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1. 发明申请

WO2010141331A2 STEREOSELECTIVE SYNTHESIS OF CERTAIN TRIFLUOROMETHYL-SUBSTITUTED ALCOHOLS 审中-公开
标题翻译：某些三氟甲磺酸取代醇的立体选择性合成
公开(公告)号：WO2010141331A2
公开(公告)日：2010-12-09
申请号：PCT/US2010/036499
申请日：2010-05-28
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , FANDRICK, Daniel Robert , REEVES, Jonathan Timothy , SONG, Jinhua J. , TAN, Zhulin , QU, Bo , YEE, Nathan , RODRIGUEZ, Sonia
发明人： FANDRICK, Daniel Robert , REEVES, Jonathan Timothy , SONG, Jinhua J. , TAN, Zhulin , QU, Bo , YEE, Nathan , RODRIGUEZ, Sonia
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07B2200/07
摘要： A process for stereoselective synthesis of a compound of Formula (X): wherein: wherein: R 1 is an aryl group substituted with one to three substituent groups, wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl, wherein each substituent group of R 1 is optionally independently substituted with one to three substituents selected from C 1 -C 3 alkyl, C 1 -C 3 alkoxy, phenyl, and alkoxyphenyl; R 2 and R 3 are each independently C 1 -C 5 alkyl; R 4 is C 1 -C 5 alkyl optionally independently substituted with one to three substituent groups, wherein each substituent group of R 4 is independently C 1 -C 3 alkyl, hydroxy, halogen, amino, or oxo; and R 5 is a heteroaryl group substituted with one to three substituent groups, wherein each substituent group of R 5 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkylsulfonylamino, aminosulfonyl, C 1 - C 5 alkylaminosulfonyl, C 1 -C 5 dialkylaminosulfonyl, halogen, hydroxy, carboxy, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, or C 1 -C 5 alkylthio wherein the sulfur atom is optionally oxidized to a sulfoxide or sulfone.
摘要翻译：一种用于立体选择性合成式（X）的化合物的方法：其中：其中：R1是被1至3个取代基取代的芳基，其中R1的每个取代基独立地是C1-C5烷基，氨基羰基，烷基氨基羰基，二烷基氨基羰基，卤素，羧基，氰基或三氟甲基，其中R 1的每个取代基任选地独立地被一至三个选自C 1 -C 3烷基，C 1 -C 3烷氧基，苯基和烷氧基苯基的取代基取代; R2和R3各自独立地为C1-C5烷基; R4是任选独立地被1至3个取代基取代的C 1 -C 5烷基，其中R 4的每个取代基独立地是C 1 -C 3烷基，羟基，卤素，氨基或氧代; R5是被一至三个取代基取代的杂芳基，其中R5的每个取代基独立地是C 1 -C 5烷基，氨基羰基，烷基氨基羰基，二烷基氨基羰基，烷基磺酰基氨基，氨基磺酰基，C 1 -C 5烷基氨基磺酰基，C 1 -C 5二烷基氨基磺酰基，卤素，羟基，羧基，氰基，三氟甲基，三氟甲氧基，三氟甲硫基或C 1 -C 5烷硫基，其中硫原子任选被氧化成亚砜或砜。

2. 发明申请

WO2005040145A1 STEREOSELECTIVE SYNTHESIS OF CERTAIN TRIFLUOROMETHYL-SUBSTITUTED ALCOHOLS 审中-公开
标题翻译：某些三氟甲磺酸取代醇的立体选择性合成
公开(公告)号：WO2005040145A1
公开(公告)日：2005-05-06
申请号：PCT/US2004/032257
申请日：2004-09-30
申请人： BOEHRINGER INGELHEIM PHARMACEUTICALS, INC. , SONG, Jinhua, J. , TAN, Zhulin , XU, Jinghua , YEE, Nathan, K. , SENANAYAKE, Chris, H.
发明人： SONG, Jinhua, J. , TAN, Zhulin , XU, Jinghua , YEE, Nathan, K. , SENANAYAKE, Chris, H.
IPC分类号： C07D303/22
CPC分类号： C07D303/22
摘要： A process for stereoselective synthesis of compounds of Formula (X) wherein: R 1 is an aryl or heteroaryl group, each optionally independently substituted with one to three substituent groups, wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, C 2 -C 5 alkenyl, C 2 -C 5 alkynyl, C 3 -C 8 cycloalkyl, heterocyclyl, aryl, heteroaryl, C 1 -C 5 alkoxy, C 2 -C 5 alkenyloxy, C 2 -C 5 alkynyloxy, aryloxy, C 1 -C 5 alkanoyloxy, C 1 -C 5 alkanoyl, aroyl, trifluoromethyl, trifluoromethoxy, or C 1 -C 5 alkylthio, wherein each substituent group of R 1 is optionally independently substituted with one to three substituent groups selected from methyl, methoxy, fluoro, chloro, hydroxy, oxo, cyano, or amino; and R 2 an R 3 are each independently hydrogen or C 1 -C 5 alkyl, or R 2 and R 3 together with the carbon atom they are commonly attached to form a C 3 -C 8 spiro cycloalkyl ring.
摘要翻译：用于立体选择性合成式（X）的化合物的方法，其中：R 1是芳基或杂芳基，每个任选地独立地被一至三个取代基取代，其中R 1的每个取代基独立地是C 1 -C 5 烷基，C 2 -C 5烯基，C 2 -C 5炔基，C 3 -C 8环烷基，杂环基，芳基，杂芳基，C 1 -C 5烷氧基，C 2 -C 5链烯氧基，C 2 -C 5炔氧基，芳氧基，C 1 -C 5烷酰氧基，C 1 -C 5烷酰基，芳酰基，三氟甲基，三氟甲氧基或C 1 -C 5烷硫基，其中R 1的每个取代基任选独立地被一至三个选自甲基，甲氧基，氟，氯，羟基，氧代，氰基或氨基的取代基取代。 R 2和R 3各自独立地为氢或C 1 -C 5烷基，或R 2和R 3与它们通常连接的碳原子一起形成C 3 -C 8螺环烷基环。

3. 发明申请

WO2019027860A1 INTERMEDIATE COMPOUNDS AND METHDODS 审中-公开
公开(公告)号：WO2019027860A1
公开(公告)日：2019-02-07
申请号：PCT/US2018/044279
申请日：2018-07-30
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BEYER, Phouvieng , BRAZZILLO, Jason A. , ERIKSSON, Magnus , LORENZ, Jon Charles , NUMMY, Laurence J. , RODRIGUEZ, Sonia , SAVOIE, Jolaine , SIDHU, Kanwar Pal Singh , SIEBER, Joshua Daniel , TAMPONE, Thomas Gabriel , TAN, Zhulin , WANG, June , ZHANG, Li
发明人： BEYER, Phouvieng , BRAZZILLO, Jason A. , ERIKSSON, Magnus , LORENZ, Jon Charles , NUMMY, Laurence J. , RODRIGUEZ, Sonia , SAVOIE, Jolaine , SIDHU, Kanwar Pal Singh , SIEBER, Joshua Daniel , TAMPONE, Thomas Gabriel , TAN, Zhulin , WANG, June , ZHANG, Li
IPC分类号： C07D487/10
摘要： The present invention relates to compounds of (II) and an acceptable salt or hydrate thereof method of making same.

4. 发明申请

WO2010141332A3 STEREOSELECTIVE SYNTHESIS OF CERTAIN TRIFLUOROMETHYL-SUBSTITUTED OXIRANES 审中-公开
公开(公告)号：WO2010141332A3
公开(公告)日：2010-12-09
申请号：PCT/US2010/036502
申请日：2010-05-28
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , FANDRICK, Daniel, Robert , KUZMICH, Daniel , REEVES, Jonathan, Timothy , SONG, Jinhua, J. , TAN, Zhulin , LEE, Thomas
发明人： FANDRICK, Daniel, Robert , KUZMICH, Daniel , REEVES, Jonathan, Timothy , SONG, Jinhua, J. , TAN, Zhulin , LEE, Thomas
IPC分类号： C07D303/08
摘要： A process for stereoselective synthesis of a compound of Formula (X) or Formula (X') : wherein: R 1 is an aryl group substituted with one to three substituent groups, wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, C 2 -C 5 alkenyl, C 2 - C 5 alkynyl, C 1 -C 5 alkoxy, C 1 -C 5 alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, C 1 -C 5 alkoxycarbonylamino, aminosulfonyl, C 1 -C 5 alkylaminosulfonyl, C 1 -C 5 dialkylaminosulfonyl, halogen, hydroxy, carboxy, cyano, trifluoromethyl, trifluoromethoxy, nitro, or C 1 -C 5 alkylthio wherein the sulfur atom is oxidized to sulfoxide or sulfone, and R 2 and R 3 are each independently hydrogen or C 1 -C 5 alkyl.

5. 发明申请

WO2009137432A1 A METHOD FOR PREPARING MACROCYCLES 审中-公开
标题翻译：一种制备大环化合物的方法
公开(公告)号：WO2009137432A1
公开(公告)日：2009-11-12
申请号：PCT/US2009/042773
申请日：2009-05-05
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG , SHU, Chutian , SENANAYAKE, Chris, Hugh , TAN, Zhulin , YEE, Nathan , ZENG, Xingzhong
发明人： SHU, Chutian , SENANAYAKE, Chris, Hugh , TAN, Zhulin , YEE, Nathan , ZENG, Xingzhong
IPC分类号： C07K1/00 , C07K5/12 , C07C6/06
CPC分类号： C07K5/0804 , C07K1/107
摘要： The present invention is directed to a method for the preparation of macrocyclic compounds of formula (I), comprising the step of cyclizing a diene of formula (II), in the presence of a catalyst, wherein R 1 -R 6 , A, W and V are as defined herein. The present invention is also directed to intermediate compounds of formula (II).
摘要翻译：本发明涉及一种制备式（I）的大环化合物的方法，包括在催化剂存在下使式（II）二烯环化的步骤，其中R 1 -R 6，A，W和V 如本文所定义。本发明还涉及式（II）的中间体化合物。

6. 发明申请

WO2018106746A3 NOVEL CHIRAL DIHYDROBENZOOXAPHOSPHOLE LIGANDS AND SYNTHESIS THEREOF 审中-公开
公开(公告)号：WO2018106746A3
公开(公告)日：2018-06-14
申请号：PCT/US2017/064797
申请日：2017-12-06
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , DESROSIERS, Jean-Nicolas , FANDRICK, Daniel Robert , HADDAD, Nizar , LI, Guisheng , PATEL, Nitinchandra D. , QU, Bo , RODRIGUEZ, Sonia , SENANAYAKE, Chris Hugh , SIEBER, Joshua Daniel , TAN, Zhulin , WANG, Xiao-Jun , YEE, Nathan K. , ZHANG, Li , ZHANG, Yongda
发明人： DESROSIERS, Jean-Nicolas , FANDRICK, Daniel Robert , HADDAD, Nizar , LI, Guisheng , PATEL, Nitinchandra D. , QU, Bo , RODRIGUEZ, Sonia , SENANAYAKE, Chris Hugh , SIEBER, Joshua Daniel , TAN, Zhulin , WANG, Xiao-Jun , YEE, Nathan K. , ZHANG, Li , ZHANG, Yongda
IPC分类号： C07F9/6568 , C07B53/00 , C07F15/00
摘要： This invention relates to novel phosphorous ligands useful for organic transformations. Methods of making and using the ligands in organic synthesis are described. The invention also relates to processes for preparing the novel ligands

7. 发明申请

WO2018106746A2 NOVEL CHIRAL DIHYDROBENZOOXAPHOSPHOLE LIGANDS AND SYNTHESIS THEREOF 审中-公开
公开(公告)号：WO2018106746A2
公开(公告)日：2018-06-14
申请号：PCT/US2017/064797
申请日：2017-12-06
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , DESROSIERS, Jean-Nicolas , FANDRICK, Daniel Robert , HADDAD, Nizar , LI, Guisheng , PATEL, Nitinchandra D. , QU, Bo , RODRIGUEZ, Sonia , SENANAYAKE, Chris Hugh , SIEBER, Joshua Daniel , TAN, Zhulin , WANG, Xiao-Jun , YEE, Nathan K. , ZHANG, Li , ZHANG, Yongda
发明人： DESROSIERS, Jean-Nicolas , FANDRICK, Daniel Robert , HADDAD, Nizar , LI, Guisheng , PATEL, Nitinchandra D. , QU, Bo , RODRIGUEZ, Sonia , SENANAYAKE, Chris Hugh , SIEBER, Joshua Daniel , TAN, Zhulin , WANG, Xiao-Jun , YEE, Nathan K. , ZHANG, Li , ZHANG, Yongda
IPC分类号： C07F9/6568 , C07B53/00 , C07F15/00
摘要： This invention relates to novel phosphorous ligands useful for organic transformations. Methods of making and using the ligands in organic synthesis are described. The invention also relates to processes for preparing the novel ligands

8. 发明申请

WO2010141332A2 STEREOSELECTIVE SYNTHESIS OF CERTAIN TRIFLUOROMETHYL-SUBSTITUTED ALCOHOLS 审中-公开
标题翻译：某些三氟甲磺酸取代醇的立体选择性合成
公开(公告)号：WO2010141332A2
公开(公告)日：2010-12-09
申请号：PCT/US2010036502
申请日：2010-05-28
申请人： BOEHRINGER INGELHEIM INT , FANDRICK DANIEL ROBERT , KUZMICH DANIEL , REEVES JONATHAN TIMOTHY , SONG JINHUA J , TAN ZHULIN , LEE THOMAS
发明人： FANDRICK DANIEL ROBERT , KUZMICH DANIEL , REEVES JONATHAN TIMOTHY , SONG JINHUA J , TAN ZHULIN , LEE THOMAS
IPC分类号： C07D303/08
CPC分类号： C07D301/02 , C07B2200/07 , C07D303/08
摘要： A process for stereoselective synthesis of a compound of Formula (X) or Formula (X') : wherein: R1 is an aryl group substituted with one to three substituent groups, wherein each substituent group of R1 is independently C1-C5 alkyl, C2-C5 alkenyl, C2- C5 alkynyl, C1-C5 alkoxy, C1-C5 alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, C1-C5 alkoxycarbonylamino, aminosulfonyl, C1-C5 alkylaminosulfonyl, C1-C5 dialkylaminosulfonyl, halogen, hydroxy, carboxy, cyano, trifluoromethyl, trifluoromethoxy, nitro, or C1-C5 alkylthio wherein the sulfur atom is oxidized to sulfoxide or sulfone, and R2 and R3 are each independently hydrogen or C1-C5 alkyl.
摘要翻译：一种用于立体选择性合成式（X）或式（X'）的化合物的方法：其中：R1是被一至三个取代基取代的芳基，其中R1的每个取代基独立地为C 1 -C 5烷基， C5链烯基，C2-C5炔基，C1-C5烷氧基，C1-C5烷氧基羰基，氨基羰基，烷基氨基羰基，二烷基氨基羰基，C1-C5烷氧基羰基氨基，氨基磺酰基，C1-C5烷基氨基磺酰基，C1-C5二烷基氨基磺酰基，卤素，羟基，羧基，氰基，，三氟甲氧基，硝基或C 1 -C 5烷硫基，其中硫原子被氧化为亚砜或砜，R2和R3各自独立地为氢或C1-C5烷基。

9. 发明申请

WO2011149822A1 2-OXO-1,2-DIHYDROPYRIDIN-4-YLBORONIC ACID DERIVATIVES 审中-公开
标题翻译： 2-氧代-1,2-二氢吡啶-4-基硼酸衍生物
公开(公告)号：WO2011149822A1
公开(公告)日：2011-12-01
申请号：PCT/US2011/037525
申请日：2011-05-23
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , TAN, Zhulin
发明人： TAN, Zhulin
IPC分类号： C07F5/02
CPC分类号： C07F5/025 , C07D413/10
摘要： The present invention relates to a compound of formula (I) wherein R 1 , R 2 and n are as defined herein. The invention also relates to processes for making the compounds of formula (I) and methods of using the compounds of formula (I) as reagents in organic synthesis.
摘要翻译：本发明涉及其中R 1，R 2和n如本文所定义的式（I）化合物。本发明还涉及制备式（I）化合物的方法和使用式（I）化合物作为有机合成中的试剂的方法。

10. 发明申请

WO2010036632A1 AZAINDAZOLE COMPOUNDS AS CCR1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为CCR1受体拮抗剂的AZAINDAZOLE化合物
公开(公告)号：WO2010036632A1
公开(公告)日：2010-04-01
申请号：PCT/US2009/057778
申请日：2009-09-22
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , COOK, Brian Nicholas , DISALVO, Darren , FANDRICK, Daniel Robert , HARCKEN, Christian , KUZMICH, Daniel , LEE, Thomas Wai-Ho , LIU, Pingrong , LORD, John , MAO, Can , NEU, Jochen , RAUDENBUSH, Brian Christopher , RAZAVI, Hossein , REEVES, Jonathan Timothy , SONG, Jinhua, J. , SWINAMER, Alan, David , TAN, Zhulin
发明人： COOK, Brian Nicholas , DISALVO, Darren , FANDRICK, Daniel Robert , HARCKEN, Christian , KUZMICH, Daniel , LEE, Thomas Wai-Ho , LIU, Pingrong , LORD, John , MAO, Can , NEU, Jochen , RAUDENBUSH, Brian Christopher , RAZAVI, Hossein , REEVES, Jonathan Timothy , SONG, Jinhua, J. , SWINAMER, Alan, David , TAN, Zhulin
IPC分类号： C07D471/04 , A61K31/4375 , A61P29/00
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.
摘要翻译：公开了式（I）化合物，其可用于治疗通过包括自身免疫疾病如类风湿性关节炎和多发性硬化的CCR1的活性介导或维持的多种疾病和病症。还公开了制备方法及其使用方法。

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