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51. 发明授权

US08536208B2 Antifungal composition 有权
标题翻译：抗真菌组合物
公开(公告)号：US08536208B2
公开(公告)日：2013-09-17
申请号：US12674048
申请日：2008-08-20
申请人： Christian Bucher , Günter Ditzinger , Estelle Dubois , Delphine Marchaud
发明人： Christian Bucher , Günter Ditzinger , Estelle Dubois , Delphine Marchaud
IPC分类号： A01N43/78 , A01N55/02 , A01N43/64 , A61K31/41 , A61K31/555
CPC分类号： A61K9/107
摘要： A pharmaceutical composition for oral administration which is self-emulsifying on contact with an aqueous phase, in particular gastrointestinal fluids, and which comprises: (a) an antifungally active compound of formula (I) wherein R1, R2 and R3 are independently of one another hydrogen, F or Cl; or a pharmaceutically acceptable acid addition salt thereof, and (b) a carrier comprising a solubilizer component for the antifungally effective component (a).
摘要翻译：一种用于口服给药的药物组合物，其与水相特别是胃肠液接触时自乳化，并且其包含：（a）式（I）的抗真菌活性化合物，其中R 1，R 2和R 3彼此独立地氢，F或Cl; 或其药学上可接受的酸加成盐，和（b）包含抗真菌有效成分（a）的增溶剂组分的载体。

52. 发明授权

US08486996B2 Aroylfuranes and aroylthiophenes 有权
标题翻译：芳酰基呋喃和芳酰基噻吩
公开(公告)号：US08486996B2
公开(公告)日：2013-07-16
申请号：US11433511
申请日：2006-05-12
申请人： Martin Eberle , Felix Bachmann , Alessandro Strebel , Subho Roy , Goutam Saha , Subir Kumar Sadhukhan , Rohit Saxena , Sudhir Srivastava
发明人： Martin Eberle , Felix Bachmann , Alessandro Strebel , Subho Roy , Goutam Saha , Subir Kumar Sadhukhan , Rohit Saxena , Sudhir Srivastava
IPC分类号： A61K31/34 , C07D307/87
CPC分类号： C07D213/85
摘要： The invention relates to novel substituted 2-(phenyl-, pyridyl- or pyrimidyl-carbonyl)-furanes and -thiophenes and related phenoxy/phenylthio-acetophenones and corresponding heterocyclic compounds, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of neoplastic diseases and autoimmune diseases, and a method for the treatment of such a diseases.
摘要翻译：本发明涉及新的取代的2-（苯基 - ，吡啶基或嘧啶基 - 羰基） - 呋喃和 - 噻吩和相关的苯氧基/苯硫基 - 苯乙酮及其相应的杂环化合物，其制备方法，含有它们的药物组合物，其用途任选地与一种或多种用于治疗肿瘤性疾病和自身免疫疾病的其它药学活性化合物组合，以及治疗这种疾病的方法。

53. 发明申请

US20120277174A1 NEW MACROLIDES AND THEIR USE 有权
标题翻译：新的MACROLIDES及其使用
公开(公告)号：US20120277174A1
公开(公告)日：2012-11-01
申请号：US13389394
申请日：2010-08-13
申请人： Johannes Laurenz Kellenberger , Jürg Dreier
发明人： Johannes Laurenz Kellenberger , Jürg Dreier
IPC分类号： A61K31/706 , A61P29/00 , A61P37/08 , A61P35/00 , A61P11/06 , A61P19/02 , A61P17/00 , A61P1/00 , C07H17/08 , A61P11/00
CPC分类号： C07D498/04 , C07H17/08
摘要： The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with antiinflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.
摘要翻译：本发明涉及式（I）的大环内酯类化合物，所述化合物作为药物的用途，特别是用于治疗或预防炎症和过敏性疾病，含有所述化合物的药物组合物及其制备方法。本发明特别涉及主要通过抑制磷酸二酯酶4（PDE4）介导的具有抗炎活性的大环内酯类化合物，其使它们可用于治疗和/或预防炎性和过敏性疾病如慢性阻塞性肺疾病（COPD），哮喘，类风湿关节炎，特应性皮炎或炎症性肠病或增殖性疾病如癌症。

54. 发明申请

US20120264792A1 FURAZANOBENZIMIDAZOLES AS PRODRUGS TO TREAT NEOPLASTIC OR AUTOIMMUNE DISEASES 有权
标题翻译：作为PROPRUGS治疗神经性或自身免疫性疾病的FURAZANOBENZIMIDAZOLES
公开(公告)号：US20120264792A1
公开(公告)日：2012-10-18
申请号：US13384467
申请日：2010-07-26
申请人： Jens Pohlmann , Felix Bachmann
发明人： Jens Pohlmann , Felix Bachmann
IPC分类号： A61K31/4245 , A61P37/06 , A61P37/00 , C07D413/04 , A61P35/00
CPC分类号： C07D413/04
摘要： A compound of formula (II) wherein represents a divalent benzene residue which is unsubstituted or substituted by one or two additional substituents independently selected from lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, mono(lower alkyl)amino, di(lower alkyl)amino, mono(lower alkenyl)amino, di(lower alkenyl)amino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halogen, and nitro; or wherein two adjacent substituents can be methylenedioxy; or a divalent pyridine residue (Z=N) which is unsubstituted or substituted additionally by lower alkyl, lower alkoxy, lower alkoxy-lower alkoxy, amino, optionally substituted by one or two substituents selected from lower alkyl, lower alkenyl and alkylcarbonyl, halo-lower alkyl, lower alkoxy-lower alkyl, or halogen; R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; and R2 represents a group selected from: or pharmaceutically acceptable salts thereof.
摘要翻译：式（II）的化合物，其表示未取代的或被一个或两个独立地选自低级烷基，卤代低级烷基，羟基 - 低级烷基，低级烷氧基 - 低级烷基，酰氧基 - 低级烷基苯基，羟基，低级烷氧基，羟基 - 低级烷氧基，低级烷氧基 - 低级烷氧基，苯基 - 低级烷氧基，低级烷基羰基氧基，氨基，单（低级烷基）氨基，二（低级烷基）氨基，单（低级烯基）氨基，二（低级烯基）氨基，低级烷氧基羰基氨基，低级烷基羰基氨基，取代氨基，其中氮上的两个取代基与氮杂环基，低级烷基羰基，羧基，低级烷氧基羰基，氰基，卤素和硝基形成。或其中两个相邻的取代基可以是亚甲二氧基; 或未经取代或被低级烷基，低级烷氧基，低级烷氧基 - 低级烷氧基取代的二价吡啶残基（Z = N），任选被一个或两个选自低级烷基，低级烯基和烷基羰基，卤代烷基，低级烷基，低级烷氧基 - 低级烷基或卤素; R 1表示氢，低级烷基羰基，羟基 - 低级烷基或氰基 - 低级烷基; 并且R 2表示选自下列的基团：或其药学上可接受的盐。

55. 发明申请

US20110137026A1 Crystalline (6r,7r)-7--3- [(R)-1'-Tert-Butoxycarbonyl-2-Oxo-[1,3']Bipyrrolidinyl-(3e)-Ylidenemethyl]-8-Oxo-5-Thia-1-Aza-Bicyclo[4.2.0] Oct-2-Ene-2-Carboxylic Acid Benzhydryl Ester; Its Manufacture and Use 有权
标题翻译：结晶（6r，7r）-7- 3 - [（R）-1'-叔丁氧羰基-2-氧代 - [1,3']联吡咯烷基 - （3e） - 亚甲基甲基] -8-氧代-5-硫杂 -1-氮杂 - 双环[4.2.0]十二-2-烯-2-羧酸二苯甲酯; 其制造和使用
公开(公告)号：US20110137026A1
公开(公告)日：2011-06-09
申请号：US12937607
申请日：2009-04-14
申请人： Marco Alpegiani , Walter Cabri , Markus Heubes , Davide Longoni , Michael Schleimer
发明人： Marco Alpegiani , Walter Cabri , Markus Heubes , Davide Longoni , Michael Schleimer
IPC分类号： C07D501/60 , C07D501/12
CPC分类号： C07D501/12 , C07D501/54
摘要： A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.
摘要翻译：描述了式（I）化合物的固体DMSO溶剂化物，其是制备广谱抗生素头孢匹双和头孢匹双酸甲酯的有用中间体。

56. 发明授权

US07459561B2 N-substituted carbamoyloxyalkyl-azolium derivatives 有权
标题翻译： N-取代氨基甲酰氧基烷基 - 唑鎓衍生物
公开(公告)号：US07459561B2
公开(公告)日：2008-12-02
申请号：US11504299
申请日：2006-08-15
申请人： Hiroshi Fukuda , Tadakatsu Hayase , Eisaku Mizuguchi , Nobuo Shimma , Jun Ohwada , Nobuhiro Oikawa , Masahiro Sakaitani , Masao Tsukazaki , Isao Umeda
发明人： Hiroshi Fukuda , Tadakatsu Hayase , Eisaku Mizuguchi , Nobuo Shimma , Jun Ohwada , Nobuhiro Oikawa , Masahiro Sakaitani , Masao Tsukazaki , Isao Umeda
IPC分类号： C07D401/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D417/06 , C07D417/14
摘要： N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.
摘要翻译：具有抗真菌活性并可用于治疗真菌疾病的N-取代氨基甲酰氧基烷基 - 唑鎓衍生物。

57. 发明申请

US20080221171A1 Phenylaminopyridines 有权
标题翻译：苯基氨基吡啶
公开(公告)号：US20080221171A1
公开(公告)日：2008-09-11
申请号：US11662047
申请日：2005-09-05
申请人： Martin Eberle , Felix Bachmann , Alessandro Strebel , Subho Roy , Goutam Saha , Godhuli Nandi
发明人： Martin Eberle , Felix Bachmann , Alessandro Strebel , Subho Roy , Goutam Saha , Godhuli Nandi
IPC分类号： A61K31/44 , C07D213/04 , A61P43/00
CPC分类号： C07D213/74 , C07D241/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The invention relates to novel substituted 3-phenylamino-5-(3-aminophenyl)pyridines and corresponding pyrazines of formula (I), wherein A is CH, C-lower alkyl or N, R1 represents C(═O)R9, S(═O)2R10, P(═O)(OR11)2, optionally substituted phenyl or optionally substituted heteroaryl, and the other substituents have the meaning described in the specification, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of neoplastic diseases and autoimmune diseases, and a method for the treatment of such diseases.
摘要翻译：本发明涉及式（I）的新的取代的3-苯基氨基-5-（3-氨基苯基）吡啶和相应的吡嗪，其中A是CH，C-低级烷基或N，R 1表示C （-O）R 9，S（-O）2 R 10，P（-O）（OR 11）其它取代基具有本说明书中描述的含义，其制备方法，含有该取代基的药物组合物，其任选与用于治疗肿瘤性疾病和自身免疫性疾病的一种或多种其它药物活性化合物，以及治疗这些疾病的方法。

58. 发明申请

US20080032962A1 Stabilized Freeze-Dried Formulation for Cephalosporin Derivatives 审中-公开
标题翻译：头孢菌素衍生物的稳定冻干制剂
公开(公告)号：US20080032962A1
公开(公告)日：2008-02-07
申请号：US11667535
申请日：2005-11-10
申请人： Markus Heubes , Wilhelm Scigalla
发明人： Markus Heubes , Wilhelm Scigalla
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04
CPC分类号： A61K9/19 , A61K9/0019 , A61K47/26 , A61K47/32
摘要： The present invention relates to a freeze-dried formulation for cephalosporin derivatives having increased stability, a solution for obtaining and a method for preparing such a formulation, as well as the use of certain compounds for stabilizing cephalosporin derivatives in freeze-dried formulations. The compounds preferably used as stabilizers according to the invention are mannitol, trehalose, and PVP.
摘要翻译：本发明涉及具有增加的稳定性的头孢菌素衍生物的冷冻干燥制剂，用于获得的溶液和制备这种制剂的方法，以及在冷冻干燥制剂中使用某些化合物来稳定头孢菌素衍生物。根据本发明优选用作稳定剂的化合物是甘露醇，海藻糖和PVP。

59. 发明申请

US20070043061A1 Furazanobenzimidazoles 有权
标题翻译：呋喃并苯并咪唑
公开(公告)号：US20070043061A1
公开(公告)日：2007-02-22
申请号：US10557539
申请日：2004-05-19
申请人： Martin Eberle , Felix Bachmann , Alessandro Strebel , Subho Roy , Sudhir Srivastava , Goutham Saha
发明人： Martin Eberle , Felix Bachmann , Alessandro Strebel , Subho Roy , Sudhir Srivastava , Goutham Saha
IPC分类号： A61K31/506 , A61K31/4439 , A61K31/4245 , C07D413/14
CPC分类号： C07D413/04 , C07D413/14
摘要： The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is oxygen, a carbonyl group, an oxime derivative of a carbonyl group or an α,β-unsaturated carbonyl group, and the substituents R1 to R6 have the meanings given in the specification, for use as medicaments, to novel compounds of formula (I), to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.
摘要翻译：本发明涉及式（I）化合物，其中R表示芳基或杂芳基，X为氧，羰基，羰基的肟衍生物或α，β-不饱和羰基，取代基R 1 R 6具有本说明书中给出的用作药物的含义，式（I）的新型化合物，合成这些化合物的方法，包含含有化合物式（I）化合物与式（I）化合物在制备用于治疗肿瘤和自身免疫性疾病的药物组合物中的用途，以及使用式（I）化合物治疗肿瘤和自身免疫性疾病的方法，或含有其的药物组合物。

60. 发明授权

US06872836B2 Process for the manufacture of 3-amino-pyrrolidine derivatives 失效
标题翻译： 3-氨基 - 吡咯烷衍生物的制备方法
公开(公告)号：US06872836B2
公开(公告)日：2005-03-29
申请号：US10629483
申请日：2003-07-29
申请人： Marc Muller , Milan Soukup
发明人： Marc Muller , Milan Soukup
IPC分类号： C07D207/14 , C07D501/14 , C07D207/04
CPC分类号： C07D207/14 , Y02P20/55
摘要： The invention is concerned with a process for the manufacture of 3-amino-pyrrolidine derivatives of the formula wherein R1 signifies hydrogen or an amino protecting group; Z signifies hydrogen or an amino protecting group; and * represents a center of chirality. 3-Amino-pyrrolidine derivatives, especially optically active 3-amino-pyrrolidine derivatives, are intermediates for the production of agrochemicals and of pharmaceutically active substances such as, for example, of vinylpyrrolidinone-cephalosporin derivatives.
摘要翻译：本发明涉及制备式（Ⅳ）的3-氨基 - 吡咯烷衍生物的方法，意指氢或氨基保护基; Z表示氢或氨基保护基; *表示手性中心。 3-氨基 - 吡咯烷衍生物，特别是光学活性3-氨基 - 吡咯烷衍生物，是生产农用化学品和药物活性物质例如乙烯基吡咯烷酮 - 头孢菌素衍生物的中间体。

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