ИНГИБИТОРЫ КАТЕПСИН-ЦИСТЕИНПРОТЕАЗЫ

Изобретение относится к соединениям, представленным формулой где значения заместителей указаны в описании, и их фармацевтически приемлемым солям, которые могут использоваться для лечения и/или профилактики катепсин-зависимых состояний или болезней млекопитающих, нуждающихся в этом. Эти соединения являются полезными для лечения заболеваний, при которых показано ингибирование резорбции кости, таких как остеопороз, повышение минеральной плотности кости и снижение риска переломов. Задачей настоящего изобретения является применение заявленных соединений для изготовления лекарственного средства, обладающего ингибирующей активностью в отношении катепсина. 8 н. и 16 з.п. ф-лы, 4 табл.

ПРОИЗВОДНЫЕ БЕТА-ФЕНОКСИНИТРИЛОВ И СПОСОБ БОРЬБЫ С ГРИБКОВЫМИ ЗАБОЛЕВАНИЯМИ КУЛЬТУР

Использование: сельское хозяйство, в качестве вещества, обладающего фунгицидной активностью. Сущность изобретения: продукт формулы , где R - водород, метил, этил, изопропил, н-пропил, аллил; n = 1 или 2; x - атом кислорода или серы; y - хлор, бром, фтор; m = 1, 2, 3. Реагент I: . Реагент II: (Hal)2CH2. Реагент III: . Способ борьбы с грибковыми заболеваниями культур обработки листвы продуктом в количестве 0,03 - 1,0 кг/га. 2 с.п. ф-лы, 4 табл.

БЕНЗОЦИКЛОГЕПТЕНЫ, БЕНЗОКСЕПИНЫ И БЕНЗТИЕПИНЫ, СПОСОБЫ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Предложены соединения общей формулы, приведенной в описании. Эти соединения являются мощными активаторами калиевых каналов.

Способ получения производных 2-бензоил-3-аминопиридина или их солей

Способ получения 6-аза-3н-1,4-бензодиазепинов

Способ получения нафталин-,бензофуран-или бензо-/ @ /-тиофенкарбоновых кислот или их фармацевтически допустимых солей

Способ ползгчения нафталин-, бензофуран- или бензо- Ь -тиофенкарбоновых кислот общей формулы где у присоединен к кольцу А, и означает -СООН, -СОО(С -С -алкил), X-0,S или , R .присоединен к атом углерода кольца В, означает водород. где R и X имеют указанные -значения;. Q - галоид, С -С -алкилсульфонилокси или ArSOjO, где Аг - фенил, возможно g замещенный 1 или 2 заместителями, выбранными из группы С -С -алкила, СП С -С -алкокси и галоида, а группы (С -С -алкш1)-0-С , и CHjQ присоединены соответственно к атому углерода колец А и В, подвергают взаимодейS ствию либо с имидазолом в присутствии дополнительного основания, либо с металлсодержащей солью имидазола, ;О 4 после чего при необходимости полученный продукт переводят в соединение формулы I, где Y- группа -СОСИ, ьо м путем кислотного или щелочного гидролиза или соединение формулы I пере00 водят в фармацевтически допустимую соль.

Способ получения 6-аза-1,2-дигидро-3н1,4-бензодиазепинов или их солей

Способ получения производных 2-бензоил3-(аминоацетиламидо)-пиридина или их солей

Способ получения циклических амидинов

Способ получения замещенных ацетонитрилов

The known synthesis for the production of aromatic substituted acetonitriles by reaction of aromatic substances with cyanogen chloride in the gas phase is improved by feeding the starting materials in gaseous form and separated from each other into the reactor. The process can be used to synthesize in general aromatic and especially hetero-aromatic substituted acetonitrile.

4-STILBENYL-1,2,3-TRIAZOLE, VERFAHREN ZU DEREN HERSTELLUNG UND IHRE VERWENDUNG ALS OPTISCHE AUFHELLER

Thioamides - as gastric acid secretion inhibitors

Cpds. (I): (where R1 is 2-pyridyl, 2- or 4-pyrimidyl, 2-pyrazinyl, 2-pyrrolyl, 2-quinolyl, or 2- or 4-thiazolyl; and (a) R2 is H, alkyl, alkenyl, Ph or PhCH2 and R3 is dialkylamino-, N-alkyl-N-phenyl-amino, pyrrolidino-piperidino-, morpholino- or N-alkyl-piperazino, methylamino; (b) R2 is H, alkyl, alkenyl or Ph opt. substd. by halogen. Alkyl or alkoxy and R3 is (3-6C)-cycloalkylamino or (3-6C)-cycloalkylmethylamino; (c) R2 is (CH2)m NR4R5, m = 0 or 1, and R4 and R5 are alkyl or NR4R5 is piperidino, pyrrolidino, or N-alkylpiperazino and R3 is NH-(CH2)n (3-6C)-cycloalkyl or NR6R7; R6 and R7 are H or alkyl; n is 0 or 1, (d) R2 is (CH2)mOR8, m is 0, 1 or 2, R8 is alkyl, allyl or cyclopropanemethyl and R3 is PhNH, NH(CH2)n (3-6C)-cycloalkyl or NR9R10 and R9 and R10 is H or alkyl, and n is 0 or 1; (e) R2 is H, alkyl, alkenyl, alkoxy, allyloxy, cyclopropanemethoxy, Ph, PhCH2 or (CH2)n NR11R12; n is 0 or 1 and R11 and R12 are alkyl or NR11R12 is piperidino, pyrrolidino, morpholino or N-alkyl-( ...

VERFAHREN ZUR HERSTELLUNG VON DIHYDROPYRIDINYLIDENMALONONITRILEN

Verfahren zur Herstellung von beta-Hydroxyalkylpicoliniumsalzen sowie Picoliniumsalze als Zwischenprodukte zur Herstellung kationischer Farbstoffe

DERIVATE VON AROMATISCHE HETEROCYCLEN ENTHALTENDE INTEGRASEINHIBITOREN

(3-AMINO-1H-PYRAZOL-4-YL)(ARYL)KETONE.

HETEROCYCLIC COMPOUNDS

INTERMEDIATES

PROCESS FOR THE PREPARATION OF 5-ALKYLPYRIDINE DERIVATIVES HAVING A TETRAZOLE RADICAL

... 1346379 Substituted pyridyl- and pyridylmethyl-tetrazoles BANYU PHARMACEUTICAL CO Ltd and H HIDAKA 4 April 1972 [9 April 1971] 15398/72 Heading C2C Compounds of formula wherein R is C 1-9 alkyl and n is 0 or 1 are prepared by reacting a 2-cyano- or 2-cyanomethyl- 5-alkylpyridine with an inorganic azide. Intermediates also prepared are 2-X-5-butylpyridines, where X is COCl, CONH 2 , CH 2 OH or CH 2 Cl.

Novel ª‡-substituted 2-pyridinethioacetamides and a process for their preparation

Novel compounds of the general formula where X is H, Cl, Br, F, I, methyl or methoxy are prepared (a) by reaction of the corresponding acetamide with P2S5, (b) by reaction of ammonia with a compound of formula or (c) by contacting a compound of formula with H2S. Nitriles of the last general formula above are prepared by reacting the appropriate a -substituted acetonitrile with 2-halopyridine.

PROCESS FOR THE PREPARATION OF SUBSTITUTED MALONIC ACID DINITRILES

2, 6-DIOXOPIPERIDINE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

OLEFINE DERIVATIVES

Alkyl -‡-benzyl--‡-phenyl--†-tertiaryaminopropyl ketones, their preparation and reduction, and pharmaceutical compositions containing such products

... 1,135,842. - Benzyl - - phenyl - - tertiaryaminopropyl ketones and reduction products. JOHN WYETH & BROTHER Ltd. 8 March, 1967 [10 March, 1966], No. 10550/66. Heading C2C. Novel compounds of general formula wherein Ar and Ar1 are each, phenyl, naphthyl or phenyl substituted by hydroxy, alkoxy, aralkoxy, alkyl, acyloxy or halogen and R is a radical of formula wherein R1 and R2 are alkyl radicals or together complete a ring optionally containing a further hetero atom and R3 is H or alkyl with the proviso that Ar and Ar1 each is one of the substituted phenyl radicals specified above when R is a 1-piperidino or diethylamino radical; and acid addition and quaternary ammonium salts thereof are prepared by reacting a nitrile of Formula II with a Grignard reagent or an alkyl lithium with the proviso that if Ar or Ar1 contain reactive substituents these are blocked prior to the reaction and regenerated later and optionally followed by salt formation ...

5-substituted aza-dibenzo-cycloheptenes and the preparation thereof

The invention comprises compounds of the formula wherein the dotted line represents an optional double bond, A represents hydrogen or one of the substituents halogen, trifluoromethyl, alkoxy, C1- 12 alkyl, hydroxy and acyloxy attached to one or more of the 6-, 7-, 8- and 9-positions, B represents, together with the carbon atoms to which it is attached, a pyridine ring and Z represents one of the groups in which either U and W are both hydrogen or U is a univalent group containing an amino group the nitrogen atom of which is separated from C-5 of the tricyclic nucleus by at least two carbon atoms and W is H or OH, and V is an oxygen atom or a divalent group containing an amino group the nitrogen atom of which is separated from C-5 of the tricyclic nucleus by at least two carbon atoms; and pharmaceutically acceptable acid addition salts thereof. The compounds wherein Z is other than a carbonyl group are prepared by (a) reacting a compound of the formula ...

ANTIARRYTHMIC COMPOSITIONS CONTAINING PYRROLIDINYL DERIVATIVES

... 1519210 Anti-arrythmic compositions A H ROBINS CO INC 23 Dec 1975 [26 Dec 1974] 52611/75 Heading A5B [Also in Division C2] Pharmaceutical compositions having activity against cardiac arrythmia comprise a compound of formula (I): wherein R is C 1-8 alkyl, C 3-9 cycloalkyl or phenyl C 1-8 alkyl; and Y is carbamoyl, cyano or hydrogen, or a pharmaceutically acceptable salt thereof, and a pharmaceutical carrier. The compositions may be in forms for oral or injectable administration or for inhalation.

6-(pyridinyl)-3(2H)-pyridazones

... 2-R-6-PY-3(2H)-pyridazinones (I) or salts thereof, which are useful as cardiotonics, where R is hydrogen, lower-alkyl or lower-hydroxyalkyl, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents, are prepared by reacting 2-R-4,5-dihydro-6-PY-3(2H)-pyridazinone with a dehydrogenating agent. Also shown are: cardiotonic compositions and a method for increasing cardiac contractility using I or salts; and, the preparation of the corresponding intermediate 4,5-dihydro compounds.

FUNGICIDES

Fungicides

Compounds having ...

Substituted N-({Aminoiminomethyl or aminomethyl} phenyl] propyl amides.

The compounds according to the invention are substituted N-[ (aminoiminomethyl or aminomethyl) phenyl]propyl amides of formula (I) herein which exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are Factor Xa inhibitors. The present invention is directed to compounds of formula (I), compositions containing compounds of formula (I), methods for their preparation and their use, which are for treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of Factor"' Xa.

Substituted N-[(Aminoiminomethyl or aminomethyl) Phenyl] Propyl amides.

This invention relates to compounds of formula (I) which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.

Benzoylpyridine derivative or its salt, Fungicide containing it as an active ingredient, its production process and intermediate for producing it.

The present invention relates to a fungicide containing a novel benzoylpyridine derivative or its salt. The present invention provides a fungicide containing a benzoylpyridine derivative represented by the formula (I) or its salt: wherein X is a halogen atom, a nitro group, a substitutable alkoxy group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable hydrocarbon group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group; n is 1, 2, 3, or 4; R1 is a substitutable alkyl group; R2 is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group; and m is 1, 2, 3 or 4, provided that when m is at least 2, R2 may contain an oxygen atom to form a condensed ring.

Process for the production of quinazolines

FUNGICIDES

Subs itute n-Ú( minoi inome hyl or aminomethyl)phenyl¾propyl amides

Substituted n-[(aminoiminomethyl or aminomethyl) phenyl]propyl amides

Benzoylpyridine derivative or its salt fungicide containing it as an active ingredient its production process and intermediate for production process and intermedieate for producing it

Process for the production of quinazolines.

The invention provides a process for the production of a compound of formula (a)or a pharmaceutically acceptable salt or solvate thereof, where in R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R3 represents a 5- or 6-membered heterocyclic ring which is optionally substituted R4 is a 4-, 5-, 6- or 7-membered heterocyclic ring which is optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring, the ring sysytem as a whole being optionally substituted; the process comprising condensing a compound of formula (B), Wherein R1 to R3 are as defined above; with a compound of formula (C)Wherein R5 and R6 taken together with the N atom to which they are attached represent a 4-, 5-,6-or 7-membered N-containing heterocyclic ring, the ring being optionally fused to a benzene ring or a 5- or a 5- or 6-membered heterocyclic ring, the ring system as a whole being optionally substituted.

Substituted n-Ä(aminoiminomethyl or aminomethyl)p henylÜpropyl amides

Derived from - the butyrolactone protective of the myocardium presenting a antiarythmic activity, proceeded for their preparation and drugs while containing.

Derived from the pipéridinedione protective of the myocardium presenting a antiarythmic activity, their method of preparation and the drugs which contain the aforementioned derivatives.

New esters derived from carboxylic acids 2,2-dimethyl cyclopropane and alcohols biarylic, their method of preparation, their application to the fight against the parasites and compositions containing them.

New derivatives of pyridylacétonitriles, their preparation and their use as antifongic in the agricultural domain.

New derivatives of the 2,2-dimethyl acid bearing carboxylic cyclopropane in 3 a saturated halogenous chain, their method and intermediaries of preparation, their application like pesticides and compositions containing them.

Substituted N-[(aminoiminomethyl or aminomethyl) phenyl]propyl amides

Benzoylpyridine derivative or its salt fungicide containing it as an active ingredient its production process and intermediate for production process and intermedieate for producing it

Benzoylpyridine derivative or its salt fungicide containing it as an active ingredient its production process and intermediate for production process and intermedieate for producing it

Substituted n-[(aminoiminomethyl or aminomethyl) phenyl]propyl amides

Process for the production of quinazolines

Subs itute n-Ú( minoi inome hyl or aminomethyl)phenyl¾propyl amides

SUBSTITUTED PYRIDINYL-2-PROPENOATES AND HOMOLOGS THEREOF

SUBSTITUTED PYRIDINYL-2-PROPENOATES AND HOMOLOGS THEREOF

Process for the production of quinazolines

SUBSTITUTED HETERO ARYL ALKANE ACID AND YOUR USE AS INHIBITORS OF THE ALDOSE REDUCTASE

NEW IMMUNOTHERAPEUTI MEANS AND THEIR USE IN THE REDUCTION OF CYTOKINENSPIEGEL

PROCEDURE FOR THE PRODUCTION OF NEW ONE 1.2.3 - TRIAZOLDERIVATEN

CATHEPSIN CYSTEIN PROTEASe HEMMER

Procedure for the production of new Pyridinverbindungen

VERFAHREN ZUR HERSTELLUNG DES NEUEN 3- (4-BROMPHENYL)-N-METHYL-3- (3-PYRIDYL)-ALLYLAMINS, SEINER STEREOISOMEREN UND SEINER PHARMAZEUTISCH AKZEPTABLEN SALZE

VERFAHREN ZUR HERSTELLUNG VON NEUEN 6-AZA-3H-1,4- BENZODIAZEPINEN, DEREN OPTISCHEN ISOMEREN UND DEREN SALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN 6-AZA-3H-1,4-BENZODIAZEPINEN, DEREN OPTISCHEN ISOMEREN UND DEREN SALZEN

DERIVATIVES OF AROMATIC HETEROCYCLEN ABSTENTION INTEGRASEINHIBITOREN

VERFAHREN ZUR HERSTELLUNG VON NEUEN 6-PYRIDAZINONEN

PROCEDURE FOR THE PRODUCTION OF SUBSTITUTED ACETONITRILEN

PROCEDURE FOR THE PRODUCTION OF NEW ALPHA ARYL ALPHA, ALPHA-BIS (OMEGA (OF DISUBSTITUIERTES AMINO) ALKYL) ACETAMIDEN

PROCEDURE FOR the PRODUCTION OF NEW ONE 4,5-DIHYDRO-6 (PYRIDIYNL) - 3 (2H) - PYRIDAZINONEN AND YOUR SALTS

N, N-SUBSTITUTING CYCLI AMINE DERIVATIVES

NEW 1-ARYL-4-PIPERAZINYL of CYCLOHEXANE CARBONIC ACID NITRILES, YOUR PRODUCTION AND USE

BETA PHENOXYNITRIL CONNECTIONS.

3-ARYL-5-ISOTHIAZOLDERIVATE.

PROCEDURES FOR THE PRODUCTION OF IN POSITION 3 BY A HALOGENIERTE SATISFYING CHAIN SUBSTITUTED CYCLOPROPANCARBONSAEUREDERIVATEN.

PIPERIDINDION DERIVATIVES WITH HEART-MUSCLE-CAREFUL AND ANTI-ARRHYTHMIC EFFECT, PROCEDURES FOR YOUR PRODUCTION AND IT CONTAINING DRUGS.

PROCEDURE FOR THE PRODUCTION OF NITRILES.

ALPHA-HETERO-CYCLIC-SUBSTITUTED TOLUNITRILE.

USE OF PENYLIMINOMETHYLPYRIDINE DERIVATIVES AS FUNGICIDES AND PLANT GROWTH MODULATORS, IT ABSTENTIONS ZUSMAMMENSETZUNGEN, PHENYLIMINOMETHYLPYRIDINE DERIVATIVES AND THEIR PRODUCTION.

PROCEDURE FOR the PRODUCTION OF NEW ONE 6-AZA-1,2-DIHYDRO-3H-1,4 BENZODIAZEPINEN, THEIR OPTICAL ISOMERS AND THEIR SALTS

FUNGICIDES.

INDENDERIVATE AND PROCEDURE.

AMINE DERIVATIVES

HETERO-CYCLIC ACETONITRILE AND YOUR USE AS FUNGICIDES.

GAMMA BUTYROLACTONDERIVATE ONE WITH HEART-MUSCLE-CAREFUL AND ANTI-ARRHYTHMIC EFFECT, PROCEDURE FOR YOUR PRODUCTION AND IT CONTAINING DRUGS.

2-CYANO-3,5-DIHYDROXY-HEX-2-EN-CARBONSÄURE of AMIDE DERIVATIVES, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE AS DRUGS

SUN PROTECTION COMPOSITIONS AS WELL AS DIHYDROPYRIDINE AND DIHYDROPYRANE

FLUORINE COMPOUNDS AS FLAVORS SE INHIBITORS

STYRYLSUBSTITUIERTE HETERO ARYL CONNECTIONS, WHICH EGF RECEPTOR TYROSINKINASE ONE INHIBIEREN

PYRIDO (2,3-B) INDOLIZINDERIVATE AND AZA SIMILAR ONE: CRF1 SPECIFIC LIGANDS

SUBSTITUTED SPIROVERBINDUNGEN FOR THE TREATMENT OF INFLAMMATIONS

PHARMACEUTICAL COMPOSITIONS CONTAINING TYRPHOSTINE

PROCEDURE FOR the PRODUCTION OF 1 (6-METHYLPYRIDIN 3-YL) - 2 (4 (METHYL SULPHONYL) - PHENYL) ETHANON

New Azokomponenten in the Diazotypie

NEW IMMUNOTHERAPEUTI MEANS AND THEIR USE IN THE REDUCTION OF CYTOKINENSPIEGEL

NEW IMMUNOTHERAPEUTI MEANS AND THEIR USE IN THE REDUCTION OF CYTOKINENSPIEGEL

NEW IMMUNOTHERAPEUTI MEANS AND THEIR USE IN THE REDUCTION OF CYTOKINENSPIEGEL

NEW IMMUNOTHERAPEUTI MEANS AND THEIR USE IN THE REDUCTION OF CYTOKINENSPIEGEL

NEW IMMUNOTHERAPEUTI MEANS AND THEIR USE IN THE REDUCTION OF CYTOKINENSPIEGEL

NEW IMMUNOTHERAPEUTI MEANS AND THEIR USE IN THE REDUCTION OF CYTOKINENSPIEGEL

NEW IMMUNOTHERAPEUTI MEANS AND THEIR USE IN THE REDUCTION OF CYTOKINENSPIEGEL

NEW IMMUNOTHERAPEUTI MEANS AND THEIR USE IN THE REDUCTION OF CYTOKINENSPIEGEL

NEW IMMUNOTHERAPEUTI MEANS AND THEIR USE IN THE REDUCTION OF CYTOKINENSPIEGEL

CYCLOPROPYLAMINE DERIVATIVES USEFUL AS LSD1 INHIBITORS

The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection. 4. The compound of wherein (G) is a heterocyclyl.5. (canceled)6. The compound of wherein (G) is phenyl.78-. (canceled)9. The compound of wherein E is —X═X— claim 1 , and X claim 1 , X claim 1 , Xand Xare independently C(R2) or N.10. The compound of wherein E is —X═X— claim 1 , and X claim 1 , X claim 1 , Xand Xare independently C(R2).1112-. (canceled)13. The compound of wherein E is —S— claim 1 , and Xand Xare independently C(R2) or N.1420-. (canceled)21. The compound of wherein each (R1) is independently chosen from alkyl claim 1 , aryl claim 1 , amino claim 1 , amido claim 1 , nitro claim 1 , halo claim 1 , haloalkyl claim 1 , haloalkoxy claim 1 , cyano claim 1 , heterocycle claim 1 , sulfonyl claim 1 , sulfonamide claim 1 , hydroxyl claim 1 , or alkoxy.22. The compound of wherein each (R1) is independently chosen from —CF claim 1 , —F claim 1 , —Cl claim 1 , —CN claim 1 , —CH claim 1 , —OH claim 1 , —OCH claim 1 , —C(═O)NH claim 1 , —NH—CO—CH claim 1 , —NH—SO—CH claim 1 , —NH—SO—CH—CH claim 1 , —NH—SO—CH(CH)—CH claim 1 , —NH—SO—(CH) claim 1 , —NH—SO—(CH)—CN claim 1 , —NHSOCF claim 1 , or —S(═O)NHCH.2328-. (canceled)30. The compound of wherein E is —S— or —X═X—.3137-. (canceled)38. The compound of wherein (G) is an aryl or heterocyclyl.3941-. (canceled)42. The compound of wherein each (R1) is independently chosen from alkyl claim 29 , aryl claim 29 , amino claim 29 , amido claim 29 , nitro claim 29 , halo claim 29 , haloalkyl claim 29 , cyano claim 29 , heterocyclyl claim 29 , sulfonyl claim 29 , sulfonamide claim 29 , hydroxyl claim 29 , or alkoxy.4446-. (canceled)47. The compound of wherein (G) is an aryl or heterocyclyl.4850-. (canceled)51. The compound of wherein each (R1) is independently chosen from alkyl claim 43 , aryl ...

STABLE INSECTICIDE COMPOSITIONS AND METHODS FOR PRODUCING SAME

Insect controlling compositions including an N-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximine compound exhibiting increased stability, along with methods for preparing same, are disclosed. 4. The method of claim 1 , wherein X represents NOor CN claim 1 , Y represents —CF claim 1 , and Rand Rindependently represent hydrogen claim 1 , methyl or ethyl.5. The method of claim 1 , wherein the composition further includes a spinosyn selected from the group consisting of spinetoram claim 1 , spinosad and mixtures thereof.6. The method of claim 1 , which further includes claim 1 , subsequent to said heating claim 1 , applying to a locus where control is desired an insect-inactivating amount of the composition.7. The method of claim 1 , wherein the heating is performed at a minimum of about 50° C. from about four to about seventy two hours.9. The method of claim 8 , wherein the heating is performed at a minimum of about 50° C. from about four to about seventy two hours.10. The method of claim 8 , wherein the composition includes a spinosyn selected from the group consisting of spinetoram claim 8 , spinosad and mixtures thereof.11. The method of claim 8 , wherein X represents NOor CN claim 8 , Y represents —CFand Rand Rindependently represent hydrogen claim 8 , methyl or ethyl.12. A composition claim 8 , comprising a stereoisomeric mixture of {1-[6-(trifluoromethyl)pyridin-3-yl]ethyl}(methyl)oxido-λ-sulfanylidenecyanamide defined by a first pair of diastereomers and a second pair of diastereomers claim 8 , wherein the first and second pairs of diastereomers are present at a ratio of at least about 3:1.13. The composition of claim 12 , wherein the first and second pairs of diastereomers are present at a ratio from about 3:1 to about 100:1.14. The composition of claim 12 , wherein the first and second pairs of diastereomers are present at a ratio from about 3:1 to about 40:1.15. The composition of claim 12 , wherein the first pair of diastereomers is defined by {(R)-1-[6 ...

NITRILE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS

Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I 2. A method according to claim 1 , wherein the compound is one wherein Z is sulphur.4. A method according to claim 1 , with the proviso that said composition does not contain S-cyanomethylisothiourea HBr.5. A method according to claim 1 , wherein the compound is selected from S-(3-cyanopropyl)isothiourea claim 1 , S-(2-cyanoethyl)isothiourea claim 1 , S-(4-cyanobutyl)isothiourea claim 1 , S-(5-cyanopentyl)isothiourea claim 1 , S-(4-cyanomethylphenyl)methylisothiourea claim 1 , S-2(4-[2-cyanoethyl]phenyl)ethylisothiourea claim 1 , S-(2-cyanomethylphenyl)methylisothiourea claim 1 , S-(6-cyanomethylpyridin-2-yl)methylisothiourea claim 1 , S-(3-cyanomethylphenyl)methylisothiourea claim 1 , S-(1-cyanomethylnaphth-2-yl))methylisothiourea claim 1 , and their pharmaceutically acceptable salts.6. A method according to claim 1 , wherein the hyperproliferative disease is cellular hyperproliferation such as cancer.7. A method according to claim 6 , wherein said hyperproliferative disease is selected from resistant non-small cell lung cancer claim 6 , breast cancer claim 6 , colon cancer claim 6 , squamous cell carcinoma cancer claim 6 , prostate cancer claim 6 , head and neck cancer and glioma.8. A method according to claim 6 , wherein said medicament is administered prior to radiation treatment.9. A method according to claim 1 , wherein said medicament is for treatment of a condition selected from inflammatory diseases claim 1 , viral infections or bacterial infections.10. A method according to claim 1 , wherein said medicament is formulated for administration of a dose of 200 mg/kg three times per week.11. A method according to claim 1 , wherein said medicament is for use in conjunction with 5-FU.12. A pharmaceutical composition comprising a compound as specified in .13. A pharmaceutical composition according to ...

PROCESSES AND REAGENTS FOR MAKING DIARYLIODONIUM SALTS

This invention relates to processes and reagents for making diaryliodonium salts, which are useful for the preparation of fluorinated and radiofluorinated aromatic compounds. 2. The process of claim 1 , wherein the process is carried out in the absence of added acid.3. The process of claim 1 , wherein the process utilizes (1-chloromethyl-4-fluoro-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate).4. The process of claim 1 , wherein the process utilizes (1-fluoro-4-methyl-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate).5. The process of claim 1 , wherein the process utilizes N-fluoro-2 claim 1 ,3 claim 1 ,4 claim 1 ,5 claim 1 ,6-pentachloropyridinium tetrafluoroborate.6. The process of claim 1 , wherein the process utilizes less than 2 equivalents of (1-chloromethyl-4-fluoro-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate) claim 1 , (1-fluoro-4-methyl-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate) claim 1 , or optionally substituted N-fluoropyridinium tetrafluoroborate for 1 equivalent of the compound of Formula II.7. The process of claim 1 , wherein the process utilizes less than 1.5 equivalents of (1-chloromethyl-4-fluoro-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate) claim 1 , (1-fluoro-4-methyl-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate) claim 1 , or optionally substituted N-fluoropyridinium tetrafluoroborate for 1 equivalent of the compound of Formula II.8. The process of claim 1 , wherein each X is claim 1 , independently claim 1 , a ligand that is a conjugate base of an acid HX claim 1 , wherein HX has a pKa of less than or equal to 5.9. The process of claim 1 , wherein each X is O(C═O)CH.10. The process of claim 1 , wherein the tetravalent silicon moiety is (R)Si—X claim 1 , wherein each Ris claim 1 , independently claim 1 , Calkyl or aryl.11. The process of claim 10 , wherein each Ris methyl.12. The process of claim 10 , wherein (R)Si—X is (CH)Si—X.13. The ...

NOVEL HETEROARYLAMIDE DERIVATIVES HAVING ANTIANDROGENIC PROPERTIES

The invention relates to novel heteroarylamide derivatives having formula (I) and N-oxides, stereoisomers and pharmaceutically acceptable salts thereof, where R, R, R1 1, R′, R″, z and X are as defined in the claims. The arylamide derivatives of formula (I) have antiandrogenic properties. The invention also relates to compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising them and to their preparation. 7. Heteroarylamide derivative according to claim 6 , where R1″ claim 6 , R4″ claim 6 , R5″ claim 6 , R6 and R10 are hydrogen; R2″ is trifluoromethyl or halo claim 6 , especially chloro; R3″ is cyano; R8 is CFor halo claim 6 , especially chloro or fluoro; R9 is hydrogen or halo claim 6 , especially fluoro; z is 0 or 1 (R′═R″═H); X is SO; and R11 is alkyl claim 6 , especially methyl claim 6 , ethyl claim 6 , tert-butyl claim 6 , cyclopropyl claim 6 , isopropyl claim 6 , or isopentyl claim 6 , or phenyl or pyridinyl optionally substituted with halo claim 6 , especially chloro claim 6 , when z is 0 claim 6 , or phenyl optionally substituted with halo claim 6 , especially chloro claim 6 , when z is 1.9. Heteroarylamide derivative according to claim 8 , where R1 claim 8 , R5 claim 8 , R6′ claim 8 , R7′ and R10′ are hydrogen; R2 is trifluoromethyl or halo claim 8 , especially chloro; R3 is cyano; R8′ is halo claim 8 , especially chloro or fluoro; R9′ is hydrogen or halo claim 8 , especially fluoro; z is 0; X is SO; and R11 is alkyl claim 8 , especially methyl claim 8 , ethyl claim 8 , tert-butyl claim 8 , cyclopropyl claim 8 , isopropyl claim 8 , or isopentyl.11. Heteroarylamide derivative according to claim 10 , where R1 claim 10 , R5 claim 10 , R6 claim 10 , R7 and R10 are hydrogen; R2 is trifluoromethyl or halo claim 10 , especially chloro; R3 is cyano; R8 is halo claim 10 , especially chloro or fluoro; R9 is hydrogen or halo claim 10 , especially fluoro; z is 0; X is SO; and R11 is alkyl claim 10 , especially isopropyl.12. ...

Substituted 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides and methods of making the same

The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them. In particular, the present invention relates to various 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides as useful intermediates in the preparation of compounds including

Electrolyte additive for lithium battery, electrolyte including the additive, and lithium battery including the electrolyte

An electrolyte additive for a lithium battery, an electrolyte including the electrolyte additive, and a lithium battery including the electrolyte additive are disclosed. The electrolyte additive for a lithium battery includes a sulfonylmethylisocyanide-based compound. The electrolyte additive including the sulfonylmethylisocyanide-based compound may form a protective layer having improved high-temperature stability on positive and negative electrodes of a lithium battery, thereby improving the safety of the lithium battery.

INDENOPYRIDINE DERIVATIVES

Disclosed is a compound of formula (I) 19-. (canceled)14. The method of claim 13 , wherein the palladium catalyst is Pd(dba)or Pd(OAc).16. The compound of formula (V) of claim 15 , wherein X is iodo.17. The compound of formula (V) of claim 15 , wherein X is bromo.19. The method of claim 18 , wherein X is iodo. This application relates to indenopyridine derivatives. The indenopyridine derivatives of the invention are useful as intermediates for the preparation of pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors.Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridines are reportedly useful as inhibitors of 11-β-hydroxysteroid hydrogenase type 1 (“11-β-HSD1”) and for treatment of disorders associated with 11β-HSD1 activity including, for example, diabetes mellitus (e.g., type II diabetes), obesity, symptoms of metabolic syndrome, glucose intolerance, hyperglycemica (see, e.g., WO 2011/057054).The aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridines can be prepared, for example, from nitrile-substituted hexahydroindenopyridines as described in WO 2011/057054. In one method described in WO 2011/057054, the intermediate (4aR,9aS)-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine-6-carbonitrile (A) is allowed to react with 1H-benzoimidazole-5-carboxylic acid (B) followed by reaction with hydrogen chloride to provide the 11-β-HSD1 inhibitor (4a-R,9a-S)-1-(1H-benzoimidazole-5-carbonyl)-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine-6-carbonitrile (C) as depicted below:Methods of preparing the compound of formula (A) described in WO 2011/057054 include a 13-step synthesis and a low overall yield (˜2.9%). In addition, some of the described methods utilize corrosive and/or toxic reagents (e.g., trifluoromethanesulfonic acid anhydride (TfO), boron tribromide (BBr) and Zinc cyanide (Zn(CN)), which produce a problematic by-product stream. Thus, there is a need, for improved processes for making ...

CARBOXYLIC ACID COMPOUND, METHOD FOR PREPARATION THEREOF, AND USE THEREOF

The present invention relates to the technical field of medicine, and specifically relates to the carboxylic acid compound represented by the chemical formula I or chemical formula II, and a pharmaceutically acceptable salt, a prodrug, and a solvate thereof, and a method for preparation thereof, as well as a pharmaceutical composition containing the described substances, and a use thereof. 116-. (canceled)27. A pharmaceutical composition comprising the carboxylic acid compound according to claim 17 , or a pharmaceutically acceptable salt thereof claim 17 , and a pharmaceutically acceptable carrier. The invention relates to pharmaceutical technical field, specifically, to carboxylic acid compounds and pharmaceutically acceptable salts, prodrugs, and solvates thereof and preparation methods thereof, and to pharmaceutical compositions comprising the same and uses thereof.Uric acid is the final metabolite of diet and purine in human body. In vivo environment (pH 7.4, 37 degrees), uric acid is present in blood mainly in the form of sodium salt of uric acid, the serum uric acid value of normal people is generally lower than 6 mg/dL. When uric acid in serum exceeds 7 mg/dL (Shi, et al., Nature 2003, 425: 516-523), sodium salt of uric acid will crystallize out and precipitate on joints and other parts of the body, and result in disorders such as gout, urinary stones, kidney stones, etc. Patients with gout are often accompanied with other complications, including hypertension, diabetes, hyperlipidemia, dyslipidemia, atherosclerosis, obesity, metabolic disease, nephropathy, cardiovascular disease, and respiratory disease, etc. (Rock, Et al., Nature Reviews Rheumatology 2013, 9: 13-23). In 2002, Japanese scientists Endou group reported that anion transport channel protein URAT1 is a major protein responsible for reabsorption of uric acid in kidney, they also found that the blood uric acid in people with URAT1 gene mutation (causing the synthesis of such protein being ...

Methods of producing sulfilimine compounds

Methods of producing a sulfilimine compound, such as N-cyano-S-methyl-S-[1-(6-trifluoromethyl-3-pyridinyl)ethyl]sulfilimine or other substituted sulfilimine compound. The method includes combining a sulfide compound, cyanamide, a hypochlorite compound, and a base, and oxidizing the sulfide compound to form the sulfilimine compound. The sulfide compound may include a 2-trifluoromethyl-5-(1-substituted)alkyl-thiopyridine compound. The base may include sodium hydroxide. A buffer, such as a phosphate buffer, may, optionally, be used in the reaction.

COMPOUND AND ORGANIC ELECTRONIC DEVICE USING THE SAME

Provided are a novel compound and an organic electronic device using the same. The novel compound is represented by the following Formula (I): 2. The compound as claimed in claim 1 , wherein the polycyclic aromatic ring extended from Xand Xis selected from the group consisting of: a substituted or unsubstituted naphthalene ring claim 1 , a substituted or unsubstituted anthracene ring claim 1 , a substituted or unsubstituted phenanthrene ring claim 1 , a substituted or unsubstituted fluorene ring claim 1 , a substituted or unsubstituted pyrene ring claim 1 , a substituted or unsubstituted benzophenanthrene ring claim 1 , a substituted or unsubstituted benzopyrene ring claim 1 , a substituted or unsubstituted fluoranthene ring claim 1 , and a substituted or unsubstituted benzofluoranthene ring.4. The compound as claimed in claim 1 , wherein the aryl ring extended from Xand Xis a substituted or unsubstituted 6 to 60-membered carbon ring.5. The compound as claimed in claim 4 , wherein the substituted or unsubstituted 6 to 60-membered carbon ring is selected from the group consisting of: a substituted or unsubstituted benzene ring claim 4 , a substituted or unsubstituted naphthalene ring claim 4 , a substituted or unsubstituted anthracene ring claim 4 , a substituted or unsubstituted phenanthrene ring claim 4 , a substituted or unsubstituted flourene ring claim 4 , a substituted or unsubstituted pyrene ring claim 4 , a substituted or unsubstituted benzophenanthrene ring claim 4 , a substituted or unsubstituted benzopyrene ring claim 4 , a substituted or unsubstituted fluoranthene ring claim 4 , and a substituted or unsubstituted benzofluoranthene ring.6. The compound as claimed in claim 4 , wherein the substituted or unsubstituted 6 to 60-membered carbon ring is a substituted or unsubstituted benzene ring.7. The compound as claimed in claim 1 , wherein at least one of Zto Zin formula (I) is selected from the group consisting of: an alkyl group having 1 to 40 carbon atoms ...

Two-Photon Fluorescent Compounds for Specific Lipid Droplet Imaging in Live Cells and Deep Tissues at Ultralow Concentration

Fluorescent compounds that have aggregation-induced emission (AIE) characteristics. The compounds can be utilized as lipid droplet (LD)-specific bio-probes in cell imaging, with high photostability and brightness. For example, the compounds can be used for specific two-photon LDs staining in live cells and deep-tissues at ultralow concentrations. The compounds exhibit a large Stokes shift (>110 nm), high solid fluorescence quantum yields (up to 0.30), a good two-photon absorption cross-section (45-100 GM at 860 nm), high biocompatibility, and good photostability. 3. A method of cellular imaging , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'contacting a target cell with the compound of ; and'}identifying a target of interest in the target cell using an imaging method.4. The method of claim 3 , wherein the target of interest comprises lipid droplets.5. The method of claim 3 , wherein the imaging method is selected from the group consisting of fluorescence microscopy and confocal laser scanning microscopy.6. The method of claim 5 , wherein the fluorescence microscopy comprises two-photon fluorescence imaging.7. The method of claim 3 , wherein the target cell is a live cell.8. The method of claim 7 , wherein the target cell is in live tissue.9. The method of claim 3 , wherein a concentration of the compound is 50 nM or less.11. A method of cellular imaging claim 3 , comprising:{'claim-ref': {'@idref': 'CLM-00010', 'claim 10'}, 'contacting a target cell with the compound of ; and'}identifying a target of interest in the target cell using an imaging method.12. The method of claim 11 , wherein the target of interest comprises lipid droplets.13. The method of claim 11 , wherein the imaging method is selected from the group consisting of fluorescence microscopy and confocal laser scanning microscopy.14. The method of claim 11 , wherein the fluorescence microscopy comprises two-photon fluorescence imaging.15. The method of claim 11 , wherein the target cell ...

ORGANIC COMPOUND, AND ORGANIC LIGHT EMITTING DIODE AND ORGANIC LIGHT EMITTING DISPLAY DEVICE INCLUDING THE SAME

An embodiment of the present invention provides an organic compound represented by following Formula: 2. The organic compound according to claim 1 , wherein all of Rto Rare the cyano group.3. The organic compound according to claim 1 , wherein A is one of benzene claim 1 , naphthalene claim 1 , pyridine claim 1 , diazine claim 1 , dibenzofurane and dibenzothiophene.6. The organic light emitting diode according to claim 5 , wherein all of Rto Rare the cyano group.7. The organic light emitting diode according to claim 5 , wherein A is one of benzene claim 5 , naphthalene claim 5 , pyridine claim 5 , diazine claim 5 , dibenzofurane and dibenzothiophene.9. The organic light emitting diode according to claim 5 , wherein a lowest unoccupied molecular orbital (LUMO) level of the organic compound is substantially equal to or smaller than a highest occupied molecular orbital (HOMO) level of the first hole transporting layer.10. The organic light emitting diode according to claim 5 , wherein the hole injection layer further includes a host material claim 5 , and an LUMO level of the organic compound is substantially equal to or smaller than a HOMO level of the host material.11. The organic light emitting diode according to claim 5 , further comprising:a second emitting part between the first emitting part and the electron auxiliary layer and including a second hole transporting layer; anda charge generation layer between the first and second emitting parts,wherein the charge generation layer includes the organic compound.13. The organic light emitting diode according to claim 12 , wherein all of Rto Rare the cyano group.14. The organic light emitting diode according to claim 12 , wherein A is one of benzene claim 12 , naphthalene claim 12 , pyridine claim 12 , diazine claim 12 , dibenzofurane and dibenzothiophene.16. The organic light emitting diode according to claim 12 , wherein an LUMO level of the organic compound is substantially equal to or smaller than a HOMO level of ...

Malononitrile Compounds for Controlling Animal Pests

The invention relates to the use of a compound of formula (I) 132-. (canceled)34. The compound of claim 33 , wherein{'sup': 5', '6', 'a, 'sub': 5', '1', '6', '2', '6', '2', '6, 'each R, Ris independently selected from the group consisting of halogen, cyano, azido, nitro, —SCN, SF, C-Calkyl, C-Calkenyl, C-Calkynyl, wherein the carbon atoms of the aforementioned aliphatic radicals are unsubstituted or substituted with one or more R;'}{'sub': 3', '8', '3', '8, 'sup': 'b', 'C-Ccycloalkyl or C-Ccycloalkenyl, wherein the carbon atoms of the aforementioned cycloaliphatic radicals are unsubstituted or substituted with one or more R;'}{'sup': 'c', 'phenyl unsubstituted or substituted with up to 5 R;'}{'sub': '2', 'sup': 'd', 'a 3-, 4-, 5-, 6- or 7-membered saturated, partially unsaturated or aromatic heterocyclic ring containing 1, 2 or 3 heteroatoms or heteroatom groups selected from the group consisting of N, O, S, NO, SO, SO, wherein the aforementioned ring is unsubstituted or substituted with up to 5 R;'}{'sup': e', 'f', 'f', 'h', 'h', 'i', 'i', 'm', 'm', 'm', 'f', 'i', 'm', 'm, 'sub': 3', 'x', 'x', '2, 'Si(R), OR, SR, OS(O)R, S(O)R, N(R), N(R)C(═O)R, OC(═O)R, C(═O)R, C(═O)OR, C(═NR)R, C(═S)R;'}or{'sup': 5', 'K', 'K', '5, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '3, 'two Ron two adjacent carbon atoms present on one phenyl ring are together a bridge selected from the group consisting of CHCHCHCH, N═CH—CH═CH, CH═N—CH═CH, N═CH—N═CH, OCHCHCH, OCH═CHCH, CHOCHCH, OCHCHO, OCHOCH, CHCHCH, CH═CHCH, CHCHO, CH═CHO, CHOCH, CHC(═O)O, C(═O)OCH, O(CH)O, SCHCHCH, SCH═CHCH, CHSCHCH, SCHCHS, SCHSCH, CHCHS, CH═CHS, CHSCH, CHC(═S)S, C(═S)SCH, S(CH)S, CHCHNR, CHCH═N, CH═CH—NR, OCH═N, SCH═N and form together with the carbon atoms the two Rare bonded to a 5- or 6-membered partially ...

NOVEL PHENICOL ANTIBACTERIAL AGENTS

The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical compositions containing these novel compounds, and methods for the preparation of these compounds. 2. A compound of wherein X and Y are each chloro claim 1 , or X and Y are each fluoro.5. A compound of wherein Ris —H or —CN claim 4 , Ris —CH claim 4 , and Z is —CH— or absent.6. A compound of selected from the group consisting of:2,2-difluoro-N-((1R,2S)-3-fluoro-1-hydroxy-1-(4-(6-(S-methylsulfonimidoyl)-pyridin-3-yl)phenyl)propan-2-yl)acetamide;2,2-difluoro-N-{(1S,2R)-1-fluoromethyl-2-hydroxy-2-[4-(6-N-(cyano)methyl pyridine sulfoximine-3-yl)phenyl]-ethyl}-acetamide;2,2-dichloro-N-((1R,2S)-3-fluoro-1-hydroxy-1-(4-(6-(S-methylsulfonimidoyl)-pyridin-3-yl)phenyl)propan-2-yl)acetamide;2,2-difluoro-N-{(1S,2R)-1-fluoromethyl-2-hydroxy-2-[4-(6-(S-methylsulfonimidoylmethyl)pyridine-3-yl)-phenyl]-ethyl}-acetamide; and2,2-difluoro-N-{(1S,2R)-1-fluoromethyl-2-hydroxy-2-[4-(6-N-[(cyano)methyl]-methyl pyridine sulfoximine-3-yl)-phenyl]-ethyl}-acetamide.7. A compound of wherein W is absent and Z is absent.9. A compound of wherein Ris —H or —CN and Ris —CHor —CH—F.10. A compound of selected from the group consisting of2,2-dichloro-N-((1R,2S)-3-fluoro-1-hydroxy-1-(4-(S-methylsulfonimidoyl)phenyl) propan-2-yl)acetamide;2,2-dichloro-N-[(1S,2R)-1-fluoromethyl-2-hydroxy-2-(4-(cyano)methyl-phenyl sulfoximine)-ethyl]-acetamide;2,2-difluoro-N-[(1S,2R)-1-fluoromethyl-2-hydroxy-2-(4-(cyano)methyl-phenyl sulfoximine)-ethyl]-acetamide;2,2-dichloro-N-((1R,2S)-3-fluoro-1-(4-(S-(fluoromethyl)sulfonimidoyl)phenyl)-1-hydroxypropan-2-yl)acetamide; and2,2-dichloro-N-((1R,2S)-3-fluoro-1-(4-(S-(fluoromethyl)sulfonimidoyl)phenyl)-1-hydroxypropan-2-yl)acetamide.13. A compound of wherein X and Y are each chloro or X and Y are each fluoro.14. A compound of selected from the group consisting of:2,2-difluoro-N-((1R,2S)-3-fluoro-1-hydroxy-1-(4-(6-(S-methylsulfonimidoyl)-pyridin-3-yl) ...

INSECTICIDAL N-SUBSTITUTED (6-HALOALKYLPYRIDIN-3-YL)-ALKYL SULFOXIMINES

N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects. 2. A compound of in which X represents NOor CN.3. A compound of in which Y represents —CF.4. A compound of in which Rand Rindependently represent hydrogen claim 1 , methyl or ethyl.7. A compound of in which X represents NOor CN claim 6 , Y represents CF claim 6 , Rrepresents methyl or ethyl claim 6 , Rand Rindependently represent hydrogen claim 6 , methyl or ethyl claim 6 , and n is an integer from 1-3.87. A composition for controlling insects which comprises a compound of any one of - in combination with a phytologically-acceptable carrier.97. A method of controlling insects which comprises applying to a locus where control is desired an insect-inactivating amount of a compound of any one of -.10. A process comprising submitting data related to a compound of directly to a governmental or regulatory authority or indirectly through another to a governmental or regulatory authority in order to gain approval for the use or sale or both of said compound. This application is a continuation of, and claims the benefit of, U.S. patent application Ser. No. 14/158,103, which was filed on Jan. 17, 2014, which is a continuation of, and claims the benefit of, U.S. patent application Ser. No. 13/558,378, now U.S. Pat. No. 8,669,278, which was filed on Jul. 26, 2012, which is a division of, and claims the benefit of, U.S. patent application Ser. No. 12/706,513, now U.S. Pat. No. 8,269,016, which was filed on Feb. 16, 2010, which is a division of, and claims the benefit of, U.S. patent application Ser. No. 11/704,842, now U.S. Pat. No. 7,687,634, which was filed on Feb. 9, 2007, which claims priority from, and benefit of: U.S. provisional application 60/836,044, which was filed on Aug. 7, 2006; and U.S. provisional application 60/772,108, which was filed on Feb. 10, 2006. The entire contents of these applications are incorporate by reference into this application.The present invention ...

Process for the preparation of certain substituted sulfilimines

Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides, cyanamide and hypochlorite by adding the sulfide to a solution of the cyanamide and hypochlorite in the presence of a nitrile solvent while maintaining the pH from about 8 to about 12.

POLYCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING DEVICE INCLUDING THE SAME

The present specification provides a polycyclic compound and an organic light emitting device including the same. 4. The compound of claim 3 , wherein Ain Chemical Formula 3 is hydrogen; a nitrile group; a substituted or unsubstituted pyridyl group; or a substituted or unsubstituted benzimidazole group; and Ais hydrogen; a nitrile group; a substituted or unsubstituted pyridyl group; a substituted or unsubstituted benzimidazole group; or a substituted or unsubstituted benzoimidazophenanthridine group.10. An organic light emitting device comprising:a first electrode;a second electrode provided opposite to the first electrode; andone or more organic material layers provided between the first electrode and the second electrode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein one or more layers of the organic material layers include the compound of .'}11. The organic light emitting device of claim 10 , wherein the organic material layer including the compound is an electron transfer layer. This application claims priority to and the benefits of Korean Patent Application No. 10-2014-0127112, filed with the Korean Intellectual Property Office on Sep. 23, 2014, the entire contents of which are incorporated herein by reference.The present specification relates to a polycyclic compound and an organic light emitting device including the same.An organic light emission phenomenon generally refers to a phenomenon converting electrical energy to light energy using an organic material. An organic light emitting device using an organic light emission phenomenon normally has a structure including an anode, a cathode, and an organic material layer therebetween. Herein, the organic material layer is often formed in a multilayer structure formed with different materials in order to increase efficiency and stability of the organic light emitting device, and for example, may be formed with a hole injection layer, a hole transfer layer, a light emitting layer, an electron ...

ANTIFUNGAL COMPOUND PROCESS

The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof. 4. The process of any one of - , wherein forming the trimethylsilyl-cyanohydrin is performed in the presence of a chiral catalyst.8. The process of claim 7 , wherein Z is phenyl claim 7 , p-tolyl claim 7 , methyl claim 7 , or ethyl.9. The process of claim 7 , wherein the crystallization solvent or crystallization solvent mixture is ethyl acetate claim 7 , isopropyl acetate claim 7 , ethanol claim 7 , methanol claim 7 , or acetonitrile claim 7 , or combinations thereof.10. The process of claim 7 , wherein the crystallization co-solvent or crystallization co-solvent mixture is pentane claim 7 , methyl tert-butylether claim 7 , hexane claim 7 , heptane claim 7 , or toluene claim 7 , or combinations thereof.11. The process of claim 7 , wherein forming the trimethylsilyl-cyanohydrin is performed in the presence of a chiral catalyst.12. The process of claim 11 , further comprising enriching the enantiomeric purity of amino-alcohol 1-6 or 1-7 to afford enantio-enriched amino-alcohol 1-6* or 1-7*.13. The process of claim 7 , further comprising enriching the enantiomeric purity of amino-alcohol 1-6 or 1-7 to afford enantio-enriched amino-alcohol 1-6* or 1-7*. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/955,633 filed Mar. 19, 2014, which is expressly incorporated by reference herein.This invention was created in the performance of a Cooperative Research and Development Agreement with the National Institutes of Health, an Agency of the Department of Health and Human Services. The Government of the United States has certain rights in this invention.The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide a new ...

ORALLY BIOAVAILABLE CAFFEIC ACID RELATED ANTICANCER DRUGS

The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as inhibitors of Jak2/STAT3 pathways and downstream targets and inhibit the growth and survival of cancerous cell lines. 2. The method of claim 1 , wherein Ris selected from the group consisting of cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl and cyclohexyl.3. The method of claim 1 , wherein Ris selected from the group consisting of phenyl claim 1 , benzyl claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl and cyclohexyl.4. The method of claim 1 , wherein Xor Xis selected from the group consisting of —F claim 1 , —Cl claim 1 , —Br and —I.5. The method of claim 1 , wherein Ris selected from a group consisting of hydroxy claim 1 , acetoxy and 2 claim 1 ,2-dimethylpropionyloxy.6. The method of claim 1 , wherein Xor Xis selected from the group consisting of methoxy claim 1 , —F claim 1 , —Cl claim 1 , —Br and —I.7. The method of claim 1 , wherein Ror Ris selected from the group consisting of methyl and cyclopropyl.8. The method of claim 1 , wherein Xis selected from a group consisting of methyl and acetoxymethyl.9. The method of claim 1 , wherein A is —S(O)—.10. (canceled)1244.-. (canceled)4686.-. (canceled)87. The method of claim 1 , wherein the subject is a mammal.88. The method of claim 87 , wherein the mammal is a human.89. (canceled)90. The method of claim 1 , wherein the cell proliferative disease is cancer.91. The method of claim 90 , wherein the cancer is melanoma claim 90 , non-small cell lung claim 90 , small cell lung claim 90 , lung claim 90 , hepatocarcinoma claim 90 , retinoblastoma claim 90 , astrocytoma claim 90 , glioblastoma claim 90 , leukemia claim 90 , blood claim 90 , brain claim 90 , skin claim 90 , eye claim 90 , tongue claim 90 , gum claim 90 , neuroblastoma claim 90 , head claim 90 , neck claim 90 , breast claim 90 , pancreatic claim 90 , renal claim 90 ...

N-TYPE SEMICONDUCTOR, AND ORGANIC PHOTOELECTRIC DEVICE, IMAGE SENSOR, AND ELECTRONIC DEVICE INCLUDING THE SAME

Disclosed are an n-type semiconductor including compound represented by Chemical Formula 1 or Chemical Formula 2, an image sensor, and an electronic device. 2. The n-type semiconductor of claim 1 , wherein L claim 1 , L claim 1 , and Lare independently a C1 to C30 alkylene group substituted with an electron withdrawing functional group claim 1 , a C2 to C30 alkenylene group substituted with an electron withdrawing functional group claim 1 , or a C2 to C30 alkynylene group substituted with an electron withdrawing functional group.3. The n-type semiconductor of claim 1 , wherein the electron withdrawing functional group is a halogen claim 1 , a C1 to C10 haloalkyl group claim 1 , a cyano group (—CN) claim 1 , a cyano-containing group claim 1 , a nitro group (—NO) claim 1 , a C1 to C10 carboxyl group claim 1 , a C2 to C30 N-containing heteroaryl group claim 1 , or a carbonyl group (—C(═O)R claim 1 , wherein R is a C1 to C10 alkyl group claim 1 , a C2 to C10 heteroalkyl group claim 1 , a C6 to C14 aryl group claim 1 , or a C2 to C10 heteroaryl group).5. The n-type semiconductor of claim 4 , wherein L claim 4 , L claim 4 , and Lare independently a C1 to C30 alkylene group substituted with an electron withdrawing functional group claim 4 , a C2 to C30 alkenylene group substituted with an electron withdrawing functional group claim 4 , or a C2 to C30 alkynylene group substituted with an electron withdrawing functional group.6. The n-type semiconductor of claim 4 , wherein the electron withdrawing functional group is a halogen claim 4 , a C1 to C10 haloalkyl group claim 4 , a cyano group (—CN) claim 4 , a cyano-containing group claim 4 , a nitro group (—NO) claim 4 , a C1 to C10 carboxyl group claim 4 , a C2 to C30 N-containing heteroaryl group claim 4 , or a carbonyl group (—C(═O)R claim 4 , wherein R is a C1 to C10 alkyl group claim 4 , a C2 to C10 heteroalkyl group claim 4 , a C6 to C14 aryl group claim 4 , or a C2 to C10 heteroaryl group.8. The n-type semiconductor of ...

Substituted 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides and methods of making the same

The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them. In particular, the present invention relates to various 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides as useful intermediates in the preparation of compounds including

PROCESS FOR THE PREPARATION OF CERTAIN SUBSTITUTED SULFILIMINES

Cyano-substituted sulfilimines are produced efficiently and in high yield from the corresponding sulfides, cyanamide and hypochlorite by adding the sulfide to a solution of the cyanamide and hypochlorite in the presence of a nitrile solvent while maintaining the pH from about 8 to about 12. 18-. (canceled) This application claims the benefit of U.S. patent application Ser. No. 14/101,536, which was filed on 10 Dec. 2013, which claims the benefit of, and priority from, U.S. Provisional Application Ser. No. 61/735,573, which was filed on 11 Dec. 2012, and the benefit of, and priority from, U.S. Provisional Application Ser. No. 61/735,612, which was filed on 11 Dec. 2012, the entire disclosures of these applications is hereby incorporated by reference.The present invention concerns an improved process for preparing certain cyano-substituted sulfilimines.Cyano-substituted sulfilimines are useful intermediates for the preparation of certain new insecticidal sulfoximines; see, for example, U.S. Pat. Nos. 7,678,920 B2 and 7,687,634 B2. U.S. Pat. No. 7,868,027 B2 describes the manufacture of substituted sulfilimines by the reaction of the corresponding sulfide with cyanamide and hypochlorite solution in a suitable organic solvent. While the hypochlorite process of U.S. Pat. No. 7,868,027 B2 is preferable to the iodobenzene diacetate process described in U.S. Pat. Nos. 7,678,920 B2 and 7,687,634 B2, it is plagued by significant levels of competing byproducts derived from the sulfide starting materials. It would be advantageous to produce the substituted sulfilimines efficiently and in higher yield from the corresponding sulfides by the hypochlorite route.Thus, the present invention concerns a process for preparing certain substituted sulfilimines, having the general structure of (I),wherein X represents halogen, C-Calkyl or C-Chaloalkyl which comprises mixing a sulfide of formula (II)wherein X is as previously definedwith an aqueous solution of cyanamide and hypochlorite at ...

SUBSTITUTED PYRIDINES AS SODIUM CHANNEL BLOCKERS

The invention relates to substituted pyridine and pyrimidine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R, R, R, A, A, X, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain. 2. (canceled)8. (canceled)9. The compound of claim 1 , wherein Ris —NRR claim 1 , and Rand Rare each independently selected from the group consisting of hydrogen and alkyl claim 1 , or a pharmaceutically acceptable salt or solvate thereof.1017-. (canceled)18. The compound of claim 1 , wherein Aselected from the group consisting of optionally substituted phenyl claim 1 , optionally substituted 2-pyridyl claim 1 , optionally substituted 3-pyridyl claim 1 , and optionally substituted 4-pyridyl claim 1 , or a pharmaceutically acceptable salt or solvate thereof.19. The compound of claim 18 , wherein the optional substituents of the Agroup are selected from the group consisting of halo claim 18 , cyano claim 18 , haloalkyl claim 18 , and Calkyl claim 18 , or a pharmaceutically acceptable salt or solvate thereof.20. (canceled)22. (canceled)23. The compound of claim 21 , wherein one or two of R claim 21 , R claim 21 , R claim 21 , R claim 21 , and Rare halo or haloalkyl claim 21 , and the others are hydrogen claim 21 , or a pharmaceutically acceptable salt or solvate thereof.24. (canceled)2628-. (canceled)29. The compound of claim 25 , wherein one of R claim 25 , R claim 25 , and R claim 25 , are halo or haloalkyl claim 25 , and the others are hydrogen claim 25 , or a pharmaceutically acceptable salt or solvate thereof.30. The compound of claim 1 , wherein Z is N claim 1 , or a pharmaceutically acceptable salt or solvate thereof.31. The compound of claim 1 , wherein Z is CR claim 1 , and Ris hydrogen claim 1 , or a ...

NOVEL MICROBIOCIDES

Compounds of formula (I) wherein the other substituents HetAr, R, R, R, R, R, R, Rand Rare as defined in claim , and their use in compositions and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds. 2. The compound of formula (I) according to characterized in thatHetAr is an optionally substituted monocyclic heteroaromatic moietyn is an integer with a value of 0, 1 or 2{'sup': 1', '2, 'Rand Rare independently fluoride or chloride'}{'sup': 1', '2, 'or Rand Rtogether with the carbon atom to which they are attached form an optionally substituted 3- to 6-membered ring, optionally containing an oxygen, sulphur or nitrogen atom'}{'sup': '3', 'sub': '3', 'Ris hydroxy, alkoxy, haloalkoxy, cyano, halo, or —OSi(alkyl)'}{'sup': '4', 'sub': 1', '6', '1', '6', '3', '6', '3', '6, 'Ris C-Calkyl, C-Chaloalkly, optionally substituted C-Ccycloalkyl or an optionally substituted C-Chalocycloalkyl'}{'sup': '5', 'sub': 1', '4', '1', '4', '1', '4', '1', '4, 'Ris independently C-Calkyl, cyano, C-Chaloalkyl, C-Calkoxy, halogen, or C-Chaloalkoxy'}m is an integer with a value of 0, 1 or 2{'sup': '6', 'sub': 1', '6', '1', '6', '3', '6', '2', '5', '6', '10', '1', '3, 'Ris C-Calkyl, C-Chaloalkyl, optionally substituted C-Ccycloalkyl, optionally substituted C-Cheterocyclyl, optionally substituted C-Caryl or an optionally substituted C-Cheteroaromatic and agronomically acceptable salts thereof.'}{'sup': 1', '2', '6, 'sub': 1', '7, 'When n is equal to 1: R, Rand Rtogether can form a triple bond to form an optionally substituted C-Calkynyl'}{'sup': 7', '8, 'sub': 1', '4', '1', '4, 'Rand Rare independently hydrogen, C-Calkyl or C-Chaloalkyl'}{'sup': 7', '8, 'or Rand Rtogether with the carbon atoms to which they are attached form an optionally substituted 3- to 6-membered ring, optionally containing an oxygen, sulphur or nitrogen atom.'}3. The compound of formula (I) according to ...

Probe for dual-mode bio-imaging

The present subject matter relates to compounds that have aggregation-induced emission (AIE) characteristics and are capable of generating Raman signals in the Raman cell-silent region (1800 cm −1 -2800 cm −1 ). The compounds can be used in dual-mode cell imaging by fluorescence and Raman microscopes

CATHEPSIN CYSTEINE PROTEASE INHIBITORS

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

CATECHOL DIETHERS AS POTENT ANTI-HIV AGENTS

The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection. 2. A compound according to wherein Rand R′ are each independently H claim 1 , halogen claim 1 , CN claim 1 , NO claim 1 , NH claim 1 , NHCHor morpholinylethoxy.3. A compound according to wherein either of Rand R′ is H.4. A compound according to wherein Rand R′ are independently H or a halogen.5. A compound according to wherein Ris Cl or F and R′ is H.6. A compound according to wherein X and Y are each independently H claim 1 , halogen claim 1 , CN claim 1 , NO claim 1 , (E)-cyanovinyl claim 1 , methoxyethoxy or 3-hydroxypropan-1-oxy.7. A compound according to wherein X′ and Y′ are both O claim 1 , j claim 1 , jand nare each a bond and j is 1 or 2.8. A compound according to wherein Rp is a pyrimidine attached at the N−1 position and substituent R claim 1 , attached at the 5-position of the pyrimidine claim 1 , is H claim 1 , CH claim 1 , F claim 1 , Cl claim 1 , Br or I.9. A compound according to wherein Rp is a uracil group attached at the N−1 position and Ris H or CH.12. A compound according to wherein Rand R′ are each independently H claim 11 , halogen claim 11 , CN claim 11 , NO claim 11 , NH claim 11 , NHCH. or a morpholinylethoxy group.13. A compound according to wherein Rand R′ are H or a halogen.14. A compound according to wherein Ris Cl or F and R′ is H.15. A compound according to wherein Ris H claim 11 , a halogen or CN.16. A compound according to wherein X′ and Y′ are both O claim 11 , j claim 11 , jand nare each a bond and j is 1 or 2.17. A compound according to wherein Rp is a pyrimidine attached at the N−1 position and substituent R claim 11 , and attached at the 5-position of the pyrimidine is H claim 11 , CH claim ...

COMPOUND AND ORGANIC ELECTRONIC DEVICE USING THE SAME

Provided are a novel compound and an organic electronic device using the same. The novel compound is represented by the following Formula (I): 2. The compound as claimed in claim 1 , wherein h claim 1 , i claim 1 , j claim 1 , k claim 1 , l are each independently an integral of 1 to 2 claim 1 , and the total of h claim 1 , i claim 1 , j claim 1 , k claim 1 , and l is not more than 6.6. The compound as claimed in claim 5 , wherein Rand Rare each selected from the group consisting of: the pyridine group claim 5 , the pyrimidine group claim 5 , the pyrazine group claim 5 , the pyridazine group claim 5 , the cyano group claim 5 , the nitro group claim 5 , the trifluoromethyl group claim 5 , the fluoro group claim 5 , the phenylpyridine group claim 5 , the phenylpyrimidine group claim 5 , the phenylpyrazine group claim 5 , the phenylpyridazine group claim 5 , the cyanophenyl group claim 5 , the nitrophenyl group claim 5 , and the trifluoromethylphenyl group.9. The compound as claimed in claim 1 , wherein Gto Gare each independently selected from the group consisting of: a hydrogen atom claim 1 , a deuterium atom claim 1 , a halogen group claim 1 , a nonsubstituted alkyl group having 1 to 12 carbon atoms claim 1 , a nonsubstituted alkenyl group having 2 to 12 carbon atoms claim 1 , and a nonsubstituted alkynyl group having 2 to 12 carbon atoms.10. The compound as claimed in claim 1 , wherein Gand Gare the same.11. The compound as claimed in claim 1 , wherein Gand Ware the same.13. An organic electronic device claim 1 , comprising a first electrode claim 1 , a second electrode claim 1 , and an organic layer disposed between the first electrode and the second electrode claim 1 , wherein the organic layer comprises the compound as claimed in .14. The organic electronic device as claimed in claim 13 , wherein the organic electronic device is an organic light emitting device.15. The organic electronic device as claimed in claim 14 , wherein the organic light emitting device ...

VIOLOGEN-BASED ROTAXANES

Disclosed herein are nanoactuating rotaxanes comprising a threading component, the threading component comprising a oligoviologen, and at least two macrocylic components, wherein the oligoviologen is threaded through each of the macrocylic components. Also disclosed are methods for making and using the rotaxanes. 1. An nanoaccuator comprising a rotaxane ,wherein the rotaxane comprises a threading component and at least two macrocylic components;wherein the threading component comprises a oligoviologen; andwherein the threading component is threaded through each of the macrocylic components.2. The nanoaccuator of claim 1 , wherein the threading component further comprises a first linking subunit claim 1 , L claim 1 , and/or a second linking subunit claim 1 , L′.3. The nanoaccuator of claim 1 ,wherein the threading component further comprises a first stopper, S, and/or a second stopper, S′.4. The nanoaccuator of claim 2 ,wherein the threading component further comprises a first stopper, S, and/or a second stopper, S′ andwherein the L links a first end of the oligoviologen to S and the L′ links a second end of the oligoviologen to the S′.5. The nanoaccuator of claim 1 , wherein the oligoviologen comprises n+1 viologen subunits claim 1 , V claim 1 , and wherein n is an integer.6. The nanoaccuator of claim 5 , wherein V is a BIPY subunits.7. The nanoaccuator of claim 1 , wherein the oligoviolgen further comprises n bridging subunits claim 1 , B claim 1 , linking the viologen subunits.8. The nanoaccuator of claim 7 , wherein B is a paraxylene subunit.9. The nanoaccuator of claim 5 , wherein n is 3 or 4.10. The nanoaccuator of claim 1 , wherein the at least two macrocylic components are CBPQT macrocylic components.11. The nanoaccuator of claim 2 , wherein the first linking subunit claim 2 , L claim 2 , the second linking subunit claim 2 , L′ claim 2 , or both the first linking subunit and the second linking subunit comprise an alkyl subunit.12. The nanoaccuator of claim 2 ...

DEUBIQUITINASE INHIBITORS AND METHODS FOR USE OF THE SAME

Disclosed herein are methods of inhibiting a deubiquitinase (DUB) by contact with a compound of formula (I) 2. The compound of claim 1 , wherein Rand Rtogether form a nitrogen-containing optionally substituted heteroaryl.4. The compound of any one of to claim 1 , wherein Ris propyl or isopentyl.5. The compound of or claim 1 , wherein R is hydrogen and Ris a heterocyclyl substituted alkoxy.6. The compound of claim 5 , wherein Ris —Oalkyleneheterocyclyl.7. The compound of or claim 5 , wherein Ris hydrogen and R is a heterocyclyl substituted alkoxy.8. The compound of claim 7 , wherein R is —Oalkyleneheterocyclyl.9. The compound of any one of to claim 7 , wherein the heterocyclyl is morpholinyl claim 7 , sulfoxymorpholinyl claim 7 , pyrrolidinyl claim 7 , piperazinyl claim 7 , or piperidinyl.10. The compound of claim 9 , wherein the heterocyclyl is morpholinyl.11. The compound of or claim 9 , wherein Ror R is —O(CH)N(Me)(CH)NMe; —O(CH)N(Me)(CH)NHMe; —O(CH)N(Me)(CH)NEt; —O(CH)N(Me)(CH)NHEt; —O(CH)O(CH)NMe; —O(CH)O(CH)NHMe; —O(CH)O(CH)NEt; or —O(CH)O(CH)NHEt claim 9 , and m is 1 claim 9 , 2 claim 9 , 3 claim 9 , 4 claim 9 , 5 claim 9 , 6 claim 9 , 7 claim 9 , 8 claim 9 , 9 claim 9 , or 10.12. The compound of any one of and - claim 9 , wherein Rand Rare each halo.13. The compound of claim 12 , wherein Rand Rare the same.14. The compound of claim 12 , wherein Rand Rare different.15. The compound of claim 12 , claim 12 , or claim 12 , wherein at least one of Rand Ris chloro.16. The compound of claim 15 , wherein each of Rand Ris chloro.17. The compound of claim 15 , claim 15 , claim 15 , or claim 15 , wherein at least one of Rand Ris fluoro.18. The compound of claim 17 , wherein each of Rand Ris fluoro.21. A pharmaceutical composition comprising the compound of any one of - and a pharmaceutically acceptable excipient.22. The pharmaceutical composition of formulated for oral claim 21 , topical claim 21 , intravenous claim 21 , subcutaneous claim 21 , intramuscular claim 21 , ...

METALLOENZYME INHIBITOR COMPOUNDS AS FUNGICIDES

The instant invention describes compounds of Formula I having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. 239-. (canceled) This application claims the benefit of U.S. Provisional Patent Application Ser. Nos. 61/979,540 filed Apr. 15,2014 and 62/047,384 filed Sep. 8, 2014, which are expressly incorporated by reference herein.Fungicides are compounds, of natural or synthetic origin, which act to protect and/or cure plants against damage caused by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consequently, research is ongoing to produce fungicides that may have better performance, are easier to use, and cost less.The present disclosure relates to metalloenzyme inhibitors and their use as fungicides. The compounds of the present disclosure may offer protection against ascomycetes, basidiomycetes, deuteromycetes and oomycetes.One embodiment of the present disclosure may include compounds of Formula I:Where:Z is optionally substituted 5-pyrimidinyl, optionally substituted 4-pyrimidinyl, optionally substituted thiazolyl, optionally substituted oxazolyl, or optionally substituted 3-pyridinyl;Ris alkyl, haloalkyl, aryl, heteroaryl, each optionally substituted with 0,1,2 or 3 independent R;Ris aryl or heteroaryl each optionally substituted with 0,1,2 or 3 independent R;Ris independently H, alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl, —C(O)alkyl, or —Si(alkyl), each optionally substituted with 0,1,2 or 3 independent R;R, R, R, and Rare independently H, alkyl, haloalkyl, alkoxy, halo, or cyano; andRis independently aryl, heteroaryl, alkyl, thioalkyl, cyano, haloalkyl, cyanoalkyl, hydroxy, alkoxy, halo, haloalkoxy, —C(O)alkyl, —C(O)OH, —C(O)O-alkyl, —SCF, —SF, —SCN, or —SO-alkyl.Another embodiment of the present disclosure may include a fungicidal composition for the control or prevention of fungal attack comprising the compounds ...

CARBOXYLIC ACID COMPOUND, METHOD FOR PREPARATION THEREOF, AND USE THEREOF

The present invention relates to the technical field of medicine, and specifically relates to the carboxylic acid compound represented by the chemical formula I or chemical formula II, and a pharmaceutically acceptable salt, a prodrug, and a solvate thereof, and a method for preparation thereof, as well as a pharmaceutical composition containing the described substances, and a use thereof. 116-. (canceled)18. The carboxylic acid compound according to claim 17 , or pharmaceutically acceptable salt claim 17 , prodrug claim 17 , or solvate thereof claim 17 ,wherein:{'sup': a', 'b, 'Rand Rare each independently hydrogen, C1-3 alkyl or bond to each other to form a substituted or unsubstituted benzene ring structure, wherein the substituent in the substituted benzene ring structure is halogen, C1-3 alkyl or C1-3 alkoxy;'}{'sup': 'c', 'Ris —CN, carboxyl, hydroxyl-substituted or unsubstituted C1-3 alkyl, hydroxyl-substituted or unsubstituted C3-5 cycloalkyl, hydroxyl-substituted or unsubstituted 3- to 5-membered heterocycloalkyl containing 1 to 3 heteroatom(s) selected from O, S and N.'}20. The carboxylic acid compound according to claim 17 , or pharmaceutically acceptable salt claim 17 , prodrug claim 17 , or solvate thereof claim 17 ,wherein:A is S;M is H;{'sup': a', 'b, 'Rand Rare each independently hydrogen, or bond to each other to form a benzene ring;'}{'sup': 'c', 'Ris —CN, carboxyl, methyl, ethyl, propyl, hydroxymethyl, hydroxyethyl, hydroxypropyl, cyclopropyl, cyclobutyl, hydroxyl-substituted cyclopropyl, hydroxyl-substituted cyclobutyl, oxiranyl, oxetanyl, hydroxyl-substituted oxiranyl or hydroxyl-substituted oxetanyl.'}22. The carboxylic acid compound according to claim 17 , wherein M is Na.23. A pharmaceutical composition comprising the carboxylic acid compound according to claim 17 , or pharmaceutically acceptable salt claim 17 , prodrug claim 17 , or solvate thereof claim 17 , and a pharmaceutically acceptable carrier.24. A method of promoting excretion of ...

Photoelectric conversion element, dye-sensitized solar cell, metal complex dye, dye solution, dye-adsorbed electrode, and method for producing dye-sensitized solar cell

A photoelectric conversion element, having a photoconductor layercontaining semiconductor fine particles carrying a metal complex dye of Formula (I); a metal complex dye, a dye solution, a dye-adsorbed electrode, a dye-sensitized solar cell, and a method for producing the solar cell: M ( LA )( LD )( LX ) mX ·( CI ) mY   Formula (I) M represents a metal ion, LA represents a ligand of Formula (AL), LD represents a bidentate or tridentate ligand, at least one of coordinating atoms being an anion; LX represents a monodentate ligand; CI represents a counter ion; mX is 0 or 1; mY is 0 to 3; Rings A to C represent a heterocycle; Z 1 and Z 2 represent a carbon or nitrogen atom; Anc1 to Anc3 represent an acidic group; X 1 to X 3 represent a single bond or linking group; R 1 to R 3 represent a substituent; l1, l3, l2, m1, m3, m2, n1, n2, and n3 each are an integer.

CATALYTIC HYDROGENATION OF NITRILES

The present invention relates to a novel catalytic hydrogenation of substituted 2-methyl cyanopyridyl derivatives, in particular 3-chloro-5-(trifluoromethyl)pyridin-2-yl]acetonitrile [=Py-CN] to substituted 2-ethylaminopyridine derivatives, in particular 2-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]ethanamine [=Py-ethanamine] or salts thereof in the presence of metal catalysts, in particular palladium catalysts. 2. A process according to claim 1 , further comprisingin (B3), adding a solvent and an acid to a reaction mixture comprising a precipitated compound according to formula (I).3. A process according tocomprising in (B4), separating an organic phase comprising a compound according to formula (I) from a water phase.4. A process according to claim 3 , comprisingin (B2), adding a base to a reaction mixture.5. A process according towherein p is 1 or 2;q is 1;Y is independently of the others, as being fluorine, chlorine, or difluoromethyl, trifluoromethyl, dichloromethyl, trichloromethyl; andthe phenyl moiety is substituted by Y in 2- and/or in 6-position;X is independently of the others, as being fluorine, chlorine, or difluoromethyl, trifluoromethyl, dichloromethyl, trichloromethyl; andthe 2-pyridyl moiety is substituted by X in 3- and/or in 5-position.6. A process according to claim 1 ,wherein the compound according to formula (I) is (N-[2-[3-chloro-5-(trifluoromethyl)-2-pyridinyl]ethyl]-2-(trifluoromethyl)benzamide). This application is a divisional application of U.S. patent application Ser. No. 15/033,987, filed 3 May 2016, which is a 371 National Stage entry of PCT/EP2014/074212, filed 11 Nov. 2014, which claims priority to EP 13193164.4, filed 15 Nov. 2013. The disclosures of the priority applications are incorporated in their entirety herein by reference.The present invention relates to a novel catalytic hydrogenation of substituted 2-methyl cyanopyridyl derivatives, wherein the substitution is present on the pyridine ring, in particular 3-chloro-5-( ...

PYRIDINE COMPOUNDS AND THE USES THEREOF

The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R, A, A, E, G, Z, and Zare defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain. 36-. (canceled)89-. (canceled)1115-. (canceled)1718-. (canceled)2025-. (canceled)26. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , or solvate claim 1 , thereof claim 1 , wherein:{'sup': '1', 'Ais selected from the group consisting of optionally substituted aryl and optionally substituted heteroaryl;'}X is —O—; and{'sup': '2', 'Ais optionally substituted phenyl.'}2730-. (canceled)31. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , or solvate thereof claim 1 , wherein Aselected from the group consisting of:a) optionally substituted phenyl;b) optionally substituted pyridin-2-yl;c) optionally substituted pyridin-3-yl; andd) optionally substituted pyridin-4-yl.33. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , or solvate thereof claim 1 , wherein Rand Rare each hydrogen.3536-. (canceled)3842-. (canceled)4447-. (canceled)4951-. (canceled)52. The compound of claim 33 , wherein E is optionally substituted heteroaryl or halogen.5375-. (canceled)76. A pharmaceutical composition claim 1 , comprising the compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , or solvate thereof claim 1 , and a pharmaceutically acceptable carrier.7780-. (canceled)81. A method for treating pain in a mammal claim 1 , comprising administering an effective amount of a compound as claimed in claim 1 , or a pharmaceutically acceptable salt claim 1 , or solvate thereof claim 1 , to a mammal in need of such treatment.8283-. (canceled)84. The method of claim 81 , wherein said pain is ...

SUBSTITUTED 4-CYAN-3-PHENYL-4-(PRYRIDINE-3-YL)BUTANOATES, PROCESSES FOR PREPARATION THEREOF AND USE THEREOF AS HERBICIDES AND PLANT GROWTH REGULATORS

Substituted 4-cyano-3-phenyl-4-(pyridin-3-yl)butanoates, processes for their preparation and their use as herbicides and plant growth regulators 2. Compound and/or salt thereof according to claim 1 , wherein{'sup': '1', 'Rrepresents hydrogen or an optionally substituted hydrocarbon radical or an optionally substituted heterocyclyl radical, where each of the two last-mentioned carbon-containing radicals including substituents has 1 to 30 carbon atoms, optionally 1 to 24 carbon atoms, 1 to 20 carbon atoms, or'}{'sup': 1', 'a', 'b', 'c', 'a', 'b', 'c', 'd, 'claim-text': {'sup': a', 'b', 'c', 'd', 'a', 'b', 'c', 'a', 'b', 'a', 'b', 'c', 'd', 'c', 'd', 'a', 'b', 'e', 'd, 'sub': '3', 'where in the 3 last-mentioned formulae each of the radicals R, R, Rand Rindependently of the others represents hydrogen or an optionally substituted hydrocarbon radical, where, however, SiHfor SiRRRis excluded, or Rand Rtogether with the nitrogen atom of the group —NRRrepresent a 3- to 9-membered heterocycle which, in addition to the nitrogen atom, may contain one or two further ring heteroatoms from the group consisting of N, O and S and which is unsubstituted or substituted, or Rand Rtogether with the carbon atom of the group —N═CRRrepresent a 3- to 9-membered carbocyclic radical or a heterocyclic radical which may contain 1 to 3 ring heteroatoms from the group consisting of N, O and S, where the carbocyclic or heterocyclic radical is unsubstituted or substituted, where each of the radicals R, R, Rand Rincluding substituents has up to 30 carbon atoms, or'}, 'Rrepresents a radical of the formula SiRRR, —NRRor —N═CRR,'}{'sup': 1', 'e', 'f', 'e', 'f', '1', '1', '1', '1', '1, 'sub': 2', '1', '8', '1', '4', '2', '8', '2', '8', '1', '6', '1', '6', '1', '8', '1', '6', '1', '8', '1', '4', '1', '4', '1', '8', '1', '4', '1', '8', '3', '8', '3', '8', '1', '8', '3', '8', '1', '8', '3', '8', '3', '8', '1', '8', '3', '8', '1', '8', '1', '4', '1', '4', '1', '8', '3', '6', '3', '6', '1', '8', '3', '6', '1 ...

METALLOENZYME INHIBITOR COMPOUNDS AS FUNGICIDES

The instant invention describes compounds of Formula I having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. 2. The compound according to wherein Ris methyl claim 1 , ethyl claim 1 , tert-butyl claim 1 , iso-propyl claim 1 , cyclopropyl claim 1 , trifluoromethyl claim 1 , 2 claim 1 ,4-difluorophenyl claim 1 , 2-fluoro-4-chlorophenyl claim 1 , —CF-(2 claim 1 ,4-difluorophenyl) claim 1 , —CF-(2-fluoro-4-chlorophenyl) claim 1 , —CH-(2 claim 1 ,4-difluorophenyl) claim 1 , or —CH-(2-fluoro-4-chlorophenyl)3. The compound according to wherein Z is optionally substituted 5-pyrimidinyl claim 1 , optionally substituted 4-pyrimidinyl claim 1 , or optionally substituted 3-pyridinyl.4. The compound according to wherein Z is 5-pyrimidinyl or 3-pyridinyl.5. The compound according to wherein Ris phenyl claim 1 , 2-pyridinyl claim 1 , 3-pyridinyl claim 1 , or 5-pyrimidinyl optionally substituted with 0 claim 1 , 1 claim 1 , 2 or 3 independent R.6. The compound according to wherein Ris halo claim 5 , haloalkyl claim 5 , cyanoalkyl claim 5 , haloalkoxy claim 5 , or cyano.7. The compound according to wherein Ris phenyl substituted at the 4 position with a halo claim 5 , haloalkyl claim 5 , cyanoalkyl claim 5 , haloalkoxy claim 5 , or cyano.8. The compound according to wherein Ris 2-pyridinyl substituted at the 5 position with a halo claim 5 , haloalkyl claim 5 , cyanoalkyl claim 5 , haloalkoxy claim 5 , or cyano.9. The compound according to wherein Ris 3-pyridinyl substituted at the 6 position with a halo claim 5 , haloalkyl claim 5 , cyanoalkyl claim 5 , haloalkoxy claim 5 , or cyano substituent.10. The compound according to wherein Rand Rare independently H claim 1 , CF claim 1 , methyl claim 1 , or halo.11. The compound according to wherein Rand Rare both H.12. The compound according to wherein Rand Rare both F.13. The compound according to wherein Rand Rare both Cl.14. The compound according to ...

METALLOENZYME INHIBITOR COMPOUNDS AS FUNGICIDES

The instant invention describes compounds of Formula I having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. 118-. (canceled)21. The method according to claim 20 , wherein the disease or disorder is cancer claim 20 , cardiovascular disease claim 20 , endocrinologic disease claim 20 , inflammatory disease claim 20 , infectious disease claim 20 , gynecologic disease claim 20 , metabolic disease claim 20 , opthalmologic disease claim 20 , central nervous system (CNS) disease claim 20 , urologic disease claim 20 , or gastrointestinal disease.22. The method according to claim 20 , wherein the disease or disorder is systemic fungal infection claim 20 , mucosal infection claim 20 , or dermal infection.2332-. (canceled)34. The composition according to claim 33 , further comprising an additional therapeutic agent.35. The composition according to claim 33 , further comprising an additional therapeutic agent that is an anti-cancer agent claim 33 , antifungal agent claim 33 , cardiovascular agent claim 33 , antiinflammatory agent claim 33 , chemotherapeutic agent claim 33 , an anti-angiogenesis agent claim 33 , cytotoxic agent claim 33 , an anti-proliferation agent claim 33 , metabolic disease agent claim 33 , opthalmologic disease agent claim 33 , central nervous system (CNS) disease agent claim 33 , urologic disease agent claim 33 , or gastrointestinal disease agent.3639-. (canceled) This application claims the benefit of U.S. Provisional Patent Application Ser. Nos. 61/979,540 filed Apr. 15, 2014 and 62/047,384 filed Sep. 8, 2014, which are expressly incorporated by reference herein.Fungicides are compounds, of natural or synthetic origin, which act to protect and/or cure plants against damage couased by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consquently, research is ongoing to produce fungicides that may have better performance, are easier ...

Thioamides and Amides for Controlling Animal Pests

The invention relates to the use of a compound of formula (I) 136-. (canceled)38. The method of claim 37 , wherein{'sup': 5', '5, 'Y is phenyl unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents R; or naphthyl unsubstituted or substituted with 1 or 2 substituents R;'}{'sup': 6', '6', '6', '6, 'Q is phenyl unsubstituted or substituted with 1, 2, 3 or 4 substituents R; cyclohexyl unsubstituted or substituted with 1 or 2 substituents R; cyclopentyl unsubstituted or substituted with 1 or 2 substituents R; or a 6-membered aromatic heterocyclic ring containing 1, 2 or 3 nitrogen atoms in the ring, wherein the aforementioned ring is unsubstituted or substituted with 1, 2, 3 or 4 substituents R;'}{'sup': '1', 'sub': 1', '6', '2', '6', '2', '6', '3', '6', '1', '6', '1', '6', '3', '1', '6', '2', '6', '2', '6', '3', '6', '1', '6', '1', '6, 'Ris selected from the group consisting of H, halogen, cyano, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl or (C-C-alkoxy)carbonyl, wherein the five radicals last mentioned are unsubstituted or substituted with 1, 2 or 3 substituents selected from halogen, cyano, hydroxy, OSi(C-C-alkyl), C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl, C-C-alkoxy and (C-C-alkoxy)carbonyl,'}wherein the six radicals last mentioned are unsubstituted or partially or fully halogenated;{'sup': '2', 'Ris selected from the group consisting of H and halogen;'}or{'sup': 1', '2, 'Rand Rform together with the carbon atom to which they are attached a methylene group;'}{'sup': '3', 'sub': 1', '6', '2', '6', '2', '6', '3', '6', '1', '6', '1', '6', '3', '1', '6', '2', '6', '2', '6', '3', '6', '1', '6', '1', '6, 'Ris selected from the group consisting of H, halogen, cyano, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl or (C-C-alkoxy)carbonyl, wherein the five radicals last mentioned are unsubstituted or substituted with 1, 2 or 3 substituents selected from halogen, cyano, hydroxy, OSi(C-C-alkyl), C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl ...

Poly-Cyanostilbene Macrocycles

The present disclosure concerns synthesis and anion binding features of poly-cyanostilbene macrocycles of Formula (I): 112-. (canceled)14. The complex of claim 13 , wherein R claim 13 , R claim 13 , R claim 13 , R claim 13 , and Rcomprise identical substituents.15. The complex of claim 13 , wherein R claim 13 , R claim 13 , R claim 13 , R claim 13 , and Rcomprise tert-butyl groups.17. The complex of claim 13 , wherein the anion is selected from BF claim 13 , ClO claim 13 , PF claim 13 , N(SOCF) claim 13 , N(SOCF) claim 13 , CHSO claim 13 , CFSO claim 13 , AsO claim 13 , AsF claim 13 , AlCl claim 13 , PO claim 13 , HPO claim 13 , HPO claim 13 , SO claim 13 , HSO claim 13 , B(CN) claim 13 , Cl claim 13 , Br claim 13 , I claim 13 , cyanide claim 13 , BrO claim 13 , IO claim 13 , F claim 13 , HF claim 13 , TcO claim 13 , RPO claim 13 , RPO claim 13 , RSO claim 13 , SCN claim 13 , N claim 13 , I claim 13 , CO claim 13 , HCO claim 13 , FeCl claim 13 , PtCl claim 13 , S where n=1-8 claim 13 , and x=1 or 2 claim 13 , PO claim 13 , HPO claim 13 , HPO claim 13 , HPO claim 13 , a polyphosphate polyanion claim 13 , a tetrazine anion claim 13 , a dithiadiazolide anion claim 13 , RBF claim 13 , Ar—O claim 13 , wherein R comprises a substituent.19. The complex of claim 18 , wherein R claim 18 , R claim 18 , R claim 18 , and Rcomprise identical substituents.20. The complex of claim 18 , wherein R claim 18 , R claim 18 , R claim 18 , and Rcomprise tert-butyl groups.22. The complex of claim 18 , wherein the anion is selected from BF claim 18 , ClO claim 18 , PF claim 18 , N(SOCF) claim 18 , N(SOCF) claim 18 , CHSO claim 18 , CFSO claim 18 , AsO claim 18 , AsF claim 18 , AlCl claim 18 , PO claim 18 , HPO claim 18 , HPO claim 18 , SO claim 18 , HSO claim 18 , B(CN) claim 18 , Cl claim 18 , Br claim 18 , I claim 18 , cyanide claim 18 , BrO claim 18 , IO claim 18 , F claim 18 , HF claim 18 , TcO claim 18 , RPO claim 18 , RPO claim 18 , RSO claim 18 , SCN claim 18 , N claim 18 , I claim ...

COMPOUNDS FOR USE AS GPR120 AGONISTS

The present invention relates to a compound of formula (I), or a tautomer, stereoisomer, geometrical isomer, prodrug, carboxylic acid isostere, solvate, polymorph, N-oxide, S-oxide or pharmaceutically acceptable salt thereof, which are GPR120 agonists. The present invention also relates to a pharmaceutical composition of a compound of formula (I) for the treatment of metabolic disorders, particularly Type 2 diabetes and associated diseases. 3. A compound according to claim 1 , wherein{'sup': 1', '2, 'Rand Rare combined together with one or two atoms of Ring A to formi) a 3- to 8-membered, partly saturated or saturated carbocycle; orii) a 3- to 8-membered, saturated heterocycle which contains 1, 2 or 3 heteroatoms independently selected from the group consisting of N, O and S;{'sub': 1', '6', '1', '6', '1', '6', '6', '10, 'wherein the carbocycle or heterocycle is unsubstituted or substituted with the one or more groups independently selected from the group consisting of (C-C)alkyl, halo(C-C)alkyl, (C-C)alkoxy, hydroxy, halogen, cyano, (C-C)aryl, heteroaryl and heterocyclyl.'}5. A compound according to claim 1 , wherein Ring A is 6- to 10-membered aromatic carbocycle claim 1 , wherein aromatic carbocycle is unsubstituted or substituted with one or more groups independently selected from the group consisting of (C-C)alkyl claim 1 , halo(C-C)alkyl claim 1 , hydroxy claim 1 , halogen claim 1 , (C-C)alkoxy claim 1 , halo(C-C)alkoxy claim 1 , (C-C)aryl claim 1 , (C-C)cycloalkyl claim 1 , heteroaryl claim 1 , heterocyclyl claim 1 , amino claim 1 , cyano claim 1 , nitro claim 1 , —C(O)O(C-C)alkyl claim 1 , —C(O)NRRand —S(O)R; wherein R claim 1 , R claim 1 , Rand t are as defined above.6. A compound according to claim 1 , wherein Ring A is phenyl; wherein phenyl is unsubstituted or substituted with one or more groups independently selected from the group consisting of (C-C)alkyl claim 1 , halo(C-C)alkyl claim 1 , hydroxy claim 1 , halogen claim 1 , (C-C)alkoxy claim 1 , halo( ...

Iodine(III)-Mediated Radiofluorination

A process for fluorination of aromatic compounds employing iodonium ylides and applicable to radiofluorination using 18 F is described. Processes, intermediates, reagents and radiolabelled compounds are described.

Poly-Cyanostilbene Macrocycles

The present disclosure concerns synthesis and anion binding features of poly-cyanostilbene macrocycles of Formula (I): 2. The poly-cyanostilbene macrocycle of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rcomprise identical substituents.3. The poly-cyanostilbene macrocycle of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rcomprise tert-butyl groups.5. The poly-cyanostilbene macrocycle of claim 1 , wherein Ris iodo and R claim 1 , R claim 1 , R claim 1 , and Rcomprise substituents other than iodo.6. The poly-cyanostilbene macrocycle of claim 5 , wherein R claim 5 , R claim 5 , R claim 5 , and Rcomprise identical substituents.7. The poly-cyanostilbene macrocycle of claim 6 , wherein R claim 6 , R claim 6 , R claim 6 , and Rcomprise tert-butyl groups.10. (canceled)11. The poly-cyanostilbene macrocycle of claim 9 , wherein R claim 9 , R claim 9 , R claim 9 , and Rcomprise tert-butyl groups.14. (canceled)15. The complex of claim 13 , wherein R claim 13 , R claim 13 , R claim 13 , R claim 13 , and Rcomprise tert-butyl groups.17. The complex of claim 13 , wherein the anion is selected from BF claim 13 , ClO claim 13 , PF claim 13 , N(SOCF) claim 13 , N(SOCF) claim 13 , CHSO claim 13 , CFSO) claim 13 , AsO claim 13 , AsF claim 13 , AlCl claim 13 , PO claim 13 , HPO claim 13 , HPO claim 13 , SO claim 13 , HSO claim 13 , B(CN) claim 13 , Cl claim 13 , Br claim 13 , I claim 13 , cyanide claim 13 , BrO claim 13 , IO claim 13 , F claim 13 , HF claim 13 , TcO claim 13 , RPO claim 13 , RPO claim 13 , RSO claim 13 , SCN claim 13 , N claim 13 , I claim 13 , CO claim 13 , HCO claim 13 , FeCl claim 13 , PtCl claim 13 , wherein R comprises a substituent.19. (canceled)20. The complex of claim 18 , wherein R claim 18 , R claim 18 , R claim 18 , and Rcomprise tert-butyl groups.22. The complex of claim 18 , wherein the anion is selected from BF claim 18 , ClO claim 18 , PF claim 18 , N(SOCF) claim 18 , N(SOCF) claim 18 , CHSO claim 18 , CFSO ...

Insecticidal n-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines

Ν-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects.

Ionic uv-a sunscreens and compositions containing them

The present invention relates to novel 1,4-dihydropyridine derivatives, to novel cosmetic or dermatological sunscreen compositions containing these derivatives and the use of these derivatives for photoprotecting human skin and/or hair against UV radiation, in particular solar radiation.

过渡金属催化的c-h偶联反应高效制备邻氰基化芳香环或不饱和脂肪环类化合物

本发明涉及一种基于N 1 ,N 3 ‑二取代咪唑型离子液体为溶剂，N‑氰基‑N‑苯基对甲苯磺酰胺为氰基源，过渡金属催化的C‑H偶联反应高效制备邻氰基化芳香环或不饱和脂肪环类化合物的绿色合成新方法。本发明相比于传统技术，更安全、简便、高效、环境友好；官能团容忍性好，收率高；溶剂和催化剂可循环使用，大大降低了成本；无需进行底物的预活化并且反应条件温和，降低了操作难度。可以快速高效地获得邻氰基化衍生物分子库，并且氰基可以进一步转化为羧基、氨基、杂环等功能基团，为天然产物以及药物分子的后期修饰提供重要帮助。

Photoelectric conversion element, dye-sensitized solar cell, metal complex dye, dye solution, dye-adsorbing electrode, and method for producing dye-sensitized solar battery

一种荧光探针及其制备方法和应用

本发明公开了一种荧光探针及其制备方法，该荧光探针具有式(1)中的化学结构式：

METHODS TO PRODUCE SULFYLIMINE COMPOUNDS

Reivindicación 1: Un método para producir un compuesto sulfilimina, que comprende: combinar un compuesto sulfido, cianamida, un compuesto de hipoclorito y una base; y oxidizar el compuesto sulfido para formar un compuesto sulfilimina. Reivindicación 2: El método de la reivindicación 1, que comprende adicionalmente un amortiguador al compuesto sulfido, cianamida, compuesto de hipoclorito y base. Reivindicación 3: El método de la reivindicación 1, en donde la combinación de un compuesto sulfido, cianamida, un compuesto de hipoclorito y una base comprende combinar cianamida, compuesto de hipoclorito y base con un compuesto sulfido que tiene la estructura química de fórmula (1) en donde Het es una parte seleccionada del grupo de fórmulas (2); X es una parte seleccionada del grupo que consiste en un halógeno, un alquilo C₁₋₄, un haloalquilo C₁₋₄, un alquenilo C₂₋₄, un alquinilo C₂₋₄, un haloalquenilo C₂₋₄, un alcoxi C₁₋₄, un haloalcoxi C₁₋₄, CN, NO₂, SOₘR⁶ donde m es un número entero de 0 - 2, COOR⁴ y CONR⁴R⁵; Y es una parte seleccionada del grupo que consiste en hidrógeno, un halógeno, un alquilo C₁₋₄, un haloalquilo C₁₋₄, un alquenilo C₂₋₄, un alquinilo C₂₋₄, un haloalquenilo C₂₋₄, un alcoxi C₁₋₄, un haloalcoxi C₁₋₄, CN, NO₂, SOₘR¹ donde m es un número entero de 0 - 2, COOR⁴, CONR⁴R⁵, arilo y heteroarilo; n es un número entero de 0 - 3; L es ya sea un enlace simple, -CH(CH₂)ₚ- donde R¹, S y L tomados juntos son un anillo de 4, 5 ó 6 miembros y p es un número entero de 1 - 3, -CH(CH₂OCH₂)- donde R¹, S y L tomados juntos son un anillo de 6 miembros, o -CH- donde L, R² y el carbono común al cual se conectan tomados juntos son un anillo de 4, 5 ó 6 miembros con hasta 1 heteroátomo, pero no más; R¹ es una parte seleccionada del grupo que consiste en un alquilo C₁₋₄, un haloalquilo C₁₋₄, un alquenilo C₃₋₆, un alquinilo C₃₋₆, un haloalquenilo C₃₋₆, un arilalquilo, un heteroarialquilo, o -CH₂-, en casos donde R¹, S y L tomados juntos son un anillo de 4, 5 ó 6 miembros; cada R² ...

다환 화합물 및 이를 포함하는 유기 발광 소자

본 명세서는 다환 화합물 및 이를 포함하는 유기 발광 소자를 제공한다.

헤테로고리 화합물 및 이를 포함하는 유기 발광 소자

본 출원은 유기 발광 소자의 수명, 효율, 전기 화학적 안정성 및 열적 안정성을 크게 향상시킬 수 있는 헤테로고리 화합물 및 상기 헤테로고리 화합물이 유기물층에 함유되어 있는 유기 발광 소자를 제공한다.

술필이민 화합물의 제조 방법

술필이민 화합물, 예컨대 N -시아노- S -메틸- S -[1-(6-트리플루오로메틸-3-피리디닐)에틸]술필이민 또는 다른 치환 술필이민 화합물의 제조 방법. 상기 방법은 술피드 화합물, 시안아미드, 차아염소산 화합물 및 염기를 배합하고, 술피드 화합물을 산화시켜 술필이민 화합물을 형성하는 것을 포함한다. 술피드 화합물은 2-트리플루오로메틸-5-(1-치환)알킬-티오피리딘 화합물을 포함할 수 있다. 염기는 수산화나트륨을 포함할 수 있다. 완충액, 예컨대 포스페이트 완충액이 선택적으로 반응에서 사용될 수 있다.

Indene derivative and method for producing the same

Stable insecticidal composition and method of its obtaining (versions)

FIELD: chemistry. SUBSTANCE: invention relates to agriculture. Obtaining an insecticidal composition, having the first ratio of stereoisomers of a compound, which has the following structure: and heating of the composition for 4-72 hours at a temperature of 23-70°C with obtaining the second, different ratio of stereoisomers are realised. EFFECT: invention makes it possible to increase the composition stability. 12 cl, 3 tbl, 9 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК A01N 47/40 A01N 43/22 A01P 7/04 C07D 213/26 C07D 213/34 C07D 409/04 (13) 2 523 293 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2011131067/13, 22.12.2009 (24) Дата начала отсчета срока действия патента: 22.12.2009 (72) Автор(ы): ЦИНЬ Куйдэ (US), БАУЧЕР Рэймонд Е. Мл. (US) (73) Патентообладатель(и): ДАУ АГРОСАЙЕНСИЗ, ЭлЭлСи (US) Приоритет(ы): (30) Конвенционный приоритет: R U 26.12.2008 US 61/203,600 (43) Дата публикации заявки: 10.02.2013 Бюл. № 4 (45) Опубликовано: 20.07.2014 Бюл. № 20 2 5 2 3 2 9 3 (56) Список документов, цитированных в отчете о поиске: US 2007/0203191 A1 30.08.2007. WO 2007/095229 A2 23.08.2007. WO 2007/149134 A1 27.12.2007. EA 10091 B1 30.06.2008 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 26.07.2011 (86) Заявка PCT: 2 5 2 3 2 9 3 R U (87) Публикация заявки PCT: C 2 C 2 US 2009/006670 (22.12.2009) WO 2010/074747 (01.07.2010) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" (54) СТАБИЛЬНАЯ ИНСЕКТИЦИДНАЯ КОМПОЗИЦИЯ И СПОСОБ ЕЁ ПОЛУЧЕНИЯ (ВАРИАНТЫ) (57) Реферат: Изобретение относится к сельскому хозяйству. Осуществляютполучение инсектицидной композиции, имеющей первое соотношение стереоизомеров соединения, имеющего следующую структуру: и нагревание композиции в течение 4-72 часов при температуре 23-70°С с получением второго, иного соотношения стереоизомеров. Изобретение Стр ...

Method for sulphylimin compounds production

FIELD: chemistry. SUBSTANCE: invention relates to a method for preparation of a sulphylimine compound, such as N-cyano-S-methyl-S-[1-(6-trifluoromethyl-3-pyridinyl)ethyl]sulfinylimine, or another substituted sulphylimine compound which includes reaction of a sulfide compound, cyanamide, hypochlorite and base, and sulphide compound oxidizing to produce a sulphylimine compound. A buffer compound, such as a phosphate buffer, may be optionally used in the reaction. EFFECT: method improvement. 17 cl, 4 tbl, 4 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 634 718 C2 (51) МПК C07D 213/34 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2014137257, 15.02.2013 (24) Дата начала отсчета срока действия патента: 15.02.2013 (72) Автор(ы): АДАУЭЙ Тимоти Дж. (US) (73) Патентообладатель(и): ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи (US) Дата регистрации: (56) Список документов, цитированных в отчете о поиске: WO 2008106006, A1, 04.09.2008. WO Приоритет(ы): (30) Конвенционный приоритет: 1998021178, A1, 22.05.1998. RU 2187507, C2, 20.08.2002. 16.02.2012 US 61/599,489 (45) Опубликовано: 03.11.2017 Бюл. № 31 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 16.09.2014 (86) Заявка PCT: US 2013/026377 (15.02.2013) (87) Публикация заявки PCT: 2 6 3 4 7 1 8 (43) Дата публикации заявки: 10.04.2016 Бюл. № 10 R U 03.11.2017 (54) СПОСОБ ПОЛУЧЕНИЯ СУЛЬФИЛИМИНОВЫХ СОЕДИНЕНИЙ (57) Реферат: Изобретение относится к способу получения соединения, цианамида, гипохлорита и основания, сульфилиминового соединения, такому как Nи окисление сульфидного соединения с циано-S-метил-S-[1-(6-трифторметил-3получением сульфилиминового соединения. В пиридинил)этил]сульфилимин, или другому реакции может быть необязательно использовано замещенному сульфилиминовому соединению, буферное соединение, такое как фосфатный который включает в себя реакцию сульфидного буфер. 2 н. и 15 з.п. ф-лы, 4 табл., 4 пр. R U 2 6 3 4 7 1 8 Адрес для переписки: 129090, Москва, ул. ...

N'-cyano-n-alkyl halide imide amide derivatives

N'-cyano-N-haloalkyl-imideamide derivatives

Die vorliegende Anmeldung betrifft neue substituierte N'-Cyano-N-halogenalkyl-imidamid-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Bekämpfung von tierischen Schädlingen, vor allem von Arthropoden, insbesondere Insekten. The present application relates to novel substituted N'-cyano-N-haloalkyl-imidamide derivatives, processes for their preparation and their use for controlling animal pests, especially of arthropods, in particular insects.

IMPROVED METHOD FOR PRODUCING N-CYANO-S- [1- (PYRIDIN-3-IL) Ethyl] -S-Methylsulfylimines

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2015 128 003 A (51) МПК C07D 213/34 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2015128003, 10.12.2013 (71) Заявитель(и): ДАУ АГРОСАЙЕНСИЗ ЭлЭлСи (US) Приоритет(ы): (30) Конвенционный приоритет: 11.12.2012 US 61/735,612; 11.12.2012 US 61/735,573 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 13.07.2015 US 2013/074006 (10.12.2013) (87) Публикация заявки PCT: R U Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" (54) УСОВЕРШЕНСТВОВАННЫЙ СПОСОБ ПОЛУЧЕНИЯ N-ЦИАНО-S-[1-(ПИРИДИН-3-ИЛ)ЭТИЛ] -S-МЕТИЛСУЛЬФИЛИМИНОВ (57) Формула изобретения 1. Способ получения сульфилиминов формулы (I), , где Х представляет собой галоген, C1-C4-алкил или C1-C4-галогеналкил, который включает в себя смешивание сульфида формулы (II) , где Х является таким, как определено выше, с водным раствором цианамида и 10-13% гипохлорита, при температуре от около -20°С до около 10°С в присутствии нитрильного растворителя при поддержании рН от около 8 до около 12. Стр.: 1 A 2 0 1 5 1 2 8 0 0 3 A WO 2014/093276 (19.06.2014) 2 0 1 5 1 2 8 0 0 3 (86) Заявка PCT: R U (43) Дата публикации заявки: 16.01.2017 Бюл. № 02 (72) Автор(ы): ГОНСАЛЕС Майкл А. (US), МЕЕСЕ Чад (US), ЧЕН Сяоюнь (US), ДЭН Флорин (US) 2. Способ по п. 1, в котором Х представляет собой CF3. 3. Способ по п. 1 или 2, в котором нитрильным растворителем является ацетонитрил. 4. Способ по п. 1 или 2, в котором температура составляет от около -15°С до около -5°С. 5. Способ по п. 1 или 2, в котором рН составляет от около 9 до около 11. 6 Способ по п. 1 или 2, в котором гипохлорит и сульфид одновременно добавляют к цианамиду, при условии, что около 10-30% гипохлорита добавляется к цианамиду перед началом добавления сульфида и первоначальный избыток гипохлорита относительно сульфида сохраняется в течение одновременного добавления. 7. Способ по п. 1 или 2, в котором рН ...

Photo-electric conversion element, solar cell and its manufacture method, compound, metal complex dye, pigment solution and electrode

本发明提供一种光电转换元件、金属络合物色素、色素溶液、色素吸附电极、色素增感太阳电池及其制造方法、及化合物，光电转换元件具有导电性支撑体、含电解质的感光体层、含电解质的电荷转移体层及对电极，且感光体层含有承载有式(I)所表示的金属络合物色素的半导体微粒子。本发明的光电转换元件及色素增感太阳电池对半导体微粒子表面的吸附稳定性或耐久性优异。M(LA)(LD)(LX) mX ·(CI) mY 式(I)M表示金属离子，LA表示式(AL)所表示的三齿配体，LD表示配位原子的至少一个为阴离子的二齿或三齿配体，LX表示单齿配体，CI表示反荷离子，mX表示0或1，mY表示0～3的整数。

Metal complex compound and organic electroluminescence device containing the same

A metal complex compound having a partial structure represented by the general formula: (I) [wherein the moiety B is a benzene ring residue having groups R1 to R4 which each independently represent H, etc. provided that at least one of the groups R1 to R4 is CN; R1 may be bonded with R2, R2 with R3 and R3 with R4 to thereby form a ring structure; the moiety A represents a C3-C20 cyclic structure having at least one C=N bond which may have a substituent and may form a ring structure with the above R4 included therein; and M is Ir, Rh, Pt or Pd]. There is further provided an organic electroluminescence device comprising a pair of electrodes and, interposed therebetween, one or multiple organic thin-film layers having at least a light emitting layer, wherein at least one of the organic thin-film layers contains the above metal complex compound. The organic electroluminescence device emits light when voltage is applied between the electrodes with high luminous efficiency, and the service life of the organic electroluminescence device is prolonged.

Method of producing 1-cyclohexyl-4-aryl-4-piperidincarboxylic acids derivatives or their stereochemical isomeric forms (versions)

1, Способ получени  производных 1-циклогексил-4-арил-4-пиперидинкар- боновой кислоты общей формулы С АГ R / v COR Ar где R - водород или низший алкил; R - гидроксил, низший алкоксил, низший алкокси - низший алкоксил , фенокси - низший алкилJ фенокси - низший алкоксил , в котором фенил может .быть замещен низшим ал- коксилом или низшим алкилом, амино , ди(низший алкил)ами- но , ди (низший алкил)амино- иизпгий алкоксил, 4-морфоли- нил. 1-пирролидинил, 1-пипе- ридинил, ( 1-пирролидинил} низший алкоксил или (4-мор- фолинил) - низший алкоксил; АГ и АГ -независимо один от другого фенил или фенил, моно- или дизамещенный разными группами , выбранными из атома галогена, низшего алкила, низшего алкокси, алкоксикар- бонила, трифторметила, или пиридинил, или тиенил, или их кислотно-аддитивных солей, или их стереохимических изомерных форм, отличающийс  тем, что провод т гидрогенизацию смеси соединений общих формул /;о (У) где R , R, Ar и Ar имеют указанные выше значени , в инертном органическом растворителе при 30-100 С в присутствии катализатора, такого как палладий на угле или платина на угле, с последующим вьщелением целевого продукта в свободном виде или в виде их кислотна-аддитивных,солей, или в виде стереохимических изомерных форм. 2. Способ получени  производных 1-циклогексил 4-арил-4-пиперидинкар- боновой кислоты общей формулы ю 00 о 4 Од СМ

Organic electroluminescent device and anthracene compound containing 2,6,9, 10-tetra-substitution

本发明涉及含有2,6,9,10‑位四取代的蒽化合物的有机电致发光器件，本发明的2,6,9,10‑位四取代的蒽化合物具有如下通式(1)所示的结构。由于本发明的化合物具有合适的HOMO和LUMO能级，载流子传输性能更佳，因而，本发明的有机电致发光器件具有更好地实用性能。采用本发明化合物与LiQ掺杂，或者本发明的两种化合物掺杂作为双层电子传输层材料所制备的有机电致发光器件能够在电压、效率以及寿命等方面对于非掺杂器件表现出更优的性质。

Compound, electron transport material and organic electroluminescent device

本申请提供了一种通式(I)的化合物，其可以用于电子传输材料。该化合物原子间的键能高，具有良好的热稳定性，并有利于分子间的固态堆积，电子的跃迁能力强，用作电子传输材料使用能有效降低有机电致发光器件驱动电压、提高其电流效率、延长其使用寿命。本申请还提供了一种包含通式(I)化合物的有机电致发光器件和显示装置。

Method of producing derivatives of 2-(3-pyridyl)-2-phenyl-aminoacetic acid (versions)

Nouveaux dérivés de l'acide (pyridyl-3)-2 phénylamino-2 acétique répondant à la formule: avec: R o : -CN, -COOH, CONH 2 , COOR 4 , R 1 : H, alkyle inférieur, cycloalkyle, phényle, éventuellement substitué, aralkyle éventuellement substitué, R 2 : H, alkyle inférieur, éventuellement substitué, Ar: phényle éventuellement substitué, Z: halogène, alkyle inférieur, alkoxy inférieur, alkylthio inférieur. Ils sont utilisables en agriculture pour la lutte contre les champignons phytopathogènes tels que les sclérotiniacées.

Organic compound having electron-transporting and/or hole-blocking performance and its use and OLEDs comprising the compound

Disclosed herein are several organic compounds having electron-transporting and/or hole-blocking performance and their preparation method and use and the OLEDs comprising the organic compound. The organic compounds exhibit high ionization potential (IP), electron affinity (Ea), glass transition temperature (Tg) and high electron mobility, and are a kind of good electron-transporting material with good hole-blocking ability. The devices comprising these compounds as one of the emitting layer, electron-transporting layer (ETL) and hole-blocking layer (HBL) show improved efficiency and better color purity.

Novel molecular structures with controllable electron conducting properties

Aromatic and heteroaromatic molecular structures with controllable electron conducting properties are derived from the incorporation of electron active substituents in selective positions. Such compounds can form self-assembled layers on metal or other substrates, and can be used in molecular scaled opto-electronic devices including field-effect transistors, light-emitting diodes and photovoltaic cells.

Molecular structures with controllable electron conducting properties

Aromatic and heteroaromatic molecular structures with controllable electron conducting properties are derived from the incorporation of electron active substituents in selective positions. Such compounds can form self-assembled layers on metal or other substrates, and can be used in molecular scaled opto-electronic devices including field-effect transistors, light-emitting diodes and photovoltaic cells.

3, 6-di (prop-2-ylidene) cyclohexa-1, 4-diene derivatives, methods of making, uses, and devices

本发明公开了3,6‑二(丙‑2‑亚基)环己‑1,4‑二烯衍生物及其制备方法、应用和器件，3,6‑二(丙‑2‑亚基)环己‑1,4‑二烯衍生物的结构式中，R 1 ‑R 8 分别单独的选自卤素、碳原子数为1‑60的烷基、取代或无取代的芳香杂环基、以及取代或无取代的芳香环基中的任意一种基团。本发明通过对该3,6‑二(丙‑2‑亚基)环己‑1,4‑二烯衍生物键连的化学结构等进行改进，将该衍生物作为传输层材料或阻挡层材料应用于有机电致发光器件中，能够有效的提高注入空穴的能力，并降低启动电压。

2-Pyridinones and their use as cardiotonic agents

3,4-Dihydro-3-R 1 -4-R 2 -5-Q-6-R-2(1H)-pyridinones (I), where R 1 and R 2 are each hydrogen or methyl, R is lower-alkyl, and Q is 4(or 3)-hydroxyphenyl, 4(or 3)-methoxyphenyl, 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two lower-alkyl substituents, or acid-addition salts thereof, and their preparation are shown. Also shown is the cardiotonic use of I where Q is 4(or 3)-hydroxyphenyl, 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two lower-alkyl substituents.

2(1H)-pyridinones and preparation, useful as cardiotonics

3,4-Dihydro-3-R 1 -4-R 2 -5-Q-6-R-2 (1H)-pyridinones (I), where R 1 and R 2 are each hydrogen or methyl, R is lower-alkyl, and Q is 4 (or 3)-hydroxyphenyl, 4 (or 3)-methoxyphenyl, 4 (or 3)-pyridinyl or 4 (or 3)-pyridinyl having one or two lower-alkyl substituents, or acid-addition salts thereof, as well as the corresponding 3-R 1 -4-R 2 -5-Q-6-R-2 (1H)-pyridinones where at least one of R 1 and R 2 is methyl. The compounds have cardiotonic use when Q is 4 (or 3)-hydroxyphenyl, 4 (or 3)-pyridinyl or 4 (or 3)-pyridinyl having one or two lower-alkyl substituents. Said compounds are prepared from butanenitriles, butanoates, acrylamides or mixtures of alkanones and acetoacetamide, with optional conversion of the 3,4-dihydro compounds obtained to the 3,4-unsaturated compounds by heating with sulfur in an inert solvent and conversion of the methoxyphenyl compounds to the hydroxyphenyl compounds.

Methods of producing sulfilimine compounds

술필이민 화합물, 예컨대 N -시아노- S -메틸- S -[1-(6-트리플루오로메틸-3-피리디닐)에틸]술필이민 또는 다른 치환 술필이민 화합물의 제조 방법. 상기 방법은 술피드 화합물, 시안아미드, 차아염소산 화합물 및 염기를 배합하고, 술피드 화합물을 산화시켜 술필이민 화합물을 형성하는 것을 포함한다. 술피드 화합물은 2-트리플루오로메틸-5-(1-치환)알킬-티오피리딘 화합물을 포함할 수 있다. 염기는 수산화나트륨을 포함할 수 있다. 완충액, 예컨대 포스페이트 완충액이 선택적으로 반응에서 사용될 수 있다. Processes for preparing sulfilimine compounds such as N -cyano- S -methyl- S- [1- (6-trifluoromethyl-3-pyridinyl) ethyl] sulfilimin or other substituted sulfimiline compounds. The method includes combining a sulfide compound, a cyanamide, a hypochlorous acid compound and a base, and oxidizing the sulfide compound to form a sulfilimine compound. The sulfide compound may comprise a 2-trifluoromethyl-5- (1-substituted) alkyl-thiopyridine compound. The base may comprise sodium hydroxide. Buffers such as phosphate buffers can optionally be used in the reaction.

Liquid crystal medium with a nematic phase, useful in electro optical display, comprises a pyran-containing component

Liquid crystal medium (Q) with a nematic phase comprises a component (A) containing a pyran compound (I). Liquid crystal medium (Q) with a nematic phase comprises a component (A) containing a pyran compound of formula (I). R 1>1-7C, preferably 1-5C -alkyl or -alkoxy, alkenyl-, alkenyloxy-, alkynyl- or alkynyloxy with 2-7C (where CH 2 groups are optionally substituted by O, CO, S or halo) or H; Z 1>CH 2-CH 2, CH 2-O, CF 2-O, COO, OCO or a bond; X 1>halo, fluorinated alkyl, fluorinated 1-5C-alkoxy or fluorinated alkenyl, alkenyloxy or 2-4C oxaalkyl; and Y 1> 1>, Y 1> 2>H or F. Where the two oxygen atoms are not bonded directly with each other. An independent claim is included for an electro optical display comprising (Q). [Image].

Process for removing metals from hydrocarbons

Method of producing the derivatives of piperidinedion-2,6 or salts thereof

Изобретение касаетс  производных пиперидина, в частности получени  пиперидиндиона-2,6 или их солей общей формулы: KM-i-C (,0) -NR/-C (О) -CHR, j, где К 2-пиперидил, М CH -CH2N(L)2; L CH(CH,).j ; R, , R,j и R, Н или R Н или С(-С -алкил или (Rj + RA) - (CHj) , которые обладают антиаритмическим действием и могут быть использованы в медицине. Цель - создание новых активных веществ указанного класса. Их синтез ведут из 2-пиридилацетонитрила и 1- -хлор-2-диизопропиламиноэтана в присутствии бензилтриэтиламмоний-хлори- да и 50%-ного водного NaOH при 10-35 С с последующей обработкой полученного продукта нитрилом RR,C , где указано выше, в присутствии бензилтриметиламмоний- гидроксида при О-30°С. Далее полученный динитрил нагревают до 100-150 С в присутствии кислоты (НС1) с последующими , при необходимости,, алкилиро- ванием по азоту и вьщелением целевого продукта в свободном виде или в виде соли. Новые вещества оказывают антиаритмическое действие на желудочковую тахикардию в течение 1,5-4 ч. 1 табл. ОТ со со К 00 сы The invention relates to piperidine derivatives, in particular the preparation of piperidinedione-2,6 or their salts of the general formula: KM-iC (, 0) -NR / -C (O) -CHR, j, where K 2-piperidyl, M CH-CH2N ( L) 2; L CH (CH,). J; R, R, j and R, H or R H or C (-C-alkyl or (Rj + RA) - (CHj), which have an antiarrhythmic effect and can be used in medicine. The goal is to create new active substances of the specified class Their synthesis is carried out from 2-pyridylacetonitrile and 1-chloro-2-diisopropylaminoethane in the presence of benzyltriethylammonium chloride and 50% aqueous NaOH at 10-35 ° C, followed by treatment of the resulting product with nitrile RR, C, as indicated above, in the presence of benzyltrimethylammonium hydroxide at O-30 ° C. Next, the resulting dinitrile is heated to 100-150 ° C in the presence of and acids (HC1) followed by, if necessary, alkylation on nitrogen and the release of the target product in free form or in the form of ...

It is stored and the application in reading based on monomolecular multiple controllable light reaction and its in information

本发明公开了一种氰基苯乙烯化合物，其结构如下式(I)所示，其中X为阴离子，Y为烷基、烷氧基、芳基或其他功能性官能团。它能够通过调节聚集形貌的不同或者使用不同的激发光来得到多重可控的光反应，也可以通过用具有不同空腔大小的环化合物来控制光二聚的速度，并且能用水凝胶的固液两相催化反应实现无需提纯地大量制备光二聚产物。

Method of producing 2-benzoyl-3-aminopyridine or salts thereof

Process for preparation of sulfamide derivatives

NOVEL DERIVATIVES OF PYRIDYLACETONITRILES, THEIR PREPARATION AND THEIR USE AS ANTIFUNGAL IN THE AGRICULTURAL FIELD

NOUVEAUX DERIVES DE PYRIDYLACETONITRILE REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) AVEC:R : H, ALKYLE INFERIEUR, PHENYLE, ARALKYLE EVENTUELLEMENT SUBSTITUES,R : H, ALKYLE INFERIEUR, EVENTUELLEMENT SUBSTITUE,R : PYRIDYL-3 EVENTUELLEMENT SUBSTITUE,AR : PHENYLE EVENTUELLEMENT SUBSTITUE. ILS SONT UTILISABLES EN AGRICULTURE POUR LA LUTTE CONTRE LES CHAMPIGNONS PHYTOPATHOGENES. NEW DERIVATIVES OF PYRIDYLACETONITRILE RESPONDING TO THE FORMULA: (CF DRAWING IN BOPI) WITH: R: H, LOWER ALKYL, PHENYL, ARALKYL POSSIBLY SUBSTITUTED, R: H, LOWER ALKYL, POSSIBLY R-SUBSTITUTED: SUBSTITUTED 3: SUBSTITUTED: 3 POSSIBLE SUBSTITUTE PHENYL. THEY CAN BE USED IN AGRICULTURE FOR THE FIGHT AGAINST PHYTOPATHOGENOUS FUNGI.

PYRIDINE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Patent FR2535721B1

Patent FR2444026B1

4,5-DIHYDRO-6- (PYRIDINYL) -3 (2H) -PYRIDAZINONES, THEIR PREPARATION AND THEIR USE AS CARDIOTONIC AGENTS

L'INVENTION CONCERNE DES 2-R-4,5-DIHYDRO-4-R-6-PY-3(2H)-PYRIDAZINONES DE FORMULE (CF DESSIN DANS BOPI) OU UN DE LEURS SELS, OU R EST UN GROUPEMENT ALKYLE OU HYDROXYALKYLE INFERIEUR, R EST UN ATOME D'HYDROGENE OU UN GROUPEMENT METHYLE ET OU R PEUT EGALEMENT ETRE UN ATOME D'HYDROGENE QUAND R EST UN GROUPEMENT METHYLE; ET PY EST UN GROUPEMENT 4- OU 3-PYRIDINYLE EVENTUELLEMENT SUBSTITUE. ON PREPARE CES COMPOSES PAR REACTION DU 4-OXO-4-PY-2-R-BUTANENITRILE AVEC UN SEL DE N-R-HYDRAZINE OU PAR REACTION D'UN 4-OXO-4-PY-2-R-BUTONOATE OU D'UN 4-(BN)-4-CYANO-4-PY-2-R-BUTANOATE D'ALKYLE INFERIEUR AVEC UNE N-R-HYDRAZINE, BN ETANT LE RESTE D'UNE AMINE CYCLIQUE BN-H. CES COMPOSES AINSI OBTENUS SONT UTILES COMME AGENTS CARDIOTONIQUES. THE INVENTION RELATES TO 2-R-4,5-DIHYDRO-4-R-6-PY-3 (2H) -PYRIDAZINONES OF FORMULA (CF DRAWING IN BOPI) OR ONE OF THEIR SALTS, OR R IS AN ALKYL GROUP OR LOWER HYDROXYALKYL, R IS A HYDROGEN ATOM OR A METHYL GROUP AND OR R MAY ALSO BE A HYDROGEN ATOM WHEN R IS A METHYL GROUP; AND PY IS A POSSIBLY SUBSTITUTE 4- OR 3-PYRIDINYL GROUP. THESE COMPOUNDS ARE PREPARED BY REACTION OF 4-OXO-4-PY-2-R-BUTANENITRILE WITH NR-HYDRAZINE SALT OR BY REACTION OF 4-OXO-4-PY-2-R-BUTONOATE OR A LOWER ALKYL 4- (BN) -4-CYANO-4-PY-2-R-BUTANOATE WITH NR-HYDRAZINE, BN BEING THE REMAINDER OF CYCLIC AMINE BN-H. THESE COMPOUNDS SO OBTAINED ARE USEFUL AS CARDIOTONIC AGENTS.

New amino-pyrazole which can be used in therapy, in particular as a drug for the treatment of inflammatory conditions.

Patent FR2467200B1

2,5-DISUBSTITUTED PYRIDINES, PROCESS FOR THE PREPARATION THEREOF, LIQUID CRYSTALLINE MATERIAL, AND ELECTRO-OPTICAL DEVICE

LES PYRIDINES DISUBSTITUEES EN 2,5 DE L'INVENTION ONT POUR FORMULE: (CF DESSIN DANS BOPI) R ETANT CH2N1 OU CH2N1O, N 4-8. LEUR PROCEDE DE PREPARATION CONSISTE A FAIRE REAGIR UN SEL DE PYRYLIUM DE FORMULE: (CF DESSIN DANS BOPI) R AYANT LES SIGNIFICATIONS CI-DESSUS, SUR L'ACETATE D'AMMONIUM AU SEIN D'UN MILIEU ORGANIQUE. LE MATERIAU CRISTALLIN LIQUIDE CONTIENT AU MOINS UNE DES PYRIDINES DISUBSTITUEES EN 2,5 PRECITEES ETOU UN COMPOSE DE FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE R CH2N1, N ETANT EGAL A 1-9. CE MATERIAU PEUT CONTENIR UN DIELECTRIQUE ORGANIQUE ET UN COLORANT DICHROIQUE. IL ENTRE, A TITRE DE CORPS DE SERVICE 1, DANS UN DISPOSITIF ELECTRO-OPTIQUE DESTINE A AFFICHER ET A TRANSFORMER LES INFORMATIONS. THE 2.5-DISUBSTITLED PYRIDINES OF THE INVENTION HAVE THE FORMULA: (CF DRAWING IN BOPI) R BEING CH2N1 OR CH2N1O, N 4-8. THEIR PREPARATION PROCESS CONSISTS OF REACTING A PYRYLIUM SALT OF FORMULA: (CF DRAWING IN BOPI) WITH THE ABOVE MEANINGS, ON AMMONIUM ACETATE IN AN ORGANIC MEDIUM. THE LIQUID CRYSTALLINE MATERIAL CONTAINS AT LEAST ONE OF THE ABOVE 2.5 DISUBSTITUTED PYRIDINS AND OR A COMPOUND OF THE FORMULA: (CF DRAWING IN BOPI) IN WHICH R CH2N1, EQUAL TO 1-9. THIS MATERIAL MAY CONTAIN ORGANIC DIELECTRIC AND DICHROIC COLOR. IT ENTERS, AS A SERVICE BODY 1, IN AN ELECTRO-OPTICAL DEVICE INTENDED TO DISPLAY AND TRANSFORM INFORMATION.

Patent FR2184077A1

PYRIDINE DERIVATIVES

2-PHENYLPYRIDINE AND LIQUID CRYSTAL COMPOSITIONS CONTAINING THEM

PHENYLPYRIDINES. ELLES REPONDENT A LA FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE Y EST R-, Z PHENYLPYRIDINES. THEY MEET THE FORMULA: (CF DRAWING IN BOPI) IN WHICH IS R-, Z

MYOCARDIAL PROTECTIVE G-BUTYROLACTONE DERIVATIVES WITH ANTIARRHYTHMIC ACTIVITY, PROCESS FOR THEIR PREPARATION AND MEDICAMENTS CONTAINING THEM

LA PRESENTE INVENTION CONCERNE : -LES PRODUITS DE FORMULE GENERALE (CF DESSIN DANS BOPI) DANS LAQUELLE : R REPRESENTE UN GROUPE ALKYLE DROIT THE PRESENT INVENTION CONCERNS: -PRODUCTS OF GENERAL FORMULA (CF DESIGN IN BOPI) IN WHICH: R REPRESENTS A LAW ALKYL GROUP

Process for preparing 1-(6-methylpyridin-3yl)-2-[(4-methylsulfonyl)phenyl]ethanone

1-(6-Methylpyridin-3-yl)-2-[(4-(methylsulfonyl)phenyl]ethanone of the formula (see formula I) and a process for preparing such is disclosed. 1-(6-Methylpyridin-3- yl)-2-[(4-(methylsulfonyl)phenyl]ethanone is an important intermediate for preparing so-called COX-2 inhibitors, which are pharmaceutically active compounds having analgesic and anti-inflammatory action .

PYRIDINE DERIVATIVES

DERIVES DE LA PYRIDINE REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE A REPRESENTE UN GROUPE ALKYLENE EVENTUELLEMENT SUBSTITUE, SITUE EN POSITION 3 OU EN POSITION 4 DU NOYAU PYRIDINE, E DESIGNE UN GROUPE REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) (DANS LAQUELLE R REPRESENTE UN ATOME D'HYDROGENE OU UN GROUPE ALKYLE), B-Z-D REPRESENTE UNE SIMPLE LIAISON, R REPRESENTE UN GROUPE -COOR OU -COSR (OU R REPRESENTE UN ATOME D'HYDROGENE, UN GROUPE ALKYLE, UN GROUPE ARALKYLE, UN GROUPE CYCLOALKYLE EVENTUELLEMENT SUBSTITUE, UN GROUPE PHENYLE EVENTUELLEMENT SUBSTITUE, UN GROUPE TRIFLUOROMETHYLE, UN GROUPE ALKYLE OU ALCOXY OU ALKYLTHIO, UN GROUPE NITRO OU PHENYLE), R REPRESENTE UN ATOME D'HYDROGENE, OU UN GROUPE ALKYLE ET SES SELS D'ADDITION AUX ACIDES NON TOXIQUES, ET, LORSQUE R REPRESENTE UN GROUPE CARBOXY OU THIOCARBOXY, SES SELS NON TOXIQUES. APPLICATION POUR LE TRAITEMENT DE L'INFLAMMATION, DE L'HYPERTENSION, ET DE L'APOPLEXIE CEREBRALE. DERIVATIVES OF PYRIDINE RESPONDING TO THE FORMULA: (CF DRAWING IN BOPI) IN WHICH AN ALKYLENE GROUP REPRESENTS POSSIBLY SUBSTITUTED, LOCATED IN POSITION 3 OR IN POSITION 4 OF THE PYRIDINE CORE, E DESIGNATES A GROUP RESPONDING TO THE FORMULA: (CF BOPI) (IN WHICH R REPRESENTS A HYDROGEN ATOM OR AN ALKYL GROUP), BZD REPRESENTS A SINGLE BOND, R REPRESENTS A -COOR OR -COSR GROUP (OR R REPRESES A HYDROGEN ATOM, AN ALKYL ARKYL GROUP, A GROUP , A POSSIBLY SUBSTITUTES CYCLOALKYL GROUP, A POSSIBLY SUBSTITUTES PHENYL GROUP, A TRIFLUOROMETHYL GROUP, AN ALKYL OR ALCOXY OR ALKYLTHIO GROUP, A NITRO OR PHENYL GROUP, AND SGENE REPRESENT A UNDENYL TO NON-TOXIC ACIDS, AND, WHEN R REPRESENTS A CARBOXY OR THIOCARBOXY GROUP, ITS NON-TOXIC SALTS. APPLICATION FOR THE TREATMENT OF INFLAMMATION, HYPERTENSION, AND CEREBRAL APOPLEXY.

Method of producing the derivatives of the 2.6-piperidinedion

Изобретение касаетс  производных 2,6-пиперидона, в частности соединений общей формулы (I)t KMC-C(0)-NH-C(0)-CR,K -СН, где К - (CH)-N(R,)2 ; М - 2 (или 3 или 4)- пиперидил; R , - - алкил M:IH N(R,)j - морфолино-, пиперидино-груп- па, не- или замещенна  С,-С4 - алки- лом; п 2 или 3; R,,; Rj - СН., или (R 4 Rj) - (CHj)-, которые могут -образовывать соли с минераль(ыми или органическими кислотами и ггро в- л ют антиаритмическое действие. Цель- создание веществ указаннот о класса с новым видом активности. Их синтез ведут из пиридилацетонитрила и соответствующего эфирокетона при кипении с последующим восстановлением в присутствии Pd/C при комнатной температуре и дальнейщей обработкой хлористым алкиламином при комнатной температуре . Затем ведут циклизацию в кислой среде при 100-110 С с выделением целевых веществ. Последние не  вл ютс  токсичными веществами и про вл ют лучшее по длительности антиаритмическое действие, чем известные. 2 табл. ш О)

PYRIDINE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Dérivés de la pyridine répondant à la formule : Pyridine derivatives corresponding to the formula:

Insecticidal composition comprising N-substituted (6-haloalkylpyridin-3-YL)alkyl sulfoximines

A composition comprising a compound being N -Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines which are effective at controlling insects.

Method of preparing 1-(6-methylpyridine-3-yl)-2- 4-(methylsulfonyl)phenyl ethanone

Insecticidal composition comprising N-substituted (6-haloalkylpyridin-3-yl) alkyl sulfoximins

Una composición que comprende un compuesto de la fórmula (I) en la que X representa NO2, CN o COOR4; L representa un enlace sencillo o R1, S y L tomados juntos representan un anillo de 4-, 5- ó 6-miembros; R1 representa alquilo C1-C4; R2 y R3 representan independientemente hidrógeno, alquilo C1-C4, flúor, cloro o bromo; n es un número entero de 0-3; Y representa haloalquilo C1-C4; y R4 representa alquilo C1-C3, en el que el término alquilo incluye grupos de cadena lineal, cadena ramificada ycíclicos; y uno o más otros insecticidas o fungicidas o herbicidas.