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7601712 |
Carboxylic acid compounds and medicinal compositions containing the same as the active ingredient
A compound represented by formula (I)
wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP...
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7423154 |
Asymmetric process for the preparation of diarylethylpiperazines derivatives and novel asymmetric diarylmethylamines as intermediates
An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention...
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7291621 |
Substituted biaryl amides C5a receptor modulators
Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C 5 a receptor activity in vivo or in vitro, and are particularly useful in the...
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7141674 |
Anti-inflammatory compounds
This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:
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7122561 |
Treatment of skin conditions
The present invention provides piperine and analogues or derivatives thereof for the treatment of skin conditions treatable by stimulation of melanocyte proliferation, such as vitiligo, and also...
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7119049 |
Oxathiinecarboxamides
This invention relates to novel oxathiinecarboxamides of the formula (I)
in which R, R 1 and m are as defined in the disclosure, to a plurality of processes for preparing these substances...
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7078565 |
Benzamide derivatives as antagonists of orexin receptors
Disclosed are phenyl-alkylene benzamides useful as orexin antagonists
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7067551 |
Deacetylase inhibitors
The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.
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7026339 |
Inhibitors of HCV NS5B polymerase
The present invention relates to compounds, process for their synthesis, compositions and methods for the treatment and prevention of hepatitis C virus (HCV) infection. In particular, the present...
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7019028 |
Endiandric acid H and its derivatives, process for their preparation and use thereof
The invention relates to compounds of the formula (I)
process for their preparation starting from the plant Beilschmiedia fulva , PLA 101037, and the use thereof for producing a medicament, in...
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7019024 |
Pharmaceutical for treatment of neurological and neuropsychiatric disorders
The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula:
or a pharmaceutically acceptable salt thereof.
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6878706 |
Cyanamides useful as reversible inhibitors of cysteine proteases
Compounds according to the following formula (I):
wherein the variables Q and R 1 to R 6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F,...
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6858648 |
Laetispicine and laetispicine analogues, methods of use and preparation
A compound having the following Formula:
wherein R1, R2, Z, and Y are defined herein, and methods of preparation and application for treating mental disorders and inflammation are provided...
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6849649 |
N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R 1 is optionally substituted C 1-6 alkyl, optionally substituted carbocyclyl, optionally...
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6767921 |
Polymorphic forms of fasidotril, their methods of preparation and pharmaceutical compositions comprising them
The subject of the present invention is the various polymorphic forms I, II, III, IV of benzyl (S,S)-2-(2-acetylsulphanylmethyl-3-benzo[1,3]dioxol-5-ylprop
ionyl-amino)propionate, hereinafter...
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6762318 |
Glucagon antagonists
Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.
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6730705 |
Alkoximino acetic acid amides
The invention relates to new alkoximinoacetic acid amides, a process for their preparation and their use as agents for combating pests.
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6680391 |
Treatment of skin conditions
The present invention provides piperine and analogues or derivatives thereof for the treatment of skin conditions treatable by stimulation of melanocyte proliferation, such as vitiligo, and also...
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6677456 |
Pentacyclic taxan compound
This invention is to provide a novel taxol derivative useful as an antitumor compound having respective substituent groups, represented by the following formula (I) which can be orally administered
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6638970 |
Substituted alkylene diamine compounds
Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage...
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6603044 |
Phthalamide derivatives, or salt thereof agrohorticultural insecticide, and method for using the same
The present invention provides a phthalamide derivative of the formula (I): wherein A 1 is (substituted) C 1 -C 8 alkylene, (substituted) C 3 -C 8 alkenylene, (substituted) C 3 -C 8 ...
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6515124 |
Dehydroamino acids
Aromatic dehydroamino acids are disclosed that are active as LFA-1 arnagonists This activity enables these compounds to prevent inflammation which is a consequence of T cell activation and...
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6509379 |
Phenylacetic acid derivatives, process and intermediate products for their preparation, and their use as fungicides and pesticides
Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful...
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6509369 |
Anti-inflammatory compounds
This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:
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6472414 |
Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method
Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including...
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6458801 |
Benzofurane derivatives, preparation method, use as medicines and pharmaceutical compositions containing same
A compound of the formula wherein the substituents are as defined in the specification and its pharmaceutically acceptable salts and its prodrug useful for treating osteoporosis.
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6344570 |
Substituted urea derivatives as cell adhesion inhibitors
Compounds of formula (II) where R 1 is in the para or meta position and is (A); R 2 and R 3 are each independently selected from hydrogen, nitro, C 1-6 alkyl, C 3-6 cycloalkyl, C 2-6 alkenyl,...
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6340704 |
Cell differentiation inducing amide derivatives, their production and use
The present invention provides a compound represented by the formula: wherein R 1 is an amino group which may be substituted; R 2 is a hydrogen atom or a lower alkyl group which may be...
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6323227 |
Substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides
This invention relates to compounds of formula ##STR1## which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of...
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6306873 |
Substituted β-thiocarboxylic acids
This invention relates to compounds of general formula (I): ##STR1## in which Ar is a group selected from: ##STR2## A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and...
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6303799 |
Polynucleotide crosslinking agents
Novel aryl derivatives comprising an aryl olefin moiety linked to a non-nucleosidic backbone moiety are disclosed. The resulting molecules are typically used as photoactivated crosslinking groups...
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6214870 |
Dioxocyclopentyl hydroxamic acids
The present invention relates to dioxocyclopentyl hydroxamide derivatives of the formula ##STR1## wherein X, Z and Q are as defined in the specification, and to pharmaceutical compositions and...
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6214869 |
Heterocyclic cis cyclopropane derivatives as melatonergic agents
There is provided a novel series of cis cyclopropane compounds of Formula I ##STR1## wherein R 1 , R 2 , R 3 , R 4 , X, Y, Z and m are as defined herein which bind to the human melatonin receptor...
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6214859 |
Ethylamine derivatives
Ethylamine derivatives of the formula (I): ##STR1## (wherein R 1 is hydrogen, hydroxyl, lower alkoxy or halogen; R 2 is alkyl having 2 to 5 carbon atoms; R 3 is hydrogen, alkyl having 2 to 5...
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6211240 |
O-benzyl oxime ether derivatives and their use as pesticides
Compounds of the formula I ##STR1## in which Y is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, OH, CN, NO 2 , Si(CH 3 ) 3 , CF 3 or halogen, Z is a group a) ##STR2## R 1 is hydrogen, C...
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6207686 |
Endothelin antagonists
A compound of formula (I), in which: R 1 is lower alkyl, cyclo(lower)alkyl, optionally substituted aryl, optionally substituted heterocyclic group, cyclo(lower)alkyl(lower)alkyl, or...
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6194448 |
N, N-disubstituted amides that inhibit the binding of integrins to their receptors
A method for the inhibition of the binding of α 4 β 1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding;...
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6150416 |
Nanomolar, non-peptide inhibitors of cathepsin D
The present invention provides non-peptide cathepsin D binding compounds and methods for using such compounds in the detection, labelling and inhibition of cathepsin D.
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6130251 |
Alkoximinoacetic acid amides
The invention relates to new alkoximinoacetic acid amides, a process for their preparation and their use as agents for combating pests.
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6040339 |
Urea derivatives having ACAT inhibitory activity, their preparation and their therapeutic and prophylactic use
Compounds of formula (I): ##STR1## wherein: R 1 is alkyl; R 2a , R 2b , R 2c and R 2d are the same or different and each is hydrogen, optionally substituted alkyl or various other organic...
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6011059 |
Acyl guanidine sodium/proton exchange inhibitors and method
Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure ##STR1## wherein n is 1 to 5; X is N or C--R 5 wherein R 5 is H, halo, alkenyl, alkynyl,...
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5998667 |
Substituted biphenyl oxazolines
The invention relates to new substituted biphenyloxazolines of the formula (I) ##STR1## in which R 1 represents C 1 -C 6 -halogenoalkylthio and R 2 represents hydrogen, or R 1 and R 2 ...
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5981571 |
Benzodioxa alkylene ethers as melatonergic agents
Novel derivatives of benzodioxa alkylene ethers are provided which are useful as melatonergic agents.
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5948778 |
Difluoro statone antiviral analogs
This invention relates to novel statone antiviral analogs, to the processes and intermediates useful for their preparation and to their use as antiviral agents.
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5945548 |
Process for the synthesis of α-substituted acrylic acids and their application
Process for the synthesis of α-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II). ##STR1##
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5919954 |
Stereoselective process for producing dihydro-2,3-benzodiazepine derivatives
A process for stereoselectively forming N-substituted dihydro-2,3 benzodiazepines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the...
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5880147 |
Amide derivatives having ACAT inhibitory activity, their preparation and their therapeutic and prohylactic use
Compounds of formula (I): ##STR1## wherein: R 1 is alkyl; R 2a , R 2b , R 2c and R 2d are the same or different and each is hydrogen, optionally substituted alkyl, --(CO)--B 1 (wherein B 1 ...
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5846956 |
Amino acids derivatives, the process for their preparation and their applications to therapy
Amino acid derivatives of formula (Ia) and (Ib) and pro-drugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as...
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5801197 |
Rotamase enzyme activity inhibitors
This invention relates to the method of using specially formulated neurotrophic pipecolic acid derivative compounds having an affinity for FKBP-type immunophilins as inhibitors of the enzyme...
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5770620 |
Aryl acrylic acid derivatives useful as protein tyrosine phosphatase inhibitors
The present invention provides novel protein tyrosine phosphatase modulating compounds having an aryl acrylic acid structure, compositions comprising the compounds, and methods of making and using...
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