N-(1-methyl-1H-indazol-4-yl)-N'-[(4R)-8-(trifluoromethyl)-3,4-dihydro-2H-chromen-4-yl]urea | 1144501-94-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: N-(1-methyl-1H-indazol-4-yl)-N'-[(4R)-8-(trifluoromethyl)-3,4-dihydro-2H-chromen-4-yl]urea
• 英文别名: 1-(1-methylindazol-4-yl)-3-[(4R)-8-(trifluoromethyl)-3,4-dihydro-2H-chromen-4-yl]urea
• CAS: 1144501-94-9
• 化学式: C₁₉H₁₇F₃N₄O₂
• 分子量: 390.365
• InChiKey: AKNOZIFJWLJPFN-OAHLLOKOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  28
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  68.2
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• [EN] TRPV1 ANTAGONISTS<br/>[FR] ANTAGONISTES DE TRPV1
  申请人：ABBOTT LAB

  公开号：WO2010045402A1

  公开（公告）日：2010-04-22

  Disclosed herein are compounds of formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

  本文披露了式（I）的化合物，或其药用可接受的盐、溶剂化合物、前药、前药的盐或它们的组合，其中R1、R2、R3、R4和m在规范中有定义。还披露了包含这种化合物的组合物以及使用这种化合物和组合物治疗疾病和疾病的方法。
• 11-Beta-Hydroxysteroid Dehydrogenase Inhibitors
  申请人：Vicker Nigel

  公开号：US20090042929A1

  公开（公告）日：2009-02-12

  There is provided a compound having Formula (I) R 1 -Z-R 2 wherein R 1 is a group selected from optionally substituted fused polycyclic groups, substituted alkyl groups, branched alkyl groups, and optionally substituted cycloalkyl groups Z is a linker which is or comprises a carbonyl group or a isostere of a carbonyl group R 2 is selected from optionally substituted aromatic rings and optionally substituted heterocyclic rings wherein (a) R 2 is a 2-substituted thiophene group, and/or (b) Z is a group of the formula —C(═O)—CR 3 R 4 —X—(CR 5 R 6 )n-, wherein X is selected from NR 7 , S, O, S═O, and S(═O) 2 , wherein n is 0 or 1 and/or (c) R 1 is an adamantyl group and Z is or comprises an amide group, and/or (d) R 1 is an adamantyl group and Z is or comprises a group of the formula —(CR 8 R 9 )p-NR 10 —S(═O) 2 —(CR 11 R 12 )q-, wherein p is 0 or 1 and q is 0 or 1 and/or (e) R 1 is an adamantyl group and Z is or comprises a group of the formula —(CR 13 R 14 )V—Y—(CR 15 R 16 )W— where Y is a heteroaryl group in which a bond in the heteroaryl ring is a isostere of a carbonyl group, wherein v is o or 1 and w is 0 or 1; wherein each of R 3 , R 4 , R 5 , R 6 , R 8 , R 9 , R 11 , R 12 , R 13 , R 14 , R 15 and R 16 , are independently selected from H, hydrocarbyl and halogen, wherein each of R 7 and R 10 are independently selected from H and hydrocarbyl.

  提供一种化合物，其化学式为(I) R1-Z-R2，其中R1是选自可选取代的融合多环基团、取代的烷基基团、支链烷基基团和可选取代的环烷基基团的基团；Z是一个连接基团，可以是或包含一个羰基基团或一个羰基基团的同分异构体；R2是选自可选取代的芳香环和可选取代的杂环；其中(a) R2是2-取代噻吩基团，和/或(b) Z是一个化学式为—C(═O)—CR3R4—X—(CR5R6)n-的基团，其中X选自NR7、S、O、S═O和S(═O)2，n为0或1，和/或(c) R1是一个金刚烷基团，Z是或包含一个酰胺基团，和/或(d) R1是一个金刚烷基团，Z是或包含一个化学式为—(CR8R9)p-NR10—S(═O)2—(CR11R12)q-的基团，其中p为0或1，q为0或1，和/或(e) R1是一个金刚烷基团，Z是或包含一个化学式为—(CR13R14)V—Y—(CR15R16)W—的基团，其中Y是一个杂环基团，在杂环环中的一个键是羰基基团的同分异构体，v为0或1，w为0或1；其中R3、R4、R5、R6、R8、R9、R11、R12、R13、R14、R15和R16各自独立地选自H、烃基和卤素，R7和R10各自独立地选自H和烃基。
• TRPV1 ANTAGONISTS
  申请人：Gomtsyan Arthur R.

  公开号：US20100120846A1

  公开（公告）日：2010-05-13

  Disclosed herein are compounds of formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R 1 , R 2 , R 3 , R 4 , and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

  本文揭示了式(I)的化合物，或其药学上可接受的盐、溶剂、前药盐、前药的盐或其组合物，其中R1、R2、R3、R4和m在规范中被定义。还揭示了包含这些化合物的组合物以及使用这些化合物和组合物治疗疾病和病症的方法。
• Compound
  申请人：Vicker Nigel

  公开号：US20100120789A1

  公开（公告）日：2010-05-13

  There is provided a compound having Formula I R 1 —Z—R 2 Formula I wherein R 1 is a group selected from optionally substituted fused polycyclic groups, substituted alkyl groups, branched alkyl groups, and optionally substituted cycloalkyl groups Z is a linker which is or comprises a carbonyl group or a isostere of a carbonyl group R 2 is selected from optionally substituted aromatic rings and optionally substituted heterocyclic rings wherein (a) R 2 is a 2-substituted thiophene group, and/or (b) Z is a group of the formula —C(═O)—CR 3 R 4 —X—(CR 5 R 6 )n-, wherein X is selected from NR 7 , S, O, S═O, and S(═O) 2 , wherein n is 0 or 1 and/or (c) R 1 is an adamantyl group and Z is or comprises an amide group, and/or (d) R 1 is an adamantyl group and Z is or comprises a group of the formula —(CR 8 R 9 )p- NR 10 —S(═O) 2 —(CR 11 R 12 )q-, wherein p is 0 or 1 and q is 0 or 1 and/or (e) R 1 is an adamantyl group and Z is or comprises a group of the formula —(CR 13 R 14 )v-Y—(CR 15 R 16 )w- where Y is a heteroaryl group in which a bond in the heteroaryl ring is a isostere of a carbonyl group, wherein v is o or 1 and w is 0 or 1; wherein each of R 3 , R 4 , R 5 , R 6 , R 8 , R 9 , R 11 , R 12 , R 13 , R 14 , R 15 and R 16 , are independently selected from H, hydrocarbyl and halogen, wherein each of R 7 and R 10 are independently selected from H and hydrocarbyl.

  提供了一种具有IR1-Z-R2式的化合物，其中： R1是从可选取代的融合多环基团，取代的烷基基团，分支烷基基团和可选取代的环烷基基团中选择的基团； Z是或包括一个羰基或羰基的同分异构体的连接基团； R2是从可选取代的芳香环和可选取代的杂环中选择的基团，其中 (a) R2是2-取代噻吩基团，和/或 (b) Z是公式-C（═O）-CR3R4-X-（CR5R6）n-的基团，其中X从NR7，S，O，S═O和S（═O）2中选择，n为0或1，和/或 (c) R1是金刚烷基团，Z是或包括酰胺基团，和/或 (d) R1是金刚烷基团，Z是或包括公式-CR8R9p-NR10-S（═O）2-（CR11R12）q-的基团，其中p为0或1，q为0或1，和/或 (e) R1是金刚烷基团，Z是或包括公式（CR13R14）v-Y-（CR15R16）w-的基团，其中Y是杂环基团，其中杂环环中的一个键是羰基的同分异构体，v为0或1，w为0或1； 其中R3，R4，R5，R6，R8，R9，R11，R12，R13，R14，R15和R16中的每一个独立选择自H，烃基和卤素，其中R7和R10各自独立选择自H和烃基。
• SOLID DISPERSION PRODUCT CONTAINING N-ARYL UREA-BASED COMPOUND
  申请人：Schroeder Rudolf

  公开号：US20090143423A1

  公开（公告）日：2009-06-04

  A solid dispersion product comprising at least one N-aryl urea-based pharmaceutically active agent or an agent of related structural type is obtained by a) preparing a liquid mixture containing the at least one active agent, at least one pharmaceutically acceptable matrix-forming agent, at least one pharmaceutically acceptable surfactant and at least one solvent, and b) removing the solvent(s) from the liquid mixture to obtain the solid dispersion product.

  通过a)制备含有至少一种N-芳基脲基药物活性剂或相关结构类型的药剂学活性剂的固体分散产品，包括制备液体混合物，其中包含至少一种活性剂、至少一种药学上可接受的基质形成剂、至少一种药学上可接受的表面活性剂和至少一种溶剂，然后b)从液体混合物中去除溶剂，以获得固体分散物。