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6794507 |
Compounds that inhibit factor Xa activity
The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, hydrate or a pharmaceutically acceptable formulation thereof. Those compounds can be...
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6777425 |
Isoquinoline compounds having antiinfective activity
Isoquinoline compounds having the formula where R 1 , R 2 , Y, m, n, and Z are as defined herein, bind to the minor groove of DNA and have antifungal and antibacterial activity.
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6774086 |
3-Aminocarbonyl-substituted benzoylcyclohexanediones
There are described derivatives of benzoylcyclohexanediones of the formula (I) and their use as herbicides. In this formula (I), R 1a , R 1b , R 1c , R 2 , R 3 , R 4 and R 5 are various...
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6770656 |
Amine derivatives for the treatment of apoptosis
The present invention is related to substituted amine derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such amine derivatives...
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6753317 |
Dmt-Tic di- and tri-peptide derivatives and related compositions and methods of use
A compound of formula: comprising the Dmt-Tic pharmacophore and related compositions and methods of use in the inhibition of the binding of an opioid receptor-binding compound with a...
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6747041 |
Heterocyclic dicarboxylic acid diamide derivatives, agricultural/horticultural insecticides and method of using the same
Heterocyclic dicarboxylic acid diamide derivative represented by the general formula (I): wherein R 1 , R 2 and R 3 represent each H, optionally halogenated C 3-6 cycloalkyl, etc.; Het...
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6747050 |
Isoxazoline derivative and a process for the preparation thereof
The present invention provides to an isoxazoline derivative of formula (I), the pharmaceutically acceptable salts, esters and stereochemically isomeric forms thereof, and the use of the derivative...
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6720427 |
Thiazole derivatives
The invention provides compounds of formula 1 wherein R 1 , R 3 , and R 4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity...
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6710056 |
Amidinophenylpyruvic acid derivatives
An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood...
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6693199 |
Method of making HIV protease inhibitors
A method of making HIV protease inhibitors of general formula (1): These HIV compounds inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV...
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6677354 |
Piperdines for use as orexin receptor antagonists
Disclosed are compounds of formula (I): wherein: Y represents a group (CH 2 ) n , wherein n represents 0, 1 or 2; R 1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3...
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6664393 |
N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
The present invention relates to compounds of the formula I, in which A, L, Y, and k have the meanings indicated in the specification and claims. The compounds of the formula I are valuable...
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6664277 |
Prenylation inhibitors containing dimethylcyclobutane and methods of their synthesis and use
The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical...
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6653321 |
Naphthylsulfonic acids and related compounds as glucose uptake agonists
Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or...
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6642228 |
α1b-adrenergic receptor antagonists
There are provided compounds represented by the general formula (I): [wherein Ar is indole etc., R 1 is hydrogen etc., B is bond, or B—N—R 1 forms a ring structure and is piperidine etc.,...
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6627641 |
Antimalarial naphthylisoquinoline alkaloids and pharmaceutical compositions and medical uses thereof
The present invention provides antimalarial pharmaceutical compositions containing antimalarial naphthylisoquinoline alkaloids or antimalarial derivatives thereof, useful new antimalarial...
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6620947 |
Compounds for use in 11-oxa prostaglandin synthesis
Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.
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6610701 |
Thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R 3 is hydrogen or halogen,...
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6605721 |
Intermediates for making HIV-protease inhibitors and methods for making HIV-protease inhibitors
HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel...
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6602864 |
Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds
The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from...
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6596732 |
1,3-dihydro-2h-indol-2-one, preparation method and pharmaceutical compositions containing same
The invention relates to compounds of formula: and their solvates and/or hydrates exhibiting an affinity and a selectivity for arginine-vasopressin V 1b receptors or for both V 1b and V 1a ...
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6586597 |
Continuous process for the preparation of optically pure decahydroisoquinolinecarboxamide
The present invention relates to a continuous process for the preparation of [3S-(3α, 4 a β, 8 a β)]-N-tert-butyl-decahydro-3-isoquinolinecarboxamide, an intermediate useful in the synthesis of...
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6579886 |
Selective iglur5 receptor antagonists
The present invention provides compounds of formula (I): wherein W represents hydrogen, C 1 -C 4 alkyl, —CH 2 CO 2 H, or CO 2 H; and X represents hydrogen, C 1 -C 4 alkyl, —CH 2 CO 2 H, or CO...
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6562822 |
Heterocyle carboxamides as antiviral agents
The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
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6538006 |
Retroviral protease inhibitors
N-heterocyclic moiety-containing hydroxyethylamine protease inhibitor compounds, methods for making the compounds, and intermediates useful in the method. Also, a method for inhibiting retroviral...
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6534650 |
Benzisoxazole and 4-amidino-3-hydroxyphenyl chemical intermediates
This invention relates to compounds of Formula V H—Y—G—R V and Formula VI (wherein f, X, Y, G and R have the values defined in the description) which are useful as intermediates for the...
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6531478 |
Amino pyrazole derivatives useful for the treatment of obesity and other disorders
Amino pyrazole derivatives of the formula: which are ligands for the neuropeptide Y, subtype 5 receptor and pharmaceutical compositions containing an amino pyrazole derivative as the active...
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6528525 |
Amidocarboxylic acid derivatives
Amidocarboxylic acid derivatives of the formula: wherein R 1 represents a hydrogen atom, etc.; R 2 represents an alkylene group; R 3 represents a hydrogen atom, etc.; R 4 represents a...
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6511990 |
Class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof
The present invention provides the compound having the formula: wherein each of R 1 and R 2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino,...
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6492387 |
Isoindolyl and isoquinolinyl aroyl pyrrole compounds
This invention is directed to isoindolyl and isoquinolinyl aroyl pyrrole compounds pharmaceutically useful as agents or modulators for the treatment of central nervous system disorders and methods...
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6482859 |
Microbicidal N-sulfonylglycin alkynyloxyphenethyl amide derivatives
The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R 1 is...
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6479436 |
Hetaroyl cyclohexanedione derivatives with herbicidal effect
Hetaroyl derivatives of the formula I where: R 1 and R 2 are each hydrogen, nitro, halogen, cyano, thiocyanato, hydroxyl, mercapto, C 1 -C 6 -alkyl, C 1 -C 6 -alkoxy, C 1 -C 6 -alkylthio, C 1...
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6476048 |
Substituted phenanthridinones and methods of use thereof
This invention provides a novel class of substituted 6(5H)phenanthridinone compounds. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable...
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6469041 |
Certain pyrazole derivatives as corticotropin-releasing factor CRF1 ligands
Disclosed are compounds that are highly selective partial agonists or antagonists at human CRF 1 receptors that are useful in the diagnosis and treatment of treating stress related disorders such...
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6469047 |
Tyrosine derivatives
The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.
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6452009 |
4-unsubstituted dihydroisoquinolinone derivatives and combinatorial libraries thereof
The present invention relates to novel dihydroisoquinolinone (DHQ) derivative compounds of the following formula: wherein R 1 to R 7 , X, Y, Z, b, c and d have the meanings provided herein. The...
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6441196 |
Processes and novel intermediates for 11-oxa prostaglandin synthesis
Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.
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6437134 |
Process for a phenylthiobutyl-isoquinoline and intermediates therefor
A method for making phenylthiobutyl-isoquinoline compounds of formula and novel intermediates therefor.
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6436960 |
Farnesyl transferase inhibitors having a piperidine structure and process for preparation thereof
The present invention relates to a novel piperidine derivative represented by formula (1) which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts...
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6436989 |
Prodrugs of aspartyl protease inhibitors
The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl...
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6433177 |
Process for the preparation of (S)-N-tert-butyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
It is here described a new process for the synthesis of (S)-N-tertbutyl-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
wherein the N-carboxy anhydride of formula is treated with tert-butylamine...
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6432962 |
Benzophenones as inhibitors of IL-1β and TNF-α
Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1β and TNF-α and may therefore be useful in the therapy of inflammatory diseases and conditions.
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6432995 |
Aromatic heterocyclic compounds and their use as anti-inflammatory agents
Novel aromatic heterocyclic compounds inhibit cytokines production involved in immunoregulation and inflammation such as interleukin-1 and tumor necrosis factor production. The compounds are...
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6429312 |
N-aminoalkyldibenzothiopencarboxamide receptor subtype specific ligands
Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: R 1 , R 2 , R 3 , R 4 are the same or different and represent hydrogen, C 1 -C 6...
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6417362 |
Nitrogenous heterocyclic compounds and hyperlipemia remedy containing the same
Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can...
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6410529 |
Phenyl urea and phenyl thiourea derivatives as HFGAN72 antagonists
Phenyl urea and phenylthiourea derivatives, processes for their production and their uses as pharmaceuticals are disclosed.
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6403577 |
Hexamethyleneiminyl tachykinin receptor antagonists
This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention...
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RE37729 |
4-Heteroaryl-1-piperidinealkylamines 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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6399627 |
Inhibitors of factor Xa
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating...
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6395749 |
Carboxamide compounds, methods, and compositions for inhibiting PARP activity
The present invention provides carboxamine compounds, methods and compositions for inhibiting PARP activity.
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