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42 条记录 (耗时 0.016 秒)

    Cyclic octapeptide neuromedin B receptor antagonists
    3.
    发明授权
    Cyclic octapeptide neuromedin B receptor antagonists 失效
    循环八肽神经介肽B受体拮抗剂

    公开(公告)号：US5569741A

    公开(公告)日：1996-10-29

    申请号：US352392

    申请日：1994-12-08

    申请人： David H. Coy ,  John E. Taylor

    发明人： David H. Coy ,  John E. Taylor

    IPC分类号： A61K38/00 ,  A61K38/31 ,  A61P43/00 ,  C07K7/06 ,  C07K7/52 ,  C07K14/655 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

    CPC分类号： A61K38/31 ,  C07K14/6555

    摘要： A cyclic octapeptide of the formula: ##STR1## wherein: A.sup.1 is D-Nal or D-Trp;A.sup.3 is Phe, F.sub.5 -Phe, or X-Phe wherein X is a halogen, NO.sub.2, CH.sub.3, or OH;A.sup.5 is --NH--CH(Y)--CO-- wherein Y is (CH.sub.2).sub.m --R.sub.4 --N(R.sub.5)(R.sub.6) or (CH.sub.2).sub.n --R.sub.4 --NH--C(R.sub.7)--N(R.sub.5) (R.sub.6);A.sup.6 is the D-- or L-- isomer of Thr, Leu, Ile, Nle, Val, and Abu;A.sup.8 is Nal or Trp;m is 1, 2, or 3;n is 1, 2, 3, 4 or 5;each of R.sub.1 and R.sub.2, independently, is H, E, COE, or COOE wherein E is C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl, phenyl, naphthyl, C.sub.7-12 phenylalkyl or alkylphenyl, C.sub.8-12 phenylalkenyl or alkenylphenyl, C.sub.8-12 phenylalkynyl or alkynylphenyl, C.sub.11-20 naphthylalkyl or alkylnaphthyl, C.sub.12-20 naphthylalkenyl or alkenylnaphthyl, or C.sub.12-20 naphthylalkynyl or alkynylnaphthyl, provided that when one of R.sub.1 or R.sub.2 is COE or COOE, the other must be H;R.sub.4 is C.sub.6 H.sub.4 or absent;R.sub.7 is .dbd.NR.sub.8, .dbd.S, or .dbd.O; andeach of R.sub.3, R.sub.5, R.sub.6, and R.sub.8, independently, is H or E.

    摘要翻译： 下式的环状八肽：其中：A1为D-Nal或D-Trp; A3是Phe，F5-Phe或X-Phe，其中X是卤素，NO 2，CH 3或OH; A5是-NH-CH（Y）-CO-，其中Y是（CH2）m-R4-N（R5）（R6）或（CH2）n-R4-NH-C（R7）-N（R5） ）; A6是Thr，Leu，Ile，Nle，Val和Abu的D-或L-异构体; A8是Nal或Trp; m为1,2或3; n为1,2,3,4或5; R 1和R 2各自独立地是H，E，COE或COOE，其中E是C 1-12烷基，C 2-12烯基，C 2-12炔基，苯基，萘基，C 7-12苯基烷基或烷基苯基，C 8-12苯基烯基 或烯基苯基，C 8-12苯基炔基或炔基苯基，C 11-20萘基烷基或烷基萘基，C 12-20萘基烯基或链烯基萘基，或C 12-20萘基炔基或炔基萘基，条件是当R 1或R 2中的一个为COE或COOE时，另一个必须为H ; R4为C6H4或不存在; R 7 = NR 8，= S或= O; R 3，R 5，R 6和R 8各自独立地为H或E.

    Antiulcer compounds
    5.
    发明授权
    Antiulcer compounds 失效
    抗溃疡化合物

    公开(公告)号：US4598067A

    公开(公告)日：1986-07-01

    申请号：US661354

    申请日：1984-10-16

    申请人： Sun H. Kim

    发明人： Sun H. Kim

    IPC分类号： C07D487/04 ,  A61K31/415 ,  A61K31/47 ,  A61K31/472 ,  A61K38/00 ,  A61P1/04 ,  C07C67/00 ,  C07C231/00 ,  C07C237/12 ,  C07D207/28 ,  C07D217/16 ,  C07D217/26 ,  C07D233/64 ,  C07D403/12 ,  C07D471/04 ,  C07K5/06 ,  C07K5/078 ,  A61K37/43 ,  C07K5/08

    CPC分类号： C07D403/12 ,  C07D207/28 ,  C07D471/04 ,  C07K5/06026 ,  C07K5/06173 ,  A61K38/00

    摘要： A compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein A is N--Ac--Sar, pGlu, or homo-pGlu-; B is an aryl group, a heteroaryl group, a cycloalkyl group, an aralkyl group, a heteroalkyl group, a heteroaralkyl group, a benzoyl group, an alkyl group, an acetyl group, or a substituted aryl group wherein the substituent is halogen, hydroxy, alkoxy, nitro, cyano, or hydroxyalkyl; E is H or an alkyl group; B and E being separate substituents or, together with C.sub.1 and the nitrogen atom to which B is attached, forming a 5,6, or 7-membered ring; m is an integer between 0 and 4; either F is ##STR2## wherein R is an alkoxy group or an aralkoxy group; or F is ##STR3## and is capable of forming a 6-membered ring with the nitrogen atom of A, provided that F can only be ##STR4## forming a ring with A when A is pGlu or homo-pGlu.

    摘要翻译： 具有式“IMAGE”的化合物或其药学上可接受的盐，其中A是N-Ac-Sar，pGlu或homo-pGlu-; B是芳基，杂芳基，环烷基，芳烷基，杂烷基，杂芳烷基，苯甲酰基，烷基，乙酰基或取代的芳基，其中取代基是卤素，羟基 ，烷氧基，硝基，氰基或羟基烷基; E是H或烷基; B和E是独立的取代基，或者与C1和与B连接的氮原子一起形成5,6或7-元环; m是0和4之间的整数; F是F，其中R是烷氧基或芳烷氧基; 或者F是，并且能够与A的氮原子形成6元环，条件是当A是pGlu或homo-pGlu时，F只能与A形成环。

    Imidazole compounds which reduce gastric acid secretion
    6.
    发明授权
    Imidazole compounds which reduce gastric acid secretion 失效
    减少胃酸分泌的咪唑化合物

    公开(公告)号：US4495193A

    公开(公告)日：1985-01-22

    申请号：US454733

    申请日：1982-12-30

    申请人： Sun H. Kim ,  Jacques-Pierre Moreau

    发明人： Sun H. Kim ,  Jacques-Pierre Moreau

    IPC分类号： C07D209/46 ,  C07D403/06 ,  C07D403/12 ,  A61K31/415

    CPC分类号： C07D403/06 ,  C07D209/46 ,  C07D403/12

    摘要： A compound having gastric acid secretion reducing activity and having the formula ##STR1## wherein each V and W, independently, is H, --CH.sub.2 COOR.sup.4 where R.sup.4 is H or lower alkyl, --CH.sub.2 CN, or ##STR2## or V and W together represent .dbd.CHCOOR.sup.4 or .dbd.CHCN; A is ##STR3## R.sup.1 is H or CH.sub.3 ; L is CH.sub.2 S; Q is O or CH.sub.2 S; n is 0 or 1; 2 m 4; each R.sup.2 and R.sup.3, independently, is hydrogen, lower alkyl, lower cycloalkyl, or lower aralkyl; or R.sup.2 and R.sup.3, together with the nitrogen atom to which they are attached, form a 4, 5, or 6 membered heterocyclic ring containing 0, 1, or 2 oxygen atoms and 1, 2, or 3 nitrogen atoms and being unsubstituted or lower alkyl substituted; and Ar is a single ring aromatic group selected from aryl, substituted aryl, fused aryl, or heteroaryl; or the pharmaceutically acceptable salt thereof.

    摘要翻译： 具有胃酸分泌降低活性并具有下式的化合物：其中每个V和W独立地是H，-CH 2 COOR 4，其中R 4是H或低级烷基，-CH 2 CN或V和W一起代表= CHCOOR4或= CHCN; A是 + TR R1是H或CH3; L是CH2S; Q是O或CH2S; n为0或1; 2 m 4; 每个R 2和R 3独立地是氢，低级烷基，低级环烷基或低级芳烷基; 或R 2和R 3与它们所连接的氮原子一起形成含有0,1或2个氧原子和1,2或3个氮原子的4,5或6元杂环，并且是未取代的或低级的 烷基取代; Ar为选自芳基，取代芳基，稠合芳基或杂芳基的单环芳基; 或其药学上可接受的盐。

    Methods of using a somatostatin analogue
    7.
    发明授权
    Methods of using a somatostatin analogue 失效
    使用生长抑素类似物的方法

    公开(公告)号：US6150333A

    公开(公告)日：2000-11-21

    申请号：US361394

    申请日：1999-07-26

    申请人： Jacques-Pierre Moreau

    发明人： Jacques-Pierre Moreau

    IPC分类号： A61K38/31 ,  A61K38/00

    CPC分类号： A61K38/31

    摘要： The present invention is directed to a method of treating one or more of the following disease and/or conditions, which comprises administering to a patient in need thereof the compound H-.beta.-D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Thr-NH.sub.2, where the Cysteines are bonded by a disulfide bond, or a pharmaceutically acceptable salt thereof, most preferably the acetate salt of the compound, in the treatment of certain diseases and/or conditions such as gastroenterological conditions and/or diseases, endocrinological diseases and/or conditions, various types of cancers and conditions associated with cancer such as cancer cachexia and in the treatment of hypotension and panic attacks.

    摘要翻译： 本发明涉及一种治疗以下疾病和/或病症中的一种或多种的方法，其包括向有需要的患者施用化合物H-β-D-Nal-Cys-Tyr-D-Trp-Lys -Val-Cys-Thr-NH2，其中半胱氨酸通过二硫键键合，或其药学上可接受的盐，最优选化合物的乙酸盐，用于治疗某些疾病和/或病症如胃肠病学和 /或疾病，内分泌疾病和/或病症，与癌症如癌症恶病质相关的各种类型的癌症和病症以及治疗低血压和恐慌发作。

    Octapeptide bombesin analogs
    10.
    发明授权
    Octapeptide bombesin analogs 失效
    八肽铃蟾肽类似物

    公开(公告)号：US5877277A

    公开(公告)日：1999-03-02

    申请号：US337127

    申请日：1994-11-10

    申请人： David H. Coy ,  Jacques-Pierre Moreau ,  Sun Hyuk Kim

    发明人： David H. Coy ,  Jacques-Pierre Moreau ,  Sun Hyuk Kim

    IPC分类号： A61K38/00 ,  C07K7/02 ,  C07K7/08 ,  C07K7/18 ,  C07K14/575 ,  C07K14/685 ,  C07K5/00 ,  C07K7/00 ,  C07K7/06

    CPC分类号： C07K7/086 ,  C07K14/57572 ,  C07K14/685 ,  C07K7/02 ,  C07K7/18 ,  A61K38/00

    摘要： A linear (i.e., non-cyclic) analog of biologically active amphibian bombesin, mammalian gastrin-releasing peptide (GRP), or mammalian growth hormone releasing factor (GRF), having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell. Cleavage of a peptide bond in the active site of naturally occurring bombesin, GRP, or GRF is unnecessary for in vivo biological activity. The analog has one of the following modifications: (a) a deletion of an amino acid residue within the active site and a modification of an amino acid residue outside of the active site, (b) a replacement of two amino acid residues within the active site with a synthetic amino acid, a .beta.-amino acid, or a .gamma.-amino acid residue, or (c) a non-peptide bond instead of a peptide bond between an amino acid residue of the active site and an adjacent amino acid residue.

    摘要翻译： 具有活性位点和负责肽结合的结合位点的生物活性水陆两栖铃蟾肽，哺乳动物胃泌素释放肽（GRP）或哺乳动物生长激素释放因子（GRF）的线性（即非循环）类似物 到目标细胞上的受体。 在天然存在的铃蟾肽，GRP或GRF的活性位点中肽键的切割对于体内生物活性是不必要的。 类似物具有以下修饰之一：（a）活性位点内的氨基酸残基的缺失和活性位点之外的氨基酸残基的修饰，（b）在活性位点内置换两个氨基酸残基 具有合成氨基酸，β-氨基酸或γ-氨基酸残基的位点，或（c）非肽键代替活性位点的氨基酸残基与相邻氨基酸残基之间的肽键 。