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Patent # Description
2016/0289239 PYRROLOBENZODIAZEPINES AND TARGETED CONJUGATES
A compound, or a pharmaceutically acceptable salt or solvate thereof, or conjugates thereof, selected from the group consisting of: ##STR00001## ##STR00002## ...
2016/0289238 HETEROCYCLIC COMPOUNDS AS LSD1 INHIBITORS
The present invention is directed to compounds of Formula I which are LSD1 inhibitors useful in the treatment of diseases such as cancer. ##STR00001##
2016/0289237 MERCAPTOALKYLGLYCOLURILS AND USE OF SAME
The invention provides a mercaptoalkylglycoluril represented by the general formula (I): ##STR00001## wherein R.sup.1 and R.sup.2 each independently represent a...
2016/0289236 Protein Kinase Inhibitors
The present invention relates to a novel family of protein kinase inhibitors, more specifically the present invention is directed to inhibitors of the members...
2016/0289235 COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the...
2016/0289234 The Crystalline Forms of Temozolomide and the Method for Preparing Same
Provided in the present invention are a new method for preparing the crystalline forms of Temozolomide and three types of crystalline form of Temozolomide by...
2016/0289233 NOVEL N-ACYL-(3-SUBSTITUTED)-(8-METHYL)-5,6-DIHYDRO-[1,2,4]TRIAZOLO[4,3-a] PYRAZINES AS SELECTIVE NK-3 RECEPTOR...
Novel compounds of Formula I ##STR00001## and their use in therapeutic treatments.
2016/0289232 TRICYCLIC IMIDAZOLE COMPOUNDS AS INHIBITORS OF TRYPTOPHAN HYDROXYLASE
The present invention relates to compounds of the formula (I) ##STR00001## wherein R.sup.1a, R.sup.1b, R.sup.2, R.sup.3, and X are as described in the...
2016/0289231 POLYMORPHS AND PROCESS FOR PRETARATION OF ...
A process for preparation of compound of Formula (I) is disclosed. The application is also directed to polymorphic forms of the compound of formula (I). ...
2016/0289230 NOVEL AZAINDOLE DERIVATIVES AS SELECTIVE HISTONE DEACETYLASE (HDAC) INHIBITORS AND PHARMACEUTICAL COMPOSITIONS...
The present invention relates to novel azaindole derivatives, and more particularly, to novel azaindole derivatives having histone deacetylase (HDAC)...
2016/0289229 TOLL LIKE RECEPTOR MODULATOR COMPOUNDS
The present disclosure relates generally to toll like receptor modulator compounds, such as diamino pyrido[3,2 D]pyrimidine compounds and pharmaceutical...
2016/0289228 Tetrahydroimidazopyridine Derivatives as Modulators of TNF Activity
A series of substituted 5,6,7,8-tetrahydroimidazo[1,2-.alpha.]pyridine derivatives, being potent modulators of human TNF.alpha. activity, are accordingly of...
2016/0289227 SUBSTITUTED IMIDAZOPYRIDINE AND TRIAZOLOPYRIDINE COMPOUNDS AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR5
Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds;...
2016/0289226 [9,10-DIMETHOXY-3-(2-METHYLPROPYL)-1H,2H,3H,4H,6H,7H,11BH-PYRIDO-[2,1-A]IS- OQUINOLIN-2-YL]METHANOL AND...
Compounds having a structure of formula (I), including stereoisomers and pharmaceutically acceptable salts and solvates thereof: ##STR00001## wherein R.sub.1 is...
2016/0289225 PYRIDINYLPYRAZOLOQUINOLINE COMPOUNDS
A compound represented by formula (I), or a pharmaceutically acceptable salt thereof: ##STR00001## wherein R.sup.1 represents a group represented by the...
2016/0289224 Antifungal Treatment
A method of treating or preventing fungal infection, which includes identifying a plant or animal having a fungal infection and administering an effective...
2016/0289223 DESFERRITHIOCIN ANALOGS AND USES THEREOF
Iron overload is associated with pathological conditions such as oxidative stress, transfusional iron overload, thalassemia, primary hemochromatosis, secondary...
2016/0289222 LXR MODULATORS
The present invention provides compounds of Formula I and Formula II: or pharmaceutically acceptable salts or solvates thereof, as modulators of liver X...
2016/0289221 Difluoroethyl-oxazole sustituted bridged spiro[2.4]heptane derivatives as alx receptor agonists
The present invention relates to difluoroethyl-oxazole substituted bridged spiro[2.4] heptane derivatives of formula (I), ##STR00001## wherein the substituents...
2016/0289220 NOVEL SALTS
Salts of 1-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)-2,4-dioxo-3-[- (1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]-1,2,3,4-tetrahydropyri- ...
2016/0289219 MONOMERS AND POLYMERS FOR FUNCTIONAL POLYCARBONATES AND POLY(ESTER-CARBONATES) AND PEG-CO-POLYCARBONATE HYDROGELS
The invention generally relates to functional polymers and hydrogels. More particularly, the invention provides versatile monomers and polymers with...
2016/0289218 AZIRIDINATED TRIGLYCERIDES AND POLYMERS FORMED THEREFROM
Various embodiments disclosed relate to aziridinated triglycerides and polymers formed therefrom. In various embodiments, the present invention provides an...
2016/0289217 COUMARIN BASED HSP90 INHIBITORS WITH UREA AND ETHER SUBSTITUENTS
Compounds of the formulas: wherein: R.sub.1-R.sub.4, X.sub.1, Y.sub.1, and A are as defined herein are provided. Pharmaceutical compositions of the compounds...
2016/0289216 FUSED 1,4-DIHYDRODIOXIN DERIVATIVES AS INHIBITORS OF HEAT SHOCK TRANSCRIPTION FACTOR 1
The present invention relates to compounds of formula I as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1)....
2016/0289215 BIPYRAZOLE DERIVATIVES AS JAK INHIBITORS
The present invention provides compounds of Formula I: ##STR00001## or pharmaceutically acceptable salts thereof, as well as their compositions and methods of...
2016/0289214 FLUOROMETHYL-SUBSTITUTED PYRROLE CARBOXAMIDES AS CAV2.2 CALCIUM CHANNEL BLOCKERS
The invention relates to pyrrole carboxamides bearing a fluoromethyl-moiety as voltage gated calcium channel blockers, to pharmaceutical compositions...
2016/0289213 PROCESS FOR THE PREPARATION OF 5-FLUORO-1H-PYRAZOLES
A new process for the preparation of 5-fluoro-1H-pyrazoles of the general formula (I) as described herein comprising reacting an olefin with an hydrazine.
2016/0289212 HEPATITIS B ANTIVIRAL AGENTS
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y-Z-L-R.sub.1 (I) which inhibit...
2016/0289211 CERTAIN HETEROCYCLES, COMPOSITIONS THEREOF, AND METHODS FOR THEIR USE
Provided are compounds of Formula I: ##STR00001## or a pharmaceutically acceptable salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,...
2016/0289210 Substituted Pyridine Derivatives Useful as GSK-3 Inhibitors
The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds...
2016/0289209 SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS
The present invention provides compounds of Formula (I): ##STR00001## or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables...
2016/0289208 2-PYRIDONE COMPOUND
This 2-pyridone compound represented by formula [1] or a tautomer of said compound, or a pharmaceutically acceptable salt of said compound or said tautomer, or...
2016/0289207 COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY
The present invention is directed to substituted indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of...
2016/0289206 CARBOXYMETHYL PIPERIDINE DERIVATIVE
The present invention provides a new compound which has NK.sub.1 receptor antagonist activity, whose CYP3A4 inhibitory activity is reduced compared to...
2016/0289205 PHARMACOLOGICAL TREATMENT OF OBSESSIVE-COMPULSIVE DISORDER
The present invention relates to a compound of the following formula (I): ##STR00001## or a pharmaceutically acceptable salt thereof, for use in the prevention...
2016/0289204 GRISEOFULVIN DERIVATIVES
The present invention relates to compounds of the following general formula (I), or to a pharmaceutically acceptable salt thereof, as well as to the uses...
2016/0289203 A PROCESS FOR SYNTHESIS OF FURAN DERIVATIVE USING AN ACID CATALYST AND PREPARATION THEREOF
In accordance with the present subject matter, there is provided a process for preparing a furan derivative, the process comprising the steps of contacting a...
2016/0289202 1-[2-(2,4-DIMETHYLPHENYLSULFANYL) PHENYL]PIPERAZINE ACETATE IN CRYSTALLINE FORM
The present invention relates to 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine acetate in crystalline form and to methods for the preparation thereof. In...
2016/0289201 BIS-MMF DERIVATIVES
The present invention relates to novel compounds, e.g. for use as a medicament. In particular, the present invention relates to novel medicaments, preferably...
2016/0289200 PROCESSES AND INTERMEDIATES FOR MAKING SWEET TASTE ENHANCERS
The present invention includes methods/processes and intermediates for preparing compounds having structural Formula (I): ##STR00001## wherein X is alkyl,...
2016/0289199 TRPV1 Vanilloid Receptor Antagonists With A Bicyclic Portion
The invention discloses compounds of formula I ##STR00001## wherein Y is a group of formula A, B, C, D, or E: ##STR00002## and W, Q, n, R1, R2, R3, U1-U5, J and K...
2016/0289198 BENDAMUSTINE DERIVATIVES AND METHODS OF USING SAME
The present invention is directed to bendamustine esters and bendamustine amides and their use for the treatment of cancer.
2016/0289197 PRODUCTION METHOD FOR PRODUCING N-BENZYL-2-(2-NITRO-1H-IMIDAZOL-1-YL) ACETAMIDE
The invention relates to the synthesis of a therapeutic agent which is effective against American trypanosomiasis (Chagas disease) caused by the protozoa...
2016/0289196 PYRAZOLE DERIVATIVES AS TNIK, IKKe AND TBK1 INHIBITOR AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
Provided is pyrazole derivatives as a TNIK (Traf2- and NCK-interacting kinase), IKK.epsilon. (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1)...
2016/0289195 FLUOROPHENYL PYRAZOL COMPOUNDS
The present invention provides a compound of the Formula: wherein X is selected from the group consisting of, R is selected from the group consisting of H and...
2016/0289194 PROCESS FOR THE PREPARATION OF 5-FLUORO-1H-PYRAZOLES
A new process for the preparation of 5-fluoro-1H-pyrazoles of the general formula (I) as described herein, resulting from the reaction of an olefin with...
2016/0289193 PROCESS FOR PREPARING 3,5-BIS(HALOALKYL)PYRAZOLE DERIVATIVES FROM a,a-DIHALOAMINES
The present invention relates to a novel process for preparing 3,5-bis(haloalkyl)pyrazole derivatives.
2016/0289192 IVABRADINE HYDROCHLORIDE FORM IV
Ivabradine hydrochloride Form IV, its pharmaceutical composition, process for its preparation, and its use as therapeutically active ingredient and ...
2016/0289191 ORGANIC COMPOUNDS
The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate...
2016/0289190 PROCESSES OF MAKING AND CRYSTALLINE FORMS OF A MDM2 INHIBITOR
The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsu- ...
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