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| Number | Title | Issue Date |
| 7332504 | Heterocyclic substituted aminoazacycles useful as central nervous system agents Heterocyclic substituted aminoazacyclic compounds of formula I Z-R3I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions ... | 02/19/2008 |
| 7253171 | Urea derivatives as integrin α4 antagonists Novel antagonists of ∝4β1 integrin and/or ∝4β7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents —CH— or a nitrogen atom, and p is from 0 to 4. ... | 08/07/2007 |
| 7160880 | Short-acting benzodiazepines The present invention provides a compound of formula (I): wherein all variables are as defined herein, pharmaceutical formulations containing the same, processes for preparing the same and their use therapy. ... | 01/09/2007 |
| 7151097 | Bicyclic pyrazolyl and imidazolyl compounds and uses thereof Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of the cannabinoid... | 12/19/2006 |
| 7122662 | Tricyclic compound having spiro union This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which e... | 10/17/2006 |
| 7109233 | Protease inhibitors This invention relates in general to certain substituted substituted 1,1,4-1l6-trioxo[1,2]thiazepan-4-ylamides of formula I as defined herein which are protease inhibitors. ... | 09/19/2006 |
| 7078409 | Fused quinazoline derivatives useful as tyrosine kinase inhibitors The present invention is directed to a compound having the structure wherein A is a 7–18 membered ring that comprises 0 to 6 heteroatoms selected from O, S, and N; R1 is selected from the group consi... | 07/18/2006 |
| 7060698 | Benzoxazepinone derivatives The invention relates to benzoxazepinone derivatives of formula wherein R1, R2, R3, R4, and n are as defined in the specification and... | 06/13/2006 |
| 7053123 | Substituted (e)-styryl benzylsulfones for treating proliferative disorders (E)-Styryl benzylsulfones useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: R1 is selected from the group consisting of halogen, C1–C6 alkoxy, nitro, phosphonato, amino, sulfamyl... | 05/30/2006 |
| 7030107 | Fused bicyclic pyridine derivatives as tachykinin receptor antagonists A novel fused bicyclic pyridine derivative or a salt thereof that acts as a tachykinin receptor antagonist, in particular as an NK1 receptor antagonist, is represented by the following general formula (1): ... | 04/18/2006 |
| 7026501 | Inhibitors of α4 mediated cell adhesion The present invention relates to a phenylalanine derivative of Formula (I) wherein X1 is a halogen atom, X2 is a halogen atom, Q is a CH2R— is a carboxyl group which may be esterified; or a pharmaceutically acceptable salt thereof.... | 04/11/2006 |
| 7026309 | Fused bicyclic pyridine derivative as tachykinin receptor antagonist A fused bicyclic pyridine derivative represented by the following general formula (1), or a salt thereof: wherein the rings A and B are each a benzene ring, which may have 1 to 3 substituents (a... | 04/11/2006 |
| 7014981 | Benzoindole styryl compounds and their uses in high-density recording media The invention discloses new benzoindole styryl compounds and its use for a high-density optical recording medium. The invention uses the dyes of the new benzoindole styryl compounds to form the recording layer of high-density recording media. The new benzoindole sty... | 03/21/2006 |
| 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 general formula (1): wherein... | 02/07/2006 |
| 6953798 | β-alanine derivates Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra′)R (1) Ar1 is an optionally substituted aromatic or... | 10/11/2005 |
| 6911451 | Phenylalanine derivatives Phenylalanine derivatives of formula (1) are described: wherein L1 is a linker atom or group; X1 is a group selected from —N(R3)CO—, —N(R3)SO | 06/28/2005 |
| 6908934 | Therapeutic compounds for treating dyslipidemic conditions Compounds of Formula I and the pharmaceutically acceptable salts and esters thereof, wherein Z is selected from the group consisting of: (a) Formula Ia | 06/21/2005 |
| 6867298 | Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or a... | 03/15/2005 |
| 6846833 | Vitronectin receptor antagonist bicyclic compounds, preparation method and compositions containing same Compounds of formula (1): wherein: G represents an optionally substituted phenyl or optionally substituted heterocycle, G1 and G2 being N or C, ... | 01/25/2005 |
| 6759404 | Cyclic malonamides as inhibitors of aβ protein production Novel cyclic malonamides having the formula (I): and their pharmaceutical compositions. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-pept... | 07/06/2004 |
| 6686350 | Cell adhesion inhibitors The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of us... | 02/03/2004 |
| 6613761 | Benzoxazepine compounds, their production and use This invention provides new benzoxazepine compounds represented by the formula: ##STR1## [wherein R stands for a lower alkyl group optionally substituted with a hydroxyl group, X stands for an optionally substituted carbamoyl group or an optionally s... | 09/02/2003 |
| 6537987 | 4,1-benzoxazepines or 4,1-benzothiazepines and their use as squalene synthetase inhibitors This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, anti-Alzheimer's agents or anti-acne agents.... | 03/25/2003 |
| 6506744 | Benzazepinone-derivatives Compounds of formula I ##STR1## as well as pharmaceutically usable salts and esters thereof, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be ... | 01/14/2003 |
| 6489320 | 5, 5-disubstituted-1, 5-dihydro-4, 1-benzoxazepin-2 (3H)-ones useful as HIV reverse transcriptase inhibitors The present invention relates to benzoxazepinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical composition... | 12/03/2002 |
| 6486315 | Recrystallization processes Mercaptoalkanoylamino lactam acids are recrystallized by treatment with an agent that minimizes the formation of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite.... | 11/26/2002 |
| 6458827 | Method of locking 1-OH of vitamin D compounds in axial orientation A method of modifying or altering the structure of a 1-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1-hydroxyl in... | 10/01/2002 |
| 6455522 | Cyclic sulfonamide derivatives as metalloproteinase inhibitors The present application describes novel lactams and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic sulfonamide containing from 0-3 additional heteroatoms sel... | 09/24/2002 |
| 6423840 | Inhibitors of interleukin-1ଲ converting enzyme The present invention relates to novel classes of compounds which are inhibitors of interleukin-1ଲ converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also rel... | 07/23/2002 |
| 6403578 | Bicyclic fibrinogen antagonists This invention relates to compounds of the formulae: ##STR1## wherein A1 is O, S, N--R1 or CHR1 ; A4 is N--R4 or CHR4 ; R2 is a sidechain containing an acid or ester group; R1, ... | 06/11/2002 |
| 6352982 | 4,1-benzoxazepines, their analogues, and their use as somatostatin agonists The present invention provides a compound of the formula: ##STR1## wherein ring A is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ring; ring B is an optionally substituted aromatic hydrocarbon ring or aromatic heterocyclic ... | 03/05/2002 |
| 6353099 | Substituted ureas as cell adhesion inhibitors Compounds of Formula I are antagonists of VLA-4 and/or 댔ଲ.sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical ... | 03/05/2002 |
| 6340752 | Deprotection and recrystallization processes Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosph... | 01/22/2002 |
| 6248882 | Preparation of (s)-2-amino-6,6-dimethoxyhexanoic acid methyl ester via novel dioxolanes The glycinamide of the formula ##STR1## is reacted with the dioxolane of the formula ##STR2## wherein L is a leaving group such as iodo, bromo, alkylsulfonyloxy, or arylsulfonyloxy to give the dioxolane of the formula ##STR3## Treating the dioxolane ... | 06/19/2001 |
| 6207663 | Vitronectin receptor antagonists, their preparation and use Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I A--B--D--E--F--G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as ... | 03/27/2001 |
| 6204261 | Inhibitors of interleukin-1ଲ Converting enzyme inhibitors The present invention relates to pyradazino[1,2-a][1,2]diazepine-1-carboxamide compounds of formula: ##STR1## which compounds are inhibitors of interleukin-1beta converting enzyme.... | 03/20/2001 |
| 6162913 | Preparation of [4S-(4,7,10aଲ)]-4-amino-octahydro-5-oxo-7H-pyrido[2,1 -b] [1,3]thiazepine-7-carboxylic acid, methyl ester and salts thereof via novel disulfides N-protected-L-homocysteine disulfide of the formula ##STR1## or an activated form thereof is reacted with (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester to give the disulfide intermediate of the formula ##STR2## Cleavage of the disulf... | 12/19/2000 |
| 6147071 | Cyclic compounds, their production and use Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.CC | 11/14/2000 |
| 6140320 | 5,5-disubstituted-1,5-dihydro-4,1-benzoxazepin-2 (3H)-ones useful as HIV reverse transcriptase inhibitors The present invention relates to benzoxazepinones of formula I: ##STR1## or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compos... | 10/31/2000 |
| 6114522 | Process of production of 4-substituted-3-halogeno-1,4-benzoxazepine derivative and salts thereof A process for producing 4-substituted-3-halogeno-1,4-benzoxazepin derivative or the salt thereof comprising: deprotonizing a benzoxazepine derivative having the formula (II): ##STR1## with a base; and then, reacting the deprotonized product with a p... | 09/05/2000 |