公开(公告)号：JP2013249307A

公开(公告)日：2013-12-12

申请号：JP2013167044

申请日：2013-08-09

Applicant: Janssen Pharmaceutica Nv ,  ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap

Inventor： PAPANIKOS ALEXANDRA ,  FREYNE EDDY JEAN EDGARD ,  TEN HOLTE PETER ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHAN ,  MEVELLEC LAURENCE ANNE ,  STORCK PIERRE HENRI

IPC: C07D498/18 ,  A61K31/519 ,  A61K31/541 ,  A61P9/00 ,  A61P9/10 ,  A61P35/00 ,  A61P43/00

CPC classification number: C07D498/14 ,  C08K5/544

Abstract: PROBLEM TO BE SOLVED: To provide a certain kind of new quinazoline derivative, having an antitumor activity and useful in a treating method for a human body or an animal body.SOLUTION: A quinazoline derivative is expressed by formula (I) (wherein, Y, X, X, R, Rand Rare each optionally a halogen atom or an organic group) or its N-oxy form, pharmaceutically acceptable addition salt or stereochemically isomeric form.

Abstract translation: 要解决的问题：提供一种具有抗肿瘤活性并可用于人体或动物体的治疗方法的新型喹唑啉衍生物。解决方案：喹唑啉衍生物由式（I）表示（其中Y为 ，X，X，R，R 3各自任选是卤素原子或有机基团）或其N-氧基形式，药学上可接受的加成盐或立体化学异构形式。

公开(公告)号：WO2006061417A3

公开(公告)日：2006-08-03

申请号：PCT/EP2005056609

申请日：2005-12-08

Applicant: JANSSEN PHARMACEUTICA NV ,  FREYNE EDDY JEAN EDGARD ,  WILLEMS MARC ,  TEN HOLTE PETER ,  PAPANIKOS ALEXANDRA ,  EMBRECHTS WERNER CONSTANT JOHA ,  STORCK PIERRE HENRI ,  PONCELET VIRGINIE SOPHIE

Inventor： FREYNE EDDY JEAN EDGARD ,  WILLEMS MARC ,  TEN HOLTE PETER ,  PAPANIKOS ALEXANDRA ,  EMBRECHTS WERNER CONSTANT JOHA ,  STORCK PIERRE HENRI ,  PONCELET VIRGINIE SOPHIE

IPC: C07D498/08 ,  A61K31/529 ,  A61P35/00 ,  C07D239/00 ,  C07D273/00

CPC classification number: C07D498/06 ,  C07D498/08

Abstract: The present invention concerns kinase inhibitors formula, formula (I), the N-oxide forms, the pharmaceutically isomeric forms thereof, wherein Z represents NH and the other substituents are defined as in the claims.

Abstract translation: 本发明涉及激酶抑制剂式（I），N-氧化物形式及其药学上异构体形式，其中Z表示NH且其它取代基如权利要求中所定义。

公开(公告)号：WO2005012304A3

公开(公告)日：2007-04-26

申请号：PCT/EP2004051457

申请日：2004-07-12

Applicant: JANSSEN PHARMACEUTICA NV ,  FREYNE EDDY JEAN EDGARD ,  LOVE CHRISTOPHER JOHN ,  COOYMANS LUDWIG PAUL ,  VANDERMAESEN NELE ,  BUIJNSTERS PETER JACOBUS JOHAN ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA

Inventor： FREYNE EDDY JEAN EDGARD ,  LOVE CHRISTOPHER JOHN ,  COOYMANS LUDWIG PAUL ,  VANDERMAESEN NELE ,  BUIJNSTERS PETER JACOBUS JOHAN ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA

IPC: C07D487/04 ,  A61K31/519 ,  A61P3/10 ,  A61P25/24 ,  C07D235/00 ,  C07D249/00

CPC classification number: C07D487/04

Abstract: This invention concerns compounds of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochernically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R 1 represents hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 a]kyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonytoxy; or optionally substituted C 1-6 alkyloxyCl-6alkylcarbonyl; X 1 represents a direct bond; -(CH 2 ) n3 - or -(CH 2 ) n4 -X 1a -X 1b -; R 2 represents optionally substituted C 3-7 CYCloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatorn selected from 0, S or N; benzoxazolyl or a radical of formula (a-1); X 2 represents a direct bond; -NR 1 -NR 1 -(CH 2 ) N3 -; -0-; -0-(CH 2 ) n3 -; -C(=O)-; -C(=O)- (CH 2 ) n3 -; -C(=O)-NR 5 -(CH 2 ) n3 -; -C(=S)-; -S-; -S(=O) n1 -; -(CH 2 ) n3 -; -(CH 2 ) n4 -X 1a -X 1b -; -X 1a .-X 1b -(CH 2 ) n4 -; -S(=O) n1 -NR 5 -(CH 2 ) n3 -NR 5 _ or -S(=O) n1 ,-NR 5 -(CH 2 ) n3 -; R 3 represents an optionally substituted 5-or 6-membered monocyclic heterocycle containing at least one heteroatom selected from 0, S or N, or a 9-or 10-membered bicyclic heterocycle containing at least one heteroatom selected from 0, S or N; R 4 represents hydrogen; halo; hydroxy; optionally substituted C 1-4 alkyl; optionally substituted C 2-4 alkenyl or C 2-4 alkynyl; polyhaloC 1-3 alkyl; optionally substituted C 1-4 alkyloxy; polyhaloC 1-3 alkyloxy; C 1-4 alkylthio; polyhaloC 1-3 alkylthio; C 1-4 alkyloxycarbonyl; C 1-4 alkylcarbonyloxy; C 1-4 alkylcarbonyl; polyhaloC 1-4 alkylcarbonyl; nitro; cyano; carboxyl; NR 9 R 10 ; C(=O)NR 9 R 10 ;-NR 5_ C(=O)-NR 9 R 10 ; -NR 5 -C(=O)-R 5 ; -S(=O) n1 ,-R 11 -NR 5 -S(=O) n1 ,-R 11 -S-CN; -NR 5 -CN; their use, pharmaceutical compositions comprising them and processes for their preparation.

Abstract translation: 本发明涉及式（I）的化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体异构体形式，其中环A表示苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; R 1表示氢; 芳基; 甲酰基; C 1-6烷基羰基; C 1-6 a] kyl; C 1-6烷氧基羰基; 被甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基取代的C 1-6烷基， / SUB> alkylcarbonytoxy; 或任选取代的C 1-6烷氧基C 1-6烷基羰基; X 1表示直接键; - （CH 2 2）n3 - 或 - （CH 2）n4 - - - - - SUB> -X _{图1b - ; R 2表示任选取代的C 3-7环烷基; 苯基; 含有至少一个选自0，S或N的杂化子的4,5,6-或7-元单环杂环; 苯并恶唑基或式（a-1）基团; X 2代表直接键; -NR 1 - （CH 2）N 3 - ;（CH 2）N 3 - 。 -0-; -O-（CH 2 ） N3 - ; -C（= O） - ; -C（= O） - （CH 2）n3 - ; -C（= O）-NR ^{5 - （CH 2 ） N3 - ; -C（= S） - ; -S-; -S（= O） N1 - ; - （CH 2 ） N3 - ; - （CH 2 ） N4 -X 1A -X 图1b - ; -X 1A .- X 图1b - （CH 2 ） N4 - ; -S（= O） N1 -NR 5 - （CH 2 ） N3 -NR 5 n =（CH 2）n或-S（= O）n1， - NR 5 - （CH 2）n 3 - ; R 3表示含有至少一个选自O，S或N的杂原子或含有至少一个杂原子的9元或10元双环杂环的任选取代的5元或6元单环杂环 从0，S或N; R 4表示氢; 光环; 羟基; 任选取代的C 1-4烷基; 任选取代的C 2-4 - 烯基或C 2-4 - 炔基; 多卤代 1-3 烷基; 任选取代的C 1-4烷氧基; 多卤代 1-3 烷氧基; ç 1-4 烷硫基; 多卤代 1-3 烷硫基; ç 1-4 烷氧基羰基; ç 1-4 烷基羰基氧基; ç 1-4 烷基羰基; 多卤代 1-4 烷基羰基; 硝基; 氰基; 羧基; NR 9 - [R 10 ; C（= O）NR 9 - [R 10 ; - NR 5 _ C（= O）-NR 9 ř 10 ; -NR 5 C（= O）-R 5 ; -S（= O）n1， - R 11 -NR 5 -S（= O）n1， -R 11 -S-CN; -NR 5 -CN; 其用途，包含它们的药物组合物及其制备方法。}}

公开(公告)号：WO03037891A8

公开(公告)日：2003-09-04

申请号：PCT/EP0212077

申请日：2002-10-29

Applicant: JANSSEN PHARMACEUTICA NV ,  FREYNE EDDY JEAN EDGARD ,  BUIJNSTERS PETER JACOBUS JOHAN ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA ,  LOVE CHRISTOPHER JOHN ,  JANSSEN PAUL ADRIAAN JAN ,  LEWI PAULUS JOANNES ,  HEERES JAN ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  VINKERS HENDRIK MAARTEN ,  VAN AKEN KOEN JEANNE ALFONS ,  DIELS GASTON STANISLAS MARCELL

Inventor： FREYNE EDDY JEAN EDGARD ,  BUIJNSTERS PETER JACOBUS JOHAN ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA ,  LOVE CHRISTOPHER JOHN ,  JANSSEN PAUL ADRIAAN JAN ,  LEWI PAULUS JOANNES ,  HEERES JAN ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  VINKERS HENDRIK MAARTEN ,  VAN AKEN KOEN JEANNE ALFONS ,  DIELS GASTON STANISLAS MARCELL

IPC: A61K31/435 ,  A61K31/4406 ,  A61K31/50 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61P3/10 ,  A61P17/00 ,  A61P21/04 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P31/18 ,  A61P35/00 ,  A61P35/02 ,  C07D213/53 ,  C07D213/74 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

CPC classification number: C07D213/74 ,  C07D239/42 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

Abstract: This invention concerns a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxy C1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C1-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C1-6alkyl; R21-O-; R21-S-; R21-C(=0)-; R21-S(=0)p-; R7-S =O R7-S(=O)p-NH-; R21-S(=O)p-NH-; R7-C(=0)-; -NHC(=0)H; -C(=O)NHNH2; R7-C(=O)-NH-; R21-C(=O)-NH-; -C(=NH)R7; -C(=NH)R21; R° is an optionally substituted heterocycle provided that -X-R2 and/or R3 is other than hydrogen;their use, pharmaceutical compositions comprising them and processes for their preparation.

Abstract translation: 本发明涉及式（I）化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中环A为6-元杂环; R1是氢; 芳基; 甲酰基; C1-6烷基; 任选取代的C 1-6烷基; C1-6alkyloxycarbonyl; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是直接键或连接原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 1-6烯基或C 2-6炔基; C1-6烷; C 1-6烷; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; 羧基; 氰基; 硝基; 氨基; 单或二（C 1-6烷基）氨基; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C 1-6烷基; R21-O-; R21-S-; R21-C（= O） - ; R21-S（= O）p - ; R7-S = O R7-S（= O）p-NH-; R21-S（= O）P-NH-; R7-C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; R7-C（= O）-NH-; R21-C（= O）-NH-; -C（= NH）R 7; -C（= NH）R 21; R°是任选取代的杂环，条件是-X-R 2和/或R 3不是氢;它们的用途，包含它们的药物组合物及其制备方法。

公开(公告)号：WO2008006884A3

公开(公告)日：2008-03-06

申请号：PCT/EP2007057200

申请日：2007-07-12

Applicant: JANSSEN PHARMACEUTICA NV ,  PAPANIKOS ALEXANDRA ,  FREYNE EDDY JEAN EDGARD ,  TEN HOLTE PETER ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA ,  MEVELLEC LAURENCE ANNE ,  STORCK PIERRE HENRI

Inventor： PAPANIKOS ALEXANDRA ,  FREYNE EDDY JEAN EDGARD ,  TEN HOLTE PETER ,  WILLEMS MARC ,  EMBRECHTS WERNER CONSTANT JOHA ,  MEVELLEC LAURENCE ANNE ,  STORCK PIERRE HENRI

IPC: C07D498/14 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D498/14 ,  C08K5/544

Abstract: The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y represents -C 3-9 alkyl-, -C 1-5 alkyl-NR 6 -C 1-5 alkyl- or -C 1-5 alkyl-NR 7 -CO-C 1-5 alkyl-; X 1 represents -O-; X 2 represents NR 5 -C 1-2 alkyl-; R 1 represents hydrogen, halo or Het 3 -O-; R 2 represents hydrogen; R 3 represents hydroxy, C 1-4 alkyloxy- or C 1-4 alkyloxy subst ituted with one or two substituents each independently selected from Het 4 , hydroxy, C 1-4 alkyloxy-, C 1-4 alkyloxy-C 1-4 alkyloxy and NR 9 R 10 ; R 5 represents hydrogen or C 1-4 alkyl; R 6 represents hydrogen or C 1-4 alkyl; R 7 represents hydrogen; R 9 and R 10 each independently represent hydrogen; C 1-4 alkyl-S(=O) 2 -C 1-4 alkyl-C(=O)-; C 1-4 alkyl or C 1-4 alkyl substituted with hydroxy; Het 3 represents pyridinyl optionally substituted with C 1-4 alkyl; Het 4 represents morpholinyl, piperidinyl or piperazinyl wherein said Het 4 is optionally substituted with hydroxy-C 1-4 alkyl or C 1-4 alkyl-S(=O) 2 -C 1-4 alkyl-.

Abstract translation: 本发明涉及式（I）化合物的N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中Y代表-C 3-9 - 烷基 - ， - 烷基-C 1-6烷基-C 1-6烷基-C 1-6烷基-C 1-6烷基-C 1-6烷基-C 1-6烷基-C ^{7 -CO-C _{1-5 烷基 - ; X 1表示-O-; X 2表示NR 5 -C 12烷基 - ; R 1表示氢，卤素或Het 3 -O-; R 2表示氢; R 3表示羟基，C 1-4烷基氧基或C 1-4烷氧基，其被一个或两个独立地选自Het的取代基取代 羟基，C 1-4烷氧基 - ，C 1-4烷基氧基-C 1-4烷氧基（C 1 -C 4）烷基氧基 和NR 9 R 10; R 5表示氢或C 1-4烷基; R 6表示氢或C 1-4烷基; R 7表示氢; R 9和R 10各自独立地表示氢; ç 1-4 烷基-S（= O） 2 -C 1-4 烷基-C（= O） - ; C 1-4烷基或被羟基取代的C 1-4烷基; Het 3表示任选被C 1-4烷基取代的吡啶基; Het 4表示吗啉基，哌啶基或哌嗪基，其中所述Het 4任选被羟基-C 1-4烷基或C 1〜 -4 烷基-S（= O） 2 -C 1-4 烷基 - 。}}

公开(公告)号：EP3126365B1

公开(公告)日：2018-01-10

申请号：EP15713523

申请日：2015-04-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： DIELS GASTON STANISLAS MARCELLA ,  SCHOENTJES BRUNO ,  VERSELE MATTHIAS LUC AIMÉ ,  BERTHELOT DIDIER JEAN-CLAUDE ,  WILLEMS MARC ,  VIELLEVOYE MARCEL ,  SOMMEN FRANÇOIS MARIA ,  WROBLOWSKI BERTHOLD ,  MEERPOEL LIEVEN

IPC: C07D471/22 ,  A61K31/505 ,  A61P35/00 ,  C07D498/22

CPC classification number: C07D471/22 ,  C07D491/22 ,  C07D498/22 ,  C07D513/22 ,  Y02P20/582

Abstract: wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

公开(公告)号：AU2015239098B2

公开(公告)日：2019-08-01

申请号：AU2015239098

申请日：2015-04-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： MEERPOEL LIEVEN ,  DIELS GASTON STANISLAS MARCELLA ,  SCHOENTJES BRUNO ,  VERSELE MATTHIAS LUC AIME ,  BERTHELOT DIDIER JEAN-CLAUDE ,  WILLEMS MARC ,  VIELLEVOYE MARCEL ,  EMBRECHTS WERNER CONSTANT JOHAN ,  WROBLOWSKI BERTHOLD

IPC: C07D471/22 ,  A61K31/505 ,  A61P35/00 ,  C07D498/22

Abstract: The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

公开(公告)号：AU2015239100B2

公开(公告)日：2019-06-27

申请号：AU2015239100

申请日：2015-04-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： DIELS GASTON STANISLAS MARCELLA ,  SCHOENTJES BRUNO ,  VERSELE MATTHIAS LUC AIME ,  BERTHELOT DIDIER JEAN-CLAUDE ,  WILLEMS MARC ,  VIELLEVOYE MARCEL ,  SOMMEN FRANCOIS MARIA ,  WROBLOWSKI BERTHOLD ,  MEERPOEL LIEVEN

IPC: C07D471/22 ,  A61K31/505 ,  A61P35/00 ,  C07D498/22

Abstract: The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

公开(公告)号：EA029758B1

公开(公告)日：2018-05-31

申请号：EA201692000

申请日：2015-04-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： DIELS GASTON STANISLAS MARCELLA ,  SCHOENTJES BRUNO ,  VERSELE MATTHIAS LUC AIME ,  BERTHELOT DIDIER JEAN-CLAUDE ,  WILLEMS MARC ,  VIELLEVOYE MARCEL ,  SOMMEN FRANCOIS MARIA ,  WROBLOWSKI BERTHOLD ,  MEERPOEL LIEVEN

IPC: C07D471/22 ,  A61K31/505 ,  A61P35/00 ,  C07D498/22

Abstract: Изобретениеотноситсяк замещенныммакроциклическимпроизводнымпиримидинаформулы (I)гдепеременныеимеютзначения, определенныев формулеизобретения. Соединенияв соответствиис изобретениемобладают EF2K-ингибирующейактивностьюи необязательнотакже Vps34-ингибирующейактивностью. Изобретение, крометого, относитсяк способамполучениятакихновыхсоединений, кфармацевтическимкомпозициям, содержащимуказанныесоединенияв качествеактивногоингредиента, атакжек применениюуказанныхсоединенийв качествелекарственногопрепарата.

公开(公告)号：PE20161365A1

公开(公告)日：2016-12-17

申请号：PE2016001843

申请日：2015-04-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BERTHELOT DIDIER JEAN-CLAUDE ,  DIELS GASTON STANISLAS MARCELLA ,  MEERPOEL LIEVEN ,  SCHOENTJES BRUNO ,  WROBLOWSKI BERTHOLD ,  VERSELE MATTHIAS LUC AIME ,  VIELLEVOYE MARCEL ,  WILLEMS MARC ,  SOMMEN FRANÇOIS MARIA

IPC: A61K31/505 ,  A61P35/00 ,  C07D471/22 ,  C07D498/22

Abstract: Se refiere a compuestos de formula I, donde: Xa, Xb y Xc son independientemente CH o N; X1 es -(CHR12)s-NR1-Xe-alcanodiil C1-C4- (SO2)p3- o –(CH2)s-O-Xe-alcanodiil C1-C4-(SO2)p3-; Xe es –C(=O)-, entre otros; a es NR4-C(=O)-[C(R5b)2]r, NR4-C(R5b)2-C(=O)- o C(=O)- NR4-C(R5b)2; b es i), donde Xd1 es CH o N, Xd2 es CH2 o NH; el anillo A es fenilo o piridilo; R1 es hidrogeno, alquilo C1-C4, entre otros; R12 es hidrogeno o alquilo C1-C4; o R1 y R12 se unen para formar alcanodiilo C1-C4, entre otros; s es 0, 1 o 2; p3 es es 0 o 1; R3 es hidrogeno, oxo, entre otros; R4 es hidrogeno, alquilo C1-C4 o alquiloxi C1-C4-alquilo C1-C4; R5b es hidrogeno, alquilo C1-C4, entre otros; p2 y r son 0, 1 o 2; R6 es hidrogeno, halo, entre otros; n es 1 o 2. Dichos compuestos son inhibidores de EF2K y opcionalmente tienen actividad inhibidora de Vps34, siendo utiles en el tratamiento de neoplasias malignas hematologicas y de tumores solidos como glioblastoma, meduloblastoma, entre otros