公开(公告)号：US08158825B2

公开(公告)日：2012-04-17

申请号：US11922740

申请日：2006-06-21

Applicant: Jonathan Grimm ,  Paul Harrington ,  Richard Heidebrecht, Jr. ,  Thomas Miller ,  Karin Otte ,  Phieng Siliphaivanh ,  David Sloman ,  Matthew Stanton ,  Kevin Wilson ,  David Witter ,  Solomon Kattar ,  Paul Tempest

Inventor： Jonathan Grimm ,  Paul Harrington ,  Richard Heidebrecht, Jr. ,  Thomas Miller ,  Karin Otte ,  Phieng Siliphaivanh ,  David Sloman ,  Matthew Stanton ,  Kevin Wilson ,  David Witter ,  Solomon Kattar ,  Paul Tempest

IPC: C07C233/02 ,  C07C255/60 ,  C07C311/46 ,  C07C311/08 ,  C07C235/84 ,  A61K31/519 ,  A61K31/44 ,  C07D265/30 ,  C07D495/04 ,  C07D215/06 ,  C07D211/06 ,  C07D213/82

CPC classification number: C07C235/78 ,  C07C233/75 ,  C07C233/80 ,  C07C235/42 ,  C07C235/56 ,  C07C235/74 ,  C07C235/84 ,  C07C255/60 ,  C07C311/08 ,  C07C311/16 ,  C07C311/46 ,  C07C2602/08 ,  C07D207/06 ,  C07D207/327 ,  C07D209/14 ,  C07D209/20 ,  C07D211/06 ,  C07D213/40 ,  C07D213/56 ,  C07D213/82 ,  C07D215/06 ,  C07D215/12 ,  C07D215/40 ,  C07D231/40 ,  C07D249/08 ,  C07D261/14 ,  C07D265/30 ,  C07D277/28 ,  C07D277/46 ,  C07D277/56 ,  C07D295/135 ,  C07D295/155 ,  C07D295/185 ,  C07D307/68 ,  C07D319/16 ,  C07D319/18 ,  C07D333/20 ,  C07D333/38 ,  C07D333/70 ,  C07D413/14 ,  C07D495/04

Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate 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 modified malonate derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the modified malonate derivatives in vivo.

Abstract translation: 本发明涉及一类新型改性丙二酸衍生物。 修饰的丙二酸酯化合物可用于治疗癌症。 修饰的丙二酸酯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（CNS）的疾病，例如 神经退行性疾病 本发明还提供包含改性丙二酸酯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修饰的丙二酸酯衍生物。

公开(公告)号：US20100160327A1

公开(公告)日：2010-06-24

申请号：US11922740

申请日：2006-06-21

Applicant: Jonathan Grimm ,  Paul Harrington ,  Richard Heidebrecht, JR. ,  Thomas Miller ,  Karin Otte ,  Phieng Siliphaivanh ,  David Sloman ,  Matthew Stanton ,  Kevin Wilson ,  David Witter ,  Solomon Kattar ,  Paul Tempest

Inventor： Jonathan Grimm ,  Paul Harrington ,  Richard Heidebrecht, JR. ,  Thomas Miller ,  Karin Otte ,  Phieng Siliphaivanh ,  David Sloman ,  Matthew Stanton ,  Kevin Wilson ,  David Witter ,  Solomon Kattar ,  Paul Tempest

IPC: A61K31/5375 ,  A61K31/519 ,  A61K31/47 ,  A61K31/4453 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/426 ,  A61K31/42 ,  A61K31/4196 ,  A61K31/404 ,  A61K31/402 ,  A61K31/381 ,  A61K31/357 ,  A61K31/34 ,  A61K31/277 ,  A61K31/18 ,  A61K31/167 ,  C07D265/30 ,  C07D495/04 ,  C07D215/06 ,  C07D211/06 ,  C07D213/82 ,  C07D213/56 ,  C07D277/46 ,  C07D277/56 ,  C07D261/14 ,  C07D249/08 ,  C07D209/20 ,  C07D207/327 ,  C07D333/70 ,  C07D319/16 ,  C07D307/68 ,  C07C255/60 ,  C07C311/46 ,  C07C311/08 ,  C07C235/84 ,  A61P35/00

CPC classification number: C07C235/78 ,  C07C233/75 ,  C07C233/80 ,  C07C235/42 ,  C07C235/56 ,  C07C235/74 ,  C07C235/84 ,  C07C255/60 ,  C07C311/08 ,  C07C311/16 ,  C07C311/46 ,  C07C2602/08 ,  C07D207/06 ,  C07D207/327 ,  C07D209/14 ,  C07D209/20 ,  C07D211/06 ,  C07D213/40 ,  C07D213/56 ,  C07D213/82 ,  C07D215/06 ,  C07D215/12 ,  C07D215/40 ,  C07D231/40 ,  C07D249/08 ,  C07D261/14 ,  C07D265/30 ,  C07D277/28 ,  C07D277/46 ,  C07D277/56 ,  C07D295/135 ,  C07D295/155 ,  C07D295/185 ,  C07D307/68 ,  C07D319/16 ,  C07D319/18 ,  C07D333/20 ,  C07D333/38 ,  C07D333/70 ,  C07D413/14 ,  C07D495/04

Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate 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 modified malonate derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the modified malonate derivatives in vivo.

Abstract translation: 本发明涉及一类新型改性丙二酸衍生物。 修饰的丙二酸酯化合物可用于治疗癌症。 修饰的丙二酸酯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（CNS）的疾病，例如 神经退行性疾病 本发明还提供包含改性丙二酸酯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修饰的丙二酸酯衍生物。

公开(公告)号：US20100048555A1

公开(公告)日：2010-02-25

申请号：US12374535

申请日：2007-07-20

Applicant: Ian Churcher ,  Victoria Alexandra Doughty ,  Peter Hunt ,  Matthew Stanton

Inventor： Ian Churcher ,  Victoria Alexandra Doughty ,  Peter Hunt ,  Matthew Stanton

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/429 ,  C07D413/14 ,  C07D417/14 ,  C07D513/04 ,  A61P25/28

CPC classification number: C07D513/04

Abstract: Compounds of formula (I): are inhibitors of MARK, and hence useful for treatment of disorders involving 10 hyperphosphorylation of tau.

Abstract translation: 式（I）化合物：是MARK的抑制剂，因此可用于治疗涉及10个tau蛋白过度磷酸化的病症。

公开(公告)号：US20080015233A1

公开(公告)日：2008-01-17

申请号：US11547994

申请日：2005-04-20

Applicant: James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Joseph Vacca ,  Shawn Stachel ,  Craig Coburn ,  Matthew Stanton

Inventor： James Barrow ,  Georgia McGaughey ,  Philippe Nantermet ,  Hemaka Rajapakse ,  Harold Selnick ,  Shaun Stauffer ,  Joseph Vacca ,  Shawn Stachel ,  Craig Coburn ,  Matthew Stanton

IPC: A61K31/4439 ,  A61P25/28 ,  C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

CPC classification number: C07D413/04 ,  C07D401/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention is directed to 2,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract translation: 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的2,4,6-取代的吡啶衍生物化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

公开(公告)号：US20070142634A1

公开(公告)日：2007-06-21

申请号：US10582856

申请日：2004-12-15

Applicant: James Barrow ,  Craig Coburn ,  Philippe Nantermet ,  Harold Selnick ,  Shawn Stachel ,  Matthew Stanton ,  Shaun Stauffer ,  Linghang Zhuang ,  Jennifer Davis

Inventor： James Barrow ,  Craig Coburn ,  Philippe Nantermet ,  Harold Selnick ,  Shawn Stachel ,  Matthew Stanton ,  Shaun Stauffer ,  Linghang Zhuang ,  Jennifer Davis

IPC: A61K31/5377 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02 ,  C07D213/72

CPC classification number: C07D213/81 ,  C07D213/75 ,  C07D257/04 ,  C07D401/04 ,  C07D409/12 ,  C07D413/12

Abstract: The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract translation: 本发明涉及苯酰胺和吡啶酰胺衍生物化合物，其是β-分泌酶的抑制剂，可用于治疗其中涉及β-分泌酶的疾病，例如阿尔茨海默氏病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。

公开(公告)号：US20070117824A1

公开(公告)日：2007-05-24

申请号：US11600426

申请日：2006-11-16

Applicant: Scott Berk ,  Joshua Close ,  Christopher Hamblett ,  Richard Heidebrecht ,  Solomon Kattar ,  Laura Kliman ,  Dawn Mampreian ,  Joey Methot ,  Thomas Miller ,  David Sloman ,  Matthew Stanton ,  Paul Tempest ,  Anna Zabierek

Inventor： Scott Berk ,  Joshua Close ,  Christopher Hamblett ,  Richard Heidebrecht ,  Solomon Kattar ,  Laura Kliman ,  Dawn Mampreian ,  Joey Methot ,  Thomas Miller ,  David Sloman ,  Matthew Stanton ,  Paul Tempest ,  Anna Zabierek

IPC: A61K31/4747 ,  C07D471/10

CPC classification number: C07D471/10 ,  C07D487/10 ,  C07D491/10 ,  C07D491/107 ,  C07D498/10

Abstract: The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can 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 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.

Abstract translation: 本发明涉及一类新的取代的螺环化合物。 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。

公开(公告)号：US20100240647A1

公开(公告)日：2010-09-23

申请号：US12223157

申请日：2007-01-23

Applicant: Ian Churcher ,  Peter Hunt ,  Matthew Stanton

Inventor： Ian Churcher ,  Peter Hunt ,  Matthew Stanton

IPC: A61K31/519 ,  A61P25/00 ,  A61K31/5377 ,  C07D487/04

CPC classification number: C07D487/04 ,  A61K31/519

Abstract: Compounds of formula (I) inhibit microtubule affinity regulating kinase (MARK), and hence are suitable for treating diseases associated with abnormal phosphorylation of tau.

Abstract translation: 式（I）化合物抑制微管亲和调节激酶（MARK），因此适用于治疗与tau异常磷酸化有关的疾病。

公开(公告)号：US07772238B2

公开(公告)日：2010-08-10

申请号：US11918912

申请日：2006-04-14

Applicant: Jed Lee Hubbs ,  Sam Kattar ,  Joey Methot ,  Thomas Miller ,  Phieng Siliphaivanh ,  Matthew Stanton ,  Kevin Wilson ,  David J. Witter

Inventor： Jed Lee Hubbs ,  Sam Kattar ,  Joey Methot ,  Thomas Miller ,  Phieng Siliphaivanh ,  Matthew Stanton ,  Kevin Wilson ,  David J. Witter

IPC: A61K31/496 ,  A61K31/381 ,  C07D405/04 ,  C07D333/56

CPC classification number: C07D333/70 ,  A61K31/38 ,  A61K31/381 ,  A61K31/41

Abstract: The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid 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 are also 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 hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

Abstract translation: 本发明涉及一类新型异羟肟酸衍生物。 异羟肟酸化合物可用于治疗癌症。 异羟肟酸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，例如神经变性 疾病 本发明进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物，它们易于遵循，并且其在体内导致治疗有效量的异羟肟酸衍生物。

公开(公告)号：US20090069391A1

公开(公告)日：2009-03-12

申请号：US11918912

申请日：2006-04-14

Applicant: Jed Lee Hubbs ,  Sam Kattar ,  Joey Methot ,  Thomas Miller ,  Phieng Siliphaivanh ,  Matthew Stanton ,  Kevin Wilson ,  David J. Witter

Inventor： Jed Lee Hubbs ,  Sam Kattar ,  Joey Methot ,  Thomas Miller ,  Phieng Siliphaivanh ,  Matthew Stanton ,  Kevin Wilson ,  David J. Witter

IPC: A61K31/381 ,  C07D333/52 ,  A61K31/4245 ,  A61P25/00 ,  A61P35/00 ,  C07D271/10

CPC classification number: C07D333/70 ,  A61K31/38 ,  A61K31/381 ,  A61K31/41

Abstract: The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid 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 are also 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 hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

Abstract translation: 本发明涉及一类新型异羟肟酸衍生物。 异羟肟酸化合物可用于治疗癌症。 异羟肟酸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，例如神经变性 疾病 本发明进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物，它们易于遵循，并且其在体内导致治疗有效量的异羟肟酸衍生物。

公开(公告)号：US20090031669A1

公开(公告)日：2009-02-05

申请号：US11888539

申请日：2007-07-31

Applicant: Matthew Stanton

Inventor： Matthew Stanton

IPC: E04B5/00

CPC classification number: B27M3/04

Abstract: A method for marketing reclaimed wood as flooring includes providing a plurality of flooring planks comprising wood reclaimed from a structure and marking at least one of the planks to indicate the information about the source of the reclaimed wood. The information includes the geographic location of the structure from which the reclaimed wood was reclaimed, information about the construction date of the structure from which the wood was reclaimed and information about the type of the reclaimed wood. The marking is achieved by engraving the plank, stamping the plank, mounting a plaque to the plank or any other means for visibly marking the information on the plank. The marking is used to display the information about the source structure when the wood planks are installed in the commercial or residential application.

Abstract translation: 将回收木材营销作为地板营销的方法包括提供多个地板板，其包括从结构回收的木材并且标记至少一个木板以指示关于回收木材的来源的信息。 信息包括回收木材的结构的地理位置，关于回收木材的结构的施工日期以及回收木材类型的信息。 标记通过雕刻板，冲压板，将板放置在板上或用于可见地标记板上的信息的任何其它方式来实现。 当木板安装在商业或住宅应用中时，该标记用于显示关于源结构的信息。