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31. 发明授权

US08084473B2 Heterocyclic compounds with affinity to muscarinic receptors 有权
标题翻译：对毒蕈碱受体具有亲和力的杂环化合物
公开(公告)号：US08084473B2
公开(公告)日：2011-12-27
申请号：US12108275
申请日：2008-04-23
申请人： Axel Stoit , Hein K. A. C. Coolen , Cornelis G. Kruse , Jan H. Reinders , Louise Terwel, legal representative
发明人： Axel Stoit , Hein K. A. C. Coolen , Cornelis G. Kruse , Jan H. Reinders
IPC分类号： C07D413/00 , C07D401/00 , A01N43/40 , A61K31/44
CPC分类号： C07D471/08 , A61K31/439 , A61K45/06 , C07D401/04 , C07D403/04 , C07D413/04 , C07F7/1804
摘要： The present invention relates to heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof.
摘要翻译：本发明涉及式（I）的杂环化合物或其药学上可接受的盐，溶剂化物或水合物。

32. 发明申请

US20080153867A1 COMPOUNDS WITH A COMBINATION OF CANNABINOID-CB1 ANTAGONISM AND ACETYLCHOLINESTERASE INHIBITION 有权
标题翻译：具有CANNABINOID-CB1拮抗剂和乙酰胆碱酯酶抑制剂的组合的化合物
公开(公告)号：US20080153867A1
公开(公告)日：2008-06-26
申请号：US11957948
申请日：2007-12-17
申请人： Josephus H.M. Lange , Cornelis G. Kruse , Belal Shadid
发明人： Josephus H.M. Lange , Cornelis G. Kruse , Belal Shadid
IPC分类号： A61K31/4439 , C07D219/12 , A61P35/00 , A61P25/00 , A61P25/28
CPC分类号： C07D401/12
摘要： Embodiments of this invention relate to compounds having a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition is a compound of formula (1) wherein the symbols have the meanings given in the specification.
摘要翻译：本发明的实施方案涉及具有大麻素-CB 1拮抗作用和胆碱酯酶抑制的组合的化合物，包含这些化合物的药物组合物，制备这些化合物的方法，制备用于合成的新中间体的方法的这些化合物，以及制备包含这些化合物的组合物的方法。本发明还涉及通过向有需要的患者施用包含这些化合物的药物组合物来治疗阿尔茨海默病，认知障碍，记忆障碍，痴呆，注意力缺陷障碍，创伤性脑损伤，药物依赖，成瘾或药物滥用的方法。具有大麻素-CB 1拮抗剂和胆碱酯酶抑制剂的组合的化合物是式（1）的化合物，其中符号具有说明书中给出的含义。

33. 发明申请

US20070281973A1 SULPHUR CONTAINING PYRAZOLE DERIVATIVES AS SELECTIVE CANNABINOID CB1 RECEPTOR ANTAGONISTS 有权
标题翻译：含硫胺衍生物作为选择性CANNABINOID CB1受体拮抗剂
公开(公告)号：US20070281973A1
公开(公告)日：2007-12-06
申请号：US11754544
申请日：2007-05-29
申请人： Josephus H.M. Lange , Cornelis G. Kruse , Bernard J. Van Vliet
发明人： Josephus H.M. Lange , Cornelis G. Kruse , Bernard J. Van Vliet
IPC分类号： A61K31/454 , A61K31/416 , C07D403/02
CPC分类号： C07D401/12 , C07D403/12
摘要： The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, 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：本发明涉及含硫吡唑衍生物及其S-氧化的活性代谢物，作为具有高CB 1 / CB 2的选择性大麻素CB 1受体拮抗剂受体亚型选择性，制备这些化合物的方法，可用于合成这些吡唑衍生物的新中间体，包含一种或多种这些吡唑衍生物作为活性成分的药物组合物，以及使用的这些用于治疗精神和神经障碍的药物组合物。化合物具有通式（I），其中符号具有说明书中给出的含义。

34. 发明授权

US06780864B1 Piperazine and piperidine compounds 失效
标题翻译：哌嗪和哌啶化合物
公开(公告)号：US06780864B1
公开(公告)日：2004-08-24
申请号：US09831149
申请日：2001-08-14
申请人： Roelof Feenstra , Johannes A. M. Van Der Heijden , Cornelis G. Kruse , Stephen K. Long , Johannes Mos , Gerben M. Visser , Gustaaf J. M. Van Scharrenburg , Gerrit P. Toorop
发明人： Roelof Feenstra , Johannes A. M. Van Der Heijden , Cornelis G. Kruse , Stephen K. Long , Johannes Mos , Gerben M. Visser , Gustaaf J. M. Van Scharrenburg , Gerrit P. Toorop
IPC分类号： C07D26358
CPC分类号： C07D263/58 , C07D209/34 , C07D235/26 , C07D277/68 , C07D401/04 , C07D413/04 , C07D417/04 , Y02P20/55
摘要： The invention relates to a group of novel piperazine and piperidine derivatives of formula (I), wherein: S1 is hydrogen, halogen, alkyl (1-3C), CN, CF3, OCF3, SCF3, alkoxy (1-3C), amino or mono- or dialkyl (1-3C) substituted amino, or hydroxy; X represents NR3, S, CH2, O, SO or SO2, wherein R3 is H or alkyl (1-3C); . . . Z represents ═C or —N; —R1 independently represent H or alkyl (1-3C), or R1 and R2 together can form a bridge 2 or 3 C-atoms; R4 is hydrogen or alkyl (1-3C); Q is methyl, ethyl, ethyl substituted with one or more fluorine atoms, cyclopropyl—methyl, optionally substituted with one or more fluorine atoms, and salts and prodrugs thereof. It has been found that these compounds have both partial dopamine D2-receptor agonism and partial serotonin 5-HT1A-receptor agonism mediated activities.
摘要翻译：本发明涉及一组式（I）的新的哌嗪和哌啶衍生物，其中：S1为氢，卤素，烷基（1-3C），CN，CF3，OCF3，SCF3，烷氧基（1-3C），氨基或单或二烷基（1-3C）取代的氨基或羟基; X表示NR 3，S，CH 2，O，SO或SO 2，其中R 3是H或烷基（1-3C）; 。。。 Z表示= C或-N; -R1独立地表示H或烷基（1-3C），或者R1和R2一起可以形成桥2或3个C原子; R4是氢或烷基（1-3C）; Q是甲基，乙基，被一个或多个氟原子取代的乙基，任选被一个或多个氟原子取代的环丙基甲基，及其盐和前药。已经发现这些化合物具有部分多巴胺D2受体激动和部分5-羟色胺5-HT 1A受体激动介导的活性。

35. 发明授权

US06281216B1 2-aminoquinoline derivatives having d4-agonistic activity 有权
标题翻译：具有d4-激动活性的2-氨基喹啉衍生物
公开(公告)号：US06281216B1
公开(公告)日：2001-08-28
申请号：US09601765
申请日：2000-10-23
申请人： Jacobus A. J. Den Hartog , Gerben M. Visser , Bartholomeus J. Van Steen , Martinus T. M. Tulp , Eric Ronken , Cornelis G. Kruse
发明人： Jacobus A. J. Den Hartog , Gerben M. Visser , Bartholomeus J. Van Steen , Martinus T. M. Tulp , Eric Ronken , Cornelis G. Kruse
IPC分类号： A61K31496
CPC分类号： C07D215/38 , C07D401/12 , C07D405/12
摘要： The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 1 or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)amino, or two groups R1 at adjacent carbon atoms together with the benzene ring may form the benzdioxane group or benzofuran group, X represents nitrogen or carbon, and the dotted line may represent a double bond, (R2)p represents 0, 1 or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)p is a methylene bridge or ethylene bridge, R3 is hydrogen or methyl, and (R)m represents 0, 1, or 2 substituents, which can be the same or different and can be located at all available positions of the quinolyl group, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)amino, on the understanding that R1 cannot represent o-OCH3 when X is nitrogen, (R2)p and R3 are hydrogen, m is 0 and n is 1
摘要翻译：本发明涉及一组新的2-氨基喹啉衍生物，其是多巴胺D4-受体的有效和选择性激动剂。化合物具有通式（I），其中（R1）n表示1或2个可以相同或不同的取代基，可以是C1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，氨基和单 - 或二烷基（C1-2）氨基或相邻碳原子上的两个基团R 1与苯环可以形成苯并二恶烷基或苯并呋喃基，X代表氮或碳，虚线可以表示双键，（R2）p 代表0,1或2个与甲基和乙基基团相同或不同的取代基，或（R2）p是亚甲基桥或乙烯桥，R3是氢或甲基，（R）m表示0， 1或2个取代基，其可以相同或不同，并且可以位于喹啉基的所有可用位置，C 1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，氨基和单 - 或二烷基（C1-2）氨基，可以理解，当X是氮时，R1不能表示o-OCH3，（R2）p和R3是氢，m是0，而ni s 1

36. 发明授权

US6090812A Piperazine and piperidine compounds 有权
标题翻译：哌嗪和哌啶化合物
公开(公告)号：US6090812A
公开(公告)日：2000-07-18
申请号：US158520
申请日：1998-09-22
申请人： Roelof Willem Feenstra , Jacobus A. J. Den Hartog , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
发明人： Roelof Willem Feenstra , Jacobus A. J. Den Hartog , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
IPC分类号： C07D411/12 , A61K31/00 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D295/12
CPC分类号： C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12
摘要： A group of new piperazine and piperidine compounds having interesting advantageous pharmacological properties and have the formula (a) ##STR1## wherein A represents a heterocyclic group having 5-7 ring atoms wherein 1-3 heteroatoms selected from the group O, N and S are present,R.sub.1 is hydrogen or fluoro,R.sub.2 is C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or an oxo group, and p is 0, 1 or 2,Z represents carbon or nitrogen, and the dotted line represents a single bond when Z is nitrogen, and represents a single or double bond when Z is carbon,R.sub.3 and R.sub.4 independently are hydrogen or C.sub.1-4 -alkyl,n has the value 1 or 2,R.sub.5 is 2-pyridyl, 3-pyridyl or 4-pyridyl substituted at the meta-position with respect to the methylene bridge with a group Y, and optionally substituted with (R.sub.6)q,Y is a phenyl, furanyl or thienyl group, which groups may be substituted with 1-3 substituents from the group hydroxy, halogen, CF.sub.3, C.sub.1-4 -alkoxy, C.sub.1-4 -alkyl, cyano aminocarbonyl, mono- or di-C.sub.1-4 -alkylaminocarbonyl,R.sub.6 is halogen, hydroxy, C.sub.1-4 -alkoxy or C.sub.1-4 -alkyl, and q is 0, 1, 2 or 3 and salts thereof, are disclosed.
摘要翻译：一组具有有趣的药理学性质的新的哌嗪和哌啶化合物，其具有式（a）其中A表示具有5-7个环原子的杂环基，其中存在1-3个选自O，N和S的杂原子，R 1 是氢或氟，R 2是C 1-4 - 烷基，C 1-4 - 烷氧基或氧代基，p是0,1或2，Z表示碳或氮，当Z是氮时，虚线表示单键并且当Z是碳时表示单键或双键，R 3和R 4独立地是氢或C 1-4 - 烷基，n具有数值1或2，R 5是2-吡啶基，3-吡啶基或4-吡啶基相对于具有基团Y的亚甲基桥的间位，并且任选地被（R 6）q取代，Y是苯基，呋喃基或噻吩基，该基团可以被1-3个取代基取代，羟基，卤素， CF 3，C 1-4 - 烷氧基，C 1-4 - 烷基，氰基氨基羰基，单 - 或二-C 1-4 - 烷基氨基羰基，R 6是卤素，羟基， C 1-4 - 烷氧基或C 1-4 - 烷基，q为0,1,2或3及其盐。

37. 发明授权

US5348949A Method of preparing N-oxo-tetrahydro-.beta.-carbolines 失效
标题翻译：制备N-氧代 - 四氢-β-咔啉的方法
公开(公告)号：US5348949A
公开(公告)日：1994-09-20
申请号：US16675
申请日：1993-02-12
申请人： Peter H. H. Hermkens , Jan H. Van Maarseveen , Johan W. Scheeren , Cornelis G. Kruse
发明人： Peter H. H. Hermkens , Jan H. Van Maarseveen , Johan W. Scheeren , Cornelis G. Kruse
IPC分类号： C07D209/14 , A61K31/435 , A61K31/535 , A61K31/55 , A61P31/12 , A61P35/00 , C07D498/14 , C07D499/14 , C07D515/14 , C07D209/24
CPC分类号： C07D515/14
摘要： The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## by an intramolecular ringclosure reaction of compounds of formula 2. ##STR2## wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a function during the ringclosure reaction.The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumour activity.
摘要翻译：本发明涉及制备式I化合物的N-氧代 - 四氢-β-咔啉的方法。式（2）化合物的反应其中Z是醛官能团或缩醛官能团，或是一种官能团，可以在环形防腐反应过程中转化成这样的功能。具有式1的化合物组中的雌二醇衍生物具有强的抗病毒和抗肿瘤活性。

38. 发明授权

US5189219A Method for the preparation of erythro vicinal amino-alcohols 失效
标题翻译：制备硫代氨基甲醇的方法
公开(公告)号：US5189219A
公开(公告)日：1993-02-23
申请号：US810139
申请日：1991-12-19
申请人： Johannes Brussee , Arne van der Gen , Cornelis G. Kruse
发明人： Johannes Brussee , Arne van der Gen , Cornelis G. Kruse
IPC分类号： C07F7/18 , C07B53/00 , C07C213/00 , C07C213/02 , C07C215/30 , C07C215/52 , C07C215/60
CPC分类号： C07C213/02 , C07C213/00 , C07C215/30 , Y02P20/55
摘要： The present invention is concerned with the preparation of erythro N-substituted vicinal aminoalcohol derivatives from hydroxyl-protected cyanohydrin derivatives by successive Grignard reaction, transimination using a primary amine, reduction of the resulting imine and removal of the hydroxyl-protecting group. The products are obtained either as a racemate or in an optically pure form, depending upon the stereochemical composition of the cyanohydrin derivatives.

39. 发明授权

US4791132A Phenyl, Pyrrolidin-2-yl substituted pyrroles having antipsychotic properties 失效
标题翻译：具有抗精神病性质的苯基，吡咯烷-2-基取代的吡咯
公开(公告)号：US4791132A
公开(公告)日：1988-12-13
申请号：US94746
申请日：1987-09-09
申请人： Ineke Van Wijngaarden , Cornelis G. Kruse , Roelof Van Hes , Johannes A. M. Van Der Heyden
发明人： Ineke Van Wijngaarden , Cornelis G. Kruse , Roelof Van Hes , Johannes A. M. Van Der Heyden
IPC分类号： A61K31/40 , A61P25/00 , C07D207/32 , C07D207/333 , C07D207/335 , C07D403/04 , C07D405/04 , C07D207/30
CPC分类号： C07D207/333 , C07D207/335 , C07D403/04 , C07D405/04
摘要： The invention relates to a group of new phenyl, pyrrolidin-2-yl substituted 5-ring heterocyclic compounds of the formula ##STR1## wherein A is an unsaturated heterocyclic 5-ring having at least one nitrogen or oxygen atom in the ring, with the proviso that the phenyl substituent is in a meta-position with respect to the 2-pyrrolidinyl substituent.The compounds have interesting pharmacological, notably antipsychotic properties.

40. 发明授权

US4772604A Phenyl-substituted (N-piperazinyl) methylazoles for treating affections in the central nervous system 失效
标题翻译：用于治疗中枢神经系统感觉的苯基取代的（N-哌嗪基）甲基唑
公开(公告)号：US4772604A
公开(公告)日：1988-09-20
申请号：US18164
申请日：1987-02-24
申请人： Ineke van Wijngaarden , Cornelis G. Kruse , Johannes A. M. van der Heyden , Martinus T. M. Tulp
发明人： Ineke van Wijngaarden , Cornelis G. Kruse , Johannes A. M. van der Heyden , Martinus T. M. Tulp
IPC分类号： C07D319/00 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/495 , A61P25/18 , A61P25/20 , C07D207/32 , C07D207/335 , C07D231/12 , C07D321/00 , C07D401/06 , C07D403/06 , C07D405/12
CPC分类号： C07D207/335 , C07D231/12 , C07D401/06 , C07D403/06
摘要： The invention relates to new aryl-substituted (N-piperidinyl)methyl- and (N-piperazinyl)methylazoles having interesting pharmacological, notably antipsychotic, properties.The compounds may be prepared in a manner known for the synthesis of analogous compounds and be processed to compositions according to known methods.

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