公开(公告)号：US20100216809A1

公开(公告)日：2010-08-26

申请号：US12663009

申请日：2008-06-05

申请人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

发明人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

IPC分类号： A61K31/506 ,  A61K31/496 ,  A61K31/454 ,  C07D403/10 ,  C07D413/10 ,  C07D513/04 ,  C07D487/04 ,  C07D401/10 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P1/16

CPC分类号： C07D513/04 ,  C07D231/12 ,  C07D239/26 ,  C07D239/42 ,  C07D249/08 ,  C07D249/12 ,  C07D271/06 ,  C07D271/10 ,  C07D271/107 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D487/04

摘要： The invention further 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 —NRx—C(═O)—; —Z—C(═O)—; —Z—NRx—C(═O)—; —S(═O)p-; C(═S)—; —NRx—C(═S)—; —Z—C(═S)—; —Z—NRx—C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 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-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; 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 of said compounds.

摘要翻译： 本发明还涉及式（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-NR x -C（= O） - ; -Z-C（= O） - ; -Z-NRx-C（= O） - ; -S（= O）p-; C（═S） - ; -NR x -C（= S） - ; -Z-C（= S） - ; -Z-NRx-C（= S） - ; -O-C（= O） - ; -C（= O）-C（= O） - ; R1表示含有至少2个杂原子的5元单环杂环; 6元芳族单环杂环; 或含有至少2个与苯基，环己基或5或6元杂环稠合的杂原子的5元杂环; 其中每个所述杂环可任选被取代; R2表示R3; R 3表示C 3-6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-苯并二恶基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或6-元芳香杂环可以任选被取代; 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用作所述化合物的药物。

公开(公告)号：US08981094B2

公开(公告)日：2015-03-17

申请号：US12663013

申请日：2008-06-06

申请人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Gustaaf Maria Boeckx ,  Petr Vladimirivich Davidenko

发明人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Gustaaf Maria Boeckx ,  Petr Vladimirivich Davidenko

IPC分类号： C07D211/00 ,  C07D241/04 ,  C07D295/00 ,  C07D401/00 ,  C07D403/00 ,  C07D295/205 ,  C07D207/09 ,  C07D211/26 ,  C07D211/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D233/18 ,  C07D295/192 ,  C07D295/21 ,  C07D295/215 ,  C07D295/24 ,  C07D295/26 ,  C07D307/52 ,  C07D307/79 ,  C07D309/04 ,  C07D317/58 ,  C07D333/24

CPC分类号： C07D295/205 ,  C07D207/09 ,  C07D211/26 ,  C07D211/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D233/18 ,  C07D295/192 ,  C07D295/21 ,  C07D295/215 ,  C07D295/24 ,  C07D295/26 ,  C07D307/52 ,  C07D307/79 ,  C07D309/04 ,  C07D317/58 ,  C07D333/24

摘要： 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 —C(═O)—; —O—C(═O)—; C(═O)—C(═O)—; —NRx—C(═O)—; —Z1—C(O)—; —Z1—NRx—C(═O)—; —C(═O)—Z1—; —NRx—C(═O)—Z1—; —S(═O)p-; —C(═S)—; —NRx—C(═S)—; —Z1—C(═S)—; —Z1—NRx—C(═S)—; —C(═S)—Z1-; —NRx—C(═S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z2—NRy—C(=0)-; —NRx—C(=0)-Z2—NRy—C(=0)-O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(═O)—O—Z2—O—C(═O)—; —NRx—C(═O)—Z2—C(═O)—NRy—; —NRx—C(═O)—Z2—NRy—C(=0)-NRy—; —C(═O)—Z2—; —C(═O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)-NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cycloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents —NRX—C(═O)—Z2—; —NRx—C(=0)-Z2—NRy; —NRX—C(═O)—Z2—C(═O)—NRy—; —C(═O)—Z2—; —NRx—C(=0)-Z2—NRy—C(=0)-NRy—; —C(═O)—NRX—Z2—; —C(═O)—NRX—O—Z2—; or —C(=0)-NRx—Z2—NRy—; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents —O—C(═O)—; the R2 represents R3; and provided that (A) is 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 of said compounds.

公开(公告)号：US08835437B2

公开(公告)日：2014-09-16

申请号：US12663009

申请日：2008-06-05

申请人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Nestor Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

发明人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Nestor Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

IPC分类号： A61K31/496 ,  C07D487/04 ,  C07D513/04 ,  C07D239/42 ,  C07D239/26 ,  A61K31/506 ,  A61K31/454 ,  C07D231/12 ,  C07D249/08 ,  C07D249/12 ,  C07D271/06 ,  C07D401/10

CPC分类号： C07D513/04 ,  C07D231/12 ,  C07D239/26 ,  C07D239/42 ,  C07D249/08 ,  C07D249/12 ,  C07D271/06 ,  C07D271/10 ,  C07D271/107 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D487/04

摘要： The invention further 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 —NRx—C(═O)—; —Z—C(═O)—; —Z—NRx—C(═O)—; —S(═O)p—; C(═S)—; —NRx—C(═S)—; —Z—C(═S)—; —Z—NRx—C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 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-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; 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 of said compounds.

摘要翻译： 本发明还涉及式（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-NR x -C（= O） - ; -Z-C（= O） - ; -Z-NRx-C（= O） - ; -S（= O）p-; C（═S） - ; -NR x -C（= S） - ; -Z-C（= S） - ; -Z-NRx-C（= S） - ; -O-C（= O） - ; -C（= O）-C（= O） - ; R1表示含有至少2个杂原子的5元单环杂环; 6元芳族单环杂环; 或含有至少2个与苯基，环己基或5或6元杂环稠合的杂原子的5元杂环; 其中每个所述杂环可任选被取代; R2表示R3; R 3表示C 3-6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-苯并二恶基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或6-元芳香杂环可以任选被取代; 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用作所述化合物的药物。

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。

公开(公告)号：US08946228B2

公开(公告)日：2015-02-03

申请号：US12663011

申请日：2008-06-06

申请人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Petr Vladimirivich Davidenko

发明人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Petr Vladimirivich Davidenko

IPC分类号： A61K31/4965 ,  C07D241/04 ,  C07D295/00 ,  A61K31/451 ,  A61K31/495 ,  C07D207/323 ,  C07D211/26 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D235/18 ,  C07D249/08 ,  C07D257/04 ,  C07D263/34 ,  C07D277/56 ,  C07D279/02 ,  C07D279/12 ,  C07D295/20 ,  C07D307/54 ,  C07D319/18 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

CPC分类号： 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

摘要： The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof, and 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.

摘要翻译： 本发明涉及式（I）的DGAT抑制剂，包括其任何立体化学异构形式，其N-氧化物，其药学上可接受的盐或其溶剂合物，以及制备这些化合物的方法，包含所述化合物的药物组合物 作为所述化合物作为DGAT抑制剂的药物使用。

公开(公告)号：US08633197B2

公开(公告)日：2014-01-21

申请号：US12663007

申请日：2008-06-05

申请人： Jean-Pierre André Marc Bongartz ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Christophe Francis Robert Nestor Buyck

发明人： Jean-Pierre André Marc Bongartz ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Christophe Francis Robert Nestor Buyck

IPC分类号： A61K31/4965 ,  C07D241/04 ,  C07D295/00

CPC分类号： C07D295/215 ,  C07D231/12

摘要： The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof, and methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

摘要翻译： 本发明涉及一种DGAT抑制剂，其包括其任何立体化学异构形式，其N-氧化物，其药学上可接受的盐或其溶剂合物，以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用作 所述化合物的药物。

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