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1. 发明授权

US07282508B2 Substituted 4-phenyl-4-(1H-imidazol-2-yl)-piperidine derivatives and their use as selective non-peptide delta opioid agonists 有权
标题翻译：取代的4-苯基-4-（1H-咪唑-2-基） - 哌啶衍生物及其作为选择性非肽δ阿片激动剂的用途
公开(公告)号：US07282508B2
公开(公告)日：2007-10-16
申请号：US10491379
申请日：2002-10-10
申请人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Francisco Javier Fernández-Gadea , Antonio Gómez-Sánchez , Theo Frans Meert
发明人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Francisco Javier Fernández-Gadea , Antonio Gómez-Sánchez , Theo Frans Meert
IPC分类号： A61K31/445 , C07D401/00
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. In particular are claimed compounds according to Formula (I) in which A═B is C═O or SO2, X is a covalent bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar; or A═B and R1 together form a benzoxazolyl radical; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen. The invention also relates to processes for the preparation of the compounds according to the invention and their use in medicine, in particular as selective non-peptide δ-opioid agonists for use in the treatment of various pain conditions.
摘要翻译：本发明涉及式（I）的新的4-苯基-4- [1H-咪唑-2-基] - 哌啶衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其互变异构体及其N-氧化物形式。特别是根据式（I）的化合物，其中AB是CO或SO 2，X是共价键，R 1是烷氧基，烷氧基烷基，Ar或NR 其中R 9和R 10各自独立地是氢或Ar;其中R 9和R 10各自独立地是氢或Ar; 或A-B和R 1一起形成苯并恶唑基; p为0，R 3为任选被羟基，烷基或烷氧基羰基取代的苄基，R 4和R 5各自为氢。本发明还涉及根据本发明的化合物的制备方法及其在医学中的用途，特别是用于治疗各种疼痛病症的选择性非肽δ-阿片样物质激动剂。

2. 发明授权

US07390822B2 Substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives for reducing ischaemic damage 有权
标题翻译：取代的4-苯基-4- [1H-咪唑-2-基] - 哌啶衍生物，用于减少缺血性损伤
公开(公告)号：US07390822B2
公开(公告)日：2008-06-24
申请号：US10492778
申请日：2002-10-10
申请人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Francisco Javier Fernández-Gadea , Paul Joannes Ludovicus Herijgers , Theo Frans Meert , Antonio Gómez-Sánchez , Willem Flameng , Marcel J. M. Borgers
发明人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Francisco Javier Fernández-Gadea , Paul Joannes Ludovicus Herijgers , Theo Frans Meert , Antonio Gómez-Sánchez , Willem Flameng , Marcel J. M. Borgers
IPC分类号： A61K31/445 , A61K31/454
CPC分类号： A61K31/454
摘要： The present invention relates to an agent for reducing ischaemic damage to an organ, in particular to a heart and a brain, pharmaceutical compositions comprising said agent and the use of said agent for the treatment of ischaemic diseases to the heart and the brain. The agent comprises a substituted 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivative according to Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof, the N-oxide forms thereof and the prodrugs thereof. In particular are claimed the compounds according to Formula (I) in which A=B is C═O or SO2, X is a covalent bond, R1 is alkyloxy, alkyloxyalkyl, Ar or NR9R10, wherein R9 and R10 each independently are hydrogen or Ar; or A=B and R1 together form a benzoxazolyl radical; p is zero, R3 is benzyl optionally substituted with hydroxy, alkyl or alkyloxycarbonyl and R4 and R5 each are hydrogen. The use of said agents has important clinical ramifications with regard to the reduction of ischaemic damage to an organ in a mammal, in particular to a heart and/or a brain, the prevention of coronary artery diseases in a mammal by inducing a cardioprotective effect and the treatment and prevention of stroke.
摘要翻译：本发明涉及用于减轻对器官特别是心脏和脑的缺血性损伤的药剂，包含所述药物的药物组合物和所述药物用于治疗心脏和脑部的缺血性疾病的用途。该试剂包含根据式（I）的取代的4-苯基-4- [1H-咪唑-2-基] - 哌啶衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其互变异构形式，其N-氧化物形式及其前药。特别要求保护的是根据式（I）的化合物，其中A = B是CO或SO 2，X是共价键，R 1是烷氧基，烷氧基烷基， Ar或NR 9 R 10，其中R 9和R 10各自独立地为氢或Ar; 或A = B和R 1一起形成苯并恶唑基; p为0，R 3为任选被羟基，烷基或烷氧基羰基取代的苄基，R 4和R 5各自为氢。所述试剂的使用对于减少对哺乳动物，特别是心脏和/或脑的器官的缺血损伤，通过诱导心脏保护作用来预防哺乳动物的冠状动脉疾病，具有重要的临床后果，以及治疗和预防中风。

3. 发明授权

US07476662B2 Substituted tetracyclic imidazole derivatives, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine 有权
标题翻译：取代的四环咪唑衍生物，其制备方法，包含它们的药物组合物及其作为药物的用途
公开(公告)号：US07476662B2
公开(公告)日：2009-01-13
申请号：US10479839
申请日：2002-06-11
申请人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Koenraad Arthur Van Rossem , Manuel Jesús Alcázar-Vaca , Pedro Martínez-Jiménez , José Manuel Bartolomé-Nebreda , Antonio Gómez-Sánchez , Francisco Javier Fernández-Gadea , Jos Van Reempts
发明人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Koenraad Arthur Van Rossem , Manuel Jesús Alcázar-Vaca , Pedro Martínez-Jiménez , José Manuel Bartolomé-Nebreda , Antonio Gómez-Sánchez , Francisco Javier Fernández-Gadea , Jos Van Reempts
IPC分类号： A61K31/00 , A61P43/00 , C07D487/04 , C07D519/00 , C07D495/04 , C07D487/14
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention concerns novel substituted tetracyclic imidazole derivatives useful for the treatment of elevated intracranial pressure (ICP) and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine. The novel compounds comprise compounds according to the general Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-l-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-α]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof.
摘要翻译：本发明涉及可用于治疗升高的颅内压（ICP）和/或继发性缺血的新型取代的四环咪唑衍生物，特别是由脑损伤引起的，特别是由创伤性（TBI）和非创伤性脑损伤引起的其制备方法，包含它们的药物组合物及其作为药物的用途。新化合物包括根据通式（I）的化合物，其药学上可接受的酸或碱加成盐，其立体化学异构形式及其N-氧化物形式。特别地，优选的化合物是3- [2- [4-（11,12-二氢-6H-苯并咪唑并[2,1-b] [3]苯并氮杂-6-基）-2-（苯基-1-甲基）-1-哌啶基]乙基] -2,10-二甲基嘧啶并[1,2-a]苯并咪唑-4（10H） - 酮，其药学上可接受的酸或碱加成盐，其立体化学异构形式和N- 氧化物形式。

4. 发明授权

US07732437B2 Use of anti-histaminics for acute reduction of elevated intracranial pressure 有权
标题翻译：使用抗组胺药物急性降低颅内压升高
公开(公告)号：US07732437B2
公开(公告)日：2010-06-08
申请号：US10494006
申请日：2002-11-22
申请人： Frank Tegtmeier , Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Koenraad Arthur van Rossem , Manuel Jesús Alcázar-Vaca , Pedro Martínez-Jiménez , José Manuel Bartolomé-Nebreda , Antonio Gómez-Sánchez , Francisco Javier Fernández-Gadea , Jozef Leo Henri Van Reempts
发明人： Frank Tegtmeier , Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Koenraad Arthur van Rossem , Manuel Jesús Alcázar-Vaca , Pedro Martínez-Jiménez , José Manuel Bartolomé-Nebreda , Antonio Gómez-Sánchez , Francisco Javier Fernández-Gadea , Jozef Leo Henri Van Reempts
IPC分类号： A61P9/10 , A61P37/02 , A61P37/08 , A61K31/415 , A61K31/425 , C07D519/00 , C07D487/04 , C07D471/04
CPC分类号： C07D471/00 , C07D487/00 , C07D519/00
摘要： The invention concerns a novel histamine receptor antagonist and the use of an histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and/or secondary ischaemida, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. The novel compounds comprise compounds according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-α]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. Also claimed is the novel use of commercially available histamine H1-and H2-receptor antagonists for the reduction of intracranial pressure (ICP).
摘要翻译：本发明涉及一种新的组胺受体拮抗剂和组胺受体拮抗剂用于降低颅内压（ICP）的用途，特别是用于预防和治疗颅内压升高和/或继发性白斑，特别是由脑损伤引起的，更特别是由创伤性（TBI）和非创伤性脑损伤引起的。新化合物包括根据通式（I）的药学上可接受的酸或碱加成盐，其立体化学异构形式和其N-氧化物形式的化合物。特别地，优选的化合物是3- [2- [4-（11,12-二氢-6H-苯并咪唑并[2,1-b] [3]苯并氮杂-6-基）-2-（苯基 - 甲基） - 1-哌啶基]乙基] -2,10-二甲基嘧啶并[1,2-a]苯并咪唑-4（10H） - 酮，其药学上可接受的酸或碱加成盐，其立体化学异构形式和N-氧化物形式其中。还要求的是市售的组胺H1和H2受体拮抗剂用于降低颅内压（ICP）的新颖用途。

5. 发明授权

US06194405B1 Method of using substituted tetracyclic tetrahydrofuran derivatives 有权
标题翻译：使用取代四环四氢呋喃衍生物的方法
公开(公告)号：US06194405B1
公开(公告)日：2001-02-27
申请号：US09533625
申请日：2000-03-22
申请人： Pilar Gil-Lopetegui , Francisco Javier Fernández-Gadea , Theo Frans Meert
发明人： Pilar Gil-Lopetegui , Francisco Javier Fernández-Gadea , Theo Frans Meert
IPC分类号： A01N4346
CPC分类号： C07D493/04 , C07D307/93
摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3,4:6,7]-cyclohepta[1,2-b]-furan-2-methanamine oxalic acid. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.
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异构形式，其中n为0-6; p和q为零至4; r为0〜5; R1和R2各自独立地为氢; 任选取代的C 1-6烷基; C 1-6烷基羰基; 卤代甲基羰基; 或者R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; 每个R 3和R 4独立地是卤素，氰基，羟基，卤代甲基，卤代甲氧基，羧基，硝基，氨基，单或二（C 1-6烷基）氨基，C 1-6烷基羰基氨基，氨基磺酰基，一或二（C 1-6烷基）氨基磺酰基， C 1-6烷基，C 1-6烷氧基，C 1-6烷基羰基，C 1-6烷氧基羰基; 每个R 5独立地是C 1-6烷基，氰基或卤代甲基; X是CR 6 R 7，NR 8，O，S，S（= O）或S（= O）2; 芳基是任选取代的苯基; 条件是该化合物不是（±）-3,3a，8,12b-四氢-N-甲基-2H-二苯并[3,4：6,7] - 环庚并[1,2-b] - 呋喃-2-基 - 草胺草酸。式（I）化合物可用作治疗或预防CNS障碍，心血管疾病或胃肠道疾病的治疗剂。

6. 发明授权

US06288058B1 Substituted tetracyclic tetrahydrofuran derivatives 失效
标题翻译：取代的四环四氢呋喃衍生物
公开(公告)号：US06288058B1
公开(公告)日：2001-09-11
申请号：US09745517
申请日：2000-12-21
申请人： Pilar Gil-Lopetegui , Francisco Javier Fernández-Gadea , Theo Frans Meert
发明人： Pilar Gil-Lopetegui , Francisco Javier Fernández-Gadea , Theo Frans Meert
IPC分类号： A61K63155
CPC分类号： C07D493/04 , C07D307/93
摘要： This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; aryl is optionally substituted phenyl; provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3,4:6,7]-cyclohepta[1,2-b]-furan-2-methanamine oxalic acid. The compounds of formula (I) may be used as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.
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异构形式，其中n为0-6; p和q为零至4; r为0〜5; R1和R2各自独立地为氢; 任选取代的C 1-6烷基; C 1-6烷基羰基; 卤代甲基羰基; 或者R 1和R 2与它们所连接的氮原子一起可以形成吗啉基环或任选取代的杂环; 每个R 3和R 4独立地是卤素，氰基，羟基，卤代甲基，卤代甲氧基，羧基，硝基，氨基，单或二（C 1-6烷基）氨基，C 1-6烷基羰基氨基，氨基磺酰基，一或二（C 1-6烷基）氨基磺酰基， C 1-6烷基，C 1-6烷氧基，C 1-6烷基羰基，C 1-6烷氧基羰基; 每个R 5独立地是C 1-6烷基，氰基或卤代甲基; X是CR 6 R 7，NR 8，O，S，S（= O）或S（= O）2; 芳基是任选取代的苯基; 条件是该化合物不是（±）-3,3a，8,12b-四氢-N-甲基-2H-二苯并[3,4：6,7] - 环庚并[1,2-b] - 呋喃-2-基 - 草胺草酸。式（I）化合物可用作治疗或预防CNS障碍，心血管疾病或胃肠道疾病的治疗剂。

7. 发明授权

US07169786B2 Isoxazoline derivatives as anti-depressants 有权
标题翻译：异恶唑啉衍生物作为抗抑郁剂
公开(公告)号：US07169786B2
公开(公告)日：2007-01-30
申请号：US10468555
申请日：2002-02-13
申请人： José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Manuel Jesús Alcázar-Vaca , José Maria Cid-Nuñez , Joaquin Pastor-Fernandez , Antonius Adrianus Hendrikus Petrus Megens , Godelieve Irma Christine Maria Heylen , Xavier Jean Michel Langlois , Margaretha Henrica Maria Bakker , Thomas Horst Wolfgang Steckler
发明人： José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Manuel Jesús Alcázar-Vaca , José Maria Cid-Nuñez , Joaquin Pastor-Fernandez , Antonius Adrianus Hendrikus Petrus Megens , Godelieve Irma Christine Maria Heylen , Xavier Jean Michel Langlois , Margaretha Henrica Maria Bakker , Thomas Horst Wolfgang Steckler
IPC分类号： A61K31/496 , A61K31/454 , C07D498/04 , C07D498/14
CPC分类号： A61K31/495 , C07D261/20
摘要： The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonine (5-HT) reuptake inhibitor activity in combination with additional α2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative. Compounds according to the invention arc also suitable for treating patients with anxiety disorders and disorders of body weight. The invention also relates to novel combination of substituted isoxazolines derivatives having anti-depressant activity and/or anxiolytic activity and/or body weight control activity with antidepressants, anxiolytics and/or antipsychotics to improve efficacy and/or onset of action
摘要翻译：本发明涉及根据式（I）的取代的异恶唑啉衍生物：其中X = CH 2＃191，NR 7，S或O，R 1，R 2， 2和R 3是某些特定取代基，Pir是任选取代的哌啶基或哌嗪基，R 3表示任选取代的芳族碳环或杂环系统，其包括部分或完全氢化的烃链最大6个原子长，其中环体系连接到Pir基团并且其可以含有一个或多个选自O，N和S的杂原子; 其制备方法，包含它们的药物组合物及其作为药物的用途，特别是用于治疗抑郁症和/或焦虑和体重紊乱。根据本发明的化合物令人惊奇地显示具有与另外的α2-肾上腺素受体拮抗剂活性组合的5-羟色胺（5-HT）再摄取抑制剂活性，并且在没有镇静作用的情况下表现出强烈的抗抑郁活性。根据本发明的化合物也适用于治疗患有焦虑症和体重紊乱的患者。本发明还涉及具有抗抑郁活性和/或抗焦虑活性和/或体重控制活性的抗抑郁药，抗焦虑药和/或抗精神病药的取代的异恶唑啉衍生物的新组合，以改善作用和/或起效作用

8. 发明授权

US07081453B2 Compounds for treating impaired fundic relaxation 有权
公开(公告)号：US07081453B2
公开(公告)日：2006-07-25
申请号：US10311612
申请日：2001-06-13
申请人： Kristof Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encarnacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
发明人： Kristof Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encarnacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
IPC分类号： A61K31/397
CPC分类号： C07D411/04 , C07D491/04
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharma-ceutically acceptable acid addition salt thereof, wherein —a1═a2—a3═a4— is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH═; —Z1—Z2— is a bivalent radical; —A— is a bivalent radical of formula —N(R6)—Alk2— or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula (d-1), (d-2), (d-3), (d-4), (d-5) wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. 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 disturbed fundic accomodation

9. 发明授权

US07423048B2 Compounds for treating fundic disaccomodation 有权
公开(公告)号：US07423048B2
公开(公告)日：2008-09-09
申请号：US11355402
申请日：2006-02-16
申请人： Kristol Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encamacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
发明人： Kristol Van Emelen , Marcel Frans Leopold De Bruyn , Manuel Jesús Alcázar-Vaca , José Ignacio Andrés-Gil , Francisco Javier Fernández-Gadea , Maria Encamacion Matesanz-Ballesteros , José Manuel Bartolomé-Nebreda
IPC分类号： C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D403/06 , C07D403/14 , A61K31/436 , A61P1/14
CPC分类号： C07D411/04 , C07D491/04
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a1═a2-a3═a4- is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH═; -Z1-Z2- is a bivalent radical; -A- is a bivalent radical of formula —N(R6)-Alk2- or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ═NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. 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 disturbed fundic accomodation.

10. 发明授权

US07799785B2 Substituted tetracyclic tetahydrofuran, pyrrolidine and tetrahydrothiophene derivatives 有权
标题翻译：取代四环四氢呋喃，吡咯烷和四氢噻吩衍生物
公开(公告)号：US07799785B2
公开(公告)日：2010-09-21
申请号：US11815726
申请日：2005-12-06
申请人： José Maria Cid-Núñez , Antonius Andrianus Hendrikus Petrus Megens , Andrés Avelino Trabanco-Suárez , Mohamed Koukni , Georges Joseph Cornelius Hoornaert , Frans Josef Cornelius Compernolle , Tomasz Kozlecki , Hua Mao , Sushil Chandra Jha , Francisco Javier Fernández-Gadea
发明人： José Maria Cid-Núñez , Antonius Andrianus Hendrikus Petrus Megens , Andrés Avelino Trabanco-Suárez , Mohamed Koukni , Georges Joseph Cornelius Hoornaert , Frans Josef Cornelius Compernolle , Tomasz Kozlecki , Hua Mao , Sushil Chandra Jha , Francisco Javier Fernández-Gadea
IPC分类号： A61K31/403 , A61K31/4985 , A61K31/352 , A61P3/04 , A61P25/00 , A61K31/381 , A61K31/407 , C07D487/04 , C07D209/56 , C07D491/044
CPC分类号： C07D333/80 , C07D209/70 , C07D221/18 , C07D307/93 , C07D311/94 , C07D487/04 , C07D491/04
摘要： This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production.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.
摘要翻译：本发明涉及对5-羟色胺受体，特别是5-HT2A和5-HT2C受体以及对多巴胺受体，特别是多巴胺D2受体和去甲肾上腺素再摄取抑制性质具有结合亲和力的新型取代四环四氢呋喃，吡咯烷和四氢噻吩衍生物，包含根据本发明的化合物，其用作药物，特别是用于预防和/或治疗一系列精神和神经障碍，特别是某些精神病性，心血管和胃肠功能障碍及其生产方法。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-氧化物形式及其前药，其中所有取代基定义为在权利要求1中。

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