НОВЫЕ СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ КАТЕПСИНА

... 1. Соединение формулы I где X1 и X2 оба представляют метилен, или X1 представляет этилен и X2 представляет связь; R3 представляет -CR5=CHR6, -CR5(CR63)2 или -CR7=NR8, где R5 представляет водород и R6 представляет водород, или (C1-4)алкил, или R5 и R6 вместе с атомами, к которым присоединены R5 и R6, образуют (C3-12 )циклоалкенил, гетеро(C5-12)циклоалкенил, (C6-12)арил, гетеро(C6-12)арил, (C9-12)бициклоарил или гетеро(C8-12)бициклоарил и R7и R8вместе с атомами, к которым присоединены R7 и R8, образуют гетеро(C5-12)циклоалкенил, гетеро(C6-12)арил или гетеро(C8-12 )бициклоарил, где R3 необязательно замещен 1-5 радикалами, независимо выбранными из группы, состоящей из (C1-4)алкила, циано, галогена, галогензамещенного (C1-4 )алкила, нитро, -Х4NR9R9, -X4OR9, -X4SR9, -Х4С(О)NR9R9, -X4C(O)OR9, -X4S(О)R10, -X4S(О)2 R10 и -X4С(О)R10, где X4 представляет связь или (C1-2)алкилен, R9 в каждом случае независимо представляет водород, (C1-3 )алкил или галогензамещенный (C1-3)алкил, и R10 представляет ( ...

METHOD FOR OBTAINING 1-ARYLSULPHONYLPYRROLIDINE-2-THIONE OR 1-ARYLSULPHONYLPIPERIDINE-2-THIONE DERIVATIVES

CПOCOБ ПOЛУЧEHИЯ ПPOИЗBOДHЫX ПИPPOЛO [2,1- ] TИAЗOЛA

Способ получения N-замещенных галоидпирролидинонов-2

The herbicidal preparation contains, as active component, a compound of the formula I. The substituents have the meaning given in the patent claim. The abovementioned compounds are prepared by cyclization of corresponding N-alkenylhalocyanamides in the presence of a catalytic amount of iron(II) ions. <IMAGE>

Способ получения производных индола или их солей

Hydantoinverbindungen

VERFAHREN ZUR HERSTELLUNG EINES GESCHÜTZTEN 4-AMINOMETHYL-PYRROLIDIN-3-ONS

New supported transition metal complex useful as catalyst in the transition metal catalyzed reaction, and in olefin metathesis reaction

Supported transition metal complex (T) based on a polystyrene matrix or silica gel matrix comprising a phenyl compound (I) or a phenyl-ketone compound (II), respectively, is new. Supported transition metal complex (T) based on a polystyrene matrix or silica gel matrix comprising a phenyl compound of formula (I) or a phenyl-ketone compound of formula (II), respectively, is new. X : a direct bond, O, S, -N(R 1>)-, -C(=O)O-, -O(O=)C-, -N(R 1>)(O=)C-, -C(=O)N(R 1>)-, -O-CHR 1>-O-, -OC(=O)N(R 1>)-, -N(R 1>)C(=O)O-, =C(=O) or =C(=S); R 1>, R 3>H or 1-4C alkyl; K 1>a transition metal complex; Z : a bond or a spacer; m, n, x, y : 1-5000; q : 2-5; and z : 3-20. An independent claim is included for a procedure for the transition metal catalyzed conversion of a reactant to a product in the presence of a supercritical carbon dioxide comprising using (T), as the catalyst. [Image] [Image].

OXOAMINO ACID DERIVATIVES

Tetrapeptide analogs

3-phenyl-4-halogeno-pyrrole derivatives and process for preparing the same

... 1,125,169. Pyrrole derivatives; antibiotics. SANKYO CO. Ltd. 13 July, 1966 [13 July, 1965], No. 31535/66. Headings C2A and C2C. The invention comprises novel antimicrobic 3 - phenyl - 4 - halogenopyrrole derivatives of the general formula wherein X 1 and X 2 are the same or different and represent hydrogen, a halogen, a nitro group or an alkoxy group containing from 1 to 5 carbon atoms and X represents bromine or chlorine, with the exception of 3-(21-nitro-31-chlorophenyl)-4-chloropyrrole, and the preparations thereof, including by heating 1-alkoxycarbonyl- 3 - phenyl - 4 - halogenopyrrole derivatives of the general formula wherein R represents an alkyl group containing from 1 to 5 carbon atoms, in the presence of an alkali metal hydroxide. 1 - Alkoxycarbonyl - 3 - phenyl 4 - halogenopyrrole derivatives of the second general formula above are prepared either by reacting 1-alkoxycarbonyl - 3 - phenyl - 4 - oxopyrrolidine derivatives of the general formula with phosphorus ...

4-(ALKOXY-PHENYL)-2-PYRROLIDONES THEIR PREPARATION AND US

... 1498705 4-(Alkoxyphenyl)-2-pyrrolidones, their preparation and use SCHERING AG 20 March 1975 [20 March 1974] 11686/75 Heading C2C Racemic and optically active 4-(alkoxyphenyl)-2-pyrrolidones of the formula wherein each R 1 and R 2 may be the same or different and is a hydrocarbon group which is optionally substituted by one or more halogen atoms, hydroxyl groups, cyano groups, carboxyl groups, alkoxy groups, alkoxycarbonyl, carboxamido or optionally substituted amino groups, or may be a heterocyclic group containing oxygen or sulphur, or one of R 1 and R 2 is hydrogen and the other represents said hydrocarbon group, or R 1 and R 2 together represent a C 1-3 alkylene group, with the proviso that when R 1 is methyl, R 3 is H or 5-methoxy, R 4 is H and X is oxygen, R 2 is other than methyl, R 3 represents a hydrogen atom or a methoxy group, R 4 represents a hydrogen atom or an alkyl, aryl, acyl or carboxamido group, and X represents an oxygen or sulphur atom, may be prepared (a) by hydrolysing ...

Process for preparing a protected 4-aminomethyl-pyrrolidin-3-one.

A process for preparing a compound of formula (I) in which P1 and P2 are protecting groups; comprising a) reaction of a compound of formula (5) wherein P1 is as defined for formula (I); with a Raney-nickel catalyst in a solvent under hydrogen to produce a compound of formula (6) wherein P1 is as defined for formula (I); b) protecting the amino group to produce a compound of formula (7) wherein P1 and P2 are as defined for formula (I); and c) selective reduction of the double bond to produce the compound of formula (I).

Pyrrolidinyl and pyrrolinyl ethylamine compounds as opioid kappa receptor agonists.

A compound of the formula:and the salts thereof, wherein A is halo, hydroxy or the like; the broken line represents an optional double bond with proviso that if the broken line is a .double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl^selected from phenyl, naphthyl, pyridyl and the like, the aryl or heteroaryl being optionally substituted; R is hydrogen, hydroxy, Ci-C4 alkyl or the like; and R2 and R3 are independently selected from optionally substituted Ci-C? alkyl Cs-Ce cycloalkyl, C2-Cs alkenyl, Ci-Cg alkynyl and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Inhibitors of factor XA and other serine proteases involved in the coagulation cascade

The present invention provides compounds of formula (I), wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thrombotic disorders. Also disclosed are pharmaceutical compositions comprising one or more compounds of formula (I), processes for preparing compounds of formula (I), and intermediates useful for preparing compounds of formula (I).

Process for preparing a protected 4-aminomethyl-pyrrolidin-3-one

Inhibitors of factor xa and other serine proteasesinvolved in the coagulation cascade.

Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists

Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists

Aminoalkoxyphenyl derivatives process of preparation and compositions containing the same

Inhibitors of factor XA and other serine proteasesinvolved in the coagulation cascade.

Process for preparing a protected 4-aminomethyl-pyrrolidin-3-one.

Inhibitors of factor xa and other serine proteasesinvolved in the coagulation cascade.

Process for preparing a protected 4-aminomethyl-pyrrolidin-3-one

Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists

Inhibitors of factor xa and other serine proteasesinvolved in the coagulation cascade.

Process for preparing a protected 4-aminomethyl-pyrrolidin-3-one

PROCEDURE FOR the PRODUCTION OF NEW SUBSTITUTED ONES 2-BENZYLPYRROLIDINEN, ITS QUATERNAEREN ALKYL CONNECTIONS AND ITS SAEUREADDITIONSSALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN DERIVATEN VON PERHYDRO-AZA-HETEROCYCLEN UND IHREN SAEURE- ADDITIONSSALZEN

BIOELECTRICALLY ACTIVE TEXTILE SUPPORT

VERFAHREN ZUR HERSTELLUNG VON NEUEN 2-PYRROLIDONDERIVATEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN SUBSTITUIERTEN 2-BENZYLPYRROLIDINEN, IHREN QUATERNAEREN ALKYLVERBINDUNGEN UND IHREN SAEUREADDITIONSSALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN SUBSTITUIERTEN 2-(2-IMINO-AETHYLIDEN)- -AZAHETEROCYCLEN UND TAUTOMEREN 2-(2-AMINO- AETHENYL)-AZAHETEROCYCLEN

ACRYLATE FUNGICIDES

5-OXO AND 5-THIOXOPROLINE, PROCEDURE FOR YOUR PRODUCTION AND IT ABSTENTION PHARMACEUTICAL ONE COMPOSITIONS.

CARBOXYL THIO PYRROLIDINYL BETA LACTAM DERIVATIVES AND YOUR PRODUCTION.

PYRROLIDIN DERIVATIVES, PRODUCTION AND USE AS CURES.

INDANDERIVATE, MANUFACTURING METHODS AND TREATMENT.

N-ACYLSULFONAMID-APOPTOSIs-PROMOTER

Procedure for the production of new Pyrrolidinderivaten and their salts

PROCEDURE FOR THE PRODUCTION OF A PROTECTING 4 - AMINOMETHYL-PYRROLIDIN-3-ONS

Herbicidal 3-substituted lactams

This disclosure relates, in part, to compounds of Formula (1) (including all stereoisomers), ...

RETROVIRAL PROTEASE INHIBITING COMPOUNDS

Phenoxy-pyrrolidine derivative and its use and compositions

The present invention is directed to the compound 2-(4- (hydroxymethyl)phenoxy)-1 -(3-(2-(trifluoromethyl)phenoxy)pyrrolidin-1 -yl)ethanone, its use as an inhibitor of stearoyl CoA desaturase and to pharmaceutical compositions containing this compound.

Therapeutic compounds

N-`4-(2-IMINO-PYRROLIDIN-1-YL)PHENYL

NITROGENOUS CYCLIC KETONE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE

Farnesoid X receptor agonists and uses thereof

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

Pyrrolidinyl and pyrrolinyl ethylamine compounds as kappa agonists

Retroviral protease inhibiting compounds

ALKYLAMINOALKOXYPHENYL DERIVATIVES, PROCESS OF PREPARATION AND COMPOSITIONS CONTAINING THE SAME

EXO-AMIDE PROSTAGLANDIN ANALOGUES

Cis-substituted aminocyclopropane derivatives

3-SUBSTITUTED INDOLES AND PRECURSORS THEREFOR

PROCESS FOR PREPARING 5-BIPHENYL-4-AMINO-2-METHYL PENTANOIC ACID

The present invention relates to pyrrolidin-2-ones according to the formu la (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting gr oup, methods for their preparation and their use in the preparation of NEP-i nhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S )-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or sa lt thereof.

PREPARATION OF PYRROLIDINE DERIVATIVES, AND PRODUCTS THUS OBTAINED

L'invention concerne un procédé pour la préparation de dérivés de formule générale (I): < IMG > (I) dans laquelle X est oxygène ou soufre, R est hydrogène ou alcoyle,Ro est hydrogène, alcoyle ou phényle éventuellement substitué par halogène, alcoyle, alcoyloxy, alcoylthio ou nitro, A représente un atome d'azote ou un radical =CH-, les symboles Y, identiques ou différents sont hydrogène, halogène, alcoyle, alcoyloxy, alcoylthio, alcoylcarbonyle, nitro, amino, alcoylcarbonylamino, alcoylamino, dialcoylamino, alcoylsulfinyle, alcoylsulfonyle, alcoyloxycarbonyle, cyano, trifluorométhyle, hydroxy, mercapto, alcoylcarbonyloxy ou alcoylsarbonylthio,n est égal à 0 ou 1 et p est égal à 1, 2 ou 3. L'invention concerne également les dérivés obtenus. Ces dérivés sont notamment utiles comme antidépresseurs.

N-ACYLSULFONAMIDE APOPTOSIS PROMOTERS

N-Benzoyl arylsulfonamides having the formula (I) are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.

2-BENZYLPYRROLIDINES, PROCESS FOR THEIR PREPARATION, AND MEDICAMENTS CONTAINING THEM

THERAPEUTIC PYRROLIDINE COMPOUNDS

Disclosed herein is a compound having a structure (I), or a pharmaceutically acceptable salt thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

AROMATIC SULFONAMIDE DERIVATIVES

Substituted aromatic sulfonamides of formula (I) pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.

NECROSIS INHIBITORS

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

ACRYLATE FUNGICIDES

Compounds of formula I (I) wherein X is oxygen or sulphur, W is CH or N, m is 0 or 1, and either a) n is 1 and Q is a non-aromatic heterocyclic ring of 3 to 10 ring atoms, containing one to three hetero atoms selected from oxygen, sulphur and nitrogen, which may be substituted and may be fused to another ring, with the proviso a) that if Q is thiazol-2-in-2-yl, it is substituted but not by methylene, and b) Q is not a six membered ring containing only two nitrogen atoms, or b) n is 0 or 1 and Q is where R1 is alkyl, alkoxy or alkylthio, and R2 is heteroaryl, non aromatic heterocyclyl, optionally substituted cycloalkyl or optionally substituted alkyl containing at least 5 carbon atoms, phenyl substituted by one or more groups selected from halogen, optionally substituted alkyl, alkoxy, haloalkoxy, aryloxy, alkylthio and alkoxycarbonyl, and when R1 is alkyl or alkoxy, or, when W is nitrogen, R2 can also be unsubstituted phenyl, have pesticidal especially fungicidal activity.

PYRROLIDINYL AND PYRROLINYL ETHYLAMINE COMPOUNDS AS KAPPA AGONISTS

A compound of formula (I) and the salts thereof, wherein A is halo, hydroxy or the like; the broken line represents an optional double bond with proviso th at if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, naphthyl, pyridyl and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl or the like; an d R2 and R3 are independently selected from optionally substituted C1-C7 alkyl C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optional ly substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Verfahren zur Herstellung von 1,3,3-trisubstituierten 4-( -subst.-Äthyl)-2-pyrrolidinonen

Verfahren zur Herstellung von 1,3,3-trisubstituierten 4-(o-Aminoalkyl)-2-pyrrolidinonen und -2-thionpyrrolidinonen

Procédé de préparation d'esters de 3-phényl-3-pyrrolidinols

Procédé de préparation de dérivés de la pyrrolidine

Verfahren zur Herstellung von Pyrrolderivaten

Procédé de préparation de nouveaux dérivés du pyrrole

Verfahren zur Herstellung von 4-Alkylprolinen

Process for the preparation of substituted indoles, and their use

Herbicidal preparation

Herbicidal preparation

The herbicidal preparation contains, as active ingredient, a compound of the formula I. The substituents have the meanings given in patent claim 1. The abovementioned compounds are prepared by cyclization of corresponding N-alkenylhaloacylamines in the presence of a catalytic amount of iron(II) ions. ...

PROCEDURE FOR the PRODUCTION OF NEW ONE 4 (POLYALKOXYPHENYL) - 2-PYRROLIDONEN.

Process for the preparation of pyrrole-2-acetic acids, their nitriles and esters

Pyrrole-2-acetic acid esters and nitriles of the respective formulae and are prepared by subjecting a pyrrolidene-malonic acid derivative of the formula II to catalytic dehydrogenation, preferably using dehydrogenation catalysts which contain, or consist of, palladium, platinum or rhodium. In the above formulae, X and Y independently of one another denote groups of the formulae -COO(lower alkyl) or -CN, and R1 and R2 independently of one another denote hydrogen atoms or lower alkyl radicals. The esters nitriles obtained can be hydrolysed to give the corresponding pyrrole-2-acetic acid. The products obtained may be used, for example, to prepare corresponding 5-aroyl-pyrrole-2-acetic acid derivatives, which are effective anti-inflammatory agents.

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF PERHYDRO AZA HETEROCYCLEN.

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF PERHYDRO AZA HETEROCYCLEN.

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF PERHYDRO AZA HETEROCYCLEN.

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF PERHYDRO AZA HETEROCYCLEN.

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF PERHYDRO AZA HETEROCYCLEN.

PROCEDURE FOR the PRODUCTION OF 1-METHYL-2-BENZYLPYRROLIDINEN.

DERIVATIVES [...] ACID 4.5 DIHYDRO-1H PYRROLE 2-CARBOXYLIC ACIDS AND 1.4.5.6-TETRAHYDROPYRIDINE DERIVATIVES AND 2-CARBOXYLIC ACIDS.

1-Mercaptoacyl derivatives of keto-substituted proline or keto-substituted piperidine-2-carboxylic acid

... 1-Mercaptoacyl derivatives of keto-substituted proline or keto-substituted piperidine-2-carboxylic acid of the general formula I in which R, R1, R2, R3, R4, m, p and q have the meaning indicated in Patent Claim 1, and their salts with bases are useful pharmaceuticals for the treatment of hypertension. The compounds of the formula (I) are prepared from keto-substituted proline- or piperidine-2-carboxylic acid derivatives of the formula (II). Such derivatives are reacted with carboxylic acid or chemical equivalents of the formula (III). ...

CHEMICAL COMPOUNDS

METHOD OF SYNTHESIS OF AND INTERMEDIATE COMPOUNDS

АНАЛОГИ ТЕТРАПЕПТИДА

Разработаны соединения, композиции и способы лечения гиперпролиферативных заболеваний, таких как рак.

ПРОТИВООПУХОЛЕВОЕ СРЕДСТВО

Настоящее изобретение обеспечивает терапевтическое средство для лечения опухоли, выбранной из опухоли кроветворной ткани и солидной опухоли, включающее в качестве активного ингредиента бензоильное соединение общей формулы (I) (где n представляет собой целое число от 1 до 5; R1 представляет собой замещенный или незамещенный низший алкокси, замещенный или незамещенный низший алкоксикарбонил, CONR7R8 или подобные; R2 представляет собой замещенный или незамещенный арил или замещенную или незамещенную ароматическую гетероциклическую группу; R3 и R5 могут быть одинаковыми или различными, и каждый представляет собой атом водорода, замещенный или незамещенный низший алкил или подобные; R4 представляет собой атом водорода, гидрокси или галоген и R6 представляет собой атом водорода, галоген, замещенный или незамещенный низший алкил или подобные), его пролекарство или его фармацевтически приемлемую соль.

ИНГИБИТОРЫ ФАКТОРА Ха И ДРУГИХ СЕРИНОВЫХ ПРОТЕАЗ, ВОВЛЕЧЁННЫХ В КОАГУЛЯЦИОННЫЙ КАСКАД

Настоящее изобретение относится к соединению формулы (I), где А, В, C, G и W1 имеют значения, определенные в описании, и к его фармацевтически приемлемой соли, которые могут использоваться при лечении тромботических заболеваний. Предложены также фармацевтические композиции, содержащие одно или несколько соединений формулы (I), способ получения соединений формулы (I) и промежуточные продукты для получения соединений формулы (I).

СПОСОБ ПОЛУЧЕНИЯ ЗАЩИЩЕННОГО 4-АМИНОМЕТИЛПИРРОЛИДИН-3-ОНА, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ И СПОСОБ ПОЛУЧЕНИЯ 3-АМИНОМЕТИЛ-4-АЛКОКСИИМИНОПИРРОЛИДИНА

... 1. Способ получения соединения формулы (1) в которой Р1и Р2обозначают защитные группы; включающий а) восстановление соединения формулы (5) где Р1 такой, как определено для формулы (1); в присутствии катализатора никель Ренея в растворителе в атмосфере водорода в присутствии одной или более добавок с получением соединения формулы (6) где Р1такой, как определено для формулы (1); b) защиту аминогруппы в присутствии одного или более оснований с получением соединения формулы (7) где Р1и Р2такие, как определено для формулы (1); и с) селективное восстановление двойной связи с получением соединения формулы (1). 2. Способ по п.1, где Р1и Р2 независимо выбраны из ацетила, трет-бутоксикарбонила и пивалоила. 3. Способ по п.2, где Р1и Р2оба обозначают трет-бутоксикарбонил. 4. Способ по любому из предыдущих пунктов, где растворитель на стадии а) представляет спирт или простой эфир. 5. Способ по любому из предыдущих пунктов, где на стадии а) растворитель используют в 2-20-кратном объемном количестве по ...

Procedure for the production of new Pyrrolinderivaten and their salts

NOUVEAUX DERIVES DE PERHYDRO-AZA-HETEROCYCLES UTILES COMME MEDICAMENTS ET PROCEDE POUR LEUR PREPARATION

La présente invention concerne des composés chimiques nouveaux et un procédé pour leur préparation. Les composés de l'invention correspondent à la formule ...

New pyrroles and their manufactoring processes

THIOINDOLES SUBSTITUTE ON the SULPHUR ATOM AND POSSIBLY ON the CORE INDOL, METHOD OF PREPARATION OF THOSE, AND THERAPEUTIC AGENTS BY COMPRISING APPLICATION

4-(Polyalkoxyphenyl)-2-pyrrolidones

3-hydroxy-3-methyl-2-methylene pyrrolidinium iodides - with vasodilator, hypotensive and analgesic activity

INHIBITORS OF FACTOR Xa AND OTHER SERINE PROTEASES INVOLVED IN THE COAGULATION CASCADE

THIONATION PROCESS AND A THIONATING AGENT

A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline PS.2 CHN as a thionating agent. A thionating agent which is crystalline PS.2 CHN. 1. A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product , by use of crystalline PS.2 CHN as a thionating agent.2. A process according to claim 1 , wherein the thionating agent and the compound are allowed to react with each other in a liquid solvent medium for the compound and for the thionating agent.3. The process according to claim 1 , wherein the liquid solvent medium comprises pyridine claim 1 , a C1-C3 alkylnitrile claim 1 , a cyclic sulfone and/or a C1-C3 dialkylsulfone.4. The process according to claim 1 , wherein the liquid solvent medium comprises pyridine claim 1 , sulfolane claim 1 , dimethyl sulfone and/or acetonitrile.5. The process according to claim 1 , wherein the reaction is performed at a temperature of 60° C. to 180° C.6. The process according to claim 5 , wherein the reaction is performed at temperature of 115° C. to 175° C.7. The process according to claim 1 , wherein the compound comprises a group (I) that is present in an amide function.8. The process according to claim 1 , wherein the compound comprises a group (I) that is present in a ketone function.9. The process according to claim 1 , wherein the thionating agent is used at a molar ratio to the group (I) to be transformed of 1 mole PS.2 CHN per 1-4 moles of group (I).10. The process according to claim 1 , comprising separating the thionated reaction product from the reaction.11. The process according to claim 10 , wherein water is added to the reaction and the thionated reaction product is separated as a solid material claim 10 , by precipitation or crystallization.12. A thionating agent which is ...

NEW PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL FOR THE MANUFACTURE NEP INHIBITORS

The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising -amino- -biphenyl- -methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof. 2. A process according to wherein the transition metal catalyst comprises Palladium (Pd).5. A process according to claim 4 , wherein the reduction reaction is carried out with hydrogen in the presence of a transition metal catalyst.8. A process according to claim 7 , wherein the reduction reaction is carried out with hydrogen in the presence of a transition metal catalyst.11. The compound according to whereinR1 is hydrogen;R2 is BOC; andR3 is a carboxyl group; orR1 and R2 are hydrogen; andR3 is a carboxyl group13. The use of a compound according to claim 9 , in the synthesis of an NEP-inhibitor or a prodrug thereof claim 9 , such as a NEP inhibitor or prodrug thereof comprising a -amino- -biphenyl- -methylalkanoic acid claim 9 , or acid ester claim 9 , backbone14. The use according to claim 13 , wherein the NEP-inhibitor is N-(3-carboxy-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methylbutanoic acid or a salt or a prodrug thereof.15. The use according to claim 14 , wherein the NEP-inhibitor prodrug is N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.16. A process for preparing N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester claim 9 , or a salt thereof claim 9 , comprising the manufacture of compound of formula (4) claim 9 , or salt thereof claim 9 , as defined in . The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, ...

METHOD FOR PRODUCING 3,4-DISUBSTITUTED PYRROLIDINE DERIVATIVE

The present invention provides an inexpensive and industrially advantageous method for producing an optically active form of an anti-(3S,4R)-3-alkylcarbamoyl-4-hydroxypyrrolidine derivative or it's enantiomer, which is a key intermediate for producing a high-quality optically active form of (3R,4S)-3-alkylaminomethyl-4-fluoropyrrolidine or it's enantiomer useful as an intermediate for producing pharmaceuticals. 4. The production method according to claim 1 , wherein the optically active catalyst in Step A is an optically active ruthenium catalyst having a chiral ligand.5. The production method according to claim 1 , wherein in Step A claim 1 , the chiral ligand in the optically active catalyst is an optically active 2 claim 1 ,2′-bis(diphenylphosphino)-1 claim 1 ,1′-binaphthyl (BINAP) or it's analogue claim 1 , 5 claim 1 ,5′-bis(diphenylphosphino)-4 claim 1 ,4′-bi-1 claim 1 ,3-benzodioxole (SEGPHOS) or it's analogue claim 1 , or (2 claim 1 ,2′-bisdiphenylphosphino)-6 claim 1 ,6′-dimethoxy-1 claim 1 ,1′-biphenyl (MeO-BIPHEP) or it's analogue.6. The production method according to claim 1 , wherein in Step A claim 1 , the chiral ligand in the optically active catalyst is 2 claim 1 ,2′-bis(diphenylphosphino)-1 claim 1 ,1′-binaphthyl (BINAP) or 5 claim 1 ,5′-bis(diphenylphosphino)-4 claim 1 ,4′-bi-1 claim 1 ,3-benzodioxole (SEGPHOS).7. The production method according to claim 1 , wherein the protecting group for the amino group represented by PGis an aralkoxycarbonyl group or an alkoxycarbonyl group.8. The production method according to claim 1 , wherein the protecting group for the amino group represented by PGis an aralkoxycarbonyl group.9. The production method according to claim 1 , wherein the protecting group for the amino group represented by PGis a benzyloxycarbonyl group.10. The production method according to claim 1 , wherein Ris a cyclopropyl group.11. The production method according to claim 1 , wherein the reaction in Step A is carried out under the ...

Psyllid Attractants and Their Uses

The present specification discloses psyllid attractants, compositions comprising such attractants, lures, traps and other devices using such attractants, methods and uses to attract, capture and/or kill psyllids using such attractants, compositions and/or lures, traps and/or other devices, and methods and uses for monitoring a psyllid population using such attractants, compositions and/or lures, traps and/or other devices. 156-. (canceled)62. The compound of claim 57 , wherein the compound has a binding affinity for a psyllid OBP or SAP having an equilibrium dissociation constant of less than 0.500 nM claim 57 , less than 0.450 nM claim 57 , less than 0.400 nM claim 57 , less than 0.350 nM claim 57 , less than 0.300 nM claim 57 , less than 0.250 nM claim 57 , less than 0.200 nM claim 57 , less than 0.150 nM claim 57 , less than 0.100 nM claim 57 , or less than 0.050 nM.63. A composition comprising one or more of the compounds as defined in .64. The composition of claim 57 , wherein the composition is a liquid composition claim 57 , a semi-solid composition claim 57 , or a solid composition.65. A device comprising one or more of the compounds as defined in .66. A method of capturing psyllids claim 57 , the method comprising using one or more of the compounds as defined in to attract the psyllids to a device claim 57 , thereby capturing the psyllids.67. A method of killing psyllids claim 57 , the method comprising using one or more of the compounds as defined in to attract the psyllids to a device claim 57 , thereby killing the psyllids.68. A method of monitoring a psyllid population claim 57 , the method comprising a) using one or more of the compounds as defined in to attract psyllids to a device claim 57 , thereby capturing the psyllids; b) counting the psyllids to determine a number of captured psyllids; and c) performing a statistical analysis on the number of captured psyllids in order to determine the psyllid population claim 57 , thereby monitoring the psyllid ...

Thionating agent

A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P 2 S 5 .2 C 5 H 5 N as a thionating agent. A thionating agent which is crystalline P 2 S 5 .2 C 5 H 5 N.

PROCESS FOR PREPARING BICYCLIC AMINE DERIVATIVES

The present invention provides a process for preparing a bicyclic amine derivative of the formula (Ia) or (Ib), 2. The process as claims in claim 1 , wherein the rhodium catalyst is a rhodium(I) compound.3. The process as claimed in claim 2 , wherein the rhodium(I) compound is of formula (IIIa) claim 2 , (IIIb) or (IIIc) claim 2 ,{'br': None, 'sup': '1', 'sub': '2', '[RhLiAn]\u2003\u2003(IIIa)'}{'br': None, 'sup': '2', 'sub': 2', 'n, '[RhLiAn]\u2003\u2003(IIIb)'}{'br': None, 'sup': '1', 'sub': '2', '[RhLiAn]\u2003\u2003(IIIc)'}wherein{'sup': '1', 'sub': 5', '12', '5', '12', '5', '12, 'Liis C-C-alkadiene, C-C-cycloalkadiene or C-C-bicycloalkadiene;'}{'sup': '2', 'sub': 2', '12', '5', '8, 'Liis C-C-alkene or C-C-cycloalkene;'}n is 1 or 2; andAn is halide, tetrafluoroborate, trifluoromethanesulfonate or acetylacetonate.4. The process as claimed in claim 3 , wherein the rhodium(I) compound is of formula (IIIa) with Libeing C-C-cycloalkadiene or C-C-bicycloalkadiene claim 3 , in particular 1 claim 3 ,5-cyclooctadiene or norbornadiene claim 3 , and An being chloride.5. The process as claimed in claim 1 , wherein the chiral phosphine ligand is a chiral diphosphine ligand.6. The process as claimed in claim 5 , wherein the diphosphine ligand comprises a ferrocene moiety.8. The process as claimed in claim 7 , wherein the diphosphine ligand is of the formula (IVa) or (IVb) with Rand Rhaving the same meaning and Rand Rhaving the same meaning.9. The process as claimed in claim 8 , wherein Rand Rare both C-C-alkyl and Rand Rare both optionally substituted C-C-hetaryl or optionally substituted C-C-aryl.10. The process as claimed in claim 9 , wherein Rand Rare both tert-butyl and Rand Rare both 1-naphthyl or 2-furyl.12. The process as claimed in claim 9 , wherein the bicyclic amine derivative is a compound of the formula (Ia) and the chiral phosphine ligand is the diphosphine of formula (IVa) claim 9 , as defined in .13. The process as claimed in claim 1 , wherein Xin formulae (Ia) ...

Serotonin receptor modulator

Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.

ASYMMETRIC SYNTHESIS METHOD, RELATED RAW MATERIAL AND PREPARATION METHOD OF (S,S)-2,8-DIAZABICYCLO[4,3,0]NONANE

The present invention relates to an asymmetric synthesis method of a chiral intermediate (S,S)-2,8-diazabicyclo[4,3,0]nonane (I) of moxifloxacin, wherein an imide or enamine compound is obtained by dehydration reaction of the pyrrolidine-3-ketone as shown in formula (II) and chiral amine(R)-1-phenylethylamine, followed by the reduction of the imide or enamine compound to obtain a compound of formula (III) or (IV) having the chiral structure of formula (I), and then a compound of formula (I) is obtained by intramolecular cyclization, and removal of the chiral auxiliary group and amino-protecting group. The present invention also relates to pyrrolidine-3-ketone as shown in formula (II) and a preparation method therefor, 2. The method according to claim 1 , characterized in that claim 1 , the reduction method is catalytic hydrogenation.3. The method according to claim 2 , characterized in that claim 2 , the catalyst in the catalytic hydrogenation is Raney nickel.4. The method according to claim 2 , characterized in that claim 2 , the catalyst in the catalytic hydrogenation is a palladium catalyst.5. The method according to claim 4 , characterized in that claim 4 , the palladium catalyst is palladium on carbon.6. The method according to claim 1 , characterized in that claim 1 , the dehydration reaction adopts a method of solvent refluxing water separation claim 1 , and the solvent is selected from the group consisting of methylbenzene claim 1 , benzene and n-hexane claim 1 , the solvent forming an azeotrope with water. The present invention relates to the technical field of preparation for a medicine intermediate, and in particular relates to the technical field of preparation for a chiral intermediate of quinolone antibacterial moxifloxacin, specifically an asymmetric synthesis method of a chiral intermediate (S,S)-2,8-diazabicyclo[4,3,0]nonane of quinolone antibacterial moxifloxacin, and simultaneously, the present invention further relates to a raw material ...

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity. 1131-. (canceled)134. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:ring B is phenyl; orring B is monocyclic 6-membered heteroaryl selected from pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.136. The compound of claim 134 , or a pharmaceutically acceptable salt or solvate thereof claim 134 , wherein:ring D is phenyl; orring D is monocyclic heteroaryl selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl; or{'sub': 2', '8, 'ring D is a monocyclic heterocycle that is a monocyclic C-Cheterocycloalkyl containing at least 1 N atom in the ring that is selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidine-2,5-dionyl, piperidinyl, piperidin-2-onyl, piperazinyl, morpholinyl, thiomorpholinyl, and azepanyl.'}138. The compound of claim 136 , or a pharmaceutically acceptable salt or solvate thereof claim 136 , wherein:{'sup': 3', '10, 'Lis absent, —O—, —S—, —CH═CH—, —C≡C—, or —NR—.'}139. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:{'sub': 3', '8, 'ring A is C-Ccycloalkyl'}140. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:{'sub': 2', '8, 'ring A is C-Cheterocycloalkyl.'}141. The compound of claim 140 , or a pharmaceutically acceptable salt or solvate thereof claim 140 , wherein:{'sub': 2', '8', '5', '8', '5', '8', '5', '8', '5', '8, 'ring A is a monocyclic C-Cheterocycloalkyl or a bicyclic C-Cheterocycloalkyl ...

Lysosome-Cleavable Linker

The present invention relates to a linker for forming conjugates of a protein or peptide with a therapeutically active agent and which comprise a thiomaleamic acid moiety that is susceptible to cleavage under the pH conditions prevalent in the lysosome. 3. A compound according to claim 1 , wherein said first sulfur atom is the sulfur atom of a first cysteine residue in R.4. A compound according to claim 3 , which is a compound of formula (Ic) and wherein said second sulfur atom is the sulfur atom of a second cysteine residue in R.5. A compound according to claim 4 , wherein said first sulfur atom and said second sulfur atom are attached to one another via a disulfide bridge —S—S— when the protein or peptide is in isolated form.6. A compound according to claim 1 , wherein Ris capable of specific binding to a target cell.7. A compound according to claim 6 , wherein Ris capable of specific binding to a cancer cell.8. A compound according to claim 1 , wherein Ris an antibody or an antibody fragment.9. A compound according to claim 8 , wherein said antibody or antibody fragment is capable of specific binding to an antigen selected from MY9 claim 8 , B4 claim 8 , EpCAM claim 8 , CD2 claim 8 , CD3 claim 8 , CD4 claim 8 , CD5 claim 8 , CD6 claim 8 , CD11 claim 8 , CD19 claim 8 , CD20 claim 8 , CD22 claim 8 , CD25 claim 8 , CD26 claim 8 , CD30 claim 8 , CD33 claim 8 , CD37 claim 8 , CD38 claim 8 , CD40 claim 8 , CD44 claim 8 , CD56 claim 8 , CD64 claim 8 , CD70 claim 8 , CD74 claim 8 , CD79 claim 8 , CD105 claim 8 , CD138 claim 8 , CD205 claim 8 , CD227 claim 8 , EphA receptors claim 8 , EphB receptors claim 8 , EGFR claim 8 , EGFRvIII claim 8 , HER2 claim 8 , HER3 claim 8 , BCMA claim 8 , PSMA claim 8 , Lewis Y claim 8 , mesothelin claim 8 , cripto claim 8 , alpha(v)beta3 claim 8 , alpha(v)beta5 claim 8 , alpha(v)beta6 integrin claim 8 , C242 claim 8 , CA125 claim 8 , GPNMB claim 8 , ED-B claim 8 , TMEFF2 claim 8 , FAP claim 8 , TAG-72 claim 8 , GD2 claim 8 , CAIX and 5T4. ...

Necrosis Inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition. 2. The compound of claim 1 , wherein:{'sub': '1', 'Ris substituted or unsubstituted: phenyl, cyclohexyl, furan, thiophene or azole;'}{'sub': '2', 'Ris substituted or unsubstituted: aziridine, azetidine, pyrrolidine, piperidine, oxazolidine, oxazinane; diazolidine, diazinane, pyrrole, dihydropyrrole, dihydropyridine, or tetrahydropyridine; and'}{'sub': '3', 'Ris 1,1-dimethylpropyl, 1,1-dimethylprop-2-enyl, or 1,1-dimethylprop-2-ynyl, each optionally fluorinated with 1-4 F atoms; or'}a corresponding sulfonamide of the amide compound, ora pharmaceutically acceptable salt, hydrate or stereoisomer of the compound or corresponding sulfonamide.3. The compound of claim 1 , wherein:{'sub': '1', 'Ris substituted or unsubstituted: phenyl, cyclohexyl, furan, thiophene or azole;'}{'sub': '2', 'Ris substituted or unsubstituted: azetidine, pyrrolidine, piperidine, oxazolidine, diazolidine, or diazinane; and'}{'sub': '3', 'Ris 1,1-dimethylpropyl, 1,1-dimethylprop-2-enyl, or 1,1-dimethylprop-2-ynyl, each optionally fluorinated with 1-4 F atoms; or'}a corresponding sulfonamide of the amide compound, ora pharmaceutically acceptable salt, hydrate or stereoisomer of the compound or corresponding sulfonamide.4. The compound of claim 1 , wherein:{'sub': '1', 'Ris substituted or unsubstituted: phenyl, cyclohexyl, furan, thiophene or azole;'}{'sub': '2', 'Ris substituted or unsubstituted: azetidine or pyrrolidine; and'}{'sub': '3', 'Ris 1,1-dimethylpropyl, 1,1-dimethylprop-2-enyl, or 1,1-dimethylprop- ...

ECO-FRIENDLY MATERIALS AND METHODS FOR RENEWABLE AND SUSTAINABLE APPLICATIONS IN MATERIAL CHEMISTRY

The invention relates to novel hydrazide-based templates, methods of making the same, and methods of using the hydrazide-based templates as molecular scaffolds for asymmetric light driven transformations, light driven material synthesis, and biological applications. Furthermore, the present invention relates to photoinitiators, monomers, and polymers derived from biomass, together with methods and methods of using the same. 2. The molecular scaffold of claim 1 , wherein the organic functional group is an acid anhydride claim 1 , an alcohol claim 1 , an aldehyde claim 1 , an alkane claim 1 , an alkene claim 1 , an alkyl claim 1 , an alkyne claim 1 , an amide claim 1 , an amine claim 1 , an arene claim 1 , an azo compound claim 1 , a cabamate claim 1 , a carboxylic acid claim 1 , an ether claim 1 , an epoxide claim 1 , an ester claim 1 , an imine claim 1 , an isocyanate claim 1 , a ketone claim 1 , a nitrile claim 1 , a thiol claim 1 , derivatives thereof or combination thereof.3. The molecular scaffold of claim 1 , wherein at least one of R claim 1 , R claim 1 , R claim 1 , or Rcomprises a thiol group or thiol-based derivative.4. The molecular scaffold of claim 1 , wherein the inorganic functional group comprises an actinide claim 1 , an alkali metal claim 1 , an alkaline metal claim 1 , a metalloid claim 1 , a lanthanide claim 1 , a nitrogen-containing compound claim 1 , a phosphorus-containing compound claim 1 , a sulfur-containing compound claim 1 , a transition metal claim 1 , derivatives thereof claim 1 , and combinations thereof.5. The molecular scaffold of claim 1 , wherein the inorganic functional group comprises a nitrate claim 1 , a nitrite claim 1 , a phosphate claim 1 , a phosphite claim 1 , a sulfate claim 1 , a sulfite claim 1 , a sulfonate claim 1 , derivative thereof claim 1 , or combination thereof.6. A method of performing visible light mediated chemical transformation comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'irradiating the ...

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity. 4. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring B is phenyl.5. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring B is monocyclic 6-membered heteroaryl selected from pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.7. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring D is phenyl.8. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring D is monocyclic heteroaryl selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.11. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:{'sub': 2', '8, 'ring D is a monocyclic heterocycle that is a monocyclic C-Cheterocycloalkyl containing at least 1 N atom in the ring that is selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidine-2,5-dionyl, piperidinyl, piperidin-2-onyl, piperazinyl, morpholinyl, thiomorpholinyl, and azepanyl.'}12. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:{'sup': 3', '2', '4', '4', '2, 'Lis —X-L- or -L-X—;'}{'sup': 2', '10', '10', '10', '10', '10, 'sub': 2', '2', '2', '2, 'Xis absent, —O—, —S—, —S(═O)—, —S(═O)—, —S(═O)NR—, —CH—, —CH═CH—, —C≡C—, —C(═O)—, —C(═O)O—, —OC(═O)—, —C(═O)NR—, —NRC(═O)—, —NRS(═O)—, or —NR—;'}{'sup': '4', 'sub': '2', 'Lis absent or —CH—.'}13. The compound of any one of - , or a pharmaceutically ...

HUMAN PLASMA KALLIKREIN INHIBITORS

Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity. 2. The compound of claim 1 , wherein Rrepresents —OH claim 1 , —OR claim 1 , alkyl claim 1 , aryl claim 1 , haloalkyl claim 1 , or cycloalkyl;Z is absent or represents one or more occurrences of halo;{'sub': 2', 'p, 'sup': c', 'c', 'c, 'X represents —C(NH)—, —C(NH(R))—, —C(NHS(O)R)—, or —C(NHC(O)R)—;'}{'sup': '3', 'Rrepresents optionally substituted aryl or heteroaryl;'}{'sup': '3a', 'Ris absent or represents one or more substituents independently selected from the group consisting of alkyl and cyano;'}{'sup': 4', '4', '4, '—Y—Rrepresents -alkylene-Ror —N(alkyl)-R; and'}{'sup': '4', 'Rrepresents cycloalkyl.'}3. The compound of claim 1 , wherein Rrepresents —OH claim 1 , —O((C-C)alkyl) claim 1 , (C-C)alkyl claim 1 , haloalkyl claim 1 , cycloalkyl claim 1 , or aryl.4. The compound of claim 3 , wherein n is 1; and{'sup': '1', 'sub': 3', '2', '2', '3', '2', '3', '3, 'Rrepresents —OH, —CH—OCHCHCH, —OCHCH, or —OCH.'}511-. (canceled)12. The compound of claim 3 , wherein n is 2; and the two occurrences of Rare geminal.13. The compound of claim 12 , wherein Rrepresents —OH claim 12 , —OCH claim 12 , —CH claim 12 , —CF claim 12 , cyclopropyl claim 12 , or phenyl.14. The compound of claim 12 , wherein:{'sup': 1', '1, 'sub': 1', '6, '(a) one occurrence of Rrepresents —OH or —((C-C)alkyl); and the other occurrence of Rrepresents aryl or cycloalkyl heteroaryl;'}{'sup': 1', '1, 'sub': 1', '6, '(b) one occurrence of Rrepresents —OH or —((C-C)alkyl); and the other occurrence of Rrepresents alkyl or haloalkyl; or'}{'sup': '1', '(c) both occurrences of Rare halo.'}15. ...

Substituted Fused Pyrrolo-Diazepinones and Uses Thereof

Disclosed are compounds, pharmaceutical compositions, and methods of treatment. The disclosed compounds are based on fused 1,4-diazepine and pyrrolidinedione scaffolds. The compounds may be utilized in pharmaceutical compositions and methods for treating diseases and disorders associated with cell proliferation such as cancer and may have a formula illustrated as follows:

Heterocyclic inhibitors of mct4

Disclosed herein are compounds and compositions useful in the treatment of MCT4 mediated diseases, such as proliferative and inflammatory diseases, having the structure of Formula I: Methods of inhibition MCT4 activity in a human or animal subject are also provided.

HERBICIDAL 3-SUBSTITUTED LACTAMS

This disclosure relates, in part, to compounds of Formula 1 (including all stereoisomers), N-oxides of such compounds, and salts of such compounds and N-oxides: 2. The compound of wherein{'sup': A', '8', '1, 'sub': 1', '7', '1', '7', '3', '9', '1', '7', '1', '7', '3', '9, 'Ris C-Calkyl, C-Chaloalkyl, C-Ccycloalkyl, C-Calkoxy or C-Chaloalkoxy, C-Ccycloalkoxy, each substituted or unsubstituted with up to 2 substituents independently selected from Ror G; or'}{'sup': A', '1, 'Ris G;'}{'sup': 'B', 'sub': 1', '4', '1', '4', '1', '4, 'Ris H, C-Calkoxy, C-Chaloalkyl or C-Calkyl;'}{'sup': 'C', 'sub': 1', '4', '1', '4', '1', '4, 'Ris H, C-Calkoxy, C-Chaloalkyl or C-Calkyl;'}{'sup': 'D', 'sub': 1', '3', '2', '3, 'Ris H, C-Calkyl or C-Calkylcarbonyl;'}{'sup': 'E', 'sub': 2', '1', '6', '1', '6', '2', '6', '3', '6', '4', '8', '2', '8', '3', '8', '2', '8', '2', '8', '2', '8', '2', '8', '2', '8', '2', '8', '2', '8', '4', '10', '5', '10', '2', '8', '2', '8', '4', '10', '2', '8', '3', '10', '4', '10', '1', '6', '1', '6', '1', '6', '3', '8', '1', '6', '1', '6', '3', '8', '1', '6', '2', '8, 'Ris H, hydroxy, amino, cyano, formyl, —C(O)NH, C-Calkyl, C-Chaloalkyl, C-Ccyanoalkyl, C-Ccycloalkyl, C-Ccycloalkylalkyl, C-Calkoxyalkyl, C-Calkoxyalkoxyalkyl, C-Chaloalkoxyalkyl, C-Calkenyl, C-Chaloalkenyl, C-Calkenylalkyl, C-Chaloalkenylalkyl, C-Calkylcarbonyl, C-Chaloalkylcarbonyl, C-Ccycloalkylcarbonyl, C-Ccycloalkylcarbonylalkyl, C-Calkoxycarbonyl, C-Chaloalkoxycarbonyl, C-Ccycloalkoxycarbonyl, C-Calkylaminocarbonyl, C-Cdialkylaminocarbonyl, C-Ccycloalkylaminocarbonyl, C-Calkoxy, C-Calkylsulfinyl, C-Chaloalkylsulfinyl, C-Ccycloalkylsulfinyl, C-Calkylsulfonyl, C-Chaloalkylsulfonyl, C-Ccycloalkylsulfonyl, C-Calkylaminosulfonyl or C-Cdialkylaminosulfonyl;'}{'sup': F', '16, 'sub': 2', '2', '8', '2', '8', '4', '10', '2', '8', '2', '8', '4', '10', '2', '8', '3', '10', '4', '10', '1', '6', '1', '6', '3', '8', '1', '6', '1', '6', '3', '8', '1', '6', '2', '8', '2', '1', '6', '1', '6', '3', '8', '2', '8 ...

ECO-FRIENDLY MATERIALS AND METHODS FOR RENEWABLE AND SUSTAINABLE APPLICATIONS IN MATERIAL CHEMISTRY

The invention relates to novel hydrazide-based templates, methods of making the same, and methods of using the hydrazide-based templates as molecular scaffolds for asymmetric light driven transformations, light driven material synthesis, and biological applications. Furthermore, the present invention relates to photoinitiators, monomers, and polymers derived from biomass, together with methods and methods of using the same. 1. A biomass derived , photodegradable polymer comprising at least one functionalized monomeric from the group consisting of: a phenacyl , a hydrazide , methylmethacrylate , or derivatives thereof.2. The photodegradable polymer of claim 1 , further comprising at least one second monomeric unit comprising a phototrigger.3. The photodegradable polymer of claim 2 , further comprising at least one third monomeric unit claim 2 , wherein the third monomeric unit is not a derived from biomass.4. The photodegradable polymer of claim 1 , wherein the first monomeric unit is also a photoinitiator.5. The photodegrabale polymer of claim 4 , wherein the photoinitiator is derived from biomass.6. The photodegradable polymer of claim 1 , wherein photocleavage of said polymer occurs from exposure to light from about 300 nm to about 450 nm in wavelength. This application is a divisional of U.S. patent application Ser. No. 16/124,418, filed Sep. 7, 2018, which is a continuation of PCT/US2017/21277, filed Mar. 8, 2017, which claims priority under 35 U.S.C § 119 to Provisional patent Application Ser. No. 62/305,044 filed Mar. 8, 2016, Provisional patent Application Ser. No. 62/324,194 filed Apr. 18, 2016, and Provisional patent Application Ser. No. 62/324,189 filed Apr. 18, 2016, herein incorporated by reference in their entirety.This invention was made with government support under Contract No. 1465075 awarded by the National Science Foundation (NSF), and by the National Science EPSCoR (EPS IIA-1355466) for the Center for Sustainable Materials Science (CSMS), North ...

HETEROCYCLIC INHIBITORS OF MCT4

Disclosed herein are compounds and compositions useful in the treatment of MCT4 mediated diseases, such as proliferative and inflammatory diseases, having the structure of Formula I: 2. The compound as recited in claim 1 , or a salt thereof claim 1 , wherein exactly one of A claim 1 , A claim 1 , and Ais N.3. The compound as recited in claim 2 , or a salt thereof claim 2 , wherein Aand Aare C; and Ais N.4. The compound as recited in claim 3 , or a salt thereof claim 3 , wherein X is hydrogen.6. The compound as recited in claim 4 , or a salt thereof claim 4 , wherein:{'sup': '2', 'Y is chosen from aryl and heteroaryl, any of which is optionally substituted with one to three Rgroups; and'}{'sup': '2', 'each Ris independently chosen from alkyl, alkoxy, alkoxyalkyl, alkylthio, haloalkyl, haloalkoxy, cycloalkoxy, cycloalkylmethoxy, heterocycloalkylmethoxy, carboxamido, sulfonamido, halo, aryl, and heteroaryl.'}8. The compound as recited in claim 7 , or a salt thereof claim 7 , wherein:{'sup': '2', 'each Ris independently chosen from alkyl, alkoxy, alkoxyalkyl, haloalkyl, haloalkoxy, cycloalkoxy, cycloalkylmethoxy, and halo, or'}{'sup': '2', 'two R, together with the intervening atoms, form a 5-7 membered cycloalkyl or heterocycloalkyl ring.'}9. The compound as recited in claim 8 , or a salt thereof claim 8 , wherein Z is chosen from phenyl claim 8 , pyridinyl claim 8 , pyridazinyl claim 8 , pyrimidinyl claim 8 , and pyrazinyl claim 8 , any of which is optionally substituted with one or two Rgroups.10. The compound as recited in claim 9 , or a salt thereof claim 9 , wherein each Ris independently chosen from alkyl claim 9 , alkoxy claim 9 , haloalkyl claim 9 , haloalkoxy claim 9 , amino claim 9 , aminoalkyl claim 9 , and halo claim 9 , and and is optionally substituted with one or two Rgroups.11. The compound as recited in claim 10 , or a salt thereof claim 10 , wherein Y is heteroaryl claim 10 , and is substituted with one or two Rgroups.12. The compound as recited in ...

PHOTOALIGNING MATERIALS

The present invention relates to polymer, homo- or copolymer or oligomer for the photoalignment of liquid crystals, especially for the planar orientation of liquid crystals, comprising a main chain and a side chain, wherein the side chain and/or main chain comprises a polar group, compositions thereof, and its use for optical and electro optical devices, especially liquid crystal devices (LCDs). 4. Polymer claim 1 , homo- or copolymer or oligomer comprising a compound of formula (I) according to claim 1 , as one basic building block.5. Copolymer comprising a compound of formula (I) as described in claim 1 , and a further compound of formula (I) as described in wherein B is substituted by one claim 1 , two claim 1 , three claim 1 , four claim 1 , five claim 1 , six or seven fluorine atoms.6. Composition comprising at least one first compound of formula (I) according to and optionally at least one second compound of formula (I) according to claim 1 , which is not identical to the at least one first compound of formula (I) claim 1 , and/or an additive.7. Process for the preparation of a polymer claim 1 , homo- or copolymer or oligomer comprising polymerisation of a compound of formula (I) according to claim 1 , wherein the compound is a diamine.8. Polymer claim 7 , homo- or copolymer or oligomer obtainable by the process according to .9. Composition comprising{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a polymer, homo- or copolymer, or oligomer comprising at least a compound of formula (I) according to which is a diamine as basic building block.'}10. Orientation layer claim 4 , comprising at least one polymer claim 4 , homo- or copolymer or oligomer according .11. Method for the preparation of a polymer layer or oligomer layer claim 4 , wherein one or more polymers claim 4 , homo- or copolymers or oligomers according to is treated with aligning light.12. Polymer claim 11 , homo- or copolymer or oligomer layer which is an orientation layer obtainable by the ...

Novel Promysalin Analogues and Methods of Use Thereof

The present invention includes novel analogs of promysalin useful in preventing or treating a microbial infection. The present invention also includes methods preventing or treating a microbial infection in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of the invention. 37.-. (canceled)8. The compound of claim 1 , wherein Ris F.9. (canceled)10. The compound of claim 1 , wherein the bond between carbons 3 and 4 represents a single bond.11. The compound of claim 1 , wherein the bond between carbons 3 and 4 represents a double bond.12. The compound of claim 1 , wherein X is O.13. The compound of claim 1 , wherein Y is H.14. The compound of claim 1 , wherein Y is OR.15. The compound of claim 1 , wherein n is 1.16. The compound of claim 1 , wherein n is 2.17. The compound of claim 1 , wherein m is 5.18. The compound of claim 1 , wherein the compound is selected from the group consisting of (1R claim 1 ,7R)-1-carbamoyl-1-hydroxytridecan-7-yl (2S)-1-(2-hydroxybenzoyl)pyrrolidine-2-carboxylate claim 1 , (1R claim 1 ,7R)-1-carbamoyl-1-hydroxytridecan-7-yl (2S)-1-(2-hydroxybenzoyl)piperidine-2-carboxylate claim 1 , (1R claim 1 ,7R)-1-carbamoyl-1-hydroxytridecan-7-yl (2S claim 1 ,4R)-4-hydroxy-1-(2- hydroxybenzoyl)pyrrolidine-2-carboxylate claim 1 , (7R claim 1 ,13R)-14-amino-13-hydroxy-14-oxotetradecan-7-yl (S)-4-fluoro-1-(2-hy droxybenzoyl)-2 claim 1 ,3-dihydro-1H-pyrrol e-2-carboxyl ate claim 1 , (7R claim 1 ,13R)-14-amino-13-hydroxy-14-oxotetradecan-7-yl (S)-1-(2-hydroxybenzoyl)-4-methyl-2 claim 1 ,3-dihydro-1H-pyrrole-2-carboxylate claim 1 , (1R claim 1 ,7R)-1-carbamoyl-1-hydroxytridecan-7-yl (2S)-1-(2-methoxybenzoyl)-2 claim 1 ,3-dihydro-1H-pyrrole-2-carboxylate claim 1 , (7R claim 1 ,13R)-14-amino-13-hydroxy-14-oxotetradecan-7-yl (S)-1-(3-hydroxybenzoyl)-2 claim 1 ,3-dihydro-1H-pyrrole-2-carboxylate claim 1 , (1R claim 1 ,7R)-1-carbamoyl-1-hydroxytridecan-7-yl (2S)-1-(4-hydroxybenzoyl)-2 claim 1 ,3- ...

ANDROGEN RECEPTOR MODULATORS AND METHODS FOR THEIR USE

Compounds having a structure of formula (I), (I-A), (Ia)-(Ie), (A)-(E), and (II) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of disorders including prostate cancer are also provided. 2. The compound of claim 1 , wherein R is W.3. The compound of or claim 1 , wherein W is hydrogen claim 1 , halogen claim 1 , —CF claim 1 , or —NRR.4. The compound of any one of - claim 1 , wherein L is -E-R.5. The compound of any one of - claim 1 , wherein Ris selected from hydrogen claim 1 , optionally substituted C-Calkyl claim 1 , optionally substituted —OR claim 1 , optionally substituted —SR claim 1 , optionally substituted C-Calkoxy claim 1 , —NRR claim 1 , —NRSR claim 1 , —NRSOR claim 1 , —NRSOR claim 1 , —NRCOR claim 1 , —CONRR claim 1 , —SONRR claim 1 , —SONRR claim 1 , optionally substituted —SOR claim 1 , or optionally substituted —SOR.6. The compound of any one of - claim 1 , wherein Ris selected from hydrogen claim 1 , —C-Calkyl claim 1 , —NRSO(C-Calkyl) claim 1 , —NRSO(C-Calkyl) claim 1 , —SONRR claim 1 , —SONRR claim 1 , SOR claim 1 , or —SOR.9. The compound of any one of claim 1 , claim 1 , and claim 1 , wherein B is phenyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , or thiophenyl.11. The compound of any one of claim 1 , claim 1 , and claim 1 , wherein A is phenyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , or thiophenyl.13. The compound of any one of - claim 1 , wherein X is a bond.14. The compound of any one of - claim 1 , wherein X is —(CRR)— or —NR—.15. The compound of any one of - claim 1 , wherein X is —NR—.16. The compound of any one of - claim 1 , wherein R is hydrogen or optionally substituted C-Calkyl.17. The compound of any one of - claim 1 , wherein Ris hydrogen.18. The compound of any one of - claim 1 , wherein Ris methyl.19. The compound of any one of - claim 1 ...

HYDROFLUOROCARBOXIMIDATE AND METHODS OF MAKING AND USING THE SAME

Described herein is an hydrofluorocarboximidate of formula (I) where: Ris a linear or branched alkyl group comprising 1 or 2 carbon atoms and (a) R1 and R2 are independent-selected from a linear or branched perfluorinated alkyl group comprising 1-8 carbon atoms and optionally comprising at least one catenated atom selected from oxygen, nitrogen, or combinations thereof; or (b) R1 and R2 are connected to form a ring structure comprising a total of 4-8 carbon atoms and in addition to the nitrogen atom from the carboximidate the ring structure may optionally comprises at least one catenated atom selected from oxygen, nitrogen, or combinations thereof. A method of making the hydrofluorocarboximidate with improved yield is described as well as various uses for the hydrofluorocarboximidate of Formula (I). 2. The method of claim 1 , wherein Rand Rform a perfluorinated 6-membered ring claim 1 , wherein the ring comprises an oxygen atom.3. The method of claim 1 , wherein (R) and Rform a perfluorinated 5-membered ring.4. The method of claim 1 , wherein Ris a perfluoro ethyl group and Ris a perfluoro propyl group.5. The method of claim 1 , wherein Ris a methyl group.6. The method of claim 1 , wherein Ris an ethyl group.9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)16. The method of claim 1 , wherein the hydrofluorocarboximidate based on closed-cup flashpoint testing following ASTM D-327-96 e-1 is not flammable.17. The method of claim 1 , wherein the hydrofluorocarboximidate has a global warming potential of less than 100.18. The method of claim 1 , wherein the hydrofluorocarboximidate has a boiling point of 80 to 150 C.19. The working fluid of claim 8 , wherein the working fluid further comprises a co-solvent.20. The working fluid of claim 8 , wherein Rand Rform a perfluorinated 6-membered ring claim 8 , wherein the ring comprises an oxygen atom.21. The working fluid of claim 8 , wherein (R) and Rf2 form a perfluorinated 5-membered ring.22. ...

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity. 4. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring B is phenyl.5. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring B is monocyclic 6-membered heteroaryl selected from pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.7. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring D is phenyl.8. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring D is monocyclic heteroaryl selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.11. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:{'sub': 2', '8, 'ring D is a monocyclic heterocycle that is a monocyclic C-Cheterocycloalkyl containing at least 1 N atom in the ring that is selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidine-2,5-dionyl, piperidinyl, piperidin-2-onyl, piperazinyl, morpholinyl, thiomorpholinyl, and azepanyl.'}12. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:{'sup': 3', '2', '4', '4', '2, 'Lis —X-L- or -L-X—;'}{'sup': 2', '10', '10', '10', '10', '10, 'sub': 2', '2', '2', '2, 'Xis absent, —O—, —S—, —S(═O)—, —S(═O)—, —S(═O)NR—, —CH—, —CH═CH—, —C≡C—, —C(═O)—, —C(═O)O—, —OC(═O)—, —C(═O)NR—, —NRC(═O)—, —NRS(═O)—, or —NR—;'}{'sup': '4', 'sub': '2', 'Lis absent or —CH—.'}13. The compound of any one of - , or a pharmaceutically ...

Substituted Fused Pyrrolo-Diazepinones and Uses Thereof

Disclosed are compounds, pharmaceutical compositions, and methods of treatment. The disclosed compounds are based on fused 1,4-diazepine and pyrrolidinedione scaffolds. The compounds may be utilized in pharmaceutical compositions and methods for treating diseases and disorders associated with cell proliferation such as cancer. 2. The compound of claim 1 , wherein Rand Rare methyl.3. The compound of claim 1 , wherein Ris methyl.4. The compound of claim 1 , wherein Ris selected from methyl claim 1 , isopropyl claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , furanyl claim 1 , pyridinyl claim 1 , phenyl fluorophenyl claim 1 , chlorophenyl claim 1 , carboxyphenyl claim 1 , methoxyphenyl benzyl claim 1 , thiophenyl chlorothiophenyl claim 1 , tetrahydrofuranyl claim 1 , thiazolyl claim 1 , 1 claim 1 ,3-benzodioxolyl claim 1 , 1 claim 1 ,4-benzodioxanyl claim 1 , and piperidinyl.7. The compound of claim 1 , wherein Ris 3 claim 1 ,4-dichlorophenyl and Ris oxobenzyl.8. A pharmaceutical composition comprising any effective amount of the compound of and a pharmaceutical carrier claim 1 , excipient claim 1 , or diluent.9. A method for treating a disease or disorder in a subject in need thereof claim 8 , the method comprising administering to the subject the pharmaceutical composition of .10. The method of claim 9 , wherein the disease or disorder is a cell proliferative disease or disorder.11. The method of claim 9 , wherein the disease or disorder is cancer.12. A compound selected from compounds listed in Table 2 in the Specification that accompanies these claims.13. A pharmaceutical composition comprising any effective amount of the compound of and a pharmaceutical carrier claim 12 , excipient claim 12 , or diluent.14. A method for treating a disease or disorder in a subject in need thereof claim 13 , the method comprising administering to the subject the pharmaceutical composition of .15. The method of claim 14 , wherein the disease or disorder is a cell proliferative ...

Necrosis Inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

HUMAN PLASMA KALLIKREIN INHIBITORS

Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity. 2. The compound of claim 1 , wherein Rrepresents —OH claim 1 , —OR claim 1 , —NH claim 1 , —NHR claim 1 , —NRR claim 1 , alkyl claim 1 , aryl claim 1 , heteroaryl claim 1 , halo claim 1 , haloalkyl claim 1 , cycloalkyl claim 1 , —OC(O)R claim 1 , —NHC(O)R claim 1 , or —NRC(O)R; or two geminal occurrences of Rtaken together with the carbon to which they are attached represent —C(O)—; or two vicinal or geminal occurrences of Rtaken together form an optionally substituted fused or spirocyclic carbocyclic or heterocyclic ring.3. The compound of claim 2 , wherein Rrepresents —OH claim 2 , —OR claim 2 , —NH claim 2 , alkyl claim 2 , aryl claim 2 , halo claim 2 , haloalkyl claim 2 , cycloalkyl claim 2 , or —OC(O)R; and n is 1 or 2.4. The compound of claim 3 , wherein n is 1 and Rrepresents —OH claim 3 , —O((C-C)alkyl) claim 3 , —OC(O)((C-C)alkyl) claim 3 , —NH claim 3 , or (C-C)alkyl.511-. (canceled)12. The compound of claim 3 , wherein n is 2 and the two occurrences of Rare geminal.13. (canceled)14. The compound of claim 12 , wherein:{'sup': 1', 'c', '1, '(a) one occurrence of Rrepresents —OH or —OR; and the other occurrence of Rrepresents aryl or heteroaryl;'}{'sup': 1', '1, '(b) one occurrence of Rrepresents —OH or —OR; and the other occurrence of Rrepresents haloalkyl;'}{'sup': '1', '(c) both occurrences of Rare halo; or'}{'sup': '1', '(d) the two geminal occurrences of Rtaken together with the carbon to which they are attached represent —C(O)—.'}1517-. (canceled)18. The compound of claim 3 , wherein n is 2; the two occurrences of Rare vicinal; and the ...

HUMAN PLASMA KALLIKREIN INHIBITORS

Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity. 156-. (canceled)58. The method of claim 57 , wherein the disease or condition characterized by unwanted plasma kallikrein activity is selected from the group consisting of stroke claim 57 , inflammation claim 57 , reperfusion injury claim 57 , acute myocardial infarction claim 57 , deep vein thrombosis claim 57 , post fibrinolytic treatment condition claim 57 , angina claim 57 , edema claim 57 , angioedema claim 57 , hereditary angioedema claim 57 , sepsis claim 57 , arthritis claim 57 , hemorrhage claim 57 , blood loss during cardiopulmonary bypass claim 57 , inflammatory bowel disease claim 57 , diabetes mellitus claim 57 , retinopathy claim 57 , diabetic retinopathy claim 57 , diabetic macular edema claim 57 , diabetic macular degeneration claim 57 , age-related macular edema claim 57 , age-related macular degeneration claim 57 , proliferative retinopathy claim 57 , neuropathy claim 57 , hypertension claim 57 , brain edema claim 57 , increased albumin excretion claim 57 , macroalbuminuria claim 57 , and nephropathy.59. The method of claim 57 , wherein the disease or condition characterized by unwanted plasma kallikrein activity is angioedema.60. The method of claim 57 , wherein the disease or condition characterized by unwanted plasma kallikrein activity is hereditary angioedema.61. The method of claim 57 , wherein the disease or condition characterized by unwanted plasma kallikrein activity is stroke.62. The method of claim 57 , wherein the disease or condition characterized by unwanted plasma kallikrein activity is reperfusion injury.63. The ...

MASP-2 INHIBITORS AND METHODS OF USE

The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds. 1489-. (canceled)491. The compound or salt thereof of claim 490 , wherein the compound is of formula (I-1).492. The compound or salt thereof of claim 490 , wherein the compound is of formula (IIA).493. The compound or salt thereof of claim 490 , wherein the compound is of formula (IIB).494. The compound or salt thereof of claim 490 , wherein the compound is of formula (III).495. The compound or salt thereof of claim 490 , wherein the compound is of formula (IV).499. A small molecule compound with MASP-2 inhibitory activity claim 490 , for therapeutic use in the treatment of a MASP-2-associated disease or disorder claim 490 , wherein the compound has one or more of the following interactions (a) to (e):a) the compound binds via H-bonds with one or more of PRO 606, ASP 627, SER 628, ARG 630, SER 633, SER 654, GLY 656, SER 657, CYS 660 and GLN 665 in MASP-2;b) the compound binds via ionic or electrostatic interactions or hydrogen bonding to one or more of ASP 627 and ARG 630 in MASP-2;c) the compound interacts via a water molecule in MASP-2 to one or more of TYR 602, TYR 607, ASP 627, SER 628, SER 657, ASN 659, GLU 662, TRP 655, GLY656, CYS660, GLN 665, TYR 666, VAL 668, and ARG 630 in MASP-2;d) the compound interacts via π-π interactions with one or more of PHE 529, TYR 607, and TRP 655 in MASP-2; ande) the compound interacts via van der Waals contacts to one or more of ALA 468, ALA 469, HIS 483, ASP 526, ALA 527, GLY 528, PHE 529, LEU 575, PRO 606, TYR 607, PRO 608, SER 611, ASP 627, SER 628, CYS 629, ARG 630, GLY 631, ASP 632, SER 633, GLY 634, GLY 635, VAL 653, SER 654, TRP 655, GLY656, SER 657, MET 658, ASN 659, CYS 660, GLN 665, GLY 667, and TYR 669 in MASP-2,wherein the compound is not an endogenous MASP-2 ligand.500. A small molecule compound for use in the treatment of MASP-2-associated diseases ...

Chemical conjugates of evans blue derivatives and their use in the production of long-acting therapeutics

The present invention is directed to a compound of Formula I or Formula II or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: Formula I Formula II The compounds of Formula I may be covalently bonded to a therapeutic compound or fragment thereof to provide a compound of Formula II and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.

Lysosome-cleavable linker

The present invention relates to a linker for forming conjugates of a protein or peptide with a therapeutically active agent and which comprise a thiomaleamic acid moiety that is susceptible to cleavage under the pH conditions prevalent in the lysosome.

임의적으로 베타-위치가 치환된 알파-아릴알킬기의 제거를통해 3급 아미드 화합물로부터 2급 아미드 화합물을제조하는 방법

본 발명은 임의적으로 β-위치가 치환된 α-아릴알킬기가 결합된 3급 아미드 화합물을 유기용매 중에서 양성자산과 반응시킴으로써 이 α-아릴알킬기가 제거된 2급 아미드 화합물을 고순도 및 고수율로 간편하게 제조하는 방법에 관한 것이다.

Mct4的杂环抑制剂

本文披露了用于治疗MCT4介导的疾病例如增殖性和炎性疾病的化合物和组合物，其具有式(I)的结构。还提供了抑制人或动物受试者中的MCT4活性的方法。

Способ тионирования и тионирующий реагент

1. Способ превращения группы >C=O (I) в соединении в группу >C=S (II) или в таутомерную форму группы (II) в реакции, дающей тионированный продукт реакции, при использовании кристаллического PS·2CHN в качестве тионирующего реагента.2. Способ по п.1, в котором тионирующий реагент и соединение взаимодействуют друг с другом в жидкой для соединения и тионирующего реагента среде растворителя.3. Способ по п.2, в котором жидкая среда растворителя включает пиридин, С1-С3алкилнитрил, циклический сульфон и/или С1-С3диалкилсульфон.4. Способ по п.2, в котором жидкая среда растворителя включает пиридин, сульфолан, диметилсульфон и/или ацетонитрил.5. Способ по п.1, в котором реакцию проводят при температуре 60-180°С.6. Способ по п.2, в котором реакцию проводят при температуре 60-180°С.7. Способ по п.3, в котором реакцию проводят при температуре 60-180°С.8. Способ по п.4, в котором реакцию проводят при температуре 60-180°С.9. Способ по п.1, в котором реакцию проводят при температуре 115-175°С.10. Способ по любому из пп.1-9, в котором соединение включает группу (I), которая присутствует в виде амидной функциональной группы.11. Способ по любому из пп.1-9, в котором соединение включает группу (I), которая присутствует в виде кетонной функциональной группы.12. Способ по любому из пп.1-9, в котором тионирующий реагент используют с мольным отношением к реагирующей группе (I) 1 моль PS·2CHN на 1-4 моля группы (I).13. Способ по п.10, в котором тионирующий реагент используют с мольным отношением к реагирующей группе (I) 1 моль PS·2CHN на 1-4 моля группы (I).14. Способ по п.11, в котором тионирующий реагент используют с мольным отношением к реагирующей группе (I) 1 моль PS·2CHN на 1-4 моля группы (I).15. Способ по любому из пп.1-9, � РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07B 45/00 (13) 2013 140 771 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2013140771/04, 03.02.2012 (71) Заявитель(и): ВИРОНОВА ТИОНЕЙШЕН АБ (SE) ...

Apoptosis promoters

Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.

Apoptosis promoters

Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.

Apoptosis promoters

Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.

Apoptosis promoters

Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.

Coferons and methods of making and using them

Cyclic amides as metap-2 inhibitors

하기 화학식 (I) 의 화합물은 메티오닌 아미노펩티다아제의 억제제이며, 종양의 치료에 이용될 수 있다: [식 중, R 1 , R 3 , R 5 , R 6 , R 7 , R, X 및 Y 는 청구항 제 1 항에 제시된 의미를 가짐]. Compounds of formula (I) are inhibitors of methionine aminopeptidase and can be used to treat tumors: Wherein R 1 , R 3 , R 5 , R 6 , R 7 , R, X and Y have the meaning set forth in claim 1.

Benzene ring derivative and application thereof in medicine

本发明涉及一种苯环衍生物及其制备方法和在医药上的应用，具体而言涉及如通式(A)所示的苯环衍生物，或者其立体异构体、溶剂化物、代谢产物、前药、药学上可接受的盐或者共晶，其制备方法、包含其的药物组合物以及本发明化合物或者组合物在中枢神经领域的用途，其中，通式(A)中各取代基的定义与说明书的定义相同。

Method of thionation and thionizing reagent

FIELD: chemistry. SUBSTANCE: invention relates to a method of converting group >C=O (I) in a compound into group >C=S (II) or into a tautomeric form of group (II) in a reaction resulting in a thionated reaction product when using the crystalline P 2 S 5 ·2C 5 H 5 N as a thionizing reagent, as well as to a thionizing agent, that is a crystalline P 2 S 5 ·2C 5 H 5 N and has the melting point of 167-169 °C. EFFECT: proposed is a novel method of converting group >C=O (I) in a compound into group >C=S (II). 22 cl, 3 tbl, 4 dwg, 7 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 605 412 C2 (51) МПК C07B 45/00 (2006.01) C07D 213/06 (2006.01) C07C 325/02 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2013140771/04, 03.02.2012 (24) Дата начала отсчета срока действия патента: 03.02.2012 Приоритет(ы): (30) Конвенционный приоритет: (72) Автор(ы): ПЕТЕРСОН Биргитта (SE), ХАСИМБЕГОВИК Ведран (SE), СВЕНСОН Пер. Х. (SE), БЕРГМАН Ян (SE) R U (73) Патентообладатель(и): ВИРОНОВА ТИОНЕЙШЕН АБ (SE) 04.02.2011 EP 11153421.0; 04.02.2011 US 61/439,522 (43) Дата публикации заявки: 10.03.2015 Бюл. № 7 C 2 C 2 (56) Список документов, цитированных в отчете о поиске: Fluck and Binder, ZEITSCHRIFT FUR ANORGANISCHE UND ALLGEMEINE CHEMIE, 1967, Vol:354, Nr:3-4, стр. 113 - 129. Meisel and Grunze, ZEITSCHRIFT FUR ANORGANISCHE UND ALLGEMEINE CHEMIE, 1968, Vol:360, Nr:1968, стр. 277 - 283. KLINGSBERG E, PAPA D, Journal of the American Chemical Society, 1951, Vol:73, Nr:10, стр. 4988 - 4989. RU 2265596 C2, 10.12.2005. (85) Дата начала рассмотрения заявки PCT на национальной фазе: 04.09.2013 2 6 0 5 4 1 2 (86) Заявка PCT: R U 2 6 0 5 4 1 2 (45) Опубликовано: 20.12.2016 Бюл. № 35 EP 2012/051864 (03.02.2012) (87) Публикация заявки PCT: WO 2012/104415 (09.08.2012) Адрес для переписки: 109012, Москва, ул. Ильинка, 5/2, ООО "Союзпатент" (54) СПОСОБ ТИОНИРОВАНИЯ И ТИОНИРУЮЩИЙ РЕАГЕНТ (57) Реферат: Изобретение относится к способу ...

Phenoxy-pyrrolidine derivative and its use and compositions

본 발명은 화합물 2-(4-(히드록시메틸)페녹시)-1-(3-(2-(트리플루오로메틸)페녹시)피롤리딘-1-일)에타논), 이의 스테아로일 CoA 디새튜라아제의 억제제로서의 용도 및 이 화합물을 함유하는 약학 조성물에 관한 것이다. The present invention relates to compound 2- (4- (hydroxymethyl) phenoxy) -1- (3- (2- (trifluoromethyl) phenoxy) pyrrolidin-1-yl) ethanone), stearose thereof It relates to the use of one CoA desaturase as an inhibitor and to a pharmaceutical composition containing the compound.

Novel method for obtaining intermediate compounds, applied in obtaining nep inhibitors

FIELD: chemistry. SUBSTANCE: invention relates to novel method of obtaining intermediate compounds, used for obtaining NEP inhibitors or their prodrugs, in particular NEP inhibitors, containing structure of γ-amino-δ-biphenyl-α-methylalkane acid or acid ester, such as ethyl ester of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino (2R)methylbutanic acid or its salt. EFFECT: increase of method efficiency. 15 cl, 1 dwg, 2 tbl, 8 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 227/22 C07C 269/06 C07C 271/22 C07D 207/38 C07D 207/27 (13) 2 573 824 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2013112856/04, 22.08.2011 (24) Дата начала отсчета срока действия патента: 22.08.2011 Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 27.09.2014 Бюл. № 27 (73) Патентообладатель(и): НОВАРТИС АГ (CH) R U 23.08.2010 CN PCT/CN2010/076249 (72) Автор(ы): ХУК Дэвид (CH), РИСС Бернхард (CH), ЧЖОУ Цзяньгуан (CN), ЛИ Юньчжун (CN), БАППЕРТ Эрхард (CH) (45) Опубликовано: 27.01.2016 Бюл. № 3 C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 25.03.2013 (86) Заявка PCT: 2 5 7 3 8 2 4 EP 2011/064411 (22.08.2011) R U 2 5 7 3 8 2 4 (56) Список документов, цитированных в отчете о поиске: RU 2469019 C2, 10.12.2012. US 5217996 A, 08.06.1993. WO 2009090251 A2, 23.07.2009. WO 2008083967 A2, 17.07.2008. WO 2008138561 A1, 20.11.2008. KSANDER G M ET AL: "DICARBOXYLIC ACID DIPEPTIDE NEUTRAL ENDOPEPTIDASE INHIBITORS", JOURNAL OF MEDICINAL CHEMISTRY, 1995, vol. 38, no. 10, pages 1689-1700. (87) Публикация заявки PCT: WO 2012/025502 (01.03.2012) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" (54) НОВЫЙ СПОСОБ ПОЛУЧЕНИЯ ПРОМЕЖУТОЧНЫХ СОЕДИНЕНИЙ, ИСПОЛЬЗУЕМЫХПРИ ПОЛУЧЕНИИИНГИБИТОРОВ NEP (57) Реферат: Изобретение относится к новому способу кислоты, таких как этиловый эфир ...

Benzidine derivative, method for preparing same, and pharmaceutical composition containing benzidine derivative for treating liver disease caused by hepatitis c virus

본 발명은 C형 바이러스에 대하여 항바이러스 활성을 갖는 화합물, 이의 광학 이성질체, 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 C형 간염 바이러스에 의한 간질환의 예방 또는 치료용 약학적 조성물에 관한 것으로, 본 발명에 따른 벤지딘 유도체는 C형 간염 바이러스에 대한 항바이러스 활성이 우수하고 생체 내에서 뛰어난 약리활성을 나타냄으로써, 이를 유효성분으로 포함하는 약학적 조성물은 C형 간염 바이러스에 의해 발병되는 급성 C형 간염, 만성 C형 간염, 간경변, 간세포성 암과 같은 간질환 예방 또는 치료용 약학적 조성물로 유용하게 사용될 수 있다.

Androgen receptor modulators and methods for their use

Compounds having a structure of formula (I), (I-A), (Ia)-(Ie), (A)-(E), and (II) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of disorders including prostate cancer are also provided.

Phenoxy-pyrrolidine derivative and its use and compositions

本发明公开了化合物2-(4-(羟甲基)苯氧基)-1-(3-(2-(三氟甲基)苯氧基)吡咯烷-1-基)乙酮、其作为硬脂酰辅酶A去饱和酶的抑制剂的应用，以及包含该化合物的药物组合物。

Composition for silver nano particle preparation and silver nano particle preparation method using the same

본 발명은 은 나노입자 제조용 화합물 및 이를 이용한 은 나노입자의 제조방법에 관한 것으로서, 상기 은 나노입자 제조용 화합물은 하기 [화학식 1] 내지 [화학식 4]으로 표시되고, 이를 이용하여 환원제나 분산제를 따로 사용할 필요 없이 안정하게 은 나노입자를 제조할 수 있으며, 또한 제조된 은 나노입자를 용매 등으로부터 쉽고 빠르게 분리할 수 있는 장점이 있고, 제조하고자 하는 은 나노입자의 모양, 크기 및 입도를 조절할 수 있어 항균 소재, 은 나노입자가 운반체로 사용되는 촉진수송 기체분리막, 은 나노입자가 분산된 전해질을 사용하는 태양전지 및 각종 센서 등 다양한 분야에 활용할 수 있다. 상기 [화학식 1] 내지 [화학식 4]에서, n은 1 내지 18의 정수이다. The present invention relates to a compound for preparing silver nanoparticles and a method for preparing silver nanoparticles using the silver nanoparticle. The silver nanoparticle preparation compound is represented by the following formulas (1) to (4) The silver nanoparticles can be stably prepared without the need to use them and the silver nanoparticles can be easily and quickly separated from the solvent and the like, and the shape, size and size of silver nanoparticles to be prepared can be controlled Antimicrobial materials, facilitated transport gas separation membranes in which silver nanoparticles are used as carriers, solar cells using an electrolyte in which silver nanoparticles are dispersed, and various sensors. In the above Chemical Formulas 1 to 4, n is an integer of 1 to 18.

Method for producing aminophenoxy derivatives

FIELD: medicine. SUBSTANCE: desired products have formula I where B, Cy, A, R 3 and R 4 have appropriate values. 4-alkoxyphenyl derivative having formula II where B, Cy, A and X are as mentioned above is used as reagent 1. Amine of HNR 3 R 4, formula where R 3 , R 4 have appropriate values is used as reagent 2. Desired product is isolated in free state or as salt, if desired said salt may be converted into base, and if it is desired base is converted into salt. Structural formula of I and II are as follows: 6995$ 0с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) 307/38//А 61 К 31/34, 31/38, 31/40 ВИ” 2 032 669 ' (51) МПК 13) Сл С 070 209/10, 307/82, 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 4830121/04, 15.06.1990 (30) Приоритет: 07.08.1987 Ш$ 082554 (46) Дата публикации: 10.04.1995 (56) Ссылки: Патент США М 4117128, кл. С 070 307/82, опублик. 1978.Патент Франции М 2341578, кл. С 070 471/04, опублик.1977... Мед. Спет. \. 1970, 13(3), с.359.Срит. ТВег, М, ТЭ ТР, Г (5), с.369.)3п9. Спет., 1977, М, 59(283), с.3-23.Ныегосусе$., 1984, М, 2265), с.1235.Ечг. у. Мед. Спет. Твег., 1977, М, 12(5), с.483.Патент Франции М 2400515, кл. С 070 307/68, опублик.1979 Патент США М 4220645, кл. С 070 41312, опублик.1980.Сваг!ег КВ. "Вгихе|ез Меа!са!", 1969, М 9, с.543...А.М.А., 1982, с.247, с.1911. (71) Заявитель: Санофи (ЕК) (72) Изобретатель: Жан Гюбэн[ВЕ], Пьер Шатлэн[ВЕ], Анри Иньон[ВЕ], Жан Люкшетти[ВЕ], Жан-Мари Маокс[ ВЕ], Жан-Ноэль Валла[ЕК] (73) Патентообладатель: Санофи (ЕК) (54) СПОСОБ ПОЛУЧЕНИЯ АМИНОФЕНОКСИПРОИЗВОДНЫХ (57) Реферат: Использование: в медицине в качестве средства, проявляющего ингибигующую активность в отношении транспортировки кальция, а также гипотензивную активность. Сущность изобретения: продукт - аминофеноксипроизводные ф-лы 1, где В, Су, А, Кзи К имеют соответствующие значения, или их солей. Соединения ф-лы | в дозе 5,89 - 0,12 проявляют анти - Альфа и Бэта эффекты 50% и более. Реагент 1: 4 - ...

Ion channel modulating activity II

Methods, compositions, dosing regimes, and routes of administration for the treatment or prevention of arrhythmias. In these methods, arrythmias (e.g. atrial fibrillation, atrial flutter, early afterdepolarizations and prolongation of QT interval) may be reduced or eliminated by administering ion channel modulating compounds to a subject in need thereof. The ion channel modulating compounds may be cycloalkylamine ether compounds, particularly cyclohexylamine ether compounds. Also described are compositions of ion channel modulating compounds and drugs which induce early afterdepolarizations, prolongation of QT interval and/or Torsades de Pointes.

Preparing process for pyrolidine derivatives

Pyrrolidine derivs. (I) are prepd. from the cpd. of formula (II) [X=halo and the ag. soln. of formula (III) [m=alkali metal; Z=O or S . Thus, a soln. of 5.64g (II) (X=Br) and 1.68g Na2CO3 in 20ml H2O is reacted with 40ml of (III)(M=Na; Z=O) soln. at 65-70≰C for 5hr. The reactant is extd. with CH2Cl2 at pH1.0 and evaporated in vacuo to give yellow syrup, which is treated with 1N H2SO4 and Zn powder, extd. with EtOAc, washed with satd. NaCl soln., dried on MgSO4, filtered, and concd. in vacuo. The concd. syrup is purified with EtOAc/hexane solvent and dried at 40≰C overnight to give 4.1g (I).

Composition for solving a cross-linked polymer

본 발명은 망상형 고분자 용해용 조성물에 관한 것으로서, 보다 상세하게는, 특정 고리형 아민과 특정 사슬형 아민 중 적어도 하나인 아민 화합물; 탄소수 1 내지 20의 불화알킬암모늄; 및 극성 비양성자성 용매를 포함함으로써, 망상형 고분자를 효과적으로 제거하는 망상형 고분자 용해용 조성물에 관한 것이다.

A thionation process and a thionating agent

티오화된 반응 산물을 수득하는 반응에서, 결정질 P 2 S 5 ·2C 5 H 5 N을 티오화제로서 사용함으로써 화합물의 >C=O (I)기를 >C=S (II)기 또는 상기 (II)기의 호변이성질체 형태로 변환시키는 방법이 개시된다. 결정질 P 2 S 5 ·2C 5 H 5 N인 티오화제가 개시된다.

HIV inhibiting pyrimidine derivative

This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR 4 or N; n is 0 to 4; Q is hydrogen or —NR 1 R 2 ; R 1 and R 2 are selected from hydrogen, hydroxy, C 1-12 alkyl, C 1-12 alkyloxy, C 1-12 alkylcarbonyl, C 1-12 alkyloxycarbonyl, aryl, amino, mono- or di(C 1-12 alkyl)amino, mono- or di(C 1-12 alkyl)aminocarbonyl wherein each C 1-12 alkyl may optionally be substituted; or R 1 and R 2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C 1-12 alkyl)aminoC 1-4 alkylidene; R 3 is hydrogen, aryl, C 1-6 alkylcarbonyl, optionally substituted C 1-6 alkyl, C 1-6 alkyloxycarbonyl,; and R 4 is hydroxy, halo, optionally substituted C 1-6 alkyl, C 1-6 alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R 5 is hydrogen or C 1-4 alkyl; L is optionally substituted C 1-10 alkyl, C 3-10 alkenyl, C 3-10 alkynyl, C 3-7 cycloalkyl; or L is —X 1 —R 6 or —X 2 -Alk-R 7 wherein R 6 and R 7 are optionally substituted phenyl; X 1 and X 2 are —NR 3 —, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O) 2 —; Alk is C 1-4 alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

HIV Inhibiting pyrimidine derivatives

This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR 4 or N; n is 0 to 4; Q is hydrogen or —NR 1 R 2 ; R 1 and R 2 are selected from hydrogen, hydroxy, C 1-12 alkyl, C 1-12 alkyloxy, C 1-12 alkylcarbonyl, C 1-12 alkyloxycarbonyl, aryl, amino, mono- or di(C 1-12 alkyl)amino, mono- or di(C 1-12 alkyl)aminocarbonyl wherein each C 1-12 alkyl may optionally be substituted; or R 1 and R 2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C 1-12 alkyl)aminoC 1-4 alkylidene; R 3 is hydrogen, aryl, C 1-6 alkylcarbonyl, optionally substituted C 1-6 alkyl, C 1-6 alkyloxycarbonyl,; and R 4 is hydroxy, halo, optionally substituted C 1-6 alkyl, C 1-6 alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R 5 is hydrogen or C 1-4 alkyl; L is optionally substituted C 1-10 alkyl, C 3-10 alkenyl, C 3-10 alkynyl, C 3-7 cycloalkyl; or L is —X 1 —R 6 or —X 2 —Alk—R 7 wherein R 6 and R 7 are optionally substituted phenyl; X 1 and X 2 are —NR 3 —, —NH—NH—, —N═N—, —O—, —S—, —S(═O)— or —S(═O) 2 —; Alk is C 1-4 alkanediyl; aryl is potionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical: for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

Method of preparing nitrocompound

This invention concerns compounds showing activity as histamine H 2 -receptor antagonists. The compounds of the invention are of Structure where Het is a substituted or unsubstituted, fully-unsaturated 5- or 6- membered heterocycle containing at least one nitrogen atom, or a furan or thiophene ring substituted by a substituted or unsubstituted aminoalkyl group; Z is sulphur, methylene or oxygen; m is 0, 1 or 2, n is 2 or 3 with m + n being 3 or 4; and B is a substituted or unsubstituted alkanediyl group or a 2-substituted-2-aza-1,3-propanediyl group; and acid addition salts thereof. The compounds of the invention can be prepared by reacting a compound of formula Het(CH 2 ) m Z(CH 2 ) n NH 2 or Het(CH 2 ) m Y (where Y is a group displaceable by a mercaptan) with an appropriate 2-subst)tuted-3-nitro-heterocyde. The compositions of the invention contain at least one compound of the invention and a pharmaceutical carrier.

Method of obtaining 5-biphenyl-4-amino-2-methylpentanoic acid

FIELD: chemistry. SUBSTANCE: invention relates to novel compounds of formula or their salts, where R1 stands for H, C1-C6-alkylcarbonyl, C1-C6-alkoxycarbonyl, SiR7R8R9, where R7, R8, R9 independently on each other stand for C1-C6-alkyl, phenyl-C1-C2-alkoxycarbonyl, or R1 stands for trimethylsilylethoxymethyl (SEM), C1-C2-alkyl, with the latter being substituted with C6-C10-aryl, preferably phenyl, or a heterocyclic group, which represents a monocyclic saturated ring system with 5 ring atoms, one of which is nitrogen, represents hydrogen or a nitrogen-protective group. Various methods of obtaining the said compounds and their application for obtaining a NEO-inhibitor, in particular, in obtaining ethyl ether of N-(3-carboxyl-1-oxopropyl)-(4S)-(n-phenylphenylmethyl)-4-amino-(2R)-methylbutyric acid or its salts are described. EFFECT: obtaining novel compounds. 67 cl, 12 dwg, 61 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 207/26 C07D 207/28 C07D 207/38 C07D 207/267 C07D 207/27 C07D 207/277 ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 207/44 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07C 227/22 C07C 229/34 C07F 7/18 (12) ОПИСАНИЕ (21)(22) Заявка: (13) 2 530 900 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2009130534/04, 10.01.2008 (24) Дата начала отсчета срока действия патента: 10.01.2008 12.01.2007 EP 07100451.9 (45) Опубликовано: 20.10.2014 Бюл. № 29 (56) Список документов, цитированных в отчете о поиске: J.Med.Chem. 1995, 38, 1689-1700 (см. прод.) (73) Патентообладатель(и): НОВАРТИС АГ (CH) (85) Дата начала рассмотрения заявки PCT на национальной фазе: 12.08.2009 2 5 3 0 9 0 0 (43) Дата публикации заявки: 20.02.2011 Бюл. № 5 R U Приоритет(ы): (30) Конвенционный приоритет: (72) Автор(ы): Дейвид ХУК (CH), Томас РУХ (CH), Бернхард РИСС (FR), Бернхард ВИТФЕЛЬД (DE), Готтфрид ЗЕДЕЛЬМАЙЕР (DE), Маттиас НАПП (DE), Маркус БЭНЦИГЕР (CH), Стивен ХОКЕР (GB), Лех ЦИШЕВСКИЙ (US), Лиладхар Мурлидхар УЭЙКОУЛ (US) 2 5 3 0 9 0 ...

VLA-4 inhibitor compounds

Compounds that selectively inhibit the binding of ligands to α4β1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are pharmaceutical compositions, methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion, which involve compounds of Formula I.

Vla-4 inhibitor compounds

Patent RU2019115930A3

ВУ’ 2019115930” АЗ Дата публикации: 05.05.2021 Форма № 18 ИЗ,ПМ-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 2019115930/04(030330) 12.12.2017 РСТ/О$2017/065864 12.12.2017 Приоритет установлен по дате: [Х] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [ ] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 62/433,113 12.12.2016 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) Гетероциклические ингибиторы МСТ4 Заявитель: ВЕТТОРЕ, ЛЛС, 0$ 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) (070 231/12 (2006.01) (070 405/12 (2006.01) Аб1Р 19/02 (2006.01) (070 403/04 (2006.01) С07р 409/04 (2006.01) Аб1Р 35/00 (2006.01) (070 403/06 (2006.01) С07О 417/04 (2006.01) С07р 401/06 (2006.01) Аб1К 31/415 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07р 231/12 С07О 405/12 Аб1Р 19/02 С07О 403/04 С07Р 409/04 Аб1Р 35/00 С07Р 403/06 С07р 417/04 С07РО 401/06 (2006.0 0)ГАбТК 31/415 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 ...

Method of synthesis of aminoalkoxyphenyl-derivatives or their pharmaceutically acceptible salts

Использование: в качестве антиадре- нэргических средств в медицине. Сущность изобретени : продукт аминоалкоксифе- нильные производные общей формулы Су- B-fcC&deg;C-C-C C-0-A-NRiR2, где В - S- или SOa-rpynna; A - линейный или разветвленный алкиленовый радикал, содержащий 2-5 атомов углерода; RI - Ci-Ci-алкил или AlkАг , где Alk - одинарна  св зь или Ci-Cs-ал- килен; Аг-- пиридил, фенил, 2,3-метиленди- оксифенил или фенил, замещенный одним или несколькими заместител ми, которые могут быть как одинаковыми, так и различными , выбранными из атомов галогена, низших алкильных или алкоксильных групп; R2 - водород или Ст-С алкил, или Rt и R2 вместе образуют Сз-Се-алкилен; Су- инодо- линин-3-ил, индолил, бёнзофурил, бензоти- енил, хинолинил, пирроло (1,2-а) пиридил, 4,5-дигидрофуранил или фенил, при условии , что когда Су - бензо(Ь) фурил или бензо (Ь) тиенил, то В  вл етс  502-гру.ппой, а RI - Afk-Ar или же фармацевтически приемлемые соли. Реагент 1: 4-оксифенил формулы Су-В-СбН4ОН. Реагент 2: X-A-NRiRa, где Х- галоген, С|-С4-алкилсульфонилокси, или С1 С4-арилсульфонилоксигруппа. Услови  реакции:- в присутствии щелочного агента в среде пол рного растворител  при температуре от комнатной до температуры кипени  реакционной смеси. 3 табл. i .- , о ел G

Intermediates useful for the synthesis of pyrrolobenzodiazepines

A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.

Synthesis method and intermediates useful in the preparation of pyrrolobenzodiazepines

A compound of formula I wherein: R7 is selected from: ORA, where RA is selected from C1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH2; -CH2-O-C(=O)Me; R8 is OProt°, where Prot° is a silicon-based oxygen protecting group orthogonal to Rc; R9 is selected from H, methyl and methoxy; Rs is selected from CF3, (CF2)3CF3, CH3 and (formula 2) and Rc is selected from: (i) -C(=O)-ORC1, where RC1 is a saturated C1-4 alkyl group; (ii) -CH2-O-C(=0)RC2, where RC2 is methyl or phenyl; (iii) -CH2-O-Si-(RSi1)(RSi2)(RSi3), where RSi1, RSi2, RSi3 are independently selected from C1-6 a saturated alkyl group and a phenyl group; and (iv) -C(-YRC3)(-YRC4) where each Y is independently O or S, and where RC3 and RC4 are independently a saturated C1-4 alkyl group, or together form a C2-3 alkylene.

Synthesis method and intermediates

Synthesis method and intermediates useful in the preparation of pyrrolobenzodiazepines

A compound of formula I wherein: R 7 is selected from: OR A , where R A is selected from C 1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH 2 ; —CH 2 —O—C(═O)Me; R 8 is OProt o , where Prot o is a silicon-based oxygen protecting group orthogonal to R c ; R 9 is selected from H, methyl and methoxy; R s is selected from CF 3 , (CF 2 ) 3 CF 3 , CH 3 and (formula 2) and R c is selected from: (i) C(═O)—OR C1 , where R C1 is a saturated C 1-4 alkyl group; (ii) —CH 2 —O—C(═O)R C2 , where R C2 is methyl or phenyl; (iii) CH 2 —O—Si—(R Si1 )(R Si2 )(R Si3 ), where R Si1 , R Si2 , R Si3 are independently selected from C 1-6 a saturated alkyl group and a phenyl group; and (iv) C(—YR C3 )(—YR C4 ) where each Y is independently O or S, and where R C3 and R C4 are independently a saturated C 1-4 alkyl group, or together form a C 2-3 alkylene.

Synthesis method and intermediates useful in the preparation of pyrrolobenzodiazepines

A compound of formula I wherein: R

Synthesis method and intermediates useful in the preparation of pyrrolobenzodiazepines

A compound of formula I wherein: R 7 is selected from: OR A , where R A is selected from C 1-4 saturated alkyl, optionally substituted by phenyl, which may bear a chloro substituent, pyridyl and furanyl; chloro; NH 2 ; -CH 2 -O-C(=O)Me; R 8 is OProt°, where Prot° is a silicon-based oxygen protecting group orthogonal to R c ; R 9 is selected from H, methyl and methoxy; R s is selected from CF 3 , (CF 2 ) 3 CF 3 , CH 3 and (formula 2) and R c is selected from: (i) -C(=O)-OR C1 , where R C1 is a saturated C 1-4 alkyl group; (ii) -CH 2 -O-C(=0)R C2 , where R C2 is methyl or phenyl; (iii) -CH 2 -O-Si-(R Si1 )(R Si2 )(R Si3 ), where R Si1 , R Si2 , R Si3 are independently selected from C 1-6 a saturated alkyl group and a phenyl group; and (iv) -C(-YR C3 )(-YR C4 ) where each Y is independently O or S, and where R C3 and R C4 are independently a saturated C 1-4 alkyl group, or together form a C 2-3 alkylene.

Intermediates useful for the synthesis of pyrrolobenzodiazepines

A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.

Peptides capable of inhibiting the activity of HIV protease, their preparation and their use

Nitric oxide synthase inhibitors derived from cyclic amidines

Compounds having formula (I) wherein R1, R5, R6 and R7 are hydrogen or certain specified substituents; R8 and R9 are independently hydrogen, hydroxy or alkoxy; and X, A and B are independently NR2, O, S, SO, SO2, CH=CH or (CH2)p, p being 0-6; are useful as nitric oxide synthase inhibitors.

MASP-2 inhibitors and methods of use

本公开内容尤其提供具有MASP‑2抑制活性的化合物、此类化合物的组合物以及制备和使用此类化合物的方法。

Process for preparing a protected 4-aminomethyl-pyrrolidin-3-one

A process for preparing a compound of formula (1) in which P1 and P2 are protecting groups; comprising a) reaction of a compound of formula (5) wherein P1 is as defined for formula (1); with a Raney-nickel catalyst in a solvent under hydrogen to produce a compound of formula (6) wherein P1 is as defined for formula (1); b) protecting the amino group to produce a compound of formula (7) wherein P1 and P2 are as defined for formula (1); and c) selective reduction of the double bond to produce the compound of formula (1).

NOVEL N-BENZOYL PROLINE DERIVATIVES, PROCESS FOR PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

Composés de formule générale (I): (CF DESSIN DANS BOPI) où A, R1 , R2 , R3 , R4 , R5 et R6 sont définis dans la description. Médicaments. Compounds of general formula (I): (CF DRAWING IN BOPI) where A, R1, R2, R3, R4, R5 and R6 are defined in the description. Medicines.

Method of obtaining 4-(polyalkoxyphenyl)-2-pyrrolidones

2-BENZYL-PYRROLIDINES, PROCESS FOR THEIR PREPARATION AND MEDICINAL PRODUCT CONTAINING THESE COMPOUNDS

L'invention concerne des 2-benzyl-pyrrolidines substituées ainsi que les dérivés alkylpyrrolidinium quaternaires correspondants et leurs sels d'addition avec les acides. Ces composés peuvent être préparés par réduction de 2-benzyl-pyrrolidines correspondantes, par introduction d'une fonction chimique dans des 2-benzyl-pyrrolidines correspondantes ou réduction de N-acyl-2-benzyl-pyrrolidines. Ces composés sont utilisés comme médicaments agissant sur le système nerveux central, la tension et les états douloureux des humains et des animaux à sang chaud. The invention relates to substituted 2-benzyl-pyrrolidines as well as the corresponding quaternary alkylpyrrolidinium derivatives and their addition salts with acids. These compounds can be prepared by reduction of corresponding 2-benzyl-pyrrolidines, by introduction of a chemical function into corresponding 2-benzyl-pyrrolidines or reduction of N-acyl-2-benzyl-pyrrolidines. These compounds are used as drugs for central nervous system, blood pressure and pain conditions in warm-blooded humans and animals.

Protease inhibitors

This invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, which are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in whi ch inhibition of bone loss is a factor.

OXOAMINOACID DERIVATIVES, MANUFACTURING METHOD AND PHARMACEUTICAL COMPOSITION

DERIVE D'OXOAMINOACIDE REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE A EST UNE SIMPLE LIAISON, OU -CH-, -CH-CH-, CHCH, B EST UNE SIMPLE LIAISON OU -CH-, X EST -CH- OU UN ATOME O OU S, OU UN GROUPE NR, R EST H, OU UN ALKYLE INFERIEUR, R EST H OU UN ALCANOYLE INFERIEUR OU UN BENZOYLE, R EST H, UN ALKYLE INFERIEUR EVENTUELLEMENT SUBSTITUE. APPLICATION COMME MEDICAMENT POUR LE TRAITEMENT DE L'HYPERTENSION. OXOAMINOACID DERIVATIVE RESPONDING TO THE FORMULA: (CF DRAWING IN BOPI) IN WHICH A IS A SINGLE BOND, OR -CH-, -CH-CH-, CHCH, B IS A SINGLE BOND OR -CH-, X IS -CH - OR AN ATOM O OR S, OR A GROUP NR, R IS H, OR A LOWER ALKYL, R IS H OR A LOWER ALKANOYL OR A BENZOYL, R IS H, A LOWER ALKYL POSSIBLY SUBSTITUTED. APPLICATION AS A MEDICINE FOR THE TREATMENT OF HYPERTENSION.

PROCESS FOR THE PREPARATION OF PYRROLIDINE DERIVATIVES

Patent FR2537133B1

NOVEL DERIVATIVES OF (PIPERAZINYL-1) -5 PYRROLIDINE, THEIR PREPARATION AND THE MEDICINAL PRODUCTS CONTAINING THEM

NOUVEAUX DERIVES DE FORMULE GENERALE I DANS LAQUELLE X EST OXYGENE OU SOUFRE, R EST HYDROGENE, ALCOYLE 1 A 4 C OU BENZYLE, Y, IDENTIQUES OU DIFFERENTS SONT HYDROGENE, HALOGENE, ALCOYLE, ALCOYLOXY, ALCOYTHIO, ALCOYL-CARBONYLE, NITRO, AMINO, ALCOYLCARBONYLAMINO, ALCOYLAMINO, DIALCOYLAMINO, DIMETHYLSULFAMOYLE, ALCOYLSULFINYLE, ALCOYLSULFONYLE, CARBOXY, ALCOYLOXYCARBONYLE, CYANO, TRIFLUOROMETHYLE, HYDROXY, MERCAPTO, ALCOYLCARBONYLOXY, ALCOYLCARBONYLTHIO OU METHYLENEDIOXY, ET N EST EGAL A 0, 1, 2 OU 3. CES NOUVEAUX DERIVES SONT UTILES COMME ANTIDEPRESSEURS. NEW DERIVATIVES OF GENERAL FORMULA I IN WHICH X IS OXYGEN OR SULFUR, R IS HYDROGEN, ALCOYL 1 TO 4 C OR BENZYL, Y, IDENTICAL OR DIFFERENT ARE HYDROGEN, HALOGEN, ALCOYL, ALCOYLOXY, ALCOYTHIO, ALITROYL-CARB, ALCOYL-CARR alkylcarbonylamino, alkylamino, dialkylamino, dimethylsulfamoyl, alkylsulphinyl, alkylsulphonyl, cARBOXY, alkyloxycarbonyl, cYANO, tRIFLUOROMETHYL, hYDROXY, mERCAPTO, alkylcarbonyloxy, methylenedioxy ALCOYLCARBONYLTHIO OR, AND SHALL N 0, 1, 2 OR 3 ARE THESE DERIVATIVES USEFUL AS ANTIDEPRESSANTS .

Delta1-pyrroline derivatives

Delta1-pyrroline derivatives

Patent JPS6011028B2

Method for preparing protected 4-aminomethyl-pyrrolidone-3-on

본 발명은 제 1 단계에서 하기 화학식 5의 화합물을 용매중에서 수소압력하에 라니-니켈 촉매와 반응시켜 하기 화학식 6의 화합물을 제조하고, 제 2 단계에서 염기 존재하에 용매중에서 화학식 6 화합물의 아미노기를 보호기화 반응시켜 하기 화학식 7의 화합물을 제조한 후, 제 3 단계에서 화학식 7의 화합물을 용매중에서 수소압력하에 금속 촉매와 반응시켜 이중결합을 선택적으로 환원시킴을 특징으로 하여 퀴놀론계 항생제를 합성하는데 필수적으로 사용되는 중간체인 하기 화학식 1의 보호된 4-아미노메틸-피롤리딘-3-온을 제조하는 방법 및 이 방법을 수행하는데 중간체로서 생성되는 신규한 화학식 6 및 7의 화합물에 관한 것이다: 상기식에서 P 1 및 P 2 는 각각 독립적으로 아세틸, t-부톡시카보닐 또는 피발로일을 나타낸다.

NEW IMINO COMPOUNDS USEFUL AS MEDICINAL PRODUCTS AND THEIR PREPARATION PROCESS

Carboxyl-thio-pyrrolidinyl beta-lactam derivatives and their preparation.

MERCOPTOACYLATED DERIVATIVES OF PROLINE AND PIPECOLIC ACID WITH CETONIC FUNCTION WITH ANTI-HYPERTENSIVE ACTION

COMPOSES DE FORMULE: (CF DESSIN DANS BOPI) AINSI QUE LEURS SELS PHYSIOLOGIQUEMENT ACCEPTABLES, DANS LA FORMULE DESQUELS: R EST UN ATOME D'HYDROGENE OU UN RADICAL ALKYLE INFERIEUR; R ET R SONT CHOISIS INDEPENDAMMENT ENTRE LES ATOMES D'HYDROGENE ET LES RADICAUX ALKYLE INFERIEUR, ALKYLTH CES COMPOSES SONT UTILES POUR LE TRAITEMENT DE L'HYPERTENSION. COMPOUNDS OF THE FORMULA: (CF DRAWING IN BOPI) AS WELL AS THEIR PHYSIOLOGICALLY ACCEPTABLE SALTS, IN THE FORMULA IN WHICH: R IS A HYDROGEN ATOM OR A LOWER RADICAL ALKYL; R AND R ARE SELECTED INDEPENDENTLY BETWEEN HYDROGEN ATOMS AND LOWER ALKYL RADICALS, ALKYLTH THESE COMPOUNDS ARE USEFUL FOR THE TREATMENT OF HYPERTENSION.

Lactam derivatives

내용 없음. No content.

2-BENZYL-PYRROLIDINES, PROCESS FOR THEIR PREPARATION AND MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS

Process for preparing a protected 4-aminomethyl-pyrrolidin-3-one

A process for preparing a compound of formula (1) in which P1 and P2 are protecting groups; comprising a) reaction of a compound of formula (5) wherein P1 is as defined for formula (1); with a Raney-nickel catalyst in a solvent under hydrogen to produce a compound of formula (6) wherein P1 is as defined for formula (1); b) protecting the amino group to produce a compound of formula (7) wherein P1 and P2 are as defined for formula (1); and c) selective reduction of the double bond to produce the compound of formula (1).

METHOD OF PRODUCING NEW CYCLIC IMINE COMPOUNDS METHOD OF PRODUCING NEW CYCLIC IMINE COMPOUNDS

Tetrapeptide analogs

Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.

Patent FR2305434B1

Therapeutic compounds

Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y, A, B, and J are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Method for the preparation of n-substituted 4-ketoproline derivatives

Method for the preparation of N-protected 4-ketoproline derivatives of formula I Formula I by oxidation of the corresponding N-protected 4-hydroxyproline derivatives of formula III Formula III using the system TEMPO (2,2,6,6-tetramethylpiperidinyl oxy free radical)/NaOCl.

Pyrrolidines and their use as attractant for ants

1501929 Attractants for ants NEDERLANDS APPLIED SCIENTIFIC RESEARCH FOR INDUSTRY TRADE & COMMERCE 27 June 1975 [28 June 1974] 27281/75 Heading A5E [Also in Division C2] The invention comprises an attractant preparation for ants comprising as an active ingredient at least one compound of the general formula: wherein R is an alkyl radical having from 1 to 13 carbon atoms. Example III describes the biological properties of 2-(5'-n-hexenyl)-5- n pentyl pyrrolidins.

Method for preparing ring-opening impurity of carbapenems

本发明涉及一种碳青霉烯类抗生素的开环杂质的制备方法，该开环杂质具有式(Ⅰ)的结构：其中R表示美罗培南支链、厄他培南支链或多尼培南支链；包括步骤如下：(1)将碳青霉烯类抗生素加入碱性溶液中，搅拌反应1～4h；(2)调节pH至6.0～9.0；(3)将物料冻干，即得。该方法操作简单，反应时间短，产物纯度在95％以上，可直接作为对照品对碳青霉烯类产品开环杂质进行定性定量研究，从而更有效地控制产品质量。