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1. 发明申请

US20110294878A1 Inhibitors of Dimethylarginine Dimethylaminohydrolase 有权
标题翻译：二甲基精氨酸二甲基氨基水解酶抑制剂
公开(公告)号：US20110294878A1
公开(公告)日：2011-12-01
申请号：US13133799
申请日：2009-12-08
申请人： Bernd Clement , Jürke Kotthaus , Dennis Schade
发明人： Bernd Clement , Jürke Kotthaus , Dennis Schade
IPC分类号： A61K31/27 , C07C279/24 , C07C271/20 , A61P35/00 , A61P7/00 , A61P11/06 , A61P25/28 , A61P25/00 , A61P9/10 , C07C335/28 , A61P29/00
CPC分类号： A61K31/155 , A61K31/17 , C07C257/14 , C07C279/12
摘要： The invention relates to an inhibitor of dimethylarginine dimethylaminohydrolase (DDAH) of general structural formula (I), wherein B is a branched or unbranched, substituted or non-substituted, saturated or unsaturated hydrocarbon chain having a chain length of 1 to 6 and/or a substituted or non-substituted aromatic system having a ring size of 3 to 6; R1 is selected from the group of structures (i-vii), wherein R2, R3 and R4 are selected from the group consisting of hydrogen, an alkyl or aryl radical, R5 and R6 are selected from the group consisting of hydrogen, a hydrocarbon chain having a chain length of 1 to 8 and an aryl radical, R7, R8, R9 and R10 are selected from the group consisting of hydrogen, and alkyl or aryl radical; W is oxygen (O) or nitrogen (N); and X is a methylene group (CH2) or a secondary amino group (NH); Y is a branched or unbranched, substituted or non-substituted, saturated or unsaturated hydrocarbon chain having a chain length of 1 to 6 and/or a substituted or non-substituted aromatic system having a ring size of 3 to 6; Z is hydrogen (H) or a methoxyl group; and the radical (B) carrying the amino group has no carboxyl group.
摘要翻译：本发明涉及一般结构式（I）的二甲基精氨酸二甲氨基水解酶（DDAH）抑制剂，其中B是链长为1-6的支链或非支链，取代或未取代的饱和或不饱和烃链和/或具有3至6个环的取代或未取代的芳族体系; R1选自结构式（i-vii），其中R2，R3和R4选自氢，烷基或芳基，R5和R6选自氢，烃链具有1至8个链长和芳基，R 7，R 8，R 9和R 10选自氢和烷基或芳基; W是氧（O）或氮（N）; 并且X是亚甲基（CH 2）或仲氨基（NH）; Y是链长为1至6的支链或非支链，取代或未取代的饱和或不饱和烃链和/或具有3至6个环的取代或未取代的芳族体系; Z是氢（H）或甲氧基; 并且带有氨基的基团（B）没有羧基。

2. 发明授权

US08921421B2 Inhibitors of dimethylarginine dimethylaminohydrolase 有权
标题翻译：二甲基精氨酸二甲氨基水解酶抑制剂
公开(公告)号：US08921421B2
公开(公告)日：2014-12-30
申请号：US13133799
申请日：2009-12-08
申请人： Bernd Clement , Jürke Kotthaus , Dennis Schade
发明人： Bernd Clement , Jürke Kotthaus , Dennis Schade
IPC分类号： A61K31/22 , A01N37/12 , A01N37/44 , A61K31/155 , A61K31/17 , C07C257/14 , C07C279/12
CPC分类号： A61K31/155 , A61K31/17 , C07C257/14 , C07C279/12
摘要： The invention relates to an inhibitor of dimethylarginine dimethylaminohydrolase (DDAH) of general structural formula (I), wherein B is a branched or unbranched, substituted or non-substituted, saturated or unsaturated hydrocarbon chain having a chain length of 1 to 6 and/or a substituted or non-substituted aromatic system having a ring size of 3 to 6; R1 is selected from the group of structures (i-vii), wherein R2, R3 and R4 are selected from the group consisting of hydrogen, an alkyl or aryl radical, R5 and R6 are selected from the group consisting of hydrogen, a hydrocarbon chain having a chain length of 1 to 8 and an aryl radical, R7, R8, R9 and R10 are selected from the group consisting of hydrogen, and alkyl or aryl radical; W is oxygen (O) or nitrogen (N); and X is a methylene group (CH2) or a secondary amino group (NH); Y is a branched or unbranched, substituted or non-substituted, saturated or unsaturated hydrocarbon chain having a chain length of 1 to 6 and/or a substituted or non-substituted aromatic system having a ring size of 3 to 6; Z is hydrogen (H) or a methoxyl group; and the radical (B) carrying the amino group has no carboxyl group.
摘要翻译：本发明涉及一般结构式（I）的二甲基精氨酸二甲氨基水解酶（DDAH）抑制剂，其中B是链长为1-6的支链或非支链，取代或未取代的饱和或不饱和烃链和/或具有3至6个环的取代或未取代的芳族体系; R1选自结构式（i-vii），其中R2，R3和R4选自氢，烷基或芳基，R5和R6选自氢，烃链具有1至8个链长和芳基，R 7，R 8，R 9和R 10选自氢和烷基或芳基; W是氧（O）或氮（N）; 并且X是亚甲基（CH 2）或仲氨基（NH）; Y是链长为1至6的支链或非支链，取代或未取代的饱和或不饱和烃链和/或具有3至6个环的取代或未取代的芳族体系; Z是氢（H）或甲氧基; 并且带有氨基的基团（B）没有羧基。

3. 发明授权

US09387185B2 N-ω-hydroxy-L-arginine derivatives for the treatment of diseases 有权
标题翻译： N-ω-羟基-L-精氨酸衍生物用于治疗疾病
公开(公告)号：US09387185B2
公开(公告)日：2016-07-12
申请号：US13143156
申请日：2010-01-04
申请人： Bernd Clement , Dennis Schade , Jürke Kotthaus
发明人： Bernd Clement , Dennis Schade , Jürke Kotthaus
IPC分类号： C07C279/04 , C07H15/04 , A61K31/155 , A61K31/7028
CPC分类号： A61K31/155 , A61K31/7028 , C07C279/04 , C07H15/04
摘要： The present invention relates to physically-chemically and pharmacokinetically enhanced Nω-hydroxy-L-arginine (NOHA) derivatives and a method for producing the NOHA derivatives having enhanced physical-chemical and pharmacokinetic properties according to the invention.
摘要翻译：本发明涉及物理化学和药代动力学增强的Nω-羟基-L-精氨酸（NOHA）衍生物以及根据本发明具有增强的物理化学和药代动力学性质的NOHA衍生物的制备方法。

4. 发明申请

US20120123111A1 Nª -Hydroxy-L-Arginine Derivatives for the Treatment of Diseases 有权
标题翻译： Nα-羟基-L-精氨酸衍生物治疗疾病
公开(公告)号：US20120123111A1
公开(公告)日：2012-05-17
申请号：US13143156
申请日：2010-01-04
申请人： Bernd Clement , Dennis Schade , Jürke Kotthaus
发明人： Bernd Clement , Dennis Schade , Jürke Kotthaus
IPC分类号： C07C279/24 , C07H15/04
CPC分类号： A61K31/155 , A61K31/7028 , C07C279/04 , C07H15/04
摘要： The present invention relates to physically-chemically and pharmacokinetically enhanced Nω-hydroxy-L-arginine (NOHA) derivatives and a method for producing the NOHA derivatives having enhanced physical-chemical and pharmacokinetic properties according to the invention.
摘要翻译：本发明涉及物理化学和药代动力学增强的Nω-羟基-L-精氨酸（NOHA）衍生物以及根据本发明具有增强的物理化学和药代动力学性质的NOHA衍生物的制备方法。

5. 发明申请

US20120077876A1 Method For Improved Bioactivation Of Pharmaceuticals 审中-公开
标题翻译：改进药物生物活化的方法
公开(公告)号：US20120077876A1
公开(公告)日：2012-03-29
申请号：US13143866
申请日：2010-01-08
申请人： Bernd Clement , Dennis Schade
发明人： Bernd Clement , Dennis Schade
IPC分类号： A61K31/351 , C07C257/18 , C07C279/18 , C07C277/08 , A61K31/196 , A61P33/02 , A61P7/02 , A61P9/00 , A61P25/00 , A61P31/12 , A61P31/16 , A61P31/18 , C07D309/28 , A61P35/00
CPC分类号： C07C279/18 , C07C257/18 , C07D309/28
摘要： This invention relates to a prodrug comprising a partial structure having the general formula (I) or (II), where R1 and R2 are hydrogen, alkyl, or aryl radicals.
摘要翻译：本发明涉及包含具有通式（I）或（II）的部分结构的前药，其中R 1和R 2是氢，烷基或芳基。

6. 发明授权

US08853245B2 Orally bioavailable dabigatran prodrugs for the treatment of diseases 有权
标题翻译：口服生物可利用达比加群前体药物治疗疾病
公开(公告)号：US08853245B2
公开(公告)日：2014-10-07
申请号：US13556612
申请日：2012-07-24
申请人： Bernd Clement , Joscha Kotthaus , Juerke Kotthaus , Dennis Schade
发明人： Bernd Clement , Joscha Kotthaus , Juerke Kotthaus , Dennis Schade
IPC分类号： C07D401/12 , A61K31/4439 , A61K9/10 , A61K9/00 , A61K45/06
CPC分类号： C07D401/12 , A61K9/0019 , A61K9/0095 , A61K9/10 , A61K45/06
摘要： The present invention relates to prodrug derivatives of dabigatran, their use in the treatment and/or prophylaxis of diseases, in particular thrombotic diseases, stroke, cardiac infarction and/or atrial fibrillation and cardiac arrhythmia, as well as oncological diseases of any pathogenesis.
摘要翻译：本发明涉及达比加群的前药衍生物，其用于治疗和/或预防疾病，特别是血栓性疾病，中风，心肌梗塞和/或心房颤动和心律失常以及任何发病机理的肿瘤疾病。

7. 发明授权

US09403800B2 Compounds for inhibition of cancer cell proliferation 有权
标题翻译：用于抑制癌细胞增殖的化合物
公开(公告)号：US09403800B2
公开(公告)日：2016-08-02
申请号：US13748770
申请日：2013-01-24
申请人： John Cashman , Mark Mercola , Dennis Schade , Masanao Tsuda
发明人： John Cashman , Mark Mercola , Dennis Schade , Masanao Tsuda
IPC分类号： C07D403/12 , C07D487/00 , A61K31/635 , C07D401/12 , C07D413/12 , C07H17/02 , A61K45/06 , A61K31/706 , A61K31/4745 , A61K31/513 , A61K31/555
CPC分类号： C07D403/12 , A61K31/4745 , A61K31/513 , A61K31/555 , A61K31/635 , A61K31/706 , A61K45/06 , C07D401/12 , C07D413/12 , C07D487/00 , C07H17/02 , A61K2300/00
摘要： Methods and small molecule compounds for inhibition of cancer cell proliferation are provided. One example of a class of compounds that may be used is represented by the compound of Formula I or a pharmaceutically acceptable salt, N-oxide or solvate thereof, wherein A, B, D, E, F, G, I, J, R, R1, R2, R2′, R3, R4, R5, R6, R7, R8, R9 are as described herein.
摘要翻译：提供了抑制癌细胞增殖的方法和小分子化合物。可以使用的一类化合物的一个实例由式I化合物或其药学上可接受的盐，N-氧化物或溶剂化物表示，其中A，B，D，E，F，G，I，J，R ，R1，R2，R2'，R3，R4，R5，R6，R7，R8，R9如本文所述。

8. 发明申请

US20130157947A1 COMPOUNDS FOR STEM CELL DIFFERENTIATION 有权
标题翻译：用于干细胞分化的化合物
公开(公告)号：US20130157947A1
公开(公告)日：2013-06-20
申请号：US13428647
申请日：2012-03-23
申请人： MARK MERCOLA , John Cashman , Marion Lanier , Erik Willems , Dennis Schade
发明人： MARK MERCOLA , John Cashman , Marion Lanier , Erik Willems , Dennis Schade
IPC分类号： C07D215/54 , C12N5/071 , A61K31/4709 , C07D401/10 , A61K31/475 , A61K31/47 , A61K38/18 , C12N5/079
CPC分类号： C07D215/54 , A61K31/47 , A61K31/4709 , A61K31/475 , A61K38/1841 , A61K38/1875 , C07D215/20 , C07D401/10 , C07D401/12 , C12N5/0618 , C12N5/0652 , C12N5/0655 , C12N5/0657 , C12N5/067 , C12N5/0676
摘要： Small molecule compounds and methods for stem cell differentiation are provided herein. An example of a class of compounds that may be used to practice the methods disclosed herein is represented by enantiomerically pure isomers of compounds of Formula I: or a chirally pure stereoisomer, pharmaceutically acceptable salt, or solvate thereof, wherein R1, R2, R3, R4, R5, R5′, R6, R6′, R7, R7′ are as described herein.
摘要翻译：本文提供了小分子化合物和干细胞分化方法。可用于实施本文公开的方法的一类化合物的实例由式I化合物的对映体纯的异构体或其手性纯的立体异构体，药学上可接受的盐或溶剂合物表示，其中R1，R2，R3， R4，R5，R5'，R6，R6'，R7，R7'如本文所述。

9. 发明授权

US09233926B2 Compounds for stem cell differentiation 有权
标题翻译：用于干细胞分化的化合物
公开(公告)号：US09233926B2
公开(公告)日：2016-01-12
申请号：US13428647
申请日：2012-03-23
申请人： Mark Mercola , John Cashman , Marion Lanier , Erik Willems , Dennis Schade
发明人： Mark Mercola , John Cashman , Marion Lanier , Erik Willems , Dennis Schade
IPC分类号： C07D215/38 , A61K31/47 , C07D215/54
CPC分类号： C07D215/54 , A61K31/47 , A61K31/4709 , A61K31/475 , A61K38/1841 , A61K38/1875 , C07D215/20 , C07D401/10 , C07D401/12 , C12N5/0618 , C12N5/0652 , C12N5/0655 , C12N5/0657 , C12N5/067 , C12N5/0676
摘要： Small molecule compounds and methods for stem cell differentiation are provided herein. An example of a class of compounds that may be used to practice the methods disclosed herein is represented by enantiomerically pure isomers of compounds of Formula I: or a chirally pure stereoisomer, pharmaceutically acceptable salt, or solvate thereof, wherein R1, R2, R3, R4, R5, R5′, R6, R6′, R7, R7′ are as described herein.
摘要翻译：本文提供了小分子化合物和干细胞分化方法。可用于实施本文公开的方法的一类化合物的实例由式I化合物的对映体纯的异构体或其手性纯的立体异构体，药学上可接受的盐或溶剂合物表示，其中R1，R2，R3， R4，R5，R5'，R6，R6'，R7，R7'如本文所述。

10. 发明授权

US09023340B2 Wnt inhibitors for human stem cell differentiation 有权
标题翻译： Wnt抑制剂用于人类干细胞分化
公开(公告)号：US09023340B2
公开(公告)日：2015-05-05
申请号：US13540590
申请日：2012-07-02
申请人： John Cashman , Marion Lanier , Mark Mercola , Dennis Schade , Erik Willems
发明人： John Cashman , Marion Lanier , Mark Mercola , Dennis Schade , Erik Willems
IPC分类号： A01N63/00 , C07D401/12 , C07D209/76 , C12N5/077 , A61K35/34
CPC分类号： C07D401/12 , A61K35/34 , C07D209/76 , C12N5/0657 , C12N2501/415 , C12N2503/02 , C12N2506/02
摘要： Methods and small molecule compounds for stem cell differentiation and treatment of animals with diseases are provided. One example of a class of compounds that may be used is represented by the compound of Formula I and II: or a pharmaceutically acceptable salt or solvate thereof, wherein A, X, Q, R1, R2, R3, R4 are as described herein.
摘要翻译：提供了用于具有疾病的动物的干细胞分化和治疗的方法和小分子化合物。可以使用的一类化合物的一个实例由式I和II的化合物或其药学上可接受的盐或溶剂合物表示，其中A，X，Q，R 1，R 2，R 3，R 4如本文所述。

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