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    • 1. 发明申请
      WO1997038009A1 CYCLIC ADHESION INHIBITORS 审中-公开
    • CYCLIC ADHESION INHIBITORS
    • CYCLIC粘附抑制剂
    • WO1997038009A1
    • 1997-10-16
    • PCT/EP1997001657
    • 1997-04-02
    • MERCK PATENT GMBH , JONCZYK, Alfred , GOODMAN, Simon , DIEFENBACH, Beate , KESSLER, Horst , KOPPITZ, Marcus
    • MERCK PATENT GMBH
    • C07K07/64
    • C07K7/64 , A61K38/00 , C07K14/75
    • The invention concerns cyclopeptides of formula (I): Cyclo-(Arg-Gly-Asp-X-Y) in which X is Cha, Nal, Phe, 2-R -Phe, 3-R -Phe, 4-R -Phe, homo-Phe, Phg, Thi, Trp, Tyr or derivatives of Tyr, whereby the OH group can be etherified by alkyl groups containing 1-18 C-atoms and the amino-acid groups given can also be derivatives, R is NH2, NO2, I, Br, Cl, F, alkyl with 1-18 C-atoms, Ar, Ar-O or H, Y is Gly in which the alpha N-atom may be substituted by R and/or the alpha C-atom may be substituted by R and/or R , with the provision that Gly has at least one of the substituents specified, Ar is phenyl which may be substituted by one or two of the groups NH2, NO2, I, Br, Cl, F, alkyl with 1-6 C-atoms or H, R , R or R , independently of each other, are alkyl with 1-18 C-atoms or R and R or R and R together in each case are a branched or unbranched alkylene chain with 3 to 18 C-atoms so that either the alpha N-atom and the alpha C-atom together with the alkylene chain, or the alpha C-atom alone, forms a ring with the alkylene chain, whereby, when optically active amino-acid or amino-acid-derivative groups are involved, both the D- and the L-form are included, plus derivatives, in particular the beta -ester of aspartic acid or N-guanidine acyl derivatives of arginine or prodrug as well as their physiologically acceptable salts. These compounds act as integrin inhibitors and may be used particularly for the prophylaxis and treatment of circulatory and angiogenic conditions and microbial infections as well as in tumor therapy.
    • 本发明涉及式（I）下式的新的环肽：环 - （精氨酸 - 甘氨酸 - 天冬氨酸-XY）中的X是茶，碘化钠，苯丙氨酸，2-R <1> -Phe，3-R <1> -Phe，4- [R <1> -Phe，同型苯丙氨酸，PHG，氏，色氨酸，酪氨酸或其中OH基团可以被具有1-18个碳原子的烷基基团被醚化的Tyr，的衍生物，以及其中提及的氨基酸残基也另外被衍生 可能; [R <1> NH 2，NO 2，I，溴，氯，F，烷基具有1-18个碳原子中，Ar中，Ar-O或<3> H; Y是甘氨酸，其特征在于，所述α-N-原子由R <2>和/或由R阿尔法-C原子<3>和/或R <4>可以被取代，其条件是至少甘氨酸容易 表明为取代的方式; Ar是苯基，其可以任选地单 - 或二取代的NH 2，NO 2，I，溴，氯，F，具有1-6个C原子的烷基，或<3> H; [R <2>，R <3>或R <4>各自独立地是烷基在每种情况下具有1-18个C原子，或R <2>和R <3>或R <3>和R <4>也一起 是指具有碳原子数为3〜18，有支链或无支链的亚烷基链，以使这些阿尔法 - N-原子和α-C与亚烷基链一起原子，或α-C与亚烷基链形成环单独原子， 其中，如果是光学活性的氨基酸和氨基酸衍生物，无论是D和L形式都包括在内，和衍生物，特别是天冬氨酸酸性β-酯或精氨酸的N-胍酰基衍生物，前药的基团， 和它们的生理学可接受的盐。 这些化合物作为整联蛋白抑制剂，并且可以特别地用于循环的障碍，血管生成病症，微生物感染的预防和治疗以及在肿瘤治疗中使用。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 6. 发明专利
      BR7105458D0  未知
    • BR7105458D0
    • 1973-05-10
    • BR545871
    • 1971-08-20
    • MERCK PATENT GMBH
    • MERCK PATENT GMBH
    • C07H19/10
    • 1348289 Thiopyrimidine nucleotide derivatives MERCK PATENT GmbH 10 Aug 1971 [22 Aug 1970] 37535/71 Heading C2P [Also in Divisions A5 and C3] The invention comprises thiopyrimidine derivatives of the general formula in which R is B is the radical of a pyrimidine or purine base, X is S or NH, m is an integer from 1 to 3 and n is a whole number from 0 to 2000 and in which the sum of m and n is at least 2 and different B radicals may be present in the same molecule, their metal and ammonium salts, and the disulphides of the derivatives in which X is sulphur. They may be obtained by (a) reacting 2,4 - dithiouridine monophosphate or 2- thiocytidine monophosphate or a compound of the above general Formula (I) in which m=1 with an inorganic or organic ortho- or pyrophosphate, one of the reactants being in activated form, (b) treating a compound of Formula I but in which the XH group is replaced by a radical which can be substituted by XH with a compound of formula H 2 X, or (c) treating a compound I but in which at least one OH, SH or NH 2 group is present in a functionally modified form or in which a reducible functional group is present with a solvolysing or reducing agent respectively in order to liberate one of the groups OH, SH or NH 2 . The products I may be subjected to the action of a polymerizing enzyme, if desired in the presence of a further nucleotide, to form oligo- or poly-nucleotides and/ or treated with an oxidizing agent and/or treated with an ammonolysing agent to convert an SH group when present therein to an NH 2 group, if necessary in a multistage reaction. The substituent B is preferably a 2,4-dithiouracilyl, 2-thiocytosyl, or adenylyl radical. In method (a) one of the reactants must be present in activated form, e.g. as an imidazolidate, morpholidate, anilide, or activated ester, e.g. pnitrophenyl ester or 2-pyridyl ester. In method (b) the radical replacing the XH group is suitably a C 1 -C 4 alkyl mercapto or benzyl mercapto radical, a sulphonic acid radical (or salt thereof), a sulphonic alkyl or aryl ester radical, or a halogen atom, e.g. Cl or Br. In method (c) the functionally modified group may suitably be an acyloxy, acyl-mercapto or acylamido group, benzyloxy or triphenylmethoxy or may comprise neighbouring OH groups in acetal, ketal or orthoester-like form. Such groups are preferably solvolytically split off in an aqueous alkaline or weakly acid medium which may also contain an organic solvent. When an additional nucleotide is added during the above referred to enzyme polymerization it becomes incorporated in the polynucleotide formed which may thus contain different nitrogen base radicals, e.g. 2,4-dithiouracilyl and adenylyl. Suitable enzymes for the polymerization are polynucleotide phosphorylases and the polymerization is preferably effected in an aqueous medium at pH 5À5 to 9À5 preferably in the presence of a buffer and of an inorganic salt such as magnesium-, manganese (II)- or calcium chloride. The mono or polynucleotide products can be oxidized to the corresponding disulphides by means of oxidizing agents, e.g. iodine. When an SH group is present in a compound of Formula I it may be converted to an NH 2 group, e.g. treating a trialkylammonium salt of I (X=S) with gaseous ammonia in a solvent. Reducible functional groups such as benzyloxy, triphenylmethoxy, NO 2 or azido present in compounds corresponding to those of Formula I can also be converted to free OH or NH 2 groups by means of reducing agents, thus the disodium salt of 4-azido-2-thiopyrimidyl-(1 1 #,D-ribose)- 5 1 -diphosphate is converted to the disodium salt of 2 - thiocytidine - 5 1 - diphosphate by reaction with zinc dust in aqueous acetic acid (see Example 7). Examples are also given for the production of 2,4-dithiouridine-5 1 -di-(and tri)phosphates and 2-thiocytidine-5 1 -di-(and tri- ) phosphates which are isolated in the form of their di-(or tri-)sodium salts, and of various polynucleotides. The products have antiviral and antitumour activity and may be used as active ingredients in pharmaceutical compositions of conventional type.
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