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1. 发明授权

US07514445B2 Heteroaryl amines as glycogen synthase kinase 3β inhibitors (GSK3 inhibitors) 有权
标题翻译：杂芳基胺作为糖原合酶激酶3β抑制剂（GSK3抑制剂）
公开(公告)号：US07514445B2
公开(公告)日：2009-04-07
申请号：US10493452
申请日：2002-10-29
申请人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts , Christopher John Love , Paul Adriaan Jan Janssen , Paulus Joannes Lewi , Jan Heeres , Marc René de Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Koen Jeanne Alfons Van Aken , Gaston Stanislas Marcella Diels
发明人： Eddy Jean Edgard Freyne , Peter Jacobus Johannes Antonius Buijnsters , Marc Willems , Werner Constant Johan Embrechts , Christopher John Love , Paul Adriaan Jan Janssen , Paulus Joannes Lewi , Jan Heeres , Marc René de Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Koen Jeanne Alfons Van Aken , Gaston Stanislas Marcella Diels
IPC分类号： A61K31/506 , A61P3/10 , A61P25/28 , A61P25/02 , C07D403/06 , C07D403/12 , C07D403/14
CPC分类号： C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
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 is a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21—C1-6alkyl; R21—O—; R21—S—; R21—C(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7—C(═NH)R21; R4 is an optionally substituted heterocycle provided that —X—R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式的化合物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是6-元杂环; R1是氢; 芳基; 甲酰基 C 1-6烷基羰基; 任选取代的C 1-6烷基; C 1-6烷氧基羰基; 任选取代的C 1-6烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是直接键或连接原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，所述基团中的每一个可任选被取代; R3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 2-6烯基或C 2-6炔基; C 1-6烷氧基; C 1-6烷硫基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; 羧基; 氰基; 硝基氨基; 单或二（C 1-6烷基）氨基; 多卤代C 1-6烷基; 多卤代C 1-6烷氧基; 多卤代C 1-6烷硫基; R21; R21-C1-6烷基; R21-O-; R21-S-; R21-C（-O） - ; R21-S（-O）p-; R7-S（-O）p-; R7-S（-O）p-NH-; R21-S（-O）p-NH-; R7-C（-O） - ; -NHC（-O）H; -C（-O）NHNH 2; R7-C（-O）-NH-; R 21 -C（-O）-NH-; -C（ - NH）R 7 -C（-NH）R 21; R4是任选取代的杂环，条件是-X-R 2和/或R 3不是氢; 其用途，包含它们的药物组合物及其制备方法。

2. 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。

3. 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。

4. 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。

5. 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。

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

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。

8. 发明授权

US06395742B1 2,4-diaminopyrimidine derivatives 有权
标题翻译： 2,4-二氨基嘧啶衍生物
公开(公告)号：US06395742B1
公开(公告)日：2002-05-28
申请号：US09667458
申请日：2000-09-22
申请人： Jean-Paul René Marie André Bosmans , Christopher John Love , Guy Rosalia Eugène Van Lommen
发明人： Jean-Paul René Marie André Bosmans , Christopher John Love , Guy Rosalia Eugène Van Lommen
IPC分类号： C07D40112
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl or C3-6alkenediyl; R1 is hydrogen or C1-4alkyl; R2 and R3 each independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; or R2 and R3 may also be taken together with the nitrogen atom to which they are attached, thus forming a pyrrolidine, a piperidine or a perhydro azepine ring; R4 is hydrogen or halo; Q is aryl, aryloxy, di(aryl)methyl or heteroaryl; aryl is naphthyl or phenyl, said naphthyl and phenyl may optionally be substituted; and heteroaryl is quinolinyl, isoquinolinyl, pyridinyl, thienyl, indolyl, 2,3-dihydro-1,4-benzodioxinyl, 2,3-dihydro-benzofuranyl or benzodioxolanyl; said heteroaryls may optionally be substituted; it further relates to processes for their preparation, compositions comprising them as well as their use as a medicine; compounds of formula (I) containing a radioactive isotope; a process of marking dopamine D4 receptor sites; and a process for imaging an organ are disclosed.
摘要翻译：本发明涉及配制N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中Alk是C 1-6烷二基或C 3-6亚烯基; R1是氢或C1-4烷基; R2和R3各自独立地为氢，C1-6烷基或C3-7环烷基; 或者R 2和R 3也可以与它们所连接的氮原子一起，从而形成吡咯烷，哌啶或全氢吖庚因环; R4是氢或卤素; Q是芳基，芳氧基，二（芳基）甲基或杂芳基; 芳基是萘基或苯基，所述萘基和苯基可任选被取代; 异喹啉基，吡啶基，噻吩基，吲哚基，2,3-二氢-1,4-苯并二氧杂环戊烯基，2,3-二氢 - 苯并呋喃基或苯并二氧杂环戊烷基; 所述杂芳基可任选被取代; 它还涉及它们的制备方法，包含它们的组合物以及它们作为药物的用途; 含有放射性同位素的式（I）化合物; 标记多巴胺D4受体位点的过程; 并且公开了用于成像器官的方法。

9. 发明授权

US06800628B2 N-substituted 4-((-4′-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties 有权
标题翻译：具有胃动力学性质的N-取代的4 - （（ - 4'-氨基苯甲酰基） - 氧基甲基） - 哌啶
公开(公告)号：US06800628B2
公开(公告)日：2004-10-05
申请号：US10299317
申请日：2002-11-19
申请人： Jean-Paul René Marie Bosmans , Christopher John Love , Marc Gustaaf Celine Verdonck , Joannes Adrianus Jacobus Schuurkes
发明人： Jean-Paul René Marie Bosmans , Christopher John Love , Marc Gustaaf Celine Verdonck , Joannes Adrianus Jacobus Schuurkes
IPC分类号： A61K31501
CPC分类号： C07D401/06 , C07D211/22 , C07D401/12 , C07D405/12 , C07D405/14 , C07D417/14
摘要： This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-26alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R3 is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula —Alk—R4, —Alk—NR5R6, 1-R6-4-piperidinyl, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; R4 is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Ar—, di(Ar)methyl, Ar-oxy- or Het1; R5 is hydrogen or C1-6alkyl; R6 is Het2; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, Ar or Het2; X is O, S, SO2 or NR8; said R8 being hydrogen, C1-6alkyl or Ar; R9 is hydrogen, C1-6alkyl, C3-6cyclo-alkyl, Ar, ArC1-6alkyl, di(Ar)methyl, C1-6alkyloxy or hydroxy; Y is NR10 or a direct bond; said R10 being hydrogen, C1-6alkyl or Ar; R11 and R12 each independently are hydrogen, C1-6alkyl, C3-6cycloalkyl, Ar or ArC1-6alkyl, or R11 and R12 combined with the nitrogen atom bearing R11 and R12 may form a pyrrolidinyl or piperidinyl ring both being optionally substituted with C1-6alkyl, amino or mono or di(C1-6alkyl)amino, or said R11 and R12 combined with the nitrogen bearing R11 and R12 may form a piperazinyl or 4-morpholinyl radical both being optionally substituted with C1-6alkyl. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
摘要翻译：本发明涉及配制N-氧化物形式的化合物，其药学上可接受的酸加成盐及其立体化学异构形式，其中R 1为C 1-6烷氧基，C 2-6烯氧基或C 2-6-26炔氧基; R 2是氢或C 1-6烷氧基，或者当R 1和R 2一起可以形成下式的二价基团时，其中在所述二价基团中，一个或两个氢原子可以被C 1-6烷基取代，R 3是氢或卤素; L是C3-6环烷基，C5-6环烷酮，任选被芳基取代的C 2-6链烯基，或L是式-Alk-R 4，-Alk-NR 5 R 6，1-R 6 其中每个Alk为C1（= O）-R9，-Alk-YC（= O）-NR11R12，其中每个Alk为C1 -12烷二基; R 4是氢，C 1-6烷基磺酰基氨基，C 3-6环烷基，C 5-6环烷酮，Ar-，二（Ar）甲基，Ar-氧基或Het 1。 R 5是氢或C 1-6烷基; R 6是Het 2; R 7是氢，C 1-6烷基，羟基C 1-6烷基，C 3-6环烷基，Ar或Het 2; X是O，S，SO 2或NR 8; 所述R 8为氢，C 1-6烷基或Ar; R 9是氢，C 1-6烷基，C 3-6环烷基，Ar，ArC 1-6烷基，二（Ar）甲基，C 1-6烷氧基或羟基; Y是NR 10或直接键; 所述R 10为氢，C 1-6烷基或Ar; R 11和R 12各自独立地为氢，C 1-6烷基，C 3-6环烷基，Ar或ArC 1-6烷基，或R 11和R 12与带有R 11和R 10的氮原子结合可以形成任选被C

10. 发明授权

US06291481B1 N-substituted 4-(4′-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties 有权
标题翻译： N-取代的4-（4'-氨基苯甲酰基） - 氧甲基） - 哌啶具有胃动力学性质
公开(公告)号：US06291481B1
公开(公告)日：2001-09-18
申请号：US09125901
申请日：1998-08-27
申请人： Jean-Paul René Marie Bosmans , Christopher John Love , Marc Gustaaf Celine Verdonck , Joannes Adrianus Jacobus Schuurkes
发明人： Jean-Paul René Marie Bosmans , Christopher John Love , Marc Gustaaf Celine Verdonck , Joannes Adrianus Jacobus Schuurkes
IPC分类号： A61K314523
CPC分类号： C07D401/06 , C07D211/22 , C07D401/12 , C07D405/12 , C07D405/14 , C07D417/14
摘要： Compounds of formula I the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the substituents are as described in the specification, and process for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impairment of gastric emptying.
摘要翻译：式I化合物为N-氧化物形式，其药学上可接受的酸加成盐及其立体化学异构形式，其中取代基如说明书所述，制备所述产物的方法，包含所述产物的制剂及其作为药物的用途是特别是用于治疗与胃排空障碍相关的病症。

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