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7618988 |
Use of substituted aminomethyl chromans
Compounds of formula I in which R has a meaning as indicated in claim 1 , or one of their optical isomers or pharmaceutically acceptable salts, used for the treatment of extrapyramidal movement...
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7601731 |
Antimicrobial flush solutions
The present invention provides antimicrobial solutions that comprise at least one alcohol, at least one antimicrobial agent and at least one chelator and/or anticoagulant. Also provided are methods...
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7601354 |
Compositions and methods for treating cancer using immunoconjugates and chemotherapeutic agents
The present invention is based on the discovery that the administration of at least one immunoconjugate and at least one chemotherapeutic agent provides an unexpectedly superior treatment for...
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7585874 |
Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives
The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula I:
wherein
R 1 to R 5 are as defined in the specification and pharmaceutically...
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7585854 |
Method for treating endometriosis
A drug effective for prevention and therapy of endometriosis is disclosed. The drug for prevention and/or therapy of endometriosis according to the present invention comprises an antiallergic agent...
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7572798 |
Combi-molecules having signal transduction inhibitory properties and DNA damaging properties
The present invention relates to a series of new chemical agents that demonstrate anti-tumor activity. More particularly, the present invention relates to molecules, referred to as...
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7557119 |
Large substituent, non-phenolic opioids
8-Substituted-2,6-methano-3-benzazocines of general structure
are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. One embodiment is...
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7541364 |
Pyridomorphinans, pyridazinomorphinans and use thereof
Compounds represented by the formula:
wherein R is C 1-6 alkyl; C 4-6 cycloalkylalkyl; or C 3-6 alkenyl; R′ is H or C 1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl,...
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7534799 |
Pyridomorphinans, thienomorphinans and use thereof
Compounds represented by the formulae:
wherein each of Y, X and R individually is selected from the group consisting of hydrogen, hydroxy, halo, CF 3 , NO 2 , CN, NH 2 , COR 1 and CO 2 R 2 ...
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7524858 |
Substituted pyrroline kinase inhibitors
The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.
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7511054 |
Transdermally deliverable opioid prodrugs, abuse-resistant compositions and methods of using opioid prodrugs
Described herein are opioid prodrugs, methods of making opioid prodrugs, formulations comprising opioid prodrugs, and methods of using opioid prodrugs. One embodiment described herein relates to...
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7456192 |
3β-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof
The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a...
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7427629 |
Immunostimulatory compositions and methods of stimulating an immune response
The present invention provides immunostimulatory compositions that include an immune response modifier portion paired with an antigenic portion.
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7417050 |
Heterocyclic compounds
Compounds of formula I:
and pharmaceutically-acceptable salts thereof, wherein Ar and R are as defined in the specification, compositions containing such compounds and the use of such compounds...
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7417049 |
Furyl compounds
Compounds of formula I:
and pharmaceutically-acceptable salts thereof, wherein Ar and R are as defined in the specification, compositions containing such compounds and methods of using such...
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7410978 |
Once daily dosage forms of trospium
A pharmaceutical composition of a pharmaceutically acceptable trospium salt, with upon administration to a human patient generates an average steady state blood levels of trospium with a minimum (C...
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7407939 |
Protein kinase inhibitors comprising ATP mimetics conjugated to peptides or peptidomimetics
The present invention provides small molecules having high affinity to the ATP binding site of protein kinases, which are conjugated to apeptide or peptidomimetic moiety which mimics the substrate...
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7399860 |
Manufacture of polyglutamate-therapeutic agent conjugates
The invention provides new processes for preparing polyglutamic acid-therapeutic agent conjugates for clinical development and pharmaceutical use, and polyglutamic acid-therapeutic agent conjugates...
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7399769 |
Aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives
The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives of formula
wherein:
R 1 , R 2 , and R 3 are as defined herein and pharmaceutically acceptable...
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7390817 |
Combinations of a vanilloid antagonist and an NSAID for the treatment of pain
A method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, a vanilloid VR-1 antagonist or a...
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7384942 |
Pyrazine based inhibitors of glycogen synthase kinase 3
New bicyclic based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The...
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7335659 |
Substituted 10-aryl-11H-benzo[b]fluorenes and 7-aryl-5, 6-dihydro-benzo[a]anthracenes for selective effects on estrogen receptors
This invention provides a compound, or its possible salt, having the formula,
wherein: R e and ′R e are OH, optionally independently etherified or esterified; Z is —CH 2 CH 2 — or...
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RE39707 |
Camptothecin derivatives
(20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an oxyalkanoic acid and camptothecin, which is are optionally substituted at the 7, 9, 10, 11, and 12...
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7232829 |
Therapeutic compounds and methods
The invention provides kappa receptor agonists of formula (I) and delta receptor antagonists of formula (II), wherein R 1 –R 6 X and n have any of the meanings given in the specification, as...
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7220753 |
2,7-substituted octahydro-1H-pyrido[1,2-a]pyrazine derivatives as ligands for serotonin receptors
Substituted pyrido[1,2-a]pyrazines of general formula I; wherein Ar and Ar 1 represent various carbocyclic and heterocyclic aromatic rings; A represents O, S, SO, SO 2 , CHOH, C═O, or —(CR 3 R...
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7214701 |
Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising
(a) compounds of the formula (I)
in which W, X, Y, Z, A, B, D and G...
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7202255 |
Substituted [1,4] benzodioxino[2,3-e] isoindole derivatives, method for preparing and pharmaceutical compositions containing same
Compounds of formula (I):
wherein:
A is as defined in the description, Y represents a group selected from an oxygen atom and a methylene group, R 2 represents a hydrogen atom and in...
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7199129 |
Derivatives of morphine-like opioid compounds
The present disclosure concerns compounds of formula (I) and pharmaceutically acceptable salts, hydrates, solvates, pharmaceutically acceptable derivatives, pro-drugs, tautomers and/or isomers...
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7173041 |
Polyglutamic acid-camptothecin conjugates and methods of preparation
The invention provides polyglutamic acid-therapeutic agent conjugates and methods for their preparation and use.
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7153864 |
Polyglutamic acid-camptothecin conjugates and methods of preparation
The invention provides polyglutamic acid-therapeutic agent conjugates and methods for their preparation and use.
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7125884 |
N-but-3-enyl norbuprenorphine and its use as analgesic
The present invention provides compound having the structure: and pharmaceutically acceptable salts or derivatives thereof, as well as compositions including such compounds. The invention also...
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7125873 |
Beta-amino tetrahydroimidazo (1, 2-a) pyrazines and tetrahydrotrioazolo (4, 3-a) pyrazines as 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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7119100 |
Oripavine derivatives and their uses as pharmaceuticals
The present invention relates to oripavine derivatives of formula (I),
wherein R 1 is hydrogen or methyl, R 2 is methyl, cyclopropyl methyl, cyclobutyl methyl or allyl, R 3 is...
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7109243 |
Inhibitors of cathepsin S
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at...
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7084150 |
Analogs and prodrugs of buprenorphine
Disclosed are prodrugs and analogs of buprenorphine.
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7078209 |
CAK inhibitors and uses thereof
The present invention relates to compounds useful as inhibitors of CAK, compositions thereof. The present invention also relates to methods using the compositions for treating CAK-mediated...
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7071202 |
Compositions and formulations of 9-nitrocamptothecin polymorphs and methods of use therefor
A polymorphic form of 9-nitrocamptothecin is provided, the polymorph being characterizable as having, by differential scanning calorimetry, no observable endotherm and an exotherm at between 273.6...
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7064132 |
Composition and method for treatment of otitis external
A compound, process and method for increasing external auditory canal patency while simultaneously preventing the occurrence of otitis externa is disclosed wherein an aerosolized mixture of lipid...
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7049322 |
Compositions and formulations of 9-nitrocamptothecin polymorphs and methods of use therefor
A polymorphic form of 9-nitrocamptothecin is provided, the polymorph being characterizable as having, by differential scanning calorimetry, an endotherm at between 273.9 to 275.9° C., and an...
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7012079 |
Optically pure camptothecin analogues
The invention relates in particular to the compounds of general formula
in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 represent various radicals; their use as medicaments and pharmaceutical...
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7005440 |
Therapeutic uses of tri-aryl acid derivatives
The use of triaryl acid derivatives of formula (I)
and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as...
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7001906 |
Pyrido-pyrido-pyrrolo pyrrolo-indole and pyrido-pyrrolo pyrrolo carbazole derivatives, method for the production thereof and pharmaceutical compositions containing said derivatives
Compounds of formula (I):
wherein:
W 1 and W 2 , together with the carbon atoms to which they are bonded, represent a phenyl group or a pyridyl group, and at least one of the groups W 1...
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6962927 |
Method for potentiating primary drugs in treating multidrug resistant disease
The specification discloses a method for enhancing the inhibiting action of drugs against multidrug resistant cells, apparently by reversing or inhibiting the glycoprotein “pumps” associated...
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6949257 |
Pharmaceutical compositions
Spontaneously dispersible pharmaceutical compositions comprising a piperidine, e.g. 1-acylpiperidine Substance P Antagonist and its use in the treatment of CNS disorders, e.g. depression and social...
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6939856 |
Method for preparing dexchlor tannate
The invention pertains to a method for preparing dexchlorpheniramine (“dexchlor”) tannate by reacting dexchlorpheniramine free base at a temperature of about 75 to about 150° C. with tannic...
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6916822 |
Phenoxyalkylamine derivatives useful as opioid δ receptor agonists
A medicament useful for preventive and/or therapeutic treatment of nerve system diseases which comprises, as an active ingredient, a compound represented by the following general formula (I) or a...
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6896898 |
Transdermal delivery system for alkaloids of aconitum species
The present invention provides a composition of transdermally administered aconitine alkaloids for ameliorating pain and inflammation. In one aspect, an aconitine alkaloid is delivered in a...
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6893668 |
Process for isolation of anticancer agent camptothecin from Nothapodytes foetida
The present invention relates to an improved and economical process for the isolation of anticancer agent Camptothecin from the twigs and stem of Nothapodytes foetida using hot extraction 20(S)...
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6887882 |
Pharmaceutical compositions comprising chelidonine or derivatives thereof
The present invention relation to a pharmaceutical composition comprising chelidonine or derivatives thereof, with pharmaceutically acceptable carriers. The compositions according to the present...
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6878737 |
Reversal of multidrug resistance in human colon carcinoma cells
The present invention describes the use of fumitremorgin A, B and C and a series of diketopiperazines of Formula (I) to resensitize multidrug resistant (MDR) cancer cells to the cytotoxic effects...
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