Patent RU2018131460A3

ВИ“? 2018131460” АЗ Дата публикации: 24.03.2020 Форма № 18 ИЗИМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение ж 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2018131460/04(05129Т) 03.02.2017 РСТЛВ2017/000075 03.02.2017 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 62/290,707 03.02.2016 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) НОВЫЕ БИАРОМАТИЧЕСКИЕ СОЕДИНЕНИЯ ПРОПИНИЛА, ФАРМАЦЕВТИЧЕСКИЕ И КОСМЕТИЧЕСКИЕ КОМПОЗИЦИИ, ИХ СОДЕРЖАЩИЕ, И ИХ ПРИМЕНЕНИЕ Заявитель: ГАЛДЕРМА РЕСЕРЧ ЭНД ДЕВЕЛОПМЕНТ, ЕК 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) Аб1К 85/368 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07С 65/19, Аб1К 8/368, АбТО 19/08, С07С 63/66, Аб1К 31/192, АБР 17/19, С07Р 213/80, Аб1К 31/44, Аб1Р 35/00 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): ЕАРАТГУ, Езрасепек, ]-Р1а Рав Рабеагсв, КОРТО, ОЗРТО 6. ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ...

СОЕДИНЕНИЯ, ОБЛАДАЮЩИЕ ИЗБИРАТЕЛЬНОСТЬЮ В ОТНОШЕНИИ РЕЦЕПТОРОВ РЕТИНОИДА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ (ВАРИАНТЫ), СПОСОБ МОДУЛИРОВАНИЯ ПРОЦЕССОВ (ВАРИАНТЫ), СПОСОБ ПОДАВЛЕНИЯ ПАТОЛОГИЧЕСКИХ СОСТОЯНИЙ

Описываются новые соединения общей формулы (I), где значения R1-R5, R14, Q и n указаны в п. 1 формулы, обладающие избирательной активностью в отношении специфических рецепторов ретиноевой кислоты; они могут найти применение при ле чении различных патологических состояний. Описываются фармацевтические композиции на основе соединений формулы (I), способ подавления патологических состояний, а также способ модулирования процессов (варианты). 6 с. и 20 з.п.ф-лы, 12 ил., 6 табл.

СОЕДИНЕНИЯ /ЛИГАНДЫ/, ОБЛАДАЮЩИЕ ИЗБИРАТЕЛЬНОСТЬЮ В ОТНОШЕНИИ РЕЦЕПТОРОВ РЕТИНОИДА Х, ФАРМАКОМПОЗИЦИИ, СПОСОБЫ МОДУЛИРОВАНИЯ ПРОЦЕССОВ, ОПОСРЕДУЕМЫХ РЕЦЕПТОРАМИ РЕТИНОИДА Х, СПОСОБ ЛЕЧЕНИЯ

Примерами таких соединений являются бициклические бензил, пиридинил, тиофен, фуранил и пиррол производные. Описаны способы применения соединений для модуляции процессов, избирательно опосредованных рецепторами ретиноида X.

VERBINDUNGEN MIT SELEKTIVER WIRKUNG FUER RETINOID X REZEPTOREN, UND MITTEL FUER STEUERUNG FUER DURCH RETINOID X REZEPTOREN BEDINGTE PROZESSE

SYNTHESE UND VERWENDUNG VON RETINOID-VERBINDUNGEN MIT NEGATIVER HORMON UND/ODER ANTAGONISTAKTIVITÄT

Stilben derivatives

Compounds of the general formula wherein n is 1 or 2 and, when n is 1, R<1> and R<2> are hydrogen, alkoxy or halogen, or, when n is 2, R<1> is hydrogen, alkoxy or halogen and R<2> is hydrogen; R<3>, R<4>, R<5> and R<6> are hydrogen or alkyl; R<7> is hydrogen, methyl or ethyl; R<8> and R<9> are hydrogen, alkyl or halogen, and R10 is -(CH=CR<19>)m, in which m is zero or 1 and R<11> is or 2-oxazolinyl, or, when m is 1, also is hydrogen; R<12> is hydrogen or alkyl; R<13> is hydrogen, alkyl or -N(R<17>, R<18>) or -OR<14>; R<14> is hydrogen, alkyl or alkanoyl; R<15> is hydrogen, alkyl or -OR<16> or -(CH2)pN(R<17>, R<18>); R<16> is hydrogen, alkyl, hydroxy alkyl or optionally, substituted aryl, or aralkyl; R<17> and R<18> are hydrogen or alkyl or R<17> and R<18> together with the nitrogen atom form a heterocyclic group; R<19> is hydrogen or alkyl and p is zero, 1, 2 or 3; ketals and salts thereof are useful for the treatment of neoplasms, dermatological conditions and rheumatic illnesses.

SUBSTITUTED (5,6) - DIHYDRONAPHTHALINYLVERBINDUNGEN WITH RETINOID WELL-BEHAVED EFFECT

BIARYL PHOSPHOLIPASE a2 INHIBITORS

ALICYCLI PHOSPHOLIPASE a2 INHIBITORS

ARYLODER HETEROARYL-SUBSTITUTED 3,4DIHYDROANTHRACENE AS WELL AS ARYLODER HETEROARYL-SUBSTITUTED BENZO (1,2G) - CHROM-3-EN, BENZO (1, 2G) - THIOCHROM-3-ENUND BENZO (1,2G) - 1,2DIHYDROCHINOLIN-DERIVATE WITH RETINOID MORE ANTAGONISTICALLY OR INVERSE of ANTAGONISTIC ACTIVITY

Procedure for the production of aromatic connections with Stilbenkonfiguration (EN)

SYNTHESIS AND USE OF RETINOIDEN WITH NEGATIVES HORMONELLEN AND/OR ANTAGONISTIC EFFECTS

RETINOID X RECEPTOR SELECTIVE CONNECTIONS

Alkyl, alkenyl and alkynyl chrysamine g derivatives for the antemortem diagnosisof alzheimer's disease and (in vivo) imaging and prevention of amyloid depositi on

Novel ligands that are antagonists of raf receptors, process for preparing them and use thereof in human medicine and in cosmetics

Retinoid-like compounds

Treatment of neurodegenerative diseases

The present disclosure relates to compounds to be used in a low dose in treatment of neurodegenerative diseases or disorders. It also relates to methods for treatment of a neurodegenerative diseases or disorders.

Aryl or heteroaryl substituted 3,4-dihydroanthracene and aryl or heteroaryl substituted benzo{1,2-g}-chrom-3-ene, benzo{1,2-g}-thiochrom-3-ene and benzo{1,2-g}-1,2-dihydroquinoline derivatives

Diaromatic propynyl or dienyl compounds

4-VINYLBENZOIC ACID DERIVATIVES; PROCESS FOR PREPARING THE SAME AND THEIR USE AS LIGANDS AND THERAPEUTIC AGENTS

Société dite : laboratoires CHAUVIN-BLACHE Inventeurs : COQUELET Claude ROUSSILLON Samia SINCHOLLE Daniel BONNE Claude ALAZET Alain Nouveaux dérivés de l'acide vinyl-4 benzoïque, leur procédé de préparation et leurs applications en thérapeutique et comme ligands. L'invention a pour objet des composés de formule Ces composés peuvent être utilisés en thérapeutique pour le traitement de l'acné, du psoriasis, des troubles de la kératinisation, dans certaines formes de cancer et comme agents cicatrisants, notamment dans le domaine oculaire. Fig. Néant ...

COSMETICS

L'invention a pour objet de nouvelles compositions cosmétiques contenant de nouveaux dérivés insaturés cycloaliphatiques à titre d'agents actifs ou d'ingrédients. Ces nouveaux dérivés peuvent être représentés par la formule: dans laquelle R1 à R7 représentent H ou C1-C4 alkyle; R8 représente -C=N, oxazolinyle, -CH2OR9 ou =?-R10; Z représente un radical monoaliphatique saturé ou un radical bi ou tri-cyclique; a et e représentent 0,1 ou 2 et b, c et d représentent 0 ou 1, étant entendu que: a + c + e ? 1 et b et/ou d = 1.

TETRALIN DERIVATIVES, THEIR PREPARATION AND THEIR USE

Disclosed are novel tetralin derivative of the formula (I): (I) where R1 is hydrogen, C1-C4-alkyl, C1-C4-alkoxy or halogen, R2 is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl, X is -CH2-CO-, -CH2-CHOH, -CH2-C(R4)OH-, -CH2-C(OCOR4)H-, -CH2-C(R4)(OCHOR5)-, -CHOH-CHOH-, -CH=CH-, -CH(OCOR4) -CH(OCOR4)-, -CH2-CH(OR4)- (where R4 and R5 are each C1-C4-alkyl) and R3 is nitrile, C2-C10-ketal or -CH(R7)(R8)- or -CO-R9, where R7 is hydrogen or C1-C3-alkyl, R8 is hydrogen, C1-C3-alkyl or -OR10 or -NR11R12 (where R10, R11 and R12 are each hydrogen, C1-C4-alkyl, C2-C20-alkanoyl or unsubstituted or substituted benzoyl) and R9 is hydrogen, halogen, C1-C4-alkyl, azido, or -OR13 (where R13 is hydrogen or C1-C8-alkyl or is C2-C6 alkyl which is substituted by one or more hydroxyl groups or a C1 -C4 - alkoxy group, or is aryl or aralkyl) and, where relevant, its physiologically tolerated salts. These derivatives are useful in the therapy of dermatological disorders and the prophylactic and therapeutic treatment ...

MONOSTYRYL-NAPHTHALENE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS OPTICAL BRIGHTENERS

STILBENE DERIVATIVE AND PREPARATION METHOD THEREOF

The present invention relates to a stilbene derivative and a method for preparing same. More particularly, the present invention relates to a novel stilbene derivative inhibiting a function of a cyclophilin and effective for preventing a cyclophilin-associated disease or treating a symptom thereof, and to a method for preparing the stilbene derivative.

DRUG DERIVATIVES

The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention ...

AROMATIC CARBOXYLIC ACID DERIVATIVES

Compounds of the formula I wherein R1 is a residue of the formula (a) or (b) and R2-R10 have the significance given in the specification can be used as pharmaceuticals, particularly for dermatological and oncological indications.

COMPOUNDS HAVING SELECTIVITY FOR RETINOID X RECEPTORS

Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

RXR HOMODIMER FORMATION AND BRIDGED BICYCLIC AROMATIC COMPOUNDS AND THEIR USE IN MODULATING GENE EXPRESSION

... 2149882 9412880 PCTABS00032 The invention provides a method of screening a substance for the ability to affect the formation of a retinoid X receptor homodimer comprising combining the substance and a solution containing retinoid X receptors and determining the presence of homodimer formation. The screening method can be used to determine compounds which selectively activate homodimer formation and heterodimer formation. Also provided is a method of screening a substance for an effect on a retinoid X receptor homodimer's ability to bind DNA comprising combining the substance with the homodimer and determining the effect of the compound on the homodimer's ability to bind DNA. Finally, the invention provides methods of activating retinoid X receptor homodimer formation. Bridged bicyclic aromatic compounds are provided having structure (I); wherein R1, R2, R3, R4, R5 and n are as defined herein. The compounds are useful for modulating gene expression of retinoic acid receptors, vitamin D receptors ...

PPAR GAMMA ANTAGONISTS FOR TREATING OBESITY

The present invention relates to a method of treating obesity, diabetes and other metabolic disorders in a mammal by administering to the mammal a pharmaceutical composition containing a compound that antagonizes the activi ty of PPAR.gamma. protein, or reduces the expression of PPAR.gamma. protein. Th is invention also features methods of screening for compounds for treating obesity, diabetes and other metabolic disorders.

UNSATURATED DERIVATIVES IN POSITION -4 OF 6-TERT-BUTYL-1, 1-DIMETHYLINDAN AND THEIR USE IN HUMAN OR VETERINARY MEDICINE AND IN COSMETICS

Dérivés insaturés en position -4 du 6-tert-butyl-1,1-diméthyl-indane de formule : (voir fig. I) X représente : (i) soit un radical de formule : (a) (voir fig. II) et Y représente un radical de formule : (b) (voir fig. III) , (ii) soit un radical de formule : (c) (voir fig. IV) et Y représente soit un radical de formule (b) soit un radical de formule : (voir fig. V) (voir fig. VI) ou (voir fig. VII) Z étant -O-, -S- ou ~N-R3, R1 représente -CH3, -(CH2)p-OR4, -(CH2)p-COR5, ou -S(O)t-R6, p étant 0, 1, 2 ou 3, t étant 0, 1 ou 2, R2 représente H ou alkyle inférieur, R3 représente H, alkoxy inférieur ou -OCOR7, R4 représente H, alkyle inférieur, -COR7, aryle, aralkyle, mono ou polyhydroxyalkyle, ou un radical poly éther, R5 représente H, alkyle inférieur, -OR8 ou - N(r')(r"), R6 représente H ou alkyle inférieur, R7 représente alkyle inférieur, R9 représente H, alkyle, alkén yle, alkynyle, aryle, aralkyle, mono- ou polyhydroxyalkyle, un reste de sucre ou d'acide aminé. r' et r" représentent H, ...

SYNTHESIS AND USE OF RETINOID COMPOUNDS HAVING NEGATIVE HORMONE AND/OR ANTAGONIST ACTIVITIES

Aryl-substituted and aryl and (3-oxo-1-propenyl)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.

Styryl-naphthalene derivatives as optical brighteners

Styryl-naphthalene compounds, which are colourless or at most slightly coloured, have formula:- A-CH=CH-B-CH-A', where B is a naphthalene residue which has the A-CH=CH- and A'-CH=CH- groups in the 1,5- or 2,6-positions, A and A' are benzene residues, naphthalene residues or biphenyl residues and at least 1 of the ring systems A, A' and B has a (functionally modified) sulphonic acid group, a sulphone group, a (modified) carboxylic acid group or a nitrile group, and may also have 1 or more C is not >18 alkyl or alkoxy groups, halogen atoms or methylene dioxy groupings. The compounds are optical brighteners, for use in synthetic high-molecular polymers, semi-synthetic materials such as cellulose derivatives and casein synthetics, and natural materials such as textile fibres, natural resins, rubber, gutta-percha and balata. They can also be used as scintillators in photographic products.

Verfahren zur Herstellung von Styrylnaphthalin-Derivaten

Verfahren zur Herstellung von neuen Bis-stilbenverbindungen

Bis-stilbene compds for use as optical brighteners

Fluorescent bis-stilbene compds. for use as optical brighteners have formula (I). R1 - CH = CH - X - CH = CH - R2 X = a diphenyl group linked at the 4 and 4' positions with the CH group; and R1 and R2 = each monocyclic benzene groups, diphenyl groups or naphthalene groups; and at least one of the rings X, R1 and R2 is substd. by sulphonic acid, sulphone, carboxylic acid, nitrile, hydroxyl, mercapto or methyl. (I) are useful optical bighteners for treating org. materials, including synthetic polymers and fibres.

Prepg. fluorescent bis-stilbene cpds. - for use as optical brighteners for organic materials

Title cpds. of formula (I): (where R3 is diphenylyl or the gp. (a): R4 is phenyl, diphenyl, alpha- or beta-naphthyl or the gp. (a) V1', V2' and V3' replacing V1, V2 and V3, and in which V1 and V2' are indep. sulpho gps. together with their salts, esters, amides and halides or carboxyl gps. together with their salts, esters and amides, or they are CN, Me, OH or sulphonyl; V2 and V2' are indep. H, 1-18C alkyl, 1-12C alkoxy, halogen, or sulpho gps. together with their salts, esters or amides; V3 and V3' are indep. H or 1-4C alkyl; W1 is sulpho together with the salts, esters or amides, 1-4C alkyl or alkoxy, carboxyl together with the salts, esters, or amides, CN or halogen; W1 or V1 and/or V1' may also be H; when W1 differs from H, R3 and/or R4 are diphenylyl) are prepd. by reacting 1 mol. of (II): with 1 mol. of R3-CHO and 1 mol. of R4-CHO, or 1 mol. of (II) where CHO-replaces Z3 is reacted with 1 mol. of R3-Z3 and 1 mol. of Z3-R4 (where Z3 is -CH2-PO(OR)2, -CH2(PO)ROR or -CH=P(R)3, in which ...

Makromolekularen organischen Stoff und optischen Aufheller enthaltende Mischung

Verfahren zur Herstellung aromatischer, Äthylendoppelbindungen enthaltender Verbindungen

VERFAHREN ZUR HERSTELLUNG NEUER STILBEN-DERIVATE.

Bis-stilbene compds for use as optical brighteners

Fluorescent bis-stilbene compds. for use as optical brighteners have formula (I). R1 - CH = CH - X - CH = CH - R2 X = a diphenyl group linked at the 4 and 4' positions with the CH group; and R1 and R2 = each monocyclic benzene groups, diphenyl groups or naphthalene groups; and at least one of the rings X, R1 and R2 is substd. by sulphonic acid, sulphone, carboxylic acid, nitrile, hydroxyl, mercapto or methyl. (I) are useful optical bighteners for treating org. materials, including synthetic polymers and fibres.

NAPHTHALENIC DERIVATIVES WITH RETINOIC, METHODS FOR THEIR PREPARATION AND MEDICINAL AND COSMETIC COMPOSITIONS CONTAINING THEM.

THE CYCLOALIPHATIC UNSATURATED COMPOUNDS AND PHARMACEUTICAL OR COSMETIC COMPOSITIONS CONTAINING THEM.

Verwendung von Bis-stilbenverbindungen als optische Aufhellmittel für textile organische Materialien

КАРБОНОВЫЕ КИСЛОТЫ

Настоящее изобретение относится к карбоновым кислотам формулы (I) и их применению для лечения и/или предупреждения ожирения и/или расстройств обмена веществ, опосредуемых инсулинорезистентностью или гипергликемией, включая диабет типа I и/или II, неадекватную толерантность к глюкозе, инсулинорезистентность, гиперлипидемию, гипертриглицеридемию, гиперхолестеринемию, синдром поликистоза яичников (PCOS). В частности, настоящее изобретение относится к применению карбоновых кислот формулы (I) для модуляции, особенно, для ингибирования активности РТР.

ДИАРОМАТИЧЕСКИЕ СОЕДИНЕНИЯ ПРОПИНИЛА ИЛИ ДИЕНИЛА, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ, ФАРМАЦЕВТИЧЕСКИЕ И КОСМЕТИЧЕСКИЕ КОМПОЗИЦИИ НА ОСНОВЕ УКАЗАННЫХ СОЕДИНЕНИЙ И ПРИМЕНЕНИЕ КОСМЕТИЧЕСКИХ КОМПОЗИЦИЙ

DERIVATIVES OF MEDICINAL AGENTS

КАРБОНОВЫЕ КИСЛОТЫ

Настоящее изобретение относится к карбоновым кислотам формулы (I) и их применению для лечения и/или предупреждения ожирения и/или расстройств обмена веществ, опосредуемых инсулинорезистентностью или гипергликемией, включая диабет типа I и/или II, неадекватную толерантность к глюкозе, инсулинорезистентность, гиперлипидемию, гипертриглицеридемию, гиперхолестеринемию, синдром поликистоза яичников (PCOS). В частности, настоящее изобретение относится к применению карбоновых кислот формулы (I) для модуляции, особенно, для ингибирования активности РТР.

DIAROMATIC COMPOUNDS PROPINILA OR DIENILA, INTERMEDIATE COMPOUNDS, PHARMACEUTICAL AND COSMETIC COMPOSITIONS BASED ON INDICATED COMPOUNDS AND APPLICATION OF COSMETIC COMPOSITIONS

DERIVED FROM THE STILBENE, THEIR PREPARATION AND THEIR APPLICATION AS DRUGS

Dérivés du stilbène, leur préparation et leur application en tant que médicaments. Les composés selon l'invention ont pour fomule : Stilbene derivatives, their preparation and application as drugs. The compounds according to the invention have the following formula:

DERIVES DU STILBENE, LEUR PREPARATION ET LEUR APPLICATION EN TANT QUE MEDICAMENTS

Dérivés du stilbène, leur préparation et leur application en tant que médicaments. Les composés selon l'invention ont pour fomule : ...

DERIVED FROM THE STILBENE, THEIR PREPARATION AND THEIR APPLICATION AS DRUGS

AZULENIC RETINOID COMPOUNDS, COMPOSITIONS AND METHODS

Novel azulenic retinoid compounds and therapeutic compositions are disclosed, along with method for their production and use as anti-cancer and cancer-prevention agents. The compositions of the present invention will also find use in treating dermatological disorders such as acne and psoriasis, as well as dermatologically-related conditions such as repair and effacement of wrinkles.

Biaromatic propynyl compounds, pharmaceutical and cosmetic compositions containing same, and uses thereof

Compounds of general formula (I) are described. Also described, is the use of such compounds in pharmaceutical compositions for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmologic disorders, in particular), or in cosmetic compositions.

EBNA1 inhibitors and their method of use

Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.

MICROPOROUS COORDINATION COMPLEX AND METHOD OF MAKING THE SAME

Disclosed herein is a three-dimensional coordination complex that includes a plurality of inorganic centers; a plurality of a first bis(bidentate) linker; and a plurality of a second bis(bidentate) linker, where the first and the second bis(bidentate) linkers are have different lengths, and the bidentate binding sites on each linker face in opposite directions on an axis.

РЕТИНОИДНЫЕ СОЕДИНЕНИЯ (ВАРИАНТЫ), КОМПОЗИЦИЯ, СПОСОБ ОПРЕДЕЛЕНИЯ АНТАГОНИСТОВ РЕТИНОИДНЫХ ГОРМОНОВ, СПОСОБ ЛЕЧЕНИЯ И ПРОМЕЖУТОЧНЫЕ ПРОДУКТЫ

FIELD: organic chemistry, medicine. SUBSTANCE: invention relates to novel retinoid compounds of general formulas (I) , (II) , (III) and (IV) eliciting retinoid negative hormonal biological activity and/or similar activity of antagonist of retinoids based on thereof, method of assay of antagonists of retinoid hormones, method of treatment of pathological state in mammal showing sensitivity to treatment with retinoid antagonist or negative hormone by administration of compound of the formula (I) or (II). In indicated compounds of formulas (I), (II), (III) and (IV) X is taken among oxygen, sulfur atom, [C(R 1 ) 2 ] n′ , respectively; R 1 means hydrogen atom or alkyl with number of carbon atoms from 1 to 6; R 2 means hydrogen atom pr lower alkyl with number of carbon atoms from 1 to 6, fluorine, chlorine, bromine, iodine atoms, CF 3 , fluorosubstituted alkyl with number of carbon atoms from 1 to 6, hydroxygroup, SH-group, alkoxy-group with number of carbon atoms from 1 to 6 or alkylthio-group with number of carbon atoms from 1 to 6; R 3 means hydrogen atom or lower alkyl with number of carbon atoms from 1 to 6 or fluorine atom; m means whole number from 0 to 3; o means whole number from 0 to 3; Z means -C≡C-, -CO-NH, -COO-, -CSNH-, -CH=CH-, -(CR 1 =CR 1 ) n′ where n' means whole number from 0 to 5 or Z is absent; Y means phenyl or naphthyl group or heteroaryl taken among group consisting of pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyranozyl, thiazolyl, oxazolyl, imidazolyl and pyrazolyl. EFFECT: improved method of assay and treatment, valuable properties of compounds. 167 cl, 18 tbl, 20 dwg тзЗзЗ$ 0ОССс ПЧ сэ (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ” 2 203 884 ' (51) МПК” 13) С2 335/06, С 07 0 335/06, А 61 К 31/245, 31/382, 38/09, А 61 Р 5/00 С 07С 69/48, 63/331, 403/20, 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 98105966/04 , 23.08.1996 (24) Дата начала действия патента: 23.08.1996 (30) Приоритет: 01.09. ...

Способ получения бис-стильбеновых соединений

Neue Styrylnaphthalin-Derivate,Verfahren zu deren Herstellung und Verwendung

5,6-DIHYDRONAPHTHALENYLDERIVATE MIT RETINOID-ARTIGER AKTIVITÄT

TETRALIN-DERIVATE, IHRE HERSTELLUNG UND VERWENDUNG

PLEIADENE AND DIBENZOHEPTALENE DERIVATIVES

1357027 Pleiadenones and dibenzoheptalenones; organolithium compounds SANDOZ Ltd 27 Sept 1971 [1 Oct 1970] 44811/71 Headings C2C and C2J Novel pleiadenones and dibenzoheptalenones of the general formula wherein n is 1 or 2, R 1 is a hydrogen, fluorine or chlorine atom or a trifluoromethyl group and R 2 is as R 1 or a straight chain C 1 -C 4 alkyl or C 1 -C 4 alkoxy group, provided that R 2 is other than an alkoxy group when n is 1, are prepared by cyclization of an o-toluic acid derivative of the general formula wherein Z is a hydroxy or C 1 -C 4 alkoxy group or a chlorine, bromine or iodine atom. o-Toluic acid derivatives of the second general formula above wherein Z is a hydroxy group are prepared by reaction of a ketone and a lithium compound of the respective general formulae wherein R 3 is a C 1 -C 4 alkyl group, followed by hydrolysis, treatment of the resulting otoluamide derivative of the general formula with a strong base, followed by a strong mineral acid, and reduction of the resulting lactone or hydroxy-carboxylic acid of the respective general formulae The lithium compounds of the fourth general formula above are prepared by treating the corresponding 2 - methyl - 4 - R 1 - N - R 3 - benzamide with a n-butyl lithium.

UNSATURATED CYCLOALIPHATIC DERIVATIVES

SELECTIVITY FOR RETINOID X RECEPTORS CONTAINING CONNECTIONS

USE OF AROMATIC CARBONIC ACID DERIVATIVES FOR THE PRODUCTION OF PHARMACEUTICAL PREPARATIONS

IN WATER DISPERSE-CASH, UV-RADIATION ABSORBING COPOLYMER

Optical clarification means

TREATMENT OF NIDDM (NICHTINSULINABHÄNGIGE DIABETES MELLITUS) WITH RXR AGONISTEN

4-VINYLBENZOESAEURE-DERIVATE, YOUR PRODUCTION AND USE AS DRUGS AND LIGANDE.

TETRALIN DERIVATIVES, YOUR PRODUCTION AND USE.

PROCEDURE FOR THE PRODUCTION OF NEW STILBEN DERIVATIVES AND THEIR SALTS

TETRACYCLI AROMATIC RETINOIDE CONNECTIONS, YOUR PRODUCTION AND USE

TRISUBSTITUTED PHENYL DERIVATIVES WITH RETINOID AGONIST, ANTAGONIST OR INVERSAGONIST BIOLOGICAL ACTIVITY

Novel biaromatic propynyl compounds, pharmaceutical and cosmetic compositions containing same, and uses thereof

The invention relates to novel compounds of general formula (I), as well as the use of said compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmologic disorders, in particular), or in cosmetic compositions.

Alicyclic phospholipase A2 inhibitors

1,1'-(1,2-ETHYNEDIYL)BIS-BENZENE DERIVATIVES AS PTP 1-B INHIBITORS

... ²²²The present invention is related to carboxylic acids of Formula (I) and use ²thereof for the treatment and/or prevention of obesity and/or metabolic ²disorders mediated by insulin resistance or hyperglycemia, comprising diabetes ²type I and/or II, inadequate glucose tolerance, insulin resistance, ²hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, polycystic ovary ²syndrome (PCOS). In particular, the present invention is related to the use of ²carboxylic acids of Formula (I) to modulate, notably to inhibit the activity ²of PTPs.² ...

DERIVES NAPHTALENIQUES, LEUR PROCEDES DE PREPARATION ET COMPOSITION COSMETIQUE LES CONTENANT

L'invention concerne un compose de formule (II): (II) (II) et les isomères et sels correspondants, formule dans lequelle a et b sont des entiers pouvant prendre, indépendamment l'un de l'autre, les valeurs 0 ou 1, R1, R2, R3 et R4 représentent, indépendamment, un atome d'hydrogène, un radical alkyle linéaire ou ramifié C1-C6 ou un radical alcoxy C1-C6, R6 représente un radical alkyle C1-C6, R5 et R12 représentent un atome d'hydrogène ou un radical alkyle C1-C6, sous réserve que R5 ne peut représenter l'hydrogène si a = b = 0, et R11 a diverses significations. L'invention concerne également un procédé pour la préparation des composés de formule (II) ainsi que des compositions cosmétiques contenant lesdits composés.

BICYCLIC NAPHTHALENIC DERIVATIVES, PROCESS FOR THEIR PREPARATION AND USE IN HUMAN AND VETERINARY MEDICINE

L'invention concerne les composés de formule générale (I) (I) dans laquelle: - A représente un radical méthylène ou diméthylène, substitués ou non par un radical alkyle inférieur, - R1, R2, R3 et R4, identiques ou différents, représentent un atome d'hydrogène ou un radical alkyle inférieur ayant de 1 à 6 atomes de carbone, ou R1 et R3, pris ensemble, forment un pont méthylène ou diméthylène, quand A représente un radical diméthylène, - R' représente un atome d'hydrogène, un radical OH, un radical alkoxy ayant de 1 à 4 atomes de carbone, un radical acyloxy ayant de 1 à 4 atomes de carbone ou un radical amino, - R" représente un atome d'hydrogène ou un radical alkoxy ayant de 1 à 4 atomes de carbone, ou - R' et R", pris ensemble, forment un radical oxo (=O), méthano (=CH2) ou hydroxyimino (=N-OH), et - R représente le radical -CH2OH ou le radical -COR5, R5 représentant un atome d'hydrogène, le radical OR6 où R6 représente un atome d'hydrogène, un radical alkyle ayant de 1 à 20 atomes ...

STILBENE DERIVATIVES

This invention is concerned with compounds of the general formula (I) wherein n stands for 1 or 2 and, when n stands for 1, R1 and R2 represent hydrogen, lower alkoxy or halogen, or, when n stands for 2, R1 represents hydrogen, lower alkoxy or halogen and R2 represents hydrogen; R3, R4, R5 and R6 represent hydrogen or lower alkyl; R7 represents hydrogen, methyl or ethyl; R8 and R9 represent hydrogen, lower alkyl or halogen; and R10 represents a group of the formula -(CH=CR19)mR11, in which m stands for zero or 1 and R11 represents a group of the formula or or the 2-oxazolinyl group, or, when m stands for 1, also represents hydrogen; R12 represents hydrogen or lower alkyl; R13 represents hydrogen, lower alkyl of a group of the formula -N(R17,R18) or -OR14; R14 represents hydrogen, lower alkyl or alkanoyl; R15 represents hydrogen, lower alkyl or a group of the formula -OR16 or -(CH2)pN(R17, R18) R16 represents hydrogen, lower alkyl, hydroxy-(lower alkyl), aryl, substituted aryl, aralkyl or ...

CYCLOALIPHATIC UNSATURATED DERIVATIVES, PROCESS FOR THEIR PREPARATION AND USE AS THERAPEUTIC AGENTS

NOVEL LIGANDS THAT ARE ANTAGONISTS OF RAR RECEPTORS, PROCESS FOR PREPARING THEM AND USE THEREOF IN HUMAN MEDICINE AND IN COSMETICS

RETINOID-LIKE COMPOUNDS

The present invention relates to a compound of formula I I or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, in which X is -O-CO-, -NH-CO-, -CS-NH-, -CO-O-, -CO-NH-, -COS-, -SCO-, -SCH2-, -CH2-CH2-, -C?C-, -CH2-NH-, -COCH2 -, -NHCS-, -CH2S-, -CH20-, -OCH2-, -NHCH2- or -CR5=CR6-; Rm and Rk are independently hydrogen, halogen, C1-6alkyl, hydroxy, C1-6alkyloxy or nitro; n is zero or one; R4 is -(CH2)t-Y, C1-6alkyl, or C3-6cycloalkyl; R1 is -CO2Z, C1-6alkyl, CH2OH, -CONHRY, or CHO; R2 and R3 are independently hydrogen or C1-6alkyl; Ra and Rb are independently hydrogen or C1-6alkyl; but when n is one, Ra and Rb together can form a radical of the formula ; Y is naphthyl or phenyl, both radicals can be optionally substituted with one to three same or different C1-6alkyl or halogen; Z is hydrogen or C1-6alkyl; R5, R6 and RY are independently hydrogen or C1-6alkyl; and t is zero to six. Also provided by this invention are methods for ...

DIAROMATIC PROPYNYL OR DIENYL COMPOUNDS

L'invention concerne de nouveaux composés propynyl ou diényl biaromatiques qui présentent comme formule générale (I), ainsi que l'utilisation de ces derniers dans des compositions pharmaceutiques destinées à un usage en médecine humaine ou vétérinaire (affections dermatologiques, rhumatismales, respiratoires, cardiovasculaires et ophtalmologiques notamment), ou bien encore dans des compositions cosmétiques.

SYNTHESIS AND USE OF RETINOID COMPOUNDS HAVING NEGATIVE HORMONE AND/OR ANTAGONIST ACTIVITIES

Aryl-substituted and aryl and (3-oxo-I-propenyl)- substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.

ALKYL, ALKENYL AND ALKYNYL CHRYSAMINE G DERIVATIVES FOR THE ANTEMORTEM DIAGNOSIS OF ALZHEIMER'S DISEASE AND IN VIVO IMAGING AND PREVENTION OF AMYLOID DEPOSITION

Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.

NEW STYRYLNAPHTHALENE DERIVATIVES, PROCESS FOR THEIR MANUFACTURE AND USE

2-SUBSTITUTED-5-OXO-5H-DIBENZO %A,D<-CYCLOHEPTENES, THE SALTSAND ESTERS THEREOF, HAVING PHARMACEUTICAL ACTIVITY, AND METHODS AND COMPOSITIONS FOR THE USE THEREOF

Alicyclic phospholipase A2 inhibitors number

TREATMENT OF DMNDI WITH AGONISTAS OF OF RXR

COMPOSTOS,PROCESSO PARA SUA FABRICACAO,PREPARACAO FARMACEUTICA,E COMPOSTOS UTEIS COMO INTERMEDIARIOS PARA OBTENCAO DOS COMPOSTOS SUPRA MENCIONADOS

Bicyclic naphthalenic derivatives, a process for preparing the same and human or veterinary medicines and cosmetic compositions containing said derivatives

A bicyclic naphthalenic compound has the formula (I) wherein A represents methylene or dimethylene, substituted or not by lower alkyl, R1, R2, R3 and R4 represent hydrogen or lower alkyl, or R1 and R3 taken together form a methylene or dimethylene bridge when A represents dimethylene, R' represents hydrogen, OH, alkoxy having 1-4 carbon atoms, acyloxy having 1-4 carbon atoms or amino, R'' represents hydrogen or alkoxy having 1-4 carbon atoms, or r' and R'' taken together form an oxo, methano or hydroxyimino group, R represents -CH2OH or -COR5, R5 represents hydrogen, -OR6 or R6 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl, polyhydroxyalkyl, aryl or aralkyl optionally substituted, the residue of a sugar or p is 1, 2 or 3, and r' and r'', each independently, represent hydrogen, lower alkyl, monohydroxyalkyl optionally interrupted by a heteroatom, polyhydroxyalkyl, aryl or benzyl optionally substituted, the residue of an amino acid, an aminoester ...

Benzocycloheptene derivatives

A compound of the formula см. иллюстрацию в PDF-документе wherein R1 is hydroxy, lower-alkoxy, amino, mono- or di-lower-alkylamino; R2 is hydrogen, alkyl, akoxy or halogen; R3, R4, R5, R6, R11 and R12 independently are hydrogen or lower-alkyl; R3 and R5 taken together are methylene or hydroxymethylene; R7, R8, R9 and R10 independently are hydrogen or lower-alkyl; R11 and R12 taken together are oxo or spiro-cyclo-lower alkyl; or R11 is hydrogen and R12 is hydroxy or acetoxy; and one of the residues R13 and R14 is hydrogen and the other is lower-alkyl or trifluoromethyl, as well as physiologically compatible salts of carboxylic acids of formula I, which can be used as medicaments, especially for the treatment of neoplasms, acne and psoriasis, are described. The compounds of the invention can be prepared by the synthesis of the C(R13)=C(R14) double bond according to Wittig from a corresponding bicyclic component and a corresponding monocyclic component and optional subsequent transformation ...

An intermediate in the preparation of 2-(5H-dibenzo[a,d]cyclophepten-5-on-2-yl)acetic, propionic and butyric acids

... 2-(5H-Dibenzo[a,d]cyclohepten-5-on-2-yl)acetic, propionic and butyric acids, are prepared from glycidonitrile intermediates. The acid products exhibit anti-inflamatory, analgesic and anti-pyretic activity.

Compounds having selective activity for retinoid X receptors, and means for modulation of processes mediated by retinoid X receptors

Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

Trisubstituted phenyl derivatives having retinoid agonist, antagonist or inverse agonist type biological activity

Compounds of the formulawhere the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.

Naphtenic and heterocyclic retinoic acid analogues

Naphthenic and heterocyclic retinoic acid analogues such as (E)-6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthaldehyde, methyl 6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthoate, 6-[2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethenyl]-2-naphthoic acid, (E)-1-(5-carbethoxy-2-furanyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexe n-1-yl)-1,3-butadiene, (E)-1-(5-carboxy-2-furanyl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1 -yl)-1,3-butadiene, (E)-1-(5-carbethoxythien-2-yl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexe n-1-yl)-1,3-butadiene, and (E)-1-(5-carboxythien-2-yl)-2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-1 -yl)-1,3-butadiene. These retinoids are useful as chemopreventive agents for inhibiting tumor promotion in epithelial cells and for treating nonmalignant skin disorders.

NEW COMPOUNDS, THEIR PREPARATION AND USE

The present invention provides novel compounds of general formula (I) wherein R1, R2, W, Z and R5 to R9 are defined more fully in the description. The compounds are useful in the treatment of ailments and disorders where a reduction of the blood glucose is beneficial, such as diabetes.

Novel bexarotene analogs

The present invention relates to analogs of bexarotene and methods of use thereof.

Compositions and Methods for Modification of Biomolecules

The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Metal-organic framework materials with ultrahigh surface areas

A metal organic framework (MOF) material including a Brunauer-Emmett-Teller (BET) surface area greater than 7,010 m 2 /g. Also a metal organic framework (MOF) material including hexa-carboxylated linkers including alkyne bond. Also a metal organic framework (MOF) material including three types of cuboctahedron cages fused to provide continuous channels. Also a method of making a metal organic framework (MOF) material including saponifying hexaester precursors having alkyne bonds to form a plurality of hexa-carboxylated linkers including alkyne bonds and performing a solvothermal reaction with the plurality of hexa-carboxylated linkers and one or more metal containing compounds to form the MOF material.

RESINOUS COMPOUND CRYSTALLIZATION USING NON-POLAR SOLVENT SEQUENCE

A resin containing a desirable compound is extracted from plant material and dissolved in a volatile non-polar solvent. The solvent is evaporated, cooling the solution and increasing the saturation level of the compound in the solution. A second volatile non-polar solvent, in which the compound is less soluble, is then added to the solution and evaporated. This again cools the solution and increases the saturation level until the compound has started to crystallize. The crystals are then filtered and rinsed. Crystallization is more rapid compared to traditional techniques. The resin is obtained from the plant material using an extraction solvent to form a solution, which is then floated above an immiscible liquid, where it is drawn off through a screen and the extraction solvent evaporated. 1. A method for crystallizing a compound from a resin , comprising:mixing a first non-polar solvent with the resin to form a solution;evaporating the first non-polar solvent from the solution;then, mixing a second non-polar solvent with the solution, wherein the compound has a lower solubility in the second non-polar solvent than in the first non-polar solvent;removing the second non-polar solvent from the solution to cause a temperature of the solution to drop and the compound to form crystals.2. The method of claim 1 , wherein the first non-polar solvent has a higher boiling point than the second non-polar solvent.3. The method of claim 1 , wherein the first non-polar solvent is miscible with the second non-polar solvent.4. The method of claim 1 , wherein the first non-polar solvent is butane and the second non-polar solvent is propane.5. The method of claim 1 , wherein the first non-polar solvent is evaporated by pumping off the first non-polar solvent in its gaseous phase.6. The method of claim 1 , wherein the solution is maintained at a temperature of 0-20° C. and between a pressure of 0-140 kPa while evaporating the first non-polar solvent from the solution.7. The method of ...

ANTICONVULSANT COMPOUNDS

The present application relates to compounds and methods for reducing the severity of convulsant activity or epileptic seizures, or for the treatment of chronic or acute pain. 132-. (canceled)341. The compound of claim , wherein R=R=CH , or a pharmaceutically acceptable salt thereof.352. The compound of claim , wherein Ris:H;{'sub': 5', '5', '3', '2', '5', '3', '2', '3, 'C(O)R, wherein Ris H, CH, CH, CH(CH), CHCHCN, or aryl;'}{'sup': '−', 'sub': 6', '6', '2', '6', '5', '2, 'C(O)—O, or C(O)—O—R, wherein Ris H, a straight or branched C1 to C6 alkyl, CHCH, or CH(CH)n, and wherein n is an integer from 2 to 5;'}{'sub': 2', '6', '7', '8', '7', '8', '2', '6', '5', '7', '8', '2, 'C(O)NH, C(O)NHRor C(O)NRRwherein Rand Rindependently =C1 to C6 alkyl (straight chain or branched), CHCH, aryl, or Rand Rtogether =(CH)m, and wherein m is an integer from 3 to 5; or'}{'sub': 3', '2', '6', '5, 'OH, OCH, or OCHCH,'}or a pharmaceutically acceptable salt thereof.371. A compound of claim , wherein R=H and R=aryl.396. The compound of claim , wherein R=R=CH , or a pharmaceutically acceptable salt thereof.407. The compound of claim , wherein Ris{'sub': 2', '2', '6', '5', '3', '6', '5', '3', '2', '3', '2', '4', '9', '6', '5, 'a straight C5 to C6 alkyl, branched C3 to C6 alkyl, or CH(CH)n, wherein n is an integer from 3 to 5; CHSCH; CH═CHC(O)CH; CH═CHC(O)CH; CH═CHC(O)—O—CH; CH═CHC(O)—O—CH; CH═CHC(O)—O—CH(CH); CH═CHC(O)—O—CH; or CH═CHC(O)—O—CH, or'}a pharmaceutically acceptable salt thereof. This application is a Continuation Application of U.S. patent application Ser. No. 16/723,630 filed Dec. 20, 2019 which is a Divisional Application of U.S. patent application Ser. No. 15/866,924 filed Jan. 1, 2018, U.S. Pat. No. 10,556,853 issued Feb. 11, 2020 which claims priority from provisional application No. 62/444,474 filed Jan. 10, 2017, the entire contents of each are hereby incorporated by reference herein.The present invention relates to compounds with anti-convulsant and pain activity. These ...

Antimicrobial compounds

Disclosed herein are compounds for use as antimicrobial agents, having a structure of formula (I):

COMPOSITIONS AND METHODS FOR MODIFICATION OF BIOMOLECULES

The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids). 9. A compound of any one of Formulas III-XXII.10. A method for chemoselective modification of a target molecule comprising an azide , the method comprising reacting an azide of a target molecule with a modified cycloalkyne of any one of Formulas III-XXII , wherein said reacting produces a conjugate between the azide of the target molecule and the modified cycloalkyne.11. The method of claim 10 , wherein the target molecule is a sugar.12. The method of claim 11 , wherein the sugar is a substrate of sialic acid biosynthesis.13. The method of claim 11 , wherein the sugar is mannosamine or acetylated mannosamine.14. The method of claim 10 , wherein the target molecule is an amino acid.15. The method of claim 10 , wherein said reacting is performed in aqueous conditions.16. The method of claim 10 , wherein said reacting is performed under physiological conditions.17. The method of claim 10 , wherein the target molecule comprising the azide is expressed on a cell surface.18. A method for synthetically modifying a cellular component claim 10 , the method comprising:introducing an azide moiety into a cellular component, thereby generating an azide-modified cellular component; andcontacting the cell comprising the azide-modified cellular component with a reactive partner comprising a modified cycloalkyne of any ...

COMPOSITIONS AND METHODS FOR IMMUNE MODULATION AND TREATMENT OF CANCER

The disclosure relates to rexinoids, including compounds of the Formula (I) and (II) or a pharmaceutically acceptable salt, polymorph, prodrug, solvate or clathrate thereof. These rexinoids are useful for increasing PD-L1 in vivo, for treatment of cancer, and for inhibiting the onset of cancer. 3. A pharmaceutical composition comprising one or more of the compounds of claim 1 , or a pharmaceutically acceptable salt claim 1 , polymorph claim 1 , prodrug claim 1 , solvate or clathrate thereof claim 1 , and a pharmaceutically acceptable carrier.4. (canceled)5. (canceled)6. The composition of claim 3 , further comprising one or more types of anti-PD-L1 antibodies or one or more chemotherapeutic agents.7. (canceled)8. (canceled)10. The composition of claim 3 , comprisingan amount of one or more of the compounds effective to reduce tumor weight in a subject by at least 2%, or 5%, or 10%, or 15%, or 20%, or 25%, or 30%, or 35%, or 40%, or 45%, or 50%, or 55%, or 60%, or 65%, or %70, or 80%, or 90%, 95%, or 97%, or 99%, or 120%, or 150%, or 200%, or 250%, or 300%, or any numerical percentage between 5% and 300% compared to a control;an amount of one or more of the compounds effective to increase PD-L1 levels in a subject for in a sample of cells from the subject) by at least 2%, or 5%, or 10%, or 15%, or 20%, or 25%, or 30%, or 35%, or 40%, or 45% or 50%, or 55%, or 60%, or 65% or %70, or 80%, or 90%, 95%, or 97%, or 99%, or 120%; or 150%, or 200%, or 250%, or 300%, or any numerical percentage between 5% and 300% compared to a control;an amount of one or more of the compounds effective to increase PD-L1 levels in a subject (or in a sample of cells from the subject) by at least 2-fold, or 3-fold, or 4-fold, or 5-fold, or 7-fold, or 10-fold compared to a control;an amount of one or more of the compounds effective to reduce PD-1, CD206; pSTAT1, and/or FOXP3 expression in a subject (or in a sample of cells from the subject) by at least 2%, or 5%, or 10%, or 15%, or 20%, or 75%, ...

New bi-aromatic propynyl compounds, pharmaceutical and cosmetic compositions containing them and uses thereof

The invention relates to new compounds of the general formula (I): as well as the use thereof in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, in particular), or in the use of cosmetic compositions.

EBNA1 INHIBITORS AND THEIR METHOD OF USE

Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection. 4. The method of claim 1 , wherein the compound is at least one selected from the group consisting of:3-{2-[3-(methylsulfamoyl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indol-3-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(3-methanesulfonamidophenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-[2-(3-sulfamoylphenyl)ethynyl]benzoic acid;3-[2-(3-carbamoylphenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-6-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(2-hydroxypyridin-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indazol-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-{2-[3-(3,3-dimethyl-2-oxoazetidin-1-yl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{3-[(2-carboxy-2,2-dimethylethyl)amino]phenyl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyrazin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-5-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-(2-{1H-pyrrolo[2,3-b]pyridin-5-yl}ethynyl)benzoic acid;3-[2-(1-methyl-1H-indol-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-methyl-1H-indol-5-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-benzothiophen-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indol-7-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-{2-[2-( ...

Synthetic retinoids for use in rar mediated conditions

There are described novel compounds of formula I: in which R 1 , R 2 , R 3 , R 4 , R 5 , X 1 and X 2 are each as herein defined, for use in the treatment or alleviation of an RAR miated condition: and methods related thereto.

Ndm inhibitor

An objective of the present invention is to provide a novel NDM (New Delhi metallo-β-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of β-lactam antibiotics that have been inactivated as a result of decomposition by NDM. According to the present invention, there is provided an NDM inhibitor contains a compound represented by general formula (I):

Compounds that Modulate Store Operated Calcium Channels

Store operated calcium channel modulating compounds, and methods for using the same, are provided. These compounds and methods find use in a variety of applications in which modulation of store operated calcium channels is desired. 1. A method for modulating a store operated calcium channel in a cell , the method comprising:contacting the cell with a store operated calcium channel modulating effective amount of a compound selected from the group consisting of a chromenone, an octahydro-naphthalene, a dibenzo-diheteropin-1 1-one, a 3a,7a-dihydro-4H-benzofuran-5-one, a tetrahydro-furo[3,4-c]furan-1-one and a 3,3a,4,5-tetrahydro-2H-benzofuran-6-one.22. A pharmaceutical composition comprising a store operated calcium channel modulating compound selected from the group consisting of a chromenone , an octahydro-naphthalene , a dibenzo-diheteropin-11-one , a dihydro-benzofuran-5-one , a tetrahydro-furofuran-1-one and a tetrahydro-benzofuran-6-one. This invention was made with Government support under grants R01 NS048564 and R01 GM45374 awarded by the National Institutes of Health. The Government has certain rights in this invention.Calcium has an important role in many cellular functions such as the transduction of signals into and within cells. Processes that depend on calcium are involved in cellular responses to growth factors, neurotransmitters, hormones and other signal molecules. Intracellular calcium concentrations are tightly controlled by a variety of pumps and channels. As calcium is the most abundant second messenger in cell signaling, such tight control is necessary to produce specific calcium mediated responses.Store Operated Calcium Entry, which involves Calcium Release-Activated Calcium (CRAC) channels and their currents (I), is one of many ways of regulating intracellular calcium levels. Store-operated calcium channels (SOCs) comprise the major receptor-activated calcium entry pathway in non-excitable mammalian cells and play important roles in the control ...

DESIGN, SYNTHESIS AND CHARACTERIZATION OF METAL ORGANIC FRAMEWORKS

A molecular building block composition can include a metal ion component; and a ligand component including a core including at least one functional group associated with the metal ion component and the core. 120-. (canceled)21. A metal organic framework (MOF) comprising:a plurality of polynuclear metal clusters, wherein at least one of the polynuclear metal clusters includes a rare earth metal; anda plurality of polydentate ligands each linking two or more of the polynuclear metal clusters;wherein the MOF has a ftw or ftw-a topology.22. The MOF of claim 21 , wherein the polydentate ligand is a square or quadrangular ligand.23. The MOF of claim 22 , wherein the polydentate ligand is selected from the group consisting of 3 claim 22 ,3″ claim 22 ,5 claim 22 ,5″-tetrakis(4-carboxyphenyl)-p-terphenyl claim 22 , 3′ claim 22 ,3″ claim 22 ,5′ claim 22 ,5″-tetrakis(4-carboxyphenyl)-1 claim 22 ,4-diphenylnaphthalene claim 22 , 3′ claim 22 ,3″ claim 22 ,5′ claim 22 ,5″-tetrakis(4-carboxyphenyl)-9 claim 22 ,10-diphenylanthracene claim 22 , 3 claim 22 ,3″ claim 22 ,5 claim 22 ,5″-tetra-2-(4-carboxyphenyl)ethynyl-p-terphenyl claim 22 , and 4 claim 22 ,4′ claim 22 ,4″ claim 22 ,4′″-((benzene-1 claim 22 ,2 claim 22 ,4 claim 22 ,5-tetrayltetrakis(methylene))tetrakis(oxy))tetrabenzoic acid.24. The MOF of claim 21 , wherein the polynuclear cluster is a cuboctahedral 12-c molecular building block (MBB).25. The MOF of claim 21 , wherein the rare earth metal is selected from yttrium claim 21 , ytterbium claim 21 , terbium claim 21 , and combinations thereof.26. The MOF of claim 21 , wherein the MOF has a (1 claim 21 , 12) or (4 claim 21 , 12) connectivity.27. A method of making of metal organic framework (MOF) having a ftw or ftw-a topology comprising:contacting a rare earth metal ion component and a polydentate ligand to form a mixture;allowing the mixture to react whereby a crystalline metal organic framework with a ftw or ftw-a topology forms.28. The method of claim 27 , wherein the ...

ANTICONVULSANT COMPOUNDS

The present application relates to compounds and methods for reducing the severity of convulsant activity or epileptic seizures, or for the treatment of chronic or acute pain. 120-. (canceled)22. The method of claim 21 , wherein R=R=CH.23. The method of claim 22 , wherein R=C1 to C6 alkyl (straight chain or branched) claim 22 , CH(CH)n claim 22 , wherein n=3-5 claim 22 , or aryl;{'sub': 2', '6', '5', '2', '2', '6', '5, 'CHSCH, or CHSOCH;'}{'sub': 6', '5', '6', '5', '2', '6', '5, 'S—CH, S(O)CH, or SOCH; or'}{'sub': 3', '6', '5', '3', '2', '5', '3', '2', '4', '9', '6', '5, 'b': '13', 'CH═CHC(O)CH, CH═CHC(O)CH, CH═CHC(O)—O—CH, CH═CHC(O)—O—CH, CH═CHC(O) O—CH(CH), CH═CHC(O)—O—CH, or CH═CHC(O)—O—CH.'} This application is a Divisional Application of U.S. patent application Ser. No. 15/866,924 filed Jan. 1, 2018 which claims priority from provisional application No. 62/444,474 filed Jan. 10, 2017, the entire contents of each are hereby incorporated by reference herein.The present invention relates to compounds with anti-convulsant and pain activity. These compounds are useful in modulating voltage-gated sodium channel activity and are thus useful in the treatment of epilepsy and chronic or acute pain.Anti-convulsant compounds are presently in wide use in the treatment of a variety of conditions and diseases, including epilepsy. Epilepsy is a neurological condition which affects the nervous system and causes affected individuals to suffer from seizures. These seizures are caused by in appropriate electrical communication between neurons in the brain and can be conceptualized as brain activity that is inappropriately synchronous. Seizures are often seen in electro encephalograms (EEGs) as high amplitude neural discharges that occur across brain regions. This brain activity is accompanied by behavioral disturbances that include loss of balance, jerking muscle movement, visual disturbances, and loss of consciousness. It is estimated that about 0.5% of the world's population has ...

ANTIMICROBIAL COMPOUNDS

A compound for use as an antimicrobial having a formula (A). 116-. (canceled)18. The compound of claim 17 , wherein each of W claim 17 , W claim 17 , W claim 17 , and Wis a Calkene.19. The compound of claim 18 , wherein the Calkene is in an E configuration.20. The compound of claim 18 , wherein the Calkene is in a Z configuration. The present invention relates to novel aryl compounds. More particularly the present invention relates to novel aryl compounds and their use as antimicrobials to treat bacterial infections or diseases.Compounds with antimicrobial properties have attracted great interest in recent times as a result of an increase in the prevalence of infections caused by Gram-positive bacteria, resulting in serious or fatal diseases. Furthermore, the regular use of broad spectrum antibiotic formulas has led to the increased occurrence of bacterial strains resistant to some antimicrobial formulations.Novel antimicrobial compounds have the potential to be highly effective against these types of treatment-resistant bacteria. The pathogens, having not previously been exposed to the antimicrobial formulation, may have little to no resistance to the treatment.Those skilled in the art will appreciate that the invention described herein is susceptible to variations and modifications other than those specifically described. It is to be understood that the invention includes all such variation and modifications. The invention also includes all of the steps, features, compositions and compounds referred to or indicated in the specification, individually or collectively and any and all combinations or any two or more of the steps or features.The present invention is not to be limited in scope by the specific embodiments described herein, which are intended for the purpose of exemplification only. Functionally equivalent products, compositions and methods are clearly within the scope of the invention as described herein.The entire disclosures of all publications ( ...

EBNA1 INHIBITORS AND THEIR METHOD OF USE

Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection. 122-. (canceled)25. The compound of claim 23 , wherein the compound is selected from the group consisting of:3-{2-[3-(methylsulfamoyl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indol-3-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(3-methanesulfonamidophenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-[2-(3-sulfamoylphenyl)ethynyl]benzoic acid;3-[2-(3-carbamoylphenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-6-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(2-hydroxypyridin-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indazol-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-{2-[3-(3,3-dimethyl-2-oxoazetidin-1-yl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{3-[(2-carboxy-2,2-dimethylethyl)amino]phenyl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyrazin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-5-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-(2-{1H-pyrrolo[2,3-b]pyridin-5-yl}ethynyl)benzoic acid;3-[2-(1-methyl-1H-indol-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-methyl-1H-indol-5-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-benzothiophen-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indol-7-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-{2-[2-( ...

Anticonvulsant compounds

The present application relates to compounds and methods for reducing the severity of convulsant activity or epileptic seizures, or for the treatment of chronic or acute pain.

Metal-organic frameworks

The present invention relates to compounds capable of forming metal-organic frameworks (MOFs), particularly f-block metal MOFs which selectively sorb one component (e.g. para-xylene) from a mixture of components (e.g. m-/p-xylene mixture). The invention also relates to methods of producing and using said compounds.

Treatment of neurodegenerative diseases

The present disclosure relates to compounds to be used in a low dose in treatment of neurodegenerative diseases or disorders. It also relates to methods for treatment of a neurodegenerative diseases or disorders.

DESIGN, SYNTHESIS AND CHARACTERIZATION OF METAL ORGANIC FRAMEWORKS

A molecular building block composition can include a metal ion component; and a ligand component including a core including at least one functional group associated with the metal ion component and the core. 1. A molecular building block composition comprising:a metal moiety including at least seven metal ions, anda plurality of fluorinated precursor moieties.2. The molecular building block composition of claim 1 , wherein the metal moiety comprises nine metal ions.3. The molecular building block composition of claim 2 , wherein the metal moiety is a nonanuclear metal cluster coordinated by at least one polytopic ligand.4. The molecular building block composition of claim 3 , wherein the at least one polytopic ligand is selected from the group consisting of 1 claim 3 ,3 claim 3 ,5-benzene(tris)benzoate claim 3 , biphenyl-3 claim 3 ,4 claim 3 ,5-tricarboxylic acid claim 3 , 5-(4-carboxybenzyloxy)-isophthalic acid claim 3 , 4 claim 3 ,4′-(pyridine-2 claim 3 ,6-diyl)dibenzoic acid claim 3 , carbazole-3 claim 3 ,6-dicarboxylic acid claim 3 , 5′ claim 3 ,5″″-((5-((4-(3 claim 3 ,6-dicarboxy-9H-carbazol-9-yl)phenyl)ethynyl)-1 claim 3 ,3-phenylene)bis(ethyne-2 claim 3 ,1-iyl))bis([1 claim 3 ,1′:3′ claim 3 ,1″-terphenyl]-4 claim 3 ,4″-dicarboxylic acid) claim 3 , 9-(4-carboxyphenyl)-9Hcarbazole-3 claim 3 ,6-dicarboxylic acid claim 3 , 2-bromoterephthalic acid claim 3 , aminoterephthalic acid claim 3 , 2 claim 3 ,5-diaminoterephthalic acid claim 3 , 2 claim 3 ,5-dihydroxyterephthalic acid claim 3 , 2-nitroterephthalic acid claim 3 , 2 claim 3 ,6-naphthalene dicarboxylic acid claim 3 , 4 claim 3 ,4′-dihydroxybiphenyl-3 claim 3 ,3′-dicarboxylic acid claim 3 , 4 claim 3 ,4′-biphenyldicarboxylic acid claim 3 , 3-chlorobiphenyl-4 claim 3 ,4′-dicarboxylic acid claim 3 , ethine dibenzoic acid claim 3 , 1 claim 3 ,4-benzene dicarboxylic acid claim 3 , oxybis(benzoic) acid claim 3 , sulfonyl dibenzoic acid claim 3 , benzophenone dicarboxylic acid claim 3 , 4 claim 3 ,4′-( ...

EBNA1 INHIBITORS AND THEIR METHOD OF USE

The invention provides EBNA1 inhibitors, and pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by EBNA1 activity such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The compounds and compositions of the invention are further useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. The compounds and compositions of the invention are further useful for the treatment of diseases caused by lytic EBV infection. 35-. (canceled)79-. (canceled)1113-. (canceled)1517-. (canceled)18. The compound of claim 1 , wherein the compound is at least one selected from the group consisting of:3-{2-[3-(methylsulfamoyl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indol-3-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(3-methanesulfonamidophenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-[2-(3-sulfamoylphenyl)ethynyl]benzoic acid;3-[2-(3-carbamoylphenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-6-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(2-hydroxypyridin-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indazol-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-{2-[3-(3,3-dimethyl-2-oxoazetidin-1-yl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{3-[(2-carboxy-2,2-dimethylethyl)amino]phenyl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyrazin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-5-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-(2-{1H-pyrrolo[2,3-b]pyridin-5-yl}ethynyl)benzoic acid;3-[2-(1-methyl-1H-indol-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-methyl-1H-indol-5-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-benzothiophen-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-( ...

ANTIMICROBIAL COMPOUNDS

Disclosed herein are compounds for use as antimicrobial agents, having a structure of formula (I): 116.-. (canceled)18. The method of claim 17 , wherein at least one of Rand Rare chosen from the list comprising: COOH claim 17 , COOCH claim 17 , COOCHCH claim 17 , COOCHCHCHor COOCHCHCHCH. and wherein Rand Rcannot be both COOH.19. The method according to claim 17 , wherein at least one of Rand Rare chosen from the list comprising: COOCH claim 17 , COOCHCH claim 17 , COOCHCHCHor COOCHCHCHCH.20. The method according to claim 17 , wherein at least one of Rand Rare chosen from the list comprising: COOCH claim 17 , COOCHCH.21. The method according to claim 17 , wherein both Rand Rare chosen from the list comprising: COOCH claim 17 , COOCHCH.22. The method according to claim 17 , wherein both Rand Rare COOCH.23. The method according to claim 17 , wherein Rand Rare independently: O-alkyl claim 17 , or C-alkenyl.24. The method according to claim 17 , wherein Rand Rare: C-alkenyl. The present invention relates to novel aryl compounds. More particularly the present invention relates to novel aryl compounds and their use as antimicrobials to treat bacterial infections or diseases.Compounds with antimicrobial properties have attracted great interest in recent times as a result of an increase in the prevalence of infections caused by Gram-positive bacteria, resulting in serious or fatal diseases. Furthermore, the regular use of broad spectrum antibiotic formulas has led to the increased occurrence of bacterial strains resistant to some antimicrobial formulations.Novel antimicrobial compounds have the potential to be highly effective against these types of treatment-resistant bacteria. The pathogens, having not previously been exposed to the antimicrobial formulation, may have little to no resistance to the treatment.Those skilled in the art will appreciate that the invention described herein is susceptible to variations and modifications other than those specifically described. It ...

THERAPEUTIC PROSTAGLANDIN RECEPTOR AGONISTS

Described herein are compounds which can be used in topical liquids, creams, or other dosage forms such as solids, for reducing intraocular pressure, treating glaucoma, growing hair, treating wounds, or other medical and/or cosmetic uses.

INHIBITORS OF SOX18 PROTEIN ACTIVITY FOR TREATING ANGIOGENESIS-AND/OR LYMPHANGIOGENESIS-RELATED DISEASES

Disclosed are compounds of a formula provided herein that show efficacy in the inhibition of SOX18 protein activity, and in particular with respect to the ability of SOX18 to bind DNA and/or particular protein partners. Further, methods of treating angiogenesis- and/or lymphangiogenesis-related diseases, disorders or conditions, such as cancer metastasis and vascular cancers, are provided herein. 2. The compound of claim 1 , wherein Ris selected from the group consisting of OH and OMe.4. The compound of any one of the preceding claims claim 1 , wherein Ris selected from the group consisting of H claim 1 , OH claim 1 , OMe claim 1 , Cl and Me.5. The compound of any one of the preceding claims claim 1 , wherein Ris selected from the group consisting of H claim 1 , OH and OMe.6. The compound of any one of the preceding claims claim 1 , wherein Rand Rare H.7. The compound of any one of the preceding claims claim 1 , wherein L is a linker selected from C-Calkyl claim 1 , C-Calkenyl and C-Calkoxyalkyl.10. The compound of any one of the preceding claims claim 1 , wherein the SOX18 activity includes contacting and/or binding to a DNA sequence and/or a protein.11. The compound of claim 10 , wherein the protein is selected from the list consisting of SOX7 claim 10 , RBPJ claim 10 , XRCC5 claim 10 , SOX18 claim 10 , ILF3 claim 10 , DDX17 and any combination thereof.12. A pharmaceutical composition comprising a compound of any one of the preceding claims claim 10 , or a pharmaceutically acceptable salt claim 10 , solvate or prodrug thereof claim 10 , and a pharmaceutically acceptable carrier claim 10 , diluent and/or excipient.13. A method of treatment or prevention of an angiogenesis- and/or lymphangiogenesis-related disease claim 10 , disorder or condition in a subject including the step of administering to the subject an effective amount of the compound of any one of to claim 10 , or a pharmaceutically effective salt claim 10 , solvate or prodrug thereof claim 10 , or the ...

LUMINESCENT NANOCRYSTAL COMPLEX

“Object” A problem to be solved by the present invention is to provide a luminescent nanocrystal complex that tends to disperse orderly in a polymer matrix and is superior in dispersibility in structurally mesogenic crosslinkable polymer matrices. “Solution” The present invention is a luminescent nanocrystal complex that contains luminescent nanocrystals and a surface-modifying compound that modifies the surface of the luminescent nanocrystals. The surface-modifying compound has a mesogenic backbone and a group that binds to the surface of the luminescent nanocrystals. 1. A luminescent nanocrystal complex comprising luminescent nanocrystals and a surface-modifying compound modifying a surface of the luminescent nanocrystals , whereinthe surface-modifying compound has a mesogenic group and at least one group that binds to the surface of the luminescent nanocrystals.2. The luminescent nanocrystal complex according to claim 1 , wherein the group of the surface-modifying compound that binds to the surface of the luminescent nanocrystals contains one or two or more types of atoms selected from the group consisting of sulfur claim 1 , nitrogen claim 1 , oxygen claim 1 , and phosphorus.3. The luminescent nanocrystal complex according to claim 1 , wherein the group of the surface-modifying compound that binds to the surface of the luminescent nanocrystals is any one or more of hydroxy claim 1 , thiol claim 1 , carboxylic acid claim 1 , amine claim 1 , sulfonic acid claim 1 , phosphine claim 1 , phosphine oxide claim 1 , and thioether.5. The luminescent nanocrystal complex according to claim 4 , wherein MGin general formula (i) is a divalent organic group incorporating a cyclic group optionally with a hydrogen atom in the cyclic group substituted with general formula (i-3):{'br': None, 'sup': i2', 'i2', 'i3, 'sub': 'ni2', 'R-(MGSp)-\u2003\u2003(i-3)'}{'sup': 'i2', '(In general formula (i-3) above, MGrepresents a mesogenic group,'}{'sup': 'i3', 'SPrepresents a single bond or ...

Process for preparing 2-aryl-substituted indenes

A process is disclosed for preparing 2-aryl-substituted indenes by reacting an indene with an arene compound substituted with an halogen atom, preferably a iodine atom, or with an organosulphonate group, said reaction being carried out in a basic medium in the presence of a palladium catalyst. The compounds obtainable by this process can be used to prepare metallocene compounds with transition metals such as titanium, zirconium or hafnium, which are useful as catalyst components in the polymerization of olefins.

Salt and photoresist composition containing the same

하기 화학식 (I-Pa)로 표시되는 염: 상기 식에서, X Pa 는 단일 결합 또는 C1-C4 알킬렌기를 나타내고, R Pa 는 단일 결합, C4-C36의 2가의 지환식 탄화수소 기 또는 C6-C36의 2가의 방향족 탄화수소 기를 나타내며, 2가의 지환식 탄화수소 기 내의 1 이상의 메틸렌기가 -O- 또는 -CO-로 치환될 수 있고, Y Pa 는 중합 가능 기를 나타내며, Z Pa+ 는 유기 양이온을 나타낸다. A salt represented by the following formula (I-Pa): In this formula, X Pa represents a single bond or a C1-C4 alkylene group, R Pa represents a single bond, a divalent alicyclic hydrocarbon group of C4-C36 or a divalent aromatic hydrocarbon group of C6-C36, and one or more methylene groups in the divalent alicyclic hydrocarbon group may be substituted with -O- or -CO- However, Y Pa represents a polymerizable group, Z Pa + represents an organic cation.

Dimer-Selective RXR Modulators and How to Use Them

본 발명은 RXR 호모다이머 및/또는 RXR 헤테로다이머와 관련한 작용제, 부분작용제 및/또는 길항제 활성을 갖는 다이머-선택적 RXR 변조제 화합물에 관한 것이다. 본 발명은 또한 이러한 다이머-선택적 RXR 변조제 화합물을 함유하는 약제학적 조성물 및 그의 치료학적 사용방법에 관한 것이다. The present invention relates to dimer-selective RXR modulator compounds having agonist, partial agonist and / or antagonist activity in connection with RXR homodimers and / or RXR heterodimers. The present invention also relates to pharmaceutical compositions containing such dimer-selective RXR modulator compounds and methods of therapeutic use thereof.

Stilbene derivative

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Novel biaromatic propynyl compounds, pharmaceutical and cosmetic compositions containing same, and uses thereof

The invention relates to novel compounds of general formula (I), as well as the use of said compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmologic disorders, in particular), or in cosmetic compositions.

NEW BIAROMATIC COMPOUNDS OF PROPINYL, PHARMACEUTICAL AND COSMETIC COMPOSITIONS, THEIR CONTAINING, AND THEIR APPLICATION

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2018 131 460 A (51) МПК A61K 8/368 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2018131460, 03.02.2017 (71) Заявитель(и): ГАЛДЕРМА РЕСЕРЧ ЭНД ДЕВЕЛОПМЕНТ (FR) Приоритет(ы): (30) Конвенционный приоритет: 03.02.2016 US 62/290,707 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 03.09.2018 R U (43) Дата публикации заявки: 04.03.2020 Бюл. № 7 (72) Автор(ы): ПОРТАЛЬ Тибо (FR) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2017/134513 (10.08.2017) (54) НОВЫЕ БИАРОМАТИЧЕСКИЕ СОЕДИНЕНИЯ ПРОПИНИЛА, ФАРМАЦЕВТИЧЕСКИЕ И КОСМЕТИЧЕСКИЕ КОМПОЗИЦИИ, ИХ СОДЕРЖАЩИЕ, И ИХ ПРИМЕНЕНИЕ (57) Формула изобретения 1. Биароматические соединения пропинила общей формулы (I): A где: Аr представляет собой радикал, выбранный из радикалов формул (а) или (b) ниже: R U 2 0 1 8 1 3 1 4 6 0 A Адрес для переписки: 125047, Москва, ул. Лесная, 7, БЦ "Белые Сады", АО "Дентонс Юроп" 2 0 1 8 1 3 1 4 6 0 IB 2017/000075 (03.02.2017) где R5 имеет значения, приведенные ниже, Стр.: 1 R U (d) радикал -OR8, где R8 имеет значения, приведенные ниже, R8 представляет собой атом водорода, линейный или разветвленный алкил, имеющий 1-20 атомов углерода, алкенил, моно- или полигидроксиалкил, необязательно замещенный арил или аралкил, или остаток сахара, или аминокислотный остаток, или пептидный остаток, R9 представляет собой низший алкил или линейный или разветвленный алкил, имеющий 1-20 атомов углерода, R и R представляют собой атом водорода, низший алкил, моно- или полигидроксиалкил, необязательно замещенный арил или аминокислотный остаток, или пептидный остаток, или остаток сахара, или вместе образуют гетероцикл, t - целое число, равное 0, 1 или 2, а также их соли и оптические или геометрические изомеры. 2. Соединения по п. 1, отличающиеся тем, что они представлены в виде солей щелочных или щелочноземельных металлов, цинка или органического амина. 3. Соединения по п. 1 или 2, отличающиеся тем, что низший ...

Salt and photoresist composition containing the same

A salt represented by the formula (I-Pa): wherein X pa represents a single bond or a C1-C4 alkylene group, R pa represents a single bond, a C4-C36 divalent alicyclic hydrocarbon group or a C6-C36 divalent aromatic hydrocarbon group, and one or more methylene groups in the divalent alicyclic hydrocarbon group can be replaced by —O— or —CO—, Y pa represents a polymerizable group, and Z pa+ represents an organic cation.

Salt and photoresist composition containing the same

A salt represented by the formula (I-Pa): wherein X pa represents a single bond or a C1-C4 alkylene group, R pa represents a single bond, a C4-C36 divalent alicyclic hydrocarbon group or a C6-C36 divalent aromatic hydrocarbon group, and one or more methylene groups in the divalent alicyclic hydrocarbon group can be replaced by —O— or —CO—, Y pa represents a polymerizable group, and Z pa+ represents an organic cation.

Alkyl, alkenyl and alkynyl Chrysamine G derivatives for the antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition

Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.

Compounds having selectivity for retinoid x receptors

Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

BIAROMATIC PROPYNYL COMPOUNDS

RETINOID-TYPE AROMATIC POLYCYCLIC DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR USE FOR THE MANUFACTURE OF PHARMACEUTICAL AND COSMETIC COMPOSITIONS

New dihydronaphthalenyl-substituted carboxylic acid derivatives are retinoic acid receptor antagonists useful e.g. for treating dermatological or ophthalmological disorders or precancerous lesions

8,8-Dimethyl-5-phenyl-7,8-dihydro-naphthalen-2-yl-substituted carboxylic acid derivatives (I) are new. Dihydronaphthalene derivatives of formula (I) and their optical isomers and acid or base addition salts are new. A = CH2, CH(OH), CO, C(=NOH), S or Se; B' = (E)-C6H4-CH=CH-, -Cequivalent toC-C(CH3)=CH-, -Cequivalent toC-Ar'-, (E)-CH=CH-Ar', naphthalene-2,6-diyl or -CONH-Ar'-; Ar' = pyridine-2,5-diyl, pyridine-5,2-diyl or R3-substituted p-phenylene; R = OH, OR4, NHR5 or NR5R6; R2 = H, F, Cl, Br, 1-5C alkyl, CF3, OR7, NHR8, NR8R9, 2-naphthyl, 2-, 3- or 4-pyridyl, 2-thienyl, CH2OR10, CH2NR11R12 or phenyl (optionally substituted by one or more of F, Me, Et, isopropyl, tert. butyl or CF3); R3 = H, F, Cl, OH, OR13, CF3 or NR14R15; R4, R6 = 1-4C alkyl; R5 = H, OH or 1-4C alkyl; R7 = H, 1-6C alkyl, CH2OR16 or benzyl (optionally substituted by one or more of F, Me, Et, isopropyl, tert. butyl or CF3); R8, R9, R11, R14, R15 = H, 1-4C alkyl, COR17 or COOR17; R10 = 1-4C alkyl, benzyl or phenyl; R13 = CH3, C2H5 or COCH3; R16 = CH3, C2H5 or CH2CH2OCH3; and R17 = H, OH or 1-4C alkyl. Provided that compounds (I; R2 = CH3; A = CO; B = (E)-CH=CH-pC6H4-; Ar' = unsubstituted phenylene) are excluded.

UNSATURATED DERIVATIVES IN POSITION -4 OF 6-TERT-BUTYL-1,1- DIMETHYLINDANE AND THEIR USE IN HUMAN OR VETERINARY MEDICINE AND IN COSMETICS

CYCLOALIPHATIC UNSATURATED DERIVATIVES, THEIR PREPARATION METHODS AND THEIR USE IN THERAPEUTICS AND COSMETICS

Keto-naphthalene derivatives, process for their preparation and their application in the pharmaceutical and cosmetic fields

Keto-naphthalene derivatives, characterised in that they correspond to the following general formula: in which: R1-R4 represent -H or lower alkyl, or R1 and R3 together represent methylene or dimethylene, and R5 represents lower alkyl, -CH2OH or -CO-R6, R6 being especially -H, -OH, alkoxy, amino, dialkylamino and the like, their preparation and their application as therapeutic and/or cosmetic agents especially in the treatment of dermatological illnesses connected to keratinisation disorders.

NOVEL BAPHYCLIC NAPHTHALENIC DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR USE IN HUMAN AND VETERINARY MEDICINE AND IN COSMETICS.

Dimer-selective RXR modulators and methods for their use

Dimer-selective RXR modulator compounds having agonist, partial agonist and/or antagonist activity in the context of an RXR homodimer and/or RXR heterodimers are provided. Also provided are pharmaceutical compositions incorporating such dimer-selective RXR modulator compounds and methods for their therapeutic use.

Diaromatic Propynyl or Dienyl Compounds

본 발명은 하기 화학식 Ⅰ 을 갖는 신규 프로피닐 또는 디에닐 이방향족 화합물 뿐만 아니라, 의학 또는 수의학 (특히, 피부, 류마티스성, 호흡, 심장 및 안과학적 질병) 에 사용하기 위한 약학적 조성물 또는 선택적으로 미용 조성물 내에서 상기 화합물의 용도에 관한 것이다: [화학식 Ⅰ]

Diaromatic propynyl or dienyl compounds

본 발명은 하기 화학식 Ⅰ 을 갖는 신규 프로피닐 또는 디에닐 이방향족 화합물 뿐만 아니라, 의학 또는 수의학 (특히, 피부, 류마티스성, 호흡, 심장 및 안과학적 질병) 에 사용하기 위한 약학적 조성물 또는 선택적으로 미용 조성물 내에서 상기 화합물의 용도에 관한 것이다: The present invention relates to novel propynyl or dietenyl diaromatic compounds having the general formula (I) as well as pharmaceutical compositions or optionally cosmetics for use in medicine or veterinary medicine (especially dermatological, rheumatic, respiratory, heart and ophthalmological diseases) Relates to the use of said compound in a composition: [화학식 Ⅰ] [Formula I]

Benzocycloheptene derivatives

Abstract Compounds of the general formula I wherein R1 signifies hydroxy, lower-alkoxy, amino, mono- or di-lower-alkylamino: R2 signifies hydrogen, alkyl, alkoxy or halogen; R3 , R4 , R5 , R6 , R11 and R12 each independently signify hydrogen or lower-alkyl; R3 and R together signify a methylene or hydroxy-methylene group; R7, R8, R9 and R10 signify hydrogen or lower--alkyl; R11 and R12 together signify an oxo group or spiro--cyclo-lower alkyl; or R11 signifies hydrogen and R12 signifies hydroxy or acetoxy: and one of the residues R13 and R14 signifies hydrogen and the other signifies lower-alkyl or trifluoromethyl, as well as physiologically compatible salts of carboxylic acids of formula I can be used as medicaments, especially for the treatment of neoplasms, acne and psoriasis. The novel compounds can be manufactured by the synthesis of the C(R13)=C(R14) double bond according to Wittig from a corresponding bicyclic component and a corresponding monocyclic component and optional subsequent transform-ation of functional groups.

Compounds with Selectivity to Retinoid X Receptors

본 발명은 레티노산 수용체(RAR)의 아강의 구성원에 우선하여, 레티노이드 X 수용체(RXR)의 아강의 구성원에 대한 선택 활성을 갖는, 화합물, 조성물, 및 레티노이드 유사 화합물을 사용하여 레티노이드 X 수용체에 의해 매개되는 반응을 조절하는 방법에 관한 것이다. 이러한 화합물의 예로는 비시클릭 벤질, 피리디닐, 티오펜, 푸라닐 및 피롤 유도체가 있다. 개시된 방법은 레티노이드 X 수용체에 의해 선택적으로 매개되는 반응을 조절하기 위한 화합물을 사용한다. The present invention is directed to retinoid X receptors using compounds, compositions, and retinoid-like compounds that have preferential activity over members of the subclasses of retinoid X receptors (RAR), prior to members of the subclasses of retinoic acid receptors (RAR). It relates to a method of controlling the mediated response. Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl and pyrrole derivatives. The disclosed method uses compounds to modulate a response selectively mediated by the retinoid X receptor.

Treating niddm with rxr agonists

This invention relates to methods and compositions for the treatment of noninsulin-dependent diabetes mellitus using an RXR agonist alone or in combination with a PPAR.gamma. agonist such as a thiazolidinedione compound.

Compositions and methods for modification of biomolecules

The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Process for preparing bifunctional Z-stilbene compounds, new bifunctional Z-stilbene compounds and their use for preparing polymers

New selective retinoid agonists

This invention relates to new RAR selective retinoid agonists of formula (1) wherein the symbols are as defined in the specification to their pharmaceutically acceptable salts, individual isomers or to a racemic or non-racemic mixture; to pharmaceutical compositions containing them, and to methods for their use as therapeutic agents.

Benzocycloheptene derivatives and their use as a medicament

Compounds of the general formula …<IMAGE>… in which… R<1> denotes hydroxyl, lower alkoxy, amino, mono- or di-lower alkylamino;… R<2> denotes hydrogen, alkyl, alkoxy or halogen;… R<3>, R<4>, R<5>, R<6>, R<1><1> and R<1><2> independently of one another denote hydrogen or lower alkyl;… R<3> and R<5> together denote a methylene or hydroxymethylene group;… R<7>, R<8>, R<9> and R<1><0> denote hydrogen or lower alkyl; or… R<1><1> and R<1><2> together denote an oxo group or spirocyclo-lower alkyl; or R<1><1> denotes hydrogen and R<1><2> denotes hydroxyl or acetoxy; and one of the radicals R<1><3> and R<1><4> denotes hydrogen and the other denotes lower alkyl or trifluoromethyl,… and physiologically tolerable salts of carboxylic acids of the formula I can be used as medicines, in particular for the treatment of neoplasias, acne and psoriasis. The novel compounds can be prepared by synthesis of the C(R<1><3>)=C(R<1><4>) double bond according to Wittig from an appropriate bicyclic and an appropriate monocyclic component and, if appropriate, subsequent modification of functional groups.

carboxylic acid

Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities

Aryl-substituted and aryl and (3-oxo-1-propenyl)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.

CYCLOALIPHATIC UNSATURATED DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR USE IN THERAPEUTICS AND COSMETICS

COMPOSES DE FORMULE : (CF DESSIN DANS BOPI) DANS LAQUELLE R A R REPRESENTENT HYDROGENE OU ALKYLE INFERIEUR, R REPRESENTE NOTAMMENT -CN OU OXAZOLINYLE, Z REPRESENTE UN RESTE MONO CYCLOALIPHATIQUE SATURE AYANT DE 8 A 12 ATOMES DE CARBONE, OU UN RADICAL BI- OU TRI-CYCLIQUE EVENTUELLEMENT SUBSTITUE, A ET E REPRESENTENT 0,1 OU 2 ET B, C ET D REPRESENTENT 0 OU 1, ETANT ENTENDU QUE : A C E 1 ET QUE B ETOU D 1, ET LES ISOMERES GEOMETRIQUES ET OPTIQUES DESDITS COMPOSES DE FORMULE I AINSI QUE LEURS SELS; ET LEUR APPLICATION COMME AGENTS PHARMACEUTIQUES OU COSMETIQUES. COMPOUNDS OF FORMULA: (CF DRAWING IN BOPI) IN WHICH RAR REPRESENTS HYDROGEN OR LOWER ALKYL, R REPRESENTS IN PARTICULAR -CN OR OXAZOLINYL, Z REPRESENTS A SATURATED MONO CYCLOALIPHATIC REMAINDER HAVING 8 TO 12 ATOMES OF CARBON BI-, OR ONE CARBON TRI. -CYCLIC POSSIBLE SUBSTITUTE, A AND E REPRESENT 0,1 OR 2 AND B, C AND D REPRESENT 0 OR 1, WHEREAS: ACE 1 AND THAT B AND OR D 1, AND THE GEOMETRIC AND OPTICAL ISOMERS OF SAID COMPOUNDS OF FORMULA I AS WELL THAT THEIR SALTS; AND THEIR APPLICATION AS PHARMACEUTICAL OR COSMETIC AGENTS.

Compounds having selectivity for retinoid x receptors

Compounds, compositions, and method for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

BICYCLIC NAPHTHALINE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE IN HUMAN AND VETERINARY MEDICINE AND COSMETICS.

Process for the production of bifunctional Z-stilbene compounds, new bifunctional Z-stilbene compounds and the use of the Z-stilbene compounds for the production of polymers.

NOVEL RETINOICALLY ACTIVE NAPHTHALENIC DERIVATIVES, PREPARATION METHODS THEREOF, AND MEDICINAL AND COSMETIC COMPOSITIONS CONTAINING THEM

Unsaturated cycloaliphatic compounds, and cosmetic and pharmaceutical preparations containing these unsaturated cycloaliphatic compounds.

NOVEL RETINOICALLY ACTIVE NAPHTHALENIC DERIVATIVES, PREPARATION METHODS THEREOF, AND MEDICINAL AND COSMETIC COMPOSITIONS CONTAINING THEM

Dimer-selective rxr modulators and methods for their use

Dimer-selective RXR modulator compounds having agonist, partial agonist and/or antagonist activity in the context of an RXR homodimer and/or RXR heterodimers are provided. Also provided are pharmaceutical compositions incorporating such dimer-selective RXR modulator compounds and methods for their therapeutic use.

Novel bexarotene analogs

The present invention relates to analogs of bexarotene and methods of use thereof.

Bis-stilbene compounds

Compounds with selectivity to retinoid x receptors.

Therapeutic prostaglandin receptor agonists

Described herein are compounds which can be used in topical liquids, creams, or other dosage forms such as solids, for reducing intraocular pressure, treating glaucoma, growing hair, treating wounds, or other medical and/or cosmetic uses.

E b n a 1 inhibitors and their method of use

본 발명의 약학적 조성물은 EBNA1 활성에 의해 유발된 질병, 예컨대 암, 감염성 단핵구증, 만성 피로 증후군, 다발성 경화증, 전신 홍반성 루프스 및 류마티스 관절염을 치료하는데 유용한 EBNA1 억제제를 포함한다. 본 발명의 약학적 조성물은 또한, 잠복성 엡스타인-바 바이러스(EBV) 감염에 의해 유발된 질병의 치료에 유용한 EBNA1 억제제들을 포함한다. 본 발명의 약학적 조성물은 또한, 용해성 엡스타인-바 바이러스(EBV) 감염에 의해 유발된 질병들의 치료에 유용한 EBNA1 억제제들을 포함한다.

Novel ligands that are antagonists of rar receptors, process for preparing them and use thereof in human medicine and in cosmetics

The invention relates to novel compounds corresponding to formula (I) below: and to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine, or alternatively in cosmetic compositions.

Process for preparing 2-aryl-substituted indenes

A process is disclosed for preparing 2-aryl-substituted indenes by reacting an indene with an arene compound substituted with an halogen atom, preferably a iodine atom, or with an organosulphonate group, said reaction being carried out in a basic medium in the presence of a palladium catalyst. The compounds obtainable by this process can be used to prepare metallocene compounds with transition metals such as titanium, zirconium or hafnium, which are useful as catalyst components in the polymerization of olefins.

Diaryl acetylenes, their preparation and use

Diaromatic propynyl or dienyl compounds

Novel diaromatic propynyl or dienyl compounds having general formula (I), and the use thereof in pharmaceutical compositions useful in human or veterinary medicine (in particular for the treatment of dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders), or in cosmetic compositions, are disclosed.

Microporous coordination complex and method of making the same

Disclosed herein is a three-dimensional coordination complex that includes a plurality of inorganic centers; a plurality of a first bis(bidentate) linker; and a plurality of a second bis(bidentate) linker, where the first and the second bis(bidentate) linkers are have different lengths, and the bidentate binding sites on each linker face in opposite directions on an axis.

Arylation of olefin(s)

Prodn. of substd. olefins (I), comprises reaction of aryl- diazonium salts (II) with olefins in the presence of a Pd catalyst. Substd. olefins (with Z = -CH=CHR) are pref. obtd. by reaction of a cpd. of formula (I) (with Z = -N2(+)G(-)) with an olefin of formula R-CH=CH2; (where R = H, 1-12C alkyl, opt. substd. 6-10C aryl, opt. substd. heteroaryl with 3-5C and 1-3 O, S or N atoms, or CN, COOM, COO(1-12C alkyl) or SO3M; M = a normal cation; n = 0 or 1 (if n = 0, free valency on ring A is occupied by H); m = 1 or 2; rings A-D and (hetero)aryl gps. are opt. substd. with 1 or more F, Cl, Br, I, 1-12C alk(ox)yl, CF3, OCF3, CN, nitro, COOM, COO(1-12C alkyl), SO3M, CO(1-12C alkyl), CO(6-10C aryl), 6-10C aryl, heteroaryl or opt. 1-12C alkyl-substd. amino gps.; G = normal counterion); reaction is carried out in the presence of a base, with metallic Pd and/or organic or inorganic Pd cpds., opt. combined with complex-forming cpds.; reaction medium is water or an alcohol, with Pd or a salt as catalyst, or in water in presence of a Pd complex derived from a cpd. with hydrophilic gps., pref. sulphonic acid gp(s). esp. a bis-(dibenzylidene acetone) Pd complex with 1-8 sulphonic acid gps.; pref. (I) is of formula RCH=CH-(A)-(-(B)-CH=CHR)n (with rings A, B as above), with R = H or opt. substd. Ph; (II) are sulphobenzene- diazonium salts; the ethylene is introduced into the mixt. with an intensive gassing device, pref. a surface or bulk gasifier, opt. with additional mechanical mixing.

Ebna1 inhibitors and their method of use

New Bls-stilbene compounds and processes for their production

Alicyclic phospholipase A2 inhibitors

Certain novel alicyclic compounds are effective phospholipase A2 (PLA2) inhibitors.

Stilbene derivative and method for preparing same

The present invention relates to a stilbene derivative and a method for preparing same. More particularly, the present invention relates to a novel stilbene derivative inhibiting a function of a cyclophilin and effective for preventing a cyclophilin-associated disease or treating a symptom thereof, and to a method for preparing the stilbene derivative.

Anticonvulsant compounds

Diaromatic propynyl or dienyl compounds and their use for dermatological and cosmetical purposes

A találmány tárgya (I) általánős képletű prőpinil-diarőmás vegyületek,valamint sói és őptikai és geőmetriai izőmerei - a képletben R1jelentése -CH3, -CH2-O-R6, -O-R6, vagy -CO-R7 csőpőrt, Ar jelentéseadőtt esetben szűbsztitűált 5 vagy 6 tagú arőmás vagy heterőarőmásgyűrű, X jelentése adőtt esetben szűbsztitűált kettős vagy hármaskötést tartalmazó csőpőrt, R2 és R3 jelentése azőnős vagy különböző,és lehet hidrőgénatőm, egyenes vagy elágazó láncú alkilcsőpőrt, -OR6,vagy -SR6 csőpőrt, R2 és R3 jelentése lehet tővábbá együttesen ahőzzájűk kapcsőlódó arőmás csőpőrttal együtt egy adőtt esetbenszűbsztitűált 5 vagy 6 tagú gyűrű, R4 és R5 jelentése azőnős vagykülönböző, és lehet hidrőgén- vagy halőgénatőm, egyenes vagy elágazóláncú alkilcsőpőrt, vagy -OR6 csőpőrt, R6 jelentése hidrőgénatőm,rövid szénláncú alkil- vagy egy szűbsztitűált karbőnilcsőpőrt, és R7jelentése hidrőgénatőm, alkil- vagy adőtt esetben szűbsztitűáltaminőcsőpőrt. A találmány vőnatkőzik tővábbá a fenti (I) általánősképletnek megfelelő vegyületek alkalmazására gyógyszerkészítményekben,valamint kőzmetikai készítményekben. ŕ FIELD OF THE INVENTION The present invention relates to proline proline compounds of formula (I) as well as salts and analytical agents thereof, wherein R 1 is -CH 3, -CH 2 -O-R 6, -O-R 6, or -CO-R 7, in the case where Ar is defined. 5 or 6-membered aromatic or heterocyclic ring, X is an optionally substituted double or triple-bonded tubular moiety, R2 and R3 are predominant or different and may be hydrogen, straight or branched chain alkyl, -OR6, or -SR6; moreover, in combination with a coalesced coarse-grained tubular tubular tube, an added 5-membered or 6-membered ring-attached ring, R 4 and R 5 are prime or different and may be hydrogen or halogen, straight or branched chain alkyl, or -OR 6, R 6 is hydrogen, lower alkyl, or a \ t and a R7 meaning h in the case of oestrus genes, alkyl or in the case of hypodermic hypothalamus. The invention further relates to the use of the compounds of ...

Selective retinoic acid analogs

NOVEL VINYL-4 BENZOIC ACID DERIVATIVES, PREPARATION METHOD THEREOF AND THERAPEUTIC APPLICATIONS THEREOF AND AS LIGANDS

PCT No. PCT/FR85/00074 Sec. 371 Date Dec. 5, 1985 Sec. 102(e) Date Dec. 5, 1985 PCT Filed Apr. 3, 1985 PCT Pub. No. WO85/04652 PCT Pub. Date Oct. 24, 1985.The invention relates to compounds of the formula I These compounds may be used in therapeutics for the treatment of acne, psoriasis, disorders of keratinization, in certain forms of cancer and as healing agents, particularly in the ocular field.

Bis-stilbene compounds for use as optical clarifiers.

ANALOGY PROCEDURE FOR THE PREPARATION OF THERAPEUTIC ACTIVE TETRALIN DERIVATIVES.

Process for the preparation of therapeutically useful aromatic carboxylic acid derivatives

Pharmaceutical compositions containing aromatic and araliphatic carboxylic acid derivatives for treating light and age-damaged skin and for promoting wound healing and some novel such compounds

Method for producing 2-aryl substituted indenes

SUBSTITUTED 4-HYDROXYANILIDES, ITS PRODUCTION AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM

Alkyl alkenyl and alkynyl Chrysamine G derivatives for the antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition.

Aromatic polycyclic retinoid-type derivatives, method for preparing same, and use thereof for making pharmaceutical and cosmetic compositions

Novel aromatic polycyclic retinoid-type derivatives of general formula (I), wherein groupings R3 and R4 attached to the double bond between carbons 11 and 12 are cis groupings, and pharmaceutical and cosmetic compositions containing same, are disclosed.

Compounds with retinoid x receptor selectivity

Aromatic carboxylic acid derivatives

Соединения могут применяться в качестве лекарственного средства, в частности, для дерматологических и онкологических показаний.

Patent SU391781A3

Ndm inhibitor

An objective of the present invention is to provide a novel NDM (New Delhi metallo-β-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of β-lactam antibiotics that have been inactivated as a result of decomposition by NDM. According to the present invention, there is provided an NDM inhibitor contains a compound represented by general formula (I):