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公开(公告)号：EP2035394B1
公开(公告)日：2009-08-19
申请号：EP07765355.8
申请日：2007-06-11
发明人： HEBEISEN, Paul , IDING, Hans , NETTEKOVEN, Matthias Heinrich , OBST SANDER, Ulrike , ROEVER, Stephan , WEISS, Urs , WIRZ, Beat
IPC分类号： C07D241/24 , C07D241/26 , C07D401/12 , C07D403/12 , C07D405/12 , A61K31/497 , A61P25/32
CPC分类号： C07D241/26 , C07D241/24 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention relates to compounds of the formula (I) wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.
摘要翻译： 本发明涉及其中R 1至R 8如说明书和权利要求书中所定义的式（I）化合物及其药学上可接受的盐。 该化合物可用于治疗和/或预防与CB1受体调节相关的疾病，如肥胖。
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12.发明授权ENZYMATIC PROCESS FOR THE PREPARATION OF SUBSTITUTED 2-AMINO-3-(2-AMINO-PHENYLSULFANYL)-PROPIONIC ACID 有权酶促过程用于生产取代的2-氨基-3-（2-氨基 - 苯基硫烷基） - 丙
公开(公告)号：EP1434870B1
公开(公告)日：2006-12-27
申请号：EP02779375.1
申请日：2002-09-19
发明人： BLEICHER, Konrad , BORTHWICK, Scott , IDING, Hans , ROGERS-EVANS, Mark , SCHMID, Stefan , TONG, Han, Min , WIRZ, Beat
IPC分类号： C12P13/04 , C12P11/00 , C07C323/63
CPC分类号： C12P13/04 , C07C323/59 , C07C323/63 , C07D285/36 , C12P11/00 , C12P41/005
摘要： The compounds of formula (I) are useful for the preparation of 1,5-benzothiazepines which are useful as enzyme inhibitors, such as protease, interleukin-1β-converting enzyme, elastase or angiotensin enzyme, GPCR antagonists (cholecystokinin, angiotensin II receptor). The present invention relates to a new process for the preparation compounds of formula (I), wherein R?1, R2, R3¿ and n are as described in the description which process comprises reacting compounds of formula (II), wherein R?1, R2, R3¿, n and R4 are as described in the description, with a protease in an aqueous system containing an organic co-solvent.
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13.发明授权N-SUBSTITUTED-1H-INDOL-5-PROPIONIC ACID COMPOUNDS AS PPAR AGONISTS USEFUL FOR THE TREATMENT OF DIABETES 有权N-取代的-1H-吲哚-5-丙烷羧酸化合物AS PPAR激动剂用于治疗糖尿病
公开(公告)号：EP1539746B1
公开(公告)日：2006-11-15
申请号：EP03747962.3
申请日：2003-09-04
发明人： BINGGELI, Alfred , GRETHER, Uwe , HILPERT, Hans , HUMM, Roland , IDING, Hans , KUHN, Bernd , MAERKI, Hans-Peter , MEYER, Markus , MOHR, Peter , WIRZ, Beat
IPC分类号： C07D413/06 , A61K31/405 , C07D413/14 , C07D417/06 , A61P3/06 , A61P3/10 , A61P9/10
CPC分类号： C07D413/06 , C07D417/06
摘要： Compounds of formula (I), as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R8, A, A1 and n have the significance given in claim 1 can be used in the form of pharmaceutical preparations.
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公开(公告)号：EP3626710A1
公开(公告)日：2020-03-25
申请号：EP19191353.2
申请日：2015-09-25
发明人： GOSSELIN, Francis , HAN, Chong , IDING, Hans , REENTS, Reinhard , SAVAGE, Scott , WIRZ, Beat
IPC分类号： C07D239/46
摘要： The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5 H -cyclopenta[ d ] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib ( i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5 H -cyclopenta[ d ]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.
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公开(公告)号：EP3283622B1
公开(公告)日：2019-07-03
申请号：EP16717321.0
申请日：2016-04-13
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公开(公告)号：EP3283622A1
公开(公告)日：2018-02-21
申请号：EP16717321.0
申请日：2016-04-13
发明人： BORNSCHEUER, Uwe , HANLON, Steven Paul , IDING, Hans , PAVLIDIS, Ioannis , SPURR, Paul , STEFFEN WEISS, Martin , WIRZ, Beat
CPC分类号： C12N9/1096 , C07K2319/00 , C07K2319/21 , C12N1/16 , C12N1/20 , C12P13/001 , C12Y206/01
摘要： The present invention relates to a mutant transaminase with increased transaminase activity relative to the wild-type transaminase, a fusion protein comprising the transaminase, a polynucleotide coding for the transaminase, a host cell comprising the polynucleotide, mutant transaminase and/or fusion protein, a method of producing an amine with the mutant transaminase or fusion protein and the use of the mutant transaminase or fusion protein for the production of an amine.
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17.发明公开PROCESSES FOR THE PREPARATION OF (3R, 4R) -N- (4 -CHLOROPHENYL) -1- (2, 2-DIFLUOROETHYL) -N' - [2-FLUORO-4- (2-OXO-1 (2H) -PYRIDINYL) PHENYL]-3, 4-PYRROLIDINEDICARBOXAMIDE 审中-公开制备（3R，4R）-N-（4-氯苯基）-1-（2,2-二氟乙基）-N' - [2-氟-4-（2-氧代-1（2H） - 吡啶基] ）苯基] -3,4-吡咯烷二甲酰胺
公开(公告)号：EP2097401A1
公开(公告)日：2009-09-09
申请号：EP07857495.1
申请日：2007-12-12
发明人： ADAM, Jean-Michel , DOTT, Pascal , IDING, Hans , MAIR, Hans-Juergen , REENTS, Reinhard , WIRZ, Beat
IPC分类号： C07D401/12 , C07D401/14
CPC分类号： C07D401/12 , C07D401/14
摘要： The invention is concerned with processes for the manufacture of pyrrolidine-3,4- dicarboxamide derivative of formula (I), and the intermediates useful for those processes.
摘要翻译： 本发明涉及制备式（I）的吡咯烷-3,4-二甲酰胺衍生物的方法，以及用于那些方法的中间体。
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公开(公告)号：EP1877404A2
公开(公告)日：2008-01-16
申请号：EP06777206.1
申请日：2006-04-24
发明人： GROEBKE-ZBINDEN, Katrin , HAAP, Wolfgang , HILPERT, Hans , PANDAY, Narendra , RICKLIN, Fabienne , WIRZ, Beat
IPC分类号： C07D409/14 , C07D413/14 , C07D401/14 , C07D513/04 , C07D207/16 , C07D207/14 , C07D207/12 , A61K31/4025 , A61P7/02
CPC分类号： C07D207/12 , C07D207/14 , C07D207/16 , C07D401/14 , C07D409/14 , C07D413/14 , C07D513/04
摘要： The invention is concerned with novel cyclic amines of formula (I) wherein X1 to X3, Y1 to Y3, R1’ , R1’’ and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
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公开(公告)号：EP1868999A1
公开(公告)日：2007-12-26
申请号：EP06725329.4
申请日：2006-03-27
发明人： HEBEISEN, Paul , IDING, Hans , NETTEKOVEN, Matthias Heinrich , OBST, Ulrike , ROEVER, Stephan , WIRZ, Beat
IPC分类号： C07D213/64 , C07D213/74 , A61P25/34 , A61P3/00 , A61K31/465
CPC分类号： C07D213/64 , C07D213/74 , C07D213/82 , C07D401/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of the formula (I) wherein X and R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.
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公开(公告)号：EP0316374B1
公开(公告)日：1991-07-31
申请号：EP88903165.4
申请日：1988-05-02
发明人： SCHMID, Rudolf , WIRZ, Beat
IPC分类号： C07C69/16 , C07C69/28 , C07C31/13 , C12P1/00 , C07D311/94
CPC分类号： C12P41/004 , C12P7/62
摘要： New optically active compounds, namely optically active derivatives of 2-methyl-1,3-propanediol, have formula (I), where R is a C1-10 alkyl, in particular a C1-5 alkyl. A microbial process for their manufacture is also described. The compounds (I) are valuable intermediate products, in particular in the manufacture of vitamin E.
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