公开(公告)号：US07598412B2

公开(公告)日：2009-10-06

申请号：US10961485

申请日：2004-10-08

申请人： Sara S. Hadida Ruah ,  Ashvani K. Singh ,  Mark T. Miller ,  Matthew Hamilton ,  Peter D. J. Grootenhuis

发明人： Sara S. Hadida Ruah ,  Ashvani K. Singh ,  Mark T. Miller ,  Matthew Hamilton ,  Peter D. J. Grootenhuis

IPC分类号： C07C229/00 ,  C07C233/00

CPC分类号： C07D307/87 ,  A61K31/00 ,  A61K31/335 ,  A61K31/38 ,  A61K31/40 ,  A61K31/41 ,  A61K31/435 ,  A61K31/495 ,  A61K45/06 ,  C07C233/22 ,  C07C233/60 ,  C07C233/65 ,  C07C233/73 ,  C07C235/34 ,  C07C235/46 ,  C07C235/48 ,  C07C311/16 ,  C07C311/17 ,  C07C323/60 ,  C07C2601/08 ,  C07D209/42 ,  C07D213/82 ,  C07D215/54 ,  C07D217/26 ,  C07D231/14 ,  C07D231/56 ,  C07D237/28 ,  C07D261/20 ,  C07D307/68 ,  C07D307/85 ,  C07D333/32 ,  C07D333/70 ,  C07D407/12

摘要： The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.

摘要翻译： 本发明提供了可用作ABC转运蛋白活性调节剂的式I化合物或其药学上可接受的盐，其中RB，n，B，RC，RD，RE，A和Z通常在下面的类别和亚类中进行描述。 本发明还提供了与式I相关的药物组合物，方法和试剂盒，其用作调节剂，以及用于治疗与ABC转运蛋白相关的疾病和疾病状况。

公开(公告)号：US07169798B2

公开(公告)日：2007-01-30

申请号：US10779532

申请日：2004-02-13

申请人： Jeremy Green ,  Guy Bemis ,  Anne-Laure Grillot ,  Mark Ledeboer ,  Francesco G. Salituro ,  Edmund Harrington ,  Huai Gao ,  Christopher Baker ,  Jingrong Cao ,  Michael Hale

发明人： Jeremy Green ,  Guy Bemis ,  Anne-Laure Grillot ,  Mark Ledeboer ,  Francesco G. Salituro ,  Edmund Harrington ,  Huai Gao ,  Christopher Baker ,  Jingrong Cao ,  Michael Hale

IPC分类号： C07D401/04 ,  C07D413/04 ,  A61K31/42 ,  C07D403/04

CPC分类号： C07D413/04 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/42 ,  C07D413/14

摘要： The present invention provides compounds of formula I: where R1 is H, CONH2, T(n)-R, or T(n)-Ar2, n may be zero or one, and G, XYZ, and Q are as described below. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

摘要翻译： 本发明提供了式I的化合物：其中R 1是H，CONH 2，T（N，N）-R或T（< n可以是0或1，并且G，XYZ和Q如下所述。 这些化合物是蛋白激酶的抑制剂，特别是JNK的抑制剂，哺乳动物蛋白激酶涉及细胞增殖，细胞死亡和对细胞外刺激的反应。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。

公开(公告)号：US07115746B2

公开(公告)日：2006-10-03

申请号：US10775687

申请日：2004-02-10

申请人： John R. Snoonian ,  Patricia Ann Oliver-Shaffer

发明人： John R. Snoonian ,  Patricia Ann Oliver-Shaffer

IPC分类号： C07D213/02

CPC分类号： C07D213/75 ,  C07D213/56 ,  C07D213/80 ,  C07D213/803 ,  C07D213/82

摘要： The present invention relates to processes for the facile synthesis of diaryl amines and analogues thereof. The processes of the present invention produce diaryl amines in high yield and purity. The present invention also relates to intermediates useful in the process of the present invention.

摘要翻译： 本发明涉及易于合成二芳基胺及其类似物的方法。 本发明的方法以高产率和纯度产生二芳基胺。 本发明还涉及可用于本发明方法的中间体。

公开(公告)号：US06949655B2

公开(公告)日：2005-09-27

申请号：US10170965

申请日：2002-06-13

申请人： David Lauffer ,  Ronald Tomlinson ,  Eckhard Ottow ,  Martyn Botfield

发明人： David Lauffer ,  Ronald Tomlinson ,  Eckhard Ottow ,  Martyn Botfield

IPC分类号： C07D295/18 ,  A61K31/445 ,  A61K31/495 ,  A61K45/00 ,  A61P3/10 ,  A61P9/10 ,  A61P19/00 ,  A61P19/02 ,  A61P21/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07B61/00 ,  C07D211/16 ,  C07D295/185

CPC分类号： C07D295/185 ,  C07D211/16 ,  C40B40/00

摘要： A compound having the formula (I): wherein: each R1, R2, R3 and R4 are independently selected from (C1-C10)-straight or branched alkyl, Ar-substituted- (C1-C10)-straight or branched alkyl, (C2-C10)-straight or branched alkenyl or alkynyl, or Ar-substituted-(C2-C10)-straight or branched alkenyl or alkynyl; wherein one to two CH2 groups of said alkyl, alkenyl, or alkynyl chains in each of R1, R2, R3 and R4 are optionally and independently replaced with O, S, S(O), S(O), S(O)2, C(O) or N(R5) in a chemically stable arrangement, wherein the CH2 group of R1 and R2 bound directly to said nitrogen cannot be replaced with C(O); or R1 and R2 taken together form a 4 to 7 membered ring; or R3 and R4 taken together form a 3 to 7 membered ring; wherein a CH2 in either the R1 and R2 ring system or the R3 and R4 ring system is independently and optionally replaced with O, C(O), N(R5), S, S(O), S(O)2 in a chemically stable arrangement; or wherein either or both of the R1 and R2 ring system and the R3 and R4 ring system is optionally fused with Ar. These compounds are useful for treating or preventing neuronal damage, particularly damage associated with neurological diseases. These compounds are also useful for stimulating nerve growth. The invention also provides compositions comprising these compounds, and methods of utilizing those compositions for treating or preventing neuronal damage or for stimulating nerve growth.

公开(公告)号：US06949580B2

公开(公告)日：2005-09-27

申请号：US10686690

申请日：2003-10-16

申请人： Michael Hale ,  James Janetka ,  Francois Maltais

发明人： Michael Hale ,  James Janetka ,  Francois Maltais

IPC分类号： C07D231/12 ,  A61K31/4155 ,  A61K31/4196 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  A61L33/00 ,  A61P1/16 ,  A61P3/10 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P17/06 ,  A61P19/08 ,  A61P25/28 ,  A61P31/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07D231/14 ,  C07D231/38 ,  C07D249/08 ,  C07D401/14 ,  C07D403/02 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

CPC分类号： C07D231/38 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

摘要： Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1, R2, T and Ht are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

摘要翻译： 本文描述了可用作具有下式的蛋白激酶抑制剂的化合物：其中R 1，R 2，T和H t在说明书中描述。 该化合物可用于治疗由蛋白激酶抑制剂，特别是癌症，炎症性疾病，再狭窄和心血管疾病等疾病减轻的哺乳动物的疾病状态。

公开(公告)号：US06884804B2

公开(公告)日：2005-04-26

申请号：US10146984

申请日：2002-05-16

申请人： Young Choon-Moon

发明人： Young Choon-Moon

IPC分类号： C07D401/04 ,  A61F2/00 ,  A61F9/00 ,  A61K9/00 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/00 ,  A61P1/04 ,  A61P1/18 ,  A61P3/10 ,  A61P11/06 ,  A61P13/12 ,  A61P19/08 ,  A61P19/10 ,  A61P25/00 ,  A61P25/02 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

CPC分类号： A61F9/0017 ,  A61F2250/0067 ,  A61K9/0051 ,  Y02A50/463

摘要： The present invention provides compounds of formula I: wherein A is N or CR, and G, R1, R2 and R3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of Src mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

摘要翻译： 本发明提供式I化合物：其中A为N或CR，G，R 1，R 2和R 3为 在说明书中描述。 这些化合物是蛋白激酶的抑制剂，特别是参与细胞增殖，细胞死亡和细胞外刺激反应的Src哺乳动物蛋白激酶的抑制剂。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。

公开(公告)号：US07592340B2

公开(公告)日：2009-09-22

申请号：US11004657

申请日：2004-12-03

申请人： Guy W. Bernis ,  John P. Duffy

发明人： Guy W. Bernis ,  John P. Duffy

IPC分类号： C07D241/42 ,  C07D241/44 ,  A61K31/498 ,  A61P35/04 ,  A61P37/02 ,  A61P25/28

CPC分类号： C07D241/26 ,  C07D241/44 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

摘要： The present invention relates to compounds of formula I useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

摘要翻译： 本发明涉及可用作蛋白激酶抑制剂的式I化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

公开(公告)号：US07115739B2

公开(公告)日：2006-10-03

申请号：US09953471

申请日：2001-09-14

申请人： David Bebbington ,  Ronald Knegtel ,  Hayley Binch ,  Julian M. C. Golec ,  Pan Li ,  Jean-Damien Charier

发明人： David Bebbington ,  Ronald Knegtel ,  Hayley Binch ,  Julian M. C. Golec ,  Pan Li ,  Jean-Damien Charier

IPC分类号： C07D403/12 ,  C07D403/14 ,  A61K31/517 ,  A61P5/48

CPC分类号： C07D401/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

摘要： This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.

摘要翻译： 本发明描述了式IX的新型三唑化合物：其中Z 1是氮或CR 9和Z 2是氮或CH，条件是在 Z 1和Z 2中的至少一个是氮; G是环C或环D; 环C选自苯基，吡啶基，嘧啶基，哒嗪基，吡嗪基或1,2,4-三嗪基，其中所述环C具有一个或两个独立地选自-R 1的邻位取代基; 环D是选自芳基，杂芳基，杂环基或碳环基的5-7元单环或8-10元双环; R＆lt; x＆gt;和＆lt; y＆gt; y＆lt; / sup＆gt;是独立地选自TR 3，或R x x和R y， / SUP>与它们的插入原子一起形成稠环; R 1，R 3和R 3如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为GSK-3和Aurora的抑制剂，用于治疗诸如糖尿病，癌症和阿尔茨海默病的疾病。

公开(公告)号：US07087642B2

公开(公告)日：2006-08-08

申请号：US10287405

申请日：2002-11-04

申请人： Dean Stamos ,  Martin Trudeau ,  Scott Bethiel ,  Steven Ronkin ,  Michael Badia ,  Jeffrey Saunders

发明人： Dean Stamos ,  Martin Trudeau ,  Scott Bethiel ,  Steven Ronkin ,  Michael Badia ,  Jeffrey Saunders

IPC分类号： A61K47/00 ,  A61K31/27 ,  C07C229/00 ,  C07C255/00

CPC分类号： C07C275/40 ,  C07B2200/07 ,  C07C275/42 ,  C07D263/32 ,  C07F9/653

摘要： The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

公开(公告)号：US07087603B2

公开(公告)日：2006-08-08

申请号：US10736426

申请日：2003-12-15

申请人： David Bebbington ,  Jean-Damien Charrier

发明人： David Bebbington ,  Jean-Damien Charrier

IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/4439 ,  A61P3/10

CPC分类号： C07D403/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/16 ,  C07D487/04 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D513/04

摘要： This invention describes novel pyrazole compounds of formula IV: wherein Z1 or Z2 is nitrogen, Q is —S—, —O—, —N(R4)—, —C(R6′)2—, 1,2-cyclopropanediyl, 1,2-cyclobutanediyl, or 1,3-cyclobutanediyl, and R1 is T-Ring D, wherein Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3 or L—Z—R3, or Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5–7 membered ring having 0–3 heteroatoms; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

摘要翻译： 本发明描述了式IV的新型吡唑化合物：其中Z 1或Z 2是氮，Q是-S - ， - O - ， - N（R' 4 - ， - C（R 6'）2 - ，1,2-环丙烷二基，1,2-环丁烷二基或1,3-环丁烷二基 并且R 1是T环D，其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; R＆lt; x＆gt;和＆lt; y＆gt; y＆lt; / sup＆gt;独立地选自TR 3或LZR 3，或R x， / SUP＆gt;和R＆lt; y＆gt;与它们的插入原子一起形成具有0-3个杂原子的稠合的，不饱和的或部分不饱和的5-7元环; 和R 2和R 2'如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为Aurora-2和GSK-3的抑制剂用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病。