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1. 发明授权

US08466309B2 Amino acid derivatives, method for preparing same, and therapeutic use thereof 有权
标题翻译：氨基酸衍生物，其制备方法及其治疗用途
公开(公告)号：US08466309B2
公开(公告)日：2013-06-18
申请号：US12991999
申请日：2009-05-13
申请人： Marie-Claude Fournie-Zaluski , Hervé Poras , Bernard Roques
发明人： Marie-Claude Fournie-Zaluski , Hervé Poras , Bernard Roques
IPC分类号： C07C69/74 , C07C321/00 , C07C323/00 , C07C381/00 , A01N43/16
CPC分类号： C07C323/65 , C07C323/60
摘要： The disclosure relates to novel compounds of the formula (I) R1NH—CH(R2)CH2—S—S—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7, in which R1 is a (acyloxy)alkyl carbamate-C(O)—O—C(R8)(R9)—OC(O)—R10 group; R2 is a hydrocarbon chain, a methylene radical substituted by a heterocycle, R4 is a hydrogen atom and R3 is a phenyl or benzyl radical, a heteroaryl, a methylene group substituted by a heterocycle or R3 and R4 form together a saturated cycle; R5 and R6 are hydrogen, a hydrocarbon chain, a phenyl or benzyl radical or R5 and R6 form together a saturated cycle; R7 is hydrogen, a phenyl or benzyl radical, a group of the formula CR12(R13)C(O)OR14 or OCR12(R13)OC(O)R14 or OCR12(R13)OC(O)OR14. The disclosure also relates to the use of these compounds as a drug, and to a pharmaceutical composition containing said compounds and a pharmaceutically acceptable carrier. The disclosure further relates to the combined use of at least one cannabinoid derivative and/or morphine or one derivative thereof and/or Gaba derivatives for enhancing the analgesic and anti-depressive effect of the compounds of the formula (I).
摘要翻译：本发明涉及式（I）的新化合物：R1NH-CH（R2）CH2-SS-CH2-C（R3）（R4）-CONH-C（R5）（R6）-COOR7，其中R1是（酰氧基）烷基氨基甲酸酯-C（O）-OC（R 8）（R 9）-OC（O）-R 10基团; R2是烃链，被杂环取代的亚甲基，R4是氢原子，R3是苯基或苄基，杂芳基，被杂环取代的亚甲基或R3和R4一起形成饱和环; R5和R6是氢，烃链，苯基或苄基或R5和R6一起形成饱和循环; R 7是氢，苯基或苄基，式CR 12（R 13）C（O）OR 14或OCR 12（R 13）OC（O）R 14或OCR 12（R 13）OC（O）OR 14的基团。本公开还涉及这些化合物作为药物的用途，以及含有所述化合物和药学上可接受的载体的药物组合物。本公开还涉及至少一种大麻素衍生物和/或吗啡或其一种衍生物和/或Gaba衍生物用于增强式（I）化合物的止痛和抗抑郁作用的组合使用。

2. 发明授权

US08703747B2 Aminophosphinic derivatives that can be used in the treatment of pain 有权
标题翻译：可用于治疗疼痛的氨基亚磷酸衍生物
公开(公告)号：US08703747B2
公开(公告)日：2014-04-22
申请号：US13055096
申请日：2009-07-22
申请人： Bernard Roques , Hervé Poras , Marie-Claude Fournie-Zaluski
发明人： Bernard Roques , Hervé Poras , Marie-Claude Fournie-Zaluski
IPC分类号： A61K31/66 , A01N57/00 , A01N57/18
CPC分类号： C07F9/306 , A61K31/662 , A61K31/67 , A61K31/675 , A61K39/08 , A61K45/06 , C07F9/301 , C07F9/303 , C07F9/3211 , C07F9/3241 , C07F9/4816 , C07F9/59 , C07F9/655345
摘要： The present invention relates to a compound of the following general formula (I): R1—NH—CH(R2)—P(═O)(OR3)—CH2—C(R4)(R5)—CONH—CH(R6)—COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a —C(═O)—O—C(R8)(R9)—OC(═O)—R10 group; R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R3 represents a hydrogen atom or a —C(R12)(R13)—OC(═O)—R14 group; R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted; and R7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, —CHMe—COOR18, —CHR19—OC(═O)OR20 and —CHR19—OC(═O)OR20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more advantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.
摘要翻译：本发明涉及以下通式（I）的化合物：R1-NH-CH（R2）-P（= O）（OR3）-CH2-C（R4）（R5）-CONH-CH（R6） -COOR7（I）或其后者的药学上可接受的盐，任何比例的异构体或异构体混合物，特别是对映异构体的混合物，特别是外消旋混合物，其中R1表示-C（= O） - O-C（R 8）（R 9）-OC（= O）-R 10基; R2表示任选取代的烃基链，芳基或杂芳基或被杂环取代的亚甲基; R3表示氢原子或-C（R12）（R13）-OC（= O）-R14基团; R4和R5与带有它们的碳一起形成饱和烃基环或任选取代的哌啶环，或R4表示氢原子，R 5表示任选取代的苯基或苄基，杂芳环或亚甲基被杂环取代的基团; R6表示任选取代的烃基链或任选取代的苯基或苄基; 并且R 7表示氢原子或苄基，烷基，杂芳基，烷基杂芳基，-CHMe-COOR 18，-CHR 19 -OC（= O）OR 20和-CHR 19 -OC（= O）OR 20基团。本发明还涉及这些化合物作为药用产品的用途，特别是用于治疗其合成方法的疼痛，更有利的是神经性和神经炎性疼痛，以及含有它们的组合物。

3. 发明申请

US20110124601A1 AMINOPHOSPHINIC DERIVATIVES THAT CAN BE USED IN THE TREATMENT OF PAIN 有权
标题翻译：可用于治疗疼痛的氨基磷酸衍生物
公开(公告)号：US20110124601A1
公开(公告)日：2011-05-26
申请号：US13055096
申请日：2009-07-22
申请人： Bernard Roques , Hervé Poras , Marie-Claude Fournie-Zaluski
发明人： Bernard Roques , Hervé Poras , Marie-Claude Fournie-Zaluski
IPC分类号： A61K31/662 , C07F9/30 , C07F9/32 , C07F9/6553 , A61K31/67 , C07F9/59 , A61K31/675 , A61P29/00 , A61P25/04
CPC分类号： C07F9/306 , A61K31/662 , A61K31/67 , A61K31/675 , A61K39/08 , A61K45/06 , C07F9/301 , C07F9/303 , C07F9/3211 , C07F9/3241 , C07F9/4816 , C07F9/59 , C07F9/655345
摘要： The present invention relates to a compound of the following general formula (I): R1—NH—CH(R2)—P(═O)(OR3)—CH2—C(R4)(R5)—CONH—CH(R6)—COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a —C(═O)—O—C(R8)(R9)—OC(═O)—R10 group; R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R3 represents a hydrogen atom or a —C(R12)(R13)—OC(═O)—R14 group; R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted; and R7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, —CHMe—COOR18, —CHR19—OC(═O)OR20 and —CHR19—OC(═O)OR20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more advantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.
摘要翻译：本发明涉及以下通式（I）的化合物：R1-NH-CH（R2）-P（= O）（OR3）-CH2-C（R4）（R5）-CONH-CH（R6） -COOR7（I）或其后者的药学上可接受的盐，任何比例的异构体或异构体混合物，特别是对映异构体的混合物，特别是外消旋混合物，其中R1表示-C（= O） - O-C（R 8）（R 9）-OC（= O）-R 10基; R2表示任选取代的烃基链，芳基或杂芳基或被杂环取代的亚甲基; R3表示氢原子或-C（R12）（R13）-OC（= O）-R14基团; R4和R5与带有它们的碳一起形成饱和烃基环或任选取代的哌啶环，或R4表示氢原子，R 5表示任选取代的苯基或苄基，杂芳环或亚甲基被杂环取代的基团; R6表示任选取代的烃基链或任选取代的苯基或苄基; 并且R 7表示氢原子或苄基，烷基，杂芳基，烷基杂芳基，-CHMe-COOR 18，-CHR 19 -OC（= O）OR 20和-CHR 19 -OC（= O）OR 20基团。本发明还涉及这些化合物作为药用产品的用途，特别是用于治疗其合成方法的疼痛，更有利的是神经性和神经炎性疼痛，以及含有它们的组合物。

4. 发明申请

US20110071218A1 NOVEL AMINO ACID DERIVATIVES, METHOD FOR PREPARING SAME, AND THERAPEUTIC USE THEREOF 有权
标题翻译：新型氨基酸衍生物，其制备方法及其治疗用途
公开(公告)号：US20110071218A1
公开(公告)日：2011-03-24
申请号：US12991999
申请日：2009-05-13
申请人： Marie-Claude Fournie-Zaluski , Hervé Poras , Bernard Roques
发明人： Marie-Claude Fournie-Zaluski , Hervé Poras , Bernard Roques
IPC分类号： A61K31/352 , A61K31/215 , A61K31/225 , A61K31/22 , C07C69/74 , C07C381/00 , A61P25/00 , A61P25/24
CPC分类号： C07C323/65 , C07C323/60
摘要： The disclosure relates to novel compounds of the formula (I) R1NH—CH(R2)CH2—S—S—CH2—C(R3)(R4)—CONH—C(R5)(R6)—COOR7, in which R1 is a (acyloxy)alkyl carbamate-C(O)—O—C(R8)(R9)—OC(O)—R10 group; R2 is a hydrocarbon chain, a methylene radical substituted by a heterocycle, R4 is a hydrogen atom and R3 is a phenyl or benzyl radical, a heteroaryl, a methylene group substituted by a heterocycle or R3 and R4 form together a saturated cycle; R5 and R6 are hydrogen, a hydrocarbon chain, a phenyl or benzyl radical or R5 and R6 form together a saturated cycle; R7 is hydrogen, a phenyl or benzyl radical, a group of the formula CR12(R13)C(O)OR14 or OCR12(R13)OC(O)R14 or OCR12(R13)OC(O)OR14. The disclosure also relates to the use of these compounds as a drug, and to a pharmaceutical composition containing said compounds and a pharmaceutically acceptable carrier. The disclosure further relates to the combined use of at least one cannabinoid derivative and/or morphine or one derivative thereof and/or Gaba derivatives for enhancing the analgesic and anti-depressive effect of the compounds of the formula (I).
摘要翻译：本发明涉及式（I）R1NH-CH（R2）CH2-S-S-CH2-C（R3）（R4）-CONH-C（R5）（R6）-COOR7的新型化合物，其中R1为（O）-O-C（R 8）（R 9）-OC（O）-R 10基团的（酰氧基）烷基氨基甲酸酯-C（O） R2是烃链，被杂环取代的亚甲基，R4是氢原子，R3是苯基或苄基，杂芳基，被杂环取代的亚甲基或R3和R4一起形成饱和环; R5和R6是氢，烃链，苯基或苄基或R5和R6一起形成饱和循环; R 7是氢，苯基或苄基，式CR 12（R 13）C（O）OR 14或OCR 12（R 13）OC（O）R 14或OCR 12（R 13）OC（O）OR 14的基团。本公开还涉及这些化合物作为药物的用途，以及含有所述化合物和药学上可接受的载体的药物组合物。本公开还涉及至少一种大麻素衍生物和/或吗啡或其一种衍生物和/或Gaba衍生物用于增强式（I）化合物的止痛和抗抑郁作用的组合使用。

5. 发明申请

US20130243691A1 AGENTS FOR THE MOLECULAR IMAGING OF SERINE-PROTEASE IN HUMAN PATHOLOGIES 有权
标题翻译：人类病理学中丝氨酸蛋白酶分子成像的试剂
公开(公告)号：US20130243691A1
公开(公告)日：2013-09-19
申请号：US13990845
申请日：2011-12-05
申请人： Jean-Baptiste Michel , François Rouzet , Dominique Leguludec , Hervé Poras , Marie-Claude Fournie-Zaluski , Bernard Roques
发明人： Jean-Baptiste Michel , François Rouzet , Dominique Leguludec , Hervé Poras , Marie-Claude Fournie-Zaluski , Bernard Roques
IPC分类号： A61K49/00
CPC分类号： A61K51/088 , A61K49/0004 , A61K49/14 , A61K51/048 , A61K51/0482 , A61K51/08 , C07K5/1024
摘要： The present invention is directed to the use of an irreversible ligand of a serine protease selected from the group consisting of leukocyte elastase, thrombin, tissue plasminogen activator (t-PA) and plasmin for the molecular imaging of said serine protease and the diagnosis of pathophysiological conditions associated with said serine protease activity.
摘要翻译：本发明涉及使用选自白细胞弹性蛋白酶，凝血酶，组织纤溶酶原激活剂（t-PA）和纤溶酶的丝氨酸蛋白酶的不可逆配体用于所述丝氨酸蛋白酶的分子成像和诊断病理生理学与所述丝氨酸蛋白酶活性相关的条件。

6. 发明授权

US06716852B2 Amino acid derivatives and use thereof as NEP, ACE and ECE inhibitors 失效
标题翻译：氨基酸衍生物及其作为NEP，ACE和ECE抑制剂的用途
公开(公告)号：US06716852B2
公开(公告)日：2004-04-06
申请号：US10203704
申请日：2002-08-12
申请人： Bernard P. Roques , Marie-Claude Fournie-Zaluski , Nicolas Inguimbert , Hervé Poras , Elizabeth Scalbert , Caroline Bennejean , Pierre Renard
发明人： Bernard P. Roques , Marie-Claude Fournie-Zaluski , Nicolas Inguimbert , Hervé Poras , Elizabeth Scalbert , Caroline Bennejean , Pierre Renard
IPC分类号： A61K31435
CPC分类号： C07D471/04 , C07D209/20 , C07D215/14 , C07D219/02 , C07D333/60
摘要： The invention relates to compounds of formula (I): wherein 0≦n≦3, 0≦m≦6, R3 and R4 together form phenyl, B represents heteroaryl, R1 and R2 represent hydrogen or groups as defined in the description. and medicinal products containing the same which are useful in treating or preventing arterial hypertension and cardiovascular diseases.
摘要翻译：本发明涉及式（I）化合物：其中0≤N＆LE; 3,0 <= M＆LE; 6，R 3和R 4一起形成苯基，B表示杂芳基，R 1和R 2 >表示说明书中定义的氢或基团，以及含有该基团的药物，其可用于治疗或预防动脉高血压和心血管疾病。

7. 发明授权

US09272054B2 Agents for the molecular imaging of serine-protease in human pathologies 有权
标题翻译：人类病理学中丝氨酸蛋白酶分子成像剂
公开(公告)号：US09272054B2
公开(公告)日：2016-03-01
申请号：US13990845
申请日：2011-12-05
申请人： Jean-Baptiste Michel , François Rouzet , Dominique Leguludec , Hervé Poras , Marie-Claude Fournie-Zaluski , Bernard Rogues
发明人： Jean-Baptiste Michel , François Rouzet , Dominique Leguludec , Hervé Poras , Marie-Claude Fournie-Zaluski , Bernard Rogues
IPC分类号： A61K51/00 , A61M36/14 , A61K49/00 , A61K49/14 , A61K51/08
CPC分类号： A61K51/088 , A61K49/0004 , A61K49/14 , A61K51/048 , A61K51/0482 , A61K51/08 , C07K5/1024
摘要： The present invention is directed to the use of an irreversible ligand of a serine protease selected from the group consisting of leukocyte elastase, thrombin, tissue plasminogen activator (t-PA) and plasmin for the molecular imaging of said serine protease and the diagnosis of pathophysiological conditions associated with said serine protease activity.
摘要翻译：本发明涉及使用选自白细胞弹性蛋白酶，凝血酶，组织纤溶酶原激活剂（t-PA）和纤溶酶的丝氨酸蛋白酶的不可逆配体用于所述丝氨酸蛋白酶的分子成像和诊断病理生理学与所述丝氨酸蛋白酶活性相关的条件。

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