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1. 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）。

2. 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。

3. 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）

4. 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.

5. 发明申请

US20120238561A1 MORPHOLINOTHIAZOLES AS ALPHA 7 POSITIVE ALLOSTERIC MODULATORS 有权
标题翻译：作为ALPHA 7的阳离子调节剂的摩尔比洛兹
公开(公告)号：US20120238561A1
公开(公告)日：2012-09-20
申请号：US13512464
申请日：2010-11-25
申请人： Gregor James Macdonald , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
发明人： Gregor James Macdonald , Benoît Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts
IPC分类号： A61K31/5377 , A61P25/00 , A61P25/22 , A61P25/18 , A61P25/24 , A61P25/16 , A61P25/14 , A61P25/34 , A61P29/00 , A61P31/00 , A61P11/06 , A61P17/06 , A61P1/00 , A61P9/04 , A61P11/00 , A61P37/06 , C07D417/14 , C07D498/08 , A61K31/5386 , A61P25/28
CPC分类号： C07D417/14
摘要： The present invention relates to morpholinothiazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists.
摘要翻译：本发明涉及吗啉代噻唑衍生物及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。本发明特别涉及烟碱乙酰胆碱受体的正变构调节剂，这种正性变构调节剂具有增加烟碱受体激动剂功效的能力。

6. 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。

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

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。

9. 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。

10. 发明申请

US20060128721A1 Novel formulations of opioid-based treatments of pain comprising substituted 1,4-di-piperidin-4-yl-piperazine derivatives 审中-公开
标题翻译：基于阿片样物质治疗疼痛的新型制剂包括取代的1,4-二哌啶-4-基 - 哌嗪衍生物
公开(公告)号：US20060128721A1
公开(公告)日：2006-06-15
申请号：US10560476
申请日：2004-06-07
申请人： Frans Janssens , Francois Sommen , Benoit Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts , Yves Emiel, Maria Van Roosbroeck , Theo Frans Meert
发明人： Frans Janssens , Francois Sommen , Benoit Christian Albert Ghislain De Boeck , Joseph Elisabeth Leenaerts , Yves Emiel, Maria Van Roosbroeck , Theo Frans Meert
IPC分类号： A61K31/496
CPC分类号： A61K45/06 , A61K31/496 , A61K31/551 , A61K2300/00
摘要： This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in opioid-based acute and chronic pain treatments, more in particular in inflammatory, post-operative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NK1-receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression in opioid-based treatments of pain. The pharmaceutical formulations according to the invention comprise a pharmaceutically acceptable carrier and, as active ingredients, a therapeutically effective amount of an opioid analgesic and NK1-antagonists according to the general Formula (I) 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. The pharmaceutical composition according to the invention reduces to a large extent a number of unwanted side-effects associated with opioid analgesics, in particular emesis, respiratory depression and tolerance, thereby increasing the total tolerability of said opioids in pain treatment.
摘要翻译：本发明涉及用于基于阿片样物质治疗疼痛和/或伤害感受的新制剂，其包含具有神经激肽拮抗活性的阿片类镇痛药和1,4-二哌啶-4-基 - 哌嗪衍生物，特别是NK1 拮抗活性，所述制剂用于制备用于预防和/或治疗呕吐，疼痛和/或伤害感受，特别是基于阿片样物质的急性和慢性疼痛治疗的药物的用途，特别是在炎性，手术，急诊室（ER），突破性，神经病理性和癌症疼痛治疗，以及使用NK 1受体拮抗剂制备用于预防和/或治疗阿片样物质中呼吸抑制的药物的治疗疼痛。根据本发明的药物制剂包含药学上可接受的载体，并且作为活性成分，具有治疗有效量的根据通式（I）的药学上可接受的酸的阿片样物质止痛剂和NK 1拮抗剂或其碱加成盐，其立体化学异构形式，其N-氧化物形式和其前药，其中所有取代基如权利要求1中所定义。根据本发明的药物组合物在很大程度上降低了多个不需要的副产物，与阿片类止痛药相关的作用，特别是呕吐，呼吸抑制和耐受性，从而增加所述阿片类药物在疼痛治疗中的总耐受性。

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