(2Z,5Z)-N-(2-{4-[(5-{[2-(cyclopropylcarbonylamino)(1,3-thiazol-5-yl)]methylene}-4-oxo(1,3-thiazolidin-2-ylidene))azamethyl]-3-methylphenoxy}ethyl)-N-methylmethoxycarboxamide | 1253209-29-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: (2Z,5Z)-N-(2-{4-[(5-{[2-(cyclopropylcarbonylamino)(1,3-thiazol-5-yl)]methylene}-4-oxo(1,3-thiazolidin-2-ylidene))azamethyl]-3-methylphenoxy}ethyl)-N-methylmethoxycarboxamide
• 英文别名: methyl N-[2-[4-[[(5Z)-5-[[2-(cyclopropanecarbonylamino)-1,3-thiazol-5-yl]methylidene]-4-oxo-1,3-thiazolidin-2-ylidene]amino]-3-methylphenoxy]ethyl]-N-methylcarbamate
• CAS: 1253209-29-8
• 化学式: C₂₃H₂₅N₅O₅S₂
• 分子量: 515.614
• InChiKey: KOMCXACAGVQVIE-WQRHYEAKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  35
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  176
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• THIAZOLIDINONE DERIVATIVE
  申请人：Irie Takayuki

  公开号：US20110190299A1

  公开（公告）日：2011-08-04

  An object of the present invention is to provide thiazolidinone derivatives. More specifically, an object of the present invention is to provide novel compounds having a CDC7 inhibitory action. The present invention provides thiazolidinone derivatives represented by the formula (I) The compounds of the present invention inhibit the CDC7 protein kinase activity, and suppress cell proliferation.

  本发明的目的是提供噻唑烷酮衍生物。更具体地，本发明的目的是提供具有CDC7抑制作用的新化合物。本发明提供由式(I)表示的噻唑烷酮衍生物。本发明的化合物抑制CDC7蛋白激酶活性，并抑制细胞增殖。
• NOVEL 1-(BIPHENYL-4-YL-METHYL)-1H-IMIDAZOLE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING SAME
  申请人：Miura Toru

  公开号：US20120264753A1

  公开（公告）日：2012-10-18

  Disclosed is a novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative represented by general formula (I), which has both angiotensin II receptor antagonist activity and PPAR-γ activating activity and is useful as a prophylactic and/or therapeutic agent for cardiovascular diseases and metabolic diseases. Also disclosed is a pharmaceutical composition which contains the novel 1-(biphenyl-4-yl-methyl)-1H-imidazole derivative. In general formula (I), ring A represents a group represented by formula (II) or (III); R 1 represents a C 1-6 alkyl group; R 2 represents a C 1-6 alkyl group which may be substituted by a hydroxy group, or a group represented by formula —CO—R 4 (wherein R 4 represents a hydroxy group, a C 1-6 alkoxy group, an amino group, a mono(C 1-6 alkyl)amino group, a di(C 1-6 alkyl)amino group, a morpholino group, a piperidino group or a pyrrolidino group); R 3 represents a halogen atom or a C 1-6 alkoxy group; and X and Y may be the same or different and each represents a nitrogen atom or CH.

  揭示了一种由通式（I）表示的新型1-(联苯基-4-基甲基)-1H-咪唑衍生物，具有血管紧张素II受体拮抗活性和PPAR-γ激活活性，并可用作心血管疾病和代谢性疾病的预防和/或治疗剂。还揭示了一种含有这种新型1-(联苯基-4-基甲基)-1H-咪唑衍生物的药物组合物。在通式（I）中，环A代表由式（II）或（III）表示的基团；R1代表C1-6烷基基团；R2代表可以被羟基取代的C1-6烷基基团，或者由式—CO—R4（其中R4代表羟基、C1-6烷氧基、氨基、单(C1-6烷基)氨基、二(C1-6烷基)氨基、吗啉基、哌啶基或吡咯基）表示的基团；R3代表卤素原子或C1-6烷氧基团；X和Y可以相同也可以不同，每个代表氮原子或CH。
• Suppository and composition comprising at least one polyethylene glycol
  申请人：Anestic ApS

  公开号：US20020048601A1

  公开（公告）日：2002-04-25

  There is provided a suppository comprising at least one biocompatible polymer, wherein the biocompatible polymer is essentially non-biodegradable, and wherein the suppository essentially does not swell when contacted with an aqueous fluid. The suppository may further comprise a plurality of open cells at least partly separated from one another by an interpenetrating matrix comprising at least one biocompatible polymer in branched or crosslinked form. The plurality of interlinked, open cells are capable of containing an aqueous fluid, and the permeability of the suppository ensures that entry of body fluids into the open cells under practical circumstances occurs essentially without dehydration of mucousal membrane tissue contacting the suppository. The suppository furthermore preferably comprises a controlled release formulation.

  提供了一种含有至少一种生物相容性聚合物的栓剂，其中该生物相容性聚合物基本上不可生物降解，且当与水性液体接触时，该栓剂基本上不膨胀。该栓剂还可以进一步包括多个开放单元，这些单元至少部分地由相互穿插的基质分隔开，该基质包含至少一种分支或交联形式的生物相容性聚合物。这些互相连接的开放单元能够包含水性液体，而栓剂的渗透性确保体液进入开放单元时，在实际情况下基本上不会导致接触栓剂的粘膜组织脱水。此外，该栓剂最好包含控制释放配方。
• Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the phophylaxis and treatment of disorders related thereto
  申请人：Jones M. Robert

  公开号：US20070155763A1

  公开（公告）日：2007-07-05

  The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及公式（I）的某些三取代芳基和杂环芳基衍生物，它们是代谢调节剂。因此，本发明的化合物在预防或治疗代谢性疾病及其并发症方面是有用的，如糖尿病和肥胖症。
• N-[(piperazinyl)hetary]arylsulfonamide compounds with affinity for the dopamine d3 receptor
  申请人：Braje Wilfried

  公开号：US20070054918A1

  公开（公告）日：2007-03-08

  The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula (I) in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents R a which is/are selected, independently of each other, from halogen, CN, NO 2 , CO 2 R 4 , COR 5 , C 1 —C 4 -alkyl and C 1 —C 4 -haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents R b , which is/are selected from halogen, NO 2 , CN, CO 2 R 4 , COR 5 , C 1 —C 6 -alkyl, C 2 —C 6 -alkenyl, C 2 —C 6 -alkynyl, C 3 —C 6 -cycloalkyl, C 3 —C 6 -cycloalkyl-C 1 —C 4 -alkyl and C 1 —C 4 -haloalkyl, with it also being possible for two radicals R b which are bonded to adjacent C atoms of Ar to be together C 3 —C 4 -alkylene; R 1 is hydrogen, C 1 —C 4 -alkyl, C 1 —C 4 -haloalkyl, C 3 —C 6 -cycloalkyl, C 3 —C 6 -cycloalkyl-C 1 —C 4 -alkyl, C 1 —C 4 -hydroxyalkyl, C 1 —C 4 -alkoxy-C 1 —C 4 -alkyl, C 3 —C 4 -alkenyl or C 3 —C 4 -alkynyl; with the radicals n, R 1 , R 2 , R 3 , R 4 and R 5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropriate together with physiologically acceptable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D 3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.

  本发明涉及一般式（I）中的N-[(哌嗪基)杂芳基]芳基磺酰胺化合物，其中Q是一个双价的6元杂环芳基基团，其具有1或2个N原子作为环成员，并且可选地携带一个或两个取代基Ra，该取代基独立地选择自卤素、CN、NO2、CO2R4、COR5、C1-C4烷基和C1-C4卤代烷基；Ar是苯基或一个6元杂环芳基基团，其具有1或2个N原子作为环成员，并且可选地携带一个或两个取代基Rb，该取代基独立地选择自卤素、 、CN、CO2R4、COR5、C1-C6烷基、C2-C6烯基、C2-C6炔基、C3-C6环烷基、C3-C6环烷基-C1-C4烷基和C1-C4卤代烷基，其中还可能有两个与Ar相邻的C原子结合的Rb基团共同成为C3-C4烷基；R1是氢、C1-C4烷基、C1-C4卤代烷基、C3-C6环烷基、C3-C6环烷基-C1-C4烷基、C1-C4羟基烷基、C1-C4烷氧基-C1-C4烷基、C3-C4烯基或C3-C4炔基；具有在专利权要求中给出的含义的基团n、R1、R2、R3、R4和R5，以及这些化合物的N-氧化物和生理上耐受的酸加合盐，以及包含至少一种在权利要求1到10中要求的N-[(哌嗪基)杂芳基]芳基磺酰胺化合物和/或一种I的生理上耐受的酸加合盐和/或I的N-氧化物的制药组合物，如有必要，还包括用于治疗对多巴胺D3受体拮抗剂或激动剂影响有反应的疾病的生理上可接受的载体和/或辅助物质，特别是用于治疗中枢神经系统疾病和肾功能障碍。