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    Nuevo proceso de obtención de cloruros de ácido
    4.
    发明专利
    Nuevo proceso de obtención de cloruros de ácido 未知

    公开(公告)号：ES2377570T3

    公开(公告)日：2012-03-29

    申请号：ES06807399

    申请日：2006-10-19

    Applicant: HOFFMANN LA ROCHE

    Inventor： HOFFMANN URSULA ,  RIMMLER GOESTA

    IPC: C07C51/60 ,  C07C53/44

    Abstract: Un proceso para la obtención de un compuesto de la fórmula I en la que R1 es hidrógeno, alquilo C1-C8 o alquenilo C2-C8, que están sin sustituir o sustituidos por uno o más sustituyentes elegidos entre alcoxi C1-C8 y cicloalquilo C3-C8; y 10 R2 y R3 junto con el átomo de carbono al que están unidos forman un cicloalquilo C3-C7 o un cicloalquenilo C5-C8; que consiste en hacer reaccionar un compuesto de la fórmula II en la que R1, R2 y R3 tienen los significados recién definidos; con cloruro de tionilo en presencia de tributilamina.

    7.
    发明专利
    未知

    公开(公告)号：BRPI0407520A

    公开(公告)日：2006-02-14

    申请号：BRPI0407520

    申请日：2004-02-11

    Applicant: HOFFMANN LA ROCHE

    Inventor： BUBENDORF ANDRE GERARD ,  HENNIG MICHAEL ,  HIDBER PIRMIN ,  RIMMLER GOESTA ,  ROHRER FRANZISKA

    IPC: A61K31/517 ,  A61P35/00 ,  C07D239/94

    Abstract: The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. The [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride is an inhibitor of tyrosine kinase enzymes, and are useful in the treatment of cancer. Also disclosed are methods of making and using the novel polymorph, as well as pharmaceutical compositions containing the novel polymorph.

    9.
    发明专利
    未知

    公开(公告)号：DK1103546T3

    公开(公告)日：2004-02-23

    申请号：DK00125665

    申请日：2000-11-23

    Applicant: HOFFMANN LA ROCHE

    Inventor： HILPERT HANS ,  HOFFMANN-EMERY FABIENNE ,  RIMMLER GOESTA ,  ROGERS-EVANS MARK ,  STAHR HELMUT WERNER ,  WALDMEIER PIUS

    IPC: A61K31/496 ,  A61K31/5377 ,  A61P1/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D213/75 ,  C07D213/76 ,  C07D213/82 ,  A61K31/44 ,  A61K31/455

    Abstract: The present invention relates to a process for the preparation of compounds of the general formula wherein the definitions of substituents are described in claim 1, which process comprises 1a) reacting a compound of formula wherein A denotes R or R , and R is halogen, R and R have the significances given in claim 1 and R has the same meaning as R , wherein R and R may he independent from each other, with a compound of formula R Mghal wherein R' is described in claim 1, to a mixture of compounds of formulae wherein the substituents are described in claim 1, or 1a') reacting a compound of formula IV-1, wherein A is R, with a compound of formula V and with a compound of formula HR wherein R is described in claim 1, in one reaction step to a compound of formula wherein R , R , R and R have the significances given in claim 1, and 1b) oxidizing a compound of formulae X-1, XI-1 or VI, which is obtained in step 1a) or 1a') with an oxidizing agent to a compound of formula or wherein R, R , R , R and R have the significances given in claim 1, and, 1b') if desired, reacting a compound of formula XII with a compound of formula VII to a compound of formula VIII, and 1c) reacting a compound of formula VIII with a compound of formula wherein R , R and R are described in claim 1 and R is halogen, to give a compound of formula wherein X is -CON(R )-, or 2 d) transforming a compound of formula VIII to a compound of formula wherein R and R have the significances given in claim 1, and 2 e) reacting a compound of formula XIII to a compound of formulas or wherein the definition of the substituents is given in claim 1, and 2f) transforming the compounds of formulae XIV and XV to a compound of formula wherein R is methyl and 2 g) reacting a compound of formula XVI with a compound of formula to give a compound of formula wherein X is -N(R )C(O)- and the other substituents are described in claim 1.

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