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31. 发明授权

US08080541B2 Carbocyclic GlyT-1 receptor antagonists 有权
标题翻译：碳环GlyT-1受体拮抗剂
公开(公告)号：US08080541B2
公开(公告)日：2011-12-20
申请号：US12859305
申请日：2010-08-19
申请人： Sabine Kolczewski , Emmanuel Pinard
发明人： Sabine Kolczewski , Emmanuel Pinard
IPC分类号： A61K31/166 , A61K31/40 , A61K31/5375 , A61K31/397 , A61K31/451 , A61K31/351 , A61K31/382 , C07D207/04 , C07D295/155 , C07D205/04 , C07D211/06 , C07D207/12 , C07D309/14 , C07D335/02 , C07D487/10 , C07D211/74 , C07D211/62 , C07C235/58 , A61P25/28 , A61P25/18 , A61P29/00 , A61P25/00
CPC分类号： A61K31/166 , A61K31/397 , A61K31/40 , A61K31/4453 , A61K31/495 , A61K31/5375 , C07C233/79 , C07C235/62 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/06 , C07D207/10 , C07D207/12 , C07D211/38 , C07D211/46 , C07D295/12 , C07D295/20 , C07D309/14 , C07D335/02 , C07D487/10
摘要： The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
摘要翻译：本发明涉及其中R 1，R 2，R 3，R 4，X和n如本文所定义或其药学上可接受的酸加成盐的式I化合物与外消旋混合物或其相应的对映体和/ 或用于治疗精神病，疼痛，记忆功能障碍和学习，注意力缺陷，精神分裂症，痴呆症或阿尔茨海默病的光学异构体。

32. 发明授权

US08026365B2 4,4-disubstituted piperidine derivatives 失效
标题翻译： 4,4-二取代哌啶衍生物
公开(公告)号：US08026365B2
公开(公告)日：2011-09-27
申请号：US12111230
申请日：2008-04-29
申请人： Andreas Christ , Rainer Martin , Peter Mohr
发明人： Andreas Christ , Rainer Martin , Peter Mohr
IPC分类号： A61K31/438 , C07D471/10
CPC分类号： C07D471/10 , C07D211/66 , C07D401/12
摘要： This invention relates to 4,4-disubstituted piperidine derivatives of the formula wherein A and R1 to R5 are as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
摘要翻译：本发明涉及下式的4,4-二取代哌啶衍生物，其中A和R 1至R 5如说明书中所定义，及其药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。

33. 发明授权

US08026255B2 Substituted piperidines as somatostatin receptor subtype 5 (SSTR5) antagonists 失效
标题翻译：取代的哌啶作为生长抑素受体5型（SSTR5）拮抗剂
公开(公告)号：US08026255B2
公开(公告)日：2011-09-27
申请号：US12776748
申请日：2010-05-10
申请人： Alfred Binggeli , Andreas D. Christ , Hans P. Maerki , Rainer E. Martin
发明人： Alfred Binggeli , Andreas D. Christ , Hans P. Maerki , Rainer E. Martin
IPC分类号： A61K31/445
CPC分类号： C07D211/58 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D471/04
摘要： This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
摘要翻译：本发明涉及下式的化合物及其药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。

34. 发明申请

US20110177067A1 COMBINATION THERAPY OF A TYPE II ANTI-CD20 ANTIBODY WITH INCREASED ANTIBODY DEPENDENT CELLULAR CYTOTOXICITY (ADCC) 审中-公开
标题翻译：具有增加的抗体依赖性细胞毒性（ADCC）的II型抗CD20抗体的组合治疗
公开(公告)号：US20110177067A1
公开(公告)日：2011-07-21
申请号：US13042305
申请日：2011-03-07
申请人： Charles Dumontet , Thomas Friess , Frank Herting , Christian Klein , Pablo Umana
发明人： Charles Dumontet , Thomas Friess , Frank Herting , Christian Klein , Pablo Umana
IPC分类号： A61K39/395 , A61P35/00
CPC分类号： A61K39/39558 , A61K31/475 , A61K31/573 , A61K31/664 , A61K31/675 , A61K31/704 , A61K2039/505 , C07K16/2887 , C07K2317/24 , C07K2317/732 , A61K2300/00
摘要： The present invention is directed to a pharmaceutical composition comprising: (A) a type II anti-CD20 antibody with increased antibody dependent cellular cytotoxicity (ADCC); and (B) a chemotherapeutic agent selected from the group consisting of: cyclophosphamide, vincristine and doxorubicine. The present invention is also directed to a method for the treatment of a CD20 expressing cancer, comprising administering to a patient in need of such treatment (i) an effective first amount of a type II anti-CD20 antibody with increased antibody dependent cellular cytotoxicity; and (ii) an effective second amount of one or more chemotherapeutic agents selected from the group consisting of cyclophosphamide, vincristine and doxorubicine.
摘要翻译：本发明涉及药物组合物，其包含：（A）具有增加的抗体依赖性细胞毒性（ADCC）的II型抗CD20抗体; 和（B）选自环磷酰胺，长春新碱和多柔比星的化疗剂。本发明还涉及一种用于治疗表达CD20的癌症的方法，包括对需要这种治疗的患者施用（i）有效的第一量的具有增加的抗体依赖性细胞毒性的II型抗CD20抗体; 和（ii）有效的第二量的一种或多种选自环磷酰胺，长春新碱和多柔比星的化学治疗剂。

35. 发明授权

US07968554B2 Pyrazolo[3,4-d]pyrimidine derivatives 有权
标题翻译：吡唑并[3,4-d]嘧啶衍生物
公开(公告)号：US07968554B2
公开(公告)日：2011-06-28
申请号：US12175562
申请日：2008-07-18
申请人： David Joseph Bartkovitz , Xin-Jie Chu , Kin-Chun Luk
发明人： David Joseph Bartkovitz , Xin-Jie Chu , Kin-Chun Luk
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： Disclosed are novel pyrazolo[3,4-d]pyrimidine derivatives that are inhibitors of Raf kinase. These compounds and their pharmaceutically-acceptable salts and esters are anti-proliferative agents useful in the treatment or control of proliferative disorders such as solid tumors, in particular breast tumor, colon tumor, lung tumor, prostate tumor, and melanoma. Also disclosed are a composition and a unit dose formulation comprising such a compound, or a pharmaceutically-acceptable salt or ester thereof, methods for making such compounds, and methods for using such compounds, or their pharmaceutically-acceptable salts or esters, in the treatment of proliferative disorders.
摘要翻译：公开了作为Raf激酶抑制剂的新型吡唑并[3,4-d]嘧啶衍生物。这些化合物及其药学上可接受的盐和酯是可用于治疗或控制增殖性疾病如固体肿瘤，特别是乳腺肿瘤，结肠肿瘤，肺肿瘤，前列腺肿瘤和黑素瘤的抗增殖剂。还公开了包含这种化合物或其药学上可接受的盐或酯的组合物和单位剂量制剂，以及用于制备这些化合物的方法，以及在治疗中使用这些化合物或其药学上可接受的盐或酯的方法的增殖性疾病。

36. 发明授权

US07846896B2 PEG conjugates of NK4 有权
标题翻译： NK4的PEG缀合物
公开(公告)号：US07846896B2
公开(公告)日：2010-12-07
申请号：US11869797
申请日：2007-10-10
申请人： Michael Brandt , Apollon Papdimitriou
发明人： Michael Brandt , Apollon Papdimitriou
IPC分类号： A61K38/18 , C07K38/00
CPC分类号： A61K47/60
摘要： The present invention provides a conjugate consisting essentially of a NK4 molecule and a polyethylene glycol group having a molecular weight of from about 20 to about 40 kDa. The invention also provides a composition in which the monoPEGylated conjugates comprise at least 90% of the total of pegylated NK4 molecules and unpegylated NK4 molecules in the composition. Also provided is a composition in which the monoPEGylated conjugates comprise conjugates in which the PEG groups are attached to groups randomly selected from the lysine side chains of NK4 molecules and the N-terminal amino groups of NK4 molecules. A method for the treatment of cancer by administering 1 to 30 mg monoPEGylated NK4 per kg per day is further provided.
摘要翻译：本发明提供了基本上由NK4分子和分子量为约20至约40kDa的聚乙二醇基团组成的缀合物。本发明还提供了一种组合物，其中单聚乙二醇化缀合物包含组合物中聚乙二醇化NK4分子和未聚乙二醇化NK4分子总数的至少90％。还提供了其中单PEG化缀合物包含缀合物的组合物，其中PEG基团连接到随机选自NK4分子的赖氨酸侧链和NK4分子的N-末端氨基的基团。进一步提供通过每公斤施用1至30mg单PEG化的NK4来治疗癌症的方法。

37. 发明授权

US07799933B2 Sulfonamide derivatives 有权
标题翻译：磺酰胺衍生物
公开(公告)号：US07799933B2
公开(公告)日：2010-09-21
申请号：US11951426
申请日：2007-12-06
申请人： Simona M. Ceccarelli , Odile Chomienne , Patrizio Mattei , Ulrike Obst Sander
发明人： Simona M. Ceccarelli , Odile Chomienne , Patrizio Mattei , Ulrike Obst Sander
IPC分类号： A61K31/404 , C07D209/12
CPC分类号： C07D209/08 , C07D215/58 , C07D417/12
摘要： The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型磺酰胺衍生物，其中R 1，R 2，R 3，X和Y如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物抑制L-CPT1，可用作药物。

38. 发明授权

US07790733B2 8-alkoxy or cycloalkoxy-4-methyl-3,4-dihydro-quinazolin-2-ylamines 失效
标题翻译： 8-烷氧基或环烷氧基-4-甲基-3,4-二氢 - 喹唑啉-2-基胺
公开(公告)号：US07790733B2
公开(公告)日：2010-09-07
申请号：US11472084
申请日：2006-06-21
申请人： Alexander Alanine , Luca Claudio Gobbi , Sabine Kolczewski , Thomas Luebbers , Jens-Uwe Peters , Lucinda Steward
发明人： Alexander Alanine , Luca Claudio Gobbi , Sabine Kolczewski , Thomas Luebbers , Jens-Uwe Peters , Lucinda Steward
IPC分类号： A61K31/517 , C07D239/84
CPC分类号： C07D239/84
摘要： The present invention relates to compounds of formula wherein R1, R2, R3, and n are as described in the specification and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I can be used for the treatment of 5-HT5A receptor antagonists related diseases, which include depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, disorders of eating behaviors, sexual dysfunction, sleep disorders, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, dementia in Parkinson's disease, neuroleptic-induced Parkinsonism and tardive dyskinesias, as well as other psychiatric disorders and gastrointestinal disorders such as irritable bowel syndrome.
摘要翻译：本发明涉及下式的化合物，其中R 1，R 2，R 3和n如说明书及其药学上可接受的酸加成盐所述。式I化合物可用于治疗5-HT5A受体拮抗剂相关疾病，包括抑郁症，焦虑症，精神分裂症，惊恐障碍，广场恐怖症，社会恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，饮食行为障碍，性功能障碍，睡眠障碍，戒除药物，运动障碍如帕金森病，帕金森病中的痴呆，精神分裂症引起的帕金森综合征和迟发性运动障碍，以及其他精神疾病和胃肠道疾病如过敏性肠综合征。

39. 发明授权

US07772253B2 Amide derivatives as somatostatin receptor 5 antagonists 失效
标题翻译：酰胺衍生物作为促生长素抑制素受体5拮抗剂
公开(公告)号：US07772253B2
公开(公告)日：2010-08-10
申请号：US11442619
申请日：2006-05-26
申请人： Alfred Binggeli , Andreas Christ , Luke Gideon Granville Green , Wolfgang Guba , Hans-Peter Maerki , Rainer Eugen Martin , Peter Mohr
发明人： Alfred Binggeli , Andreas Christ , Luke Gideon Granville Green , Wolfgang Guba , Hans-Peter Maerki , Rainer Eugen Martin , Peter Mohr
IPC分类号： A61K31/4545 , C07D403/02
CPC分类号： C07D211/58 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/14
摘要： This invention is concerned with compounds of the formula wherein R1 to R5, R5′ and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
摘要翻译：本发明涉及下式的化合物，其中R 1至R 5，R 5'和A如说明书和权利要求书中所定义，及其药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。

40. 发明申请

US20100179306A1 ANTIBODIES FOR IDENTIFYING AND/OR ISOLATING AT LEAST ONE CELL POPULATION 审中-公开
标题翻译：用于识别和/或分离至少一个细胞群体的抗体
公开(公告)号：US20100179306A1
公开(公告)日：2010-07-15
申请号：US12686992
申请日：2010-01-13
申请人： Hans-Joerg BUEHRING , Reiner LAMMERS , Selim KUCI , Tim CONZE
发明人： Hans-Joerg BUEHRING , Reiner LAMMERS , Selim KUCI , Tim CONZE
IPC分类号： C07K16/00 , C07K14/00
CPC分类号： C07K16/18 , C07K16/28
摘要： Monoclonal antibodies, or fragments thereof, are used for isolating and/or identifying at least one cell population. The cell population can include any of the following types of cells: haematopoietic stem cells, neuronal stem cells, neuronal progenitor cells, mesenchymal stem cells and mesenchymal progenitor cells. The antibodies, or fragments thereof, bind to an antigen which is the same as that bound by an antibody which is produced by the hybridoma cell lines CUB1, CUB2, CUB3 and CUB4, which were deposited in the DSMZ under the numbers DSM ACC2569, DSM ACC2566 and DSM ACC2565, on 14 Aug. 2002, and DSM ACC2551, on 12 Jul. 2002.
摘要翻译：单克隆抗体或其片段用于分离和/或鉴定至少一个细胞群体。细胞群可以包括以下类型的细胞：造血干细胞，神经元干细胞，神经元祖细胞，间充质干细胞和间充质祖细胞。抗体或其片段与由通过杂交瘤细胞系CUB1，CUB2，CUB3和CUB4产生的抗体结合的抗原结合，所述抗体以DSM ACC2569，DSM 2002年8月14日的ACC2566和DSM ACC2565以及2002年7月12日的DSM ACC2551。

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