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1. 发明授权

US08759579B2 Cyclobutyl sulfones as notch sparing gamma secretase inhibitors 有权
标题翻译：环丁基砜作为缺口保护性γ分泌酶抑制剂
公开(公告)号：US08759579B2
公开(公告)日：2014-06-24
申请号：US12989131
申请日：2009-04-17
申请人： Richard W. Heidebrecht , Chaomin Li , Benito Munoz , Andrew Rosenau , Laura M. Surdi , Paul Tempest
发明人： Richard W. Heidebrecht , Chaomin Li , Benito Munoz , Andrew Rosenau , Laura M. Surdi , Paul Tempest
IPC分类号： C07C311/13 , C07C61/16 , A61K31/195 , A61K31/18
CPC分类号： C07C317/30 , C07C2601/04 , C07D309/12
摘要： The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明包括一类新的环丁基砜衍生物，它们通过推定的γ-分泌酶抑制APP的加工，同时保留Notch信号传导途径，因此可用于治疗或预防阿尔茨海默病而不发展Notch抑制介导的胃肠道问题。还包括药物组合物和使用方法。

2. 发明授权

US07981874B2 Phosphorus derivatives as histone deacetylase inhibitors 失效
标题翻译：磷衍生物作为组蛋白脱乙酰酶抑制剂
公开(公告)号：US07981874B2
公开(公告)日：2011-07-19
申请号：US12309459
申请日：2007-07-16
申请人： Joshua Close , Jonathan Grimm , Richard W. Heidebrecht, Jr. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Paul J. Tempest , Kevin J. Wilson , David J. Witter
发明人： Joshua Close , Jonathan Grimm , Richard W. Heidebrecht, Jr. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Paul J. Tempest , Kevin J. Wilson , David J. Witter
IPC分类号： A61K31/662 , A61K31/683 , A61K31/67 , A61K31/675 , A61K31/4747 , A61K31/4545 , A61K31/4436 , A61K31/415 , A61K31/427 , C07F9/28 , C07F9/53 , C07F9/40 , C07F9/32 , C07F9/6571 , C07F9/6584 , C07D333/20 , C07D277/50 , C07D231/40 , C07D221/20 , C07F9/58 , C07F9/59
CPC分类号： C07F9/655345 , C07F9/5304 , C07F9/5325 , C07F9/65031 , C07F9/65586 , C07F9/657154 , C07F9/657181 , C07F9/6584
摘要： The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the phosphorus derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the phosphorus derivatives in vivo.
摘要翻译：本发明涉及一类新型的磷衍生物。磷化合物可用于治疗癌症。磷化合物也可以抑制组蛋白脱乙酰酶，适用于选择性诱导末端分化，阻止肿瘤细胞的细胞生长和/或细胞凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如神经退行性疾病本发明进一步提供包含磷衍生物和这些药物组合物的安全给药方案的药物组合物，其易于遵循，并且其在体内导致治疗有效量的磷衍生物。

3. 发明申请

US20110130361A1 SILICON DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：硅酮衍生物作为脱乙酰壳多糖抑制剂
公开(公告)号：US20110130361A1
公开(公告)日：2011-06-02
申请号：US12672441
申请日：2008-08-05
申请人： Jonathan Grimm , Richard W. Heidebrecht, JR. , Dawn M. Mampreian , Joey L. Methot , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Kevin J. Wilson , David J. Witter
发明人： Jonathan Grimm , Richard W. Heidebrecht, JR. , Dawn M. Mampreian , Joey L. Methot , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Kevin J. Wilson , David J. Witter
IPC分类号： A61K31/695 , C07C271/28 , C07D333/22 , C07D209/32 , C07F7/02 , A61K31/24 , A61K31/381 , A61K31/4015 , A61P35/00
CPC分类号： C07F7/0812
摘要： The present invention relates to a novel class of Silicon derivatives. The Silicon compounds can be used to treat cancer. The Silicon compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the Silicon derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the Silicon derivatives in vivo.
摘要翻译：本发明涉及一类新型的硅衍生物。硅化合物可用于治疗癌症。硅化合物还可以抑制组蛋白脱乙酰酶，并且适用于选择性诱导末端分化，并阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统疾病（CNS），例如神经退行性疾病本发明还提供包含硅衍生物和这些药物组合物的安全给药方案的药物组合物，其易于遵循，并且其在体内导致治疗有效量的硅衍生物。

4. 发明申请

US20110039925A1 CYCLOBUTYL SULFONES AS NOTCH SPARING GAMMA SECRETASE INHIBITORS 有权
公开(公告)号：US20110039925A1
公开(公告)日：2011-02-17
申请号：US12989131
申请日：2009-04-17
申请人： Richard W. Heidebrecht , Chaomin Li , Benito Munoz , Andrew Rosenau , Laura M. Surdi , Paul Tempest
发明人： Richard W. Heidebrecht , Chaomin Li , Benito Munoz , Andrew Rosenau , Laura M. Surdi , Paul Tempest
IPC分类号： C07C311/13 , A61K31/195 , A61K31/18 , C07C61/16 , A61K31/351 , C07D309/10 , A61P25/28
CPC分类号： C07C317/30 , C07C2601/04 , C07D309/12
摘要： The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明包括一类新的环丁基砜衍生物，它们通过推定的γ-分泌酶抑制APP的加工，同时保留Notch信号传导途径，因此可用于治疗或预防阿尔茨海默病而不发展Notch抑制介导的胃肠道问题。还包括药物组合物和使用方法。

5. 发明申请

US20090270351A1 PHOSPHORUS DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 失效
标题翻译：作为组蛋白脱乙酰酶抑制剂的磷酸衍生物
公开(公告)号：US20090270351A1
公开(公告)日：2009-10-29
申请号：US12309459
申请日：2007-07-16
申请人： Joshua Close , Jonathan Grimm , Richard W. Heidebrecht, JR. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Paul J. Tempest , Kevin J. Wilson , David J. Witter
发明人： Joshua Close , Jonathan Grimm , Richard W. Heidebrecht, JR. , Solomon Kattar , Thomas A. Miller , Karin M. Otte , Scott Peterson , Phieng Siliphaivanh , Paul J. Tempest , Kevin J. Wilson , David J. Witter
IPC分类号： A61K31/675 , A61K31/67 , C07F9/28 , C07D333/04
CPC分类号： C07F9/655345 , C07F9/5304 , C07F9/5325 , C07F9/65031 , C07F9/65586 , C07F9/657154 , C07F9/657181 , C07F9/6584
摘要： The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the phosphorus derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the phosphorus derivatives in vivo.
摘要翻译：本发明涉及一类新型的磷衍生物。磷化合物可用于治疗癌症。磷化合物也可以抑制组蛋白脱乙酰酶，适用于选择性诱导末端分化，阻止肿瘤细胞的细胞生长和/或细胞凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统疾病（CNS），例如神经退行性疾病本发明进一步提供包含磷衍生物和这些药物组合物的安全给药方案的药物组合物，其易于遵循，并且其在体内导致治疗有效量的磷衍生物。

6. 发明申请

US20090209566A1 Spirocyclic Compounds 有权
标题翻译：螺环化合物
公开(公告)号：US20090209566A1
公开(公告)日：2009-08-20
申请号：US12085396
申请日：2006-11-17
申请人： Scott C. Berk , Joshua Close , Christopher Hamblett , Richard W. Heidebrecht , Solomon D. Kattar , Laura T. Kliman , Dawn M. Mampreian , Joey L. Methot , Thomas Miller , David L. Sloman , Matthew G. Stanton , Paul Tempest , Anna A. Zabierek
发明人： Scott C. Berk , Joshua Close , Christopher Hamblett , Richard W. Heidebrecht , Solomon D. Kattar , Laura T. Kliman , Dawn M. Mampreian , Joey L. Methot , Thomas Miller , David L. Sloman , Matthew G. Stanton , Paul Tempest , Anna A. Zabierek
IPC分类号： A61K31/438 , C07D471/10 , C07D491/107 , C07D498/10 , C07D487/10 , A61K31/4439 , A61K31/506 , A61P35/00
CPC分类号： C07D471/10 , C07D487/10 , C07D491/10 , C07D491/107 , C07D498/10
摘要： The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR12, NR1a, C(O) and O; E is selected from a bond, CR12, NR1a, C(O) and O; wherein at least one of A, B, D or E is CR12; and provided that when A is O, then E is not O; G is CR12; R is selected from NH2 and OH; These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing termin differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.
摘要翻译：本发明涉及由下列结构式表示的新一类取代的螺环化合物：其中A，B和D独立地选自CR12，NR1a，C（O）和O; E选自键，CR12，NR1a，C（O）和O; 其中A，B，D或E中的至少一个为CR 12; 并且条件是当A为O时，则E不为O; G是CR12; R选自NH 2和OH; 这些化合物可以抑制组蛋白脱乙酰酶，适用于选择性诱导终末分化，阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统疾病（CNS），例如神经退行性疾病本发明进一步提供包含本发明化合物和易于遵循的这些药物组合物的安全给药方案的药物组合物，并且其在体内导致治疗有效量的这些化合物。

7. 发明授权

US08871796B2 Diaryl ether derivatives as notch sparing gamma secretase inhibitors 有权
标题翻译：二芳基醚衍生物作为缺口保留的γ分泌酶抑制剂
公开(公告)号：US08871796B2
公开(公告)日：2014-10-28
申请号：US13501628
申请日：2010-10-05
申请人： William Colby Brown , Jason Brubaker , Christian Fischer , Richard W. Heidebrecht , John T. Hendrix , Elizabeth H. Kelley , Rachel N. MacCoss , Joey L. Methot , Thomas Miller , Karin M. Otte , Phieng Siliphaivanh , Thomas Reger , Peter D. Williams , Catherine M. Wiscount
发明人： William Colby Brown , Jason Brubaker , Christian Fischer , Richard W. Heidebrecht , John T. Hendrix , Elizabeth H. Kelley , Rachel N. MacCoss , Joey L. Methot , Thomas Miller , Karin M. Otte , Phieng Siliphaivanh , Thomas Reger , Peter D. Williams , Catherine M. Wiscount
IPC分类号： A61K31/415 , C07D401/00 , C07D421/00 , C07D405/10 , C07D413/12 , C07D409/12 , C07D417/12 , C07D231/22 , C07D413/14 , C07D491/113 , C07D405/12 , C07D401/04 , C07D405/14 , C07D401/12
CPC分类号： C07D231/22 , C07D231/20 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D491/113
摘要： The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明包括一类新的二芳基醚衍生物，其抑制通过推定的γ-分泌酶处理APP，同时保留Notch信号通路，因此可用于治疗或预防阿尔茨海默病而不发展Notch抑制介导的胃肠道问题。还包括药物组合物和使用方法。

8. 发明授权

US08461189B2 Pyridyl derivatives as histone deacetylase inhibitors 有权
标题翻译：吡啶衍生物作为组蛋白脱乙酰酶抑制剂
公开(公告)号：US08461189B2
公开(公告)日：2013-06-11
申请号：US12666415
申请日：2008-06-24
申请人： Richard W. Heidebrecht, Jr. , Thomas A. Miller , Matthew G. Stanton , David J. Witter
发明人： Richard W. Heidebrecht, Jr. , Thomas A. Miller , Matthew G. Stanton , David J. Witter
IPC分类号： A01N43/40 , A01N47/10 , A61K31/44 , C07D213/55
CPC分类号： C07D213/75 , C07D409/04 , C07D409/14
摘要： The present invention relates to a novel class of pyridyl and pyrimidinyl derivatives. The pyridyl and pyrimidinyl compounds can be used to treat cancer. The pyridyl and pyrimidinyl compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the pyridyl and pyrimidinyl derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the pyridyl and pyrimidinyl derivatives in vivo.
摘要翻译：本发明涉及一类新的吡啶基和嘧啶基衍生物。吡啶基和嘧啶基化合物可用于治疗癌症。吡啶基和嘧啶基化合物也可以抑制组蛋白脱乙酰酶，适用于选择性诱导终末分化，阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如神经退行性疾病本发明进一步提供包含吡啶基和嘧啶基衍生物的药物组合物以及易于遵循的这些药物组合物的安全给药方案，并且其在体内导致治疗有效量的吡啶基和嘧啶基衍生物。

9. 发明授权

US07834026B2 Spirocyclic compounds 有权
标题翻译：螺环化合物
公开(公告)号：US07834026B2
公开(公告)日：2010-11-16
申请号：US12085396
申请日：2006-11-17
申请人： Scott C. Berk , Joshua Close , Christopher Hamblett , Richard W. Heidebrecht , Solomon D. Kattar , Laura T. Kliman , Dawn M. Mampreian , Joey L. Methot , Thomas Miller , David L. Sloman , Matthew G. Stanton , Paul Tempest , Anna A. Zabierek
发明人： Scott C. Berk , Joshua Close , Christopher Hamblett , Richard W. Heidebrecht , Solomon D. Kattar , Laura T. Kliman , Dawn M. Mampreian , Joey L. Methot , Thomas Miller , David L. Sloman , Matthew G. Stanton , Paul Tempest , Anna A. Zabierek
IPC分类号： A01N43/42 , A01N43/12 , A01N43/26 , A61K31/44 , A61K31/34 , A61K31/335 , C07D237/00 , C07D239/00 , C07D241/00 , C07D491/10 , C07D491/20 , C07D495/10 , C07D495/20 , C07D497/10 , C07D497/20 , C07D311/96 , C07D313/06 , C07D313/20 , C07D315/00
CPC分类号： C07D471/10 , C07D487/10 , C07D491/10 , C07D491/107 , C07D498/10
摘要： The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR12, NR1a, C(O) and O; E is selected from a bond, CR12, NR1a, C(O) and O; wherein at least one of A, B, D or E is CR12; and provided that when A is O, then E is not O; G is CR12; R is selected from NH2 and OH; These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing termin differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.
摘要翻译：本发明涉及由下列结构式表示的新一类取代的螺环化合物：其中A，B和D独立地选自CR12，NR1a，C（O）和O; E选自键，CR12，NR1a，C（O）和O; 其中A，B，D或E中的至少一个为CR 12; 并且条件是当A为O时，则E不为O; G是CR12; R选自NH 2和OH; 这些化合物可以抑制组蛋白脱乙酰酶，适用于选择性诱导终末分化，阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如神经退行性疾病本发明进一步提供包含本发明化合物和易于遵循的这些药物组合物的安全给药方案的药物组合物，并且其在体内产生治疗有效量的这些化合物。

10. 发明申请

US20090156825A1 Fluorescent compounds that bind to histone deacetylase 审中-公开
标题翻译：结合组蛋白脱乙酰酶的荧光化合物
公开(公告)号：US20090156825A1
公开(公告)日：2009-06-18
申请号：US12313799
申请日：2008-11-25
申请人： Richard W. Heidebrecht, JR. , Astrid M. Kral , Thomas A. Miller
发明人： Richard W. Heidebrecht, JR. , Astrid M. Kral , Thomas A. Miller
IPC分类号： C07D213/78
CPC分类号： C07D213/75 , C07D311/90
摘要： The present invention relates to a novel class of fluorescent compounds that bind to histone deacetylases. The fluorescent compounds can be used to determine binding association and dissociation rates of histone deacetylase inhibitors via fluorescence polarization.
摘要翻译：本发明涉及结合组蛋白脱乙酰酶的新型荧光化合物。荧光化合物可用于通过荧光偏振来测定组蛋白脱乙酰酶抑制剂的结合关联和解离速率。

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