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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...
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...
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
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...
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...
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.
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...
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...
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...
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...
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...
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...
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)...
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...
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...
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...
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,...
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...
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...
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...
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...
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...
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′ —,...
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...
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...
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...
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...
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.
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,...
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...
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...
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...
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...
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...
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...
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...
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...
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...
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...
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...
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...
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...
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...
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...
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.
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...
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...
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...
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...
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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