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    DERIVATIVES OF 1,2,4,5-TETRAHYDRO-3H-BENZAZEPINES, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
    3.
    发明申请
    DERIVATIVES OF 1,2,4,5-TETRAHYDRO-3H-BENZAZEPINES, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
    1,2,4,5-四氢-3H-苯并嗪的衍生物，其制备方法及含有该化合物的药物组合物

    公开(公告)号：WO2009066041A2

    公开(公告)日：2009-05-28

    申请号：PCT/FR2008001268

    申请日：2008-09-11

    Applicant: SERVIER LAB ,  PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  DESSINGES AIMEE ,  CAIGNARD PASCAL ,  VILAINE JEAN-PAUL ,  THOLLON CATHERINE ,  VILLENEUVE NICOLE ,  CHIMENTI STEFANO

    Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  DESSINGES AIMEE ,  CAIGNARD PASCAL ,  VILAINE JEAN-PAUL ,  THOLLON CATHERINE ,  VILLENEUVE NICOLE ,  CHIMENTI STEFANO

    CPC classification number: C07D223/16

    Abstract: The invention relates to compounds having formula (I), wherein: R1 represents a hydrogen atom or a group selected from cycloalkyl, benzyl and alkyl, optionally substituted; R2, R3, R4 and R5 each represent a hydrogen atom or a hydroxy, methyl, -OSO2R10, -OCOR10, alkoxy group, optionally substituted, or R2 and R3,or R3 and R4, or R4 and R5 together form a group -O-(CH2)q-O-, -O-CH=CH-O- or -O-CH=CH-; R6, R7, R8 and R9 each represent a hydrogen atom or an alkoxy group, or R6 and R7, or R7 and R8, or R8 and R9 together form a group -O-(CH2)q-O-; R10 a group selected from linear or branched alkoxy C1-C6, NR11R'11,and alkyl, optionally substituted; R11 and R'11 each represent a hydrogen atom or an alkyl group, or R11 and R'11 together with the nitrogen atom bearing same form an optionally substituted mono- or bi-cyclic nitrogenous heterocycle; - X represents O, NH or CH2; m and p each represent 0 or 1; n and q each represent 1 or 2, said compound being in racemic form or in the form of optical isomers, as well as the pharmaceutically acceptable acid addition salts thereof. The invention is suitable for use in drugs.

    Abstract translation: 本发明涉及具有式（I）的化合物，其中：R 1表示氢原子或选自环烷基，苄基和烷基，任选取代的基团; R2，R3，R4和R5各自表示氢原子或羟基，甲基，-OSO2R10，-OCOR10，任选取代的烷氧基，或R2和R3，或R3和R4，或R4和R5一起形成基团-O - （CH 2）q O - ， - O-CH = CH-O-或-O-CH = CH-; R6，R7，R8和R9各自表示氢原子或烷氧基，或R6和R7，或R7和R8，或R8和R9一起形成-O-（CH 2）q -O-基团; R10是选自直链或支链烷氧基C1-C6，NR11R11和选择取代的烷基; R 11和R 11各自表示氢原子或烷基，或R 11和R 11与具有相同形式的任选取代的单环或双环含氮杂环的氮原子一起形成; -X表示O，NH或CH 2; m和p各自表示0或1; n和q各自表示1或2，所述化合物为外消旋形式或以旋光异构体的形式，以及其药学上可接受的酸加成盐。 本发明适用于药物。

    DERIVES DE 1,2,4,5-TETRAHYDRO-3H-BENZAZEPINES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
    4.
    发明专利
    DERIVES DE 1,2,4,5-TETRAHYDRO-3H-BENZAZEPINES, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT 未知

    公开(公告)号：CA2639349C

    公开(公告)日：2011-03-22

    申请号：CA2639349

    申请日：2008-09-02

    Applicant: SERVIER LAB

    Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  DESSINGES AIMEE ,  CAIGNARD PASCAL ,  VILAINE JEAN-PAUL ,  THOLLON CATHERINE ,  VILLENEUVE NICOLE ,  CHIMENTI STEFANO

    IPC: C07D223/16 ,  A61K31/55 ,  A61P9/00

    Abstract: Composés de formule (I) : (voir formule I) dans laquelle : - R1 représente un atome d'hydrogène ou un groupement choisi parmi cycloalkyle, benzyle et alkyle éventuellement substitué, - R2, R3, R4 et R5 représentent chacun un atome d'hydrogène ou un groupement hydroxy, méthyle, -OSO2R10, -OCOR10, alkoxy éventuellement substitué, ou bien R2 et R3, ou R3 et R4, ou R4 et R5 forment ensemble un groupement -O-(CH2)q-O-, -0-CH=CH-O- ou -O-CH=CH-, - R6, R7, R8 et R9 représentent chacun un atome d'hydrogène ou un groupement alkoxy, ou bien R6 et R7, ou R7 et R8, ou R8 et R9 forment ensemble un groupement -O-(CH2)q-O-, - R10 représente un groupement choisi parmi alkoxy C1-C6 linéaire ou ramifié, NR11R'11, et alkyle éventuellement substitué, - R11 et R'11 représentent chacun un atome d'hydrogène ou un groupement alkyle, ou bien R11 et R'11 forment ensemble, avec l'atome d'azote qui les porte, un hétérocycle azoté mono-ou bicyclique éventuellement substitué, - X représente O, NH ou CH2, - m et p représentent chacun 0 ou 1, - n et q représentent chacun 1 ou 2, sous forme racémique ou d'isomères optiques, ainsi que leurs sels d'addition avec un acide pharmaceutiquement acceptable. Utilisation des composés de formule (I) telle que définie ci-haut destinés au traitement ou la prévention des pathologies dans lesquelles une accélération de la fréquence cardiaque joue un rôle déclenchant ou aggravant ou destinés au traitement curatif ou préventif des douleurs, de la vessie interactive ou de la sensation de sècheresse oculaire.

    6.
    发明专利
    未知

    公开(公告)号：BRPI0804091A2

    公开(公告)日：2009-05-05

    申请号：BRPI0804091

    申请日：2008-09-11

    Applicant: SERVIER LAB

    Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  DESSINGES AIMEE ,  CAIGNARD PASCAL ,  VILAINE JEAN-PAUL ,  THOLLON CATHERINE ,  VILLENEUVE NICOLE ,  CHIMENTI STEFANO

    IPC: C07D223/16 ,  A61K31/075 ,  A61K31/085 ,  A61K31/13 ,  A61K31/135 ,  A61K31/33 ,  A61K31/395 ,  A61K31/55 ,  C07C13/44 ,  C07C13/45 ,  C07C13/465

    Abstract: 1,2,4,5-Tetrahydro-3H-benzazepine compounds (I) and their optical isomers or acid addition salts are new. 1,2,4,5-Tetrahydro-3H-benzazepine compounds of formula (I) and their optical isomers or acid addition salts are new. R 1> : H, 3-7C cycloalkyl, benzyl or alkyl (optionally saturated and substituted by 3-7C cycloalkyl or one or more halo); either R 2>, R 3>, R 4>, R 5> : H, OH, CH 3, -OSO 2R 10>, -OCOR 10>or 1-6C alkoxy (optionally saturated); or R 2>R 3>, R 3>R 4>, R 4>R 5> : -O-(CH 2) q-O-, -O-CH=CH-O- or -O-CH=CH-; either R 6>, R 7>, R 8>, R 9> : H or 1-6C alkoxy (optionally saturated); or R 6>R 7>, R 7>R 8>, R 8>R 9> : -O-(CH 2) q-O-; R 10> : 1-6C alkoxy, NR 11>R11a or 1-6C alkyl (optionally substituted by one or more halo); either R 11>, R11a : H or 1-6C alkyl; or NR 11>R11a : nitrogen containing mono or bicyclic heterocycle ring with 5-8 chains (optionally containing heteroatoms of O or N and substituted by one or more halo); X : O, NH or CH 2; m, p : 0 or 1; and n, q : 1 or 2. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Cardiant; Vasotropic; Antiarrhythmic; Antianginal; Hypotensive; Antidiabetic; Antilipemic. MECHANISM OF ACTION : None given.

    DERIVADOS DE 1,2,4,5-TETRAHIDRO-3H-BENZAZEPINAS, SU PROCEDIMIENTO DE PREPARACIÓN Y LAS COMPOSICIONES FARMACÉUTICAS QUE LAS CONTIENEN
    7.
    发明专利
    DERIVADOS DE 1,2,4,5-TETRAHIDRO-3H-BENZAZEPINAS, SU PROCEDIMIENTO DE PREPARACIÓN Y LAS COMPOSICIONES FARMACÉUTICAS QUE LAS CONTIENEN 未知

    公开(公告)号：ECSP088731A

    公开(公告)日：2008-10-31

    申请号：ECSP088731

    申请日：2008-09-10

    Applicant: SERVIER LAB

    Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  DESSINGES AIMEE ,  CAIGNARD PASCAL ,  VILAINE JEAN-PAUL ,  THOLLON CATHERINE ,  VILLENEUVE NICOLE

    Abstract: Compuestos de fórmula (I): en la que:- R1 representa un átomo de hidrógeno o un grupo elegido entre cicloalquilo, bencilo y alquilo opcionalmente sustituido, - R2, R3, R4 y R5 representan cada uno un átomo de hidrógeno o un grupo hidroxi, metilo, ?OSO2R10, -OCOR10, alcoxi opcionalmente sustituido, o bien R2 y R3, o R3 y R4, o R4 y R5 forman juntos un grupo -O-(CH2)q-O-, -O-CH=CH-O- o -O-CH=CH-, - R6, R7, R8 y R9 representan cada uno un átomo de hidrógeno o un grupo alcoxi, o bien R6 y R7, o R7 y R8, o R8 y R9 forman juntos un grupo -O-(CH2)q-O-,- R10 representa un grupo elegido entre alcoxi C1-C6 lineal o ramificado, NR11R'11 y alquilo opcionalmente sustituido,- R11 y R'11 representan cada uno un átomo de hidrógeno o un grupo alquilo, o bien R11 y R'11 forman juntos, con el átomo de nitrógeno que les soporta, un heterociclo nitrogenado mono-o bicíclico opcionalmente sustituido,- X representa O, NH o CH2,- m y p representan cada uno 0 ó 1,- n y q representan cada uno 1 ó 2,en forma racémica o de isómeros ópticos,así como sus sales de adición con un ácido farmacéuticamente aceptable.Medicamentos.

    10.
    发明专利
    未知

    公开(公告)号：DK1113014T3

    公开(公告)日：2005-08-29

    申请号：DK00403673

    申请日：2000-12-26

    Applicant: SERVIER LAB

    Inventor： PEGLION JEAN-LOUIS ,  BOURGUIGNON MARIE-PIERRE ,  THOLLON CATHERINE ,  POITEVIN CHRISTOPHE ,  VILAINE JEAN-PAUL ,  VILLENEUVE NICOLE

    IPC: C07D417/14 ,  A61K31/00 ,  A61K31/437 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61K31/551 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D209/08 ,  C07D211/00 ,  C07D211/26 ,  C07D211/58 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/06 ,  C07D471/04 ,  C07D491/04 ,  A61K31/415 ,  A61K31/445 ,  A61K31/505 ,  C07D209/04 ,  C07D211/06

    Abstract: Piperidinyl- or piperazinyl-substituted linear or cyclic urea derivatives (or analogs) (I) are new. Piperidine or piperazine derivatives of formula (I) and their isomers, hydrates, solvates and acid addition salts are new. [Image] V, M : direct bond or linear or branched 1-6C alkylene; A, E : N or CH, provided that at least one is N; W : diaza-cyclic group of formula (a) or bicyclic group of formula (b), or may also be a bicyclic group of formula (c) if V = direct bond and A = N; [Image] * : attachment point; X : CO, SO or SO 2; G 12-4C n-alkylene (optionally containing a double bond and/or substituted by OH); G 2direct bond; and G 32-3C n-alkylene (optionally containing a double bond); or G 2CH 2; and G 31-2C n-alkylene (optionally containing a double bond); T : fused benzene or pyridine ring; R 1H, alkyl, Ar or Ar-alkyl; R 2 a, R 2 bH, halo, alkyl, OH, alkoxy, SH, alkylthio, trihaloalkyl, CN, NO 2, NH 2, mono- or dialkylamino, trihaloalkoxy, Ar-alkoxy, alkylsulfonate, trihaloalkylsulfonate or alkylsulfonyl; or R 2 a + R 2 bOCH 2O, O(CH 2) 2O, O(CH 2) 3O or CH 2CH 2 (optionally substituted by CN, CH 2OH, alkoxycarbonyl, ArOCO, or Ar-alkoxycarbonyl); R 3Ar or Het 1 (both optionally substituted by one or more R 2 a); Y : OAr, OHet 1 or Het 2 (all optionally substituted by one or more R 2 a); Ar : phenyl, biphenyl, naphthyl, dihydronaphthyl, tetrahydronaphthyl, indanyl, indenyl or benzocyclobutyl; Het 15-12 membered mono- or bicyclic aromatic system containing 1 or 2 of O, S and N as heteroatom(s), where in the case of bicyclic systems one of the rings may be partially hydrogenated; and Het 25-12 membered mono- or bicyclic aromatic system containing 1-3 of O, S and N as heteroatom(s). alkyl moieties have 1-6C unless specified otherwise; provided that: (i) if V = direct bond, W = (a) and R 3 = Ph, then Y cannot be 3-indolyl; (ii) if M = direct bond, W = (a) and Y = bicyclic Het 2 in which one ring is a benzene ring, then Y cannot be bonded to M via this benzene ring; and (iii) if M = direct bond, V = CH 2CH 2, W = (a) and R 3 = Ph, then Y cannot be 1,2-benzisoxazol-3-yl. An independent claim is included for the preparation of (I). ACTIVITY : Vasotropic; antiarteriosclerotic; cardiant; hypotensive. MECHANISM OF ACTION : Endothelial nitrogen monoxide (NO) synthase inhibitor antagonist; superoxide antagonist; antioxidant. (I) reduce endothelial dysfunction and reduction in vascular NO availability induced by inhibition of endothelial NO synthase or by oxidative stress associated with production of superoxide anion. In tests in rat aortic rings, N-(2-(4-(phenoxymethyl)-1-piperidinyl)-ethyl)-1-indoline-carboxamide (Ia) at a concentration of 30 nM gave 26 % inhibition of endothelial dysfunction induced by the NO synthase inhibitor N(G)-nitro-L-arginine.

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