Macrocyclic lactone compounds and methods for their use

    公开(公告)号:US10123996B2

    公开(公告)日:2018-11-13

    申请号:US15181284

    申请日:2016-06-13

    Abstract: A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 and M7 are each independently a member selected from the group consisting of H, C1-6 alkyl, OH and C1-6 hydroxyalkyl; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: wherein each M8 is independently a member selected from the group consisting of C1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L2 and L3 are independently selected from the group consisting of: and salts, isomers, or N-oxides thereof.

    LUMINAL PROSTHESES AND METHODS FOR COATING THEREOF

    公开(公告)号:US20190070334A1

    公开(公告)日:2019-03-07

    申请号:US15910779

    申请日:2018-03-02

    Abstract: Luminal prostheses comprise scaffolds having coatings adhered to at least a portion of their outer surfaces. The surfaces are modified to enhance binding of the coatings. For example, the surfaces may be microblasted, laser treated, chemically etched, exposed to plasma, or exposed to a corona discharge, allowing a polymeric coating to adhere to the scaffold more tightly than in the absence of the surface modification. The coatings can be used to deliver therapeutic or other agents dispersed therein.

    MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE
    4.
    发明申请
    MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE 审中-公开
    MACROCYCLIC LACTONE化合物及其使用方法

    公开(公告)号:US20150352089A1

    公开(公告)日:2015-12-10

    申请号:US14831747

    申请日:2015-08-20

    Abstract: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 and M7 are each independently a member selected from the group consisting of H, C1-6 alkyl, OH and C1-6 hydroxyalkyl; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: wherein each M8 is independently a member selected from the group consisting of C1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L2 and L3 are independently selected from the group consisting of: and salts, hydrates, isomers, metabolites N-oxides and prodrugs thereof.

    Abstract translation: 本发明提供包含药学上可接受的赋形剂和下式化合物的药物组合物:其中R1,R2,R3,R5,R6,R8,M1,M2,M3,M4,M5,M6和M7各自独立地为成员 选自H,C 1-6烷基,OH和C 1-6羟基烷基; R 4,R 7和R 9各自独立地选自C 1-6烷氧基和OH; R 10是选自H,-OH,-OP(O)Me 2,-O-(CH 2)n -OH和-O-(CH 2)m -O-(CH 2)o -CH 3的成员,其中 下标n和m各自独立地为2至8,下标o为1至6; L1和L4各自独立地选自:其中每个M8独立地是选自C 1-6烷基,OH和C 1-6羟基烷基的成员; L2和L3中的每一个独立地选自:盐,水合物,异构体,代谢物N-氧化物和前药。

    MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE

    公开(公告)号:US20230165839A1

    公开(公告)日:2023-06-01

    申请号:US17941888

    申请日:2022-09-09

    Abstract: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula:




    wherein R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 and M7 are each independently a member selected from the group consisting of H, C1-6 alkyl, OH and C1-6 hydroxyalkyl; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2,




    —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of:




    wherein each M8 is independently a member selected from the group consisting of C1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L2 and L3 are independently selected from the group consisting of:




    and salts, hydrates, isomers, metabolites, N-oxides and prodrugs thereof.

    MACROCYCLIC LACTONE COMPOUNDS AND METHODS FOR THEIR USE

    公开(公告)号:US20210008040A1

    公开(公告)日:2021-01-14

    申请号:US16879115

    申请日:2020-05-20

    Abstract: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 and M7 are each independently a member selected from the group consisting of H, C1-6 alkyl, —OH and C1-6 hydroxyalkyl; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: wherein each M8 is independently a member selected from the group consisting of C1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L2 and L3 are independently selected from the group consisting of: and salts, hydrates, isomers, metabolites, N-oxides and prodrugs thereof.

    Macrocyclic lactone compounds and methods for their use

    公开(公告)号:US10695327B2

    公开(公告)日:2020-06-30

    申请号:US16154501

    申请日:2018-10-08

    Abstract: A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 and M7 are each independently a member selected from the group consisting of H, C1-6 alkyl, OH and C1-6 hydroxyalkyl; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: wherein each M8 is independently a member selected from the group consisting of C1-6 alkyl, OH and C1-6 hydroxyalkyl; each of L2 and L3 are independently selected from the group consisting of: and salts, isomers, or N-oxides thereof.

    ANTICOAGULANT COMPOUNDS, METHODS AND DEVICES FOR OPHTHALMIC USE

    公开(公告)号:US20230293540A1

    公开(公告)日:2023-09-21

    申请号:US18179160

    申请日:2023-03-06

    Abstract: Devices, formulations, compositions, and methods are provided for inhibiting an inflammatory ophthalmic disease or eye condition in a patient. A therapeutic composition comprising a direct factor Xa inhibitor and/or a direct factor II inhibitor is provided. A therapeutically effective dose of the therapeutic composition is delivered to a site of the inflammatory ophthalmic disease or condition in the patient’s eye(s). The therapeutic composition may be formulated for delivery to the patient by via injection, an implant, an eye drop, an emulsion, a suspension, an ointment, a nanomicelle, a nanoparticle, a nanosuspension, a liposome, an in-situ gel, a contact lens, or a microneedle or the like. The therapeutic composition may include one or more additional therapeutically active substances and/or one or more additional pharmaceutical agents. The one or more additional therapeutically active substances and/or one or more additional pharmaceutical agents may be delivered together with the direct factor Xa inhibitor and/or direct factor IIa inhibitor, or separately from the direct factor Xa inhibitor and/or direct factor IIa inhibitor.

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