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41. 发明专利

PE00792005A1 DERIVADOS DE PIRROLIDONA COMO INHIBIDORES DE MAOB 未知
公开(公告)号：PE00792005A1
公开(公告)日：2005-03-01
申请号：PE0009582003
申请日：2003-09-18
申请人： HOFFMANN LA ROCHE
发明人： WOSTL WOLFGANG , RODRIGUEZ-SARMIENTO ROSA MARIA , JOLIDON SYNESE , THOMAS ANDREW WILLIAM , WIRZ BEAT , KRUMMENACHER DANIELA , IDING HANS , WYLER RENE
IPC分类号： A61K31/4015 , A61P25/16 , A61P25/28 , C07D207/26 , C07D207/273 , C07D207/277 , C07D401/04
CPC分类号： C07D207/273 , C07D207/277
摘要： REFERIDA A UN COMPUESTO DE FORMULA I, DONDE Q ES =N-, =C(R24)-; X-Y ES -CH2-CH2-, -CH=CH-, -CH2-O-; R1, R1.1 Y R1.2 SON CADA UNO H, HALOGENO, CIANO, ENTRE OTROS; R21, R22 Y R23 SON CADA UNO H, HALOGENO; R24 ES H, HALOGENO, METILO; R3 ES -NHR6; R4 ES H. TAMBIEN REFERIDA A PROCESOS PARA SU PREPARACION DONDE SON COMPUESTOS PREFERIDOS: (RS)-N-{1-[4-(3--FLUORO-BENCILOXI)-FENIL]-5-OXO-PIRROLIDIN-3-IL}-ACETAMIDA; (RS)-N-{1-[4-(3-FLUORO-BENCILOXI)-FENIL]- 5-OXO-PIRROLIDIN-3-IL}-FORMAMIDA Y (RS)-{1-[4-(3-FLUORO-BENCILOXI)-FENIL]-5-OXO-PIRROLIDIN-3-IL}-CARBAMATO DE METILO; ENTRE OTROS. DICHOS COMPUESTOS SON UTILES EN LA PREPARACION Y TRATAMIENTO DE ENFERMEDADES MEDIADAS POR INHIBIDORES DE MONOAMINO OXIDASA B COMO LA DE ALZHEIMER O DEMENCIA SENIL, ENTRE OTRAS

42. 发明专利

PE20050050A1 DERIVADOS DE INDOLILO 未知
公开(公告)号：PE20050050A1
公开(公告)日：2005-02-18
申请号：PE2003000917
申请日：2003-09-10
申请人： HOFFMANN LA ROCHE
发明人： MOHR PETER , MAERKI HANS-PETER , GRETHER UWE , HILPERT HANS , MEYER MARKUS , HUMM ROLAND , IDING HANS , KUHN BERND , WIRZ BEAT , BINGGELI ALFRED
IPC分类号： A61K31/405 , A61P3/06 , A61P3/10 , A61P9/10 , C07D413/06 , C07D413/14 , C07D417/06
摘要： REFERIDA A UN COMPUESTO DE FORMULA I, DONDE R1 ES ARILO O HETEROARILO; R2 H, ALQUILO, CICLOALQUILO; R3 ES ARILOXILO, ALQUENILOXILO, ALCOXILO, ENTRE OTROS; R4 ES H, ALQUILO, CICLOALQUILO; R5, R6, R7 Y R8 SON CADA UNO H, ALQUILO, CICLOALQUILO; n ES 1-3; A Y A1 ES N Y EL OTRO ES O O S. SON COMPUESTOS PREFERIDOS: ACIDO (S)-3-{1-[2-(2-CLORO-FENIL)-5-METIL-OXAZOL-4-ILMETIL]-1H-INDOL-5-IL}-2-ETOXI-PROPIONICO; ACIDO RAC-2-ETOXI-3-{3-METIL-1-[5-METIL-2-(4-TRIFLUORO-METIL-FENIL)-OXAZOL-4-ILMETIL]-1H-INDOL-5-IL}-PROPIONICO Y ACIDO RAC-3-{1-[5-METIL-2-(4-TRIFLUOROMETIL-FENIL)-OXAZOL-4-ILMETIL]-1H-INDOL-5-IL}-2-PROPOXI-PROPIONICO; ENTRE OTROS. TAMBIEN REFERIDO A SU COMPOSICION FARMACEUTICA QUE ADEMAS COMPRENDE UN INHIBIDOR DE LIPASAS COMO ORLISTAT LA QUE ES UTIL EN CASOS DE DIABETES, SINDROME METABOLICO Y ENFERMEDADES ATEROSCLEROTICAS, ENTRE OTRAS

43. 发明专利

PA8583501A1 DERIVADOS DE PIRROLIDONA COMO INHIBIDORES DE MAOB 未知
公开(公告)号：PA8583501A1
公开(公告)日：2004-04-23
申请号：PA8583501
申请日：2003-09-18
申请人： HOFFMANN LA ROCHE
发明人： WYLER RENE , THOMAS ANDREW WILLIAM , SARMIENTO ROSA MARIA RODRIGUEZ , JOLIDON SYNESE , IDING HANS , WIRZ BEAT , KRUMMENACHER DANIELA , WOSTL WOLFGANG
IPC分类号： A61K31/4015 , A61P25/16 , A61P25/28 , C07D207/26 , C07D207/273 , C07D207/277 , C07D401/04 , C08G69/24
摘要： DERIVADOS DE 4-PIRROLIDINO RACEMICOS O ENANTIOMERICAMENTE PUROS, PROCESOS PARA SU PREPARACION, COMPOSICIONES FARMACEUTICAS QUE COMPRENDEN DICHOS DERIVADOS, Y SU USO EN LA PREVENCION Y TRATAMIENTO DE UNA ENFERMEDADAD QUE ESTA MEDIADA POR EL INHIBIDOR DE LA MONOAMINA OXIDASA B, EN PARTICULAR LA ENFERMEDAD DE ALZHEIMER Y DEMENCIA SENIL.

44. 发明专利

AU2003270213A1 PYRROLIDONE DERIVATIVES AS MAOB INHIBITORS 未知
公开(公告)号：AU2003270213A1
公开(公告)日：2004-04-08
申请号：AU2003270213
申请日：2003-09-18
申请人： HOFFMANN LA ROCHE
发明人： IDING HANS , JOLIDON SYNESE , KRUMMENACHER DANIELA , RODRIGUEZ-SARMIENTO ROSA MARIA , THOMAS ANDREW WILLIAM , WIRZ BEAT , WOSTL WOLFGANG , WYLER RENE
IPC分类号： A61K31/4015 , A61P25/16 , A61P25/28 , C07D207/26 , C07D207/273 , C07D207/277 , C07D401/04
摘要： The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, e.g. which are mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.

45. 发明专利

CA2461296A1 ENZYMATIC PROCESS FOR THE PREPARATION OF SUBSTITUTED 2-AMINO-3-(2-AMINO-PHENYLSULFANYL)-PROPIONIC ACID 未知
公开(公告)号：CA2461296A1
公开(公告)日：2003-04-10
申请号：CA2461296
申请日：2002-09-19
申请人： HOFFMANN LA ROCHE
发明人： SCHMID STEFAN , ROGERS-EVANS MARK , BORTHWICK SCOTT , BLEICHER KONRAD , IDING HANS , WIRZ BEAT , TONG HAN MIN
IPC分类号： C07C323/59 , C07C323/63 , C07D285/36 , C12P11/00 , C12P13/04 , C12P17/00 , C12P41/00
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-1.beta.-converting enzyme, elastase or angiotensin enzyme, GPCR antagonists (cholecystokinin, angiotensin II receptor). The present inventio n relates to a new process for the preparation compounds of formula (I), where in R1, R2, R3 and n are as described in the description which process comprises reacting compounds of formula (II), wherein R1, R2, R3, n and R4 are as described in the description, with a protease in an aqueous system containin g an organic co-solvent.

46. 发明专利

AU2021266084A1 Process for the preparation of a chiral piperazine-2-carboxylic acid 未知
公开(公告)号：AU2021266084A1
公开(公告)日：2022-10-20
申请号：AU2021266084
申请日：2021-04-26
申请人： HOFFMANN LA ROCHE
发明人： CINQUALBRE JOSÉPHINE , HILDBRAND STEFAN , TOSATTI PAOLO , PUENTENER KURT , WETZL DENNIS , IDING HANS , STOCKER PATRICK , FÉDOU NICOLAS MICKAEL , SPURR PAUL
IPC分类号： C07D295/02 , C07D487/04
摘要： The invention relates to a novel process for the preparation of a chiral piperazine-2- carboxylic acid or of a salt thereof of the formula (I). The chiral piperazine-2-carboxylic acid derivatives of the formula (I) are key intermediates for the preparation of fused heteroaryl dihydro pyrimidines which are useful for the treatment and prophylaxis of hepatitis B virus infections.

47. 发明专利

NZ731073A Processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds 未知
公开(公告)号：NZ731073A
公开(公告)日：2021-11-26
申请号：NZ73107315
申请日：2015-09-25
申请人： HOFFMANN LA ROCHE , GENENTECH INC
发明人： GOSSELIN FRANCIS , REENTS REINHARD , HAN CHONG , IDING HANS , SAVAGE SCOTT , WIRZ BEAT
IPC分类号： C07D239/70
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-5H-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-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The process involves an intramolecular bromide/nitrile cyclization. The present disclosure additionally relates to various compounds that are intermediates employed in these processes.

48. 发明专利

AU2016249780B2 Mutant transaminases as well as methods and uses relating thereto 未知
公开(公告)号：AU2016249780B2
公开(公告)日：2021-07-22
申请号：AU2016249780
申请日：2016-04-13
申请人： HOFFMANN LA ROCHE
发明人： BORNSCHEUER UWE , HANLON STEVEN PAUL , IDING HANS , PAVLIDIS IOANNIS , SPURR PAUL , STEFFEN WEISS MARTIN , WIRZ BEAT
IPC分类号： C12N9/10 , C12P13/00
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.

49. 发明专利

SG11202012171SA SOLID FORMS OF 3-((1R,3R)-1-(2,6-DIFLUORO-4-((1-(3-FLUOROPROPYL)AZETIDIN-3-YL)AMINO)PHENYL)-3-METHYL-1,3,4,9-TETRAHYDRO-2H-PYRIDO[3,4-B]INDOL-2-YL)-2,2-DIFLUOROPROPAN-1-OL AND PROCESSES FOR PREPARING FUSED TRICYCLIC COMPOUNDS COMPRISING A SUBSTITUTED PHENYL OR PYRIDINYL MOIETY, INCLUDING METHODS OF THEIR USE 未知
公开(公告)号：SG11202012171SA
公开(公告)日：2021-01-28
申请号：SG11202012171S
申请日：2019-06-17
申请人： HOFFMANN LA ROCHE
发明人： CHUNG CHEOL KEUN , XU JIE , IDING HANS , CLAGG KYLE , DALZIEL MICHAEL , FETTES ALEC , GOSSELIN FRANCIS , LIM NGIAP-KIE , ZHANG HAIMING , CHAKRAVARTY PAROMA , NAGAPUDI KARTHIK , ROBINSON SARAH
IPC分类号： A61P35/00 , A61K31/437 , C07D471/04
摘要： Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

50. 发明专利

RU2732404C2 СПОСОБЫ ПОЛУЧЕНИЯ (ЦИКЛОПЕНТИЛ[d]ПИРИМИДИН-4-ИЛ)ПИПЕРАЗИНОВЫХ СОЕДИНЕНИЙ 未知
公开(公告)号：RU2732404C2
公开(公告)日：2020-09-16
申请号：RU2020101483
申请日：2015-09-25
申请人： HOFFMANN LA ROCHE
发明人： GOSSELIN FRANCIS , HAN CHONG , IDING HANS , REENTS REINHARD , SAVAGE SCOTT , WIRZ BEAT
IPC分类号： C07D239/70 , C07D239/26 , C07D241/04
摘要： Изобретениеотноситсяк областиорганическойхимии, аименнок способуполучениясоединенияформулы I:илиегосоли. Способвключает: А. (а) циклизациюсоединения VIилиегосолис образованиемсоединенияформулы (V), гдекаждыйХ представляетсобойгидроксил;(b) бромированиесоединенияформулы V илиегосолибромирующимагентомс образованиемсоединенияформулы IV илиегосоли, где Y представляетсобойбром; (с) взаимодействиесоединенияформулы IV спиперазиновымсоединением, имеющимструктуру:илиегосолью, где Lv представляетсобойудаляемуюгруппуи Rпредставляетсобойаминозащитнуюгруппу, собразованиемсоединенияформулы III илиегосоли; В. (d) взаимодействиесоединенияформулы III сметаллизующимагентомс образованиемсоединенияформулы I илиегосоли; где Rпредставляетсобойводородилиаминозащитнуюгруппу. Такжепредложенспособполучениясоединения VIТехническийрезультат: предложенспособсинтеза, которыйявляетсяболееэкономическивыгодными экологическичистым, атакжепозволяетснизитьвероятностьобразованияпобочныхпродуктов. 2 н. и 16 з.п. ф-лы, 7 пр.

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