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    Transition metal catalyzed synthesis of N-aminoindoles
    3.
    发明申请
    Transition metal catalyzed synthesis of N-aminoindoles 有权
    过渡金属催化N-氨基吲哚的合成

    公开(公告)号：US20100168429A1

    公开(公告)日：2010-07-01

    申请号：US12576339

    申请日：2009-10-09

    Applicant: Nis HALLAND ,  Marc NAZARE ,  Andreas LINDENSCHMIDT ,  Omar AKYEK ,  Matthias URMANN ,  Jorge ALONSO

    Inventor： Nis HALLAND ,  Marc NAZARE ,  Andreas LINDENSCHMIDT ,  Omar AKYEK ,  Matthias URMANN ,  Jorge ALONSO

    IPC: C07D471/04 ,  C07D209/04 ,  C07D401/04

    CPC classification number: C07D209/08

    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

    Abstract translation: 本发明涉及一种用于区域选择性合成式I化合物的方法，其中R 0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4，Q，T和J具有权利要求中所示的含义。 本发明提供了从2-卤代 - 苯基乙炔或（2-磺酸根合）苯基 - 乙炔和N，N-二取代的，由式I表示的多种多官能N-氨基吲哚或N-氨基 - 氮杂吲哚的直接过渡金属催化方法 肼，可用于生产药物，诊断剂，液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

    Transition metal catalyzed synthesis of 2H-indazoles
    4.
    发明授权
    Transition metal catalyzed synthesis of 2H-indazoles 有权
    过渡金属催化合成2H-吲唑

    公开(公告)号：US08283476B2

    公开(公告)日：2012-10-09

    申请号：US12644371

    申请日：2009-12-22

    Applicant: Nis Halland ,  Marc Nazare ,  Andreas Lindenschmidt ,  Jorge Alonso ,  Omar Rkyek ,  Matthias Urmann

    Inventor： Nis Halland ,  Marc Nazare ,  Andreas Lindenschmidt ,  Jorge Alonso ,  Omar Rkyek ,  Matthias Urmann

    IPC: C07D231/56

    CPC classification number: C07D231/56

    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines.

    Abstract translation: 本发明涉及一种用于区域选择性合成式I化合物的方法，其中R 0; R1; R2; R3; R4; R5; A1; A2; A3; A4，Q和J具有权利要求中所示的含义。 本发明提供了对2-卤代苯基乙炔或（2-磺酸基）苯基乙炔和单取代肼的多种式（I）的多官能2H-吲唑或2H-氮杂吲唑的直接过渡金属催化方法。

    Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles
    5.
    发明申请
    Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles 有权
    苯并咪唑和氮杂苯并咪唑的区域选择性钯催化合成

    公开(公告)号：US20090203912A1

    公开(公告)日：2009-08-13

    申请号：US12353271

    申请日：2009-01-14

    Applicant: Jorge ALONSO ,  Andreas LINDENSCHMIDT ,  Marc NAZARE ,  Nis HALLAND ,  Omar RKYEK ,  Matthias URMANN

    Inventor： Jorge ALONSO ,  Andreas LINDENSCHMIDT ,  Marc NAZARE ,  Nis HALLAND ,  Omar RKYEK ,  Matthias URMANN

    IPC: C07D471/04 ,  C07D235/08

    CPC classification number: C07D235/10 ,  C07D235/08 ,  C07D235/16 ,  C07D401/04 ,  C07D471/04

    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

    Abstract translation: 本发明涉及一种用于区域选择性合成式I化合物的方法，其中R 0; R1; R2; R3; R4; R5; A1; A2; A3; A4，Q和J具有权利要求中所示的含义。 本发明提供了直接钯催化的区域选择性方法，用于从2-卤代 - 硝基芳烃和用于制备药物，诊断剂的N-取代酰胺开始的各种不对称，多官能的取代的苯并咪唑或式I的氮杂苯并咪唑， 液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

    Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles
    6.
    发明授权
    Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles 有权
    苯并咪唑和氮杂苯并咪唑的区域选择性钯催化合成

    公开(公告)号：US08188282B2

    公开(公告)日：2012-05-29

    申请号：US12353271

    申请日：2009-01-14

    Applicant: Jorge Alonso ,  Andreas Lindenschmidt ,  Marc Nazare ,  Nis Halland ,  Omar Rkyek ,  Matthias Urmann

    Inventor： Jorge Alonso ,  Andreas Lindenschmidt ,  Marc Nazare ,  Nis Halland ,  Omar Rkyek ,  Matthias Urmann

    IPC: C07D513/02 ,  C07D235/00

    CPC classification number: C07D235/10 ,  C07D235/08 ,  C07D235/16 ,  C07D401/04 ,  C07D471/04

    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

    Abstract translation: 本发明涉及一种用于区域选择性合成式I化合物的方法，其中R 0; R1; R2; R3; R4; R5; A1; A2; A3; A4，Q和J具有权利要求中所示的含义。 本发明提供了直接钯催化的区域选择性方法，用于从2-卤代 - 硝基芳烃和用于制备药物，诊断剂的N-取代酰胺开始的各种不对称，多官能的取代的苯并咪唑或式I的氮杂苯并咪唑， 液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

    Transition metal catalyzed synthesis of N-aminoindoles
    7.
    发明授权
    Transition metal catalyzed synthesis of N-aminoindoles 有权
    过渡金属催化N-氨基吲哚的合成

    公开(公告)号：US08026375B2

    公开(公告)日：2011-09-27

    申请号：US12576339

    申请日：2009-10-09

    Applicant: Nis Halland ,  Marc Nazare ,  Andreas Lindenschmidt ,  Omar Rkyek ,  Matthias Urmann ,  Jorge Alonso

    Inventor： Nis Halland ,  Marc Nazare ,  Andreas Lindenschmidt ,  Omar Rkyek ,  Matthias Urmann ,  Jorge Alonso

    IPC: C07D471/04 ,  C07D209/04

    CPC classification number: C07D209/08

    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

    Abstract translation: 本发明涉及一种用于区域选择性合成式I化合物的方法，其中R 0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4，Q，T和J具有权利要求中所示的含义。 本发明提供了从2-卤代 - 苯基乙炔或（2-磺酸根合）苯基 - 乙炔和N，N-二取代的，由式I表示的多种多官能N-氨基吲哚或N-氨基 - 氮杂吲哚的直接过渡金属催化方法 肼，可用于生产药物，诊断剂，液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

    N-[4-(1H-PYRAZOLO[3,4-b]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS
    8.
    发明申请
    N-[4-(1H-PYRAZOLO[3,4-b]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 审中-公开
    N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基] - 磺酰胺及其作为药物的用途

    公开(公告)号：US20130072493A1

    公开(公告)日：2013-03-21

    申请号：US13236027

    申请日：2011-09-19

    Applicant: Marc NAZARE ,  Nis Halland ,  Friedemann Schmidt ,  Tilo Weiss ,  Uwe Dietz ,  Armin Hofmeister

    Inventor： Marc NAZARE ,  Nis Halland ,  Friedemann Schmidt ,  Tilo Weiss ,  Uwe Dietz ,  Armin Hofmeister

    IPC: A61K31/4985 ,  A61P19/02 ,  A61P19/04 ,  A61P9/10 ,  A61P9/00 ,  A61P43/00 ,  A61P29/00 ,  A61P35/00 ,  C07D487/04 ,  A61P3/10

    CPC classification number: A61K31/4985 ,  C07D487/04

    Abstract: The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

    Abstract translation: 本发明涉及式I的N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基] - 磺酰胺，其中Ar，R 1，R 2和n具有如 索赔。 式I的化合物是调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶同工型1（SGK-1，SGK1）的活性的有价值的药理活性化合物，并且是 适合于治疗SGK活动不适当的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。 本发明还涉及式I化合物的制备方法，它们作为药物的用途，以及包含它们的药物组合物。

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