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7378421 |
Chromenone derivatives
Novel compounds of the formula I
in which
R 1 , R 2 , R 3 and Het are as defined herein, which
are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of...
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7335660 |
Isochroman compounds for treatment of CNS disorders
This invention relates to compounds of formula (I)
where R 1 to R 12 , —W—V—, —X—Y—, p and n have the values defined in claim 1 , their preparation and use as pharmaceuticals for...
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7312242 |
Use of parthenolide derivatives as antileukemic and cytotoxic agents
Compounds of the formula having anti-tumor activity, wherein R 1 and R 2 are as described herein
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7271168 |
Piperazine derivatives having SST1 antagonistic activity
The invention provides compounds of formula ( 1 )
wherein X, R 1 and R 2 are as defined in the specification, their, preparation and to their use in treating, e.g., depression, anxiety and...
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7256187 |
Rifamycin C-11 oxime derivatives effective against drug-resistant microbes
The invention relates to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms, specifically, the rifamycin derivatives having an oxime...
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7253172 |
Dipeptidyl peptidase inhibitors for the treatment of diabetes
Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (I) are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of...
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7208497 |
Substituted piperazines and diazepanes
A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor....
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7189726 |
Benzofuran derivatives as inhibitors of p38-α kinase
The invention is directed to methods to inhibit p38-α kinase using compounds which contain an aromatic residue coupled to an benzofuran moiety through a piperidine.
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7186752 |
Derivatives of N-(iminomethyl)amines, their preparation, their use as medicaments and the pharmaceutical compositions containing them
N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.
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7176236 |
Water-soluble etoposide analogs and methods of use thereof
Etoposide analogs with improved water-solubility such as 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-n
itroanilino)-4-desoxy-podophyllotoxin (8) and...
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7144883 |
Bicyclic sulfonamide compounds
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful...
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7135473 |
Cyclic diamine compound with condensed-ring groups
A cyclic diamine compound of formula (1):
wherein R 1 and R 2 are individually a hydrogen atom or a methoxy group, provided R 1 is a methoxy group when R 2 is a hydrogen atom, or a hydrogen...
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7084144 |
Sulfonyl group containing compounds and their use for the treatment of erectile dysfunction
A compound having the general formula (I):
wherein: X is N or C; R 0 is H, a lower alkyl group, a lower O-alkyl group,
lower alkyl group, a benzyl group, a phenyl group, a heterocyclic...
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7067513 |
Phenylpiperazines
The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D 2 receptor and/or the serotonin reuptake site,...
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7026314 |
Therapeutic chromone compounds
Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating,...
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6995153 |
Fused bicyclic pyrimidine derivatives
A novel fused bicyclic pyrimidine derivative or a salt thereof that acts as a tachykinin receptor antagonist and, in particular, as an NK1 receptor antagonist is represented by the following...
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6967201 |
Benzofurylpiperazines and benzofurylhomopiperazines: serotonin agonists
The present invention provides serotonergic benzofurylpiperazines of Formula I:
where:
A is a piperazine of formula:
and R, R 1 , R 2 , R 3 , R 4 , R 5 , R 5′ , R 6 , R 6′ , R 7...
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6916831 |
Flavone acetic acid analogs and methods of use thereof
Compounds are described having a structure according to Formula I or Formula II:
wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O...
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6916812 |
Alpha-aminoamide derivatives as melanocortin agonists
Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the...
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6900213 |
Bisaryl derivatives having FSH modulatory activity
The invention relates to bisaryl derivatives of the formula I,
wherein (R,R) is selected from (H,H), O, (H,CH 3 ), (H,OH) and (H,CN); Ar is substituted phenyl
and A is a group of formula II,...
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6894052 |
Diarylalkylpiperazines active on the lower urinary tract
Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are diarylalkylpiperazine derivatives. The methods comprise the...
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6867230 |
Hygromycin A derivatives
This invention relates to compounds of the formula
and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R 1 , R 2 , R 3 and R 10 are as defined herein. The...
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6852723 |
Aralkyl substituted piperazine compounds
Novel compounds of the general formula:
and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage...
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6825202 |
Arylsulfonyl derivatives with 5-HT6 receptor affinity
This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula (I): wherein Ar, R 1 , R 2 , R 3 or R 4 are as defined in the...
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6825201 |
Indole, azaindole and related heterocyclic amidopiperazine derivatives
The invention comprises substituted indole, azaindole and related heterocyclic amidopiperazine derivatives of general Formula I wherein: Q is —may represent a bond; A is selected from the...
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6821977 |
Antidiabetic agents
A compound of the formula whereon R 1 is: R 5 is: and n, m, Z, R 8 , R 9 , R 10 and R 11 are as defined herein, useful in the treatment of diabetes, insulin resistance, diabetic...
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6821967 |
Substituted piperazine derivatives, the preparation thereof and their use as medicaments
The present invention relates to substituted piperazine derivatives of general formula wherein R a , R b , R c , R f , R g , X, m and n are defined as in claim 1, the isomers and salts thereof,...
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6777414 |
Nitrogen-containing heterocyclic compounds and benamide compounds and drugs containing the same
Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing...
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6770649 |
1-&lsqb 1-(hetero)aryl-1-perhydroxyalkylmethyl&rsqb -piperazine compounds, process for their preparation and pharmaceutical compositions containing them
Novel 1-[1-(hetero)aryl-1-perhydroxyalkylmethyl]-piperazine compounds which are antagonistic to tachykinin receptors, of the general formula I, wherein R 6 , R 7 , A and Z have the meanings...
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6753331 |
Heterocyclic derivatives which inhibit factor Xa
The invention relates to heterocyclic derivatives of formula (I), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful...
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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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6699858 |
Halogen substituted tetracyclic tetrahydrofuran derivatives
This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2,...
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6680318 |
Piperazinomethylbenzamides as delta-opioid receptor agonists
The present application is directed to compounds having the general formula: and to the use of these compounds in therapeutic methods.
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6677343 |
Substituted piperazine compounds
Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage...
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6664258 |
Spirocyclic dopamine receptor subtype ligands
This invention relates to novel, pharmaceutically active compounds of formula (I) wherein a, b and R 1 through R 6 are as defined in the specification These compounds exhibit central...
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6645951 |
Benzopyran or thiobenzopyran derivatives
The present invention provides novel benzopyran compounds, pharmaceutically acceptable salts thereof and stereoisomers thereof where the benzopyran compounds of the invention are compounds...
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6638972 |
Chroman and benzofuran derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
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6638936 |
Benzofurylpiperazine serotonin agonists
The present invention provides serotonergic benzofurans of Formula I: where R is methyl or ethyl, or pharmaceutically acceptable acid addition salts thereof.
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6620843 |
Anticancer treatment using triptolide prodrugs
Water soluble triptolide prodrugs are used as anticancer agents, and are found to be more effective in vivo, at lower doses, in reducing tumor size than the widely used chemotherapeutic agents...
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6608089 |
Derivatives of flavones, xanthones and coumarins
Compounds having the formula (I) Z—OCH 2 —C≡CCH 2 —NRR 1 (I) or a pharmaceutically acceptable salt or solvate thereof wherein Z can represent the formula (1A) or (1B). The compounds...
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6599904 |
Sulphonamide derivatives, process for their preparation, and their use as medicaments
Novel sulphonamide derivatives having CNS activity, processes for their preparation and their use as medicaments are disclosed. The present compounds are of formula (I) or a salt thereof: ...
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6596745 |
Method for treating fibrotic diseases with azolium chroman compounds
Provided is a method of treating or ameliorating hypertension in an animal comprising administering an effective amount of a compound of formula I:
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6596722 |
Piperidine, tetrahydropyridine and piperazine derivatives, their preparation and use
A piperidine, tetrahydropyridine or piperazine derivative having formula (I), any of its enantiomers or any mixture thereof, or an acid addition salt thereof, wherein B is C 1-10 -alkylene, C...
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6552022 |
Benzamide derivatives and their use as ApoB-100 secretion inhibitors
The invention relates to therapeutic benzamide compounds of formula (I) wherein A, X, Z, R 1 , Y, R 2 , R 3 , are as defined herein, and physiologically acceptable salts, solvates or derivatives...
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6514967 |
Compound for preparing medicines for treating pathologies involving extracellular glutamate, and methods for obtaining same
The invention relates to compounds of the following general formula (I): in which: R 1 and R 2 represent a hydrogen atom, or form a ring, especially a benzene ring, R 3 represents a hydrogen...
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6506555 |
Use of HIV protease inhibiting compounds
The invention relates to the use of at least one compound that inhibits HIV (human immunodeficiency virus) protease, selected from ritonavir, saquinavir or one of the pharmaceutically acceptable...
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6492368 |
Benzamidine derivatives as factor XA inhibitors
Novel compounds of the formula I in which X, Y, R 1 , R 2 and R 3 are as defined in Patent Claim 1 are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or...
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6486164 |
6-(4-arylalkylpiperazin-1-yl) benzodioxane and 6-(4-arylalkylpiperazin-1-yl) chromane derivatives: dopamine 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 and R 5 are the same or different and represent hydrogen,...
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6486163 |
Thienopyranecarboxamide derivatives
The invention relates to novel N-(substituted phenyl)-N′-[ω-(5-substituted-7-oxo-7H-thieno[3,2-b]pyran-
3-carbonylamino)alkyl]piperazines their N-oxides and pharmaceutically acceptable salts...
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6482827 |
Matrix metalloproteinase inhibitors
A compound, which is an amine derivative of formula (I) wherein W is —CNHOH or —COOH: R 1 and R 2 are each hydrogen or an organic residue, R 3 is an organic group, Q is a secondary or...
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