Lopac-J-4252

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: Lopac-J-4252
• 英文别名: (2-methyl-1-propylindol-3-yl)-naphthalen-2-ylmethanone
• 化学式: C₂₃H₂₁NO
• 分子量: 327.4
• InChiKey: ZNIBIJIBEXSCNO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.8
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  22
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• PHARMACEUTICAL COMPOSITIONS
  申请人：LAZZARI Paolo

  公开号：US20100216785A1

  公开（公告）日：2010-08-26

  Microemulsions of pharmaceutical compositions comprising, the following components (% by weight), the sum of the components being 100%: S) from 0.01 to 95% of one or more compounds selected from surfactants, polymers, forming organized structures as: aggregates, micelles, liquid crystals, vesicles, in the liquid in which they are solubilized, O) from 0.01 to 95% of one or more oils selected from esters of C 4 -C 32 acids or C 4 -C 32 acids, PA) from 0.001 to 90% of compounds having affinity for the CB1 and/or CB2 cannabinoidergic receptors of formula A′: AD) from 0 to 60% by weight of one or more compounds selected from modifiers of the water and/or oil polarity, modifiers of the film curvature of component S), co-surfactants, water or a saline aqueous solution the difference to 100%, wherein the ratio by weight S)/PA) is lower than that of microemulsions wherein component O) is absent.

  药物组成的微乳液包含以下组分（按重量百分比计算），各组分总和为100％：S）从0.01到95％的一种或多种化合物，选自表面活性剂、聚合物，形成有序结构，如：聚集体、胶束、液晶、囊泡，在它们被溶解的液体中，O）从0.01到95％的一种或多种油，选自C4-C32酸酯或C4-C32酸，PA）从0.001到90％的化合物，具有亲和力为公式A'的CB1和/或CB2大麻素受体，AD）从0到60％的一种或多种化合物，按重量计算，选自调节剂，水和/或油极性的调节剂，组分S）的膜曲率调节剂，共表面活性剂，水或盐水溶液之差为100％，其中按重量比S）/PA）低于不含组分O）的微乳液的比例。
• Tricyclic pyrazole derivatives and microemulsions thereof as CB1- and/or CB2-inhibitors
  申请人：Neuroscienze Pharmaness S.C. A R.L.

  公开号：EP2223913A1

  公开（公告）日：2010-09-01

  Microemulsions of pharmaceutical compositions comprising the following components (% by weight), the sum of the components being 100%: S) from 0.01 to 95% of one or more compounds selected from surfactants, polymers forming organized structures as: aggregates, micelles, liquid crystals, vesicles, in the liquid in which they are solublized, O) from 0.01 to 95% of one or more oils selected from esters of C4-C32 acids or C4-C32 acids, PA) from 0.001 to 90% of compounds having affinity for the CB1 and/or CB2 cannabinoidergic receptors of formula A': AD) from 0 to 60% by weight of one or more compounds selected from modifiers of the water and/or oil polarity, modifiers of the film curvature of component S), co-surfactants, water or a saline aqueous solution the difference to 100%, wherein the ratio by weight S)/PA) is lower than that of microemulsions wherein component O) is absent.

  医药组合物的微乳液包含以下组分（按重量百分比计），各组分之和为100%：S）从0.01到95%的一种或多种从表面活性剂、形成有序结构的聚合物，如：聚集体、胶束、液晶、囊泡，在它们溶解的液体中选择的化合物，O）从0.01到95%的一种或多种选择自C4-C32酸酯或C4-C32酸的油，PA）从0.001到90%的具有亲和力的化合物CB1和/或CB2大麻素受体的配方A'，AD）从0到60%的一种或多种选择自水和/或油极性修饰剂，成分S）的膜曲率修饰剂，共表面活性剂，水或盐水溶液的差异为100%，其中按重量比S）/PA）低于不含成分O）的微乳液。
• Pharmaceutical compounds
  申请人：Lazzari Paolo

  公开号：US20050261281A1

  公开（公告）日：2005-11-24

  Pyrazole derivatives of the following formula (I), having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: R is a group selected from: C 1 -C 10 alkyl; aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; A is a group selected from the following: an ether group of formula —(CH 2 )—O—(CH 2 ) v —R″ wherein v is equal to 1 or 2; R″ is as defined in the present application; a ketone group of formula —C(O)-Z′, wherein Z′ is as defined in the present application; a substituent having an hydroxyl function of formula —CH(OH)-Z′, Z′ being as defined in the present application; Description of the industrial invention in the name of: NEUROSCIENZE S.c. a r.l., of Italian nationality, with head office in Cagliari, via Palabanda 9.

  以下式子（I）的吡唑衍生物具有对大麻素受体CB1和/或CB2的亲和力：其中：R是以下组中选择的一组：C1-C10烷基；芳基，芳基烷基或芳基烯基，未取代或具有一个到四个取代基，相互相同或不同；A是以下组中选择的一组：化学式为—（CH2）-O-（CH2）v-R″的醚基，其中v等于1或2；R″如本申请所定义；化学式为—C（O）-Z′的酮基，其中Z′如本申请所定义；具有羟基功能的取代基，化学式为—CH（OH）-Z′，其中Z′如本申请所定义；该工业发明的描述以NEUROSCIENZE S.c. a r.l.的名义进行，该公司是意大利国籍，总部位于卡利亚里，Palabanda 9号。
• PHARMACEUTICAL COMPOUNDS
  申请人：LAZZARI Paolo

  公开号：US20090081123A1

  公开（公告）日：2009-03-26

  Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH 2 ) t —, —(CH 2 )—S(O) z —, or —S(O) z —(CH 2 )—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R′ is a group selected from the following: an ether group of formula —(CH 2 )—O—(CH 2 ) v —R″, a ketonic group of formula —C(O)-Z′, wherein Z′ is as defined below; a substituent having an hydroxyl function of formula —CH(OH)-Z′; an amide substituent of formula —C(O)—NH-T′.

  以下公式（I）的三环吡唑衍生物具有对大麻素受体CB1和/或CB2的亲和力：其中：A代表从以下一种中选择的基团：（CH2）t—、—（CH2）—S(O)z—或—S(O)z—（CH2）—，B是杂环芳基，可选地取代；R是从以下选择的基团：烷基、芳基、芳基烷基或芳基烯基，未取代或具有从一个到四个取代基，相同或不同；R'是从以下选择的基团：公式为—（CH2）—O—（CH2）v—R″的醚基团、公式为—C（O）-Z′的酮基团，其中Z′如下所定义；具有羟基功能的取代基团，其公式为—CH（OH）-Z′；公式为—C（O）—NH-T′的酰胺取代基团。
• PYRAZOLE DERIVATIVES HAVING AFFINITY FOR CB1 AND/OR CB2 RECEPTORS
  申请人：NEUROSCIENZE PHARMANESS S.C. a R.L.

  公开号：EP1602656A1

  公开（公告）日：2005-12-07

  Pyrazole derivatives of the following formula (I), having affinity for the cannabinoidergic CB1 and/or CB2 receptors:    wherein: R is a group selected from: C1-C10 alkyl; aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; A is a group selected from the following: an ether group of formula -(CH2)-O-(CH2)v-R" wherein    - v is equal to 1 or 2;    - R" is as defined in the present application; a ketone group of formula -C(O)-Z', wherein Z' is as defined in the present application; a substituent having an hydroxyl function of formula -CH(OH)-Z', Z' being as defined in the present application; an amide substituent of formula -C(O)-NH-T', T' being as defined in the present application; B is a group as defined in the present application; D is an heteroaryl optionally substituted.

  对大麻素能 CB1 和/或 CB2 受体具有亲和力的下式 (I) 吡唑衍生物： 其中 R 是选自以下各项的基团 C1-C10 烷基 芳基、芳烷基或芳烯基，未被取代或具有一至四个相互等同或不同的取代基； A 是选自以下的基团 式中的醚基-(CH2)-O-(CH2)v-R" 其中 - v 等于 1 或 2； - R "如本申请中所定义； 式-C(O)-Z'的酮基，其中 Z'如本申请中所定义； 式-CH(OH)-Z'的具有羟基官能团的取代基，其中 Z'定义如本申请所 述； 式-C(O)-NH-T'的酰胺取代基，T'如本申请中所定义； B 是本申请中所定义的基团； D 是任选取代的杂芳基。