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Patent # Description
2017/0313706 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...
2017/0313705 PURINONE DERIVATIVE
Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition...
2017/0313704 PROCESS FOR MAKING TRICYCLIC LACTAM COMPOUNDS
Processes are described for the preparation of tricyclic lactam compound of Formula (I), having the structure and intermediates useful for the preparation of...
2017/0313703 Cis-tetrahydro-spiro(cyclohexane-1,1?-pyrido[3,4-b]indole)-4-amine Compounds
Cis-tetrahydro-spiro(cyclohexane-1,1'-pyrido[3,4-b]indole)-4-amine compounds which act on the nociceptin/ORL-1 receptor system as well as on the .mu.-opioid...
2017/0313702 HISTONE DEMETHYLASE INHIBITORS
The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine...
2017/0313701 Fused Heterocyclic Compounds as Selective BMP Inhibitors
The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation,...
2017/0313700 SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINES AND IMIDAZO[1,2-A]PYRAZINES AND THEIR USE
The present application relates to novel substituted pyrazolo[1,5-a]pyridines and imidazo[1,2-a]pyrazines, to processes for preparation thereof, to the use...
2017/0313699 PROCESS FOR THE PREPARATION OF APIXABAN AND INTERMEDIATES THEREOF
The present invention relates to an improved process for the preparation of Apixaban and intermediates thereof. Further the present invention also relates to...
2017/0313698 POLYHETEROARL HISTONE DEACETYLASE INHIBITORS AND THEIR USE IN THERAPY
The present invention is a compound having the following formula: or a pharmaceutically acceptable salt thereof, wherein e.g. L and Y are each independently an...
2017/0313697 PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AND USE THEREOF
Disclosed in the disclosure are a pyrazolo[1,5-a]pyrideine compound with structural features as shown in formula (I) or a pharmaceutically acceptable salt,...
2017/0313696 ISOXAZOLE DERIVATIVE AS MUTANT ISOCITRATE DEHYDROGENASE 1 INHIBITOR
It has been found that a compound of the general formula (I) having an isoxazole skeleton has excellent inhibitory activity against mutant IDH1 protein and...
2017/0313695 PROCESS FOR THE PREPARATION OF APIXABAN
The present invention relates to an improved process for the preparation of Apixaban and its intermediates.
2017/0313694 Crystalline Form of (R)-7-Chloro-N-(Quinuclidin-3-YL)benzo[B]thiophene-2-Carboxamide Hydrochloride Monohydrate
Crystalline Forms I and II of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide hydrochloride monohydrate and compositions, methods of...
2017/0313693 PIPERIDINE OXADIAZOLE AND THIADIAZOLE OREXIN RECEPTOR ANTAGONISTS
The present invention is directed to piperidine oxadiazole and thiadiazole orexin compounds which are antagonists of orexin receptors. The present invention is...
2017/0313692 AGONISTS OF THE MU OPIOID RECEPTOR
The present technology is directed to compounds, compositions, and methods related to non-morphinan-like mu opioid receptor agonists. Compounds of the present...
2017/0313691 6-AMINOPYRIDIN-3-YL THIAZOLES AS MODULATORS OF RORyT
The present invention comprises compounds of Formula I. ##STR00001## wherein: A.sup.1, A.sup.2, A.sup.3, A.sup.4, A.sup.5, R.sup.1, and R.sup.2 are defined in...
2017/0313690 NOVEL MODULATORS OF CALCIUM RELEASE-ACTIVATED CALCIUM CHANNEL
Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and...
2017/0313689 PROCESS FOR PREPARING A POLYMORPH OF RIVAROXABAN
This invention describes a process for the preparation of rivaroxaban modification I comprising: (i) dissolving rivaroxaban in a mixture of a solvent (e.g....
2017/0313688 HISTONE DEACETYLASE INHIBITORS AND USES THEREOF
Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the...
2017/0313687 Compounds and Compositions for Cognition-Enhancement, Methods of Making, and Methods of Treating
Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing...
2017/0313686 COMPOUNDS AND THEIR USE AS BACE INHIBITORS
The present application relates to compounds of formula (I), (Ia), or (Ib) and their pharmaceutical compositions/preparations. This application further relates...
2017/0313685 BROAD-SPECTRUM NON-COVALENT CORONAVIRUS PROTEASE INHIBITORS
This invention pertains to materials and methods for the treatment of patients with coronavirus infection and the control of zoonotic disease outbreaks using...
2017/0313684 PYRAZOLE OREXIN RECEPTOR ANTAGONISTS
The present invention is directed to pyrazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the...
2017/0313683 BTK INHIBITOR
Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug...
2017/0313682 ISOQUINOLIN-3-YL CARBOXAMIDES AND PREPARATION AND USE THEREOF
Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an...
2017/0313680 RHO KINASE INHIBITOR BA-1049 (R) AND ACTIVE METABOLITES THEREOF
The disclosure provides rho kinase inhibitor BA-1049(R), an hydroxy metabolite of BA-1049(R), and adipate salts and deuterated forms thereof, useful for...
2017/0313679 Novel Carboxylic Acid Compounds Useful for Inhibiting Microsomal Prostaglandin E2 Synthase-1
The present invention provides compounds of Formula 1, or a pharmaceutically acceptable salts, thereof, where R, X, A, E, and G are as described herein,...
2017/0313678 CRYSTALLINE FORM OF A SUBSTITUTED QUINOLINE COMPOUND AND PHARMACEUTICAL COMPOSITIONS THEREOF
The present invention relates to a crystalline form of N-(3-fluoro-4-((7-(2-hydroxy-2-methylpropoxy)quinolin-4-yl)oxy)phenyl)-1,- ...
2017/0313677 Isoindoline Derivatives
The present invention relates to isoindoline derivatives according to formula (I), which are Positive Allosteric Modulators of D1 and accordingly of benefit as...
2017/0313676 ISOINDOLINE DERIVATIVE, INTERMEDIATE, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
Provided are an isoindoline derivative, intermediate, preparation method, pharmaceutical composition and use thereof. The isoindoline derivative and the...
2017/0313675 HETEROARYLAMIDE INHIBITORS OF TBK1
Disclosed are compounds of formula 1: ##STR00001## which are useful as inhibitors of TBK1. Also disclosed are pharmaceutical compositions which contain the...
2017/0313674 BENZYLHYDROXIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
The invention relates to benzylhydroxyde derivatives of formula (I): The invention also relates to the preparation and the therapeutic use of the compounds of...
2017/0313673 CHROMENE-2 DERIVATIVES AND USE THEREOF IN THE TREATMENT OF FIBROSIS
Disclosed are chromene-2 derivatives and the use thereof in the treatment of fibrosis. Specifically, disclosed are the derivatives of a compound having a main...
2017/0313672 BIS(SULFONAMIDE) DERIVATIVES AND THEIR USE AS MPGES INHIBITORS
The present invention relates to bis(sulfonamide) compounds and pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutical...
2017/0313671 NEW SALT OF ABEXINOSTAT, ASSOCIATED CRYSTALLINE FORM, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL...
Abexinostat tosylate of formula (II): ##STR00001## and its crystalline form I characterised by its X-ray powder diffraction diagram, its Raman spectrum and its...
2017/0313670 PREPARATION OF DIALKYL ESTERS OF 2,5-FURANDICARBOXYLIC ACID
Dialkyl esters of 2,5-furandicarboxylic acid are prepared from a 2,5-furandicarboxylic acid-containing starting material in a process, which includes:...
2017/0313669 LACTONE COMPOUNDS AND METHODS OF MAKING AND USING SAME
Provided herein are lactone compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as...
2017/0313668 METHODS AND COMPOSITIONS RELATED TO RETINOID RECEPTOR-SELECTIVE PATHWAY
Provided herein are methods and compositions related to a retinoid receptor-selective pathway. As described herein, this pathway can be targeted to manipulate...
2017/0313667 Method of preparing ATG's analogue, and the application of ATG and it's analogue
The present invention provides the use of ATG in the preparation of a reagent for adjusting the activity of PP2A; and the use of ATG in increasing the activity...
2017/0313666 CRYSTALLINE FORMS OF TYROSINE KINASE INHIBITORS AND THEIR SALTS
The disclosure relates to various polymorphic forms and amorphous form of sodium 4-((3-(4-cyclohexylpiperazin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol- ...
2017/0313665 HYDROXYALKYL-SUBSTITUTED PHENYLTRIAZOLE DERIVATIVES AND USES THEREOF
The present invention relates to novel 5-(hydroxyalkyl)-1-phenyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to...
2017/0313664 NOVEL FORM OF PYRIMIDINE COMPOUND HAVING DIBENZYLAMINE STRUCTURE
It is an object of the present invention to provide a novel form of (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methy- ...
2017/0313663 Bendamustine Derivatives and Related Compounds, and Medical Use Thereof in Cancer Therapy
The present invention relates to bendamustine derivatives and related compounds of formula (VII), (VIII) and (IX), and medical uses thereof in particular in...
2017/0313662 AN IMPROVED PROCESS FOR THE PREPARATION OF ENZALUTAMIDE
The present invention relates to an improved process for the preparation of enzalutamide by conventional synthesis, which avoids utilization of microwave...
2017/0313661 KINASE MODULATORS FOR THE TREATMENT OF CANCER
A method of treating cancer in which a compound that inhibits the expression, production or release of IL-10 by immune cells is combined with a compound that...
2017/0313660 Novel Fungicidal Pyridylamidines
The invention relates to compounds of formula (I) wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are as...
2017/0313659 COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective...
2017/0313658 2-Amino-3,5-Difluoro-3,6-Dimethyl-6-Phenyl-3,4,5,6-Tetrahydropyridines as BACE1 Inhibitors for Treating...
The present invention is directed to compounds according to Formula (I) which compounds are inhibitors of the BACE1 enzyme. Separate aspects of the invention...
2017/0313657 METHOD FOR THE PREPARATION OF 1-(2-HALOGEN-ETHYL)-4 PIPERIDINE-CARBOXYLIC ACID ETHYL ESTERS
The present invention refers to a process for the preparation of 1-(2-halogen-ethyl)-4-piperidinecarboxylic acid ethyl esters, in particular of...
2017/0313656 Branched Discrete PEG Constructs
Disclosed are general and "substantially pure" branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups,...
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