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1. 发明申请

WO1998017678A1 ANTITHROMBOTIC AZACYCLOALKYLALKANOYL PEPTIDES AND PSEUDOPEPTIDES 审中-公开
标题翻译：抗生素亚卡吡啶基胆碱酯酶和抗病毒药物
公开(公告)号：WO1998017678A1
公开(公告)日：1998-04-30
申请号：PCT/US1997014578
申请日：1997-08-15
申请人： RHONE-POULENC RORER PHARMACEUTICALS INC. , KLEIN, Scott, I. , MOLINO, Bruce, F. , CZEKAJ, Mark , GARDNER, Charles, J.
发明人： RHONE-POULENC RORER PHARMACEUTICALS INC.
IPC分类号： C07K05/08
CPC分类号： C07K5/06113 , A61K38/00 , C07K5/0806 , Y02P20/55
摘要： The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-[N-[N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl]-(L)-aspartyl]-(L)- beta -cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes and intermediates for preparing a compound of formula (II) wherein: A, B, Z, E , E , G, R, m, n and p are as defined herein.
摘要翻译：本发明涉及抗血栓形成的化合物N- [N- [N-（4-哌啶-4-基）丁酰基）-N-乙基甘氨酰] - （L） - 天门冬酰基] - （L ） - β-环己基 - 丙氨酸酰胺，制备所述稳定结晶形式的方法，其制备方法及其中间体，本发明还涉及制备式（II）化合物的方法和中间体，其中：A ，B，Z，E 1，E 2，G，R，m，n和p如本文所定义。

2. 发明申请

WO1997049723A1 CATIONIC LIPIDS FOR DELIVERY OF NUCLEIC ACID TO CELLS 审中-公开
标题翻译：用于向细胞输送核酸的阳离子脂肪
公开(公告)号：WO1997049723A1
公开(公告)日：1997-12-31
申请号：PCT/US1997011225
申请日：1997-06-26
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , LIN, Kuei-Ying , MATTEUCCI, Mark, D.
IPC分类号： C07K05/08
CPC分类号： C07D233/64 , A61K38/00 , C07K5/06026 , C07K5/06147 , C07K5/0806 , Y10T436/207497
摘要： The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two substituted histidine residues, or similar compounds, linked to a lipophilic moiety. The lipids form a complex when mixed with polyanions such as nucleic acids or peptides. The complexes permit efficient transfer of polyanions into cells, usually without significant toxicity to the cells.
摘要翻译：本发明涉及其合成中的新的阳离子脂质和中间体，其可用于将核酸或肽转染到原核或真核细胞中。脂质包含与亲油部分连接的一个或两个取代的组氨酸残基或类似化合物。当与聚阴离子例如核酸或肽混合时，脂质形成复合物。复合物允许聚阴离子有效转移到细胞中，通常对细胞没有显着的毒性。

3. 发明申请

WO1995033763A1 NOVEL ELASTASE INHIBITORS 审中-公开
标题翻译：新型ELASTASE抑制剂
公开(公告)号：WO1995033763A1
公开(公告)日：1995-12-14
申请号：PCT/US1995005618
申请日：1995-05-05
申请人： HOECHST MARION ROUSSEL, INC. , METZ, William, A., Jr. , GALLION, Steven, L. , BURKHART, Joseph, P. , ANGELASTRO, Michael, R. , PEET, Norton, P.
发明人： HOECHST MARION ROUSSEL, INC.
IPC分类号： C07K05/08
CPC分类号： C07K5/06191 , A61K38/00
摘要： This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase. The inhibitors are short, synthetic peptides in which the P2 moiety is substituted with various nitrogen-containing heterocyclic groups. As inhibitors of human neutrophil elastase, the compounds are useful in the treatment of a patient afflicted with a neutrophil associated inflammatory disease.
摘要翻译：本发明涉及作为弹性蛋白酶抑制剂，特别是人嗜中性粒细胞弹性蛋白酶的化合物。抑制剂是其中P2部分被各种含氮杂环基团取代的短合成肽。作为人嗜中性粒细胞弹性蛋白酶抑制剂，该化合物可用于治疗患有嗜中性粒细胞相关性炎性疾病的患者。

4. 发明申请

WO1995029189A1 FACTOR Xa INHIBITORS 审中-公开
标题翻译：因子Xa抑制剂
公开(公告)号：WO1995029189A1
公开(公告)日：1995-11-02
申请号：PCT/US1995005268
申请日：1995-04-25
申请人： SELECTIDE CORPORATION
发明人： SELECTIDE CORPORATION , AL-OBEIDI, Fahad , LEBL, Michal , OSTREM, James, A. , SAFAR, Pavel , STIERANDOVA, Alena , STROP, Peter , WALSER, Armin
IPC分类号： C07K05/08
CPC分类号： C07K7/06 , A61K38/00 , C07K5/0207 , C07K5/06034 , C07K5/06078 , C07K5/06086 , C07K5/0806 , C07K5/0812 , C07K5/0815 , C07K5/0821 , C07K5/101 , C07K5/1016 , C07K7/64 , C07K14/811 , C12Q1/56 , Y02P20/55
摘要： The invention provides compounds which specifically inhibit factor Xa activity. The compounds consist of the structure X1-YIR-X2, wherein X1 is H, acyl, alkyl, acylalkyl, arylalkyl or one or more amino acids, and X2 is a modified C-terminal group, one or more carboxy-protecting groups or one or more amino acids or other substituent, and Y, I and R are tyrosine, isoleucine and arginine, respectively, or peptidomimetic or organic structures that possess the same functional activity as Y, I and R, respectively. In addition, the present invention provides a compound having the structure A1-A2-(A3)m-B, where m is 0 or 1. A compound of the invention can be linear or cyclic and can be about 2 and 43 residues in length. A compound of the invention is characterized, in part, in that it exhibits a specific inhibition of factor Xa activity with a Ki of
摘要翻译：本发明提供特异性抑制因子Xa活性的化合物。化合物由结构X1-YIR-X2组成，其中X1是H，酰基，烷基，酰基烷基，芳烷基或一个或多个氨基酸，X2是修饰的C端基，一个或多个羧基保护基或一个或更多的氨基酸或其他取代基，Y，I和R分别是酪氨酸，异亮氨酸和精氨酸，或分别具有与Y，I和R相同功能活性的拟肽或有机结构。此外，本发明提供具有结构A1-A2-（A3）m-B的化合物，其中m为0或1.本发明的化合物可以是直链或环状的，并且其长度可以为约2和43个残基。本发明的化合物的特征在于其部分表现出具有Ki =100μM，优选

5. 发明申请

WO1987002674A1 ANALOGS OF ATRIAL NATRIURETIC PEPTIDES 审中-公开
标题翻译： ATRIAL NATRIURETIC PEPTIDES的模拟
公开(公告)号：WO1987002674A1
公开(公告)日：1987-05-07
申请号：PCT/US1986002362
申请日：1986-11-03
申请人： BIOTECHNOLOGY RESEARCH ASSOCIATES, J.V.
发明人： BIOTECHNOLOGY RESEARCH ASSOCIATES, J.V. , LEWICKI, John, A. , SCARBOROUGH, Robert, M., Jr. , JOHNSON, Lorin, K.
IPC分类号： C07K05/08
CPC分类号： C07K14/58 , A61K38/00
摘要： Compounds and compositions comprising synthetic analogs of Atrial Natriuretic Peptides, together with methods for their production and use as natriuretics, diuretics and/or vasodilators, or as intermediates for or modulators of such useful compounds or of native Atrial Natriuretic Peptides.
摘要翻译：包含心房钠尿肽合成类似物的化合物和组合物，以及其生产和用作利尿剂，利尿剂和/或血管扩张剂的方法，或作为这些有用化合物或天然心房钠尿肽的中间体或调节剂。

6. 发明申请

WO1996040747A1 UROKINASE RECEPTOR LIGANDS 审中-公开
标题翻译：尿激酶受体配体
公开(公告)号：WO1996040747A1
公开(公告)日：1996-12-19
申请号：PCT/US1996009648
申请日：1996-06-06
申请人： CHIRON CORPORATION , ROSENBERG, Steve , SPEAR, Kerry, L. , MARTIN, Eric, J.
发明人： CHIRON CORPORATION
IPC分类号： C07K05/08
CPC分类号： C07K5/0806 , A61K38/00 , Y02A50/395
摘要： Compounds of the invention inhibit urokinase plasminogen activator or uPAR, represented by general formula (I), where R10 is -CH(R9)XCH(R1)(R11) or a capping group, where X is NR12, CR12R15, O, S, SR12, or SR12R15; R1, R9, R11, R12, R15 are each H, lower alkyl, lower alkenyl, lower alkynyl, aryl, aralkyl, aryl-alkenyl, aryl-alkynyl, aryl-cycloalkyl, substituted with 0-3 halo, OH, NH2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, CN or NO2; R16 is -CH(R5)C(=O)NH2, H, lower alkyl, cycloalkyl, or lower alkenyl; R2 is aryl or aralkyl, unsubstituted or substituted with 1-3 halo, OH, NH2, CN, NO2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, or cycloalkyl; R3 and R5 are each independently H or lower alkyl; R4 is -CH2C(=O)NR13R14, where R13 is H, lower alkyl, phenyl or benzyl, and R14 is H, aryl, or aralkyl, where R6 and R7 are each independently H, OH, NH2, CN, NO2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, or cycloalkyl, and n and m are each independently an integer from 1 to 3; and pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明的化合物抑制由通式（I）表示的尿激酶纤溶酶原激活物或uPAR，其中R10是-CH（R9）XCH（R1）（R11）或封端基团，其中X是NR12，CR12R15，O，S， SR12或SR12R15; R1，R9，R11，R12，R15各自为H，低级烷基，低级烯基，低级炔基，芳基，芳烷基，芳基 - 烯基，芳基 - 炔基，芳基 - 环烷基，被0-3卤代，OH，NH2，低级烷基，卤代低级烷基，低级烷氧基，低级烷基氨基，低级烷硫基，CN或NO 2; R 16是-CH（R 5）C（= O）NH 2，H，低级烷基，环烷基或低级烯基; R 2是未取代或被1-3个卤素，OH，NH 2，CN，NO 2，低级烷基，卤代低级烷基，低级烷氧基，低级烷基氨基，低级烷硫基或环烷基取代的芳基或芳烷基。 R3和R5各自独立地为H或低级烷基; R4是-CH2C（= O）NR13R14，其中R13是H，低级烷基，苯基或苄基，R14是H，芳基或芳烷基，其中R6和R7各自独立地是H，OH，NH2，CN，NO2，低级烷基，卤代低级烷基，低级烷氧基，低级烷基氨基，低级烷硫基或环烷基，n和m各自独立地为1至3的整数; 及其药学上可接受的酸加成盐。

7. 发明申请

WO1996003427A1 PEPTIDE DERIVED RADIONUCLIDE CHELATORS 审中-公开
标题翻译：肽衍生的放射性核素螯合剂
公开(公告)号：WO1996003427A1
公开(公告)日：1996-02-08
申请号：PCT/CA1995000249
申请日：1995-04-28
申请人： RESOLUTION PHARMACEUTICALS INC. , POLLAK, Alfred , GOODBODY, Anne
发明人： RESOLUTION PHARMACEUTICALS INC.
IPC分类号： C07K05/08
CPC分类号： C07K5/0827 , A61K51/0478 , A61K51/088 , A61K2123/00 , Y02P20/55
摘要： For use in imaging sites of diagnostic interest within the body, the present invention provides radionuclide chelators of formula (I), wherein X is a linear or branched, saturated or unsaturated C1-4alkyl chain that is optionally interrupted by one or two heteroatoms selected from N, O and S; and is optionally substituted by at least one group selected from halogen, hydroxyl, amino, carboxyl, C1-4alkyl, aryl and C(O)Z; Y is H or a substituent defined by X; X and Y may together form a 5- to 8-membered saturated or unsaturated heterocyclic ring optionally substituted by at least one group selected from halogen, hydroxyl, amino, carboxyl, oxo, C1-4alkyl, aryl and C(O)Z; R through R are selected independently from H; carboxyl; C1-4alkyl; C1-4alkyl substituted with a group selected from hydroxyl, amino, sulfhydryl, halogen, carboxyl, C1-4alkoxycarbonyl and aminocarbonyl; an alpha carbon side chain of a D- or L-amino acid other than proline; and C(O)Z; R and R are selected independently from H; carboxyl; amino; C1-4alkyl; C1-4alkyl substituted by hydroxyl, carboxyl or amino; and C(O)Z; R is selected from H and a sulfur protecting group; and Z is selected from hydroxyl, C1-4alkoxy and a targeting molecule.
摘要翻译：本发明提供式（I）的放射性核素螯合剂，其中X是直链或支链的饱和或不饱和C 1-4烷基链，其任选被一个或两个选自以下的杂原子中断： N，O和S; 并且任选被至少一个选自卤素，羟基，氨基，羧基，C 1-4烷基，芳基和C（O）Z的基团取代; Y是H或由X定义的取代基; X和Y可以一起形成任选被至少一个选自卤素，羟基，氨基，羧基，氧代，C 1-4烷基，芳基和C（O）Z中的基团取代的5至8元饱和或不饱和杂环; R 1至R 4独立地选自H; 羧基; C 1-4烷基; 被选自羟基，氨基，巯基，卤素，羧基，C 1-4烷氧基羰基和氨基羰基取代的C 1-4烷基; 除脯氨酸以外的D-或L-氨基酸的α碳侧链; 和C（O）Z; R 5和R 6独立地选自H; 羧基; 氨基; C 1-4烷基; 被羟基，羧基或氨基取代的C 1-4烷基; 和C（O）Z; R 7选自H和硫保护基; Z选自羟基，C 1-4烷氧基和靶向分子。

8. 发明申请

WO1994024153A1 CYCLIC COMPOUNDS AND COMPOSITIONS WHICH INHIBIT BONE RESORPTION 审中-公开
标题翻译：循环化合物和抑制骨质疏松的组合物
公开(公告)号：WO1994024153A1
公开(公告)日：1994-10-27
申请号：PCT/EP1994000977
申请日：1994-03-28
申请人： CIBA-GEIGY AG , RINK, Hans , ALTMANN, Eva , BLOMMERS, Marcel , MÜLLER, Klaus , HALL, Tony
发明人： CIBA-GEIGY AG
IPC分类号： C07K05/08
CPC分类号： C07K7/06 , C07K5/101 , C07K5/1013 , C07K14/635
摘要： Described are new cyclic compounds that inhibit excess bone resorption and methods for the production of said compounds. Described are also compositions containing said compounds associated with pharmaceutical suitable carriers and methods for the treatment of diseases characterized by excess bone resorption, which method comprises administering to a subject in need of such treatment a bone resorption inhibitory effective amount of any of the novel cyclic compounds or a mixture of said compounds, optionally together with a pharmaceutical suitable carrier.
摘要翻译：描述了抑制过量骨吸收的新的环状化合物和用于生产所述化合物的方法。还描述了含有与药物合适的载体相关的所述化合物的组合物和用于治疗以过量骨吸收为特征的疾病的方法，该方法包括向需要这种治疗的受试者施用骨吸收抑制有效量的任何新型环状化合物或所述化合物的混合物，任选地与药物合适的载体一起。

9. 发明申请

WO1994014838A1 ANTIBIOTICS GE 37468 A, B AND C 审中-公开
标题翻译：抗生素GE 37468 A，B和C
公开(公告)号：WO1994014838A1
公开(公告)日：1994-07-07
申请号：PCT/EP1993003541
申请日：1993-12-15
申请人： GRUPPO LEPETIT S.P.A. , STELLA, Sergio , MONTANINI, Nicoletta , LE MONNIER, Francis, John , COLOMBO, Luigi , SELVA, Enrico , DENARO, Maurizio
发明人： GRUPPO LEPETIT S.P.A.
IPC分类号： C07K05/08
CPC分类号： C07K5/0821 , A23K20/195 , A61K38/00 , C07K5/06139 , C12R1/465
摘要： The present invention is directed to new antibiotic substances denominated antibiotics GE 37468 A (I), B and C, their addition salts with bases, the pharmaceutical compositions thereof and their use as medicaments, particularly in the treatment of infectious diseases involving microorganisms susceptible to them. The compounds of the invention are also active as growth promotant agents in animals, such as poultry, swine, ruminants, etc.
摘要翻译：本发明涉及新的抗生素物质，称为抗生素GE 37468A（I），B和C，它们与碱的加成盐，其药物组合物及其作为药物的用途，特别是用于治疗涉及对其敏感的微生物的感染性疾病。本发明的化合物在动物如动物，如家禽，猪，反刍动物等中也是有活性的。

10. 发明申请

WO1987005608A1 NOVEL PEPTIDE DERIVATIVES 审中-公开
标题翻译：新肽衍生物
公开(公告)号：WO1987005608A1
公开(公告)日：1987-09-24
申请号：PCT/SE1987000141
申请日：1987-03-19
申请人： KABIVITRUM AB
发明人： KABIVITRUM AB , ARIELLY, Salo , GUSTAVSSON, Stig, Ake, Ingemar
IPC分类号： C07K05/08
CPC分类号： C07K5/06026 , C07K5/0817
摘要： Tripeptide derivatives, characterized by general formula: R1 - X - D-Arg - A - Arg - NH - R2 wherein R1 is hydrogen, alpha - or beta -naphtyl residue, lower alkyl residue which may be substituted with a carboxyl group, unsubstituted or substituted phenyl- or phenylalkyl residue. X is (I), (II), (III) or a single bond with the proviso that when R1 is hydrogen then and only then X is a single bond; A = Gly or Sar; R2 = an aromatic or heterocyclic residue which gives a compound R2-NH2 by enzymatic hydrolysis, which can be determined quantitatively; or disalts and trisalts of inorganic or organic acids thereof, process for their preparation and method for determination of serine proteases, especially Factor Xa; or components which can interact with serine proteases or zymogen forms thereof.
摘要翻译：以通式表示的三肽衍生物：R1-X-D-Arg-A-Arg-NH-R2其中R1是氢，α-或β-萘基残基，可被羧基取代的低级烷基残基，未取代或未取代的取代的苯基或苯基烷基残基。 X是（I），（II），（III）或单键，条件是当R1是氢时，只有X是单键; A = Gly或Sar; R2 =通过酶水解得到化合物R2-NH2的芳族或杂环残基，其可以定量测定; 或其无机或有机酸的三卤化物，其制备方法和丝氨酸蛋白酶，特别是因子Xa的测定方法; 或可与丝氨酸蛋白酶或其酶原形式相互作用的组分。

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