公开(公告)号：US5705515A

公开(公告)日：1998-01-06

申请号：US684901

申请日：1996-07-25

申请人： Michael H. Fisher ,  Elizabeth M. Naylor ,  Emma R. Parmee ,  Thomas Shih ,  Hyun Ok ,  Ann E. Weber

发明人： Michael H. Fisher ,  Elizabeth M. Naylor ,  Emma R. Parmee ,  Thomas Shih ,  Hyun Ok ,  Ann E. Weber

IPC分类号： C07D277/24 ,  A61K31/395 ,  A61K31/40 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/42 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/435 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/535 ,  A61P1/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07C311/21 ,  C07C311/47 ,  C07D209/04 ,  C07D209/08 ,  C07D213/38 ,  C07D213/73 ,  C07D215/36 ,  C07D233/32 ,  C07D233/36 ,  C07D261/06 ,  C07D261/08 ,  C07D271/06 ,  C07D277/20 ,  C07D277/28 ,  C07D277/30 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/02 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00 ,  C07D275/02 ,  C07D277/02

CPC分类号： C07C311/21 ,  C07C311/47 ,  C07D209/08 ,  C07D213/38 ,  C07D213/73 ,  C07D215/36 ,  C07D233/32 ,  C07D271/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

摘要翻译： 取代磺酰胺是具有非常少的β1和β2肾上腺素能受体活性的选择性β3肾上腺素能受体激动剂，因此这些化合物能够增加细胞中的脂肪分解和能量消耗。 因此，这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。 通过将氨基烷基苯基磺酰胺与适当取代的环氧化物偶合来制备化合物。 还公开了用于治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或增加肠道运动性的组合物和方法。

公开(公告)号：US5561142A

公开(公告)日：1996-10-01

申请号：US445630

申请日：1995-05-22

申请人： Michael H. Fisher ,  Elizabeth M. Naylor ,  Dong Ok ,  Ann E. Weber ,  Thomas Shih ,  Hyun Ok

发明人： Michael H. Fisher ,  Elizabeth M. Naylor ,  Dong Ok ,  Ann E. Weber ,  Thomas Shih ,  Hyun Ok

IPC分类号： C07C311/21 ,  C07C311/47 ,  C07D209/08 ,  C07D213/38 ,  C07D213/73 ,  C07D215/36 ,  C07D233/32 ,  C07D271/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61K31/44 ,  A61K31/47 ,  C07D213/30

CPC分类号： C07D213/73 ,  C07C311/21 ,  C07C311/47 ,  C07D209/08 ,  C07D213/38 ,  C07D215/36 ,  C07D233/32 ,  C07D271/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

摘要翻译： 取代磺酰胺是具有非常少的β1和β2肾上腺素能受体活性的选择性β3肾上腺素能受体激动剂，因此这些化合物能够增加细胞中的脂肪分解和能量消耗。 因此，这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。 通过将氨基烷基苯基磺酰胺与适当取代的环氧化物偶合来制备化合物。 还公开了用于治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或增加肠蠕动的组合物和方法。

公开(公告)号：US06699871B2

公开(公告)日：2004-03-02

申请号：US10189603

申请日：2002-07-05

申请人： Scott D. Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E. Weber ,  Jinyou Xu

发明人： Scott D. Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E. Weber ,  Jinyou Xu

IPC分类号： C07D48704

CPC分类号： A61K31/4985 ,  A61K31/498 ,  A61K38/28 ,  A61K45/06 ,  C07D487/04 ,  Y10S514/866 ,  A61K2300/00

摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

公开(公告)号：US20110190308A1

公开(公告)日：2011-08-04

申请号：US13086563

申请日：2011-04-14

申请人： Scott D. Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E. Weber ,  Jinyou Xu

发明人： Scott D. Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E. Weber ,  Jinyou Xu

IPC分类号： A61K31/4985 ,  A61P3/10

CPC分类号： A61K31/4985 ,  A61K31/498 ,  A61K38/28 ,  A61K45/06 ,  C07D487/04 ,  Y10S514/866 ,  A61K2300/00

摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

公开(公告)号：US20100130504A1

公开(公告)日：2010-05-27

申请号：US12694758

申请日：2010-01-27

申请人： Scott D. Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E. Weber ,  Jinyou Xu

发明人： Scott D. Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E. Weber ,  Jinyou Xu

IPC分类号： A61K31/4985 ,  A61P3/10

CPC分类号： A61K31/4985 ,  A61K31/498 ,  A61K38/28 ,  A61K45/06 ,  C07D487/04 ,  Y10S514/866 ,  A61K2300/00

摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

公开(公告)号：US5451677A

公开(公告)日：1995-09-19

申请号：US168105

申请日：1993-12-15

申请人： Michael H. Fisher ,  Robert J. Mathvink ,  Hyun O. Ok ,  Emma R. Parmee ,  Ann E. Weber

发明人： Michael H. Fisher ,  Robert J. Mathvink ,  Hyun O. Ok ,  Emma R. Parmee ,  Ann E. Weber

IPC分类号： A61K31/18 ,  A61K31/335 ,  A61K31/34 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/40 ,  A61K31/403 ,  A61K31/415 ,  A61K31/42 ,  A61K31/423 ,  A61K31/425 ,  A61K31/428 ,  A61K31/433 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4433 ,  A61K31/47 ,  A61K31/496 ,  A61K31/505 ,  A61K31/63 ,  A61K31/635 ,  A61P3/04 ,  A61P3/08 ,  A61P3/10 ,  C07C311/02 ,  C07C311/10 ,  C07C311/13 ,  C07C311/14 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07C311/46 ,  C07C311/47 ,  C07D209/02 ,  C07D209/08 ,  C07D209/12 ,  C07D209/34 ,  C07D213/65 ,  C07D213/71 ,  C07D213/73 ,  C07D213/75 ,  C07D215/36 ,  C07D233/54 ,  C07D239/34 ,  C07D261/20 ,  C07D277/64 ,  C07D277/74 ,  C07D285/10 ,  C07D285/14 ,  C07D307/78 ,  C07D307/79 ,  C07D307/82 ,  C07D311/08 ,  C07D317/62 ,  C07D319/18 ,  C07D333/34 ,  C07D333/54 ,  C07D333/62 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D455/00 ,  C07C311/01 ,  C07D307/10

CPC分类号： C07D213/73 ,  C07C311/13 ,  C07C311/14 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07C311/46 ,  C07C311/47 ,  C07D209/08 ,  C07D209/12 ,  C07D209/34 ,  C07D213/65 ,  C07D213/71 ,  C07D215/36 ,  C07D261/20 ,  C07D277/74 ,  C07D285/14 ,  C07D307/79 ,  C07D307/82 ,  C07D311/08 ,  C07D317/62 ,  C07D319/18 ,  C07D333/34 ,  C07D333/54 ,  C07D333/62 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07C2102/08 ,  C07C2102/10

摘要： Substituted phenylsulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted alkyl epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

摘要翻译： 取代的苯基磺酰胺是具有非常少的β1和β2肾上腺素能受体活性的选择性β3肾上腺素能受体激动剂，因此化合物能够增加细胞中的脂肪分解和能量消耗。 因此，这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。 通过将氨基烷基苯基磺酰胺与适当取代的烷基环氧化物偶联制备化合物。 还公开了用于治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或增加肠蠕动的组合物和方法。

公开(公告)号：US07125873B2

公开(公告)日：2006-10-24

申请号：US10481353

申请日：2002-07-05

申请人： Scott D Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E Weber ,  Jinyou Xu

发明人： Scott D Edmondson ,  Michael H. Fisher ,  Dooseop Kim ,  Malcolm Maccoss ,  Emma R. Parmee ,  Ann E Weber ,  Jinyou Xu

IPC分类号： A61K31/44

CPC分类号： A61K31/4985 ,  A61K31/498 ,  A61K38/28 ,  A61K45/06 ,  C07D487/04 ,  Y10S514/866 ,  A61K2300/00

摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

摘要翻译： 本发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）抑制剂的化合物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

公开(公告)号：US6034106A

公开(公告)日：2000-03-07

申请号：US868556

申请日：1997-06-04

申请人： Tesfaye Biftu ,  Michael H. Fisher ,  Danqing Dennis Feng ,  Chan-Hwa Kuo ,  Gui-Bai Liang ,  Elizabeth M. Naylor ,  Ann E. Weber

发明人： Tesfaye Biftu ,  Michael H. Fisher ,  Danqing Dennis Feng ,  Chan-Hwa Kuo ,  Gui-Bai Liang ,  Elizabeth M. Naylor ,  Ann E. Weber

IPC分类号： C07D413/12 ,  C07D413/10 ,  A61K31/44

CPC分类号： C07D413/12

摘要： Oxadiazole substituted benzenesulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

摘要翻译： 恶二唑取代的苯磺酰胺是具有非常少的β1和β2肾上腺素能受体活性的选择性β3肾上腺素能受体激动剂，因此化合物能够增加细胞中的脂肪分解和能量消耗。 因此，这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。 通过将氨基烷基苯基磺酰胺与适当取代的环氧化物偶合来制备化合物。 还公开了用于治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或增加肠蠕动的组合物和方法。

公开(公告)号：US5541197A

公开(公告)日：1996-07-30

申请号：US404566

申请日：1995-03-21

申请人： Michael H. Fisher ,  Elizabeth M. Naylor ,  Ann E. Weber

发明人： Michael H. Fisher ,  Elizabeth M. Naylor ,  Ann E. Weber

IPC分类号： C07C311/21 ,  C07C311/47 ,  C07D209/08 ,  C07D213/38 ,  C07D213/73 ,  C07D215/36 ,  C07D233/32 ,  C07D271/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D215/04 ,  A61K31/47

CPC分类号： C07D213/73 ,  C07C311/21 ,  C07C311/47 ,  C07D209/08 ,  C07D213/38 ,  C07D215/36 ,  C07D233/32 ,  C07D271/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

公开(公告)号：US5714506A

公开(公告)日：1998-02-03

申请号：US717659

申请日：1996-09-23

申请人： Michael H. Fisher ,  Hyun O. Ok ,  Ann E. Weber

发明人： Michael H. Fisher ,  Hyun O. Ok ,  Ann E. Weber

IPC分类号： C07D213/38 ,  C07D213/61 ,  C07D213/73 ,  C07D405/04 ,  A61K31/44 ,  C07D213/30

CPC分类号： C07D213/73 ,  C07D213/38 ,  C07D213/61 ,  C07D405/04

摘要： Compounds of formula ##STR1## are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents.

摘要翻译： 式I的化合物是具有非常少的β1和β2肾上腺素能受体活性的选择性β3肾上腺素能受体激动剂，因此化合物能够增加细胞中的脂肪分解和能量消耗。 因此，这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。