2或NR2SO2，其中R2是H或C1-C6烷基; R1是H，C1-C6烷基或C3-C6环烷基; R 3是C 1 -C 6烷基，C 3 -C 6环烷基或（CH 2）n - 芳基，其中芳基是苯基或含有一个或两个选自N，O和S的杂原子并可以被单取代或二取代的杂芳环; n为0-4; R9是C1-C6烷基，C3-C6环烷基，OCF3，OCHF2，OCH2F，卤素，CONR6R7，CN，CF3，OH，C1-C6烷氧基，NR6R7，SO3CH3，SO3CF3，SO2NR6R7，未取代或取代的杂环或杂芳环一个或两个选自N和O的杂原子，其中取代基是（C 1 -C 6）烷基; 或COR8; 其中R 6，R 7和R 8如上所定义，为（R） - 对映异构体，（S） - 对映异构体或游离碱形式的外消旋体或其药学上可接受的盐或溶剂合物，其制备方法，含有治疗活性化合物和所述活性化合物在治疗中的用途。

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