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5985908 |
MCBI analogs of CC-1065 and the duocarmycins
MCBI (7-methoxy-1,2,9a-tetra-hydrocyclopropa[c]benz[e]indol-4-one
) is employable as a DNA alkylating agent and can be incorporated into analogs of CC-1065 and the duocarmycins for constructing...
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5981592 |
Method and composition for treating cystic fibrosis
A composition for use in preventing colorectal cancer and other neoplastic diseases, such as breast cancer, includes an enantiomerically stable R-NSAID or a pharmaceutically acceptable salt thereof...
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5965571 |
Cholinesterase inhibitors for treatment of Parkinson's disease
Parkinson's disease can be treated with an at least one cholinesterase inhibitor. The cholinesterase inhibitor has been found to alleviate both any symptoms of dementia as well as to reduce...
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5962501 |
Enantiomer of carbazole derivative as 5-HT1-like agonists
A (+) or (-) enantiomer of a compound of formula (I) wherein R 4 is methyl or ethyl, or a salt, solvate, or hydtrate thereof, processes for preparing said compounds and pharmaceutical compostions...
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5955491 |
Method for treating osteoporosis
The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R 1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which...
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5955469 |
Pharmaceutical composition
A pharmaceutical emulsion composition or solution composition in an organic solvent containing a compound represented by the following chemical formula and having immunosuppressive activity is...
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5942547 |
2-Deoxystreptamine derivatives, pharmaceutical compositions thereof and therapeutic methods using same
This invention provides a compound having the formula: ##STR1## wherein R 1 and R 3 independently are hydrogen, --CHO, --COCH 3 , --COR 7 , --A--Ar--(Q) z , etc.; wherein D is a C 1 -6 linear, C...
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5942532 |
2-substituted phenyl-benzimidazole antibacterial agents
The invention relates to benzimidazole antibacterial compounds of the Formula I: ##STR1## as described herein, pharmaceutical compositions containing the compounds, and methods for their production...
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5919802 |
Methods of preventing and/or treating temporal lobe epilepsy
A method of preventing and/or treating epileptic seizures in a mammal in need of such treatment, which comprises administration to said mammal of a therapeutic amount of a 5HT1A antagonist.
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5877184 |
Macrolides having immunosuppressive activity
Macrolides of the general structural Formula I: ##STR1## are immunosuppressants useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of...
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5877199 |
Heterocyclic compounds, their preparation and their therapeutic use
A compound of formula (I): ##STR1## wherein Y 1 , Y 2 , Y 3 and Y 4 are each hydrogen, halogen, nitro, cyano, hydroxyl, thiol, amino, alkyl, haloalkyl, alkylthio, a protected or unprotected...
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5866598 |
Medicament for treating or preventing cerebrovascular dementia
Compounds for treating or preventing cerebrovascular diseases are disclosed. These compounds are 5-HT antagonists. More specifically, these compounds, when combined with pharmaceutically acceptable...
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5861425 |
Indole-ethanamines
The present invention provides 3-ethanamine and 3-ethanamine related compounds which are useful intermediates and have beneficial central nervous system activity.
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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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5854275 |
Cyclic imide derivatives
The invention relates to a compound of the formula I ##STR1## wherein R 1 is a cyclic imide group and X, Y, R 2 , and R 3 are as defined herein. The invention further relates to pharmaceutical...
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5854274 |
Tricyclic heterocyclic sulfonamide and sulfonic ester derivatives
Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have excellent antitumor activity and are represented by the following general formula (I) and processes...
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5849781 |
Tricyclic amides
The invention relates to a compound selected from these of formula (I): ##STR1## in which R 7 , R 8 , Y, n and A are as defined in the description, and medicinal product containing the same useful...
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5843937 |
DNA-binding indole derivatives, their prodrugs and immunoconjugates as anticancer agents
The present invention relates to novel DNA alkylating agents and the prodrugs of these agents which are useful as antitumor agents and DNA labelling agents. The compounds are hydroxy...
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5834481 |
Heterotricyclically substituted phenyl-cyclohexane-carboxylic acid derivatives
Heterotricyclically substituted phenyl-cyclohexanecarboxylic acid derivatives are prepared by reacting the heterocyclic compounds with cyclohexanecarboxylic acid derivatives which are substituted...
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5830911 |
Pyranoindole and tetrahydrocarbazole inhibitors of COX-2
This invention provides compounds of formula I having the structure ##STR1## wherein R is (CH 2 ) n COOR 4 ; R 1 is hydrogen, alkyl, alkenyl, alkynyl, alkylcycloalkyl, and alkoxyalkyl; R 4...
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5830910 |
Cytochalasins useful in providing protection against nerve cell injury associated with neurodegenerative disorders
The present invention relates to novel therapeutic uses of certain compounds to protect nerve cells from injury and death. The compounds include cytochalasin D and related analogs, and cytochalasin...
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5827871 |
Medicaments 1,2,3,4-tetrahydrocarbazoles and 5-HT.sub.1 agonist use thereof
Use of a compound of general formula (I): ##STR1## wherein R 1 represents hydrogen, halogen, trifluoromethyl, nitro, hydroxy, C 1 -6 alkyl, C 1 -6 alkoxy, arylC 1 -6 alkoxy, --CO 2 R 4 , --(CH 2...
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5824699 |
Carbazole inhibitors of Cox-2
This invention provides compounds of formula I having the structure ##STR1## wherein R 1 , R 2 , R 3 and R 4 are, each, independently, hydrogen, alkyl, alkenyl, alkynyl, alkoxy, aralkoxy,...
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5817689 |
Indole derivatives having a 2-phenyl-ethanolamino-substituted lower alkyl group at the 2-or 3-position thereof
An indole derivative of the formula: ##STR1## wherein R 1 is lower alkoxy, lower alkoxycarbonyl-lower alkoxy, carboxy-lower alkoxy, lower alkoxycarbonyl, phenyl-lower alkoxy, lower alkyl being...
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5814653 |
Pharmaceutical method using 6-substituted-1, 2, 3, 4-tetrahydro-9H-carbazoles and 7-substituted-10H -cyclohepta (7, 6-B) indoles
This invention provides novel 6-substituted-1,2,3,4-tetrahydro-9H-carbazoles and 7-substituted-10H-cyclohepta 7,6-b!indoles. These compounds are 5-HT 1F agonists which are useful for the treatment...
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5814633 |
Iminooxymethylene anilides, process for preparing the same and their use
Iminooxymephyleneanilides of the formula I ##STR1## where the index and the substituents have the following meanings: n is 0, 1, 2, 3 or 4; R is nitro, cyano, halogen, unsubst. or subst. alkyl,...
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5807883 |
2-oxoindoline derivative
Disclosed is a 2-oxoindoline derivative represented by the formula (I): ##STR1## wherein Ring A represents a benzene ring which is substituted in the 5-position or 6-position by a lower alkyl group...
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5801023 |
Antiparasitic pyrrolobenzoxazine compounds
This invention provides compounds of the following chemical formula or their pharmaceutically-acceptable salts: ##STR1## wherein R is hydrogen or chloro. Also, the present invention provides a...
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5801174 |
Fused indole and quinoxaline derivatives, their preparation and use
The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R 1 is hydrogen, alkyl or benzyl; X is O or NOR 2 ,...
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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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5786377 |
Pyrrolo 3,2-E!indol derivatives, process for the preparation thereof and applications
The pyrrolo 3,2-e! derivatives of the present invention have the formulae (I), (Ia) and (II) wherein R is substituted or unsubstituted aryl or heteroaryl, R' is substituted or unsubstituted...
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5780493 |
AMPA antagonists and method of treatment therewith
The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R 1 is hydrogen, alkyl or benzyl; X is O or NOR 2 , wherein R 2 is...
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5776962 |
Lactone compounds for treating patient with precancerous lesions
Substituted lactone compounds are useful in the treatment of precancerous lesions and neoplasms.
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5776963 |
3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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5776891 |
Compositions for reducing multidrug resistance
The present invention comprises methods and compositions for reducing or eliminating multidrug resistance in cancers or certain infections by drug resistant microorganisms in patients. According to...
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5776967 |
Pyranoindole inhibitors of COX--2
This invention provides compounds of formula I having the structure ##STR1## wherein R 1 , R 2 , R 3 and R 4 are, each, independently, hydrogen, alkyl, alkenyl, alkynyl, alkoxy, aralkoxy,...
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5773434 |
Facilitation of AMPA receptor-mediated synaptic transmission in brain as a treatment for schizophrenia
Psychotic symptoms are treated by the administration of drugs which amplify the ability of natural stimulators of AMPA receptors to enhance the mediation of excitatory synaptic response. What is...
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5756532 |
Aminomethyl-2 3 8 9-tetrahydro-7H-1 4-dioxino 2 3-E!-indol-8-ones and derivatives
The compounds of formula I: ##STR1## wherein R 1 and R 2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R 1 and R 2 , taken together, are benzylidene optionally substituted with R 3 ...
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5753690 |
N-substituted azobicycloheptane derivatives, the preparation and use thereof
A compound of the formula ##STR1## in which A, R 1 and n have the meanings stated in the description are described. The novel compounds are suitable for controlling diseases.
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5750556 |
2-(aminomethyl)-3,4,7,9-tetrahydro-2H-pyrano- 2,3-E!indol-8-ones and derivatives
Compounds of Formula I are selective autoreceptor agonists useful in treating disease states involving hyperactivity of dopamine systems: ##STR1## in which X is --(CH 2 ) n --; n is 1-3; R 1 is...
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5741814 |
Cyclooctadiene derivatives
Cyclooctadiene derivative of the following formula (1): ##STR1## wherein A 1 , A 2 , A 3 and A 4 each independently represent COOR 5 (where R 5 represents a hydrogen atom, a C 1 -C 10 alkyl...
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5731320 |
Macrocyclic amide and urea immunomodulators
Immunomodulatory macrocyclic compounds having the formula: ##STR1## and pharmaceutically-acceptable salts, esters, amides and prodrugs thereof, as well as pharmaceutical compositions containing the...
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5721244 |
Combination of angiotensin-converting enzyme inhibitors with calcium antagonists as well as their use in drugs
The invention relates to combinations of angiotensin-converting enzyme inhibitors with calcium antagonists, processes for their preparation and their use as medicaments.
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5721245 |
4- 3-indolyl!-1H-pyrrolone
A compound of the formula ##STR1## wherein R is hydrogen or hydroxy, R 1 and R 2 taken together are a group of the formula --(CH 2 ) m -- and R 7 is hydrogen or R 1 and R 7 taken together are...
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5712151 |
Antifungal agent
There is disclosed a novel compound having the formula ##STR1## which exhibits antifungal activity.
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5705509 |
Tricyclic heterocyclic compounds as 5-HT.sub.4 receptor antagonists
Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X 1 --(CH 2 ) x --X 2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X 1 ...
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5705498 |
Piperidine derivatives as 5-HT.sub.4 receptor antagonists
Compounds of formula (I): ##STR1## wherein X g is O, S, SO, SO 2 , CH 2 , CH, N or NR wherein R is hydrogen or C 1 -6 alkyl; A is a saturated or unsaturated polymethylene chain of 2-4 carbon...
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5703112 |
Method of preventing emesis using tetrahydrobenz CD!indole-6-carbonxamides
The present invention provides methods of preventing emesis and treating sexual dysfunction in mammals utilizing certain tetrahydrobenz cd!indoles. The invention further provides pharmaceutical...
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5698571 |
5-HT.sub.1F mediated inhibition of neurogenic meningeal extravasation: a method for the treatment of migraine
The present invention provides a method for the treatment of migraine with compounds or compositions that are selective agonists of 5-HT 1F receptors relative to other serotonin receptors that...
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5696130 |
Tricyclic steroid receptor modulator compounds and methods
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds,...
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