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Patent # Description
US-9,663,537 Chemokine receptor antagonists and methods of use
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises...
US-9,663,536 Inhibitors of human immunodeficiency virus replication
The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The...
US-9,663,535 Ataxia telengiectasia and Rad3-related (ATR) protein kinase inhibitors
Macrocyclic compounds having the structure of Formula (A), or pharmaceutically acceptable salts thereof, are provided, ##STR00001## wherein R.sup.1, R.sup.2,...
US-9,663,534 Fused bicyclic isoxazolines as inhibitors of cholesterol ester transfer protein
Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is (CH.sub.2) or O, are CETP inhibitors and...
US-9,663,533 Thieno[3,2-C]pyridin-4(5H)-ones as BET inhibitors
Thienopyridone compounds of formula (I): ##STR00001## or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in...
US-9,663,532 Artemisinin derivatives, methods for their preparation and their use as antimalarial agents
Derivatives of the antimalarial agent artemisinin, compositions comprising the derivatives, methods for preparing the derivatives, and their uses in...
US-9,663,531 Process for the industrial synthesis of sordidin
The present invention relates to a process for preparing sordidin, comprising a step of preparing 4-(2-ethyl-1,3-dioxolan-2-yl)pentan-2-one by means of a...
US-9,663,530 5-oxa-2-azabicyclo[2.2.2]OCTAN-4-yl and 5-oxa-2-azabicyclo[2.2.1]heptan-4-yl derivatives
The present invention relates to compounds of formula of formula I wherein X, Ar, R.sup.1, m and n are as described herein, compositions containing compounds of...
US-9,663,529 Tricyclic pyrido-carboxamide derivatives as rock inhibitors
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables...
US-9,663,528 Substituted 1,2,3,4,6,8,12,12a-octahydro-1,4-methanodipyrido[1,2-a:1',2'-d]pyrazines and methods for...
Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): ##STR00001## ...
US-9,663,527 Factor XIa inhibitors
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said...
US-9,663,526 Aminopyrimidinyl compounds
A compound having the structure: ##STR00001## or an acceptable salt thereof, wherein X is N or CR, where R is hydrogen, alkyl, etc.; A is selected from the...
US-9,663,525 Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: ##STR00001## or a pharmaceutically...
US-9,663,524 Substituted pyrido[2,3-d]pyrimidines as protein kinase inhibitors
The present invention provides compounds of formula I-h: ##STR00001## useful as inhibitors of protein kinases, pharmaceutically acceptable compositions...
US-9,663,523 BET protein-inhibiting 5-aryltriazoleazepines
The present invention relates to BET-protein-inhibitory, in particular BRD4-inhibitory 5-aryltriazoloazepines of the general formula (I) ##STR00001## in which...
US-9,663,522 3-aminocycloalkyl compounds as RORgammaT inhibitors and uses thereof
The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the...
US-9,663,521 Compounds and methods for the prevention and treatment of tumor metastasis and tumorigenesis
The disclosure provides compounds for reducing the prevalence of the perinucleolar compartment in cells, for example, of formula (I), wherein R.sup.1, R.sup.2,...
US-9,663,520 Bicyclic bromodomain inhibitors
The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical...
US-9,663,519 Compounds useful as inhibitors of ATR kinase
The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions...
US-9,663,518 Process for preparation of (2S, 5R)-1,6-diaza-bicyclo[3.2.1]octane-2-carbonitrile-7-oxo-6-(sulfooxy)-mono ...
A process for preparation of a compound of Formula (I) is disclosed. ##STR00001##
US-9,663,517 Compositions and uses thereof
Provided are solid dispersions, solid molecular complexes, salts and crystalline polymorphs involving propane-1-sulfonic acid ...
US-9,663,516 Bicyclic-pyrimidinedione compounds
The present invention provides novel bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions...
US-9,663,515 Dihydropyrrolopyridine inhibitors of ROR-gamma
Provided are novel compounds of Formula (I): ##STR00001## pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful...
US-9,663,514 Substituted 6-aza-isoindolin-1-one derivatives
Disclosed are compounds of Formula 1, ##STR00001## and pharmaceutically acceptable salts thereof, wherein G, p, R.sup.1, R.sup.2, R.sup.3a, R.sup.4, and...
US-9,663,513 Pyrimidine PDE10 inhibitors
The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders...
US-9,663,512 Bicyclic heterocycle compounds and their uses in therapy
The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the...
US-9,663,511 Sphingosine 1-phosphate receptor antagonists
The present invention relates to sphingosine-1-phosphate (S1P) receptors and compounds of the general formula: ##STR00001## that are useful in the treatment...
US-9,663,510 Substituted triazolopyridines and their use as TTK inhibitors
The present invention relates to substituted triazolopyridine compounds of general formula (I): ##STR00001## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, and...
US-9,663,507 Crystallisation of thiamine hydrochloride
A method of producing crystalline pharmaceutical grade Thiamine hydrochloride by crystallization from an isopropanol-water mixture. The method can be tuned to...
US-9,663,506 Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators,...
The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) ##STR00001## wherein ring A, R.sup.Q, -L-, R.sup.1,...
US-9,663,505 Process for the preparation of rivaroxaban
Disclosed is a process for the preparation of rivaroxaban and purifying rivaroxaban.
US-9,663,504 Salts of heterocyclic modulators of HIF activity for treatment of disease
The present disclosure relates to salts of heterocyclic compounds and methods that inhibit HIF pathway activity. The compounds are designed to treat or prevent...
US-9,663,503 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]py- razine-2-carbonitrile and...
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to ...
US-9,663,502 2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the...
The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.a,...
US-9,663,501 Process for preparing a novel crystalline form of thifensulfuron-methyl and use of the same
A the crystalline form of thifensulfuron-methyl of formula (I), the crystal preparation process, the analyzes of the crystal through various analytical methods...
US-9,663,500 Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for...
Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention...
US-9,663,499 Small molecule inhibitors of fibrosis
Described herein are compounds and compositions for the treatment of a fibrotic disease.
US-9,663,498 Aromatic heterocyclic compounds and their application in pharmaceuticals
Provided herein are novel aromatic heterocyclic compounds or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a...
US-9,663,497 Benzoimidazol-2-yl pyrimidine modulators of the histamine H.sub.4 receptor
Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders,...
US-9,663,496 AMPK-activating heterocyclic compounds and methods for using the same
Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure ...
US-9,663,495 Triazolone derivatives or salts thereof and pharmaceutical composition comprising the same
Provided is a triazolone derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising...
US-9,663,494 Inhibitors of bruton's tyrosine kinase
This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit BTK. The compounds...
US-9,663,493 Pyridazine compounds, compositions and methods
The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine...
US-9,663,492 Methods for the preparation of charged crosslinkers
Processes for the preparation of charged crosslinkers bearing a sulfonic acid moiety are disclosed. These procedures also optionally include methods to convert...
US-9,663,491 Metalloenzyme inhibitor compounds as fungicides
The instant invention describes compounds of Formula I having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof...
US-9,663,490 Process for making reverse transcriptase inhibitors
The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1- ...
US-9,663,489 Process for the preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine
This disclosure relates to the field of preparation of 3-(3-chloro-1H-pyrazol-1-yl)pyridine and intermediates therefrom. These intermediates are useful in the...
US-9,663,488 Metalloenzyme inhibitor compounds
The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by...
US-9,663,487 Phosphoinositide 3-kinase inhibitors
A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R and R.sub.6 are each independently (LQ).sub.mY;...
US-9,663,486 Selectively substituted quinoline compounds
Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8,...
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