中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

188 records (took 0.023 seconds)

    7.
    发明专利
    未知

    公开(公告)号：NO330294B1

    公开(公告)日：2011-03-21

    申请号：NO20052414

    申请日：2005-05-19

    Applicant: SERVIER LAB

    Inventor： NANTEUIL GUILLAUME DE ,  BENOIST ALAIN ,  COMBETTES MURIELLE ,  HARLEY ELISZABETH

    IPC: C07D207/06 ,  C07D295/18 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/426 ,  A61K31/427 ,  A61K31/438 ,  A61P3/10 ,  A61P43/00 ,  C07D207/10 ,  C07D207/16 ,  C07D277/06 ,  C07D277/12 ,  C07D295/185 ,  C07D311/96 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    Abstract: Spiro-cycloalkyl N-acyl pyrrolidine or thiazolidine derivatives (I), their optical isomers and acid addition salts are new. Spiro-cycloalkyl N-acyl pyrrolidine or thiazolidine derivatives of formula (I), and their optical isomers and acid addition salts, are new. X 1CR 4aR 4b, O, S(O) q1 or NR 5; R 4a and R 4bhydrogen or 1-6 C linear or branched alkyl or together complete a 3-7C cycloalkyl; q1 : 0-2; R 5hydrogen or 1-6C linear or branched alkyl, optionally substituted by hydroxy; m1 : 0-4; m2 : 1-4; n1 and n2 : 1-3; R 1hydrogen, carboxy, 1-6C linear or branched alkoxycarbonyl, carbamoyl (optionally substituted by 1 or 2 1-6C linear or branched alkyl), or 1-6C linear or branched alkyl (optionally substituted by hydroxy) or amino (optionally substituted by 1 or 2 1-6C linear or branched alkyl); R 2hydrogen or 1-6C linear or branched alkyl; Ak : 1-4C linear or branched alkylene, optionally substituted by one or more halo, particularly fluoro; p : 0-2; R 3hydrogen or cyano; X 2 and X 3S(O) q2 or CR 6aR 6b; R 6a and R 6bhydrogen or halo, preferably fluoro, or R 6a = hydrogen and R 6b = hydroxy; and q2 : 0-2. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : Antidiabetic; Anorectic. MECHANISM OF ACTION : Inhibition of dipeptidyl-peptidase IV (DPPIV). The compound (2S)-1-({[9-(hydroxymethyl)-3-oxaspiro[5,5]undec-9-yl]amino}acetyl)-2-pyrrolidinecarbonitrile had IC 50 76.1 nM against porcine renal DPPIV, in an assay based on cleavage of Gly-Pro-p-nitroanilide.

    10.
    发明专利
    未知

    公开(公告)号：AT476416T

    公开(公告)日：2010-08-15

    申请号：AT08290885

    申请日：2008-09-19

    Applicant: SERVIER LAB

    Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  GLOANEC PHILIPPE ,  PARMENTIER JEAN-GILLES ,  BENOIST ALAIN ,  VERBEUREN TONY ,  RUPIN ALAIN ,  COURCHAY CHRISTINE ,  SIMONET SERGE

    IPC: C07D207/09 ,  A61K31/385 ,  A61K31/40 ,  C07D209/42 ,  C07D209/52 ,  C07D217/26 ,  C07D233/36 ,  C07D271/08

    Abstract: Compounds e.g. perindopril-ethoxycarbonyl-butyl-amino-propionyl-octahydro-indole-2-carboxylic acid (I) are new. Compounds e.g. perindopril-ethoxycarbonyl-butyl-amino-propionyl-octahydro-indole-2-carboxylic acid of formula (A) m(B1) n(I) are new. A : angiotensin converting enzyme inhibitor moiety comprising at least one basic functional group; B1 : a moiety comprising at least one acid functional group and at least one NO donor group; m : number of acid functional group of B1; and n : number of basic functional groups of A, where A and B1 are ionic type. Independent claims are included for: (1) alkyl compounds of formula X-(AK 1) x-(Y 1) y-(Ak 2) z-Z (III); and (2) preparation of (I). X : CO 2H, SO 3H or P(O)(OH) 2; Ak 1, Ak 2 : 1-8C alkylene (optionally branched and optionally saturated, where one or more C atom is replaced by O, S, N or SO 2, and optionally substituted by carboxy, OH or amino); x, y, z : 0 or 1; Y 1 : CO or CONH; Z : 4-benzenesulfonyl-5-oxy-furazan-3-oxo moiety of formula (a) or (b); and R 4, R1a 4 : H, halo, 1-6C alkyl, CF 3or -OCF 3. [Image] ACTIVITY : Cardiovascular-Gen.; Hypotensive; Nephrotropic; Vasotropic; Cardiant; Antiarteriosclerotic; Prevention: Anticoagulant; Thrombolytic; Antimicrobial; Cerebroprotective; Antidiabetic; Antiinflammatory; Tranquilizer; Metabolic; Anorectic. MECHANISM OF ACTION : Angiotensin converting enzyme inhibitor. The effect of (I) to inhibit angiotensin converting enzyme was tested in rats. The result showed that (2S)-2-[(3-{[5-oxido-4-(phenylsulfonyl)-1,2,5-oxadiazol-3-yl]-oxy}-propionyl)-amino]-succinic acid-(2S,3as,7aS)-1-[(2S)-2-{[(1S)-1-(ethoxycarbonyl)-butyl]-amino}-propionyl]-octahydro-1H-indole-2-carboxylic acid exhibited 80-85% of inhibition.

Patent Agency Ranking