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11. 发明授权

US07026316B2 Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes 失效
标题翻译：二肽基肽酶抑制剂用于治疗或预防糖尿病
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。

12. 发明授权

US5436259A Substituted 1,2,4-triazolin-3-one compounds bearing acidic functional groups as balanced angiotensin II antagonists 失效
标题翻译：具有酸性官能团的取代的1,2,4-三唑啉-3-酮化合物作为平衡血管紧张素II拮抗剂
公开(公告)号：US5436259A
公开(公告)日：1995-07-25
申请号：US154883
申请日：1993-11-18
申请人： Wallace T. Ashton , Prasun K. Chakravarty , Linda L. Chang
发明人： Wallace T. Ashton , Prasun K. Chakravarty , Linda L. Chang
IPC分类号： C07D249/12 , C07D413/10 , C07D417/10 , C07D419/10 , A61K31/41
CPC分类号： C07D413/10 , C07D249/12 , C07D417/10 , C07D419/10
摘要： Novel substituted 1,2,4-triazolin-3-ones of the formula (I) are useful as angiotensin II antagonists. ##STR1##
摘要翻译：式（I）的新型取代的1,2,4-三唑啉-3-酮可用作血管紧张素II拮抗剂。我

13. 发明授权

US5114925A Renin inhibitors containing the 2-[[(2R,3S)-3-amino-4-cyclohexyl-2-hydroxy-1-butyl]thio)alkanoyl moiety and the corresponding sulfoxide and sulfone derivatives 失效
标题翻译：含有2 - [[（2R，3S）-3-氨基-4-环己基-2-羟基-1-丁基]硫基）烷酰基部分和相应的亚砜和砜衍生物的肾素抑制剂
公开(公告)号：US5114925A
公开(公告)日：1992-05-19
申请号：US756632
申请日：1991-09-09
申请人： Wallace T. Ashton , Christine L. Cantone , Richard L. Tolman
发明人： Wallace T. Ashton , Christine L. Cantone , Richard L. Tolman
IPC分类号： A61K38/00 , C07C317/44 , C07C323/52 , C07D207/46 , C07D233/54 , C07D295/108 , C07D295/13 , C07D303/36 , C07K5/02
CPC分类号： C07D233/64 , C07C317/44 , C07C323/52 , C07D207/46 , C07D295/108 , C07D295/13 , C07D303/36 , C07K5/0227 , A61K38/00
摘要： Compounds of the formula: ##STR1## which are potent inhibitors of human renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory compounds, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these conditions which employ these novel compounds.
摘要翻译：下式的化合物：其是人肾素的有效抑制剂，可用于治疗各种形式的肾素相关性高血压，醛固酮增多症和充血性心力衰竭; 含有这些肾素抑制性化合物的组合物，任选与其它抗高血压药物组合; 以及治疗高血压，醛固酮增多症或充血性心力衰竭的方法，或在使用这些新化合物的这些病症中建立肾素作为致病因子。

14. 发明授权

US5110799A Antiherpetic agents 失效
标题翻译：抗菌剂
公开(公告)号：US5110799A
公开(公告)日：1992-05-05
申请号：US386071
申请日：1989-07-28
申请人： Richard L. Tolman , Wallace T. Ashton , Mu T. Wu
发明人： Richard L. Tolman , Wallace T. Ashton , Mu T. Wu
IPC分类号： A61K38/00 , A61P31/12 , A61P31/22 , C07D233/54 , C07K5/06 , C07K5/072 , C07K5/078 , C07K5/08 , C07K5/097
CPC分类号： C07D233/64 , C07K5/06113 , C07K5/06139 , C07K5/06147 , A61K38/00
摘要： A series of carboxyl-containing N-alkyldipeptides have been found to posess antiviral potency--specifically against herpes simplex virus--by selectively inhibiting the viral ribonucleotide reductase enzyme.

15. 发明授权

US4017503A Antifungal 1-substituted benzimidazoles 失效
标题翻译：抗真菌剂1-取代苯并咪唑
公开(公告)号：US4017503A
公开(公告)日：1977-04-12
申请号：US586438
申请日：1975-06-12
申请人： Wallace T. Ashton , Edward F. Rogers
发明人： Wallace T. Ashton , Edward F. Rogers
IPC分类号： C07D417/04 , A01N20060101 , A01N47/16 , A61K31/425 , C07C68/02 , C07D20060101 , C07D277/20 , C07D417/00
CPC分类号： C07C68/02
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 exhibiting particularly useful hydrophilic and lypophilic effects. 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 loweralkoxy or phenylloweralkoxy substituted ethoxy or polyethoxy carbonyl group of a chain with up to 4 ethoxy groups connected to the carbonyl. The compounds are generally prepared by contacting a 1-unsubstituted benzimidazole with a loweralkoxy or phenylloweralkoxy substituted ethoxy or polyethoxy chloroformate.
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虫剂，其表现出特别有用的亲水性和溶血性作用。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-位取代基是具有与羰基连接的多达4个乙氧基的链的低级烷氧基或苯基低级烷氧基取代的乙氧基或聚乙氧基羰基。通常通过使1-未取代的苯并咪唑与低级烷氧基或苯基低级烷氧基取代的乙氧基或聚乙氧基氯甲酸酯接触来制备化合物。

16. 发明授权

US07238683B2 Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes 有权
标题翻译：稠合苯丙氨酸衍生物作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病
公开(公告)号：US07238683B2
公开(公告)日：2007-07-03
申请号：US10573108
申请日：2004-10-29
申请人： Wallace T. Ashton , Hong Dong , Jinyou Xu
发明人： Wallace T. Ashton , Hong Dong , Jinyou Xu
IPC分类号： C07D207/04 , C07D401/10 , C07D403/10 , C07D487/04 , A61K31/40 , A61K31/4439 , A61K31/454 , A61K31/437 , A61K31/4985 , A61K31/506 , A61K31/4725 , A61P3/10
CPC分类号： C07D207/10 , A61K38/00 , C07D205/04
摘要： The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV 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-RV抑制剂”）的抑制剂的稠合苯丙氨酸衍生物，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如作为糖尿病，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。

17. 发明授权

US5312820A Substituted carbamoyl and oxycarbonyl derivatives of biphenylmethylamines 失效
标题翻译：联苯基甲基胺的取代氨基甲酰基和氧羰基衍生物
公开(公告)号：US5312820A
公开(公告)日：1994-05-17
申请号：US917642
申请日：1992-07-17
申请人： Wallace T. Ashton , Linda L. Chang , William J. Greenlee , Steven M. Hutchins , Ralph A. Rivero
发明人： Wallace T. Ashton , Linda L. Chang , William J. Greenlee , Steven M. Hutchins , Ralph A. Rivero
IPC分类号： C07C311/51 , C07D209/08 , C07D213/75 , C07D215/08 , C07D215/22 , C07D215/227 , C07D215/38 , C07D215/48 , C07D219/16 , C07D231/56 , C07D235/06 , C07D239/42 , C07D241/42 , C07D257/04 , C07D265/36 , C07D265/38 , C07D279/16 , C07D401/12 , A61K31/47 , A61K31/17 , A61K31/27 , A61K31/34 , A61K31/415 , A61K31/535 , A61K31/54 , C07C275/28 , C07D207/16 , C07D275/04 , C07D295/22
CPC分类号： C07D215/38 , C07C311/51 , C07D209/08 , C07D213/75 , C07D215/08 , C07D215/227 , C07D215/48 , C07D219/16 , C07D231/56 , C07D235/06 , C07D239/42 , C07D241/42 , C07D257/04 , C07D265/36 , C07D265/38 , C07D279/16 , C07D401/12
摘要： Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT.sub.1 and AT.sub.2 activity useful in the treatment of hypertension and related disorders and ocular hypertension. ##STR1## where X is --O-- or --N(R.sup.7)--.
摘要翻译：结构I的联苯甲胺的氨基甲酰基和氧羰基衍生物是具有平衡的AT1和AT2活性的血管紧张素-II拮抗剂，其用于治疗高血压和相关疾病和高眼压症。其中X是-O-或-N（R 7） - 。

18. 发明授权

US5281614A Substituted 1,2,4-triazoles bearing acidic functional groups as angiotensin II antagonists 失效
标题翻译：取代的具有酸性官能团的1,2,4-三唑作为血管紧张素II拮抗剂
公开(公告)号：US5281614A
公开(公告)日：1994-01-25
申请号：US970360
申请日：1992-11-02
申请人： Wallace T. Ashton , Prasun K. Chakravarty , Linda L. Chang , William J. Greenlee , Dooseop Kim , Nathan B. Mantlo , Arthur A. Patchett
发明人： Wallace T. Ashton , Prasun K. Chakravarty , Linda L. Chang , William J. Greenlee , Dooseop Kim , Nathan B. Mantlo , Arthur A. Patchett
IPC分类号： A61K31/395 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/41 , A61K31/4196 , A61K31/4245 , A61K31/425 , A61K31/433 , A61K31/54 , A61K31/675 , A61P9/10 , A61P9/12 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , C07D209/48 , C07D249/12 , C07D249/14 , C07D271/06 , C07D285/10 , C07D291/04 , C07D291/06 , C07D401/10 , C07D403/10 , C07D405/10 , C07D413/10 , C07D417/10 , C07D419/10 , C07F9/6518 , C07F9/6558 , A61K31/505 , A61K31/535 , C07D249/10
CPC分类号： C07D413/10 , C07D249/12 , C07D417/10 , C07D419/10
摘要： Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists. ##STR1##
摘要翻译：式I的新型取代的三唑啉酮，三唑啉硫酮和三唑啉亚胺化合物可用作血管紧张素II拮抗剂。（*化学结构*）（I）

19. 发明授权

US5262412A Substituted pyrazoles, compositions and use 失效
标题翻译：取代的吡唑，组合物和用途
公开(公告)号：US5262412A
公开(公告)日：1993-11-16
申请号：US28845
申请日：1993-03-10
申请人： Wallace T. Ashton , Linda L. Chang , William J. Greenlee , Steven M. Hutchins
发明人： Wallace T. Ashton , Linda L. Chang , William J. Greenlee , Steven M. Hutchins
IPC分类号： A61K31/415 , C07D231/12 , C07D231/14 , C07D413/12
CPC分类号： C07D231/14 , A61K31/415
摘要： Substituted pyrazole compounds are angiotensin II antagonists and therefore useful in the treatment of hypertension, and related cardiovascular disorders and ocular hypertension. These compounds have the general formula I: ##STR1##
摘要翻译：取代的吡唑化合物是血管紧张素II拮抗剂，因此可用于治疗高血压，以及相关的心血管疾病和高眼压症。这些化合物具有通式I： I

20. 发明授权

US5187179A Angiotensin II antagonists incorporating a substituted imidazo [1,2-b][1,2,4]triazole 失效
标题翻译：取代替咪唑（1,2-B）（1,2,4）三唑的ANGIOTENSIN II拮抗剂
公开(公告)号：US5187179A
公开(公告)日：1993-02-16
申请号：US673630
申请日：1991-03-22
申请人： Wallace T. Ashton , Steven M. Hutchins , Malcolm MacCoss
发明人： Wallace T. Ashton , Steven M. Hutchins , Malcolm MacCoss
IPC分类号： A61K31/415 , A61P9/12 , A61P27/02 , C07D249/08 , C07D487/04 , C07F9/6561
CPC分类号： C07D487/04 , C07F9/6561
摘要： There are disclosed substituted imidazo[1,2-b][1,2,4]triazole derivatives of Formula I which are useful as angiotensin II antagonists. ##STR1##

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