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6869955 |
Tetrahydropteridines and pyridylpiperazines for treatment of neurological disorders
Corticotropin releasing factor (CRF) antagonists of formula I:
and their use in treating anxiety, depression, and other psychiatric and neurological disorders.
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6869945 |
Pyrrolyl-and imidazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6867208 |
Vitronectin receptor antagonists, their preparation and their use
The present invention relates to compounds of the formula I
A—B—D—E—F—G (I)
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6863904 |
Compositions and methods for prophylactic and therapeutic supplementation of nutrition in subjects
The present invention relates to compositions without added iron and methods for prophylactic nutritional supplementation and therapeutic nutritional supplementation. Specifically, the method...
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6861427 |
Azabicyclylmethyl derivatives of 2,3-dihydro-1,4-dioxino[2,3-f]quinoline as 5-HT1A antagonists
Compounds of the formula
are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia, and are...
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6861422 |
Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
The present invention relates to new dihydropteridinones of general formula (I):
wherein the groups L and R 1 -R 5 have the meanings given in the claims and specification, the isomers...
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6858613 |
Fused bicyclic-N-bridged-heteroaromatic carboxamides for the treatment of disease
The invention provides compounds of Formula I:
These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful...
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6858612 |
Use of tetrahydropteridine derivatives as no synthase inhibitors
The present invention relates to the use of pteridine derivatives of the formula I
in which X is O or NH and R 4 , for example, is hydrogen, phenyl or the radical R 4a —CH 2 — and R 4a ,...
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6858611 |
Potassium channel inhibitors
Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.
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6855712 |
Combination of benzoquinazoline antifolates and protecting agents
The use of a protecting agent, for example a folate derivative such as folic acid or leucovorin, in combination with a non-competitive folic acid analogue, for example benzoquinazoline derivatives,...
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6852721 |
Pharmaceutical compositions and methods for use
The present invention relates to diazabicyclic compounds, preferably to N-aryl diazabicyclic compounds. Of particular interest are 2-pyridinyl diazabicyclic compounds, such as...
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6852722 |
Compositions and methods for stimulating gastrointestinal mobility
The present invention is directed to methods for stimulating the motility of the gastrointestinal system in a patient which comprises administering a growth hormone secretagogue, a prodrug thereof...
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6849632 |
Heteroaryl alkyl piperazine derivatives
Novel compounds of the general formula:
and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage...
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6849628 |
Optically active compounds
The present invention relates to the preparation of substantially pure diastereoisomers of derivatives of tetrahydrofolate and the use of such diastereoisomers. More particularly the present...
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6849634 |
Potassium channel inhibitors
Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.
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6846823 |
Method of treating lower urinary tract disorders
The invention relates to a method of treating at least one symptom of a lower urinary tract disorder in a subject in need of treatment wherein the symptom is selected from the group consisting of...
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6846822 |
Product comprising a heterotrimeric G protein signal transduction inhibitor associated with anti-hypertensive agent for therapeutic use in the treatment of arterial hypertension
The invention concerns a product comprising at least an inhibitor of heterotrimeric G protein signal transduction, associated with at least another anti-hypertensive agent, in particular calcium...
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6844343 |
N-substituted 4-aminopteridines, synthesis and use thereof as pharmaceutical agent
Compounds of formula (I), where preferably: A=a bridge of partial formula (II) or (III), R 1 and R 2 =independently (substituted) alkyl, aryl or aralkyl, or together form a heterocycle, R 3 =H,...
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6844341 |
Pyrimidine derivatives for inhibition of cell proliferation
Compounds of the formula (I): wherein Ring A, R 1 , R 3 , R 4 , p, q, and n are as defined within and a pharmaceutically acceptable salts and in vivo hydrolyzable esters are described. Also...
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6844344 |
Benzofuran derivatives
The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of...
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6844345 |
Piperazine derivatives
The present invention provides piperazine derivatives in accordance with formula (I)
as well as salts, hydrates and esters thereof. The substituent designations are as provided in the...
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6835733 |
Tropane linked benzofuran derivatives
The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of...
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6821967 |
Substituted piperazine derivatives, the preparation thereof and their use as medicaments
The present invention relates to substituted piperazine derivatives of general formula wherein R a , R b , R c , R f , R g , X, m and n are defined as in claim 1, the isomers and salts thereof,...
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6818643 |
Neurotrophic bicyclic diamides
The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel bicyclic diamide compounds that are neuroprotective...
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6815442 |
Quinoxalinones for enhancing chemotherapy
The present invention provides 1H-quinoxalinones, of the formula: or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , and n are as defined herein. Also disclosed are pharmaceutical...
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6815214 |
Pharmaceutical uses and synthesis of diketopiperazines
The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of...
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6790462 |
Calcium dietary supplement
A dietary supplement composition contains phosphorus and from greater than 1.3 to less than 2.2 parts by weight calcium per part by weight phosphorus, and may, optionally, further contain Vitamin...
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6784178 |
Pharmacotherapy for vascular dysfunction associated with deficient nitric oxide bioactivity
A patient with a disorder involving endothelial dysfunction associated with deficient nitric oxide bioactivity, e.g., coronary artery disease, atherosclerosis, hypertension, diabetes or...
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6780861 |
Azabicyclic carbamates and their use as α-7 nicotinic acetylcholine receptor agonists
The invention provides compounds of formula (I) wherein n, A, R 1 , R 2 and R 3 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as...
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6777413 |
2-&lsqb 1H&rsqb -quinolone and 2-&lsqb 1H&rsqb -quinoxalone inhibitors of factor Xa
Novel compounds of general formula I: including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivative having activity against mammalian factor Xa is...
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6774121 |
Phospholipid prodrugs of anti-proliferative drugs
The invention discloses prodrugs comprising anti-proliferative drugs covalently linked, via bridging group, to a phospholipid moiety such that the active species is preferentially released,...
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6770653 |
Method and dosage form for treating tumors by the administration of tegafur, uracil, folinic acid, paclitaxel and carboplatin
This invention provides a method of treating a tumor in a warm-blooded animal by administering an anti-tumor effective amount of tegafur, uracil, folinic acid, paclitaxel and carboplatin.
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6762185 |
Compounds useful for treatment of cancer, compositions containing the same, and methods of their use
The invention involves compounds having the general formula (I) as described in the claims and pharmaceutical compositions comprising such compounds. The invention also relates to the use of such...
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6756367 |
Benzo-oxadiazoles, -thiadiazoles and -1,4-diazines, pharmaceutical compositions containing them and a process for preparing them
The invention provides a compound of formula I wherein X, R 1 , R 2 and Het are as defined in the description, and a process for preparing them. The compounds of formula I are useful as...
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6746673 |
Pharmaceutical compositions containing anti-Fas antibody
A pharmaceutical composition containing an anti-human Fas antibody having apoptosis inducing activity and a compound having a folate antagonist activity or a dihydrofolate reductase inhibiting...
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6743793 |
Indole derivatives, process for preparation of the same and use thereof
Indole derivatives represented by formula (I): (wherein all symbols are described in the description), a process for the preparation of the same and a DP receptor antagonist comprising it as an...
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RE38524 |
Dipeptide derivatives as growth hormone secretagogues
This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone...
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6740654 |
Squaric acid derivatives
Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L 2 is a covalent bond or an atom or group —O—,...
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6734182 |
Aryl sulfonamides and sulfamide derivatives and uses thereof
This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of...
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6730677 |
Benzofurazan compounds which enhance AMPA receptor activity
Compounds of general structural formula ( 1 ) are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of behaviors...
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6730676 |
Pyrazino-pyridazine derivatives as ligands for GABA receptors
A class of pyrazino[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 5-position, a substituted alkoxy moiety at the 3-position,...
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6727245 |
Heterobicyclic derivatives
Heterobicyclic derivatives of the formula: wherein R 1 is aryl which may have suitable substituent(s), ar(lower)alkyl which may have suitable substituent(s), halo(lower)alkyl, protected...
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6720304 |
Conjugate comprising a folic acid antagonist and a carrier
The invention relates to conjugates comprising a D-enantiomer of a folic acid antagonist and a carrier. Furthermore, the invention relates to the production of such conjugates as well as their use.
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6713482 |
Benzimidazole cyclooxygenase-2 inhibitors
This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof, wherein Ar is heteroaryl; X 1 and X 2 are independently selected from halo, C 1...
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6709679 |
Antineoplastic conjugates of transferin, albumin and polyethylene glycol
Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at...
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6706713 |
Conjugate for treating inflammatory infectious and/or skin diseases
This invention relates to the use of a conjugate comprising an active substance and a native protein which is not recognized as foreign protein for the production of a pharmaceutical preparation...
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6699856 |
Pyrazinones, compositions containing such compounds and methods of use
Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also...
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6699855 |
Inhibitors of hepatitis C virus NS3 protease
The present invention relates to compounds of Formula (I): wherein A 1 is methylene, ethylene or propylene group and A 2 is N or CR 5 , or stereoisomeric forms, stereoisomeric mixtures, or...
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6699871 |
Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in...
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6696437 |
Heterocyclically substituted benzimidazoles, the production and application thereof
The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.
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