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| Number | Title | Issue Date |
| 8110566 | Therapeutic agents 713 Disclosed herein are compounds of formula I in which R1, R2, R3, R4, R5, A, X, Y are as described in the specification, their use in pharmaceutical compositions and in ... | 02/07/2012 |
| 8022057 | MAPK/ERK kinase inhibitors Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; metho... | 09/20/2011 |
| 7915249 | Heterocyclic tetracyclic tetrahydrofuran derivatives as 5HTinhibitors in the treatment of CNS disorders This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamin... | 03/29/2011 |
| 7897594 | Preventive/remedy for retinal nerve diseases containing alkyl ether derivatives or salts thereof An alkyl ether derivative represented by the following general formula [1] or its salt: wherein R1 and R2 represent each a substituent such as hydrogen, halogeno or alkyl; R3 represents alky... | 03/01/2011 |
| 7754708 | N-aryl azaspiroalkene and azaspiroalkane compounds and methods of preparation and use thereof Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptab... | 07/13/2010 |
| 7598236 | Diazabicyclic central nervous system active agents Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals. ... | 10/06/2009 |
| 7384929 | N-aryl azaspiroalkene and azaspiroalkane compounds and methods of preparation and use thereof Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptab... | 06/10/2008 |
| 7288563 | Substituted bicycloalkylamine derivatives as modulators of chemokine receptor activity The present application describes modulators of MCP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein X, Z, a, b, c, d, bond g, n, s, R1, R2, R4 | 10/30/2007 |
| 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 |
| 7217705 | Combination of a CB1 receptor antagonist and of a product which activates dopaminergic neurotransmission in the brain, the pharmaceutical compositions comprising them and their use in the treatment of parkinson's disease The present invention relates to the combination of one or more CB1 antagonist azetidine derivatives and of one or more products which activate dopaminergic neurotransmission in the brain, to the pharmaceutical compositions comprising them and to their use in the tr... | 05/15/2007 |
| 7172767 | Opioid agonist / antagonist combinations The invention is directed in part to oral dosage forms comprising a combination of an orally analgesically effective amount of an opioid agonist and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide ... | 02/06/2007 |
| 7141598 | Imidazole derivatives, production method thereof and use thereof The present invention provides a compound having a steroid C17,20-lyase-inhibitory activity and useful for the therapy and prophylaxis of tumor such as prostatism, breast cancer and the like, and a method for efficiently separating an optically active com... | 11/28/2006 |
| 7135465 | Sustained release beadlets containing stavudine Extended dosage forms of stavudine are provided comprising beadlets formed by extrusion-spheronization and coated with a seal coating. The beadlets are also coated with a modified release coating such that a hard gelatin capsule containing such beadlets will provide... | 11/14/2006 |
| 7132441 | Immunosuppressive effects of administration of a cyclooxygenase-2 inhibitor and a 5-lipoxygenase inhibitor This invention is in the field of a combination comprising a therapeutically-effective amount of a cyclooxygenase-2 inhibitor, a 5-lipoxygenase inhibitor and an immunosuppressive drug selected from antiproliferative agents, antiinflammatory-acting compounds and inhi... | 11/07/2006 |
| 7105504 | Combination of a CB1 receptor antagonist and of a product which activates dopaminergic neurotransmission in the brain, the pharmaceutical compositions comprising them and their use in the treatment of parkinson's disease The present invention relates to the combination of one or more CB1 antagonist azetidine derivatives and of one or more products which activate dopaminergic neurotransmission in the brain, to the pharmaceutical compositions comprising them and to their use in the tr... | 09/12/2006 |
| 6821964 | Modulators of chemokine receptor activity Chemokine receptor antagonists, in particular, bicyclic diamine compounds of Formula (I) that act as antagonists of chemokine CCR2 and CCR3 receptors including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumul... | 11/23/2004 |
| 6602864 | Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibit... | 08/05/2003 |
| 6489354 | 3-alkyl substituted pyrrolidine modulators of chemokine receptor activity The present invention is directed to pyrrolidine compounds of the formula I: ##STR1## (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine ... | 12/03/2002 |
| 6350760 | Substituted piperidines as melanocortin-4 receptor agonists Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention ... | 02/26/2002 |
| 6271264 | Polymers containing spirobicyclic ammonium moieties as bile acid sequestrants The present invention relates to a method for sequestering bile acids in a patient and to particular polymers for use in the method. The method comprises administering a therapeutically effective amount of a spirobicyclic ammonium moiety-containing polyme... | 08/07/2001 |
| 6113527 | Diaza-spiro[3,5] nonane derivatives The invention relates to compounds of the general formula ##STR1## wherein R1 is C6-12 -cycloalkyl, optionally substituted by lower alkyl or C(O)O lower alkyl, indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; ace... | 09/05/2000 |
| 6083957 | Heterocyclic compounds and their preparation and use The present invention relates to therapeutically active quaternary azacyclic or azabicyclic compounds with formula I: ##STR1## wherein X is oxygen or sulfur and wherein G is selected from the group of azacyclic or azabicyclic ring systems consisting ... | 07/04/2000 |
| 6051575 | Piperazino derivatives as neurokinin antagonists The invention relates to compounds of the formula ##STR1## wherein Z, Rc, y, m, u, Ar2, n, X, Rc', I and Ar2 are as described herein. These compounds are neurokinin antagonists. These compounds are useful i... | 04/18/2000 |
| 6013644 | Spiro-substituted azacycles as modulators of chemokine receptor activity The present invention is directed spiro-substituted azacycles of formula I: (wherein R1, R2, R3, R4, R5, k, l and m are defined herein) which are useful as modulators of chemokine receptor activity. I... | 01/11/2000 |
| 5998404 | Heterocyclic compounds and their use The present invention relates to therapeutically active azacyclic or azabicyclic compounds of formula I ##STR1## and to pharmaceutical formulations comprising these compounds and methods of treatment comprising administering these compounds to a subj... | 12/07/1999 |
| 5998434 | Composition for treating pain The present invention provides a composition and method for treating pain using Selected Muscarinic Compounds and one or more compounds selected from the group consisting of Nonsteroidal Anti-inflammatory drugs, acetaminophen, opioids, and alpha-adrenergi... | 12/07/1999 |
| 5962447 | Benzoxazines for enhancing synaptic response Compounds based on the benzoxazine ring system are disclosed for use in enhancing synaptic responses mediated by AMPA receptors. The compounds are effective in the treatment of subjects suffering from impaired nervous or intellectual functioning due to de... | 10/05/1999 |
| 5888999 | Method for treating anxiety with muscarinic cholinergic receptor agonists The present invention relates a method for treating anxiety using azacyclic and azabicyclic pyrazine compounds.... | 03/30/1999 |
| 5889022 | Indole, indoline and quinoline derivatives with 5HT1D (anti-depressive) activity Novel indole, indoline and quinoline derivatives of formula (I) processes for their preparation, pharmaceutical compositions containing them, and their use in medicine is disclosed. A structurally distinct class of compounds have now been discovered and h... | 03/30/1999 |
| 5834458 | Heterocyclic compounds and their use The present invention relates to therapeutically active heterocyclic compounds and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the m... | 11/10/1998 |
| 5763457 | Method for treating anxiety The present invention relates a method for treating anxiety using azacyclic and azabicyclic oxadiazole compounds.... | 06/09/1998 |
| 5760029 | Spirocycle integrin inhibitors This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3-8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspi ro-4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are useful as antagonists of the v ଲ | 06/02/1998 |
| 5736543 | Benzoxazines for enhancing synaptic response Compounds based on the benzoxazine ring system ##STR1## are disclosed for use in enhancing synaptic responses mediated by AMPA receptors. The compounds are effective in the treatment of subjects suffering from impaired nervous or intellectual functio... | 04/07/1998 |
| 5712287 | Method of treating urinary bladder dysfunctions The present invention relates to a novel method for treating a mammal suffering from urinary bladder dysfunctions.... | 01/27/1998 |
| 5665745 | Heterocyclic compounds and their preparation and use The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nerv... | 09/09/1997 |
| 5646154 | Pharmaceutical compositions for inhibiting the formation of tumor necrosis factor Quinazoline compounds represented by general formula (1) or (2) possess an activity of significantly inhibiting the production or secretion of a tumor necrosis factor and are useful as drugs for the treatment of diseases wherein a tumor necrosis factor is... | 07/08/1997 |
| 5605908 | Heterocyclic compounds and their use The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nerv... | 02/25/1997 |
| 5574028 | Method for treating anxiety The present invention provides a method for treating anxiety in a human in need thereof, comprising administering to the human an antianxiety amount of a muscarinic agonist compound of the general formula ##STR1## wherein Z is a 5-membered heterocycl... | 11/12/1996 |
| 5556851 | Cinnoline-3-carboxylic acid derivatives A novel cinnoline derivative having an antagonistic activity against serotonin 5-HT3 receptor, its pharmaceutically acceptable salts, its N-oxide derivatives or solvates thereof, and pharmaceutical formulations containing the same for the preve... | 09/17/1996 |
| 5541194 | Certain 1-azabicyclo[2.2.1]heptanes and 1-azabicyclo[2.2.2]octanes Novel compounds of formula (I), processes for their preparation, and their use as pharmaceutical agents are described: ##STR1## in which p represents an integer of 2 to 4; r represents an integer of 1 or 2; s represents 0 or 1; and X represents a gro... | 07/30/1996 |
