公开(公告)号：US09139577B2

公开(公告)日：2015-09-22

申请号：US14315399

申请日：2014-06-26

Applicant: Andreas Blum ,  Dirk Gottschling ,  Armin Heckel ,  Joerg P. Hehn ,  Bernhard Schmid ,  Dieter Wiedenmayer

Inventor： Andreas Blum ,  Dirk Gottschling ,  Armin Heckel ,  Joerg P. Hehn ,  Bernhard Schmid ,  Dieter Wiedenmayer

IPC: C07D413/14 ,  C07D239/94 ,  A61K31/517 ,  C07D409/12 ,  C07D401/12 ,  C07D413/12 ,  C07D411/12 ,  C07D409/14 ,  C07D495/10 ,  C07D403/12 ,  A61K45/06 ,  A61K31/541 ,  C07D401/14 ,  C07D405/12 ,  C07D417/04 ,  C07D417/14

CPC classification number: C07D239/94 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D411/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D495/10

Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.

Abstract translation: 本发明涉及式I的新型磺酰亚胺取代的喹唑啉衍生物，其中Ar，R 1和R 2如说明书和权利要求中所定义，以及它们作为MNK1（MNK1a或MNK1b）和/或MNK2（MNK2a或MNK2b）激酶抑制剂，药物 含有该化合物的组合物，以及使用其作为治疗或改善MNK1（MNK1a或MNK1b）和/或MNK2（MNK2a或MNK2b）介导的病症的药剂的方法。

公开(公告)号：US09073954B2

公开(公告)日：2015-07-07

申请号：US14330017

申请日：2014-07-14

Applicant: Joerg Kley ,  Sara Frattini ,  Dieter Hamprecht ,  Armin Heckel

Inventor： Joerg Kley ,  Sara Frattini ,  Dieter Hamprecht ,  Armin Heckel

IPC: C07D403/12 ,  C07D403/14 ,  C07D493/04 ,  C07F9/6509 ,  A61K31/675 ,  A61K45/06 ,  A61K31/497 ,  A61K31/683 ,  A61K31/5377

CPC classification number: C07F9/650952 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/675 ,  A61K31/683 ,  A61K45/06 ,  C07D403/12 ,  C07D403/14 ,  C07D493/04

Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.

Abstract translation: 本发明涉及通式（I）的化合物及其互变异构体及其盐，特别是其与无机或有机酸和碱的药学上可接受的盐，其具有有价值的药理学性质，特别是对上皮钠通道的抑制作用， 其用于治疗疾病，特别是肺和气道疾病。

公开(公告)号：US08853193B2

公开(公告)日：2014-10-07

申请号：US13035023

申请日：2011-02-25

Applicant: Armin Heckel ,  Frank Himmelsbach ,  Joerg Kley ,  Thorsten Lehmann-Lintz ,  Norbert Redemann ,  Achim Sauer ,  Leo Thomas ,  Dieter Wiedenmayer ,  Phillip Black ,  Wesley Blackaby ,  Ian Linney ,  Matthias Austen ,  John Danilewicz ,  Martin Schneider ,  Kay Schreiter

Inventor： Armin Heckel ,  Frank Himmelsbach ,  Joerg Kley ,  Thorsten Lehmann-Lintz ,  Norbert Redemann ,  Achim Sauer ,  Leo Thomas ,  Dieter Wiedenmayer ,  Phillip Black ,  Wesley Blackaby ,  Ian Linney ,  Matthias Austen ,  John Danilewicz ,  Martin Schneider ,  Kay Schreiter

IPC: C07D495/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/56 ,  A61P29/00 ,  A61P35/00 ,  A61P25/28 ,  A61P13/12 ,  A61K31/395

CPC classification number: C07D495/04

Abstract: The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.

Abstract translation: 本发明涉及包含这些化合物的通式药物组合物的新型噻吩并嘧啶化合物及其用于预防和/或治疗可受到抑制Mnk1和/或Mnk2（Mnk2a或Mnk2b的激酶活性）的疾病的治疗用途 ）和/或其变体。

公开(公告)号：US20140135309A1

公开(公告)日：2014-05-15

申请号：US14073907

申请日：2013-11-07

Applicant: Andreas BLUM ,  Dirk GOTTSCHLING ,  Armin HECKEL ,  Joerg HEHN ,  Thorsten LEHMANN-LINTZ ,  Dieter WIEDENMAYER

Inventor： Andreas BLUM ,  Dirk GOTTSCHLING ,  Armin HECKEL ,  Joerg HEHN ,  Thorsten LEHMANN-LINTZ ,  Dieter WIEDENMAYER

IPC: A61K31/541 ,  A61K31/517 ,  C07D405/12 ,  C07D409/14 ,  A61K45/06 ,  C07D239/94 ,  C07D401/14 ,  C07D405/14 ,  C07D411/14 ,  C07D417/12 ,  C07D493/04 ,  C07D401/12

CPC classification number: A61K31/541 ,  A61K31/517 ,  A61K45/06 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D411/14 ,  C07D417/12 ,  C07D493/04

Abstract: This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined herein, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.

Abstract translation: 本发明涉及式I的新型磺酰亚胺取代喹唑啉衍生物，其中Ar，R 1和R 2如本文所定义，以及它们作为MNK1（MNK1a或MNK1b）和/或MNK2（MNK2a或MNK2b）激酶抑制剂的用途，含有它们的药物组合物 以及使用其作为治疗或改善MNK1（MNK1a或MNK1b）和/或MNK2（MNK2a或MNK2b）介导的病症的药剂的方法。

公开(公告)号：US20140128409A1

公开(公告)日：2014-05-08

申请号：US14153542

申请日：2014-01-13

Applicant: John Edward PARK ,  Nveed CHAUDHARY ,  Gerald Juergen ROTH ,  Armin HECKEL ,  Thorsten LEHMANN-LINTZ ,  Joerg KLEY

Inventor： John Edward PARK ,  Nveed CHAUDHARY ,  Gerald Juergen ROTH ,  Armin HECKEL ,  Thorsten LEHMANN-LINTZ ,  Joerg KLEY

IPC: A61K31/496 ,  C07D403/06 ,  A61K31/4178 ,  A61K31/404 ,  C07D209/34

CPC classification number: A61K31/496 ,  A61K31/404 ,  A61K31/4178 ,  C07D209/34 ,  C07D403/06

Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R6 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.

Abstract translation: 本发明涉及在6位上被取代的通式的二氢吲哚酮的用途，其中R 1至R 6和X如权利要求1中所定义，其异构体及其盐，特别是其生理上可接受的盐作为药物用于 预防或治疗特定的纤维化疾病。

公开(公告)号：US07989474B2

公开(公告)日：2011-08-02

申请号：US12334323

申请日：2008-12-12

Applicant: Gerald Juergen Roth ,  Armin Heckel ,  Rainer Walter ,  Frank Hilberg ,  Rudolf Hauptmann ,  Martin Fredrich Stefanic ,  Florian Colbatzky ,  Steffan Ernest

Inventor： Gerald Juergen Roth ,  Armin Heckel ,  Rainer Walter ,  Frank Hilberg ,  Rudolf Hauptmann ,  Martin Fredrich Stefanic ,  Florian Colbatzky ,  Steffan Ernest

IPC: A61K31/445

CPC classification number: A61K45/06 ,  A61K31/404 ,  A61K31/454 ,  A61K31/517 ,  A61K2300/00

Abstract: The invention relates to a method of treating immunologic diseases or pathological conditions involving an immunologic component using certain Lck inhibitors already known as kinase inhibitors for therapy in oncology, optionally in combination with one or more other drugs selected from NSAIDs, steroids, DMARDs, immunsuppressives, biologic response modifiers and antinfectives, pharmaceutical compositions comprising said Lck inhibitors together with said other drugs, and the use of the Lck inhibitors for the manufacture of a pharmaceutical composition for the treatment of immunologic diseases or pathological conditions involving an immunologic component.

Abstract translation: 本发明涉及一种治疗免疫学疾病或病理状态的方法，该方法使用已知的用作肿瘤学治疗的激酶抑制剂的某些Lck抑制剂，任选与一种或多种其它选自NSAID，类固醇，DMARD，免疫抑制剂， 生物反应调节剂和抗感染剂，包含所述Lck抑制剂与所述其它药物的药物组合物，以及使用Lck抑制剂制备用于治疗免疫学疾病或涉及免疫组分的病理状况的药物组合物。

公开(公告)号：US20100204211A1

公开(公告)日：2010-08-12

申请号：US12645151

申请日：2009-12-22

Applicant: John Edward PARK ,  Gerald Juergen ROTH ,  Armin HECKEL ,  Nveed CHAUDHARY ,  Trixi BRANDL ,  Georg DAHMANN ,  Matthias GRAUERT

Inventor： John Edward PARK ,  Gerald Juergen ROTH ,  Armin HECKEL ,  Nveed CHAUDHARY ,  Trixi BRANDL ,  Georg DAHMANN ,  Matthias GRAUERT

IPC: A61K31/496 ,  A61K31/404 ,  A61K31/551 ,  A61K31/5377 ,  A61P11/00

CPC classification number: A61K31/4045 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/44 ,  A61K31/445 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D209/34 ,  C07D295/155 ,  C07D295/215 ,  C07D401/12 ,  C07D403/12 ,  A61K2300/00

Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.

Abstract translation: 本发明涉及在6位上被取代的通式的二氢吲哚酮的用途，其中R 1至R 5和X如权利要求1中所定义，其异构体及其盐，特别是其生理上可接受的盐作为药物用于 预防或治疗特定的纤维化疾病。

公开(公告)号：US20060142373A1

公开(公告)日：2006-06-29

申请号：US11275223

申请日：2005-12-20

Applicant: John Park ,  Gerald Roth ,  Armin Heckel ,  Nveed Chaudhary ,  Trixi Brandl ,  Georg Dahmann ,  Matthias Grauert

Inventor： John Park ,  Gerald Roth ,  Armin Heckel ,  Nveed Chaudhary ,  Trixi Brandl ,  Georg Dahmann ,  Matthias Grauert

IPC: A61K31/404

CPC classification number: A61K31/4045 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/44 ,  A61K31/445 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D209/34 ,  C07D295/155 ,  C07D295/215 ,  C07D401/12 ,  C07D403/12 ,  A61K2300/00

Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.

Abstract translation: 本发明涉及在6位上被取代的通式的二氢吲哚酮的用途，其中R 1至R 5和X如权利要求1所定义，异构体和 其盐，特别是其生理上可接受的盐作为预防或治疗特定纤维化疾病的药物。

公开(公告)号：US20050203104A1

公开(公告)日：2005-09-15

申请号：US11077355

申请日：2005-03-10

Applicant: Armin Heckel ,  Gerald Roth ,  Joerg Kley ,  Stefan Hoerer ,  Ingo Uphues

Inventor： Armin Heckel ,  Gerald Roth ,  Joerg Kley ,  Stefan Hoerer ,  Ingo Uphues

IPC: A61K31/404 ,  A61K31/454 ,  A61K31/496 ,  C07D209/34 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D451/14

CPC classification number: C07D209/34 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D451/14

Abstract: The present invention relates to cycloalkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined as in claims 1 to 6, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).

Abstract translation: 本发明涉及通式如下的环烷基5-丙烯基吲哚酮：其中R 1至R 3定义如权利要求1至6中所述，互变异构体，对映异构体， 具有有价值的药理学特性，特别是对蛋白激酶的抑制作用，特别是对糖原合酶激酶（GSK-3）的活性的抑制作用的非对映异构体，其混合物及其盐。

公开(公告)号：US06794395B1

公开(公告)日：2004-09-21

申请号：US10069557

申请日：2002-07-22

Applicant: Gerald Juergen Roth ,  Armin Heckel ,  Rainer Walter ,  Ulrike Tontsch-Grunt ,  Walter Spevak ,  Jacobus C. A. Van Meel

Inventor： Gerald Juergen Roth ,  Armin Heckel ,  Rainer Walter ,  Ulrike Tontsch-Grunt ,  Walter Spevak ,  Jacobus C. A. Van Meel

IPC: A61K31404

CPC classification number: C07D401/04 ,  C04B35/632 ,  C07D209/34 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D491/04

Abstract: The present invention relates to substituted indolinones of general formula wherein R1 to R6 and X are defined as in claim 1, the isomers and the salts thereof, in particular the physiologically acceptable salts thereof which have valuable pharmacological properties, especially an inhibitory effect on various receptor-tyrosine kinases, and cycline/CDK complexes as well as on the proliferation of endothelial cells and various tumor cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Abstract translation: 本发明涉及通式为R 1至R 6的取代的二氢吲哚酮和X如权利要求1所定义，其异构体及其盐，特别是其生理上可接受的盐具有有价值的药理学性质，特别是对各种受体酪氨酸的抑制作用 激酶和循环/ CDK复合物以及内皮细胞和各种肿瘤细胞的增殖，含有这些化合物的药物组合物，其用途和制备方法。