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1. 发明申请

WO0069424A2 METHOD OF TREATING PSYCHOTIC DISORDERS 审中-公开
标题翻译：治疗心理障碍的方法
公开(公告)号：WO0069424A2
公开(公告)日：2000-11-23
申请号：PCT/EP0003506
申请日：2000-04-14
申请人： SOLVAY PHARM BV , HES ROELOF VAN , HEIJDEN JOHANNES A M V D , KRUSE CORNELIS G , LONG STEPHEN K
发明人： VAN HES ROELOF , VAN DER HEIJDEN JOHANNES A M , KRUSE CORNELIS G , LONG STEPHEN K
IPC分类号： C07D401/14 , A61K31/00 , A61K31/404 , A61K31/4184 , A61K31/4439 , A61K31/4523 , A61K31/517 , A61K31/519 , A61K45/06 , A61P25/18 , A61P43/00 , C07D209/14 , C07D209/46 , C07D209/48 , C07D403/08 , C07D513/04
CPC分类号： A61K31/4439 , A61K31/00
摘要： The invention relates to the use of compounds having both dopamine D2-antagonistic activity and serotonin reuptake inhibitory (SRI) activity for the treatment of psychotic disorders such as schizophrenia. The invention further relates to a group of novel (1, 2, 3,6-tetrahydropyridin-4-yl) indole and -furan derivatives having these activities.
摘要翻译：本发明涉及具有多巴胺D2拮抗活性和5-羟色胺再摄取抑制（SRI）活性的化合物用于治疗精神病性疾病如精神分裂症的用途。本发明还涉及一组具有这些活性的新的（1,2,3,6,6-四氢吡啶-4-基）吲哚和呋喃衍生物。

2. 发明申请

WO0114330A2 NEW PHENYLPIPERAZINES 审中-公开
标题翻译：新型苯乙烯
公开(公告)号：WO0114330A2
公开(公告)日：2001-03-01
申请号：PCT/EP0008190
申请日：2000-08-22
申请人： SOLVAY PHARM BV , HES ROELOF VAN , HEIJDEN JOHANNES A M V D , KRUSE CORNELIS G , TIPKER JACOBUS , TULP MARTINUS T M , VISSER GERBEN M , VLIET BERNARD J VAN
发明人： HES ROELOF VAN , HEIJDEN JOHANNES A M VAN DER , KRUSE CORNELIS G , TIPKER JACOBUS , TULP MARTINUS T M , VISSER GERBEN M , VLIET BERNARD J VAN
IPC分类号： C07D401/14 , A61K31/404 , A61K31/4184 , A61K31/428 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/538 , A61K31/541 , A61K31/5415 , A61K31/55 , A61P1/08 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , C07D20060101 , C07D209/00 , C07D209/34 , C07D209/40 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D401/12 , C07D209/34 , C07D209/40 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The invention relates to a group of phenylpiperazines having high affinity for the dopamine D2-receptor and are good serotonin reuptake inhibitors (SRI's). The invention relates to a group of phenylpiperazine derivatives of formula (I) wherein: a.o. x is 1) a group of formula (1) wherein: S1 is hydrogen or halogen; S2 and S3 are independently hydrogen, alkyl (1-6C), phenyl or benzyl; S4 represents two hydrogen atoms or an oxo group, S5 is H or alkyl (1-4C); and Y is C, O or S, and salts there of.
摘要翻译：本发明涉及对多巴胺D2受体具有高亲和力的一组苯基哌嗪，并且是良好的5-羟色胺再摄取抑制剂（SRI's）。本发明涉及一种式（I）的苯基哌嗪衍生物，其中：a.o. x为1）式（1）的基团，其中：S1为氢或卤素; S2和S3独立地是氢，烷基（1-6C），苯基或苄基; S4代表两个氢原子或氧代基，S5是H或烷基（1-4C）; 并且Y是C，O或S，以及其中的盐。

3. 发明申请

WO2005080345A3 IMIDAZOLINE DERIVATIVES HAVING CB1-ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有CB1拮抗活性的咪唑啉衍生物
公开(公告)号：WO2005080345A3
公开(公告)日：2006-12-21
申请号：PCT/EP2005050680
申请日：2005-02-16
申请人： SOLVAY PHARM BV , LANGE JOSEPHUS H M , KRUSE CORNELIS G , VAN STUIVENBERG HERMAN H
发明人： LANGE JOSEPHUS H M , KRUSE CORNELIS G , VAN STUIVENBERG HERMAN H
IPC分类号： C07D233/28 , A61K31/4164
CPC分类号： C07D233/16 , C07D233/50 , C07D233/52
摘要： The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及1,2,4-三取代的咪唑啉衍生物，制备这些化合物的方法，可用于合成所述咪唑啉衍生物的新中间体，制备这些中间体的方法，药物组合物含有一种或多种这些咪唑啉衍生物作为活性成分，以及这些药物组合物用于治疗精神病和神经障碍的用途。化合物具有通式（I），其中符号具有说明书中给出的含义。

4. 发明申请

WO2008087123A3 USE OF 5-HT6 ANTAGONISTS TO PREVENT RELAPSE INTO ADDICTION 审中-公开
标题翻译： 5-HT6拮抗剂的使用，以防止患者继续使用
公开(公告)号：WO2008087123A3
公开(公告)日：2008-11-27
申请号：PCT/EP2008050360
申请日：2008-01-15
申请人： SOLVAY PHARM BV , DE BRUIN NATASJA M W J , VAN LOEVEZIJN ARNOLD , WIJNEN JOHAN , HERREMANS ARNOLDUS H J , KRUSE CORNELIS G
发明人： DE BRUIN NATASJA M W J , VAN LOEVEZIJN ARNOLD , WIJNEN JOHAN , HERREMANS ARNOLDUS H J , KRUSE CORNELIS G
IPC分类号： A61K31/404 , A61K31/4045 , A61K31/415 , A61K31/496 , A61K31/505 , A61P25/30
CPC分类号： A61K31/404 , A61K31/4045 , A61K31/415 , A61K31/496 , A61K31/505
摘要： The invention relates to a novel use of compounds and pharmaceutically acceptable salts thereof, which are 5-HT6 antagonists. These compounds are useful for the preparation of medicaments for preventing relapse into addiction, in particular relapse into addiction to substances of abuse, including opiates, hallucinogens, inhalants, phencyclidine, amphetamines, cocaine, cannabis, nicotine, and alcohol, into relapse to addiction to certain medicines, including sedatives, hypnotics and anxiolytics, and into relapse to certain addictive behaviors, including gambling.
摘要翻译：本发明涉及作为5-HT 6拮抗剂的化合物及其药学上可接受的盐的新用途。这些化合物可用于制备用于预防复发成瘾的药物，特别是复制成滥用物质，包括鸦片剂，致幻剂，吸入剂，苯环利定，苯丙胺，可卡因，大麻，尼古丁和酒精，成瘾成瘾某些药物，包括镇静剂，安眠药和抗焦虑药物，并复发到某些上瘾行为，包括赌博。

5. 发明申请

WO2007128674A2 MUSCARINIC AGONISTS TO TREAT IMPULSE CONTROL DISORDERS 审中-公开
标题翻译：治疗肿瘤控制障碍的药物治疗
公开(公告)号：WO2007128674A2
公开(公告)日：2007-11-15
申请号：PCT/EP2007053934
申请日：2007-04-23
申请人： SOLVAY PHARM BV , DE BRUIN NATASJA M W J , VAN DRIMMELEN MARLIES L , HERREMANS ARNOLDUS H J , TULP MARTINUS TH M , KRUSE CORNELIS G
发明人： DE BRUIN NATASJA M W J , VAN DRIMMELEN MARLIES L , HERREMANS ARNOLDUS H J , TULP MARTINUS TH M , KRUSE CORNELIS G
IPC分类号： A61K31/00 , A61K31/439 , A61K31/4439 , A61K31/551 , A61P25/18
CPC分类号： A61K31/439 , A61K31/00 , A61K31/4439 , A61K31/551 , A61K31/5513
摘要： The invention relates to a novel use of compounds and pharmaceutically acceptable salts thereof, which are muscarinic, in particular muscarine-1 (M 1 ) agonists. These compounds are useful for the preparation of medicaments for treatment, amelioration or prevention of impulse control disorders. These include impulse control disorders 'Not Elsewhere Classified' such as intermittent explosive disorder, pyromania, kleptomania, pathological gambling and trichotillomania; and impulse control disorders 'Not Otherwise Specified' such as: compulsive buying disorder, binge eating and binge drinking disorder, impulsive self-injurious behaviour such as pathological skin picking, nail-biting and nose-picking, gouging, head banging and self- biting; paraphilic sexual addictions, including exhibitionism, fetishism, frotteurism, pedophilia, masochism, sadism, transvestic fetishism and voyeurism; compulsive Internet use and excessive mobile phone use.
摘要翻译：本发明涉及毒蕈碱型化合物及其药学上可接受的盐，特别是毒蕈碱-1（M 1 H 1）激动剂的新用途。这些化合物可用于制备用于治疗，改善或预防冲动控制障碍的药物。这些包括脉冲控制障碍“非其他分类”，如间歇性爆发性疾病，pyromania，kleptomania，病态赌博和拔毛病; 和冲动控制障碍“无其他指定”，如：强迫性购买障碍，暴饮暴食饮酒障碍，脉冲性自我伤害行为，如病理性皮肤采摘，咬咬和鼻子抽搐，气刨，头部撞击和自咬 ; 淫秽性成瘾，包括露胸主义，拜物教，愚蠢主义，恋童癖，受虐狂，虐待狂，变性拜拜教和窥视主义; 强制上网使用和手机使用过多。

6. 发明申请

WO2008129054A3 HETEROCYCLIC COMPOUNDS WITH AFFINITY TO MUSCARINIC RECEPTORS 审中-公开
标题翻译：具有对肌肉受体的亲和性的杂环化合物
公开(公告)号：WO2008129054A3
公开(公告)日：2009-02-05
申请号：PCT/EP2008054897
申请日：2008-04-23
申请人： SOLVAY PHARM BV , STOIT AXEL , COOLEN HEIN K A C , KRUSE CORNELIS G , TERWEL LOUISE HEIR OF REINDERS
发明人： STOIT AXEL , COOLEN HEIN K A C , KRUSE CORNELIS G , TERWEL LOUISE HEIR OF REINDERS
IPC分类号： C07D401/04 , A61K31/439 , A61K31/4427 , A61K31/4439 , A61P25/28 , C07D401/14 , C07D413/04 , C07D453/02 , C07D471/08
CPC分类号： C07D401/04 , C07D401/14 , C07D413/04 , C07D453/02 , C07D471/08
摘要： The present invention relates to heterocyclic compounds of the formula (I) wherein - the heterocycle comprises two double bonds which may be present at several positions, represented by the dashed lines ( -- ); - the heterocycle contains two heteroatoms, - W being N or NH; - Y being CH, O or NH, wherein if Y is O, X1 is CH and X2 is the residue C-Z-R2 or C-R3, wherein Z is NH, O, or S; and if Y is CH or NH, one of X1 and X2 is CH or N, the other being the residue C-Z-R2 or C-R3, wherein Z is NH or S; - R1 is selected from the structures (a), (b) and (c): - R2 is selected from (C1-C10)alkyl, (C2-C10)alkenyl and (C2-C10)alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, oxo, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkenyloxy, (C1-C6)alkenylthio, (C1-C4)alkoxy(C1-C4)alkoxy, (C5-C7)cycloalkyl, a 5-membered unsaturated heterocycle (optionally substituted with halogen), phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or - R2 is an unbranched (C2-C8)alkyl substituted at the Za-symbol of a group with the formula (Ia) wherein if X1 is CH or N1 X1 is CH or N and X2a is C-Za-, or if X1 is C-Z-R2, X1a is C-Za- and X2a is CH or N; and the symbols Wa, Ya and Za and the substituent R1a have the same meanings as defined previously for the symbols W, Y and Z and the substituent R1, and are not independently selected, each of the symbols Wa, Ya and Za and the substituent R1 a representing identical symbols and substituents, respectively, as the symbols W, Y and Z and the substituent R1 in the other part of the structure of formula (I); - R3 is selected from (C4-C10) alkyl, (C2-C10) alkenyl and (C2-C10) alkynyl, optionally independently substituted with one or more substituents selected from halogen, hydroxy, cyano, (C1C6) alkoxy, (C1C6) alkylthio, (C1C6)alkenyloxy, (C1C6) alkenylthio, (C1-C4) alkoxy (C1-C4) alkoxy, (C5-C7) cycloalkyl, a 5-membered unsaturated heterocycle optionally substituted with halogen, phenyl, phenyloxy and phenylthio, wherein the phenyl group is optionally substituted with halogen; or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to muscarinic receptors and may be used in the treatment, alleviation or prevention of muscarinic receptor mediated diseases and conditions.
摘要翻译：本发明涉及式（I）的杂环化合物，其中 - 杂环包含两个双键，其可以存在于由虚线（ - ）表示的几个位置。 - 杂环含有两个杂原子，-W为N或NH; - Y是CH，O或NH，其中如果Y是O，则X1是CH，X2是残基C-Z-R2或C-R3，其中Z是NH，O或S; 并且如果Y是CH或NH，则X1和X2之一是CH或N，另一个是残基C-Z-R2或C-R3，其中Z是NH或S; -R 1选自（C 1 -C 10）烷基，（C 2 -C 10）烯基和（C 2 -C 10）炔基，任选独立地被一个（C1-C6）烷氧基，（C1-C6）烷氧基，（C1-C6）烯硫基，（C1-C4）烷氧基（C1- C4烷氧基，（C5-C7）环烷基，5元不饱和杂环（任选被卤素取代），苯基，苯氧基和苯硫基，其中苯基任选被卤素取代; 或 - R 2是在具有式（Ia）的基团的Za符号取代的未支化的（C 2 -C 8）烷基，其中如果X 1是CH或N 1是CH或N 1且X 2是C a Z a，或者如果X 1 是CZ-R2，X1a是C-Za，X2a是CH或N; 并且符号Wa，Ya和Za以及取代基R 1a具有与前面对符号W，Y和Z以及取代基R所定义的相同的含义，并且不是独立地选择，每个符号Wa，Ya和Za以及取代基 R1a分别表示与式（I）结构的另一部分中的符号W，Y和Z以及取代基R 1相同的符号和取代基; 羟基，氰基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷基，（C 2 -C 10）烷基硫基，（C1C6）烯氧基，（C1C6）烯基硫代，（C1-C4）烷氧基（C1-C4）烷氧基，（C5-C7）环烷基，任选被卤素，苯基，苯氧基和苯硫基取代的5元不饱和杂环，其中苯基任选被卤素取代; 或其药学上可接受的盐，溶剂合物或水合物。本发明的化合物对毒蕈碱受体具有亲和力，可用于治疗，缓解或预防毒蕈碱受体介导的疾病和病症。

7. 发明申请

WO2008034863A3 SULFONYLPYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS 审中-公开
标题翻译：作为5-HT6拮抗剂的磺酰基吡唑烷酮衍生物
公开(公告)号：WO2008034863A3
公开(公告)日：2008-05-08
申请号：PCT/EP2007059944
申请日：2007-09-20
申请人： SOLVAY PHARM BV , IWEMA BAKKER WOUTER I , KEIZER HISKIAS G , NEUT VAN DER MARTINA A W , KRUSE CORNELIS G , LOEVEZIJN VAN ARNOLD , ZORGDRAGER JAN
发明人： IWEMA BAKKER WOUTER I , KEIZER HISKIAS G , NEUT VAN DER MARTINA A W , KRUSE CORNELIS G , LOEVEZIJN VAN ARNOLD , ZORGDRAGER JAN
IPC分类号： C07D231/06 , A61K31/415 , A61K31/4155 , A61P25/00 , C07D231/12 , C07D401/04 , C07D401/12 , C07D403/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/12 , C07D513/04
CPC分类号： C07D513/04 , A61K9/0019 , A61K9/0031 , A61K9/1652 , A61K9/2054 , C07D231/06 , C07D231/12 , C07D231/54 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/10 , C07D491/10 , C07D491/107 , C07D519/00
摘要： This invention concerns sulfonylpyrazoline carboxamidine derivatives as antagonists of 5-HT 6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1), wherein the symbols have the meanings given in the description.
摘要翻译：本发明涉及作为5-HT 6受体拮抗剂的磺酰吡唑啉甲脒衍生物，涉及制备这些化合物的方法和用于它们合成的新型中间体。本发明还涉及这些化合物和组合物的用途，特别是它们在给予患者以在帕金森病，亨廷顿氏舞蹈症，精神分裂症，焦虑症，抑郁症，躁狂抑郁症，精神病，癫痫，强迫症中的治疗效果方面的用途，情绪障碍，偏头痛，阿尔茨海默病，年龄相关认知衰退，轻度认知障碍，睡眠障碍，进食障碍，厌食症，贪食症，暴饮暴食症，惊恐发作，静坐不动，注意力缺陷多动障碍，注意力缺陷障碍，可卡因滥用，乙醇，尼古丁或苯并二氮杂，疼痛，与脊髓损伤或头部损伤相关的疾病，脑积水，功能性肠病，肠易激综合征，肥胖症和2型糖尿病。化合物具有通式（1），其中符号具有说明书中给出的含义。

8. 发明申请

WO2006061372A3 PHENYLPIPERAZINES WITH A COMBINATION OF AFFINITY FOR DOPAMINE -D2 RECEPTORS AND SEROTONIN REUPTAKE SITES 审中-公开
标题翻译：多巴胺-D2受体和5-羟色胺再灌注位点联合应用的苯基哌嗪类化合物
公开(公告)号：WO2006061372A3
公开(公告)日：2006-11-23
申请号：PCT/EP2005056500
申请日：2005-12-06
申请人： SOLVAY PHARM BV , VAN HES ROELOF , SMID PIETER , KRUSE CORNELIS G , TULP MARTINUS TH M
发明人： VAN HES ROELOF , SMID PIETER , KRUSE CORNELIS G , TULP MARTINUS TH M
IPC分类号： C07D319/18 , A61K31/496 , A61P25/28 , C07D215/38 , C07D265/36 , C07D295/12 , C07D307/82 , C07D311/18 , C07D321/10
CPC分类号： C07D319/18 , C07D215/38 , C07D263/58 , C07D265/36 , C07D295/13 , C07D307/82 , C07D311/18 , C07D321/10
摘要： The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine -D2 receptors and to methods for the preparation of these compounds. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula ( 1 ) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明涉及一组具有双重作用模式的新型苯基哌嗪衍生物：5-羟色胺再摄取抑制作用和对多巴胺-D2受体的亲和力以及制备这些化合物的方法。本发明还涉及本文公开的化合物用于制造产生有益效果的药物的用途。该化合物具有通式（1），其中符号具有说明书中给出的含义。

9. 发明申请

WO2006061373A3 TETRAHYDROPYRIDIN-4-YL INDOLES WITH A COMBINATION OF AFFINITY FOR DOPAMINE-D2 RECEPTORS AND SEROTONIN REUPTAKE SITES 审中-公开
标题翻译：四氢吡啶-4-基吲哚类化合物对多巴胺D2受体和5-羟色胺再灌注位点的亲和力组合
公开(公告)号：WO2006061373A3
公开(公告)日：2006-09-21
申请号：PCT/EP2005056501
申请日：2005-12-06
申请人： SOLVAY PHARM BV , VAN HES ROELOF , SMID PIETER , KRUSE CORNELIS G , TULP MARTINUS TH M
发明人： VAN HES ROELOF , SMID PIETER , KRUSE CORNELIS G , TULP MARTINUS TH M
IPC分类号： C07D401/14 , A61K31/519 , A61P25/00 , C07D471/04 , C07D487/04 , C07D513/04
CPC分类号： C07D401/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine -D 2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin -4-yl indoles of the formula (I) and tautomers, stereoisomers, prodrugs, N -oxides, pharmacologically acceptable salts, hydrates and solvates thereof , wherein: - R 1 is hydrogen, halogen, alkyl (C 1-3 ) or alkoxy(C 1-3 ), CN or CF 3 , - R 2 is hydrogen or alkyl (C 1-3 ), R 3 is hydrogen or alkyl (C 1-3 ), - Z is hydrogen or alkyl (C 1-3 ), alkoxy(C 1-3 ) or alkylthio(C 1-3 ), - A is hydrogen or alkyl (C 1-3 ), or - A and Z together form a saturated or (partly) unsaturated 5 - or 6- membered ring which may be substituted with halogen, alkyl (C 1-3 ) or phenyl, in which ring Z represents carbon, sulfur of nitrogen .
摘要翻译：本发明涉及一组具有双重作用模式的新四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D受体的亲和力，涉及制备这些化合物的方法和涉及可用于合成所述四氢吡啶-4-基吲哚的新颖中间体。本发明还涉及本文公开的化合物用于制造产生有益效果的药物的用途。本发明涉及式（I）的新型四氢吡啶-4-基吲哚及其互变异构体，立体异构体，前药，N-氧化物，药理学上可接受的盐，水合物和溶剂化物，其中：-R 1是氢，卤素，烷基（C 1-3 1-3）或烷氧基（C 1-3 1-3），CN或CF 3，-R _{2是氢或烷基（C 1-3 1-3），R 3是氢或烷基（C 1-3 1-3），-Z是氢或烷基（C 1-3 1-3），烷氧基（C 1-3 1-3）或烷硫基（C 1-3 1-3），-A是氢或烷基（C 1-3 1-3），或者-A和Z一起形成可以被卤素，烷基（例如甲基），乙基（C 1-3）或苯基，其中环Z表示碳，氮的硫。}

10. 发明申请

WO9940067A2 BENZISOXAZOLE DERIVATIVES HAVING D4-ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有D4-拮抗活性的苯并恶唑衍生物
公开(公告)号：WO9940067A2
公开(公告)日：1999-08-12
申请号：PCT/EP9900852
申请日：1999-02-05
申请人： DUPHAR INT RES , HARTOG JACOBUS A J , VISSER GERBEN M , STEEN BARTHOLOMEUS J VAN , TULP MARTINUS T M , RONKEN ERIC , KRUSE CORNELIS G , LANGE JOSEPHUS H M
发明人： DEN HARTOG JACOBUS A J , VISSER GERBEN M , VAN STEEN BARTHOLOMEUS J , TULP MARTINUS T M , RONKEN ERIC , KRUSE CORNELIS G , LANGE JOSEPHUS H M
IPC分类号： A61K31/445 , A61K31/454 , A61K31/55 , A61P25/00 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D413/14 , C07D
CPC分类号： C07D413/14
摘要： The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 0, 1, or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono- or dialkyl (C1-2)-amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino, X is O, S, NH or NCH3, Y represents CH2 or (CH2)2, (R2)m represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)m is a methylene bridge or ethylene bridge, A is a group -CH2-(CRH)p- wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2- or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C-1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono- or dialkyl (C1-2)amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino.
摘要翻译：本发明涉及一组新颖的苯并异恶唑衍生物，它们是多巴胺D4-受体的有效和选择性拮抗剂。所述化合物具有通式（I）：其中（R 1）n表示0,1或2个取代基，所述取代基可以相同或不同，选自C 1-3烷基或烷氧基，卤素，三氟甲基，硝基，（C1-2） - 氨基，磺酰基 - （C1-3）烷基或 - 烷氧基，磺酰基三氟甲基，磺酰基氨基和磺酰基单或二烷基（C1-2） - 氨基，X是O，S，NH或 NCH 3，Y代表CH 2或（CH 2）2，（R 2）m代表0,1或2个可与甲基和乙基相同或不同的取代基，或（R 2）m是亚甲基桥或亚乙基桥基，A是基团-CH 2 - （CRH）p - ，其中R是氢或甲基，p是0或1，B代表2-或3-吲哚基或2-苯并咪唑基，这些基团可以在碳上被1 或C1-C3-烷基或烷氧基，卤素，三氟甲基，硝基，氨基，单或二烷基（C1-2）氨基，磺酰基 - （C1-3）烷基或 - 烷氧基，磺酰基三氟甲基，磺酰基氨基和磺酰基单或二烷基（C1-2） - 氨基。

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