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1. 发明专利

AU2007328286B2 Inhibitors of Akt activity 未知
公开(公告)号：AU2007328286B2
公开(公告)日：2011-01-20
申请号：AU2007328286
申请日：2007-12-03
申请人： MSD KK , MERCK SHARP & DOHME
发明人： ONOZAKI YU , OGINO YOSHIO , SANDERSON PHILIP E , LAYTON MARK E , KELLY MICHAEL J , LIQUORI MICHAEL E , WANG JIABING
IPC分类号： C07D401/04 , A61K31/4353 , A61P35/00 , C07D401/06 , C07D403/04 , C07D403/06 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. Compounds disclosed herein have the following chemical structure:

2. 发明专利

CA2750051A1 INHIBITORS OF AKT ACTIVITY 未知
公开(公告)号：CA2750051A1
公开(公告)日：2010-08-05
申请号：CA2750051
申请日：2010-01-25
申请人： MERCK SHARP & DOHME , MSD KK
发明人： ARMSTRONG DONNA J , GOTO YASUHIRO , HASHIHAYATA TAKASHI , KATO TETSUYA , KELLY MICHAEL J III , LAYTON MARK E , LINDSLEY CRAIG W , OGINO YOSHIO , ONOZAKI YU , RODZINAK KEVIN J , ROSSI MICHAEL A , SANDERSON PHILIP E , WANG JIABING , YAROSCHAK MELISSA M
IPC分类号： C07D471/02
摘要： The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

3. 发明专利

AU2010208480A1 Inhibitors of Akt activity 未知
公开(公告)号：AU2010208480A1
公开(公告)日：2011-07-28
申请号：AU2010208480
申请日：2010-01-25
申请人： MSD KK , MERCK SHARP & DOHME
发明人： ARMSTRONG DONNA J , YASUHIRO GOTO , TAKASHI HASHIHAYATA , TETSUYA KATO , KELLY III MICHAEL J , LAYTON MARK E , LINDSLEY CRAIG W , YOSHIO OGINO , YU ONOZAKI , RODZINAK KEVIN J , ROSSI MICHAEL A , SANDERSON PHILIP E , JIABING WANG , YAROSCHAK MELISSA M
IPC分类号： C07D471/02
摘要： The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

4. 发明专利

AU2009255358A1 Inhibitors of Akt activity 未知
公开(公告)号：AU2009255358A1
公开(公告)日：2009-12-10
申请号：AU2009255358
申请日：2009-05-28
申请人： MSD KK , MERCK SHARP & DOHME
发明人： MITA TAKASHI , OGINO YOSHIO , LAYTON MARK E , KAWANISHI NOBUHIKO , FURUYAMA HIDETOMO , ONOZAKI YU , NAYA AKIRA , GOTO YASUHIRO , SAKAMOTO TOSHIHIRO , WANG JIABING , RODZINAK KEVIN J , SANDERSON PHILIP E
IPC分类号： A61K31/44 , A61K31/52
摘要： The compounds of Formula D are of the class of triazolo-pyrido-pyrazines which are inhibitors of AKT useful for the treatment of cancer

5. 发明公开

EP2403339A4 COMBINATION CANCER THERAPY WITH AN AKT INHIBITOR AND OTHER ANTICANCER AGENTS 有权
标题翻译： WITH A AKT抑制剂和其他ANTUMORMITTELN肿瘤联合治疗
公开(公告)号：EP2403339A4
公开(公告)日：2012-12-12
申请号：EP10749110
申请日：2010-02-23
申请人： MERCK SHARP & DOHME , MSD KK
发明人： LAYTON MARK E , HIRAI HIROSHI , KOTANI HIDEHITO
IPC分类号： A01N43/58 , A61K31/4196 , A61K31/495 , A61K31/50
CPC分类号： A61K31/495 , A61K31/4196 , A61K31/50 , A61K2300/00

6. 发明专利

AU2009255329A1 Inhibitors of Akt activity 未知
公开(公告)号：AU2009255329A1
公开(公告)日：2009-12-10
申请号：AU2009255329
申请日：2009-05-27
申请人： MSD KK , MERCK SHARP & DOHME
发明人： ROSSI MICHAEL A , SAKAMOTO TOSHIHIRO , WANG JIABING , MITA TAKASHI , GOTO YASUHIRO , OGINO YOSHIO , ONOZAKI YU , SANDERSON PHILIP E , LAYTON MARK E , KAWANISHI NOBUHIKO , FURUYAMA HIDETOMO
IPC分类号： A01N43/90
摘要： The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.

8. 发明专利

ES2527567T3 Inhibidores de la actividad de Akt 未知
公开(公告)号：ES2527567T3
公开(公告)日：2015-01-26
申请号：ES07862428
申请日：2007-12-03
申请人： MERCK SHARP & DOHME , MSD KK
发明人： KELLY MICHAEL J , LAYTON MARK E , LIQUORI MICHAEL E , OGINO YOSHIO , ONOZAKI YU , SANDERSON PHILIP E , WANG JIABING
IPC分类号： C07D401/04 , A61K31/4353 , A61P35/00 , C07D401/06 , C07D403/04 , C07D403/06 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/14
摘要： Un compuesto de acuerdo con la Fórmula A:**Fórmula** donde: E, F, G, H, I, J, K, L y M se seleccionan independientemente entre: C o N, donde cada E, F, G, H, I, J, K, L y M están opcionalmente sustituidos con R1; a es 0 o 1; b es 0 o 1; m es 0, 1 o 2; p es independientemente 0, 1,2, 3, 4 o 5; El anillo Y es cicloalquilo (C4-C7), dicho cicloalquilo se sustituye opcionalmente con uno o más sustituyentes seleccionados entre: alquilo (C1-C6), alcoxi (C1-C6), CO2H, halo, CN, OH y NH2; El anillo Z se selecciona entre: cicloalquilo (C3-C8), arilo, heteroarilo y heterociclilo; R1 se selecciona entre: H, oxo, (C>=O)aOb alquilo (C1-C)10, arilo (C>=O)aOb, (C>=O)aOb alquenilo (C2-C10), (C>=O)aOb alquinilo (C2-C10), CO2H, halo, OH, Ob perfluoroalquilo (Cr-C6), (C>=O)aNR7R8, CN, (C>=O)aOb cicloalquilo (C3-C8), S(O)mNR7R815 , SH, S(O)m-alquilo (C1-C10) y (C>=O)aOb-heterociclilo, dichos alquilo, arilo, alquenilo, alquinilo, cicloalquilo y heterociclo se sustituyen opcionalmente con uno o más sustituyentes seleccionados entre R6; R2 se selecciona independientemente entre: oxo, (C>=O)aOb alquilo (C1-C10), arilo (C>=O)aOb, (C>=O)aOb alquenilo (C2-C10), (C>=O)aOb alquinilo (C2-C10), CO2H, halo, OH, Ob perfluoroalquilo (Cr-C6), (C>=O)aNR7R8, CN, (C>=O)aOb cicloalquilo (C3-C8), SH, S(O)mNR7R8, S(O)m-alquilo (C1-C10) y (C>=O)aOb-heterociclilo, dichos alquilo, arilo, alquenilo, alquinilo, cicloalquilo y heterociclo se sustituyen opcionalmente con uno o más sustituyentes seleccionados entre R6; R6 es: (C>=O)aOb alquilo C1-C10, arilo (C>=O)aOb, alquenilo C2-C10, alquinilo C2-C10, heterociclilo (C>=O)aOb, CO2H, halo, CN, OH, perfluoroalquilo ObC1-C6, Oa(C>=O)bNR7R8, oxo, CHO, (N>=O)R7R8, S(O)mNR7R8, SH, S(O)m-alquilo (C1-C10) o (C>=O)aOb cicloalquilo C3-C8, dichos alquilo, arilo, alquenilo, alquinilo, heterociclilo y cicloalquilo opcionalmente sustituidos con uno o más sustituyentes seleccionados entre R6a; R6a se selecciona entre: (C>=O)aOb alquilo (C1-C)10, Oa perfluoroalquilo (C1-C3), alquileno (C0-C6)-S(O)mRa, SH, oxo, OH, halo, CN, alquenilo (C2-C10), alquenilo (C2-C10), cicloalquilo (C3-C6), alquilen-(C0-C6)-arilo, alquilen-(C0-C6)-heterociclilo, alquilen (C0-C6)-N(Rb)2, C(O)Ra, alquilen (C0-C6)-CO2Ra, C(O)H, y alquilen (C0-C6)-CO2H, dichos alquilo, alquenilo, alquinilo, cicloalquilo, arilo y heterociclo se sustituyen opcionalmente con hasta tres sustituyentes seleccionados entre Rb OH, alcoxi (C1-C6), halógeno, CO2H, CN, Oa(C>=O)b alquilo (C1-C6), oxo, y N(Rb)2; R7 y R8 se seleccionan independientemente entre: H, (C>=O)aOb alquilo (C1-C)10, (C>=O)aOb cicloalquilo (C3-C8), arilo (C>=O)aOb, heterociclilo (C>=O)aOb, alquenilo (C2-C10), alquenilo (C2-C10), SH, SO2Ra y (C>=O)aNRb 2, dichos alquilo, cicloalquilo, arilo, heterociclilo, alquenilo y alquinilo están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre R6a o R7 y R8 35 se pueden tomar junto al nitrógeno al cual se unen para formar un heterociclo monocíclico o bicíclico con 3-7 miembros en cada anillo y que contiene opcionalmente, además del nitrógeno, uno o dos heteroátomos adicionales seleccionados entre N, O y S, dicho heterociclo monocíclico o bicíclico sustituido opcionalmente con uno o más sustituyentes seleccionados entre R6a; Ra es alquilo (C1-C6), cicloalquilo (C3-C6), arilo o heterociclilo; y Rb es independientemente: H, alquilo (C1-C6), arilo, heterociclilo, cicloalquilo (C3-C6), (C>=O)aOb alquilo (C1-C)6 o S(O)mRa, o una sal, un estereoisómero o un tautómero farmacéuticamente aceptables del mismo.

9. 发明专利

HK1137758A1 INHIBITORS OF AKT ACTIVITY AKT 未知
公开(公告)号：HK1137758A1
公开(公告)日：2010-08-06
申请号：HK10102928
申请日：2010-03-19
申请人： MERCK SHARP & DOHME , MSD KK
发明人： KELLY MICHAEL J , LAYTON MARK E , LIQUORI MICHAEL E , OGINO YOSHIO , ONOZAKI YU , SANDERSON PHILIP E , WANG JIABING
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. Compounds disclosed herein have the following chemical structure:

10. 发明申请

WO2011156245A3 POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 审中-公开
标题翻译： MGLUR2的阳性免疫调节剂
公开(公告)号：WO2011156245A3
公开(公告)日：2012-04-19
申请号：PCT/US2011039205
申请日：2011-06-06
申请人： MERCK SHARP & DOHME , ARRINGTON KENNETH L , DUDKIN VADIM , LAYTON MARK E , PERO JOSEPH E , REIF ALEXANDER J
发明人： ARRINGTON KENNETH L , DUDKIN VADIM , LAYTON MARK E , PERO JOSEPH E , REIF ALEXANDER J
IPC分类号： A01N43/50 , A61K31/415
CPC分类号： C07D471/04 , C07D519/00 , C07F7/10
摘要： The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
摘要翻译：本发明涉及作为mGluR2受体的正变构调节剂的5-取代的1,3-二氢-2H-咪唑并[4,5-b]吡啶-2-酮衍生物，其可用于治疗或预防神经和与谷氨酸功能障碍相关的精神疾病和涉及mGluR2受体的疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病如精神分裂症中的用途。

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