2-(1-Ethenylcyclobutyl)acetic acid | 1245649-55-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-(1-Ethenylcyclobutyl)acetic acid
• CAS: 1245649-55-1
• 化学式: C₈H₁₂O₂
• 分子量: 140.18
• InChiKey: WYXFZXIHQCPNJL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  10
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Novel 4-(2-furoyl) aminopiperidines, intermediates in synthesizing the same, process for producing the same and medicinal use of the same
  申请人：Fukutomi Ryuuta

  公开号：US20050085508A1

  公开（公告）日：2005-04-21

  There are provided novel 4-(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is CH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH 2 or NH; W is O or S; T is O or N—R 15 wherein R 15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R 1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxycarbonyl group, or the like. The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.

  提供了一种新的4-(2-呋喃酰基)氨基哌啶化合物，其通式表示为(I)，以及它们的合成中间体、制备过程和含有它们的药物。 在上述式中，X为CH或N，Y为以下通式(II)、式(II-a)或式(III)的基团： 其中a、b和c均为0-6的整数；Z为CH2或NH；W为O或S；T为O或N—R15，其中R15为H、C1-C6烷基、苄基或苯乙基；R1为H、C1-C6烷氧羰基、苄氧羰基或类似基团。本发明所述的4-(2-呋喃酰基)氨基哌啶衍生物具有阿片μ受体拮抗活性，可用于治疗或预防由μ受体激动剂引起的副作用，包括便秘、恶心/呕吐或瘙痒，或用于治疗或预防特发性便秘、术后肠梗阻、麻痹性肠梗阻、肠易激综合征或慢性瘙痒。
• Novel 4-(2-furoyl) aminopiperidienes, intermediates for synthesizing the same, processes for preparing the same and medicinal use of the same
  申请人：Fukutomi Ryuuta

  公开号：US20080194826A1

  公开（公告）日：2008-08-14

  A compound represented the general formula (V): wherein X is CH or N; and Y a is a group of the general formula selected from:

  一个化合物的一般式表示为(V)：其中X是CH或N; 而Y是从一般式中选择的一个基团：
• NOVEL 4-(2FUROYL)AMINOPIPERIDINES, INTERMEDIATES IN SYNTHESIZING THE SAME, PROCESS FOR PRODUCING THE SAME AND MEDICINAL USE OF THE SAME
  申请人：Kyorin Pharmaceutical Co., Ltd.

  公开号：EP1443046A1

  公开（公告）日：2004-08-04

  There are provided novel 4-(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is CH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III):    wherein    a, b and c are each an integer of 0-6;    Z is CH2 or NH;    W is O or S;    T is O or N-R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and    R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxycarbonyl group, or the like. The 4-(2-furoyl) aminopiperidine derivatives according to this invention possess opioid µ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by µ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.

  本发明提供了由通式(I)代表的新型 4-(2-呋喃基)氨基哌啶类化合物、其合成中间体、制备工艺以及含有这些化合物的药物。 在上式中，X 是 CH 或 N，Y 是下式（II）、式（II-a）或式（III）的基团： 其中 a、b 和 c 各为 0-6 的整数； Z 是 CH2 或 NH W 是 O 或 S； T 是 O 或 N-R15，其中 R15 是 H、C1-C6 烷基、苄基或苯乙基；以及 R1 是 H、C1-C6 烷氧基羰基、苄氧基羰基或类似基团。 根据本发明的 4-(2-呋喃基)氨基哌啶衍生物具有阿片μ拮抗活性，可用于治疗或预防由μ受体激动剂引起的副作用，这些副作用可选自便秘、恶心/呕吐或瘙痒，或用于治疗或预防特发性便秘、术后回肠梗阻、麻痹性回肠梗阻、肠易激综合征或慢性瘙痒。
• 3-CARBAMOYL-2-PYRIDONE DERIVATIVE
  申请人：SHIONOGI & CO., LTD.

  公开号：EP1806342A1

  公开（公告）日：2007-07-11

  The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1 is optionally substituted C1-C8 alkyl and the like; R2 is C1-C6 alkyl; R3 is C1-C6 alkyl and the like; or R2 and R3 taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R4 is hydrogen and the like; G is a group selected from the groups shown by the formula an the like: wherein R5 is hydrogen and the like; X1 is a single bond and the like; X2 is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of -O-, or -N(R6)-, wherein R6 is hydrogen and the like, and the like; X3 is a single bond and the like; a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.

  本发明提供了对大麻素受体具有激动活性的化合物，该受体由式 (I) 表示： 其中 R1 是任选取代的 C1-C8 烷基及类似物；R2 是 C1-C6 烷基；R3 是 C1-C6 烷基及类似物；或 R2 和 R3 一起可形成任选取代的 5 至 10 个成员的非芳香族碳环；R4 是氢及类似物；G 是选自式所示基团及类似物的基团： 其中 R5 是氢和类似物；X1 是单键和类似物；X2 是可被一个或两个基团-O-或-N(R6)-取代的任选取代的 C1-C8 亚烷基，其中 R6 是氢和类似物；X3 是单键和类似物； 其药学上可接受的盐或溶液，以及药物组合物、特应性皮炎治疗剂和止痒剂，尤其是口服和外用的止痒剂，其中每一种都含有上述化合物作为活性成分。
• US7375115B2
  申请人：——

  公开号：US7375115B2

  公开（公告）日：2008-05-20