公开(公告)号：US20170334918A1

公开(公告)日：2017-11-23

申请号：US15598540

申请日：2017-05-18

Applicant: ASAF ALIMARDANOV ,  GREGORY D. CUNY ,  GURMIT SINGH GREWAL ,  ARTHUR LEE ,  JOHN C. MCKEW ,  AGUSTIN H. MOHEDAS ,  MIN SHEN ,  XIN XU ,  PAUL B. YU

Inventor： ASAF ALIMARDANOV ,  GREGORY D. CUNY ,  GURMIT SINGH GREWAL ,  ARTHUR LEE ,  JOHN C. MCKEW ,  AGUSTIN H. MOHEDAS ,  MIN SHEN ,  XIN XU ,  PAUL B. YU

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.

公开(公告)号：US20090023930A1

公开(公告)日：2009-01-22

申请号：US12172472

申请日：2008-07-14

Applicant: Asaf Alimardanov ,  Antonia Nikitenko ,  Gregg Feigelson ,  John Potoski

Inventor： Asaf Alimardanov ,  Antonia Nikitenko ,  Gregg Feigelson ,  John Potoski

IPC: C07D263/26 ,  C07D333/34 ,  C07C51/36

CPC classification number: C07C303/40 ,  C07C51/083 ,  C07C51/36 ,  C07C57/58 ,  C07C57/60 ,  C07C213/00 ,  C07D263/22 ,  C07D333/34 ,  C07D409/12 ,  C07C311/17 ,  C07C215/28

Abstract: Methods for preparing compound of formula (I) are described, wherein R1-R3 are defined herein, as are methods for preparing the intermediates formed therein. Also described are methods for enantioselectively preparing a chiral compound of the following structure, wherein R2 and R3 are defined herein.

Abstract translation: 描述了制备式（I）化合物的方法，其中R 1 -R 3在本文中定义，以及制备其中形成的中间体的方法。 还描述了对映选择性制备下列结构的手性化合物的方法，其中R 2和R 3在本文中定义。

公开(公告)号：US07479561B2

公开(公告)日：2009-01-20

申请号：US11201705

申请日：2005-08-11

Applicant: Diane Harris Boschelli ,  Jay Thomas Afragola ,  Asaf Alimardanov ,  Biqi Wu

Inventor： Diane Harris Boschelli ,  Jay Thomas Afragola ,  Asaf Alimardanov ,  Biqi Wu

IPC: C07D215/38

CPC classification number: C07D405/04 ,  C07D405/14

Abstract: This invention relates to compounds having the structure of Formula I wherein R1, R2, R3, and R4 are described herein.

Abstract translation: 本发明涉及具有式I结构的化合物，其中R1，R2，R3和R4如本文所述。

公开(公告)号：US20060035930A1

公开(公告)日：2006-02-16

申请号：US11201705

申请日：2005-08-11

Applicant: Diane Boschelli ,  Jay Afragola ,  Asaf Alimardanov ,  Biqi Wu

Inventor： Diane Boschelli ,  Jay Afragola ,  Asaf Alimardanov ,  Biqi Wu

IPC: A61K31/4709 ,  C07D405/14 ,  C07D405/02

CPC classification number: C07D405/04 ,  C07D405/14

Abstract: This invention relates to compounds having the structure of Formula I wherein R1, R2, R3, and R4 are described herein.

Abstract translation: 本发明涉及具有式I结构的化合物，其中R 1，R 2，R 3和R 4， SUP>。

公开(公告)号：US20090023903A1

公开(公告)日：2009-01-22

申请号：US12172486

申请日：2008-07-14

Applicant: Terrence Joseph Connolly ,  Anita Wai-Yin Chan ,  Zhixian Ding ,  Mousumi Ghosh ,  Xinxu Shi ,  Jianxin Ren ,  Eric Hansen ,  Roger Farr ,  Michael MacEwan ,  Asaf Alimardanov ,  Antonia Nikitenko ,  John Potoski

Inventor： Terrence Joseph Connolly ,  Anita Wai-Yin Chan ,  Zhixian Ding ,  Mousumi Ghosh ,  Xinxu Shi ,  Jianxin Ren ,  Eric Hansen ,  Roger Farr ,  Michael MacEwan ,  Asaf Alimardanov ,  Antonia Nikitenko ,  John Potoski

IPC: C07C311/17 ,  C07C311/00 ,  C07D333/34 ,  C07D263/20 ,  C07C33/46 ,  C07D265/30 ,  C09B29/36

CPC classification number: C07D295/108 ,  C07D263/26 ,  C07D333/34

Abstract: A novel trifluoroacetylating agent, i.e., N-trifluoroacetylmorpholine, is described. This reagent is useful in the preparation of phenyl and heterocyclic sulfonamide compounds. Methods are therefore described for preparing sulfonamide compounds of the following structure, wherein R1 and R2 are defined herein, using N-trifluoroacetylmorpholine. The sulfonamide compounds that may be prepared as described herein include 5-chloro-thiophene-2-sulfonic acid [(1S,2R)-2-(3,5-difluoro-phenyl)-3,3,3-trifluoro-1-hydroxymethyl-propyl]-amide using N-trifluoroacetylmorpholine.

Abstract translation: 描述了一种新型的三氟乙酰化剂，即N-三氟乙酰基吗啉。 该试剂可用于制备苯基和杂环磺酰胺化合物。 因此，描述了制备以下结构的磺酰胺化合物的方法，其中R1和R2在本文中定义，使用N-三氟乙酰基吗啉。 可以如本文所述制备的磺酰胺化合物包括5-氯 - 噻吩-2-磺酸[（1S，2R）-2-（3,5-二氟 - 苯基）-3,3,3-三氟-1- 羟甲基 - 丙基] - 酰胺，使用N-三氟乙酰基吗啉。

公开(公告)号：US20080146645A1

公开(公告)日：2008-06-19

申请号：US11843364

申请日：2007-08-22

Applicant: Anita Wai-Yin Chan ,  Zhixian Ding ,  Mousumi Ghosh ,  Mahmut Levent ,  Panolil Raveendranath ,  Jianxin Ren ,  Maotang Zhou ,  Asaf Alimardanov ,  Alexander V. Gontcharov ,  Antonia A. Nikitenko ,  John R. Potoski ,  Girija Raveendranath ,  Vijay Raveendranath ,  Sanjay Raveendranath

Inventor： Anita Wai-Yin Chan ,  Zhixian Ding ,  Mousumi Ghosh ,  Mahmut Levent ,  Panolil Raveendranath ,  Jianxin Ren ,  Maotang Zhou ,  Asaf Alimardanov ,  Alexander V. Gontcharov ,  Antonia A. Nikitenko ,  John R. Potoski ,  Girija Raveendranath ,  Vijay Raveendranath ,  Sanjay Raveendranath

IPC: C07D209/34 ,  A61K31/4015

CPC classification number: C07D209/34

Abstract: Processes are disclosed for preparing indolinone phenylaminopropanol derivatives, particularly chiral indolinone phenylaminopropanol derivatives of the general formula: The processes disclosed may be used to prepare, inter alia, 7-fluoro-1-[(1S, 2R)-1-(3-fluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one and 7-fluoro-1-[(1S, 2R)-1-(3,5-difluorophenyl)-2-hydroxy-3-(methylamino)propyl]-3,3-dimethyl-1,3-dihydro-2H-indol-2-one. Intermediates of the processes are also disclosed.

Abstract translation: 公开了制备吲哚啉酮苯基氨基丙醇衍生物的方法，特别是具有以下通式的手性吲哚啉酮苯基氨基丙醇衍生物：所公开的方法可用于特别地制备7-氟-1 - [（1S，2R）-1-（3- 氟甲基）-2-羟基-3-（甲基氨基）丙基] -3,3-二甲基-1,3-二氢-2H-吲哚-2-酮和7-氟-1 - [（1S，2R）-1 - （3,5-二氟苯基）-2-羟基-3-（甲基氨基）丙基] -3,3-二甲基-1,3-二氢-2H-吲哚-2-酮。 还公开了该方法的中间体。