公开(公告)号：US5756507A

公开(公告)日：1998-05-26

申请号：US760851

申请日：1996-12-05

申请人： Mark Goulet ,  Lin Chu ,  Wallace T. Ashton ,  Michael H. Fisher ,  Matthew J. Wyvratt ,  Roy G. Smith ,  Robert L. Bugianesi ,  Mitree M. Ponpipom ,  Yi Tien Yang ,  Peter Lin

发明人： Mark Goulet ,  Lin Chu ,  Wallace T. Ashton ,  Michael H. Fisher ,  Matthew J. Wyvratt ,  Roy G. Smith ,  Robert L. Bugianesi ,  Mitree M. Ponpipom ,  Yi Tien Yang ,  Peter Lin

IPC分类号： C07D209/14 ,  C07D209/16 ,  A61K31/405 ,  A61K31/495 ,  C07D209/10 ,  C07D403/06

CPC分类号： C07D209/14 ,  C07D209/16

摘要： There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

公开(公告)号：US5292726A

公开(公告)日：1994-03-08

申请号：US885416

申请日：1992-05-19

申请人： Wallace T. Ashton ,  Conrad P. Dorn ,  William J. Greenlee ,  Malcolm MacCoss ,  Sander G. Mills ,  Mu T. Wu

发明人： Wallace T. Ashton ,  Conrad P. Dorn ,  William J. Greenlee ,  Malcolm MacCoss ,  Sander G. Mills ,  Mu T. Wu

IPC分类号： A01N43/60 ,  A01N47/16 ,  A01N47/38 ,  C07D241/04 ,  C07D295/215 ,  C07D403/06 ,  A61K31/675 ,  A61K31/495 ,  C07F9/6509

CPC分类号： C07D295/215 ,  A01N43/60 ,  A01N47/16 ,  A01N47/38 ,  C07D241/04 ,  C07D403/06

摘要： Diacylpiperazines of general structure ##STR1## are: angiotensin II (A-II) antagonists selective for the type 2 (AT.sub.2) subtype useful in the treatment of cerebrovascular, cognitive, and CNS disorders; tachykinin receptor antagonists useful in the treatment of inflammatory diseases and pain or migraine; and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

摘要翻译： 一般结构的二酰基哌嗪是一种对可用于治疗脑血管，认知和中枢神经系统疾病的2型（AT2）亚型选择性的血管紧张素II（A-II）拮抗剂; 用于治疗炎性疾病和疼痛或偏头痛的速激肽受体拮抗剂; 和钙通道阻滞剂可用于治疗心血管疾病如心绞痛，高血压或缺血。

公开(公告)号：US4863927A

公开(公告)日：1989-09-05

申请号：US48290

申请日：1987-05-11

申请人： Richard L. Tolman ,  Wallace T. Ashton

发明人： Richard L. Tolman ,  Wallace T. Ashton

IPC分类号： A61K31/505 ,  A61P31/12 ,  A61P31/22 ,  C07D239/54 ,  C07D239/553

CPC分类号： C07D239/54 ,  C07D239/553

摘要： 1-[2-(Hydroxymethyl)cycloalkylmethyl]-5-substituted uracils which are herpes simplex viral thymidine kinase inhibitors, their acyl derivatives, and their pharmaceutically-acceptable salts; pharmaceutical formulations containing these compounds; the treatment of DNA viral, particularly herpes viral, infections with these compounds; methods of preparing these compounds; and novel intermediates useful in their preparation.

公开(公告)号：US4782062A

公开(公告)日：1988-11-01

申请号：US48289

申请日：1987-05-11

申请人： Richard L. Tolman ,  John D. Karkas ,  Wallace T. Ashton

发明人： Richard L. Tolman ,  John D. Karkas ,  Wallace T. Ashton

IPC分类号： C07D473/18 ,  A61K31/52 ,  A61K31/522 ,  A61P31/12 ,  C07D473/00

CPC分类号： C07D473/00

摘要： 9-[2-(Hydroxymethyl)cycloalkylmethyl]guanines which are herpes simplex viral thymidine kinase inhibitors, their acyl derivatives, their phosphate derivatives and their pharmaceutically-acceptable salts; pharmaceutical formulations containing these compounds; the treatment of DNA viral, particularly herpes viral, infections with these compounds; methods of preparing these compounds; and novel intermediates useful in their preparation.

公开(公告)号：US4277603A

公开(公告)日：1981-07-07

申请号：US19986

申请日：1979-03-12

申请人： Richard L. Tolman ,  Wallace T. Ashton ,  Ronald D. Brown

发明人： Richard L. Tolman ,  Wallace T. Ashton ,  Ronald D. Brown

IPC分类号： C07D239/54 ,  C07D239/545 ,  C07D471/04 ,  C07H15/18

CPC分类号： C07D239/545 ,  C07D471/04 ,  C07H15/18

摘要： This invention relates generally to a novel process for preparing 5-deazariboflavins by the cyclization of the corresponding 6-(N-substituted arylamino)uracils with trialkylorthoformate in the presence of a strong acid catalyst. An improved process for preparing the uracil intermediate is also disclosed. More particularly, it is concerned with the process for preparing 5-deazariboflavin by cyclizing 6-[3,4-dimethyl-N-(D-ribityl)anilino[uracil with trialkylorthoformate in the presence of a strong acid catalyst and hydrolyzing the resulting alkoxymethylene derivative. The corresponding uracil intermediate is prepared by reacting 6-chlorouracil with N-D-ribityl-3,4-xylidine.5-Deazariboflavins having the general Formula (I) herein below: ##STR1## wherein R.sub.7 is hydrogen or methyl, R.sub.8 is methyl, hydroxy or acyloxy and R.sub.10 is a ribityl group and the corresponding acyl and alkoxymethylene derivatives are useful as riboflavin antagonists with particular utility for the chemotherapy of coccidiosis in chickens or as intermediates for the preparation of said antagonists. The bis(alkoxymethylene) derivatives described herein are useful as prodrug forms of 5-deazariboflavins.When used for the treatment of coccidiosis, such compounds are administered to the animals by way of the feed and are effective in preventing coccidiosis when administered at levels of from about 0.0005% to about 0.05% by weight of the total feed consumed, the amount required for optimum prevention or control of the disease varying with the particular compound employed.

摘要翻译： 本发明一般涉及在强酸催化剂存在下，通过使相应的6-（N-取代的芳基氨基）尿嘧啶与三烷基原甲酸酯环化制备5-脱氮黄素的新方法。 还公开了一种制备尿嘧啶中间体的改进方法。 更具体地说，它涉及通过在强酸催化剂存在下使6- [3,4-二甲基-N-（D-核糖基）苯胺基[尿嘧啶与三烷基原甲酸酯]环化来制备5-脱氮黄素的方法，并水解得到的烷氧基亚甲基 衍生物。 通过6-氯尿嘧啶与N-D-核糖基-3,4-二甲苯胺反应制备相应的尿嘧啶中间体。 具有下述通式（I）的5-脱氮维生素：其中R 7是氢或甲基，R 8是甲基，羟基或酰氧基，R 10是ribityl基团，并且相应的酰基和烷氧基亚甲基衍生物可用作特定的核黄素拮抗剂 用于鸡的球虫病化疗或用作制备所述拮抗剂的中间体的效用。 本文所述的双（烷氧基亚甲基）衍生物可用作5-脱氮白蛋白的前药形式。 当用于治疗球虫病时，通过饲料将这些化合物施用于动物，并且当以所消耗的总饲料的约0.0005重量％至约0.05重量％的水平施用量时，有效地预防球虫病，所需量 用于最佳预防或控制随所用特定化合物变化的疾病。

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：US5780437A

公开(公告)日：1998-07-14

申请号：US760816

申请日：1996-12-05

申请人： Mark Goulet ,  Wallace T. Ashton ,  Lin Chu ,  Michael H. Fisher ,  Narindar N. Girotra ,  Peter Lin ,  Matthew J. Wyvratt

发明人： Mark Goulet ,  Wallace T. Ashton ,  Lin Chu ,  Michael H. Fisher ,  Narindar N. Girotra ,  Peter Lin ,  Matthew J. Wyvratt

IPC分类号： C07D20060101 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D487/08 ,  A61K38/00 ,  A61K31/40 ,  A61K31/54

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D487/08

摘要： There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

摘要翻译： 公开了式（I）的化合物及其药学上可接受的盐，其可用作GnRH的拮抗剂，因此可用于治疗两种男性中各种性激素相关和其他病症 和妇女。

公开(公告)号：US5559135A

公开(公告)日：1996-09-24

申请号：US306271

申请日：1994-09-14

申请人： Wallace T. Ashton ,  Linda L. Chang ,  William J. Greenlee

发明人： Wallace T. Ashton ,  Linda L. Chang ,  William J. Greenlee

IPC分类号： A61K45/06 ,  C07D405/12 ,  A61K31/44

CPC分类号： C07D405/12 ,  A61K45/06

摘要： Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.

摘要翻译： 苯氧基苯基乙酸和一般结构式I的衍生物具有内皮素拮抗剂活性，可用于治疗心血管疾病，如高血压，缺血性肾衰竭，血管痉挛，脑和心脏缺血，心肌梗死，内毒素性休克，良性前列腺增生 ，包括雷诺氏病和哮喘的炎性疾病。

公开(公告)号：US5538991A

公开(公告)日：1996-07-23

申请号：US306275

申请日：1994-09-14

申请人： Wallace T. Ashton ,  Linda L. Chang ,  William J. Greenlee

发明人： Wallace T. Ashton ,  Linda L. Chang ,  William J. Greenlee

IPC分类号： C07D317/60 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/41

CPC分类号： C07D405/12 ,  C07D317/60 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.

摘要翻译： 苯氧基苯基乙酸和一般结构式I的衍生物具有内皮素拮抗剂活性，可用于治疗心血管疾病，如高血压，缺血性肾衰竭，血管痉挛，脑和心脏缺血，心肌梗死，内毒素性休克，良性前列腺增生 ，包括雷诺氏病和哮喘的炎性疾病。

公开(公告)号：US5411980A

公开(公告)日：1995-05-02

申请号：US994228

申请日：1992-12-21

申请人： Wallace T. Ashton ,  Linda L. Chang ,  Malcolm MacCoss ,  Prasun K. Chakravarty ,  William J. Greenlee ,  Arthur A. Patchett ,  Kelly Flanagan

发明人： Wallace T. Ashton ,  Linda L. Chang ,  Malcolm MacCoss ,  Prasun K. Chakravarty ,  William J. Greenlee ,  Arthur A. Patchett ,  Kelly Flanagan

IPC分类号： C07D249/12 ,  C07D249/14 ,  C07D401/14 ,  C07D403/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  A61K31/41

CPC分类号： C07D401/14 ,  C07D249/12 ,  C07D249/14 ,  C07D403/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10

摘要： There are disclosed new substituted triazolinone, triazolinethione, and triazolinimine compounds which are useful as angiotensin II antagonists. These compounds have the general formula: ##STR1## wherein G is R.sup.1 or ##STR2##

摘要翻译： 公开了可用作血管紧张素II拮抗剂的新的取代的三唑啉酮，三唑啉硫酮和三唑啉亚胺化合物。 这些化合物具有以下通式：其中G为R 1或