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公开(公告)号：US08609685B2
公开(公告)日：2013-12-17
申请号：US12741862
申请日：2008-11-05
申请人： Carlo Scolastico , Leonardo Pierpaolo Manzoni , Pierfausto Seneci , Laura Belvisi , Domenico Delia , Martino Bolognesi , Eloise Mastrangelo , Mario De Mayo De Mari Milani , Ilaria Motto , Carmelo Drago
发明人： Carlo Scolastico , Leonardo Pierpaolo Manzoni , Pierfausto Seneci , Laura Belvisi , Domenico Delia , Martino Bolognesi , Eloise Mastrangelo , Mario De Mayo De Mari Milani , Ilaria Motto , Carmelo Drago
IPC分类号： A01N43/42 , A01N43/00 , A61K31/44 , A61K31/55 , C07D451/00 , C07D453/00 , C07D455/00
CPC分类号： C07D487/04 , C07K5/0808
摘要： The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
摘要翻译： 本发明涉及具有作为细胞凋亡蛋白抑制剂（IAP）抑制剂功能的Smac的构象约束模拟物的化合物，本发明还涉及这些化合物在治疗中的用途，其中诱导凋亡性细胞死亡是有益的，特别是在 治疗癌症，单独或与其他活性成分组合。
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公开(公告)号：US20100267692A1
公开(公告)日：2010-10-21
申请号：US12741862
申请日：2008-11-05
申请人： Carlo Scolastico , Leonardo Pierpaolo Manzoni , Pierfausto Seneci , Laura Belvisi , Domenico Delia , Martino Bolognesi , Eloise Mastrangelo , Mario Milani , Ilaria Motto , Carmelo Drago
发明人： Carlo Scolastico , Leonardo Pierpaolo Manzoni , Pierfausto Seneci , Laura Belvisi , Domenico Delia , Martino Bolognesi , Eloise Mastrangelo , Mario Milani , Ilaria Motto , Carmelo Drago
IPC分类号： A61K31/55 , C07D487/14 , C07D487/04 , A61P35/00
CPC分类号： C07D487/04 , C07K5/0808
摘要： The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
摘要翻译： 本发明涉及具有作为细胞凋亡蛋白抑制剂（IAP）抑制剂功能的Smac的构象约束模拟物的化合物，本发明还涉及这些化合物在治疗中的用途，其中诱导凋亡性细胞死亡是有益的，特别是在 治疗癌症，单独或与其他活性成分组合。
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公开(公告)号：US09730976B2
公开(公告)日：2017-08-15
申请号：US15071677
申请日：2016-03-16
申请人： Pierfausto Seneci , Laura Belvisi , Federica Cossu , Domenico Delia , Carmelo Drago , Daniele Lecis , Stefano Maiorana , Leonardo Pierpaolo Manzoni , Eloise Mastrangelo , Mario Milani de Mayo de Mari , Paola Maria Chiara Perego , Francesca Vasile
发明人： Pierfausto Seneci , Laura Belvisi , Federica Cossu , Domenico Delia , Carmelo Drago , Daniele Lecis , Stefano Maiorana , Leonardo Pierpaolo Manzoni , Eloise Mastrangelo , Mario Milani de Mayo de Mari , Paola Maria Chiara Perego , Francesca Vasile
IPC分类号： A61K31/5517 , A61K38/07 , C07K5/083 , C07D519/00 , A61K38/06 , A61K45/06 , C07K5/103 , A61K38/00
CPC分类号： A61K38/07 , A61K38/00 , A61K38/06 , A61K45/06 , C07D519/00 , C07K5/0804 , C07K5/0806 , C07K5/0808 , C07K5/1005 , C07K5/1008 , C07K5/101
摘要： The present invention relates to conformationally constrained homo- and heterodimeric mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
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公开(公告)号：US20160317605A1
公开(公告)日：2016-11-03
申请号：US15071677
申请日：2016-07-21
申请人： Pierfausto Seneci , Laura Belvisi , Federica Cossu , Domenico Delia , Carmelo Drago , Daniele Lecis , Stefano Maiorana , Leonardo Pierpaolo Manzoni , Eloise Mastrangelo , Mario Milani de Mayo de Mari , Paola Maria Chiara Perego , Francesca Vasile
发明人： Pierfausto Seneci , Laura Belvisi , Federica Cossu , Domenico Delia , Carmelo Drago , Daniele Lecis , Stefano Maiorana , Leonardo Pierpaolo Manzoni , Eloise Mastrangelo , Mario Milani de Mayo de Mari , Paola Maria Chiara Perego , Francesca Vasile
CPC分类号： A61K38/07 , A61K38/00 , A61K38/06 , A61K45/06 , C07D519/00 , C07K5/0804 , C07K5/0806 , C07K5/0808 , C07K5/1005 , C07K5/1008 , C07K5/101
摘要： The present invention relates to conformationally constrained homo- and heterodimeric mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
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5.发明授权公开(公告)号：US09321808B2
公开(公告)日：2016-04-26
申请号：US14379675
申请日：2012-02-20
申请人： Pierfausto Seneci , Laura Belvisi , Federica Cossu , Domenico Delia , Carmelo Drago , Daniele Lecis , Stefano Maiorana , Leonardo Pierpaolo Manzoni , Eloise Mastrangelo , Mario Milani de Mayo de Mari , Paola Maria Chiara Perego , Francesca Vasile
发明人： Pierfausto Seneci , Laura Belvisi , Federica Cossu , Domenico Delia , Carmelo Drago , Daniele Lecis , Stefano Maiorana , Leonardo Pierpaolo Manzoni , Eloise Mastrangelo , Mario Milani de Mayo de Mari , Paola Maria Chiara Perego , Francesca Vasile
IPC分类号： C07D487/04 , C07K5/103 , C07K5/083 , C07D519/00 , A61K38/06 , A61K38/07 , A61K45/06 , A61K38/00
CPC分类号： A61K38/07 , A61K38/00 , A61K38/06 , A61K45/06 , C07D519/00 , C07K5/0804 , C07K5/0806 , C07K5/0808 , C07K5/1005 , C07K5/1008 , C07K5/101
摘要： The present invention relates to conformationally constrained homo- and heterodimeric mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
摘要翻译： 本发明涉及具有作为细胞凋亡蛋白抑制剂（IAP）抑制剂的功能的Smac的构象约束的同型和异二聚体模拟物，本发明还涉及这些化合物在治疗中的用途，其中凋亡细胞死亡的诱导是有益的， 特别是在癌症的治疗中，单独或与其它活性成分组合。
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6.发明申请New Homo- and Heterodimeric SMAC Mimetic Compounds as Apoptosis Inducers 有权新型均质和异二聚体SMAC模拟化合物作为细胞凋亡诱导剂公开(公告)号：US20150119342A1
公开(公告)日：2015-04-30
申请号：US14379675
申请日：2012-02-20
申请人： Pierfausto Seneci , Laura Belvisi , Federica Cossu , Domenico Delia , Carmelo Drago , Daniele Lecis , Stefano Maiorana , Leonardo Pierpaolo Manzoni , Eloise Mastrangelo , Mario Milani de Mayo de Mari , Paola Maria Chiara Perego , Francesca Vasile
发明人： Pierfausto Seneci , Laura Belvisi , Federica Cossu , Domenico Delia , Carmelo Drago , Daniele Lecis , Stefano Maiorana , Leonardo Pierpaolo Manzoni , Eloise Mastrangelo , Mario Milani de Mayo de Mari , Paola Maria Chiara Perego , Francesca Vasile
CPC分类号： A61K38/07 , A61K38/00 , A61K38/06 , A61K45/06 , C07D519/00 , C07K5/0804 , C07K5/0806 , C07K5/0808 , C07K5/1005 , C07K5/1008 , C07K5/101
摘要： The present invention relates to conformationally constrained homo- and heterodimeric mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.
摘要翻译： 本发明涉及具有作为细胞凋亡蛋白抑制剂（IAP）抑制剂的功能的Smac的构象约束的同型和异二聚体模拟物，本发明还涉及这些化合物在治疗中的用途，其中凋亡细胞死亡的诱导是有益的， 特别是在癌症的治疗中，单独或与其它活性成分组合。
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7.发明授权Basic proline-amide derivatives of GE 2270 and GE 2270-like antibiotics 失效GE 2270和GE 2270样抗生素的基本脯氨酰胺衍生物
公开(公告)号：US6143739A
公开(公告)日：2000-11-07
申请号：US875707
申请日：1997-07-31
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention refers to basic amides derivatives of GE 2270 and GE 2270-like antibiotics of general formula (1), wherein the group GE represents the antibiotic core molecule. The amide derivatives of antibiotic GE 2270 of formula (I) are antimicrobial agents mainly active against gram positive bacteria. ##STR1##
摘要翻译： PCT No.PCT / EP96 / 00407 Sec。 371日期1997年7月31日 102（e）日期1997年7月31日PCT提交1996年2月1日PCT公布。 出版物WO96 / 24607 日期：1996年8月15日本发明涉及GE 2270的碱性酰胺衍生物和通式（1）的GE2270样抗生素，其中GE代表抗生素核心分子。 式（I）抗生素GE2270的酰胺衍生物是主要对革兰氏阳性细菌有活性的抗微生物剂。
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公开(公告)号：US5985905A
公开(公告)日：1999-11-16
申请号：US214648
申请日：1999-05-05
IPC分类号： A61K31/404 , A61K31/427 , A61P19/10 , A61P31/12 , A61P35/00 , C07D403/06 , C07D405/06 , C07D417/06 , A61K31/405 , A61K31/425
CPC分类号： C07D403/06 , C07D405/06 , C07D417/06
摘要： The invention relates to indole compounds, a process for preparing, pharmaceutical compositions containing the compounds and treating diseases associated with over activity of osteoclasts.
摘要翻译： PCT No.PCT / EP97 / 03711 Sec。 371日期1999年5月5日 102（e）日期1999年5月5日PCT 1997年7月7日PCT公布。 第WO98 / 01445号公报 日本1998年1月15日本发明涉及吲哚化合物，一种制备含有该化合物的药物组合物和治疗与破骨细胞的过度活性相关的疾病的方法。
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9.发明授权N-carbacycle monosubstituted indolocarbazoles as protein kinase inhibitors 失效N-半胱氨酸单取代的吲哚卡巴唑作为蛋白激酶抑制剂公开(公告)号：US07262215B2
公开(公告)日：2007-08-28
申请号：US10496505
申请日：2002-12-04
申请人： Heidi Sahagun-Krause , Olivier Thillaye Du Boullay , Valerie Thillaye Du Boullay , Laura Casiraghi , Hans-Wolfgang Klafki , Pierfausto Seneci , Tobias Braxmeier , Silvia Müller , Wolfgang Fr{hacek over (o)}hner , Barbara Monse , Sandra Gordon , Hanno M. Roder
发明人： Heidi Sahagun-Krause , Olivier Thillaye Du Boullay , Valerie Thillaye Du Boullay , Laura Casiraghi , Hans-Wolfgang Klafki , Pierfausto Seneci , Tobias Braxmeier , Silvia Müller , Wolfgang Fr{hacek over (o)}hner , Barbara Monse , Sandra Gordon , Hanno M. Roder
IPC分类号： A61K31/4035 , A61K31/5377 , A61K31/4192 , A61K31/407 , C07D249/04 , C07D413/14 , C07D487/14 , C09B5/26
CPC分类号： C07D487/14
摘要： This invention relates to N-carbacycle monosubstituted indolocarbazole compounds. Furthermore, this invention relates to medicaments comprising N-carbacycle monosubstituted indolocarbazoles compounds and the use of such compounds for treating non-insulin dependent diabetes mellitus, acute stroke and other neurotraumatic injuries, for treating diabetes mellitus, as a chemotherapeutic for the treatment of various malignant diseases, for treating diseases caused by malfunctioning of specific signaling pathways, and for treating neurodegenerative diseases such as for example Alzheimer's disease.
摘要翻译： 本发明涉及N-碳酸酯单取代的吲哚咔唑化合物。 此外，本发明涉及包含N-碳酸酯单取代的吲哚并唑化合物的药物，以及这些化合物用于治疗非胰岛素依赖性糖尿病，急性中风和其他神经创伤性损伤的用途，用于治疗糖尿病，作为治疗各种恶性肿瘤的化学治疗剂 疾病，用于治疗由特异性信号通路异常引起的疾病，以及用于治疗神经变性疾病例如阿尔茨海默氏病。
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公开(公告)号：US5500410A
公开(公告)日：1996-03-19
申请号：US461208
申请日：1995-06-05
CPC分类号： C07K9/008
摘要： The present invention is directed to new C.sup.63 amide derivatives of teicoplanin wherein the amide moiety is derived from a di- or poly-alkylamine, and to a process for preparing them. The derivatives are prepared by reacting a teicoplanin-like product with an active ester forming reagent such as chloroacetonitrile and then contacting said active ester with the appropriate di- or poly-alkylamine. The amide derivatives of the invention are active against gram positive and gram negative bacteria.
摘要翻译： 本发明涉及替考拉宁的新C63酰胺衍生物，其中酰胺部分衍生自二 - 或多 - 烷基胺，以及制备它们的方法。 通过使替考拉宁样产物与活性酯形成试剂如氯乙腈反应制备衍生物，然后使所述活性酯与合适的二 - 或多烷基胺接触。 本发明的酰胺衍生物对革兰氏阳性菌和革兰氏阴性菌具有活性。
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