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    Novel pharmaceutical compositions having an antidiabetic action, and process for their preparation
    12.
    发明申请
    Novel pharmaceutical compositions having an antidiabetic action, and process for their preparation 审中-公开
    具有抗糖尿病作用的新型药物组合物及其制备方法

    公开(公告)号：US20040039031A1

    公开(公告)日：2004-02-26

    申请号：US10432386

    申请日：2003-05-21

    发明人： Nathalie Cugnardey ,  Nicolas Wiernsperger

    IPC分类号： A61K031/44 ,  A61K031/403 ,  A61K031/175

    CPC分类号： A61K31/155 ,  A61K31/64 ,  A61K2300/00

    摘要： The present invention relates to the field of therapeutic chemistry and more particularly to the preparation of novel medicinal products for treating diabetes. Specifically, a subject of the invention is novel antidiabetic medicinal products consisting of a combination of two active principles that are effective via the oral route, at subliminal doses, formed from an antidiabetic biguanide and an antidiabetic sulfonamide, in combination or as a mixture with one or more inert, pharmaceutically acceptable excipients. The invention also relates to a process for the preparation of such medicinal products formed from a biguanide and a sulfonamide.

    摘要翻译： 本发明涉及治疗化学领域，更具体地涉及用于治疗糖尿病的新药用产品的制备。 具体地说，本发明的主题是新的抗糖尿病药物产品，其组合是通过口服途径有效的两种活性成分组合的，由起义剂量由抗糖尿病双胍类和抗糖尿病性磺酰胺组合形成，或与一种 或更多惰性的药学上可接受的赋形剂。 本发明还涉及由双胍和磺酰胺形成的这种药物的制备方法。

    Combinations comprising dipeptidylpeptidase-iv inhibitor
    14.
    发明申请
    Combinations comprising dipeptidylpeptidase-iv inhibitor 审中-公开
    包括二肽基肽酶-IV抑制剂的组合

    公开(公告)号：US20030139434A1

    公开(公告)日：2003-07-24

    申请号：US10181169

    申请日：2002-10-10

    发明人： Bork Balkan ,  Thomas Edward Hughes ,  David Grenville Holmes ,  Edwin Bernard Villhauer

    IPC分类号： A61K038/28 ,  A61K031/506 ,  A61K031/4439 ,  A61K031/426 ,  A61K031/401 ,  A61K031/365 ,  A61K031/195 ,  A61K031/28 ,  A61K031/175

    CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/4025 ,  A61K31/44 ,  A61K31/505 ,  A61K2300/00

    摘要： The invention relates to a combination which comprises a DPP-IV inhibitor and at least one further antidiabetic compound, preferably selected from the group consisting of insulin signalling pathway modulators, like inhibitors of protein tyrosine phosphatases (PTPases), non-small molecule mimetic compounds and inhibitors of glutamine-fructose-6-phosphate amidotransferase (GFAT), compounds influencing a dysregulated hepatic glucose production, like inhibitors of glucose-6-phosphatase (G6Pase), inhibitors of fructose-1,6-bisphosphatase (F-1,6-BPase), inhibitors of glycogen phosphorylase (GP), glucagon receptor antagonists and inhibitors of phosphoenolpyruvate carboxykinase (PEPCK), pyruvate dehydrogenase kinase (PDHK) inhibitors, insulin sensitivity enhancers, insulin secretion enhancers, null-glucosidase inhibitors, inhibitors of gastric emptying, insulin, and null2-adrenergic antagonists, for simultaneous, separate or sequential use in the prevention, delay of progression or treatment of conditions mediated by dipeptidylpeptidase-IV (DPP-IV), in particular diabetes, more especially type 2 diabetes mellitus, conditions of impaired glucose tolerance (IGT), conditions of impaired fasting plasma glucose, metabolic acidosis, ketosis, arthritis, obesity and osteoporosis; and the use of such combination for the cosmetic treatment of a mammal in order to effect a cosmetically beneficial loss of body weight.

    摘要翻译： 本发明涉及包含DPP-IV抑制剂和至少一种另外的抗糖尿病化合物的组合，其优选选自胰岛素信号通路调节剂，如蛋白酪氨酸磷酸酶（PTPases）的抑制剂，非小分子模拟化合物和 谷氨酰胺 - 果糖-6-磷酸酰胺转移酶（GFAT）的抑制剂，影响失调的肝脏葡萄糖产生的化合物，如葡萄糖-6-磷酸酶（G6Pase）的抑制剂，果糖-1,6-二磷酸酶抑制剂（F-1,6- BPA），糖原磷酸化酶（GP）的抑制剂，胰高血糖素受体拮抗剂和磷酸烯醇丙酮酸羧激酶（PEPCK），丙酮酸脱氢酶激酶（PDHK）抑制剂，胰岛素敏感性增强剂，胰岛素分泌增强剂，α-葡糖苷酶抑制剂，胃排空抑制剂，胰岛素 和α2-肾上腺素能拮抗剂，用于同时，分开或顺序用于预防，延缓进展或治疗 由二肽基肽酶-IV（DPP-IV）介导的病症，特别是糖尿病，尤其是2型糖尿病，葡萄糖耐量降低的病症（IGT），空腹血浆葡萄糖受损的病症，代谢性酸中毒，酮症，关节炎，肥胖和骨质疏松症 ; 以及使用这种组合来进行哺乳动物的美容治疗，以实现美容上有益​​的体重损失。

    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
    18.
    发明申请
    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 失效
    碳环和杂环取代的缩氨基脲和缩氨基硫脲和其用途

    公开(公告)号：US20020061886A1

    公开(公告)日：2002-05-23

    申请号：US10003249

    申请日：2001-12-06

    申请人： CoCensys, Inc.

    发明人： Yan Wang ,  Sui Xiong Cai ,  John FW Keana

    IPC分类号： A61K031/535 ,  A61K031/495 ,  A61K031/445 ,  A61K031/175

    CPC分类号： C07D213/643 ,  A61K31/17 ,  A61K31/175 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61K31/505 ,  C07C281/12 ,  C07C281/14 ,  C07C2601/14 ,  C07D209/14 ,  C07D211/46 ,  C07D213/68 ,  C07D215/12 ,  C07D307/91 ,  C07D309/12 ,  C07D317/50 ,  C07D317/58 ,  C07D317/62 ,  C07D317/64 ,  C07D319/18

    摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: 1 or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.

    摘要翻译： 本发明涉及由式I表示的碳环和杂环取代的缩氨基脲和缩氨基硫脲或其药学上可接受的盐或前药，其中：Y是氧或硫; R1，R21，R22和R23独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基; 或R 22和R 23与N一起形成杂环; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR 24，CR 25 R 26，C（O），NR 24 C（O），C（O）NR 24，SO，SO 2或共价键; 其中R 24，R 25和R 26独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。 本发明还涉及使用碳环和杂环取代的缩氨基脲和缩氨基硫脲来治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS），用于治疗和预防 涉及谷氨酸毒性和治疗，预防或改善疼痛，作为抗惊厥药，以及作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病和尿失禁的抗疟药抑制剂。

    Solid oral dosage form of metformin and glyburide and the method of preparation thereof
    19.
    发明申请
    Solid oral dosage form of metformin and glyburide and the method of preparation thereof 审中-公开
    二甲双胍和格列本脲的固体口服剂型及其制备方法

    公开(公告)号：US20040175421A1

    公开(公告)日：2004-09-09

    申请号：US10794993

    申请日：2004-03-05

    发明人： Suresh Kumar Gidwani ,  Purushottam Sharshikant Singnurkar

    IPC分类号： A61K031/175 ,  A61K031/155 ,  A61K031/535

    CPC分类号： A61K31/155 ,  A61K9/167 ,  A61K9/2077 ,  A61K9/2866 ,  A61K31/64 ,  A61K2300/00

    摘要： The present invention relates to a simple and easy method for the preparation of solid oral dosages of the combination of metformin and glyburide. Specifically, glyburide is homogenized in an organic solution whereby about 8 to 15% w/w of glyburide goes into solution and form a slurry. The resulted slurry is then sprayed onto pharmaceutical excipients or metformin granules, and the solid oral dosage of metformin and glyburide is formed. The present invention further relates to the solid oral dosages prepared by the disclosed process, and the method of treating non-insulin dependent diabetes by administering to a patient in need thereof a solid oral dosage prepared by the current invention.

    摘要翻译： 本发明涉及一种用于制备二甲双胍和格列本脲组合的固体口服剂量的简单和容易的方法。 具体地，将格列本脲在有机溶液中匀化，由此约8至15％w / w的格列本脲进入溶液并形成浆料。 然后将得到的浆液喷雾到药物赋形剂或二甲双胍颗粒上，形成二甲双胍和格列本脲的固体口服剂量。 本发明还涉及通过公开的方法制备的固体口服剂量以及通过向有需要的患者施用本发明制备的固体口服剂量来治疗非胰岛素依赖型糖尿病的方法。