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41. 发明申请

US20100105676A1 FUSED HETEROCYCLIC COMPOUNDS USEFUL AS KINASE MODULATORS 有权
标题翻译：熔化的杂环化合物作为激酶调节剂有用
公开(公告)号：US20100105676A1
公开(公告)日：2010-04-29
申请号：US12532330
申请日：2008-03-20
申请人： Chunjian Liu , Katerina Leftheris , Andrew J. Tebben
发明人： Chunjian Liu , Katerina Leftheris , Andrew J. Tebben
IPC分类号： A61K31/5355 , C07D413/14 , C07D487/04 , A61K31/53 , A61P37/02
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, [PLEASE INSERT CHEMICAL STRUCTURE HERE] (I) are useful as kinase modulators, including Btk modulation, wherein R1, R2, R4, Q, Y, A and D are as defined herein.
摘要翻译：具有式（I）的化合物及其对映异构体和非对映体药学上可接受的盐可用作激酶调节剂，包括Btk调节，其中R1，R2，R4，Q， Y，A和D如本文所定义。

42. 发明授权

US06617323B2 Amino-substituted compounds useful as inhibitors of IMPDH enzyme 有权
标题翻译：可用作IMPDH酶抑制剂的氨基取代的化合物
公开(公告)号：US06617323B2
公开(公告)日：2003-09-09
申请号：US10155274
申请日：2002-05-23
申请人： Edwin J. Iwanowicz , Katerina Leftheris , Chunjian Liu , Toomas Mitt , Scott H. Watterson
发明人： Edwin J. Iwanowicz , Katerina Leftheris , Chunjian Liu , Toomas Mitt , Scott H. Watterson
IPC分类号： A61K31535
CPC分类号： C07D413/12 , C07D263/32
摘要： The present invention discloses compounds useful in treating or preventing IMPDH-associated disorders, such as transplant rejection and autoimmune diseases, having the formula (I), wherein X is —C(O)—, —C(S)—, or —S(O)2—; A is an optionally-substituted saturated or unsaturated monocyclic or bicyclic ring; B is a saturated or unsaturated monocyclic or bicyclic ring system having at least one substituent Q which is selected from R7 and R8; R7 is selected from (C0-C6)alkyl, (C2-C6)alkenyl and (C2-C6)alkynyl and R7 is substituted with R8 is selected from (C0-C6)alkyl, (C2-C6)alkenyl and (C2-C6)alkynyl and R8 is substituted with and Z1 through Z5 are as defined in the specification.
摘要翻译：本发明公开了可用于治疗或预防具有式（I）的IMPDH相关疾病如移植排斥反应和自身免疫性疾病的化合物，其中X是-C（O） - ， - C（S） - 或-S （O）2 - ; A是任选取代的饱和或不饱和单环或双环; B是具有至少一个选自R7和R8的取代基Q的饱和或不饱和单环或双环体系; R 7选自（C 0 -C 6）烷基，（C 2 -C 6）烯基和（C 2 -C 6）炔基，R 7被R 8取代为（C 0 -C 6）烷基，（C 2 -C 6）烯基和（C 2 -C 6 ）炔基和R8被Z取代，Z 1至Z 5如说明书中所定义。

43. 发明授权

US08044040B2 N-heterocyclic inhibitors of TNF-alpha expression 有权
标题翻译： TNF-α表达的N-杂环抑制剂
公开(公告)号：US08044040B2
公开(公告)日：2011-10-25
申请号：US11778219
申请日：2007-07-16
申请人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
发明人： Gulzar Ahmed , Axel Metzger , Ian Henderson , David J. Diller , Jun Wen , Stephen T. Wrobleski , Katerina Leftheris , Chunjian Liu
IPC分类号： C07D239/48 , A61K31/505
CPC分类号： C07D239/48 , C07D213/85 , C07D239/47 , C07D239/50 , C07D401/12 , C07D403/12
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
摘要翻译：公开了通过抑制p38激酶阻断细胞因子产生的N-杂环化合物。在一个实施方案中，本发明化合物由式（I）表示：还公开了使用本发明化合物治疗与p38激酶活性不适或TNF-α表达相关的病症的生产方法，药物组合物和方法。

44. 发明授权

US07462616B2 Pyrrolo-triazine aniline compounds useful as kinase inhibitors 有权
标题翻译：用作激酶抑制剂的吡咯并三嗪苯胺化合物
公开(公告)号：US07462616B2
公开(公告)日：2008-12-09
申请号：US11585598
申请日：2006-10-24
申请人： Alaric J. Dyckman , John T. Hynes , Katerina Leftheris , Chunjian Liu , Stephen T. Wrobleski
发明人： Alaric J. Dyckman , John T. Hynes , Katerina Leftheris , Chunjian Liu , Stephen T. Wrobleski
IPC分类号： C07D487/04 , C07D403/12 , C07D413/08 , A61K31/53 , A61K31/5377 , A61P19/02 , A61P19/04 , A61P9/10 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.
摘要翻译：具有式（I）的化合物及其药学上可接受的盐，前药和溶剂合物可用作激酶抑制剂，其中R1，R2，R3，R4，R5，R6，X和Z如说明书中所述。

45. 发明申请

US20070185175A1 Benzothiazole and azabenzothiazole compounds useful as kinase inhibitors 有权
标题翻译：可用作激酶抑制剂的苯并噻唑和氮杂苯并噻唑化合物
公开(公告)号：US20070185175A1
公开(公告)日：2007-08-09
申请号：US11494234
申请日：2006-07-27
申请人： Chunjian Liu , Katerina Leftheris , James Lin
发明人： Chunjian Liu , Katerina Leftheris , James Lin
IPC分类号： A61K31/428 , C07D417/02
CPC分类号： C07D513/04 , C07D417/04
摘要： A compound of Formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein A is independently selected from: further wherein R1, R2, R3, R4, R5, R6, R7, and W are as described herein. Also disclosed is a compound of Formula (II) or an enantiomer, diastereomer, or a pharmaceutically-acceptable salt thereof, wherein each of G, X and Y are independently CH or N, wherein at each occurrence at least one of G, X or Y is N and the other two of G, X or Y are CH; and B is independently selected from: further wherein R1, R2, R3, R4, R5, R8, R9 and Z are as described herein. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and Formula (II), and methods of treating conditions associated with the activity of p38 kinase.
摘要翻译：式（I）的化合物或其对映异构体，非对映异构体或其药学上可接受的盐，其中A独立地选自：其中R 1，R 2，R 2， R 4，R 4，R 5，R 6，R 7和/或R 4， W如本文所述。还公开了式（II）的化合物或其对映异构体，非对映异构体或其药学上可接受的盐，其中G，X和Y各自独立地为CH或N，其中在每次出现时，G，X或 Y为N，G，X或Y中的两个为CH; 并且B独立地选自：其中R 1，R 2，R 3，R 4，R 4，R 4， R 5，R 9，R 9和Z如本文所述。还公开了含有式（I）和式（II）化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。

46. 发明授权

US07572795B2 Pyrrolotriazine aniline prodrug compounds useful as kinase inhibitors 有权
标题翻译：可用作激酶抑制剂的吡咯并三嗪苯胺前药化合物
公开(公告)号：US07572795B2
公开(公告)日：2009-08-11
申请号：US11682331
申请日：2007-03-06
申请人： Chunjian Liu , Katerina Leftheris , Vivekananda M. Vrudhula , James Lin
发明人： Chunjian Liu , Katerina Leftheris , Vivekananda M. Vrudhula , James Lin
IPC分类号： C07D487/04 , A61K31/53 , A61P19/02 , A61P17/06 , A61P9/10
CPC分类号： C07D487/04
摘要： Compounds having the Formula (I), including pharmaceutically acceptable salts thereof, wherein at least one of X1, X2 or X3 is and any remaining X1, X2 or X3 is hydrogen, which are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, A1, A2 and m are as described herein.
摘要翻译：具有式（I）的化合物，包括其药学上可接受的盐，其中X 1，X 2或X 3中的至少一个为，并且任何其余的X 1，X 2或X 3为氢，其可用作激酶抑制剂，其中R 1，R 2，R 3， R4，R5，R6，A1，A2和m如本文所述。

47. 发明申请

US20090156555A1 PYRROLOTRIAZINE ANILINE PRODRUG COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：吡咯烷酮苯胺衍生物化合物作为激酶抑制剂有用
公开(公告)号：US20090156555A1
公开(公告)日：2009-06-18
申请号：US12370081
申请日：2009-02-12
申请人： Chunjian Liu , Katerina Leftheris , Vivekananda M. Vrudhula , James Lin
发明人： Chunjian Liu , Katerina Leftheris , Vivekananda M. Vrudhula , James Lin
IPC分类号： A61K31/675 , C07F9/6561 , A61K31/53 , C07D487/04 , A61P29/00
CPC分类号： C07D487/04
摘要： Compounds having the Formula (I), including pharmaceutically acceptable salts thereof wherein at least one of X1, X2 or X3 is and any remaining X1, X2 or X3 is hydrogen, which are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, A1, A2 and m are as described herein.
摘要翻译：具有式（I）的化合物，包括其药学上可接受的盐，其中X 1，X 2或X 3中的至少一个为，并且任何其余的X 1，X 2或X 3为氢，其可用作激酶抑制剂，其中R 1，R 2，R 3，R 4 R5，R6，A1，A2和m如本文所述。

48. 发明授权

US07253167B2 Tricyclic-heteroaryl compounds useful as kinase inhibitors 有权
标题翻译：可用作激酶抑制剂的三环杂芳基化合物
公开(公告)号：US07253167B2
公开(公告)日：2007-08-07
申请号：US11170571
申请日：2005-06-29
申请人： James Lin , Stephen T. Wrobleski , Chunjian Liu , Katerina Leftheris
发明人： James Lin , Stephen T. Wrobleski , Chunjian Liu , Katerina Leftheris
IPC分类号： C07D487/14 , A61K31/53 , A61P11/00 , A61P19/02 , A61P37/06
CPC分类号： C07D487/14
摘要： The present invention relates to compounds having the formula, wherein, Q is optionally substituted aryl or heteroaryl, R1 is hydrogen or C1-4alkyl, and R2, R3, R4 and R5 are hydrogen or optional substituents as defined in the specification.
摘要翻译：本发明涉及具有下式的化合物，其中Q为任选取代的芳基或杂芳基，R 1为氢或C 1-4烷基，R 1为氢或C 1-4烷基， R 2，R 3，R 4和R 5是氢或说明书中定义的任选的取代基。

49. 发明授权

US06399773B1 Compounds derived from an amine nucleus that are inhibitors of IMPDH enzyme 有权
标题翻译：衍生自作为IMPDH酶抑制剂的胺核的化合物
公开(公告)号：US06399773B1
公开(公告)日：2002-06-04
申请号：US09428432
申请日：1999-10-27
申请人： Chunjian Liu , T. G. Murali Dhar , Henry H. Gu , Edwin J. Iwanowicz , Katerina Leftheris , William J. Pitts
发明人： Chunjian Liu , T. G. Murali Dhar , Henry H. Gu , Edwin J. Iwanowicz , Katerina Leftheris , William J. Pitts
IPC分类号： C07D26528
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D263/32 , C07D263/48 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH mediated diseases, such as transplant rejection and autoimmune diseases.
摘要翻译：本发明公开了IMPDH（肌苷-5'-单磷酸脱氢酶）的新型抑制剂的鉴定。本文公开的化合物和药物组合物可用于治疗或预防IMPDH介导的疾病，例如移植排斥反应和自身免疫性疾病。

50. 发明授权

US06653304B2 Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators for treating respiratory and non-respiratory diseases 有权
标题翻译：大麻素受体调节剂，其制备方法和使用大麻素受体调节剂治疗呼吸和非呼吸系统疾病
公开(公告)号：US06653304B2
公开(公告)日：2003-11-25
申请号：US09779109
申请日：2001-02-08
申请人： Katerina Leftheris , Hong Wu , Stephen Wrobleski , Ping Chen , John Hynes , John Tokarski
发明人： Katerina Leftheris , Hong Wu , Stephen Wrobleski , Ping Chen , John Hynes , John Tokarski
IPC分类号： C07D40312
CPC分类号： C07D207/416 , A61K31/40 , A61K31/415 , A61K31/44 , C07D209/42 , C07D231/14 , C07D231/56 , C07D233/90 , C07D257/04 , C07D263/32 , C07D271/06 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D471/08
摘要： Use of a compound for treating a respiratory disease in a mammal wherein the compound is a cannabinoid receptor modulator is disclosed. Compounds useful as cannabinoid receptor modulators for treating respiratory and non-respiratory leukocyte-activation associated diseases comprise compounds of formula (I), in which A and B are nitrogen or carbon, provided only one of A and B is nitrogen; and R1-R6 are as defined in the specification, wherein R2 with R5 may form a ring, and/or two R4 groups may form a six-membered aryl or heteroaryl ring, optionally having a substituent R6 forming a ring with R3.
摘要翻译：公开了在化合物是大麻素受体调节剂的哺乳动物中用于治疗呼吸系统疾病的化合物的用途。用作治疗呼吸道和非呼吸性白细胞活化相关疾病的大麻素受体调节剂的化合物包括式（I）化合物，其中A和B为氮或碳，只提供A和B之一为氮; 和R 1 -R 6如说明书中所定义，其中R 2与R 5可以形成环，和/或两个R 4基团可以形成六元芳基或杂芳基环，任选地具有与R 3形成环的取代基R 6。

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