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1. 发明申请

WO2004064826A1 BIS (THIO-HYDRAZIDE AMIDE) COMPOUNDS FOR TREATING MULTI-DRUG RESISTANT CANCER 审中-公开
标题翻译： BIS（THIO-HYDRAZIDE AMIDE）化合物用于治疗多种耐药性癌症
公开(公告)号：WO2004064826A1
公开(公告)日：2004-08-05
申请号：PCT/US2004/001089
申请日：2004-01-15
申请人： SYNTA PHARMACEUTICALS CORP. , KOYA, Keizo , SUN, Lijun , WU, Yaming , KORBUT, Timoty , ZHOU, Dan , DU, Zhenjian , CHEN, Shoujun , TATSUTA, Noriaki , LIANG, Guiqing , ONO, Mitsunori
发明人： KOYA, Keizo , SUN, Lijun , WU, Yaming , KORBUT, Timoty , ZHOU, Dan , DU, Zhenjian , CHEN, Shoujun , TATSUTA, Noriaki , LIANG, Guiqing , ONO, Mitsunori
IPC分类号： A61K31/165
CPC分类号： A61K31/165 , A61K31/16 , A61K31/277
摘要： One embodiment of the present invention is a method of treating a subject with a multi-drug resistant cancer. The method comprises administering to the subject an effective amount of a compound represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group, or, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. R 1 -R 4 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R 1 and R 3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R 2 and R 4 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. Preferably R 1 and R 2 are the same and R 3 and R 4 are the same. R 5 -R 6 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. Z is =O or =S.
摘要翻译：本发明的一个实施方案是用多药耐药性癌症治疗受试者的方法。该方法包括向受试者施用有效量的由结构式（I）表示的化合物：Y是共价键或取代或未取代的直链烃基，或Y与两个> C = Z基团一起连接至其是键合的，是取代或未取代的芳基。 R 1 -R 4独立地为-H，脂族基团，取代的脂族基团，芳基或取代的芳基，或者R 1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 与它们所键合的碳原子和氮原子一起形成任选地与芳环稠合的非芳族杂环。优选地，R 1和R 2相同，并且R 3和R 4相同。 R5-R6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 Z = 0或= S。

2. 发明申请

WO2003047516A2 PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：嘧啶化合物
公开(公告)号：WO2003047516A2
公开(公告)日：2003-06-12
申请号：PCT/US2002/038161
申请日：2002-11-27
申请人： SYNTA PHARMACEUTICALS CORPORATION , ONO, Mitsunori , SUN, Lijun , PRZEWLOKA, Teresa , ZHANG, Shijie , KOSTIK, Elena , YING, Weiwen , WADA, Yumiko , KOYA, Keizo , WU, Yaming , ZHOU, Dan , TATSUTA, Noriaki
发明人： ONO, Mitsunori , SUN, Lijun , PRZEWLOKA, Teresa , ZHANG, Shijie , KOSTIK, Elena , YING, Weiwen , WADA, Yumiko , KOYA, Keizo , WU, Yaming , ZHOU, Dan , TATSUTA, Noriaki
IPC分类号： A61K
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): R 1 is formula (II), aryl, or heteroaryl; each of R 2 and R 4 , independently, is R c , halogen, nitro, cyano, isothionitro, SR c , or OR c ; or R 2 and R 4 , taken together, is carbonyl; R 3 is R c , alkenyl, alkynyl, OR c , OC(O)R c , S0 2 R c , S(O)R c , S(0 2 )NR c R d , SR c , NR c R d , NR c COR d , NR c C(O)OR d , NR c C(O)NR c R d , NR c S0 2 R d , COR c , C(O)OR c , or C(O)NR c R d ; R 5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(0 2 ), or NR c ; Y is a covalent bond, CH 2 , C(O), C=N-R c , C=N-OR c , C=N-SR c , O, S, S(O), S(0 2 ), or NR c ; Z is N or CH; one of U and V is N, and the other is CR c ; and W is O, S, S(O), S(0 2 ), NR c , or NC(O)R c ; in which each of R a and R b , independently, is H, alkyl, aryl, heteroaryl; and each of R c and R d , independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl. The compounds are useful for treating IL-12 overproduction related diseases (e.g., rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis, psoriasis, or insulin-dependent diabetes mellitus).
摘要翻译：本发明的特征是式（I）的嘧啶化合物：R1是式（II），芳基或杂芳基; 每个R 2和R 4独立地为R c，卤素，硝基，氰基，异硫氰酸根，SR c， sup>或OR ^{c ; 或者R 2和R 4合在一起为羰基; R 3是R c，烯基，炔基，OR c，OC（O）R c，S 0，（O）R c，S（O 2）NR c，其中R 1，R 2， R c，NR c，NR c，NR c，NR c，NR c，NR c R c，（O）OR d，NR c C（O）NR s，C（O）NR c， R c，R c，R c，R c，R c，R c，R c，R c，R c，R c， C（O）OR c或C（O）NR c R d; R 5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，CH 2，C（O），C = NR c，C = N-OR c，C = N -S（O）S，S（O），S（O 2）或NR C; Z是N或CH; U和V中的一个是N，另一个是CR ^{c ; 和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; 并且每个R c和R d独立地为H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基。该化合物可用于治疗IL-12过量产生相关疾病（例如类风湿性关节炎，败血症，克罗恩氏病，多发性硬化症，牛皮癣或胰岛素依赖性糖尿病）。}}

3. 发明申请

WO2009064374A3 ORAL FORMULATIONS OF BIS(THIOHYDRAZIDE AMIDES) 审中-公开
标题翻译： BIS（THIOHYDRAZIDE AMIDES）的口服制剂
公开(公告)号：WO2009064374A3
公开(公告)日：2010-05-06
申请号：PCT/US2008012613
申请日：2008-11-07
申请人： SYNTA PHARMACEUTICALS CORP , TATSUTA NORIAKI , INOUE TAKAYO , KOYA KEIZO
发明人： TATSUTA NORIAKI , INOUE TAKAYO , KOYA KEIZO
IPC分类号： A61K9/00 , A61K31/16
CPC分类号： A61K9/19 , A61K9/1075 , A61K31/16 , A61K31/165
摘要： Disclosed herein are oral formulations of bis(thio-hydrazide amides) compounds of the following structural formula (I) : or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R7, R8, Z, and Y are defined herein.
摘要翻译：本文公开了以下结构式（I）的双（硫代酰肼酰胺）化合物或其药学上可接受的盐的口服制剂，其中R 1，R 2，R 3，R 4，R 7，R 8，Z和Y在本文中定义。

4. 发明申请

WO2003006430A1 TAXOL ENHANCER COMPOUNDS 审中-公开
标题翻译： TAXOL增强剂化合物
公开(公告)号：WO2003006430A1
公开(公告)日：2003-01-23
申请号：PCT/US2002/021717
申请日：2002-07-10
申请人： SBR PHARMACEUTICALS CORP. , KOYA, Keizo , SUN, Lijun , CHEN, Shoujun , TATSUTA, Noriaki , WU, Yaming , ONO, Mitsunori
发明人： KOYA, Keizo , SUN, Lijun , CHEN, Shoujun , TATSUTA, Noriaki , WU, Yaming , ONO, Mitsunori
IPC分类号： C07C327/56
CPC分类号： A61K47/48176 , A61K31/16 , A61K31/165 , A61K31/277 , A61K31/337 , A61K31/381 , A61K31/44 , A61K31/505 , A61K31/53 , A61K47/58 , C07C327/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D209/44 , C07D213/83 , C07D261/18 , C07D305/14 , C07D307/68 , C07D333/38 , C07D333/68 , C07D407/12
摘要： Disclosed is a compound represented by the Structural Formula (I); Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or -C(R 7 R 8 )-. R 1 and R 2 are independently an aryl group or a substituted aryl group, R 3 and R 4 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R 5 -R 6 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R 7 and R 8 are each independently -H, an aliphatic or substituted aliphatic group, or R 7 is -H and R 8 is a substituted or unsubstituted aryl group, or, R 7 and R 8 , taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is =O or =S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with taxol or an analog of taxol.
摘要翻译：公开了由结构式（I）表示的化合物; Y是共价键，亚苯基或取代或未取代的直链烃基。此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。优选Y为共价键或-C（R 7 R 8） - 。 R 1和R 2独立地是芳基或取代的芳基，R 3和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。 R5-R6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团，或者R 7为-H且R 8为取代或未取代的芳基，或者R 7和R 8一起为C 2 -C 6取代或未取代的亚烷基。 Z = 0或= S。还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。还公开了通过向受试者施用结构式（I）的化合物与紫杉醇或紫杉醇的类似物组合治疗患有癌症的受试者的方法。

5. 发明申请

WO0024361A3 BIS(HALOETHYL)AMINOBENZENE DERIVATIVES 审中-公开
标题翻译： BIS（HALOETHYL）氨基苯衍生物
公开(公告)号：WO0024361A3
公开(公告)日：2000-09-08
申请号：PCT/US9922646
申请日：1999-09-29
申请人： SHIONOGI BIORESEARCH CORP , ONO MITSUNORI , KOYA KEIZO , SUN LIJUN , WRONA WOJCIECH , HOLDEN SYLVIA , TATSUTA NORIAKI
发明人： ONO MITSUNORI , KOYA KEIZO , SUN LIJUN , WRONA WOJCIECH , HOLDEN SYLVIA , TATSUTA NORIAKI
IPC分类号： C07D307/58 , A61K31/196 , A61K31/245 , A61K31/341 , A61K31/343 , A61P35/00 , C07C229/60 , C07C229/64 , C07D307/42 , C07C229/00
CPC分类号： C07D307/42 , C07C229/60 , C07C229/64 , C07C2601/02 , C07C2601/04
摘要： The present invention relates to bis(haloethyl)- aminobenzene derivatives featured by having carboxyl- containing moiety and one other moiety at the orthoposition with respect to the bis(haloethyl)amino substituent of the benzene ring. The moiety at the ortho position can be alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkyl(cycloalkyl), alkyl(heterocycloalkyl), alkyl(hetero-aryl), alkyl(aryl), -(-O- alkyl)2-5 or- Y - Y in which Y is O, S, or N(R ) wherein R is hydrogen or alkyl, and Y is alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroacryl, alkyl(cycloalkyl), alkyl(hetero-cycloalkyl), alkyl(aryl), or alkyl(heteroaryl).
摘要翻译：本发明涉及双（卤代乙基） - 氨基苯衍生物，其特征在于在苯环的双（卤代乙基）氨基取代基的相对位置具有含羧基的部分和一个其它部分。邻位的部分可以是烷基，环烷基，杂环烷基，芳基，杂芳基，烷基（环烷基），烷基（杂环烷基），烷基（杂芳基），烷基（芳基）， - （ - 或Y 1是Y，其中Y 1是O，S或N（R 5），其中R 5是氢或烷基，Y 2是烷基，烯基，环烷基，杂环烷基，芳基，异丙基丙烯基，烷基（环烷基），烷基（杂环烷基），烷基（芳基）或烷基（杂芳基）。

6. 发明申请

WO2009064374A2 ORAL FORMULATIONS OF BIS(THIOHYDRAZIDE AMIDES) 审中-公开
标题翻译：口服制剂BIS（硫代肼酰胺）
公开(公告)号：WO2009064374A2
公开(公告)日：2009-05-22
申请号：PCT/US2008/012613
申请日：2008-11-07
申请人： SYNTA PHARMACEUTICALS CORP. , TATSUTA, Noriaki , KOYA, Keizo , INOUE, Takayo
发明人： TATSUTA, Noriaki , KOYA, Keizo , INOUE, Takayo
IPC分类号： A61K9/00 , A61K31/16
CPC分类号： A61K9/19 , A61K9/1075 , A61K31/16 , A61K31/165
摘要： Disclosed herein are oral formulations of bis(thio-hydrazide amides) compounds of the following structural formula (I) : or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 7 , R 8 , Z, and Y are defined herein.
摘要翻译：本文公开了下列结构式（I）的双（硫代 - 酰肼酰胺）化合物的口服制剂：或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 7，R 8，Z 和Y在此定义。

7. 发明申请

WO2003006428A1 TAXOL ENHANCER COMPOUNDS 审中-公开
标题翻译： TAXOL增强剂化合物
公开(公告)号：WO2003006428A1
公开(公告)日：2003-01-23
申请号：PCT/US2002/021714
申请日：2002-07-10
申请人： SBR PHARMACEUTICALS CORP. , KOYA, Keizo , SUN, Lijun , CHEN, Shoujun , TATSUTA, Noriaki , WU, Yaming , ONO, Mitsunori , XIA, Zhi-Qiang
发明人： KOYA, Keizo , SUN, Lijun , CHEN, Shoujun , TATSUTA, Noriaki , WU, Yaming , ONO, Mitsunori , XIA, Zhi-Qiang
IPC分类号： C07C327/56
CPC分类号： C07D307/68 , A45D2008/006 , A61K31/337 , A61K31/505 , A61K31/53 , A61K31/5377 , A61K47/58 , C07C327/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D209/44 , C07D213/83 , C07D261/18 , C07D333/38 , C07D333/68
摘要： One embodiment of the present invention is a compound represented by Structural Formula (I) wherein Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or -C(R 7 R 8 )-. R 1 is an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, or a substituted non-aromatic hetereocyclic group, R 2 -R 4 are independently -H, an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, a substituted non-aromatic hetereocyclic group, an aryl group or a substituted aryl group, or R 1 and R 3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R 2 and R 4 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. R 5 -R 6 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R 7 and R 8 are each independently -H, an aliphatic or substituted aliphatic group, or R 7 is -H and R 8 is a substituted or unsubstituted aryl group, or, R 7 and R 8 , taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is =0 or =S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.
摘要翻译：本发明的一个实施方案是由结构式（I）表示的化合物，其中Y是取代或未取代的直链烃基的共价键。此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。优选Y为共价键或-C（R 7 R 8） - 。 R1是脂肪族基团，取代脂肪族基团，非芳香族杂环基团或取代的非芳香族杂环基团，R2-R4独立地是-H，脂肪族基团，取代的脂肪族基团，非芳香族的杂环基团，取代的非芳香族杂环基团，芳基或取代的芳基，或者R 1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与碳和氮原子一起形成与芳环稠合的非芳族杂环。 R5-R6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团，或者R 7为-H且R 8为取代或未取代的芳基，或者R 7和R 8一起为C 2 -C 6取代或未取代的亚烷基。 Z = 0或= S。还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。

8. 发明申请

WO2009064374A8 ORAL FORMULATIONS OF BIS(THIOHYDRAZIDE AMIDES) 审中-公开
标题翻译： BIS（THIOHYDRAZIDE AMIDES）的口服制剂
公开(公告)号：WO2009064374A8
公开(公告)日：2009-07-23
申请号：PCT/US2008012613
申请日：2008-11-07
申请人： SYNTA PHARMACEUTICALS CORP , TATSUTA NORIAKI , INOUE TAKAYO , KOYA KEIZO
发明人： TATSUTA NORIAKI , INOUE TAKAYO , KOYA KEIZO
IPC分类号： A61K9/00 , A61K31/16
CPC分类号： A61K9/19 , A61K9/1075 , A61K31/16 , A61K31/165
摘要： Disclosed herein are oral formulations of bis(thio-hydrazide amides) compounds of the following structural formula (I) : or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R7, R8, Z, and Y are defined herein.
摘要翻译：本文公开了以下结构式（I）的双（硫代酰肼酰胺）化合物或其药学上可接受的盐的口服制剂，其中R 1，R 2，R 3，R 4，R 7，R 8，Z和Y在本文中定义。

9. 发明申请

WO2006009940A1 BIS(THIO-HYDRAZIDE AMIDE) SALTS FOR TREATMENT OF CANCERS 审中-公开
标题翻译： BIS（THIO-HYDRAZIDE AMIDE）用于治疗癌症的药物
公开(公告)号：WO2006009940A1
公开(公告)日：2006-01-26
申请号：PCT/US2005/021642
申请日：2005-06-20
申请人： SYNTA PHARMACEUTICALS CORP. , KOSTIK, Elena , VAGHEFI, Farid , LIANG, Guiqing , KOYA, Keizo , SUN, Lijun , TATSUTA, Noriaki , CHEN, Shoujun , INOUE, Takayo , XIA, Zhi-Qiang
发明人： KOSTIK, Elena , VAGHEFI, Farid , LIANG, Guiqing , KOYA, Keizo , SUN, Lijun , TATSUTA, Noriaki , CHEN, Shoujun , INOUE, Takayo , XIA, Zhi-Qiang
IPC分类号： C07C327/56
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. R 1 -R 4 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R 1 and R 3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R 2 and R 4 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 M 2+ 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）二盐，Y是共价键或取代或未取代的直链烃基。 [R <子

10. 发明申请

WO03047516A3 PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：吡嗪化合物
公开(公告)号：WO03047516A3
公开(公告)日：2003-07-31
申请号：PCT/US0238161
申请日：2002-11-27
申请人： SYNTA PHARMACEUTICALS CORP , ONO MITSUNORI , SUN LIJUN , PRZEWLOKA TERESA , ZHANG SHIJIE , KOSTIK ELENA , YING WEIWEN , WADA YUMIKO , KOYA KEIZO , WU YAMING , ZHOU DAN , TATSUTA NORIAKI
发明人： ONO MITSUNORI , SUN LIJUN , PRZEWLOKA TERESA , ZHANG SHIJIE , KOSTIK ELENA , YING WEIWEN , WADA YUMIKO , KOYA KEIZO , WU YAMING , ZHOU DAN , TATSUTA NORIAKI
IPC分类号： C07D239/42 , A61K20060101 , A61K31/5377 , A61K31/541 , A61P1/04 , A61P3/10 , A61P17/06 , A61P25/00 , A61P29/00 , A61P31/04 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/14 , C07D239/32 , A61K31/295 , A61K31/506 , C07D239/38 , C07D239/47 , C07D239/50 , C07D239/52 , C07D239/56 , C07D279/06
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 formula (II), aryl, or heteroaryl; each of R2 and R4, independently, is R , halogen, nitro, cyano, isothionitro, SR , or OR ; or R2 and R4, taken together, is carbonyl; R3 is R , alkenyl, alkynyl, OR , OC(O)R , S02R , S(O)R , S(02)NR R , SR , NR R , NR COR , NR C(O)OR , NR C(O)NR R , NR S02R , COR , C(O)OR , or C(O)NR R ; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(02), or NR ; Y is a covalent bond, CH2, C(O), C=N-R , C=N-OR , C=N-SRc, O, S, S(O), S(02), or NR ; Z is N or CH; one of U and V is N, and the other is CR ; and W is O, S, S(O), S(02), NR , or NC(O)R ; in which each of R and R , independently, is H, alkyl, aryl, heteroaryl; and each of R and R , independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl. The compounds are useful for treating IL-12 overproduction related diseases (e.g., rheumatoid arthritis, sepsis, Crohn's disease, multiple sclerosis, psoriasis, or insulin-dependent diabetes mellitus).
摘要翻译：本发明具有式（I）的嘧啶化合物：R 1是式（II），芳基或杂芳基; R 2和R 4各自独立地是R c，卤素，硝基，氰基，异硫代，SR c或OR c; 或R 2和R 4一起是羰基; R 3是R c，烯基，炔基，OR c，OC（O）R c，SO 2 R c，S（O）R c，S（O 2）NR c NR c C（O）OR d，NR c C（O）NR c， R d，NR c，SO 2 R d，COR c，C（O）OR c或C（O）NR c R d; 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，CH 2，C（O），C = NR c，C = N-OR c，C = N-SRc，O，S，S（O），S（O 2） 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 a和R b各自独立地是H，烷基，芳基，杂芳基; R c和R d各自独立地是H，烷基，芳基，杂芳基，环基，杂环基或烷基羰基。该化合物可用于治疗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性糖尿病）。

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