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11. 发明公开

EP2193116A2 PROCESS FROM SHIKIMIC ACID TO OSELTAMIVIR PHOSPHATE 有权
标题翻译：鳗鱼UR UR UM AT AT AT AT AT AT AT AT AT AT AT AT
公开(公告)号：EP2193116A2
公开(公告)日：2010-06-09
申请号：EP08803807.0
申请日：2008-09-08
申请人： F. Hoffmann-La Roche AG
发明人： TRUSSARDI, René
IPC分类号： C07C227/28 , C07C229/48
CPC分类号： C07C227/04 , C07C229/48 , C07C247/14 , C07C303/28 , C07C303/30 , C07C2601/16 , C07F9/2466 , C07F9/564 , C07C309/66
摘要： The present invention relates to a process for the preparation of a 4,5-diamino shikimic acid derivative of formula I and pharmaceutically acceptable addition salts thereof wherein R1, R1' are independent of each other H or alkyl, R2 is an alkyl and R3, R4 are independent of each other H or an alkanoyl, with the proviso that not both R3 and R4 are H. 4,5-diamino shikimic acid derivatives of formula I, especially the (3R,4R,5S)-5- amino-4-acetylamino-3-( l-ethyl-propoxy)-cyclohex-l-ene-carboxylic acid ethyl ester and its pharmaceutically acceptable additional salts are potent inhibitors of viral neuraminidase.
摘要翻译：本发明提供了通过中间磷酰胺VII将莽草酸转化为奥司他韦（I）和任选地转化成酸加成盐的新方法。

12. 发明公开

EP1778252A2 NONCARDIOTOXIC PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译： NICHTKARDIOTOXISCHE药物化合物
公开(公告)号：EP1778252A2
公开(公告)日：2007-05-02
申请号：EP05786819.2
申请日：2005-08-09
申请人： Barbeau, Donald L.
发明人： Barbeau, Donald L.
IPC分类号： A61K31/675 , C07F9/59
CPC分类号： C07F9/2458 , C07F9/2462 , C07F9/2466 , C07F9/247 , C07F9/2475 , C07F9/5532 , C07F9/5535 , C07F9/5728 , C07F9/588 , C07F9/591 , C07F9/65061 , C07F9/650958 , C07F9/6533 , C07F9/6547 , C07F9/65517 , C07F9/65527 , C07F9/655345 , C07F9/65583 , C07F9/65586 , C07F9/6561
摘要： The present invention relates to novel noncardiotoxic compounds and pharmaceutical compositions useful in the treatment of a variety of disorders including the treatment of depression, allergies, psychoses, cancer and gastrointestinal disorders. In particular, the present invention describes pharmaceutical compositions that mitigate life-threatening arrhythmias such as torsade de pointes. Torsade de pointes is a particular cardiac problem associated with many therapeutic agents and has been implicated as a possible cause of sudden death, particularly in those individuals with a past history of disturbances of cardiac rhythm, myocardial infarction, congenital repolarization abnormalities and cardiac risk factors such as hyperlipidemia and age. This arrhythmia is a variant of paroxysmal ventricular tachycardia associated with a prolonged QTc interval or prominent U waves on the ECG. Torsade de pointes is potentially lethal because it can progress to ventricular fibrillation, life-threatening arrhythmias or precipitate sudden death.

13. 发明公开

EP0165507A2 Phosphoric triamides and polymers thereof as dopants 失效
标题翻译：磷酸三酰胺和Polymere daraus als Dotiermittel。
公开(公告)号：EP0165507A2
公开(公告)日：1985-12-27
申请号：EP85106490.7
申请日：1985-05-25
申请人： ALLIED CORPORATION
发明人： Anello, Louis Gene c/o Allied Corporation , Kirtley, Stephen Wakefield c/o Allied Corporation , Harnish, Daniel Franklin c/o Allied Corporation
IPC分类号： C08L85/02 , H01L21/312 , H01L21/225
CPC分类号： H01L21/02118 , C07F9/224 , C07F9/2466 , C07F9/591 , C07F9/6587 , C07F9/659 , C08G79/02 , C08L85/02 , H01L21/02282 , H01L21/02337 , H01L21/2225 , H01L21/2254 , H01L21/312
摘要： Phosphorus triamides or their polymers are described as phosphorus dopants adapted to be spun-on to a semiconductor substrate and used in integrated circuit manufacture. Sheet resistivities of 4 to 13 ohms per square are obtained at low weight loadings in 1 hour, 1000°C diffusions.
The polymer (or monomers), are homogeneous and soluble and are easily distributed uniformly on the semicon- ` ductor surface, such as by the spin-on method; are relatively non-volatile so that when the solvent is removed and the material heated to diffusion temperatures, the desired film will be substantially intact; and are capable of being rendered insoluble, i.e. crosslinked thermally or otherwise, and are characterized as glassy rather than crystalline.
The polymeric solution may be employed in the manufacture of semiconductor components and, as such, the solution may be spun-on silicon wafers to function as a phosphorus impurity source (dopant) in thermal diffusions. Such doped wafers are then used in integrated circuit manufacture.
摘要翻译：磷三酰胺或其聚合物被描述为适于旋涂到半导体衬底上并用于集成电路制造中的磷掺杂剂。在1小时，1000℃扩散的低重量载荷下获得4至13欧姆/平方的片电阻率。聚合物（或单体）是均匀和可溶的，并且容易地均匀地分布在半导体表面上，例如通过旋涂法; 是相对不挥发的，因此当除去溶剂并将材料加热至扩散温度时，所需的膜将基本上完整; 并且能够变得不溶，即热交联或以其它方式交联，并且被表征为玻璃状而不是结晶。聚合物溶液可以用于制造半导体组件，因此，溶液可以是旋转硅晶片，以在热扩散中用作磷杂质源（掺杂剂）。然后将这样的掺杂晶片用于集成电路制造。

14. 发明公开

EP0105415A1 Cyclopropyl-methyl-(thio)-phosphorsäureamide, Verfahren zu ihrer Herstellung und ihre Verwendung zur Bekämpfung von Schädlingen 有权
标题翻译：环丙基甲基（硫代）-phosphorsäureamide，它们的制备方法及其在防治害虫中的用途。
公开(公告)号：EP0105415A1
公开(公告)日：1984-04-18
申请号：EP83109424.8
申请日：1983-09-22
申请人： BASF Aktiengesellschaft
发明人： Buerstinghaus, Rainer, Dr. , Kiehs, Karl, Dr. , Adolphi, Heinrich, Dr.
IPC分类号： C07F9/24 , A01N57/26
CPC分类号： C07F9/242 , A01N57/30 , C07F9/2466 , C07F9/26
摘要： Cyclopropyl-methyl-(thio)-phosphorsäureamid der Formel
in der

R 1 , R 2 , R 3 , R 4 , R 5 und X die in Ansprüchen und Beschreibung angegebene Bedeutung haben, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel.
摘要翻译：环丙基甲基式其中R 1，R 2，R 3，R <4>，R <5>和X的含义在权利要求和说明书所示的（硫代）-phosphorsäureamid，它们的制备和它们的用途作为农药。

15. 发明公开

EP3277380A4 DNA ALKYLATING AGENTS 有权转让
公开(公告)号：EP3277380A4
公开(公告)日：2018-08-01
申请号：EP16762438
申请日：2016-03-09
申请人： THRESHOLD PHARMACEUTICALS INC , OBI PHARMA INC
发明人： DUAN JIAN-XIN , CAO YEYU , CAI XIAOHONG , JIAO HAILONG , MA JING YUAN , MATTEUCCI MARK
IPC分类号： A61P35/00 , A61K31/04 , A61K31/06 , A61K31/664 , C07F9/24 , G01N33/574
CPC分类号： C07F9/2466 , G01N33/57484 , G01N33/57496 , G01N2333/904 , G01N2800/52
摘要： Provided herein are compounds of formula I: wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds.

16. 发明公开

EP1745056A2 ENANTIOSELECTIVE PHOSPHORAMIDITE COMPOUNDS AND CATALYSTS 审中-公开
标题翻译：对流式亚磷酸盐化合物及催化剂
公开(公告)号：EP1745056A2
公开(公告)日：2007-01-24
申请号：EP05778948.9
申请日：2005-04-29
申请人： Yale University Corporation
发明人： HARTWIG, John, F. , LEITNER, Andreas , SHU, Chutian
IPC分类号： C07F9/22 , B01J31/18
CPC分类号： C07D295/023 , B01J31/186 , B01J2231/348 , B01J2231/44 , B01J2231/645 , B01J2531/16 , B01J2531/17 , B01J2531/64 , B01J2531/66 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2531/827 , B01J2531/828 , B01J2531/847 , C07B53/00 , C07C209/60 , C07C213/08 , C07C319/20 , C07F9/2466 , C07F9/657154 , C07C211/28 , C07C211/45 , C07C217/58 , C07C323/36
摘要： This invention relates to phosphoramidite compounds and catalyst complexes which can be used to provide enantioselective reactions including hydroamination reactions, etherification reactions and conjugate addition reactions and allylic substitution reactions, among others. In a first aspect, the present invention is directed to phosphoramidite and related compounds according to general structure (I), where Z is absent or is a group containing O, N or S, preferably O; R1 and R2 are independently an optionally substituted C1-12 alkyl group, an optionally substituted (CH2)n-aromatic group or (CH2)n-heteroaromatic group, or are linked together to form an optionally substituted aliphatic or (CH2)n-aromatic dianion of a diol, diamine, dithiol, aminoalcohol, aminohiolate or a alcoholthiol group; R3’ and R3 are each independently H, an optionally substituted C1-C12 alkyl group or an optionally substituted (CH2)n-aromatic group with the proviso that R3’ and R3 are not both H, or together R3’ and R3 form an optionally substituted C5-C15 saturated or unsaturated carbocyclic ring; R4 is H, an optionally substituted C1-C12 alkyl group or an optionally substituted (CH2)n-aromatic group; R5 is absent, H, an optionally substituted C1-C12 alkyl group or an optionally substituted (CH2)n-aromatic or (CH2)n-heteroaromatic group; Ra and Ra’ are each independently H or a C1-C3 alkyl group, or Ra and Ra’ together with the carbon to which they are attached form a optionally substituted C5-C15 saturated or unsaturated carbocyclic or heterocyclic ring, or an aromatic or heteroaromatic ring; R6 and R7 are each independently H, an optionally substituted C1-C12 alkyl group or an optionally substituted (CH2)n-aromatic group, with the proviso that R5, R6 and R7 cannot simultaneously be H, and when Ra and Ra’, together with the carbon to which they are attached, form a carbocyclic ring, heterocyclic ring or an aromatic or heteroaromatic ring, R5 is absent or is preferably H; R6 and R7 are preferably H or CH3; and each n is independently 0, 1, 2, 3, 4, 5 or 6 and wherein at least one of the carbon atoms attached to the nitrogen of the phosphoramidite group is a chiral center.
摘要翻译：本发明涉及可用于提供对映选择性反应的亚磷酰胺化合物和催化剂配合物，包括加氢胺化反应，醚化反应和共轭加成反应以及烯丙基取代反应等。在第一方面，本发明涉及根据通用结构（I）的亚磷酰胺和相关化合物，其中Z不存在或是含有O，N或S，优选O的基团; R 1和R 2独立地为任选取代的C 1-12烷基，任选取代的（CH 2）n - 芳族基团或（CH 2）n - 杂芳族基团，或者连接在一起形成任选取代的脂族或（CH 2）n - 芳族二醇，二胺，二硫醇，氨基醇，氨基硫醇盐或醇硫醇基的二价阴离子; R 3'和R 3各自独立地为H，任选取代的C 1 -C 12烷基或任选取代的（CH 2）n - 芳基，条件是R 3'和R 3不都是H，或一起R 3' 取代的C5-C15饱和或不饱和碳环; R4为H，任选取代的C1-C12烷基或任选取代的（CH2）n-芳基; R 5不存在，H，任选取代的C 1 -C 12烷基或任选取代的（CH 2）n - 芳族或（CH 2）n - 杂芳族基团; Ra和Ra'各自独立地为H或C1-C3烷基，或者Ra和Ra'与它们所连接的碳一起形成任选取代的C5-C15饱和或不饱和的碳环或杂环，或芳族或杂芳族环; R 6和R 7各自独立地为H，任选取代的C 1 -C 12烷基或任选取代的（CH 2）n - 芳族基团，条件是R 5，R 6和R 7不能同时为H，并且当Ra和Ra' 与它们所连接的碳形成碳环，杂环或芳族或杂芳族环，R5不存在或优选为H; R6和R7优选为H或CH3; 并且每个n独立地为0,1,2,3,4,5或6，并且其中连接到亚磷酰胺基团的氮上的至少一个碳原子是手性中心。

17. 发明公开

EP1521736A1 FABRICATION DE NITRILES A PARTIR DE COMPOSES A INSATURATION ETHYLENIQUE 有权转让
标题翻译： HERSTELLUNG VON NITRILEN AUS ETHYLENISCHUNGESÄTTIGTENVERBINDUNGEN
公开(公告)号：EP1521736A1
公开(公告)日：2005-04-13
申请号：EP03748206.4
申请日：2003-07-11
申请人： Rhodia Polyamide Intermediates
发明人： GALLAND, Jean-Christophe , DIDILLON, Blaise , MARION, Philippe , BOURGEOIS, Damien
IPC分类号： C07C253/10 , C07F9/145 , C07F9/58 , C07F9/655 , C07F9/141 , C07F9/24 , C07F9/6571 , C07F9/6574
CPC分类号： C07F9/2479 , C07C253/10 , C07C253/30 , C07F9/1415 , C07F9/145 , C07F9/2466 , C07F9/2475 , C07F9/585 , C07F9/65517 , C07F9/657154 , C07F9/65746 , C07C255/04 , C07C255/07
摘要： The invention concerns a method for hydrocyanation of ethylenically unsaturated organic compounds into compounds comprising at least one nitrile function. It concerns particularly hydrocyanation of diolefins such as butadiene or substituted olefins such as alkenenitriles like pentenenitriles. The method is characterized in that the reaction is carried out in the presence of a metal complex catalyst comprising a transition metal such as nickel and an organic ligand.
摘要翻译：本发明涉及一种将烯属不饱和有机化合物氢化成含有至少一个腈官能团的化合物的方法。它更具体地涉及二烯烃如丁二烯或取代的烯烃如亚烯腈，例如戊烯腈的氢氰化。根据本发明的方法，反应在含有过渡金属如镍和有机配体的金属络合物催化剂的存在下进行。

18. 发明公开

EP0096993A2 Phosphoramidothionate, and their production and use 失效
标题翻译： Phosphoramidothionate und ihre Herstellung und Verwendung。
公开(公告)号：EP0096993A2
公开(公告)日：1983-12-28
申请号：EP83303056.2
申请日：1983-05-26
申请人： SUMITOMO CHEMICAL COMPANY, LIMITED
发明人： Kohsaka, Hideo , Sasaki, Mitsuru , Ishiguri, Yukio
IPC分类号： C07F9/24 , A01N57/26
CPC分类号： C07F9/2462 , A01N57/30 , A01N57/32 , C07F9/242 , C07F9/2458 , C07F9/2466 , C07F9/65517 , C07F9/65586
摘要： A compound of the formula:
wherein R, is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkylnyl group, a lower cycloalkyl group, a lower cycloalkyl(lower)alkyl group, a halo(lower)-alkyl group, a lower alkoxy(lower)alkyl group, a di(lower)-alkoxy(lower)alkyl group, a cyano(lower)alkyl group, a lower alkylthio(lower)alkyl group, a lower alkynylthio(lower)alkyl group, a lower dioxothiacycloalkyl group, a lower thiacycloalkyl group, a lower oxacycloalkyl group, a lower oxacycloalkyl(lower)alkyl group or a thienyl(lower)alkyl group, R 2 is a lower alkyl group and R 3 is a 3,5-dimethoxyphenyl group, a 3,4-methylenedioxyphenyl group or a 4,5-methylenedioxy-2-nitrophenyl group, which is useful as a fungicide.
摘要翻译：下式的化合物：其中R 1是氢原子，低级烷基，低级烯基，低级炔基，低级环烷基，低级环烷基（低级）烷基，卤素（低级）烷基，低级烷氧基（低级）烷基，低级烷氧基（低级）烷基，低级烷氧基（低级）烷基，低级烷氧基（低级）低级二氧代硫代环烷基，低级硫杂环烷基，低级环氧烷基，低级环氧烷基（低级）烷基或噻吩基（低级）烷基，R2为低级烷基，R3为3,5-二甲氧基苯基， 3,4-亚甲二氧基苯基或4,5-亚甲基二硅氧基-2-硝基苯基，其可用作杀真菌剂。

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