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1. 发明申请

WO2018189065A1 ANTI-BACTERIAL PEPTIDE MACROCYCLES AND USE THEREOF 审中-公开
公开(公告)号：WO2018189065A1
公开(公告)日：2018-10-18
申请号：PCT/EP2018/058957
申请日：2018-04-09
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： ALANINE, Alexander , AMREIN, Kurt , BLEICHER, Konrad , FASCHING, Bernhard , HILPERT, Hans , KOLCZEWSKI, Sabine , KROLL, Carsten , SCHAEUBLIN, Adrian , ZAMPALONI, Claudia
IPC分类号： C07K5/02 , A61K38/00 , A61P31/04
摘要： The present invention relates to compounds of formula (I) wherein X 1 to X 8 and R 1 to R 8 are as described herein, as well as pharmaceutically acceptable salts thereof for the use in the treatment or prevention of infections and resulting diseases caused by Pseudomonas aeruginosa.

2. 发明申请

WO2017072062A1 PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII 审中-公开
标题翻译：肽抗巨细胞病毒的MACROCYCLES
公开(公告)号：WO2017072062A1
公开(公告)日：2017-05-04
申请号：PCT/EP2016/075499
申请日：2016-10-24
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： ALANINE, Alexander , BEIGNET, Julien , BLEICHER, Konrad , FASCHING, Bernhard , HILPERT, Hans , HU, Taishan , MACDONALD, Dwight , JACKSON, Stephen , KOLCZEWSKI, Sabine , KROLL, Carsten , SCHAEUBLIN, Adrian , SHEN, Hong , STOLL, Theodor , THOMAS, Helmut , WAHHAB, Amal , ZAMPALONI, Claudia
IPC分类号： C07K5/02 , A61P31/04 , A61K38/00
CPC分类号： C07K5/0827 , A61K38/00 , C07K5/02 , C07K5/06086 , C07K5/08 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K5/0815 , C07K5/0821
摘要： The present invention provides compounds of formula (I) wherein X 1 to X 8 and R 1 to R 8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
摘要翻译：本发明提供了式（I）的化合物，其中X 1至X 8和R 1至R 如上所述，以及其药学上可接受的盐。此外，本发明涉及式（I）化合物的制造，包含它们的药物组合物以及它们作为药物用于治疗由鲍曼不动杆菌引起的疾病和感染的用途。

3. 发明申请

WO2006117305A1 (3,4-DIHYDRO-QUINAZOLIN-2-YL)-(2-ARYLOXY-ETHYL)-AMINES HAVING AN ACTIVITY ON THE 5-HT RECEPTOR 审中-公开
标题翻译：（3,4-DIHYDRO-喹唑啉-2-基） - （2-氰基乙基） - 胺在5-HT受体上具有活性
公开(公告)号：WO2006117305A1
公开(公告)日：2006-11-09
申请号：PCT/EP2006/061779
申请日：2006-04-24
申请人： F. HOFFMANN-LA ROCHE AG , ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
发明人： ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
IPC分类号： C07D239/84 , C07D409/04 , C07D413/04 , A61K31/517 , A61P25/24 , A61P25/18
CPC分类号： C07D239/84 , A61K31/517 , C07D409/04 , C07D413/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkyl substituted by halogen; R is hydrogen or halogen; or R 1 and R are together with the carbon atom to which they are attached -CH=CH-CH=CH-; R 2 is hydrogen, lower alkyl, phenyl optionally substituted by halogen, or is hetaryl, optionally substituted by lower alkyl; R 3 is hydrogen, lower alkyl, phenyl, benzyl, lower alkenyl, lower alkoxy, phenyloxy, benzyloxy, S-lower alkyl, halogen, CN, lower alkyl substituted by halogen or O-lower alkyl substituted by halogen; R 4 is hydrogen or lower alkyl, aryl is phenyl or naphthyl; n is 1, 2 or 3; m is 1 or 2; and pharmaceutically acceptable acid addition salts and tautomeric forms thereof. It has been found that the compounds of formula I have a good activity on the 5-HT5A receptor. Therefore, the invention provides the use of a compound of formula I or a pharmaceutically acceptable salt thereof for the manufacture of medicaments for the treatment of certain CNS disorders.
摘要翻译：本发明涉及其中R 1为氢，低级烷基，低级烷氧基，卤素或被卤素取代的低级烷基的式（I）化合物; R是氢或卤素; 或R 1和R 2与它们所连接的碳原子一起-CH = CH-CH = CH-; R 2是氢，低级烷基，任选被卤素取代的苯基，或者是杂芳基，任选被低级烷基取代; R 3是氢，低级烷基，苯基，苄基，低级烯基，低级烷氧基，苯氧基，苄氧基，S-低级烷基，卤素，CN，被卤素取代的低级烷基或被卤素; R 4是氢或低级烷基，芳基是苯基或萘基; n为1,2或3; m为1或2; 和其药学上可接受的酸加成盐和互变异构体。已经发现式I化合物对5-HT5A受体具有良好的活性。因此，本发明提供式I化合物或其药学上可接受的盐在制备用于治疗某些CNS疾病的药物中的用途。

4. 发明申请

WO2003053954A1 BENZOTHIOPHENES AS ADENOSINE RECEPTOR MODULATORS 审中-公开
标题翻译：苯并噻吩作为腺苷受体调节剂
公开(公告)号：WO2003053954A1
公开(公告)日：2003-07-03
申请号：PCT/EP2002/013704
申请日：2002-12-04
申请人： F. HOFFMANN-LA ROCHE AG
发明人： ALANINE, Alexander , FLOHR, Alexander
IPC分类号： C07D333/66
CPC分类号： C07D409/12 , C07D333/66
摘要： The invention relates to compounds of the general formula (I), wherein R is phenyl, optionally substituted by halogen, or is pyridin 3-or 4-yl, optionally substituted by lower alkyl, or is -NR 1 R 2 , wherein R l and R 2 form together with the N atom to which they are attached heterocyclic rings, selected from the group consisting of morpholinyl, thiomorpholinyl, piperidinyl or piperazinyl, optionally substituted by -(CH 2 ) n -hydroxy, lower alkyl or lower alkoxy; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds of formula (I) have a good affinity to the A2A receptor and they are therefore useful for the treatment of diseases related to this receptor.
摘要翻译：本发明涉及通式（I）的化合物，其中R是任选被卤素取代的苯基，或者是被低级烷基或-NR 1 R 2取代的吡啶3-或4-基，其中R 1和R 2一起形成与它们所连接的N原子杂环，选自吗啉基，硫代吗啉基，哌啶基或哌嗪基，任选被 - （CH 2）n - 羟基，低级烷基或低级烷氧基取代; n为0,1或2; 及其药学上可接受的酸加成盐。已经表明式（I）化合物对A2A受体具有良好的亲和力，因此它们可用于治疗与该受体有关的疾病。

5. 发明申请

WO2007000393A1 8-ALK0XY-4-METHYL-3 , 4-DIHYDR0-QUINAZ0LIN-2-YL AMINES AND THEIR USE AS 5-HT5A RECEPTOR LIGANDS 审中-公开
标题翻译： 8-ALK0XY-4-甲基-3,4-二氢喹喔啉-2-基]胺及其作为5-HT5A受体配体的用途
公开(公告)号：WO2007000393A1
公开(公告)日：2007-01-04
申请号：PCT/EP2006/063269
申请日：2006-06-16
申请人： F. HOFFMANN-LA ROCHE AG , ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
发明人： ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
IPC分类号： C07D239/84 , A61K31/517
CPC分类号： C07D239/84
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen, halogen or lower alkyl; R 2 is lower alkyl or cycloalkyl; R 3 is hydrogen, lower alkyl, lower alkyl substituted by halogen, cycloalkyl or is benzyl, optionally substituted by halogen; n is 0, 1 or 2; and pharmaceutically acceptable acid addition salts thereof. The compounds of formula (I) may be used for the treatment of 5-HT 5A receptor antagonists related diseases, which are 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：本发明涉及其中R 1为氢，卤素或低级烷基的式（I）化合物; R 2是低级烷基或环烷基; R 3是氢，低级烷基，被卤素取代的低级烷基，环烷基或是任选被卤素取代的苄基; n为0,1或2; 及其药学上可接受的酸加成盐。式（I）化合物可用于治疗5-HT 5A受体拮抗剂相关疾病，其为抑郁症，焦虑症，精神分裂症，惊恐障碍，广场恐惧症，社交恐惧症，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，帕金森病痴呆，精神分裂症引起的帕金森综合征和迟发性运动障碍，为以及其他精神疾病和胃肠道疾病如肠易激综合征。

6. 发明申请

WO2006108773A1 (3,4-DIHYDRO-QUINAZOLIN-2-YL)-INDAN-1-YL-AMINES 审中-公开
标题翻译：（3,4-二氢 - 喹唑啉-2-基） - 茚满-1-基胺
公开(公告)号：WO2006108773A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/061279
申请日：2006-04-03
申请人： F. HOFFMANN-LA ROCHE AG , ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
发明人： ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
IPC分类号： C07D239/84 , A61K31/517 , A61P25/24
CPC分类号： C07D409/04 , C07D239/84 , C07D413/04
摘要： The present invention relates to compounds of formula (I) wherein R1 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkyl substituted by halogen; R2 is hydrogen, lower alkyl, aryl or hetaryl, wherein aryl and hetaryl may be optionally substituted by one or more substituents selected from the group consisting of lower alkyl or halogen; n is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of formula I have a good activity on the 5-HT5A receptor. Therefore, the invention provides the use of a compound of formula I for 5-HT5Areceptor related diseases.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，低级烷基，低级烷氧基，卤素或被卤素取代的低级烷基; R2是氢，低级烷基，芳基或杂芳基，其中芳基和杂芳基可以任选被一个或多个选自低级烷基或卤素的取代基取代; n为1或2; 及其药学上可接受的酸加成盐。已经发现式I化合物对5-HT5A受体具有良好的活性。因此，本发明提供式I化合物用于5-HT5受体相关疾病的用途。

7. 发明申请

WO2003037333A1 PYRIDINE DERIVATIVES AS NMDA-RECEPTOR SUBTYPE BLOCKERS 审中-公开
标题翻译：吡啶衍生物作为NMDA受体亚型阻断剂
公开(公告)号：WO2003037333A1
公开(公告)日：2003-05-08
申请号：PCT/EP2002/011782
申请日：2002-10-22
申请人： F. HOFFMANN-LA ROCHE AG
发明人： ALANINE, Alexander , BUETTELMANN, Bernd , HEITZ NEIDHART, Marie-Paule , PINARD, Emmanuel , WYLER, René
IPC分类号： A61K31/44
CPC分类号： C07D213/73 , C07D213/38 , C07D213/53 , C07D213/74 , C07D213/79 , C07D213/84 , C07D409/04
摘要： The present invention relates to compounds of formulas (IA) or (IB) wherein R 1 /R 2 independently from each other hydrogen, lower alkyl, -(CH 2 ) n NR 5 R 5' or -(CH 2 ) n+1 OH; R 5 and R 5' are independently from each hydrogen, lower alkyl; R 3 /R 4 are independently from each other hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl or hydroxy; Ar is phenyl or thiophenyl; the dotted line is -CH 2 -CH 2 -, -CH 2 -CHR'-, wherein R' is lower alkyl or are two hydrogen atoms, not forming a bridge and; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof, with the exception of 6-styryl-pyridin-2-yl-amine. The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and may be used in the treatment of diseases related to this receptor.
摘要翻译：本发明涉及式（IA）或（IB）的化合物，其中R 1彼此独立地为氢，低级烷基， - （CH 2）n - 2 ） n NR 5 或 - （CH ） n 1 OH; R 5和R 5'独立地为每个氢，低级烷基; R 3彼此独立地为氢，低级烷基，低级烷氧基，卤素，三氟甲基或羟基; Ar是苯基或噻吩基; 虚线是-CH 2 S 2 CH 2 - ， - CH 2 -S- CHR' - ，其中R'是低级烷基或两个氢原子，不形成桥; n为0,1或2; 和其药学上可接受的酸加成盐，但6-苯乙烯基 - 吡啶-2-基 - 胺除外。本发明的化合物是NMDA（N-甲基-D-天冬氨酸）受体亚型阻断剂，可用于治疗与该受体有关的疾病。

8. 发明申请

WO2002060877A1 IMIDAZOLE DERIVATIVES 审中-公开
标题翻译：咪唑衍生物
公开(公告)号：WO2002060877A1
公开(公告)日：2002-08-08
申请号：PCT/EP2002/000552
申请日：2002-01-21
申请人： F. HOFFMANN-LA ROCHE AG
发明人： ALANINE, Alexander , BUETTELMANN, Bernd , HEITZ NEIDHART, Marie-Paule , JAESCHKE, Georg , PINARD, Emmanuel , WYLER, Rene
IPC分类号： C07D233/54
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D233/84 , C07D249/08
摘要： The invention related to compounds of the general formula (I), wherein the substituents are defined in claim 1. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are therefore suitable in the control or treatment of diseases, related to this receptor.
摘要翻译：本发明涉及通式（I）的化合物，其中取代基如权利要求1中所定义。这些化合物对NMDA（N-甲基-D-天冬氨酸） - 受体亚型选择性阻断剂具有良好的亲和力，其具有关键在调节神经元活动和可塑性方面起作用，这使他们成为介导中枢神经系统发育过程以及学习和记忆形成的关键因素。因此，这些化合物适用于与该受体相关的疾病的控制或治疗。

9. 发明申请

WO2007000392A2 CHLORO-SUBSTITUTED GUANIDINES 审中-公开
标题翻译： CHLORO取代的股份有限公司
公开(公告)号：WO2007000392A2
公开(公告)日：2007-01-04
申请号：PCT/EP2006/063267
申请日：2006-06-16
申请人： F. HOFFMANN-LA ROCHE AG , ALANINE, Alexander , GOBBI, Luca, Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
发明人： ALANINE, Alexander , GOBBI, Luca, Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
CPC分类号： C07D239/42 , C07D403/12 , C07D405/12
摘要： The present invention relates to compounds of formula wherein R 1 is hydrogen or halogen; R 2 is lower alkyl; R 3 is hydrogen, lower alkyl, -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -phenyl optionally substituted by halogen, or is lower alkyl substituted by halogen, or is -(CH 2 ) n -heterocyclyl, -(CH 2 ) n N-di-lower alkyl, -(CH 2 ) n NHC(O)-lower alkyl, adamantly or -(CH 2 ) n -O-lower alkyl; n is 0, 1, 2 or 3; and pharmaceutically acceptable acid addition salts and tautomers thereof. It has been found that the compounds of formula I have a good activity on the 5-HT 5A receptor. Therefore, the invention provides the use of a compound of formula I or a pharmaceutically acceptable salt thereof for the treatment of diseases, related to this 15 receptor.
摘要翻译：本发明涉及下式的化合物，其中R 1是氢或卤素; R 2是低级烷基; R 3是氢，低级烷基， - （CH 2 CH 2）n - 环烷基， - （CH 2 CH 2）或者是被卤素取代的低级烷基，或者是 - （CH 2 CH 2）n - 杂环基， - （（O） - （CH 2）n N 2 - （CH 2）n - 低级烷基，金刚烷基或 - （CH 2）n - 低级烷基; n为0,1,2或3; 及其药学上可接受的酸加成盐和互变异构体。已经发现式I化合物在5-HT 5A受体上具有良好的活性。因此，本发明提供式I化合物或其药学上可接受的盐在治疗与该15受体有关的疾病中的用途。

10. 发明申请

WO2006097391A1 USE OF 2 -ANILINO - 3 , 4 -DIHYDRO - QUINAZOLINES AS 5HT5A RECEPTOR ANTAGONISTS 审中-公开
标题翻译：使用2-氨基-3,4-二氢喹诺酮作为5HT5A受体拮抗剂
公开(公告)号：WO2006097391A1
公开(公告)日：2006-09-21
申请号：PCT/EP2006/050762
申请日：2006-02-08
申请人： F. HOFFMANN-LA ROCHE AG , ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-uwe , STEWARD, Lucinda
发明人： ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-uwe , STEWARD, Lucinda
IPC分类号： A61K31/517 , C07D239/94
CPC分类号： A61K31/517 , C07D239/94
摘要： The present invention relates to the use of compounds of formula (I): wherein R1 is hydrogen, lower alkyl or halogen; R2 is hydrogen, lower alkyl, lower alkoxy, halogen, lower alkyl substituted by halogen or cyano; aryl is phenyl, naphthyl or indan-5-yl; n is 1 or 2; and pharmaceutically acceptable acid addition salts thereof for the manufacture of medicaments for the treatment of diseases related to the 5-HT5A receptor.
摘要翻译：本发明涉及式（I）化合物的用途：其中R 1是氢，低级烷基或卤素; R2是氢，低级烷基，低级烷氧基，卤素，被卤素或氰基取代的低级烷基; 芳基是苯基，萘基或茚满-5-基; n为1或2; 及其药学上可接受的酸加成盐，用于制备用于治疗与5-HT5A受体有关的疾病的药物。

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