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71. 发明授权

US07592450B2 Piperazinyl-, piperidinyl- and morpholinyl-derivatives as inhibitors of histone deacetylase 有权
标题翻译：哌嗪基，哌啶基和吗啉基衍生物作为组蛋白脱乙酰酶的抑制剂
公开(公告)号：US07592450B2
公开(公告)日：2009-09-22
申请号：US10507084
申请日：2003-03-11
申请人： Kristof Van Emelen
发明人： Kristof Van Emelen
IPC分类号： C07D413/04 , C07D413/14 , C07D239/42 , A61K31/496 , A61K31/506
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 , C12Q1/44 , C12Q1/48
摘要： This invention comprises the novel compounds of formula (I) wherein t, R1, R2, L, Q, X, Y, Z and (a) 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t，R 1，R 2，L，Q，X，Y，Z和（a）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。

72. 发明申请

US20080255140A1 Squaric Acid Derivatives as Inhibitors of Histone Deacetylase 有权
标题翻译：方酸衍生物作为组蛋白脱乙酰酶的抑制剂
公开(公告)号：US20080255140A1
公开(公告)日：2008-10-16
申请号：US12090771
申请日：2006-10-23
申请人： Kristof Van Emelen
发明人： Kristof Van Emelen
IPC分类号： A61K31/506 , C07D403/04 , C07D403/14 , A61P35/00
CPC分类号： C07D239/42 , C07D401/12 , C07D403/12
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2 and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括具有组蛋白脱乙酰酶抑制酶活性的式（I）的新化合物，其中R 1，R 2和X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。

73. 发明申请

US20080139601A1 3-Cyano-Quinoline Derivatives With Antiproliferative Activity 有权
公开(公告)号：US20080139601A1
公开(公告)日：2008-06-12
申请号：US10596509
申请日：2004-12-15
申请人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Antonius Buijnsters , Kristof Van Emelen , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
发明人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Antonius Buijnsters , Kristof Van Emelen , Werner Constant Johan Embrechts , Timothy Pietro Suren Perera
IPC分类号： A61K31/4745 , C07D487/02 , A61P35/00
CPC分类号： C07D215/54 , A61K31/4748 , C07D498/06
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.

74. 发明授权

US07358239B2 Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives 有权
公开(公告)号：US07358239B2
公开(公告)日：2008-04-15
申请号：US11079606
申请日：2005-03-14
申请人： Marcel Frans Leopold De Bruyn , Kristof Van Emelen , Piet Tom Bert Paul Wigerinck , Wim Gaston Verschueren
发明人： Marcel Frans Leopold De Bruyn , Kristof Van Emelen , Piet Tom Bert Paul Wigerinck , Wim Gaston Verschueren
IPC分类号： A61P1/00 , A61K31/00 , A61K31/55 , A61K31/54 , A61K31/497 , A61K31/4965 , A61K31/517 , A61K31/505 , A61K31/41 , A61K31/415 , A61K31/40 , C07D245/00 , C07D487/00 , C07D243/00 , C07D273/00 , C07D285/00 , C07D239/00 , C07D241/00 , C07D403/00 , C07D417/00 , C07D513/00 , C07D233/00
CPC分类号： C07D405/12 , C07D405/14
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.

75. 发明授权

US07273862B2 Aminoalkyl substituted (benzodioxan, benzofuran or benzopyran) derivatives 有权
标题翻译：氨基烷基取代的（苯并二恶烷，苯并呋喃或苯并吡喃）衍生物
公开(公告)号：US07273862B2
公开(公告)日：2007-09-25
申请号：US10999187
申请日：2004-11-29
申请人： Kristof Van Emelen , Marcel Frans Leopold De Bruyn
发明人： Kristof Van Emelen , Marcel Frans Leopold De Bruyn
IPC分类号： C07D403/12 , C07D417/12 , A61K31/506 , A61K31/549
CPC分类号： C07D405/12 , C07D417/12
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.
摘要翻译：本发明涉及式（I）化合物，其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中-Z 1 -Z 2， SUP> - 是二价基团; R 1，R 2和R 3各自独立地选自氢，C 1-6烷基，羟基，卤素等; 或当R 1和R 2在相邻的碳原子上时，R 1和R 2可以一起形成式的二价基团; Alk＆lt; 1＆gt;和Alk 2是任选取代的C 1-6烷二基; R 6是氢或苯基甲基; R 5是下式的基团，其中n是1或2; p <0> 1是0，p <2>是1或2; 或p <1> 1是1或2，并且p O是0; X是氧，硫或-NR 9; Y是氧或硫; R 7是氢，C 1-6烷基，C 3-6环烷基，苯基或苯基甲基; R 8是C 1-6烷基，C 3-6环烷基苯基或苯基甲基; R 9是氰基，C 1-6烷基，C 3-6环烷基，C 1-6 烷氧基羰基或氨基羰基; R 10为氢或C 1-6烷基; 而Q是二价基团。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与减退的放松有关的病症。

76. 发明申请

US20050148613A1 Carbonylamino-derivatives as novel inhibitors of histone deacetylase 有权
标题翻译：羰基氨基衍生物作为组蛋白脱乙酰酶的新型抑制剂
公开(公告)号：US20050148613A1
公开(公告)日：2005-07-07
申请号：US10507788
申请日：2003-03-11
申请人： Kristof Van Emelen , Marc Verdonck , Sven Franciscus Van Brandt , Leo Backx
发明人： Kristof Van Emelen , Marc Verdonck , Sven Franciscus Van Brandt , Leo Backx
IPC分类号： C07D249/12 , A61K31/40 , A61K31/438 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/4545 , A61K31/4709 , A61K31/472 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/517 , A61K31/53 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K45/00 , A61P1/04 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/08 , A61P13/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/10 , A61P17/14 , A61P17/16 , A61P19/02 , A61P19/06 , A61P21/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07C259/10 , C07D207/09 , C07D207/14 , C07D211/26 , C07D211/58 , C07D213/74 , C07D213/78 , C07D217/02 , C07D217/04 , C07D239/42 , C07D241/04 , C07D295/14 , C07D295/155 , C07D295/20 , C07D295/22 , C07D295/26 , C07D307/68 , C07D317/58 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/02 , C07D413/04 , C07D413/12 , C07D471/10 , C12Q1/48 , C07D43/02
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 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/04 , C07D471/04 , C07D471/10 , C07D513/04 , C12Q1/34 , C12Q1/48 , G01N33/573 , G01N2333/98
摘要： This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y 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：本发明包括新的式（I）化合物，其中n，m，t，R 1，R 2，R 3，R 3，具有组蛋白脱乙酰酶抑制酶活性的含义，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。

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