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91. 发明公开

EP1455792A1 UREAS OF 2-AMINOBENZOTHIAZOLES AS ADENOSINE MODULATORS 有权
标题翻译： HARNSTOFE 2-氨基苯并作为腺苷调节剂
公开(公告)号：EP1455792A1
公开(公告)日：2004-09-15
申请号：EP02804578.9
申请日：2002-12-05
申请人： F. HOFFMANN-LA ROCHE AG
发明人： FLOHR, Alexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
IPC分类号： A61K31/5377 , A61K31/428 , A61P25/00
CPC分类号： A61K31/428 , A61K31/5377 , C07D277/82 , C07D417/12 , C07D451/06 , C07D453/06 , C07D471/10 , C07D487/10 , C07D491/08
摘要： The present invention relates to the use of compounds of the general formula (I) and to pharmaceutically acceptable acid addition salts thereof for the manufacture of medicaments for the treatment of diseases, related to the adenosine A2 receptor system like Alzheimer's disease, Parkinson disease, anxiety pain and other neurological disorders.

92. 发明公开

EP1448198A1 NICOTIN-OR ISONICOTIN BENZOTHIAZOLE DERIVATIVES 有权
标题翻译：烟酸或ISONICOTIN苯并噻唑衍生物
公开(公告)号：EP1448198A1
公开(公告)日：2004-08-25
申请号：EP02787632.5
申请日：2002-11-11
申请人： F. HOFFMANN-LA ROCHE AG
发明人： FLOHR, Alexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
IPC分类号： A61K31/4439 , C07D417/12 , C07D417/14
CPC分类号： C07D417/12 , C07D417/14
摘要： The present invention relates to compounds of the general formula(I) wherein R1 is phenyl, piperidin-1-yl or morpholinyl; A is-O-and R is-(CH¿2?)n-N(R')-C(O)-lower alkyl, -(CH2)n-O-lower alkyl, -(CH2)n-O-(CH2)n-O-lower alkyl, lower alkyl, -(CH2)n-morpholinyl, -(CH2)n-phenyl,-(CH2)n-N(R')2, (CH2)n-pyridinyl, -(CH2)n-CF3, (CH2)n-2-oxo-pyrrolidinyl or C4-6-cycloalkyl; R' is independently from each other hydrogen or lower alkyl and n is 1 or 2; or A is-N(R')-and R is lower alkyl, C4-6-cycloalkyl, -(CH2)n-O-lower alkyl, -(CH2)n-pyridinyl, -(CH2)n-piperidinyl, -(CH2)n-phenyl, (CH2)n-N(R')-C(O)-lower alkyl, -(CH2)n-morpholinyl, or (CH2)n-N(R')2; R' and R' are independently from each other hydrogen or lower alkyl and n is 1 or 2; or A is CH2- and R is-N(R')-(CH2)m-O-lower alkyl, -N(R')2 S-lower alkyl, or is acetidinyl, pyrrolidinyl or piperidinyl, which optionally substituted by hydroxy or lower alkoxy or is morpholinyl, -N(R')-CH2)m-C4-6-cycloalkyl, -N(R')-(CH2m-C(O)O-lower alkyl, -N(R')-(CH2)m-C(O)OH, -2-oxo pyrrolidinyl, -N(R')-C(O)O-lower alkyl, -O(CH2)m-O-lower alkyl or alkoxy; R' is independently from each other hydrogen or lower alkyl and m is 1, 2 or 3; A is S- and R is lower alkyl; or A-R are together piperazinyl, substituted by lower alkyl, -C(O)-lower alkyl or a oxo group, or is piperidinyl, substituted by lower alkoxy or hydroxy, or is morpholinyl, substituted by lower alkyl, or is C4-6-cycloalkyl, -azetidin-1-yl, optionally substituted by hydroxy or lower alkoxy, thiomorpholine-1,1-dioxo, -tetrahydopyran or 2-oxa-5-aza-bicyclo[2.2.1]hept-5-yl; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of general formula I are adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they are therefore useful in the treatment of diseases related to this receptor.

93. 发明授权

EP0837680B1 USE OF PHENOXY PYRIDINE DERIVATIVES FOR THE TREATMENT OF ILLNESSES CAUSED BY DISORDERS OF THE DOPAMINE SYSTEM 失效
标题翻译： PHENOXYPYRIDINDERIVATEN用于治疗由多巴胺系统的错误使用导致的疾病
公开(公告)号：EP0837680B1
公开(公告)日：2001-01-31
申请号：EP96921928.6
申请日：1996-06-04
申请人： F. HOFFMANN-LA ROCHE AG
发明人： GODEL, Thierry , HARTMAN, Deborah , RIEMER, Claus
IPC分类号： A61K31/44
CPC分类号： A61K31/4418
摘要： The invention is concerned with the use of compounds of general formula (I), wherein R signifies hydrogen, lower-alkyl, halogen, lower-alkoxy or nitro; R signifies hydrogen, lower alkyl or trifluoromethyl; and R signifies hydrogen, lower alkyl, trifluoromethyl, benzyl, hydroxy-lower-alkyl, lower alkoxy, lower-alkyl-carbonyl-amino, carbonyl-lower-alkyl, benzyl, di-lower-alkyl-amino-carbonyl, carbonyl-amino or amino-carbonyl-amino; or R and R together optionally signify a fused benzene ring and R signifies hydrogen or halogen, as well as pharmaceutically acceptable salts of compounds of general formula (I), for the treatment or prevention of illnesses which are caused by disorders of the dopamine system and, respectively, for the production of corresponding medicaments.

94. 发明公开

EP4263518A1 NEW QUINAZOLINONE DERIVATIVES 审中-实审
公开(公告)号：EP4263518A1
公开(公告)日：2023-10-25
申请号：EP21839167.0
申请日：2021-12-16
申请人： F. Hoffmann-La Roche AG
发明人： DOLENTE, Cosimo , HEWINGS, David Stephen , HUNZIKER, Daniel , KRUMMENACHER, Daniela , PETTAZZONI, Piergiorgio Francesco Tommaso , RICKLIN, Fabienne , RIEMER, Claus , WICHMANN, Juergen
IPC分类号： C07D401/06 , C07D401/14 , C07D403/12 , C07D239/90 , C07D239/91 , A61P35/00 , A61K31/517

95. 发明公开

EP4168392A1 SULFONE DERIVATIVES 审中-实审
公开(公告)号：EP4168392A1
公开(公告)日：2023-04-26
申请号：EP21733139.6
申请日：2021-06-21
申请人： F. Hoffmann-La Roche AG
发明人： BELL, Andrew, Simon , BESNARD, Jérémy , BRADLEY, Anthony, Richard , GREEN, Luke , HAAP, Wolfgang , KOCER, Buelent , KUGLSTATTER, Andreas , LUCAS, Xavier , MATTEI, Patrizio , MAZUNIN, Dmitry , RIEMER, Claus , VAN HOORN, Willem Paul
IPC分类号： C07D231/56 , C07D487/04 , A61P35/00 , A61K31/416

96. 发明公开

EP2364295A1 3-(BENZYLAMINO)-PYRROLIDINE DERIVATIVES AND THEIR USE AS NK-3 RECEPTOR ANTAGONISTS 有权
标题翻译： 3-（苄基氨基）吡咯烷及其作为NK-3受体拮抗剂
公开(公告)号：EP2364295A1
公开(公告)日：2011-09-14
申请号：EP09737458.1
申请日：2009-10-26
申请人： F. Hoffmann-La Roche AG
发明人： BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D207/14 , A61K31/401 , A61K31/4025 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D491/08
CPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D491/08
摘要： The present invention relates to a compounds of formula I wherein Ar is aryl; R
1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano, amino, mono or di-lower alkyl amino, C(O)-lower alkyl, or is aryl or heteroaryl; R
2 is hydrogen or halogen; R
3 is -(CH
2 )
p -heterocyclyl, optionally substituted by one or two substituents R
4 ; or is lower alkyl, lower alkoxy, -(CH
2 )
p -O-lo wer alkyl, -(CH
2 )
P -CN, -O-(CH
2 )
p -CN, -(CH
2 )
p -heteroaryl, -(CH
2 )
p -C(O)-heteroaryl, -O-(CH
2 )
p -heterocyclyl, -(CH
2 )
p -aryl, optionally substituted by lower alkoxy or halogen, -(CH
2 )
p -O-aryl, optionally substituted by lower alkyl, -(CH
2 )
p -NR'-heterocyclyl, optionally substituted by lower alkyl, -CH
2 )
p -NR'R", -CH
2 )
p -NR'-CH
2 )
p' -NR'R", -CH
2 )
p -NR'-CH
2 )
p' -CN, -CH
2 )
p -C(O)-NR'R" or is -O-(CH
2 )
p -NR'R"; R
4 is hydroxy, lower alkyl, -(CH
2 )
P -OH, -(CH
2 )
P -NR'R", -NR'-C(O)-lower alkyl, -(CH
2 )
p -CN, -S(O)
2 -lower alkyl, -NR'-S(O)
2 -lower alkyl, -S(O)2-NR'R", -C(O)-lower alkyl, -C(O)-lower cycloalkyl, wherein the cycloalkyl may be substituted by lower alkyl, or is -C(O)-NR'R", heterocyclyl, optionally substituted by =0, or is heteroaryl, optionally substituted by alkoxy or cyano, or is aryl optionally substituted by alkoxy, cyano or is 2-oxa-5-aza-bicyclo[2.2.1]hept-5-yl; R' and R' ' are independently from each other hydrogen, lower alkyl or -(CH
2 )
P -OH; n is 1 or 2; in case n is 1 or 2, R
1 may be the same or different; o is 1 or 2; in case o is 1 or 2, R
2 may be the same or different; p,p' are the same or different and are O, 1, 2 3 or 4; or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

97. 发明授权

EP2185540B1 PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 有权
标题翻译： PYRROLIDINARYLETHER AS NK-3受体拮抗剂
公开(公告)号：EP2185540B1
公开(公告)日：2011-07-20
申请号：EP08786547.3
申请日：2008-07-29
申请人： F. Hoffmann-La Roche AG
发明人： JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , WU, Xihan
IPC分类号： C07D401/08 , C07D401/06
CPC分类号： C07D401/06 , C07D401/08
摘要： The invention relates to a compound of general formula (I) wherein Ar1 is aryl or a five or six membered heteroaryl; Ar2 is aryl or a five or six membered heteroaryl; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, -S(O)2-lower alkyl, -S(O)2-di-lower alkyl amino, -(CH2)qR, cyano, amino, mono or di-lower alkyl amino, NHC(O)-lower alkyl, cycloalkyl or is or a five membered heteroaryl, optionally substituted by lower alkyl; wherein R is cyano, di-lower alkyl amino or pyrrolidin-1-yl; R2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R3 is hydrogen or lower alkyl or CH2OH; R4 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; n is 1, 2 or 3; in case n is 2 or 3, R1 may be the same or different; o is 1, 2 or 3; in case o is 2 or 3, R2 may be the same or different; p is 1, 2 or 3; in case p is 2 or 3, R4 may be the same or different; q is 1 or 2; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

98. 发明公开

EP2294063A1 PYRROLIDINE ETHER DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 有权
标题翻译：作为NK3受体拮抗剂的吡咯烷衍生物
公开(公告)号：EP2294063A1
公开(公告)日：2011-03-16
申请号：EP09761673.4
申请日：2009-06-08
申请人： F. Hoffmann-La Roche AG
发明人： JABLONSKI, Philippe , KAWASAKI, Kenichi , KNUST, Henner , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D401/12 , C07D401/14 , A61K31/445 , A61P25/00
CPC分类号： C07D401/14 , C07D401/12
摘要： The present invention relates to a compounds of formula I wherein R
1 , R
2 , R
3 , R', Ar, o, n and m are as defined in the specification. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，R 3，R'，Ar，o，n和m如说明书中所定义。已经发现本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意力缺陷多动症（ADHD）的高潜力NK-3受体拮抗剂。

99. 发明公开

EP2254666A1 2-AMINOQUINOLINES AS 5-HT5A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2-氨基喹啉AS 5-HT 5A受体拮抗剂
公开(公告)号：EP2254666A1
公开(公告)日：2010-12-01
申请号：EP09720136.2
申请日：2009-03-03
申请人： F. Hoffmann-La Roche AG
发明人： KOLCZEWSKI, Sabine , RIEMER, Claus , ROCHE, Olivier , STEWARD, Lucinda , WICHMANN, Juergen , WOLTERING, Thomas
IPC分类号： A61P3/06 , A61P25/00 , A61K31/4709 , C07D215/38 , C07D405/12
CPC分类号： C07D405/12 , C07D215/38 , C07D491/08
摘要： The present invention is concerned with 2-Aminoquinoline derivatives as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders. In particular, the present invention is concerned with compounds of the general formula (I) wherein R and R are as described herein.

100. 发明公开

EP2195296A1 QUINOLINE DERIVATIVES AS 5HT5A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： CHINOLINDERIVATE ALS 5HT5A-REZEPTORANTAGONISTEN
公开(公告)号：EP2195296A1
公开(公告)日：2010-06-16
申请号：EP08804358.3
申请日：2008-09-18
申请人： F. Hoffmann-La Roche AG
发明人： KOLCZEWSKI, Sabine , RIEMER, Claus , STEWARD, Lucinda , WICHMANN, Juergen , WOLTERING, Thomas
IPC分类号： C07D215/38 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/12 , A61K31/4709 , A61K31/506 , A61P25/18 , A61P25/22 , A61P25/24
CPC分类号： C11D11/0017 , C07D215/38 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/12 , C11D3/001 , C11D3/50 , C11D3/502 , C11D17/0086
摘要： The present invention relates to 2-Aminoquinoline derivatives which are represented by the general formula I wherein R1, R2 and R3 are as defined in the specification as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译：本发明涉及式I的2-氨基喹啉，其中R1，R2和R3如说明书中所定义，作为5-HT5A受体拮抗剂，其制备方法，含有它们的药物组合物及其用于治疗CNS障碍的用途。

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