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7482337 |
Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
Disclosed are substituted xanthines of general formula
wherein R 1 to R 4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts...
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7482339 |
2-Naphthylimino-1,3-thiazine derivative
The formula (I):
wherein each of R 2 and R 3 is, same or different, C2-C4 alkyl or the like; or R 2 and R 3 are taken together with the adjacent carbon atom to form a 5 to 8 membered...
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7459450 |
Neuropeptide receptor modulators
The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses...
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7384938 |
Aqueous formulations of parasiticides for skin applications
The present invention relates to water-containing formulations for the dermal control of parasitic insects on animals, having the following composition
a) agonists or antagonists of the...
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7375102 |
Tetrahydroquinazolin-4(3H)-one-related and tetrahydropyrido[2,3-D]pyrimidin-4(3H)-one-related compounds, compositions and methods for their use
Compounds are provided having the formula:
wherein variables A 1 , A 2 , A 3 , A 4 , R 1 , R 2 , R 3 , R 4 , Q and L are as described herein. The subject compounds are useful for treatment of...
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7223754 |
Thiazolidinone, oxazolidinone, and imidazolone derivatives for treating lower urinary tract and related disorders
The invention relates to methods of using Cav2.2 subunit calcium channel modulators, particularly thiazolidinone, oxazolidinone, and imidazolone derivatives, to treat lower urinary tract and...
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7205309 |
Quinazoline derivatives
Compounds of formula I
as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 , R 2 , R 3 and A have the significance given in the specification are provided. The...
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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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7166609 |
Pyrimidine-4,6-dicarboxylic acid diamides for selectively inhibiting collagenases
Pyrimidine-4,6-dicarboxylic acid diamides of the formula I
are suitable for selectively inhibiting collagenase (MMP 13). The pyrimidine-4,6-dicarboxylic acid diamides can therefore be used for...
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7087626 |
Pyrrole derivatives as pharmaceutical agents
Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors. The disclosed invention relates to compounds of the...
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7084151 |
5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-5H-chromeno[3,4-ƒ]quinolines as selective progesterone receptor modulator compounds
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such...
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7022705 |
Isoxazoline derivatives useful as antimicrobials
Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof,
wherein, for example,
HET is an N-linked 5-membered, fully or partially...
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6936606 |
Cyanoamido-containing heterocyclic compounds useful as reversible inhibitors of cysteine proteases
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 8 , R 9 and X are defined herein. The...
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6916806 |
Medicinal composition containing 1,3-thiazine derivative
A compound of the formula (I) having a binding activity to the cannabinoid type 2 receptor:
wherein R 1 is optionally substituted heterocyclic group or the like; R 2 and R 2 each is...
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6903119 |
Amino acid derivatives and drugs containing the same as the active ingredient
The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification).
The compounds of the formula (I)...
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6767907 |
4-aryl-1-(indanmethyl dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl) piperidines tetrahydropyridines or piperazines
4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH 2 and...
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6743817 |
Substituted fused pyrroleimines and pyrazoleimines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R 1 and R 2 are defined herein. These compounds are highly selective agonists,...
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6743798 |
Substituted pyrazole derivatives condensed with six-membered heterocyclic rings
The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R 1 , R 2 , R 3 and A are each as defined, and to processes for their preparation and...
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6699898 |
Substituted N,N-disubstituted non-fused heterocyclo amino compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer...
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6566362 |
Benzo&lsqb f&rsqb naphthyridine derivatives, their preparation and compositions containing them
Benzo[f]naphthyridine derivatives of formula (I): benzo[f]naphthyridine derivatives and benzo[f]naphthyridine esters of formula (IVa): aminoquinoline derivatives of formula (X): processes for...
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6559155 |
Pyrimidinone derivatives for the treatment of atherosclerosis
Pyrimidones of formula (I) are inhibitors of the enzyme LpPLA 2 and thereof use in treating inter alia atherosclerosis, in which: R 1 is COOH or a salt thereof, COOR 10 , CONR 11 R 12 , CN or...
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6525076 |
Selective factor Xa inhibitors
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating...
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6514988 |
Condensed-ring thiophene derivatives, their production and use
A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or...
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6469000 |
1,3-diheterocyclic metalloprotease inhibitors
Disclosed are compounds which are inhibitors of metalloproteases having the following structure: where Ar, W, X, Y, Z, R 1 and R 2 have the meanings described in the specification and optical...
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6391327 |
Pesticidal composition
A pesticidal composition comprising prallethrin and a neonicotinoid compound given in the following formula (1), (2) or (3), as an active ingredient wherein, A represents a 6-chloro-3-pyridyl,...
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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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6346530 |
Process for the preparation of a bioavailable oral dosage form of cefuroxime axetil
This invention relates to a process of mixing of crystalline cefuroxime axetil with amorphous cefuroxime axetil for the preparation of a bioavailable oral dosage form comprising of amorphous...
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6319912 |
Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides
This invention relates to cyclic combination therapies utilizing, in combination with a progestin, an estrogen, or both, progesterone receptor antagonists of the general structure: ##STR1## wherein...
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6303638 |
Substituted pyridines as modulators of the mammalian neuronal nicotinic acetylcholine receptor
Novel compounds are provided that modulate the neuronal nicotinic acetylcholine receptor (nAChR), particularly the mammalian nAChR (m-nAChR). The compounds are substituted pyridine derivatives such...
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6248736 |
4-oxo-1,4-dihydro-3-quinolinecarboxamides as antiviral agents
The present invention provides a compound of formula I ##STR1## Wherein R 1 is C 1 -7 alkyl, optionally substituted by hydroxy or NR 4 R 5 ; R 2 is C 1 -7 alkyl substituted by hydroxy or NR 4 ...
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6228867 |
Antagonists of gonadotropin releasing hormone
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety...
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6218394 |
4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophene-methyl) piperazines
4-Aryl-1-(indanmethyl, dihydrobenzofuramethyl or dihydrobenzothiophenemethyl) piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I) ##STR1## wherein one of X and Y is CH 2...
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6200957 |
Antagonists of gonadotropin releasing hormone
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety...
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6194426 |
5,6,7,8 tetrahydroindolizines derivatives
A novel therapeutic use of pyrrole derivatives of the folloeing formula: ##STR1## in which the variables are as defined in the specification and their salts thereof for treating conditions in which...
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6011028 |
Cyclic amidino agents useful as nitric oxide synthase inhibitors
The current invention discloses useful amidino derivative useful as nitric oxide synthase inhibitors.
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6004950 |
2-aminopyridines as inhibitors of cyclooxygenase-2
The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a...
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5998408 |
Triterpene derivatives with immunosuppressant activity
The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
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5977156 |
Fungicidal pyrazoles
Method for protecting plants against fungal or bacterial attack, which comprises applying a 1-phenyl-pyrazole or 1-(2-pyridyl)pyrazole.
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5972934 |
Stabilized nithiazine compositions
Stabilized compositions of nithiazine which are suitable for long term use in an agricultural application. The compositions typically contain nithiazine, a hydroxyalkyl-tert-amine and an...
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5972975 |
Substituted 2-aminopyridines as inhibitors of nitric oxide synthase
Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders....
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5965565 |
Piperidines promote release of growth hormone
The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R 1 , R 1a , R...
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5929114 |
Arylthio compounds
Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O,...
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5914351 |
Anti-viral aromatic hydrazones
Compounds of the formula ##STR1## wherein Q is a hydrazone derivative; R 1 is hydrogen, halogen, alkyl or alkoxy; R 2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl,...
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5891874 |
Anti-viral compound
A series of benzimidazole compounds having the following general structure are provided which inhibit the growth of picornaviruses (e.g., rhinoviruses, enteroviruses, polioviruses, coxsackieviruses...
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5824677 |
Substituted amino alcohol compounds
Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty....
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5789404 |
3-substituted 1-arylindole compounds
3-Substituted 1-arylindole compounds are provided having general formula (I) ##STR1## wherein Ar is an optionally substituted aryl group; X represents a divalent hydrocarbon group, methyleneoxy or...
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5783203 |
Insecticidal fertilizer mixtures
The present invention relates to insecticidal fertilizer mixtures comprising a fertilizer component and an agonist or antagonist of the nicotinergic acetylcholine receptors of insects.
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5767118 |
4-Heterocyclic peperidines promote release of growth hormone
The present invention is directed to certain novel compounds identified as 4-heterocycle substituted piperidines of the general structural formula: ##STR1## wherein R 1 , R 4 , R 5 , A, R 3 and...
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5760033 |
1.3 oxa (thia) zines and pest control agents
A compound represented by the chemical formula 1!: ##STR1## wherein Z is oxygen or sulfur, Y is halogen, optionally substituted alkyl, optionally substituted alkoxycarbonyl, optionally substituted...
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5739130 |
Heterotricyclic derivatives, process for their preparation and pharmaceutical compositions containing them
Heterotricyclic derivatives of the formula: ##STR1## wherein R 1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino, R 2 is hydroxy, protected...
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