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| Number | Title | Issue Date |
| 8012978 | Prodrugs of CC-A1065 analogs The present invention provides prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group containing a sulfonic acid containing phenyl carbamate, in which the protecting group confers enhanced water solubility upon the prodrug, and ... | 09/06/2011 |
| 7655660 | Prodrugs of CC-1065 analogs Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the pr... | 02/02/2010 |
| 7655661 | Prodrugs of CC-1065 analogs Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the pr... | 02/02/2010 |
| 7393845 | Heteroaryl derivates, their preparation and use A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disord... | 07/01/2008 |
| 7388026 | Prodrugs of CC-1065 analogs Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the pr... | 06/17/2008 |
| 7300937 | Derivatives of cyano-aryl (or cyanoheteroaryl)-carbonyl-piperazinyl-pyrimidines, their preparation and application as medication New derivatives of cyanoaryl (or cyanoheteroaryl)-carbonyl-piperazinyl-pyrimidines (I), where R1 represents an OR3 radical, where R3 represents a radical derived from a saturated hydrocarbon, with a linear or branched chain of 1 to 4... | 11/27/2007 |
| 7244758 | N-type calcium channel blockers Compounds that are derivatives of 3-aminomethyl-pyrrolidine generally containing at least one benzhydril moiety are useful in treating conditions which benefit from blocking calcium ion channels. ... | 07/17/2007 |
| 7208495 | Benzo-fused 5-membered hetrocycle compounds, process for preparation of the same, and use thereof A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R... | 04/24/2007 |
| 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 |
| 7045519 | Inhibitors of glycogen synthase kinase 3 New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may... | 05/16/2006 |
| 6995159 | 5-HT receptor ligands and uses thereof Compounds of Formula (IC) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2 receptors in animals are described herein . ... | 02/07/2006 |
| 6953803 | Pyrimidine compounds Pyrmidinone compounds of formula (I) are inhibitors of the enzyme Lp-PLA2 and of use in therapy, in particular for treating atherosclerosis. ... | 10/11/2005 |
| 6916804 | Pyrimidine A2b selective antagonist compounds, their synthesis and use The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R | 07/12/2005 |
| 6908920 | Pyrimidine derivatives Compounds of formula (I), wherein R1, p, R2, q, R3 and R4 are defined within, and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and th... | 06/21/2005 |
| 6867226 | Serotonin 5-HT3 receptor partial activator This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect. | 03/15/2005 |
| 6849660 | Antimicrobial biaryl compounds Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1′ is —C(O)NR5R5′ | 02/01/2005 |
| 6767907 | 4-aryl-1-(indanmethyl dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl) piperidines tetrahydropyridines or piperazines 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH;... | 07/27/2004 |
| 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 |
| 6713474 | Pyrrolopyrimidines as therapeutic agents Chemical compounds having structural formula I and physiologically acceptable salts and metabolites thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases, whose activity is inhi... | 03/30/2004 |
| 6602874 | Heterocyclic carboxamides A compound of the formula ##STR1## wherein X, Y, Z, R2 and R3 are as defined above, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1, agonist or antagonist is indicated.... | 08/05/2003 |
| 6552057 | Serotonin 5-HT3 receptor partial activator This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side... | 04/22/2003 |
| 6537995 | Heterocyclic carboxamides A method is provided for treating or preventing a disorder or condition selected from hypertension, depression, generalized anxiety disorder, phobias, posttraumatic stress syndrome, avoidant personality disorder, premature ejaculation, eating disorders, o... | 03/25/2003 |
| 6440965 | Substituted pyrimidine derivatives, their preparation and their use in the treatment of neurodegenerative or neurological disorders of the central nervous system The present invention relates to novel derivatives of a series of substituted pyrimidines, to pharmaceutical compositions which contain them, to methods for their preparation and to their use in therapy, particularly in the treatment of neurodegenerative ... | 08/27/2002 |
| 6277852 | Piperazinyl 5-HT1 agonists and antagonists A compound of the formula ##STR1## or the pharmaceutically acceptable salt thereof, wherein Z is oxygen, S(O)m wherein m is 0, 1 or 2; or NQ wherein Q is hydrogen, (C1 -C6)alkyl or phenyl; X is hydrogen, chloro, fluoro, bromo, ... | 08/21/2001 |
| 6218394 | 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophene-methyl) piperazines 4-Aryl-1-(indanmethyl, dihydrobenzofuramethyl or dihydrobenzothiophenemethyl) piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I) ##STR1## wherein one of X and Y is CH2, and the other one is CH2, O or S; ... | 04/17/2001 |
| 6150356 | Potassium channel inhibitors and method Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure ##STR1## where A, B, D, Q, X1, R, R1, X2 and R2 are as defined herein. These compounds... | 11/21/2000 |
| 6143744 | Sulfamide-metalloprotease inhibitors This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.... | 11/07/2000 |
| 6066631 | Chroman derivatives The present invention relates to chroman derivatives of the formula (I): ##STR1## [wherin R1 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C3-6 alkoxymethyl group, e... | 05/23/2000 |
| 6060468 | N-substituted azaheterocyclic compounds The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R1, R1a, R2, R2a, p, r and s are as defined in the detailed part of the presen... | 05/09/2000 |
| 6054437 | Method for inducing death of neoplastic cells using piperazine derivatives A method for inducing cell death in neoplastic cells, includes the step of administering a compound of formula I or a pharmaceutically acceptable salt thereof, as a primary chemotherapeutic agent or substantially contemporaneously with chemotherapy, to a ... | 04/25/2000 |
| 5935958 | Muscarinic antagonists Di-N-substituted piperazine or 1,4-di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein Q, n, R, R1, R2, R3, R4, R21 | 08/10/1999 |
| 5922719 | Coumarin dopamine D4 receptor antagonists This invention relates to compounds that are antagonists of dopamine D4 receptors, to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors, and to pharmaceutically acceptable compositions that con... | 07/13/1999 |
| 5916889 | 1,4-disubstituted piperazines The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R1, R2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their ... | 06/29/1999 |
| 5866578 | Substituted pyrimidines for control of diabetic complications This invention relates to methods of inhibiting sorbitol dehydrogenase, lowering fructose levels, and treating or preventing diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic microangiopathy or diabet... | 02/02/1999 |
| 5861397 | Piperazine based cytofectins The present invention relates to piperazine based amphilic cationic lipids useful for gene therapy, transfection, and introducing immunogenic compounds for the purpose of vaccination. The disclosed compounds have lipophilic moieties linked to the ring nit... | 01/19/1999 |
| 5859013 | Method for inducing death of neoplastic cells using piperazine derivatives A method for inducing cell death in neoplastic cells, includes the step of administering a compound of formula I or a pharmaceutically acceptable salt thereof, as a primary chemotherapeutic agent or substantially contemporaneously with chemotherapy, to a ... | 01/12/1999 |
| 5856323 | Compounds and methods for the treatment of disorders mediated by platelet activating factor or products of 5-lipoxygenase 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respira... | 01/05/1999 |
| 5837708 | Sulphonamides Compounds of the formula ##STR1## wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders which are associated with endothelin activities, ... | 11/17/1998 |
| 5807860 | Urea derivatives A compound represented by formula (I) and a salt thereof, and a hydrate and solvate thereof: ##STR1## wherein R1, R2 and R3 represent independently, for example, hydrogen atom, hydroxyl group, or C1-3 alkox... | 09/15/1998 |
| 5763444 | Antidepressant 1-arylalkyl-4-(alkoxy pyridinyl)-and 4-(alkoxypyrimidinyl) piperazine derivatives Novel compound of formula I and pharmaceutically acceptable salts thereof are useful CNS agents: ##STR1## wherein X is CH or N; X' is CH or a direct covalent link; Y is CH, CH2 or N; Y' is N, NH, O or S; R1 is H, Br, Cl, F, C1-4... | 06/09/1998 |
