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1. 发明授权

US4732978A Novel substituted naphthyloxymethyl quinoline derivatives as anti-inflammatory and antiallergy agents 失效
标题翻译：新型取代的萘氧基甲基喹啉衍生物作为抗炎和抗过敏剂
公开(公告)号：US4732978A
公开(公告)日：1988-03-22
申请号：US905619
申请日：1986-09-12
申请人： Anthony F. Kreft , Kenneth L. Kees , John H. Musser , James J. Bicksler , Winifred P. Howse
发明人： Anthony F. Kreft , Kenneth L. Kees , John H. Musser , James J. Bicksler , Winifred P. Howse
IPC分类号： C07D217/02 , C07D215/14 , C07D215/24 , C07D277/64 , A61K31/47 , C07D215/12
CPC分类号： C07D215/14 , C07D215/24 , C07D277/64
摘要： There are disclosed compounds having the formula ##STR1## wherein X is CR or N when n=1; orX is O, S, NR or CR when n=0;R is hydrogen or lower alkyl;Y is --CH.sub.2 --, --S--, --O-- or ##STR2## and A is ##STR3## Z is CH or N; R.sup.1 is halo or trifluoromethyl;R.sup.2 is hydrogen or halo;R.sup.3 is hydrogen or halo;with the proviso that when A is naphthyl, Y is --O-- and n=0, X is other than S; and their use in the treatment of inflammatory conditions and in the treatment of leukotriene-medicated naso-bronchial obstructive passageway conditions.
摘要翻译：公开了具有式“IMAGE”的化合物，其中当n = 1时X是CR或N; 或者当n = 0时X是O，S，NR或CR; R是氢或低级烷基; Y是-CH 2 - ， - S-，-O-或，A是Z是CH或N; R1是卤素或三氟甲基; R2是氢或卤素; R3是氢或卤素; 条件是当A是萘基时，Y是-O-和n = 0，X不是S; 并用于治疗炎症性疾病和治疗白三烯药物鼻支气管阻塞性通气条件。

2. 发明授权

US4528392A Aromatic compounds as antiallergic agents 失效
标题翻译：芳香族化合物作为抗过敏剂
公开(公告)号：US4528392A
公开(公告)日：1985-07-09
申请号：US601521
申请日：1984-04-18
申请人： John H. Musser , Kenneth L. Kees
发明人： John H. Musser , Kenneth L. Kees
IPC分类号： C07C205/35 , C07D207/26 , C07D207/277 , C07C101/44 , C07C83/10 , C07C153/023 , C07C153/03
CPC分类号： C07D207/277 , C07C205/35
摘要： There are disclosed compounds of the formula ##STR1## wherein X is OR.sup.2, SR.sup.2, N(R.sup.2).sub.2 or halo;W is --CH.sub.2 --, ##STR2## Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, ##STR3## m is 0-6; n is 0-6;p is 1-3;A is O or S;B is OR.sup.2, SR.sup.2 or N(R.sup.2).sub.2 ;R.sup.1 is hydrogen, loweralkyl, loweralkoxy or halo;R.sup.2 is hydrogen or loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.
摘要翻译：公开了下式的化合物：其中X是OR 2，SR 2，N（R 2）2或卤素; W是-CH 2 - ，Y是-CH 2 O-，-OCH 2 - ， - CH 2 S - ， - CH 2 - ， - n为0-6; p为1-3; A是O或S; B为OR2，SR2或N（R2）2; R1是氢，低级烷基，低级烷氧基或卤素; R2是氢或低级烷基; 及其药学上可接受的盐，以及它们在治疗白三烯介导的鼻支气管阻塞性空气通道病症如过敏性鼻炎，过敏性支气管哮喘等中的用途。

3. 发明授权

US5194435A 4-arylmethyl-5-alkyl-3h-pyrazol-3-ones 失效
标题翻译： 4-芳基甲基-5-烷基-3H-吡唑-3-酮
公开(公告)号：US5194435A
公开(公告)日：1993-03-16
申请号：US932139
申请日：1992-08-19
申请人： Kenneth L. Kees
发明人： Kenneth L. Kees
IPC分类号： C07D231/20 , C07D231/32
CPC分类号： C07D231/32 , C07D231/20
摘要： The compounds of the formula: ##STR1## in which the dotted lines represent optional unsaturation when n is 1 or 2 and X is CR.sup.5, Y is CR.sup.6 or X or Y are N; R.sup.1 is hydrogen, alkyl, aryl or arylalkyl; R.sup.2 is hydrogen, alkyl, aryl or arylalkyl; R.sup.3 is alkyl, perfluoromethyl or alkoxy; R.sup.4 is halogen, alkyl or alkoxy; X is CR.sup.5, O, S or N, in which R.sup.5 is hydrogen, halogen, alkyl, or alkoxy; Y is CR.sup.6, O, S or N, in which R.sup.6 is hydrogen, halogen, alkyl or alkoxy; n is one of the integers 0, 1 or 2; m is one of the integers 0, 1, 2, or 3; or a pharmaceutically acceptable salt thereof, with the provisos that one of X and Y is O,S or N and R.sup.3 is other than alkyl when n and m are 0 and X and Y are O, are useful hypolglycemic agents in the treatment of non-insulin dependent diabetes melitus.
摘要翻译：其中当n为1或2且X为CR 5时，虚线表示任选的不饱和度，Y为CR 6或X或Y为N的下式的化合物： R1是氢，烷基，芳基或芳烷基; R2是氢，烷基，芳基或芳基烷基; R3是烷基，全氟甲基或烷氧基; R4是卤素，烷基或烷氧基; X是CR 5，O，S或N，其中R 5是氢，卤素，烷基或烷氧基; Y是CR 6，O，S或N，其中R 6是氢，卤素，烷基或烷氧基; n是整数0,1或2之一; m是整数0,1,2或3之一; 或其药学上可接受的盐，条件是当n和m为0且X和Y为O时，X和Y中的一个为O，S或N，R3为烷基以外的其它烷基，可用于治疗非糖尿病中的低血糖剂胰岛素依赖性糖尿病。

4. 发明授权

US06281234B1 (2-Acylaminothiazole-4-yl)acetic acid derivative 失效
标题翻译：（2-酰基氨基噻唑-4-基）乙酸衍生物
公开(公告)号：US06281234B1
公开(公告)日：2001-08-28
申请号：US09307919
申请日：1999-05-10
申请人： Kenneth L. Kees
发明人： Kenneth L. Kees
IPC分类号： A61K31425
CPC分类号： A61K31/425
摘要： This invention provides compounds of Formula I having the structure wherein R1, R2 are both hydrogen or form a bond, or are each, independently, alkyl of 1-6 carbon atoms or aryl of 6-12 carbon atoms; m=0-10; n=1-3; and p=0-10; with the proviso that m+p is less than or equal to 15; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
摘要翻译：本发明提供具有结构的式I化合物，其中R1，R2均为氢或形成键，或各自独立地为1-6个碳原子的烷基或6-12个碳原子的芳基; m = 0-10; n = 1-3; andp = 0-10;条件是m + p小于或等于15;或其药学上可接受的盐，其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。

5. 发明授权

US4728739A Hypoglycemic thiazolidinediones 失效
标题翻译：低血糖噻唑烷二酮类
公开(公告)号：US4728739A
公开(公告)日：1988-03-01
申请号：US62268
申请日：1987-06-15
申请人： Kenneth L. Kees , Robert S. Cheeseman
发明人： Kenneth L. Kees , Robert S. Cheeseman
IPC分类号： C07D277/34
CPC分类号： C07D277/34
摘要： The compounds: ##STR1## in which R is hydrogen, lower alkyl, phenyl or benzyl, and R.sup.2 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt thereof, are useful hypoglycemic and hypoinsulinemic agents for the treatment of diabetes mellitus and cardiovascular disease states involved in elevated insulin levels such as atherosclerosis.
摘要翻译：化合物：其中R是氢，低级烷基，苯基或苄基，R 2是氢或低级烷基或其药学上可接受的盐，是用于治疗糖尿病和心血管疾病状态的有用的低血糖和低胰岛素药物涉及升高的胰岛素水平如动脉粥样硬化。

6. 发明授权

US5183825A 4-arylmethyl-5-alkyl-3H-pyrazol-3-ones and hypoglycemic use 失效
标题翻译： 4-芳基甲基-5-烷基-3H-吡唑-3-酮和降血糖用途
公开(公告)号：US5183825A
公开(公告)日：1993-02-02
申请号：US864986
申请日：1992-04-07
申请人： Kenneth L. Kees
发明人： Kenneth L. Kees
IPC分类号： C07D231/20 , C07D231/32
CPC分类号： C07D231/20 , C07D231/32
摘要： The compounds of the formula: ##STR1## in which the dotted lines represent optional unsaturation when X is CR.sup.5, Y is CR.sup.6 or X or Y are N; R.sup.1 is hydrogen, alkyl, aryl or arylalkyl; R.sup.2 is hydrogen, alkyl, aryl or arylalkyl; R.sup.3 is alkyl, perfluoromethyl or alkoxy; R.sup.4 is halogen, alkyl or alkoxy; X is CR.sup.5, O, S or N, in which R.sup.5 is hydrogen, halogen, alkyl, or alkoxy; Y is CR.sup.6, O, S or N, in which R.sup.6 is hydrogen, halogen, alkyl or alkoxy; n is one of the integers 0, 1 or 2; m is one of the integers 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof, are useful hypoglycemic agents in the treatment of non-insulin dependent diabetes mellitus.
摘要翻译：当X是CR 5，Y是CR 6或X或Y是N时，其中虚线表示可选的不饱和度的下式的化合物： R1是氢，烷基，芳基或芳烷基; R2是氢，烷基，芳基或芳基烷基; R3是烷基，全氟甲基或烷氧基; R4是卤素，烷基或烷氧基; X是CR 5，O，S或N，其中R 5是氢，卤素，烷基或烷氧基; Y是CR 6，O，S或N，其中R 6是氢，卤素，烷基或烷氧基; n是整数0,1或2之一; m是整数0,1,2或3之一; 或其药学上可接受的盐是用于治疗非胰岛素依赖性糖尿病的有效的降血糖剂。

7. 发明授权

US4845231A Tetrazoles and their use as hypoglycemic agents 失效
标题翻译：四唑类及其用作降血糖药
公开(公告)号：US4845231A
公开(公告)日：1989-07-04
申请号：US155386
申请日：1988-02-12
申请人： Kenneth L. Kees
发明人： Kenneth L. Kees
IPC分类号： C07D257/04 , C07D401/06
CPC分类号： C07D257/04 , C07D401/06
摘要： Compounds of the formula: ##STR1## in which R is a substituted or unsubstituted monocyclic or bicyclic alkyl group containing from 3 to 8 ring carbon atoms, wherein any substituent is alkyl of 1 to 3 carbon atoms, oxo, hydroxy, carboxy or when the hydroxy and carboxy substituents taken together they form a 1,3-carbonyloxy lactone ring closed structure;n is one of the integers 0, 1, 2 or 3;X is --O--, ##STR2## or --SO.sub.2 NH--; and Z is .dbd.CH-- or --N.dbd.;or a pharmaceutically acceptable salt thereof, are anti-hyperglycemic agents.
摘要翻译：下式的化合物：其中R是含有3至8个环碳原子的取代或未取代的单环或双环烷基，其中任何取代基是1至3个碳原子的烷基，氧代，羟基，羧基，或当羟基和羧基取代基一起形成1,3-羰氧基内酯环封闭结构; n是整数0,1,2或3之一; X是-O-，或-SO 2 NH-; 且Z为= CH-或-N =; 或其药学上可接受的盐是抗高血糖剂。

8. 发明授权

US5274111A Trifluoromethyl substituted 1H-pyrazoles and derivatives thereof 失效
标题翻译：三氟甲基取代的1H-吡唑及其衍生物
公开(公告)号：US5274111A
公开(公告)日：1993-12-28
申请号：US56967
申请日：1993-05-03
申请人： Kenneth L. Kees
发明人： Kenneth L. Kees
IPC分类号： A61K31/415 , C07D231/20
CPC分类号： A61K31/415
摘要： The compounds of the formulae: ##STR1## in which R.sup.1 is alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy of 1 to 6 carbon atoms, alkylthio, perfluoroalkylthio, alkylsulfinyl, alkylamino, halo, alkanoyl, 1-hydroxyalkyl or 1-(hydroxyimino) alkyl;R.sup.2 is hydrogen or alkyl of 1 to 3 carbon atoms;R.sup.3 is alkyl of 1 to 3 carbon atoms;R.sup.4 is alkyl of 1 to 6 carbon atoms;or a pharmaceutically acceptable salt thereof, are antihyperglycemic agents.
摘要翻译：下式的化合物：其中R 1是烷基，全氟烷基，烷氧基，1至6个碳原子的全氟烷氧基，烷硫基，全氟烷硫基，烷基亚磺酰基，烷基氨基，卤代，烷酰基， - 羟烷基或1-（羟基亚氨基）烷基; R2是氢或1至3个碳原子的烷基; R3是1〜3个碳原子的烷基; R4是1至6个碳原子的烷基; 或其药学上可接受的盐是抗高血糖剂。

9. 发明授权

US5264451A Process for treating hyperglycemia using trifluoromethyl substituted 3H-pyrazol-3-ones 失效
标题翻译：使用三氟甲基取代的3H-吡唑-3-酮处理高血糖的方法
公开(公告)号：US5264451A
公开(公告)日：1993-11-23
申请号：US864990
申请日：1992-04-07
申请人： Kenneth L. Kees
发明人： Kenneth L. Kees
IPC分类号： A61K31/415
CPC分类号： A61K31/415 , Y10S514/866
摘要： The compound of the formula: ##STR1## in which the dotted lines represent two sites of unsaturation appropriately located based on the identity of R.sup.2, R.sup.3 and R.sup.4 and, R.sup.1 is alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, alkylthio, perfluoroalkylthio, alkylsulfinyl, alkylamino, halo, alkanoyl, 1-hydroxyalkyl or (1-hydroxyimino) alkyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or alkyl; R.sup.4 is hydrogen or alkyl; n is 0 or 1; or a pharmaceutically acceptable salt thereof, are antihyperglycemic agents.
摘要翻译：其中虚线表示基于R 2，R 3和R 4的同一性适当定位的两个不饱和位置，且R1是烷基，全氟烷基，烷氧基，全氟烷氧基，烷硫基，全氟烷硫基，烷基亚磺酰基，烷基氨基，卤素，烷酰基，1-羟基烷基或（1-羟基亚氨基）烷基; R2是氢或烷基; R3是氢或烷基; R4是氢或烷基; n为0或1; 或其药学上可接受的盐是抗高血糖剂。

10. 发明授权

US4764623A N-(1H-tetrazol-5-yl-alkylphenyl)polyfluoroalkanamides 失效
标题翻译： N-（1H-四唑-5-基 - 烷基苯基）多氟烷酰胺
公开(公告)号：US4764623A
公开(公告)日：1988-08-16
申请号：US62270
申请日：1987-06-15
申请人： Kenneth L. Kees
发明人： Kenneth L. Kees
IPC分类号： C07D257/04
CPC分类号： C07D257/04 , Y10S514/866 , Y10S514/884
摘要： Compounds of the formula: ##STR1## where R is hydrogen or A--(CF.sub.2).sub.m --CH.sub.2 --; A is --F or --H; n is an integer from 1 to 10, inclusive; m is an integer from 0 to 9, inclusive; p is an integer from 0 to 4, inclusive; and Y is hydrogen, halo, trifluoromethyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, or hydroxy; or a pharmaceutically acceptable salt thereof. The compounds are useful as anti-hyperglycemic and anti-hyperinsulinemic agents.
摘要翻译：下式的化合物：其中R是氢或A-（CF 2）m -CH 2 - ; A是-F或-H; n为1〜10的整数，包括1和10; m为0〜9的整数，包括0和9; p为0〜4的整数，包括0和4; Y为氢，卤素，三氟甲基，1至6个碳原子的烷基，1至6个碳原子的烷氧基或羟基; 或其药学上可接受的盐。该化合物可用作抗高血糖和抗高血胰岛素药物。

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