公开(公告)号：US08637517B2

公开(公告)日：2014-01-28

申请号：US13252608

申请日：2011-10-04

Applicant: Dominik Feuerbach ,  Mathias Frederiksen ,  Konstanze Hurth ,  Bernard Lucien Roy ,  Beatrix Wagner

Inventor： Dominik Feuerbach ,  Mathias Frederiksen ,  Konstanze Hurth ,  Bernard Lucien Roy ,  Beatrix Wagner

IPC: A61K31/439 ,  C07D471/08

CPC classification number: C07D471/08 ,  A61K31/439 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06

Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.

Abstract translation: 本发明涉及式（I）的1-氮杂 - 双环烷基衍生物，其中取代基如本说明书中所定义，并且其制备方法为包含它们的药物组合物及其在制备用于治疗和/ /或延迟精神病和再生障碍的进展。

公开(公告)号：US20120172359A1

公开(公告)日：2012-07-05

申请号：US13414440

申请日：2012-03-07

Applicant: Sangamesh BADIGER ,  Murali CHEBROLU ,  Mathias FREDERIKSEN ,  Philipp HOLZER ,  Konstanze HURTH ,  Rainer Martin LUEOEND ,  Lei LI ,  Hui LIU ,  Rainer MACHAUER ,  Henrik MOEBITZ ,  Ulf NEUMANN ,  Rita RAMOS ,  Heinrich RUEEGER ,  Michael SCHAEFER ,  Siem Jacob VEENSTRA ,  Marina TINTELNOT-BLOMLEY ,  Markus VOEGTLE ,  Xin XIONG

Inventor： Sangamesh BADIGER ,  Murali CHEBROLU ,  Mathias FREDERIKSEN ,  Philipp HOLZER ,  Konstanze HURTH ,  Rainer Martin LUEOEND ,  Lei LI ,  Hui LIU ,  Rainer MACHAUER ,  Henrik MOEBITZ ,  Ulf NEUMANN ,  Rita RAMOS ,  Heinrich RUEEGER ,  Michael SCHAEFER ,  Siem Jacob VEENSTRA ,  Marina TINTELNOT-BLOMLEY ,  Markus VOEGTLE ,  Xin XIONG

IPC: A61K31/5377 ,  A61P25/18 ,  A61P25/00 ,  A61P35/00 ,  A61P25/22 ,  A61P25/08 ,  A61P25/06 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P17/04 ,  A61P1/08 ,  A61P3/04 ,  A61P21/02 ,  A61P27/16 ,  A61P27/06 ,  A61P25/30 ,  C07D413/12

CPC classification number: C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.

Abstract translation: 本发明涉及下式的新型杂环化合物，其中所有变量如本说明书中所定义，以游离形式或盐形式，其制备，其医疗用途和包含它们的药物。

公开(公告)号：US08048885B2

公开(公告)日：2011-11-01

申请号：US12732646

申请日：2010-03-26

Applicant: Dominik Feuerbach ,  Mathias Frederiksen ,  Konstanze Hurth ,  Bernard Lucien Roy ,  Beatrix Wagner

Inventor： Dominik Feuerbach ,  Mathias Frederiksen ,  Konstanze Hurth ,  Bernard Lucien Roy ,  Beatrix Wagner

IPC: C07D471/08 ,  A61K31/439

CPC classification number: C07D471/08 ,  A61K31/439 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06

Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.

Abstract translation: 本发明涉及式（I）的1-氮杂 - 双环烷基衍生物，其中取代基如本说明书中所定义，并且其制备方法为包含它们的药物组合物及其在制备用于治疗和/ /或延迟精神病和再生障碍的进展。

公开(公告)号：US20100144741A1

公开(公告)日：2010-06-10

申请号：US12515521

申请日：2007-11-22

Applicant: Mathias Frederiksen ,  Rainer Martin Luond ,  Clive McCarthy ,  Henrik Moebitz ,  Jean-Michel Rondeau ,  Bernard Lucien Roy ,  Heinrich Rueeger

Inventor： Mathias Frederiksen ,  Rainer Martin Luond ,  Clive McCarthy ,  Henrik Moebitz ,  Jean-Michel Rondeau ,  Bernard Lucien Roy ,  Heinrich Rueeger

IPC: A61K31/4402 ,  C07D401/02 ,  C07D239/42 ,  C07C233/40 ,  C07D213/72 ,  C07D405/10 ,  C07D237/20 ,  C07D487/04 ,  A61K31/505 ,  A61K31/506 ,  A61K31/4418 ,  A61K31/50 ,  A61K31/5025 ,  A61P25/00

CPC classification number: C07D401/12 ,  C07C233/40 ,  C07C2601/02 ,  C07D213/74 ,  C07D231/38 ,  C07D237/20 ,  C07D239/42 ,  C07D239/47 ,  C07D239/52 ,  C07D261/14 ,  C07D487/04

Abstract: The invention relates to novel cyclic compounds of the formula (I), in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.

Abstract translation: 本发明涉及以游离碱形式或以酸加成盐形式的式（I）的新型环状化合物，其制备方法，其用作药物和包含它们的药物。

公开(公告)号：US07713977B2

公开(公告)日：2010-05-11

申请号：US12097689

申请日：2006-12-14

Applicant: Dominik Feuerbach ,  Mathias Frederiksen ,  Konstanze Hurth ,  Bernard Lucien Roy ,  Manuel Koller

Inventor： Dominik Feuerbach ,  Mathias Frederiksen ,  Konstanze Hurth ,  Bernard Lucien Roy ,  Manuel Koller

IPC: C07D471/08 ,  A61K31/439

CPC classification number: C07D471/08 ,  A61K31/429

Abstract: The present invention relates to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5 R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: in free base or acid addition salt form, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及式（I）化合物，其中n表示0,1,2,3,4或5个R表示彼此独立的羟基，氰基，硝基，卤素，烷基，烷氧基烷基羰基，烷氧基羰基，烷基胺，二烷基胺， 烷基羰基胺，烷基氨基甲酸酯Y代表下列基团之一：游离碱或酸加成盐形式，其制备方法，它们作为药物的用途以及包含它们的药物组合物。

公开(公告)号：US07713976B2

公开(公告)日：2010-05-11

申请号：US12097681

申请日：2006-12-14

Applicant: Dominik Feuerbach ,  Mathias Frederiksen ,  Konstanze Hurth ,  Bernard Lucien Roy ,  Beatrix Wagner

Inventor： Dominik Feuerbach ,  Mathias Frederiksen ,  Konstanze Hurth ,  Bernard Lucien Roy ,  Beatrix Wagner

IPC: C07D471/08 ,  A61K31/439

CPC classification number: C07D471/08 ,  A61K31/439 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06

Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及式（I）的1-氮杂 - 双环烷基衍生物，其中取代基如说明书中所定义，及其制备方法，作为药物的用途以及包含它们的药物组合物。

公开(公告)号：US20080255135A1

公开(公告)日：2008-10-16

申请号：US12090931

申请日：2006-10-19

Applicant: Dominik Feuerbach ,  Mathias Frederiksen ,  Martin Marzi ,  Bernard Lucien Roy

Inventor： Dominik Feuerbach ,  Mathias Frederiksen ,  Martin Marzi ,  Bernard Lucien Roy

IPC: A61K31/501 ,  C07D487/08 ,  A61P25/18 ,  A61K31/439

CPC classification number: C07D453/02

Abstract: The present invention provides a compound of formula (I) where X, R, Y, D, A and B are as defined herein.

Abstract translation: 本发明提供式（I）化合物，其中X，R，Y，D，A和B如本文所定义。

公开(公告)号：US08933090B2

公开(公告)日：2015-01-13

申请号：US12907506

申请日：2010-10-19

Applicant: Dominik Feuerbach ,  Werner Müller ,  Bernard Lucien Roy ,  Thomas J. Troxler ,  Konstanze Hurth ,  Mathias Frederiksen

Inventor： Dominik Feuerbach ,  Werner Müller ,  Bernard Lucien Roy ,  Thomas J. Troxler ,  Konstanze Hurth ,  Mathias Frederiksen

IPC: A61K31/506 ,  C07D239/28 ,  C07D471/08 ,  A61P29/00 ,  A61P25/28 ,  A61P25/16 ,  A61P25/24

CPC classification number: C07D471/08

Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.

Abstract translation: 本发明涉及式（I）的1-氮杂 - 双环烷基衍生物; 其中取代基如本说明书中所定义，其制备方法，它们作为药物的用途以及包含它们的药物组合物。 式（I）其中A表示O或N（R1）; Y表示一组式，或其中左键连接至A基团，右键连接至R基团; R代表取代或未取代的C 5 -C 10芳基，取代或未取代的杂-C 5 -C 10芳基，基团N（R 1）（R 4）或基团N（R 2）（CH 3 R 4）。 R代表氢，C1-C4烷基或CF3; R 2表示氢，C 1 -C 4烷基或CF 3; R3表示氢，C1-C4烷基或CF3; R4表示取代或未取代的C5-C10芳基或取代或未取代的C5-C10杂芳基; 在游离碱或酸加成盐形式。

公开(公告)号：US08173667B2

公开(公告)日：2012-05-08

申请号：US12090931

申请日：2006-10-19

Applicant: Dominik Feuerbach ,  Mathias Frederiksen ,  Martin Marzi ,  Bernard Lucien Roy

Inventor： Dominik Feuerbach ,  Mathias Frederiksen ,  Martin Marzi ,  Bernard Lucien Roy

IPC: A61K31/44 ,  C07D453/02 ,  C07D221/04 ,  A61P29/00 ,  A61P25/22 ,  A61P25/28 ,  A61P25/16 ,  A61P25/24 ,  A61P25/18 ,  A61P25/08

CPC classification number: C07D453/02

Abstract: The present invention provides a compound of formula (I) where X, R, Y, D, A and B are as defined herein.

Abstract translation: 本发明提供式（I）化合物，其中X，R，Y，D，A和B如本文所定义。

公开(公告)号：US20110034475A1

公开(公告)日：2011-02-10

申请号：US12907506

申请日：2010-10-19

Applicant: Dominik FEUERBACH ,  Werner Müller ,  Bernard Lucien Roy ,  Thomas J. Troxler ,  Konstanze Hurth ,  Mathias Frederiksen

Inventor： Dominik FEUERBACH ,  Werner Müller ,  Bernard Lucien Roy ,  Thomas J. Troxler ,  Konstanze Hurth ,  Mathias Frederiksen

IPC: A61K31/501 ,  C07D487/08 ,  A61K31/439 ,  A61K31/506 ,  A61P25/18 ,  A61P25/28

CPC classification number: C07D471/08

Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.

Abstract translation: 本发明涉及式（I）的1-氮杂 - 双环烷基衍生物; 其中取代基如本说明书中所定义，其制备方法，它们作为药物的用途以及包含它们的药物组合物。 式（I）其中A表示O或N（R1）; Y表示一组式，或其中左键连接至A基团，右键连接至R基团; R代表取代或未取代的C 5 -C 10芳基，取代或未取代的杂-C 5 -C 10芳基，基团N（R 1）（R 4）或基团N（R 2）（CH 3 R 4）。 R代表氢，C1-C4烷基或CF3; R 2表示氢，C 1 -C 4烷基或CF 3; R3表示氢，C1-C4烷基或CF3; R4表示取代或未取代的C5-C10芳基或取代或未取代的C5-C10杂芳基; 在游离碱或酸加成盐形式。