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| Number | Title | Issue Date |
| 6548677 | Method of producing 2-alkyl-3-(4,5-dihydroisoxazole-3-yl)-halobenzenes A novel process for preparing the compounds of the formula I ##STR1## where: n is 0, 1 or 2; R1, R2 are C1 -C6 -alkyl; R3, R4, R5 are hydrogen or C1 -C6 -alkyl, or ... | 04/15/2003 |
| 6528653 | Thienopyrrolidinones The invention is directed to substituted thieno[2,3-b]pyrrolidin-5-ones. The compounds are useful as inhibitors of cellular production of tumor necrosis factor (TNF-) and as antiproliferative agents. These compounds are useful in the treatment or c... | 03/04/2003 |
| 6518434 | Coupling process There is provided a process for the production of a compound of formula I, ##STR1## which process comprises reaction of a compound of formula II, ##STR2## with a compound of formula III, ##STR3## wherein R1, R2, n and R3 h... | 02/11/2003 |
| 6515133 | Pharmaceutical compositions containing certain diarylimidazole derivatives Certain diaryl imidazoles act as partial agonists or antagonists for NPY receptors, in particular NPY 5 receptors. They are of use, for example in treating loss of appetite. Such compounds bear aryl groups in the 2 position. Many of the compounds are nove... | 02/04/2003 |
| 6515184 | Cyclopentane-1,3-dione derivatives, herbicidal and pesticidal compositions containing them, methods of using them to combat pests and weeds and process for the preparation thereof The present invention relates to novel bicyclic cyclopentane-1,3-dione derivatives of the formula (I) ##STR1## to a process for their preparation and to their use as pesticides and herbicides.... | 02/04/2003 |
| 6504043 | Color-stable solution of dimethylaminoacetonitrile in water and process for preparing it The present invention relates to a process for preparing a colour-stable, aqueous dimethylaminoacetonitrile solution from a formaldehyde source, dimethylamine and hydrocyanic acid, wherein the reaction mixture contains 2,4-diamino-6-phenyl-1,3,5-triazine(... | 01/07/2003 |
| 6498256 | Phosphinite-oxazolines and metal complexes thereof Compounds of formulae I and Ia, ##STR1## wherein X1 is secondary phosphino; R3 is hydrogen, a hydrocarbon radical having from 1 to 20 carbon atoms, a heterohydrocarbon radical, bonded via a carbon atom, having from 2 to 20 atoms and ... | 12/24/2002 |
| 6492528 | 1,3-dialkyl-2-imidazolidinones and a manufacturing process therefor This invention provides a convenient process for manufacturing 1,3-dialkyl-2-imidazolidinones in a direct one-step reaction from industrially available alkylene carbonate, N-alkylethanolamine or 1,2-diol, which can minimize forming solid materials and be ... | 12/10/2002 |
| 6486339 | Phosphorylated product made by heating alkylated phenol in presence of solid acid catalyst The isomerization of an alkylated phenol composition that contains an ortho-alkyl substituted phenol component to isomerize and reduce the level of ortho-alkyl substituted phenol component therein can be accomplished by heating that composition in the pre... | 11/26/2002 |
| 6486187 | N-[4-(heteroarylmethyl)phenyl]-heteroarylamines The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6 alkyl or aryl; ... | 11/26/2002 |
| 6482944 | Processes for preparing tertiary aminoalkylorganometallic compounds Processes for the preparation of haloalkylamines and tertiary aminoalkylorganometallic compounds are disclosed. The haloalkylamines can be prepared by direct reaction of an amine with an , ω-dihaloalkane or an , ω-dihaloalkene. Tertiary ... | 11/19/2002 |
| 6479531 | Gastrin and cholecystokinin receptor ligands ##STR1## Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently .dbd.N--, --N(R5)--.dbd.CH--, --S-- or --O--. n is from 1 to 4; R1 is H ... | 11/12/2002 |
| 6476233 | Transition metal-catalyzed reactions based on chiral amine oxazolinyl ligands and related compounds This invention is to develop novel transition metal catalysts for the practical synthesis of important chiral molecules. The invention emphasizes asymmetric catalysis based on chiral amine oxazolinyl ligands and related ligands. Specially, a direct asymme... | 11/05/2002 |
| 6472550 | Process for the preparation of low chloride stabilizers A process for the preparation of a stabilizer mixture containing a low amount of chloride comprising a) 50-80% by weight of tetrakis(2,4-di-tert-butylphenyl)biphenylene diphosphonite and its isomers, b) 5-25% by weight of bis(2,4-di-tert-butylphenyl)biphenylen... | 10/29/2002 |
| 6472415 | Androgen receptor suppressors in the therapy and diagnosis of prostate cancer, alopecia and other hyper-androgenic syndromes Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. The compounds bind ... | 10/29/2002 |
| 6472533 | Ligands for chiral catalysis Novel phosphine oxazoline ligands of formula (I) ##STR1## wherein m is 1, 2, 3 or 4; n, p, q, r are independently zero or 1 provided that at least one of n, p, q and r is 1; X is O, S, Se, CH2, NH; Y is N, P, As, S; R is H; a straight, branched or c... | 10/29/2002 |
| 6469167 | Process for the preparation of thiazolidine-2,4-dione derivatives An improved process for the preparation of 5-[4-[[3-Methyl-4-oxo-3,4-dihydroquinazolin-2-yl]methoxy]benzyl]thiazolidi ne-2,4-dione of formula (1) which comprises: reducing the compound of formula (2') where R represents a (C1 -C4)alky... | 10/22/2002 |
| 6455744 | Synthesis of vicinal difluoro aromatics and intermediates thereof A method of preparing vicinal difluoro aromatic compounds in high yield from hydroxy aromatic compounds and a method of preparing intermediates thereof. The hydroxy aromatic compound can be a mono-, bi- or tricyclic aromatic in which the rings are separat... | 09/24/2002 |
| 6455702 | Process for the production of N,N-carbonyl diimidazole A high purity N,N-Carbonyl diimidazole (I) is obtained by the reaction of Imidazole, general formula-II, and bis (trichloromethyl) carbonate. Synthesis of N,N-Carbonyl diimidazole (I) is described: ##STR1##... | 09/24/2002 |
| 6452044 | Benzenedicarboxylic acid derivatives New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnstic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NA... | 09/17/2002 |
| 6448260 | Endothelin receptor antagonists Novel indane and indene derivatives are described which are endothelin receptor antagonists.... | 09/10/2002 |
| 6444829 | Pyrrolidine compounds The present invention relates to a pyrrolidine compound and pharmaceutically acceptable esters and/or salts thereof. The compounds are useful as inhibitors of metalloproteases, e.g. zinc proteases, particularly zinc hydrolases, and which are effective in ... | 09/03/2002 |
| 6441015 | Tetrazole compounds as thyroid receptor ligands The present invention relates to tetrazole compounds of Formula I, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, and pharmaceutically acceptable salts of the prodrugs. ##STR1## The invention also relates to compositions comprising... | 08/27/2002 |
| 6440749 | Method of treating certain indications associated with hyperglycemia The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylatio... | 08/27/2002 |
| 6441230 | Triphos polymer compounds and acylation agent useful in their preparation Material and process of preparing such material, of the formula ##STR1## where R1 is a linker and C(R2 P(R3)2)3 group is a triphos moiety; and wherein R1 is selected from branched and linear ... | 08/27/2002 |
| 6437165 | Phosphate derivatives as immunoregulatory agents Immunoregulatory compounds are disclosed of the formula: ##STR1## as well as the pharmaceutically acceptable salts and hydrates thereof, are disclosed. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, org... | 08/20/2002 |
| 6437147 | Imidazole compounds A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for... | 08/20/2002 |
| 6437167 | Chiral stationary phases for enantiomers separation and their preparation The present invention describes new chiral stationary phases and optically active compounds therein contained. The optically active compounds contained in the stationary phases are represented by the formula of structure (I), containing at least one asymm... | 08/20/2002 |
| 6436967 | Process for preparing prodrugs of benzenesulfonamide-containing cox-2 inhibitors This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelli... | 08/20/2002 |
| 6437146 | Oxazole compounds as prostaglandin e2 agonists or antagonists Oxazole compounds of formula (I), wherein R1 is aryl which may be substituted with halogen(s), R2 is aryl which may be substituted with halogen(s), X is single bond, (a) or SO2, R3 and R4 are independ... | 08/20/2002 |
| 6433184 | Polyamide-imide having head-to-tail backbone The present invention relates to polyamide-imides having head-to-tail backbone and more particularly, to polyamide-imimdes having head-to-tail ragularity to provide excellent heat and chemical resistance, physical and mechanical properties, processability... | 08/13/2002 |
| 6433175 | Pyrroloindoles, pyridoindoles and azepinoindoles as 5-ht2c agonists A chemical compound of formula (I), wherein n is 1, 2 or 3; R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydro... | 08/13/2002 |
| 6429328 | Processes and intermediate compounds for preparing guanidine and amidine derivatives The invention relates to new compounds of general formula I ##STR1## or the pharmaceutically acceptable salts thereof, wherein X=N-R3 or CH-R4, Y=CH2 or (CH2)2, Z=O or H2 ; and R1, R2... | 08/06/2002 |
| 6429223 | Modified forms of pharmacologically active agents and uses therefor In accordance with the present invention, there are provided modified forms of nonsteroidal anti-inflammatory drugs (NSAIDs). Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits ... | 08/06/2002 |
| 6426357 | Antagonists of follicle stimulating hormone activity The present invention provides a compound of the formula: ##STR1## and methods for using the same, wherein R1, R2, R3, R4 and X are those defined herein.... | 07/30/2002 |
| 6426360 | 4,5-substituted imidazolyl compounds for the treatment of inflammation A class of compounds is described for treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula ##STR1## wherein R1 is selected from lower alkyl, lower haloalkyl, lower hydroxyalkyl, ... | 07/30/2002 |
| 6423710 | Cyclic AMP-specific phosphodiesterase inhibitors Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, a... | 07/23/2002 |
| 6423712 | 2,4-Substituted imidazolidine derivatives, their preparation, their use and pharmaceutical preparations comprising them The present invention relates to imidazolidine compounds of the formula I, ##STR1## The compounds of the formula I are valuable pharmaceutical active compounds, which are suitable, for example, for the therapy and prophylaxis of inflammatory disorders, fo... | 07/23/2002 |
| 6423709 | Methods of using novel compounds as neuro-protective agents This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.... | 07/23/2002 |
| 6420364 | Compound useful as reversible inhibitors of cysteine proteases Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel c... | 07/16/2002 |
