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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。
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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。
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3.
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。
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4.
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。
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5.
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。
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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。
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公开(公告)号:US08658826B2
公开(公告)日:2014-02-25
申请号:US12847544
申请日:2010-07-30
IPC分类号: C07C257/00
CPC分类号: C07C251/64 , A61K31/155 , A61K31/401 , C07C249/12 , Y02A50/409
摘要: The invention relates to a method for improving bioavailability of pharmaceutical substances and for allowing the pharmaceutical substances to permeate the blood-brain barrier, the pharmaceutical substances having at least one or more amidine, guanidine, N-hydroxyamidine (amidoxime) or N-hydroxyguanidine functions. The invention also relates to medicaments containing the correspondingly modified pharmaceutical substances.
摘要翻译: 本发明涉及一种提高药物物质生物利用度和允许药物渗透血脑屏障的方法,具有至少一种或多种脒,胍,N-羟基脒(偕胺肟)或N-羟基胍功能的药物物质 。 本发明还涉及含有相应修饰的药物的药物。
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8.
公开(公告)号:US07807681B2
公开(公告)日:2010-10-05
申请号:US12105975
申请日:2008-04-18
IPC分类号: A61K31/4965
CPC分类号: C07D295/185 , C07K5/06078 , C07K5/06191
摘要: The present invention relates to novel compounds for inhibiting the urokinase plasminogen activator (uPA), which have high bioavailability and oral administerability, and also to the use thereof as therapeutic active compounds for the treatment of urokinase- or/and urokinase receptor-associated disorders such as, for example, tumors and metastasizing. The invention relates in particular to compounds containing hydroxyamidine or hydroxyguanidine groups.
摘要翻译: 本发明涉及用于抑制尿激酶纤溶酶原激活物(uPA)的新化合物,其具有高的生物利用度和口服施用性,并且还涉及作为用于治疗尿激酶或/和尿激酶受体相关疾病的治疗活性化合物的用途, 例如,肿瘤和转移。 本发明特别涉及含有羟基脒或羟基胍基团的化合物。
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9.
公开(公告)号:US20080261998A1
公开(公告)日:2008-10-23
申请号:US12105975
申请日:2008-04-18
IPC分类号: A61K31/495 , A61P35/00 , A61P35/04
CPC分类号: C07D295/185 , C07K5/06078 , C07K5/06191
摘要: The present invention relates to novel compounds for inhibiting the urokinase plasminogen activator (uPA), which have high bioavailability and oral administerability, and also to the use thereof as therapeutic active compounds for the treatment of urokinase- or/and urokinase receptor-associated disorders such as, for example, tumors and metastasizing. The invention relates in particular to compounds containing hydroxyamidine or hydroxyguanidine groups.
摘要翻译: 本发明涉及用于抑制尿激酶纤溶酶原激活物(uPA)的新化合物,其具有高的生物利用度和口服施用性,并且还涉及作为用于治疗尿激酶或/和尿激酶受体相关疾病的治疗活性化合物的用途, 例如,肿瘤和转移。 本发明特别涉及含有羟基脒或羟基胍基团的化合物。
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公开(公告)号:US20140323763A1
公开(公告)日:2014-10-30
申请号:US13995261
申请日:2011-12-21
申请人: Franz Furkert , Bernd Clement , Britta Gerig , Dieter Heber
发明人: Franz Furkert , Bernd Clement , Britta Gerig , Dieter Heber
IPC分类号: C07C225/16 , C07C211/63 , C07C211/29
CPC分类号: A61K31/14 , A61K31/135 , A61K33/22 , C07C211/29 , C07C211/63 , C07C225/16
摘要: The invention relates to the use of a substance of the general form (I) to produce an antibacterial and/or antifungal drug, wherein X is a methylene group or a carbonyl group; R1, R2, and R3 are each selected from the group comprising hydrogen, an alkyl group having a chain length of 1-4 carbon atoms, an alkoxy group having a chain length of 1-3 carbon atoms, and a halogen; R4 and R5 are each selected from the group comprising hydrogen and an alkyl group having a chain length of 1-4 carbon atoms; and n=3 to 6.
摘要翻译: 本发明涉及一般形式(I)物质生产抗菌和/或抗真菌药物的用途,其中X为亚甲基或羰基; R1,R2和R3各自选自氢,链长为1-4个碳原子的烷基,链长为1-3个碳原子的烷氧基和卤素; R4和R5各自选自氢和链长为1-4个碳原子的烷基; n = 3〜6。
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