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    3.
    发明专利
    未知

    公开(公告)号：DK1413579T3

    公开(公告)日：2005-05-09

    申请号：DK03292634

    申请日：2003-10-22

    Applicant: SERVIER LAB

    Inventor： KOPP MARINA ,  LANCELOT JEAN-CHARLES ,  LEMAITRE STEPHANE ,  CAIGNARD DANIEL-HENRI ,  BIZOT-ESPIARD JEAN-GUY ,  RAULT SYLVAIN ,  RENARD PIERRE

    IPC: A61K31/381 ,  A61K31/402 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/44 ,  A61K31/4439 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06

    Abstract: Imidazoline derivatives (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new. Imidazoline derivatives of formula (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new: R1 = heteroaryl optionally substituted by T1; R2 = cycloalkyl optionally substituted by T1; T1 = halogen, alkyl, alkoxy, OH, CN, NO2, (di)(alkyl)amino, COOH, COO-alkyl or CONH2-C(O)Rd; Rd = OH, alkoxy or amino; R4 , R5 = H, halogen, (polyhalo)alkyl, R10-C(X)-R11-, R10-Y-C(X)-R11-, R11-Y-R11-, or R10-S-(O)n-R11-; R11 = a bond, alkylene, alkenylene or alkynylene; X = O, S, or NR12; R3, R10, R12 = H or alkyl; Y = O, S or (alkyl)amino; and n = 1 or 2. Alkyl, alkoxy and alkylene have 1-6C, alkenylene have 2-6C and 1-3 double bonds, alkynylene have 2-6C and 1-3 triple bonds, polyhaloalkyl have 1-3C and 1-7 halogens, heteroaryl has 5 - 11 members and is mono or bicyclic with at least one aromatic ring and with 1-3 heteroatoms selected from O, N and S and may be substituted by an oxo group on a non-aromatic part of the structure, cycloalkyl has 3-10C, is mono or bicyclic and may have 1 or 2 unsaturations. An Independent claim is also included for the preparation of (I).

    New dihydroimidazolylaminopyridine derivatives useful in the treatment of diabetes, obesity, insulin resistance and glucose intolerance
    4.
    发明专利
    New dihydroimidazolylaminopyridine derivatives useful in the treatment of diabetes, obesity, insulin resistance and glucose intolerance 未知

    公开(公告)号：FR2846655A1

    公开(公告)日：2004-05-07

    申请号：FR0213801

    申请日：2002-11-05

    Applicant: SERVIER LAB

    Inventor： RAULT SYLVAIN ,  KOPP MARINA ,  LANCELOT JEAN CHARLES ,  LEMAITRE STEPHANE ,  PFEIFFER BRUNO ,  BIZOT ESPIARD JEAN GUY ,  RENARD PIERRE

    IPC: A61P3/04 ,  A61P3/10 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D413/14 ,  A61K31/4439 ,  C07D401/14

    Abstract: 3-Dihydroimidazolyl-2-aminopyridine derivatives (I) their enantiomers, diastereoisomers, tautomers, and salts with acids and bases are new. 3-Dihydroimidazolyl-2-aminopyridine derivatives (I) their enantiomers, diastereoisomers, tautomers, and salts with acids and bases are new; R1, R2 = H, alkyl, cycloalkyl, aryl (optionally substituted), heteroaryl (optionally substituted), or Ra-C(Y)-; NR1R2 = aromatic or non-aromatic heterocycle of 5-8 members including 1-3 heteroatoms (O, N, S)and optionally substituted by 1 or 2 groups selected from halogens, alkyl, polyhaloalkyl, alkoxy, OH, CN, NO2, amino, mono- or di-alkylamino, -COOH, -COO-alkyl, or -CONH2; Ra = H, alkyl, alkoxy, aryl (optionally substituted), or heteroaryl (optionally substituted); Y = O, S, or NRb; Rb = H or alkyl; R3 = H, alkyl, alkoxy, OH, CN, NO2, amino, mono- or di-alkylamino, -COOH, -COO-alkyl, or -CONH2; R4, R5 = H or alkyl; X = O, S, or NRe; Re = H or alkyl. With the proviso that (I) is not 3-(4,5-dihydro-1H-imidazol-2-yl)-2-pyridinamine, 3-(4,5-dihydro-1H-imidazol-2-yl)-N-phenyl-2-pyridinamine, 3-(4,5-dihydro-1H-imidazol-2-yl)-N-methyl-2-pyridinamine, or N-(3-(4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl)-2-pyridinyl)-N-phenylamine. In the above definitions, alkyl and alkoxy groups have 1-6 C atoms, polyhaloalkyl groups have 1-3 C atoms and 1-7 halogen atoms, heteroaryl groups have 5-11 members, are mono- or bicyclic, at least one of which is aromatic, and have 2 or 3 heteroatoms (O, N, S), cycloalkyl groups are mono- or bicyclic with 3-10 C atoms and optionally 1 or 2 unsaturations, and optional substituents on cycloalkyl and heteroaryl groups are 1 or 2 groups selected from halogens, alkyl, alkoxy, polyhaloalkyl, OH, CN, NO2, NH2, alkylamino, dialkylamino, -COOH, -COO-alkyl, -CONH2, and non-aromatic rings on heteroaryl groups may also be substituted by oxo. An Independent claim is also included for the preparation of (I).

    5.
    发明专利
    未知

    公开(公告)号：FR2846328A1

    公开(公告)日：2004-04-30

    申请号：FR0213194

    申请日：2002-10-23

    Applicant: SERVIER LAB

    Inventor： RAULT SYLVAIN ,  KOPP MARINA ,  LANCELOT JEAN CHARLES ,  LEMAITRE STEPHANE ,  CAIGNARD DANIEL HENRI ,  BIZOT ESPIARD JEAN GUY ,  RENARD PIERRE

    IPC: A61K31/381 ,  A61K31/402 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/44 ,  A61K31/4439 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  A61K31/4025 ,  A61K31/4402

    Abstract: Imidazoline derivatives (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new. Imidazoline derivatives of formula (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new: R1 = heteroaryl optionally substituted by T1; R2 = cycloalkyl optionally substituted by T1; T1 = halogen, alkyl, alkoxy, OH, CN, NO2, (di)(alkyl)amino, COOH, COO-alkyl or CONH2-C(O)Rd; Rd = OH, alkoxy or amino; R4 , R5 = H, halogen, (polyhalo)alkyl, R10-C(X)-R11-, R10-Y-C(X)-R11-, R11-Y-R11-, or R10-S-(O)n-R11-; R11 = a bond, alkylene, alkenylene or alkynylene; X = O, S, or NR12; R3, R10, R12 = H or alkyl; Y = O, S or (alkyl)amino; and n = 1 or 2. Alkyl, alkoxy and alkylene have 1-6C, alkenylene have 2-6C and 1-3 double bonds, alkynylene have 2-6C and 1-3 triple bonds, polyhaloalkyl have 1-3C and 1-7 halogens, heteroaryl has 5 - 11 members and is mono or bicyclic with at least one aromatic ring and with 1-3 heteroatoms selected from O, N and S and may be substituted by an oxo group on a non-aromatic part of the structure, cycloalkyl has 3-10C, is mono or bicyclic and may have 1 or 2 unsaturations. An Independent claim is also included for the preparation of (I).

    6.
    发明专利
    未知

    公开(公告)号：NO20034722D0

    公开(公告)日：2003-10-22

    申请号：NO20034722

    申请日：2003-10-22

    Applicant: SERVIER LAB

    Inventor： RAULT SYLVAIN ,  KOPP MARINE ,  LANCELOT JEAN-CHARLES ,  LEMAITRE STEPHANE ,  CAIGNARD DANIEL-HENRI ,  BIZOT-ESPIARD JEAN-GUY ,  RENARD PIERRE

    IPC: A61K31/381 ,  A61K31/402 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/44 ,  A61K31/4439 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  C07D

    Abstract: Imidazoline derivatives (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new. Imidazoline derivatives of formula (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new: R1 = heteroaryl optionally substituted by T1; R2 = cycloalkyl optionally substituted by T1; T1 = halogen, alkyl, alkoxy, OH, CN, NO2, (di)(alkyl)amino, COOH, COO-alkyl or CONH2-C(O)Rd; Rd = OH, alkoxy or amino; R4 , R5 = H, halogen, (polyhalo)alkyl, R10-C(X)-R11-, R10-Y-C(X)-R11-, R11-Y-R11-, or R10-S-(O)n-R11-; R11 = a bond, alkylene, alkenylene or alkynylene; X = O, S, or NR12; R3, R10, R12 = H or alkyl; Y = O, S or (alkyl)amino; and n = 1 or 2. Alkyl, alkoxy and alkylene have 1-6C, alkenylene have 2-6C and 1-3 double bonds, alkynylene have 2-6C and 1-3 triple bonds, polyhaloalkyl have 1-3C and 1-7 halogens, heteroaryl has 5 - 11 members and is mono or bicyclic with at least one aromatic ring and with 1-3 heteroatoms selected from O, N and S and may be substituted by an oxo group on a non-aromatic part of the structure, cycloalkyl has 3-10C, is mono or bicyclic and may have 1 or 2 unsaturations. An Independent claim is also included for the preparation of (I).

    8.
    发明专利
    未知

    公开(公告)号：AT288432T

    公开(公告)日：2005-02-15

    申请号：AT03292634

    申请日：2003-10-22

    Applicant: SERVIER LAB

    Inventor： RAULT SYLVAIN ,  KOPP MARINA ,  LANCELOT JEAN-CHARLES ,  LEMAITRE STEPHANE ,  CAIGNARD DANIEL-HENRI ,  BIZOT-ESPIARD JEAN-GUY ,  RENARD PIERRE

    IPC: A61K31/381 ,  A61K31/402 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/44 ,  A61K31/4439 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06

    Abstract: Imidazoline derivatives (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new. Imidazoline derivatives of formula (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new: R1 = heteroaryl optionally substituted by T1; R2 = cycloalkyl optionally substituted by T1; T1 = halogen, alkyl, alkoxy, OH, CN, NO2, (di)(alkyl)amino, COOH, COO-alkyl or CONH2-C(O)Rd; Rd = OH, alkoxy or amino; R4 , R5 = H, halogen, (polyhalo)alkyl, R10-C(X)-R11-, R10-Y-C(X)-R11-, R11-Y-R11-, or R10-S-(O)n-R11-; R11 = a bond, alkylene, alkenylene or alkynylene; X = O, S, or NR12; R3, R10, R12 = H or alkyl; Y = O, S or (alkyl)amino; and n = 1 or 2. Alkyl, alkoxy and alkylene have 1-6C, alkenylene have 2-6C and 1-3 double bonds, alkynylene have 2-6C and 1-3 triple bonds, polyhaloalkyl have 1-3C and 1-7 halogens, heteroaryl has 5 - 11 members and is mono or bicyclic with at least one aromatic ring and with 1-3 heteroatoms selected from O, N and S and may be substituted by an oxo group on a non-aromatic part of the structure, cycloalkyl has 3-10C, is mono or bicyclic and may have 1 or 2 unsaturations. An Independent claim is also included for the preparation of (I).

    9.
    发明专利
    未知

    公开(公告)号：FR2846328B1

    公开(公告)日：2004-12-10

    申请号：FR0213194

    申请日：2002-10-23

    Applicant: SERVIER LAB

    Inventor： RAULT SYLVAIN ,  KOPP MARINA ,  LANCELOT JEAN CHARLES ,  LEMAITRE STEPHANE ,  CAIGNARD DANIEL HENRI ,  BIZOT ESPIARD JEAN GUY ,  RENARD PIERRE

    IPC: A61K31/381 ,  A61K31/402 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/44 ,  A61K31/4439 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  A61K31/4025 ,  A61K31/4402

    Abstract: Imidazoline derivatives (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new. Imidazoline derivatives of formula (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new: R1 = heteroaryl optionally substituted by T1; R2 = cycloalkyl optionally substituted by T1; T1 = halogen, alkyl, alkoxy, OH, CN, NO2, (di)(alkyl)amino, COOH, COO-alkyl or CONH2-C(O)Rd; Rd = OH, alkoxy or amino; R4 , R5 = H, halogen, (polyhalo)alkyl, R10-C(X)-R11-, R10-Y-C(X)-R11-, R11-Y-R11-, or R10-S-(O)n-R11-; R11 = a bond, alkylene, alkenylene or alkynylene; X = O, S, or NR12; R3, R10, R12 = H or alkyl; Y = O, S or (alkyl)amino; and n = 1 or 2. Alkyl, alkoxy and alkylene have 1-6C, alkenylene have 2-6C and 1-3 double bonds, alkynylene have 2-6C and 1-3 triple bonds, polyhaloalkyl have 1-3C and 1-7 halogens, heteroaryl has 5 - 11 members and is mono or bicyclic with at least one aromatic ring and with 1-3 heteroatoms selected from O, N and S and may be substituted by an oxo group on a non-aromatic part of the structure, cycloalkyl has 3-10C, is mono or bicyclic and may have 1 or 2 unsaturations. An Independent claim is also included for the preparation of (I).

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