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Class 560/13 - Plural nitrogens in acid moiety


Subclass of Class 560 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the acid radical contains more than one
No. of patents: 485
Last issue date: 10/05/2010


1                      
NumberTitleIssue Date
7807850Preparation of 2R,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-P-nitrobenzenesulfonylamide hydrochloride and other derivatives of 2-hydroxy-1,3-diamines
The present invention provides a new process for the preparation of 2R,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbuty1)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of t...
10/05/2010
7442718Inhibitors of aspartyl protease
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. T...
10/28/2008
7417059Substituted aromatic-ring compounds, process for producing the same and use
The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of d...
08/26/2008
7414144Preparation of 2S,3S--isobutyl--(2-hydroxy-3-amino-4-phenylbutyl)--nitrobenzenesulfonylamide hydrochloride and other derivatives of 2-hydroxy-1,3-diamines
The present invention provides a new process for the preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of t...
08/19/2008
7388008Lysine based compounds
The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for exampl...
06/17/2008
7375120Peptide deformylase inhibitors
Novel PDF inhibitors and novel methods for their use are provided. ...
05/20/2008
7338958Sulfoximine-substituted pyrimidines as CDK-and/or VEGF inhibitors, their production and use as pharmaceutical agents
This invention relates to pyrimidine derivatives of general formula I in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, ...
03/04/2008
7326511Sulfonate derivatives and the use thereof as latent acids
Chemically amplified photoresist compositions comprising, (a) a compound which cures upon the action of an acid or a compound whose solubility is increased upon the action of an acid; and (b) a compound of the formula (Ia), (Ib), (IIa), (IIb), (IIIa), (IIIb), (Iva),...
02/05/2008
7320983α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. ...
01/22/2008
7288526Dipeptide and related 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 treatment of inflammatory diseases in a mammalian patient, e.g., human, su...
10/30/2007
7268164Anti-epileptogenic agents
Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and epileptogenesis. Methods for preparing the compounds of the invention are also d...
09/11/2007
7262317Freeze-dried preparation of n[o-(p-pivaloyloxybenzenasulfonylamino) benzoyl] glycine monosodium salt tetrahydrate and process for producing same
A method for the preparation of a freeze-dried product of N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetra-hydrate dissolved in a mixed solvent of water and ethanol, and the freeze-dried product obtained by the method. According t...
08/28/2007
7256215Crystals of 5-hydroxycarbamimidoyl-2-hydroxybenzenesulfonamide derivative
The present invention provides a novel crystalline form of n-butyl[4-[2-[2-hydroxy-5-(N-hydroxycarbamimidoyl) benzenesulfonylamino]ethyl]-2′-methanesulfonyl-3-yloxy] acetate hydrochloride, pharmaceutical compositions containing the same and their uses, which exhib...
08/14/2007
7244544Oxime derivatives and the use thereof as latent acids
New oxime sulfonate compounds of the formula I, II, III, IV, V, VI and VII R1 is for example C1–C18alkylsulfonyl, R2 is halogen o...
07/17/2007
7199158Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein R1–R6, R7, R7′, R8, R30–R34, X′, Y, Y′, t,...
04/03/2007
7166580Compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su...
01/23/2007
7163942Sulfonamide compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula I wherein R1, R2, R3, m, and n are as defined. Compounds of the Formula I have activity inhibiting production of Aβ-pept...
01/16/2007
7161033Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to ...
01/09/2007
7153869Substituted amino acids as erythropoietin mimetics
This invention relates to a series of substitituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molec...
12/26/2006
7084178Antiamyloid phenylsulfonamides: N-cycloalkylcarboxamides derivatives
A series of N-cycloalkylcarboxamide derivatives of N-benzyl benzenesulfonamides of Formula I are described. The compounds inhibit β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's...
08/01/2006
7074820Amidino derivatives and their use as thrombin inhibitors
There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like protease...
07/11/2006
7057043Processes for preparing aminophenylsulfonylureas, and intermediates therefor
The invention relates to the preparation of compounds (I) in which A=H or acyl and R1, R2, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement ...
06/06/2006
7030114Compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su...
04/18/2006
7026094Substituted oxime derivatives and the use thereof as latent acids
New oxime sulfonate compounds of the formula (I) and (II), wherein R1 is C1-C12alkyl, C1C4haloalkyl, hydrogon, OR9, NR10R11, SR12 or is phenyl which is unsubstituted o...
04/11/2006
7022851PNA monomer and precursor
This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers:
04/04/2006
6995283Benzophenones as inhibitors of reverse transcriptase
The present invention is directed to beazophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties. ...
02/07/2006
6992105Dipeptide derivatives
Compounds of the formula wherein R, R1, COOR2, R3–R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral e...
01/31/2006
6951886Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors and in particular as inhibitors o...
10/04/2005
6939855Anti-inflammatory compositions and method
The disclosed invention includes pharmaceutical compositions and methods for treating inflammatory conditions, particularly those that are characterized by increased binding of alpha-9 integrin to one or more of its ligands. Also disclosed are methods for selecting ...
09/06/2005
6930112Anti-epileptogenic agents
Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and epileptogenesis. Methods for preparing the compounds of the invention are also d...
08/16/2005
6924310Malonamic acids and derivatives thereof as thyroid receptor ligands
The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias...
08/02/2005
6919369Serine protease inhibitors
Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
07/19/2005
6916837Amidino derivatives and anticoagulants and thrombosis therapeutic agents containing them
Amidino derivatives represented by the following general formula (I): {where X is a group represented by R1SO2NR2— (wherein R1 represents optionally substituted C6-14 ...
07/12/2005
6890942Acyl sulfonamides as inhibitors of HIV integrase
The present invention relates a series of compounds of Formula I wherein R1, R2, R3, and B are as defined in the specification. The compounds are useful for the inhibition of HIV integr...
05/10/2005
6861539Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to ...
03/01/2005
6855842Intermediates for making a bezofuran or benzothiophene derivative nitrated in position 5 and uses thereof
The invention concerns novel nitroaromatic compounds of general formula (I′) wherein: R, R′1, R2, Z and n are as defined in claim 1. The invention also concerns a method for preparing nitroaromatic compounds nitrated in position 4. The invention further c...
02/15/2005
6849626Aza-amino acid derivatives (factor Xa inhibitors 15)
The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formul...
02/01/2005
6790866Sulfonamide and carboxamide derivatives and drugs containing the same as the active ingredient
The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is ...
09/14/2004
6777572Use of propargyl glycine amino propargyl diol compounds for treatment of renal failure
Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of renal failure. Compounds of particular interest are those of Formula I wherein A is selected from CO and...
08/17/2004
6770764Trypsin substrate and diagnostic device, and method of using same
A compound of the formula (I) wherein R1 is a protecting group for Nα, R2 is a protecting group for NG, and R3 is aryl, and wherein the compound of formula (I) is a trypsin su...
08/03/2004
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