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| Number | Title | Issue Date |
| 7435734 | N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are def... | 10/14/2008 |
| 7335657 | Cytokine inhibitors Disclosed are compounds of formula (I) Where Ar1, X, Y, Q, W, R3, R4, R5, R6 and Ry are defined herein. The compounds of the invention inhibit production of ... | 02/26/2008 |
| 7323465 | Alkansulfonamides as endothelin antagonists The invention relates to novel alkansulfonamides of structure (I), wherein R1 is a lowel alzyl group and the other variables are as defined in the description, and their use as active ingredients in the preparation of pharmaceutical compositions. The inve... | 01/29/2008 |
| 7312215 | Benzimidazole C-2 heterocycles as kinase inhibitors Benzimidazole derivatives having the general formula I are provided. These compounds are useful as tyrosine kinase inhibitors, especially for the treatment of cancer. ... | 12/25/2007 |
| 7301021 | Substituted imidazole compounds Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ... | 11/27/2007 |
| 7297694 | Pyridylfurans and pyrroles as Raf kinase inhibitors Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. ... | 11/20/2007 |
| 7285549 | Sulfamides and their use as endothelin receptor antagonists The invention relates to novel sulfamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions contain... | 10/23/2007 |
| 7279502 | Polyamine analog conjugates and quinone conjugates as therapies for cancers and prostate diseases Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions... | 10/09/2007 |
| 7279475 | Fluorinated di-aryl urea compounds Disclosed are compounds of formula(I): wherein R1, R2, W and X of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus... | 10/09/2007 |
| 7273856 | Linear basic compounds having NK-2 antagonist activity and formulations thereof Described herein are compounds of formula (I) useful as antagonists of tachykinins in general, and in particular of neurokinin A; and the pharmaceutical formulations comprising the compounds of formula (I) ... | 09/25/2007 |
| 7235551 | 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases Novel substituted pyrimidol[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ... | 06/26/2007 |
| 7232819 | Dihydroxypyrimidine carboxamide inhibitors of HIV integrase 4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevent... | 06/19/2007 |
| 7223760 | Substituted triazole compounds Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ... | 05/29/2007 |
| 7217712 | 4-Substituted-5-cyano-1H-pyrimidin-6-(thi)ones as GSK-3 inhibitors The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The inventi... | 05/15/2007 |
| 7169780 | N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase N-substituted 5-hydroxypyrimidin-6-one-4-carboxamides of formula (I): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful... | 01/30/2007 |
| 7166595 | Compounds, methods and compositions Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed. ... | 01/23/2007 |
| 7160892 | Pyrimidone compounds and pharmaceutical compositions containing the same The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A1, A2A, and A2B receptors), particularly, compounds represented by the general formula (1), salts thereof, or solvates of... | 01/09/2007 |
| 7151101 | Inhibitors of p38 The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention relates to compounds having the formula: | 12/19/2006 |
| 7105467 | Nickel catalyzed cross-coupling reactions between organomagnesium compounds and anisole derivatives The present invention provides nickel catalysts and solvents which are useful in a cross-coupling reaction between an organomagnesium compound and an aromatic ether compound, such as an anisole derivative. ... | 09/12/2006 |
| 7101873 | Pyrimidinedione derivatives Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them are useful for the tre... | 09/05/2006 |
| 7094781 | Sulfamides and their use as endothelin receptor antagonists The invention relates to novel sulfamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions contain... | 08/22/2006 |
| 7091201 | Arylalkane-sulfonamides having endothelin-antagonist activity The invention relates to novel aryl-alkane-sulfonamides and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compos... | 08/15/2006 |
| 7091209 | Dihydroxypyridmidine carboxylic acids as viral polymerase inhibitors A class of 2-aryl-4,5-dihydroxy-6-carboxypyrimidines of formula (I): wherein Ar is an optionally substituted aryl or heterocyclicgroup; as well as compounds of formula (I) which are derivatized at one or more of the 4-hydroxy, 5-hydroxy or 6-carboxy groups; and taut... | 08/15/2006 |
| 7057038 | Kinetic resolutions of chiral 2- and 3-substituted carboxylic acids One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomer... | 06/06/2006 |
| 7053098 | 3,4-Dihydro-(1H) quinazolin-2-one compounds as CSBP/P38 kinase inhibitors Novel substituted quinazoline compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ... | 05/30/2006 |
| 7053099 | 3,4-dihydro-(1H)quinazolin-2-one compounds as CSBP/p38 kinase inhibitors Novel substituted quinazoline compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ... | 05/30/2006 |
| 7037916 | Pyrimidine derivatives as IL-8 receptor antagonists Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I In these compounds, Q... | 05/02/2006 |
| 7034019 | Prodrugs of HIV replication inhibiting pyrimidines The present invention concerns compounds of formula (A1)(A2)N—R1 (I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R1 is sub... | 04/25/2006 |
| 6939872 | 2-anilino-pyrimidine derivatives as cyclin dependent kinase inhibitors Compounds of the formula (I): wherein R1, R2, R3, p, q, and X are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their u... | 09/06/2005 |
| 6852717 | Compounds useful as anti-inflammatory agents Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds. ... | 02/08/2005 |
| 6833372 | Non-peptide GnRH agents, Pharmaceutical compositions, and methods for their use Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonad... | 12/21/2004 |
| 6833364 | Substituted pyrazole derivatives The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R1, R2, R3, A, X and Y are each as defined, and to processes... | 12/21/2004 |
| 6821971 | Fused pyrazolone compounds which inhibit the release of inflammatory cytokines The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: | 11/23/2004 |
| 6806367 | Process for producing carbonyl hydrazones This invention relates to a method for producing compounds of the formula (I) or their salts: wherein each of R1 and R2 is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substitute... | 10/19/2004 |
| 6787539 | 2,4,5,-trisubstituted pyrimidine derivatives The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2) | 09/07/2004 |
| 6756380 | 5-phenyl-pyrimidine derivatives Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethy... | 06/29/2004 |
| 6750342 | Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a var... | 06/15/2004 |
| 6743798 | Substituted pyrazole derivatives condensed with six-membered heterocyclic rings The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation an... | 06/01/2004 |
| 6743914 | Kinetic resolutions of chiral 2-and 3-substituted carboxylic acids One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomer... | 06/01/2004 |
| 6720321 | 1,4-disubstituted benzo-fused cycloalkyl urea compounds Disclosed are compounds of the formula (I) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds. wherein n, X, A, L, J, p, Q, Y and z are described herei... | 04/13/2004 |
