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    New amidomethyl substituted 1-(carboxyalkyl)-cyclopentylcarbonylamino-benzazepine-n-acetic acid derivatives useful to treat cardiovascular disorders or diseases; hypertension; sexual dysfunction; or neurodegenerative disorders
    33.
    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.

    34.
    发明专利
    未知

    公开(公告)号：AT276254T

    公开(公告)日：2004-10-15

    申请号：AT02013861

    申请日：2002-06-22

    Applicant: SOLVAY PHARM GMBH

    Inventor： SCHOEN UWE ,  MESSINGER JOSEF ,  BRUECKNER REINHARD ,  ZIEGLER DIETER

    IPC: A61K31/435 ,  A61K31/439 ,  A61P9/00 ,  A61P9/06 ,  C07D221/00 ,  C07D471/08 ,  C07D471/10

    Abstract: 7-Alkyl-3-(substituted phenyl)-9,9-(dialkyl or alkylene)-3,7-diazabicyclo (3.3.1) nonane derivatives (I) are new. Diazabicyclononane derivatives of formula (I) and their acid addition salts are new. R1 = 1-6C alkyl or 4-7C cycloalkylalkyl; R2, R3 = 1-4C alkyl; or R2 + R3 = 3-6C alkylene; and R4 = phenyl (monosubstituted in the ortho- or para-position by NO2, CN or 2-5C alkanoyl) or 2,4-dinitrophenyl. An Independent claim is also included for the preparation of (I).

    36.
    发明专利
    未知

    公开(公告)号：PT958496E

    公开(公告)日：2003-02-28

    申请号：PT98905382

    申请日：1998-02-02

    Applicant: SOLVAY PHARM GMBH

    Inventor： MESSINGER JOSEF ,  GUNDLACH FRANK ,  SINNER ERNST

    IPC: B01D15/00 ,  B01D15/08 ,  G01N30/46

    Abstract: The invention relates to a device or equipment as well as to a method for the simultaneous, fractionating operation of a plurality of parallel chromatographic columns. It is particularly advantageous to apply this equipment and method in research, in the framework of organic synthesis for simultaneous, parallel separation, isolation and purification of a plurality of chemical compounds, e.g. of potential new active ingredients for medicaments, particularly also on the semi-preparative scale.

    38.
    发明专利
    未知

    公开(公告)号：DE59805688D1

    公开(公告)日：2002-10-31

    申请号：DE59805688

    申请日：1998-02-02

    Applicant: SOLVAY PHARM GMBH

    Inventor： MESSINGER JOSEF ,  GUNDLACH FRANK ,  SINNER ERNST

    IPC: B01D15/00 ,  B01D15/08 ,  G01N30/46

    Abstract: The invention relates to a device or equipment as well as to a method for the simultaneous, fractionating operation of a plurality of parallel chromatographic columns. It is particularly advantageous to apply this equipment and method in research, in the framework of organic synthesis for simultaneous, parallel separation, isolation and purification of a plurality of chemical compounds, e.g. of potential new active ingredients for medicaments, particularly also on the semi-preparative scale.

    39.
    发明专利
    未知

    公开(公告)号：DK0958496T3

    公开(公告)日：2002-10-14

    申请号：DK98905382

    申请日：1998-02-02

    Applicant: SOLVAY PHARM GMBH

    Inventor： MESSINGER JOSEF ,  GUNDLACH FRANK ,  SINNER ERNST

    IPC: B01D15/00 ,  B01D15/08 ,  G01N30/46

    Abstract: The invention relates to a device or equipment as well as to a method for the simultaneous, fractionating operation of a plurality of parallel chromatographic columns. It is particularly advantageous to apply this equipment and method in research, in the framework of organic synthesis for simultaneous, parallel separation, isolation and purification of a plurality of chemical compounds, e.g. of potential new active ingredients for medicaments, particularly also on the semi-preparative scale.

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