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1. 发明授权

US5234936A Pyrimidocycloalkanes as a II antagonists 失效
公开(公告)号：US5234936A
公开(公告)日：1993-08-10
申请号：US782017
申请日：1991-10-24
申请人： John L. Primeau , Lloyd M. Garrick , Timothy D. Ocain , Richard M. Soll , Paul J. Dollings
发明人： John L. Primeau , Lloyd M. Garrick , Timothy D. Ocain , Richard M. Soll , Paul J. Dollings
IPC分类号： C07D239/74 , A61K31/505 , A61K31/517 , A61P3/06 , A61P9/00 , A61P9/12 , C07D239/70 , C07D239/78 , C07D239/80 , C07D239/94 , C07D239/95 , C07D403/12
CPC分类号： C07D403/12 , C07D239/70 , C07D239/94
摘要： There are disclosed compounds of the general formula I: ##STR1## wherein X is H, NR.sup.12 R.sup.13, OR.sup.14, CN, F, Cl, I, Br, perfluoroalkyl, alkyl, alkoxy, alkyl-OH, alkoxyalkyl, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13 ;Y is NR.sup.15, NR.sup.18 CR.sup.16 R.sup.17, CR.sup.16 R.sup.17 NR.sup.15 ;R.sup.1 is 5-tetrazolyl, CO.sub.2 R.sup.14, SO.sub.3 H, NHSO.sub.2 CH.sub.3, NHSO.sub.2 CF.sub.3 ;R.sup.2, R.sup.3 is H, alkyl, alkoxy, alkoxyalkyl, alkyl-OH perfluoroalkyl, aralkyl, CN, NO.sub.2, SO.sub.2 R.sup.19, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13, OR.sup.14, F, Cl, Br, I, NR.sup.12 R.sup.13 ;R.sup.4 -R.sup.11 is H, F, alkyl, alkoxy, alkoxyalkyl, --OCOR.sup.14, alkyl-OH, perfluoroalkyl, aralkyl, aryl, CN, NO.sub.2, SO.sub.2 R.sup.19, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13, OH, OR.sup.14, --NR.sup.12 R.sup.13, any two geminal groups can be O or CH.sub.2 ;R.sup.12, R.sup.13 is H, alkyl, aralkyl;R.sup.14 is H, alkyl, aralkyl, alkoxyalkyl;R.sup.15 is H, alkyl, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, alkoxyalkyl, aralkyl, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13, OR.sup.14, perfluoroalkyl, alkyl-OH, --COR.sup.14, --CONR.sup.12 R.sup.13 ;R.sup.16, R.sup.17 is H, alkyl, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, CN, NO.sub.2, SO.sub.2 R.sup.19, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13 ;R.sup.18 is H, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, OR.sup.14, --(CH.sub.2).sub.n CO.sub.2 R.sup.14, --(CH.sub.2).sub.n CONR.sup.12 R.sup.13, alkyl, --COR.sup.14, --CONR.sup.12 R.sup.13 ;R.sup.19 is alkyl, aralkyl;n is 0, 1, 2 or 3;m is 1-5;wherein alkyl is defined as 1-8 carbons, branched or straight chain; perfluoroalkyl is defined as 1-6 carbons; aralkyl is defined as 7-12 carbons or 7-12 carbons substituted with fluorine, bromine or chlorine; aryl is defined as 6-10 carbons or 6-10 carbons substituted with fluorine, bromine or chlorine and the pharmaceutically acceptable salts, solvates and hydrates thereof, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension and congestive heart-failure. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.

2. 发明授权

US06221902B1 Biphenyl sulfonyl aryl carboxylic acids useful in the treatment of insulin resistance and hyperglycemia 失效
公开(公告)号：US06221902B1
公开(公告)日：2001-04-24
申请号：US09307888
申请日：1999-05-10
申请人： Michael S. Malamas , Folake O. Adebayo , Paul J. Dollings
发明人： Michael S. Malamas , Folake O. Adebayo , Paul J. Dollings
IPC分类号： A61K31343
CPC分类号： C07D307/80 , C07D263/32 , C07D333/16 , C07D333/56
摘要： This invention provides compounds of Formula I having the structure wherein A, Q, R3, and R4 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

3. 发明授权

US06187755B1 Benzylmaltosides as inhibitors of smooth muscle cell proliferation 失效
标题翻译：苄基麦芽糖苷作为平滑肌细胞增殖的抑制剂
公开(公告)号：US06187755B1
公开(公告)日：2001-02-13
申请号：US09444076
申请日：1999-11-22
申请人： Paul J. Dollings
发明人： Paul J. Dollings
IPC分类号： A61K317016
CPC分类号： C07H15/18 , A61K31/7016 , A61K31/7028 , A61K31/7042
摘要： This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure Y is hydrogen, halogen, azido, or Het optionally substituted with R10; Het is 1,3-dioxo-1,3-dihydro-isoindol-2-yl, imidazol-1-yl, or benzimidazol-1-yl; R1, R2, R3 and R4, are each, independently, hydrogen, acyl of 2-7 carbon atoms, perfluoroacyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, benzoyl, or benzyl; R5 is hydrogen, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, halogen, nitrile, nitro, alkoxy of 1-6 carbon atoms; R6 and R 7, are each, independently, hydrogen, acyl of 2-7 carbon atoms, perfluoroacyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkylsulfonyl of 1-6 carbon atoms, perfluoroalkylsulfonyl of 1-6 carbon atoms, arylsulfonyl of 6-10 carbon atoms, or arylsulfonyl substituted with halo of 6-10 carbon atoms; R8 and R9, are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkyl of 1-6 carbon atoms, haloalkyl of 1-6 carbon atoms, nitriloalkyl of 1-6 carbon atoms, nitroalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, aryl of 6-10 carbon atoms, aryl of 6-10 carbon atoms substituted with R11, aralkyl of 7-12 carbon atoms or aralkyl of 7-12 carbon atoms substituted with R11; R10 is halogen, nitrile, nitro, amino, acylamino of 2-7 carbon atoms, perfluoroacylamino of 2-7 carbon atoms, carboxyl, carboxyaldehyde, perfluoroalkyl of 1-6 carbon atoms, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, perfluoroalkoxy of 1-6 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, aryl of 6-10 carbon atoms, or mercapto; R11 is halogen, nitrile, nitro, or perfluoroalkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有结构Y的结构式I的平滑肌细胞增殖抑制剂，其为任选被R 10取代的氢，卤素，叠氮基或Het; Het为1,3-二氧代-1,3-二氢 - 异吲哚-2-基，苯并咪唑-1-基或苯并咪唑-1-基; R 1，R 2，R 3和R 4各自独立地为氢，2-7个碳原子的酰基，2-7个碳原子的全氟酰基，1-6个碳原子的烷基， 1-6个碳原子的全氟烷基，苯甲酰基或苄基; R5是氢，1-6个碳原子的烷基，1-6个碳原子的全氟烷基，卤素，腈，硝基，1-6个碳原子的烷氧基; R6和R 7，各自独立地为氢，2-7个碳原子的酰基，2-7个碳原子的全氟酰基，1-6个碳原子的烷基，1-6个碳原子的全氟烷基，1-6个碳原子的烷基磺酰基，全氟烷基磺酰基 1-6个碳原子的芳基磺酰基或6-10个碳原子的卤素取代的芳基磺酰基; R8和R9各自独立地为氢，1-6个碳原子的烷基，烷基 1-6个碳原子的1-6个碳原子的卤代烷基，1-6个碳原子的次氮基烷基，1-6个碳原子的硝基烷基，1-6个碳原子的烷氧基，6-10个碳原子的芳基，被R11取代的6-10个碳原子，7-12个碳原子的芳烷基或被R11取代的7-12个碳原子的芳烷基; R10是2-7个碳原子的卤素，腈，硝基，氨基，酰基氨基，2- 7个碳原子，羧基，羧甲醛，1-6个碳原子的全氟烷基，1-6个碳原子的烷基，1-6个碳原子的烷氧基，1-6个碳原子的全氟烷氧基，2-7个碳原子的烷氧基羰基，全氟烷氧基羰基 2-7个碳原子的芳基或6-10个碳原子的芳基，或巯基; R11是1-6个碳原子的卤素，腈，硝基或全氟烷基; 或其药学上可接受的盐。

4. 发明授权

US5482942A (3,4-dioxocyclobuten-1-yl)chromene, indene, and dihydronaphthalenone derivatives as smooth muscle relaxants 失效
标题翻译：（3,4-二氧杂环丁烯-1-基）色烯，茚和二氢萘酮衍生物作为平滑肌松弛剂
公开(公告)号：US5482942A
公开(公告)日：1996-01-09
申请号：US267691
申请日：1994-06-28
申请人： Richard M. Soll , Paul J. Dollings
发明人： Richard M. Soll , Paul J. Dollings
IPC分类号： A61K31/35 , A61K31/352 , A61P9/00 , A61P9/02 , A61P11/00 , A61P13/02 , A61P15/00 , C07C225/20 , C07D311/58 , A61K31/495 , A61K31/415 , C07C229/40 , C07D211/82 , C07D241/02 , C07D311/74 , C07D407/02
CPC分类号： C07D311/58
摘要： This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.1-6 perfluoroacylamino, mono or di-C.sub.1-12 alkylamino, C.sub.1-6 alkylsulfonyl, C.sub.6-10 arylsulfonyl, carboxyl, C.sub.1-12 mono or di-alkylaminocarbonyl, or hydrogen;a and b together form an --O-- linkage, C.dbd.O, or a direct bond:R.sub.3 and R.sub.4, independent from each other, are H or C.sub.1-6 alkyl, optionally substituted by fluorine;R.sub.5 is amino or C.sub.1-12 mono alkylamine;R.sub.6 is H, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.6-10 aryl, or mono or bicyclic heteroaryl containing 1-3 heteroatoms selected from N, O, or S.
摘要翻译：本发明涉及具有平滑肌松弛活性的新型4-（3,4-二氧杂环丁烯-1-基）色烯和二氢萘酮及其3-（3,4-二氧杂环丁烯-1-基）茚及其盐，用于治疗高血压以及治疗周围血管疾病，充血性心力衰竭，涉及尿路过度平滑肌收缩的疾病，例如失禁或胃肠道，例如肠易激综合征，哮喘和脱发，以及药物组合物含有发明化合物。本发明公开了由式（I）表示的化合物：其中：R 1和R 2彼此独立地选自如下：C 1-6全氟烷氧基，C 1-6全氟烷基，C 1-6烷基，C 1 1-6烷氧基，羟基，C 1-6烷氧基羰基，硝基，氰基，卤素，C 1-6烷基磺酰氨基，C 1-6全氟烷基磺酰氨基，氨基，C 1-6酰氨基，C 1-6全氟酰基氨基，单或二-C 1-12烷基氨基， 6烷基磺酰基，C 6-10芳基磺酰基，羧基，C 1-12单或二烷基氨基羰基或氢; a和b一起形成O-键，C = O或直接键：R 3和R 4彼此独立地是H或任选被氟取代的C 1-6烷基; R5是氨基或C1-12单烷基胺; R 6是H，C 1-6全氟烷基，C 1-6烷基，C 6-10芳基或含有1-3个选自N，O或S的杂原子的单或双环杂芳基。

5. 发明授权

US07132402B2 Acylated benzylmaltosides as inhibitors of smooth muscle cell proliferation 有权
标题翻译：作为平滑肌细胞增殖的抑制剂的酰化苄基甲基卤化物
公开(公告)号：US07132402B2
公开(公告)日：2006-11-07
申请号：US10699233
申请日：2003-10-31
申请人： Scott Christian Mayer , Robert E. McDevitt , Paul J. Dollings
发明人： Scott Christian Mayer , Robert E. McDevitt , Paul J. Dollings
IPC分类号： A61K31/7036
CPC分类号： C07H17/02 , A61K31/704 , C07H5/06
摘要： This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure
摘要翻译：本发明提供具有该结构的式I的平滑肌细胞增殖抑制剂

6. 发明授权

US06248764B1 Furans, benzofurans, and thiophenes useful in the treatment of insulin resistance and hyperglycemia 失效
标题翻译：呋喃，苯并呋喃和噻吩可用于治疗胰岛素抵抗和高血糖
公开(公告)号：US06248764B1
公开(公告)日：2001-06-19
申请号：US09564496
申请日：2000-05-04
申请人： Paul J. Dollings , Robert E. McDevitt , Folake O. Adebayo
发明人： Paul J. Dollings , Robert E. McDevitt , Folake O. Adebayo
IPC分类号： A61K3141
CPC分类号： C07D307/42 , C07D307/46 , C07D307/80 , C07D307/81 , C07D333/22 , C07D333/56 , C07D409/12
摘要： This invention provides compounds of Formula I having the structure 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化合物及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。

7. 发明授权

US06063815A Benzopenones useful in the treatment of insulin resistance and hyperglycemia 失效
标题翻译：苯妥英酮可用于治疗胰岛素抵抗和高血糖症
公开(公告)号：US06063815A
公开(公告)日：2000-05-16
申请号：US307920
申请日：1999-05-10
申请人： Paul J. Dollings
发明人： Paul J. Dollings
IPC分类号： A61K31/192 , A61K31/216 , A61K31/24 , A61K31/12 , A61K31/135 , A61K31/195 , C07C229/00
CPC分类号： A61K31/216 , A61K31/192
摘要： This invention provides compounds of Formula I having the structure ##STR1## wherein Y is ##STR2## R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl mono-, di- or tri-substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy;R.sup.3 and R.sup.4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, hydroxyalkanoyl of 1-6 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, aminoalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, alkylsulfanyl of 1-6 carbon atoms, nitrile, nitro, amino, --NHSO.sub.2 CF.sub.3, carbamoyl, carboxyaldehyde, halogen, acyl of 1-6 carbon atoms, acylamino of 1-6 carbon atoms, 3-hydroxy-cyclobut-3-ene-4-yl-1,2-dione, pyridyl, isoxazolyl, pyrimidyl or pyrimidyl substituted with mercapto, tetronic acid, --OCOR.sup.8, --OR.sup.8R.sup.8 is aryl of 6-12 carbon atoms, aralkyl of 7-13 carbon atoms, monocyclic or bicyclic heteroaryl or a monocyclic or bicyclic heteroaralkyl, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms;R.sup.5 is hydrogen, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, perfluoroalkoxy of 1-6 carbon atoms, or halogen;X is --CH.sub.2 NR.sup.6 --, --NR.sup.6 --, or O;R.sup.6 and R.sup.7 are each, hydrogen or alkyl of 1-6 carbon atoms;Z is phenyl, naphthyl,or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
摘要翻译：本发明提供具有以下结构的式I化合物，其中Y为R 1且R 2各自独立地为氢，1-6个碳原子的烷基，卤素，1-6个碳原子的全氟烷基，3-8个碳原子的环烷基，噻吩基，呋喃基，苯基或被三氟甲基，氯，甲氧基或三氟甲氧基单，二或三取代的苯基; R 3和R 4各自独立地为氢，羧基，羟基，1-6个碳原子的羟基烷基，1-6个碳原子的羟基烷酰基，7-13个碳原子的芳氧基羰基，2-7个碳原子的烷氧基羰基，2-氟烷氧基羰基， 7个碳原子，1-6个碳原子的烷基，1-6个碳原子的全氟烷基，1-6个碳原子的氨基烷基，1-6个碳原子的烷基氨基，每个烷基1-6个碳原子的二烷基氨基，四唑基，巯基，1-6个碳原子的烷基硫烷基，腈，硝基，氨基，-NHSO 2 CF 3，氨基甲酰基，羧甲醛，卤素，1-6个碳原子的酰基，1-6个碳原子的酰基氨基，3-羟基 - 环丁-3-烯 - 吡啶基，异恶唑基，嘧啶基或被巯基取代的嘧啶基，-OCOR8，-OR8 R8是6-12个碳原子的芳基，7-13个碳原子的芳烷基，单环或双环杂芳基或单环或双环杂芳烷基，1-6个碳原子的烷基，1-6个碳原子的全氟烷基; R5是氢，1-6个碳原子的烷基，1-6个碳原子的全氟烷基，1-6个碳原子的烷氧基，1-6个碳原子的全氟烷氧基或卤素; X是-CH 2 NR 6 - ， - NR 6 - 或O; R6和R7各自为氢或1-6个碳原子的烷基; Z是苯基，萘基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。

8. 发明授权

US5500442A Cyclobut-3-ene-1,2-dione derivatives as smooth muscle relaxants 失效
标题翻译：环丁-3-烯-1,2-二酮衍生物作为平滑肌松弛剂
公开(公告)号：US5500442A
公开(公告)日：1996-03-19
申请号：US257998
申请日：1994-06-10
申请人： Richard M. Soll , Paul J. Dollings , William A. Kinney
发明人： Richard M. Soll , Paul J. Dollings , William A. Kinney
IPC分类号： A61K31/40 , A61P9/00 , A61P9/12 , A61P11/00 , A61P17/00 , A61P25/02 , C07D405/04 , C07D209/34
CPC分类号： C07D405/04
摘要： The present invention relates to novel cyclobut-3-ene-1,2-dione-3-yl substituted benzopyrans, indanes and tetrahydronaphthalenones having smooth muscle relaxant activity, pharmaceutical compositions containing them, and to their use in the treatment of diseases and disorders involving excessive smooth muscle contractions in the cardiovascular system, urinary tract, pulmonary system, or gastrointestinal tract.The compounds of this invention are represented by Formula (I): ##STR1## wherein: the substituents are as defined herein.
摘要翻译：本发明涉及新颖的环丁-3-烯-1,2-二酮-3-基取代的苯并吡喃，具有平滑肌松弛活性的茚满和四氢萘酮，含有它们的药物组合物及其用于治疗涉及心血管系统，尿路，肺系统或胃肠道过度平滑肌收缩。本发明的化合物由式（I）表示：其中：取代基如本文所定义。

9. 发明授权

US06683107B2 Furans, benzofurans, and thiophenes useful in the treatment of insulin resistance and hyperglycemia 失效
公开(公告)号：US06683107B2
公开(公告)日：2004-01-27
申请号：US10215311
申请日：2002-08-08
申请人： Paul J. Dollings , Robert E. McDevitt , Folake O. Adebayo
发明人： Paul J. Dollings , Robert E. McDevitt , Folake O. Adebayo
IPC分类号： A61K31381
CPC分类号： C07D307/42 , C07D307/46 , C07D307/80 , C07D307/81 , C07D333/22 , C07D333/56 , C07D409/12
摘要： This invention provides compounds of Formula I having the structure wherein R1 and R2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy; R3 and R4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, perfluoroalkoxy of 1-6 carbon atoms, alkanoyloxy of 2-7 carbon atoms, perfluoroalkanoyloxy of 2-7 carbon atoms, arylalkoxy of 7-15 carbon atoms, aryloxy of 6-12 carbon atoms, aroyloxy of 6-12 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamnino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, nitrile, nitro, amino, —NHSO2CF3, carbamoyl, carboxyaldehyde, halogen, acylamino, 3-hydroxy-cyclobut-3-ene-4-yl-1,2-dione, pyridyl, isoxazolyl, pyrimidyl or pyrimidyl substituted with mercapto, or tetronic acid; R5 is hydrogen, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, naphthalenylmethyl, benzyl or benzyl substituted with halogen, R6 and R7 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, or perfluoroalkyl of 1-6 carbon atoms, or R6 and R7 may be taken together as a diene unit having the structure —CH═CH—CH═CH—; W is S or O, X is —NR8CH2—, —NR8—, or O; R8 is hydrogen or alkyl; Y is carbonyl, methylene, ethyl, or —NHCH2—; Z is phenyl, pyridyl, naphthyl, thienyl, furyl, pyrrolyl, pyrazolyl, isoxazolyl, or isothiazolyl; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

10. 发明授权

US06451845B1 Furans, benzofurans, and thiophenes useful in the treatment of insulin resistance and hyperglycemia 失效
公开(公告)号：US06451845B1
公开(公告)日：2002-09-17
申请号：US09887672
申请日：2001-04-23
申请人： Paul J. Dollings , Robert E. McDevitt , Folake O. Adebayo
发明人： Paul J. Dollings , Robert E. McDevitt , Folake O. Adebayo
IPC分类号： A61K31381
CPC分类号： C07D307/42 , C07D307/46 , C07D307/80 , C07D307/81 , C07D333/22 , C07D333/56 , C07D409/12
摘要： This invention provides compounds of Formula I having the structure wherein R1 and R2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy; R3 and R4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, perfluoroalkoxy of 1-6 carbon atoms, alkanoyloxy of 2-7 carbon atoms, perfluoroalkanoyloxy of 2-7 carbon atoms, arylalkoxy of 7-15 carbon atoms, aryloxy of 6-12 carbon atoms, aroyloxy of 6-12 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, nitrile, nitro, amino, —NHSO2CF3, carbamoyl, carboxyaldehyde, halogen, acylamino, 3-hydroxy-cyclobut-3-ene-4-yl-1,2-dione, pyridyl, isoxazolyl, pyrimidyl or pyrimidyl substituted with mercapto, or tetronic acid; R5 is hydrogen, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, naphthalenylmethyl, benzyl or benzyl substituted with halogen, R6 and R7 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, or perfluoroalkyl of 1-6 carbon atoms, or R6 and R7 may be taken together as a diene unit having the structure —CH═CH—CH═CH—; W is S or O, X is —NR8CH2—, —NR8—, or O; R8 is hydrogen or alkyl; Y is carbonyl, methylene, ethyl, or —NHCH2—; Z is phenyl, pyridyl, naphthyl, thienyl, furyl, pyrrolyl, pyrazolyl, isoxazolyl, or isothiazolyl; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

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