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41. 发明授权

US5047557A Complexes having optically active ligands, a process for their preparation and their use 失效
标题翻译：具有光学活性配体的配合物，其制备方法及其应用
公开(公告)号：US5047557A
公开(公告)日：1991-09-10
申请号：US481416
申请日：1990-02-16
申请人： Andreas Hafner , Rudolf Duthaler , Guido Bold
发明人： Andreas Hafner , Rudolf Duthaler , Guido Bold
IPC分类号： C07B41/02 , C07B43/04 , C07B53/00 , C07C29/14 , C07C29/143 , C07C33/025 , C07C33/22 , C07C33/30 , C07C209/24 , C07C269/00 , C07C271/22 , C07D317/20 , C07D407/14 , C07F7/00 , C07F7/28 , C07F9/6596
CPC分类号： C07D407/14 , C07D317/20 , C07F7/00 , C07F7/006
摘要： Compounds of the formula I ##STR1## in which Me is Ti, Zr or Hf, R.sub.1 is a group transferable to aldehyde, keto or imine groups, for example methyl, allyl, vinyl or the radical of an enol or enamine, R.sub.2 is, for example, cyclopentadienyl, R.sub.3 and R.sub.4 are, for example, H or alkyl, R.sub.5 is, for example, phenyl and the C(1) and C(2) atoms are chiral and have predominantly one configuration, are suitable for use as chiral reactants for aldehydes, ketones and imines for the preparation of both enantiomers of secondary or tertiary alcohols or tertiary amines.
摘要翻译：其中Me为Ti，Zr或Hf的式I（I）化合物，R1为可转移到醛，酮或亚胺基团的基团，例如甲基，烯丙基，乙烯基或烯醇或烯胺的基团， R2是例如环戊二烯基，R 3和R 4是例如H或烷基，R 5是例如苯基，C（1）和C（2）原子是手性的并且主要具有一个构型，适用于用作醛，酮和亚胺的手性反应物，用于制备仲醇或叔醇或叔胺的两种对映异构体。

42. 发明授权

US09249108B2 Multicomponent system of rosuvastatin calcium salt and sorbitol 有权
标题翻译：罗苏伐他汀钙盐和山梨醇的多组分体系
公开(公告)号：US09249108B2
公开(公告)日：2016-02-02
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 , A61K31/505 , A61K47/26 , A61K47/48
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 crystallization behavior 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，例如结晶行为和稳定性。

43. 发明授权

US08785142B2 Test arrangement 有权
标题翻译：测试安排
公开(公告)号：US08785142B2
公开(公告)日：2014-07-22
申请号：US13577366
申请日：2011-02-09
申请人： Georg Gübitz , Eva Sigl , Andrea Hasmann , Marc Schröder , Konstantin Schneider , Alexandra Rollett , Franz Kaufmann , Andreas Hafner
发明人： Georg Gübitz , Eva Sigl , Andrea Hasmann , Marc Schröder , Konstantin Schneider , Alexandra Rollett , Franz Kaufmann , Andreas Hafner
IPC分类号： G01N33/573
CPC分类号： C12Q1/001 , C12Q1/04
摘要： The invention relates to an arrangement, comprising a solid carrier and a matrix arranged on the solid carrier, said matrix comprising at least one enzymatically convertible or modifiable molecule and comprising at least one enzyme that can be released by the conversion or modification of the molecule, said enzyme being capable of converting at least one color-changing substrate located in the matrix and/or on the solid carrier.
摘要翻译：本发明涉及一种包括固体载体和布置在固体载体上的基质的布置，所述基质包含至少一种可酶促转化或可修饰的分子，并且包含至少一种可通过分子转化或修饰释放的酶，所述酶能够转化位于基质和/或固体载体上的至少一种变色基质。

44. 发明授权

US08758730B2 Compositions, use and method for the use of surface active proteins in topical drug delivery across keratin 有权
标题翻译：组合物，使用和使用表面活性蛋白在角蛋白局部药物递送中的应用
公开(公告)号：US08758730B2
公开(公告)日：2014-06-24
申请号：US13202112
申请日：2010-02-19
申请人： Andreas Buthe , Andreas Hafner , Franz Kaufmann , Babette Fiedler , Guido Meurer , Gordon Bradley
发明人： Andreas Buthe , Andreas Hafner , Franz Kaufmann , Babette Fiedler , Guido Meurer , Gordon Bradley
IPC分类号： A61K47/42 , A61Q3/00
CPC分类号： A61K9/0014 , A61K31/522 , A61K38/02 , A61K45/06 , A61K47/42 , A61K2300/00
摘要： The present invention provides the use of surface active proteins, especially class I and class II hydrophobins, in topically applied pharmaceutical formulations. The invention is particularly directed to topically applied pharmaceutical products for enhancing the penetration to achieve a transungual delivery of a prophylactically and/or therapeutically effective amount of an active ingredient (drug) to a patient (including animals and humans) into and/or through a nail, of the animal or human body, in order to treat one or more of a variety of diseases or disorders. Related embodiments of the invention are also disclosed.
摘要翻译：本发明提供了表面活性蛋白质，特别是I类和II类疏水蛋白在局部施用的药物制剂中的用途。本发明特别涉及用于增强渗透性以实现预防和/或治疗有效量的活性成分（药物）向患者（包括动物和人）递送到和/或通过指甲，动物或人体，以治疗各种疾病或病症中的一种或多种。还公开了本发明的相关实施例。

45. 发明授权

US08716305B2 Multicomponent crystalline system of rosuvastatin calcium salt and vanillin 有权
公开(公告)号：US08716305B2
公开(公告)日：2014-05-06
申请号：US13643579
申请日：2012-04-16
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： A01N43/42 , A61K31/44 , A61K31/505 , C07D239/42
CPC分类号： A61K31/505 , A61K31/11 , A61K47/10 , C07D239/42
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 vanillin or vanillin derivatives. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystallization behavior stability and decreased hydroscopic behavior.

46. 发明授权

US08226967B2 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中的赋形剂
公开(公告)号：US08226967B2
公开(公告)日：2012-07-24
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： A01N25/34 , C07K1/00
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其各自的天然来源分离或通过重组技术制备并在合适的宿主中表达。

47. 发明申请

US20050043552A1 Process for the synthesis of amine ethers from secondary amino oxides 有权
标题翻译：从仲氨基氧化物合成胺醚的方法
公开(公告)号：US20050043552A1
公开(公告)日：2005-02-24
申请号：US10919776
申请日：2004-08-17
申请人： Andreas Hafner , Hans Kirner , Franz Schwarzenbach , Paul Van Der Schaaf , Peter Nesvadba
发明人： Andreas Hafner , Hans Kirner , Franz Schwarzenbach , Paul 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 , C07D303/08 , C07C239/10
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 cydoalkyl; 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-C12 cycloalkyl 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.
摘要翻译：式A的胺醚，其中a为1或2; 当a为1时，E为E'; 当a为2时，E为L; E'是C 1 -C 36烷基; C3-C18烯基; C2-C18炔基; C5-C18环烷基; C5-C18环烯基; 7-12个碳原子的饱和或不饱和脂族二环或三环烃基团; C 2 -C 7烷基或被卤素取代的C 3 -C 7链烯基; 被C 1 -C 4烷基或苯基取代的C 7 -C 15芳烷基或C 7 -C 15芳烷基; 或E'是如权利要求1所述的式（VII）的基团; T'是叔C4-C18烷基或苯基，其各自为未取代的或被卤素，OH，COOR21或C（O）-R22取代; 或T'为C 5 -C 12环烷基; 被至少一个O或-NR 18 - 中断的C 5 -C 12环烷基; 具有7-18个碳原子的多环烷基或被至少一个O或-NR 18 - 中断的相同基团; 或T'为-C（G1）（G2）-T“; 或被T“取代的C 1 -C 18烷基或C 5 -C 12环烷基是氢，卤素，NO 2，氰基，或是包含1-50个碳原子的一价有机基团; 或T“和T'一起形成二价有机连接基团，与受阻胺氮原子和被G1和G2取代的季碳原子一起形成任选取代的五元或六元环结构; 并且所有其它残基如权利要求1中所定义，通过在有机氢过氧化物和催化量的铜或其盐的存在下与烃E1-H或HLH反应，由相应的N-氧基受阻胺前体以良好的产率获得铜化合物。本发明的产品可用作有机材料的聚合调节剂和/或光稳定剂。

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