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7351567 |
Enzymatic resolution of selective estrogen receptor modulators
The present invention relates to a process for preparing 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen-2-ol compounds useful as an estrogen agonist.
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7294629 |
Quinazoline derivatives
A compound of the formula (I)
or a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, an optically active compound thereof, a racemate thereof or a diastereomer...
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7279481 |
Quinoline and quinazoline derivatives having affinity for 5HT1-type receptors
Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided:
wherein R 1 , m, X, R 2 , n, W, p, Y, Z, R 3 , R 4 , R 5 and q have the meanings as defined in the...
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7253172 |
Dipeptidyl peptidase inhibitors for the treatment of diabetes
Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (I) are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of...
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7232824 |
Quinazoline derivatives as medicaments
Quinazoline derivatives have the formula:
or the pharmaceutically acceptable salts thereof; wherein each of Z 5 , Z 6 , Z 7 and Z 8 is N or CH and wherein one or two Z 5 , Z 6 , Z 7 and...
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7229996 |
Rifamycin derivatives
Novel rifamycin derivatives of formula I (both hydroquinone and corresponding quinone (C 1 -C 4 ) forms):
or their salts, hydrates or prodrugs thereof,
wherein: a preferred R comprises...
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7223756 |
Quinazoline compounds with therapeutic use
The invention concerns the use of the quinazoline derivatives of Formula (I) wherein each of m, R 1 , Z, n and R 3 have any of the meanings defined in the description in the manufacture of a...
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7202233 |
Alprazolam inclusion complexes and pharmaceutical compositions thereof
A pharmaceutical composition an inclusion complex and methods for treating patients and preparing said complex disclosed for transmucosal delivery comprising an inclusion complex of (a) alprazolam...
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7196086 |
Substituted dihydroquinazolines
The invention relates to substituted dihydroquinazolines and to processes for their preparation and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in...
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7148233 |
Treatment of cardiovascular and related pathologies
Methods for treating cardiovascular and related diseases such as hypertrophy are described. The methods are directed to concurrently administering a compound such as pyridoxal-5′-phosphate,...
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7144892 |
Treatment of cardiovascular and related pathologies
Methods for treating cardiovascular and related diseases such as myocardial infarction are described. The methods are directed to concurrently administering a compound such as...
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7135473 |
Cyclic diamine compound with condensed-ring groups
A cyclic diamine compound of formula (1):
wherein R 1 and R 2 are individually a hydrogen atom or a methoxy group, provided R 1 is a methoxy group when R 2 is a hydrogen atom, or a hydrogen...
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7132430 |
Treatment of cardiovascular and related pathologies
Methods for treating cardiovascular and related diseases such as arrhythmia are described. The methods are directed to concurrently administering a compound such as pyridoxal-5′-phosphate,...
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7125889 |
Treating of cardiovascular and related pathologies
Methods for treating cardiovascular and related diseases such as blood clots are described. The methods are directed to concurrently administering a compound such as pyridoxal-5′-phosphate,...
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7119084 |
Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them
The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the...
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7115626 |
Treatment of cardiovascular and related pathologies
Methods for treating cardiovascular and related diseases such as ischemia, ischemia reperfusion injuries, and myocardial ischemia, are described. The methods are directed to concurrently...
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7115625 |
Treatment of cardiovascular and related pathologies
Methods for treating cardiovascular and related diseases such congestive heart failure are described. The methods are directed to concurrently administering a compound such as...
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7115615 |
Quinazoline derivatives
The invention concerns quinazoline derivatives of Formula (I)
wherein each of m, R 1 , n, R 2 and R 3 have any of the meanings defined in the description; processes for their preparation,...
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7094780 |
3-aminoquinazolin-2,4-dione antibacterial agents
Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R 1 and R 3 include alkyl, alkenyl, cycloalkyl, aryl, hetero-cyclic, and heteroaryl; R 5 , R 6 , and R 8 include H, alkyl,...
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7087610 |
Benzothiazole antiviral agents
The invention encompasses a series of benzothiazole compounds which inhibit HIV entry and are useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions...
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7049308 |
C-nitroso compounds and use thereof
A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon,...
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7045526 |
Substituted 4-amino-2-aryl-tetrahydroquinazolines, their preparation, their use and pharmaceutical preparations comprising them
The present invention relates to compounds of formula I:
wherein R 1 , R 2 , and R 3 have the meanings indicated in the specification, which are valuable pharmaceutical active compounds for...
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7011839 |
Otic microbial combination for treatment of animals with ruptured tympanic membrane
Disclosed herein is an improved composition that is useful in treating otic infections comprising an antimicrobial and silver sulfadiazine in a therapeutically effective combination to treat otic...
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6969713 |
Piperidine and piperazine acetamide derivatives
The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the...
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6956039 |
Nitrogenous heterocylic compounds
The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which...
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6939866 |
Quinazoline derivatives
The invention concerns quinazoline derivatives of Formula (I)
wherein each of m, R 1 , n, R 2 and R 3 have any of the meanings defined in the description; process for the preparation,...
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6911446 |
Methods of modulating serine/threonine protein kinase function with quinazoline-based compounds
The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express...
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6911442 |
Quinoline derivatives as antibacterials
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt and/or N-oxide thereof:
corresponding novel medicaments, pharmaceutical compositions and/or...
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6903096 |
Quinazoline derivatives as medicaments
The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula
or the pharmaceutically acceptable salts thereof
wherein R 3 is a...
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6849625 |
Quinazoline derivatives with anti-tumour activity
The invention concerns quinazoline derivatives of Formula I
wherein each of m, R 1 , n, R 2 and R 3 have any of the meanings defined in the description; processes for their preparation,...
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6838461 |
N-(indolcarbonyl-)piperazine derivatives
Compounds of the formula I
in which R 1 , R 2 , R 4 and R 5 have the meanings indicated in claim 1 , are potent 5-HT 2A antagonists and are suitable for the treatment of psychoses,...
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6821967 |
Substituted piperazine derivatives, the preparation thereof and their use as medicaments
The present invention relates to substituted piperazine derivatives of general formula wherein R a , R b , R c , R f , R g , X, m and n are defined as in claim 1, the isomers and salts thereof,...
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6794389 |
Quinazoline derivatives and drugs
There is provided an excellent novel analgesic having an analgesic effect which is effective widely against a pain including a chronic pain or an allodynia accompanied with herpes zoster by acting...
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6699861 |
Anti-quinazoline compounds
Dihydroquinazoline derivatives of the formula where R 3 is —(CH 2 ) p —A where p is from 1 to 4 and A is a 5- or 6-membered N-containing heterocyclic ring attached via the N atom or A is...
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6689782 |
Fungal efflux pump inhibitors
This invention relates to compounds that are efflux pump inhibitors and therefore are useful as potentiators of anti-fungal agents for the treatment of infections caused by fungi that employ an...
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6673831 |
Combination therapy for reducing the risks associated with cardiovascular disease
The instant invention provides methods for preventing or reducing the risk of developing atherosclerosis, as well as for halting or slowing the progression of atherosclerotic disease once it has...
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6653305 |
Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
A compound of formula (I) wherein: R a is a benzyl or 1-phenylethyl group or a phenyl group substituted by the groups R 1 and R 2 , wherein: R 1 is a hydrogen, fluorine, chlorine, or bromine...
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6649615 |
Method for inhibiting fibrogenesis
The present invention relates to a method for inhibiting hepatic fibrogenesis, especially liver fibrogenesis, which method comprises administering an effective amount of an alpha-adrenergic...
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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., R 1 and R 2 represent...
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6635648 |
Combination therapy using sympathetic nervous system antagonists and endothelin antagonists
Methods are provided for preventing or inhibiting adverse cardiovascular effects associated with administration of a sympathetic nervous system antagonist in a subject, in which a subject in need...
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6617329 |
Aminoquinazolines and their use as medicaments
Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the...
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6613772 |
Substituted 2-aryl-4-amino-chinazolines, method for the production and use thereof as medicaments
Compounds of the formula I in which R 1 , R 2 , R 3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and...
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6566361 |
Azapirone pain treatment
A method of treating pain with acetaminophen comprises the concurrent administration of an azapirone such as buspirone. This combination of agents surprisingly results in a strengthened analgesic...
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6559186 |
Compositions and methods of treatment of sympathetically maintained pain
Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other...
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6500830 |
Conversion of modification D to modification A of doxazosin mesylate
A process for preparing doxazosin mesylate in modification A which comprises dissolving doxazosin with methanesulfonic acid in methanol or a mixture of an aprotic, polar organic solvent and...
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6489333 |
Integrin antagonists
This invention relates to novel heterocycles which are useful as antagonists of the α v β 3 integrin, the α 2b β 3 integrin, and related cell surface adhesive protein receptors, to...
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6479496 |
Methods for treating angina with ranolazine
A sustained release ranolazine formulation contains an intimate mixture of ranolazine and a partially neutralized pH-dependent binder to form a film that is mostly insoluble in aqueous media below...
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6476037 |
L-arginine and phosphodiesterase (PDE) inhibitor synergism
This invention pertains to the discovery that L-arginine and type V phosphodiesterases act synergistically to inhibit vasospasm and/or to induce vasodilation. Methods are provided using...
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6476033 |
Medicaments containing doxazosin mesylate of crystalline modification D
Drugs comprising modification D of doxazosin mesylate are described. They are suitable for treating high blood pressure.
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6423716 |
Nitrogenous heterocyclic compounds
The present invention relates to nitrogen-containing heterocyclic compounds represented by formula (I): wherein W represents 1,4-piperazinediyl, etc.; U represents NR 1 R 2 (wherein R 1 ...
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