公开(公告)号：WO2017106429A3

公开(公告)日：2017-08-17

申请号：PCT/US2016066799

申请日：2016-12-15

Applicant: BOEHRINGER INGELHEIM INT

Inventor： BOSANAC TODD ,  BENTZIEN JOERG ,  BURKE MICHAEL JASON ,  FRYER RYAN MICHAEL ,  LARSON ERIC THOMAS ,  TSCHANTZ MATT AARON ,  MCKIBBEN BRYAN PATRICK ,  MAO WANG ,  SHEN YUE ,  SOLEYMANZADEH FARIBA

IPC: C07D401/14 ,  A61K31/4155 ,  A61K31/4439 ,  A61P37/06 ,  C07D403/14

CPC classification number: C07D403/14 ,  C07D401/14

Abstract: The present invention encompasses compounds of the formula (I) wherein the groups R1, Cy and Y are defined herein, which are suitable for the treatment of diseases related to BTK, and processes for making these compounds, pharmaceutical preparations containing these compounds, and their methods of use.

Abstract translation: 本发明包括式（I）化合物，其中基团R1，Cy和Y在本文中定义，它们适用于治疗与BTK有关的疾病，以及制备这些化合物的方法，含有这些化合物的药物制剂和它们的 使用方法。

公开(公告)号：WO2015169431A3

公开(公告)日：2015-12-30

申请号：PCT/EP2015000903

申请日：2015-05-04

Applicant: BOEHRINGER INGELHEIM INT

Inventor： EICHER JOACHIM ,  GATZ JOSEF ,  HERRMANN FRANK ,  HOELZ HUBERT ,  JUNG ANDREE ,  MEISENHEIMER MARTIN ,  MUELLER MARKUS ,  VON SCHUCKMANN ALFRED ,  WACHTEL HERBERT ,  WINKLER ROBERT GERHARD ,  WUTTKER GILBERT ,  ZIEGLER JOCHEN

IPC: A61M15/00 ,  A61M11/00 ,  B05B11/00 ,  G06M1/02

CPC classification number: A61M15/0081 ,  A61M11/00 ,  A61M11/007 ,  A61M15/0021 ,  A61M15/0026 ,  A61M15/0035 ,  A61M15/0036 ,  A61M15/004 ,  A61M15/0041 ,  A61M15/0065 ,  A61M15/0071 ,  A61M15/0073 ,  A61M2202/0468 ,  A61M2205/273 ,  A61M2205/583 ,  A61M2205/586 ,  A61M2207/10 ,  B05B11/0054 ,  B05B11/308 ,  A61M2202/0007

Abstract: A nebulizer (1) as well as a container (3) with a fluid (2) and an indicator device (25) for such a nebulizer are proposed. The indicator device stops further use of the container in a locked state when a predetermined number of uses has been reached or exceeded. Then, the nebulizer is partially opened and blocked against further use. After replacement of the container including the indicator device, the nebulizer can be used again.

Abstract translation: 提出了一种喷雾器（1）以及具有流体（2）的容器（3）和用于这种雾化器的指示器装置（25）。 当达到或超过预定数量的使用时，指示装置停止在处于锁定状态的容器的进一步使用。 然后，雾化器部分打开并阻止进一步使用。 在更换包括指示装置的容器之后，可以再次使用雾化器。

公开(公告)号：WO2012122340A8

公开(公告)日：2013-04-25

申请号：PCT/US2012028205

申请日：2012-03-08

Applicant: BOEHRINGER INGELHEIM INT ,  BRENNEMAN JEHROD BURNETT ,  HUBER JOHN D ,  RAUDENBUSH BRIAN CHRISTOPHER ,  SARKO CHRISTOPHER RONALD

Inventor： BRENNEMAN JEHROD BURNETT ,  HUBER JOHN D ,  RAUDENBUSH BRIAN CHRISTOPHER ,  SARKO CHRISTOPHER RONALD

IPC: C07D401/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/55 ,  A61P9/00 ,  A61P13/00 ,  A61P25/00 ,  A61P29/00 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, A and B are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Abstract translation: 本发明涉及式（I）的化合物及其药学上可接受的盐，其中R1，R2。 R3，R4，R5，R6，A和B如本文所定义。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。

公开(公告)号：WO2011143772A9

公开(公告)日：2012-12-20

申请号：PCT/CA2011050308

申请日：2011-05-17

Applicant: BOEHRINGER INGELHEIM INT ,  LEPAGE OLIVIER ,  BHARDWAJ PUNIT K ,  FAUCHER ANNE-MARIE ,  GRAND-MAITRE CHANTAL ,  LACOSTE JEAN-ERIC ,  LAMORTE LOUIE ,  MERCIER JEAN-FRANCOIS

Inventor： LEPAGE OLIVIER ,  BHARDWAJ PUNIT K ,  FAUCHER ANNE-MARIE ,  GRAND-MAITRE CHANTAL ,  LACOSTE JEAN-ERIC ,  LAMORTE LOUIE ,  MERCIER JEAN-FRANCOIS

IPC: C07D487/04 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/497 ,  A61P31/18

CPC classification number: C07D487/04

Abstract: Compounds of formula (I) wherein R1, R2, n and R3 are defined herein, are useful as inhibitors of HIV replication.

Abstract translation: 其中R1，R2，n和R3在本文中定义的式（I）化合物可用作HIV复制的抑制剂。

公开(公告)号：WO2009052138A8

公开(公告)日：2012-11-15

申请号：PCT/US2008079925

申请日：2008-10-15

Applicant: BOEHRINGER INGELHEIM INT ,  BOEHRINGER INGELHEIM PHARMA ,  FRUTOS ROGELIO ,  KRISHNAMURTHY DHILEEPKUMAR ,  MULDER JASON ALAN ,  RODRIGUEZ SONIA ,  SENANAYAKE CHRIS HUGH ,  TAMPONE THOMAS G

Inventor： FRUTOS ROGELIO ,  KRISHNAMURTHY DHILEEPKUMAR ,  MULDER JASON ALAN ,  RODRIGUEZ SONIA ,  SENANAYAKE CHRIS HUGH ,  TAMPONE THOMAS G

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: The invention relates to improved methods of preparing dihydrothienopyrimidines of formula 1, and intermediates thereof,(I) wherein X is SO or SO2, preferably SO, and wherein RA, R1, R2, R3, R4 and R5 have the meanings given in the description. The methods according to this invention are more suitable for large-scale synthesis of said compounds than prior methods because the new synthetic process avoids distillation and chromatographic purification between steps and results in a higher overall yield of the desired product.

Abstract translation: 本发明涉及制备式1的二氢噻吩并嘧啶的改进方法及其中间体，其中X是SO或SO 2，优选SO，其中RA，R 1，R 2，R 3，R 4和R 5具有在说明书中给出的含义 。 根据本发明的方法比现有方法更适合于大规模合成所述化合物，因为新的合成方法避免了步骤之间的蒸馏和色谱纯化并导致所需产物的更高的总产率。

公开(公告)号：WO2011138427A3

公开(公告)日：2012-03-08

申请号：PCT/EP2011057285

申请日：2011-05-06

Applicant: BOEHRINGER INGELHEIM INT ,  GRAUERT MATTHIAS ,  BAKKER REMKO ,  BREITFELDER STEFFEN ,  BUETTNER FRANK ,  EICKELMANN PETER ,  FOX THOMAS ,  GRUNDL MARC ,  LEHMANN-LINTZ THORSTEN ,  RIST WOLFGANG

Inventor： GRAUERT MATTHIAS ,  BAKKER REMKO ,  BREITFELDER STEFFEN ,  BUETTNER FRANK ,  EICKELMANN PETER ,  FOX THOMAS ,  GRUNDL MARC ,  LEHMANN-LINTZ THORSTEN ,  RIST WOLFGANG

IPC: C07D413/04 ,  A61K31/501 ,  A61P3/00 ,  C07D413/14

CPC classification number: C07D413/10 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D453/02 ,  C07D498/04

Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.

Abstract translation: 本发明涉及通式I的哒嗪酮衍生物，其中基团A，G和R 1如本申请中所定义，其互变异构体，其立体异构体，其混合物及其盐具有有价值的药理学性质， 特异性结合GPR119受体并调节其活性。

公开(公告)号：WO2011003853A3

公开(公告)日：2012-01-19

申请号：PCT/EP2010059546

申请日：2010-07-05

Applicant: BOEHRINGER INGELHEIM INT ,  BARTA ALBERT

Inventor： BARTA ALBERT

IPC: A61K9/20 ,  A61J3/10 ,  A61K9/16 ,  A61K9/28 ,  A61K31/517

CPC classification number: A61K31/517 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2095 ,  A61K9/2813 ,  A61K9/2826 ,  A61K9/2853 ,  A61K9/2866

Abstract: The present invention relates to a drying process of BIBW 2992 or the salts thereof, preferably the dimaleate salt, as well as of solid pharmaceutical formulations comprising BIBW2992 or a salt thereof, and to pharmaceutical compositions comprising BIBW 2992 or a salt thereof as the active product ingredient, characterized by a water activity of the formulation of not more than 0.20 or a water content (Karl-Fischer) of not more than 4.2 %.

Abstract translation: 本发明涉及BIBW 2992或其盐，优选二马来酸盐以及包含BIBW2992或其盐的固体药物制剂的干燥方法，以及包含BIBW 2992或其盐作为活性产物的药物组合物 成分，其特征在于制剂的水分活度不超过0.20或水含量（卡尔费休）不超过4.2％。

公开(公告)号：WO2011089183A3

公开(公告)日：2011-11-17

申请号：PCT/EP2011050749

申请日：2011-01-20

Applicant: BOEHRINGER INGELHEIM INT ,  VAN RYN JOANNE ,  PARK JOHN EDWARD ,  HAUEL NORBERT ,  KUNZ ULRICH ,  LITZENBURGER TOBIAS ,  CANADA KEITH ,  SINGH SANJAYA ,  WATERMAN ALISA

Inventor： VAN RYN JOANNE ,  PARK JOHN EDWARD ,  HAUEL NORBERT ,  KUNZ ULRICH ,  LITZENBURGER TOBIAS ,  CANADA KEITH ,  SINGH SANJAYA ,  WATERMAN ALISA

IPC: A61K39/00 ,  C07K16/44

CPC classification number: C07K16/44 ,  A61K31/4439 ,  A61K39/39583 ,  C07K2317/24 ,  C07K2317/54 ,  C07K2317/55 ,  C07K2317/565 ,  C07K2317/569 ,  C07K2317/622 ,  C07K2317/626 ,  C07K2317/76 ,  G01N33/86 ,  G01N2500/02 ,  G01N2500/10

Abstract: The present invention relates to antibody molecules against anticoagulants, in particular dabigatran, and their use as antidotes of such anticoagulants.

Abstract translation: 本发明涉及针对抗凝血剂的抗体分子，特别是达比加群，以及它们作为此类抗凝剂的解毒剂的用途。

公开(公告)号：WO2011039307A4

公开(公告)日：2011-07-28

申请号：PCT/EP2010064562

申请日：2010-09-30

Applicant: BOEHRINGER INGELHEIM INT ,  KAEMPER MARKUS ,  SCHULZ JOERN-ERIC

Inventor： KAEMPER MARKUS ,  SCHULZ JOERN-ERIC

IPC: A61M15/00

CPC classification number: A61M15/0028 ,  A61M15/0026 ,  A61M15/0035 ,  A61M15/0061 ,  A61M15/0081 ,  A61M2202/064 ,  A61M2205/6045 ,  A61M2205/6081 ,  A61M2209/06

Abstract: The invention relates to an inhaler for inhaling powdery pharmaceuticals from capsules, comprising - a bottom part (6) - a plate (3) received in the bottom part (6), and a mounting (18) introduced in the bottom part (6), - a mouth piece (2) that can be latched to the bottom part (6) on the plate (3), - a cover (1) that covers the mouth piece (2) in a closed position and latches by means of a closure element (14), wherein the bottom part (6) and the cover (1) are rotatably connected to each other by an axis (4), and - an actuating member (7, 10), which can be set in motion from a position of rest and in the process cooperates with at least one needle (8, 11) that can pierce the mounting (18), said needle being located in a needle holder of the inner actuating member (10). An exchange tube (22) can be inserted in the mounting (18) as a discharge channel, the tube comprising a capsule chamber (21) with the capsule.

Abstract translation: 吸入器在下部从胶囊吸入粉状药物组合物，其包括-a底部部分（6）-a（6）记录盘（3），并在下部部分引入一个（6）支撑件（18）-A（6至下部 ）可锁定在所述板（3），所述嘴件（2），-a盖（1）覆盖所述吹口（2）在关闭位置和（由封闭元件14的方式）接合，其中所述下部分（6）和所述盖（1 ）可旋转的相互（由（4轴），4）相连接，并且-an致动构件（7,10），其是从静止位置位移到一个运动，从而具有至少一个（在保持器18）einstoßbaren针（8， 11）延伸的位于内致动构件的针保持器（10）协作。 在保持器（18）是一个替换管（22）被用作具有胶囊室（21）与胶囊的排出通道。

公开(公告)号：WO2011039368A3

公开(公告)日：2011-06-23

申请号：PCT/EP2010064693

申请日：2010-10-01

Applicant: BOEHRINGER INGELHEIM INT ,  BORGES ERIC ,  GSCHWIND ANDREAS ,  BOUCNEAU JOACHIM ,  DE TAVERNIER EVELYN ,  KOLKMAN JOOST ,  MERCHIERS PASCAL ,  VAN HOORICK DIANE

Inventor： BORGES ERIC ,  GSCHWIND ANDREAS ,  BOUCNEAU JOACHIM ,  DE TAVERNIER EVELYN ,  KOLKMAN JOOST ,  MERCHIERS PASCAL ,  VAN HOORICK DIANE

IPC: C07K16/28 ,  A61P35/00

CPC classification number: C07K16/28 ,  A61K2039/505 ,  C07K2317/22 ,  C07K2317/55 ,  C07K2317/565 ,  C07K2317/569 ,  C07K2317/76 ,  C07K2317/92

Abstract: DII4-binding molecules, preferably DII4-binding immunoglobulin single variable domains like VHHs and VHs, pharmaceutical compositions containing same and their use in the treatment of diseases that are associated with DII4-mediated effects on angiogenesis. Bispecific DII4-binding molecules that also bind to VEGF-A. Nucleic acids encoding DII4-binding molecules, host cells and methods for preparing same.

Abstract translation: DII4结合分子，优选DII4结合免疫球蛋白单可变结构域如VHH和VH，含有它们的药物组合物以及它们在治疗与DII4介导的血管发生作用有关的疾病中的用途。 也结合VEGF-A的双特异性DII4结合分子。 编码Dll4结合分子的核酸，宿主细胞及其制备方法。