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11. 发明授权

US09265734B2 Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors 有权
标题翻译：组合物包括作为HDAC抑制剂的6-氨基己酸衍生物
公开(公告)号：US09265734B2
公开(公告)日：2016-02-23
申请号：US13062030
申请日：2009-09-03
申请人： James R. Rusche , Norton P. Peet , Allen T. Hopper
发明人： James R. Rusche , Norton P. Peet , Allen T. Hopper
IPC分类号： C07C237/04 , A61K31/166 , A61K31/00 , A61K31/16 , C07C235/16 , C07C237/22 , C07C255/57 , C07C311/16 , C07C311/19 , C07C317/44 , C07C323/62 , C07D209/48 , C07D213/30 , C07D231/56 , C07D277/56 , C07D295/14 , C07D307/84 , C07D409/12
CPC分类号： C07C233/80 , A61K31/00 , A61K31/16 , C07C235/16 , C07C237/22 , C07C255/57 , C07C311/16 , C07C311/19 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07D209/48 , C07D213/30 , C07D213/81 , C07D217/24 , C07D231/12 , C07D231/56 , C07D237/24 , C07D241/24 , C07D241/44 , C07D271/12 , C07D277/56 , C07D295/14 , C07D295/15 , C07D307/84 , C07D307/85 , C07D333/38 , C07D409/12 , Y02A50/411
摘要： This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.
摘要翻译：本发明涉及式（I）化合物，其中Cy1，L1，Y，R1，L2和Ar2在本文中定义，用于治疗癌症，炎性疾病和神经病症。

12. 发明申请

US20100009992A1 AMPK MODULATORS 有权
标题翻译： AMPK调制器
公开(公告)号：US20100009992A1
公开(公告)日：2010-01-14
申请号：US12365671
申请日：2009-02-04
申请人： Neal C. Birnberg , Hong Liu , Qing Ping Weng , Haibo Shang , Pan Yin , Sharanappa B. Rajur , Hwa-Ok Kim , Paresh D. Salgaonkar , Norton P. Peet
发明人： Neal C. Birnberg , Hong Liu , Qing Ping Weng , Haibo Shang , Pan Yin , Sharanappa B. Rajur , Hwa-Ok Kim , Paresh D. Salgaonkar , Norton P. Peet
IPC分类号： A61K31/437 , A61K31/4985 , A61K31/4375 , A61K31/47 , A61K31/404 , C07D498/04 , C07D471/04 , C07D215/20 , C07D209/12 , A61P35/00 , A61P3/10 , A61P3/04
CPC分类号： C07D498/04 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/42 , C07D215/54 , C07D215/56 , C07D401/04 , C07D403/04 , C07D471/04
摘要： The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.
摘要翻译：本发明涉及式（I）或（II）的化合物和药学上可接受的盐，酯和前药：其可用作对受试者中有效治疗糖尿病，肥胖和癌症的AMPK调节剂。

13. 发明授权

US06693072B2 Elastase inhibitors 失效
标题翻译：弹性蛋白酶抑制剂
公开(公告)号：US06693072B2
公开(公告)日：2004-02-17
申请号：US09741536
申请日：2000-12-20
申请人： Steven L. Gallion , William A. Metz Jr. , Joseph P. Burkhart , Michael R. Angelastro , Norton P. Peet
发明人： Steven L. Gallion , William A. Metz Jr. , Joseph P. Burkhart , Michael R. Angelastro , Norton P. Peet
IPC分类号： A61K3800
CPC分类号： C07K5/06191 , A61K38/00
摘要： This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase. The inhibitors are short, synthetic peptides in which the P2 moiety is substituted with various nitrogen-containing heterocyclic groups. As inhibitors of human neutrophil elastase, the compounds are useful in the treatment of a patient afflicted with a neutrophil associated inflammatory disease.
摘要翻译：本发明涉及作为弹性蛋白酶抑制剂，特别是人嗜中性粒细胞弹性蛋白酶的化合物。抑制剂是其中P2部分被各种含氮杂环基团取代的短合成肽。作为人嗜中性粒细胞弹性蛋白酶抑制剂，该化合物可用于治疗患有嗜中性粒细胞相关性炎性疾病的患者。

14. 发明授权

US06642231B2 6,9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines 失效
标题翻译： 6,9-二取代的2- [反 - （4-氨基环己基）氨基]嘌呤
公开(公告)号：US06642231B2
公开(公告)日：2003-11-04
申请号：US10178494
申请日：2002-06-24
申请人： Jennifer A. Dumont , Alan J. Bitonti , David R. Borcherding , Norton P. Peet , H. Randall Munson, Jr. , Patrick W. Shum
发明人： Jennifer A. Dumont , Alan J. Bitonti , David R. Borcherding , Norton P. Peet , H. Randall Munson, Jr. , Patrick W. Shum
IPC分类号： C07D47316
CPC分类号： C07D473/00
摘要： The present invention comprises 6-9-Disubstituted 2-[trans-(4-aminocyclohexyl]aminopurines that are useful in inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.
摘要翻译：本发明包括可用于抑制细胞周期蛋白依赖性激酶，特别是cdk-2的6-9-二取代的2- [反 - （4-氨基环己基）氨基嘌呤，本发明还提供了一种预防神经元细胞凋亡的方法和方法抑制肿瘤的发展。

15. 发明授权

US06413951B2 20-fluoro-17(20)-vinyl steroids 失效
标题翻译： 20-氟-17（20） - 乙烯基类固醇
公开(公告)号：US06413951B2
公开(公告)日：2002-07-02
申请号：US09886818
申请日：2001-06-21
申请人： Norton P. Peet , Philip M. Weintraub , Joseph P. Burkhart , Cynthia A. Gates
发明人： Norton P. Peet , Philip M. Weintraub , Joseph P. Burkhart , Cynthia A. Gates
IPC分类号： A61K3156
CPC分类号： C07J13/007
摘要： The invention relates to 20&xgr;-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20&xgr;-fluoro-3&bgr;-hydroxypregna-5,17(20)-dien-21-oic acid ethyl ester, 20&xgr;-fluoro-21-hydroxypregna-4,17 (20)-dien-3-one, 20&xgr;-fluoropregna-5,17(20)-dien-3&bgr;,21-diol and related compounds and to compositions incorporating these compounds, as well as the inhibition of C17,20 lyase, 5&agr;-reductase and C17-hydroxylase, and to the use of these compounds in the treatment of androgen and estrogen mediated or dependent disorders, including benign prostatic hyperplasia, prostate cancer, breast cancer and DHT-mediated disorders such as acne and hirsutism. Treatment of disorders related to the over synthesis of cortisol, for example, Cushing's Syndrome are also included. The treatment of androgen-dependent disorders also includes a combination therapy with known androgen-receptor antagonists, such as flutamide. The compounds of the invention have the following general formulae:
摘要翻译：本发明涉及20和xgr-氟孕烷-4,17（20） - 二烯-21-蓖麻油酸乙酯，20＆xgr-氟-3β-羟基孕烯-5,17（20） - 二烯-21-酸（20） - 二烯-3-酮，20和xgr-氟孕烷-5,17（20） - 二烯-3β，21-二醇及相关化合物，并与掺入这些化合物的组合物以及C17,20裂解酶，5α-还原酶和C17-羟化酶的抑制，以及这些化合物在治疗雄激素和雌激素介导或依赖性疾病（包括良性前列腺增生症，前列腺癌）中的用途，乳腺癌和DHT介导的疾病如痤疮和多毛症。还包括治疗与过度合成皮质醇有关的疾病，例如库欣综合征。雄激素依赖性疾病的治疗还包括与已知的雄激素受体拮抗剂如氟他胺的联合治疗。本发明化合物具有以下通式：

16. 发明授权

US06313161B1 2,19-methyleneoxy and 2,19-methylenethio bridged steroids as aromatase, 19-hydroxylase inhibitors and methods of their use in the treatment of estrogen mediated disorders 失效
标题翻译： 2,19-亚甲基氧基和2,19-亚甲硫基桥连类固醇作为芳香酶，19-羟化酶抑制剂及其用于治疗雌激素介导的病症的方法
公开(公告)号：US06313161B1
公开(公告)日：2001-11-06
申请号：US09426993
申请日：1999-10-26
申请人： Norton P. Peet , J. O'Neal Johnston , Joseph P. Burkhart
发明人： Norton P. Peet , J. O'Neal Johnston , Joseph P. Burkhart
IPC分类号： A61K31352
CPC分类号： C07J71/0078 , C07J71/0005
摘要： The present invention is directed to a method of using a certain compounds which are 2,19-methyleneoxy or 2,19 methylenethio bridged steroids, and related steroidal compounds as inhibitors of the enzyme steroid aromatase, 19-hydroxylase and as treatment for various estrogen dependent/mediated disorders including hormonal dependent breast cancer.
摘要翻译：本发明涉及一种使用2,19-亚甲氧基或2,19个亚甲硫基桥连类固醇的某些化合物和相关甾体化合物作为类固醇芳香酶，19-羟化酶酶抑制剂和各种雌激素依赖性的治疗方法 /介导的疾病，包括激素依赖性乳腺癌。

17. 发明授权

US06265381B1 Orally-active elastase inhibitors 失效
标题翻译：口服活性弹性蛋白酶抑制剂
公开(公告)号：US06265381B1
公开(公告)日：2001-07-24
申请号：US09491814
申请日：2000-01-28
申请人： Norton P. Peet , Michael R. Angelastro , Joseph P. Burkhart
发明人： Norton P. Peet , Michael R. Angelastro , Joseph P. Burkhart
IPC分类号： A61K3800
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827
摘要： This invention relates to novel morpholinourea and related derivatives of pentafluoroethyl peptides which are orally active elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases and emphysema.
摘要翻译：本发明涉及作为口服活性弹性蛋白酶抑制剂的五氟乙基肽的新型吗啉代脲和相关衍生物。这些化合物可用于治疗各种炎性疾病和肺气肿。

18. 发明授权

US5698523A Acylated enol derivatives as prodrugs of elastase inhibitors 失效
标题翻译：作为弹性蛋白酶抑制剂前药的酰化烯醇衍生物
公开(公告)号：US5698523A
公开(公告)日：1997-12-16
申请号：US670136
申请日：1996-06-25
申请人： Norton P. Peet , Joseph P. Burkhart , Shujaath Mehdi
发明人： Norton P. Peet , Joseph P. Burkhart , Shujaath Mehdi
IPC分类号： C07D295/18 , A61K31/27 , A61K31/535 , A61K31/5375 , A61K31/64 , A61K38/00 , A61K38/55 , A61P1/00 , A61P11/00 , A61P29/00 , A61P43/00 , C07C271/22 , C07K5/06 , C07K5/08 , C07K5/10 , C07K14/81 , C07D43/12 , A61K38/06 , C07K5/083
CPC分类号： C07K5/0827 , C07C271/22 , C07K5/06191 , A61K38/00 , Y02P20/582
摘要： This invention relates to acylated enol derivatives of known elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema or as prodrugs of compounds which are useful in the treatment of said diseases.
摘要翻译：本发明涉及已知的弹性蛋白酶抑制剂的酰化烯醇衍生物。这些化合物可用于治疗各种炎性疾病，包括囊性纤维化和肺气肿，或可用于治疗所述疾病的化合物的前药。

19. 发明授权

US5691368A Substituted oxazolidine calpain and/or cathepsin B inhibitors 失效
标题翻译：取代的恶唑烷钙蛋白酶和/或组织蛋白酶B抑制剂
公开(公告)号：US5691368A
公开(公告)日：1997-11-25
申请号：US552139
申请日：1995-12-11
申请人： Norton P. Peet , Shujaath Mehdi , Matthew D. Linnik , Michael R. Angelastro , Hwa-Ok Kim
发明人： Norton P. Peet , Shujaath Mehdi , Matthew D. Linnik , Michael R. Angelastro , Hwa-Ok Kim
IPC分类号： C07D263/06 , A61K31/42 , A61K31/421 , A61K31/535 , A61K31/5377 , A61K38/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/28 , A61P43/00 , C07D263/04 , C07D263/18 , C07K5/062
CPC分类号： C07D263/04
摘要： This invention relates to oxazolidine inhibitors of calpain and/or cathepsin B and to compositions containing them. As inhibitors of calpain and/or cathepsin B, the compounds are useful in the treatment of patients afflicted with acute or chronic neurodegenerative disorders.
摘要翻译：本发明涉及钙蛋白酶和/或组织蛋白酶B的恶唑烷抑制剂以及含有它们的组合物。作为钙蛋白酶和/或组织蛋白酶B的抑制剂，该化合物可用于治疗患有急性或慢性神经变性疾病的患者。

20. 发明授权

US5661167A Prolyl endopeptidase inhibitors 失效
标题翻译：脯氨酰内肽酶抑制剂
公开(公告)号：US5661167A
公开(公告)日：1997-08-26
申请号：US759323
申请日：1996-12-02
申请人： Norton P. Peet , Shujaath Mehdi , Joseph P. Burkhart
发明人： Norton P. Peet , Shujaath Mehdi , Joseph P. Burkhart
IPC分类号： C07D277/04 , A61K31/40 , A61K31/401 , A61K31/425 , A61K31/426 , A61P25/28 , A61P43/00 , C07D207/16 , C07D277/06 , C07D403/06 , C07D417/06 , C07D417/14
CPC分类号： C07D207/16 , C07D277/06
摘要： The present invention relates to compounds of formula 1, ##STR1## including all of its stereoisomers, compositions, and processes for preparation of the same. The compounds of the present invention are also useful in their pharmacological activities as they directly act as inhibitors of prolyl endopeptidase and thereby provide a methods for memory enhancement, preventing or slowing the affects of amnesia or memory deficits.
摘要翻译：本发明涉及式1化合物，其包含其所有的立体异构体，组合物及其制备方法。本发明的化合物也可用于其药理活性，因为它们直接作为脯氨酰内肽酶的抑制剂，从而提供记忆增强，预防或减缓健忘症或记忆缺陷的影响的方法。

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