公开(公告)号：US20090082329A1

公开(公告)日：2009-03-26

申请号：US12173191

申请日：2008-07-15

Applicant: Frank HALLEY ,  Youssef EL-AHMAD ,  Victor CERTAL ,  Corinne VENOT ,  Anne DAGALLIER ,  Hartmut STROBEL ,  Kurt RITTER ,  Sven RUF

Inventor： Frank HALLEY ,  Youssef EL-AHMAD ,  Victor CERTAL ,  Corinne VENOT ,  Anne DAGALLIER ,  Hartmut STROBEL ,  Kurt RITTER ,  Sven RUF

IPC: A61K31/4545 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  A61K31/506 ,  A61K31/496 ,  A61P3/00 ,  A61P37/00 ,  A61P11/00 ,  A61P35/00 ,  A61P9/00 ,  C12N9/99 ,  A61K31/5377 ,  C07D403/14 ,  C07D413/06 ,  A61K31/4439

CPC classification number: C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14

Abstract: The disclosure relates to compounds of formula (I): wherein Ra, Rb, R, and n are as defined in the disclosure, to pharmaceutical compositions comprising said compounds, and to processes for making and methods of using the same.

Abstract translation: 本公开涉及式（I）化合物：其中Ra，Rb，R和n如本公开所定义，包含所述化合物的药物组合物，及其制备方法及其使用方法。

公开(公告)号：US20120172360A1

公开(公告)日：2012-07-05

申请号：US13331199

申请日：2011-12-20

Applicant: Victor CERTAL ,  Bruno FILOCHE-ROMME ,  Frank HALLEY ,  Karl Andreas KARLSSON ,  Fabienne THOMPSON

Inventor： Victor CERTAL ,  Bruno FILOCHE-ROMME ,  Frank HALLEY ,  Karl Andreas KARLSSON ,  Fabienne THOMPSON

IPC: A61K31/5377 ,  A61P35/00 ,  A61P35/04 ,  C07D413/14

CPC classification number: C07D403/06 ,  C07D413/06

Abstract: The invention relates to the novel products of formula (I): in which Z represents —O—, —NH or Nalk; n represents 0 to 4; R1 represents Hal, hydroxyl, alkyl or alkoxy; the alkyl and alkoxy radicals being optionally substituted; R2 and R3 represent H, Hal or alkyl optionally substituted with one or more halogen atoms; R4 represents H; these products being in all the isomer forms and the salts, as medicaments, in particular as inhibitors of AKT(PKB) phosphorylation.

Abstract translation: 本发明涉及式（I）的新产物：其中Z表示-O-，-NH或Nalk; n表示0〜4; R1表示Hal，羟基，烷基或烷氧基; 烷基和烷氧基任选被取代; R2和R3表示H，Hal或任选被一个或多个卤素原子取代的烷基; R4表示H; 这些产品是所有异构体形式和盐，作为药物，特别是作为AKT（PKB）磷酸化抑制剂。

公开(公告)号：US08791255B2

公开(公告)日：2014-07-29

申请号：US13338011

申请日：2011-12-27

Applicant: Jean-Christophe Carry ,  Victor Certal ,  Frank Halley ,  Karl Andreas Karlsson ,  Laurent Schio ,  Fabienne Thompson

Inventor： Jean-Christophe Carry ,  Victor Certal ,  Frank Halley ,  Karl Andreas Karlsson ,  Laurent Schio ,  Fabienne Thompson

IPC: C07D413/04

CPC classification number: C07D239/22 ,  C07D239/47 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04

Abstract: The invention relates to the novel materials of formula (I), wherein each of the substituents R, R1, R2, R3, R4 and R5 is as defined herein. The materials are useful as inhibitors of AKT(PKB) phosphorylation.

Abstract translation: 本发明涉及式（I）的新型材料，其中取代基R 1，R 2，R 3，R 4和R 5中的每一个如本文所定义。 该物质可用作AKT（PKB）磷酸化抑制剂。

公开(公告)号：US20130274253A1

公开(公告)日：2013-10-17

申请号：US13977396

申请日：2011-12-22

Applicant: Maurice Brollo ,  Jean-Christophe Carry ,  Victor Certal ,  Eric Didier ,  Gilles Doerflinger ,  Youssef EL Ahmad ,  Bruno Filoche-Romme ,  Frank Halley ,  Karl Andreas Karlsson ,  Laurent Schio ,  Fabienne Thompson

Inventor： Maurice Brollo ,  Jean-Christophe Carry ,  Victor Certal ,  Eric Didier ,  Gilles Doerflinger ,  Youssef EL Ahmad ,  Bruno Filoche-Romme ,  Frank Halley ,  Karl Andreas Karlsson ,  Laurent Schio ,  Fabienne Thompson

IPC: C07D403/06 ,  C07D403/14

CPC classification number: C07D403/06 ,  C07D209/30 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/10

Abstract: The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.

Abstract translation: 本发明涉及衍生自嘧啶的新化合物，其制备方法，获得的新型中间体，作为药物的用途，含有其的药物组合物及其作为AKT抑制剂的治疗用途。

公开(公告)号：US20120270867A1

公开(公告)日：2012-10-25

申请号：US13338011

申请日：2011-12-27

Applicant: Jean-Christophe CARRY ,  Victor CERTAL ,  Frank HALLEY ,  Karl Andreas KARLSSON ,  Laurent SCHIO ,  Fabienne THOMPSON

Inventor： Jean-Christophe CARRY ,  Victor CERTAL ,  Frank HALLEY ,  Karl Andreas KARLSSON ,  Laurent SCHIO ,  Fabienne THOMPSON

IPC: A61K31/5377 ,  C07D471/04 ,  C07D413/14 ,  A61K31/538 ,  A61P35/00 ,  C07D413/04

CPC classification number: C07D239/22 ,  C07D239/47 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04

Abstract: The invention relates to the novel materials of formula (I), where: R1 is an optionally substituted aryl or heteroaryl; R is an H or, when formed with R1, a 5- or 6-member ring fused with an aryl or heretoaryl group optionally containing one or more of O, S, N, NH, and Nalk, being optionally substituted; R2 and R3 are, independently, an H, Hal, or alkyl optionally substituted by one or more Hal; R4 is H; and R5 is an H or alkyl optionally substituted by one or more halogen atoms. Said materials being in any isomeric form and the salts thereof, and are intended for drugs, particularly AKT(PKB) phosphorylation inhibitors.

Abstract translation: 本发明涉及式（I）的新型材料，其中：R1是任选取代的芳基或杂芳基; R是H或当与R 1形成时，与任选地含有一个或多个O，S，N，NH和Nalk的芳基或亚芳基稠合的5-或6-元环任选被取代; R2和R3独立地是H，Hal或任选被一个或多个Hal取代的烷基; R4是H; 并且R 5是任选被一个或多个卤素原子取代的H或烷基。 所述材料为异构体形式及其盐，并且用于药物，特别是AKT（PKB）磷酸化抑制剂。

公开(公告)号：US09133168B2

公开(公告)日：2015-09-15

申请号：US13977396

申请日：2011-12-22

Applicant: Maurice Brollo ,  Jean-Christophe Carry ,  Victor Certal ,  Eric Didier ,  Gilles Doerflinger ,  Youssef El Ahmad ,  Frank Halley ,  Karl Andreas Karlsson

Inventor： Maurice Brollo ,  Jean-Christophe Carry ,  Victor Certal ,  Eric Didier ,  Gilles Doerflinger ,  Youssef El Ahmad ,  Frank Halley ,  Karl Andreas Karlsson

IPC: C07D413/14 ,  C07D413/04 ,  C07D401/04 ,  C07D403/06 ,  C07D209/30 ,  C07D403/04 ,  C07D471/10 ,  C07D403/14

CPC classification number: C07D403/06 ,  C07D209/30 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/10

Abstract: The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.

Abstract translation: 本发明涉及衍生自嘧啶的新化合物，其制备方法，获得的新型中间体，作为药物的用途，含有其的药物组合物及其作为AKT抑制剂的治疗用途。

公开(公告)号：US20110166169A1

公开(公告)日：2011-07-07

申请号：US12881414

申请日：2010-09-14

Applicant: Jean-Marie RUXER ,  Victor CERTAL ,  Marcel ALASIA ,  Luc BERTIN ,  Herve MINOUX ,  Patrick MAILLIET ,  Frank HALLEY ,  Maria MENDEZ-PEREZ

Inventor： Jean-Marie RUXER ,  Victor CERTAL ,  Marcel ALASIA ,  Luc BERTIN ,  Herve MINOUX ,  Patrick MAILLIET ,  Frank HALLEY ,  Maria MENDEZ-PEREZ

IPC: A61K31/506 ,  C07D403/10 ,  C07D401/10 ,  C07D471/04 ,  C07D413/14 ,  C07D401/14 ,  A61K31/4184 ,  A61K31/4709 ,  A61K31/437 ,  A61K31/423 ,  A61K31/4439 ,  A61P25/28 ,  A61P33/06 ,  A61P33/02 ,  A61P31/10 ,  A61P21/00 ,  A61P17/06 ,  A61P25/16 ,  A61P25/00 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D451/04 ,  C07D453/00 ,  C07D471/04 ,  C07D493/08

Abstract: The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R′1; R is selected from the group comprising Formula (A′), (B), (C), (D), or (E), with R1 and/or R′1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.

Abstract translation: 本发明涉及式（I）中的新物质：其中Het是任选被一个或多个基团R 1或R 11取代的杂环; R选自式（A'），（B），（C），（D）或（E）中的R 1和/或R 1选自H，卤素，CF 3，硝基，氰基， 烷基，羟基，巯基，氨基，烷基氨基，二烷基氨基，烷氧基，苯基氧基，烷基或羧基，它们被烷基，甲酰胺，CO-NH（烷基），CON（烷基）2，NH-CO-烷基， 磺酰胺，NH-SO 2 - 烷基，S（O）2 -NH烷基或S（O 2）-N（烷基）2基团; 所有这些基团任选被取代; W1，W2和W3独立地为CH或N; X为0，S，NR2，C（O），S（O）或S（0）2; Z是任选取代的H，Hal，-O-R 2或-NH-R 2，其中R 2是H，烷基，环烷基或杂环烷基; 并且这些物质都是用作药物的异构形式及其盐。

公开(公告)号：US07935819B2

公开(公告)日：2011-05-03

申请号：US12173380

申请日：2008-07-15

Applicant: Frank Halley ,  Youssef El-Ahmad ,  Victor Certal ,  Corinne Venot ,  Anne Dagallier ,  Hartmut Strobel ,  Kurt Ritter ,  Sven Ruf

Inventor： Frank Halley ,  Youssef El-Ahmad ,  Victor Certal ,  Corinne Venot ,  Anne Dagallier ,  Hartmut Strobel ,  Kurt Ritter ,  Sven Ruf

IPC: C07D239/02

CPC classification number: C07D401/14 ,  C07D401/06 ,  C07D403/06 ,  C07D403/14

Abstract: Compounds of formula (I): wherein Ra, Rb, R, X1 and X2 are as defined in the disclosure, pharmaceutical compositions comprising said compounds, processes for making and methods of using the same are provided.

Abstract translation: 式（I）化合物：其中Ra，Rb，R，X1和X2如本公开所定义，提供包含所述化合物的药物组合物，制备方法和使用方法。

公开(公告)号：US08507483B2

公开(公告)日：2013-08-13

申请号：US13331199

申请日：2011-12-20

Applicant: Victor Certal ,  Bruno Filoche-Rommé ,  Frank Halley ,  Karl Andreas Karlsson ,  Fabienne Thompson

Inventor： Victor Certal ,  Bruno Filoche-Rommé ,  Frank Halley ,  Karl Andreas Karlsson ,  Fabienne Thompson

IPC: A61K31/535 ,  C07D413/14

CPC classification number: C07D403/06 ,  C07D413/06

Abstract: The invention relates to the novel products of formula (I): in which Z represents —O—, —NH or Nalk; n represents 0 to 4; R1 represents Hal, hydroxyl, alkyl or alkoxy; the alkyl and alkoxy radicals being optionally substituted; R2 and R3 represent H, Hal or alkyl optionally substituted with one or more halogen atoms; R4 represents H; these products being in all the isomer forms and the salts, as medicaments, in particular as inhibitors of AKT(PKB) phosphorylation.

Abstract translation: 本发明涉及式（I）的新产物：其中Z表示-O-，-NH或Nalk; n表示0〜4; R1表示Hal，羟基，烷基或烷氧基; 烷基和烷氧基任选被取代; R2和R3表示H，Hal或任选被一个或多个卤素原子取代的烷基; R4表示H; 这些产品是所有异构体形式和盐，作为药物，特别是作为AKT（PKB）磷酸化抑制剂。

公开(公告)号：US08309721B2

公开(公告)日：2012-11-13

申请号：US12881414

申请日：2010-09-14

Applicant: Jean-Marie Ruxer ,  Victor Certal ,  Marcel Alasia ,  Luc Bertin ,  Herve Minoux ,  Patrick Mailliet ,  Frank Halley ,  Maria Mendez-Perez

Inventor： Jean-Marie Ruxer ,  Victor Certal ,  Marcel Alasia ,  Luc Bertin ,  Herve Minoux ,  Patrick Mailliet ,  Frank Halley ,  Maria Mendez-Perez

IPC: C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D451/04 ,  C07D453/00 ,  C07D471/04 ,  C07D493/08

Abstract: The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R′1; R is selected from the group comprising Formula (A′), (B), (C), (D), or (E), with R1 and/or R′1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.

Abstract translation: 本发明涉及式（I）中的新物质：其中Het是任选被一个或多个基团R 1或R 11取代的杂环; R选自式（A'），（B），（C），（D）或（E）中的R 1和/或R 1选自H，卤素，CF 3，硝基，氰基， 烷基，羟基，巯基，氨基，烷基氨基，二烷基氨基，烷氧基，苯基氧基，烷基或羧基，它们被烷基，甲酰胺，CO-NH（烷基），CON（烷基）2，NH-CO-烷基， 磺酰胺，NH-SO 2 - 烷基，S（O）2 -NH烷基或S（O 2）-N（烷基）2基团; 所有这些基团任选被取代; W1，W2和W3独立地为CH或N; X为0，S，NR2，C（O），S（O）或S（0）2; Z是任选取代的H，Hal，-O-R 2或-NH-R 2，其中R 2是H，烷基，环烷基或杂环烷基; 并且这些物质都是用作药物的异构形式及其盐。