Ping Chen - San Diego CA Mark Anderson - San Diego CA Ya-Li Deng - San Diego CA Smita Gaur - San Diego CA Chen Chen Kan - Arcadia CA Chun Luo - San Diego CA Karen Lundgren - San Diego CA Stephen Margosiak - Escondido CA Binh Nguyen - San Diego CA Patrick OConnor - San Diego CA James Register - San Diego CA Anna Tempczyk Russell - San Diego CA Jay Sarup - San Diego CA
The present invention relates to the identification, isolation and purification of the catalytic domain of the human effector checkpoint protein kinase (hChk1). A 1. 7 crystal structure of the hChk1 kinase domain in the active conformation is reported herein. The kinase domain of hChk1 and its associated crystal structure is described for use in the discovery, identification and characterization of inhibitors of hChk1. This structure provides a three-dimensional description of the binding site of the hChk1 for structure-based design of small molecule inhibitors thereof as therapeutic agents. Inhibitors of hChk1 find utility in the treatment of hyperproliferative disorders such as HIV and cancer.
Cyanoamide Compounds Useful As Malonyl-Coa Decarboxylase Inhibitors
Mark D. Kafka - San Diego CA, US Mark E. Wilson - Ramona CA, US Anna Russell - Ramona CA, US Gary D. Lopaschuk - Edmonton, CA Jason R. Dyck - Sherwood Park, CA
Assignee:
Chugai Seiyaku Kabushiki Kaisha - Tokyo
International Classification:
A61K 31/44 A61K 31/425 A61K 31/415
US Classification:
514301, 514302, 514367, 514387
Abstract:
The present invention provides methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.
Cyanoamide Compounds Useful As Malonyl-Coa Decarboxylase Inhibitors
Mark D. Kafka - San Diego CA, US Mark E. Wilson - Ramona CA, US Anna Russell - Ramona CA, US Gary D. Lopaschuk - Edmonton, CA Jason R. Dyck - Sherwood Park, CA
Assignee:
Chugai Sciyaku Kabushiki Kaisha - Tokyo
International Classification:
A61K 31/44 A61K 31/41 A61K 31/425 A61K 31/42
US Classification:
514301, 514302, 514361, 514367, 514376
Abstract:
The present invention provides previous methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.
Catalytic Domain Of The Human Effector Cell Cycle Checkpoint Protein Kinase Chk1 Materials And Methods For Identification Of Inhibitors Thereof
Ping Chen - San Diego CA, US Mark Anderson - San Diego CA, US Ya-Li Deng - San Diego CA, US Smita Gaur - San Diego CA, US Chen Kan - Arcadia CA, US Chun Luo - San Diego CA, US Karen Lundgren - San Diego CA, US Stephen Margosiak - Escondido CA, US Binh Nguyen - San Diego CA, US Patrick O'Connor - San Diego CA, US James Reqister - San Diego CA, US Anna Russell - San Diego CA, US Jay Sarup - San Diego CA, US
The present invention relates to the identification, isolation and purification of the catalytic domain of the human effector checkpoint protein kinase (hChk1). A 1.7 crystal structure of the hChk1 kinase domain in the active conformation is reported herein. The kinase domain of hChk1 and its associated crystal structure is described for use in the discovery, identification and characterization of inhibitors of hChk1. This structure provides a three-dimensional description of the binding site of the hChk1 for structure-based design of small molecule inhibitors thereof as therapeutic agents. Inhibitors of hChk1 find utility in the treatment of hyperproliferative disorders such as HIV and cancer.
Bisphenyl Compounds Useful As Vitamin D3 Receptor Agonists
David Wallace - San Diego CA, US Thomas Arrhenius - Del Mar CA, US Anna Russell - San Diego CA, US Dingguo Liu - San Marcos CA, US Amy Xing - San Diego CA, US Sovouthy Tith - Phoenix AZ, US Zheng Hou - San Diego CA, US Tadakatsu Takahashi - Shizuoka, JP Yoshiyuki Ono - Shizuoka, JP Hirotaka Kashiwagi - Shizuoka, JP Kazuki Shimizu - Shizuoka, JP Hitoshi Ikura - Kanagawa, JP
The present invention discloses bisphenyl compounds of the formula: wherein R1, R2, R3, R4, R5, R6, X, Y, W are defined herein after. These compounds are useful as pharmaceuticals.
Anna Russell, 19, and Enrique Soto, 25, were charged Wednesday with aggravated assault, endangering the welfare of a child, reckless endangerment and other offenses for the incident Aug. 1 in their apartment in the 300 block of Dorothy Street.
City Secretary Anna Russell initially counted enough signatures to put the repeal referendum on the ballot, but Feldman looked through all of the petition pages to see if the signatures met city charter requirements. He looked at whether the signature gatherers were Houston residents and whether the
When she went into labor early, Anna Russell was given shots to delay delivery, but they didnt work. Lane stayed in the neonatal intensive care unit for 51 days before his parents were able to take him home.