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5764 条记录 (耗时 0.038 秒)

    Tissue-selective insulin analogs
    1.
    发明授权
    Tissue-selective insulin analogs 失效
    组织选择性胰岛素类似物

    公开(公告)号：US5268453A

    公开(公告)日：1993-12-07

    申请号：US918953

    申请日：1992-07-30

    申请人： Robin J. Andy ,  Eric R. Larson

    发明人： Robin J. Andy ,  Eric R. Larson

    IPC分类号： A61K38/00 ,  C07K14/62 ,  C07K7/00 ,  A61K37/26 ,  C12P21/06

    CPC分类号： C07K14/62 ,  A61K38/00 ,  Y10S514/866

    摘要： Human insulin analogs are disclosed. These analogs are tissue-selective. Accordingly, pharmaceutical formulations containing the analogs of the invention provide superior clinical benefits as compared to human insulin when used in the treatment of patients suffering from diabetes. The analogs are modified at amino residue A12, A15 or A19, are different from the naturally occurring residue at said position, and are hepatoselective. Also disclosed are human insulin analogs modified at amino acid residues A12 or A14 or amino acid residues A10 and A13 different from naturally occurring residues or residues at said position or positions and are peripheral selective. DNA sequences and microorganisms comprising sequences coding for human insulin analogs are also provided. Processes for preparing the human insulin analogs are described.

    摘要翻译： 人胰岛素类似物被公开。 这些类似物是组织选择性的。 因此，当用于治疗患有糖尿病的患者时，与人胰岛素相比，含有本发明类似物的药物制剂提供了优异的临床益处。 类似物在氨基残基A12，A15或A19处被修饰，与所述位置处的天然存在的残基不同，并且是肝选择性的。 还公开了在氨基酸残基A12或A14处修饰的人胰岛素类似物或在所述位置或位置处与天然存在的残基或残基不同的氨基酸残基A10和A13，并且是周边选择性的。 还提供了包含编码人胰岛素类似物的序列的DNA序列和微生物。 描述了制备人胰岛素类似物的方法。

    TREATMENT WITH SITE SPECIFIC HER2 ANTIBODY-DRUG CONJUGATES
    4.
    发明申请
    TREATMENT WITH SITE SPECIFIC HER2 ANTIBODY-DRUG CONJUGATES 有权

    公开(公告)号：US20230061858A1

    公开(公告)日：2023-03-02

    申请号：US17786722

    申请日：2020-12-17

    申请人： Pfizer Inc.

    发明人： Abraham Leung ,  Matthew Sung

    IPC分类号： A61K47/68 ,  A61P35/00

    摘要： The present disclosure provides for dosing regimens for the treatment of patients with cancer, particularly a HER2-expressing cancer, with an anti-HER2 antibody-drug conjugate (ADC). The present disclosure further provides for methods for the treatment of patients with cancer in which an anti-HER2 ADC is administered. In one embodiment, the anti-HER2 ADC is T(kK183C+K290C)-vc0101 (PF-06804103), in which the antibody T(kK183C+K290C) is linked to the auristatin drug 2-methylalanyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-{[(1S)-2 -phenyl-1-(1,3-thiazol-2-yl) ethyl]amino}propyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide (also known as “0101”) via the cleavable linker maleimidocaproyl-valine-citmlline-p-aminobenzyloxycarbonyl (also known as “vc”).

    PYRAZOLO[1,5-A]PYRAZIN-4-YL DERIVATIVES
    6.
    发明申请
    PYRAZOLO[1,5-A]PYRAZIN-4-YL DERIVATIVES 有权

    公开(公告)号：US20230045252A1

    公开(公告)日：2023-02-09

    申请号：US17939375

    申请日：2022-09-07

    申请人： PFIZER INC.

    发明人： Matthew Frank BROWN ,  Alpay DERMENCI ,  Andrew FENSOME ,  Brian Stephen GERSTENBERGER ,  Matthew Merrill HAYWARD ,  Dafydd Rhys OWEN ,  Stephen Wayne WRIGHT ,  Li Huang XING ,  Xiaojing YANG

    IPC分类号： C07D487/04 ,  A61K31/4985

    摘要： A compound compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A, A′ and A″ are independently O, C═O, C—R′ or N—R″, where R′ and R″ may independently be H, amino, —NR7COR6, COR6, —CONR7R8, C1-C6 alkyl, or hydroxy(C1-C6 alkyl), and R″ may be present or absent, and is present where the rules of valency permit, and where not more than one of A, A′ and A″ is O or C═O; R0 and R are independently H, Br, Cl, F, or C1-C6 alkyl; R1 is H, C1-C6 alkyl, or hydroxy(C1-C6 alkyl); R2 is selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, hydroxy(C1-C6 alkyl), phenyl(C1-C6 alkyl), formyl, heteroaryl, heterocyclic, —COR6, —OCOR6, —COOR6, —NR7COR6, —CONR7R8, and —(CH2)n—W, where W is cyano, hydroxy, C3-C8 cycloalkyl, —SO2NR7R8, and —SO2—R9, where R9 is C1-C6 alkyl, C3-C8 cycloalkyl, heteroaryl, or heterocyclic; wherein each of said alkyl, cycloalkyl, heterocyclic, or heteroaryl may be unsubstituted or substituted by halo, cyano, hydroxy, or C1-C6 alkyl; X is C—R3 or N, where R3 may be H or C1-C6 alkyl; R4 and R5 are independently H, amino, C1-C6 alkyl, or hydroxy(C1-C6 alkyl); R6, R7 and R8 are each independently H, C1-C6 alkyl, C1-C4 alkoxy(C1-C6 alkyl), or C3-C8 cycloalkyl, said C1-C6 alkyl is optionally substituted by halo, CN or hydroxy; or, R7 and R8 together with the atom bonded thereto form a 5- or 6-membered ring, said ring being optionally substituted by halo, hydroxy, CN, or C1-C6 alkyl; and, n is 0, 1, 2 or 3. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.