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1. 发明申请

WO2008049808A1 MTP INHIBITING TETRAHYDRO-NAPHTHALENE-1-CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译： MTP抑制四氢萘-1-羧酸衍生物
公开(公告)号：WO2008049808A1
公开(公告)日：2008-05-02
申请号：PCT/EP2007/061289
申请日：2007-10-22
申请人： JANSSEN PHARMACEUTICA NV , MEERPOEL, Lieven , BACKX, Leo Jacobus Jozef , TEN HOLTE, Peter , BUSSCHER, Guuske Frederike
发明人： MEERPOEL, Lieven , BACKX, Leo Jacobus Jozef , TEN HOLTE, Peter , BUSSCHER, Guuske Frederike
IPC分类号： C07C235/52 , C07C235/54 , C07C233/57 , C07C231/02 , C07C231/16 , C07C233/78 , C07C235/60 , C07D207/14 , C07D223/12 , C07D265/30 , A61K31/216 , A61K31/4025 , A61K31/40 , A61K31/5377 , A61K31/55
CPC分类号： C07C235/60 , C07C233/78 , C07C2602/10 , C07D207/14 , C07D213/82 , C07D223/12 , C07D265/30 , C07D401/12 , C07D413/12
摘要： The present invention is concerned with novel 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. Formula (I).
摘要翻译：本发明涉及具有apoB分泌/ MTP抑制活性和伴随降脂活性的新型四氢萘-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。式（I）。

2. 发明申请

WO2008049806A1 PIPERIDINE OR PIPERAZINE SUBSTITUTED TETRAHYDRO-NAPHTHALENE-1-CARBOXYLIC ACID MTP INHIBITING COMPOUNDS 审中-公开
标题翻译：哌啶或哌啶取代的四氢萘-1-羧酸的MTP抑制化合物
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
申请人： JANSSEN PHARMACEUTICA NV , MEERPOEL, Lieven , LINDERS, Joannes Theodorus Maria , JAROSKOVA, Libuse , VIELLEVOYE, Marcel , BACKX, Leo Jacobus Jozef , BERTHELOT, Didier Jean-Claude , BUSSCHER, Guuske Frederike
发明人： MEERPOEL, Lieven , LINDERS, Joannes Theodorus Maria , JAROSKOVA, Libuse , VIELLEVOYE, Marcel , BACKX, Leo Jacobus Jozef , BERTHELOT, Didier Jean-Claude , BUSSCHER, Guuske Frederike
IPC分类号： C07D211/58 , C07D241/20 , C07D295/10 , C07D401/12 , C07D401/14 , A61K31/495 , A61K31/445 , A61P3/00
CPC分类号： C07D241/20 , C07D211/58 , C07D295/10 , C07D401/12 , C07D401/14
摘要： 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.
摘要翻译：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。

3. 发明申请

WO2005085226A1 MTP INHIBITING ARYL PIPERIDINES OR PIPERAZINES SUBSTITUTED WITH 5-MEMBERED HETEROCYCLES 审中-公开
标题翻译： MTP抑制由5个成员的杂环取代的芳基哌嗪或哌嗪
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
申请人： 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
发明人： 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分类号： C07D401/04
CPC分类号： C07D233/54 , C07D249/08 , C07D401/04 , C07D401/14 , C07D403/10 , C07D413/12 , C07D417/10 , C07D417/12
摘要： 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.
摘要翻译：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。

4. 发明申请

WO2007014941A2 QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：喹啉衍生物作为抗菌剂
公开(公告)号：WO2007014941A2
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064858
申请日：2006-07-31
申请人： JANSSEN PHARMACEUTICA N.V. , GUILLEMONT, Jérôme, Emile, Georges , PASQUIER, Elisabeth, Thérèse, Jeanne , LANÇOIS, David, Francis, Alain , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil , BACKX, Leo, Jacobus, Jozef , MEERPOEL, Lieven
发明人： GUILLEMONT, Jérôme, Emile, Georges , PASQUIER, Elisabeth, Thérèse, Jeanne , LANÇOIS, David, Francis, Alain , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil , BACKX, Leo, Jacobus, Jozef , MEERPOEL, Lieven
IPC分类号： A61K31/47 , A61P31/04 , C07D215/22 , C07D215/18
CPC分类号： C07D215/227 , A61K31/47
摘要： Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (I), a pharmaceutically acceptable acid or base addition salt, a quaternary amine, a stereochemically isomeric form, a tautomeric form or a N -oxide form thereof, wherein R 1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1 to 3; s is O to 4; R 2 is hydrogen; halo; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het or a radical of formula (II), R 3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is O to 4 ; R 4 and R 5 each independently are hydrogen, alkyl or benzyl; or R 4 and R 5 may be taken together including the N to which they are attached ; R 6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl ; or two vicinal R 6 radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1 to 5 ; R 7 is hydrogen, alkyl, Ar or Het ; R 8 is hydrogen, alkyl, hydroxyl, aminocarbonyl, mono-or di(alkyl)aminocarbonyl, Ar, Het, alkyl substituted with one or two Het, alkyl substituted with one or two Ar, Het-C(=O)- or Ar-C(=O)-; provided that when the R 3 bearing radical is placed in position 3 of the quinoline moiety; R 7 is placed in position 4 and R 2 is placed in position 2 and represents hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula (III), then s is 1 to 4.
摘要翻译：化合物在制备用于治疗细菌感染的药物中的用途，条件是细菌感染不是分枝杆菌感染，所述化合物是式（I）化合物，药学上可接受的盐可接受的酸或碱加成盐，季胺，立体化学异构形式，互变异构形式或其N-氧化物形式，其中R 1为氢，卤素，卤代烷基氰基，羟基，Ar，Het，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，Ar-烷基或二（Ar）烷基; p是1至3; s是0到4; R 2是氢; 光环; 烷基; 羟基; 巯基; 任选取代的烷氧基; 烷氧基烷; 烷; 其中烷基可任选被取代的单或二（烷基）氨基; Ar组成; Het或式（II）的基团，R 3为烷基，Ar，Ar-烷基，Het或Het-烷基; q是0到4; R 4和R 5各自独立地为氢，烷基或苄基; 或者R 4和R 5可以一起包括它们所连接的N; Ar为烷基或二（Ar）烷基; R为氢，或两个邻近的R 6基团可以与它们所连接的苯环一起形成萘基; r是1至5; R 7是氢，烷基，Ar或Het; R 8是氢，烷基，羟基，氨基羰基，单或二（烷基）氨基羰基，Ar，Het，被一个或两个Het取代的烷基，被一个或两个Ar取代的烷基，Het-C （= O） - 或Ar-C（= O） - ; 条件是当含有R 3 3的基团置于喹啉部分的3位时; R 7位于4位，R 2位于2位并代表氢，羟基，巯基，烷氧基，烷氧基烷氧基，烷硫基，单或二（烷基）氨基或式（III）的基团，则s为1至4.

5. 发明申请

WO2004017969A1 N-ARYL PIPERIDINE SUBSTITUTED BIPHENYLCARBOXAMIDES AS INHIBITORS OF APOLIPOPROTEIN B SECRETION 审中-公开
标题翻译：作为APOLIPOPROTEIN B分泌的抑制剂的N-亚乙基哌啶取代的联苯酰胺
公开(公告)号：WO2004017969A1
公开(公告)日：2004-03-04
申请号：PCT/EP2003/008694
申请日：2003-08-05
申请人： JANSSEN PHARMACEUTICA N.V. , MEERPOEL, Lieven , BACKX, Leo, Jacobus, Jozef , ROEVENS, Peter, Walter, Maria
发明人： MEERPOEL, Lieven , BACKX, Leo, Jacobus, Jozef , ROEVENS, Peter, Walter, Maria
IPC分类号： A61K31/445
CPC分类号： C07D401/04 , C07D211/34 , C07D211/62
摘要： N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) 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. The compounds act as inhibitors of apolipoprotein B.
摘要翻译：式（I）的N-芳基哌啶取代的联苯甲酰胺化合物制备此类化合物的方法，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型糖尿病的药物的用途。该化合物作为载脂蛋白B的抑制剂。

6. 发明申请

WO2007000435A1 QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：喹诺酮衍生物作为抗菌剂
公开(公告)号：WO2007000435A1
公开(公告)日：2007-01-04
申请号：PCT/EP2006/063553
申请日：2006-06-26
申请人： JANSSEN PHARMACEUTICA N.V. , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil , GUILLEMONT, Jérôme, Emile, Georges , LANÇOIS, David, Francis, Alain , MOTTE, Magali, Madeleine, Simone , DORANGE, Ismet , BACKX, Leo, Jacobus, Jozef , MEERPOEL, Lieven
发明人： ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil , GUILLEMONT, Jérôme, Emile, Georges , LANÇOIS, David, Francis, Alain , MOTTE, Magali, Madeleine, Simone , DORANGE, Ismet , BACKX, Leo, Jacobus, Jozef , MEERPOEL, Lieven
IPC分类号： A61K31/47 , A61P31/04 , C07D215/22
CPC分类号： A61K31/47 , C07D215/227
摘要： Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N -oxide form thereof, wherein R 1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R 2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula ; R 3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 1, 2 or 3; R 4 and R 5 are hydrogen, alkyl or benzyl; or R 4 and R 5 together and including the N to which they are attached may form a ring; R 6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl ; or two vicinal R 6 radicals may be taken together to form a bivalent radical of formula - CH=CH-CH=CH-; r is 1, 2, 3, 4 or 5; R 7 is hydrogen, alkyl, Ar or Het; R 8 is hydrogen or alkyl; R 9 is oxo ; or R 8 and R 9 together form the radical -CH=CH-N=.
摘要翻译：使用化合物制造用于治疗细菌感染的药物，只要细菌感染不是分枝杆菌感染，所述化合物是式（Ia）或（Ib）的化合物，其药学上可接受的酸或碱加成其盐，其立体化学异构形式，其互变异构形式或其N-氧化物形式，其中R 1是氢，卤素，卤代烷基，氰基，羟基，Ar，Het，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar）烷基; p为1,2,3或4; R 2是氢，羟基，巯基，烷氧基，烷氧基烷氧基，烷硫基，一或二（烷基）氨基或式的基团; R 3是烷基，Ar，Ar-烷基，Het或Het-烷基; q为1,2或3; R 4和R 5是氢，烷基或苄基; 或R 4和R 5一起并且包括它们所连接的N可以形成环; R 6是氢，卤素，卤代烷基，羟基，Ar，烷基，烷氧基，烷硫基，烷氧基烷基，烷硫基烷基，芳烷基或二（Ar）烷基; 或两个邻位R 6个基团可以一起形成式-CH = CH-CH = CH-的二价基团; r为1,2,3,4或5; R 7是氢，烷基，Ar或Het; R 8是氢或烷基; R 9是氧代; 或R 8和R 9一起形成基团-CH = CH-N =。

7. 发明申请

WO2003076422A1 SULFONYL-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译：磺酰衍生物作为HISTONE脱乙酰壳多糖的新型抑制剂
公开(公告)号：WO2003076422A1
公开(公告)日：2003-09-18
申请号：PCT/EP2003/002516
申请日：2003-03-11
申请人： JANSSEN PHARMACEUTICA N.V. , VAN EMELEN, Kristof , ARTS, Janine , BACKX, Leo, Jacobus, Jozef , DE WINTER, Hans, Louis, Jos , VAN BRANDT, Sven, Franciscus, Anna , VERDONCK, Marc, Gustaaf, Celine , MEERPOEL, Lieven , PILATTE, Isabelle, Noëlle, Constance , PONCELET, Virginie, Sophie , DYATKIN, Alexey, Borisovich
发明人： VAN EMELEN, Kristof , ARTS, Janine , BACKX, Leo, Jacobus, Jozef , DE WINTER, Hans, Louis, Jos , VAN BRANDT, Sven, Franciscus, Anna , VERDONCK, Marc, Gustaaf, Celine , MEERPOEL, Lieven , PILATTE, Isabelle, Noëlle, Constance , PONCELET, Virginie, Sophie , DYATKIN, Alexey, Borisovich
IPC分类号： C07D295/22
CPC分类号： 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 , C07D207/277 , C07D207/28 , C07D211/14 , C07D211/58 , C07D213/78 , C07D213/81 , C07D213/82 , C07D217/02 , C07D217/04 , C07D217/16 , C07D233/90 , C07D239/42 , C07D241/04 , C07D241/24 , C07D243/08 , C07D261/10 , C07D295/155 , C07D295/22 , C07D295/26 , C07D307/68 , C07D307/79 , C07D333/34 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48 , G01N33/573 , G01N2333/91
摘要： This invention comprises the novel compounds of formula (I) wherein n, m, t, 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.
摘要翻译：本发明包括式（I）的新化合物，其中n，m，t，R 1，R 2，R 3，R 4，L，Q，X，Y，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。

8. 发明申请

WO2006136553A1 IMIDAZOLINONE AND HYDANTOINE DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译：咪唑啉酮和羟胺衍生物作为乙酰脱乙酰壳多糖的新型抑制剂
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
申请人： JANSSEN PHARMACEUTICA N.V. , TEN HOLTE, Peter , VAN EMELEN, Kristof , ANGIBAUD, Patrick, René , MARCONNET-DECRANE, Laurence, Françoise, Bernadette , MEERPOEL, Lieven
发明人： TEN HOLTE, Peter , VAN EMELEN, Kristof , ANGIBAUD, Patrick, René , MARCONNET-DECRANE, Laurence, Françoise, Bernadette , MEERPOEL, Lieven
IPC分类号： C07D401/14 , C07D413/14 , A61K31/4166 , A61P35/00
CPC分类号： C07D413/14 , C07D401/14 , C07D405/14
摘要： 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.
摘要翻译：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。

9. 发明申请

WO2003076400A1 NEW INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译： HISTONE DEACETYLASE的新抑制剂
公开(公告)号：WO2003076400A1
公开(公告)日：2003-09-18
申请号：PCT/EP2003/002514
申请日：2003-03-11
申请人： JANSSEN PHARMACEUTICA N.V. , ANGIBAUD, Patrick, René , PILATTE, Isabelle, Noëlle, Constance , VAN BRANDT, Sven, Franciscus, Anna , ROUX, Bruno , TEN HOLTE, Peter , VERDONCK, Marc, Gustaaf, Celine , MEERPOEL, Lieven , DYATKIN, Alexey, Borisovich
发明人： ANGIBAUD, Patrick, René , PILATTE, Isabelle, Noëlle, Constance , VAN BRANDT, Sven, Franciscus, Anna , ROUX, Bruno , TEN HOLTE, Peter , VERDONCK, Marc, Gustaaf, Celine , MEERPOEL, Lieven , DYATKIN, Alexey, Borisovich
IPC分类号： C07D211/58
CPC分类号： 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
摘要： This invention comprises the novel compounds of formula (I) wherein n, t, 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.
摘要翻译：本发明包括其中n，t，R 1，R 2，R 3，R 4，L，Q，X，Y，Z并具有定义的具有组蛋白脱乙酰酶抑制酶活性的式（I）化合物。其制剂，含有它们的组合物及其作为药物的用途。

10. 发明申请

WO2011154298A1 NOVEL ANTIFUNGAL 5,6-DIHYDRO-4-[(DIFLUOROETHYL)PHENYL]-4H-PYRROLO[1,2-a][1,4]BENZODIAZEPINE AND 4-(DIFLUOROETHYL)PHENYL-6H-PYRROLO[1,2-a][1,4]BENZODIAZEPINE DERIVATIVES 审中-公开
标题翻译：新的反式5,6-二羟基-4 - [（二氟乙基）苯基] -4H-吡咯并[1,2-a] [1,4]苯并嗪和4-（二氟乙基）苯基-6H-吡咯并[1,2-a ] [1,4]苯并咪唑衍生物
公开(公告)号：WO2011154298A1
公开(公告)日：2011-12-15
申请号：PCT/EP2011/059058
申请日：2011-06-01
申请人： JANSSEN PHARMACEUTICA NV , MEERPOEL, Lieven , MAES, Louis, Jules, Roger, Marie , DE WIT, Kelly
发明人： MEERPOEL, Lieven , MAES, Louis, Jules, Roger, Marie , DE WIT, Kelly
IPC分类号： C07D487/04 , A61K31/5517 , A61P31/10
CPC分类号： C07D487/04
摘要： The present invention concerns novel compounds 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.
摘要翻译：本发明涉及式（I）的新化合物，其中R 1，R 2，R 3，R 4，R 5和R 6具有权利要求中定义的含义。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。

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