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41. 发明申请

US20080267912A1 NOVEL INHIBITORS OF GLUTAMINYL CYCLASE 有权
标题翻译： GLUTAMINYL CYCLASE的新型抑制剂
公开(公告)号：US20080267912A1
公开(公告)日：2008-10-30
申请号：US12105874
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
发明人： Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
IPC分类号： A61K38/20 , C07D233/54 , A61K31/4164 , A61K38/21 , A61P31/00 , A61P3/00 , A61P9/00 , A61P25/00 , A61P35/00 , A61K31/4178 , A61K39/395
CPC分类号： C07D233/61 , C07D233/64 , C07D235/06 , C07D405/12 , C07D417/12
摘要： Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
摘要翻译：式（I）化合物，其用于疾病治疗的组合和用途，或其药学上可接受的盐，溶剂化物或多晶型物，包括所有互变异构体和立体异构体，其中：A表示和B，R 1，R R 3，R 4，R 4，R 5，R 6和Z 3，在整个说明书和权利要求书中都是定义的。

42. 发明授权

US08541596B2 Inhibitors 有权
公开(公告)号：US08541596B2
公开(公告)日：2013-09-24
申请号：US13091276
申请日：2011-04-21
申请人： Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
发明人： Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
IPC分类号： A61K31/4184 , C07D235/08
CPC分类号： C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14
摘要： Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.

43. 发明授权

US08227498B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US08227498B2
公开(公告)日：2012-07-24
申请号：US12105874
申请日：2008-04-18
申请人： Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
发明人： Mirko Buchholz , Ulrich Heiser , Torsten Hoffmann , Livia Boehme
IPC分类号： A61K31/417 , C07D233/64 , C07D235/06
CPC分类号： C07D233/61 , C07D233/64 , C07D235/06 , C07D405/12 , C07D417/12
摘要： Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
摘要翻译：式（I）化合物，其用于疾病治疗的组合和用途，或其药学上可接受的盐，溶剂化物或多晶型物，包括所有互变异构体和立体异构体，其中：A表示和B，R1，R2，R3，R4，R5，R6 和Z如在说明书和权利要求书中所定义。

44. 发明申请

US20110262388A1 NOVEL INHIBITORS 有权
公开(公告)号：US20110262388A1
公开(公告)日：2011-10-27
申请号：US13091276
申请日：2011-04-21
申请人： Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
发明人： Ulrich Heiser , Daniel Ramsbeck , Torsten Hoffmann , Livia Boehme
IPC分类号： A61K38/20 , C07D405/14 , C07D409/14 , C07D417/14 , C07D401/14 , C07D409/12 , C07D417/12 , A61K31/4184 , A61K31/428 , A61K31/433 , A61K31/4709 , A61K39/395 , A61K31/4409 , A61K38/21 , A61P35/00 , A61P25/18 , A61P35/04 , A61P17/06 , A61P29/00 , A61P25/00 , A61P5/00 , A61P25/28 , A61P9/10 , A61P19/02 , A61P9/00 , A61P15/08 , A61P3/00 , C07D235/08
CPC分类号： C07D209/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14
摘要： Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.

45. 发明申请

US20110178055A1 DUAL NK1/NK3 RECEPTOR ANTAGONISTS 有权
标题翻译：双NK1 / NK3受体拮抗剂
公开(公告)号：US20110178055A1
公开(公告)日：2011-07-21
申请号：US13076891
申请日：2011-03-31
申请人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
发明人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
IPC分类号： A61K31/4427 , A61K31/44 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/551 , A61K31/5377 , A61P25/18
CPC分类号： C07D213/75 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/46 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/547 , A61K31/551 , A61K31/554 , C07D401/04 , C07D413/04 , C07D417/04 , C07D419/04 , C07D451/04 , C07D487/08 , C07D491/10 , C07D495/10 , C07D497/10 , C07D513/08
摘要： The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In particular, the invention provides methods for treating both positive and negative symptoms of schizophrenia through dual inhibition of NK1 and NK3 receptors. The invention also provides novel compounds with formula I and methods for preparing compounds of the invention.
摘要翻译：本发明提供了一种治疗精神分裂症的方法，其包括给予下列化合物，其中取代基如本文所述或其药学活性的酸加成盐。特别地，本发明提供了通过NK1和NK3受体的双重抑制来治疗精神分裂症的正和负症状的方法。本发明还提供具有式I的新化合物和制备本发明化合物的方法。

46. 发明申请

US20110053954A1 METHOD OF TREATMENT AND/OR PREVENTION OF BRAIN, SPINAL OR NERVE INJURY 审中-公开
标题翻译：治疗和/或预防脑，脊髓或神经损伤的方法
公开(公告)号：US20110053954A1
公开(公告)日：2011-03-03
申请号：US12886691
申请日：2010-09-21
申请人： Torsten Hoffmann , Alan Nimmo , Andrew Sleight , Pierre Vankan , Robert Vink
发明人： Torsten Hoffmann , Alan Nimmo , Andrew Sleight , Pierre Vankan , Robert Vink
IPC分类号： A61K31/496 , A61P25/00
CPC分类号： A61K31/435
摘要： The invention relates to a method of treatment and/or prevention of brain, spinal or nerve injury comprising administration to a person in need of such treatment, of a therapeutically effective amount of an NK-1 receptor antagonist compound of the formula wherein the meanings of R, R1, R2, R2′, R3, and R4 are explained in the specification and the pharmaceutically acceptable acid addition salts and the prodrugs thereof either alone or in combination with a magnesium salt. Exemplified is the use of N-(3,5-bis-trifluoromethyl-benzyl)-N-methyl-6-(4-methyl-piperazin-1-yl)-4-o-tolyl-nicotinamide. The invention also relates to pharmaceutical composition comprising one or more such NK-1 receptor antagonists, optionally in combination with a magnesium salt, and a pharmaceutically acceptable excipient for the treatment and/or prevention of brain, spinal or nerve injury.
摘要翻译：本发明涉及一种治疗和/或预防脑，脊髓或神经损伤的方法，包括向需要这种治疗的人施用治疗有效量的下式的NK-1受体拮抗剂化合物，其中，说明书和其药学上可接受的酸加成盐及其前药单独或与镁盐组合说明了R，R 1，R 2，R 2'，R 3和R 4。举例说明了使用N-（3,5-双 - 三氟甲基 - 苄基）-N-甲基-6-（4-甲基 - 哌嗪-1-基）-4-邻甲苯基 - 烟酰胺。本发明还涉及包含一种或多种这样的NK-1受体拮抗剂，任选与镁盐组合的药物组合物和用于治疗和/或预防脑，脊髓或神经损伤的药学上可接受的赋形剂。

47. 发明申请

US20090137806A1 DUAL NK1/NK3 RECEPTOR ANTAGONISTS 有权
标题翻译：双NK1 / NK3受体拮抗剂
公开(公告)号：US20090137806A1
公开(公告)日：2009-05-28
申请号：US12361569
申请日：2009-01-29
申请人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
发明人： Torsten Hoffmann , Andreas Koblet , Jens-Uwe Peters , Patrick Schnider , Andrew Sleight , Heinz Stadler
IPC分类号： C07D401/04 , C07D497/10
CPC分类号： C07D213/75 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/46 , A61K31/496 , A61K31/4995 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/547 , A61K31/551 , A61K31/554 , C07D401/04 , C07D413/04 , C07D417/04 , C07D419/04 , C07D451/04 , C07D487/08 , C07D491/10 , C07D495/10 , C07D497/10 , C07D513/08
摘要： The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula wherein the substituents are as described herein or a pharmaceutically active acid-addition salt thereof. In particular, the invention provides methods for treating both positive and negative symptoms of schizophrenia through dual inhibition of NK1 and NK3 receptors. The invention also provides novel compounds with formula I and methods for preparing compounds of the invention.
摘要翻译：本发明提供了一种治疗精神分裂症的方法，其包括给予下列化合物，其中取代基如本文所述或其药学活性的酸加成盐。特别地，本发明提供了通过NK1和NK3受体的双重抑制来治疗精神分裂症的正和负症状的方法。本发明还提供具有式I的新化合物和制备本发明化合物的方法。

48. 发明授权

US06297375B1 4-phenyl-pyridine derivatives 有权
标题翻译： 4-苯基 - 吡啶衍生物
公开(公告)号：US06297375B1
公开(公告)日：2001-10-02
申请号：US09507456
申请日：2000-02-22
申请人： Michael Bös , Quirico Branca , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
发明人： Michael Bös , Quirico Branca , Guido Galley , Thierry Godel , Torsten Hoffmann , Walter Hunkeler , Patrick Schnider , Heinz Stadler
IPC分类号： C07D21382
CPC分类号： C07D213/30 , C07D213/38 , C07D213/40 , C07D213/74 , C07D213/75 , C07D213/82 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14
摘要： The compounds of the related invention are related to 4-phenyl-pyridine derivatives connected by a bridge containing oxygen or nitrogen to a phenyl derivative.
摘要翻译：相关发明的化合物涉及通过含有氧或氮的桥与苯基衍生物连接的4-苯基 - 吡啶衍生物。

49. 发明授权

US06225316B1 3-phenyl-pyridine-derivatives 失效
标题翻译： 3-苯基 - 吡啶衍生物
公开(公告)号：US06225316B1
公开(公告)日：2001-05-01
申请号：US09505359
申请日：2000-02-16
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： A61K3150
CPC分类号： C07D213/75 , C07D213/38 , C07D213/81
摘要： The invention relates to compounds of the formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; or R and R1 may be together —CH═CH—CH═CH—; R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R3 is hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, —N(R5)2, —N(R5)S(O)2-lower alkyl, —N(R5)C(O)R5 or a cyclic tertiary amine of the group R5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, —N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, —CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is —C(O)N(R5)—, —(CH2)mO—, —(CH2)mN(R5)—, —N(R5)C(O)—, or —N(R5)(CH2)m—; n is 0-4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor.
摘要翻译：本发明涉及式Ⅳ的化合物，其中R是氢，低级烷基，低级烷氧基，卤素或三氟甲基; R 1是氢或卤素; 或R 1可以是-CH = CH-CH = CH-; R 2是氢，卤素，三氟甲基，低级烷氧基或氰基; R 3是氢，低级烷基或形成环烷基; R 4是氢，-N（R 5） 2，-N（R 5）S（O）2-低级烷基，-N（R 5）C（O）R 5或基团R 5的环状叔胺彼此独立地为氢，C 3-6 - 环烷基，苄基或低级烷基; R6是氢，羟基，低级烷基，-N（R5）CO-低级烷基，羟基 - 低级烷基，氰基，-CHO或5-或6-元杂环基，任选地通过亚烷基键合，X 是（C） - （CH 2）m O - ， - （CH 2）m N（R 5） - ， - N（R 5）C（O） - 或-N（R 5） - ; n为0-4; 和m为1或2;以及其药学上可接受的酸加成盐。已经显示上述化合物对NK-1受体具有良好的亲和力。

50. 发明授权

US09011919B2 Compositions for targeted delivery of siRNA 有权
标题翻译：用于靶向递送siRNA的组合物
公开(公告)号：US09011919B2
公开(公告)日：2015-04-21
申请号：US13615938
申请日：2012-09-14
申请人： David B. Rozema , David L. Lewis , Darren H. Wakefield , Torsten Hoffmann , Eric Kitas , Peter Mohr , Philipp Hadwiger , Wilma Thuer , Linda Valis
发明人： David B. Rozema , David L. Lewis , Darren H. Wakefield , Torsten Hoffmann , Eric Kitas , Peter Mohr , Philipp Hadwiger , Wilma Thuer , Linda Valis
IPC分类号： A61K9/14 , C07H21/02 , C07K1/00 , A61K47/32 , A61K9/08 , A61K48/00 , C12N15/11 , C12N15/87 , A61K47/48
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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