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1. 发明申请

WO2005077940A1 DEHYDROPHENYLAHISTINS AND ANALOGS THEREOF AND THE SYNTHESIS OF DEHYDROPHENYLAHISTINS AND ANALOGS THEREOF 审中-公开
标题翻译：去甲羟化酶及其类似物及其脱氢维生素及其类似物的合成
公开(公告)号：WO2005077940A1
公开(公告)日：2005-08-25
申请号：PCT/US2005/003636
申请日：2005-02-04
申请人： NEREUS PHARMACEUTICALS, INC. , PALLADINO, Michael, A. , LLOYD, George, Kenneth , HAYASHI, Yoshio , NICHOLSON, Benjamin
发明人： PALLADINO, Michael, A. , LLOYD, George, Kenneth , HAYASHI, Yoshio , NICHOLSON, Benjamin
IPC分类号： C07D403/06
CPC分类号： C07D405/14 , C07D403/06 , C07D403/14 , C07D407/14 , C07D487/04
摘要： Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ', R 1 '', R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.
摘要翻译：公开了由以下结构（I）表示的化合物：制备这种化合物的方法，其中所述方法包括使二酰基二酮哌嗪与第一醛反应以产生中间体化合物; 并使所述中间体化合物与第二醛反应以产生一类具有通式结构的化合物，其中第一种醛和第二种醛选自恶唑烷羧醛，咪唑甲醛，苯甲醛，咪唑甲醛衍生物和苯甲醛衍生物，从而形成上述化合物，其中R1，R1'，R1“，R2，R3，R4，R5和R6，X1和X2，Y，Z，Z1，Z2，Z3和Z4各自可以以与所附描述一致。还公开了治疗血管增生的组合物和方法。

2. 发明申请

WO2006091669A1 ANTI-CANCER AND ANTI-MICROBIAL OXAZOLIDINONES AND ANALOGUES 审中-公开
标题翻译：抗癌和抗微生物氧化应激和类似物
公开(公告)号：WO2006091669A1
公开(公告)日：2006-08-31
申请号：PCT/US2006/006278
申请日：2006-02-22
申请人： NEREUS PHARMACEUTICALS, INC. , MACHERLA, Venkata, Rami, Reddy , NICHOLSON, Benjamin , LAM, Kin, Sing
发明人： MACHERLA, Venkata, Rami, Reddy , NICHOLSON, Benjamin , LAM, Kin, Sing
IPC分类号： C07D263/40 , C07C257/06 , A61K31/421 , A61K31/19 , A61P35/00 , A61P31/14 , C12P17/14 , C12P13/00
CPC分类号： C07D263/40 , C07C257/06 , C12P17/14
摘要： Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.
摘要翻译：本文公开了各种新的恶唑烷酮，咪唑啉酮和噻唑烷酮类似物以及使用这些类似物治疗癌症和/或微生物感染的方法。特定的4-恶唑烷酮化合物显示具有抗癌和抗微生物活性。

3. 发明授权

EP1856066B1 ANTI-CANCER AND ANTI-MICROBIAL OXAZOLIDINONES AND ANALOGUES 有权
标题翻译：抗癌和抗微生物恶唑烷酮类及其类似物
公开(公告)号：EP1856066B1
公开(公告)日：2011-03-30
申请号：EP06735789.7
申请日：2006-02-22
申请人： Nereus Pharmaceuticals, Inc.
发明人： MACHERLA, Venkata, Rami, Reddy , NICHOLSON, Benjamin , LAM, Kin, Sing
IPC分类号： C07D263/40 , C07C257/06 , A61K31/421 , A61K31/19 , A61P35/00 , A61P31/14 , C12P17/14 , C12P13/00
CPC分类号： C07D263/40 , C07C257/06 , C12P17/14
摘要： Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.

4. 发明公开

EP1856066A1 ANTI-CANCER AND ANTI-MICROBIAL OXAZOLIDINONES AND ANALOGUES 有权
标题翻译：抗癌和抗微生物恶唑烷酮类及其类似物
公开(公告)号：EP1856066A1
公开(公告)日：2007-11-21
申请号：EP06735789.7
申请日：2006-02-22
申请人： Nereus Pharmaceuticals, Inc.
发明人： MACHERLA, Venkata, Rami, Reddy , NICHOLSON, Benjamin , LAM, Kin, Sing
IPC分类号： C07D263/40 , C07C257/06 , A61K31/421 , A61K31/19 , A61P35/00 , A61P31/14 , C12P17/14 , C12P13/00
CPC分类号： C07D263/40 , C07C257/06 , C12P17/14
摘要： Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.

5. 发明公开

EP1812443A2 [3.2.0] HETEROCYCLIC COMPOUNDS AND METHODS OF USING THE SAME 审中-公开
标题翻译： [3.2.0] - 杂环化合物及其使用方法
公开(公告)号：EP1812443A2
公开(公告)日：2007-08-01
申请号：EP05818192.6
申请日：2005-04-29
申请人： Nereus Pharmaceuticals, Inc.
发明人： POTTS, Barbara, Christine , MACHERLA, Venkata, Rami, Reddy , MITCHELL, Scott, Sherman , MANAM, Rama, Rao , REED, Katherine, Anne , LAM, Kin, Sing , NEUTEBOOM, Saskia Theodora Cornelia , CHAO, Ta-Hsiang , NICHOLSON, Benjamin , BILLSTROM, Cheryl
IPC分类号： C07D491/04 , C07D207/12 , C07F5/02 , A61K31/407
CPC分类号： C07D491/04 , C07D207/28 , C07F5/025
摘要： Compounds of Formulae I-VI and derivatives thereof having anti-cancer, anti-inflammatory, and anti-microbial properties and to compositions that include one or more of compounds and their derivatives or analogs having anti-cancer, anti-inflammatory and anti-microbial properties are disclosed. Pharmaceutical compositions comprising such compounds and methods of treating cancer, inflammatory conditions, and microbial infections with the disclosed compounds or the disclosed pharmaceutical compositions are also disclosed.

6. 发明申请

WO2006028525A2 [3.2.0] HETEROCYCLIC COMPOUNDS AND METHODS OF USING THE SAME 审中-公开
标题翻译： [3.2.0]杂环化合物及其使用方法
公开(公告)号：WO2006028525A2
公开(公告)日：2006-03-16
申请号：PCT/US2005/014846
申请日：2005-04-29
申请人： NEREUS PHARMACEUTICALS, INC. , POTTS, Barbara, Christine , MACHERLA, Venkata, Rami, Reddy , MITCHELL, Scott, Sherman , MANAM, Rama, Rao , REED, Katherine, Anne , LAM, Kin, Sing , NEUTEBOOM, Saskia, Theodora, Cornelia , CHAO, Ta-Hsiang , NICHOLSON, Benjamin , BILLSTROM, Cheryl
发明人： POTTS, Barbara, Christine , MACHERLA, Venkata, Rami, Reddy , MITCHELL, Scott, Sherman , MANAM, Rama, Rao , REED, Katherine, Anne , LAM, Kin, Sing , NEUTEBOOM, Saskia, Theodora, Cornelia , CHAO, Ta-Hsiang , NICHOLSON, Benjamin , BILLSTROM, Cheryl
IPC分类号： A61K31/407 , C07D207/28 , C07D491/02 , C07D491/04
CPC分类号： C07D491/04 , C07D207/28 , C07F5/025
摘要： Compounds of Formulae I-VI and derivatives thereof having anti-cancer, anti-inflammatory, and anti-microbial properties and to compositions that include one or more of compounds and their derivatives or analogs having anti-cancer, anti-inflammatory and anti-microbial properties are disclosed. Pharmaceutical compositions comprising such compounds and methods of treating cancer, inflammatory conditions, and microbial infections with the disclosed compounds or the disclosed pharmaceutical compositions are also disclosed.
摘要翻译：具有抗癌，抗炎和抗微生物性质的式I-VI及其衍生物的化合物和包含一种或多种具有抗癌，抗炎和抗微生物的化合物及其衍生物或类似物的组合物属性被公开。还公开了包含这些化合物的药物组合物和用所公开的化合物或所公开的药物组合物治疗癌症，炎性病症和微生物感染的方法。

7. 发明申请

WO2004034970A2 MACROCYCLIC LACTAMS 审中-公开
公开(公告)号：WO2004034970A2
公开(公告)日：2004-04-29
申请号：PCT/US2003/030518
申请日：2003-09-25
申请人： NEREUS PHARMACEUTICALS, INC.
发明人： MITCHELL, Scott, S. , NICHOLSON, Benjamin
IPC分类号： A61K
CPC分类号： C07D225/02
摘要： Compounds represented by Formula (I), acid-addition salts and pro-drugs are disclosed, wherein the ring structure includes no substitutions, one substitution, or more than one substitution; and wherein n is equal to an integer greater than 1, preferably 2, 3, or 4; m is equal to a positive integer, preferably 1, 2 or 3, and each separate X n and X are each separately selected from a nucleophilic residue, preferably -H, -OH, -O-CO-alkyl, -O-alkyl, -NH 2 , a halogen and the like; and wherein the dashed line represents a C-C bond or a C-H bond, and the dashed and solid line represents either a carbon-carbon single bond or a carbon-carbon double bond.
摘要翻译：公开了由式（I）表示的化合物，酸加成盐和前药，其中环结构不包括取代，一个取代或一个以上的取代; 并且其中n等于大于1，优选2,3或4的整数; m等于正整数，优选1,2或3，并且每个分开的X和n各自独立地选自亲核残基，优选-H，-OH，-O-CO- 烷基，-O-烷基，-NH 2，卤素等; 并且其中虚线表示C-C键或者C-H键，并且虚线和实线表示碳 - 碳单键或者碳 - 碳双键。

8. 发明公开

EP1711487A1 DEHYDROPHENYLAHISTINS AND ANALOGS THEREOF AND THE SYNTHESIS OF DEHYDROPHENYLAHISTINS AND ANALOGS THEREOF 审中-公开
标题翻译： DEHYDROPHENYLAHISTINE及其类似物与DEHYDROPHENYLAHISTINEN和其类似物的合成
公开(公告)号：EP1711487A1
公开(公告)日：2006-10-18
申请号：EP05712910.8
申请日：2005-02-04
申请人： Nereus Pharmaceuticals, Inc.
发明人： PALLADINO, Michael, A. , LLOYD, George, Kenneth , HAYASHI, Yoshio , NICHOLSON, Benjamin
IPC分类号： C07D403/06 , C07D403/14 , C07D405/14 , C07D407/14 , C07D487/04 , A61K31/496 , A61P31/00 , A61P35/00
CPC分类号： C07D405/14 , C07D403/06 , C07D403/14 , C07D407/14 , C07D487/04
摘要： Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R1, R1', R1'', R2, R3, R4, R5, and R6, X1 and X2, Y, Z, Z1, Z2, Z3, and Z4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating vascular proliferation are also disclosed.

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