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    • 2. 发明授权
    • Depsipeptide and congeners thereof for use as immunosuppressants
    • 其作为免疫抑制剂的前列腺素及其同系物
    • US06403555B1
    • 2002-06-11
    • US09732183
    • 2000-12-06
    • Søren Skov
    • Søren Skov
    • A61K3702
    • C07K11/02A61K38/00C07K5/101C07K7/56
    • Depsipeptides and congeners thereof are disclosed having the following structure: wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.
    • 公开了具有以下结构的脱肽及其同系物:其中m,n,p,q,X,R 1,R 2和R 3如本文所定义。 这些化合物,包括FR901228,具有例如免疫抑制剂的活性,以及​​用于预防或治疗患有或有遭受炎症,自身免疫或免疫系统相关疾病(包括移植物抗宿主病和增强)的风险的患者 移植后的移植物/组织存活。 还提供了抑制淋巴细胞活化,增殖和/或抑制IL-2分泌的方法。
    • 6. 发明授权
    • Use of GPE to protect glial cells or non-dopaminergic cells from death from neural injury or disease
    • 使用GPE来保护神经损伤或疾病的神经胶质细胞或非多巴胺能细胞免于死亡
    • US06780848B2
    • 2004-08-24
    • US09910461
    • 2001-07-20
    • Peter D. GluckmanChristopher E. Williams
    • Peter D. GluckmanChristopher E. Williams
    • A61K3702
    • A61K38/30A61K38/05A61K38/06
    • The tripeptide glycine-proline-glutamine (GPE) may be administered before, or usually after, injury to reduce damage to the central nervous system. GPE appears useful for neuronal rescue particularly but not exclusively within the hippocampus. Advantages of GPE include: (a) that it crosses the blood-brain barrier, so is effective by injected peripheral administration, (b) it is unlikely to challenge the immune system, (c) it is cheap, and (d) its therapeutic ratio is high. GPE may also be infused into the CSF. It may be administered prior to parturition or elective brain or cardiac surgery. Transdermal routes may be useful for chronic neural disorders. The CNS of mammals (including foetal mammals) after trauma including hypoxic/ischaemic experimental insults showed reduced damage under GPE protection as measured by histological assessment of cell damage or death and regional shrinkage.
    • 三肽甘氨酸 - 脯氨酸 - 谷氨酰胺(GPE)可以在损伤之前或通常在损伤后施用以减少对中枢神经系统的损伤。 GPE似乎对神经元的拯救有用,特别是但不限于海马内。 GPE的优点包括:(a)它穿过血脑屏障,因此通过注射的外周给药是有效的,(b)不可能挑战免疫系统,(c)它是便宜的,和(d)其治疗 比例高。 GPE也可以输入CSF。 它可以在分娩或选择性脑或心脏手术之前进行。 透皮途径可用于慢性神经障碍。 包括缺氧/缺血性实验性损伤在内的哺乳动物(包括胎儿哺乳动物)的CNS显示,在通过细胞损伤或死亡和区域收缩的组织学评估测量的GPE保护下减少的损伤。
    • 7. 发明授权
    • Therapeutic uses of depsipeptides and congeners thereof
    • 去磷脂肽及其同源物的治疗用途
    • US06548479B1
    • 2003-04-15
    • US10115576
    • 2002-04-02
    • Søren Skov
    • Søren Skov
    • A61K3702
    • C07K11/02A61K38/00C07K5/101C07K7/56
    • Depsipeptides and congeners thereof are disclosed having the following structure: wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.
    • 公开了具有以下结构的脱肽及其同系物:其中m,n,p,q,X,R 1,R 2和R 3如本文所定义。 这些化合物,包括FR901228,具有例如免疫抑制剂的活性,以及​​用于预防或治疗患有或有遭受炎症,自身免疫或免疫系统相关疾病(包括移植物抗宿主病和增强)的风险的患者 移植后的移植物/组织存活。 还提供了抑制淋巴细胞活化,增殖和/或抑制IL-2分泌的方法。
    • 9. 发明授权
    • Treatment of tropical spastic paresis with peptide T
    • 用T肽治疗热带痉挛性麻痹
    • US06242564B1
    • 2001-06-05
    • US07898691
    • 1992-06-15
    • Candace B. PertMichael R. Ruff
    • Candace B. PertMichael R. Ruff
    • A61K3702
    • C07K14/005A61K38/162A61K39/00C07K14/70514C07K16/1063C12N2740/16122
    • Intranasal therapy using short peptides of the formula (I): Ra-Ser-Thr-Thr-Thr-Asn-Tyr-Rb  (I) where Ra represents an amino terminal residue Ala-, D-Ala or Cys-Ala- and Rb represents a carboxy terminal residue -Thr, -Thr-amide, -Thr-Cys or -Thr-Cys-amide, or a derivative thereof, or a peptide of formula (II): R1-R2-R3-R4-R5  (II) where R1 is an amino terminal residue XR6 or R6 wherein R6 is Thr-, Ser-, Asn-, Leu-, Ile-, Arg- or Glu- and X is Cys, R2 is Thr, Ser or Asp, R3 is Thr, Ser, Asn, Arg, Gln, Lys or Trp, R4 is Tyr and R5 is a carboxy terminal residue which is R7X or R7 wherein R7 may be any amino acid and X is Cys, or an ester or amide derivative thereof, or a physiologically acceptable salt of (I) or (II) is disclosed. Such peptides bind to T4 receptors and are useful for intranasal administration in preventing viral infectivity in mammals by viruses which bind to the T4 receptors. These peptides are believed to act as competitive blocking agents.
    • 使用式(I)的短肽的鼻内治疗:其中Ra表示氨基末端残基Ala-,D-Ala或Cys-Ala-和Rb表示羧基末端残基-Thr,-Thr-amide,-Thr-Cys或 -Thr-Cys-酰胺或其衍生物或式(II)的肽:其中R 1是氨基末端残基XR 6或R 6,其中R 6是Thr-,Ser-,Asn-,Leu-,Ile-,Arg- 或Glu-和X是Cys,R2是Thr,Ser或Asp,R3是Thr,Ser,Asn,Arg,Gln,Lys或Trp,R4是Tyr,R5是R7X或R7的羧基末端残基,其中R7可以是 任何氨基酸和X是Cys,或其酯或酰胺衍生物,或(I)或(II)的生理学上可接受的盐。 这些肽与T4受体结合,并且可用于通过结合T4受体的病毒预防哺乳动物的病毒感染性进行鼻内给药。 据信这些肽作为竞争性阻断剂。