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11. 发明授权

US08361971B2 Tablet formulation of ezatiostat 失效
标题翻译：片剂制剂
公开(公告)号：US08361971B2
公开(公告)日：2013-01-29
申请号：US13246732
申请日：2011-09-27
申请人： Robert T. Lum , Stephan D. Parent , Chunsheng Qiao , Steven R. Schow
发明人： Robert T. Lum , Stephan D. Parent , Chunsheng Qiao , Steven R. Schow
IPC分类号： A61K38/05 , A61K9/20
CPC分类号： C07K5/0215 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K31/165 , A61K31/216
摘要： Disclosed herein are tablets comprising ezatiostat hydrochloride wherein the ezatiostat hydrochloride comprises from about 75 to about 82 percent by weight of the tablet.
摘要翻译：本文公开了包含盐酸西替伐他汀的片剂，其中盐酸替扎他昔坦包含片剂的约75-约82重量％。

12. 发明授权

US5834487A Inhibition of 26S and 20S proteasome by indanones 失效
标题翻译：通过茚二酮抑制26S和20S蛋白酶体
公开(公告)号：US5834487A
公开(公告)日：1998-11-10
申请号：US719042
申请日：1996-09-24
申请人： Robert T. Lum , Steven R. Schow , Alison Joly , Suresh Kerwar , Marek G. Nelson , Michael M. Wick
发明人： Robert T. Lum , Steven R. Schow , Alison Joly , Suresh Kerwar , Marek G. Nelson , Michael M. Wick
IPC分类号： A61K38/00 , A61K31/00 , A61K31/12 , A61K31/122 , A61K31/165 , A61K31/40 , A61K31/445 , A61K31/505 , A61K38/04 , A61K38/05 , A61K38/06 , A61P9/00 , A61P29/00 , A61P31/00 , A61P37/00 , C07C49/115 , C07C49/537 , C07C49/67 , C07C233/22 , C07C235/78 , C07D295/185 , C07K5/06 , C07K5/062 , A61K31/195
CPC分类号： C07D295/185 , A61K31/165 , A61K31/40 , A61K31/445 , A61K31/505 , A61K38/05 , A61K38/06 , C07C233/22 , C07C235/78 , C07C2101/04 , C07C2102/08
摘要： This invention is a method for inhibiting cell proliferation using indanones.
摘要翻译：本发明是使用茚满酮抑制细胞增殖的方法。

13. 发明申请

US20120021054A1 TABLET FORMULATION OF EZATIOSTAT 失效
标题翻译： EZATIOSTAT的片剂配方
公开(公告)号：US20120021054A1
公开(公告)日：2012-01-26
申请号：US13246732
申请日：2011-09-27
申请人： Robert T. Lum , Stephan D. Parent , Chunsheng Qiao , Steven R. Schow
发明人： Robert T. Lum , Stephan D. Parent , Chunsheng Qiao , Steven R. Schow
IPC分类号： A61K9/28 , A61K38/05
CPC分类号： C07K5/0215 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K31/165 , A61K31/216
摘要： Disclosed herein are tablets comprising ezatiostat hydrochloride wherein the ezatiostat hydrochloride comprises from about 75 to about 82 percent by weight of the tablet.
摘要翻译：本文公开了包含盐酸西替伐他汀的片剂，其中盐酸替扎他昔坦包含片剂的约75-约82重量％。

14. 发明授权

US06117887A Inhibition of 26S and 20S proteasome by indanones 失效
标题翻译：通过茚二酮抑制26S和20S蛋白酶体
公开(公告)号：US06117887A
公开(公告)日：2000-09-12
申请号：US88581
申请日：1998-06-02
申请人： Robert T. Lum , Steven R. Schow , Alison Joly , Suresh Kerwar , Marek G. Nelson , Michael M. Wick
发明人： Robert T. Lum , Steven R. Schow , Alison Joly , Suresh Kerwar , Marek G. Nelson , Michael M. Wick
IPC分类号： A61K38/00 , A61K31/00 , A61K31/12 , A61K31/122 , A61K31/165 , A61K31/40 , A61K31/445 , A61K31/505 , A61K38/04 , A61K38/05 , A61K38/06 , A61P9/00 , A61P29/00 , A61P31/00 , A61P37/00 , C07C49/115 , C07C49/537 , C07C49/67 , C07C233/22 , C07C235/78 , C07D295/185 , C07K5/06 , C07K5/062 , A61K31/95
CPC分类号： C07D295/185 , A61K31/165 , A61K31/40 , A61K31/445 , A61K31/505 , A61K38/05 , A61K38/06 , C07C233/22 , C07C235/78 , C07C2101/04 , C07C2102/08
摘要： This invention is novel indanone compositions useful for inhibiting cell proliferation disorders in mammals.
摘要翻译：本发明是用于抑制哺乳动物细胞增殖紊乱的新型二氢茚酮组合物。

15. 发明申请

US20110300215A1 TABLET FORMULATION OF EZATIOSTAT 审中-公开
标题翻译： EZATIOSTAT的片剂配方
公开(公告)号：US20110300215A1
公开(公告)日：2011-12-08
申请号：US13075116
申请日：2011-03-29
申请人： Robert T. Lum , Stephan D. Parent , Chunsheng Qiao , Steven R. Schow
发明人： Robert T. Lum , Stephan D. Parent , Chunsheng Qiao , Steven R. Schow
IPC分类号： A61K38/06 , A61K9/28
CPC分类号： C07K5/0215 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K31/165 , A61K31/216
摘要： Disclosed herein are tablets comprising ezatiostat hydrochloride wherein the ezatiostat hydrochloride comprises from about 75 to about 82 percent by weight of the tablet.
摘要翻译：本文公开了包含盐酸西替伐他汀的片剂，其中盐酸替扎他昔坦包含片剂的约75-约82重量％。

16. 发明授权

US06794390B2 Purine inhibitors of cyclin dependent kinase 2 & ikappabalpha 失效
标题翻译：嘌呤抑制剂的细胞周期蛋白依赖性激酶2＆ikappabalpha
公开(公告)号：US06794390B2
公开(公告)日：2004-09-21
申请号：US09929771
申请日：2001-08-14
申请人： Robert T. Lum , Cheri Lynn Blum , Richard Mackman , Michael M. Wick , Steven R. Schow
发明人： Robert T. Lum , Cheri Lynn Blum , Richard Mackman , Michael M. Wick , Steven R. Schow
IPC分类号： C07D47316
CPC分类号： C07D473/16 , C07D473/40
摘要： A compound having the formula: wherein: R1 is —X—R1′; in which R1′ is lower alkyl, substituted lower alkyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl, or heterocyclic, and X is —NH—; R2 is isopropyl; and R3 is —NR4R5; in which R4 is hydrogen and R5 is lower alkyl substituted with amino or R4 and R5 are both lower alkyl substituted with one, two or three groups chosen from hydroxy and amino, or an acid addition salt or cationic salt thereof. The compounds inhibit CDK-2 activity and are useful for treating disorders characterized by undesirable cell proliferation.
摘要翻译：具有下式的化合物：其中：R1是-X-R1'; 其中R 1'是低级烷基，取代的低级烷基，芳基，取代的芳基，杂芳基或取代的杂芳基或杂环，X是-NH-; R2是异丙基; 且R 3为-NR 4 R 5; 其中R4是氢，R5是被氨基取代的低级烷基，R4和R5都是被一个，两个或三个选自羟基和氨基的基团取代的低级烷基，或其酸加成盐或阳离子盐。该化合物抑制CDK-2活性，并且可用于治疗以不期望的细胞增殖为特征的疾病。

17. 发明授权

US06781000B1 Alpha-ketoamide inhibitors of 20S proteasome 失效
标题翻译： 20S蛋白酶体的α-酮酰胺抑制剂
公开(公告)号：US06781000B1
公开(公告)日：2004-08-24
申请号：US09356842
申请日：1999-07-19
申请人： Lisa Wang , Robert T. Lum , Steven R. Schow , Alison Joly , Suresh Kerwar , Michael M Wick
发明人： Lisa Wang , Robert T. Lum , Steven R. Schow , Alison Joly , Suresh Kerwar , Michael M Wick
IPC分类号： C07D20912
CPC分类号： C07K5/0202 , A61K38/00 , C07K5/0205 , C07K5/0207 , C07K5/06043 , C07K5/0808
摘要： &agr;-ketoamide compounds useful for treating disorders mediated by 20S proteasome in mammals having the following formula: wherein X2 is Ar or Ar—X3 wherein X3 is is —C═O, or —CH2CO—, and wherein Ar is phenyl, substituted phenyl, indole, substituted indoles, and any other heteroaryls; R1, and R2 are each individually selected from the side chains of the known natural &agr;-amino acids and unnatural amino acids, hydrogen, 1-10 carbon linear and branched alkyl, 1-10 carbon linear and branched substituted alkyl, aryl, substituted aryl, 1-10 carbon linear, branched substituted aryl, alkoxyaryl, 3-8 carbon cycloalkyl, heterocycle substituted heterocycle, heteroaryl and substituted heteroaryl; X1 is selected from hydroxide, monoalkylamino, dialkylamino, alkoxide, arylkoxide and wherein X4 is hydroxide, arylamino, monoalkylamino, dialkylamino, alkoxide, or arylalkoxide; and R3 is selected from the known natural &agr;-amino acids, unnatural amino acids, hydrogen, 1-10 carbon linear and branched alkyl, 1-10 carbon linear and branched substituted alkyl, aryl, substituted aryl, 1-10 carbon linear and branched substituted aryl, alkoxyaryl, 3-8 carbon cycloalkyl, heterocycle, substituted heterocycle, heteroaryl and substituted heteroaryl.
摘要翻译：用于治疗由20S蛋白酶体介导的疾病的α-酮酰胺化合物，其具有下式：其中X 2是Ar或Ar-X 3，其中X 3是-C = O或-CH 2 CO-，并且其中Ar是苯基，取代的苯基，吲哚，取代的吲哚和任何其它杂芳基; R1和R2分别选自已知天然α-氨基酸和非天然氨基酸的侧链，氢，1-10碳直链和支链烷基，1-10碳直链和支链取代的烷基，芳基，取代芳基，1-10碳直链，支链取代的芳基，烷氧基芳基，3-8碳环烷基，杂环取代的杂环，杂芳基和取代的杂芳基; X1选自氢氧化物，一烷基氨基，二烷基氨基，醇盐，芳基氧化物，其中X4为氢氧化物，芳基氨基，单烷基氨基，二烷基氨基，醇盐或芳基醇盐; R 3选自已知的天然α-氨基酸，非天然氨基酸，氢，1-10碳直链和支链烷基，1-10碳直链和支链取代的烷基，芳基，取代的芳基，1-10碳直链和支链取代的芳基，烷氧基芳基，3-8碳环烷基，杂环，取代的杂环，杂芳基和取代的杂芳基。

18. 发明授权

US6075150A .alpha.-ketoamide inhibitors of 20S proteasome 失效
标题翻译： 20S蛋白酶体的α-酮酰胺抑制剂
公开(公告)号：US6075150A
公开(公告)日：2000-06-13
申请号：US13365
申请日：1998-01-26
申请人： Lisa Wang , Robert T. Lum , Steven R. Schow , Alison Joly , Suresh Kerwar , Michael M Wick
发明人： Lisa Wang , Robert T. Lum , Steven R. Schow , Alison Joly , Suresh Kerwar , Michael M Wick
IPC分类号： A61K38/00 , A61K38/04 , A61P37/00 , C07K5/02 , C07K5/023 , C07K5/027 , C07K5/03 , C07K5/06 , C07K5/062 , C07K5/083 , C07D209/12 , A01N43/38
CPC分类号： C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06043 , C07K5/0808 , A61K38/00
摘要： .alpha.-ketoamide compounds useful for treating disorders mediated by 20S proteasome in mammals having the following formula: wherein X.sub.2 is Ar or Ar--X.sub.3 wherein X.sub.3 is --C.dbd.O, or --CH.sub.2 CO--, and wherein Ar is phenyl, substituted phenyl, indole, substituted indoles, and any other heteroaryls; R.sub.1, and R.sub.2 are each individually selected from the side chains of the known natural .alpha.-amino acids and unnatural amino acids, hydrogen, 1-10 carbon linear and branched alkyl, 1-10 carbon linear and branched substituted alkyl, aryl, substituted aryl, 1-10 carbon linear, branched substituted aryl, alkoxyaryl, 3-8 carbon cycloalkyl, heterocycle substituted heterocycle, heteroaryl and substituted heteroaryl; X.sub.1 is selected from hydroxide, monoalkylamino, dialkylamino, alkoxide, arylkoxide and ##STR1## wherein X.sub.4 is hydroxide, arylamino, monoalkylamino, dialkylamino, alkoxide, or arylalkoxide; and R.sub.3 is selected from the known natural .alpha.-amino acids, unnatural amino acids, hydrogen, 1-10 carbon linear and branched alkyl, 1-10 carbon linear and branched substituted alkyl, aryl, substituted aryl, 1-10 carbon linear and branched substituted aryl, alkoxyaryl, 3-8 carbon cycloalkyl, heterocycle, substituted heterocycle, heteroaryl and substituted heteroaryl.
摘要翻译：用于治疗由20S蛋白酶体介导的疾病的α-酮酰胺化合物，其具有下式：其中X2是Ar或Ar-X3，其中X3是-C = O或-CH2CO-，其中Ar是苯基，取代的苯基，吲哚取代的吲哚和任何其它杂芳基; R1和R2分别选自已知天然α-氨基酸和非天然氨基酸的侧链，氢，1-10碳直链和支链烷基，1-10碳直链和支链取代的烷基，芳基，取代的芳基，1-10碳直链，支链取代的芳基，烷氧基芳基，3-8碳环烷基，杂环取代的杂环，杂芳基和取代的杂芳基; X1选自氢氧化物，单烷基氨基，二烷基氨基，醇盐，芳基醇盐，其中X4是氢氧根，芳基氨基，单烷基氨基，二烷基氨基，醇盐或芳基醇盐; R 3选自已知的天然α-氨基酸，非天然氨基酸，氢，1-10碳直链和支链烷基，1-10碳直链和支链取代的烷基，芳基，取代芳基，1-10碳直链和支链取代的芳基，烷氧基芳基，3-8碳环烷基，杂环，取代的杂环，杂芳基和取代的杂芳基。

19. 发明授权

US5866702A Purine inhibitors of cyclin dependent kinase 2 失效
标题翻译：细胞周期蛋白依赖性激酶2的嘌呤抑制剂
公开(公告)号：US5866702A
公开(公告)日：1999-02-02
申请号：US692012
申请日：1996-08-02
申请人： Richard Mackman , Robert T. Lum , Steven R. Schow , Michael M. Wick
发明人： Richard Mackman , Robert T. Lum , Steven R. Schow , Michael M. Wick
IPC分类号： C07D473/00 , A61K31/52 , A61P3/10 , A61P9/00 , A61P13/12 , A61P19/06 , A61P25/00 , A61P31/10 , A61P35/00 , C07D233/00 , C07D239/00 , C07D473/04 , C07D473/16 , C07D473/18 , C07D473/20 , C07D473/22 , C07D473/24 , C07D473/30 , C07D473/32 , C07D473/34 , C07D473/36 , C07D473/38 , C07D473/40
CPC分类号： C07D473/16 , C07D473/40
摘要： A 2,6,9-trisubstituted purine composition having the following formula: ##STR1## where X is a amino, oxo, thio, of sulfone moiety, R.sub.1 is a lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, aryl, substituted aryl, heterocycle, hetaryl, substituted hetaryl, aralkyl, heteroaralkyl, heteroalkyl, alkyl alkenyl, alkyl alkynyl, alkyl cycloalkyl, or alkyl cycloheteroalkyl, each having from 1 to 20 carbon atoms; R.sub.2 is hydrogen, lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycle, hetaryl, substituted hetaryl, aralkyl, heteroaralkyl, heteroalkyl, alkyl alkenyl, alkyl alkynyl, alkyl cycloalkyl, or alkyl cycloheteroalkyl; and R.sub.3 is halogen, hydroxyl, thio, alkoxy, alkylthio, lower alkyl, --NR.sub.4 R.sub.5 or a component having the formula: ##STR2## wherein when R.sub.3 is 2-hydroxyethylamino and R.sub.2 is methyl, R.sub.1 -X is not amino, 3-methyl-2-butenylamino, benzylamino, or m-hydroxybenzyl-amino, when R.sub.3 is 2-hydroxyethylamino and R.sub.2 is isopropyl, R.sub.1 -X is not benzylamino, m-hydroxybenzylamino, or 3-methylbutylamino, when R.sub.3 is 2-hydroxyethylamino and R.sub.2 is 2-hydroxyethyl, R.sub.1 -X is not benzylamino and when R.sub.3 is selected from the group consisting of 2-propanol-2-methylamino and 2-dimethylaminoethylamino and R.sub.2 is methyl, then R.sub.1 -X is not benzylamino.
摘要翻译：具有下式的2,6,9-三取代嘌呤组合物：其中X是砜部分的氨基，氧代，硫代，R1是低级烷基，取代的低级烷基，环烷基，取代的环烷基，环杂烷基，取代的杂环烷基，芳基，取代的芳基，杂环，杂芳基，取代的杂芳基，芳烷基，杂芳烷基，杂烷基，烷基烯基，烷基炔基，烷基环烷基或烷基环杂烷基，各自具有1至20个碳原子; R 2是氢，低级烷基，取代的低级烷基，环烷基，取代的环烷基，芳基，取代的芳基，杂环，杂芳基，取代的杂芳基，芳烷基，杂芳烷基，杂烷基，烷基烯基，烷基炔基，烷基环烷基或烷基环杂烷基。 R 3为卤素，羟基，硫代，烷氧基，烷硫基，低级烷基，-NR 4 R 5或具有下式的组分：其中当R 3为2-羟基乙基氨基且R 2为甲基时，R 1 -X不为氨基， -2-丁烯基氨基，苄基氨基或间羟基苄基 - 氨基，当R 3为2-羟基乙基氨基且R 2为异丙基时，当R 3为2-羟基乙基氨基时，R 1 -X为苄基氨基，间羟基苄基氨基或3-甲基丁基氨基， 2-羟乙基，R1-X不是苄基氨基，当R3选自2-丙醇-2-甲基氨基和2-二甲基氨基乙基氨基，R2是甲基时，则R1-X不是苄基氨基。

20. 发明申请

US20120283325A1 EXCIPIENT COMPATIBILITY WITH EZATIOSTAT 审中-公开
标题翻译：与EZATIOSTAT的特殊兼容性
公开(公告)号：US20120283325A1
公开(公告)日：2012-11-08
申请号：US13449432
申请日：2012-04-18
申请人： Robert T. Lum
发明人： Robert T. Lum
IPC分类号： A61K31/216 , A61P7/00
CPC分类号： A61K31/222 , A61K9/2018
摘要： Disclosed herein is the surprising and unexpected discovery that mannitol inhibits the growth of impurities and enhances shelf life of ezatiostat hydrochloride formulations.
摘要翻译：本文公开了令人惊讶和意想不到的发现，即甘露醇抑制杂质生长并增加盐酸还原剂制剂的保质期。

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