公开(公告)号：WO2006084854A2

公开(公告)日：2006-08-17

申请号：PCT/EP2006050744

申请日：2006-02-08

Applicant: SOLVAY PHARM BV ,  FEENSTRA ROELOF W ,  KEIZER HISKIAS G ,  PRAS-RAVES MARIA L ,  VAN VLIET BERNARD J ,  VAN SCHARRENBURG GUSTAAF J M

Inventor： FEENSTRA ROELOF W ,  KEIZER HISKIAS G ,  PRAS-RAVES MARIA L ,  VAN VLIET BERNARD J ,  VAN SCHARRENBURG GUSTAAF J M

IPC: C07D285/01 ,  A61K31/425 ,  A61K31/427 ,  A61P25/28 ,  C07D401/12 ,  C07D403/12

CPC classification number: C07D285/01 ,  A61K31/425 ,  A61K31/427 ,  C07D417/04 ,  C07D417/12

Abstract: The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]- dithiazolidine-3,5-diylidene-diamine derivatives as inducers of glutha-thione-S- transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament useful in the for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): wherein the symbols have the meanings given in the specification.

Abstract translation: 本发明涉及作为谷胱甘肽诱导剂的5-亚氨基-5H- [1,2,4] - 二噻唑-3-基 - 胺和[1,2,4] - 二噻唑烷-3,5-二亚基 - 二胺衍生物， 硫酮-S-转移酶（GST）和NADPH醌氧化还原酶（NQO），制备这些化合物的方法和用于合成所述[1,2,4] - 二噻唑啉（二）衍生物的新中间体。 本发明还涉及本文公开的化合物在制备用于预防和治疗与一般的细胞毒性和特别是细胞凋亡有关的不利病症的药物中的用途。 本发明涉及通式（I）的化合物：其中符号具有说明书中给出的含义。

公开(公告)号：WO03068207A2

公开(公告)日：2003-08-21

申请号：PCT/EP0350015

申请日：2003-02-11

Applicant: SOLVAY PHARM BV ,  BRONZOVA JULIANA B ,  FEENSTRA ROELOF W ,  GLENNON JEFFREY C ,  MCCREARY ANDREW C ,  VAN RANDEN JAN ,  RONKEN ERIC ,  VAN SCHARRENBURG GUSTAAF J M

Inventor： BRONZOVA JULIANA B ,  FEENSTRA ROELOF W ,  GLENNON JEFFREY C ,  MCCREARY ANDREW C ,  VAN RANDEN JAN ,  RONKEN ERIC ,  VAN SCHARRENBURG GUSTAAF J M

IPC: A61K45/00 ,  A61K31/00 ,  A61K31/138 ,  A61K31/445 ,  A61K31/48 ,  A61K31/495 ,  A61K31/535 ,  A61K31/55 ,  A61K45/06 ,  A61P25/00 ,  A61P25/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00

CPC classification number: A61K31/55 ,  A61K31/00 ,  A61K31/138 ,  A61K31/445 ,  A61K31/48 ,  A61K31/495 ,  A61K31/535

Abstract: The invention relates to the use of a compound or a combination of compounds having partial dopamine-D2 receptor agonistic activity and serotonin and/or noradrenaline reuptake inhibitory activity, for the preparation of a pharmaceutical composition for the treatment of psychiatric and/or neurologic disorders caused by disturbances of the major monoaminergic dopamine, serotonin and/or nordrenaline systems or that can be treated via manipulation of those systems.

Abstract translation: 本发明涉及使用具有部分多巴胺-D2受体激动活性的化合物或组合，以及5-羟色胺和/或去甲肾上腺素再摄取抑制活性，用于制备用于治疗引起的精神病和/或神经障碍的药物组合物 主要的单胺能多巴胺，5-羟色胺和/或肾上腺素系统的紊乱或可以通过操纵这些系统来治疗。

公开(公告)号：WO2006089861A3

公开(公告)日：2006-10-26

申请号：PCT/EP2006060060

申请日：2006-02-17

Applicant: SOLVAY PHARM BV ,  DRUKARCH BENJAMIN ,  SCHOFFELMEER ANTON N M ,  FEENSTRA ROELOF W ,  CHRISTEN MARIE-ODILE ,  BURGOT JEAN-LOUISE ,  CHOLLET MARYLENE ,  IWEMA BAKKER WOUTER I ,  VAN VLIET BERNARD J ,  TULP MARTINUS TH M

Inventor： DRUKARCH BENJAMIN ,  SCHOFFELMEER ANTON N M ,  FEENSTRA ROELOF W ,  CHRISTEN MARIE-ODILE ,  BURGOT JEAN-LOUISE ,  CHOLLET MARYLENE ,  IWEMA BAKKER WOUTER I ,  VAN VLIET BERNARD J ,  TULP MARTINUS TH M

IPC: C07D339/04 ,  A61K31/385

CPC classification number: C07D409/12 ,  A61K31/385 ,  C07D339/04

Abstract: The invention relates to dithiolethiones derivatives as monoamino oxidase inhibitors, in particular MAO-B inhibitors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said dithiolethiones derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. In embodiments of the invention specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment, amelioration or prevention of conditions associated with dysfunction of monoamine neurotransmission. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

Abstract translation: 本发明涉及二硫代硫代乙烯衍生物作为单氨基氧化酶抑制剂，特别是MAO-B抑制剂，涉及制备这些化合物的方法和用于合成所述二硫代硫代衍生物的新型中间体。 本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。 在本发明的实施方案中，本文公开的具体化合物用于制备可用于治疗，改善或预防与单胺神经传递功能障碍相关的病症的药物。 化合物具有通式（1），其中符号具有说明书中给出的含义。

公开(公告)号：AU2006212209B2

公开(公告)日：2011-02-10

申请号：AU2006212209

申请日：2006-02-08

Applicant: SOLVAY PHARM BV

Inventor： SCHARRENBURG GUSTAAF J M VAN ,  PRAS-RAVES MARIA L ,  VLIET BERNARD J VAN ,  KEIZER HISKIAS G ,  FEENSTRA ROELOF W

IPC: C07D285/01 ,  A61K31/425 ,  A61K31/427 ,  A61P25/28 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]- dithiazolidine-3,5-diylidene-diamine derivatives as inducers of glutha-thione-S- transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament useful in the for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): wherein the symbols have the meanings given in the specification.

公开(公告)号：BRPI0607547A2

公开(公告)日：2010-04-06

申请号：BRPI0607547

申请日：2006-02-08

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  KEIZER HISKIAS G ,  PRAS-RAVES MARIA L ,  VAN SCHARRENBURG GUSTAAF J M ,  VAN VLIET BERNARD J

IPC: C07D285/01 ,  A61K31/425 ,  A61K31/427 ,  A61P25/28 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]- dithiazolidine-3,5-diylidene-diamine derivatives as inducers of glutha-thione-S- transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament useful in the for prophylaxis and treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): wherein the symbols have the meanings given in the specification.

公开(公告)号：ES2317335T3

公开(公告)日：2009-04-16

申请号：ES05816322

申请日：2005-12-06

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  STOIT AXEL ,  TERPSTRA JAN-WILLEM ,  PRAS-RAVES MARIA L ,  MCCREARY ANDREW C ,  VAN VLIET BERNARD J

IPC: A61K31/423 ,  A61P25/00 ,  C07D263/58

Abstract: Compuestos de fórmula general (1): ** ver fórmula** en donde X= Su O, R1 es H, alquilo(C1-C6), CF3, CH2CF3, OH u O-alquilo(C1-C6), R 2 es H, alquilo(C 1-C 6), halógeno o ciano, R3 es H ó alquilo(C1-C6), R 4 es H, alquilo(C 1-C 6), opcionalmente sustituido con un átomo de halógeno, en donde: ** ver fórmula** se selecciona del grupo que consiste en:** ver fórmula** y los tautómeros, estereoisómeros y N-óxidos de los mismos, así como las sales, hidratos y solvatos farmacológicamente aceptables de dichos compuestos de fórmula (1) y sus tautómeros, estereoisómeros y N-óxidos.

公开(公告)号：PT1919883E

公开(公告)日：2009-03-26

申请号：PT06778284

申请日：2006-08-21

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  MCCREARY ANDREW C ,  HESSELINK MAYKE B ,  KOOPMAN THEODORUS S M ,  KOSTER HENDRIK J ,  AMSTERDAM PETER H VAN ,  VERHAGE MARINUS ,  SCHARRENBURG GUSTAAF J M VAN

IPC: C07D263/58 ,  A61K31/423 ,  A61P25/00 ,  C07D263/00 ,  C07D295/00 ,  C07D295/24

公开(公告)号：AR064275A1

公开(公告)日：2009-03-25

申请号：ARP070105532

申请日：2007-12-11

Applicant: SOLVAY PHARM BV

Inventor： SMID PIETER ,  FEENSTRA ROELOF W ,  KRUSE CORNELIS G

IPC: C07K5/06 ,  A61K38/05 ,  A61P25/16 ,  A61P25/00 ,  A61P9/00

Abstract: Inhibidores selectivos de las enzimas que degradan la neurotensina, composiciones que contienen estos compuestos, métodos para preparar los compuestos, métodos para preparar novedosos intermediarios utiles en su síntesis, y métodos para preparar composiciones. También se refiere a los usos de tales compuestos y composiciones, particularmente su uso en la fabricacion de medicamentos para regular la presion sanguínea o el vaciamiento gástrico, o tratar la enfermedad de Parkinson, ansiedad, depresion o psicosis. Reivindicacion 1: Un compuesto de formula (1), o un tautomero, estereoisomero, N-oxido, análogo isotopicamente marcado, o una sal, hidrato o solvato farmacologicamente aceptable de cualquiera de los mismos, en donde: R1 representa un grupo arilo monocíclico, heteroarilo monocíclico, arilo bicíclico o heteroarilo bicíclico, los cuales grupos están opcionalmente sustituidos, n es un entero y puede tener los valores 3, 4 o 5 cuando R1 representa grupos arilo o heteroarilo monocíclicos, y los valores 1, 2, 3, 4 o 5 cuando R1 representa grupos arilo o heteroarilo bicíclicos, R2 representa un átomo de hidrogeno o alquilo C1-3, o R2 y R3, junto con los átomos a los cuales están unidos, pueden formar un anillo de cinco o seis miembros que puede contener un átomo de azufre, R3 representa un átomo de hidrogeno, alquilo C1-8 ramificado o no ramificado o un grupo bencilo opcionalmente sustituido, R4 representa un átomo de hidrogeno, alquilo C1-8 ramificado o no ramificado o bencilo opcionalmente sustituido, R5 representa hidrogeno, metilo, etilo, metoximetilo o etoximetilo.

公开(公告)号：DE602006004363D1

公开(公告)日：2009-01-29

申请号：DE602006004363

申请日：2006-08-21

Applicant: SOLVAY PHARM BV

Inventor： KOOPMAN THEODORUS S ,  KOSTER HENDRIK J ,  VAN AMSTERDAM PETER H ,  FEENSTRA ROELOF W ,  VERHAGE MARINUS ,  MCCREARY ANDREW C ,  HESSELINK MAYKE B ,  VAN SCHARRENBURG GUSTAAF J

IPC: C07D263/58 ,  A61K31/423 ,  A61P25/00 ,  C07D295/24

Abstract: The present invention relates to N-oxides of certain piperazine and piperidine derivatives and to methods for the preparation of these compounds. The invention also relates to the use of compounds disclosed herein for the manufacture of a medicament giving a beneficial effect. A beneficial effect is disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. The invention also relates to the use of a compound of the invention for the manufacture of a medicament for treating or preventing a disease or condition. More particularly, the invention relates to a new use for the treatment of a disease or condition disclosed herein or apparent to a person skilled in the art from the specification and general knowledge in the art. In embodiments of the invention specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment of CNS-disorders, in particular the treatment of anxiety disorders, including generalized anxiety disorder and panic disorder, obsessive compulsive disorder, aggression, addiction (including craving), depression, autism, vertigo, schizophrenia and other psychotic disorders, Parkinson's disease and disturbances of cognition and memory. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.

公开(公告)号：DK1827427T3

公开(公告)日：2008-11-24

申请号：DK05850037

申请日：2005-12-06

Applicant: SOLVAY PHARM BV

Inventor： FEENSTRA ROELOF W ,  STOIT AXEL ,  TERPSTRA JAN-WILLEM ,  PRAS-RAVES MARIA L ,  MCCREARY ANDREW C ,  VAN VLIET BERNARD J ,  HESSELINK MAYKE B ,  KRUSE CORNELIS G ,  VAN SCHARRENBURG GUSTAAF J M

IPC: A61K31/423 ,  A61P25/00 ,  C07D263/58 ,  C07D413/12

Abstract: The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine -D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1) wherein the symbols have the meanings given in the specification.