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1. 发明授权

US07115632B1 Sulfonyl aryl or heteroaryl hydroxamic acid compounds 失效
标题翻译：磺酰基芳基或杂芳基异羟肟酸化合物
公开(公告)号：US07115632B1
公开(公告)日：2006-10-03
申请号：US09569034
申请日：2000-05-11
申请人： Louis J Bedell , Joseph J McDonald , Thomas E Barta , Daniel P Becker , Rao N Shashidhar , John N Freskos , Brent V Mischke , Daniel P Getman , Gary A DeCrescenzo , Clara I Villamil
发明人： Louis J Bedell , Joseph J McDonald , Thomas E Barta , Daniel P Becker , Rao N Shashidhar , John N Freskos , Brent V Mischke , Daniel P Getman , Gary A DeCrescenzo , Clara I Villamil
IPC分类号： A61K31/445 , C07D401/12
CPC分类号： C07C311/16 , C07C311/21 , C07C317/44 , C07D207/48 , C07D211/96 , C07D295/26
摘要： A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.
摘要翻译：公开了包括抑制基质金属蛋白酶活性的磺酰芳族或杂芳族环异羟肟酸化合物，其处理方法包括将具有MMP酶抑制有效量的考虑的磺酰芳族或杂芳族环异羟肟酸化合物施用于具有条件与病理基质金属蛋白酶活性相关。考虑的化合物在结构上对应于下式，其中W和R基团在其他地方定义。

2. 发明授权

US06583299B1 &agr;-amino-&bgr;-sulfonyl hydroxamic acid compounds 失效
标题翻译： α-氨基-β-磺酰异羟肟酸化合物
公开(公告)号：US06583299B1
公开(公告)日：2003-06-24
申请号：US09572019
申请日：2000-05-16
申请人： Susan L Hockerman , Daniel P. Becker , Louis J Bedell , Gary A DeCrescenzo , John N Freskos , Daniel P Getman , Robert M Heintz , Madeleine H Li , Brent V Mischke , Clara I Villamil , Thomas E Barta
发明人： Susan L Hockerman , Daniel P. Becker , Louis J Bedell , Gary A DeCrescenzo , John N Freskos , Daniel P Getman , Robert M Heintz , Madeleine H Li , Brent V Mischke , Clara I Villamil , Thomas E Barta
IPC分类号： C07D31500
CPC分类号： C07K5/06026 , A61K38/00 , C07C317/48 , C07C317/50 , C07C323/65 , C07D307/58
摘要： A family of molecules is disclosed that inhibit matrix metalloprotease (MMP) activity, and particularly inhibit the activity of one or more of MMP-2, MMP-9, or MMP-13, while generally exhibiting little activity against MMP-1. A contemplated compound also exhibits little inhibition of the production of TNF. A contemplated compound is an &agr;-amino-&bgr;-sulfonyl carbocyclo, heterocyclo, aryl, or heteroaryl hydroxamic acid. Also disclosed are processes for preparing a contemplated compound and for treating a mammal having a condition associated with pathological matrix metalloprotease activity.
摘要翻译：公开了分子家族抑制基质金属蛋白酶（MMP）活性，特别是抑制MMP-2，MMP-9或MMP-13中的一种或多种的活性，而通常对MMP-1几乎没有活性。预期的化合物也对TNF的产生几乎没有抑制作用。预期的化合物是α-氨基-β-磺酰基碳环，杂环基，芳基或杂芳基异羟肟酸。还公开了制备预期化合物和用于治疗具有与病理基质金属蛋白酶活性相关的病症的哺乳动物的方法。

3. 发明授权

US06750228B1 Aromatic sulfone hydroxamic acid metalloprotease inhibitor 失效
公开(公告)号：US06750228B1
公开(公告)日：2004-06-15
申请号：US09570731
申请日：2000-05-12
申请人： Thomas E Barta , Daniel P Becker , Louis J Bedell , Terri L Boehm , Jeffrey N Carroll , Gary A DeCrescenzo , Yvette M Fobian , John N Freskos , Daniel P Getman , Joseph J McDonald , Madeleine H Li , Susan L Hockerman , Susan C Howard , Steve A Kolodziej , Deborah A Mischke , Joseph G Rico , Nathan W Stehle , Michael B Tollefson , William F Vernier , Clara I Villamil
发明人： Thomas E Barta , Daniel P Becker , Louis J Bedell , Terri L Boehm , Jeffrey N Carroll , Gary A DeCrescenzo , Yvette M Fobian , John N Freskos , Daniel P Getman , Joseph J McDonald , Madeleine H Li , Susan L Hockerman , Susan C Howard , Steve A Kolodziej , Deborah A Mischke , Joseph G Rico , Nathan W Stehle , Michael B Tollefson , William F Vernier , Clara I Villamil
IPC分类号： A61K31445
CPC分类号： C07D231/12 , C07D211/66 , C07D233/56 , C07D249/08 , C07D309/08 , C07D335/02 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12
摘要： A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor. A contemplated compound corresponds in structure to formula B, below,

4. 发明授权

US06265439B1 Halogenated phenylacetonitrile alkylaminoalkylphenyl compounds as immunosuppressives 失效
标题翻译：卤代苯乙腈烷基氨基烷基苯基化合物作为免疫抑制剂
公开(公告)号：US06265439B1
公开(公告)日：2001-07-24
申请号：US09542261
申请日：2000-04-03
申请人： Richard A Mueller , Thomas E Barta , John P McKearn , Susan A Gregory , Richard A Partis , Francis J Koszyk
发明人： Richard A Mueller , Thomas E Barta , John P McKearn , Susan A Gregory , Richard A Partis , Francis J Koszyk
IPC分类号： A61K31275
CPC分类号： C07C255/42 , C07C2601/10
摘要： A class of halogenated phenylacetonitrile alkylaminoalkylphenyl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula wherein m is a number selected from three to five, inclusive; wherein n one or two; wherein R1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclhexylmethyl, benzyl and phenethyl; wherein R2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclhexylmethyl, benzyl and phenethyl; wherein each of R3 through R7 is selected from hydrido, fluoro, chloro, bromo, azide, trifluoromethyl, difluorochloromethyl, 1,1-difluoroethyl, 2,2,2-trifluoroethyl, perfluoroethyl and 2,2,3,3-tetrafluoropropyl; with the proviso that at least one of R3 through R7 is selected from fluoro and trifluoromethyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类具有免疫抑制特性的卤代苯基乙腈烷基氨基烷基苯基化合物。该类化合物可用于减少移植器官的受体排斥和治疗自身免疫性或炎性疾病。特别感兴趣的化合物是式（3）的化合物，其中m为选自三至五的数字，包括端值; 其中n个或两个; 其中R1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，叔丁基，异丁基，正戊基，异戊基，环丙基，环丁基，环戊基，环己基，环丙基甲基，环丁基甲基，环戊基甲基，环己基甲基，苄基和苯乙基; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，叔丁基，异丁基，正戊基，异戊基，环丙基，环丁基，环戊基，环己基，环丙基甲基，环丁基甲基，环戊基甲基，环己基甲基，苄基和苯乙基; 其中R3至R7各自选自氢，氟，氯，溴，叠氮化物，三氟甲基，二氟氯甲基，1,1-二氟乙基，2,2,2-三氟乙基，全氟乙基和2,2,3,3-四氟丙基; 条件是R3至R7中的至少一个选自氟和三氟甲基; 或其互变异构体或其药学上可接受的盐。

5. 发明授权

US06426360B1 4,5-substituted imidazolyl compounds for the treatment of inflammation 失效
标题翻译：用于治疗炎症的4,5-取代的咪唑基化合物
公开(公告)号：US06426360B1
公开(公告)日：2002-07-30
申请号：US09571033
申请日：2000-05-15
申请人： Richard M Weier , Paul W Collins , Michael A Stealey , Thomas E Barta , Renee M Huff
发明人： Richard M Weier , Paul W Collins , Michael A Stealey , Thomas E Barta , Renee M Huff
IPC分类号： A01N4350
CPC分类号： C07D233/64 , C07D233/84 , C07D233/88 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04
摘要： A class of compounds is described for treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula wherein R1 is selected from lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower alkenyloxyalkyl, mercapto, lower alkylcarbonyl, lower haloalkylcarbonyl, phenylcarbonyl, lower aralkylcarbonyl, lower aralkenyl, lower aryloxyalkyl, lower aralkyloxyalkyl, lower arylsulfonyl, lower aralkylsulfonyl, lower arylthioalkyl, lower heteroarylalkylthioalkyl, and heteroaryl selected from 2-thienyl, 2-furyl, 3-furyl, 2-pyridyl, 4-pyridyl and 2-benzofuryl; wherein R2 and R3 are independently selected from heteroaryl, cycloalkyl and aryl, wherein the heteroaryl, cycloalkyl and aryl radicals are substituted at a substitutable position with one or more radicals selected from hydrido, halo, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, aminosulfonyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkoxy, amino, lower alkylamino, phenylamino and nitro; and wherein R4 is selected from hydrido, lower alkyl and acyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由通式Ⅵ所定义：R1选自低级烷基，低级卤代烷基，低级羟烷基，低级烷氧基烷基，低级烯氧基烷基，巯基，低级烷基羰基，低级卤代烷基羰基，苯基羰基，低级芳烷基羰基，低级芳烯基，低级芳氧基烷基，低级芳烷氧基烷基，芳基磺酰基，低级芳烷基磺酰基，低级芳基硫代烷基，低级杂芳基烷硫基烷基和选自2-噻吩基，2-呋喃基，3-呋喃基，2-吡啶基，4-吡啶基和2-苯并呋喃基的杂芳基。其中R2和R3独立地选自杂芳基，环烷基和芳基，其中杂芳基，环烷基和芳基在可取代的位置被一个或多个选自氢，卤代，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，氨基磺酰基，低级烷基，氰基，羧基，低级烷氧基羰基，低级卤代烷基，羟基，低级烷氧基，低级羟基烷基，低级烷氧基烷基，低级卤代烷氧基，氨基，低级烷基氨基，苯基氨基和硝基。并且其中R 4选自氢，低级烷基和酰基; 或其药学上可接受的盐。

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