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1. 发明专利

JP2000154156A CHIRAL DIPHENYLDIPHOSPHINES AND ITS D-8 METAL COMPLEX 失效
公开(公告)号：JP2000154156A
公开(公告)日：2000-06-06
申请号：JP32898399
申请日：1999-11-19
申请人： SOLVIAS AG
发明人： PUGIN BENOIT , STEINER IVO , AUFDENBLATTEN RHONY NIKLAUS , TOGNI ANTONIO
IPC分类号： B01J31/24 , C07B53/00 , C07B61/00 , C07C25/18 , C07C33/46 , C07C39/367 , C07C43/225 , C07C211/52 , C07F9/50 , C07F9/655 , C07F9/6568 , C07F9/6596 , C07F15/00
摘要： PROBLEM TO BE SOLVED: To obtain a new diphenyl derivative readily separable from a reaction mixture and reusable, useful as an enantiomer selective hydrogenation catalyst, etc. SOLUTION: This compound is shown by formula I (R1 is chloromethyl, bromomethyl or iodomethyl; R2 is a 1-4C alkyl, a 1-4C alkoxy or the like; R3 is Br, I or NH2), formula II (R4 is hydroxymethyl, aminomethyl or the like; R5 is R4, a 1-4C alkyl or the like) of formula III [R6 and R7 are each a secondary phosphino group; R8 is CH2-OH, CH2-O-NH2 or the like; R9 is R8, a 1-4C alkyl or the like; R8 and R9 are bonded to form HOCH(CH2-O-)2, H2NCH(CH2- O-)2 or the like] such as hydroxymethyldiphenyl diiodide. The compound of formula I is obtained, for example, by reacting (R)-[6,6'-dimethyldiphen-2,2'- diyl]bisiodide with N-bromosuccinimide in carbon tetrachloride in the presence of α,α'-azoisobutyronitrile.

2. 发明专利

JP2011116766A New compound and use thereof 审中-公开
标题翻译：新化合物及其用途
公开(公告)号：JP2011116766A
公开(公告)日：2011-06-16
申请号：JP2011037116
申请日：2011-02-23
申请人： Destiny Pharma Ltd , Solvias Ag , ソルビアスアーゲー , デスティニーファーマリミテッド
发明人： BRUNDISH DEREK , FENG XIANGDONG , LOVE WILLIAM , RHYS-WILLIAMS WILLIAM , PUGIN BENOIT
IPC分类号： C07D487/22 , A61K31/409 , A61P19/02 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , A61P31/22 , A61P33/02 , A61P33/04 , A61P33/06 , A61P33/10 , A61P33/12
CPC分类号： C07D487/22
摘要： PROBLEM TO BE SOLVED: To solve such problems that the utility of known porphyrin-based photodynamic therapy agents is limited due to their toxicity against mammalian host tissue cells, that is, the compounds are unable to differentiate between target microbial cells and host cells and in addition, the utility of the above therapy agents is further limited by their relatively low potency for target microbial cells.
SOLUTION: There are disclosed a compound of formula I (respective symbols have meanings given in the description) and metallated forms useful for the treatment of medical conditions for which a photodynamic compound is indicated. There are also disclosed pharmaceutical formulations and methods for treatment of a medical condition for which a photodynamic agent is indicated. Sterilizing solutions comprising a compound of the invention, and the use thereof are also disclosed.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：为了解决已知的卟啉基光动力治疗剂由于其对哺乳动物宿主组织细胞的毒性而受到限制的问题，即化合物不能区分目标微生物细胞和宿主此外，上述治疗剂的效用进一步受到其对靶微生物细胞的相对低效力的限制。解决方案：公开了式I化合物（各符号在说明书中给出的含义）和用于治疗其中指示光动力化合物的医疗条件的金属化形式。还公开了用于治疗指示光动力学药剂的医疗状况的药物制剂和方法。还公开了包含本发明化合物的灭菌溶液及其用途。版权所有（C）2011，JPO＆INPIT

3. 发明申请

WO2007017522A9 FERROCENE-DIPHOSPHINE LIGANDS 审中-公开
标题翻译：糠醛 - 双胍配体
公开(公告)号：WO2007017522A9
公开(公告)日：2008-02-07
申请号：PCT/EP2006065196
申请日：2006-08-10
申请人： SOLVIAS AG , WEISSENSTEINER WALTER , WANG YAPING , SPINDLER FELIX , PUGIN BENOIT , FENG XIANGDONG
发明人： WEISSENSTEINER WALTER , WANG YAPING , SPINDLER FELIX , PUGIN BENOIT , FENG XIANGDONG
IPC分类号： C07F17/02 , B01J31/00 , C07B31/00 , C07F19/00
CPC分类号： C07F17/02
摘要： Compounds of the formula (I) in the form of racemates, mixtures of stereoisomers or optically pure stereoisomers, formula (I), where X 1 and X 2 are each, independently of one another, a secondary phosphino group; R 1 is a halogen atom or a substituent bound via a C atom, N atom, S atom, Si atom, a P(O) group or a P(S) group to the cyclopentadienyl ring; R 2 is C 1 -C 4 -alkyl or phenyl; m is from 1 to 3 and n is 0 or from 1 to 5, are ligands for complexes of transition metals as enantioselective and homogeneous catalysts. As a result of the substitution, the conversion, the stereoselectivity and/or the configuration of the adduct formed can be influenced and optimization of catalysts can be made possible in this way.
摘要翻译：外消旋物形式的式（I）化合物，立体异构体的混合物或光学纯立体异构体式（I），其中X 1和X 2各自独立地为一个二次膦基; R 1是通过C原子，N原子，S原子，Si原子，P（O）基或P（S）键连接到环戊二烯基环上的卤素原子或取代基; R 2是C 1 -C 4 - 烷基或苯基; m为1至3，n为0或1至5，为过渡金属络合物作为对映选择性和均相催化剂的配体。作为取代的结果，可以影响形成的加合物的转化率，立体选择性和/或构型，并且可以以这种方式使催化剂的优化成为可能。

4. 发明申请

WO2006114438A2 MULTIPLY SUBSTITUTED FERROCENES 审中-公开
标题翻译：多取代二茂铁
公开(公告)号：WO2006114438A2
公开(公告)日：2006-11-02
申请号：PCT/EP2006061861
申请日：2006-04-27
申请人： SOLVIAS AG , PUGIN BENOIT , FENG XIANGDONG
发明人： PUGIN BENOIT , FENG XIANGDONG
IPC分类号： C07F17/02
CPC分类号： C07F17/02
摘要： Disclosed are compounds of formulas (I) and (II) in the form of enantiomer-pure diastereomers o diastereomer mixtures. In said formulas (I) and (II), R' 1 represents C 1 -C 4 alkyl while n represents 0 or an integer from 1 to 5; R 1 represents a hydrogen atom, a hydrocarbon radical with 1 to 20 C atoms, secondary phosphino, a mercaptan radical with 1 to 20 C atoms in the hydrocarbon radical, or a silyl radical with 3 C 1 -C 12 hydrocarbon radicals; R 2 is the monovalent radical of an electrophilic organic compound; X 1 represents F, Cl, Br, or I; and Y represents vinyl, methyl, ethyl, -CH 2 -N(C 1 -C 4 -alkyl) 2 , -CH 2 -OR wherein R is a hydrocarbon radical, or a C-bonded, S-bonded, or P-bonded chiral group that directs metals of metallization reagents into the ortho position X 1 . The inventive compounds are coordinating ligands for metal complexes of transition metals as homogeneous catalysts for coupling reactions and intermediate products for producing bidentate ligands.
摘要翻译：式（I）和（II）化合物对映体纯非对映体的形式或者非对映体，其中R“_{1 C _{1 -C _{4 烷基，n是0或代表1〜5的整数; [R _{1 代表氢原子，具有1至20个碳原子，仲膦基，具有在烃1至20个碳原子的硫醇，或具有图3C _{1 甲硅烷基的烃基 -C _{12 表示烃基; [R _{2 是一价基团的亲电有机化合物的; X _{1 是F，Cl，Br或I; 和Y是乙烯基，甲基，乙基，-CH _{2 N（C _{1 -C _{4 烷基）_{2 ，-CH _{2 -OR，其中R是烃基，或C，S或在邻位金属化X的P-结合金属_{1 引导手性基团表示koordinerende是过渡金属作为用于偶联反应和中间体双齿配体的制备均相催化剂的金属配合物的配体。}}}}}}}}}}}}}}

5. 发明申请

WO2004089920A3 AMINE-SUBSTITUTED DIPHENYLDIPHOSPHINES AND THE USE THEREOF IN METAL COMPLEXES FOR ASYMMETRIC ADDITION REACTIONS 审中-公开
标题翻译：氨基取代的二苯基二苯膦及其在不对称合成金属配合物中的应用
公开(公告)号：WO2004089920A3
公开(公告)日：2005-03-17
申请号：PCT/EP2004050439
申请日：2004-04-05
申请人： SOLVIAS AG , PUGIN BENOIT , MARTIN PIERRE , MUELLER MARKUS , NAUD FREDERIC , SPINDLER FELIX , THOMMEN MARC , MELONE GIANPIETRO , KESSELGRUBER MARTIN
发明人： PUGIN BENOIT , MARTIN PIERRE , MUELLER MARKUS , NAUD FREDERIC , SPINDLER FELIX , THOMMEN MARC , MELONE GIANPIETRO , KESSELGRUBER MARTIN
IPC分类号： B01J31/18 , B01J31/24 , C07B53/00 , C07D265/36 , C07F9/50 , C07F9/653 , C07F9/6533 , C07F15/00
CPC分类号： C07B53/00 , B01J31/1865 , B01J31/1875 , B01J31/2409 , B01J2231/323 , B01J2231/44 , B01J2231/643 , B01J2531/80 , B01J2531/821 , B01J2531/822 , B01J2531/827 , C07D265/36 , C07F9/5027 , C07F9/65324 , C07F9/65335 , C07F15/0033 , C07F15/004 , C07F15/0073 , C07F15/008
摘要： The invention relates to the 1,1'-diphenyl-2,2'-diphosphines of formulae (Ia), (Ib), having at least one amine substituent in para position to the phosphine group. These novel compounds are ligands for metal complexes that are catalysts for asymmetric addition reactions of prochiral organic compounds and whose catalytic properties can be adjusted in a substrate-specific manner via the substitution of the amino group.
摘要翻译： 1,1'-二苯基-2,2'-二膦具有在对位上的至少一个胺取代基具有下式的用于金属配合物的配体通过胺基的取代作为催化剂前手性有机化合物的不对称加成反应，以及它们的催化性能的膦基团可以专门针对基材进行调整。

6. 发明申请

WO2004089920A8 AMINE-SUBSTITUTED DIPHENYLDIPHOSPHINES AND THE USE THEREOF IN METAL COMPLEXES FOR ASYMMETRIC SYNTHESES 审中-公开
标题翻译：阿明 - 取代diphenyldiphosphines及它们在金属络合物不对称合成
公开(公告)号：WO2004089920A8
公开(公告)日：2005-05-26
申请号：PCT/EP2004050439
申请日：2004-04-05
申请人： SOLVIAS AG , PUGIN BENOIT , MARTIN PIERRE , MUELLER MARKUS , NAUD FREDERIC , SPINDLER FELIX , THOMMEN MARC , MELONE GIANPIETRO , KESSELGRUBER MARTIN
发明人： PUGIN BENOIT , MARTIN PIERRE , MUELLER MARKUS , NAUD FREDERIC , SPINDLER FELIX , THOMMEN MARC , MELONE GIANPIETRO , KESSELGRUBER MARTIN
IPC分类号： B01J31/18 , B01J31/24 , C07B53/00 , C07D265/36 , C07F9/50 , C07F9/653 , C07F9/6533 , C07F15/00
CPC分类号： C07B53/00 , B01J31/1865 , B01J31/1875 , B01J31/2409 , B01J2231/323 , B01J2231/44 , B01J2231/643 , B01J2531/80 , B01J2531/821 , B01J2531/822 , B01J2531/827 , C07D265/36 , C07F9/5027 , C07F9/65324 , C07F9/65335 , C07F15/0033 , C07F15/004 , C07F15/0073 , C07F15/008
摘要： The invention relates to the 1,1'-diphenyl-2,2'-diphosphines of formulae (Ia), (Ib), having at least one amine substituent in para position to the phosphine group. These novel compounds are ligands for metal complexes that are catalysts for asymmetric addition reactions of prochiral organic compounds and whose catalytic properties can be adjusted in a substrate-specific manner via the substitution of the amino group.
摘要翻译： 1,1'-二苯基-2,2'-二膦具有在对位上的至少一个胺取代基具有下式的用于金属配合物的配体通过胺基的取代作为催化剂前手性有机化合物的不对称加成反应，以及它们的催化性能的膦基团可以具体调整到基材上。

7. 发明申请

WO2005056566A3 METHOD FOR PRODUCING ORTHOMETALATED AND ORTHOSUBSTITUTED AROMATIC COMPOUNDS 审中-公开
标题翻译：制备邻位和正位芳香族化合物的方法
公开(公告)号：WO2005056566A3
公开(公告)日：2005-12-01
申请号：PCT/EP2004053388
申请日：2004-12-10
申请人： SOLVIAS AG , PFALTZ ANDREAS , LOTZ MATTHIAS , SCHOENLEBER MARC , PUGIN BENOIT , KESSELGRUBER MARTIN , THOMMEN MARC
发明人： PFALTZ ANDREAS , LOTZ MATTHIAS , SCHOENLEBER MARC , PUGIN BENOIT , KESSELGRUBER MARTIN , THOMMEN MARC
IPC分类号： C07F9/48 , C07F9/6584 , C07F17/02
CPC分类号： C07F9/65848 , C07F17/02
摘要： The invention relates to compounds having a structural element of formula (I) in an aromatic hydrocarbon ring, wherein: M represents -Li, -MgX3, (C1-C18-Alkyl)3Sn-, -ZnX3 or -B(O-C1-C4-Alkyl)2; X1 and X2, independent of one another, represent O or N, and C-bound hydrocarbon radicals or heterohydrocarbon radicals are bound to the free bonds of the O and N atoms; group -C=C-, together with C atoms, forms a hydrocarbon aromatic compound and represents X3 Cl, Br or I. The inventive compounds are easily obtained by directly substituting the hydrogen in the ortho position to the P atom with metalation reagents. The metal atoms can then be substituted by a reactive electrophilic compound. The group -P(X1-)(X2-)----(BH3)0,1 can then be converted into a secondary phosphine group. The inventive method enables the production of monophosphines and diphosphines even on a large scale, which are valuable ligands for metal complexes serving as catalysts for, e.g. enantioselective hydrogenations.
摘要翻译：具有式（I）的结构元件的化合物中的芳香族烃环，其中M是Li，-MgX3，（C1-C18烷基）3Sn-，-ZnX3或-B（O-C1-C4-烷基）2， X1和X2独立地是O或N-均值和C连接的烃基或杂烃基结合到O和N原子的自由键，形成基团-C = C-的碳一起原子的烃基芳族化合物，和 X3代表Cl，Br或I，通过用金属化试剂将邻位的氢直接取代至P原子而容易地获得。金属原子可以被活性亲电子化合物取代。然后可以将-P（X1-）（X2-） - （BH3）0.1基团转化为仲膦基团。与单 - 和二膦也可以在更大的范围是对于金属配合物作为催化剂用于对映选择性氢化有价值的配体产生的，例如该过程。

8. 发明申请

WO2004056828A2 NOVEL COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：新化合物及其用途
公开(公告)号：WO2004056828A2
公开(公告)日：2004-07-08
申请号：PCT/GB0305649
申请日：2003-12-23
申请人： DESTINY PHARMA LTD , SOLVIAS AG , BRUNDISH DEREK , FENG XIANG DONG , LOVE WILLIAM , RHYS-WILLIAMS WILLIAM , PUGIN BENOIT
发明人： BRUNDISH DEREK , FENG XIANG DONG , LOVE WILLIAM , RHYS-WILLIAMS WILLIAM , PUGIN BENOIT
IPC分类号： A61P19/02 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , A61P31/22 , A61P33/02 , A61P33/04 , A61P33/06 , A61P33/10 , A61P33/12 , C07D487/22 , C07D487/00
CPC分类号： C07D487/22
摘要： A compound of formula (I): wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4 and Z have meanings given in the description, and metallated forms of such compounds, which are useful in the treatment of medical conditions for which a photodynamic compound is indicated. Pharmaceutical formulations and methods of treatment of a medical condition for which a photodynamic agent is indicated are also disclosed. Sterilising solutions comprising a compound of the invention, and the use thereof, are also disclosed.
摘要翻译：式（I）化合物：其中X 1，X 2，X 3，X 4，Y 1，Y 2，Y 3，Y 4和Z具有说明书中给出的含义，以及这些化合物的金属化形式，其可用于治疗其中指出了光动力化合物。还公开了药物制剂和治疗其中指示有光动力药物的医学病症的方法。还公开了包含本发明化合物的灭菌溶液及其用途。

9. 发明专利

CA2653150C CHIRAL LIGANDS USED IN TRANSITION METAL CATALYSTS FOR ASYMMETRIC ADDITION REACTIONS ESPECIALLY HYDROGENATION 未知
公开(公告)号：CA2653150C
公开(公告)日：2014-05-13
申请号：CA2653150
申请日：2007-05-23
申请人： SOLVIAS AG
发明人： PFALTZ ANDREAS , RIBOURDOUILLE YANN , FENG XIANGDONG , RAMALINGAM BALAMURUGAN , PUGIN BENOIT , SPINDLER FELIX
IPC分类号： C07F9/46 , C07C51/36 , C07C67/28 , C07C67/283 , C07C213/02 , C07C221/00 , C07F15/00 , C07F17/02
摘要： The invention provides a compound of the formula l having at least two chiral centres in the form of mixtures of diastereomers or pure diastereomers, wherein formula l is: secondary phosphine-Q-P*(=O)HR1 in which secondary phosphine is a secondary phosphine group with hydrocarbon radicals or heterohydrocarbon radicals as substituents. The compound of formula l may be used in preparing a metal complex with a transition metal, and the metal complex may be used as a catalyst in preparing a chiral organic compound by asymmetric addition of hydrogen to a carbon or carbon-heteroatom double bond in a prochiral organic compound.

10. 发明专利

AT530557T 未知
公开(公告)号：AT530557T
公开(公告)日：2011-11-15
申请号：AT07765731
申请日：2007-06-29
申请人： SOLVIAS AG
发明人： PUGIN BENOIT , FENG XIANGDONG , SPINDLER FELIX
IPC分类号： C07F17/00 , B01J31/00 , C07B31/00 , C07B53/00

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