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1. 发明授权

US5654451B1 Amino acids and peptides having modified c-terminals and modified n-terminals 失效
标题翻译：氨基酸和肽具有修饰的c-末端和修饰的n末端
公开(公告)号：US5654451B1
公开(公告)日：2000-02-22
申请号：US43046295
申请日：1995-04-28
申请人： MAGAININ PHARMA
发明人： KARI U PRASAD
IPC分类号： C07C237/20 , C07C279/14 , C07C279/36 , C07C233/05
CPC分类号： C07C279/14 , C07C237/20 , C07C279/36

2. 发明申请

WO0066708A9 ASTHMA ASSOCIATED FACTORS AS TARGETS FOR TREATING ATOPIC ALLERGIES INCLUDING ASTHMA AND RELATED DISORDERS 审中-公开
标题翻译：哮喘相关因素作为治疗特应性包括哮喘和相关疾病的目标
公开(公告)号：WO0066708A9
公开(公告)日：2001-06-28
申请号：PCT/US0011712
申请日：2000-05-01
申请人： MAGAININ PHARMA , LOUAHED JAMILA , DONG CHARLES QU , LEVITT ROY C , MALOY W LEE , ZHOU YUHONG , NICOLAIDES NICHOLAS C
发明人： LOUAHED JAMILA , DONG CHARLES QU , LEVITT ROY C , MALOY W LEE , ZHOU YUHONG , NICOLAIDES NICHOLAS C
IPC分类号： G01N33/53 , A61K31/56 , A61K31/7088 , A61K38/00 , A61K38/16 , A61K39/395 , A61K45/00 , A61K48/00 , A61P1/04 , A61P11/06 , A61P37/02 , A61P37/08 , C07K14/435 , C07K14/47 , C07K16/18 , C07K16/24 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/70 , C12N15/74 , C12N15/79 , C12P21/02 , C12P21/08 , C12Q1/02 , C12Q1/68 , C12R1/91 , C12N15/12
CPC分类号： C07K16/24 , A61K38/00 , A61K2039/505 , C07K14/47
摘要： A novel TH2 associated gene that is induced by IL-9 has been identified and isolated, thereby providing a therapeutic target for IL-9 mediated diseases such as atopic allergy and asthma-related disorders. The invention also includes methods for the identification and use of small molecule inhibitors of this gene and its products to treat these disorders, methods for diagnosing susceptibility to, and assessing treatment of atopic allergy or asthma-related disorders by measuring the level of gene expression in biologic samples using antibody specific for this protein. The use of this protein as a therapeutic agent for the treatment of autoimmune diseases is also indicated.
摘要翻译：已经鉴定和分离了由IL-9诱导的新型TH2相关基因，从而为IL-9介导的疾病如特应性变态反应和哮喘相关疾病提供了治疗靶点。本发明还包括用于鉴定和使用该基因的小分子抑制剂及其产品来治疗这些病症的方法，通过测量在特应性变态反应或哮喘相关病症中的基因表达水平来诊断易感性和评估特应性变态反应或哮喘相关病症的方法使用对该蛋白特异的抗体进行生物学样品。还指出了使用这种蛋白质作为治疗自身免疫性疾病的治疗剂。

3. 发明申请

WO9965931A9 NON-ENZYMATIC CHEMICAL AMIDATION PROCESS 审中-公开
标题翻译：非化学化学吸附过程
公开(公告)号：WO9965931A9
公开(公告)日：2000-03-23
申请号：PCT/US9913626
申请日：1999-06-17
申请人： MAGAININ PHARMA , JONES STEPHEN R , NOECKER LINCOLN A , FEIBUSH BINYAMIN
发明人： JONES STEPHEN R , NOECKER LINCOLN A , FEIBUSH BINYAMIN
IPC分类号： C07K1/12 , C07K14/47 , C07K2/00 , C07K14/00 , C12P21/06
CPC分类号： C07K14/4723 , C07K1/124
摘要： A simple non-enzymatic method of preparing a peptide C-terminal amide is described. Such method may be applied to a variety of peptide C-terminal carboxylic acid ester substrates. A simple non-enzymatic method of preparing a peptide C-terminal amide from a fusion peptide C-terminal carboxylic acid ester is also described. Peptide C-terminal amides may be used to prepare various pharmaceutical compositions.
摘要翻译：描述了制备肽C-末端酰胺的简单非酶法。这种方法可以应用于多种肽C末端羧酸酯底物。还描述了从融合肽C-端羧酸酯制备肽C-末端酰胺的简单非酶法。肽C末端酰胺可用于制备各种药物组合物。

4. 发明申请

WO9824904A3 IL-9 RECEPTOR VARIANTS, USEFUL IN TREATING AND DIAGNOSING ATOPIC ALLERGIES INCLUDING ASTHMA AND RELATED DISORDERS 审中-公开
标题翻译： IL-9受体变异体，有助于治疗和诊断包括哮喘和相关疾病的特应性过敏症
公开(公告)号：WO9824904A3
公开(公告)日：1998-11-05
申请号：PCT/US9721992
申请日：1997-12-02
申请人： MAGAININ PHARMA
发明人： LEVITT ROY CLIFFORD , GRASSO LUIGI , NICOLAIDES NICHOLAS C , HOLROYD KENNETH J
IPC分类号： C12N15/09 , A61K38/00 , A61K38/17 , A61P11/06 , C07K14/715 , C12N5/10 , C12N15/11 , C12N15/12 , C12Q1/68 , G01N33/566 , G01N33/68
CPC分类号： C12Q1/6883 , A61K38/00 , C07K14/7155 , C12Q2600/156
摘要： This invention relates to the diagnosis, treatment and methods for discovery of new therapeutics for atopic asthma and related disorders based on variants of Asthma Associated Factor (2). One embodiment of the invention is a variant of AAF2, wherein codon 173 is deleted resulting in the loss of glutamine 173 from the mature protein precursor. This single amino acid deletion results in a non-functional AAF2 protein and therefore the presence of this phenotype should be associated with less evidence of atopic asthma. Correspondingly, the lack of susceptibility to an asthmatic, atopic phenotype is characterized by the loss of glutamine at codon 173. The invention includes isolated DNA molecules which are variants of the wild type sequence as well as the proteins encoded by such DNA and the use of such DNA molecules and expressed protein in the diagnosis and treatment of atopic asthma.

5. 发明申请

WO9604373A2 RECOMBINANT PRODUCTION OF BIOLOGICALLY ACTIVE PEPTIDES AND PROTEINS 审中-公开
标题翻译：生物活性肽和蛋白质的重组生产
公开(公告)号：WO9604373A2
公开(公告)日：1996-02-15
申请号：PCT/US9510219
申请日：1995-07-26
申请人： MAGAININ PHARMA
发明人： WILLIAMS JON I , PIERCE JAMES C , ANDERSON G MARK , KARI PRASAD
IPC分类号： C07K14/435 , C07K14/46 , C12N15/62 , C12N15/67 , C12N15/70 , C12N15/10 , C07K1/14 , C07K14/00 , C12N21/10
CPC分类号： C07K14/435 , C07K14/46 , C07K2319/23 , C12N15/62 , C12N15/67 , C12N15/70
摘要： The present invention relates to the recombinant production of amphiphilic peptides with biologically and therapeutically significant activities. In one embodiment, this invention relates to recombinantly producing an amphiphilic peptide by providing a protease-deficient microbial host transformed with an expression vector containing DNA that encodes the amphiphilic peptide under the control of a regulatory sequence operable in the microbial host and expressing the amphiphilic peptide in the tranformed microbial host. In another embodiment, this invention relates to providing an E. coli protease-deficient K-12 cell transformed with a vector that expresses a cleavable fusion protein comprising at least part of a carbohydrate binding protein and the amphiphilic peptide in the cell, expressing the fusion protein in the cell, and cleaving the fusion protein to obtain the amphiphilic peptide substantially free of carbohydrate binding protein residues. The biologically active amphiphilic peptide so produced can be further treated chemically or enzymatically to obtain a chemically distinct amphiphilic peptide with improved biological and therapeutic properties.
摘要翻译：本发明涉及具有生物学和治疗学重要活性的两亲肽的重组生产。在一个实施方案中，本发明涉及通过提供用含有编码两亲肽的表达载体转化的蛋白酶缺陷型微生物宿主来重组产生两亲性肽，所述表达载体在可在微生物宿主中操作的调节序列的控制下并表达两亲肽在转化的微生物宿主中。在另一个实施方案中，本发明涉及提供用表达可切割融合蛋白的载体转化的大肠杆菌蛋白酶缺陷型K-12细胞，所述载体包含至少部分碳水化合物结合蛋白和细胞中的两亲肽，表达融合蛋白质，并切割融合蛋白以获得基本上不含碳水化合物结合蛋白质残基的两亲肽。如此生产的生物活性两亲肽可以进一步进行化学或酶学处理，以获得具有改善的生物学和治疗性质的化学不同的两亲性肽。

6. 发明申请

WO0009137A2 AMINOSTEROL COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：氨基甾醇化合物及其用途
公开(公告)号：WO0009137A2
公开(公告)日：2000-02-24
申请号：PCT/US9918322
申请日：1999-08-12
申请人： MAGAININ PHARMA , RAO MEENA , FEIBUSH BINYAMIN , KINNEY WILLIAM , ZASLOFF MICHAEL , NOECKER LINCOLN
发明人： RAO MEENA , FEIBUSH BINYAMIN , KINNEY WILLIAM , ZASLOFF MICHAEL , NOECKER LINCOLN
IPC分类号： A61K31/575 , A61P31/04 , C07J41/00
CPC分类号： A61K31/575
摘要： Newly isolated aminosterol compounds and pharmaceutical compositions based on the aminosterol compounds are described. Methods for the treatment of various disorders, for example, a microbial infection, are also described.
摘要翻译：描述了基于氨基甾醇化合物的新分离的氨基甾醇化合物和药物组合物。还描述了治疗各种病症的方法，例如微生物感染。

7. 发明申请

WO0066708A2 ASTHMA ASSOCIATED FACTORS AS TARGETS FOR TREATING ATOPIC ALLERGIES INCLUDING ASTHMA AND RELATED DISORDERS 审中-公开
标题翻译： ASTHMA相关因素作为治疗特发性过敏症的目标，包括哮喘和相关疾病
公开(公告)号：WO0066708A2
公开(公告)日：2000-11-09
申请号：PCT/US0011712
申请日：2000-05-01
申请人： MAGAININ PHARMA , LOUAHED JAMILA , DONG QU , LEVITT ROY C , MALOY W LEE , ZHOU YUHONG , NICOLAIDES NICHOLAS C
发明人： LOUAHED JAMILA , DONG QU , LEVITT ROY C , MALOY W LEE , ZHOU YUHONG , NICOLAIDES NICHOLAS C
IPC分类号： G01N33/53 , A61K31/56 , A61K31/7088 , A61K38/00 , A61K38/16 , A61K39/395 , A61K45/00 , A61K48/00 , A61P1/04 , A61P11/06 , A61P37/02 , A61P37/08 , C07K14/435 , C07K14/47 , C07K16/18 , C07K16/24 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/70 , C12N15/74 , C12N15/79 , C12P21/02 , C12P21/08 , C12Q1/02 , C12Q1/68 , C12R1/91 , C12N
CPC分类号： C07K16/24 , A61K38/00 , A61K2039/505 , C07K14/47
摘要： A novel TH2 associated gene that is induced by IL-9 has been identified and isolated, thereby providing a therapeutic target for IL-9 mediated diseases such as atopic allergy and asthma-related disorders. The invention also includes methods for the identification and use of small molecule inhibitors of this gene and its products to treat these disorders, methods for diagnosing susceptibility to, and assessing treatment of atopic allergy or asthma-related disorders by measuring the level of gene expression in biologic samples using antibody specific for this protein. The use of this protein as a therapeutic agent for the treatment of autoimmune diseases is also indicated.
摘要翻译：已经鉴定和分离了由IL-9诱导的新型TH2相关基因，从而为IL-9介导的疾病如特应性变态反应和哮喘相关疾病提供治疗靶标。本发明还包括用于鉴定和使用该基因的小分子抑制剂及其治疗这些疾病的产物的方法，通过测量基因表达水平来诊断特应性变态反应或哮喘相关病症的易感性和评估治疗方法使用此蛋白特异性抗体的生物样品。也表明使用该蛋白质作为治疗自身免疫疾病的治疗剂。

8. 发明申请

WO9949876A3 BACTERIAL OR YEAST EXTRACTS WHICH STIMULATE THE PRODUCTION OF DEFENSINS AND METHODS OF USE THEREOF 审中-公开
标题翻译：刺激防御剂生产的细菌或酵母提取物及其使用方法
公开(公告)号：WO9949876A3
公开(公告)日：1999-12-23
申请号：PCT/US9907071
申请日：1999-03-31
申请人： ABBOTT LAB , MAGAININ PHARMA
发明人： MUKERJI PRADIP , ANDERSON GLEN M , KROENING TERRY A , KIRCHNER STEPHEN J , ZASLOFF MICHAEL A , FEHLBAUM PASCALE
IPC分类号： A61K35/74 , A61K36/06 , A61K36/064 , A61K39/02 , A61K39/39 , C12N5/00 , C12Q1/68 , A61K35/72
CPC分类号： C12Q1/6897 , A61K35/745 , A61K35/747 , A61K36/06 , A61K36/064 , A61K39/39 , A61K2039/55588 , A61K2039/55594 , C12Q1/6809 , A61K2300/00
摘要： The subject invention relates to extracts derived from, for example, a spent medium, a portion of a bacterial cell, a lysed yeast cell, or a portion of a lysed yeast cell which may be used to stimulate the production of defensins in eukaryotic cells such as, for example, mammalian cells. Furthermore, the present invention includes compositions containing these extracts as well as methods of using these extracts, for example, in the prevention and treatment of various disease states, in rehydration, and in the stimulation of the immune system.
摘要翻译：本发明涉及衍生自例如废培养基，细菌细胞的一部分，裂解酵母细胞或裂解酵母细胞的一部分的提取物，其可用于刺激真核细胞中防御素的产生，例如例如，哺乳动物细胞。此外，本发明包括含有这些提取物的组合物，以及使用这些提取物的方法，例如在预防和治疗各种疾病状态，再水化和免疫系统的刺激中。

9. 发明申请

WO9914242A3 ASTHMA ASSOCIATED FACTORS AS TARGETS FOR TREATING ATOPIC ALLERGIES INCLUDING ASTHMA AND RELATED DISORDERS 审中-公开
标题翻译：哮喘相关因素作为治疗特应性包括哮喘和相关疾病的目标
公开(公告)号：WO9914242A3
公开(公告)日：1999-06-03
申请号：PCT/US9819626
申请日：1998-09-18
申请人： MAGAININ PHARMA , LUDWIG INST CANCER RES
发明人： RENAULD JEAN-CHRISTOPHE , LOUAHED JAMILA , GRASSO LUIGI , LEVITT ROY , NICOLAIDES NICHOLAS
IPC分类号： G01N33/53 , A61K31/336 , A61K31/351 , A61K31/366 , A61K31/575 , A61K38/00 , A61K45/00 , A61P11/08 , A61P35/00 , A61P35/02 , A61P37/08 , A61P43/00 , C07K14/47 , C07K14/82 , C07K16/32 , C12N15/09 , C12N15/12 , C12P21/02 , C12P21/08 , C12Q1/02 , G01N33/574 , A61K38/17 , C12N15/11 , C12Q1/68
CPC分类号： C07K14/4718 , A61K38/00 , G01N33/57484
摘要： A new gene in the Ras family that is induced by IL-9, thereby providing a therapeutic target in IL-9 mediated development of atopic allergy, asthma-related disorders and certain lymphomas or leukemias. A method for the identification and use of small molecule inhibitors of Ras to treat these disorders. A method for diagnosing susceptibility to, and assessing treatment of atopic allergy, asthma-related disorders and certain lymphomas and leukemias by measuring the level of Ras in biologic samples using antibody specific for the Ras protein.
摘要翻译： Ras家族中由IL-9诱导的新基因，从而提供IL-9介导的异位过敏，哮喘相关疾病和某些淋巴瘤或白血病的发展的治疗靶点。一种鉴定和使用Ras小分子抑制剂治疗这些疾病的方法。通过使用对Ras蛋白特异的抗体测量生物样品中Ras水平来诊断对特应性变态反应，哮喘相关病症和某些淋巴瘤和白血病的易感性和评估治疗的方法。

10. 发明申请

WO9903488A3 BIOLOGICALLY ACTIVE PEPTIDES WITH REDUCED TOXICITY IN ANIMALS AND A METHOD FOR PREPARING SAME 审中-公开
标题翻译：动物中具有降低毒性的生物活性肽及其制备方法
公开(公告)号：WO9903488A3
公开(公告)日：1999-04-08
申请号：PCT/US9814610
申请日：1998-07-15
申请人： MAGAININ PHARMA
发明人： KARI U PRASAD , WILLIAMS TAFFY J , MCLANE MICHAEL
IPC分类号： A61K38/00 , A61P31/00 , A61P35/00 , C07K1/02 , C07K14/435 , C07K14/46 , C07K14/47 , A61K38/17 , A61K38/04 , C07K14/00
CPC分类号： C07K14/46 , A61K38/00 , C07K14/43563
摘要： The present invention relates to biologically active peptides with reduced toxicity and methods of preparing them. The peptides of the invention, which can be unsubstituted or N-terminal substituted have formula (I), wherein X is a biologically active amphiphilic ion channel-forming peptide or protein, T is a lipophilic moiety or hydrogen, and W is T or hydrogen. Preferably T is formula (II), wherein R is a hydrocarbon (alkyl or aromatic or alkylaromatic) having at least 2 and no more than 10 carbon atoms. T is preferably an octanoyl group. The peptides and proteins of the invention have improved antimicrobial and anti-tumor biological activity while exhibiting reduced toxicity. A preferred method of reducing toxicity involves the formation of related methane sulfonate derivatives or analogues. Additionally, the compounds of the invention may be used to treat sepsis, septic shock, and lung infections, such as those occuring in cystic fibrosis.
摘要翻译：本发明涉及毒性降低的生物活性肽及其制备方法。可以是未取代或N-末端取代的本发明的肽具有式（I），其中X是生物活性两亲离子通道形成肽或蛋白质，T是亲脂性部分或氢，W是T或氢。 T优选为式（II），其中R为具有至少2个且不超过10个碳原子的烃（烷基或芳族或烷基芳族）。 T优选为辛酰基。本发明的肽和蛋白质具有改善的抗微生物和抗肿瘤生物活性，同时显示降低的毒性。降低毒性的优选方法涉及形成相关的甲磺酸衍生物或类似物。此外，本发明的化合物可用于治疗败血症，败血性休克和肺部感染，例如发生在囊性纤维化中的那些。

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