会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 3. 发明授权
    • Gamma-conopeptides
    • 伽玛肽
    • US06624288B1
    • 2003-09-23
    • US09210952
    • 1998-12-15
    • Michael FainzilberKarel S. KitsAlma L. BurlingameBaldomero M. OliveraCraig WalkerMaren WatkinsReshma ShettyLourdes J. CruzJulita ImperialClark Colledge
    • Michael FainzilberKarel S. KitsAlma L. BurlingameBaldomero M. OliveraCraig WalkerMaren WatkinsReshma ShettyLourdes J. CruzJulita ImperialClark Colledge
    • C07K500
    • C07K14/43504A61K38/00
    • This invention relates to relatively short peptides about 25-40 residues in length, which are naturally available in minute amounts in the venom of the cone snails or analogs to the naturally available peptides, and which include three cyclizing disulfide linkages and one or more &ggr;-carboxyglutamate residues. More specifically, the present invention is directed to &ggr;-conopeptides having the general formula I: Xaa1-Cys-Xaa2-Cys-Xaa3-Xaa4-Cys-Cys-Xaa5-Cys-Xaa6-Cys-Xaa7 (SEQ ID NO:1), as described herein; or having the general formula II: Xaa1-Cys-Xaa2-Cys-Xaa3-Xaa4-Cys-Cys-Xaa5-Xaa6-Cys-Xaa7-Cys-Xaa8 (SEQ ID NO:2), as defined herein; or having the general formula III: Xaa1-Cys-Xaa2-Cys-Xaa3-Xaa4-Xaa5-Cys-Cys-Ser-Asn-Ser-Cys-Asp-Xaa2-Cys-Xaa7 (SEQ ID NO:3), as described herein; or having the general formula IV: Xaa1-Cys-Xaa2-Cys-Xaa3-Xaa4-Xaa5-Cys-Cys-Ser-Asn-Ser-Cys-Asp-Xaa6-Cys-Xaa7 (SEQ ID NO:4), as described herein; or having the general formula V: Xaa1-Xaa2-Cys-Xaa3-Xaa4-Phe-Xaa5-Cys-Thr-Xaa6-Ser-Xaa7-Cys-Cys-Ser-Asn-Ser-Cys-Asp-Gln-Thr-Tyr-Cys-Xaa8-Leu-Xaa9 (SEQ ID NO:5), as described herein. The invention further relates to specific &ggr;-conopeptides, specific pro-&ggr;-conopeptides and nucleic acids encoding the pro-&ggr;-conopeptides. The invention also includes pharmaceutically acceptable salts of the conopeptides. These conopeptides are useful as agonists of neuronal pacemaker calcium channels.
    • 本发明涉及长度约25-40个残基的相对较短的肽,其在锥形蜗牛的毒液中或天然存在的肽的类似物中天然可用量少,并且其包括三个环化二硫键和一个或多个γ- 羧基谷氨酸残基。 更具体地,本发明涉及具有通式I的X射线衍生肽:Xaa1-Cys-Xaa2-Cys-Xaa3-Xaa4-Cys-Cys-Xaa5-Cys-Xaa6-Cys-Xaa7(SEQ ID NO:1) ,如本文所述; 或具有如本文所定义的通式II:Xaa1-Cys-Xaa2-Cys-Xaa3-Xaa4-Cys-Cys-Xaa5-Xaa6-Cys-Xaa7-Cys-Xaa8(SEQ ID NO:2) 或具有通式III:Xaa1-Cys-Xaa2-Cys-Xaa3-Xaa4-Xaa5-Cys-Cys-Ser-Asn-Ser-Cys-Asp-Xaa2-Cys-Xaa7(SEQ ID NO:3) 在这里 或具有通式IV:Xaa1-Cys-Xaa2-Cys-Xaa3-Xaa4-Xaa5-Cys-Cys-Ser-Asn-Ser-Cys-Asp-Xaa6-Cys-Xaa7(SEQ ID NO:4) 在这里 或具有通式V:Xaa1-Xaa2-Cys-Xaa3-Xaa4-Phe-Xaa5-Cys-Thr-Xaa6-Ser-Xaa7-Cys-Cys-Ser-Asn-Ser-Cys-Asp-Gln-Thr-Tyr -Cys-Xaa8-Leu-Xaa9(SEQ ID NO:5),如本文所述。 本发明进一步涉及具体的γ-配体肽,特异性前-γ-肽和编码前γ-多肽的核酸。 本发明还包括肽的药学上可接受的盐。 这些肽可用作神经元起搏器钙通道的激动剂。
    • 5. 发明授权
    • 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
    • 1H-吡咯并[2,3-D]嘧啶衍生物及其使用方法
    • US07429596B2
    • 2008-09-30
    • US10871732
    • 2004-06-18
    • Masahiro TanakaChao ZhangKevan M. ShokatAlma L. BurlingameKirk HansenRaynard L. BatemanStephen G. DiMagno
    • Masahiro TanakaChao ZhangKevan M. ShokatAlma L. BurlingameKirk HansenRaynard L. BatemanStephen G. DiMagno
    • C07D487/04C07D413/06A61K31/519A61K31/675A61K31/662A61K31/497A61K31/5355C07F9/38A61P35/04A61P35/02
    • C07D487/04
    • This invention generally relates to pyrazolo pyrimidine derivatives useful as inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. The invention further relates to pharmaceutical compositions and methods of preventing or treating disease with 1H-Pyrrolo[2.3-d]pyrimidine derivatives. More specifically, the invention relates to a 1H-Pyrrolo[2.3-d]pyrimidine which is a compound of Formula I or II: or a pharmaceutically-acceptable salt or prodrug thereof; wherein: Y is N or CR5; Z is NR3R4, halo, H, OH, alkyl, alkyloxy, or haloalkyl; and R1a is indolyl, thiazolyl, benzyl, biphenylyl, thiophenyl, pyrrolyl, or phenyl, wherein said phenyl is substituted with at least one of OH, —NR3R4, —C(═O)NR6R7, —CN, NO2—C(═O)OH, —C(═O)O-alkyl, (C1-C4)alkyl, halo, haloalkyl or haloaryl; and wherein said indolyl, thiazolyl, benzyl, biphenylyl, thiophenyl, or pyrrolyl is optionally substituted with OH, —NR3R4, —C(═O)NR6R7, —CN, NO2, —C(═O)O—R3, (C1-C4)alkyl, halo, haloalkyl or haloaryl.
    • 本发明一般涉及可用作NAD(P)(H)依赖性氧化还原酶的短链脱氢酶/还原酶(SDR)家族的抑制剂的吡唑并嘧啶衍生物。 本发明还涉及用1H-吡咯并[2,3-d]嘧啶衍生物预防或治疗疾病的药物组合物和方法。 更具体地,本发明涉及作为式I或II化合物的1H-吡咯并[2,3-d]嘧啶或其药学上可接受的盐或前药; 其中:Y是N或CR 5; Z是NR 3 R 4,卤素,H,OH,烷基,烷氧基或卤代烷基; 并且R 1a是吲哚基,噻唑基,苄基,联苯基,噻吩基,吡咯基或苯基,其中所述苯基被OH,-NR 3 R 3中的至少一个取代, -C(-O)NR 6 R 7,-CN,NO 2 -C(-O(O) )OH,-C(-O)O-烷基,(C 1 -C 4 -C 4)烷基,卤素,卤代烷基或卤代芳基; 并且其中所述吲哚基,噻唑基,苄基,联苯基,噻吩基或吡咯基任选被OH,-NR 3 R 4,-C( - )NR -C(O)OR 3,-C(-O)OR 3,(C 1 -C 6) C 1 -C 4烷基,卤素,卤代烷基或卤代芳基。