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1. 发明申请

WO2003097574A3 AMINOALKOXY-FUNCTIONAL CHALCONES 审中-公开
公开(公告)号：WO2003097574A3
公开(公告)日：2003-11-27
申请号：PCT/DK2003/000332
申请日：2003-05-19
申请人： LICA PHARMACEUTICALS A/S , NIELSEN, Simon, Feldbæk , BOESEN, Thomas , LARSEN, Mogens , NIELSEN, Mette, Bjerg , KROMANN, Hasse
发明人： NIELSEN, Simon, Feldbæk , BOESEN, Thomas , LARSEN, Mogens , NIELSEN, Mette, Bjerg , KROMANN, Hasse
IPC分类号： C07C217/18
摘要： The invention provides novel alkoxyaminochalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic, bacteriostatic, and bacteriocidal agents.

2. 发明申请

WO2003097574A2 AMINOALKOXY-FUNCTIONAL CHALCONES 审中-公开
标题翻译：氨基酸功能性中间体
公开(公告)号：WO2003097574A2
公开(公告)日：2003-11-27
申请号：PCT/DK2003/000332
申请日：2003-05-19
申请人： LICA PHARMACEUTICALS A/S , NIELSEN, Simon, Feldbæk , BOESEN, Thomas , LARSEN, Mogens , NIELSEN, Mette, Bjerg , KROMANN, Hasse
发明人： NIELSEN, Simon, Feldbæk , BOESEN, Thomas , LARSEN, Mogens , NIELSEN, Mette, Bjerg , KROMANN, Hasse
IPC分类号： C07C217/18
CPC分类号： C07C233/36 , C07C45/00 , C07C45/44 , C07C47/277 , C07C47/55 , C07C47/575 , C07C49/813 , C07C217/22 , C07C225/16 , C07C225/22 , C07C233/33 , C07C237/04 , C07C255/56 , C07C311/21 , C07C323/32 , C07D213/65 , C07D295/088 , C07D295/112 , C07D295/185 , C07D307/79 , C07D309/12 , C07D317/66
摘要： The invention provides novel alkoxyaminochalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic, bacteriostatic, and bacteriocidal agents.
摘要翻译：本发明提供新的烷氧基氨基查尔酮衍生物及其类似物。还公开了将化合物或其组合物用于药物活性剂，特别是抗细菌和寄生虫感染的用途。本发明还涉及一种用于检测对例如细菌，寄生虫，真菌和蠕虫的抑制作用的方法。本发明的查尔酮携带氨基取代基并显示出增强的生物效应以及改善的代谢和物理化学性质，使得化合物可用作药物物质，特别是作为抗寄生虫，抑菌剂和杀菌剂。

3. 发明申请

WO2003097575A3 AMINO-FUNCTIONAL CHALCONES 审中-公开
公开(公告)号：WO2003097575A3
公开(公告)日：2003-11-27
申请号：PCT/DK2003/000331
申请日：2003-05-19
申请人： LICA PHARMACEUTICALS A/S , NIELSEN, Simon, Feldbæk , KROMANN, Hasse , LARSEN, Mogens , HANSEN, Majbritt , BOESEN, Thomas
发明人： NIELSEN, Simon, Feldbæk , KROMANN, Hasse , LARSEN, Mogens , HANSEN, Majbritt , BOESEN, Thomas
IPC分类号： C07C225/16
摘要： The invention provides novel amino-functionalised chalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic, and bacteriocidal agents.

4. 发明申请

WO2003097575A2 AMINO-FUNCTIONAL CHALCONES 审中-公开
标题翻译：辅助功能障碍
公开(公告)号：WO2003097575A2
公开(公告)日：2003-11-27
申请号：PCT/DK2003/000331
申请日：2003-05-19
申请人： LICA PHARMACEUTICALS A/S , NIELSEN, Simon, Feldbæk , KROMANN, Hasse , LARSEN, Mogens , HANSEN, Majbritt , BOESEN, Thomas
发明人： NIELSEN, Simon, Feldbæk , KROMANN, Hasse , LARSEN, Mogens , HANSEN, Majbritt , BOESEN, Thomas
IPC分类号： C07C225/16
CPC分类号： C07C233/36 , C07C45/00 , C07C45/44 , C07C47/277 , C07C47/55 , C07C47/575 , C07C49/813 , C07C217/22 , C07C225/16 , C07C225/22 , C07C233/33 , C07C237/04 , C07C255/56 , C07C311/21 , C07C323/32 , C07D213/65 , C07D295/088 , C07D295/112 , C07D295/185 , C07D307/79 , C07D309/12 , C07D317/66
摘要： The invention provides novel amino-functionalised chalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic, and bacteriocidal agents.
摘要翻译：本发明提供新的氨基官能化查耳酮衍生物及其类似物。还公开了将化合物或其组合物用于药物活性剂，特别是抗细菌和寄生虫感染的用途。本发明还涉及一种用于检测对例如细菌，寄生虫，真菌和蠕虫的抑制作用的方法。本发明的查尔酮携带氨基取代基并表现出增强的生物效应以及改善的代谢和物理化学性质，使得该化合物可用作药物物质，特别是作为抗寄生虫剂和杀菌剂。

5. 发明申请

WO2003097576A3 DIAMINO-FUNCTIONAL CHALCONES 审中-公开
公开(公告)号：WO2003097576A3
公开(公告)日：2003-11-27
申请号：PCT/DK2003/000333
申请日：2003-05-19
申请人： LICA PHARMACEUTICALS A/S , NIELSEN, Simon, Feldbæk , SCHØNNING, Kristian , KROMANN, Hasse , BOESEN, Thomas , LARSEN, Mogens
发明人： NIELSEN, Simon, Feldbæk , SCHØNNING, Kristian , KROMANN, Hasse , BOESEN, Thomas , LARSEN, Mogens
IPC分类号： C07C225/22
摘要： The invention provides novel diamino-functionalised chalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic and bacteriostatic agents.

6. 发明申请

WO2003097576A2 DIAMINO-FUNCTIONAL CHALCONES 审中-公开
标题翻译： DIAMINO功能障碍
公开(公告)号：WO2003097576A2
公开(公告)日：2003-11-27
申请号：PCT/DK2003/000333
申请日：2003-05-19
申请人： LICA PHARMACEUTICALS A/S , NIELSEN, Simon, Feldbæk , SCHØNNING, Kristian , KROMANN, Hasse , BOESEN, Thomas , LARSEN, Mogens
发明人： NIELSEN, Simon, Feldbæk , SCHØNNING, Kristian , KROMANN, Hasse , BOESEN, Thomas , LARSEN, Mogens
IPC分类号： C07C225/22
CPC分类号： C07C233/36 , C07C45/00 , C07C45/44 , C07C47/277 , C07C47/55 , C07C47/575 , C07C49/813 , C07C217/22 , C07C225/16 , C07C225/22 , C07C233/33 , C07C237/04 , C07C255/56 , C07C311/21 , C07C323/32 , C07D213/65 , C07D295/088 , C07D295/112 , C07D295/185 , C07D307/79 , C07D309/12 , C07D317/66
摘要： The invention provides novel diamino-functionalised chalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic and bacteriostatic agents.
摘要翻译：本发明提供新的二氨基官能化查耳酮衍生物及其类似物。还公开了将化合物或其组合物用于药物活性剂，特别是抗细菌和寄生虫感染的用途。本发明还涉及一种用于检测对例如细菌，寄生虫，真菌和蠕虫的抑制作用的方法。本发明的查尔酮携带氨基取代基并表现出增强的生物效应以及改善的代谢和物理化学性质，使得该化合物可用作药物物质，特别是作为抗寄生虫和抑菌剂。

7. 发明申请

WO2005042467A1 QUATERNARY AMINO-FUNCTIONAL CHALCONES 审中-公开
标题翻译：第四季度AMINO-FUNCTIONAL CHALCONES
公开(公告)号：WO2005042467A1
公开(公告)日：2005-05-12
申请号：PCT/DK2004/000746
申请日：2004-10-28
申请人： LICA PHARMACEUTICALS A/S , NIELSEN, Simon, Feldbæk
发明人： NIELSEN, Simon, Feldbæk
IPC分类号： C07C225/22
CPC分类号： C07D295/112 , C07C217/22 , C07C225/16 , C07C225/22
摘要： The present invention provides novel quaternary amino-functional chalcone derivatives and analogues exhibiting interesting antibacterial activity. The compounds have the general formula (Y 1 ) m -Ar 1 (X 1 )-C(=O)Var 2 (X 2 )-(Y 2 ) p (I), wherein V designates -CH 2 -CH 2 -, -CH=CH-or -C=C; Ar 1 and Ar 2 independently are aryl and heteroary.; m=0, 2, p=0, 1, 2, m+p>0; each Y 1 and Y 2 independently is -Z-N + (R 1 )(R 2 )R 4 Q - (A); -NR 3 -Z-N + (R 1 )(R 2 )R 4 Q - (B), or O-Z-N + (R 1 )(R 2 )R 4 Q - (C), R 1 , R 2 , R 3 , R 4 , X 1 , X 2 are substituents, and Q - is an anion. The present invention also relates to the compounds for sue as pharmaceutically active agents, in particular against bacterial infections (such as Gram-negative and Gram-positive bacteria, including antibiotic-sensitive or resistant strains), and in the medical treatment of bacterial infections in mammals.
摘要翻译：本发明提供了具有令人感兴趣的抗菌活性的新型季氨基功能查耳酮衍生物和类似物。这些化合物具有通式（Y 1）m -Ar 1（X 1）-C（= O）Var 2（X 2） - （Y 2）p（I ），其中V表示-CH 2 -CH 2 - ， - CH = CH-或-C = C; Ar 1和Ar 2独立地是芳基和杂芳基。 m = 0,2，p = 0,1,2，m + p> 0; 每个Y 1和Y 2独立地是-Z-N +（R 1）（R 2）R 4 Q - （A）; （R 1）（R 2）R 4（B）或OZN +（R 1）（R 2））R 4（C），R 1，R 2，R 3，R 4，X 1，X 2均为取代基，是阴离子。本发明还涉及作为药物活性剂的药物，特别是针对细菌感染（例如革兰氏阴性和革兰氏阳性菌，包括抗生素敏感或抗性菌株）的化合物，以及在细菌感染的治疗中哺乳动物。

8. 发明申请

WO2005058309A1 NOVEL THERAPEUTIC USE OF INDOLINONE DERIVATIVES 审中-公开
标题翻译：吲哚啉酮衍生物的新治疗方法
公开(公告)号：WO2005058309A1
公开(公告)日：2005-06-30
申请号：PCT/DK2004/000875
申请日：2004-12-16
申请人： LEO PHARMA A/S , BOUERAT, Laetitia, Maud, Elysa , FENSHOLDT, Jef , NIELSEN, Simon, Feldbæk , LIANG, Xifu , HAVEZ, Sophie, Elisabeth , ANDERSSON, Ellen, Christina , JENSEN, Lene , HANSEN, Jens, Rainer
发明人： BOUERAT, Laetitia, Maud, Elysa , FENSHOLDT, Jef , NIELSEN, Simon, Feldbæk , LIANG, Xifu , HAVEZ, Sophie, Elisabeth , ANDERSSON, Ellen, Christina , JENSEN, Lene , HANSEN, Jens, Rainer
IPC分类号： A61K31/404
CPC分类号： A61K31/4439 , A61K31/404 , A61K31/454
摘要： Certain oxindole compounds have been found to be effective in experimentally induced autoimmune encephalitis and are therefore suggested for the preparation of a medicament for the prevention, treatment or amelioration of multiple sclerosis, or to delay the onset of or reduce the relapse rate in multiple sclerosis.
摘要翻译：已经发现某些羟吲哚化合物在实验诱导的自身免疫性脑炎中是有效的，因此建议用于制备用于预防，治疗或改善多发性硬化的药物，或延迟多发性硬化症中的复发率或降低复发率。

9. 发明申请

WO2008077404A1 SUBSTITUTED ACETOPHENONES USEFUL AS PDE4 INHIBITORS 审中-公开
标题翻译：替代的乙草胺作为PDE4抑制剂有用
公开(公告)号：WO2008077404A1
公开(公告)日：2008-07-03
申请号：PCT/DK2007/000564
申请日：2007-12-21
申请人： LEO PHARMA A/S , FELDING, Jakob , NIELSEN, Simon, Feldbæk
发明人： FELDING, Jakob , NIELSEN, Simon, Feldbæk
IPC分类号： C07D213/61 , C07D413/12 , C07D417/12 , A61K31/44 , A61K31/4427 , A61P25/00 , A61P29/00 , A61P31/00 , A61P35/00
CPC分类号： C07D213/61 , C07D413/12 , C07D417/12
摘要： The present invention relates to a compound according to formula: (I); wherein X 1 , X 2 , X 3 , X 4 and X 5 independently of each other represent -CH- or N; or X 3 , X 4 and X 5 independently of each other represent -CH- or N, and Xi and X 2 independently of each other represent C and form part of an additional 6- membered aromatic ring; R 1 represents hydrogen, alkyl, alke nyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R 2 and R 3 independently represent hydrogen, -CH 2 -C(O)NR-R', alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, alkylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R 11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X 1 -X 5 represent -CH- or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hyd rates, 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X 1，X 2，X 3，X 4和X 5，彼此独立地表示-CH-或N; 或X 3，X 4和X 5各自独立地表示-CH-或N，且X 1和X 2' 彼此独立地表示C并形成额外的6-元芳环的一部分; R 1表示氢，烷基，芳基，炔基，卤代烷基，羟基烷基或烷基羰基，它们均为任选取代的; R 2和R 3独立地表示氢，-CH 2 -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，它们均为任选取代的; 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，对映异构体和非对映异构体; 及其药学上可接受的盐，水合速率或溶剂化物。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。

10. 发明申请

WO2012003829A1 NOVEL HOMOPIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：新型双酚A衍生物作为蛋白酪氨酸激酶抑制剂及其药物用途
公开(公告)号：WO2012003829A1
公开(公告)日：2012-01-12
申请号：PCT/DK2011/000080
申请日：2011-07-08
申请人： LEO PHARMA A/S , NIELSEN, Simon, Feldbæk , GREVE, Daniel, Rodriguez , GRUE-SØRENSEN, Gunnar , RYTTERSGAARD, Carsten , SCHOU, Søren, Christian , SAMS, Anette, Graven
发明人： NIELSEN, Simon, Feldbæk , GREVE, Daniel, Rodriguez , GRUE-SØRENSEN, Gunnar , RYTTERSGAARD, Carsten , SCHOU, Søren, Christian , SAMS, Anette, Graven
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00 , A61P37/02
CPC分类号： C07D487/04 , A61K31/5513 , A61K45/00
摘要： The invention relates to compounds of general formula (I) wherein R 1 ,R 2 , R 3 , R 4 , m and n are defined 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, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disesase, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1，R 2，R 3，R 4，m和n如本文所定义，以及其药学上可接受的盐，水合物或溶剂合物，可单独使用或与一种或多种更多其他药物活性化合物 - 在治疗中，作为用于预防，治疗或改善疾病及其并发症的JAK激酶和蛋白酪氨酸激酶抑制剂，包括例如牛皮癣，特应性皮炎，酒渣鼻，狼疮，多发性硬化，类风湿性关节炎，I型糖尿病，哮喘，癌症，自身免疫性甲状腺疾病，溃疡性结肠炎，克罗恩病，阿尔茨海默病，白血病，眼睛疾病如糖尿病性视网膜病变和黄斑变性以及其他自身免疫性疾病以及例如在器官移植中需要免疫抑制的适应症。

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