- Five-membered or six-membered heterocyclic pyrimidine compound and applications thereof
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The invention relates to a five-membered or six-membered heterocyclic pyrimidine compound for treating diseases responsive to activation of a TLR7 receptor, and a pharmaceutical composition.
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Paragraph 0508-0515
(2020/05/08)
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- DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES
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The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.
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Page/Page column 39; 107
(2020/01/24)
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- AROMATIC ALDEHYDES WITH SUSTAINED AND ENHANCED IN VITRO AND IN VIVO PHARMACOLOGIC ACTIVITY TO TREAT SICKLE CELL DISEASE
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Compounds and methods for preventing and/or treating one or more symptoms of sickle cell diseases (SCD) by administering at least one of the compounds are provided. The compounds are based on vanillin which is chemically modified to increase bioavailability and activity, e.g. so that the compounds bind to the F helix of hemoglobin (Hb) and prevent adhesion of red blood cells (RBCs).
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Page/Page column 34
(2019/10/15)
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- An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders
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A set of novel Kv7.2/7.3 (KCNQ2/3) channel blockers was synthesized to address several liabilities of the known compounds XE991 (metabolic instability and CYP inhibition) and the clinical compound DMP 543 (acid instability, insolubility, and lipophilicity). Using the anthrone scaffold of the prior channel blockers, alternative heteroarylmethyl substituents were installed via enolate alkylation reactions. Incorporation of a pyridazine and a fluorinated pyridine gave an analog (compound 18, JDP-107) with a promising combination of potency (IC50 = 0.16 μM in a Kv7.2 thallium flux assay), efficacy in a Kv7.2/7.3 patch clamp assay, and drug-like properties.
- Porter, Jacob D.,Vivas, Oscar,Weaver, C. David,Alsafran, Abdulmohsen,DiMilo, Elliot,Arnold, Leggy A.,Dickson, Eamonn J.,Dockendorff, Chris
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supporting information
(2019/11/11)
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- Structure-based design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine-based p38 MAP kinase inhibitors
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We identified novel potent inhibitors of p38 MAP kinase using structure-based design strategy. X-ray crystallography showed that when p38 MAP kinase is complexed with TAK-715 (1) in a co-crystal structure, Phe169 adopts two conformations, where one intera
- Kaieda, Akira,Takahashi, Masashi,Takai, Takafumi,Goto, Masayuki,Miyazaki, Takahiro,Hori, Yuri,Unno, Satoko,Kawamoto, Tomohiro,Tanaka, Toshimasa,Itono, Sachiko,Takagi, Terufumi,Hamada, Teruki,Shirasaki, Mikio,Okada, Kengo,Snell, Gyorgy,Bragstad, Ken,Sang, Bi-Ching,Uchikawa, Osamu,Miwatashi, Seiji
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p. 647 - 660
(2018/01/03)
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- PIPERIDINYLPYRAZOLOPYRIMIDINONES AND THEIR USE
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The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
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- Novel S1P1 receptor agonists - Part 4: Alkylaminomethyl substituted aryl head groups
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In a previous communication we reported on the discovery of alkylamino pyridine derivatives (e.g. 1) as a new class of potent, selective and efficacious S1P1 receptor (S1PR1) agonists. However, more detailed profiling revealed that this compound class is phototoxic in vitro. Here we describe a new class of potent S1PR1 agonists wherein the exocyclic nitrogen was moved away from the pyridine ring (e.g. 11c). Further structural modifications led to the identification of novel alkylaminomethyl substituted phenyl and thienyl derivatives as potent S1PR1 agonists. These new alkylaminomethyl aryl compounds showed no phototoxic potential. Based on their in vivo efficacy and ability to penetrate the brain, the 5-alkyl-aminomethyl thiophenes appeared to be the most interesting class. Potent and selective S1PR1 agonist 20e, for instance, maximally reduced the blood lymphocyte count (LC) for 24 h after oral administration of 10 mg/kg to rat and its brain concentrations reached >500 ng/g over 24 h.
- Lescop, Cyrille,Müller, Claus,Mathys, Boris,Birker, Magdalena,De Kanter, Ruben,Kohl, Christopher,Hess, Patrick,Nayler, Oliver,Rey, Markus,Sieber, Patrick,Steiner, Beat,Weller, Thomas,Bolli, Martin H.
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supporting information
p. 222 - 238
(2016/04/20)
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- (Aza)pyridopyrazolopyrimidinones and indazolopyrimidinones and their use
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The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
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- (AZA)PYRIDOPYRAZOLOPYRIMIDINONES AND INDAZOLOPYRIMIDINONES AS INHIBITORS OF FIBRINOLYSIS
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The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
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- NOVEL COMPOUNDS
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This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
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Paragraph 0367; 0368; 0369
(2013/06/26)
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- INDAZOLE- AND PYRROLOPYRIDINE-DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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The present invention relates to a novel indazole- or pyrrolopyridine-derivative, represented by the formula (1) below, that has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same. Formula (1) [wherein each substituent is as defined in claim 1]
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Page/Page column 196
(2013/02/27)
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- INDOLIZINE INHIBITORS OF 5-LIPOXYGENASE
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Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders.
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Page/Page column 85-86
(2011/04/24)
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- NOVEL PYRIMIDINE-PYRIDINE DERIVATIVES
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The invention relates to novel pyrimidine-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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Page/Page column 23
(2011/04/14)
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- PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
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The invention relates to novel pyridine derivatives of formula (D, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents and the other substituents are as defined in the claims.
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Page/Page column 31
(2011/09/20)
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- PHENYLALANINE AMIDE DERIVATIVES USEFUL FOR TREATING INSULIN-RELATED DISEASES AND CONDITIONS
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Provided herein are compounds of formula I: wherein A, B, X, R1 , R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions
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Page/Page column 68; 69
(2010/09/03)
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- PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
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The invention relates to novel pyridine derivatives of formula (D, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents and the other substituants are as defined in the claims.
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Page/Page column 85
(2009/04/25)
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- NOVEL PYRIMIDINE-PYRIDINE DERIVATIVES
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The invention relates to novel pyrimidine-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula I.
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Page/Page column 56-57
(2009/10/22)
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- MGLUR5 MODULATORS II
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 20
(2008/06/13)
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- MGluR5 modulators IV
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 12
(2008/06/13)
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- mGluR5 modulators III
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The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
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Page/Page column 13
(2008/06/13)
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- Process for the preparation of isonicotinic acid derivatives
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The present invention relates to a process for the manufacture of compounds of formula Ia or Ib and pharmaceutically acceptable additional salts thereof, wherein R is lower alkyl. The compounds of formula Ia or Ib are valuable intermediate products for the manufacture of compounds that are pharmaceutically active as adenosine A2a receptor antagonist or metabotropic Glutamate receptor 2 antagonist. Such compounds are important in the regulation of many aspects of cellular metabolism and in the modulation of different central nervous system activities.
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Page/Page column 4
(2010/11/08)
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- Sulfone-mediated synthesis of polysubstituted pyridines
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Base-mediated and/or palladium(0)-catalysed bis(allylation) of alkyl 2-(tolylsulfonyl)acetates gives 1,6-dienes, which upon ozonolytic cleavage of the double bonds and ammonolysis give 2,6-disubstituted pyridine-4-carboxylic esters. Decarboxylation of one
- Craig, Donald,Henry, Gavin D.
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p. 2559 - 2562
(2007/10/03)
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- NEW COMPOUNDS
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The present invention relates to new compounds of formula I, (I) a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
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Page 138-139
(2010/02/06)
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- Chemical compounds
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The invention relates to quinazoline derivatives of the formula: [wherein: Y1represents —O—, —S—, —CH2—, —SO—, —SO2—, —NR5CO—, —CONR6—, —SO2NR7—, —NR8SO2— or —NR9— (wherein R5, R6, R8and R9each independently represents hydrogen, alkyl or alkoxyalkyl); R1represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino. R2represents hydrogen, hydroxy, halogeno, alkyl, alkoxy, trifluoromethyl, cyano, amino or nitro; m is an integer from 1 to 5; R3represents hydroxy, halogeno, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, cyano, amino or nitro; R4represents a group which is or which contains an optionally substituted pyridone, phenyl or aromatic heterocyclic group] and salts thereof; processes for their preparation and pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
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- Imidazole derivatives and their use as cytokine inhibitors
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As cytokine inhibitors 2,4,5-triarylimidazole compounds and compositions for use as cytokine inhibitors.
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- Pyridine derivatives and perfumery compositions containing the derivatives
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Described is pyridine derivatives defined according to one of generic formula (I) STR1 wherein R2 represents isopropenyl group when R1 is methyl or ethyl group, R2 represents isopropenyl or acetyl group when R1 is isopropenyl group, R2 represents methyl group when R1 is isopropyl group and R2 represents isopropenyl, or isopropyl group when R1 is acetyl group; and perfumery composition containing the derivatives.
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- SPIROPIPERIDINE DERIVATIVES
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Compounds are disclosed of formula (I) STR1 wherein R 1 represents hydroxy, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 carboxyalkyl, phenyl, oxo, amino, carboxy, amido,--NR 4 COR 5 (where R 4 and R 5 both represent C 1-6 alkyl), optionally substituted methyli
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- Piperidine derivatives
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Compounds are disclosed of formula (I) wherein, R1 represents hydroxy, C1 6 alkyl, C1 6 hydroxyalkyl, C1 6 carboxyalkyl, phenyl, oxo, amino, carboxy, amido, -NR4CORsu
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