公开(公告)号：WO2009126635A1

公开(公告)日：2009-10-15

申请号：PCT/US2009/039785

申请日：2009-04-07

Applicant: ABBOTT LABORATORIES ,  SWANN, Steven, L. ,  VASUDEVAN, Anil

Inventor： SWANN, Steven, L. ,  VASUDEVAN, Anil

IPC: C07D413/04 ,  C07D417/04 ,  C07D471/14 ,  C07D471/04 ,  A61K31/428 ,  A61K31/423

CPC classification number: C07D417/04 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04

Abstract: Disclosed herein are compounds of formula (I) or pharmaceutical acceptable salts thereof, (I) wherein X, R 1 , R 2 , R 3 , R 4 , L 1 , and m, are defined in the specification. Compositions comprising said compounds which can be useful for inhibiting Rho kinase (ROCK) and methods for using said 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，（I）其中X，R 1，R 2，R 3，R 4，L 1和m在本说明书中定义。 还描述了包含可用于抑制Rho激酶（ROCK）的所述化合物的组合物和使用所述组合物的方法。

公开(公告)号：WO2009089082A1

公开(公告)日：2009-07-16

申请号：PCT/US2009/030005

申请日：2009-01-02

Applicant: ABBOTT LABORATORIES ,  PERNER, Richard, J. ,  KORT, Michael, E. ,  DIDOMENICO, Stanley, Jr. ,  CHEN, Jun ,  VASUDEVAN, Anil

Inventor： PERNER, Richard, J. ,  KORT, Michael, E. ,  DIDOMENICO, Stanley, Jr. ,  CHEN, Jun ,  VASUDEVAN, Anil

IPC: A61K31/15 ,  A61K45/06 ,  A61P19/02 ,  A61P29/00 ,  A61P13/10

CPC classification number: C07C251/40 ,  A61K31/15 ,  A61K45/06 ,  C07C45/004 ,  C07C49/235 ,  C07C251/00 ,  A61K2300/00

Abstract: Compounds of formula (I), wherein R 1 , R 2 , R 3 , m, and Y are defined in the specification are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

Abstract translation: 其中R1，R2，R3，m和Y在本说明书中定义的式（I）化合物是TRPA1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：WO2008154241A1

公开(公告)日：2008-12-18

申请号：PCT/US2008/065727

申请日：2008-06-04

Applicant: ABBOTT LABORATORIES ,  AKRITOPOULOU-ZANZE, Irini ,  WAKEFIELD, Brian D ,  MACK, Helmut ,  TURNER, Sean C ,  GASIECKI, Alan F ,  GRACIAS, Vijaya J ,  SARRIS, Kathy ,  KALVIN, Douglas M ,  MICHMERHUIZEN, Melissa J ,  SHUAI, Qi ,  PATEL, Jyoti R ,  BAKKER, Margaretha ,  TEUSCH, Nicole ,  JOHNSON, Eric T ,  KOVAR, Peter J ,  DJURIC, Stevan W ,  LONG, Andrew J ,  VASUDEVAN, Anil ,  HOBSON, Adrian ,  ST. JOHN MOORE, Nigel ,  WANG, Lu ,  GEORGE, Dawn ,  LI, Biqin ,  FRANK, Kristine

Inventor： AKRITOPOULOU-ZANZE, Irini ,  WAKEFIELD, Brian D ,  MACK, Helmut ,  TURNER, Sean C ,  GASIECKI, Alan F ,  GRACIAS, Vijaya J ,  SARRIS, Kathy ,  KALVIN, Douglas M ,  MICHMERHUIZEN, Melissa J ,  SHUAI, Qi ,  PATEL, Jyoti R ,  BAKKER, Margaretha ,  TEUSCH, Nicole ,  JOHNSON, Eric T ,  KOVAR, Peter J ,  DJURIC, Stevan W ,  LONG, Andrew J ,  VASUDEVAN, Anil ,  HOBSON, Adrian ,  ST. JOHN MOORE, Nigel ,  WANG, Lu ,  GEORGE, Dawn ,  LI, Biqin ,  FRANK, Kristine

IPC: C07D403/04 ,  C07D413/04 ,  C07D417/04

CPC classification number: C07D403/04 ,  C07D413/04 ,  C07D417/04

Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R 1 , R 2 , R 3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3和m在说明书中定义。 本发明还涉及制备所述化合物的方法和含有所述化合物的组合物，其可用于抑制激酶如糖原合酶激酶3（GSK-3），Rho激酶（ROCK），Janus激酶（JAK），AKT，PAK4 ，PLK，CK2，KDR，MK2，JNK1，极光，pim1和nek2。

公开(公告)号：WO2003070244A1

公开(公告)日：2003-08-28

申请号：PCT/US2003/005510

申请日：2003-02-21

Applicant: ABBOTT LABORATORIES

Inventor： KYM, Philip, R. ,  HARTANDI, Kresna ,  GAO, Ju ,  PHELAN, Kathleen, M. ,  AKRITOPOULOU-ZANZE, Irini ,  COLLINS, Christine, A. ,  VASUDEVAN, Anil ,  VERZAL, Mary, K.

IPC: A61K31/4706

CPC classification number: C07D401/12 ,  C07D215/46 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders. The present invention is directed to the compouds of formula (I).

Abstract translation: 本发明涉及黑色素浓缩激素（MCH）通过黑色素浓缩激素受体的作用的拮抗作用，其可用于预防或治疗进食障碍，体重增加，肥胖，生殖和性行为异常，甲状腺激素 分泌，利尿和水/电解质体内平衡，感觉加工，记忆，睡眠，唤醒，焦虑，抑郁，癫痫发作，神经变性和精神疾病。 本发明涉及式（I）的化合物。

公开(公告)号：EP2021316A1

公开(公告)日：2009-02-11

申请号：EP07797725.4

申请日：2007-05-24

Applicant: ABBOTT LABORATORIES

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: 其中X1，C1和D1在本文中定义的式（I）化合物是polo样激酶的抑制剂。 式（I）化合物可用于治疗细胞增殖疾病，例如癌症。

公开(公告)号：EP1494672A1

公开(公告)日：2005-01-12

申请号：EP03719683.9

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 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/551 ,  C07D213/82 ,  C07D491/10 ,  C07D213/81 ,  C07D401/06 ,  C07D401/12 ,  C07D409/04 ,  C07D401/04 ,  C07D405/12 ,  C07D241/24 ,  C07D239/28

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; R1 and R2, 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; R3 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 CH2; and m is 0-4.

公开(公告)号：EP2249820A1

公开(公告)日：2010-11-17

申请号：EP09700426.1

申请日：2009-01-02

Applicant: Abbott Laboratories

Inventor： PERNER, Richard, J. ,  KORT, Michael, E. ,  DIDOMENICO, Stanley, Jr. ,  CHEN, Jun ,  VASUDEVAN, Anil

IPC: A61K31/15 ,  A61K45/06 ,  A61P19/02 ,  A61P29/00 ,  A61P13/10

CPC classification number: C07C251/40 ,  A61K31/15 ,  A61K45/06 ,  C07C45/004 ,  C07C49/235 ,  C07C251/00 ,  A61K2300/00

Abstract: Compounds of formula (I), wherein R1, R2, R3, m, and Y are defined in the specification are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

Abstract translation: 其中R 1，R 2，R 3，m和Y在说明书中定义的式（I）化合物是TRPA1拮抗剂。 还公开了包含此类化合物的组合物以及使用此类化合物和组合物治疗疾病和病症的方法。

公开(公告)号：EP2240450A1

公开(公告)日：2010-10-20

申请号：EP09700714.0

申请日：2009-01-02

Applicant: Abbott Laboratories

Inventor： PERNER, Richard J. ,  KORT, Michael E. ,  DIDOMENICO, Stanley, Jr. ,  CHEN, Jun ,  VASUDEVAN, Anil

IPC: C07D213/53 ,  C07D215/12 ,  C07D217/14 ,  C07D333/20 ,  A61K31/4406 ,  A61P29/00

CPC classification number: C07D333/22 ,  A61K31/381 ,  A61K31/44 ,  A61K31/47 ,  A61K31/472 ,  A61K45/06 ,  C07D213/53 ,  C07D213/61 ,  C07D213/64 ,  C07D215/12 ,  C07D217/14 ,  C07D333/20

Abstract: Compounds of formula (I) wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

公开(公告)号：EP1301480B1

公开(公告)日：2007-09-12

申请号：EP01952653.2

申请日：2001-07-11

Applicant: ABBOTT LABORATORIES

Inventor： BENNANI, Youssef, L. ,  FAGHIH, Ramin ,  DWIGHT, Wesley, J. ,  VASUDEVAN, Anil ,  CONNER, Scott, E.

IPC: C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D403/04 ,  C07D417/14 ,  A61K31/4025 ,  A61P9/10 ,  A61P25/28 ,  A61P29/00

CPC classification number: C07D401/12 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of formula (I) are useful in treating diseases or conditions prevented by or ameliorated with histamine-3 receptor ligands. Also disclosed are histamine-3 receptor ligand compositions and methods of antagonizing or agonizing histamine-3 receptors.

公开(公告)号：EP1467727A1

公开(公告)日：2004-10-20

申请号：EP03701286.1

申请日：2003-01-10

Applicant: Abbott Laboratories

Inventor： BENNANI, Youssef, L. ,  FAGHIH, Ramin ,  DWIGHT, Wesley, J. ,  VASUDEVAN, Anil ,  CONNER, Scott, E.

IPC: A61K31/40 ,  A61P9/10 ,  A61P25/28 ,  C07D207/14

CPC classification number: C07D403/04 ,  C07D207/12 ,  C07D207/14 ,  C07D207/24 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of formula I, are useful in treating diseases or conditions prevented by or ameliorated with histamine-3 receptor ligands. Also disclosed are histamine-3 receptor ligand compositions and methods of antagonizing or agonizing histamine-3 receptors.