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1. 发明授权

US5525328A Nanoparticulate diagnostic diatrizoxy ester X-ray contrast agents for blood pool and lymphatic system imaging 失效
标题翻译：纳米颗粒诊断二硫唑酯X射线造影剂用于血液池和淋巴系统成像
公开(公告)号：US5525328A
公开(公告)日：1996-06-11
申请号：US265550
申请日：1994-06-24
申请人： Edward R. Bacon , Carl R. Illig , Irennegbe K. Osifo , Thomas S. Caulfield
发明人： Edward R. Bacon , Carl R. Illig , Irennegbe K. Osifo , Thomas S. Caulfield
IPC分类号： A61K49/04 , C07C233/54 , C07C229/60
CPC分类号： B82Y5/00 , A61K49/0485
摘要： This invention relates to methods of x-ray diagnostic imaging the blood pool and/or lymph system of a mammal comprising administering a contrast effective amount of a particulate iodinated aroyloxy ester contrast agent having the structure: ##STR1## wherein n is an integer from 3 to 20; R.sup.1 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl;R.sup.2, R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, alkoxy, aryloxy, halogen, hydroxy, acylamino, acetamidoalkyl, --COO-alkyl, --COO-aryl, --COO-aralkyl, cyano, sulfonyl, carboxamido or sulfonamido;R.sup.5 is H, alkyl, fluoroalkyl, halogen, hydroxy, acylamino, acetamidoalkyl, cyano, sulfonyl, carboxamido or sulfonamido;R.sup.6 and R.sup.7 are independently alkyl, cycloalkyl, aryl or aralkyl; andR.sup.8 and R.sup.9 are independently H or --COR.sup.6.This invention further relates to novel iodinated aroyloxy ester contrast agents having the above structure wherein n is an integer from 5 to 20, to x-ray contrast compositions comprising such agents, and to methods of x-ray diagnostic imaging utilizing such agents.
摘要翻译：本发明涉及对哺乳动物的血液池和/或淋巴系统进行x射线诊断成像的方法，该方法包括施用对比有效量的具有以下结构的颗粒状碘化芳氧基酯造影剂：具有以下结构的烷基，氟代烷基，环烷基，芳基，芳烷基，烷氧基烷基或乙酰氨基烷基; R 2，R 3和R 4独立地是H，烷基，氟烷基，烷氧基，芳氧基，卤素，羟基，酰氨基，乙酰氨基烷基，-COO-烷基，-COO-芳基，-COO-芳烷基，氰基，磺酰基，甲酰氨基或亚磺酰氨基; R5是H，烷基，氟烷基，卤素，羟基，酰氨基，乙酰胺基烷基，氰基，磺酰基，甲酰胺基或亚磺酰氨基; R6和R7独立地是烷基，环烷基，芳基或芳烷基; 并且R 8和R 9独立地为H或-COR 6。本发明还涉及具有上述结构的具有上述结构的新型碘化芳酰氧基酯造影剂，其中n为5-20的整数，以及包含这些试剂的x射线对比剂组合物，以及利用这些试剂的X射线诊断成像方法。

2. 发明授权

US06576614B1 Peptide analogs as irreversible interleukin-1&bgr; protease inhibitors 失效
标题翻译：肽类似物作为不可逆的白细胞介素-1β蛋白酶抑制剂
公开(公告)号：US06576614B1
公开(公告)日：2003-06-10
申请号：US09421954
申请日：1999-10-20
申请人： Roland E. Dolle , Irennegbe K. Osifo , Stanley J. Schmidt , Denton W. Hoyer , Tina Morgan Ross , Prasad V. Chaturvedula , Catherine P. Prouty , Mohamed M. A. Awad , Joseph M. Salvino , James M. Rinker , Eric P. Lodge , Jasbir Singh , Mark A. Ator
发明人： Roland E. Dolle , Irennegbe K. Osifo , Stanley J. Schmidt , Denton W. Hoyer , Tina Morgan Ross , Prasad V. Chaturvedula , Catherine P. Prouty , Mohamed M. A. Awad , Joseph M. Salvino , James M. Rinker , Eric P. Lodge , Jasbir Singh , Mark A. Ator
IPC分类号： C07K506
CPC分类号： C07D233/64 , C07C233/51 , C07C235/12 , C07C237/36 , C07C271/22 , C07C311/16 , C07C311/19 , C07D295/088 , C07D295/30 , C07D307/68 , C07D333/36 , C07D333/38 , C07K5/06191
摘要： Disclosed are compounds, compositions, and methods for inhibiting interleukin-1&bgr; protease activity, wherein the compounds are &agr;-substituted methyl ketones having formula (I) as set forth herein. These compounds are inhibitors of IL-1&bgr; converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.
摘要翻译：公开了用于抑制白细胞介素-1β蛋白酶活性的化合物，组合物和方法，其中所述化合物是如本文所述的具有式（I）的α-取代的甲基酮。这些化合物是IL-1β转换酶的抑制剂，因此可用作某些感染性疾病的治疗剂。

3. 发明授权

US5622967A Quinolone carboxamide Calpain inhibitors 失效
标题翻译：喹诺酮羧酰胺钙蛋白酶抑制剂
公开(公告)号：US5622967A
公开(公告)日：1997-04-22
申请号：US450961
申请日：1995-05-25
申请人： Roland E. Dolle , Todd L. Graybill , Irennegbe K. Osifo , Alex L. Harris , Matthew S. Miller , Jill S. Gregory
发明人： Roland E. Dolle , Todd L. Graybill , Irennegbe K. Osifo , Alex L. Harris , Matthew S. Miller , Jill S. Gregory
IPC分类号： C07D401/04 , C07D215/233 , A61K31/47
CPC分类号： C07D401/04
摘要： A compound of the formula ##STR1## wherein: Z is aryl, substituted aryl, phenyl-lower-alkyl, hetero-aryl, substituted heteroaryl, heterocycloalkyl, heterocyclocalkyl-lower-alkyl, hetero-aryl-lower-alkyl wherein one or more hydrogens of aryl and heteroaryl is optionally replaced by A and B;Y is lower cycloalkyl, aryl, phenyl-lower-alkyl, hetero-aryl, heterocycloalkyl, heterocyclocalkyl-lower-alkyl, hetero-aryl-lower-alkyl wherein one or more hydrogens of aryl and heteroaryl is optionally replaced by A and B;X is CONH.sub.2, CONHOH, tetrazole, SO.sub.2 N(R).sub.2, PO(OH).sub.2, CON(R).sub.2, or CONR--CHR--CO--A or CONR--(CHR).sub.n --A;A and B is independently H, OH, OR, halo, CF.sub.3, lower alkyl, N(R).sub.2, CON(R).sub.2, SR, NHSO.sub.2 R, hydroxy-lower-alkyl, NHCOR, NRSO.sub.2 CF.sub.3, OSO.sub.2 CF.sub.3, or CN;R is H, lower-alkyl, phenyl-lower-alkyl, hydroxy-lower-alkyl, CO-lower-alkyl, or CO--(CH.sub.2).sub.n --aryl; andn is 1, 2, or 3, and a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）的化合物，其中：Z是芳基，取代的芳基，苯基 - 低级 - 烷基，杂芳基，取代的杂芳基，杂环烷基，杂环烷基 - 低级 - 烷基，杂 - 芳基 - 低级烷基，其中一个或更多的芳基和杂芳基的氢任选地被A和B取代; Y是芳基和杂芳基的一个或多个氢任选地被A和B取代的低级环烷基，芳基，苯基 - 低级烷基，杂芳基，杂环烷基，杂环烷基 - 低级烷基，杂芳基 - 低级烷基， X是CONH 2，CONHOH，四唑，SO 2 N（R）2，PO（OH）2，CON（R）2或CONR-CHR-CO-A或CONR-（CHR）n-A; A和B独立地是H，OH，OR，卤素，CF 3，低级烷基，N（R）2，CON（R）2，SR，NHSO 2 R，羟基 - 低级烷基，NHCOR，NRSO 2 CF 3，OSO 2 CF 3或CN; R为H，低级烷基，苯基 - 低级 - 烷基，羟基 - 低级 - 烷基，CO-低级 - 烷基或CO-（CH2）n-芳基; 和n为1,2或3及其药学上可接受的盐。

4. 发明授权

US5521218A Nanoparticulate iodipamide derivatives for use as x-ray contrast agents 失效
标题翻译：用作x射线造影剂的纳米颗粒碘代酰胺衍生物
公开(公告)号：US5521218A
公开(公告)日：1996-05-28
申请号：US440794
申请日：1995-05-15
申请人： Irennegbe K. Osifo
发明人： Irennegbe K. Osifo
IPC分类号： A61K49/04 , C07C237/46 , C07C229/34
CPC分类号： B82Y5/00 , A61K49/049 , C07C237/46
摘要： This invention relates to methods of x-ray diagnostic imaging the blood pool, liver, spleen and/or lymph system of a mammal comprising administering a contrast effective amount of a contrast agent having the structure: ##STR1## wherein: R is alkyl having from 1 to 20 carbon atoms, aryl having from 6 to 11 carbon atoms, or R.sup.1 CO.sub.2 R.sup.2 andR.sup.1 and R.sup.2 are independently alkyl containing from 1 to 20 carbon atoms.This invention further relates to novel contrast agents having the above structure wherein both Rs are alkyl to x-ray contrast compositions comprising such agents, and to method of x-ray diagnostic imaging utilizing such agents.
摘要翻译：本发明涉及对哺乳动物的血液池，肝脏，脾脏和/或淋巴系统进行x射线诊断成像的方法，该方法包括施用对比有效量的具有以下结构的造影剂：其中：R是具有 1至20个碳原子，具有6至11个碳原子的芳基或R 1 CO 2 R 2以及R 1和R 2独立地为含有1至20个碳原子的烷基。本发明还涉及具有上述结构的新型造影剂，其中两个Rs是包含这些试剂的烷基至X射线造影剂组合物，以及使用这种试剂的X射线诊断成像方法。

5. 发明授权

US5985838A Peptide analogs as irreversible interleukin-1.beta. protease inhibitors 失效
标题翻译：肽类似物作为不可逆的白细胞介素-1β蛋白酶抑制剂
公开(公告)号：US5985838A
公开(公告)日：1999-11-16
申请号：US679350
申请日：1996-07-10
申请人： Roland E. Dolle , Irennegbe K. Osifo , Stanley J. Schmidt , Denton W. Hoyer , Tina Morgan Ross , Prasad V. Chaturvedula , Catherine P. Prouty , Mohamed M. A. Awad , Joseph M. Salvino , James M. Rinker , Eric P. Lodge , Jasbir Singh , Mark A. Ator
发明人： Roland E. Dolle , Irennegbe K. Osifo , Stanley J. Schmidt , Denton W. Hoyer , Tina Morgan Ross , Prasad V. Chaturvedula , Catherine P. Prouty , Mohamed M. A. Awad , Joseph M. Salvino , James M. Rinker , Eric P. Lodge , Jasbir Singh , Mark A. Ator
IPC分类号： A61P31/00 , C07C233/51 , C07C235/12 , C07C237/36 , C07C271/22 , C07C311/16 , C07C311/19 , C07D233/54 , C07D295/092 , C07D295/30 , C07D307/68 , C07D333/36 , C07D333/38 , C07K5/06 , A61K38/05
CPC分类号： C07D233/64 , C07C233/51 , C07C235/12 , C07C237/36 , C07C271/22 , C07C311/16 , C07C311/19 , C07D295/088 , C07D295/30 , C07D307/68 , C07D333/36 , C07D333/38 , C07K5/06191
摘要： Disclosed are compounds, compositions and methods for inhi.beta.iting interleukin-1.beta. protease activity, the compounds .alpha.-substituted methyl ketones having the formula (I) set forth herein. These compounds are inhibitors of IL-1.beta. converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.
摘要翻译：公开了化合物，组合物和方法，用于测定白细胞介素-1β蛋白酶活性，化合物具有式（I）的α-取代的甲基酮。这些化合物是IL-1β转换酶的抑制剂，因此可用作某些感染性疾病的治疗剂。

6. 发明授权

US5500204A Nanoparticulate diagnostic dimers as x-ray contrast agents for blood pool and lymphatic system imaging 失效
标题翻译：纳米颗粒诊断二聚体作为血液和淋巴系统成像的X射线造影剂
公开(公告)号：US5500204A
公开(公告)日：1996-03-19
申请号：US386788
申请日：1995-02-10
申请人： Irennegbe K. Osifo
发明人： Irennegbe K. Osifo
IPC分类号： A61K49/04
CPC分类号： B82Y5/00 , A61K49/049
摘要： This invention relates to methods of x-ray diagnostic imaging the blood pool, liver, spleen and/or lymph system of a mammal comprising administering a contrast effective amount of a succinic acid derivative disubstituted with benzoic acid residue as a contrast agent having the structure: ##STR1## R.sup.1 and R.sup.2 are alkyl of from 2 to 18 carbon atoms; A.sub.r is ##STR2## R.sup.3 is selected from the group consisting of NCH.sub.2, NHAc, and ##STR3## wherein R is an alkyl of 1 to 10 carbon atoms;R.sup.6 is H, alkyl of from 1 to 4 carbon atoms;R.sup.4 is selected from the group consisting of ##STR4## NHC--COH and CONHCH.sub.3, having 1 to 10 carbon atoms.R.sup.5 is alkyl having 1 to 18 carbon atoms and A.sub.c is acyl.This invention further relates to novel contrast agents having the above structure wherein R.sup.1 and R.sup.2 are C.sub.2 H.sub.5, to x-ray contrast compositions comprising such agents, and to method of x-ray diagnostic imaging utilizing such agents.
摘要翻译：本发明涉及对哺乳动物的血液池，肝脏，脾脏和/或淋巴系统进行x射线诊断成像的方法，该方法包括施用对比有效量的苯甲酸残基二取代的琥珀酸衍生物作为造影剂，其结构如下：结构式I R1和R2是2至18个碳原子的烷基; Ar是选自NCH 2，NHAc和的基团，其中R是1至10个碳原子的烷基; R6是H，1至4个碳原子的烷基; R 4选自 10个碳原子。 R5是具有1至18个碳原子的烷基，Ac是酰基。本发明还涉及具有上述结构的新颖造影剂，其中R1和R2是C2H5，X射线造影剂包含这些药剂，以及使用这种药剂的x射线诊断成像方法。

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