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1. 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。

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

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。

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。

5. 发明专利

ES2439732T3 Procedimiento para preparar compuestos macrocíclicos 未知
公开(公告)号：ES2439732T3
公开(公告)日：2014-01-24
申请号：ES06737166
申请日：2006-03-06
申请人： BOEHRINGER INGELHEIM INT , BOEHRINGER INGELHEIM PHARMA
发明人： BUSACCA CARL , 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
摘要： Un procedimiento para preparar un compuesto de la fórmula (I) siguiente:**Fórmula** en la cual W es CH o N, L0 es H, halo, alquilo C1-6, cicloalquilo C3-6, haloalquilo C1-6, alcoxi C1-6, cicloalcoxi C3-6, hidroxi o N(R23)2, en donde cada R23 es independientemente H, alquilo C1-6 o cicloalquilo C3-6; L1, L2 son cada uno independientemente H, halógeno, alquilo C1-4, -O-alquilo C1-4 o -S-alquilo C1-4 (estando el azufreen cualquier estado de oxidación); o L0 y L1 o L0 y L2 pueden estar covalentemente unidos para formar, junto con los dos átomos de C a los que están unidos, unanillo carbocíclico de 4, 5 ó 6 miembros, en el cual uno o dos (en el caso de un anillo de 5 ó 6 miembros) grupos -CH2- no directamente unidos entre sí, pueden estar reemplazados cada uno independientemente por -O- o NRa, endonde Ra es H o alquilo C1-4, y en donde dicho anillo está opcionalmente mono- o di-sustituido con alquilo C1-4;R2 es H, halo, alquilo C1-6, cicloalquilo C3-6, haloalquilo C1-6, tioalquilo C1-6, alcoxi C1-6, cicloalcoxi C3-6, (alcoxi C2-7)-alquilo C1-6, arilo C6 o C10, o Het, en donde Het es un heterociclo saturado o insaturado de cinco, seis o sietemiembros que contiene de uno a cuatro heteroátomos seleccionados entre nitrógeno, oxígeno y azufre; estando dicho cicloalquilo, arilo o Het sustituido con R6, en donde R6 es H, halo, alquilo C1-6, cicloalquilo C3-6, alcoxi C1-6, cicloalcoxi C3-6, NO2, N(R7)2, NH-C(O)-R7; o NHC(O)-NH-R7, en donde cada R7 es, independientemente: H, alquilo C1-6 o cicloalquilo C3-6; o R6 es NH-C(O)-OR8, en donde R8 es alquilo C1-6 o cicloalquilo C3-6; R3 es hidroxi, NH2 o un grupo de fórmula -NH-R9, en donde R9 es arilo C6 o C10, heteroarilo, -C(O)-R10, -C(O)-NHR10 o -C(O)-OR10, en donde R10 es alquilo C1-6 o cicloalquilo C3-6; D es una cadena de alquileno insaturado de 5 a 10 átomos.

6. 发明专利

DE60141654D1 未知
公开(公告)号：DE60141654D1
公开(公告)日：2010-05-06
申请号：DE60141654
申请日：2001-05-15
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： SONG JINHUA J , YEE NATHAN K , KAPADIA SURESH R
IPC分类号： C07D213/38 , C07D213/61
摘要： Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.

7. 发明专利

ES2290769T3 SINTESIS ESTEREOSELECTIVA DE CIERTOS ALCOHOLES SUBSTITUIDOS CON TRIFLUORMETILO. 未知
公开(公告)号：ES2290769T3
公开(公告)日：2008-02-16
申请号：ES04789408
申请日：2004-09-30
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： SONG JINHUA J , TAN ZHULIN , XU JINGHUA , YEE NATHAN K , SENANAYAKE CHRIS H
IPC分类号： C07D303/22 , C07D301/27 , C07F3/04
摘要： Un procedimiento para la síntesis estereoselectiva de un compuesto de fórmula, en donde R1 es un grupo arilo o heteroarilo, cada uno opcionalmente independientemente substituido con uno a tres grupos substituyentes, en donde cada grupo substituyente de R1 es independientemente alquilo de 1 a 5 átomos de carbono, alquenilo de 2 a 5 átomos de carbono, alquinilo de 2 a 5 átomos de carbono, cicloalquilo de 3 a 8 átomos de carbono, heterociclilo, arilo, heteroarilo, alcoxilo de 1 a 5 átomos de carbono, alqueniloxilo de 2 a 5 átomos de carbono, alquiniloxilo de 2 a 5 átomos de carbono, ariloxilo, alcanoiloxilo de 1 a 5 átomos de carbono, alcanoilo de 1 a 5 átomos de carbono, aroilo, trifluormetilo, trifluormetoxilo, ó alquiltio de 1 a 5 átomos de carbono, en donde cada grupo substituyente de R1 está opcional-mente independientemente substituido con uno a tres grupos substituyentes seleccionados entre metilo, metoxilo, flúor, cloro o hidroxilo; y R2 y R3 son cada uno independientemente, hidrógenoo alquilo de 1 a 5 átomos de carbono ó R2 y R3 juntamente con el átomo de carbono están habitualmente unidos para formar un anillo cicloalquilo espiro de 3 a 8 átomos de carbono.

8. 发明专利

AT366726T 未知
公开(公告)号：AT366726T
公开(公告)日：2007-08-15
申请号：AT04789408
申请日：2004-09-30
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： SONG JINHUA J , TAN ZHULIN , XU JINGHUA , YEE NATHAN K , SENANAYAKE CHRIS H
IPC分类号： C07D303/22 , C07D301/27 , C07F3/04
摘要： A process for stereoselective synthesis of compounds of Formula X wherein: R1 is an aryl or heteroaryl group, each optionally independently substituted with one to three substituent groups, wherein each substituent group of R1 is independently C1-C5 alkyl, C2-C5 alkenyl, C2-C5 alkynyl, C3-C8 cycloalkyl, heterocyclyl, aryl, heteroaryl, C1-C5 alkoxy, C2-C5 alkenyloxy, C2-C5 alkynyloxy, aryloxy, C1-C5 alkanoyloxy, C1-C5 alkanoyl, aroyl, trifluoromethyl, trifluoromethoxy, or C1-C5 alkylthio, wherein each substituent group of R1 is optionally independently substituted with one to three substituent groups selected from methyl, methoxy, fluoro, chloro, hydroxy, oxo, cyano, or amino; and R2 and R3 are each independently hydrogen or C1-C5 alkyl, or R2 and R3 together with the carbon atom they are commonly attached to form a C3-C8 spiro cycloalkyl ring.

9. 发明专利

CA2557896A1 STEREOSELECTIVE SYNTHESIS OF CERTAIN TRIFLUOROMETHYL-SUBSTITUTED ALCOHOLS 未知
公开(公告)号：CA2557896A1
公开(公告)日：2005-09-29
申请号：CA2557896
申请日：2005-03-04
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： XU JINGHUA , GALLOU FABRICE , SONG JINHUA J , YEE NATHAN K , TAN ZHULIN , SENANAYAKE CHRIS HUGH
IPC分类号： C07D471/02 , C07C33/46 , C07C323/03 , C07D471/04

10. 发明专利

CA2542741A1 STEREOSELECTIVE SYNTHESIS OF CERTAIN TRIFLUOROMETHYL-SUBSTITUTED ALCOHOLS 未知
公开(公告)号：CA2542741A1
公开(公告)日：2005-05-06
申请号：CA2542741
申请日：2004-09-30
申请人： BOEHRINGER INGELHEIM PHARMA
发明人： YEE NATHAN K , SENANAYAKE CHRIS H , SONG JINHUA J , XU JINGHUA , TAN ZHULIN
IPC分类号： C07D303/22 , C07D301/27 , C07F3/04
摘要： A process for stereoselective synthesis of compounds of Formula X wherein: R1 is an aryl or heteroaryl group, each optionally independently substituted with one to three substituent groups, wherein each substituent group of R1 is independently C1-C5 alkyl, C2-C5 alkenyl, C2-C5 alkynyl, C3-C8 cycloalkyl, heterocyclyl, aryl, heteroaryl, C1-C5 alkoxy, C2-C5 alkenyloxy, C2-C5 alkynyloxy, aryloxy, C1-C5 alkanoyloxy, C1-C5 alkanoyl, aroyl, trifluoromethyl, trifluoromethoxy, or C1-C5 alkylthio, wherein each substituent group of R1 is optionally independently substituted with one to three substituent groups selected from methyl, methoxy, fluoro, chloro, hydroxy, oxo, cyano, or amino; and R2 and R3 are each independently hydrogen or C1-C5 alkyl, or R2 and R3 together with the carbon atom they are commonly attached to form a C3-C8 spiro cycloalkyl ring.

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