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8178545 Dual small molecule inhibitors of cancer and angiogenesis  
The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule...
7906521 Quinazoline potassium channel inhibitors  
The present invention relates to compounds useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
7893071 Synthesis and evaluation of novel phthalimide mimics as anti-angiogenic  
The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R1 is...
7741332 Fused ring heterocycles as potassium channel modulators  
Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More...
7709479 Quinazoline derivatives and their use as pharmaceuticals  
The use of a compound of formula (I) or a salt, ester, amide or prodrug thereof; where X is O, or S, S(O) or S(O)2, NH or NR12 where R12 is hydrogen or C1-6 alkyl; R5 is selected from a group...
7696216 Aryl-quinazoline/aryl-2-amino-phenyl methanone derivatives  
A compound of formula (I): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of...
7625909 Substituted quinazolinone compounds  
A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to...
7521455 Fused ring 4-oxopyrimidine derivative  
The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist...
7491728 Pyrimidinone compounds as calcilytics  
The pyrimidinone compounds are disclosed. Methods of preparing the pyrimidinone compounds are also disclosed.
7456188 C-5 substituted quinazolinone derivatives as selective estrogen receptor beta modulators  
The present application describes compounds according to Formula I, wherein Q, R1, R2 and X are described herein, that are useful as Estrogen Receptor Beta (ERβ) modulators. Additionally, the ...
7442704 Amide derivatives  
The invention concerns amide derivatives of Formula (Ia) wherein X is —NHCO— or —CONH—; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy...
7381730 3-arylquinazoline derivatives as selective estrogen receptor beta modulators  
Novel quinazoline derivatives possessing activity as estrogen receptor beta (ERβ) modulators are provided which have the general formula I wherein X is O or S;A and B are each independently ...
7368453 Quinazolinone compounds with reduced bioaccumulation  
A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to...
7285557 Pyrimidinones as melanin concentrating hormone receptor 1  
A compound of formula (Ia) comprising a pharmaceutically acceptable salt or solvate thereof, formulations, processes of preparing, and methods of administering to mammals are provided
7223768 Fused ring heterocycles as potassium channel modulators  
Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More...
7214676 Spirotricyclic derivatives and their use as phosphodiesterase-7 inhibitors  
The invention provides compounds which are PDE7 inhibitors, having the following formula (I), (II) and (III) in which X1, X2, X3, X4, X, Y, Z, A and Z1 are as defined in the description, methods...
7205309 Quinazoline derivatives  
Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3 and A have the significance given in the specification are provided. The compounds can be...
7081461 Quinazoline compounds and pharmaceutical compositions containing them  
The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, NH or NR8 where R8 is hydrogen or C1-6alkyl; Ra is a 3-quinoline group or a group of...
7060706 Quinazolinones  
Quinazolinones of formula (I) in which R, R1, R2, R3, R4, Y, n and m have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists
6962922 Alkynylated quinazoline compounds  
A compound selected from those of formula (I): whereinW1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN;W2 represents a group selected from hydrogen, CF3, NH2, m...
6759410 3,4-dihydro-(1H)-quinazolin-2-ones and their use as CSBP/p38 kinase inhibitors  
The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolines of formula (1), or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms...
6645971 Quinazolinone derivatives  
A compound given by general formula (1): [wherein T represents oxygen or sulfur atom, Y represents alkyl, cycloalkyl group, etc., ring W represents benzene ring, etc., R1 and R2 represent...
6610678 CRF antagonistic quino-and quinazolines  
This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR6R7, OR6 or SR7; R2 is...
6562830 Method of treating a patient having precancerous lesions with phenyl quinazolinone derivatives  
Derivatives of 2-phenyl quinazolinones are useful for the treatment of patients having precancerous lesions. These compounds are also useful to inhibit growth of neoplastic cells.
6479499 2-phenyl-4-quinazolinone compounds, 2-phenyl-4-alkoxy-quinazoline compounds and their pharmaceutical compositions  
Two series of 6,7,2′,3′,4′,5′-substituted 2-phenyl-4-quinazolinones and 6,2′,3′,4′,5′-substituted 2,3-dihydro-2-phenyl-4-quinazolinones are synthesized and evaluated for cytotoxicity ag...
6316455 Method of improving the effectiveness of a cytotoxic drug or radiotherapy using a quinazolinone compound  
A range of 3-oxybenzamide compounds and related quinazolinone compounds are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC...
6306864 Atropisomers of 3-aryl-4(3H)-quinazolinones and their use as AMPA-receptor antagonists  
The present invention relates to novel atropisomers of 2-(aryl or heteroaryl)-3-aryl-4(3H)-quinazolinones of the formula I, and their pharmaceutically acceptable salts, and pharmaceutical...
6303615 2,3 disubstituded-4(3H)-quinazolinones  
The present invention relates to novel 2,3 disubstituted-4(3H)-quinazolinone compounds of the formula I: ##STR1##wherein, R1, R2 and R3 are as defined in the specification; and to the...
6225315 Method of treating nitrate-induced tolerance  
The present invention relates to methods for treating nitrate-induced tolerance in a mammal by administering a nitrate-induced tolerance treating amount of a compound of formulae (I), (II), (III)...
6225317 Crystalline (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-3,4-dihydro-2(1H)-quin azolinone  
The potent reverse transcriptase inhibitor (-)-6-Chloro-4-cyclopropylethynyl-4-trifluoromethyl-3,4-dihy dro-2(1H)-quin azolinone is produced in solvate and crystalline form. These forms are...
6114340 Fungicidal compositions  
An improved fungicidal composition is a mixture of (a) fungicide used to combat phytopathogenic fungi and (b) at least one phosphonate or phosphinate of formula R1 R2 P(O)OR3 where R1 is C6-20...
5814623 Parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamides  
Disclosed herein are parenteral solutions containing 7-halo-1,2,3, 4-tetrahydro-3-aryl-6-quinazoline sulfonamide in Tris or Bis-Tris or Tris buffer useful in the treatment of hypertension, heart...
5783577 Synthesis of quinazolinone libraries and derivatives thereof  
The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.
5721238 2,8-disubstituted quinazolinones  
2,8-Disubstituted quinazolinones are prepared by first subjecting the quinazolinone basic skeleton to condensation by customary reactions and then introducing the desired substituents into the...
5633240 Parenteral solutions containing metolazone  
Disclosed herein are parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamide in Tris or Bis-Tris or Tris buffer useful in the treatment of hypertension, heart...
5482941 Quinazolinone antianginal agents  
Compounds of formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R1 is H, C1 -C4 alkyl, C1 -C4 alkoxy or CONR5 R6 ; R2 is H or- C1 -C4 alkyl; R3 is C2 -C4 alkyl; R4 is H, C2 -C4...
5283247 Anticonvulsant substituted quinazolones  
Disclosed herein are substituted quinazolones and their N1 -oxide derivatives, methods of synthesizing such compounds, and methods of using them to treat or prevent convulsions in mammals. The...
5264439 Quinazolinone, triazolinone and pyrimidinone angiotensin II antagonists incorporating a substituted benzyl element  
Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists. ##STR1##
5248678 Methods for increasing arousal and alertness and for the amelioration of comatose states  
A method of treating comatose patients or near-comatose patients to increase their arousal and alertness as measured by the Glascow Coma Score by administering effective amounts of an adenosine...
5155110 Fenamic acid hydroxamate derivatives having cyclooxygenase and 5-lipoxygenase inhibition  
The present invention is novel selected hydroxamic acid derivatives of fenamic acids having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating...
5147875 2-(substituted phenyl)-4-oxo-quinazolines  
This invention relates to quinazolinone derivatives which have bronchodilator activity. A compound of the invention is 2-(2-propoxyphenyl)quinazolin-4(3H)-one.
5081124 Method of producing antitumor effect using quinazolin-4-one derivatives  
A quinazoline of the formula: ##STR1## wherein R1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylalkyl, halogeno, hydroxy, mercapto, pyridylthio, pyrimidinylthio, or...
5030635 6-7-dimethoxy-1,2-dihydro-2-arylquinazoline-3-oxides  
Novel 6,7-dimethoxy-1,2-dihydro-2-arylquinazoline-3-oxides and their synthesis are described. These novel compounds are cardiotonic agents and bronchodilating agents, and as such are useful for the...
5011843 Treatment of glaucoma using phosphodiesterase inhibitors  
Lowering of intraocular pressure, e.g. in the treatment of glaucoma is carried out by administering a phosphodiesterase inhibitor to a patient. Particular ophthalmic pharmaceutical compositions are...
5008266 4(3H)-quinazolinone derivatives and pharmaceutical compositions  
4(3H)-Quinazolinone derivative of formula (I) are provided. ##STR1## wherein R1 is a hydrogen atom, a C1 -C6 alkyl group, an aryl group, a substituted aryl group, or an aralkyl group; R2 is a C1...
4963554 6,7-dimethoxy-1,2-dihydro-2-arylquinazoline-3-oxides  
Novel 6,7-dimethoxy-1,2-dihydro-2-arylquinazoline-3-oxides and their synthesis are described. These novel compounds are cardiotonic agents and bronchodilating agents, and as such are useful for the...
4883800 Quinazoline derivatives and process for their production  
The invention relates to compounds having aldose reductase-inhibitory activity of the formula: ##STR1## in which R1 and R2 are each hydrogen, halogen, lower alkoxy or halo(lower)alkyl, R3 is...
4833144 2-Alkylsulfinyl-4(3H)-quinazolinone derivatives and pharmaceutical compositions  
2-Alkylsulfinyl-4(3H)-quinazolinone derivatives of formula (I) are provided. ##STR1## wherein R1 is a C1 -C6 alkyl group, an aryl group, a substituted aryl group or an aralkyl group, R2 is a phenyl...
4753943 Algicidal and fungicidal 2-haloalkyl-3-oxo-4-substituted quinazoline  
2-Haloalkyl-3-oxo-4-substituted quinazolines represented by the formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkyl substituted with one to three of the same or different halogens,...
4734419 Quinazoline derivatives, compositions thereof and their use in treating diabetic complications  
The invention relates to compounds of the formula: ##STR1## in which R1 and R2 are each hydrogen, halogen, lower alkoxy or halo(lower)alkyl, R3 is dihalophenyl, naphthyl(lower)alkyl,...
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