Felix Hoffmann, a German chemist, was searching for something to relieve his father's arthritis. In doing so, he "rediscovered" acetylsalicylic acid and in 1900, patented a stable process for developing it. Hence, we have aspirin.
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| Number | Title | Issue Date |
| 7807850 | Preparation 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 |
| 7442718 | Inhibitors 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 |
| 7417059 | Substituted 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 |
| 7414144 | Preparation 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 |
| 7388008 | Lysine 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 |
| 7375120 | Peptide deformylase inhibitors Novel PDF inhibitors and novel methods for their use are provided. ... | 05/20/2008 |
| 7338958 | Sulfoximine-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 |
| 7326511 | Sulfonate 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 |
| 7320983 | α- 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 |
| 7288526 | Dipeptide 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 |
| 7268164 | Anti-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 |
| 7262317 | Freeze-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 |
| 7256215 | Crystals 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 |
| 7244544 | Oxime 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 |
| 7199158 | Succinoylamino 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 |
| 7166580 | Compounds 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 |
| 7163942 | Sulfonamide 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 |
| 7161033 | Bis-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 |
| 7153869 | Substituted 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 |
| 7084178 | Antiamyloid 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 |
| 7074820 | Amidino 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 |
| 7057043 | Processes 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 |
| 7030114 | Compounds 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 |
| 7026094 | Substituted 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 |
| 7022851 | PNA 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 |
| 6995283 | Benzophenones 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 |
| 6992105 | Dipeptide 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 |
| 6951886 | Succinoylamino 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 |
| 6939855 | Anti-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 |
| 6930112 | Anti-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 |
| 6924310 | Malonamic 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 |
| 6919369 | Serine 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 |
| 6916837 | Amidino 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 |
| 6890942 | Acyl 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 |
| 6861539 | Bis-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 |
| 6855842 | Intermediates 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 |
| 6849626 | Aza-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 |
| 6790866 | Sulfonamide 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 |
| 6777572 | Use 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 |
| 6770764 | Trypsin 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 |