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7612059 |
Pyrrolidine bicyclic compounds and its derivatives, compositions and methods of use
N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo 4-7 alkanes or thiazacyclo 4-7 alkanes, salts or...
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7605153 |
Use of paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells
The invention relates to paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives...
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7601723 |
Pyridyl substituted xanthines
The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula I
which are selective antagonists of A 2B adenosine receptors...
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7595311 |
Azepinoindole derivatives as pharmaceutical agents
Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for...
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7572784 |
Compounds and methods for inhibiting mitotic progression
This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the...
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7566707 |
Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula
wherein Y and R 1 to R 4 are defined as in claim 1 , the tautomers, enantiomers,...
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7541354 |
Bicyclo-pyrazoles
Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.
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7531531 |
Method of treating diseases associated with altered kinase activity with bicyclo-pyrazoles
Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.
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7514422 |
5HT2c receptor modulators
The present invention relates to novel compounds of Formula (I):
which act as 5HT 2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the...
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7485634 |
Azepinoindole and pyridoindole derivatives as pharmaceutical agents
Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the...
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7465722 |
Biphenyl vasopressin agonists
A compound of the formulae (I) or (II):
wherein:
Y is a moiety selected from NR or —(CH 2 ) n ;
wherein R is hydrogen or (C 1 -C 6 ) lower alkyl,
and n is 1;
represents:
...
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7419975 |
Organic compounds
Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I
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7407949 |
Benzamide derivatives as oxytocin agonists and vasopressin antagonists
Novel compounds according to general formula 1, wherein G 1 is NR 5 R 6 or a fused polycyclic group that are specific OT receptor agonists and/or V 1a receptor antagonists. Pharmaceutical...
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7393834 |
LHRH-antagonists in the treatment of fertility disorders
A method of treating infertility disorders by 1) administering an LH-RH antagonist, preferably Cetrorelix, in amounts to selectively suppress endogenous LH but not FSH secretion and 2) inducing...
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7390797 |
Fused indazole compounds
The present invention provides a novel fused indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt...
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RE40245 |
Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I:
or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase...
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7342018 |
Urokinase inhibitors and uses thereof
The invention relates to the use of derivatives of 3-amidinophenylalanine as urokinase inhibitors for treating malignant tumors and the formation of metastases.
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7329653 |
Cyclohexylphenyl vasopressin agonists
The present invention provides compounds of the general formulas:
wherein Y is NR or —(CH 2 ) n ; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic...
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7297691 |
Treatment of sleep disorders with cholinesterase inhibitors
The present invention is concerned with treatment of sleep disorders by administering a cholinesterase inhibitor, and in particular, by administering galantamine or a pharmaceutically acceptable...
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7262189 |
Benzothiazine and benzothiadiazine derivatives, method for preparing same and pharmaceutical compositions containing same
Compounds of formula (I):
wherein:
R 1 represents aryl or heteroaryl, R 2 represents hydrogen, halogen or hydroxy, X represents oxygen or sulphur, Y represents oxygen, sulphur or NR wherein...
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7235547 |
Pharmaceutical composition comprising an AChE inhibitor and a mGluR2 antagonist
The present invention relates to a pharmaceutical composition comprising an inhibitor of acetylcholinesterase (AChE inhibitor) and a metabotropic glutamate receptor 2 antagonist (mGluR2 antagonist)...
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7232815 |
1-oxa-3-aza-dibenzoazulenes as inhibitors of tumor necrosis factor production and intermediates for the production thereof
The present invention relates to derivatives of 1-oxa-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation...
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7232814 |
Use of paullone derivatives for making medicines
The invention concerns the use for producing of GSK-3β inhibiting medicines from paullone derivatives. The invention is useful for treating pathologies involving GSK-3β and CDK5.
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7211574 |
Selective D1/D5 receptor antagonists for the treatment of obesity and CNS disorders
The present invention provides compounds, which, are novel antagonists for D 1 /D 5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides...
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7196076 |
Androgen receptor modulators and methods of use thereof
Compounds of structural formula (I) are disclosed as useful for modulating the androgen receptor (AR) in a tissue selective manner in a patient in need of such modulation, and in particular for...
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7192951 |
Treatment of congestive heart failure
Combinations of diuretics and vasopressin antagonists are useful to slow and reverse the symptoms and process of congestive heart failure, to increase the excretion of water in the urine, and to...
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7176195 |
Fused azepine derivatives and their use as antidiuretic agents
Compounds according to general formulae (1 and 2), wherein G 1 is an azepine derivative and G 2 is a group according to general formulae (9–11) are new. Compounds according to the invention are...
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7166588 |
Derivatives and analogs of galanthamine
New compounds of general formula I
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7138408 |
HIV integrase inhibitors, pharmaceutical compositions and methods for their use
Beta-carboline hydroxamic acid compounds represented by formula (I)
are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to...
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7122545 |
Imidazo-benzothiazoles
The invention relates to 2-imidazo-benzothiazoles of general formula
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R′, R″, X, R′″ and n are defined herein, or a pharmaceutically...
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7067510 |
Dihydro-dibenzo[b,e]oxepine based selective estrogren receptor modulators, compositions and methods
The present invention provides a compound of the formula (I) wherein R 1 is —H, —OH, —O(C 1 –C 4 alkyl), —OCOC 6 H 5 , —OCO(C 1 –C 6 alkyl), or —OSO 2 (C 2 –C 6 alkyl); R 0 ,...
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7056910 |
1,4,5.6-tetrahydroimidazo[4,5-d]diazepine derivatives or salts thereof
To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof.
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7056909 |
Alpha v integrin receptor antagonists
The present invention relates to novel chain-fluorinated alkanoic acid derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of...
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7049310 |
Fab I inhibitors
Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections.
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7037919 |
Tetrahydroquinoline derivatives
Tetrahydroquinoline derivatives of general formula (I) or salts thereof, having a specific and strong binding affinity for AR and exhibiting AR agonism or antagonism; and pharmaceutical...
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7030109 |
1,2,3,4,5,6-Hexahydroazepino[4,5-b]indoles containing arylsulfones at the 9-position
The present invention discloses radioligands of 9-arylsulfone of the formula (X)
or a pharmaceutically acceptable salt or enantiomer thereof, which are useful in diagnosing depression, obesity...
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7022694 |
Indoles and indolines having 5-HT activity
The present invention provides compounds of Formula (I):
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and --- have any of the values defined in the specification, as well as pharmaceutical...
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6987104 |
Pyrrolidine bicyclic compounds and its derivatives, compositions and methods of use
N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo 4-7 alkanes or thiazacyclo 4-7 alkanes, salts or...
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6960577 |
Combination therapy for treatment of refractory depression
Methods for treating a patient suffering from or susceptible to treatment resistant major depression comprising administering olanzapine and fluoxetine are disclosed.
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6953787 |
5HT2C receptor modulators
The present invention relates to novel compounds of Formula (I):
which act as 5HT 2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the...
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6933304 |
Heteroarylalkanoic acids as integrin receptor antagonists
The present invention relates to a class of compounds represented by the Formula I
or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the...
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6903090 |
Substituted azepino[4,5b]indole derivatives
Disclosed are compounds of Formula (I):
wherein R 1 -R 4 , p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical...
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6897211 |
Thienodibenzoazulene compounds as tumor necrosis factor inhibitors
The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-α) and...
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6875762 |
Tetracyclic azepinoindole compounds
The present invention provides compounds of formula I:
wherein R 1 , R 2 , X and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising the...
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6852741 |
Compositions and methods for treatment of neurological disorders
The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotinic acetylcholine receptors by co-administration of metanicotine and...
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6852730 |
Substituted fused pyrazolecarboxylic acid arylamides and related compounds
Heterocyclic compounds such as 3,4,5,6-tetrahydro-2,3,10-triaza-benzo[e]azulene-1-carboxyli
c acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinoline-9-carboxylic acid arylamides,...
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6828314 |
Substituted azepino&lsqb 4,5b&rsqb indoline derivatives
The invention provides compounds of Formula (I): wherein R 1 -R 4 , p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical...
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6777406 |
Substituted pyrroloquinolines and pyridoquinolines as serotinin agonists and antagonists
The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein is R 1 , R 6a , R 6b , R 7 , R 8 , R...
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6767907 |
4-aryl-1-(indanmethyl dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl) piperidines tetrahydropyridines or piperazines
4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH 2 and...
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6765004 |
Indoloazepines as vasopressin receptor antagonists
The invention is directed to tricyclic indoloazepine compounds useful as vasopressin receptor antagonists, pharmaceutical compositions comprising the compounds of the present invention and methods...
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