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1.发明公开SYNTHESIS OF DIHYDROTHIENO[3,2-d]PYRIMIDINE DIOLS AND SIMILAR PYRIMIDINE DIOLS 有权二氢蝶啶[3,2-d]嘧啶二醇和类似的嘧啶二醇的合成
公开(公告)号：EP2315755A2
公开(公告)日：2011-05-04
申请号：EP09736709.8
申请日：2009-05-07
发明人： FRUTOS, Rogelio, Perez , TAMPONE, Thomas, G. , MULDER, Jason, Alan , KRISHNAMURTHY, Dhileepkumar , SENANAYAKE, Chris, Hugh
IPC分类号： C07D239/70 , 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，其效率高，产率高，并且不需要昂贵且潜在不稳定的中间体。 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或胃肠疾病和不适症状，外周或中枢神经系统疾病和病症，炎性病症和癌症。
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2.发明授权SYNTHESIS OF DIHYDROTHIENO[3,2-d]PYRIMIDINE DIOLS AND SIMILAR PYRIMIDINE DIOLS 有权二氢噻的合成[3,2-D] PYRIMIDINDIOLEN及类似PYRIMIDINDIOLEN
公开(公告)号：EP2315755B1
公开(公告)日：2012-08-08
申请号：EP09736709.8
申请日：2009-05-07
发明人： FRUTOS, Rogelio, Perez , TAMPONE, Thomas, G. , MULDER, Jason, Alan , KRISHNAMURTHY, Dhileepkumar , SENANAYAKE, Chris, Hugh
IPC分类号： C07D239/70 , 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.-
3.发明授权NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA 有权新哌啶DIHYDROTHIEN嘧啶亚砜及其用途用于治疗哮喘和COPD的治疗
公开(公告)号：EP2748156B1
公开(公告)日：2015-12-16
申请号：EP12762543.2
申请日：2012-08-17
发明人： POUZET, Pascale, A., J. , NICKOLAUS, Peter , WERTHMANN, Ulrike , FRUTOS, Rogelio, P. , YANG, Bing-Shiou , KIM, Soojin , MULDER, Jason, Alan , PATEL, Nitinchandra , SENANAYAKE, Chris, H. , TAMPONE, Thomas, G. , WEI, Xudong
IPC分类号： C07D401/04 , C07D495/04 , C07C211/35 , A61K31/519 , A61P29/00
CPC分类号： C07D495/04 , A61K31/519 , A61K45/06 , C07B2200/13 , C07C213/00 , C07D401/04 , C07C215/42
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4.发明公开NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA 有权新哌啶DIHYDROTHIEN嘧啶亚砜及其用途用于治疗哮喘和COPD的治疗
公开(公告)号：EP2748156A1
公开(公告)日：2014-07-02
申请号：EP12762543.2
申请日：2012-08-17
发明人： POUZET, Pascale, A., J. , NICKOLAUS, Peter , WERTHMANN, Ulrike , FRUTOS, Rogelio, P. , YANG, Bing-Shiou , KIM, Soojin , MULDER, Jason, Alan , PATEL, Nitinchandra , SENANAYAKE, Chris, H. , TAMPONE, Thomas, G. , WEI, Xudong
IPC分类号： C07D401/04 , C07D495/04 , C07C211/35 , A61K31/519 , A61P29/00
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 CI 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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