公开(公告)号：US4999436A

公开(公告)日：1991-03-12

申请号：US397325

申请日：1989-08-22

申请人： Bruce E. Witzel ,  Debra L. Allison ,  Charles G. Caldwell ,  Kathleen Rupprecht

发明人： Bruce E. Witzel ,  Debra L. Allison ,  Charles G. Caldwell ,  Kathleen Rupprecht

IPC分类号： C07D333/32 ,  C07D333/50 ,  C07D333/64 ,  C07D333/78 ,  C07D333/80 ,  C07D409/04

CPC分类号： C07D409/04 ,  C07D333/32 ,  C07D333/50 ,  C07D333/64 ,  C07D333/78 ,  C07D333/80

摘要： Aryl substituted thiophenes 3-ols, its dihydro derivatives, 1-oxide and 1,1-dioxide analogs, as well as aryl substituted furans, are 5-lipoxygenase inhibitors useful in the treatment of inflammation and other leukotriene-mediated diseases.

摘要翻译： 芳基取代的噻吩3-ols，其二氢衍生物，1-氧化物和1,1-二氧化物类似物以及芳基取代的呋喃是可用于治疗炎症和其它白三烯介导的疾病的5-脂氧合酶抑制剂。

公开(公告)号：US07956061B2

公开(公告)日：2011-06-07

申请号：US11793093

申请日：2006-01-18

申请人： Wallace T. Ashton ,  Charles G. Caldwell ,  Hong Dong ,  Ying-Duo Gao ,  Giovanna Scapin ,  Ann E. Weber

发明人： Wallace T. Ashton ,  Charles G. Caldwell ,  Hong Dong ,  Ying-Duo Gao ,  Giovanna Scapin ,  Ann E. Weber

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P3/10

CPC分类号： C07D487/04 ,  C07D495/14

摘要： The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-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（“DPP-IV抑制剂”）的抑制剂的新型取代的双环嘧啶，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病， 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：US4746669A

公开(公告)日：1988-05-24

申请号：US30313

申请日：1987-03-26

申请人： Charles G. Caldwell ,  Ihor Kopka ,  Milton L. Hammond ,  Robert A. Zambias

发明人： Charles G. Caldwell ,  Ihor Kopka ,  Milton L. Hammond ,  Robert A. Zambias

IPC分类号： C07D277/22 ,  C07D417/04 ,  C07D417/14 ,  A61K31/38 ,  C07D217/04 ,  C07D409/04 ,  C07D409/06

CPC分类号： C07D417/04 ,  C07D417/14

摘要： Thiazole derivatives have been made, for example, by reacting a 2-aryl-2,2-dialkoxyethylamine with an appropriately substituted aryl acetyl halide followed by treating the resulting amide with diphosphoryl pentasulfide. The thiazole derivatives are found to be effective immunoregulants.

摘要翻译： 噻唑衍生物例如通过使2-芳基-2,2-二烷氧基乙胺与适当取代的芳基乙酰卤反应，然后用二硫代二磷酰基处理得到的酰胺来制备。 发现噻唑衍生物是有效的免疫调节剂。

公开(公告)号：US4966907A

公开(公告)日：1990-10-30

申请号：US230825

申请日：1988-08-12

申请人： Charles G. Caldwell ,  Milton L. Hammond ,  Ihor E. Kopka ,  Stanley H. B. Wright ,  Robert A. Zambias

发明人： Charles G. Caldwell ,  Milton L. Hammond ,  Ihor E. Kopka ,  Stanley H. B. Wright ,  Robert A. Zambias

IPC分类号： C07D307/79

CPC分类号： C07D307/79

摘要： Novel position-4 and/or position-6 substituted 5-hydroxy-2,3-dihydrobenzofuran and analogs of the following general structural formula (I) are disclosed: ##STR1## These compounds are found to be potent inhibitors of leukotriene biosynthesis.

摘要翻译： 公开了新的位置-4和/或位置-6取代的5-羟基-2,3-二氢苯并呋喃以及下列通式（I）的类似物：（I）这些化合物被发现是白细胞三烯的有效抑制剂 生物合成。

公开(公告)号：US20100234403A1

公开(公告)日：2010-09-16

申请号：US12223143

申请日：2007-02-09

申请人： Tesfaye Biftu ,  Charles G. Caldwell ,  Ann E. Weber ,  Ping Chen ,  Xiaoxia Qian ,  Danqing Feng ,  Jason M. Cox

发明人： Tesfaye Biftu ,  Charles G. Caldwell ,  Ann E. Weber ,  Ping Chen ,  Xiaoxia Qian ,  Danqing Feng ,  Jason M. Cox

IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P3/10

CPC分类号： C07D471/04 ,  C07D405/04 ,  C07D487/04

摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme 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： 本发明涉及结构式I的新型取代的氨基四氢吡喃，其是二肽基肽酶-IV酶的抑制剂，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：US07265128B2

公开(公告)日：2007-09-04

申请号：US10542214

申请日：2004-01-13

申请人： Wallace T. Ashton ,  Charles G. Caldwell ,  Robert J. Mathvink ,  Hyun O. Ok ,  Leah Bitalac Reigle ,  Ann E. Weber

发明人： Wallace T. Ashton ,  Charles G. Caldwell ,  Robert J. Mathvink ,  Hyun O. Ok ,  Leah Bitalac Reigle ,  Ann E. Weber

IPC分类号： A61K31/4365 ,  C07D513/04

CPC分类号： C07D498/04 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives of structural formula (I) 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”）的抑制剂的结构式（I）的3-氨基-4-苯基丁酸衍生物，其可用于治疗或预防疾病 其中涉及二肽基肽酶-IV酶，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：US07026316B2

公开(公告)日：2006-04-11

申请号：US10472771

申请日：2002-03-22

申请人： Wallace T. Ashton ,  Charles G. Caldwell ,  Hyun O. Ok ,  Emma R. Parmee ,  Ann E. Weber

发明人： Wallace T. Ashton ,  Charles G. Caldwell ,  Hyun O. Ok ,  Emma R. Parmee ,  Ann E. Weber

IPC分类号： A61K31/426 ,  A61K31/40 ,  C07D207/00 ,  C07D277/04 ,  C07D417/04

CPC分类号： C07D417/06 ,  C07D207/09 ,  C07D277/04 ,  C07D417/12 ,  C07D417/14

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：US5679700A

公开(公告)日：1997-10-21

申请号：US555535

申请日：1995-11-09

申请人： Charles G. Caldwell ,  Philippe L. Durette ,  Joung L. Goulet ,  William K. Hagmann ,  Soumya P. Sahoo

发明人： Charles G. Caldwell ,  Philippe L. Durette ,  Joung L. Goulet ,  William K. Hagmann ,  Soumya P. Sahoo

IPC分类号： A61K31/66 ,  A61K31/665 ,  A61K31/67 ,  A61K31/675 ,  A61P1/02 ,  A61P7/02 ,  A61P9/10 ,  A61P27/02 ,  A61P35/00 ,  A61P43/00 ,  C07F9/30 ,  C07F9/32 ,  C07F9/547 ,  A61K31/40

CPC分类号： A61K31/675 ,  A61K31/66 ,  C07F9/301

摘要： Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. These inhibitors may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation. ##STR1##

摘要翻译： 发现式I的新的含次膦酸的肽基化合物是有用的基质金属蛋白酶介导的疾病的抑制剂，包括骨关节炎，类风湿性关节炎，脓毒性关节炎，某些癌症中的肿瘤侵袭，牙周病，角膜溃疡，蛋白尿，疏水性表皮松解性大疱性炎症和 与动脉粥样硬化斑块破裂相关的冠状动脉血栓形成。 这些抑制剂也可用于预防可能导致永久性残疾的创伤性损伤后的病理后遗症。 这些化合物也可以通过预防排卵或植入作为避孕的手段。 我

公开(公告)号：US5403952A

公开(公告)日：1995-04-04

申请号：US133493

申请日：1993-10-08

申请人： William Hagmann ,  Charles G. Caldwell ,  Paul R. Gooley

发明人： William Hagmann ,  Charles G. Caldwell ,  Paul R. Gooley

IPC分类号： C07C237/22 ,  C07K7/100

CPC分类号： C07C237/22 ,  C07C2101/08 ,  C07C2101/10 ,  C07C2101/14 ,  C07C2101/16

摘要： Novel substituted cyclic compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also be useful as novel birth control agents by preventing ovulation or implantation. ##STR1##

摘要翻译： 发现式I的新型取代的环状化合物是基质金属蛋白酶介导的疾病的有用的抑制剂，包括骨关节炎，类风湿性关节炎，脓毒性关节炎，某些癌症中的肿瘤侵袭，牙周病，角膜溃疡，蛋白尿，营养不良的表皮松解性大疱性和冠状动脉血栓相关 动脉粥样硬化斑块破裂。 基质金属蛋白酶是含有蛋白酶的家族，包括但不限于基质溶素，胶原酶和明胶酶，其能够降解关节软骨和基底膜的主要成分。 本文所要求的抑制剂也可用于预防可能导致永久性残疾的外伤性损伤后的病理后遗症。 这些化合物也可以通过防止排卵或植入而用作新的避孕药。 我

公开(公告)号：US20090105210A1

公开(公告)日：2009-04-23

申请号：US11793093

申请日：2006-01-18

申请人： Wallace T. Ashton ,  Charles G. Caldwell ,  Hong Dong ,  Ying-Duo Gao ,  Giovanna Scapin ,  Ann E. Weber

发明人： Wallace T. Ashton ,  Charles G. Caldwell ,  Hong Dong ,  Ying-Duo Gao ,  Giovanna Scapin ,  Ann E. Weber

IPC分类号： A61K31/5377 ,  A61K31/519 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D495/14

摘要： The present invention is directed to novel substituted bicyclic pyrimidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-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（“DPP-IV抑制剂”）的抑制剂的新型取代的双环嘧啶，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病， 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。