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11. 发明申请

US20130237553A1 MULTICOMPONENT SYSTEM OF RESUVASTATIN CALCIUM SALT AND SORBITOL 有权
标题翻译： RESIVASASTIN CALCUM盐和SORBITOL多功能体系
公开(公告)号：US20130237553A1
公开(公告)日：2013-09-12
申请号：US13574005
申请日：2011-11-21
申请人： Andreas Hafner , Fritz Blatter , Martin Szelagiewicz , Bernd Siebenhaar
发明人： Andreas Hafner , Fritz Blatter , Martin Szelagiewicz , Bernd Siebenhaar
IPC分类号： C07D239/42 , C07C29/00 , C07C31/26
CPC分类号： C07D239/42 , A61K31/505 , A61K47/26 , A61K47/6941 , C07C29/00 , C07C31/26
摘要： A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and sorbitol. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystal-lization behaviour and stability.
摘要翻译：新型固体形式的罗苏伐他汀作为活性成分包含双[（E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基） - 氨基]嘧啶-5-基 ] - （3R，5S）-3,5-二羟基庚-6-烯酸]和山梨糖醇。包含两种组分的晶体和少量的水显示出改进的性能，例如晶体化行为和稳定性。

12. 发明申请

US20120164162A1 METHODS IN CELL CULTURES, AND RELATED INVENTIONS, EMPLOYING CERTAIN ADDITIVES 有权
标题翻译：细胞培养方法和相关发明，使用某些添加剂
公开(公告)号：US20120164162A1
公开(公告)日：2012-06-28
申请号：US13389549
申请日：2010-08-11
申请人： Franz Kaufmann , Trine Hefsgaard Miller , Johannes Flothmann , Beate Winter , Andreas Hafner
发明人： Franz Kaufmann , Trine Hefsgaard Miller , Johannes Flothmann , Beate Winter , Andreas Hafner
IPC分类号： C12P21/00 , C12N9/00 , C12N1/20 , C07K14/575 , A61K39/00 , C07K14/00 , C07K14/555 , C07K14/715 , C07K14/475 , C07H21/00 , C12P19/34 , A61P37/04 , C07K14/525 , C07K14/54 , C12P1/04
CPC分类号： C12N1/38 , C12P21/02
摘要： A method for the manufacture of products by biotechnological methods in bacterial cell culture is disclosed as well as products obtained, the use of certain additives to the media used in the manufacture of said products in bacterial cell culture media, and the use of said additives in reducing the detrimental effects of radicals in the manufacture of the products, as well as aspects related to these invention embodiments. The manufacturing process or method comprises adding one or more radical scavenging and/or antioxidative additive preferably selected from the group consisting of sterically hindered nitroxyls, sterically hindered hydroxylamines, sterically hindered hydroxylamine salt compounds, sterically hindered amino compounds and sterically hindered N-hydrocarbyloxyamines, benzofuranone compounds, as obligatory component(s) to the medium used during biosynthesis.
摘要翻译：公开了通过生物技术在细菌细胞培养中制造产品的方法，以及获得的产品，在细菌细胞培养基中用于制造所述产品的培养基中使用某些添加剂，以及所述添加剂在降低了在制造产品中自由基的有害影响，以及与本发明实施方案相关的方面。制备方法或方法包括加入一种或多种自由基清除和/或抗氧化添加剂，其优选选自空间位阻硝酰基，空间位阻羟胺，空间位阻羟胺盐化合物，空间位阻氨基化合物和空间位阻N-烃氧基胺，苯并呋喃酮作为生物合成过程中使用的培养基的强制性成分。

13. 发明授权

US07402675B2 Process for the synthesis of amine ethers from secondary amino oxides 有权
公开(公告)号：US07402675B2
公开(公告)日：2008-07-22
申请号：US10919776
申请日：2004-08-17
申请人： Andreas Hafner , Hans Jürg Kirner , Franz Schwarzenbach , Paul Adriaan Van Der Schaaf , Peter Nesvadba
发明人： Andreas Hafner , Hans Jürg Kirner , Franz Schwarzenbach , Paul Adriaan Van Der Schaaf , Peter Nesvadba
IPC分类号： C07D211/54
CPC分类号： C07D401/14 , C04B35/632 , C07D209/44 , C07D211/94 , C07D217/26 , C07D241/08 , C07D401/12 , C07D405/12 , C08K5/3412
摘要： An amine ether of formula A wherein a is 1 or 2; and when a is 1, E is E′; when a is 2, E is L; E′ is C1-C36 alkyl; C3-C18 alkenyl; C2-C18 alkinyl; C5-C18 cycloalkyl; C5-C18 cycloalkenyl; a radical of a saturated or unsaturated aliphatic bicyclic or tricyclic hydrocarbon of 7 to 12 carbon atoms; C2-C7alkyl or C3-C7alkenyl substituted by halogen; C7-C15 aralkyl or C7-C15 aralkyl substituted by C1-C4 alkyl or phenyl; or E′ is a radical of formula (VII) as explained in claim 1; T′ is tertiary C4-C18alkyl or phenyl, each of which are unsubstituted or substituted by halogen, OH, COOR21 or C(O)—R22; or T′ is C5-C12cycloalkyl; C5-C12cycloalkyl which is interrupted by at least one O or —NR18—; a polycyclic alkyl radical having 7-18 carbon atoms, or the same radical which is interrupted by at least one O or —NR18—; or T′ is —C(G1)(G2)-T″; or C1-C18alkyl or C5-C12cycloalkyl substituted by T″ is hydrogen, halogen, NO2, cyano, or is a monovalent organic radical comprising 1-50 carbon atoms; or T″ and T′ together form a divalent organic linking group completing, together with the hindered amine nitrogen atom and the quaternary carbon atom substituted by G1 and G2, an optionally substituted five- or six-membered ring structure; and all other residues are as defined in claim 1, are obtained in good yield from the corresponding N-oxyl hindered amine precursor by reaction with a hydrocarbon E1-H or H-L-H in the presence of an organic hydroperoxide and a catalytic amount of copper or a copper compound. The products of present process find utility as polymerization regulators and/or light stabilizers for organic material.

14. 发明授权

US06900328B2 Process for the synthesis of amine ethers from secondary amino oxides 有权
公开(公告)号：US06900328B2
公开(公告)日：2005-05-31
申请号：US10296107
申请日：2001-05-17
申请人： Andreas Hafner , Hans Jürg Kirner , Franz Schwarzenbach , Paul Adriaan Van Der Schaaf , Peter Nesvadba
发明人： Andreas Hafner , Hans Jürg Kirner , Franz Schwarzenbach , Paul Adriaan Van Der Schaaf , Peter Nesvadba
IPC分类号： B01J27/122 , C07B61/00 , C07D209/44 , C07D211/94 , C07D217/26 , C07D241/08 , C07D401/12 , C07D401/14 , C07D405/12 , C08F4/00 , C08K5/3412 , C08K5/3435 , C08L101/00 , C09K15/30 , C09K21/10 , C07D211/54
CPC分类号： C07D401/14 , C04B35/632 , C07D209/44 , C07D211/94 , C07D217/26 , C07D241/08 , C07D401/12 , C07D405/12 , C08K5/3412
摘要： An amine ether of formula (A) wherein a is 1 or 2; and when a is 1, E is E′; when a is 2, E is L; E′ is C1-C36 alkyl; C3-C18 alkenyl; C2-C18 alkinyl; C5-C18 cycloalkyl; C5-C18 cycloalkenyl; a radical of a saturated or unsaturated aliphatic bicyclic or tricyclic hydrocarbon of 7 to 12 carbon atoms; C2-C7alkyl or C3-C7alkenyl substituted by halogen; C7-C15aralkyl or C7-C15 aralkyl substituted by C1-C4 alkyl or phenyl; or E′ is a radical of formula (VII) as explained in claim 1; T′ is tertiary C4-C18alkyl or phenyl, each of which are unsubstituted or substituted by halogen, OH, COOR21 or C(O)—R22; or T′ is C5-C12cycloalkyl; C5-C12cacloalkyl which is interrupted by at least one O or —NR18—; a polycyclic alkyl radical having 7-18 carbon atoms, or the same radical which is interrupted by at least one O or —NR18—; or T′ is —C(G1)(G2)—T″; or C1-C18alkyl or C5-C12cycloalkyl substituted by F(I)T″ is hydrogen, halogen, NO2, cyano, or is a monovalent organic radical comprising 1-50 carbon atoms; or T″ and T′ together form a divalent organic linking group completing, together with the hindered amine nitrogen atom and the quaternary carbon atom substituted by G1 and G2, an optionally substituted five- or six-membered ring structure; and all other residues are as defined in claim 1, are obtained in good yield from the corresponding N-oxyl hindered amine precursor by reaction with a hydrocarbon E1—H or H—L—H in the presence of an organic hydroperoxide and a catalytic amount of copper or a copper compound. The products of present process find utility as polymerization regulators and/or light stabilizers for organic material

15. 发明授权

US06407190B1 Ruthenium and osmium carbene catalysts 有权
标题翻译：钌和铯卡因催化剂
公开(公告)号：US06407190B1
公开(公告)日：2002-06-18
申请号：US09445909
申请日：1999-12-15
申请人： Paul Adriaan Van Der Schaaf , Andreas Hafner , Andreas Mühlebach
发明人： Paul Adriaan Van Der Schaaf , Andreas Hafner , Andreas Mühlebach
IPC分类号： C08F480
CPC分类号： B01J31/2404 , B01J31/182 , B01J31/2204 , B01J31/2265 , B01J31/24 , B01J2231/14 , B01J2231/543 , B01J2531/821 , B01J2531/825 , C07F15/002 , C07F15/0046 , C08G61/02
摘要： The invention relates to penta- and hexacoordinated ruthenium and osmium carbene catalysts, in which a sulfur, oxygen or nitrogen atom is attached to the carbene group which is coordinated with the central ruthenium or osmium atom, to their preparation and to their use for synthesizing polymers, for ring-closing metathesis of olefins and for isomerizing olefins.
摘要翻译：本发明涉及五价和六配位的钌和锇卡宾催化剂，其中硫，氧或氮原子连接至与中心钌或锇原子配位的卡宾基团，其制备及其用于合成聚合物，用于烯烃的闭合复分解和异构化烯烃。

16. 发明授权

US06281307B1 Polymerizable composition, process for producing cross linked polymers, and cross-linkable polymers 失效
标题翻译：可聚合组合物，交联聚合物的生产方法和可交联聚合物
公开(公告)号：US06281307B1
公开(公告)日：2001-08-28
申请号：US08875529
申请日：1997-07-31
申请人： Andreas Mühlebach , Andreas Hafner , Paul Adriaan Van Der Schaaf
发明人： Andreas Mühlebach , Andreas Hafner , Paul Adriaan Van Der Schaaf
IPC分类号： C08F480
CPC分类号： C08G18/6204 , B33Y70/00 , C08G61/00
摘要： Composition comprising (a) catalytic amounts of a one-component catalyst for metathesis polymerization and (b) at least one polymer with strained cycloalkenylene radicals bonded in the polymer backbone, alone or as a mixture with strained cycloolefins. The composition can be polymerized thermally or photochemically by metathesis polymerization and is suitable for the production of shaped articles, coatings and relief images. The catalyst is selected from Ruthenium and Osmium compounds.
摘要翻译：组合物，其包含（a）催化量的用于复分解聚合的单组分催化剂和（b）至少一种具有结合在聚合物主链中的应变亚链烯基的聚合物，单独或作为与应变环烯烃的混合物。组合物可以通过复分解聚合进行热或光化学聚合，并且适用于生产成形制品，涂层和浮雕图像。催化剂选自钌和锇化合物。

17. 发明授权

US6077805A Hexacoordinated ruthenium or osmium carbene catalysts 失效
标题翻译：六配位的钌或镉卡因催化剂
公开(公告)号：US6077805A
公开(公告)日：2000-06-20
申请号：US33265
申请日：1998-03-02
申请人： Paul Adriaan Van Der Schaaf , Andreas Hafner , Andreas Muhlebach
发明人： Paul Adriaan Van Der Schaaf , Andreas Hafner , Andreas Muhlebach
IPC分类号： B01J31/22 , B01J31/24 , C07F15/00 , C08G61/02 , C08G61/08 , B01J31/00 , C07D231/00 , C07D233/00 , C07F17/02
CPC分类号： B01J31/1815 , B01J31/181 , B01J31/183 , B01J31/2265 , B01J31/24 , B01J31/2404 , C07F15/002 , C07F15/0046 , C08G61/02 , B01J2231/14 , B01J2231/543 , B01J2531/821 , B01J2531/825
摘要： Hexacoordinated ruthenium and osmium catalysts of the formulae ##STR1## in which M and M' independently of one another are ruthenium or osmium;X, X', Y and Y' independently of one another are anionic ligands, or X and Y and X' and Y' in each case together are bis-anionic ligandsL.sup.1 and L.sup.1' independently of one another are tertiary phosphine;L.sup.2 and L.sup.3 independently of one another are a monodentate ligand, or L.sup.2 and L.sup.3 together are bidentate, neutral electron donor ligands;L.sup.4 is tetradentate, neutral electron donor ligand;L.sup.5 is a bidentate, neutral electron donor ligand; andT and T' indepedently of one another are H or organic substituents, are useful for the synthesis of custom-tailored polymers and for the ring-closing metathesis of olefins.
摘要翻译：其中M和M'彼此独立的下式的六配位钌和锇催化剂是钌或锇; X，X'，Y和Y'彼此独立的是阴离子配体，或者X和Y以及X'和Y'各自在一起是双阴离子配体，L1和L1'彼此独立地是叔膦; L2和L3彼此独立是单齿配体，或L2和L3一起是双齿中性电子给体配体; L4是四齿中性电子给体配体; L5是二齿中性电子给体配体; 且T和T'彼此独立地是H或有机取代基，可用于合成定制聚合物和烯烃的闭环复分解。

18. 发明授权

US5342929A Process for the preparation of glycosides 失效
标题翻译：糖苷的制备方法
公开(公告)号：US5342929A
公开(公告)日：1994-08-30
申请号：US937818
申请日：1992-08-31
申请人： Beat Ernst , Michael Heneghan , Andreas Hafner
发明人： Beat Ernst , Michael Heneghan , Andreas Hafner
IPC分类号： B01J31/02 , B01J31/18 , B01J31/24 , C07B61/00 , C07H15/04 , C07H15/10 , C07H15/18 , C07H15/203 , C07H17/00
CPC分类号： C07H15/04 , C07H15/10 , C07H15/18 , C07H15/203
摘要： The invention relates to a process for the preparation of glycosides by reacting protected sugars carrying an anomeric hydroxyl group with an aglycon selected from the group consisting of alcohol, thiol and a protected sugar carrying a non-anomeric hydroxyl group, in an inert solvent, in the preferred temperature range from -20.degree. to +250.degree. C., in the presence of catalytic amounts of metal complex salts. The glycosides are obtained in high yield. Often an excess of the .alpha.- or .beta.-form is obtained and even the pure .alpha.- oder .beta.-forms are obtainable.
摘要翻译：本发明涉及一种制备糖苷的方法，该方法通过在惰性溶剂中，将惰性羟基的保护的糖与选自醇，硫醇和携带非端基异构羟基的被保护的糖的糖苷配基反应，优选的温度范围为-20℃至+ 250℃，在催化量的金属络合盐存在下进行。以高产率获得糖苷。通常可以获得过量的α或β形式，甚至可以获得纯的α-β形式。

19. 发明授权

US5002334A Vehicle roof 失效
标题翻译：车顶
公开(公告)号：US5002334A
公开(公告)日：1991-03-26
申请号：US349826
申请日：1989-05-10
申请人： Klaus Meiler , Hans Jardin , Andreas Hafner
发明人： Klaus Meiler , Hans Jardin , Andreas Hafner
IPC分类号： B60J7/00 , B60J7/08
CPC分类号： B60J7/003
摘要： Vehicle roof having a cover which, in a closed position, covers a roof opening in a fixed roof surface, and which can be extended above a fixed roof surface by pivotal movement about a pivotal axis which extends between its lateral edges. Below the cover, a cover liner is provided which, during upward extension of the cover, is bent about a center axis which is parallel to the pivotal axis of the cover. The liner, in a transversely extending center area, is provided with at least one cutout that extends transversely across a main portion of the liner and which reaches downwardly from the upper side of the liner, through a portion of the thickness of the liner sufficient to create a flexible hinge-like portion, thus permitting the liner to bend when the cover is extended. When the liner is in its unbent condition, the cutout has a cross-sectional shape that widens upwardly.
摘要翻译：具有盖的车顶，其处于关闭位置，覆盖固定屋顶表面中的屋顶开口，并且可以通过围绕其侧向边缘之间延伸的枢转轴线的枢转运动而在固定的屋顶表面上方延伸。在盖的下面，提供一种盖衬套，其在盖的向上延伸期间围绕平行于盖的枢转轴线的中心轴弯曲。衬里在横向延伸的中心区域中设置有至少一个切口，其横向延伸穿过衬套的主要部分并且从衬套的上侧向下延伸穿过衬垫的厚度的一部分，足以至产生柔性的铰链状部分，从而允许衬套在盖延长时弯曲。当衬垫处于其未弯曲状态时，切口具有向上变宽的横截面形状。

20. 发明申请

US20110268792A1 SURFACE ACTIVE PROTEINS AS EXCIPIENTS IN SOLID PHARMACEUTICAL FORMULATIONS 有权
标题翻译：表面活性蛋白作为固体药物制剂的优点
公开(公告)号：US20110268792A1
公开(公告)日：2011-11-03
申请号：US13130128
申请日：2009-11-13
申请人： Andreas Buthe , Andreas Hafner , Franz Kaufmann , Esther Gabor , Guido Meurer , Jürgen Eck , Gordon Bradley
发明人： Andreas Buthe , Andreas Hafner , Franz Kaufmann , Esther Gabor , Guido Meurer , Jürgen Eck , Gordon Bradley
IPC分类号： A61K9/48 , A61P39/00 , A61K9/16 , A61K9/02 , A61K9/00 , A61K9/38
CPC分类号： A61K9/4891 , A61K9/0065 , A61K9/2063 , A61K9/2095 , A61K9/2873 , C07K14/37
摘要： The invention relates to a use of surface active hydrophobins for applications in pharmaceutical technology, in particular as excipients for galenic use. Provided is a method for either admixture of hydrophobins to galenic compositions or for treating the surface of pharmaceutical forms with a hydrophobin-containing solution to modify the pharmaceutical properties of the galenic form. In a preferred embodiment of the invention hydrophobins are used to improve the properties of a pharmaceutical composition, e.g. to act as a surfactant or to increase resistance to disintegration of the galenic forms to achieve a retarded drug release. The galenic form to be modified by the use of surface active proteins as excipients can be capsules, tablets, pills, microparticles, vesicles, and suppositories, although further galenic forms are envisioned. The surface active proteins used for the purpose of present invention can either be isolated from their respective natural source or prepared by recombinant techniques and expression in a suitable host.
摘要翻译：本发明涉及用于制药技术中的表面活性疏水蛋白的用途，特别是作为涂覆液使用的赋形剂。提供了将疏水蛋白与盖仑组合物混合或用含疏水蛋白的溶液处理药物形式的表面以改变盖仑膜形式的药物性质的方法。在本发明的优选实施方案中，疏水蛋白用于改善药物组合物的性质，例如，作为表面活性剂或增加耐受霜冻形式的崩解以实现延缓药物释放。通过使用表面活性蛋白质作为赋形剂来修饰的盖仑形式可以是胶囊，片剂，丸剂，微粒，囊泡和栓剂，尽管可以预见到更多的盖仑制剂形式。用于本发明目的的表面活性蛋白质可以从它们各自的天然来源中分离或者通过重组技术制备并在合适的宿主中表达。

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