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Patent # Description
2016/0264583 COMPOUNDS
The present invention relates to compounds of formula (I) ##STR00001## and to compositions comprising the same and to the use of the compounds and their...
2016/0264582 (Indazol-4-YL) Hexahydropyrrolopyrrolones and Methods of Use
Compounds of formula (I) ##STR00001## and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein G.sup.Ar, L.sup.1, Z.sup.1...
2016/0264581 AZA-PYRIDONE COMPOUNDS AND USES THEREOF
Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same....
2016/0264580 BICYCLIC AZAHETEROCYCLOBENZYLAMINES AS PI3K INHIBITORS
The present invention provides bicyclic azaheterocyclobenzylamines of Formula I: ##STR00001## wherein the variables are defined herein, that modulate the...
2016/0264579 PYRROLO PYRIMIDINE DERIVATIVE
A compound represented by the general formula (1) has a pyridone ring structure introduced into a pyrrolo pyrimidine skeleton, so that the compound has a...
2016/0264578 PYRAZOLOPYRIMIDONE OR PYRROLOTRIAZONE DERIVATIVES, METHOD OF PREPARING SAME, AND PHARMACEUTICAL APPLICATIONS...
Pyrazolopyrimidone and pyrrolotriazone derivatives, methods of preparation thereof, and pharmaceutical uses thereof are described. Specifically,...
2016/0264577 HSP90 INHIBITORS
The disclosure relates to Compounds of Formulae (IA) and (IB), and pharmaceutically acceptable salts thereof wherein Z.sub.1, Z.sub.2, Z.sub.3, Xa, Xb, Xc, Xd,...
2016/0264576 PURINONE DERIVATIVE HYDROCHLORIDE
The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-di- hydro-8H-purin-8-one hydrochloride has Btk-selective...
2016/0264575 TETRACYCLIC AUTOTAXIN INHIBITORS
Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such...
2016/0264574 7-BENZYL-4-(METHYLBENZYL)-2,4,6,7,8,9-HEXAHYDROIMIDAZO[1,2-A]PYRIDO[3,4-E]- PYRIMIDIN-5 (1H)-ONE, SALTS THEREOF...
This disclosure relates, at least in part, to a method of treatment. In one embodiment, the method of treatment comprises administering to a subject in need of...
2016/0264573 PROCESS FOR PRODUCING DIAZABICYCLOOCTANE DERIVATIVE AND INTERMEDIATE THEREOF
A process for producing a diazabicyclooctane derivative represented by Formula (IV) and intermediates thereof by carrying out the following steps: ...
2016/0264572 SUBSTITUTED PYRAZOLO[1,5-A] PYRIDINE AS TROPOMYOSIN RECEPTOR KINASE (TRK) INHIBITORS
The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein...
2016/0264571 IMIDAZO[1,5-a]PYRIDINIUM ION FLUOROPHORES, AND METHODS OF MAKING AND USING THE SAME
A fluorophore and methods of detecting cations and hydrophobic environments using the fluorophore are disclosed. The fluorophore includes an...
2016/0264570 METHOD OF BLOCKING TRANSMISSION OF MALARIAL PARASITE
The invention provides a method of blocking transmission of a Plasmodium parasite and a method of treating or preventing malaria comprising administering to an...
2016/0264569 SALT OF NAPHTHYRIDINE CARBOXYLIC ACID DERIVATIVE
7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-- oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates...
2016/0264568 SUBSTITUTED TRIAZOLOPYRIDINES HAVING ACTIVITY AS MPS-1 INHIBITORS
The present invention relates to substituted triazolopyridine compounds of general formula (I), in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as...
2016/0264567 SUBSTITUTED SULFONAMIDE COMPOUNDS
The invention is concerned with the compounds of formula I: ##STR00001## and salts thereof and other compounds of formulas II-IX as disclosed herein. In...
2016/0264566 ANTI-ALPHAVBETA1 INTEGRIN INHIBITORS AND METHODS OF USE
Provided herein, inter alia, are methods and compositions for inhibiting .alpha.v.beta.1 integrin and for treating fibrosis.
2016/0264565 CRYSTALLINE DASATINIB PROCESS
The present invention relates to a process for preparation of crystalline Form-SDI of Dasatinib (I). ##STR00001## Said crystalline Form-SDI of Dasatinib is...
2016/0264564 Pyrazol-3-ones That Activate Pro-apoptotic BAX
This application features pyrazol-3-one compounds that activate pro-apoptotic BAX. Also featured are methods of using such compounds, e.g., for the treatment...
2016/0264563 PROCESSES FOR PREPARING DIHYDROPYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF
The present invention refers to processes for preparing a dihydropyrimidine compound having Formula (I), or a tautomer thereof having Formula (Ia), as well as...
2016/0264562 PROCESSES FOR PREPARING DIHYDROPYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF
The present invention refers to processes for preparing a dihydropyrimidine compound having Formula (I), or a tautomer thereof having Formula (la), as well as...
2016/0264561 DETERGENT COMPOSITIONS
A compound of formula (I) wherein R.sup.1 is a C.sub.5 to C.sub.39 alkyl or alkenyl group and R.sup.2 is (c) wherein A is an anion. ##STR00001##
2016/0264560 SMALL MOLECULE C-MYC INHIBITORS
This invention provides small molecule Myc-inhibitors. Also provided in the invention are therapeutic applications of these compounds for treating Myc-driven...
2016/0264559 SALT AND CRYSTAL FORMS OF PLK-4 INHIBITOR
A fumarate salt and a maleate salt of compound (I) represented by the following structural formula, as well as their corresponding pharmaceutical compositions,...
2016/0264558 FLUOROGENIC PROTECTING GROUP
A fluorogenic compound comprising a biologically active component and a hypoxia-activated protecting group which is fluorogenic. The biologically active...
2016/0264557 NEW CYCLOHEXYLAMINE DERIVATIVES HAVING 2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES
The present invention relates to novel compounds having .beta.2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions...
2016/0264556 ITRACONAZOLE ANALOGS AND USE THEREOF
Provided herein are Itraconazole analogs. Also provided herein are methods of inhibition of Hedgehog pathway, vascular endothelial growth factor receptor 2...
2016/0264555 NOVEL QUINAZOLINE DERIVATIVE
The present invention provides a quinazoline derivative represented by the following formula (I): ##STR00001## wherein R.sup.1 and R.sup.2 represent a hydrogen...
2016/0264554 POLYCYCLIC INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers,...
2016/0264553 GDF-8 Inhibitors
Disclosed are 2,2'-bipyridyl compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure ...
2016/0264552 HETEROMAROMATIC COMPOUNDS USEFUL FOR THE TREATMENT OF PROLFERATIVE DISEASES
The present invention provides novel compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, tautomers,...
2016/0264551 HETEROAROMATIC COMPOUNDS USEFUL FOR THE TREATMENT OF PROLFERATIVE DISEASES
The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers,...
2016/0264550 PROCESS FOR ACYLATING AMINES
The present invention is concerned with the formation of amide bonds. More specifically, the present invention, relates to processes for the manufacture of...
2016/0264549 SUBSTITUTED 6, 7-DIALKOXY-3-ISOQUINOLINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE 10 (PDE 10A)
The invention relates to compounds of the formula ##STR00001## or a pharmaceutically acceptable salt thereof, wherein R', R.sup.1 through R.sup.7 and Ar are as...
2016/0264548 HETEROARYL COMPOUNDS AS BTK INHIBITORS AND USES THEREOF
The present invention relates to pyridine, pyrimidine, pyrazine, and pyridazine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK...
2016/0264547 Herbicidal Compounds
The invention relates to pyrrolone compounds of the formula (I), wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.a, R.sup.b, R.sup.c and R.sup.d are as defined in...
2016/0264546 NEW PROCESS FOR PREPARING PI3K INHIBITOR BUPARSILIB
The present disclosure provides a new process for preparing PI3K inhibitor buparsilib. The whole reaction route of the present invention is simple and easy to...
2016/0264545 Dithiol Compounds, Derivatives, and Uses Therefor
Dithiol compounds and derivatives thereof are disclosed. The agents are useful for treating ocular disease, especially presbyopia and cataract.
2016/0264544 Tetrahydrothiophene-based GABA Aminotransferase Inactivators
Tetrahydrothiophene and related heterocyclic analogs and related methods for GABA aminotransferase inactivation.
2016/0264543 PROCESS FOR THE OXIDATION OF ORGANIC CARBONYL COMPOUNDS
A process for the oxidation of an organic carbonyl compound comprising reacting the compound, optionally in the presence of a solvent, with hydrogen peroxide...
2016/0264542 DETERGENT COMPOSITIONS
A surfactant component comprising a compound of formula (I): (I) wherein R.sup.1 is a C.sub.5 to C.sub.39 alkyl or alkenyl group and R.sup.2 is a group of...
2016/0264541 VITAMIN C PRODRUGS AND USES THEREOF
Described herein are vitamin C prodrugs of Formula (I), (II), or (III), and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical...
2016/0264540 COMPOUNDS FOR TREATING PROSTATE CANCER
A compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: ...
2016/0264539 COMPOUNDS WITH (1E, 6E)-1,7-BIS-(3,4-DIMETHOXYPHENYL)-4-4-DISUBSTITUTED-HEPTA-1,6-DIENE-3,5-D- IONE...
The present invention relates to compounds having at least one (substituted phenyl)-propenal moiety. The compounds are useful in treating a subject suffering...
2016/0264538 C6-SPIRO IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally...
2016/0264537 CYCLIC PROTEIN TYROSINE KINASE INHIBITORS
Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of...
2016/0264536 HETEROCYCLIC COMPOUND
The problem of the present invention is to provide a compound having a PDE2A inhibitory action, and useful as a prophylactic or therapeutic drug for...
2016/0264535 BENZOFURAZAN ANTI-AMYLOID COMPOUNDS AND METHODS
In general, among other things, compounds of Formula I are provided: ##STR00001## in which R.sub.11 is selected from the group consisting of benzylamino, ...
2016/0264534 SYNTHESIS OF 3,4-BIS(4-NITRO-1,2,5-OXADIAZOL-3-YL)-1,2,5-OXADIAZOLE-N-OXIDE (DNTF) USING...
A novel method for preparing 3-chlorocarbohydroxymoyl-4-nitro-1,2,5-oxadiazole by reacting 4-amino-3-chlorocarbohydroxymoyl-1,2,5-oxadiazole with...
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