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1. 发明授权

US07803823B2 2-amino-4,5-trisubstituted thiazolyl derivatives 有权
标题翻译： 2-氨基-4,5-三取代噻唑基衍生物
公开(公告)号：US07803823B2
公开(公告)日：2010-09-28
申请号：US11742741
申请日：2007-05-01
申请人： Christopher John Love , Guy Rosalia Eugeen Van Lommen , Julien Georges Pierre-Olivier Doyon , Jean-Pierre André Marc Bongartz , Marcel Jozef Maria Van der Aa , Robert Jozef Maria Hendrickx , Peter Jacobus Johannes Antonius Buijnsters , Ludwig Paul Cooymans , Nele Vandermaesen , Erwin Coesemans , Gustaaf Maria Boeckx
发明人： Christopher John Love , Guy Rosalia Eugeen Van Lommen , Julien Georges Pierre-Olivier Doyon , Jean-Pierre André Marc Bongartz , Marcel Jozef Maria Van der Aa , Robert Jozef Maria Hendrickx , Peter Jacobus Johannes Antonius Buijnsters , Ludwig Paul Cooymans , Nele Vandermaesen , Erwin Coesemans , Gustaaf Maria Boeckx
IPC分类号： A61K31/425 , C07D277/20
CPC分类号： C07D417/04 , C07D277/42 , C07D471/04
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; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(═O)2—; mono- or di(C1-6alkyl)aminoS(═O)2; —C(═N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula L is optionally 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 inflammatory and/or auto-immune 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; C 1-6烷基羰基; C 1-6烷氧基羰基; 氨基羰基; 被羟基，羧基，氰基，氨基，被哌啶取代的氨基，被C 1-4烷基取代的哌啶基取代的氨基，单或二（C 1-6烷基）氨基，氨基羰基，一或二（C 1-6烷基）氨基羰基 C 1-6烷氧基羰基，C 1-6烷氧基，哌啶基，哌嗪基，吗啉基，硫代吗啉基; 多卤代C 1-4烷基; 氰基; 氨基; 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; 氨基S（= O）2-; 单或二（C 1-6烷基）氨基S（= O）2; -C（= N-Rx）NR y R z; Q是任选取代的C 3-6环烷基，苯基，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是式L的基团是任选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介导的炎症和/或自身免疫疾病的药物。

2. 发明授权

US07232838B2 2-amino-4,5-trisubstituted thiazolyl derivatives 有权
标题翻译： 2-氨基-4,5-三取代噻唑基衍生物
公开(公告)号：US07232838B2
公开(公告)日：2007-06-19
申请号：US10486819
申请日：2002-08-09
申请人： Christopher John Love , Guy Rosalia Eugeen Van Lommen , Julien Georges Pierre-Olivier Doyon , Jean-Pierre André Marc Bongartz , Marcel Jozef Maria Van der AA , Robert Jozef Maria Hendrickx , Peter Jacobus Johannes Antonius Buijnsters , Ludwig Paul Cooymans , Nele Vandermaesen , Erwin Coesemans , Gustaaf Maria Boeckx
发明人： Christopher John Love , Guy Rosalia Eugeen Van Lommen , Julien Georges Pierre-Olivier Doyon , Jean-Pierre André Marc Bongartz , Marcel Jozef Maria Van der AA , Robert Jozef Maria Hendrickx , Peter Jacobus Johannes Antonius Buijnsters , Ludwig Paul Cooymans , Nele Vandermaesen , Erwin Coesemans , Gustaaf Maria Boeckx
IPC分类号： A61K31/425 , C07D277/00 , C07D277/20
CPC分类号： C07D417/04 , C07D277/42 , C07D471/04
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; C1-6alkylcarbonyl; C1-6alkyloxy -carbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(═O)2—; mono- or di(C1-6alkyl)aminoS(═O)2; —C(═N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula (b-1), (b-2), or (b-3), L is optionally 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 inflammatory and/or auto-immune diseases mediated through TNF-α and/or IL-12
摘要翻译：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体形式的用途，其中Z是卤素; C 1-6烷基; C 1-6烷基羰基; C 1-6烷氧基羰基; 氨基羰基; 用羟基，羧基，氰基，氨基，被哌啶取代的氨基，被C 1-4烷基取代的哌啶基取代的氨基，单或二（ C 1-6烷基）氨基，氨基羰基，一或二（C 1-6烷基）氨基羰基，C 1-6烷氧基羰基， C 1-6烷基氧基，哌啶基，哌嗪基，吗啉基，硫代吗啉基; 多卤代1-4烷基; 氰基; 氨基; 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; 氨基-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为任选取代的C 3-6环烷基，苯基，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为式（b-1），（b-2）或（b-3）中，L是任选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介导的炎症和/或自身免疫疾病的药物

3. 发明申请

US20090036471A1 Triazolopyrimidine Derivatives As Glycogen Synthase Kinase 3 Inhibitors 审中-公开
标题翻译：三唑并嘧啶衍生物作为糖原合酶激酶3抑制剂
公开(公告)号：US20090036471A1
公开(公告)日：2009-02-05
申请号：US12211361
申请日：2008-09-16
申请人： Eddy Jean Edgard , Christopher John Love , Ludwig Paul Cooymans , Nele Vandermaesen , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts
发明人： Eddy Jean Edgard , Christopher John Love , Ludwig Paul Cooymans , Nele Vandermaesen , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts
IPC分类号： A61K31/519 , A61P25/00 , A61P3/10 , A61P29/00 , A61P17/00
CPC分类号： C07D487/04
摘要： This invention concerns compounds of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines and stereochemically isomeric forms thereof, their use, pharmaceutical compositions comprising them, processes for their preparation, and methods of their use.
摘要翻译：本发明涉及式N-氧化物的化合物，药学上可接受的加成盐，季胺及其立体化学异构形式，它们的用途，包含它们的药物组合物，其制备方法及其使用方法。

4. 发明授权

US07560458B2 Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors 有权
标题翻译：三氮代嘧啶衍生物作为糖原合酶激酶3抑制剂
公开(公告)号：US07560458B2
公开(公告)日：2009-07-14
申请号：US10564844
申请日：2004-07-12
申请人： Eddy Jean Edgard Freyne , Christopher John Love , Ludwig Paul Cooymans , Nele Vandermaesen , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts
发明人： Eddy Jean Edgard Freyne , Christopher John Love , Ludwig Paul Cooymans , Nele Vandermaesen , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts
IPC分类号： A61K31/535 , A61K31/501 , A61K31/519 , A01N43/90 , C07D413/00 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D487/04
摘要： This invention concerns compounds of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines and stereochemically isomeric forms thereof, their use, pharmaceutical compositions comprising them, and processes for their preparation.
摘要翻译：本发明涉及式N-氧化物的化合物，药学上可接受的加成盐，季胺及其立体化学异构形式，其用途，包含它们的药物组合物及其制备方法。

5. 发明授权

US07449465B2 Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors 有权
标题翻译：三氮代嘧啶衍生物作为糖原合酶激酶3抑制剂
公开(公告)号：US07449465B2
公开(公告)日：2008-11-11
申请号：US10565065
申请日：2004-07-12
申请人： Eddy Jean Edgard Freyne , Christopher John Love , Ludwig Paul Cooymans , Nele Vandermaesen , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts
发明人： Eddy Jean Edgard Freyne , Christopher John Love , Ludwig Paul Cooymans , Nele Vandermaesen , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts
IPC分类号： A61K31/501 , A61K31/4965 , A61K31/519 , A01N43/90 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D487/04
摘要： This invention concerns compounds of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines and stereochemically isomeric forms thereof, their use, pharmaceutical compositions comprising them, and processes for their preparation.
摘要翻译：本发明涉及式N-氧化物的化合物，药学上可接受的加成盐，季胺及其立体化学异构形式，其用途，包含它们的药物组合物及其制备方法。

6. 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。

7. 发明申请

US20100160349A1 TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
标题翻译：三氮唑嘧啶衍生物作为GLYCOGEN SYNTHASE激酶3抑制剂
公开(公告)号：US20100160349A1
公开(公告)日：2010-06-24
申请号：US11813973
申请日：2006-01-13
申请人： Christopher John Love , Ludwig Paul Cooymans , Nele Vandermaesen
发明人： Christopher John Love , Ludwig Paul Cooymans , Nele Vandermaesen
IPC分类号： A61K31/519 , C07D487/04 , A61P7/12 , A61P25/28 , A61P25/16 , A61P25/18 , A61P25/24 , A61P37/06 , A61P17/00 , A61P3/10 , A61P35/00
CPC分类号： C07D487/04
摘要： This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; C1-6alkyl substituted with formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl or C1-6alkylcarbonyloxy; X represents a direct bond; —(CH2)n3— or —(CH2)n4—X1a—X1b—; R2 represents an optionally substituted cyclic system; provided that N,3-diphenyl-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-amine is not included; their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及下式的化合物：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表示苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; R1表示氢; 芳基; 甲酰基 C 1-6烷基羰基; C 1-6烷基; C 1-6烷氧基羰基; 被甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基或C 1-6烷基羰氧基取代的C 1-6烷基; X表示直接键; - （CH 2）n3-或 - （CH 2）n4-X1a-X1b-; R2表示任选取代的环状体系; 条件是不包括N，3-二苯基-3H-1,2,3-三唑并[4,5-d]嘧啶-5-胺; 其用途，包含它们的药物组合物及其制备方法。

8. 发明申请

US20070203189A1 2-Amino-4,5-Trisubstituted Thiazolyl Derivatives 有权
标题翻译： 2-氨基-4,5-三取代噻唑衍生物
公开(公告)号：US20070203189A1
公开(公告)日：2007-08-30
申请号：US11742741
申请日：2007-05-01
申请人： Christopher Love , Guy Van Lommen , Julien Georges Doyon , Jean-Pierre Bongartz , Marcel Van der Aa , Robert Hendrickx , Peter Jacobus Antonius Buijnsters , Ludwig Cooymans , Nele Vandermaesen , Erwin Coesemans , Gustaaf Boeckx
发明人： Christopher Love , Guy Van Lommen , Julien Georges Doyon , Jean-Pierre Bongartz , Marcel Van der Aa , Robert Hendrickx , Peter Jacobus Antonius Buijnsters , Ludwig Cooymans , Nele Vandermaesen , Erwin Coesemans , Gustaaf Boeckx
IPC分类号： A61K31/454 , A61K31/427 , A61K31/426 , C07D417/02
CPC分类号： C07D417/04 , C07D277/42 , C07D471/04
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; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(═O)2—; mono- or di(C1-6alkyl)aminoS(═O)2; —C(═N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula L is optionally 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 inflammatory and/or auto-immune 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; C 1-6烷基羰基; C 1-6烷氧基羰基; 氨基羰基; 用羟基，羧基，氰基，氨基，被哌啶取代的氨基，被C 1-4烷基取代的哌啶基取代的氨基，单或二（ C 1-6烷基）氨基，氨基羰基，一或二（C 1-6烷基）氨基羰基，C 1-6烷氧基羰基， C 1-6烷基氧基，哌啶基，哌嗪基，吗啉基，硫代吗啉基; 多卤代1-4烷基; 氰基; 氨基; 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; 氨基-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C 3-6环烷基，苯基，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是式L的基团是任选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介导的炎症和/或自身免疫疾病的药物。

9. 发明申请

US20060205721A1 Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors 有权
公开(公告)号：US20060205721A1
公开(公告)日：2006-09-14
申请号：US10564844
申请日：2004-07-12
申请人： Eddy Edgard Freyne , Christopher Love , Ludwig Cooymans , Nele Vandermaesen , Peter Jacobus Buijinsters
发明人： Eddy Edgard Freyne , Christopher Love , Ludwig Cooymans , Nele Vandermaesen , Peter Jacobus Buijinsters
IPC分类号： A61K31/5377 , A61K31/519 , C07D487/02
CPC分类号： C07D487/04
摘要： This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; C1-6alkyl substituted with formyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; or C1-6alkyloxyC1-6alkylcarbonyl optionally substituted with C1-6alkyloxycarbonyl; X represents a direct bond; —(CH2)n3— or —(CH2)n4—X1a—X1b—; R2 represents C3-7cycloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatom selected from O, S or N; benzoxazolyl or a radical of formula wherein said R2 substituent may optionally be substituted; R3 represents halo; hydroxy; optionally substituted C1-6alkyl; C2-6alkenyl or C2-6alkynyl, each optionally substituted; optionally substituted polyhaloC1-6alkyl; optionally substituted C1-6alkyloxy; optionally substituted polyhaloC1-6alkyloxy; C1-6alkylthio; polyhaloC1-6alkylthio; C1-6alkyl-oxycarbonyl; C1-6alkylcarbonyloxy; C1-6alkylcarbonyl; polyhaloC1-6alkylcarbonyl; cyano; carboxyl; aryloxy; arylthio; arylcarbonyl; NR6bR7b; C(═O)—NR6bR7b; —NR5—C(═O)—NR6bR7b; —NR5—C(═O)—R5; —S(═O)n1—R8b; —NR5—S(═O)n1—R8b; —S—CN; —NR5—CN; R4 represents hydrogen; halo; hydroxy; optionally substituted C1-4alkyl; C2-4alkenyl or C2-4alkynyl, each optionally substituted; polyhaloC1-3alkyl; optionally substituted C1-4alkyloxy; polyhaloC1-3alkyloxy; C1-4alkylthio; polyhaloC1-3alkylthio; C1-4alkyloxycarbonyl; C1-4alkylcarbonyloxy; C1-4alkylcarbonyl; polyhaloC1-4alkylcarbonyl; nitro; cyano; carboxyl; NR10R11; C(═O)NR10R11; —NR5—C(═O)—NR10R11; —NR5—C(═O)—R5; —S(═O)Sn1—R12; —NR5—S(═O)n1—R12; —S—CN; —NR5—CN; their use, pharmaceutical compositions comprising them and processes for their preparation.

10. 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。

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