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Quinoline patents



      
           
This page is updated frequently with new Quinoline-related patent applications. Subscribe to the Quinoline RSS feed to automatically get the update: related Quinoline RSS feeds. RSS updates for this page: Quinoline RSS RSS


Date/App# patent app List of recent Quinoline-related patents
11/20/14
20140343480
 Systems, methods, and compositions for cross-linking patent thumbnailnew patent Systems, methods, and compositions for cross-linking
Various agents and additives for cross-linking treatments are identified in disclosed studies. The characteristics of the various agents and additives may be advantageously employed in formulations applied in cross-linking treatments of the eye.
11/20/14
20140343096
 Deuterated n-ethyl-n-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, salts and uses thereof patent thumbnailnew patent Deuterated n-ethyl-n-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, salts and uses thereof
The subject invention provides deuterated n-ethyl-n-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, its salts and uses.. .
11/20/14
20140343063
 Method of treating a viral infection using elvitegravir combinations patent thumbnailnew patent Method of treating a viral infection using elvitegravir combinations
The invention includes methods, compositions, and kits useful for treating a viral infection by administering 6-(3-chloro-2-fluorobenzyl)-1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof, with atazanavir or a pharmaceutically acceptable salt thereof, and optionally with a compound that inhibits cytochrome p-450, or a pharmaceutically acceptable salt thereof.. .
11/20/14
20140343062
 Method of treating a viral infection using elvitegravir combinations patent thumbnailnew patent Method of treating a viral infection using elvitegravir combinations
The invention includes methods, compositions, and kits useful for treating a viral infection by coadministering 6-(3-chloro-2-fluorobenzyl)-1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof, with lopinavir or a pharmaceutically acceptable salt thereof.. .
11/20/14
20140343036
 Isoquinoline and naphthyridine derivatives patent thumbnailnew patent Isoquinoline and naphthyridine derivatives
Wherein a, r1 and r2 are as described herein, compositions including the compounds and methods of using the compounds.. .
11/20/14
20140341994
 Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2 patent thumbnailnew patent Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (vmat2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.. .
11/13/14
20140336393
 Process for preparing modulators of cystic fibrosis transmembrane conductance regulator patent thumbnailProcess for preparing modulators of cystic fibrosis transmembrane conductance regulator
The present invention relates to processes for preparing solid state forms of n-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including compound 1 form a, compound 1 form a-hcl, compound 1 form b, and compound 1 form b-hcl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.. .
11/13/14
20140336386
 Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2 patent thumbnailFormulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
The present invention relates to new pharmaceutical compositions comprising benzoquinoline compounds, and methods to inhibit vesicular monoamine transporter 2 (vmat2) activity in a subject for the treatment of chronic hyperkinetic movement disorders.. .
11/13/14
20140336262
 Pharmaceutical compositions comprising napthamides patent thumbnailPharmaceutical compositions comprising napthamides
Disclosed herein are naphthamide and quinoline carboxamide compounds containing two bicyclic moieties, pharmaceutical compositions comprising those compounds and methods of using the compositions in the treatment of cancers mediated by cyclic-amp (camp) response element binding protein (creb). The disclosed compositions have utility in the treatment of lung, prostate and breast cancers in a human subject..
11/13/14
20140336221
 Antibiotic and anti-parasitic agents that modulate class ii fructose 1, 6-bisphosphate aldolase patent thumbnailAntibiotic and anti-parasitic agents that modulate class ii fructose 1, 6-bisphosphate aldolase
This invention provides a family of compounds that inhibit class ii fructose 1,6-bisphosphate aldolase (fba), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivatization and optimization of 8-hydroxyquinoline-2-carboxylic acid and related compounds.
11/13/14
20140336188
N-substituted indenoisoquinolines and syntheses thereof
N-substituted indenoisoquinoline compounds, and pharmaceutical formulations of n-substituted indenoisoquinoline compounds are described. Also described are processes for preparing n-substituted indenoisoquinoline compounds.
11/06/14
20140329855
Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
The present invention relates to solid state forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (compound 1), pharmaceutical compositions thereof and methods therewith.. .
11/06/14
20140329852
N-(imidazolidin-2-ylidene)quinoline derivatives as modulators of alpha 2 adrenergic receptors
The present invention relates to novel n-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.. .
10/30/14
20140323731
Lipidated imidazoquinoline derivatives
The compounds of the subject invention are adjuvant molecules that comprise an imidazoquinoline molecule covalently linked to a phospho- or phosphonolipid group. The compounds of the invention have been shown to be inducers of interferon-a, il-12 and other immunostimulatory cytokines and possess an improved activity profile in comparison to known cytokine inducers when used as adjuvants for vaccine antigens..
10/30/14
20140323521
Pharmaceutical compositions and administrations thereof
The present invention relates to the use of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, solids forms, and pharmaceutical compositions thereof for the treatment of cftr mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations.. .
10/30/14
20140323311
Pesticidal mixtures
The present invention relates to an agrochemical mixture for increasing the health of a plant, comprising as active ingredients a herbicidal compound (i) selected from the group consisting of: benzoic acids, pyridine carboxylic acids, quinoline carboxylic acids, and benazolin-ethyl; and a fungicidal compound (ii) in synergistically effective amounts. The present invention further relates to a method for improving the health of a plant, wherein the plant, the locus where the plant is growing or is expected to grow or plant propagation material from which the plant grows is treated with an effective amount of a mixture as defined above.
10/30/14
20140323310
Pesticidal mixtures
The present invention relates to an agrochemical mixture for increasing the health of a plant, comprising as active ingredients a herbicidal compound (i) selected from the group consisting of: benzoic acids, pyridine carboxylic acids, quinoline carboxylic acids, and benazolin-ethyl; and a fungicidal compound (ii) in synergistically effective amounts. The present invention further relates to a method for improving the health of a plant, wherein the plant, the locus where the plant is growing or is expected to grow or plant propagation material from which the plant grows is treated with an effective amount of a mixture as defined above.
10/30/14
20140323302
Process for the preparation of a quinoline carboxylic acid
The invention provides a process for the preparation of a carboxylic acid of formula (iv) (which is useful as a safener for herbicides): wherein r1 is hydrogen or chlorine, comprising the steps of: (i) subjecting a compound of formula (v) wherein: r1 is as defmed above; and r2 is c1-c18 alkyl; c1-c6 alkoxyc1-c8 alkyl-; optionally substituted phenyl; or optionally substituted benzyl; to hydrolysis under acidic conditions to give a solution of a quinolinium salt; and (ii) addingbase to the solution obtained in step (i) to give the free carboxylic acid (iv). The invention also provides a solid (e.g.
10/30/14
20140322296
Piperaquine microcapsules and compositions containing them
The present invention provides a microcapsule pharmaceutical composition of at least a bisquinoline drug. Said microcapsule comprises a drug core of a pharmaceutically effective amount of a bisquinoline drug and a polymeric coating over the core.
10/23/14
20140315948
Pharmaceutical composition and administrations thereof
The present invention relates to pharmaceutical compositions comprising a solid dispersion of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.. .
10/23/14
20140315944
Substituted naphthyridine and quinoline compounds as mao inhibitors
Wherein r1, r2, r3, y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting mao, and mao-b selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a cns disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.. .
10/16/14
20140309227
Quinoline carboxamide and quinoline carbonitrile derivatives as mglur2-negative allosteric modulators, compositions, and their use
The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (i) wherein ring a, rq, -l-, r1, n, r2, and r3 are as defined herein. The compounds of the invention are useful as non-competitive mglur2 antagonists, or mglur2 negative allosteric modulators (nams), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mglur2-nam receptor is involved, such as alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
10/02/14
20140296528
4-aryl-1-(biarylmethylene) piperidine compounds
The 4-aryl-1-(biarylmethylene)piperidine compounds are piperadine compounds having a biaryl substituent linked to the nitrogen atom of the piperidine ring by a methylene (—ch2—) group, and an aryl moiety attached to the 4-position of the piperidine ring. The aryl moiety may be a methoxy quinoline group, a 2-oxo quinoline group, or a 2-oxo, 3,4-dihydroxy quinoline group.
10/02/14
20140296251
Multifunctional quinoline derivatives as anti-neurodegenerative agents
Novel quinoline derivatives are disclosed. Also disclosed are synthesis and use thereof for treating neurodegenerative diseases..
10/02/14
20140296236
Quinolines as fgfr kinase modulators
The invention relates to new quinoline derivative compounds of formula (i), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. Cancer.
10/02/14
20140296224
Quinoline derivatives as pi3 kinase inhibitors
Invented is a method of inhibiting the activity/function of pi3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives..
10/02/14
20140296215
Cyanoquinoline compounds having activity in correcting mutant-cftr processing and increasing ion transport and uses thereof
The present disclosure provides pharmaceutical compositions, pharmaceutical preparations and methods for increasing activity of a mutant cystic fibrosis transmembrane conductance regulator protein (mutant-cftr). The pharmaceutical compositions, pharmaceutical preparations and methods are useful for the study and treatment of disorders associated with mutant-cftr, such as cystic fibrosis.
10/02/14
20140296214
Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
The present invention provides compounds of formula (i): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor xia and/or plasma kallikrein which may be used as medicaments..
09/25/14
20140288310
7--6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid crystal
Disclosed is a technique for improving the water solubility and storage stability of 7-{(3s,4s)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-y1}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound (1)) that is safe and not only has a strong antibacterial action but also is effective for resistant bacteria for which conventional antibacterial agent are less effective. Crystals of the hydrochloride salt of the compound (1), crystals of the hydrochloride salt hydrate of the compound (1), and crystals of the methanesulfonate salt of the compound (1) are provided.
09/25/14
20140284556
6h-indeno[2,1-b]quinoline derivative and organic light emitting diode using the same
A 6h-indeno[2,1-b]quinoline derivative has a structure of formula (i). Each of ar1 and ar2 is a member selected from the group consisting of a substituted or non-substituted aryl group and a substituted or non-substituted heteroaryl group and r1 to r9 are substituents.
09/18/14
20140275548
Substituted naphthyridine and quinoline compounds as mao inhibitors
Wherein r1, r2, r3, y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting mao, and mao-b selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a cns disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.. .
09/18/14
20140275161
Combination therapy
Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog.
09/18/14
20140275160
Combination therapy
Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog.
09/18/14
20140275129
Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone compounds
Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone derivatives represented by formula (i), pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for treating hyperproliferative disorders by administering the compounds are also described.
09/18/14
20140275061
Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
The present invention provides compounds of formula (i): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor xia and/or plasma kallikrein which may be used as medicaments..
09/18/14
20140274960
Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
The present invention provides compounds of formula (i) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor xia and/or plasma kallikrein which may be used as medicaments..
09/18/14
20140273109
Benzylisoquinoline alkaloids (bia) producing microbes, and methods of making and using the same
Aspects of the invention include host cells that are engineered to produce benzylisoquinoline alkaloids (bias). The host cells include heterologous coding sequences for a variety of enzymes involved in synthetic pathways from starting compounds to bias of the host cell.
09/18/14
20140271878
Crystals of laquinimod sodium and improved process for the manufacture thereof
F) an amount of methyl 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carboxylate (mcqme) in the mixture is no more than 0.12% relative to the amount of laquinimod sodium as measured by hplc.. .
09/11/14
20140256948
3-cyano-quinoline derivatives with antiproliferative activity
Ar5 represents phenyl optionally substituted with cyano.. .
09/11/14
20140256938
Process for preparing quinoline derivatives
(c) coupling a compound of formula a with an amine of formula b to form a compound of formula i.. .
09/11/14
20140256922
Toll-like receptor-7 and -8 modulatory 1h imidazoquinoline derived compounds
The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides tlr7 agonists and tlr7/tlr8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof.
09/11/14
20140256769
Crystalline form of a quinolinone-carboxamide compound
The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1s,3r,5r)-8-[(r)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-ht4 receptor activity, and processes useful for preparing such crystalline salt forms..
09/11/14
20140256670
Azidothymidine quinoline conjugated compound, preparation method therefor and application thereof in anti-hepatoma therapy
The invention provides zidovudine conjugated quinoline compound n-((1-(2-(hydroxy-methyl)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2h)-yl)-tetrahydrofuran-3-yl)-1h-1,2,3-triazol-4-yl)methyl)-6-(4b,8,8-trimethyl-4b,5,6,7,8,8a-hexahydrodibenzo[a,c]phenazin-2-yloxy)hexanamide. The compound can selectively kills the hepatoma cells especially the hepatoma cells with hepatitis b, and inhibit the growth of subcutaneous tumors in mice, but has no significant toxicity to normal liver cells.
09/11/14
20140255483
Pharmaceutical composition and administrations thereof
The present invention relates to pharmaceutical compositions containing a solid dispersion of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical composition.. .
09/04/14
20140249312
[1,3]dioxolo[4,5-g]quinoline-6(5h)thione and [1,3]dioxolo[4,5-g][1,2,4]triazolo[1,5-a]quinoline derivatives as inhibitors of the late sv40 factor (lsf) for use in treating cancer
The present invention relates generally to [1,3]dioxolo[4,5-g]quinoline-6(5h)thione and [1,3]dioxolo[4,5-g][1,2,4]triazolo[1,5-a]quinoline derivatives and/or compositions for use in inhibiting, preventing and/or treating cancer, e.g. Hepatocellular carcionoma (hcc).
09/04/14
20140249201
Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents.
09/04/14
20140249174
Aryl-and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline
Wherein the variables r1, r2, r3, r4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (hsd) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia..
09/04/14
20140249144
Prophylactic and/or therapeutic agent for anemia comprising tetrahydroquinoline compound as active ingredient
Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of epo and/or an activity of enhancing the production of hemoglobin. Specifically disclosed is and epo production enhancer and/or a hemoglobin production enhancer comprising a 1-acyl-4-(substituted oxy, substituted amino, or substituted thio)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by general formula (1) [wherein r1, r2, r2′, r3 and r3′ independently represent a hydrogen atom, a c1-6 alkyl group, or the like; r4, r5, r6, r7, r8, r9 and r10 independently represent a hydrogen atom, a halogen atom, a c1-6 alkyl group, or the like; a represents n—r11, a sulfur atom, or an oxygen atom; r11 represents a hydrogen atom, a c1-6 alkyl group, or the like; b represents a c6-14 aryl group, or a 5- to 10-membered heterocyclic group; and n represents an integer of 0 or 1], a salt of the tetrahydroquinoline compound, or a solvate of the tetrahydroquinoline compound or the salt..
08/28/14
20140243524
Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
With r1, r2, r3, r4, r5, r6, r7, r8, and r14 defined herein.. .
08/28/14
20140243396
Method of treating mucoepidermoid carcinoma
Imidazoquinolines, as set forth in formula (i), are useful for inhibiting growth or proliferation of mucoepidermoid carcinoma cells. The therapeutic and prophylactic treatments provided by this invention are practiced by administering to a patient in need thereof an amount of a compound of formula (i) that is effective to inhibit growth or proliferation of the mucoepidermoid carcinoma cells..
08/28/14
20140243311
Novel octahydrothienoquinoline derivative, pharmaceutical composition comprising derivative, and use of these
The present invention provides compounds represented by the general formula (i): or pharmaceutical acceptable salts thereof, wherein r1 is cyano or the like; r2 and r3 are hydrogen or the like; r4 is c1-6 alkyl or the like; r5 is c1-6 alkyl, halo-c1-6 alkyl, cycloalkyl, cycloalkyl-c1-6 alkyl, aralkyl or the like; r6 and r7 are each hydrogen, c1-6 alkyl, halo-c1-6 alkyl, cycloalkyl, c1-6 alkoxy-c1-6 alkyl, r12r13n—c1-6 alkyl or the like, which exhibit potent dopamine d2 receptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof..
08/28/14
20140242172
Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
The present invention relates to solid state forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (compound 1), pharmaceutical compositions thereof and methods therewith.. .
08/28/14
20140242121
Novel imidazole quinoline-based immune system modulators
The present invention relates to a compound of formula i: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.. .
08/21/14
20140235862
Method for producing 4, 4-difluoro-3,4-dihydroisoquinoline derivatives
Is reacted with hydrogen fluoride.. .
08/21/14
20140235644
Indolyl-substituted pyrazino-quinolines and their use for the treatment of cancer
Wherein the wedged bonds, r1, r2, r3, r4, r5, r5a, r6, r7, r8, r9, r10, r11, r12, r13, r14, x and y have meanings given in the description, and pharmaceutically-acceptable salts thereof; and methods of using such compounds useful in the treatment of cancer and conditions affected by inhibition of angiogenesis. Also provided, are processes for the preparation of formula i, by reacting formula i with other compounds; and processes for the preparation of a pharmaceutical formulation by bringing into association, a compound of formula i, with therapeutic agents and/or a pharmaceutically-acceptable adjuvant, diluent, or carrier..
08/21/14
20140235593
Substituted 2-alkyl-1-oxo-n-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides for antimalarial therapies
In one aspect, the invention relates to novel substituted 2-alkyl-1-oxo-n-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating and/or preventing malaria. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention..
08/14/14
20140228576
Method for producing 3,4-dihydroisoquinoline derivatives and production intermediates of same
Provided are an efficient method for producing 3,4-dihydroisoquinoline derivatives and useful production intermediates thereof. Provided is a method for producing 3,4-dihydroisoquinoline derivatives represented by general formula (1), comprising converting a compound represented by general formula (3) in the presence of acid after reacting with an aniline derivative, or converting a compound represented by general formula (3) by reacting with an aniline derivative in the presence of an acid..
08/14/14
20140228575
Process for the preparation of solifenacin and salts thereof
The invention provides a new process for the preparation of solifenacin or a pharmaceutically acceptable acid addition salt thereof, comprising reacting (r)-quinuclidin-3-yl phenethylcarbamate with benzaldehyde in the presence of an acid to obtain a diasteroisomeric mixture (s,r)—((r)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1h)-carboxylate of formula (iv) which can be resolved and the solifenacin or a pharmaceutically acceptable acid addition salt thereof recovered. The invention also provides the new key intermediate (r)-quinuclidin-3-yl phenethylcarbamate involved in the process.
08/14/14
20140228572
Method for producing optically active tetrahydroquinolines
In the presence of a hydrogen donor compound and an iridium (iii) complex having a chiral prolinamide compound as a ligand to give an optically active 2-substituted-1,2,3,4-tetrahydroquinoline represented by formula [ii]:. .
08/14/14
20140228392
Compositions and methods for treating cancer
The present invention is bis-acridine or bis-quinoline intercalators having a modified bis(4-aminophenyl)ether tether to improve activity, selectivity, solubility and bioavailability of the antitumor compound.. .
08/14/14
20140228371
Quinoline and quinazoline amides as modulators of sodium channels
The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.. .


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Quinoline topics: Isoquinolin, Praziquantel, Carbon Atoms, Crystallin, Quinoline Derivatives, Pharmaceutically Acceptable Salt, Alkyl Group, Cycloalkyl, Pharmaceutically Acceptable Salts, Immunodeficiency, Retrovirus, Viral Infection, Human Immunodeficiency Virus, Angiogenesis, Sulfonamide

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