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公开(公告)号：JPH11209343A
公开(公告)日：1999-08-03
申请号：JP30771998
申请日：1998-10-29
Applicant: HOFFMANN LA ROCHE
Inventor： HERTEL CORNELIA , HOFFMANN TORSTEN , JACOB-ROETNE ROLAND , NORCROSS ROGER DAVID
IPC: C07K5/078 , A61K31/00 , A61K31/40 , A61K31/401 , A61K31/4015 , A61K38/08 , A61P3/00 , A61P3/10 , A61P9/04 , A61P9/10 , A61P25/00 , A61P25/28 , A61P43/00 , C07D207/16 , C07D207/22 , C07D207/277 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D419/14 , C07D521/00
Abstract: PROBLEM TO BE SOLVED: To provide a new compound especially useful as pharmaceuticals for the treatment or prevention of amyloidosis. SOLUTION: This compound is expressed by formula II or formula II [R is SH, benzyl or phenyl; R is H or a halogen; X is (CH2 )n or the like; Y is S-S, (CH2 )n of the like; X' is (CH2 )n or the like; R is a lower alkyl, a lower alkoxy or the like; (n) is 0-3], preferably (R)-1-[(S)-3-[(S)-3-[(R)-2-carboxy- pyrrolidin-1-yl]-2-methyl-3-oxopropyl-disulfanyl]-2-methyl-propionyl]- pyrrolidine-2- carboxylic acid, etc. The objective compound can be produced e.g. by converting a compound of formula III successively to a compound of formula IV and then a compound of formula V by reacting in a solvent such as methanol in the presence of ammonia at room temperature in an inert atmosphere for about 2 hr.
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公开(公告)号：WO2006128802A3
公开(公告)日：2007-04-12
申请号：PCT/EP2006062514
申请日：2006-05-23
Applicant: HOFFMANN LA ROCHE , MALHERBE PARICHEHR , MASCIADRI RAFFAELLO , NORCROSS ROGER DAVID , PRINSSEN ERIC
Inventor： MALHERBE PARICHEHR , MASCIADRI RAFFAELLO , NORCROSS ROGER DAVID , PRINSSEN ERIC
IPC: C07C225/22 , A61K31/47 , A61K31/4709 , C07D215/36 , C07D215/38 , C07D215/42 , C07D265/22 , C07D401/04
CPC classification number: C07D265/22 , C07D215/36 , C07D215/38 , C07D215/42 , C07D401/04
Abstract: The present invention relates to compounds of formula (I) wherein R 1 , R 2 and R 3 are as defined hereinabove which are active at the GABA B receptor and which can be used for the preparation of medicaments useful in the control or prevention of CNS disorders.
Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 2，R 3和R 3如上所定义，其在 GABA B 受体，其可用于制备可用于控制或预防CNS障碍的药物。
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公开(公告)号：WO0162233A3
公开(公告)日：2002-01-03
申请号：PCT/EP0101679
申请日：2001-02-15
Applicant: HOFFMANN LA ROCHE
Inventor： BORRONI EDILIO MAURIZIO , HUBER-TROTTMANN GERDA , KILPATRICK GAVIN JOHN , NORCROSS ROGER DAVID
IPC: A61K31/00 , A61K31/44 , A61K31/4418 , A61K31/443 , A61K31/4436 , A61K31/444 , A61K31/4709 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/519 , A61K31/5377 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P21/02 , A61P25/04 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P37/08 , A61P43/00 , C07D213/57 , C07D213/85 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/48 , C07D239/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D407/04 , C07D407/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D495/04 , C07D521/00
CPC classification number: C07D239/42 , A61K31/44 , A61K31/443 , A61K31/4436 , A61K31/444 , A61K31/4709 , A61K31/505 , A61K31/506 , C07D213/85 , C07D231/12 , C07D233/56 , C07D239/47 , C07D239/48 , C07D239/56 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D495/04
Abstract: The invention relates to cyclic heteroaromatic compounds, containing at least one nitrogen atom, and to their use in the manufacture of medicaments for the treatment of diseases, related to adenosine receptor modulators, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses, hypoxia, ischaemia, seizure, substance abuse, sedation and they may be active as muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardioprotective agents.
Abstract translation: 本发明涉及含有至少一个氮原子的环状杂芳族化合物，以及它们在制备用于治疗与腺苷受体调节剂诸如阿尔茨海默氏病，帕金森病，神经保护，精神分裂症，焦虑症等相关的疾病的药物中的用途， 疼痛，呼吸困难，抑郁症，哮喘，过敏反应，缺氧，局部缺血，癫痫发作，物质滥用，镇静作用，它们可能作为肌肉松弛剂，抗精神病药，抗癫痫药，抗惊厥药和心脏保护剂起作用。
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公开(公告)号：WO0197786A3
公开(公告)日：2002-12-12
申请号：PCT/EP0106506
申请日：2001-06-08
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , FLOHR ALEXANDER , MILLER AUBRY KERN , NORCROSS ROGER DAVID , RIEMER CLAUS
IPC: A61K31/422 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/455 , A61K31/4725 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/5513 , A61P11/06 , A61P21/02 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , C07D277/82 , C07D417/04 , C07D417/12 , C07D417/14
CPC classification number: C07D417/04 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/444 , A61K31/455 , A61K31/5375 , A61K31/541 , A61K31/5513 , C07D277/82 , C07D417/12 , C07D417/14
Abstract: The present invention relates to compounds of the general formula (I) and to their pharmaceutically acceptable salts for the treatment of diseases related to the adenosine A2 receptor, novel compounds of formula I-A per se,their manufacture, medicaments based on a compound in accordance with the invention and their production as well as the use of compounds of compounds of formula I in the control or prevention of illnesses based on the modulation of the adenosine system, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses hypoxia, ischaemia, seizure and substance abuse. Furthermore, compounds of the present invention may be useful as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents.
Abstract translation: 本发明涉及通式（I）的化合物及其药学上可接受的盐，用于治疗与腺苷A2受体相关的疾病，式IA本身的新化合物及其制备，基于根据 本发明及其生产以及式I化合物的化合物在控制或预防基于腺苷系统如阿尔茨海默氏病，帕金森病，神经保护，精神分裂症，焦虑，疼痛，呼吸的腺苷系统的调节中的用途 缺陷，抑郁症，哮喘，过敏反应缺氧，局部缺血，癫痫发作和药物滥用。 此外，本发明的化合物可用作镇静剂，肌肉松弛剂，抗精神病药，抗癫痫剂，抗惊厥药和心脏保护剂。
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5.发明申请
公开(公告)号：WO9825930A2
公开(公告)日：1998-06-18
申请号：PCT/EP9706865
申请日：1997-12-09
Applicant: HOFFMANN LA ROCHE
Inventor： HUBER TROTTMANN GERDA , JAKOB-ROETNE ROLAND , KOLCZEWSKI SABINE , NORCROSS ROGER DAVID , WOLTERING THOMAS JOHANNES
IPC: C07D455/02 , C07D455/06 , C07D471/14 , C07D495/14 , C07D495/00
CPC classification number: C07D471/14 , C07D455/02 , C07D455/06 , C07D495/14
Abstract: The invention is concerned with the use of bi- and tricyclic pyridone compounds of general formula (I) and of their pharmaceutically acceptable salts for the production of medicaments for the prophylaxis or treatment of illnesses which are connected with an inhibition of beta -amyloid peptide activity, especially for the treatment of Alzheimer's disease.
Abstract translation: 本发明涉及使用通式（I）的二环和三环吡啶酮化合物及其药学上可接受的盐来生产用于预防或治疗与β-淀粉样蛋白肽活性的抑制相关的疾病的药物 ，特别是用于治疗阿尔茨海默病。
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Patent Agency Ranking
公开(公告)号：CL2021003373A1
公开(公告)日：2022-10-07
申请号：CL2021003373
申请日：2021-12-16
Applicant: HOFFMANN LA ROCHE
Inventor： GOERGLER ANNICK , JAESCHKE GEORG , KUHN BERND , NAGEL YVONNE ALICE , RICCI ANTONIO , RUEHER DANIEL , STEINER SANDRA , DOLENTE COSIMO , HEWINGS DAVID STEPHEN , NORCROSS ROGER DAVID , OBST-SANDER CHRISTA ULRIKE
IPC: A61K31/427 , A61P35/00 , C07D417/14
Abstract: La invención proporciona nuevos compuestos como se describen en la presente, composiciones que incluyen los compuestos y métodos para usar los compuestos.
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公开(公告)号：PE20220807A1
公开(公告)日：2022-05-20
申请号：PE2021002083
申请日：2020-06-19
Applicant: HOFFMANN LA ROCHE
Inventor： DOLENTE COSIMO , GOERGLER ANNICK , HEWINGS DAVID STEPHEN , JAESCHKE GEORG , KUHN BERND , NAGEL YVONNE ALICE , NORCROSS ROGER DAVID , OBST-SANDER CHRISTA ULRIKE , RICCI ANTONIO , RUEHER DANIEL , STEINER SANDRA
IPC: A61P35/00 , A61K31/427 , C07D417/14
Abstract: Referido a compuestos inhibidores de receptor del factor de crecimiento epidermico (EGFR). Un compuesto seleccionado es 2-(6,7-dihidro-5H-pirrolo[1,2-c]imidazol-1-il)-2-[6-[4-(1-etil-4-piperidil)fenil]-1-oxo-4-(trifluorometil) isoindolin-2-il]-N-tiazol-2-il-acetamida. Tambien se refiere a procedimientos para su preparacion, productos intermedios, formulaciones farmaceuticas que comprenden dichos compuestos, y uso en el tratamiento terapeutico y/o profilactico del cancer, en particular cancer de pulmon no microcitico.
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公开(公告)号：AU2020296933A1
公开(公告)日：2021-12-02
申请号：AU2020296933
申请日：2020-06-19
Applicant: HOFFMANN LA ROCHE
Inventor： DOLENTE COSIMO , GOERGLER ANNICK , HEWINGS DAVID STEPHEN , JAESCHKE GEORG , KUHN BERND , NAGEL YVONNE ALICE , NORCROSS ROGER DAVID , OBST-SANDER CHRISTA ULRIKE , RICCI ANTONIO , RUEHER DANIEL , STEINER SANDRA
IPC: A61P35/00 , A61K31/427 , C07D417/14
Abstract: The invention provides novel compounds as described herein, compositions including the compounds and methods of using the compounds.
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公开(公告)号：ECSP13013072A
公开(公告)日：2014-01-31
申请号：ECSP13013072
申请日：2013-12-09
Applicant: HOFFMANN LA ROCHE
Inventor： NORCROSS ROGER DAVID , GALLEY GUIDO , PFLIEGER PHILIPPE , GHELLAMALLAH CÉDRIC
IPC: A61K31/4245 , A61P25/00 , C07D413/12 , C07D413/14
Abstract: La invención se refiere a compuestos de la fórmula IA o IBen las que:R1 es hidrógeno o fenilo opcionalmente sustituido por haló-geno, CN o alcoxi inferior o alcoxi inferior sustituido por halógeno; R2 es hidrógeno o alquilo inferior;R3 es hidrógeno o alquilo inferior o es fenilo opcionalmente sustituido por uno o más sustituyentes elegidos entre halógeno, ciano o alcoxi inferior sustituido por halógeno, o es piridinilo opcionalmente sustituido por halógeno o alquilo inferior sustituido por halógeno, o es pirimidinilo, opcionalmente sustituido por alquilo inferior sustituido por halógeno, o es pirazinilo, opcionalmente sustituido por halógeno, ciano o alquilo inferior sustituido por halógeno;R4 es hidrógeno, alquilo inferior o fenilo;Z es un enlace, -CH2- u -O-;o a una sal de adición de ácido farmacéuticamente aceptable de los mismos.Ahora se ha encontrado que los compuestos de las fórmulas IA e IB tienen buena afinidad con los receptores asociados con las aminas traza (TAARs), en especial con el TAAR1.Estos compuestos pueden utilizarse para el tratamiento de la depresión, los trastornos de ansiedad, el trastorno bipolar, el trastorno de hiperactividad con déficit de atención (ADHD), los trastornos relacionados con el estrés, los trastornos psicóticos como son la esquizofrenia, las enfermedades neurológicas, por ejemplo la enfermedad de Parkinson, los trastornos neurodegenerativos, por ejemplo la enfermedad de Alzheimer, la epilepsia, la migraña, la hipertensión, el abuso de sustancias y los trastornos metabólicos, por ejemplo los trastornos de ingestión de comida, la diabetes, las complicaciones diabéticas, la obesidad, la dislipidemia, los trastornos de consumo y asimilación de energía, los trastornos y malfunción de la temperatura corporal, la homeostasis, los trastornos del sueño y del ritmo circadiano y los trastornos cardiovasculares.
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公开(公告)号：CA2413086C
公开(公告)日：2011-06-28
申请号：CA2413086
申请日：2001-06-08
Applicant: HOFFMANN LA ROCHE
Inventor： ALANINE ALEXANDER , FLOHR ALEXANDER , MILLER AUBRY KERN , NORCROSS ROGER DAVID , RIEMER CLAUS
IPC: C07D417/14 , A61K31/422 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/455 , A61K31/4725 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/5513 , A61P11/06 , A61P21/02 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , C07D277/82 , C07D413/04 , C07D417/04 , C07D417/12
Abstract: The present invention relates to compounds of the general formula (I) and to their pharmaceutically acceptable salts for the treatment of diseases related to the adenosine A2 receptor, novel compounds of formula I-A per se,their manufacture, medicaments based on a compound in accordance with the invention and their production as well as the use of compounds of compounds of formula I in the control or prevention of illnesses based on the modulation of the adenosine system, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses hypoxia, ischaemia, seizure and substance abuse. Furthermore, compounds of the present invention may be useful as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents.
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