147992-27-6Relevant academic research and scientific papers
Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines
Abe, Masahito,Seto, Mabel,Gogliotti, Rocco G.,Loch, Matthew T.,Bollinger, Katrina A.,Chang, Sichen,Engelberg, Eileen M.,Luscombe, Vincent B.,Harp, Joel M.,Bubser, Michael,Engers, Darren W.,Jones, Carrie K.,Rodriguez, Alice L.,Blobaum, Anna L.,Conn, P. Jeffrey,Niswender, Colleen M.,Lindsley, Craig W.
supporting information, p. 1110 - 1115 (2017/10/18)
Herein, we report the structure-activity relationships within a series of mGlu7 PAMs based on a pyrazolo[1,5-a]pyrimidine core with excellent CNS penetration (Kps > 1 and Kp,uus > 1). Analogues in this series proved to dis
Difluoro methylation reagent, preparation method and application thereof (by machine translation)
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Paragraph 0514; 0515; 0516; 0545; 0546; 0547, (2017/10/23)
The present invention discloses a two-trifluoromethylation of the reagent, preparation method and application thereof. The invention [...] methylation reagent preparation process is simple, high yield; and the reagent can be a more moderate, high-efficiently the sulfonic acid, alcohol, carbonyl and on the α carbon atom of the difluoromethyl. (by machine translation)
Novel Cyclopropabenzofuranyl Pyridopyrazinediones
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Paragraph 0371; 0372, (2016/08/29)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I wherein X, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6, R7, R10, R11, and y are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
4-AMINO-6-(4-SUBSTITUTED-PHENYL)-PICOLINATES AND 6-AMINO-2-(4-SUBSTITUTED-PHENYL)-PYRIMIDINE-4-CARBOXYLATES AND THEIR USE AS HERBICIDES
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Paragraph 0273; 0274, (2014/09/29)
Provided herein are 4-amino-6-(4-substituted-phenyl)-picolinic acids and their derivatives, and 6-amino-2-(4-substituted-phenyl)-pyrimidine-4-carboxylic acids and their derivatives, compositions comprising the acids and their derivatives, and methods of use thereof as herbicides.
Structure-activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2
Sifferlen, Thierry,Koberstein, Ralf,Cottreel, Emmanuelle,Boller, Amandine,Weller, Thomas,Gatfield, John,Brisbare-Roch, Catherine,Jenck, Francois,Boss, Christoph
, p. 3857 - 3863 (2013/07/27)
Replacement of the dimethoxyphenyl moiety in the core skeleton of almorexant by appropriately substituted imidazoles afforded novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as potent dual orexin receptor antagonists. We describe in th
NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
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Page/Page column 110, (2012/11/14)
The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
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Page/Page column 104, (2012/12/13)
The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
HETEROCYCLIC COMPOUNDS AND THEIR USE AS INHIBITORS OF PI3K ACTIVITY
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Page/Page column 228, (2012/01/15)
Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia ( T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE COMPOUNDS
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Page/Page column 18, (2011/05/08)
The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I) wherein R1, R2, R3, and R4 are as described n the description, to salts, especially pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE COMPOUNDS
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Page/Page column 38, (2010/01/30)
The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5- a]pyrazine derivatives of formula (I) wherein R1, R2, R3, and R4 are as described n the description, to salts, especially pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
