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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
08/27/15
20150239845 
 Quinoline derivatives useful as cb-1 inverse agonists patent thumbnailnew patent Quinoline derivatives useful as cb-1 inverse agonists
The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the cb-1 receptor; more particularly, in the treatment of disorders and conditions responsive to inverse agonism of the cb-1 receptor. For example, the compounds of the present invention are useful in the treatment of metabolic disorders..
Janssen Pharmaceutica Nv


08/27/15
20150239844 
 Quinoline derivatives useful as cb-1 inverse agonists patent thumbnailnew patent Quinoline derivatives useful as cb-1 inverse agonists
The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the cb-1 receptor; more particularly, in the treatment of disorders and conditions responsive to inverse agonism of the cb-1 receptor. For example, the compounds of the present invention are useful in the treatment of metabolic disorders..
Janssen Pharmaceutica Nv


08/27/15
20150238488 
 Drug composition for treating tumors and application thereof patent thumbnailnew patent Drug composition for treating tumors and application thereof
The present invention belongs to the field of medicine and pharmaceutical chemistry, specifically relates to novel antitumor pharmaceutical combinations, and particularly relates to pharmaceutical combinations of bisbenzylisoquinoline alkaloids (e.g. Berbamine and tetrandrine) and imatinib mesylates and their use in treating tumors..
Hangzhou Bensheng Pharmaceutical Co., Ltd.


08/20/15
20150232445 
 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.. .

08/20/15
20150231237 
 Methods and products for treating proliferative diseases patent thumbnailMethods and products for treating proliferative diseases
Methods and products for treating proliferative diseases, and wounds, using as a pharmacon an autophagy inhibitor, a glycolytic inhibitor, and/or an agent able to alter cellular production of reactive oxygen, or combination thereof, optionally in combination with one or more chemotherapeutic agents. In some embodiments, the invention combines a 4-aminoquinoline, exemplified by chloroquine, with a glycolytic inhibitor, exemplified by 2-deoxy-d-glucose and anti-vegf antibodies.
The Regents Of The University Of Colorado, A Body Corporate


08/20/15
20150231128 
 Pharmaceutical compositions comprising 7-(1h-imidazol-4-ylmethyl)-5,6,7,8-tetrahydro-quinoline for treating skin diseases and conditions patent thumbnailPharmaceutical 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.


08/13/15
20150225348 
 Process for preparing (1s)-1-phenyl-3,4-dihydro-2(1h)-isoquinoline-carboxylate patent thumbnailProcess for preparing (1s)-1-phenyl-3,4-dihydro-2(1h)-isoquinoline-carboxylate
In formula i and ii, r is an alkyl or a substituted alkyl; lg is a leaving group.. .

08/06/15
20150218207 
 N-substituted indenoisoquinolines and syntheses thereof patent thumbnailN-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.
The Government Of The United States Of America As Represented By The Secretary Of The Department Of


08/06/15
20150218162 
 Substituted imidazoquinolines, imidazopyridines, and imidazonaphthyridines patent thumbnailSubstituted imidazoquinolines, imidazopyridines, and imidazonaphthyridines
Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.. .
3m Innovative Properties Company


08/06/15
20150218102 
 6-heteroaryloxy- or 6-aryloxy-quinoline-2-carboxamides and  use patent thumbnail6-heteroaryloxy- or 6-aryloxy-quinoline-2-carboxamides and use
And pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein r1, r2, and r3 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by voltage-gated sodium channels, e.g., nav1.7 and/or nav1.8. Methods for making the compounds are disclosed.

08/06/15
20150216866 

Substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors


The present invention provides a method for treating or preventing a condition or disease in a human or an animal subject wherein the condition or disease is associated with lipoprotein metabolism, the method comprising administering to the subject a composition comprising benzylamine compounds.. .
Dr. Reddy's Laboratories Ltd.


08/06/15
20150216181 

Pesticide having an insecticide, acaricide and nematicide action based on isoquinoline alkaloids and flavonoids


The present invention relates to a pesticide having an insecticide, acaricide and nematicide action obtained from plant extracts that have important synergic interactions in their pesticide activity, the characteristics of which are efficient control of insects, mites and nematodes; low toxicity for mammals and low persistence in the environment. This pesticide is a composition based on plant extracts which is characterized because it is constituted by: isoquinoline alkaloids and their derivatives (0.1-20%) and flavonoids and their glycosylated derivatives (0.001-10%).
Promotora Tecnica Industrial, S.a. De C.v.


07/30/15
20150210711 

Hexahydrodibenzo[a,g]quinolizine compound, preparation method thereof, pharmaceutical composition and use thereof


The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (i) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor.
Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences


07/30/15
20150210644 

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.. .
Northwestern University


07/30/15
20150209364 

Method for treating epidermoid carcinoma


Disclosed herein is a method for enhancing the susceptibility of a subject having epidermoid carcinoma toward a tyrosine kinase inhibitor. The method includes administering to the subject an effective amount of a targeted therapy sensitizer and an effective amount of gefitinib.
Johnpro Biotech Inc.


07/30/15
20150209351 

Alpha adrenergic receptor modulators


Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure.
Allergan, Inc.


07/23/15
20150203491 

Imidazo[4,5-c]quinolines as dna-pk inhibitors


The invention relates to compounds of the formulae (i) and (ii) in which r1, r2, r3, r4, r5, r8, x and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (i) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation.
Merck Patent Gesellschaft Mit Beschrankter Haftung


07/23/15
20150203488 

Pyrroloquinoline quinone tetraalkali salt and crystal thereof, methods for producing these, and composition


Wherein m is each independently one selected from the group consisting of li, k, na, rb and cs.. .

07/16/15
20150197735 

7,11-methanocycloocta [b] quinoline derivative as highly functionalizable acetylcholinesterase inhibitors


A method for preparing such compounds and their use for treating neurological diseases in which the level of acetylcholine is affected such as alzheimer's disease.. .

07/09/15
20150191494 

Tetrahydroisoquinolines and intermediates therefor


Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4s)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form..
Albany Molecular Research, Inc.


07/09/15
20150191450 

Isoquinoline-5-carboxamide derivative having inhibitory activity for protein kinase


A compound selected from the group consisting of an isoquinoline-5-carboxamide derivative of formula (i), a pharmaceutically acceptable salt, an isomer, a hydrate and a solvate thereof is effective for the prevention or treatment of diseases associated with abnormal cell growth, which are caused by abnormal activation of a protein kinases.. .
Hanmi Pharm. Co., Ltd.


07/02/15
20150183764 

Process for the manufacture of (e)-4-n,n-dialkylamino crotonic acid in hx salt form and use thereof for synthesis of egfr tyrosine kinase inhibitors


Wherein r1 and r2 independently denote c1-3-alkyl groups and x− denotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of egfr tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt i and activated derivatives thereof as intermediates.. .

06/25/15
20150175586 

Therapeutic agents for ocular hypertension


This invention provides well defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds for treating glaucoma or ocular hypertension.. .
Allergan, Inc.


06/25/15
20150175550 

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.


06/25/15
20150174117 

4-oxoquinoline compound and use thereof as pharmaceutical agent


Wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has hiv integrase inhibitory action and is useful as an anti-hiv agent for the prophylaxis or therapy of aids.

06/18/15
20150168374 

Senescence tracers


The instant invention relates to novel compounds useful for visualizing cell senescence, their preparation and use. In particular, this invention relates to novel fucose and aminoquinoline derivatives useful as senescence traces and their preparation..
Eberhard Karls Universitaet Tuebingen Medizinische Fakultaet


06/11/15
20150158895 

Substituted 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..

06/11/15
20150158816 

Crystal form of quinoline compound and process for its production


The water content is adjusted to a level of from 5 to 15%, and the crystal form is controlled to be crystal form a, thereby to obtain a drug substance excellent in stability.. .

06/11/15
20150157624 

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..

06/04/15
20150152099 

Methods of manufacturing benzoquinoline compounds


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


06/04/15
20150150869 

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


The present invention relates to compositions and methods for cancer treatment comprising compounds of formulae i, ii, and iii. In some aspects, the invention relates to the treatment of b-cell lymphoma or other hematopoietic cancers.
Eutropics Pharmaceuticals, Inc.


05/28/15
20150148377 

Quinoline derivatives


The invention relates to quinoline compounds of the formula (i) and/or pharmaceutically acceptable salts and/or solvates thereof, wherein y, w, u, q, r1, r5 r7 and r30 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the pi3k enzymes..
Novartis Ag


05/28/15
20150148376 

Novel 5-aminotetrahydroquinoline-2-carboxylic acids and their use


The present application relates to novel 5-amino-5,6,7,8-tetrahydroquinoline-2-carboxylic acids, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular and cardiopulmonary disorders.. .
Bayer Pharma Aktiengesellschaft


05/28/15
20150148370 

Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase i inhibitors


The invention described herein pertains to substituted indenoisoquinoline compounds as described herein, wherein ra, rd, w, x and y are defined herein, pharmaceutical compositions and formulations comprising the indenoisoquinoline compounds, their synthesis, and methods for their use in the treatment and/or prevention of cancer.. .
Purdue Research Foundation


05/28/15
20150148344 

Quinoline derivatives as bromodomain inhibitors


Wherein r1, r2, r3, r4, r7, w, x, and z are as described herein.. .

05/28/15
20150148292 

Bone morphogenetic protein pathway activation, compositions for ossification, and methods related thereto


The disclosure relates to compounds and compositions for bone formation, fracture treatment, bone grafting, bone fusion, cartilage maintenance and repair, and methods related thereto. In certain embodiments, the disclosure relates to compositions comprising one or more compound(s) disclosed herein, such as 2-(2-methoxybenzylidene)-1-indan-one; n-(4-arsonophenyl)glycine; 1,2-benzenedicarboxylic acid, 1-(1-methylheptyl)ester; (4′-hydroxybiphenyl-4-yl) (phenyl)methanone; 2,2-dimethylchroman-6-carboxylic acid, (4,7-dihydroxy-8-methyl-2-oxo-2h-chromen-3-yl)amide; ethyl 2-((4-chlorophenyl)thio)-1,3-benzothiazol-6-yl carbamate; ethyl (2-(azepan-1-yl)benzo[d]thiazol-6-yl) carbamate; porfiromycin; 1,3-benzodioxol-5-yl-[4-(3,4,5-trimethoxybenzoyl)-3-furyl]methanone; tricinolone acetophenonide; 2,4-bis(3,4-dimethoxyphenyl)-4h-pyrano[3,2-c]chromen-5-one; methyl 5-fluoro-4-methoxy-2,6-dioxohexahydro-5-pyrimidine carboxylate; 5-(naphthalen-1-yl)-1-phenyl-1h-tetrazole; 5-(2-phenylquinolin-4-yl)-1,3,4-oxadiazol-2-ol; n-[2,4,5-trimethyl-4-(trichloromethyl)cyclohexa-2,5-dien-1-ylidene]hydroxylamine; 4-benzoyl-3,4-dihydro-benzo[f]quinoline-3-carbonitrile; 2-nitro-3-phenylspiro[cyclopropane-1,9′-fluorene]; 3-[4-(furan-2-ylmethyl)-5-sulfanylidene-1,2,4-dithiazolidin-3-ylidene]-1,1-dimethyl-thiourea; (6-acetamido-7-methyl-5,8-dioxo-2,3-dihydro-1h-pyrrolo[1,2-a]benzimidazol-3-yl)2-methoxyacetate; 5-iodo-1h-indole-2,3-dione; 4,5-dihydro-1,2,9,10-tetramethoxy dibenzo[de,g]quinoline-6-carboxylic acid, ethyl ester; [2,6-bis(2,4-dimethylphenyl)-4-(2-methoxyacetyl)oxy-phenyl]2-methoxyacetate; 5,11-dimethyl-2-(2-piperidin-1-ylethyl)-6h-pyrido[4,3-b]carbazol-2-ium-9-ol; 2-[3-[[4-[(3-nitroacridin-9-yl)amino]phenyl]sulfamoyl]propyl]guanidine; 1-[[2-(dimethylamino)ethyl]amino]-7-hydroxy-4-methyl-9h-thioxanthen-9-one; 5-amino-1h-1,2,4-triazole-3-carboxylic acid, methyl ester; methyl n-cyano-n′-prop-2-en-1-ylcarbamimidothioate; 5,7-dinitro-8-quinolinol; 5-nitrosoquinolin-8-ol; cantharidin; 1,7-diaminoacridine; 3-methyl-3-(1-naphthyl)-2-benzofuran-1(3h)-one; dichlorolapachol; lycobetaine; 6-(1-aziridinyl)-2,3-dihydro-3-(propionyl)-7-methyl-1h-pyrrolo[1,8]-dione; 4-nitroestrone 3-methyl ether; 5,11-dimethyl-6h-pyrido[4,3-b]carbazole-1-carboxamide hydrochloride; 5-methoxysterigmatocysin; (6-acetamido-7-methyl-5,8-dioxo-2,3-dihydro-1h-pyrrolo[1,2-a]benzimidazol-3-yl)2-methoxyacetate; horminon; 7′,8′-dimethyl-2′-oxo-4′,4a′,6a′,7′-tetrahydro-2′h-spiro[oxirane-2,1′-pentaleno[1,6a-c]pyran]-5′-carboxylate; nybomycin acetate; 5h-[1,6]indeno[1,2-c]isoquinoline-5,12-dione; 2,3-dimethoxy-6-methyl-nitidine; iproplatin; 3-[(deoxyhexosyl)oxy]-2-(3,4-di-hydroxyphenyl)-6,8-dihdroxy-4h-1-benzopyran-4-one; 2-o-benzyl 8-o-methyl 3-(4-methylphenyl)sulfonyl-4,5-dioxo-6h-pyrrolo[3,2-e]indole-2,8-dicarboxylate; 6-bromo-5,8-dihydroxy-7-[4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl]naphthalene-1,4-dione; 5-methylbenzo[c]phenanthridin-5-ium-2,3,8,9-tetrol; (6-acetyl-4-oxo-1,3-diphenyl-2-sulfanylidenethieno[2,3-d]pyrimidin-5-yl)-2,4-dichlorobenzoate; n—[c-[4-[bis(2-cyanoethyl)amino]-2-methylphenyl]-n-(4-methylanilino)carbonimidoyl]imino-4-methylbenzamide; gelcohol; curcumin; tirandamycin; noscapine; aristolochic acid; himbacine; fumagillin; fumitremorgin c; physalin b; derivatives, or salt thereof, for use in bone growth processes.
Emory University


05/21/15
20150141652 

Process for preparing 2-[(2e)-2-fluoro-2-(3-piperidinylidene)ethyl]-1h-isoindole-1,3(2h)-dione


The present invention relates to an improved process for preparing 2-[(2e)-2-fluoro-2-(3-piperidinylidene)ethyl]-1h-isoindole-1,3(2h)-dione, or a salt thereof, which is an intermediate in the synthesis route of the antibacterial compound 7-[(3e)-3-(2-amino-1-fluoroethylidene)-1-piperidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo 3-quinolinecarboxylic acid.. .
Janssen Pharmaceutica Nv


05/21/15
20150141444 

N-methyl tetrahydroquinoline m1 receptor positive allosteric modulators


The present invention is directed to n-methyl tetrahydroquinoline 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 compositions 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.


05/21/15
20150141431 

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..

05/21/15
20150141415 

Methionine aminopeptidase inhibitors for treating infectious diseases


The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof..

05/14/15
20150133666 

Tritoqualine for use in the treatment of cystic fibrosis


The present invention relates to the use of a histamine h4 agonist molecule, the enantiomers of the (amino-7 triethoxy-4,5,6 oxo-1 dihydro-1,3 isobenzofurannyl-3)-1methoxy-8 methyl-2 methylenedioxy-6,7 tetrahydro-,2,3,4 isoquinoline or tritoqualine for the treatment of respiratory impairment caused by cystic fibrosis and the reduction and prevention of bronchial superinfections.. .

05/14/15
20150133450 

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


The present invention relates to compositions and methods for cancer treatment comprising compounds of formulae i, ii, and iii. In some aspects, the invention relates to the treatment of b-cell lymphoma or other hematopoietic cancers.

05/14/15
20150133445 

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..

05/07/15
20150126743 

Process for the preparation of pyrido [2,1-a] isoquinoline derivatives comprising optical resolution of an enamine


Wherein rco2− is the conjugate base of the resolving agent.. .

05/07/15
20150126550 

Pharmaceutical uses of 6-amino quinazoline or 3-cyano quinoline derivatives


Pharmaceutical uses of 6-amino quinazoline or 3-cyano quinoline derivatives are disclosed. Specifically, the 6-amino quinazoline or 3-cyano quinoline derivatives presented by general formula (i), or tautomers, enantiomers, diastereomers, racemates or pharmaceutically acceptable salts thereof, or metabolites, metabolic precursors or prodrugs thereof, are protein kinase inhibitors, in which each substitutent group of general formula (i) is as defined in the specification..
Shanghai Hengrui Pharmaceutical Co., Ltd.


05/07/15
20150126537 

Bicyclic compounds as kinases inhibitors


The present invention is directed to novel bicyclic compounds, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are useful for the treatment of protein kinases mediated diseases and conditions.
Hangzhouderenyucheng Biotechnology Ltd


05/07/15
20150126517 

Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof


Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders.
Albany Molecular Research, Inc.


04/30/15
20150119419 

6-aminoisoquinoline compounds


6-amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided.
Aerie Pharmaceuticals, Inc.


04/23/15
20150112072 

Process of preparing solifenacin or salt thereof, and novel intermediate used in the process


Disclosed herein is a method of preparing solifenacin or a salt thereof, including the steps of: (a) reacting (r)-quinuclidinol with bis(pentafluorophenyl)carbonate in an organic solvent to prepare a solifenacin intermediate, (3r)-1-azabicyclo[2,2,2]oct-3-yl pentafluorophenylcarbonate, and (b) reacting the solifenacin intermediate with (1s)-1-phenyl-1,2,3,4-tetrahydroisoquinoline in an organic solvent to prepare solifenacin. The method is advantageous in that high-purity solifenacin or a salt thereof can be simply and efficiently prepared with high yield using a novel intermediate..
Kyung Dong Pharm. Co., Ltd.


04/23/15
20150111884 

Tricyclic tetrahydroquinoline antibacterial agents


Methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical composition.. .

04/23/15
20150111867 

Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy


The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquin oline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are glyt1 inhibitors..

04/16/15
20150105422 

Salts and solvates of a tetrahydroisoquinoline derivative


(s)-2-(diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described..
Spinifex Pharmaceuticals Pty Ltd


04/16/15
20150105370 

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.. .
Eisai R&d Management Co., Ltd.


04/16/15
20150104482 

Use of cpg oligonucleotides co-formulated with an antibiotic to accelerate wound healing


Pharmaceutical compositions are provided that include an antibiotics, but that include ingredients that counteract the effect of that antibiotic on wound healing, without altering the bactericidal properties of the antibiotic. These pharmaceutical compositions include an effective amount of 1) an imidazoquinoline having toll-like receptor 7 (tlr7) ligand activity, 2) an immunostimulatory k-type cpg oligodeoxynucleotide (odn) comprising an unmethylated cpg motif, 3) an antibiotic, and 4) a surfactant, wherein the composition is formulated for topical administration.
The United States Of America, As Represented By The Secretary, Department Of Health And Human Serv


04/02/15
20150094475 

Preparation of pyridonecarboxylic acid antibacterials


A process for making 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, and therapeutically acceptable salts thereof, and intermediates used in the process are disclosed.. .
Abbvie, Inc.


04/02/15
20150094334 

8-hydroxy quinoline derivatives


Or pharmaceutically acceptable salts, hydrates, or solvates thereof.. .

04/02/15
20150094333 

Amino-quinolines as kinase inhibitors


Wherein r1, r2r3, r4 and r5 are as defined herein, and methods of making and using the same.. .

03/26/15
20150087824 

Novel production isoquinoline derivatives and salts thereof


The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (i) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (i) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (iii) or a salt thereof with a compound represented by formula (ii) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base..
Kowa Co., Ltd.


03/26/15
20150083570 

Method of obtaining a high quality coke from low rank coal liquefaction


The present disclosure provides methods and systems for coal liquefaction and obtaining a high quality coke from a low rank coal extract. A method of obtaining a high quality coke from a low rank coal extract may include exposing coal to a hydrogenated vegetable oil in the presence of a coal-derived solvent to form a slurry, elevating the temperature of the slurry to facilitate liquefying the coal and liberating a volatile matter, separating the insoluble components from the slurry to obtain a de-ashed coal extract that is quinoline insoluble-free, distilling the coal extract under vacuum to obtain a pitch with a suitable softening point, and coking the pitch to obtain a coke.
West Virginia University


03/19/15
20150080431 

Pharmaceutical compositions for the treatment of cftr-mediated disorders


The present invention relates to the use of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (compound 1), solids forms, and pharmaceutical compositions thereof for the treatment of cftr-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. The present invention also relates to the use of compound 1 in combination with 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (compound 2), and compound 1 in combination with (s)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl)cyclopropanecarboxamide (compound 3), for the treatment of cftr-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations.
Vertex Pharmaceuticals Incorporated


03/19/15
20150080429 

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.. .
N30 Pharmaceuticals, Inc.


03/19/15
20150080427 

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.


03/19/15
20150080426 

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.


03/19/15
20150076031 

Process for producing mesophase pitch by hydrogenation of high-temperature coal tar


A process for producing mesophase pitch from high-temperature coal tar comprises: removing salts and quinoline insoluble fraction from a high-temperature coal tar to obtain a decant oil; using the decant oil as a hydrogenation feedstock, or pre-distilling the decant oil to obtain a residue with a boiling point higher than 230 and formulating the residue into a hydrogenation feedstock; catalytic hydrorefining the hydrogenation feedstock to obtain a hydrofined oil; distilling the hydrofined oil to obtain hydrogenated pitch; and subjecting the hydrogenated pitch to the thermal polymerization to obtain the mesophase pitch. The process has features such as an easily controllable degree of hydrogenation, complete removal of impurities, good raw material flowability, not tending to form the carbon deposition and the coking during the process, and not tending to jam the reactor.
Dalian University Of Technology


03/12/15
20150073151 

Supercritical fluid extraction of bis-benzyl isoquinolines


An improved process for obtaining at least one bis-benzyl isoquinoline alkaloid from botanical material involves contacting the botanical material with a supercritical fluid having as a major component one or more aliphatic hydrocarbon compounds, such as alkanes, alkenes, cyclic aliphatic hydrocarbons, or a combination of these compounds.. .
Cba Pharma, Inc.


03/12/15
20150069226 

Mass spectrometry phosphorylated peptides and sugar chains


The present invention provides a method for mass spectrometry of phosphorylated peptides or sugar chains, which suppresses the desorption of an unstable site during ionization and achieves high sensitivity (i.e., detects molecular-related ions at a high ionic strength and at a relatively higher ionic strength than other ion species derived from the desorption of an unstable site). A method for mass spectrometry of phosphorylated peptides or sugar chains, the method comprising using, as a liquid matrix, an ionic liquid comprising a 3-aminoquinoline ion and a p-coumaric acid ion.
Shimadzu Corporation


03/05/15
20150065502 

Antibacterial quinoline derivatives


A pharmaceutically acceptable salt thereof, a n-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection.

03/05/15
20150065499 

3-aminothieno[3,2-c]quinoline derivatives, methods of preparation and uses


The present invention relates to compounds according to formula i: and salts thereof, wherein r1, r2, r3, r4, r5, r6, r7, x, and y are as defined herein. Methods for preparing compounds of formula i are also provided.
Temple University - Of The Commonwealth System Of Higher Education


03/05/15
20150065489 

Substituted quinolines and their use as medicaments


R1 and r2 are defined herein, the processing of making and using the same.. .

02/26/15
20150057312 

Substituted quinolines as bruton's tyrosine kinases inhibitors


The present invention is directed to novel quinolines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are useful for the treatment of protein kinases mediated diseases and conditions.
Hangzhouderenyucheng Biotechnology Ltd


02/26/15
20150057311 

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)


02/26/15
20150056137 

Caspase-triggered nano-aggregation probes and methods of use


Provided is an activatable probe that undergoes intramolecular cyclization and subsequent aggregation in apoptotic tumor cells upon peptidase-initiated, and most advantageously caspase-3, activation. These caspase-sensitive nano-aggregation probes (c-snafs) are generally biocompatible, possess nir spectral properties or may serve as pet or mri imaging agents, and have a mechanism of target-mediated nanostructure self-assembly amenable to in vivo use.
The Board Of Trustees Of The Leland Stanford Junior University


02/19/15
20150051419 

Intermediate compounds and processes for the preparation of quinoline derivatives such as laquinimod sodium


The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (laquinimod sodium). The present invention further relates to intermediates formed in such processes..
Mapi Pharma Ltd.


02/19/15
20150051244 

Antibacterial quinoline derivatives


The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds..



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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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