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| Number | Title | Issue Date |
| 8420823 | Long-chain fatty acyl elongase inhibitor comprising arylsulfonyl derivative as active ingredient [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [M... | 04/16/2013 |
| 8420824 | Substituted pyrazoles, compositions containing these, method of production and use The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; c... | 04/16/2013 |
| 8410278 | Method for preparing a non-hydratable crystal form A method is disclosed for preparing a non-hydratable crystal form from a hydratable crystal form of 3-bromo-1-(3-chloro-2-pyridinyl)-N-[4-cyano-2-methyl-6-[(methylamino)-carbonyl]phenyl]-1H-pyrazole-5-carboxamide (Compound 1). ... | 04/02/2013 |
| 8399679 | Aryl-substituted pyrazoles The present invention relates to a process for preparing 1-aryl-substituted pyrazoles, comprising the reaction of alkoxy enones and enamino ketones with arylhydrazine derivatives to give 1-aryl-substituted dihydro-1H-pyrazoles, the further reaction thereof with elim... | 03/19/2013 |
| 8362261 | Process for preparing pyridyl-substituted pyrazoles The present invention relates to a process for preparing 1-pyridyl-substituted pyrazoles, comprising the reaction of acetyleneketones with pyridylhydrazine derivatives to give 1-pyridyl-substituted dihydro-1H-pyrazoles, the further reaction thereof with elimination ... | 01/29/2013 |
| 8324390 | Tetrazole-substituted anthranilamides as pesticides The present invention relates to tetrazole-substituted anthranilamides of the formula (I) in which R1, R2, R3 R4, R5, n, X and Q have the meanings given in the descript... | 12/04/2012 |
| 8299260 | Process for preparing aryl-substituted pyrazoles The present invention relates to a process for preparing 1-aryl-substituted pyrazoles, comprising the reaction of alkoxy enones and enamino ketones with arylhydrazine derivatives to give 1-aryl-substituted dihydro-1H-pyrazoles, the further reaction thereof with elim... | 10/30/2012 |
| 8293917 | Pyrazole compounds as CCR1 antagonists Disclosed are compounds of the formula (I) which block the interaction of CCR1 and its ligands and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rhe... | 10/23/2012 |
| 8247569 | Cyclohexane derivative and pharmaceutical use thereof A compound has a strong analgesic action against both nociceptive pain and neuropathic pain and has less side effects, and is medically useful. The compound includes cyclohexane derivatives represented by the following compound, or pharmaceutically acceptable salts ... | 08/21/2012 |
| 8242279 | Process for preparing 2-amino-5-cyanobenzoic acid derivatives Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with a metal cyanide reagent, a copper(I) salt reagent, an iodide salt reagent and at least one compound of Formula 3 ... | 08/14/2012 |
| 8217179 | Preparation method of phenylcarboxamides A preparation method of phenylcarboxamides of formula (I), the reaction scheme of which is as follows: wherein the groups are defined in the description. In this method, 3-halo-1-(3-chloro-2-pyridinyl)-4,5-dihydro-1H-pyrazo... | 07/10/2012 |
| 8183381 | N-linked heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. ... | 05/22/2012 |
| 8119811 | Method for producing amide compound Disclosed is a method for producing an amide compound represented by the formula (3) below and having an excellent control activity against a harmful arthropod, which is characterized in that an aniline compound represented by the formula (1) below and an aldehyde c... | 02/21/2012 |
| 8115006 | Process for producing anthranilamide compound To provide a process for producing a specific anthranilamide compound or its salt. To provide a process for producing an anthranilamide compound represented by the formula (I) or its salt: wherein each of R1a | 02/14/2012 |
| 8101773 | Hydroxy methyl phenyl pyrazolyl urea compounds useful in the treatment of cancer The compound 4-{4-[({3-tert-Butyl-1-[3-(hydroxymethyl)phenyl]-1H-pyrazol-5-yl}carbamoyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide and alternative forms thereof (e.g., salts, solvates, hydrates, prodrugs, polymorphs and metabolites); pharmaceutical compo... | 01/24/2012 |
| 8071782 | Synthesis of 1,3,4-trisubstituted and 1,3,4,5-tetrasubstituted pyrazoles This invention concerns the synthesis of highly substituted pyrazoles, which are structural components of pharmacological compounds, through reaction of hydrazones with nitroolefins. ... | 12/06/2011 |
| 7951953 | Conversion of 2-pyrazolines to pyrazoles using bromine This invention relates to a method for preparing a compound of Formula 1 wherein L, R1, R2 and X are as defined in the disclosure, comprising contacting a 2 pyrazoline of Formula 2 with bromine at a temperature of at least about 80° C. (Formul... | 05/31/2011 |
| 7919627 | Processes for the preparation of hydroxylamines The present invention relates generally to novel methods for the synthesis of O-(6-pyrazol-1-yl-pyridin-3-ylmethyl)-hydroxylamine which is an essential reagent in the synthesis of one of the bridged erythromycin derivatives and their respective pharmaceutically acce... | 04/05/2011 |
| 7855297 | Amide derivatives and medicinal use thereof The present invention relates to an amide derivative of the formula (1), having a C5a receptor antagonistic action wherein each symbol is as defined in the specification. The above-mentioned amide derivative, an opt... | 12/21/2010 |
| 7834186 | Preparation and use of 2-substituted-5-oxo-3-pyrazolidinecarboxylates A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(... | 11/16/2010 |
| 7812170 | Insecticides Compounds of the formula (I) in which Z, is an oxygen atom; or a sulfur atom; Z2 is an oxygen atom; or a sulfur atom; R, is an aryl or heteroaryl group, which is unsubstituted or substituted; R2 is hydrogen; or an organic substituent; R3 | 10/12/2010 |
| 7538225 | Processes for the preparation of o-(6-pyrazol-1-yl-pyridin-3-ylmethyl)-hydroxylamine The present invention relates generally to novel methods for the synthesis of O-(6-pyrazol-1-yl-pyridin-3-ylmethyl)-hydroxylamine which is an essential reagent in the synthesis of one of the bridged erythromycin derivatives and their respective pharmaceutically acce... | 05/26/2009 |
| 7442702 | Prostaglandin agonists This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatmen... | 10/28/2008 |
| 7442799 | Preparation and use of 2-substituted-5-oxo-3-pyrazolidinecarboxylates A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I. The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(R2b)C(O)Y (i.e. Formula II)wher... | 10/28/2008 |
| 7414060 | Pyridine-2-carboxyamide derivatives The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods... | 08/19/2008 |
| 7414055 | Inhibitors of Akt activity The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this inven... | 08/19/2008 |
| 7407972 | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thro... | 08/05/2008 |
| 7396929 | Synthesis of 3-amino-4-substituted pyrazole derivatives This application discloses a novel process to synthesize 3-amino-4-substituted pyrazole derivatives, which may be used, for example, as intermediates to prepare compounds having, for example, pharmaceutical utility. ... | 07/08/2008 |
| 7396935 | Aryl-substituted pyrazole-amide compounds useful as kinase inhibitors The present invention relates to compounds having the formula, and pharmaceutically-acceptable salts, prodrugs, solvates, isomers, and/or hydrates thereof, wherein Q is an optionally-substituted pyridyl, ring; R2 | 07/08/2008 |
| 7390907 | Vanilloid receptor ligands and their use in treatments Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascu... | 06/24/2008 |
| 7388018 | 4-Piridinylmethylsulphonamide derivatives as fungicidal plant protein agents Sulfonamides of the formula I where the substituents are as follows: R1 is hydrogen, alkyl, alkoxy, alkenyl or alkynyl; and R2, R3, R4, R5 are... | 06/17/2008 |
| 7375232 | Ortho-heterocyclic substituted aryl amides for controlling invertebrate pests Compounds of Formula I, their N-oxides and salts are disclosed wherein A is O or S; G is a 5- or 6-membered heteroaromatic ring or a 5- or 6-membered nonaromatic heterocyclic ring optionally including one or two ring member... | 05/20/2008 |
| 7354938 | Pyrazole compounds and uses related thereto Substituted pyrazoles are provided that are useful for the treatment of, for example, diabetes, obesity and metabolic syndrome. ... | 04/08/2008 |
| 7348342 | Heterocyclic compounds process for their preparation and pharmaceutical compositions containing them and their use in medicine We describe substituted benzenesulfoximine compounds having anti-inflammatory activity, processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of inflammatory diseases. ... | 03/25/2008 |
| 7329670 | Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas The compounds are aryl and heteroaryl substituted heterocyclic ureas of the formula A—NH—C(O)—NH—B where A is the aryl or hetaryl substituted heterocyclic group and B is an aryl or heteroaryl moiety. The compounds inhibit raf kinase and are useful in the tre... | 02/12/2008 |
| 7312350 | Process for preparing arylalkynes The invention relates to a process for preparing arylvinyl halides and sulphonates and arylalkynes by reacting haloaromatics or aryl sulphonates with vinyl halides or sulphonates in the presence of a palladium catalyst and a base and, if appropriate, subsequent elim... | 12/25/2007 |
| 7309710 | Crystals Obtaining the crystal of 4,6-dimethyl-4′-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]nicotinanilide having excellent activity of inhibiting Ca2+ release-activated Ca2+ channel and suppressing IL-2 production to find that the compound includes t... | 12/18/2007 |
| 7297797 | Pyrrolines The invention relates to novel Δ1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R | 11/20/2007 |
| 7288541 | Propylcarbamate derivatives as inhibitors of serine and cysteine proteases The present invention includes ketone derivatives (I) and (II), which are useful as cathepsin K inhibitors. The described invention also includes methods of making such ketone derivatives as well as methods of using the same in the treatment of disorders, including ... | 10/30/2007 |
| 7285554 | Pyrazole derivative Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors conta... | 10/23/2007 |
