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1. 发明申请

US20050090495A1 Novel IL-5 inhibiting 6-azauracil derivatives for marking and identifying receptors and imaging organs 审中-公开
公开(公告)号：US20050090495A1
公开(公告)日：2005-04-28
申请号：US10671205
申请日：2003-09-25
申请人： Jean Lacrampe , Eddy Freyne , Marc Venet , Gustaaf Boeckx
发明人： Jean Lacrampe , Eddy Freyne , Marc Venet , Gustaaf Boeckx
IPC分类号： A61P37/08 , C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , A61K31/53
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 C1-4allyl; R4 and R5 independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, 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)NR7R3, 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.

2. 发明申请

US20070249691A1 Mercaptoimidazoles as Ccr2 Receptor Antagonists 审中-公开
标题翻译：巯基咪唑作为Ccr2受体拮抗剂
公开(公告)号：US20070249691A1
公开(公告)日：2007-10-25
申请号：US11569268
申请日：2005-05-24
申请人： Gustaaf Boeckx , Guy Rosalia Eugeen Van Lommen , Julien Georges Pierre-Olivier Doyon , Erwin Coesemans
发明人： Gustaaf Boeckx , Guy Rosalia Eugeen Van Lommen , Julien Georges Pierre-Olivier Doyon , Erwin Coesemans
IPC分类号： A61K31/4164 , A61K31/421 , A61K31/4245 , A61K31/426 , A61P29/00 , C07D233/84 , C07D261/06 , C07D271/10 , C07D277/18
CPC分类号： C07C211/29 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/4439 , A61K31/501 , A61K31/502 , C07D233/84 , C07D233/88 , C07D401/04 , C07D401/06 , C07D403/06 , C07D409/04 , C07D409/06 , C07D413/04 , C07D413/06 , C07D417/06
摘要： The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine, a polymorphic form or a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, optionally substituted C1-6alkyl, C(═O)—O—R5, C(═O)—NR6aR6b, C(═S)—NR6aR6b, S(═O)2—NR6aR6b or C(═O)—R7; R4 represents hydrogen or C1-6alkyl; n is 1, 2, 3, 4 or 5; Z represents a cyclic ring system. The invention also relates to processes for preparing the compounds of formula (I), their use as CCR2 antagonists and pharmaceutical compositions comprising them.
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，多晶型或其立体化学异构形式，其中R 1表示氢， C 1-6烷基，C 3-7环烷基，C 1-6烷氧基C 1-6烷基，二（C 1-6烷基）氨基C 1-6烷基，芳基或杂芳基; 每个R 2独立地代表卤素，C 1-6烷基，C 1-6烷氧基，C 1-6 烷硫基，多卤C 1-6烷基，多卤C 1-6烷氧基，氰基，氨基羰基，氨基，单或二（C 1-4）烷基）氨基，硝基，芳基或芳氧基; R 3表示氢，氰基，任选取代的C 1-6烷基，C（-O）-OR 5，C（O） -NR 6 C 6b，C（-S）-NR 6a R 6b，S（-O） C 1 -C 6烷基或C（-O）-R 7; R 4表示氢或C 1-6烷基; n为1,2,3,4或5; Z表示环状体系。本发明还涉及制备式（I）化合物的方法，它们作为CCR2拮抗剂的用途和包含它们的药物组合物。

3. 发明申请

US20070244138A1 Mercaptoimidazoles as Ccr2 Receptor Antagonists 审中-公开
标题翻译：巯基咪唑作为Ccr2受体拮抗剂
公开(公告)号：US20070244138A1
公开(公告)日：2007-10-18
申请号：US11569321
申请日：2005-05-24
申请人： Gustaaf Boeckx , Guy Van Lommen , Julien Georges Doyon , Erwin Coesemans
发明人： Gustaaf Boeckx , Guy Van Lommen , Julien Georges Doyon , Erwin Coesemans
IPC分类号： A61K31/41 , A61K31/505 , A61P29/00 , C07D233/00 , C07D239/02 , C07D257/04 , C07D271/06 , C07D271/10
CPC分类号： C07D413/04 , C07D233/84 , C07D401/04 , C07D403/04 , C07D405/04 , C07D417/04
摘要： The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl) amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, optionally substituted C1-6alkyl, C(═O)—O—R5, C(═O)—NR6aR6b, C(═S)—NR6aR6b, S(═O)2—NR6aR6b or C(═O)—R7; R4 represents hydrogen or C1-6alkyl; n is 1, 2, 3, 4 or 5; Z represents a cyclic ring system. The invention also relates to processes for preparing the compounds of formula (I), their use as CCR2 antagonists and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）化合物的N-氧化物，其药学上可接受的加成盐，季胺或其立体化学异构形式，其中R 1表示氢，C 1〜 C 1-6烷基，C 3-7环烷基，C 1-6烷基氧基C 1-6烷基，二（C 1 -C 6）烷基，烷基，芳基或杂芳基; 每个R 2独立地代表卤素，C 1-6烷基，C 1-6烷氧基，C 1-6 烷硫基，多卤C 1-6烷基，多卤C 1-6烷氧基，氰基，氨基羰基，氨基，一或二（C 1-4）烷基）氨基，硝基，芳基或芳氧基; R 3表示氢，氰基，任选取代的C 1-6烷基，C（-O）-OR 5，C（O） -NR 6 C 6b，C（-S）-NR 6a R 6b，S（-O） C 1 -C 6烷基或C（-O）-R 7; R 4表示氢或C 1-6烷基; n为1,2,3,4或5; Z表示环状体系。本发明还涉及制备式（I）化合物的方法，其用作CCR2拮抗剂和包含它们的药物组合物。

4. 发明申请

US20070167456A1 Mercaptoimidazoles as ccr2 receptor antagonists 审中-公开
标题翻译：巯基咪唑作为ccr2受体拮抗剂
公开(公告)号：US20070167456A1
公开(公告)日：2007-07-19
申请号：US11572770
申请日：2005-08-10
申请人： Guy Lommen , Gustaaf Boeckx
发明人： Guy Lommen , Gustaaf Boeckx
IPC分类号： A61K31/506 , A61K31/498 , A61K31/4439 , A61K31/427 , A61K31/433 , A61K31/4245 , A61K31/422 , A61K31/4196 , A61K31/4178 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D403/12 , C07D233/90 , C07D401/12 , C07D405/12 , C07D413/12
摘要： The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents cyano, C(═O)—O—R5, C(═O)—NR6aR6b or C(═O)—R7; or a cyclic ring system; R4 represents hydrogen or C1-6alkyl; n is 1, 2, 3, 4 or 5; R10 represents hydrogen, C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, arylcarbonyl, heteroarylcarbonyl, —C(═O)—NH—R5, —C(═S)—NH—R5 or —S(═O)2—R5. The invention also relates to processes for preparing the compounds of formula (I), their use as CCR2 antagonists and pharmaceutical compositions comprising them.
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，其中R 1表示氢，C 1〜 C 1-6烷基，C 3-7环烷基，C 1-6烷基氧基C 1-6烷基，二（C 1 -C 6）烷基，烷基，芳基或杂芳基; 每个R 2独立地代表卤素，C 1-6烷基，C 1-6烷氧基，C 1-6 烷硫基，多卤C 1-6烷基，多卤C 1-6烷氧基，氰基，氨基羰基，氨基，单或二（C 1-4）烷基）氨基，硝基，芳基或芳氧基; R 3表示氰基，C（= O）-OR 5，C（-O）-NR 6a R 6b， SUB或C（-O）-R 7; 或环状体系; R 4表示氢或C 1-6烷基; n为1,2,3,4或5; R 10表示氢，C 1-6烷基，C 1-6烷基羰基，C 1-6烷基氧基羰基，芳基羰基，杂芳基羰基，-C（-O）-NH-R 5，-C（-S）-NH-R 5或-S（-O） SUB> 2 5 。本发明还涉及制备式（I）化合物的方法，它们作为CCR2拮抗剂的用途和包含它们的药物组合物。

5. 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。

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