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7592348 |
Heterocyclic aspartyl protease inhibitors
Disclosed are compounds of the formula I
or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein
W is a bond, —C(═S)—, —S(O)—, —S(O) 2...
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7585870 |
HIV replication inhibiting pyrimidines and triazines
This invention concerns HIV replication inhibitors of formula (I), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms...
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7566710 |
Dual molecules containing a peroxide derivative, synthesis and therapeutic applications thereof
The invention relates to dual molecules formed from coupling products complying with the formula
wherein A represents a residue of molecule with anti-malarial activity, Y 1 and Y 2 ,...
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7563788 |
Substituted Imidazo[1,2-a]pyridines as Antibacterial Agents
Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable...
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7560464 |
Polycyclic pyrimidines as potassium ion channel modulators
The present invention provides a genus of polycyclic pyrimidines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and...
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7531548 |
HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines
HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a 1 =a 2 -a 3 =a 4 - is...
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7531547 |
Diaminopyrimidines as P2X3 and P2X2/3 modulators
Compounds and methods for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a...
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7514445 |
Heteroaryl amines as glycogen synthase kinase 3β inhibitors (GSK3 inhibitors)
This invention concerns a compound of formula
a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a...
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7507738 |
5-protected aminopyrimidine compound, production method thereof and intermediate therefor
The present invention provides a production method of 5-aminopyrimidine compound represented by the formula (5) by reacting a glycine compound represented by the formula (1) with...
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7504410 |
Chk-, Pdk- and Akt-inhibitory pyrimidines, their production and use as pharmaceutical agents
This invention relates to pyrimidine derivatives of general formula (I) as inhibitors of kinases, their production as well as their use as medications for treating various diseases.
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7504396 |
Substituted heterocyclic compounds and methods of use
The present invention relates to pyrimidine or pyridine carboxamides or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell...
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7494997 |
Amide derivative
The present invention provides an amide derivative represented by the following general formula (1):
wherein R 1 represents a saturated cyclic amino group, R 2 represents alkyl, halogen or...
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7491383 |
Compositions having enhanced pharmacokinetic characteristics
Compositions comprising a therapeutic component and an efficacy enhancing component, that enhances the pharmacokinetic disposition of the therapeutic component, are disclosed. The therapeutic...
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7479495 |
N-heterocyclic inhibitors of TNF-α expression
N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I:
Methods of...
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7470700 |
Dipeptidyl peptidase inhibitors
Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV inhibitors comprising Formula I:
wherein the substituents are as described herein.
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7470685 |
Pyrimidine compounds
This invention features pyrimidine compounds of formula (I):
R 1 is
in which one of R a and R b is H or alkyl, and the other is aryl or heteroaryl optionally substituted with R d and R...
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7465735 |
5-Phenypyrimidines their preparation compositions comprising them and their use
5-Phenylpyrimidines, their preparation, compositions comprising them and their use 5-Phenylpyrimidines of the formula I
in which the substituents and the index are as defined below:
R 1 ,R 2 ...
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7462625 |
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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7452879 |
Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms...
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7449471 |
5-phenylpyrimidines, their preparation, compositions comprising them and their use
5-Phenylpyrimidines of the formula I
in which the substituents and the index are as defined below:
R 1 ,R 2 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl,...
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7442705 |
HIV replication inhibiting pyrimidines and triazines
This invention concerns HIV replication inhibitors of formula (I), The N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms...
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7429594 |
Substituted heterocyclic compounds and methods of use
The present invention relates to compounds having the general formula
or a pharmaceutically acceptable salt thereof, wherein R 1 is a saturated or unsaturated 5-, 6- or 7-membered, ring...
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7423148 |
Small molecule PI 3-kinase inhibitors and methods of their use
Compounds having formula I are provided where the variables have the values described herein.
Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a...
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7405221 |
Substituted pyrimidines
Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases...
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7378413 |
2-amino-3-(alkyl)-pyrimidone derivatives
A pyrimidone derivative represented by formula (I) or a salt thereof:
Wherein:
R1 represents a hydrogen atom or a C 1-6 alkyl group which may be substituted by a C 6,10 aryl group; R2...
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RE40332 |
Fungicidal trifluoromethylalkylamino-triazolopyrimidines
The novel compounds of formula I:
wherein (R 1 , R 2 , Hal and L 1 through L 5 are defined in the specification) show selective fungicidal activity. The new compounds may be processed with...
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7371758 |
Antimalarial pyrimidine derivatives and methods of making and using them
Compounds of the formula (I) wherein R 1 represents a hydrogen atom or a 3-halogen atom, and R 2 represents a straight-chain alkyl group containing up to 6 carbon atoms, a straight-chain alkyl...
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7358239 |
Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7345050 |
Pyrimidine compounds
The present invention relates to new compounds of the formula (I) a process for their preparation, pharmaceutical formulations containing said therapeutically active compounds and to the use of...
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7338958 |
Sulfoximine-substituted pyrimidines as CDK-and/or VEGF inhibitors, their production and use as pharmaceutical agents
This invention relates to pyrimidine derivatives of general formula I
in which Q, R 1 , R 2 , R 3 , R 4 , R 5 , X, and m have the meanings that are contained in the description, as inhibitors...
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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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7288547 |
CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents
This invention relates to 2-heteroaryl-pyrimidine derivatives of general formula I or I f as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for...
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7276510 |
HIV replication inhibitors
This invention concerns HIV replication inhibitors of formula
the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms...
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7256199 |
Pyrimidone derivatives
A pyrimidone derivative represented by the formula (I) or a salts thereof:
wherein R 1 represents an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group and the...
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7241458 |
Antiviral compositions
The present invention is concerned with pharmaceutical compositions of antiviral compounds which can be administered to a mammal, in particular a human, suffering from a viral infection. These...
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7235560 |
Pyrimidine derivative as selective COX-2 inhibitors
The invention provides the compounds of formula (I)
or a pharmaceutically acceptable salt thereof.
Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the...
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7217718 |
Induction of immune tolerance
Methods of inducing immune tolerance by administering an immunosuppressive agent and a compound represented by Formula (I) are disclosed:
Additionally methods of suppressing an immune response...
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7205302 |
Heterocyclic compound derivatives and medicines
The present invention provides a compound which is useful as a PGI 2 receptor agonist, and a pharmaceutical composition. The present invention is directed to a pharmaceutical composition...
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7183287 |
Substituted pyrimidinones
Disclosed are compounds Formula I
and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 4 , and R 5 are defined herein. These compounds are useful for treating diseases and...
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7153862 |
αv integrin receptor antagonists
The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present...
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7151106 |
Crystal modification of a N-phenyl-2-pyrimidineamine derivative, processes for its manufacture and its use
The invention relates to a new crystalline form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-
yl)pyrimidin-2-ylamino)phenyl]-benzamide of...
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7148219 |
Biaryl heterocyclic compounds and methods of making and using the same
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of...
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7138405 |
Pharmaceutical combinations
Pharmaceutical combinations suitable for treating the lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH) in men are described herein. The combinations contain an...
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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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7125882 |
Treatment of acne using alkonolamine compositions
Acne is treated or prevented by the topical application of compositions containing an alkanolamine such as dimethylaminoethanol, tyrosine, and a sulfur ingredient such as lipoic acid or...
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7109204 |
Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to...
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7105529 |
Substituted oxindole derivatives as protein tyrosine and as protein serine/threonine kinase inhibitors and compositions and methods of treating chemotherapy and radiation therapy side effects
Compounds of formula (I): wherein X is N, CH, CCF 3 , or C(C 1-12 aliphatic); R 4 is sulfonic acid, C 1-12 aliphatic-sulfonyl, sulfonyl-C 1-12 aliphatic, C 1-12 aliphatic-sulfonyl-C 1-6 ...
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7094787 |
Compositions for regulating desire for smoking
An object of the present invention is to provide a composition for suppressing craving for smoking with high safety and no dependence such that there can be performed (1) suppression of craving for...
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7091201 |
Arylalkane-sulfonamides having endothelin-antagonist activity
The invention relates to novel aryl-alkane-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including...
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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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