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7629338 |
Substituted monocyclic CGRP receptor antagonists
Compounds of formula I:
(wherein variables A 1 , A 2 , A 3 , A 4 , m, n, J, Q, R 4 , E a , E b , E c , R 6 , R 7 , R e , R f , R PG and Y are as described herein) which are antagonists of CGRP...
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7612205 |
Crystals of quinolinecarboxylic acid derivative solvate
A main object is to provide a crystal of 6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)-me
thyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3
-carboxylic acid acetonitrile...
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7582761 |
Vanilloid receptor ligands and their use in treatments
Therapeutic benzimidazoles having the general structure:
and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache,...
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7576087 |
Heterocyclyl-3-sulfonylazaindole or -azaindazole derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
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7557107 |
Farnesyl protein transferase inhibitors as antitumor agents
Disclosed are novel tricyclic compounds of the formula:
and a pharmaceutically acceptable salts or solvates thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also...
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7531535 |
Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
The present application describes lactam-containing compounds and derivatives thereof of Formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7...
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7465742 |
Heterocyclic compounds having anti-HBV activity
This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to...
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7462717 |
C6-and C9-substituted chromeno[4,3-c]isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and...
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7446110 |
17-Heterocyclic-4-azasteroid derivatives as androgen receptor modulators
Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment...
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7435726 |
Compositions and methods for the treatment of cancer
This invention relates to compositions comprising thalidomide and another anti-cancer drug which can be used in the treatment or prevention of cancer. Preferred anti-cancer drugs are topoisomerase...
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7432276 |
ABCA1 elevating compounds
The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of...
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7388016 |
Dibenzonaphthyridine derivatives and methods of use thereof
The present invention relates to Dibenzonaphthyridine Derivatives, compositions comprising an effective amount of a Dibenzonaphthyridine Derivative and methods for treating or preventing a...
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7384939 |
Process for preparation of pyridine derivatives of NK-1 receptor antagonist
The present invention provides a process for preparing a pyridine compound of the formula:
wherein R 1 , R 2 , R 3 and a are those defined herein.
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7354918 |
Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol and applications thereof
The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I)
in which R represents a radical —AR′ wherein A represents a heteroatom and R′...
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7320984 |
Remedies or preventives for urinary frequency or urinary incontinence and morphinan derivatives having nitrogen-containing heterocyclic group
The invention provides a morphinan derivative of the Formula (I):
wherein R 1 is methyl, cyclopropylmethyl or the like; R 2 and R 3 are hydroxy, methoxy, acetoxy or the like; both Y and Z...
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7312209 |
Acridone inhibitors of IMPDH enzyme
Compounds having the formula (I),
wherein R 3 is selected from H, OH and NH 2 ; R 30 is selected from ═O and ═S; W is —C(═O)—, —S(═O)—, or —S(O) 2 —; or W may be —CH 2...
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7265103 |
Substituted amino isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and...
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7247641 |
Compounds, derivatives, compositions, preparation and uses
This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
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RE39707 |
Camptothecin derivatives
(20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an oxyalkanoic acid and camptothecin, which is are optionally substituted at the 7, 9, 10, 11, and 12...
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7230105 |
9-aminoacridine derivatives and process for the preparation thereof
The present invention relates to a new 9-aminoacridine derivative which exhibits prominent antitumor activity and low toxicity.
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7226928 |
Methods for the treatment of periodontal disease
The disclosure provides methods for the treatment and prevention of periodontal disease. In preferred embodiments, the invention provides for local treatment of periodontal tissues with a...
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7211417 |
Antibiotic P175-A and semisynthetic derivatives thereof
This invention relates to a new antibiotic designated P175-A, to production of fermentation of Micromonospora echinospora NRRL 30633, to methods for recovery and concentration from the crude...
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7199128 |
8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents
The invention provides compounds and salts of Formula I and Formula II:
which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making...
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7186724 |
Heterocyclic substituted carbonyl derivatives and their use as dopamine D3 receptor ligands
The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D 3 receptors. In another aspect, the invention relates to a method for treating...
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7176214 |
Imidazo-fused oxazolo[4,5-β]pyridine and imidazo-fused thiazolo[4,5-β]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I),
wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as described herein. The present invention...
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7169786 |
Isoxazoline derivatives as anti-depressants
The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R 7 , S or O, R 1 , R 2 and R 3 are certain specific substituents, Pir is an...
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7153849 |
Antidepressant arylpiperazine derivatives of hetrocycle-fused benzodioxans
Compounds of the formula I:
are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
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7135480 |
Substituted 1-benzoyl-3-cyano-pyrrolo [1,2-a] quinolines and analogs as activators of caspases and inducers of apoptosis
The present invention is directed to substituted 1-benzoyl-3-cyano-pyrrolo[1,2-α]quinolines and analogs thereof, represented by the general Formula I:
wherein R 1 –R 8 , L, Q, dash line and...
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7115621 |
Chemical compounds
Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disorders
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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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7053091 |
17 β-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17β-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical...
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6943199 |
Spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines
Substituted spiro[isobenzofuran-1,4′-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4′-piperidines capable of modulating NPY5 receptor activity are provided. Such compounds may be used to...
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6943168 |
Calcium channel inhibitors comprising benzhydril spaced from piperazine
Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.
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6936622 |
6-phenylbenzonaphthyridines
Compounds of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in the description, are novel effective PDE3/4 Inhibitors.
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6916809 |
Heterocyclic acridone inhibitors of IMPDH enzyme
Compounds having the formula (I),
wherein R 3 is selected from H, OH and NH 2 ; R 30 is selected from ═O and ═S; W is —C(═O)—, —S(═O)—, or —S(O) 2 —; or W may be —CH 2...
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6897219 |
Heteroaryl diazacycloalkanes, their preparation and use
The present invention discloses compounds of the formula
any of its enantiomers or any mixture thereof, isotopes thereof or a pharmaceutically acceptable salt thereof;
wherein
n is 1,...
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6828319 |
Substituted indeno&lsqb 1,2-c&rsqb isoquinoline derivatives and methods of use thereof
The invention provides novel classes of substituted Indeno[1,2-c]isoquinoline Compounds. Pharmaceutical compositions and methods of making and using the compounds, are also described.
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6815449 |
LK6-A derivatives
Compounds having immunosuppressive activity, cell growth inhibitory activity, anti-tumor activity, etc. are represented by formula I: and pharmaceutically acceptable salts thereof.
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6809201 |
Intercalator suitable for electrochemical detection of double strand DNAs and a process for preparing thereof
The present invention relates to the compound of formula (I) useful as an intercalator in electrochemical detection of double-stranded DNAs, and a method for preparation thereof:
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6800636 |
Farnesyl protein transferase inhibitors
Disclosed are compounds of the formula: wherein R 8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R 9 represents a carbamate, urea, amide or sulfonamide group; and the...
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6762191 |
Therapeutic compounds
The present invention provides compounds of formula (I): wherein: R 1 , R 2 , R 3 R 4 , R 5 , R 6 , X, - - - , m, and n have any of the values defined in the specification, as well as...
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6759414 |
Aromatic amides
This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa,...
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6743794 |
Methods and compounds for inhibiting MRP1
The present invention further relates to a method of inhibiting MRP1 in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound of formula (I).
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6740661 |
Farnesyl protein transferase inhibitors
Disclosed are compounds of the formula: wherein R 13 represents an imidazole ring; R 14 represents a carbamate, urea, amide or sulfonamide group; R 8 represents H when the alkyl chain between...
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6723733 |
Sulfonamide and carbamide derivatives of 6(5H)phenanthridinones and their uses
This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
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6720332 |
Oxindole derivatives
Oxindole derivatives, specifically pyrrolo[3,2-f]quinoline-2-ones, which are useful as CDK4 inhibitors are described herein. The described invention also includes methods of making such oxindole...
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6716982 |
Method for preparing camptothecin derivatives
The present invention relates to a process for preparing camptothecin and camptothecin analogs of Formula (I) from compounds of Formula (II) and to novel intermediates useful in their preparation, ...
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6699872 |
N-substituted urea inhibitors of farnesyl-protein transferase
Novel halo-N-substituted urea compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras...
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6699864 |
Substituted phenyl-piperazine derivatives, their preparation and use
The present invention provides compounds of the formula: wherein R 1 -R 8 , X, Y, Z, n and m are defined in the application. The compounds of the invention have affinity for the 5-HT 1A receptor.
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6693112 |
Compounds for enhancing chemotherapy
The present invention provides 2,3-dihydro-1H-pyrrolo[2,3-b]quinolin-4-ylamines, of the formula: or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , and R 7 are as defined...
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