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1. 发明授权

US06734291B2 Synthesis of [2.2.1]bicyclo nucleosides 有权
标题翻译： [2.2.1]双环核苷的合成
公开(公告)号：US06734291B2
公开(公告)日：2004-05-11
申请号：US10233177
申请日：2002-12-16
申请人： Alexei Kochkine , Jef Fensholdt , Henrik M. Pfundheller
发明人： Alexei Kochkine , Jef Fensholdt , Henrik M. Pfundheller
IPC分类号： C07H1504
CPC分类号： C07H19/06 , C07H19/16
摘要： A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-&agr;-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5′-sulfonated ring-closed intermediate also allows for synthesis of 5′-amino- and thio-LNAs
摘要翻译：较短且提供更高总产率的[2.2.1]双环核苷的合成通过通式III的关键中间体进行，其中R 4和R 5为例如磺酸盐，且R 7为例如卤素或乙酸盐。从通式II的化合物，如3-O-芳基-4-C-羟甲基-1,2-邻 - 异丙叉-α-D-呋喃核糖，通式Ⅲ的中间体适用于与甲硅烷基化的核碱基偶联。在形成的[2.2.1]双环核苷上进行一锅碱诱导的闭环和脱磺化，证明了向腺苷，胞嘧啶，尿苷，胸苷和胍的每个LNA（锁定核酸）衍生物的短路径。使用5'-磺化的闭环中间体还可以合成5'-氨基和硫代-LNA

2. 发明申请

US20100317582A1 NOVEL CYCLIC HYDROCARBON COMPOUNDS FOR THE TREATMENT OF DISEASES 审中-公开
标题翻译：用于治疗疾病的新型循环碳水化合物
公开(公告)号：US20100317582A1
公开(公告)日：2010-12-16
申请号：US12744137
申请日：2008-11-20
申请人： Jef Fensholdt , Sophie Elisabeth Havez , Bjarne Nørremark
发明人： Jef Fensholdt , Sophie Elisabeth Havez , Bjarne Nørremark
IPC分类号： A61K38/23 , C07C211/30 , A61K31/137 , C07D295/027 , A61K31/5375 , C07D271/06 , A61K31/4245 , A61P25/28 , A61P9/10 , A61P13/12 , A61K31/59
CPC分类号： C07D295/182 , C07C211/35 , C07C211/36 , C07C211/48 , C07C215/28 , C07C217/52 , C07C217/74 , C07C233/05 , C07C233/41 , C07C237/24 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/36 , C07C237/40 , C07C239/14 , C07C255/03 , C07C255/32 , C07C255/50 , C07C257/18 , C07C259/10 , C07C259/18 , C07C271/44 , C07C309/15 , C07C311/05 , C07C311/08 , C07C311/37 , C07C311/51 , C07C317/32 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/80 , C07D231/12 , C07D231/40 , C07D233/61 , C07D233/90 , C07D263/22 , C07D271/06 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/192 , C07D295/195 , C07D295/26 , C07D305/08 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/79 , C07D309/10 , C07D319/18 , C07D333/38 , C07D333/40 , C07D333/58 , C07D413/04 , C07D413/06 , C07D417/06
摘要： The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
摘要翻译：本发明涉及新的环烃化合物及其衍生物，其制备方法，用作药物的所述化合物，用于治疗的所述化合物，包含所述化合物的药物组合物，涉及用所述化合物治疗疾病的方法，以及所述化合物在制备药物中的用途。

3. 发明授权

US06639059B1 Synthesis of [2.2.1]bicyclo nucleosides 有权
标题翻译： [2.2.1]双环核苷的合成
公开(公告)号：US06639059B1
公开(公告)日：2003-10-28
申请号：US09534769
申请日：2000-03-24
申请人： Alexei Kochkine , Jef Fensholdt , Henrik M. Pfundheller
发明人： Alexei Kochkine , Jef Fensholdt , Henrik M. Pfundheller
IPC分类号： C07H1500
CPC分类号： C07H19/06 , C07H19/16
摘要： A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-&agr;-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5′-sulfonated ring-closed intermediate also allows for synthesis of 5′-amino- and thio-LNAs.
摘要翻译：较短且提供更高总产率的[2.2.1]双环核苷的合成通过通式III的关键中间体进行，其中R 4和R 5为例如磺酸盐，且R 7为例如卤素或乙酸盐。从通式II的化合物，如3-O-芳基-4-C-羟甲基-1,2-邻 - 异丙叉-α-D-呋喃核糖，通式Ⅲ的中间体适用于与甲硅烷基化的核碱基偶联。在形成的[2.2.1]双环核苷上进行一锅碱诱导的闭环和脱磺化，证明了向腺苷，胞嘧啶，尿苷，胸苷和胍的每个LNA（锁定核酸）衍生物的短路径。使用5'-磺化的闭环中间体还可以合成5'-氨基和硫代-LNA。

4. 发明授权

US08034811B2 Hydroxamic acid esters and pharmaceutical use thereof 有权
标题翻译：羟肟酸酯及其药物用途
公开(公告)号：US08034811B2
公开(公告)日：2011-10-11
申请号：US10580967
申请日：2004-12-02
申请人： Jef Fensholdt , Jacob Thorhauge , Bjarne Nørremark
发明人： Jef Fensholdt , Jacob Thorhauge , Bjarne Nørremark
IPC分类号： A61K31/5377 , C07D295/04
CPC分类号： C07D417/12 , C07C259/10 , C07D213/38 , C07D213/53 , C07D213/61 , C07D213/84 , C07D233/22 , C07D261/04 , C07D295/192 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12
摘要： The invention relates to compounds of general formula I wherein D, E, F, G, W, Y, R1, A, R9, X, B, R8 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.
摘要翻译：本发明涉及通式I的化合物，其中D，E，F，G，W，Y，R 1，A，R 9，X，B，R 8如本文所定义，及其药学上可接受的盐，水合物或溶剂合物，单独使用或与一种或多种其它药学活性化合物组合在治疗中，用于治疗与失调的血管生成相关的疾病，例如癌症。

5. 发明申请

US20070244117A1 Novel Hydroxamic Acid Esters and Pharmaceutical Use Thereof 有权
标题翻译：新型羟肟酸酯及其药物用途
公开(公告)号：US20070244117A1
公开(公告)日：2007-10-18
申请号：US10580967
申请日：2004-12-02
申请人： Jef Fensholdt , Jacob Thorhauge , Bjarne Norremark
发明人： Jef Fensholdt , Jacob Thorhauge , Bjarne Norremark
IPC分类号： C07C259/10 , A61K31/165 , C07D213/84 , C07D401/12 , C07D413/06
CPC分类号： C07D417/12 , C07C259/10 , C07D213/38 , C07D213/53 , C07D213/61 , C07D213/84 , C07D233/22 , C07D261/04 , C07D295/192 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12
摘要： The invention relates to compounds of general formula I wherein D, E, F, G, W, Y, R1, A, R9, X, B, R8 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.
摘要翻译：本发明涉及通式I的化合物，其中D，E，F，G，W，Y，R 1，A，R 9，X，B，本文所定义的其它药学上可接受的盐，水合物或溶剂合物，用于治疗与单独使用或与一种或多种其它药学活性化合物组合用于治疗与失调血管发生相关的疾病，如癌症。

6. 发明授权

US06531591B1 Synthesis of stable quinone and photoreactive ketone phosphoramidite reagents for solid phase synthesis of photoreactive-oligomer conjugates 有权
标题翻译：用于固相合成光反应低聚物共轭物的稳定醌和光反应性亚磷酰胺试剂的合成
公开(公告)号：US06531591B1
公开(公告)日：2003-03-11
申请号：US09611833
申请日：2000-07-07
申请人： Jef Fensholdt
发明人： Jef Fensholdt
IPC分类号： C07H2100
CPC分类号： C07H21/00 , C07F9/2408
摘要： Quinone phosphoramidite reagents as well as photoreactive ketone phosphoramidite reagents, such as anthraquinone phosphoramidite reagents and benzophenone phosphoramidite reagents were synthesized and used for the solid phase synthesis of photoreactive-oligonucleotide conjugates. These phosphoramidite reagents are stable, suitable for large-scale synthesis and designed for automated solid phase synthesis of oligomers terminating in a photoreactive moiety.
摘要翻译：喹诺酮亚磷酰胺试剂和光反应性亚磷酰胺试剂如蒽醌亚磷酰胺试剂和二苯甲酮亚磷酰胺试剂合成并用于光活化寡核苷酸共轭物的固相合成。这些亚磷酰胺试剂是稳定的，适用于大规模合成并设计用于自由基固相合成终端于光反应性部分的低聚物。

7. 发明授权

US09487494B2 Cyclic hydrocarbon compounds for the treatment of diseases 有权
标题翻译：用于治疗疾病的环状碳氢化合物
公开(公告)号：US09487494B2
公开(公告)日：2016-11-08
申请号：US12744137
申请日：2008-11-20
申请人： Jef Fensholdt , Sophie Elisabeth Havez , Bjarne Nørremark
发明人： Jef Fensholdt , Sophie Elisabeth Havez , Bjarne Nørremark
IPC分类号： C07D295/182 , C07C211/35 , C07C211/36 , C07C211/48 , C07C215/28 , C07C217/52 , C07C217/74 , C07C233/05 , C07C233/41 , C07C237/24 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/36 , C07C237/40 , C07C239/14 , C07C255/03 , C07C255/32 , C07C255/50 , C07C257/18 , C07C259/10 , C07C259/18 , C07C271/44 , C07C309/15 , C07C311/05 , C07C311/08 , C07C311/37 , C07C311/51 , C07C317/32 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/80 , C07D231/12 , C07D231/40 , C07D233/61 , C07D233/90 , C07D263/22 , C07D271/06 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/192 , C07D295/195 , C07D295/26 , C07D305/08 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/79 , C07D309/10 , C07D319/18 , C07D333/38 , C07D333/40 , C07D333/58 , C07D413/04 , C07D413/06 , C07D417/06
CPC分类号： C07D295/182 , C07C211/35 , C07C211/36 , C07C211/48 , C07C215/28 , C07C217/52 , C07C217/74 , C07C233/05 , C07C233/41 , C07C237/24 , C07C237/30 , C07C237/32 , C07C237/34 , C07C237/36 , C07C237/40 , C07C239/14 , C07C255/03 , C07C255/32 , C07C255/50 , C07C257/18 , C07C259/10 , C07C259/18 , C07C271/44 , C07C309/15 , C07C311/05 , C07C311/08 , C07C311/37 , C07C311/51 , C07C317/32 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D205/04 , C07D207/08 , C07D207/12 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/12 , C07D209/20 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/80 , C07D231/12 , C07D231/40 , C07D233/61 , C07D233/90 , C07D263/22 , C07D271/06 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/192 , C07D295/195 , C07D295/26 , C07D305/08 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/79 , C07D309/10 , C07D319/18 , C07D333/38 , C07D333/40 , C07D333/58 , C07D413/04 , C07D413/06 , C07D417/06
摘要： The invention relates to novel cyclic hydrocarbon compounds and derivatives thereof, processes for the preparation thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
摘要翻译：本发明涉及新的环烃化合物及其衍生物，其制备方法，用作药物的所述化合物，用于治疗的所述化合物，包含所述化合物的药物组合物，涉及用所述化合物治疗疾病的方法，以及所述化合物在制备药物中的用途。

8. 发明申请

US20100279936A1 SUBSTITUTED ACETYLENIC COMPOUNDS USEFUL FOR THE TREATMENT OF DISEASES 审中-公开
标题翻译：替代乙酰化合物可用于治疗疾病
公开(公告)号：US20100279936A1
公开(公告)日：2010-11-04
申请号：US12376417
申请日：2007-08-16
申请人： Xifu Liang , Thomas Høyer , Jef Fensholdt , Sophie Elisabeth Havez , Bjarne Nørremark
发明人： Xifu Liang , Thomas Høyer , Jef Fensholdt , Sophie Elisabeth Havez , Bjarne Nørremark
IPC分类号： A61K38/23
CPC分类号： C07D213/40 , C07B2200/07 , C07C211/29 , C07C211/30 , C07C211/49 , C07C215/24 , C07C215/28 , C07C215/30 , C07C215/50 , C07C215/54 , C07C217/46 , C07C217/58 , C07C217/62 , C07C229/30 , C07C229/34 , C07C229/38 , C07C233/36 , C07C233/38 , C07C233/62 , C07C235/10 , C07C235/60 , C07C237/16 , C07C255/30 , C07C255/58 , C07C271/20 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C311/05 , C07C311/18 , C07C311/29 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07D207/12 , C07D209/08 , C07D211/46 , C07D211/58 , C07D211/62 , C07D231/12 , C07D263/32 , C07D295/13 , C07D295/182 , C07D309/08 , C07D309/10 , C07D317/28 , C07D317/58 , C07D333/20 , C07D333/58 , C07F7/081 , C07F7/1804
摘要： The invention relates to novel compounds according to formula Ia and Ib; (Formula Ia and Ib) wherein A represents substituted or unsubstituted C1-10heteroaryl, C6-14aryl or C6-10heterocycloalkylaryl; R1 is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6hydroxyalkyl, C1-6haloalkyl, C1-6amino, C3-6 cycloalkyl, or C1-6heterocycloalkyl, each of which are optionally substituted; X represents —CR3R4—(CR5R6)n—(CR7═CR8)m—(C6-14aryl)r-(C1-10heteroaryl)s-(CR9R10)p—(CR11═CR12)q, R2 represents C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6hydroxyalkyl, C1-6haloalkyl, C1-6amino, C1-12alkylsilyl, C6-30alkylarylsilyl, C1-10heteroaryl, C6-14aryl, C1-10heterocycloalkyl, C1-10heterocycloalkenyl, C1-8cycloalkyl, C1-18cycloalkenyl, each of which is optionally substituted, or R2 represents hydrogen, carboxy, or hydroxy; or a pharmaceutically acceptable salt, solvate, or ester thereof; to processes for the preparation thereof, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, wherein said compounds being useful, e.g. in the treatment of diseases associated with disturbances of CaSR activity, such as hyperparathyroidism.
摘要翻译：本发明涉及根据式Ia和Ib的新化合物; （式Ia和Ib）其中A表示取代或未取代的C1-10杂芳基，C6-14芳基或C6-10杂环烷基芳基; R 1是C 1-6烷基，C 2-6烯基，C 2-6炔基，C 1-6羟基烷基，C 1-6卤代烷基，C 1-6氨基，C 3-6环烷基或C 1-6杂环烷基，其各自任选被取代; X表示-CR3R4-（CR5R6）n-（CR7 = CR8）m-（C6-14芳基）r-（C1-10杂芳基）s-（CR9R10）p-（CR11 = CR12）q，R2表示C1-6烷基，C2 6-烯基，C 2-6炔基，C 1-6羟基烷基，C 1-6卤代烷基，C 1-6氨基，C 1-12烷基甲硅烷基，C 6-30烷基芳基甲硅烷基，C 1-10杂芳基，C 6-14芳基，C 1-10杂环烷基，C 1-10杂环烯基，C 1-8环烷基，，其各自任选被取代，或R 2表示氢，羧基或羟基; 或其药学上可接受的盐，溶剂化物或酯; 涉及用于制备其的所述化合物，用于治疗的所述化合物，包含所述化合物的药物组合物，其中所述化合物是有用的。治疗与CaSR活动相关的疾病，如甲状旁腺功能亢进。

9. 发明申请

US20100099710A1 SRC FAMILY KINASE INHIBITORS 审中-公开
标题翻译： SRC家族激素抑制剂
公开(公告)号：US20100099710A1
公开(公告)日：2010-04-22
申请号：US12596636
申请日：2008-04-16
申请人： Lene Jensen , Jef Fensholdt
发明人： Lene Jensen , Jef Fensholdt
IPC分类号： A61K31/4545 , C12N5/071 , C07D213/44 , C07D211/72 , C07D211/68 , A61K31/444 , A61K31/44 , A61P31/00
CPC分类号： C07D213/75
摘要： The invention relates to compounds of general formula (I) wherein X, A, R1 and R2 are as defined herein for use as antiinflammatory agents capable of modulating the activity of a protein tyrosine kinase of the Src family.
摘要翻译：本发明涉及通式（I）的化合物，其中X，A，R 1和R 2如本文所定义，用作能够调节Src家族蛋白酪氨酸激酶活性的抗炎剂。

10. 发明申请

US20070167488A1 Novel therapeutic use 审中-公开
标题翻译：新型治疗用途
公开(公告)号：US20070167488A1
公开(公告)日：2007-07-19
申请号：US10582935
申请日：2004-12-16
申请人： Laetitia Bouerat Duvold , Jef Fensholdt , Simon Nielsen , Xifu Liang , Sophie Havez , Ellen Anderson , Lene Jensen , Jens Hansen
发明人： Laetitia Bouerat Duvold , Jef Fensholdt , Simon Nielsen , Xifu Liang , Sophie Havez , Ellen Anderson , Lene Jensen , Jens Hansen
IPC分类号： A61K31/454 , A61K31/4439 , 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。

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