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7622586 |
Opiate intermediates and methods of synthesis
Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided.
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7601739 |
Compounds having antiestrogenic and tissue selective estrogenic properties, and compounds with anti-androgenic properties for treatment of prostate cancer and androgen receptor dependent diseases
Compounds for the treatment of estrogen-receptor related maladies are provided. Compounds with anti-androgenic properties also are provided. In particular, the invention provides compounds that are...
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7595399 |
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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7538121 |
Vanilloid receptor modulators
Certain compounds of formula (I),
or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 , R 2 , R 3 , P, X, Y, q, r ans s are as defined in the specification, a process for...
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7511060 |
Opiate intermediates and methods of synthesis
Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided.
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7312222 |
Heterocyclic piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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7309708 |
Hepatitis C virus inhibitors
Hepatitis C virus inhibitors are disclosed having the general formula:
wherein R 1 , R 2 , R 3 , R′, B, Y and X are described in the description. Compositions comprising the compounds and...
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7217706 |
Propanolamine derivatives
This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]:
Wherein each symbol is as defined in the specification or salts thereof which...
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RE39265 |
Heteroarylpiperidines, and their use as antipsychotics and analgetics
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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7041664 |
2-aminoquinolinecarboxamides: neurokinin receptor ligands
Disclosed are compounds of the formula:
or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof,
wherein R 1 , R 2 , R 3 , X, Q 1 and Q 2 are defined herein,
...
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6949565 |
Protein kinase inhibitors
Novel isoquinoline derivatives which are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes are disclosed. Preferred compounds which are specific inhibitors...
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6875765 |
Arylsulfonamide ethers, and methods of use thereof
The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1β converting enzyme and other cysteine proteases in the ICE family are...
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6825213 |
β3-adrenoreceptor agonists, agonist compositions and methods of using
The invention provides β 3 -adrenoreceptor agonists, pharmaceutical compositions comprising β 3 -adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating...
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6809091 |
Substances capable of inducing apoptosis
A method for the manufacture of a substance having an apoptosis-inducing ability characterized in including a step of subjecting at least one compound selected from the following (a), (b), (c) and...
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6784186 |
Therapeutic compounds
This invention relates to novel structural analogues and derivatives of compounds with general analgesic or related pharmacological activity. In particular the invention relates to derivatives of...
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6703392 |
1,2,3,4-tetrahydroisoquinoline derivatives
The invention relates to novel 1,2,3,4-tetrahydroisochinoline derivatives of formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also...
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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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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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6573278 |
Aryl sulfonamides and analogues thereof and their use in the treatment of neurodegenerative diseases
The present invention relates to new aryl ether sulphonamides and analogues, processes for their preparation and their use for the treatment of neurodegenerative disorders, in particular for the...
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6509351 |
Phenyl- and pyridyl-tetrahydro-pyridines having TNF inhibiting activity
The present invention relates to compounds of formula (I): as well as the salts or solvates thereof, to pharmaceutical compositions containing them, to a process for preparing them and to...
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6476226 |
Isoxazoline fibrinogen receptor antagonists
This invention relates to novel isoxazolines and isoxazoles of formula (I): or a pharmaceutically acceptable salt or prodrug form thereof. The invention relates to novel isoxazolines which are...
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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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6414154 |
Tetraisoquinoline derivatives as modulators of dopamine D3 receptors
Compounds of formula (I), wherein: R 1 represents a substituent selected from: a hydrogen or halogen atom; a hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy,...
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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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6288071 |
1-ethylene-2-alkylene-1,4-cyclohexadiene pesticides
Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in...
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6265408 |
Sulphonamide derivatives and their use in the treatment of CNS disorders
Sulphonamide compounds according to formula (I) or pharmaceutically acceptable salts thereof: ##STR1## wherein: Ar is naphthyl, phenyl or thienyl optionally substituted by one or more...
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6211196 |
Benzyloxy-substituted, fused N-heterocycles, processes for their preparation, and their use as bradykinin receptor antagonists
Benzyloxy-substituted, fused N-heterocycles, because of their ability to act as bradykinin receptor antagonists, have been found to be useful as therapeutics for the treatment and prevention of...
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6184381 |
Process for preparing optically active compounds
This document describes a novel and practically excellent process for the preparation of optically active compounds, such as optically active alcohols or amines which are useful for various...
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RE37029 |
N-[(3-heteroaryl-1-pyrrolidinyl)-alkyl]phthalimides and related compounds 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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6087346 |
Sigma receptor ligands and the use thereof
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6063925 |
Separation of enantiomers of octahydroisoquinoline
This invention describes a process for the isolation of (-)1-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline
from a racemic mixture, which involves treating partially resolved mixtures...
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6046190 |
Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
The invention relates to sulfonamide-containing hydroxyethylamine protease inhibitor compounds, their process of making, composition and method of use for inhibiting retroviral proteases such as...
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6043253 |
Fused piperidine substituted arylsulfonamides as β3-agonists
Fused piperidine substituted arylsulfonamides are β 3 adrenergic receptor agonists with very little β 1 and β 2 adrenergic receptor activity and as such the compounds are capable of...
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6015903 |
Method of resolving racemic mixtures
A process for resolving racemates of compounds of the formula I ##STR1## in which a, A, B, D, E, F, M, Q and R have the meanings given in the description is described. The process is carried in a...
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5994507 |
Method for binding albumin and means to be used in the method
A method for binding albumin by contacting an aqueous liquid containing an albumin with an albumin-binding compound is selected from albumin-binding compounds containing the scaffold...
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5981521 |
Tetrahydroisoquinoline derivatives as LHRH antagonists
Tetrahydroisoquinoline derivatives of the formula: ##STR1## or a pharmaceutically acceptable salt, ester, or prodrug thereof, having activity as an LHRH antagonist, as well as pharmaceutical...
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5955471 |
Tetrahydroisoquinolinealkanol derivatives and pharmaceutical compositions containing same
The present invention provides novel 1,2,3,4-tetrahydroisoquinoline carbamate and thiocarbamate derivatives represented by Formula I ##STR1## wherein: X 1 and X 2 are the same or different from...
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5904877 |
Trifluoratetrahydroisoquinoline derivatives, and the use thereof in liquid-crystalline mixtures
1,8,8-Trifluoro-5,6,7,8-tetrahydroisoquinoline derivatives, and their use in liquid-crystalline mixtures 1,8,8-Trifluoro-5,6,7,8-tetrahydroisoquinoline derivatives of the formula (I) R 1 (--M 1...
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5882546 |
1,8-Difluorisoquinoline derivatives and the use thereof in liquid crystalline mixtures
1,8-Difluoroisoquinoline derivatives of the formula (I) R 1 (--M 1 ) a (--A 1 --M 2 ) b (--A 2 --M 3 ) c --B(--M 4 --A 3 ) d (--M 5 --A 4 ) e (--M 6 ) f --R 2 (I) in...
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5880285 |
Process for manufacture of optically active isochinole compounds
A process for the manufacture of optically active (R)- or (S)-1-(4-methoxy-benzyl)-1,2,3,4,5,6,7,8-octahydro-isoquinol
ine adducts of the formula ##STR1## wherein HX signifies a mineral acid from...
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5856503 |
Aminoalkyl-substituted benzo-heterocyclic compounds
Aminoalkyl-substituted benzo-heterocyclic compounds of the formula ##STR1## wherein M, Q, R and T are as defined in the specification, as well as acid addition salts thereof. These compounds are...
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5817674 |
Quinoline compounds
Compounds of the formula ##STR1## in all possible racemic, enantiomeric and diastereoisomeric forms and their non-toxic, pharmaceutically acceptable salts with acids and bases having antagonistic...
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5776963 |
3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
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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5763613 |
Monomeric naphthylisoquinoline alkaloids and synthesis methods thereof
The present invention provides methods of preparing monomeric naphthylisoquinoline alkaloids, including the antiparasitic korupensamines and related compounds, as well as non-korupensamines and...
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5756516 |
1,2,3,4-tetrahydroisoquinoline derivatives and pharmaceutical composition thereof
The invention relates to compounds of formula (I) ##STR1## wherein R 1 is an optional substituent any position of phenyl ring and is selected from halogen, --NO 2 , --NH 2 , --OH and --O--CR 1 -6...
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5721247 |
Isothiourea derivatives useful in therapy
There are provided novel compounds of formula I ##STR1## wherein D, R 1 , R 2 , R 3 , X and p are as defined in the specification together with processes for their preparation, compositions...
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5668285 |
Total synthesis of northebaine, normophine, noroxymorphone enantiomers and derivatives via N-Nor intermediates
The invention involves a method of making key intermediates useful in the synthesis of many opiate narcotics and antagonists and agonists; and the non-opiate enantiomers thereof which have potent...
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5663449 |
Intermediate compounds in the synthesis of heteroarylpiperidines, pyrrolidines and piperazines
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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5654319 |
N-[(4-heteroaryl-1-piperidinyl)alkyl]-2,3-naphthalimides and related compounds 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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5654306 |
Piperidine derivative and pharmaceutical composition
A piperdine derivative having the formula (I) or a pharmacologically acceptable salt thereof: R 1 --X--A--R 2 (I) wherein R 1 is selected from the group...
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