公开(公告)号：US20060148815A1

公开(公告)日：2006-07-06

申请号：US11377772

申请日：2006-03-15

申请人： Benny Bang-Andersen ,  Jan Kehler ,  Jakob Felding

发明人： Benny Bang-Andersen ,  Jan Kehler ,  Jakob Felding

IPC分类号： A61K31/496 ,  A61K31/454 ,  C07D403/02 ,  C07D401/02

CPC分类号： C07D215/227 ,  C07D209/08 ,  C07D209/30 ,  C07D217/06 ,  C07D295/073

摘要： The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; provided that X is not O or S when the group Q is attached via an N atom; and any of its enantiomers and acid addition salts thereof. These compounds have high affinity for D4 receptors.

摘要翻译： 本发明涉及具有式I的取代的4-苯基-1-哌嗪基衍生物，其中W是C，CH或N，当W是C时，由W发出的虚线表示键，当W是N或CH时，没有键 ; X是CH 2，O，S，CO，CS，SO或SO 2; Q为下式的基团，其中Z为3至4个链成员的链; 其中链成员选自C，CH，CH 2，CO，N和NH，条件是链中只有一个可以是N或NH，并且所述链任选地含有一个或两个双 债券 条件是当基团Q经由N原子连接时，X不为O或S; 及其任何对映异构体及其酸加成盐。 这些化合物对D 4 S受体具有高亲和力。

公开(公告)号：US06762307B2

公开(公告)日：2004-07-13

申请号：US10183958

申请日：2002-06-25

申请人： Hans Petersen ,  Jakob Felding

发明人： Hans Petersen ,  Jakob Felding

IPC分类号： C07D30778

CPC分类号： C07D307/87 ,  C07C215/34 ,  C07D307/28 ,  Y02P20/55

摘要： The present invention relates to a method for the preparation of citalopram or any of its enantiomers and acid addition salts thereof comprising reaction of a compound of formula II with a diene having the formula wherein X is O, S, SO2, —N═N—, —CO—O—, —O—CO—, or or with a diene having the formula wherein R is alkyl or optionally substituted aryl or arylalkyl. The invention also relates to intermediates used in the new process for the preparation of citalopram, as well as citalopram prepared according to the new process.

摘要翻译： 本发明涉及一种制备西酞普兰或其任何对映异构体及其酸加成盐的方法，其包括式Ⅱ化合物与具有式（Ⅳ）的二烯的反应为O，S，SO 2，-N = N-， CO-O-，-O-CO-，oror与具有式R取代的二烯的烷基或任选取代的芳基或芳基烷基。本发明还涉及用于制备西酞普兰的新方法中的中间体，以及西酞普兰 根据新进程。

公开(公告)号：US08829190B2

公开(公告)日：2014-09-09

申请号：US12595922

申请日：2008-04-16

申请人： Jakob Felding ,  Morten Dahl Sørensen

发明人： Jakob Felding ,  Morten Dahl Sørensen

IPC分类号： C07D471/04 ,  A61K31/437

CPC分类号： C07D471/04 ,  A61K31/437

摘要： The present invention relates to a compound according to formula (I), wherein X and Y are either C and N or N and C; Z is CH2, CH2—CH2, CH2—NH, or NH; R1 is halogen, or R1 is alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, cycloalkyl, alkoxycarbonyl, aryl, all of which are optionally substituted; R2 is hydrogen, or R2 is alkyl, cycloalkyl, alkoxy, heterocycloalkyl, aryl, heteroaryl, alkoxycarbonyl, aminocarbonyl, amino, all of which are optionally substituted; A is aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocycloalkyl or heterocycloalkenyl, all of which are optionally substituted; and pharmaceutically acceptable salts, hydrates, or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments, in particular for the treatment of dermal diseases.

摘要翻译： 本发明涉及式（I）化合物，其中X和Y为C和N或N和C; Z是CH 2，CH 2 -CH 2，CH 2 -NH或NH; R1是卤素，或R1是烷基，烯基，炔基，卤代烷基，烷氧基，环烷基，烷氧基羰基，芳基，它们都是任选被取代的; R2是氢，或R2是烷基，环烷基，烷氧基，杂环烷基，芳基，杂芳基，烷氧基羰基，氨基羰基，氨基，它们都是任选被取代的; A是芳基，环烷基，环烯基，杂芳基，杂环烷基或杂环烯基，它们都是任选被取代的; 和其药学上可接受的盐，水合物或溶剂合物。 本发明还涉及用于治疗的所述化合物，包含所述化合物的药物组合物，治疗疾病的方法，例如， 所述化合物的皮肤病，以及所述化合物在制备药物中的用途，特别是用于治疗真皮疾病。

公开(公告)号：US08497380B2

公开(公告)日：2013-07-30

申请号：US13546758

申请日：2012-07-11

申请人： Jakob Felding ,  Simon Feldbæk Nielsen

发明人： Jakob Felding ,  Simon Feldbæk Nielsen

IPC分类号： A61K31/44 ,  C07D211/70

CPC分类号： C07D213/61 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to a compound according to formula: (1); wherein X1, X2, X3, X4 and X5 independently of each other represent —CH— or N; or X3, X4 and X5 independently of each other represent —CH— or N, and X1 and X2 independently of each other represent C and form part of an additional 6-membered aromatic ring; R1 represents hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R2 and R3 independently represent hydrogen, —CH2, —C(O)NR—R′, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, aikylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5 represent —CH— or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to methods of treating dermal disease.

摘要翻译： 本发明涉及式（1）化合物： 其中X1，X2，X3，X4和X5彼此独立地表示-CH-或N; 或X 3，X 4和X 5彼此独立地表示-CH-或N，并且X 1和X 2彼此独立地表示C并形成另外的6元芳环的一部分; R 1表示氢，烷基，烯基，炔基，卤代烷基，羟基烷基或烷基羰基，它们均为任选取代的; R2和R3独立地表示氢，-CH2，-C（O）NR-R'，烷基，环烷基，烯基，环烯基，炔基，卤代烷基，羟基烷基，杂环烯基，烷基芳基，烷基烷氧基羰基，烷基羰基氧基或烷氧基烷基， 取代 R 11表示氢，卤素，氰基，氨基，烷氧基或烷基氨基，X 1 -X 5表示-CH-或N，包括N-氧化物，对映体和非对映体; 及其药学上可接受的盐，水合物或溶剂化物。 本发明进一步涉及治疗真皮病的方法。

公开(公告)号：US20050176729A1

公开(公告)日：2005-08-11

申请号：US11073497

申请日：2005-03-03

申请人： Benny Bang-Andersen ,  Jakob Felding ,  Jan Kehler ,  Kim Andersen

发明人： Benny Bang-Andersen ,  Jakob Felding ,  Jan Kehler ,  Kim Andersen

IPC分类号： A61K31/4709 ,  A61K31/4725 ,  A61K31/538 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  C07D401/14 ,  C07D413/14 ,  A61K31/496 ,  C07D43/14

CPC分类号： C07D401/14 ,  C07D413/14

摘要： The present invention relates to dopamine D4 ligands having the general formula I wherein R1-R10, W, X, Y1-Y4, and n are as described herein. The compounds of the invention are potent dopamine D4 receptor ligands.

摘要翻译： 本发明涉及具有通式I的多巴胺D 4配体，其中R 1，R 2，R 10，W，X，Y， 1 4，n如本文所述。 本发明的化合物是有效的多巴胺D 4 S受体配体。