(3R)-3-[di(cyclobutyl)amino]-8-fluoro-3,4-dihydro-2H-chromene-5-carboxamide;2,3-dihydroxybutanedioic acid

• 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: (3R)-3-[di(cyclobutyl)amino]-8-fluoro-3,4-dihydro-2H-chromene-5-carboxamide;2,3-dihydroxybutanedioic acid
• 化学式: C22H29FN2O8
• 分子量: 468.5
• InChiKey: ZWCZKERDOMOAGZ-BTQNPOSSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.51
• 重原子数：
  33
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  171
• 氢给体数：
  5
• 氢受体数：
  10

文献信息

• [EN] A NEW SALT<br/>[FR] NOUVEAU SEL
  申请人：ASTRA AKTIEBOLAG

  公开号：WO1998054166A1

  公开（公告）日：1998-12-03

  (EN) A new salt ($i(R))-3-$i(N,N)-dicyclobutylamino-8-fluoro-3,4-dihydro-2$i(H)-1-benzopyran-5-carboxamide hydrogen tartrate, particularly the (2R,3R)-tartrate thereof, most particularly the ($i(R))-3-$i(N,N)-dicyclobutylamino-8-fluoro-3,4-dihydro-2$i(H)-1-benzopyran-5-carboxamide hydrogen (2$i(R),3$i(R))-tartrate monohydrate, processes for the manufacture of said tartrate salt, the use of the salt in medicine, the use of the tartrate salt in the manufacture of pharmaceutical formulations, and a method for the treatment of CNS disorders by administration of the tartrate salt to a host in need of such treatment.(FR) L'invention concerne un nouveau hydrogéno-tartrate de ($i(R))-3-$i(N,N)-dicyclobutylamino-8-fluoro-3,4-dihydro-2$i(H)-1-benzopyran-5-carboxamide notamment son tartrate-(2R,3R), et plus particulièrement le monohydrate de tartrate-(2$i(R),3$i(R)) hydrogéno ($i(R)-3-$i(N,N)-dicyclobutylamino-8-fluoro-3,4-dihydro-2$i(H)-1-benzopyran-5-carboxamide. L'invention concerne également des procédés de production de ce tartrate, l'utilisation de ce sel en médecine, l'utilisation du tartrate dans la production de formulations pharmaceutiques, et un procédé de traitement de troubles du système nerveux central par administration du tartrate chez un hôte nécessitant un tel traitement.

  一种新的盐（$ i（R））-3-$ i（N，N）-二环丁基氨基-8-氟-3,4-二氢-2 $ i（H）-1-苯并吡喃-5-羧酰胺氢酒石酸盐，特别是其（2R，3R）-酒石酸盐，尤其是（$ i（R））-3-$ i（N，N）-二环丁基氨基-8-氟-3,4-二氢-2 $ i（H）-1-苯并吡喃-5-羧酰胺氢（2 $ i（R），3 $ i（R））-酒石酸盐一水合物，制造该酒石酸盐的工艺，该盐在医学上的用途，该酒石酸盐在制造制药配方中的用途，以及通过向需要此类治疗的宿主给予酒石酸盐治疗中枢神经系统疾病的方法。
• TARTRATE SALTS OF (R) -3-N,N- DICYCLOBUTYLAMINO-8-FLUORO-3,4-DIHYDRO-2H-1- BENZOPYRAN-5-CARBOXAMIDE
  申请人：——

  公开号：US20030109576A1

  公开（公告）日：2003-06-12

  A new salt (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen tartrate, particularly the (2R,3R)-tartrate thereof, most particularly the (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate, processes for the manufacture of said tartrate salt, the use of the salt in medicine, the use of the tartrate salt in the manufacture of pharmaceutical formulations, and a method for the treatment of CNS disorders by administration of the tartrate salt to a host in need of such treatment.

  一种新盐(R)-3-N,N-二环丁基氨基-8-氟-3,4-二氢-2H-1-苯并吡喃-5-甲酰胺酒石酸氢盐，特别是其(2R,3R)-酒石酸盐，尤其是(R)-3-N,N-二环丁基氨基-8-氟-3,4-二氢-2H-1-苯并吡喃-5-甲酰胺酒石酸氢盐(2R,3R)一水合物、 制造所述酒石酸盐的工艺、酒石酸盐在医药中的用途、酒石酸盐在制造药物制剂中的用途，以及通过向需要治疗的宿主施用酒石酸盐来治疗中枢神经系统疾病的方法。
• Extended release oral dosage form
  申请人：——

  公开号：US20040204482A1

  公开（公告）日：2004-10-14

  The present invention relates to an extended release oral dosage form of a pharmaceutically active substance, (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide, in the form of the free base or pharmaceutically acceptable salts and/or hydrates or solvates thereof. Furthermore, the invention relates to an extended release oral dosage form that provides a defined blood concentration profile having no rapid initial rise in blood plasma concentration of said active substance when administered at low dose. The invention further relates to processes for preparing said dosage form, the use of said dosage form and a method of prevention and/or treatment of CNS disorders and related medical disturbances using said dosage form.

  本发明涉及一种药物活性物质(R)-3-N,N-二环丁氨基-8-氟-3,4-二氢-2H-1-苯并吡喃-5-甲酰胺的缓释口服剂型，其形式为游离碱或其药学上可接受的盐和/或水合物或溶剂。此外，本发明还涉及一种缓释口服剂型，该剂型可提供确定的血药浓度曲线，在低剂量给药时，所述活性物质的血浆浓度不会出现快速的初始上升。本发明还涉及制备所述剂型的工艺、所述剂型的用途以及使用所述剂型预防和/或治疗中枢神经系统紊乱及相关医疗干扰的方法。
• Tartrate salts of (R)-3-N,N-dicyclo-butylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide
  申请人：Nyqvist Hakan

  公开号：US20050085532A1

  公开（公告）日：2005-04-21

  A new salt (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen tartrate, particularly the (2R,3R)-tartrate thereof, most particularly the (R)-3-N,N-dicyclobutylamino-8-fluoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R)-tartrate monohydrate, processes for the manufacture of said tartrate salt, the use of the salt in medicine, the use of the tartrate salt in the manufacture of pharmaceutical formulations, and a method for the treatment of CNS disorders by administration of the tartrate salt to a host in need of such treatment.

  一种新盐(R)-3-N,N-二环丁基氨基-8-氟-3,4-二氢-2H-1-苯并吡喃-5-甲酰胺酒石酸氢盐，特别是其(2R,3R)-酒石酸盐，尤其是(R)-3-N,N-二环丁基氨基-8-氟-3,4-二氢-2H-1-苯并吡喃-5-甲酰胺酒石酸氢盐(2R,3R)一水合物、制造所述酒石酸盐的工艺、酒石酸盐在医药中的用途、酒石酸盐在制造药物制剂中的用途，以及通过向需要治疗的宿主施用酒石酸盐来治疗中枢神经系统疾病的方法。
• A NEW SALT
  申请人：Astra Aktiebolag

  公开号：EP0984952A1

  公开（公告）日：2000-03-15