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    PROCESS FOR PREPARATION OF DIBENZO [b,d]AZEPIN-6-ONE DERIVATIVE
    2.
    发明专利
    PROCESS FOR PREPARATION OF DIBENZO [b,d]AZEPIN-6-ONE DERIVATIVE 审中-公开
    制备二苯并[b，d]亚氨基-6-酮衍生物的方法

    公开(公告)号：JP2014037431A

    公开(公告)日：2014-02-27

    申请号：JP2013222376

    申请日：2013-10-25

    Applicant: F. Hoffmann-La Roche Ag ,  エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft

    Inventor： HOFFMANN-EMERY FABIENNE ,  JAKOB-ROETNE ROLAND

    IPC: C07D223/18

    CPC classification number: C07D225/08

    Abstract: PROBLEM TO BE SOLVED: To provide a novel process for preparation of enantiomerically pure 7-amino-5H,7H-dibenzo [b,d]azepin-6-one.SOLUTION: A process includes an optical resolution using chiral menthyl chloroformate of dibenzo [b,d]azepin-one derivative represented by formula (II), where Ris hydrogen or halogen, Ris a Calkyl which is possibly substituted by a Ccycloalkyl, or a benzyl which is possibly substituted by a Calkoxy.

    Abstract translation: 要解决的问题：提供制备对映异构纯的7-氨基-5H，7H-二苯并[b，d]氮杂-6-酮的新方法。方法：一种方法包括使用二苯并[ b，d]吖庚因衍生物，其中R 1为氢或卤素，R为可被C环烷基取代的C烷基或可被Calkoxy取代的苄基。

    PROCESS FOR THE PREPARATION OF DIBENZO [B,D]AZEPIN-6-ONE DERIVATIVE
    5.
    发明申请
    PROCESS FOR THE PREPARATION OF DIBENZO [B,D]AZEPIN-6-ONE DERIVATIVE 审中-公开
    二苯并[B，D]亚氨基-6-酮衍生物的制备方法

    公开(公告)号：WO2008145525A3

    公开(公告)日：2009-08-13

    申请号：PCT/EP2008055937

    申请日：2008-05-15

    Applicant: HOFFMANN LA ROCHE ,  HOFFMANN-EMERY FABIENNE ,  JAKOB-ROETNE ROLAND

    Inventor： HOFFMANN-EMERY FABIENNE ,  JAKOB-ROETNE ROLAND

    IPC: C07D225/08

    CPC classification number: C07D225/08

    Abstract: The invention relates to a process for the optical resolution of a dibenzo[b,d]azepinone derivative of the formula (II) wherein R1 is hydrogen or halogen and R2 has the meaning of C1- 4-alkyl optionally substituted with C3-7-cycloalkyl or benzyl which is optionally substituted with C1-4-alkoxy to obtain a (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-one of the formula (I) wherein R1 is as above. The (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-ones of formula (I) can be used as chiral building blocks for the preparation of malonamide derivatives which have the potential to act as ?-secretase inhibitors and therefore may be useful in the treatment of Alzheimer's disease and cancer.

    Abstract translation: 本发明涉及一种用于光学拆分式（II）的二苯并[b，d]氮杂酮衍生物的方法，其中R 1是氢或卤素，R 2具有任选被C 3-7 - 环烷基或苄基，其任选被C 1-4 - 烷氧基取代，得到其中R 1如上所述的式（I）的（S）-7-氨基-5H，7H-二苯并[b，d]氮杂- 。 式（I）的（S）-7-氨基-5H，7H-二苯并[b，d]吖庚因-6-酮可以用作制备具有作为脯氨酸的可能性的丙二酰胺衍生物的手性结构单元。 - 分泌酶抑制剂，因此可用于治疗阿尔茨海默氏病和癌症。

    MALONAMIDE DERIVATIVES
    6.
    发明申请
    MALONAMIDE DERIVATIVES 审中-公开
    马来酰胺衍生物

    公开(公告)号：WO2006061136A2

    公开(公告)日：2006-06-15

    申请号：PCT/EP2005012834

    申请日：2005-12-01

    Applicant: HOFFMANN LA ROCHE ,  FLOHR ALEXANDER ,  JAKOB-ROETNE ROLAND ,  WOSTL WOLFGANG

    Inventor： FLOHR ALEXANDER ,  JAKOB-ROETNE ROLAND ,  WOSTL WOLFGANG

    IPC: C07D267/14 ,  A61K31/553 ,  A61P25/28

    CPC classification number: C07D267/14 ,  C07D413/12

    Abstract: The invention relates to compounds of the general Formula (I) wherein R is halogen, lower alkyl or lower alkyl substituted by halogen; R 1 is hydrogen, lower alkyl or lower alkyl substituted by halogen or hydroxy, or is lower alkenyl, -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -COR', or is benzyl, optionally substituted by halogen, or is -(CH 2 ) n -morpholinyl; R' is lower alkoxy, hydroxy or amino; R 2 is hydrogen, lower alkyl or di-lower alkyl, lower alkyl substituted by halogen or hydroxy, or is benzyl or cycloalkyl; R 3 is lower alkyl or lower alkyl substituted by halogen, or is benzyl, optionally substituted by two halogen atoms, or is -(CH 2 ) n -cycloalkyl or -(CH 2 ) n -pyridinyl; X is -CR 4 R 4 - or - CR 4 R 4' -O-; R 4 /R 4 ' is independently from each other hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy or -CH 2 -2-[1,3]dioxalan-; N is 0, 1 or 2; to pharmaceutically suitable acid addition salts thereof and to all forms of optically pure enantiomers, recemates or diastereomers and diastereomeric mixtures thereof for the treatment of Alzheimer's disease.

    Abstract translation: 本发明涉及通式（I）的化合物，其中R是卤素，被卤素取代的低级烷基或低级烷基; R 1是氢，被卤素或羟基取代的低级烷基或低级烷基，或者是低级烯基， - （CH 2 CH 2）n - ， - （CH 2 CH 2）n -COR'，或是任选被卤素取代的苄基，或是 - （CH 2）2 - >名词 - 吗啉基; R'是低级烷氧基，羟基或氨基; R 2是氢，低级烷基或二低级烷基，被卤素或羟基取代的低级烷基，或是苄基或环烷基; R 3是被卤素取代的低级烷基或低级烷基，或是任选被两个卤素原子取代的苄基，或是 - （CH 2） - （CH 2）n - 亚烷基或 - （CH 2）n - X是-CR 4 S 4 - 或 - CR 4 -OR 4'-O-; R 4和R 4彼此独立地为氢，卤素，低级烷基，低级烷氧基，羟基或-CH 2 - [1,3] dioxalan-; N为0,1或2; 其药学上合适的酸加成盐和所有形式的用于治疗阿尔茨海默氏病的光学纯对映异构体，受体或非对映异构体和非对映体混合物。

    COMT INHIBITORS
    8.
    发明申请
    COMT INHIBITORS 审中-公开
    COMT抑制剂

    公开(公告)号：WO2005058228A3

    公开(公告)日：2005-12-08

    申请号：PCT/EP2004014186

    申请日：2004-12-13

    Applicant: HOFFMANN LA ROCHE ,  DIEDERICH FRANCOIS ,  JAKOB-ROETNE ROLAND ,  LERNER CHRISTIAN ,  PAULINI RALPH

    Inventor： DIEDERICH FRANCOIS ,  JAKOB-ROETNE ROLAND ,  LERNER CHRISTIAN ,  PAULINI RALPH

    IPC: C07D473/34 ,  C07H19/16 ,  C07H19/22 ,  A61K31/52 ,  A61K31/7076

    CPC classification number: C07H19/22 ,  C07D473/34 ,  C07H19/16

    Abstract: Objects of the present invention are the compounds of formula (I) wherein R is H, CN, halogen, COR ; -S(O)xR , C1-12-alkyl, C2-12-alkenyl, C3-8-cycloalkyl, a heterocyclyl group, an aryl group, a heteroaryl group, C3-8-cycloalkyl(C1-3)alkyl, a heterocyclyl-(Cl-3)alkyl group, an aryl(C1-3)alkyl or a heteroaryl(C1-3)alkyl group; the alkyl, alkenyl, alkoxy, cycloalkyl, heterocyclyl group, aryl and heteroaryl groups may all be optionally substituted; R is -N(R , R ), C1-6-alkyl, C3-8-cycloalkyl, heterocyclyl, aryl, heteroaryl, C3-8-cycloalkyl(C1-3)alkyl, a heterocyclyl(C1-3)alkyl group, an aryl(C1-3)alkyl or a heteroaryl(C1-3)alkyl group, the Cl-6-alkyl, C3-8-cycloalkyl, heterocyclyl, aryl, heteroaryl may all be optionally substituted; R and R are independently hydrogen or (C1-3)-alkyl; x is 0, 1 or 2; and the ester thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof, the use of compounds of formula (I) and their pharmaceutically acceptable salts for the manufacture of medicaments for the treatment of diseases, related to the COMT inhibition, their manufacture, medicaments based on a compound in accordance with the invention and their production as well as the use of compounds of formula (I) in the control or prevention of diseases such as depression, schizophrenia, Parkinson's disease, and to improve cognition.

    Abstract translation: 本发明的目的是式（I）的化合物，其中R 1是H，CN，卤素，COR 2; （O）xR 2，C 1-12烷基，C 2-12烯基，C 3-8环烷基，杂环基，芳基，杂芳基，C 3-8 - 环烷基（C 1-3） 烷基，杂环基 - （C1-3）烷基，芳基（C1-3）烷基或杂芳基（C1-3）烷基; 烷基，烯基，烷氧基，环烷基，杂环基，芳基和杂芳基可全部任选被取代; （R 3，R 3'），C 1-6 - 烷基，C 3-8 - 环烷基，杂环基，芳基，杂芳基，C 3-8 - 环烷基（C 1-3）烷基， （C 1-3）烷基，芳基（C 1-3）烷基或杂芳基（C 1-3）烷基，C 1-6 - 烷基，C 3-8 - 环烷基，杂环基，芳基，杂芳基可全部为 任选取代的; R 3和R 3'独立地为氢或（C 1-3） - 烷基; x是0,1或2; 及其在生理条件下可水解的酯及其药学上可接受的盐，式（I）化合物及其药学上可接受的盐在制备用于治疗与COMT抑制有关的疾病的药物中的用途，它们的制造 ，基于根据本发明的化合物的药物及其制备以及式（I）化合物在控制或预防疾病例如抑郁症，精神分裂症，帕金森病中的用途以及改善认知的用途。

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