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41. 发明授权

US4469885A Halogenated protease inhibitors 失效
标题翻译：卤化蛋白酶抑制剂
公开(公告)号：US4469885A
公开(公告)日：1984-09-04
申请号：US492843
申请日：1983-05-09
申请人： Richard A. Mueller , Richard A. Partis
发明人： Richard A. Mueller , Richard A. Partis
IPC分类号： A61K31/19 , A61K31/235 , A61P43/00 , C07C45/46 , C07C49/807 , C07C51/00 , C07C63/00 , C07C63/70 , C07C63/74 , C07C65/00 , C07C65/01 , C07C65/32 , C07C67/00 , C07C69/00 , C07C69/76 , C07D263/00 , C07D263/10
CPC分类号： C07D263/10 , C07C45/46 , C07C49/807 , C07C63/70 , C07C63/74 , C07C65/01 , C07C65/32 , Y10S514/825
摘要： This invention relates to novel compounds for preventing or retarding the degradation of elastin or other proteins and therefore preventing or retarding the disease states caused by said degradation, of the formula: ##STR1## or its pharmacologically acceptable salts. The invention also relates to novel methods and intermediates for making the compounds.
摘要翻译：本发明涉及用于预防或延缓弹性蛋白或其它蛋白质降解并因此预防或延缓由所述降解引起的疾病状态的新颖化合物，其具有下式：其药理学上可接受的盐。本发明还涉及制备该化合物的新方法和中间体。

42. 发明授权

US4422317A Apparatus and process for selectively expanding a tube 失效
标题翻译：用于选择性地扩管的装置和方法
公开(公告)号：US4422317A
公开(公告)日：1983-12-27
申请号：US342338
申请日：1982-01-25
申请人： Richard A. Mueller
发明人： Richard A. Mueller
IPC分类号： B21D22/10 , B21D39/20 , B21D39/08
CPC分类号： B21D39/203 , B21D22/105 , B21D39/206
摘要： An apparatus and process for selectively expanding the wall of a tube by compression and subsequent radial expansion of one or more elastomeric bars lodged within longitudinal slots of a bushing positioned inside the tube. Expansion of the elastomeric bars against the inner surface of the tube results in expansion of the tube wall at intermittent locations about the circumference of the tube.
摘要翻译：一种用于通过压缩和随后径向膨胀管子壁的方法来选择性地膨胀管子的壁，所述一个或多个弹性体杆被放置在位于管内的衬套的纵向槽内。将弹性体棒膨胀到管的内表面上导致管壁在围绕管圆周的间歇位置膨胀。

43. 发明授权

US4336252A 1-Cycloalkyl phosphonium salts 失效
标题翻译： 1-环烷基鏻盐
公开(公告)号：US4336252A
公开(公告)日：1982-06-22
申请号：US175790
申请日：1980-08-06
申请人： Richard A. Mueller
发明人： Richard A. Mueller
IPC分类号： A01N57/34 , C07F9/54 , A01N9/36 , A61K31/66 , A61L13/00
CPC分类号： C07F9/5435 , A01N57/34
摘要： 1-Cycloalkyl phosphonium salts represented by the formula ##STR1## wherein: R is selected from the group consisting of lower alkyl, hydroxy lower alkyl, halo lower alkyl, amino lower alkyl, cyano lower alkyl, lower alkenyl with the limitation that the double bond is not on the carbon atom attached to the oxygen atom, benzyl, substituted benzyl and ##STR2## wherein q is 0 or 1 and R.sub.4 is selected from the group consisting of hydroxy, loweralkoxy, phenyl, substituted phenyl, and ##STR3## wherein R.sub.5 and R.sub.6 are the same or different members of the group consisting of hydrogen and loweralkyl or taken together form a 5 or 6 membered ring; m is 1, 2 or 3; n is 0 or 1; o is 0 or 1; p is 0 or 1; R.sub.1, R.sub.2 and R.sub.3 are the same or different members of the group consisting of hydrogen, lower alkyl, lower alkoxy and halo; and X is a pharmaceutically acceptable anion. The compounds are useful as analgesic agents.
摘要翻译：由式“IMAGE”表示的1-环烷基鏻盐，其中：R选自低级烷基，羟基低级烷基，卤代低级烷基，氨基低级烷基，氰基低级烷基，低级烯基，限制双键不在与氧原子连接的碳原子上，苄基，取代的苄基和其中q是0或1，R4选自羟基，低级烷氧基，苯基，取代的苯基和其中R5 和R6是由氢和低级烷基组成的组中相同或不同的成员或一起形成5或6元环; m为1,2或3; n为0或1; o为0或1; p为0或1; R1，R2和R3是由氢，低级烷基，低级烷氧基和卤素组成的组中相同或不同的成员; X是药学上可接受的阴离子。该化合物可用作止痛剂。

44. 发明授权

US4297487A Phosphonium salts 失效
标题翻译：鏻盐
公开(公告)号：US4297487A
公开(公告)日：1981-10-27
申请号：US175791
申请日：1980-08-06
申请人： Richard A. Mueller
发明人： Richard A. Mueller
IPC分类号： C07F9/535 , C07F9/655 , C07F9/54
CPC分类号： C07F9/5352 , C07F9/65515 , C07F9/65517
摘要： Phosphonium salts represented by the formula ##STR1## wherein: R is selected from the group consisting of lower alkyl, phenyl, substituted phenyl, benzyl and substituted benzyl; R.sub.1 is hydrogen or lower alkyl; R.sub.2 is hydrogen or loweralkyl; or R.sub.1 and R.sub.2 taken together form a 5 or 6 membered saturated or unsaturated carbocyclic ring with the limitation that R.sub.1 is on the carbon atom adjacent the carbon atom bearing R.sub.2, m is 1,2 or 3; n is 0 or 1; o is 0 or 1; p is 0 or 1; R.sub.3, R.sub.4 and R.sub.5 are the same or different members of the group consisting of hydrogen, lower alkyl, lower alkoxy and halo; R.sub.6 is hydrogen or C.sub.1 --C.sub.3 straight or branched chain alkyl; and X is a pharmaceutically acceptable anion. Compounds wherein R is phenyl, substituted phenyl, benzyl or substituted benzyl are narcotic antagonists. Compounds wherein R.sub.1 and R.sub.2 are hydrogen or lower alkyl when R is lower alkyl are mixed agonist/antagonist analgesic agents and compounds where R.sub.1 and R.sub.2 taken together form a carbocyclic ring are analgesic agents.
摘要翻译：由式表示的鏻盐，其中：R选自低级烷基，苯基，取代的苯基，苄基和取代的苄基; R1是氢或低级烷基; R2是氢或低级烷基; 或者R 1和R 2一起形成5或6元饱和或不饱和的碳环，其限制在于R1在与碳原子相邻的碳原子上具有R2，m是1,2或3; n为0或1; o为0或1; p为0或1; R3，R4和R5是由氢，低级烷基，低级烷氧基和卤素组成的组中相同或不同的成员; R6是氢或C1-C3直链或支链烷基; X是药学上可接受的阴离子。其中R是苯基，取代的苯基，苄基或取代的苄基的化合物是麻醉拮抗剂。当R为低级烷基时，其中R 1和R 2为氢或低级烷基的化合物为混合的激动剂/拮抗剂止痛剂和其中R 1和R 2一起形成碳环的化合物为止痛剂。

45. 发明授权

US07199158B2 Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors 失效
标题翻译：用作逆转录病毒蛋白酶抑制剂的琥珀酰氨基羟基氨基磺酰脲衍生物
公开(公告)号：US07199158B2
公开(公告)日：2007-04-03
申请号：US11183230
申请日：2005-07-18
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Eric T. Sun
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Eric T. Sun
IPC分类号： C07C311/00 , A61K31/18
CPC分类号： C07D213/42 , C07C307/06 , C07C2601/02 , C07C2601/14 , C07D207/16 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/088 , C07D295/13 , C07D295/185 , C07D303/36
摘要： Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7′, R8, R30–R34, X′, Y, Y′, t, x, and n are as defined herein, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译：下式的琥珀酰氨基羟基氨基磺酰脲衍生物：

46. 发明授权

US07038084B2 Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效
公开(公告)号：US07038084B2
公开(公告)日：2006-05-02
申请号：US10784916
申请日：2004-02-24
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
IPC分类号： C07C311/03 , C07C311/07 , C07C311/08 , C07D295/04 , C07D333/10
CPC分类号： C07C311/05 , C07C311/18 , C07C311/29
摘要： Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

47. 发明授权

US06951886B2 Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors 失效
标题翻译：用作逆转录病毒蛋白酶抑制剂的琥珀酰氨基羟基氨基磺酰脲衍生物
公开(公告)号：US06951886B2
公开(公告)日：2005-10-04
申请号：US10315254
申请日：2002-12-10
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Eric T. Sun
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Eric T. Sun
IPC分类号： C07C307/06 , C07D207/16 , C07D213/42 , C07D295/088 , C07D295/13 , C07D295/185 , C07D521/00 , C07C311/00 , A61K31/18
CPC分类号： C07D213/42 , C07C307/06 , C07C2601/02 , C07C2601/14 , C07D207/16 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/088 , C07D295/13 , C07D295/185 , C07D303/36
摘要： Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors and in particular as inhibitors of HIV protease.
摘要翻译：下式的琥珀酰氨基羟基氨基磺酰脲衍生物：其中取代基如说明书中所定义，作为逆转录病毒蛋白酶抑制剂，特别是作为HIV蛋白酶的抑制剂是有效的。

48. 发明授权

US06743929B1 Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效
标题翻译：用作逆转录病毒蛋白酶抑制剂的磺酰基烷酰氨基羟乙基氨基磺酰胺
公开(公告)号：US06743929B1
公开(公告)日：2004-06-01
申请号：US09655844
申请日：2000-09-06
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
IPC分类号： C07D30346
CPC分类号： A61K31/63 , A61K31/18 , C07C317/44
摘要： Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译：含磺酰胺的羟乙胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。

49. 发明授权

US06534493B1 &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效
公开(公告)号：US06534493B1
公开(公告)日：2003-03-18
申请号：US09694785
申请日：2000-10-24
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
IPC分类号： A61K3800
CPC分类号： C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/64 , C07D239/26 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D417/12 , C07K5/06026 , C07K5/06139
摘要： &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

50. 发明授权

US06472407B1 &agr; and &bgr;-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效
标题翻译：可用作逆转录病毒蛋白酶抑制剂的α和β-氨基酸羟乙基氨基磺酰胺
公开(公告)号：US06472407B1
公开(公告)日：2002-10-29
申请号：US09511005
申请日：2000-02-22
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
IPC分类号： A61K3147
CPC分类号： C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/64 , C07D239/26 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D417/12 , C07K5/06026 , C07K5/06139
摘要： &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译： α-和β-氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。

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