CONJUGATES OF MONTELUKAST AND PEPTIDES
    1.
    发明公开

    公开(公告)号:US20230348536A1

    公开(公告)日:2023-11-02

    申请号:US18316496

    申请日:2023-05-12

    摘要: There is provided a peptide-containing compound that comprises a peptide component which is an amino acid sequence of from 2 to 45 (e.g. from 6 to 15) amino acids, which peptide component is covalently bonded to one or more compounds of the formula I:




    wherein:

    R1 is selected from the group consisting of —C(CH3)2OH, —COCH3, —C(CH3)═CH2 and —C(CH3)2H; and
    n is 0, 1 or 2,
    as well as regioisomers, stereoisomers, and pharmaceutically- or cosmetically-acceptable salts of said peptide-containing compound. The compound of formula I is preferably montelukast, montelukast styrene or hydrogenated montelukast styrene. The peptide-containing compound is particularly useful in the treatment of conditions characterised by inflammation, including wounds, hemorrhoids, burns, psoriasis, acne, atopic dermatitis, allergic rhinitis, allergic conjunctivitis, chronic obstructive pulmonary disease, inflammatory bowel disease (such as ulcerative colitis). Compounds of the invention are also useful in the treatment of idiopathic pulmonary fibrosis.

    NEW PEPTIDE-BASED DIAGNOSTIC AND THERAPEUTIC AGENTS

    公开(公告)号:US20240182520A1

    公开(公告)日:2024-06-06

    申请号:US18282362

    申请日:2022-03-17

    IPC分类号: C07K7/06 A61K38/00 A61K51/08

    CPC分类号: C07K7/06 A61K51/088 A61K38/00

    摘要: Provided is a modified peptide compound comprising one or more of the peptide components (a), (b) or (c): (a) a peptide component of formula I, A-Q-B I A and B represent Z or represent A1-1-B1, A1 and B1 independently represent Z or A2-Q2-B2, A2 and B2 independently represent Z or Z-Q3-Z, Q1, Q2 and Q3 represent, for example, Lys and Z represents a peptide component of the amino acid sequence: [W-Lys-X1-Ser-U-X2-Y] n-W-Lys-X1-Ser-U-X2-Y- (SEQ ID No: 3) (b) a peptide component of the amino acid sequence: [Ala-Lys-X1-Ser-U-X2-Y] p-Ala-Lys-X1-Ser-U-X2-Y-G (SEQ ID No: 4); or (c) a peptide component of the amino acid sequence: W1-Lys-X1-Ser-U1-X2-Y-G (SEQ ID No: 5) wherein: n p, W, W1, X1, U, U1, X2, Y and G have meanings given in the description, and wherein the peptide component is modified to include a labelling groups or labelling components that is/are capable of medical imaging of internal regions of the body non-invasively, and/or of diagnosing and/or therapeutically treating one or more diseases (such as cancers) in a patient.

    Conjugates of montelukast and peptides

    公开(公告)号:US11680082B2

    公开(公告)日:2023-06-20

    申请号:US16645355

    申请日:2019-09-14

    摘要: There is provided a peptide-containing compound that comprises a peptide component which is an amino acid sequence of from 2 to 45 (e.g. from 6 to 15) amino acids, which peptide component is covalently bonded to one or more compounds of formula I:




    wherein:



    R1 is selected from the group consisting of —C(CH3)2OH, —COCH3, —C(CH3)═CH2 and —C(CH3)2H; and
    n is 0, 1 or 2,

    as well as regioisomers, stereoisomers, and pharmaceutically- or cosmetically-acceptable salts of said peptide-containing compound. The compound of formula I is preferably montelukast, montelukast styrene or hydrogenated montelukast styrene. The peptide-containing compound is particularly useful in the treatment of conditions characterised by inflammation, including wounds, hemorrhoids, burns, psoriasis, acne, atopic dermatitis, allergic rhinitis, allergic conjunctivitis, chronic obstructive pulmonary disease, inflammatory bowel disease (such as ulcerative colitis). Compounds of the invention are also useful in the treatment of idiopathic pulmonary fibrosis.

    NEW CONJUGATES OF PEPTIDES AND POLYSACCHARIDE

    公开(公告)号:US20230113836A1

    公开(公告)日:2023-04-13

    申请号:US17781543

    申请日:2020-12-02

    摘要: Provided is a conjugate formed between one or more linear polysaccharide chains and a peptide selected from one or more of the peptide components (a), (b), (c) or (d) as defined below: (a) a peptide component of formula (I), A-Q-B I wherein Q represents a structural fragment of formula (II), wherein: the squiggly lines and m have meanings given in the description and A and B have meanings given in the description, but may represent a peptide component of the amino acid sequence: [W-Lys-X1-Ser-U-X2-Y] n-W-Lys-X1-Ser-U-X2-Y--- (SEQ ID No: 3), wherein the dashed line, n, W, X1, U, X2 and Y have meanings given in the description; (b) a peptide component of the amino acid sequence: [Ala-Lys-X1-Ser-U-X2-Y] p-Ala-Lys-X1-Ser-U-X1-Y-G (SEQ ID No: 4) wherein p, G, X1, U, X2 and Y have meanings given in the description; (c) a peptide component of the amino acid sequence: W-Lys-X1-Ser-U-X2-Y-G (SEQ ID No: 5), wherein W, X1, U, X2, Y and G have meanings given in the description; or (d) a peptide component of the amino acid sequence: K-W1-Lys-X1-Ser-U1-X2-Y1-I-J (SEQ ID No: 6), wherein K, W1, U1, Y1, I, J, X1 and X2 have meanings as well as regioisomers, stereoisomers, and pharmaceutically- or cosmetically-acceptable salts of said conjugates, which conjugates are particularly useful in the treatment of conditions characterised by inflammation, including wounds, burns, and disorders of the mucosa, such as anorectal diseases, inflammatory bowel diseases, gynaecological diseases and dental diseases. Preferred linear polysaccharides include hyaluronic acid.

    NEW PEPTIDES
    8.
    发明公开
    NEW PEPTIDES 审中-公开

    公开(公告)号:US20240124521A1

    公开(公告)日:2024-04-18

    申请号:US17642764

    申请日:2020-09-11

    摘要: Provided is a peptide compound comprising the amino acid sequence: G-W-Lys-X1-Ser-U-X2-Y-Z-Q wherein: G represents an optional N-terminal a 3,4-dihydrocinnamic acid group; W represents Ala or Ser, or is absent; U represents Tyr, DOPA or a single bond; X1 and X2 independently represent Pro, Hyp or diHyp; Y represents a single bond or represents a 1 to 5 amino acid sequence, in which the amino acids are selected from one or more of the group Pro, Hyp, diHyp, Thr, DOPA and Tyr; Z represents Pro, Hyp, diHyp, Thr, DOPA or Tyr; and Q represents Lys or is absent, as well as regioisomers, stereoisomers, and pharmaceutically- or cosmetically-acceptable salts of said peptide compound, provided that when G is not present, W represents Ala or is absent and Q represents Lys, then Z represents Pro, Hyp, diHyp or Thr. The compounds are particularly useful in the treatment of conditions characterised by inflammation, including wounds, burns, and disorders of the mucosa, such as anorectal diseases, inflammatory bowel diseases, gynaecological diseases and dental diseases.

    NEW MULTI-FUNCTIONAL OLIGOPEPTIDES
    9.
    发明公开

    公开(公告)号:US20230331792A1

    公开(公告)日:2023-10-19

    申请号:US17781438

    申请日:2020-12-02

    IPC分类号: C07K14/435 A61P17/02 C07K7/06

    摘要: There is provided a compound of formula (I), A-Q-B I wherein Q represents a structural fragment of formula (II), wherein: the squiggly lines and m have meanings given in the description, and wherein A and B have meanings given in the description, but may represent a peptide component of the amino acid sequence: [W-Lys-X1-Ser-U—X2—Y]n—W-Lys-X1-Ser-U—X2—Y— (SEQ ID No: 3) wherein the dashed line, n, W, X1, U, X2 and Y have meanings given in the description, which compounds are useful in medicine, including as pharmaceutical excipients, adhesives and film-forming materials and/or are useful in the treatment of conditions characterised by inflammation, including wounds, burns, and disorders of the mucosa, such as anorectal diseases, inflammatory bowel diseases, gynaecological diseases and dental diseases.