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11. 发明授权

US09346809B2 Heterocyclic compounds as JAK receptor and protein tyrosine kinase inhibitors 有权
标题翻译：杂环化合物作为JAK受体和蛋白酪氨酸激酶抑制剂
公开(公告)号：US09346809B2
公开(公告)日：2016-05-24
申请号：US13382665
申请日：2010-07-08
申请人： Simon Feldbæk Nielsen , Daniel Rodriguez Greve , Carsten Ryttersgaard , Gunnar Grue-Sørensen , Erik Rytter Ottosen , Tina Dahlerup Poulsen , Søren Christian Schou , Anthony Murray
发明人： Simon Feldbæk Nielsen , Daniel Rodriguez Greve , Carsten Ryttersgaard , Gunnar Grue-Sørensen , Erik Rytter Ottosen , Tina Dahlerup Poulsen , Søren Christian Schou , Anthony Murray
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519 , C07D471/04 , A61P37/00 , A61P19/02 , A61P25/28 , A61P35/00 , A61P11/06 , A61P3/10 , A61P17/06 , A61P17/14 , A61P17/10 , A61P17/00 , A61P17/08 , A61P17/04 , A61P19/06 , A61P11/00
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： The invention relates to compounds of general formula (I) wherein A, R1, R2, R3, R4, R5, R9, 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 disease, 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A，R 1，R 2，R 3，R 4，R 5，R 9，m和n如本文所定义，及其药学上可接受的盐，水合物或溶剂化物，或与一种或多种其它药物活性化合物组合，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和适应症，其中需要免疫抑制器官移植的例子。

12. 发明申请

US20130331446A1 3-ACYL-INGENOLS II 有权
公开(公告)号：US20130331446A1
公开(公告)日：2013-12-12
申请号：US13997011
申请日：2011-12-22
申请人： Gunnar Grue-Sørensen , Xifu Liang , Thomas Högberg , Kristoffer Månsson , Per Vedsø
发明人： Gunnar Grue-Sørensen , Xifu Liang , Thomas Högberg , Kristoffer Månsson , Per Vedsø
IPC分类号： C07C69/74 , A61K45/06 , C07C69/75 , C07C255/46 , C07C229/56 , C07C69/78 , A61K31/235 , C07C69/76 , C07C229/64 , A61K31/245 , A61K31/215 , A61K31/277
CPC分类号： C07C69/74 , A61K31/215 , A61K31/235 , A61K31/245 , A61K31/277 , A61K45/06 , C07C69/013 , C07C69/75 , C07C69/753 , C07C69/76 , C07C69/78 , C07C69/92 , C07C229/56 , C07C229/58 , C07C229/64 , C07C233/54 , C07C255/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2603/86
摘要： The invention relates to compounds of general formula I, (I), wherein R is wherein R is aryl substituted by R3; or R is (C3-Ci3)-cycloalkyl, (C3-Ci3)-cycloalkenyl or (C7-Ci3)-cycloalkynyl optionally substituted by R4; 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 preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
摘要翻译：本发明涉及通式I（I）的化合物，其中R是其中R是被R3取代的芳基; 或R 3为（C 3 -C 13） - 环烷基，（C 3 -C 13） - 环烯基或任选被R 4取代的（C 7 -C 13） - 环炔基; 其药学上可接受的盐，水合物或溶剂合物，用于单独或与一种或多种其它药学活性化合物组合用于治疗，用于预防，治疗或改善响应刺激的中性粒细胞氧化性突发的反应的疾病或病症的角质形成细胞IL-8释放或响应于坏死的诱导。

13. 发明授权

US06399797B1 Vitamin D analogues 失效
标题翻译：维生素D类似物
公开(公告)号：US06399797B1
公开(公告)日：2002-06-04
申请号：US09543418
申请日：2000-04-05
申请人： Welf von Daehne , Gunnar Grue-Sørensen , Martin John Calverley , Claus Aage Svensgaard Bretting
发明人： Welf von Daehne , Gunnar Grue-Sørensen , Martin John Calverley , Claus Aage Svensgaard Bretting
IPC分类号： C07C40100
CPC分类号： C07C401/00
摘要： The present invention relates to compounds of formula (I), in which formula X is hydrogen or hydroxy or protected hydroxy; R1 an R2 stand for hydrogen, methyl or ethyl, or, when taken together with the carbon atom bearing the group X, R1 and R2 can form a C3-C5 carbocyclic ring; Q is a C3-C6 hydrocarbylene, hydrocarbylene indicating the diradical obtained after removal of 2 hydrogen atoms for a straight or banched, saturated or unsaturated hydrocarbon, in which one of any CH2 groups may optionally be replaced by an oxygen atom or a carbonyl group, such that the carbon atom (C-22) directly bonded to C-20 is an sp2 or sp3 hybridized carbon atom, i.e. bonded to 2 or 3 other atoms; and in which another of the CH2 groups may be replaced by phenylene, and where Q may optionally be substituted with one or more hydroxy or C1-C4-alkoxy groups. These compounds have been discovered to possess exceptionally high immunosuppressive activites together with high tumour cell proliferation inhibiting activities.
摘要翻译：本发明涉及式（I）化合物，其中式X为氢或羟基或被保护的羟基; R1，R2代表氢，甲基或乙基，或者当与带有基团X的碳原子一起时，R 1和R 2可以形成C 3 -C 5碳环; Q是C3-C6亚烃基，表示在去除2个氢原子之后获得的直链或带有饱和或不饱和烃的二价基团，其中任何一个CH 2基团可以任选被氧原子或羰基取代，使得直接键合到C-20的碳原子（C-22）是sp2或sp3杂化的碳原子，即键合到2或3个其它原子; 并且其中另一个CH 2基团可以被亚苯取代，并且其中Q可以任选地被一个或多个羟基或C 1 -C 4 - 烷氧基取代。已经发现这些化合物具有特别高的免疫抑制活性以及高肿瘤细胞增殖抑制活性。

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