公开(公告)号：US20050192228A1

公开(公告)日：2005-09-01

申请号：US10635696

申请日：2003-08-05

申请人： Jean Rapin ,  Hans Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

发明人： Jean Rapin ,  Hans Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

IPC分类号： A61K38/05 ,  A61K38/06 ,  C07K7/06

CPC分类号： A61K38/06

摘要： The invention relates to the use of specific tripeptides for the treatment of neurodegenerative diseases. The tripeptide derivatives satisfy the following formula (I): wherein X represents OH, (C1-5)alkoxy, NH2, NH—C1-5-alkyl, N(C1-5alkyl)2; R1 is a residue derived from any of the amino acids Phe, Tyr, Trp, Pro, each of which may optionally be substituted by a (C1-5)alkoxy group, a (C1-5)alkyl group or a halogen atom, and Ala, Val, Leu, or Ile; R2 is a residue which is derived from any of the amino acids Gly, Ala, Ile, Val, Ser, Thr, His, Arg, Lys, Pro, Glu, Gln, pGlu, Asp, Leu and Asn; R3 and R4 independently represent H, OH, (C1-5)alkyl, or (C1-5)alkoxy, provided that R3 and R4 are not both OH or (C1-5)alkoxy; R5 represents H, OH, (C1-5)alkyl or (C1-5)alkoxy; and wherein R0 preferably represents a cinnamoyl residue; or pharmaceutically acceptable salts thereof.

摘要翻译： 本发明涉及特异性三肽用于治疗神经变性疾病的用途。 三肽衍生物满足下式（I）：其中X表示OH，（C 1-5 - ）烷氧基，NH 2，NH-C 1-5 N（C 1-5烷基）亚烷基，N（C 1-5烷基） R 1是来自任何氨基酸Phe，Tyr，Trp，Pro的残基，其各自可任选地被（C 1-5 - ）烷氧基 （C 1-5）烷基或卤素原子，Ala，Val，Leu或Ile; R 2是衍生自任何氨基酸Gly，Ala，Ile，Val，Ser，Thr，His，Arg，Lys，Pro，Glu，Gln，pGlu，Asp，Leu的残基 和Asn; R 3和R 4独立地表示H，OH，（C 1-5 - ）烷基，或（C 1-5） 其中R 3和R 4不都是OH或（C 1-5 - ）烷氧基， R 5表示H，OH，（C 1-5 - ）烷基或（C 1-5 - ）烷氧基; 并且其中R 0优选表示肉桂酰残基; 或其药学上可接受的盐。

公开(公告)号：US5849725A

公开(公告)日：1998-12-15

申请号：US505139

申请日：1995-07-21

申请人： Jacques Gonella ,  Alberto Reiner

发明人： Jacques Gonella ,  Alberto Reiner

IPC分类号： C07F9/09 ,  C07F9/572 ,  C07F9/12 ,  A61K31/66

CPC分类号： C07F9/5728 ,  C07F9/091

摘要： The principal activity of the amides of ethanol-.beta.-aminophosphoric acid with active moieties having anti-inflammatory and analgesic activity (FANS) remains substantially unchanged but they have considerably lower toxicity particularly in terms of damage to the stomach. The method for their preparation is also described.

摘要翻译： 具有抗炎和止痛活性的活性部分（FANS）的乙醇-β-氨基磷酸的酰胺的主要活性基本上保持不变，但是它们具有显着降低的毒性，特别是在对胃的损害方面。 还描述了其制备方法。

公开(公告)号：US20050080016A1

公开(公告)日：2005-04-14

申请号：US10635805

申请日：2003-08-05

申请人： Jean Rapin ,  Hans Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

发明人： Jean Rapin ,  Hans Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

IPC分类号： A61K38/00 ,  A61K38/06 ,  A61P9/10 ,  A61P17/02 ,  A61P25/00 ,  C07K5/08 ,  C07K5/083 ,  C07K5/087 ,  C07K5/097 ,  A61K38/08

CPC分类号： A61K38/06

摘要： The invention relates to the use of specific tripeptides for the treatment of postlesional diseases of ischemic, traumatic or toxic origin. The tripeptide derivatives satisfy the following formula (I): (see formula I as in paper form) wherein X represents OH, (C1-5) alkoxy, NH2, NH—C1-5-alkyl, N(C1-5 alkyl)2; R1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one or more (C1-5) alkoxy groups, (C1-5) alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, and Pro; Y1 and Y2 independently from each other represent H or (C1-5) alkyl; R3 and R4 independently from each other represent H, OH, (C1-5) alkyl or (C1-5) alkoxy, provided that R3 and R4 are not both OH or (C1-5) alkoxy; and R5 represents H, OH, (C1-5) alkyl or (C1-5) alkoxy; or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及特异性三肽用于治疗缺血性，创伤性或毒性起源性的postsional疾病的用途。 三肽衍生物满足下式（I）：（参见式I），其中X表示OH，（C 1-5）烷氧基，NH 2，NH-C 1-5 - 烷基，N（C 1-5烷基）2 ; R1是衍生自氨基酸Phe，Tyr，Trp，Pro之一的残基，其各自可以任选地被一个或多个（C 1-5）烷氧基，（C 1-5）烷基或卤素原子取代 如Ala，Val，Leu或Ile; R2是衍生自氨基酸Gly，Ala，Ile，Val，Ser，Thr和Pro之一的残基; Y 1和Y 2彼此独立地表示H或（C 1-5）烷基; R 3和R 4彼此独立地表示H，OH，（C 1-5）烷基或（C 1-5）烷氧基，条件是R 3和R 4不同时为OH或（C 1-5）烷氧基; 并且R 5表示H，OH，（C 1-5）烷基或（C 1-5）烷氧基; 或其药学上可接受的盐。

公开(公告)号：US4411909A

公开(公告)日：1983-10-25

申请号：US358370

申请日：1982-03-15

申请人： Jacques Gonella

发明人： Jacques Gonella

IPC分类号： A61K31/38 ,  A61K31/381 ,  A61P11/00 ,  A61P11/10 ,  A61P27/16 ,  C07D333/36

CPC分类号： C07D333/36

摘要： The present invention relates to [(2-oxo-3-tetrahydrothienylcarbamoyl)-alkylthio]-acetic acids, their salts and esters of formula: ##STR1## in which n is 0 or 1, one of the substituents R.sub.1 and R.sub.2 is a hydrogen atom or a methyl group and the other represents a group -S-CH.sub.2 -COOR.sub.3, where R.sub.3 is a hydrogen atom or an alkali metal or a lower alkyl group or a group: ##STR2## It also relates to a process for preparing said acids, salts and esters, and to the drugs containing same.

摘要翻译： 本发明涉及[（2-氧代-3-四氢噻吩基氨基甲酰基） - 烷硫基] - 乙酸，其盐和酯，其中n为0或1，其中一个取代基R 1和R 2为氢 原子或甲基，另一个表示基团-S-CH 2 -COOR 3，其中R 3是氢原子或碱金属或低级烷基或基团：其还涉及制备所述酸的方法 ，盐和酯，以及含有它们的药物。

公开(公告)号：US07163922B2

公开(公告)日：2007-01-16

申请号：US10635808

申请日：2003-08-05

申请人： Jean Rapin ,  Hans Klaus Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

发明人： Jean Rapin ,  Hans Klaus Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

IPC分类号： A61K38/00

CPC分类号： A61K38/06

摘要： The invention relates to the use of specific tripeptides for the treatment of postlesional diseases of ischemic, traumatic or toxic origin. The tripeptide derivatives satisfy formula (I), wherein X represents OH, (C1-5)alkoxy, NH2, NH—C1-5-alkyl, N(C1-5 alkyl)2; R1 is a residue derived from any of the amino acids Phe, Tyr, Trp, Pro, each of which may optionally be substituted by a (C1-5) alkoxy group, a (C1-5) alkyl group or a halogen atom, and Ala, Val, Leu, or Ile; R2 is a residue which is derived from any of the amino acids Gly, Ala, Ile, Val, Ser, Thr, His, Arg, Lys, Pro, Glu, Gln, pGlu, Asp, Leu and Asn; R3 and R4 independently represent H, OH, (C1 –C5) alkyl, or (C1-5)alkoxy, provided that R3 and R4 are not both OH or (C1-5)alkoxy; R5 represents H, OH, (C1-5)alkyl or (C1-5)alkoxy; and wherein R0 preferably represents a cinnamoyl residue; or pharmaceutically acceptable salts thereof.

摘要翻译： 本发明涉及特异性三肽用于治疗缺血性，创伤性或毒性起源性的postsional疾病的用途。 三肽衍生物满足式（I），其中X表示OH，（C 1-5 - ）烷氧基，NH 2，NH-C 1-5 - 亚烷基，N（C 1-5烷基）亚烷基; R 1是来自任何氨基酸Phe，Tyr，Trp，Pro的残基，其各自可任选地被（C 1-5 - ）烷氧基 （C 1-5）烷基或卤素原子，Ala，Val，Leu或Ile; R 2是衍生自任何氨基酸Gly，Ala，Ile，Val，Ser，Thr，His，Arg，Lys，Pro，Glu，Gln，pGlu，Asp，Leu的残基 和Asn; R 3和R 4独立地表示H，OH，（C 1 -C 5）烷基或（C 1-5 - ）烷氧基，条件是 R 3和R 4不同时为OH或（C 1-5 - ）烷氧基; R 5表示H，OH，（C 1-5 - ）烷基或（C 1-5 - ）烷氧基; 并且其中R 0优选表示肉桂酰残基; 或其药学上可接受的盐。

公开(公告)号：US07129213B2

公开(公告)日：2006-10-31

申请号：US10635797

申请日：2003-08-05

申请人： Jean Rapin ,  Hans Klaus Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

发明人： Jean Rapin ,  Hans Klaus Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

IPC分类号： A61K38/00 ,  A61K38/06 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00 ,  C07K38/00

CPC分类号： C07K5/0823 ,  A61K38/00 ,  C07K5/08 ,  C07K5/0802

摘要： The invention relates to the use of specific tripeptides for the treatment of neurodegenerative diseases, and to pharmaceutical compositions comprising the tripeptides. The tripeptide derivatives satisfy the following formula (I): wherein X represents OH, (C1-5) alkoxy, NH2, NH—C1-5-alkyl, N(C1-5 alkyl)2; R1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one or more (C1-5)alkoxy groups, (C1-5)alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, Leu and Pro; Y1 and Y2 independently from each other represent H or (C1-5)alkyl; R3 and R4 independently from each other represent H, OH, (C1-5)alkyl or (C1-5)alkoxy, provided that R3 and R4 are not both OH or (C1-5)alkoxy; and R5 represents H, OH, (C1-5)alkyl or (C1-5)alkoxy; or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及特异性三肽用于治疗神经变性疾病的用途，以及包含三肽的药物组合物。 三肽衍生物满足下式（I）：其中X表示OH，（C 1-5 - ）烷氧基，NH 2，NH-C 1-5 N（C 1-5烷基）亚烷基，N（C 1-5烷基） R 1是衍生自氨基酸Phe，Tyr，Trp，Pro之一的残基，其各自可以任选地被一个或多个（C 1-5 - （C 1-5）烷基或卤素原子，以及Ala，Val，Leu或Ile; R 2是衍生自氨基酸Gly，Ala，Ile，Val，Ser，Thr，Leu和Pro之一的残基; Y 1和Y 2彼此独立地表示H或（C 1-5烷基）烷基; R 3和R 4彼此独立地表示H，OH，（C 1-5烷基）烷基或（C 1〜 5 S）烷氧基，条件是R 3和R 4不同时为OH或（C 1-5）烷氧基; 和R 5表示H，OH，（C 1-5烷基）烷基或（C 1-5 H 5）烷氧基; 或其药学上可接受的盐。

公开(公告)号：US20050101538A1

公开(公告)日：2005-05-12

申请号：US10635797

申请日：2003-08-05

申请人： Jean Rapin ,  Hans Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

发明人： Jean Rapin ,  Hans Witzmann ,  Jean-Marie Grumel ,  Jacques Gonella

IPC分类号： A61K38/00 ,  A61K38/05 ,  A61K38/06 ,  A61P25/28 ,  C07K5/00 ,  C07K5/06 ,  C07K5/08 ,  C07K5/097

CPC分类号： C07K5/0823 ,  A61K38/00 ,  C07K5/08 ,  C07K5/0802

摘要： The invention relates to the use of specific tripeptides for the treatment of neurodegenerative diseases, and to pharmaceutical compositions comprising the tripeptides. The tripeptide derivatives satisfy the following formula (I): wherein X represents OH, (C1-5) alkoxy, NH2, NH—C1-5-alkyl, N(C1-5 alkyl)2; R1 is a residue derived from one of the amino acids Phe, Tyr, Trp, Pro, which each may be optionally substituted with one or more (C1-5)alkoxy groups, (C1-5)alkyl groups or halogen atoms, as well as Ala, Val, Leu or Ile; R2 is a residue derived from one of the amino acids Gly, Ala, Ile, Val, Ser, Thr, Leu and Pro; Y1 and Y2 independently from each other represent H or (C1-5)alkyl; R3 and R4 independently from each other represent H, OH, (C1-5)alkyl or (C1-5)alkoxy, provided that R3 and R4 are not both OH or (C1-5)alkoxy; and R5 represents H, OH, (C1-5)alkyl or (C1-5)alkoxy; or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及特异性三肽用于治疗神经变性疾病的用途，以及包含三肽的药物组合物。 三肽衍生物满足下式（I）：其中X表示OH，（C 1-5 - ）烷氧基，NH 2，NH-C 1-5 N（C 1-5烷基）亚烷基，N（C 1-5烷基） R 1是衍生自氨基酸Phe，Tyr，Trp，Pro之一的残基，其各自可以任选地被一个或多个（C 1-5 - （C 1-5）烷基或卤素原子，以及Ala，Val，Leu或Ile; R 2是衍生自氨基酸Gly，Ala，Ile，Val，Ser，Thr，Leu和Pro之一的残基; Y 1和Y 2彼此独立地表示H或（C 1-5烷基）烷基; R 3和R 4彼此独立地表示H，OH，（C 1-5烷基）烷基或（C 1〜 5 S）烷氧基，条件是R 3和R 4不同时为OH或（C 1-5）烷氧基; 和R 5表示H，OH，（C 1-5烷基）烷基或（C 1-5 H 5）烷氧基; 或其药学上可接受的盐。

公开(公告)号：US5665377A

公开(公告)日：1997-09-09

申请号：US358897

申请日：1994-12-19

申请人： Jacques Gonella

发明人： Jacques Gonella

IPC分类号： A61K9/70 ,  A61K31/565 ,  A61K31/57 ,  A61K47/10 ,  A61K47/12 ,  A61L15/44 ,  A61F13/02

CPC分类号： A61K9/7061 ,  A61K31/565

摘要： The adhesive plaster for the transdermal administration of estradiol or mixture estradiol/progestin is composed of an impermeable carrier film and of an adhesive composition. The latter represents a matrix or reservoir layer and is composed of a solvent-based polyacrylate or polyisobutylene adhesive which contains a saturated or unsaturated fatty acid with 6 to 18 C atoms as permeability enhancer, estradiol or mixture estradiol/progestin as active substance and optionally propylene glycol as solvent.The adhesive plaster is used for the systemic administration of hormones in hormone replacement therapy for a time of at least 3 days.

摘要翻译： 用于经皮给药雌二醇或混合雌二醇/孕激素的胶粘剂由不透水的载体膜和粘合剂组合物组成。 后者代表基质或储层，并由含有6-18个碳原子的饱和或不饱和脂肪酸作为渗透性增强剂，雌二醇或混合雌二醇/孕激素作为活性物质的溶剂基聚丙烯酸酯或聚异丁烯粘合剂组成， 乙二醇作为溶剂。 胶粘剂用于在激素替代治疗中全身给予激素至少3天的时间。

公开(公告)号：US4476120A

公开(公告)日：1984-10-09

申请号：US344960

申请日：1982-02-02

申请人： Jacques Gonella

发明人： Jacques Gonella

IPC分类号： C07H17/08 ,  A61K31/71

CPC分类号： C07H17/08

摘要： The thiolic salts of erythromycin and of the propionic ester of erythromycin with thenoyl alpha-mercaptopropionylglycine find therapeutical use in the cases in which erythromycin or its propionic ester are used and are generally endowed with very low toxicity and high hematic levels.

摘要翻译： 在使用红霉素或其丙酸酯的情况下，红霉素和红霉素与噻吩甲酰基α-巯基丙酰基甘氨酸的丙酸酯的硫醇盐可用于治疗用途，通常具有非常低的毒性和高血糖水平。

公开(公告)号：US4393053A

公开(公告)日：1983-07-12

申请号：US344961

申请日：1982-02-02

申请人： Jacques Gonella

发明人： Jacques Gonella

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P11/00 ,  A61P11/10 ,  A61P31/04 ,  C07H17/08 ,  A61K31/71

CPC分类号： C07H17/08

摘要： The thiolic salts of erythromycin and of the propionic ester of erythromycin with thenoyl alpha-mercaptopropionylglycine find therapeutical use in the cases in which erythromycin or its propionic ester are used and are generally endowed with very low toxicity and high hematic levels.

摘要翻译： 在使用红霉素或其丙酸酯的情况下，红霉素和红霉素与噻吩甲酰基α-巯基丙酰基甘氨酸的丙酸酯的硫醇盐可用于治疗用途，通常具有非常低的毒性和高血糖水平。