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    • 93. 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。
    • 95. 发明授权
    • Kappa-opiate agonists effective in the treatment of postoperative ileus
    • 卡帕阿片激动剂有效治疗术后肠梗阻
    • US5977161A
    • 1999-11-02
    • US27228
    • 1998-02-20
    • Andrew BarberChristoph SeyfriedGerd BartoszykRudolf Gottschlich
    • Andrew BarberChristoph SeyfriedGerd BartoszykRudolf Gottschlich
    • C07D207/08A61K31/135A61K31/165A61K31/40A61K31/4015A61K31/4025A61P1/00A61P1/04A61P29/00A61P43/00C07D207/12
    • A61K31/4025
    • Disclosed herein are pharmaceutical preparations which are suitable for the treatment of postoperative ileus and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms,R.sup.2 is Ar, orR.sub.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2,R.sup.5 is OH, CH.sub.2 OH,R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring,A is alkyl having 1-7 C atoms,Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.2, O, S, NH, NA, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 NH--, --CH.sub.2 --NA-- or a bondandHal is F, Cl, Br or I.
    • 本文公开了适用于治疗术后肠梗阻并含有至少一种其中R 1为Ar的式I化合物或具有3-7个C原子的环烷基或具有4-8个C原子的环烷基烷基,R2为Ar, 或R 1和R 2一起为R 3为H,OH,OA或A,R 4为A或可任选被Hal,OH,OA,CF 3,NO 2,NH 2,NHA,NHCOA,NHSO 2 A单取代或二取代的苯基和/或 NA2,R5分别为H,Hal,OH,OA,CF3,NH2,NHA,NA2,NHCOA,NHCONH2,NO2或亚甲二氧基的OH,CH2OH,R6和R7彼此独立地键合, A是具有1-7个C原子的烷基,Ar是可以在环中任选含有N,O或S原子的单环或双环芳族基团,并且可以被A, ,Hal,OH,OA,CF 3,NH 2,NHA,NA 2,NHCOA和/或NHCONH 2,D是CH 2,O,S,NH,NA,-CH 2 -CH 2 - , - CH = CH-, - CH 2 NH-, CH2-NA-或键,Hal为F,Cl,Br或I.