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51. 发明申请

US20090054647A1 Method for Preparing Substituted Pyrimidines 有权
标题翻译：取代嘧啶的制备方法
公开(公告)号：US20090054647A1
公开(公告)日：2009-02-26
申请号：US11886653
申请日：2006-05-12
申请人： Gary David Annis
发明人： Gary David Annis
IPC分类号： C07D239/42
CPC分类号： C07D239/42 , C07D239/30 , C07D239/36
摘要： Disclosed a method for preparing a compound of Formula 1, wherein R1 is cyclopropyl, 4-chlorophenyl or 4-bromophenyl; and R2 is C1-C14 alkyl; comprising contacting a compound of Formula 2 with a persulfate oxidant in the presence of a strong sulfur- or phosphorus-containing mineral acid and an oxidation resistant solvent. Also disclosed are methods for preparing the compound of Formula 2 from a compound of Formula 5 as well as compounds of Formula 6 and salts thereof, wherein R is NH2, Cl or OH; X is H or Cl; R1 is cyclopropyl, 4-chlorophenyl or 4-bromophenyl; and R2 is C1-C14 alkyl; provided that when R is NH2 or Cl, then X is Cl; which are useful a process intermediates.
摘要翻译：公开了制备式1化合物的方法，其中R 1是环丙基，4-氯苯基或4-溴苯基; R2为C1-C14烷基; 包括在强硫或磷的无机酸和抗氧化溶剂的存在下使式2的化合物与过硫酸盐氧化剂接触。还公开了从式5化合物制备式2化合物的方法以及式6化合物及其盐，其中R是NH 2，Cl或OH; X是H或Cl; R1是环丙基，4-氯苯基或4-溴苯基; R2为C1-C14烷基; 条件是当R为NH 2或Cl时，则X为Cl; 这是一个有用的过程中间体。

52. 发明授权

US07491728B2 Pyrimidinone compounds as calcilytics 失效
标题翻译：嘧啶酮化合物作为钙质
公开(公告)号：US07491728B2
公开(公告)日：2009-02-17
申请号：US10552363
申请日：2004-04-07
申请人： Irina V. Shcherbakova , Manuel F. Balanddrin , Guangfei Huang , Otto Geoffroy , John Fox , Robert Marquis , Dennis Shinji Yamashita , Juan Luengo , Wenyong Wang
发明人： Irina V. Shcherbakova , Manuel F. Balanddrin , Guangfei Huang , Otto Geoffroy , John Fox , Robert Marquis , Dennis Shinji Yamashita , Juan Luengo , Wenyong Wang
IPC分类号： A61K31/517 , A61K31/50 , C07D403/14 , C07D239/30 , C07D239/46 , A61P35/00
CPC分类号： C07D239/36 , C07D239/70 , C07D239/91 , C07D401/04
摘要： The pyrimidinone compounds are disclosed. Methods of preparing the pyrimidinone compounds are also disclosed.
摘要翻译：公开了嘧啶酮化合物。还公开了制备嘧啶酮化合物的方法。

53. 发明授权

US07348334B2 Monocyclic derivatives of aryl alkanoic acids and their use in medicine: process for their preparation and pharmaceutical compositions containing them 失效
标题翻译：芳基链烷酸的单环衍生物及其在医药中的应用：其制备方法和含有它们的药物组合物
公开(公告)号：US07348334B2
公开(公告)日：2008-03-25
申请号：US10119300
申请日：2002-04-08
申请人： Javed Iqbal , Gurram Ranga Madhavan , Saibal Kumar Das , Debnath Bhunia , Ranjan Chakrabarti , Ramanujam Rajagopalan
发明人： Javed Iqbal , Gurram Ranga Madhavan , Saibal Kumar Das , Debnath Bhunia , Ranjan Chakrabarti , Ramanujam Rajagopalan
IPC分类号： A61K31/506 , C07D239/22
CPC分类号： C07D239/36
摘要： The present invention relates to novel hypolipidemic, antihyperglycemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel β-aryl-α-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
摘要翻译：本发明涉及新型降血脂，抗高血糖化合物，其衍生物，其类似物，其互变异构形式，其立体异构体，其多晶型物，其药学上可接受的盐，其药学上可接受的溶剂化物和含有它们的药学上可接受的组合物。更具体地，本发明涉及通式（I）的新型β-芳基-α-氧代取代的烷基羧酸，其衍生物，它们的类似物，其互变异构形式，它们的立体异构体，它们的多晶型物，其药学上可接受的盐，它们的药学上可接受的溶剂合物和含有它们的药学上可接受的组合物。

54. 发明授权

US07217712B2 4-Substituted-5-cyano-1H-pyrimidin-6-(thi)ones as GSK-3 inhibitors 失效
标题翻译： 4-取代的5-氰基-1H-嘧啶-6-（thi）的GSK-3抑制剂
公开(公告)号：US07217712B2
公开(公告)日：2007-05-15
申请号：US10799507
申请日：2004-03-12
申请人： Young-Choon Moon
发明人： Young-Choon Moon
IPC分类号： C07D239/36 , C07D239/56 , C07D405/04 , A61K31/513
CPC分类号： C07D239/36 , C07D239/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D417/04
摘要： The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various GSK-3-mediated disorders, such as diabetes and Alzheimer's disease.
摘要翻译：本发明涉及可用作GSK-3抑制剂的式I化合物。本发明还涉及使用式I化合物或包含式I化合物的药物组合物抑制GSK-3活性的方法。本发明还提供了利用这些化合物和药物组合物治疗和预防各种GSK-3介导的疾病如糖尿病和阿尔茨海默氏病的方法。

55. 发明申请

US20070037822A1 Azinone and diazinone V3 inhibitors for depression and stress disorders 失效
标题翻译：氮嗪酮和二嗪酮V3抑制剂用于抑郁和应激障碍
公开(公告)号：US20070037822A1
公开(公告)日：2007-02-15
申请号：US11422710
申请日：2006-06-07
申请人： Jeffrey Letourneau , Koc-Kan Ho , Michael Ohlmeyer , Patrick Jokiel , Christopher Riviello
发明人： Jeffrey Letourneau , Koc-Kan Ho , Michael Ohlmeyer , Patrick Jokiel , Christopher Riviello
IPC分类号： A61K31/513 , A61K31/4965 , A61K31/4412 , C07D213/63 , C07D239/02
CPC分类号： C07D213/82 , C07D239/26 , C07D239/36 , C07D241/24 , C07D295/088 , C07D403/04 , C07D403/12 , C07D413/04
摘要： Substituted pyridines, pyrimidines, pyrazines, pyridinones, pyrimidinones, pyrazinones and phenylacetamides useful in treating depression, stress and other disorders are disclosed. The compounds are of the formualae: Other embodiments are also disclosed.
摘要翻译：公开了用于治疗抑郁症，压力和其它疾病的取代的吡啶，嘧啶，吡嗪，吡啶酮，嘧啶酮，吡嗪酮和苯乙酰胺。化合物是形式：其他实施方案也被公开。

57. 发明申请

US20060111303A1 Diketohydrazine derivative compounds and drugs contaiing the compounds as the active ingredient 失效
标题翻译：二酮肼衍生物化合物和化合物作为活性成分的药物
公开(公告)号：US20060111303A1
公开(公告)日：2006-05-25
申请号：US10512348
申请日：2003-04-24
申请人： Akira Hatayama , Hitoshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
发明人： Akira Hatayama , Hitoshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
IPC分类号： A61K38/04 , C07K5/04
CPC分类号： C07D209/48 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/4152 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/429 , C07C243/34 , C07C251/76 , C07C251/84 , C07C251/86 , C07C2601/08 , C07C2601/14 , C07D207/22 , C07D207/50 , C07D209/46 , C07D211/28 , C07D211/72 , C07D211/86 , C07D211/98 , C07D213/70 , C07D213/76 , C07D213/77 , C07D213/78 , C07D233/38 , C07D233/52 , C07D233/80 , C07D239/10 , C07D239/18 , C07D239/36 , C07D241/08 , C07D241/18 , C07D263/26 , C07D263/28 , C07D265/08 , C07D265/10 , C07D265/33 , C07D275/02 , C07D275/03 , C07D275/06 , C07D277/18 , C07D277/36 , C07D277/50 , C07D277/54 , C07D277/60 , C07D277/82 , C07D279/02 , C07D279/06 , C07D279/12 , C07D285/10 , C07D285/16 , C07D309/04 , C07D309/28 , C07D335/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D513/10 , C07F9/59 , C07F9/65583 , Y02A50/411
摘要： The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
摘要翻译：本发明涉及式（I）的二酮肼衍生物及其药学上可接受的盐（式中的符号具有与说明书中所述相同的含义）。式（I）化合物对半胱氨酸蛋白酶具有抑制活性，可用于治疗炎性疾病，免疫疾病，缺血性疾病，呼吸系统疾病，循环系统疾病，血液病，神经元疾病，肝或胆道疾病，骨质或关节疾病，代谢疾病等。该化合物对弹性蛋白酶具有抑制活性，也可用于治疗慢性阻塞性肺疾病（慢性障碍性肺疾病）。

58. 发明申请

US20060089500A1 New monocyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them 失效
公开(公告)号：US20060089500A1
公开(公告)日：2006-04-27
申请号：US11296749
申请日：2005-12-07
申请人： Ranga Gurram , Venkateswarlu Akella , Rajagopalan Ramanujam , Ranjan Chakrabarti , Parimal Misra , Vidya Lohray , Braj Lohray , Rao Paraselli
发明人： Ranga Gurram , Venkateswarlu Akella , Rajagopalan Ramanujam , Ranjan Chakrabarti , Parimal Misra , Vidya Lohray , Braj Lohray , Rao Paraselli
IPC分类号： A61K31/513 , C07D239/02
CPC分类号： C07D239/36 , C07C217/22 , C07C237/32 , C07C247/04 , C07D239/90
摘要： The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel β-aryl-α-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds, their analogs, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them. The present invention also relates to novel intermediates, processes for their preparation and their use in the preparation of compounds of formula (I).

59. 发明申请

US20050234051A1 5-Substituted 2-aryl-4 pyrimidinones 失效
标题翻译： 5-取代的2-芳基-4-嘧啶酮
公开(公告)号：US20050234051A1
公开(公告)日：2005-10-20
申请号：US11147895
申请日：2005-06-07
申请人： Kevin Hodgetts , Dario Doller
发明人： Kevin Hodgetts , Dario Doller
IPC分类号： G01N33/50 , A61J1/14 , A61K31/513 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P1/04 , A61P1/12 , A61P1/14 , A61P3/04 , A61P5/14 , A61P9/04 , A61P9/12 , A61P15/08 , A61P17/06 , A61P19/02 , A61P25/18 , A61P25/22 , A61P25/24 , A61P29/00 , A61P37/08 , A61P43/00 , C07D239/34 , C07D239/36 , C07D239/46 , C07D239/47 , C07D239/52 , C12Q1/02 , G01N33/15 , G01N33/58 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号： C07D239/36 , C07D239/47 , C07D239/52
摘要： Arylpyrimidinone compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：提供作为CRF 1受体的选择性调节剂的芳基嘧啶酮化合物。这些化合物可用于治疗许多中枢神经系统和周围疾病，特别是压力，焦虑，抑郁，心血管疾病和进食障碍。还提供了治疗这种疾病以及包装的药物组合物的方法。本发明的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。给出了在受体定位研究中使用化合物的方法。

60. 发明申请

US20050171355A1 Pyridine derivative production method 有权
标题翻译：吡啶衍生物的制备方法
公开(公告)号：US20050171355A1
公开(公告)日：2005-08-04
申请号：US11046743
申请日：2005-02-01
申请人： Hirokazu Kuwabara , Chang Zhang , Hiromitsu Saitoh , Takayuki Sonoda
发明人： Hirokazu Kuwabara , Chang Zhang , Hiromitsu Saitoh , Takayuki Sonoda
IPC分类号： C07D213/06 , C07D213/09 , C07D213/16 , C07D213/22 , C07D213/26 , C07D213/38 , C07D213/61 , C07D213/65 , C07D213/78 , C07D213/80 , C07D213/84 , C07D213/85 , C07D221/04 , C07D239/36 , C07D239/40 , C07D239/42 , C07D213/08
CPC分类号： C07D221/04 , C07D213/08 , C07D213/16 , C07D213/22 , C07D213/26 , C07D213/65 , C07D213/80 , C07D213/84 , C07D213/85 , C07D239/36 , C07D239/42
摘要： A method in which a pyridinium derivative such as 1,3-dimethyl-2,3-dihydro-2-oxopyrimidinium chloride is reacted with an acetyl compound such as 4-acetylpyridine, and then the reaction product is reacted with ammonia or an ammonium salt.
摘要翻译：其中将诸如1,3-二甲基-2,3-二氢-2-氧代嘧啶鎓氯化物的吡啶鎓衍生物与诸如4-乙酰基吡啶的乙酰基化合物反应的方法，然后将反应产物与氨或铵盐。

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