Author
Jacques Y. Roberge
Bio: Jacques Y. Roberge is an academic researcher from Bristol-Myers Squibb. The author has contributed to research in topics: Aryl & Purine. The author has an hindex of 17, co-authored 43 publications receiving 828 citations.
Papers
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Patent•
18 Dec 2002TL;DR: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds are discussed in this article.
Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
74 citations
Patent•
03 Aug 1998TL;DR: In this article, the authors present novel imidazoquinoxalines and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.
Abstract: Novel imidazoquinoxalines and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.
62 citations
TL;DR: EGT1442 showed favorable properties both in vitro and in vivo and could be beneficial to the management of type 2 diabetic patients and could help to promote normalization of blood glucose without hypoglycemia in the setting of type 1 diabetes.
59 citations
Patent•
11 May 2005TL;DR: In this paper, the pyridyl or phenyl ureas and analogues thereof are used as selective inhibitors of the human P2Y1 receptor, and various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2y1 receptor activity.
Abstract: The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
58 citations
Patent•
22 Aug 2008
TL;DR: In this paper, compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT are provided. And the authors also provide pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by sGLT inhibition.
Abstract: Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.
57 citations
Cited by
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TL;DR: The application ofadium-catalyzed amination reactions of aryl halides in C-N cross-coupling reactions in the synthesis of heterocycles and pharmaceuticals, in materials science, and in natural product synthesis is discussed.
Abstract: Palladium-catalyzed amination reactions of aryl halides have undergone rapid development in the last 12 years, largely driven by the implementation of new classes of ligands. Biaryl phosphanes have proven to provide especially active catalysts in this context. This Review discusses the application of these catalysts in C-N cross-coupling reactions in the synthesis of heterocycles and pharmaceuticals, in materials science, and in natural product synthesis.
1,722 citations
TL;DR: Dialkylbiaryl phosphines are a valuable class of ligand for Pd-catalyzed amination reactions and have been applied in a range of contexts and this review attempts to aid the reader in the selection of the best choice of reaction conditions and ligand.
Abstract: Dialkylbiaryl phosphines are a valuable class of ligand for Pd-catalyzed amination reactions and have been applied in a range of contexts. This perspective attempts to aid the reader in the selection of the best choice of reaction conditions and ligand of this class for the most commonly encountered and practically important substrate combinations.
1,241 citations
01 Sep 2010
TL;DR: In this paper, the selection of the best choice of reaction conditions and ligand of this class for the most commonly encountered and practically important substrate combinations for Pd-catalyzed amination reactions is discussed.
Abstract: Dialkylbiaryl phosphines are a valuable class of ligand for Pd-catalyzed amination reactions and have been applied in a range of contexts. This perspective attempts to aid the reader in the selection of the best choice of reaction conditions and ligand of this class for the most commonly encountered and practically important substrate combinations.
966 citations
TL;DR: This review concludes that Etherification without Cyclization and N-Alkylation should be considered as separate science, and the proposed treatment of Etherification with Cyclization as a separate science should be reconsidered.
Abstract: 10. Patented Literature 2616 10.1. Esterification 2616 10.2. Ether Formation 2619 10.2.1. Etherification without Cyclization 2619 10.2.2. Etherification with Cyclization 2624 10.3. N-Alkylation 2625 10.4. Other Reactions 2627 11. Summary and Outlook 2628 12. Note Added in Proof 2628 13. Abbreviations Used in This Review 2629 14. Acknowledgments 2629 15. Supporting Information Available 2630 16. References 2630
909 citations
DOI•
20 Sep 2000
TL;DR: Thiazolidinediones(TDs)是一类新型的胰岛素抵抗治疗药物动物及临床实验证实TDs通过激活核受体过氧化物酶体增
Abstract: Thiazolidinediones(TDs)是一类新型的胰岛素抵抗治疗药物。动物及临床实验证实TDs通过激活核受体过氧化物酶体增殖物激活受体-γ(PPAR-γ)显著增加胰岛素敏感性，改善胰岛β-细胞功能，降低血糖和胰岛素水平，缓解高血压及脂代谢紊乱，对2型糖尿病大血管和微血管病变亦具有保护作用。临床使用耐受性好，低血糖发生率低。但其中的Troglitazone具有明显的肝脏毒性。
688 citations