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7495126 |
Process of preparation of substituted tetrafluorobenzylaniline compound and its pharmaceutically approved salts
This invention relates to a method for preparing tetrafluorobenzyl-5-aminosalicylic acid derivative and its pharmaceutically acceptable salt compounds. In particular, this invention relates to a...
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7408078 |
Anthranilic acid derivatives useful in treating infection with hepatitis C virus
The present invention provides pharmaceutical compositions useful in treating hepatitis C infection. The present invention also provides methods of treating hepatitis C infection by administering...
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7378546 |
Method for producing 2-amino-5-iodobenzoic acid
A method for producing 2-amino-5-iodobenzoic acid which comprises bringing 2-aminobenzoic acid (A) and molecular iodine (B) into reaction with each other in the liquid phase in the presence of an...
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7371867 |
Non-racemic trifluoroleucine, and methods of making and using
One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the invention relates to the synthesis of protein cores...
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7321044 |
Synthesis of oxygen-substituted benzocycloheptenes as valuable intermediate products for the production of tissue-selective estrogens
The invention relates to intermediate products and a new process for the production of benzocycloheptene C.
The process for the production of its new intermediate products according to the...
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7202364 |
Certain phenylacetic acids and derivatives
Compounds of formula (I)
wherein
R is hydrogen, lower alkyl, (C 3 –C 6 )cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally...
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7132559 |
Non-racemic hexafluoroleucine, and methods of making and using it
One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the nvention relates to the synthesis of protein cores...
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7115662 |
Certain 5-alkyl-2-arylaminophenylacetic acids and derivatives
Disclosed are the compounds of formula I
wherein R is methyl or ethyl; R 1 is chloro or fluoro; R 2 is hydrogen or fluoro; R 3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or...
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7019033 |
2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives
Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula
where R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are hydrogen or substituent groups such as alkyl, and...
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7015349 |
Reduction of hair growth
Compositions including a conjugate of α-difluoromethylornithine can be applied topically to reduce hair growth.
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7001905 |
Substituted diarylamines as MEK inhibitors
Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C 1-6 alkoxy, or NR 6 OR 7 ; X is OR 12 , NR 13 R 12 , or NR 14 ; inhibitors of MEK and...
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6974595 |
Pharmaceutical compositions based on Diclofenae
New pharmaceutical compositions for oral use containing Diclofenac together with alkali metal bicarbonates in amounts of from 20 to 80 by weight with respect to Diclofenac are described. These...
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6900244 |
Anilino liver X-receptor modulators
The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is...
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6727281 |
Certain 5-alkyl-2-arylaminophenylacetic acids and derivatives
Disclosed are the compounds of formula I wherein R is methyl or ethyl; R 1 is chloro or fluoro; R 2 is hydrogen or fluoro; R 3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or...
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6727250 |
Carboxylic acid amides, pharmaceutical compositions containing these compounds, their use and preparation
Carboxylic acid amides of general formula which inhibit telomerase and are useful for treating tumor diseases such as carcinomas, sarcomas and leukaemias. Exemplary compounds are: (1)...
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6686499 |
Method for making 2-(N-phenylamino)benzoic acids
The present invention relates to a method for making 2-N-phenylamino)benzoic acids by coupling a benzoic acid and an aniline using an alkaline metal hexamethyldisilazide as a base.
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6677479 |
Substituted fluoroaromatics, process for preparing them and their use
Compounds of the formula (I) and also process for preparing them where substituents X 1 , X 2 , Y and Z are defined as follows: X 1 is H or F X 2 is H or F Y is CI, Br, or I Z is CHO or COOH...
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6573252 |
Medicine nitrate salts
The present invention relates to nitrate salts of compounds having therapeutic activity in bony disorders, such compounds being characterized in that they contain at least a reactive group capable...
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6521794 |
Method for production of aromatic compounds
For the production of an aromatic compound by hydrolyzing and decarboxylating a corresponding aromatic cyano compound in the presence of an acidic substance, this invention provides a method for...
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6504052 |
Excitatory amino acid receptor modulators
Compounds of the formula (I) in which R 1 is C 1-10 allyl; C 2-10 alkenyl; C 2-10 alkynyl; phenyl-C 2-10 alkyl or phenyl-C 2-10 alkenyl; and salts and esters thereof, modulate metabotropic...
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6369270 |
Benzoic acid intermediates to 4-benzoylisoxazole herbicides
Compound of the formula are useful as intermediates to new 4-benzoylisoxazoles.
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6274762 |
Preparation of tri-iodo benzene compounds
The invention provides an improved process for the preparation of a compound containing a 2,4,6-triiodinated benzene ring, said process comprising reacting a 2,4,6-unsubstituted 5-amino-benzoic...
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6258982 |
Process for the preparation of substituted aromatic amino compounds
The present invention relates to a hydrogenation process for the preparation of aromatic amino compounds containing directly on the aryl ring or in a side chain one or more entities that may also...
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6172058 |
Compounds with pharmaceutical properties
A pharmaceutical compound of the formula ##STR1## in which R 1 is C 1 -10 alkyl, C 2 -10 alkenyl, C 2 -10 alkynyl, C 3 -10 cycloalkyl, C 3 -10 cycloalkyl-C 1 -10 alkyl, C 3 -10 cycloalkyl-C 2 -10...
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6168913 |
Coding combinatorial libraries with fluorine tags
The present invention relates to coding combinatorial chemical libraries synthesized on a plurality of solid supports by attaching "tags" that comprise fluorine containing compounds in combinations...
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6137003 |
Bis (haloethyl) aminobenzene derivatives
The present invention relates to bis(haloethyl)aminobenzene derivatives featured by having carboxyl-containing moiety and one other moiety at the ortho position with respect to the...
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6127392 |
Anthranilic acid analogs
Compounds of the formula: wherein: R 1 , R 2 , R 3 , R 4 ,R 5 , R 6 , R 7 and R 8 are, independently, hydrogen, COOR 15 , halogen, nitro, cyano, C 1 -10 alkoxy, C 1 -10 haloalkoxy, sulfonic...
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6114386 |
Inhibitors of bacterial sialidase
A sialidase inhibitor of the shown formula I: ##STR1## where dashed lines d 1 and d 2 , X 1 , R 1 , R 2 , R 6 , R 3 , R 4 and R 5 are as described in the specification; or an analog,...
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5945556 |
Process for preparing N-carboxymethylene-4-chloro-anthranilic acid and its dialkyl esters
A process for preparing N-carboxymethylene-4-chloroanthranilic acid, and its dialkyl esters. The invention relates to a process for preparing N-carboxymethylene-4-chloroanthranilic acid and its...
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5916922 |
Phenyl glyoxamides as SPLA2 inhibitors
A class of novel phenyl glyoxamides is disclosed together with the use of such compounds for inhibiting sPLA 2 mediated release of fatty acids for treatment of conditions such as septic shock.
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5821385 |
Process for the preparation of N-(2-carboxy-5-chloro-phenyl)glycine
The present invention relates to a process for the preparation of N-(2-carboxy-5-chloro-phenyl)glycine of the formula (1) ##STR1## which comprises reacting 2,4-dichlorobenzoic acid of the formula...
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5773651 |
Process for the preparation of fluorine-containing chemical compounds
Process for the preparation of fluorine-containing compounds by reduction in a container provided with a stirrer, the stirrer being constructed entirely or partly of a carbon material.
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5763481 |
Vinylcarboxylic acid derivatives
Compounds of the formula ##STR1## wherein R 1 is C 3 -C 8 cycloalkyl, halo-C 3 -C 8 cycloalkyl, C 3 -C 8 cycloalkyl-C 1 -C 6 alkyl, halo-C 3 -C 8 cycloalkyl-C 1 -C 6 alkyl, --Si(R 3 )...
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5763650 |
Process for the preparation of a halosubstituted aromatic acid
The present invention refers to a process for the preparation of 5-amino-2,4,6-triiodo-1,3-benzenedicarboxylic acid, comprising the following steps: a) catalytic hydrogenation of...
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5744638 |
Process for the preparation of haloanthranilic acids
The present invention relates to a process for the preparation of compounds of the general formula I ##STR1## in which X and Y, independently of each other, represent hydrogen, fluorine, chlorine...
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5739169 |
Aromatic compounds for inhibiting immune response
Novel compounds ##STR1## wherein R 1 to R 13 are independently selected from C 2 -C 4 linear and branched alkyls, H, NH 2 , CH 3 , OR 14 , fluorine, chlorine, iodine, NO 2 , CF 3 , NHCOCH 3 ,...
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5717109 |
Excitatory amino acid receptor antagonists
The present invention provides compounds of formula ##STR1## in which R represents an organic group, or a pharmaceutically acceptable metabolically labile ester or amide thereof, or a...
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5672708 |
Process for the preparation of N-arylaminoacrylic acid derivatives and the use of N-arylaminoacrylic acid derivatives thus prepared for the preparation of 4-quinolone-3-carboxylic acid derivatives
N-arylaminoacrylic acid derivatives are obtained in good yields and in high purities when benzoylacetic acid derivatives are reacted with N-arylimino ethers. The products thus prepared are used, in...
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5550291 |
Process for key intermediates for HIV protease inhibitors
Disclosed herein is a stereospecific synthesis amenable to the large scale preparation of a hydrochloric acid addition salt of a chlorohydrin of the formula ##STR1## wherein R 1 and R 2 are amino...
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5543550 |
Process for the preparation of 5-fluoroanthranilic alkyl esters and/or 5-fluoroanthranilic acid
The present invention relates to a process for the preparation of 5-fluoroanthranilic alkyl esters and/or 5-fluoroanthranilic acid, which comprises dissolving a 3-fluorobenzoic alkyl ester in...
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5527956 |
Process for the oxidation of aromatic methyl groups
Fluro-substituted aromatic carboxylic acids, and particular 2- and 4-fluorobenzoic acid can be made from the corresponding fluoro-methyl compound such as fluorotoluene in a single stage by the...
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5523476 |
Processes for producing tetrafluorophthalic anhydride and fluorobenzoic acids
A process for producing tetrafluorophthalic anhydride, which comprises chlorinating tetrachlorophthalic anhydride to obtain 3,3,4,5,6,7-hexachloro-1-[3H]-isobenzofuranone, then fluorinating it to...
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5523472 |
Process for the preparation of 5-fluoroanthranilic acid
The present invention relates to a process for the preparation of 5-fluoroanthranilic acid, which comprises reacting 5-fluoro-2-bromotoluene in the presence of a catalyst and of an acidic solvent,...
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5482942 |
(3,4-dioxocyclobuten-1-yl)chromene, indene, and dihydronaphthalenone derivatives as smooth muscle relaxants
This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to...
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5475132 |
Antifungal agents based on amides containing a phenyl group
R 3 , R 4 and R 5 , each represents a hydrogen or halogen atom (at least one of R 3 , R 4 and R 5 being other than hydrogen or halogen); optionally substituted amino; optionally halogenated or...
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5385917 |
Carboxylic acid derivatives
Carboxylic acid derivatives of the formula: ##STR1## are provided, which are useful for treatment of androgen dependent diseases.
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5359120 |
Improvements relating to the production of prodrugs
The invention provides compounds of the formula XX: M-Ar-CONH-R, where Ar represents an aromatic ring system, R-NH is the residue of an α-amino acid R-NH 2 or oligopeptide R-NH 2 and contains at...
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5344959 |
Tetrahydronaphthyl and cyclopropyl substituted 1,3-butadienes having retinoid-like activity
Compounds of the formula ##STR1## wherein m is 1-4; R 1 -R 4 independently are hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, or I; R 5 is hydrogen, lower alkyl of 1 to 6 carbons, Cl, Br, I,...
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5334747 |
Method of preparing substituted malonic ester anilides and malonic acid mono-anilides
Malonic mono-ester mono-anilides and malonic acid mono-anilides and bis-anilides are produced by reaction of malonic acid di-alkyl esters with an aniline in the presence of a stoichiometric amount,...
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5324747 |
N-substituted anilines, inhibitors of phospholipases A.sub.2
Compounds of the formula ##STR1## wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , n, m, o, p and q are as hereinafter set forth, and, when R 2 is hydrogen, pharmaceutically acceptable...
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