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1.发明申请[1,2,4]-DITHIAZOLI(DI)NE DERIVATIVES, INDUCERS OF GLUTHATHIONE-S-TRANSFERASE AND NADPH QUINONE OXIDO-REDUCTASE, FOR PROPHYLAXIS AND TREATMENT OF ADVERSE CONDITIONS ASSOCIATED WITH CYTOTOXICITY IN GENERAL AND APOPTOSIS IN PARTICULAR 审中-公开[1,2,4] - 二硫苏糖醇（DI）NE衍生物，谷胱甘肽硫转移酶和NADPH醌氧化还原酶的诱导剂，用于预防和治疗与一般细胞毒性和细胞凋亡有关的不利条件
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。
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公开(公告)号：DK1824479T3
公开(公告)日：2009-03-09
申请号：DK05816322
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 G J M
IPC: A61K31/423 , A61P25/00 , C07D263/58
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.
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公开(公告)号：AU2003250232B2
公开(公告)日：2008-09-11
申请号：AU2003250232
申请日：2003-05-28
Applicant: ARQULE INC , SOLVAY PHARM BV
Inventor： GUSTAFSON GARY R , PRAS-RAVES MARIA L , REINDERS JAN H , HARTOG JACOBUS A J DEN , SCHARRENBURG GUUSTAAF J M VAN
IPC: C07D251/42 , A61K31/53 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P3/10 , A61P7/02 , A61P7/06 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , A61P27/06 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/08 , A61P43/00 , C07D251/50 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14
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公开(公告)号：NO20072977L
公开(公告)日：2007-09-05
申请号：NO20072977
申请日：2007-06-11
Applicant: SOLVAY PHARM BV
Inventor： SCHARRENBURG GUSTAAF JOHAN MAR , FEENSTRA ROELOF W , KRUSE CORNELIS GERRIT , MCCREARY ANDREW C , PRAS-RAVES MARIA L , HESSELINK MAYKE B , TERPSTRA JAN-WILLEM , STOIT AXEL , VLIET BERNARD J VAN
IPC: C07D263/58 , A61K31/423 , A61P25/00 , 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.
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公开(公告)号：NO20072969A
公开(公告)日：2007-08-31
申请号：NO20072969
申请日：2007-06-11
Applicant: SOLVAY PHARM BV
Inventor： SCHARRENBURG GUSTAAF JOHAN MAR , FEENSTRA ROELOF W , KRUSE CORNELIS GERRIT , MCCREARY ANDREW C , PRAS-RAVES MARIA L , HESSELINK MAYKE B , TERPSTRA JAN-WILLEM , STOIT AXEL , VLIET BERNARD J VAN
IPC: C07D263/58
CPC classification number: C07D263/58 , C07D413/12
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Patent Agency Ranking
公开(公告)号：MX2007006817A
公开(公告)日：2007-07-24
申请号：MX2007006817
申请日：2005-12-06
Applicant: SOLVAY PHARM BV
Inventor： KRUSE CORNELIS G , TERPSTRA JAN-WILLEM , SCHARRENBURG GUSTAAF J M VAN , FEENSTRA ROELOF W , STOIT AXEL , PRAS-RAVES MARIA L , MCCREARY ANDREW C , VLIET BERNARD J VAN , HESSELINK MAYKE B
IPC: A61K31/00 , C07D263/58 , A61P25/00
Abstract: La invencion se refiere a un grupo de derivados novedosos de fenilpiperazina con un doble modo de accion: inhibicion de la reabsorcion de serotonina y agonismo parcial de receptores de dopamina-D2; la invencion tambien se refiere al uso de un compuesto que se describe en la presente para la fabricacion de un medicamento que tiene un efecto beneficioso; los compuestos tienen la formula general (1): (ver formula (1)) en donde los simbolos tienen los significados dados en la especificacion, y los tautomeros, estereoisomeros y N-oxidos de los mismos, asi como tambien las sales, hidratos y solvatos farmacologicamente aceptables de dichos compuestos de formula (1) y sus tautomeros, estereoisomeros y N-oxidos.
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公开(公告)号：CA2587202A1
公开(公告)日：2006-06-15
申请号：CA2587202
申请日：2005-12-06
Applicant: SOLVAY PHARM BV
Inventor： VAN SCHARRENBURG GUSTAAF J M , STOIT AXEL , TERPSTRA JAN-WILLEM , VAN VLIET BERNARD J , PRAS-RAVES MARIA L , MCCREARY ANDREW C , HESSELINK MAYKE B , KRUSE CORNELIS G , FEENSTRA ROELOF W
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.
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公开(公告)号：AU2005313312A1
公开(公告)日：2006-06-15
申请号：AU2005313312
申请日：2005-12-06
Applicant: SOLVAY PHARM BV
Inventor： HESSELINK MAYKE B , KRUSE CORNELIS G , VLIET BERNARD J VAN , TERPSTRA JAN-WILLEM , MCCREARY ANDREW C , FEENSTRA ROELOF W , STOIT AXEL , SCHARRENBURG GUSTAAF J M VAN , PRAS-RAVES MARIA L
IPC: A61K31/423 , A61P25/00 , 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.
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公开(公告)号：AU2003250232A1
公开(公告)日：2003-12-19
申请号：AU2003250232
申请日：2003-05-28
Applicant: SOLVAY PHARM BV , HARTOG JACOBUS A J , REINDERS JAN H , SCHARRENBURG GUUSTAAF J M VAN , PRAS RAVES MARIA L , GUSTAFSON GARY R
Inventor： HARTOG JACOBUS A J DEN , REINDERS JAN H , SCHARRENBURG GUUSTAAF J M VAN , PRAS-RAVES MARIA L , GUSTAFSON GARY R
IPC: C07D251/42 , A61K31/53 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P3/10 , A61P7/02 , A61P7/06 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/28 , A61P27/06 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/08 , A61P43/00 , C07D251/50 , C07D401/04 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14
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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.
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