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193 条记录 (耗时 0.016 秒)

    Secnidazole for use in the treatment of sexually transmitted infection
    63.
    发明授权
    Secnidazole for use in the treatment of sexually transmitted infection 有权

    公开(公告)号：US11602522B2

    公开(公告)日：2023-03-14

    申请号：US17314833

    申请日：2021-05-07

    申请人： LUPIN INC.

    发明人： Helen S. Pentikis ,  David Palling ,  Carol J. Braun ,  Richard Holl

    IPC分类号： A61K31/4164 ,  A61K45/06 ,  C07D233/94 ,  A61K31/565 ,  A61K31/567 ,  A61K9/00 ,  A61K9/16 ,  A61K9/50

    摘要： Method of treating sexually transmitted infection in a subject in need thereof involving administering to the subject a therapeutically effective amount of secnidazole in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules having a volume-weighted particle size distribution within a microgranule population, wherein the volume-weighted particle size distribution as measured from a representative sample of the microgranule population comprises (a) 10% of the microgranule population having a volume-weighted particle size about no less than 470 micrometers; (b) 50% of the microgranule population having a volume-weighted particle size between about no less than 640 micrometers and about no more than 810 micrometers; (c) 90% of the microgranule population having a volume-weighted particle size about no more than 1170 micrometers; or (d) a combination thereof, which can include some or all of (a) through (c) above. Pharmaceutical compositions and uses thereof are included herein.

    Antimicrobial drug synthesis and therapeutic compositions
    64.
    发明授权
    Antimicrobial drug synthesis and therapeutic compositions 有权

    公开(公告)号：US11135200B2

    公开(公告)日：2021-10-05

    申请号：US16885585

    申请日：2020-05-28

    申请人： John Malcolm Hall Gregg

    发明人： John Malcolm Hall Gregg

    IPC分类号： A61K31/4164 ,  C07D233/94 ,  A61K45/06 ,  A61K9/00

    摘要： This invention relates to the medical use of an antimicrobial agent, racemic Ornidazole, its (R) and (S) enantiomers, or pharmaceutically acceptable salts or esters thereof, and to methods of treatment which involve treating a subject with Ornidazole. The racemic (rac)-ornidazole, its enantiomers, or pharmaceutically acceptable salts or esters thereof, may be used in combination with other actives. The invention also relates to pharmaceutical formulations and compositions comprising (rac)-ornidazole, (R)-ornidazole, (S)-ornidazole, or pharmaceutically acceptable salts or esters thereof, and/or other actives as well as methods to stereoselectively manufacture the enantiomers.

    SECNIDAZOLE FOR USE IN THE TREATMENT OF SEXUALLY TRANSMITTED INFECTION
    65.
    发明申请
    SECNIDAZOLE FOR USE IN THE TREATMENT OF SEXUALLY TRANSMITTED INFECTION 有权

    公开(公告)号：US20210260038A1

    公开(公告)日：2021-08-26

    申请号：US17314833

    申请日：2021-05-07

    申请人： LUPIN INC.

    发明人： Helen S. PENTIKIS ,  David PALLING ,  Carol J. BRAUN ,  Richard HOLL

    IPC分类号： A61K31/4164 ,  A61K45/06 ,  C07D233/94 ,  A61K31/565 ,  A61K31/567 ,  A61K9/00 ,  A61K9/16 ,  A61K9/50

    摘要： Method of treating a sexually transmitted infection in a subject in need thereof involving administering to the subject a therapeutically effective amount of secnidazole in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules having a volume-weighted particle size distribution within a microgranule population, wherein the volume-weighted particle size distribution as measured from a representative sample of the microgranule population comprises (a) 10% of the microgranule population having a volume-weighted particle size about no less than 470 micrometers; (b) 50% of the microgranule population having a volume-weighted particle size between about no less than 640 micrometers and about no more than 810 micrometers; (c) 90% of the microgranule population having a volume-weighted particle size about no more than 1170 micrometers; or (d) a combination thereof, which can include some or all of (a) through (c) above. Pharmaceutical compositions and uses thereof are included herein.

    SECNIDAZOLE FOR USE IN THE TREATMENT OF TRICHOMONIASIS
    67.
    发明申请
    SECNIDAZOLE FOR USE IN THE TREATMENT OF TRICHOMONIASIS 审中-公开

    公开(公告)号：US20200306228A1

    公开(公告)日：2020-10-01

    申请号：US16901739

    申请日：2020-06-15

    申请人： LUPIN INC.

    发明人： Helen S. PENTIKIS ,  David PALLING ,  Carol J. BRAUN ,  Richard HOLL

    IPC分类号： A61K31/4164 ,  A61K45/06 ,  C07D233/94 ,  A61K31/565 ,  A61K31/567 ,  A61K9/00 ,  A61K9/16 ,  A61K9/50

    摘要： Method of treating trichomoniasis in a subject in need thereof involving administering to the subject a therapeutically effective amount of secnidazole in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules having a volume-weighted particle size distribution within a microgranule population, wherein the volume-weighted particle size distribution as measured from a representative sample of the microgranule population comprises (a) 10% of the microgranule population having a volume-weighted particle size about no less than 470 micrometers; (b) 50% of the microgranule population having a volume-weighted particle size between about no less than 640 micrometers and about no more than 810 micrometers; (c) 90% of the microgranule population having a volume-weighted particle size about no more than 1170 micrometers; or (d) a combination thereof, which can include some or all of (a) through (c) above.

    SECNIDAZOLE FOR USE IN THE TREATMENT OF BACTERIAL VAGINOSIS
    69.
    发明申请
    SECNIDAZOLE FOR USE IN THE TREATMENT OF BACTERIAL VAGINOSIS 审中-公开

    公开(公告)号：US20200206192A1

    公开(公告)日：2020-07-02

    申请号：US16817246

    申请日：2020-03-12

    申请人： LUPIN INC.

    发明人： Helen S. PENTIKIS ,  David PALLING ,  Carol J. BRAUN ,  Richard HOLL

    IPC分类号： A61K31/4164 ,  A61K9/50 ,  A61K9/16 ,  A61K9/00 ,  A61K31/567 ,  A61K31/565 ,  C07D233/94 ,  A61K45/06

    摘要： Method of treating bacterial vaginosis in a subject in need thereof involving administering to the subject a therapeutically effective amount of secnidazole in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules having a volume-weighted particle size distribution within a microgranule population, wherein the volume-weighted particle size distribution as measured from a representative sample of the microgranule population comprises (a) 10% of the microgranule population having a volume-weighted particle size about no less than 470 micrometers; (b) 50% of the microgranule population having a volume-weighted particle size between about no less than 640 micrometers and about no more than 810 micrometers; (c) 90% of the microgranule population having a volume-weighted particle size about no more than 1170 micrometers; or (d) a combination thereof, which can include some or all of (a) through (c) above.

    Method for preparing phenyloxymethyl-nitro-imidazole derivatives and use of same
    70.
    发明授权
    Method for preparing phenyloxymethyl-nitro-imidazole derivatives and use of same 有权

    公开(公告)号：US09758488B2

    公开(公告)日：2017-09-12

    申请号：US14647017

    申请日：2012-11-22

    申请人： SANOFI

    发明人： Zsolt Parkanyi ,  Edit Alattyani ,  Zoltan Bugir ,  Marton Harsanyi

    IPC分类号： C07D233/94

    CPC分类号： C07D233/94

    摘要： Fexinidazole is prepared according to a method which comprises the following steps: a) reacting 1-methyl-2-hydroxymethyl-5-nitro-imidazole with methanesulfonyl chloride in the presence of a suspension of powdered alkaline carbonate in an anhydrous organic solvent suitable for performing nucleophile substitution reactions; b) adding to the resulting reaction medium a solution of 4-methyl-mercapto-phenol in the same organic solvent as referred to in step a); c) separating fexinidazole from the reaction mixture as its hydrochloride salt and d) converting said hydrochloride salt into fexinidazole and optionally, purifying the latter.