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1. 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）。

2. 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。

3. 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）。

4. 发明授权

US07122665B2 Heterocyclic compounds 有权
公开(公告)号：US07122665B2
公开(公告)日：2006-10-17
申请号：US10686505
申请日：2003-10-14
申请人： Lijun Sun , Mitsunori Ono , Yumiko Wada , Weiwen Ying , Teresa Przewloka , Elena Kostik
发明人： Lijun Sun , Mitsunori Ono , Yumiko Wada , Weiwen Ying , Teresa Przewloka , Elena Kostik
IPC分类号： C07D413/14 , C07D413/04 , C07D487/02
CPC分类号： C07D473/34 , C07D473/16 , C07D473/18
摘要： This invention features a compound of formula (I): R1 is aryl or heteroaryl; each of R2 and R4, independently, is H, halogen, CN, alkyl, ORa, or NRaRb; R3 is H, halogen, CN, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, ORa, OC(O)Ra, OC(O)NRaRb, NRaRb, NRaC(O)Rb, NRaS(O)Rb, NRaS(O)2Rb, NRaC(O)NRbRc, NRaC(S)NRbRc, NRaC(NRb)NRcRd, NRaC(O)ORb, S(O)NRaRb, S(O)2NRaRb, S(O)Ra, S(O)2Ra, C(O)Ra, C(O)ORa, or C(O)NRaRb; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; A is O, S, S(O), S(O)2, or NRe; B is N or CRf; X is O, S, S(O), S(O)2, NRe, or C(O); Y is a covalent bond, C(O), C═NRa, O, S, S(O), S(O)2, or NRe; Z is N or CH; each of U and V, independently, is N or CR; and W is O, S, or NRe; in which each of Ra, Rb, Rc, and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; Re is H, alkyl, aryl, acyl, or sufonyl; and Rf is H, alkyl, aryl, acyl, sulfonyl, alkoxyl, amino, ester, amide, CN, or halogen. The compound is useful for treating an interleukin-12 overproduction-related disorder.

5. 发明授权

US07935698B2 Heteroaryl-hydrazone compounds 有权
标题翻译：杂芳基腙化合物
公开(公告)号：US07935698B2
公开(公告)日：2011-05-03
申请号：US10985716
申请日：2004-11-10
申请人： Mitsunori Ono , Lijun Sun , Yumiko Wada , Elena Kostik , Howard P. Ng
发明人： Mitsunori Ono , Lijun Sun , Yumiko Wada , Elena Kostik , Howard P. Ng
IPC分类号： A61K31/535 , 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，溶剂合物，包合物，水合物，前药或多晶型物，其中X为-C（R g）= 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。

6. 发明授权

US07470681B2 Pyrimidine compounds 失效
标题翻译：嘧啶化合物
公开(公告)号：US07470681B2
公开(公告)日：2008-12-30
申请号：US11193002
申请日：2005-07-29
申请人： Lijun Sun , Mitsunori Ono , Teresa Przewloka , Elena Kostik , Yumiko Wada
发明人： Lijun Sun , Mitsunori Ono , Teresa Przewloka , Elena Kostik , Yumiko Wada
IPC分类号： A61K31/506 , A61P17/06 , A61P19/02 , A61P25/28 , C07D401/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07D239/24
CPC分类号： C07D239/48 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D401/14 , C07D403/12
摘要： This invention features pyrimidine compounds of formula (I): R1 is 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 each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
摘要翻译：本发明具有式（I）的嘧啶化合物：R1各自为R 2，R 4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 a和R b各自独立地为H，烷基，芳基，杂芳基; Rc是H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基。

7. 发明授权

US07410990B2 Heterocyclic compounds 有权
公开(公告)号：US07410990B2
公开(公告)日：2008-08-12
申请号：US11542963
申请日：2006-10-03
申请人： Lijun Sun , Mitsunori Ono , Yumiko Wada , Weiwen Ying , Teresa Przewloka , Elena Kostik
发明人： Lijun Sun , Mitsunori Ono , Yumiko Wada , Weiwen Ying , Teresa Przewloka , Elena Kostik
IPC分类号： A61K31/4184 , A61K31/5377 , C07D265/30 , C07D235/30
CPC分类号： C07D473/34 , C07D473/16 , C07D473/18
摘要： This invention features a compound of formula (I): R1 is aryl or heteroaryl; each of R2 and R4, independently, is H, halogen, CN, alkyl, ORa, or NRaRb; R3 is H, halogen, CN, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, ORa, OC(O)Ra, OC(O)NRaRb, NRaRb, NRaC(O)Rb, NRaS(O)RbNRaS(O)2Rb, NRaC(O)NRbRc, NRaC(S)NRbRc, NRaC(NRb)NRcRd, NRaC(O)ORb, S(O)NRaRb, S(O)2NRaRb, S(O)Ra, S(O)2Ra, C(O)Ra, C(O)ORa, or C(O)NRaRb; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; A is O, S, S(O), S(O)2, or NRe; B is N or CRf; X is O, S, S(O), S(O)2, NRe, or C(O); Y is a covalent bond, C(O), C═NRa, O, S, S(O), S(O)2, or NRe; Z is N or CH; each of U and V, independently, is N or CR; and W is O, S, or NRe; in which each of Ra, Rb, Rc, and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; Re is H, alkyl, aryl, acyl, or sufonyl; and Rf is H, alkyl, aryl, acyl, sulfonyl, alkoxyl, amino, ester, amide, CN, or halogen. The compound is useful for treating an interleukin-12 overproduction-related disorder.

8. 发明申请

US20070027151A1 Heterocyclic compounds 有权
公开(公告)号：US20070027151A1
公开(公告)日：2007-02-01
申请号：US11542963
申请日：2006-10-03
申请人： Lijun Sun , Mitsunori Ono , Yumiko Wada , Weiwen Ying , Teresa Przewloka , Elena Kostik
发明人： Lijun Sun , Mitsunori Ono , Yumiko Wada , Weiwen Ying , Teresa Przewloka , Elena Kostik
IPC分类号： A61K31/5377 , C07D473/14
CPC分类号： C07D473/34 , C07D473/16 , C07D473/18
摘要： This invention features a compound of formula (I): R1 is aryl or heteroaryl; each of R2 and R4, independently, is H, halogen, CN, alkyl, ORa, or NRaRb; R3 is H, halogen, CN, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, ORa, OC(O)Ra, OC(O)NRaRb, NRaRb, NRaC(O)Rb, NRaS(O)RbN, RaS(O)2Rb, NRaC(O)NRbRc, NRaC(S)NRbRc, NRaC(NRb)NRcRd, NRaC(O)ORb, S(O)NRaRb, S(O)2NRaRb, S(O)Ra, S(O)2Ra, C(O)Ra, C(O)ORa, or C(O)NRaRb; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; A is O, S, S(O), S(O)2, or NRe; B is N or CRf; X is O, S, S(O), S(O)2, NRe, or C(O); Y is a covalent bond, C(O), C═NRa, O, S, S(O), S(O)2, or NRe; Z is N or CH; each of U and V, independently, is N or CR; and W is O, S, or NRe; in which each of Ra, Rb, Rc, and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; Re is H, alkyl, aryl, acyl, or sufonyl; and Rf is H, alkyl, aryl, acyl, sulfonyl, alkoxyl, amino, ester, amide, CN, or halogen. The compound is useful for treating an interleukin-12 overproduction-related disorder.

9. 发明授权

US07465725B2 Pyrimidine compounds 失效
标题翻译：嘧啶化合物
公开(公告)号：US07465725B2
公开(公告)日：2008-12-16
申请号：US11193001
申请日：2005-07-29
申请人： Mitsunori Ono , Lijun Sun , Teresa Przewloka , Shijie Zhang , Elena Kostik , Weiwen Ying , Yumiko Wada , Keizo Koya
发明人： Mitsunori Ono , Lijun Sun , Teresa Przewloka , Shijie Zhang , Elena Kostik , Weiwen Ying , Yumiko Wada , Keizo Koya
IPC分类号： A61K31/506 , A61P17/06 , A61P19/02 , A61P25/28 , C07D401/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07D239/24
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 aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a 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 each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
摘要翻译：本发明具有式（I）的嘧啶化合物：R1是芳基或杂芳基; R 2和R 4各自独立地是Rc，卤素，硝基，氰基，异硫脲，SRc或ORc; 或R 2和R 4一起是羰基; R3是Rc，烯基，炔基，ORc，OC（O）Rc，SO2Rc，S（O）Rc，S（O2）NRcRd，SRc，NRcRd，NRcCORd，NRcC（O）ORd，NRcC（O）NRcRd，NRcSO2Rd， CORc，C（O）ORc或C（O）NRcRd; R5是H或烷基; n是0，1，2，3，4，5或6; X是O，S，S（O），S（O 2）或NR c; 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 a和R b各自独立地为H，烷基，芳基，杂芳基; R c和R d各自独立地为H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基。

10. 发明申请

US20060030560A1 Pyrimidine compounds 失效
标题翻译：嘧啶化合物
公开(公告)号：US20060030560A1
公开(公告)日：2006-02-09
申请号：US11193002
申请日：2005-07-29
申请人： Lijun Sun , Mitsunori Ono , Teresa Przewloka , Elena Kostik , Yumiko Wada
发明人： Lijun Sun , Mitsunori Ono , Teresa Przewloka , Elena Kostik , Yumiko Wada
IPC分类号： A61K31/541 , A61K31/5377
CPC分类号： C07D239/48 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D401/14 , C07D403/12
摘要： This invention features pyrimidine compounds of formula (I): R1 is 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 each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
摘要翻译：本发明具有式（I）的嘧啶化合物：R 1和R 2各自为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 a，R b和R b各自独立地是H，烷基，芳基，杂芳基; 和R c是H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基。

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