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1. 发明授权

US08895743B2 Methysergide derivatives 有权
标题翻译：甲基海马衍生物
公开(公告)号：US08895743B2
公开(公告)日：2014-11-25
申请号：US14134114
申请日：2013-12-19
申请人： Map Pharmaceuticals, Inc.
发明人： Libo Wu , Jian Zhang
IPC分类号： C07D457/06 , C07D457/04 , C07D471/06
CPC分类号： C07D471/06 , C07D457/06
摘要： Provided herein are novel methysergide derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders or symptoms thereof, such as, migraine and Parkinson's disease using the compounds and compositions disclosed herein. In still other embodiments, provided herein, such as, for example, are methods for antagonizing the 5-HT2B receptor without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein such as, for example, are methods of agonizing the 5-HT1A receptor using the compounds and compositions disclosed herein.
摘要翻译：本文提供了新颖的甲基麦芽糖衍生物及其组合物。在其它实施方案中，本文提供了使用本文公开的化合物和组合物治疗，预防或改善各种医学病症或其症状（例如偏头痛和帕金森病）的方法。在本文提供的其它实施方案中，例如，是使用本文公开的化合物和组合物来拮抗5-HT 2B受体而不激发5-HT 2B受体的方法。在其它实施方案中，本文提供的例如是使用本文公开的化合物和组合物来激发5-HT 1A受体的方法。

2. 发明申请

US20110137035A1 PREPARATION OF MICROBIOLOGICALLY PRODUCED ERGOT ALKALOIDS 审中-公开
标题翻译：微生物生产的ERGOT ALKALOIDS的制备
公开(公告)号：US20110137035A1
公开(公告)日：2011-06-09
申请号：US13001876
申请日：2009-06-26
申请人： Stephan Bertel
发明人： Stephan Bertel
IPC分类号： C07D457/04
CPC分类号： C12P17/183 , C07D457/04
摘要： The present invention relates to a method for preparing microbiologically produced ergot alkaloids of the following formula (I), comprising the step of: a) extracting the fermentation product occurring during the biological production, said product containing at least one ergot alkaloid of formula (I), at a pH of 8-14 using an extractant with a solubility in water of 0.2 g/100 g of water to 25 g/100 g water at 20° C., wherein the amount of extractant is sufficient to form a 2-phase system together with the fermentation product.
摘要翻译：本发明涉及一种制备下式（I）的微生物生产的麦角生物碱的方法，包括以下步骤：a）提取在生物生产过程中发生的发酵产物，所述产物含有至少一种式（I ），pH为8-14，使用在20℃下具有0.2g / 100g水的溶解度至25g / 100g水的萃取剂，其中萃取剂的量足以形成2- 相系统与发酵产物。

3. 发明授权

US5654313A Method for modifying or regulating the glucose metabolism of an animal or human subject 失效
标题翻译：用于修饰或调节动物或人受试者的葡萄糖代谢的方法
公开(公告)号：US5654313A
公开(公告)日：1997-08-05
申请号：US465674
申请日：1995-06-06
申请人： Anthony H. Cincotta , Albert H. Meier
发明人： Anthony H. Cincotta , Albert H. Meier
IPC分类号： A61K31/00 , A61K31/13 , A61K31/137 , A61K31/15 , A61K31/166 , A61K31/195 , A61K31/221 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/405 , A61K31/435 , A61K31/439 , A61K31/445 , A61K31/4515 , A61K31/454 , A61K31/46 , A61K31/475 , A61K31/48 , A61K31/496 , A61K31/54 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/695 , A61K38/22 , A61K45/00 , A61K45/06 , A61P3/06 , A61P3/08 , A61P3/10 , C07D457/00 , C07D457/04 , G01N33/74 , A61K31/44 , A61K31/495
CPC分类号： G01N33/74 , A61K31/00 , A61K31/13 , A61K31/137 , A61K31/15 , A61K31/166 , A61K31/195 , A61K31/221 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/405 , A61K31/435 , A61K31/439 , A61K31/445 , A61K31/4515 , A61K31/454 , A61K31/46 , A61K31/475 , A61K31/48 , A61K31/496 , A61K31/4985 , A61K31/54 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/695 , A61K38/2257 , A61K45/06 , Y10S514/866 , Y10S514/909
摘要： A process for the long term modification and regulation of lipid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species. The dopamine agonist is administered at the time of, or just after the time of peak plasma prolactin concentration found in lean animals of the same species and the prolactin stimulator is administered at a time just before the plasma prolactin rhythm reaches its peak in lean animals. Insulin resistance, and hyperinsulinemia or hyperglycemia, or both, can also be controlled in humans on a long term basis by treatment corresponding to that of the treatment for obesity. The short term daily injections reset hormonal timing in the neural centers of the brain to produce long term effects.
摘要翻译：长期改变和调节脂质和葡萄糖代谢的过程 - 通常通过给脊椎动物施用来减少肥胖，胰岛素抵抗和高胰岛素血症或高血糖或两者（这些是非胰岛素依赖型或II型糖尿病的标志）动物或人类的多巴胺激动剂和催乳素刺激剂。多巴胺激动剂和催乳素刺激剂分别以每天的剂量施用，取决于类似物种的脂肪和瘦成员的正常昼夜节律。基于妊娠峰值催乳素的昼夜节律，峰值催乳素和糖皮质激素峰值，为类似物种的瘦胰岛素敏感成分建立的血液水平，以每日定时序列治疗肥胖物种的身体脂肪沉积物的减少。多巴胺激动剂在同一物种的瘦动物中发现的血浆催乳素浓度峰值之前或之后施用，并且在等离子体催乳素节律在瘦动物中达到峰值之前的时间施用催乳素刺激剂。胰岛素抵抗和高胰岛素血症或高血糖或两者也可以通过与肥胖症治疗相对应的治疗长期控制。短期每日注射在脑神经中枢复位激素时间产生长期效应。

4. 发明授权

US5554623A Method for the long term reduction of body fat stores, insulin resistance, hypersinsulinemia and hyperglycemia in vertebrates 失效
标题翻译：长期减少身体脂肪储存的方法，胰岛素抵抗，高胰岛素血症和脊椎动物高血糖
公开(公告)号：US5554623A
公开(公告)日：1996-09-10
申请号：US249808
申请日：1994-05-26
申请人： Anthony H. Cincotta , Albert H. Meier
发明人： Anthony H. Cincotta , Albert H. Meier
IPC分类号： A61K31/00 , A61K31/13 , A61K31/137 , A61K31/15 , A61K31/166 , A61K31/195 , A61K31/221 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/405 , A61K31/435 , A61K31/439 , A61K31/445 , A61K31/4515 , A61K31/454 , A61K31/46 , A61K31/475 , A61K31/48 , A61K31/496 , A61K31/54 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/695 , A61K38/22 , A61K45/00 , A61K45/06 , A61P3/06 , A61P3/08 , A61P3/10 , C07D457/00 , C07D457/04 , G01N33/74 , A61K31/44
CPC分类号： G01N33/74 , A61K31/00 , A61K31/13 , A61K31/137 , A61K31/15 , A61K31/166 , A61K31/195 , A61K31/221 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/405 , A61K31/435 , A61K31/439 , A61K31/445 , A61K31/4515 , A61K31/454 , A61K31/46 , A61K31/475 , A61K31/48 , A61K31/496 , A61K31/4985 , A61K31/54 , A61K31/5415 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/695 , A61K38/2257 , A61K45/06 , Y10S514/866 , Y10S514/909
摘要： A process for the long term modification and regulation of lipid and glucose metabolism--generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these being the hallmarks of noninsulin dependent, or Type II diabetes)--by administration to a vertebrate, animal or human, of a dopamine agonist and a prolactin stimulator. The dopamine agonist and prolactin stimulator are administered in daily dosages, respectively, at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean insulin sensitive members of a similar species. The dopamine agonist is administered at the time of, or just after the time of peak plasma prolactin concentration found in lean animals of the same species and the prolactin stimulator is administered at a time just before the plasma prolactin rhythm reaches its peak in lean animals. Insulin resistance, and hyperinsulinemia or hyperglycemia, or both, can also be controlled in humans on a long term basis by treatment corresponding to that of the treatment for obesity. The short term daily injections reset hormonal timing in the neural centers of the brain to produce long term effects.
摘要翻译：长期改变和调节脂质和葡萄糖代谢的过程 - 通常通过给脊椎动物施用来减少肥胖，胰岛素抵抗和高胰岛素血症或高血糖或两者（这些是非胰岛素依赖型或II型糖尿病的标志）动物或人类的多巴胺激动剂和催乳素刺激剂。多巴胺激动剂和催乳素刺激剂分别以每天的剂量施用，取决于类似物种的脂肪和瘦成员的正常昼夜节律。基于妊娠峰值催乳素的昼夜节律，峰值催乳素和糖皮质激素峰值，为类似物种的瘦胰岛素敏感成分建立的血液水平，以每日定时序列治疗肥胖物种的身体脂肪沉积物减少。多巴胺激动剂在同一物种的瘦动物中发现的血浆催乳素浓度峰值之前或之后施用，并且在等离子体催乳素节律在瘦动物中达到峰值之前的时间施用催乳素刺激剂。胰岛素抵抗和高胰岛素血症或高血糖或两者也可以通过与肥胖症治疗相对应的治疗长期控制。短期每日注射在脑神经中枢复位激素时间产生长期效应。

5. 发明授权

US4914107A Method for selectively blocking 5-HT.sub.2 receptors 失效
标题翻译：选择性阻断5-HT2受体的方法
公开(公告)号：US4914107A
公开(公告)日：1990-04-03
申请号：US297208
申请日：1989-01-17
申请人： Marlene L. Cohen , Mark J. Goldberg , Louis Lemberger
发明人： Marlene L. Cohen , Mark J. Goldberg , Louis Lemberger
IPC分类号： C07D457/04 , A61K31/48 , A61P9/08 , A61P9/12 , A61P25/04 , A61P25/06 , A61P25/24 , A61P25/26 , A61P43/00
CPC分类号： A61K31/48
摘要： This invention relates to the use in vivo of 1-isopropyldihydrolysergic acid as a 5-HT.sub.2 antagonist.

6. 发明授权

US4782063A Ergoline esters useful as serotonin antagonists 失效
标题翻译：可用作5-羟色胺拮抗剂的二甘油酯
公开(公告)号：US4782063A
公开(公告)日：1988-11-01
申请号：US48166
申请日：1987-05-11
申请人： William L. Garbrecht , Gifford P. Marzoni , Pawel Fludzinski
发明人： William L. Garbrecht , Gifford P. Marzoni , Pawel Fludzinski
IPC分类号： A61K31/475 , A61P7/02 , A61P9/08 , A61P9/12 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/24 , A61P25/26 , A61P35/00 , A61P43/00 , C07D457/04 , A61K31/48
CPC分类号： C07D457/04
摘要： The present invention provides novel bicyclic ergoline esters useful as serotonin antagonists.

7. 发明授权

US4713384A Selective method for blocking 5HT.sub.2 receptors 失效
公开(公告)号：US4713384A
公开(公告)日：1987-12-15
申请号：US782338
申请日：1985-10-01
申请人： Marlene L. Cohen , Ray W. Fuller , William L. Garbrecht , Kathleen R. Whitten
发明人： Marlene L. Cohen , Ray W. Fuller , William L. Garbrecht , Kathleen R. Whitten
IPC分类号： C07D457/04 , A61K31/48 , A61P9/08 , A61P9/12 , A61P25/04 , A61P25/18 , A61P25/24 , A61P25/26 , A61P43/00
CPC分类号： A61K31/48
摘要： Method of blocking 5HT without effect on alpha receptors with 1-loweralkyl-6-straight chain alkyl-8.beta.-hydroxycycloalkyloxycarbonylergolines.

8. 发明授权

US4683236A Cycloalkanol esters of dihydrolysergic acid useful as 5Ht.sub.2 receptor antagonists 失效
标题翻译：用作5Ht2受体拮抗剂的二氢山梨酸的环烷醇酯
公开(公告)号：US4683236A
公开(公告)日：1987-07-28
申请号：US782337
申请日：1985-10-01
申请人： Kathleen R. Whitten , William L. Garbrecht , Gifford P. Marzoni , C. John Parli
发明人： Kathleen R. Whitten , William L. Garbrecht , Gifford P. Marzoni , C. John Parli
IPC分类号： C07D457/04 , A61K31/48
CPC分类号： C07D457/04
摘要： Cycloalkyl or ketocycloalkyl esters of 1-substituted-6-C.sub.1-4 straight chain alkyl (or allyl)-ergoline-8.beta.-carboxylic acids, useful as 5HT.sub.2 receptor antagonists.
摘要翻译：可用作5HT2受体拮抗剂的1-取代-6-C 1-4直链烷基（或烯丙基） - 麦角灵-8β-羧酸的环烷基或酮环烷基酯。

9. 发明授权

US4491664A Process for the production of ergot alkaloids 失效
标题翻译：麦角生物碱生产工艺
公开(公告)号：US4491664A
公开(公告)日：1985-01-01
申请号：US357526
申请日：1982-03-12
申请人： Wolfgang Oppolzer
发明人： Wolfgang Oppolzer
IPC分类号： C07D209/08 , C07D209/10 , C07D209/14 , C07D209/18 , C07D311/94 , C07D457/04 , C07F9/6561 , C07D457/00
CPC分类号： C07D457/04 , C07D209/08 , C07D209/10 , C07D209/14 , C07D209/18 , C07D311/94 , C07F9/6561
摘要： A process for the production of an ergot alkaloid comprising intramolecularly cyclizing a 3-iminoethyl-4-trans-buta-1',3'-dienylindole to produce an 8-ergolene and as necessary converting the resultant ergolene into the desired ergot alkaloid.
摘要翻译：一种生产麦角生物碱的方法，其包括使3-亚氨基乙基-4-反式丁基-1'，3'-二烯基吲哚分子内环化以产生8-熟麦醇，并且根据需要将所得的白屈麦烯转化为所需的麦角生物碱。

10. 发明授权

US4348392A 8.alpha.-Substituted ergoline-I derivatives 失效
标题翻译： 8α-取代的麦角灵-I衍生物
公开(公告)号：US4348392A
公开(公告)日：1982-09-07
申请号：US189295
申请日：1980-09-22
申请人： Theodor Fehr , Paul Stadler , Peter Stutz
发明人： Theodor Fehr , Paul Stadler , Peter Stutz
IPC分类号： C07D457/02 , C07D457/04 , C07D457/12 , A61K31/48
CPC分类号： C07D457/04 , C07D457/02 , C07D457/12
摘要： This invention provides new compounds of formula I, ##STR1## wherein X is hydrogen, chlorine or bromine,R.sub.1 is methyl or ethyl, andR.sub.2 is CH.sub.2 --CN, or a group NR.sub.3 R.sub.4, whereinR.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms, andR.sub.4 is SO.sub.2 R.sub.5, wherein R.sub.5 is alkyl of 1 to 4 carbon atoms, mono- to tri-halogenalkyl of 1 to 4 carbon atoms, phenyl, pyridyl, phenyl monosubstituted by halogen or alkoxy of 1 to 4 carbon atoms, or a group NR.sub.6 R.sub.7, wherein each ofR.sub.6 and R.sub.7 is independently hydrogen or alkyl of 1 to 4 carbon atoms, orR.sub.6 and R.sub.7 together are one of the groups (CH.sub.2).sub.n or (CH.sub.2).sub.2 --A--(CH.sub.2).sub.2, whereinn is a number from 3 to 7, andA is oxygen, sulphur or nitrogen substituted by alkyl of 1 to 4 carbon atoms or phenyl,useful as prolactin secretion agents and antiparkinson agents.
摘要翻译：本发明提供了新的式I化合物，其中X是氢，氯或溴，R1是甲基或乙基，R2是CH2-CN，或NR3R4基团，其中R3是氢或1-4个碳原子的烷基碳原子，R 4为SO 2 R 5，其中R 5为1至4个碳原子的烷基，1至4个碳原子的一至三卤代烷基，苯基，吡啶基，被卤素或1-4个碳原子的烷氧基取代的苯基，或基团NR 6 R 7，其中R 6和R 7各自独立地为氢或1至4个碳原子的烷基，或者R 6和R 7一起为（CH 2）n或（CH 2）2 -A-（CH 2）2基团之一，其中 n为3至7的数，A为氧，硫或被1至4个碳原子的烷基取代的氮或苯基，可用作催乳激素分泌剂和抗帕金森药剂。

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