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 Anthropod repellent chemicals patent thumbnailAnthropod repellent chemicals
Compositions and methods for repelling arthropods. The compositions include a carrier and an arthropod repelling compound, which can be a compound discovered by a novel and complex cheminformatic process to demonstrate repellency behavior across a broad spectrum of arthropods.
The Regents Of The University Of California


 Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline patent thumbnailAryl- 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..

 Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde 10a) patent thumbnailSubstituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde 10a)
Or a pharmaceutically acceptable salt thereof, wherein r′, r1 through r7 and ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (pde10a) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type ii diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases..

 Organic electroluminescent materials and devices patent thumbnailOrganic electroluminescent materials and devices
Novel ligands for metal complexes, where the ligands contain fused carbo or heterocycles on the quinoline building block are disclosed. More extended aromaticity within the molecule allows red shift when the molecules are used as light emitting dopants in organic light emitting diodes/devices..
Universal Display Corporation


 Tetrahydroquinoline compositions as bet bromodomain inhibitors patent thumbnailTetrahydroquinoline compositions as bet bromodomain inhibitors
Wherein w, x, y, z, r1, r2, r5, and r8 are as described herein.. .

 Aminoisoquinoline derivatives as protein kinase inhibitors patent thumbnailAminoisoquinoline derivatives as protein kinase inhibitors
The present invention provides novel aminoisoquinoline compounds as defined in the specification, compositions thereof use of these compounds as protein kinase inhibitors and as therapeutic agents for treatment of raf kinase, in particular brafv600e kinase, related diseases or disorders, such as cancers. In addition, the invention also includes methods and processes for preparing these novel aminoisoquinoline compounds..
Eternity Bioscience Inc.


 Injectable pharmaceutical compositions of an anthracenedione derivative with anti-tumoral activity patent thumbnailInjectable pharmaceutical compositions of an anthracenedione derivative with anti-tumoral activity
Injectable pharmaceutical compositions containing 6,9-bis[(2-aminoethyl)amino]benzo[g]isoquinoline-5,10-dione dimaleate as active ingredient in the form of a lyophilised powder with a carrier selected from lactose and dextran, mixed with sodium chloride.. .
Cti Biopharma Corp.


 H3 receptor antagonist for use in the treatment of alzheimer's disease patent thumbnailH3 receptor antagonist for use in the treatment of alzheimer's disease
The disclosure relates to the compound 2-(cyclohexylmethyl)-n-{2-[(2s)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide or a pharmaceutically acceptable salt thereof, intended for the treatment of alzheimer's disease and other types of dementia.. .
Sanofi


 Tetrahydroquinoline compositions as bet bromodomain inhibitors patent thumbnailTetrahydroquinoline compositions as bet bromodomain inhibitors
Wherein w, x, y, z, r1, r2, r5, and r8 are as described herein.. .

 Benzylisoquinoline alkaloid (bia) precursor producing microbes, and methods of making and using the same patent thumbnailBenzylisoquinoline alkaloid (bia) precursor producing microbes, and methods of making and using the same
Host cells that are engineered to produce benzylisoquinoline alkaloid (bias) precursors, such as norcoclaurine (nc) and norlaudanosoline (nl), are provided. The host cells may have one or more engineered modifications selected from: a feedback inhibition alleviating mutation in a enzyme gene; a transcriptional modulation modification of a biosynthetic enzyme gene; an inactivating mutation in an enzyme; and a heterologous coding sequence.
The Board Of Trustees Of The Leland Stanford Junior University


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.
Aerie Pharmaceuticals, Inc.


Isoquinoline compounds


Described herein are compounds of formula (i) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.. .
Gilead Sciences, Inc.


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.. .
Auspex Pharmaceuticals, Inc.


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.
Purdue Research Foundation


Novel pyridyloxyacetyl tetrahydroisoquinoline compounds useful as nampt inhibitors


The present invention provides novel pyridyloxyacetyl tetrahydroisoquinoline compounds that inhibit nampt and may be useful in the treatment of cancer.. .
Eli Lilly And Company


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.. .
Vertex Pharmaceuticals Incorporated


Process for preparing quinoline derivatives


(c) coupling a compound of formula a with an amine of formula b to form a compound of formula 1.. .

Heterocyclic compound, light-emitting element, light-emitting device, electronic device, and lighting device


Provided is a novel heterocyclic compound which can be used as a host material for dispersing a light-emitting material in a light-emitting layer of a light-emitting element. Further provided is a light-emitting element which is driven at a low voltage and has high current efficiency.
Semiconductor Energy Laboratory Co., Ltd.


4-amino-imidazoquinoline compounds


Wherein r1 to r4 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are tlr agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer or infectious diseases..

Formulations 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.. .
Auspex Pharmaceuticals, Inc.


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.


Novel substituted quinoline compounds as s-nitrosoglutathione reductase inhibitors


The present invention is directed to novel quinoline compounds useful as s-nitrosoglutathione reductase (gsnor) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.. .
Nivalis Therapeutics, Inc.


Compounds and use for treating cancer


The present invention relates to certain 2,4-disubstituted quinoline derivatives, to their therapy, as well as to pharmaceutical compositions comprising said compounds. More specifically the invention relates to certain 2,4-disubstituted quinoline derivatives or pharmaceutical compositions comprising said compounds for the treatment of cancers characterized by overactive ras and/or rac or signalling pathway..
Glionova Ab


Triarylamine-substituted benzo[h]quinoline-derivatives as materials for electronic devices


The invention relates to a heteroaryl compound according to formula (i) and to the use thereof in electronic devices.. .
Merck Patent Gmbh


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.


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


Composition 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


Substituted 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


Organic 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.

Novel quinoline -substituted compound


The present invention provides a compound represented by formula (i) below, or a salt thereof.. .

Isoindoline 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.. .

Process 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.


Cyanoquinoline derivatives


Wherein r1, r2, r3 and r4 are each as defined in the present application.. .

Substituted 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..

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.

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.. .

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.


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.


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.


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


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.


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


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..

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.

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.


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.

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.. .

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.


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.


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.


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


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


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


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.


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.


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..

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


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.


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.


Quinoline inhibitor of the macrophage stimulating 1 receptor mstr1


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

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.

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


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)


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..

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.

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..

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..

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.. .

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


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.. .

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


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


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..

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.. .

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


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..

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.


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.. .

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.. .

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.. .

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.. .

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.




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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