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1. 发明申请

WO0105810A3 CYCLIC PEPTIDE DERIVATIVES AS INHIBITORS OF INTEGRIN alpha V beta 6 审中-公开
标题翻译：环状肽衍生物作为抑制剂的整合素v的β6
公开(公告)号：WO0105810A3
公开(公告)日：2001-05-17
申请号：PCT/EP0006188
申请日：2000-07-03
申请人： MERCK PATENT GMBH , JONCZYK ALFRED , DIEFENBACH BEATE , GOODMAN SIMON , GROTH ULRICH , ZISCHINSKY GUNTHER
发明人： JONCZYK ALFRED , DIEFENBACH BEATE , GOODMAN SIMON , GROTH ULRICH , ZISCHINSKY GUNTHER
IPC分类号： A61K38/00 , A61P7/02 , A61P9/10 , A61P17/02 , A61P17/06 , A61P19/10 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07K7/50 , C07K7/64 , C07K7/56 , A61K38/04
CPC分类号： C07K7/64 , A61K38/00
摘要： The invention relates to novel peptide derivatives of formula (I): Cyclo-(Arg-X -Asp-X -X -X -X -X -R ); which are biologically active as ligands of integrin alpha v beta 6, X representing Ser, Gly or Thr; X representing Leu, Ile, Nle, Val or Phe; X representing Asp, Glu, Lys or Phe; X representing Gly, Ala or Ser; X representing Leu, Ile, Nle, Val or Phe; X representing Arg, Har or Lys; and R being left out or representing one or more omega -aminocarboxylic acid radicals, said omega -aminocarboxylic acid radical(s) being 500 to 2500 pm in length. Said amino acids can also be derivatised and the D and L forms of the optically active amino acid radicals are enclosed. The invention also relates to the physiologically suitable salts and solvates of the inventive derivatives.
摘要翻译：本发明涉及适用作的整合素v的β6配体的生物活性式（I）的新型肽衍生物：环（精氨酸 - X <1> -Asp-X <2> -X <3> -X <4> -X <5> -X <6> -R <1>），其中X <1>丝氨酸，甘氨酸或Thr，X <2>亮氨酸，异亮氨酸，NLE，缬氨酸或Phe，X <3>天冬氨酸，谷氨酸，赖氨酸或Phe，X <4>甘氨酸，丙氨酸，或Ser，X <5>亮氨酸，异亮氨酸，NLE，缬氨酸或Phe，X <6>精氨酸中，HAr或Lys，R <1>不存在或一种或多种ω-Aminocarbonsäurerest （e）其中，所述一种或多种ω-Aminocarbonsäurerest（E）具有500至2500分的长度已平均，其中所述氨基酸也可以被衍生化，其被并入D-和光学活性的氨基酸残基的L型，和生理上可接受的盐和溶剂合物。

2. 发明申请

WO0220566A3 NOVEL MMP-2 DERIVATIVES FOR USE AS INHIBITORS OF INTEGRIN alpha V beta 3 审中-公开
标题翻译：新的衍生AS MMP-2抑制剂的整合素v的β3的
公开(公告)号：WO0220566A3
公开(公告)日：2002-06-27
申请号：PCT/EP0109899
申请日：2001-08-28
申请人： MERCK PATENT GMBH , JONCZYK ALFRED , DIEFENBACH BEATE , GROTH ULRICH , ZISCHINSKY GUNTHER
发明人： JONCZYK ALFRED , DIEFENBACH BEATE , GROTH ULRICH , ZISCHINSKY GUNTHER
IPC分类号： C12N9/50 , A61K38/55 , A61P1/04 , A61P3/10 , A61P3/14 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/14 , A61P11/00 , A61P13/10 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P27/02 , A61P27/06 , A61P27/10 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P35/00 , A61P43/00 , C07K14/47 , C12N9/64 , A61K38/48
CPC分类号： C12N9/6491
摘要： The invention relates to novel compounds of the formula (I), which are biologically active as the ligands of integrin alpha V beta 3and wherein X represents H, an acyl or a peptide fragment of 1 to 20 amino acids, selected from the list of the naturally occurring amino acids, Y represents a peptide fragment selected from the sequence range 466-660 of human Pro-MMP-2, Z represents OH, NH2, NHA, NA2 or a peptide fragment of 1 to 20 amino acids, selected from the list of the naturally occurring amino acids, A represents an alkyl having 1-10 C atoms, and acyl represents an alkanoyl having 1-10 C atoms, wherein the primary amino groups can be also provided with conventional amine protecting groups. The invention further relates to the physiologically acceptable salts and solvates of these novel compounds.
摘要翻译：本发明涉及适用作整合素v的β3，其中X是H，酰基，或由天然存在的氨基酸的列表中选出的1〜20个氨基酸的肽片段的配体的生物活性式（I）的新化合物，Y是所选择的肽片段从人原MMP-2的序列区域466-660，Z为OH，NH 2，NHA，NA2或1〜20个氨基酸的肽片段从天然存在的氨基酸的列表中选择，a为具有1-10个C原子的烷基，酰基是链烷酰基具有1-10个C原子的，意思是说，其特征在于，所述伯氨基，也可以提供与常规的氨基保护基团，和它们的生理学上可接受的盐和溶剂合物。

3. 发明专利

DE19928820A1 Fixative for cells and tissues, useful in cytological or histological diagnosis, comprises mixture of alcohols, acetone, evaporation retardant and pH regulator 未知
公开(公告)号：DE19928820A1
公开(公告)日：2000-12-21
申请号：DE19928820
申请日：1999-06-17
申请人： GROTH ULRICH
发明人： GROTH ULRICH
IPC分类号： G01N1/30 , C12Q1/24 , G01N1/28 , G01N33/48
摘要： A fixative (A) for cells and tissue comprising (by volume): (1) 20-77% mixed alcohols (ethanol, methanol, 1- and 2-propanols); (2) 20-77% acetone; (3) 0-10% distilled water; (4) 1-2.5% poly(ethylene glycol) (PEG) of molecular weight 200-6000 or glycerol; (5) 1-4% each of acetic acid (as 96% acid) and/or saturated potassium acetate solution; and (6) has a pH of 2-6.5, is new.

4. 发明专利

DE502004007051D1 未知
公开(公告)号：DE502004007051D1
公开(公告)日：2008-06-19
申请号：DE502004007051
申请日：2004-01-14
申请人： MERCK PATENT GMBH
发明人： JONCZYK ALFRED , GROTH ULRICH , ZISCHINSKY GUNTHER
IPC分类号： C07K7/06 , A61K38/00 , A61K38/08
摘要： The invention relates to novel peptides which are biologically active as ligands of blood platelet integrin GPIIbIIIa and the αv integrins, preferably the av&bgr;s and αv&bgr;3 integrin, having the formula (I): R1-Arg-X-Asp-Leu-Asp-Ser-Leu-Arg-R2 (I), in which R1 denotes H, acetyl or acyl and R2 denotes -Oh, OR3NH2, NHR3, N(R3)2 R3 denotes atkyl, aralkyl, aryl, Het and X denotes an amino acid of the formula (II), in which A denotes (CH2)n R4 denotes H, alkyl, aralkyl or aryl, and n denotes 1, 2, 3, 4, 5 or 6, and the amino acid of the formula (II) is bonded to the adjacent Arg via a peptide bond of the α-amino group and to the α-amino group of the adjacent Asp via a peptide bond of the α-carboxyl group.

5. 发明专利

PT1196433E DERIVADOS DE PEPTIDOS CICLICOS COMO INIBIDORES DA INTEGRINA CLVBG 未知
公开(公告)号：PT1196433E
公开(公告)日：2007-01-31
申请号：PT00943971
申请日：2000-07-03
申请人： MERCK PATENT GMBH
发明人： JONCZYK ALFRED , GOODMAN SIMON , DIEFENBACH BEATE , GROTH ULRICH , ZISCHINSKY GUNTHER
IPC分类号： A61K38/00 , C07K7/56 , A61K38/04 , A61P7/02 , A61P9/10 , A61P17/02 , A61P17/06 , A61P19/10 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07K7/50 , C07K7/64

6. 发明专利

ZA200507116B Peptidic sulfonamides 未知
公开(公告)号：ZA200507116B
公开(公告)日：2006-08-30
申请号：ZA200507116
申请日：2005-09-05
申请人： MERCK PATENT GMBH
发明人： JONCZYK ALFRED , ZISCHINSKY GUNTHER , GROTH ULRICH
IPC分类号： A61K20060101 , A61K38/00 , A61K38/08 , C07K20060101 , C07K7/06
摘要： The invention relates to novel peptides which are biologically active as ligands of blood platelet integrin GPIIbIIIa and the αv integrins, preferably the av&bgr;s and αv&bgr;3 integrin, having the formula (I): R1-Arg-X-Asp-Leu-Asp-Ser-Leu-Arg-R2 (I), in which R1 denotes H, acetyl or acyl and R2 denotes -Oh, OR3NH2, NHR3, N(R3)2 R3 denotes atkyl, aralkyl, aryl, Het and X denotes an amino acid of the formula (II), in which A denotes (CH2)n R4 denotes H, alkyl, aralkyl or aryl, and n denotes 1, 2, 3, 4, 5 or 6, and the amino acid of the formula (II) is bonded to the adjacent Arg via a peptide bond of the α-amino group and to the α-amino group of the adjacent Asp via a peptide bond of the α-carboxyl group.

7. 发明专利

CA2377224A1 INHIBITORS OF THE INTEGRIN .ALPHA.V.BETA.6 未知
公开(公告)号：CA2377224A1
公开(公告)日：2001-01-04
申请号：CA2377224
申请日：2000-06-13
申请人： MERCK PATENT GMBH
发明人： ZISCHINSKY GUNTHER , DIEFENBACH BEATE , JONCZYK ALFRED , GROTH ULRICH
IPC分类号： A61K38/00 , A61P7/02 , A61P9/10 , A61P11/00 , A61P17/06 , A61P19/10 , A61P21/00 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07K7/02 , C07K7/06 , A61K38/04
摘要： The invention relates to novel peptides of formula (I) Ac-Arg-X1-Asp-X2-X3-X 4- X5-X6-NH2 which are biologically active as ligands of the integrin .alpha.v.beta.6, wherein: Ac represents Acetyl, X1 represents Ser, Gly, Thr, Asp, Arg, Val, Tyr, His or Ala; X2 represents Leu, Ile, Nle, Val or Phe; X3 represents Asp, Glu, Lys, Phe, Aib, Nal, Gly, Ala, Bgl or Phg; X4 represents Gly, Ala, Ser, .beta.-Ala or .omega.-Abu; X5 represents Leu, Ile, Nle, Val o r Phe, and; X6 represents Arg, Har, Lys, Leu, Orn, Phe, Ala, Tyr, Gly, Ser or Asp, whereby the aforementioned amino acids can be derivatized. The amino ac id radicals are linked to one another in a peptide-like manner via the .alpha.- amino groups and the .alpha.-carboxy groups. The dextrorotatory forms and th e levorotatory forms of the optically active amino acid radicals are contained as well as the salts of said peptides. Ac-Arg-Thr-Asp-Leu-Asp-Ser-Leu-Arg-NH 2 is excluded. The inventive peptides can also be used as effective inhibitors of the .alpha.v.beta.6 integrin receptor and thus for treating different diseases and pathological findings.

8. 发明专利

ES2309487T3 SULFONAMIDAS PEPTIDICAS. 未知
公开(公告)号：ES2309487T3
公开(公告)日：2008-12-16
申请号：ES04701939
申请日：2004-01-14
申请人： MERCK PATENT GMBH
发明人： JONCZYK ALFRED , GROTH ULRICH , ZISCHINSKY GUNTHER
IPC分类号： C07K7/06 , A61K38/00 , A61K38/08
摘要： Compuestos peptídicos de fórmula I R 1 - Arg - X - Asp - Leu - Asp - Ser - Leu - Arg - R 2 I en la que R 1 representa H, acetilo o acilo y R 2 representa -OH, OR 3 NH2,NHR 3 , N(R 3 )2 R 3 representa alquilo, aralquilo, arilo, Het y X representa un aminoácido de fórmula II (Ver fórmula) en la que A representa representa (CH2)n R 4 representa aralquilo o arilo y n representa 1, 2, 3, 4, 5 o 6 y el aminoácido de fórmula II está unido mediante un enlace peptídico del grupo alfa-amino con la Arg contigua y mediante un enlace peptídico del grupo alfa-carboxilo con el grupo alfa-amino de la Asp contigua, así como sus compuestos de utilidad farmacéutica a) profármacos, seleccionados entre compuestos de fórmula I modificados con grupos alquilo o acilo, azúcares u oligopéptidos, b) derivados, seleccionados entre N-metil-, N-etil-, N-propil-, N-bencil- y Calfa-metilderivados, así como derivados que llevan grupos acetilo N-terminales o en los que los grupos acetilo se sustituyen por otra función acilo, seleccionada entre propionilo, butirilo y benzoilo, c) solvatos, d) estereoisómeros y e) sales de estos, incluyendo sus mezclas en todas las proporciones.

9. 发明专利

AT394415T 未知
公开(公告)号：AT394415T
公开(公告)日：2008-05-15
申请号：AT04701939
申请日：2004-01-14
申请人： MERCK PATENT GMBH
发明人： JONCZYK ALFRED , GROTH ULRICH , ZISCHINSKY GUNTHER
IPC分类号： C07K7/06 , A61K38/00 , A61K38/08
摘要： The invention relates to novel peptides which are biologically active as ligands of blood platelet integrin GPIIbIIIa and the αv integrins, preferably the av&bgr;s and αv&bgr;3 integrin, having the formula (I): R1-Arg-X-Asp-Leu-Asp-Ser-Leu-Arg-R2 (I), in which R1 denotes H, acetyl or acyl and R2 denotes -Oh, OR3NH2, NHR3, N(R3)2 R3 denotes atkyl, aralkyl, aryl, Het and X denotes an amino acid of the formula (II), in which A denotes (CH2)n R4 denotes H, alkyl, aralkyl or aryl, and n denotes 1, 2, 3, 4, 5 or 6, and the amino acid of the formula (II) is bonded to the adjacent Arg via a peptide bond of the α-amino group and to the α-amino group of the adjacent Asp via a peptide bond of the α-carboxyl group.

10. 发明专利

AU771099B2 Inhibitors of the integrin alphavbeta6 未知
公开(公告)号：AU771099B2
公开(公告)日：2004-03-11
申请号：AU6263000
申请日：2000-06-13
申请人： MERCK PATENT GMBH
发明人： JONCZYK ALFRED , DIEFENBACH BEATE , GROTH ULRICH , ZISCHINSKY GUNTHER
IPC分类号： A61K38/00 , A61P7/02 , A61P9/10 , A61P11/00 , A61P17/06 , A61P19/10 , A61P21/00 , A61P29/00 , A61P31/00 , A61P35/00 , A61P43/00 , C07K7/02 , C07K7/06 , A61K38/04
摘要： The invention relates to novel peptides of formula (I) Ac-Arg-X -Asp-X -X -X -X -X -NH2 which are biologically active as ligands of the integrin alpha v beta 6, wherein: Ac represents Acetyl, X represents Ser, Gly, Thr, Asp, Arg, Val, Tyr, His or Ala; X represents Leu, Ile, Nle, Val or Phe; X represents Asp, Glu, Lys, Phe, Aib, Nal, Gly, Ala, Bgl or Phg; X represents Gly, Ala, Ser, beta -Ala or omega -Abu; X represents Leu, Ile, Nle, Val or Phe, and; X represents Arg, Har, Lys, Leu, Orn, Phe, Ala, Tyr, Gly, Ser or Asp, whereby the aforementioned amino acids can be derivatized. The amino acid radicals are linked to one another in a peptide-like manner via the alpha -amino groups and the alpha -carboxy groups. The dextrorotatory forms and the levorotatory forms of the optically active amino acid radicals are contained as well as the salts of said peptides. Ac-Arg-Thr-Asp-Leu-Asp-Ser-Leu-Arg-NH2 is excluded. The inventive peptides can also be used as effective inhibitors of the alpha v beta 6 integrin receptor and thus for treating different diseases and pathological findings.

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