公开(公告)号：WO2003105850A1

公开(公告)日：2003-12-24

申请号：PCT/US2003/018959

申请日：2003-06-17

Applicant: ABBOTT LABORATORIES

Inventor： COLLINS, Christine, A. ,  GAO, Ju ,  KYM, Philip, R. ,  LEWIS, Jared, C. ,  SOUERS, Andrew, J. ,  VASUDEVAN, Anil ,  WODKA, Dariusz

IPC: A61K31/47

CPC classification number: C07D215/38 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D411/12 ,  C07D413/12

Abstract: The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, which antagonize the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor and are useful for the prevention or treatment of eating disorders, weight gain and obesity.

Abstract translation: 本发明涉及通过黑色素浓缩激素受体拮抗黑色素浓缩激素（MCH）的作用的式（I）化合物或其治疗上合适的盐或前药，并且可用于预防或治疗饮食 疾病，体重增加和肥胖。

公开(公告)号：WO2010017150A1

公开(公告)日：2010-02-11

申请号：PCT/US2009/052617

申请日：2009-08-03

Applicant: ABBOTT LABORATORIES ,  VASUDEVAN, Anil ,  BROWN, Brian, S. ,  KEDDY, Ryan, G. ,  HOBSON, Adrian, D.

Inventor： VASUDEVAN, Anil ,  BROWN, Brian, S. ,  KEDDY, Ryan, G. ,  HOBSON, Adrian, D.

IPC: A61K31/454 ,  A61P9/00

CPC classification number: A61K31/437 ,  C07D471/04

Abstract: Disclosed herein are compounds of formula (I) or pharmaceutical acceptable salts thereof, wherein A, X 1 , X 2 , R 1 , R 2 , R 3 , m, n, and p are defined in the specification. Compositions including the compounds which can be useful for inhibiting Rho kinase (ROCK) and methods for using the compositions are also described.

Abstract translation: 本文公开了式（I）化合物或其药学上可接受的盐，其中A，X 1，X 2，R 1，R 2，R 3，m，n和p在本说明书中定义。 还描述了包括可用于抑制Rho激酶（ROCK）的化合物的组合物和使用该组合物的方法。

公开(公告)号：WO2009055749A1

公开(公告)日：2009-04-30

申请号：PCT/US2008/081229

申请日：2008-10-25

Applicant: ABBOTT LABORATORIES ,  PERNER, Richard J. ,  KOENIG, John R. ,  DIDOMENICO, Stanley, Jr. ,  BAYBURT, Erol, K. ,  DAANEN, Jerome, F. ,  GOMTSYAN, Arthur, R. ,  KORT, Michael E. ,  KYM, Philip R. ,  VASUDEVAN, Anil ,  SCHMIDT, Robert, G. ,  VOIGHT, Eric

Inventor： PERNER, Richard J. ,  KOENIG, John R. ,  DIDOMENICO, Stanley, Jr. ,  BAYBURT, Erol, K. ,  DAANEN, Jerome, F. ,  GOMTSYAN, Arthur, R. ,  KORT, Michael E. ,  KYM, Philip R. ,  VASUDEVAN, Anil ,  SCHMIDT, Robert, G. ,  VOIGHT, Eric

IPC: C07D263/48 ,  C07D413/04 ,  C07D413/12 ,  A61K31/421 ,  A61P29/00

CPC classification number: C07D413/12 ,  C07D263/48 ,  C07D413/04

Abstract: Compounds of formula (I) wherein R 1 , R 2 , R 4 , and W are defined in the description are TRPV1 antagonists with CNS penetration. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

Abstract translation: 在描述中定义R1，R2，R4和W的式（I）化合物是具有CNS穿透的TRPV1拮抗剂。 还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。

公开(公告)号：WO2009023539A2

公开(公告)日：2009-02-19

申请号：PCT/US2008/072560

申请日：2008-08-08

Applicant: ABBOTT LABORATORIES ,  KYM, Philip R ,  BROWN, Brian S ,  DAANEN, Jerome F ,  GOMTSYAN, Arthur R ,  KEDDY, Ryan G ,  KORT, Michael ,  MATULENKO, Mark A ,  VASUDEVAN, Anil

Inventor： KYM, Philip R ,  BROWN, Brian S ,  DAANEN, Jerome F ,  GOMTSYAN, Arthur R ,  KEDDY, Ryan G ,  KORT, Michael ,  MATULENKO, Mark A ,  VASUDEVAN, Anil

IPC: C07D401/04 ,  A61K31/4545

CPC classification number: C07D401/04

Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, and R3, are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，前药，前药盐或其组合，其中R1，R2和R3在本说明书中定义。 还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。

公开(公告)号：WO2007140233A1

公开(公告)日：2007-12-06

申请号：PCT/US2007/069630

申请日：2007-05-24

Applicant: ABBOTT LABORATORIES ,  DIEBOLD, Robert B. ,  DJURIC, Stevan W. ,  GIRANDA, Vincent L ,  HEXAMER, Laura ,  LIN, Nan-horng ,  MIYASHIRO, Julie M. ,  PENNING, Thomas D. ,  PRZYTULINSKA, Magdalena ,  SOWIN, Thomas ,  SULLIVAN, Gerard ,  TAO, Zhi-fu ,  TONG, Yunsong ,  VASUDEVAN, Anil ,  WANG, Le ,  WOODS, Keith W. ,  XIA, Zhiren ,  ZHANG, Henry Q.

Inventor： DIEBOLD, Robert B. ,  DJURIC, Stevan W. ,  GIRANDA, Vincent L ,  HEXAMER, Laura ,  LIN, Nan-horng ,  MIYASHIRO, Julie M. ,  PENNING, Thomas D. ,  PRZYTULINSKA, Magdalena ,  SOWIN, Thomas ,  SULLIVAN, Gerard ,  TAO, Zhi-fu ,  TONG, Yunsong ,  VASUDEVAN, Anil ,  WANG, Le ,  WOODS, Keith W. ,  XIA, Zhiren ,  ZHANG, Henry Q.

IPC: C07C225/20 ,  C07D249/14 ,  C07D277/64 ,  C07D285/06 ,  C07D333/20 ,  A61P35/00 ,  A61K31/132 ,  A61K31/505

CPC classification number: C07D249/14 ,  C07C225/20 ,  C07C2601/02 ,  C07C2601/04 ,  C07D277/64 ,  C07D285/06 ,  C07D333/20

Abstract: Compounds that inhibit Plk1, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.

Abstract translation: 公开了抑制Plk1的化合物，含有该化合物的组合物和使用该化合物治疗疾病的方法。

公开(公告)号：WO2003086398A1

公开(公告)日：2003-10-23

申请号：PCT/US2003/011066

申请日：2003-04-03

Applicant: ABBOTT LABORATORIES

Inventor： HAVIV, Fortuna ,  BRADLEY, Michael, F. ,  HENKIN, Jack ,  DINGES, Jürgen ,  SAUER, Daryl, R. ,  KOLACZKOWSKI, Lawrence ,  VASUDEVAN, Anil ,  PARK, David, C.

IPC: A61K31/455

CPC classification number: C07D213/81 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/4747 ,  A61K31/496 ,  A61K31/541 ,  A61K31/551 ,  C07D213/82 ,  C07D239/28 ,  C07D241/24 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D491/10

Abstract: Compounds having the formula (I) are angiogenesis inhibitors. Also disclosed are compositions containing the compounds, methods of making the compounds, and methods of treatment using the compounds. A is selected from the group consisting of pyridine, pyridine N-oxide, pyridazine, pyrimidine. pyrazine, and triazine; R 1 and R 2 , together with the nitrogen atom to which they are attached, form a five - to eight - membered ring containing an additional zero to two heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur; wherein the ring can be optionally substituted with one, two, or three substituents independently selected from the group consisting of alkoxyalkyl, alkoxycarbonyl, alkyl, unsubstituted alkylcarbonyl, amino, aminocarbonyl, aryl, arylalkoxycarbonyl, wylalkyl, carboxy, formyl, haloalkyl, heterocycle, (heterocycle)alkyl, hydroxy, hydroxyalkoxyalkyl, hydroxyalkyl, and spiroheterocycle; R 3 at each occurance is independently selected from the group consisting 'of alkenyl, alkoxy, alkoxyalkyl, alkoxycarbonyl, alkyl, unsubstituted alkylcarbonyl, alkylsulfanyl, amino, aminocarbonyl, aryl, arylalkyl, aryloxy, cyano, cyanoalkyl, cyanoalkyl, (cycloalkyl)alkyl, halo, haloalkyl, heterocycle, hydroxy, hydroxyalkyl, and nitro; X is selected from the group consisting of O, S, and CH 2 ; and m is 0-4.

Abstract translation: 具有式（I）的化合物是血管发生抑制剂。 还公开了含有化合物的组合物，制备化合物的方法和使用该化合物的治疗方法。 A选自吡啶，吡啶N-氧化物，哒嗪，嘧啶。 吡嗪和三嗪; R 1和R 2与它们所连接的氮原子一起形成含有另外的0至2个选自氮，氧和硫的杂原子的五元至八元环; 其中所述环可以任选被一个，两个或三个独立地选自烷氧基烷基，烷氧基羰基，烷基，未取代的烷基羰基，氨基，氨基羰基，芳基，芳基烷氧基羰基，二烷基，羧基，甲酰基，卤代烷基，杂环，（ 杂环）烷基，羟基，羟基烷氧基烷基，羟烷基和螺杂环; R 3各自独立地选自：烯基，烷氧基，烷氧基烷基，烷氧基羰基，烷基，未取代的烷基羰基，烷基硫烷基，氨基，氨基羰基，芳基，芳烷基，芳氧基，氰基，氰基烷基，氰基烷基，（环烷基） 烷基，卤素，卤代烷基，杂环，羟基，羟基烷基和硝基; X选自O，S和CH 2; m为0-4。

公开(公告)号：WO2012097478A1

公开(公告)日：2012-07-26

申请号：PCT/CN2011/000109

申请日：2011-01-21

Applicant: ABBOTT LABORATORIES ,  VASUDEVAN, Anil ,  PENNING, Thomas ,  CHEN, Huanming ,  LIANG, Bo ,  WANG, Shaohui ,  WU, Fengchun ,  SHEN, Yan ,  LIU, Cuihua ,  ZOU, Zhenguang

Inventor： VASUDEVAN, Anil ,  PENNING, Thomas ,  CHEN, Huanming ,  LIANG, Bo ,  WANG, Shaohui ,  WU, Fengchun ,  SHEN, Yan ,  LIU, Cuihua ,  ZOU, Zhenguang

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D519/00 ,  A61K31/4353 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X 1 , X 2 , X 3 , X 4 , R 1 , R 2 , R 3 , A, B, Z, n, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中X 1，X 2，X 3，X 4，R 1，R 2，R 3，A，B，Z，n和m在说明书中定义。 本发明还涉及含有可用于抑制ALK等激酶的化合物的组合物和治疗诸如癌症的疾病的方法。

公开(公告)号：WO2004033419A1

公开(公告)日：2004-04-22

申请号：PCT/US2003/031671

申请日：2003-10-06

Applicant: ABBOTT LABORATORIES

Inventor： COMESS, Kenneth, M. ,  ERICKSON, Scott, A. ,  HENKIN, Jack ,  KALVIN, Douglas, M. ,  KAWAI, Megumi ,  KIM, Ki, H. ,  BAMAUNG, Nwe, Y. ,  PARK, Chan, Hoon ,  SHEPPARD, George, S. ,  VASUDEVAN, Anil ,  WANG, Jieyi ,  BARNES, David, M. ,  FIDANZE, Steve, D. ,  KOLACZKOWSI, Lawrence ,  MANTEI, Robert, A. ,  PARK, David, C. ,  SANDERS, William, J. ,  TEDROW, Jason, S. ,  WANG, Gary, T.

IPC: C07C311/08

CPC classification number: C07C323/25 ,  C07C311/08 ,  C07C311/13 ,  C07C311/21 ,  C07C311/29 ,  C07C311/37 ,  C07C311/44 ,  C07C311/46 ,  C07C317/28 ,  C07C323/49 ,  C07C323/63 ,  C07C323/67 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12 ,  C07D209/08 ,  C07D209/42 ,  C07D213/70 ,  C07D213/71 ,  C07D215/36 ,  C07D215/48 ,  C07D231/18 ,  C07D233/54 ,  C07D233/84 ,  C07D261/10 ,  C07D285/06 ,  C07D285/14 ,  C07D333/34 ,  C07D333/38 ,  C07D413/04

Abstract: Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.

Abstract translation: 描述了具有甲硫氨酸氨基肽酶-2抑制剂（MetAP2）的化合物。 还描述了包含该化合物的药物组合物，使用该化合物的治疗方法，抑制血管生成的方法和治疗癌症的方法。

公开(公告)号：WO2012100135A1

公开(公告)日：2012-07-26

申请号：PCT/US2012/021985

申请日：2012-01-20

Applicant: ABBOTT LABORATORIES ,  VASUDEVAN, Anil ,  PENNING, Thomas D. ,  PLIUSCHEV, Marina

Inventor： VASUDEVAN, Anil ,  PENNING, Thomas D. ,  PLIUSCHEV, Marina

IPC: C07D213/81 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  A61K31/444 ,  A61P35/00

CPC classification number: C07D401/12 ,  C07D213/81 ,  C07D409/12 ,  C07D413/12

Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R 1 , R 2 , R 3 , A, B, Z, n, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中R 1，R 2，R 3，A，B，Z，n和m在说明书中定义。 本发明还涉及含有可用于抑制ALK等激酶的化合物的组合物和治疗诸如癌症的疾病的方法。

公开(公告)号：WO2012048222A1

公开(公告)日：2012-04-12

申请号：PCT/US2011/055366

申请日：2011-10-07

Applicant: ABBOTT LABORATORIES ,  CALDERWOOD, David, J. ,  WILSON, Noel, S. ,  COX, Philip ,  HOEMANN, Michael, Z. ,  CLAPHAM, Bruce ,  MULLEN, Kelly, D. ,  VASUDEVAN, Anil ,  VILLAMIL, Clara I ,  LI, Bin ,  SOMAL, Gagandeep

Inventor： CALDERWOOD, David, J. ,  WILSON, Noel, S. ,  COX, Philip ,  HOEMANN, Michael, Z. ,  CLAPHAM, Bruce ,  MULLEN, Kelly, D. ,  VASUDEVAN, Anil ,  VILLAMIL, Clara I ,  LI, Bin ,  SOMAL, Gagandeep

IPC: A01N43/54 ,  C07D239/42 ,  C07D471/04

CPC classification number: C07D491/048 ,  C07D519/00

Abstract: The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.

Abstract translation: 本发明涉及式（I）的新化合物，其药学上可接受的盐，生物活性代谢物，前药，外消旋物，对映异构体，非对映异构体，溶剂合物和水合物，其中变量如本文所定义。 式（I）的化合物可用作激酶抑制剂，因此可用于治疗某些病症和疾病，特别是炎性病症和疾病以及增殖性疾病和病症，例如癌症。