专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

11. 发明授权

US09303027B2 Kappa opioid receptor agonists 有权
标题翻译：卡帕阿片受体激动剂
公开(公告)号：US09303027B2
公开(公告)日：2016-04-05
申请号：US13811020
申请日：2011-07-19
申请人： Pradip Kumar Sasmal , Vamsee Krishna Chintakunta , Vijay Potluri , Ish Kumar Khanna , Ashok Tehim , Mahaboobi Jaleel , Thomas Hogberg , Oystein Rist , Lisbeth Elster , Thomas Michael Frimurer , Lars-Ole Gerlach
发明人： Pradip Kumar Sasmal , Vamsee Krishna Chintakunta , Vijay Potluri , Ish Kumar Khanna , Ashok Tehim , Mahaboobi Jaleel , Thomas Hogberg , Oystein Rist , Lisbeth Elster , Thomas Michael Frimurer , Lars-Ole Gerlach
IPC分类号： C07D419/12 , C07D207/09 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D207/12 , C07D209/34 , C07D213/76 , C07D215/12 , C07D215/227 , C07D231/56 , C07D249/18 , C07D261/20 , C07D263/56 , C07D263/58 , C07D275/06 , C07D277/30 , C07D279/02 , C07D295/13
CPC分类号： C07D419/12 , C07D207/09 , C07D207/12 , C07D209/34 , C07D213/76 , C07D215/12 , C07D215/227 , C07D231/56 , C07D249/18 , C07D261/20 , C07D263/56 , C07D263/58 , C07D275/06 , C07D277/30 , C07D279/02 , C07D295/13 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
摘要翻译：本发明涉及一系列具有通式（I）的取代的化合物，包括其立体异构体和/或其药学上可接受的盐。（I）其中A，m，R 1，R 2，R 3，R 4如本文所定义。本发明还涉及制备这些化合物包括中间体的方法。本发明的化合物在κ（αKα）阿片受体（KOR）位点是有效的。因此，本发明的化合物可用作药物，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性疼痛以及相关疾病，特别是周边功能在CNS。

12. 发明申请

US20090105218A1 CRTH2 Receptor Ligands For Therapeutic Use 审中-公开
标题翻译： CRTH2受体配体用于治疗用途
公开(公告)号：US20090105218A1
公开(公告)日：2009-04-23
申请号：US11597938
申请日：2005-05-30
申请人： Trond Ulven , Thomas Frimurer , Oystein Rist , Evi Kostenis , Thomas Hogberg
发明人： Trond Ulven , Thomas Frimurer , Oystein Rist , Evi Kostenis , Thomas Hogberg
IPC分类号： A61K31/196 , A61K31/44 , A61K31/381 , A61K31/341 , A61K31/5375 , A61K31/445 , A61K31/55 , A61P17/00 , A61P25/00 , A61P1/00 , A61P11/00
CPC分类号： A61K31/245 , A61K31/196 , A61K31/341 , A61K31/40 , A61K31/4453 , A61K31/5375 , A61K31/55 , A61K31/63 , A61K31/635
摘要： Compounds of formula (I) are useful in the treatment of disease responsive to modulation of CRTH2 receptor activity, wherein: A represents a carboxyl group —COOH, or a carboxyl bioisostere; L1 is a bond, —CH2—, —OCH2—, —CH2CH2— or —CH═CH—; L2 is CONH—, —NHCO—, SO2NR1—, —NR1SO2 wherein R1 is hydrogen or C1-C3 alkyl, or a divalent radical of formula (X) or (Y), wherein ring Q is a non aromatic heterocyclic ring containing 5 to 7 ring atoms, including the nitrogen shown; L3 is a divalent linker radical of formula -(Alk1)m-(Z)n-(Alk2)p as defined in the description; ring Ar1 is an optionally substituted divalent phenyl radical or divalent 5- or 6-membered monocyclic heteroaryl radical, in which L1 and the H[B]sL3L2Ar2CONH-radical are linked to adjacent ring carbon atoms; ring Ar2 is an optionally substituted 1,3-phenylene radical, or an optionally substituted divalent 5- or 6-membered monocyclic heteroaryl radical, in which AL1Ar1NHCO-radical and the H[B]sL3L2-radical are linked to ring carbon atoms which are not in ortho relationship; ring B is as defined for Ar2, or an optionally substituted cycloalkyl, N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; and s is 0 or 1.
摘要翻译：式（I）化合物可用于治疗对CRTH2受体活性调节作用的疾病，其中：A表示羧基-COOH或羧基生物电子等排体; L 1是键，-CH 2 - ， - OCH 2 - ， - CH 2 CH 2 - 或-CH-CH-; L2是CONH，-NHCO-，SO2NR1，-NR1SO2，其中R1是氢或C1-C3烷基，或式（X）或（Y）的二价基团，其中环Q是非芳族杂环， 7个环原子，包括所示的氮; L3是描述中定义的式 - （Alk1）m-（Z）n-（Alk2）p的二价连接基团; 环Ar1是任选取代的二价苯基或二价5-或6-元单环杂芳基，其中L1和H [B] sL3L2Ar2CONH-基团与相邻的环碳原子连接; 环Ar2是任选取代的1,3-亚苯基或任选取代的二价5-或6-元单环杂芳基，其中AL1Ar1NHCO-基和H [B] sL3L2-自由基与环碳原子连接，不在邻近关系; 环B如Ar 2所定义，或任选取代的环烷基，N-吡咯烷基，N-哌啶基或N-氮杂环基; s为0或1。

13. 发明申请

US20080119456A1 Substituted Thiazoleacetic Acid as Crth2 Ligands 审中-公开
标题翻译：取代噻唑乙酸作为Crth2配体
公开(公告)号：US20080119456A1
公开(公告)日：2008-05-22
申请号：US11597839
申请日：2005-05-30
申请人： Trond Ulven , Thomas Frimurer , Oystein Rist , Evi Kostenis , Thomas Hogberg , Jean-Marie Receveur , Marie Grimstrup
发明人： Trond Ulven , Thomas Frimurer , Oystein Rist , Evi Kostenis , Thomas Hogberg , Jean-Marie Receveur , Marie Grimstrup
IPC分类号： A61K31/53 , A61K31/506 , A61K31/55 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D277/30 , C07D417/04 , C07D417/06
摘要： Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is —S—, —O—, —N═N—. —NR7—, —CR7═CR8—, —CR7═N—, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group —COOH, or a carboxyl bioisostere; rings Ar2 and Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar2 and Ar3, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.
摘要翻译：式（I）化合物可用于治疗对CRTH2受体活性调节作用的疾病，例如哮喘，鼻炎，过敏性气道综合征和过敏性鼻炎支原体炎; 其中X 1是-S - ， - O - ， - N-N-。 -NR 7 - ，-CR 7 -CR 8 - ，-CR 7-N-，其中R R 7和R 8独立地是氢或C 1 -C 3烷基; A是羧基-COOH或羧基生物电子等排体; 环Ar 2和Ar 3各自独立地表示苯基或5或6元单环杂芳基环，或由5-或6-元环组成的双环系统苯并稠合或稠合到5-或6-元单环杂芳基环的碳环或杂环，所述环或环系统任选被取代; 环B如Ar 2和Ar 3所定义，或任选取代的N-吡咯烷基，N-哌啶基或N-氮杂环丁基环; s为0或1; L1，L2和L4是描述中定义的连接基团; Q 1和Q 2表示如说明书中定义的取代基。

14. 发明授权

US6153641A Pharmaceutically active compounds 失效
标题翻译：药物活性化合物
公开(公告)号：US6153641A
公开(公告)日：2000-11-28
申请号：US981003
申请日：1997-12-18
申请人： H.ang.kan Bergstrand , Thomas Hogberg , Kostas Karabelas , Anders Tunek
发明人： H.ang.kan Bergstrand , Thomas Hogberg , Kostas Karabelas , Anders Tunek
IPC分类号： A61P37/00 , C07D401/14 , C07D403/14 , C07D409/14 , C07D487/04 , A61K31/404 , C07D403/04
CPC分类号： C07D401/14 , C07D403/14 , C07D409/14 , C07D487/04
摘要： The present invention provides novel compounds of the formula (I):R.sub.20 --(CH.sub.2).sub.n --R (I)wherein:T.sub.20 is a bisindolylmaleimide moiety linked to the --(CH.sub.2).sub.n -group through an indolyl nitrogen,n is 0 or 1,R is a 5 or 6 membered aromatic carbocyclic or heterocyclic ring, the heterocyclic ring containing N or S,R is substituted by R.sub.1 and up to four of R.sub.2, R.sub.3, R.sub.4 and R.sub.5,wherein;R.sub.1 is aminomethyl, (N--(C.sub.1-4 -alkyl)amino)methyl, (N,N-di(C.sub.1-4 -alkyl)amino)methyl or pyridiniummethyl, andR.sub.2, R.sub.3, and R.sub.4 and R.sub.5 (if present), which may be the same or different, are each hydrogen, hydroxy, C.sub.1-4 -alkoxy, C.sub.1-4 -alkoxy) or halogen,or R.sub.2 when in a position contiguous to the bond connecting R to the --(CH.sub.2).sub.n -- group and n is 1 may, together with the 2-carbon atom on the indole to which the --(CH.sub.2) group is attached, form a ring,and pharmaceutically acceptable salts thereof; and the use of such compounds in medical therapy.
摘要翻译： PCT No.PCT / SE97 / 01504 Sec。 371 1997年12月18日第 102（e）1997年12月18日PCT PCT 1997年9月8日PCT公布。公开号WO98 / 11102 日期：1998年3月19日本发明提供式（I）的新化合物：R 20 - （CH 2）n R（I）其中：T 20是通过吲哚基氮连接至 - （CH 2）n - 基的双吲哚基马来酰亚胺部分，n 是0或1，R是5或6元芳族碳环或杂环，含有N或S的杂环，R被R 1和多至四个R 2，R 3，R 4和R 5取代，其中： R1是氨基甲基，（N-（C1-4 - 烷基）氨基）甲基，（N，N-二（C1-4 - 烷基）氨基）甲基或吡啶鎓甲基，R2，R3和R4以及R5（如果存在），其可以相同或不同，分别为氢，羟基，C 1-4 - 烷氧基，C 1-4 - 烷氧基）或卤素，或者当R 2连接至 - （CH 2）n - 基团和n为1可以与 - （CH 2）基团连接的吲哚上的2-碳原子一起形成环，及其药学上可接受的盐; 以及这些化合物在药物治疗中的应用。

15. 发明授权

US5908833A Colon or ileum-specific steroid derivatives 失效
标题翻译：结肠或回肠特异性类固醇衍生物
公开(公告)号：US5908833A
公开(公告)日：1999-06-01
申请号：US764985
申请日：1996-12-13
申请人： Ralph Lennart Brattsand , Peter Edman , Thomas Hogberg , Stinabritt Nilsson , Bror Arne Thalen , Jan Erik Ulmius
发明人： Ralph Lennart Brattsand , Peter Edman , Thomas Hogberg , Stinabritt Nilsson , Bror Arne Thalen , Jan Erik Ulmius
IPC分类号： A61K31/58 , A61P1/00 , A61P29/00 , C07J20060101 , C07J71/00 , A61K31/705
CPC分类号： C07J71/0031
摘要： Novel compounds which are a glucocorticosteroid (GCS) chemically bound to a sugar, having the general formulaGCS.sup.1 --O--Sugar.sup.1for colon- or ileum-specific delivery of the GCS to inflamed bowel mucosa, as well as processes for their preparation, pharmaceutical preparations containing the compounds and the use of said compounds in therapy.
摘要翻译：化学结合糖的糖皮质激素（GCS）的新型化合物，具有通式GCS1-O-糖1用于结肠或回肠特异性递送GCS至发炎肠粘膜，以及其制备方法，药物制剂含有化合物和所述化合物在治疗中的用途。

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