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1. 发明申请

WO2005090383A3 PROCESS FOR PREPARING MACROCYCLIC DIPEPTIDES WHICH ARE SUITABLE FOR THE TREATMENT OF HEPATITIS C VIRAL INFECTIONS 审中-公开
标题翻译：制备适用于治疗丙型肝炎病毒感染的大环吡咯的方法
公开(公告)号：WO2005090383A3
公开(公告)日：2005-12-01
申请号：PCT/US2005008366
申请日：2005-03-11
申请人： BOEHRINGER INGELHEIM INT , BUSACCA CARL ALAN , FARINA VITTORIO , GALLOU FABRICE , HADDAD NIZAR , WANG XIAO-JUN , WEI XUDONG , XU JINGHUA , XU YIBO , YEE NATHAN K , ZHANG LI
发明人： BUSACCA CARL ALAN , FARINA VITTORIO , GALLOU FABRICE , HADDAD NIZAR , WANG XIAO-JUN , WEI XUDONG , XU JINGHUA , XU YIBO , YEE NATHAN K , ZHANG LI
IPC分类号： A61K31/4709 , A61K38/00 , A61K38/12 , C07D417/14 , C07K1/00 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/12
CPC分类号： C07K5/0802 , A61K38/00 , C07D417/14 , C07K1/006 , C07K5/06165 , C07K5/0827
摘要： Disclosed is a multi-step process for preparing a macrocyclic compound of the formula (I); wherein Q is a radical of the following formula (II); and the other variables are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
摘要翻译：公开了用于制备式（I）的大环化合物的多步骤方法; 其中Q是下式（II）的基团; 其他变量如本文所定义。式（I）化合物是治疗丙型肝炎病毒（HCV）感染的有效活性剂。

2. 发明申请

WO2006096652A2 PROCESS FOR PREPARING MACROCYCLIC COMPOUNDS 审中-公开
标题翻译：制备大分子化合物的方法
公开(公告)号：WO2006096652A2
公开(公告)日：2006-09-14
申请号：PCT/US2006007954
申请日：2006-03-06
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA , BUSACCA CARL ALAN , GALLOU FABRICE , HADDAD NIZAR , HOSSAIN AZAD , KAPADIA SURESH R , LIU JIANXIU , SENANAYAKE CHRIS HUGH , WEI XUDONG , YEE NATHAN K
发明人： BUSACCA CARL ALAN , GALLOU FABRICE , HADDAD NIZAR , HOSSAIN AZAD , KAPADIA SURESH R , LIU JIANXIU , SENANAYAKE CHRIS HUGH , WEI XUDONG , YEE NATHAN K
IPC分类号： C07K5/08 , C07D401/04 , C07D417/04
CPC分类号： C07D401/04 , C07D417/04 , C07D487/04 , C07K5/0808 , C07K5/0812
摘要： Disclosed is a process for preparing a macrocyclic compound of the formula (I) wherein a hydroxyl-substituted macrocyclic compound of formula (3) is reacted with a sulfonyl-substituted compound of formula QUIN. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
摘要翻译：公开了制备式（I）的大环化合物的方法，其中式（3）的羟基取代的大环化合物与磺酰基取代的式QuIN化合物反应。式（I）化合物是用于治疗丙型肝炎病毒（HCV）感染的有效活性剂。

3. 发明申请

WO2004092203A3 PROCESS FOR PREPARING MACROCYCLIC COMPOUNDS 审中-公开
标题翻译：制备大环化合物的方法
公开(公告)号：WO2004092203A3
公开(公告)日：2004-12-09
申请号：PCT/US2004010476
申请日：2004-04-06
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA , DONSBACH KAI , ECKER DIETER , FRUTOS ROGELIO PEREZ , GALLOU FABRICE , GUTHEIL DIETER , HADDAD NIZAR , HAGENKOETTER ROBERT , KEMMER DIRK , KROEBER JUTTA , NICOLA THOMAS , SCHNAUBELT JUERGEN , SCHUL MICHAEL , SIMPSON ROBERT DONALD , WEI XUDONG , WINTER ERIC , XU YIBO , YEE NATHAN K , BRANDENBURG JOERG
发明人： DONSBACH KAI , ECKER DIETER , FRUTOS ROGELIO PEREZ , GALLOU FABRICE , GUTHEIL DIETER , HADDAD NIZAR , HAGENKOETTER ROBERT , KEMMER DIRK , KROEBER JUTTA , NICOLA THOMAS , SCHNAUBELT JUERGEN , SCHUL MICHAEL , SIMPSON ROBERT DONALD , WEI XUDONG , WINTER ERIC , XU YIBO , YEE NATHAN K , BRANDENBURG JOERG
IPC分类号： B01J31/22 , C07D491/08 , C07K1/00 , C07K1/08 , C07K5/083 , C07K5/087 , C07B37/10 , C07D207/10 , C07D265/32 , 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, R through R , D,A and R are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
摘要翻译：公开了制备式（I）的大环化合物的方法，其中使用式（II）的中间体其中W，R 1至R 4，D，A和R 12为如本文所定义的。式（I）化合物是治疗丙型肝炎病毒（HCV）感染的有效活性剂。

4. 发明申请

WO2008080891A3 PROCESS FOR THE SYNTHESIS OF DERIVATIVES OF 3-AMINO-TETRAHYDROFURAN-3-CARBOXYLIC ACID AND USE THEREOF AS MEDICAMENTS 审中-公开
标题翻译：合成3-氨基 - 四氢呋喃-3-羧酸衍生物的方法及其用作药物
公开(公告)号：WO2008080891A3
公开(公告)日：2008-10-02
申请号：PCT/EP2007064406
申请日：2007-12-21
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA , HAN ZHENGXU , GERLACH KAI , KRISHNAMURTHY DHILEEPKUMAR , MATTHES BURKHARD , NAR HERBERT , PFAU ROLAND , PRIEPKE HENNING , SCHULER-METZ ANNETTE , SENANAYAKE CHRIS H , SIEGER PETER , TANG WENJUN , WIENEN WOLFGANG , XU YIBO , YEE NATHAN K
发明人： HAN ZHENGXU , GERLACH KAI , KRISHNAMURTHY DHILEEPKUMAR , MATTHES BURKHARD , NAR HERBERT , PFAU ROLAND , PRIEPKE HENNING , SCHULER-METZ ANNETTE , SENANAYAKE CHRIS H , SIEGER PETER , TANG WENJUN , WIENEN WOLFGANG , XU YIBO , YEE NATHAN K
IPC分类号： C07D307/24 , C07D409/14 , C07D413/14
CPC分类号： C07D409/14 , C07D307/24 , C07D413/14
摘要： The present invention relates to a process for the manufacturing of substituted 3- amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) and their precursors in high optical purity to the precursors of the synthesis of substituted S-Amino-tetrahydrofuran-S-carboxylic acid amides of general formula (I) in high optical purity, and to the tautomers, enantiomers, diastereomers, mixtures and salts of substituted 3-amino- tetrahydrofuran-3-carboxylic acid amides of general formula (I) in high optical purity, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
摘要翻译：本发明涉及通式（I）的取代的3-氨基 - 四氢呋喃-3-羧酸酰胺及其前体在高光学纯度下制备成取代的S-氨基 - 四氢呋喃-3-羧酸酰胺的合成前体的方法，具有高光学纯度的通式（I）的S-羧酸酰胺，以及通式（I）的取代的3-氨基 - 四氢呋喃-3-羧酸酰胺的高光学性质的互变异构体，对映异构体，非对映异构体，混合物和盐纯度，特别是其具有有价值特性的无机酸或有机酸或碱的生理学上可接受的盐。

6. 发明专利

CA2556917C PROCESS FOR PREPARING MACROCYCLIC COMPOUNDS 未知
公开(公告)号：CA2556917C
公开(公告)日：2013-07-09
申请号：CA2556917
申请日：2005-03-11
申请人： BOEHRINGER INGELHEIM INT
发明人： BUSACCA CARL ALAN , FARINA VITTORIO , GALLOU FABRICE , HADDAD NIZAR , WANG XIAO-JUN , WEI XUDONG , XU JINGHUA , XU YIBO , YEE NATHAN K , ZHANG LI
IPC分类号： C07K5/06 , A61K31/4709 , A61K38/00 , A61K38/12 , C07D417/14 , C07K1/00 , C07K5/078 , C07K5/08 , C07K5/12
摘要： Disclosed is a multi-step process for preparing a macrocyclic compound of the formula (I); wherein Q is a radical of the following formula (II); and the other variables are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.

7. 发明专利

AU2006220708B9 Process for preparing macrocyclic compounds 未知
公开(公告)号：AU2006220708B9
公开(公告)日：2013-01-17
申请号：AU2006220708
申请日：2006-03-06
申请人： BOEHRINGER INGELHEIM INT
发明人： SENANAYAKE CHRIS HUGH , YEE NATHAN K , KAPADIA SURESH R , HADDAD NIZAR , GALLOU FABRICE , LIU JIANXIU , WEI XUDONG , HOSSAIN AZAD , BUSACCA CARL ALAN
IPC分类号： C07K5/08 , C07D401/04 , C07D417/04
摘要： Disclosed is a process for preparing a macrocyclic compound of the formula (I) wherein a hydroxyl-substituted macrocyclic compound of formula (3) is reacted with a sulfonyl-substituted compound of formula QUIN. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.

8. 发明专利

AU2006220708B2 Process for preparing macrocyclic compounds 未知
公开(公告)号：AU2006220708B2
公开(公告)日：2012-09-27
申请号：AU2006220708
申请日：2006-03-06
申请人： BOEHRINGER INGELHEIM INT
发明人： SENANAYAKE CHRIS HUGH , YEE NATHAN K , KAPADIA SURESH R , HADDAD NIZAR , GALLOU FABRICE , LIU JIANXIU , WEI XUDONG , HOSSAIN AZAD , BUSACCA CARL ALAN
IPC分类号： C07K5/08 , C07D401/04 , C07D417/04
摘要： Disclosed is a process for preparing a macrocyclic compound of the formula (I) wherein a hydroxyl-substituted macrocyclic compound of formula (3) is reacted with a sulfonyl-substituted compound of formula QUIN. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.

9. 发明专利

UA96973C2 СПОСОБ СИНТЕЗА ПРОИЗВОДНЫХ 3-АМИНОТЕТРАГИДРОФУРАН-3-КАРБОНОВОЙ КИСЛОТЫ И ИХ ПРИМЕНЕНИЕ КАК ЛЕКАРСТВЕННЫХ СРЕДСТВ 未知
公开(公告)号：UA96973C2
公开(公告)日：2011-12-26
申请号：UAA200907732
申请日：2007-12-21
申请人： BOEHRINGER INGELHEIM INT
发明人： PFAU ROLAND , HAN ZHENGXU , GERLACH KAI , KRISHNAMURTHY DHILEEPKUMAR , MATTHES BURKHARD , NAR HERBERT , PRIEPKE HENNING , SCHULER-METZ ANNETTE , SENANAYAKE CHRIS H , SIEGER PETER , TANG WENJUN , WIENEN WOLFGANG , XU YIBO , YEE NATHAN K
IPC分类号： C07D307/24 , C07D409/14 , C07D413/14
摘要： Взаявкеописанспособполучениязамещенныхамидов 3-аминотетрагидрофуран-3-карбоновойкислотыобщейформулы (I) иихпредшественниковвысокойоптическойчистоты(I),предшественниковсинтезазамещенныхамидов 3-аминотетрагидрофуран-3-карбоновойкислотыобщейформулы (I) высокойоптическойчистотыи таутомеров, энантиомеров, диастереоизомеров, смесейи солейзамещенныхамидов 3-аминотетрагидрофуран-3-карбоновойкислотыобщейформулы (I) высокойоптическойчистоты, преимущественно - ихфизиологическиприемлемыхсолейс неорганическимиилиорганическимикислотамиилиоснованиями, которыеимеютценныесвойства.

10. 发明专利

AR078123A1 SINTESIS ESTEREOSELECTIVA DE CIERTOS ALCOHOLES SUSTITUIDOS CON TRIFLUOROMETILO 未知
公开(公告)号：AR078123A1
公开(公告)日：2011-10-19
申请号：ARP100101947
申请日：2010-06-02
申请人： BOEHRINGER INGELHEIM INT
发明人： FANDRICK DANIEL ROBERT , YEE NATHAN K , REEVES JONATHAN TIMOTHY , SONG JINHUA J
IPC分类号： C07C49/105 , C07C49/167
摘要： Reivindicacion 1: Un proceso para la síntesis de un compuesto de formula (10) en la que R1 es un grupo arilo sustituido con uno a tres grupos sustituyentes, donde cada grupo sustituyente de R1 es independientemente alquilo C1-5, aminocarbonilo, alquilaminocarbonilo, dialquilaminocarbonilo, halogeno, carboxi, ciano o trifluorometilo, donde cada grupo sustituyente de R1 está opcionalmente sustituido independientemente con uno a tres sustituyentes seleccionados entre alquilo C1-3, alcoxi C1-3, fenilo y alcoxifenilo; y cada uno de R2 y R3 es independientemente alquilo C1-5, caracterizado porque comprende: (a) hacer reaccionar el ácido de Meldrum de formula (A) con un compuesto de carbonilo de formula (B) que tiene R2 y R3, en un disolvente adecuado, en presencia de una base adecuada, para proporcionar la alquilideno-diona de formula (C); (b) hacer reaccionar la alquilideno-diona de formula (C) con un organohaluro adecuado de formula (D) en la que Hal es Br o I, en presencia de un reactivo organometálico adecuado tal como un cloruro de alquil magnesio, en un disolvente adecuado, y posteriormente anadir a la mezcla de reaccion agua y un ácido adecuado, tal como ácido clorhídrico, y calentar para formar el ácido de formula (E); (c) hacer reaccionar el ácido de formula (E) con un reactivo de trifluorometilo tal como anhídrido trifluoroacético, en un disolvente adecuado, en presencia de una base adecuada, para proporcionar un compuesto de formula (10).

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