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Patent # Description
US-9,493,482 Compounds and methods for preventing or treating sensory hair cell death
Disclosed herein are compounds, and pharmaceutical compositions that include such compounds, for preventing or treating hearing loss. The compounds and...
US-9,493,481 Substituted 5-aminothieno[2,3--C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the...
In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6 -carboxamide analogs, derivatives thereof, and related compounds, which are...
US-9,493,480 Monomeric trioxane amide sulfur compounds
Anilide derivatives of the natural trioxane artemisinin were prepared and evaluated for antimalarial efficacy in Plasmodium berghei-infected mice. Selected...
US-9,493,479 Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors
The present invention relates to 4-Pyridone Compounds of Formula (I); and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R.sup.1, R.sup.2,...
US-9,493,478 Fused ring compound containing furan or salt thereof and pharmaceutical composition comprising same
The present invention provides a fused ring compound containing furan or a pharmaceutically acceptable salt thereof, a method for preparing same, a...
US-9,493,477 Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof
A method of providing a patient with controlled release of ketone-containing opioid using a prodrug capable, upon enzymatic activation and intramolecular...
US-9,493,476 Macrocyclic compounds as trk kinase inhibitors
Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R.sup.2, R.sup.2a, R.sup.3, R.sup.3a, and Z are as...
US-9,493,475 Textile treatment compounds and compositions
A cationic polymer is disclosed, represented by: A) wherein "P.sup.1" and "P.sup.2" represent portions of the cationic polymer to which the first functional...
US-9,493,474 Inhibitors of the renal outer medullary potassium channel
This invention relates to compounds of Formula I having the following general structure: ...
US-9,493,473 Processes for making ponatinib and intermediates thereof
Novel synthetic approaches to make 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin- -1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide,...
US-9,493,472 Substituted benzoxazoles
The invention relates to substituted benzoxazoles and to processes for their preparation and to their use for preparing medicaments for the treatment and/or...
US-9,493,471 Pyrimidine derivatives as protein kinase inhibitors
The present invention relates to pyrimidine derivatives capable of inhibiting one or more protein kinases. Further aspects relate to pharmaceutical compositions...
US-9,493,470 Crystalline forms of 3-(imidazo[1,2-B] pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl) ...
Novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin- -1-yl)methyl]-3-(trifluoromethyl)phenyljbenzamide free base...
US-9,493,469 Piperidine inhibitors of Janus kinase 3
The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof. ...
US-9,493,468 Antifungal 5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzo-diazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines...
The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines...
US-9,493,467 PI3 kinase antagonists
The present invention provides novel PI3-Kinase antagonists having the formula: ##STR00001## and methods of use thereof.
US-9,493,466 Treatment of cancer with TOR kinase inhibitors
Provided herein are methods for treating or preventing a solid tumor, non-Hodgkin lymphoma or multiple myeloma in a patient, comprising administering an...
US-9,493,465 3-hydroxypyrrolidine inhibitors of 5'-methylthioadenosine phosphorylase and nucleosidase
The present invention relates to 3-hydroxypyrrolidine compounds of the general formula (I) which are inhibitors of 5'-methylthioadenosine phosphorylase or...
US-9,493,464 Wee1 degradation inhibitors
The invention provides compounds that inhibit the degradation of Wee1. The compounds of the present invention are generally ...
US-9,493,463 Substituted xanthine derivatives
This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention...
US-9,493,462 Polymorphs
The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.
US-9,493,461 Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds,...
US-9,493,460 Diimide compounds
The invention relates to novel compounds which are naphthalene diimides of general formula (I): ##STR00001## The compounds are used in therapy, particularly...
US-9,493,459 Azetidine and piperidine compounds useful as PDE10 inhibitors
Azetidine and piperidine compounds of formula (I): ##STR00001## as defined in the specification, compositions containing them, and processes for preparing...
US-9,493,457 4,5,6,7-tetrahyroimidazo[4,5-c]pyridine compounds
The present invention relates to compounds of formula (I), ##STR00001## and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers,...
US-9,493,456 Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators
Disclosed herein is a compound of Formula I: ##STR00001## wherein X, R.sup.1, R.sup.2, and R.sup.3 are as defined herein, or a pharmaceutically acceptable...
US-9,493,455 Azaindole derivatives as inhibitors of protein kinases
The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers,...
US-9,493,454 Multiple kinase pathway inhibitors
Kinase with inhibitory activity against kinases disposed in multiple signaling pathways and their therapeutic uses.
US-9,493,453 Piperazinyl pyrimidine derivatives, preparation method and use thereof
Provided are piperazinyl pyrimidine derivatives of formula I having CCR.sub.4 antagonism, and the preparation method, pharmaceutical composition and use thereof...
US-9,493,452 Compounds and derivatives of 2H-pyrido (3,2-b)(1, 4) oxazin 3)4H)-ones as raf kinase and LRRK2 inhibitors
The present invention provides pharmaceutical compound of formula: ##STR00001## wherein A and B are individually an C or N and R1 is an alkyl and R2 is a...
US-9,493,451 Amine derivatives as potassium channel blockers
The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found...
US-9,493,450 Cyclopropylamines as LSD1 inhibitors
The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
US-9,493,449 Carboxamide derivatives and use thereof
The present disclosure provides substituted pyridyl-, pyrimidinyl-, pyrazinyl-, pyridazinyl-, and triazinyl-based carboxamides of Formula I-A: R.sup.10 Z-HET-E...
US-9,493,448 Cycloalkane derivatives
Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated...
US-9,493,447 Optically active PDE10 inhibitor
The present invention is directed to a pure enantiomer of 1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,- ...
US-9,493,446 Orexin receptor antagonists which are [ortho bi-(hetero-)aryl]-[2-(meta ...
The present invention relates to [ortho bi-(hetero-)aryl]-[2-(meta bi-(hetero-)aryl)-pyrrolidin-1-yl]-methanone derivatives of formula (I) ##STR00001## wherein...
US-9,493,445 Insecticidal compounds
The invention relates to compounds of formula (I): ##STR00001## where A.sup.1, A.sup.2, A.sup.3, A.sup.4, G, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as...
US-9,493,444 Azaheterocyclic compounds
The invention provides novel substituted azaheterocyclic compounds according to Formula (I), ##STR00001## their manufacture and use for the treatment of...
US-9,493,443 Process for the preparation of vilazodone hydrochloride and its amorphous form
The present invention relates to an improved process for the preparation of vilazodone hydrochloride and a process for preparation of novel pure amorphous form...
US-9,493,442 Cyclopropylamines as LSD1 inhibitors
The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
US-9,493,441 Acyclic cyanoethylpyrazoles as janus kinase inhibitors
The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as...
US-9,493,440 Compounds inhibiting leucine-rich repeat kinase enzyme activity
The present invention is directed to indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in...
US-9,493,439 Proteasome inhibitors
Compounds of formula (I) ##STR00001## are useful for inhibiting a proteasome in a cell. Compounds, pharmaceutical compositions and methods of use are provided...
US-9,493,438 4,4-difluoro-piperidine-compounds
The invention, in a first aspect relates to compounds of formula (I) ##STR00001## or a pharmaceutically acceptable salt thereof, wherein R is a 6-membered...
US-9,493,437 .beta.- and .gamma.-diketones and .gamma.-hydroxyketones as Wnt/ .beta.-catenin signaling pathway activators
The present application discloses a compound which is ##STR00001## which activates Wnt/.beta.-catenin signaling and thus treats or prevents diseases related to...
US-9,493,436 Tyrosine phosphatase inhibitors and uses thereof to modulate the activity of enzymes involved in the pathology...
A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and...
US-9,493,435 IRE-1.alpha. inhibitors
The invention provides compounds which directly inhibit IRE-1.alpha. activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds...
US-9,493,434 Substituted indenes as medicaments
The present invention relates to new indene derivatives of formula (I) ##STR00001## having a great affinity for sigma receptors, especially sigma-1 receptors,...
US-9,493,433 Method for preserving aqueous solution containing leuco chromogen
Described is a method for preserving an aqueous solution comprising a leuco chromogen, comprising adding at least one compound selected from the group...
US-9,493,432 Cyclopentylbenzamide derivatives and their use for the treatment of psychotic and cognitive disorders
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, L, X, R.sup.a, R.sup.b, R.sup.1, R.sup.2 and...
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