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| Number | Title | Issue Date |
| 8163730 | Fused tricyclic compounds as inhibitors of tumor necrosis factor-alpha Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R... | 04/24/2012 |
| 7713956 | Dealkylated derivatives of pyrrolo[2,1-b]benzothiazepines with atypical antipsychotic activity Derivatives of pyrrolo[2,1-b]benzothiazepines with formula (I) where A is CH—CH2C═CH; R is hydrogen, halogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, C5-C6 cyc... | 05/11/2010 |
| 7696192 | Tricyclic anilide spirolactam CGRP receptor antagonists The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R | 04/13/2010 |
| 7419969 | HIV integrase inhibitors: cyclic pyrimidinone compounds The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates us... | 09/02/2008 |
| 7407949 | Benzamide derivatives as oxytocin agonists and vasopressin antagonists Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds ... | 08/05/2008 |
| 7320973 | Dihydrodiaryloxazepine derivative and pharmaceutical composition containing the same The present invention provides dihydrodiaryloxazepine derivative represented by the following formula [1], analogs thereof and pharmaceutical compositions containing them. Those compounds have an excellent effect of improving functional diseases of gastrointestinal ... | 01/22/2008 |
| 7273859 | HIV integrase inhibitors: cyclic pyrimidinone compounds The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates us... | 09/25/2007 |
| 7148214 | Antihistaminic spiro compounds This invention concerns the compounds of formula or a prodrug, a N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof wherein R1, R2, —A—B—, L, and n hav... | 12/12/2006 |
| 7119088 | Triazole compounds useful in therapy A compound of formula (I), or a pharmaceutically acceptable derivative thereof, wherein A, B, V, W, X, Y, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof. ... | 10/10/2006 |
| 7105172 | Treatment of rosacea Disclosed herein are methods for the treatment or prevention of rosacea in a patient, including administering a compound that inhibits one or more components of the bradykinin activation pathway in an amount sufficient to reduce or prevent one or more symptoms of ro... | 09/12/2006 |
| 7087595 | Antihistaminic spiro compounds This invention concerns the compounds of formula or a prodrug, a N-oxide, an addition salt, a quaternary amine or a stereochemically isomeric form thereof wherein R1, R2, -A-B—, L, and n h... | 08/08/2006 |
| 7078521 | Process for the preparation of 9-amino substituted 9,10-dihydropyrrolo[2,1-b][1,3]benzotiazepines A process is described for the preparation of compounds with the following formula where the groups are as defined below; in particular, R1 is a substituted amine; said process includes essentially the reaction of pyrrolobenzothiazepin-9-one with amine R | 07/18/2006 |
| 7041661 | Use of thiazolobenzoheterocycles for treating multiple sclerosis The invention relates to the use of compound of Formula I in treating patients for inflammatory or neuropathic pain as well as various symptoms of multiple sclerosis ... | 05/09/2006 |
| 6806267 | Apoptosis-inducing compounds The present invention relates to pyrrolobenzoxazepines, pyrrolobenzthiazepines and related compounds having the ability to induce apoptosis, to pharmaceutical compositions comprising these compounds and to their use as anti-tumour agents. ... | 10/19/2004 |
| 6794391 | Derivatives of pyrimido[6.1-a]isoquinolin-4-one The invention provides compounds or salts thereof of the general formula (I): wherein each of R1 and R2 independently represents a C1-6 alkyl or C2-7 acyl group; X represents O... | 09/21/2004 |
| 6649614 | Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent for treatment of depression or anxiety The present invention relates to the treatment of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and an antidepressant or anti-anxiety agent.... | 11/18/2003 |
| 6512004 | Promoters of neural regeneration The invention provides methods and compositions for promoting neural cell growth and/or regeneration. The general methods involve contacting with an activator of a cyclic nucleotide dependent protein kinase a neural cell subject to growth repulsion mediat... | 01/28/2003 |
| 6468971 | Maintaining kidney function during surgery or trauma Kappa-opioid agonists prevent the impairment of renal function otherwise caused by the combination of gaseous anesthesia and surgery or severe trauma. Not only do these agents preserve renal function and maintain urine output, they also maintain plasma el... | 10/22/2002 |
| 6444664 | Method for controlling the plasma level of lipoproteins to treat alzheimeris disease A compound which is an antagonist of platelet activating factor (PAF-antagonist) or a structurally related compound thereof not having PAF-antagonistic activity can be used for decreasing the plasma level of lipoprotein(a) and/or increasing the plasma lev... | 09/03/2002 |
| 6391870 | Pyrrolo [2,1-b][1,3]benzothiazepines with atypical antipsychotic activity Polycondensated heterocycles with a pyrrole[2,1-b][1,3]benzothiazepine structure of the following formula (I) ##STR1## where the groups are defined as in the description are disclosed. As compared to known antipsychotic agents, these compounds present ... | 05/21/2002 |
| 6268352 | Promoters of neural regeneration The invention provides methods and compositions for promoting neural cell growth and/or regeneration. The general methods involve contacting with an activator of a cyclic nucleotide dependent protein kinase a neural cell subject to growth repulsion mediat... | 07/31/2001 |
| 6191126 | Topical use of .kappa. opioid agonists to treat ocular pain The present invention relates to the pharmaceutical treatment of pain. In particular, the present invention relates to the topical use of kappa opioid receptor agonists and partial agonists for the prevention or alleviation of pain in the eye.... | 02/20/2001 |
| 6174878 | Topical use of kappa opioid agonists to treat otic pain Compositions and methods for treating otic pain are disclosed. In particular, the invention discloses compositions and methods of using kappa opioid agonists locally for the prevention or alleviation of otic pain.... | 01/16/2001 |
| 6127362 | 9,10-diazatricyclo[4,4,1,12,5 ] decane and 2,7-diazatricyclo [4,4,0,03,8 ] decane derivatives having analgesic activity 9,10-DIAZATRICYCLO[4,4,1,12,5 ]DECANE (la) AND 2,7-DIAZATRICYCLO[4,4,0,03,8 ]DECANE (1b) DERIVATIVES HAVING ANALGESIC ACTIVITY. ##STR1##... | 10/03/2000 |
| 6114329 | 5-HT4 receptor antagonists useful in the treatment of gastroinstestinal, cardiovascular and CNS disorders Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof: X--CO--CH2 --Z (I) wherein X is a monocyclic or po... | 09/05/2000 |
| 5852014 | Condensed indole derivatives as 5HT4 -receptor antagonists Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.... | 12/22/1998 |
| 5834459 | Alkyl-substituted compounds having dopamine receptor affinity Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings; X1 is selected from CH | 11/10/1998 |
| 5753649 | Therapeutic agent for osteoporosis and diazepine compound A therapeutic agent for osteoporosis, comprising an azepine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof as an active ingredient, a method for treating ost... | 05/19/1998 |
| 5705498 | Piperidine derivatives as 5-HT4 receptor antagonists Compounds of formula (I): ##STR1## wherein Xg is O, S, SO, SO2, CH2, CH, N or NR wherein R is hydrogen or C1-6 alkyl; A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms; R1g | 01/06/1998 |
| 5536715 | Combinations of anthelmintically active agents Pharmaceutical compositions comprising a compound of formula (I) and at least one other anthelmintically active compound, being an avermectin or a milbemycin, are useful in the treatment of helminthiasis. In formula (I): R is optionally substituted phenyl... | 07/16/1996 |
| 5104868 | Tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and esters This invention relates to novel tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and certain esters and cation salts thereof. The compounds of this invention are substituted at the 7-position by vinyl, W--CH.dbd.C... | 04/14/1992 |
| 4985420 | 1,7-annelated indolecarboxylic acid esters and -amides The invention relates to new 1,7-annelated esters and amides of indolecarboxylic acids having general formula 2, ##STR1## wherein the symbols have the meanings given in the specification. The compounds and their salts are very strong and selective an... | 01/15/1991 |
| 4918069 | Spiro[(piperidine- pyrrolidine- or hexahydroazepinyl substituted) pyrrolo[2,][1,4]benzoxazepines] This invention relates to spiro-[(piperidine-, pyrrolidine-, or -hexahydroazepinyl substituted) pyrrolo[2,1-c][1,4]-benzoxazepines] having the following formula ##STR1## wherein R is hydrogen, lower alkyl, arylloweralkyl, acyl, lower alkenyl, lo... | 04/17/1990 |
| 4865764 | 5-aryl-11-substituted-5H,11H-pyrrolo[2,1-][1,4]benzoxazepines as hypotensive agents There are disclosed compounds of the formula, ##STR1## where X and Y are each independently hydrogen, loweralkyl, halogen or trifluoromethyl; Z is hydrogen or 2- or 3-Cl, Br, I, CHO or CH.dbd.CR1 R2 where R1 and R | 09/12/1989 |
| 4814344 | Indole derivatives The invention relates to compounds of formula (I) ##STR1## wherein R1 represents a hydrogen atom or a group selected from C1-10 alkyl, C3-6 alkenyl, C3-10 alkynyl, C3-7 cycloalkyl, C3-7 | 03/21/1989 |
| 4812450 | Spiro((piperidine-pyrrolidine- or hexahydroazepinyl substituted) pyrrolo(2,1-C) (1,4)benzoxazepines) This invention relates to spiro-[(piperidine-, pyrrolidine-, or -hexahyroazepinyl substituted) pyrrolo[2,1-c][1,4]-benzoxazepines] having the following formula ##STR1## wherein R is hydrogen, lower alkyl, arylloweralkyl, acyl, lower alkenyl, low... | 03/14/1989 |
| 4794110 | 5-Aryl-11-substituted-5H,11H-pyrrolo[2,1-c][1,4]benzoxazepined as analgesic and hypotensive agents There are disclosed compounds of the formula, ##STR1## where X and Y are each independently hydrogen, loweralkyl, halogen or trifluoromethyl; Z is hydrogen or 2- or 3-Cl, Br, I, CHO or CH.dbd.CR1 R2 where R1 and R | 12/27/1988 |
| 4758559 | Pyrrolo[1,2-a] [4,1]benzoxazepine derivatives useful as calmodulin and histamine inhibitors Disclosed are the compounds of the formula ##STR1## wherein n represents the integer 1,2,3 or 4; R1 represents hydrogen, lower alkyl, halogen, trifluoromethyl, hydroxy or lower alkoxy; R2 represents hydrogen or lower alkyl; R | 07/19/1988 |
| 4681879 | 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines as antipsychotic and analgesic agents There are described novel 11-substituted 5H,11H-pyrrolo[2,1-c][1,4]benzoxazepines of the general formula ##STR1## where m and n are each independently 0, 1 or 2 and m+n is 1 or 2, X and Y are each independently hydrogen, loweralkyl or halogen, and R ... | 07/21/1987 |
| 4659734 | Olinecarboxylic acid derivatives A compound of the formula ##STR1## R1 is hydrogen, alkali metal, alkaline earth metal, lower alkyl, pivaloyloxymethyl or phthalidyl; R2, R3, R4 and R5 are the same or different and are hydrogen, ... | 04/21/1987 |
