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7419969 |
HIV integrase inhibitors: cyclic pyrimidinone compounds
The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating...
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7407949 |
Benzamide derivatives as oxytocin agonists and vasopressin antagonists
Novel compounds according to general formula 1, wherein G 1 is NR 5 R 6 or a fused polycyclic group that are specific OT receptor agonists and/or V 1a receptor antagonists. Pharmaceutical...
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7320973 |
Dihydrodiaryloxazepine derivative and pharmaceutical composition containing the same
The present invention provides dihydrodiaryloxazepine derivative represented by the following formula [1], analogs thereof and pharmaceutical compositions containing them. Those compounds have an...
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7148214 |
Antihistaminic spiro compounds
This invention concerns the compounds of formula
or a prodrug, a N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof wherein R 1 , R 2 , —A—B—, L,...
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7119088 |
Triazole compounds useful in therapy
A compound of formula (I),
or a pharmaceutically acceptable derivative thereof, wherein A, B, V, W, X, Y, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.
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7087595 |
Antihistaminic spiro compounds
This invention concerns the compounds of formula
or a prodrug, a N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof wherein R 1 , R 2 , -A-B—, L, and n...
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7041661 |
Use of thiazolobenzoheterocycles for treating multiple sclerosis
The invention relates to the use of compound of Formula I in treating patients for inflammatory or neuropathic pain as well as various symptoms of multiple sclerosis
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6806267 |
Apoptosis-inducing compounds
The present invention relates to pyrrolobenzoxazepines, pyrrolobenzthiazepines and related compounds having the ability to induce apoptosis, to pharmaceutical compositions comprising these...
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6794391 |
Derivatives of pyrimido&lsqb 6.1-a&rsqb isoquinolin-4-one
The invention provides compounds or salts thereof of the general formula (I): wherein each of R 1 and R 2 independently represents a C 1-6 alkyl or C 2-7 acyl group; X represents OCH 2 or a...
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6649614 |
Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent for treatment of depression or anxiety
The present invention relates to the treatment of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and an antidepressant or...
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6512004 |
Promoters of neural regeneration
The invention provides methods and compositions for promoting neural cell growth and/or regeneration. The general methods involve contacting with an activator of a cyclic nucleotide dependent...
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6468971 |
Maintaining kidney function during surgery or trauma
Kappa-opioid agonists prevent the impairment of renal function otherwise caused by the combination of gaseous anesthesia and surgery or severe trauma. Not only do these agents preserve renal...
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6444664 |
Method for controlling the plasma level of lipoproteins to treat alzheimeris disease
A compound which is an antagonist of platelet activating factor (PAF-antagonist) or a structurally related compound thereof not having PAF-antagonistic activity can be used for decreasing the...
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6391870 |
Pyrrolo &lsqb 2,1-b&rsqb &lsqb 1,3&rsqb benzothiazepines with atypical antipsychotic activity
Polycondensated heterocycles with a pyrrole[2,1-b][1,3]benzothiazepine structure of the following formula (I) where the groups are defined as in the description are disclosed. As compared to...
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6191126 |
Topical use of κ opioid agonists to treat ocular pain
The present invention relates to the pharmaceutical treatment of pain. In particular, the present invention relates to the topical use of kappa opioid receptor agonists and partial agonists for the...
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6174878 |
Topical use of kappa opioid agonists to treat otic pain
Compositions and methods for treating otic pain are disclosed. In particular, the invention discloses compositions and methods of using kappa opioid agonists locally for the prevention or...
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6127362 |
9,10-diazatricyclo[4,4,1,1.sup.2,5 ] decane and 2,7-diazatricyclo [4,4,0,0.sup.3,8 ] decane derivatives having analgesic activity
9,10-DIAZATRICYCLO[4,4,1,1 2 ,5 ]DECANE (la) AND 2,7-DIAZATRICYCLO[4,4,0,0 3 ,8 ]DECANE (1b) DERIVATIVES HAVING ANALGESIC ACTIVITY. ##STR1##
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6114329 |
5-HT.sub.4 receptor antagonists useful in the treatment of gastroinstestinal, cardiovascular and CNS disorders
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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5834459 |
Alkyl-substituted compounds having dopamine receptor affinity
Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, unsaturated 5- or 6-membered, homo- or...
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5753649 |
Therapeutic agent for osteoporosis and diazepine compound
A therapeutic agent for osteoporosis, comprising an azepine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof as...
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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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5536715 |
Combinations of anthelmintically active agents
Pharmaceutical compositions comprising a compound of formula (I) and at least one other anthelmintically active compound, being an avermectin or a milbemycin, are useful in the treatment of...
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5104868 |
Tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and esters
This invention relates to novel tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and certain esters and cation salts thereof. The compounds of this...
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4918069 |
Spiro[(piperidine- pyrrolidine- or hexahydroazepinyl substituted) pyrrolo[2,][1,4]benzoxazepines]
This invention relates to spiro-[(piperidine-, pyrrolidine-, or -hexahydroazepinyl substituted) pyrrolo[2,1-c][1,4]-benzoxazepines] having the following formula ##STR1## wherein R is hydrogen,...
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4865764 |
5-aryl-11-substituted-5H,11H-pyrrolo[2,1-][1,4]benzoxazepines as hypotensive agents
There are disclosed compounds of the formula, ##STR1## where X and Y are each independently hydrogen, loweralkyl, halogen or trifluoromethyl; Z is hydrogen or 2- or 3-Cl, Br, I, CHO or CHCR 1 R...
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4814344 |
Indole derivatives
The invention relates to compounds of formula (I) ##STR1## wherein R 1 represents a hydrogen atom or a group selected from C 1 -10 alkyl, C 3 -6 alkenyl, C 3 -10 alkynyl, C 3 -7 cycloalkyl, C 3 -7...
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4794110 |
5-Aryl-11-substituted-5H,11H-pyrrolo[2,1-c][1,4]benzoxazepined as analgesic and hypotensive agents
There are disclosed compounds of the formula, ##STR1## where X and Y are each independently hydrogen, loweralkyl, halogen or trifluoromethyl; Z is hydrogen or 2- or 3-Cl, Br, I, CHO or CHCR 1 R...
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4758559 |
Pyrrolo[1,2-a] [4,1]benzoxazepine derivatives useful as calmodulin and histamine inhibitors
Disclosed are the compounds of the formula ##STR1## wherein n represents the integer 1,2,3 or 4; R 1 represents hydrogen, lower alkyl, halogen, trifluoromethyl, hydroxy or lower alkoxy; R 2 ...
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4681879 |
11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines as antipsychotic and analgesic agents
There are described novel 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines of the general formula ##STR1## where m and n are each independently 0, 1 or 2 and m+n is 1 or 2, X and Y are each...
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4659734 |
Olinecarboxylic acid derivatives
A compound of the formula ##STR1## R 1 is hydrogen, alkali metal, alkaline earth metal, lower alkyl, pivaloyloxymethyl or phthalidyl; R 2 , R 3 , R 4 and R 5 are the same or different and are...
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4532248 |
Method of combatting coronary and vascular diseases
1,4-Dihydropyridines of the formula ##STR1## in which n is 0,1 or 2, and R 1 to R 7 can have a wide variety of meanings, which possess inotropic action, and many of which are new, are useful...
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4426381 |
Carboxylic acid derivatives
Quinolinecarboxylic acid derivatives, such as compound 7-fluoro-8-(4-methyl-1-piperazinyl)-5-oxo-1,2-dihydro-5H-thi
azolo(3,2-a)-q uinoline-4-carboxylic acid, a pharmaceutical composition...
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4322417 |
Antihypertensive polyfluoroisopropyl tricyclic carbostyrils
Polyfluorohydroxyisopropyl tricyclic carbostyrils, such as 2,3-dihydro-7-methyl-9-[2,2,2-trifluoro-1-hydroxy-1-(trifluo
romethyl)ethyl ]-5H-[1,4]thiazino[2,3,4-ij]-quinolin-5-one, useful as...
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4053599 |
Piperazionalkylpyrrolobenzoxazalkanes
Novel piperazinoalkylpyrrolobenzoxazalkanes, physiologically tolerable acid addition salts thereof and a method of preparing same are described. These compounds are useful as antihypertensive agents.
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