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    Fluorinated lysine derivatives as dipeptidyl peptidase IV inhibitors
    2.
    发明申请
    Fluorinated lysine derivatives as dipeptidyl peptidase IV inhibitors 审中-公开
    氟化赖氨酸衍生物作为二肽基肽酶IV抑制剂

    公开(公告)号：US20050043292A1

    公开(公告)日：2005-02-24

    申请号：US10923146

    申请日：2004-08-19

    申请人： Janice Parker ,  Bernard Hulin

    发明人： Janice Parker ,  Bernard Hulin

    IPC分类号： C07D207/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  A61K31/397 ,  A61K31/445

    CPC分类号： C04B35/632 ,  C07D207/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

    摘要： The invention relates to new therapeutically active and selective inhibitors of the enzyme dipeptidyl peptidase-IV (“DPP-IV”), pharmaceutical compositions comprising the compounds and the use of such compounds for treating diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes, metabolic syndrome (syndrome X or insulin resistance syndrome), hyperglycemia, impaired glucose tolerance, glucosuria, metabolic acidosis, arthritis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, conditions exacerbated by obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome, anxiety, depression, insomnia, chronic fatigue, epilepsy, eating disorders, chronic pain, alcohol addiction, diseases associated with intestinal motility, ulcers, irritable bowel syndrome, inflammatory bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of identifying an insulin secretagogue agent for diabetes.

    摘要翻译： 本发明涉及酶二肽基肽酶-IV（“DPP-IV”）的新的治疗活性和选择性抑制剂，包含该化合物的药物组合物以及这些化合物用于治疗与经受加工的蛋白质相关的疾病的用途 DPP-IV，如2型糖尿病，代谢综合征（X综合征或胰岛素抵抗综合征），高血糖症，葡萄糖耐量降低，糖尿病，代谢性酸中毒，关节炎，白内障，糖尿病性神经病，糖尿病性肾病，糖尿病性视网膜病，糖尿病性心肌病，1型 糖尿病，肥胖症，肥胖症，高血压，高脂血症，动脉粥样硬化，骨质疏松症，骨质减少，虚弱，骨质疏松，骨折，急性冠状动脉综合征，多囊卵巢综合征不育，短肠综合征，焦虑症，抑郁症，失眠症，慢性疲劳 ，癫痫，饮食失调，慢性疼痛，酒精成瘾，与肠蠕动相关的疾病， 溃疡，肠易激综合征，炎性肠综合征，并预防2型糖尿病的疾病进展。 本发明还涉及鉴定糖尿病的胰岛素促分泌剂的方法。

    Synthesis of 3,3,4,4-tetrafluoropyrrolidine and novel dipeptidyl peptidase-IV inhibitor compounds
    7.
    发明授权
    Synthesis of 3,3,4,4-tetrafluoropyrrolidine and novel dipeptidyl peptidase-IV inhibitor compounds 失效
    合成3,3,4,4-四氟吡咯烷和新型二肽基肽酶-IV抑制剂化合物

    公开(公告)号：US06812350B2

    公开(公告)日：2004-11-02

    申请号：US10455747

    申请日：2003-06-03

    申请人： Bernard Hulin

    发明人： Bernard Hulin

    IPC分类号： C07D20504

    CPC分类号： C07D207/10

    摘要： The present invention relates to a method of making novel dipeptidyl peptidase-IV (“DPP-IV’) inhibitor compounds useful for treating, inter alia, diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, metabolic syndrome (Syndrome X or insulin resistance syndrome), hyperglycemia, impaired glucose tolerance, glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of making 3,3,4,4-tetrafluoropyrrolidine, a starting material utilized in the afore-mentioned method for preparing DPP-IV compounds.

    摘要翻译： 本发明涉及一种制备新的二肽基肽酶-IV（“DPP-IV”）抑制剂化合物的方法，其用于治疗特别是与DPP-IV进行加工的蛋白质相关的疾病，例如2型 糖尿病，代谢综合征（X综合征或胰岛素抵抗综合征），高血糖症，糖耐量异常，糖尿病，代谢性酸中毒，白内障，糖尿病性神经病变，糖尿病性肾病，糖尿病性视网膜病变，糖尿病性心肌病，1型糖尿病，肥胖症，高血压，高脂血症，动脉粥样硬化 骨质疏松症，骨质疏松症，骨质疏松症，骨折，急性冠状动脉综合征，多囊卵巢综合症不育症，短肠综合征，预防2型糖尿病等疾病进展，本发明还涉及一种制备3,3， 4,4-四氟吡咯烷，用于上述制备DPP-IV化合物的方法中的原料。

    Thiazolidinedione hypoglycemic agents
    8.
    发明授权
    Thiazolidinedione hypoglycemic agents 失效
    噻唑烷二酮降血糖药

    公开(公告)号：US5120754A

    公开(公告)日：1992-06-09

    申请号：US679898

    申请日：1991-04-03

    申请人： David A. Clark ,  Steven W. Goldstein ,  Gerald F. Holland ,  Bernard Hulin ,  James P. Rizzi

    发明人： David A. Clark ,  Steven W. Goldstein ,  Gerald F. Holland ,  Bernard Hulin ,  James P. Rizzi

    IPC分类号： C07C311/21 ,  C07C323/22 ,  C07D213/50 ,  C07D277/34 ,  C07D417/06 ,  C07D417/10

    CPC分类号： C07D417/06 ,  C07C311/21 ,  C07C323/22 ,  C07D213/50 ,  C07D277/34 ,  C07D417/10

    摘要： Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond; A and dB are each independently CH or N, with the proviso that when A or B is N, the other is CH;X is S, SO, SO.sub.2, CH.sub.2, CHOH or CO;n is 0 or 1;Y is CHR.sup.1 or NR.sup.2, with the proviso that when n is 1 and Y is NR.sup.2, X is SO.sub.2 or CO;Z is CHR.sup.3, CH.sub.2 CH.sub.2, CH.dbd.CH, ##STR2## OCH.sub.2, SCH.sub.2, SOCH.sub.2 or SO.sub.2 CH.sub.2 ; R, R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen or methyl; andX.sup.1 and X.sup.2 are each independently hydrogen, methyl, trifluoromethyl, phenyl, benzyl, hydroxy, methoxy, phenoxy, benzyloxy, bromo, chloro or fluoro; a pharmaceutically-acceptable cationic salt thereof; or a pharmaceutically-acceptable acid addition salt thereof when A or B is N.

    摘要翻译： 式（I）的低血糖噻唑烷-2,4-二酮衍生物，其中虚线表示键或无键; A和dB各自独立地为CH或N，条件是当A或B为N时，另一个为CH; X是S，SO，SO 2，CH 2，CHOH或CO; n为0或1; Y是CHR1或NR2，条件是当n是1且Y是NR2时，X是SO2或CO; Z是CHR 3，CH 2 CH 2，CH = CH，CH 3，OCH 2，SCH 2，SOCH 2或SO 2 CH 2; R，R1，R2和R3各自独立地为氢或甲基; 苯基，苄基，羟基，甲氧基，苯氧基，苄氧基，溴，氯或氟; X 1和X 2各自独立地为氢，甲基， 其药学上可接受的阳离子盐; 或当A或B为N时，其药学上可接受的酸加成盐。

    Thiazolidinedione hypoglycemic agents
    9.
    发明授权
    Thiazolidinedione hypoglycemic agents 失效
    噻唑烷二酮降血糖药

    公开(公告)号：US5061717A

    公开(公告)日：1991-10-29

    申请号：US566436

    申请日：1990-08-14

    申请人： David A. Clark ,  Steven W. Goldstein ,  Gerald F. Holland ,  Bernard Hulin ,  James P. Rizzi

    发明人： David A. Clark ,  Steven W. Goldstein ,  Gerald F. Holland ,  Bernard Hulin ,  James P. Rizzi

    IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61P3/06 ,  A61P3/08 ,  C07C311/21 ,  C07C323/22 ,  C07D213/50 ,  C07D277/34 ,  C07D417/06 ,  C07D417/10

    CPC分类号： C07D417/06 ,  C07C311/21 ,  C07C323/22 ,  C07D213/50 ,  C07D277/34 ,  C07D417/10

    摘要： Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond; A and B are each independently CH or N, with the proviso that when A or B is N, the other is CH;X is S, SO, SO.sub.2, CH.sub.2, CHOH or CO;n is 0 or 1;Y is CHR.sup.1 or NR.sup.2, with the proviso that when n is 1 and Y is NR.sup.2, X is SO.sub.2 or CO;Z is CHR.sup.3, CH.sub.2 CH.sub.2, CH.dbd.CH, ##STR2## OCH.sub.2, SCH.sub.2, SOCH.sub.2 or SO.sub.2 CH.sub.2 ; R, R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen or methyl; andX.sup.1 and X.sup.2 are each independently hydrogen, methyl, trifluoromethyl, phenyl, benzyl, hydroxy, methoxy, phenoxy, benzyloxy, bromo, chloro or fluoro; a pharmaceutically-acceptable cationic salt thereof; or a pharmaceutically-acceptable acid addition salt thereof when A or B is N.

    摘要翻译： PCT No.PCT / US88 / 00744 Sec。 371日期1990年8月14日 （I）的低血糖噻唑烷-2,4-二酮衍生物，其中虚线表示键或无键;（e）日本1990年8月14日PCT。 A和B各自独立地为CH或N，条件是当A或B为N时，另一个为CH; X是S，SO，SO 2，CH 2，CHOH或CO; n为0或1; Y是CHR1或NR2，条件是当n是1且Y是NR2时，X是SO2或CO; Z是CHR 3，CH 2 CH 2，CH = CH，CH 3，OCH 2，SCH 2，SOCH 2或SO 2 CH 2; R，R 1，R 2和R 3各自独立地为氢或甲基; 苯基，苄基，羟基，甲氧基，苯氧基，苄氧基，溴，氯或氟; X 1和X 2各自独立地为氢，甲基， 其药学上可接受的阳离子盐; 或当A或B为N时，其药学上可接受的酸加成盐。

    Therapeutic compounds
    10.
    发明授权
    Therapeutic compounds 有权
    治疗化合物

    公开(公告)号：US07291618B2

    公开(公告)日：2007-11-06

    申请号：US11129277

    申请日：2005-05-12

    申请人： Bernard Hulin ,  David W. Piotrowski

    发明人： Bernard Hulin ,  David W. Piotrowski

    IPC分类号： A61K31/497 ,  C07D403/14

    CPC分类号： C07D207/14 ,  C07D275/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

    摘要： The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R1, R2, R3, HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof in treating diabetic complications including diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, and the like.

    摘要翻译： 本发明提供式（I）化合物，其前体药物和立体异构体，以及化合物，前药和立体异构体的药学上可接受的盐，其中R 1，R 2， R 3，HET，n，Q，X，Y和Z如本文所述; 组合物; 及其用于治疗糖尿病性神经病变，糖尿病性肾病，糖尿病性微血管病变等糖尿病并发症的用途。