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| Number | Title | Issue Date |
| 7122615 | Polyanhydrides with therapeutically useful degradation products An aromatic polyanhydride having a repeating unit with structure (I) wherein Ar is a substituted or unsubstituted aromatic ring and R is a difunctional organic moiety substituted on each Ar ortho to the anhydride group. Ortho-substituted bis-aromatic dicarboxylic ac... | 10/17/2006 |
| 6972294 | Compounds, their preparation and use Disclosed are novel compounds of formula (I) wherein A1, A2, Ar, R5, R6, R8, M, Q, Y, Z, k, m and n are as defined in the specification. These compounds are useful ... | 12/06/2005 |
| 6781000 | Alpha-ketoamide inhibitors of 20S proteasome α-ketoamide compounds useful for treating disorders mediated by 20S proteasome in mammals having the following formula: wherein X2 is Ar or Ar—X3 wherein X3 is is —C═O, or —CH | 08/24/2004 |
| 6469065 | Nitrosated and nitrosylated -adrenergic receptor antagonist, compositions and methods of use The present invention describes novel nitrosated and/or nitrosylated -adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated -adrenergic receptor antagonist, and, optionally, one or mor... | 10/22/2002 |
| 6413937 | Combinations for use in increasing the potency of a substrate for multidrug resistance related protein A combination of an agent which is a substrate for multidrug resistance related protein (MRP) and an inhibitor of MRP which is a nonsteroidal anti-inflammatory drug (NSAID) or a structural analogue thereof for simultaneous, sequential or separate use for ... | 07/02/2002 |
| 6297260 | Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least o... | 10/02/2001 |
| 6291478 | Compounds of the benzylaminodiacetamide family, compositions comprising them, preparation process and uses The present application relates to novel compounds belonging to the benzylaminodiacetamide family which have good anti-irritant and soothing properties. The invention also relates to their use in a composition comprising a physiologically acceptable mediu... | 09/18/2001 |
| 6066742 | Intermediates for the preparation of duocarmycin SA and derivatives thereof, and process for the production of the intermediates Indole derivatives shown by the formulae (1), (2a) and (2b) ##STR1## (wherein R1 is a protecting group for amino group; R2 is a protecting group for hydroxyl group; R3 is a protecting group for hydroxyl group; R4... | 05/23/2000 |
| 6063807 | Cyclo-oxygenase inhibitor and amidine derivatives salts, preparation method therefor, use thereof as drugs, and pharmaceutical compositions containing said salts Cyclo-oxygenase inhibitor and amidine derivative salts, preparation methods therefor, pharmaceutical compositions containing said salts and the use thereof particularly as NO synthase and cyclo-oxygenase inhibitors, are disclosed.... | 05/16/2000 |
| 6011053 | Substituted indole-1-carbothioic acid amides as novel antiatherosclerotic agents Antiatherosclerotic agents are provided having the structure: ##STR1## wherein R is a lower alkyl of 1-6 carbon atoms, ##STR2## wherein R5, R6, and R7 are lower alkyl of 1-6 carbon atoms; and R8, R | 01/04/2000 |
| 5965745 | Indole carbamates as leukotriene antagonists Compounds of the formula ##STR1## wherein R1 AND R2 are as defined, useful in the treatment of asthma, rheumatoid arthritis, osteoarthritis, bronchitis, chronic obstructive airways diseases, psoriasis, allergic rhinitis, atopic ... | 10/12/1999 |
| 5952355 | Propenone derivatives The present invention relates to propenone derivatives represented by the following formula (I): ##STR1## wherein R1 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, or YR5 (where... | 09/14/1999 |
| 5886191 | Amidinoindoles, amidinoazoles, and analogs thereof The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W1, W2, and W3 are selected from CH and N, provided that one of W1 and W2 is... | 03/23/1999 |
| 5877202 | Indole derivatives useful to treat estrogen-related neoplasms and disorders The present invention relates to novel indole derivatives useful in down-regulating estrogen receptor expression. Also included are methods for the treatment of neoplasms or of controlling the growth of a neoplasm in a patient afflicted with a neoplastic ... | 03/02/1999 |
| 5869518 | Azacycloalkane derivatives, their preparation and their application in therapy Azacyloalkane derivatives of general formula ##STR1## in which: R1 and R2 represent a hydrogen atom, an alkyl group or a phenyl group, or R1 and R2 together form an oxo group, R3 represents a hyd... | 02/09/1999 |
| 5840726 | Heterocyclic substituted piperazinone derivatives The present invention relates to substituted piperazinone derivatives (compounds of formula (1)) or stereoisomers, or pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment ... | 11/24/1998 |
| 5817833 | Biphenylamide compounds as 5HT1D Antagonists Compounds of formula (I) or a salt thereof: ##STR1## R1 is hydrogen, halogen, C1-6 alkyl, C3-6 cycloalkyl, COC1-6 alkyl, C1-6 alkoxy, hydroxy, hydroxyC1-6 alkyl, hydroxyC1-6... | 10/06/1998 |
| 5811547 | Method for inducing crystalline state transition in medicinal substance This invention has for its object to provide a method of inducing a transition in crystalline state of a crystallizable medicinal substance with great ease and improved efficiency and uniformity on a high production scale. According to the invention, an e... | 09/22/1998 |
| 5792786 | Non-steroidal anti-inflammatory fatty acid conjugates and their therapeutic use thereof The present invention provides therapeutic conjugates which comprise a therapeutic compound bound to one to three acyl groups derived from fatty acids. The therapeutic compounds are preferably non~steroidal anti~inflammatory agents which include a carboxy... | 08/11/1998 |
| 5747521 | N-cinnamoyl-2-methyl-5-methoxy-3-indoleacetic acid ester, and pharmaceutical preparation containing the same The present invention relates to a new N-cinnamoyl-2-methyl-5-methoxy-3-indoleacetic ester represented by the following general formula (I). It is manufactured by causing N-cinnamoyl-2-methyl-5-metboxy-3-indoleacetic acid represented by the following... | 05/05/1998 |
| 5698364 | Dyes and dye receiver elements for thermal dye transfer recording Dye-donor element for thermal dye transfer comprising at least one magenta dye having extremely low side absorption in the blue and red regions of the spectrum, said dye corresponding to the general formula (I) : ##STR1## wherein R1 is H, ... | 12/16/1997 |
| 5498729 | Prodrug compositions Compositions degrading by hydrolysis to release a bioactive compound having carboxylic acid moieties, which are organic acid anhydrides having the following formula: ##STR1## wherein R' is a residue of a therapeutic bioactive compound, for example, ... | 03/12/1996 |
| 5480999 | Dual inhibitors of NO synthase and cyclooxygenase, therapeutical compositions containing them The invention relates to compounds of the general formula AB, which may be a salt or an amide, wherein: A represents a cyclooxygenase inhibitor having an accessible acidic function and B represents the L-form of arginine analogues of the formula ##STR1## ... | 01/02/1996 |
| 5466824 | Divalent metal complexes of indomethacin, compositions and medical methods of use thereof The present invention provides a process for the preparation of a complex of indomethacin and a divalent metal comprising forming a solution by dissolving indomethacin and a salt of said divalent metal in a tertiary amide or cyclic tertiary amide, adding ... | 11/14/1995 |
| 5436265 | 1-aroyl-3-indolyl alkanoic acids and derivatives thereof useful as anti-inflammatory agents Compounds of the structures shown below are specific inhibitors of cyclooxygenase-2 useful in the treatment of cyclooxygenase-2 mediated disease states such as inflammation, pain and fever, and are non-ulcerogenic. ##STR1##... | 07/25/1995 |
| 5348976 | Condensed heterocyclic derivatives and agricultural or horticultural fungicides containing the same The present invention provides a condensed heterocyclic derivative represented by a formula: ##STR1## wherein R1 represents a lower alkyl group, an alkenyl group, or the like, R2, R3, R4, R5, and... | 09/20/1994 |
| 5310936 | Preparation of divalent metal salts of indomethacin The present invention provides a method for the treatment of inflammation and pain in a mammal requiring such treatment, comprising administering to said mammal an anti-inflammatory and analgesically effective amount of an indomethacin salt of a divalent ... | 05/10/1994 |
| 5283251 | Indole derivatives Indole derivatives of the following formula: ##STR1## wherein R1 is carboxy(lower)alkyl or protected carboxy(lower)alkyl, R2 is hydrogen, lower alkyl or halogen, R3 and R4 are each hydrogen or lower alkyl, R5 | 02/01/1994 |
| 5177223 | Indoleacetic acid derivatives, process for their preparation, and medicines containing same as active ingredients The present invention relates to an indoleacetic acid derivative and a salt thereof expressed by the following formula (I): ##STR1## [wherein X denotes a piperidino group, 1-pyrrolidinyl group or 3-hydroxy-1-pyrrolidinyl group; Y denotes ##STR2#... | 01/05/1993 |
| 5073641 | Prodrug derivatives of carboxylic acid drugs Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R1 and R2 are the same or different and ... | 12/17/1991 |
| 4920145 | Water-soluble complexes of water-insoluble pharmaceutical compounds and preparation thereof A method for increasing the water-solubility of highly insoluble organic compounds by forming a novel complex product from the reaction between the organic compound and an oligomer of vinylpyrrolidone. The complex is highly stable and results in solubilit... | 04/24/1990 |
| 4918094 | Carboxamide derivatives of indoles and leucotriene antagonizing use thereof This invention provides a series of novel heterocyclic amides of formula I in which the group >X-Y-Z< is selected from >C.dbd.CH--NC.dbd.N--NN--(CH2)--NCH--CH2 --N< and >N--N.dbd.C< and the other radicals have the meaning... | 04/17/1990 |
| 4868201 | Indoleacetic acid derivatives used as anti-inflammatories 1-(fluoro- or perfluoro lower alkyl-substituted benzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid carboxymethyl ester is found to have antiinflammatory and analgestic activity with less side effects on gastrointestinal traces than its homologue, acemata... | 09/19/1989 |
| 4851426 | Ethoxycarbonyloxy ethyl esters of non-steroidal anti-inflammatory carboxylic acids and pharmaceutical compositions thereof Novel esters of the general formula ##STR1## in which ##STR2## is the acyl residue of a non-steroidal anti-inflammatory compound containing a carboxylic acid function. The novel esters are prepared by reacting an acide R--COOH when R is as ... | 07/25/1989 |
| 4803284 | Processes for the preparation of 3-amino-2-(5-methoxy-1H-indol-3-yl) propionic acid monohydrate The compound characterized by the structural Formula I: ##STR1## is therapeutically useful as an anti-hypertensive agent. A process for the preparation of the compound having Formula I and their synthetic intermediates is described. One of the synthe... | 02/07/1989 |
| 4783487 | N-(1-carboxy-2-hydroxy-5-phenyl)-2-(6-methoxy-2-naphthyl)propionamide and anti-inflammatory use thereof Amide derivatives of non-steroidal anti-inflammatory carboxylic acids which have anti-inflammatory activity in their own right as well as being effective as pro-drugs of the carboxylic acids.... | 11/08/1988 |
| 4658039 | Process for the preparation of alkenyl esters of acemetacin The new indole derivatives of the formula ##STR1## in which R1 and R2 are identical or different and denote hydrogen or lower alkyl, R3 denotes hydrogen, lower alkyl or halogen and R4 and R5 are ident... | 04/14/1987 |
| 4652659 | Method for the production of acemetacin 1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid carboxymethyl ester as known per se is obtainable by a novel and more simple method comprising mild acid hydrolysis of 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetoxyacetic tet... | 03/24/1987 |
| 4603217 | Ester substituted alkyl-2-(2,6-dichloroanilino)phenyl acetates A novel anti-inflammatory drug, which exhibits rapidly a pharmacological activity, maintains the activity for a long time, and is free from a side effect such as a gastrointestinal disorder or a central nervous disturbance is disclosed. The drug comprises... | 07/29/1986 |
| 4532249 | Derivatives of p-acylaminophenol having a therapeutic action, and compositions having a therapeutic action containing said derivatives as pharmacologically active ingredients New acyl derivatives of p-aminophenol and esters of same useful as pharmacologically active ingredients and process for their preparation.... | 07/30/1985 |
