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1. 发明授权

US08981094B2 Piperidine/piperazine derivatives 有权
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.

2. 发明申请

US20100190789A1 PIPERIDINE/PIPERAZINE DERIVATIVES 有权
公开(公告)号：US20100190789A1
公开(公告)日：2010-07-29
申请号：US12663013
申请日：2008-06-06
申请人： Jean-Pierre Andre 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 , Peter Vladimirivich Davidenko
发明人： Jean-Pierre Andre 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 , Peter Vladimirivich Davidenko
IPC分类号： A61K31/5377 , C07D241/04 , A61K31/495 , C07D401/12 , A61K31/496 , C07D403/10 , C07D405/12 , C07D403/12 , C07D413/12 , C07D211/34 , A61K31/451 , A61P3/04 , A61P3/06 , A61P3/10 , A61P1/16
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)-Z 2—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)—NR—Z2—; —C(═O)—NR—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 O 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.

3. 发明授权

US08835437B2 Piperidine/piperazine derivatives 有权
标题翻译：哌啶/哌嗪衍生物
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。

4. 发明申请

US20100216809A1 PIPERIDINE/PIPERAZINE DERIVATIVES 有权
标题翻译：哌啶/哌嗪衍生物
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。

5. 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。

6. 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

7. 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.

8. 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。

9. 发明授权

US06867207B2 IL-5 inhibiting 6-azauracil derivatives 失效
标题翻译： IL-5抑制6-氮尿嘧啶衍生物
公开(公告)号：US06867207B2
公开(公告)日：2005-03-15
申请号：US09891888
申请日：2001-06-26
申请人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Marc Gaston Venet , Gustaaf Maria Boeckx
发明人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Marc Gaston Venet , Gustaaf Maria Boeckx
IPC分类号： A61P37/08 , C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D253/065 , A61K31/53 , A61K17/00
CPC分类号： C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR3 or a direct bond; R1 is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C1-6alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R2 is aryl, Het1, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C1-4alkyl; R4 and R5 independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6akylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6 or NR7R8; R6 is substituted sulfonyl or sulfinyl; R7 and R8 are hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R9 and R10 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, carboxyl, C1-4alkyloxycarbonyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R12 and R13 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl and R6; aryl is optionally substituted phenyl; Het1, Het2 and Het3 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
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，p和q分别为0,1,2,3或4，q也为5; X是O，S，NR 3或直接键; R 1是氢，羟基，卤素，任选取代的氨基，任选取代的C 1-6烷基，C 1-6烷氧基，C 3-7环烷基或芳基; R 2是芳基，Het 1，C 3-7环烷基，任选取代的C 1-6烷基; 并且如果X是O，S或NR 3，则R 2也可以是羰基或硫代羰基连接的取代基; R 3是氢或C 1-4烷基; R 4和R 5独立地是任选取代的C 1-6烷基，卤素，羟基，巯基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基羰基氧基，芳基，氰基，硝基，Het 3，或NR 7 R 8; R 6是取代的磺酰基或亚磺酰基; R 7和R 8是氢，任选取代的C 1-4烷基，芳基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 9和R 10各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 11是羟基，巯基，氰基，硝基，卤素，三卤代甲基，C 1-4烷氧基，羧基，C 1-4烷氧基羰基，三卤代C 1-4烷基磺酰氧基，R 6，NR 7 R 8，C（= O） NR 7 R 8，芳基，芳氧基，芳基羰基，C 3-7环烷基，C 3-7环烷氧基，邻苯二甲酰亚胺-2-基，Het 3和C（= O）Het 3; R 12和R 13各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基和R 6; 芳基是任选取代的苯基; Het <1>，Het <

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