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41. 发明专利

CA2545259A1 HETEROARYL-HYDRAZONE COMPOUNDS 未知
公开(公告)号：CA2545259A1
公开(公告)日：2005-05-26
申请号：CA2545259
申请日：2004-11-10
申请人： SYNTA PHARMACEUTICALS CORP
发明人： ONO MITSUNORI , SUN LIJUN , WADA YUMIKO , NG HOWARD P , KOSTIK ELENA
IPC分类号： A61K31/497 , A61K20060101 , 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
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 verproduction-related disorders, methods of treati ng 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.

42. 发明专利

CA2502356A1 AROMATIC BICYCLIC HETEROCYLES TO MODULATE 1L - 12 PRODUCTION 未知
公开(公告)号：CA2502356A1
公开(公告)日：2004-04-29
申请号：CA2502356
申请日：2003-10-14
申请人： SYNTA PHARMACEUTICALS CORP
发明人： ONO MITSUNORI , SUN LIJUN , WADA YUMIKO , YING WEIWEN , PRZEWLOKA TERESA , KOSTIK ELENA
IPC分类号： A61P1/00 , A61P3/10 , A61P17/06 , A61P19/02 , C07D473/16 , C07D473/18 , C07D473/34 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07D401/10 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10 , A61K31/4743 , A61K31/4745 , A61K31/496 , A61K31/52 , A61K31/522 , A61K31/5355 , A61K31/541
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; R 3 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)NRbR~, NRaC(NRb)NRcRd, NRaC(O)ORb, S(O)NTRaR t, S(O)2NRSRb, S(O)Ra, S(O)2Ra, C(O)Ra, C(O)ORa, or C(O)NRaRl; R5 is H or alkyl ; n is 0, 1, 2, 3, 4, 5, or 6; A is 0, S, S(O), S(O)2, or NW; B is N or CRC; X is0, S, S(O), S(O)2, NR, or C(O); Y is a covalent bond, C(O), C=NR a, O, S, S(O), S(O)2, or NW; Z is N or CH; each of U and V, independently, is N or CR ; and W is 0, S, or NR'; in which each of Ra, Rb, Re, and Rd, independently, i s 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.

43. 发明专利

CA2468349A1 PYRIMIDINE COMPOUNDS 未知
公开(公告)号：CA2468349A1
公开(公告)日：2003-06-12
申请号：CA2468349
申请日：2002-11-27
申请人： SYNTA PHARMACEUTICALS CORP
发明人： SUN LIJUN , ZHANG SHIJIE , PRZEWLOKA TERESA , WU YAMING , ZHOU DAN , KOSTIK ELENA , KOYA KEIZO , ONO MITSUNORI , WADA YUMIKO , YING WEIWEN , 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 , C07D279/06 , A61K31/295 , C07D239/38 , C07D239/47 , C07D239/50 , A61K31/506 , C07D239/52 , C07D239/56
摘要： This invention features pyrimidine compounds of formula (I): R1 is formula (II), 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, S02Rc, S(O)Rc, S(02)NRcR d, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcS02Rd, 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(02), or NRc; Y is a covalent bond, CH2, C(O), C=N-Rc, C=N-ORc, C=N-SRc, O, S, S(O), S(02), 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(02), 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. 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).

44. 发明专利

CY1113828T1 ΕΝΩΣΕΙΣ ΤΡΙΑΖΟΛΙΟΥ ΠΟΥ ΡΥΘΜΙΖΟΥΝ ΔΡΑΣΤΙΚΟΤΗΤΑ HSP90 未知
公开(公告)号：CY1113828T1
公开(公告)日：2016-07-27
申请号：CY131100041
申请日：2013-01-14
申请人： SYNTA PHARMACEUTICALS CORP
发明人： YING WEIWEN , JAMES DAVID , ZHANG SHIJIE , PRZEWLOKA TERESA , CHAE JUNGHYUN , CHIMMANAMADA DINESH U , LEE CHI-WAN , KOSTIK ELENA , NG HOWARD P , FOLEY KEVIN , DU ZHENJIAN , BARSOUM JAMES
IPC分类号： C07D249/12 , A61K31/4196 , A61P35/00 , C07D401/04 , C07D403/04 , C07D405/04
摘要： Ηπαρούσαεφεύρεσηαφοράσευποκατεστημένεςενώσειςτριαζολίουκαισυνθέσειςπουπεριλαμβάνουνυποκατεστημένεςενώσειςτριαζολίου. Ηεφεύρεσηπεραιτέρωαφοράσεμεθόδουςαναστολήςτηςδραστικότητα Hsp90 σεέναυποκείμενοπουέχειανάγκηαυτήςκαιμεθόδουςγιααποτροπήή θεραπείαυπερπολλαπλασιαστικώνδιαταραχώνόπωςκαρκίνουσεέναυποκείμενοπουέχειανάγκηαυτής, πουπεριλαμβάνειχορήγησηστουποκείμενομιαςυποκατεστημένηςένωσηςτριαζολίουτηςεφεύρεσηςή μιαςσύνθεσηςπουπεριλαμβάνειμιατέτοιαένωση.

45. 发明专利

ME01644B BIS(TIO-HIDRAZID AMIDNE) SOLl ZA TRETMAN KANCERA 未知
公开(公告)号：ME01644B
公开(公告)日：2014-09-20
申请号：MEP12413
申请日：2005-06-20
申请人： SYNTA PHARMACEUTICALS CORP
发明人： VAGHEFI FARID , LIANG GUIQING , KOYA KEIZO , SUN LIJUN , TATSUTA NORIAKI , CHEN SHOUJUN , INOUE TAKAYO , XIA ZHI-QIANG , KOSTIK ELENA
IPC分类号： A61K31/16 , A61P35/00 , C07C327/56

46. 发明专利

ES2399241T3 Compuestos de triazol que modulan la actividad de HSP90 未知
公开(公告)号：ES2399241T3
公开(公告)日：2013-03-26
申请号：ES05851788
申请日：2005-11-17
申请人： SYNTA PHARMACEUTICALS CORP
发明人： YING WEIWEN , JAMES DAVID , ZHANG SHIJIE , PRZEWLOKA TERESA , CHAE JUNGHYUN , CHIMMANAMADA DINESH , LEE CHI-WAN , KOSTIK ELENA , NG HOWARD , FOLEY KEVIN , DU ZHENJIAN , BARSOUM JAMES
IPC分类号： C07D249/12 , A61K31/4196 , A61P35/00 , C07D401/04 , C07D403/04 , C07D405/04
摘要： Un compuesto representado por la siguiente fórmula estructural: o un tautómero, o una sal, un solvato o un clatrato farmacéuticamente aceptables del mismo, en la que: el anillo A es un arilo o un heteroarilo, en la que el arilo o el heteroarilo están opcionalmente sustituidos adicionalmente con uno o más sustituyentes además de R3; R1 y R3 son, independientemente, -OH, -SH, -NR7H, -OR26, -SR26, -NHR26, -O(CH2)mOH, -O(CH2)mSH, -O(CH2)mNR7H, -S(CH2)mOH, -S(CH2)mSH, -S(CH2)mNR7H, -OC(O)NR10R11, -SC(O)NR10R11, -NR7C(O)NR10R11, -OC(O)R7, -SC(O)R7, -NR7C(O)R7, -OC(O)OR7, -SC(O)OR7, -NR7C(O)OR7, -OCH2C(O)R7, -NR7CH2C(O)R7, -OCH2C(O)OR7, -NR7CH2C(O)OR7, -OCH2C(O)NR10R11, 10 NR7CH2C(O)NR10R11, -OS(O)pR7, -SS(O)pR7, -S(O)pOR7, -NR7S(O)pR7, -OS(O)pNR10R11, -SS(O)pNR10R11, -NR7S(O)pNR10R11, -OS(O)pOR7, -SS(O)pOR7, -NR7S(O)pOR7, -OC(S)R7, -SC(S)R7, -NR7C(S)R7, -OC(S)OR7, -SC(S)OR7, -NR7C(S)OR7, -OC(S)NR10R11, -SC(S)NR10R11, -NR7C(S)NR10R11, -OC(NR8)R7, -SC(NR8)R7, -NR7C(NR8)R7, -OC(NR8)OR7, -SC(NR8)OR7, -NR7C(NR8)OR7, -OC(NR8)NR10R11, -SC(NR8)NR10R11, -NR7C(NR8)NR10R11, -OP(O)(OR7)2 o -SP(O)(OR7)2; R5 es un heteroarilo opcionalmente sustituido o un arilo de 8 a 14 miembros opcionalmente sustituido; R7 y R8, para cada aparición, son, independientemente, -H, un alquilo opcionalmente sustituido, un alquenilo opcionalmente sustituido, un alquinilo opcionalmente sustituido, un cicloalquilo opcionalmente sustituido, un cicloalquenilo opcionalmente sustituido, un heterociclilo opcionalmente sustituido, un arilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, un aralquilo opcionalmente sustituido o un heteraralquilo opcionalmente sustituido; R10 y R11, para cada aparición, son independientemente -H, un alquilo opcionalmente sustituido, un alquenilo opcionalmente sustituido, un alquinilo opcionalmente sustituido, un cicloalquilo opcionalmente sustituido, un cicloalquenilo opcionalmente sustituido, un heterociclilo opcionalmente sustituido, un arilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, un aralquilo opcionalmente sustituido o 25 un heteraralquilo opcionalmente sustituido; o R10 y R11, tomados junto con el nitrógeno al que están unidos, forman un heterociclilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; R26 es un alquilo C1-C6; p, para cada aparición, es, independientemente, 0, 1 ó 2; y m, para cada aparición, es independientemente, 1, 2, 3 ó 4; con la condición de que el anillo A no sea un [1,2,3]triazol sustituido; y con la condición de que el compuesto no sea 3-(2,4-dihidroxi-fenil)-4-(naftalen-1-il)-5-mercapto-triazol.

47. 发明专利

PT1817295E COMPOSTOS DE TRIAZOL QUE MODULAM A ACTIVIDADE DA HSP90 未知
公开(公告)号：PT1817295E
公开(公告)日：2013-02-18
申请号：PT05851788
申请日：2005-11-17
申请人： SYNTA PHARMACEUTICALS CORP
发明人： ZHANG SHIJIE , YING WEIWEN , JAMES DAVID , PRZEWLOKA TERESA , CHAE JUNGHYUN , CHIMMANAMADA DINESH U , LEE CHI-WAN , KOSTIK ELENA , NG HOWARD P , FOLEY KEVIN , BARSOUM JAMES
IPC分类号： C07D249/12 , A61K31/4196 , A61P35/00 , C07D401/04 , C07D403/04 , C07D405/04

48. 发明专利

AU2005304393B2 IL-12 modulatory compounds 未知
公开(公告)号：AU2005304393B2
公开(公告)日：2012-09-27
申请号：AU2005304393
申请日：2005-11-10
申请人： SYNTA PHARMACEUTICALS CORP
发明人： SUN LIJUN , KOSTIK ELENA , PRZEWLOKA TERESA , NG HOWARD P , CHIMMANAMADA DINESH , DEMKO ZACHARY
IPC分类号： C07D413/00 , A61K31/535 , A61K31/5377
摘要： The invention relates to heterocyclic compounds, compositions including the compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, in modulating IL-12 production and processes mediated by IL-12.

49. 发明专利

AU2005244745B2 Disalt inhibitors of IL-12 production 未知
公开(公告)号：AU2005244745B2
公开(公告)日：2012-05-03
申请号：AU2005244745
申请日：2005-04-13
申请人： SYNTA PHARMACEUTICALS CORP
发明人： SUN LIJUN , KOSTIK ELENA
IPC分类号： C07D403/04 , A61K31/496 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/541 , C07D239/48 , C07D401/12 , C07D401/14 , C07D413/04 , C07D417/04 , C07D473/18 , C07D487/04
摘要： This invention relates to disalt nitrogen-heteroaryl inhibitors of IL-12 production, and related methods and pharmaceutical compositions.

50. 发明专利

AU2005306484B2 Triazole compounds that modulate Hsp90 activity 未知
公开(公告)号：AU2005306484B2
公开(公告)日：2010-03-18
申请号：AU2005306484
申请日：2005-11-17
申请人： SYNTA PHARMACEUTICALS CORP
发明人： JAMES DAVID , LEE CHI-WAN , YING WEIWEN , CHIMMANAMADA DINESH U , NG HOWARD P , FOLEY KEVIN , KOSTIK ELENA , DU ZHENJIAN , CHAE JUNGHYUN , BARSOUM JAMES , ZHANG SHIJIE , PRZEWLOKA TERESA
IPC分类号： C07D249/12 , A61K31/4196 , A61P35/00 , C07D401/04 , C07D403/04 , C07D405/04
摘要： The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.

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