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1. 发明授权

US07138403B2 2,4,5-trisubstituted thiazolyl derivatives and their antiinflammatory activity 有权
标题翻译： 2,4,5-三取代噻唑衍生物及其抗炎活性
公开(公告)号：US07138403B2
公开(公告)日：2006-11-21
申请号：US10486820
申请日：2002-08-09
申请人： Christopher John Love , Jean Pierre Frans Van Wauwe , Marc J. De Brabander , Roger Clive Moses , Mykhalyo Goncharenko , Ludwig Paul Cooymans , Nele Vandermaesen , Gaston Stanislas Marcella Diels , Anthony William Sibley , Caterina Noula
发明人： Christopher John Love , Jean Pierre Frans Van Wauwe , Marc J. De Brabander , Roger Clive Moses , Mykhalyo Goncharenko , Ludwig Paul Cooymans , Nele Vandermaesen , Gaston Stanislas Marcella Diels , Anthony William Sibley , Caterina Noula
IPC分类号： C07D239/24 , A61K31/495
CPC分类号： C07D417/04 , C07D277/28 , C07D417/14
摘要： This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl or C1-6alkyloxy; polyhaloC1-4alkyl; C1-4alkyloxy; cyano; amino; aminocarbonyl; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; H2N—S(═O)2—; mono- or di(C1-6alkyl)amino-S(═O)2; —C(═N—Rx)NRyRz; Q is an optionally substituted carbocycle or an optionally substituted heterocycle; L is substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through TNF-α and/or IL-12.
摘要翻译：本发明涉及式（I）化合物的N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构体形式的用途，其中Z为卤素; C 1-6烷基; 被羟基，羧基，氰基，氨基，一或二（C 1-6烷基）氨基，氨基羰基，一或二（C（C 1-6）烷基）氨基取代的C 1-6烷基 C 1-6烷基）氨基羰基，C 1-6烷氧基羰基或C 1-6烷基氧基; 多卤代1-4烷基; C 1-4烷氧基; 氰基; 氨基; 氨基羰基; 单或二（C 1-6烷基）氨基羰基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; H 2 -N-S（-O）2 - ; 单或二（C 1-6烷基）氨基-S（-O）2; -C（-N-R x X）NR z R z Z; Q是任选取代的碳环或任选取代的杂环; L是取代的苯基或任选取代的单环5或6元部分饱和或芳族杂环或双环部分饱和或芳族杂环; 芳基是任选取代的苯基; 用于制备用于预防或治疗通过TNF-α和/或IL-12介导的疾病的药物。

2. 发明授权

US06951857B2 6-Azauracil derivatives as IL-5 inhibitors 失效
公开(公告)号：US06951857B2
公开(公告)日：2005-10-04
申请号：US10434896
申请日：2003-05-09
申请人： Eddy Jean Edgard Freyne , Gustaaf Maria Boeckx , Jean Pierre Frans Van Wauwe , Gaston Stanislas Marcella Diels
发明人： Eddy Jean Edgard Freyne , Gustaaf Maria Boeckx , Jean Pierre Frans Van Wauwe , Gaston Stanislas Marcella Diels
IPC分类号： C07D253/06 , A61K31/53 , A61K51/00 , A61K51/04 , A61P11/06 , A61P17/00 , A61P27/02 , A61P27/14 , A61P37/08 , A61P43/00 , C07D253/075 , C07D403/10 , C07D417/10
CPC分类号： A61K51/0491 , A61K31/53 , A61K51/04 , A61K51/0461 , C07D253/075 , C07D403/10 , C07D417/10
摘要： The present invention is concerned with the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p represents 0, 1, 2 or 3; q represents 0, 1, 2, 3 or 4; R1 represents hydrogen, C1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, mercapto, C1-6alkylthio, C3-7cycloalkyl, aryl or C1-6alkyl substituted with mono- or di(C1-6alkyl)amino, C1-6alkyloxy, aryl or Het; R2 represents cyano or a radical of formula —C(═X)—Y—R5; wherein X represents O or S; Y represents O, S, NR6 or a direct bond; R5 represents hydrogen; C3-7cycloalkyl; aryl or optionally substituted C1-6alkyl; and where Y is a direct bond, R5 may also be halo or Het; R3 and R4 each independently represents halo, haloC1-6alkyl, C1-6alkyl, hydroxy, C1-6alkyloxy, C1-6alkylcarbonyloxy, mercapto, C1-6alkylthio, C1-6alkylsulfonyl, C1-6alkylsulfinyl, haloC1-6alkylsulfonyl, aryl, cyano, nitro, amino, mono- and di(C1-6alkyl)amino or (C1-6alkylcarbonyl)amino; aryl represents phenyl or substituted phenyl; and Het represents an optionally substituted heterocycle; in the manufacture of a medicament useful for treating eosinophil-dependent inflammatory diseases. The invention also relates to novel compounds, their preparation and compositions comprising them.

3. 发明授权

US06743792B2 6-azauracil derivatives as IL-5 inhibitors 失效
标题翻译： 6-氮尿嘧啶衍生物作为IL-5抑制剂
公开(公告)号：US06743792B2
公开(公告)日：2004-06-01
申请号：US09855068
申请日：2001-05-14
申请人： Eddy Jean Edgard Freyne , Gustaaf Maria Boeckx , Jean Pierre Frans Van Wauwe , Gaston Stanislas Marcella Diels
发明人： Eddy Jean Edgard Freyne , Gustaaf Maria Boeckx , Jean Pierre Frans Van Wauwe , Gaston Stanislas Marcella Diels
IPC分类号： C07D253075
CPC分类号： A61K51/0491 , A61K31/53 , A61K51/04 , A61K51/0461 , C07D253/075 , C07D403/10 , C07D417/10
摘要： The present invention is concerned with the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p represents 0, 1, 2 or 3; q represents 0, 1, 2, 3 or 4; R1 represents hydrogen, C1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, mercapto, C1-6alkylthio, C3-7cycloalkyl, aryl or C1-6alkyl substituted with mono- or di(C1-6alkyl)-amino, C1-6alkyloxy, aryl or Het; R2 represents cyano or a radical of formula —C(═X)—Y—R5; wherein X represents O or S; Y represents O, S, NR6 or a direct bond; R5 represents hydrogen; C3-7cycloalkyl; aryl or optionally substituted C1-6alkyl; and where Y is a direct bond, R5 may also be halo or Het; R3 and R4 each independently represents halo, haloC1-6alkyl, C1-6alkyl, hydroxy, C1-6alkyloxy, C1-6alkylcarbonyloxy, mercapto, C1-6alkylthio, C1-6alkylsulfonyl, C1-6alkylsulfinyl, haloC1-6alkylsulfonyl, aryl, cyano, nitro, amino, mono- and di(C1-6alkyl)amino or (C1-6alkylcarbonyl)amino; aryl represents phenyl or substituted phenyl; and Het represents an optionally substituted heterocycle; in the manufacture of a medicament useful for treating eosinophil-dependent inflammatory diseases. The invention also relates to novel compounds, their preparation and compositions comprising them.
摘要翻译：本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐及其立体化学异构形式，其中p代表0,1,2或3; q表示0,1,2,3或4; R 1表示氢，C 1-6烷基，一或二（C 1-6烷基）氨基C 1-6烷氧基，巯基，C 1-6烷硫基，C 3-7环烷基，芳基或被单或二（C 1-6烷基）氨基，C 1-6烷氧基，芳基或Het; R 2表示氰基或式-C（= X）-Y-R 5的基团; 其中X表示O或S; Y表示O，S，NR 6或直接键; R 5表示氢; C 3-7环烷基; 芳基或任选取代的C 1-6烷基; 并且其中Y是直接键，R 5也可以是卤素或Het; R 3和R 4各自独立地表示卤素，卤代C 1-6烷基，C 1-6烷基，羟基，C 1-6烷氧基，C 1-6烷基羰氧基，巯基，C 1-6烷硫基，C 1-6烷基磺酰基，C 1-6烷基亚磺酰基，卤代C 1-6烷基磺酰基，芳基，氰基，硝基，氨基，单和二（C 1-6烷基）氨基或（C 1-6烷基羰基）氨基; 芳基表示苯基或取代的苯基; 并且Het表示任选取代的杂环; 在制备可用于治疗嗜酸性粒细胞依赖性炎性疾病的药物中。本发明还涉及新化合物，其制备方法和包含它们的组合物。

4. 发明授权

US07893280B2 2,4-disubstituted thiazolyl derivatives 有权
标题翻译： 2,4-二取代噻唑衍生物
公开(公告)号：US07893280B2
公开(公告)日：2011-02-22
申请号：US11435335
申请日：2006-05-16
申请人： Christopher Love , Jean Pierre Frans Van Wauwe , Marc De Brabander , Ludwig Cooymans , Nele Vandermaesen , Ludo Edmond Josephine Kennis
发明人： Christopher Love , Jean Pierre Frans Van Wauwe , Marc De Brabander , Ludwig Cooymans , Nele Vandermaesen , Ludo Edmond Josephine Kennis
IPC分类号： A61K31/425 , C07D207/00
CPC分类号： C07D417/04 , C07D277/42 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： This invention concerns the use of a compound of formula (I′) a N-oxide, pharmaceutically acceptable addition salt, quaternary amine and stereochemically isomeric form thereof, wherein Q is optionally substituted C3-6cycloalkyl, phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl; or Q is a radical of formula wherein X and Y each independently are O, NR3, CH2 or S, with R3 being hydrogen or C1-4alkyl; q is 1 to 4; Z is O or NR4 with R4 being hydrogen or C1-4alkyl; r is 1 to 3; L is optionally substituted phenyl or L is Het with Het being an optionally substituted five- or six-membered heterocyclic ring or an optionally substituted bicyclic heterocyclic ring; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through cytokines.
摘要翻译：本发明涉及式（I'）化合物的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的用途，其中Q是任选取代的C 3-6环烷基，苯基，萘基，吡啶基，嘧啶基，吡嗪基，哒嗪基，苯并噻唑基，苯并恶唑基，苯并咪唑基，吲唑基或咪唑并吡啶基; 或Q是下式的基团，其中X和Y各自独立地是O，NR 3，CH 2或S，其中R 3是氢或C 1-4烷基; q为1〜4; Z是O或NR4，其中R4是氢或C1-4烷基; r为1〜3; L是任选取代的苯基或L是Het，Het是任选取代的五元或六元杂环或任选取代的双环杂环; 用于制备用于预防或治疗通过细胞因子介导的疾病的药物。

5. 发明授权

US07105550B2 2,4-disubstituted thiazolyl derivatives 有权
标题翻译： 2,4-二取代噻唑衍生物
公开(公告)号：US07105550B2
公开(公告)日：2006-09-12
申请号：US10220350
申请日：2001-02-20
申请人： Christopher Love , Jean Pierre Frans Van Wauwe , Marc De Brabander , Ludwig Cooymans , Nele Vandermaesen , Ludo Edmond Josephine Kennis
发明人： Christopher Love , Jean Pierre Frans Van Wauwe , Marc De Brabander , Ludwig Cooymans , Nele Vandermaesen , Ludo Edmond Josephine Kennis
IPC分类号： A61K31/41 , A61K31/425 , A61K31/415
CPC分类号： C07D417/04 , C07D277/42 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： This invention concerns the use of a compound of formula (I′) a N-oxide, pharmaceutically acceptable addition salt, quaternary amine and stereochemically isomeric form thereof, wherein Q is optionally substituted C3-6cycloalkyl, phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl; or Q is a radical of formula wherein X and Y each independently are O, NR3, CH2 or S, with R3 being hydrogen or C1-4alkyl; q is 1 to 4; Z is O or NR4 with R4 being hydrogen or C1-4alkyl; r is 1 to 3; L is optionally substituted phenyl or L is Het with Het being an optionally substituted five- or six-membered heterocyclic ring or an optionally substituted bicyclic heterocyclic ring; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through cytokines.
摘要翻译：本发明涉及式（I'）化合物的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的用途，其中Q是任选取代的C 3-6环烷基，苯基，萘基，吡啶基，嘧啶基，吡嗪基，哒嗪基，苯并噻唑基，苯并恶唑基，苯并咪唑基，吲唑基或咪唑并吡啶基。或Q是下式的基团，其中X和Y各自独立地为O，NR 3，CH 2或S，其中R 3为氢或C 1-4烷基; q为1〜4; Z为O或NR 4，其中R 4为氢或C 1-4烷基; r为1〜3; L是任选取代的苯基或L是Het，Het是任选取代的五元或六元杂环或任选取代的双环杂环; 用于制备用于预防或治疗通过细胞因子介导的疾病的药物。

6. 发明授权

US07511068B2 Mercaptoimidazoles as CCR2 receptor antagonists 失效
标题翻译：巯基咪唑作为CCR2受体拮抗剂
公开(公告)号：US07511068B2
公开(公告)日：2009-03-31
申请号：US10544569
申请日：2004-01-30
申请人： Guy Rosalia Eugeen Van Lommen , Julien Georges Pierre-Olivier Doyon , Jean Pierre Frans Van Wauwe , Marina Lucie Louise Cools , Erwin Coesemans
发明人： Guy Rosalia Eugeen Van Lommen , Julien Georges Pierre-Olivier Doyon , Jean Pierre Frans Van Wauwe , Marina Lucie Louise Cools , Erwin Coesemans
IPC分类号： A61K31/4164 , C07D233/04
CPC分类号： A61K31/4174 , A61K31/4178 , A61K31/5025 , C07D233/84 , C07D233/90 , C07D263/44 , C07D409/06 , C07D487/04
摘要： The present invention relates to a compound of formula (I) having CCR2 receptor antagonistic properties, particularly anti-inflammatory properties.
摘要翻译：本发明涉及具有CCR2受体拮抗性质，特别是抗炎性质的式（I）化合物。

7. 发明授权

US06451812B1 Farnesyl protein transferase inhibitors for treating arthropathies 有权
标题翻译：用于治疗关节病的法呢基蛋白转移酶抑制剂
公开(公告)号：US06451812B1
公开(公告)日：2002-09-17
申请号：US09743077
申请日：2001-01-03
申请人： David William End , Marina Lucie Louise Cools , Jean Pierre Frans Van Wauwe
发明人： David William End , Marina Lucie Louise Cools , Jean Pierre Frans Van Wauwe
IPC分类号： A61K3147
CPC分类号： A61K31/4709 , A61K31/47 , A61K31/4704
摘要： The present invention is concerned with the finding that farnesyl protein transferase inhibitors are useful for preparing a pharmaceutical composition for treating arthropathies such as rheumatoid arthritis, osteoarthritis, juvenile arthritis, and gout.
摘要翻译：本发明涉及法呢基蛋白转移酶抑制剂可用于制备治疗关节病如药物性关节炎，骨关节炎，幼年关节炎和痛风的药物组合物。

8. 发明申请

US20090030039A1 Piperidine Derivatives as Cxcr3 Receptor Antagonists 审中-公开
标题翻译：哌啶衍生物作为Cxcr3受体拮抗剂
公开(公告)号：US20090030039A1
公开(公告)日：2009-01-29
申请号：US12278719
申请日：2007-02-06
申请人： Erwin Coesemans , Jean-Pierre Andre Marc Bongartz , Guy Rosali Eugeen Van Lommen , Jean Pierre Frans Van Wauwe , Mieke Buntinx
发明人： Erwin Coesemans , Jean-Pierre Andre Marc Bongartz , Guy Rosali Eugeen Van Lommen , Jean Pierre Frans Van Wauwe , Mieke Buntinx
IPC分类号： A61K31/4545 , C07D401/04
CPC分类号： C07D401/04 , C07D401/14
摘要： The present invention relates to a compound of formula (I) a N-oxide thereof, a pharmaceutically acceptable salt thereof, a stereochemically isomeric form thereof or a solvate thereof, wherein X represents N or CH; Y and Z each independently represent C(═O) or CH2 provided that at least one of Y and Z represents C(═O); R1 represents CH(R4)-aryl or CH(R4)-heteroaryl; R2 represents aryl2 or heteroaryl; R3 represents hydrogen; C1-4alkylcarbonyl; C1-6alkyl optionally substituted with C1-6alkyloxy, C1-6alkylthio, C1-6alkyloxycarbonyl or aryl1; provided that when Y and Z each represent C(═O), X represents CH, R3 represents hydrogen, R4 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then aryl in the definition of R1 is other than phenyl substituted with one halo or with one or two C1-4alkyl; and provided that when Y and Z each represent C(═O), X represents CH, R3 represents hydrogen, and R2 represents unsubstituted pyridyl or phenyl optionally substituted with one halo or with one C1-4alkyloxy or with one or two C1-4alkyl, then heteroaryl in the definition of R1 is other than unsubstituted thienyl or unsubstituted pyridyl. The present invention also relates to the use of a compound of formula (I) for the manufacture of a medicament for preventing or treating a disease mediated through activation of the CXCR3 receptor; to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的化合物，其N-氧化物，其药学上可接受的盐，其立体化学异构形式或其溶剂合物，其中X表示N或CH; Y和Z各自独立地表示C（-O）或CH 2，条件是Y和Z中的至少一个表示C（-O）; R 1表示CH（R 4） - 芳基或CH（R 4） - 杂芳基; R 2表示芳基2或杂芳基; R3表示氢; C 1-4烷基羰基; 任选被C 1-6烷氧基，C 1-6烷硫基，C 1-6烷氧基羰基或芳基取代的C 1-6烷基; 条件是当Y和Z各自表示C（-O）时，X表示CH，R 3表示氢，R 4表示氢，R 2表示未取代的吡啶基或任选被一个卤素或一个C 1-4烷氧基取代的苯基或与一个或两个C 1 -4-烷基，则R1定义中的芳基不同于被一个卤素或一个或两个C 1-4烷基取代的苯基; 并且条件是当Y和Z各自表示C（-O）时，X表示CH，R 3表示氢，R 2表示未取代的吡啶基或任选被一个卤素或一个C 1-4烷氧基取代或与一个或两个C 1-4烷基取代的苯基，那么R1的定义中的杂芳基不是未取代的噻吩基或未取代的吡啶基。本发明还涉及式（I）化合物在制备用于预防或治疗通过活化CXCR3受体介导的疾病的药物中的用途; 制备式（I）化合物的方法和包含它们的药物组合物。

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