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7625905 |
Octahydro-pyrrolo[3,4-c]pyrrole CCR5 receptor antagonists
Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) wherein R 1 -R 3 and Ar are as defined herein are antagonists of chemokine CCR5...
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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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7511038 |
Pyridazin-3(2H)-one derivatives and their use as PDE4 inhibitors
New pyridazin-e-(2H)-one derivatives having the chemical structure of general formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and...
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7507734 |
Pyridazinone derivatives
Disclosed are compounds according to the general formula (I), where the definitions of the substituents X, R 1 and R 2 are detailed in the description, as well as their physiologically acceptable...
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7491722 |
Pyridazin-3(2H)-one derivatives
Pyridazin-3(2H)-one derivatives of formula (I) are found to inhibit PDE-4. R 1 , R 2 and R 4 are organic radicals, R 3 is a cyclic group, and R 5 is an ester or an aryl or heteroaryl group.
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7476673 |
Disubstituted chalcone oximes as selective agonists of RARγ retinoid receptors
Compounds of the formula
where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases...
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7470689 |
4-benzimidazol-2-ylpyridazin-3-one derivatives
Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R 1 and R 2 are detailed in the description, and the physiologically tolerated salts...
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7465811 |
Indoline compounds
Sulfonylindoline compounds of formula I,
wherein R1 through R4, Y and Z have defined meanings, a process for preparation of such compounds, and the use as pharmaceutically active substances,...
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7462613 |
Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them
The present invention relates to novel pyridazinone derivatives of the general formula (I)
wherein
A is A1 or A2;
R is unsubstituted or at least monosubstituted C 1 -C 10 -alkyl, aryl,...
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7407950 |
N-(heteroaryl)-1H-indole-2-carboxamide derivatives and their use as vanilloid TRPV1 receptor ligands
The invention concerns compounds of general formula (I), wherein n, X 1 , X 2 , X 3 , X 4 , Z 1 , Z 2 , Z 3 , Z 4 , Z 5 and W are as defined herein.
Said compounds are ligands of the TRPV 1 ...
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7399765 |
Substituted diazabicycloalkane derivatives
Compounds of formula (I)
Z-Ar 1 —Ar 2 (I)
wherein Z is a diazabicyclic...
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7285551 |
Fused-ring compounds and use thereof as drugs
The present invention provides a fused ring compound of the following formula [I]
wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a...
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7282498 |
Substituted fused pyrroleoximes and fused pyrazoleoximes
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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7265115 |
Diazabicyclic CNS active agents
Compounds of formula I:
or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.
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7148249 |
Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments
The present invention relates to heterocyclically substituted indolinones of general formula
wherein
R 1 to R 5 and X are defined as in claim 1, the tautomers, the diastereomers, the...
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7081458 |
Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues
Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are...
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6974815 |
Hexahydro-benzimidazolone compounds useful as anti-inflammatory agents
The present invention is directed to compounds having the formula (I):
useful in treating inflammatory and immune diseases, in which K is O or S; Q is —C(═O)— or optionally substituted C...
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6903112 |
Heterocyclylindazole and -azaindazole compounds as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
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6897229 |
Synergistic combination comprising roflumilast and a PDE-3 inhibitor
The PDE 4 inhibitor N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-difluorome
thoxy benzamide, a pharmacologically tolerable salt or N-oxide thereof, in combination with a PDE 3 inhibitor is...
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6867206 |
6-carboxyphenyldihydropyridazinone derivatives and use thereof
The present invention relates to 6-carboxyphenyldihydropyridazinone derivatives having the formula
wherein R 1 , R 2 , R 3 , A, D, G, and E are as defined in the specification and claims, a...
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6861430 |
β-carboline derivatives and its pharmaceutical use against depression and anxiety
The invention provides compounds of formula (I) wherein R1 to R5 are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals.
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6846818 |
Selective inhibitors of cyclooxygenase-2
The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I:
pharmaceutical compositions containing them, to their medicinal use, and to their preparations. The...
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6762182 |
Converting cox inhibition compounds that are not COX-2 selective inhibitors to derivatives that are COX-2 selective inhibitors
A method of altering specificity of cyclooxygenase-inhibiting compounds that have a COOH moiety by changing the various COOH containing compounds, such as indomethacin, into ester derivatives or...
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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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6680316 |
Pyridazin-3-one derivatives and medicines containing the same
Objects of the invention are to provide compounds having excellent activity against interleukin-1β production and also medicines comprising them as effective ingredients. Pyridazin-3-one...
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6656941 |
Aryl substituted tetrahydroindazoles
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables R 1 , R 2 , R 3 , n, and Ar are defined herein. These compounds are highly...
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6649613 |
Diacylhydrazine derivatives
Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R 1 , 2 and R 3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin...
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6620834 |
Medicinal compositions for treating colorectal cancer
Medicinal compositions for colorectal cancer to be administered to the large intestine by taking advantage of preparations disintegrating in the large intestine, characterized by containing a...
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6562817 |
Tricyclic compound
The present invention provides a compound of the formula (I): wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5-...
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6555540 |
Combinations of aldose reductase inhibitors and selective cyclooxygenase-2 inhibitors
This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or...
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6538010 |
Compounds and methods for promoting smoking cessation
Compounds and methods for promoting smoking cessation. The compounds may be used to treat a variety of other conditions and disease states.
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6521656 |
Remedies for male sterility
Efficacious remedies for male sterility which are in the form of preparations containing as the active ingredient an adenosine A 1 antagonist.
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6511968 |
Combination therapy for treating, preventing, or reducing the risks associated with acute coronary ischemic syndrome and related conditions
The invention provides a method for treating, preventing, or reducing the risk of developing a condition selected from the group consisting of acute coronary ischemic syndrome, thrombosis,...
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6492366 |
Cyano-indole serotonin-reuptake inhibitor compound
A compound selected from those of formula (I): wherein: R 1 and R 2 each independently represent hydrogen or, alkyl, T 1 and T 2 each independently represent alkylene, G represents a...
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6472416 |
Sulfonylphenylpyrazole compounds useful as COX-2 inhibitors
The present invention encompasses novel sulfonylphenylpyrazole compounds useful in the treatment of cyclooxygenase-2 mediated diseases.
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6384070 |
Indole derivatives useful as endothelin receptor antagonists
Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R 1 and R 2 are optional substituents and independently represent C 1-6 alkyl, C 2-6 alkenyl, optionally...
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6358978 |
Substituted benzimidazoles
Compounds of formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NFκB is involved.
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6355640 |
Pyrazolopyridine adenosine antagonists
The present invention relates to a novel pyrazolopyridine compound of the following formula: wherein R 1 is aryl, and R 2 is cyclo(lower)alkyl which may have one or more suitable...
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6329418 |
Substituted pyrrolidine hydroxamate metalloprotease inhibitors
The invention provides compounds which are potent inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the...
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6306890 |
Esters derived from indolealkanols and novel amides derived from indolealkylamides that are selective COX-2 inhibitors
A compound of the formula ##STR1## where: n, and X are as defined in the specification, and the compound possesses selectivity for inhibition of cyclooxygenase-2.
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6297243 |
Methods of treating hot flashes, estrogen deficiencies and deferring menopause by the administration of a luteinizing hormone antagonist
A pharmaceutical composition comprising a LH antagonist or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier is useful for deferring the onset of menopause.
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6277877 |
Substituted n-(indole-2-carbonyl)glycinamides and derivates as glycogen phosphorylase inhibitors
Compounds of Formula (I) ##STR1## wherein R 6 is carboxy, (C 1 -C 8 )alkoxycarbonyl, benzyloxycarbonyl, C(O)NR 8 R 9 or C(O)R 12 as glycogen phosphorylase inhibitors, pharmaceutical...
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6245797 |
Combination therapy for reducing the risks associated with cardio-and-cerebrovascular disease
The instant invention provides a drug combination comprised of an HMG-CoA reductase inhibitor in combination with a COX-2 inhibitor, which is useful for treating, preventing, and/or reducing the...
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6225324 |
Antidepressant heterocyclic compounds
Compounds of formula I are useful antidepressant agents ##STR1## demonstrating potent inhibition of 5-HT reuptake. Z is selected from among various phenyl and hetaryl moieties while Y is benzyl or...
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6177442 |
Bicyclic amine derivatives
The invention provides a compound of formula (I): ##STR1## wherein A represents a bidentate group of formula --CH 2 --X--CH 2 -- (wherein X is methylene, sulfur or oxygen), X'CCY or X'WC--CYZ...
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6174883 |
3-substituted-2-oxindoles derivatives
This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H 2 synthase,...
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6166041 |
2-heteroaryl and 2-heterocyclic benzoxazoles as PDE IV inhibitors for the treatment of asthma
Novel compounds which are effective PDE IV inhibitors are disclosed. The present invention is directed to compounds having the general formula I ##STR1## wherein: X is a halogen; Q is --CH 2 ...
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6156753 |
Local administration of type III phosphodiesterase inhibitors for the treatment of erectile dysfunction
A method is provided for treating erectile dysfunction, e.g., vasculogenic erectile dysfunction such as vasculogenic impotence. The method involves the administration of a Type III...
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6100268 |
Vasoconstrictive dihydrobenzopyran derivatives
The present invention is concerned with compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R 1 is...
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