专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20070027158A1 High affinity small molecule C5a receptor modulators 失效
标题翻译：高亲和力小分子C5a受体调节剂
公开(公告)号：US20070027158A1
公开(公告)日：2007-02-01
申请号：US10853731
申请日：2004-05-24
申请人： Andrew Thurkauf , Xiao-shu He , He Zhao
发明人： Andrew Thurkauf , Xiao-shu He , He Zhao
IPC分类号： C07D41/02 , C07D43/02
CPC分类号： C07D207/327 , C07C233/11 , C07C233/22 , C07C233/65 , C07C233/66 , C07C233/73 , C07C233/78 , C07C235/46 , C07C235/48 , C07C235/54 , C07C235/60 , C07C235/62 , C07C235/66 , C07C237/20 , C07C323/62 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2603/18 , C07D213/38 , C07D213/82 , C07D215/12 , C07D217/04 , C07D217/06 , C07D217/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D233/68 , C07D235/02 , C07D235/14 , C07D235/18 , C07D317/58 , C07D333/24 , C07D333/28 , C07D333/54 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04
摘要： This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure, 2) heteroaryl in structure, 3) a pharmaceutically acceptable oral dose can provide a detectable in vitro effect, 4) comprise fewer than four or preferably no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. This invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.
摘要翻译：本发明涉及作为哺乳动物补体C5a受体调节剂的低分子量，非肽，非拟肽，有机分子，优选用作高亲和力C5a受体配体的调节剂，还涉及作为拮抗剂或反向激动剂的这些配体的补体C5a受体。本发明优选的化合物具有一些或全部以下性质，因为它们是：1）结构中的多芳基，2）结构中的杂芳基，3）药学上可接受的口服剂量可提供可检测的体外效应，4）包含少于四个或优选不存在酰胺键，以及5）能够以纳摩尔或亚纳摩尔浓度抑制白细胞趋化性。本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗各种炎性和免疫系统疾病中的用途。此外，本发明涉及使用这些化合物作为C5a受体定位的探针。

2. 发明授权

US06884815B1 High affinity small molecule C5a receptor modulators 失效
标题翻译：高亲和力小分子C5a受体调节剂
公开(公告)号：US06884815B1
公开(公告)日：2005-04-26
申请号：US10461311
申请日：2003-06-12
申请人： Andrew Thurkauf , Xiao-shu He , He Zhao , John Peterson , Xiaoyan Zhang , Robbin Brodbeck , James Krause , George Maynard , Alan Hutchison
发明人： Andrew Thurkauf , Xiao-shu He , He Zhao , John Peterson , Xiaoyan Zhang , Robbin Brodbeck , James Krause , George Maynard , Alan Hutchison
IPC分类号： C07C233/11 , C07C233/22 , C07C233/65 , C07C233/66 , C07C233/73 , C07C233/78 , C07C235/46 , C07C235/48 , C07C235/54 , C07C235/60 , C07C235/62 , C07C235/66 , C07C237/20 , C07C323/62 , C07D207/32 , C07D207/327 , C07D213/38 , C07D213/82 , C07D215/12 , C07D217/04 , C07D217/06 , C07D217/14 , C07D217/16 , C07D231/12 , C07D233/54 , C07D233/68 , C07D235/02 , C07D235/10 , C07D235/14 , C07D235/18 , C07D317/58 , C07D333/24 , C07D333/28 , C07D333/54 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04 , A61K31/415 , A61K31/44 , C07D233/02 , C07D401/04 , C07D403/02
CPC分类号： C07D207/327 , C07C233/11 , C07C233/22 , C07C233/65 , C07C233/66 , C07C233/73 , C07C233/78 , C07C235/46 , C07C235/48 , C07C235/54 , C07C235/60 , C07C235/62 , C07C235/66 , C07C237/20 , C07C323/62 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2603/18 , C07D213/38 , C07D213/82 , C07D215/12 , C07D217/04 , C07D217/06 , C07D217/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D233/68 , C07D235/02 , C07D235/14 , C07D235/18 , C07D317/58 , C07D333/24 , C07D333/28 , C07D333/54 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04
摘要： This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure, 2) heteroaryl in structure, 3) a pharmaceutically acceptable oral dose can provide a detectable in vitro effect, 4) comprise fewer than four or preferably no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations.This invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.
摘要翻译：本发明涉及作为哺乳动物补体C5a受体调节剂的低分子量，非肽，非拟肽，有机分子，优选用作高亲和力C5a受体配体的调节剂，还涉及作为拮抗剂或反向激动剂的这些配体的补体C5a受体。本发明优选的化合物具有一些或全部以下性质，因为它们是：1）结构中的多芳基，2）结构中的杂芳基，3）药学上可接受的口服剂量可提供可检测的体外效应，4）包含少于四个或优选不存在酰胺键，以及5）能够以纳摩尔或亚纳摩尔浓度抑制白细胞趋化性。本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗各种炎性和免疫系统疾病中的用途。此外，本发明涉及使用这些化合物作为C5a受体定位的探针。

3. 发明授权

US06432946B1 3-aminoalkylamino-2H-1,4-benzoxazines and 3-aminoalkylamino-2H-1,4-benzothiazines: dopamine receptor subtype specific ligands 失效
标题翻译： 3-氨基烷基氨基-2H-1,4-苯并恶嗪和3-氨基烷基氨基-2H-1,4-苯并噻嗪类：多巴胺受体亚型特异性配体
公开(公告)号：US06432946B1
公开(公告)日：2002-08-13
申请号：US09633042
申请日：2000-08-04
申请人： Xiao-shu He
发明人： Xiao-shu He
IPC分类号： A61K3154
CPC分类号： C07D413/12 , C07D265/36 , C07D417/12
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: Ar represents aryl or heteroaryl; R1 and R2 are the same or different and represent organic or inorganic substituents; R5 is hydrogen or C1-C6 alkyl; W represents CH or nitrogen; X is oxygen or sulfur; and A represents an alkylene group, which compounds bind selectively with high affinity to the dopamine D4 receptor subtype and are therefore of use in treatment of various neuropsychological disorders.
摘要翻译：公开了下式的化合物或其药学上可接受的酸加成盐，其中：Ar表示芳基或杂芳基; R 1和R 2相同或不同，表示有机或无机取代基; R 5表示氢或C 1 -C 6烷基; W表示 CH或氮; X为氧或硫; 并且A表示亚烷基，该化合物以高亲和力选择性结合多巴胺D4受体亚型，因此可用于治疗各种神经心理障碍。

4. 发明授权

US06245768B1 1-(N′-(arylalkylaminoalkyl)) aminoisoindoles; a new class of dopamine receptor subtype specific ligands 失效
标题翻译： 1-（N' - （芳基烷基氨基烷基））氨基异吲哚; 一类新的多巴胺受体亚型特异性配体
公开(公告)号：US06245768B1
公开(公告)日：2001-06-12
申请号：US09366371
申请日：1999-08-03
申请人： Xiao-shu He , Brian de Costa , Jan W. F. Wasley
发明人： Xiao-shu He , Brian de Costa , Jan W. F. Wasley
IPC分类号： C07D40112
CPC分类号： C07D401/12 , C07D209/44 , C07D403/12
摘要： Disclosed are compounds of the formula or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy; Ar represents optionally substituted aryl or heteroaryl Z represents carbon or nitrogen provided that where Z is carbon, R11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; and where Z is nitrogen, R11 represents an electron pair; R5 is hydrogen or lower alkyl, L and m represent integers; n is 0, or an integer; R12 and R13 independently represent lower alkyl; or together may together form an optionally substituted 5-11 membered ring with the nitrogen atoms to which they are bonded;CR′R″ represents a methylene group optionally substituted with lower alkyl;and k is an integer of from 1 to 3, which compounds are useful in treating various neuropsychochological disorders including, for example, schizophrenia, dementia, depression, anxiety, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
摘要翻译：公开的是式的化合物或其药学上可接受的盐，其中6元环可任选被至多四个独立地选自卤素，羟基，低级烷基或低级烷氧基的基团取代; Ar表示任选取代的芳基或杂芳基Z表示碳或氮，其中Z为碳，R 11表示氢，卤素，羟基，低级烷基或低级烷氧基，或任选被一个或两个选自氢，卤素，羟基，低级烷基或低级烷氧基的基团取代的苯基; 并且其中Z是氮，R 11表示电子对; R 5是氢或低级烷基，L和m表示整数; n是0或整数; R 12和R 13独立地代表低级烷基; 或者一起可以与它们所键合的氮原子一起形成任选取代的5-11元环; CR'R“表示任选被低级烷基取代的亚甲基;并且k是1至3的整数，其中化合物可用于治疗各种神经精神障碍，包括例如精神分裂症，痴呆，抑郁症，焦虑症，帕金森样运动障碍和与使用神经安定药相关的运动障碍。

5. 发明授权

US6100255A 3-aminoalkylamino-2H-1,4-benzoxazines and 3-aminoalkylamino-2H-1,4-benzothiazines: dopamine receptor subtype specific ligands 失效
标题翻译： 3-氨基烷基氨基-2H-1,4-苯并恶嗪和3-氨基烷基氨基-2H-1,4-苯并噻嗪类：多巴胺受体亚型特异性配体
公开(公告)号：US6100255A
公开(公告)日：2000-08-08
申请号：US181624
申请日：1998-10-28
申请人： Xiao-shu He
发明人： Xiao-shu He
IPC分类号： C07D265/36 , C07D413/12 , C07D417/12 , A61K31/496 , A61K31/5355
CPC分类号： C07D413/12 , C07D265/36 , C07D417/12
摘要： Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein:Ar represents aryl or heteroaryl;R.sub.1 and R.sub.2 are the same or different and represent organic or inorganic substituents;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl;W represents CH or nitrogen;X is oxygen or sulfur; andA represents an alkylene group,which compounds bind selectively with high affinity to the dopamine D.sub.4 receptor subtype and are therefore of use in treatment of various neuropsychological disorders.
摘要翻译：公开了下式的化合物或其药学上可接受的酸加成盐，其中：Ar表示芳基或杂芳基; R1和R2相同或不同，代表有机或无机取代基; R5是氢或C1-C6烷基; W表示CH或氮; X是氧或硫; 并且A表示亚烷基，该化合物以高亲和力选择性结合多巴胺D4受体亚型，因此可用于治疗各种神经心理障碍。

6. 发明授权

US5744472A 1-(N'-(arylalkylaminoalkyl)) aminoisoindoles; a new class of dopamine receptor subtype specific ligands 失效
标题翻译： 1-（N' - （芳基烷基氨基烷基））氨基异吲哚; 一类新的多巴胺受体亚型特异性配体
公开(公告)号：US5744472A
公开(公告)日：1998-04-28
申请号：US463430
申请日：1995-06-05
申请人： Xiao-shu He , Brian de Costa , Jan W. F. Wasley
发明人： Xiao-shu He , Brian de Costa , Jan W. F. Wasley
IPC分类号： C07D209/44 , C07D401/12 , C07D403/12 , A61K31/495 , A61K31/50 , C07D401/02 , C07D403/02
CPC分类号： C07D401/12 , C07D209/44 , C07D403/12
摘要： Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy; Ar represents optionally substituted aryl or heteroaryl Z represents carbon or nitrogen provided that where Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; and where Z is nitrogen, R.sub.11 represents an electron pair; R.sub.5 is hydrogen or lower alkyl; L and m represent integers; n is 0, or an integer; R.sub.12 and R.sub.13 independently represent lower alkyl; or together may together form an optionally substituted 5-11 membered ring with the nitrogen atoms to which they are bonded;CR'R" represents a methylene group optionally substituted with lower alkyl; and k is an integer of from 1 to 3, which compounds are useful in treating various neuropsychochological disorders including, for example, schizophrenia, dementia, depression, anxiety, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
摘要翻译：公开了式IMA的化合物或其药学上可接受的盐，其中6元环可任选被至多四个独立地选自卤素，羟基，低级烷基或低级烷氧基的基团取代; Ar表示任选取代的芳基或杂芳基Z表示碳或氮，条件是其中Z为碳，R11表示氢，卤素，羟基，低级烷基或低级烷氧基，或任选被一个或两个选自氢，卤素，羟基，低级烷基或低级烷氧基; 并且其中Z是氮，R11表示电子对; R5是氢或低级烷基; L和m表示整数; n为0，或整数; R 12和R 13独立地表示低级烷基; 或一起可以一起形成与它们所键合的氮原子的任选取代的5-11元环; CR'R“表示任选被低级烷基取代的亚甲基; k为1〜3的整数，该化合物可用于治疗各种神经精神障碍，包括精神分裂症，痴呆，抑郁症，焦虑症，帕金森样运动障碍以及与使用精神抑制药有关的运动障碍。

7. 发明授权

US5571832A Nitrogen-containing cyclohetero alkylamino aryl derivatives for CNS disorders 失效
标题翻译：用于CNS障碍的含氮环杂烷基氨基芳基衍生物
公开(公告)号：US5571832A
公开(公告)日：1996-11-05
申请号：US261796
申请日：1994-06-20
申请人： Brian R. de Costa , Wayne D. Bowen , Xiao-Shu He , Lilian Radesca , Kenner C. Rice
发明人： Brian R. de Costa , Wayne D. Bowen , Xiao-Shu He , Lilian Radesca , Kenner C. Rice
IPC分类号： C07D207/09 , C07D211/22 , C07D211/26 , C07D211/42 , C07D211/56 , C07D211/60 , A61K31/40 , C07D207/08 , C07D207/12 , C07D207/46
CPC分类号： C07D211/22 , C07D207/09 , C07D211/26 , C07D211/42 , C07D211/56 , C07D211/60
摘要： Compounds comprising a pyrrolidinyl ring are disclosed for use in the treatment of cerebral ischemia.
摘要翻译：公开了包含吡咯烷基环的化合物用于治疗脑缺血。

8. 发明授权

US08119665B2 Aryl imidazoles and related compounds as C5a receptor modulators 失效
标题翻译：芳基咪唑和相关化合物作为C5a受体调节剂
公开(公告)号：US08119665B2
公开(公告)日：2012-02-21
申请号：US11680865
申请日：2007-03-01
申请人： George P. Luke , George D. Maynard , Scott Mitchell , Andrew Thurkauf , Linghong Xie , LuYan Zhang , Suoming Zhang , He Zhao , Bertrand L. Chenard , Yang Gao , Bingsong Han , Xiao Shu He
发明人： George P. Luke , George D. Maynard , Scott Mitchell , Andrew Thurkauf , Linghong Xie , LuYan Zhang , Suoming Zhang , He Zhao , Bertrand L. Chenard , Yang Gao , Bingsong Han , Xiao Shu He
IPC分类号： A61K31/4439 , A61K31/4164 , A61K31/4178
CPC分类号： C07D233/64 , A61K31/4164 , C07D233/68 , C07D235/02 , C07D235/30 , C07D237/12 , C07D401/04 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention provides packaged pharmaceutical preparations of Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula where the variables are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.
摘要翻译：本发明提供了芳基取代的咪唑，吡唑，吡啶并且其中变量在本文中定义的相关化合物的包装药物制剂。这些化合物是C5a受体的配体。本发明优选的化合物作用以高亲和力结合C5a受体，在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物。它还涉及这些化合物在治疗各种炎性和免疫系统疾病中的应用。

9. 发明授权

US06432958B1 2-piperazinoalkylaminobenzoazole derivatives: dopamine receptor subtype specific ligands 失效
标题翻译： 2-哌嗪基烷基氨基苯并唑衍生物：多巴胺受体亚型特异性配体
公开(公告)号：US06432958B1
公开(公告)日：2002-08-13
申请号：US09942219
申请日：2001-08-29
申请人： Xiao Shu He
发明人： Xiao Shu He
IPC分类号： A61K31496
CPC分类号： C07D263/58 , C07D235/30 , C07D277/82 , C07D413/12 , C07D417/12
摘要： Disclosed are compounds of the formula: or pharmaceutically acceptable salts thereof, wherein: A is (un)substituted alkylene; R1 and R2 are the same or different and represent hydrogen, halogen, alkyl, alkoxy, alkylthio, hydroxy, (un)substituted amino, cyano, nitro, sulfonamide, trifluoromethyl or trifluoromethoxy; R3, R4, R5, R6, and R8 are independently hydrogen or alkyl; and X is sulfur, oxygen or NR7 where R8 is defined herein; m is an integer chosen from 0, 1 or 2; and Ar is an aryl or heteroaryl group as further defined herein, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
摘要翻译：公开了下式的化合物或其药学上可接受的盐，其中：A是（未）取代的亚烷基; R 1和R 2相同或不同，表示氢，卤素，烷基，烷氧基，烷硫基，羟基，（取代的）取代的氨基氰基，硝基，磺酰胺，三氟甲基或三氟甲氧基; R3，R4，R5，R6和R8独立地为氢或烷基; 并且X是硫，氧或NR 7，其中R 8在本文中定义; m是选自0,1或2的整数; 并且Ar是本文进一步定义的芳基或杂芳基，所述化合物可用于治疗和/或预防神经心理障碍，包括但不限于精神分裂症，躁狂症，痴呆，抑郁症，焦虑症，强迫行为，药物滥用，帕金森病类运动障碍和与使用精神安定药有关的运动障碍。

10. 发明授权

US06310064B1 Aralkyl diazabicycloalkane derivatives for CNS disorders 失效
标题翻译：用于CNS病症的芳烷基二氮杂双环烷烃衍生物
公开(公告)号：US06310064B1
公开(公告)日：2001-10-30
申请号：US09347659
申请日：1999-07-06
申请人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： C07D47104
CPC分类号： C07D471/04 , A61K31/495 , C07D487/04
摘要： Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions. For example, compounds of interest are of the formula:
摘要翻译：公开了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病，例如脑缺血，精神病和抽搐。例如，感兴趣的化合物具有下式：

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式