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1. 发明申请

WO2004029622A2 ANTIBODY TOOLS FOR THE DIAGNOSTIC USE IN THE MEDICAL THERAPY WITH INHIBITORS OF HISTONE DEACETYLASES 审中-公开
标题翻译：用于药物治疗的药物治疗用抗生素的工具与抗体脱乙酰壳多糖的抑制剂
公开(公告)号：WO2004029622A2
公开(公告)日：2004-04-08
申请号：PCT/EP0310842
申请日：2003-09-30
申请人： G2M CANCER DRUGS AG , PELICCI PIER GIUSEPPE , MINUCCI SAVERIO , PICCINI DANIELE , MACCARANA MARCO , RONZONI SIMONA , ARECES LILIANA BEATRIZ , FARETTA MARCO
发明人： PELICCI PIER GIUSEPPE , MINUCCI SAVERIO , PICCINI DANIELE , MACCARANA MARCO , RONZONI SIMONA , ARECES LILIANA BEATRIZ , FARETTA MARCO
IPC分类号： C07K16/18 , C12Q1/44 , G01N33/50
CPC分类号： C12Q1/44 , C07K16/18
摘要： The invention relates to a method for determining whether a treatment of a disorder with an HDAC inhibitor is to be started/continued or not comprising determining the level of histone acetylation in the sample by use of an antibody capable of binding to acetylated histone, and classifying the disorder as to be treated with an HDAC inhibitor when the level of histone acetylation is significantly lower than that of a reference sample. The invention further relates to the diagnostic and prognostic use of specific antibodies and cell lines producing them.
摘要翻译：本发明涉及一种用于确定是否开始/继续使用HDAC抑制剂治疗病症的方法，包括通过使用能够结合乙酰化组蛋白的抗体来确定样品中组蛋白乙酰化的水平，并分类当组蛋白乙酰化水平显着低于参考样品的水平时，用HDAC抑制剂治疗的病症。本发明还涉及特异性抗体和产生它们的细胞系的诊断和预测性应用。

2. 发明申请

WO2004027418A3 THE USE OF MOLECULAR MARKERS FOR THE PRECLINICAL AND CLINICAL PROFILING OF INHIBITORS OF ENZYMES HAVING HISTONE DEACETYLASE ACTIVITY 审中-公开
标题翻译：分子标记用于具有组织脱乙酰酶活性的酶抑制剂的临床和临床分类的使用
公开(公告)号：WO2004027418A3
公开(公告)日：2004-05-13
申请号：PCT/EP0310404
申请日：2003-09-18
申请人： G2M CANCER DRUGS AG , KARLSRUHE FORSCHZENT , HEINZEL THORSTEN , KRAEMER OLIVER H , GOETTLICHER MARTIN , ZHU PING , GOLEBIEWSKI MARTIN , PELICCI PIER GIUSEPPE , MAURER ALEXANDER B , HENTSCH BERND , MINUCCI SAVERIO
发明人： HEINZEL THORSTEN , KRAEMER OLIVER H , GOETTLICHER MARTIN , ZHU PING , GOLEBIEWSKI MARTIN , PELICCI PIER GIUSEPPE , MAURER ALEXANDER B , HENTSCH BERND , MINUCCI SAVERIO
IPC分类号： C12Q1/68 , G01N33/48 , G01N33/573 , G01N33/574
CPC分类号： G01N33/6875 , C12Q1/6883 , C12Q1/6886 , C12Q2600/106 , C12Q2600/136 , G01N33/573 , G01N33/574 , G01N2333/70578 , G01N2333/9015 , G01N2333/916 , G01N2500/04
摘要： The present invention relates to the use of molecular markers and related signaling mechanisms for the preclinical and clinical profiling of inhibitors of enzymes having histone deacetylase activity. The invention also relates to the use of such markers as diagnostic and/or prognostic tools for the treatment of tumor patients with such inhibitors.
摘要翻译：本发明涉及分子标记和相关信号传导机制在具有组蛋白脱乙酰酶活性的酶抑制剂的临床前和临床分析中的用途。本发明还涉及这种标记物作为用于治疗具有这种抑制剂的肿瘤患者的诊断和/或预后工具的用途。

3. 发明申请

WO03024442A3 VALPROIC ACID AND DERIVATIVES FOR THE COMBINATORIAL THERAPEUTIC TREATMENT OF HUMAN CANCERS AND FOR THE TREATMENT OF TUMOR METASTASIS AND MINIMAL RESIDUAL DISEASE 审中-公开
标题翻译：人类癌症组合治疗和治疗肿瘤转移和最小残疾的病毒和衍生物
公开(公告)号：WO03024442A3
公开(公告)日：2003-09-18
申请号：PCT/EP0210419
申请日：2002-09-17
申请人： G2M CANCER DRUGS AG , GRONER BERND , HEINZEL THORSTEN , HENTSCH BERND , WELS WINFRIED STEPHAN , HERRLICH PETER A , MINUCCI SAVERIO , PELICCI PIER GIUSEPPE , GOETTLICHER MARTIN
发明人： GRONER BERND , HEINZEL THORSTEN , HENTSCH BERND , WELS WINFRIED STEPHAN , HERRLICH PETER A , MINUCCI SAVERIO , PELICCI PIER GIUSEPPE , GOETTLICHER MARTIN
IPC分类号： G01N33/50 , A61K31/19 , A61K31/20 , A61K31/203 , A61K31/28 , A61K31/59 , A61K31/593 , A61K39/00 , A61K39/395 , A61K45/00 , A61K45/06 , A61P35/00 , A61P43/00 , G01N33/15 , G01N33/53 , G01N33/566 , G01N33/574 , A61K31/282 , A61K41/00
CPC分类号： A61K45/06 , A61K31/19 , A61K31/20 , A61K31/28 , A61K31/59 , A61K2300/00
摘要： The present invention relates to the use of the drug valproic acid and derivatives thereof as inhibitors of enzymes having histone deacetylase for the sensitizing treatment of human cancers in combination with established therapeutic principles. The invention also relates to the use of those compounds for the treatment of tumor metastasis and minimal residual disease. Another aspect of the invention is a method for the identification of substance being useful for combinatorial cancer therapy and a diagnostic method to identify tumors comprising the step of testing in vitro whether a tumor is responsive to treatment with combinations of VPA or derivatives thereof and established tumor therapeutics.The invention includes the manufacture of a clinically used substance for the treatment of human cancers.
摘要翻译：本发明涉及药物丙戊酸及其衍生物作为具有组蛋白脱乙酰酶的酶抑制剂用于人类癌症的敏化治疗以及既定治疗原理的用途。本发明还涉及这些化合物用于治疗肿瘤转移和最小残留疾病的用途。本发明的另一方面是用于鉴定可用于组合癌症治疗的物质的方法和用于鉴定肿瘤的诊断方法，其包括在体外测试肿瘤是否对VPA或其衍生物的组合进行治疗和建立的肿瘤的反应本发明包括制备用于治疗人类癌症的临床用途物质。

4. 发明申请

WO0173433A3 METHODS RELATING TO SELF-INTERACTING OLIGOMERIC COMPLEXES 审中-公开
标题翻译：与自交互作用复合物相关的方法
公开(公告)号：WO0173433A3
公开(公告)日：2002-04-18
申请号：PCT/GB0101274
申请日：2001-03-22
申请人： CANCER RES VENTURES LTD , MINUCCI SAVERIO , PELICCI PIER GIUSEPPE
发明人： MINUCCI SAVERIO , PELICCI PIER GIUSEPPE
IPC分类号： G01N33/50 , G01N33/68
CPC分类号： G01N33/5011
摘要： The invention provides materials and methods capable of modulating the strong-self-association of chimeric transcription factors to form high molecular weight (HMW) complexes. The invention further provides compounds comprising the oligomerization domains of oligomeric substances and a polypeptide for modulating the activity of that polypeptide intra or inter-cellularly.
摘要翻译：本发明提供能够调节嵌合转录因子的强自身结合以形成高分子量（HMW）复合物的材料和方法。本发明进一步提供了包含寡聚物质的寡聚化结构域的化合物和用于调节多肽内部或细胞内活性的多肽。

5. 发明专利

IL182237A HISTONE DEACETYLASE INHIBITORS, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND USE THEREOF 未知
公开(公告)号：IL182237A
公开(公告)日：2012-03-29
申请号：IL18223707
申请日：2007-03-27
申请人： DAC SRL , MINUCCI SAVERIO , PELICCI PIER GIUSEPPE , MAI ANTONELLO , BALLARINI MARCO , GARGIULO GAETANO , MASSA SILVIO
发明人： MINUCCI SAVERIO , PELICCI PIER GIUSEPPE , MAI ANTONELLO , BALLARINI MARCO , GARGIULO GAETANO , MASSA SILVIO
摘要： New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.

6. 发明专利

CA2500384A1 ANTIBODY TOOLS FOR THE DIAGNOSTIC USE IN THE MEDICAL THERAPYWITH INHIBITORS OF HISTONE DEACETYLASES 未知
公开(公告)号：CA2500384A1
公开(公告)日：2004-04-08
申请号：CA2500384
申请日：2003-09-30
申请人： G2M CANCER DRUGS AG
发明人： PELICCI PIER GIUSEPPE , ARECES LILIANA BEATRIZ , PICCINI DANIELE , MINUCCI SAVERIO , MACCARANA MARIO , FARETTA MARCO , RONZONI SIMONA
IPC分类号： C07K16/18 , C12Q1/44 , G01N33/50
摘要： The invention relates to a method for determining whether a treatment of a disorder with an HDAC inhibitor is to be started/continued or not comprising determining the level of histone acetylation in the sample by use of an antibody capable of binding to acetylated histone, and classifying the disorder as to be treated with an HDAC inhibitor when the level of histone acetylation is significantly lower than that of a reference sample. The invention further relates to the diagnostic and prognostic use of specific antibodies and cell lines producing them.

7. 发明专利

CA2499685A1 THE USE OF MOLECULAR MARKERS FOR THE PRECLINICAL AND CLINICAL PROFILING OF INHIBITORS OF ENZYMES HAVING HISTONE DEACETYLASE ACTIVITY 未知
公开(公告)号：CA2499685A1
公开(公告)日：2004-04-01
申请号：CA2499685
申请日：2003-09-18
申请人： G2M CANCER DRUGS AG , KARLSRUHE FORSCHZENT
发明人： HEINZEL THORSTEN , PELICCI PIER GIUSEPPE , GOLEBIEWSKI MARTIN , MAURER ALEXANDER B , ZHU PING , MINUCCI SAVERIO , HENTSCH BERND , GOTTLICHER MARTIN , KRAMER OLIVER H
IPC分类号： C12Q1/68 , G01N33/48 , G01N33/573 , G01N33/574
摘要： The present invention relates to the use of molecular markers and related signaling mechanisms for the preclinical and clinical profiling of inhibitor s of enzymes having histone deacetylase activity. The invention also relates t o the use of such markers as diagnostic and/or prognostic tools for the treatment of tumor patients with such inhibitors.

8. 发明专利

AT314063T 未知
公开(公告)号：AT314063T
公开(公告)日：2006-01-15
申请号：AT02777129
申请日：2002-09-17
申请人： G2M CANCER DRUGS AG
发明人： GRONER BERND , HEINZEL THORSTEN , HENTSCH BERND , WELS WINFRIED STEPHAN , HERRLICH PETER A , MINUCCI SAVERIO , PELICCI PIER GIUSEPPE , GOETTLICHER MARTIN
IPC分类号： G01N33/50 , A61K31/19 , A61K31/20 , A61K31/203 , A61K31/28 , A61K31/59 , A61K31/593 , A61K39/00 , A61K39/395 , A61K45/00 , A61K45/06 , A61P35/00 , A61P43/00 , G01N33/15 , G01N33/53 , G01N33/566 , G01N33/574
摘要： The present invention relates to the use of the drug valporic acid and derivatives thereof as inhibitors of enzymes having histone deacetylase activity for the manufacture of a medicament to sensitize human cancer cells for treatment efficacy in combination with clinically established anti-cancer therapeutic drugs. The invention also relates to the treatment of tumor metastasis and minimal residual disease.

9. 发明专利

DE60208397D1 未知
公开(公告)号：DE60208397D1
公开(公告)日：2006-02-02
申请号：DE60208397
申请日：2002-09-17
申请人： G2M CANCER DRUGS AG
发明人： GRONER BERND , HEINZEL THORSTEN , HENTSCH BERND , WELS STEPHAN , HERRLICH A , MINUCCI SAVERIO , PELICCI GIUSEPPE , GOETTLICHER MARTIN
IPC分类号： G01N33/50 , A61K31/19 , A61K31/20 , A61K31/203 , A61K31/28 , A61K31/59 , A61K31/593 , A61K39/00 , A61K39/395 , A61K45/00 , A61K45/06 , A61P35/00 , A61P43/00 , G01N33/15 , G01N33/53 , G01N33/566 , G01N33/574
摘要： The present invention relates to the use of the drug valporic acid and derivatives thereof as inhibitors of enzymes having histone deacetylase activity for the manufacture of a medicament to sensitize human cancer cells for treatment efficacy in combination with clinically established anti-cancer therapeutic drugs. The invention also relates to the treatment of tumor metastasis and minimal residual disease.

10. 发明专利

AU2003271663A1 ANTIBODY TOOLS FOR THE DIAGNOSTIC USE IN THE MEDICAL THERAPY WITH INHIBITORS OF HISTONE DEACETYLASES 未知
公开(公告)号：AU2003271663A1
公开(公告)日：2004-04-19
申请号：AU2003271663
申请日：2003-09-30
申请人： G2M CANCER DRUGS AG
发明人： MACCARANA MARCO , RONZONI SIMONA , ARECES LILIANA BEATRIZ , FARETTA MARCO , PELICCI PIER GIUSEPPE , MINUCCI SAVERIO , PICCINI DANIELE
IPC分类号： C07K16/18 , C12Q1/44 , G01N33/50
摘要： Determining (M1) whether treatment of disorder with histone deacetylase (HDAC) inhibitor is to be started/continued/not by contacting sample from tissue affected by disorder with antibody binding to acetylated histone but not to deacetylated histone, determining histone level acetylation in sample and classifying disorder as to be treated with HDAC inhibitor when histone acetylation level is significantly less than control sample. Independent claims are also included for: (1) use of an antibody capable of binding to acetylated histone for determining whether a treatment of a disorder with an HDAC inhibitor is to be started/continued or not, and/or the classification of tumors; (2) an antibody (I) capable of binding to peptides having a sequence of Ser-Gly-Arg-Gly-Lys-Gly-Gly-Lys-Gly-Leu-Gly-Lys-Gly-Gly-Ala-Lys- Arg (histone H4 tail, mono-acetylated at lysine 8) (S1) and Ser-Gly-Arg-Gly-Lys-Gly-Gly-Lys-Gly-Leu-Gly-Lys-Gly-Gly-Ala-Lys- Arg (histone H4 tail, mono-acetylated at lysine 12) (S2) but not to anyone of the peptides having the sequences of Ser-Gly-Arg-Gly-Lys-Gly-Gly-Lys-Gly-Leu-Gly-Lys-Gly-Gly-Ala-Lys- Arg (histone H4 tail, mono-acetylated at lysine 16) (S3), Ser-Gly-Arg-Gly-Lys-Gly-Gly-Lys-Gly-Leu-Gly-Lys-Gly-Gly-Ala-Lys- Arg (non-acetylated peptide) (S4), Ala-Val-Cys-Asp-Lys-Cys-Leu-Lys-Phe-Tyr-Ser-Lys and Val-Trp-Asp-Gln-Glu-Phe-Leu-Lys-Val-Asp-Gln-Gly; (3) an antibody (II) capable of binding to peptides having (S1), (S2) and (S3) but not to peptides having (S4); (4) an antibody produced by a hybridoma cell line chosen from hybridoma cell lines G2M-T25-H4ac and G2M-T52-ac deposited at DSMZ; (5) a hybridoma cell line producing (I) or (II); (6) a hybridoma cell line which has the identifying characteristics of the cell line G2M-T25-H4ac deposited at DSMZ; (7) a hybridoma cell line which has the identifying characteristics of the cell line G2M-T52-ac deposited at DSMZ; (8) a diagnostic kit (III) for determining the level of histone acetylation containing an antibody capable of binding to acetylated histone but not to deacetylated histone, an HDAC inhibitor, and optionally, a secondary antibody directed against the antibody, and optionally reagents for the measurement of a signal derived from an antibody binding to acetylated histones; and (9) use of the antibodies T25 and/or T52 (IV) to direct substances conjugated to these antibodies to sites of histone hyperacetylation.

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