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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...
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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.;...
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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...
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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...
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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...
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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...
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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,...
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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.
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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...
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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...
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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,...
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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 ,...
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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,...
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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...
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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...
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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-...
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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.
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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.
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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...
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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...
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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...
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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,...
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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...
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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.,...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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 ...
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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...
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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...
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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...
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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.
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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,...
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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.
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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...
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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...
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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,...
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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.
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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...
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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,...
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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...
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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...
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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...
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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...
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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.
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