公开(公告)号：WO2014173917A8

公开(公告)日：2015-06-18

申请号：PCT/EP2014058172

申请日：2014-04-23

Applicant: HOFFMANN LA ROCHE ,  HOFFMANN LA ROCHE

Inventor： FETTES ALEC ,  MARTY HANS-PETER ,  SCALONE MICHELANGELO

IPC: C07D213/79 ,  C07D213/803 ,  C07D213/85 ,  C07D241/24 ,  C07D413/12

CPC classification number: C07D213/84 ,  C07D213/79 ,  C07D213/803 ,  C07D213/85 ,  C07D241/24 ,  C07D413/12

Abstract: The present invention provides a one step carbonylation of a compound of formula II in the presence of water to afford a compound of formula (I), useful in processes to manufacture BACE inhibitors.

Abstract translation: 本发明提供式II化合物在水存在下的一步羰基化，得到式（I）化合物，可用于制备BACE抑制剂的方法。

公开(公告)号：WO2011018445A3

公开(公告)日：2011-06-23

申请号：PCT/EP2010061579

申请日：2010-08-10

Applicant: HOFFMANN LA ROCHE ,  BACHMANN STEPHAN ,  FETTES ALEC ,  SCALONE MICHELANGELO

Inventor： BACHMANN STEPHAN ,  FETTES ALEC ,  SCALONE MICHELANGELO

IPC: C07C315/02 ,  C07C315/04 ,  C07C317/44 ,  C07D241/20

CPC classification number: C07D261/04 ,  B01J31/189 ,  B01J31/2295 ,  B01J31/2409 ,  B01J31/2433 ,  B01J2231/645 ,  B01J2531/0205 ,  B01J2531/821 ,  B01J2531/822 ,  B01J2531/827 ,  B01J2531/842 ,  C07B53/00 ,  C07B2200/07 ,  C07C315/02 ,  C07C315/04 ,  C07C2601/08 ,  C07D241/20 ,  C07D333/30 ,  C07D409/04 ,  C07C317/44

Abstract: The present invention relates to a process for the preparation of (R)-2-phenyl propionic acid derivatives of the formula (I), wherein R1 is C1-6-alkyl and R2 is hydrogen or halogen, or of a salt thereof by asymmetric hydrogenation of the corresponding acrylicacid derivative. (R)-2-phenyl propionic acid derivatives of the formula (I) are key intermediates in the synthesis of 5-substituted -pyrazine or pyridine glucokinase activators of the formula (II).

Abstract translation: 本发明涉及制备式（I）的（R）-2-苯基丙酸衍生物的方法，其中R 1为C 1-6 - 烷基且R 2为氢或卤素，或其盐为不对称的 氢化相应的丙烯酸衍生物。 式（I）的（R）-2-苯基丙酸衍生物是合成式（II）的5-取代的吡嗪或吡啶葡糖激酶活化剂的关键中间体。

公开(公告)号：HRP20250178T1

公开(公告)日：2025-04-11

申请号：HRP20250178

申请日：2022-05-03

Applicant: HOFFMANN LA ROCHE

Inventor： BACHMANN STEPHAN ,  CHYTIL LUKAS ,  FANTASIA SERENA MARIA ,  FETTES ALEC ,  HOFFMANN URSULA ,  KAPPE CHRISTIAN OLIVER ,  LEBL RENE ,  PUENTENER KURT ,  TOSATTI PAOLO ,  WILLIAMS JASON DOUGLAS

IPC: C07D405/14 ,  C07D487/04 ,  C07D519/00

公开(公告)号：ES3012969T3

公开(公告)日：2025-04-10

申请号：ES22727275

申请日：2022-05-03

Applicant: HOFFMANN LA ROCHE

Inventor： BACHMANN STEPHAN ,  CHYTIL LUKAS ,  FANTASIA SERENA MARIA ,  FETTES ALEC ,  HOFFMANN URSULA ,  KAPPE CHRISTIAN OLIVER ,  LEBL RENE ,  PUENTENER KURT ,  TOSATTI PAOLO ,  WILLIAMS JASON DOUGLAS

IPC: C07D405/14 ,  C07D487/04 ,  C07D519/00

Abstract: Se proporcionan métodos para preparar el compuesto inhibidor de la tirosina quinasa de Bruton ("BTK") 2-{3'-hidroximetil-1-metil-5-[5-((S)-2-metil-4-oxetan-3-il-piperazin-1-il)-piridin-2-ilamino]-6-oxo-1,6-dihidro-[3,4']bipiridinil-2'-il}-7,7-dimetil-3,4,7,8-tetrahidro-2H,6H-ciclopenta[4,5]pirrolo[1,2-a]pirazin-1-ona. (Traducción automática con Google Translate, sin valor legal)

公开(公告)号：MX2022016065A

公开(公告)日：2023-02-02

申请号：MX2022016065

申请日：2020-10-29

Applicant: HOFFMANN LA ROCHE

Inventor： IDING HANS ,  GOSSELIN FRANCIS ,  FETTES ALEC ,  ZHANG HAIMING ,  LIM NGIAP- KIE ,  CHAKRAVARTY PAROMA ,  NAGAPUDI KARTHIK ,  CHUNG CHEOL KEUN ,  XU JIE ,  CLAGG KYLE ,  DALZIEL MICHAEL ,  MCCLORY(FINADO) ANDREW ,  ROBINSON SARAH

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

Abstract: En la presente se proveen formas sólidas, sales tales como el Compuesto B, y formulaciones de 3-((1R,3R)-1-(2,6-difluoro-4-((1-( 3-fluoropropil)azetidin-3-il)amino)fenil)-3-metil-1,3,4,9-tetrahi dro-2H-pirido[3,4-b]indol-2-il)-2,2-difluoropropan-1-ol, procesos y síntesis de estos y métodos para su uso en el tratamiento del cáncer.

公开(公告)号：AU2022202967A1

公开(公告)日：2022-05-26

申请号：AU2022202967

申请日：2022-05-03

Applicant: HOFFMANN LA ROCHE

Inventor： 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: C07D471/04 ,  A61K31/437 ,  A61P35/00

Abstract: Abstract Provided herein are solid forms, salts such as Compound B, 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. HO2C

公开(公告)号：AU2020292763A1

公开(公告)日：2022-01-20

申请号：AU2020292763

申请日：2020-06-09

Applicant: HOFFMANN LA ROCHE

Inventor： FETTES ALEC ,  GEISER ACHIM ,  JAITZ LEONHARD ,  CHOI HONGRIM ,  JUNG KYEONG EUN ,  KIM SUNG WON

IPC: C07H1/00 ,  C07H21/00

Abstract: The invention relates to a process for the production of a mixed P=O/P=S backbone oligonucleotide comprising a selective oxidation of an intermediary phosphite triester compound of formula I into a phosphodiester compound of formula II according to the scheme with an oxidation solution obtained by mixing iodine, an organic solvent and water, characterized in that the oxidation solution has been aged for a time period that is sufficient to selectively oxidize the phosphite triester compound of formula I into the phosphodiester compound of formula II without oxidizing the phosphorothioate intenucleotide linkages.

公开(公告)号：MX2021015197A

公开(公告)日：2022-01-18

申请号：MX2021015197

申请日：2020-06-09

Applicant: HOFFMANN LA ROCHE

Inventor： KIM SUNG WON ,  FETTES ALEC ,  GEISER ACHIM ,  JAITZ LEONHARD ,  CHOI HONGRIM ,  JUNG KYEONG EUN

IPC: C07H1/00 ,  C07H21/00

Abstract: La invención se refiere a un proceso para la producción de un oligonucleótido de cadena principal P=O/P=S mixta que comprende una oxidación selectiva de un compuesto de triéster de fosfito intermediario de la fórmula I hasta un compuesto de fosfodiéster de la fórmula II de acuerdo con el esquema de reacción, (ver Fórmulas) con una solución de oxidación obtenida al mezclar yodo, un solvente orgánico y agua, en donde la solución de oxidación se ha envejecido durante un período que es suficiente para oxidar selectivamente el compuesto de triéster de fosfito de la fórmula I hasta el compuesto de fosfodiéster de la fórmula II sin oxidar los enlaces internucleotídicos de fosforotioato.

公开(公告)号：AU2021201052A1

公开(公告)日：2021-03-11

申请号：AU2021201052

申请日：2021-02-18

Applicant: HOFFMANN LA ROCHE

Inventor： BEAUDRY DANIAL ,  CRAVILLION THERESA ,  GOSSELIN FRANCIS ,  LIM NGIAP-KIE ,  MALHOTRA SUSHANT ,  TIAN QINGPING ,  ZHANG HAIMING ,  GMEHLING ALEXANDER ,  FETTES ALEC ,  BACHMANN STEPHAN

IPC: C07D487/04

Abstract: PROCESS FOR PREPARING BTK INHIBITORS Abstract Methods for preparing the Bruton's Tyrosine Kinase ("BTK") inhibitor compound 2-{3'-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4']bipyridinyl-2'-yl}-7,7 dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-l-one are provided. Methods for preparing tricyclic lactam compounds are also provided.

公开(公告)号：AU2020201261B2

公开(公告)日：2020-11-19

申请号：AU2020201261

申请日：2020-02-21

Applicant: HOFFMANN LA ROCHE

Inventor： BEAUDRY DANIAL ,  CRAVILLION THERESA ,  GOSSELIN FRANCIS ,  LIM NGIAP-KIE ,  MALHOTRA SUSHANT ,  TIAN QINGPING ,  ZHANG HAIMING ,  GMEHLING ALEXANDER ,  FETTES ALEC ,  BACHMANN STEPHAN

IPC: C07D487/04

Abstract: PROCESS FOR PREPARING BTK INHIBITORS Methods for preparing the Bruton's Tyrosine Kinase ("BTK") inhibitor compound 2-{3'-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2 ylamino]-6-oxo-1,6-dihydro-[3,4']bipyridinyl-2'-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided. Methods for preparing tricyclic lactam compounds are also provided.