利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

66 条记录 (耗时 0.038 秒)

    1,4-disubstituted piperazines
    1.
    发明授权
    1,4-disubstituted piperazines 失效
    1,4-取代的哌嗪

    公开(公告)号：US5177077A

    公开(公告)日：1993-01-05

    申请号：US728492

    申请日：1991-07-11

    申请人： Rolf Hohlweg ,  Erling Guddal ,  Erik Nielsen

    发明人： Rolf Hohlweg ,  Erling Guddal ,  Erik Nielsen

    IPC分类号： C07D333/16 ,  C07D409/12

    CPC分类号： C07D409/12 ,  C07D333/16

    摘要： A disubstituted piperazine compound having the formula I ##STR1## wherein R.sup.1 is thienyl or phenyl, which may be substituted with C.sub.1-6 -alkyl or halogen, and R.sup.2 is thienyl, which may be substituted with C.sub.1-6 -alkyl or halogen, and R.sup.3 is C.sub.1-8 -alkyl, C.sub.3-8 -alkenyl or C.sub.3-8 -cycloalkyl which all may be substituted with hydroxy, oximino or keto in any position giving a stable tertiary amine or R.sup.3 is C.sub.1-8 -alkyl or C.sub.3-8 -alkenyl which in any position may be substituted as above, but is terminally substituted with phenoxy, phenyl, thienyl, furyl, methoxy or --CN and pharmaceutically acceptable acid addition salts thereof.The compounds are useful in the treatment of mental disorders in which a dopaminergic deficit is implicated.

    摘要翻译： 具有式I的二取代哌嗪化合物（I）其中R 1是噻吩基或苯基，其可以被C 1-6 - 烷基或卤素取代，R 2是噻吩基，其可以被C 1-6 - 烷基或 卤素和R 3是C 1-8 - 烷基，C 3-8 - 烯基或C 3-8 - 环烷基，其全部可以被羟基，肟基或酮基取代，得到稳定的叔胺或R3是C1-8 - 烷基或 在任何位置可以如上所述被取代，但被苯氧基，苯基，噻吩基，呋喃基，甲氧基或-CN末端取代的C 3-8 - 烯基及其药学上可接受的酸加成盐。 这些化合物可用于治疗涉及多巴胺能缺乏症的精神障碍。

    1,4-disubstituted piperazines
    2.
    发明授权
    1,4-disubstituted piperazines 失效
    1,4-二取代的哌嗪

    公开(公告)号：US5276035A

    公开(公告)日：1994-01-04

    申请号：US879518

    申请日：1992-05-04

    申请人： Rolf Hohlweg ,  Erling Guddal ,  Erik B. Nielsen

    发明人： Rolf Hohlweg ,  Erling Guddal ,  Erik B. Nielsen

    IPC分类号： C07D261/08 ,  C07D263/10 ,  C07D271/06 ,  C07D295/084 ,  C07D295/088 ,  C07D295/15 ,  C07D333/20 ,  C07D333/22 ,  C07F9/6509 ,  A61K31/495 ,  A61K33/42 ,  C07D409/06

    CPC分类号： C07D263/10 ,  C07D261/08 ,  C07D271/06 ,  C07D295/084 ,  C07D295/088 ,  C07D295/15 ,  C07D333/20 ,  C07D333/22 ,  C07F9/650958

    摘要： A disubstituted piperazine compound having the formula ##STR1## wherein R.sup.1 is halogen, methoxy, C.sub.1-6 -alkyl or trifluoromethyl, and R.sup.2 is methyl or substituted C.sub.1-8 -alkyl, C.sub.3-8 -alkenyl or C.sub.3-8 -cycloalkyl, where substituents may be hydroxy-, keto- or oximino-groups in any position leading to a stable tertiary amine; or R.sup.2 is a straight or branched C.sub.1-8 -alkyl or C.sub.3-8 -alkenyl, which in any position may be substituted as above, but is terminally substituted with one of the following groups: cyano, optionally C.sub.1-4 -alkoxy-substituted C.sub.1-4 -alkoxy, dimethoxy, optiontionally substituted phenoxy, phosphonic acid, thienyl, furyl, oxazoline, isoxazole, oxadiazole, where the optional substitution is represented by C.sub.1-6 -alkyl or phenyl, provided that when cyano is the only substituent in R.sup.2, R.sup.2 must contain at least four carbon atoms, and pharmaceutically acceptable acid addition salts thereof.The compounds are useful in the treatment of mental disorders in which a dopaminergic deficit is implicated.

    摘要翻译： 具有式（I）的二取代哌嗪化合物，其中R 1是卤素，甲氧基，C 1-6 - 烷基或三氟甲基，R 2是甲基或取代的C 1-8 - 烷基，C 3-8 - 烯基或C 3-8 - 环烷基，其中取代基可以是导致稳定叔胺的任何位置的羟基，酮基或肟基; 或R 2是直链或支链C 1-8 - 烷基或C 3-8 - 烯基，其在任何位置可以如上所述被取代，但被下列基团之一末端取代：氰基，任选地C 1-4 - 烷氧基取代 C 1-4 - 烷氧基，二甲氧基，选择性取代的苯氧基，膦酸，噻吩基，呋喃基，恶唑啉，异恶唑，恶二唑，其中任选的取代由C 1-6 - 烷基或苯基表示，条件是当氰基是R 2中的唯一取代基 ，R2必须含有至少四个碳原子，及其药学上可接受的酸加成盐。 这些化合物可用于治疗涉及多巴胺能缺乏症的精神障碍。

    Heterocyclic H3 Antagonists
    6.
    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
    7.
    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。

    N-substituted azaheterocyclic compounds
    9.
    发明授权
    N-substituted azaheterocyclic compounds 失效
    N-取代的氮杂环化合物

    公开(公告)号：US06187770B1

    公开(公告)日：2001-02-13

    申请号：US09267302

    申请日：1999-03-15

    申请人： Tine Krogh Jørgensen ,  Rolf Hohlweg ,  Knud Erik Andersen ,  Uffe Bang Olsen ,  Zdenék Polivka ,  Karel Sindelar

    发明人： Tine Krogh Jørgensen ,  Rolf Hohlweg ,  Knud Erik Andersen ,  Uffe Bang Olsen ,  Zdenék Polivka ,  Karel Sindelar

    IPC分类号： A61K31395

    CPC分类号： C07D513/04

    摘要： The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula wherein X, Z, R1, R2 and r are as defined in the detailed part of the present description, or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation, as well as their use for treatment of indications caused by or related to the secretion and circulation of insulin antagonising peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

    摘要翻译： 本发明涉及通式为X，Z，R 1，R 2和r的新的N-取代的氮杂杂环化合物，如本说明书的详细部分所定义，或其盐，其制备方法，含有它们的组合物 ，以及它们用于临床治疗疼痛，痛觉过敏和/或炎性病症，其中C纤维通过引发神经源性疼痛或炎症而发挥病理生理学作用，以及它们用于治疗由分泌物引起或与分泌有关的适应症 和胰岛素拮抗肽的循环，例如 非胰岛素依赖性糖尿病（NIDDM）和衰老相关性肥胖。