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5859048 |
Pharmaceutics for mucosal administration
In pharmaceutics for mucosal administration containing pharmacologically active peptides or proteins and tolmetin or salts thereof exhibited very excellent effect as mucosal absorption enhancers....
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5859045 |
Crystalline -! 3R 4R-trans-7 methoxy 2,2-dimethyl1-3-phenyl 1-4 4-12 pyrrolidin-1 -Y1!ethoxyl 1!chromane hydrogen fumarate
The present invention provides novel crystalline (-)-3R,4R-trans-7-methoxy-2,2-dimethyl-3-phenyl-4-{4- 2-(pyrrolidin-1-yl)e thoxy!phenyl}chromane, hydrogen fumarate useful for reducing or...
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5854277 |
Thiophenebutanoic acid derivatives as matrix metalloprotease inhibitors
Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have...
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5852047 |
Pharmaceutical product comprising a salicylate of an esterifiable ace-inhibitor
Salicylates of esterifiable ACE-inhibitors, especially captopril-S-aspirinate, and processes for their preparation are described. Such compounds are useful as analgesics, in the process of...
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5849801 |
4-amino-5-oxy-2,6,6-trimethyl-2-cycloheptene compounds
4-amino-5-oxy-2,6,6-tri methyl-2-cycloheptene compounds represented by the following general formula: ##STR1## (wherein R 1 and R 2 each independently represent a hydrogen atom, an alkyl group...
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5846980 |
N-(benzhydryloxyalkyl)-4-(carboxy/carbamoyl methyl)-piperidine derivatives as antidepressants
The invention relates to substituted nitrogenous heterocycles derivatives of general formula (I) ##STR1## in the racemic or optically pure form and/or in the form of cis/trans isomers, their...
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5843983 |
Diphenylethane compounds containing a saturated heterocyclic group, their preparation, and their therapeutic use
Compounds of formula (I): ##STR1## wherein: R 1 represents a saturated heterocyclic group attached to the bond or group represented by A through a ring carbon atom; R 2a , R 2b , R 2c , R 3a , R...
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5837720 |
N-2-(pyrrolidinyl-1)-1-phenethyl) acetamides as kappa receptor antagonists
A compound of formula (I): ##STR1## and its pharmaceutically acceptable salt, wherein R is hydrogen or hydroxy; Ar is unsubstituted or substituted phenyl; X is unsubstituted or substituted phenyl...
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5837717 |
Hydroxamic acid anesthetic compounds
A compound of the following formula: ##STR1## and its pharmaceutically acceptable salt thereof, wherein R 1 and R 2 are independently hydrogen, C 1 -4 alkyl, C 3 -7 cycloalkyl, C 2 -4 alkenyl, C...
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5827876 |
Inhibition of bone loss by 3-(4-acrylamidobenzoyl) benzo b!-thiophenes
This invention relates to 3-(4-acrylamidobenzoyl)benzo b! thiophenes, to the process for their preparation, to pharmaceutical compositions and to their use for modifying the balance between bone...
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5821261 |
Substituted saturated aza heterocycles as inhibitors of nitric oxide synthase
Disclosed herein are compounds of Formula (I) ##STR1## and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and...
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5821254 |
Uses of 9-cis-retinoic acids and derivatives thereof alone or in combination with antineoplastic agents in the prevention or treatment of cancer
This invention relates to methods and compositions for preventing or treating cancer. Specifically this invention relates to the use of 9-cis-retinoic acid or derivatives thereof in preventing or...
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5821253 |
Tetrahydrobenzo a!fluorene compounds and methods of use
The invention provides tetrahydrobenzo a!fluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological...
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5811421 |
Naphthyl and dihydronaphthyl intermediates, compounds, compositions, and methods
The present invention provides compounds of formula ##STR1## wherein R 1 is --H, --OH, --O(C 1 -C 4 alkyl), --OCOC 6 H 5 , --OCO(C 1 -C 6 alkyl), or --OSO 2 (C 4 -C 6 alkyl); R 2 is C...
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5804595 |
Kappa opioid receptor agonists
The invention provides certain amino acid conjugates of substituted 2-phenyl-N- 1-(phenyl)-2-(1-heterocycloalkyl- or heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid...
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5801197 |
Rotamase enzyme activity inhibitors
This invention relates to the method of using specially formulated neurotrophic pipecolic acid derivative compounds having an affinity for FKBP-type immunophilins as inhibitors of the enzyme...
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5792762 |
Dihydrobenzofluorene compounds, intermediates, compositions and methods
The invention provides dihydronaphthofluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological...
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5792786 |
Non-steroidal anti-inflammatory fatty acid conjugates and their therapeutic use thereof
The present invention provides therapeutic conjugates which comprise a therapeutic compound bound to one to three acyl groups derived from fatty acids. The therapeutic compounds are preferably...
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5780494 |
Piperidinyl-terminated alkylamino ethynl alanine amino diol compounds for treatment of hypertension
Compounds characterized generally as piperidinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of...
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5776972 |
Kappa-opiate agonists for inflammatory bowel disorders
Pharmaceutical preparations which are suitable for the treatment of inflammatory bowel disorders and contain at least one compound of the formula I ##STR1## in which R 1 is Ar, cycloalkyl having...
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5770624 |
Certain alpha-substituted arylsulfonamido acetohydroxamic acids
Particularly the invention relates to the compounds of formula I ##STR1## wherein Ar represents carbocyclic aryl, heterocyclic aryl or biaryl; R 1 represents lower alkyl, cycloalkyl, aryl-lower...
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5763460 |
N-(piperidinyl-1-alkyl)-substituted cyclohexane carboxylic acid amides as 5-htia receptor antagonists
Compounds of formula (I) and the pharmaceutically acceptable acid addition salts thereof are 5-HT 1A binding agents and may be used, for example, as anxiolytics. In the formula a and b each...
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5756531 |
Iminoxy derivatives of indole and indene compounds as inhibitors of prostaglandin biosynthesis
The present invention provides a class of substituted indole and indene iminoxy derivatives of the formula ##STR1## which inhibit leukotriene biosynthesis and are useful in the treatment of...
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5753715 |
2-disubstituted cyclohexenyl and cyclohexyl antimicrobial agents
The invention relates to cyclohexenyl antibacterial compounds of the formula I: ##STR1## and pharmaceutical compositions containing the compounds, methods for their production and use.
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5753680 |
Heterocyclyl-benzoylguanidines
Heterocyclyl-benzoylguanidines of the formula I ##STR1## in which R 1 , R 2 , R 3 and Het have the meanings given herein, and physiologically unobjectionable salts thereof, display antiarrhythmic...
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5750559 |
Potentiation of the antireactive-antiasthmatic effect of inhaled loop diuretics by inhaled non-steroidal anti-inflammatory drugs
The antireactive-antiasthmatic effect of inhaled loop diuretics is potentiated by the use of a combination of a loop diuretic and a non-steroidal anti-inflammatory drug as an inhalant for combating...
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5747523 |
Substituted ethyl α,α-diarylmethyl ether derivatives
The invention relates to substituted ethyl α,α-diarylmethyl ether derivatives and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, and methods of...
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5744468 |
Hypotensive intraocular pressure activity of clozapine and sulpiride
This invention introduces a novel anti-glaucoma solution which comprises of Clozapine or Sulpiride and a pharmaceutical vehicle. This is the first time all the above agents have been prepared in...
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5741801 |
5-HT.sub.4 receptor antagonist
Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof: X--CO--CH 2 --Z ...
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5739142 |
4-aminobenzoylguanidine derivatives
4-Aminobenzoylguanidines of the formula I ##STR1## in which A, R 1 , R 2 and R 3 have the meanings given, and the physiologically unobjectionable salts thereof exhibit antiarrhythmic properties...
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5731335 |
(1-Heteroazolyl-1-heterocycane derivatives and their use as neuroprotective agents
This invention provides heterocyclic compounds of formula (I) that are potentially useful in the treatment of neuropsychiatric disorders associated with progressive processes leading to neuronal...
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5719136 |
Combination of progesterone antagonists and antiestrogens with partial agonistic action for hormone substitution therapy for perimenopausal and postmenopausal women
This invention describes the use of at least one compound having a progesterone-antagonistic (PA) action and at least one compound having an antiestrogenic (AO) action with a simultaneous partial...
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5716993 |
Anthranilic acid derivatives
The present invention provides an anthranilic acid derivative having a cGMP-PDE inhibitory activity. An anthranilic acid derivative represented by the general formula (I) or a pharmacologically...
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5714491 |
Peptidyl derivatives as metalloproteinase inhibitors
Peptidyl derivatives are disclosed that are orally active metalloproteinase inhibitors. The peptidyl derivatives have a selective gelatinase action, have a long duration of action, and are useful...
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5708010 |
Methods of inhibiting myeloperoxidase activity
A method of inhibiting myeloperoxidase activity or a physiological condition associated with an excess thereof, comprising administering to a human in need thereof an effective amount of a compound...
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5698572 |
Methods of inhibiting turner's syndrome
A method of inhibiting Turner's Syndrome 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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5691353 |
Method of inhibiting aortal smooth muscle cell proliferation using naphthyl compounds
The present invention provides a compound of formula I ##STR1## wherein R 1 is H, OH, halo, OCO(C 1 -C 6 alkyl), OCO(aryl), OSO 2 (C 4 -C 6 alkyl), OCOO(C 1 -C 6 alkyl), OCOO(aryl), OCONH...
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5686447 |
Aminoalkyloximes for treating depression and affective disorders
Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.
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5679700 |
Substituted phosphinic acid-containing peptidyl derivatives as antidegenerative agents
Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis,...
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5670546 |
N-Arylalkylphenylacetamide derivatives
N-arylalkylphenylacetamide compounds of formula (I), and pharmaceutically acceptable salts thereof, possess potent analgesic and anti-inflammatory activities. ##STR1##
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5670514 |
Compositions for inhibiting bone loss
The present invention provides methods of inhibiting bone loss in mammals via the administration to a mammal in need of such treatment an effective amount of a compound from a series of...
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5658931 |
Method for inhibiting mammalian breast carcinoma with tamoxifen, and analogs thereof, and certain naphthyl compounds
The present invention provides a method of inhibiting hormone-dependent breast carcinoma in a mammal comprising administering to said mammal in need of treatment an effective amount of a first...
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5650397 |
Antioccidial method
The present invention is directed to anticoccidial methods, animal feed premixes, and animal feeds, employing a specified o-phenylenediamine or benzimidazole. The present invention is also directed...
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5643960 |
Method of delaying onset of alzheimer's disease symptoms
The present invention relates, in general, to a method of preventing or delaying the onset of Alzheimer's disease and related neurodegenerative disorders. The method involves the administration to...
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5637310 |
Method of treating prostatic adenocarcinoma
Invented is a Method of Treating Prostatic Adenocarcinoma by employing asteroid 5-α-reductase inhibiting compound or a combination of steroid 5-α-reductase inhibiting compounds.
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5633277 |
Sulfonamide aminomethylene derivatives as immunosuppressants
Compounds which suppress human T-lymphocyte proliferation are disclosed. The active compounds essentially contain at least the following structure: ##STR1##
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5622975 |
Methods for inhibiting vascular smooth muscle cell migration
Methods of inhibiting vascular smooth muscle cell migration comprising administering to a human or other mammal in need of treatment an effective amount of a compound having the formula ##STR1##...
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5614536 |
Substituted N-aminoalkylmethane sulfanilide as antispasmodica
Substituted N-aminoalkylmethane sulfanilide of formula (I), their solutions and pharmaceutically acceptable addition salts, their pharmaceutical compositions and their therapeutic use. In formula...
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5607956 |
1-heteroazolyl-1-heterocyclyl alkane derivatives and their use and their use as neuroprotective agents
The present invention relates to novel heterocyclic compounds having the general formula (1) ##STR1## geometric and optical isomers and racemates thereof where such isomers exist, as well as...
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5607950 |
Muscarinic receptor antagonists
The invetion is a method of treating irritable bowel syndrome with a compound selected from the formula ##STR1## wherein R, R 1 , m, n p are as defined in the specification, or a pharmaceutically...
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