公开(公告)号：US20160168131A1

公开(公告)日：2016-06-16

申请号：US14907225

申请日：2014-07-24

Applicant: NOVARTIS AG

Inventor： Zhenxing DU ,  Samuel HINTERMANN ,  Konstanze HURTH ,  Sébastien JACQUIER ,  Hansjoerg LEHMANN ,  Henrik MOEBITZ ,  Nicolas SOLDERMANN ,  Aleksandar STOJANOVIC

IPC: C07D403/14 ,  A61K31/52 ,  C07D473/16 ,  A61K31/517 ,  C07D417/14

CPC classification number: C07D403/14 ,  A61K31/517 ,  A61K31/52 ,  C07D401/14 ,  C07D417/14 ,  C07D473/16

Abstract: Provided are substituted quinazolin-4-one compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein R1, R2, R3, R5, R6 and L are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the class I PI3K kinases.

Abstract translation: 提供式（I）的取代喹唑啉-4-酮化合物和/或其药学上可接受的盐和/或溶剂合物，其中R1，R2，R3，R5，R6和L如说明书中所定义。 这些化合物适用于治疗由I型PI3K激酶的活性介导的病症或疾病。

公开(公告)号：US20130165436A1

公开(公告)日：2013-06-27

申请号：US13721805

申请日：2012-12-20

Applicant: Novartis AG

Inventor： Giorgio CARAVATTI ,  Sylvie CHAMOIN ,  Pascal FURET ,  Klemens HOGENAUER ,  Konstanze HURTH ,  Christoph KALIS ,  Karen KAMMERTOENS ,  Ian LEWIS ,  Henrik MOEBITZ ,  Alexander Baxter SMITH ,  Nicolas SOLDERMANN ,  Romain WOLF ,  Frederic ZECRI

IPC: A61K31/538 ,  C07D413/14

CPC classification number: A61K31/5383 ,  A61K31/538 ,  C07D413/14 ,  C07D498/04 ,  C12N9/12 ,  C12Q1/25 ,  C12Q1/686 ,  Y02A50/409 ,  Y02A50/411

Abstract: The invention relates to dihydro-benzo-oxazine and dihydro-pyrido-oxazine compounds of the formula (I) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein Y, V, W, U, Q, R1, R5, R7 and R30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.

Abstract translation: 本发明涉及式（I）的二氢 - 苯并恶嗪和二氢 - 吡啶并恶嗪化合物和/或其药学上可接受的盐和/或溶剂合物，其中Y，V，W，U，Q，R 1，R 5，R 7 和R30如说明书中所定义。 这些化合物适用于治疗由PI3K酶的活性介导的病症或疾病。

公开(公告)号：US20150087650A1

公开(公告)日：2015-03-26

申请号：US14558776

申请日：2014-12-03

Applicant: NOVARTIS AG

Inventor： Dominik FEUERBACH ,  Werner Müller ,  Bernard Lucien ROY ,  Thomas TROXLER ,  Konstanze HURTH ,  Mathias FREDERIKSEN

IPC: C07D471/08

CPC classification number: C07D471/08

Abstract: The present invention relates to 1-aza-bicy-cloalkyl 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(R′); 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（R'）; 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：US20250115572A1

公开(公告)日：2025-04-10

申请号：US18729949

申请日：2023-01-20

Applicant: Novartis AG

Inventor： Christopher M. ADAMS ,  Lara C. CZABANIUK ,  Stefanie FLOHR ,  François GESSIER ,  Michael Christoph HEDIGER ,  Konstanze HURTH ,  Nancy LABBE-GIGUERE ,  Fabio LIMA ,  Tajesh PATEL ,  Oliver SIMIC ,  Martin SENDZIK ,  Angela VITREY ,  Anna VULPETTI

IPC: C07D401/06 ,  A61K31/438 ,  A61K31/444 ,  C07D401/14 ,  C07D405/14

Abstract: Provided herein are compounds of formula (I) and pharmaceutical compositions thereof useful for treating diseases or disorders mediated by the complement factor B. (I).

公开(公告)号：US20140256940A1

公开(公告)日：2014-09-11

申请号：US14285942

申请日：2014-05-23

Applicant: NOVARTIS AG

Inventor： Mathias FREDERIKSEN ,  Dominik FEUERBACH ,  Konstanze HURTH ,  Manuel KOLLER ,  Bernard Lucien ROY

IPC: C07D471/08

CPC classification number: C07D471/08 ,  A61K31/429

Abstract: The present invention related to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5, represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate, Y represents one of the following groups: (Ia) in free base or acid addition salt form, to processes for their production, to pharmaceutical compositions comprising them and their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and neurodegenerative disorders.

Abstract translation: 本发明涉及式（I）化合物，其中n代表0,1,2,3,4或5相互独立地表示羟基，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代表以下基团之一：游离碱或酸加成盐形式的（Ia），其制备方法，包含它们的药物组合物及其在制备用于治疗和/或 延迟精神病和神经退行性疾病的进展。

公开(公告)号：US20170320864A1

公开(公告)日：2017-11-09

申请号：US15385147

申请日：2016-12-20

Applicant: NOVARTIS AG

Inventor： Sangamesh BADIGER ,  Murali CHEBROLU ,  Konstanze HURTH ,  Sebastien JACQUIER ,  Rainer Martin LUEOEND ,  Rainer MACHAUER ,  Heinrich RUEEGER ,  Marina TINTELNOT-BLOMLEY ,  Siem Jacob VEENSTRA ,  Markus VOEGTLE

IPC: C07D413/14 ,  A61K31/5377 ,  C07D487/04 ,  C07D471/04 ,  C07B59/00

CPC classification number: C07D413/14 ,  A61K31/5377 ,  C07B59/002 ,  C07B2200/05 ,  C07D471/04 ,  C07D487/04 ,  A61K2300/00

Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.

公开(公告)号：US20140113908A1

公开(公告)日：2014-04-24

申请号：US14138527

申请日：2013-12-23

Applicant: NOVARTIS AG

Inventor： Dominik FEUERBACH ,  Mathias FREDERIKSEN ,  Konstanze HURTH ,  Bernard Lucien ROY ,  Beatrix WAGNER

IPC: C07D471/08 ,  A61K31/506 ,  A61K45/06 ,  A61K31/439 ,  A61K31/501

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：US20140057921A1

公开(公告)日：2014-02-27

申请号：US14068004

申请日：2013-10-31

Applicant: NOVARTIS AG

Inventor： Dominik FEUERBACH ,  Mathias FREDERIKSEN ,  Konstanze HURTH ,  Bernard Lucien ROY

IPC: C07D453/02

CPC classification number: C07D453/02 ,  C07D487/08

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 in the prevention and treatment of psychotic and neurodegenerative disorders. The claimed compounds act as nicotinic acetylcholine receptors (NACHR) ligands.

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，其制备方法，它们作为药物用于预防和治疗精神病和神经变性疾病。 所要求的化合物作为烟碱乙酰胆碱受体（NACHR）配体。