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    Synthetic inhibitors of mammalian collagenase
    1.
    发明授权
    Synthetic inhibitors of mammalian collagenase 失效
    哺乳动物胶原酶的合成抑制剂

    公开(公告)号：US5686422A

    公开(公告)日：1997-11-11

    申请号：US468491

    申请日：1995-06-06

    申请人： Robert D. Gray ,  Arno F. Spatola ,  Robert B. Miller ,  Frank R. Burns ,  Christopher Paterson

    发明人： Robert D. Gray ,  Arno F. Spatola ,  Robert B. Miller ,  Frank R. Burns ,  Christopher Paterson

    IPC分类号： A61K38/00 ,  C07K5/065 ,  C07K5/068 ,  C07K5/087 ,  A61K37/00

    CPC分类号： C07K5/0812 ,  C07K5/06078 ,  C07K5/06086 ,  A61K38/00

    摘要： The present invention relates to compounds of the formula: R.sub.1 SCH(R.sub.2)CH(R.sub.3)CO-AA.sub.1 �AA.sub.2 !.sub.m �AA.sub.3 !.sub.n --X or HSCH.sub.2 �CH.sub.2 CH(CH.sub.3).sub.2 !CO--Nal--NH.sub.2 wherein Nal is L-3-(2-naphthyl)alanine; m is the integer 0 or 1; n is an integer from 0-2; AA.sub.1 is a non-polar hydrophobic aromatic amino acid; AA.sub.2 is alanine, glycine, leucine, isoleucine or phenylalanine; AA.sub.3 is one of the twenty naturally occurring amino acids, preferably glutamine or arginine; R.sub.1 is hydrogen, alkyl having from 1-10 carbon atoms, alkanoyl having from 2-10 carbon atoms, or aroyl having from 7-10 carbon atoms; R.sub.2 is hydrogen or alkyl having from 1-6 carbon atoms; R.sub.3 is hydrogen, alkyl having from 2-10 carbon atoms, cycloalkyl having from 3-6 carbon atoms, aryl or arylalkyl, wherein aryl moieties have from 6-10 carbon atoms; X is NH.sub.2, OH, OCH.sub.3 or OCH.sub.2 CH.sub.3 ; and salts thereof.

    摘要翻译： 本发明涉及下式的化合物：R1SCH（R2）CH（R3）CO-AA1 [AA2] m [AA3] nX或HSCH2 [CH2CH（CH3）2] CO-Nal-NH2，其中Nal是L-3-（2 - 萘基）丙氨酸; m是整数0或1; n是0-2的整数; AA1是非极性疏水性芳香族氨基酸; AA2是丙氨酸，甘氨酸，亮氨酸，异亮氨酸或苯丙氨酸; AA3是二十种天然存在的氨基酸之一，优选为谷氨酰胺或精氨酸; R1是氢，具有1-10个碳原子的烷基，具有2-10个碳原子的烷酰基，或具有7-10个碳原子的芳酰基; R2是氢或具有1-6个碳原子的烷基; R3是氢，具有2-10个碳原子的烷基，具有3-6个碳原子的环烷基，芳基或芳烷基，其中芳基部分具有6-10个碳原子; X是NH 2，OH，OCH 3或OCH 2 CH 3; 及其盐。

    Antimicrobial agents
    4.
    发明授权
    Antimicrobial agents 失效
    抗微生物剂

    公开(公告)号：US06551998B1

    公开(公告)日：2003-04-22

    申请号：US09599787

    申请日：2000-06-22

    申请人： Arno F. Spatola ,  James Jun Wen ,  David M. Vogel

    发明人： Arno F. Spatola ,  James Jun Wen ,  David M. Vogel

    IPC分类号： A61K3807

    CPC分类号： C07K5/0207 ,  A61K38/00 ,  C07K7/02 ,  Y02P20/55

    摘要： Antimicrobial compounds of formula I are disclosed: R1—X—R2 wherein X is a group comprising of from about 4 to about 10 amino acids, wherein at least one of the amide (—CONH—) linkages is replaced by —CRaRaRbNRc—; Ra, Rb, and Rc are each independently hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C3-C8)cycloalkyl, (C1-C6)alkoxycarbonyl, aryl, or heterocycle; and R1 and R2 are each independently hydrogen, a saccharide, a lipid, a solubilizing agent, or a suitable protecting group; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising such compounds or salts, and methods of using such compounds or salts to treat a bacterial infection.

    摘要翻译： 公开了式I的抗微生物化合物：其中X是包含约4至约10个氨基酸的基团，其中至少一个酰胺（-CONH-）键被-CR a R a R b NR c - 取代; R a，R b和R c是 各自独立地为氢，（C1-C6）烷基，（C2-C6）烯基，（C2-C6）炔基，（C3-C8）环烷基，（C1-C6）烷氧基羰基，芳基或杂环; 并且R 1和R 2各自独立地为氢，糖，脂质，增溶剂或合适的保护基;或其药学上可接受的盐，以及包含这些化合物或盐的药物组合物，以及使用这些化合物或盐 治疗细菌感染。

    Cyclic peptide mixtures via side chain or backbone attachment and solid phase synthesis
    5.
    发明授权
    Cyclic peptide mixtures via side chain or backbone attachment and solid phase synthesis 失效
    通过侧链或骨架连接和固相合成的环状肽混合物

    公开(公告)号：US6008058A

    公开(公告)日：1999-12-28

    申请号：US423091

    申请日：1995-04-18

    申请人： Arno F. Spatola ,  Krzysztof Darlak ,  James Jun Wen ,  Peteris Romanovskis

    发明人： Arno F. Spatola ,  Krzysztof Darlak ,  James Jun Wen ,  Peteris Romanovskis

    IPC分类号： C07K1/04 ,  C07K7/50 ,  C07K7/64 ,  G01N33/543 ,  C07C7/00 ,  C07C17/00 ,  C07C5/12

    CPC分类号： C07K7/64 ,  C07K1/047 ,  C07K7/50

    摘要： A method of preparing cyclic peptide mixtures via side chain or backbone and solid phase synthesis. The cyclic peptide mixtures form libraries that are useful for screening purposes featuring the attachment of an amino acid to a solid support through its side chain or backbone in order to mimic solution cyclization procedures with linear peptides. In the preferred embodiment, Boc chemistry is used for peptide synthesis, wherein the initial attachment of a trifunctional amino acid is by the aspartyl side chain (with OFm for alpha-carboxyl protection). Cyclization is performed using uronium reagents with racemization suppressant, and a strong acid (HF) is used for deprotection and cleavage. The strategy has been used for the preparation of a series of cyclic peptide mixtures. The procedure is expandable to include at least twenty different amino acids at each position (except the resin linked position where most attachments are by Asp, Lys, Glu, or Orn). The cyclic peptide mixtures vary in ring size from about four to about twelve residues.

    摘要翻译： 通过侧链或骨架和固相合成制备环肽混合物的方法。 环状肽混合物形成可用于筛选目的的文库，其特征在于通过其侧链或主链将氨基酸连接到固体支持物上，以模拟具有线性肽的溶液环化程序。 在优选的实施方案中，Boc化学用于肽合成，其中三官能氨基酸的初始附着是通过天冬氨酰侧链（具有用于α-羧基保护的OFm）。 使用具有消旋抑制剂的尿素试剂进行环化，使用强酸（HF）进行脱保护和切割。 该策略已被用于制备一系列环肽混合物。 该程序可扩展至每个位置至少包含二十个不同的氨基酸（除大多数附着物由Asp，Lys，Glu或Orn组成的树脂连接位置除外）。 环肽混合物的环尺寸约为四至十二个残基。

    Thionated analogues of thyrotropin releasing hormone
    6.
    发明授权
    Thionated analogues of thyrotropin releasing hormone 失效
    Throtated类似物的促甲状腺激素释放激素

    公开(公告)号：US5244884A

    公开(公告)日：1993-09-14

    申请号：US963026

    申请日：1992-10-19

    申请人： Arno F. Spatola ,  Leszek Lankiewicz ,  Virender M. Labroo ,  Stefan Vonhof

    发明人： Arno F. Spatola ,  Leszek Lankiewicz ,  Virender M. Labroo ,  Stefan Vonhof

    IPC分类号： A61K38/00 ,  C07K5/097

    CPC分类号： C07K5/0821 ,  A61K38/00

    摘要： There are disclosed thionated analogues of thyrotropin releasing hormone, having the formula: ##STR1## wherein, Q, W, X and Y, same or different, are oxygen or sulfur, with the proviso that at least one of Q, W, X and Y is always sulfur;Z is lower alkyl or (4-imidazolyl)methyl; and the pharmaceutically acceptable salts thereof. The disclosed compounds highly and selectively bind to TRH binding sites in animal tissues, and their utility in treating a variety of diverse physical conditions is disclosed. Pharmaceutical compositions containing the compounds are also disclosed.

    摘要翻译： 公开了具有以下分子式的促甲状腺激素释放激素的分解类似物：其中Q，W，X和Y相同或不同，是氧或硫，条件是Q，W，X和 Y总是硫; Z是低级烷基或（4-咪唑基）甲基; 及其药学上可接受的盐。 所公开的化合物高度和选择性地结合动物组织中的TRH结合位点，并且其在治疗各种各样的物理条件中的用途被公开。 还公开了含有这些化合物的药物组合物。