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Patent # Description
US-1,007,2026 Crystalline form of 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-- ...
The invention provides a crystalline form of the compound of formula: ##STR00001## that is an inhibitor of JAK kinases. The invention also provides...
US-1,007,2025 Ethyl N-boc piperidinyl pyrazolo pyridones 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-1,007,2024 Benzoxazinone derivatives for treatment of skin diseases
The present invention relates to methods and compositions for inhibiting the activity of skin proteases, especially human kallikrein 7 (KLK7), human kallikrein...
US-1,007,2023 Diarylethene compounds and uses thereof
A compound according to Formula IA and IB, reversibly convertible under photochromic and electrochromic conditions between a ring-open isomer A and a...
US-1,007,2022 Oridonin analogs, compositions, and methods related thereto
Certain embodiments are directed to oridonin analogs or derivatives. In certain aspects, the derivatives are used as anticancer or anti-inflammatory agents.
US-1,007,2021 Compound for inhibiting binding between DX2 protein and P14/ARF protein, and pharmaceutical composition for...
Disclosed is a new compound that inhibits binding between a DX2 protein and a p14/ARF protein, a pharmaceutical composition including the new compound as an...
US-1,007,2020 Isatin spiro compounds with antibacterial activities and a method of preparing the same
An isatin spiro compound having the following formula (I): ##STR00001## R.sub.1 is halogen or C.sub.1-3 alkyl; R.sub.2 is C.sub.1-3 alkyl or benzyl; and...
US-1,007,2019 Substituted pyrrolo, -furano, and cyclopentylpyrimidines having antimitotic and/or antitumor activity and...
The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of Formula III, ##STR00001## and Formula IV, ...
US-1,007,2018 Compounds for treatment of pain
The aspects of the disclosed embodiments are directed to novel compounds, specifically, quaternary ammonium derivatives of tertiary amine containing opioid drug...
US-1,007,2017 Compounds and methods for the treatment of cystic fibrosis
The invention relates to a compound of Formula I or IA compositions comprising compounds of Formula I or IA, and methods of treating cystic fibrosis comprising...
US-1,007,2016 Substituted 4-phenylpiperidines, their preparation and use
The present invention provides a compound having the structure: ##STR00001## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are each independently...
US-1,007,2015 HIV inhibiting bicyclic pyrimidine derivatives
HIV replication inhibitors of formula ##STR00001## wherein a.sup.1=a.sup.2-a.sup.3=a.sup.4- is --CH.dbd.CH--CH.dbd.CH--, --N.dbd.CH--CH.dbd.CH--,...
US-1,007,2014 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of MGLUR2...
The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic...
US-1,007,2013 Selective PI3K delta inhibitors
The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and...
US-1,007,2012 Process for crystalline pemetrexed dipotassium salt
The present invention provides process for preparing crystalline Pemetrexed dipotassium (I) Form-SP9 ##STR00001## characterized by X-ray powder diffraction...
US-1,007,2011 Substituted bridged urea analogs as sirtuin modulators
The present invention relates to novel substituted bridged urea analog compounds of Formula (I) or pharmaceutically acceptable salts thereof, corresponding...
US-1,007,2010 Substituted pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalines for inhibiting serotonin reuptake transporter activity
The invention relates to substituted pyrido[3',4':4,5]pyrrolo[1,2,3-de]-quinoxaline compounds, represented by Formula 1, defined herein, free base or...
US-1,007,2009 N-substituted beta-carbolinium compounds as potent P-glycoprotein inducers
The present invention relates to the N-substituted beta-carbolinium compounds of general formula A and formulae I and II wherein, R.sub.1 and R.sub.2 groups are...
US-1,007,2008 Spiro-isoquinoline-3,4'-piperidine compounds having activity against pain
The present invention relates to compounds having pharmacological activity towards the sigma (.sigma.) receptor, and more particularly to ...
US-1,007,2007 Tetracycline compounds
The present invention is directed to a compound represented by Structural Formula (I): ##STR00001## or a pharmaceutically acceptable salt thereof. The...
US-1,007,2006 Heterocyclic compounds and their use in preventing or treating bacterial infections
The present invention relates to heterocyclic compounds, their process of preparation, pharmaceutical compositions comprising these compounds and use thereof,...
US-1,007,2005 4-azaindole derivatives
4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying...
US-1,007,2004 Process for preparing N-(5-(3-(7-(3-fluorophenyl)-3H-imidazo ...
Provided herein is a synthetic process for preparing a compound of Formula (1). ##STR00001## The disclosure also provides useful intermediates and salts,...
US-1,007,2003 Tetrahydronaphthyridine derivatives as mGluR2-negative allosteric modulators, compositions, and their use
The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein...
US-1,007,2002 Pyridinylaminopyrimidine derivatives, preparation process and use thereof
The present invention relates to pyridinylaminopyrimidine derivatives represented by the following formula (I), and pharmaceutically acceptable salts,...
US-1,007,2001 Tank-binding kinase inhibitor compounds
Compounds having the following formula (I) and methods of their use and preparation are disclosed: ##STR00001##
US-1,007,2000 Method of treating insomnia with halogenated pyrazolo[1,5-a]pyrimidines
The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R.sub.1, X and Y have different meanings, and pharmaceutically...
US-1,007,1999 Crystalline forms of (3-amino-oxetan-3-ylmethyl)-[2-(5,5-dioxo-5,6,7,9-tetrahydro-5lambda*6*-t- ...
The present invention relates to novel crystalline forms of compound (I), ##STR00001## ...
US-1,007,1998 Iminothiadiazine dioxides bearing an amine-linked substituent as BACE inhibitors, compositions, and their use
In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): or a tautomers thereof, and...
US-1,007,1997 Pesticidally active amide heterocyclic derivatives with sulphur containing substituents
Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and...
US-1,007,1996 Optical isomer of 1,4-benzothiazepine-1-oxide derivative, and pharmaceutical composition prepared using same
The present invention provides: a novel compound which is characterized by being capable of increasing the number of heart beats or a blood pressure mildly to...
US-1,007,1995 Substituted oxopyridine derivatives
The invention relates to substituted oxopyridine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments...
US-1,007,1994 N-sulfonyl homoserine lactone derivatives, preparation method and use thereof
The invention relates to a homoserine lactone derivative of Formula I, preparation method and use thereof. The compound has an effect of regulatory of bacterial...
US-1,007,1993 Carbazole derivative, light-emitting element material and organic semiconductor material
An object is to provide a novel carbazole derivative that has an excellent carrier-transport property and can be suitably used for a transport layer or as a...
US-1,007,1992 Diacylglycerol acyl transferase 2 inhibitors
Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in...
US-1,007,1991 Substituted pyridine derivatives useful as c-fms kinase inhibitors
The present invention is directed to substituted pyridine derivatives, pharmaceutical compositions containing said derivatives and the use of said derivatives...
US-1,007,1990 Site-specific orthogonal labeling of the carboxy terminus of .alpha.-tubulin in live cells
A technique is provided to visualize microtubules in live cells that does not require genetic manipulation or microinjection. Moreover, this method also avoids...
US-1,007,1989 Substituted cinnamamide derivative, preparation method and use thereof
The present invention relates to substituted cinnamamide derivatives, the method for preparing thereof and the use thereof. Each of said derivatives has a...
US-1,007,1988 Substituted 1,2,3-triazoles as NR2B-selective NMDA modulators
Substituted 1,2,3-triazoles as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for...
US-1,007,1987 Aminomethylene pyrazolones with therapeutic activity
A compound having the structure according to formula III ##STR00001## wherein: X is NH or S; R.sup.1 is H or (1C-4C)alkyl; R.sup.2 is (1C-4C)alkyl, phenyl or...
US-1,007,1986 Substituted pyrroles active as kinases inhibitors
The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases...
US-1,007,1985 Therapeutic compounds
The present disclosure relates to a compound of formula (Ia), (Ib), (IIa), and (IIb): ##STR00001## ##STR00002## which are useful in the treatment of a...
US-1,007,1984 Histone demethylase inhibitors
The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted ...
US-1,007,1983 Activatable fluorogenic compounds and uses thereof as near infrared probes
Novel fluorogenic compounds designed such that upon a chemical event, compounds capable of emitting NIR light are generated, are disclosed. The compounds...
US-1,007,1982 Method of treating neuropathic pain
Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.
US-1,007,1981 Method of priming plants against abiotic stress factors
A method of reducing cellular damage to a plant by treating the plant with a compound containing an NO-releasing moiety and an H.sub.2S-releasing moiety...
US-1,007,1980 Agonists that enhanced binding of integrin-expressing cells to integrin receptors
A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein...
US-1,007,1979 Process of producing cycloalkylcarboxamido-indole compounds
The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6- ...
US-1,007,1978 Process for the production of alpha-tocotrienol and derivatives
The invention discloses novel processes for production, enrichment and/or isolation of alpha-tocotrienol from source material comprising at least one...
US-1,007,1977 Highly purifid pharmaceutical grade tasimelteon
A process for preparing a batch of highly purified, pharmaceutical grade tasimelteon comprises analyzing a batch of tasimelteon synthesized under GMP conditions...
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