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    • 7. 发明授权
    • Cyclic adhesion inhibitors
    • 环状粘连抑制剂
    • US6001961A
    • 1999-12-14
    • US694387
    • 1996-09-16
    • Alfred JonczykSimon GoodmanBeate DiefenbachArne SutterGunter HolzemannHorst KesslerMichael Dechantsreiter
    • Alfred JonczykSimon GoodmanBeate DiefenbachArne SutterGunter HolzemannHorst KesslerMichael Dechantsreiter
    • A61K38/00A61K38/04A61K38/12A61P9/00A61P31/04A61P35/00A61P35/04A61P39/00A61P43/00C07K1/113C07K7/64C07K7/00
    • C07K7/64A61K38/00
    • The invention relates to novel cyclopeptides of the formula Icyclo-(nArg-nGly-nAsp-nD-nE) I,in whichD and E in each case independently of one another are Gly, Ala, .beta.-Ala, Asn, Asp, Asp(OR), Arg, Cha, Cys, Gln, Glu, His, Ile, Leu, Lys, Lys(Ac), Lys(AcNH.sub.2), Lys(AcSH), Met, Nal, Nle, Orn, Phe, 4-Hal-Phe, homo-Phe, Phg, Pro, Pya, Ser, Thr, Tia, Tic, Trp, Tyr or Val, which amino acid residues can also be derivatized,R is alkyl having 1-18 carbon atoms,Hal is F, Cl, Br, I,Ac is alkanoyl having 1-10 carbon atoms, aroyl having 7-11 carbon atoms or aralkanoyl having 8-12 carbon atoms,n denotes no substituent or an alkyl radical R, benzyl or an aralkyl radical having 7-18 carbon atoms on the alpha-amino function of the relevant amino acid residue,with the proviso that at least one amino acid residue has a substituent n and that, where residues of optically active amino acids and amino acid derivatives are involved, both the D and the L forms are included, and also their physiologically acceptable salts.These compounds act as integrin inhibitors and can be used in particular for the prophylaxis and treatment of disorders of the circulation, angiogenic disorders, microbial infections and in tumor therapy.
    • 本发明涉及式I环 - (nArg-nGly-nAsp-nD-nE)I的新型环肽,其中D和E各自独立地为Gly,Ala,β-Ala,Asn,Asp,Asp (OR),Arg,Cha,Cys,Gln,Glu,His,Ile,Leu,Lys,Lys(Ac),Lys(AcNH 2),Lys(AcSH),Met,Nal,Nle,Orn, -Phe,Phe-Phe,Phg,Pro,Pya,Ser,Thr,Tia,Tic,Trp,Tyr或Val,该氨基酸残基也可被衍生化,R是具有1-18个碳原子的烷基,Hal是F, Cl,Br,I,Ac是具有1-10个碳原子的烷酰基,具有7-11个碳原子的芳酰基或具有8-12个碳原子的芳烷酰基,n表示没有取代基或烷基R,苄基或具有7- 相关氨基酸残基的α-氨基官能团上的18个碳原子,条件是至少一个氨基酸残基具有取代基n,并且当涉及光学活性氨基酸和氨基酸衍生物的残基时,D 并且包括L形式,也包括它们的生理学 可接受的盐。 这些化合物用作整联蛋白抑制剂,特别可用于预防和治疗循环障碍,血管生成障碍,微生物感染和肿瘤治疗。
    • 9. 发明授权
    • Cyclic adhesion inhibitors
    • 环状粘连抑制剂
    • US06127335A
    • 2000-10-03
    • US155721
    • 1999-04-08
    • Alfred JonczykSimon GoodmanBeate DiefenbachHorst KesslerMarcus Koppitz
    • Alfred JonczykSimon GoodmanBeate DiefenbachHorst KesslerMarcus Koppitz
    • A61K38/00A61K31/00A61K38/12A61P7/02A61P31/00A61P31/04A61P35/00B01D15/08B01J20/281C07K1/22C07K7/64C07K14/75C07K14/78G01N30/88C07K5/12
    • C07K7/64C07K14/75A61K38/00
    • The invention concerns cyclopeptides of formula (I): Cyclo-(Arg-Gly-Asp-X-Y) in which X is Cha, Nal, Phe, 2-R.sup.1 -Phe, 3-R.sup.1 -Phe, 4-R.sup.1 -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.sup.1 is NH.sub.2, NO.sub.2, I Br, Cl, F, alkyl with 1-18 C-atoms, Ar, Ar--O or.sup.3 H, Y is Gly in which the .alpha. N-atom may be substituted by R.sup.2 and/or the .alpha. C-atom may be substituted by R.sup.3 and/or R.sup.4, 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 groups NH.sub.2, NO.sub.2, I, Br, Cl, F, alkyl with 1-6 C-atoms or .sup.3 H, R.sup.2, R.sup.3 or R.sup.4, independently of each other, are alkyl with 1-18 C-atoms or R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 together in each case are a branched or unbranched alklyene chain with 3 to 18 C-atoms so that either the .alpha. N-atom or the .alpha. C-atom together with the alkylene chain, or the .alpha. C-atom alone, forms a ring with 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.
    • PCT No.PCT / EP97 / 01657 Sec。 371日期1999年4月8日 102(e)1999年4月8日PCT PCT 1997年4月2日PCT公布。 公开号WO97 / 38009 日期:1997年10月16日本发明涉及式(I)的环肽:其中X为Cha,Nal,Phe,2-R1-Phe,3-R1-Phe,4- R1-Phe,hom-Phe,Phg,Thi,Trp,Tyr或Tyr的衍生物,其中OH基团可以被含有1-18个C原子的烷基醚化,并且所给出的氨基酸基团也可以是衍生物,R1 是NH 2,NO 2,I Br,Cl,F,具有1-18个C原子的烷基,Ar,Ar-O或3 H,Y是其中αN原子可以被R 2和/或αC- 原子可以被R 3和/或R 4取代,条件是Gly具有至少一个指定的取代基,Ar是可被一个或两个NH 2,NO 2,I,Br,Cl,F, 具有1-6个C原子的烷基或3H,R 2,R 3或R 4彼此独立地是具有1-18个碳原子的烷基或者R 2,R 3或R 3和R 4在每种情况下一起是支链或非支链烷基链 具有3至18个C原子,使得αN原子或αC原子与亚烷基链一起,或者 单独的αC原子形成具有亚烷基链的环,由此当涉及光学活性氨基酸或氨基酸衍生物基团时,包括D-和L-形式,加上衍生物,特别是β 的天冬氨酸或精氨酸或前药的N-胍酰基衍生物及其生理上可接受的盐。 这些化合物作为整合素抑制剂起作用,可用于预防和治疗循环和血管生成病症和微生物感染以及肿瘤治疗。