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    Heterocyclic H3 Antagonists
    22.
    发明申请
    Heterocyclic H3 Antagonists 失效
    杂环H3拮抗剂

    公开(公告)号：US20100267721A1

    公开(公告)日：2010-10-21

    申请号：US12663103

    申请日：2008-05-19

    申请人： Rolf Hohlweg ,  Jane Marie Lundbeck ,  Johannes Cornelis de Jong

    发明人： Rolf Hohlweg ,  Jane Marie Lundbeck ,  Johannes Cornelis de Jong

    IPC分类号： A61K31/5377 ,  C07D401/14 ,  A61K31/4545 ,  C07D413/14 ,  A61K31/497 ,  C07D403/04 ,  A61K31/501 ,  A61P3/04 ,  A61P1/16 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P11/06 ,  A61P19/02 ,  A61P25/28 ,  A61P1/12 ,  A61P35/00

    CPC分类号： C07D405/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/10 ,  C07D413/14

    摘要： Compound of formula (I) wherein W, X, Y, Z is —C(R′)═ or N; R1 is hydrogen or alkyl, V is N or C (i.e. carbon), A is a bond or an alkylene linker with 1 to 3 carbon atoms, with the proviso that when A is a bond, V must be CH, R is ethyl, propyl, a branched C3-6 alkyl or a cyclic C3-8 alkyl, m and n is 1-3, D is heteroaryl optionally substituted with halogen, hydroxy, cyano, alkyl, cycloalkyl, alkoxy, —(CH2)o—(C═O)p—NR2R3, or D is aryl optionally substituted with one or more of the groups independently selected from hydrogen, halogen, hydroxy, cyano, alkyl, cycloalkyl, haloalkyl, alkoxy, haloalkoxy, alkylsulfonyl, alkylsulfinyl, heterocyclyl, heterocyclylalkyl, heterocyclyl-alkoxy, heterocyclylcarbonyl, alkylcarbonyl, alkoxycarbonyl, alkylcarboxy, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylcarbonylamino, alkylcarbonylaminoalkyl, arylcarbonylamino, aryl-carbonylaminoalkyl, heteroarylcarbonylamino or heteroarylcarbonylaminoalkyl, —(CH2)0—(C═O)p—NR2R3, wherein o is 0-3, p is 0 or 1, and R2 and R3 independently are hydrogen, alkyl or cycloalkyl; or R2 and R3, can together with the attached nitrogen form a heterocyclyl group, and salts and solvates thereof have binding affinity for the histamine H3 receptor.

    摘要翻译： 式（I）化合物，其中W，X，Y，Z为-C（R'）=或N; R1是氢或烷基，V是N或C（即碳），A是具有1至3个碳原子的键或亚烷基接头，条件是当A是键时，V必须是CH，R是乙基， 丙基，支链C 3-6烷基或环C 3-8烷基，m和n为1-3，D为任选被卤素，羟基，氰基，烷基，环烷基，烷氧基， - （CH 2）o - （C ≡O）p-NR2R3，或D是任选被一个或多个独立地选自氢，卤素，羟基，氰基，烷基，环烷基，卤代烷基，烷氧基，卤代烷氧基，烷基磺酰基，烷基亚磺酰基，杂环基，杂环基烷基，杂环基 - 烷基羰基，烷氧基羰基，烷氧基烷基，烷基羰基氨基，烷基羰基氨基烷基，芳基羰基氨基，芳基 - 羰基氨基烷基，杂芳基羰基氨基或杂芳基羰基氨基烷基， - （CH2）O-（C = O）p-NR2R3，其中o为0 -3，p为0或1，R2和R3独立地为氢，烷基o 环烷基 或R 2和R 3可以与连接的氮一起形成杂环基，其盐和溶剂合物对组胺H3受体具有结合亲和力。

    Novel Medicaments
    23.
    发明申请
    Novel Medicaments 失效
    新药

    公开(公告)号：US20090312309A1

    公开(公告)日：2009-12-17

    申请号：US11917823

    申请日：2006-06-30

    申请人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    发明人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    IPC分类号： A61K31/5513 ,  A61K31/5377 ,  A61K31/501 ,  A61K31/497 ,  C07D413/14 ,  C07D403/04

    CPC分类号： C07D213/74 ,  C07D213/84 ,  C07D213/87 ,  C07D237/20 ,  C07D403/04 ,  C07D403/12 ,  C07D417/10

    摘要： Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

    摘要翻译： 定义与组胺H3受体相互作用的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 该新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在该环的其余位置上有碳原子或氮原子。

    Medicaments
    24.
    发明授权
    Medicaments 有权
    药剂

    公开(公告)号：US08846677B2

    公开(公告)日：2014-09-30

    申请号：US13472090

    申请日：2012-05-15

    申请人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    发明人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    IPC分类号： A61K31/501 ,  C07D401/00 ,  C07D409/00

    CPC分类号： C07D213/74 ,  C07D213/84 ,  C07D213/87 ,  C07D237/20 ,  C07D403/04 ,  C07D403/12 ,  C07D417/10

    摘要： Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

    摘要翻译： 定义与组胺H3受体相互作用的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 该新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在该环的其余位置上有碳原子或氮原子。

    Medicaments
    25.
    发明授权
    Medicaments 失效
    药剂

    公开(公告)号：US08501739B2

    公开(公告)日：2013-08-06

    申请号：US11917823

    申请日：2006-06-30

    申请人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    发明人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    IPC分类号： A61K31/50 ,  C07D401/00

    CPC分类号： C07D213/74 ,  C07D213/84 ,  C07D213/87 ,  C07D237/20 ,  C07D403/04 ,  C07D403/12 ,  C07D417/10

    摘要： Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

    摘要翻译： 定义与组胺H3受体相互作用的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 该新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在该环的其余位置上有碳原子或氮原子。

    Heterocyclic H3 antagonists
    27.
    发明授权
    Heterocyclic H3 antagonists 失效
    杂环H3拮抗剂

    公开(公告)号：US08344001B2

    公开(公告)日：2013-01-01

    申请号：US12663103

    申请日：2008-05-19

    申请人： Rolf Hohlweg ,  Jane Marie Lundbeck ,  Johannes Cornelis de Jong

    发明人： Rolf Hohlweg ,  Jane Marie Lundbeck ,  Johannes Cornelis de Jong

    IPC分类号： A61K31/44

    CPC分类号： C07D405/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/10 ,  C07D413/14

    摘要： Compound of formula (I) wherein W, X, Y, Z is —C(R1)═ or N; R1 is hydrogen or alkyl, V is N or C (i.e. carbon), A is a bond or an alkylene linker with 1 to 3 carbon atoms, with the proviso that when A is a bond, V must be CH, R is ethyl, propyl, a branched C3-6 alkyl or a cyclic C3-8 alkyl, m and n is 1-3, D is heteroaryl optionally substituted with halogen, hydroxy, cyano, alkyl, cycloalkyl, alkoxy, —(CH2)0—(C═O)p—NR2R3, or D is aryl optionally substituted with one or more of the groups independently selected from hydrogen, halogen, hydroxy, cyano, alkyl, cycloalkyl, haloalkyl, alkoxy, haloalkoxy, alkylsulfonyl, alkylsulfinyl, heterocyclyl, heterocyclylalkyl, heterocyclyl-alkoxy, heterocyclylcarbonyl, alkylcarbonyl, alkoxycarbonyl, alkylcarboxy, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylcarbonylamino, alkylcarbonylaminoalkyl, arylcarbonylamino, aryl-carbonylaminoalkyl, heteroarylcarbonylamino or heteroarylcarbonylaminoalkyl, —(CH2)0—(C═O)p—NR2R3, wherein o is 0-3, p is 0 or 1, and R2 and R3 independently are hydrogen, alkyl or cycloalkyl; or R2 and R3, can together with the attached nitrogen form a heterocyclyl group, and salts and solvates thereof have binding affinity for the histamine H3 receptor.

    摘要翻译： 式（I）的化合物，其中W，X，Y，Z是-C（R 1）=或N; R1是氢或烷基，V是N或C（即碳），A是具有1至3个碳原子的键或亚烷基接头，条件是当A是键时，V必须是CH，R是乙基， 丙基，支链C 3-6烷基或环C 3-8烷基，m和n是1-3，D是任选被卤素，羟基，氰基，烷基，环烷基，烷氧基， - （CH 2）O-（C ≡O）p-NR2R3，或D是任选被一个或多个独立地选自氢，卤素，羟基，氰基，烷基，环烷基，卤代烷基，烷氧基，卤代烷氧基，烷基磺酰基，烷基亚磺酰基，杂环基，杂环基烷基，杂环基 - 烷基羰基，烷氧基羰基，烷氧基烷基，烷基羰基氨基，烷基羰基氨基烷基，芳基羰基氨基，芳基 - 羰基氨基烷基，杂芳基羰基氨基或杂芳基羰基氨基烷基， - （CH2）O-（C = O）p-NR2R3，其中o为0 -3，p为0或1，R2和R3独立地为氢，烷基o 环烷基 或R 2和R 3可以与连接的氮一起形成杂环基，其盐和溶剂合物对组胺H3受体具有结合亲和力。

    Novel Medicaments
    28.
    发明申请
    Novel Medicaments 有权
    新药

    公开(公告)号：US20120232078A1

    公开(公告)日：2012-09-13

    申请号：US13472090

    申请日：2012-05-15

    申请人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    发明人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    IPC分类号： A61K31/506 ,  A61P3/04 ,  A61P25/24 ,  A61K31/5377

    CPC分类号： C07D213/74 ,  C07D213/84 ,  C07D213/87 ,  C07D237/20 ,  C07D403/04 ,  C07D403/12 ,  C07D417/10

    摘要： Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

    摘要翻译： 定义与组胺H3受体相互作用的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 该新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在该环的其余位置上有碳原子或氮原子。

    4,5,6,7-tetrahydro-thieno[3, 2-C]pyridine derivatives, their preparation and use
    30.
    发明授权
    4,5,6,7-tetrahydro-thieno[3, 2-C]pyridine derivatives, their preparation and use 失效
    4,5,6,7-四氢 - 噻吩并[3,2-C]吡啶衍生物，其制备和用途

    公开(公告)号：US06177443B1

    公开(公告)日：2001-01-23

    申请号：US09035464

    申请日：1998-03-05

    申请人： Peter Madsen ,  Jane Marie Lundbeck ,  Niels Westergarrd ,  Lars Naerum ,  Annemarie Reinhardt Varming ,  Helle Demuth ,  Morten Heide

    发明人： Peter Madsen ,  Jane Marie Lundbeck ,  Niels Westergarrd ,  Lars Naerum ,  Annemarie Reinhardt Varming ,  Helle Demuth ,  Morten Heide

    IPC分类号： A61K3144

    CPC分类号： A61K31/4365 ,  A61K31/44 ,  A61K31/47

    摘要： The present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent and a compound of formula I wherein A together with the double bond of formula I is benzene or thiophene; R1 is optionally substituted C1-6 alkyl or optionally substituted aryl; R2 is optionally substituted C1-6-alkyl, optionally substituted aralkyl, or —COR3, wherein R3 is optionally substituted C1-6-alkyl, optionally substituted aralkyl, or optionally substituted aryl; R4 and R5 independently are hydrogen, halogen, perhalomethyl, optionally substituted C1-6-alkyl, hydroxy, optionally substituted C1-6-alkoxy, nitro, cyano, amino, optionally substituted mono- or optionally substituted di-C1-6-alkylamino, acylamino, C1-6-alkoxycarbonyl, carboxy or carbamoyl; n is 0, and m is 1, and methods of treating or preventing a disease of the endocrinologic system.

    摘要翻译： 本发明涉及包含药学上可接受的载体或稀释剂和式I化合物的药物组合物，其中A与式I的双键是苯或噻吩; R1是任选取代的C 1-6烷基或任选取代的芳基; R 2是任选取代的C 1-6 - 烷基，任选取代的芳烷基或-COR 3，其中R 3是任选取代的C 1-6 - 烷基，任选取代的芳烷基或任选取代的芳基; R 4和R 5独立地是氢，卤素，全卤甲基，任选取代的C 1-6 - 烷基，羟基，任选取代的C 1-6 - 烷氧基，硝基，氰基，氨基，任选取代的单 - 或任选取代的二-C 1-6烷基氨基， 酰基氨基，C 1-6 - 烷氧基羰基，羧基或氨基甲酰基; n为0，m为1，以及治疗或预防内分泌系统疾病的方法。