Bromocriptinmesilat

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 麦角林及其衍生物
• 英文名称: Bromocriptinmesilat
• 英文别名: 2-bromo-α-ergocryptine methanesulphonate；2-bromo-α-ergocryptine methanesulfonate；2-Bromo-alpha-ergocryptine methane-sulfonate；[(1S,2R,4R,7S)-4-[[(6aR,9R)-5-bromo-7-methyl-6,6a,8,9-tetrahydro-4H-indolo[4,3-fg]quinoline-9-carbonyl]amino]-7-(2-methylpropyl)-5,8-dioxo-4-propan-2-yl-3-oxa-6,9-diazatricyclo[7.3.0.02,6]dodecan-2-yl] methanesulfonate
• 化学式: C₃₃H₄₂BrN₅O₇S
• 分子量: 732.696
• InChiKey: VTTPPEFVGTXKDU-BYJHUQIUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  47
• 可旋转键数：
  7
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  150
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  溴隐亭 以 丁酮 为溶剂， 生成 Bromocriptinmesilat
  参考文献：
  名称：

  Process for the preparation of 2-bromo-.alpha.-ergocryptine

  摘要：

  该发明涉及一种新的制备2-溴-α-埃尔果克里普汀及其酸盐的方法，通过在室温下使用不含超过0.02%水的二甲基亚砜-溴化氢混合物对α-埃尔果克里普汀进行溴化，如果需要，以已知方法将得到的2-溴-α-埃尔果克里普汀转化为酸盐。

  公开号：

  US04697017A1

文献信息

• Ophthalmic ointments for the treatment of glaucoma, comprising ergot alkaloids
  申请人：LEK, tovarna farmacevtskih in kemicnih izdelkov, n.sol.o.

  公开号：EP0342396A1

  公开（公告）日：1989-11-23

  There are described a novel stable ophthalmic ointment for the treatment of increased intraocular pressure in glaucoma patients, comprising a therapeutically effective amount of a peptidic ergot alkaloid of the formula wherein R₁ is hydrogen or halogen, R₂ is hydrogen or alkyl having 1 to 4 carbon atoms, and (i) R₃ is isopropyl, sec. butyl or isobutyl, R₄ is methyl, ethyl or isopropyl, and R₅ is hydrogen and R₆ is hydrogen or methoxy or R₅ and R₆ together are a single bond, or (ii) R₃ is benzyl, R₄ is methyl, R₅ is hydrogen and R₆ is hydrogen or methoxy, in the form of free base or in the form of a pharmaceutically acceptable acid addition salt, in a concentration between 0.005 and 0.05 % by weight in a topically applicable ophthal­mic pharmaceutically acceptable carrier and other excipients, the use thereof in a method for the treatment of increased intraocular pressure in glaucoma patients and a process for preparing the same.

  描述了一种用于治疗青光眼患者眼压升高的新型稳定眼膏，其中含有治疗有效量的肽麦角生物碱，其式为 其中 R₁ 是氢或卤素、 R₂ 是氢或具有 1 至 4 个碳原子的烷基，以及 (i) R₃ 是异丙基、仲丁基或异丁基、 R₄ 是甲基、乙基或异丙基，以及 R₅ 是氢，R₆ 是氢或甲氧基，或 R₅ 和 R₆ 合在一起是单键，或 (ii) R₃ 是苄基，R₄ 是甲基，R₅ 是氢，R₆ 是氢或甲氧基、 以游离碱的形式或以药学上可接受的酸加成盐的形式，在局部适用的眼科药学上可接受的载体和其他赋形剂中的浓度在 0.005 和 0.05 %（重量百分比）之间，将其用于治疗青光眼患者眼压升高的方法和制备方法。
• Processes for the preparation of pharmaceutical compositions containing bromocriptine having high stability and related products
  申请人：POLI INDUSTRIA CHIMICA S.p.A.

  公开号：EP0391374A2

  公开（公告）日：1990-10-10

  Processes for the preparation of bromocriptine tablets or capsules wherein the active ingredient is protected by inclusion in an excipient or by separated granulation of the excipients and mixing granulate wiht a mixture of the active ingredient and a excipient having low moisture content.

  制备溴隐亭片剂或胶囊的工艺，其中有效成分通过加入辅料或辅料分离制粒以及将有效成分与含水量低的辅料混合物混合制粒而得到保护。
• Method and composition for the treatment of lipid and glucose metabolism disorders
  申请人：PLIVA D.D.

  公开号：EP1776955A1

  公开（公告）日：2007-04-25

  This invention is directed to modifying or regulating in a subject of at least one of lipid and glucose metabolism by administering to a subject in need of such treatment a dopamine D1 agonist in conjunction with one agent or agent combination selected from i) a dopamine D2 agonist, ii) at least one of an adrenergic alpha1 antagonist, an adrenergic alpha2 agonist and a serotonergic inhibitor, or iii) a dopamine D2 agonist further conjoined with at least one of an adrenergic alpha1 antagonist, an adrenergic alpha2 agonist and a serotonergic inhibitor.

  本发明的目的是通过向需要治疗的受试者施用多巴胺 D1 激动剂与选自 i) 多巴胺 D2 激动剂的一种制剂或制剂组合，改变或调节受试者的脂质和葡萄糖代谢中的至少一种、肾上腺素能α1拮抗剂、肾上腺素能α2激动剂和5-羟色胺能抑制剂中的至少一种；或 iii) 多巴胺D2激动剂与肾上腺素能α1拮抗剂、肾上腺素能α2激动剂和5-羟色胺能抑制剂中的至少一种进一步结合。
• METHODS OF TREATING VASCULAR DISEASES USING BROMOCRIPTINE
  申请人：VeroScience LLC

  公开号：EP3090745A1

  公开（公告）日：2016-11-09

  The present invention is directed to a method of simultaneously treating hypertension, hypertriglyceridemia, a pro-inflammatory state, a pro-coagulative state, and insulin resistance (with or without treating obesity or endothelial dysfunction), associated with or independent from Metabolic Syndrome, as well as vascular disease such as cardiovascular, cerebrovascular, or peripheral vascular disease comprising the step of administering to a patient suffering from such disorders a therapeutically effective amount of a central acting dopamine agonist. In one embodiment, the central acting dopamine agonist is bromocriptine, optionally combined with a pharmaceutically acceptable carrier.

  本发明涉及一种同时治疗高血压、高甘油三酯血症、促炎症状态、促凝血状态和胰岛素抵抗（治疗或不治疗肥胖或内皮功能障碍）（与代谢综合征有关或无关）以及心血管、脑血管或外周血管疾病等血管疾病的方法，该方法包括向患有此类疾病的患者施用治疗有效量的中枢作用多巴胺激动剂。在一个实施方案中，中枢作用多巴胺激动剂是溴隐亭，可选择与药学上可接受的载体结合使用。
• Systems pharmacology for treating ocular disorders
  申请人：Case Western Reserve University

  公开号：US10117868B2

  公开（公告）日：2018-11-06

  A method of treating an ocular disorder in a subject includes administering to the subject subtherapeutic amounts of two or more agents that inhibit and/or blocks the activation of Gs- or Gq-protein coupled receptors or Gs- or Gq-signaling cascade in ocular cells of the subject, and/or activates Gi-protein coupled receptors, which is induced or triggered by light induced all-trans-retinal generation.

  一种治疗受试者眼部疾病的方法包括向受试者施用亚治疗量的两种或两种以上抑制和/或阻断受试者眼部细胞中 Gs 或 Gq 蛋白偶联受体或 Gs 或 Gq 信号级联激活的制剂，和/或激活 Gi- 蛋白偶联受体，这是由光诱导全反式视网膜生成诱导或触发的。