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61.发明授权Use of inhibtors of glutaminyl cyclases for treatment and prevention of disease 有权使用谷氨酰胺环化酶抑制剂治疗和预防疾病公开(公告)号：US08685664B2
公开(公告)日：2014-04-01
申请号：US12101497
申请日：2008-04-11
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre Johannes Niestroj , Stephan Schilling , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Andre Johannes Niestroj , Stephan Schilling , Ulrich Heiser
CPC分类号： C07F9/6561 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506
摘要： Novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译： 哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新型生理底物，QC的新效应物，筛选此类效应物的方法，以及包含这些效应物的这种效应物和药物组合物的用途，用于治疗可由 调节QC活性。 优选的组合物还包含用于治疗或减轻可通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV类似酶的抑制剂。
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62.发明申请公开(公告)号：US20120172412A1
公开(公告)日：2012-07-05
申请号：US13336028
申请日：2011-12-23
申请人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffmann , Kerstin Jahn-Hofmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
发明人： David B. Rozema , Darren H. Wakefield , David L. Lewis , Jon A. Wolff , Andrei V. Blokhin , Jonathan D. Benson , Jeffrey C. Carlson , Philipp Hadwiger , Eric A. Kitas , Torsten Hoffmann , Kerstin Jahn-Hofmann , Peter Mohr , Hans Martin Mueller , Guenther Ott , Ingo Roehl
CPC分类号： A61K38/00 , A61K31/7088 , A61K47/60 , A61K47/65 , A61K48/00 , C07C69/96 , C07C271/20 , C07H15/04 , C07H15/20 , C07H15/26 , C07K7/02 , C07K2317/77 , C12N15/1138 , C12N15/87 , C12N2310/14 , C12N2310/321 , C12N2310/322 , C12N2310/351 , C12N2320/30
摘要： The present invention is directed compositions for delivery of RNA interference (RNAi) polynucleotides to cells in vivo. The compositions comprise amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or DPC) are further covalently linked to an RNAi polynucleotide or co-administered with a targeted RNAi polynucleotide-targeting molecule conjugate.
摘要翻译： 本发明涉及用于将RNA干扰（RNAi）多核苷酸递送至细胞体内的组合物。 组合物包含用酶切割二肽 - 氨基苄基 - 碳酸酯掩蔽剂可逆地修饰的两亲膜活性多胺。 改性掩盖聚合物的膜活性，而可逆性提供生理反应性。 可逆修饰的多胺（动态多偶联物或DPC）进一步共价连接到RNAi多核苷酸或与靶向RNAi多核苷酸靶向分子缀合物共同施用。
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63.发明申请公开(公告)号：US20120157509A1
公开(公告)日：2012-06-21
申请号：US13327271
申请日：2011-12-15
申请人： Philipp Hadwiger , Torsten Hoffmann , Eric A. Kitas , Peter Mohr , Ingo Roehl , Linda Valis , David B. Rozema , David L. Lewis , Darren H. Wakefield
发明人： Philipp Hadwiger , Torsten Hoffmann , Eric A. Kitas , Peter Mohr , Ingo Roehl , Linda Valis , David B. Rozema , David L. Lewis , Darren H. Wakefield
IPC分类号： A61K31/7088 , C07K14/00 , C07H21/02
CPC分类号： C07K5/1021 , C07H21/02
摘要： The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cell in vivo. The pharmacokinetic modulator improve in vivo targeting compared to the targeting ligand alone. Targeting ligand-pharmacokinetic modulator targeting moiety targeted RNAi polynucleotides can be administered in vivo alone or together with co-targeted delivery polymers.
摘要翻译： 本发明涉及用于靶向将RNA干扰（RNAi）多核苷酸递送至细胞体内的组合物。 与单独的靶向配体相比，药代动力学调节剂改善体内靶向。 靶向配体 - 药代动力学调节剂靶向部分靶向的RNAi多核苷酸可以单独施用或与共靶向递送聚合物一起施用。
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公开(公告)号：US20110207799A1
公开(公告)日：2011-08-25
申请号：US13032029
申请日：2011-02-22
申请人： David B. Rozema , David L. Lewis , Darren H. Wakefield , Torsten Hoffmann , Erik Kitas , Peter Mohr , Philipp Hadwiger , Wilma Thuer , Linda Valis
发明人： David B. Rozema , David L. Lewis , Darren H. Wakefield , Torsten Hoffmann , Erik Kitas , Peter Mohr , Philipp Hadwiger , Wilma Thuer , Linda Valis
IPC分类号： A61K31/7105 , A61K31/711 , A61K31/713 , A61P1/16 , A61P35/00 , A61P31/12 , A61P3/00 , A61P3/10 , A61P3/06
CPC分类号： C12N15/113 , A61K9/08 , A61K31/713 , A61K47/32 , A61K47/549 , A61K47/60 , A61K47/65 , A61K48/0041 , C12N15/111 , C12N15/87 , C12N2310/14 , C12N2310/141 , C12N2310/3515 , C12N2320/32
摘要： The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery polymers.
摘要翻译： 本发明涉及用于将体内RNA干扰（RNAi）多核苷酸靶向递送至肝细胞的组合物。 靶向RNAi多核苷酸与共靶向递送聚合物一起施用。 递送聚合物提供膜穿透功能，用于将RNAi多核苷酸从细胞外部移动到细胞内。 可逆修饰提供对递送聚合物的生理反应性。
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公开(公告)号：US07608577B2
公开(公告)日：2009-10-27
申请号：US10216305
申请日：2002-08-09
CPC分类号： C07K7/06 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812
摘要： The present invention relates to compounds of the general formula 1 and pharmaceutically acceptable salts thereof, to the use of the compounds for the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidosis, diabetes mellitus, diabetic neuropathy and nephropathy and of sequelae caused by diabetes mellitus in mammals.
摘要翻译： 本发明涉及通式1的化合物及其药学上可接受的盐，该化合物用于治疗葡萄糖耐量异常，糖尿病，高脂血症，代谢性酸中毒，糖尿病，糖尿病性神经病变和肾病以及由 哺乳动物糖尿病。
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公开(公告)号：US20090068699A1
公开(公告)日：2009-03-12
申请号：US12039066
申请日：2008-02-28
IPC分类号： C12Q1/02 , C07D235/16 , A61K31/4184 , A61K31/5377 , C07D413/12 , C07D417/12 , A61K31/428
CPC分类号： A61K31/4178 , A61K31/4184 , C07D231/12 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04
摘要： An inhibitor of a glutaminyl peptide cyclotransferase, and use thereof for the treatment and/or prevention of a disease or disorder selected from the group consisting of inflammatory diseases selected from a. neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, Familial Danish Dementia, multiple sclerosis, b. chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, c. fibrosis, e.g. lung fibrosis, liver fibrosis, renal fibrosis, d. cancer, e.g. cancer/hemangioendothelioma proliferation, gastric carcinomas, e. metabolic diseases, e.g. hypertension, f. and other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis. Additionally disclosed are a respective diagnostic method, assay and kit.
摘要翻译： 谷氨酰胺肽环转移酶的抑制剂及其用于治疗和/或预防选自以下的炎性疾病的疾病或病症的用途： 神经变性疾病，例如 轻度认知障碍（MCI），阿尔茨海默病，唐氏综合征神经变性，家族性英国痴呆，家族性丹麦痴呆，多发性硬化，b。 慢性和急性炎症，例如 类风湿关节炎，动脉粥样硬化，再狭窄，胰腺炎，c。 纤维化，例如 肺纤维化，肝纤维化，肾纤维化，d。 癌症，例如 癌症/血管内皮瘤增生，胃癌，e。 代谢疾病，例如 高血压，f。 和其它炎性疾病，例如 神经性疼痛，移植物排斥/移植物衰竭/移植物血管病变，HIV感染/艾滋病，睾丸炎，结节性硬化症。 另外公开了相应的诊断方法，测定和试剂盒。
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公开(公告)号：US20070191366A1
公开(公告)日：2007-08-16
申请号：US11685881
申请日：2007-03-14
申请人： Torsten Hoffmann , Stephan Schilling , Andre Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
发明人： Torsten Hoffmann , Stephan Schilling , Andre Niestroj , Hans-Ulrich Demuth , Ulrich Heiser , Mirko Buchholz
IPC分类号： A61K31/5377 , A61K31/517 , A61K31/454 , A61K31/4439 , A61K31/4184 , A61K31/4178
CPC分类号： A61K31/4178 , A61K31/00 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4439 , A61K31/454 , A61K31/517 , A61K31/5377 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
摘要翻译： 本发明提供哺乳动物谷氨酰胺酰环化酶（QC，EC 2.3.2.5）的新生理底物，QC的新效应物，用于筛选此类效应物的方法，以及使用这些效应物和包含这些效应物的药物组合物，用于治疗 可以通过调节QC活性来治疗。 优选的组合物另外包含用于治疗或减轻可以通过调节QC和DP IV-活性治疗的病症的DP IV或DP IV样酶的抑制剂。
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68.发明申请Serotonin transporter (SERT) inhibitors for the treatment of depression and anxiety 审中-公开用于治疗抑郁和焦虑的血清素转运蛋白（SERT）抑制剂公开(公告)号：US20070129419A1
公开(公告)日：2007-06-07
申请号：US11603515
申请日：2006-11-22
IPC分类号： A61K31/40 , C07D207/04
CPC分类号： C07D207/08 , C07D207/09
摘要： The present invention relates to cis-derivatives of formula wherein R1, R2, and R3 are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors). By virtue of their efficacy as SERT inhibitors, the compounds of the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.
摘要翻译： 本发明涉及下式的顺式衍生物，其中R 1，R 2，R 3和R 3如本文所定义，并且与药学上可接受的酸 其加成盐。 式I化合物是5-羟色胺转运蛋白（SERT抑制剂）的良好抑制剂。 由于其作为SERT抑制剂的功效，本发明的化合物特别可用于治疗CNS紊乱和精神病，特别是治疗或预防抑郁状态和/或治疗焦虑症。
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公开(公告)号：US20060194852A1
公开(公告)日：2006-08-31
申请号：US11369606
申请日：2006-03-07
IPC分类号： A61K31/426 , A61K31/401 , C07D277/56
CPC分类号： C07D277/24
摘要： The present invention provides compounds of the formula: wherein X═CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arthritis, obesity, immune and autoimmune disorders, allograft transplantation, cancer, neuronal disorders and dermal diseases.
摘要翻译： 本发明提供下式的化合物：其中X-CH 2或S或其药学上可接受的盐可用于治疗由DPIV或DPIV样酶如关节炎，肥胖，免疫和自身免疫介导的病症 疾病，同种异体移植，癌症，神经元疾病和皮肤疾病。
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公开(公告)号：US20060029670A1
公开(公告)日：2006-02-09
申请号：US11163297
申请日：2005-10-13
IPC分类号： A61K31/7024 , A61K9/26
CPC分类号： A61K9/1694 , A61K9/1623 , A61K47/26
摘要： The invention relates to a process of making an oral pharmaceutical formulation with variably adjustable release rate, which comprises one or more active ingredients, and one or more sucrose ester of a fatty acid as the sole release-controlling agent for said active ingredient wherein when the dosage form is a granule or a pellet. The formulation is made by melting the oral formulation and granulating or pelletizing the melt.
摘要翻译： 本发明涉及制备具有可变调节释放速率的口服药物制剂的方法，其包含一种或多种活性成分，和一种或多种脂肪酸蔗糖酯作为所述活性成分的唯一释放控制剂，其中当 剂型是颗粒或颗粒。 该制剂通过熔化口腔制剂并使熔体成粒或造粒而制成。
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