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RE38761 Styryl compounds which inhibit EGF receptor protein tyrosine kinase  
A method of inhibiting cell proliferation in a patient suffering from such disorder comprising administering to said patient an effective amount of a composition comprising, in admixture with a...
6875770 Indole derivative having heterocycle and mono- or diazaindole derivative  
There is provided a compound represented by the general formula (1): wherein Het represents an optional substituted heterocylic group A 1 and A 2 each independently represent —CH═, etc.;...
6864266 4-piperidinyl alkyl amine derivatives as muscarinic receptor antagonists  
This invention relates to the (R)-isomers of compounds which are generally muscarinic receptor antagonists and which are represented by Formula I: wherein p, R 1 , R 2 , R 3 and A are as...
6855730 3-methylidenyl-2-indolinone modulators of protein kinase  
The present invention relates to novel 3-methylidenyl-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore...
6852717 Compounds useful as anti-inflammatory agents  
Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are...
6806278 Amino-tetralin derivatives as muscarinic receptor antagonists  
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein R 1 , R 2 , R 3 and R 4 are as defined in the...
6800646 Sulfamato hydroxamic acid metalloprotease inhibitor  
A sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses,...
6770637 Substituted 4-phenyl-pyridine compounds with activity as antagonists of neurokinin 1 receptors  
Substituted 4-phenyl-pyridine compounds with activity as antagonists of Neurokinin 1 receptors, methods of making these compounds and preparing.
6770659 Benzoyl piperidine compounds  
Provided herein are racemic or enantiomerically enriched benzoyl piperidine compounds and pharmaceutically useful salts thereof, pharmaceutical compositions comprising an effective amount of...
6759412 Acylated 6,7,8,9-tetrahydro-5H-benzocycloheptenyl amines and their use as pharmaceutical agents  
The present invention relates to compounds according to the general formula (I), wherein R 1 -R 4 have the meanings given in the description, A is CH 2 , CHOH or CH—(C 1 -C 3 -alkyl), B, C...
6759414 Aromatic amides  
This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa,...
6750216 Kappa agonist compounds and pharmaceutical formulations thereof  
Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formula IIIB have the structure: wherein R 1 ,...
6743817 Substituted fused pyrroleimines and pyrazoleimines  
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R 1 and R 2 are defined herein. These compounds are highly selective agonists,...
6743788 Carbamate and oxamide compounds  
Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or...
6730671 Compounds useful as reversible inhibitors of cathespin S  
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are...
6723718 Substituted α, β-anellated butyrolactones  
The present invention relates to novel substituted α,β-fused butyrolactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper-...
6699864 Substituted phenyl-piperazine derivatives, their preparation and use  
The present invention provides compounds of the formula: wherein R 1 -R 8 , X, Y, Z, n and m are defined in the application. The compounds of the invention have affinity for the 5-HT 1A receptor.
6683079 3-(amino-or aminoalkyl) pyridinone derivatives and their use for the treatment of HIV related diseases  
3-(amino- or aminoalkyl) pyridinone derivatives having the formula (1) wherein Q, X, Y, and R 3 -R 6 are as defined, which derivatives are useful for the treatment of HIV related diseases.
6670382 Hydroxyformamidine derivatives and medicines containing the same  
Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or...
6656959 PDE IV inhibiting pyridine derivatives  
The present invention concerns pyridine derivatives having the formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein...
6656954 Sulfonyl divalent aryl or heteroaryl hydroxamic acid compounds  
A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises...
6645962 Process of using prodigiosin as an immunosuppressive  
There are disclosed a novel microorganism Serratia marcescens strain and a prodigiosin isolated from the microorganism. The prodigiosin is useful as an immunosuppressive in various fields,...
6642233 1-Phenacyl-3-phenyl-3-(piperidylethyl)piperidine derivatives, process for the preparation thereof and pharmaceutical compositions containing them  
The invention relates to the compounds of formula: as well as to the salts thereof with inorganic or organic acids, to solvates thereof and/or to hydrates thereof, which have strong affinity and...
6642228 α1b-adrenergic receptor antagonists  
There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R 1 is hydrogen etc., B is bond, or B—N—R 1 forms a ring structure and is piperidine etc.,...
6638930 Morpholine and thiomorpholine tachykinin receptor antagonists  
Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium...
6635637 Cyclic oxyguanidine protease inhibitors  
Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R 1 , R 3 -R 6 , R 21 -R 26 , L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or...
6613765 Use of NK-1 receptor antagonists for treating major depressive disorders  
The present invention provides methods for the treatment of major depressive disorders comprising oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and...
6610707 Heterocyclic compounds as inhibitors of rotomase enzymes  
Compounds of the formula: wherein R 1 , Y, W, A and R 2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal...
6608057 Compounds useful as reversible inhibitors of cathepsin S  
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are...
6608052 Compounds useful as anti-inflammatory agents  
Disclosed are novel aromatic compounds of the formula(I) wherein G, E, W, Ar, X, Y and Z. The compounds are useful for treating diseases or pathological conditions involving inflammation such as...
6599902 5-aralkysufonyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives as kinase inhibitors  
The present invention relates to certain 5-aralkylsulfonyl-3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions...
6586431 3,3-Biarylpiperidine and 2,2-biarylmorpholine derivatives  
The present invention relates to compounds of the formula I, wherein Z 1 , Z 2 , X, Q, R 1 , R 2 and R 3 are defined as in the specification, pharmaceutical compositions containing such...
6579873 3 (5)-heteroaryl substituted pyrazoles as p38 kinase inhibitors  
A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I wherein R 1 , R 2 , Ar 1 and HetAr 2 ...
6579872 Bezamide derivatives for the treatment of diseases mediated by cytokines  
The invention concerns the use of amide derivatives of formula (I) wherein: R 1 and R 2 are substituents such as hydroxy, C 1-6 alkoxy, mercapto, C 1-6 alkylthio, amino, C 1-6 alkylamino and...
6576650 Peripherally active anti-hyperalgesic opiates  
Compositions and methods using the compositions for treatment of peripheral hyperalgesia are provided. The compositions contain an anti-hyperalgesia effective amount of one or more compounds that...
6573267 Useful aroyl aminoacyl pyrrole compounds  
This invention is directed to aroyl aminoacyl pyrroles pharmaceutically useful as agents and modulators for the treatment of central nervous system disorders and a method for the treatment of...
6573261 Method for treating or preventing psychosomatic and psychoimmunologic disorders  
This invention relates to the use of a tachykinin receptor antagonist for treating a psychosomatic or a psychoimmunological disorder in a patient.
6566376 Diphenyl-piperidine derivative  
The invention provides compounds of general formula (I) wherein R 1 , R 2 , R 3 , R 4 , A, Q, U, V, W, X, Y and n are as defined in the specification, processes for their preparation,...
6562820 Method for treatment and prevention of mastitis  
The invention is directed to a method of treatment or prevention of mastitis in mammals with known oxazolidinone anti-bacterial agents, either alone or in combination with exogenous lactoferrins.
6552020 Compositions including antibiotics and methods for using same  
Compositions including a quinolone component, such as ofloxacin, having fungistatic activity in the compositions, present in an amount effective as an antibiotic when the composition is placed in a...
6548497 Methods of reducing non-inflammatory pain  
Methods for reducing non-inflammatory pain caused by injuries and traumas include administering to a mammal eye having non-inflammatory pain a therapeutically effective amount of a composition...
6545021 Use of substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds for treating hepatitis virus infections  
N-Substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds of Formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections,...
6544992 Urotensin-II receptor antagonists  
The present invention relates to pyrrolyl and pyridyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of urotensin II.
6544991 Compositions and methods for treating bacterial infections  
A composition having antibacterial activity is disclosed. More particularly, a mixture of an oxazolidinone compound, sulbactam, and ampicillin active agents, demonstrating activity against...
6511975 Spiropiperidine derivatives  
A compound of the formula (I) wherein R 1 and R 2 is a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group. A is CH 2 , CO or SO 2 . B is a single bond,...
6495550 Pyridine-substituted benzanilides as potassium ion channel openers  
The present invention provides a genus of pyridine-substituted benzanilides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and...
6492361 Antibiotic compositions and methods for using same  
Compositions including a quinolone component in an amount effective as an antibiotic when the composition is placed in a mammalian eye, and a carrier component in an amount effective to act as a...
6489354 3-alkyl substituted pyrrolidine modulators of chemokine receptor activity  
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of chemokine...
6489324 Piperazine compounds as inhibitors of MMP or TNF  
A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R 1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an...
6482829 Substituted heterocyclic siprodecane compound active as an antagonist of neurokinin 1 receptor  
The invention relates to compounds of the formula as described herein and pharmaceutically acceptable acid addition salts thereof. The described compounds have a good affinity to the NK1 receptor.