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    17beta-HSD1 and STS inhibitors
    2.
    发明专利
    17beta-HSD1 and STS inhibitors 未知

    公开(公告)号：AU2006251154B2

    公开(公告)日：2012-06-28

    申请号：AU2006251154

    申请日：2006-05-24

    Applicant: SOLVAY PHARM GMBH

    Inventor： PIRKKALA LILA ,  MESSINGER JOSEF ,  HUSEN BETTINA ,  THOLE HEINRICH-HUBERT ,  WESKE MICHAEL ,  KOSKIMIES PASI

    IPC: C07J41/00 ,  A61K31/565 ,  A61K31/58 ,  A61P5/32 ,  C07J43/00 ,  C07J71/00

    Abstract: The present invention relates to novel substituted steroid derivatives which represent selectiv inhibitors of the 17&bgr;-hydroxysteroid dehydrogenase type I (17&bgr;-HSD1) and, in addition, which may represent inhibitors of the steroid sulphatase, as well as to their salts, to pharmaceutical preparations containing these compounds and to processes for the preparation of these compounds. Furthermore, the invention concerns the therapeutic use of said novel substituted steroid derivatives, particularly their use in the treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17&bgr;-hydroxysteroid dehydrogenase type I and/or steroid sulphatase enzymes and/or requiring the lowering of the endogenous 17&bgr;-estradiol concentration.

    New amidomethyl substituted 1-(carboxyalkyl)-cyclopentylcarbonylamino-benzazepine-n-acetic acid derivatives useful to treat cardiovascular disorders or diseases; hypertension; sexual dysfunction; or neurodegenerative disorders
    10.
    发明专利
    New amidomethyl substituted 1-(carboxyalkyl)-cyclopentylcarbonylamino-benzazepine-n-acetic acid derivatives useful to treat cardiovascular disorders or diseases; hypertension; sexual dysfunction; or neurodegenerative disorders 未知

    公开(公告)号：DE10344848A1

    公开(公告)日：2005-04-14

    申请号：DE10344848

    申请日：2003-09-26

    Applicant: SOLVAY PHARM GMBH

    Inventor： HOELTHE DAGMAR ,  FISCHER YVAN ,  ZIEGLER DIETER ,  WESKE MICHAEL ,  MICHAELIS KATRIN ,  KARIMI-NEJAD YASMIN ,  MESSINGER JOSEF ,  PAHL AXEL ,  HOEFER CONSTANZE

    IPC: A61K38/00 ,  C07K5/02 ,  C07K5/078 ,  C07D223/16 ,  A61K31/55 ,  A61K38/05 ,  C07K5/06

    Abstract: Amidomethyl substituted 1-(carboxyalkyl)-cyclopentylcarbonylamino-benzazepine-n-acetic acid derivatives (I) and their salts are new. Amidomethyl substituted 1-(carboxyalkyl)-cyclopentylcarbonylamino-benzazepine-n-acetic acid derivatives of formula (I) and their salts are new. [Image] R 1>, R 4>H or a group forming a biolabile ester; and either R 2>H, 1-4C alkyl or 1-4C hydroxyalkyl (where the OH is optionally esterified with 2-4C alkanoyl or an amino acid residue); and R 3>1-4C alkyl, 1-4C alkoxy-1-4C alkyl; 1-4C hydroxyalkyl (optionally substituted by a second hydroxyl group and the hydroxyl groups of which are each optionally esterified with 2-4C alkanoyl or an amino acid residue); (0-4C alkyl) 2amino-1-6C alkyl, 3-7C cycloalkyl(1-4C alkyl), phenyl-1-4C alkyl or phenylcarbonylmethyl (where the phenyl group is optionally substituted 1-2 times by 1-4C alkyl, 1-4C alkoxy and/or halo), naphthyl-1-4C alkyl, 3-6C oxoalkyl or 2-oxoazepanyl; or R 2> + R 3>4-7C alkylene (where the methylene groups are optionally replaced 1-2 times by carbonyl, nitrogen, oxygen and/or sulfur and/or which are optionally substituted once by OH, which is optionally esterified with 2-4C alkanoyl or an amino acid residue), 1-4C alkyl; 1-4C hydroxyalkyl (where the OH group is optionally esterified with 2-4C alkanoyl or an amino acid residue); phenyl or benzyl. Independent claims are also included for: (1) preparation of (I); and (2) a carboxyalkyl-cyclopentylcarbonylamino-benzazepine-n-acetic acid derivatives of formula (II). [Image] R 1> 0> 1>, R 4> 0> 1>an acid-protecting group. ACTIVITY : Cardiovascular-Gen.; Hypotensive; Nephrotropic; Respiratory-Gen.; Endocrine-Gen.; Vasotropic; Neuroprotective; Cerebroprotective; Antiinflammatory; Nootropic; Antiarteriosclerotic; Anti-HIV; Muscular-Gen.; Anticonvulsant; Vulnerary; Antiparkinsonian; Antiinflammatory; Hepatotropic; Antibacterial; Virucide; CNS-Gen.; Dermatological; Antiemetic; Cytostatic; Gastrointestinal-Gen.; Antiulcer; Antimicrobial; Immunosuppressive; Antialcoholic; Antiarthritic; Osteopathic; Immunostimulant; Hemostatic; Antirheumatic; Cardiant; Antithyroid; Anabolic; Hypertensive; Antidiabetic; Antipsoriatic; Gynecological; Antiallergic; Auditory; Antianemic; Antiseborrheic; Keratolytic; Vasotropic; Anticoagulant; Vulnerary; Ophthalmological; Metabolic; Protozoacide; Fungicide; Antidote; Antirheumatic. MECHANISM OF ACTION : Neutral endopeptidase (NEP) inhibitor; Human soluble endopeptidase (hSEP) inhibitor. The ability of (I) to inhibit (NEP) was assessed in vitro. The results showed that median inhibitory concentration (IC 5 0) value of (I) was less than 1 nM.

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