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Class 548/579 - The five-membered hetero ring is unsubstituted or is alkyl substituted only (e.g., pyrrolidine, etc.)


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the five-membered hetero ring is unsubstituted,
No. of patents: 157
Last issue date: 06/03/2008


1        
NumberTitleIssue Date
7381827Processes 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 caspase inhibitors and/or prodrugs thereof. ...
06/03/2008
7335681Amino ceramide-like compounds and therapeutic methods of use
Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer sy...
02/26/2008
7226917Derivatives of N-[phenyl(pyrrolidine-2-yl)methyl]benzamide and N-[(azepan-2-yl)phenylmethyl]benzamide, preparation, and use in treatment of schizophrenia
Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic ...
06/05/2007
7220884Hydroaminomethylation of olefins
The present invention relates to a method comprising the step of contacting under hydroaminomethylation conditions, an olefin, an amine, a rhodium-phosphorous ligand, and synthesis gas (syngas). In particular, it has been discovered that, under some circumstances, a...
05/22/2007
7175670Couplers of 2,3,5-triaminopyridine and use of the same for dyeing keratin fibers
The present invention relates to a dye composition comprising at least one oxidation base and at least one coupler of the 2,3,5-triaminopyridine type. This composition may be useful for dyeing keratin fibers, such as the hair. Also disclosed are a process for dyeing...
02/13/2007
7148251Amino ceramide-like compounds and therapeutic methods of use
Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer sy...
12/12/2006
71450052-(6-{2-[(2R)-2-Methyl-1-pyrrolidin-1-yl]-ethyl}-2-naphthalen-2-yl)-2H-pyridazin-3-one salts and their preparation
The present invention relates to salts of 2-(6-{2-[(2R)-2-methyl-1-pyrrolidin-1-yl]-ethyl}-2-naphthalen-2-yl)-2H-pyridazin-3-one, processes for their preparation, pharmaceutical compositions comprising such compounds, method of using them, and a process for preparin...
12/05/2006
7119122Compounds for the inhibition of nitric oxide synthase
There are provided novel compounds of formula (I) wherein A, R1, R3, R4, R5, T, U, V, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their prepara...
10/10/2006
7071212N-(4-carbamimidoyl-phenyl)-glycine derivatives
The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in ...
07/04/2006
6969744Living and quasiliving cationic telechelic polymers quenched by N-substituted pyrrole and methods for their preparation
Disclosed is a method of preparing terminally functionalized telechelic polymers using a cationic living polymer product or a terminal tert-chloride chain end of a carbocationic quasiliving polymer product, which comprises quenching the polymer product with an N-sub...
11/29/2005
6800618Chemosensitizing agents against chloroquine resistant plasmodium falciparum and methods of making and using thereof
A compound having the structural formula or a pharmaceutically acceptable salt or prodrug thereof, wherein X is a substituted or unsubstituted alkyl or a heteroatom; n is 4, 5 or 6; Y is a substituted or unsubstituted al...
10/05/2004
6800659Compounds for modulating cell proliferation
Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed. The compounds are of the Formula I: ...
10/05/2004
6797820Succinate compounds, compositions and methods of use and preparation
Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The hydroxymates are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of pept...
09/28/2004
6787563Crystalline 3-{4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile citrate
The present invention relates to substituted N-(cyclopropylmethyl)azacycloalkanes of the following formula (I): in which, independently, R1 is hydrogen or halogen, R2 is hydrogen or halogen and X is...
09/07/2004
6753447Functionalized monomers for synthesis of rubbery polymers
This invention discloses a process for synthesizing an amine functionalized monomer that comprises (1) reacting a secondary amine with a 2,3-dihalopropene to produce a vinyl halide containing secondary amine having a structural formula selected from the group consis...
06/22/2004
6750216Kappa agonist compounds and pharmaceutical formulations thereof
Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formula IIIB have the structure: wherein R1, R2
06/15/2004
6749988Amine compounds, resist compositions and patterning process
Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enh...
06/15/2004
6743564Amine compounds, resist compositions and patterning process
Amine compounds having a cyano group are useful in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist. ...
06/01/2004
6734177Certain salts of discodermolide acid, pharmaceutical compositions containing them and their use in treating tumors
The present invention relates to certain salts of discodermolide acid, pharmaceutical compositions containing said salts, the use of said salts in treating tumors and to a process for making said salts. ...
05/11/2004
6713467Acid derivatives useful as serine protease inhibitors
Compounds of formula I and II, or pharmaceutically-acceptable salts thereof, are useful as inhibitors of Factor VIIa, Factor IXa, Factor Xa, Factor FXIa, tryptase, and urokinase, wherein ring B is phenyl or pyridyl, L is...
03/30/2004
6562965Convergent synthesis of ଱-aryl-ଲ-ketonitriles
The present invention relates to processes for the production of ଱-aryl-ଲ-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) rece...
05/13/2003
6521761Primary intermediates for oxidative coloration of hair
Primary intermediates useful hair coloring systems comprise quaternized pyrrolidine compounds. The invention provides new quaternized pyrrolidine of Formula (1): ##STR1## wherein X is Cl, Br, I, or R3 S04 ; R is a C1 to C
02/18/2003
6489515Gas-phase dehydration reaction process
Here is provided a process capable of efficiently carrying out a gas-phase dehydration reaction comprising contacting a raw material gas with a solid oxide catalyst containing an alkali metal element to allow reaction to progress by inhibiting decompositi...
12/03/2002
6476063Kappa agonist compounds, pharmaceutical formulations and method of prevention and treatment of pruritus therewith
Method for the prevention or treatment of pruritus with anti-pruritic compounds is provided. The compounds of formulae I, II, IIA, III, IIIA, IV and IVA have the structure: ##STR1## ##STR2## wherein R1, R2, R3, R...
11/05/2002
6447749Perfluoro-alkyl containing dye molecules and galencial formulations
This invention describes galenical formulations that contain perfluoroalkyl-containing dye molecules and other perfluoroalkyl-containing substances. The new formulations are suitable as, i.a., contrast media for near-infrared diagnosis....
09/10/2002
6444662Stable hyperforin salts, method for producing same and their use in the treatment of alzheimer's disease
Described are salts of hyperforin and adhyperforin of formula I [A- ]m [B]p+ (I) wherein m is an integer from 1 to 3, p is equal to m and gives the total number of positive charges of the residue [B], [A- ] is an anion o...
09/03/2002
6423710Cyclic AMP-specific phosphodiesterase inhibitors
Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, a...
07/23/2002
6420364Compound useful as reversible inhibitors of cysteine proteases
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel c...
07/16/2002
6417353Preparing amines
Amines are prepared by reacting aldehydes or ketones at elevated temperature under elevated pressure with nitrogen compounds selected from the group of ammonia, primary and secondary amines, and with hydrogen in the presence of a catalyst containing coppe...
07/09/2002
6369069Biphenylsulfonyl cyanamides, method for the production thereof and their utilization as a medicament
The invention relates to compounds of the formula (I), ##STR1## in which the symbols have the following meaning: R(1) is 1. alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms; 2. alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, in which one to all hydrogen ...
04/09/2002
6362333Method for simultaneously producing a cyclic lactam and a cyclic amine
A cyclic lactam and a cyclic amine are coproduced by coreacting an aliphatic alpha, omega-diamine and an aliphatic alpha, omega-aminonitrile with water in the gas phase in the presence of a heterogeneous catalyst....
03/26/2002
6362332Coproduction of a cyclic lactam and a cyclic amine
A cyclic lactam and a cyclic amine are coproduced by reacting an aliphatic alpha, omega-diamine with water in the gas phase in the presence of a heterogeneous catalyst....
03/26/2002
6353118Dewatering and purification of crude pyrrolidine
In a process for purifying crude pyrrolidine to give a pyrrolidine composition comprising more than 99% (m/m) of pyrrolidine and less than 0.3% (m/m) of water, crude pyrrolidine comprising from 40 to 98% (m/m) of pyrrolidine and having a water content of ...
03/05/2002
6353099Substituted ureas as cell adhesion inhibitors
Compounds of Formula I are antagonists of VLA-4 and/or 댔ଲ.sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical ...
03/05/2002
6159673Oxonol compound, light-sensitive material and process for the synthesis of oxonol compound
An oxonol compound is represented by the following formula (I): ##STR1## in which Z is an atomic group that forms a cyclic amide ring; each of W1 and W2 independently is an atomic group that forms an acidic nucleus ring; and M i...
12/12/2000
6153766Method of producing 4-hydroxy-2-pyrrolidinone and method of purifying the same
4-Hydroxy-2-pyrrolidinone which is useful as a raw material of drugs can be produced rapidly and highly selectively in a high yield from an optically active or recemic 4-amino-3-hydroxybutylic acid derivative or a 4-azido-3-hydroxybutyric acid derivative ...
11/28/2000
6136803Antidepressants
The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment ...
10/24/2000
6133262Antithrombotic agents
This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the ...
10/17/2000
6048877Tetralone derivatives as antiarrhythmic agents
Tetralone derivatives of the formula ##STR1## where R1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, ...
04/11/2000
60136562-(arylalkenyl) azacycloalkane derivatives as ligands for sigma receptors
New 2-(arylalkenyl)azacycloalkane derivatives which are ligands for sigma receptors, of the formula (I) ##STR1## in which: Ar is aryl or heteroaryl, optionally mono- to trisubstituted, m has the value 1 or 2, n has the value 1 to 3, R is phenyl, or cycloa...
01/11/2000
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