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1. 发明授权

US06476060B2 4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity 有权
标题翻译：具有CB1拮抗活性的4,5-二氢-1H-吡唑衍生物
公开(公告)号：US06476060B2
公开(公告)日：2002-11-05
申请号：US09814694
申请日：2001-03-23
申请人： Josephus H. M. Lange , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Bernard J. Van Vliet
发明人： Josephus H. M. Lange , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Bernard J. Van Vliet
IPC分类号： A61K31415
CPC分类号： C07D231/06 , C07D231/08 , C07D401/04 , C07D409/04
摘要： The present invention relates, among many things, to novel 4,5-dihydro-1H-pyrazole compounds which can be potent antagonists of the cannabis CB1-receptor. The compounds have the formula (I) wherein R and R1 are the same or different and represent unsubstituted or substituted phenyl, thienyl, or pyridyl, or naphthyl. naphthyl R2 represents hydrogen, hydroxy, C1-3-alkoxy, acetyloxy or propionyloxy, Aa represents one of the groups (i), (ii), (iii), (iv) or (v) as defined herein, Bb represents sulfonyl or carbonyl, and R3 represents benzyl, phenyl, thienyl or pyridyl, each of which is unsubstituted or substituted, or R3 represents C1-8 branched or unbranched alkyl or C3-8 cycloalkyl, or R3 represents naphthyl.
摘要翻译：本发明涉及新的4,5-二氢-1H-吡唑化合物，其可以是大麻CB1-受体的有效拮抗剂。化合物具有式（I），其中R和R 1相同或不同，代表未取代或取代的苯基，噻吩基或吡啶基或萘基。萘基R 2表示氢，羟基，C 1-3 - 烷氧基，乙酰氧基或丙酰氧基，A a表示如本文所定义的基团（ⅰ），（ⅱ），（ⅲ），（ⅳ）或（Ⅴ）中的一个，Bb表示磺酰基或羰基，R 3表示苄基，苯基，噻吩基或吡啶基，其各自为未取代或取代的，或R3表示C1-8支链或非支链烷基或C3-8环烷基，或R3表示萘基。

2. 发明授权

US07456182B2 Phenylpiperazines 有权
标题翻译：苯基哌嗪
公开(公告)号：US07456182B2
公开(公告)日：2008-11-25
申请号：US11450323
申请日：2006-06-12
申请人： Roelof Van Hes , Johannes A. M. Van der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
发明人： Roelof Van Hes , Johannes A. M. Van der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
IPC分类号： A61K31/496 , C07D403/12 , C07D413/12
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 novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia.The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.
摘要翻译：本发明涉及具有令人感兴趣的药理学性质的新一组苯基哌嗪，例如对多巴胺D 2 O受体和/或5-羟色胺再摄取位点的高亲和力，以及治疗与多巴胺能和/或血清素能系统如焦虑障碍，抑郁症，帕金森病和精神分裂症。本发明涉及一组新的式（I）的苯基哌嗪衍生物：其中：X是本文定义的式1,2,3,4,5,6或7的基团，m的值为2 至6; n的值为0-2; R 5和R 6独立地是H或烷基（1-3C）; 或R 5 + R 6表示基团 - （CH 2）2 - ，其中p的值为3 -5和R 7是烷基（1-3C），烷氧基（1-3C），卤素或氰基; 或吲哚基的第7位上的R 6（R 7）表示 - （CH 2）2 - 其中q具有2-4，及其盐。

3. 发明授权

US06391896B1 3-Tetrahydropyridin-4-yl indoles for treatment of psychotic disorders 有权
标题翻译： 3-四氢吡啶-4-基吲哚用于治疗精神病
公开(公告)号：US06391896B1
公开(公告)日：2002-05-21
申请号：US09807408
申请日：2001-07-03
申请人： Roelof Van Hes , Johannes A. M. Van Der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
发明人： Roelof Van Hes , Johannes A. M. Van Der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
IPC分类号： C07D40106
CPC分类号： C07D401/14
摘要： The invention is related to the following compounds: wherein all variables are as defined in the specification. The compounds are useful for treating psychotic disorders.
摘要翻译：本发明涉及以下化合物：其中所有变量如说明书中所定义。这些化合物可用于治疗精神病。

4. 发明授权

US07605162B2 Phenylpiperazine 失效
标题翻译：苯基哌嗪
公开(公告)号：US07605162B2
公开(公告)日：2009-10-20
申请号：US12258591
申请日：2008-10-27
申请人： Roelof Van Hes , Johannes A. M. Van der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
发明人： Roelof Van Hes , Johannes A. M. Van der Heijden , Cornelis G. Kruse , Jacobus Tipker , Martinus T. M. Tulp , Gerben M. Visser , Bernard J. Van Vliet
IPC分类号： A61K31/496 , C07D403/12
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 novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia.The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.
摘要翻译：本发明涉及具有令人感兴趣的药理学性质的新一组苯基哌嗪，例如对多巴胺D2受体和/或5-羟色胺再摄取位点的高亲和力，以及治疗与多巴胺能和/或血清素能系统中的干扰相关的病症的能力，例如作为焦虑障碍，抑郁症，帕金森病和精神分裂症。本发明涉及一组新的式（I）的苯基哌嗪衍生物：其中：X是本文定义的式1,2,3,4,5,6或7的基团，m的值为2 至6; n的值为0-2; R5和R6独立地是氢或烷基（1-3C）; 或R 5 + R 6表示基团 - （CH 2）p - 其中p具有3-5，R 7是烷基（1-3C），烷氧基（1-3C），卤素或氰基; 或R6 + R7（吲哚基的第7位的R7）表示基团 - （CH 2）q，其中q具有2-4，及其盐。

5. 发明授权

US06335326B1 Benzisoxazole derivatives having d4-antagonistic activity 有权
标题翻译：具有d4拮抗活性的苯并异恶唑衍生物
公开(公告)号：US06335326B1
公开(公告)日：2002-01-01
申请号：US09601795
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 , Josephus H. M. Lange
发明人： Jacobus A. J. Den Hartog , Gerben M. Visser , Bartholomeus J. Van Steen , Martinus T. M. Tulp , Eric Ronken , Cornelis G. Kruse , Josephus H. M. Lange
IPC分类号： A01N4346
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：本发明涉及一组新的苯并异恶唑衍生物，其是多巴胺D4受体的有效和选择性拮抗剂。化合物具有通式（I），其中（R1）n表示0,1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，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，X是O，S，NH或 NCH 3，Y表示CH 2或（CH 2）2，（R 2）m表示0,1或2个与甲基和乙基基团相同或不同的取代基，或（R2）m是亚甲基桥或乙基桥，A是-CH 2 - （CRH）p - 基团，其中R是氢或甲基，p是0或1，B表示2-或3-吲哚基或2-苯并咪唑基，该基团可以在碳上被取代， 1或2个C 1-3 - 烷基或烷氧基，卤素，三氟甲基，硝基，氨基，一或二烷基（C 1-2）氨基，磺酰基 - （C 1-3）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（C 1-2） - 氨基。

6. 发明授权

US06214829B1 Piperazine compounds, their preparation, and methods of using them 有权
标题翻译：哌嗪化合物，它们的制备方法和使用它们的方法
公开(公告)号：US06214829B1
公开(公告)日：2001-04-10
申请号：US09144076
申请日：1998-08-31
申请人： Roelof W. Feenstra , Gerben M. Visser , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
发明人： Roelof W. Feenstra , Gerben M. Visser , Cornelis G. Kruse , Martinus T. M. Tulp , Stephen K. Long
IPC分类号： A61K31496
CPC分类号： C07D263/58 , C07D215/38 , C07D265/36 , C07D401/12 , C07D409/12
摘要： Novel piperazine and piperidine derivative compounds having interesting and advantageous pharmacological properties. The disdosed compounds have the general formula (a) and salts thereof. These compounds have high affinity for both the dopamine D2 receptors and serotonine 5-HT1A receptors, rendering them useful for the treatment of CNS-disorders, in particular schizophrenia.
摘要翻译：新颖的哌嗪和哌啶衍生化合物具有有趣和有利的药理学性质。所述化合物具有通式（a）及其盐。这些化合物对多巴胺D2受体和5-羟色胺5-HT 1A受体具有高亲和力，使其可用于治疗中枢神经系统疾病，特别是精神分裂症。

7. 再颁专利

USRE41425E1 Piperazine and piperidine compounds 有权
标题翻译：哌嗪和哌啶化合物
公开(公告)号：USRE41425E1
公开(公告)日：2010-07-06
申请号：US12081710
申请日：2008-04-18
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： C07D295/12 , A61K31/496
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) 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, R1 is hydrogen or fluoro, R2 is C1-4-alkyl, C1-4-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, R3 and R4 independently are hydrogen or C1-4-alkyl, n has the value 1 or 2, R5 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 (R6)q, Y is a phenyl, furanyl or thienyl group, which groups may be substituted with 1-3 substituents from the group hydroxy, halogen, CF3, C1-4-alkoxy, C1-4-alkyl, cyano aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl, R6 is halogen, hydroxy, C1-4-alkoxy or C1-4-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。

8. 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

9. 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。

10. 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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