1903-91-9Relevant academic research and scientific papers
PYRIMIDINE DERIVATIVE
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Paragraph 0277-0278, (2019/11/14)
Cystic fibrosis is developed through mutation of Cystic Fibrosis Transmembrane conductance Regulator (CFTR), which is one type of chloride channel. An object of the present invention is to provide compounds effective in the treatment of cystic fibrosis th
TRICYCLIC PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
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, (2018/03/25)
Described herein are tricyclic compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS AND COMBINATIONS THEREOF
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Page/Page column 83, (2015/07/07)
Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS
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Page/Page column 68, (2014/01/18)
Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.
PYRROLIDINONE GLUCOKINASE ACTIVATORS
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Page/Page column 91, (2009/10/30)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
A COMBINATION OF NIACIN AND A PROSTAGLANDIN D2 RECEPTOR ANTAGONIST
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Page/Page column 212, (2008/06/13)
The present invention is directed to a pharmaceutical composition comprising Niacin or a pharmaceutically acceptable salt, solvate or N-oxide thereof, or a nicotinic acid receptor agonist, and a compound of formula (I) as defined herein, or an N-oxide thereof, or an ester prodrug thereof, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and its use for treating atherosclerosis, dyslipidemia, diabetes or a related condition while reducing substantial flushing.
2, 6-SUBSTITUTED-4-MONOSUBSTITUTEDAMINO-PYRIDIMIDINE AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS
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Page/Page column 213, (2008/06/13)
The present invention is directed a compound of Formula (I) as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, discorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like by administering to said patient a pharmaceutically effective amount of a compound according to Formula (I).
SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN
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Page/Page column 47, (2010/02/11)
The present invention provides a compound of formula (I): Y-J-NH-Z wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alkyl, C1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alkyl, C1-4alkyl, C3-5cycloalkyl, C1-4alkoxy, hydroxyC1-4alkyl, cyano, hydroxy, C1-4cycloalkoxy, C1-4alkylthio, haloC1-4alkoxy, nitro, Q, (CH2)pQ, NR2R3, -(CH2)pNR2R3 and -O(CH2)pNR2R3; wherein J is substituted at positions meta to each other by NH and Y; and Z is phenyl or pyridyl optionally substituted with one or two substituents independently selected from halogen, haloC1-4alkyl, C1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; Q is phenyl, a five-membered heterocyclic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, or a six-membered heterocyclic ring containing one, two or three nitrogen atoms, optionally substituted by C1-4alkyl; each R2 and R3 is chosen from H and C1-4alkyl, or R2 and R3, together with the nitrogen atom to which they are attached, may form a six-membered ring optionally containing an oxygen atom or a further nitrogen atom, which ring is optionally substituted by C1-4alkyl or Q; p is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in methods of therapy; use of it for manufacturing medicaments; and methods of using it to treat diseases requiring administration of a VR1 antagonist such as pain, cough, GERD and depression.
11B-HSD1 inhibitors for the treatment of diabetes
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Page/Page column 12, (2008/06/13)
Compounds of the formula (I): as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
Metabolites of the angiotensin II antagonist tasosartan: The importance of a second acidic group
Ellingboe, John W.,Collini, Michael D.,Quagliato, Dominick,Chen, James,Antane, Madelene,Schmid, Jean,Hartupee, Dale,White, Valerie,Park, C. Hyung,Tanikella, Tarak,Bagli, Jehan F.
, p. 4251 - 4260 (2007/10/03)
Described in this paper is the synthesis and pharmacological activity of five metabolites of the angiotensin II antagonist tasosartan (1). Of particular interest is the effect of the additional acidic group of the enol metabolite (8) on activity. As suggested by the structural-activity relationship of other angiotensin II antagonist series, a second acidic group can improve receptor binding activity but decrease in vivo activity after oral dosing. The metabolic introduction of a second acidic group in tasosartan bypasses this problem and contributes to the excellent profile of the compound. A molecular modeling study provides a rationale for the role of the enol group of 8 in AT1 receptor binding.
