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7598379 |
Methods for the synthesis of unsymmetrical cycloalkyl substituted xanthines
The present invention provides processes for making pyridyl-linked-xanthines of formula VII, from 5,6-diamino-1H-pyrimidine-2,4-diones of formula II and acylating agents of formula VI.
The...
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7569575 |
Synthesis of locked nucleic acid derivatives
The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as α- L -oxy-LNA, amino-LNA, α- L -amino-LNA, thio-LNA, α- L -thio-LNA, seleno-LNA and...
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7521396 |
Substituted (thioxo)carbonylaminophenyluracils
The invention relates to compounds of the formula (I)
in which Q, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 are as defined in the disclosure, to processes for their preparation, and to...
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7462625 |
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ...
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7419983 |
Gonadotropin-releasing hormone receptor antagonists and methods related thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ...
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7358239 |
Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7232926 |
Method for the production of sulphamic acid halogenides
The present invention relates to a process for preparing sulfamoyl halides of primary or secondary amines, comprising the following steps:
i) reacting a primary or secondary amine A1 with at...
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7229995 |
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ...
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RE39590 |
Substituted benzene compounds, process for their preparation, and herbicidal and defoliant compositions containing them
Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I)
are described. W, X, Y, Z, and Q are as defined in the disclosure. Also described are...
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7148229 |
Sulfonamide substituted xanthine derivatives
The present invention is a sulfonamide substituted xanthine derivative of formula I:
or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl,...
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7135467 |
HIV integrase inhibitors
Compounds useful for treating HIV are disclosed having the general formula
wherein R 1 , R 2 , and B are as defined in the specification. Compositions containing the compounds and methods for...
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7115544 |
Plant growth regulators for cotton hervest
A plant growth regulator for cotton harvest, which contains as an active ingredient, a compound of formula (I):
wherein X is CH or nitrogen; Z is halogen; A is oxygen, sulfur, or NH; R 1 is...
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7115616 |
Pyrimidinone compounds
Pyrimidinone compounds of formula (10 are inhibitors of the enzyme Lp-PLA 2 and of use in therapy, in particular for treating atherosclerosis.
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7109334 |
Stereoselective methods for the preparation of nucleosides
A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A):
wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof...
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7071200 |
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ...
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7034156 |
Method for the production of 1-amino-3-phenyluracil derivatives
The present invention relates to a novel process for preparing known 1-amino-3-phenyluracil derivatives, to novel 1-amino-6-hydroxy-3-phenyldihydro-2,4(1H,3H)pyrimidinedione derivatives of the...
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7026270 |
Biocidal compounds and their preparation
This invention concerns new biocidal compounds of formula (I) wherein R is H or CH 3 . Of particular interest are two isomers that are named malayamycin A and desmethylmalayamycin A. These isomers,...
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RE39056 |
4-Azasteroids for treatment of hyperandrogenic conditions
Compounds of structural Formula (I)
and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type...
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7019136 |
8-quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors
A compound of formula (I):
R 1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R 2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl,...
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7015230 |
Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
The invention relates to substituted polycyclic aryl and heteroaryl uracil compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for...
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7015226 |
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ...
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7001910 |
Thiazolidinedione derivatives as antidiabetic agents
The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for...
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6987114 |
Antiviral pyrimidinedione derivatives and process for the preparation thereof
The present invention relates to pyrimidinedione derivatives of following formula (I) which are useful as antiviral agents, especially as agents for treatment of AIDS, pharmaceutically acceptable...
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6951856 |
Arylethene-sulfonamides
The invention relates to novel aryl-ethene-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including...
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6911450 |
Pyrimidine acyclonucleoside derivatives, preparation method and use thereof
The invention relates to a compound having general formula (I): wherein n is equal to 3; R 1 is an ethyl or isopropyl group; each of the R 2 groups is independently of each other a hydrogen atom,...
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6900222 |
Pyrrolidinyl, piperdinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein...
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6806367 |
Process for producing carbonyl hydrazones
This invention relates to a method for producing compounds of the formula (I) or their salts: wherein each of R 1 and R 2 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or...
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6784293 |
Process for making Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils
The present invention provides a process for the efficient assembly of Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils via a one-pot solution phase or...
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6780821 |
Substituted phenyl uracils
The invention relates to new substituted phenyluracils of the general formula (I) in which n, Q, R 1 , R 2 , R 3 , R 4 , R 5 and X have the meanings given in the description, to process and new...
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6770597 |
Benzohydrazide derivatives as herbicides and desiccant compositions containing them
The compound of the formula: wherein Y, X, Z, T and Q are defined in the specification,
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6734139 |
N-aryl-uracile-based herbicides
The present invention provides herbicidal active compound combinations which comprise, N-aryl-uracils and herbicidally active compounds and/or compounds which improve crop plant compatibility. The...
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6730787 |
2,4Dioxo-5-arylidenimino-1,3-pyrimidines
The invention relates to medicine, and more specifically to pharmacology, and in particular to synthetic biologically active derivatives of pyrimidine, and it is designated mainly for use as...
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6713486 |
Antiviral 2,4-pyrimidinedione derivatives and process for the preparation thereof
2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R 1 is a C 6-10 aryl or...
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6624120 |
Substituted herbicidal phenyluracils
The invention relates to novel substituted phenyluracils of the general formula (I) in which m, n, Q, R 1 , R 2 , R 3 , R 4 , R 5 , X and Y are each as defined in the description, to processes...
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6617281 |
Substituted acylamino phenyl uracils
The invention relates to new substituted acylaminophenyl-uracils of the general formula (I) in which n, A, Ar, Q 1 , R 1 , R 2 , R 3 , R 4 , R 5 and R 6 have the meanings given in the...
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6600044 |
Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers
A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof,...
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6548449 |
Substituted phenyluracils with herbicidal effect
The invention relates to novel substituted phenyluraciles of the general formula (I) in which m, n, Q and R 1-7 are each as defined in the description, and to processes for their preparation...
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6531600 |
Treatment and compounds
A method for the treatment of cerebrovascular disorders and/or disorders associated with cerebral senility and/or other disorders which method comprises the administration of an effective,...
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6525050 |
(4-oxo-2-pyrimidinyl)thioalkyl compounds useful as AICARFT inhibitors
Compounds of the formula: (where R 1 , R 2 and R 3 are defined in the specification) are inhibitors of AICARFT. These compounds, as well as their pharmaceutically acceptable salts, solvents,...
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RE37979 |
Pyrimidine derivatives and anti-viral agent containing the same as active ingredient thereof
The disclosure concerns pyrimidine derivatives represented by the following general formulas [I] and [I′] and having antiviral activity, particularly antiretroviral activity such as anti-HIV...
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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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6476224 |
Method for producing ar(alk)yluraciles, novel corresponding intermediate products and method for producing said intermediate products
The invention relates to a process for preparing ar(alk)yluracils of the general formula (I) in which A represents a single bond or represents alkanedlyl, Ar represents optionally substituted...
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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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6465650 |
Substituted N-ethylglycine derivatives for preparing PNA and PNA/DNA hybrids
The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH 2 , O,...
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6448203 |
Substituted aryluracils
The invention relates to novel substituted aryluracils of the formula (I): to processes for their preparation and to their use as crop protection agents.
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6444616 |
Substituted p-trifluoromethylphenyluracils
The invention relates to novel substituted p-trifluoromethylphenyluracils of the general formula (I) in which R 1 , R 2 , R 3 , R 4 and R 5 are each as defined in the description, to a process...
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6440984 |
Use of aryl-substituted pyrimidines as insecticidal and acaricidal agents
There are provided compositions and methods comprising compounds of formula I: wherein R 1 , A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.
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6437126 |
Substituted phenyluracils
The invention is directed to a process for the preparation of a substituted phenyluracil of the formula: The process broadly comprises reacting a carbonylphenyluracil of the formula: with an...
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6432963 |
Pyrimidine-5-carboxamide derivatives
Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR 1 , CO, NR 1 CO, CONR 1 , C═N—OR 1 or...
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6432962 |
Benzophenones as inhibitors of IL-1β and TNF-α
Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1β and TNF-α and may therefore be useful in the therapy of inflammatory diseases and conditions.
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