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    USE OF COMPOUNDS WITH COMBINED NEP/MP-INHIBITORY ACTIVITY INTHE PREPARATION OF MEDICAMENTS
    15.
    发明专利
    USE OF COMPOUNDS WITH COMBINED NEP/MP-INHIBITORY ACTIVITY INTHE PREPARATION OF MEDICAMENTS 未知

    公开(公告)号：CA2447598A1

    公开(公告)日：2002-11-28

    申请号：CA2447598

    申请日：2002-05-14

    Applicant: SOLVAY PHARM GMBH

    Inventor： WALDECK HARALD ,  BERGER CLAUDIA ,  FISCHER YVAN ,  HOLTJE DAGMAR ,  ZIEGLER DIETER ,  WESKE MICHAEL

    IPC: C12N15/09 ,  A61K31/00 ,  A61K31/444 ,  A61K31/55 ,  A61K31/675 ,  A61K45/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P25/04 ,  A61P35/00 ,  A61P43/00 ,  C07D223/16 ,  A61K38/55 ,  A61K31/4353

    Abstract: This invention relates to the use of a compound having combined, in particul ar concurrent, inhibitorz activity on neutral endopeptidase (NEP) and on a nove l metalloprotease designated IGS5, or of a pharmaceutically acceptable salt or solvate or biolabile ester thereof, for the manufacture of a medicament (pharmaceutical composition) for treating a larger mammal, preferably a huma n, suffering from or being susceptible to a disease or condition which can be alleviated or prevented by combined or concurrent inhibition of NEP and IGS5 . In a particular aspect the present invention pertains to the use of said compounds with combined or concurrent NEP/IGS5 inhibitory activity for treating a larger mammal, preferably a human, suffering from or being susceptible to a disease or condition where bit-ET-l levels are elevated and which disease or condition can be alleviated or prevented by cobined or concurrent inhibition of NEP and IGS5. In a further particular aspect the present invention pertainsto the use of said compounds with combined or concurrent NEP/IGS5 inhibitory activity for treating a larger mammal, preferably a human, suffering from or being susceptible to a disease or condition where ET-1 is significantly upregulated and which disease or condition can be alleviated or prevented by combined or concurrent inhibitio n of NEP and IGS5. In the present invention said compounds with combined or concurrent NEP/IGS5-inhibitory activity preferably are used for the treatmen t and/or prophylaxis of hypertension, including secondary forms of hypertensio n such as renal or pulmonary hypertension, heart failure, angina pectoris, arrhythmias, myorcadial infarction, cardiac hypertrophy, cerebral ischemia, peripheral vascular disease, subarachnoidal hemorrhage, chronic obstructive pulmonary disease (COPD), asthma, renal disease, atherosclerosis, and pain i n colorectal cancer or prostate cancer, in mammals, preferably in humans, and more preferably in a patient sub-population suffering from or being susceptible to a disease or condition which can be alleviated or prevented b y combined or concurrent inhibition of NEP and IGS5. Furthermore, it may be beneficial to additionally combine the said compounds showing combined or concurrent NEP/IGS5 inhibitory activity with other individual and/or combine d metalloprotease inhibitors than the NEP/IGS5 inhibitors, e.g. with separate ACE- and/or NEP-inhibitors and/or mixed inhibitors of these metalloproteases .

    17BETA-HSD1 E INHIBIDORES STS.
    20.
    发明专利
    17BETA-HSD1 E INHIBIDORES STS. 未知

    公开(公告)号：MX2007014736A

    公开(公告)日：2008-02-15

    申请号：MX2007014736

    申请日：2006-05-24

    Applicant: SOLVAY PHARM GMBH

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

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

    Abstract: La presente invencion se refiere a nuevos derivados de esteroides sustituidos que representan inhibidores selectivos de la enzima 17??-hidroxiesteroide deshidrogenasa tipo I (17??-HSD1) y, ademas, que pueden representar inhibidores del esteroide sulfatasa, asi como a sus sales, a preparaciones farmaceuticas que contienen a estos compuestos y a procedimientos para la preparacion de estos compuestos. Ademas de ello, la invencion concierne al uso terapeutico de dichos nuevos derivados de esteroides sustituidos, en particular a su uso en el tratamiento o la prevencion de enfermedades o trastornos dependientes de hormonas esteroides, tales como enfermedades o trastornos dependientes de la hormona esteroide que requieren la inhibicion de las enzimas 17??-hidroxiesteroide deshidrogenasa tipo I y/o sulfatasa esteroide y/o que requieren la reduccion de la concentracion de 17??-estradiol endogena.

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