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6384060 |
2,4,6-trisbstituted pyridines with estrogenic activity and methods for the solid phase synthesis thereof
The present invention relates to novel substituted pyridine compounds of Formula (I) wherein the moiety Z, R 1 , R 2 and R 3 are as herein defined, having estrogenic activity, to processes for...
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6372770 |
Benzoxazoles
Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard...
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6369086 |
Substituted oxidole derivatives as protein tyrosine and as protein serine/threonine kinase inhibitors
The present invention relates generally to novel substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or...
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6369083 |
2-methoxyimino-2 (pyrinyloxymethyl) phenyl acetamides with polyether derivatives on the pyridine ring
The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamide compounds with polyether substituents on the pyridine ring, their use as fungicidal compounds, and their...
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6365584 |
Arylysulphonamide-substituted benzimidazoles having tryptase-inhibiting activity
Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are:...
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6365605 |
Substituted hydrochromenopyrroles
Compounds of formula (I): wherein: m is 0 to 3 inclusive, n is 0 to 3 and 2≦m+n≦3, p is 1 to 6 inclusive, X represents cyano or —CO—NR 4 R 5 , R 4 and R 5 being selected from hydrogen,...
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6362196 |
Method to treat pain utilizing benzimidazole NMDA/NR2B antagonists
Substituted benzimidazole derivatives that are NMDA NR2B antagonists are utilized to treat pain.
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6355653 |
Amino-triazolopyridine derivatives
The invention relates to compounds of formula wherein R 1 is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally...
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6353006 |
Substituted 2-arylimino heterocycles and compositions containing them, for use as progesterone receptor binding agents
This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones,...
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6348032 |
Method of inhibiting neoplastic cells with benzimidazole derivatives
A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to benzimidazole derivatives.
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6342497 |
2″-deoxy hygromycin derivatives
This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R 1 and R 2 are as defined herein. The compounds of formula...
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6340704 |
Cell differentiation inducing amide derivatives, their production and use
The present invention provides a compound represented by the formula: wherein R 1 is an amino group which may be substituted; R 2 is a hydrogen atom or a lower alkyl group which may be...
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6340676 |
4-aryl-1-oxa-9-thia-cyclopenta (b) fluorenes
This invention provides compounds of Formula I having the structure wherein B and D are each, independently, hydrogen, halogen, —CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon...
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6335351 |
Hydroxylansoprazole compositions and methods
Methods and compositions are disclosed utilizing hydroxylansoprazole for the treatment of ulcers in humans. Hydroxylansoprazole exhibits a lessened liability toward drug-drug interactions than...
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6326384 |
Dry blend pharmaceutical unit dosage form
The present invention provides dry blend pharmaceutical formulations in unit dosage forms comprising per dosage unit one or more active pharmaceutical ingredients or pharmaceutically acceptable...
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6326385 |
Methods for treating or preventing pain
The present invention relates to a novel method of treating of pain, using compounds that modulate KCNQ potassium channels and currents.
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6326377 |
Substituted hydrochromenopyridines
Compounds of formula (I): ##STR1## wherein: m is 0 to 3 inclusive, n is 0 to 3 and 2≤m+n≤3, p is 1 to 6 inclusive, X represents cyano or --CO--NR 4 R 5 , R 4 and R 5 being...
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6319904 |
Formulation comprising antibacterial substance and antiulcer substance
The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal...
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6316474 |
2-benzyl and 2-heteroaryl benzimidazole NMDA/NR2B antagonists
Benzimidazoles, substituted in the 2-position by substituted benzyl groups or heteroaryl groups are effective as NMDA NR2B antagonists and are useful for relieving pain.
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6310050 |
Therapeutic use of compounds with β3-agonist activity
The invention relates to the method of use of compounds with B 3 -agonist activity for inhibiting uterine contractions, preventing or slowing down premature labor, or for the treatment and/or...
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6303639 |
Propanolamine derivatives substituted by heterocyclic radicals, processes for their preparation, pharmaceuticals comprising these compounds and their use
Substituted propanolamine derivatives and pharmaceutically tolerated salts and physiologically functional derivatives thereof are described. Also described are compounds of formula (I), ##STR1## in...
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6294586 |
Hydroxyomeprazole compositions and methods
Methods and compositions are disclosed utilizing hydroxyomeprazole for the treatment of ulcers in humans. Hydroxyomeprazole exhibits a lessened liability toward drug-drug interactions than...
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6291486 |
Polycyclic Dihydrothiazoles, their preparation and use as pharmaceuticals
Polycyclic dihydrothiazoles, processes for their preparation, and their pharmaceutical uses are provided. Preferred compounds are represented by the formula I ##STR1## wherein the radicals may have...
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6280773 |
Optimally stabilized microgranule comprising 5-pyrrolyl-2-pyridylmethylsulfinylbenzimidazole derivative
The present invention relates to a microgranule prepared by using an alkali compound as a stabilizer for a 5-pyrrolyl-2-pyridylmethylsulfinylbenzimidazole derivative having the following formula...
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6274600 |
Heteroatom substituted benzoyl derivatives that enhance synaptic responses mediated by AMPA receptors
Compounds ##STR1## are useful for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof and methods for their use for treatment of...
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6271241 |
Cycloalkyl and aryl fused aminoalkyl-imidazole derivatives: modulators and GLP-1 receptors
Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , A, B, C, and D are variables defined...
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6262086 |
Pharmaceutical unit dosage form
Pharmaceutical oral unit dosage forms are comprised of, per dosage unit, one or more active ingredients or pharmaceutically acceptable salts, solvates, hydrates, or combinations thereof.
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6262084 |
Compounds that inhibit the binding of integrins to their receptors
A method for the inhibition of the binding of α 4 β 1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding;...
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6262083 |
Genipin derivative having liver protection activity
The present invention relates to novel genipin derivatives which have an excellent liver protection activity with little cytotoxicity, and these compounds are so stable in vivo that they do not...
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6255324 |
Amino-and mercurio-substituted 4',5'-dihydropsoralens and therapeutical uses thereof
5'-substituted, 4',5'-dihydropsoralen compounds (5) bearing tertiary amines (and salts thereof), quaternary ammonium moieties or organomercurial moieties are described. ##STR1## Also described are...
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6251922 |
Polycyclic 2- aminothiazole systems, processes for their preparation and pharmaceuticals comprising these compounds
The invention relates to polycyclic 2-aminothiazole systems and their physiologically tolerated salts and physiologically functional derivatives. The polycyclic 2-aminothiazole systems are...
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6248758 |
Pharmaceutical antacid
A pharmaceutical formulation comprising a benzimidazole derivative as active ingredient, and as excipients, at least one cyclodextrin and at least one amino acid.
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6228400 |
Orally administered pharmaceutical formulations of benzimidazole derivatives and the method of preparing the same
The present invention provides pharmaceutical formulations which contain (a) an inert core of sugar, sugar and starch, or microcrystalline cellulose, (b) a drug emulsion layer which is made from...
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6218388 |
Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation
Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation. ##STR1## The compounds are especially useful in treating cancer,...
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6214865 |
Macrocyclic analogs and methods of their use and preparation
The invention provides halichondrin analogs having pharmaceutical activity, such as anticancer or antimitotic (mitosis-blocking) activity, and methods of identifying agents that induce a sustained...
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6214834 |
Integrin inhibitor prodrugs
This invention relates to novel heterocycles which are useful as antagonists of the α v β 3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions...
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6211200 |
Metal complexes
Invented are zinc chelated G-CSF receptor ligands, pharmaceutical compositions containing these compounds, and methods of using these compounds as agonist of the G-CSF receptor. Also invented are...
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6207671 |
Cycloalkano-pyridines
The cycloalkano-pyridines are prepared by reacting corresponding cycloalkano-pyridine-aldehydes with suitable organometallic compounds or Wittig or Grignard reagents or reacting compounds of the...
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6207686 |
Endothelin antagonists
A compound of formula (I), in which: R 1 is lower alkyl, cyclo(lower)alkyl, optionally substituted aryl, optionally substituted heterocyclic group, cyclo(lower)alkyl(lower)alkyl, or...
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RE37087 |
Insecticidal triffluormethyl alkane derivatives
There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R 1 , R 2 , R 3 , R 4 and A have the meanings given in the description, processes for their...
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6194448 |
N, N-disubstituted amides that inhibit the binding of integrins to their receptors
A method for the inhibition of the binding of α 4 β 1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding;...
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6194426 |
5,6,7,8 tetrahydroindolizines derivatives
A novel therapeutic use of pyrrole derivatives of the folloeing formula: ##STR1## in which the variables are as defined in the specification and their salts thereof for treating conditions in which...
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6187752 |
Method for treating schizophrenia employing an ace inhibitor
A method is provided for treating schizophrenia in a mammalian species by administering an ACE inhibitor, such as captopril, alone or with a neuroleptic such as cholecystokinin, fluphenazine or...
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6177424 |
4'-Substituted-4',5'-dihydropsoralens and therapeutical uses thereof
The invention relates to 4'-substituted-4',5'-dihydropsoralen compounds of formula(V): ##STR1## In the formula R is hydrogen, a halogen, CN or an acyl group; T is a halogen, CN, a carboalkoxy group...
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6174902 |
R-rabeprazole compositions and methods
Methods and compositions are disclosed utilizing optically pure (+) rabeprazole for the treatment of ulcers in humans while substantially reducing the concomitant liability of adverse effects...
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6174910 |
AT1 receptor antagonist for the stimulation of apoptosis
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6172073 |
Compounds having effects on serotonin-related systems
A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1 A receptor. The...
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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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6166008 |
Treatment of schizophrenia with ampakines and neuroleptics
This invention relates to treatment of schizophrenia and related psychotic disorders, including enhancement of receptor functioning in synapses in brain networks responsible for higher order...
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6162815 |
RXR-agonist polycyclic aromatic compounds, pharmaceutical/cosmetic compositions comprising said compound and uses thereof
Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds having the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## which are...
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