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6677353 |
Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer...
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6677341 |
(R)-Chiral halogenated substituted heteroaryl benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma...
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6673829 |
Aminoazetidine,-pyrrolidine and -piperidine derivatives
Novel aminoazetidine, -pyrrolidine, and -piperidine derivatives, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of...
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6673940 |
Compositions and methods relating to cyclic compounds that undergo nucleotide base pair-specific interactions with double-stranded nucleic acids
The design, synthesis, and use of cyclic compounds, including cyclic polyamides, is described. Such compounds comprise at least two polymer portions, one of which comprises at least three molecular...
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6664248 |
2-nitromethylidene/2-cyanimino/2-nitro-imino-pyrrolidines and piperidines, intermediates, and their use as pesticides
Compounds of formula wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a...
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6660732 |
Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are...
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6656933 |
Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are...
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6656952 |
Cis-substituted fluoromethylpyrrolidine derivative
An antibacterial drug having potent antibacterial activities upon various bacteria including resistant strains and high safety is disclosed, which comprises as an active ingredient, quinolone...
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6649642 |
Succinate derivative compounds useful as cysteine protease inhibitors
Disclosed are novel succinate derivative compounds of the formula(I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine...
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6635621 |
Cysteine protease inhibitors
This invention relates to derivatives of alpha-amino acid amides, to pharmaceutical compositions containing such compounds, and to their use in medicine as inhibitors of cysteine proteases,...
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6620839 |
1,3-disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications
Compounds of formula I are useful in treating diseases or conditions prevented by or ameliorated with histamine-3 receptor ligands. Also disclosed are histamine-3 receptor ligand compositions...
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6586433 |
Substituted N-heteroaryl-N-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer...
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6555541 |
Substituted phenyl compounds with immunosuppressing activity and pharmaceutical compositions
The invention provides substituted phenyl compounds of general formula wherein R 1 , T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions...
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6545162 |
Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from...
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6544992 |
Urotensin-II receptor antagonists
The present invention relates to pyrrolyl and pyridyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of urotensin II.
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6531594 |
Process for producing 1H-3-aminopyrrolidine and derivatives thereof
A process for producing 1H-3-aminopyrrolidine and derivatives thereof is disclosed. The process is especially useful for producing optically active 1H-3-aminopyrrolidine and derivatives thereof and...
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6506906 |
Preparation and use of bifunctional molecules having DNA sequence binding specificity
Small molecule polyamides that specifically bind with subnanomolar affinity to any predetermined sequence in the human genome with potential use in molecular biology and human medicine are...
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6476054 |
Cyclic amine modulators of chemokine receptor activity
The present invention is directed to cyclic amines of the formula I: (wherein R 1 , R 2 , R 3 , m and n are defined herein) which are useful as modulators of chemokine receptor activity. In...
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6472389 |
Pyrrolo&lsqb 1,2-b&rsqb pyridazine derivatives having sPLA2 inhibitory effect
The present invention provides a compound having sPLA 2 inhibiting activity. The compound represented by the formula (I): wherein R 1 is —(L 1 )—R 6 wherein L 1 is a divalent linking...
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6468998 |
Pyrrolidine compounds and medicinal utilization thereof
The present invention provides a pyrrolidine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof and a pharmaceutically...
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6451842 |
Cyclic amine derivatives and their use as drugs
A compound represented by the general formula (I), a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C 1 -C 6 alkyl addition salt thereof, and their medical...
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6423689 |
Peptidyl calcium channel blockers
The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat...
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6423843 |
Enantiomerically pure substituted oxaaza compounds, salts of the same, and processes for the preparation of both
This invention provides a method for conveniently obtaining a compound of formula (Ia) which is a production intermediate of antimicrobial compounds, in which a salt of optically active acid of...
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6417372 |
Stable arylpyrrole particles, process for their preparation and suspension concentrate compositions comprising them
The present invention relates to arylpyrrole particles which are prepared by a process in which the particles are aged and milled, and pesticidal suspension concentrate compositions comprising...
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6399824 |
Substituted cinnamic, acid guanidides, process for their preparation, their use as a medicament, and medicament comprising them
Substituted cinnamic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I which may be obtained by...
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6387949 |
Substituted urea compounds useful in pain management
Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel...
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6380241 |
Treatment of diseases using endothelin antagonists
A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing...
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6369077 |
Protease inhibitors
This invention relates to compounds of formula (I): wherein: Y is Ar or NR 1 R 2 ; R 1 is R″, R″C(O), R″C(S), R″SO 2 , R″OC(O), R″R′NC(O), or R″R′NC(S); R 2 is H, C 1-6...
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6342609 |
Process for preparing 3-(7-amidino-2-naphthyl)-2-phenylpropionic acid derivatives
A process for industrially preparing intermediates of aromatic amidine derivatives having anticoagulant activity, i.e., compounds represented by formula (3) or salts thereof, by the following...
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6323229 |
N-acyl and N-aroyl aralkylamides
A compound of the formula ##STR1## wherein m, R 1 , R 2 , R 3 , R 4 , R 5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT 1 ...
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6316467 |
Elevation of HDL cholesterol by 4-[(Aminothioxomethyl)-hydrazono]-N-(substituted)-4-arylbutanamides
Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the "good" cholesterol and as such may be useful for treating diseases such as atherosclerosis. These...
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6258822 |
Urokinase inhibitors
Compounds having the formula ##STR1## are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions...
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6251919 |
Heterocyclic substituted aniline calcium channel blockers
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6201133 |
Certain cyclic thio substituted acylaminoacid amide derivatives
Disclosed are compound of formula I ##STR1## wherein R represents hydrogen, lower alkyl, cycloalkyl, bicycloalkyl, adamantyl, aryl, biaryl, or mono- or di-(cycloalkyl, aryl or biaryl)-lower...
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6177408 |
Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents
A compound which is a distamycin derivative of formula (I), wherein n is 2, 3 or 4; R 0 is C 1 -C 4 alkyl or C 1 -C 3 haloalkyl; R 1 and R 2 , which may be the same or different, are each...
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6156784 |
Compounds useful as phosphotyrosine mimics
Disclosed are compositions containing compounds of the formula (I) below wherein A,B,C,G,Q and R are defined herein. The compounds are useful as phosphotyrosine mimics that, when incorporated into...
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6096766 |
3-benzylaminopiperidines as tachykinin receptor antagonists
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6057342 |
Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof
The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof,...
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6034093 |
Substituted sulfonic acid N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds
The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain...
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6011161 |
Process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(perfluoro-alkylmethyl)arylimidoyl chloride compounds
There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(perfluoroalkylmethyl)arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole...
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5989440 |
Method of using oxygen scavenger and removing oxygen from water
An oxygen scavenger characterized in that the effective component thereof consists of a heterocyclic compound with N--N bond in a ring thereof An oxygen scavenger characterized in that the...
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5981764 |
Process for producing 1-aminopyrrolidine, and 1-aminopyrrolidine according to the process
1-Aminopyrrolidine which is obtained by reacting hydrazine hydrate with a compound represented by the following formula (I): X 1 --C 4 H 8 --X 2 (I) wherein X 1 and X...
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5977360 |
Process for producing cyclic hydrazine derivatives, tetra-hydropyridazine and hexahydropyridazine
The present invention relates to a process for producing alicyclic hydrazine derivatives, tetrahydropyridazine and hexahydropyridazine which are useful as intermediate starting materials such as...
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5977381 |
Process for making 3-amino-pyrolidine derivatives
The invention is concerned with a process for making a compound of formula ##STR1## wherein R 1 is hydrogen, alkyl, cyclo-alkyl, alkenyl, aryl or an amino protecting group; and R 2 , R 3 each...
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5968963 |
PLA.sub.2 inhibitors and their use for inhibition of intestinal cholesterol absorption
Certain compounds have been synthesized and found to be effective inhibitors of phospholipase A 2 (PLA 2 ), and thereby useful in the treatment of intestinal cholesterol absorption and the disease...
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5958918 |
Substituted (sulfinic acid, sulfonic acid, sulfonylamino or sulfinylamino) N- (aminominomethyl)phenylalkyl!-azaheterocyclylamide compounds
The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain...
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5952363 |
Pyrrolidine compounds useful in the treatment of diabetes
The present invention relates to novel pyrrolidine compounds having the general formula I ##STR1## and pharmaceutically acceptable acid addition salts or hydrates or prodrugs thereof, wherein R 1 ...
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5935585 |
Biaromatic amido compounds and pharmaceutical/cosmetic compositions comprised thereof
Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e):...
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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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5885990 |
Substituted amidinonaphthyl ester derivative
Substituted amidinonaphthyl ester compounds effective for treatment of thrombosis are represented by the following formula (I) and pharmaceutically acceptable acid addition salts thereof: ##STR1##...
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