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1. 发明授权

US06576630B1 Compounds and compositions as protease inhibitors 失效
标题翻译：化合物和组成作为蛋白酶抑制剂
公开(公告)号：US06576630B1
公开(公告)日：2003-06-10
申请号：US09525507
申请日：2000-03-15
申请人： John O. Link , Arnold J. Martelli , Valeri Martichonok , John W. Patterson , Oliver L. Saunders , Sheila Zipfel
发明人： John O. Link , Arnold J. Martelli , Valeri Martichonok , John W. Patterson , Oliver L. Saunders , Sheila Zipfel
IPC分类号： C07D26356
CPC分类号： C07D213/30 , A61K31/42 , A61K31/44 , A61K45/06 , C07D209/08 , C07D263/14 , C07D263/26 , C07D263/32 , C07D263/34 , C07D263/56 , C07D263/60 , C07D307/80 , C07D413/04 , C07D413/12 , C07D413/14 , C07F7/1804 , A61K2300/00
摘要： The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.
摘要翻译：本发明涉及新型烷酰基取代的杂环衍生物，它们是半胱氨酸蛋白酶抑制剂; 其药学上可接受的盐和N-氧化物; 它们作为治疗剂的用途及其制备方法。

2. 发明授权

US06492362B1 Compounds and compositions as cathepsin S inhibitors 失效
标题翻译：化合物和组合物作为组织蛋白酶S抑制剂
公开(公告)号：US06492362B1
公开(公告)日：2002-12-10
申请号：US09663449
申请日：2000-09-15
申请人： Michael Graupe , John O. Link , John W. Patterson , Sheila Zipfel
发明人： Michael Graupe , John O. Link , John W. Patterson , Sheila Zipfel
IPC分类号： A61K315375
CPC分类号： C07D213/81 , C07C317/48 , C07C317/50 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07D209/08 , C07D211/66 , C07D213/82 , C07D213/89 , C07D215/48 , C07D215/54 , C07D241/24 , C07D295/185 , C07D295/205 , C07D309/08 , C07D317/68 , C07D333/38 , C07D333/40 , C07D333/70
摘要： The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译：本发明涉及新的选择性组织蛋白酶S抑制剂，其药学上可接受的盐和N-氧化物，它们作为治疗剂的用途及其制备方法。

3. 发明授权

US07064123B1 Compounds and compositions as cathepsin inhibitors 失效
标题翻译：化合物和组合物作为组织蛋白酶抑制剂
公开(公告)号：US07064123B1
公开(公告)日：2006-06-20
申请号：US10035783
申请日：2001-12-24
申请人： Michael Graupe , John W. Patterson , Stephen D. Pickett , John O. Link , Jiayao Li , David Aldous , Sukanthini Thurairatnam , Andreas P. Timm , Frank Halley , Justine Lai Yeun Quai
发明人： Michael Graupe , John W. Patterson , Stephen D. Pickett , John O. Link , Jiayao Li , David Aldous , Sukanthini Thurairatnam , Andreas P. Timm , Frank Halley , Justine Lai Yeun Quai
IPC分类号： A61K31/535 , C07D295/00 , A61P29/00
CPC分类号： C07D207/273 , A61K31/5375 , A61K31/5377 , C07C317/44 , C07C323/60 , C07D205/08 , C07D207/24 , C07D213/40 , C07D223/10 , C07D223/12 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/26 , C07D277/64 , C07D285/08 , C07D295/185 , C07D413/04 , C07D413/12 , Y02A50/411
摘要： The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译：本发明涉及新的选择性组织蛋白酶S抑制剂，其药学上可接受的盐和N-氧化物，它们作为治疗剂的用途及其制备方法。

4. 发明授权

US5633279A 5-substituted derivatives of mycophenolic acid 失效
标题翻译： 5-取代的霉酚酸衍生物
公开(公告)号：US5633279A
公开(公告)日：1997-05-27
申请号：US483042
申请日：1995-06-06
申请人： David Morgans, Jr. , David B. Smith , Francisco X. Talam as , Dean R. Artis , Alicia Cervantes , Todd R. Elworthy , Mario Fern andez , Fidencio Franco , Ronald C. Hawley , Teresa Lara , David G. Loughhead , Peter H. Nelson , John W. Patterson , John C. Rohloff , Eric B. Sjogren , Alejandra Trejo , Ann M. Waltos , Robert J. Weikert
发明人： David Morgans, Jr. , David B. Smith , Francisco X. Talam as , Dean R. Artis , Alicia Cervantes , Todd R. Elworthy , Mario Fern andez , Fidencio Franco , Ronald C. Hawley , Teresa Lara , David G. Loughhead , Peter H. Nelson , John W. Patterson , John C. Rohloff , Eric B. Sjogren , Alejandra Trejo , Ann M. Waltos , Robert J. Weikert
IPC分类号： A61K31/34 , A61K31/365 , A61K31/38 , A61K31/40 , A61K31/4025 , A61K31/42 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/06 , C07D307/83 , C07D307/88 , C07D405/06 , C07D405/10 , C07D407/06 , C07D407/10 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/12 , C07F9/655 , A61K31/445 , A61K31/535
CPC分类号： C07D405/06 , C07D307/88 , C07D407/06 , C07D409/06 , C07D413/06 , C07F9/65517
摘要： The disclosed hexenoic acid side-chain derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil, including immune, inflammatory, tumor, proliferative, viral or psoriatic disorders.
摘要翻译：公开的霉酚酸的己烯酸侧链衍生物是治疗药物，其有利于治疗指示霉酚酸和/或霉酚酸酯的疾病状态，包括免疫，炎性，肿瘤，增殖性，病毒性或牛皮癣性疾病。

5. 发明授权

US3975378A 20-Cyano-20,21-epoxy steroids 失效
标题翻译： 20-Cyano-20,21-环氧类固醇
公开(公告)号：US3975378A
公开(公告)日：1976-08-17
申请号：US590776
申请日：1975-06-27
申请人： John W. Patterson
发明人： John W. Patterson
IPC分类号： A61K31/575 , A61P29/00 , C07J71/00 , C07J17/00
CPC分类号： C07J71/0031 , Y10S514/887
摘要： Novel compounds useful as anti-inflammatories are represented by the formula ##SPC1##Wherein Z is a single or double bond; X and X.sup.1 are independently H, F or Cl; and X.sup.2 is OH or when X.sup.1 is Cl X.sup.2 may also be Cl. The compounds are prepared by reacting a suitable 21-hydrocarbon sulfonate steroid with an alkali cyanide.
摘要翻译：用作抗炎剂的新型化合物由式WHEREIN Z表示为单键或双键表示; X和X 1独立地为H，F或Cl; 并且X 2是OH或当X 1是Cl X 2也可以是Cl。通过使合适的21-烃磺酸盐类固醇与碱金属氰化物反应制备化合物。

6. 发明授权

US07476727B2 Conjugates of mycophenolic acid 失效
标题翻译：霉酚酸的结合物
公开(公告)号：US07476727B2
公开(公告)日：2009-01-13
申请号：US11673180
申请日：2007-02-09
申请人： Mitali Ghoshal , Gerald Sigler , Raymond A. Hui , Ronald Hawley , Eva Hoess , Erasmus J. Huber , John W. Patterson , Salvatore J. Salamone , Allan Dorn
发明人： Mitali Ghoshal , Gerald Sigler , Raymond A. Hui , Ronald Hawley , Eva Hoess , Erasmus J. Huber , John W. Patterson , Salvatore J. Salamone , Allan Dorn
IPC分类号： C07G3/00 , C07H15/20 , C07D233/00 , C07D473/00 , C07D211/72
CPC分类号： C07D405/12 , C07D307/88 , C07D473/08 , C07H15/20 , C07H15/22 , C07H15/24 , C07J17/00 , C07J19/005 , C07J41/0005 , C07J41/0055 , C07J43/003 , G01N33/53 , G01N33/535 , G01N33/5735 , G01N33/581 , G01N33/78 , G01N33/9453 , G01N2333/904
摘要： The present invention provides a method for the measurement of an analyte in biological samples whereby an uncompetitive inhibitor is coupled to a ligand and utilized in a homogeneous assay. The analyte can be a drug or drug derivative, hormone, polypeptide, or oligonucleotide.The present invention also provides novel compounds, assay reagents and packaged kits useful for performing such measurements.
摘要翻译：本发明提供了一种用于测量生物样品中分析物的方法，由此使非竞争性抑制剂与配体偶联并用于均匀测定。分析物可以是药物或药物衍生物，激素，多肽或寡核苷酸。本发明还提供了可用于进行这种测量的新型化合物，测定试剂和包装的试剂盒。

7. 发明授权

US07030116B2 Compounds and compositions as cathepsin inhibitors 失效
标题翻译：化合物和组合物作为组织蛋白酶抑制剂
公开(公告)号：US07030116B2
公开(公告)日：2006-04-18
申请号：US10183128
申请日：2002-06-26
申请人： Michael Graupe , James T. Palmer , John W. Patterson , David J. Aldous , Sukanthini Thurairatnam , Andreas P. Timm , John Link , Jiayao Li
发明人： Michael Graupe , James T. Palmer , John W. Patterson , David J. Aldous , Sukanthini Thurairatnam , Andreas P. Timm , John Link , Jiayao Li
IPC分类号： A61K31/535
CPC分类号： C07D213/40 , A61K31/4245 , A61K31/5375 , A61K31/5377 , C07C317/44 , C07C323/60 , C07D205/08 , C07D207/24 , C07D213/75 , C07D223/12 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/26 , C07D277/64 , C07D285/08 , C07D295/185 , C07D413/04 , C07D413/12
摘要： The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.
摘要翻译：本发明涉及新型组织蛋白酶S抑制剂，其药学上可接受的盐和N-氧化物，它们作为治疗剂的用途及其制备方法。

8. 发明授权

US5554612A 4-amino 6-substitutes mycophenolic acid and derivatives 失效
标题翻译： 4-氨基-6-取代霉酚酸及其衍生物
公开(公告)号：US5554612A
公开(公告)日：1996-09-10
申请号：US452243
申请日：1995-05-26
申请人： John W. Patterson , David Morgans, Jr. , Eric B. Sjogren , David B Smith , Francisco X. Talam as , Dean R. Artis , Alicia Cervantes , Todd R. Elworthy , Mario Fern andez , Fidencio Franco , Ronald C. Hawley , Teresa Lara , David G. Loughhead , Peter H. Nelson , Alejandra Trejo , Ann M. Waltos , Robert J. Weikert
发明人： John W. Patterson , David Morgans, Jr. , Eric B. Sjogren , David B Smith , Francisco X. Talam as , Dean R. Artis , Alicia Cervantes , Todd R. Elworthy , Mario Fern andez , Fidencio Franco , Ronald C. Hawley , Teresa Lara , David G. Loughhead , Peter H. Nelson , Alejandra Trejo , Ann M. Waltos , Robert J. Weikert
IPC分类号： A61K31/365 , A61K31/38 , A61K31/40 , A61K31/4025 , A61P17/00 , A61P29/00 , A61P35/00 , A61P37/06 , C07D307/88 , C07D405/06 , C07D407/06 , C07D409/06 , A61K31/535 , C07D413/12
CPC分类号： C07D307/88
摘要： The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
摘要翻译：公开的霉酚酸衍生物是治疗针对霉酚酸和/或霉酚酸酯和其它免疫抑制剂的疾病状态的治疗剂。

9. 发明授权

US5328907A 4-isoxazolecarboxamide derivatives 失效
标题翻译： 4-异恶唑甲酰胺衍生物
公开(公告)号：US5328907A
公开(公告)日：1994-07-12
申请号：US818185
申请日：1992-01-08
申请人： John W. Patterson , Bruce H. Devens
发明人： John W. Patterson , Bruce H. Devens
IPC分类号： A61K31/42 , A61P25/04 , A61P29/00 , A61P35/00 , A61P37/06 , C07D261/18 , C07D413/12 , A61K31/535
CPC分类号： C07D413/12 , C07D261/18 , C07D413/10
摘要： This invention is directed to compounds of the formula (I): ##STR1## wherein R.sup.1 is --OR.sup.4 (where R.sup.4 is hydrogen, lower alkyl, lower hydroxyalkyl, phenyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n Y where n is an integer from 1 to 4 and Y is morpholino, --SR.sup.5, --C(O)OR.sup.5, --C(O)N(R.sup.6).sub.2, --N(R.sup.6).sub.2, or --N.sup.+ (R.sup.6).sub.3 X.sup.-, in which R.sup.5 is lower alkyl, each R.sup.6 is independently selected from hydrogen or lower alkyl, and X is halogen)or --SR.sup.7 (where R.sup.7 is lower alkyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n W whereW is --N(R.sup.6).sub.2 or --N.sup.+ (R.sup.6).sub.3 X.sup.-, and n, R.sup.6 and X are as previously defined);R.sup.2 is lower alkyl, phenyl or phenyl-lower-alkyl;R.sup.3 is halo, hydroxy, lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, or --C(O)OR.sup.5 where R.sup.5 is as previously defined; andZ is a bond, 2,5-thienyl or 2,5-furanyl;or a pharmaceutically acceptable salt thereof. These compounds are useful in treating inflammation, autoimmune disease or allograft rejection in mammals.
摘要翻译：本发明涉及式（I）的化合物：其中R 1是-OR 4（其中R 4是氢，低级烷基，低级羟烷基，苯基，苯基 - 低级烷基或 - （CH 2）n Y 其中n是1至4的整数，Y是吗啉代，-SR 5，-C（O）OR 5，-C（O）N（R 6）2，-N（R 6）2或-N + ，其中R 5是低级烷基，每个R 6独立地选自氢或低级烷基，X是卤素）或-SR 7（其中R 7是低级烷基，苯基 - 低级 - 烷基或 - （CH 2）n W，其中W是-N （R6）2或-N +（R6）3X-，n，R6和X如前定义）; R2是低级烷基，苯基或苯基 - 低级 - 烷基; R 3是卤素，羟基，低级烷基，低级烷氧基，低级卤代烷基，低级卤代烷氧基或-C（O）OR 5，其中R 5如前所定义; Z为键，2,5-噻吩基或2,5-呋喃基; 或其药学上可接受的盐。这些化合物可用于治疗哺乳动物的炎症，自身免疫性疾病或同种异体移植排斥反应。

10. 发明授权

US5108999A 4-isoxazolecarboxamide derivatives 失效
标题翻译： 4-异恶唑甲酰胺衍生物
公开(公告)号：US5108999A
公开(公告)日：1992-04-28
申请号：US631181
申请日：1990-12-19
申请人： John W. Patterson , Bruce H. Devens
发明人： John W. Patterson , Bruce H. Devens
IPC分类号： C07D261/18 , C07D413/12
CPC分类号： C07D413/10 , C07D261/18
摘要： This invention is directed to compounds of the formula (I): ##STR1## wherein R.sup.1 is --OR.sup.4 (where R.sup.4 is hydrogen, lower alkyl, lower hydroxyalkyl, phenyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n Y where n is an integer from 1 to 4 and Y is morpholino, --SR.sup.5, --C(O)OR.sup.5, --C(O)N(R.sup.6).sub.2, --N(R.sup.6).sub.2, or --N.sup.+ (R.sup.6).sub.3 X.sup.-, in which R.sup.5 is lower alkyl, each R.sup.6 is independently selected from hydrogen or lower alkyl, and X is halogen) or --SR.sup.7 (where R.sup.7 is lower alkyl, phenyl-lower-alkyl, or --(CH.sub.2).sub.n W where W is --N(R.sup.6).sub.2 or --N.sup.+ (R.sup.6).sub.3 X.sup.-, and n, R.sup.6 and X are as previously defined);R.sup.2 is lower alkyl, phenyl or phenyl-lower-alkyl;R.sup.3 is halo, hydroxy, lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, or --C(O)OR.sup.5 where R.sup.5 is as previously defined; andZ is a bond, 2,5-thienyl or 2,5-furanyl; or a pharmaceutically acceptable salt thereof. These compounds are useful in treating inflammation, autoimmune disease or allograft rejection in mammals.
摘要翻译：本发明涉及式（I）的化合物：其中R 1是-OR 4（其中R 4是氢，低级烷基，低级羟烷基，苯基，苯基 - 低级烷基或 - （CH 2）n Y 其中n是1至4的整数，Y是吗啉代，-SR 5，-C（O）OR 5，-C（O）N（R 6）2，-N（R 6）2或-N + ，其中R 5是低级烷基，每个R 6独立地选自氢或低级烷基，X是卤素）或-SR 7（其中R 7是低级烷基，苯基 - 低级 - 烷基或 - （CH 2）n W，其中W是 - N（R6）2或-N +（R6）3X-，n，R6和X如前定义）; R2是低级烷基，苯基或苯基 - 低级 - 烷基; R 3是卤素，羟基，低级烷基，低级烷氧基，低级卤代烷基，低级卤代烷氧基或-C（O）OR 5，其中R 5如前所定义; Z为键，2,5-噻吩基或2,5-呋喃基; 或其药学上可接受的盐。这些化合物可用于治疗哺乳动物的炎症，自身免疫性疾病或同种异体移植排斥反应。

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