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| Number | Title | Issue Date |
| 8084606 | Process for preparation of substantially optically pure levorotatory and dextrorotatory enantiomers of cetirizine using novel intermediates The present invention relates to a novel and commercially viable process for substantially optically pure levorotatory and dextrorotatory enantiomers of cetirizine intermediate, 1-[(4-chlorophenyl)phenylmethyl]piperazine, thereby producing substantially optically pu... | 12/27/2011 |
| 7829713 | Therapeutic piperazines The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compou... | 11/09/2010 |
| 7439362 | Piperazinyl-or piperidinylamine-sulfamic acid amides as inhibitors of steroid sulfatase Piperazinyl- or piperidinylamine-sulfamic acid amides and their use for the manufacture of a medicament in diseases mediated by the action of steriod sulfatase. ... | 10/21/2008 |
| 7371747 | Cyanoalkylamino derivatives as protease inhibitors The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by... | 05/13/2008 |
| 7365075 | Aryl sulfonamide compounds and uses related thereto The present invention provides Aryl Sulfonamide Compounds having the formula: and prodrugs or pharmaceutically acceptable salts or prodrugs thereof. The Aryl Sulfonamide Compounds are useful for treating diabetes, obesity, ... | 04/29/2008 |
| 7297793 | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: | 11/20/2007 |
| 7285553 | Serotonergic 5HTreceptor compounds for treating ocular and CNS disorders Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for... | 10/23/2007 |
| 7223751 | Sulfonamide derivatives, intermediate thereof, its preparation methods, and pharmaceutical composition comprising the same The present invention relates to a novel sulfonamide derivatives and novel intermediates thereof, preparation thereof, and a pharmaceutical composition comprising the same, and more particularly, to novel sulfonamide derivatives and intermediates thereof that are us... | 05/29/2007 |
| 7166600 | Thiocarbamate inhibitors of alpha-4 integrins The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1 | 01/23/2007 |
| 7153896 | Element for protein microarrays An element for the attachment of protein arrays, the element comprising a surface to which are attached a plurality of piperazine functional groups wherein the piperazine functional groups are represented by Formula I: | 12/26/2006 |
| 7119203 | Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metallop... | 10/10/2006 |
| 7094778 | Heterocyclylalkylamines as muscarinic receptor antagonists This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are... | 08/22/2006 |
| 7091219 | Bis-sulfonamide hydroxyethyl-amino retroviral protease inhibitors Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: | 08/15/2006 |
| 7084144 | Sulfonyl group containing compounds and their use for the treatment of erectile dysfunction A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl ... | 08/01/2006 |
| 7067660 | Process for the preparation of pyrazolopyrimidinones There is provided a process for the production a compound of general formula I: wherein A, R1, R2, R3 and R4 have meanings given in the description, which process compr... | 06/27/2006 |
| 7030242 | Selective inhibition of aggrecanase in osteoarthritis treatment This invention relates to a method of treatment for osteoarthritis involving inhibitors of aggrecanase that demonstrate IC50s of less than 20 nM and demonstrate differential potency against matrix metalloproteinases (MMPs) and a disintegrin and metallopro... | 04/18/2006 |
| 7026323 | Platelet adenosine diphosphate receptor antagonists Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmace... | 04/11/2006 |
| 7022831 | Regulation of BCL-2 gene expression The present invention provides novel anticode oligomers and methods of using them for controlling the growth of cancer cells expressing the bcl-2 gene. ... | 04/04/2006 |
| 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 |
| 7022707 | Piperazine derivatives The present invention is a chemical compound of formula (I) or a pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R4, A1, A2 m and n are as descri... | 04/04/2006 |
| 7015323 | Thiocarbamate inhibitors of alpha-4 integrins The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1 | 03/21/2006 |
| 7005520 | Process for the preparation of pyrazolopyrimidinones There is provided a process for the production a compound of general formula I: wherein A, R1, R2, R3 and R4 have meanings given in the description, which process comprises th... | 02/28/2006 |
| 6974869 | Piperizinones as modulators of chemokine receptor activity The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases. ... | 12/13/2005 |
| 6943253 | 6-phenylpyrrolopyrimidinedione derivatives The invention relates to new 6-phenylpyrrolopyrimidine derivatives of formula (I): wherein: —X—C—Y— represents or —X—C—Y— represe... | 09/13/2005 |
| 6943179 | Biurethane derivatives Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and... | 09/13/2005 |
| 6924251 | Substituted benzoylcyclohexandiones The invention relates to novel substituted benzoylcyclohexanediones of the general formula (I), in which m, n, A, R1, R2, R3, R4 and Z are each as defined in the... | 08/02/2005 |
| 6878707 | Carboxamides useful as inhibitors of microsomal triglyceride transfer protein and of apolipoprotein b secretion Compounds of formula (I) wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, heteroaryl or (aryl or heteroaryl)-lo... | 04/12/2005 |
| 6878712 | Amides as inhibitors for pyruvate dehydrogenase A compound of formula (I): wherein: Ring A is a nitrogen linked mono or bicyclic heterocyclic ring as defined within; R1 and R2 are independentl... | 04/12/2005 |
| 6875831 | Mono and multifunctional alkoxyamines for the preparation of functionalized macromers The invention pertains to a compound of formula (I), (II) or (III) wherein R1 and R2 are independently of each other hydrogen, C1-C18alkyl, C3-C18alkeny... | 04/05/2005 |
| 6852718 | Phenylsulphonylipiperazinyl derivatives as 5-HT receptor ligands A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted piperazine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the ... | 02/08/2005 |
| 6852855 | Synthesis of piperazine ring A novel process for preparing a compound of the formula I: wherein R1 denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy; R2 denotes substituted or unsubstit... | 02/08/2005 |
| 6846825 | Antibacterial agents Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(═O) or the formula: —C(═O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted... | 01/25/2005 |
| 6815214 | Pharmaceutical uses and synthesis of diketopiperazines The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of diverse diketopiperazines and process for their synthesis as a library an... | 11/09/2004 |
| 6809100 | Hydroxamic acid derivatives The invention encompasses novel compounds which are inhibitors of matrix metalloproteinase, ADAM or ADAM-TS enzymes, and which are useful for the treatment of diseases mediated by those enzymes, including degenerative diseases and certain cancers. ... | 10/26/2004 |
| 6809202 | Diketodiazacyclic compounds, diazacyclic compounds and combinatorial libraries thereof The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl gorup and 6-8 atoms in... | 10/26/2004 |
| 6794511 | Sulfonyl aryl or heteroaryl hydroxamic acid compounds A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid ... | 09/21/2004 |
| 6787536 | Hydroxamic acid derivatives The invention encompasses novel compounds which are inhibitors of matrix metalloproteinase, ADAM or ADAM-TS enzymes, and which are useful for the treatment of diseases mediated by those enzymes, including degenerative diseases and certain cancers. ... | 09/07/2004 |
| 6770637 | Substituted 4-phenyl-pyridine compounds with activity as antagonists of neurokinin 1 receptors Substituted 4-phenyl-pyridine compounds with activity as antagonists of Neurokinin 1 receptors, methods of making these compounds and preparing. ... | 08/03/2004 |
| 6734183 | Compounds Compounds of the formula I useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13. ... | 05/11/2004 |
| 6734184 | Arylpiperazines and their use as metalloproteinase inhibiting agents (MMP) Arylpiperazines of formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13. ... | 05/11/2004 |
