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| Number | Title | Issue Date |
| 8153816 | Process for production of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-OXO-2-substituted-2,3-dihydro-1,2-benzisoxazol-6-yl)methoxy]phenyl]propionate ester and intermediate for the process A 6-(halomethyl)-1,2-benzisoxazol-3(2H)-one derivative represented by the formula: wherein R5 is a methyl group that is substituted with one or more optionally substituted phenyl groups, or an optionally substitu... | 04/10/2012 |
| 8034955 | Therapeutic compounds and methods of use Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis. ... | 10/11/2011 |
| 8017789 | Process for production of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-OXO-2-substituted-2,3-dihydro-1,2-benzisoxazol-6-yl]methoxy]phenyl]proprionate ester and intermediate for the process A preparation method using as an intermediate 6-(halomethyl)-1,2-benzisoxazol-3(2H)-one derivative represented by general formula wherein R5 is a methyl group that is substituted with one or more optionally subst... | 09/13/2011 |
| 7977492 | Crystal of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl]propionic acid The crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid having peaks at the position of 14.0, 16.0, 23.3, 23.7 and 26.3° and the crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-... | 07/12/2011 |
| 7960559 | Synthesis of enone intermediate The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously suscep... | 06/14/2011 |
| 7893275 | Polycyclic ketone compound and process for producing the same The present application provides polycyclic ketone compounds that have a quarternary asymmetric carbon center and conform to Formula (I): Also provided is a stereoselective method for synthesizing the polycyclic ketone comp... | 02/22/2011 |
| 7807842 | Synthesis of tetracyclines and analogues thereof The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously suscep... | 10/05/2010 |
| 7459564 | Substituted biaryl compounds as factor XIa inhibitors The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein.... | 12/02/2008 |
| 7453001 | Isoxazole derivatives and process for producing the same The present invention provides isoxazole derivatives represented by the following formula (I): (wherein R1 represents a hydrogen atom, C1-C20 hydrocarbon group or —C(═O)OR1a (... | 11/18/2008 |
| 7414132 | Opioid receptor antagonists A compound of the formula (I); wherein the variables X1 to X10, R1 to R7 including R3′, E, W, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereom... | 08/19/2008 |
| 7393960 | Indoles having anti-diabetic activity Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipi... | 07/01/2008 |
| 7375126 | Fused compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor The present invention discloses novel compounds of general formula (I) or a pharmaceutically acceptable salt or prodrug thereof (in which X1-X5, R5-R8b, Z1-Z2 | 05/20/2008 |
| 7375233 | Process for the preparation of zonisamide and the intermediates thereof The present invention provides a novel and improved process for the preparation of Zonisamide and the intermediates thereof. In one aspect of the present invention, the process provides for: the preparation and isolation of a novel crystalline form of anhydrous 1,2-... | 05/20/2008 |
| 7342036 | Isoxazole derivatives and process for producing the same The present invention provides isoxazole derivatives represented by the following formula (I): (wherein R1 represents a hydrogen atom, C1-C20 hydrocarbon group or —C(═O)OR1a (... | 03/11/2008 |
| 7291638 | 3-amido-1,2-benzoisoxazole derivatives, process for preparation, and use thereof The present invention relates to 3-amido-1,2-benzoisoxazole derivatives and their salts represented by formula 1, processes for preparation and usees thereof. More particularly, it relates to a method for improving its bioavailability introducing amino acid residue ... | 11/06/2007 |
| 7291742 | Process for the preparation of benzo [d] isoxazol-3-yl-methanesulfonic acid and the intermediates thereof A process for the preparation of benzo[d]isoxazol-3-yl-methanesulfonic acid of formula (I), or a salt thereof, and the intermediates thereof, useful as an intermediate in the preparation of zonisamide. ... | 11/06/2007 |
| 7268234 | Method for sulfonation of 1,2-benzisoxazole-3-acetic acid An efficient method for the preparation of 1,2-benzisoxazole-3-methanesulfonic acid involves a reaction of 1,2-benzisoxazole-3-acetic acid in toluene with chlorosulfonic acid optionally mixed with an inert solvent in the presence of a particular Lewis base (ester or... | 09/11/2007 |
| 7265220 | Amino acid derivatives, method for production thereof and pharmaceutical compositions comprising said derivative Compound of formula (I): wherein: R1 represents aryl, heteroaryl or alkyl which is optionally substituted, or a group of formula —(CO)—CR6R7NR8R9 ... | 09/04/2007 |
| 7262304 | One-pot process for the preparation of 1,2-benzisoxazole-3-methanesulfonamide A process for the preparation of 1,2-benzisoxazole-3-methanesulfonamide without isolation of intermediates in solid form, by using 4-hydroxycoumarin as a starting compound, and water and 1,2-dichloroethane as solvents; and an industrially useful process for the prep... | 08/28/2007 |
| 7253165 | Benzisoxazolyl-, pyridoisoxazolyl-and benzthienyl-phenoxy derivatives useful as Dantagonists The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These c... | 08/07/2007 |
| 7235575 | Guanidine mimics as factor Xa inhibitors The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which a... | 06/26/2007 |
| 7217727 | Phospholipase inhibitors A novel class of 3-oxo-3H-benzo[d]isoxazole carboxamide compounds is disclosed together with the use of such compounds for inhibiting hepatic lipase and/or endothelial lipase activity for treatment, amelioration or prevention of hepatic lipase and/or endothelial lip... | 05/15/2007 |
| 7166725 | Benzo[d]isoxazol-3-ol DAAO inhibitors Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia, or neuropathic pain, or preventing loss... | 01/23/2007 |
| 7153960 | Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibi... | 12/26/2006 |
| 7144907 | Heterocyclic inhibitors of MEK and methods of use thereof Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W and Y a... | 12/05/2006 |
| 7125863 | Inhibitors of dipeptidyl peptidase IV Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of t... | 10/24/2006 |
| 7125903 | Thienoisoxazolyl-and thienylpyrrazolyl-phenoxy substituted propyl derivatives useful as Dantagonists The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. Th... | 10/24/2006 |
| 7125865 | Therapeutic compounds for treating dyslipidemic conditions The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol. | 10/24/2006 |
| 7122534 | Aryl fused azapolycyclic compounds The present invention relates to compounds of formula (I) and their pharmaceutically acceptable salts, wherein R1, R2, R3 and Z are as defined herein, intermediates in the synthesis of ... | 10/17/2006 |
| 7119104 | Activator of peroxisome proliferator-activated receptor delta A compound represented by the formula (I) or a salt of the compound, and a PPAR-δ activator which contains the compound or salt as the active ingredient: (wherein A represents O or S; B | 10/10/2006 |
| 7115545 | Tricyclic benzoylpyrazole derivatives used as a herbicide Tricyclic benzoylpyrazole derivatives of the formula I wherein X, Y, R1, R2, R6, R7, R3, R4, R5, l, R8 and R9 are... | 10/03/2006 |
| 7105564 | Pharmaceutical composition comprising a dual antagonist against PGD/TXAreceptors having a [2.2.1] or [3.1.1] bicyclic skeleton The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D2 receptor and pharmaceutical compositions comprising them. A compound of the formula (I): | 09/12/2006 |
| RE39265 | Heteroarylpiperidines, and their use as antipsychotics and analgetics Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compound... | 09/05/2006 |
| 7091230 | 2-aryloxy-2-arylalkanoic acids for diabetes and lipid disorders A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyper... | 08/15/2006 |
| 7081539 | One-pot process for the preparation of 1,2-benzisoxazole-3-methanesulfonamide A process for the preparation of 1,2-benzisoxazole-3-methanesulfonamide without isolation of intermediates in solid form, by using 4-hydroxycoumarin as a starting compound, and water and 1,2-dichloroethane as solvents; and an industrially useful process for the prep... | 07/25/2006 |
| 7038059 | Process for preparation of 4-n-substituted amino-2-aza-1-oxabicyclo[3.3.0] oct-2-ene-6-carboxylic acid esters and process for preparation of their intermediates 4-N-substituted amino-2-aza-1-oxabicyclo[3.3.0]oct-2-ene-6-carboxylic acid esters are produced by adding a Brønsted acid to a mixture of a 2-azabicyclo[2.2.1]hept-5-en-3-one and an alcohol, thereby causing these components to react with each other to give a salt of... | 05/02/2006 |
| 7015330 | Sulfonation method for zonisamide intermediate in zonisamide synthesis and their novel crystal forms The present invention relates to a novel sulfonation of an intermediate of zonisamide. The sulfonation processes using chlorosulfonic acid as well as acetic anhydride and sulfuric acid in an organic solvent are disclosed. Crystalline forms of benzisoxazole methane s... | 03/21/2006 |
| 6958356 | Guanidine mimics factor Xa inhibitors The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are use... | 10/25/2005 |
| 6949550 | Substituted amino methyl factor Xa inhibitors The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa. ... | 09/27/2005 |
| 6949556 | Acylated 1,2,3,4-tetrahydronaphthyl amines and their use as pharmaceutical agents The present invention relates to compounds of general formula (I), wherein R1-R4 have the meanings given in the specification, A is CH2, CHOH or CH—(C1-C3-alkyl), B and C a... | 09/27/2005 |
