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91. 发明专利

HRP20050664A2 NEW CRYSTALLINE MODIFICATION OF 2-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-N-[6-(1,1-DIOXO-1λ6-THIOMORPHOLIN-4-YL)-A(4-FLUORO-2-METHYL-PHENYL)-PYRIDIN-3-YL]-N-METHYL-ISOBUTYRAMIDE 未知
公开(公告)号：HRP20050664A2
公开(公告)日：2006-12-31
申请号：HRP20050664
申请日：2005-07-21
申请人： HOFFMANN LA ROCHE
发明人： HOFFMANN TORSTEN , HOFFMANN-EMERY FABIENNE , NICK SONIA , SCHWITTER URS , WALDMEIER PIUS
IPC分类号： A61K31/54 , A61P25/00 , C07D213/75
摘要： The present invention relates to a new crystalline modification of 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1lambda 6 -thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide characterized by the following X-ray diffraction pattern obtained with a Cu Kalpha , radiation at 2theta (2Theta)=4.5, 6.4, 7.5, 7.7, 8.0, 8.2, 10.0, 10.2, 10.9, 11.1, 12.9, 13.4, 14.0, 14.5, 15.1, 15.6, 16.2, 16.5, 17.3, 17.5, 18.0, 18.9, 19.3, 19.5, 19.9, 20.1, 20.6, 21.0, 21.4, 22.7, 23.1 and 23.6 and an infrared spectrum having sharp bands at 2925, 2854, 1637, 1604, 1484, 1395, 1375, 1285, 1230, 1172, 1125, 1082, 999, 943, 893, 868, 860, 782, 705, 684 cm -1 , and wherein the extrapolated melting point (DSC) is 137.2° C.

92. 发明专利

NO20053431A 未知
公开(公告)号：NO20053431A
公开(公告)日：2005-10-05
申请号：NO20053431
申请日：2005-07-14
申请人： HOFFMANN LA ROCHE
发明人： HOFFMANN TORSTEN , HOFFMAN-EMERY FABIENNE , NICK SONIA , SCHWITTER URS , WALDMEIER PIUS
IPC分类号： A61P25/00 , A61K31/54 , C07D213/75
CPC分类号： C07D213/75

93. 发明专利

DE60104923T2 未知
公开(公告)号：DE60104923T2
公开(公告)日：2005-08-25
申请号：DE60104923
申请日：2001-03-15
申请人： HOFFMANN LA ROCHE
发明人： CRAMERI YVO , SCALONE MICHELANGELO , WALDMEIER PIUS , WIDMER ULRICH
IPC分类号： A61K31/445 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00 , C07B53/00 , C07B61/00 , C07C315/04 , C07C317/22 , C07D211/42 , C07D211/74
摘要： The present invention relates to a new process for the preparation of compounds of the general formulae wherein R - R are, independently from each other, hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, or acetamido; R -R are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy; and their pharmaceutically acceptable acid addition salts. The compounds of formulae I-a and I-b are 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 including learning and memory formation and function.

94. 发明专利

PE09442004A1 NUEVA MODIFICACION CRISTALINA DE LA 2-(3,5-BIS-TRIFLUORMETIL-FENIL)-N-[6-1,1-DIOXO-1l6-TIOMORFOLIN-4-IL)-4-(4-FLUOR-2-METIL-FENIL)-PIRIDIN-3-IL]-N-METIL-ISOBUTIRAMIDA 未知
公开(公告)号：PE09442004A1
公开(公告)日：2004-12-14
申请号：PE0001102004
申请日：2004-01-28
申请人： HOFFMANN LA ROCHE
发明人： HOFFMANN TORSTEN , HOFFMANN-EMERY FABIENNE , NICK SONIA , WALDMEIER PIUS , SCHWITTER URS
IPC分类号： A61K31/54 , A61P25/00 , C07D213/75
CPC分类号： C07D213/75
摘要： SE REFIERE A UNA FORMA CRISTALINA DE 2-(3,5-BIS-TRIFLUORMETIL-FENIL)-N-[6-(1,1-DIOXO-1l6-TIOMORFOLIN-4-IL)-4-(4-FLUOR-2-METIL-FENIL)-PIRIDIN-3-IL]-N-METIL-ISOBUTIRAMIDA QUE PRESENTA UN MODELO DE DIFRACCION DE RAYOS X OBTENIDO CON UNA RADIACION Cuka A 2q IGUAL A 4,5, 6,4, 7,5, 7,7, 8,0, 8,2, 10,0, 10,2, 10,9, 11,1, 12,9, 13,4, 14,0, 14,5, 15,1, 15,6, 16,2, 16,5, 17,3, 17,5, 18,0, 18,9, 19,3, 19,5, 19,9, 20,1, 20,6, 21,0, 21,4, 22,7, 23,1 Y 23,6 Y UN ESPECTRO INFRARROJO CON BANDAS AGUDAS A 2925, 2854, 1637, 1604, 1484, 1395, 1375, 1285, 1230, 1172, 1125, 1082, 999, 943, 893, 868, 860, 782, 705, 684 cm-1, Y EN DONDE EL PUNTO DE FUSION EXTRAPOLADO (DSC) ES DE 137,2°C. LA 2-(3,5-BIS-TRIFLUORMETIL-FENIL)-N-[6-(1,1-DIOXO-1l6-TIOMORFOLIN-4-IL)-4-(4-FLUOR-2-METIL-FENIL)-PIRIDIN-3-IL]-N-METIL-ISOBUTIRAMIDA ES ACTIVA SOBRE EL RECEPTOR NK1 Y ES UTIL PARA EL TRATAMIENTO DE MIGRANNA, ARTRITIS REUMATOIDE, ASMA

95. 发明专利

DE60104923D1 未知
公开(公告)号：DE60104923D1
公开(公告)日：2004-09-23
申请号：DE60104923
申请日：2001-03-15
申请人： HOFFMANN LA ROCHE
发明人： CRAMERI YVO , SCALONE MICHELANGELO , WALDMEIER PIUS , WIDMER ULRICH
IPC分类号： A61K31/445 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00 , C07B53/00 , C07B61/00 , C07C315/04 , C07C317/22 , C07D211/42 , C07D211/74
摘要： The present invention relates to a new process for the preparation of compounds of the general formulae wherein R - R are, independently from each other, hydrogen, halogen, hydroxy, amino, nitro, lower-alkyl-sulfonylamido, or acetamido; R -R are, independently from each other hydrogen, lower-alkyl, halogen, trifluoromethyl or lower-alkoxy; and their pharmaceutically acceptable acid addition salts. The compounds of formulae I-a and I-b are 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 including learning and memory formation and function.

96. 发明专利

CA2514037A1 NEW CRYSTALLINE MODIFICATION OF 2-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-N-[6-(1,1-DIOXO-1.LAMBDA.6-THIOMORPHOLIN-4-YL)-4(4-FLUORO-2-METHYL-PHENYL)-PYRIDIN-3-YL]-N-METHYL-ISOBUTYRAMIDE 未知
公开(公告)号：CA2514037A1
公开(公告)日：2004-08-12
申请号：CA2514037
申请日：2004-01-23
申请人： HOFFMANN LA ROCHE
发明人： WALDMEIER PIUS , SCHWITTER URS , NICK SONIA , HOFFMANN-EMERY FABIENNE , HOFFMANN TORSTEN
IPC分类号： A61K31/54 , A61P25/00 , C07D213/75
摘要： The present invention relates to a new crystalline modification of 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1lambda 6 -thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide characterized by the following X-ray diffraction pattern obtained with a Cu Kalpha , radiation at 2theta (2Theta)=4.5, 6.4, 7.5, 7.7, 8.0, 8.2, 10.0, 10.2, 10.9, 11.1, 12.9, 13.4, 14.0, 14.5, 15.1, 15.6, 16.2, 16.5, 17.3, 17.5, 18.0, 18.9, 19.3, 19.5, 19.9, 20.1, 20.6, 21.0, 21.4, 22.7, 23.1 and 23.6 and an infrared spectrum having sharp bands at 2925, 2854, 1637, 1604, 1484, 1395, 1375, 1285, 1230, 1172, 1125, 1082, 999, 943, 893, 868, 860, 782, 705, 684 cm -1 , and wherein the extrapolated melting point (DSC) is 137.2° C.

97. 发明专利

ES2208206T3 未知
公开(公告)号：ES2208206T3
公开(公告)日：2004-06-16
申请号：ES00125665
申请日：2000-11-23
申请人： HOFFMANN LA ROCHE
发明人： HILPERT HANS , HOFFMANN-EMERY FABIENNE , RIMMLER GOESTA , ROGERS-EVANS MARK , STAHR HELMUT WERNER , WALDMEIER PIUS
IPC分类号： A61K31/496 , A61K31/5377 , A61P1/08 , A61P25/18 , A61P25/22 , A61P25/24 , C07D213/75 , C07D213/76 , C07D213/82 , A61K31/44 , A61K31/455
摘要： The present invention relates to a process for the preparation of compounds of the general formula wherein the definitions of substituents are described in claim 1, which process comprises 1a) reacting a compound of formula wherein A denotes R or R , and R is halogen, R and R have the significances given in claim 1 and R has the same meaning as R , wherein R and R may he independent from each other, with a compound of formula R Mghal wherein R' is described in claim 1, to a mixture of compounds of formulae wherein the substituents are described in claim 1, or 1a') reacting a compound of formula IV-1, wherein A is R, with a compound of formula V and with a compound of formula HR wherein R is described in claim 1, in one reaction step to a compound of formula wherein R , R , R and R have the significances given in claim 1, and 1b) oxidizing a compound of formulae X-1, XI-1 or VI, which is obtained in step 1a) or 1a') with an oxidizing agent to a compound of formula or wherein R, R , R , R and R have the significances given in claim 1, and, 1b') if desired, reacting a compound of formula XII with a compound of formula VII to a compound of formula VIII, and 1c) reacting a compound of formula VIII with a compound of formula wherein R , R and R are described in claim 1 and R is halogen, to give a compound of formula wherein X is -CON(R )-, or 2 d) transforming a compound of formula VIII to a compound of formula wherein R and R have the significances given in claim 1, and 2 e) reacting a compound of formula XIII to a compound of formulas or wherein the definition of the substituents is given in claim 1, and 2f) transforming the compounds of formulae XIV and XV to a compound of formula wherein R is methyl and 2 g) reacting a compound of formula XVI with a compound of formula to give a compound of formula wherein X is -N(R )C(O)- and the other substituents are described in claim 1.

98. 发明专利

PL2768827T3 SPOSÓB WYTWARZANIA KWASÓW IZOKSAZOLILOMETOKSYNIKOTYNOWYCH 未知
公开(公告)号：PL2768827T3
公开(公告)日：2017-05-31
申请号：PL12772788
申请日：2012-10-17
申请人： HOFFMANN LA ROCHE
发明人： DOTT PASCAL , HANLON STEVEN PAUL , HILDBRAND STEFAN , IDING HANS , THOMAS ANDREW , WALDMEIER PIUS
IPC分类号： C07D413/12 , C07D413/14 , C07D487/04

99. 发明专利

HUE025022T2 Új eljárások propán-1-szulfonsav-{3-[5-(4-klór-fenil)-1H-pirrolo[2,3-B]piridin-3-karbonil]-2,4-difluorfenil}-amid elõállítására 未知
公开(公告)号：HUE025022T2
公开(公告)日：2016-05-30
申请号：HUE11735858
申请日：2011-07-18
申请人： HOFFMANN LA ROCHE
发明人： BRUMSTED COREY JAMES , MOORLAG HENDRIK , RADINOV ROUMEN NIKOLAEV , REN YI , WALDMEIER PIUS

100. 发明专利

BRPI1012618A2 derivados de hidróxi-metil isoxazol como moduladores de gaba a 未知
公开(公告)号：BRPI1012618A2
公开(公告)日：2016-03-29
申请号：BRPI1012618
申请日：2010-03-30
申请人： HOFFMANN LA ROCHE
发明人： THOMAS ANDREW , BUETTELMANN BERND , LUCAS MATTHEW C , SPURR PAUL , WALDMEIER PIUS , JAKOB-ROETNE ROLAND , GABRIEL STEPHEN DEEMS , HANLON STEVEN PAUL
IPC分类号： C07D413/14 , A61K31/4439 , A61P25/28 , C07D413/12

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