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1. 发明授权

US06340687B1 Substituted tetrahydro-pyrimidine-2(1H)-thione HDL-C elevators useful as antiatherosclerotic agents 失效
标题翻译：用作抗动脉粥样硬化剂的取代的四氢嘧啶-2（1H） - 硫酮HDL-C电梯
公开(公告)号：US06340687B1
公开(公告)日：2002-01-22
申请号：US09145895
申请日：1998-09-02
申请人： Amedeo A. Failli , Jay S. Shumsky , Kevin A. Memoli , Donald P. Strike
发明人： Amedeo A. Failli , Jay S. Shumsky , Kevin A. Memoli , Donald P. Strike
IPC分类号： C07D23940
CPC分类号： C07D239/10
摘要： Antiatherosclerotic agents are provided having the following structure: wherein: R1 is hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, or phenylalkyl of 7-10 carbon atoms; and R2, R3, R4, R5, and R6 are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, aralkyl of 7-10 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy of 6-12 carbon atoms, aralkyloxy of 7-12 carbon atoms, fluoroalkoxy of 1-6 carbon atoms, trifluoromethyl, alkylthio of 1-3 carbon atoms, alkylsulfonyl of 1-3 carbon atoms, —SCF3, nitro, alkylamino in which the alkylamino moiety has 1-6 carbon atoms, or dialkylamino in which each alkyl group has 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译：提供具有以下结构的抗动脉粥样硬化剂：其中：R1是氢，1-6个碳原子的烷基，3-8个碳原子的环烷基，2-7个碳原子的链烯基，2-7个碳原子的炔基或苯基烷基 7-10个碳原子; 和R 2，R 3，R 4，R 5和R 6各自独立地为氢，卤素，1-6个碳原子的烷基，3-8个碳原子的环烷基，2-7个碳原子的烯基，2-7个碳原子的炔基 7-10个碳原子的芳烷基，1-6个碳原子的烷氧基，6-12个碳原子的芳氧基，7-12个碳原子的芳烷氧基，1-6个碳原子的氟烷氧基，三氟甲基，1-3个碳原子的烷硫基，1-3个碳原子的烷基磺酰基，-SCF 3，硝基，其中烷基氨基部分具有1-6个碳原子的烷基氨基，或每个烷基具有1-6个碳原子的二烷基氨基; 或其药学上可接受的盐。

2. 发明授权

US06268364B1 Substitued tetrahydro-1,3,5-triazin-2[1H]-thiones as anti-atherosclerotic agents 失效
标题翻译：将取代的四氢-1,3,5-三嗪-2 [1H] - 噻二唑作为抗动脉粥样硬化剂
公开(公告)号：US06268364B1
公开(公告)日：2001-07-31
申请号：US09483711
申请日：2000-01-14
申请人： Kevin A. Memoli , Donald P. Strike , Amedeo A. Failli , Robert J. Steffan
发明人： Kevin A. Memoli , Donald P. Strike , Amedeo A. Failli , Robert J. Steffan
IPC分类号： A61K3153
CPC分类号： C07D251/08
摘要： This invention provides compounds of formula 1 having the structure wherein R1, R2, R3, R4, and R5 are each independently, hydrogen, halogen, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkyl, alkoxy, aryloxy, fluoroalkoxy, trifluoromethyl, alkylthio, alkylsulfony, —SCF3, nitro, alkylamino, or dialkylamino; R6 is hydrogen, alkyl, cycloalkyl, or arylalkyl; and R7 is alkyl, cycloalkyl, or arylalkyl or a pharmaceutically acceptable salt thereof which are useful as antiatherosclerotic agents.
摘要翻译：本发明提供具有其中R 1，R 2，R 3，R 4和R 5各自独立地为氢，卤素，烷基，环烷基，烯基，炔基，苯基烷基，烷氧基，芳氧基，氟烷氧基，三氟甲基，烷硫基，烷基磺酰基， SCF 3，硝基，烷基氨基或二烷基氨基; R 6是氢，烷基，环烷基或芳基烷基; 和R7是可用作抗动脉粥样硬化剂的烷基，环烷基或芳烷基或其药学上可接受的盐。

3. 发明授权

US6160114A Substituted tetrahydro-1,3,5-triazin-2[1H]-thiones as anti-atherosclerotic agents 失效
标题翻译：取代的四氢-1,3,5-三嗪-2 [1H] - 噻二唑作为抗动脉粥样硬化剂
公开(公告)号：US6160114A
公开(公告)日：2000-12-12
申请号：US960832
申请日：1997-10-30
申请人： Kevin A. Memoli , Donald P. Strike , Amedeo A. Failli , Robert J. Steffan
发明人： Kevin A. Memoli , Donald P. Strike , Amedeo A. Failli , Robert J. Steffan
IPC分类号： A61P3/06 , A61P9/10 , C07D251/08 , C07D239/40
CPC分类号： C07D251/08
摘要： This invention provides compounds of formula 1 having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are each independently, hydrogen, halogen, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkyl, alkoxy, aryloxy, fluoroalkoxy, trifluoromethyl, alkylthio, alkylsulfony, --SCF.sub.3, nitro, alkylamino, or dialkylamino;R.sup.6 is hydrogen, alkyl, cycloalkyl, or arylalkyl; andR.sup.7 is alkyl, cycloalkyl, or arylalkylor a pharmaceutically acceptable salt thereof which are useful as antiatherosclerotic agents.
摘要翻译：本发明提供具有其中R 1，R 2，R 3，R 4和R 5各自独立地为氢，卤素，烷基，环烷基，烯基，炔基，苯基烷基，烷氧基，芳氧基，氟烷氧基，三氟甲基，烷硫基，烷基磺酰基，-SCF 3，硝基，烷基氨基或二烷基氨基; R6是氢，烷基，环烷基或芳基烷基; 并且R 7是可用作抗动脉粥样硬化剂的烷基，环烷基或芳烷基或其药学上可接受的盐。

4. 发明授权

US5861517A 2-thioxo-imidazolidin-4-one derivatives 失效
标题翻译： 2-硫代 - 咪唑烷-4-酮衍生物
公开(公告)号：US5861517A
公开(公告)日：1999-01-19
申请号：US749367
申请日：1996-11-21
申请人： Hassan M. Elokdah , Sie-Yearl Chai , Theodore S. Sulkowski , Donald P. Strike
发明人： Hassan M. Elokdah , Sie-Yearl Chai , Theodore S. Sulkowski , Donald P. Strike
IPC分类号： C07D233/86
CPC分类号： C07D233/86
摘要： The compound of formula I: ##STR1## in which R.sup.1 is alkyl or alkenyl; R.sup.2 is alkyl and R.sup.3 and R.sup.4 are, independently, hydrogen or alkyl; or R.sup.2 is hydrogen and R.sup.3 and R.sup.4 taken together are ortho substituted trimethylene or tetramethylene are useful for increasing blood serum HDL levels.
摘要翻译：式I化合物：其中R 1是烷基或链烯基; R2是烷基，R3和R4独立地是氢或烷基; 或R2是氢，R3和R4一起是邻位取代的三亚甲基或四亚甲基可用于增加血清HDL水平。

5. 发明授权

US5783707A 2-thioxo-imidazolidin-4-one derivatives 失效
标题翻译： 2-硫代 - 咪唑烷-4-酮衍生物
公开(公告)号：US5783707A
公开(公告)日：1998-07-21
申请号：US754440
申请日：1996-11-21
申请人： Hassan M. Elokdah , Sie-Yearl Chai , Theodore S. Sulkowski , Donald P. Strike
发明人： Hassan M. Elokdah , Sie-Yearl Chai , Theodore S. Sulkowski , Donald P. Strike
IPC分类号： C07D233/70 , C07D233/84 , C07D233/86
CPC分类号： C07D233/86
摘要： The compound of formula I ##STR1## in which R.sup.1 is alkyl; and R is alkyl, naphthyl, benzhydryl, fluorophenylmethyl, phenethyl, 1-(fluorophenyl)ethyl, 5-chloro-2-methoxyphenyl, trifluoromethoxyphenyl, trifluoromethylphenyl, methylsulfanylphenyl or pyridyl are useful for increasing blood serum HDL levels.
摘要翻译：式Ⅰ化合物其中R 1是烷基; 和R是烷基，萘基，二苯甲基，氟苯基甲基，苯乙基，1-（氟苯基）乙基，5-氯-2-甲氧基苯基，三氟甲氧基苯基，三氟甲基苯基，甲硫基苯基或吡啶基可用于提高血清HDL水平。

6. 发明授权

US5663363A 2-thioxo-imidazolidin-4-one derivatives 失效
标题翻译： 2-硫代 - 咪唑烷-4-酮衍生物
公开(公告)号：US5663363A
公开(公告)日：1997-09-02
申请号：US754449
申请日：1996-11-21
申请人： Hassan M. Elokdah , Sie-Yearl Chai , Theodore S. Sulkowski , Donald P. Strike
发明人： Hassan M. Elokdah , Sie-Yearl Chai , Theodore S. Sulkowski , Donald P. Strike
IPC分类号： C07D233/86 , C07D233/42 , C07D233/32
CPC分类号： C07D233/86
摘要： The compound of formula I ##STR1## in which R is alkynyl; and X and Y are, independently, alkyl, halo, perfluoralkyl, perfluoralkoxy, or, taken together, X and Y are ortho substituted trimethylene or tetramethylene are useful for increasing blood serum HDL levels.
摘要翻译：其中R是炔基的式Ⅰ化合物; 并且X和Y独立地是烷基，卤素，全氟烷基，全氟烷氧基，或者X和Y一起是邻位取代的三亚甲基或四亚甲基可用于增加血清HDL水平。

7. 发明授权

US5401769A Dibenzofuranyl N-alkyl carbamates 失效
标题翻译：二苯并呋喃基N-烷基氨基甲酸酯
公开(公告)号：US5401769A
公开(公告)日：1995-03-28
申请号：US190402
申请日：1994-02-02
申请人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
发明人： Thomas J. Commons , Richard E. Mewshaw , Donald P. Strike
IPC分类号： C07D307/91 , A61K31/34
CPC分类号： C07D307/91
摘要： A compound of formula A: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, cyano, nitro, alkyl, alkoxy, --CO.sub.2 H, alkylcarbonyl, alkylcarbonyloxy, alkoxycarbonyl, alkoxycarbonyloxy, mono or dialkylaminocarbonyl, or mono or dialkylaminocarbonyloxy; R.sup.3 is hydrogen or alkyl; R.sup.4 is alkyl, cycloalkylalkyl or phenylalkyl or substituted phenylalkyl, and the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl, are anti-cholesterolemic agents.
摘要翻译：式A的化合物：其中R 1和R 2独立地是氢，氟，氯，溴，碘，三氟甲基，氰基，硝基，烷基，烷氧基，-CO 2 H，烷基羰基，烷基羰基氧基，烷氧基羰基，或二烷基氨基羰基，或单或二烷基氨基羰基氧基; R3是氢或烷基; R4是烷基，环烷基烷基或苯基烷基或取代的苯基烷基，苯环上的取代基是烷基，烷氧基，卤素，硝基，氰基，三氟甲基或苯基，是抗胆固醇血症药。

8. 发明授权

US5179216A N,N', N'-trisubstituted-5-bisaminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-coa:cholesterol-acyl transferase 失效
标题翻译： N，N'，N'-三取代-5-联苯甲酰-1,3-二氧戊环-4,6-二酮的ACYL-COA：胆固醇 - 乙酸转移酶抑制剂
公开(公告)号：US5179216A
公开(公告)日：1993-01-12
申请号：US719873
申请日：1991-06-24
申请人： William F. Fobare , Donald P. Strike
发明人： William F. Fobare , Donald P. Strike
IPC分类号： A61K31/335 , A61K31/357 , A61P3/06 , A61P9/10 , C07D319/06 , C07D405/12 , C07F7/18
CPC分类号： C07D405/12 , C07D319/06 , C07F7/1852
摘要： The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is alkyl, hydroxyalkyl, alkenyl, cycloalkyl, phenylcycloalkyl, 1-hydroxymethylphenethyl, 1-(t-butyl)dimethylsilyloxymethyl-phenethyl, 1-(t-butyl)dimethylsilyloxymethylisopentyl, 1-hydroxymethylisopentyl, phenyl, benzyl or substituted phenyl or benzyl, where the substituents are alkyl, alkoxy, halogen, cyano, trifluoromethyl, amino, alkylamino, dialkylamino, nitro or phenyl, benzyl, phenethyl or R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino; R.sub.2 is alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.

9. 发明授权

US4743692A N-(pyridinylalkyl)-thieno-or benzo-isothiazol-3-amine derivatives 失效
标题翻译： N-（吡啶基烷基） - 噻吩并或苯并异噻唑-3-胺衍生物
公开(公告)号：US4743692A
公开(公告)日：1988-05-10
申请号：US913876
申请日：1986-09-30
申请人： Daniel M. Teller , Donald P. Strike , Arthur A. Santilli , Guy A. Schiehser
发明人： Daniel M. Teller , Donald P. Strike , Arthur A. Santilli , Guy A. Schiehser
IPC分类号： C07D417/12 , C07D513/04
CPC分类号： C07D417/12 , C07D513/04
摘要： A compound of the formula: ##STR1## in which A is a 3,4-; 3,2-; or 2,3-fused thieno- moiety or a benzo- moiety;X is alkylene of 2 to 5 carbon atoms;R.sup.1 is hydrogen, bromo or methyl;R.sup.2 is methoxy when R.sup.1 is hydrogen, methyl when R.sup.1 is bromo, and bromo when R.sup.1 is methyl;R.sup.3 is hydrogen or alkyl of 1 to 6 carbon atoms;R.sup.4 is hydrogen or alkyl of 1 to 6 carbon atoms;R.sup.3 and R.sup.4, taken together, are ethylene when X is ethylene;R.sup.5 is hydrogen when A is thieno, and when A is benzo, R.sup.5 is hydrogen, alkyl of 1 to 6 carbon atoms, halo or alkoxy of 1 to 6 carbon atoms;R.sup.6 is hydrogen when A is thieno, and when A is benzo, R.sup.5 is hydrogen, alkyl of 1 to 6 carbon atoms, halo, alkoxy of 1 to 6 carbon atoms, amino, nitro, sulfamoyl or pyridinyl;m is one of the integers 0 or 1;n is one of the integers 3, 4 or 5;p is one of the integers 0, 1 or 2; andthe dotted line in the thiazole ring represents unsaturation necessary to complete the 3,2- or 2,3- thieno- ring;or a pharmaceutically acceptable salt thereof are histamine H.sub.1 -antagonists useful in the treatment of various allergic reactions in the mammal.
摘要翻译：下式的化合物：其中A是3,4-; 3,2; 或2,3-稠合的噻吩并 - 部分或苯并 - 部分; X是2至5个碳原子的亚烷基; R1是氢，溴或甲基; 当R 1为氢时，R 2为甲氧基，当R 1为溴时，R 2为甲基; R3是氢或1至6个碳原子的烷基; R4是氢或1至6个碳原子的烷基; 当X是亚乙基时，R 3和R 4一起是乙烯; 当A为噻吩并且当A为苯甲基时，R 5为氢，R 5为氢，1至6个碳原子的烷基，卤素或1至6个碳原子的烷氧基; 当A为噻吩并且当A为苯甲基时，R 6为氢，R 5为氢，1至6个碳原子的烷基，卤素，1至6个碳原子的烷氧基，氨基，硝基，氨磺酰基或吡啶基; m是整数0或1之一; n是整数3,4或5之一; p是整数0,1或2之一; 并且噻唑环中的虚线表示完成3,2-或2,3-噻吩环所必需的不饱和键; 或其药学上可接受的盐是用于治疗哺乳动物各种过敏反应的组胺H1拮抗剂。

10. 发明授权

US4728734A C-3'thioiminosulfonyl cephalosporin analogs 失效
标题翻译： C-3'硫代亚氨基磺酰头孢菌素类似物
公开(公告)号：US4728734A
公开(公告)日：1988-03-01
申请号：US801645
申请日：1985-11-25
申请人： Jerauld S. Skotnicki , Donald P. Strike
发明人： Jerauld S. Skotnicki , Donald P. Strike
IPC分类号： C07D501/24 , C07D501/46 , C07D519/00 , C07D501/36 , A61K31/545
CPC分类号： C07D501/46 , C07D501/24 , C07D519/00
摘要： There are disclosed novel antibacterial compounds having the formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo lower alkyl, aryl of 6-12 carbon atoms, all the said foregoing groups being optionally substituted with carboxy, lower alkoxycarbonyl, phenoxycarbonyl, amino, mono- or di-lower alkyl substituted amino, hydroxy, lower alkoxy, phenoxy, carbamoyl, lower alkyl carbonyl, benzoyl, cyano, nitro, formamido, lower alkanoylamino or benzamido;R.sup.1 is hydrogen, lower alkyl or an alkali metal cation;A is ##STR2## R.sup.2 and R.sup.3 are each individually lower alkyl, carboxy, lower alkoxycarbonyl, phenoxycarbonyl, amino, mono- or di-lower alkyl substituted amino, hy, lower alkoxy, phenoxy, carbamoyl, mono- or di-lower alkyl substituted cabamoyl, lower alkylcarbonyl, benzoyl, cyano, nitro, lower alkanoylamino or benzamido;m=0-1;n=0-1;B represents ##STR3## or a 5- or 6- membered unsaturated aza-, diaza-, triaza-, tetraza-, thia-, thiaza-, oxathia-, oxathiaza-, oxa-, dioxa-, oxaza- or, oxadiazacyclic moiety; and the dotted line denotes an optional double bond.
摘要翻译：公开了具有式“IMAGE”的新型抗菌化合物，其中R是氢，低级烷基，低级烯基，低级炔基，环低级烷基，6-12个碳原子的芳基，所有上述基团任选被羧基取代，低级烷氧基羰基，苯氧基羰基，氨基，一或二低级烷基取代的氨基，羟基，低级烷氧基，苯氧基，氨基甲酰基，低级烷基羰基，苯甲酰基，氰基，硝基，甲酰氨基，低级烷酰氨基或苯甲酰氨基。 R1是氢，低级烷基或碱金属阳离子; A是R 2和R 3各自独立地为低级烷基，羧基，低级烷氧基羰基，苯氧基羰基，氨基，一或二低级烷基取代的氨基，高级，低级烷氧基，苯氧基，氨基甲酰基，一或二 - 低级烷基取代氨基甲酰基，低级烷基羰基，苯甲酰基，氰基，硝基，低级烷酰氨基或苯甲酰氨基; m = 0-1; n = 0-1; B表示5或6-元不饱和氮杂 - ，二氮杂 - ，三氮杂 - ，四嗪 - ，硫杂 - ，硫杂 - 氧基硫杂 - 氧基硫杂 - 氧杂 - 二氧杂 - 恶唑并或恶二唑环 ; 虚线表示任选的双键。

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