公开(公告)号：WO2011135376A1

公开(公告)日：2011-11-03

申请号：PCT/GB2011/050851

申请日：2011-04-28

Applicant: ASTEX THERAPEUTICS LIMITED ,  SAXTY, Gordon ,  MURRAY, Christopher William ,  BERDINI, Valerio ,  BESONG, Gilbert Ebai ,  HAMLETT, Christopher Charles Frederick ,  JOHNSON, Christopher Norbert ,  WOODHEAD, Steven John ,  READER, Michael ,  REES, David Charles ,  MEVELLEC, Laurence Anne ,  ANGIBAUD, Patrick René ,  FREYNE, Eddy Jean Edgard ,  GOVAERTS, Tom Cornelis Hortense ,  WEERTS, Johan Erwin Edmond ,  PERERA, Timothy Pietro Suren ,  GILISSEN, Ronaldus Arnodus Hendrika Joseph ,  WROBLOWSKI, Berthold ,  LACRAMPE, Jean Fernand Armand ,  PAPANIKOS, Alexandra ,  QUEROLLE, Oliver Alexis Georges ,  PASQUIER, Elisabeth Thérèse Jeanne ,  PILATTE, Isabelle Noëlle Constance ,  BONNET, Pascal Ghislain André ,  EMBRECHTS, Werner Constant Johan ,  AKKARI, Rhalid ,  MEERPOEL, Lieven

Inventor： SAXTY, Gordon ,  MURRAY, Christopher William ,  BERDINI, Valerio ,  BESONG, Gilbert Ebai ,  HAMLETT, Christopher Charles Frederick ,  JOHNSON, Christopher Norbert ,  WOODHEAD, Steven John ,  READER, Michael ,  REES, David Charles ,  MEVELLEC, Laurence Anne ,  ANGIBAUD, Patrick René ,  FREYNE, Eddy Jean Edgard ,  GOVAERTS, Tom Cornelis Hortense ,  WEERTS, Johan Erwin Edmond ,  PERERA, Timothy Pietro Suren ,  GILISSEN, Ronaldus Arnodus Hendrika Joseph ,  WROBLOWSKI, Berthold ,  LACRAMPE, Jean Fernand Armand ,  PAPANIKOS, Alexandra ,  QUEROLLE, Oliver Alexis Georges ,  PASQUIER, Elisabeth Thérèse Jeanne ,  PILATTE, Isabelle Noëlle Constance ,  BONNET, Pascal Ghislain André ,  EMBRECHTS, Werner Constant Johan ,  AKKARI, Rhalid ,  MEERPOEL, Lieven

IPC: C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/08 ,  A61K31/498 ,  A61P35/00

CPC classification number: C07D403/04 ,  A61K31/498 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/08 ,  C07D491/113 ,  C07F9/6524

Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract translation: 本发明涉及新的喹喔啉衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法和所述化合物在治疗疾病中的用途。 癌症。

公开(公告)号：WO2008148849A3

公开(公告)日：2008-12-11

申请号：PCT/EP2008/057008

申请日：2008-06-05

Applicant: JANSSEN PHARMACEUTICA N.V. ,  BONGARTZ, Jean-Pierre, André, Marc ,  LINDERS, Joannes, Theodorus, Maria ,  MEERPOEL, Lieven ,  VAN LOMMEN, Guy, Rosalia, Eugeen ,  COESEMANS, Erwin ,  BRAEKEN, Mirielle ,  BUYCK, Christophe, Francis, Robert, Nestor ,  BERWAER, Monique, Jenny, Marie ,  DE WAEPENAERT, Katharina, Antonia, Germania, J.M. ,  ROEVENS, Peter, Walter, Maria ,  DAVIDENKO, Petr, Vladimirivich

Inventor： BONGARTZ, Jean-Pierre, André, Marc ,  LINDERS, Joannes, Theodorus, Maria ,  MEERPOEL, Lieven ,  VAN LOMMEN, Guy, Rosalia, Eugeen ,  COESEMANS, Erwin ,  BRAEKEN, Mirielle ,  BUYCK, Christophe, Francis, Robert, Nestor ,  BERWAER, Monique, Jenny, Marie ,  DE WAEPENAERT, Katharina, Antonia, Germania, J.M. ,  ROEVENS, Peter, Walter, Maria ,  DAVIDENKO, Petr, Vladimirivich

IPC: A61K31/451 ,  A61K31/495 ,  A61P3/06 ,  A61P9/00 ,  A61P35/00 ,  C07D295/135

Abstract: The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C(=O)-; -C(=O)-C(=O)-; -NR X -C(=O)-; -Z-C(=O)-; -Z-NR X -C(=O)-; -C(=O)-Z-; -NR X -C(=O)-Z-; -C(=S)-; -NR X -C(=S)-; -Z-C(=S)-; -Z-NR X -C(=S)-; - C(=S)-Z-; -NR X -C(=S)-Z-; Z represents a bivalent radical selected from C 1-6 alkanediyl, C 2-6 alkenediyl or C 2-6 alkynediyl; wherein each of said C 1-6 alkanediyl, C 2-6 alkenediyl or C 2-6 alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C 1-6 alkanediyl may optionally be replaced by C 1-6 alkanediyl; Y represents -C(=O)-NR X - or -NR X -C(=O)-; R 1 represents adamantanyl, C 3-6 cycloalkyl; aryl 1 or Het 1 ; R 2 represents C 3-6 cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3- dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C 3-6 Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R 7 represents hydrogen, halo, C 1-4 alkyl, C 1-4 alkyl substituted with hydroxyl; provided that the following compounds (II), (III) are excluded; a N -oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.

公开(公告)号：WO2008148849A2

公开(公告)日：2008-12-11

申请号：PCT/EP2008057008

申请日：2008-06-05

Applicant: JANSSEN PHARMACEUTICA NV ,  BONGARTZ JEAN-PIERRE ANDRE MARC ,  LINDERS JOANNES THEODORUS MARIA ,  MEERPOEL LIEVEN ,  VAN LOMMEN GUY ROSALIA EUGEEN ,  COESEMANS ERWIN ,  BRAEKEN MIRIELLE ,  BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR ,  BERWAER MONIQUE JENNY MARIE ,  DE WAEPENAERT KATHARINA ANTONIA GERMANIA J ,  ROEVENS PETER WALTER MARIA ,  DAVIDENKO PETR VLADIMIRIVICH

Inventor： BONGARTZ JEAN-PIERRE ANDRE MARC ,  LINDERS JOANNES THEODORUS MARIA ,  MEERPOEL LIEVEN ,  VAN LOMMEN GUY ROSALIA EUGEEN ,  COESEMANS ERWIN ,  BRAEKEN MIRIELLE ,  BUYCK CHRISTOPHE FRANCIS ROBERT NESTOR ,  BERWAER MONIQUE JENNY MARIE ,  DE WAEPENAERT KATHARINA ANTONIA GERMANIA J ,  ROEVENS PETER WALTER MARIA ,  DAVIDENKO PETR VLADIMIRIVICH

IPC: A61K31/451 ,  A61K31/495 ,  A61P3/06 ,  A61P9/00 ,  A61P35/00 ,  C07D295/135

CPC classification number: A61K31/4523 ,  A61K31/451 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  C07D207/277 ,  C07D207/323 ,  C07D211/26 ,  C07D211/60 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D235/18 ,  C07D249/08 ,  C07D257/04 ,  C07D263/34 ,  C07D277/56 ,  C07D279/02 ,  C07D279/12 ,  C07D295/20 ,  C07D295/205 ,  C07D295/21 ,  C07D295/215 ,  C07D307/54 ,  C07D319/18 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

Abstract: The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents -O-C(=O)-; -C(=O)-C(=O)-; -NRX-C(=O)-; -Z-C(=O)-; -Z-NRX-C(=O)-; -C(=O)-Z-; -NRX-C(=O)-Z-; -C(=S)-; -NRX-C(=S)-; -Z-C(=S)-; -Z-NRX-C(=S)-; - C(=S)-Z-; -NRX-C(=S)-Z-; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents -C(=O)-NRX- or -NRX-C(=O)-; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3- dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (II), (III) are excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.

Abstract translation: 本发明涉及式（I）的DGAT抑制剂，其包括其任何立体化学异构形式，其中A表示CH或N; 在A代表碳原子的情况下，虚线代表任意键; X表示-O-C（= O） - ; -C（= O）-C（= O） - ; -NRX-C（= O） - ; -Z-C（= O） - ; -Z-NRX-C（= O） - ; -C（= O）-Z-; -NRX-C（= O）-Z-; -C（= S） - ; -NRX-C（= S） - ; -Z-C（= S） - ; -Z-NRX-C（= S） - ; -C（= S）-Z-; -NRX-C（= S）-Z-; Z表示选自C 1-6烷二基，C 2-6亚烯基或C 2-6炔二基的二价基团; 其中所述C 1-6烷二基，C 2-6亚烯基或C 2-6炔二基中的每一个可任选被取代; 并且其中连接在C 1-6烷二基中的相同碳原子上的两个氢原子可任选地被C 1-6烷二基取代; Y表示-C（= O）-NRX-或-NRX-C（= O） - ; R1表示金刚烷基，C3-6环烷基; 芳基1或Het1; R2代表C3-6环烷基，苯基，萘基，2,3-二氢-1,4-苯并二氧杂环己烯基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或含有1或2个N原子的6元芳族杂环，其中所述C3 -6环烷基，苯基，萘基，2,3-二氢-1,4-苯并二恶英，1,3-苯并二恶唑基或杂环可以任选被取代; R 7表示氢，卤素，C 1-4烷基，被羟基取代的C 1-4烷基; 条件是排除以下化合物（II），（III）; 其N-氧化物，其药学上可接受的盐或其溶剂合物。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及作为所述化合物的DGAT抑制剂的药物用途。

公开(公告)号：WO2008049806A1

公开(公告)日：2008-05-02

申请号：PCT/EP2007/061286

申请日：2007-10-22

Applicant: JANSSEN PHARMACEUTICA NV ,  MEERPOEL, Lieven ,  LINDERS, Joannes Theodorus Maria ,  JAROSKOVA, Libuse ,  VIELLEVOYE, Marcel ,  BACKX, Leo Jacobus Jozef ,  BERTHELOT, Didier Jean-Claude ,  BUSSCHER, Guuske Frederike

Inventor： MEERPOEL, Lieven ,  LINDERS, Joannes Theodorus Maria ,  JAROSKOVA, Libuse ,  VIELLEVOYE, Marcel ,  BACKX, Leo Jacobus Jozef ,  BERTHELOT, Didier Jean-Claude ,  BUSSCHER, Guuske Frederike

IPC: C07D211/58 ,  C07D241/20 ,  C07D295/10 ,  C07D401/12 ,  C07D401/14 ,  A61K31/495 ,  A61K31/445 ,  A61P3/00

CPC classification number: C07D241/20 ,  C07D211/58 ,  C07D295/10 ,  C07D401/12 ,  C07D401/14

Abstract: The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.

Abstract translation: 本发明涉及具有apoB分泌/ MTP抑制活性和伴随的降脂活性的新型哌啶或哌嗪取代的四氢 - 萘-1-羧酸衍生物。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗动脉粥样硬化，胰腺炎，肥胖症，高甘油三酯血症，高胆固醇血症，高脂血症，糖尿病和II型糖尿病的药物的用途。

公开(公告)号：WO0220501A3

公开(公告)日：2002-06-27

申请号：PCT/EP0109926

申请日：2001-08-27

Applicant: JANSSEN PHARMACEUTICA NV ,  MEERPOEL LIEVEN ,  ROEVENS PETER WALTER MARIA ,  BACKX LEO JACOBUS JOZEF ,  VAN DER VEKEN LOUIS JOZEF ELIS ,  VIELLEVOYE MARCEL

Inventor： MEERPOEL LIEVEN ,  ROEVENS PETER WALTER MARIA ,  BACKX LEO JACOBUS JOZEF ,  VAN DER VEKEN LOUIS JOZEF ELIS ,  VIELLEVOYE MARCEL

IPC: C07D243/08 ,  A61K31/4409 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/551 ,  A61P1/18 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P9/14 ,  C07D211/26 ,  C07D211/34 ,  C07D211/70 ,  C07D211/82 ,  C07D213/40 ,  C07D213/55 ,  C07D213/56 ,  C07D295/14 ,  C07D295/15 ,  C07D307/54 ,  C07D333/24 ,  C07D401/12

CPC classification number: C07D213/40 ,  C07D211/26 ,  C07D211/34 ,  C07D211/70 ,  C07D213/55 ,  C07D213/56 ,  C07D241/04 ,  C07D243/08 ,  C07D295/15 ,  C07D307/54 ,  C07D333/24

Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.

Abstract translation: 式（I）的聚芳基酰胺化合物可用作降脂剂。

公开(公告)号：WO2012084804A1

公开(公告)日：2012-06-28

申请号：PCT/EP2011/073215

申请日：2011-12-19

Applicant: JANSSEN PHARMACEUTICA NV ,  MEERPOEL, Lieven ,  MAES, Louis, Jules, Roger, Marie ,  DE WIT, Kelly

Inventor： MEERPOEL, Lieven ,  MAES, Louis, Jules, Roger, Marie ,  DE WIT, Kelly

IPC: C07D487/04 ,  A61K31/5517 ,  A61P31/10

CPC classification number: C07D487/04

Abstract: The present invention is concerned with novel antifungal 5,6-dihydro-4 H -pyrrolo- [1,2- a ][1,4]benzodiazepines and 6 H -pyrrolo[1,2- a ][1,4]benzodiazepines substituted with bicyclic benzene derivatives of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. 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.

Abstract translation: 本发明涉及新型抗真菌5,6-二氢-4H-吡咯并[1,2-a] [1,4]苯并二氮杂和6H-吡咯并[1,2-a] [1,4]苯并二氮杂 其中R 1，R 2，R 3，R 4，R 5，R 6和R 7具有权利要求中定义的含义的式（I）的双环苯衍生物。 根据本发明的化合物主要是抗皮肤癣菌和全身真菌感染的活性物质。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：WO2012069380A1

公开(公告)日：2012-05-31

申请号：PCT/EP2011/070458

申请日：2011-11-18

Applicant: JANSSEN PHARMACEUTICA NV ,  MEERPOEL, Lieven ,  MAES, Louis, Jules, Roger, Marie ,  DE WIT, Kelly

Inventor： MEERPOEL, Lieven ,  MAES, Louis, Jules, Roger, Marie ,  DE WIT, Kelly

IPC: C07D487/04 ,  A61K31/5517 ,  A61P31/10

CPC classification number: C07D487/04

Abstract: The present invention is concerned with novel antifungal 5,6-dihydro-4 H -pyrrolo-[1,2- a ][1,4]benzodiazepines and 6 H -pyrrolo[1,2- a ][1,4]benzodiazepines of Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. 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.

Abstract translation: 本发明涉及新型抗真菌5,6-二氢-4H-吡咯并[1,2-a] [1,4]苯并二氮杂和6H-吡咯并[1,2-a] [1,4]苯并二氮杂 （I）其中R1，R2，R3，R4，R5和R6具有权利要求中限定的含义。 根据本发明的化合物主要是抗皮肤癣菌和全身真菌感染的活性物质。 本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物以及所述化合物作为药物的用途。

公开(公告)号：WO2006136553A1

公开(公告)日：2006-12-28

申请号：PCT/EP2006/063351

申请日：2006-06-20

Applicant: JANSSEN PHARMACEUTICA N.V. ,  TEN HOLTE, Peter ,  VAN EMELEN, Kristof ,  ANGIBAUD, Patrick, René ,  MARCONNET-DECRANE, Laurence, Françoise, Bernadette ,  MEERPOEL, Lieven

Inventor： TEN HOLTE, Peter ,  VAN EMELEN, Kristof ,  ANGIBAUD, Patrick, René ,  MARCONNET-DECRANE, Laurence, Françoise, Bernadette ,  MEERPOEL, Lieven

IPC: C07D401/14 ,  C07D413/14 ,  A61K31/4166 ,  A61P35/00

CPC classification number: C07D413/14 ,  C07D401/14 ,  C07D405/14

Abstract: This invention comprises the novel compounds of Formula (I) wherein R 1 , R 2 , R 3 , X, Y and Z have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract translation: 本发明包括式（I）的新化合物，其中R 1，R 2，R 3，X，Y和Z具有定义的含义 ，具有组蛋白脱乙酰酶抑制酶活性; 其制剂，含有它们的组合物及其作为药物的用途。

公开(公告)号：WO2005085226A1

公开(公告)日：2005-09-15

申请号：PCT/EP2005/051010

申请日：2005-03-07

Applicant: JANSSEN PHARMACEUTICA N.V. ,  MEERPOEL, Lieven ,  BACKX, Leo, Jacobus, Jozef ,  JAROSKOVA, Libuse ,  ROEVENS, Peter, Walter, Maria ,  VAN DER VEKEN, Louis, Jozef, Elisabeth ,  VIELLEVOYE, Marcel ,  LINDERS, Joannes, Theodorus, Maria

Inventor： MEERPOEL, Lieven ,  BACKX, Leo, Jacobus, Jozef ,  JAROSKOVA, Libuse ,  ROEVENS, Peter, Walter, Maria ,  VAN DER VEKEN, Louis, Jozef, Elisabeth ,  VIELLEVOYE, Marcel ,  LINDERS, Joannes, Theodorus, Maria

IPC: C07D401/04

CPC classification number: C07D233/54 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

Abstract: The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes (Formula (I)). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hyper­triglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.

Abstract translation: 本发明涉及用具有apoB分泌/ MTP抑制活性和伴随的降脂活性的某些5-元杂环取代的新的芳基哌啶或哌嗪化合物。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗高脂血症，肥胖症和II型糖尿病的药物（式（I））的用途。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及所述化合物作为治疗动脉粥样硬化，胰腺炎，肥胖症，高甘油三酯血症，高胆固醇血症，高脂血症，糖尿病和II型糖尿病的药物的用途。

公开(公告)号：WO2003076421A1

公开(公告)日：2003-09-18

申请号：PCT/EP2003/002511

申请日：2003-03-11

Applicant: JANSSEN PHARMACEUTICA N.V. ,  VAN EMELEN, Kristof ,  DE WINTER, Hans, Louis, Jos ,  DYATKIN, Alexey, Borisovich ,  VERDONCK, Marc, Gustaaf, Celine ,  MEERPOEL, Lieven

Inventor： VAN EMELEN, Kristof ,  DE WINTER, Hans, Louis, Jos ,  DYATKIN, Alexey, Borisovich ,  VERDONCK, Marc, Gustaaf, Celine ,  MEERPOEL, Lieven

IPC: C07D295/20

CPC classification number: C07D413/12 ,  A61K31/40 ,  A61K31/402 ,  A61K31/435 ,  A61K31/4427 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/472 ,  A61K31/495 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D207/09 ,  C07D207/14 ,  C07D211/14 ,  C07D211/58 ,  C07D213/78 ,  C07D217/02 ,  C07D217/04 ,  C07D217/16 ,  C07D239/42 ,  C07D295/155 ,  C07D295/26 ,  C07D307/68 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D471/04 ,  C07D471/10 ,  C07D513/04 ,  C12Q1/34 ,  C12Q1/48

Abstract: This invention comprises the novel compounds of formula (I)wherein n, R 1 , R 2 , R 3 , R 4 , L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.

Abstract translation: 本发明包括具有组蛋白脱乙酰酶抑制酶活性的式（I）的新化合物，其中n，R 1，R 2，R 3，R 4，L，Q，X，Y，Z具有定义的含义; 其制剂，含有它们的组合物及其作为药物的用途。