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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明授权

US06197772B1 1- (1,2-disubstituted piperidinyl) -4-substituted piperazine derivatives 失效
标题翻译： 1-（1,2-二取代的哌啶基）-4-取代的哌嗪衍生物
公开(公告)号：US06197772B1
公开(公告)日：2001-03-06
申请号：US09054963
申请日：1998-04-03
申请人： Frans Eduard Janssens , François Maria Sommen , Dominique Louis Nestor Ghislaine Surleraux , Joseph Elisabeth Leenaerts , Yves Emiel Maria Van Roosbroeck
发明人： Frans Eduard Janssens , François Maria Sommen , Dominique Louis Nestor Ghislaine Surleraux , Joseph Elisabeth Leenaerts , Yves Emiel Maria Van Roosbroeck
IPC分类号： A61K31496
CPC分类号： C07D401/12 , C07D211/58 , C07D405/12 , C07D413/14 , C07D417/12 , C07D471/04 , Y02P20/55
摘要： This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, as substance-P antagonists; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及配制N-氧化物形式的化合物，其药学上可接受的加成盐和立体异构形式作为物质-P拮抗剂; 其制剂，含有它们的组合物及其作为药物的用途。

6. 发明授权

US07087595B2 Antihistaminic spiro compounds 有权
公开(公告)号：US07087595B2
公开(公告)日：2006-08-08
申请号：US10898844
申请日：2004-07-26
申请人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts
发明人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts
IPC分类号： A61P37/00 , A61K31/55 , A61K31/44
CPC分类号： C07D471/20 , C07D487/20 , C07D495/22 , C07D498/20 , C07D519/00 , Y02P20/55
摘要： This invention concerns the compounds of formula or a prodrug, a N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof wherein R1, R2, -A-B—, L, and n have the meaning given in the description. The invention relates to preparations and compositions of the present compounds and their use as medicines.

7. 发明授权

US07572786B2 Substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists 失效
公开(公告)号：US07572786B2
公开(公告)日：2009-08-11
申请号：US10540045
申请日：2003-12-17
申请人： Frans Eduard Janssens , Francois Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
发明人： Frans Eduard Janssens , Francois Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
IPC分类号： A61K31/551 , A61K31/496 , C07D211/58 , C07D211/96 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D513/04
CPC分类号： C07D405/14 , C07D211/58 , C07D211/96 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
摘要： This invention concerns substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety and depression, irritable bowel syndrom (IBS), circadian rhythm disturbances, visceral pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. 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 tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P, Neurokinin A and Neurokinin B by blocking the NK1, NK2 and NK3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality 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.

8. 发明授权

US07148214B1 Antihistaminic spiro compounds 有权
标题翻译：抗组胺螺化合物
公开(公告)号：US07148214B1
公开(公告)日：2006-12-12
申请号：US09868535
申请日：1999-12-15
申请人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts
发明人： Frans Eduard Janssens , Joseph Elisabeth Leenaerts
IPC分类号： A61K31/55 , A61K31/44 , A61P37/08 , C07D225/04 , C07D401/00
CPC分类号： C07D471/20 , C07D487/20 , C07D495/22 , C07D498/20 , C07D519/00 , Y02P20/55
摘要： This invention concerns the compounds of formula or a prodrug, a N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof wherein R1, R2, —A—B—, L, and n have the meaning given in the description. The invention relates to preparations and compositions of the present compounds and their use as medicines.
摘要翻译：本发明涉及式或其前药，N-氧化物，加成盐，季胺或立体化学异构体形式的化合物，其中R 1，R 2， -AB-，L和n具有在说明书中给出的含义。本发明涉及本发明化合物的制剂和组合物及其作为药物的用途。

9. 发明授权

US6110939A (Benzimidazolyl- and imidazopyridinyl) containing 1-(1,2-disubstituted piperidinyl) derivatives 失效
标题翻译：（苯并咪唑基 - 和咪唑并吡啶基），其含有1-（1,2-二取代的哌啶基）衍生物
公开(公告)号：US6110939A
公开(公告)日：2000-08-29
申请号：US102121
申请日：1998-06-19
申请人： Frans Eduard Janssens , Fran.cedilla.ois Maria Sommen , Dominique Louis Nester Ghislaine Surleraux , Joseph Elisabeth Leenaerts
发明人： Frans Eduard Janssens , Fran.cedilla.ois Maria Sommen , Dominique Louis Nester Ghislaine Surleraux , Joseph Elisabeth Leenaerts
IPC分类号： A61K31/00 , A61K31/415 , A61K31/435 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/498 , A61K31/55 , A61P1/00 , A61P9/00 , A61P11/00 , A61P17/00 , A61P25/00 , A61P25/04 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
CPC分类号： C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; X is a covalent bond or a bivalent radical of formula --O--, --S--, --NR.sup.3 --; .dbd.Q is .dbd.O or .dbd.NR.sup.3 ; R.sup.1 is Ar.sup.1, Ar.sup.1 C.sub.1-6 alkyl or di(Ar.sup.1)C.sub.1-6 alkyl wherein the C.sub.1-6 alkyl group is optionally substituted; R.sup.2 is Ar.sup.2, Ar.sup.2 C.sub.1-6 alkyl, Het or HetC.sub.1-6 alkyl; L is a benzimidazole or imidazopyridine derivative of formula (A) or (B) Ar.sup.1 is optionally substituted phenyl Ar.sup.2 is naphtalenyl or optionally substituted phenyl; and Het is an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.
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n为0,1或2; m为1或2，条件是如果m为2，则n为1; X是共价键或式-O-，-S-，-NR 3 - 的二价基团; = Q是= O或= NR3; R1是Ar1，Ar1C1-6烷基或二（Ar1）C1-6烷基，其中C1-6烷基任选被取代; R2是Ar2，Ar2C1-6烷基，Het或HetC1-6烷基; L是式（A）或（B）的苯并咪唑或咪唑并吡啶衍生物.Ar1是任选取代的苯基Ar 2是萘基或任选取代的苯基; Het是任选取代的单环或双环杂环; 作为P物质拮抗剂; 其制剂，含有它们的组合物及其作为药物的用途。

10. 发明授权

US07795261B2 Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists 有权
标题翻译：取代的1-哌啶-4-基-4-吡咯烷-3-基 - 哌嗪衍生物及其作为神经激肽拮抗剂的用途
公开(公告)号：US07795261B2
公开(公告)日：2010-09-14
申请号：US10540447
申请日：2003-12-17
申请人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
发明人： Frans Eduard Janssens , François Maria Sommen , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
IPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/496 , A61K31/498
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, anxiety, depression, emesis 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 tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P and Neurokinin B by blocking the NK1, NK2 and NK3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality 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特异性N-哌啶-4-基-4-吡咯烷-3-基 - 哌嗪衍生物，特别是NK1拮抗活性，组合的NK1 / NK3拮抗活性和组合的NK1 / NK2 / NK3拮抗活性，它们的制备，包含它们的组合物及其作为药物的用途，特别是用于治疗精神分裂症，焦虑，抑郁，呕吐和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-氧化物形式及其前药，其中所有取代基定义为鉴于其通过阻断神经激肽受体拮抗速激肽的作用的能力，特别是通过阻断NK1，NK2和NK3受体拮抗物质P和神经激肽B的作用，本发明的化合物是可用作药物，特别是在速激肽介导的病症例如CNS疾病，特别是分裂情感障碍，抑郁症，焦虑障碍，应激相关疾病，睡眠障碍，认知障碍，人格障碍的预防和治疗中的治疗，进食障碍，神经变性疾病，成瘾症，情绪障碍，性功能障碍疼痛等CNS相关病情; 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。

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