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Quinoline patents



      

This page is updated frequently with new Quinoline-related patent applications.




Date/App# patent app List of recent Quinoline-related patents
07/21/16
20160208299 
 Production of isoquinoline alkaloids and flavonoids in plant cell cultures of goldenseal (hydrastis canadensis) patent thumbnailnew patent Production of isoquinoline alkaloids and flavonoids in plant cell cultures of goldenseal (hydrastis canadensis)
Natural product preparations of isoquinoline alkaloids are obtained from plant callus cells of goldenseal, hydrastis canadensis, grown in suspension cell culture. The natural product preparations can be extracted from the cells and/or obtained from the culture medium in which the cells are grown.
Dianaplantsciences Inc.


07/21/16
20160208269 
 Compositions and methods for producing benzylisoquinoline alkaloids patent thumbnailnew patent Compositions and methods for producing benzylisoquinoline alkaloids
The present invention relates to host cells that produce compounds that are characterized as benzylisoquinolines, as well as select precursors and intermediates thereof. The host cells comprise one, two or more heterologous coding sequences wherein each of the heterologous coding sequences encodes an enzyme involved in the metabolic pathway of a benzylisoquinoline, or its precursors or intermediates from a starting compound.
California Institute Of Technology


07/14/16
20160201067 
 Composition for enhancing transgene expression in eukaryotic cells and  enhancing production of a target protein encoded by a transgene patent thumbnailComposition for enhancing transgene expression in eukaryotic cells and enhancing production of a target protein encoded by a transgene
Production of dna vectors with the inserted gene of a target protein and the production of recombinant protein in eukaryotic cell cultures is disclosed. A composition for the intensive production of target protein in eukaryotic cells comprises a dna vector with the inserted gene of a target protein and an agonist of cell receptors belonging to the pattern recognition receptor (prr) family selected from the following agonists: tlr2, or tlr4, or tlr5, or tlr7, or tlr8, or tlr9, or nod1 receptor, or nod2 receptor, used in an optimal ratio.
Silezia Group Pte. Ltd


07/14/16
20160200685 
 Substituted 1,2,3,4-tetrahydroisoquinoline derivatives for the treatment of hormone-dependent diseases patent thumbnailSubstituted 1,2,3,4-tetrahydroisoquinoline derivatives for the treatment of hormone-dependent diseases
Provided are compounds of general formula a and a′, wherein x1 and x2 are each c, ch or n; r3 and r4 are each h, optionally substituted c1-c30 saturated or unsaturated chemical group, or together form an optionally substituted c5-c8 cycle; z1; z2 and z3 are each n or ch; v is c═o, c═s or ch2; n is from 1 to 12; w1 and w2 are each h, ch2, o or s; and r1 and r2 are each h, cr1c6 alkyl, c1c6 aryl, c1c12 alkylaryl, optionally substituted phenyl, c1c6 alkoxy, c1c6 thioalkoxy, f, cl, br or i. These compounds inhibit steroid sulfatase (sts), act as selective estrogen receptor modulators (serms), increase alkaline phosphatase (alp) activity, and are useful in the treatment of medical conditions involving hormones such as breast cancer, prostate cancer, endometriosis, osteoporosis, benign prostatic hyperplasia and endometrial cancer..
UniversitÉ Laval


07/07/16
20160197285 
 Organic electroluminescent materials and devices patent thumbnailOrganic electroluminescent materials and devices
Formula i, is disclosed. In the structure of formula i: x is selected from a group consisting of o, s and se; g2 and g3 are each independently selected from benzene, biphenyl, fluorene, naphthalene, phenanthrene, tripheylene, dibenzofuran, dibenzothiophene, dibenzoselenophene, pyridine, pyrimidine, quinoline, isoquinoline, phenanthroline, aza-fluorene, and combinations thereof; l is selected from phenyl, biphenyl, terphenyl and pyridine, and combinations thereof; g2, g3 and l are each optionally further substituted with one or more unfused substituents; r1, r2, and each r3, r4, r5 and r6 are an unfused substituent selected from hydrogen, deuterium, alkyl, alkoxyl, cycloalkyl, cycloalkoxyl, halogen, nitro, nitrile, silyl, benzene, biphenyl, terphenyl, pyridine, and combinations thereof; and r1 and r2 are optionally joined to form a ring.

07/07/16
20160194332 
 Novel quinoline -substituted compound patent thumbnailNovel quinoline -substituted compound
The present invention provides a compound represented by formula (i) below, or a salt thereof.. .

07/07/16
20160194304 
 Isoindoline or isoquinoline compounds, a process for their preparation and pharmaceutical compositions containing them patent thumbnailIsoindoline or isoquinoline compounds, a process for their preparation and pharmaceutical compositions containing them
Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.. .

07/07/16
20160194285 
 Process for making isoquinoline compounds patent thumbnailProcess for making isoquinoline compounds
The present invention relates to methods for making isoquinoline compounds and the intermediate compounds achieved thereby. Such compounds can be used to prepare compounds and compositions capable of decreasing hif hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (hif)..
Fibrogen, Inc.


06/30/16
20160185728 
 Cyanoquinoline derivatives patent thumbnailCyanoquinoline derivatives
Wherein r1, r2, r3 and r4 are each as defined in the present application.. .

06/30/16
20160185727 
 Substituted 4-amino-5-(cyclohexyloxy)quinoline-3-carboxylic acids as sweet flavor modifiers patent thumbnailSubstituted 4-amino-5-(cyclohexyloxy)quinoline-3-carboxylic acids as sweet flavor modifiers
Disclosed herein are 4-amino-5-(cyclohexyloxy)quinoline-3-carboxylic acid compounds having useful as sweet flavor modifiers. Also disclosed herein are ingestible compositions that include one or more of these compounds in combination with a natural or artificial sweetener..

06/30/16
20160185725 

C-met modulators and use


The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-met, kdf, c-kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.

06/23/16
20160176841 

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, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (sle) and lupus nephritis.. .

06/16/16
20160168161 

Method for producing heterocyclic compound


There is provided a method for producing with a high efficiency a heterocyclic compound that is useful as a raw material for pharamaceuticals. A novel production method for producing 2,2,7,9-tetramethyl-2h-pyrano[2,3-g]quinoline (compound (6)) that has a quinoline ring and a chromene ring using n-(3-acetyl-4-hydroxyphenyl)butylamide (compound (1′)) that is commercially available as a raw material for pharamaceuticals or the like as a starting raw material; and a method for purifying compound (6), characterized by purifying by subjecting it to conversion into a salt form..
Nissan Chemical Industies, Ltd.


06/16/16
20160168121 

Quinoline derivative


A compound represented by general formula (i) has a strong axl inhibitory activity by introducing a distinctive bicyclic structure in which a saturated carbon ring is fused to a pyridone ring, and can be a therapeutic agent for axl-related diseases, for example, cancer such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases.. .
Ono Pharmaceutical Co., Ltd.


06/16/16
20160168100 

Anti-hiv compounds


This invention provides, among other things, tetrahydroisoquinolines useful for treating viral infections, pharmaceutical formulations containing such compounds, as well as methods of inhibiting the replication of a virus, such as hiv, or treating a disease, such as aids.. .
Prosetta Antiviral, Inc.


06/16/16
20160168099 

Novel bisaminoquinoline compounds, pharmaceutical compositions prepared therefrom and their use


The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and/or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention.
The Trustees Of The University Of Pennsylvania


06/09/16
20160160250 

Hyphomicrobium sp. microorganism and producing pyrroloquinoline quinone using the same


Provided are a hyphomicrobium sp. Mutant strain swb-p91 (kctc12695bp) having high productivity of pyrroloquinoline quinone, and a method of producing a hyphomicrobium sp.
Sungwun Bio Co., Ltd.


06/09/16
20160159790 

Pyrroloquinoline derivatives as 5-ht6 antagonists, preparation method and use thereof


This invention concerns pyrroloquinoline derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in schizophrenia, anxiety, depression, maniac depression, epilepsy, obsessive compulsive disorders, mood disorders, migraine, alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, panic attacks, attention deficit hyperactivity disorder, attention deficit disorder, parkinson's disease, huntington's disease, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, obesity and type-2 diabetes, functional bowel disorder, irritable bowel syndrome.
Universite De Montpellier


06/09/16
20160159788 

Method for preparation of 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4as,7as)-octahydro-6h-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid


This invention relates to methods for preparation of chemical compound 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4a8,7as)-octahydro-6h-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid, which comprise addition of heterocyclic amine containing protecting group, to ethyl-3-oxo-3-(2,4,5-trifluoro-3-methoxyphenyl)propanoate, followed by interaction with triethyl orthoformate, addition of cyclic amine, subsequent cyclization and formation of target product. The method for preparation claimed is technologically simple in comparison with analogue and requires no special complex technical operations, which in its turn simplifies method for preparation of this chemical compound, and reduces cost of the final product, while the commercial production utilizing the mehod claimed has low degree of environmental threat..

06/09/16
20160159744 

Quinoline carboxamide and quinoline carbonitrile derivatives as mglur2-negative allosteric modulators, compositions, and their use


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, including potentially 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.

06/09/16
20160158220 

Benzoquinoline inhibitors of vesicular monoamine transporter 2


The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (vmat2), pharmaceutical compositions thereof, and methods of use thereof.. .
Auspex Pharmaceuticals, Inc.


06/09/16
20160158217 

Quinoline carboxamide and quinoline carbonitrile derivatives as mglur2-negative allosteric modulators, compositions, and their use


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, including potentially 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.

06/09/16
20160158216 

Crystals of laquinimod sodium and improved process for the manufacture thereof


F) an amount of 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.. .

06/02/16
20160151349 

Pharmaceutical compositions comprising 7-(1h-imidazol-4-ylmethyl)-5,6,7,8-tetrahydro-quinoline for treating skin diseases and conditions


The present invention relates to a method for treating skin diseases and skin conditions in a patient in need thereof which comprises of administering a therapeutically effective amount of a pharmaceutical composition comprising a therapeutically effective amount of 7-(1h-imidazol-4-ylmethyl)-5,6,7,8-tetrahydro-quinoline, or its individual enantiomers or the tautomers thereof, or a pharmaceutically acceptable salt thereof.. .
Allergan, Inc.


06/02/16
20160151346 

N-ethyl-n-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide, preparation and uses thereof


The subject invention provides a pharmaceutical composition containing laquinimod or a pharmaceutically acceptable salt thereof, and a compound of n-ethyl-n-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide or a salt thereof.. .
Teva Pharmaceutical Industries, Ltd.


06/02/16
20160151345 

N-ethyl-n-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide, preparation and uses thereof


The subject invention provides a pharmaceutical composition containing laquinimod or a pharmaceutically acceptable salt thereof, and a compound of n-ethyl-n-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide or a salt thereof.. .
Teva Pharmaceutical Industries, Ltd.


05/26/16
20160145263 

Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors


The present invention provides compounds of formula (i), or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor xia inhibitors or dual inhibitors of fxia and plasma kallikrein.
Bristol-myers Squibb Company


05/26/16
20160145213 

Heterocyclic compounds and methods of their use


The present invention relates generally to compounds that are useful in antagonizing the angiotensin ii type 2 (at2) receptor. More particularly, the invention relates to substituted isoquinoline compounds and their use as at2 receptor antagonists.
Novartis Ag


05/26/16
20160143899 

Method for treating abnormal b-amyloid mediated diseases


A method for treating abnormal β-amyloid mediated diseases is disclosed, comprising administering a pharmaceutical composition to a subject in need, wherein the pharmaceutical composition comprises an indolylquinoline derivative represented by the following formula 1:. .
National Taiwan Normal University


05/19/16
20160137641 

Pyrroloquinoline quinone lithium salt crystal and preparation method and application thereof


The present invention provides pyrroloquinoline quinone lithium salt crystal and a preparation method and application thereof. Characteristic absorption peaks appear when the diffraction angles are 6.222±0.2°, 7.379±0.2°, 7.941±0.2°, 23.631±0.2°, 24.044±0.2°, 25.497±0.2°, 27.541±0.2°, 30.736±0.2°, and 32.306±0.2° degrees in a powder x-ray diffraction pattern of the pyrroloquinoline quinine lithium salt crystal.
Shanghai Ri Xin Biotechnology Co., Ltd.


05/19/16
20160136166 

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.
Rexahn Pharmaceuticals, Inc.


05/12/16
20160130264 

Synthesis of fatostatin based polycyclic compounds


The r substituents are h, methyl, isopropyl, benzyl, cyclohexyl, cyclopropylmethyl, methoxy, tert-butyloxycarbonyl, methanesulfonyl, p-toluenesulfonyl, quinolinesulfonyl, or thiophenesulfonyl groups. The method comprises condensing prothionamide with a halo nitroacetophenone to form a nitrophenyl substituted thiazole, reducing the nitro group to form an amine and derivatizing the amine to produce the compound..

05/05/16
20160122338 

Novel photochromic tetrahydroindolizines


Photochromic tetrahydroindolizines (this) bearing dihydroisoquinoline derivatives as heterocyclic bases and central fluorene groups have been synthesized via different chemical and photochemical pathways. Three alternative pathways for the synthesis of the target photochromic thi-based pyridazinopyrrolo[1,2-b]isoquinolines via in situ trapping with hydrazine hydrate are also provided.
Umm Al-qura University


05/05/16
20160122303 

Biocatalyzed synthesis of the optically pure (r) and (s) 3-methyl-1,2,3,4-tetrahydroquinoline and their use as chiral synthons for the preparation of the antithrombic (21r)- and (21s)-argatroban


The present invention relates to the biocatalyzed synthesis of enantiomerically pure (3r) and (3s)-methyl-1,2,3,4-tetrahydroquinoline. Said enantiomerically pure compounds are useful as chiral synthons in organic synthesis and, in particular, for the preparation of diastereomerically pure (21r) and (21s)-agratroban and its analogues.
Euticals S.p.a.


05/05/16
20160120859 

Pharmaceutical formulations of a hif hydroxylase inhibitor


The present disclosure relates to pharmaceutical formulations of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid and methods of use thereof.. .
Fibrogen, Inc.


04/28/16
20160115154 

Quinoline inhibitor of the macrophage stimulating 1 receptor mstr1


Is an inhibitor of ron and can be employed, for the treatment of cancer.. .

04/28/16
20160115090 

Pyrotechnic yellow smoke compositions based on solvent yellow 33


A yellow smoke composition useful in hand held signals, such as the u.s. Army m194 yellow smoke parachute signal; which composition contains the nontoxic, environmentally safe, quinoline solvent yellow 33 color agent and critically exhibits the requisite dense yellow smoke for the requisite 9 to 18 second burn time upon use.

04/28/16
20160113919 

Chloroquine stereoisomer for treating tuberculosis related diseases


This disclosure provides a method of treating a subject infected with a mycobacteria of the m. Tuberculosis complex or infected with an atypical mycobacterium.
The Board Of Trustees Of The Leland Stanford Junior University


04/28/16
20160113918 

Heterocyclic gsk-3 allosteric modulators


The present invention relates to heterocyclic substituted quinoline derivatives as allosteric inhibitors of the glycogen synthase kinase-3 (gsk-3) enzyme. Therefore, these compounds are useful for the manufacturing of a medicament designed for the treatment and/or prevention of diseases wherein gsk-3 is involved, such as neurodegenerative diseases, inflammatory diseases, cancer, diabetes, and to promote various regenerative processes..
Consejo Superior De Investigaciones Cientificas (csic)


04/21/16
20160108042 

Indolizino[3,2-c]quinoline derivatives, pharmaceutically acceptable salt thereof, preparation method thereof and pharmaceutical composition for treatment of cystic fibrosis containing the same as active ingredient


Provided are an indolizino[3,2-c]quinoline derivative, pharmaceutically acceptable salt thereof, and a method for preparing the same. The indolizino[3,2-c]quinoline derivative, pharmaceutically acceptable salt thereof may function as an agonist of cystic fibrosis conductance transmembrane regulator, and thus may be useful for an agent for preventing or treating diseases caused by degradation of activity of cystic fibrosis conductance transmembrane regulator and for a pharmaceutical composition for stimulating proliferation of stem cells..

04/21/16
20160106869 

Fluorescent solid lipid nanoparticles composition and preparation thereof


The present invention discloses a solid lipid nanoparticle (sln) comprising: a) a solid lipid core comprising at least a glyceride and/or at least a fatty acid; b) a mixture of amphiphilic components forming a shell around said core a); c) an alkaline-earth complex with a compound of formula i and/or ii: d) at least a fluorescent dye selected from: a cyanine fluorescent dye and/or a polyetherocyclic compound selected from: coumarin, pyrano, quinoline, pyranoquinoline, indole and pyranoindole derivates in acid form or a pharmaceutically acceptable salt thereof. These nanoparticles allow a prolonged blood circulation half-life, show enhanced photostability and improved fluorescence signal.

04/14/16
20160104553 

Binder pitch and producing the same


The object of the present invention is to provide a binder pitch increased in carbonization yield (fixed carbon content) without varying the softening point thereof. A binder pitch has a carbon-to-hydrogen molar ratio of 1.90 or more, a quinoline insoluble content of 12.0% to 30.0% by mass, a free carbon content of 12.0% to 30.0% by mass, a mesophase content of 0.50% by mass or less, a toluene insoluble content of 24.0% by mass or more, and a fixed carbon content of 58.0% by mass or more..

04/14/16
20160101173 

Aqueous gel formulations containing immune response modifiers


Aqueous gel formulations, including an immune response modifier (irm), such as those chosen from imidazoquinoline amines, tetrahydroimidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, 1,2-bridged imidazoquinoline amines, imidazonaphthyridine amines, imidazotetrahydronaphthyridine amines, oxazoloquinoline amines, thiazoloquinoline amines, oxazolopyridine amines, thiazolopyridine amines, oxazolonaphthyridine amines, thiazolonaphthyridine amines, pyrazolopyridine amines, pyrazoloquinoline amines, tetrahydropyrazoloquinoline amines, pyrazolonaphthyridine amines, tetrahydropyrazolonaphthyridine amines, and 1h-imidazo dimers fused to pyridine amines, quinoline amines, tetrahydroquinoline amines, naphthyridine amines, or tetrahydronaphthyridine amines, are provided. Methods of use and kits are also provided..

04/14/16
20160101099 

H3 receptor antagonist for use in the treatment of alzheimer's disease


This disclosure relates to methods of using 2-(cyclohexylmethyl)-n-{2-[(2s)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide in a disease modifying therapy of alzheimer's disease, other tauopathies and related neurodegenerative diseases.. .

04/07/16
20160096807 

Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator


The present disclosure relates to co-crystals comprising n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (compound 1) and a co-former and methods for their preparation. The present disclosure further relates to pharmaceutical compositions comprising the co-crystal forms, as well as methods of treatment therewith and kits..
Vertex Pharmaceuticals Incorporated


04/07/16
20160096806 

2-aminoquinoline-based compounds for potent and selective neuronal nitric oxide synthase inhibition


Various 2-aminoquinoline compounds as can be used, in vivo or in vitro, for selective inhibition of neuronal nitric oxide synthase.. .

04/07/16
20160095849 

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..
Theravance Biopharma R&d Ip, Llc


03/24/16
20160083671 

Polyalkylene glycol-based industrial lubricant compositions


A lubricant composition comprises as a lubricant base, an oil soluble polyalkylene glycol suitable for use as a lubricant in an industrial oil, grease or metal working fluid; and an additive comprising (1) alkylated phenyl-α-naphthylamine; and (2) 2,2,4-trialkyl-1,2-dihydroquinoline.. .
Vanderbilt Chemical, Llc


03/24/16
20160083385 

Pyrazinoisoquinoline compounds


Where the designation (r) indicates that the designated carbon has the (r) stereochemistry; and wherein z1 is hydrogen or fluorine; z2 is hydrogen, deuterium, or fluorine; z3 is deuterium; z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m+n does not exceed 10; and when both z1 and z2 are hydrogen, the sum of m+n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel..

03/24/16
20160083351 

Tetrahydroisoquinolines as selective nadph oxidase 2 inhibitors


Wherein “” represents a single or double bond, r1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; ra is hydrogen, —ch2r2, r3, or —so2r4; r2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; r3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; r4 is lower aliphatic, or substituted or unsubstituted aryl; and r5 is hydrogen, halogen, or lower aliphatic.. .

03/24/16
20160081999 

Synthesis and use of dual tyrosyl-dna phosphodiesterase i (tdp1) - topoisomerase i (top1) inhibitors


The invention described herein pertains to the synthesis and use of certain n-substituted indenoisoquinoline compounds which inhibit the activity tyrosyl-dna phosphodiesterase i (tdp1) or topoisomerase i (top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel n-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel n-substituted indenoisoquinoline compounds..
Purdue Research Foundation


03/17/16
20160075715 

Substituted tetrahydroisoquinoline compounds as factor xia inhibitors


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..

03/17/16
20160075700 

Yellow reduced pyrroloquinoline quinone crystal and producing the same, and food, pharmaceutical, gel, composition and producing composition


A yellow reduced pyrroloquinoline quinone crystal having a solubility in water of 0.040 to 0.20 (mg/ml).. .
Mitsubishi Gas Chemical Company, Inc.


03/17/16
20160075688 

New 3,4-dihydro-2h-isoquinoline-1-one and 2,3-dihydro-isoindol-1-one compounds


Wherein r1, r2, r3, r4, r5, r6, r7, r8, r9, r10, r11, r12, r13, r14, r15, a, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.. .

03/17/16
20160075687 

New 3,4-dihydro-2h-isoquinoline-1-one and 2,3-dihydro-isoindol-1-one compounds


Wherein r1, r2, r3, r4, r5, r6, r7, r8, r9, r10, r11, r12, r13, r14, r15, a, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.. .

03/17/16
20160075686 

New 3,4-dihydro-2h-isoquinoline-1-one and 2,3-dihydro-isoindol-1-one compounds


Wherein r1, r2, r3, r4, r5, r6, r7, r8, r9, r10, r11, r12, r13, r14, a, b, m, n and p are as described herein, compositions including the compounds and methods of using the compounds.. .

03/17/16
20160075657 

Tetrahydroisoquinoline derivatives, pharmaceutical compositions and uses thereof


Wherein r1 to r6, n and m are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.. .

03/17/16
20160075656 

Quinoline amide m1 receptor positive allosteric modulators


The present invention is directed to quinoline amide compounds of formula (i) which are m1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the m1 receptor is involved, such as alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositious comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the m1 receptor..
Merck Sharp & Dohme Corp.


03/17/16
20160074377 

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.. .

03/03/16
20160060270 

New aryl-quinoline derivatives


Wherein r1, r2, r3, r4, r5, r6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (fabp) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases..

03/03/16
20160060263 

Pyrazinoisoquinoline compounds


This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel.
Concert Pharmaceuticals, Inc.


03/03/16
20160060222 

Amino-quinolines as kinase inhibitors


Wherein r1, r2 and a are as defined herein, and methods of making and using the same.. .

03/03/16
20160058749 

Treatments for neuropathy


Small fiber neuropathy is treated or prevented by topically administering to a subject in need thereof topically active quinoline compounds or pharmaceutically acceptable salts thereof under conditions effective to treat or prevent neuropathy in the subject. Glial cell-derived neurotrophic factor (gdnf) receptors are modulated with the subject active quinoline compounds, which may be formulated in topical lotions..
Children's Medical Center Corporation


02/25/16
20160052889 

Phenoxyethyl dihydro-1h-isoquinoline compounds


The present invention provides a compound of the formula i: wherein r is h or f; or a pharmaceutically acceptable salt thereof.. .
Eli Lilly And Company


02/25/16
20160051534 

Pharmaceutical compositions comprising 7-(1h-imidazol-4-ylmethyl)-5,6,7,8- tetrahydro-quinoline for treating skin diseases and conditions


The present invention relates to a method for treating skin diseases and skin conditions in a patient in need thereof which comprises of administering a therapeutically effective amount of a pharmaceutical composition comprising a therapeutically effective amount of 7-(1h-imidazol-4-ylmethyl)-5,6,7,8-tetrahydro-quinoline, or its individual enantiomers or the tautomers thereof, or a pharmaceutically acceptable salt thereof.. .
Allergan, Inc.


02/18/16
20160046623 

Salt of pyrazoloquinoline derivative, and crystal thereof


The present invention provides a salt of (s)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1h-pyrazolo[4,3-c]quinolin-4(5h)-one and an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, malonic acid, maleic acid, tartaric acid, methanesulfonic acid, benzenesulfonic acid and toluenesulfonic acid; or a crystal thereof with a potential to be used as drug substance in pharmaceuticals.. .
Eisai R&d Management Co., Ltd.


02/18/16
20160046603 

Crystalline forms of d-glucitol, 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridine-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1-yl)-4-oxo-3-quinolinecarboxylate


The present disclosure relates generally to crystalline forms of anhydrous d-glucitol, 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1- yl)-4-oxo-3-quinolinecarboyxlate, compositions comprising the same, and methods of making the same. Delafloxacin is an fluoroquinolone antibiotic with the chemical structure and the chemical name 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxyazetidin-1-yl)-4-oxo-3-quinolinecarboyxlate.
Melinta Therapeutics, Inc.


02/18/16
20160046583 

Isoquinoline derivatives


For the treatment of schizophrenia, obsessive-compulsive personality disorder, depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, parkinson's disease, dementia, alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction (“chemobrain”), down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine or cocaine.. .

02/18/16
20160045489 

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.. .
Allergan, Inc.


02/18/16
20160045447 

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.
Adare Pharmaceuticals S.r. L.


02/11/16
20160039816 

Crystals of pyrroloquinolinequinone sodium salts


A crystal of pyrroloquinoline quinone disodium salt having peaks at 2θ of 9.1°, 10.3°, 13.8°, 17.7°, 18.3°, 24.0°, 27.4°, 31.2° and 39.5° (±0.2° for each) in powder x-ray diffractometry using cu kα radiation, or a crystal of pyrroloquinoline quinone trisodium salt having peaks at 2θ of 6.6°, 11.4°, 13.0°, 22.6°, 26.9°, 27.9°, 37.0°, 38.9° and 43.4° (±0.2° for each) in powder x-ray diffractometry using cu kα radiation.. .
Mitsubishi Gas Chemical Company, Inc.


02/11/16
20160039786 

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..
Mitsui Chemicals Agro, Inc.


02/11/16
20160038503 

Methods and compositions useful for treating diseases involving bcl-2 family proteins with isoquinoline and quinoline derivatives


The present invention relates to a compositions for and methods for cancer treatment, for example, hematopoietic cancers (e.g. B-cell lymphoma).

02/11/16
20160038478 

Composition and methods for treating skin conditions


Compositions and methods for treatment of conditions affecting skin and/or mucosal surfaces of a subject that make use of an imidazoquinoline compound and a retinoid agent are described.. .
442 Ventures, Llc


02/04/16
20160030416 

Methods of treating b2-bradykinin receptor mediated angioedema


Methods of treating b2-bradykinin receptor mediated angioedema in a subject by administering a composition containing a 8-(heteroarylmethoxy)quinolone compound, a 8-(arylmethoxy)quinoline compound, or a salt, a stereoisomer, a hydrate, or a solvate thereof. Oral formulations containing a 8-(heteroarylmethoxy)quinolone compound, a 8-(arylmethoxy)quinoline compound, or a salt, a stereoisomer, a hydrate, or a solvate thereof for the treatment of b2-bradykinin receptor mediated angioedema.
Shire Human Genetic Therapies, Inc.


02/04/16
20160030414 

Benzoquinoline inhibitors of vmat 2


The present invention relates to new benzoquinolone inhibitors of vmat2, pharmaceutical compositions thereof, and methods of use thereof.. .
Auspex Pharmaceuticals, Inc.


01/28/16
20160022675 

Processes for preparing tetrahydroisoquinolines


Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and compositions comprising the tetrahydroisoquinolines and other compounds, e.g, intermediates and by-products of the processes described herein. Pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression are also disclosed..
Bristol-myers Squibb Company


01/21/16
20160016954 

Tricyclic quinoline and quinoxaline derivatives


The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-ht2c receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-ht2c receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-ht2c receptor.. .
Abbvie Deutschland Gmbh & Co. Kg


01/21/16
20160016951 

Novel naphthyridines and isoquinolines and their use as cdk8/19 inhibitors


The present invention relates to naphthyridine and isoquinoline compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of cdk8/19, and for the treatment of cdk8/19-related disorders.. .
Cancer Research Technology, Ltd.


01/21/16
20160016933 

Isoquinolines as potassium ion channel inhibitors


A compound of formula (i) (i) wherein a, r1, r1a, r3 and r24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, ikur-associated disorders, and other disorders mediated by ion channel function..
Bristol-myers Squibb Company


01/21/16
20160016908 

2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors


The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy.. .
Glaxosmithkline Intellectual Property (no.2) Limited




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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