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    NOVEL SMALL MOLECULE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS
    1.
    发明申请
    NOVEL SMALL MOLECULE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS 有权

    公开(公告)号：US20110245247A1

    公开(公告)日：2011-10-06

    申请号：US13073087

    申请日：2011-03-28

    申请人： Wilfried Braje ,  Katja Jantos ,  Hervé Geneste ,  Mario Mezler ,  Margaretha Henrica Maria Bakker

    发明人： Wilfried Braje ,  Katja Jantos ,  Hervé Geneste ,  Mario Mezler ,  Margaretha Henrica Maria Bakker

    IPC分类号： A61K31/5377 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D403/12 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/4709 ,  A61K31/498 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/08 ,  A61P25/06

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14

    摘要： The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I wherein X1 is N or C—R1, X2 is N or C—R2, X3 is N or C—R3, X4 is N or C—R4 provided that none or one of X1, X2, X3 or X4 is N; Y1 is N, C or C—R5, Y2 is N, C or C—R6, Y3 is Y1, Y2, N, C or C—R7, Y4 is N, C or C—R8 provided that only the moiety Y1, Y2, Y3 or Y4 to which Z is bound is C and further provided at most one of Y1, Y2, Y3 or Y4 is N; Z is O, S, S(O), S(O)2 or NRZ; Q is CH2 or CH2CH2, where one or two of the hydrogen atoms in CH2 or CH2CH2 may be replaced by halogen, C1-C4-alkyl or C1-C4-haloalkyl; R1 is inter alia hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C4-haloalkoxy, C3-C8-cycloalkyl, a radical NR1aR1b, C-bound 3- to 7-membered, saturated heterocyclyl having 1 or 2 nitrogen atoms and 0 or 1 heteroatoms, selected from O and S, as ring members, aryl, aryl-CH2, aryloxy, hetaryl, hetaryloxy or hetaryl-CH2, wherein the heterocyclyl, aryl and hetaryl rings ring in the last six radicals themselves are unsubstituted or carry 1, 2, 3, 4 or 5 identical or different radicals R1c; R2 has one of the meanings given for R1; R3 and R4 are, inter alia, selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl, phenyl, C1-C4-haloalkoxy, a radical (CH2)nNR′R″; R5, R6, R7, R8 are, independently of each other, selected from hydrogen, halogen, etc.; Ra is C3-C6-cycloalkyl, C1-C6-haloalkyl or C1-C6-alkyl, which is unsubstituted or carries one radical selected from C1-C4-alkoxy, C1-C4-haloalkoxy and a radical NRa1Ra2; and the N-oxides and the pharmaceutically acceptable salts thereof.

    Small molecule potentiators of metabotropic glutamate receptors
    3.
    发明授权
    Small molecule potentiators of metabotropic glutamate receptors 有权

    公开(公告)号：US08314120B2

    公开(公告)日：2012-11-20

    申请号：US13073087

    申请日：2011-03-28

    申请人： Wilfried Braje ,  Katja Jantos ,  Hervé Geneste ,  Mario Mezler ,  Margaretha Henrica Maria Bakker

    发明人： Wilfried Braje ,  Katja Jantos ,  Hervé Geneste ,  Mario Mezler ,  Margaretha Henrica Maria Bakker

    IPC分类号： A61K31/4375 ,  A61K31/4725 ,  A61K31/403 ,  C07D471/04 ,  C07D217/22 ,  C07D487/04 ,  C07D209/46

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14

    摘要： The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I wherein X1 is N or C—R1, X2 is N or C—R2, X3 is N or C—R3, X4 is N or C—R4 provided that none or one of X1, X2, X3 or X4 is N; Y1 is N, C or C—R5, Y2 is N, C or C—R6, Y3 is Y1, Y2, N, C or C—R7, Y4 is N, C or C—R8 provided that only the moiety Y1, Y2, Y3 or Y4 to which Z is bound is C and further provided at most one of Y1, Y2, Y3 or Y4 is N; Z is O, S, S(O), S(O)2 or NRZ; Q is CH2 or CH2CH2, where one or two of the hydrogen atoms in CH2 or CH2CH2 may be replaced by halogen, C1-C4-alkyl or C1-C4-haloalkyl; R1 is inter alia hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C4-haloalkoxy, C3-C8-cycloalkyl, a radical NR1aR1b, C-bound 3- to 7-membered, saturated heterocyclyl having 1 or 2 nitrogen atoms and 0 or 1 heteroatoms, selected from O and S, as ring members, aryl, aryl-CH2, aryloxy, hetaryl, hetaryloxy or hetaryl-CH2, wherein the heterocyclyl, aryl and hetaryl rings ring in the last six radicals themselves are unsubstituted or carry 1, 2, 3, 4 or 5 identical or different radicals R1c; R2 has one of the meanings given for R1; R3 and R4 are, inter alia, selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl, phenyl, C1-C4-haloalkoxy, a radical (CH2)nNR′R″; R5, R6, R7, R8 are, independently of each other, selected from hydrogen, halogen, etc.; Ra is C3-C6-cycloalkyl, C1-C6-haloalkyl or C1-C6-alkyl, which is unsubstituted or carries one radical selected from C1-C4-alkoxy, C1-C4-haloalkoxy and a radical NRa1Ra2; and the N-oxides and the pharmaceutically acceptable salts thereof.

    NOVEL SMALL MOLECULE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS I
    4.
    发明申请
    NOVEL SMALL MOLECULE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS I 有权

    公开(公告)号：US20110245232A1

    公开(公告)日：2011-10-06

    申请号：US13071753

    申请日：2011-03-25

    申请人： Wilfried Braje ,  Katja Jantos ,  Hervé Geneste ,  Mario Mezler ,  Margaretha Henrica Maria Bakker ,  Jayne Froggett

    发明人： Wilfried Braje ,  Katja Jantos ,  Hervé Geneste ,  Mario Mezler ,  Margaretha Henrica Maria Bakker ,  Jayne Froggett

    IPC分类号： A61K31/553 ,  C07D401/12 ,  A61K31/4439 ,  C07D413/14 ,  A61K31/5377 ,  C07D401/14 ,  A61K31/496 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/08 ,  A61P25/06

    CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

    摘要： The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I wherein X2 is N or C—R2, X3 is N or C—R3, X4 is N or C—R4 provided that none or one of X2, X3 or X4 is N; Y1 is N, C or C—R5, Y2 is N, C or C—R6, Y3 is N, C or C—R7, Y4 is N, C or C—R8 provided that only the moiety Y1, Y2, Y3 or Y4 to which Z is bound is C and further provided at most one of Y1, Y2, Y3 or Y4 is N; Z is O, S, S(O), S(O)2 or NRZ; Q is CH2 or CH2CH2, where one or two of the hydrogen atoms in CH2 or CH2CH2 may be replaced by halogen, C1-C4-alkyl or C1-C4-haloalkyl; R1 is inter alia hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C4-haloalkoxy, C3-C8-cycloalkyl, a radical NR1aR1b, C-bound 3- to 7-membered, saturated heterocyclyl having 1 or 2 nitrogen atoms and 0 or 1 heteroatoms, selected from O and S, as ring members, aryl, aryl-CH2, aryloxy, hetaryl, hetaryloxy or hetaryl-CH2, wherein the heterocyclyl, aryl and hetaryl rings ring in the last six radicals themselves are unsubstituted or carry 1, 2, 3, 4 or 5 identical or different radicals R1c; R2, R3 and R4 are, inter alia, selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl, phenyl, C1-C4-haloalkoxy, a radical (CH2)nNR′R″; R5, R6, R7, R8 are, independently of each other, selected from hydrogen, halogen, etc.; Ra is C3-C6-cycloalkyl, C1-C6-haloalkyl or C1-C6-alkyl, which is unsubstituted or carries one radical selected from C1-C4-alkoxy, C1-C4-haloalkoxy and a radical NRa1Ra2, Rb is hydrogen, halogen or C1-C4-alkyl; and the N-oxides and the pharmaceutically acceptable salts thereof.

    Carboxamide compounds and their use as calpain inhibitors IV
    6.
    发明授权
    Carboxamide compounds and their use as calpain inhibitors IV 有权
    羧甲酰胺化合物及其作为钙蛋白酶抑制剂的用途

    公开(公告)号：US08598211B2

    公开(公告)日：2013-12-03

    申请号：US12972679

    申请日：2010-12-20

    申请人： Andreas Kling ,  Katja Jantos ,  Helmut Mack ,  Achim Möller ,  Wilfried Hornberger ,  Gisela Backfisch ,  Yanbin Lao ,  Marjoleen Nijsen

    发明人： Andreas Kling ,  Katja Jantos ,  Helmut Mack ,  Achim Möller ,  Wilfried Hornberger ,  Gisela Backfisch ,  Yanbin Lao ,  Marjoleen Nijsen

    IPC分类号： A61K31/4439 ,  C07D401/04

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14

    摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3 R4, R5, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted phenyl-C1-C2-alkyl or hetaryl-C1-C2-alkyl, R2 is optionally substituted aryl, hetaryl, aryl-C1-C6-alkyl, aryl-C2-C6-alkenyl or hetaryl-C1-C4-alkyl, R3 is C3-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or 1,3-benzoxazol-2-yl-methyl, R4 and R5 independently of one another are halogen, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.

    摘要翻译： 本发明涉及新的羧酰胺化合物及其用于制备药物的用途。 羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。 因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。 羧酰胺化合物是通式I的化合物，其中R 1，R 2，R 3，R 4，R 5，m和n具有权利要求书和描述中所述的含义，其互变异构体，其水合物及其药学上合适的盐。 在这些化合物中，优选其中R 1为任选取代的苯基-C 1 -C 2 - 烷基或杂芳基-C 1 -C 2烷基，R 2为任选取代的芳基，杂芳基，芳基-C 1 -C 6 - 烷基，芳基-C 2 -C 6 - 烯基 或杂芳基-C 1 -C 4 - 烷基，R 3是C 3 -C 4 - 烷基，C 1 -C 4 - 卤代烷基，C 2 -C 4 - 烯基，C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基-C 1 -C 2烷基，C 3 -C 6 - 杂环烷基-C 1 -C 2 - 烷基，苯基-C 1 -C 3 - 烷基，吡啶-2-基-C 1 -C 3 - 烷基或1,3-苯并恶唑-2-基 - 甲基，R 4和R 5彼此独立地是卤素 ，CF 3，CHF 2，CH 2 F，C 1 -C 2 - 烷基或C 1 -C 2 - 烷氧基，m和n彼此独立地为0或1。

    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV
    9.
    发明申请
    CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS IV 有权
    羧酰胺化合物及其作为抑制剂的用途IV

    公开(公告)号：US20110152325A1

    公开(公告)日：2011-06-23

    申请号：US12972679

    申请日：2010-12-20

    申请人： Andreas Kling ,  Katja Jantos ,  Helmut Mack ,  Achim Möller ,  Wilfried Hornberger ,  Gisela Backfisch ,  Yanbin Lao ,  Marjoleen Nijsen

    发明人： Andreas Kling ,  Katja Jantos ,  Helmut Mack ,  Achim Möller ,  Wilfried Hornberger ,  Gisela Backfisch ,  Yanbin Lao ,  Marjoleen Nijsen

    IPC分类号： A61K31/4439 ,  C07D401/04 ,  A61P25/28 ,  A61P25/00 ,  A61P25/08 ,  A61P25/04 ,  A61P13/12 ,  A61P35/00 ,  A61P31/18 ,  A61P37/02 ,  A61P33/06

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14

    摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3 R4, R5, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein R1 is optionally substituted phenyl-C1-C2-alkyl or hetaryl-C1-C2-alkyl, R2 is optionally substituted aryl, hetaryl, aryl-C1-C6-alkyl, aryl-C2-C6-alkenyl or hetaryl-C1-C4-alkyl, R3 is C3-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C3-C6-heterocycloalkyl-C1-C2-alkyl, phenyl-C1-C3-alkyl, pyridin-2-yl-C1-C3-alkyl or 1,3-benzoxazol-2-yl-methyl, R4 and R5 independently of one another are halogen, CF3, CHF2, CH2F, C1-C2-alkyl or C1-C2-alkoxy, and m and n independently of one another are 0 or 1.

    摘要翻译： 本发明涉及新的羧酰胺化合物及其用于制备药物的用途。 羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。 因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。 羧酰胺化合物是通式I的化合物，其中R 1，R 2，R 3，R 4，R 5，m和n具有权利要求书和描述中所述的含义，其互变异构体，其水合物及其药学上合适的盐。 在这些化合物中，优选其中R 1为任选取代的苯基-C 1 -C 2 - 烷基或杂芳基-C 1 -C 2烷基，R 2为任选取代的芳基，杂芳基，芳基-C 1 -C 6 - 烷基，芳基-C 2 -C 6 - 烯基 或杂芳基-C 1 -C 4 - 烷基，R 3是C 3 -C 4 - 烷基，C 1 -C 4 - 卤代烷基，C 2 -C 4 - 烯基，C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基-C 1 -C 2烷基，C 3 -C 6 - 杂环烷基-C 1 -C 2 - 烷基，苯基-C 1 -C 3 - 烷基，吡啶-2-基-C 1 -C 3 - 烷基或1,3-苯并恶唑-2-基 - 甲基，R 4和R 5彼此独立地是卤素 ，CF 3，CHF 2，CH 2 F，C 1 -C 2 - 烷基或C 1 -C 2 - 烷氧基，m和n彼此独立地为0或1。

    Carboxamide compounds and their use as calpain inhibitors
    10.
    发明授权
    Carboxamide compounds and their use as calpain inhibitors 有权
    羧酰胺化合物及其作为钙蛋白酶抑制剂的用途

    公开(公告)号：US09018206B2

    公开(公告)日：2015-04-28

    申请号：US13610975

    申请日：2012-09-12

    申请人： Helmut Mack ,  Andreas Kling ,  Katja Jantos ,  Achim Moeller ,  Wilfried Hornberger ,  Charles W. Hutchins

    发明人： Helmut Mack ,  Andreas Kling ,  Katja Jantos ,  Achim Moeller ,  Wilfried Hornberger ,  Charles W. Hutchins

    IPC分类号： C07D211/76 ,  C07D233/34 ,  C07D239/10 ,  C07D207/22 ,  C07D211/78 ,  C07D233/32 ,  C07D275/03 ,  C07D401/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D207/26

    CPC分类号： C07D207/22 ,  C07D207/26 ,  C07D207/28 ,  C07D211/76 ,  C07D211/78 ,  C07D213/81 ,  C07D233/32 ,  C07D233/34 ,  C07D239/10 ,  C07D275/03 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    摘要： The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2—CH2, CH2—CH2—CH2, N(Ry#)—CH2, N(Ry#)—CH2—CH2 or CH═CH—CH═, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.

    摘要翻译： 本发明涉及新的羧酰胺化合物及其用于制备药物的用途。 羧酰胺化合物是钙蛋白酶（钙依赖性半胱氨酸蛋白酶）的抑制剂。 因此，本发明还涉及这些羧酰胺化合物用于治疗与升高的钙蛋白酶活性相关的病症的用途。 羧酰胺化合物是通式I的化合物，其中R 1，R 2，R 3a，R 3b，R 4，Q，Y，A和X具有权利要求和说明书中所述的含义及其互变异构体及其药学上合适的盐。 特别地，化合物具有通式Ia和Ib，其中R1，r，R2b，R3a，R3b，R4，Y和X具有权利要求中提及的含义，包括其互变异构体及其药学上合适的盐。 在这些化合物中，优选其中Y为CH2-CH2，CH2-CH2-CH2，N（Ry＃）-CH2，N（Ry＃）-CH2-CH2或CH = CH-CH≡，各自任选具有1 或2个H原子被相同或不同的基团Ry取代，其中Ry和Ry＃具有权利要求中提及的含义。