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1. 发明申请

WO2006099968A1 METABOLITES FOR NK-I ANTAGONISTS FOR EMESIS 审中-公开
标题翻译：用于EMESIS的NK-1拮抗剂的代谢物
公开(公告)号：WO2006099968A1
公开(公告)日：2006-09-28
申请号：PCT/EP2006/002313
申请日：2006-03-14
申请人： F. HOFFMANN-LA ROCHE AG , FUNK, Christoph , HOFFMANN, Torsten , KOBLET, Andreas
发明人： FUNK, Christoph , HOFFMANN, Torsten , KOBLET, Andreas
IPC分类号： C07D213/75 , A61K31/44 , A61P25/22 , A61P25/24
CPC分类号： C07D213/75
摘要： The present invention relates to compounds of the general formula (I) wherein R is methyl; and R 1 is 4-methyl-4-oxy-piperazin-l-yl; or R is CH 2 OH and R 1 is 4-methyl-piperazin-l-yl or is 4-methyl-4-oxy-piperazin-l-yl; and to pharmaceutically acceptable acid addition salts thereof for the treatment of NK-I receptor related diseases.
摘要翻译：本发明涉及通式（I）的化合物，其中R是甲基; 并且R 1是4-甲基-4-氧 - 哌嗪-1-基; 或R为CH 2 OH，R 1为4-甲基 - 哌嗪-1-基，或为4-甲基-4-氧 - 哌嗪-1-基; 和其药学上可接受的酸加成盐，用于治疗NK-1受体相关疾病。

2. 发明申请

WO2005002577A1 DUAL NK1/NK3 ANTAGONISTS FOR TREATING SCHIZOPHRENIA 审中-公开
标题翻译：用于处理SCHIZOPHRENIA的双NK1 / NK3拮抗剂
公开(公告)号：WO2005002577A1
公开(公告)日：2005-01-13
申请号：PCT/EP2004/006929
申请日：2004-06-25
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN, Torsten , KOBLET, Andreas , PETERS, Jens-Uwe , SCHNIDER, Patrick , SLEIGHT, Andrew , STADLER, Heinz
发明人： HOFFMANN, Torsten , KOBLET, Andreas , PETERS, Jens-Uwe , SCHNIDER, Patrick , SLEIGHT, Andrew , STADLER, Heinz
IPC分类号： A61K31/44
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 use of compounds of the general formula wherein the substituents are as described in claim 1 or pharmaceutically active acid-addition salts thereof for the preparation of medicaments for the treatment of schizophrenia.
摘要翻译：使用通式的化合物，其中取代基如权利要求1所述或其药学活性的酸加成盐用于制备治疗精神分裂症的药物。

3. 发明申请

WO2007063009A1 SEROTONIN TRANSPORTER (SERT) INHIBITORS 审中-公开
标题翻译： SEROTONIN TRANSPORTER（SERT）抑制剂
公开(公告)号：WO2007063009A1
公开(公告)日：2007-06-07
申请号：PCT/EP2006/068740
申请日：2006-11-22
申请人： F. HOFFMANN-LA ROCHE AG , GRUNDSCHOBER, Christophe , HOFFMANN, Torsten , KOBLET, Andreas , SCHNIDER, Patrick
发明人： GRUNDSCHOBER, Christophe , HOFFMANN, Torsten , KOBLET, Andreas , SCHNIDER, Patrick
IPC分类号： C07D207/08 , C07D207/09 , A61K31/40
CPC分类号： C07D207/08 , C07D207/09
摘要： The present invention relates to cis- derivatives of formula (I) wherein R 1 is hydrogen, halogen or lower alkyl; R 2 /R 3 are independently from each other hydrogen, halogen, CN, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; X is -O- or -N(R)-; R is hydrogen or lower alkyl; 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 in 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：本发明涉及式（I）的顺式衍生物，其中R 1是氢，卤素或低级烷基; R 2彼此独立地为氢，卤素，CN，低级烷基，被卤素取代的低级烷基，被卤素取代的低级烷氧基或低级烷氧基; X是-O-或-N（R） - ; R是氢或低级烷基; 及其药学上可接受的酸加成盐。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，本发明中的化合物特别可用于治疗CNS障碍和精神病性障碍，特别是治疗或预防抑郁状态和/或治疗焦虑症。

4. 发明申请

WO2012049190A1 N-PYRIDIN-3-YL OR N-PYRAZIN-2-YL CARBOXAMIDES 审中-公开
标题翻译： N-吡啶-3-基或N-吡咯啉-2-基羧酸酰胺
公开(公告)号：WO2012049190A1
公开(公告)日：2012-04-19
申请号：PCT/EP2011/067753
申请日：2011-10-12
申请人： F. HOFFMANN-LA ROCHE AG , GRETHER, Uwe , HEBEISEN, Paul , HOFFMANN, Torsten , ROEVER, Stephan
发明人： GRETHER, Uwe , HEBEISEN, Paul , HOFFMANN, Torsten , ROEVER, Stephan
IPC分类号： C07D213/75 , C07D401/12 , C07D403/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D498/04 , A61K31/444 , A61K31/4965 , A61P9/00
CPC分类号： C07D213/75 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D498/04
摘要： The present invention relates to compounds of the formula I wherein A, R 1 to R 7 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
摘要翻译：本发明涉及式I化合物，其中A，R 1至R 7在说明书中定义，及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其作为用于治疗和/或预防疾病的药物的用途其可以用HDL-胆固醇升高剂治疗，例如特别是血脂异常，动脉粥样硬化和心血管疾病。

5. 发明申请

WO2011104169A1 COMPOSITIONS FOR TARGETED DELIVERY OF SIRNA 审中-公开
标题翻译： SIRNA的目标交付组合物
公开(公告)号：WO2011104169A1
公开(公告)日：2011-09-01
申请号：PCT/EP2011/052393
申请日：2011-02-18
申请人： F. HOFFMANN-LA ROCHE AG , HADWIGER, Philipp , HOFFMANN, Torsten , KITAS, Eric A. , LEWIS, David L. , MOHR, Peter , ROZEMA, David B. , THUER, Wilma , VALIS, Linda Christine , WAKEFIELD, Darren H.
发明人： HADWIGER, Philipp , HOFFMANN, Torsten , KITAS, Eric A. , LEWIS, David L. , MOHR, Peter , ROZEMA, David B. , THUER, Wilma , VALIS, Linda Christine , WAKEFIELD, Darren H.
IPC分类号： C12N15/11 , A61K31/713 , A61K47/18 , A61K48/00 , C12N15/87
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。

6. 发明申请

WO2006089658A2 NK1 ANTAGONISTS 审中-公开
标题翻译： NK1拮抗剂
公开(公告)号：WO2006089658A2
公开(公告)日：2006-08-31
申请号：PCT/EP2006/001310
申请日：2006-02-14
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN, Torsten , SCHNIDER, Patrick
发明人： HOFFMANN, Torsten , SCHNIDER, Patrick
IPC分类号： C07D213/75 , A61K31/44 , A61P25/18
CPC分类号： C07D213/75 , C07D213/82
摘要： The present invention relates to compounds of the formula (I), wherein R 1 /R 1’ are hydrogen or methyl; X is -C(O)N(CH 3 )- or -N(CH 3 )C(O)-; and to pharmaceutically acceptable acid addition salts thereof for the treatment of numerous inflammatory conditions, migraine, rheumatoid arthritis, asthma, inflammatory bowel disease, mediation of the emetic reflex, Parkinson's disease, anxiety, depression, psychosis, motion sickness, induced vomiting, pain, headache, migraine, Alzheimer's disease, multiple sclerosis, attenuation of morphine withdrawal, cardiovascular changes, oedema, such as oedema caused by thermal injury, chronic inflammatory diseases such as rheumatoid arthritis, asthma/bronchial hyperreactivity and other respiratory diseases including allergic rhinitis, inflammatory diseases of the gut including ulcerative colitis and Crohn's disease, ocular injury and ocular inflammatory diseases, traumatic brain injury, motion sickness, emesis and psychoimmunologic or psychosomatic disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 1，R 2， X是-C（O）N（CH 3） - 或-N（CH 3）C（O） - ; 以及其药学上可接受的酸加成盐，用于治疗许多炎性病症，偏头痛，类风湿性关节炎，哮喘，炎症性肠病，呕吐反射调节，帕金森病，焦虑症，抑郁症，精神病，运动病，诱导性呕吐，疼痛，头痛，偏头痛，阿尔茨海默病，多发性硬化，吗啡戒断减轻，心血管改变，水肿，如热损伤引起的水肿，慢性炎性疾病如类风湿性关节炎，哮喘/支气管高反应性和其他呼吸系统疾病，包括过敏性鼻炎，炎性疾病的肠道，包括溃疡性结肠炎和克罗恩病，眼部损伤和眼部炎症性疾病，创伤性脑损伤，运动病，呕吐和心理免疫或心身疾病。

7. 发明申请

WO2010069859A1 CYCLOHEXANECARBOXAMIDE DERIVATIVES USEFUL AS INHIBITORS OF CHOLESTERYL ESTER TRANSFER PROTEIN 审中-公开
标题翻译：作为胆固醇转运蛋白的抑制剂的环己基甲酰胺衍生物
公开(公告)号：WO2010069859A1
公开(公告)日：2010-06-24
申请号：PCT/EP2009/066863
申请日：2009-12-10
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN, Torsten , KUEHNE, Holger , NIESOR, Eric J. , PFLIEGER, Philippe
发明人： HOFFMANN, Torsten , KUEHNE, Holger , NIESOR, Eric J. , PFLIEGER, Philippe
IPC分类号： C07C323/52 , C07C327/30 , A61K31/167 , A61K31/216 , A61P9/00
CPC分类号： C07C323/52 , C07C327/30 , C07C2601/14
摘要： The invention is concerned with novel compound of formula (I) wherein R, R 2 and Q are as defined in the description and in the claims, and pharmaceutically acceptable salts thereof, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的新化合物，其中R，R 2和Q如说明书和权利要求书中所定义，及其药学上可接受的盐，其制备方法，它们作为药物的用途和包含它们的药物组合物。

8. 发明申请

WO2008128891A1 PYRROLIDINE DERIVATIVES AS DUAL NK1/NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK1 / NK3受体拮抗剂
公开(公告)号：WO2008128891A1
公开(公告)日：2008-10-30
申请号：PCT/EP2008/054261
申请日：2008-04-09
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , HOFFMANN, Torsten , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
发明人： BISSANTZ, Caterina , HOFFMANN, Torsten , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , WU, Xihan
IPC分类号： C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D471/10 , A61K31/5377 , A61P25/28
CPC分类号： C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D471/10
摘要： The invention relates to pyrrolidine derivatives of formula (I) wherein R 1 is hydrogen, halogen or lower alkyl; R 2 is hydrogen, halogen, lower alkoxy or lower alkyl substituted by halogen; R 3 is -(CH 2 ) p -heterocyclyl optionally substituted by lower alkyl, halogen, -S(O) 2 -lower alkyl, -C(O)-lower alkyl, -C(O)O-lower alkyl, hydroxy, lower alkyl substituted by hydroxy, -(CH 2 ) p -O-lower alkyl, -NHCO-lower alkyl, or is C 3-6 -cycloalkyl optionally substituted by =O, -(CH 2 ) p -O-lower alkyl or lower alkinyl, or is unsubstituted or substituted aryl or heteroaryl, wherein the substituents are selected from the group consisting of lower alkyl, CN, -S(O) 2 -lower alkyl, halogen, -C(O) -lower alkyl, hydroxy, lower alkoxy or lower alkoxy substituted by halogen; or is -(CH 2 ) P -NR 4 R 5 ; R 4 /R 5 are independently from each other hydrogen, lower alkyl, -(CRR')p-lower alkyl substituted by hydroxy, -(CRR')p-O-lower alkyl, -(CRR')p-S-lower alkyl, -(CRR') p -O-lower alkyl substituted by hydroxy or C 3-6 -cycloalkyl; R/R' are independently from each other hydrogen, lower alkyl or lower alkyl substituted by hydroxyl; n is 1 or 2; o is 1 or 2; P is 0, 1, 2, 3 or 4; or to pharmaceutically active acid-addition salts thereof.
摘要翻译：本发明涉及式（I）的吡咯烷衍生物，其中R 1是氢，卤素或低级烷基; R 2是氢，卤素，低级烷氧基或被卤素取代的低级烷基; R 3是 - 任选被低级烷基，卤素，-S（O）2取代的 - （CH 2）2 - 杂环基）低级烷基，-C（O） - 低级烷基，-C（O）O-低级烷基，羟基，被羟基取代的低级烷基， - （CH 2）或低级烷基，-NHCO-低级烷基，或为任选被= O， - （CH 2）2取代的C 3-6环烷基，低级烷基或低级炔基，或未取代或取代的芳基或杂芳基，其中取代基选自低级烷基，CN，-S（O）2，低级烷基，卤素，-C（O） - 低级烷基，羟基，低级烷氧基或被卤素取代的低级烷氧基; 或是 - （CH 2）2 - - - - - - - - - - - - - - - R 4和R 5彼此独立地是氢，低级烷基， - 被羟基取代的 - （CRR'）对 - 低级烷基， - （CRR'）pO-低级烷基， - （CRR'）pS-低级烷基， - （CRR'）由羟基或C 3-6 - 环烷基取代的-O-低级烷基; R / R'彼此独立地为氢，被羟基取代的低级烷基或低级烷基; n为1或2; o是1或2; P为0,1,2,3或4; 或其药学活性的酸加成盐。

9. 发明申请

WO2012089602A1 SMALL MOLECULE CONJUGATES FOR INTRACELLULAR DELIVERY OF BIOLOGICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：用于细胞内递送生物活性化合物的小分子
公开(公告)号：WO2012089602A1
公开(公告)日：2012-07-05
申请号：PCT/EP2011/073718
申请日：2011-12-22
申请人： F. HOFFMANN-LA ROCHE AG , HADWIGER, Philipp , HOFFMANN, Torsten , JAHN-HOFMANN, Kerstin , KITAS, Eric A. , LEWIS, David L. , MOHR, Peter , MUELLER, Hans Martin , OTT, Guenther , ROEHL, Ingo , ROZEMA, David B.
发明人： HADWIGER, Philipp , HOFFMANN, Torsten , JAHN-HOFMANN, Kerstin , KITAS, Eric A. , LEWIS, David L. , MOHR, Peter , MUELLER, Hans Martin , OTT, Guenther , ROEHL, Ingo , ROZEMA, David B.
IPC分类号： C12N15/87 , C12N15/11 , A61K48/00 , A61K31/713 , A61K47/18
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 invention provides novel compounds and conjugates of these compounds useful for the delivery of biologically active substances. Further novel design criteria for chemically stabilized siRNA particular useful when covalently attached to a delivery polymer to achieve in vivo mRNA knock down are disclosed therein.
摘要翻译：本发明提供了用于递送生物活性物质的这些化合物的新化合物和缀合物。其中公开了当共价连接到递送聚合物以实现体内mRNA敲低时特别有用的化学稳定的siRNA的新颖设计标准。

10. 发明申请

WO2012089352A1 SMALL MOLECULE CONJUGATES FOR INTRACELLULAR DELIVERY OF NUCLEIC ACIDS 审中-公开
标题翻译：小分子共聚物用于细胞内输送核酸
公开(公告)号：WO2012089352A1
公开(公告)日：2012-07-05
申请号：PCT/EP2011/063436
申请日：2011-08-04
申请人： F. HOFFMANN-LA ROCHE AG , HADWIGER, Philipp , HOFFMANN, Torsten , JAHN-HOFMANN, Kerstin , KITAS, Eric A. , LEWIS, David L. , MOHR, Peter , MUELLER, Hans Martin , OTT, Guenther , ROEHL, Ingo , ROZEMA, David B.
发明人： HADWIGER, Philipp , HOFFMANN, Torsten , JAHN-HOFMANN, Kerstin , KITAS, Eric A. , LEWIS, David L. , MOHR, Peter , MUELLER, Hans Martin , OTT, Guenther , ROEHL, Ingo , ROZEMA, David B.
IPC分类号： C12N15/87 , C12N15/11 , A61K48/00 , A61K31/713 , A61K47/18
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： Use of compounds for the delivery of nucleic acids as well as conjugates of these compounds with nucleic acids, in particular siRNAs, are provided. Also discloses are stabilized siRNA that are useful when covalently bound to such compound and co- administered with a delivery polymer to achieve mRNA knock-down in vivo. In particular, the invention provides the use of a compound of formula (I) For the delivery of nucleic acids, wherein: Y is a linker group selected from -(CH 2 ) 3 or -C(0)-N-(CH 2 -CH 2 -0)p-CH 2 -CH 2 - R 1 is -(C1 -6) alkyl; -(CH 2 )-naphthyl; or -(CH 2 ) m -phenyl, which phenyl is unsubstituted or up to four times substituted with a substituent selected from: -N0 2 , -CN, Halogen, -0-(CH 2 )-phenyl, -0-(C1- 6) alkyl, or -C(0)-NH 2 R 2 is Hydrogen; -(CH 2 ) k -N-C(Ph) 3 , which phenyl rings are unsubstituted or independently substituted with -0-(Cl -4) alkyl; -(CH 2 )k-C(0)-NH 2 ; -(CH 2 )k-phenyl; -(C1 -6) alkyl, which is unsubstituted or once substituted with -S-CH 3 ; R 3 is -NH-phenyl, which phenyl group is further substituted with a substituent independently selected from -(CH 2 )-OH or -(CH 2 )-0-C(0)-0-(4-nitro-phenyl); k is 1, 2, 3, 4, 5, or 6; m is 1, 2, 3 or 4; n is 0 or 1; and p is an integer from 1 to 20.
摘要翻译：提供了化合物用于递送核酸以及这些化合物与核酸，特别是siRNA的缀合物的用途。还公开了当与这种化合物共价结合并与递送聚合物共同施用以在体内实现mRNA敲低时有用的稳定的siRNA。特别地，本发明提供式（I）化合物用于递送核酸，其中：Y是选自 - （CH 2）3或-C（O）-N-（CH 2 -CH 2 -O）p-CH 2 -CH 2 -R 1是 - （C 1-6）烷基; - （CH 2） - 萘基; 或 - （CH 2）m - 苯基，该苯基是未取代的或至多四次被选自：-NO 2，-CN，卤素，-O-（CH 2） - 苯基，-O-（C 1-6）烷基或-C（O）-NH 2 R 2是氢; - （CH 2）k-N-C（Ph）3，该苯环是未取代的或独立地被-O-（C 1-4）烷基取代; - （CH2）K-C（O）-NH 2; - （CH 2）K - 苯基; - （C 1-6）烷基，其未被取代或一次被-S-CH 3取代; R3是-NH-苯基，该苯基进一步被独立地选自 - （CH 2）-OH或 - （CH 2）-O-C（O）-O-（4-硝基 - 苯基）的取代基取代; k为1,2,3,4,5或6; m为1,2,3或4; n为0或1; p为1〜20的整数。

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