公开(公告)号：US08637537B2

公开(公告)日：2014-01-28

申请号：US13593776

申请日：2012-08-24

Applicant: Ignacio Aliagas-Martin ,  James Crawford ,  Wendy Lee ,  Simon Mathieu ,  Joachim Rudolph

Inventor： Ignacio Aliagas-Martin ,  James Crawford ,  Wendy Lee ,  Simon Mathieu ,  Joachim Rudolph

IPC: A01N43/54 ,  A61K31/505

CPC classification number: C07D403/14 ,  A61K31/506 ,  A61K45/06

Abstract: Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.

Abstract translation: 具有式I的化合物，其中A，Z，R 1a，R 1b，R 2，R 3，R 4，R 5，R 6，R 7，R 9，R 10，R a，R b和n如本文所定义是PAK1的抑制剂。 还公开了用于治疗癌症和过度增殖性疾病的组合物和方法。

公开(公告)号：US20110110889A1

公开(公告)日：2011-05-12

申请号：US12920045

申请日：2009-02-27

Applicant: Kateri A. Ahrendt et al. ,  Alexander J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

Inventor： Kateri A. Ahrendt et al. ,  Alexander J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

IPC: A61K38/21 ,  C07D471/04 ,  C07D401/10 ,  C07D401/02 ,  A61K31/437 ,  A61K31/5377 ,  A61K31/497 ,  A61K39/395 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07C311/08

Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式（I）的化合物可用于抑制Raf激酶。 公开了使用式（I）化合物及其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20090082328A1

公开(公告)日：2009-03-26

申请号：US12151855

申请日：2008-05-09

Applicant: Yingfu Li ,  Joachim Rudolph ,  Jacques P. Dumas ,  Daniel Auclair ,  Mario Lobell ,  Marion Hitchcock ,  Ingo Hartung ,  Marcus Koppitz ,  Dominic Brittain ,  Florian Puehler ,  Kirstin Petersen ,  Judith Guenther

Inventor： Yingfu Li ,  Joachim Rudolph ,  Jacques P. Dumas ,  Daniel Auclair ,  Mario Lobell ,  Marion Hitchcock ,  Ingo Hartung ,  Marcus Koppitz ,  Dominic Brittain ,  Florian Puehler ,  Kirstin Petersen ,  Judith Guenther

IPC: A61K31/445 ,  C07C205/45 ,  C07D211/32 ,  C07C255/58 ,  C07D317/30 ,  C07C237/28 ,  A61K31/397 ,  A61K31/40 ,  A61K31/27 ,  A61P35/00 ,  A61K31/44 ,  A61K31/166 ,  C07D295/14 ,  C07D279/12 ,  C07D265/30 ,  A61K31/54 ,  A61K31/5375

CPC classification number: C07D233/60 ,  C07C217/92 ,  C07C237/30 ,  C07C237/44 ,  C07C243/38 ,  C07C255/58 ,  C07C255/59 ,  C07C271/16 ,  C07C271/28 ,  C07C271/44 ,  C07C275/28 ,  C07C275/36 ,  C07C307/02 ,  C07C307/10 ,  C07C309/66 ,  C07C311/08 ,  C07C311/09 ,  C07C311/17 ,  C07C311/48 ,  C07C2601/08 ,  C07C2601/10 ,  C07D205/04 ,  C07D207/08 ,  C07D207/27 ,  C07D207/48 ,  C07D209/08 ,  C07D211/22 ,  C07D211/46 ,  C07D211/96 ,  C07D213/30 ,  C07D213/34 ,  C07D213/68 ,  C07D231/18 ,  C07D233/84 ,  C07D265/30 ,  C07D277/22 ,  C07D295/088 ,  C07D295/185 ,  C07D295/26 ,  C07D317/22 ,  C07D317/64 ,  C07D327/04 ,  C07D403/12

Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

Abstract translation: 本发明涉及新的取代的苯基氨基苯化合物，含有这些化合物的药物组合物，以及这些化合物或组合物用于治疗高增殖和/或血管生成障碍，作为唯一试剂或与其它活性成分组合的用途。

公开(公告)号：US20060258571A1

公开(公告)日：2006-11-16

申请号：US10522667

申请日：2003-07-18

Applicant: Thomas Lampe ,  Isabelle Adelt ,  Dieter Beyer ,  Nina Brunner ,  Rainer Endermann ,  Kerstin Ehlert ,  Hein-Peter Kroll ,  Franz Nussbaum ,  Siegfried Raddatz ,  Joachim Rudolph ,  Guido Schiffer ,  Andreas Schumacher ,  Yolanda Cancho-Grande ,  Martin Michels ,  Stefan Weigand

Inventor： Thomas Lampe ,  Isabelle Adelt ,  Dieter Beyer ,  Nina Brunner ,  Rainer Endermann ,  Kerstin Ehlert ,  Hein-Peter Kroll ,  Franz Nussbaum ,  Siegfried Raddatz ,  Joachim Rudolph ,  Guido Schiffer ,  Andreas Schumacher ,  Yolanda Cancho-Grande ,  Martin Michels ,  Stefan Weigand

IPC: A61K38/12 ,  A61K31/395 ,  C07K5/12

CPC classification number: C07K5/0812 ,  A61K38/00

Abstract: The invention relates to antibacterial ester macrocycles of formula (I), methods for the production thereof, and the use thereof for producing medicaments used for the treatment and/or prophylaxis of diseases, particularly bacterial infections.

Abstract translation: 本发明涉及式（I）的抗菌酯大环化合物，其制备方法及其用于制备用于治疗和/或预防疾病，特别是细菌感染的药物的用途。

公开(公告)号：US20060084680A1

公开(公告)日：2006-04-20

申请号：US10537630

申请日：2003-12-19

Applicant: Louis-David Cantin ,  Soongyu Choi ,  Roger Clark ,  Martin Hentemann ,  Xin Ma ,  Joachim Rudolph ,  Sidney Liang ,  Christiana Akuche ,  Rico Lavoie ,  Libing Chen ,  Dyuti Majumdar ,  Philip Wickens

Inventor： Louis-David Cantin ,  Soongyu Choi ,  Roger Clark ,  Martin Hentemann ,  Xin Ma ,  Joachim Rudolph ,  Sidney Liang ,  Christiana Akuche ,  Rico Lavoie ,  Libing Chen ,  Dyuti Majumdar ,  Philip Wickens

IPC: A61K31/445 ,  A61K31/195 ,  A61K31/192

CPC classification number: C07D213/30 ,  C07C59/72 ,  C07C59/90 ,  C07C69/734 ,  C07C211/48 ,  C07C217/24 ,  C07C255/54 ,  C07C327/48 ,  C07C333/04 ,  C07C2602/08 ,  C07D209/08 ,  C07D213/63 ,  C07D213/83 ,  C07D213/84 ,  C07D215/20 ,  C07D231/12 ,  C07D239/26 ,  C07D239/42 ,  C07D239/46 ,  C07D239/47 ,  C07D239/52 ,  C07D249/06 ,  C07D249/08 ,  C07D261/20 ,  C07D263/32 ,  C07D263/56 ,  C07D277/24 ,  C07D277/34 ,  C07D277/56 ,  C07D277/64 ,  C07D277/66 ,  C07D285/08 ,  C07D307/42 ,  C07D307/79 ,  C07D333/16 ,  C07D405/04 ,  C07D417/04 ,  C07D513/04

Abstract: This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.

公开(公告)号：US5939568A

公开(公告)日：1999-08-17

申请号：US842732

申请日：1997-04-16

Applicant: K. Barry Sharpless ,  Joachim Rudolph

Inventor： K. Barry Sharpless ,  Joachim Rudolph

IPC: C07D301/12 ,  C07D303/00

CPC classification number: C07D301/12

Abstract: Rhenium-catalyzed epoxidation of olefinic substrates is accelerated by the use of acclerants having a nitrogenous aromatic heterocyclic structure. Use of the accelerants also enables the use of aqueous hydrogen peroxide as an oxidant. To achieve optimum acceleration, the accelerant should have a concentration within a range from 2.0 mole percent to 100 mole percent of the acclerant with respect to 1 mole of the olefinic substrate. Use of the accelerant also results in an increased yield with respect to the conversion of the olefinic substrate to epoxide product.

Abstract translation: 通过使用具有含氮芳族杂环结构的增加剂来加速烯属底物的铼催化环氧化。 使用促进剂也可以使用过氧化氢水溶液作为氧化剂。 为了达到最佳加速，促进剂的浓度应在1摩尔烯属底物的2.0摩尔％至100摩尔百分数之间。 促进剂的使用也导致相对于烯属底物转化为环氧化物产物的增加的产率。

公开(公告)号：US4850835A

公开(公告)日：1989-07-25

申请号：US89229

申请日：1987-08-25

Applicant: Joachim Rudolph

Inventor： Joachim Rudolph

IPC: B29B9/06 ,  B29B13/04

CPC classification number: B29B9/06 ,  B29B13/045

Abstract: A cooling device for plastic granulate which is formed by cutting plastic strands emerging from a nozzle plate of an extruder and is fed to a stream of cooling water which adjoins the nozzle plate in the region of a cutting device. A pipe conducts the stream of cooling water containing the granulate to a granulate-water separator. In order to obtain a well-defined, infinitely adjustable dwell time of the granulate in the stream of cooling water, the pipe is essentially developed as a vertically arranged riser having a larger cross section passage area than that of the pipe itself. The upper outlet end of the riser is connected to the suction side of a feed pump, which serves as a section pump, and to a suction pipe which has an end connected to ambient atmosphere. A regulating valve is connected in the suction pipe. The delivery side of the feed pump communicates with the granulate-water separator.

Abstract translation: 一种用于塑料颗粒的冷却装置，其通过切割从挤出机的喷嘴板出来的塑料线而形成，并且在切割装置的区域中被供给到与喷嘴板相邻的冷却水流。 管道将含有颗粒的冷却水流导向颗粒 - 水分离器。 为了在冷却水流中获得明确定义的无限可调的颗粒状停留时间，管道基本上显影为具有比管道本身更大的横截面通道面积的垂直布置的提升管。 提升管的上出口端连接到作为分段泵的进料泵的吸入侧和连接到环境大气的端部的吸入管。 调节阀连接在吸入管中。 进料泵的输送侧与颗粒 - 水分离器连通。

公开(公告)号：US4684488A

公开(公告)日：1987-08-04

申请号：US825232

申请日：1986-02-03

Applicant: Joachim Rudolph

Inventor： Joachim Rudolph

IPC: B29C47/10 ,  B01F3/18 ,  B01F15/04 ,  B01F15/06 ,  B29B7/72 ,  B29B7/88 ,  B29C31/10 ,  B29C47/40 ,  B29C47/92 ,  G05D11/02

CPC classification number: B01F15/0408 ,  B01F15/00214 ,  B01F15/0483 ,  B29C47/40 ,  B29C47/6037 ,  B29C47/92 ,  B01F3/18 ,  B29C2947/92257 ,  B29C2947/924 ,  B29C2947/9259 ,  B29C2947/92752 ,  B29C2947/92828 ,  B29C2947/92885 ,  B29C2947/92952

Abstract: A method and apparatus for regulating the drive of dosaging devices for the controlled feeding of plastic particles, color concentrates and additives into a supply hopper of a screw extruder for producing a mixed plastic product of determined coloration, comprising periodically measuring the coloration of the mixed product at an outlet of the extruder by a spectrometer connected to a measurement probe, comparing the measured coloration of the mixed product with the coloration of the desired product, and adjusting the supply of the plastic product, concentrates and additives, as necessary, so that the measured coloration of the product at the outlet of the extruder is the same as the coloration of the desired product.

Abstract translation: 一种用于调节用于将塑料颗粒，着色浓缩物和添加剂受控地输送到螺杆挤出机的供料斗中的剂量装置的驱动的方法和装置，用于生产确定着色的混合塑料产品，包括周期性地测量混合产品的着色 通过与测量探头连接的光谱仪在挤出机的出口处，将测量的混合产物的着色与所需产物的着色进行比较，并根据需要调整塑料产品，浓缩物和添加剂的供应，使得 在挤出机出口处测量的产品着色与所需产品的着色相同。

公开(公告)号：US07964622B2

公开(公告)日：2011-06-21

申请号：US12508314

申请日：2009-07-23

Applicant: Xin Ma ,  Louis-David Cantin ,  Soongyu Choi ,  Roger Clark ,  Martin Hentemann ,  Joachim Rudolph ,  Rico Lavoie ,  Zhonghua Zhang

Inventor： Xin Ma ,  Louis-David Cantin ,  Soongyu Choi ,  Roger Clark ,  Martin Hentemann ,  Joachim Rudolph ,  Rico Lavoie ,  Zhonghua Zhang

IPC: A61K31/425 ,  A61K31/42 ,  C07D417/00 ,  C07D277/20 ,  C07D498/00 ,  C07D263/30

CPC classification number: C07D403/12 ,  C07D209/08 ,  C07D401/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

Abstract: This invention is directed to indole acetic acid derivatives and their use in pharmaceutical compositions for the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic disease. The invention is also directed to intermediates useful in preparation of indole acetic derivatives and to methods of preparation.

Abstract translation: 本发明涉及吲哚乙酸衍生物及其在药物组合物中用于治疗疾病如糖尿病，肥胖症，高脂血症和动脉粥样硬化疾病的用途。 本发明还涉及可用于制备吲哚乙酸衍生物的中间体和制备方法。

公开(公告)号：US20110092479A1

公开(公告)日：2011-04-21

申请号：US12920050

申请日：2009-02-27

Applicant: Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jason De Meese ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  Paul Lunghofer ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Jeongbeob Seo ,  Hongqi Tian ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

Inventor： Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jason De Meese ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  Paul Lunghofer ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Jeongbeob Seo ,  Hongqi Tian ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

IPC: A61K31/437 ,  C07D471/04 ,  A61K31/5377 ,  A61K31/496 ,  A61P35/00 ,  A61P35/02 ,  A61P13/12

CPC classification number: C07D471/04 ,  C07C311/08

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式I化合物可用于抑制Raf激酶。 公开了使用式I化合物和立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。