公开(公告)号：US20080280889A1

公开(公告)日：2008-11-13

申请号：US11547367

申请日：2005-04-05

Applicant: Mark T. Bilodeau ,  Peter C. Chua ,  Nicholas D.P. Cosford ,  Jacob M. Hoffman ,  Johnny Yasuo Nagasawa

Inventor： Mark T. Bilodeau ,  Peter C. Chua ,  Nicholas D.P. Cosford ,  Jacob M. Hoffman ,  Johnny Yasuo Nagasawa

IPC: A61K31/501 ,  A61P35/00 ,  C07D401/14 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/541 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D417/14 ,  A61K31/501 ,  A61K31/506 ,  C07D401/14

Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration (if the compounds of the invention.

Abstract translation: 本发明涉及含有取代的哒嗪和嘧啶部分的化合物，其抑制Akt（丝氨酸/苏氨酸蛋白激酶）的活性。 本发明进一步涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括给药（如果本发明的化合物。

公开(公告)号：US06958340B2

公开(公告)日：2005-10-25

申请号：US10485170

申请日：2002-07-26

Applicant: Mark T. Bilodeau ,  Peter J. Manley ,  Adrienne Balitza ,  George D. Hartman ,  Leonard Rodman

Inventor： Mark T. Bilodeau ,  Peter J. Manley ,  Adrienne Balitza ,  George D. Hartman ,  Leonard Rodman

IPC: A61P35/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/506

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

公开(公告)号：US06794393B1

公开(公告)日：2004-09-21

申请号：US10110872

申请日：2002-04-18

Applicant: Mark E. Fraley ,  Kenneth L. Arrington ,  Mark T. Bilodeau ,  George D. Hartman ,  William F. Hoffman ,  Yuntae Kim ,  Randall W. Hungate

Inventor： Mark E. Fraley ,  Kenneth L. Arrington ,  Mark T. Bilodeau ,  George D. Hartman ,  William F. Hoffman ,  Yuntae Kim ,  Randall W. Hungate

IPC: C07D40114

CPC classification number: C07D401/14 ,  A61K31/495 ,  A61K45/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K2300/00

Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

公开(公告)号：US06306874B1

公开(公告)日：2001-10-23

申请号：US09690598

申请日：2000-10-17

Applicant: Mark E. Fraley ,  Kenneth L. Arrington ,  Mark T. Bilodeau ,  George D. Hartman ,  William F. Hoffman ,  Yuntae Kim ,  Randall W. Hungate

Inventor： Mark E. Fraley ,  Kenneth L. Arrington ,  Mark T. Bilodeau ,  George D. Hartman ,  William F. Hoffman ,  Yuntae Kim ,  Randall W. Hungate

IPC: A01N4342

CPC classification number: C07D413/14 ,  A61K31/495 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  A61K2300/00

Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

公开(公告)号：US6090789A

公开(公告)日：2000-07-18

申请号：US977215

申请日：1997-11-24

Applicant: Samuel J. Danishefsky ,  Mark T. Bilodeau ,  Shuang Hua Hu ,  Tae Kyo Park ,  John T. Randolph ,  In Jong Kim ,  Philip O. Livingston

Inventor： Samuel J. Danishefsky ,  Mark T. Bilodeau ,  Shuang Hua Hu ,  Tae Kyo Park ,  John T. Randolph ,  In Jong Kim ,  Philip O. Livingston

IPC: C07H11/00 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7042 ,  A61K31/7048 ,  A61K38/00 ,  A61K39/00 ,  A61K39/39 ,  A61P35/00 ,  A61P37/04 ,  C07H3/06 ,  C07H15/10 ,  C07H15/18 ,  C07H17/02 ,  C07H17/04 ,  C07K1/04 ,  C07K9/00 ,  C07K16/30 ,  C07K16/44 ,  C07H5/06 ,  C07H15/04 ,  G01N33/00

CPC classification number: C07H15/10 ,  A61K39/0011 ,  C07H15/18 ,  C07H17/02 ,  C07H3/06 ,  C07K1/04 ,  C07K16/3015 ,  C07K16/44 ,  C07K9/005 ,  A61K38/00

Abstract: The present invention provides a process for synthesizing a compound having the structure: ##STR1## wherein R is H, as well as related oligosaccharides useful as a vaccine for inducing antibodies to human breast cancer cells in an adjuvant therapy therefor.

Abstract translation: 本发明提供一种合成具有以下结构的化合物的方法：其中R为H，以及可用作用于在其辅助治疗中诱导人乳腺癌细胞抗体的疫苗的相关寡糖。

公开(公告)号：US5859041A

公开(公告)日：1999-01-12

申请号：US871382

申请日：1997-06-09

Applicant: Nigel J. Liverton ,  David A. Claremon ,  John W. Butcher ,  Mark T. Bilodeau

Inventor： Nigel J. Liverton ,  David A. Claremon ,  John W. Butcher ,  Mark T. Bilodeau

IPC: A61K31/506 ,  A61P1/00 ,  A61P7/00 ,  A61P9/00 ,  A61P9/10 ,  A61P19/02 ,  A61P19/08 ,  A61P29/00 ,  A61P31/00 ,  A61P37/06 ,  A61P43/00 ,  C07D233/54 ,  C07D233/56 ,  C07D401/14 ,  A61K31/415 ,  C07D401/02

CPC classification number: C07D401/14 ,  Y10S514/825

Abstract: Compounds represented by formula I: ##STR1## are disclosed. .sup.AR represents an aromatic group containing 6-10 atoms; and ##STR2## represents a 4 to 10 membered non-aromatic heterocycle containing at least one N atom, and optionally containing 1-2 additional N atoms and 0-1 O or S atom. A pharmaceutical composition is also included. Methods of treating cancer and cytokine mediated diseases are also included.

Abstract translation: 由式I表示的化合物：其中公开了。 AR表示含有6-10个原子的芳族基团; 并且表示含有至少一个N原子，任选地含有1-2个另外的N原子和0-1O或S原子的4至10元非芳族杂环。 还包括药物组合物。 还包括治疗癌症和细胞因子介导的疾病的方法。

公开(公告)号：US09233977B2

公开(公告)日：2016-01-12

申请号：US13880992

申请日：2011-10-25

Applicant: John A. McCauley ,  Hemaka A. Rajapakse ,  Thomas J. Greshock ,  John Sanders ,  Boyoung Kim ,  Vanessa L. Rada ,  Jonathan T. Kern ,  Heather H. Stevenson ,  Mark T. Bilodeau

Inventor： John A. McCauley ,  Hemaka A. Rajapakse ,  Thomas J. Greshock ,  John Sanders ,  Boyoung Kim ,  Vanessa L. Rada ,  Jonathan T. Kern ,  Heather H. Stevenson ,  Mark T. Bilodeau

IPC: C07D495/04 ,  C07D495/10 ,  A61K31/438 ,  A61K31/4365

CPC classification number: C07D495/04 ,  C07D495/10

Abstract: Disclosed are compounds of Formula (I): and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO2—, —O— or NRac—, wherein Rac is H, or C1-20 alkyl and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.

Abstract translation: 公开了式（I）的化合物及其药学上可接受的盐，其中“A”为S-; -SO - ， - SO 2 - ， - O-或NRac-，其中Rac是H，或C 1-20烷基和R 1至R 5在本文中定义。 还公开了包含式I化合物的药物制剂以及通过抑制LRRK2激酶活性（例如帕金森病）治疗，治疗或改善易于治疗，治疗或改善的疾病的方法。

公开(公告)号：US20120196894A1

公开(公告)日：2012-08-02

申请号：US13499844

申请日：2010-09-28

Applicant: Mark T. Bilodeau ,  Melissa Egbertson ,  Ahren Green ,  John C. Hartnett ,  Yiwei Li

Inventor： Mark T. Bilodeau ,  Melissa Egbertson ,  Ahren Green ,  John C. Hartnett ,  Yiwei Li

IPC: A61K31/136 ,  C07D215/38 ,  A61K31/47 ,  C07C255/59 ,  A61K31/4706 ,  C07D311/74 ,  A61K31/352 ,  A61P29/00 ,  C07D215/44 ,  C07C211/48 ,  A61K31/277

CPC classification number: C07C215/20 ,  A61K31/133 ,  C07C25/02 ,  C07C211/34 ,  C07C215/44 ,  C07C255/58 ,  C07C2602/10 ,  C07D215/38 ,  C07D215/44 ,  C07D311/74 ,  C07D311/76 ,  C07D405/04 ,  C07D405/06

Abstract: The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function. The present invention further relates to methods and compositions that antagonize both a function of TRPA1 and a function of one or more additional TRP channels.

Abstract translation: 本发明涉及调节至少一种TRP家族成员的组合物和方法。 具体地说，本发明涉及新型TRPA1拮抗剂及其用于治疗慢性炎性和神经性疼痛等疼痛的用途。 可以调节一种或多种TRPA1功能的化合物在许多方面是有用的，包括但不限于维持钙稳态; 维持钠稳态; 调节细胞内钙含量; 调节膜极化（膜电位）; 调节阳离子水平; 和/或治疗或预防与钙稳态相关的疾病，病症或病症，钠稳态，钙或钠血管平衡，或膜极化/超极化（包括低钠和过度兴奋性）和/或治疗或预防与疾病，病症或病症相关 与TRPA1表达或功能调节或失调。 本发明还涉及拮抗TRPA1的功能和一种或多种另外的TRP通道的功能的方法和组合物。

公开(公告)号：US07910561B2

公开(公告)日：2011-03-22

申请号：US11792121

申请日：2005-12-09

Applicant: Jeannie M. Arruda ,  Brian T. Campbell ,  Nicholas D. P. Cosford ,  Jacob M. Hoffman ,  Essa H. Hu ,  Mark E. Layton ,  Yiwei Li ,  Jun Liang ,  Kevin J. Rodzinak ,  Tony Siu ,  Brian A. Stearns ,  Lida R. Tehrani ,  Mark T. Bilodeau ,  Peter J. Manley

Inventor： Jeannie M. Arruda ,  Brian T. Campbell ,  Nicholas D. P. Cosford ,  Jacob M. Hoffman ,  Essa H. Hu ,  Mark E. Layton ,  Yiwei Li ,  Jun Liang ,  Kevin J. Rodzinak ,  Tony Siu ,  Brian A. Stearns ,  Lida R. Tehrani ,  Mark T. Bilodeau ,  Peter J. Manley

IPC: A01N43/04 ,  A01N43/58 ,  A01N43/42 ,  A61K31/541 ,  A61K31/70 ,  A61K31/50 ,  A61K31/495 ,  A61K31/52 ,  C09B25/00 ,  C07D487/00 ,  C07D491/00 ,  C07H15/00

CPC classification number: C07D471/04

Abstract: The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.

Abstract translation: 本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代萘啶的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。 与PCT公开WO2003 / 086394中报道的其它萘啶类相比，这些取代的萘啶具有意想不到的有利性质，这种意想不到的有利性质可包括增加的细胞效力/溶解度，更大的选择性，增强的药物动力学性质，缺乏目标活性等。

公开(公告)号：US20090233897A1

公开(公告)日：2009-09-17

申请号：US12083475

申请日：2006-10-17

Applicant: B. Wesley Trotter ,  Kausik K. Nanda ,  Scott Wolkenberg ,  M. Brad Nolt ,  Peter Manley ,  Nathan R. Kett ,  Mark T. Bilodeau

Inventor： B. Wesley Trotter ,  Kausik K. Nanda ,  Scott Wolkenberg ,  M. Brad Nolt ,  Peter Manley ,  Nathan R. Kett ,  Mark T. Bilodeau

IPC: A61K31/444 ,  C07D401/14 ,  C07D401/06

CPC classification number: C07D401/14 ,  C07D213/38 ,  C07D213/57 ,  C07D213/74

Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.