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7585855 |
Bengamides with a substituted caprolactam cycle, method for the preparation thereof, compositions containing them and use thereof
The invention relates to the preparation of substituted caprolactams, a method for the preparation thereof, compositions containing them and the use thereof as a medicament, particularly as...
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7501406 |
Fluoro substituted 2-oxo-azepan derivatives
The invention relates to compounds of general formula
wherein
R 1 , R 2 , R 3 /R 3′ , R 4 /R 4′ and R 5 /R 5′ are as defined in the specification
and to pharmaceutically acceptable...
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7378410 |
Substituted lactams and their use as anti-cancer agents
This invention relates to certain substituted lactam compounds of the formula (I), particularly caprolactam compounds, which are useful for the treatment of cancer
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7361648 |
Heterocyclylakylamines as muscarinic receptor antagonists
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I:
wherein X, Y, and Z are O, S or NR 5 , and the other...
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7342007 |
Lactams and uses thereof
This invention relates to novel compounds having formula (I) to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit secretase and thereby inhibit the...
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7326698 |
Prostaglandin analogs
Compounds comprising
or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. A, X, J, and E are as described herein. These compounds are useful for treating diseases.
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7294622 |
Lactams and uses thereof
Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid β protein production and...
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7253158 |
Sulfonamides
The invention relates to compounds of the general formula
in which R 1 , R 2 , R3, R 4 , R 2′ , R3′, R 4′ , R 5 , and X is —CHR— are as defined in the specification. The invention...
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7208488 |
N-substituted benzene sulfonamides
Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease.
In Formula (I), R 1 , R 2 , R 3 , R 4 , R 3′ , R 10 and R...
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7153846 |
Bengamide derivatives, process for preparing them, and their use
The present invention relates to bengamide derivatives which are formed, during fermentation, by the microorganism Myxococcus virescens ST200611 (DSM 15898), to their use for treating cancer...
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7141561 |
Substituted diaryl heterocycles, process for their preparation and their use as medicaments
This invention discloses and claims diary heterocycles of formula (I)
and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using said compounds of...
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7087596 |
2-oxo-piperidinyl- and 2-oxo-azepanyl alkanoic acid derivatives for the treatment of epilepsy and other neurological disorders
This invention relates to new 2-oxo-piperidinyl- and 2-oxo-azepanyl alkanoic acid derivatives of formula (1) having anticonvulsant activity which are useful as therapeutic agents for the treatment...
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7001899 |
Interleukin converting enzyme inhibitors
The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula:
wherein each X is independently selected from:
i)...
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6992103 |
Benzamide derivatives, processes for their preparation, and their pharmaceutical use
The present invention relates to novel hydroxyethylene compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them...
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6953788 |
3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase
The present invention relates to certain novel 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase. Pharmaceutical compositions...
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6906056 |
Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions...
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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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6894041 |
Oxazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6869945 |
Pyrrolyl-and imidazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6770640 |
1-Carboxymethyl-2-oxo-azepan derivatives useful as selective inhibitors of MMP-12
The present invention relates to certain novel 1-carboxymethyl-2-oxo-azepan derivatives of the formula useful as inhibitors of matrix metalloproteinases (MMPs). The compounds of formula (1) are...
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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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6667301 |
Heterocyclylalkylamines as muscarinic receptor antagonists
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR 5 , and the other...
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6664250 |
Lactam derivatives as antiarrhythmic agents
Lactam derivatives of the formula where X is —C(═O)NR 3′ —, —NR 3′ C(═O)—, —C(═NCN)NR 3′ —, —NR 3′ C(═NCN)—, —CH 2 NR 3′ —, —CH(alkyl)NR 3′ —,...
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6599898 |
Use of certain substituted caprolactam carbonates and ethers in treating tumors
The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors...
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6555533 |
Use of certain substituted caprolactams in treating tumors
The present invention relates to certain substituted caprolactam compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for...
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6534495 |
Serine protease inhibitors
The invention relates to a compound having the formula (I): R 1 SO 2 —B—X—Z—C(O)—Y, B is a bond, an amino acid of the formula —NR—CH[(CH 2 ) p C(O)OH]—C(O)— or an ester derivative...
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6521613 |
Lactam compounds for penetration enhancement
Compounds, compositions and methods are disclosed useful for enhancing penetration of a pharmacologically active substances across skin or tissue membranes. Compounds for use in such compositions...
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6511973 |
Lactam inhibitors of FXa and method
Compound of the formula are inhibitors of the enzyme Factor Xa. These compounds are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.
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6509330 |
Hydroxamic acid containing compounds useful as ACE inhibitors and/or NEP inhibotors
Hydroxamic acids are provided which are ACE and/or NEP inhibitors and have the structure wherein R*, R and R 1 are as defined herein and A is a dipeptide preferably derived from an amino acid,...
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6503897 |
Antibacterial agents
Compounds of formula (I) are antibacterial agents wherein: R 3 and R 4 , taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated...
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6495540 |
Lactams as inhibitors of A-β protein production
This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid...
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6468996 |
Substituted hetero-polycyclic compounds as PPARα and PPAR&ggr activators
The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the...
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6458781 |
Substituted diarylalkyl amides as calcium channel antagonists
The present invention provides compounds that block calcium channels and have the Formula I: The present invention also provides pharmaceutical compositions containing the compounds of Formula I...
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6455521 |
Condensed thiophene compounds and pharmaceutical use thereof
A condensed thiophene compound of the formula (I) wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of the...
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6432983 |
Benzothiophene compounds intermediates processes and methods of use
The instant invention provides compound of formula I wherein: R 1 is —H, —OH, —O(C 1 -C 4 alkyl), —O—CO—(C 1 -C 6 alkyl), —O—CO—O(C 1 -C 6 alkyl), —O—CO—Ar in which...
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6432982 |
Benzothiophenes, and formulations and methods using same
The invention provides novel benzothiophenes of the formula: wherein R 1 is —H, —OH, —O(C 1 -C 4 alkyl), —O—CO(C 1 -C 6 alkyl), —OSO 2 (C 4 -C 6 alkyl, or —OCOAr where Ar is...
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6413954 |
Certain substituted caprolactam carbonates and ethers, pharmaceutical compositions containing them and their use in treating tumors
The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors...
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6344450 |
Lactam compounds and their use as inhibitors of serine proteases and method
Lactam inhibitors are provided which have the structure X is wherein Y is O or S and R 4 is R 7 O— or R 8 and R 1 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 8 , are as defined herein. These...
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6319917 |
Acylaminoalkenylene-amide derivatives as NK1 and NK2 antagonists
Compounds of formula I ##STR1## wherein R 1 , R 1 -R 3 , R 4 ', R 4 " and R 5 are as defined in the description, have valuable pharmaceutical properties and are effective especially as NK1 and...
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6284754 |
Pharmaceutical compositions containing 1-oleylazacycloheptan-2-one as enhancing agent of transport across biological membranes
The invention relates to pharmaceutical compositions for topical application containing at least one physiologically active agent and an effective amount of 1-oleylazacycloheptan-2-one as the human...
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6239127 |
Certain substituted caprolactams, pharmaceutical compositions containing them and a process for their preparation
The present invention relates to certain substituted caprolactam compounds of formula (I), where R 1 is (C 1 -6)alkyl or (C 3 -6)cycloalkyl; R 2 hydrogen or (C 1 -6)alkyl; X is (C 1...
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6140319 |
Vasopeptidase inhibitors to treat angina pectoris
Vasopeptidaes inhibitors, especially omapatrilat, are useful in treating and/or relieving the symptoms of angina pectoris. The vasopeptidase inhibitor may be used in combination with other...
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6066631 |
Chroman derivatives
The present invention relates to chroman derivatives of the formula (I): ##STR1## [wherin R 1 represents a hydrogen atom, a halogen atom, a C 1 -6 alkyl group, a C 1 -6 alkoxy group, a C 3 -6...
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5929067 |
1-aryl-2-acylamino-ethane compounds and their use as neurokinin especially neurokinin 1 antagonists
1-Aryl-2-acylaminoethane compounds of formula I ##STR1## wherein R 1 -R 4 , X and Am are as defined in the description, have valuable pharmaceutical properties and are especially effective as NK-1...
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5912242 |
N-(4-substituted-benzyl)-2-aminolactam derivatives
The present invention relates to novel N-(4-substituted-benzyl)-2-aminolactams as therapeutic agents, pharmaceutical compositions and a process of preparation.
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5773434 |
Facilitation of AMPA receptor-mediated synaptic transmission in brain as a treatment for schizophrenia
Psychotic symptoms are treated by the administration of drugs which amplify the ability of natural stimulators of AMPA receptors to enhance the mediation of excitatory synaptic response. What is...
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5753642 |
Dihydropyridazinones, pyridazinones and related compounds as fungicides
This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R1 are as defined within, compositions containing these...
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5693630 |
Phenylethyl and phenylpropylamines
Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain, m is 2 or 3, R 1 is a hydrogen atom, or a...
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5672598 |
Lactam-containing hydroxamic acids
The present invention relates to compounds that exhibit inhibitory activity against matrix metalloproteases ("MMPs"). Because MMPs are known to play a role in tissue degradation, the compounds of...
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5643904 |
Substituted hexahdryoazepinones and tetrahydrobenzazepinones
The present invention relates to novel substituted hexahydroazepinones and tetrahydrobenzazepinones of the formulae ##STR1## wherein R 1 , Z 1 , Z 2 , W 1 , W 2 , Y 1 and Y 2 are as defined...
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