公开(公告)号：US08722852B2

公开(公告)日：2014-05-13

申请号：US13614337

申请日：2012-09-13

Applicant: Hugo Ziegler ,  Dominik Imfeld ,  Martin Stockli ,  Marc Heidl

Inventor： Hugo Ziegler ,  Dominik Imfeld ,  Martin Stockli ,  Marc Heidl

IPC: C07K5/11

CPC classification number: A61Q19/08 ,  A61K8/64 ,  C07K5/0815 ,  C07K5/1019

Abstract: Cosmetic composition which can be applied topically, comprising at least one compound of the general formula (I) in which R1 is H, C1-C20-alkyl, cycloalkyl or aryl-C1-C4-alkyl, n is 1-4, X is —O—, —NH— or —NR2— and R2H or C1-C20-alkyl; and at least one compound corresponding to the above formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid; use of these compounds and of the composition for stimulating the synthesis of the proteins of the basement membrane; and also both those compounds of the formula (I) in which X is —NR2— and both R1 and R2 are different from H, and the compounds corresponding to formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid, as such.

Abstract translation: 可以局部施用的化妆品组合物，其包含至少一种通式（I）的化合物，其中R 1是H，C 1 -C 20 - 烷基，环烷基或芳基-C 1 -C 4 - 烷基，n是1-4，X是 -O - ， - NH-或-NR 2 - 和R 2 H或C 1 -C 20 - 烷基; 和至少一种对应于上述式（I）的化合物，但其中具有可能含义为-NH-的X的XR1为α-氨基酸的残基; 使用这些化合物和组合物刺激基底膜的蛋白质的合成; 以及其中X为-NR 2 - 且R 1和R 2不同于H的式（I）化合物以及对应于式（I）的化合物，但其中具有可能含义为-NH的X的XR1 - 是这样的α-氨基酸的残基。

公开(公告)号：US20120094919A1

公开(公告)日：2012-04-19

申请号：US13254564

申请日：2010-03-16

Applicant: Remo Gräub ,  Marc Heidl ,  Dominik Imfeld ,  Eike Müller ,  Peter Wikstroem ,  Hugo Ziegler

Inventor： Remo Gräub ,  Marc Heidl ,  Dominik Imfeld ,  Eike Müller ,  Peter Wikstroem ,  Hugo Ziegler

IPC: A61K8/64 ,  A61Q19/00

CPC classification number: A61K8/64 ,  A61K38/06 ,  A61Q1/02 ,  A61Q1/04 ,  A61Q1/10 ,  A61Q5/02 ,  A61Q5/12 ,  A61Q19/00 ,  A61Q19/06 ,  A61Q19/08 ,  A61Q19/10

Abstract: The present invention relates to the use of tripeptide derivatives for tightening, firming and/or moisturizing skin. Furthermore, the invention relates to a method for stimulating the synthesis of glycosaminoglycans containing a D-glucosamine and/or N-acetyl-D-glucosamine residue and/or proteoglycans by fibroblasts and/or keratinocytes such as in particular the synthesis of Hyaluronic acid and/or of the proteoglycans Decorin and/or Lumican.

Abstract translation: 本发明涉及三肽衍生物用于紧固，固紧和/或保湿皮肤的用途。 此外，本发明涉及用于刺激含有D-葡糖胺和/或N-乙酰基-D-葡糖胺残基和/或蛋白聚糖的成纤维细胞和/或角质形成细胞的糖胺聚糖的合成的方法，所述方法尤其是合成透明质酸和 /或蛋白聚糖Decorin和/或Lumican。

公开(公告)号：US07863417B2

公开(公告)日：2011-01-04

申请号：US10555994

申请日：2004-05-07

Applicant: Hugo Ziegler ,  Marc Heidl ,  Dominik Imfeld

Inventor： Hugo Ziegler ,  Marc Heidl ,  Dominik Imfeld

IPC: C07K5/08

CPC classification number: C07K7/08 ,  A61K8/64 ,  A61Q19/08

Abstract: The invention relates to compounds and to the cosmetically acceptable salts thereof, which correspond to general formula (I), wherein: R1 represents H, —C(O)—R6, —SO2—R6 or —C(O)—XR6; R2 and R4, independent of one another, represent (CH2)n—NH2 or (CH2)3—NHC(NH)NH2; n equals 1 4; R3 represents linear or branched C1-C4 alkyl that is optionally substituted by hydroxy; R5 and R6, independent of one another, represent hydrogen, optionally substituted (C1-C24) alkyl, optionally substituted C2-C24 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C1-C4 alkyl or 9-fluorenyl-methyl; X represents oxygen (—O—) or —NH—; or XR5 with X═O also represents the esters of a-tocopherol, tocotrienol or retinol, with the provision that R1 and R5 do not represent hydrogen and X does not represent oxygen at the same time. The invention also relates to the production of the compounds of general formula (I) and to a cosmetically active composition that contains at least one compound of formula (I).

Abstract translation: 本发明涉及对应于通式（I）的化合物及其化学上可接受的盐，其中：R 1表示H，-C（O）-R 6，-SO 2 -R 6或-C（O）-XR 6; R 2和R 4彼此独立地表示（CH 2）n -NH 2或（CH 2）3 -NHC（NH）NH 2; n等于1 4; R3表示任选被羟基取代的直链或支链C 1 -C 4烷基; R 5和R 6彼此独立地表示氢，任选取代的（C 1 -C 24）烷基，任选取代的C 2 -C 24烯基，任选取代的苯基，任选取代的苯基-C 1 -C 4烷基或9-芴基 - 甲基; X表示氧（-O-）或-NH-; 或具有X = O的XR5也表示α-生育酚，生育三烯酚或视黄醇的酯，其条件是R1和R5不表示氢，X不同时代表氧。 本发明还涉及通式（I）的化合物的生产和含有至少一种式（I）化合物的化妆品活性组合物。

公开(公告)号：US20090155347A1

公开(公告)日：2009-06-18

申请号：US12226191

申请日：2006-04-28

Applicant: Hugo Ziegler ,  Dominik Imfeld ,  Martin Stockli ,  Marc Heidl

Inventor： Hugo Ziegler ,  Dominik Imfeld ,  Martin Stockli ,  Marc Heidl

IPC: A61K9/127 ,  C07K5/09 ,  A61K38/06

CPC classification number: A61Q19/08 ,  A61K8/64 ,  C07K5/0815 ,  C07K5/1019

Abstract: Cosmetic composition which can be applied topically, comprising at least one compound of the general formula (I) in which R1 is H, C1-C20-alkyl, cycloalkyl or aryl-C1-C4-alkyl, n is 1-4, X is —O—, —NH— or —NR2— and R2H or C1-C20-alkyl; and at least one compound corresponding to the above formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid; use of these compounds and of the composition for stimulating the synthesis of the proteins of the basement membrane; and also both those compounds of the formula (I) in which X is —NR2— and both R1 and R2 are different from H, and the compounds corresponding to formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid, as such.

Abstract translation: 可以局部施用的化妆品组合物，其包含至少一种通式（I）的化合物，其中R 1是H，C 1 -C 20 - 烷基，环烷基或芳基-C 1 -C 4 - 烷基，n是1-4，X是 -O - ， - NH-或-NR 2 - 和R 2 H或C 1 -C 20 - 烷基; 和至少一种对应于上述式（I）的化合物，但其中具有可能含义为-NH-的X的XR1为α-氨基酸的残基; 使用这些化合物和组合物刺激基底膜的蛋白质的合成; 以及其中X为-NR 2 - 且R 1和R 2不同于H的式（I）化合物以及对应于式（I）的化合物，但其中具有可能含义为-NH的X的XR1 - 是这样的α-氨基酸的残基。

公开(公告)号：US08420778B2

公开(公告)日：2013-04-16

申请号：US12954142

申请日：2010-11-24

Applicant: Hugo Ziegler ,  Marc Heidl ,  Dominik Imfeld

Inventor： Hugo Ziegler ,  Marc Heidl ,  Dominik Imfeld

IPC: C07K5/08

CPC classification number: C07K7/08 ,  A61K8/64 ,  A61Q19/08

Abstract: The invention relates to compounds and to the cosmetically acceptable salts thereof, which correspond to general formula (I), wherein: R1 represents H, —C(O)—R6, —SO2—R6 or —C(O)—XR6; R2 and R4, independent of one another, represent (CH2)n—NH2 or (CH2)3—NHC(NH)NH2; n equals 1 4; R3 represents linear or branched C1-C4 alkyl that is optionally substituted by hydroxy; R5 and R6, independent of one another, represent hydrogen, optionally substituted (C1-C24)alkyl, optionally substituted C2-C24 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C1-C4 alkyl or 9-fluorenyl-methyl; X represents oxygen (—O—) or NH—; or XR5 with X═O also represents the esters of a-tocopherol, tocotrienol or retinol, with the provision that R1 and R5 do not represent hydrogen and X does not represent oxygen at the same time. The invention also relates to the production of the compounds of general formula (I) and to a cosmetically active composition that contains at least one compound of formula (I).

Abstract translation: 本发明涉及对应于通式（I）的化合物及其化学上可接受的盐，其中：R 1表示H，-C（O）-R 6，-SO 2 -R 6或-C（O）-XR 6; R 2和R 4彼此独立地表示（CH 2）n -NH 2或（CH 2）3 -NHC（NH）NH 2; n等于1 4; R3表示任选被羟基取代的直链或支链C 1 -C 4烷基; R 5和R 6彼此独立地表示氢，任选取代的（C 1 -C 24）烷基，任选取代的C 2 -C 24烯基，任选取代的苯基，任选取代的苯基-C 1 -C 4烷基或9-芴基 - 甲基; X表示氧（-O-）或NH-; 或具有X = O的XR5也表示α-生育酚，生育三烯酚或视黄醇的酯，其条件是R1和R5不表示氢，X不同时代表氧。 本发明还涉及通式（I）的化合物的生产和含有至少一种式（I）化合物的化妆品活性组合物。

公开(公告)号：US08293712B2

公开(公告)日：2012-10-23

申请号：US12226191

申请日：2006-04-28

Applicant: Hugo Ziegler ,  Dominik Imfeld ,  Martin Stöckli ,  Marc Heidl

Inventor： Hugo Ziegler ,  Dominik Imfeld ,  Martin Stöckli ,  Marc Heidl

IPC: A61K38/39 ,  A61K38/00 ,  A61K31/74

CPC classification number: A61Q19/08 ,  A61K8/64 ,  C07K5/0815 ,  C07K5/1019

Abstract: Cosmetic composition which can be applied topically, comprising at least one compound of the general formula (I) in which R1 is H, C1-C20-alkyl, cycloalkyl or aryl-C1-C4-alkyl, n is 1-4, X is —O—, —NH— or —NR2— and R2H or C1-C20-alkyl; and at least one compound corresponding to the above formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid; use of these compounds and of the composition for stimulating the synthesis of the proteins of the basement membrane; and also both those compounds of the formula (I) in which X is —NR2— and both R1 and R2 are different from H, and the compounds corresponding to formula (I) but in which XR1 with X having the possible meaning of —NH— is the residue of an alpha-amino acid, as such.

Abstract translation: 可以局部施用的化妆品组合物，其包含至少一种通式（I）的化合物，其中R 1是H，C 1 -C 20 - 烷基，环烷基或芳基-C 1 -C 4 - 烷基，n是1-4，X是 -O - ， - NH-或-NR 2 - 和R 2 H或C 1 -C 20 - 烷基; 和至少一种对应于上述式（I）的化合物，但其中具有可能含义为-NH-的X的XR1为α-氨基酸的残基; 使用这些化合物和组合物刺激基底膜的蛋白质的合成; 以及其中X为-NR 2 - 且R 1和R 2不同于H的式（I）化合物以及对应于式（I）的化合物，但其中具有可能含义为-NH的X的XR1 - 是这样的α-氨基酸的残基。

公开(公告)号：US20110142895A1

公开(公告)日：2011-06-16

申请号：US12954142

申请日：2010-11-24

Applicant: Hugo Ziegler ,  Marc Heidl ,  Dominik Imfeld

Inventor： Hugo Ziegler ,  Marc Heidl ,  Dominik Imfeld

IPC: A61K8/64 ,  A61Q19/08 ,  A61K38/06 ,  A61Q19/04 ,  A61P17/10 ,  A61P17/18 ,  A61P29/00 ,  A61Q19/06 ,  A61P31/00 ,  A61P17/00 ,  A61Q17/04 ,  A61K8/02 ,  B82Y5/00

CPC classification number: C07K7/08 ,  A61K8/64 ,  A61Q19/08

Abstract: The invention relates to compounds and to the cosmetically acceptable salts thereof, which correspond to general formula (I), wherein: R1 represents H, —C(O)—R6, —SO2—R6or —C(O)—XR6; R2 and R4, independent of one another, represent (CH2)n—NH2 or (CH2)3—NHC(NH)NH2; n equals 1 4; R3 represents linear or branched C1-C4 alkyl that is optionally substituted by hydroxy; R5 and R6, independent of one another, represent hydrogen, optionally substituted (C1-C24)alkyl, optionally substituted C2-C24 alkenyl, optionally substituted phenyl, optionally substituted phenyl-C1-C4 alkyl or 9-fluorenyl-methyl; X represents oxygen (—O—) or NH—; or XR5 with X═O also represents the esters of a-tocopherol, tocotrienol or retinol, with the provision that R1 and R5 do not represent hydrogen and X does not represent oxygen at the same time. The invention also relates to the production of the compounds of general formula (I) and to a cosmetically active composition that contains at least one compound of formula (I).

Abstract translation: 本发明涉及对应于通式（I）的化合物及其化学上可接受的盐，其中：R 1表示H，-C（O）-R 6，-SO 2 -R 6或-C（O）-XR 6; R 2和R 4彼此独立地表示（CH 2）n -NH 2或（CH 2）3 -NHC（NH）NH 2; n等于1 4; R3表示任选被羟基取代的直链或支链C 1 -C 4烷基; R 5和R 6彼此独立地表示氢，任选取代的（C 1 -C 24）烷基，任选取代的C 2 -C 24烯基，任选取代的苯基，任选取代的苯基-C 1 -C 4烷基或9-芴基 - 甲基; X表示氧（-O-）或NH-; 或具有X = O的XR5也表示α-生育酚，生育三烯酚或视黄醇的酯，其条件是R1和R5不表示氢，X不同时代表氧。 本发明还涉及通式（I）的化合物的生产和含有至少一种式（I）化合物的化妆品活性组合物。

公开(公告)号：US20120129786A1

公开(公告)日：2012-05-24

申请号：US13264059

申请日：2010-04-23

Applicant: Marc Heidl ,  Roman Wille ,  Hugo Ziegler

Inventor： Marc Heidl ,  Roman Wille ,  Hugo Ziegler

IPC: A61K8/64 ,  C01D15/04 ,  C01F11/24 ,  C01D3/04 ,  C01F5/30 ,  A61Q19/00 ,  C01G9/04

CPC classification number: C07K5/0815 ,  A61K8/19 ,  A61K8/64 ,  A61Q19/00 ,  A61Q19/06 ,  C07K5/1019

Abstract: The present invention relates to compositions comprising a peptide with 2-12 amino acids substituted with a lipophilic moiety and a water soluble salt of an alkali, earth alkaline metal or transition metal. Furthermore, the invention relates to a container comprising such compositions. Additionally, the invention relates to the use of a water soluble salt of an alkali, earth alkaline metal or transition metal for reducing the adhesion of a peptide with 2-12 amino acids substituted with a lipophilic moiety to a surface.

Abstract translation: 本发明涉及包含用亲脂性部分取代的2-12个氨基酸的肽和碱金属，碱土金属或过渡金属的水溶性盐的组合物。 此外，本发明涉及包含这种组合物的容器。 此外，本发明涉及碱，碱土金属或过渡金属的水溶性盐用于降低被亲脂性部分取代的2-12个氨基酸与表面的粘附的用途。

公开(公告)号：US20050065090A1

公开(公告)日：2005-03-24

申请号：US10493856

申请日：2002-10-30

Applicant: Christian Ludin ,  Marc Heidl ,  Hugo Ziegler

Inventor： Christian Ludin ,  Marc Heidl ,  Hugo Ziegler

IPC: A61K38/00 ,  A61P17/00 ,  C07K5/068 ,  C07K14/78 ,  A61K38/08 ,  C07K7/06

CPC classification number: C07K14/78 ,  A61K38/00 ,  C07K5/06086

Abstract: Oligopeptides and derivatives thereof, peptide analogs and derivatives thereof as well as pharmaceutically acceptable salts of these compounds, which correspond to general formula (I) wherein R1 represents H, —C(O)—R7, —SO2—R7, —C(O)—OR7 or —C(O)—N(R7)2 R2 represents, independent of one another, H or —(C1-C4)-alkyl, R3 and R6 represent, independent of one another, —(CH2)q—N(R1)R8 R4 and R5 represent, independent of one another, —CH2—OR2, —CH(CH3)OR8 or —CH2—CH2—OR8 R7 represents hydrogen, optionally substituted (C1-C19)-alkyl; optionally substituted (C1-C19)-alkenyl; phenyl-(C1-C4)-alkyl whose phenyl radical is optionally substituted with amino in the para position R8 represents H, —(C1-C4)-alkyl, —C(O)—R7, —C(O)—OR7, —C(O)—N(R7)2 or —SO2—R7 X represents oxygen (—O—) or —NH—; or XR7, with X=O, also represents the esters of α-tocopherol, tocotrienol or retinol or the carboxylic acid (with R7=H) m, n, p represent, independent of one another, zero or 1 and q in R3 and R6 represent, independent of one another, an integer from 1 to 4, with the provision that the following conditions do not simultaneously occur: R4=—CH(CH3)—OH and R5=—CH(CH3)—OH and R6=—(CH2)4—NH2; dermopharmaceutically and/or cosmetically active compositions containing at least one compound of formula (I).

Abstract translation: 对应于通式（I）的寡肽及其衍生物，肽类似物及其衍生物以及这些化合物的药学上可接受的盐，其中R 1表示H，-C（O）-R 7，-SO 2 - R 7，-C（O）-OR 7或-C（O）-N（R 7）2 R 2彼此独立地表示H或 - （C 1 -C 4） - 烷基，R 3和R 6彼此独立地表示 - （CH 2）q N（R 1）R 8 R 4和R 5彼此独立地表示 - CH2-OR2，-CH（CH3）OR8或-CH2-CH2-OR8表示氢，任选取代的（C 1 -C 19） - 烷基; 任选取代的（C 1 -C 19） - 烯基; 苯基 - （C 1 -C 4） - 烷基，其苯基任选被对位R 8中的氨基取代，代表H， - （C 1 -C 4） - 烷基，-C（O）-R 7，-C （O）-OR 7，-C（O）-N（R 7）2或-SO 2 -R 7表示氧（-O-）或-NH-; 或XR 7，X = O也表示α-生育酚，生育三烯酚或视黄醇或羧酸（R 7 = H）m，n，p彼此独立地为0或 1和q在R 3和R 6中彼此独立地表示1至4的整数，条件是不同时发生以下条件：R 4 = -CH（CH 3） - OH和R 5 = -CH（CH 3）-OH，R 6 = - （CH 2）4 -NH 2; 含有至少一种药物的药物和/或化妆品活性组合物

公开(公告)号：US07671009B2

公开(公告)日：2010-03-02

申请号：US10493856

申请日：2002-10-30

Applicant: Christian Ludin ,  Marc Heidl ,  Hugo Ziegler

Inventor： Christian Ludin ,  Marc Heidl ,  Hugo Ziegler

IPC: A61K38/00

CPC classification number: C07K14/78 ,  A61K38/00 ,  C07K5/06086

Abstract: Oligopeptides and derivatives thereof, peptide analogs and derivatives thereof as well as pharmaceutically acceptable salts of these compounds, which correspond to general formula (I) wherein R1 represents H, —C(O)—R7, —SO2—R7, —C(O)—OR7 or —C(O)—N(R7)2 R2 represents, independent of one another, H or —(C1-C4)-alkyl, R3 and R6 represent, independent of one another, —(CH2)q—N(R1)R8 R4 and R5 represent, independent of one another, —CH2—OR2, —CH(CH3)OR8 or —CH2—CH2—OR8 R7 represents hydrogen, optionally substituted (C1-C19)-alkyl; optionally substituted (C1-C19)-alkenyl; phenyl-(C1-C4)-alkyl whose phenyl radical is optionally substituted with amino in the para position R8 represents H, —(C1-C4)-alkyl, —C(O)—R7, —C(O)—OR7, —C(O)—N(R7)2 or —SO2—R7 X represents oxygen (—O—) or —NH—; or XR7, with X=O, also represents the esters of α-tocopherol, tocotrienol or retinol or the carboxylic acid (with R7=H) m, n, p represent, independent of one another, zero or 1 and q in R3 and R6 represent, independent of one another, an integer from 1 to 4, with the provision that the following conditions do not simultaneously occur: R4=—CH(CH3)—OH and R5=—CH(CH3)—OH and R6=—(CH2)4—NH2; dermopharmaceutically and/or cosmetically active compositions containing at least one compound of formula (I).

Abstract translation: 对应于通式（I）的寡肽及其衍生物，肽类似物及其衍生物以及这些化合物的药学上可接受的盐，其中R 1表示H，-C（O）-R 7，-SO 2 -R 7，-C（O ）-OR 7或-C（O）-N（R 7）2 R 2彼此独立地表示H或 - （C 1 -C 4） - 烷基，R 3和R 6彼此独立地表示 - （CH 2）q - N（R 1）R 8 R 4和R 5彼此独立地表示-CH 2 OR 2，-CH（CH 3）OR 8或-CH 2 -CH 2 -OR 8 R 7表示氢，任选取代的（C 1 -C 19） - 烷基; 任选取代的（C 1 -C 19） - 烯基; 苯基 - （C 1 -C 4） - 烷基，其苯基任选被对位R8上的氨基取代，代表H， - （C1-C4） - 烷基，-C（O）-R7，-C（O）-OR7， -C（O）-N（R 7）2或-SO 2 -R 7 X表示氧（-O-）或-NH-; 或具有X = O的XR7也表示α-生育酚，生育三烯酚或视黄醇或羧酸（R7 = H）m，n，p表示彼此独立的零或1和q在R3和 R6代表彼此独立的1至4的整数，条件是不同时发生以下条件：R4 = -CH（CH3）-OH，R5 = -CH（CH3）-OH，R6 = - （CH 2）4 -NH 2; 含有至少一种式（I）化合物的药物和/或化妆品活性组合物。