ПРОИЗВОДНЫЕ БЕНЗАМИДОВ И ГЕТЕРОАРЕНОВ

Настоящее изобретение относится к новым соединениям формулы I: ! , ! а также к их фармацевтически приемлемым солям, обладающим ингибирующей активностью в отношении белка-переносчика холестерилового эфира (БПХЭ), к способу их получения, фармацевтической композиции на их основе и к их применению для приготовления лекарственных средств. Значения заместителей R1, R2, R4, R5, а также А, В, D и n указаны в формуле изобретения. 4 н. и 10 з.п. ф-лы.

НОВЫЙ СПОСОБ СИНТЕЗА 7-МЕТОКСИ-НАФТАЛИН-1-КАРБАЛЬДЕГИДА И ЕГО ПРИМЕНЕНИЕ В СИНТЕЗЕ АГОМЕЛАТИНА

Настоящее изобретение относится к способу синтеза соединения формулы (I) – промежуточного соединения для получения агомелатина, обладающего ценными фармакологическими свойствами. Способ заключается в том, что 7-метокси-нафталин-2-ол формулы (III) взаимодействует с этилортоформиатом в присутствии анилина с последующим гидролизом полученного промежуточного иминового соединения с получением соединения формулы (IV), затем соединение формулы (IV) подвергают реакции сульфонилирования, чтобы получить соединение формулы (V), где R означает -СН3 или толильную группу, и полученное соединение формулы (V) подвергают реакции дезоксигенирования в присутствии переходного металла и восстановителя, чтобы получить соединение формулы (I), которое выделяют в форме твердого вещества. Предлагаемый способ позволяет получить целевой продукт в соответствии с требованиями воспроизводимости, без использования трудоемкой очистки. Также настоящее изобретение относится к способу синтеза агомелатина, к соединению формулы ...

Способ получения 2-/4-(4-хлор-бЕНзОилАМиНОэТил)-фЕНОКСи/-2-МЕТил--пРОпиОНОВОй КиСлОТы

AROMATISCHE VERBINDUNGEN, DIESE ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN UND IHRE THERAPEUTISCHE ANWENDUNG

Verwendung von Phenolen und Phenolderivaten als Arzneimittel mit fibrinogensenkender Wirkung

NAPHTHOYLAMINO ALKYL PHENOXY-ALKYL-CARBOXYLIC ACID DERIVATIVES

... 1449586 41-(Naphthoylaminoalkyl)-phenoxyacetic acids and esters BOEHRINGER MANNHEIM GmbH 3 Feb 1975 [6 Feb 1974] 4483/75 Heading C2C Novel compounds I in which R 1 and R 2 are H or C 1-3 alkyl, Z is OH or C 1-3 alkyl and n is 1 or 2 and their salts when Z is OH are prepared by reacting 4-(aminomethyl or -ethyl)-phenol (II) or a reactive derivative thereof simultaneously or successively with 1- or 2-naphthoic acid (III) or a derivative thereof and a compound (IV) X-CR 1 R 2 -COZ in which X is a radical derived from an anion of a hydrohalic or sulphonic acid and, when the aminophenol is reacted successively with the other two components, the amino or hydroxy group of compound (II) is blocked by a protecting group which is removed after the first stage to allow the second stage to be carried out. Compounds I (R 1 , R 2 =C 1-3 alkyl) are also prepared by using a mixture of R 1 COR 2 , CCl 3 and an alkali metal hydroxide in place of compound (IV). The free acids are also obtained by ...

Entry inhibitors of the HIV virus.

Benzamides

“New derivatives with naphthalenic structure, their method of preparation and the compositions pharmaceutical which contain them”.

Benzamides

Entry inhibitors of the HIV virus.

Benzamides

Entry inhibitors of the HIV virus.

AMIN-1,2 AND -1,3-DIOLVERBINDUNGEN AND THEIR USE FOR THE TREATMENT OF ALZHEIMER ILLNESS

PROCEDURE FOR THE PRODUCTION OF NEW ANILIDE

VERFAHREN ZUR HERSTELLUNG NEUER ALFA-SUBSTITUIERTER BENZHYDROL-DERIVATE

VERFAHREN ZUM HERSTELLEN VON NEUEN BENZIMIDAZOLDERIVATEN UND VON ESTERN UND SALZEN HIEVON

VERRAHREN FOR MANUFACTURING NEW PHENYLAETHYLAMINDERIVATE

PROCEDURE FOR MANUFACTURING NEW BENZIMIDAZOLDERIVATEN AND ESTERS AND SALTS HIEVON

AROMATIC CONNECTIONS THESE CONTAINING PHARMACEUTICAL COMPOSITIONS AND YOUR THERAPEUTIC USE

VERFAHREN ZUR HERSTELLUNG VON NEUEN PHENOXYALKYLCARBONSAUREN UND VON DEREN ESTERN

N-PHENYLALKYLBENZAMIDE ONE WITH FUNGICIDAL EFFECT.

NAPHTHALIN DERIVATIVES, PROCEDURES FOR YOUR PRODUCTION AND IT ABSTENTION PHARMACEUTICAL COMPOSITIONS.

PROCEDURE FOR THE PRODUCTION NEW-RAL-FABENZHYDROL

BENZAMIDINDERIVATE AS ANTAGONISTS OF OREXINREZEPTOREN

Procedure for the production of new 4-Benzamidoalkylphenoxyalkansäuren and its alkyl star or salts

SUBSTITUTED DIMERE CONNECTIONS PROCEDURES FOR THEIR PRODUCTION AND THEIR PHARMACEUTICAL COMPOSITIONS

DISUBSTITUIERTE BIPHENYLOXAZOLINE

BENZOZYKLOALKENVERBINDUNGEN, THEIR PRODUCTION AND USE

NEW HEMMERN OF ADVANCED GLYKOSILIERUNG FINAL PRODUCTS

Compounds for use in the treatment or prophylaxis of pain, inflammation and/or autoimmunity

The present invention relates to a polymorphic form of (S,S)-2-N(3-O-(propan-2-ol)-1-propyl- 4-hydroxybenzene)-3-phenylpropylamide or synonymously named N-[2-(4-Hydroxy-phenyl)- -(2-hydroxy-propoxymethyl)-ethyl]-3-phenyl-propionamide and to the treatment or prophylaxis of pain, inflammation and/or autoimmunity and provides a method of treating or preventing pain, inflammation and/or autoimmunity as well as the use of this polymorphic form in the manufacture of medicaments for the treatment or prophylaxis of pain (preferably nociceptive or neuropathic), inflammation and/or autoimmunity in humans and/or non-human animals.

Benzamides

The present application relates to compounds of formula (I), wherein R1 to R5 are as defined in claim 1, a pharmaceutical composition thereof and said compounds for use in the treatment of diseases related with the activity of P2X7 receptor.

Substitued biphenyloxazolines

Substituted cyclohexane derivates and the use thereof in medicaments for treating cardiovascular diseases

Substitued biphenyloxazolines

HETEROCYCLIC AMINO-ALCOHOL DERIVATIVES AND THEIR PREPARATION

Amino-alcohol derivative having the formula : (I) wherein :(a) R1 represents hydrogen, one or two linear or ramified alkyl radicals (C1-C3), a phenyl radical or a carboxy radical;(b) R2 is a linear or ramified alkyl radical (C1-C3);(c) R3 is : - a mono or polyunsaturated alkenyl radical (C3-C18);- a mono or polylunsaturated alkenyl radical (C3-C12) substituted by oxygen, sulfur or a phenyl radical;- a mono or polyunsaturated alkynyl radical (C3-C18);- a mono or polyunsaturated alkynyl radical (C3-C12) substituted by oxygen, sulfur or a phenyl radical;- a cycloalkyl radical (C3-C10);- a linear or ramified alkyl radical (C2-C10);- a linear or ramified alkyl radical (C2-C18), substituted by at least an atom and/or radical selected from the group comprising:(1) oxygen or sulfur ,(2) alkoxycarbonyl radicals (C1-C3), pyrrolidine, pyrroli dinone or imidazolidone,(3) phenyl, phenoxy, phenylthio, benzoyl, indanyloxy, naphthyloxy radicals,(4) phenyl, phenoxy, phenylthio, benzoyl radicals substituted ...

ACYL ANILINES EXERTING A FUNGICIDAL ACTION

Acyl anilines are disclosed having the formula (I) wherein R = H; CH3; C2H5; n.C3H7 -CH2-CH=CH2; or - CH=CH-CH3; R1=CH3; C2H5; n.C3H7; -CH2-CH=CH2; or -CH=CH-CH3; R3= H or C1-C3 alkyl and R4 = H; or R3 and R4 together are -CH2-; X =. wherein R9=C1-C3 alkyl; or .-CH-(OR5)2 wherein R5 = C1-C3 alkyl; Z =.-CH2 -Y wherein Y = . phenyl which may be substituted with C1-C3 alkoxy; . cyclohexyl; . furyl; or . thienyl . wherein R8 = CH3; C1-C3 alkoxy or halomethyl; or .a phenyl radical which may be substituted with C1-C3 alkyl, C1-C3 alkoxy and halogen. The compounds of formula I are endowed with a high fungicidal activity and with a low phytotoxicity.

ORGANIC COMPOUNDS

Compounds of the formula (I) provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the present invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases (IBDs), ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.

NOVEL ANTICANCER COMPOUNDS

The present invention relates to compounds of formula (I): (I) their pharmacologically acceptable salts, or solvates and hydrates, and their prodrugs, respectively, and to pharmaceutical compositions containing the same as active ingredient. These novel compounds are especially useful in the treatment of cancer.

ISOLATED STEREOISOMERIC FORMS OF (S)2-N(3-O-(PROPAN 2-OL)-1-PROPYL-4-HYDROXYBENZENE)-3-PHENYLPROPYLAMIDE

Isolated stereoisomeric forms of the compound (S)2-N(3-O-(propan 2-ol)-1-propyl-4-hydroxybenzene)-3-phenylpropylamide and uses in the treatment of pain. The invention discloses a compound of formula II (see formula II) having the specific stereochemistry of (S)2-N(3-O-((S)propan 2-ol)-1-propyl-4-hydroxybenzene)-3-phenylpropylamide or a pharmaceutically acceptable salt or hydrate thereof, wherein the compound comprises at least 90% of (S)2-N(3-O-((S)propan 2-ol)-1-propyl-4-hydroxybenzene)-3-phenylpropylamide and less than 10% of other stereoisomeric forms of the compound.

Process for the preparation of heterocyclic aminoalcohol derivatives

Process for the preparation of heterocyclic aminoalcohol derivatives

Aminoalcohol derivatives corresponding to the formula (I) in which the substituents have the meaning shown in Claim 1 are prepared by reduction of a corresponding alpha -aminoketone to the aminoalcohol of formula I. Preferably, a starting alpha -aminoketone is used in situ which is obtained by reaction of an alpha -haloketone with an amine R3R4NH. The alcohol can then be esterified by reaction with an acid or an anhydride. The compounds obtained have activities on the cardiovascular system, for example antihypertensive and/or antispasmodic activities, peripheral vasodilative activity, protective activity against myocardial anoxia, hypolipidemiating activity, antithrombotic activity, beta -lytic activity or platelet aggregation inhibiting activity, and/or activities on the central nervous system, for example a tranquillising activity.

PROCEDURE FOR THE PRODUCTION OF NEW, ALPHA-SUBSTITUTED BENZHYDROLDERIVATE.

Process for the preparation of novel alpha-ethylbenzhydrol derivatives

Novel, alpha -substituted benzhydrol derivatives are prepared. The compounds have the following formula in which the substituents are defined in Claim 1. These compounds are obtained by reacting an appropriate propiophenone with a phenylmagnesium halide. The said compounds are pharmaceutically active and they have an inhibitory or inductive effect on the microsomal enzyme system of the liver which metabolises exogenous substances.

PROCEDURE FOR the PRODUCTION OF 2 (4 (4-CHLORBENZOYLAMINO-AETHYL) - PHENOXY) - 2-METHYLPROPIONSAEURE.

PHENYLETHYLAMINE DERIVATIVES AND THEIR PREPARATION AS WELL AS COMPOSITION CONTAINING THE SAME.

BENZIMIDAZOLE DERIVATIVES, THEIR PREPARATION AS WELL AS COMPOSITION CONTAINING THE SAME.

ACILANILINE TO ACTION FUNGICIDE.

HETEROCYCLIC THE INHIBITORS

BENZAMIDE AND HETEROARENE DERIVATIVES

METHOD FOR AGOMELATINE SYNTHESIS, CRYSTALLINE FORM OF AGOMELATINE, AND PHARMACEUTICAL COMPOSITION

БЕНЗАМИДЫ

Изобретение относится к соединениям формулы I, где R1-R5 такие, как определено в п.1, их фармацевтической композиции и указанным соединениям для применения в лечении болезней, обусловленных активностью рецептора Р2Х7 Формула I ...

ANTAGONISTS CXCR3

БЕНЗАМИДЫ

Изобретение относится к новым бензамидным соединениям, формулы (I), (I) содержащим их фармацевтическим композициям и для применения в лечении заболеваний, обусловленных активностью рецептора P2X7. Пункты: 3 независ. 17 завис.

Novel decamethyl zirconocene coordination compound as well as preparation method and application thereof

DERIVED FROM PHENYLETHYLAMINE, THEIR PREPARATION AND USE IN THE TREATMENT OF THE CARDIOVASCULAR AFFECTIONS, AND COMPOSITIONS THE CONTAINER

FUNGICIDAL APPLICATION OF DERIVED BENZAMIDIQUES

ALPHA-SUBSTITUTED BENZHYDROL DERIVATIVES AND A PROCESS FOR THE PREPARATION THEREOF

BENZIMIDAZOLE DERIVATIVES, THEIR PREPARATION AND USE IN THE TREATMENT OF CARDIOVASCULAR CONDITIONS AND COMPOSITIONS CONTAINING THEM

NEW DERIVATIVES DIMERIQUES SUBSTITUTE, THEIR METHOD OF PREPARATION AND THE COMPOSITIONS PHARMACEUTICAL WHICH CONTAIN THEM

L'invention concerne les composés de formule (I). A-G1-Cy-G2-Cy-G3-B dans laquelle : - A, B, représentent un groupement NR1C (Q) R2 , C (Q) NR1R2 ou NR1C (Q) NR2R3, - G1 , G3 représentent une chaîne alkylène éventuellement substituée, - Cy représente une structure cyclique - G2 représente une chaîne Médicaments.

NEW ACYL ANILINES AND THEIR FUNGICIDAL APPLICATION

DUAL MODULATORS OF FARNESOID X RECEPTOR AND SOLUBLE EPOXIDE HYDROLASE

PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR MODULATORS

The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.

Catalyst and method for amide formation

The invention is a catalyst, the use of the catalyst and a method of using the catalyst in the formation of a compound with an amide bond. The catalyst is an HOBT derivative having the following formula (1): where R1 is a group bearing a positive charge at pH 5-7; where Y is a bond or a substituted or unsubstituted alkylene chain containing 1-10 carbon atoms and 0-2 heteroatoms selected from the group consisting of N, S and O; and where X is a linker group selected from -CO- or -SO2-. In the method, an amine, a carboxylic acid, an amide coupling agent and a catalyst of formula (1) are reacted for a time sufficient to produce an amide bond between the amine and the carboxylic acid. Thereafter, the compound containing the amide bond is isolated.

Use of aryl and hetaryl carboxamides as endoparasiticides

The present application relates to known and novel aryl- and hetarylcarboxamides of the formula (I) and to their use as medicaments for controlling endoparasites in animals or humans, and also to parasiticidal compositions, in particular endoparasites, comprising aryl- and hetarylcyclylcarboxamides.

PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR MODULATORS

BENZYLOXYPROPYLAMINE DERIVATIVE

Using allosteric hemoglobin modifiers to decrease oxygen affinity in blood

A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.

NEW 3,5-DI-TERT.BUTYL-4-HYDROXYPHENYL DERIVATIVES, METHODS OF PREPARING THEM AND DRUGS CONTAINING THEM

Described are compounds of formula (I), in which A is a valency bond or a straight or branched alkyl chain with 1 to 5 C-atoms; X is an -NR-CO (amide) or -NR-CO-NR- (urea) group in which R is a hydrogen atom or a C1-C4 alkyl group; and Y is a straight or branched, saturated or unsaturated hydrocarbon chain with 1 to 6 C-atoms (which may be substituted by an aryl, hetero-aryl, aryloxy or arylthio group), a C3-C6 cycloalkyl group or an aryl group, whereby the aryl or hetero-aryl group may be substituted in any possible positions on the ring with one to three CN, hydroxymethyl, methylenedioxy, halogen, trifluoromethyl, C1-C4 alkyl, amino, C1-C4 acylamino, di-(C1-C4)-alkylamino, hydroxy, C1-C4 alkoxy, carboxy, oxyacetic acid ethyl ester or nitro groups, with the provision that Y may only be an unsubstituted phenyl group when A is anything other than -CH2- or -CH2-CH2, as well as the pharmacologically acceptable salts of such compounds. The invention also concerns methods of preparing such compounds ...

Amide compounds, process for preparing the same, and composition for activating gastric motor function containing the same

AROMATIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE IN THERAPY

АКТИВАТОР ALDH2

Способ получения амидов ароматических кислот

Сущность изобретения: продукт-амиды ароматических кислот формулы 2R2- 4Рз+5Р 1+СбН2-М-СбН4-4Я1, где Rt - галоген, ORs, R2-H, низший алкил, RS и R4 вместе алкилен Сз-Cs с неразветвленной цепью, Rs-H, ацетил, морфолино-низш.алкил, М- CONH, NHCO. Реагент 1: 2R2-4R3-5R4- СеН2А. Реагент 2: 4RiCeH4B,. где А - карбоксил или реакционноспособное его производное и В-аминогруппа или А-ами- ногруппа и В-карбоксил или реакционноспособное его производное. 4 з.п. ф-лы.

Способ получения производных феноксиалкилкарбоновых кислот или их солей

Phenylamide - Verfahren zu ihrer Herstellung sowie diese Verbindungen enthaltende Arzneimittel.

Verfahren zur Synthese von Carboxamiden.

SUBSTITUIERTE PHENYLPROPIONSÄUREDERIVATE ALS AGONISTEN DES MENSCHLICHEN PEROXISOM-PROLIFERATOR-AKTIVERTEN REZEPTORS ALPHA(PPAR)

PHENOXYPROPANOLAMINES

[[-benzaminoethylphenoxycyclohexylacetic acid derivatives compound

Benzaminoethylphenoxycyclohexylacetic acid derivatives having the formula wherein R1 represents hydrogen atom, a halogen atom, hydroxyl group, a lower alkyl group or a lower alkoxy group; n is 1 or 2; and R2 represents hydrogen atom, a lower alkyl group which can have a substituent of phenyl group, a lower alkoxycarbonyl group, 3,3,5-trimethylcyclohexyloxycarbonyl group or a heterocyclic group; hexadecyl group; phenyl group which can have a substituent of a lower alkyl group, a lower alkoxy group, a lower alkoxycarbonyl group or a halogen atom; a cyclohexyl group or alpha -?4-(4-chlorobenzaminoethyl) phenoxy!- alpha -cyclohexylacetoxycyclohexyl group a antihyperlipidemic compositions thereof.

STABLE AND CRYSTALLINE FORM OF BEZAFIBRAT

TRICYCLI DERIVATIVES AND PHAMAZEUTI COMPOSITIONS IT CONTAINING

AROMATIC CONNECTIONS, THESE CONTAINING PHARMACEUTICAL COMPOSITIONS AND YOUR THERAPEUTIC APPLICATION

PROCEDURE FOR THE PRODUCTION OF 1 (PHENYL) - 1 - HYDROXY-2-AMINO-3-FLUOR-PROPAN-DERIVATEN

CARBONIC ACID DERIVATIVES AND THESE AS ACTIVE SUBSTANCE CONTAINING DRUGS

VERFAHREN ZUR HERSTELLUNG VON NEUEN AMINO- ALKOHOL-DERIVATEN

VERFAHREN ZUR HERSTELLUNG NEUER ALFA-ATHYLBENZHYDROL-DERIVATE

SUBSTITUTED PHENYLMETHYLBICYCLOCARBONSÄUREAMIDVERBINDUNGEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN ALFA-SUBSTITUIERTEN BENZHYDROL-DERIVATEN

AMIDE CONNECTIONS, PROCEDURES FOR YOUR PRODUCTION AND COMPOSITION FOR THE ACTIVATION OF GASTROMOTORI FUNCTIONS.

PHENYLAMIDE - PROCEDURES FOR YOUR PRODUCTION AS WELL AS THESE CONNECTIONS CONTAINING DRUGS.

PROCEDURE FOR THE PRODUCTION OF NEW ALFA SUBSTITUTING BENZHYDROL DERIVATIVES

BENZENE DERIVATIVES AND THEIR MEDICAL USE

CB 1/CB 2 RECEPTOR LIGANDS AND THEIR USE IN THE TREATMENT OF PAIN

1-ARYL-2-HYDROXYETHYL AMIDES AS POTASSIUM CHANNEL OPENERS

NEW ACYL ANILINES

BENZAMINOETHYL PHENOXYCYCLOHEXYL ACETIC ACID

NOVEL REAGENTS AND METHOD FOR CONJUGATING BIOLOGICAL MOLECULES

A compound of the general formula X-[Q-W—(CH═CH)—(CH)-L](I) in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing group; n represents 0 or an integer of from 1 to 4; L represents a leaving group; and m represent an integer of from 1 to 8. The compounds find use in the conjugation of biological molecules. 1. A compound of the general formula:{'br': None, 'sub': n', '2', 'm, 'X—[NH—CO—Ar—W—(CH═CH)—CH═CH]\u2003\u2003(Va)'}in which X represents a polymer; W represents a keto group; n represents 0 or an integer of from 1 to 4; m represents an integer of from 1 to 8; and Ar represents an unsubstituted or substituted aryl group.2. A compound as claimed in claim 1 , in which Ar represents a phenyl group optionally substituted by one or more of the same or different substituents selected from the group consisting of alkyl claim 1 , —CN claim 1 , —NO claim 1 , —COR claim 1 , —COH claim 1 , —CHOH claim 1 , —COR claim 1 , —OR claim 1 , —OCOR claim 1 , —OCOR claim 1 , —SR claim 1 , —SOR claim 1 , —SOR claim 1 , —NHCOR claim 1 , —NRCOR claim 1 , —NHCOR claim 1 , —NR.COR claim 1 , —NO claim 1 , —NHOH claim 1 , —NR.OH claim 1 , —C═N—NHCOR claim 1 , —C═N—NR.COR claim 1 , —NR claim 1 , —NH claim 1 , —NHR claim 1 , —NHR claim 1 , halogen claim 1 , —C≡CR claim 1 , —C═CRand —C═CHR claim 1 , in which each R independently represents a hydrogen atom or an alkyl claim 1 , aryl claim 1 , or alkyl-aryl group.3. A compound as claimed in claim 1 , in which Ar represents a phenyl group.4. A compound as claimed in claim 1 , in which X is a polyalkylene glycol claim 1 , polyvinylpyrrolidone claim 1 , polyacrylate claim 1 , polymethacrylate claim 1 , polyoxazoline claim 1 , polyvinylalcohol claim 1 , polyacrylamide claim 1 , polymethacrylamide claim 1 , HPMA copolymer claim 1 , polyester claim 1 , polyacetal claim 1 , poly(ortho ester) claim 1 , polycarbonate claim 1 , poly(imino carbonate) claim 1 , polyamide claim 1 , copolymer of divinylether-maleic ...

BENZYLAMINO-OXOETHYL BENZAMIDE ANALOGS AND METHODS OF USE

Benzylamino-oxoethyl benzamide compounds for use in treating diseases and conditions associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic β-cell dysfunction and death, for example in the treatment of Type 1 and Type 2 diabetes. The compounds can also be used in treatments for chronic heart disease, neurodegenerative diseases, retinal degeneration, and other metabolic disorders associated with ER stress. 2. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and R=H claim 1 , R=OH claim 1 , R=CF claim 1 , and n=1.3. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and R=H claim 1 , R=OH claim 1 , and R=CF claim 1 , and n=1.4. The compound of claim 1 , wherein n=1 claim 1 , R=H claim 1 , R=CF claim 1 , and Rand Rare selected from the group consisting of H and OH claim 1 , with the proviso that one of Rand R=H claim 1 , and one of Rand R=OH.5. The compound of of disposed in a pharmaceutically-acceptable carrier claim 1 , diluent or vehicle claim 1 , forming a composition.6. A conjugate claim 1 , comprising the compound of covalently linked to a targeting molecule claim 1 , wherein the targeting molecule is able to bind to a target cell or a portion of a target cell.7. The conjugate of claim 6 , wherein the targeting molecule targets a pancreatic β-cell.9. The method of claim 8 , wherein in chemical structure I: R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , and R=H claim 8 , R=OH claim 8 , R=CF claim 8 , and n=1.10. The method of claim 8 , wherein in chemical structure I: R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , R claim 8 , and R=H claim 8 , R=OH claim 8 , R=CF claim 8 , and n=1.11. The method of claim 8 , wherein in chemical ...

Aromatic Derivatives As Anti-Malarial

The present invention discloses anti-malarial compound of formula (I) Formula (I) wherein, X is selected from O or NH; R, R, R, Rand Ris selected from H or OMe or CH, —CH—O—CH— or —CH═CH—CH═CH—; Y is selected from O or NH and R, Ris selected from the following compounds: or pharmaceutically acceptable salts thereof, process for preparation and a pharmaceutical composition containing the same. 2. The compounds as claimed in claim 1 , wherein said compounds are selected from(S)-2-cinnamamido-1-(3,4-dimethoxyphenyl)ethyl cinnamate (1),(R)-2-cinnamamido-1-(3,4-dimethoxyphenyl)ethylcinnamate (2),(S)-1-(3,4-dimethoxyphenyl)ethane-1,2-diyl(2E,2′E)-bis(3-phenylacrylate) (3),(R)-1-(3,4-dimethoxyphenyl)ethane-1,2-diyl(2E,2′E)-bis(3-phenylacrylate)(4),(S)-2-cinnamamido-1-(3,4,5-trimethoxyphenyl) ethyl cinnamate (5),(R)-2-cinnamamido-1-(3,4,5-trimethoxyphenyl)ethyl cinnamate (6),(S)-1-(3,4,5-trimethoxyphenyl)ethane-1,2-diyl (2E,2′E)-bis(3-phenylacrylate) (7),(R)-1-(3,4,5-trimethoxyphenyl)ethane-1,2-diyl(2E,2′E)-bis(3-phenylacrylate) (8),(S)-2-cinnamamido-1-(2-methoxyphenyl)ethylcinnamate (9),(R)-2-cinnamamido-1-(2-methoxyphenyl)ethylcinnamate (10),(S)-1-(2-methoxyphenyl)ethane-1,2-diyl(2E,2′E)-bis(3-phenylacrylate)(11),(R)-1-(2-methoxyphenyl)ethane-1,2-diyl(2E,2′E)-bis(3-phenylacrylate) (12),(S)-2-cinnamamido-1-(3-methoxyphenyl)ethyl cinnamate (13),(R)-2-cinnamamido-1-(3-methoxyphenyl)ethylcinnamate (14),(S)-1-(3-methoxyphenyl)ethane-1,2-diyl (2E,2′E)-bis(3-phenylacrylate)(15),(R)-1-(3-methoxyphenyl)ethane-1,2-diyl(2E,2′E)-bis(3-phenylacrylate)(16),(S)-2-cinnamamido-1-(4-methoxyphenyl)ethyl cinnamate (17),(R)-2-cinnamamido-1-(4-methoxyphenyl)ethylcinnamate (18),(S)-1-(4-methoxyphenyl)ethane-1,2-diyl (2E,2′E)-bis(3-phenylacrylate) (19),(R)-1-(4-methoxyphenyl)ethane-1,2-diyl(2E,2′E)-bis(3-phenylacrylate)(20),(S)-2-cinnamamido-1-(2,3-dimethoxyphenyl)ethyl cinnamate (21),(R)-2-cinnamamido-1-(2,3-dimethoxyphenyl)ethyl cinnamate (22),(S)-1-(2,3-dimethoxyphenyl)ethane-1,2-diyl(2E,2′E ...

Processes for the preparation of tyramine derivatives

Patent FR2154739A1

Substituted m-biphenyloxazoline derivatives

The invention concerns novel m-biphenyloxazoline derivatives of formula (I) in which R<1> and R<2> have the meanings given in the description. The invention also concerns methods and novel intermediate products for their preparation and their use as pesticides.

METHOD OF PREPARING A MEDICINAL PRODUCT WITH LIPID-LOWERING ACTION, THE PREPARED MEDICINAL PRODUCT OBTAINED ACCORDING TO THAT METHOD AND A METHOD FOR PREPARING A PHENOXYALKAAN CARBON ACID DERIVATIVE FOR THE APPLICATION OF THE MEDICINAL PRODUCT.

Synthesis of biphenylalaninol via novel intermediates

The invention relates to a novel synthesis route towards R- biphenylalaninol and to the intermediates applied in this synthesis route. The process according to the invention and the intermediate compounds are useful in the synthesis of pharmaceutically active compounds.

Patent HU164572B

Arthropodicidal benzamides

Compounds of Formula (I), and their agriculturally suitable salts, are disclosed which are useful as arthropodicides, wherein the substituents are described in the specification. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling arthropods which involves contacting the arthropods or their environment with an effective amount of a compound of Formula (I).

Patent FR2154739B1

Ester compound, preparation method and application thereof

Phenoxyalkylcarboxylic acid derivatives and processes for their preparation and their use

Phenoxy-alkyl-carboxylic acid derivatives and process for their preparation

β-三氟甲基烯胺衍生物及其制备方法

本发明涉及一种β‑三氟甲基烯胺衍生物，其结构通式如下： 其中，R 1 、R 2 、R 3 、R 4 、R 5 、R 6 、R 7 、R 8 、R 9 、R 10 独立地选自氢、烷基、烷氧基、卤素或三氟甲基。本发明还提供了一种上述β‑三氟甲基烯胺衍生物的制备方法，包括以下步骤：将取代N‑(2‑苯基‑1‑乙烯基)苯甲酰胺衍生物和tongi试剂在碱、配体和铜盐催化剂的作用下在有机溶剂中于80‑100℃下反应，得到β‑三氟甲基烯胺衍生物。本发明的方法可以高收率的得到多种β‑三氟甲基烯胺衍生物；反应条件温和、操作和后处理过程简单，适合于规模化生产。

안식향산 유도체

내용 없음

Catalysts for chemical reactions in a water-surfactant mixture

The present invention is directed to reaction mixtures comprising a water-surfactant mixture, wherein the catalyst comprises a compound with solubilizing groups. This technology improves the solubility of the reaction components in the water-surfactant mixture and thereby, greatly increases the productivity and selectivity of the chemical reaction.

安息香酸衍生物及其制造方法

本发明涉及由通式[I]即所表示的安息香酸衍生物及其生理学上所允许的盐和它们的制造方法。本发明的化合物在施入人和动物时显示出较强的降脂质作用，并只有极低的毒性，所以作为血中TC、TG值高的高脂血症及动脉硬化症的治疗剂是十分有效的。

水／界面活性剤混合物中における化学反応のための触媒

本発明は、水／界面活性剤混合物を含み、触媒が可溶化基を有する化合物を含む、反応混合物に関する。この技術は、反応成分の水／界面活性剤混合物中における溶解性を向上し、それによって化学反応の生産性および選択性を大幅に向上するものである。

Catalysts for chemical reactions in a water-surfactant mixture

The present invention is directed to reaction mixtures comprising a water-surfactant mixture, wherein the catalyst comprises a compound with solubilizing groups. This technology improves the solubility of the reaction components in the water-surfactant mixture and thereby, greatly increases the productivity and selectivity of the chemical reaction.

用于水-表面活性剂混合物中的化学反应的催化剂

本发明是针对包含水‑表面活性剂混合物的反应混合物，其中该催化剂包含具有增溶基团的化合物。本技术改进了反应组分在水‑表面活性剂混合物中的溶解度，并且从而极大地增加了该化学反应的生产率和选择性。

Disubstituierte biphenyloxazoline

Disubstituted biphenyloxazolines

The present invention relates to novel biphenyloxazolines of the formula (I)in whichX1, X2, X3, R1, R2 and R3 are each as defined in the description,to processes for their preparation and to the use of the biphenyloxazolines for controlling animal pests.

Preparation of ionic pharmaceutical cocrystals using solid and liquid components

Embodiments of the present disclosure pertain to methods of forming a co-crystallized composition by mixing a first molecule in a solid phase with a second molecule in a liquid phase to form a mixture, and then co-crystallizing the mixture to form the co-crystallized composition in the form of a crystalline solid. The mixing of the first and second molecules may occur through the utilization of mechanical force, such as milling. The co-crystallization of the first and second molecules may occur by adding a solvent to the mixture of the molecules and then evaporating the added solvent. The methods may also include a step of utilizing the co-crystallized composition as seed crystals to grow additional co-crystallized compositions. Further embodiments of the present disclosure pertain to the formed co-crystallized compositions.

Bifeniloxazolinas disubstituidas.

Se describen nuevas bifeniloxazolinas de fórmula (I) *fórmula*, en la que X{sup,1}, X{sup,2}, X{sup,3}, R{sup,1}, R{sup,2} y R{sup,3} tienen los significados dados en la descripción, así como procedimientos para preparar estas bifeniloxazolinas y su uso para controlar plagas animales.

Disubstituted biphenyloxazolines

The present invention relates to novel biphenyloxazolines of the formula (I) in which X 1 , X 2 , X 3 , R 1 , R 2 and R 3 are each as defined in the description, to processes for their preparation and to the use of the biphenyloxazolines for controlling animal pests.

Disubstituted biphenyloxazolines

一种生物基自组装酰胺类成核剂及其制备方法和应用

本发明公开了一种生物基自组装酰胺类成核剂，该成核剂由4‑羟基苯乙胺、3,4‑二羟基苯乙胺或3,4,5‑三羟基苯乙胺中的任意一种与对苯二甲酰氯反应生成；本发明的成核剂通过熔融共混的方法与聚乳酸混合，通过挤出或注塑成聚乳酸制品，在制备过程中能够为聚乳酸提供良好的成核效率，并且成核的效果十分稳定，得到的聚乳酸制品具有生物可降解性和力学性能优秀等特点。该类型成核剂制备方法简单，原料来源于生物基，具有可持续发展潜力，易实现大规模生产，能够广泛应用于工业聚乳酸塑料制品的制备。

用于水-表面活性剂混合物中的化学反应的催化剂

本发明是针对包含水‑表面活性剂混合物的反应混合物，其中该催化剂包含具有增溶基团的化合物。本技术改进了反应组分在水‑表面活性剂混合物中的溶解度，并且从而极大地增加了该化学反应的生产率和选择性。