КРИСТАЛЛЫ

... 1. Форма-I кристалла 2-{4-[N-(5,6-дифенилпиразин-2-ил)-N-изопропиламино]бутилокси}-N-(метилсульфонил)ацетамида, демонстрирующая пики дифракции в спектре порошковой рентгеновской дифракции, по крайней мере, при следующих значениях углов дифракции 2θ: 9,4 градуса, 9,8 градуса, 17,2 градуса и 19,4 градуса, где спектр порошковой рентгеновской дифракции получали с использованием Cu Кα излучения.2. Форма-II кристалла 2-{4-[N-(5,6-дифенилпиразин-2-ил)-N-изопропиламино]бутилокси}-N-(метилсульфонил)ацетамида, демонстрирующая пики дифракции в спектре порошковой рентгеновской дифракции, по крайней мере, при следующих значениях углов дифракции 2θ: 9,0 градусов, 12,9 градуса, 20,7 градуса и 22,6 градуса, где спектр порошковой рентгеновской дифракции получали с использованием Cu Кα излучения.3. Форма-III кристалла 2-{4-[N-(5,6-дифенилпиразин-2-ил)-N-изопропиламино]бутилокси}-N-(метилсульфонил)ацетамида, демонстрирующая пики дифракции в спектре порошковой рентгеновской дифракции, по крайней мере, при ...

VERFAHREN ZUR SYNTHESE VON 2- BENZOLSULFONAMID-3-METOXYPYRAZIN

Chemical compounds

VERFAHREN ZUR HERSTELLUNG VON NEUEN DERIVATEN DER PENAM-3-CARBONSAEURE UND CEPHEM-4-CARBONSAEURE

Heteroaryl sulfonamides and CCR2

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Crystals

Provided are the following novel crystals of 2-{4-[N-(5,6-diphenylpyradin-2-yl)-N-isopropylamino]butyl­oxy}-N-(methylsulfonyl)acetamide (hereinafter, referred to as "compound A"): I-form crystals of the compound A which give an X-ray powder diffraction spectrum having diffraction peaks at least at diffraction angles (2) of 9.4º, 9.8º, 17.2º, and 19.4º; II-form crystals of the compound A which give an X-ray powder diffraction spectrum having diffraction peaks at least at diffraction angles (2) of 9.0º, 12.9º, 20.7º, and 22.6º; and III-form crystals of the compound A which give an X-ray powder diffraction spectrum having diffraction peaks at least at diffraction angles (2) of 9.3º, 9.7º, 16.8º, 20.6º, and 23.5º.

Sulfonamide compounds and uses as TNAP inhibitors

Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper- mineralization.

HETEROARYL SULFONAMIDES AND CCR2

... ²² Compounds are provided that act as potent antagonists of the CCR2 ²receptor. Animal testing demonstrates that these compounds are useful for ²treating inflammation, a hallmark disease for CCR2. The compounds are ²generally aryl sulfonamide derivatives and are useful in pharmaceutical ²compositions, methods for the treatment of CCR2-mediated diseases, and as ²controls in assays for the identification of CCR2 antagonists. The compounds ²of the present invention include, for example, those of formula (I):²²(see formula I)²²where Ar, R1, Y1, Y2, Y3, Y4, L and Z1 are defined in the herein application.² ...

Verfahren zur Herstellung eines neuen Benzolsulfonamidderivates.

Verfahren zur Herstellung eines neuen Benzolsulfonamidderivates.

Verfahren zur Herstellung eines neuen Benzolsulfonamidderivates.

Verfahren zur Herstellung eines Benzolsulfonamidderivates.

Verfahren zur Herstellung eines Benzolsulfonamidderivates.

Verfahren zur Herstellung eines Benzolsulfonamidderivates.

Verfahren zur Herstellung von 2-Sulfanilamido-pyrazin.

Verfahren zur Herstellung eines Benzolsulfonamidderivates.

Verfahren zur Herstellung eines neuen Benzolsulfonamidderivates.

Verfahren zur Herstellung von 2-(N1-Acetyl-sulfanilamido)-3-methoxy-pyrazin

Verfahren zur Herstellung von 3-Methoxy-2-sulfapyrazin

Verfahren zur Herstellung von neuen 3-Alkoxy-2-sulfanilamidopyrazinen

Verfahren zur Herstellung von neuen Sulfanilamiden

Verfahren zur Herstellung von 3-Methoxy-2-sulfanilamidopyrazin

Verfahren zur Herstellung eines therapeutisch wirksamen Mittels, insbesondere eines Antimalariamittels, mit einem Chinolinringsystem

VERFAHREN ZUR HERSTELLUNG VON 3-METHOXY-2-SULFANILAMIDOPYRAZIN.

Verfahren zur Herstellung von Pyrazinderivaten

Verfahren zur Herstellung neuer Sulfonamide

METHOD FOR PRODUCTION OF SUBSTITUTED N - (3 - AMINOKhINOKSALIN - 2 - YL) SULFONAMIDE AND THEIR INTERMEDIATE N - (3 - KhLORKhINOKSALIN - 2 - YL) SULFONAMIDE

Method of preparation of derived from sulphonamides

Sulphachloro-pyrazine prepn. - by chlorination of pyrazine dioxide to 2,6-dichloropyrazine which is then condensed with sulphanilamide

Sulphachlosopyrazine (I) prepn. comprises conversion of pyrazine N,N'-dioxide into 2,6-dichloropyrazine which is then condensed with sulphanilamide to give (I). The known antibacterial agent (I), used in agriculture and in feeding stuffs, is obtained in high yield, with low reaction temps. and without a catalyst which needs regeneration.

HETEROARYL SULFONAMIDES AND CCR2/CCR9

Compounds are provided that act as potent antagonists of the CC R2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CC R2 antagonists.

Heteroaryl sulfonamides and CCR2

A compound of the formula (I), or a salt thereof: where Ar is selected from the group consisting of substituted or unsubstituted C6-10 aryl and substituted or unsubstituted 5- to 10-membered heteroaryl; R1 is selected from the group consisting of hydrogen, unsubstituted C1 alkyl, substituted or unsubstituted C3-8 alkyl, substituted or unsubstituted C2-6alkenyl, substituted or unsubstituted C2-6 alkynyl, and substituted or unsubstituted 3- to 10-membered heterocyclyl; Y1 is selected from the group consisting of -CR2a-, -N-, and -N+(O)--; Y2 is selected from the group consisting of -CR2b-, -N-, and -N+(O)--; Y3 is selected from the group consisting of -CR2c-, -N-, and -N+(O)--; R2a, R2b, and R2c are each independently selected from the group consisting of hydrogen, halogen, -CN, -C(O)R3, -CO2R, -C(O)NR3R4, -OR3, -OC(O)R3, -OC(O)NR3R4, -SR3, -S(O)R3, -S(O)2R3, -S(O)2NR3R4, -NO2, -NR3R4, -NR3C(O)R4, -NR3C(O)OR4, - NR3S(O)2R4, -NR3C(O)NR4R5, substituted or unsubstituted C1-8 alkyl, substituted ...

SULPHONAMIDE COMPOUNDS THAT MODULATE CHEMOKINE RECEPTOR ACTIVITY (CCR4)

КРИСТАЛЛЫ

СУЛЬФОНАМИДНЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ TNAP

... 1. Соединение Формулы I или его фармацевтически приемлемая соль, сольват, таутомер или N-оксид:в которой:Yи Yнезависимо представляют собой связь или -N(R)-, при этом, по меньшей мере, один из Yи Yпредставляет собой -N(R)-;Lи Lнезависимо представляют собой связь или необязательно замещенный алкилен;Xпредставляет собой =N- или =C(R)-;Xпредставляет собой =N- или =C(R)-;Rи Rнезависимо выбраны из группы, состоящей из водорода, галогена, -CN, -C(O)-N(R)-R, -C(O)-O-R, необязательно замещенного алкила, необязательно замещенного циклоалкила, необязательно замещенного гетероциклоалкила, необязательно замещенного алкокси, галогеналкила, галогеналкокси, необязательно замещенного фенила и необязательно замещенного 5- или 6-членного гетероарила;R, Rи Rнезависимо выбраны из группы, состоящей из водорода, галогена, -CN, -C(O)-N(R)-R, -C(O)-O-R, необязательно замещенного алкила, необязательно замещенного циклоалкила, необязательно замещенного гетероциклоалкила, необязательно замещенного алкокси, галогеналкила ...

N-ПИРАЗИНИЛ-ФЕНИЛСУЛЬФОНАМИДЫ И ИХ ПРИМЕНЕНИЕ В ЛЕЧЕНИИ ХЕМИКИН- МЕДИИРОВАННЫХ ЗАБОЛЕВАНИЙ

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) 2004 119 966 (13) A C 07 D 241/22 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2004119966/04, 14.01.2003 (71) Çà âèòåëü(è): ÀñòðàÇåíåêà ÀÁ (SE) (30) Ïðèîðèòåò: 16.01.2002 SE 0200119-6 17.06.2002 SE 0201857-0 (43) Äàòà ïóáëèêàöèè çà âêè: 10.06.2005 Áþë. ¹ 16 (74) Ïàòåíòíûé ïîâåðåííûé: Ïîëèêàðïîâ Àëåêñàíäð Âèêòîðîâè÷ (87) Ïóáëèêàöè PCT: WO 03/059893 (24.07.2003) Àäðåñ äë ïåðåïèñêè: 193036, Ñàíêò-Ïåòåðáóðã, à/ 24, "ÍÅÂÈÍÏÀÒ", ïàò.ïîâ. À.Â.Ïîëèêàðïîâó, ðåã.¹ 0009 (54) N-ÏÈÐÀÇÈÍÈË-ÔÅÍÈËÑÓËÜÔÎÍÀÌÈÄÛ È ÈÕ ÏÐÈÌÅÍÅÍÈÅ Â ËÅ×ÅÍÈÈ ÕÅÌÈÊÈÍ- R U Ôîðìóëà èçîáðåòåíè 1. Ñîåäèíåíèå ôîðìóëû (I) èëè åãî ôàðìàöåâòè÷åñêè ïðèåìëåìà ñîëü èëè ñîëüâàò A 2 0 0 4 1 1 9 9 6 6 A ÌÅÄÈÈÐÎÂÀÍÍÛÕ ÇÀÁÎËÅÂÀÍÈÉ â êîòîðûõ R 1, R 2 è R 3 íåçàâèñèìî ïðåäñòàâë þò ñîáîé âîäîðîä, ãàëîãåí, öèàíî, CF3, OCF3, ÎÑ1-6àëêèë èëè Ñ1-6àëêèë; R 4 ïðåäñòàâë åò ñîáîé ãàëîãåí, CO2R 12, C1-6àëêîêñè, ãäå àëêèëüíà ãðóïïà ìîæåò îáðàçîâàòü 3-6-÷ëåííîå íàñûùåííîå êîëüöî èëè ìîæåò áûòü çàìåùåíà 1-3 àòîìàìè ôòîðà èëè öèàíãðóïïîé; Ñ3-6àëêåíèëîêñè èëè Ñ3-6àëêèíèëîêñè, êîòîðûå ìîãóò áûòü, âîçìîæíî, çàìåùåíû ãèäðîêñè, ëèáî NR 14R 15; ÎÑ1-6àëêèë-Õ-Ñ1-6àëêèë, ãäå àëêèëüíûå ãðóïïû ìîãóò îáðàçîâàòü 3-6-÷ëåííîå íàñûùåííîå êîëüöî; ÎÑ1-6àëêèëR11 èëè ÎÑ2-6àëêèë-Õ-R 11, ãäå àëêèëüíà ãðóïïà ìîæåò îáðàçîâàòü 3-6-÷ëåííîå íàñûùåííîå êîëüöî è, âîçìîæíî, çàìåùåíà 1-3 ãðóïïàìè, âûáðàííûìè èç ãèäðîêñè, ãàëîãåíà, NR 14R 15, SR 13, S(O)2R 13, S(O)R 13 èëè COR 13; ÎÑ1-6àëêèëR16; Ñòðàíèöà: 1 RU 2 0 0 4 1 1 9 9 6 6 (86) Çà âêà PCT: SE 03/00041 (14.01.2003) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 16.08.2004 (72) Àâòîð(û): ÁÀÊÑÒÅÐ Ýíäðþ (GB), ÄÆÎÍÑÎÍ Òèìîòè (GB), ÊÈÍÄÎÍ Íèêîëàñ (GB), ÐÎÁÅÐÒÑ Áðàéàí (GB), ÑÒÎÊÑ Ìàéêë (GB) A 2 0 0 4 1 1 9 9 6 6 A R U 2 0 0 4 1 1 9 9 6 6 Ñòðàíèöà: 2 R U R 5 è R 6 íåçàâèñèìî ïðåäñòàâë þò ñîáîé âîäîðîä, öèàíî, ãàëîãåí, CO2R 12, CONR 14R 15; Ñ1-6àëêèë, âîçìîæíî çàìåùåííûé ãèäðîêñè, NR 14R ...

Pyrazine derivatives

The invention comprises the compounds of general formula wherein R1 is Cl or NH2, and R2 is OCH3 or Cl provided that when R1 is Cl, R2 is also Cl; and (1) the preparation of 2,3,5-trichloropyrazine by chlorinating with phosphorus oxychloride at 100-170 DEG C. 2,3,5-triketopyrazine, which may be prepared by condensing aminoacetamide or one of its salts with an ester of oxalic acid in the presence of an aliphatic alcohol and an alkali metal salt thereof, and (2) the preparation of 2 - amino - 3,5 - dichloropyrazine by treating the trichloro compound with aqueous ammonia, and (3) the preparation of 2-amino-5-chloro-3-methoxy-pyrazine by treating the 3-chloro compound with an alkali metal salt of methanol in methanolic solution.

N-Diazine-benzenesulphonamide derivatives as endothelin receptor antagonists

The invention concerns N-heterocyclyl sulphonamide derivatives of the formula I in which the variables R<3>-R<6> and the ring containing in, W, X, Y and Z and bearing substituent A have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutically compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

NEW n (FLUORPYRAZINYL) PHENYLSULFONAMIDE AS MODULATORS of the CHEMOKINREZEPTORS CCR4

2,3-SUBSTITUIERTE PYRAZINSULFONAMIDE AS CRTH2HEMMER

SULFONE AMIDE CONNECTIONS, (CCR4) MODULATING CHEMOKINREZEPTORAKTIVITÄT

HETERO ARYL SULFONE AMIDES AND CCR2

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF THE PENAM-3-CARBONSAURE AND CEPHEM-4-CARBONSAURE

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF THE PENAM-3-CARBONSAEURE AND CEPHEM-4-CARBONSAEURE

Heteroaryl sulfonamides and CCR2

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

SULFONAMIDES AND PROCESS FOR THE PREPARATION THEREOF

DERIVATIVES OF PENAM-3-CARBOXYLIC ACID AND CEPHEM-4-CARBOXYLIC ACID AND PROCESSES FOR THEIR MANUFACTURE

... 6-Acylamino-penam-3-carboxylic acids and 7acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula in which R1 is hydrogen, R2 is optionally substituted phenyl, thienyl or furyl or R1 and R2 together are optionally substituted cycloalkyl, and R is a radical which is linked through a carbon, oxygen, sulphur or nitrogen atom.

THERAPEUTIC COMPOUNDS AND COMPOSITIONS

Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) and pharmaceutically acceptable salts, solvates, and hydrates thereof, for example, compounds that activate PKM2 are described herein. Also provided are pharmaceutical compositions comprising a compound provided herewith and the use of such compositions in methods of treating diseases and conditions that are related to pyruvate kinase function (e.g.,PKM2 function), including, e.g., cancer, diabetes, obesity, autoimmune disorders, and benign prostatic hyperplasia (BPH). The pharmaceutical composition may comprise a compound or a pharmaceutically acceptable salt of formula (I) (see formula I) ...

NOVEL N-(FLUORO-PYRAZINYL)-PHENYLSULFONAMID.ES AS MOODULATORS OF CHEMOKINE RECEPTOR CCR4.

The invention provides N-(fluoro-pyrazinyl)-phenylsulfonamides of formula (I) wherein R1 -R5 are as defined in the specification; processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy ...

Sulphonamide compounds that modulate chemokine receptor activity (ccr4)

The invention relates to sulphonamide compounds, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

КРИСТАЛЛЫ

FIELD: medicine, pharmaceutics. SUBSTANCE: invention describes crystals of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulphonyl)acetamide ("compound A"), as a form I of the compound A crystal, which shows diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in its power X-ray diffraction spectrum, as a form II of the compound A crystal, which shows diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in its power X-ray diffraction spectrum, as a form III of the compound A crystal, which shows diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in its power X-ray diffraction spectrum. There are also described methods for producing the forms I, II and III of the compound A crystal, based pharmaceutical composition and PGI2 receptor agonist agent, an accelerating agent for angiogenic therapy, gene engineering or autoimmune bone marrow transplantation, and an accelerating agent for angiogenesis for peripheral artery recovery or angiogenic therapy on the basis thereof; there are also described a preventive or therapeutic agent for a wide range of diseases and conditions. EFFECT: preparing the new therapeutic agent for the wide range of diseases and conditions. 11 cl, 6 dwg, 6 tbl, 5 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 556 206 C2 (51) МПК C07D 241/20 (2006.01) A61K 31/4965 (2006.01) A61P 3/06 (2006.01) A61P 7/00 (2006.01) A61P 9/00 (2006.01) A61P 11/06 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A61P 11/08 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61P 13/12 (2006.01) A61P 17/02 (2006.01) A61P 37/00 (2006.01) (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2012102678/04, 25.06.2010 (24) Дата начала отсчета срока действия патента: 25.06.2010 (73) Патентообладатель(и): НИППОН СИНЯКУ КО., ЛТД. (JP) 2 5 5 6 2 0 6 26.06.2009 JP 2009-151727; 26.06.2009 JP 2009-151728; 26.06.2009 JP 2009-151729 (43) Дата публикации заявки: 10.08.2013 Бюл. № 22 (45) ...

НОВЫЕ N-(ФТОР-ПИРАЗИНИЛ)-ФЕНИЛСУЛЬФОНАМИДЫ В КАЧЕСТВЕ МОДУЛЯТОРОВ ХЕМОКИНОВОГО РЕЦЕПТОРА CCR4

1. Соединение формулы (I) или его фармацевтически приемлемая соль: ! ! где R1 выбран из метила, хлора и фтора; ! R2 выбран из метила, хлора и фтора; ! R3 представляет собой метокси; ! один из R4 и R5 представляет собой фтор, а другой из R4 и R5 выбран из водорода и гидрокси метила. ! 2. Соединение по п.1 или его фармацевтически приемлемая соль, где R1 выбран из хлора и фтора, и R2 выбран из хлора и фтора. ! 3. Соединение по п.1 или 2 или его фармацевтически приемлемая соль, где R4 представляет собой фтор, и R5 выбран из водорода и гидроксиметила. ! 4. Соединение по п.1 или 2 или его фармацевтически приемлемая соль, где R5 представляет собой фтор, и R4 выбран из водорода и гидроксиметила. ! 5. Соединение по п.1 или 2 или его фармацевтически приемлемая соль, где один из R4 и R5 представляет собой фтор, а другой из R4 и R5 представляет собой водород. ! 6. Соединение по п.1 или 2 или его фармацевтически приемлемая соль, где один из R4 и R5 представляет собой фтор, а другой из R4 и R5 представляет собой гидроксиметил. ! 7. Соединение по п.1, выбранное из ! 2-хлор-3-фтор-N-(5-фтор-3-метоксипиразин-2-ил)-бензолсульфонамида, ! 2,3-дихлор-N-(5-фтор-3-метоксипиразин-2-ил)-бензолсульфонамида, ! 2,3-дихлор-N-(6-фтор-3-метоксипиразин-2-ил)-бензолсульфонамида, ! 2,3-дихлор-N-[6-фтор-5-(гидроксиметил)-3-метоксипиразин-2-ил]-бензолсульфонамида, ! 3-хлор-2-фтор-N-(5-фтор-3-метоксипиразин-2-ил)-бензолсульфонамида, ! 2,3-дихлор-N-[5-фтор-6-(гидроксиметил)-3-метоксипиразин-2-ил]-бензолсульфонамида, ! 3-хлор-N-(5-фтор-3-метоксипиразин-2-ил)-2-метил-бензолсульфонамида или его фармацевтически приемлемая соль. ! 8. Фармацевтическая композиция, содержащая соединение формулы (I) или его фармацевтически приемлемую соль по любому из пп.1-7 совместн� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2008 122 401 (13) A (51) МПК C07D 241/22 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2008122401/04, 11.12.2006 (71) ...

HETEROARYLSULFONAMIDE UND CCR2

Heterocyclic compounds

BENZENE SULFONE AMIDE DERIVATIVES AND YOUR APPLICATION AS DRUGS

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF THE PENAM-3-CARBONSÄURE AND CEPHEM-4-CARBONSÄURE

VERFAHREN ZUR HERSTELLUNG VON NEUEN DERIVATEN DER PENAM-3-CARBONSAURE UND CEPHEM-4-CARBONSAURE

Procedure for the production of 3-Methoxy-2-sulfanylamido-pyrazin and its salts

2,3 SUBSTITUTED PYRAZINE SULFONAMIDES AS INHIBITORS OF CRTH2

The present invention is related to the use of 2,3 substituted pyrazine sulfonamides of formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of 2,3 substituted pyrazine sulfonamides for the modulation, notably the inhibition, of CRTH2 activity.

BENZENESULFONAMIDE-DERIVATIVES AND THEIR USE AS MEDICAMENTS

Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R1 and R2 are substituents as defined within; R3 and R4 are defined within and are alkyl or halo alkyl or together form a cycloalkyl or halocycloalkyl ring; R5 is a substituent as defined within; Y-Z is a linking group as defined within; are useful in the production of an elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.

METHOD FOR PREPARING SUBSTITUTED N-(3-AMINO-QUINOXALIN-2-YL)-SULFONAMIDES AND THEIR INTERMEDIATES N-(3-CHLORO-QUINOXALIN-2-YL)SULFONAMIDES

The present invention provides a new synthesis for preparing N-(3-amino-quinoxalin-2-yl)-sulfonamides of general formulae (I) or (I') and intermediates sulfonamides of formula (II) or (II'): ...

NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION

The present invention relates to a compound of formula I: (see formula I) wherein: R1 is a hydrogen atom, F, CN, etc.; R1' is a hydrogen atom or lower alkyl which may be substituted; R2 is O, S, SO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: (see formula II) wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.

2,3 substituted pyrazine sulfonamides as inhibitors of CRTH2

SULFONAMIDES AND PROCESS FOR THE PREPARATION THEREOF

Derived from pyrazine and process to prepare them

Heteroaryl sulfonamides and CCR2

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

SULFONAMIDE COMPOUNDS AND USES AS TNAP INHIBITORS

Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.

2,3-ЗАМЕЩЕННЫЕ ПИРАЗИНСУЛЬФОНАМИДЫ В КАЧЕСТВЕ ИНГИБИТОРОВ CRTH2

FIELD: chemistry. SUBSTANCE: invention relates to 2,3-substituted pyrazine sulphonamides of formula (I), use thereof in treating allergic diseases, inflammatory dermatosis, immonological disorders and neurodegenerative disorders, as well as pharmaceutical compositions, having CRTH2 receptor inhibiting action and inhibiting chemoattractant receptor, homologous to the molecule expressed on T-helpers 2. in general formula . A is selected from a group consisting of , n denotes an integer independently selected from 0, 1, 2, 3 or 4; m equals 1 or 2; B is selected from a group consisting of phenyl or piperazinyl; R 1 denotes hydrogen; R 2 denotes phenyl, where R 2 is optionally substituted with one or more substitutes selected from a group consisting of halogen, cyano, (C 1- C 6 )alkyl; R 3 is selected from a group consisting of (C 1- C 6 )alkyl, aryl, heteroaryl, (C 1- C 6 )alkylaryl, (C 1- C 6 )alkylheteroaryl, (C 3 -C 8 )cycloalkyl and (C 3 -C 8 )heterocycloalkyl, where each of said (C 1- C 6 )alkyl, aryl, heteroaryl, (C 1- C 6 )alkylaryl, (C 1- C 6 )alkylheteroaryl, (C 3 -C 8 )cycloalkyl and (C 3 -C 8 )heterocycloalkyl is optionally substituted with one or more substitutes selected from a group consisting of halogen, cyano, (C 1- C 6 )alkyl, (C 1- C 6 )alkoxy, heteroaryl, aryl, thioalkoxy and thioalkyl, or where said aryl, heteroaryl, (C 1- C 6 )alkylaryl, (C 1- C 6 )alkylheteroaryl, (C 3 -C 8 )cycloalkyl or (C 3 -C 8 )heterocycloalkyl can be condensed with one or more aryl, heteroaryl, (C 3 -C 8 )cycloalkyl or (C 3 -C 8 )heterocycloalkyl groups and can be substituted with one or more substitutes selected from a group consisting of (C 1- C 6 )alkyl, alkoxy, aryl, heteroaryl, carboxyl, cyano, halogen, hydroxy, amino, aminocarbonyl, nitro, sulphoxy, sulphonyl, sulphonamide and trihaloalkyl; R 7 is selected from a group consisting of hydrogen, (C 1- C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, aryl, heteroaryl, (C 3 -C 8 )cycloalkyl, (C 3 -C 8 )heterocycloalkyl, ...

НОВЫЕ АМИНОПИРИДИНОВЫЕ ПРОИЗВОДНЫЕ С СЕЛЕКТИВНОЙ ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ АВРОРЫ А

... 1. Соединение общей формулы 1: ! ! где R1 представляет собой атом водорода, F, CN, COORa1, CONRa2Ra2', NRa3CORa3', CONRa4ORa4', NRa5CONRa5'Ra5'', NRa6COORa6', SO2NRa7Ra7', NRa8SO2Ra8', CORa9, SO2Ra10, NO2, ORa11 или NRa12Ra12', ! где каждый из Ra1, Ra3, Ra4, Ra5, Ra6 и Ra8 независимо представляет собой атом водорода или низший алкил; ! каждый из Ra2, Ra2', Ra5', Ra5'', Ra7, Ra7', Ra12 и Ra12' независимо представляет собой атом водорода или низший алкил, который может быть замещен одним или несколькими одинаковыми или разными заместителями, выбранными из <группы-заместителя L1>, где <группа-заместитель L1> представляет собой атом галогена, гидрокси, нитро, циано, амино, карбамоил, аминосульфонил, имино, низшую алкиламиногруппу, ди(низший)алкиламиногруппу, низший алкилсульфонил, низшую алкилсульфониламиногруппу, низший алкокси, низший алкоксикарбонил, низшую алкоксикарбониламиногруппу, низший алканоил, низший алканоилокси, низший алкилтио и карбоксил; однако при условии, что каждые из Ra2 ...

ЛЕКАРСТВЕННЫЕ СОЕДИНЕНИЯ И КОМПОЗИЦИИ

... 1. Соединение формулы (I)или его фармацевтически приемлемую соль, гдеW, X, Y и Z независимо выбраны из СН или N;D и Dнезависимо выбраны из связи или NR;А представляет необязательно замещенный бициклический гетероарил;L является связью, -С(O)-, -(CRR)-, -OC(O)-, -(CRR)-OC(O)-, -(CRR)-C(O)-, -NRC(S)-, или -NRC(O)-;Rвыбран из алкила, циклоалкила, арила, гетероарила, и гетероциклила;каждый из которых замещается 0-5 вхождением R;каждый Rнезависимо выбран из гало, галоалкила, алкила, гидроксила и -ORили два соседних Rсовместно с атомами углерода, к которым они присоединены, формируют необязательно замещенный циклил;каждый Rнезависимо выбран из алкила, ацила, гидроксиалкила и галоалкила;каждый Rнезависимо выбран из водорода и алкила;каждый Rнезависимо выбран из водорода, гало, алкила, алкокси и галоалкокси, или два Rв сочетании с атомами углерода, к которым они присоединены, формируют необязательно замещенный циклоалкил;каждый Rнезависимо выбран из гало, галоалкила, галоалкокси, алкила, алкинила ...

BENZOLSULFONAMID-DERIVATE UND IHRE ANWENDUNG ALS ARZNEIMITTEL

Substituted 2-p-aminobenzensulphonamido-pyrazines

The invention comprises compounds of general formula wherein R is OCH3 or Cl; and (1) the preparation of 3,5-dichloro-2-p-aminobenzenesulphonamidopyrazine by treating 2,3,5-trichloropyrazine with sulphanilamide at from 80 DEG to 150 DEG C. in the presence of an acid acceptor, and (2) the preparation of 5 - chloro - 3 - methoxy - 2 - p - aminobenzenesulphonamidopyrazin either by treating the corresponding 3,5-dichloro compound with an alkali metal salt of methanol in methanolic solution at 40-120 DEG C. for 2-20 hours, or by condensing the corresponding 2-amino compound with a p-acylamino-benzene-sulphohalide in the presence of a tertiary-amine and subsequently hydrolysing with alkali the acyl group in the N4-position of the sulphanilamide group of the intermediate (e.g. 2-(p-acetylaminobenzenesulphonamido) - 5 - chloro - 3 - methoxy-pyrazine); also the preparation of 3 - methoxy - 2 - p - aminobenzenesulphonamido-pyrazine by catalytically hydrogenating the 5-chloro compound ...

A process for preparing 2-sulphanilamidopyrazine and the 2-sulphanilamidopyrazine resulting therefrom

... 2-Sulphanilamidopyrazine is prepared by reacting 2-aminopyrazine with a benzene-sulphonyl chloride which carries in the p-position an acylamino group convertible to an amino group by hydrolysis, such as acetylamino or propionylamino, and finally hydrolysing the group so convertible, to give the required product. In an example, p-acetylaminobenzene sulphonyl chloride reacts with 2-aminopyrazine in pyridine to give 2-(N4-acetylsulphanilamido) pyrazine which is hydrolysed by hydrochloric acid in alcohol to give 2-sulphanilamidopyrazine.

Procedure for the production of new hetero-cyclic Sulfonamiden and their salts

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF THE PENAM-3-CARBONSÄURE AND CEPHEM-4-CARBONSÄURE

N-PYRAZINYL-PHENYLSULFONAMIDE ONE AND THEIR USE FOR THE TREATMENT OF BY CHEMOKINE OBTAINED DISEASES

2,3 substituted pyrazine sulfonamides as inhibitors of CRTH2

NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION

Disclosed is a compound represented by the general formula [I] below or a pharmaceutically acceptable salt or ester thereof. (I) (In the formula, R1 represents a hydrogen atom, F, CN or the like; R1' represents a hydrogen ato m or an optionally substituted lower alkyl group; R2 represents O, S, SO, SO 2 or the like;R3 represents an optionally substituted phenyl group; X1, X2 a nd X3 independently represent CH, N or the like, provided that none or one o f X1, X2 and X3 is N; and W represents a group represented by the following formula: , wherein W1, W2 and W3 independently represent CH, N or the like.) ...

Process of preparation of the 2-sulfanilamidopyrazine and its derivatives

Method of preparation of sulfon-amido-pyrazines

Method of preparation of new derivatives of pyrazine

Novel pyrazine derivatives

Verfahren zur Herstellung von Pyrazinderivaten

Improvements in or relating to the production of sulphonamides and intermediates thereof

... p - Hydroxybenzenesulphonamido - heterocyclic compounds of the general formula in which R is hydrogen or an aliphatic, aralkyl or heterocyclic residue, are prepared by condensing a p-acyloxybenzenesulphonyl halide with an amino heterocyclic compound having the formula NHR-Het, and hydrolyzing the p - acyloxybenzenesulphonamido - heterocyclic compound so formed until the acyl group is replaced by hydrogen. The hydrolysis preferably takes place in the presence of an aqueous solvent and at a temperature between 0 DEG and 150 DEG C. using either acidic or alkaline agents. In examples: (1) 2-aminothiazole is condensed with 1 - benzoyloxybenzene - 4-sulphonyl chloride in pyridine and the product hydrolysed by heating with aqueous sodium hydroxide; (2) 2-aminothiazole is condensed with 1 - carbethoxyoxybenzene - 4 - sulphonyl chloride in pyridine and the product hydrolysed; (3) 2 - amino - 5 - carbethoxy - thiazole is condensed with 1-carbethoxyoxybenzene-4-sulphonyl chloride ...

2,3 substituted pyrazine sulfonamides as inhibitors of CRTH2

The present invention is related to the use of 2,3 substituted pyrazine sulfonamides of formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of 2,3 substituted pyrazine sulfonamides for the modulation, notably the inhibition, of CRTH2 activity.

N-heterocyclyl sulphonamide derivatives and their use as endothelin antagonists

THERAPEUTIC COMPOUNDS AND COMPOSITIONS

Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

Method of preparation of derived from sulphamides, in particular of derived from sulphanilamide

HETEROARYL SULFONAMIDES AND CCR2

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

N-heterocyclic sulfonamides having endothelin receptor activity

The invention concerns pharmaceutically useful compounds of the formula I, in which R1, R2, R3, n, m and Het have any of the meanings defined herein, and their pharmaceutically-acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processess for the manufacture of the novel compounds and the use of the compounds in medical treatment.

HETEROARYL SULFONAMIDES AND CCR2

НОВЫЕ АМИНОПИРИДИНОВЫЕ ИЛИ АМИНОПИРАЗИНОВЫЕ ПРОИЗВОДНЫЕ С СЕЛЕКТИВНОЙ ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ АВРОРЫ А

FIELD: chemistry. SUBSTANCE: invention relates to a compound of general formula where: R 1 denotes COOR a1 , CONR a2 R a2' , CONR a4 OR a4' , where: each of R a1 and R a4 denotes a hydrogen atom; each of R a2 and R a2 ' denotes a hydrogen atom; R a4' denotes a lower alkyl; or R 1 denotes a heterocyclic group selected from the following groups, where Y 2 denotes a hydrogen atom or a lower alkyl: R 2 denotes O, S, SO, SO 2 ; R 3 denotes a phenyl which is substituted with 2 substitutes selected from halogen, CF 3 ; X 2 denotes CH or N; W denotes the following residue: where: W 1 denotes CH or S; W 2 denotes CH; W 3 denotes C or N; and at least one of W 1 , W 2 and W 3 denotes a carbon atom; or pharmaceutically acceptable salt or ester thereof. The invention also relates to a pharmaceutical composition having Avrora A selective inhibitory action, which, along with a pharmaceutically acceptable carrier or diluent, contains at least one compound of formula I a an active ingredient. EFFECT: aminopyridine or aminopyrazine derivatives which inhibit growth of tumour cells based on Avrora A kinase selective inhibitory action. 11 cl, 3 tbl, 24 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 437 880 (13) C2 (51) МПК ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ C07D C07D C07D C07D A61K A61K A61P 401/12 (2006.01) 417/12 (2006.01) 403/12 (2006.01) 413/14 (2006.01) 31/4427 (2006.01) 31/497 (2006.01) 35/00 (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2009111599/04, 29.08.2007 (24) Дата начала отсчета срока действия патента: 29.08.2007 C 2 2 4 3 7 8 8 0 C 2 R U (56) Список документов, цитированных в отчете о поиске: WO 2002/066461 A1, 29.08.2002. WO 2002/059112 A2, 01.08.2002. CA 2585638 A1, 04.05.2006. RU 2003122209 A, 10.02.2005. RU 2003122210 A, 27.12.2004. WO 2001/17995 A1, 15.03.2001. WO 2002/50066 A2, 27.06.2002. WO 2002/068415 A1, 06.09.2002. CA 2567569 A1, 19.05.2005. CA 2585638 A1, 04.05.2006. (85) Дата начала рассмотрения заявки PCT на ...

ПРОИЗВОДНЫЕ ХИНОЛИНСУЛЬФОНАМИДОВ И ИХ ПРИМЕНЕНИЕ ДЛЯ МОДУЛИРОВАНИЯ ПКМ2 АКТИВНОСТИ

FIELD: chemistry. SUBSTANCE: invention relates to field of organic chemistry, namely to heterocyclic compounds of general formula (I) and to their pharmaceutically acceptable salts, where each W, X, Y and Z represents CH; each W, X and Y represents CH and Z represents N or each W, X and Z represents CH and Y represents N; D and D 1 are independently selected from bond or NR b ; A represents chinolinyl; L is bond, -C(O)-, -(CR c R c ) m -, -OC(O)-, -(CR c R c ) m -OC(O)-, -(CR c R c ) m -C(O)-, -NR b C(S)- or -NR b C(O)- (where point of binding to R 1 is on the left side); R 1 is selected from C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, aryl (where aryl represents phenyl or naphthyl), heteroaryl (where heteroaryl represents 5-10-membered mono- or bicyclic aromatic ring with 1-3 heteroatoms, selected from nitrogen and sulphur) and heterocyclyl (where heterocyclyl represents tetrahydrofuranyl or azetidinyl) each of which is substituted with 0-5 substituents R d ; each R 3 is independently selected from halo-C 1 -alkyl, C 1 -C 6 alkyl, hydroxyl and -OR a ; each R a is independently selected from C 1 -C 6 alkyl and acyl (where acyl represents -C(O)CH 3 ), hydroxy-C 1 -C 2 alkyl; each R b is independently selected from hydrogen and C 1 -C 6 alkyl; each R c is independently selected from hydrogen, C 1 -C 6 alkyl or two R c , taken together with atoms of carbon, which they are bound to, form C 3 -cycloalkyl; each R d is independently selected from halo-C 1 -alkyl, halo-C 1 -alkoxy, C 1 -C 6 alkyl, C 2 -C 6 alkinyl, cyano, hydroxyl, -C(O)R a , -OC(O)R a , -C(O)OR a , -SR a , -NR a R b and -OR a ; n equals 0 or 1; m equals 1, 2 or 3; h equals 1 or 2 and g equals 1. Invention also relates to particular compounds, pharmaceutical composition, based on formula (I) compound and method of modulating PKM2 activity. EFFECT: novel heterocyclic compounds, useful for modulating PKM2 activity, have been obtained. 46 cl, 1 dwg, 2 tbl, 2 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 401/12 ( ...

СУЛЬФОНАМИДНЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ TNAP

FIELD: chemistry. SUBSTANCE: invention relates to compounds of Formula I: wherein: Y 1 is a bond and Y 2 is -N(R 6 )-; L 1 and L 2 are each a bond; X 1 is =N- or =C(R2)-; X 2 is =N- or =C(R 3 )-; R 1 and R 4 are independently selected from the group consisting of -F, -Cl, -Br, -CN, -C(O)N(R 7 )-R 8 , -C(O)-O-R 9 , methyl, -OMe, -OCF 3 , optionally substituted phenyl and optionally substituted 5- or 6-membered heteroaryl; R 2 , R 3 and R 5 are hydrogen; R 6 is hydrogen; R 7 is hydrogen and R 8 is selected from hydrogen, optionally substituted C 1 -C 4 alkyl, optionally substituted C 3 -C 6 cycloalkyl or optionally substituted phenyl; either R 7 and R 8 together with the nitrogen atom to which they are attached form an optionally substituted heterocycloamino which is an optionally substituted pyrrolidine, an optionally substituted piperidine, an optionally substituted morpholine or an optionally substituted piperazine; R 9 is selected from hydrogen, optionally substituted C 1 -C 4 alkyl, optionally substituted C 3 -C 6 cycloalkyl or optionally substituted phenyl; A is selected from the group consisting of -C(O)-N(R 7 )-R 8 or -C(O)-O-R 9 , or A is , R 12 and R 13 are independently selected from the group consisting of hydrogen, halogen, -CN, -OH, -C(O)-O-R 19 , optionally substituted C 1 -C 4 alkyl, optionally substituted C 3 -C 6 cycloalkyl optionally substituted with C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, optionally substituted phenyl and optionally substituted 5- or 6-membered heteroaryl, R 19 is selected from the group consisting of hydrogen, optionally substituted C 1 -C 4 lkila, C 1 -C 4 haloalkyl, optionally substituted C 3 -C 6 cycloalkyl and optionally substituted phenyl; and R 15 represents hydrogen or C 1 -C 4 alkyl; Wherein the substituted group is substituted by -CO 2 H, nitrile, hydroxyl, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, phenyl, C 3 -C 6 cycloalkyl or diC 1 -C 4 alkylamine, which modulate TNAP activity. EFFECT: improved properties of ...

N-ПИРАЗИНИЛФЕНИЛСУЛЬФОНАМИДЫ И ИХ ПРИМЕНЕНИЕ ПРИ ЛЕЧЕНИИ ОПОСРЕДОВАННЫХ ХЕМОКИНАМИ ЗАБОЛЕВАНИЙ

Настоящее изобретение относится к N-пиразинилфенилсульфонамидам общей формулы I или их фармацевтически приемлемым солям или сольватам, в которой R1, R2 и R3 независимо представляют собой водород, галоген, циано, CF3, OCF3, ОС1-6алкил или С1-6алкил; R4 представляет собой галоген, CO2 R12, С1-6алкокси, С3-6алкенилокси или С3-6алкинилокси, ОС1-6алкил-Х-С1-6алкил, ОС1-6алкилR11 или ОС2-6алкил-Х-R11, ОС1-6 алкилR16, R5 и R6 независимо представляют собой водород, циано, галоген, CO2R12, CONR14R15; С1-6алкил, возможно замещенный гидрокси, NR14R15 или 1-3 атомами фтора; С1-6алкилR11 или XCH(R11)С1-6алкил или XCH(R16)С1-6алкил, NR14R15; N(R11)R11; X-(CH2)q NR14R15; (CH2 )nNR14R15; NHC(O)С1-6алкил, возможно замещенный одной или более чем одной гидроксигруппой; С3-6алкинил или С3-6алкенил, возможно разветвленные и, возможно, замещенные 1-3 группами, выбранными из гидрокси, циано, галогена и =O; Соединения могут быть использованы при лечении опосредованных хемокинами заболеваний, например воспалительных ...

2, 3-ЗАМЕЩЕННЫЕ ПИРАЗИНСУЛЬФОНАМИДЫ В КАЧЕСТВЕ ИНГИБИТОРОВ CRTH2

... 1. Соединение согласно формуле (I) ! ! а также его геометрические изомеры, его оптически активные формы, такие как энантиомеры, диастереомеры, его рацемические формы и таутомеры, а также его фармацевтически приемлемые соли и фармацевтически активные производные, где ! А выбирают из группы, состоящей из ! ! ! n означает целое число, независимо выбранное из 0, 1, 2, 3 или 4, ! m означает или 1, или 2, ! В выбирают из группы, состоящей из (С2-С6)алкинила, (С3-С8)циклоалкила, (С3-С8)гетероциклоалкила, арила и моноциклического гетероарила, ! R1 означает водород или (С1-С6)алкил, ! R2 выбирают из группы, состоящей из (С1-С6)алкила, арила, гетероарила, (С3-С8)-циклоалкила и (С3-С8)гетероциклоалкила, где R2 необязательно замещен одним или несколькими заместителями, выбранными из группы, состоящей из галогена, циано, (С1-С6)алкила, (С1-С6)алкокси, тиоалкокси и тиоалкила, ! R3 выбирают из группы, состоящей из (С1-С6)алкила, арила, гетероарила, (C1-С6)-алкиларила, (С3-С6)алкилгетероарила, (С3-С8)циклоалкила ...

N-ПИРАЗИНИЛФЕНИЛСУЛЬФОНАМИДЫ И ИХ ПРИМЕНЕНИЕ ПРИ ЛЕЧЕНИИ ОПОСРЕДОВАННЫХ ХЕМОКИНАМИ ЗАБОЛЕВАНИЙ

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to N-pyrazinylphenylsulfonamides of the general formula (I) or their pharmaceutically acceptable salts or solvates wherein each R 1 , R 2 and R 3 represents independently hydrogen atom, halogen atom, cyano-group, -CF 3 , -OCF 3 , -O-(C 1 -C 6 )-alkyl or (C 1 -C 6 )-alkyl; R 4 represents halogen atom, -CO 2 R 12 , (C 1 -C 6 )-alkoxy-, (C 3 -C 6 )-alkenyloxy- or (C 3 -C 6 )-alkynyloxy-group, -O-(C 1 -C 6 )-alkyl-X-(C 1 -C 6 )-alkyl, -O-(C 1 -C 6 )-alkyl-R 11 , -O-(C 2 -C 6 )-alkyl-X-R 11 or -O-(C 1 -C 6 )-alkyl-R 16 ; each R 5 and R 6 represents independently hydrogen atom, halogen atom, -CO 2 R 12 , -CONR 14 R 15 , (C 1 -C 6 )-alkyl substituted possibly with hydroxy-group, -NR 14 R 15 or 1-3 fluorine atoms; (C 1 -C 6 )-alkyl-R 11 , -XCH(R 11 )-(C 1 -C 6 )-alkyl or -XCH(R 16 )-(C 1 -C 6 )-alkyl, -NR 14 R 15 , -N(R 11 )R 11 , X-(CH 2 ) q NR 14 R 15 , (CH 2 ) n NR 14 R 15 , -NHC(O)-(C 1 -C 6 )-alkyl substituted possibly with one or more hydroxy-group, (C 3 -C 6 )-alkynyl or (C 3 -C 6 )-alkenyl possibly branched and, possibly, substituted with 1-3 groups chosen from hydroxy-, cyano-group, halogen atom and =O. Proposed compounds can be used in treatment of chemokine-mediates diseases, for example, inflammatory diseases, such as asthma. Also, invention describes methods for synthesis of compounds of the formula (I), pharmaceutical composition based on thereof, method for preparing pharmaceutical composition and using compounds in producing a medicinal agent. EFFECT: improved method of synthesis, valuable medicinal properties of compounds and pharmaceutical composition. 17 cl, 212 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2 312 105 (13) C9 (51) ÌÏÊ C07D 241/22 C07D 401/12 C07D 409/12 A61K 31/497 A61P 11/06 A61P 29/00 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ÑÊÎÐÐÅÊÒÈÐÎÂÀÍÍÎÅ ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ...

Method for preparing substituted N-(3-amino-quinoxalin-2-yl)-sulfonamides and their intermediates N-(3-chloro-quinoxalin-2-yl)-sulfonamides

The present invention provides a new synthesis for preparing N-(3-amino-quinoxalin-2-yl)-sulfonamides of general formulae (I) or (I′) and intermediates sulfonamides of formula (II) or (II′): 2. The process as defined in wherein the polar aprotic solvent is selected from DMA claim 1 , DMF claim 1 , NMP and DMSO.3. The process of wherein the alkali metal hydroxide is selected from LiOH and KOH.4. The process of wherein the step b) is performed in the presence of a pyridine base.5. The process of wherein the pyridine base is selected from pyridine claim 4 , methyl pyridine claim 4 , and 2 claim 4 ,6-di-methylpyridine.6. The process of wherein the pyridine base is lutidine.7. The process of wherein step b) is performed in a polar solvent.8. The process of wherein the polar solvent is selected from DMA claim 7 , DMF claim 7 , NMP claim 7 , DMSO or alcohol. The present invention provides a new synthesis for preparing N-(3-amino-quinoxalin-2-yl)-sulfonamides of general formula (I) and its intermediate N-(3-chloro-quinoxalin-2-yl)-sulfonamides of formula (II). The compounds of formulae (I) and (II) are useful building blocks, in particular in the synthesis of drugs.The present invention is related to a new synthesis for preparing N-(3-amino-quinoxalin-2-yl)-sulfonamides of general formulae (I) and (I′), and their intermediates N-(3-chloro-quinoxalin-2-yl)-sulfonamides of formulae (II) and (II′):Ris selected from the group consisting of A, C-C-cylcoalkyl, Het, and Ar. Ris selected from the group consisting of Ar and Het. Ar denotes a monocyclic or bicyclic, aromatic carbocyclic ring having 6 to 14 carbon atoms, which is unsubstituted or monosubstituted, disubstituted or trisubstituted by Hal, CF, OCF, NO, CN, perfluoroalkyl, A, —OR, —NHR, —COR, —CONHR, —CON(R), —NRCOR, —NRCOR, —NRSOA, NRCONR′R″, —COOR, —SOA, —SONRA, —SOHet, —SONRHet, Ar, Het, —NRSONRHet, COHet, COAr, or C-C-cycloalkyl. Het denotes a monocyclic or bicyclic saturated, unsaturated or aromatic heterocyclic ring ...

SULFONAMIDE COMPOUNDS AND USES AS TNAP INHIBITORS

Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization. 2. (canceled)3. (canceled)4. (canceled)5. (canceled)7. (canceled)8. The method of claim 1 , wherein Xis ═C(R)—.9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. The method of claim 1 , wherein Ris optionally substituted phenyl or optionally substituted 5- or 6-membered heteroaryl.14. (canceled)15. The method of claim 1 , wherein Rand Rare independently selected from the group consisting of —F claim 1 , —Cl claim 1 , —Br claim 1 , —CN claim 1 , —OMe claim 1 , and —OCF.16. (canceled)17. (canceled)18. (canceled)21. (canceled)22. The method of claim 20 , wherein: A is —C(O)—O—R claim 20 , wherein Ris selected from hydrogen claim 20 , optionally substituted alkyl claim 20 , optionally substituted cycloalkyl claim 20 , and optionally substituted phenyl.23. (canceled)24. (canceled)25. The method of claim 20 , wherein: A is —C(O)—N(R)—(R) claim 20 , wherein Rand Rtogether with the nitrogen atom to which they are attached form an optionally substituted heterocycloamino.26. The method of claim 25 , wherein the optionally substituted heterocycloamino is an optionally substituted pyrrolidine claim 25 , an optionally substituted piperidine claim 25 , an optionally substituted morpholine claim 25 , or an optionally substituted piperazine.27. The method of claim 20 , wherein: A is —C(O)—N(R)—(R) claim 20 , wherein Ris hydrogen and Ris optionally substituted alkyl claim 20 , optionally substituted cycloalkyl claim 20 , or optionally substituted phenyl.28. (canceled)29. The method of claim 20 , wherein: A is —C(O)—N(R)—(R) claim 20 , wherein Rand Rare hydrogen.30. (canceled)31. (canceled)32. (canceled)33. The method of claim 1 , wherein the vascular calcification is an arterial calcification.34. The method of ...

Heteroaryl Sulfonamides and CCR2/CCR9

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists. 2. The compound of claim 1 , wherein L is —C(O)—.3. The compound of claim 1 , wherein Xand Xare each independently halogen or Chaloalkyl.4. The compound of claim 1 , wherein X claim 1 , X claim 1 , and Xare each H.5. The compound of claim 1 , wherein Ris hydrogen.6. The compound of claim 1 , wherein Yis unsubstituted Calkyl.7. The compound of claim 1 , wherein Yis hydrogen.8. The compound of claim 1 , wherein Yis —N— or —N+(O)—.9. The compound of claim 1 , wherein Zand Zare —CH—.10. The compound of claim 1 , wherein Zis —N—.11. The compound of claim 1 , wherein Ris hydrogen.12. The compound of claim 1 , wherein Ris hydrogen.16. A composition comprising a pharmaceutically acceptable carrier and the compound or salt of .17. A method of modulating CCR2 function in a cell claim 1 , comprising contacting the cell with a CCR2 modulating amount of the compound of . This application is a continuation of U.S. application Ser. No. 16/272,401, filed Feb. 11, 2019, which is a continuation of U.S. application Ser. No. 15/383,788, filed Dec. 19, 2016, which is a divisional of U.S. application Ser. No. 13/938,119, filed Jul. 9, 2013, which is a continuation of U.S. application Ser. No. 12/309,314, filed Feb. 1, 2011, now U.S. Pat. No. 8,519,135, which issued Aug. 27, 2013, which is a 371 national phase of PCT/US2007/015893, filed Jul. 12, 2007, which is a continuation-in-part of U.S. application Ser. No. 11/486,974, filed Jul. 14, 2006, now U.S. Pat. No. 7,622,583, which issued Nov. 24, 2009. The disclosures of these priority applications are incorporated herein in ...

Heteroaryl sulfonamides and ccr2/ccr9

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Chemical compounds

The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or a pharmaceutically acceptable salt thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes, and to methods of treatment, wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the description.

Fluoro-containing compounds, use and preparation thereof

The present teachings relate to a fluoro-containing compound, a composition thereof, a method of using the compound or the composition in treating a disease, and a method of preparing the compound. In a particular example, the compound is chosen from Formulae 4, 4f, 7, 8, 9, 10, 11, or 12, or a salt thereof, or a solvate of any of the foregoing.

Heteroaryl sulfonamides and CCR2

Therapeutic compounds and compositions

본 발명은 화합물 및 피루브산 키나아제 M2 (PKM2)를 조절하는 화합물을 포함한 조성물에 관한 것이다. 또한, 본 발명은 것은 PKM2를 조절하는 화합물을 암의 치료에 이용한 방법에 대해 기재하고 있다. The present invention relates to a composition comprising a compound and a compound that modulates pyruvate kinase M2 (PKM2). In addition, the present invention describes a method of using a compound that regulates PKM2 in the treatment of cancer.

Ccr4 antagonist and medicinal use thereof

Novel aminopyridine derivatives having selective inhibition of Aurora A

本発明は、一般式［Ｉ］：［式中、Ｒ１は、水素原子、Ｆ、ＣＮなどであり；Ｒ１’は、水素原子又は置換されてもよい低級アルキル基であり； Ｒ２は、Ｏ、Ｓ、ＳＯ、ＳＯ２などであり； Ｒ３は、置換されてもよいフェニル基であり； Ｘ１、Ｘ２、及びＸ３は、それぞれ独立して、ＣＨ、Ｎなどであるが、但し、Ｘ１、Ｘ２、及びＸ３のうち、Ｎであるものの数は０個ないし１個であり； Ｗは、次の基：であり、ここで、Ｗ１、Ｗ２、及びＷ３は、それぞれ独立して、ＣＨ、Ｎなどである。］で示される化合物、又はその薬学的に許容される塩若しくはエステル、に関する。 In the present invention, a compound represented by the general formula [I]: [wherein R1 is a hydrogen atom, F, CN, etc .; R1 ′ is a hydrogen atom or an optionally substituted lower alkyl group; R3 is an optionally substituted phenyl group; X1, X2, and X3 are each independently CH, N, etc. provided that X1, X2, and The number of N in X3 is 0 to 1; W is the following group: where W1, W2, and W3 are each independently CH, N, etc. . Or a pharmaceutically acceptable salt or ester thereof.

Substituted carbamate derivatives as modulators of corticotropin-releasing factor receptor activity

本发明提供了式(I)的化合物包括它们的盐以及组合物和使用所述化合物的方法。所述化合物为CRF受体拮抗剂且可用于治疗与异常CRF水平或者CRF受体的异常功能相关的病症。

Pyrazine derivatives and processes for their preparation

Sulfonamide compounds and uses as tnap inhibitors

본 발명은 TNAP의 활성을 조절하는 화합물에 관한 것이다. 일부 실시양태에서, 본원에 기재된 화합물은 TNAP를 억제한다. 특정 실시양태에서, 본원에 기재된 화합물은 무기질 과잉증과 관련된 병태의 치료에 유용하다. The present invention relates to compounds that modulate the activity of TNAP. In some embodiments, compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful for the treatment of conditions associated with hyperthyroidism.

Broad spectrum anti-cancer compounds

Described herein, inter alia, are compounds for treating cancer and methods of use. This disclosure features chemical entities (e.g., small hairpin RNAs (shRNAs), micro RNA (miRNAs), small interfering RNA (siRNAs), small molecule inhibitors, antisense nucleic acids, peptides, viruses, CRISPR-sgRNAs, or combinations thereof) that inhibit one or more of m6A writers (e.g., methyltransferase like 3 (Mettl3 or MT-A70) or methyltransferase like-14 (Mettl14)), m6Am writers (e.g., phosphorylated CTD interacting factor I (PCIF 1), or Mettl3/14), m6A erasers (e.g., fat-mass and obesity-associated protein (FTO) or ALKB homolog 5 (ALKBH5)), m6Am erasers (e.g., FTO), m6A readers (e.g., YTH domain-containing family proteins (YTHs)), YTF domain family member 1 (YTHDF 1), YTF domain family member 2 (YTHDF 2), YTF domain family member 3 (YTHDF 3), or tyrosine-protein phosphatase non-receptor type 2 (PTPN2).

Patent FR2256916B3

Crystals

[Problem] A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (hereinafter referred to as "compound A"). [Means for Resolution] A Form-I crystal of compound A, showing diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in the powder X-ray diffraction spectrum thereof. A Form-II crystal of compound A, showing diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in the powder X-ray diffraction spectrum thereof. A Form-III crystal of compound A, showing diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in the powder X-ray diffraction spectrum thereof.

THERAPEUTIC COMPOUNDS AND COMPOSITIONS

La presente invención se refiere a compuestos y composiciones que comprenden compuestos que modulan a piruvato cinasa M2 (PKM2). También se describen métodos para usar los compuestos que modulan PKM2 en el tratamiento de cáncer.

Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain

The present invention relates to compounds of formula (IV) useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Derivatives of 2-aminopyrazine and process for their preparation

KINOLIN-8-SULFONAMIDE PRODUCTS HAVE ANTI-CANCER ACTION

Ενώσεις και συνθέσεις περιλαμβάνοντας ενώσεις που διαμορφώνουν την κινάση πυρουβικού Μ2 (ΡΚΜ2) περιγράφονται εις το παρόν. Επίσης περιγράφονται εις το παρόν και μέθοδοι χρήσης των ενώσεων που διαμορφώνουν το ΡΚΜ2 στην αγωγή καρκίνου. Compounds and compositions comprising compounds that form pyruvate M2 kinase (PKM2) are described herein. Methods of using the compounds that modulate PKM2 in cancer treatment are also described herein.

Novel compounds

Aromatic amine derivative and use thereof

The present invention provides a novel SCD inhibitor. An SCD inhibitor containing a compound represented by the formula [I] wherein ring A is an optionally substituted aromatic ring, ring B is an optionally substituted ring, ring C is an optionally substituted aromatic ring, R is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, and X is a spacer having 1 to 5 atoms in the main chain, or a salt thereof, or a prodrug thereof.

Novel aminopyridine derivatives having aurora a selective inhibitory action

The present invention relates to a compound of general formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R2 is O, S, SO, SO2, etc.; R3 is a phenyl which may be substituted; X2 is CH, N, etc.; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.

Compositions useful as inhibitors of voltage-gated sodium channels

The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Heter Garylsulfonamides and CCR2

CRYSTALS

Problema.- Un objeto principal de la presente invención es proporcionar un nuevo cristal de 2-{4-[N-(5,6-difenilpirazin-2-il)-N-isopropilamino]butiloxil-N- (metilsulfonil)acetamida (referida más adelante en la presente como "compuesto A").Medios para resolución.- Un cristal de Forma I del compuesto A, que muestra picos de difracción a 9.4 grados, 9.8 grados, 17.2 grados y 19.4 grados en el espectro de difracción en polvo de rayos X del mismo.Un cristal de Forma II del compuesto A, que muestra picos de difracción 9.0 grados, 12.9 grados, 20.7 grados y 22.6 grados en el espectro de difracción en polvo de rayos X del mismo.Un cristal de Forma III del compuesto A, que muestra picos de difracción a 9.3 grados, 9.7 grados, 16.8 grados, 20.6 grados y 23.5 grados en el espectro de difracción en polvo de rayos X del mismo. Problem.- A main object of the present invention is to provide a new crystal of 2- {4- [N- (5,6-diphenylpyrazin-2-yl) -N-isopropylamino] butyloxy-N- (methylsulfonyl) acetamide (referred to hereinafter as "compound A") Means for resolution.- A Form I crystal of compound A, which shows diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in the powder diffraction spectrum X-ray thereof. A Form II crystal of compound A, showing diffraction peaks 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in the X-ray powder diffraction spectrum thereof. A Form III crystal of the compound A, which shows diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in the X-ray powder diffraction spectrum thereof.

Crystals

A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyradin-2-yl)-N-isopropylamino]butyl-oxy}-N-(methylsulfonyl)acetamide (hereinafter, referred to as "compound A"). [Means for Resolution] A Form-I crystal of the compound A, showing diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in the powder X-ray diffraction spectrum thereof A Form-II crystal of the compound A, showing diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in the powder X-ray diffraction spectrum thereof. A Form-III crystal of the compound A, showing diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in the powder X-ray diffraction spectrum thereof.

Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain

Disclosed are compounds of formula III, wherein the substituents are as defined in the specification, their properties as inhibitors of voltage-gated sodium or calcium channel blockers and their utility in the treatment of pain. Also disclosed is a broader class of voltage-gated sodium/calcium channel blockers having formula T-L1-A-L2-Z wherein the substituents are as defined in the specification. (62) Divided Out of 545710

Heteroaryl sulfonamides and ccr2

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

2,3 substituted pyrazine sulfonamides as inhibitors of crth2

The present invention is related to the use of 2,3 substituted pyrazine sulfonamides of formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of 2,3 substituted pyrazine sulfonamides for the modulation, notably the inhibition, of CRTH2 activity.

Pyruvate kinase m2 (pkm2) modulator compounds, compositions comprising the same and uses thereof

Kynurenine production inhibitor

A kynurenine production inhibitor or the like, which contains a nitrogen-containing heterocyclic compound represented by formula (I).  (In the formula, R 50 and R 51 may be the same or different and each represents a hydrogen atom or the like; G 1 and G 2 may be the same or different and each represents a nitrogen atom or the like; X represents a group represented by formula (III) (wherein m 1 and m 2 may be the same or different and each represents an integer of 0 or 1; Y represents an oxygen atom or the like; and R 6 and R 7 may be the same or different and each represents a hydrogen atom or the like); R 1 represents an optionally substituted lower alkyl group or the like; R 2 represents a hydrogen atom or the like; and R 3 represents an optionally substituted lower alkyl group or the like.)

HETEROCYCLES COMPOUNDS AS MODULATORS OF PYRUVATE KINASE M2 (PKM2)

SE REFIERE A COMPUESTOS HETEROCICLOS DE FORMULA (I) DONDE Y, W, X Y Z SON CADA UNO CH O N; D Y D1 SON CADA UNO UN ENLACE O NRb, EN DONDE Rb ES H O ALQUILO; A ES HETEROARILO BICICLICO OPCIONALMENTE SUSTITUIDO; L ES UN ENLACE, -C(O)-, -OC(O)-, -NRbC(S)-, ENTRE OTROS; R1 ES ALQUILO, CICLOALQUILO, ARILO, HETEROARILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS CON Rd, EN DONDE Rd ES HALO, HALOALCOXI, ALQUINILO, NITRO, ENTRE OTROS; R3 ES HALO, HALOALQUILO, ALQUILO, HIDROXILO, ENTRE OTROS; n, h Y g SON CADA UNO DE 0 A 2. SON COMPUESTOS PREFERIDOS: 5-CLORO-2-METOXI-N-(4-(4-(2-METOXIFENIL)PIPERAZIN-1-CARBONIL)FENIL)BENCEN-SULFONAMIDA; N-(4-(4-(2-METOXIFENIL)PIPERAZIN-1-CARBONIL)FENIL)NAFTALEN-2-SULFONAMIDA; N-(4-(4-(2-METOXIFENIL)PIPERAZIN-1-CARBONIL)FENIL)BENZO[d]TIAZOL-5-SULFONAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE LA PIRUVATO CINASA M2 (PKM2) SIENDO UTILES EN EL TRATAMIENTO DE CANCER, DIABETES, OBESIDAD REFERS TO HETEROCICLUS COMPOUNDS OF FORMULA (I) WHERE Y, W, X AND Z ARE EACH CH O N; D AND D1 ARE EACH A LINK OR NRb, WHERE Rb IS H OR RENT; A IS OPTIONALLY REPLACED BICYCLE HETEROARYL; L IS A LINK, -C (O) -, -OC (O) -, -NRbC (S) -, AMONG OTHERS; R1 IS ALKYL, CYCLOALKYL, ARYL, HETEROARYL, AMONG OTHERS, OPTIONALLY SUBSTITUTED WITH Rd, WHERE Rd IS HALO, HALOALCOXY, ALKINYL, NITRO, AMONG OTHERS; R3 IS HALO, HALOALKYL, ALKYL, HYDROXYL, AMONG OTHERS; n, h AND g ARE EACH FROM 0 TO 2. PREFERRED COMPOUNDS ARE: 5-CHLORO-2-METOXY-N- (4- (4- (2-METOXYPHENYL) PIPERAZIN-1-CARBONYL) PHENYL) BENZEN-SULFONAMIDE; N- (4- (4- (2-METOXYPHENIL) PIPERAZIN-1-CARBONYL) PHENYL) NAPHTHALEN-2-SULFONAMIDE; N- (4- (4- (2-METOXYPHENYL) PIPERAZIN-1-CARBONYL) PHENYL) BENZO [d] THIAZOL-5-SULFONAMIDE; AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SAID COMPOUNDS ARE MODULATORS OF PYRUVATE KINASE M2 (PKM2), BEING USEFUL IN THE TREATMENT OF CANCER, DIABETES, OBESITY

Heteroaryl sulfonamides and ccr2.

Se proporcionan compuestos que actuan como antagonistas potentes del receptor CCR2. Las pruebas en animales demuestran que estos compuestos son utiles en el tratamiento de la inflamacion, un trastorno con sello distintivo para el CCR2. Los compuestos generalmente son derivados de la aril-sulfonamida y son utiles en composiciones farmaceuticas, metodos para el tratamiento de trastornos mediados con CCR2, y como controles en ensayos para la identificacion de antagonistas CCR2.

N-HETEROCYCLYL SULPHONAMIDE DERIVATIVES AND THEIR USE AS ENDOTHELINE ANTAGONISTS

Novel aminopyridine derivative having aurora a-selective inhibitory activity

Therapeutic compounds and compositions

Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

Preparation of 2-(n4-acylsulphanilamido) pyrazine

N-gallic amide-pyrimidine phenyl sulfonamide derivative as well as preparation method and application thereof

本发明涉及涉及一种N-没食子酰胺-嘧啶基苯磺酰胺类化合物及其制备方法，以及这类化合物在制备抗菌和促进软骨细胞生长方面的药物方面的应用。该N-没食子酰胺-嘧啶基苯磺酰胺类化合物及其水溶性盐。在体外对金黄色葡萄球菌、大肠杆菌、绿脓杆菌、不动杆菌、变形杆菌、肺科杆菌等具有一定的抑菌作用；并具能够促进骨细胞的增殖，对软骨细胞内总蛋白、糖胺聚糖的合成有明显的促进作用，还可上调蛋白聚糖、II 型胶原及SOX9基因的基因水平，抑制I 型胶原的基因水平，促进软骨细胞外基质的分泌与合成，可用于制备治疗骨性关节炎的药物。

Compositions useful as inhibitors of voltage-gated ion channels

Therapeutic compounds and compositions

本文描述了化合物和包含调节丙酮酸激酶M2(PKM2)的化合物的组合物。本文还描述了在治疗癌症中使用调节PKM2的化合物的方法。

Crystals

本发明的主要目的在于提供一种2-{4-[N-(5，6-二苯基吡嗪-2-基)-N-异丙基氨基]丁氧基}-N-(甲基磺酰基)乙酰胺(以下称为化合物A)的新型晶体。化合物A的I型晶体在其粉末X射线衍射图中至少在下述衍射角2θ：9.4度、9.8度、17.2度及19.4度处显示出衍射峰。化合物A的II型晶体在其粉末X射线衍射图中至少在下述衍射角2θ：9.0度、12.9度、20.7度及22.6度处显示出衍射峰。化合物A的III型晶体在其粉末X射线衍射图中至少在下述衍射角2θ：9.3度、9.7度、16.8度、20.6度及23.5度处显示出衍射峰。

2,3 substituted pyrazine sulfonamides as inhibitors of crth2.

La presente invencion se refiere al uso de pirazona-sulfonamidas 2,3-sustituidas en la formula (I) para el tratamiento y/o prevencion de enfermedades alergicas, dermatosis inflamatorias y otras enfermedades con un componente inflamatorio. Especificamente la presente invencion se refiere al uso de pirazina-sulfonamidas 2,3-sustituidas para la modulacion, notablemente la inhibicion, de la actividad de CRTH2.

Novel aminopyridine derivatives having selective inhibition of Aurora A

SULFONAMIDE COMPOUNDS THAT MODULATE THE ACTIVITY OF CHEMIOQUINE RECEPTORS (CCR4).

Un compuesto de la fórmula (I) o una sal o solvato farmacéuticamente aceptable del mismo: (Ver fórmula) en la que: Ar 1 es fenilo o tienilo, cada uno de los cuales está opcionalmente sustituido por uno a tres sustituyentes R 1 , R 2 y R 3 seleccionados entre halógeno, ciano, CF3, OCF3, O-alquilo C1 - 6 ó alquilo C1 - 6; R 4 es alcoxi C1 - 6,donde el grupo alquilo puede formar un anillo saturado de 3-6 miembros o puede estar sustituido con 1-3 átomos de flúor o un grupo ciano; o O-alquilo C1 - 6-R 11 , ó O-alquilo C2 - 6-X-R 11 , donde el grupo alquilo puede formar un anillo saturado de 3-6 miembros y está opcionalmente sustituido con 1-3 grupos seleccionados entre hidroxi, halógeno, NR 14 R 15 , SR 13 , S(O)2 R 13 , S(O)R 13 ó COR 13 ; uno de R 5 ó R 6 es XCH2-alquilo C1 - 4, donde el grupo alquilo está sustituido en una posición por R 11 y bien NR 14 R 15 o bien hidroxi, o R 5 /R 6 es XR 16 , donde R 16 es un anillo saturado de 4-8 miembros que contiene 1-3 heteroátomos seleccionados entre nitrógeno, oxígeno o azufre y opcionalmente sustituido con 1-3 grupos seleccionados entre hidroxi, ciano, halógeno y =O, y R 16 está sustituido por R 11 ; y el otro es hidrógeno, halógeno, amino, NH-alquilo C1 - 6, N(alquilo C1 - 6)2, alcoxi C1 - 6 o alquilo C1 - 6 opcionalmente sustituido por uno o más grupos fluoro o hidroxilo; X es NR 13 , O, S, S(O) ó S(O)2; R 11 es un grupo arilo o un anillo heteroaromático de 5-7 miembros que contiene 1-4 heteroátomos seleccionados entre nitrógeno, oxígeno o azufre, grupo arilo o anillo heteroaromático que puede estar opcionalmente sustituido por 1-3 grupos seleccionados entre halógeno, C(O)NR 14 R 15 , C(O)OR 12 , hidroxi, =O, =S, CN, NO2, COR 13 , NR 14 R 15 , X(CH2)qNR14R15, (CH2)nNR 14 R 15 , (CH2)nOH, SR 13 , S(O)R 13 , S(O)2R 13 alquilo C1 - 6-X-alquilo C1 - 6, alquilo C1 - 6 ó alcoxi C1 - 6, donde el grupo alquilo puede formar un anillo de 3-6 miembros o está opcionalmente sustituido con 1-3 grupos seleccionados entre hidroxi, haló ...

Derivatives of penam-3-carboxylic acid and cephem-4-carboxylic acid and processes for their manufacture

6-acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula <IMAGE> in which R1 is hydrogen, R2 is optionally substituted phenyl, thienyl or furyl or R1 and R2 together are optionally substituted cycloalkyl, and R is a radical which is linked through a carbon, oxygen, sulphur or nitrogen atom. [US3996208A]

Crystals

본 발명의 주목적은, 2-{4-[N-(5,6-디페닐피라진-2-일)-N-이소프로필아미노]부틸옥시}-N-(메틸술포닐)아세트아미드(이하, 「화합물 A」라고 함.)의 신규 결정을 제공하는 것에 있다. 분말 X선 회절 스펙트럼에 있어서, 적어도 다음의 회절각 2θ: 9.4도, 9.8도, 17.2도 및 19.4도에 회절 피크를 나타내는, 화합물 A의 I형 결정. 분말 X선 회절 스펙트럼에 있어서, 적어도 다음의 회절각 2θ: 9.0도, 12.9도, 20.7도 및 22.6도에 회절 피크를 나타내는, 화합물 A의 II형 결정. 분말 X선 회절 스펙트럼에 있어서, 적어도 다음의 회절각 2θ: 9.3도, 9.7도, 16.8도, 20.6도 및 23.5도에 회절 피크를 나타내는, 화합물 A의 III형 결정.

Quinoline-8-sulfonamide derivatives having an anticancer activity

Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

Process for the preparation of pyrazine derivatives

Patent FR2181839B1

Crystals

[Problem] A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2- y1)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (hereinafter referred to as "compound A").[Means for Resolution]A. Form-I crystal of compound A, showing diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in the powder X-ray diffraction spectrum thereof.A Form-II crystal of compound A, showing diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in the powder X-ray diffraction spectrum thereof.A Form-III crystal of compound A, showing diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in the powder X-ray diffraction spectrum thereof.[Selected Drawing] None

N-PIRACINIL-PHENYLSULPHONAMIDES AND ITS USES IN THE TREATMENT OF CHEMIOCINE-MEDIUM DISEASES.

Un compuesto de fórmula (I) o una sal o solvato farmacéuticamente aceptable del mismo: en la que: R 1 , R 2 y R 3 son independientemente hidrógeno, halógeno, ciano, CF3, OCF3, O-alquilo C1-6 o alquilo C1-6; R 4 es halógeno, CO2R 12 , (I) alcoxi C1-6 en el que el grupo alquilo puede formar un anillo saturado de 3-6 miembros o puede sustituirse con 1-3 átomos de flúor o un grupo ciano; alqueniloxi C3-6 o alquiniloxi C3-6 en el que cualquiera puede sustituirse opcionalmente con hidroxi o NR 14 R 15 ; O-alquil C1-6-X-alquilo C1-6 en el que los grupos alquilo pueden formar un anillo saturado de 3-6 miembros; O-alquil C1-6-R 11 u O-alquil C2-6-X-R 11 en el que el grupo alquilo puede formar un anillo saturado de 3-6 miembros y está opcionalmente sustituido con 1-3 grupos seleccionados de hidroxi, halógeno, NR 14 R 15 , SR 13 , S(O)2R 13 , S(O)R 13 o COR 13 ; O-alquilo C1-6R 16 ; R 5 y R 6 son independientemente hidrógeno, ciano, halógeno, CO2R 12 , CONR 14 R 15 ; alquilo C1-6 opcionalmente sustituido por hidroxi, NR 14 R 15 o 1-3 átomos de flúor; alquilo C1-6R 11 o XCH(R 11 )alquilo C1-6 o XCH(R 16 )alquilo C1-6 en el que el grupo alquilo puede sustituirse opcionalmente con 1-3 grupos seleccionados de hidroxi y NR 14 R 15 ; NR 14 R 15 ; N(R 11 )R 11 ; X-(CH2)qNR 14 R 15 ; (CH2)nNR 14 R 15 ; NHC(O)alquilo C1-6 opcionalmente sustituido por uno o más grupos hidroxi, alquinilo C3-6 o alquenilo C3-6 opcionalmente ramificado y opcionalmente sustituido con 1-3 grupos seleccionados de hidroxi, ciano, halógeno y =O; R 11 ; X-R 11 ; X-R 12 ; X-alquil C1-6R 16 ; X-R 16 ; X-(CH2)nCO2R 12 ; X-(CH2)nCONR 14 R 15 ; X-(CH2)nR 11 ; X-(CH2)nCN; X- (CH2)qOR 12 ; (CH2)nOR 12 ; (CH2)n-X-R 11 ; X-(CH2)qNHC(O)NHR 12 ; X-(CH2)qNHC(O)R 12 ; X-(CH2)qNHS(O)2R 12 ; X- (CH2)qNHS(O)2R 11 ; X-alquenilo C3-6; X-alquinilo C3-6; n es 1 ,2, 3, 4 o 5; q es 2, 3, 4, 5 o 6; X es NR 13 , O, S, S(O), S(O)2; R 11 es un grupo arilo o un anillo heteroaromático de 5-7 miembros que contiene 1-4 heteroátomos ...

Heteroaryl sulfonamides and CCR2

2,3 Substituted Pyrazine Sulfonamides as Inhibitors of CRTH2

The present invention is related to the use of 2,3 substituted pyrazine sulfonamides of formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of 2,3 substituted pyrazine sulfonamides for the modulation, notably the inhibition, of CRTH2 activity.

Therapeutic compounds and compositions

本文中描述調節丙酮酸激酶M2(PKM2)之化合物及包含該等化合物之組成物。本文中亦描述使用該等調節PKM2之化合物治療癌症的方法。

Therapeutic compounds and compositions

Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

Patent LTPA2023513I1

Therapeutic compounds and compositions

6-membered heteroarylaminosulfonamides for treating diseases and conditions mediated by deficient CFTR activity

The invention relates to heteroaryl compounds, pharmaceutically acceptable salts thereof, and pharmaceutical preparations thereof. Also described herein are compositions and the use of such compounds in methods of treating diseases and conditions mediated by deficient CFTR activity, in particular cystic fibrosis.

Therapeutic compounds and compositions

Crystals.

Problema.- Un objeto principal de la presente invención es proporcionar un nuevo cristal de 2-{4-[N-(5,6-difenilpirazin-2-il) -N-isopropilamino]butiloxil-N-(metilsulfonil)acetamida (referida más adelante en la presente como "compuesto A"). Medios para resolución. - Un cristal de Forma I del compuesto A, que muestra picos de difracción a 9.4 grados, 9.8 grados, 17.2 grados y 19.4 grados en el espectro de difracción en polvo de rayos X del mismo. Un cristal de Forma II del compuesto A, que muestra picos de difracción 9.0 grados, 12.9 grados, 20.7 grados y 22.6 grados en el espectro de difracción en polvo de rayos X del mismo. Un cristal de Forma III del compuesto A, que muestra picos de difracción a 9.3 grados, 9.7 grados, 16.8 grados, 20.6 grados y 23.5 grados en el espectro de difracción en polvo de rayos X del mismo.

Pyruvate kinase m2 (pkm2) modulator compounds, compositions comprising the same and uses thereof

THERAPEUTIC COMPOUNDS AND COMPOSITIONS

La presente invención se refiere a compuestos y composiciones que comprenden compuestos que modulan a piruvato cinasa M2 (PKM2). También se describen métodos para usar los compuestos que modulan PKM2 en el tratamiento de cáncer.

NOVEDOUS AMINOPIRIDINE DERIVATIVES THAT HAVE SELECTIVE INHIBITING ACTION ON AURORA A

La presente invencion se refiere al compuesto de formula I: en el que: R1 es un atomo de hidrogeno, F,CN, etc.; R2 es O, S, SO, SO2, etc.; R3 es un fenilo que puede estar sustituido; X2 es CH, N, etc.; W es el siguiente resto: en el que: W1, W2, y W3 son cada uno independientemente CH, N, etc., o una de sus sales esteres farmaceuticamente aceptables.

SULPHONAMIDE COMPOUNDS MODULATING CHEMOCIN RECEPTOR ACTIVITY (CCR4)

Sulfonamide compounds and uses as tnap inhibitors

本文描述了调节TNAP的活性的化合物。在一些实施方案中，本文描述的化合物抑制TNAP。在某些实施方案中，本文描述的化合物可用于治疗与矿质过多相关的状况。

2-Amino-3-methoxy-pyrazine and process for its preparation

Heteroaryl sulfonamides and CCR2

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Sulfonamide compounds and uses as tnap inhibitors

Novel aminopyridine derivative having aurora a-selective inhibitory activity

The present invention relates to a compound of formula I: wherein: R 1 is a hydrogen atom, F, CN, etc.; R 1 ' is a hydrogen atom or lower alkyl which may be substituted; R 2 is O, S, SO, SO 2 , etc.; R 3 is a phenyl which may be substituted; X 1 , X 2 , and X 3 each independently CH, N, etc. provided, however, that among X 1 , X 2 and X 3 , the number of nitrogen is 0 or 1; W is the following residue: wherein: W 1 , W 2 , and W 3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.

Novel aminopyridine derivatives having aurora a selective inhibitory action

Heteroaryl sulfonamides and ccr2

Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists. The compounds of the present invention include, for example, those of formula (I): (see formula I) where Ar, R1, Y1, Y2, Y3, Y4, L and Z1 are defined in the herein application.

Crystals

A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide (hereinafter referred to as "compound A"). [Means for Resolution] A Form-I crystal of compound A, showing diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in the powder X-ray diffraction spectrum thereof. A Form-II crystal of compound A, showing diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in the powder X-ray diffraction spectrum thereof. A Form-III crystal of compound A, showing diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in the powder X-ray diffraction spectrum thereof.

Sulfonamide derivatives as urat-1 inhibitors

The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide URAT-1 inhibitors of formula (I): or pharmaceutically acceptable salt thereofs, wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the description. URAT-1 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly gout.

6-membered heteroarylaminosulfonamides for treating diseases and conditions mediated by deficient CFTR activity

본 발명은 헤테로아릴 화합물, 그의 제약학적으로 허용되는 염, 및 그의 제약 조제물에 관한 것이다. 또한 본원에서는 이러한 화합물의 조성물, 및 결핍된 CFTR 활성에 의해 매개되는 질환 및 병태, 특히 낭포성 섬유증을 치료하는 방법에서 이러한 화합물의 용도가 기재된다.

Patent FR2181839A1

Fluorine-containing compound, use thereof and method for producing same

本发明涉及含氟化合物、其组合物、使用所述化合物或所述组合物治疗疾病的方法以及制备所述化合物每个R 3 独立地选自卤素、叠氮化物的方法。在一个特定的示例中，所述化合物选自式4、4f、7、8、9、10、11或12： 其盐，或前述任一种的溶剂化物。

Crystals

Benzenesulfonamide-derivatives and their use as medicaments

Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R?1 and R2¿ are substituents as defined within; R?3 and R4¿ are defined within and are alkyl or halo alkyl or together form a cycloalkyl or halocycloalkyl ring; R5 is a substituent as defined within; Y-Z is a linking group as defined within; are useful in the production of an elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.

n- (fluoro-pyrazinyl) -phenylsulfonamides as chemokine ccr4 receptor modulators

N-(FLúOR-PIRAZINIL)-FENILSULFONAMIDAS COMO MODULADORES DE RECEPTORES CCR4 DE QUIMIOCINA. A presente invenção refere-se a N-(flúor-pirazinil)-fenilsulfonamidas de Fórmula (I) em que R^ 1^-R^ 5^ são como definidos no relatório descritivo; processos e intermediários usados em sua preparação, composições farmacêuticas contendo-os e seu uso em terapia. N- (FLUOR-PIRAZINIL) -FENYLSULPHONAMIDES AS MODULATORS OF CHEMOCCIN CCR4 RECEPTORS. The present invention relates to N- (fluoro-pyrazinyl) -phenylsulfonamides of Formula (I) in which R1 - 1 - R4 - 5 are as defined in the specification; processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

Crystals

3,4,5-trihydroxy gallic acrylamide benzene sulfonamide derivatives as well as preparation method and application thereof

本发明涉及一种3,4,5-三羟基没食子酰胺苯磺酰胺类化合物及其制备方法，以及这类化合物在制备抗菌和促进软骨细胞生长方面的药物的应用。这类化合物中的大多数化合物在体外对金黄色葡萄球菌、大肠杆菌、绿脓杆菌、不动杆菌、变形杆菌、肺科杆菌等具有一定的抑菌作用；并具能够促进骨细胞的增殖，对软骨细胞内总蛋白、糖胺聚糖的合成有明显的促进作用，还可上调蛋白聚糖、II 型胶原及SOX9基因的基因水平，抑制I 型胶原的基因水平，促进软骨细胞外基质的分泌与合成，可用于制备治疗骨性关节炎的药物。

BENZENASULFONAMIDA DERIVES AND ITS USE AS MEDICINES

Medical compounds stimulating activity of pyruvate kinase m2, compositions on their basis and use in the treatment of cancer

Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer. EMBED MDLDrawOLE.MDLDrawObject.1