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1. 发明授权

US5750550A 2-(pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3 (2H)-One 1, 1-dioxides and compositions and method of use thereof 失效
标题翻译： 2-（吡唑-5-基 - 氧甲基）-1,2-苯并异噻唑-3（2H） - 1,1-二氧化物及其组合物及其使用方法
公开(公告)号：US5750550A
公开(公告)日：1998-05-12
申请号：US529121
申请日：1995-09-15
申请人： Michael A. Eissenstat , Gee-Hong Kuo , Ranjit C. Desai , Dennis J. Hlasta , John J. Court
发明人： Michael A. Eissenstat , Gee-Hong Kuo , Ranjit C. Desai , Dennis J. Hlasta , John J. Court
IPC分类号： C07C69/38 , C07D417/12 , C07D417/14 , A61K31/425 , C07D275/04
CPC分类号： C07D417/12 , C07C69/38 , C07D417/14
摘要： 2-(Pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
摘要翻译： 2-（吡唑-5-基 - 氧甲基）-1,2-苯并异噻唑-3（2H） - 酮1,1-二氧化物，含有它们的药物组合物和利用它们治疗退行性疾病的方法。

2. 发明授权

US07132420B2 Aspartic protease inhibitors 有权
标题翻译：天冬氨酸蛋白酶抑制剂
公开(公告)号：US07132420B2
公开(公告)日：2006-11-07
申请号：US10458873
申请日：2003-06-11
申请人： Ramnarayan S. Randad , John W. Erickson , Michael A. Eissenstat , Lucyna Lubkowska
发明人： Ramnarayan S. Randad , John W. Erickson , Michael A. Eissenstat , Lucyna Lubkowska
IPC分类号： A61K31/5375 , A61K31/505 , C07D413/12 , C07D239/04
CPC分类号： C07D207/27 , C07C235/20 , C07C235/50 , C07C237/34 , C07C271/20 , C07C271/22 , C07C311/29 , C07D211/60 , C07D213/30 , C07D215/48 , C07D239/10 , C07D277/24 , C07D295/215 , C07D307/20 , C07D405/12 , C07D417/12
摘要： The present invention provides an aspartic proteinase-inhibiting compound of the formula: wherein a, b, c, d, and e, can be the same or different and each are R7, OR7, SR7, NR7R8, NHCOR7, CO2R7, CN, NO2, NH2, N3, or a halogen, wherein R7 and R8 are independently H or an alkyl. Substituents R1 or R2 are each H or an alkyl. Substituent R3 is a straight chain or branched alkyl, alkenyl, or alkynyl substituent, or is a cycloalkyl. Substituent A is OH, NH2, or SH. Further provided are pharmaceutical compositions, which include a therapeutically effective amount of at least one of the foregoing compounds, and therapeutic methods of using the foregoing compounds.
摘要翻译：本发明提供了下式的天冬氨酸蛋白酶抑制化合物：其中a，b，c，d和e可以相同或不同，分别为R 7，或7 7，7号，7号，8号，7号，7号，7号， CN，NO 2，NH 2，N 3，或卤素，其中R 1，R 2， R 7和R 8独立地是H或烷基。取代基R 1或R 2各自为H或烷基。取代基R 3是直链或支链烷基，烯基或炔基取代基，或是环烷基。取代基A是OH，NH 2或SH。还提供药物组合物，其包括治疗有效量的至少一种前述化合物，以及使用前述化合物的治疗方法。

3. 发明授权

US06613764B1 Aspartic protease inhibitors 有权
标题翻译：天冬氨酸蛋白酶抑制剂
公开(公告)号：US06613764B1
公开(公告)日：2003-09-02
申请号：US09868775
申请日：2001-09-28
申请人： Ramnarayan S. Randad , John W. Erickson , Michael A. Eissenstat , Lucyna Lubkowska
发明人： Ramnarayan S. Randad , John W. Erickson , Michael A. Eissenstat , Lucyna Lubkowska
IPC分类号： A61K315377
CPC分类号： C07D207/27 , C07C235/20 , C07C235/50 , C07C237/34 , C07C271/20 , C07C271/22 , C07C311/29 , C07D211/60 , C07D213/30 , C07D215/48 , C07D239/10 , C07D277/24 , C07D295/215 , C07D307/20 , C07D405/12 , C07D417/12
摘要： The present invention provides a compound of formula (I) wherein a, b, c, d, and e, are R7, OR7, SR7, NR7R8, NHCOR7, CO2R7, CN, NO2, NH2, N3, or a halogen. R7 and R8 are H or alkyl, R1 and R2 are H or alkyl, and R3 is a non-aromatic substituent. Substituent A is OH, NH2, or SH. Substituents B and B1 include amide and sulfonamide groups, which can be cyclic, acyclic, or amino acid derivatives. Alternatively, B and R′ together with the nitrogen to which they are bonded, and/or B′ and R2 together with the nitrogen to which they are bonded, define a heterocycle. The present invention further provides a pharmaceutical composition that includes a carrier and a therapeutically effective amount of at least one compound of the present invention. The present invention further provides therapeutic methods that include administering a therapeutically effective amount of at least one compound of the present invention
摘要翻译：本发明提供式（I）化合物，其中a，b，c，d和e分别是R 7，OR 7，SR 7，NR 7 R 8，NHCOR 7，CO 2 R 7，CN，NO 2，NH 2，N 3或卤素。 R 7和R 8是H或烷基，R 1和R 2是H或烷基，R 3是非芳族取代基。取代基A是OH，NH 2或SH。取代基B和B1包括酰胺和磺酰胺基团，其可以是环状，非环状或氨基酸衍生物。或者，B和R'与它们所键合的氮一起，和/或B'和R 2与它们所键合的氮一起定义杂环。本发明还提供了包含载体和治疗有效量的至少一种本发明化合物的药物组合物。本发明进一步提供治疗方法，其包括施用治疗有效量的至少一种本发明化合物

4. 发明授权

US5356903A 1-cyclopropyl-4-pyridyl-quinolines 失效
标题翻译： 1-环丙基-4-吡啶基 - 喹啉
公开(公告)号：US5356903A
公开(公告)日：1994-10-18
申请号：US52027
申请日：1993-04-22
申请人： Michael A. Eissenstat , Gee-Hong Kuo
发明人： Michael A. Eissenstat , Gee-Hong Kuo
IPC分类号： C07D401/04 , A61K31/47
CPC分类号： C07D401/04
摘要： Compounds of formula ##STR1## wherein; R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 X where X is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;R.sub.3 and R.sub.4 are each individually hydrogen or fluoro;Z is NR.sub.5 or CR.sub.6 R.sub.7 ;R.sub.5 is hydrogen, aryl, arylthio, arylsulfonyl, lower-alkyl, cycloalkyl, heterocycloalkyl, amino-lower-alkyl, lower-alkylamino-lower-alkyl, dilower-alkylamino-lower-alkyl, lower-alkoxy, hydroxy or NR.sub.8 R.sub.9 ;R.sub.6 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro or lower-alkylsulfonyl;R.sub.7 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro, aryl, or lower-alkylsulfonyl;R.sub.8 is hydrogen, lower-alkyl, aryl, heterocycloalkyl, carbamyl, alkanoyl, aroyl, hydroxy-lower-alkyl; andR.sub.9 is hydrogen, lower-alkyl or lower-alkanoyl or pharmaceutically acceptable acid addition salts thereof are useful as anticancer agents.
摘要翻译：式的化合物其中; R1是氢，低级烷基或三氟甲基; R2是低级烷基，三氟甲基或CH2X，其中X是羟基，氯代，低级烷基氨基或二氧代 - 烷基氨基; R3和R4各自为氢或氟; Z为NR5或CR6R7; R5是氢，芳基，芳硫基，芳基磺酰基，低级烷基，环烷基，杂环烷基，氨基 - 低级 - 烷基，低级 - 烷基氨基 - 低级 - 烷基，二 - 低级 - 烷基氨基 - 低级 - 烷基，低级 - 烷氧基，羟基或NR8R9; R6是氢，氰基，低级烷氧基羰基，低级烷酰基，硝基或低级烷基磺酰基; R7是氢，氰基，低级烷氧基羰基，低级烷酰基，硝基，芳基或低级烷基磺酰基; R8是氢，低级烷基，芳基，杂环烷基，氨基甲酰基，烷酰基，芳酰基，羟基 - 低级烷基; 并且R 9为氢，低级烷基或低级烷酰基或其药学上可接受的酸加成盐可用作抗癌剂。

5. 发明授权

US5068234A 3-arylcarbonyl-1-(C-attached-N-heteryl)-1H-indoles 失效
标题翻译： 3-亚乙基-1-（C-ATTACHED-N-HETERYL）-1H-吲哚
公开(公告)号：US5068234A
公开(公告)日：1991-11-26
申请号：US484759
申请日：1990-02-26
申请人： Thomas E. D'Ambra , Edward R. Bacon , Malcolm R. Bell , Philip M. Carabateas , Michael A. Eissenstat , Virendra Kumar , John P. Mallamo , Susan J. Ward
发明人： Thomas E. D'Ambra , Edward R. Bacon , Malcolm R. Bell , Philip M. Carabateas , Michael A. Eissenstat , Virendra Kumar , John P. Mallamo , Susan J. Ward
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/545 , A61K31/55 , A61P25/04 , A61P29/00 , C07D209/12 , C07D401/02 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
CPC分类号： C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
摘要： 2-R.sub.2 -R.sub.4 -substituted-3-R.sub.3 -CO-1-[(C-attached-N-herteryl)-(Alk).sub.n ]-1H-indoles useful as analgesic, anti-rheumatic, anti-inflammatory or anti-glaucoma agents.

6. 发明授权

US5330992A 1-cyclopropyl-4-pyridyl-quinolinones 失效
标题翻译： 1-环丙基-4-吡啶基 - 喹啉酮
公开(公告)号：US5330992A
公开(公告)日：1994-07-19
申请号：US967473
申请日：1992-10-23
申请人： Michael A. Eissenstat , John D. Weaver, III , Gee-Hong Kuo , Mark P. Wentland
发明人： Michael A. Eissenstat , John D. Weaver, III , Gee-Hong Kuo , Mark P. Wentland
IPC分类号： C07D401/04 , C07D401/14 , A61K31/47 , C07D215/233
CPC分类号： C07D401/04 , C07D401/14
摘要： Compounds of formula ##STR1## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Z where Z is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;R.sub.3 and R.sub.4 are each individually hydrogen or fluoro; andAr is phenyl, an aromatic 5- or 6-membered heterocycle or any of these substituted at one or more positions with lower-alkyl, fluoro, chloro, hydroxy, amino, lower-alkylamino, dilower-alkylamino, carboxy, sulfonamido, lower alkylsulfonamido, methylenedioxy, trifluoroacetamido, lower-alkanoylamino, or carbamoyl; and their pharmaceutically acceptable acid addition salts are useful as anticancer agents.
摘要翻译：其中R 1是氢，低级烷基或三氟甲基的式IMAMA的化合物; R2是低级烷基，三氟甲基或CH2Z，其中Z是羟基，氯，低级烷基氨基或二元 - 烷基氨基; R3和R4各自为氢或氟; 并且Ar是苯基，芳族的5或6元杂环，或者它们在一个或多个位置被低级烷基，氟，氯，羟基，氨基，低级烷基氨基，二元 - 二烷基氨基，羧基，亚磺酰氨基，低级烷基亚磺酰氨基，亚甲二氧基，三氟乙酰胺基，低级烷酰氨基或氨基甲酰基; 其药学上可接受的酸加成盐可用作抗癌剂。

7. 发明授权

US5324737A 3-arylcarbonyl-1-(C-attached-N-heteryl)-1H-indoles 失效
标题翻译： 3-芳基羰基-1-（C-连接的N-异基）-1H-吲哚
公开(公告)号：US5324737A
公开(公告)日：1994-06-28
申请号：US807032
申请日：1991-09-26
申请人： Thomas E. D'Ambra , Edward R. Bacon , Malcolm R. Bell , Philip M. Carabateas , Michael A. Eissenstat , Virendra Kumar , John P. Mallamo , Susan J. Ward
发明人： Thomas E. D'Ambra , Edward R. Bacon , Malcolm R. Bell , Philip M. Carabateas , Michael A. Eissenstat , Virendra Kumar , John P. Mallamo , Susan J. Ward
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/545 , A61K31/55 , A61P25/04 , A61P29/00 , C07D209/12 , C07D401/02 , C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06 , C07D40/06
CPC分类号： C07D401/06 , C07D403/06 , C07D413/06 , C07D417/06
摘要： 2-R.sub.2 -R.sub.4 -substitutea-3-R.sub.3 -CO-1-[(C-attached-N-heteryl)(Alk).sub.n ]-1H-indoles useful as analgesic, anti-rheumatic, anti-inflammatory or anti-glaucoma agents.
摘要翻译：可用作镇痛，抗风湿，消炎或抗青光眼的2-R2-R4-替代-3-R3-CO-1 - [（C-连接的N-异基）（Alk）n] 代理商

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