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151. 发明授权

US08455686B2 Compounds for treating proliferative disorders 失效
公开(公告)号：US08455686B2
公开(公告)日：2013-06-04
申请号：US13333179
申请日：2011-12-21
申请人： Keizo Koya , Weiwen Ying , Teresa Kowalczyk-Przewloka , Lijun Sun
发明人： Keizo Koya , Weiwen Ying , Teresa Kowalczyk-Przewloka , Lijun Sun
IPC分类号： C07C391/00 , A61K31/095
CPC分类号： C07C391/00 , A61K31/165 , A61K31/18 , A61K45/06 , C07C259/20 , C07C2601/02
摘要： Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

152. 发明申请

US20110294798A1 IL-12 MODULATORY COMPOUNDS 有权
标题翻译： IL-12调节化合物
公开(公告)号：US20110294798A1
公开(公告)日：2011-12-01
申请号：US12978356
申请日：2010-12-23
申请人： Zachary Demko , Lijun Sun , Howard P. Ng
发明人： Zachary Demko , Lijun Sun , Howard P. Ng
IPC分类号： A61K31/5377 , A61P1/00 , A61P19/02
CPC分类号： C07D239/42 , C07D239/48 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The invention relates to cyclic hydrazone compounds, compositions including the cyclic hydrazone compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.
摘要翻译：本发明涉及环腙化合物，包括环腙化合物的组合物及其使用方法及其制备方法。化合物（和组合物）尤其用于调节由IL-12介导的IL-12产生和过程。

153. 发明授权

US07745436B2 Disalt inhibitors of IL-12 production 有权
标题翻译：抑制IL-12产生的抑制剂
公开(公告)号：US07745436B2
公开(公告)日：2010-06-29
申请号：US11105818
申请日：2005-04-13
申请人： Elena Kostik , Lijun Sun
发明人： Elena Kostik , Lijun Sun
IPC分类号： A61K31/5377 , C07D295/096
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D473/00 , C07D473/18 , C07D487/04
摘要： This invention relates to disalt nitrogen-heteroaryl inhibitors of IL-12 production, and related methods and pharmaceutical compositions.
摘要翻译：本发明涉及制备IL-12产生的氮杂芳族抑制剂，以及相关方法和药物组合物。

154. 发明授权

US07470685B2 Pyrimidine compounds 失效
标题翻译：嘧啶化合物
公开(公告)号：US07470685B2
公开(公告)日：2008-12-30
申请号：US11041537
申请日：2005-01-21
申请人： Lijun Sun , Mitsunori Ono , Elena Kostik , Yumiko Wada
发明人： Lijun Sun , Mitsunori Ono , Elena Kostik , Yumiko Wada
IPC分类号： A61K31/506 , A61P3/10 , A61P17/06 , A61P19/02 , A61P25/28 , C07D239/24 , C07D401/04 , C07D405/04 , C07D413/04 , C07D417/04
CPC分类号： C07D239/48 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D401/14 , C07D403/12
摘要： This invention features pyrimidine compounds of formula (I): R1 is in which one of Ra and Rb is H or alkyl, and the other is aryl or heteroaryl optionally substituted with Rd and Rem; each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C═N—Rc, C═N—ORc, C═N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; Rd is halogen, CN, alkyl, alkyloxy, alkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, alkylamino, or alkylaminocarbonyl; Re is halogen, CN, hydroxyl, alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, or heteroaryloxyl; and m is 0, 1, 2, 3, or 4. The pyrimidine compounds can be used to treat an IL-12 overproduction-related disorder (e.g., rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis, psoriasis, or insulin-dependent diabetes mellitus).
摘要翻译：本发明的特征在于式（I）的嘧啶化合物：其中R 1和R b中的一个是H或烷基，另一个是任选被Rd和Rem取代的芳基或杂芳基; R2和R4各自为H; R3是H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基; R5是H或烷基; n是0，1，2，3，4，5或6; X是NRc; Y是共价键，CH2，C（O），C-N-Rc，C-N-ORc，C-N-SRc，O，S，S（O），S（O 2）或NRc; Z是N或CH; U和V之一是N，另一个是CRc; 并且W是O，S，S（O），S（O 2），NR c或NC（O）R c; 其中R c是H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基; Rd是卤素，CN，烷基，烷氧基，烷基羰基，烷氧基羰基，芳氧基羰基，杂芳氧基羰基，羟基烷基，烷基氨基或烷基氨基羰基; Re是卤素，CN，羟基，烷基，芳基，杂芳基，烷氧基，芳氧基或杂芳氧基; 嘧啶化合物可用于治疗IL-12过度生产相关疾病（例如类风湿性关节炎，败血症，克罗恩病，多发性硬化，牛皮癣或胰岛素依赖型糖尿病）。

155. 发明申请

US20060063739A1 2-Substituted heteroaryl compounds 有权
标题翻译： 2-取代的杂芳基化合物
公开(公告)号：US20060063739A1
公开(公告)日：2006-03-23
申请号：US11174173
申请日：2005-07-01
申请人： Lijun Sun , Zachary Demko , Yumiko Wada , Shijie Zhang
发明人： Lijun Sun , Zachary Demko , Yumiko Wada , Shijie Zhang
IPC分类号： A61K31/5377 , C07D413/02 , A61K31/675
CPC分类号： C07F7/0836 , C07D213/74 , C07D239/42 , C07D239/48 , C07D251/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D417/06 , C07D417/12 , C07F5/025 , C07F9/65583
摘要： This invention relates to compounds of formula (I): or pharmaceutically acceptable salts, solvate, clathrates hydrates or polymorphs thereof, their compositions and methods of use and methods of making thereof. The compounds (and compositions) are useful in modulating IL-12 production and processes mediated by IL-12.
摘要翻译：本发明涉及式（I）的化合物：

156. 发明申请

US20050282809A1 Heteroaryl-hydrazone compounds 有权
标题翻译：杂芳基腙化合物
公开(公告)号：US20050282809A1
公开(公告)日：2005-12-22
申请号：US10985716
申请日：2004-11-10
申请人： Mitsunori Ono , Lijun Sun , Yumiko Wada , Elena Kostik , Howard NG
发明人： Mitsunori Ono , Lijun Sun , Yumiko Wada , Elena Kostik , Howard NG
IPC分类号： A61K20060101 , A61K31/497 , A61K31/5377 , C07D213/74 , C07D239/46 , C07D251/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14
CPC分类号： C07D213/74 , C07D239/47 , C07D251/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12
摘要： This invention relates to compounds having a formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, hydrate, prodrug or polymorph thereof wherein X is —C(Rg)═N-A. The invention also relates to methods of treating IL-12 overproduction-related disorders, methods of treating or preventing disorders related with excessive bone loss, methods for inhibiting osteoclast formation, and methods for treating or preventing a disorder associated with excessive bone resorption.
摘要翻译：本发明涉及具有式（I）的化合物或其药学上可接受的盐，溶剂化物，包合物，水合物，前药或多晶型物，其中X为-C（R） - N-A。本发明还涉及治疗IL-12过度生产相关疾病的方法，治疗或预防与过度骨丢失相关的障碍的方法，用于抑制破骨细胞形成的方法，以及用于治疗或预防与过度骨吸收相关的病症的方法。

157. 发明申请

US20050250787A1 Pyrimidine compounds 失效
标题翻译：嘧啶化合物
公开(公告)号：US20050250787A1
公开(公告)日：2005-11-10
申请号：US11041537
申请日：2005-01-21
申请人： Lijun Sun , Mitsunori Ono , Elena Kostik , Yumiko Wada
发明人： Lijun Sun , Mitsunori Ono , Elena Kostik , Yumiko Wada
IPC分类号： A61K31/506 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D43/04
CPC分类号： C07D239/48 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D401/14 , C07D403/12
摘要： This invention features pyrimidine compounds of formula (I): R1 is in which one of Ra and Rb is H or alkyl, and the other is aryl or heteroaryl optionally substituted with Rd and Rem; each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C═N—Rc, C═N—ORc, C═N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; Rd is halogen, CN, alkyl, alkyloxy, alkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, alkylamino, or alkylaminocarbonyl; Re is halogen, CN, hydroxyl, alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, or heteroaryloxyl; and m is 0, 1, 2, 3, or 4. The pyrimidine compounds can be used to treat an IL-12 overproduction-related disorder (e.g., rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis, psoriasis, or insulin-dependent diabetes mellitus).
摘要翻译：本发明的特征在于式（I）的嘧啶化合物：其中R a，R b和R b中的一个为H或烷基，和另一个是任选被R d和R e取代的芳基或杂芳基; R 2和R 4中的每一个是H; R 3是H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基; R 5是H或烷基; n是0，1，2，3，4，5或6; X是NR c; Y是共价键，CH 2，C（O），CNR C，O，CN-OR C， O，S，S（O），S（O 2 2）或NR C 2 O。 Z是N或CH; U和V之一是N，另一个是CR ; 和W是O，S，S（O），S（O 2 2），NR C或O或O（O）R c。其中R c为H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基; 卤素，CN，烷基，烷氧基，烷基羰基，烷氧基羰基，芳氧基羰基，杂芳氧基羰基，羟基烷基，烷基氨基或烷基氨基羰基; R e是卤素，CN，羟基，烷基，芳基，杂芳基，烷氧基，芳氧基或杂芳氧基; 嘧啶化合物可用于治疗IL-12过度生产相关疾病（例如类风湿性关节炎，败血症，克罗恩病，多发性硬化，牛皮癣或胰岛素依赖型糖尿病）。

158. 发明授权

US6071532A Synthesis of glycophospholipid and peptide-phospholipid conjugates and uses thereof 失效
标题翻译：糖磷脂和肽 - 磷脂缀合物的合成及其用途
公开(公告)号：US6071532A
公开(公告)日：2000-06-06
申请号：US729928
申请日：1996-10-15
申请人： Elliot L. Chaikof , Lijun Sun
发明人： Elliot L. Chaikof , Lijun Sun
IPC分类号： A61K9/127 , C07H15/10 , C07K1/107 , C07K9/00 , A61K38/00 , C07F9/02 , C07H19/04
CPC分类号： B82Y30/00 , A61K47/48053 , A61K9/1271 , C07H15/10 , C07K1/1077 , C07K9/001 , Y10S436/829 , Y10S530/81 , Y10T428/2984
摘要： The present invention provides glycophospholipid and peptide-phospholipid conjugates comprising a phospholipid moiety and a saccharide or peptide moiety joined by an ether linkage comprising a secondary or tertiary amine. The conjugate structure of the invention comprises a flexible spacer arm between the phospholipid and saccharide or peptide moieties which, being variable in length, serves to optimize saccharide or peptide bioactivity. This invention further provides a method for the synthesis of such conjugates comprising the step of reductive amination. The method is efficient, economical and provides a high yield of product. Glycophospholipid and peptide-phospholipid conjugates of the invention can be incorporated and, optionally, chemically polymerized in self-assembling systems such as membranes, bilayers, films, liposomes and the like, and find utility diagnostically and therapeutically in medical and immuno-biological applications.
摘要翻译：本发明提供了包含磷脂部分和通过包含仲胺或叔胺的醚键连接的糖或肽部分的糖磷脂和肽 - 磷脂缀合物。本发明的共轭结构包括在磷脂和糖或肽部分之间的柔性间隔臂，其长度可变地用于优化糖或肽的生物活性。本发明还提供了一种合成这种共轭物的方法，其包括还原胺化的步骤。该方法效率高，经济实惠，产品成品率高。本发明的糖尿病和肽 - 磷脂缀合物可以并入并任选地在诸如膜，双层，膜，脂质体等的自组装系统中化学聚合，并且在医学和免疫生物应用中在诊断和治疗上发现。

159. 发明授权

US5969133A Bioreductive cytotoxic agents 失效
标题翻译：生物还原性细胞毒素
公开(公告)号：US5969133A
公开(公告)日：1999-10-19
申请号：US83652
申请日：1998-05-22
申请人： Mitsunori Ono , Keizo Koya , Lijun Sun , Yumiko Wada , Wojciech Wrona , Natalie Dales , Xueliang Tao , Sylvia Holden
发明人： Mitsunori Ono , Keizo Koya , Lijun Sun , Yumiko Wada , Wojciech Wrona , Natalie Dales , Xueliang Tao , Sylvia Holden
IPC分类号： C07C229/56 , C07C229/60 , C07C229/64 , C07D209/08 , C07D209/12 , C07D235/12 , C07D295/112 , C07D307/42 , C07D307/79 , C07D265/30 , C07D235/02 , C07Z229/60 , C07Z261/00
CPC分类号： C07D295/112 , C07C229/56 , C07C229/60 , C07C229/64 , C07D209/08 , C07D209/12 , C07D235/12 , C07D307/42 , C07D307/79 , C07C2101/02 , C07C2101/04 , C07C2101/16
摘要： A compound which consists of a proactive alkylating moiety containing an electron-withdrawing group, a bioreductive moiety containing at least two double bonds, and a linker joining the proactive alkylating moiety and the bioreductive moiety.
摘要翻译：由包含吸电子基团的主动烷基化部分，含有至少两个双键的生物还原部分和连接主动烷基化部分和生物还原部分的连接体组成的化合物。

160. 发明申请

US20140031429A1 COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS 有权
标题翻译：用于治疗增生性疾病的化合物
公开(公告)号：US20140031429A1
公开(公告)日：2014-01-30
申请号：US13900788
申请日：2013-05-23
申请人： Keizo Koya , Weiwen Ying , Teresa Kowalczyk-Prezewloka , Lijun Sun
发明人： Keizo Koya , Weiwen Ying , Teresa Kowalczyk-Prezewloka , Lijun Sun
IPC分类号： C07C391/00 , A61K31/165 , A61K45/06 , A61K31/18
CPC分类号： C07C391/00 , A61K31/165 , A61K31/18 , A61K45/06 , C07C259/20 , C07C2601/02
摘要： Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
摘要翻译：公开了使用本发明化合物治疗患有增殖性疾病如癌症的受试者的化合物和方法，以及用于治疗响应于Hsp70诱导和/或自然杀伤诱导的病症的方法。此外，公开了包含本发明化合物和药学上可接受的载体的药物组合物。

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