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41. 发明授权

US06894072B2 Compounds as NS3-serine protease inhibitors of hepatitis C virus 失效
标题翻译：化合物作为丙型肝炎病毒的NS3-丝氨酸蛋白酶抑制剂
公开(公告)号：US06894072B2
公开(公告)日：2005-05-17
申请号：US10348094
申请日：2003-01-21
申请人： Ashok Arasappan , Frank Bennett , Stephane L. Bogen , Kevin X. Chen , Edwin Jao , Yi-Tsung Liu , Raymond G. Lovey , Vincent S. Madison , Latha G. Nair , F. George Njoroge , Anil K. Saksena , Mousumi Sannigrahi , Srikanth Venkatraman , Viyyoor M. Girijavallabhan
发明人： Ashok Arasappan , Frank Bennett , Stephane L. Bogen , Kevin X. Chen , Edwin Jao , Yi-Tsung Liu , Raymond G. Lovey , Vincent S. Madison , Latha G. Nair , F. George Njoroge , Anil K. Saksena , Mousumi Sannigrahi , Srikanth Venkatraman , Viyyoor M. Girijavallabhan
IPC分类号： A61K31/403 , A61K31/7052 , A61K38/21 , A61P1/16 , A61P31/12 , A61P31/14 , A61P43/00 , C07D207/16 , C07D207/26 , C07D207/27 , C07D209/08 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/70 , C07D213/75 , C07D217/26 , C07D233/68 , C07D243/12 , C07D253/06 , C07D271/06 , C07D277/06 , C07D277/46 , C07D277/56 , C07D295/15 , C07D307/68 , C07D317/58 , C07D335/10 , C07D401/04 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D209/02
CPC分类号： C07D207/27 , C07D207/16 , C07D209/08 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/70 , C07D213/75 , C07D217/26 , C07D233/68 , C07D243/12 , C07D253/06 , C07D271/06 , C07D277/06 , C07D277/46 , C07D277/56 , C07D295/15 , C07D307/68 , C07D317/58 , C07D335/10 , C07D401/04 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译：本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。在另一个实施方案中，本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。

42. 发明授权

US5374772A Substituted benzoic acids, inhibitors of phospholipases A.sub.2 失效
标题翻译：取代的苯甲酸，磷脂酶A2的抑制剂
公开(公告)号：US5374772A
公开(公告)日：1994-12-20
申请号：US141309
申请日：1993-10-22
申请人： Mathew Carson , Ru-Jen L. Han , Ronald LeMahieu , Vincent S. Madison
发明人： Mathew Carson , Ru-Jen L. Han , Ronald LeMahieu , Vincent S. Madison
IPC分类号： A61K31/135 , A61K31/235 , A61P1/04 , A61P11/00 , A61P17/00 , A61P19/06 , A61P37/08 , A61P43/00 , C07C43/225 , C07C65/21 , C07C65/24 , C07C69/86 , C07C69/88 , C07C69/92 , C07C219/14 , C07C315/04 , C07C317/22 , C07C65/00
CPC分类号： C07C317/22 , C07C43/225 , C07C65/24 , C07C69/92
摘要： The invention relates to compounds of the formula ##STR1## R is hydrogen, lower alkyl, --(CH.sub.2).sub.2 N(R.sub.3).sub.2 or --CH.sub.2 OOCR.sub.3 wherein R.sub.3 is lower alkyl;R.sub.1 is CH.sub.3 (CH.sub.2).sub.n --, wherein n is 0-17, or R.sub.4 (CH.sub.2).sub.p --, wherein p is 2-18 and R.sub.4 is 1- or 2-naphthyloxy, 2,3- or 3,4-dihydroxyphenyl, phenyl, phenoxy, or substituted phenyl or phenoxy wherein the substituent is selected from the group consisting of hydroxy, benzyloxy, methylsulfinyl, methylsulfonyl or phenyl;R.sub.2 is R.sub.4 (CH.sub.2).sub.p --, 1-adamantyl--CO-- or diphenylmethyl--CO--, and, when R is hydrogen, pharmaceutically acceptable salts with bases.The compounds of formula I are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of diseases, such as psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia, and trauma induced inflammation, such as spinal cord injury.
摘要翻译：本发明涉及下式的化合物：其中R 3为低级烷基; R 1为氢，低级烷基， - （CH 2）2 N（R 3）2或-CH 2 O R1是CH3（CH2）n-，其中n是0-17，或R4（CH2）p-，其中p是2-18，R4是1-或2-萘氧基，2,3-或3,4-二羟基苯基苯基，苯氧基或取代的苯基或苯氧基，其中取代基选自羟基，苄氧基，甲基亚磺酰基，甲基磺酰基或苯基; R2是R4（CH2）p-，1-金刚烷基-CO-或二苯基甲基-CO-，当R是氢时，是与碱的药学上可接受的盐。式I化合物是磷脂酶A2（PLA2's）的有效抑制剂，因此可用于治疗诸如牛皮癣，炎性肠病，哮喘，过敏，关节炎，皮炎，痛风，肺部疾病，心肌缺血和创伤等疾病引起炎症，如脊髓损伤。

43. 发明授权

US5298652A N-substituted glycines, inhibitors of phospholipase A.sub.2 失效
标题翻译： N-取代的甘氨酸，磷脂酶A2的抑制剂
公开(公告)号：US5298652A
公开(公告)日：1994-03-29
申请号：US987229
申请日：1992-12-08
申请人： Mathew Carson , Ru-Jen L. Han , Ronald A. LeMahieu , Vincent S. Madison
发明人： Mathew Carson , Ru-Jen L. Han , Ronald A. LeMahieu , Vincent S. Madison
IPC分类号： C07C235/52 , C07C235/78 , C07C237/36 , C07C237/42 , C07C229/34
CPC分类号： C07C235/78 , C07C235/52 , C07C237/36 , C07C237/42
摘要： Compounds of the formula ##STR1## R is hydrogen or --CH.sub.2 COOH; m is 0-2,x is 1-2, with the provision that when x is 2, m is always 0;R.sub.1 is CH.sub.3 (CH.sub.2).sub.n O--, CH.sub.3 (CH.sub.2).sub.n CONH--, CH.sub.3 (CH.sub.2).sub.n NHCONH--, CH.sub.3 (CH.sub.2).sub.n NHCOO--, HOOC(CH.sub.2).sub.p O-- or R.sub.3 (CH.sub.2).sub.q O--;R.sub.2 is hydrogen, carboxy, hydroxy, nitro, amino, CH.sub.3 (CH.sub.2).sub.n O--, CH.sub.3 (CH.sub.2).sub.n CONH--, CH.sub.3 (CH.sub.2).sub.n NHCONH--, CH.sub.3 (CH.sub.2).sub.n NHCOO--, HOOC(CH.sub.2).sub.p O--, R.sub.3 (CH.sub.2).sub.q O-- or R.sub.4 [O(CH.sub.2).sub.2 ].sub.r O--,wherein n is 0-17, p is 1-10, q is 1-12, r is 1-6,R.sub.3 is 1- or 2- naphthyloxy, 2,3- or 3,4-dihydroxyphenyl, phenyl, phenoxy or substituted phenyl or phenoxy, wherein the substituent is selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, nitro, amino, halo, carboxy or phenyl, andR.sub.4 is lower alkyl;and pharmaceutically acceptable salts with bases,are described.
摘要翻译：下式化合物R 1是氢或-CH 2 COOH; m为0-2，x为1-2，条件是当x为2时，m始终为0; R 1是CH 3（CH 2）n O-，CH 3（CH 2）n CONH-，CH 3（CH 2）n NHCHH-，CH 3（CH 2）n NHCOO-，HOOC（CH 2）p O-或R 3（CH 2）q O-; R 2是氢，羧基，羟基，硝基，氨基，CH 3（CH 2）n O-，CH 3（CH 2）n CONH-，CH 3（CH 2）n NHCO - ，CH 3（CH 2）n NHCOO - ，HOOC（CH 2）p O - ，R 3 ）qO-或R4 [O（CH2）2] rO-，其中n为0-17，p为1-10，q为1-12，r为1-6，R3为1-或2-萘氧基，2 ，3-或3,4-二羟基苯基，苯基，苯氧基或取代的苯基或苯氧基，其中取代基选自低级烷基，低级烷氧基，羟基，硝基，氨基，卤素，羧基或苯基，R4是低级烷基及其与碱的药学上可接受的盐。

44. 发明授权

US08440443B1 MEK1 polypeptides 失效
标题翻译： MEK1多肽
公开(公告)号：US08440443B1
公开(公告)日：2013-05-14
申请号：US11749550
申请日：2007-05-16
申请人： Thierry O. Fischmann , Hung V. Le , Vincent S. Madison , Anthony F. Mannarino , Todd W. Mayhood , Paul Reichert , Catherine Smith , Tin-Yau Chan
发明人： Thierry O. Fischmann , Hung V. Le , Vincent S. Madison , Anthony F. Mannarino , Todd W. Mayhood , Paul Reichert , Catherine Smith , Tin-Yau Chan
IPC分类号： C12N9/12
CPC分类号： C12N9/1205 , C07K2299/00 , C07K2319/40
摘要： The present invention provides, inter alia, crystals of the MEK1 polypeptide which are particularly useful for structure based drug design as well as methods of use thereof.
摘要翻译：本发明特别提供了特别可用于基于结构的药物设计的MEK1多肽的晶体及其使用方法。

45. 发明申请

US20100136620A1 SOLUBLE, STABLE FORM OF HDM2, CRYSTALLINE FORMS THEREOF AND METHODS OF USE THEREOF 失效
标题翻译：可溶性HDM2的稳定形式，其结晶形式及其使用方法
公开(公告)号：US20100136620A1
公开(公告)日：2010-06-03
申请号：US12621241
申请日：2009-11-18
申请人： Shahriar Shane Taremi , Gaolian Xie , Thomas Hesson , Jose S. Duca , Corey Strickland , William T. Windsor , Vincent S. Madison , Rumin Zhang , Paul Reichert , Yaolin Wang
发明人： Shahriar Shane Taremi , Gaolian Xie , Thomas Hesson , Jose S. Duca , Corey Strickland , William T. Windsor , Vincent S. Madison , Rumin Zhang , Paul Reichert , Yaolin Wang
IPC分类号： C12P21/00 , C07H21/04 , C12N15/63 , C12N1/21
CPC分类号： C07H21/04 , C07D209/20 , C07K14/47 , C07K2299/00
摘要： The present invention discloses modified Hdm2 proteins that are soluble. In addition, the present invention discloses nucleic acids that encode the modified Hdm2 proteins of the present invention. The invention also provides crystals of modified Hdm2 proteins that are suitable for X-ray crystallization analysis. The present invention also discloses methods of using the modified Hdm2 proteins and crystals thereof to identify, select and/or design compounds that may be used as anticancer agents. The present invention further discloses compounds that bind to modified Hdm2 proteins in protein-ligand complexes.
摘要翻译：本发明公开了可溶性的修饰的Hdm2蛋白。此外，本发明公开了编码本发明的修饰的Hdm2蛋白质的核酸。本发明还提供了适用于X射线结晶分析的修饰的Hdm2蛋白晶体。本发明还公开了使用修饰的Hdm2蛋白及其晶体鉴定，选择和/或设计可用作抗癌剂的化合物的方法。本发明还公开了与蛋白质 - 配体复合物中的修饰的Hdm2蛋白结合的化合物。

46. 发明申请

US20090081706A1 CRYSTALLINE FORM OF THE CATALYTIC DOMAIN OF AURORA 2 KINASE AND METHODS OF USE THEREOF 有权
标题翻译： AURORA 2激酶的催化域的结晶形式及其使用方法
公开(公告)号：US20090081706A1
公开(公告)日：2009-03-26
申请号：US12184770
申请日：2008-08-01
申请人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
发明人： Thierry O. Fischmann , Vincent S. Madison , Alan William Hruza , Paul Reichert , Lata Ramanathan , David Paul Sanden , Wolfgang Seghezzi
IPC分类号： G01N33/53 , C12N9/12 , G06F17/00 , C12N9/96
CPC分类号： C12N9/12
摘要： The present invention discloses nucleic acids that encode an active human Aurora 2 kinase catalytic domain. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active human Aurora 2 kinase catalytic domain. The present invention further discloses a crystalline form of a catalytic domain of human Aurora 2 kinase. In addition, the present invention discloses methods of using the X-ray diffractable crystals of human Aurora 2 kinase in structure assisted drug design to identify compounds that can modulate the enzymatic activity of human Aurora 2 kinase.
摘要翻译：本发明公开了编码活性人Aurora 2激酶催化结构域的核酸。本发明还公开了生长包含活性人Aurora 2激酶催化结构域的多肽的X射线衍射晶体的方法。本发明还公开了人Aurora 2激酶的催化结构域的结晶形式。此外，本发明公开了在结构辅助药物设计中使用人Aurora 2激酶的X射线衍射晶体的方法来鉴定可调节人Aurora 2激酶的酶活性的化合物。

47. 发明授权

US07459296B2 Hepatitis C virus NS3 helicase subdomain I 失效
标题翻译：丙型肝炎病毒NS3解旋酶子域I
公开(公告)号：US07459296B2
公开(公告)日：2008-12-02
申请号：US09825423
申请日：2001-04-03
申请人： Patricia C. Weber , Paul Reichert , Vincent S. Madison , Daniel F. Wyss , Nanhua Yao , Dingjiang Liu , Jennifer J. Gesell
发明人： Patricia C. Weber , Paul Reichert , Vincent S. Madison , Daniel F. Wyss , Nanhua Yao , Dingjiang Liu , Jennifer J. Gesell
IPC分类号： C12N9/12 , C07K14/00 , G01N31/00
CPC分类号： C07K14/005 , C12N9/90 , C12N2770/24222
摘要： This invention provides fragments of HCV NS3 helicase, and crystalline compositions thereof, based on subdomains of HCV helicase protein. The protein fragments are stable, soluble, and structurally sound. They can be expressed at high levels in conventional expressions systems, such as E. coli, to permit efficient, large-scale production for NMR-based screening applications and production of [2H,13C,15N]- and [13C,15N]-labeled polypeptides for structural NMR studies. Helicase fragments of the present invention are useful in the most advanced NMR techniques available, e.g., NMR-based drug discovery techniques such as SAR-by-NMR, in biological assays to discover inhibitors of HCV NS3 helicase, and to evaluate the mechanism of action and substrates for HCV NS3 helicase. Crystals of the present invention are useful for structure-based drug design studies using x-ray crystallographic techniques.
摘要翻译：本发明基于HCV解旋酶蛋白的亚结构域提供HCV NS3解旋酶的片段及其结晶组合物。蛋白质片段稳定，可溶，结构合理。它们可以在常规表达系统如大肠杆菌中以高水平表达，以允许基于NMR的筛选应用的有效的大规模生产和[2H，13C，15N] - 和[13C，15N] - 用于结构NMR研究的标记多肽。本发明的螺旋酶片段可用于可用的最先进的NMR技术，例如基于NMR的药物发现技术，例如通过核磁共振的核磁共振（NMR），用于发现HCV NS3解旋酶抑制剂的生物测定中，以及评估作用机制和HCV NS3解旋酶的底物。本发明的晶体可用于使用x射线晶体学技术的基于结构的药物设计研究。

48. 发明授权

US07208311B2 Catalytic domain of ADAM33 and methods of use thereof 失效
公开(公告)号：US07208311B2
公开(公告)日：2007-04-24
申请号：US10741204
申请日：2003-12-19
申请人： Wenyan Wang , Hung V. Le , Jian-Jun Liu , Vincent S. Madison , Winifred W. Prosise , Shahriar Shane Taremi , Li Xiao , Jun Zou
发明人： Wenyan Wang , Hung V. Le , Jian-Jun Liu , Vincent S. Madison , Winifred W. Prosise , Shahriar Shane Taremi , Li Xiao , Jun Zou
IPC分类号： C12N9/64 , C12N15/12 , C12N15/57 , C12N15/79
CPC分类号： C12N9/6489 , A61K38/00 , C07K14/705 , C07K2299/00 , C07K2319/00
摘要： The present invention discloses purified polypeptides that comprise an active ADAM33 catalytic domain. In addition, the present invention discloses nucleic acids that encode the polypeptides of the present invention. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active ADAM33 catalytic domain. In addition, the present invention discloses methods of using the X-ray diffractable crystals of ADAM33 in structure-based drug design to identify compounds that can modulate the enzymatic activity of ADAM33. The present invention also discloses methods of treating respiratory disorders by administering therapeutic amounts of the ADAM33 catalytic domain.

49. 发明授权

US5446189A Intermediates for the production of N-substituted anilines, inhibitors of phospholipases A.sub.2 失效
标题翻译：用于生产N-取代苯胺的中间体，磷脂酶A2抑制剂
公开(公告)号：US5446189A
公开(公告)日：1995-08-29
申请号：US216113
申请日：1994-03-22
申请人： Mathew Carson , Ru-Jen L. Han , Ronald A. LeMahieu , Vincent S. Madison
发明人： Mathew Carson , Ru-Jen L. Han , Ronald A. LeMahieu , Vincent S. Madison
IPC分类号： A61K31/19 , A61K31/195 , A61K31/215 , A61K31/27 , A61K31/44 , A61K31/4406 , A61K31/47 , A61P1/00 , A61P17/00 , A61P19/06 , A61P29/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07C229/18 , C07C229/60 , C07C229/64 , C07C233/43 , C07C237/30 , C07C237/38 , C07C271/42 , C07C271/44 , C07C271/56 , C07C275/02 , C07C311/09 , C07C317/22 , C07C317/34 , C07C317/36 , C07C317/44 , C07C323/36 , C07D213/30 , C07D215/14 , C07F9/40 , C07C229/34 , C07C229/36
CPC分类号： C07C323/36 , C07C229/18 , C07C229/60 , C07C229/64 , C07C233/43 , C07C237/30 , C07C237/38 , C07C271/44 , C07C311/09 , C07C317/22 , C07C317/36 , C07C317/44 , C07F9/4006 , C07C2103/74
摘要： Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, n, m, o, p, and q are as hereinafter set forth,and, when R.sub.2 is hydrogen, pharmaceutically acceptable salts thereof with bases, are described. The compounds of formula 1 are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.
摘要翻译：其中R1，R2，R3，R4，R5，R6，R7，R8，n，m，o，p和q如下文所述，其中R 2为氢时，药学上可接受的化合物其盐与碱的相互作用。式1的化合物是磷脂酶A2（PLA2's）的有效抑制剂，因此可用于治疗诸如精神病，炎性肠病，哮喘，变态反应，关节炎，皮炎，痛风，肺部疾病，心肌缺血/再灌注，以及创伤引起的炎症，如脊髓损伤。

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