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8163956 |
Inhibitors of GLYT1 transporters
A compound of the formula (I): wherein R1, R2, R3, R4, Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I)...
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8115031 |
Anti-inflammatory quinic acid derivatives for oral administration
Disclosed are compounds comprising analogs of quinic acids or shikimic acids having anti-inflammatory properties. The compounds are suitable for oral administration, stable, and demonstrate...
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7989439 |
Substituted pyrazoles, compositions containing these, method of production and use
The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds,...
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7947852 |
Naphthalene compounds, a process for their preparation and pharmaceutical compositions containing them
Compounds of formula (I): wherein: R1 represents alkyl, alkenyl, haloalkyl, polyhaloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl,X represents a group N—OR2 w...
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7728171 |
Process for the production of acid chlorides
A process for the preparation of acid halides of formula I which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.
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7632972 |
Compounds and methods for treatment of cancer and modulation of programmed cell death for melanoma and other cancer cells
Compounds and related methods for synthesis, and the use of compounds and combination therapies for the treatment of cancer and modulation of apoptosis in cells are disclosed. The generation of...
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7601870 |
Substituted aniline derivatives
The present invention relates to aniline derivatives of the general formula I or salts thereof, described therein, and their use.
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7592365 |
Substituted pyrroles, compositions containing same, method for making same and use thereof
The disclosure concerns substituted pyrroles of formula (I): wherein A, L, Ar, R1, R2, R5, and Ra are as defined in the disclosure, compositions containing the same, methods for making the same and...
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7560591 |
Benzamidine derivatives having anti-inflammatory and immunosuppressive activity
Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl...
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7511175 |
Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of...
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7476755 |
Therapeutic compounds
Therapeutic substituted cyclopentane compounds, and compositions, medicaments, and therapeutic methods related thereto are disclosed herein.
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7435849 |
Process for the production of acid chlorides
A process for the preparation of acid halides of formula I which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.
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7435851 |
Puleganic amides
The present invention provides substituted puleganic amides and compositions thereof, which are both useful as a topical treatment for skin, such as a repellant for insects and arthropods.
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7414152 |
N-substituted p-menthane carboxamides
Cooling compounds are provided having the formula: wherein, m is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, C1-C4 straight or branched alkyl, and a C1-C4...
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7381827 |
Processes and intermediates
The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing...
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7220814 |
Hydrophilicized blocked polyisocyanates
The present invention relates to new hydrophilicized blocked polyisocyanates, a process for preparing them and their use.
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7161016 |
Cannabimimetic lipid amides as useful medications
Novel analogs of arachidonylethanolamide are presented which have higher affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic...
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7091231 |
12-Aryl prostaglandin analogs
Compounds comprising are disclosed, wherein Y, A, X, R, D, and n are as described. A compound comprising a prostaglandin EP2 selective agonist wherein the ω-chain comprises a substituted phenyl, ...
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7071359 |
Neuropathy improvers containing nitrogenous compounds as the active ingredient
A compound represented by the Formula below, and an agent for the remedy of neural damage having the said compound as the active ingredient. [Here, G represents G1 shown below R4 represents,...
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7049317 |
CCR-3 receptor antagonists
The invention provides compounds of Formula (I): wherein R1–R4 have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing t...
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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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6683212 |
Fungicidally active carboxylic acid amides
Compounds of Formula (I) are disclosed which are useful as fungicides wherein R1 is hydrogen; halogen; C1-C2 alkoxy; C1-C2 haloalkoxy, cyano; or C1-C2 alkyl optionally substituted with halogen,...
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6667406 |
Methods for the synthesis of complex reduced isoindole, isooxyindole and isooxyquinoline libraries
Disclosed are methods of synthesizing libraries of diverse complex hexahydroisoindole, hexahydroisooxyindole and octahydroisooxyquinoline compounds through the use of a facile intramolecular Diels...
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6593312 |
Cyclic α-amino-&ggr -hydroxyamide compounds
A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members,R1 and R4, which may be identical or different, each represents...
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6576792 |
2-halo-1-cycloalkenecarboxamides and their preparation
The invention relates to a 2-halo-1-cycloalkenecarboxamides represented by Formula I: whereinn is 1 or 2;R is hydrogen or an alkyl group; andX is a halogen.
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6441232 |
Selective nitrogen functionalization of organic compounds
There is provided a method of selectively replacing a carbon-hydrogen bond at an unactivated saturated sp3 hybridised carbon atom in an organic compound by a carbon-nitrogen bond, the method...
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6437183 |
Method for making amides
The invention relates to the manufacture of amide compounds provided through the reaction of nitrile compounds and a sulfate compound to form the related amide compound. In a preferred embodiment a...
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6423748 |
Amido polybiguanides and the use thereof as antimicrobial agents
Amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of amido polybiguanides is also disclosed. The amido polybiguanides...
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6403649 |
Non-acidic cyclopentane heptanoic acid,2-cycloalkyl or arylalkyl derivatives as therapeutic agents
The present invention provides cydopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH...
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6395787 |
Ocular hypotensive lipids
Compounds of Formula 1, where the symbols are as defined in the specification, are useful as ocular hypotensive agents but do not exert their activity through the FP prostaglandin receptor. In...
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6316669 |
Bis-amido polybiguanides and the use thereof to disinfect contact lenses and preserve pharmaceutical compositions
Bis-amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of bis-amido polybiguanides is also disclosed. The bis-amido...
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6303658 |
Cyclopentane heptenoic or heptanoic acids and derivatives thereof useful as therapeutic agents
The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids,...
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6235789 |
Benzocycloalkene compounds, their production and use
A compound of the formula ##STR1##wherein R1 and R2 are H, a hydrocarbon group or a heterocyclic group, or R1 and R2 are combinedly a spiro ring; R3 is a hydrocarbon group, a substituted amino...
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6235780 |
ω-cycloalkyl-prostaglandin E1 derivatives
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6194611 |
N-sulphonyl and N-sulphinyl amino acid derivatives as microbicides
α-Amino acid amides of formula (I) wherein the substituents are defined as follows: n is the number zero or one; R1 to R7 are as herein defined; R8 is C1 -C6 alkyl, C3 -C6 alkenyl or C3 -C6 ...
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6162923 |
Process for the preparation of imidazolones
The present invention relates to a process for the preparation of a compound of general formula (I), ##STR1## wherein R1 represents a hydrogen atom or an alkyl group of 1-6 carbon atoms, and their...
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6124277 |
Antithrombotic agents
This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.
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6037361 |
Fluorinated butyric acids and their derivatives as inhibitors of matrix metalloproteinases
Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix...
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6028112 |
Spirocyclopropyl fluorenes as melatonergic agents
There is provided novel spirocyclopropyl fluorene derivatives having the general Formula I ##STR1## wherein R, R1 and X are as defined herein which are useful as melatonergic agents.
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5994562 |
Preparation of N-alkenylcarboxamides
In a process for preparing N-alkenylcarboxamides by dehydration of N-(2-hydroxyalkyl)carboxamides and/or diethers thereof in the presence of a catalyst, molecular sieves, in particular zeolites,...
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5959023 |
Moisture-crosslinking PU hot-melt adhesives
Moisture-crosslinking PU hot-melt adhesives produced by reacting an --NCO containing prepolymer and a sterically hindered polyamine which have a very high initial strength.
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5939554 |
Diarylaminopropanediol and diarylmethyl-oxazolidinone compounds
A method for preparing a diarylalanine compound is provided. The method includes reacting a diarylaminopropanediol with a reducing agent to form a diarylaminopropanol compound and/or contacting a...
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5935988 |
Tolerability of pharmaceutically active β-amino acids
The present invention relates to mixtures of α-amino acids and/or derivatives thereof and cyclopentane-β-amino acids and/or derivatives thereof, dipeptides of the abovementioned α-amino acids an...
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5925770 |
Certain fused pyrrolecarboxanilides; a new class of gaba brain receptor ligands
The present invention encompasses structures of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted...
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5925674 |
Cycloalkylcarboxanilides
This invention relates to cycloalkylcarboxanilides of the formula ##STR1## which are used to combat pests.
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5889031 |
N-acyl-2-aryl cyclopropylmethylamine derivatives as melatonergics
Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.
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5886223 |
Process for the preparation of substituted β-ketoanilide compounds
There is provided a process for the preparation of substituted β-ketoanilide compounds having the structural formula I ##STR1## The substituted β-ketoanilide compounds are useful for the control o...
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5783712 |
Vinyl ether compounds having additional functional groups other than vinyl ether groups and the use thereof in the formulation of curable compositions
The invention relates to compounds having at least one vinyl ether group which also contain in the molecule at least one further functional group selected from acrylate, methacrylate, epoxy,...
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5780512 |
Alkylated (hetero) cyclic compounds
The invention relates to a compounds selected from these of formula (I): ##STR1## in which: R1, R2, R3 and A are as defined in the description, and a medicinal product containing the same useful...
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5777138 |
Ring-opening amidation process
A process for amidating a 2-azabicyclo 2.2.1!heptan-3-one or a 2-azabicyclo 2.2.1!hept-5-en-3-one by reaction with an amine, to form the corresponding ring-opened amide, is modified by the addition...
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