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41. 发明授权

US07385084B2 Bis(thio-hydrazide amide) salts for treatment of cancers 有权
标题翻译：用于治疗癌症的双（硫代酰肼）酰胺盐
公开(公告)号：US07385084B2
公开(公告)日：2008-06-10
申请号：US11157213
申请日：2005-06-20
申请人： Keizo Koya , Lijun Sun , Elena Kostik , Farid Vaghefi , Shoujun Chen , Noriaki Tatsuta , Guiqing Liang , Takayo Inoue , Zhi-Qiang Xia
发明人： Keizo Koya , Lijun Sun , Elena Kostik , Farid Vaghefi , Shoujun Chen , Noriaki Tatsuta , Guiqing Liang , Takayo Inoue , Zhi-Qiang Xia
IPC分类号： C07C327/38 , A61K31/16
CPC分类号： C07D305/14 , C07C327/56 , C07C2601/02
摘要： Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation.Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.
摘要翻译：公开了由结构式（I）表示的双（硫代 - 酰肼酰胺）二醛：Y是共价键或取代或未取代的直链烃基。 R 1 -R 4独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基，或R 1， SUB和R 3与它们所键合的碳原子和氮原子一起，和/或R 2和R 4结合在一起与其键合的碳原子和氮原子形成任选地稠合到芳香环的非芳族杂环。 Z是-O或-S。 M + +是药学上可接受的一价阳离子，M 2 +是药学上可接受的二价阳离子。还公开了包含上述双（硫代 - 酰肼酰胺）二盐的药物组合物。进一步公开的是用癌症治疗受试者的方法。所述方法包括施用有效量的上述双（硫代 - 酰肼酰胺）二盐的步骤。

42. 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。

43. 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）。

44. 发明申请

US20100227860A1 DISALT INHIBITORS OF IL-12 PRODUCTION 审中-公开
标题翻译： IL-12生产的废物抑制剂
公开(公告)号：US20100227860A1
公开(公告)日：2010-09-09
申请号：US12782540
申请日：2010-05-18
申请人： Elena Kostik , Lijun Sun
发明人： Elena Kostik , Lijun Sun
IPC分类号： A61K31/5377 , A61P3/10 , A61P1/04 , A61P19/02 , A61P17/06 , A61P7/06 , A61P1/16 , A61P37/06 , A61P29/00
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。

45. 发明申请

US20050014754A1 Fused pyrrole compounds 审中-公开
标题翻译：熔融吡咯化合物
公开(公告)号：US20050014754A1
公开(公告)日：2005-01-20
申请号：US10799389
申请日：2004-03-12
申请人： Mitsunori Ono , Lijun Sun , ZhiQiang Xia , Elena Kostik , Keizo Koya , Masazumi Nagai , Yaming Wu
发明人： Mitsunori Ono , Lijun Sun , ZhiQiang Xia , Elena Kostik , Keizo Koya , Masazumi Nagai , Yaming Wu
IPC分类号： A61K20060101 , A61K31/429 , A61K31/5025 , A61K31/519 , A61K31/53 , C07D455/02 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
摘要： This invention relates to fused pyrrole compounds of Formula (I): and pharmaceutically acceptable salts and prodrugs thereof, wherein V1, V2, V3, V4, R1, R2, R3, W1 and W2 are as defined herein. The compounds of this invention may be used to prevent or treat cancer, inflammatory disorders, autoimmune diseasesand other conditions involving PDE4 or elevated levels of cytokines. The invention also provides methods of using the compounds to treat or prevent such disorders and pharmaceutical compositions containing the compounds.
摘要翻译：本发明涉及式（I）的稠合吡咯化合物及其药学上可接受的盐和前体药物，其中V1，V2，V3，V4，R1，R2，R3，W1和W2如本文所定义。本发明的化合物可用于预防或治疗癌症，炎症性疾病，自身免疫性疾病和涉及PDE4的其他病症或升高的细胞因子水平。本发明还提供了使用该化合物治疗或预防这些病症的方法和含有这些化合物的药物组合物。

46. 发明授权

US08637704B2 Polymorphs of N-malonyl-bis(N′-methyl-N′-thiobenzoylhydrazide) 失效
标题翻译： N-丙二酰基 - 双（N'-甲基-N'-硫代苯甲酰基酰肼）的多晶型物
公开(公告)号：US08637704B2
公开(公告)日：2014-01-28
申请号：US12745096
申请日：2008-11-28
申请人： Elena Kostik , Lijun Sun , Joanna Dziewiszek , Jun Y. Choi
发明人： Elena Kostik , Lijun Sun , Joanna Dziewiszek , Jun Y. Choi
IPC分类号： C07C327/56 , A61K31/166
CPC分类号： C07C327/56 , C07B2200/13
摘要： At least 70% by weight of Compound 1 is the single crystalline form, Form A, Form C, or Form D, of the compound. A pharmaceutical composition comprises a pharmaceutically acceptable carrier or diluent, and compound 1, wherein at least 70% by weight of the compound is the single crystalline form, Form A, Form C, or Form D, of the compound. A method of treating a subject with cancer comprises administering to the subject an effective amount of compound 1 or the pharmaceutical composition.
摘要翻译：化合物1的至少70重量％是化合物的单晶形式，形式A，形式C或形式D. 药物组合物包含药学上可接受的载体或稀释剂和化合物1，其中至少70重量％的化合物是化合物的单晶形式，形式A，形式C或形式D. 用癌症治疗受试者的方法包括向受试者施用有效量的化合物1或药物组合物。

47. 发明授权

US08461208B2 Bis(thio-hydrazide amide) salts for treatment of cancers 有权
标题翻译：用于治疗癌症的双（硫代酰肼）酰胺盐
公开(公告)号：US08461208B2
公开(公告)日：2013-06-11
申请号：US13273807
申请日：2011-10-14
申请人： Keizo Koya , Lijun Sun , Elena Kostik , Farid Vaghefi , Shoujun Chen , Noriaki Tatsuta , Guiqing Liang , Takayo Inoue , Zhi-Qiang Xia
发明人： Keizo Koya , Lijun Sun , Elena Kostik , Farid Vaghefi , Shoujun Chen , Noriaki Tatsuta , Guiqing Liang , Takayo Inoue , Zhi-Qiang Xia
IPC分类号： A61K31/16
CPC分类号： C07D305/14 , C07C327/56 , C07C2601/02
摘要： Disclosed are bis(thio-hydrazide amide) disalts and pharmaceutical compositions thereof. Also disclosed are methods of using bis(thio-hydrazide amide) disalts to treat cancer.
摘要翻译：公开了双（硫代酰肼酰胺）二盐及其药物组合物。还公开了使用双（硫代酰肼酰胺）狄尔斯治疗癌症的方法。

48. 发明申请

US20060135595A1 Bis(thio-hydrazide amide) salts for treatment of cancers 有权
标题翻译：用于治疗癌症的双（硫代酰肼）酰胺盐
公开(公告)号：US20060135595A1
公开(公告)日：2006-06-22
申请号：US11157213
申请日：2005-06-20
申请人： Keizo Koya , Lijun Sun , Elena Kostik , Farid Vaghefi , Shoujun Chen , Noriaki Tatsuta , Guiqing Liang , Takayo Inoue , Zhi-Qiang Xia
发明人： Keizo Koya , Lijun Sun , Elena Kostik , Farid Vaghefi , Shoujun Chen , Noriaki Tatsuta , Guiqing Liang , Takayo Inoue , Zhi-Qiang Xia
IPC分类号： A61K31/4015 , A61K31/16
CPC分类号： C07D305/14 , C07C327/56 , C07C2601/02
摘要： Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.
摘要翻译：公开了由结构式（I）表示的双（硫代 - 酰肼酰胺）二醛：Y是共价键或取代或未取代的直链烃基。 R 1 -R 4独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基，或R 1， SUB和R 3与它们所键合的碳原子和氮原子一起，和/或R 2和R 4结合在一起与其键合的碳原子和氮原子形成任选地稠合到芳香环的非芳族杂环。 Z是-O或-S。 M + +是药学上可接受的一价阳离子，M 2 +是药学上可接受的二价阳离子。还公开了包含上述双（硫代 - 酰肼酰胺）二盐的药物组合物。进一步公开的是用癌症治疗受试者的方法。所述方法包括施用有效量的上述双（硫代 - 酰肼酰胺）二盐的步骤。

49. 发明授权

US06858606B2 Pyrimidine compounds 失效
标题翻译：嘧啶化合物
公开(公告)号：US06858606B2
公开(公告)日：2005-02-22
申请号：US10305039
申请日：2002-11-26
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 , C07D417/04 , C07D401/04 , C07D405/04 , C07D409/04 , C07D413/04
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：R 1是R 1和R 2中的一个是H或烷基，另一个是任选被R d和R e m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为0，1，2，3，4，5或6; X是NR c; Y是共价键，CH 2，C（O），C = NR c，C = N-OR c，C = N-SR c，O，S，S（O），或NR ; Z是N或CH; U和V之一是N，另一个是CR ; 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; R d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; 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）。

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