公开(公告)号：US07425630B2

公开(公告)日：2008-09-16

申请号：US11331372

申请日：2006-01-12

申请人： Tawfik Gharbaoui ,  Dipanjan Sengupta ,  Edward A. Lally ,  Naomi S. Kato ,  Marlon Carlos ,  Natalie Rodriguez

发明人： Tawfik Gharbaoui ,  Dipanjan Sengupta ,  Edward A. Lally ,  Naomi S. Kato ,  Marlon Carlos ,  Natalie Rodriguez

IPC分类号： C07D401/12 ,  C07D231/38

CPC分类号： C07D487/04

摘要： The present invention relates to processes for preparing pyrazolo[3,4-d]pyrimidine ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic disorders such as diabetes and obesity.

摘要翻译： 本发明涉及制备作为葡萄糖代谢调节剂的吡唑并[3,4-d]嘧啶醚化合物的方法，因此可用于治疗代谢性疾病如糖尿病和肥胖症。

公开(公告)号：US20060154940A1

公开(公告)日：2006-07-13

申请号：US11331372

申请日：2006-01-12

申请人： Tawfik Gharbaoui ,  Dipanjan Sengupta ,  Edward Lally ,  Naomi Kato ,  Marlon Carlos ,  Natalie Rodriguez

发明人： Tawfik Gharbaoui ,  Dipanjan Sengupta ,  Edward Lally ,  Naomi Kato ,  Marlon Carlos ,  Natalie Rodriguez

IPC分类号： A61K31/519 ,  C07D487/02

CPC分类号： C07D487/04

摘要： The present invention relates to processes for preparing pyrazolo[3,4-d]pyrimidine ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic disorders such as diabetes and obesity.

摘要翻译： 本发明涉及制备作为葡萄糖代谢调节剂的吡唑并[3,4-d]嘧啶醚化合物的方法，因此可用于治疗代谢性疾病如糖尿病和肥胖症。

公开(公告)号：US08481535B2

公开(公告)日：2013-07-09

申请号：US12301212

申请日：2007-05-17

申请人： Tawfik Gharbaoui ,  Dipanjan Sengupta ,  Ashwin M. Krishnan ,  Nainesh Shah ,  Ryan M. Hart ,  Mark Macias ,  Edward A. Lally ,  Jonathan Duffield

发明人： Tawfik Gharbaoui ,  Dipanjan Sengupta ,  Ashwin M. Krishnan ,  Nainesh Shah ,  Ryan M. Hart ,  Mark Macias ,  Edward A. Lally ,  Jonathan Duffield

IPC分类号： A61K31/5377 ,  A61K31/496 ,  C07D295/185 ,  C07D403/12

CPC分类号： C07D231/12

摘要： The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HT2A serotonin receptor modulators, compositions thereof and methods of using the same.

公开(公告)号：US20080194836A1

公开(公告)日：2008-08-14

申请号：US11883043

申请日：2006-01-25

申请人： Tawfik Gharbaoui ,  Claudia Averbuj ,  Marlony Carlos ,  Edward A. Lally ,  Dipanjan Sengupta ,  John Robert Fritch

发明人： Tawfik Gharbaoui ,  Claudia Averbuj ,  Marlony Carlos ,  Edward A. Lally ,  Dipanjan Sengupta ,  John Robert Fritch

IPC分类号： C07D231/10

CPC分类号： C07D231/16

摘要： The present invention is directed to processes for the preparation of substituted phenylpyrazole ureas of Formula (I) that are useful as 5-HT2A serotonin receptor modulators for the treatment of disease.

摘要翻译： 本发明涉及制备式（I）的取代苯基吡唑脲的方法，其可用作治疗疾病的5-HT 2A 2 5-羟色胺受体调节剂。

公开(公告)号：US08853419B2

公开(公告)日：2014-10-07

申请号：US13575458

申请日：2011-01-27

申请人： Antonio Garrido Montalban ,  Daniel J. Buzard ,  John A. DeMattei ,  Tawfik Gharbaoui ,  Stephen R. Johannsen ,  Ashwin M. Krishnan ,  Young Mi Khulman ,  You-An Ma ,  Michael John Martinelli ,  Suzanne Michiko Sato ,  Dipanjan Sengupta

发明人： Antonio Garrido Montalban ,  Daniel J. Buzard ,  John A. DeMattei ,  Tawfik Gharbaoui ,  Stephen R. Johannsen ,  Ashwin M. Krishnan ,  Young Mi Khulman ,  You-An Ma ,  Michael John Martinelli ,  Suzanne Michiko Sato ,  Dipanjan Sengupta

IPC分类号： C07D209/80 ,  A61K31/403 ,  C07D209/94

CPC分类号： C12P17/10 ,  C07B2200/13 ,  C07C17/278 ,  C07D209/80 ,  C07D209/88 ,  C07D209/94 ,  C07D295/155

摘要： The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).

摘要翻译： 本发明涉及可用于制备（R）-2-（7-（4-环戊基-3-（三氟甲基）苄氧基）-1,2,3,4-四氢环戊二烯并[b]吲哚-3 - 基）乙酸及其盐，可用于治疗S1P1受体相关疾病的S1P1受体调节剂，例如由淋巴细胞介导的疾病和病症，移植排斥反应，自身免疫性疾病和病症，炎性 疾病和病症（例如急性和慢性炎性病症），癌症和特征在于血管完整性的潜在缺陷或与血管发生相关的病症，例如可能是病理性的（例如，可能发生在炎症，肿瘤发展和动脉粥样硬化） 。

公开(公告)号：US20120295947A1

公开(公告)日：2012-11-22

申请号：US13575458

申请日：2011-01-27

申请人： Antonio Garrido Montalban ,  Daniel J. Buzard ,  John A. DeMattei ,  Tawfik Gharbaoui ,  Stephen R. Johannsen ,  Ashwin M. Krishnan ,  Young Mi Khulman ,  You-An Ma ,  Michael John Martinelli ,  Suzanne Michiko Sato ,  Dipanjan Sengupta

发明人： Antonio Garrido Montalban ,  Daniel J. Buzard ,  John A. DeMattei ,  Tawfik Gharbaoui ,  Stephen R. Johannsen ,  Ashwin M. Krishnan ,  Young Mi Khulman ,  You-An Ma ,  Michael John Martinelli ,  Suzanne Michiko Sato ,  Dipanjan Sengupta

IPC分类号： C12P17/10 ,  A61K31/403 ,  A61P25/00 ,  A61P37/06 ,  A61P9/12 ,  A61P17/10 ,  A61P29/00 ,  A61P17/06 ,  C07D209/70 ,  A61P3/10

CPC分类号： C12P17/10 ,  C07B2200/13 ,  C07C17/278 ,  C07D209/80 ,  C07D209/88 ,  C07D209/94 ,  C07D295/155

摘要： The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).

摘要翻译： 本发明涉及可用于制备（R）-2-（7-（4-环戊基-3-（三氟甲基）苄氧基）-1,2,3,4-四氢环戊二烯并[b]吲哚-3 - 基）乙酸及其盐，可用于治疗S1P1受体相关疾病的S1P1受体调节剂，例如由淋巴细胞介导的疾病和病症，移植排斥反应，自身免疫性疾病和病症，炎性 疾病和病症（例如急性和慢性炎性病症），癌症和特征在于血管完整性的潜在缺陷或与血管发生相关的病症，例如可能是病理性的（例如，可能发生在炎症，肿瘤发展和动脉粥样硬化） 。

公开(公告)号：US20100234380A1

公开(公告)日：2010-09-16

申请号：US12301212

申请日：2007-05-17

申请人： Tawfik Gharbaoui ,  Dipanjan Sengupta ,  Ashwin M. Krishnan ,  Nainesh Shah ,  Ryan M. Hart ,  Mark Macias

发明人： Tawfik Gharbaoui ,  Dipanjan Sengupta ,  Ashwin M. Krishnan ,  Nainesh Shah ,  Ryan M. Hart ,  Mark Macias

IPC分类号： A61K31/5377 ,  C07D413/12 ,  C07D403/12 ,  C07D231/12 ,  A61K31/496 ,  A61K31/415 ,  A61P7/00 ,  A61P25/00 ,  A61P25/18 ,  A61P9/00

CPC分类号： C07D231/12

摘要： The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HT2A serotonin receptor modulators, compositions thereof and methods of using the same.

摘要翻译： 本发明涉及制备式（I）的苯基 - 吡唑的方法及其盐及其药物组合物，其可用作5-HT2A 5-羟色胺受体活性的调节剂。 本发明还涉及用于该方法及其制备的中间体。 本发明还涉及5-HT2A 5-羟色胺受体调节剂的结晶形式，其组合物及其使用方法。

公开(公告)号：US08655112B2

公开(公告)日：2014-02-18

申请号：US13492367

申请日：2012-06-08

申请人： Swarnima Bansal ,  Dipanjan Sengupta

发明人： Swarnima Bansal ,  Dipanjan Sengupta

IPC分类号： G06K9/03

CPC分类号： G06T11/60

摘要： A method and apparatus for an improved workflow for digital image editing is disclosed. The method comprises accessing a file containing a plurality of effects to apply to an image; merging a plurality of visible layers of the image to create a merged layer; applying the plurality of effects to the merged layer; installing a layer mask on the merged layer; and applying a plurality of user strokes made during an image editing process to the installed layer mask.

摘要翻译： 公开了一种用于数字图像编辑的改进工作流程的方法和装置。 该方法包括访问包含多个效果的文件以应用于图像; 合并图像的多个可见层以创建合并图层; 将多个效果应用于合并层; 在合并图层上安装图层蒙版; 以及将在图像编辑处理期间产生的多个用户笔画应用于所安装的图层蒙版。

公开(公告)号：US08946207B2

公开(公告)日：2015-02-03

申请号：US13619773

申请日：2012-09-14

申请人： Beverly L. Wolgast ,  Charles A. Gilson, III ,  Shelley Aytes ,  Scott A. Estrada ,  Dipanjan Sengupta ,  Brian Smith ,  Ulrich Weigl ,  Heidedore Jlsabeth Rey-Papina

发明人： Beverly L. Wolgast ,  Charles A. Gilson, III ,  Shelley Aytes ,  Scott A. Estrada ,  Dipanjan Sengupta ,  Brian Smith ,  Max Rey ,  Ulrich Weigl

IPC分类号： A61K31/55 ,  C07D223/16 ,  C07C209/50 ,  C07C211/29 ,  C07C213/02 ,  C07C215/08 ,  C07C231/02 ,  C07C17/16 ,  C07C25/06 ,  C07C209/74 ,  C07C211/27

CPC分类号： C07D223/16 ,  C07C17/16 ,  C07C25/06 ,  C07C59/255 ,  C07C209/50 ,  C07C209/74 ,  C07C211/27 ,  C07C211/29 ,  C07C213/02 ,  C07C215/08 ,  C07C231/02 ,  C07C233/13

摘要： The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.

公开(公告)号：US20080275232A1

公开(公告)日：2008-11-06

申请号：US12147208

申请日：2008-06-26

申请人： Byron C. Robinson ,  Dipanjan Sengupta ,  Avinash Phadke

发明人： Byron C. Robinson ,  Dipanjan Sengupta ,  Avinash Phadke

IPC分类号： C07D487/22

CPC分类号： C07D487/22 ,  A61K41/0057 ,  A61K41/0071

摘要： The present invention provides a process of preparation of naphthochlorins and other chlorins with annelated ring systems useful for photodynamic therapy and the compounds themselves. The method for producing naphthochlorin compounds include contacting compounds such as meso-(2′-hydroxymethyl)phenyl porphyrin or meso-(2′-N,N,N-trialkylaminomethyl)phenyl porphyrin precursors with at least one acid catalyst at sufficient temperature for a sufficient time to yield the desired conversion. In a similar manner chlorins possessing annelated ring systems may be made from compounds such as meso-(2′-hydroxymethyl)aryl porphyrins or meso-(2′-N,N,N-trialkylaminomethyl)phenyl porphyrin. The procedures described herein provide new routes for synthesizing naphthochlorins and chlorins with annelated ring systems.

摘要翻译： 本发明提供了用于光动力学治疗和化合物本身的具有环状环系的萘并氯和其他二氢卟酚的制备方法。 制造萘并二氢黄汞化合物的方法包括将内消旋 - （2'-羟甲基）苯基卟啉或中 - （2-N，N，N-三烷基氨基甲基）苯基卟啉前体的化合物与足够温度的至少一种酸催化剂接触， 足够的时间产生所需的转化。 类似地，具有环状环系的二氢卟酚可以由诸如中 - （2'-羟甲基）芳基卟啉或中 - （2-N，N，N-三烷基氨基甲基）苯基卟啉的化合物制备。 本文所述的方法提供用于合成具有环状环系的萘并氯和二氢卟酚的新途径。