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    TREATMENT OF CARDIOPULMONARY DISORDERS
    1.
    发明公开
    TREATMENT OF CARDIOPULMONARY DISORDERS 审中-公开

    公开(公告)号：US20240148715A1

    公开(公告)日：2024-05-09

    申请号：US18506944

    申请日：2023-11-10

    申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

    发明人： Eva Maria BECKER-PELSTER ,  Hanna TINEL ,  Michael HAHN ,  Dieter LANG ,  Gerrit WEIMANN ,  Johannes NAGELSCHMITZ ,  Lisa DIETZ ,  Soundos SALEH ,  David JUNG ,  Ildiko TEREBESI ,  Tobias MUNDRY ,  Annett RICHTER ,  Britta OLENIK ,  Birgit KEIL ,  Bernd RÖSLER ,  Peter FEY ,  Heiko SCHIRMER ,  Guido BECKER ,  Clemens BOTHE ,  Helene FABER ,  Julian EGGER ,  Mark PARRY ,  David WARD ,  Cecile VITRE

    IPC分类号： A61K31/47 ,  A61K9/00 ,  A61P9/12

    CPC分类号： A61K31/47 ,  A61K9/0075 ,  A61P9/12

    摘要： The present invention relates to the use of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), prefer-ably in form of one of its salts or solvates or hydrates, preferably (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (I) of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)-ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid inform of mono hydrate (II) of formula (I-M-II), in the inhalative treatment of cardiopulmonary and pulmonary disorders, such as pulmonary arterial hypertension (P AH), chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary hypertension (PH) associated with chronic lung disease (PH group 3) such as pulmonary hypertension in chronic obstructive pulmonary disease (PH-COPD) and pulmonary hypertension with idiopathic interstitial pneumonia (PH-IIP), characterized in that an inhalative dosage form comprising 240 to 4000 μg, preferably 480 to 2000 μg of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably in form of monohydrate I of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid in form of mono hydrate (II) of formula (I-M-II), is administered to a patient in need thereof once or twice daily for a period of at least two consecutive days, preferably at least 2 to 7 consecutive days, preferably for a period of at least 14 consecutive days, in particular from after onset of treatment for the whole course of the disease, wherein the inhalative dosage form preferably comprises the combination of the active ingredient and a pharmaceutically suitable excipient or carrier, while preferably the active ingredient and a pharmaceutically suitable excipient are filled in a hard capsule.

    NOVEL SALTS
    5.
    发明申请
    NOVEL SALTS 有权
    新的口水

    公开(公告)号：US20160289220A1

    公开(公告)日：2016-10-06

    申请号：US15035165

    申请日：2014-11-05

    申请人： Bayer Pharma Aktiengesellschaft

    发明人： Britta OLENIK ,  Birgit KEIL ,  Martin-Holger HINZ ,  Chantal FURSTNER ,  Mario JESKE ,  Jens ACKERSTAFF

    IPC分类号： C07D413/04 ,  C07C229/26

    CPC分类号： C07D413/04 ,  C07C229/26

    摘要： Salts of 1-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)-2,4-dioxo-3-[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid of the formula (I), in particular amino acid salts such as the lysine salt and alkali metal salts such as the sodium salt and the potassium salt, processes for their preparation, medicaments comprising them and their use for controlling diseases.

    摘要翻译： 1-（3-甲基-2-氧代-2,3-二氢-1,3-苯并恶唑-6-基）-2,4-二氧代-3 - [（1R）-4-（三氟甲基）-2 ，3-二氢-1H-茚-1-基] -1,2,3,4-四氢嘧啶-5-甲酸，特别是氨基酸盐如赖氨酸盐和碱金属盐，如 作为钠盐和钾盐，其制备方法，包含它们的药物及其用于控制​​疾病的用途。