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    • 2. 发明授权
    • Cyclic peptides and medicinal use thereof
    • 环状肽及其药用
    • US06511961B1
    • 2003-01-28
    • US09341435
    • 1999-07-09
    • Toshiya TakahashiNobuo SaitoHideyuki TakeshigeToshiaki TanakaMie Kainoh
    • Toshiya TakahashiNobuo SaitoHideyuki TakeshigeToshiaki TanakaMie Kainoh
    • A61K3800
    • C07K7/06A61K38/00C07K7/54C07K7/64C07K14/70542C07K14/7055
    • Novel cyclic peptides having VLA-4 adhesion inhibiting activity, and their application as therapeutic agents for inflammatory disease, for example allergic inflammatory disease, or hepatitis. Cyclic peptides represented by formula (I) where A and F may be the same or different, and are both selected from L- or D-form Cys, homo-Cys, Pen and Mpr, or both from the group comprising Asp, Glu, Aad, Dpr, Dab and Orn, B is selected from L-or D-form Ala, Ala(t-Bu), Val, Leu, Ile, aIle, Abu, Nle, Nva, Tle, Cha, Chg, Phe, Phg, Trp, Ala(3-Bzt), Ala(1-Naph), Ala(2-Naph), Ala(2-Pyr), Ala(2-Qui), His, Thi, Ala(4-Thz), 2-Abz, Pro, homo-Pro and Tic, C is selected from L-form Asp analogues, Gle analogues, Aad analogues, Asn analogues, Gln analogues, Ser, Ser(OMe), homo-Ser, Dpr, Dab, Orn, Met, Met)O), Met(O2), aIle, Nle, Nva, Chg, Phg, Tyr and Tle, D is selected from L- or D-form Tyr, Ser, homo-Ser, Leu, Ile, AIle, Nle, Nva, Chg, Cha, Val, Ala(t-Bu), Abu, Tle, Ala, Phg, homo-Phe, Phe, Ala(2-Naph), Ala(2-Pyr), Ala(3-Bzt), Ala(1-Naph), Ala(2-Qui), Thi, Ala(4-Thz), 2-Abz, Trp and His, E is selected from L- or D-form Leu, Ile, aIle, Nle, Nva, Chg, Cha, Tle, Phg, homo-Phe, Ala(2-Naph), Ala(2-Pyr), Ala(3-Bzt, Ala(1-Naph), Ala(2-Qui), Thi, Ala(4-Thz), 2-Abz and His, G represents a disulphide bond or amide bond, R1 represents hydrogen or an acyl group, and R2 is hydrogen or an alkyl group, or salts thereof, and to their use in treating inflammatory diseases.
    • 具有VLA-4粘附抑制活性的新型环肽及其作为炎症性疾病例如过敏性炎性疾病或肝炎的治疗剂的应用。 由式(I)表示的环肽,其中A和F可以相同或不同,并且均选自L-或D-型Cys,homo-Cys,Pen和Mpr,或二者均为Asp,Glu, Aad,Dpr,Dab和Orn,B选自L-型或D-型Ala,Ala(t-Bu),Val,Leu,Ile,aIle,Abu,Nle,Nva,Tle,Cha,Chg,Phe,Phg ,Trp,Ala(3-Bzt),Ala(1-Naph),Ala(2-Naph),Ala(2-Pyr),Ala(2-Qui),His,Thi,Ala(4-Thz) -Abz,Pro,homo-Pro和Tic,C选自L型Asp类似物,Gle类似物,Aad类似物,Asn类似物,Gln类似物,Ser,Ser(OMe),homo-Ser,Dpr,Dab,Orn, Met,Met)O),Met(O 2),aIle,Nle,Nva,Chg,Phg,Tyr和Tle,D选自L-或D型Tyr,Ser,homo-Ser,Leu,Ile, Nle,Nva,Chg,Cha,Val,Ala(t-Bu),Abu,Tle,Ala,Phg,hom-Phe,Phe,Ala(2-Naph),Ala(2-Pyr),Ala(3-Bzt ),Ala(1-Naph),Ala(2-Qui),Thi,Ala(4-Thz),2-Abz,Trp和His,E选自L-或D-型Leu,Ile,aIle,Nle ,Nva,Chg,Cha,Tle,Phg,hom-Phe,Ala(2-Naph),Ala(2-Pyr), Ala(3-Bzt,Ala(1-Naph),Ala(2-Qui),Thi,Ala(4-Thz),2-Abz和His,G表示二硫键或酰胺键,R1表示氢或酰基 并且R 2是氢或烷基,或其盐,以及它们在治疗炎性疾病中的用途。
    • 6. 发明申请
    • PROCESS FOR PRODUCTION OF POLYAMIDEIMIDE RESIN MICROPARTICLES, AND POLYAMIDEIMIDE RESIN MICROPARTICLES
    • 聚酰胺树脂微生物生产工艺和聚酰胺树脂微生物
    • US20120237771A1
    • 2012-09-20
    • US13508200
    • 2010-10-06
    • Hiroaki AkasakaTakae OnoToshiya Takahashi
    • Hiroaki AkasakaTakae OnoToshiya Takahashi
    • C08G73/14
    • C08J3/14C08G73/14C08J2379/08Y10T428/2982
    • A process for producing fine particles of polyamide-imide resin includes a dissolution step and a precipitation step wherein the dissolution step is selected from steps (a1) and (b1); (a1) polyamide-imide resin is dissolved in an organic solvent to prepare a polyamide-imide resin solution A1 having a polyamide-imide resin content of less than 5 mass %; and (b1) polyamide-imide resin is dissolved in an organic solvent to prepare a polyamide-imide resin solution B1 having a polyamide-imide resin content of less than 10 mass %, and the precipitation step is selected from (a2) the polyamide-imide resin solution A1 is added to a solvent that is virtually free from surface active agents and able to precipitate fine particles of the polyamide-imide resin to cause precipitation of fine particles of the polyamide-imide resin, and (b2) the polyamide-imide resin solution B1 is subjected to flash crystallization to cause precipitation of fine particles of the polyamide-imide resin.
    • 制备聚酰胺酰亚胺树脂微粒的方法包括溶解步骤和沉淀步骤,其中溶解步骤选自步骤(a1)和(b1); (a1)聚酰胺酰亚胺树脂溶解在有机溶剂中,制备聚酰胺 - 酰亚胺树脂含量小于5质量%的聚酰胺 - 酰亚胺树脂溶液A1; 和(b1)聚酰胺酰亚胺树脂溶解在有机溶剂中,制备聚酰胺 - 酰亚胺树脂含量小于10质量%的聚酰胺 - 酰亚胺树脂溶液B1,沉淀步骤选自(a2)聚酰胺 - 将酰亚胺树脂溶液A1加入到基本上不含表面活性剂的溶剂中,并能够使聚酰胺 - 酰亚胺树脂的细颗粒沉淀,使聚酰胺 - 酰亚胺树脂的细颗粒沉淀,和(b2)聚酰胺 - 酰亚胺 树脂溶液B1进行闪光结晶,使聚酰胺 - 酰亚胺树脂的微粒析出。