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11. 发明授权

US6159982A 2,4-diaminopyrimidine derivates as dopamine D4 receptor antagonist 有权
标题翻译： 2,4-二氨基嘧啶衍生物作为多巴胺D4受体拮抗剂
公开(公告)号：US6159982A
公开(公告)日：2000-12-12
申请号：US180364
申请日：1998-11-09
申请人： Jean-Paul Rene Marie Andre Bosmans , Christopher John Love , Guy Rosalia Eugene Van Lommen
发明人： Jean-Paul Rene Marie Andre Bosmans , Christopher John Love , Guy Rosalia Eugene Van Lommen
IPC分类号： A61K31/505 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein Alk is C.sub.1-6 alkanediyl or C.sub.3-6 alkenediyl; R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 and R.sup.3 each independently are hydrogen, C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; or R.sup.2 and R.sup.3 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; R.sup.4 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 D.sub.4 receptor sites; and a process for imaging an organ are disclosed.
摘要翻译： PCT No.PCT / EP97 / 02506 Sec。 371日期：1998年11月9日 102（e）1998年11月9日PCT PCT 1997年5月2日PCT公布。公开号WO97 / 43279 日期：1997年11月20日本发明涉及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; 所述杂芳基可以任选被取代：它还涉及其制备方法，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。

12. 发明授权

US08431704B2 Quinoline or isoquinoline substituted P2X7 antagonists 有权
标题翻译：喹啉或异喹啉取代的P2X7拮抗剂
公开(公告)号：US08431704B2
公开(公告)日：2013-04-30
申请号：US12988891
申请日：2009-04-21
申请人： Christopher John Love , Joseph Elisabeth Leenaerts , Ludwig Paul Cooymans , Donald Alec Lebsack , Bryan James Branstetter , Jason Christopher Rech , Elizabeth Ann Gleason , Jennifer Diane Venable , Danielle Wiener , Deborah Margaret Smith , James Guy Breitenbucher
发明人： Christopher John Love , Joseph Elisabeth Leenaerts , Ludwig Paul Cooymans , Donald Alec Lebsack , Bryan James Branstetter , Jason Christopher Rech , Elizabeth Ann Gleason , Jennifer Diane Venable , Danielle Wiener , Deborah Margaret Smith , James Guy Breitenbucher
IPC分类号： C07D215/38
CPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/08
摘要： The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I).
摘要翻译：本发明涉及具有P2X7拮抗性质的新型式（I）化合物，包含这些化合物的药物组合物，用于制备这些化合物的化学方法及其用于治疗或预防与动物中P2X7受体活性有关的疾病的用途，特别是人类。（一世）。

13. 发明申请

US20100222574A1 CYCLIC ANILINO - PYRIDINOTRIAZINES 有权
标题翻译： CYCLIC ANILINO - PYRIDINOTRIAZINES
公开(公告)号：US20100222574A1
公开(公告)日：2010-09-02
申请号：US11993237
申请日：2006-06-26
申请人： Frederik Jan Rita Rombouts , Christopher John Love , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Tongfei Wu
发明人： Frederik Jan Rita Rombouts , Christopher John Love , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Tongfei Wu
IPC分类号： C07D471/14
CPC分类号： C07D487/18 , C07D251/16 , C07D401/04 , C07D471/18 , C07D471/22 , C07D487/08
摘要： The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents 1, n represents 1, Z represents N or C, in particular N; —X1— represents C1-4alkyl, in particular methyl; —X2— represents —C1-4alkyl- or —C1-4alkyl-NR7—, in particular propyl, -ethyl-NR7— or -propyl-NR7—; —Y— represents-NR2—C1-6alkyl-CO—NR4—, -Het1-C1-6alkyl-CO—NR5— or -Het2-CO—NR6— and wherein the —C1-6alkyl-linker of —NR2—C1-6alkyl-CO—NR4— or -Het1-C1-6alkyl-CO—NR5— is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl; R1 represents hydrogen, chloro, fluoro or bromo; R2 represents —C1-4alkyl-, in particular ethyl or methyl; R7 represents hydrogen; R8 represents hydrogen; R4, R5 and R6 represent hydrogen; Het1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het2 selected from pyrrolidinyl or piperidinyl, in particular pyrrolidinyl wherein said pyrrolidinyl is optionally substituted with hydroxy.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中m表示1，n表示1，Z表示N或C，特别是N; -X1-表示C1-4烷基，特别是甲基; -X2-表示-C 1-4烷基 - 或-C 1-4烷基-NR 7 - ，特别是丙基， - 乙基-NR 7 - 或 - 丙基-NR 7 - ; -Y-表示-NR2-C1-6烷基-CO-NR4-，-Het1-C1-6烷基-CO-NR5-或-Het2-CO-NR6-，其中-NR2-C1- C 1-6烷基-CO-NR 4 - 或-Het 1 -C 1-6烷基-CO-NR 5 - 任选被一个或其中可能的两个或更多个选自羟基，卤素和苯基的取代基取代; R1代表氢，氯，氟或溴; R 2表示-C 1-4烷基，特别是乙基或甲基; R7代表氢; R8代表氢; R4，R5和R6代表氢; Het1选自哌嗪基或哌啶基，特别是哌嗪基; Het2选自吡咯烷基或哌啶基，特别是吡咯烷基，其中所述吡咯烷基任选被羟基取代。

14. 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。

15. 发明授权

US08778919B2 Cyclic anilino—pyridinotriazines 有权
标题翻译：环状苯胺基 - 吡啶并三嗪
公开(公告)号：US08778919B2
公开(公告)日：2014-07-15
申请号：US11993237
申请日：2006-06-26
申请人： Frederik Jan Rita Rombouts , Christopher John Love , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Tongfei Wu
发明人： Frederik Jan Rita Rombouts , Christopher John Love , Kristof Van Emelen , Sven Franciscus Anna Van Brandt , Tongfei Wu
IPC分类号： A61K31/33 , C07D487/00 , C07D255/02
CPC分类号： C07D487/18 , C07D251/16 , C07D401/04 , C07D471/18 , C07D471/22 , C07D487/08
摘要： The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents 1, n represents 1, Z represents N or C, in particular N; —X1— represents C1-4alkyl, in particular methyl; —X2— represents —C1-4alkyl- or —C1-4alkyl-NR7—, in particular propyl, -ethyl-NR7— or -propyl-NR7—; —Y— represents —NR2—C1-6alkyl-CO—NR4—, -Het1-C1-6alkyl-CO—NR5— or -Het2-CO—NR6— and wherein the —C1-6alkyl-linker of —NR2—C1-6alkyl-CO—NR4— or -Het1-C1-6alkyl-CO—NR5— is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl; R1 represents hydrogen, chloro, fluoro or bromo; R2 represents —C1-4alkyl-, in particular ethyl or methyl; R7 represents hydrogen; R8 represents hydrogen; R4, R5 and R6 represent hydrogen; Het1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het2 selected from pyrrolidinyl or piperidinyl, in particular pyrrolidinyl wherein said pyrrolidinyl is optionally substituted with hydroxy.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中m表示1，n表示1，Z表示N或C，特别是N; -X1-表示C1-4烷基，特别是甲基; -X2-表示-C 1-4烷基 - 或-C 1-4烷基-NR 7 - ，特别是丙基， - 乙基-NR 7 - 或 - 丙基-NR 7 - ; -Y-代表-NR2-C1-6烷基-CO-NR4-，-Het1-C1-6烷基-CO-NR5-或-Het2-CO-NR6-，其中-NR2-C1- C 1-6烷基-CO-NR 4 - 或-Het 1 -C 1-6烷基-CO-NR 5 - 任选被一个或其中可能的两个或更多个选自羟基，卤素和苯基的取代基取代; R1代表氢，氯，氟或溴; R 2表示-C 1-4烷基，特别是乙基或甲基; R7代表氢; R8代表氢; R4，R5和R6代表氢; Het1选自哌嗪基或哌啶基，特别是哌嗪基; Het2选自吡咯烷基或哌啶基，特别是吡咯烷基，其中所述吡咯烷基任选被羟基取代。

16. 发明申请

US20110092481A1 QUINOLINE OR ISOQUINOLINE SUBSTITUTED P2X7 ANTAGONISTS 有权
标题翻译：喹啉或异喹啉取代P2X7拮抗剂
公开(公告)号：US20110092481A1
公开(公告)日：2011-04-21
申请号：US12988891
申请日：2009-04-21
申请人： Christopher John Love , Joseph Elisabeth Leenaerts , Ludwig Paul Cooymans , Donald Alec Labsack , Bryan James Branstetter , Jason Christopher Rech , Elizabeth Ann Gleason , Jennifer Diane Venable , Danielle Wiener , Deborah Margaret Smith , James Guy Breitenbucher
发明人： Christopher John Love , Joseph Elisabeth Leenaerts , Ludwig Paul Cooymans , Donald Alec Labsack , Bryan James Branstetter , Jason Christopher Rech , Elizabeth Ann Gleason , Jennifer Diane Venable , Danielle Wiener , Deborah Margaret Smith , James Guy Breitenbucher
IPC分类号： A61K31/4709 , C07D401/14 , C07D413/14 , A61K31/553 , A61K31/55 , A61K31/5377 , A61K31/506 , A61K31/496 , A61K31/4725 , A61P43/00
CPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/08
摘要： The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I)
摘要翻译：本发明涉及具有P2X7拮抗性质的新型式（I）化合物，包含这些化合物的药物组合物，用于制备这些化合物的化学方法及其用于治疗或预防与动物中P2X7受体活性有关的疾病的用途，特别是人类。（一世）

17. 发明授权

US06509339B2 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：US06509339B2
公开(公告)日：2003-01-21
申请号：US09933094
申请日：2001-08-20
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： C07D40514
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 C2-6alkynyloxy; 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, C3-6cycloalkyl, 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炔基氧基; R 2是氢或C 1-6烷氧基，或者当R 1和R 2一起形成式2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C2-6烯基，或L是式-Alk-R4，-Alk-NR5R6，1-R6-4-哌啶基，Alk-X-R7， - Alk-YC（= O）-R9或-Alk-YC（= O）-NR11R12，其中每个Alk是C1-12烷二基; R4是氢，C1-6烷基磺酰氨基，C3-6环烷基，C5-6环烷酮，Ar-，二（Ar）甲基，Ar-氧基或Het1; R5是氢或C1-6烷基; R6是Het2; 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R8为氢，C1-6烷基或Ar; R 9为氢，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NR10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 12的氮原子结合可以形成吡咯烷基或哌啶基环，其两者均被C 1-6烷基，氨基或单或

18. 发明授权

US6156757A 1,2,3,4-tetrahydro-benzofuro[3,2-C]pyridine derivatives 有权
标题翻译： 1,2,3,4-四氢 - 苯并呋喃并[3,2-C]吡啶衍生物
公开(公告)号：US6156757A
公开(公告)日：2000-12-05
申请号：US402593
申请日：1999-10-04
申请人： Ludo Edmond Josephine Kennis , Christopher John Love , Paul Fran.cedilla.ois Bischoff
发明人： Ludo Edmond Josephine Kennis , Christopher John Love , Paul Fran.cedilla.ois Bischoff
IPC分类号： A61K31/00 , A61K31/427 , A61K31/435 , A61K31/4353 , A61K31/4355 , A61K31/4375 , A61K31/445 , A61K31/5025 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/529 , A61P1/00 , A61P3/00 , A61P3/10 , A61P9/00 , A61P15/00 , A61P15/10 , A61P25/00 , A61P25/02 , A61P25/16 , A61P25/24 , A61P25/28 , C07D491/04 , C07D491/048 , C07D498/04 , C07D513/04 , C07D519/00
CPC分类号： C07D491/04 , C07D513/04
摘要： The present invention concerns the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R.sup.1 is independently hydrogen, halogen, C.sub.1-6 alkyl, nitro, hydroxy or C.sub.1-4 alkyloxy; Alk is C.sub.1-6 alkanediyl; n is 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central .alpha..sub.2 -adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.
摘要翻译： PCT No.PCT / EP98 / 02136 Sec。 371 1999年10月4日第 102（e）日期1999年10月4日PCT提交1998年4月2日PCT公布。第WO98 / 45297号公报日期：1998年10月15日本发明涉及式I化合物的N-氧化物，其药学上可接受的加成盐和立体化学异构形式，其中每个R 1独立地是氢，卤素，C 1-6烷基，硝基，羟基或C 1-4烷氧基 ; Alk是C1-6烷二基; n为1或2; D是具有中枢性α2-肾上腺素受体拮抗剂活性的任选取代的单环，双环或三环含氮杂环。它还涉及它们的制备，包含它们的组合物及其作为药物的用途。

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