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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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