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1. 发明申请

WO2003037891A1 HETEROARYL AMINES AS GLYCOGEN SYNTHASE KINASE 3BETA INHIBITORS (GSK3 INHIBITORS) 审中-公开
标题翻译：杂多胺作为糖原合成酶激酶3β抑制剂（GSK3抑制剂）
公开(公告)号：WO2003037891A1
公开(公告)日：2003-05-08
申请号：PCT/EP2002/012077
申请日：2002-10-29
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LOVE, Christopher, John , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , VINKERS, Hendrik, Maarten , VAN AKEN, Koen, Jeanne, Alfons , DIELS, Gaston, Stanislas, Marcella
发明人： FREYNE, Eddy, Jean, Edgard , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , EMBRECHTS, Werner, Constant, Johan , LOVE, Christopher, John , JANSSEN, Paul, Adriaan, Jan , LEWI, Paulus, Joannes , HEERES, Jan , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , VINKERS, Hendrik, Maarten , VAN AKEN, Koen, Jeanne, Alfons , DIELS, Gaston, Stanislas, Marcella
IPC分类号： C07D403/12
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 (I), 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; R 1 is hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyloxy C 1-6 alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R 2 is hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R 3 is hydrogen; hydroxy; halo; optionally substituted C 1-6 alkyl or C 1-6 alkenyl or C 2-6 alkynyl; C 1-6 alkyloxy; C 1-6 alkylthio; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C 1-6 alkyl)amino; polyhaloC 1-6 alkyl; polyhaloC 1-6 alkyloxy; polyhaloC 1-6 alkylthio; R 21 ; R 21 -C 1-6 alkyl; R 21 -O-; R 21 -S-; R 21 -C(=0)-; R 21 -S(=0)p-; R 7 -S =O R 7 -S(=O)p-NH-; R 21 -S(=O)p-NH-; R 7 -C(=0)-; -NHC(=0)H; -C(=O)NHNH2; R 7 -C(=O)-NH-; R 21 -C(=O)-NH-; -C(=NH)R 7 ; -C(=NH)R 21 ; R° is an optionally substituted heterocycle provided that -X-R 2 and/or R 3 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（I）化合物，其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为6-元杂环; R 1是氢; 芳基; 甲酰基; ç<子> 1-6 烷基羰基; 任选取代的C 1-6烷基; ç<子> 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是直接键或连接基原子或基团; Z是直接键或连接基原子或基团; R 2是氢，C 1-10烷基，C 2-10烯基，C 2-10炔基，碳环或杂环，每个所述基团可以任选被取代; R 3是氢; 羟基; 光环; 任选取代的C 1-6烷基或C 1-6链烯基或C 2-6炔基; ç<子> 1-6 烷氧基; ç<子> 1-6 烷硫基; ç<子> 1-6 烷氧基羰基; ç<子> 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<子> 1-6 烷基; 多卤代<子> 1-6 烷氧基; 多卤代<子> 1-6 烷硫基; [R ^{21 ; [R ^{21 -C <子> 1-6 烷基; [R ^{21 -O-; [R ^{21 -S-; [R ^{21 -C（= O） - ; [R ^{21 -S（= O）p - ; R 7 -S = O R 7 -S（= O）p -NH-; [R ^{21 -S（= O）P-NH-; [R ^{7 -C（= O） - ; -NHC（= O）H; -C（= O）NHNH 2; [R ^{7 C（= O）-NH-; [R ^{21 C（= O）-NH-; -C（= NH）R ^{7 ; -C（= NH）R ^{21 ; R＆度; 是任选取代的杂环，条件是-XR 2和/或R 3不为氢;它们的用途，包含它们的药物组合物及其制备方法。}}}}}}}}}}}}

2. 发明申请

WO2004105765A1 MACROCYCLIC QUINAZOLINE DERIVATIVES AS ANTIPROLIFERATIVE AGENTS 审中-公开
标题翻译：大环喹诺酮衍生物作为抗增生剂
公开(公告)号：WO2004105765A1
公开(公告)日：2004-12-09
申请号：PCT/EP2004/005621
申请日：2004-05-25
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , PERERA, Timothy, Pietro, Suren , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , DIELS, Gaston, Stanislas, Marcella , EMBRECHTS, Werner, Constant, Johan , TEN HOLTE, Peter
发明人： FREYNE, Eddy, Jean, Edgard , PERERA, Timothy, Pietro, Suren , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , WILLEMS, Marc , DIELS, Gaston, Stanislas, Marcella , EMBRECHTS, Werner, Constant, Johan , TEN HOLTE, Peter
IPC分类号： A61K31/529
CPC分类号： C07D498/06 , C07C229/16 , C07C229/40 , C07D239/88 , C07D239/93 , C07D239/94
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 Z represents O, CH 2 , NH or S; in particular Z represents NH; Y represents -C 3-9 alkyl-, -C 3-9 alkenyl-, -C 3-9 alkynyl-, -C 3-7 alkyl-CO-NH- optionally substituted with amino, mono- or di(C 1-4 alkyl)amino or C 1-4 alkyloxycarbonylamino-, -C 3-7 alkenyl-CO-NH- optionally substituted with amino, mono- or di(C 1-4 alkyl)amino- or C 1-4 alkyloxycarbonylamino-, C 1-5 alkyl-oxy-C 1-5 alkyl-, -C 1-5 alkyl NR 13 -, -C 1-5 alkyl-, -C 1-5 alkyl-NR 14 -CO-C 1-5 alkyl-, -C 1-5 alkyl-CO NR 15 -C 1-5 alkyl-, -C 1-6 alkyl-CO-NH-, -C 1-6 alkyl-NH-CO-, -C 1-3 alkyl-NH-CS-Het 20 -, -C 1-3 alkyl-NH-CO-Het 20 -, -C 1-2 alkyl-CO-Het 21 -CO-, -Het 22 -CH 2 -CO-NH-C 1-3 alkyl-, -CO-NH-C 1-6 alkyl-, -NH-CO-C 1-6 alkyl-, -CO-C 1-7 alkyl-, -C 1-7 alkyl-CO-, -C 1-6 alkyl-CO-C 1-6 alkyl-, -C 1-2 alkyl-NH-CO-CR 16 R 17 -NH-, -C 1-2 alkyl-CO-NH-CR 18 R 19 -CO-, -C 1-2 alkyl-CO-NR 20 -C 1-3 alkyl-CO-, C 1-2 alkyl-NR 21 -CH 2 -CO-NH-C 1-3 alkyl-, or -NR 22 -CO-C 1-3 alkyl-NH-; X 1 represents a direct bond, O or -O-C 1-2 alkyl-, CO, -CO-C 1-2 alkyl-, NR 11 , -NR 11 -C 1-2 alkyl-, CH 2 -, -O-N=CH- or -C 1-2 alkyl-; X 2 represents a direct bond, O, -O-C 1-2 alkyl-, CO, -CO-C 1-2 alkyl-, NR 12 , -NR 12 -C 1-2 alkyl-, -CH 2 -, -O-N=CH- or -C 1-2 alkyl-. The growth inhibitory effect anti-tumour activity of the present compounds has been demonstrated in vitro , in enzymatic assays on the receptor tyrosine kinase EGFR.
摘要翻译：本发明涉及式（I）化合物的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Z代表O，CH2，NH或S; 特别是Z表示NH; 一个或多个（C 1-4烷基）氨基或C 1-4烷氧基羰基氨基 - 取代的C 1-3烷基 - ， - C 3-9烯基 - ， - C 3-9炔基 - ， - 一个或多个（C 1-4烷基）氨基 - 或C 1-4烷氧基羰基氨基 - ，C 1-5烷基 - 氧基-C 1-5烷基 - ， - C 1-5烷基NR 13取代的-C 3-7烯基-CO-NH- - ， - C 1-5烷基 - ， - C 1-5烷基-NR 14 -CO-C 1-5烷基 - ， - C 1-5烷基-CO NR 15 -C 1-6烷基 - ， - C 1-6烷基-CO-NH - ，-C 1-6烷基-NH-CO - ， - C 1-3烷基-NH-CS-Het 20 - ， - C 1-3烷基-NH-CO-Het 20 - ， - C 1-2烷基-CO-Het -CO-，-Het 22，-CH 2 -CO-NH-C 1-3烷基 - ， - CO-NH-C 1-6烷基 - ， - -NH-CO-C 1-6烷基 - ， - CO-C 1-7烷基 - ， - C 1-7烷基-CO - ， - C 1-6烷基-CO-C 1-6烷基 - ， - C 1-2烷基-NH-CO-CR 16 R 17 -NH-，-C 1-2烷基-CO- NH-CR 18 R 19 -CO - ， - C 1-2烷基-CO-NR 20 -C 1-3烷基-CO-，C 1-2烷基-NR 21 -CH 2 -CO-NH-C1- 3-烷基 - 或-NR 22 -CO-C 1-3烷基-NH-; X 1表示直接键，O或-O-C 1-2烷基 - ，CO，-CO-C 1-2烷基 - ，NR 11，-NR 11 -C 1-2烷基 - ，CH 2 - ，--ON = CH-或-C1-2烷基 - ; X 2表示直接键，O，-O-C 1-2烷基 - ，CO，-CO-C 1-2烷基 - ，NR 12，-NR 12 -C 1-2烷基 - ， - CH 2 - ON = CH-或-C1-2烷基。在体外，在受体酪氨酸激酶EGFR的酶学测定中已经证明了本发明化合物的生长抑制作用抗肿瘤活性。

3. 发明申请

WO2003015776A1 2,4,5-TRISUBSTITUTED THIAZOLYL DERIVATIVES AND THEIR ANTIINFLAMMATORY ACTIVITY 审中-公开
标题翻译： 2,4,5-三唑衍生物及其抗炎活性
公开(公告)号：WO2003015776A1
公开(公告)日：2003-02-27
申请号：PCT/EP2002/008956
申请日：2002-08-09
申请人： JANSSEN PHARMACEUTICA N.V. , LOVE, Christopher, John , VAN WAUWE, Jean, Pierre, Frans , DE BRABANDER, Marc, J. , MOSES, Roger, Clive , GONCHARENKO, Mykhalyo , COOYMANS, Ludwig, Paul , VANDERMAESEN, Nele , DIELS, Gaston, Stanislas, Marcella , SIBLEY, Anthony, William , NOULA, Caterina
发明人： LOVE, Christopher, John , VAN WAUWE, Jean, Pierre, Frans , DE BRABANDER, Marc, J. , MOSES, Roger, Clive , GONCHARENKO, Mykhalyo , COOYMANS, Ludwig, Paul , VANDERMAESEN, Nele , DIELS, Gaston, Stanislas, Marcella , SIBLEY, Anthony, William , NOULA, Caterina
IPC分类号： A61K31/426
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; C 1-6 alkyl; C 1-6 alkyl substituted with hydroxy, carboxyl, cyano, amino, mono -or di(C 1-6 alkyl)amino, aminocarbonyl, mono -or di(C 1-6 alkyl)aminocarbonyl, C 1-6 alkyloxycarbonyl or C 1-6 alkyloxy; polyhaloC 1-4 alkyl; C 1-4 alkyloxy; cyano; amino; aminocarbonyl; mono -or di(C 1-6 alkyl)aminocarbonyl; C 1-6 alkyloxycarbonyl; C 1-6 alkylcarbonyloxy; H 2 N-S(=O) 2 -; mono -or di(C 1-6 alkyl)amino-S(=O) 2 ; -C(=N-R x )NR y R z ; 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，其N-氧化物，其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; C1-6烷基; 被羟基，羧基，氰基，氨基，单 - 或二（C 1-6烷基）氨基，氨基羰基，单 - 或二（C 1-6烷基）氨基羰基，C 1-6烷氧基羰基或C 1-6烷氧基取代的C 1-6烷基; polyhaloC1-4alkyl; C1-4alkyloxy; 氰基; 氨基; 羰基; 单 - 或二（C 1-6烷基）氨基羰基; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; H 2 N-S（= O）2 - ; 单 - 或二（C 1-6烷基）氨基-S（= O）2; -C（= NR ）NR - [R ; 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。

4. 发明申请

WO2006008260A1 DIMERIC PIPERIDINE DERIVATIVES 审中-公开
标题翻译：二哌啶衍生物
公开(公告)号：WO2006008260A1
公开(公告)日：2006-01-26
申请号：PCT/EP2005/053351
申请日：2005-07-13
申请人： JANSSEN PHARMACEUTICA N.V. , CIK, Miroslav , DIELS, Gaston, Stanislas, Marcella , VAN LOMMEN, Guy, Rosalia, Eugeen
发明人： CIK, Miroslav , DIELS, Gaston, Stanislas, Marcella , VAN LOMMEN, Guy, Rosalia, Eugeen
IPC分类号： C07D211/96
CPC分类号： C07D211/46 , C07D211/52 , C07D211/96 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The compounds of the following formula (I) : the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, useful in the treatment of neurodegenerative mediated disorders.
摘要翻译：下式（I）的化合物：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，其可用于治疗神经变性介导的病症。

5. 发明申请

WO2006008259A1 DIMERIC COMPOUNDS OF PIPERIDINE, PIPERAZINE OR MORPHOLINE OR THEIR 7-MEMBERED ANALOGS SUITABALE FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS 审中-公开
标题翻译：哌啶，哌嗪或吗啉的二元化合物或其用于治疗神经损伤性疾病的7种成员的类似物
公开(公告)号：WO2006008259A1
公开(公告)日：2006-01-26
申请号：PCT/EP2005/053345
申请日：2005-07-13
申请人： JANSSEN PHARMACEUTICA N.V. , CIK, Miroslav , DIELS, Gaston, Stanislas, Marcella , VAN LOMMEN, Guy, Rosalia, Eugeen
发明人： CIK, Miroslav , DIELS, Gaston, Stanislas, Marcella , VAN LOMMEN, Guy, Rosalia, Eugeen
IPC分类号： C07D417/12
CPC分类号： C07D211/58 , C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12
摘要： Formula (I’’), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof.
摘要翻译：式（I“），N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式。

6. 发明申请

WO2004033428A1 SUBSTITUTED 1,4-DI-PIPERIDIN-4-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的1,4-二哌啶-4-基哌嗪衍生物及其作为神经营养因子拮抗剂的用途
公开(公告)号：WO2004033428A1
公开(公告)日：2004-04-22
申请号：PCT/EP2003/050697
申请日：2003-10-07
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth , VAN ROOSBROECK, Yves, Emiel, Maria , DIELS, Gaston, Stanislas, Marcella
发明人： JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth , VAN ROOSBROECK, Yves, Emiel, Maria , DIELS, Gaston, Stanislas, Marcella
IPC分类号： C07D211/58
CPC分类号： C07D401/14 , C07D211/58 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS. The compounds according to the invention can be represented by general Formula (I), and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N -oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1. In view of their capability to antagonize the actions of neurokinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK 1 receptor, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of neurokinin-mediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.
摘要翻译：本发明涉及具有神经激肽拮抗活性的取代的1,4-二哌啶-4-基 - 哌嗪衍生物，特别是NK1拮抗活性，其制备方法，包含它们的组合物及其作为药物的用途，特别是用于治疗呕吐，焦虑，抑郁，疼痛，胰腺炎和IBS。根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式和其前药，其中所有取代基被定义鉴于它们通过阻断神经激肽受体拮抗神经激肽的作用的能力，特别是通过阻断NK1受体拮抗物质P的作用，根据本发明的化合物可用作药物，在特别是在神经激肽介导的病症例如中枢神经系统疾病，特别是抑郁症，焦虑障碍，应激相关疾病，睡眠障碍，认知障碍，人格障碍，分裂情感障碍，进食障碍，神经变性疾病中的预防和治疗治疗中，成瘾症，情绪障碍，性功能障碍，疼痛等CNS相关c onditions; 炎; 过敏性疾病; 呕吐; 胃肠道疾病，特别是肠易激综合征（IBS）; 皮肤病; 血管痉挛性疾病; 纤维化和胶原病; 与免疫增强或抑制相关的疾病和风湿性疾病和体重控制。

7. 发明申请

WO1992001697A1 NOVEL SUBSTITUTED THIAZOLYL AND SUBSTITUTED PYRIDINYL DERIVATIVES 审中-公开
标题翻译：新的取代的噻唑啉并取代的吡啶衍生物
公开(公告)号：WO1992001697A1
公开(公告)日：1992-02-06
申请号：PCT/EP1991001292
申请日：1991-07-09
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DIELS, Gaston, Stanislas, Marcella
IPC分类号： C07D513/04
CPC分类号： C07D401/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/30 , C07D473/40 , C07D513/04
摘要： Substituted thiazolyl and substituted pyridinyl derivatives of formula (I), the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein -A =A -A =A - is a bivalent radical having the formula -CH=CH-CH=CH- (a-1), -N=CH-CH=CH- (a-2), -CH=N-CH=CH- (a-3), -CH=CH-N=CH- (a-4), -CH=CH-CH=N- (a-5), -N=CH-N=CH- (a-6) or -CH=N-CH=N- (a-7); B represents NR , CH2, O, S, SO or SO2 wherein R is hydrogen or C1-4alkyl; R is a radical of formula (b-1) or (b-2); wherein D is C1-4alkanediyl; R is C1-6alkyl; n is 0, 1 or 2; L is hydrogen; C1-12alkyl; C3-6cycloalkyl; C3-6alkenyl optionally substituted with aryl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; arylcarbonyl; aryl C1-6alkyloxycarbonyl; or a radical of formula -Alk-R (c-1); -Alk-Y-R (c-2); -Alk-Z -C(=X)-Z -R (c-3); or -CH2-CHOH-CH2-O-R (c-4); have antiallergic properties. Compositions containing the same and methods of treating warm-blooded animals suffering from allergic diseases.
摘要翻译：取代的噻唑基和式（I）的取代的吡啶基衍生物，其药学上可接受的酸加成盐及其立体化学异构形式，其中-A 1 = A 2 -A 3 = A 4 - 是二价具有式-CH = CH-CH = CH-（a-1），-N = CH-CH = CH-（a-2），-CH = N-CH = CH-（a-3）， - CH = CH-N = CH-（a-4），-CH = CH-CH = N-（a-5），-N = CH-N = CH-（a-6）或-CH = = N-（a-7）; B表示NR 1，CH 2，O，S，SO或SO 2，其中R 1是氢或C 1-4烷基; R是式（b-1）或（b-2）的基团; 其中D为C 1-4烷二基; R 2是C 1-6烷基; n为0,1或2; L是氢; C1-12烷基; 3-6环; 任选被芳基取代的C 3-6烯基; C1-6烷基; C1-6alkyloxycarbonyl; 基羰基; 芳基C 1-6烷氧基羰基; 或式-Alk-R 3（c-1）的基团; -Alk-Y-R 4（c-2）; -Alk-Z 1 -C（= X）-Z 2 -R 5（c-3）; 或-CH 2 -CHOH-CH 2 -O-R 6（c-4）; 具有抗过敏性质。含有相同的组合物和治疗患有过敏性疾病的温血动物的方法。

8. 发明授权

EP0832071B1 1,3-DIHYDRO-2H-IMIDAZOL-2-ONE DERIVATIVES HAVING PDE IV AND CYTOKININ INHIBITING ACTIVITY 失效
标题翻译： WITH PDE IV和细胞因子抑制活性的1,3-二氢-2H-咪唑-2-酮衍生物
公开(公告)号：EP0832071B1
公开(公告)日：2005-09-28
申请号：EP96911969.2
申请日：1996-03-28
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： FREYNE, Eddy, Jean, Edgard , DIELS, Gaston, Stanislas, Marcella , ANDRES-GIL, José, Ignacio , FERNANDEZ-GADEA, Francisco, Javier
IPC分类号： C07D233/70 , C07D233/32 , C07D405/04 , A61K31/415
CPC分类号： C07D405/04 , C07D233/32 , C07D233/70

9. 发明授权

EP0539420B1 SUBSTITUTED THIAZOLYL AND SUBSTITUTED PYRIDINYL DERIVATIVES 失效
标题翻译：取代的噻唑并吡啶衍生物
公开(公告)号：EP0539420B1
公开(公告)日：2000-01-05
申请号：EP91912667.2
申请日：1991-07-09
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DIELS, Gaston, Stanislas, Marcella
IPC分类号： C07D513/04 , C07D401/14 , C07D401/04 , C07D519/00 , C07D473/40 , A61K31/505 , A61K31/425 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/30
CPC分类号： C07D401/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D473/30 , C07D473/40 , C07D513/04

10. 发明公开

EP0588859A1 IMIDAZO 1,2-a](PYRROLO, THIENO OR FURANO) 3,2-d]AZEPINE DERIVATIVES, COMPOSITIONS AND METHODS OF USE 失效
标题翻译：咪唑并[1,2-A]（吡咯并，噻吩并富良野OR）（3-2-D）二氮杂草，制剂和它们的用途。
公开(公告)号：EP0588859A1
公开(公告)日：1994-03-30
申请号：EP92911643.0
申请日：1992-06-09
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： JANSSENS, Frans, Eduard , DIELS, Gaston, Stanislas, Marcella , LEENAERTS, Joseph, Elisabeth , COOYMANS, Ludwig, Paul
IPC分类号： C07D235 , A61K31 , A61P37 , C07D487 , C07D491 , C07D495 , C07D519
CPC分类号： C07D487/14 , C07D491/14 , C07D495/14
摘要： La présente invention concerne de nouvelles imidazo[1,2a](pyrrolo, thiéno ou furano)[3,2-d]azépines de la formule (I); les sels d'adition pharmaceutiquement acceptables et les formes stéréochimiquement isomères de celles-ci, dans laquelle chacune des lignes pointillées représentent indépendamment une liaison optionnelle; R1 représente hydrogène, C1-4 alkyle, halo, éthényle substitué avec hydroxycarbonyle ou C1-4alkyloxycarbonyle, hydroxyC1-4alkyle, formyle, hydroxycarbonyle ou hydroxycarbonylC1-4alkyle; R2 représente hydrogène, C1-4 alkyle, éthényle substitué avec hydroxycarbonyle ou C1-4alkyloxycarbonyl hydroxyC1-4alkyle, formyle ou hydroxycarbonyle; R3 représente hydrogène, C1-4 alkyle, hydroxyC1-4 alkyle, phényle ou halo; L représente hydrogène; C1-6alkyle; C1-6alkyle substitué avec un substituant choisi dans le groupe comprenant hydroxy, halo, C1-4alkyloxy, hydroxycarbonyle, C1-4alkyloxycarbonyle, C1-4alkyloxycarbonylC1-4alkyloxy, hydroxycarbonylC1-4alkyloxy, C1-4alkyloxycarbonylamino, C1-4alkylaminothiocarbonylamino, aryle aryloxy et arylcarbonyle; C1-6 alkyle substitué avec hydroxy et aryloxy; C3-6alcényle; C3-6alcényle substitué avec aryle; L représente un radical de la formule-Alk-Y-Het1 (a-1), -Alk-NH-CO-Het2 (a-2) ou -Alk-Het3 (a-3); ils sont utilisés comme composés antiallergiques. Compositions comprenant lesdits composés, méthodes d'utilisation et procédés pour leur préparation.

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