CN107250137A - 作为长效dpp‑iv抑制剂的取代的氨基六元饱和杂脂环类 - Google Patents
作为长效dpp‑iv抑制剂的取代的氨基六元饱和杂脂环类 Download PDFInfo
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Abstract
Description
Claims (25)
- 通式I所示的化合物或其药学上可接受的盐:其中,A环选自6元芳基或含有1-2个独立地选自N、O或S原子的5-6元杂芳基;X选自O或CH2,Y选自N或CH,并且当X为CH2时,Y不为CH;R1、R2和R3各自独立地选自H、C1-3烷基、-NH2或-OH;每个R4独立地选自卤素、-NH2、-OH、C1-6烷基、C1-6烷氧基、苯氧基或苄氧基;每个R5独立地选自C1-6烷基、卤素、-CN、-OH、-COOR6、-NHR7或-SO2R8,或者两个R5基团与和它们相连接的A环原子一起组成5-7元环;R6选自H或C1-6烷基;R7选自H、C1-6烷基或-SO2R8;每个R8独立地选自-OH、-NH2、C1-6烷基或C3-6环烷基;o和p分别独立地选自1、2或3;m和n分别独立地选自1或2。
- 根据权利要求1所述的化合物或其药学上可接受的盐,其为式II所示的化合物或其药学上可接受的盐:其中,X选自O;Y选自N或CH;R1选自-NH2或-OH;R2和R3均为H;R4a和R4b独立地选自F、Cl、Br、I、-NH2或-OH;每个R5独立地选自F、Cl、Br、I、-CN、-COOR6、-NHR7或-SO2R8;p选自1或2;R6选自H、甲基、乙基、丙基或丁基;R7选自H、甲基、乙基、丙基、丁基或-SO2R8;每个R8独立地选自-OH、-NH2、甲基、乙基、丙基、丁基、C3环烷基、C4环烷基或C5环烷基。
- 根据权利要求1所述的化合物或其药学上可接受的盐,其为式III所示的化合物或其药学上可接受的盐:其中,X选自O;Y选自N或CH;R1选自-NH2或-OH;R2和R3均为H;R4a和R4b独立地选自F、Cl、Br、-NH2或-OH;R5a和R5b各自独立地选自F、Cl、Br、I、-CN、-COOR6、-NHR7或-SO2R8;R6选自H、甲基、乙基、丙基或丁基;R7选自H、甲基、乙基、丙基、丁基或-SO2R8;每个R8独立地选自-OH、-NH2、甲基、乙基、丙基、丁基、C3环烷基、C4环烷基或C5环烷基。
- 根据权利要求1所述的化合物或其药学上可接受的盐,其为式IV所示的化合物或其药学上 可接受的盐:其中,X选自O;Y选自N或CH;R1选自-NH2或-OH;R2和R3为H;R4a和R4b独立地选自F、Cl、Br、-NH2、-OH;R5c和R5d与和它们相连接的吡唑环原子一起组成5、6或7元非芳香环,所述5、6或7元非芳香环优选地包含1、2或3个独立地选自N、O或S杂原子,所述5、6或7元非芳香环更优选地包含-SO2-基团。
- 根据权利要求1所述的化合物或其药学上可接受的盐,其为式V所示的化合物或其药学上可接受的盐:其中,X选自O;Y选自N或CH;R1、R2和R3各自独立地选自H、C1-3烷基、-NH2或-OH;每个R4独立地选自卤素、-NH2、-OH、C1-6烷基、C1-6烷氧基、苯氧基或苄氧基;每个R5独立地选自C1-6烷基、卤素、-CN、-OH、-COOR6、-NHR7或-SO2R8;R6选自H或C1-6烷基;R7选自H、C1-6烷基或-SO2R8;每个R8独立地选自-OH、-NH2、C1-6烷基或C3-6环烷基;o和p各自独立地选自1、2或3。
- 根据权利要求5所述的化合物或其药学上可接受的盐,其中R1选自-NH2或-OH。
- 根据权利要求5-6中任一项权利要求所述的化合物或其药学上可接受的盐,其中R2和R3均为H。
- 根据权利要求5-7中任一项权利要求所述的化合物或其药学上可接受的盐,其中R4选自F、Cl、Br、I、-NH2或-OH。
- 根据权利要求5-8中任一项权利要求所述的化合物或其药学上可接受的盐,其中R5选自F、Cl、Br、I、-COOR6、-NHR7或-SO2R8。
- 根据权利要求5-9中任一项权利要求所述的化合物或其药学上可接受的盐,其中R6选自H、甲基、乙基、丙基或丁基。
- 根据权利要求5-10中任一项权利要求所述的化合物或其药学上可接受的盐,其中R7选自H、甲基、乙基、丙基、丁基或-SO2R8。
- 根据权利要求5-11中任一项权利要求所述的化合物或其药学上可接受的盐,其中每个R8独立地选自-OH、-NH2、甲基、乙基、丙基、丁基、C3环烷基、C4环烷基或C5环烷基。
- 根据权利要求5-12中任一项权利要求所述的化合物或其药学上可接受的盐,其中o为2。
- 根据权利要求5-13中任一项权利要求所述的化合物或其药学上可接受的盐,其中p为1或2。
- 根据权利要求5-14中任一项权利要求所述的化合物或其药学上可接受的盐,其中R4的取代位置如结构式VI中的R4a和R4b所示:其中,R4a和R4b各自独立地选自F、Cl、Br、I、-NH2或-OH,以及其他取代基的定义与权利要求5-14中任一项权利要求中的定义相同。
- 根据权利要求5-13中任一项权利要求所述的化合物或其药学上可接受的盐,其中p为2,并且R5的取代位置如结构式VII中的R5a和R5b所示:其中,R5a和R5b各自独立地选自F、Cl、Br、I、-COOR6、-NHR7或-SO2R8,以及其他取代基的定义与权利要求5-13中任一项权利要求中的定义相同。
- 根据权利要求5-13中任一项权利要求所述的化合物或其药学上可接受的盐,其中p为1,并且R5的取代位置如结构式VIII中的R5a所示:其中,R5a选自F、Cl、Br、I、-COOR6、-NHR7或-SO2R8,以及其他取代基的定义与权利要求5-13中任一项权利要求中的定义相同。
- 如权利要求1所述的化合物或其药学上可接受的盐,其选自:
- 药物组合物,其包含治疗有效量的权利要求1-18中任一项权利要求所述的化合物或其药学上可接受的盐、溶剂化物、多晶型物、互变异构体和药学上可接受的载体。
- 权利要求1-18中任一项权利要求所述的化合物或其药学上可接受的盐或权利要求19所述的药物组合物在制备用于治疗和/或预防受益于DPP-IV抑制的疾病和病症的药物中的用途。
- 根据权利要求20所述的用途,其中所述受益于DPP-IV抑制的疾病和病症选自胰岛素抵抗、高血糖症、II型糖尿病、糖尿病性脂血异常、葡萄糖耐量减低症、禁食血浆葡萄糖减低症、代谢性酸中毒、酮症、食欲调节、肥胖症、各种癌症、神经系统病症或免疫系统病症。
- 用于治疗和/或预防受益于DPP-IV抑制的疾病和病症的方法,其包括将权利要求1-18中任一项权利要求所述的化合物或其药学上可接受的盐或权利要求19所述的药物组合物向有需要的个体给药。
- 根据权利要求22所述的治疗方法,其中所述受益于DPP-IV抑制的疾病和病症选自胰岛素抵抗、高血糖症、II型糖尿病、糖尿病性脂血异常、葡萄糖耐量减低症、禁食血浆葡萄糖减低症、代谢性酸中毒、酮症、食欲调节、肥胖症、各种癌症、神经系统病症或免疫系 统病症。
- 用于治疗和/或预防受益于DPP-IV抑制的疾病和病症的权利要求1-18中任一项权利要求所述的化合物或其药学上可接受的盐或权利要求19所述的药物组合物。
- 根据权利要求24所述的化合物或其药学上可接受的盐或药物组合物,其中所述受益于DPP-IV抑制的疾病和病症选自胰岛素抵抗、高血糖症、II型糖尿病、糖尿病性脂血异常、葡萄糖耐量减低症、禁食血浆葡萄糖减低症、代谢性酸中毒、酮症、食欲调节、肥胖症、各种癌症、神经系统病症或免疫系统病症。
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CN107250135B (zh) * | 2015-08-24 | 2020-05-26 | 四川科伦博泰生物医药股份有限公司 | 长效二肽基肽酶-ⅳ抑制剂、用途及其中间体的制备方法 |
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CN106755152B (zh) * | 2017-01-23 | 2020-06-16 | 苏州引航生物科技有限公司 | 一种制备奥格列汀中间体的方法 |
CN108456196A (zh) * | 2017-02-22 | 2018-08-28 | 四川科伦博泰生物医药股份有限公司 | 3-氨基四氢吡喃衍生物的盐及其多晶型、其制备方法和用途 |
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CN107325020B (zh) * | 2017-06-22 | 2019-06-21 | 广西科技大学 | 奥格列汀中间体的制备方法 |
CN107473988B (zh) * | 2017-08-22 | 2018-10-02 | 钟桂发 | 奥格列汀的中间体的制备方法 |
CN113831266B (zh) * | 2019-01-22 | 2024-04-05 | 河南医学高等专科学校 | 1-(2,5-二氟苯基)-1-氧代戊-4-炔-2-基氨基甲酸烷基酯的合成 |
CN111057059B (zh) * | 2019-11-25 | 2022-04-26 | 广东省测试分析研究所(中国广州分析测试中心) | 一种苯并二四氢吡咯类化合物或其药学上可接受的盐、及其制备方法和应用 |
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- 2016-02-04 EP EP16748717.2A patent/EP3257857A4/en not_active Withdrawn
- 2016-02-04 CN CN201680009635.5A patent/CN107250137B/zh active Active
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WO2007097931A2 (en) * | 2006-02-15 | 2007-08-30 | Merck & Co., Inc. | Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes |
CN101410400A (zh) * | 2006-03-28 | 2009-04-15 | 默克公司 | 作为用于糖尿病治疗或者预防的二肽基肽酶-ⅳ抑制剂的氨基四氢吡喃 |
WO2008060488A1 (en) * | 2006-11-14 | 2008-05-22 | Merck & Co., Inc. | Tricyclic heteroaromatic compounds as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes |
Also Published As
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CN111018891A (zh) | 2020-04-17 |
US10155775B2 (en) | 2018-12-18 |
AU2016218693A1 (en) | 2017-09-28 |
RU2720488C2 (ru) | 2020-04-30 |
JP6715852B2 (ja) | 2020-07-01 |
WO2016127916A1 (zh) | 2016-08-18 |
CA2975330A1 (en) | 2016-08-18 |
RU2017131354A (ru) | 2019-03-12 |
JP2018508502A (ja) | 2018-03-29 |
EP3257857A4 (en) | 2018-08-01 |
AU2016218693B2 (en) | 2020-04-30 |
US20180111950A1 (en) | 2018-04-26 |
CN105985357A (zh) | 2016-10-05 |
RU2017131354A3 (zh) | 2019-05-24 |
CN107250137B (zh) | 2019-08-16 |
CN111018891B (zh) | 2021-12-03 |
EP3257857A1 (en) | 2017-12-20 |
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