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1. 发明申请

WO1998025951A1 INHIBITORS OF PEPTIDE BINDING TO MHC CLASS II PROTEINS 审中-公开
标题翻译：肽类与MHC II类蛋白质结合的抑制剂
公开(公告)号：WO1998025951A1
公开(公告)日：1998-06-18
申请号：PCT/GB1997003397
申请日：1997-12-09
申请人： ZENECA LIMITED , LUKE, Richard, William, Arthur , COTTON, Ronald
发明人： ZENECA LIMITED
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00 , C07K14/4713
摘要： The invention concerns pharmaceutically useful peptide derivatives of the formula (I): P-AA -AA -AA -AA -AA -AA -AA -AA -Q, in which P, AA , AA , AA , AA , AA , AA , AA , AA and Q have various meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel peptide derivatives are of value in treating MHC class II dependent T-cell mediated autoimmune or inflammatory diseases, such as rheumatoid arthritis. The invention further concerns processes for the manufacture of the novel peptide derivatives and the use of the compounds in medical treatment.
摘要翻译：本发明涉及式（I）的药学上有用的肽衍生物：P-AA 1 -A 2 -AA 3 -AA 4 -AA 5 -AA 6 -AA 7 -A A 8 -A，其中P，AA 1，AA 2，AA 3，AA 4，AA 5，AA 6，AA 7，AA 8 且Q具有本文定义的各种含义及其药学上可接受的盐和含有它们的药物组合物。新型肽衍生物在治疗MHC II类依赖性T细胞介导的自身免疫性或炎性疾病如类风湿性关节炎中是有价值的。本发明还涉及制备新型肽衍生物的方法和该化合物在医疗中的用途。

2. 发明申请

WO1998012219A1 METHIONINE, PENICILLAMINE AND CYSTEINE-ANALOGUE CONTAINING PEPTIDES HAVING IMMUNOMODULATING ACTIVITY 审中-公开
标题翻译：含有免疫调节活性的甲硫氨酸，苯胺胺和CYSTEINE-ANALOGUE含有肽
公开(公告)号：WO1998012219A1
公开(公告)日：1998-03-26
申请号：PCT/SE1997001554
申请日：1997-09-15
申请人： ASTRA AKTIEBOLAG , BERGSTRAND, Håkan , ERIKSSON, Tomas , LINDVALL, Magnus , SÄRNSTRAND, Bengt
发明人： ASTRA AKTIEBOLAG
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00
摘要： Physiologically active peptides of 8ormula (I): A-R1-R2-R3-(R4)x-B, wherein each variable has the meaning mentioned in the description at least one of R1, R2 and R3 being R8 and at most one of R1, R2 and R3 being cysteine; and R8 is an amino acid residue of formula (II) or formula (III), wherein each variable has the meaning described in the description, the entire peptide sequence containing 3 to 30 amino acid residues; or a homo- or heterodimers thereof. These peptides are absorbable by the epithelial cell lining in a mammal resulting in a modulated immune response and thereby a therapeutic effect against disease.
摘要翻译：（I）：A-R1-R2-R3-（R4）xB的生理活性肽，其中每个变量具有说明书中提及的含义，R 1，R 2和R 3中的至少一个为R 8，并且至少一个R 1， R2和R3是半胱氨酸; 并且R 8是式（II）或式（III）的氨基酸残基，其中每个变量具有描述中描述的含义，整个含有3至30个氨基酸残基的肽序列; 或其同二聚体或异二聚体。这些肽可以通过哺乳动物的上皮细胞衬里吸收，导致调节的免疫应答，从而对抗疾病的治疗效果。

3. 发明申请

WO1997039025A1 A CYCLIC HEPTA-PEPTIDE DERIVATIVE FROM COLONIAL ASCIDIANS, LISSOCLINUM SP. 审中-公开
标题翻译：来自Colonique ASCIDIANS，LISSOCLINUM SP。的循环HEPTA-PEPTIDE
公开(公告)号：WO1997039025A1
公开(公告)日：1997-10-23
申请号：PCT/GB1997001088
申请日：1997-04-18
申请人： PHARMA MAR, S.A. , RUFFLES, Graham, Keith , BOWDEN, Bruce, Frederick , GARCIA, Gravalos, Dolores
发明人： PHARMA MAR, S.A. , RUFFLES, Graham, Keith
IPC分类号： C07K07/06
CPC分类号： C07K7/56 , A61K38/00 , C07K7/06
摘要： A new cyclic heptapeptide, trunkamide A, with antitumor activity has been isolated from a Lissoclinum sp. collected on the Great Barrier Reef, Australia. The structure was determined to be of formula (I).
摘要翻译：已经从Lissoclinum sp中分离出具有抗肿瘤活性的新的环七肽，树干酰胺A。收集在澳大利亚的大堡礁。该结构确定为式（I）。

4. 发明申请

WO1997022621A2 ANTINEOPLASTIC PEPTIDES 审中-公开
标题翻译：抗生素PEPTIDES
公开(公告)号：WO1997022621A2
公开(公告)日：1997-06-26
申请号：PCT/EP1996005518
申请日：1996-12-11
申请人： BASF AKTIENGESELLSCHAFT , AMBERG, Wilhelm , BARLOZZARI, Teresa , BERNARD, Harald , BUSCHMANN, Ernst , HAUPT, Andreas , HEGE, Hans-Guenther , JANSSEN, Bernd , KLING, Andreas , LIETZ, Helmut , RITTER, Kurt , ULLRICH, Martina , WEYMANN, Jürgen , ZIERKE, Thomas
发明人： BASF AKTIENGESELLSCHAFT
IPC分类号： C07K07/06
CPC分类号： A61K38/08
摘要： Novel peptides of the following formula (I): R R N-CHX-CO-A-B-D-E-(G)s-K in which R , R , A, B, D, E, G, K, X, and s have the meanings stated in the description, and the preparation thereof are described. The novel peptides have an antineoplastic effect.
摘要翻译：下式（I）的新肽：R 1 R 2 N-CHX-CO-ABDE-（G）sK，其中R 1，R 2，A，B，D，E， G，K，X和S具有说明书中所述的含义，并描述其制备。新型肽具有抗肿瘤作用。

5. 发明申请

WO1997021726A1 AGENTS FOR PROMOTING BONE FORMATION 审中-公开
标题翻译：促进骨形成的药剂
公开(公告)号：WO1997021726A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996005380
申请日：1996-12-06
申请人： ROUSSEL UCLAF , KITAMURA, Kazuyuki , KOMIYAMA, Osamu , INAZU, Mizuho , BARON, Roland , GADEK, Thomas , KNOLLE, Jochen , STILZ, Han-Ulrich , WEHNER, Volkmar , MCDOWELL, Robert, S.
发明人： ROUSSEL UCLAF
IPC分类号： C07K07/06
CPC分类号： C07K5/0821 , A61K38/04 , A61K38/05 , A61K38/07 , A61K38/12 , A61K38/1703 , A61K38/39 , C07C271/22 , C07C279/08 , C07C279/20 , C07K5/0202 , C07K5/0817 , C07K5/1019 , C07K5/1024 , C07K14/46 , C07K14/745 , C07K14/78
摘要： The object is to provide a promoting agent for bone formation, a therapeutic method for bone formation and a process for preparing a promoting agent for bone formation. A promoting agent for bone formation which comprises at least one of kistrin, echstatin, a peptide or polypeptide containing the amino acid sequence ArgGlyAsp in the molecule such as a peptide represented by Gly-Arg-Gly-Asp-Ser or a compound represented by general formula (IX) and so on, as well as a biologically acceptable salt thereof, wherein R16 represents -N(R20)2 (R20 represents a hydrogen atom or a C1-C4 alkyl group), R17 represents a hydrogen atom or a C1-C4 alkyl group, R18 represents a hydrogen atom, a C1-C4 alkyl group and so on, R19 represents OH, NH2 and so on, Y represents -NH-, -O- or a direct bond, a represents 1-3, b represents 1 or 2, c represents 0 or 1 and d represents 0 or 1.
摘要翻译：本发明提供骨形成促进剂，骨形成治疗方法及骨形成促进剂的制备方法。用于骨形成的促进剂，其包含分子中含有氨基酸序列ArgGlyAsp的丝氨酸蛋白酶，抑制素，肽或多肽中的至少一种，例如由Gly-Arg-Gly-Asp-Ser表示的肽或由通式式（IX）等，以及其生物可接受的盐，其中R 16表示-N（R 20）2（R 20表示氢原子或C 1 -C 4烷基），R 17表示氢原子或C1- C4烷基，R18表示氢原子，C1-C4烷基等，R19表示OH，NH2等，Y表示-NH-，-O-或直接键，a表示1-3，b 表示1或2，c表示0或1，d表示0或1。

6. 发明申请

WO1997019103A1 NOVEL SYNTHETIC SUBSTRATE FOR ACTIVITY ASSAY HAVING CHROMOPHORE OR FLUOROCHROMOPHORE ACTIVE AGAINST HEPATITIS C VIRUS NS3 PROTEASE 审中-公开
标题翻译：用于活性测定的新型合成基质，具有染色体或荧光素活性对抗病原体C病毒NS3蛋白
公开(公告)号：WO1997019103A1
公开(公告)日：1997-05-29
申请号：PCT/JP1996003398
申请日：1996-11-20
申请人： RATIONAL DRUG DESIGN LABORATORIES , SHIMIZU, Yasuaki , YAMAJI, Kayo , MASUHO, Yasuhiko , SHIMOTOHNO, Kunitada
发明人： RATIONAL DRUG DESIGN LABORATORIES
IPC分类号： C07K07/06
CPC分类号： C07K14/005 , C12N2770/24222
摘要： A synthetic substrate which contains a specific amino acid sequence, has a fluorochromophore or chromophore covalently bonded to the C-terminus, and carries at least one amino acid inhibiting the aminopeptidase digestion on the N-terminal side of the above sequence. The use of this substrate makes it possible to efficiently assay the activity of an NS3 protease. By effecting the assay in the presence of NS4A, the detection sensitivity can be further elevated.
摘要翻译：含有特定氨基酸序列的合成底物具有与C末端共价结合的氟发色团或发色团，并且在上述序列的N末端侧携带至少一种抑制氨基肽酶消化的氨基酸。使用该底物使得可以有效地测定NS3蛋白酶的活性。通过在NS4A存在下进行测定，可以进一步提高检测灵敏度。

7. 发明申请

WO1997018235A1 PEPTIDE CONJUGATES, USE THEREOF AS A DRUG, AND COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：作为药物使用的胶原蛋白，以及含有它们的组合物
公开(公告)号：WO1997018235A1
公开(公告)日：1997-05-22
申请号：PCT/FR1996001811
申请日：1996-11-15
申请人： SOCIETE D'ETUDE ET DE RECHERCHE DE PATHOLOGIE APPLIQUEE - SERPA , DUSSOURD D'HINTERLAND, Lucien , PINEL, Anne-Marie
发明人： SOCIETE D'ETUDE ET DE RECHERCHE DE PATHOLOGIE APPLIQUEE - SERPA
IPC分类号： C07K07/06
CPC分类号： A61K8/4986 , A61K8/36 , A61K8/64 , A61K38/00 , A61K2800/57 , A61Q19/00 , A61Q19/08 , C07K5/0819 , C07K5/1019 , C07K7/06
摘要： Peptide conjugates including a sequence of at least three amino acids selected from Lys-Lys-Gly, Gly-His-Lys and Glu-His-Lys, wherein "Lys" is Lysine or a halogenated derivative thereof, or a methylated Lysine derivative, particularly Methyl-Lysine and Dihydrobromo-Methyl-Lysine, said amino acids optionally being in D, L or DL form, and said sequence being chemically or physically conjugated with at least one compound selected from monocarboxylic acids of general formula (I): HOOC-R, or alcohol, aldehyde or amide derivatives thereof, and dicarboxylic acids of general formula (II): HOOC-R1-COOH, are disclosed. The use of such conjugates as a drug, and pharmaceutical or cosmetic compositions containing said conjugates, are also disclosed.
摘要翻译：包括选自Lys-Lys-Gly，Gly-His-Lys和Glu-His-Lys中的至少三个氨基酸的序列的肽缀合物，其中“Lys”是赖氨酸或其卤代衍生物，或甲基化赖氨酸衍生物，特别是甲基 - 赖氨酸和二氢溴 - 甲基 - 赖氨酸，所述氨基酸任选地为D，L或DL形式，所述序列与至少一种选自通式（I）的单羧酸的化合物或物理缀合：HOOC-R ，或其醇，醛或其酰胺衍生物和通式（II）的二羧酸：HOOC-R1-COOH。还公开了使用这种缀合物作为药物，以及含有所述缀合物的药物或化妆品组合物。

8. 发明申请

WO1996040752A1 NOVEL DOLASTATIN DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
标题翻译：新型DOLASTATIN衍生物，其制备和使用
公开(公告)号：WO1996040752A1
公开(公告)日：1996-12-19
申请号：PCT/EP1996002393
申请日：1996-06-03
申请人： BASF AKTIENGESELLSCHAFT , HAUPT, Andreas , EMLING, Franz , ROMERDAHL, Cynthia, A.
发明人： BASF AKTIENGESELLSCHAFT
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101
摘要： Novel dolasstatin derivatives of the formula (I): R R N-CHX-CO-A-B-D-E-(F)tK, in which R , R , A, B, D, E, F, K, X and t have the meanings stated in the description, and the preparation thereof are described. The novel substances have an antineoplastic effect.
摘要翻译：式（I）的新型多拉斯汀衍生物：R 1 R 2 N-CHX-CO-ABDE-（F）tK，其中R 1，R 2，A，B，D，E ，F，K，X和t具有说明书中所述的含义，并描述其制备。新物质具有抗肿瘤作用。

9. 发明申请

WO1996033213A1 METHOD FOR PREPARING STREPTOGRAMINES 审中-公开
标题翻译：制备STREPTOGRAMINES的方法
公开(公告)号：WO1996033213A1
公开(公告)日：1996-10-24
申请号：PCT/FR1996000575
申请日：1996-04-16
申请人： RHONE-POULENC RORER S.A. , BARRIERE, Jean-Claude , GRONDARD, Luc , LEFEVRE, Patrick , MUTTI, Stéphane
发明人： RHONE-POULENC RORER S.A.
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00
摘要： A method for preparing streptogramines of general formula (I), wherein R1 is methyl or ethyl, R2 is H and X and Y together form an oxo radical, or R1 is ethyl, R2 and X are H and Y is H or OH, or else R1 is ethyl, R2 is OH and X and Y together form an oxo radical, by demethylating a synergistin derivative of general formula (II), wherein R1, R2, X and Y are as defined above, by means of a treatment with a periodate in an acetic medium, followed by a treatment in an aqueous medium.
摘要翻译：一种制备通式（I）的链霉菌的方法，其中R1是甲基或乙基，R2是H，X和Y一起形成氧基，或R1是乙基，R2和X是H，Y是H或OH，或其中R 1为乙基，R 2为OH，X和Y一起形成氧基，通过将通式（II）的增效剂衍生物，其中R 1，R 2，X和Y如上定义，在乙酸介质中，然后在水性介质中进行处理。

10. 发明申请

WO1996031529A1 PEPTIDES AND REMEDY FOR AUTOIMMUNE DISEASES COMPRISING THE SAME 审中-公开
标题翻译：包括其的自身免疫性疾病的药物和补救措施
公开(公告)号：WO1996031529A1
公开(公告)日：1996-10-10
申请号：PCT/JP1996000917
申请日：1996-04-03
申请人： HOECHST JAPAN LIMITED , YAMAGATA, Nobuyuki , OGATA, Kenji , WAGATSUMA, Masako , TAKANASHI, Hitoshi
发明人： HOECHST JAPAN LIMITED
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00
摘要： Peptides having the following amino acid sequence, derivatives thereof and modifications of these: Ala-Xaa1-Leu-Xaa2-Phe-Xaa3-Xaa4-Xaa5-(Xaa6)n wherein Xaa1 and Xaa4 independently represent each an amino acid residue optionally having alkyl or heteroalkyl side chain(s) optionally substituted by hydroxy, amino or guanidyl; Xaa2 and Xaa6 independently represent each an amino acid residue optionally having alkyl or heteroalkyl side chain(s) optionally substituted by hydroxy; Xaa3 and Xaa5 independently represent each an amino acid residue optionally having hydrophobic side chain(s); and n is 0 or 1. The peptides and derivatives thereof are useful as medicinal compositions for preventing and treating autoimmune diseases, rejection reactions accompanying organ transplantation, inflammation, etc.
摘要翻译：具有以下氨基酸序列的肽，其衍生物及其修饰：Ala-Xaa1-Leu-Xaa2-Phe-Xaa3-Xaa4-Xaa5-（Xaa6）n其中Xaa1和Xaa4各自独立地表示任选具有烷基或任选被羟基，氨基或胍基取代的杂烷基侧链; Xaa2和Xaa6各自独立地表示任选具有任选被羟基取代的烷基或杂烷基侧链的氨基酸残基; Xaa3和Xaa5各自独立地表示任选具有疏水侧链的氨基酸残基; 并且n为0或1.肽及其衍生物可用作预防和治疗自身免疫性疾病，伴随器官移植排斥反应，炎症等的药物组合物。

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