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7384944 |
Piperazine derivatives useful as CCR5 antagonists
The use of CCR5 antagonists of the formula
or a pharmaceutically acceptable salt thereof, wherein
R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R 1 is hydrogen or...
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7381719 |
Diaryl ethers as opioid receptor antagonist
A compound of the formula (I) wherein the variables X 1 to X 10 , R 1 to R 7 including R 3′ , E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer,...
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7365069 |
Pyrimidone derivatives
The present invention relates to novel pyrimidones of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their...
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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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7351700 |
Aminomethylpyrimidines as allosteric enhancers of the GABAB receptors
The present invention relates to compounds of formula
wherein
X is —S— or —NH—; R 3 /R 4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7...
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7335659 |
Substituted 10-aryl-11H-benzo[b]fluorenes and 7-aryl-5, 6-dihydro-benzo[a]anthracenes for selective effects on estrogen receptors
This invention provides a compound, or its possible salt, having the formula,
wherein: R e and ′R e are OH, optionally independently etherified or esterified; Z is —CH 2 CH 2 — or...
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7335657 |
Cytokine inhibitors
Disclosed are compounds of formula (I)
Where Ar 1 , X, Y, Q, W, R 3 , R 4 , R 5 , R 6 and R y are defined herein. The compounds of the invention inhibit production of cytokines involved in...
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7332494 |
Method for treating allergies using substituted pyrazoles
A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
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7323464 |
Pyridine and pyrimidine derivatives
Compounds of formula (1) are described in which R a and R b is each independently a hydrogen atom or a group R c , or R a and R b together form an oxo (═O) or thio (═S) group; X is a N atom...
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7320979 |
N-[(piperazinyl)hetaryl]arylsulfonamide compounds
The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula I
in which
Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms...
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7319099 |
Benzoyl-piperazine derivatives
The invention relates to compounds of formula
wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such...
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7314878 |
Piperazine benzothiazoles as agents for the treatment of cerebral ischemic disorders or CNS disorders
The present invention is related to piperazine henzothiazole derivatives, notably for use in the treatment and/or prophylaxis of cerebral ischemic disorders or CNS disorders. The present invention...
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7314873 |
(Halo-benzo carbonyl)heterobi cyclic p38 linase inhibiting agents
Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of...
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7300937 |
Derivatives of cyano-aryl (or cyanoheteroaryl)-carbonyl-piperazinyl-pyrimidines, their preparation and application as medication
New derivatives of cyanoaryl (or cyanoheteroaryl)-carbonyl-piperazinyl-pyrimidines (I), where R 1 represents an OR 3 radical, where R 3 represents a radical derived from a saturated hydrocarbon,...
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7297698 |
N-phenyl-(2R,5S) dimethylpiperazine derivative
The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with...
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7288544 |
Pyrimidine compounds useful as N-type calcium channel antagonists
Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when...
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7273856 |
Linear basic compounds having NK-2 antagonist activity and formulations thereof
Described herein are compounds of formula (I) useful as antagonists of tachykinins in general, and in particular of neurokinin A; and the pharmaceutical formulations comprising the compounds of...
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7259162 |
Benzazole derivatives and their use as JNK modulators
The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said...
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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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7253165 |
Benzisoxazolyl-, pyridoisoxazolyl-and benzthienyl-phenoxy derivatives useful as D4 antagonists
The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D 4 antagonists. Said compounds are useful for the treatment of medical...
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7247633 |
Pyrimidine compounds and their use
A compound of the general formula (I):
wherein R 1 , R 2 , X, Y and Z are as described in the specification.
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7244735 |
Heterocyclic protein kinase inhibitors and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors of formula I:
or a pharmaceutically acceptable salt thereof, wherein Ring B, Z 1 , Z 2 , U, p, Q, R 1 , R 2 , R 3 ,...
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7238525 |
Strategy for leukemia therapy
The chimeric Bcr-Abl oncoprotein is the molecular hallmark of chronic myelogenous leukemia (CML). In the cytoplasm, the protein transduces a growth signal that is responsible for overexpansion of...
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7235556 |
Methods of treating dry eye disorders
Fused pyridazine derivatives are useful for treating dry eye disorders and other disorders requiring the wetting of the eye.
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7229995 |
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ...
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7208489 |
2-(pyridin-2-ylamino)-pyrido [2,3-d]pyrimidin-7-ones
The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders. The novel compounds of the present invention are potent inhibitors of cyclin-dependent...
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7205304 |
Sulfonyl-Derivatives as novel inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein n, m, t, R 1 , R 2 , R 3 , R 4 , L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic...
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7205297 |
Substituted 5-alkynyl pyrimidines having neurotrophic activity
The present invention relates to a series of novel substituted 5-alkynyl pyrimidines, pharmaceutical compositions which contain them, methods for their preparation, and their use in therapy,...
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7176199 |
Aryl-substituted alicyclic compound and medical composition comprising the same
An aryl-substituted alicyclic compound of the formula (I):
wherein U is 1,4,5,6-tetrahydropyrimidin-2-yl, etc., A is phenylene, etc., B is piperidine-1,4-diyl, etc., Z is —CONH—, etc., R 3 ...
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7173028 |
Pyrimidine derivatives
The present invention relates to trisubstituted pyrimidines of formula (I)
wherein
0R a to R e are defined as in claim 1, which are suitable for the treatment of illnesses characterised by...
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7166599 |
Trisubstituted pyrimidines
The present invention relates to trisubstituted pyrimidines of formula
wherein
R a to R e are defined as in claim 1, which are suitable for the treatment of illnesses in which β-amyloid...
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7160886 |
Acylated piperazine derivatives as melanocortin-4 receptor agonists
Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are...
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7151101 |
Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention relates to compounds...
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7135467 |
HIV integrase inhibitors
Compounds useful for treating HIV are disclosed having the general formula
wherein R 1 , R 2 , and B are as defined in the specification. Compositions containing the compounds and methods for...
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7132421 |
CIS-imidazoles
The present invention provides compounds according to formula I and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction...
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7112589 |
Cysteine protease inhibitors with 2-cyano-4-amino-pyrimidine structure and cathepsin k inhibitory activity for the treatment of inflammations and other diseases
The invention provides compounds of formula I or a pharmaceutically acceptable salt or ester thereof (I), wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find...
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7112585 |
Pyrimidine derivatives as corticotropin releasing factor inhibitors
The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF...
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7105520 |
Phenylalanine derivatives
Phenylalanine derivatives of the following formulae and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4...
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7105507 |
Cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and...
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7101873 |
Pyrimidinedione derivatives
Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and...
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7098214 |
Dopamine D3 receptor ligands or antagonists for use in the treatment of renal function disorders
Dopamine D 3 receptor ligands or antagonists are disclosed for use in the treatment of renal function disorders, such as diabetic nephropathy.
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7098212 |
Piperazine derivatives
The present invention relates to compounds of the formula I
and the pharmaceutically acceptable forms thereof; wherein X, Y, a, b, c, d, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein....
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7094785 |
Method of treating polycythemia vera
The invention is directed to the use of imatinib mesylate for treating polycythemia vera. Imatinib mesylate is surprisingly effective at controlling the symptoms of polycythemia vera and reducing...
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7094783 |
Bicyclic pyrimidinones as coagulation cascade inhibitors
The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel amino-bicyclic pyrimidinone compounds of Formula (I):
or a stereoisomer...
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7087614 |
Pyrimidine inhibitors of phosphodiesterase (PDE) 7
Pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula
wherein R 1 , R 2 , Z, J and L are described herein, and analogs thereof are provided which are useful in treating...
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7087608 |
Use of PDGF receptor tyrosine kinase inhibitors for the treatment of diabetic nephropathy
The present invention relates to the use of PDGF receptor tyrosine kinase inhibitors, especially of N-phenyl-2-pyrim-idine-amine derivatives of formula (I), in which the symbols and substituents...
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7067514 |
Pyrimidine compounds
This invention features pyrimidine compounds of formula (I):
R 1 is
aryl, or heteroaryl; each of R 2 and R 4 , independently, is R c , halogen, nitro, cyano, isothionitro, SR c ,...
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7056922 |
Acylamino cyclopropane derivatives
A compound of the formula
wherein D, E, F, G, L, T, W, X, Y, Z, U, A, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 R 7 are as defined in the specification, pharmaceutical compositions thereof, and...
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7022728 |
Benzimidazoles that are useful in treating male sexual dysfunction
The present invention relates to the use of compounds of formula (I)
for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual...
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7015226 |
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ...
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