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公开(公告)号:US20150258048A1
公开(公告)日:2015-09-17
申请号:US14725732
申请日:2015-05-29
申请人: Allergan, Inc.
发明人: David W. Old
IPC分类号: A61K31/192 , A61K31/381
CPC分类号: A61K31/192 , A61K31/381 , C07C65/36 , C07C65/40 , C07C2602/08 , C07C2602/10 , C07D333/40
摘要: The invention provides well-defined compounds that are either EP2 agonists, EP4 agonists, or mixed EP2/EP4 agonist. The compounds are useful for treating a variety of pathological conditions associated with activity of the EP2 and/or EP4 receptors.
摘要翻译: 本发明提供了明确定义的化合物,其是EP2激动剂,EP4激动剂或混合EP2 / EP4激动剂。 该化合物可用于治疗与EP2和/或EP4受体的活性相关的各种病理状况。
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公开(公告)号:US09051294B2
公开(公告)日:2015-06-09
申请号:US14264144
申请日:2014-04-29
申请人: Allergan, Inc.
发明人: David W. Old
IPC分类号: C07D333/40 , C07C65/36 , C07C65/40
CPC分类号: A61K31/192 , A61K31/381 , C07C65/36 , C07C65/40 , C07C2602/08 , C07C2602/10 , C07D333/40
摘要: The invention provides well-defined compounds that are either EP2 agonists, EP4 agonists, or mixed EP2/EP4 agonist. The compounds are useful for treating a variety of pathological conditions associated with activity of the EP2 and/or EP4 receptors.
摘要翻译: 本发明提供了明确定义的化合物,其是EP2激动剂,EP4激动剂或混合EP2 / EP4激动剂。 该化合物可用于治疗与EP2和/或EP4受体的活性相关的各种病理状况。
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公开(公告)号:US08431614B2
公开(公告)日:2013-04-30
申请号:US13148566
申请日:2010-02-18
IPC分类号: A61K31/192 , C07C59/48 , C07C59/86
CPC分类号: C07C205/56 , C07B2200/07 , C07C59/54 , C07C59/56 , C07C59/88 , C07C59/90 , C07C65/36 , C07C69/757 , C07C69/76 , C07C229/42 , C07C323/62 , C07C2601/08
摘要: There is provided a novel loxoprofen derivative that has no side effect such as a gastrointestinal disorder and also has excellent anti-inflammatory and analgesic effects and is represented by the following formula (I) or (II): (wherein R1 and R2 each represent a halogen atom or a substituted or unsubstituted phenyl group) or a pharmacologically acceptable salt thereof. In the derivative, the halogen atom is selected from a chlorine atom, a bromine atom, a fluorine atom, and an iodine atom, and a substituent of the substituted phenyl group is a halogen atom, a hydroxyl group, a substituted or unsubstituted lower alkyl group, a lower alkylthio group, a lower alkoxy group, a nitro group, an amino group, or a carboxyl group.
摘要翻译: 本发明提供一种新颖的洛索洛芬衍生物,其不具有胃肠功能紊乱等副作用,具有优异的抗炎镇痛效果,并且由下式(I)或(II)表示:(其中R1和R2各自表示 卤素原子或取代或未取代的苯基)或其药理学上可接受的盐。 在衍生物中,卤素原子选自氯原子,溴原子,氟原子和碘原子,取代苯基的取代基为卤素原子,羟基,取代或未取代的低级烷基 低级烷硫基,低级烷氧基,硝基,氨基或羧基。
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公开(公告)号:US20090118169A1
公开(公告)日:2009-05-07
申请号:US11941180
申请日:2007-11-16
申请人: Hisaaki Chaki , Tadakazu Takakura , Keiichi Tsuchida , Hironori Kotsubo , Yukihiko Aikawa , Shuichi Hirono , Shunichi Shiozawa
发明人: Hisaaki Chaki , Tadakazu Takakura , Keiichi Tsuchida , Hironori Kotsubo , Yukihiko Aikawa , Shuichi Hirono , Shunichi Shiozawa
IPC分类号: A61K38/03 , C07K4/00 , C07D241/04 , A61K31/495 , C07D207/333 , A61K31/40 , C07D209/42 , A61K31/404 , C07D235/26 , A61K31/4184
CPC分类号: C07D207/333 , A61K38/00 , C07C59/64 , C07C59/84 , C07C65/24 , C07C65/34 , C07C65/36 , C07C65/38 , C07C65/40 , C07C69/738 , C07C69/94 , C07C229/34 , C07C233/01 , C07C233/47 , C07C235/20 , C07C235/84 , C07C251/32 , C07C251/48 , C07C251/60 , C07C255/49 , C07C275/24 , C07C311/06 , C07C311/51 , C07D207/08 , C07D209/42 , C07D235/26 , C07D277/60 , C07K7/06 , C07K7/64 , Y02P20/55
摘要: A compound comprising the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: wherein N1 represents an atom to which a donative hydrogen atom in a hydrogen-bond donating group is bonded or a hydrogen-bond accepting atom in a hydrogen-bond accepting group; N3 represents a hydrogen-bond accepting atom in a hydrogen-bond accepting group; and N2, N4 and N5 independently represents an arbitrary carbon atom constituting a hydrophobic group and defined by the interatomic distances between N1, N2, N3, N4 and N5; and, in the optimized three-dimensional structure thereof, the distances between the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, in the optimized steric structure thereof, are the interatomic distances in a pharmacophore; or a salt thereof;inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases into which overexpression of AP-1 participates and as an AP-1 inhibitor.
摘要翻译: 包含对应于N 3的原子和选自N1,N2,N4和N5的两个或更多个原子的化合物,所述原子构成由下式表示的药效团:其中N1表示氢原子中的供体氢原子, 在氢键接受基团中键合供体基团或氢键接受原子; N3表示氢键接受基团中的氢键接受原子; N2,N4和N5独立地表示构成疏水基团的任意碳原子,由N1,N2,N3,N4和N5之间的原子间距离定义; 并且在其优化的三维结构中,在优化的空间结构中,对应于N 3的原子和选自N1,N2,N4和N5的两个或更多个原子之间的距离是药效团中的原子间距离; 或其盐; 抑制转录因子AP-1的活性,可用作预防和治疗AP-1过表达的疾病和作为AP-1抑制剂的药物。
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公开(公告)号:US20080146632A1
公开(公告)日:2008-06-19
申请号:US12024859
申请日:2008-02-01
IPC分类号: A61K31/41 , C07D403/12 , C07C321/20 , A61K31/192 , C07D333/70 , A61K31/381 , C07C321/30 , A61P37/00 , A61P19/02
CPC分类号: C07C323/56 , C07C59/68 , C07C65/36 , C07C65/38 , C07C229/60 , C07C233/05 , C07C251/24 , C07C251/86 , C07C255/41 , C07C271/22 , C07C275/24 , C07C275/42 , C07C317/44 , C07C323/22 , C07C323/60 , C07C323/62 , C07C2603/18 , C07D207/333 , C07D249/14 , C07D277/20 , C07D303/38 , C07D333/70 , C07D409/14 , C07K5/06026 , C07K5/0806
摘要: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the FcγRIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.
摘要翻译: 本发明提供能够结合Fc受体并调节Fc受体活性的化合物,其包含被富含p电子的基团取代的芳基形式的核心亲油基团。 本发明还提供了使用这些化合物治疗涉及Fc受体活性的自身免疫性疾病的方法。 还提供了一种获得调节Fc受体活性的化合物的方法,所述方法包括:(a)提供或设计具有结构特征的化合物,以配合FcγRIIa结构的凹槽; 和(b)筛选化合物以调节对Fc受体的活性。
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公开(公告)号:US20050288522A1
公开(公告)日:2005-12-29
申请号:US11205602
申请日:2005-08-17
申请人: Dennis Vogel , Kim Vogel
发明人: Dennis Vogel , Kim Vogel
IPC分类号: C07C1/24 , C07C1/207 , C07C15/20 , C07C15/56 , C07C17/35 , C07C25/22 , C07C45/46 , C07C49/617 , C07C49/665 , C07C49/675 , C07C49/697 , C07C49/753 , C07C50/22 , C07C50/24 , C07C51/377 , C07C63/331 , C07C63/72 , C07C65/34 , C07C65/36 , C07C65/40 , C07D219/06 , C07D337/12 , C07D337/14 , H01L51/00
CPC分类号: C07D337/12 , C07C1/2078 , C07C15/20 , C07C17/35 , C07C25/22 , C07C45/46 , C07C49/665 , C07C49/675 , C07C49/697 , C07C49/753 , C07C50/22 , C07C50/24 , C07C51/377 , C07C63/331 , C07C63/72 , C07C65/34 , C07C65/36 , C07C65/40 , C07C2527/03 , C07C2603/52 , C07D219/06 , C07D337/14 , H01L51/0003 , H01L51/0055 , H01L51/0071 , C07C49/76 , C07C15/38
摘要: A process for preparing substituted pentacene compounds comprises the step of cyclizing substituted bis(benzyl)phthalic acids using an acid composition comprising trifluoromethanesulfonic acid, the substituted bis(benzyl)phthalic acids being represented by the following general formulas: wherein each R (that is, each of the groups R1 through R8) is independently an electron-donating group, a halogen atom, a hydrogen atom, or a combination thereof.
摘要翻译: 制备取代并五苯化合物的方法包括使用包含三氟甲磺酸的酸组合物使取代的双(苄基)邻苯二甲酸环化的步骤,取代的双(苄基)邻苯二甲酸由以下通式表示:其中每个R(即, 基团R 1至R 8中的每一个独立地是给电子基团,卤素原子,氢原子或其组合。
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公开(公告)号:US06316404B1
公开(公告)日:2001-11-13
申请号:US09745681
申请日:2000-12-22
IPC分类号: A61K3828
CPC分类号: G01N33/5044 , A61K31/00 , A61K31/192 , A61K31/425 , A61K31/44 , A61K31/4418 , A61K38/28 , A61K45/06 , C07C57/50 , C07C59/72 , C07C63/49 , C07C63/66 , C07C65/28 , C07C65/36 , C07C251/48 , C07C2602/10 , C07C2603/24 , C07D221/08 , C07D265/34 , C07D311/92 , C07D317/30 , G01N33/5008 , G01N33/502 , G01N33/5038 , G01N33/5073 , G01N2500/00 , A61K2300/00
摘要: This invention relates to methods and compositions for the treatment of non-insulin-dependent diabetes mellitus using an RXR agonist alone or in combination with a PPAR&ggr; agonist such as a thiazolidinedione compound.
摘要翻译: 本发明涉及使用单独的RXR激动剂或与PPARγ激动剂如噻唑烷二酮化合物组合治疗非胰岛素依赖性糖尿病的方法和组合物。
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公开(公告)号:US06300376B1
公开(公告)日:2001-10-09
申请号:US09093060
申请日:1998-06-08
申请人: John Walsh , Neil Frankish , Helen Sheridan , Ronan Farrell , William Byrne
发明人: John Walsh , Neil Frankish , Helen Sheridan , Ronan Farrell , William Byrne
IPC分类号: A01N3500
CPC分类号: C07C311/20 , C07C13/465 , C07C35/32 , C07C35/52 , C07C43/188 , C07C45/46 , C07C45/511 , C07C45/62 , C07C45/65 , C07C45/673 , C07C45/68 , C07C45/71 , C07C45/74 , C07C49/67 , C07C49/683 , C07C49/697 , C07C49/755 , C07C59/86 , C07C65/36 , C07C69/007 , C07C69/013 , C07C69/738 , C07C69/76 , C07C69/92 , C07C215/44 , C07C225/20 , C07C233/32 , C07C251/44 , C07C309/66 , C07C2602/08 , C07C49/80
摘要: Indane dimer compounds and their pharmaceutical use particularly to achieve smooth muscle relaxing activity and/or mast cell stabilizing activity and/or anti-inflammatory activity are described.
摘要翻译: 描述了吲哚二聚体化合物及其药物用途,特别是实现平滑肌松弛活性和/或肥大细胞稳定活性和/或抗炎活性。
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公开(公告)号:US06228862B1
公开(公告)日:2001-05-08
申请号:US09309370
申请日:1999-05-11
IPC分类号: A61K31435
CPC分类号: G01N33/5044 , A61K31/00 , A61K31/192 , A61K31/425 , A61K31/44 , A61K31/4418 , A61K38/28 , A61K45/06 , C07C57/50 , C07C59/72 , C07C63/49 , C07C63/66 , C07C65/28 , C07C65/36 , C07C251/48 , C07C2602/10 , C07C2603/24 , C07D221/08 , C07D265/34 , C07D311/92 , C07D317/30 , G01N33/5008 , G01N33/502 , G01N33/5038 , G01N33/5073 , G01N2500/00 , A61K2300/00
摘要: This invention relates to methods and compositions for the treatment of non-insulin-dependent diabetes mellitus using an RXR agonist alone or in combination with a PPAR&ggr; agonist such as a thiazolidinedione compound.
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公开(公告)号:US5451649A
公开(公告)日:1995-09-19
申请号:US214934
申请日:1994-03-17
申请人: Roland Zenk , Helmut G. Alt , M. Bruce Welch
发明人: Roland Zenk , Helmut G. Alt , M. Bruce Welch
IPC分类号: C07C13/567 , B01J31/22 , C07C22/04 , C07C49/747 , C07C51/31 , C07C51/373 , C07C51/377 , C07C63/331 , C07C63/49 , C07C65/36 , C07F7/00 , C07F7/08 , C07F17/00 , C08F4/639 , C08F4/6392 , C08F4/64 , C08F4/642 , C08F4/659 , C08F4/6592 , C08F10/00 , C08F110/02 , C08F110/06 , C08F210/16
CPC分类号: C07F17/00 , B01J31/143 , B01J31/2295 , C07C13/567 , C07C22/04 , C07C49/747 , C07C51/31 , C07C51/373 , C07C51/377 , C07C63/331 , C07C63/49 , C07C65/36 , C07F7/006 , C07F7/0809 , C07F7/0818 , C08F10/00 , C08F110/06 , C08F210/16 , C08F4/65927 , B01J2531/40 , B01J2531/46 , B01J2531/48 , B01J2531/49 , B01J2531/50 , B01J2531/60 , C07C2101/10 , C07C2101/14 , C07C2101/16 , C07C2103/18 , C08F110/02 , C08F4/63912 , C08F4/63922 , C08F4/65912 , C08F4/65922
摘要: Benzofluorenyl-containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.
摘要翻译: 公开含有苯并芴基的金属茂以及用于制备金属茂的方法。 还公开了使用金属茂作为聚合催化剂的方法。 此外,公开了由这种聚合产生的聚合物。
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