公开(公告)号：US20210079018A1

公开(公告)日：2021-03-18

申请号：US16764563

申请日：2018-11-15

申请人： The Broad Institute, Inc. ,  Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

发明人： Steven J. Ferrara ,  Michael H. Serrano-Wu ,  Christopher Lemke ,  David McKinney ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Laura Furst ,  Guo Wei ,  Patrick Ryan MacCarren ,  Kai Thede ,  Anne Mengel ,  Clara Christ ,  Joachim Kuhnke ,  Sarah Anna Liesa Johannes ,  Philipp Buchgraber ,  Ulrich Klar ,  Ulrike Sack ,  Stefan Kaulfuss ,  Amaury Ernesto Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Mönning

IPC分类号： C07D498/14 ,  C07D487/14 ,  A61P35/00

摘要： The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

公开(公告)号：US10130633B2

公开(公告)日：2018-11-20

申请号：US14778568

申请日：2014-03-17

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Kai Thede ,  William Scott ,  Eckhard Bender ,  Stefan Golz ,  Andrea Hägebarth ,  Philip Lienau ,  Florian Puehler ,  Daniel Basting ,  Dirk Schneider ,  Manfred Möwes ,  Anja Richter ,  Ludwig Zorn ,  Ningshu Liu ,  Ursula Mönning ,  Franziska Siegel

IPC分类号： A61K31/5377 ,  A61K31/5386 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/433 ,  A61K31/4418 ,  A61K31/4995 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07C205/45 ,  C07C233/54 ,  C07C233/15 ,  C07C205/59 ,  C07C317/44 ,  C07C229/64 ,  C07C255/56 ,  C07D213/75 ,  C07D295/15 ,  C07D213/82 ,  C07D333/38 ,  C07D285/135 ,  C07D295/155 ,  C07D213/76 ,  C07D213/73 ,  C07D277/56 ,  C07D231/14 ,  C07D401/12 ,  C07D417/12 ,  C07D263/34 ,  C07D487/08 ,  C07D271/06 ,  C07D271/07 ,  C07D271/113 ,  C07D207/34 ,  C07D498/08 ,  C07D277/46

摘要： The present invention relates to substituted N-(phenyl-heteroaryl)-3-acetylamino-benzamides and N-[3-(acetylamino)phenyl]-phenyl-heteroaryl-carboxamides of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease such as cancer, wherein i.a.: LA represents an optionally substituted methylene or ethylene group; LB represents —N(H)—C(═O)— or —C(═O)—N(H)—; R1 represents an optionally substituted 5- to 8-membered heterocycloalkyl, 4- to 10-membered heterocycloalkenyl, aryl, heteroaryl or —N(R7)(Ci-C6-alkyl) group; R2 represents an optionally substituted 5- or 6-membered heteroaryl group; R3 represents an optionally substituted phenyl group.

公开(公告)号：US20150203483A1

公开(公告)日：2015-07-23

申请号：US14421994

申请日：2013-08-13

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Stephan Siegel ,  Stefan Bäurle ,  Arwed Cleve ,  Bernard Haendler ,  Amaury Ernesto Fernandiez-Montalvan ,  Ursula Mönning ,  Sabine Krause ,  Pascale Lejeune ,  Norbert Schmees ,  Matthias Busemann ,  Simon Holton ,  Joachim Kuhnke

IPC分类号： C07D417/10 ,  A61K31/551 ,  C07D413/10 ,  C07D403/10 ,  C07D413/14 ,  C07D409/10 ,  C07D401/04 ,  C07D401/14 ,  A61K31/5513 ,  C07D401/12 ,  C07D243/02 ,  C07D401/10

CPC分类号： C07D417/10 ,  A61K31/551 ,  A61K31/5513 ,  C07D243/02 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14

摘要： What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumour disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.

摘要翻译： 描述了通式（I）的BET蛋白抑制性特别是BRD4抑制性2,3-苯二氮卓类，其中R1a，R1b，R1c，R2，R3，R4，R5，A和X具有 描述，用于制备根据本发明的化合物的中间体，包含根据本发明的化合物的药物组合物及其对过度增殖性疾病，特别是肿瘤病症的预防和治疗用途。 还描述了BET蛋白抑制剂用于良性增生，动脉粥样硬化性疾病，败血症，自身免疫性疾病，血管病症，病毒感染，神经变性疾病，炎症性疾病，动脉粥样硬化性疾病和用于控制雄性生育力的用途。

公开(公告)号：US11339157B1

公开(公告)日：2022-05-24

申请号：US16758018

申请日：2018-10-23

申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft ,  Dana-Farber Cancer Institute, Inc. ,  The Broad Institute, Inc.

发明人： Stephan Siegel ,  Franziska Siegel ,  Volker Schulze ,  Markus Berger ,  Keith Graham ,  Ulrich Klar ,  Knut Eis ,  Detlev Sülzle ,  Ulf Bömer ,  Daniel Korr ,  Kirstin Petersen ,  Ursula Mönning ,  Uwe Eberspächer ,  Dieter Moosmayer ,  Matthew Meyerson ,  Heidi Greulich ,  Bethany Kaplan ,  Hassan Youssef Harb ,  Phi Manh Dinh

IPC分类号： C07D471/04 ,  A61P35/00 ,  A61K45/06

摘要： Compounds of formula (I) processes for their production and their use as pharmaceuticals.

公开(公告)号：US20220281891A1

公开(公告)日：2022-09-08

申请号：US17691862

申请日：2022-03-10

申请人： The Broad Institute, Inc. ,  Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

发明人： Steven J. Ferrara ,  Michael H. Serrano-Wu ,  Chris Lemke ,  David McKinney ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Laura Furst ,  Guo Wei ,  Patrick Ryan McCarren ,  Kai Thede ,  Anne Mengel ,  Clara Christ ,  Joachim Kuhnke ,  Sarah Anna Liesa Johannes ,  Philipp Buchgraber ,  Ulrich Klar ,  Ulrike Rauh ,  Stefan Kaulfuss ,  Amaury Ernesto Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Mönning

IPC分类号： C07D498/14 ,  A61P35/00 ,  C07D487/14

摘要： The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

公开(公告)号：US20210292341A1

公开(公告)日：2021-09-23

申请号：US16764672

申请日：2018-11-15

申请人： The Broad Institute, Inc. ,  Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

发明人： Laura Furst ,  Michael H. Serrano-Wu ,  Christopher Lemke ,  David McKinney ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Steven James Ferrara ,  Guo Wei ,  Patrick Ryan McCarren ,  Kai Thede ,  Anne Mengel ,  Clara Christ ,  Joachim Kuhnke ,  Sarah Anna Liesa Johannes ,  Philipp Buchgraber ,  Ulrich Klar ,  Ulrike Sack ,  Stefan Kaulfuss ,  Amaury Ernesto Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Mönning ,  Katrin Nowak-Reppel

IPC分类号： C07D513/14 ,  A61K31/5377 ,  A61K31/4162 ,  A61K31/454 ,  A61K45/06 ,  A61P35/02 ,  A61P35/00

摘要： The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

公开(公告)号：US20210269456A1

公开(公告)日：2021-09-02

申请号：US16764668

申请日：2018-11-15

申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft ,  The Broad Institute, Inc.

发明人： Kai Thede ,  Anne Mengel ,  Clara Christ ,  Joachim Kuhnke ,  Sarah Anna Liesa Johannes ,  Philipp Buchgraber ,  Ulrich Klar ,  Ulrike Sack ,  Stefan Kaulfuss ,  Amaury Ernesto Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Mönning ,  Katrin Nowak-Reppel ,  Sven Wittrock ,  David McKinney ,  Michael H. Serrano-Wu ,  Christopher Lemke ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Steven James Ferrara ,  Laura Furst ,  Guo Wei ,  Patrick Ryan McCarren ,  Rebecca Ann Harvey

IPC分类号： C07D498/14 ,  A61K31/4162 ,  A61K31/5377 ,  C07D498/22 ,  C07D487/14 ,  C07D471/22 ,  C07D487/22 ,  A61P35/00 ,  A61P35/02 ,  A61K45/06 ,  A61K31/496 ,  A61K31/437

摘要： The present invention relates to substituted macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

公开(公告)号：US09890147B2

公开(公告)日：2018-02-13

申请号：US14421994

申请日：2013-08-13

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Stephan Siegel ,  Stefan Bäurle ,  Arwed Cleve ,  Bernard Haendler ,  Amaury Ernesto Fernandez-Montalvan ,  Ursula Mönning ,  Sabine Krause ,  Pascale Lejeune ,  Norbert Schmees ,  Matthias Busemann ,  Simon Holton ,  Joachim Kuhnke

IPC分类号： A61K31/551 ,  C07D243/02 ,  C07D401/04 ,  C07D403/04 ,  C07D417/10 ,  C07D401/14 ,  C07D413/14 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/10 ,  A61K31/5513

CPC分类号： C07D417/10 ,  A61K31/551 ,  A61K31/5513 ,  C07D243/02 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D409/10 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14

摘要： What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumor disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.

公开(公告)号：US11286263B2

公开(公告)日：2022-03-29

申请号：US16764563

申请日：2018-11-15

申请人： The Broad Institute, Inc. ,  Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

发明人： Steven James Ferrara ,  Michael H. Serrano-Wu ,  Chris Lemke ,  David McKinney ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Laura Furst ,  Guo Wei ,  Patrick Ryan McCarren ,  Kai Thede ,  Anne Mengel ,  Clara Christ ,  Joachim Kuhnke ,  Sarah Anna Liesa Johannes ,  Philipp Buchgraber ,  Ulrich Klar ,  Ulrike Sack ,  Stefan Kaulfuss ,  Amaury Ernesto Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Mönning

IPC分类号： C07D487/14 ,  C07D403/14 ,  C07D498/14 ,  A61K31/4162 ,  A61P35/00

摘要： The present invention relates to macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

公开(公告)号：US09745285B2

公开(公告)日：2017-08-29

申请号：US14900548

申请日：2014-06-17

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Anne Mengel ,  Marion Hitchcock ,  Anja Richter ,  Lars Bärfacker ,  Hans Briem ,  Gerhard Siemeister ,  Wilhelm Bone ,  Amaury Ernesto Fernandez-Montalvan ,  Jens Schröder ,  Simon Holton ,  Cornelia Preuβe ,  Ursula Mönning

IPC分类号： C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  C07D413/14

CPC分类号： C07D401/14 ,  A61K31/506 ,  A61K45/06 ,  C07D413/14

摘要： Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.