Gerard Rosse

Tricyclic Pyrimidines As Inhibitors of DYRK1A/DYRK1B As Potential Treatment for Down's Syndrome or Alzheimer's Disease.

Title: Tricyclic Pyrimidines As Inhibitors of DYRK1A/DYRK1B As Potential Treatment for Down’s Syndrome or Alzheimer’s Disease Patent/Patent Application Number: WO 2013/026806A1 Publication date: February 28, 2013 Priority Application: Priority date: August 17, 2012 Inventors: Leblond, B.; Casagrande, A.-S.; D esir e, L.; Foucourt A.; Besson, T. Assignee Company: Exonhit SA Disease Area: Alzheimer’s disease, Down’s Syndrome Biological Target: DYRK1A/DYRK1B Summary: The patent application claims tricyclic pyrimidine derivatives as inhibitors of dual-specific tyrosine-regulated kinases (DYRKs) for the treatment of Alzheimer’s disease or Down’s Syndrome.

Novel and selective inhibitors of histone deacetylase: patent highlight.

Published: October 24, 2012 Title: Novel and Selective Inhibitors of Histone Deacetylase Patent/Patent Application Number: WO 2012/117421 A1 Publication date: March 1, 2012 Priority Application: IN 2011-CH613 Priority date: March 2, 2011 Inventors: Rajagopal, S.; Kilambi, N.; Kachadia, V.; Rathinasamy, S.; Balusubramanian, G.; Mani, U.; Rajagopalan, N.; Pushparaj, J. A.; Roy, A. M.; Vishwakarma, L.S.; Narayanan, S.; Kaliyamoorthy, V.; Thanasekaran, P.; Thatavarthy Krishna, R.; Kannan, K.; Mookkan, J.; Chidambaram Venkateswaran, S.; Ahamed Ali, F. Assignee Company: Orchid Research Laboratories Ltd., India Disease Area: CNS diseases, cancer Biological Target: HDAC6 Summary: The patent application claims a series of hydroxamic acids as selective inhibitors of histone deacetylase 6 (HDAC6) for the treatment of various diseases, including Alzheimer’s disease and cancer. Important Compound Classes: Compounds general formula:

Novel Disubstituted Pyrimidines as Inhibitors of Bruton's Tyrosine Kinase.

Title: Novel Disubstituted Pyrimidines as Inhibitors of Bruton’s Tyrosine Kinase Patent/Patent Application Number: WO 2014/100748 A1 Publication date: June 26, 2014 Priority Application: US 2012 61740862 Priority date: December 21, 2012 Inventors: Tester, R.; Chaturvedi, P.; Zhu, Z.; Surapaneni, S.; Beebe, L. Assignee Company: Celegene Avilomics Research, Inc., USA Disease Area: Cancer Biological Target: Bruton’s Tyrosine Kinase (BTK) Summary: The present application discloses a series of disubstituted pyrimidines as covalent inhibitors of BTK for the potential treatment of cancer diseases. Important Compound Classes:

Pyrazolsulfonamide agonists of oxytocin receptor.

Title: Pyrazolsulfonamide Agonists of Oxytocin Receptor Patent/Patent Application Number: WO 2014/111356 A1 Publication date: July 24, 2014 Priority Application: EP 2013-151632 Priority date: January 17, 2013 Inventors: Bissantz, C.; Grundschober, C.; Nettekoven, M.; Plancher, J.-M.; Vifian, W. Assignee Company: Hoffmann-La Roche, Inc. Disease Area: CNS Biological Target: Oxytocin receptor Summary: The present application discloses a series of pyrazolsulfonamides as agonists of the oxytocin receptor. Oxytocin is a nine amino acid cyclic peptide hormone; it is a potent uterotonic agent clinically used to induce labor. Oxytocin and its receptors exist in the nucleus accumbens and the hippocampus. Agonists of the oxytocin receptor are claimed as potential treatment for a variety of CNS diseases such as autism, schizophrenia, anxiety disorders, drug addiction, and Prader-Willi syndrome. Important Compound Classes:

Phenyl carboxamide analogues as spleen tyrosine kinase (syk) inhibitors.

Phenyl Carboxamide Analogues as Spleen Tyrosine Kinase (Syk) Inhibitors Jean-Francois Brazeau and Gerard Rosse* Structure Guided Chemistry, Dart Neuroscience LLC, 7473 Lusk Boulevard, San Diego, California 92121, United States Adjunct Associate Professor, Department of Pharmacology and Physiology, College of Medicine, Drexel University, New College Building, 245 North 15th Street, Philadelphia, Pennsylvania 19102, United States

Metabolites of the pyrimidine amine preladenant as adenosine a2a receptor antagonists.

Received: November 15, 2012 Published: November 30, 2012 Title: Metabolites of the Pyrimidine Amine Preladenant as Adenosine A2a Receptor Antagonists Patent/Patent Application Number: WO 2012135084 A1 Publication date: October 4, 2012 Priority Application: US 2011-470213P Priority date: March 31, 2011 Inventors: Ting, P.; Ma, S.; Blumenkrantz, N.; Chowdbury, S.; Neustadt, B. R. Assignee Company: Merck Sharp & Dohme Corp., USA Disease Area: Central Nervous System Disorders Biological Target: Adenosine A2a Receptor Summary: The application claims a single compound,M9, an adenosine A2a receptor antagonist, which is a metabolite of 2-(furan-2-yl)7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine (Preladenant). Preladenant is currently in phase III clinical trials for the treatment of Parkinson’s disease. In addition, the invention describes a method of determining if a subject has been administered Preladenant and of identifying its metabolites after administration to rat, dog, and human. Key Structures:

HDAC Inhibitors as Targeted Treatment of Frontotemporal Lobar Degeneration.

Received: November 15, 2012 Published: November 30, 2012 Title: HDAC Inhibitors as Targeted Treatment of Frontotemporal Lobar Degeneration Patent/Patent Application Number: WO 2012135097 A1 Publication Date: October 4, 2012 Priority Application: US 2011-467989P Priority Date: March 26, 2011 Inventors: Patzke, H.; Koenig, G.; Blain, J.-F. Assignee Company: Envivo Pharmaceuticals, Inc., United States Disease Area: Frontotemporal Lobar Degeneration (FTLD) Biological Target: Histone Deacetylases (HDACs) Summary: The application claims a series of benzooxazepine hydroxamic acids as potential treatment for Frontotemporal Dementia (FTD) or FTLD. Important Compound Classes:

Aminotriazole and Aminotetrazole Inhibitors of LSD1 as Epigenetic Modulators

Aminotriazole and Aminotetrazole Inhibitors of LSD1 as Epigenetic Modulators Vijay Kumar* and Gerard Rosse* Dart Neuroscience LLC, Structure Guided Chemistry, 12278 Scripps Summit Drive, San Diego, California 92131, United States Adjunct Associate Professor, Department of Pharmacology and Physiology, College of Medicine, Drexel University, New College Building, 245 North 15th Street, Philadelphia, Pennsylvania 19102, United States

Combination of Novel Imidazopyridazine Mps-1 Kinase Inhibitors and Bcl-2 Family Protein Inhibitors

Title: Combination of Novel Imidazopyridazine Mps-1 Kinase Inhibitors and Bcl-2 Family Protein Inhibitors Patent/Patent Application Number: WO 2014/020041 A1 Publication Date: February 6, 2014 Priority Application: EP 2012-178985 Priority Date: August, 2, 2012 Inventors: Siemeister, G.; Bader, B.; Wengner, A. M.; Mumberg, D.; Koppitz, M.; Klar, U.; Kroemer, G.; Vitale, I.; Jemaa, M. Assignee Company: BAYER Pharma AG, Germany Disease Area: Cancer Biological Target: Monopolar spindle 1 kinase (Mps-1) and antiapoptotic protein of the Bcl-2 family Summary: The present application describes imidazopyridazine derivatives (compound A) in combination with an inhibitor of an antiapoptotic protein of the Bcl-2 family (compound B) for the treatment of cancer. Compound B is selected from a group consisting of Obatoclax, Navitoclax, Beclanorsen, VMD-8018, Oblimersen, Apogossypol, 1133719, PNT-100, HG-1113, S-44563, ABT-731, ONY-701, BP-100-1.02, and AT-101. The combination described in this patent application could potentially be useful for the treatment of lung, melanoma, pancreatic, and breast cancer. Important Compound Classes:

Pyrrolopyrimidine Analogues as MKNK Inhibitors

Pyrrolopyrimidine Analogues as MKNK Inhibitors Jean-Francois Brazeau and Gerard Rosse* Structure Guided Chemistry, Dart Neuroscience LLC, 7473 Lusk Boulevard, San Diego, California 92121, United States Adjunct Associate Professor, Department of Pharmacology and Physiology, College of Medicine, Drexel University, New College Building, 245 North 15th Street, Philadelphia, Pennsylvania 19102, United States