公开(公告)号：US10407433B2

公开(公告)日：2019-09-10

申请号：US16058299

申请日：2018-08-08

申请人： The Trustees of Columbia University in the City of New York

发明人： Konstantin Petrukhin ,  Christopher Cioffi ,  Graham Johnson ,  Rando Allikmets ,  Emily Freeman ,  Ping Chen ,  Michael Conlon ,  Lei Zhu

IPC分类号： A61K31/437 ,  C07D401/14 ,  C07D211/06 ,  C07D295/00 ,  C07D487/04 ,  C07D471/04

摘要： The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof.

公开(公告)号：US10023573B2

公开(公告)日：2018-07-17

申请号：US15583238

申请日：2017-05-01

申请人： MEIJI SEIKA PHARMA CO., LTD.

发明人： Takao Abe ,  Takeshi Furuuchi ,  Yoshiaki Sakamaki ,  Seiichi Inamura ,  Akihiro Morinaka

IPC分类号： C07D211/06 ,  C07D295/00 ,  C07D471/08 ,  C07D211/60 ,  A61K45/06 ,  A61K31/43 ,  A61K31/545 ,  A61K31/546 ,  A61K31/439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/437 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/427 ,  C07F7/08

摘要： A process for preparing a diazabicyclooctane compound represented by the following formula (I): wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.

公开(公告)号：US09708340B2

公开(公告)日：2017-07-18

申请号：US14856325

申请日：2015-09-16

申请人： Hoffmann-La Roche Inc.

发明人： Bernd Buettelmann ,  Simona M. Ceccarelli ,  Aurelia Conte ,  Holger Kuehne ,  Bernd Kuhn ,  Werner Neidhart ,  Ulrike Obst Sander ,  Hans Richter

IPC分类号： C07D211/00 ,  C07D295/00 ,  A61K31/445 ,  C07D495/04 ,  C07D213/79 ,  C07D401/12 ,  C07D409/12 ,  C07D205/04 ,  C07D207/16 ,  C07D277/06 ,  C07D209/52 ,  C07D211/60

CPC分类号： C07D495/04 ,  C07D205/04 ,  C07D207/16 ,  C07D209/52 ,  C07D211/60 ,  C07D213/79 ,  C07D277/06 ,  C07D401/12 ,  C07D409/12

摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, W, A and B are as described herein, compositions including the compounds and methods of using the compounds.

公开(公告)号：US09708320B2

公开(公告)日：2017-07-18

申请号：US14872988

申请日：2015-10-01

申请人： MEIJI SEIKA PHARMA CO., LTD.

发明人： Takao Abe ,  Takeshi Furuuchi ,  Yoshiaki Sakamaki ,  Seiichi Inamura ,  Akihiro Morinaka

IPC分类号： C07D211/06 ,  C07D295/00 ,  C07D471/08 ,  C07D211/60 ,  A61K45/06 ,  A61K31/43 ,  A61K31/545 ,  A61K31/546 ,  A61K31/439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/437 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/427 ,  C07F7/08

CPC分类号： C07D471/08 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/427 ,  A61K31/43 ,  A61K31/437 ,  A61K31/439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/545 ,  A61K31/546 ,  A61K45/06 ,  C07D211/60 ,  C07F7/0812 ,  Y02P20/55 ,  A61K2300/00

摘要： A diazabicyclooctane compound, which is a beta-lactame inhibitor, represented by the following formula (I): wherein A represents Ra(Rb)N— or RcO—; B represents NH or NC1-6 alkyl; C represents benzyl, H or SO3M, wherein M represents H, an inorganic or an organic cation; Ra and Rb represent H, C1-6 alkyl or acyl; Rc represents C1-6 alkyl or a heterocyclyl; A is unsubstituted or substituted with 0 to 4 substituents Fn1, wherein Fn1 represents C1-6 alkyl, O═, or Rg-(CH2)0-3—, wherein Rg represents a heterocyclyl, phenyl, heteroaryl, acyl, RdO2S—, Re(Rf)N—, Re(Rf)NCO—, ReO—, ReOCO— or a protective group, wherein Rd represents C1-6 alkyl or MO—; Re and Rf represent H or C1-6 alkyl, and a heterocycle having at least one nitrogen atom may be formed between Ra and Rb, between Rc and B, or between Re and Rf.

公开(公告)号：US09708304B2

公开(公告)日：2017-07-18

申请号：US14765176

申请日：2014-01-31

申请人： BIOFRONTERA BIOSCIENCE GMBH

发明人： Beate Schmitz ,  Hermann Luebbert

IPC分类号： C07D211/00 ,  C07D295/00 ,  C07D409/00 ,  C07D411/00 ,  C07D417/00 ,  C07D419/00 ,  A61K31/445 ,  C07D409/04

CPC分类号： C07D409/04

摘要： The present invention relates to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine salts and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine salts; especially to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride as well as to the use of these salts for preventing or treating migraine or pulmonary hypertension.

公开(公告)号：US09695122B2

公开(公告)日：2017-07-04

申请号：US15040654

申请日：2016-02-10

申请人： Forest Laboratories Holdings Ltd.

发明人： Melanie Simone Ronsheim ,  Saibaba Racha ,  Graham Richard Lawton ,  Shao Hong Zhou ,  Yuriy B. Kalyan ,  Michael Golden ,  David Milne ,  Alexander Telford ,  Janette Cherryman ,  Alistair Boyd ,  Andrew Phillips ,  Mahendra G. Dedhiya

IPC分类号： C07D211/06 ,  C07D295/00 ,  C07D211/60 ,  C07D471/08 ,  C07D211/56 ,  A61K31/439 ,  A61K31/445

CPC分类号： C07D211/60 ,  A61K31/439 ,  A61K31/445 ,  C07D211/56 ,  C07D471/08 ,  Y02P20/55

摘要： The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).

公开(公告)号：USRE46424E1

公开(公告)日：2017-06-06

申请号：US14145892

申请日：2013-12-31

申请人： Wilex AG

发明人： Hugo Ziegler ,  Peter Wikstroem

IPC分类号： C07D295/00 ,  C07D213/00 ,  C07D295/205 ,  C07D211/60

CPC分类号： C07D295/205 ,  C07D211/60

摘要： The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate formate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.

公开(公告)号：US09656973B2

公开(公告)日：2017-05-23

申请号：US14862841

申请日：2015-09-23

申请人： Indiana University Research and Technology Corporation

发明人： James R. McCarthy

IPC分类号： C07D263/20 ,  C07D263/22 ,  C07D295/00 ,  C07D413/10

CPC分类号： C07D263/20

摘要： Processes and intermediates for preparing linezolid, and pharmaceutically acceptable salts thereof, are described herein.

公开(公告)号：US09546157B2

公开(公告)日：2017-01-17

申请号：US14640551

申请日：2015-03-06

申请人： Helsinn Healthcare SA

发明人： Claudio Giuliano ,  Silvina Garcia Rubio ,  Antoine Daina ,  Angelo Guainazzi ,  Claudio Pietra

IPC分类号： A61K31/4468 ,  C07D211/58 ,  C07D295/00 ,  C07D401/14 ,  C07D401/12 ,  C07D417/14 ,  C07D409/14 ,  C07D239/26 ,  C07D405/12 ,  C07D403/12 ,  C07D471/04 ,  C07D401/06 ,  C07D211/60 ,  C07D211/94 ,  C07D211/96 ,  C07D213/00

CPC分类号： C07F7/0812 ,  C07D211/58 ,  C07D211/60 ,  C07D211/94 ,  C07D211/96 ,  C07D213/00 ,  C07D239/26 ,  C07D241/12 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor. The compounds have the general Formula I: or pharmaceutically acceptable salts thereof.

摘要翻译： 公开了用于预防和/或治疗由生长素释放肽受体病理生理介导的疾病的化合物，组合物和方法。 化合物具有通式I或其药学上可接受的盐。

公开(公告)号：US09409154B2

公开(公告)日：2016-08-09

申请号：US14691663

申请日：2015-04-21

申请人： BASF SE

发明人： Thomas Heidemann ,  Petr Kubanek ,  Joana C. Tsou ,  Heiko Baas

IPC分类号： B01J23/835 ,  B01J23/14 ,  C07D295/00 ,  C07C213/02 ,  B01J37/03 ,  B01J37/06 ,  B01J37/08 ,  B01J37/12 ,  B01J37/16 ,  B01J35/10 ,  B01J21/04 ,  B01J35/00 ,  B01J37/02 ,  B01J37/18 ,  B01J23/889 ,  B01J23/78 ,  B01J23/83 ,  B01J23/847 ,  B01J23/888 ,  B01J33/00

CPC分类号： B01J23/835 ,  B01J21/04 ,  B01J23/14 ,  B01J23/78 ,  B01J23/83 ,  B01J23/847 ,  B01J23/888 ,  B01J23/8892 ,  B01J33/00 ,  B01J35/0006 ,  B01J35/1014 ,  B01J35/1019 ,  B01J37/0203 ,  B01J37/03 ,  B01J37/031 ,  B01J37/035 ,  B01J37/06 ,  B01J37/08 ,  B01J37/086 ,  B01J37/12 ,  B01J37/16 ,  B01J37/18 ,  B01J2523/00 ,  C07C213/02 ,  C07D295/00 ,  Y02P20/582 ,  C07C217/08 ,  B01J2523/17 ,  B01J2523/31 ,  B01J2523/43 ,  B01J2523/845 ,  B01J2523/847

摘要： The present invention relates to a process for producing a supported tin-comprising catalyst, wherein a solution (S) comprising tin nitrate and at least one complexing agent is applied to the support, where the solution (S) does not comprise any solid or has a solids content of not more than 0.5% by weight based on the total amount of dissolved components.