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7557112 |
Aromatic-ring-fused pyrimidine derivative
There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a...
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7435732 |
Crystalline polymorphs of (3S)-N-hydroxy-4-({4-[-(4-hydroxy-2-butynyl)oxy]phenyl}sulfonyl)-2,2-dimethyl-3-thiomorpholine carboxamide
This invention relates to crystalline polymorphs of (3S)-N-hydroxy4-({4-[(4-hydroxy-2-butynyl)oxy]phenyl}sulfony
l)-2,2-dimethyl-3-thiomorpholine carboxamide, and preparation and uses thereof.
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7381260 |
Thiazineindigo pigment dispersant, and pigment composition, colored composition and color filter, using the same
A thiazineindigo pigment dispersant represented by Formula (1) or (2):
where E denotes a basic group. A pigment composition contains a pigment material, and the thiazine indigo pigment...
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7323563 |
Hydroxamic acid derivatives as antibacterials
A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a...
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7282496 |
Allenic aryl sulfonamide hydroxamic acids as matrix metalloproteinase and TACE inhibitors
Compounds of the formula
are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis,...
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7183276 |
Azole compounds
The present invention provides a compound represented by the formula (I)
wherein R 1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group, an optionally substituted...
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7179911 |
Method for preparing hydroxamic acids
Processes for using a compound of formula III:
to make compounds of formulae I and II:
and processes for making the compound of formula III, where R 1-5 and J are as defined herein.
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7166590 |
Amino acid derivatives
A compound of the formula (I):
[wherein R 1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO 2 ; R 2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO,...
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7122675 |
Gamma secretase inhibitors
Novel aryl and heteroaryl sulfonamides are disclosed. The sulfonamides, which are gamma secretase inhibitors, are represented by the formula:
wherein Ar 1 and Ar 2 independently represent...
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7022846 |
Metabolites of prinomastat and their synthesis
Metabolites of a matrix metalloproteinase inhibitor prinomastat and their synthesis. These metabolites are:...
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6849732 |
Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses, and methods and intermediates useful for their preparation
The invention relates to compounds of the formula 1 :
wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring...
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6685617 |
Inhibitors of α4β1 mediated cell adhesion
The present invention relates to compound of formula (I), that are potent inhibitors of α 4 β 1 mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of...
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6599902 |
5-aralkysufonyl-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives as kinase inhibitors
The present invention relates to certain 5-aralkylsulfonyl-3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions...
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6500948 |
Metalloproteinase inhibitors-compositions, uses preparation and intermediates thereof
The invention relates to compounds of the formula 1: wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms...
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6492421 |
Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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6472404 |
HIV protease inhibitors
The present invention discloses novel isoquinoline carboxamide derivatives which are HIV protease inhibitors or prodrugs thereof, a process for their manufacture, pharmaceutical compositions and...
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6472527 |
Process for the preparation of thiazine-indigo compounds and of new intermediates therefor
New heterocyclic compounds are disclosed which are used as intermediates for the preparation of trans-thiazine-indigo pigments which are in part new compounds and can be used for the mass...
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6436980 |
Peptidomimetic efflux pump inhibitors
Compounds are described which have efflux pump inhibitor activity. Also described are methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such...
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6387896 |
Bicyclic oxazolidinones as antibacterial agents
The present invention provides compounds of formula I useful as antimicrobial agents wherein W, X, Y, R 1 , R 2 and n are as defined in thereof.
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6384219 |
1H-pyrrolo-&lsqb 1,2-b&rsqb &lsqb 1,2,4,&rsqb triazole compound and its synthetic intermediate, and method of preparing a 1H-1,2,4-triazole-5-yl-acetic acid ester compound
There is disclosed a 1H-pyrrolo-[1,2-b][1,2,4]triazole compound represented by formula (I): wherein R is an alkyl group; R 1 , R 2 , R 3 , R 1 ′, R 2 ′, and R 3 ′ each are a hydrogen atom...
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6365587 |
Substituted aryl hydroxamic acids as metalloproteinase inhibitors
The present application describes novel substituted aryl hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from...
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6355640 |
Pyrazolopyridine adenosine antagonists
The present invention relates to a novel pyrazolopyridine compound of the following formula: wherein R 1 is aryl, and R 2 is cyclo(lower)alkyl which may have one or more suitable...
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6265228 |
Process for preparing combinatorial amide alcohol libraries
Combinatorial chemical libraries of the Formula [S]--C(O)--L'--Z containing dihyroxy amides and hydroxyphosphonate amides are disclosed, in which [S] represents a solid support and --L'--Z is a...
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6262060 |
Azacycloalkane derivatives, preparation and therapeutic application
The invention relates to azacycloalkane derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to methods for the treatment of hyperglycaemia, diabetes,...
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6255305 |
Substituted triazolo-pyridazine derivatives as ligands for GABA receptors
Substituted triazolo-pyridazine derivative compounds represented by ##STR1## wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the α2 and/or...
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6159973 |
Aromatic amides, their preparation process, the compositions containing them and their use as pesticides
The subject of the invention is the compounds of formula (I): Q(CH 2 ) a --(X 1 ) b --Q 1 --Q 2 --C(X 2 )--N(R 1 )(R 2 ) (I) in which: Q represents an aryl...
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6133290 |
5-HT.sub.1F agonists
The present invention relates to a compound of formula I: ##STR1## or a pharmaceutical acid addition salt thereof; which are useful for activating 5-HT 1F receptors and inhibiting neuronal protein...
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6127357 |
N-((phenyl, benzodioxinyl or N-heteroarylpiperazinyl)alkyl)-N-(N-heteroaryl)substituted carboxamides
Piperazine derivatives of formula I ##STR1## and their pharmaceutically acceptable acid addition salts are 5-HT 1A binding agents, particularly 5-HT 1A antagonists and may be used, for example,...
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6117870 |
Cyclic amide derivatives
A cyclic amide derivative of formula (I): ##STR1## wherein R 1 represents a substituted alkyl group, a substituted alkenyl group, a substituted amino group, a substituted alkoxyl group, a...
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6080738 |
Heterocyclic amide compounds and medicinal uses thereof
A heterocyclic amide compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof...
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6071909 |
Phenylbenzimidazole derivatives as ligands for GABA receptors
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5985873 |
Certain substituted benzylamine derivatives a new class of Neuropeptide-Y1 specific ligands
This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein X 1 , X 2 , X 3 represent organic or inorganic substituents, n is 1, 2, or 3,...
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5981523 |
Compounds and methods for treating multiple sclerosis
This invention provides thiomorpholinone compounds useful for treating multiple sclerosis of formula I wherein: R 1 and R 2 are each independently selected from C 1 -C 8 alkyl; C 2 -C 8 ...
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5948785 |
Heterocyclic amide compounds and pharmaceutical use of the same
Heterocyclic amide compounds of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmacologically acceptable salts thereof, pharmaceutical compositions thereof and...
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5886175 |
7-(substituted)-8-(substituted)-9-(substitued amino)-6-demethyl-6-deoxytetracyclines
The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.
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5877119 |
Substituted pyridine compounds
Disclosed herein are herbicidal pyridine compounds substituted at the 2- or 6-position with an OR 2 moiety where R 2 is hydrogen, lower alkyl, halomethyl, lower cyanoalkyl, alkenyl or alkynyl, as...
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5863913 |
Aromatic compound and pharmaceutical composition
An aromatic compound of the formula (I): ##STR1## specifically, for example, 3- (4-carboxyphenyl)methyl!valeramido!-4-dimethylaminobenzoic acid 4'-methylpiperazide, or a salt thereof, and a...
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5817671 |
5-HT.sub.1F agonists
This invention provides 5-HT 1F agonists of Formula I: ##STR1## where A--B, X, and R are as defined in the specification. The invention also encompasses pharmaceutical formulations employing...
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5739131 |
Benzene derivatives and pharmaceutical composition
A benzene derivative of the formula (I): ##STR1## wherein R 1 is hydrogen, C 1 -6 -alkyl, C 1 -6 -haloalkyl, --NH 2 , --NHR 21 ; R 2 is hydroxyl, --OR 22 , three- to seven-membered saturated...
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5674864 |
N-substituted derivatives of α-mercapto alkylamines, their preparation process and the intermediates obtained, their use as medicaments and the compositions containing them
Novel α-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein the substituents are as defined in the specification.
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5556853 |
Epoxysuccinic acid derivatives
A compound of the general formula: ##STR1## wherein R 1 represents a carboxyl group which may optionally be esterified or amidated; R 2 represents a cyclic group which may optionally be...
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5556841 |
Thiazine or thiomorpholine derivatives
This invention relates to the compounds of the formula [I] which are useful for the treatment of cataracts, and the synthetic intermediates of the formula [II], ##STR1## wherein R 1 is hydroxy...
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5552543 |
Six-membered hetero "N" compounds
Novel six-membered hetero "N" compounds having antibiotic activity, represented by the formula: ##STR1## where XS, O, CH 2 , or Se YOH, NH 2 , NHCOR 9 , or SH R 1 ,R 2 ,R 3 ,R 4 ,R 5 ,R...
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5506242 |
Arylsufonamido-substituted hydroxamic acids
The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which...
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5504082 |
Pyridine compound and pharmaceutical compostions
A pyridine compound of the formula ##STR1## wherein R 1 is a hydrogen, a halogen, an alkyl, an alkoxy or the like, R 2 and R 3 are each a hydrogen, a halogen or an alkyl, --PQ-- is...
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5500422 |
Benzamide derivative
A benzamide derivative represented by the following formula: ##STR1## wherein R 1 represents a hydrogen atom or a lower alkanoyl group; R 2 represents a hydrogen atom or a halogen atom; R 3 ...
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5489693 |
Cyclic imino derivatives, pharmaceutical compositions containing these compounds and processes preparing them
Cyclic imino derivatives of the formula ##STR1## wherein X and R a to R g are as defined herein, useful for their inhibitory effects on aggregation, pharmaceutical compositions containing the...
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5482957 |
Azole derivatives, process for their preparation and their use
Azole derivatives, process for their preparation, and their use Azole derivatives of the formula (I) ##STR1## in which A, L, O, R 1 , X, Y, Z and q have the meanings given, process for their...
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5475106 |
N-phenylglycinamide CCK antagonists and pharmaceutical compositions containing them
Compounds of formula: ##STR1## in which R 1 represents a hydrogen atom, an alkyl or alkoxycarbonyl radical or a phenyl radical, optionally substituted, R 2 represents an alkoxy, optionally...
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5446062 |
((4-alkoxypyran-4-yl) substituted) ether, arylalkyl-, arylalkenyl-, and arylalkynyl)urea inhibitors of 5-lipoxygenase
Compounds of the structure ##STR1## where W is selected from ##STR2## where Q is oxygen or sulfur, R 6 and R 7 are hydrogen or alkyl, or R 6 and R 7 , together with the nitrogen atoms to which...
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