利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

38 条记录 (耗时 0.041 秒)

    2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine intermediates
    4.
    发明授权
    2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine intermediates 失效
    2-或3-氨基甲基-4-氨基-3,4-二氢-2H-1,4-苯并恶嗪中间体

    公开(公告)号：US5109135A

    公开(公告)日：1992-04-28

    申请号：US744558

    申请日：1991-08-13

    申请人： Thomas E. D'Ambra ,  Malcolm R. Bell

    发明人： Thomas E. D'Ambra ,  Malcolm R. Bell

    IPC分类号： C07D265/36 ,  C07D498/06 ,  C07D505/00

    CPC分类号： C07D505/00 ,  C07D265/36

    摘要： 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines, useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of a 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.

    摘要翻译： 2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶唑内酯，可用作止痛剂，通过2-或3- 氨基甲基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶嗪与芳基羧酸卤化物在路易斯酸存在下反应，或通过2-或3-氨基甲基-4-氨基 - 3,4-二氢-2H-1,4-苯并恶嗪与1-低级烷基-3-芳基-1,3-二酮或β-二芳基-β-酮戊二醛在脱水条件下反应，加热得到的腙 酸性介质。

    2- and 3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazin es
    5.
    发明授权
    2- and 3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazin es 失效
    2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶嗪

    公开(公告)号：US5066803A

    公开(公告)日：1991-11-19

    申请号：US509441

    申请日：1990-04-16

    申请人： Thomas E. D'Ambra ,  Malcolm R. Bell

    发明人： Thomas E. D'Ambra ,  Malcolm R. Bell

    IPC分类号： C07D265/36 ,  C07D498/06 ,  C07D505/00

    CPC分类号： C07D265/36 ,  C07D505/00

    摘要： 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines, useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.

    摘要翻译： 2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶唑内酯，可用作止痛剂，通过2-或3- 氨基甲基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶嗪与芳基羧酰卤在路易斯酸存在下反应，或通过2-或3-氨基甲基-4-氨基-3 ，4-二氢-2H-1,4-苯并恶嗪与1-低级烷基-3-芳基-1,3-二酮或β-芳基-β-酮戊二醛在脱水条件下反应，并将所得腙加入酸 中。

    2- and 3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo(1,2,3-DE)-1,4-benzoxazin es
    6.
    发明授权
    2- and 3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo(1,2,3-DE)-1,4-benzoxazin es 失效
    2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并（1,2,3-DE）-1,4-苯并恶嗪

    公开(公告)号：US4939138A

    公开(公告)日：1990-07-03

    申请号：US447469

    申请日：1989-12-07

    申请人： Thomas E. D'Ambra ,  Malcolm R. Bell

    发明人： Thomas E. D'Ambra ,  Malcolm R. Bell

    IPC分类号： C07D265/36 ,  C07D498/06 ,  C07D505/00

    CPC分类号： C07D505/00 ,  C07D265/36

    摘要： 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines, useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of a 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.

    摘要翻译： 2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶唑内酯，可用作止痛剂，通过2-或3- 氨基甲基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶嗪与芳基羧酸卤化物在路易斯酸存在下反应，或通过2-或3-氨基甲基-4-氨基 - 3,4-二氢-2H-1,4-苯并恶嗪与1-低级烷基-3-芳基-1,3-二酮或β-二芳基-β-酮戊二醛在脱水条件下反应，加热得到的腙 酸性介质。

    CB.sub.2 Receptor agonist compounds
    7.
    发明授权
    CB.sub.2 Receptor agonist compounds 失效

    公开(公告)号：US6013648A

    公开(公告)日：2000-01-11

    申请号：US995902

    申请日：1997-12-22

    申请人： Murielle Rinaldi ,  Francis Barth ,  Pierre Casellas ,  Christian Congy ,  Didier Oustric ,  Malcolm R. Bell ,  Thomas E. D'Ambra ,  Richard E. Philion

    发明人： Murielle Rinaldi ,  Francis Barth ,  Pierre Casellas ,  Christian Congy ,  Didier Oustric ,  Malcolm R. Bell ,  Thomas E. D'Ambra ,  Richard E. Philion

    IPC分类号： C07D295/08 ,  A61K31/135 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/435 ,  A61K31/47 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/538 ,  A61K45/00 ,  A61P29/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07D209/08 ,  C07D209/12 ,  C07D209/14 ,  C07D209/16 ,  C07D413/06 ,  C07D471/04 ,  C07D471/06 ,  C07D487/06 ,  C07D491/06 ,  C07D498/06 ,  A61K31/405

    CPC分类号： A61K31/404 ,  A61K31/5355 ,  A61K31/538

    摘要： The use of human CB.sub.2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R.sub.1 is a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11, --CHR.sub.9 CH.sub.2 NR'.sub.6 R'.sub.11, --(CH.sub.2).sub.n Z and --COR.sub.8 ; R'.sub.1 is a --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11 or --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 group; R.sub.2 and R'.sub.2 are hydrogen, halogen or C.sub.1-4 alkyl; R.sub.3 is hydrogen, C.sub.1-4 alkyl or a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 and --COR.sub.8 ; R'.sub.3 is a .dbd.CR.sub.6 R.sub.8 group; R.sub.4 has one of the meanings given for R.sub.5 or is a --COR.sub.8 group; R.sub.5 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, a halogen atom, a CF.sub.3 group, an OCF.sub.3 group or C.sub.1-4 alkylthio; R'.sub.5 has one of the meanings given for R.sub.5 and is in the 5 or 6 position of the indene ring; R.sub.6 is hydrogen or C.sub.1-4 alkyl; R'.sub.6 is C.sub.1-4 alkyl; R.sub.7 has one of the meanings given for R.sub.5 or R.sub.7 and R.sub.9 together form a --Y--CH.sub.2 -- group attached to the indole ring in the 7 position by a group Y; R.sub.8 is phenyl substituted one to four times by a substituent selected from halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy; a polycyclic ring selected from naphth-1-yl, naphth-2-yl, 1,2,3,4-tetrahydronaphth-1-yl, 1,2,3,4-tetrahydronaphth-5-yl, anthryl, benzofuryl, benzothien-2-yl, benzothien-3-yl, 2-, 3-, 4- or 8-quinolyl, said polycyclic rings optionally being substituted once or twice by a substituent selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen, cyano, hydroxyl, trifluoromethyl and imidazol-1-yl; R.sub.10 and R.sub.11 together are a group selected from --CH.sub.2 --O--CH.sub.2 --CR.sub.12 R.sub.13 -- and --(CH.sub.2).sub.p --CR.sub.12 R.sub.13 --, wherein the carbon atom substituted by R.sub.12 and R.sub.13 is attached to the nitrogen atom; R'.sub.11 is C.sub.1-4 alkyl; or R'.sub.11 and R'.sub.6, taken together with the nitrogen atom to which they are attached, form a group selected from morpholin-4-yl, thiomorpholin-4-yl, piperidin-1-yl and pyrrolidin-1-yl; each of R.sub.12 and R.sub.13 is independently hydrogen or C.sub.1-4 alkyl; n is 2, 3, 4 or 5; p is 2 or 3; Z is a methyl group or a halogen atom; and Y is a methylene group or an oxygen atom.

    4-arylcarbonyl-1-[(4-morpholinyl)-lower-alkyl]-1H-indoles
    9.
    发明授权
    4-arylcarbonyl-1-[(4-morpholinyl)-lower-alkyl]-1H-indoles 失效
    4-芳基羰基-1 - [（4-吗啉基） - 低级 - 烷基] -1H-吲哚

    公开(公告)号：US4874761A

    公开(公告)日：1989-10-17

    申请号：US337220

    申请日：1989-04-12

    申请人： Thomas E. D'Ambra ,  Malcolm R. Bell

    发明人： Thomas E. D'Ambra ,  Malcolm R. Bell

    IPC分类号： C07D209/08

    CPC分类号： C07D209/08

    摘要： 4-Arylcarbonyl-1-[(4-morpholinyl)-lower-alkyl]-1H-indoles, useful as analgesic agents, are prepared by reaction of a 3-arylcarbonyl-2-methylnitrobenzene with DMF dimethyl acetal; reductive cyclization of the product with hydrogen over a catalyst; and N-alkylation of the resulting 4-arylcarbonylindole with an appropriate 4-(halo-lower-alkyl)morpholine in the presence of a strong base.

    摘要翻译： 通过3-芳基羰基-2-甲基硝基苯与DMF二甲基缩醛的反应制备可用作止痛剂的4-芳基羰基-1 - [（4-吗啉基） - 低级 - 烷基] -1H-吲哚; 产物与催化剂上氢的还原环化; 和在强碱存在下，用合适的4-（卤代 - 低级 - 烷基）吗啉将所得的4-芳基羰基吲哚N-烷基化。

    Piperidine derivatives and process for their production
    10.
    发明授权
    Piperidine derivatives and process for their production 失效
    哌啶衍生物及其生产工艺

    公开(公告)号：US07390906B2

    公开(公告)日：2008-06-24

    申请号：US11455531

    申请日：2006-06-19

    申请人： Thomas E. D'Ambra

    发明人： Thomas E. D'Ambra

    IPC分类号： C07D211/22 ,  C07D211/40

    CPC分类号： C07D211/20 ,  C07C59/86 ,  C07C69/738 ,  C07D211/22 ,  C07D211/32

    摘要： The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.

    摘要翻译： 本发明涉及下列基本上纯的哌啶衍生物化合物：其中R 1是氢或羟基; R 2是氢; 或R 1和R 2一起形成带有R 1和R 2的碳原子之间的第二个键， ; R 3是-COOH或-COOR 4; R 4具有1至6个碳原子; A，B和D是它们各自的环的取代基，其各自可以不同或相同，并且是氢，卤素，烷基，羟基，烷氧基或其它取代基。 还公开了以基本上纯的形式制备这种哌啶衍生物化合物的方法。