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6348488 |
Remedies for motor dysfunction and GAPDH expression inhibitors
Remedies for motor dysfunction and GAPDH expression inhibitors containing as the active ingredient N-[3-[N-(4-chlorophenylmethyl)carbamoyl]propanoyl]-L-prolina
l. Since it has an effect of...
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6348464 |
Pyrrolecarbonylimino derivatives as naaladase inhibitors
The present invention relates to pharmaceutical compositions and methods of using pyrrolecarbonylimino derivatives to inhibit N-Acetylated α-Linked Acidic Dipeptidase (NAALADase) enzyme activity,...
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6342517 |
Potassium channel activators and their use
Novel thienopyran compounds are disclosed, useful as anti-hypertensive agents and for asthma treatment. One group of the compounds has a heterocyclic ring spiro-connected at the 7-position of the...
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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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6333042 |
Use of a substance P antagonist in a cosmetic composition, and the composition thus obtained
A substance P antagonist is used in a cosmetic composition to treat sensitive skin. More specifically, a cosmetic composition containing a substance P antagonist is used to prevent and/or combat...
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6333340 |
Small molecule sulfonamides for vision and memory disorders
This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance in an animal using...
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6329417 |
Hepatitis C inhibitor tri-pepitides
Racemates, diastereolsomers and optical isomers of a compound of formula (I): ##STR1## wherein B is H, a C 6 or C 10 aryl, C 7 -16 aralkyl; Het or (lower alkyl)-Het, all of which optionally...
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6329148 |
Combined therapy of diterpenoid triepoxides and death domain receptor ligands for synergistic killing of tumor cells
A synergistic combination of ligands that interact with death domain receptors, and diterpenoid triepoxides is used to increase tumor cell killing by induction of apoptosis. Ligands useful in the...
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6316494 |
cis3, 4-chroman derivatives useful in the prevention or treatment of estrogen related diseases or syndromes
The present invention relates to therapeutically active compounds of formula I ##STR1## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel...
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6316467 |
Elevation of HDL cholesterol by 4-[(Aminothioxomethyl)-hydrazono]-N-(substituted)-4-arylbutanamides
Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the "good" cholesterol and as such may be useful for treating diseases such as atherosclerosis. These...
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6316473 |
Two surfactant-containing medicinal composition
Provided is a medicinal composition having a very satisfactory drug release profile and a very satisfactory drug absorption profile after oral administration characterized by its comprising an...
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6313164 |
Dithiolin derivatives, their preparation and their therapeutic effect
Compounds of the formula (I): ##STR1## wherein one of m and n is 0, and the other is 0, 1 or 2; k is 0 or 1 to 12; R 1 is hydrogen, a substituent which is an aryl or a heterocyclic, or an...
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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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6303569 |
Trialkyl-lock-facilitated polymeric prodrugs of amino-containing bioactive agents
The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric compounds comprise the formula: ##STR1## wherein: B is H, OH, OSiR 13 , a...
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6294551 |
N-linked sulfonamides of heterocyclic thioesters
This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as...
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6291484 |
Benzothiophenes
This invention provides novel benzothiophene compounds of the formula I: ##STR1## which are useful for the treatment of the various medical conditions associated with postmenopausal syndrome, as...
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6291509 |
Synergistic immunosuppressant composition containing a 2,2'-bi-1H-pyrrole compound
A product containing: (a) an immunosuppressant agent (A) and (b) at least one immunosuppressant 2,2'-bi-1H-pyrrole compound (B) having formula (I) wherein R 1 is hydrogen, phenyl, C 1 -C 20 ...
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6291511 |
Biarylalkanoic acids as cell adhesion inhibitors
Compounds of Formula I are antagonists of VLA-4 and/or α 4 β 7 , and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds...
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6288105 |
Antithrombotic agents
This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical...
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6288058 |
Substituted tetracyclic tetrahydrofuran derivatives
This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and...
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6284784 |
Substituted 2-pyrrolidinone activators of PKC
Compounds of formula I: ##STR1## wherein R 1 and R 2 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are PKC activators and are useful for...
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6281229 |
Heat shock factor activity inhibitors
A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor...
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6281228 |
Heterocyclic inhibitors of microsomal triglyceride transfer protein and method
Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including...
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6277833 |
Substituted triols
Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.
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6277878 |
Substituted indole compounds as anti-inflammatory and analgesic agents
This invention provides a compound of the following formula: ##STR1## or the pharmaceutically acceptable salts thereof wherein R 1 is H or C 1 -4 alkyl; R 2 is C(L')R 3 or So 2 R 4 ; Y is a...
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6274569 |
Pesticidal compositions
An agrochemical composition, comprising at least two active ingredient components together with a suitable carrier, wherein component I is I) fludioxonil...
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6274601 |
Methods of inhibiting ulcerative mucositis
A method of inhibiting ulcerative mucositis comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R 1 and R 3 are independently...
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6271252 |
Cyclic amino acid derivatives as cell adhesion inhibitors
Cyclic amino acid derivatives of Formula I are antagonists of VLA-4 and/or α 4 β 7 , and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated...
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6265428 |
Substituted phenyl compounds and derivatives thereof that modulate the activity of endothelin
Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1): ##STR1## where X and Y...
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6262079 |
Prevention and treatment of cardiovascular pathologies
A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): ##STR1## wherein Z is CO or a covalent bond; Y is H or O(C 1 -C 4 )alkyl, R 1 and...
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6258826 |
Pharmaceutical formulations and applications thereof for the treatment of estrogen deprivation syndrome
Formulations and applications thereof are described which are useful for the inhibition of various medical conditions associated with estrogen deprivation syndrome including osteoporosis and...
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6255306 |
4-indole derivatives as serotonin agonists and antagonists
The present invention relates to compounds of the formula ##STR1##
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6251919 |
Heterocyclic substituted aniline calcium channel blockers
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6251921 |
Antithrombotic diamines
This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of...
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6251931 |
Inhibitors of gap junction communication
Oleamide is an endogenous fatty acid primary amide that possesses sleep-inducing properties in animals and has been shown to effect seratonergic systems and block gap junction communication in a...
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6245783 |
Method of using neurotrophic sulfonamide compounds
This invention relates to a method of using neurotrophic low molecular weight, small molecule sulfonamide compounds having an affinity for FKBP-type immunophilins, as inhibitors of the enzyme...
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6235791 |
Use of amines to produce drugs for preventing tumor cell proliferation
The present invention relates to the use of compounds capable of displacing tritiated cis-N-cyclohexyl-N-ethyl [3-(3-chloro-4-cyclohexylphenyl)-allyl]amine from its receptors for the preparation of...
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6228867 |
Antagonists of gonadotropin releasing hormone
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety...
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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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6221838 |
Methods of treating neuropeptide Y-associated conditions
This invention describes methods of treating conditions associated with an excess of neuropeptide Y which comprises administering an analog of an obesity protein. This invention further describes...
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6218423 |
Pyrrolidine derivatives for vision and memory disorders
This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using pyrrolidine...
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6218411 |
Therapeutics for diabetic complications
An agent for treating or ameliorating diabetic complications which contains at least one potassium channel activator as an active ingredient. The drug is expected to show a therapeutic or...
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6214860 |
Synergistic antitumor composition containing a naphthalensulphonic acid derivative
A pharmaceutical composition for use in antineoplastic therapy in mammals, including humans, comprising a biologically active ureido compound of formula (I) ##STR1## wherein each of m and n,...
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6211225 |
Heterocyclic aminopyrrolidine derivatives as melatonergic agents
There is provided a novel series of heterocyclic aminopyrrolidine compounds of Formula I ##STR1## wherein R 1 , R 2 , R 3 , R 4 , W, Z and the wavy bond {character pullout} are as defined herein...
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6211201 |
Multivalent salts of pyridostigmine and related compounds
A quaternary ammonium cholinergic agent is complexed with a multivalent anion, or with multiple monovalent anions. The complex may be administered orally to a patient to treat pain, or for some...
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6200957 |
Antagonists of gonadotropin releasing hormone
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety...
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6197795 |
Preparation and use of ortho-sulfonamido heteroaryl hydroxamic acids as matrix metalloproteinase and tace inhibitors
The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-α...
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6197790 |
Benzothiophene compounds, intermediates, compositions, and methods
A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I ##STR1## wherein R 1a is --H...
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6197789 |
Prevention and treatment of cardiovascular pathologies with tamoxifen analogues
A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): ##STR1## wherein Z is CO or a covalent bond; Y is H or O(C 1 -C 4 )alkyl, R 1 and...
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6194405 |
Method of using substituted tetracyclic tetrahydrofuran derivatives
This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and...
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