165547-79-5Relevant academic research and scientific papers
Medicine composition for treating myocardial damage and preparation method and use thereof
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Paragraph 0023; 0025; 0026; 0027; 0028, (2018/09/26)
The invention discloses a medical composition for treating myocardial damage, and belongs to the technical field of medicines. The medical composition comprises active components having the structureas shown in the description, one or more of a pharmaceutic adjuvant, a diluent or a carrier. The invention further relates to a preparation method and application of the medical composition. The medical composition has the effect of protecting cardiac muscle cell structures and functions, in addition, can also alleviate ischemia reperfusion injury, is notable in effect, and can be used as a medicine used by patients suffering from myocardium damage.
1-SUBSTITUTED 1,2,3,4-TETRAHYDRO-1,7-NAPHTHYRIDIN-8-AMINE DERIVATIVES AND THEIR USE AS EP4 RECEPTOR ANTAGONISTS
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Paragraph 0250, (2017/02/09)
The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof has an EP4 receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of EP4 receptor associated diseases (e.g., rheumatoid arthritis, aortic aneurysm (e.g. abdominal aortic aneurysm, thoracic aortic aneurysm, thoracoabdominal aortic aneurysm etc.), endometriosis, ankylosing spondylitis, inflammatory breast cancer etc.) and the like.
INHIBITORS OF HIF PROLYL HYDROXYLASE
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Page/Page column 108, (2016/04/20)
The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
Discovery of imigliptin, a novel selective DPP-4 inhibitor for the treatment of type 2 diabetes
Shu, Chutian,Ge, Hu,Song, Michael,Chen, Jyun-Hong,Zhou, Huimin,Qi, Qu,Wang, Feng,Ma, Xifeng,Yang, Xiaolei,Zhang, Genyan,Ding, Yanwei,Zhou, Dapeng,Peng, Peng,Shih, Cheng-Kon,Xu, Jun,Wu, Frank
supporting information, p. 921 - 926 (2014/09/17)
We report our discovery of a novel series of potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. Starting from a lead identified by scaffold-hopping approach, our discovery and development efforts were focused on exploring structure-activity relationships, optimizing pharmacokinetic profile, improving in vitro and in vivo efficacy, and evaluating safety profile. The selected candidate, Imigliptin, is now undergoing clinical trial.
Process Development and Multikilogram-Scale Synthesis of a TRPV1 Antagonist
Cleator, Ed,Scott, Jeremy P.,Avalle, Paulo,Bio, Matthew M.,Brewer, Sarah E.,Davies, Antony J.,Gibb, Andrew D.,Sheen, Faye J.,Stewart, Gavin W.,Wallace, Debra J.,Wilson., Robert D.
, p. 1561 - 1567 (2014/01/06)
The process development and multikilogram preparation of a TRPV1 antagonist, 1, is described. Pyrido[2,3-b]pyrazine 1 was prepared in a convergent manner by the coupling of two key fragments, glyoxal 2 and diamine 3. Glyoxal 2 was synthesized in six chemical steps in 20% overall yield, the key step being a challenging Grignard reaction to install the glyoxalate moiety. Diamine 3 was also prepared in six chemical steps in 46% overall yield, exploiting a regioselective nucleophilic aromatic substitution to obtain the key nitrodiamine intermediate 19.
Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin- 3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists
Dzierba, Carolyn D.,Sielecki, Thais M.,Arvanitis, Argyrios G.,Galka, Amy,Johnson, Tricia L.,Takvorian, Amy G.,Rafalski, Maria,Kasireddy-Polam, Padmaja,Vig, Shikha,Dasgupta, Bireshwar,Zhang, Ge,Molski, Thaddeus F.,Wong, Harvey,Zaczek, Robert C.,Lodge, Nicholas J.,Combs, Andrew P.,Gilligan, Paul J.,Trainor, George L.,Bronson, Joanne J.,MacOr, John E.
scheme or table, p. 4986 - 4989 (2012/08/28)
Pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones were evaluated as corticotropin-releasing factor-1 receptor antagonists. The synthesis, SAR studies and pharmacokinetic evaluation of these analogs are described herein.
FUSED PYRIDINE DERIVATIVES
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Page/Page column 29, (2012/12/13)
Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
FUSED PYRIDINE DERIVATIVES
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Page/Page column 32, (2012/12/13)
Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
HETEROCYCLIC DERIVATIVES
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Page/Page column 53, (2011/02/25)
The present invention relates to heterocyclic derivatives, and more particularly, to novel heterocyclic derivatives useful for the preparation of medicaments for treating diseases related to uric acid.
PROCESS FOR PREPARATION OF NITROPYRIDINE DERIVATIVES
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Page/Page column 15, (2010/08/18)
Disclosed here is a process for the preparation of nitropyridine derivatives of Formula (I) and its salt and precursors such as halogenated amino pyridines; Wherein; R1 is selected from amino group, hydroxyl group, acyl group, alkyl amino group, halogen atom, -NH - C (O) - R3; Where R3 is branched or linear alkyl group having 1 - 6 carbon atoms, or cycloalkyl group having 3 - 6 carbon atoms; R2 is selected from hydroxyl group, halogen atom, alkoxy group,
