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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.
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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。
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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.
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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.
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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。
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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 SUP>; 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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公开(公告)号:US06958332B2
公开(公告)日:2005-10-25
申请号:US10655672
申请日:2003-09-05
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: 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 , A61K31/506 , A61P19/02 , A61P25/28
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): 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 2和R 4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 SUP>; 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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公开(公告)号:US06693097B2
公开(公告)日:2004-02-17
申请号:US10000742
申请日:2001-11-30
申请人: Mitsunori Ono , Shijie Zhang , Teresa Przewloka , K. Koya , Elena Kostik , Yuniko Wada , Lijun Sun , Weiwen Ying
发明人: Mitsunori Ono , Shijie Zhang , Teresa Przewloka , K. Koya , Elena Kostik , Yuniko Wada , Lijun Sun , Weiwen Ying
IPC分类号: C07D41704
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): 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: 本发明的特征在于式(I)的嘧啶化合物: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,链烯基,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-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 1和R 2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。 -
公开(公告)号:US07067514B2
公开(公告)日:2006-06-27
申请号:US10656671
申请日:2003-09-05
申请人: Mitsunori Ono , Shijie Zhang , Teresa Przewloka , Keizo Koya , Elena Kostik , Yuniko Wada , Lijun Sun , Weiwen Ying
发明人: Mitsunori Ono , Shijie Zhang , Teresa Przewloka , Keizo Koya , Elena Kostik , Yuniko Wada , Lijun Sun , Weiwen Ying
IPC分类号: A61K31/506 , A61P3/10 , A61P17/06 , A61P19/02 , A61P25/28
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.
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公开(公告)号:US20060025409A1
公开(公告)日:2006-02-02
申请号:US11193001
申请日:2005-07-29
申请人: Mitsunori Ono , Shijie Zhang , Teresa Przewloka , Keizo Koya , Elena Kostik , Yuniko Wada , Lijun Sun , Weiwen Ying
发明人: Mitsunori Ono , Shijie Zhang , Teresa Przewloka , Keizo Koya , Elena Kostik , Yuniko Wada , Lijun Sun , Weiwen Ying
IPC分类号: A61K31/541 , A61K31/5377 , A61K31/53 , A61K31/506
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.
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