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1. 发明申请

WO2005080298A1 CATALYTIC ASYMMETRIC SYNTHESIS OF OPTICALLY ACTIVE α-HALO-CARBONYL COMPOUNDS 审中-公开
标题翻译：光催化不对称合成的光催化活性α-羟基碳二亚胺化合物
公开(公告)号：WO2005080298A1
公开(公告)日：2005-09-01
申请号：PCT/DK2005/000094
申请日：2005-02-11
申请人： HALLAND, Nis , JØRGENSEN, Karl Anker , MARIGO, Mauro , BRAUNTON, Alan , BACHMANN, Stephan , FIELENBACH, Doris
发明人： HALLAND, Nis , JØRGENSEN, Karl Anker , MARIGO, Mauro , BRAUNTON, Alan , BACHMANN, Stephan , FIELENBACH, Doris
IPC分类号： C07B39/00
CPC分类号： C07D207/08 , C07B53/00 , C07C45/63 , C07F7/1856 , C07F7/188 , C07C47/14 , C07C47/24 , C07C49/16 , C07C49/463 , C07C47/353 , C07C47/277 , C07C47/17
摘要： A process for the catalytic asymmetric synthesis of an optically active compound of the formula (la) or (lb): wherein R is an organic group; X is halogen; R l and R 2 which may the same or different represents H, or an organic group or R l and R 2 may be bridged together forming part of a ring system; R and R 2 may be bridged together forming part of a ring system; with the provisio that R and R l are different and R 2 , when different from H, is attached though a carbon-carbon bond, comprising the step of reacting a compound of the formula (2): with a halogenation agent in the presence of a catalytic amount of a chiral nitrogen containing organic compound.
摘要翻译：用于催化不对称合成式（Ia）或（Ib）的光学活性化合物的方法：其中R是有机基团; X是卤素; 可以相同或不同的R 1和R 2表示H或有机基团，或者R 1和R 2可以桥连在一起形成环系的一部分; R和R 2可以桥连在一起形成环系的一部分; 条件是R和R1不同，当与H不同时，R2通过碳 - 碳键连接，包括使式（2）化合物与卤化剂在催化剂存在下反应的步骤：量的手性含氮有机化合物。

2. 发明申请

WO2003050105A2 CATALYTIC ASYMMETRIC SYNTHESIS OF OPTICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：光催化不对称合成光活性化合物
公开(公告)号：WO2003050105A2
公开(公告)日：2003-06-19
申请号：PCT/DK2002/000827
申请日：2002-12-09
申请人： CHEMINOVA A/S , HALLAND, Nis , JØRGENSEN, Karl, Anker , HANSEN, Tore
发明人： HALLAND, Nis , JØRGENSEN, Karl, Anker , HANSEN, Tore
IPC分类号： C07D311/00
CPC分类号： C07D311/00
摘要： A one step catalytic asymmetric process for the synthesis of an optically active compound of formula la or lb wherein R is selected from C 1-7 alkyl, C 1-7 haloalkyl, C 1-7 alkoxy, C 1-7 haloalkoxy, halogen and hydroxy; R 3 is H or C 1-4 alkyl; R4 is selected from H, C 1-7 alkyl, C 1-7 haloalkyl, C 1-7 alkoxy, COOH, CO-C 1-7 alkoxy and an optionally substituted aryl or heterocycle; AR represents C 1-7 alkyl, optionally substituted aryl, an optionally substituted heterocycle or AR and R 4 may be bridged together forming part of a ring system; X is O or S; m is a number between 0-4; comprising the step of reacting a compound of the formula 2 with a compound of formula 3 in the presence of a catalytic amount of a chiral nitrogen containing organic compound.
摘要翻译：用于合成式Ia或Ib的光学活性化合物的一步催化不对称方法，其中R选自C 1-7烷基，C 1-7卤代烷基，C 1-7烷氧基，C 1-7卤代烷氧基，卤素和羟基; R3是H或C1-4烷基; R 4选自H，C 1-7烷基，C 1-7卤代烷基，C 1-7烷氧基，COOH，CO-C 1-7烷氧基和任选取代的芳基或杂环; AR表示C1-7烷基，任选取代的芳基，任选取代的杂环或AR和R 4可桥接在一起形成环系的一部分; X是O或S; m是0-4之间的数字; 包括在催化量的手性含氮有机化合物存在下使式2的化合物与式3的化合物反应的步骤。

3. 发明申请

WO2009003590A1 A PROCESS FOR THE PALLADIUM-CATALYZED COUPLING OF TERMINAL ALKYNES WITH HETEROARYL TOSYLATES AND HETEROARYL BENZENESULFONATES 审中-公开
标题翻译：一种具有异氰酸酯和叔丁基苯甲酸酯的末端烷基铜催化偶联的方法
公开(公告)号：WO2009003590A1
公开(公告)日：2009-01-08
申请号：PCT/EP2008/004928
申请日：2008-06-19
申请人： SANOFI-AVENTIS , R'KYEK, Omar , NAZARÈ, Marc , LINDENSCHMIDT, Andreas , ALONSO, Jorge , URMANN, Matthias , HALLAND, Nis
发明人： R'KYEK, Omar , NAZARÈ, Marc , LINDENSCHMIDT, Andreas , ALONSO, Jorge , URMANN, Matthias , HALLAND, Nis
IPC分类号： C07D213/127 , C07D213/26 , C07D213/30 , C07D215/12 , C07D215/14 , C07D231/12 , C07D231/56 , C07D239/26 , C07D333/24 , C07D471/04
CPC分类号： C07D231/12 , C07D213/127 , C07D213/26 , C07D213/30 , C07D215/12 , C07D215/14 , C07D231/56 , C07D239/26 , C07D333/38 , C07D409/06 , C07D471/04
摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), (I) wherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1 -alkynes of the formula I useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
摘要翻译：本发明涉及用于区域选择性合成式（I），（I）的化合物的方法，其中D，J和W具有权利要求中所示的含义。本发明提供了一种有效且通用的钯催化的杂芳基甲苯磺酸酯与末端炔烃的偶联方法，其可用于生产药物，诊断剂，液晶，聚合物的各种具有式I的取代的多官能杂芳基-1-炔炔，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

4. 发明申请

WO2009000411A1 A TRANSITION METAL CATALYZED SYNTHESIS OF 2H-INDAZOLES 审中-公开
标题翻译： 2H-INDAZOLES的过渡金属催化合成
公开(公告)号：WO2009000411A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/004637
申请日：2008-06-11
申请人： SANOFI-AVENTIS , HALLAND, Nis , NAZARÉ, Marc , LINDENSCHMIDT, Andreas , ALONSO, Jorge , R'KYEK, Omar , URMANN, Matthias
发明人： HALLAND, Nis , NAZARÉ, Marc , LINDENSCHMIDT, Andreas , ALONSO, Jorge , R'KYEK, Omar , URMANN, Matthias
IPC分类号： C07D231/56
CPC分类号： C07D231/56
摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4; Q and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional 2H-indazoles or 2H-azaindazoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenylacetylenes and monosubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
摘要翻译：本发明涉及一种用于区域选择性合成式（I）化合物的方法，其中R 0; R1; R2; R3; R4; R5; A1; A2; A3; A4; Q和J具有权利要求中所示的含义。本发明提供了一种直接过渡金属催化的方法，用于从2-卤代 - 苯基乙炔或（2-磺酸基）苯基乙炔和单取代的肼的多种多功能2H-吲唑或式（I）的2H-氮杂吲唑，其可用于生产药物，诊断剂，液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

5. 发明申请

WO2009003589A1 A PROCESS FOR THE PALLADIUM-CATALYZED COUPLING OF TERMINAL ALKYNES WITH ARYL TOSYLATES 审中-公开
标题翻译：一种具有芳基甲酸酯的末端烷基羧酸催化偶联的方法
公开(公告)号：WO2009003589A1
公开(公告)日：2009-01-08
申请号：PCT/EP2008/004927
申请日：2008-06-19
申请人： SANOFI-AVENTIS , R'KYEK, Omar , NAZARÈ, Marc , LINDENSCHMIDT, Andreas , URMANN, Matthias , HALLAND, Nis , ALONSO, Jorge
发明人： R'KYEK, Omar , NAZARÈ, Marc , LINDENSCHMIDT, Andreas , URMANN, Matthias , HALLAND, Nis , ALONSO, Jorge
IPC分类号： C07C17/00 , C07C22/08 , C07C45/61 , C07C49/563 , C07C213/08 , C07C217/08 , C07C231/12 , C07C233/07 , C07C253/30 , C07C255/58 , C07D295/00 , C07D333/20
CPC分类号： C07C17/263 , C07B37/04 , C07C17/35 , C07C41/30 , C07C43/225 , C07C45/61 , C07C45/70 , C07C231/12 , C07C253/30 , C07C2601/16 , C07D295/00 , C07D333/20 , C07C25/24 , C07C49/84 , C07C47/548 , C07C233/07 , C07C233/43 , C07C233/54 , C07C255/33 , C07C255/50 , C07C255/51 , C07C255/53 , C07C255/54 , C07C255/58
摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula (I) useful for the production of intermediates in the preparation for pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
摘要翻译：本发明涉及用于区域选择性合成式（I）化合物的方法，其中R1; R2; R3; R4; R5; J和W具有权利要求中所示的含义。本发明提供了对于具有末端炔烃的芳基甲苯磺酸酯与多种用于制备药物制备中间体的式（I）的取代的多官能芳基-1-炔烃的有效和一般的钯催化偶合方法，诊断剂，液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

6. 发明申请

WO2009000412A1 A REGIOSELECTIVE METAL CATALYZED SYNTHESIS OF ANNELATED BENZIMIDAZOLES AND AZABENZIMIDAZOLES 审中-公开
标题翻译：邻苯二甲酸二甲酯和亚氨基半乳糖的选择性金属催化合成
公开(公告)号：WO2009000412A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/004638
申请日：2008-06-11
申请人： SANOFI AVENTIS , ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARE, Marc , R'KYEN, Omar , URMANN, Mathias , HALLAND, Nis
发明人： ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARE, Marc , R'KYEN, Omar , URMANN, Mathias , HALLAND, Nis
IPC分类号： C07D471/04 , C07D471/14 , C07D487/04 , C07D491/14
CPC分类号： C07D487/04 , C07D471/04 , C07D471/14 , C07D491/14
摘要： A regioselective metal catalyzed synthesis of benzimidazoles and azabenzimidazoles The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N- substituted benzimidazoles or azabenzimidazoles of formula (I) starting from 2-halo- nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
摘要翻译：苯并咪唑和氮杂苯并咪唑的区域选择性金属催化合成本发明涉及用于区域选择性合成式（I）化合物的方法，其中R1; R2; R3; R4; J1; J2; J3; J4和G具有权利要求中所示的含义。本发明提供直接金属，例如，钯或铜，催化的区域选择性方法，用于从用于制备药物，诊断剂，液体的2-卤代 - 硝基芳烃和N-取代的酰胺开始的多种不对称，多官能的式（I）的N-取代的苯并咪唑或氮杂苯并咪唑晶体，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

7. 发明申请

WO2008009348A1 A REGIOSELECTIVE PALLADIUM CATALYZED SYNTHESIS OF BENZIMIDAZOLES AND AZABENZIMIDAZOLES 审中-公开
标题翻译：苯并咪唑和AZABENZIMIDAZOLES的选择性催化合成
公开(公告)号：WO2008009348A1
公开(公告)日：2008-01-24
申请号：PCT/EP2007/005816
申请日：2007-06-30
申请人： SANOFI-AVENTIS , ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARÉ, Marc , HALLAND, Nis , RKYEK, Omar , URMANN, Matthias
发明人： ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARÉ, Marc , HALLAND, Nis , RKYEK, Omar , URMANN, Matthias
IPC分类号： C07D235/10 , C07D235/12 , C07D235/08 , C07D235/02 , C07D487/04
CPC分类号： C07D235/10 , C07D235/08 , C07D235/16 , C07D401/04 , C07D471/04
摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein RO; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N -substituted benzimidazoles or azabenzimidazoles of formula (I) starting from 2-halo-nitroarenes and Λ/-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricitdes and arthropodicides.
摘要翻译：本发明涉及一种用于区域选择性合成式（I）化合物的方法，其中RO; R1; R2; R3; R4; R5; A1; A2; A3; A4，Q和J具有权利要求中所示的含义。本发明提供了直接钯催化的区域选择性方法，其可从用于制备药物的2-卤代 - 硝基芳烃和β-取代的酰胺开始，从多种不对称，多官能的式（I）的N-取代的苯并咪唑或氮杂苯并咪唑开始，诊断剂，液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，螨类和节肢动物杀虫剂。

8. 发明申请

WO2013041119A1 N-[4-(1H-PYRAZOLO[3,4-B]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译： N- [4-（1H-吡唑并[3,4-B]吡嗪-6-基） - 苯基] - 磺酰胺及其作为药物的用途
公开(公告)号：WO2013041119A1
公开(公告)日：2013-03-28
申请号：PCT/EP2011/066220
申请日：2011-09-19
申请人： SANOFI , NAZARÉ, Marc , HALLAND, Nis , SCHMIDT, Friedemann , WEISS, Tilo , DIETZ, Uwe , HOFMEISTER, Armin
发明人： NAZARÉ, Marc , HALLAND, Nis , SCHMIDT, Friedemann , WEISS, Tilo , DIETZ, Uwe , HOFMEISTER, Armin
IPC分类号： C07D487/04 , A61K31/4985 , A61P19/02
CPC分类号： C07D487/04
摘要： The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]- sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式I的N- [4-（1H-吡唑并[3,4-b]吡嗪-6-基） - 苯基]磺酰胺，其中Ar，R 1，R 2和n具有如索赔。式I的化合物是调节蛋白激酶活性，特别是血清和糖皮质激素调节激酶（SGK）的活性，特别是血清和糖皮质激素调节激酶同工型1（SGK-1，SGK1）的活性的有价值的药理学活性化合物，并且是适用于治疗SGK活动不适当的疾病，例如退行性关节疾病或炎性过程如骨关节炎或风湿病。本发明还涉及式I化合物的制备方法，它们作为药物的用途，以及包含它们的药物组合物。

9. 发明申请

WO2009000413A1 A REGIOSELECTIVE COPPER CATALYZED SYNTHESIS OF BENZIMIDAZOLES AND AZABENZIMIDAZOLES 审中-公开
标题翻译：苯并咪唑和氨苄青霉素的选择性铜催化合成
公开(公告)号：WO2009000413A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/004639
申请日：2008-06-11
申请人： SANOFI-AVENTIS , ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARÉ, Marc , URMANN, Matthias , HALLAND, Nis , R'KYEK, Omar
发明人： ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARÉ, Marc , URMANN, Matthias , HALLAND, Nis , R'KYEK, Omar
IPC分类号： C07D235/08 , C07D235/16 , C07D235/18 , C07D401/04 , C07D471/04
CPC分类号： C07D235/08 , C07D235/16 , C07D235/18 , C07D401/04 , C07D471/04
摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4; Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N /-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N /-substituted amides. The process is useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
摘要翻译：本发明涉及一种用于区域选择性合成式（I）化合物的方法，其中R 0; R1; R2; R3; R4; R5; A1; A2; A3; A4; Q和J具有权利要求中所示的含义。本发明为从2-卤代 - 硝基芳烃和N-取代的酰胺开始的多种不对称的，多官能的N-取代的苯并咪唑或式I的氮杂苯并咪唑提供直接铜催化的区域选择性方法。该方法可用于生产药物，诊断剂，液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

10. 发明申请

WO2008125207A1 A TRANSITION METAL CATALYZED SYNTHESIS OF N-AMINOINDOLES 审中-公开
标题翻译： N-AMINOINDOLES的过渡金属催化合成
公开(公告)号：WO2008125207A1
公开(公告)日：2008-10-23
申请号：PCT/EP2008/002519
申请日：2008-03-29
申请人： SANOFI-AVENTIS , HALLAND, Nis , NAZARE, M , LINDENSCHMIDT, Andreas , RKYEK, Omar , URMANN, Matthias , ALONSO, Jorge
发明人： HALLAND, Nis , NAZARE, M , LINDENSCHMIDT, Andreas , RKYEK, Omar , URMANN, Matthias , ALONSO, Jorge
IPC分类号： C07D209/08
CPC分类号： C07D209/08
摘要： The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino- azaindoles of the formula (I) from 2-halo-phenylacetylenes or (2-sulfonato)phenyl- acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
摘要翻译：本发明涉及一种用于区域选择性合成式（I）化合物的方法，其中R 0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4，Q，T和J具有权利要求中所示的含义。本发明提供了从2-卤代苯基乙炔或（2-磺酸基）苯基 - 乙炔和N，N（N）的多种多官能N-氨基吲哚或式（I）的N-氨基 - 可用于制备药物，诊断剂，液晶，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂的二取代肼。

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