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7304050 |
Antibacterial agents
Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable...
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7229986 |
Melanin-concentrating hormone antagonist
A melanin-concentrating hormone antagonist comprising a compound of the formula:
wherein R is hydrogen atom or a cyclic group which may be substituted; X is a bond or a spacer having a main...
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7173023 |
Bicyclic compounds
The present invention relates to novel benzazepine derivatives of the following formula:
wherein R 1 , R 2 , R 3 , R 4 and R 5 , X, X′, Y and Y′ are as defined in the description and...
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7122538 |
Sulfonamide derivatives as antipsychotic agents
The invention provides compounds of formula (I):
wherein
A and B represent the groups —(CH 2 ) m — and —(CH 2 ) n — respectively; R 1 represents hydrogen or C 1-6 alkyl; R 2 ...
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7008940 |
Dihydrobenzofuran derivatives, process for the preparing thereof and agents
A compound represented by the formula (I):
or a salt thereof exhibits excellent inhibitory activity of lipid peroxidation and is useful as an agent for inhibiting lipoperoxide production,...
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7008938 |
Benzene-fused heteroring derivatives and pharmaceutical agents comprising the same as active ingredient
A benzene-fused heteroring derivative of formula (I)
wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an...
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6953787 |
5HT2C receptor modulators
The present invention relates to novel compounds of Formula (I):
which act as 5HT 2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the...
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6919329 |
N-Aryl-2-oxazolidinone-5-carboxamides and their derivatives
The present invention provides antibacterial agents having the formulae I, II, and III described herein.
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6916811 |
Adenosine A2a receptor antagonists
Disclosed herein are compounds having the structural formula A
including pharmaceutically acceptable salts or solvates of said compound, wherein X, Y, Q and R are as defined in the...
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6861420 |
N-substituted 1,2,4,5-tetrahydro-1H-benzo[d]azepine compounds
The present invention provides compounds of Formula I:
wherein X, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 have any of the values defined in the specification, as well as pharmaceutical...
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6855708 |
N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors
Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds...
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6818639 |
Pharmaceutical combination formulation and method of treatment with the combination
The invention relates to method of preventing or treating a disease related to the 5-HT 2C receptor and the 5-HT 6 receptor, comprising administering to a human or animal subject in need thereof...
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6664249 |
Bicyclic vasopressin agonists
Compounds according to general formula (1), and pharmaceutically acceptable salts thereof, wherein V is a covalent bond or NH, X is selected from CH 2 , O and N-alkyl, Z is either S or...
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6649606 |
Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity
Tetrahydroisoquinoline analogs are provided which are modulators of chemokine receptor activity. The tetrahdroisoquinoline analogs thereof have the structure wherein R 1 , R 2 , R 3 , R 3a , X 1...
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6586422 |
Pyrazine and triazine derivatives of 1,2,4,5-tetrahydro-Benzo or Thieno &lsqb d&rsqb azepine
The invention relates to compounds which are represented by the formula wherein R 1 , R 2 , R 3 , R 4 , X and Y are as defined in the specification, as well as pharmaceutically acceptable salts...
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6534496 |
Thermogenic composition and benzazepine thermogenics
The object of the present invention is to provide a prophylactic and/or therapeutic drug for obesity and obesity-associated diseasestor diabetes with a reduced risk for central side effects and...
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6472403 |
αV integrin receptor antagonists
The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present...
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6458784 |
Vitronectin receptor antagonists
Pharmaceutically active benzodiazapine compounds of formula (I) are disclosed. These compounds inhibit the vitronectin receptor and are useful for treatment of osteoporosis.
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6362201 |
3-cyclopropyl and 3-cyclobutyl pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of chemokine...
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6358942 |
Phenyloxazolidinones having a c-c bond 4-8 membered heterocyclic rings
A compound of Formula (I): or pharmaceutical acceptable salts thereof wherein X is NR 1 ; R 1 is H, C 1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R 1 is —(CH 2 ) h...
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6218385 |
1,2,4,5-Tetrahydro-benzo[D]azepin derivatives
The present invention is concerned with 1,2,4,5-tetrahydro-benzo[d]azepin derivatives as well as with their pharmaceutically acceptable salts in their racemic and optically active form, which...
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6169093 |
Quinoline and quinazoline compounds useful in therapy, particularly in the treatment of benign prostatic hyperplasia
Compounds of formula I, ##STR1## wherein R 1 represents C 1 -4 alkoxy optionally substituted by one or more fluorine atoms; R 2 represents H or C 1 -6 alkoxy optionally substituted by one...
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6166037 |
Pyrrolidine and piperidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine and piperidine compounds of the formula I: ##STR1## (wherein R 1 , R 2 , R 3 , R 4a , R 4b , R 4c , R 4d , R 4e , R 4f , R 4g , R 4h , m, n, x and y...
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6048854 |
2,3-diaminopropionic acid derivative
The present invention relates to a 2,3-diaminopropionic acid derivative of the formula (1): ##STR1## or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful...
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6022868 |
Substituted azacyclic or azabicyclic compounds
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6004933 |
Cysteine protease inhibitors
The present invention relates to cysteine protease inhibitors of the general formula (I): ##STR1## wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and...
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5914351 |
Anti-viral aromatic hydrazones
Compounds of the formula ##STR1## wherein Q is a hydrazone derivative; R 1 is hydrogen, halogen, alkyl or alkoxy; R 2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl,...
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5861393 |
Antithrombotic amidinophenylalanine and amidinopyridylalanine derivatives
This invention relates to compounds of formula (I), ##STR1## pharmaceutically acceptable salt thereof, and pharmaceutically acceptable solvates of either entity, wherein X is CH or N; Y is...
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5798352 |
Antithrombotic amidinotetrahydropyridylalanine derivatives
This invention is directed to compounds of formula (I), ##STR1## pharmaceutically acceptable salts thereof, and pharmaceutically acceptable solvates of either entity, wherein Y is optionally...
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5741789 |
Compounds having effects on serotonin-related systems
A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1 A receptor. The...
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5663183 |
N-(3-Aminopropyl)-N-phenyl-5,6,7,8-tetrahydronaphthalene-2-carboxamide derivatives, their preparation and their therapeutic use
Compounds of the formula: ##STR1## in which R 1 represents a hydrogen or halogen atom or a methyl or C 1 -C 4 alkoxy group, R' 1 represents a hydrogen or halogen atom, R" 1 represents a...
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5639748 |
6,9-disubstituted benzazepines having α-adrenoceptor blocking activity
Alpha-adrenergic receptor antagonists having the formula: ##STR1## which are useful to produce α-adrenoceptor antagonism, pharmaceutical compositions including these antagonists, and methods of...
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5550162 |
N-(-3-aminopropyl)-N-phenyl-5,6,7,8-tetrahydro-naphthalene-2-carboxamide derivatives, their preparation and their therapeutic use
Compounds of the formula: ##STR1## in which R 1 represents a hydrogen or halogen atom or a methyl or C 1 -C 4 alkoxy group, R' 1 represents a hydrogen or halogen atom, R" 1 represents a...
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5462934 |
Condensed heterocyclic ketone derivatives and their use
A compound of the formula: ##STR1## wherein R 1 is H or an optionally substituted hydrocarbon or acyl group; ring A is an optionally further substituted benzene ring; n is an integer of 1 to 10; R...
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5447928 |
Benzoxazine derivatives and their application in therapy
Compounds of the formula ##STR1## in which Y represents hydrogen, fluorine, chlorine, methyl or methoxy, R 1 represents phenyl substituted by fluorine, methyl, methoxy, trifluoromethyl or phenyl,...
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5444056 |
Aminoalkoxyphenyl derivatives, process for their preparation and compositions containing them
An aminoalkoxyphenyl derivative of general formula: Cy--B--Ph--O--A--Am (1) as well as a pharmaceutically acceptable salt thereof in which B represents a...
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5360799 |
Substituted thienyl- or pyrrolylcarboxyclic acid derivatives, their preparation and medicines containing them
Compounds of formula ##STR1## in which R 1 represents OH, (C 1 -C 12 )alkyl, (C 1 -C 12 )alkoxy, benzyloxy, benzyl, phenyl, (C 1 -C 4 )alkylNZ 1 Z 2 or NZ 1 Z 2 ; R 2 represents OH, SH, (C...
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5310750 |
Heterocyclic compounds useful as α.sub.2 -adrenoceptor antagonists
A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R 1 and R 2 may each represent hydrogen or alkyl providing that at least one of R 1 or R 2 represents...
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5281591 |
Combinations of selective alpha-adrenergic agonists and antagonists useful in lowering intraocular pressure
Methods and pharmaceutical formulations of alpha 2 agonists and alpha 3 antagonists which are useful in lowering intraocular pressure (IOP) and treatment of intraocular hypertension....
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5202319 |
Substituted 3-amino-2,3,4,5-tetrahydro-1-aryloxy-3-benzazepines
There are disclosed various compounds of the formula below, ##STR1## where n is 1 or 2; m is 1 or 2; each X is independently hydrogen or loweralkoxy; Y is hydrogen, halogen or...
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5141933 |
Treatment for hyperglycaemia
A method for the treatment and/or prophylaxis of hyperglycaemia in human or non-human mammals which comprises administering to the mammal in need of such treatment and/or prophylaxis an effective...
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5096900 |
(4-piperidyl)methyl-2,3-dihydro-1H-isoindole and -2,3,4,5-tetrahydro-1H-benzazepine derivatives, their preparation and their application in therapy
A benzazepine derivative which is a compound of formula (I): ##STR1## in which: each of m and n denotes the number 1, or each of m and n denoted the number 2, or m denotes the number 3 and n...
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5079243 |
Benzazepines
Novel 2, 3, 4, 5-tetrahydro-1H-3-benzazepines, which in the 7-position have a methoxymethyloxy group, in the 8-position hydrogen, halogen, or a nitro group and in the 5-position have an optionally...
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5025033 |
Alkylene diamines
A cholinesterase inhibiting agent which contains an alkylene diamine of the formula ##STR1## wherein R 1 and R 2 each independently is a hydrogen atom or a hydrocarbon residue which may...
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5021445 |
Compounds useful for the treatment of hypoglycemia
A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R 1 and R 2 may each represent hydrogen or alkyl providing that at least one of R 1 or R 2 represents...
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5019571 |
1-carbacephalosporin antibiotics
This invention relates to antibacterial compounds of the formula ##STR1## wherein A is hydrogen or an acyl group ##STR2## R a is a negative charge; R z is hydrogen, C 1 -C 4 alkoxy, C 1 -C 4 ...
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5017571 |
Carbamic acid ester of substituted 7-hydroxy-2,3,4,5-tetrahydro-1H-3-benzazepines
Compounds having the formula ##STR1## wherein R 1 , R 4 , R 6 , R 7 , and R 8 are hydrogen or a substituent, R 2 is a substituent, R 5 is an optionally-substituted bicyclic ring system,...
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5015639 |
Substituted benzazepines, their preparation and pharmaceutical compositions containing them
Disclosed herein are novel 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines of the general formula I: ##STR1## wherein R 1 , R 2 , R 3 , R 4 and R 5 are specified substituents. R 1 is...
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4988690 |
1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines and anti-depressant use thereof
The invention relates to 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines of the formula ##STR1## wherein Y is the same or different and is hydrogen and lower alkoxy; X is hydrogen, halogen, lower...
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4977148 |
Amide derivatives
The invention concerns novel phenoxyacetic acid amide derivatives of the formula I (and pharmaceutically acceptable salts thereof) in which R 1 is hydrogen or fluoro, R 2 is phenyl, cycloalkyl,...
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