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1. 发明申请

US20080139551A1 TUMOR NECROSIS FACTOR ALPHA INHIBITORS AND THEIR USE IN THE TREATMENT OF HUMAN DISEASES 审中-公开
标题翻译：肿瘤坏死因子ALPHA抑制剂及其在治疗人类疾病中的应用
公开(公告)号：US20080139551A1
公开(公告)日：2008-06-12
申请号：US11842144
申请日：2007-08-21
申请人： Jagadish Sircar , Sunil Kumar , Timothy James Davis , Wenbin Ying , Peter Nussbaumer , Andreas Billich
发明人： Jagadish Sircar , Sunil Kumar , Timothy James Davis , Wenbin Ying , Peter Nussbaumer , Andreas Billich
IPC分类号： A61K31/5377 , A61K31/497 , A61P11/06 , A61P5/46 , A61P19/02
CPC分类号： C07D215/46 , C07D401/06 , C07D409/12 , C07D487/08 , C07D491/04 , C07D495/04
摘要： treatment of a variety of disorders, including the treatment of pathological conditions associated with tumor necrosis factor alpha. The inhibitors of tumor necrosis factor alpha have the following structures: including stereoisomers, pharmaceutically acceptable salts, and solvates thereof, wherein substituents are as defined herein. Compositions containing an inhibitor of tumor necrosis factor alpha in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.
摘要翻译：治疗各种疾病，包括治疗与肿瘤坏死因子α相关的病理状况。肿瘤坏死因子α的抑制剂具有以下结构：包括立体异构体，其药学上可接受的盐和溶剂合物，其中取代基如本文所定义。还提供了含有肿瘤坏死因子α与药学上可接受的载体组合的抑制剂的组合物，以及使用它们的方法。

2. 发明申请

US20080318255A1 Fluorescent Labeled Sphingosines 审中-公开
标题翻译：荧光标记鞘氨醇
公开(公告)号：US20080318255A1
公开(公告)日：2008-12-25
申请号：US10573602
申请日：2004-09-28
申请人： Andreas Billich , Peter Ettmayer , Diana Mechtcheriakova , Peter Nussbaumer , Alexander Wlachos
发明人： Andreas Billich , Peter Ettmayer , Diana Mechtcheriakova , Peter Nussbaumer , Alexander Wlachos
IPC分类号： G01N33/573 , C07C215/10 , C07F9/32 , C07D311/80
CPC分类号： C12N9/1205 , C07C219/20 , C07C233/71 , C07C237/08 , C07C237/10 , C07C311/41 , C07C2603/50 , C07D271/12 , C07F9/65324 , C12Q1/42 , C12Q1/485 , G01N2500/02
摘要： The present invention relates to a method (assay) for determining the activity of an enzyme selected from the group consisting of a sphingosine kinase and a phosphatase involved in the sphingolipid pathway by use of a labeled sphingosine.
摘要翻译：本发明涉及通过使用标记的鞘氨醇来测定选自鞘氨醇激酶和参与神经鞘脂途径的磷酸酶的酶的活性的方法（测定）。

3. 发明授权

US06346626B1 Chromanone and thiochromanone compounds 失效
标题翻译：色酮和硫色满酮化合物
公开(公告)号：US06346626B1
公开(公告)日：2002-02-12
申请号：US09680887
申请日：2000-10-06
申请人： Andreas Billich , Peter Nussbaumer , Erwin Schreiner , Ingeborg Schuster
发明人： Andreas Billich , Peter Nussbaumer , Erwin Schreiner , Ingeborg Schuster
IPC分类号： C07D31104
CPC分类号： C07D335/06 , C07D311/22
摘要： The invention concerns the compounds of formula I wherein R1 and R2 independently are hydrogen, acyl, alkoxycarbonyl or alkyl; either the sulfamoyloxy side chain is bound to the 6 position; R3 is alkyl; alkenyl; alkinyl; a cycloalkyl moiety optionally substituted by alkyl, alkoxy or halogen; arylalkenyl; arylalkinyl; acyl; cycloalkylalkyl; 3-oxo-2-oxacamphanyl; or is 6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl; and R4 is hydrogen; alkyl; hydroxy; or alkoxy; or the sulfamoyloxy side chain is bound to the 7 position; R3 has the significance indicated above for R4; and R4 has the significance indicated above for R3; X is O or S; and the symbol - - - is a single or a double bond; in free form or salt form. They can be prepared by sulfamoylation of corresponding hydroxylated compounds, by reduction and/or by N-substitution. They are indicated for use as pharmaceuticals, particularly in the prophylactic or curative treatment of illnesses responsive to steroid sulfatase inhibition.
摘要翻译：本发明涉及式Ⅰ化合物，其中R 1和R 2各自独立地是氢，酰基，烷氧羰基或烷基; 氨磺酰氧基侧链与6位结合; R3是烷基; 烯基; 炔基任选被烷基，烷氧基或卤素取代的环烷基部分; 芳基烯基芳基炔基酰基; 环烷基烷基; 3-氧代-2-氧杂am基; 或是6,6-二甲基双环[3.1.1]庚-2-烯-2-基; 和R 4是氢; 烷基; 羟基; 或烷氧基;或磺酰氧基侧链结合到7位; R3具有上面对R 4表示的含义; 和R 4具有上面对R 3表示的含义; X是O或S; 并且符号 - - 是单键或双键;以游离形式或盐形式。它们可以通过相应的羟基化合物的氨磺酰化，通过还原和/或通过N-取代制备。它们用作药物，特别是在针对类固醇硫酸酯酶抑制作用的疾病的预防或治疗中。

4. 发明授权

US07928093B2 Amino-propanol derivatives 有权
标题翻译：氨基丙醇衍生物
公开(公告)号：US07928093B2
公开(公告)日：2011-04-19
申请号：US11568645
申请日：2005-05-25
申请人： Klaus Hinterding , Klemens Högenauer , Peter Nussbaumer
发明人： Klaus Hinterding , Klemens Högenauer , Peter Nussbaumer
IPC分类号： C07D231/56 , C09B5/00
CPC分类号： C07C217/64 , C07C271/16 , C07F9/094
摘要： A compound of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
摘要翻译：其中R 1，R 2，R 3，R 4和R 5如本说明书中所定义的式（I）化合物，其制备方法，用途，特别是在移植中，以及含有它们的药物组合物。

5. 发明授权

US07825260B2 Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators 有权
标题翻译：氨基丙醇衍生物作为鞘氨醇-1-磷酸受体调节剂
公开(公告)号：US07825260B2
公开(公告)日：2010-11-02
申请号：US10554557
申请日：2004-04-29
申请人： Rainer Albert , Claus Ehrhardt , Peter Ettmayer , Klaus Hinterding , Klemens Högenauer , Peter Nussbaumer
发明人： Rainer Albert , Claus Ehrhardt , Peter Ettmayer , Klaus Hinterding , Klemens Högenauer , Peter Nussbaumer
IPC分类号： C07D231/56 , C07D307/00 , C07D307/87 , C09B5/00
CPC分类号： C07F9/65586 , C07C217/64 , C07C2601/14 , C07D231/56 , C07D263/56 , C07D263/57 , C07D307/79 , C07D413/04 , C07F9/1414 , C07F9/6541
摘要： Compounds of formula I, wherein X, a, b, R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
摘要翻译：式I化合物，其中X，a，b，R 1，R 2，R 3，R 4和R 5如本说明书中所定义，其制备方法及其用途和含有它们的药物组合物。

6. 发明授权

US07122184B2 Specific monoclonal antibody against terbinafine 失效
标题翻译：针对特比萘芬的特异性单克隆抗体
公开(公告)号：US07122184B2
公开(公告)日：2006-10-17
申请号：US10203076
申请日：2001-02-12
申请人： Birgit Dorobek , Peter Nussbaumer
发明人： Birgit Dorobek , Peter Nussbaumer
IPC分类号： A61K39/395
CPC分类号： C07K16/44 , A61K47/643 , A61K47/646
摘要： The invention concerns momoclonal antibodies to terbinafine in free base or salt form, immunogenic conjugates suitable for preparing them, hybridoma capable of producing them, and corresponding assay kits. The antibodies can be prepared by administering to an appropriate animal an immunogenic conjugate of a suitable derivative of terbinafine covalently linked to an immonogen, recovering antibody-producing cells sensitized to the conjugate, immortalizing the antibody-producing cells, selecting a resultant immortalized cell line, and recovering the resultant antibodies therefrom. They are indicated for use in particular in the measurement of terbinafine tissue concentration and distribution in bodily fluids or compartments, especially nails.
摘要翻译：本发明涉及以游离碱或盐形式的特比萘芬的单克隆抗体，适用于制备特异碱的免疫原性缀合物，能产生它们的杂交瘤以及相应的测定试剂盒。抗体可以通过向合适的动物施用与immonogen共价连接的特比萘芬的合适衍生物的免疫原性缀合物，回收对缀合物敏感的产生抗体的细胞，使抗体产生细胞永生化，选择所得到的永生化细胞系，并从中回收得到的抗体。它们特别用于测量特比萘芬组织的浓度和分布在体液或隔室，特别是指甲中。

7. 发明申请

US20060211656A1 Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators 有权
标题翻译：氨基丙醇衍生物作为鞘氨醇-1-磷酸受体调节剂
公开(公告)号：US20060211656A1
公开(公告)日：2006-09-21
申请号：US10554557
申请日：2004-04-29
申请人： Rainer Albert , Claus Ehrhardt , Peter Ettmayer , Klaus Hinterding , Klemens Högenauer , Peter Nussbaumer
发明人： Rainer Albert , Claus Ehrhardt , Peter Ettmayer , Klaus Hinterding , Klemens Högenauer , Peter Nussbaumer
IPC分类号： A61K31/423 , A61K31/416 , A61K31/405 , A61K31/675 , C07D333/66 , C07D263/60 , C07D231/56
CPC分类号： C07F9/65586 , C07C217/64 , C07C2601/14 , C07D231/56 , C07D263/56 , C07D263/57 , C07D307/79 , C07D413/04 , C07F9/1414 , C07F9/6541
摘要： Compounds of formula I, wherein X, a, b, R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
摘要翻译：式I的化合物，其中X，a，b，R 1，R 2，R 3，R 4， >和R 5如本说明书中所定义，其制备方法及其用途和含有它们的药物组合物。

8. 发明申请

US20050059712A1 Acylsulfonamides as inhibitors of steroid sulfatase 失效
标题翻译：酰基磺酰胺作为类固醇硫酸酯酶的抑制剂
公开(公告)号：US20050059712A1
公开(公告)日：2005-03-17
申请号：US10490464
申请日：2002-10-04
申请人： Amarylla Horvath , Philipp Lehr , Peter Nussbaumer , Erwin Schreiner
发明人： Amarylla Horvath , Philipp Lehr , Peter Nussbaumer , Erwin Schreiner
IPC分类号： C07D295/20 , A61K31/381 , A61K31/4245 , A61K31/439 , A61K31/44 , A61K31/445 , A61K31/4535 , A61K31/4545 , A61K31/495 , A61P5/28 , A61P17/08 , A61P17/10 , A61P35/00 , A61P43/00 , C07C311/51 , C07D211/24 , C07D211/34 , C07D211/48 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/70 , C07D211/78 , C07D211/96 , C07D213/71 , C07D221/22 , C07D271/06 , C07D277/38 , C07D333/34 , C07D333/38 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D451/02 , C07D451/10 , C07D451/14 , C07D471/08 , C07D333/22 , A61K31/426 , C07D213/56
CPC分类号： C07D221/22 , C07C311/51 , C07C2601/08 , C07C2601/14 , C07C2602/44 , C07C2603/74 , C07D211/24 , C07D211/34 , C07D211/48 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/70 , C07D211/78 , C07D211/96 , C07D213/71 , C07D271/06 , C07D333/34 , C07D333/38 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D451/02 , C07D451/10 , C07D451/14
摘要： A compound of formula wherein R1 is haloalkyl, alkenyl, phenyl, thienyl, pyridine, benzthiazolyl, chromanyl (1,2-dihydrobenzopyranyl) or (C6-18)aryl, and R1 or R2 independently of each other are substituted (C4-8)cycloalkyl, a substituted bridged cycloalkyl system, substituted piperidine, substituted tetrahydropyridine, or a substituted bridged heterocyclic system, useful as a pharmaceutical.
摘要翻译：下式化合物其中R 1为卤代烷基，烯基，苯基，噻吩基，吡啶，苯并噻唑基，苯并二氢吡喃基（1,2-二氢苯并吡喃基）或（C6-18）芳基，R1或R2彼此独立地为（C4-8）环烷基，取代的桥连环烷基系统，取代的哌啶，取代的四氢吡啶或用作药物的取代的桥连杂环体系。

9. 发明授权

US09453051B2 Cyclosporin derivatives 有权
标题翻译：环孢菌素衍生物
公开(公告)号：US09453051B2
公开(公告)日：2016-09-27
申请号：US14241126
申请日：2012-08-29
申请人： Gunter Fischer , Miroslav Malesevic , Frank Erdmann , Jan Kuhling , Michael Bukrinsky , Stephanie Constant , Gerd Ruhter , Peter Nussbaumer , Klaus Dinkel
发明人： Gunter Fischer , Miroslav Malesevic , Frank Erdmann , Jan Kuhling , Michael Bukrinsky , Stephanie Constant , Gerd Ruhter , Peter Nussbaumer , Klaus Dinkel
IPC分类号： A61K38/12 , C07K7/50 , C07K7/64 , C12N9/90
CPC分类号： C07K7/645 , C12N9/90 , C12Y502/01008
摘要： The present invention relates to novel cyclosporin derivatives that do not cross the cellular membrane. The compounds according to the invention are used in medicine, more particularly in the treatment/diagnosis of acute and chronic inflammatory diseases, viral infections, cancer, degenerative muscle diseases, neurodegenerative diseases and damage that is associated with calcium homeostasis impairment. The novel cyclosporin derivatives additionally have no immunosuppressive effect.
摘要翻译：本发明涉及不与细胞膜交叉的新型环孢菌素衍生物。根据本发明的化合物用于医学中，更特别地用于治疗/诊断急性和慢性炎性疾病，病毒感染，癌症，退行性肌肉疾病，神经变性疾病以及与钙稳态损伤相关的损伤。新型环孢菌素衍生物另外没有免疫抑制作用。

10. 发明授权

US09242937B2 Pharmaceutically active disubstituted pyridine derivatives 有权
标题翻译：药用活性二取代吡啶衍生物
公开(公告)号：US09242937B2
公开(公告)日：2016-01-26
申请号：US14002731
申请日：2012-03-01
申请人： Gerd Rühter , Peter Nussbaumer , Axel Choidas , Carsten Schulz-Fademrecht , Bert Klebl , Jan Eickhoff
发明人： Gerd Rühter , Peter Nussbaumer , Axel Choidas , Carsten Schulz-Fademrecht , Bert Klebl , Jan Eickhoff
IPC分类号： C07D211/72 , C07D213/74 , A61K31/4418 , A61K45/06
CPC分类号： C07D213/74 , A61K31/4418 , A61K45/06
摘要： The present invention relates to disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted pyridine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase.
摘要翻译：本发明涉及二取代的吡啶衍生物和/或其药学上可接受的盐，这些衍生物作为药物活性剂的用途，特别是用于预防和/或治疗感染性疾病，包括机会性疾病，免疫疾病，自身免疫性疾病，心血管疾病，细胞增殖性疾病，炎症，勃起功能障碍和中风，以及含有至少一种所述二取代吡啶衍生物和/或其药学上可接受的盐的药物组合物。此外，本发明涉及所述二取代的吡啶衍生物作为蛋白激酶的抑制剂的用途。

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