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公开(公告)号：US20150038731A1
公开(公告)日：2015-02-05
申请号：US14005393
申请日：2012-03-15
IPC分类号： C07C51/09 , C07F7/18 , C07C57/58 , C07C43/176 , C07C69/65
CPC分类号： C07C51/09 , C07B2200/07 , C07C43/176 , C07C51/02 , C07C51/412 , C07C51/43 , C07C57/58 , C07C57/62 , C07C69/65 , C07F7/1804
摘要： The present invention relates to a process of making a compound of formula (XII) or (XIIA): wherein R1, R2, R4 and X are as defined herein.
摘要翻译： 本发明涉及制备式（XII）或（XIIA）化合物的方法：其中R1，R2，R4和X如本文所定义。
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![Synthesis of dihydrothieno[3,2-d]pyrimidine diols](/abs-image/US/2013/06/25/US08471010B2/abs.jpg.150x150.jpg)
公开(公告)号：US08471010B2
公开(公告)日：2013-06-25
申请号：US12989575
申请日：2009-05-07
申请人： Rogelio P. Frutos , Thomas G. Tampone , Jason Alan Mulder , Dhileepkumar Krishnamurthy , Chris H. Senanayake
发明人： Rogelio P. Frutos , Thomas G. Tampone , Jason Alan Mulder , Dhileepkumar Krishnamurthy , Chris H. Senanayake
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , C07D239/70
摘要： The present invention relates to an improved process for the preparation of dihydrothieno[3,2-d]pyrimidine diols, and similar pyrimidine diols, that is efficient, high-yielding, and does not require expensive and potentially unstable intermediates. The diols are used as intermediates in the synthesis of pyrimidine compounds which inhibit PDE4, and are thus useful in the treatment of respiratory or gastrointestinal diseases and complaints, peripheral or central nervous system diseases and disorders, inflammatory conditions, and cancers.
摘要翻译： 本发明涉及制备二氢噻吩并[3,2-d]嘧啶二醇和类似的嘧啶二醇的改进方法，其是有效的，高产的，并且不需要昂贵和潜在的不稳定的中间体。 二醇用作合成抑制PDE4的嘧啶化合物的中间体，因此可用于治疗呼吸道或胃肠道疾病和投诉，外周或中枢神经系统疾病和病症，炎症状况和癌症。
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![SYNTHESIS IF DIHYDROTHIENO[3,2-D]PYRIMIDINE DIOLS](/abs-image/US/2011/06/02/US20110130563A1/abs.jpg.150x150.jpg)
公开(公告)号：US20110130563A1
公开(公告)日：2011-06-02
申请号：US12989575
申请日：2009-05-07
申请人： Rogelio Perez Frutos , Thomas G. Tampone , Jason Alan Mulder , Dhileepkumar Krishnamurthy , Chris Hugh Senanayake
发明人： Rogelio Perez Frutos , Thomas G. Tampone , Jason Alan Mulder , Dhileepkumar Krishnamurthy , Chris Hugh Senanayake
IPC分类号： C07D239/00
CPC分类号： C07D495/04 , C07D239/70
摘要： The present invention relates to an improved process for the preparation of dihydrothieno[3,2-d]pyrimidine diols, and similar pyrimidine diols, that is efficient, high-yielding, and does not require expensive and potentially unstable intermediates. The diols are used as intermediates in the synthesis of pyrimidine compounds which inhibit PDE4, and are thus useful in the treatment of respiratory or gastrointestinal diseases and complaints, peripheral or central nervous system diseases and disorders, inflammatory conditions, and cancers.
摘要翻译： 本发明涉及制备二氢噻吩并[3,2-d]嘧啶二醇和类似的嘧啶二醇的改进方法，其是有效的，高产的，并且不需要昂贵和潜在的不稳定的中间体。 二醇用作合成抑制PDE4的嘧啶化合物的中间体，因此可用于治疗呼吸道或胃肠道疾病和投诉，外周或中枢神经系统疾病和病症，炎症状况和癌症。
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![Preparation of dihydrothieno [3,2-D] pyrimidines and intermediates used therein](/abs-image/US/2014/02/18/US08653282B2/abs.jpg.150x150.jpg)
4.发明授权Preparation of dihydrothieno [3,2-D] pyrimidines and intermediates used therein 有权制备二氢噻吩并[3,2-D]嘧啶及其中使用的中间体公开(公告)号：US08653282B2
公开(公告)日：2014-02-18
申请号：US12738152
申请日：2008-10-15
申请人： Rogelio Frutos , Dhileepkumar Krishnamurthy , Jason Alan Mulder , Sonia Rodriguez , Chris Hugh Senanayake , Thomas G. Tampone
发明人： Rogelio Frutos , Dhileepkumar Krishnamurthy , Jason Alan Mulder , Sonia Rodriguez , Chris Hugh Senanayake , Thomas G. Tampone
IPC分类号： C07D333/32 , C07D495/04
CPC分类号： C07D495/04
摘要： 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.
摘要翻译： 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。
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5.发明申请公开(公告)号：US20130059866A1
公开(公告)日：2013-03-07
申请号：US13402996
申请日：2012-02-23
申请人： Horst Dollinger , Rogelio Perez Frutos , Soojin Kim , Jason Alan Mulder , Peter Nickolaus , Nitinchandra D. Patel , Pascale Pouzet , Chris Hugh Senanayake , Thomas Gabriel Tampone , Xudong Wei , Ulrike Werthmann , Bing-Shiou Yang
发明人： Horst Dollinger , Rogelio Perez Frutos , Soojin Kim , Jason Alan Mulder , Peter Nickolaus , Nitinchandra D. Patel , Pascale Pouzet , Chris Hugh Senanayake , Thomas Gabriel Tampone , Xudong Wei , Ulrike Werthmann , Bing-Shiou Yang
IPC分类号： A61K31/519 , A61P11/00 , A61P1/00 , A61P19/02 , A61P17/00 , A61P27/02 , A61P25/00 , A61P11/06 , A61P1/04 , A61P25/28 , A61P25/18 , A61P25/16 , A61P25/04 , C07C213/02 , C07D401/04 , C07D495/04
CPC分类号： C07D495/04 , A61K31/519 , A61K45/06 , C07B2200/13 , C07C213/00 , C07D401/04 , C07C215/42
摘要： The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
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![PREPARATION OF DIHYDROTHIENO [3, 2-D] PYRIMIDINES AND INTERMEDIATES USED THEREIN](/abs-image/US/2010/09/02/US20100222585A1/abs.jpg.150x150.jpg)
6.发明申请PREPARATION OF DIHYDROTHIENO [3, 2-D] PYRIMIDINES AND INTERMEDIATES USED THEREIN 有权二氢O O O O O IN IN IN IN IN IN IN IN IN IN IN IN IN IN IN IN IN IN IN IN IN公开(公告)号：US20100222585A1
公开(公告)日：2010-09-02
申请号：US12738152
申请日：2008-10-15
申请人： Rogelio Frutos , Dhileepkumar Krishnamurthy , Jason Alan Mulder , Sonia Rodriguez , Chris Hugh Senanayake , Thomas G. Tampone
发明人： Rogelio Frutos , Dhileepkumar Krishnamurthy , Jason Alan Mulder , Sonia Rodriguez , Chris Hugh Senanayake , Thomas G. Tampone
IPC分类号： C07D491/04
CPC分类号： C07D495/04
摘要： 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 pounds 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.
摘要翻译： 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磅，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。
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7.发明授权Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma 有权哌啶子基 - 二氢噻吩并嘧啶亚砜及其用于治疗COPD和哮喘的用途公开(公告)号：US09150586B2
公开(公告)日：2015-10-06
申请号：US14239818
申请日：2012-03-15
申请人： Pascale A. J. Pouzet , Peter Nickolaus , Ulrike Werthmann , Rogelio P. Frutos , Bing-Shiou Yang , Soojin Kim , Jason Alan Mulder , Nitinchandra Patel , Chris H. Senanayake , Thomas G. Tampone , Xudong Wei
发明人： Pascale A. J. Pouzet , Peter Nickolaus , Ulrike Werthmann , Rogelio P. Frutos , Bing-Shiou Yang , Soojin Kim , Jason Alan Mulder , Nitinchandra Patel , Chris H. Senanayake , Thomas G. Tampone , Xudong Wei
IPC分类号： C07D239/02 , C07D495/04 , C07D401/04 , C07C213/00 , A61K31/519 , A61K45/06
CPC分类号： C07D495/04 , A61K31/519 , A61K45/06 , C07B2200/13 , C07C213/00 , C07D401/04 , C07C215/42
摘要： The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
摘要翻译： 本发明涉及式I的新颖的哌啶子基 - 二氢噻吩并嘧啶亚砜，其中环A是可任选包含一个或两个氮原子的6元芳香环，并且其中R是Cl并且其中R可以位于对 - - 环A的邻位，其中S *是表示手性中心的硫原子，以及其所有药学上可接受的盐，对映异构体和外消旋物，水合物和溶剂合物以及这些化合物用于治疗炎性或过敏性疾病的用途 的呼吸道如COPD或哮喘。
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8.发明申请NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA 审中-公开新型哌啶二氢吲哚尼酮硫代磷酸酯及其用于治疗COPD和ASTHMA的用途公开(公告)号：US20150045376A1
公开(公告)日：2015-02-12
申请号：US13963513
申请日：2013-08-09
申请人： Pascale A.J. POUZET , Peter NICKOLAUS , Ulrike WERTHMANN , Rogelio P. FRUTOS , Bing-Shiou YANG , Soojin KIM , Jason Alan MULDER , Nitinchandra D. PATEL , Chris Hugh SENANAYAKE , Thomas Gabriel TAMPONE , Xudong WEI
发明人： Pascale A.J. POUZET , Peter NICKOLAUS , Ulrike WERTHMANN , Rogelio P. FRUTOS , Bing-Shiou YANG , Soojin KIM , Jason Alan MULDER , Nitinchandra D. PATEL , Chris Hugh SENANAYAKE , Thomas Gabriel TAMPONE , Xudong WEI
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Piperidino-dihydrothienopyrimidine sulfoxides of formula I wherein: Ring A is a 6-membered aromatic ring optionally comprising one or two nitrogen atoms and R is Cl and is located in the para-, meta-, or ortho-position of Ring A, S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
摘要翻译： 式I的哌啶子基 - 二氢噻吩并嘧啶亚砜其中：环A是任选地包含一个或两个氮原子并且R是Cl并且位于环A的对位，间位或邻位的6元芳香环，S * 是表示手性中心的硫原子及其所有药学上可接受的盐，对映异构体和外消旋体，水合物和溶剂合物，以及这些化合物用于治疗呼吸道炎症或过敏性疾病如COPD或哮喘的用途。
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公开(公告)号：US09199904B2
公开(公告)日：2015-12-01
申请号：US14005393
申请日：2012-03-15
IPC分类号： C07C51/16 , C07C51/09 , C07C51/02 , C07C51/41 , C07C51/43 , C07C57/58 , C07C57/62 , C07C43/176 , C07C69/65 , C07F7/18
CPC分类号： C07C51/09 , C07B2200/07 , C07C43/176 , C07C51/02 , C07C51/412 , C07C51/43 , C07C57/58 , C07C57/62 , C07C69/65 , C07F7/1804
摘要： The present invention relates to a process of making a compound of formula (XII) or (XIIA): wherein R1,R2, R4 and X are as defined herein.
摘要翻译： 本发明涉及制备式（XII）或（XIIA）化合物的方法：其中R1，R2，R4和X如本文所定义。
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公开(公告)号：US09029592B2
公开(公告)日：2015-05-12
申请号：US13761434
申请日：2013-02-07
IPC分类号： C07C269/00 , C07C259/14 , C07C251/40 , C07C47/24 , C07C271/12 , C07C29/143 , C07C45/27 , C07C249/08 , C07F5/02
CPC分类号： C07C259/14 , C07B2200/07 , C07C29/143 , C07C45/27 , C07C47/24 , C07C249/08 , C07C251/40 , C07C269/00 , C07C271/12 , C07C2601/02 , C07F5/025 , C07C33/46
摘要： The present invention relates to a process of making a compound of formula (I): Wherein, R1, R2, R4 and X are as defined herein.
摘要翻译： 本发明涉及制备式（I）化合物的方法：其中R1，R2，R4和X如本文所定义。
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