专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

3. 发明公开

EP4291558A1 BICYCLIC TETRAHYDROAZEPINE DERIVATIVES FOR THE TREATMENT OF CANCER 审中-实审
公开(公告)号：EP4291558A1
公开(公告)日：2023-12-20
申请号：EP22706272.6
申请日：2022-02-10
申请人： F. Hoffmann-La Roche AG
发明人： BRITSCHGI, Adrian , HUTTER, Roman , KUEHNE, Holger , KUHN, Bernd , LUEBBERS, Thomas , MARTIN, Laetitia Janine , MUELLER, Barbara Johanna , WICHMANN, Juergen , BRANDSTAETTER, Marco
IPC分类号： C07D417/10 , C07D417/14 , C07D513/04 , C07D519/00 , A61P35/00 , A61K31/554

4. 发明授权

EP2334665B1 MODULATORS FOR AMYLOID BETA 有权
标题翻译： AMYLOID BETA调制器
公开(公告)号：EP2334665B1
公开(公告)日：2013-07-10
申请号：EP09783515.1
申请日：2009-09-29
申请人： F. Hoffmann-La Roche AG
发明人： GOETSCHI, Erwin , JOLIDON, Synese , LUEBBERS, Thomas
IPC分类号： C07D401/14 , C07D403/12 , A61P25/28 , A61K31/53
CPC分类号： C07D413/14 , C07D401/14 , C07D403/12 , C07D403/14

5. 发明公开

EP2334665A1 MODULATORS FOR AMYLOID BETA 有权
标题翻译：调节剂类淀粉样蛋白-β
公开(公告)号：EP2334665A1
公开(公告)日：2011-06-22
申请号：EP09783515.1
申请日：2009-09-29
申请人： F. Hoffmann-La Roche AG
发明人： GOETSCHI, Erwin , JOLIDON, Synese , LUEBBERS, Thomas
IPC分类号： C07D401/14 , C07D403/12 , A61P25/28 , A61K31/53
CPC分类号： C07D413/14 , C07D401/14 , C07D403/12 , C07D403/14
摘要： The invention relates to compounds of formula (I) wherein R
1 is hydrogen, lower alkyl or is lower alkyl substituted by hydroxy; R
2 is hydrogen, lower alkoxy or lower alkyl; R
3 /R
4 are independently from each other hydrogen, halogen, lower alkyl, C(O)O-lower alkyl, OR', NR''R"', lower alkyl substituted by halogen or hydroxy, or is phenyl or benzyl, optionally substituted by one or two halogen atoms; R' is lower alkyl, or is phenyl, benzyl or pyridinyl, which rings are optionally substituted by one or more halogen, lower alkyl or lower alkyl substituted by fluoro; R'' is hydrogen or lower alkyl; R'" is lower alkyl, lower alkyl substituted by one or two hydroxy groups, CH(CH
2 OH)-phenyl, or is -(CH
2 )
2 O-lower alkyl, or is phenyl substituted by halogen, or R'' and R''' form together with the N-atom to which they are attached a heterocyclic ring, optionally substituted by one or more lower alkyl, CH
2 C(O)O-lower alkyl, or by CH
2 C(O)OH; Ar is a fϊve-membered heteroaryl group; or to pharmaceutically active acid addition salts. It has been found that the present compounds of formula (I) are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

6. 发明授权

EP1888538B1 (3,4-DIHYDRO-QUINAZOLIN-2-YL)-(2-ARYLOXY-ETHYL)-AMINES HAVING AN ACTIVITY ON THE 5-HT RECEPTOR 有权
标题翻译：（3,4-二氢喹唑啉-2-基） - WITH活性（2-芳氧基 - 乙基）胺在5-HT受体
公开(公告)号：EP1888538B1
公开(公告)日：2009-11-18
申请号：EP06754806.5
申请日：2006-04-24
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 , 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 R1 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkyl substituted by halogen; R is hydrogen or halogen; or R1 and R are together with the carbon atom to which they are attached -CH=CH-CH=CH-; R2 is hydrogen, lower alkyl, phenyl optionally substituted by halogen, or is hetaryl, optionally substituted by lower alkyl; R3 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; R4 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.

7. 发明公开

EP1899307A1 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-羟基-4-甲基-3,4-二氢-D-喹唑啉-2-基胺及其作为5-HT5A受体配体的用途
公开(公告)号：EP1899307A1
公开(公告)日：2008-03-19
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.
摘要翻译：本发明涉及式（I）的化合物，其中R 1为氢，卤素或低级烷基; R2是低级烷基或环烷基; R3为氢，低级烷基，被卤素取代的低级烷基，环烷基或为苄基，其任选被卤素取代; n是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，所述相关疾病为抑郁症，焦虑症，精神分裂症，恐慌症，广场恐怖症，社交恐怖症，强迫症，创伤后应激障碍，疼痛，记忆障碍，进食行为障碍，性功能障碍，睡眠障碍，戒断药物，运动障碍如帕金森病，帕金森病痴呆，精神安定药诱导的帕金森综合征和迟发性运动障碍，以及其他精神障碍和胃肠疾病如肠易激综合征。

8. 发明公开

EP1888538A1 (3,4-DIHYDRO-QUINAZOLIN-2-YL)-(2-ARYLOXY-ETHYL)-AMINES HAVING AN ACTIVITY ON THE 5-HT RECEPTOR 有权
标题翻译：（3,4-二氢喹唑啉-2-基） - WITH活性（2-芳氧基 - 乙基）胺在5-HT受体
公开(公告)号：EP1888538A1
公开(公告)日：2008-02-20
申请号：EP06754806.5
申请日：2006-04-24
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 , 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 R1 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkyl substituted by halogen; R is hydrogen or halogen; or R1 and R are together with the carbon atom to which they are attached -CH=CH-CH=CH-; R2 is hydrogen, lower alkyl, phenyl optionally substituted by halogen, or is hetaryl, optionally substituted by lower alkyl; R3 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; R4 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.

9. 发明授权

EP2812322B1 NOVEL AZETIDINE DERIVATIVES 有权
标题翻译：新的偶氮衍生物
公开(公告)号：EP2812322B1
公开(公告)日：2017-12-06
申请号：EP13702070.7
申请日：2013-02-04
申请人： F. Hoffmann-La Roche AG
发明人： ANSELM, Lilli , BANNER, David , HAAP, Wolfgang , KUHN, Bernd , LUEBBERS, Thomas , PETERS, Jens-Uwe , SPINNLER, Beat
IPC分类号： C07D401/14 , A61K31/4439 , A61P3/00
CPC分类号： C07D401/14

10. 发明授权

EP2155740B1 HETARYLANILINES AS MODULATORS FOR AMYLOID BETA 失效
标题翻译： HETARYLANILINE AS调节剂的β淀粉样蛋白
公开(公告)号：EP2155740B1
公开(公告)日：2011-01-26
申请号：EP08749887.9
申请日：2008-04-30
申请人： F. Hoffmann-La Roche AG
发明人： BAUMANN, Karlheinz , FLOHR, Alexander , JACOBSEN, Helmut , JOLIDON, Synese , LUEBBERS, Thomas
IPC分类号： C07D417/12 , C07D513/04 , A61K31/427 , A61K31/428 , A61K31/429 , A61P25/28
CPC分类号： C07D513/04 , C07D417/12
摘要： The invention relates to compounds of formula (I) : wherein hetaryl I is formula (II); hetaryl II is formula (III); or to pharmaceutically active acid addition salts. It has been found that the present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式