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81. 发明申请

WO1992005189A1 ANALOGUES OF CYCLOLINOPEPTIDE A AND THE USE THEREOF 审中-公开
标题翻译：环磷酰胺A的类似物及其用途
公开(公告)号：WO1992005189A1
公开(公告)日：1992-04-02
申请号：PCT/SE1991000628
申请日：1991-09-18
申请人： FERRING AB , WIECZOREK, Zbigniew , SIEMION, Z., Ignacy , TROJNAR, Jerzy
发明人： FERRING AB
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00 , C07K7/64
摘要： New analogues of Cyclolinopeptide A having a cyclic formula derived from the sequence of Cyclolinopeptide A (I) which sequence is extended between any two amino acid residues with the cystine derivative residue (II) in which X is selected from -H and -OH, and Y is selected from (a) and -H, wherein the amino acid residues are of L- or D-configuration, are disclosed. The above analogues can be used as medicaments, especially as immunosuppressive agents. The use of the above analogues for the preparation of a medicament for immunosuppressive treatment and pharmaceutical preparations comprising said analogues are also disclosed. A mammal, including man, in need of immunosuppressive treatment can be treated with a medicament comprising a pharmacologically effective amount of the above analogues.
摘要翻译：具有衍生自环亚氨基肽A（I）的序列的环状配方的环亚氨基肽A的新类似物，该序列在任何两个氨基酸残基之间延伸至其中X选自-H和-OH的胱氨酸衍生物残基（II），以及 Y选自（a）和-H，其中氨基酸残基为L-或D-构型。上述类似物可以用作药物，特别是作为免疫抑制剂。还公开了上述类似物用于制备用于免疫抑制治疗的药物和包含所述类似物的药物制剂的用途。可以用包含药理学有效量的上述类似物的药物治疗需要免疫抑制治疗的哺乳动物，包括人，

82. 发明申请

WO1992002546A1 SYNTHETIC PEPTIDES THAT ANTAGONIZE NEUROKININ A, THEIR SALTS AND THEIR MANUFACTURING PROCESSES 审中-公开
标题翻译：合成神经调节素A，其销售及其制造工艺的合成肽
公开(公告)号：WO1992002546A1
公开(公告)日：1992-02-20
申请号：PCT/IT1991000067
申请日：1991-07-26
申请人： A. MENARINI INDUSTRIE FARMACEUTICHE RIUNITE ... , GIULIANI, Sandro , MAGGI, Carlo, Alberto , PATACCHINI, Riccardo , PESTELLINI, Vittorio , QUARTARA, Laura , ROVERO, Paolo
发明人： A. MENARINI INDUSTRIE FARMACEUTICHE RIUNITE ...
IPC分类号： C07K07/06
CPC分类号： C07K7/22 , A61K38/00
摘要： Linear and cyclic synthetic peptides with the formula: X-Asp-Tyr-DTrp-Val-DTrp-DTrp-Y (I) where Y=A-R; A is one of the following amino acids: Lys, Orn, Glu, Gln, Asp, Asn, His, Ala, beta Ala, Val, Leu, Nle, Ile, Gly, Pro, Trp, Ser, Thr; R=NH2 (C-terminal carboxamide); X=H (free N-terminal amino group) or A is one of the following amino acids: Arg, Lys, Orn, Glu, Gln, Asp, Asn, His, Ala, beta Ala, Val, Leu, Nle, Ile, Gly, Pro, Phe, Trp, DTrp, Tyr, Met, Ser, Thr; when R and X together constitute an amide bond that joins together the two ends of the peptide chain to give a cyclic peptide; and their pharmaceutically acceptable salts with organic and inorganic acids or bases. These compounds are competitive antagonists of neurokinin A and are highly selective for the NK-2 receptor.
摘要翻译：具有下式的X-Asp-Tyr-DTrp-Val-DTrp-DTrp-Y（I）的线性和环状合成肽，其中Y = A-R; A是以下氨基酸之一：Lys，Orn，Glu，Gln，Asp，Asn，His，Ala，βAla，Val，Leu，Nle，Ile，Gly，Pro，Trp，Ser，Thr; R = NH 2（C-末端羧酰胺）; X = H（游离N-末端氨基）或A是以下氨基酸之一：Arg，Lys，Orn，Glu，Gln，Asp，Asn，His，Ala，βAla，Val，Leu，Nle，Ile， Gly，Pro，Phe，Trp，DTrp，Tyr，Met，Ser，Thr; 当R和X一起构成将肽链的两端连接在一起以产生环肽的酰胺键时; 及其与有机和无机酸或碱的药学上可接受的盐。这些化合物是神经激肽A的竞争性拮抗剂，对NK-2受体具有高选择性。

83. 发明申请

WO1992002545A1 BOMBESIN ANTAGONISTS 审中-公开
公开(公告)号：WO1992002545A1
公开(公告)日：1992-02-20
申请号：PCT/GB1991001289
申请日：1991-07-30
申请人： THE WELLCOME FOUNDATION LIMITED , KULL, Frederick, Charles , LEBAN, Johann, Jakob
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07K07/06
CPC分类号： C07K7/086 , A61K38/00
摘要： The present invention provides a polypeptide of the formula (I): XX TrpX X X X X X NH2, wherein X is a group X Arg(or D-Arg)X X and X is des NH2Pro,TyrPro,des NH2TyrPro, Ada, Pro, D-Pro or is deleted; X is Gly, Ala, D-Ala or is deleted; X is Asn, Phe, D-Phe, or Phe or D-Phe substituted by one or more halo atoms; or X is a group A-(CH2)n-CO- in which A is a group containing 1 to 3 rings of which at least one ring is aromatic, each ring system being optionally substituted; and the alkylene group is optionally substituted by one to four groups selected from amino, hydroxy, C1-4 alkoxy and C1-4 alkyl optionally substituted by halo and n is 0 to 4; or X is cyclopentyl carbonyl substituted by a group X Arg(or D-Arg)X X as hereinbefore defined; X is His, ThiAla or is deleted; X is Ala, D-Ala, CPenc, D-tBuGly or Pro; X is Val or Val substituted by one or more halo atoms; X is Gly, Ala, D-Ala, Sarcosine, Pro, D-Pro or D-Phe; X is His or ThiAla; X is D-Pro psi , Pro psi , 2-pyrrolidinyl-3-hydroxypropionyl or D-Pro; X is Nle, Leu, Phe, Val, Mox, D-Phe, Phe, or D-Phe substituted by one or more halo atoms or naphthylAla or naphthyl D-Ala or a hydrophobic, substituted aromatic amino acid or aralkylamine or is deleted, and the pharmaceutically acceptable salts thereof. The polypeptides possess antagonist properties against bombesin-like peptides and are of value in the treatment of malignant disease.
摘要翻译：本发明提供式（I）的多肽：XX TrpX 2 X 3 X 5 X 6 X 7 NH 2，其中X是基团X' Arg（或D-Arg）X 9 X 10和X 8是脱NH 2 Pro，TyrPro，des NH 2 TyrPro，Ada，Pro，D-Pro或缺失; X 9是Gly，Ala，D-Ala或缺失; X 10是被一个或多个卤原子取代的Asn，Phe，D-Phe或Phe或D-Phe; 或X是A - （CH 2）n -CO-基团，其中A是含有1至3个环的基团，其中至少一个环是芳族的，每个环系可任选被取代; 并且亚烷基任选被一至四个选自氨基，羟基，C 1-4烷氧基和任选被卤素取代的C 1-4烷基取代，n为0至4; 或X是被如上所定义的基团X 8 Arg（或D-Arg）X 9 X 10取代的环戊基羰基; X <1>是His，ThiAla或被删除; X 2是Ala，D-Ala，CPenc，D-tBuGly或Pro; X 3是被一个或多个卤原子取代的Val或Val; X 4是Gly，Ala，D-Ala，肌氨酸，Pro，D-Pro或D-Phe; X 5是His或ThiAla; X 6是D-Pro psi，Pro psi，2-吡咯烷基-3-羟基丙酰基或D-Pro; X 7是被一个或多个卤素原子或萘基取代的Nle，Leu，Phe，Val，Mox，D-Phe，Phe或D-Phe或萘基D-Ala或疏水取代的芳族氨基酸或芳烷基胺或被删除，及其药学上可接受的盐。这些多肽具有针对铃蟾肽样肽的拮抗剂性质，并且在恶性疾病的治疗中是有价值的。

84. 发明申请

WO1991016340A1 METHODS AND COMPOSITIONS FOR THE IDENTIFICATION, CHARACTERIZATION AND INHIBITION OF FARNESYL PROTEIN TRANSFERASE 审中-公开
标题翻译：鉴定，表征和抑制农杆菌蛋白转移的方法和组合物
公开(公告)号：WO1991016340A1
公开(公告)日：1991-10-31
申请号：PCT/US1991002650
申请日：1991-04-18
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , BROWN, Michael, S. , GOLDSTEIN, Joseph, L. , REISS, Yuval
发明人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00 , C07K1/1077 , C07K5/1013 , C07K5/1016 , C07K5/1019 , C07K5/1024 , C07K7/02 , C07K14/82 , C12N9/1085 , Y10S435/815
摘要： Disclosed are methods and compositions for the identification, characterization and inhibition of farnesyl protein transferases, enzymes involved in the farnesylation of various cellular proteins, including cancer related ras proteins such as p21ras. One farnesyl protein transferase which is disclosed herein exhibits a molecular weight of between about 70,000 and about 100,000 upon gel exclusion chromatography. The enzyme appears to comprise one or two subunits of approximately 50 kDa each. Methods are disclosed for assay and purification of the enzyme, as well as procedures for using the purified enzyme in screening protocols for the identification of possible anticancer agents which inhibit the enzyme and thereby prevent expression of proteins such as p21ras. Also disclosed is a family of compounds which act either as false substrates for the enzyme or as pure inhibitors and can therefore be employed for inhibition of the enzyme. The most potent inhibitors are ones in which phenylalanine occurs at the third position of a tetrapeptide whose amino terminus is cysteine.

85. 发明申请

WO1991009053A1 PEPTIDE DERIVATIVE, PROCESS FOR THE PREPARATION THEREOF, PHARMACEUTICAL PREPARATION CONTAINING IT AND METHOD FOR TREATMENT OF GLAUCOMA 审中-公开
标题翻译：肽衍生物，其制备方法，含有其的药物制剂及其用于治疗GLAUCOMA的方法
公开(公告)号：WO1991009053A1
公开(公告)日：1991-06-27
申请号：PCT/DK1990000322
申请日：1990-12-07
申请人： CARLBIOTECH LTD. A/S , WIDMER, Fred , GAURI, Kailash, Kumar
发明人： CARLBIOTECH LTD. A/S
IPC分类号： C07K07/06
CPC分类号： C07K7/06 , A61K38/00 , C07K5/0819
摘要： Peptide derivatives of 3-5 optionally substituted amino acids, a process for preparing the peptides, a pharmaceutical composition containing at least one peptide derivative active against glaucoma and intraocular hypertension and a method for treating glaucoma and intraocular hypertension.
摘要翻译： 3-5任选取代的氨基酸的肽衍生物，制备肽的方法，含有至少一种对青光眼有效的肽衍生物和眼内高血压的药物组合物，以及治疗青光眼和眼内高血压的方法。

86. 发明申请

WO1991008224A1 IM PEPTIDES 审中-公开
公开(公告)号：WO1991008224A1
公开(公告)日：1991-06-13
申请号：PCT/AU1990000564
申请日：1990-11-23
申请人： THE COUNCIL OF THE QUEENSLAND INSTITUTE OF ... , SCULLEY, Tom, Brian , MOSS, Denis, James
发明人： THE COUNCIL OF THE QUEENSLAND INSTITUTE OF ...
IPC分类号： C07K07/06
CPC分类号： C07K14/005 , A61K39/00 , C12N2710/16222 , Y10S435/975 , Y10S436/812
摘要： The invention is directed to the diagnosis and treatment of herpes virus related diseases. By noting within the Epstein-Barr virus (EBV) open reading frames (ORFs) transcribed late in the viral cycle for which a translation product may or may not have been established, and synthesizing one or more polypeptides each of which includes at least one segment, each segment comprising at least part of the amino acid sequence identified in that ORF, a specific and reliable diagnostic test for, and treatment of, infectious mononucleosis and related diseases is possible. The preferred amino acid sequences for these segments include NSPKNG, KNGSNQ, SNQLVI, AHARDK, RDKAGA, VMAMIL, SEPRPR and PSRTPS. These sequences can be further combined to provide polypeptides with at least one segment comprising sequences selected from AHARDKAGAVMAMIL, ASLNSPKNGSNQLVI, ELESEPRPRPSRTPS, QAMKKIEDKVRKSVD, SRSRGREAKKVQISD, LIKASLRKDRKLYAE, VSFSKTRRAIRESRA, CNYSAGEEDDQYHAN, RPHRRPVSKRPTHKP, EITQEENRGEQRLGH, GALRARLDRPRPTAQ, NSPKNGSNQAHARDKSEPRPR, NSPKNGSNQRDKAGASEPRPR, NSPKNGSNQSEPRPRKNGSNQ, NSPKNGSNQLVISEPRPRPSRTPS, NSPKNGSNQLVIPSRTPS and NSPKNGSNQAHARDKAGASEPRPR.
摘要翻译：本发明涉及疱疹病毒相关疾病的诊断和治疗。通过在爱泼斯坦 - 巴尔病毒（EBV）内注意到翻译产物可能已经建立或可能不被建立的病毒循环的晚期转录的开放阅读框（ORFs），并合成一个或多个多肽，每个多肽包括至少一个片段，每个片段包含在该ORF中鉴定的氨基酸序列的至少一部分，感染性单核细胞增多症和相关疾病的具体可靠的诊断测试和治疗是有可能的。这些片段的优选氨基酸序列包括NSPKNG，KNGSNQ，SNQLVI，AHARDK，RDKAGA，VMAMIL，SEPRPR和PSRTPS。这些序列可以被进一步结合以提供多肽与至少一个区段包括从AHARDKAGAVMAMIL，ASLNSPKNGSNQLVI，ELESEPRPRPSRTPS，QAMKKIEDKVRKSVD，SRSRGREAKKVQISD，LIKASLRKDRKLYAE，VSFSKTRRAIRESRA，CNYSAGEEDDQYHAN，RPHRRPVSKRPTHKP，EITQEENRGEQRLGH，GALRARLDRPRPTAQ，NSPKNGSNQAHARDKSEPRPR，NSPKNGSNQRDKAGASEPRPR，NSPKNGSNQSEPRPRKNGSNQ，NSPKNGSNQLVISEPRPRPSRTPS，NSPKNGSNQLVIPSRTPS和选择的序列 NSPKNGSNQAHARDKAGASEPRPR。

87. 发明申请

WO1990014357A1 HER2 EXTRACELLULAR DOMAIN 审中-公开
标题翻译： HER2细胞外结构域
公开(公告)号：WO1990014357A1
公开(公告)日：1990-11-29
申请号：PCT/US1990002697
申请日：1990-05-18
申请人： GENENTECH, INC.
发明人： GENENTECH, INC. , HUDZIAK, Robert, Michael , SHEPARD, H., Michael , ULLRICH, Axel
IPC分类号： C07K07/06
CPC分类号： C07K14/71 , A61K39/00
摘要： An extracellular portion of the HER2 molecule, essentially free of transmembrane and cytoplasmic portions, which is antigenic in animals. Isolated DNA encoding the extracellular portion; an expression vector containing the isolated DNA; and a cell containing the expression vector. A process for producing the extracellular domain. A vaccine containing the extracellular domain.
摘要翻译： HER2分子的细胞外部分，基本上不含跨膜和细胞质部分，其在动物中是抗原性的。编码胞外部分的分离DNA; 含有分离的DNA的表达载体; 和含有表达载体的细胞。一种产生细胞外结构域的方法。含有细胞外结构域的疫苗。

88. 发明申请

WO1990011294A1 VACCINATION AND METHODS AGAINST DISEASES RESULTING FROM PATHOGENIC RESPONSES BY SPECIFIC T CELL POPULATIONS 审中-公开
标题翻译：针对特定细胞群体的病原性反应疾病的疫苗和方法
公开(公告)号：WO1990011294A1
公开(公告)日：1990-10-04
申请号：PCT/US1990001516
申请日：1990-03-21
申请人： THE IMMUNE RESPONSE CORPORATION
发明人： THE IMMUNE RESPONSE CORPORATION , HOWELL, Mark, D. , BROSTOFF, Steven, W. , CARLO, Dennis, J.
IPC分类号： C07K07/06
CPC分类号： C07K14/7051 , A61K39/00 , A61K2039/53 , G01N2800/102
摘要： The present invention provides vaccines and a means of vaccinating a mammal so as to prevent or control specific T cell mediated pathologies or to treat the unregulated replication of T cells. The vaccine is composed of a T cell receptor (TCR) or a fragment thereof corresponding to a TCR present on the surface of T cells mediating the pathology. The vaccine fragment can be a peptide corresponding to sequences of TCRs characteristic of the T cells mediating said pathology. Means of determining appropriate amino acid sequences for such vaccines are also provided. The vaccine is administered to the mammal in a manner that induces an immune response directed against the TCR of T cells mediating the pathology. This immune response down regulates or deletes the pathogenic T cells, thus ablating the disease pathogenesis. The invention additionally provides a specific beta -chain variable region of the T cell receptor, designated V beta 17, which is central to the pathogenesis of rheumatoid arthritis (RA). Also provided are means to detect, prevent and treat RA.
摘要翻译：本发明提供疫苗和疫苗接种哺乳动物的手段，以便预防或控制特定的T细胞介导的病理学或治疗T细胞的未调节复制。疫苗由T细胞受体（TCR）或其对应于存在于介导病理学的T细胞表面上的TCR的片段组成。疫苗片段可以是对应于介导所述病理学的T细胞特征的TCR序列的肽。还提供了确定此类疫苗适当氨基酸序列的方法。疫苗以诱导针对T细胞的TCR介导病理学的免疫应答的方式施用于哺乳动物。这种免疫应答下调调节或去除病原性T细胞，从而消除疾病的发病机制。本发明另外提供了称为Vβ17的T细胞受体的特异性β链可变区，其为类风湿性关节炎（RA）的发病机制的核心。还提供了检测，预防和治疗RA的手段。

89. 发明申请

WO1990006940A1 NEW TNF PEPTIDES 审中-公开
标题翻译：新的TNF肽
公开(公告)号：WO1990006940A1
公开(公告)日：1990-06-28
申请号：PCT/EP1989001467
申请日：1989-12-02
申请人： BASF AKTIENGESELLSCHAFT , BOEHM, Hans-Joachim , DAUM, Lothar , HAUPT, Andreas , SCHMIED, Bernhard , WALKER, Nigel , ZECHEL, Johann-Christian
发明人： BASF AKTIENGESELLSCHAFT
IPC分类号： C07K07/06
CPC分类号： C07K14/525 , A61K38/00
摘要： New peptides of formula X-A-B-Pro-E-Y, in which A, B, E, X and Y have the meanings given in the description, are useful therapeutic agents. A process for producing them is also described.
摘要翻译：本发明涉及具有式X-A-B-Pro-E-Y的新型肽及其制备方法，其中A，B，E，X和Y具有在说明书中给出的含义。这些新肽可用于治疗疾病。

90. 发明申请

WO1990003983A1 PEPTIDES AND ANTIBODIES THAT INHIBIT INTEGRIN-LIGAND BINDING 审中-公开
标题翻译：抑制INTEGRIN-LIGAND结合的肽和抗体
公开(公告)号：WO1990003983A1
公开(公告)日：1990-04-19
申请号：PCT/US1989004371
申请日：1989-10-03
申请人： SCRIPPS CLINIC AND RESEARCH FOUNDATION
发明人： SCRIPPS CLINIC AND RESEARCH FOUNDATION , PLOW, Edward, F. , D'SOUZA, Stanley, D. , GINSBERG, Mark, H.
IPC分类号： C07K07/06
CPC分类号： C07K14/70557 , A61K38/00 , C07K16/2848
摘要： Polypeptides which are derived from the Arg-Gly-Asp (RGD) binding portion of an Integrin beta subunit are disclosed as are their use for modulation of Integrin ligand binding. Anti-peptide antibodies, hybridomas secreting these antibodies, as well as methods of making and using such antibodies, and recombinant DNA molecules that define the structural gene coding for the polypeptides are also contemplated as within the scope of the present invention.

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