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1. 发明申请

WO2004041258A8 CYCLIC NUCLEOTIDE PHOSPHODIESTERASE INHIBITORS, PREPARATION AND USES 审中-公开
标题翻译：循环核酸磷酸酯酶抑制剂，制备和用途
公开(公告)号：WO2004041258A8
公开(公告)日：2005-06-23
申请号：PCT/FR0303247
申请日：2003-10-30
申请人： NEURO3D , UNIV PASTEUR , CENTRE NAT RECH SCIENT , FORENAP , BOURGUIGNON JEAN-JACQUES , LUGNIER CLAIRE , ABARGHAZ MUSTAPHA , LAGOUGE YAN , WAGNER PATRICK , MONDADORI CESARE , MACHER JEAN-PAUL , SCHULTZ DOMINIQUE , RABOISSON PIERRE
发明人： BOURGUIGNON JEAN-JACQUES , LUGNIER CLAIRE , ABARGHAZ MUSTAPHA , LAGOUGE YAN , WAGNER PATRICK , MONDADORI CESARE , MACHER JEAN-PAUL , SCHULTZ DOMINIQUE , RABOISSON PIERRE
IPC分类号： A61K31/5513 , A61K31/5517 , A61P3/04 , A61P11/06 , A61P19/02 , A61P21/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P37/00 , C07D243/20 , C07D243/22 , C07D243/24 , C07D401/04 , C07D405/04 , C07D417/10 , C07D487/04
CPC分类号： C07D401/04 , A61K31/5513 , A61K31/5517 , C07D243/20 , C07D243/22 , C07D243/24 , C07D405/04 , C07D417/10 , C07D487/04
摘要： The invention concerns the use of PDE2 inhibitors for treating disorders of the central and peripheral nervous system, a method for therapeutic treatment by administering to an animal said inhibitors. More specifically, the invention concerns novel benzodiazepinone derivatives and their uses in therapeutics more particularly for treating pathologies involving activity of type 2 cyclic nucleotide phosphodiesterase. The invention also concerns methods for preparing same and novel synthesis intermediates.
摘要翻译：本发明涉及PDE2抑制剂用于治疗中枢和周围神经系统疾病的方法，一种通过向动物施用所述抑制剂进行治疗性治疗的方法。更具体地，本发明涉及新的苯并二氮杂酮衍生物及其在治疗学中的用途，更具体地涉及治疗涉及2型环核苷酸磷酸二酯酶活性的病理学。本发明还涉及制备相同和新型合成中间体的方法。

2. 发明申请

WO2004041258A2 CYCLIC NUCLEOTIDE PHOSPHODIESTERASE INHIBITORS, PREPARATION AND USES 审中-公开
标题翻译：循环核酸磷酸酯酶抑制剂，制备和用途
公开(公告)号：WO2004041258A2
公开(公告)日：2004-05-21
申请号：PCT/FR0303247
申请日：2003-10-30
申请人： NEURO3D , UNIV PASTEUR , CENTRE NAT RECH SCIENT , FORENAP , BOURGUIGNON JEAN-JACQUES , LUGNIER CLAIRE , ABARGHAZ MUSTAPHA , LAGOUGE YAN , WAGNER PATRICK , MONDADORI CESARE , MACHER JEAN-PAUL , SCHULTZ DOMINIQUE , RABOISSON PIERRE
发明人： BOURGUIGNON JEAN-JACQUES , LUGNIER CLAIRE , ABARGHAZ MUSTAPHA , LAGOUGE YAN , WAGNER PATRICK , MONDADORI CESARE , MACHER JEAN-PAUL , SCHULTZ DOMINIQUE , RABOISSON PIERRE
IPC分类号： A61K31/5513 , A61K31/5517 , A61P3/04 , A61P11/06 , A61P19/02 , A61P21/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P37/00 , C07D243/20 , C07D243/22 , C07D243/24 , C07D401/04 , C07D405/04 , C07D417/10 , C07D487/04 , A61K31/00
CPC分类号： C07D401/04 , A61K31/5513 , A61K31/5517 , C07D243/20 , C07D243/22 , C07D243/24 , C07D405/04 , C07D417/10 , C07D487/04
摘要： The invention concerns the use of PDE2 inhibitors for treating disorders of the central and peripheral nervous system, a method for therapeutic treatment by administering to an animal said inhibitors. More specifically, the invention concerns novel benzodiazepinone derivatives and their uses in therapeutics more particularly for treating pathologies involving activity of type 2 cyclic nucleotide phosphodiesterase. The invention also concerns methods for preparing same and novel synthesis intermediates.
摘要翻译：本发明涉及PDE2抑制剂用于治疗中枢和周围神经系统疾病的方法，一种通过向动物施用所述抑制剂进行治疗性治疗的方法。更具体地，本发明涉及新的苯并二氮杂酮衍生物及其在治疗学中的用途，更具体地涉及治疗涉及2型环核苷酸磷酸二酯酶活性的病理学。本发明还涉及制备相同和新型合成中间体的方法。

3. 发明专利

NZ540167A Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses 未知
公开(公告)号：NZ540167A
公开(公告)日：2007-06-29
申请号：NZ54016703
申请日：2003-10-30
申请人： NEURO3D , UNIV PASTEUR , CENTRE NAT RECH SCIENT , FORENAP
发明人： BOURGUIGNON JEAN-JACQUES , LUGNIER CLAIRE , LAGOUGE YAN , WAGNER PATRICK , MONDADORI CESARE , MACHER JEAN-PAUL , SCHULTZ DOMINIQUE , RABOISSON PIERRE , ABARGHAZ MUSTAPHA
IPC分类号： A61K31/5513 , A61K31/5517 , A61P3/04 , A61P11/06 , A61P19/02 , A61P21/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P37/00 , C07D243/20 , C07D243/22 , C07D243/24 , C07D401/04 , C07D405/04 , C07D417/10 , C07D487/04
摘要： Disclosed is a benzodiazepine derivative of formula (I) in which it substituents are as described in the specification. The compound is a PDE2 inhibitor useful for treating disorders of the central peripheral nervous system. More particularly the derivatives are utilised in treating pathologies involving activity of type 2 cyclic nucleotide phosphodiesterase.

4. 发明专利

AU2003288352A1 CYCLIC NUCLEOTIDE PHOSPHODIESTERASE INHIBITORS, PREPARATION AND USES 未知
公开(公告)号：AU2003288352A1
公开(公告)日：2004-06-07
申请号：AU2003288352
申请日：2003-10-30
申请人： CENTRE NAT RECH SCIENT , FORENAP , NEURO3D , UNIV PASTEUR
发明人： BOURGUIGNON JEAN-JACQUES , LUGNIER CLAIRE , ABARGHAZ MUSTAPHA , LAGOUGE YAN , WAGNER PATRICK , MONDADORI CESARE , MACHER JEAN-PAUL , SCHULTZ DOMINIQUE , RABOISSON PIERRE
IPC分类号： A61K31/5513 , A61K31/5517 , A61P3/04 , A61P11/06 , A61P19/02 , A61P21/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P37/00 , C07D243/20 , C07D243/22 , C07D243/24 , C07D401/04 , C07D405/04 , C07D417/10 , C07D487/04 , A61K31/00
摘要： The invention concerns the use of PDE2 inhibitors for treating disorders of the central and peripheral nervous system, a method for therapeutic treatment by administering to an animal said inhibitors. More specifically, the invention concerns novel benzodiazepinone derivatives and their uses in therapeutics more particularly for treating pathologies involving activity of a cyclic nucleotide phosphodiesterase type 2. The invention also concerns methods for preparing same and novel synthesis intermediates.

5. 发明专利

CA2503716A1 UTILISATION D'INHIBITEURS DES PHOSPHODIESTERASES DES NUCLEOTIDES CYCLIQUES, AYANT UNE STRUCTURE BENZODIAZEPINIQUE EN THERAPIE 未知
公开(公告)号：CA2503716A1
公开(公告)日：2004-05-21
申请号：CA2503716
申请日：2003-10-30
申请人： NEURO3D , CENTRE NAT RECH SCIENT , UNIV PASTEUR , FORENAP
发明人： SCHULTZ DOMINIQUE , RABOISSON PIERRE , MACHER JEAN-PAUL , WAGNER PATRICK , MONDADORI CESARE , LAGOUGE YAN , BOURGUIGNON JEAN-JACQUES , ABARGHAZ MUSTAPHA , LUGNIER CLAIRE
IPC分类号： A61K31/5513 , A61K31/5517 , A61P3/04 , A61P11/06 , A61P19/02 , A61P21/00 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P37/00 , C07D243/20 , C07D243/22 , C07D243/24 , C07D401/04 , C07D405/04 , C07D417/10 , C07D487/04
摘要： L'invention concerne l'utilisation d'inhibiteurs de PDE2 pour traiter des désordres du système nerveux central et périphérique, un procédé de traiteme nt thérapeutique par administration chez un animal de ces inhibiteurs. Elle concerne plus spécifiquement de nouveaux dérivés de type benzodiazépinones e t leurs applications dans le domaine thérapeutique tout particulièrement pour le traitement de pathologies impliquant l'activité d'une phosphodiestérase de nucléotides cycliques de type 2. Elle concerne également des procédés pour leur préparation et de nouveaux intermédiaires de synthèse.

7. 发明专利

CA2589106C PYRIDAZINE COMPOUNDS, COMPOSITIONS AND METHODS AND THEIR USE IN TREATING INFLAMMATORY DISEASES 未知
公开(公告)号：CA2589106C
公开(公告)日：2015-07-21
申请号：CA2589106
申请日：2005-11-02
申请人： UNIV NORTHWESTERN , UNIV PASTEUR , CENTRE NAT RECH SCIENT
发明人： WATTERSON D MARTIN , VAN ELDIK LINDA , HAIECH JACQUES , HIBERT MARCEL , BOURGUIGNON JEAN-JACQUES , VELENTZA ANASTASIA , HU WENHUI , ZASADZKI MAGDALENA
IPC分类号： C07D237/00 , A01N43/58 , A61K31/4965 , A61K31/50 , C07D237/02 , C07D403/00 , C07D405/00 , C07D409/00
摘要： The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.

8. 发明专利

DE60308182D1 未知
公开(公告)号：DE60308182D1
公开(公告)日：2006-10-19
申请号：DE60308182
申请日：2003-06-16
申请人： CENTRE NAT RECH SCIENT , UNIV PASTEUR
发明人： GALZI JEAN-LUC , HIBERT MARCEL , BOURGUIGNON JEAN-JACQUES , MAILLET EMELINE
IPC分类号： G01N33/557 , C07C229/14 , C07K5/068 , G01N33/15 , G01N33/50 , G01N33/542 , G01N33/566 , G01N33/58
摘要： Method for detecting an allosteric effector (I) of a receptor (R). Method for detecting an allosteric effector (I) of a receptor (R) comprises determining the variation of: (1) the kinetics of dissociation and/or association of the complex formed between R and its ligand (L); and/or (2) the amplitude of the binding between R and L, in presence of (I), relative to that in absence of (I). If the variation in amplitude is negative, then the variation is kinetics must also be measured. R and L are implicated in at least one biological response, under appropriate physiological conditions, and (I) modulates at least one such response. R is labeled with a fluorescent protein (FP), derived from cnidarians, or its derivative, having molar extinction coefficient over 14000 M to the power of -1 cm to the power of -1 and quantum yield of fluorescence over 0.38. L is labeled with: (1) an agent (A) that absorbs light emitted from FP; or (2) a fluorescent substance (FS). The measurement of variation in kinetics/binding is based on fluorescent energy transfer (FET) between (a) FP and FS, which is either excited at the emission wavelength of FP or emits at the wavelength of excitation of FP, or (b) FP and (A). An Independent claim is also included for 23 new compounds (X) identified by the new method.

9. 发明专利

CA2589102C PYRIDAZINE COMPOUNDS AND METHODS FOR USING THE COMPOUNDS TO TREAT INFLAMMATORY DISEASES 未知
公开(公告)号：CA2589102C
公开(公告)日：2013-08-13
申请号：CA2589102
申请日：2005-11-02
申请人： UNIV NORTHWESTERN , UNIV PASTEUR , CENTRE NAT RECH SCIENT
发明人： WATTERSON D MARTIN , VAN ELDIK LINDA , HAIECH JACQUES , HIBERT MARCEL , BOURGUIGNON JEAN-JACQUES , VELENTZA ANASTASIA , HU WENHUI , ZASADZKI MAGDALENA
IPC分类号： C07D237/26 , A61K31/50 , A61K31/5377 , C07D403/12 , C07D413/06
摘要： The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.

10. 发明专利

DE60308182T2 未知
公开(公告)号：DE60308182T2
公开(公告)日：2007-08-23
申请号：DE60308182
申请日：2003-06-16
申请人： CENTRE NAT RECH SCIENT , UNIV PASTEUR
发明人： GALZI JEAN-LUC , HIBERT MARCEL , BOURGUIGNON JEAN-JACQUES , MAILLET EMELINE
IPC分类号： G01N33/557 , C07C229/14 , C07K5/068 , G01N33/15 , G01N33/50 , G01N33/542 , G01N33/566 , G01N33/58
摘要： Method for detecting an allosteric effector (I) of a receptor (R). Method for detecting an allosteric effector (I) of a receptor (R) comprises determining the variation of: (1) the kinetics of dissociation and/or association of the complex formed between R and its ligand (L); and/or (2) the amplitude of the binding between R and L, in presence of (I), relative to that in absence of (I). If the variation in amplitude is negative, then the variation is kinetics must also be measured. R and L are implicated in at least one biological response, under appropriate physiological conditions, and (I) modulates at least one such response. R is labeled with a fluorescent protein (FP), derived from cnidarians, or its derivative, having molar extinction coefficient over 14000 M to the power of -1 cm to the power of -1 and quantum yield of fluorescence over 0.38. L is labeled with: (1) an agent (A) that absorbs light emitted from FP; or (2) a fluorescent substance (FS). The measurement of variation in kinetics/binding is based on fluorescent energy transfer (FET) between (a) FP and FS, which is either excited at the emission wavelength of FP or emits at the wavelength of excitation of FP, or (b) FP and (A). An Independent claim is also included for 23 new compounds (X) identified by the new method.

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