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1. 发明授权

US08829190B2 Triazolopyridines as phosphodiesterase inhibitors for treatment of dermal diseases 有权
标题翻译：三唑并吡啶类作为治疗皮肤疾病的磷酸二酯酶抑制剂
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。

2. 发明授权

US08338431B2 Phosphodiesterase inhibitors 有权
标题翻译：磷酸二酯酶抑制剂
公开(公告)号：US08338431B2
公开(公告)日：2012-12-25
申请号：US12528649
申请日：2008-02-26
申请人： Ravindra Babu Bollu , Jakob Felding , Simon Feldbæk Nielsen , Jens Christian Højland Larsen
发明人： Ravindra Babu Bollu , Jakob Felding , Simon Feldbæk Nielsen , Jens Christian Højland Larsen
IPC分类号： A61K31/497 , A61K31/4433 , A61K31/382 , A61P17/00 , A61P35/00 , A61P29/00 , C07D213/02 , C07D491/10 , C07D241/10 , C07D335/04
CPC分类号： C07D495/10 , C07D491/10 , C07D493/10
摘要： The present invention relates to a compound according to formula I, wherein X, A, G, E, R1, R2, R3 are as shown herein; and pharmaceutically acceptable salts, hydrates, N-oxides 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.
摘要翻译：本发明涉及式I化合物，其中X，A，G，E，R 1，R 2，R 3如本文所示; 及其药学上可接受的盐，水合物，N-氧化物或溶剂合物。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。

3. 发明授权

US08148537B2 Substituted acetophenones useful as PDE4 inhibitors 有权
标题翻译：用作PDE4抑制剂的取代苯乙酮
公开(公告)号：US08148537B2
公开(公告)日：2012-04-03
申请号：US12520325
申请日：2007-12-21
申请人： Jakob Felding , Simon Feldbæk Nielsen
发明人： Jakob Felding , Simon Feldbæk Nielsen
IPC分类号： C07D213/46 , A61K31/435
CPC分类号： C07D213/61 , C07D413/12 , C07D417/12
摘要： The present invention relates to a compound according to formula: (I); 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 Xi 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, alkylcarbonyloxy, 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 processes for the preparation of said compounds, 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.
摘要翻译：本发明涉及式（I）化合物：其中X1，X2，X3，X4和X5彼此独立地表示-CH-或N; 或X3，X4和X5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并且形成另外的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，杂链烯基，烷基芳基，烷基烷氧基羰基，烷基羰氧基或烷氧基烷基， ; 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。本发明进一步涉及制备所述化合物，所述化合物用于治疗的方法，包含所述化合物的药物组合物，治疗疾病的方法。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。

4. 发明申请

US20100113442A1 TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES 有权
标题翻译：作为磷酸二酯酶抑制剂治疗牙齿疾病的三唑吡啶
公开(公告)号：US20100113442A1
公开(公告)日：2010-05-06
申请号：US12595922
申请日：2008-04-16
申请人： Jakob Felding , Morten Dahl Sornesen
发明人： Jakob Felding , Morten Dahl Sornesen
IPC分类号： A61K31/437 , C07D471/04 , A61K31/5377 , A61K31/497 , A61P35/00 , A61P17/02 , A61P17/10
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。

5. 发明申请

US20090264300A1 ENZYMATIC ENCODING METHODS FOR EFFICIENT SYNTHESIS OF LARGE LIBRARIES 有权
标题翻译：用于大型图书馆有效合成的酶法编码方法
公开(公告)号：US20090264300A1
公开(公告)日：2009-10-22
申请号：US12095778
申请日：2006-12-01
申请人： Thomas Franch , Mikkel Dybro Lundorf , Soren Nyboe Jacobsen , Eva Kampmann Olsen , Anne Lee Andersen , Anette Holtmann , Anders Holm Hansen , Anders Malling Sorensen , Anne Goldbech , Daen de Leon , Ditte Kievsmose Kaldor , Frank Abildgaard Slok , Gitte Nystrup Husemoen , Johannes Dolberg , Kim Birkebaek Jensen , Lene Pedersen , Mads Norregaard-Madsen , Michael Anders Godskesen , Sanne Schroder Glad , Sore Neve , Thomas Thisted , Tine Titilola Akinleminu Kronborg , Christian Klarner Sams , Jakob Felding , Per-Ola Freskgard , Alex Haahr Gouliaev , Henrik Pedersen
发明人： Thomas Franch , Mikkel Dybro Lundorf , Soren Nyboe Jacobsen , Eva Kampmann Olsen , Anne Lee Andersen , Anette Holtmann , Anders Holm Hansen , Anders Malling Sorensen , Anne Goldbech , Daen de Leon , Ditte Kievsmose Kaldor , Frank Abildgaard Slok , Gitte Nystrup Husemoen , Johannes Dolberg , Kim Birkebaek Jensen , Lene Pedersen , Mads Norregaard-Madsen , Michael Anders Godskesen , Sanne Schroder Glad , Sore Neve , Thomas Thisted , Tine Titilola Akinleminu Kronborg , Christian Klarner Sams , Jakob Felding , Per-Ola Freskgard , Alex Haahr Gouliaev , Henrik Pedersen
IPC分类号： C40B20/04 , C40B50/06 , C40B40/06 , C07H21/00
CPC分类号： C12N15/1068 , C12N15/1089 , C40B40/08 , C40B50/04 , C40B50/06
摘要： Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).
摘要翻译：公开了一种获得包含与单链标识符寡核苷酸连接的分子的双功能复合物的方法，其中包含化学反应位点的新生双功能复合物和用于酶标记添加的引发位点是a）在化学反应位点与一种或多种反应物，和b）在起始位点用一种或多种标记反应物的标签进行酶促反应。

6. 发明授权

US07074796B2 4-phenyl-1-piperazinyl, -piperidinyl and -tetrahydropyridyl derivatives 失效
标题翻译： 4-苯基-1-哌嗪基，哌啶基和四氢吡啶基衍生物
公开(公告)号：US07074796B2
公开(公告)日：2006-07-11
申请号：US10186339
申请日：2002-06-27
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 , C07D403/06
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; R1 and R2 are independently selected from hydrogen and halogen, provided at least one of R1 and R2 is a halogen atom; R3 is selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, aryloxy, aralkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, nitro and cyano n is 2, 3, 4 or 5; 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; hvad med acyl?? R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino nitro and cyano; 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 ; R 1和R 2独立地选自氢和卤素，条件是R 1和R 2中的至少一个和/或 >是卤原子; R 3选自氢，卤素，C 1-6烷基，三氟甲基，C 1-6烷氧基，芳氧基，芳烷氧基，羟基，氨基，C 1-6烷基氨基，二（C 1-6烷基）氨基，硝基和氰基n为2,3,4或5; 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 hvad med acyl？ R 4，R 5，R 6，R 7，R 8， R 9和R 10独立地选自氢，卤素，C 1-6烷基，三氟甲基，C 1-6烷基，羟基，氨基，C 1-6烷基氨基，二（C 1-6烷基）氨基硝基和氰基; 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。

7. 发明授权

US06743809B2 Indole Derivatives useful for the treatment of CNS disorders 失效
标题翻译：吲哚衍生物可用于治疗CNS疾病
公开(公告)号：US06743809B2
公开(公告)日：2004-06-01
申请号：US10347574
申请日：2003-01-17
申请人： Jakob Felding , Benny Bang-Andersen , Garrick Paul Smith , Kim Andersen
发明人： Jakob Felding , Benny Bang-Andersen , Garrick Paul Smith , Kim Andersen
IPC分类号： A61K31454
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to substituted indole derivatives of formula I wherein R1 is hydrogen or optionally substituted C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl or C3-8-cycloalkyl-C1-6-alkyl, or R1 is optionally substituted aryl, aryl-C1-6-alkyl, heteroaryl, heteroaryl-C1-6-alkyl or R1 is —NR′R″ wherein R′ and R″ are independently selected from hydrogen and optionally substituted C1-6-alkyl, aryl, aryl-C1-6-alkyl, heteroaryl and heteroaryl-C1-6-alkyl, or R1 is a saturated or partially saturated 5- to 6-membered ring containing one, two or three hetero atoms selected from O or S, and a group N—R9 wherein R9 is hydrogen or optionally substituted C1-6-alkyl; R2 is C1-6-alkyl W, n, X, R3-R8 are as defined in the description. The compounds of the invention are potent dopamine D4 ligands.
摘要翻译：本发明涉及式I的取代的吲哚衍生物，其中R 1是氢或任选取代的C 1-6 - 烷基，C 2-6烯基，C 2-6 - 炔基，C 3-8 - 环烷基或C 3-8 - C 1-6 - 烷基或R 1是任选取代的芳基，芳基-C 1-6 - 烷基，杂芳基，杂芳基-C 1-6 - 烷基或R 1是-NR'R“，其中R'和R “独立地选自氢和任选取代的C 1-6 - 烷基，芳基，芳基-C 1-6 - 烷基，杂芳基和杂芳基-C 1-6 - 烷基，或R 1是饱和或部分饱和的5-至含有一个，两个或三个选自O或S的杂原子的6元环和NR 9基团，其中R 9是氢或任选取代的C 1-6 - 烷基; R 2是C 1-6 - 烷基W，n，X，R 3 -R 8如说明书中所定义。本发明的化合物是有效的多巴胺D4配体。

8. 发明授权

US08932992B2 Templated molecules and methods for using such molecules 有权
标题翻译：模板分子和使用这种分子的方法
公开(公告)号：US08932992B2
公开(公告)日：2015-01-13
申请号：US12330709
申请日：2008-12-09
申请人： Henrik Pedersen , Alex Haahr Gouilaev , Thomas Franch , Christian Klarner Sams , Eva Kampmann Olsen , Frank Abilgaard Sløk , Gitte Nystrup Husemoen , Jakob Felding , Lene Hyldtoft , Mads Nørregaard-Madsen , Michael Anders Godskesen , Sanne Schrøder Glad , Thomas Thisted , Per-Ola Freskgård , Anette Holtmann
发明人： Henrik Pedersen , Alex Haahr Gouilaev , Thomas Franch , Christian Klarner Sams , Eva Kampmann Olsen , Frank Abilgaard Sløk , Gitte Nystrup Husemoen , Jakob Felding , Lene Hyldtoft , Mads Nørregaard-Madsen , Michael Anders Godskesen , Sanne Schrøder Glad , Thomas Thisted , Per-Ola Freskgård , Anette Holtmann
IPC分类号： C40B40/06 , C12Q1/68 , C12Q1/70 , G01N33/53 , C07H21/00 , C07K4/00
CPC分类号： C12N15/1068 , C07B2200/11 , C07D405/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H23/00 , C12N15/1058 , C12P19/34 , C40B40/00
摘要： The present invention relates to a method for synthesizing templated molecules. In one aspect of the invention, the templated molecules are linked to the template which templated the synthesis thereof. The intion allows the generation of libraries which can be screened for e.g. therapeutic activity.
摘要翻译：本发明涉及一种合成模板分子的方法。在本发明的一个方面，模板分子连接到模板，其模板化其合成。该内容允许生成可以被筛选的文库。治疗活动。

9. 发明授权

US08808984B2 Method for synthesising templated molecules 有权
标题翻译：合成模板分子的方法
公开(公告)号：US08808984B2
公开(公告)日：2014-08-19
申请号：US12179323
申请日：2008-07-24
申请人： Henrik Pedersen , Anette Holtmann , Thomas Franch , Alex Haahr Gouliaev , Jakob Felding
发明人： Henrik Pedersen , Anette Holtmann , Thomas Franch , Alex Haahr Gouliaev , Jakob Felding
IPC分类号： C12Q1/68 , C07H21/00 , C07H21/02 , C07H21/04 , C40B40/00 , C40B50/00
CPC分类号： C12N15/1068 , C07B2200/11 , C07D405/04 , C07H21/00 , C07H21/04 , C12Q1/6816 , C40B40/06 , C40B40/14
摘要： The invention relates to a method for synthesizing templated molecules attached to the templated which directed the synthesis thereof. The method involves a template, a scaffold functional entity and a functional entity attached to a building block, which, in turn, is attached the template. The scaffold functional entity and the functional entity of the building block are both provided with complementary dimerization domains allowing the functional entities to come into close proximity when the complementary domains interact with to each other. The method may be used for generating libraries of templated molecules which may be selected for biological activity.
摘要翻译：本发明涉及一种合成连接于模板的模板分子的方法，其指导其合成。该方法涉及模板，脚手架功能实体和连接到构件块的功能实体，其又附接模板。支架功能实体和构建单元的功能实体都具有互补的二聚化结构域，使得当互补结构域彼此相互作用时，功能实体能够接近。该方法可以用于产生可以选择用于生物活性的模板分子的文库。

10. 发明申请

US20110190282A1 NOVEL VEGF-2 RECEPTOR AND PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF 有权
标题翻译：新型VEGF-2受体和蛋白酪氨酸激酶抑制剂及其药物用途
公开(公告)号：US20110190282A1
公开(公告)日：2011-08-04
申请号：US13058797
申请日：2009-08-27
申请人： Jakob Felding , Xifu Liang , Anne Marie Horneman , Tina Dahlerup Poulsen , Jens Christian Højland Larsen
发明人： Jakob Felding , Xifu Liang , Anne Marie Horneman , Tina Dahlerup Poulsen , Jens Christian Højland Larsen
IPC分类号： A61K31/44 , C07D213/72 , C07D413/12 , C07D405/12 , C07D413/06 , A61K31/4439 , A61K31/443 , A61K31/5355 , A61P27/02 , A61P17/00 , A61P17/06 , A61P35/00 , A61P29/00 , A61P9/00
CPC分类号： C07D213/75 , C07D405/12 , C07D413/12
摘要： The invention relates to compounds of general formula (I) wherein W, D, E, G, J, L, R1, R2, R3, R4, R5 and Y are as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for treating diseases associated with deregulated angiogenesis, such as cancer and skin and eye diseases.
摘要翻译：本发明涉及其中W，D，E，G，J，L，R 1，R 2，R 3，R 4，R 5和Y如本文所定义的通式（I）的化合物及其药学上可接受的盐，水合物或溶剂合物在治疗中单独使用或与一种或多种其它药物活性化合物组合用于治疗与失调的血管生成相关的疾病，例如癌症和皮肤和眼睛疾病。

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