公开(公告)号：US07304063B2

公开(公告)日：2007-12-04

申请号：US10554186

申请日：2004-04-20

Applicant: Mark T. Bilodeau ,  Craig W. Lindsley ,  Zhijian Zhao

Inventor： Mark T. Bilodeau ,  Craig W. Lindsley ,  Zhijian Zhao

IPC: C07D401/10 ,  C07D403/10 ,  A61K31/53 ,  A61P35/00 ,  C07D253/06

CPC classification number: C07D417/14 ,  C07D253/065 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention is directed to compounds which contain a heterocyclic triazine moiety 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.

Abstract translation: 本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的杂环三嗪部分的化合物。 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。

公开(公告)号：US06875767B2

公开(公告)日：2005-04-05

申请号：US10174774

申请日：2002-06-19

Applicant: Mark T. Bilodeau ,  George D. Hartman

Inventor： Mark T. Bilodeau ,  George D. Hartman

IPC: A61K31/09 ,  A61K31/138 ,  A61K31/337 ,  A61K31/4439 ,  A61K31/4465 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/575 ,  A61K31/737 ,  A61K38/00 ,  A61K38/21 ,  A61K39/395 ,  A61K45/00 ,  A61P1/18 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P25/00 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61P43/00 ,  C07D417/12 ,  C07D417/14 ,  A61K31/444 ,  A11K31/495

CPC classification number: C07D417/12 ,  C07D417/14

Abstract: The present invention relates to compounds having the formula I: 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. The compounds of the present invention are useful in treating angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

Abstract translation: 本发明涉及具有式I的化合物：其抑制，调节和/或调节酪氨酸激酶信号转导，含有这些化合物的组合物及其用于治疗酪氨酸激酶依赖性疾病和病症的方法。 本发明的化合物可用于治疗哺乳动物的血管生成，癌症，肿瘤生长，动脉粥样硬化，年龄相关性黄斑变性，糖尿病性视网膜病变，炎症性疾病等。

公开(公告)号：US06586423B2

公开(公告)日：2003-07-01

申请号：US10061817

申请日：2002-02-01

Applicant: Mark T. Bilodeau ,  George D. Hartman ,  Peter J. Manley ,  Randall W. Hungate ,  Leonard Rodman

Inventor： Mark T. Bilodeau ,  George D. Hartman ,  Peter J. Manley ,  Randall W. Hungate ,  Leonard Rodman

IPC: C07D41312

CPC classification number: C07D417/12 ,  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：US06544988B1

公开(公告)日：2003-04-08

申请号：US09914985

申请日：2001-09-06

Applicant: Mark T. Bilodeau ,  Mark E. Fraley ,  Randall W. Hungate

Inventor： Mark T. Bilodeau ,  Mark E. Fraley ,  Randall W. Hungate

IPC: C07D48704

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/535 ,  A61K41/0038 ,  A61K45/06

Abstract: The present invention relates to pyrazolo-pyrimidinyl 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.

Abstract translation: 本发明涉及抑制，调节和/或调节酪氨酸激酶信号转导的吡唑并嘧啶基化合物，其含有这些化合物的组合物及其用于治疗酪氨酸激酶依赖性疾病和病症如血管生成，癌症，肿瘤的方法 生长，动脉粥样硬化，年龄相关性黄斑变性，糖尿病性视网膜病变，炎症性疾病等。

公开(公告)号：US5708163A

公开(公告)日：1998-01-13

申请号：US430355

申请日：1995-04-28

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 ,  C07H1/00 ,  C07H5/06 ,  C07H17/00 ,  C08B37/00

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: 本发明提供了一种合成具有以下结构的化合物的方法：其中R是H，以及可用作用于在其辅助治疗中诱导人乳腺癌细胞的抗体的疫苗的相关寡糖。

公开(公告)号：US20130296317A1

公开(公告)日：2013-11-07

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

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：US08067607B2

公开(公告)日：2011-11-29

申请号：US12223357

申请日：2007-01-29

Applicant: Mark T. Bilodeau ,  Jacob M. Hoffman ,  M. Brad Nolt

Inventor： Mark T. Bilodeau ,  Jacob M. Hoffman ,  M. Brad Nolt

IPC: C07D213/00

CPC classification number: C07D213/74 ,  C07D401/14 ,  C07D417/14

Abstract: The present invention relates to pyridin-3-yl pyridin-3-amine compounds and derivatives thereof having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.

Abstract translation: 本发明涉及可用作治疗心律失常的钾通道抑制剂的结构式（I）的吡啶-3-基吡啶-3-胺化合物及其衍生物等。

公开(公告)号：US20100105697A1

公开(公告)日：2010-04-29

申请号：US12530944

申请日：2008-04-03

Applicant: Mark T. Bilodeau ,  Kausik K. Nanda ,  B. Wesley Trotter

Inventor： Mark T. Bilodeau ,  Kausik K. Nanda ,  B. Wesley Trotter

IPC: A61K31/496 ,  C07D417/14 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  A61P25/22

CPC classification number: A61K31/496 ,  C07D417/12

Abstract: The present invention is directed to therapeutic agents of the formula (I) which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction. wherein; R1 is C1-6alkyl, which is unsubstituted or substituted with 1-6 fluoro, wherein R1 and the hydroxyl group on the ring are attached to the same carbon atom; or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明涉及式（I）的治疗剂，其为非典型抗精神病药，其可用于治疗与多巴胺D2和5-羟色胺5-HT2A神经传递功能障碍相关的神经和精神障碍。 其中; R1是未取代的或被1-6个氟取代的C1-6烷基，其中R1和环上的羟基连接到相同的碳原子上; 或其药学上可接受的盐。

公开(公告)号：US20100075970A1

公开(公告)日：2010-03-25

申请号：US12621124

申请日：2009-11-18

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

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

IPC: A61K31/5377 ,  C07D403/14 ,  A61K31/501 ,  C07D413/14 ,  C07D401/14 ,  A61K31/506 ,  A61P35/00

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 of 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。

公开(公告)号：US07655649B2

公开(公告)日：2010-02-02

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: C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D498/04 ,  C07D413/14 ,  C07D417/14 ,  C07D279/12 ,  C07D295/00 ,  C07D237/08 ,  C07D237/10 ,  C07D401/10 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  C07D239/24 ,  C07D239/28 ,  C07D265/16 ,  C07D487/04 ,  C07D317/12 ,  C07F5/04 ,  A61P35/00

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 of 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。