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71. 发明授权

US06552088B2 Biphenyl derivatives 失效
标题翻译：联苯衍生物
公开(公告)号：US06552088B2
公开(公告)日：2003-04-22
申请号：US09886669
申请日：2001-06-21
申请人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
发明人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
IPC分类号： C07C23300
CPC分类号： C07D295/155 , C07C217/54 , C07C233/15 , C07C233/44 , C07C233/66 , C07C235/42
摘要： Biphenyl substituted amides with activity as antagonists of the neurokinin 1 (NK-1, substance P) receptor.
摘要翻译：具有作为神经激肽1（NK-1，物质P）受体的拮抗剂的活性的联苯取代的酰胺。

72. 发明授权

US06274588B1 4-phenyl-pyrimidine derivatives 失效
标题翻译： 4-苯基 - 嘧啶衍生物
公开(公告)号：US06274588B1
公开(公告)日：2001-08-14
申请号：US09575382
申请日：2000-05-22
申请人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
发明人： Michael Bös , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
IPC分类号： C07D23924
CPC分类号： C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D239/48 , C07D401/04
摘要： The invention provides compounds of the formula wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R1 and R2 may together be —CH═CH—CH═CH—, wherein R1 and R2 together with the two carbon ring atoms to which they are attached form a fused ring; R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R4/R4′ are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, —(CH2)n-piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, —(CH2)n-morpholinyl, —(CH2)n-piperidinyl, —(CH2)n+1-imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; and n is 0-2; X is —C(O)N(R4″)— or —N(R4″)C(O)—; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds have a good affinity to the NK-1 receptor and may therefore used for the treatment of diseases related to this receptor.
摘要翻译：本发明提供的化合物，其中R 1是氢或卤素; R 2是氢，卤素，低级烷基或低级烷氧基; R 1和R 2一起可以是-CH = CH-CH = CH-，其中R 1和R 2与两个碳环它们所连接的原子形成稠环; R3是卤素，三氟甲基，低级烷基或低级烷氧基; R4 / R4'各自独立地是氢或低级烷基; R5是低级烷基，低级烷氧基，氨基，苯基，羟基 - 低级烷基，氰基 - 低级烷基，氨基甲酰基 - 低级烷基，吡啶基，嘧啶基， - （CH2）n-哌嗪基，其任选被一个或两个低级烷基或羟基 - 低级烷基取代， - （CH 2） - （CH 2）n - 哌啶基， - （CH 2）n + 1-咪唑基，低级烷基 - 硫烷基，低级烷基磺酰基，苄基氨基，-NH-（CH 2）n + n + 1N（R4“）2，-O-（CH2）n + 1-吗啉基，-O-（CH2）n + 1-哌啶基或-O-（CH2）n + 1N（R4” 其中R4“是氢或低级烷基; 和n为0-2; X为-C（O）N（R4“） - 或-N（R4”）C（O） - ;以及其药学上可接受的酸加成盐。对NK-1受体具有良好的亲和性，因此可用于治疗与该受体有关的疾病。

73. 发明申请

US20120172412A1 In Vivo Polynucleotide Delivery Conjugates Having Enzyme Sensitive Linkages 有权
标题翻译：具有酶敏感连接的体内多核苷酸递送缀合物
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
IPC分类号： A61K48/00 , C08G63/91 , C07C69/96
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。

74. 发明申请

US20120157509A1 GALACTOSE CLUSTER-PHARMACOKINETIC MODULATOR TARGETING MOIETY FOR siRNA 有权
标题翻译：糖皮质聚合酶 - 药物调节剂靶向siRNA
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。

75. 发明申请

US20110207799A1 Compositions for Targeted Delivery of siRNA 有权
标题翻译： siRNA靶向递送组合物
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。

76. 发明申请

US20070129419A1 Serotonin transporter (SERT) inhibitors for the treatment of depression and anxiety 审中-公开
标题翻译：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
申请人： Christophe Grundschober , Torsten Hoffmann , Andreas Koblet , Patrick Schnider
发明人： Christophe Grundschober , Torsten Hoffmann , Andreas Koblet , Patrick Schnider
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。

77. 发明申请

US20060029670A1 Pharmaceutical Formulations and Method for Making 审中-公开
标题翻译：药物制剂及制备方法
公开(公告)号：US20060029670A1
公开(公告)日：2006-02-09
申请号：US11163297
申请日：2005-10-13
申请人： Torsten Hoffmann , Michael Pieroth , Gerhard Zessin , Karl-Friedrich Landgraf
发明人： Torsten Hoffmann , Michael Pieroth , Gerhard Zessin , Karl-Friedrich Landgraf
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。

78. 发明申请

US20050222102A1 Treatment of rhinitis with anticholinergics alone or in combination with antihistamines, phosphodiesterase 4 inhibitors, or corticosteroids 审中-公开
标题翻译：单用抗胆碱能药物或与抗组胺药，磷酸二酯酶4抑制剂或皮质类固醇联合治疗鼻炎
公开(公告)号：US20050222102A1
公开(公告)日：2005-10-06
申请号：US11051470
申请日：2005-02-07
申请人： Joachim Maus , Ursula Petzold , Istvan Szelenyi , Torsten Hoffmann , Mario Weingart
发明人： Joachim Maus , Ursula Petzold , Istvan Szelenyi , Torsten Hoffmann , Mario Weingart
IPC分类号： A61K31/401 , A61K31/519 , A61K31/55 , A61K31/573 , A61K39/00 , A61K45/06
CPC分类号： A61K45/06 , A61K31/401 , A61K31/519 , A61K31/55 , A61K31/573 , A61K2300/00
摘要： The present invention provides novel combinations comprising a topical anticholinergic drug alone or in combination with topically administered antihistamines, topically or orally administered phosphodiesterase 4 inhibitors or topical corticosteroids for the treatment of rhinitis of various origins. It further comprises presentation of these combinations in locally applied formulations and includes various pharmaceutical formulations suitable for topical application, e.g. nasal sprays, nasal drops, emulsions, pastes, creams and gels.
摘要翻译：本发明提供新颖的组合，其包括单独的局部抗胆碱能药物或局部施用的抗组胺剂，局部或口服给予的磷酸二酯酶4抑制剂或局部皮质类固醇用于治疗各种原因的鼻炎。其还包括在局部施用的制剂中呈现这些组合，并且包括适用于局部应用的各种药物制剂，例如。鼻喷雾剂，滴鼻剂，乳剂，糊剂，霜剂和凝胶剂。

79. 发明授权

US06897226B2 NK-1 receptor active amine oxide prodrugs 有权
标题翻译： NK-1受体活性氧化胺前药
公开(公告)号：US06897226B2
公开(公告)日：2005-05-24
申请号：US10616276
申请日：2003-07-09
申请人： Torsten Hoffmann , Sonia Maria Poli , Patrick Schnider , Andrew Sleight
发明人： Torsten Hoffmann , Sonia Maria Poli , Patrick Schnider , Andrew Sleight
IPC分类号： C07D213/76 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/4545 , A61K31/455 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P1/00 , A61P1/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/00 , A61P17/02 , A61P19/02 , A61P25/00 , A61P25/06 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/36 , A61P27/02 , A61P29/00 , A61P29/02 , A61P37/02 , A61P37/08 , A61P43/00 , C07D213/75 , C07D213/82 , C07D401/04 , C07D401/12 , C07D413/04 , C07D417/04 , C07D401/00 , C07D409/00 , C07D411/00
CPC分类号： C07D213/75 , C07D401/04 , C07D401/12
摘要： Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.
摘要翻译：本发明的化合物是显示NK1受体活性的氧化胺前药。

80. 发明授权

US06747026B2 NK-1 receptor active amine oxide prodrugs 有权
公开(公告)号：US06747026B2
公开(公告)日：2004-06-08
申请号：US10337543
申请日：2003-01-07
申请人： Torsten Hoffmann , Sonia Maria Poli , Patrick Schnider , Andrew Sleight
发明人： Torsten Hoffmann , Sonia Maria Poli , Patrick Schnider , Andrew Sleight
IPC分类号： C07D26530
CPC分类号： C07D213/75 , C07D401/04 , C07D401/12
摘要： Compounds of the invention are amine oxide prodrugs showing activity on the NK1 receptor.

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