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5877187 |
Benzimidazole derivatives with antihistaminic activity
New benzimidazole derivatives of formula: ##STR1## in which R 1 is H or a short chain hydrocarbon group such as methyl, hyl, isopropyl, cyclopropyl, vinyl, etc., and R 2 is a group selected from...
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5877182 |
Piperidines promote release of growth hormone
The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R 1 , R 1a , R...
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5869479 |
Treatment of upper airway allergic responses
Relief from the symptoms of rhinitis is obtained by treatment with: (a) an antihistaminic effective amount of a histamine H 1 receptor antagonist; together with (b) a sufficient amount of a...
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5866589 |
Alkyl substituted piperadinyl and piperazinyl anti-AIDS compounds
Anti-AIDS compounds of formula (I) ##STR1## wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are as defined in the specification and R 8 is alkyl of substituted alkyl.
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5863914 |
N,N-di(aryl) cyclic urea derivatives as anti-coagulants
N,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: ##STR1## wherein R 1 is --C(NH)NH 2 , --C(NH)N(H)OR 11 , --C(NH)N(H)C(O)R 9 , or --C(NH)N(H)C(O)OR 11 ; R...
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5863912 |
Method of treatment of hormone-unresponsive metastiatic prostate cancer
Prostate cancer particularly hormone-unresponsive metastatic prostate cancer, is treated by cyclophosphamide or other normally substantially inactive agent. Potentiation of the anti-cancer activity...
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5854263 |
1- (1,4-benzodioxanyl)alkyl!-3-(heteroaryl) pyrrolidines and related compounds and their therapeutic utility
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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5854243 |
3-heteroaryl-1-pyrrolidinealkylthiols and derivatives thereof and their therapeutic utility
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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5849759 |
Naphthyl-substituted benzimidazole derivatives as anti-coagulants
Compounds of formula (I): ##STR1## wherein: n, A, R 1 , R 2 , R 3 , and R 4 have meanings as defined herein, or a pharmaceutically acceptable salt thereof, are useful as anti-coagulants.
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5834499 |
5-HT.sub.3 receptor agonist, novel thiazole derivative and intermediate thereof
A 5-HT 3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or...
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5827499 |
Determining effects of psychoactive compounds on the brain using positron emission tomography
A method of determining the effects of administering a psychoactive compound, such as a drug, on a patient's brain using imaging techniques with position emission tomography (PET) is disclosed. The...
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5821242 |
Anti-viral compounds
The present application provides a series of benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B...
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5817676 |
Indazolecarboxamides
Indazolecarboxamides are used as antagonists and partial agonists for the serotonin receptor 5-HT 4 and provide therapeutic methods for treatment of disorders caused by or affected by dysfunction...
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5814629 |
Microbicides
The invention relates to novel microbicidal and plant-immunising compounds of formula I ##STR1## wherein: X is hydrogen, halogen, C 1 -C 4 alkyl, SR 8 , N(R 9 )R 10 , CH 2 OH, CHO or COOR 8 ; ...
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5811435 |
2- (4-heteroaryl-1-piperidinyl)alkyl!-1,3-dioxanes and related compounds and their therapeutic utility
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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5795893 |
Fibrinogen receptor antagonists
This invention relates to novel compounds which inhibit platelet aggregation, pharmaceutical compositions containing the compounds, and methods of using the compounds.
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5776931 |
Naphthimidazolyl neuropeptide Y receptor antagonists
This invention provides a series of substituted 1H-naphth 2,3-d!imidazoles which are useful in treating a condition associated with an excess of neuropeptide Y. This invention also provides methods...
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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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5773417 |
Human serum albumin-porphyrin complexes with the ability to bind oxygen and therapeutic uses thereof
The invention is directed to human serum albumin-porphyrin (HSA-P) complexes which are capable of reversible oxygen binding and their uses. These complexes may be used in applications requiring...
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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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5767118 |
4-Heterocyclic peperidines promote release of growth hormone
The present invention is directed to certain novel compounds identified as 4-heterocycle substituted piperidines of the general structural formula: ##STR1## wherein R 1 , R 4 , R 5 , A, R 3 and...
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5760054 |
Alpha IC adrenergic receptor antagonists
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1C adrenergic receptor antagonists. One application of these compounds...
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5760018 |
Gem-disubstituted azacyclic tachykinin antagonists
The present invention is directed to certain compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 ,...
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5750542 |
Benzisoxazole and benzisothizole derivatives as cholinesterase inhibitors
Described herein are compounds of the formula ##STR1## wherein R 1 R 2 , R 7 , R 8 , X, Y, M and L are defined as below. The compounds of formula I are cholinesterase inhibitors and are useful in...
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5744460 |
Combination for treatment of proliferative diseases
The invention relates to combinations of PKC-targeted (especially PKC-α-targeted) deoxyribo- and ribo-oligonucleotides and derivatives thereof with other chemotherapeutic compounds, as well as to...
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5741804 |
Substituted benzimazoles which inhibit platelet aggrecation
This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for...
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5741800 |
Azolyl-cyclic amine derivates with immunomodulatory activity
A compound of the formula (I), ##STR1## as defined in the specification, having immunomodulatory activity, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the...
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5726194 |
Endothelin receptor antagonists
Novel compounds of the formula I ##STR1## in which R 1 , R 2 , R 3 , --AB--CD--, Ar and X have the meaning indicated in claim 1, and their salts show endothelin receptor-antagonistic properties.
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5714498 |
Benzimidazole derivatives
The invention is directed to substituted benzimidazole compounds which are ligands for dopamine receptor subtypes used in the treatment of the dopamine system.
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5710169 |
Therapeutic heterocycles
Compounds of formula I ##STR1## wherein Q 1 , Q 2 , Q 3 , Q 4 , and Q 5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are...
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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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5698553 |
Benzylpiperidine derivatives
A benzylpiperidine compound of formula I ##STR1## in which R 1 is H, Hal or nitro, R 2 is a benzyl group, which is unsubstituted or substituted by Hal on the aromatic portion, in the 2-, 3- or...
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5696136 |
Method of treating psychosis using azaheterocyclylmethyl
A method of treating psychosis by administering to a patient an azaheterocyclylmethyl-chroman of the formula: ##STR1## in which E represents an azaheterocyclyl group selected from the group...
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5696137 |
Azaheterocyclymethyl-chromans
Azaheterocyclylmethyl-chromans of the formula: ##STR1## in which E represents an azaheterocyclyl group selected from the group consisting of: ##STR2## wherein R 6 represents hydrogen, hydroxyl,...
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5693652 |
Benzimidazoles for ischemic heart conditions
The present invention provides a nitrogenous heterocyclic compound represented by the following general formula (1) or a pharmacologically acceptable salt thereof which is useful for various...
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5693653 |
Method of treating depression using azaheterocyclylmethyl-chromans
Azaheterocyclylmethyl-chromans are prepared by reaction of corresponding methylchromans with corresponding azaheterocyclic compounds, optionally with subsequent variation of the substituents. The...
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5693661 |
Anti-viral compounds
Certain vinyl acetylene benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups,...
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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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5674879 |
Compositions including and methods of using conformationally restricted angiotensin II antagonist
Conformationally restricted compounds are described which are therapeutically effective as angiotensin II antagonists for the treatment of circulatory disorders.
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5670492 |
DC-89 derivatives
Provided are DC-89 derivatives represented by the formula: ##STR1## wherein X represents Cl or Br, R represents hydrogen or COR 1 , and W represents ##STR2## and pharmaceutically acceptable salts...
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5670522 |
Dopamine receptor subtype ligands
Fused tricyclic heteroaromatic compounds of formula ##STR1## wherein one of X and Y represents nitrogen, and the other of X and Y represents oxygen, sulphur or N--R 2 ; Q represents a...
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5668148 |
Alpha1a adrenergic receptor antagonists
Compounds that specifically bind to the human alpha1a adrenergic receptor, including compounds effective to reduce symptoms of benign prostatic hypertrophy include compounds of formula: ##STR1##...
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5665756 |
Aminoalkyloximes useful in the treatment of depression and obsessive compulsive disorders
Novel aminoalkyloximes of the formula ##STR1## wherein: a. X is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, or a group of the formula ##STR2## wherein Y is hydrogen or loweralkyl,...
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5665732 |
Indazole derivatives
A class of chemical compounds comprising a 1-H-indazole moiety and a substituted heterocyclic moiety, linked via the 3-position of the indazole moiety by a methylene group, are ligands for dopamine...
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5658909 |
Certain substituted 1-aryl-3-piperazin-1'-yl propanones to treat Alzheimer's Disease
Disclosed are compounds of formula I: ##STR1## or the pharmaceutically acceptable salts thereof wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted...
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5658919 |
Aqueous pharmaceutical suspension and process for preparation thereof
The present invention relates to an aqueous pharmaceutical suspension composition containing suspended acetaminophen and at least one additional pharmaceutical active, a suspension system...
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5654306 |
Piperidine derivative and pharmaceutical composition
A piperdine derivative having the formula (I) or a pharmacologically acceptable salt thereof: R 1 --X--A--R 2 (I) wherein R 1 is selected from the group...
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5654319 |
N-[(4-heteroaryl-1-piperidinyl)alkyl]-2,3-naphthalimides and related compounds and their therapeutic utility
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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5654298 |
Amine derivatives
This invention concerns novel aminopyridinium compounds of the formula I wherein R 1 , R 2 , R 3 , R 5 and R 6 are selected from the following combinations: ##STR1## (a) one of R 2 and R 6 is a...
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5652246 |
Piperidine compounds
The invention relates to the compounds of formula (I): ##STR1## in which: R 1 represents alkyl, phenyl, naphthyl, pyridyl or thienyl group, each phenyl, naphthyl, pyridyl or thienyl optionally...
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