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1. 发明申请

US20120077806A1 Deubiquitinase Inhibitors and Methods for Use of the Same 有权
标题翻译：去泛素酶抑制剂及其使用方法
公开(公告)号：US20120077806A1
公开(公告)日：2012-03-29
申请号：US13241802
申请日：2011-09-23
申请人： Nicholas J. Donato , Christiane Wobus , Hollis D. Showalter , Moshe Talpaz , Jeffrey W. Perry , Roderick J. Sorenson , Mary X. O'Riordan , Yafei Jin
发明人： Nicholas J. Donato , Christiane Wobus , Hollis D. Showalter , Moshe Talpaz , Jeffrey W. Perry , Roderick J. Sorenson , Mary X. O'Riordan , Yafei Jin
IPC分类号： A61K31/541 , C12N5/02 , A61K31/5377 , A61K31/53 , A61K31/50 , C07D413/12 , A61K31/496 , A61K31/505 , A61K31/454 , A61K31/4439 , A61K31/44 , A61K31/433 , A61K31/4245 , A61K31/426 , A61K31/42 , A61K31/4164 , A61K31/415 , A61K31/165 , C07D417/12 , C07D253/065 , C07D253/04 , C07D237/06 , C07D239/02 , A61K31/4965 , C07D401/12 , C07D213/57 , C07D285/06 , C07D285/12 , C07D271/10 , C07D277/30 , C07D261/06 , C07D233/90 , C07D231/10 , C07C255/32 , A61P25/28 , A61P31/04 , A61P31/10 , A61P31/12 , A61P33/00 , A61P35/00 , C12N9/99
CPC分类号： C07D495/04 , C07C255/43 , C07D213/30 , C07D213/32 , C07D213/61 , C07D213/68 , C07D213/74 , C07D213/75 , C07D231/12 , C07D233/54 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/08 , C07D251/16 , C07D261/08 , C07D271/04 , C07D271/10 , C07D277/30 , C07D285/12 , C07D285/16 , C07D401/12 , C07D417/12 , C12N9/99
摘要： Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.
摘要翻译：本文公开了抑制去泛素酶（DUB），治疗病原体感染（例如病毒，细菌和/或寄生虫）的方法，抑制细胞增殖的方法，治疗神经变性疾病的方法，治疗一种或多种症状的方法的神经变性疾病或遗传性疾病，以及化合物。

2. 发明申请

US20070027167A1 Use of c-Src inhibitors alone or in combinaton with STI571 for the treatment of leukaemia 审中-公开
标题翻译：单独使用c-Src抑制剂或与STI571组合用于治疗白血病
公开(公告)号：US20070027167A1
公开(公告)日：2007-02-01
申请号：US11515981
申请日：2006-09-05
申请人： Nicholas Donato , Doriano Fabbro , Paul Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
发明人： Nicholas Donato , Doriano Fabbro , Paul Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
IPC分类号： A61K31/519
CPC分类号： A61K35/02 , A61K31/506 , A61K31/519
摘要： The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamdio]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine.
摘要翻译：本发明涉及一种组合，其包含（a）至少一种降低c-Src活性的化合物和（b）N- {5- [4-（4-甲基 - 哌嗪基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺或其单甲磺酸盐; 包含所述组合的药物组合物; 以及治疗具有白血病，特别是慢性骨髓性白血病的温血动物的方法，包括向所述动物施用至少一种抑制Src激酶家族成员，Tec激酶家族或Raf激酶抑制剂的活性的化合物，特别是抑制c-Src蛋白酪氨酸激酶活性或同时抑制c-Src蛋白酪氨酸激酶活性和Bcr-Abl酪氨酸激酶活性，单独或与Bcr-Abl抑制剂组合，特别是N- {5- [ 4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺。

3. 发明申请

US20110021805A1 COMPOUNDS FOR TREATMENT OF CELL PROLIFERATIVE DISEASES 有权
标题翻译：用于治疗细胞增殖性疾病的化合物
公开(公告)号：US20110021805A1
公开(公告)日：2011-01-27
申请号：US12824901
申请日：2010-06-28
申请人： Waldemar Priebe , Nicholas Donato , Moshe Talpaz , Slawomir Szymanski , Izabela Fokt , Alexander Levitzki
发明人： Waldemar Priebe , Nicholas Donato , Moshe Talpaz , Slawomir Szymanski , Izabela Fokt , Alexander Levitzki
IPC分类号： C07C255/44
CPC分类号： C07C255/44 , A61K31/277 , A61K45/06 , C07C255/41 , C07C255/42 , C07D213/57 , C07D213/61
摘要： The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as kinase inhibitors, cause the downregulation of c-myc, and inhibit the growth and survival of cancerous cell lines.
摘要翻译：本发明涉及化合物及其用于治疗细胞增殖性疾病如癌症的用途。本发明化合物显示出作为激酶抑制剂的显着效力，引起c-myc的下调，并抑制癌细胞系的生长和存活。

4. 发明申请

US20070149539A1 USE OF C-SRC INHIBITORS ALONE OR IN COMBINATION WITH STI571 FOR THE TREATMENT OF LEUKAEMIA 审中-公开
标题翻译：使用C-SRC抑制剂或与STI571组合用于治疗白血病
公开(公告)号：US20070149539A1
公开(公告)日：2007-06-28
申请号：US11679901
申请日：2007-02-28
申请人： Nicholas Donato , Doriano Fabbro , Paul Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
发明人： Nicholas Donato , Doriano Fabbro , Paul Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
IPC分类号： A61K31/506 , A61K31/497 , A61K31/519
CPC分类号： A61K35/02 , A61K31/506 , A61K31/519
摘要： The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamdio]-2-methylphenyl }-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N- {5- [4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl }-4-(3-pyridyl)-2-pyrimidine-amine.
摘要翻译：本发明涉及一种组合，其包含（a）至少一种降低c-Src活性的化合物和（b）N- {5- [4-（4-甲基 - 哌嗪基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺或其单甲磺酸盐; 包含所述组合的药物组合物; 以及治疗具有白血病，特别是慢性骨髓性白血病的温血动物的方法，包括向动物施用至少一种抑制Src激酶家族成员，Tec激酶家族或Raf激酶抑制剂的活性的化合物，特别是抑制c-Src蛋白酪氨酸激酶活性或同时抑制c-Src蛋白酪氨酸激酶活性和Bcr-Abl酪氨酸激酶活性，单独或与Bcr-Abl抑制剂组合，特别是N- {5- [ 4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺。

5. 发明申请

US20120214850A1 COMPOUNDS FOR TREATMENT OF CELL PROLIFERATIVE DISEASES 有权
标题翻译：用于治疗细胞增殖性疾病的化合物
公开(公告)号：US20120214850A1
公开(公告)日：2012-08-23
申请号：US13350637
申请日：2012-01-13
申请人： Waldemar Priebe , Nicholas Donato , Moshe Talpaz , Slawomir Szymanski , Izabela Fokt , Alexander Levitzki
发明人： Waldemar Priebe , Nicholas Donato , Moshe Talpaz , Slawomir Szymanski , Izabela Fokt , Alexander Levitzki
IPC分类号： A61K31/44 , A61P35/02 , A61P19/02 , A61P35/00 , A61P29/00 , A61P1/00
CPC分类号： C07C255/44 , A61K31/277 , A61K45/06 , C07C255/41 , C07C255/42 , C07D213/57 , C07D213/61
摘要： The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as kinase inhibitors, cause the downregulation of c-myc, and inhibit the growth and survival of cancerous cell lines.
摘要翻译：本发明涉及化合物及其用于治疗细胞增殖性疾病如癌症的用途。本发明化合物显示出作为激酶抑制剂的显着效力，引起c-myc的下调，并抑制癌细胞系的生长和存活。

6. 发明申请

US20070004748A1 Inhibition of osteolytic lesions by SRC kinase inhibitors 有权
标题翻译： SRC激酶抑制剂对溶骨性病变的抑制作用
公开(公告)号：US20070004748A1
公开(公告)日：2007-01-04
申请号：US11455272
申请日：2006-06-16
申请人： Bryant Darnay , Janet Price , Ann Poblenz , Moshe Talpaz
发明人： Bryant Darnay , Janet Price , Ann Poblenz , Moshe Talpaz
IPC分类号： A61K31/496 , A61K31/4709
CPC分类号： A61K31/44 , A61K31/47 , A61K31/4709 , A61K31/496
摘要： The present invention include methods and compositions for treating bone-resorbing diseases or bone resorption related to a pathologic condition generally, including, but not limited to osteoporosis, arthritis, rheumatoid arthritis, cancer metastases to the bone, bone cancer, hypercalcemia, osteolytic lesions with orthopedic implants, Paget's disease, and bone loss associated with hyperparathyroidism. Representative cancers include, but are not limited to breast cancer, prostrate cancer, colon cancer, endometrial cancer, multiple myeloma, renal cell carcinoma, heck and neck cancers, and cervical carcinoma. Arthritic conditions include, but are not limited to adjuvant-, collagen-, bacterial- and antigen-induced arthritis, particularly rheumatoid arthritis.
摘要翻译：本发明包括用于治疗与病理状况相关的骨吸收疾病或骨吸收的方法和组合物，通常包括但不限于骨质疏松症，关节炎，类风湿性关节炎，对骨骼的癌症转移，骨癌，高钙血症，溶骨性病变，骨科植入物，佩吉特病和与甲状旁腺机能亢进相关的骨丢失。代表性癌症包括但不限于乳腺癌，前列腺癌，结肠癌，子宫内膜癌，多发性骨髓瘤，肾细胞癌，颈部和颈部癌症以及宫颈癌。关节炎症状包括但不限于佐剂，胶原，细菌和抗原诱导的关节炎，特别是类风湿性关节炎。

7. 发明申请

US20060074094A1 Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia 失效
标题翻译：单独或与STI571组合使用c-Src抑制剂治疗白血病
公开(公告)号：US20060074094A1
公开(公告)日：2006-04-06
申请号：US11285664
申请日：2005-11-22
申请人： Nicholas Donato , Doriano Fabbro , Paul Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
发明人： Nicholas Donato , Doriano Fabbro , Paul Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
IPC分类号： A61K31/519
CPC分类号： A61K35/02 , A61K31/506 , A61K31/519
摘要： The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine.
摘要翻译：本发明涉及一种组合，其包含（a）至少一种降低c-Src活性的化合物和（b）N- {5- [4-（4-甲基 - 哌嗪基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺或其单甲磺酸盐; 包含所述组合的药物组合物; 以及治疗具有白血病，特别是慢性骨髓性白血病的温血动物的方法，包括向所述动物施用至少一种抑制Src激酶家族成员，Btk激酶家族，Tec激酶家族的活性的化合物或 Raf激酶抑制剂，特别是抑制c-Src蛋白酪氨酸激酶活性或同时抑制c-Src蛋白酪氨酸激酶活性和Bcr-Abl酪氨酸激酶活性，单独或与Bcr-Abl抑制剂组合，特别是N - {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺。

8. 发明授权

US08648102B2 Compounds for treatment of cell proliferative diseases 有权
标题翻译：用于治疗细胞增殖性疾病的化合物
公开(公告)号：US08648102B2
公开(公告)日：2014-02-11
申请号：US13350637
申请日：2012-01-13
申请人： Waldemar Priebe , Nicholas Donato , Moshe Talpaz , Slawomir Szymanski , Izabela Fokt , Alexander Levitzki
发明人： Waldemar Priebe , Nicholas Donato , Moshe Talpaz , Slawomir Szymanski , Izabela Fokt , Alexander Levitzki
IPC分类号： A61K31/44
CPC分类号： C07C255/44 , A61K31/277 , A61K45/06 , C07C255/41 , C07C255/42 , C07D213/57 , C07D213/61
摘要： The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as kinase inhibitors, cause the downregulation of c-myc, and inhibit the growth and survival of cancerous cell lines.
摘要翻译：本发明涉及化合物及其用于治疗细胞增殖性疾病如癌症的用途。本发明化合物显示出作为激酶抑制剂的显着效力，引起c-myc的下调，并抑制癌细胞系的生长和存活。

9. 发明授权

US08119649B2 Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia 失效
公开(公告)号：US08119649B2
公开(公告)日：2012-02-21
申请号：US12466186
申请日：2009-05-14
申请人： Nicholas J Donato , Doriano Fabbro , Paul W Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
发明人： Nicholas J Donato , Doriano Fabbro , Paul W Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
IPC分类号： A61K31/519
CPC分类号： A61K35/02 , A61K31/506 , A61K31/519
摘要： The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine.

10. 发明申请

US20090227608A1 USE OF C-SRC INHIBITORS ALONE OR IN COMBINATION WITH STI571 FOR THE TREATMENT OF LEUKAEMIA 失效
标题翻译：使用C-SRC抑制剂或与STI571组合用于治疗白血病
公开(公告)号：US20090227608A1
公开(公告)日：2009-09-10
申请号：US12466186
申请日：2009-05-14
申请人： Nicholas J. Donato , Doriano Fabbro , Paul William Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
发明人： Nicholas J. Donato , Doriano Fabbro , Paul William Manley , Jurgen Mestan , Markus Warmuth , Michael Hallek , Moshe Talpaz , Ji Wu
IPC分类号： A61K31/519 , A61P35/00
CPC分类号： A61K35/02 , A61K31/506 , A61K31/519
摘要： The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine.
摘要翻译：本发明涉及一种组合，其包含（a）至少一种降低c-Src活性的化合物和（b）N- {5- [4-（4-甲基 - 哌嗪基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺或其单甲磺酸盐; 包含所述组合的药物组合物; 以及治疗具有白血病，特别是慢性骨髓性白血病的温血动物的方法，包括向所述动物施用至少一种抑制Src激酶家族成员，Btk激酶家族，Tec激酶家族的活性的化合物或 Raf激酶抑制剂，特别是抑制c-Src蛋白酪氨酸激酶活性或同时抑制c-Src蛋白酪氨酸激酶活性和Bcr-Abl酪氨酸激酶活性，单独或与Bcr-Abl抑制剂组合，特别是N - {5- [4-（4-甲基 - 哌嗪子基 - 甲基） - 苯甲酰氨基] -2-甲基苯基} -4-（3-吡啶基）-2-嘧啶胺。

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