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Isoquinolin patents



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


Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde 10a)

Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde 10a)

Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde 10a)

Substituted tetrahydroisoquinoline compounds as factor xia inhibitors

Date/App# patent app List of recent Isoquinolin-related patents
06/25/15
20150175550
 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.
06/18/15
20150166474
 Ionically bonded salt having reactive group  and thermoplastic resin composition containing same patent thumbnailIonically bonded salt having reactive group and thermoplastic resin composition containing same
In chemical formulas (1) and (2) above, r1 and r2 each independently represent a substituted or unsubstituted linear, branched, or cyclic alkyl group having from 1 to 30 carbon atoms, a substituted or unsubstituted aryl group having from 6 to 30 carbon atoms, or a substituted or unsubstituted arylalkyl group having from 7 to 31 carbon atoms, a is a linear or branched alkylene group having from 2 to 4 carbon atoms, n represents an integer of 0 to 50, and q1 and q2 each independently represent at least one kind selected from the group consisting of an ammonium ion having an ethylenically unsaturated bond, an imidazolium ion having an ethylenically unsaturated bond, a pyridinium ion having an ethylenically unsaturated bond, a pyrrolidinium ion having an ethylenically unsaturated bond, a pyrrolinium ion having an ethylenically unsaturated bond, a piperidinium ion having an ethylenically unsaturated bond, a pyrazinium ion having an ethylenically unsaturated bond, a pyrimidinium ion having an ethylenically unsaturated bond, a triazolium ion having an ethylenically unsaturated bond, a triazinium ion having an ethylenically unsaturated bond, a quinolinium ion having an ethylenically unsaturated bond, an isoquinolinium ion having an ethylenically unsaturated bond, an indolinium ion having an ethylenically unsaturated bond, a quinoxalinium ion having an ethylenically unsaturated bond, a piperazinium ion having an ethylenically unsaturated bond, an oxazolinium ion having an ethylenically unsaturated bond, a thiazolinium ion having an ethylenically unsaturated bond, and a morpholinium ion having an ethylenically unsaturated bond.. .
06/11/15
20150158895
 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..
06/11/15
20150157624
 Substituted tetrahydroisoquinoline compounds as factor xia inhibitors patent thumbnailSubstituted 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..
05/28/15
20150148370
 Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase i inhibitors patent thumbnailAlcohol-, 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
20150148292
 Bone morphogenetic protein pathway activation, compositions for ossification, and methods related thereto patent thumbnailBone 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
05/28/15
20150144281
 Method of cleaning residue from a surface using a high efficiency disposable cellulosic wiper patent thumbnailMethod of cleaning residue from a surface using a high efficiency disposable cellulosic wiper
An absorbent paper sheet for tissue or towel includes an amount by weight of pulp-derived papermaking fibers, and an amount by weight of fibrillated regenerated cellulosic microfibers prepared from a cellulosic dope of dissolved cellulose comprising a solvent selected from tertiary amine n-oxides, cellulose dissolving imidazolium salts, cellulose dissolving pyridinium salts, cellulose dissolving pyridazinium salts, cellulose dissolving pyrimidinium salts, cellulose dissolving pyrazinium salts, cellulose dissolving pyrazolium salts, cellulose dissolving oxazolium salts, cellulose dissolving 1,2,3-triazolium salts, cellulose dissolving 1,2,4-triazolium salts, cellulose dissolving thiazolium salts, cellulose dissolving piperidinium salts, cellulose dissolving pyrrolidinium salts, cellulose dissolving quinolinium salts, and cellulose dissolving isoquinolinium salts.. .
Georgia-pacific Consumer Products Lp
05/21/15
20150141431
 Pyrazinoisoquinoline compounds patent thumbnailPyrazinoisoquinoline 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..
05/14/15
20150133666
 Tritoqualine for use in the treatment of cystic fibrosis patent thumbnailTritoqualine 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
20150133445
 Synthesis and use of dual tyrosyl-dna phosphodiesterase i (tdp1) - topoisomerase i (top1) inhibitors patent thumbnailSynthesis 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..
05/14/15
20150133443

Thiazolyl- and oxazolyl-isoquinolinones and methods for using them


The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(adp-ribose) polymerase (parp). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders..
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
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.
04/30/15
20150119317

Oral solid dosage formulation of 1,1-dimethylethyl [(1s)-1-carbamoyl)pyrrolidin-1-yl]carbonyl}-2,2-dimethylpropyl]carbamate


The present invention is directed to an oral solid dosage formulation of asunaprevir, 1,1-dimethylethyl[(1s)-1-{[(2s,4r)-4-(7-chloro-4methoxyisoquinolin-1-yloxy)-2-({(1r,2s)-1-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl}carbamoyl)pyrrolidin-1-yl]carbonyl}-2,2-dimethylpropyl]carbamate, and to methods of using the formulation in the treatment and/or inhibition of the hepatitis c virus and infections caused thereby.. .
Bristol-myers Squibb Company
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.
04/16/15
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
04/09/15
20150099732

3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use


The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2h-isoquinolin-1-one compounds that, inter alia, inhibit parp (e.g., parp1, tnks1, tnks2, etc.) and/or wnt signalling.
Institute Of Cancer Research: Royal Cancer Hospital (the)
04/02/15
20150090639

Halogen-free ionic liquids in naphtha desulfurization and their recovery


Ionic liquids of the general formula c+a− where c+ represents an organic cation, specifically, but not limited to the imidazolium, pyridinium, isoquinolinium, ammonium types, which have aliphatic and aromatic substituents, while a− represents a carboxylate, aromatic and aliphatic anion. The ionic liquids are synthesized under conventional heating or microwave irradiation this invention is also related to the application of ionic liquids to remove sulfur compounds of naphthas through a liquid-liquid extraction and the recovery and reuse of ionic liquids by the application of heat, reduced pressure and washing with solvents..
Instituto Mexicano Del Petroleo
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.
03/12/15
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.
02/05/15
20150038529

Crystalline forms of a prolyl hydroxylase inhibitor


The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.. .
Fibrogen, Inc.
02/05/15
20150038528

4 -hydroxy- isoquinoline compounds as hif hydroxylase inhibitors


The present invention relates to novel compounds of formula (i), and compositions capable of inhibiting phd1 enzyme activity selectively over other isoforms, for example, phd2 and/or phd3 enzymes. The invention also relates to compounds of formula (i) for use in disorders such as muscle degeneration, colitis, ibd, and certain ischemias..
Fibrogen, Inc.
01/29/15
20150031893

An 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.. .
Sanofi
01/29/15
20150031888

Process for the preparation of pyrido[2,1-a] isoquinoline derivatives by catalytic asymmetric hydrogenation of an enamine


Wherein r2, r3, r4 and prot are as defined in the specification.. .
01/29/15
20150031696

Cyanoisoquinoline compounds and methods of use thereof


The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions. The cyanoisoquinoline compounds of the invention have the following structure:.
Fibrogen, Inc.
01/22/15
20150021197

Novel metal complex catalysts and uses thereof


The invention relates to novel metal complexes useful as catalysts in redox reactions (such as, hydrogen (h2) production). In particular, the invention provides novel transition metal (e.g., cobalt (co) or nickel (ni)) complexes, in which the transition metal is coupled with n,n-bis(2-pyridinylmethyl)-2,2′-bipyridine-6-methanamine (dpa-bpy), 6′-((bis(pyridin-2-ylmethyl)amino)methyl)-n,n-dimethyl-2,2′-bipyridin-6-amine (dpa-abpy), n,n-bis((isoquinolin-1-yl)methyl)(6-(pyridin-2-yl)pyridin-2-yl)methanamine (diq-bpy), or a derivative thereof.
University Of Memphis Research Foundation
12/25/14
20140378711

Method for synthesizing 2,7-dimethyl-2,4,6-octatriene-1,8-dialdehyde


Provided in the present invention is a method for synthesizing 2,7-dimethyl-2,4,6-octatriene-1,8-dialdehyde. The synthesis method comprises the following steps: (1) adding acetaldehyde diethyl acetal and ethyl-(1-propenyl)-ether under the effect of a catalyst to produce 1,1,3-triethoxy-2-methyl-butane; (2) pyrolysis synthesizing 1,1,3-triethoxy-2-methyl-butane under the catalytic effects of isoquinoline and p-toluenesulfonic acid to produce 1-methoxy-2-methyl-1,3-butadiene; (3) dissolving 1-methoxy-2-methyl-1,3-butadiene in anhydrous ethanol solvent for synthesis with a phase transfer catalyst, cetyl-trimethyl ammonium bromide, and a chlorinating agent, trichloroisocyanuric acid, to generate 4,4-diethoxy-3-methyl-1-chloro-butene; (4) combining 4,4-diethoxy-3-methyl-1-chloro-butene with a triphenylphosphine salt to produce a phosphonium salt; and (5) condensing the phosphonium salt under the effects of hydrogen peroxide in conjunction with sodium carbonate solution to generate 1,1,8,8-tetramethyl-2,7-dimethyl-2,4,6-octatriene; then hydrolyzing under acidic conditions to synthesize 2,7-dimethyl-2,4,6-octatriene-1,8-dialdehyde.
Zhejiang Medicine Co., Ltd. Xinchang Pharmaceutical Factory
12/25/14
20140378441

Therapeutic agent for ocular fundus disease


Disclosed herein is a prophylactic or therapeutic agent for ocular fundus disease, especially diabetic retinopathy or age-related macular degeneration. The prophylactic or therapeutic agent for ocular fundus disease comprising: (s)-(−)-1-(4-fluoro-5-isoquinolinesulfonyl)-2-methyl-1,4-homopiperazine, a salt thereof, or a solvate thereof, as an active ingredient..
Kowa Company, Ltd.
12/18/14
20140371450

Processes for preparing isoquinolinones and solid forms of isoquinolinones


Polymorphs of chemical compounds that modulate kinase activity, including pi3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including p13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof..
Infinity Pharmaceuticals, Inc.
12/11/14
20140364441

Crystalline forms of (s)-7-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoquinoline and use thereof


Novel [1,2,4]triazolo[1,5-a]pyridinyl-6-yl-substituted tetrahydroisoquinolines are described in the present invention. These compounds and crystalline forms sa1 and n-2 are used in the treatment of various neurological and physiological disorders.
12/04/14
20140357664

3,4-dihydroisoquinolin-2(1h)-yl compounds


The invention provides certain 3,4-dihydroisoquinolin-2(1h)-yl compounds, particularly compounds of formula i, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula i to treat cognitive impairment associated with parkinson's disease or schizophrenia..
12/04/14
20140357652

Rho kinase inhibitors


Disclosed are novel substituted 2h-isoquinolin-1-one and 3h-quinazolin-4-one derivatives useful as inhibitors of rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.. .
11/27/14
20140350257

Process for the preparation of a dpp-iv inhibitor


Wherein r1, r2 and r3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2s,3s,11bs)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-3-yl)-4(s)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form a and form b and to an amorphous form of said compound..
11/20/14
20140343036

Isoquinoline and naphthyridine derivatives


Wherein a, r1 and r2 are as described herein, compositions including the compounds and methods of using the compounds.. .
11/13/14
20140336192

3-phenyl-isoquinolin-1(2h)-one derivatives as parp-1 inhibitors


There are provided substituted 3-phenyl-isoquinolin-1(2h)-one derivatives which selectively inhibit the activity of poly(adp-ribose) polymerase parp-1 with respect to poly(adp-ribose) polymerase parp-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
11/13/14
20140336188

N-substituted indenoisoquinolines and syntheses thereof


N-substituted indenoisoquinoline compounds, and pharmaceutical formulations of n-substituted indenoisoquinoline compounds are described. Also described are processes for preparing n-substituted indenoisoquinoline compounds.
10/16/14
20140309253

Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (pde 10a)


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..
10/09/14
20140302987

Use of substituted isoquinolinones, isoquinolindiones, isoquinolintriones and dihydroisoquinolinones or in each case salts thereof as active agents against abiotic stress in plants


For enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and selected processes for preparing the compounds mentioned above.. .
10/02/14
20140296214

Substituted tetrahydroisoquinoline compounds as factor xia inhibitors


The present invention provides compounds of formula (i): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor xia and/or plasma kallikrein which may be used as medicaments..
09/18/14
20140275161

Combination therapy


Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog.
09/18/14
20140275160

Combination therapy


Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog.
09/18/14
20140275158

Cyclohexyl isoquinolinone compounds


The invention relates to compounds of formula (i): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of mdm2 and/or mdm4, or variants thereof..
09/18/14
20140275135

Salts and solid forms of isoquinolinones and composition comprising and methods of using the same


Solid forms of chemical compounds that modulate kinase activity, including pi3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including pi3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, solid forms thereof, and pharmaceutical compositions thereof..
09/18/14
20140275129

Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone compounds


Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone derivatives represented by formula (i), pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for treating hyperproliferative disorders by administering the compounds are also described.
09/18/14
20140275101

Crystalline form of 6-[(4s)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine


The present disclosure generally relates to a crystalline form of 6-[(4s)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form, as well of methods of using a crystalline form in the treatment of depression and other conditions and methods for obtaining such crystalline form..
09/18/14
20140275065

Substituted 7-azabicyles and their use as orexin receptor modulators


Wherein ring a is phenyl, naphthalenyl, pyridyl, quinolinyl, isoquinolinyl, imidazopyridyl, furanyl, thiazolyl, isoxazolyl, pyrazolyl, imidazothiazolyl, benzimidazolyl, or indazolyl; r1 is h, alkyl, alkoxy, hydroxyalkylene, oh, halo, phenyl, triazolyl, oxazolyl, isoxazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, piperazinyl, pyrazolyl, oxadiazolyl, pyrrolidinyl, thiophenyl, morpholinyl, or dialkylamino; r2 is h, alkyl, alkoxy, hydroxyalkylene, or halo; z is nh, n-alkyl, or o; r5 is pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, quinoxalinyl, pyrazolyl, benzoxazolyl, imidazopyrazinyl, triazolopyrazinyl, optionally substituted with a one or two substituents independently selected from the group consisting of alkyl, alkoxy, or halo; and n is 0 or 1. Methods of making the compounds of formula i are also described.
09/18/14
20140275061

Substituted tetrahydroisoquinoline compounds as factor xia inhibitors


The present invention provides compounds of formula (i): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor xia and/or plasma kallikrein which may be used as medicaments..
09/18/14
20140274960

Substituted tetrahydroisoquinoline compounds as factor xia inhibitors


The present invention provides compounds of formula (i) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor xia and/or plasma kallikrein which may be used as medicaments..
09/18/14
20140273109

Benzylisoquinoline alkaloids (bia) producing microbes, and methods of making and using the same


Aspects of the invention include host cells that are engineered to produce benzylisoquinoline alkaloids (bias). The host cells include heterologous coding sequences for a variety of enzymes involved in synthetic pathways from starting compounds to bias of the host cell.
09/04/14
20140249201

Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds


Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents.
08/28/14
20140243524

Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin


With r1, r2, r3, r4, r5, r6, r7, r8, and r14 defined herein.. .
08/28/14
20140243333

Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods


A functionalized polycyclic compound can have a structure of formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined diels-alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor.
08/21/14
20140235862

Method for producing 4, 4-difluoro-3,4-dihydroisoquinoline derivatives


Is reacted with hydrogen fluoride.. .
08/21/14
20140235593

Substituted 2-alkyl-1-oxo-n-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides for antimalarial therapies


In one aspect, the invention relates to novel substituted 2-alkyl-1-oxo-n-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating and/or preventing malaria. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention..
08/14/14
20140228576

Method for producing 3,4-dihydroisoquinoline derivatives and production intermediates of same


Provided are an efficient method for producing 3,4-dihydroisoquinoline derivatives and useful production intermediates thereof. Provided is a method for producing 3,4-dihydroisoquinoline derivatives represented by general formula (1), comprising converting a compound represented by general formula (3) in the presence of acid after reacting with an aniline derivative, or converting a compound represented by general formula (3) by reacting with an aniline derivative in the presence of an acid..
08/14/14
20140228575

Process for the preparation of solifenacin and salts thereof


The invention provides a new process for the preparation of solifenacin or a pharmaceutically acceptable acid addition salt thereof, comprising reacting (r)-quinuclidin-3-yl phenethylcarbamate with benzaldehyde in the presence of an acid to obtain a diasteroisomeric mixture (s,r)—((r)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1h)-carboxylate of formula (iv) which can be resolved and the solifenacin or a pharmaceutically acceptable acid addition salt thereof recovered. The invention also provides the new key intermediate (r)-quinuclidin-3-yl phenethylcarbamate involved in the process.
08/07/14
20140221656

Crystalline solvates of 6-(piperidin-4-yloxy)-2h-isoquinolin-1-one hydrochloride


The present invention relates to crystalline solvates of 6-(piperidin-4-yloxy)-2h-isoquinolin-1-one hydrochloride, processes for their preparation and the use thereof.. .
07/24/14
20140206686

Phthalazinones and isoquinolinones as rock inhibitors


Or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective rock inhibitors.
07/03/14
20140187785

Process for the preparation of pyrido[2,1-a] isoquinoline derivatives by catalytic asymmetric hydrogenation of an enamine


Wherein r2, r3, r4 and prot are as defined in the specification.. .
07/03/14
20140187547

Azaindenoisoquinoline topoisomerase i inhibitors


The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase i, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.. .
06/26/14
20140175406

Phosphorescent compounds and organic light emitting diode devices using the same


Where x, y, and z are each selected from the group consisting of carbon and nitrogen, and when x, y, and z are all carbon, r is any one selected from the group consisting of carbazole, α-carboline, β-carboline, γ-carboline, fluorine, dibenzothiophene, dibenzofuran, triphenylsilane, tetraphenylsilane, pyridine, quinoline, isoquinoline, pyrimidine, diphenylphosphineoxide, and substituents thereof.. .
06/05/14
20140154272

Compound and modulating opioid receptor activity


The invention provides a compound of formula (i), wherein r1 is h, c(nh)nh2, an amino acid, or a peptide; x is oh, nh2, nhr2, nr2r3, an amino acid, or a peptide; r2 and r3 are selected from alkyl, alkylenearyl, or alkyleneheteroaryl; each r4 and r5 is independently h or ch3; z is 2-amino-2,3-dihydro-1h-indene-2-carboxylic acid; 2-amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid; 6-amino-6,7,8,9-tetrahydro-5h-benzo[7]annulene 6-carboxylic acid; cyclohexylalanine; cyclohexylglycine; homophenylalanine; 1-naphthylalanine; 2-naphthylalanine; 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; or octahydro-1h-indole-2-carboxylic acid; n is 0, 1, 2, 3, or 4; with the proviso that x is not nh2 when r1 is h, r4 is h, r5 is ch3, z is aci, and n is 2; or a pharmaceutically acceptable salt, ester or solvate thereof. A method of treating pain and a method for treating a mu-opioid receptor mediated disorder and/or a delta-opioid receptor mediated disorder also are provided..
05/15/14
20140135306

Hdyroxy substituted isoquinolinone derivatives


The invention relates to compounds of formula (i): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of mdm2 and/or mdm4, or variants thereof..
05/01/14
20140121204

Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders.


The present invention relates to novel compounds according to formula i that antagonize gpr84, a g-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (ibd), rheumatoid arthritis, vasculitis, lung diseases (e.g. Chronic obstructive pulmonary disease (copd) and lung interstitial diseases (e.g.
04/24/14
20140113877

Novel 3,4,4a,10b-tetrahydro-1h-thiopyrano[4,3-c] isoquinoline compounds


In which a, x, r1, r2, r3 and r7 have the meanings as given in the description, are novel effective inhibitors of type 4 and type 5 phosphodiesterase.. .
04/24/14
20140112868

Novel tetrahydroisoquinoline compounds for use in the diagnosis and treatment of neurodegenerative diseases


The invention relates to a new class of compounds with high affinity and selectivity towards p-glycoprotein. The invention also relates to the utilization of such compounds in the in vivo diagnosis of neurodegenerative diseases and as medicaments for use in the prevention and treatment of neurodegenerative disease involving p-glycoprotein..
04/17/14
20140107127

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.
04/17/14
20140107117

Thienyl- and furanyl-isoquinolinones and methods for using them


The present invention relates to substituted thienyl- and furanyl-isoquinolinones that act, for example, as modulators of poly(adp-ribose) polymerase (parp). The present invention also relates to processes for the preparation of substituted thienyl and furanyl-isoquinolinones and to their use in treating various diseases and disorders..
03/20/14
20140080865

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..
02/27/14
20140058100

Tetrahydroisoquinolin-1-one derivative or salt thereof


To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (ibs). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (bb2) receptor antagonistic action.


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Isoquinolin topics: Isoquinolin, Quinoline Derivatives, Carbon Atoms, Praziquantel, Crystallin, Pharmaceutically Acceptable Salt, Cycloalkyl, Alkyl Group, Sulfonamide, Solifenacin, Cancer Cells, Cancer Cell, Viral Infection, Human Immunodeficiency Virus, Immunodeficiency

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