134872-23-4Relevant articles and documents
In vitro and in vivo profile of 2-(3-di-fluoromethyl-5-phenylpyrazol-1-yl)- 5-methanesulfonylpyridine, a potent, selective, and orally active canine COX-2 inhibitor
Li, Jin,Lynch, Michael P.,DeMello, Kristin Lundy,Sakya, Subas M.,Cheng, Hengmiao,Rafka, Robert J.,Bronk, Brian S.,Jaynes, Burton H.,Kilroy, Carolyn,Mann, Donald W.,Haven, Michelle L.,Kolosko, Nicole L.,Petras, Carol,Seibel, Scott B.,Lund, Lisa A.
, p. 1805 - 1809 (2005)
The synthesis of a novel canine COX-2 selective inhibitor, 2-(3-difluoromethyl-5-phenylpyrazol-1-yl)-5-methanesulfonylpyridine, and its in vitro and in vivo profile are described. Pyrazole 8 demonstrated excellent potency and selectivity for canine COX-2
PHD INHIBITOR COMPOUNDS, COMPOSITIONS, AND USE
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Paragraph 0701-0702, (2021/09/26)
The present invention provides, in part, novel small molecule inhibitors of PHD, having a structure according to Formula (A), and sub-formulas thereof: or a pharmaceutically acceptable salt thereof. The compounds provided herein can be useful for treatment of diseases including heart ( e.g. ischemic heart disease, congestive heart failure, and valvular heart disease), lung (e.g., acute lung injury, pulmonary hypertension, pulmonary fibrosis, and chronic obstructive pulmonary disease), liver (e.g. acute liver failure and liver fibrosis and cirrhosis), and kidney (e.g. acute kidney injury and chronic kidney disease) disease.
PCSK9 INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 184-185, (2020/07/31)
The invention relates to a novel inhibitor pharmacophore of PCSK9 and heteroaryl compounds that bind the PCSK9 protein.
PCSK9 INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 180, (2020/07/31)
The invention relates to novel heteroaryl compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cardiovascular diseases, and methods treating sepsis or septic shock, using the novel heterocyclic compounds disclosed herein.
NOVEL COMPOUNDS AS GPR119 AGONISTS
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Paragraph 0607-0609, (2017/10/26)
The present invention relates to novel compounds of formula (I) as GPR119 agonist, composition compositions containing such compounds and method of preparation thereof.
SUBSTITUTED PYRIDINONE DERIVATIVES AND METHODS FOR MANUFACTURING THE SAME
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Page/Page column 18-19, (2012/02/05)
Disclosed are a novel compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and the compound-containing pharmaceutical composition for treating a metabolic disorder. Specifically, the disclosed compound is represented by [Formula 1]. The compound activates GPR119, and thus can be used for treating metabolic disorders, that is, diabetes mellitus, diabetes mellitus-related diseases, diabetes mellitus-related microvessel complications, diabetes mellitus-related large vessel complications, cardiovascular disorders, metabolic syndrome and its constituent diseases, obesity, and other diseases. In Formula 1, P1, P2, P3, P4, L1, R4, n4, X, Y, Z1 and Z2 are the same as defined above.
NOVEL PYRIDAZINE DERIVATIVES
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Page/Page column 16, (2008/06/13)
The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R1 is hydrogen, C1-C6alkyl, C1-C6haloalkyl or C3-C6cycloalkyl; R2 is an optionally substituted hereroaryl; R3 is an optionally substituted heteroaryl; and R4 is hydrogen, halogen, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, hydroxy or cyano; or an agrochemically usable salt form thereof.
Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors
Cheng, Hengmiao,Lundy DeMello, Kristin M.,Li, Jin,Sakya, Subas M.,Ando, Kazuo,Kawamura,Kato, Tomoki,Rafka, Robert J.,Jaynes, Burton H.,Ziegler, Carl B.,Stevens, Rod,Lund, Lisa A.,Mann, Donald W.,Kilroy, Carolyn,Haven, Michelle L.,Nimz, Erik L.,Dutra, Jason K.,Li, Chao,Minich, Martha L.,Kolosko, Nicole L.,Petras, Carol,Silvia, Annette M.,Seibel, Scott B.
, p. 2076 - 2080 (2007/10/03)
The discovery of heteroaryl-phenyl-substituted pyrazole derivatives as canine selective COX-2 inhibitors is described. Structure-activity relationship (SAR) studies of this class of compounds led to the identification of compound 1 which demonstrated a ca
New efficient access to thieno[3,2-b]pyridine derivatives via regioselective lithiation of 3-methylthiopyridine
Comoy, Corinne,Banaszak, Estelle,Fort, Yves
, p. 6036 - 6041 (2007/10/03)
The synthesis of thieno[3,2-b]pyridines was achieved using a three-step process allowing the construction of the thiophenic ring with 17-34% overall yields. The key step was the regioselective lithiation-bromination of the 3-methylthiopyridine induced by
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine
Li, Jin,Lundy DeMello, Kristin M.,Cheng, Henry,Sakya, Subas M.,Bronk, Brian S.,Rafka, Robert J.,Jaynes, Burton H.,Ziegler, Carl B.,Kilroy, Carolyn,Mann, Donald W.,Nimz, Eric L.,Lynch, Michael P.,Haven, Michelle L.,Kolosko, Nicole L.,Minich, Martha L.,Li, Chao,Dutra, Jason K.,Rast, Bryson,Crosson, Rhonda M.,Morton, Barry J.,Kirk, Glen W.,Callaghan, Kathleen M.,Koss, David A.,Shavnya, Andrei,Lund, Lisa A.,Seibel, Scott B.,Petras, Carol F.,Silvia, Annette
, p. 95 - 98 (2007/10/03)
Structure-activity relationship (SAR) studies of 2-[3-di(and tri)fluoromethyl-5-arylpyrazol-1-yl]-5-methanesulfonylpyridine derivatives for canine COX enzymes are described. This led to the identification of 12a as a lead candidate for further progression. The in vitro and in vivo activity of 12a for the canine COX-2 enzyme as well as its in vivo efficacy and pharmacokinetic properties in dog are highlighted.