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7358239 |
Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7342006 |
Substituted 8-heteroaryl xanthines
Selective antagonists of A 2B adenosine receptors like those of formula I are provide.
The compounds and compositions are useful as pharmaceutical agents.
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7238684 |
Benzothiadiazepine derivatives, processes for their preparation and pharmaceutical compositions containing them
The present invention relates to compounds of formula (I): wherein R v , R 1 , R 2 , R x , R y , R 3 , R 4 , R 5 , R 6 , R z and v are as defined within; pharmaceutically acceptable salts,...
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RE39608 |
Substituted benzimidazoles and their use as PARP inhibitors
Compounds of the formula Ia or IB
where
A is a saturated or monounsaturated heterocyclic, 4 - to 8-membered ring which contains one or two nitrogen atoms,
and their tautomeric forms,...
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7208487 |
Compounds, compositions and methods
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
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7132416 |
Benzothiazepine and benzothiazepine derivatives with ileal bile acid transport (IBAT) inhibotory activity for the treatment hyperlipidaemia
The present invention relates to compounds of formula (I) wherein R v , R 1 , R 2 , R x , R y , M, R z , v, R 3 , R 4 , R 5 and R 6 are as defined within; pharmaceutically acceptable salts,...
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7081453 |
Compounds for treating impaired fundic relaxation
The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharma-ceutically acceptable acid addition salt thereof, wherein —a...
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7064136 |
Compounds
A compound having the general formula
and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.
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7056908 |
Pharmaceutical compositions and methods for preventing skin tumor formation and causing regression of existing tumors
Pharmaceutical compositions and methods for treating epithelial cancers and precancerous lesions employ indole carbazole compounds, such as staurosporine. Compositions containing these compounds...
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RE39112 |
Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes
The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine...
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7049309 |
3-Thia-4-arylquinolin-2-one potassium channel modulators
This invention describes compounds of Formula (I) which are modulators of potassium channels and are useful for treating conditions affected by abnormal potassium channel activity including...
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7030150 |
Benzimidazole compounds and antiviral uses thereof
The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion...
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6984652 |
Gyrase inhibitors
Compounds comprising an indazolyl group and a thiazolyl group, preferably 7-substituted 3-(thiazol-2-yl)-1H-indazole compounds in which the indazolyl group and a thiazolyl group are each...
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6962915 |
Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors
Compounds having the formula (I),
and pharmaceutically acceptable salts or prodrugs thereof, are useful as kinase inhibitors, wherein Y is —C(═O)NR 1 —, —NR 1 C(═O)—, —NR 1...
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6949539 |
Admantane derivatives
The invention provides compounds of general formula (I) in which m, A, R 1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions...
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6921759 |
Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV...
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6906057 |
Methods for modulating FXR receptor activity
Methods for modulating the activity of the mammalian FXR receptor. The methods include methods of treating a hyper- or hypocholesterolemic mammal comprising contacting the mammal with synthetic...
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6900222 |
Pyrrolidinyl, piperdinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein...
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6852715 |
Indolocarbazole alkaloids from a marine actinomycete
The invention provides compounds of formula (1) wherein R 1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; and R 2 is a hydrogen...
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6852714 |
(Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties
The present invention of compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk 1 ...
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6806266 |
Staurosporin derivatives
The present invention provides an antitumor agent comprising a staurosporin derivative or a pharmaceutically acceptable salt thereof, as an active ingredient, which is represented by the general...
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6767907 |
4-aryl-1-(indanmethyl dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl) piperidines tetrahydropyridines or piperazines
4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH 2 and...
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6730676 |
Pyrazino-pyridazine derivatives as ligands for GABA receptors
A class of pyrazino[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 5-position, a substituted alkoxy moiety at the 3-position,...
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6696480 |
Upregulation of type III endothelial cell nitric oxide synthase by agents that disrupt actin cytoskeletal organization
A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell...
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6680328 |
8-azabicyclo&lsqb 3.2.1&rsqb oct-2-ene and -octane derivatives
The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their...
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6656932 |
Benzo thiadiazine matrix metalloproteinase inhibitors
Selective MMP-13 inhibitors are benzo thiadiazines of the Formula or a pharmaceutically acceptable salt thereof, wherein R 2 is hydrogen or alkyl; R 1 and R 3 include hydrogen, alkyl, and...
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RE38332 |
Selected soluble esters of hydroxyl-containing indolocarbazoles
Esters of hydroxyl-containing indolocarbazoles and acids containing selected solubilizing groups are provided. Compositions including the indolocarbazole esters and methods for the use of the...
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6635637 |
Cyclic oxyguanidine protease inhibitors
Cyclic oxyguanidine compounds, including compounds of Formulae I and II: wherein R 1 , R 3 -R 6 , R 21 -R 26 , L, Y, Z, and A are set forth in the specification, as well as hydrates, solvates or...
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6624157 |
Thiadioxobenzodiazepine inhibitors of farnesyl protein transferase
Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas and their enantiomers, diastereomers, and their...
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6608070 |
2,3-substituted indole compounds as anti-inflammatory and analgesic agents
This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the...
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6569850 |
Treatment of multiple sclerosis (MS) and other demyelinating conditions using lofepramine in combination with L-phenylalanine, tyrosine or tyrptophan and possibly a vitamin B12 compound
Method for treating multiple sclerosis or encephalomyelitis by administering to a patient a combination of a tricyclic antidepressant drug and tyrosine or phenylalanine or both.
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6559155 |
Pyrimidinone derivatives for the treatment of atherosclerosis
Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA 2 and thereof use in treating inter alia atherosclerosis, in which: R 1 is COOH or a salt thereof, COOR 10 , CONR 11 R 12 , CN or...
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6548506 |
Benzo&lsqb 1,8&rsqb naphthyridine derivatives, their preparation and pharmaceutical compositions which comprise them
Novel 1,8-benzo-naphthyridine derivatives of general formula (I): which are useful as antimicrobial agents.
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6545057 |
Tricyclic antidepressants and their analogues as long-acting local anesthetics and analgesics
Methods and compositions of tricyclic antidepressants for inducing local long-lasting anesthesia and analgesia are provided. The methods and compositions are useful for alleviating acute and...
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6500818 |
Naphthalenecarboxamides as tachykinin receptor antagonists
Compounds having the following formula wherein L, M, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X 1 and X 2 are as defined in the specification, pharmaceutically-acceptable salt thereof, useful for...
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6482819 |
2,3-benzodiazepine derivatives
2,3-Benzodiazepines of formula (I), their stereoisomers and acid addition salts, wherein the variables have the meaning given in the specification, and pharmaceutical compositions containing...
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6472386 |
Cyclic diamine compound with 5-membered ring groups
A compound of formula (1): wherein A is a single bond, C≡C, CONH or NHCO; W is a carbon atom or a nitrogen atom; X is CH, a nitrogen atom, an oxygen atom or a sulfur atom; Y is CH, CHR 1 , in...
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6472385 |
Compositions and methods to enhance cancer chemotherapy in p53 defective tumors
Compositions which abrogate DNA damage induced cell cycle arrest thereby enhancing the cell killing activity of DNA damaging anticancer agents for use in the treatment of cancer, and in particular,...
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6451787 |
Remedies for ocular diseases
Use of the compound represented by general formula (I) for remedies of and protection against eye diseases is disclosed. General formula (I): (wherein, R 1 and R 2 independently represent a...
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6451786 |
3′-epimeric k-252a derivatives
Compounds defined by the following general structure are disclosed: These compounds display pharmacological activities, including inhibition of tyrosine kinase activity and enhancement of the...
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6436943 |
Use of dihydropyrimidines as medicaments, and novel substances
The invention relates to dihydropyrimidines of the general formula and to the use of dihydropyrimidines as medicaments for the treatment and prophylaxis of hepatitis B. The invention further...
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6395740 |
Calcitonin mimetics
Compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. Included among the calcitonin mimetics...
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6387912 |
Utilization of pyrimidine derivatives for preventing and treating cerebral ischaemia
Use of pyrimidine derivatives of the formula I where the substituents are as defined in the description, and of their physiologically tolerated salts for producing medicaments for the...
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6384056 |
Heterocyclic thioesters or ketones for vision and memory disorders
This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using heterocyclic...
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6358978 |
Substituted benzimidazoles
Compounds of formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NFκB is involved.
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6337326 |
N-aryl-(homopiperazinyl)-cyclohexyl amines
This invention provides novel compounds and methods and compositions using them in the treatment of central nervous system disorders, including depression and anxiety, the compounds having the...
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6316435 |
Combination therapy for lymphoproliferative diseases
Disclosed are methods and kits for treating lymphoproliferative diseases in a host including (co)administering to the host pentostatin, at least one alkylating agent and at least one methylated...
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6300327 |
Compositions and methods for potentiation of neurotrophin activity
Compositions and methods for use in modulating neurotrophin activity, wherein the active agent is at least one compound which potentiates neurotrophin activity. A preferred class of active agents...
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6294542 |
Pyrimidinone compounds, pharmaceutical compositions containing the compounds and the process for preparing the same
The present invention relates to a novel pyrimidinone compounds and the pharmaceutical acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, thereby, being...
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6225306 |
Biphenyl derivatives and drug composition
A biphenyl derivative represented by the following general formula (1) and a pharmaceutically acceptable salt thereof: ##STR1## [In the formula (1), A represents a single bond, --CH 2 --, --CO--,...
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