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7297711 |
Arylalkyl indoles having serotonin receptor affinity useful as therapeutic agents, process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel tetracyclic arylalkyl indoles, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically...
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7153848 |
Inhibitors of HCV replication
Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions...
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7144883 |
Bicyclic sulfonamide compounds
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful...
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7141568 |
Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
Pyrrolo[3,4-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions...
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7074782 |
Carbamate caspase inhibitors and uses thereof
This invention provides caspase inhibitors of formula I:
wherein Z is oxygen or sulfur; R 1 is hydrogen, —CHN 2 , R, CH 2 OR, CH 2 SR, or —CH 2 Y; Y is an electronegative leaving group; R 2...
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6998403 |
Benzoindoline compounds
A compound of formula (I):
wherein: R 1 and R 2 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amino, alkylamino, dialkylamino...
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6916812 |
Alpha-aminoamide derivatives as melanocortin agonists
Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the...
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6914064 |
1,4-Disubstituted piperazine derivatives useful as uro-selective α1-adrenoceptor blockers
The present invention relates to a novel 1,4-disubstituted piperazine derivatives of Formula I,
and their pharmaceutically acceptable acid addition salts having excellent uro-selective α 1...
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6890921 |
Arylsubstituted piperazines useful in the treatment of benign prostatic hyperplasia
This invention relates to a series of arylsubstituted piperazines, of Formula I
pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the...
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6861432 |
Piperazine derivatives that destabilize androgen receptors
This invention relates to new piperazine derivatives of general formula I,
in which V, W, n, R, R′, i, j, Y and Z have the meaning that is indicated in the description.
The compounds...
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6849631 |
Semicarbazides and their uses
The present invention relates to the synthesis of a new class of indeno [1,2-c]pyrazol-4-ones of formula (I):
that are potent inhibitors of the class of enzymes known as cyclin dependent...
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6841552 |
3a,4,5,9b-tetrahydro-1H-benz[e]indol-2-yl amine-derived neuropeptide Y receptors ligands useful in the treatment of obesity and other disorders
Compounds of the formula:
are disclosed as ligands for neuropeptide Y receptors and as such are useful in the treatment of obesity and disorders of the central nervous system.
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6812230 |
Non-peptide CCR1 receptor antagonists for the treatment of progressive renal fibrosis
This invention is directed to pharmaceutical compositions useful in treating progressive renal fibrosis in mammals comprising a pharmaceutically acceptable excipient and a therapeutically effective...
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6740636 |
Non-peptide CCR1 receptor antagonists in combination with cyclosporin A for the treatment of heart transplant rejection
This invention is directed to pharmaceutical compositions useful in treating heart transplant rejection in mammals comprising a pharmaceutically acceptable excipient, a therapeutically effective...
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6713473 |
Tricyclic compounds
A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents —NR 3 —CO—, —CO—NR 3 — and the like (R 3 represents a hydrogen atom, a...
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6689784 |
Carbamate caspase inhibitors and uses thereof
This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R 1 is hydrogen, —CHN 2 , R, CH 2 OR, CH 2 SR, or —CH 2 Y; Y is an electronegative leaving group; R 2...
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6664258 |
Spirocyclic dopamine receptor subtype ligands
This invention relates to novel, pharmaceutically active compounds of formula (I) wherein a, b and R 1 through R 6 are as defined in the specification These compounds exhibit central...
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6498251 |
Tetrahydrobenzindole derivatives
Compounds containing tetrahydrobenzindole which bind to serotonin receptor and are useful in treatment or prevention of disease induced by abnormality of central peripheral serotonin controlling...
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6407112 |
Optically active tetrahydrobenzindole derivative
Optically active tetrahydrobenzindole type compounds having affinity for a 5-HT receptor, useful for prevention and treatment of mental diseases. A species compound is...
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6365584 |
Arylysulphonamide-substituted benzimidazoles having tryptase-inhibiting activity
Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are:...
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6355644 |
Benzylpiperazinyl-indolinylethanones
Disclosed are benzylpiperazinyl-indolinylethanone compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania,...
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6355642 |
Tetrahydrobenzindole compounds
A compound of formula (I) for use in the treatment or prevention of mental diseases A is N, CH, C having a double bond or CR 5 ; each of B and Z is independently N, CH or CR 1 , with the proviso...
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6340682 |
Diamide compound and drugs containing the same
The present invention provides diamide derivatives represented by the following general formula (1): wherein A is a phenyl group or the like, which may be substituted, B is —CH═CH—,...
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6306876 |
4-[aryl(8-azabicyclo[3.2.1]octan-3-yl)]aminobenzoic acid derivatives
4-[aryl(8-azabicyclo[3.2.1]octan-3yl)]aminobenzoic acid derivatives are delta-opioid receptor modulators. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on...
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6150129 |
Antimicrobial determination of N-(aminoalkyl) and/or N-(Amidoalkyl) dinitrogen heterocyclic compositions
Compositions are provided comprising novel di-nitrogen heterocycle compounds containing N-(aminoalkyl) and/or N-(amidoalkyl) groups. An additional situs of functionality is also provided. The...
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6087364 |
Dopamine D4 receptor antagonists
Compounds that are antagonists of dopamine D4 receptors, methods of treating psychosis and schizophrenia using the compounds, and pharmaceutically acceptable compositions that contain the dopamine...
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6080745 |
Fused tricyclic heteroaromatic derivatives as dopamine receptor subtype ligands
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6051575 |
Piperazino derivatives as neurokinin antagonists
The invention relates to compounds of the formula ##STR1## wherein Z, R c , y, m, u, Ar 2 , n, X, R c ', I and Ar 2 are as described herein. These compounds are neurokinin antagonists. These...
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6040331 |
Nerve cell protective agents
The invention provides novel benzindole derivatives, processes for producing them, as well as a neuroprotective agent, an agent to prevent or treat diseases involving the degeneration, retraction...
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6030992 |
Methods of treating or preventing sleep apnea
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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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5902812 |
Pharmaceutical piperazine compounds
Diketopiperazines of formula (A): ##STR1## wherein each of R 1 to R 8 is H or an organic radical as described herein and the pharmaceutically acceptable salts thereof have activity as inhibitors...
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5874435 |
4-heteroaryl-1-piperazinealkanols 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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5869490 |
Azaheterocyclymethyl derivatives of 2,3,8,9-tetrahydro-7h-1,4-dioxino (2,3-e) indol-8-one
The compounds of formula I: ##STR1## wherein X is H 2 or O; R 1 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or...
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5856323 |
Compounds and methods for the treatment of disorders mediated by platelet activating factor or products of 5-lipoxygenase
2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl...
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5852018 |
Pharmaceutical piperazine compounds
Piperazine derivatives of formula (A): ##STR1## wherein - ------- denotes an optional bond, provided that either - --- a - --- and - --- c - --- are both bonds and - --- b - --- and - --- d -...
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5840725 |
Substituted oximes, hydrazones and olefins as neurokinin antagonists
Compound represented by the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or3; b, d and e are independently 0, 1 or 2; R is H, C 1 -6 alkyl,...
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5817684 |
Leukotriene antagonists for use in the treatment or inhibition of cerebral focal stroke
This invention provides methods for the treatment or prevention of cerebral focal ischemia which comprises administering to a mammal in need thereof an effective amount of a compound having...
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5801176 |
Substituted benzothienylpiperazines and their use
This invention relates to compounds of the formula ##STR1## wherein X is halogen, hydroxy, (C 1 -C 6 )alkoxy, amino or trifluoromethyl; and Y is --CN or --NR 1 R 2 ; where l is an integer of 0,...
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5795894 |
Piperazino derivatives as neurokinn antagonists
The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
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5783579 |
Spiro-substituted azacyclic-substituted piperazino derivatives as neurokinin antagonists
The invention relates to compounds of the formula ##STR1## wherein Z, R c , y, m, u, Ar 2 , n, X, R c ', I and Ar 2 are as described herein. These compounds are neurokinin antagonists. These...
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5753660 |
Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
Selected sulfonylalkanoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention...
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5731309 |
Substituted heteroalkyleneamine neurokinin antagonists
Compounds of formula I ##STR1## wherein Q 1 , Q 2 , Q 3 , and Q 4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide...
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5703080 |
Method for stabilizing duocarmycin derivatives
Stabilized duocarmycin derivatives represented by formula (I): ##STR1## wherein R is lower alkyl, allyl or benzyl, and X is Cl or Br, are prepared by adding at least a compound selected from the...
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5693643 |
Hydantoin and succinimide-substituted derivatives of spiroindanylcamphorsulfonyl oxytocin antagonists
Compounds of formula (I) wherein X is (a) or (b), R is Het as defined in the description. These compounds are oxytocin and vasopressin antagonists useful in the treatment of preterm labor,...
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5688518 |
Antidepressive therapy
A dosage form is provided for administering a drug of the formula ##STR1## to a patient to produce an anxiolytic benefit in the patient.
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5686466 |
Tricyclic condensed heterocyclic compounds their production and use
A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n...
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5674867 |
Indolocarbazole derivatives and therapeutic method for stimulating megakaicyocyte production
The present invention relates to therapeutic agents for thrombocytopenia which contain an indolocarbazole derivative represented by the formula (I) given below or a pharmaceutically acceptable salt...
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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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5656632 |
1-(N'-(arylalkylaminoalkyl)) aminoisoindoles; dopamine receptor subtype specific ligands
Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently...
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