公开(公告)号：US06673825B2

公开(公告)日：2004-01-06

申请号：US10152117

申请日：2002-05-21

申请人： Michele Launay ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Eric Antoine Nicolai ,  Edwin J. Iwanowicz ,  T. G. Murali Dhar

发明人： Michele Launay ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Eric Antoine Nicolai ,  Edwin J. Iwanowicz ,  T. G. Murali Dhar

IPC分类号： A61K314196

CPC分类号： C07D487/04

摘要： Urazole compounds having the formula (I), or pharmaceutically-acceptable salts thereof, are effective as anti-inflammatory or immunosuppressive agents, wherein L and K are O or S; Q is a linker such as —O—, —S—, C(═O), and so forth, R1 is an aryl or heteroaryl group, and R3, R4a, R4c, Z, r, s and t are as defined in the specification.

摘要翻译： 具有式（I）的吖唑化合物或其药学上可接受的盐作为抗炎或免疫抑制剂是有效的，其中L和K是O或S; Q是诸如-O - ， - S - ，C（= O）等的连接基，R 1是芳基或杂芳基，R 3，R 4a，R 4c， ，Z，r，s和t如说明书中所定义。

公开(公告)号：US07078420B2

公开(公告)日：2006-07-18

申请号：US10852576

申请日：2004-05-24

申请人： T. G. Murali Dhar ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Michele Launay ,  Eric Antoine Nicolai ,  Edwin J. Iwanowicz

发明人： T. G. Murali Dhar ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Michele Launay ,  Eric Antoine Nicolai ,  Edwin J. Iwanowicz

IPC分类号： A61K31/4439 ,  C07D401/04

CPC分类号： C07D235/02 ,  C07D233/96 ,  C07D487/10

摘要： Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, wherein L and K are O or S; Z is N or CR4b; Ar is an optionally-substituted aryl or heteroaryl; G is a linker attached to T or M or is absent; J, M and T are selected to define a three to six membered saturated or partially unsaturated non-aromatic ring; and R2, R4a, R4b, and R4c are as defined 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，水合物，对映异构体和非对映异构体及其前药可用作LFA-1 / ICAM的抑制剂和作为抗炎剂的其中L和K为O或S ; Z是N或CR 4b; Ar是任选取代的芳基或杂芳基; G是连接于T或M或不存在的接头; 选择J，M和T来定义三至六元饱和或部分不饱和的非芳香环; 和R 2，R 4a，R 4b和R 4c如说明书中所定义。

公开(公告)号：US06710064B2

公开(公告)日：2004-03-23

申请号：US10000389

申请日：2001-11-30

申请人： Michele Launay ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Eric Antoine Nicolai ,  T. G. Murali Dhar ,  Edwin J. Iwanowicz

发明人： Michele Launay ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Eric Antoine Nicolai ,  T. G. Murali Dhar ,  Edwin J. Iwanowicz

IPC分类号： A61K314184

CPC分类号： C07D471/04 ,  C07D487/04

摘要： Compounds having the formula (I): and pharmaceutically-acceptable salts thereof, are useful for treating inflammatory or immune diseases, in which A is a four to seven membered heterocyclic or carbocyclic saturated ring; L and K are O or S; M is N or CH; Y is N or CH; Z is hydrogen, alkyl or substituted alkyl; and R1-R4 are as defined 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可用于治疗其中A为4至7元杂环或碳环饱和环的炎症或免疫疾病; L和K为O或S; M为N或CH; Y为N或CH; Z是氢，烷基或取代的烷基; 和R1-R4如说明书中所定义。

公开(公告)号：US06977267B2

公开(公告)日：2005-12-20

申请号：US10262182

申请日：2002-10-01

申请人： T. G. Murali Dhar ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Michele Launay ,  Eric Antoine Nicolai ,  Edwin J. Iwanowicz

发明人： T. G. Murali Dhar ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Michele Launay ,  Eric Antoine Nicolai ,  Edwin J. Iwanowicz

IPC分类号： C07D233/76 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P7/00 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/08 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P25/28 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P39/02 ,  C07D233/96 ,  C07D235/02 ,  C07D401/04 ,  C07D401/14 ,  C07D487/10 ,  C07D487/20 ,  C07D519/00

CPC分类号： C07D235/02 ,  C07D233/96 ,  C07D487/10

摘要： Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, wherein L and K are O or S; Z is N or CR4b; Ar is an optionally-substituted aryl or heteroaryl; G is a linker attached to T or M or is absent; J, M and T are selected to define a three to six membered saturated or partially unsaturated non-aromatic ring; and R2,R4a, R4b, and R4c are as defined 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，水合物，对映异构体和非对映异构体及其前药可用作LFA-1 / ICAM的抑制剂和作为抗炎剂的其中L和K为O或S ; Z是N或CR 4b; Ar是任选取代的芳基或杂芳基; G是连接于T或M或不存在的接头; 选择J，M和T来定义三至六元饱和或部分不饱和的非芳香环; 和R 2，R 4a，R 4b和R 4c如说明书中所定义。

公开(公告)号：US06974815B2

公开(公告)日：2005-12-13

申请号：US10681924

申请日：2003-10-09

申请人： T G. Murali Dhar ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Michele Launay ,  Eric Antoine Nicolai ,  Edwin J. Iwanowicz

发明人： T G. Murali Dhar ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Michele Launay ,  Eric Antoine Nicolai ,  Edwin J. Iwanowicz

IPC分类号： A61K20060101 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/437 ,  A61K31/4745 ,  C07D235/26 ,  C07D237/26 ,  C07D403/10 ,  C07D471/02

CPC分类号： C07D235/26 ,  C07D403/10

摘要： The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K is O or S; Q is —C(═O)— or optionally substituted C1-4alkylene; Ar is optionally-substituted aryl or heteroaryl; J1, J2, J3, and Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; Z is N or C(R9); and R1, R2, R3 and R9 are as defined in the specification.

摘要翻译： 本发明涉及具有式（I）的化合物：可用于治疗其中K为O或S的炎症和免疫疾病; Q是-C（-O） - 或任选取代的C 1-4 - 亚烷基; Ar是任选取代的芳基或杂芳基; J 1，J 2，J 3和Y被选择为使得环A为五至六元任选取代的环烯基 或具有0至2个氮杂原子的杂环; Z是N或C（R 9）; 且R 1，R 2，R 3和R 9均如说明书中所定义。

公开(公告)号：US07199125B2

公开(公告)日：2007-04-03

申请号：US10957255

申请日：2004-10-01

申请人： T. G. Murali Dhar ,  Edwin Iwanowicz ,  Michele Launay ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Eric Nicolai

发明人： T. G. Murali Dhar ,  Edwin Iwanowicz ,  Michele Launay ,  Dominique Potin ,  Magali Jeannine Blandine Maillet ,  Eric Nicolai

IPC分类号： C07D497/20 ,  C07D498/20 ,  A61K31/424 ,  A61K31/429 ,  A61K31/506

CPC分类号： C07D498/20 ,  C07D513/20

摘要： The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K and L are independently, O or S; Q is —C(═O)— or optionally substituted C1-6alkylene; Ar is optionally-substituted aryl or heteroaryl; J1, J2, J3 and Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; R1 is N or C(R9); and R2, and R3, are as defined in the specification.

摘要翻译： 本发明涉及具有式（I）的化合物：

公开(公告)号：US07375237B2

公开(公告)日：2008-05-20

申请号：US11206558

申请日：2005-08-18

申请人： T. G. Murali Dhar ,  Dharmpal S. Dodd ,  Dominique Potin ,  Michele Launay

发明人： T. G. Murali Dhar ,  Dharmpal S. Dodd ,  Dominique Potin ,  Michele Launay

IPC分类号： C07D209/32 ,  A01N43/38

CPC分类号： C07D487/04 ,  A61K31/407

摘要： Pyrrolizine compounds having the formula (I), or pharmaceutically-acceptable salts thereof, are effective in treating inflammatory or immune diseases, where A is a four- to seven-membered saturated ring, K is O or S, and R1, R2, R3 n, and M are defined in the specification.

摘要翻译： 具有式（I）的吡咯嗪化合物或其药学上可接受的盐在治疗炎症或免疫疾病方面是有效的，其中A是4至7元饱和环，K是O或S，R 1 R 2，R 3，R 3和M在说明书中定义。

公开(公告)号：US07186727B2

公开(公告)日：2007-03-06

申请号：US11301454

申请日：2005-12-13

申请人： T. G. Murali Dhar ,  Michele Launay ,  Dominique Potin ,  Scott Hunter Watterson ,  Zili Xiao

发明人： T. G. Murali Dhar ,  Michele Launay ,  Dominique Potin ,  Scott Hunter Watterson ,  Zili Xiao

IPC分类号： A61K31/4439 ,  C07D401/14

CPC分类号： C07D487/10

摘要： A class of substituted spiro-hydantoin compounds (II) having the formula: its pharmaceutically acceptable salts, enantiomers, solvates, or prodrugs thereof, wherein R16 is a substituted pyridinyl group, as defined herein, is provided. Pharmaceutical compositions and methods of treating anti-inflammatory and/or immune diseases with the pyridyl-substituted spiro-hydantoin compounds are also objectives of this invention.

摘要翻译： 一类具有下式的取代的螺 - 乙内酰脲化合物（II）：其药学上可接受的盐，对映异构体，溶剂合物或前药，其中R 16是如本文所定义的取代的吡啶基， 。 用吡啶基取代的螺 - 乙内酰脲化合物治疗抗炎和/或免疫疾病的药物组合物和方法也是本发明的目的。

公开(公告)号：US20050004153A1

公开(公告)日：2005-01-06

申请号：US10869292

申请日：2004-06-16

申请人： T.G. Dhar ,  Dominique Potin ,  Magali Blandine Maillet ,  Michele Launay ,  Eric Nicolai ,  Edwin Iwanowicz

发明人： T.G. Dhar ,  Dominique Potin ,  Magali Blandine Maillet ,  Michele Launay ,  Eric Nicolai ,  Edwin Iwanowicz

IPC分类号： C07D233/76 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P7/00 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/08 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P25/28 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P39/02 ,  C07D233/96 ,  C07D235/02 ,  C07D401/04 ,  C07D401/14 ,  C07D487/10 ,  C07D487/20 ,  C07D519/00 ,  A61K31/4747

CPC分类号： C07D235/02 ,  C07D233/96 ,  C07D487/10

摘要： Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, enantiomers, and diastereomers, and prodrugs thereof, are useful as inhibitors of LFA-1/ICAM and as anti-inflammatory agents, wherein L and K are O or S; Z is N or CR4b; Ar is an optionally-substituted aryl or heteroaryl; G is a linker attached to T or M or is absent; J, M and T are selected to define a three to six membered saturated or partially unsaturated non-aromatic ring; and R2, R4a, R4b, and R4c are as defined 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，水合物，对映异构体和非对映异构体及其前药可用作LFA-1 / ICAM的抑制剂和作为抗炎剂的其中L和K为O或S ; Z是N或CR4b; Ar是任选取代的芳基或杂芳基; G是连接于T或M或不存在的接头; 选择J，M和T来定义三至六元饱和或部分不饱和的非芳香环; R2，R4a，R4b和R4c如说明书中所定义。

公开(公告)号：US20050119279A1

公开(公告)日：2005-06-02

申请号：US10957255

申请日：2004-10-01

申请人： T. G. Dhar ,  Edwin Iwanowicz ,  Michele Launay ,  Dominique Potin ,  Magali Blandine Maillet ,  Eric Nicolai

发明人： T. G. Dhar ,  Edwin Iwanowicz ,  Michele Launay ,  Dominique Potin ,  Magali Blandine Maillet ,  Eric Nicolai

IPC分类号： C07D498/20 ,  C07D513/20 ,  A61K31/519 ,  A61K31/4188 ,  A61K31/4747 ,  C07D487/12

CPC分类号： C07D498/20 ,  C07D513/20

摘要： The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K and L are independently, O or S; Q is —C(═O)— or optionally substituted C1-6alkylene; Ar is optionally-substituted aryl or heteroaryl; J1, J2, J3 and Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; R1 is N or C(R9); and R2, and R3, are as defined in the specification.

摘要翻译： 本发明涉及具有式（I）的化合物：可用于治疗其中K和L独立地为O或S的炎症和免疫疾病; Q是-C（-O） - 或任选取代的C 1-6 - 亚烷基; Ar是任选取代的芳基或杂芳基; 选择J 1，J 2，J 3和Y，使得环A为5至6元任选取代的环烯基或 具有0至2个氮杂原子的杂环; R 1是N或C（R 9）; 和R 2 R 3和R 3'如说明书中所定义。