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公开(公告)号：JP2012153690A
公开(公告)日：2012-08-16
申请号：JP2012035313
申请日：2012-02-21
发明人： O'NEIL JAMES DENNEN , BAMAT MICHAEL K , VON BORSTEL REID W , SHARMA SHALINI , ARUDCHANDRAN RAMACHANDRAN
IPC分类号： A61K31/192 , A61K31/216 , A61K45/00 , A61P9/00 , A61P9/12 , A61P13/12 , A61P19/06 , A61P25/28 , A61P35/00 , A61P43/00 , C07C65/24 , C07C65/26 , C07C65/40
CPC分类号： C07C59/68 , A23G3/36 , A23G3/38 , A23G3/42 , A23G3/48 , A23G3/563 , A61K8/498 , A61K9/0056 , A61K31/192 , A61K31/216 , A61K31/352 , A61K31/704 , A61K45/06 , A61Q11/00 , C07C59/66 , C07C59/84 , C07C59/88 , C07C59/90 , C07C61/39 , C07C69/716 , C07C69/734 , C07C69/738 , C07C2601/02
摘要： PROBLEM TO BE SOLVED: To provide new medications that can safely, conveniently and effectively treat and prevent disorders related to elevation of blood uric acid such as disorders due to urate crystals such as gouty arthritis, and diseases related to pathological effect of soluble uric acid such as cardiovascular and renal diseases.SOLUTION: A compound of Formula I or a pharmaceutically acceptable salt thereof is used for treating or preventing a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, and early-onset essential hypertension, or the like.
摘要翻译： 要解决的问题：提供可以安全，方便和有效地治疗和预防与尿酸升高相关的疾病的新药物，例如由于诸如痛风性关节炎的尿酸盐晶体引起的疾病，以及与可溶性的病理作用相关的疾病 尿酸如心血管和肾脏疾病。 解决方案：式I化合物或其药学上可接受的盐用于治疗或预防多种病症，包括痛风，高尿酸血症，升高的尿酸水平，其不符合常规证明高尿酸血症诊断的依据，肾脏 功能障碍，肾结石，心血管疾病，发展心血管疾病的风险，肿瘤溶解综合征，认知障碍和早发性原发性高血压等。 版权所有（C）2012，JPO＆INPIT
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公开(公告)号：JP2009227690A
公开(公告)日：2009-10-08
申请号：JP2009161269
申请日：2009-07-07
IPC分类号： A61K31/00 , C07C59/68 , A61K31/16 , A61K31/165 , A61K31/192 , A61K31/198 , A61K31/216 , A61K31/235 , A61K31/27 , A61K31/381 , A61K31/41 , A61K31/4196 , A61K31/4402 , A61K31/445 , A61K31/535 , A61K31/54 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/00 , A61P9/10 , A61P9/12 , A61P13/12 , A61P17/02 , A61P25/00 , A61P27/12 , C07C51/09 , C07C51/347 , C07C51/41 , C07C59/54 , C07C59/90 , C07C67/343 , C07C69/738 , C07C213/08 , C07C217/22 , C07C227/18 , C07C229/36 , C07C231/02 , C07C231/12 , C07C233/47 , C07C235/34 , C07C235/58 , C07C235/78 , C07C235/84 , C07C237/32 , C07C259/06 , C07C319/20 , C07C323/47 , C07C323/52 , C07C323/58 , C07C323/59 , C07C323/60 , C07D213/30 , C07D213/55 , C07D249/10 , C07D249/12 , C07D257/04 , C07D333/16 , C07D333/22
CPC分类号： C07B41/12 , A01N37/10 , A61K31/165 , A61K31/192 , A61K31/216 , A61K31/235 , A61K31/41 , A61K31/4196 , A61K31/44 , A61K31/445 , A61K31/535 , A61K31/54 , C07C59/68 , C07C59/90 , C07C67/47 , C07C69/738 , C07C209/68 , C07C217/22 , C07C233/31 , C07C233/47 , C07C235/78 , C07C235/84 , C07C259/06 , C07C323/52 , C07C323/59 , C07C2601/02 , C07C2601/04 , C07C2602/04 , C07D213/30 , C07D213/55 , C07D249/10 , C07D249/12 , C07D257/04 , C07D333/16 , C07D333/24 , Y10S514/866
摘要： PROBLEM TO BE SOLVED: To provide a compound useful for treating various metabolic disorders such as insulin-resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis, and arteriosclerosis. SOLUTION: The compound is a medical agent, which is a biologically active agent, is represented by the following formula or is a pharmaceutically receptible salt of the above represented compound. In the formula, n is 1 or 2; m is 0 or 1; q is 0 or 1; t is 0 or 1; R 9 is hydrogen, halo-, or 1-3C alkoxy; and X is -CH 2 - and Q is -OR 1 , or X is -CH 2 CR 12 CR 13 - or CH 2 CH(NHAc)- and Q is OR 1 , or X is -CH 2 CH 2 - and Q is NR 10 R 11 . COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译： 待解决的问题：提供可用于治疗各种代谢紊乱如胰岛素抵抗综合征，糖尿病，高脂血症，脂肪肝疾病，恶病质，肥胖症，动脉粥样硬化和动脉硬化的化合物。 解决方案：该化合物是药剂，其为生物活性剂，由下式表示，或为上述化合物的药学上可接受的盐。 在该式中，n为1或2; m为0或1; q为0或1; t为0或1; R 9是氢，卤素或1-3C烷氧基; 并且X是-CH 2 SB 2 - 且Q是-OR 1，或者X是-CH 2， 或者CH
2 CH（NHAc） - 和Q是OR SP 1，或X是-CH 2 SB SB > CH 2 - 并且Q是NR 10 R 11 。 版权所有（C）2010，JPO＆INPIT -
3.发明专利Method of decreasing toxicity of chemotherapy agent and antivirus agent by acylated pyrimidine nucleoside 审中-公开通过酰基吡嗪核苷降低化学药剂和抗病毒药物的毒性的方法
公开(公告)号：JP2009167213A
公开(公告)日：2009-07-30
申请号：JP2009110077
申请日：2009-04-28
IPC分类号： A61K31/7068 , A61K31/7115 , A61K31/505 , A61K31/513 , A61K31/515 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/712 , A61K45/06 , A61P35/00 , A61P39/02 , C07D237/02 , C07D239/00 , C07H19/06 , C07H19/067 , C07H19/10
CPC分类号： A61K45/06 , A61K31/513 , A61K31/515 , A61K31/70 , A61K31/7068 , A61K31/7072 , C07H19/06 , C07H19/10 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide a method of effectively preventing or treating toxic symptoms by antivirus or anticancer chemotherapy including disorder in the haematopoietic system and gastrointestinal mucosa but not limited to them, a compound and a method for enabling administration of a higher dosage of chemotherapy agent, and a method of preventing or improving disorders in gastrointestinal epithelium by a cell poison chemotherapy agent. SOLUTION: This method of treating a cancer includes a process (a) for administering at least over 1.5 times the ordinary maximum tolerable dosage of pyrimidine nucleoside homologue, and a process (b) for administering a pharmaceutically effective quantity of an acyl-derivative of non-methylated pyrimidine nucleoside. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译： 待解决的问题：提供通过抗病毒或抗癌化学疗法有效预防或治疗有毒症状的方法，包括造血系统和胃肠粘膜中的紊乱，但不限于此，化合物和使得能够施用更高的方法 化疗剂的剂量，以及通过细胞毒化学治疗剂预防或改善胃肠上皮细胞紊乱的方法。 治疗癌症的方法包括给予至少超过常规最大可耐受剂量的嘧啶核苷同系物的1.5倍以上的方法（a）和（b）用于施用药学上有效量的酰基 - 非甲基化嘧啶核苷衍生物。 版权所有（C）2009，JPO＆INPIT
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公开(公告)号：JP2009221232A
公开(公告)日：2009-10-01
申请号：JP2009161270
申请日：2009-07-07
IPC分类号： A61K31/00 , A61K31/192 , A61K31/16 , A61K31/165 , A61K31/198 , A61K31/216 , A61K31/235 , A61K31/27 , A61K31/381 , A61K31/41 , A61K31/4196 , A61K31/4402 , A61K31/445 , A61K31/535 , A61K31/54 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P7/00 , A61P9/10 , A61P9/12 , A61P13/12 , A61P17/02 , A61P25/00 , A61P27/02 , A61P27/12 , A61P35/00 , C07C59/54 , C07C59/68 , C07C59/90 , C07C69/738 , C07C217/22 , C07C233/47 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C259/06 , C07C323/47 , C07C323/52 , C07C323/59 , C07C323/60 , C07D213/30 , C07D213/55 , C07D249/10 , C07D249/12 , C07D257/04 , C07D333/16 , C07D333/18 , C07D333/22
CPC分类号： C07B41/12 , A01N37/10 , A61K31/165 , A61K31/192 , A61K31/216 , A61K31/235 , A61K31/41 , A61K31/4196 , A61K31/44 , A61K31/445 , A61K31/535 , A61K31/54 , C07C59/68 , C07C59/90 , C07C67/47 , C07C69/738 , C07C209/68 , C07C217/22 , C07C233/31 , C07C233/47 , C07C235/78 , C07C235/84 , C07C259/06 , C07C323/52 , C07C323/59 , C07C2601/02 , C07C2601/04 , C07C2602/04 , C07D213/30 , C07D213/55 , C07D249/10 , C07D249/12 , C07D257/04 , C07D333/16 , C07D333/24 , Y10S514/866
摘要： PROBLEM TO BE SOLVED: To provide useful compounds for treatments of various metabolic disturbances (for example, insulin resistant syndromes, diabetes mellitus, hyperlipidemia, fatty liver diseases, cachexia, obesity, atherosclerosis and arterial sclerosis). SOLUTION: Biologically active drugs, namely the drugs are compounds shown by formula I or their pharmaceutically acceptable salts, wherein n represents 1 or 2, m represents 0 or 1, q represents 0 or 1, t represents 0 or 1, R 9 represents a hydrogen, a halogen or 1-3C alkoxy, X represents -CH 2 - and Q represents -OR 1 , or X represents -CH 2 CR 12 CR 13 - or -CH 2 CH(NHAc)- and Q represents -OR 1 , or X represents -CH 2 CH 2 - and Q represents NR 10 R 11 . COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译： 要解决的问题：为治疗各种代谢紊乱（例如胰岛素抵抗综合征，糖尿病，高脂血症，脂肪肝疾病，恶病质，肥胖症，动脉粥样硬化和动脉硬化症）提供有用的化合物。 解决方案：生物活性药物，即药物是式I所示的化合物或其药学上可接受的盐，其中n表示1或2，m表示0或1，q表示0或1，t表示0或1，R
9表示氢，卤素或1-3C烷氧基，X表示-CH 2 SB 2 - ，Q表示-OR SP 1，或X表示 -CH 2 SB 2（CH 2） - 或-CH 2 SBR（NHAc） - 并且Q表示-OR 或者X代表-CH 2，而且Q代表NR SP 10， / SP>。 版权所有（C）2010，JPO＆INPIT -
公开(公告)号：JP2013129665A
公开(公告)日：2013-07-04
申请号：JP2013043951
申请日：2013-03-06
IPC分类号： A61K31/00 , A61K31/192 , A61K31/16 , A61K31/165 , A61K31/198 , A61K31/216 , A61K31/235 , A61K31/27 , A61K31/381 , A61K31/41 , A61K31/4196 , A61K31/4402 , A61K31/445 , A61K31/535 , A61K31/54 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/50 , A61P7/00 , A61P9/10 , A61P9/12 , A61P13/12 , A61P17/02 , A61P25/00 , A61P27/00 , A61P27/12 , A61P43/00 , C07C59/54 , C07C59/68 , C07C59/90 , C07C69/738 , C07C217/22 , C07C233/47 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C259/06 , C07C323/47 , C07C323/52 , C07C323/59 , C07C323/60 , C07D213/30 , C07D213/55 , C07D249/10 , C07D249/12 , C07D257/04 , C07D333/16 , C07D333/22
CPC分类号： C07B41/12 , A01N37/10 , A61K31/165 , A61K31/192 , A61K31/216 , A61K31/235 , A61K31/41 , A61K31/4196 , A61K31/44 , A61K31/445 , A61K31/535 , A61K31/54 , C07C59/68 , C07C59/90 , C07C67/47 , C07C69/738 , C07C209/68 , C07C217/22 , C07C233/31 , C07C233/47 , C07C235/78 , C07C235/84 , C07C259/06 , C07C323/52 , C07C323/59 , C07C2601/02 , C07C2601/04 , C07C2602/04 , C07D213/30 , C07D213/55 , C07D249/10 , C07D249/12 , C07D257/04 , C07D333/16 , C07D333/24 , Y10S514/866
摘要： PROBLEM TO BE SOLVED: To provide a compound useful for treatment of various metabolic disruptions (for instance, insulin resistant syndrome, diabetes, hyperlipemia, fatty liver disease, cachexia, obesity, atherosclerosis, and arteriosclerosis).SOLUTION: This compound is a biologically active agent that is a compound or its pharmaceutically acceptable salt represented by the following formula 1 (wherein n is 1 or 2; m is 0 or 1; q is 0 or 1; t is 0 or 1; Ris hydrogen, halogen, or 1-3C alkoxy; X is -CH-, and Q is -OR, or X is -CHCRCR- or CHCH(NHAc)-, and Q is OR; or X is -CHCH-, and Q is NRR).
摘要翻译： 要解决的问题：提供可用于治疗各种代谢紊乱（例如胰岛素抵抗综合征，糖尿病，高脂血症，脂肪肝疾病，恶病质，肥胖症，动脉粥样硬化和动脉硬化）的化合物。解决方案：该化合物是生物活性的 作为由下式1表示的化合物或其药学上可接受的盐（其中n为1或2; m为0或1; q为0或1; t为0或1; R 1为氢，卤素或1- C 3烷氧基; X是-CH-，Q是-OR，或X是-CHClCR-或CHCH（NHAc） - ，Q是OR;或X是-CHCH-，Q是NRR）。
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6.发明专利
公开(公告)号：JP2003201240A
公开(公告)日：2003-07-18
申请号：JP2003000721
申请日：2003-01-06
IPC分类号： A61K31/7115 , A61K31/505 , A61K31/513 , A61K31/515 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/712 , A61K45/06 , A61P35/00 , A61P39/02 , C07D237/02 , C07D239/00 , C07H19/06 , C07H19/067 , C07H19/10
摘要： PROBLEM TO BE SOLVED: To provide a method for effectively preventing or treating toxic symptoms of antiviral or anticancer chemotherapy, including but not limited to damage to the hematopoietic system and to gastrointestinal mucosa, to provide a compound and a method to permit administration of higher doses of chemotherapeutic agents, and to provide a method for preventing or ameliorating gastrointestinal epithelium damage due to cytotoxic chemotherapeutic agents. SOLUTION: This method for treating cancer comprises (a) administering a pyrimidine nucleoside analog in a dose at least 1.5 fold greater than the normal maximum tolerated dose, and (b) administering a pharmaceutically effective amount of an acyl derivative of a non-methylated pyrimidine nucleoside. COPYRIGHT: (C)2003,JPO
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