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公开(公告)号：AT522529T
公开(公告)日：2011-09-15
申请号：AT07803228
申请日：2007-09-05
Applicant: HOFFMANN LA ROCHE
Inventor： ABRECHT STEFAN , ADAM JEAN-MICHEL , FETTES ALEC , HILDBRAND STEFAN
IPC: C07D471/04
Abstract: This invention relates to a process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula wherein R1, R2, R3 and R4 are defined in the specification, comprising the optical resolution of an enamine of the formula wherein R1 is lower alkyl, in the presence of an optical active resolving agent to form an (S)-enamine salt of the formula wherein RCO2- is the conjugate base of the resolving agent.
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公开(公告)号：AU2006226447B2
公开(公告)日：2009-07-16
申请号：AU2006226447
申请日：2006-03-09
Applicant: HOFFMANN LA ROCHE
Inventor： RUF ARMIN , ABRECHT STEFAN , BUBENDORF ANDRE GERARD , GOETZOE STEPHAN , MOOG REGINA , MONTAVON FRANCOIS , SCALONE MICHELANGELO , GRASSMANN OLAF , ROHRER FRANZISKA , SCHWITTER URS , WANG SHAONING
IPC: A61K31/422 , A61P3/04 , A61P3/10 , C07D413/12
Abstract: The invention is concerned with (S)-1-{[2-(5-Methyl-2-phenyl-oxazol-4-yl)-ethylamino]-acetyl}-pyrrolidine-2-carbonitrile mesylate and crystalline polymorphs of this compound. This compound and its polymorphic forms exhibits superior properties compared to the previously known compounds and can be used as medicament for the treatment of disorders which are associated with DPP-IV.
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公开(公告)号：DE602006002612D1
公开(公告)日：2008-10-16
申请号：DE602006002612
申请日：2006-05-15
Applicant: HOFFMANN LA ROCHE
Inventor： ABRECHT STEFAN , ADAM JEAN-MICHEL , FETTES ALEC , FORICHER JOSEPH , LOHRI BRUNO , MATTEI PATRIZIO , MOINE GERARD , SCHMID RUDOLF , ZUTTER ULRICH
IPC: C07D307/32 , C07D307/38
Abstract: This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula and with its use for the manufacture of pyrido[2,1-a]isoquinoline derivatives of the formula which are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.
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公开(公告)号：CA2662413A1
公开(公告)日：2008-03-20
申请号：CA2662413
申请日：2007-09-05
Applicant: HOFFMANN LA ROCHE
Inventor： HILDBRAND STEFAN , FETTES ALEC , ADAM JEAN-MICHEL , ABRECHT STEFAN
IPC: C07D471/04
Abstract: This invention relates to a process for the preparation of pyrido[2,1-a] isoquinoline derivatives of the Formula (I), wherein R1, R2, R3 and R4 are d efined in the specification, comprising the optical resolution of an enamine of the Formula (II), wherein R1 is lower alkyl, in the presence of an optic al active resolving agent to form an (S)-enamine salt of the Formula (III), wherein RCO2- is the conjugate base of the resolving agent.
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公开(公告)号：MX2007011546A
公开(公告)日：2007-10-19
申请号：MX2007011546
申请日：2006-03-09
Applicant: HOFFMANN LA ROCHE
Inventor： SCALONE MICHELANGELO , WANG SHAONING , ABRECHT STEFAN , SCHWITTER URS , ROHRER FRANZISKA , BUBENDORF ANDRE GERARD , GOETZOE STEPHAN , GRASSMANN OLAF , MONTAVON FRANCOIS , MOOG REGINA , RUF ARMIN
IPC: C07D413/12 , A61K31/422 , A61P3/04 , A61P3/10
Abstract: La invencion se refiere al mesilato del (S)-1-{[2-(5-metil-2-fenil -oxazol-4-il)-etilamino]-acetil}-pirrolidin-2-carbonitrilo y a polimorfos cristalinos de este compuesto. Este compuesto y sus formas polimorficas poseen propiedades superiores si se comparan con los compuestos conocidos anteriormente y pueden utilizarse como medicamentos para el tratamiento de trastornos asociados con DPP-IV.
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Patent Agency Ranking
公开(公告)号：PA8666701A1
公开(公告)日：2006-12-07
申请号：PA8666701
申请日：2006-03-21
Applicant: HOFFMANN LA ROCHE
Inventor： BUBENDORF ANDRE GERARD , SCALONE MICHELANGELO , SCHWITTER URS , ABRECHT STEFAN , GOETZOE STEFAN , GRASSMANN OLAF , MONTAVON FRANCOIS , MOOG REGINA , ROHRER FRANZISKA , RUF ARMIN , WANG SHAONING
IPC: A61K31/00 , C07D207/00
Abstract: LA INVENCION SE REFIERE AL MESILATO DEL (S)-1-{[2-(5-METIL-2-FENIL-OXAZOL-4-IL)-ETILAMINO-ACETIL}PIRROLIDINA-2-CARBONITRILO Y A POLIMORFOS CRISTALINOS DE ESTE COMPUESTO. ESTE COMPUESTO Y SUS FORMAS POLIMÓRFICAS POSEEN PROPIEDADES SUPERIORES SI SE COMPARAN CON LOS COMPUESTOS CONOCIDOS ANTERIORMENTE Y PUEDEN UTILIZARSE COMO MEDICAMENTOS PARA EL TRATAMIENTO DE TRASTORNOS ASOCIADOS CON LA DPP-IV.
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公开(公告)号：DOP2006000066A
公开(公告)日：2006-09-30
申请号：DO2006000066
申请日：2006-03-21
Applicant: HOFFMANN LA ROCHE
Inventor： ABRECHT STEFAN
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公开(公告)号：TR9800403A2
公开(公告)日：1998-09-21
申请号：TR9800403
申请日：1998-03-06
Applicant: HOFFMANN LA ROCHE
Inventor： ABRECHT STEFAN
IPC: C07D463/00 , B01J27/08 , C07B61/00 , C07D207/26 , C07D207/273 , C07D498/04 , C07D501/00 , C07D501/04 , C07D501/24 , C07D501/56 , C07D505/00 , C07D507/08 , C07D201/00
CPC classification number: C07D207/273 , C07D501/00 , C07D505/00
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公开(公告)号：ZA981885B
公开(公告)日：1998-09-10
申请号：ZA981885
申请日：1998-03-05
Applicant: HOFFMANN LA ROCHE
Inventor： ABRECHT STEFAN
IPC: C07D463/00 , B01J27/08 , C07B61/00 , C07D207/26 , C07D207/273 , C07D498/04 , C07D501/00 , C07D501/04 , C07D501/24 , C07D501/56 , C07D505/00 , C07D507/08 , C07D
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公开(公告)号：ZA9801885B
公开(公告)日：1998-09-10
申请号：ZA9801885
申请日：1998-03-05
Applicant: HOFFMANN LA ROCHE
Inventor： ABRECHT STEFAN
IPC: C07D463/00 , B01J27/08 , C07B61/00 , C07D207/26 , C07D207/273 , C07D498/04 , C07D501/00 , C07D501/04 , C07D501/24 , C07D501/56 , C07D505/00 , C07D507/08 , C07D
CPC classification number: C07D207/273 , C07D501/00 , C07D505/00
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