Производные изоиндолина для применения в лечении вирусной инфекции

ПРОИЗВОДНЫЕ ГАЛАНТАМИНА И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Описываются производные галантамина как ингибиторы ацетилхолинэстеразы. В частности, описываются соединения формулы, приведенной в описании, для лечения нарушения памяти, характеризующегося пониженной холинэргической функцией, фармацевтические композиции, содержащие эти соединения, и способы получения и применения этих соединений.

НОВЫЕ ЭФИРНЫЕ ПРОИЗВОДНЫЕ ИЗОКСАЗОЛА В КАЧЕСТВЕ ПОЗИТИВНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРА ГАМК А АЛЬФА 5

Galanthamin Derivate, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Medikamente

GELDANAMYCINDERIVATE UND ANTITUMORMITTEL MIT EINEM GEHALT DERSELBEN

Eine effiziente Synthese für Benzoperylen-Derivate. Verbesserung der Diels-Alder-Clar-Reaktion

Benzoperylentetracarbonsäure-Derivate sind aus Perylentetracarbonsäurebisimiden durch Umsetzung mit Maleinsäureanhydrid unter Zusatz von Chloranil als Aromatisierungsreagenz synthetisiert worden. Durch eine Erhöhung der Reaktionstemperatur, eine Verlängerung der Reaktionszeit, eine Erhöhung der Äquivalente an Chloranil und die sukzessive Zugabe des Chloranils ließ sich eine nahezu quantitative Umsetzung erzielen. Die Synthesemethode konnte auf die Umsetzung von Imidazoloperylenbisimiden. und von Perylendicarbonsäureimiden ausgedehnt werden. Perylen reagiert glatt zweimal zum Coronenderivat und auch Benzoperylendicarbonsäureimide lassen sich effizient zu den Coronenderivaten umsetzen. Die neue Reaktionsführung ist ebenfalls erfolgreich auf die Umsetzung von PTAD (4-Phenyltriazol-1,2,4-triazol-3,5-dion) angewendet worden.

5,6,6A,7-TETRAHYDRO-4H-DIBENZ(DE,G)ISOQUINOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Alpha-adrenergene Rezeptor-Antagonisten.

Verfahren zur Herstellung neuer heterocyclischer Verbindungen

HETEROCYCLIC AMINO COMPOUNDS

Inhibitors of human immunodeficiency virus replication

Indazoles, benzisoxazoles and benzisothiazoles andtheir use as estrogenic agents

Benzothiazole compounds and their pharmaceutical use

BENZOTHIAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USE

Inhibitors of human immunodeficiency virus replication.

Napht-2-ylacetic acid derivatives to treat AIDS

Inhibitors of human immunodeficiency virus replication.

Napht-2-ylacetic acid derivatives to treat AIDS

BENZOTHIAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USE

Benzothiazole compounds and their pharmaceutical use

Benzothiazole compounds and their pharmaceutical use

BENZOTHIAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USE

Indazoles, benzisoxazoles and benzisothiazoles andtheir use as estrogenic agents

Inhibitors of human immunodeficiency virus replication.

BIARYLSULFONAMIDE AS MMP INHIBITORS

VERFAHREN ZUR HERSTELLUNG VON 1-HYDROXY-APORPHINDERIVATEN

INDAZOLE, BENZISOXAZOLE AND BENZISOTHIAZOLE AND THEIR USE AS ÖSTROGENE MEANS

VERFAHREN ZUR HERSTELLUNG VON FURO(3,4-C)PYRIDINDERIVATEN IN NICHT-RACEMISCHER FORM

ALPHA-ADRENERGIC RECEPTOR ANTAGONISTS.

BENZOPYRANO (4,3,2-CD>INDAZOLVERBINDUNGEN, PROCEDURE FOR YOUR PRODUCTION AND IT ABSTENTIONS the PHARMACEUTICAL PREPARATIONS.

PROCEDURE FOR THE ISOLATION OF GALANTHAMIN

SUBSTITUTE CHINOLIN DERIVATIVES WITH ANTIVIRAL EFFECT

CHROMENO (4,3,2-DE) ISOCHINOLINE AS EFFECTIVE ONE DOPAMINE RECEPTOR LIGAND

OXAZINOCHINOLONE TO THE TREATMENT OF VIRALEN INFECTIONS

SUBSTITUTED HETERCYCLISCH CONDENSED GAMMA CARBOLINE

SUBSTITUTED HETEROCYCLYLKONDENSIERTE GAMMA CARBOLINE

SUBSTITUTED HETEROCYCLYLKONDENSIERTE GAMMA CARBOLINE

Azo compounds for type I phototherapy

Solid state forms of HIV inhibitor

The invention relates to novel crystalline forms of (2S)-2-tert-butoxy-2-(4-(2,3- dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid, the hydrochloride salt thereof, novel crystalline forms of the hydrochloride salt, methods for the preparation thereof, pharmaceutical compositions thereof and their use in the treatment of Human Immunodeficiency Virus (HIV) infection.

Resolution of a narwedine amide derivative

Poly(adp-ribose) polymerase ("parp") inhibitors, methods and pharmaceutical compositions for treating neural or cardiovascular tissue damage

Isoindoline derivatives for use in the treatment of a viral infection

Compounds of Formula I are disclosed and methods of treating viral infections with compositions comprising such compounds (Formula I) ...

Novel 5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative

There is provided a 5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative which is useful in the treatment of respiratory syncytial virus (RSV) infection and for the prevention of disease associated with RSV infection. (Formula (I)) ...

5-HT2C receptor agonists and compositions and methods of use

Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor. Also provided in some embodiments are methods, such as, for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, ...

5-HT2C receptor agonists and compositions and methods of use

Provided in some embodiments are compounds of Formula A, as defined herein, that modulate the activity of 5-HT2C receptor. Also provided in some embodiments are methods, such as, for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, ...

BEUZODIOXINOPYRROLE DERIVATIVES

RESOLUTION OF A NARWEDINE AMIDE DERIVATIVE

The present invention provides for an efficient method of effecting the resolution of a narwedine amide, and the synthesis of galantamine.

R(-)-10,11-ALKYLENEDIOXY-N-ALKYLNORAPOMORPHINE

CHROMENO[4,3,2-DE]ISOQUINOLINES AS POTENT DOPAMINE RECEPTOR LIGANDS

Novel dopamine receptor ligands of formula (I) pharmaceutical formulations of such compounds, and a method using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system, are described. The compounds are expected to be useful in treating Parkinson's disease, improving cognition, improving memory, improving the negative symptoms of schizophrenia, improving attention-deficit hyperactivity disorder and related developmental disorders, treating substance abuse disorders, and in treating various peripheral conditions where changes in dopamine receptor occupation affects physiological function, including organ perfusion, cardiovascular function, and selected endocrine and immune system functions.

AZO AND DIAZA DERIVATIVES AND USES THEREOF IN PHOTOTHERAPY

The invention relates generally to optical agents, including Type 1 phototherapeutic agents, for biomedical applications, such as phototherapy. Provided are fused ring azo and diaza compounds comprising a plurality of fused rings including a first ring having an intra- ring azo or intra-ring diaza group capable of activation upon exposure to electromagnetic radiation in visible and/or infrared regions of the electromagnetic spectrum. Optical agents of the invention enable a versatile phototherapy platform for treatment of a range of pathological conditions, including the treatment of cancers, stenosis and inflammation. The invention further provides preparations and formulations comprising the fused ring azo and diaza compounds and methods of making and using the fused ring azo and diaza compounds as optical agents in in vivo or ex vivo biomedical procedures.

LIPID CONJUGATE PREPARED FROM SCAFFOLD MOIETY

The application relates to a lipid conjugate of formula M-X1-L wherein M is a molecule of interest such as a drug moiety; X1 is a linker group such as ester, ether or carbamate; and L is a lipid scaffold represented by formula (lId): -L1-[L2(H)(X2R)]n-L3-[L4(H)(X2R)]p-L5-L6 and wherein L comprises 5 to 40 carbon atoms and 0 to 2 carbon-carbon double bonds. The lipid conjugate can be formulated in a drug delivery vehicle such as a lipid nanoparticle (LNP).

CONDENSED PYRAZOLE DERIVATIVES AND PROCESS FOR THEIR PREPARATION

Condensed pyrazole derivatives and process for their preparation. The invention relates to compounds having the general formula (I) (I) wherein Z represents a C2-C6 alkylene chain or a -CH=CH-CH= group or an -E-CHR4-(CH2)p- group, in which p is zero, 1 or 2; E represents an oxygen atom or a ?S(O)q group, wherein q is zero, 1 or 2; and R4 is hydrogen or C1-C3 alkyl; R1 represents C1-C6 alkyl, benzyl, pyridyl or phenyl, the phenyl being unsubstituted or substituted by one or two substituents chosen independently from halogen, trifluoromethyl, C1-C6 alkyl, C1-C6 alkoxy, nitro, amino, formylamino and C2-C8 alkanoylamino; each of R2 and R3 is independently: a) hydrogen, halogen or C1-C6 alkyl; b) hydroxy, C1-C6 alkoxy or C3-C4 alkenyloxy; or c) nitro, amino, formylamino or C2-C3 alkanoylamino; and W represents: a') a -CO-?H-S(O)n-CH3 group, wherein n is 1 or 2 and R represents hydrogen or C1-C6 alkyl; or b') a -CO-?H-CN group, wherein Q represents hydrogen, carboxy, CONH2, C2-C7 alkoxycarbonyl ...

.ALPHA. -ADRENERGIC RECEPTOR ANTAGONISTS

Alpha-adrenoceptor antagonists having the formula: which are useful to produce .alpha.-adrenoceptor antagonism, pharmaceutical compositions including these antagonists, and methods of using these antagonists to produce .alpha.-adrenoceptor antagonism in mammals.

BRIDGED TRICYCLIC CARBAMOYLPYRIDONE COMPOUNDS AND THEIR PHARMACEUTICAL USE

Compounds for use in treating or preventing human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R¹, R², L, W¹, W², X, Y, and Z are as defined herein. Methods associated with the preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

NEW ISOXAZOLYL ETHER DERIVATIVES AS GABA A ALPHA5 PAM

The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, X, Y and Z are as described herein, compositions including the compounds and methods of using the compounds.

CHOLINERGIC ENHANCERS WITH IMPROVED BLOOD-BRAIN BARRIER PERMEABILITY FOR THE TREATMENT OF DISEASES ACCOMPANIED BY COGNITIVE IMPAIRMENT

The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g. galanthamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as "pro-drugs", in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. Compounds of this invention may be used as medicaments.

COMPOUNDS, METHODS AND PHARMACEUTICAL COMPOSITIONS FOR INHIBITING PARP

... ²²The present invention provides for compounds of general formula I below, which ²²inhibit poly(ADP-ribose) polymerase ("PARP"), compositions containing these ²compounds and methods for using these PARP inhibitors to treat, prevent and/or ²²ameliorate the effects of the conditions described herein.²²(see formula I)² ...

METHODS OF MODULATING NEUROTROPHIN-MEDIATED ACTIVITY

The current application discloses methods of modulating the interaction of nerve growth factor, or precursors thereof, with neurotrophin receptors by contacting cells expressing a neurotrophin receptor with a benzo-phenantroli ne core structure compound. The compounds involved in these methods are the one s of formulae (16-22). Also claimed and disclosed are specific compounds of formulae (16-21),of which formulae (16) and (21) are herein given as a chemical core type-structure of the disclosed compounds.

ISOINDOLINE DERIVATIVES FOR USE IN THE TREATMENT OF A VIRAL INFECTION

Compounds of Formula I are disclosed and methods of treating viral infections with compositions comprising such compounds (Formula I) ...

NAPHT-2-YLACETIC ACID DERIVATIVES TO TREAT AIDS

The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).

BENZOTHIAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USE

The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.

PROCESS FOR ISOLATING GALANTHAMINE

The subject matter of the present invention concerns a process for the isolation of the alkaloid galanthamine; the galanthamine itself which has been produced according to this process; the use of the galanthamine thus produced in galenic preparations; and the galanthamine thus produced for treating narrow-angle glaucoma, Alzheimer's disease, as well as alcohol and nicotine dependence. ...

VERFAHREN ZUR HERSTELLUNG VON BENZOXANTHEN- ODER BENZOTHIOXANTHENFARBSTOFFEN.

Fused-ring or bridged n1-monosubstd n-acylpyrazolidines

Prodn. of new fused-ring or bridged N'-monosubst. N-acylpyrazolidines by reacting, with the loss of H2O, (A) an olefinic aldehyde (or reactive functional deriv. thereof), the olefinic double bond of which is sepd. from the aldehyde group by 3-5 atoms of which 1 or 2 can be members of one and the same ring, with (B) an N'-monosubst. N-acyl-hydrazine. Many specific products are claimed per se. Intermediates, esp. for pharmaceuticals.

THE 4 - (DI-N) AMINO 1.3.4.5-TO-TRETRAHYDROBENZO (CD'S) INDOLE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME.

PROCEDURE FOR the PRODUCTION OF 1-HYDROXY-APORPHINDERIVATEN.

Process for preparing furo (3.4 c) pyridine derivatives in non-racemic.

DERIVATIVES OF BENZOTHIAZOL - 6 - YL ACETIC ACID AND THEIR USE FOR THE TREATMENT OF HIV-INFECTION

ISOINDOLINE DERIVATIVES FOR APPLICATION IN TREATMENT OF VIRAL INFECTION

SUBSTITUTED DERIVATIVES OF AZOANTRATsENA, PHARMACEUTICAL COMPOSITIONS AND METHODS OF THEIR APPLICATION

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ АЗОАНТРАЦЕНА, ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Изобретение относится к замещенным производным азоантрацена или их фармацевтически приемлемым солям, которые модулируют рецептор GLP-1R человека и которые могут быть применимы при лечении заболеваний, нарушений или состояний, при которых модуляция рецептора GLP-1 человека является полезной, таких как сахарный диабет 2 типа. Изобретение также относится к фармацевтическим композициям, содержащим эти соединения, и к применению этих соединений и композиций при лечении таких заболеваний, нарушений или состояний, при которых модуляция рецептора GLP-1 человека является полезной.

ИНГИБИТОРЫ РЕПЛИКАЦИИ ВИРУСА ИММУНОДЕФИЦИТА ЧЕЛОВЕКА

В заявке описаны соединения формулы I в которой a, R1, R2, R3, R4, R5 и R6 определены в настоящем изобретении, которые применимы в качестве ингибиторов репликации ВИЧ.

ИНГИБИТОРЫ РЕПЛИКАЦИИ ВИРУСА ИММУНОДЕФИЦИТА ЧЕЛОВЕКА

В заявке описаны соединения формулы I в которой значения R4 , R6 и R7 определены в настоящем изобретении, применимые в качестве ингибиторов репликации ВИЧ.

ПРОТИВОВИРУСНЫЕ ТЕРАПЕВТИЧЕСКИЕ СРЕДСТВА

В изобретении предложены соединения формулы I, описанные в настоящей заявке, а также фармацевтические композиции, содержащие эти соединения, и способы синтеза и синтетические промежуточные соединения, которые можно применять для получения указанных соединений. Соединения формулы I можно применять в качестве противовирусных агентов и/или в качестве противораковых агентов.

Benzothiazol-6-il acetic acid derivatives and their use for treating an HIV infection

ИНГИБИТОРЫ РЕПЛИКАЦИИ ВИРУСА ИММУНОДЕФИЦИТА ЧЕЛОВЕКА

В изобретении описаны соединения формулы I в которой значения R4, R6 и R7 определены в настоящем изобретении, применимые в качестве ингибиторов репликации ВИЧ.

Method of preparation of the l-tétrahydropalmatine

Antiinflammatory and CNS active phthalazines - specif 3-amino-(1)-benzopy-rano- or benzothiopyrano (4,3,2-de) phthalazines

INDAZÓIS, BENZISOXAZÓIS AND BENZISOTIAZÓIS AND ITS USES AS AGENTS ESTROGÊNICOS

2-oxa-5-azabicyclo[2.2.1]heptan-3-yl derivatives

METHODS FOR PREPARING ARENE-BIS(DICARBOXIMIDE)-BASED SEMICONDUCTING MATERIALS AND RELATED INTERMEDIATES FOR PREPARING SAME

The present teachings provide compounds of formulae I and H: where Q, Ra, R1, W, and n are as defined herein. The present teachings also provide methods of preparing compounds of formulae I and II, including methods of preparing compounds of formula II from compounds of formula I. The compounds disclosed herein can be used to prepare semiconductor materials and related composites and electronic devices.

BIARYL SULFONAMIDES AS MMP INHIBITORS

The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors: Formule (I).

alpha-ADRENERGIC RECEPTOR ANTAGONISTS

Alpha-adrenoceptor antagonists having formula (I), which are useful to produce alpha-adrenoceptor antagonism, pharmaceutical compositions including these antagonists, and methods of using these antagonists to produce alpha-adrenoceptor antagonism in mammals.

Compounds, methods and pharmaceutical compositions for treating cellular damage, such as neural or cardiovascular tissue damage

The disclosure relates to compounds, pharmaceutical compositions and methods for inhibiting PARP by use of the disclosed compositions. The compounds of the disclosure have the following structures I, II and III: ...

Water-Soluble Rhodamine Dye Conjugates

The present invention provides novel, water-soluble, red-emitting fluorescent rhodamine dyes and red-emitting fluorescent energy-transfer dye pairs, as well as labeled conjugates comprising the same and methods for their use. The dyes, energy-transfer dye pairs and labeled conjugates are useful in a variety of aqueous-based applications, particularly in assays involving staining of cells, protein binding, and/or analysis of nucleic acids, such as hybridization assays and nucleic acid sequencing.

Aziridine aldehydes, aziridine-conjugated amino derivatives, aziridine-conjugated biomolecules and processes for their preparation

The present invention relates to unprotected amino aldehydes and applications for same. More particularly, the present invention relates to novel aziridine aldehydes and processes for preparing these novel compounds. The invention also relates to aziridine-conjugated amino derivatives, and processes for preparing the same. Pentacyclic compounds may be prepared using the aziridine aldehydes of the present invention, and the invention relates to these compounds and the processes by which they are made. The invention also relates to aziridine-conjugated bioactive molecules, such as amino acids and peptides, and processes for preparing such compounds.

FUSED 2-PYRIMIDINEPROPIONIC ACID COMPOUNDS, RELATED COMPOUNDS, AND THE PROCESS FOR THEIR PREPARATION

Biaryl sulfonamides and methods for using same

The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.

Galanthamine derivatives, a process for their preparation and their use as medicaments

ИНДЕНОИЗОХИНОЛИНОНОВЫЕ АНАЛОГИ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

... 1. Соединение формулы ! ! или его фармацевтически приемлемая соль, где ! X представляет собой -CH2-, -О-, -C(O)-, -NH- или -S-; ! R1 представляет собой -(CH2)n-N(R2)(R2), -О-(CH2)m-N(R2)(R2), -(CH2)n-OR3 или -О-(CH2)m-OR3; ! каждый R2 независимо представляет собой -H, -C1-C6 алкил, -C3-C8 моноциклический циклоалкил, -C1-C6 алкиленфенил, фенил, N-концевой остаток альфа-аминокислоты, N-концевой альфа-аминогидроксиметильный остаток, C1-C6 алкиловый эфир N-концевого остатка альфа-аминокислоты или азотсодержащий, от 3- до 7-членный моноциклический гетероцикл, каждый из которых, отличный от водорода, независимо является незамещенным или замещенным одним или большим количеством заместителей, таких как -галоген, -OH, -OP(O)(OH)2, -OS(O)2OH, -C1-C6 алкил, -О-C1-C6 алкил, -C3-C8 моноциклический циклоалкил, от 3- до 7-членный моноциклический гетероцикл, -C1-C6 алкилзамещенный, от 3- до 7-членный моноциклический гетероцикл, или -N(Z3)(Z4), где Z3 и Z4 независимо представляют собой -H, -C1-C5 алкил, ...

АМИНОКИСЛОТНЫЕ И ПЕПТИДНЫЕ ПРОЛЕКАРСТВА ГАЛАНТАМИНА И ИХ ПРИМЕНЕНИЕ

... 1. Соединение Формулы 1:Формула 1или его фармацевтически приемлемая соль, гдеRявляется H,или;Rявляется H, CH,или;каждый Rявляется независимо водородом, замещенной алкильной группой или незамещенной алкильной группой;каждый R, R,R, и Rявляется независимо выбранным из водорода,, замещенной алкильной группы или незамещенной алкильной группы;каждый nявляется независимо 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 или 16;каждый nявляется независимо 1, 2, 3, 4, 5, 6, 7, 8 или 9;каждый nявляется независимо 0 или 1;каждый nявляется независимо 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 или 16;каждый nявляется независимо 0 или 1;каждый Rявляется независимо боковой цепью протеиногенной или непротеиногенной аминокислоты;каждый X является независимо (-NH-), (-O-) или отсутствует;каждый X′ является независимо (-NH-), (-O-) или отсутствует;каждый Y является независимоили;икаждый Cy представляет собой независимо 5- или 6-членный циклоалкил, 5- или 6-членный гетероцикл, 5- или 6-членный ...

ПРОИЗВОДНЫЕ БЕНЗОТИАЗОЛ-6-ИЛ УКСУСНОЙ КИСЛОТЫ И ИХ ПРИМЕНИЕ ДЛЯ ЛЕЧЕНИЯ ВИЧ-ИНФЕКЦИИ

1. Соединение или его фармацевтически приемлемая соль формулы I′:где: Rпредставляет собой, или;A представляет собой фенил, моноциклический гетероарил или моноциклический гетероцикл, где A возможно замещен от 1 до 5 Zгруппами;B представляет собой (C-C)арил, гетероарил или гетероцикл, где В возможно замещен 1-5 Zгруппами; или A и B совместно образуют бициклический (C-C)арил, бициклический гетероарил или бициклический гетероцикл, где каждый бициклический (C-C)арил, бициклический гетероарил или бициклический гетероцикл возможно замещен от 1 до 5 Zгруппами;каждый из Zнезависимо представляет собой галоген, (C-C)алкил, (C-C)алкенил, (C-C)алкинил, (C-C)галогеналкил, (C-C)карбоцикл, 3-7-членный моноциклический гетероцикл, -O(C-C)алкил, -O(C-C)алкенил, -O(C-C)алкинил, -NRR, -NRC(O)R, -C(O)ORили -C(O)NRR, где любой (C-C)карбоцикл илигетероцикл из Zвозможно независимо замещен от 1 до 5 галогенами или (C-C)алкилами;каждый из Zнезависимо представляет собой галоген, CN, (C-C)алкил, (C-C)алкенил, (C-C)алкинил, (C-C)галогеналкил, (C-C)карбоцикл, гетероарил, 3-7-членный моноциклический гетероцикла, (C-C)арил(C-C)алкил-, -OH, -O(C-C)алкил, -O(C-C)алкенил, -O(C-C)алкинил, -NRR, -NRC(O)R, -C(O)ORили -C(O)NRR, где любой (C-C)карбоцикл или гетероцикл из Zвозможно независимо замещен от 1 до 5 галогенами или (C-C)алкилами; икаждый из R, R, Rили Rнезависимо представляет собой H или (C-C)алкил;при этом каждый гетероарил, как моноциклическое кольцо или как часть 2-3-кольцевой системы, имеет от 1 до 6 атомов углерода и от 1 до 4 гетероатомов, выбранных из группы, состоящей из кислорода, азота и серы, и каждый гетероцикл, как моноциклическое кольцо или как часть 2-3-кольцевой системы, имеет от 1 до 6 атомов углерода и от 1 до 3 гетероатомов, выбранных из группы, сос РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 277/66 (13) 2014 115 227 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2014115227/04, 19.04.2013 (71) Заявитель(и): ДЖИЛИД ...

ИНГИБИТОР РФРФ4, СПОСОБ ЕГО ПОЛУЧЕНИЯ И ЕГО ФАРМАЦЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ

ИНГИБИТОРЫ ПОЛИ(АДФ-РИБОЗА) ПОЛИМЕРАЗЫ ("PARP"), СПОСОБЫ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ ДЛЯ ЛЕЧЕНИЯ ПОВРЕЖДЕНИЯ НЕРВНОЙ ИЛИ СЕРДЕЧНО-СОСУДИСТОЙ ТКАНИ

... 1. Соединение, формулы I или его фармацевтически приемлемые соль, гидрат, пролекарство или их смеси, где Y обозначает алкилгалоген, алкил-CO-G, COG, прямую связь, С= О, О, NR11 или CR8; G обозначает NR11R16, OR9, SR9 или R10; Z обозначает О, S или NR11; X обозначает NR16, О, S, CR12R13, C= O, связь, -CR12= CR13-, -C(R12R13)C(R14R15)-, или R1, R2, R3, R4, R5, R6, R7, R8, R10, R12, R13, R14 или R15 представляют собой независимо водород, галоген, алкилгалоген, гидрокси, С1-С9-алкил с прямой или разветвленной цепью, С2-С9-алкенил с прямой или разветвленной цепью, С3-С8-циклоалкил, С5 -С7-циклоалкенил, арил, амино, алкиламино, нитро, нитрозо, карбокси или аралкил; R9 обозначает водород, гидрокси, С1-С9-алкил с прямой или разветвленной цепью, С2-С9-алкенил с прямой или разветвленной цепью, С3-С8-циклоалкил, С5-С7-циклоалкенил, арил, амино, алкиламино, карбокси или аралкил; R11 или R16 обозначают независимо водород, галоген, алкилгалоген, гидрокси, С1-С9-алкил с прямой или разветвленной цепью, ...

1-ЗАМЕЩЕННОЕ ПРОИЗВОДНОЕ ТЕТРАГИДРОИЗОХИНОЛИНА

... 1. Соединение формулы (I) !! где R1a и R1b являются одинаковыми или разными и представляют собой -H, C1-6алкил, который может быть замещен, циклоалкил, который может быть замещен, арил, который может быть замещен, или ароматический гетероцикл, который может быть замещен, при условии, что оба из R1a и R1b не могут быть -H, и R1a и R1b, взятые вместе с атомом углерода, к которому они присоединены, могут представлять собой циклоалкил, который может быть замещен, ! R3a, R3b, R4a и R4b являются одинаковыми или разными и представляют собой -H или C1-6алкил, ! R5, R6, R7 и R8 являются одинаковыми или разными и представляют собой -H, C1-6алкил, который может быть замещен, -O-(C1-6алкил), который может быть замещен, циано, карбамоил, который может быть замещен одним или двумя C1-6алкилами, или галоген, и любые две соседние группы R5, R6, R7 и R8, взятые вместе, могут образовывать -O-CH2-O- или -O-(CH2)2-O-, ! R11, R12, R13, R14, R15 и R16 являются одинаковыми или разными и представляют собой -H ...

Use of rylene derivatives as photosensitizers in solar cells

Use of rylene derivatives I with the following definition of the variables: X together both —COOM; Y a radical -L-NR 1 R 2   (y1) -L-Z—R 3   (y2) the other radical hydrogen; together both hydrogen; R is optionally substituted (het)aryloxy, (het)arylthio; P is —NR 1 R 2 ; B is alkylene; optionally substituted phenylene; combinations thereof; A is —COOM; —SO 3 M; —PO 3 M 2 ; D is optionally substituted phenylene, naphthylene, pyridylene; M is hydrogen; alkali metal cation; [NR 5 ] 4 + ; L is a chemical bond; optionally indirectly bonded, optionally substituted (het)arylene radical; R 1 , R 2 are optionally substituted (cyclo)alkyl, (het)aryl; together optionally substituted ring comprising the nitrogen atom; Z is —O—; —S—; R 3 is optionally substituted alkyl, (het)aryl; R′ is hydrogen; optionally substituted (cyclo)alkyl, (het)aryl; R 5 is hydrogen; optionally substituted alkyl (het)aryl; m is 0, 1, 2; n, p m=0: 0, 2, 4 where: n+p=2, 4, if appropriate 0; m=1: 0, 2, 4 where: n+p=0, 2, 4; m=2: 0, 4, 6 where: n+p=0, 4, 6, or of mixtures thereof as photosensitizers in solar cells.

NAPHT-2-YLACETIC ACID DERIVATIVES TO TREAT AIDS

The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I). 2. The compound of wherein Ris (C-C)alkyl claim 1 , (C-C)alkenyl or —O(C-C)alkyl wherein any (C-C)alkyl or (C-C)alkenyl of Ris optionally substituted with one or more groups selected from —O(C-C)alkyl claim 1 , halo claim 1 , oxo and —CN; and wherein Ris H.4. The compound of wherein Ris selected from:{'sub': 1', '6', '2', '6', '1', '6', '3', '7', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'a) aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and heteroaryl is optionally substituted with one or more groups each independently selected from halo, (C-C)alkyl, (C-C)alkenyl, (C-C)haloalkyl, (C-C)cycloalkyl, —OH, —O(C-C)alkyl, —SH, —S(C-C)alkyl, —NH, —NH(C-C)alkyl and —N((C-C)alkyl), wherein (C-C)alkyl is optionally substituted with hydroxy, —O(C-C)alkyl, cyano or oxo;'}{'sub': 3', '14', '3', '14', '3', '7, 'sup': 1', '1, 'b) (C-C)carbocycle, wherein (C-C)carbocycle is optionally substituted with one or more Zgroups, wherein two Zgroups together with the atom or atoms to which they are attached optionally form a (C-C)carbocycle or heterocycle; and'}{'sup': 7', '1, 'c) aryl, heteroaryl and fused-heterocycle, wherein any aryl, heteroaryl and fused-heterocycle is substituted with one or more Zgroups and optionally substituted with one or more Zgroups.'}5. The compound of wherein Ris selected from:{'sub': 1', '6', '2', '6', '1', '6', '3', '7', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6, 'a) aryl, heterocycle and heteroaryl, wherein any aryl, heterocycle and ...

INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Compounds of formula I: 6. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris (C)alkyl claim 1 , —CN claim 1 , halo or (C)haloalkyl.7. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CH.11. A pharmaceutical composition comprising a compound of formula (I) according to any one of to claim 1 , or a pharmaceutically acceptable salt thereof; and one or more pharmaceutically acceptable carriers.12. A method of treating HIV infection which comprises administering to a host infected by HIV a therapeutically effective amount of a compound of formula (I) according to any one of to claim 1 , or a pharmaceutically acceptable salt thereof. This application claims benefit of U.S. Ser. No. 61/178,551, filed May 15, 2009, and U.S. Ser. No. 61/285,766, filed Dec. 11, 2009, which are herein incorporated by reference.The present invention relates to compounds, compositions and methods for the treatment of human immunodeficiency virus (HIV) infection. In particular, the present invention provides novel inhibitors of the HIV integrase enzyme, pharmaceutical compositions containing such compounds and methods for using these compounds to reduce HIV replication and in the treatment of HIV infection.Acquired immune deficiency syndrome (AIDS) is caused by the human immunodeficiency virus (HIV), particularly the HIV-1 strain. Most currently approved therapies for HIV infection target the viral reverse transcriptase and protease enzymes. There are also two approved drugs targeting HIV entry and one approved drug targeting the integrase enzyme. Within the reverse transcriptase inhibitor and protease inhibitor classes, resistance of HIV to existing drugs is a problem. Therefore, it is important to discover and develop new antiretroviral compounds.International patent application WO 2007/131350 and United States published patent application US 2006/0106070 describe compounds which are active ...

THERAPEUTIC COMPOUNDS

Compounds of formula I′: 2. The compound of wherein A is phenyl claim 1 , monocyclic heteroaryl or monocyclic heterocycle wherein any phenyl claim 1 , monocyclic heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.3. The compound of wherein A is phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle wherein any phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.4. The compound of wherein A is monocyclic N-heteroaryl claim 1 , wherein monocyclic N-heteroaryl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.5. The compound of wherein A is pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridinyl-2-one claim 1 , tetrahydropyrimidinyl-2-one claim 1 , imidazolidinyl-2-one claim 1 , pyrrolidinyl-2-one or pyrrolidinyl claim 1 , wherein pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridinyl-2-one claim 1 , tetrahydropyrimidinyl-2-one claim 1 , imidazolidinyl-2-one claim 1 , pyrrolidinyl-2-one or pyrrolidinyl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.6. The compound of wherein B is phenyl claim 1 , pyridinyl claim 1 , pyrazolyl claim 1 , pyrimidinyl claim 1 , indazolyl claim 1 , pyrazolopyridine or benzimidazolyl claim 1 , wherein any phenyl claim ...

Nanofibril materials for highly sensitive and selective sensing of amines

A sensory material with high sensitivity, selectivity, and photostability has been developed for vapor probing of organic amines. The sensory material is a perylene-3,4,9,10-tetracarboxyl compound having amine binding groups and the following formula where A and A′ are independently chosen from N—R1, N—R2, and O such that both A and A′ are not O, and R1 through R10 are amine binding moieties, solubility enhancing groups, or hydrogen such that at least one of R1 through R10 is an amine binding moiety. This perylene compound can be formed into well-defined nanofibers. Upon deposition onto a substrate, the entangled nanofibers form a meshlike, highly porous film, which enables expedient diffusion of gaseous analyte molecules within the film matrix, leading to a milliseconds response for vapor sensing.

TREATMENT OF MECP-2 ASSOCIATED DISORDERS

The invention relates to the use of cystamine, cysteamine, or a salt thereof, or of calcineurin inhibitors for treating a MeCP2-associated disorder such as Rett syndrome. 1. Cystamine or cysteamine , or a salt thereof , for use in treating a MECP2-associated disorder in a patient.2. Cystamine or cysteamine for use in treating a MECP2-associated disorder according to claim 1 , wherein the MECP2-associated disorder is selected from the group consisting of Rett syndrome claim 1 , autism claim 1 , Pervasive development disorder claim 1 , non-syndromic mental retardation claim 1 , idiopathic neonatal encephalopathy and idiopathic cerebral palsy.3. Cystamine or cysteamine for use in treating a MECP2-associated disorder according to claim 2 , wherein the MECP2-associated disorder is Rett syndrome.4. Cystamine or cysteamine for use in treating a MECP2-associated disorder according to any of to claim 2 , for use in combination with another pharmaceutically active compound.5. A calcineurin inhibitor for use in treating a MECP2-associated disorder in a human patient.6. The calcineurin inhibitor for use in treating a MECP2-associated disorder according to claim 5 , which is a macrolide.7. The calcineurin inhibitor for use in treating a MECP2-associated disorder according to or claim 5 , which is selected from the group consisting of calcipressins claim 5 , tacrolimus and tacrolimus analogs claim 5 , cyclosporine A and cyclosporine A analogs claim 5 , LxPV proteins claim 5 , 2 claim 5 ,6-diaryl-substitued pyrimidine derivatives and FK506-binding proteins8. The calcineurin inhibitor for use in treating a MECP2-associated disorder according to claim 7 , which is selected from the group consisting of calcipressin 1 claim 7 , calcipressin 2 claim 7 , calcipressin 3 claim 7 , tacrolimus claim 7 , ascomycin claim 7 , sirolimus claim 7 , pimecrolimus claim 7 , cyclosporine A claim 7 , voclosporine claim 7 , LxPVc1 claim 7 , LxPVc2 claim 7 , LxPVc3 claim 7 , 6-(3 claim 7 ,4-dichloro- ...

Diazabenzo[de] anthracen-3-one compounds and methods for inhibiting parp

The present invention relates to diazabenzo[de]anthracen-3-one compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.

SOLID STATE FORMS OF HIV INHIBITOR

The invention relates to a novel hemi-succinate salt form of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid and a novel crystalline form thereof, methods for the preparation thereof, pharmaceutical compositions thereof and their use in the treatment of Human Immunodeficiency Virus (HIV) infection. 2. The hemi-succinate salt of Compound (I) according to in crystalline Form A.3. The crystalline hemi-succinate salt of Compound (I) according to having an X-ray powder diffraction pattern comprising peaks at 7.1 claim 2 , 10.3 and 12.5 degrees 2θ (±0.2 degrees 2θ) when measured using CuKα radiation.4. The crystalline hemi-succinate salt of Compound (I) according to having an X-ray powder diffraction pattern further comprising peaks at 18.9 claim 3 , 20.1 and 25.1 degrees 2θ (±0.2 degrees 2θ) when measured using CuKα radiation.5. The crystalline hemi-succinate salt of Compound (I) according to having an X-ray powder diffraction pattern further comprising peaks at 9.0 claim 4 , 22.8 claim 4 , 26.1 and 29.9 degrees 2θ (±0.2 degrees 2θ) when measured using CuKα radiation.6. The crystalline hemi-succinate salt of Compound (I) according to having an X-ray powder diffraction pattern substantially the same as that shown in .7. The crystalline hemi-succinate salt of Compound (I) according to having a DSC thermogram substantially the same as that shown in .8. The crystalline hemi-succinate salt of Compound (I) according to having a TGA curve substantially the same as that shown in .9. The crystalline hemi-succinate salt of Compound (I) according to having an X-ray powder diffraction pattern comprising peaks at 7.1 claim 2 , 10.3 and 12.5 degrees 2θ (±0.2 degrees 2θ) when measured using CuKα radiation and having a DSC thermogram substantially the same as that shown in .10. The crystalline hemi-succinate salt of Compound (I) according to having an X-ray powder diffraction pattern comprising peaks at 7.1 claim 2 , 10.3 and 12.5 ...

SOLID STATE FORMS OF HIV INHIBITOR

The invention relates to novel crystalline forms of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid, the hydrochloride salt thereof, novel crystalline forms of the hydrochloride salt, methods for the preparation thereof, pharmaceutical compositions thereof and their use in the treatment of Human Immunodeficiency Virus (HIV) infection. 2. (canceled)3. The crystalline hydrochloride salt of Compound (I) according to in crystalline Type A having an X-ray powder diffraction pattern comprising peaks at 8.1 claim 1 , 9.3 claim 1 , 11.2 claim 1 , 28.4 and 28.6 degrees 2θ (±0.2 degrees 2θ) when measured using CuKα radiation.4. The crystalline hydrochloride salt of Compound (I) according to in crystalline Type A having an X-ray powder diffraction pattern further comprising a peak at 13.0 degrees 2θ (±0.2 degrees 2θ) when measured using CuKα radiation.5. The crystalline hydrochloride salt of Compound (I) according to in crystalline Type A having an X-ray powder diffraction pattern further comprising peaks at 10.4 claim 4 , 12.1 claim 4 , 18.8 claim 4 , 19.8 claim 4 , 22.1 and 22.4 degrees 2θ (±0.2 degrees 2θ) when measured using CuKα radiation.6. The crystalline hydrochloride salt of Compound (I) according to in crystalline Type A having an X-ray powder diffraction pattern substantially the same as that shown in .7. The crystalline hydrochloride salt of Compound (I) according to in crystalline Type A having a DSC thermal curve substantially the same as that shown in indicated as Type A.8. The crystalline hydrochloride salt of Compound (I) according to in crystalline Type A having an X-ray powder diffraction pattern comprising peaks at 8.1 claim 1 , 9.3 claim 1 , 11.2 claim 1 , 28.4 and 28.6 degrees 2θ (±0.2 degrees 2θ) when measured using CuKα radiation and having a DSC thermal curve substantially the same as that shown in indicated as Type A.9. The crystalline hydrochloride salt of Compound (I) in crystalline Type A ...

PROCESS FOR THE PREPARATION OF AN HIV INTEGRASE INHIBITOR

The present invention is directed to an improved process for the preparation of Compounds of Formula (I), which are useful in the treatment of HIV infection. In particular, the present invention is directed to an improved process for the preparation of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid, which is useful in the treatment of HIV infection. 2. The process according to claim 1 , wherein the palladium catalyst or precatalyst is [Pd(allyl)Cl].5. The process according to claim 1 , wherein the chiral alcohol F1 is converted to tert-butyl ether G1 using trifluoromethanesulfonimide as the catalyst and t-butyl-trichloroacetimidate as source tert-butyl cation.7. The process according to claim 6 , wherein the palladium catalyst or precatalyst is [Pd(allyl)Cl].10. The process according to claim 6 , wherein the chiral alcohol F1 is converted to tert-butyl ether G1 with trifluoromethanesulfonimide as the catalyst and t-butyl-trichloroacetimidate.12. The process according to claim 11 , wherein the palladium catalyst or precatalyst is [Pd(allyl)Cl].13. The process according to claim 11 , wherein the chiral alcohol F is converted to tert-butyl ether G with trifluoromethanesulfonimide as the catalyst and t-butyl-trichloroacetimidate.15. The process according to claim 14 , wherein the palladium catalyst or precatalyst is [Pd(allyl)Cl].17. The process according to claim 14 , wherein the chiral alcohol F is converted to tert-butyl ether G with trifluoromethanesulfonimide as the catalyst and t-butyl-trichloroacetimidate.18. The process according to claim 4 , wherein the halide X in compound O is converted to the corresponding boronic acid P claim 4 , in the presence of toluene.20. The process according to claim 9 , wherein the halide X in compound O is converted to the corresponding boronic acid P claim 9 , in the presence of toluene. This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Patent ...

PROCESS FOR THE PREPARATION OF AN HIV INTEGRASE INHIBITOR

The present invention is directed to an improved process for the preparation of Compounds of Formula (I) or salts thereof which are useful in the treatment of HIV infection. In particular, the present invention is directed to an improved process for the preparation of (2S)-2-tert-butoxy-2-(4-(2,3-dihydropyrano[4,3,2-de]quinolin-7-yl)-2-methylquinolin-3-yl)acetic acid or salt thereof which is useful in the treatment of HIV infection. 5. The process according to claim 1 , wherein the chiral alcohol F1 is converted to tert-butyl ether G1 using trifluoromethanesulfonimide as the catalyst and t-butyl-trichloroacetimidate as source tert-butyl cation.7. The process according to claim 6 , wherein the palladium catalyst or precatalyst is tris(dibenzylideneacetone)dipalladium(0).11. The process according to claim 6 , wherein the chiral alcohol F1 is converted to tert-butyl ether G1 with trifluoromethanesulfonimide as the catalyst and t-butyl-trichloroacetimidate.14. The process according to claim 12 , wherein the chiral alcohol F is converted to tert-butyl ether G with trifluoromethanesulfonimide as the catalyst and t-butyl-trichloroacetimidate.16. The process according to claim 15 , wherein the palladium catalyst or precatalyst is tris(dibenzylideneacetone)dipalladium(0).18. The process according to claim 15 , wherein the chiral alcohol F is converted to tert-butyl ether G with trifluoromethanesulfonimide as the catalyst and t-butyl-trichloroacetimidate.19. The process according to claim 4 , wherein the halide X in compound O is converted to the corresponding boronic acid P claim 4 , in the presence of toluene.21. The process according to claim 9 , wherein the halide X in compound O is converted to the corresponding boronic acid P claim 9 , in the presence of toluene. This application is a continuation of International PCT Patent Application No. PCT/US2012/032027, filed Apr. 3, 2012, now pending, which claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Patent ...

CHOLINERGIC ENHANCERS WITH IMPROVED BLOOD-BRAIN BARRIER PERMEABILITY FOR THE TREATMENT OF DISEASES ACCOMPANIED BY COGNITIVE IMPAIRMENT

A method for the treatment of a neurodegenerative, psychiatric or neurological disease associated with a cholinergic deficit comprising administering GLN-1062 or a pharmaceutically acceptable salt thereof by nasal administration to a patient in need thereof. 2. The method of claim 1 , wherein the disease is selected from the group consisting of Alzheimer's disease claim 1 , Parkinson's disease claim 1 , other types of dementia claim 1 , schizophrenia claim 1 , epilepsy claim 1 , stroke claim 1 , poliomyelitis claim 1 , neuritis claim 1 , oxygen and nutrient deficiencies in the brain after hypoxia claim 1 , anoxia claim 1 , asphyxia claim 1 , cardiac arrest claim 1 , chronic fatigue syndrome claim 1 , various types of poisoning claim 1 , anesthesia claim 1 , spinal cord disorders claim 1 , central nervous system inflammation claim 1 , postoperative delirium and/or subsyndronal postoperative delirium claim 1 , neuropathic pain claim 1 , subsequences of the abuse of alcohol and drugs claim 1 , addictive alcohol and nicotine craving claim 1 , and subsequences of radiotherapy.3. The method of claim 1 , wherein the neurodegenerative claim 1 , psychiatric or neurological disease is selected from the group consisting of Alzheimer's disease claim 1 , Parkinson's disease claim 1 , dementia claim 1 , schizophrenia claim 1 , stroke claim 1 , central nervous system inflammation a central inflammatory disorder claim 1 , and epilepsy.4. The method of claim 1 , wherein GLN-1062 is administered in a pharmaceutical composition as a suspension.5. The method of claim 1 , wherein GLN-1062 is administered in a pharmaceutical composition as a solution.6. The method of claim 4 , wherein the suspension comprises 0.5 to 30 wt % GLN-1062.7. The method of claim 5 , wherein the solution comprises 0.5 to 30 wt % GLN-1062.8. The method of claim 1 , comprising multiple doses to the patient claim 1 , wherein a single dose comprises between 0.1 and 20 mg of GLN-1062. The disclosure refers to ...

CYANATED BENZOXANTHENE AND BENZOTHIOXANTHENE COMPOUNDS

The present invention relates to cyanated compounds of the formula (I) wherein at least one of the radicals R, R, Rand Ris CN, and the remaining radicals are selected from hydrogen, chlorine and bromine; X is O, S, SO or SO; m is 0, 1, 2, 3 or 4; Ris selected from bromine, chlorine, cyano, —NRR, C-C-alkyl, C-C-haloalkyl, C-C-alkoxy, C-C-haloalkoxy, C-C-cycloalkyl, heterocycloalkyl, heteroaryl, C-C-aryl, C-C-aryloxy, C-C-aryl-C-C-alkylene, etc.; A is a diradical selected from diradicals of the general formulae (A.1), (A.2), (A.3), and (A.4) wherein R, (R), (R)and (R)are as defined in the claims and in the description. The invention further relates to color converters comprising at least one polymer as a matrix material and at least one cyanated compound of formula (I) or mixtures thereof as a fluorescent dye, to the use of the color converters and to lighting devices comprising at least one LED and at least one color converter. 3. The process of claim 2 , wherein Rand Rare each cyano claim 2 , and Rand Rare each hydrogen.4. The process of claim 2 , wherein A is a radical of the formula (A.2).7. The process of claim 2 , wherein m is zero or one. This application is a divisional of U.S. application Ser. No. 15/561,218 filed Sep. 25, 2017, allowed and incorporated herein by reference, which is a National Stage application of PCT/EP2016/056488 filed Mar. 24, 2016 and claims the benefit of EP 15161081.3 filed Mar. 26, 2015.The present invention relates to novel cyanated benzoxanthene compounds and cyanated benzothioxanthene compounds and derivatives thereof, to an intermediate compound for preparing them and to a novel process for the preparation of intermediate compounds. The present invention also relates to the use of the cyanated compounds as organic luminescent material, in particular as fluorescent dye in color converters comprising at least one polymer as a matrix material. The present invention also relates to the use of these color converters and to lighting ...

PERYLENEMONOIMIDE AND NAPHTHALENEMONOIMIDE DERIVATIVES AND THEIR USE IN DYE-SENSITIZED SOLAR CELLS

The present invention relates to the use of a compound of formula I: 2. The compound according to claim 1 , wherein{'sup': 1', '2, 'R, Rare each independently hydrogen, a halogen atom, an aryl group, an aryloxy group, an arylthio group, a hetaryloxy group, a hetarylthio group or a dialkylamino group,'}m, n are each independently an integer of 0, 1 or 2,{'sup': '3', 'Ris an alkyl or aryl group,'}A is —COOM, and{'sub': 1', '6, 'Z is C-C-alkylene or 1,4-phenylene.'}4. The compound according to claim 3 , wherein{'sup': 1', '2, 'R, Rare each independently hydrogen, a halogen atom, an aryl group, an aryloxy group, an arylthio group, a hetaryloxy group, a hetarylthio group or a dialkylamino group,'}m, n are each independently of each other an integer of 0, 1 or 2,{'sup': '3', 'Ris an alkyl or aryl group,'}A is —COOM, and{'sub': 1', '6, 'Z is C-C-alkylene or 1,4-phenylene.'}6. The compound according to claim 5 ,wherein{'sup': 1', '2, 'R, Rare each independently hydrogen, a halogen atom, an aryl group, an aryloxy group, an arylthio group, a hetaryloxy group, a hetarylthio group or a dialkylamino group,'}m, n are each independently an integer of 0, 1 or 2,{'sup': '3', 'Ris an alkyl or aryl group,'}A is —COOM, and{'sub': 1', '6, 'Z is C-C-alkylene or 1,4-phenylene.'}10. The compound according to claim 9 , wherein{'sup': 1', '2, 'R, Rare each independently hydrogen, a halogen atom, an aryl group, an aryloxy group, an arylthio group, a hetaryloxy group, a hetarylthio group or a dialkylamino group,'}m, n are each independently an integer of 0, 1 or 2, and{'sup': '3', 'Ris an alkyl or aryl group.'}11. A sensitizer in a dye-sensitized solar cell claim 9 , comprising{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the compound according to .'}12. A dye-sensitized solar cell claim 9 , comprising{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the compound according to .'}15. A sensitizer in a dye-sensitized solar cell claim 9 , comprising{'claim-ref': {'@idref': 'CLM-00003', ' ...

Organic electroluminescent compound and organic electroluminescent device comprising the same

The present disclosure relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. By comprising the organic electroluminescent compound of the present disclosure, an organic electroluminescent device having improved driving voltage, luminous efficiency, and/or lifespan characteristics can be provided.

COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR MODULATING SGK ACTIVITY, AND METHODS THEREOF

The invention provides novel chemical compounds useful for treating one or more of autoimmune diseases, cancer, cardiovascular diseases, inflammatory diseases and diabetes, or a related disease or disorder thereof, and pharmaceutical composition and methods of preparation and use thereof. 4. The compound of claim 1 , wherein Y claim 1 , Yand Yare selected from the group consisting of:{'sub': 1', '1', '2', '2', '3', '3, 'Y=CR, Y=CR, Y=CR;'}{'sub': 1', '1', '2', '3', '3, 'Y=CR, Y=N, Y=CR;'}{'sub': 1', '1', '2', '2', '3, 'Y=CR, Y=CR, Y=N;'}{'sub': 1', '2', '3', '3, 'Y=N, Y=N, Y=CR; and'}{'sub': 1', '2', '2', '3, 'Y=N, Y=CR, Y=N.'}5. (canceled)7. The compound of claim 1 , wherein Zand Zare selected from the group consisting of:{'sub': 1', '2, 'Z=Z=CR;'}{'sub': 1', '2, 'Z=Z=N;'}{'sub': 1', '2, 'Z=N, Z=CR; and'}{'sub': 1', '2, 'Z=CR, Z=N,'}wherein each R is H.8. (canceled)11. The compound of claim 9 , wherein X is F or Cl claim 9 , R=R=R=H claim 9 , Ris NH claim 9 , Ris OR claim 9 , wherein Ris a hydrogen or a C-Calkyl group.12. The compound of claim 9 , wherein at least one of Zand Zis N.13. The compound of claim 9 , wherein at least one of Yand Yis not N.15. The compound of claim 14 , wherein X is F claim 14 , Ris CH claim 14 , Yis CH claim 14 , Yis N claim 14 , and Ris a C-Calkyl group.16. (canceled)17. The compound of claim 14 , wherein X is F claim 14 , Ris CH claim 14 , Yis N claim 14 , Yis CH claim 14 , and Ris a C-Calkyl group.18. (canceled)19. The compound of claim 14 , wherein X is F claim 14 , Ris CH claim 14 , Yis CH claim 14 , Yis CH claim 14 , and Ris a C-Calkyl group.20. (canceled)22. (canceled)23. (canceled)2530-. (canceled)31. A unit dosage form comprising a pharmaceutical composition according to .3338-. (canceled)39. The method of claim 32 , wherein the compound effectively inhibits serum and glucocorticoid-regulated kinase (SGK) 1 and/or 2. This application claims the benefit of U.S. Provisional Application No. 62/431,203, filed Dec. 7, 2016, the ...

POLYCYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

A polycyclic compound and an organic light-emitting device, the compound being represented by Formula 1: 2. The polycyclic compound as claimed in claim 1 , wherein Lis:a phenylene group, a pentalenylene group, an indenylene group, a naphthylene group, an azulenylene group, a heptalenylene group, an indacenylene group, an acenaphthylene group, a fluorenylene group, a spiro-bifluorenylene group, a spiro-fluorene-benzofluorenylene group, a benzofluorenylene group, a dibenzofluorenylene group, a phenalenylene group, a phenanthrenylene group, an anthracenylene group, a fluoranthenylene group, a triphenylenylene group, a pyrenylene group, a chrysenylene group, a naphthacenylene group, a picenylene group, a perylenylene group, a pentaphenylene group, a hexacenylene group, a pentacenylene group, a rubicenylene group, a coronenylene group, an ovalenylene group, a pyrrolylene group, a thiophenylene group, a furanylene group, an imidazolylene group, a pyrazolylene group, a thiazolylene group, an isothiazolylene group, an oxazolylene group, an isoxazolylene group, a pyridinylene group, a pyrazinylene group, a pyrimidinylene group, a pyridazinylene group, an isoindolylene group, an indolylene group, an indazolylene group, a purinylene group, a quinolinylene group, an isoquinolinylene group, a benzoquinolinylene group, a phthalazinylene group, a naphthyridinylene group, a quinoxalinylene group, a quinazolinylene group, a cinnolinylene group, a carbazolylene group, a phenanthridinylene group, an acridinylene group, a phenanthrolinylene group, a phenazinylene group, a benzimidazolylene group, a benzofuranylene group, a benzothiophenylene group, an isobenzothiazolylene group, a benzoxazolylene group, an isobenzoxazolylene group, a triazolylene group, a tetrazolylene group, an oxadiazolylene group, a triazinylene group, a dibenzofuranylene group, a dibenzothiophenylene group, a dibenzosilolylene group, a benzocarbazolylene group, a dibenzocarbazolylene group, a thiadiazolylene group, ...

Inhibitors of Viral Replication, Their Process of Preparation and Their Therapeutical Uses

The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.

TRICYCLIC COMPOUND

The present invention provides a compound having a superior serotonin 5-HTreceptor activating action. 3. The compound or salt of claim 1 , wherein n is 0.4. The compound or salt of claim 2 , wherein n is 0 claim 2 , and Y claim 2 , Yand Yare all carbon atoms.5. The compound or salt of claim 2 , wherein Ris a halogen atom or an alkyl group optionally having substituent(s).6. The compound or salt of claim 1 , wherein X is —N(R)—.7. (2aS)-9-Chloro-1-isopropyl-2 claim 1 ,2a claim 1 ,3 claim 1 ,4 claim 1 ,5 claim 1 ,6-hexahydro-1H-azepino[3 claim 1 ,4 claim 1 ,5-cd]indole claim 1 , or a salt thereof.8. 9-Chloro-2 claim 1 ,2a claim 1 ,3 claim 1 ,4 claim 1 ,5 claim 1 ,6-hexahydro-1H-azepino[3 claim 1 ,4 claim 1 ,5-cd]indole claim 1 , or a salt thereof.9. 9-Isopropyl-1-methyl-2 claim 1 ,2a claim 1 ,3 claim 1 ,4 claim 1 ,5 claim 1 ,6-hexahydro-1H-azepino[3 claim 1 ,4 claim 1 ,5-cd]indole claim 1 , or a salt thereof.10. A medicament comprising the compound or salt of .11. The medicament of claim 10 , which is a serotonin 5-HTreceptor activator.12. The medicament of claim 10 , which is an agent for the prophylaxis or treatment of lower urinary tract symptom claim 10 , obesity and/or organ prolapse.13. A method of activating serotonin 5-HTreceptor claim 1 , which comprises administering an effective amount of the compound or salt of to a mammal.14. A method for the prophylaxis or treatment of lower urinary tract symptom claim 1 , obesity and/or organ prolapse claim 1 , which comprises administering an effective amount of the compound or salt of to a mammal.1516-. (canceled) The present invention relates to a tricyclic compound having a superior serotonin 5-HTreceptor activating action and useful as an agent for treatment or the prophylaxis of a lower urinary tract symptom, obesity and/or organ prolapse etc., and the like.Serotonin 5-HTreceptor is one of the receptors of the biological transmitter serotonin, which is distributed mainly in the central nervous system and controls ...

2- (TERT - BUTOXY) -2- (7 -METHYLQUINOLIN- 6 - YL) ACETIC ACID DERIVATIVES FOR TREATING AIDS

The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein. 5. A pharmaceutical composition comprising a compound as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.6. A method of treating an HIV infection in a patient in need thereof comprising administering a compound as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , to the patient.7. A method of treating an HIV infection in a patient in need thereof comprising administering to the patient a therapeutically effective amount of a compound as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with a therapeutically effective amount of one or more additional therapeutic agents selected from the group consisting of HIV protease inhibiting compounds claim 1 , HIV non-nucleoside inhibitors of reverse transcriptase claim 1 , HIV nucleoside inhibitors of reverse transcriptase claim 1 , HIV nucleotide inhibitors of reverse transcriptase claim 1 , HIV integrase inhibitors claim 1 , gp41 inhibitors claim 1 , CXCR4 inhibitors claim 1 , gp120 inhibitors claim 1 , CCR5 inhibitors claim 1 , capsid polymerization inhibitors claim 1 , and other drugs for treating HIV.811-. (canceled)12. A pharmaceutical composition comprising a compound as described in claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , and a pharmaceutically acceptable carrier.13. A method of treating an HIV infection in a patient in need thereof comprising administering a compound as ...

Plurality of host materials and organic electroluminescent device comprising the same

The present disclosure relates to a plurality of host materials comprising a first host material comprising a compound represented by formula 1 and a second host material comprising a compound represented by formula 2 and an organic electroluminescent device comprising the same. By comprising the host materials according to the present disclosure, an organic electroluminescent device having low driving voltage and/or high luminous efficiency and/or long lifespan can be provided.

CYANATED BENZOXANTHENE AND BENZOTHIOXANTHENE COMPOUNDS

Disclosed herein are cyanated compounds of the formula (I) wherein at least one of the radicals R, R, Rand Ris CN, and the remaining radicals are selected from hydrogen, chlorine and bromine; X is O, S, SO or SO; m is 0, 1, 2, 3 or 4; 10 is selected from bromine, chlorine, cyano, —NRR, C-C-alkyl, C-C-haloalkyl, C-C-alkoxy, C-C-haloalkoxy, C-C-cycloalkyl, heterocycloalkyl, heteroaryl, C-C-aryl, C-C-aryloxy, C-C-aryl-C-C-alkylene, etc.; A is a diradical selected from diradicals of the general formulae (A.1), (A.2), (A.3), and (A.4) wherein R, (R), (R)and (R)are as defined in the claims and in the description. Also disclosed are color converters containing at least one polymer as a matrix material and at least one cyanated compound of formula (I) or mixtures thereof as a fluorescent dye, the use of the color converters, and lighting devices containing an LED and at least one color converter. 2. The cyanated compound of formula (I) according to claim 1 , wherein X is O or S.3. The cyanated compound of formula (I) according to claim 1 , wherein Rand Rare each cyano claim 1 , and Rand Rare each hydrogen.4. The cyanated compound of formula (I) according to claim 1 , wherein A is a radical of the formula (A.2).7. The cyanated compound according to claim 1 , wherein m is zero or one.8. A color converter claim 1 ,. comprising at least one polymer as a matrix and at least one cyanated compound of or a mixture thereof as a fluorescent dye claim 1 ,wherein the at least one polymer comprises a polystyrene, a polycarbonate, a polymethylmethacrylate, a polyvinylpyrrolidone, a polymethacrylate, a polyvinyl acetate, a polyvinyl chloride, a polybutene, a silicone, a polyacrylate, an epoxy resin, a polyvinyl alcohol, a poly(ethylene vinylalcohol)-coplymer (EVA, EVOH), a polyacrylonitrile, a polyvinylidene chloride (PVDC), a polystyreneacrylonitrile (SAN), a polybutylene terephthalate (PBT), a polyethylene terephthalate (PET), a polyvinyl butyrate (PVB), a polyvinyl chloride (PVC), a ...

SPIROQUINOXALINE DERIVATIVES AS INHIBITORS OF NON-APOPTOTIC REGULATED CELL-DEATH

The present invention relates to compounds which are inhibitors of non-apoptotic regulated cell death, and to pharmaceutical compositions containing such compounds. Furthermore, the present invention relates to the use of such compounds and pharmaceutical compositions in therapy, in particular in the treatment of a condition, disorder or disease that is characterised by non-apoptotic regulated cell-death or where non-apoptotic regulated cell-death is likely to play or plays a substantial role. The compounds and pharmaceutical compositions described herein are also useful in the treatment of a condition, disorder or disease that is characterised by oxidative stress or where oxidative stress is likely to play or plays a substantial role; and/or a condition, disorder or disease that is characterised by activation of (1) one or more components of the necrosome; (2) death domain receptors; and/or (3) Toll-like receptors; and/or (4) players in ferroptotic/ferroptosis signalling, or where activation of any one of (1) to (3) and/or (4) is likely to play or plays a substantial role. 152.-. (canceled)54. The method of claim 53 , wherein ring A is a monocyclic 4- to 10-membered N-heterocycloalkylene.56. The method of claim 53 , wherein ring A is saturated.57. The method of claim 53 , wherein ring A contains 1 ring nitrogen atom and is 4- to 8-membered or contains 2 or 3 ring nitrogen atoms and is 5- to 8-membered claim 53 , preferably ring A is 5- claim 53 , 6- or 7-membered claim 53 , more preferably 6- or 7-membered.58. The method claim 53 , wherein ring A is selected from the group consisting of piperidinylene claim 53 , azepanylene (e.g. claim 53 , homopiperidinylene) claim 53 , azetidinylene claim 53 , pyrrolidinylene claim 53 , azocanylene claim 53 , pyrazolidinylene claim 53 , hexahydropyridazinylene claim 53 , hexahydropyrimidinylene claim 53 , diazepanylene (e.g. claim 53 , homopiperazinylene) claim 53 , diazocanylene claim 53 , triazepanylene claim 53 , and ...

NITROGEN-CONTAINING HETEROCYCLES FOR USE IN OLEDS

The present invention describes nitrogen-containing heterocycles substituted by carbazole groups, especially for use in electronic devices. The invention further relates to a process for preparing the compounds of the invention and to electronic devices comprising these. 10. Compound according to claim 2 , characterized in that not more than four X groups are N.11. Oligomer claim 1 , polymer or dendrimer containing one or more compounds according to claim 1 , wherein claim 1 , rather than a hydrogen atom or a substituent claim 1 , there are one or more bonds of the compounds to the polymer claim 1 , oligomer or dendrimer.12. Composition comprising at least one compound according to and at least one further compound selected from the group consisting of fluorescent emitters claim 1 , phosphorescent emitters claim 1 , emitters that exhibit TADF claim 1 , host materials claim 1 , electron transport materials claim 1 , electron injection materials claim 1 , hole conductor materials claim 1 , hole injection materials claim 1 , electron blocker materials and hole blocker materials.13. Formulation comprising at least one compound according to and at least one solvent.14. Use of a compound according to claim 1 , in an electronic device.15. Process for preparing a compound according to claim 1 , characterized in that claim 1 , in a coupling reaction claim 1 , a compound comprising at least one nitrogen-containing heterocyclic group is joined a compound comprising at least one carbazole group.16. Electronic device comprising at least one compound according to claim 1 , wherein the electronic device is selected from the group consisting of organic electroluminescent devices claim 1 , organic integrated circuits claim 1 , organic field-effect transistors claim 1 , organic thin-film transistors claim 1 , organic light-emitting transistors claim 1 , organic solar cells claim 1 , organic optical detectors claim 1 , organic photoreceptors claim 1 , organic field quench devices ...

THERAPEUTIC COMPOUNDS

The invention provides compounds of formula I: 137-. (canceled)39. The compound of claim 38 , or a pharmaceutically acceptable salt thereof claim 38 , wherein{'sup': 5a', '11', '11', '9', '10', '9', '10, 'sub': 1', '6', '3', '7', '1', '6, 'Ris H, (C-C)alkyl, (C-C)carbocycle, -(C-C)alkyl-R, —C(═O)—R, —N(R)R, —C(═O)—N(R)R, heterocycle or heteroaryl,'}{'sup': '11', 'wherein heterocycle or heteroaryl is optionally substituted with 1 to 3 Zgroups, and'}{'sup': '5b', 'sub': 2', '6', '3', '7, 'wherein Ris -(C-C)alkynyl-(C-C)carbocycle.'}41. The compound of claim 38 , or a pharmaceutically acceptable salt thereof claim 38 , wherein Ris —OC(CH).42. A pharmaceutical composition comprising a compound according to claim 38 , or a pharmaceutically acceptable salt thereof claim 38 , and a pharmaceutically acceptable carrier.43. A method of treating HIV infection in a patient in need thereof comprising administering a compound as described in claim 38 , or pharmaceutically acceptable salt thereof claim 38 , to the patient.44. A method for treating an HIV infection in a patient in need thereof comprising administering to the patient a compound as described in claim 38 , or a pharmaceutically acceptable salt thereof claim 38 , in combination with one or more additional therapeutic agents selected from the group consisting of HIV protease inhibiting compounds claim 38 , HIV non-nucleoside inhibitors of reverse transcriptase claim 38 , HIV nucleoside inhibitors of reverse transcriptase claim 38 , HIV nucleotide inhibitors of reverse transcriptase claim 38 , HIV integrase inhibitors claim 38 , gp41 inhibitors claim 38 , CXCRinhibitors claim 38 , gp120 inhibitors claim 38 , CCRinhibitors claim 38 , capsid polymerization inhibitors claim 38 , and other drugs for treating HIV claim 38 , and combinations thereof. This patent application claims the benefit of priority of U.S. application Ser. No. 61/477922, filed Apr. 21, 2011, which application is hereby incorporated by reference.Human ...

Indolo heptamyl oxime analogue as parp inhibitor

Disclosed is a type of indolo heptamyl oxime compounds as a PARP inhibitor. Specifically disclosed are a compound as represented by formula (II) and a pharmaceutically acceptable salt thereof.

FLUORESCENT MONOMERS AND TAGGED TREATMENT POLYMERS CONTAINING SAME FOR USE IN INDUSTRIAL WATER SYSTEMS

The invention is directed towards methods and compositions for making and using fluorescent monomers which are synthesized by reacting a substituted or non-substituted benzoxanthene anhydride with an amine and with a moiety containing a polymerizable group. Such monomers are useful for the preparation of tagged treatment polymers. Such tagged treatment polymers are useful as scale inhibitors in industrial water systems. 2. The method of in which Q is acrylic acid and W is acrylamide.3. The method of in which Q is acrylamide claim 1 , W is acrylic acid claim 1 , and S is N-sulfomethylacrylamide.4. The method of in which Q is acrylic acid and W is acrylamidomethylpropane sulfonic acid.5. The method of in which U is sulfonated —N-(3-N′ claim 1 ,N′-Dimethylaminopropyl)benzo(k claim 1 ,l)xanthene-3 claim 1 ,4-dicarboxylic imide claim 1 , 2-hydroxy-3-allyloxypropyl quaternary salt claim 1 , Q is acrylic acid claim 1 , W is acrylamide and S is N sulfomethylacrylamide.6. The method of in which U is sulfonated —N-(3-N′ claim 1 ,N′-Dimethylaminopropyl)benzo(k claim 1 ,l)xanthene-3 claim 1 ,4-dicarboxylic imide claim 1 , vinyl benzyl chloride quaternary salt claim 1 , Q is acrylic acid claim 1 , W is acrylamide and S is N sulfomethylacrylamide.7. The method of in which G is sulfonated —N-(3-N′ claim 1 ,N′-Dimethylaminopropyl)benzo(k claim 1 ,l)xanthene-3 claim 1 ,4-dicarboxylic imide claim 1 , allyl chloride quaternary salt claim 1 , Q is acrylic acid claim 1 , W is acrylamide and S is N sulfomethylacrylamide.8. The method of in which G is sulfonated —N-(3-N′ claim 1 ,N′-Dimethylaminopropyl)benzo(k claim 1 ,l)xanthene-3 claim 1 ,4-dicarboxylic imide claim 1 , 2-hydroxy-3-allyloxypropyl quaternary salt claim 1 , Q is acrylic acid claim 1 , W is acrylamidomethylpropane sulfonic acid.9. The method of in which U is sulfonated —N-(3-N′ claim 1 ,N′-Dimethylaminopropyl)benzo(k claim 1 ,l)xanthene-3 claim 1 ,4-dicarboxylic imide claim 1 , vinyl benzyl chloride quaternary salt claim 1 ...

NAPHTHALENE ACETIC ACID DERIVATIVES AGAINST HIV INFECTION

The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein. 9. A pharmaceutical composition comprising a compound as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.10. A method of treating an HIV infection in a patient in need thereof comprising administering a compound as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , to the patient.11. A method of treating an HIV infection in a patient in need thereof comprising administering to the patient a therapeutically effective amount of a compound as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with a therapeutically effective amount of one or more additional therapeutic agents selected from the group consisting of HIV protease inhibiting compounds claim 1 , HIV non-nucleoside inhibitors of reverse transcriptase claim 1 , HIV nucleoside inhibitors of reverse transcriptase claim 1 , HIV nucleotide inhibitors of reverse transcriptase claim 1 , HIV integrase inhibitors claim 1 , gp41 inhibitors claim 1 , CXCR4 inhibitors claim 1 , gp120 inhibitors claim 1 , CCR5 inhibitors claim 1 , capsid polymerization inhibitors claim 1 , and other drugs for treating HIV.1215-. (canceled)16. A pharmaceutical composition comprising a compound as described in claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , and a pharmaceutically acceptable carrier.17. A method of treating an HIV infection in a patient in need thereof comprising administering a compound as ...

ORGANIC ELECTROLUMINESCENT COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME

The present disclosure relates to an organic electroluminescent compound represented by formula 1 and an organic electroluminescent device comprising the same. By comprising the organic electroluminescent compound of the present disclosure, it is possible to provide an organic electroluminescent device having improved operating voltage, luminous efficiency, lifetime, and/or power efficiency. 2. The organic electroluminescent compound according to claim 1 , wherein Bto B claim 1 , each independently claim 1 , are not present or represent a substituted or unsubstituted benzene ring claim 1 , a substituted or unsubstituted naphthalene ring claim 1 , a substituted or unsubstituted pyrrole ring claim 1 , a substituted or unsubstituted furan ring claim 1 , a substituted or unsubstituted thiophene ring claim 1 , a substituted or unsubstituted cyclopentadiene ring claim 1 , a substituted or unsubstituted fluorene ring claim 1 , a substituted or unsubstituted pyridine ring claim 1 , or a substituted or unsubstituted dibenzofuran ring; with the proviso that at least five of Bto Bare present claim 1 , and the adjacent rings of Bto Bare fused with each other.5. The organic electroluminescent compound according to claim 3 , wherein the substituents of the substituted (C1-C30)alkyl(ene) claim 3 , the substituted (C6-C30)aryl(ene) claim 3 , the substituted (3- to 30-membered)heteroaryl(ene) claim 3 , and the substituted (C3-C30)cycloalkyl(ene) in Ar claim 3 , L claim 3 , Rto R claim 3 , and R claim 3 , each independently claim 3 , are at least one selected from the group consisting of deuterium; a halogen; a cyano; a carboxyl; a nitro; a hydroxyl; a (C1-C30)alkyl; a halo(C1-C30)alkyl; a (C2-C30)alkenyl; a (C2-C30)alkynyl; a (C1-C30)alkoxy; a (C1-C30)alkylthio; a (C3-C30)cycloalkyl; a (C3-C30)cycloalkenyl; a (3- to 7-membered)heterocycloalkyl; a (C6-C30)aryloxy; a (C6-C30)arylthio; a (C6-C30)aryl unsubstituted or substituted with at least one selected from the group consisting of ...

Heterocycle Amido Alkyloxy Substituted Quinazoline Derivative and Use Thereof

Heterocycle amino alkyloxy substituted quinazoline derivatives as represented by the structural Formula (I) and pharmaceutically acceptable salts thereof, capable of inhibiting the activity of receptor tyrosine kinase EGFR, and being used to treat cancers related to the expression of the receptor tyrosine kinase of the ErbB family are provided. 8. The heterocycle amino alkyloxy substituted quinazoline derivatives according to claim 6 , wherein the said group Ris phenyl having one or several substituents selected from halogen claim 6 , alkyl claim 6 , alkenyl and alkynyl.9. The heterocycle amino alkyloxy substituted quinazoline derivatives according to claim 6 , wherein the said group Ris aromatic heterocyclyl having one or several substituents selected from halogen claim 6 , alkyl claim 6 , alkenyl and alkynyl.13. The heterocycle amino alkyloxy substituted quinazoline derivatives according to claim 11 , wherein the said m claim 11 , o claim 11 , p and q are integers each independently selected from 0 to 6.14. The heterocycle amino alkyloxy substituted quinazoline derivatives according to claim 11 , wherein the said n is an integer from 2 to 4.15. The heterocycle amino alkyloxy substituted quinazoline derivatives according to claim 11 , wherein the said group Ris selected from methyl claim 11 , deuterated methyl claim 11 , ethyl claim 11 , deuterated ethyl claim 11 , trifluoromethyl claim 11 , methoxyethyl claim 11 , cyclopropyl or cyclopropyl methyl.16. The heterocycle amino alkyloxy substituted quinazoline derivatives according to claim 11 , wherein the said group Ris selected from phenyl bearing one or several substituents selected from halogen claim 11 , alkyl claim 11 , alkenyl and alkynyl claim 11 , or aromatic heterocyclyl bearing one or several substituents selected from halogen claim 11 , alkyl claim 11 , alkenyl and alkynyl.18. The heterocycle amino alkyloxy substituted quinazoline derivatives as defined in for use as medicament for a cancer selected from ...

THERAPEUTIC COMPOUNDS

Compounds disclosed herein including compounds of formula I′: 2. The compound of wherein the configuration of the —OC(CH)group as shown in formula I′ is the (S) stereochemistry.3. The compound of wherein Ris selected from aryl claim 1 , heterocycle and heteroaryl claim 1 , wherein any aryl claim 1 , heterocycle and heteroaryl of Ris optionally substituted with one or more halo or (C-C)alkyl.4. The compound wherein Ris selected from aryl and heterocycle claim 1 , wherein any aryl and heterocycle of Ris optionally substituted with one or more chloro claim 1 , fluoro or methyl.7. The compound of wherein A is phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle claim 1 , wherein any phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.8. The compound of wherein A is monocyclic N-heteroaryl claim 1 , wherein monocyclic N-heteroaryl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.9. The compound of wherein A is pyridinyl claim 1 , pyrimidinyl or pyrazinyl claim 1 , wherein pyridinyl claim 1 , pyrimidinyl or pyrazinyl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.10. The compound of wherein A is pyridinyl claim 1 , pyrimidinyl or pyrazinyl and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.11. The compound of wherein A and B together form a ...

ELECTROLUMINESCENT DEVICE

Provided is an electroluminescent device. The electroluminescent device includes an anode, a cathode, and an organic layer disposed between the anode and the cathode, wherein the organic layer at least comprises a first compound having a structure of H-L-Arand a second compound having a structure of H-L-Ar. These new compound combinations can be used as host materials in electroluminescent devices. These new compound combinations can greatly improve the lifetime of the device and provide the device with better performance. Further provided is a display assembly including the electroluminescent device. 2. The electroluminescent device of claim 1 , wherein in Formula 1 claim 1 , the ring A claim 1 , the ring B claim 1 , and the ring C are claim 1 , at each occurrence identically or differently claim 1 , selected from a 5-membered carbocyclic ring claim 1 , an aromatic ring having 6 to 18 carbon atoms or a heteroaromatic ring having 3 to 18 carbon atoms;preferably, the ring A, the ring B, and the ring C are, at each occurrence identically or differently, selected from a 5-membered carbocyclic ring, a benzene ring, a 5-membered heteroaromatic ring or a 6-membered heteroaromatic ring.4. The electroluminescent device of claim 1 , wherein at least one of R and Ris selected from deuterium claim 1 , substituted or unsubstituted aryl having 6 to 30 carbon atoms or substituted or unsubstituted heteroaryl having 3 to 30 carbon atoms;{'sub': 'x', 'preferably, at least one of R and Ris selected from deuterium, phenyl, biphenyl or pyridyl.'}5. The electroluminescent device of claim 3 , wherein at least one of groups of adjacent substituents: adjacent substituents R in Ato A claim 3 , adjacent substituents Rin Xto X claim 3 , adjacent substituents Rin Xto Xor adjacent substituents Rin Xto Xis joined to form a ring.7. The electroluminescent device of claim 1 , wherein in Formula 2 claim 1 , two substituents Rin Zand Zare joined to form a ring claim 1 , and the ring has at least 6 ...

Compounds And Methods For Treating Fibrotic Pathologies

The present application provides methods for treating or preventing diseases and conditions associated with tissue fibrosis. 3. (canceled)4. The compound of claim 1 , wherein Ris 5-6-membered heteroaryl ring comprising 1 or 2 heteroatoms selected from N claim 1 , O claim 1 , and S claim 1 , which is optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from R.5. The compound of claim 1 , wherein Ris selected from pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , diazinyl claim 1 , triazinyl claim 1 , tetrazinyl claim 1 , and pentazinyl claim 1 , each of which is optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from R.6. (canceled)7. The compound of claim 1 , wherein Ris pyridinyl claim 1 ,{'sup': '2', 'optionally substituted with 1, 2, or 3 substituents independently selected from R.'}10. (canceled)11. The compound of claim 1 , wherein Ris 3-7-membered heterocycloalkyl ring comprising 1 or 2 heteroatoms selected from N claim 1 , O claim 1 , and S claim 1 , which is optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from R.12. The compound of claim 11 , wherein Ris selected from tetrahydropyranyl claim 11 , piperidinyl claim 11 , tetrahydrofuranyl claim 11 , pyrrolidinyl claim 11 , pyranyl claim 11 , morpholinyl claim 11 , oxazinyl claim 11 , dioxanyl claim 11 , dioxinyl claim 11 , diazinanyl claim 11 , triazinanyl claim 11 , trioxanyl claim 11 , azepanyl claim 11 , azepinyl claim 11 , oxepanyl claim 11 , oxepinyl claim 11 , diazepanyl claim 11 , diazepinyl claim 11 , azocanyl claim 11 , azocinyl claim 11 , oxocanyl claim 11 , oxocinyl claim 11 , azonanyl claim 11 , azoninyl claim 11 , oxonanyl claim 11 , and oxoninyl claim 11 , each of which is optionally substituted with 1 claim 11 , 2 claim 11 , or 3 substituents independently selected from R.13. (canceled)14. The compound of claim 11 , wherein Ris tetrahydropyranyl claim 11 , ...

THERAPEUTIC COMPOUNDS

Compounds of formula I′: 2. The compound of wherein A is phenyl claim 1 , monocyclic heteroaryl or monocyclic heterocycle wherein any phenyl claim 1 , monocyclic heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.3. The compound of wherein A is phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle wherein any phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.4. The compound of wherein A is monocyclic N-heteroaryl claim 1 , wherein monocyclic N-heteroaryl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.5. The compound of wherein A is pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridinyl-2-one claim 1 , tetrahydropyrimidinyl-2-one claim 1 , imidazolidinyl-2-one claim 1 , pyrrolidinyl-2-one or pyrrolidinyl claim 1 , wherein pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridinyl-2-one claim 1 , tetrahydropyrimidinyl-2-one claim 1 , imidazolidinyl-2-one claim 1 , pyrrolidinyl-2-one or pyrrolidinyl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.6. The compound of wherein B is phenyl claim 1 , pyridinyl claim 1 , pyrazolyl claim 1 , pyrimidinyl claim 1 , indazolyl claim 1 , pyrazolopyridine or benzimidazolyl claim 1 , wherein any ...

COVALENT INHIBITORS OF CDK-7

The disclosure includes compounds of Formula (I) 5. The method according to claim 4 , wherein Ris H claim 4 , —CH claim 4 , or CH—N(CH)CH; Ris H claim 4 , CH claim 4 , CF claim 4 , CN claim 4 , or halo.9. The method of claim 1 , wherein the neoplastic disease is lung cancer claim 1 , head and neck cancer claim 1 , central nervous system cancer claim 1 , prostate cancer claim 1 , testicular cancer claim 1 , colorectal cancer claim 1 , pancreatic cancer claim 1 , liver cancer claim 1 , stomach cancer claim 1 , biliary tract cancer claim 1 , esophageal cancer claim 1 , gastrointestinal stromal tumor claim 1 , breast cancer claim 1 , cervical cancer claim 1 , ovarian cancer claim 1 , uterine cancer claim 1 , leukemia claim 1 , lymphomas claim 1 , multiple myeloma claim 1 , melanoma claim 1 , basal cell carcinoma claim 1 , squamous cell carcinoma claim 1 , bladder cancer claim 1 , renal cancer claim 1 , sarcoma claim 1 , mesothelioma claim 1 , thymoma claim 1 , myelodysplastic syndrome claim 1 , or myeloproliferative disease.10. The method of claim 1 , wherein the neoplastic disease is small cell lung cancer.15. The method according to claim 14 , wherein Ris H claim 14 , —CH claim 14 , or CH—N(CH)CH; Ris H claim 14 , CH claim 14 , CF claim 14 , CN claim 14 , or halo. This application is a continuation of International Patent Application No. PCT/US2016/021722, filed on Mar. 10, 2016, which claims the benefit of the filing date, under 35 U.S.C. 119(e), of U.S. Provisional Application No. 62/135,147 filed on Mar. 18, 2015. The entire contents of each of the aforementioned applications are incorporated herein by reference.The members of the cyclin-dependent kinase (CDK) family play critical regulatory roles in proliferation. There are currently 20 known mammalian CDKs. While CDK7-13 have been linked to transcription, only CDK1, 2, 4, and 6 show demonstrable association with the cell cycle. Unique among the mammalian CDKs, CDK7 has consolidated kinase activities, regulating ...

HIV REPLICATION INHIBITOR

The present invention provides a novel compound having an antiviral action, in particular, an HIV replication inhibiting action, as well as a pharmaceutical composition, in particular, an anti-HIV agent. 2. The compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris a hydrogen atom.3. The compound or pharmaceutically acceptable salt according to claim 1 , wherein n is 1.4. The compound or pharmaceutically acceptable salt according to claim 3 , wherein Ris substituted or unsubstituted alkyloxy.5. The compound or pharmaceutically acceptable salt according to claim 1 ,{'sup': 1', '11', '12', '12', '12', '12', '12', '13', '12', '12', '11', '12', '13', '12', '12', '12', '11', '12, 'sub': 2', '2', '2', '2, 'wherein Ris halogen, cyano, nitro, or —X—R(X is a single bond, —O—, —S—, —NR—, —CO—, —SO—, —O—CO—, —CO—O—, —NR—CO—, —CO—NR—, —NR—CO—O—, —NR—CO—NR—, —NR—SO—, or —SO—NR—; Ris a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, a substituted or unsubstituted aromatic carbocyclic group, a substituted or unsubstituted nonaromatic carbocyclic group, a substituted or unsubstituted aromatic heterocyclic group, or a substituted or unsubstituted nonaromatic heterocyclic group; Rand Rare each independently a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl. When X is —NR—, —CO—NR—, or —SO—NR—, Rand Rmay be taken together with an adjacent nitrogen atom to form a substituted or unsubstituted aromatic heterocyclic group, or a substituted or unsubstituted nonaromatic heterocyclic group),'}{'sup': 7', '71', '72', '72', '72', '72', '72', '73', '72', '72', '71', '72', '73', '72', '72', '72', '71', '72, 'sub': 2', '2', '2', '2, 'Ris halogen, cyano, nitro, or —Z—R(Z is a single bond, —O—, —S—, —NR—, —CO—, —SO—, —O—CO—, —CO—O—, —NR—CO—, —CO—NR—, —NR—CO—O—, —NR—CO—NR—, —NR—SO—, or —SO—NR—; Ris a hydrogen atom, ...

Heterocyclic Flavone Derivatives, Compositions, and Methods Related Thereto

In certain embodiments, the disclosure relates to heterocyclic flavone derivatives, such as those described by formula provided herein, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing diseases or conditions related to BDNF and TrkB activity, such as depression, stroke, Rett syndrome, Parkinson's disease, and Alzheimer's disease by administering effective amounts of pharmaceutical compositions comprising compounds disclosed herein. 1. A compound 8-(3 ,5-difluoro-4-(methylamino)phenyl)chromeno[8 ,7-d]imidazole-2 ,6(1H ,3H)-dione , derivative , prodrug , or salt thereof.2. A pharmaceutical preparation comprising the compound of and a pharmaceutically acceptable carrier.3. The pharmaceutical preparation of in the form of granules claim 2 , tablet claim 2 , capsule claim 2 , or pill.4. The pharmaceutical preparation of wherein the pharmaceutically acceptable carrier is selected from sucrose claim 2 , glucose claim 2 , dextrose claim 2 , lactose claim 2 , sorbitol claim 2 , or cellulose.5. The pharmaceutical preparation of wherein the pharmaceutically acceptable carrier is selected from dicalcium phosphate dihydrate claim 2 , calcium sulfate claim 2 , mannitol claim 2 , microcrystalline cellulose claim 2 , kaolin claim 2 , sodium chloride claim 2 , dry starch claim 2 , hydrolyzed starches claim 2 , pregelatinized starch claim 2 , silicone dioxide claim 2 , titanium oxide claim 2 , and magnesium aluminum silicate.6. The pharmaceutical preparation of wherein the pharmaceutically acceptable carrier is selected from polyethylene glycol claim 2 , wax claim 2 , acacia claim 2 , tragacanth claim 2 , sodium alginate.7. The pharmaceutical preparation of wherein the pharmaceutically acceptable carrier is selected from hydroxypropylmethylcellulose claim 2 , hydroxypropylcellulose claim 2 , and ethylcellulose.8. The pharmaceutical preparation of wherein the pharmaceutically acceptable ...

HETEROCYCLIC FLAVONE DERIVATIVES, COMPOSITIONS, AND METHODS RELATED THERETO

In certain embodiments, the disclosure relates to heterocyclic flavone derivatives, such as those described by formula provided herein, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of 5 treating or preventing diseases or conditions related to BDNF and TrkB activity, such as depression, stroke, Rett syndrome, Parkinson's disease, and Alzheimer's disease by administering effective amounts of pharmaceutical compositions comprising compounds disclosed herein to a subject in need thereof. 2. A compound of claim 1 , wherein X is O.3. The compound of claim 1 , wherein A is pyrrolidinyl.4. The compound of claim 1 , wherein Rand Rform imidazolyl or indolyl.6. The compound of claim 5 , wherein Ris hydrogen claim 5 , hydroxy claim 5 , or alkyl.7. The compound of wherein the compound is selected from:8-(4-(dimethylamino)phenyl)chromeno[7,8-d]imidazol-6(3H)-one,8-(4-(pyrrolidin-1-yl)phenyl)chromeno[7,8-d]imidazol-6(3H)-one,2-methyl-8-(4-(pyrrolidin-1-yl)phenyl)chromeno[7,8-d]imidazol-6(3H)-one, and2-(4-(pyrrolidin-1-yl)phenyl)pyrano[3,2-g]indol-4(9H)-one, or salts thereof.8. The compound of wherein the compound is selected from:8-(3,5-difluoro-4-(pyrrolidin-1-yl)phenyl)-2-methylchromeno[7,8-d]imidazol-6(3H)-one,2-chloro-8-(3,5-difluoro-4-(pyrrolidin-1-yl)phenyl)chromeno[7,8-d]imidazol-6(3H)-one,8-(3,5-difluoro-4-(pyrrolidin-1-yl)phenyl)chromeno[7,8-d]imidazole-2,6(1H,3H)-dione,8-(3,5-difluoro-4-(pyrrolidin1-yl)phenyl)-5-fluorochromeno[7,8-d]imidazole-2,6(1H,3H)-dione, and8-(2,6-difluoro-4-(pyrrolidin-1-yl)phenyl)-5-fluorochromeno[7,8-d]imidazole-2,6(1H,3H)-dione, or salts thereof.10. The compound of wherein the compound is selected from:8-(5-fluoro-6-(pyrrolidin-1-yl)pyridin-3-yl)chromeno[7,8-d]imidazole-2,6(1H,3H)-dione, and8-(5-fluoro-6-(pyrrolidin-1-yl)pyridin-3-yl)-2-methylchromeno[7,8-d]imidazol-6(3H)-one or salts thereof.11. A pharmaceutical composition comprising a compound of as in claim 10 , and a ...

MATERIALS FOR ORGANIC LIGHT EMITTING DEVICES

The present invention describes carbazole, dibenzofuran, dibenzothiophene and fluorene derivatives which are substituted by electron-deficient heteroaryl groups, in particular for use as triplet matrix materials in organic electroluminescent devices. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising these compounds. 115.-. (canceled)18. The compound according to claim 16 , wherein at least two groups X stand for N.19. The compound according to claim 16 , wherein Yand Ystand claim 16 , identically or differently on each occurrence claim 16 , for O claim 16 , NR claim 16 , where the radical R bonded to the nitrogen is not equal to H claim 16 , or S.20. The compound according to claim 16 , whereinX is, identically or differently on each occurrence, CR or N, where at least two groups X stand for N;{'sup': 1', '2, 'Y, Ystand, identically or differently on each occurrence, for O, NR, where the radical R bonded to the nitrogen is not equal to H, or S;'}{'sup': '3', 'sub': '2', 'Ystands for O, NR, where the radical R bonded to the nitrogen is not equal to H, or CR;'}L stands, identically or differently on each occurrence, for a single bond or an aromatic or heteroaromatic ring system having 5 to 24 aromatic ring atoms;Ar stands, identically or differently on each occurrence, for an aromatic or heteroaromatic ring system having 6 to 24 aromatic ring atoms, which is optionally substituted by one or more radicals R;n in formula (1a) or (2a) is, identically or differently on each occurrence, 0, 1, 2 or 3;m in formula (1a) or (2a) is, identically or differently on each occurrence, 0, 1 or 2;o in formula (1a) or (2a) is 0 or 1;{'sup': 1', '1', '1', '1', '1', '1', '1, 'sub': 2', '2', '2, 'R is selected, identically or differently on each occurrence, from the group consisting of H, D, F, CN, N(Ar), C(═O)Ar, P(═O)(Ar), a straight-chain alkyl or alkoxy group having 1 to 10 C atoms or a ...

PHENANTHRENE DERIVATIVES FOR USE AS MEDICAMENTS

The present invention refers to phenanthrene derivatives for use as medicaments, mainly in the prevention and/or treatment of Myotonic Dystrophy Type 1, Huntington's Disease Like 2, Spinocerebellar Ataxia Type 8, Myotonic Dystrophy Type 2, Spinocerebellar Ataxia Type 3, Fragile-X-Associated Tremor/Ataxia Syndrome, Frontotemporal Degeneration/Amyotrophic Lateral Sclerosis and Spinocerebellar Ataxia Type 31. In a preferred embodiment, phenanthrene derivatives of the invention are also used as antimyotonic agents. Therefore, this invention may be included either in the whole pharmaceutical or medical field. 2. (canceled)6. The method of claim 1 , wherein a pharmaceutical composition comprises the compound of Formula I claim 1 , derivatives claim 1 , or pharmaceutically acceptable salts thereof.7. (canceled)12. (canceled)14. (canceled) The present invention refers to phenanthrene derivatives for use as medicaments, mainly in the prevention and/or treatment of human diseases involving presence of toxic RNAs comprising: Myotonic Dystrophy Type 1 (DM1), Huntington's Disease Like 2 (HDL2), Spinocerebellar Ataxia Type 8 (SCA8), Myotonic Dystrophy Type 2 (DM2), Spinocerebellar Ataxia Type 3 (SCA3), Fragile-X-Associated Tremor/Ataxia Syndrome (FXTAS), Frontotemporal Degeneration/Amyotrophic Lateral Sclerosis (FTD/ALS), and Spinocerebellar Ataxia Type 31 (SCA31). In a preferred embodiment, said phenanthrene derivatives are used as antimyotonic agents. Therefore, this invention may be included either in the whole pharmaceutical or medical field.DM1, also called Dystrophia Myotonica or Steinert's disease, was described more than 100 years ago. DM1 displays an autosomal dominant mode of inheritance and is now recognized as one of the most common forms of muscular dystrophy in adults with a prevalence of 1:8,000-20,000 individuals worldwide (Harper P S. . London, UK: WB Saunders (2001)). The name myotonic dystrophy refers to two main muscle symptoms identified in this disease: ...

LIGHT HARVESTING ARRAY

The invention relates to a light harvesting array or dye comprising an acceptor linked to a donor, wherein at least one of the acceptor or the donor is an oligomeric unit comprising a first optionally substituted rylene linked via a linker group to a second optionally substituted rylene, the first optionally substituted rylene is linked to the acceptor or the donor and the second optionally substituted rylene is capable of energy transfer to at least one of the first optionally substituted rylene, the acceptor or the donor. The invention also relates to compounds which may be used as light harvesting arrays, methods for their manufacture, and devices and materials comprising the light harvesting array or dye, for example, chromophoric materials, light guides, photobioreactors, photoluminescent algae systems, photodetectors, photovoltaic devices and luminescent/fluorescent solar concentrators. 131.-. (canceled)32. A light harvesting array comprising an acceptor linked to a donor , wherein at least one of the acceptor or the donor is an oligomeric unit comprising a first optionally substituted rylene linked via a linker group to a second optionally substituted rylene , the first optionally substituted rylene is linked to the acceptor or the donor and the second optionally substituted rylene is capable of energy transfer to at least one of the first optionally substituted rylene , the acceptor or the donor.34. The light harvesting array of claim 32 , comprising an acceptor linked to one or more donors claim 32 , wherein the acceptor is an oligomeric unit comprising an optionally substituted rylene core linked via a linker group to one or more optionally substituted peripheral rylenes.35. The light harvesting array of claim 32 , comprising an acceptor linked to one or more donors claim 32 , wherein at least one donor is an oligomeric unit comprising an optionally substituted donor rylene core linked via a linker group to one or more optionally substituted peripheral ...

INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Compounds of formula I: 138-. (canceled)40. The method according to wherein Ris Het optionally substituted with 1 to 2 substituents each independently selected from halo claim 39 , (C)alkyl and —O(C)alkyl.41. The method according to wherein Ris Het optionally substituted with 1 to 2 substituents each independently selected from Cl claim 40 , F claim 40 , CHand CHCHwherein Het is a 7- to 14-membered saturated claim 40 , unsaturated or aromatic heteropolycycle having wherever possible 1 to 2 heteroatoms claim 40 , each independently selected from O claim 40 , N and S.44. The method according to wherein Ris H claim 39 , F claim 39 , Cl or (C)alkyl.45. The method according to wherein Ris H or CH.46. The method according to wherein Ris H claim 39 , F claim 39 , Cl or CH.47. The method according to wherein Ris H or CH.49. The method according to wherein the at least one other antiviral agent comprises at least one NNRTI.50. The method according to wherein the at least one other antiviral agent comprises at least one NRTI.51. The method according to wherein the at least one other antiviral agent comprises at least one protease inhibitor.52. The method according to wherein the at least one other antiviral agent comprises at least one entry inhibitor.53. The method according to wherein the at least one other antiviral agent comprises at least one integrase inhibitor. This application is a continuation of U.S. patent application Ser. No. 13/683,761, filed Nov. 21, 2012; which is a continuation of U.S. patent application Ser. No. 12/742,997, filed Aug. 19, 2010 (now U.S. Pat. No. 8,354,429); which is a 371 of PCT/CA2008/001611, filed Sep. 11, 2008; which claims the benefit of U.S. Application No. 60/988,686, filed Nov. 16, 2007. The foregoing applications are incorporated herein by reference in their entireties.The content of the following submission on ASClI text file is incorporated herein by reference in its entirety: a computer readable form (CRF) of the Sequence Listing ( ...

Use of Novel Coumarins as Glutathione and Thiol Labels

Fluorescent quinolizinocoumarin compounds substituted with electrophilic reactive groups that bind thiol compounds are described. The compounds are useful in detecting oxidative stress and processes associated therewith in live cells. 1. A 2 ,3 ,6 ,7-tetrahydro-9-halomethyl-1H ,5H-quinolizino(9 ,1-gh)coumarin.23-. (canceled)4. The 2 claim 1 ,3 claim 1 ,6 claim 1 ,7-tetrahydro-9-halomethyl-1H claim 1 ,5H-quinolizino(9 claim 1 ,1-gh)coumarin of claim 1 , further substituted with a cationic group.5. The 2 claim 1 ,3 claim 1 ,6 claim 1 ,7-tetrahydro-9-halomethyl-1H claim 1 ,5H-quinolizino(9 claim 1 ,1-gh)coumarin of claim 1 , wherein the cationic group comprises a triphenylphosphonium ion.710-. (canceled)11. The compound of claim 6 , wherein X is a substituted thiol group.1232-. (canceled)33. A method for detecting or quantifying intracellular glutathione levels in a sample claim 6 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) contacting the sample with a compound according to , to form a contacted sample;'}(b) incubating the contacted sample for an appropriate amount of time to form an incubated sample;(c) illuminating the incubated sample with an appropriate wavelength to form an illuminated sample; and(d) detecting fluorescent emissions from the illuminated sample;wherein the fluorescent emissions are used to detect or quantify the glutathione level in the sample.34. The method of claim 33 , wherein the sample comprises cells.35. The method of claim 33 , wherein the contacted sample is incubated for a sufficient amount of time for the compound to enter the cell.36. The method of claim 33 , wherein the sample comprises live cells claim 33 , intracellular fluids claim 33 , extracellular fluids claim 33 , sera claim 33 , biological fluids claim 33 , biological fermentation media claim 33 , environmental sample claim 33 , industrial samples claim 33 , proteins claim 33 , peptides claim 33 , buffer solutions biological fluids or chemical ...

Double donor functionalisation of the peri-positions of perylene and naphthalene monoimide via versatile building blocks

The present invention provides the compounds of formulae (3) and (1) wherein n is 0 or 1, R 13 and R 14 are the same or different and are selected from the group consisting of NHR 310 , NR 311 R 312 , OR 313 , SR 314 and R 315 , or R 13 and R 14 together are selected from the group consisting of (a), (b) and (c), and X is CI, Br of I, and a process for the preparation of compounds of formula (3) comprising the compounds of formula (1) as key intermediates.

TETRAZINE-CONTAINING COMPOUNDS AND SYNTHETIC METHODS THEREOF

Described herein are tetrazine derivatives and efficient synthetic methods of synthesis thereof using elimination-Heck cascade reaction. Provided herein is the synthesis of conjugated tetrazines from the tetrazine derivatives. Also provided herein are methods of use of the conjugated tetrazines as fluorogenic probes for live-cell imaging. 2. The method of claim 1 , wherein LG is an electron withdrawing group.3. The method of claim 1 , wherein:{'sub': 2', '2', '2', '2', '2', '2', '2, 'sup': +', '3A', '+', '3A', '+', '3B', '3C', '+', '3A', '3B', 'C', '+', '3A, 'LG is —N, —OR, —OSORF, a perfluoroalkylsulfonate, a tosylate, a mesylate, a halogen; —OH, —ONO, —OPO(OH), —ONO, —S(RR), —N(RRR), —OCOR, substituted or unsubstituted aryloxy or substituted or unsubstituted heteroaryloxy; and'}{'sup': 3A', '3B', '3C', '3B', '3C, 'sub': 3', '3', '3', '3', '2', '2', '2', '3', '4', '2', '2', '2', '2', '2', '2', '2', '3', '3', '3', '3', '2', '2', '2', '2, 'R, Rand Rare independently hydrogen, halogen, —CF, —CCl, —CBr, —CI, —OH, —NH, —COOH, —CONH, —NO, —SH, —SOH, —SOH, —SONH, —NHNH, —ONH, —NHC(O)NHNH, —NHC(O)NH, —NHSOH, —NHC(O)H, —NHC(O)—OH, —NHOH, —OCF, —OCCl, —OCBr, —OCI, —OCHF, —OCHC1, —OCHBr, —OCHI, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; Rand Rsubstituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl.'}4. The method of claim 1 , wherein the method further comprises a solvent.5. The method of claim 4 , wherein the solvent is an organic solvent.6. The method of claim 1 , wherein the method comprises an organic base.7. The method of claim 1 , wherein the method is conducted at a temperature of from about 25° C. to 200° C.8. The method of claim 1 , wherein the method is ...

PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS. 1. (canceled)2. A compound or salt of wherein Ris alkyl.3. A compound or salt of wherein Ris selected from hydroxyalkyl claim 9 , alkoxyalkyl claim 9 , (alkoxy)alkoxyalkyl claim 9 , ((alkoxy)alkoxy)alkoxyalkyl claim 9 , (oxetanyl)alkyl claim 9 , (tetrahydropyranyl)alkyl claim 9 , ((oxetanyl)oxy)alkyl claim 9 , ((tetrahydropyranyl)oxy)alkyl claim 9 , ((oxetanyl)alkoxy)alkyl claim 9 , ((tetrahydropyranyl)alkoxy)alkyl claim 9 , ((R)(R)N)alkyl claim 9 , or (R)(R)N.45-. (canceled)6. A compound or salt of wherein Ris tetrahydroisoquinolinyl substituted with 1 Rsubstituent.7. (canceled)8. A compound or salt of wherein Ris (Ar)alkyl or Ar.11. (canceled)12. A pharmaceutical composition comprising a compound or salt of .13. The composition of further comprising at least one other agent used for treatment of AIDS or HIV infection selected from nucleoside HIV reverse transcriptase inhibitors claim 12 , non-nucleoside HIV reverse transcriptase inhibitors claim 12 , HIV protease inhibitors claim 12 , HIV fusion inhibitors claim 12 , HIV attachment inhibitors claim 12 , CCR5 inhibitors claim 12 , CXCR4 inhibitors claim 12 , HIV budding or maturation inhibitors claim 12 , and HIV integrase inhibitors.14. The composition of wherein the other agent is dolutegravir.15. A method for treating HIV infection comprising administering a compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , to a patient in need thereof.16. The method of further comprising administering at least one other agent used for treatment of AIDS or HIV infection selected from nucleoside HIV reverse transcriptase inhibitors claim 15 , non-nucleoside HIV reverse transcriptase inhibitors claim 15 , HIV protease inhibitors claim 15 , HIV fusion ...

ORGANIC ELECTROLUMINESCENT COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME

The present disclosure relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. By using the organic electroluminescent compound of the present disclosure, it is possible to provide an organic electroluminescent device having low driving voltage and/or excellent power efficiency and/or improved driving lifespan. 2. The organic electroluminescent compound according to claim 1 , wherein the substituents of the substituted aryl(ene) claim 1 , the substituted heteroaryl(ene) claim 1 , the substituted alkyl claim 1 , and the substituted mono- or polycyclic claim 1 , alicyclic or aromatic ring claim 1 , or the combination thereof claim 1 , in L claim 1 , Ar claim 1 , Rto R claim 1 , and Rto R claim 1 , each independently claim 1 , are at least one selected from the group consisting of deuterium; a halogen; a cyano; a carboxyl; a nitro; a hydroxyl; a (C1-C30)alkyl; a halo(C1-C30)alkyl; a (C2-C30)alkenyl; a (C2-C30)alkynyl; a (C1-C30)alkoxy; a (C1-C30)alkylthio; a (C3-C30)cycloalkyl; a (C3-C30)cycloalkenyl; a (3- to 7-membered)heterocycloalkyl; a (C6-C30)aryloxy; a (C6-C30)arylthio; a (3- to 30-membered)heteroaryl unsubstituted or substituted with a (C1-C30)alkyl or a (C6-C30)aryl; a (C6-C30)aryl unsubstituted or substituted with a (3- to 30-membered)heteroaryl; a tri(C1-C30)alkylsilyl; a tri(C6-C30)arylsilyl; a di(C1-C30)alkyl(C6-C30)arylsilyl; a (C1-C30)alkyldi(C6-C30)arylsilyl; an amino; a mono- or di-(C1-C30)alkylamino; a mono- or di-(C6-C30)arylamino; a (C1-C30)alkyl(C6-C30)arylamino; a (C1-C30)alkylcarbonyl; a (C1-C30)alkoxycarbonyl; a (C6-C30)arylcarbonyl; a di(C6-C30)arylboronyl; a di(C1-C30)alkylboronyl; a (C1-C30)alkyl(C6-C30)arylboronyl; a (C6-C30)aryl(C1-C30)alkyl; and a (C1-C30)alkyl(C6-C30)aryl.3. The organic electroluminescent compound according to claim 1 , whereinL represents a single bond, a substituted or unsubstituted (C6-C25)arylene, or a substituted or unsubstituted (5- to 25-membered)heteroarylene ...

ORGANIC LIGHT EMITTING DEVICE AND COMPOUNDS FOR USE IN SAME

Specific polycyclic compounds of the general formula (I) and a process for its preparation, an electronic device comprising at least one of these compounds, an emitting layer, preferably present in an electronic device, comprising at least one compound of general formula (I) and the use of compounds according to general formula (I) in an electronic device as a host material, a charge transporting material, charge and/or exciton blocking material, preferably as a host material or an electron transporting material. 2. The polycyclic compound according to claim 1 , wherein Aris an unsubstituted or substituted C-Caryl group claim 1 , or an unsubstituted or substituted C-Cheteroaryl group.3. The polycyclic compound according to claim 1 , wherein Lis a direct bond claim 1 , an unsubstituted or substituted C-Carylene group claim 1 , or an unsubstituted or substituted C- Cheteroarylene group.4. The polycyclic compound according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare independently of each other hydrogen claim 1 , an unsubstituted or substituted C-Caryl group claim 1 , an unsubstituted or substituted C-Cheteroaryl group claim 1 , an unsubstituted or substituted C-Calkyl group claim 1 , —CN or halogen;wherein{'sup': 1', '2', '3', '4', '5', '6', '7', '8', '9', '10', '11', '12, 'sub': 6', '18, 'two of R, R, R, R, R, R, R, R, R, R, Rand R, if present at adjacent carbon atoms, together may form an unsubstituted or substituted C-Caryl ring.'}8. An electronic device comprising at least one compound as defined in .9. The electronic device according to claim 8 , comprising a cathode claim 8 , an anode claim 8 , and a plurality of organic thin film layers provided between the cathode and the anode claim 8 , the organic thin film layers comprising an emitting layer comprising the at least one compound of general formula (I).10. The electronic device ...

ISOINDOLINE DERIVATIVES FOR USE IN THE TREATMENT OF A VIRAL INFECTION

Compounds of Formula I are disclosed and methods of treating viral infections with compositions comprising such compounds. 2. A compound according to wherein Ris Calkyl.3. A compound according to wherein Ris t-butyl.4. A compound according to wherein Ris optionally substituted phenyl.5. A compound according to wherein Ris phenyl substituted by one to four substituents selected from fluorine claim 4 , methyl claim 4 , —CHCHCHO— wherein said —CHCHCHO— is bonded to adjacent carbon atoms on said phenyl to form a bicyclic ring claim 4 , or —NHCHCHO— wherein said —NHCHCHO— is bonded to adjacent carbon atoms on said phenyl to form a bicyclic ring.6. A compound according to wherein Ris Calkyl claim 1 , phenyl claim 1 , naphthyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , pyridyl claim 1 , or tetrahydropyranyl claim 1 , each of which is optionally substituted by 1-3 substituents selected from halogen claim 1 , Calkyl claim 1 , —OCalkyl claim 1 , Cfluoroalkyl claim 1 , or phenyl.11. A pharmaceutically acceptable salt of a compound according to .12. A pharmaceutical composition comprising a compound according to or a pharmaceutically acceptable salt thereof.13. A method for treating a viral infection in a patient mediated at least in part by a virus in the retrovirus family of viruses claim 12 , comprising administering to said patient a composition according to .14. The method of wherein said viral infection is mediated by the HIV virus.1517-. (canceled) The present invention relates to substituted isoindoline compounds, pharmaceutical compositions, and methods of use thereof for (i) inhibiting HIV replication in a subject infected with HIV, or (ii) treating a subject infected with HIV, by administering such compounds.Human immunodeficiency virus type 1 (HIV-1) leads to the contraction of acquired immune deficiency disease (AIDS). The number of cases of HIV continues to rise, and currently over twenty-five million individuals worldwide suffer from the virus. ...

Fluorescent monomers and tagged treatment polymers containing same for use in industrial water systems

The present disclosure relates to methods and compositions for making and using fluorescent monomers which are synthesized by reacting a substituted or non-substituted benzoxanthene anhydride with an amine and with a moiety containing a polymerizable group. Such monomers are useful for the preparation of tagged treatment polymers. Such tagged treatment polymers are useful as scale inhibitors in industrial water systems.

MATERIALS FOR ORGANIC LIGHT EMITTING DEVICES

The present invention describes carbazole, dibenzofuran, dibenzothiophene and fluorene derivatives which are substituted by electron-deficient heteroaryl groups, in particular for use as triplet matrix materials in organic electroluminescent devices. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising these compounds. 115.-. (canceled)17. The compound according to claim 16 , whereinn is 1 andm is on each occurrence 0.18. The compound according to claim 16 , wherein Yand Ystand claim 16 , identically or differently on each occurrence claim 16 , for O or S.19. The compound according to claim 16 , for which:Ar stands, identically or differently on each occurrence, for an aromatic or heteroaromatic ring system having 6 to 24 aromatic ring atoms, which may be substituted by one or more radicals R;{'sup': 1', '1', '1', '1', '1', '1', '1, 'sub': 2', '2', '2, 'R is selected, identically or differently on each occurrence, from the group consisting of H, D, F, CN, N(Ar), C(═O)Ar, P(═O)(Ar), a straight-chain alkyl or alkoxy group having 1 to 10 C atoms or a branched or cyclic alkyl or alkoxy group having 3 to 10 C atoms or an alkenyl group having 2 to 10 C atoms, each of which may be substituted by one or more radicals R, where one or more non-adjacent CHgroups may be replaced by O and where one or more H atoms may be replaced by D or F, an aromatic or heteroaromatic ring system having 5 to 24 aromatic ring atoms, which may in each case be substituted by one or more radicals R, or an aralkyl or heteroaralkyl group having 5 to 25 aromatic ring atoms, which may be substituted by one or more radicals R; two substituents R which are bonded to the same carbon atom or to adjacent carbon atoms may optionally form a monocyclic or polycyclic, aliphatic, aromatic or heteroaromatic ring system here, which may be substituted by one or more radicals R.'}20. The compound according to claim 16 , ...

COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

A compound is represented by one selected from Formulae 1 and 2:

Covalent inhibitors of cdk-7

The disclosure includes compounds of Formula (I) wherein R 0 , R 1 , R 2 , R 3 , R 4 , R 5 , and L are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.

POLYCYCLIC COMPOUND AND ORGANIC ELETROLUMINESCENCE DEVICE INCLUDING THE SAME

A polycyclic compound according to an embodiment of the inventive concept is represented by the following Formula 1: 5. The polycyclic compound of claim 1 ,wherein A is represented by Formula 2-1, and{'sub': 1', '2', '1', '2, 'Arand Arare each independently selected from substituted or unsubstituted phenyl group, substituted or unsubstituted anthracenyl group, substituted or unsubstituted pyrenyl group, substituted or unsubstituted phenanthryl group, substituted or unsubstituted chrysenyl group, substituted or unsubstituted triphenylenyl group, substituted or unsubstituted carbazolyl group, and substituted or unsubstituted pyridyl group, where Arand Aroptionally combine with each other to form a ring.'} This patent application claims priority to and the benefit of Korean Patent Application No. 10-2016-0056626, filed on May 9, 2016 in the Korean Intellectual Property Office (KIPO), the contents of which are incorporated herein by reference.One or more aspects of embodiments of the present disclosure herein relate to a polycyclic compound and an organic electroluminescence device including the same.Recently, the development of an organic electroluminescence display as an image display is being actively conducted. The organic electroluminescence display is different from a liquid crystal display in that it is a self-luminescent display capable of displaying images via the recombination of holes and electrons injected from a first electrode and a second electrode into an emission layer and the light emission via a luminescent material including an organic compound in the emission layer.An example organic electroluminescence device includes, for example, a first electrode, a hole transport layer disposed (e.g., positioned) on the first electrode, an emission layer disposed on the hole transport layer, an electron transport layer disposed on the emission layer, and a second electrode disposed on the electron transport layer. Holes are injected from the first electrode, ...

Novel antiviral compounds

The present invention relates to compounds of formula (A), as further defined herein, having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. The invention further relates to the use of such compounds, optionally combined with one or more other drugs having antiviral activity, for the treatment of animals suffering from viral infections, in particular HIV infection.

Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use

including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2, L, W1, W2, X, Y, and Z are as defined herein. Methods associated with the preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

MACROCYCLIC BENZOFURAN AND AZABENZOFURAN COMPOUNDS FOR THE TREATMENT OF HEPATITIS C

Compounds of formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. 2. A compound of wherein n and m are each 1.3. A compound of wherein Ris phenyl substituted with halo.4. A compound of wherein halo is fluoro.5. A compound of wherein R claim 1 , R claim 1 , Rand Rare each hydrogen.6. A compound of wherein X and Y are each NR.7. A compound of wherein Ris hydrogen or S(O)CH.8. A compound of wherein A is at least a 12-member ring.9. A compound of wherein A is at least a 15-member ring.10. A compound of wherein A is at least a 17-member ring.11. A compound of wherein A is at least a 19-member ring.13. A composition comprising a compound of or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.14. A composition comprising a compound of or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.15. A method of treating hepatitis C infection comprising administering a therapeutically effective amount of a compound of to a patient. This application claims the priority of U.S. Provisional Application Ser. No. 61/750,967 filed Jan. 10, 2013 which is herein incorporated by reference.The invention relates to novel compounds, including their salts, which have activity against hepatitis C virus (HCV) and which are useful in treating those infected with HCV. The invention also relates to compositions and methods of making and using these compounds.Hepatitis C virus (HCV) is a major human pathogen, infecting an estimated 170 million persons worldwide—roughly five times the number infected by human immunodeficiency virus type 1. A substantial fraction of these HCV infected individuals develop serious progressive liver disease, including cirrhosis and hepatocellular carcinoma (Lauer, G. M.; Walker, B. D. 2001, 345, 41-52).HCV is a positive-stranded RNA ...

CYANOARYL SUBSTITUTED BENZ(OTHI)OXANTHENE COMPOUNDS

The present invention relates to a cyanoaryl substituted compound of formula (I), (I) wherein m is 0-4; R, R, Rand Rare selected from hydrogen, chlorine, bromine and C-C-aryl, which carries one to three cyano; each Rindependently from each other is selected from bromine, chlorine, cyano, —NRaRb, C-C-alkyl, C-C-haloalkyl, C1-C24-alkoxy, C-C-haloalkoxy, C-C-cycloalkyl, heterocycloalkyl, heteroaryl, C-C-aryl, C-C-aryloxy, C-C-aryl-C-C-alkylene, etc., with the proviso that at least one of the radicals R, R, R, Rand Ris C-C-aryl, which carries one to three cyano; X is O, S, SO or SO; A is a diradical of the formulae (A.1), (A.2), (A.3), or (A.4) wherein *, R, (R)n, (R)o and (R)p are as defined in the claims and in the description. The invention also relates to the use of said compound(s) in color converters, to said color converters and their use, to lighting devices, to a backlight unit for liquid crystal displays; a liquid crystal display device and a self-emissive display device comprising at least one compound (I). 123-. (canceled)25. The cyanoaryl substituted compound of formula (I) according to claim 24 , in which X is O.26. The cyanoaryl substituted compound of formula (I) according to claim 24 , where Rand Rare each phenyl claim 24 , which comprises 1 claim 24 , 2 or 3 cyano groups claim 24 , and Rand Rare each hydrogen.27. The cyanoaryl substituted compound of formula (I) according to claim 24 , wherein A is a radical of formula (A.2).31. The cyanoaryl substituted compound of formula (I) according to claim 30 , wherein m in formula (I) is 0 or 1 and when m is 1 claim 30 , Ris a radical of formula (D.1) claim 30 , in which Rand Rare each independently C-C-alkyl or Ris a radical of formula (D.2) claim 30 , in which Rand Rare each independently C-C-alkyl and Ris branched C-C-alkyl or Ris a radical of formula (D.5) claim 30 , where Ris cyano or C-C-alkyl claim 30 , y is 0 and x is 1 or 2.32. A color converter comprising at least one cyanoaryl substituted compound of ...

COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

A compound, an organic light-emitting device, and a display apparatus, the compound being represented by Formula 1: 6. The compound as claimed in claim 1 , wherein claim 1 , in Formula 1 claim 1 , X claim 1 , X claim 1 , X claim 1 , and Xare each CH.7. The compound as claimed in claim 1 , wherein claim 1 , in Formula 1 claim 1 , X1 is N.8. The compound as claimed in claim 1 , wherein claim 1 , in Formula 1 claim 1 , X claim 1 , X claim 1 , and Xare each CH claim 1 , and Xis N.9. The compound as claimed in claim 1 , wherein claim 1 , in Formula 1 claim 1 , Rand Rare each CH.13. An organic light-emitting device claim 1 , comprising:a first electrode;a second electrode facing the first electrode; andan organic layer between the first electrode and the second electrode, the organic layer including an emission layer,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the organic layer includes the compound as claimed in .'}14. The organic light-emitting device as claimed in claim 13 , wherein the emission layer is a fluorescent emission layer.15. The organic light-emitting device as claimed in claim 13 , wherein the emission layer includes the compound.16. The organic light-emitting device as claimed in claim 13 , whereinthe first electrode is an anode,the second electrode is a cathode, andthe organic layer includes:a hole transport region between the first electrode and the emission layer, the hole transport region including at least one selected from a hole transport layer, a hole injection layer, and an electron blocking layer, andan electron transport region between the emission layer and the second electrode, the electron transport region including at least one selected from an electron transport layer, a hole blocking layer, and an electron injection layer.17. The organic light-emitting device as claimed in claim 16 , wherein the hole transport region includes a charge-generating material.18. The organic light-emitting device as claimed in claim 17 , wherein ...

Nanofibril Materials for Highly Sensitive and Selective Sensing of Amines

A sensory material with high sensitivity, selectivity, and photostability has been developed for vapor probing of organic amines. The sensory material is a perylene-3,4,9,10-tetracarboxyl compound having amine binding groups and the following formula where A and A′ are independently chosen from N—R1, N—R2, and O such that both A and A′ are not O, and R1 through R10 are amine binding moieties, solubility enhancing groups, or hydrogen such that at least one of R1 through R10 is an amine binding moiety. This perylene compound can be formed into well-defined nanofibers. Upon deposition onto a substrate, the entangled nanofibers form a meshlike, highly porous film, which enables expedient diffusion of gaseous analyte molecules within the film matrix, leading to a milliseconds response for vapor sensing.

ORGANIC ELECTROLUMINESCENT COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME

The present disclosure relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. By using the organic electroluminescent compound of the present disclosure, it is possible to provide an organic electroluminescent device having low driving voltage and/or excellent power efficiency and/or improved driving lifespan. 2. The organic electroluminescent compound according to claim 1 , wherein the substituents of the substituted aryl(ene) claim 1 , the substituted heteroaryl(ene) claim 1 , the substituted alkyl claim 1 , and the substituted mono- or polycyclic claim 1 , alicyclic or aromatic ring claim 1 , or the combination thereof claim 1 , in L claim 1 , Ar claim 1 , Rto R claim 1 , and Rto R claim 1 , each independently claim 1 , are at least one selected from the group consisting of deuterium; a halogen; a cyano; a carboxyl; a nitro; a hydroxyl; a (C1-C30)alkyl; a halo(C1-C30)alkyl; a (C2-C30)alkenyl; a (C2-C30)alkynyl; a (C1-C30)alkoxy; a (C1-C30)alkylthio; a (C-C30)cycloalkyl; a (C-C30)cycloalkenyl; a (3- to 7-membered)heterocycloalkyl; a (C6-C30)aryloxy; a (C6-C30)arylthio; a (3- to 30-membered)heteroaryl unsubstituted or substituted with a (C1-C30)alkyl or a (C6-C30)aryl; a (C6-C30)aryl unsubstituted or substituted with a (3- to 30-membered)heteroaryl; a tri(C1-C30)alkylsilyl; a tri(C6-C30)arylsilyl; a di(C1-C30)alkyl(C6-C30)arylsilyl; a (C1-C30)alkyldi(C6-C30)arylsilyl; an amino; a mono- or di- (C1-C30)alkylamino; a mono- or di- (C6-C30)arylamino; a (C1-C30)alkyl(C6-C30)arylamino; a (C1-C30)alkylcarbonyl; a (C1-C30)alkoxycarbonyl; a (C6-C30)arylcarbonyl; a di(C6-C30)arylboronyl; a di(C1-C30)alkylboronyl; a (C1-C30)alkyl(C6-C30)arylboronyl; a (C6-C30)aryl(C1-C30)alkyl; and a (C1-C30)alkyl(C6-C30)aryl.3. The organic electroluminescent compound according to claim 1 , whereinL represents a single bond, a substituted or unsubstituted (C6-C25)arylene, or a substituted or unsubstituted (5- to 25-membered)heteroarylene ...

CARBAZOLE DERIVATIVES

The present invention relates to carbazole derivatives, especially for use in electronic devices. The invention further relates to a process for preparing the compounds of the invention and to electronic devices comprising these. 115.-. (canceled)22. The compound according to claim 16 , wherein the Ar group comprises or constitutes a hole transport group.23. The compound according to claim 16 , wherein the Ar group comprises or constitutes an electron transport group.24. The compound according to claim 23 , wherein the Ar group is a group that can be represented by the formula (QL){'br': None, 'sup': '1', 'Q-L-\u2003\u2003 Formula (QL)'}{'sup': 1', '1, 'in which Lrepresents a bond or an aromatic or heteroaromatic ring system which has 5 to 40 aromatic ring atoms and may be substituted by one or more Rradicals, and Q is an electron transport group, where'}{'sup': 1', '1', '2', '1', '2', '1', '1', '1', '2', '1', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'sub': 2', '2', '2', '2', '2', '2', '2', '3', '3', '2', '2', '2', '2, 'claim-text': {'sub': 2', '2, 'sup': 2', '2', '2', '1, '—O—, —S—, SO or SOand where one or more hydrogen atoms may be replaced by D, F, Cl, Br, I, CN or NO, or an aromatic or heteroaromatic ring system which has 5 to 40 aromatic ring atoms and may be substituted in each case by one or more Rradicals, or an aryloxy or heteroaryloxy group which has 5 to 40 aromatic ring atoms and may be substituted by one or more Rradicals, or an aralkyl or heteroaralkyl group which has 5 to 40 aromatic ring atoms and may be substituted by one or more Rradicals, or a combination of these systems; at the same time, two or more Rradicals together may form a mono- or polycyclic, aliphatic, heteroaliphatic, aromatic or heteroaromatic ring system;'}, 'Ris the same or different at each instance and is H, D, F, Cl, Br, I, CN, NO, N(Ar), N(R), C(═O)Ar, C(═O)R, P(═O)(Ar), P(Ar), B(Ar), B(OR), Si(Ar), Si(R), a straight-chain alkyl, alkoxy or thioalkoxy group having 1 ...

HIV REPLICATION INHIBITOR

The present invention provides a novel compound having an antiviral activity, in particular, an HIV replication inhibiting activity, as well as a pharmaceutical composition, in particular, an anti-HIV agent. 2: The compound according to or its pharmaceutically acceptable salt claim 1 , wherein Ris a hydrogen atom.3: The compound according to claim 1 , or its pharmaceutically acceptable salt claim 1 , wherein n is 1.4: The compound according to or its pharmaceutically acceptable salt claim 3 , wherein Ris substituted or unsubstituted alkyloxy claim 3 , or substituted or unsubstituted cycloalkyloxy.5: The compound according to or its pharmaceutically acceptable salt claim 1 , wherein ring A is monocyclic aromatic carbocycle claim 1 , monocyclic non-aromatic carbocycle claim 1 , monocyclic aromatic heterocycle or monocyclic non-aromatic heterocycle claim 1 ,{'sup': 'A', 'wherein the ring may be fused with another aromatic carbocycle, non-aromatic carbocycle, aromatic heterocycle, or non-aromatic heterocycle; the ring may form a spiro ring together with another aromatic carbocycle, non-aromatic carbocycle, aromatic heterocycle or non-aromatic heterocycle; two atoms constituting ring A which are not adjacent to each other may be cross-linked with alkylene, alkenylene or alkynylene; and/or, rings may be substituted with one or more of R;'}{'sup': A', 'A', 'A1, 'wherein Ris each independently, halogen, cyano, nitro, oxo, azide, trimethylsilyl or —X—R;'}{'sup': A', 'A2', 'A2', 'A2', 'A2', 'A2', 'A2', 'A2', 'A2', 'A2', 'A2', 'A3', 'A2', 'A2, 'sub': 2', '2', '2, 'Xis a single bond, —O—, —S—, —NR—, ═N—, —CO—, —SO—, —O—CO—, —CO—O—, —NR—CO—, —CO—NR—, —NR—CO—O—, —CO—O—NR—, —O—CO—NR—, —NR—O—CO—, —CO—NR—O—, —O—NR—CO—, —NR—CO—NR—, —NR—SO— or —SO—NR—;'}{'sup': A1', 'A', 'A1, 'Ris a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aromatic carbocyclyl, substituted or ...

HETERO-CONDENSED PHENYLQUINAZOLINES AND THEIR USE IN ELECTRONIC DEVICES

The present invention relates to compounds of the general formula (I) and to a process for their preparation, to an electronic device comprising at least one of these compounds, to an emitting layer, preferably present in an electronic device, comprising at least one compound of general formula (I) and to the use of a compound according to general formula (I) in an electronic device as a host material and/or charge transporting material. 2: The compound according to claim 1 , wherein Xand Xare N.3: The compound according to claim 1 , wherein Xis CRand Xis N or Xis N and Xis CR.4: The compound according to claim 1 , wherein Xis CR claim 1 , Xis CR claim 1 , Xis CR claim 1 , Xis CR claim 1 , Xis CR claim 1 , Xis CR claim 1 , Xis CRand Xis CR.5: The compound according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare independently of each other selected from H claim 1 , a group of formula -(L)-(L)-(L)-(L)-R claim 1 , wherein L claim 1 , L claim 1 , L claim 1 , Lare independently of each other selected from a C-Caryl group which is unsubstituted or substituted by at least one group E or C-Cheteroaryl group which is unsubstituted or substituted by at least one group E claim 1 , and Ris independently of each other selected from H or a C-Calkyl group which unsubstituted or substituted by at least one group E and/or interrupted by at least one group D.6: The compound according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand R claim 1 , if present claim 1 , are independently of each other selected from H claim 1 , a C-Caryl group which is unsubstituted or substituted by at least one group E or a C-CN-comprising heteroaryl group which is unsubstituted or substituted by at least one group.10: The compound according to claim 7 , wherein m is 1 claim 7 , M is a C-Carylene group which is unsubstituted or substituted by at least one ...

VISIBLE LIGHT ACTIVATED PRINTING INK

A visible light activated ink that produces a color change when exposed to visible light is provided. The ink includes a visible light activated photochromic compound, one or more binders, additives including one or more surfactants, and a solvent. The visible light activated ink is substantially colorless in the as-deposited state and requires a visible light intensity of approximately 300 W/mor greater at a wavelength of approximately 400-700 nm to produce a color change. 1. A visible light activated ink comprising:a visible light activated photochromic compound in an amount of approximately 0.2 to 20 weight percent selected from one or more of π-extended conjugation heterocyclic compounds of naphthopyran, benzopyran, spirooxazine, spiropyran, fulgide, diarylethene, and/or perimidinespirocyclohexadienone;one or more binders in an amount of approximately 10 to 45 weight percent;additives in an amount from approximately 2 to 8 weight percent, the additives including one or more surfactants; anda solvent in an amount of approximately 35 to 70 weight percent;{'sup': '2', 'wherein the visible light activated ink requires a visible light intensity of approximately 300 W/mor greater at a wavelength of approximately 400-700 nm to produce a color change.'}2. The visible light activated ink of claim 1 , wherein the one or more binders is/are selected from one or more polymeric binders.3. The visible light activated ink of claim 1 , wherein the one or more surfactants is/are selected from one or both of polyethylene glycol sorbitan monolaurate and polyoxyethylenesorbitan monolaurate.4. The visible light activated ink of claim 1 , wherein the solvent is selected from one or more of water claim 1 , alcohols claim 1 , polyols claim 1 , esters claim 1 , ketones claim 1 , glycerol claim 1 , and/or vegetable oils.13. The visible light activated ink of wherein the binder is selected from one or more of rubbers claim 1 , polyvinyl alcohol claim 1 , styrene acrylic latex claim 1 , ...

Use of rylene derivatives as photosensitizers in solar cells

Verwendung von Rylenderivaten I DOLLAR F1 mit folgender Bedeutung der Variablen: DOLLAR A X zusammen DOLLAR F2 beide -COOM; DOLLAR A Y ein Rest DOLLAR F3 der andere Rest Wasserstoff; DOLLAR A zusammen DOLLAR F4 beide Wasserstoff; DOLLAR A R gegebenenfalls substituiertes (Het)Aryloxy, (Het)Arylthio; DOLLAR A P -NR·1·R·2·; DOLLAR A B Alkylen; gegebenenfalls substiutiertes Phenylen; Kombinationen davon; DOLLAR A A -COOM; -SO¶3¶M; -PO¶3¶M¶2¶; DOLLAR A D gegebenenfalls substituiertes Phenylen, Naphthylen, Pyridylen; DOLLAR A M Wasserstoff; Alkalimetallkation; [NR·5·]¶4¶+; DOLLAR A L chemische Bindung; gegebenenfalls indirekt gebundener, gegebenenfalls substituierter (Het)Arylenrest; DOLLAR A R·1·, R·2· gegebenenfalls substituiertes (Cyclo)Alkyl, (Het)Aryl; zusammen das Stickstoffatom enthaltender, gegebenenfalls substituierter Ring; DOLLAR A Z -O-; -S-; DOLLAR A R·3· gegebenenfalls substituiertes Alkyl, (Het)Aryl; DOLLAR A R' Wasserstoff, gegebenenfalls substituiertes (Cyclo)Alkyl, (Het)Aryl; DOLLAR A R·5· Wasserstoff; gegebenenfalls substituiertes Alkyl, (Het)Aryl; DOLLAR A m 0, 1, 2; DOLLAR A n, p, m = 0 : 0, 2, 4 mit: n + p = 2, 4, gegebenenfalls 0; DOLLAR A m = 1 : 0, 2, 4 mit: n + p = 0, 2, 4; DOLLAR A m = 2 : 0, 4, 6 mit: n + p = 0, 4, 6, DOLLAR A oder von deren Mischungen als Photosensibilisatoren in Solarzellen. Use of rylene derivatives I DOLLAR F1 with the following meaning of the variables: DOLLAR A X together DOLLAR F2 both -COOM; DOLLAR A Y one remainder DOLLAR F3 the other remainder hydrogen; DOLLAR A together DOLLAR F4 both hydrogen; DOLLAR A R optionally substituted (Het) aryloxy, (Het) arylthio; DOLLAR A P -NR x 1 x R x 2 x; DOLLAR A B alkylene; optionally substituted phenylene; Combinations thereof; DOLLAR A A COOM; -SO¶3¶M; -PO¶3¶M¶2¶; DOLLAR A D optionally substituted phenylene, naphthylene, pyridylene; DOLLAR A M hydrogen; Alkali metal cation; [NR · 5 ·] ¶4¶ +; DOLLAR A L chemical bond; optionally indirectly bonded, optionally substituted (Het) ...

一种磷光化合物和使用该化合物的有机发光二极管器件

本发明涉及一种磷光化合物和使用该化合物的有机发光二极管器件。所述磷光化合物的结构式如式1或式2所示， 在上述式1和式2中Ar1和Ar2分别独立地选自C6～C60芳基，芴基，包括O、N、S、Si和P其中至少一种杂原子的C2～C60杂环基，C3～C60脂环族和C6～C60芳香族环的稠环基，C2～C20烯基，C2～C20炔基中的一种。L1和L2分别独立地选自由单键、C6～C60亚芳基、芴烯基组成的基团，C3～C60脂环族和C6～C60芳香族环的稠环基，C2～C60杂环基中的一种。X1～X2独立地选自N原子或C原子,其中X1至X2中的至少一个为N。其中Z选自O,S,Se和NAr3；其中环A和环B选自H、取代或未取代的C6～C60芳基。使用结构式1和结构式2所示的磷光化合物作为有机发光二极管器件的发光层，具有优异的色纯度和亮度以及延长的耐久性效果。

Biaryl sulfonamides and methods for using same

The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.

Use of rylene derivatives as photosensitizers in solar cells

Use of rylene derivatives (I) in which the variables are defined as follows: X together Formulae (x1) (x2) (x3) both -COOM; Y a radical -L-NR1R2 (y1) -L- Z-R3 (y2) the other radical hydrogen; together Formulae (y3) (y4) both hydrogen; R optionally substituted (Het)aryloxy, (Het)arylthio; P -NR1R2; B alkylene; optionally substituted phenylene; combinations thereof; A -COOM; -SO3M; -PO3M2; D optionally substituted phenylene, naphthylene, pyridylene; M hydrogen; alkali metal cation; [NR5]4+; L chemical bond; optionally indirectly bonded, optionally substituted (Het)arylene radical; R1, R2 optionally substituted (cyclo)alkyl, (Het)aryl; together the nitrogen atom containing, optionally substituted ring; Z -O-; -S-; R3 optionally substituted alkyl, (Het)aryl; R' hydrogen; optionally substituted (cyclo)alkyl, (Het)aryl; R5 hydrogen; optionally substituted alkyl, (Het)aryl; m 0, 1, 2; n, p m=0: 0, 2, 4 with: n+p = 2, 4, optionally 0; m=1: 0, 2, 4 with: n+p = 0, 2, 4; m=2: 0, 4, 6 with: n+p = 0, 4, 6, or of mixtures thereof as photosensitizers in solar cells.

Process

A process for the preparation of substantially single enantiomer (-)-narwedine comprises seeding a solution of racemic narwedine dissolved in a solvent with substantially single enantiomer (-)-narwedine, provided that if an added amine base is present the ratic solvent:added amine base is greater than 15:1.

스플라이싱을 조절하기 위한 화합물 및 방법

본 발명은 특히 핵산 스플라이싱, 예를 들어 프리(pre)-mRNA의 스플라이싱을 조절하는 화합물 및 관련 조성물과, 이의 사용 방법을 특징으로 한다.

萘嵌苯衍生物在太阳能电池中作为光敏剂的用途

本发明涉及萘嵌苯衍生物(I)或其混合物在太阳能电池中作为光敏剂的用途：其中各变量如下所定义：X一起为式(x1)、(x2)或(x3)，均为－COOM基团；Y为基团－L－NR 1 R 2 (y1)，－L－Z－R 3 (y2)，且另一个基团为氢；一起为式(y3)或(y4)；或均为氢；R为任选取代的(杂)芳基氧基或(杂)芳基硫基；P为－N 1 R 2 ；B为亚烷基、任选取代的亚苯基或其组合；A为－COOM、－SO 3 M或－PO 3 M 2 ；D为任选取代的亚苯基、亚萘基或亚吡啶基；M为氢、金属阳离子、[NR 5 ] 4 + ；L为化学键；任选间接连接，任选取代的(杂)亚芳基；R 1 、R 2 为任选取代的(环)烷基或(杂)芳基；一起为含有氮原子的任选取代的环；Z为－O－或－S－；R 3 为任选取代的烷基、(杂)芳基；R′为氢；任选取代的(环)烷基或(杂)芳基；R 5 为氢；任选取代的烷基或(杂)芳基；m为0、1或2；n、p在m＝0时为0、2或4，其中n+p＝2、4，任选0；n、p在m＝1时为0、2或4，其中n+p＝0、2、4；n、p在m＝2时为0、4、6，其中n+p＝0、4或6。

苯并噻唑-6-基乙酸衍生物及其治疗hiv感染的用途

本发明提供了包括式I’化合物的公开化合物及其盐：

유기 발광 소자용 재료

본 발명은, 특히 유기 전계발광 소자에서 삼중항 매트릭스 재료로서 사용하기 위한, 전자-결핍 헤테로아릴 기에 의해 치환되어 있는 카르바졸, 디벤조푸란, 디벤조티오펜 및 플루오렌 유도체를 기재한다. 본 발명은 또한 본 발명에 따른 화합물의 제조 방법 및 이러한 화합물을 포함하는 전자 소자에 관한 것이다.

Method of preparing derivatives of 1-ohyaporphyn

A process for the preparation of 1-hydroxyaporphine derivatives of the general formula: <IMAGE> I wherein R1, R3 and R4, which are the same or different, are lower alkyl, aryl or aralkyl radicals or R3 and R4 can together form a lower alkylene bridge member and R2 is a hydrogen atom or a lower alkyl, aralkyl or alkoxycarbonyl radical or an acyl radical derived from an aliphatic, aromatic or araliphatic carboxylic acid.

태양 전지 중 감광제로서의 릴렌 유도체의 용도

본 발명은 하기의 변수 정의를 갖는 릴렌 유도체 (I) 또는 상기 릴렌 유도체의 혼합물의, 태양 전지 중 감광제로서의 용도에 관한 것이다: X는 함께 이거나, 상기 X 둘 모두가 -COOM이고; Y는 한 라디칼이 이거나, 다른 라디칼이 수소이며; 함께 이거나, 상기 Y 둘 모두가 수소이고; R은 임의로 치환된 (헤트)아릴옥시, (헤트)아릴티오이며; P는 -NR 1 R 2 이고; B는 알킬렌; 임의로 치환된 페닐렌; 이들의 조합이며; A는 -COOM; -SO 3 M; -PO 3 M 2 이고; D는 임의로 치환된 페닐렌, 나프틸렌, 피리딜렌이며; M은 수소; 알칼리 금속 양이온; [NR 5 ] 4 + 이고; L은 화학 결합; 임의로 간접 결합되고, 임의로 치환되는 (헤트)아릴렌 라디칼이며; R 1 , R 2 는 임의로 치환된 (시클로)알킬, (헤트)아릴; 함께 질소 원자를 포함하는 임의로 치환된 고리이고; Z는 -O-; -S-이며; R 3 는 임의로 치환된 알킬, (헤트)아릴이고; R'은 수소; 임의로 치환된 (시클로)알킬, (헤트)아릴이며; R 5 는 수소; 임의로 치환된 알킬 (헤트)아릴이고; m은 0, 1, 2이며; n, p은 m이 0이고 n + p가 2, 4, 필요한 경우 0인 경우에 0, 2, 4이고; m이 1이고 n + p가 0, 2, 4인 경우에 0, 2, 4이며; m이 2이고 n + p가 0, 4, 6인 경우에 0, 4, 6이다.

用于有机发光器件的材料

本发明涉及被缺电子杂芳基基团取代的咔唑、二苯并呋喃、二苯并噻吩和芴衍生物，其特别用作有机发光器件中的三重态基质材料。本发明还涉及用于制造根据本发明的化合物的方法，和涉及包含所述化合物的电子器件。

Novel method for preparing selenyl-substituted aromatic aldehyde compounds

본원은, 셀레닐-치환된 방향족 알데하이드(selenyl-substituted aromatic aldehyde)계 화합물의 신규한 제조 방법에 관한 것으로서, 구체적으로, 셀레놀레이트 친핵체(selenolate nucleophile)를 형성하여 방향족 알데하이드계 출발물질을 친핵성 치환시키는 것을 포함하는, 셀레닐-치환된 방향족 알데하이드계 화합물의 신규한 제조 방법에 관한 것이다. The present invention relates to a novel process for the preparation of selenyl-substituted aromatic aldehyde-based compounds, and more particularly to a process for the preparation of selenolate nucleophiles to form an aromatic aldehyde- Substituted aromatic aldehyde-based compounds.

Compound and Organic light emitting device comprising same

하기 화학식 1로 표시되는 화합물: <화학식 1> 상기 화학식 1의 치환기에 대한 내용은 상세한 설명을 참조한다.

Ret syndrome drug

Azoanthracene substituted derivatives, pharmaceutical compositions and methods of use thereof

Un compuesto de Fórmula (I), o una sal farmacéuticamente aceptable del mismo**Fórmula** donde W, X, Y y Z del anillo A forman el grupo**Fórmula** o el grupo**Fórmula** en donde R4 es seleccionado del grupo que consiste de: a) -hidrógeno; b) -C1-6 alquilo; y c) -C(O)-C1-6 alquilo; R5 es -G3-L2-Q2-L3-G4, en donde L2 es seleccionado del grupo que consiste de: -CH2-, -O-, -N(R26)-, y -C(O)-, en donde R26 es seleccionado del grupo que consiste de: hidrógeno, -alquilo, -arilo, y -alquilen-arilo; L3 es un enlace directo; Q2 es un grupo alquileno C1-C10; G3 es un grupo fenileno, en donde G3 es opcionalmente sustituido 1-4 veces con sustituyentes seleccionados independientemente de R8, en donde R8 se selecciona de Rb; y G4 es seleccionado del grupo que consiste de: cicloalquilo, fenilo, piridinilo, benzotiofeneilo, benzotiazolilo, donde G4 es opcionalmente sustituido 1-4 veces con sustituyentes seleccionados independientemente de R9, en donde R9 se selecciona de Rb; R es -(CH2)p-G1-L1-G2, en donde p es 1; L1 es un enlace directo; G1 es fenilo, en donde G1 es opcionalmente sustituido 1-4 veces con sustituyentes seleccionados independientemente de R10, en donde R10 es Rb; G2 es seleccionado del grupo que consiste de: indol, piridina, pirimidina, quinolina, e isoxazol, en donde G2 es opcionalmente sustituido 1-4 veces con sustituyentes seleccionados independientemente de R11, en donde R" es Rb, R1 es seleccionado del grupo que consiste de: -CO2H y -CO2R12, en donde R12 es seleccionado del grupo que consiste de: -C1-10 alquilo, -cicloalquilo; y -arilo, en donde R12 es opcionalmente sustituido 1-4 veces con un grupo seleccionado independientemente de Rc; R2 es seleccionado del grupo que consiste de: -hidrógeno y -C1-10 alquilo; R3 es bien sea seleccionado del grupo consistente de: a) -C1-10 alquilo, b) -fenilo, c) -tiofeneilo, d) -furanilo, e) -piridilo, f) -C1-10 alquilen-piridilo, g) -C1-10 alquilen-aminotiazolilo, h) -C1-10 alquilen-imidazolilo, i) -C1-10 alquilen- ...

Heteroatom-bridged carbazole derivatives and uses thereof

本发明涉及有机电致发光元件用材料技术领域，尤其涉及杂原子桥联咔唑衍生物及其应用；所述杂原子桥联咔唑衍生物的结构如式(I)所示：本发明所述的杂原子桥联咔唑衍生物具有较高的三重态能级、高的玻璃化温度，适宜作为有机电致发光元件用材料使用，含有所述的杂原子桥联咔唑衍生物的有机电致发光元件用材料，具有启动电压低，发光效率和亮度高的特点。另外，本发明的杂原子桥联咔唑衍生物具有良好的热稳定性和成膜性能，应用在有机电致发光元件用材料、有机电致发光元件、显示装置、照明装置中，能够延长使用寿命，从而能够降低有机电致发光元件用材料、有机电致发光元件、显示装置、照明装置的制造成本。

6-member ring structure used in electroluminescent devices

An organic material having a 6-member ring structure represented by the following formulae (I), wherein: ring A, ring B, and ring C each include substituted or un-substituted aromatic rings comprising 6 to 60 carbon atoms, or substituted or un-substituted heteroaromatic rings comprising 4 to 60 carbon atoms, and ring A and ring C form a fused aromatic or heteroaromatic structure; X is a carbon atom, a nitrogen atom, a sulfur atom, a silicon atom, an oxygen atom, a phosphorus atom, a selenium atom, or a germanium atom.

NEW ANTI-VIRAL COMPOUNDS

1. Соединение формулы (A):,где- каждая пунктирная линия представляет собой возможную двойную связь, при этом, если пунктирная линия «a» образует двойную связь, то пунктирная линия «b» не образует двойную связь, и при этом, если пунктирная линия «b» образует двойную связь, то пунктирная линия «а» не образует двойную связь;- Rнезависимо выбран из алкила; алкенила; алкинила; циклоалкила; циклоалкенила; циклоалкинила; арила; гетероцикла; арилалкила; арилалкенила; арилалкинила; гетероцикл-алкила; гетероцикл-алкенила или гетероцикл-алкинила;- где в циклоалкильной, циклоалкенильной, циклоалкинильной, алкильной, алкенильной или алкинильной группировке указанного алкила, алкенила, алкинила, циклоалкила, циклоалкенила, циклоалкинила, арилалкила, арилалкенила, арилалкинила, гетероцикл-алкила, гетероцикл-алкенила или гетероцикл-алкинила один или более чем один -CH, -CH-, -CH= и/или ≡CH возможно заменен одним или более чем одним -NH, -NH-, -O-, -S-, -N= и/или ≡N;- и где указанный алкил, алкенил, алкинил, циклоалкил, циклоалкенил, циклоалкинил, арил, гетероцикл, арилалкил, арилалкенил, арилалкинил, гетероцикл-алкил, гетероцикл-алкенил или гетероцикл-алкинил может быть незамещенным или замещен одним или более чем одним Z;- и где возможно атом углерода или гетероатом указанного алкила, алкенила, алкинила, циклоалкила, циклоалкенила, циклоалкинила, арила, гетероцикла, арилалкила, арилалкенила, арилалкинила, гетероцикл-алкила, гетероцикл-алкенила или гетероцикл-алкинила может быть окислен с образованием C=O, C=S, N=O, N=S, S=O или S(O);- каждый из Rи Rнезависимо выбран из водорода; циано; алкила; алкенила; алкинила; арилалкила; арилалкенила; арилалкинила; гетероцик� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 221/06 (13) 2013 121 785 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2013121785/04, 15.11.2011 (71) Заявитель(и): КАТОЛИКЕ УНИВЕРЗИТАЙТ ЛОЙФЕН (BE) Приоритет(ы): (30) Конвенционный приоритет: 15.11.2010 EP ...

Substituted heterocycle fused gamma-carbolines

The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R 1 , R 5 , R 6a , R 6b , R 7 , R 8 , R 9 , X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Substituted heterocycle fused gamma-carbolines

The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R 1 , R 5 , R 6a , R 6b , R 7 , R 8 , R 9 , X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Substituted heterocycle fused gamma-carbolines

The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R 1 , R 5 , R 6a , R 6b , R 7 , R 8 , R 9 , X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.

Organic electroluminescent device

The present invention relates to electronic devices, in particular organic electroluminescent devices, containing compounds according to formula (1), the corresponding compounds, and a method for preparing said compounds.

Materials for organic light emitting devices

Die vorliegende Erfindung beschreibt Carbazol-, Dibenzofuran-, Dibenzothiophen- und Fluorenderivate, welche mit elektronenarmen Heteroarylgruppen substituiert sind, insbesondere zur Verwendung als Triplettmatrixmaterialien in organischen Elektrolumineszenzvorrichtungen. Die Erfindung betrifft ferner ein Verfahren zur Herstellung der erfindungsgemäßen Verbindungen sowie elektronische Vorrichtungen, enthaltend diese.

Nitrogen-containing heterocyclic compounds and organic electroluminescence devices containing them

The present invention relates to compounds of the general formula (11), to a material for an organic electroluminescence device comprising ot least one of these compounds, to an organic electroluminescence device comprising at least one of these compounds, and to the use of a compound according to general formula (11) in an organic electroluminescence device as a host material or an electron transporting material.

Nitrogen-containing heterocycles for use in oleds

Die vorliegende Erfindung beschreibt stickstoffhaltige Heterocyclen, welche mit Carbazol-Gruppen substituiert sind, insbesondere zur Verwendung in elektronische Vorrichtungen. Die Erfindung betrifft ferner ein Verfahren zur Herstellung der erfindungsgemäßen Verbindungen sowie elektronische Vorrichtungen, enthaltend diese.

Carbazole derivatives

The present invention relates to carbazole derivatives, particularly for use in electronic devices. The invention further relates to a method for producing the compounds according to the invention and to electronic devices comprising the same.

Fused phenylquinazolines bridged with a heteroatom

Fused phenylquinazolines bridged with a heteroatom and a process for their preparation, an electronic device comprising at least one of these fused phenylquinazolines, an emitting layer, preferably present in an electronic device, comprising at least one of said fused phenylquinazolines and use of said compounds in an electronic device as a host material, a charge transporting material, charge and/or exciton blocking material, preferably as a host material or an electron transporting material. The present invention further relates to specifically substituted phenylquinazolines bridged with a heteroatom, to a process for their preparation, to an electronic device comprising at least one of these specifically substituted phenylquinazolines, to an emitting layer, preferably present in an electronic device, comprising at least one of said specifically substituted phenylquinazolines and to the use of said specifically substituted compounds.

Compounds that can be used in an organic electronic device

The present invention relates to compounds, particularly for use in electronic devices. The invention further relates to a method for producing the compounds according to the invention, and to electronic devices comprising the same.

Benzimidazole derivatives

The invention relates to benzimidazole derivatives which are suitable for use in electronic devices, and to electronic devices, in particular organic electroluminescent devices, containing said compounds.

Materials for organic electroluminescent devices

The invention relates to compounds which are suitable for use in electronic devices, and electronic devices, in particular organic electroluminescent devices, containing said compounds.

Hetero-condensed phenylquinazolines and their use in electronic devices

The present invention relates to compounds of the general formula (I) and to a process for their preparation, to an electronic device comprising at least one of these compounds, to an emitting layer, preferably present in an electronic device, comprising at least one compound of general formula (I) and to the use of a compound according to general formula (I) in an electronic device as a host material and/or charge transporting material.

Nitrogen-containing heterocycles for use in oleds

Die vorliegende Erfindung beschreibt stickstoffhaltige Heterocyclen, welche mit Carbazol-Gruppen substituiert sind, insbesondere zur Verwendung in elektronische Vorrichtungen. Die Erfindung betrifft ferner ein Verfahren zur Herstellung der erfindungsgemäßen Verbindungen sowie elektronische Vorrichtungen, enthaltend diese. The present invention describes nitrogen-containing heterocycles substituted with carbazole groups, particularly for use in electronic devices. The invention also relates to a method for producing the compounds according to the invention and electronic devices containing them.

Chlorinated naphthalenetetracarboxylic acid derivatives, preparation thereof and use thereof in organic electronics

The present invention relates to chlorinated naphthalenetetracarboxylic acid derivatives, preparation thereof and use thereof as charge transport materials, exciton transport materials or emitter materials.