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1. 发明公开

EP3609904A1 ANTI-BACTERIAL PEPTIDE MACROCYCLES AND USE THEREOF 有权
公开(公告)号：EP3609904A1
公开(公告)日：2020-02-19
申请号：EP18717558.3
申请日：2018-04-09
申请人： F. Hoffmann-La Roche AG
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

2. 发明公开

EP1861102A1 USE OF 2-ANILINO-3,4-DIHYDRO-QUINAZOLINES AS 5HT5A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2-苯胺-3,4-二氢喹唑啉AS-HT 5A受体拮抗剂的用途
公开(公告)号：EP1861102A1
公开(公告)日：2007-12-05
申请号：EP06708108.3
申请日：2006-02-08
申请人： F. Hoffmann-La Roche AG
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.

3. 发明授权

EP1224174B1 BENZODIAZEPINE DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS 有权
标题翻译：苯二氮衍生物及其作为代谢型谷氨酸受体拮抗剂的用途
公开(公告)号：EP1224174B1
公开(公告)日：2003-09-17
申请号：EP00969347.4
申请日：2000-09-29
申请人： F. HOFFMANN-LA ROCHE AG
发明人： ADAM, Geo , ALANINE, Alexander , GOETSCHI, Erwin , MUTEL, Vincent , WOLTERING, Thomas, Johannes
IPC分类号： C07D243/12 , A61K31/55 , A61P43/00 , C07D409/04 , C07D405/04 , C07D417/04 , C07D401/04 , C07D403/10 , C07D401/14 , C07D417/14 , C07D413/10 , C07D405/06 , C07D401/06 , C07D417/10 , C07F7/10
CPC分类号： C07D243/12
摘要： The present invention relates to compounds of general formula (I) wherein X is a single bond or an ethynediyl group, wherein, in case X is a single bond, R1 is halogen or phenyl which is optionally substituted with halogen, lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, or cyano; In case X is an ethynediyl group, R1 is phenyl, optionally substituted with halogen, lower alkyl, halo-lower alkyl, lower cycloalkyl, lower alkoxy or halo-lower alkoxy; R3 is a 5 or 6 membered aryl or heteroaryl which are optionally substituted. The compounds according to the present invention can be used for treating or preventing acute and/or chronic neurological disorders such as psychosis, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits.

4. 发明授权

EP1899307B1 8-ALK0XY-4-METHYL-3, 4-DIHYDR0-QUINAZ0LIN-2-YL AMINES AND THEIR USE AS 5-HT5A RECEPTOR LIGANDS 有权
标题翻译： 8 ALK0XY -4-甲基-3-，4- DIHYDR0-CHINAZ0LIN -2-基胺及其作为5-HT 5A受体配体
公开(公告)号：EP1899307B1
公开(公告)日：2010-06-30
申请号：EP06777337.4
申请日：2006-06-16
申请人： F. Hoffmann-La Roche AG
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 R1 is hydrogen, halogen or lower alkyl; R2 is lower alkyl or cycloalkyl; R3 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-HT5A 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.

5. 发明授权

EP1899306B1 CHLORO-SUBSTITUTED GUANIDINES 有权
标题翻译：氯取代的瓜氨酸
公开(公告)号：EP1899306B1
公开(公告)日：2008-10-15
申请号：EP06777336.6
申请日：2006-06-16
申请人： F. Hoffmann-La Roche AG
发明人： ALANINE, Alexander , GOBBI, Luca, Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
IPC分类号： C07D239/84
CPC分类号： C07D239/42 , C07D403/12 , C07D405/12
摘要： The present invention relates to compounds of formula wherein R1 is hydrogen or halogen; R2 is lower alkyl; R3 is hydrogen, lower alkyl, -(CH2)n-cycloalkyl, -(CH2)n-phenyl optionally substituted by halogen, or is lower alkyl substituted by halogen, or is -(CH2)n-heterocyclyl, -(CH2)nN-di-lower alkyl, -(CH2)nNHC(O)-lower alkyl, adamantly or -(CH2)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-HT5A 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; R2是低级烷基; R 3是氢，低级烷基， - （CH 2）n - 环烷基， - （CH 2）n - 苯基，其任选被卤素取代，或者是被卤素取代的低级烷基，或是 - （CH 2）n - 杂环基， - （CH 2） - （CH2）nNHC（O） - 低级烷基，金刚烷基或 - （CH2）nO-低级烷基; n是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化合物对5-HT 5A受体具有良好的活性。因此，本发明提供了式I化合物或其药学上可接受的盐在治疗与该受体有关的疾病中的用途。

6. 发明公开

EP1358165A1 IMIDAZOLE DERIVATIVES 有权
标题翻译：咪唑衍生物
公开(公告)号：EP1358165A1
公开(公告)日：2003-11-05
申请号：EP02714095.3
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 , C07D233/61 , C07D233/84 , C07D401/06 , A61K31/4164 , A61P25/28
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，其具有键在调节神经元活动和可塑性方面起作用，这使得它们成为介导中枢神经系统发育过程以及学习和记忆形成过程的关键参与者。因此这些化合物适用于控制或治疗与该受体有关的疾病。

7. 发明公开

EP3368544A1 PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII 有权
公开(公告)号：EP3368544A1
公开(公告)日：2018-09-05
申请号：EP16785469.4
申请日：2016-10-24
申请人： F. Hoffmann-La Roche AG
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 X1 to X8 and R1 to R8 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.

8. 发明授权

EP1456196B1 BENZOTHIOPHENES AS ADENOSINE RECEPTOR MODULATORS 有权
标题翻译：苯并二氢S。。。。。。。。。。
公开(公告)号：EP1456196B1
公开(公告)日：2009-01-07
申请号：EP02792882.9
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 , A61K31/38 , A61P25/28 , A61P25/24 , A61P25/16
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 -NR1R2, wherein Rl and R2 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 -(CH2) 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.

9. 发明授权

EP1313703B1 PRODRUGS TO NMDA RECEPTOR LIGANDS 有权
标题翻译：的前药NMDA受体配体
公开(公告)号：EP1313703B1
公开(公告)日：2008-02-13
申请号：EP01965201.5
申请日：2001-08-20
申请人： F. HOFFMANN-LA ROCHE AG
发明人： ALANINE, Alexander , BUETTELMANN, Bernd , FISHER, Holger , HEITZ NEIDHART, Marie-Paule , HUWYLER, Joerg , JAESCHKE, Georg , PINARD, Emmanuel , WYLER, Rene
IPC分类号： C07D211/42 , A61K31/445 , A61P25/28 , C07F9/59
CPC分类号： C07D211/42 , C07F9/591
摘要： The invention relates to compounds of the general formula (I) wherein R is a) -C(O)(CH2)nC(O)OH, b) wherein R1 is -N(R?2)(R3) and R2/R3¿ are independently from each other hydrogen or lower alkyl, or is a cyclic tertiary amine, optionally substituted by lower alkyl, c) -P(O)(OH)¿2?, or is d) -C(O)(CH)2)nNHC(O)(CH2)nN(R?2)(R3¿); and n is 1, 2, 3 or 4; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used as prodrugs for the parentcompound of formula (II) which are useful in the treatment of NMDA receptor-related diseases.

10. 发明授权

EP1224175B1 BENZODIAZEPINE DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS 有权
标题翻译：苯二氮衍生物及其作为代谢型谷氨酸受体拮抗剂的用途
公开(公告)号：EP1224175B1
公开(公告)日：2004-03-17
申请号：EP00971302.5
申请日：2000-09-29
申请人： F. HOFFMANN-LA ROCHE AG
发明人： ADAM, Geo , ALANINE, Alexander , GOETSCHI, Erwin , MUTEL, Vincent , WOLTERING, Thomas, Johannes
IPC分类号： C07D243/12 , A61K31/55 , A61P43/00 , C07D409/04 , C07D405/04 , C07D417/04 , C07D401/04 , C07D403/10 , C07D401/14 , C07D417/14 , C07D413/10 , C07D405/06
CPC分类号： C07D401/04 , C07D243/12 , C07D403/10 , C07D405/06 , C07D413/10 , C07D417/06 , C07D417/10
摘要： The present invention relates to compounds of general formula (I) wherein R3 is phenyl; pyridine; thiophenyl or thiazolyl, which are optionally substituted. The compounds according to the present invention can be used for treating or preventing acute and/or chronic neurological disorders such as psychosis, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits.

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