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公开(公告)号：US4079069A
公开(公告)日：1978-03-14
申请号：US794771
申请日：1977-05-09
IPC分类号： C07D471/04 , A23K1/16 , A61K31/505 , A61K31/675 , A61P33/02 , C07D521/00
CPC分类号： A61K31/505 , A23K20/116 , A61K31/675
摘要： 5-Deazariboflavin, its phosphate ester and nontoxic salts thereof and its novel bis(loweralkoxymethylene) derivatives have antiprotozoal and antiparasitic activity. They are particularly useful for controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance. The compounds are included in compositions useful for the prevention and treatment of coccidiosis in poultry.
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公开(公告)号：US4017504A
公开(公告)日：1977-04-12
申请号：US586439
申请日：1975-06-12
IPC分类号： C07C59/01 , C07D417/00
CPC分类号： C07C59/01
摘要： New water soluble benzimidazoles with a high degree of stability, which are substituted at the 1-position with carboxyalkoxycarbonyl substituents and at the 2-position with a 4-thiazolyl group are effective fungicides and anthelmintics. The compounds as well as processes for their preparation are described along with antifungal and anthelmintic compositions for their use. The 1-position substituent is a carboxyalkoxycarbonyl group of from 3 to 11 carbon atoms including certain salts and derivatives of the carboxy group. The compounds are generally prepared by contacting a 1-unsubstituted benzimidazole with a protected carboxyalkoxycarbonyl chloride.
摘要翻译： 具有高度稳定性的新的水溶性苯并咪唑在1-位被羧基烷氧基羰基取代基取代，在2-位被4-噻唑基取代是有效的杀真菌剂和驱肠虫剂。 该化合物及其制备方法与抗真菌和驱虫剂组合物一起使用。 1-位取代基是含有3-11个碳原子的羧基烷氧基羰基，包括某些盐和羧基衍生物。 通常通过使1-未取代的苯并咪唑与受保护的羧基烷氧基羰基氯接触来制备化合物。
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33.发明授权Bicyclic pyrimidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 有权二环嘧啶作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病公开(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。
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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。
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公开(公告)号：US5559135A
公开(公告)日：1996-09-24
申请号：US306271
申请日：1994-09-14
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。
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公开(公告)号：US5538991A
公开(公告)日：1996-07-23
申请号：US306275
申请日：1994-09-14
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。
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37.发明授权Substituted triazolinones, triazolinethiones, and triazolinimines as angiotensin II antagonists 失效作为血管紧张素II拮抗剂的取代的三唑啉酮，三唑啉硫酮和三唑啉亚胺
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
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公开(公告)号：US4406902A
公开(公告)日：1983-09-27
申请号：US285161
申请日：1981-07-23
IPC分类号： A61K31/40 , C07D213/70 , C07D213/80 , C07D233/84 , C07D239/56 , C07D257/04 , C07D277/36 , C07D477/10 , C07D477/20
CPC分类号： C07D213/70 , A61K31/40 , C07D213/80 , C07D239/56 , C07D257/04 , C07D277/36 , C07D477/10 , C07D477/20
摘要： Novel chemical compounds are provided which selectively inhibit the metabolism of dipeptidase (E.C.3.4.13.11) and therefore are useful in combination with antibacterial products. These chemical compounds are Z-2-(2,2-dimethylcyclo-propanecarboxamido)-.omega.-pyridylthio-2-alkenoic acids (and related arylthio and heterocyclylthio analogs).
摘要翻译： 提供了选择性抑制二肽酶代谢（E.C.3.4.13.11）的新型化合物，因此可与抗菌产品组合使用。 这些化合物是Z-2-（2,2-二甲基环丙烷甲酰氨基）-ω-吡啶基硫代-2-烯酸（和相关的芳硫基和杂环硫基类似物）。
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公开(公告)号：US4017505A
公开(公告)日：1977-04-12
申请号：US625335
申请日：1975-10-23
IPC分类号： C07D417/04 , C07D417/00
CPC分类号： C07D417/04
摘要： New benzimidazoles substituted at the 1-position with carbonyl substituents and at the 2-position with a 4-thiazolyl group are effective fungicides and anthelmintics. The compounds as well as processes for their preparation are described along with antifungal and anthelmintic compositions for their use. The 1-position substituent is a hydrocarbon group of from 5 to 12 carbon atoms connected to the carbonyl group through an oxygen or a sulfur atom. The compounds are generally prepared by contacting a 1-unsubstituted benzimidazole with a hydrocarbon radical substituted chloroformate or chlorothiol formate.
摘要翻译： 在1-位被羰基取代基取代的2-苯并咪唑和2-噻唑基的2-位是有效的杀真菌剂和驱肠虫剂。 该化合物及其制备方法与抗真菌和驱虫剂组合物一起使用。 1位取代基是通过氧或硫原子连接到羰基的5至12个碳原子的烃基。 通常通过使1-未取代的苯并咪唑与烃基取代的氯甲酸酯或氯代硫代甲酸酯接触来制备化合物。
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