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公开(公告)号：EP1615947A2
公开(公告)日：2006-01-18
申请号：EP04759130.0
申请日：2004-04-06
发明人： DONSBACH, Kai , ECKER, Dieter , FRUTOS, Rogelio., Boehringer Ingelheim PharmaInc. , GALLOU, Fabrice, Boehringer Ingelheim Pharma. Inc. , GUTHEIL, Dieter , HADDAD, Nizar, Boehringer Ingelheim Pharma. Inc. , HAGENKOETTER, Robert , KEMMER, Dirk , KROEBER, Jutta , NICOLA, Thomas , SCHNAUBELT, Juergen , SCHUL, Michael , SIMPSON, Robert, Donald , WEI, Xudong, Boehringer Ingelheim Pharma. Inc. , WINTER, Eric , XU, Yibo, Boehringer Ingelheim Pharmaceuticals Inc , YEE, Nathan, K., Boehringer Ingelheim Pharma. Inc. , BRANDENBURG, Joerg
IPC分类号： C07K1/00 , C07K1/08 , C07B37/10 , C07D265/32 , C07D207/10 , B01J31/22 , C07K5/08
CPC分类号： B01J31/2226 , B01J31/2265 , B01J31/2404 , B01J2231/543 , B01J2531/821 , C07D491/08 , C07K1/006 , C07K1/086 , C07K5/0804 , C07K5/0812
摘要： Disclosed is a process for preparing a macrocyclic compound of the formula (I) which is carried out using an intermediate of the formula (II) wherein W, R1 through R4, D,A and R12 are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
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2.发明公开SYNTHESIS OF 6,7-DIHYDRO-5H-IMIDAZOÝ1,2-A¨IMIDAZOLE-3-SULFONIC ACID AMIDES 审中-公开6,7-二氢-5H-咪唑并[1,2-a〕咪唑-3-磺酰胺的合成
公开(公告)号：EP1776367A1
公开(公告)日：2007-04-25
申请号：EP05775277.6
申请日：2005-07-25
发明人： WANG, X., Boehringer Ingelheim Pharma. Inc. , WIRTH, Thomas , NICOLA, Thomas , ZHANG, L., Boehringer Ingelheim Pharma. Inc. , FRUTOS, R. P., Boehringer Ingelheim Pharma. Inc. , XU, Y., Boehringer Ingelheim Pharma. Inc. , KRISHNAMURTHY, D., Boehringer Ingelheim Phrm. Inc. , NUMMY, L. J., Boehringer Ingelheim Pharm. Inc. , VARSOLONA, R. J., Boehringer Ingelheim Pharm. Inc. , KROEBER, Jutta , SENANAYAKE, C. H., Boehringer Ingelheim Phrm. Inc.
IPC分类号： C07D487/04 , A61P29/00 , A61K31/4188
CPC分类号： C07D487/04 , C07C275/24 , C07D239/06
摘要： Disclosed is a multi-step process for preparing a compound of Formula I wherein R1 to R3 are as defined herein. The compounds of Formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.
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3.发明公开PROCESS FOR THE MANUFACTURE OF (E)-4-N,N-DIALKYLAMINO CROTONIC ACID IN HX SALT FORM AND USE THEREOF FOR SYNTHESIS OF EGFR TYROSINE KINASE INHIBITORS 有权用于生产（E）-4-N，N-二烷基氨基巴豆酸IN HX盐形式及其用途用于合成的EGFR酪氨酸激酶抑制剂的
公开(公告)号：EP3089961A1
公开(公告)日：2016-11-09
申请号：EP14828037.3
申请日：2014-12-23
发明人： ZHENG, Juncheng , DENG, Da , LV, Guanghua , YAN, Jun , BRANDENBURG, Joerg , KROEBER, Jutta , SCHOLZ, Ulrich
IPC分类号： C07C227/10 , C07C227/18 , C07C229/30 , C07D405/04
CPC分类号： C07D405/04 , C07C221/00 , C07C227/10 , C07C227/16 , C07C227/18 , C07C229/30
摘要： The present invention is directed to an efficient process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form of formula I wherein R1 and R2 independently denote C1-3-alkyl groups and X− denotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of EGFR tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt I and activated derivatives thereof as intermediates.
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公开(公告)号：EP3089961B1
公开(公告)日：2018-07-11
申请号：EP14828037.3
申请日：2014-12-23
发明人： ZHENG, Juncheng , DENG, Da , LV, Guanghua , YAN, Jun , BRANDENBURG, Joerg , KROEBER, Jutta , SCHOLZ, Ulrich
IPC分类号： C07C227/10 , C07C227/18 , C07C229/30 , C07D405/04
CPC分类号： C07D405/04 , C07C221/00 , C07C227/10 , C07C227/16 , C07C227/18 , C07C229/30
摘要： The present invention is directed to an efficient process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form of formula I wherein R1 and R2 independently denote C1-3-alkyl groups and X− denotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of EGFR tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt I and activated derivatives thereof as intermediates.
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5.发明公开PROCESS FOR THE PREPARATION OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-A]IMIDAZOLE-3-SULFONIC ACID AMIDES AND INTERMEDIATES USED THEREIN 审中-公开用于生产6,7-二氢-5H-咪唑并[1,2-a〕咪唑-3-磺酰胺和ITS中使用的中间产物
公开(公告)号：EP1979309A2
公开(公告)日：2008-10-15
申请号：EP07710134.3
申请日：2007-01-16
发明人： WIRTH, Thomas , GUTHEIL, Dieter , KROEBER, Jutta , NICOLA, Thomas , RAPP, Armin , ORLICH, Simone , WANG, Xiao-jun , KRISHNAMURTHY, Dhileepkumar
IPC分类号： C07C275/18 , C07C275/24 , C07D487/04
CPC分类号： C07D317/28 , C07C273/1836 , C07D487/04 , C07C275/24
摘要： Disclosed is an improved multi-step process for preparing a compound of Formula I and intermediates used therein: (I) wherein R1 to R3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.
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