Method of preparation of new sulfanilamido-pyrazoles.

AMINOPYRAZOLDERIVATE FOR THE TREATMENT OF PREDOMINANCE AND OTHER HEALTH TROUBLE

Vasopressin V1A antagonists

Small molecule inhibitors of the pleckstrin homology domain and methods for using same

Small molecule inhibitors of the pleckstrin homology domain and methods for using same

Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

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 acetylenic sulfonamide and phosphinic acid amide hydroxamic acid taceinhibitors

Inhibition of p38 kinase activity using substituted heterocyclic ureas

PPAR.GAMMA. MODULATORS

To provide PPAR.gamma. modulators seemingly usable in remedies for involutional osteoporosis which inhibit the accelerated differentiation of adipocytes and promote the formation and differentiation of osteoblasts from stem cells, or remedies for diabetes which are free from excessive formation of adipocytes, liver functional failure, vascular lesion, heart failure, etc . Compounds represented by general formula (I) or pharmacologically acceptable salts thereof: wherein A represents phenyl, etc.; B represents aryl, etc.; X represents oxygen, etc.; and n is 0 or 1.

INHIBITORS OF ION CHANNELS

Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through volt age-gated sodium channels. More particularly, the invention provides substit uted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the i ndicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pai n by the inhibition of ion flux through a voltage-gated sodium channel.

SMALL MOLECULE INHIBITORS OF THE PLECKSTRIN HOMOLOGY DOMAIN AND METHODS FOR USING SAME

Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

Verfahren zur Herstellung eines neuen Benzolsulfonamidderivates.

Verfahren zur Herstellung eines Benzolsulfonamidderivates.

Verfahren zur Herstellung eines neuen Aminobenzolsulfonamids

Verfahren zur Herstellung eines neuen Aminobenzolsulfonamids

Verfahren zur Herstellung eines neuen Aminobenzolsulfonamids

Verfahren zur Herstellung von 2-Aryl-3-amino-pyrazolen

Verfahren zur Herstellung von neuen Sulfanilamido-pyrazolen

Verfahren zur Herstellung von neuen Sulfanilamido-pyrazolen

Verfahren zur Herstellung neuer Sulfonamide

Verfahren zur Herstellung neuer Sulfonamide

Verfahren zur Herstellung neuer Sulfonamide

Verfahren zur Herstellung von Sulfanilamidopyrazolen

Verfahren zur Herstellung eines therapeutisch wirksamen Sulfonamides

Procédé de préparation de composés hétérocycliques azotés

Procédé de préparation de composés hétérocycliques azotés

Verfahren zur Herstellung von photographischen farbigen Direktpositiv-Bildern

Verfahren zur Herstellung von Methylen-5-(p-amino-benzolsulfonylamido)-1-phenyl-pyrazol

Verfahren zur Herstellung neuer Sulfonamide

Verfahren zur Herstellung neuer N-Acyl-sulfonamide

Verfahren zur Herstellung von Sulfonamiden

Verfahren zur Herstellung neuer Sulfonamide

Verfahren zur Herstellung von 5-Aminopyrazolen

PREPARATION AND USE OF ORTHO-SULFONAMIDO HETEROARYL HYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS

PURPOSE: Novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases(MMP, e.g. gelatinases, stromelysins and collagenases) and TNF-.agr. converting enzyme(TACE, tumor necrosis factor-.agr. converting enzyme) are provided. CONSTITUTION: Ortho-sulfonamido heteroaryl hydroxamic acids of formula(A) are useful for the treatment of diseases in which the enzymes MMP and TACE are implicated, such as arthritis, tumor growth and metastasis, angiogenesis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, proteinuria, aneurysmal aortic disease, degenerative cartilage loss following traumatic joint injury, demyelinating diseases of the nervous system, graft rejection,cachexia, anorexia, inflammation, fever, insulin resistance, septic shock,congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel diseases, HIV infection, age related macular degeneration, diabetic retinopathy, proliferative vitreoretinopathy, retinopathy ...

NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS

The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.

Composição, processos para dissociar um ìon de metal de uma proteìna contendo dedo de zinco, para inativar um vìrus e para selecionar um composto capaz de dissociar um ìon de metal quelado com um dedo de zinco de uma proteìna viral, vìrus isolado e inativado, kit para selecionar um composto capaz de dissociar um ìon de metal de um dedo de zinco de uma proteìna viral, composição viricida, e, formulação farmacêutica.

Sulfur substituted sulfonylaminocarboxylic acid N-arylamides, their preparation, their use and pharmaceutical preparations comprising them

The present invention relates to compounds of the formula I, wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.

(3-SULFUR-SUBSTITUTED PHENYL)PYRAZOLE DERIVATIVE

Disclosed is an insecticidal compound having a novel molecular structure which is considered to have an action different from those of commercially available insecticides. Specifically disclosed is a (3-sulfur-substituted phenyl)pyrazole derivative represented by the general formula (I) below or a salt thereof. (I) (In the formula, R1 represents an alkyl group, an alkenyl group or a cycloalkyl group; A represents a halogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a (hydroxyimino)methyl group, an (alkoxyimino)methyl group, a heteroaryl group or a cyano group; X represents a halogen atom; m represents a number of 0-3; n represents 0 or 1; and Q represents a pyrazole group.) ...

HETEROARYL ACETYLENIC SULFONAMIDE AND PHOSPHINIC ACID AMIDE HYDROXAMIC ACID TACE INHIBITORS

Cette invention concerne des composés correspondant à la formule (I) qui sont utiles dans le traitement d'états maladifs induits par le facteur de nécrose tumorale 'alpha', tels que l'arthrite rhumatoïde, l'arthrose, la septicémie, le SIDA, la colite ulcéreuse, la sclérose multiple, la maladie de Crohn et la perte de cartilage dégénérative.

Nitrogen containing heteroaromatics as factor Xa inhibitors

The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.

SYNTHETIC LETHAL TARGETING OF GLUCOSE TRANSPORT

The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.

N-(1-ARYLPYRAZOL-4L)SULFONAMIDES AND THEIR USE AS PARASITICIDES

The invention relates to a sulfonamide compound of formula (I) or a pharmaceutically, veterinarily or agriculturally acceptable salt or solvate thereof, where the groups R1-R5 are described in the description, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.

SULFUR SUBSTITUTED SULFONYLAMINOCARBOXYLIC ACID N-ARYLAMIDES, THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL PREPARATIONS COMPRISING THEM

The present invention relates to compounds of formula (I), wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of formula (I) are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of formula (I), to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of formula (I).

АНТАГОНИСТЫ РЕЦЕПТОРА ВАЗОПРЕССИНА V1a

FIELD: pharmacology. SUBSTANCE: invention concerns novel compounds of formula (1a), formula (1b), formula (1c) and formula (1d), as well as pharmaceutical composition based on them and their application in medicine obtainment. R 1 -R 4 , G, W, X, X 1 , U, V, a, b are defined in the invention claim. EFFECT: compound with antagonistic effect on vasopressin V1A receptor. 73 cl, 133 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 370 497 (13) C2 (51) МПК C07D C07D C07D C07D C07D C07D C07D ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ,C07D C07D ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ C07D (12) ОПИСАНИЕ (24) Дата начала отсчета срока действия патента: 24.08.2005 (43) Дата публикации заявки: 10.10.2008 (72) Автор(ы): АНДЖЕЙ Роман Батт (GB), БАКСТЕР Эндрю Джон (GB), ХИНИ Селин (GB), СТОКЛИ Мартин Ли (GB), БРАЙАН РО Майкл (GB), ХАДСОН Питер (DK), ХЭНДИ Рейчел (GB) C 2 (56) Список документов, цитированных в отчете о поиске: ЕР 0186817 А1, 09.07.1986. POCIECHA D. et al. New mesogenic compounds having fork-like or cyclic amide terminal groups. Liquid Crystals, 2002, том 29, №5, стр.663-667. WO 03/016316 A1, 27.02.2003. US 5843952 A, 01.12.1998. US 5968930 A, 19.10.1999. US 5760031 A, 02.06.1998. WO 2004/037788 A1, 06.05.2004. WO 02/00626 A1, 03.01.2002. WO 01/29005 A1, 26.04.2001. RU 2213094 C1, 20.09.1999. RU 2129123 C1, 20.04.1999. (85) Дата перевода заявки PCT на национальную фазу: 26.03.2007 (86) Заявка PCT: DK 2005/000540 (24.08.2005) (87) Публикация PCT: WO 2006/021213 (02.03.2006) Адрес для переписки: 191036, Санкт-Петербург, а/я 24, "НЕВИНПАТ", пат.пов. А.В.Поликарпову (54) АНТАГОНИСТЫ РЕЦЕПТОРА ВАЗОПРЕССИНА V (57) Реферат: Настоящее изобретение относится к новым соединениям формулы (1а), формулы (1b), формулы (1c) и формулы (1d), обладающим антагонистической активностью в отношении 2 3 7 0 4 9 7 C 2 223/16 (2006.01) 31/55 (2006.01) 31/553 (2006.01) 31/5517 (2006.01) 31/495 (2006.01) 31/38 (2006.01) 9/04 (2006.01) 9/12 (2006.01) 25/24 (2006.01) 35/00 (2006.01) (73) Патентообладатель(и ...

МОДУЛЯТОРЫ PPARγ

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 ...

SCHWEFEL-SUBSTITUIERTE SULFONYLAMINOCARBONSÄURE N-ARYLAMIDE, IHRE HERSTELLUNG, IHRE ANWENDUNG UND DIESE ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN

Verfahren zur Herstellung von 5-Sulfanilamidopyrazolen

New sulfonamide derivative and process for its manufacture

The invention comprises N : N1-methylene-bis-[3-(p-aminobenzenesulphonamido) - 2 - phenyl-pyrazole and its preparation by treating 3-sulphanilamido-2-phenyl pyrazole with formaldehyde in the presence of dilute acid. The compound is used therapeutically (see Group VI).ALSO:Therapeutic preparations for treatment of intestinal infections comprise methylene-N:N1-bis 3-(p-aminobenzenesulphonamido)-2-phenylpyrazole] (see Group IV(b)) and a pharmaceutical diluent preferably suitable for enteral administration. The preparations may take the form of tablets, dragees, solutions, suspensions or emulsions containing conventional diluents e.g. water, gelatine, lactose, starch, magnesium stearate, talc, vegetable oils, benzyl alcohols, gums, polyalkylene glycols, preserving, wetting and emulsifying agents and osmotic pressure or buffer substances. They contain about 10% to 90% of active compound.

New sulphonamides

The invention comprises 3-(N1-acyl-sulphanilamids)-2-phenyl-pyrazoles unsubstituted in the 4- and 5- positions and their preparation by acylating a p-amino benzenesulphonamido-2-phenyl-pyrazole. The p-substituent may also be a group convertible to amino, e.g. by hydrolysis or reduction which is subsequently so converted. The preferred product is 3-(N1-acetyl-sulphanilamido)-2-phenyl pyrazole. The compounds are used as chemotherapeutic agents, (see Group VI).ALSO:Pharmaceutical preparations comprise 3-(N1-acyl-sulphanilamide)-2-phenyl-pyrazoles unsubstituted in the 4- and 5-positions (see Group IV (b)), in association with pharmaceutical carriers such as water, gelatine, lactose, starches, colloidal silicic acid, magnesium stearate, talc, vegetable oils, benzyl alcohols, gums, polyalkylene glycols, petroleum jelly or cholesterol. The preparations may take the form of suspensions, emulsions, tablets, dragees, salves or creams.

Novel 4-substituted-pyrazole derivatives and a process for the manufacture and conversion thereof

The invention comprises compounds of the formula: <FORM:0788140/IV (b)/1> and acid addition salts thereof, where R is a lower alkyl or alkenyl group of up to six carbon atoms or a cycloalkyl, cycloalkenyl or aryl group, for example a methyl, ethyl, propyl, isopropyl, butyl, isobutyl, allyl, crotyl, methylallyl, cyclopropyl, cyclohexyl, cyclohexenyl, phenyl or substituted phenyl group, and the preparation of these compounds by reacting hydrazine with an acetonitrile which is substituted in the alpha position by a radical R and treating the product with acid or alkali if desired to convert the product into a salt or the free base. The reaction is suitably carried out in alcoholic solution in the presence of an acid such as acetic acid. The invention also comprises treating the resulting 4-substituted-3-amino - 5 - methyl - pyrazole or a salt thereof with a benzene sulphonyl halide substituted in the para position by an amino group or an acylamino or nitro group and, when the para substituent is an acylamino or nitro group, converting this to an amino group by hydrolysis or reduction to give the corresponding 3-sulphanilamide pyrazole. Examples describe the reaction of the appropriately substituted acetoacetonitrile with hydrazine to give (1) 3-amino-4 : 5 - dimethylpyrazole; (2) 3 - amino - 4- 5 - methylpyrazole; (3) 3 - amino-4 - phenyl - 5 - methylpyrazole; (4) 3 - amino-4 - allyl - 5 - methylpyrazole; and (5) 3-amino - 4 - [cyclohexen - (21) - yl] - 5 - methyl pyrazole; the products are treated with N-acetyl-sulphanilyl chloride in pyridine to give the corresponding 3-(N-acetylsulphanilamido)-pyrazoles, which are hydrolysed to give the corresponding 3-sulphanilamido compounds. Starting materials. The a -substituted acetoacetonitriles used as starting materials may be prepared either by Claisen condensation of the appropriate ester and nitrile, or by splitting off water from the corresponding aceto-acetamide. For example, a -[cyclohexen-(2)-yl] aceto- ...

New sulphonamides and process for preparing same

Novel compounds of formula wherein R1 represents an alkyl radical, a cycloalkyl radical which may be substituted by an alkyl group, or a phenyl radical which may be substituted by a halogen atom, or alkyl, alkoxy or trifluoromethyl radical, R2 represents an alkoxy-alkyl group, and R3 represents hydrogen or an alkyl or alkoxy radical, their N1-alkanoyl derivatives and N4-formaldehyde condensation products, and their alkali, alkaline-earth or earth metal salts, are prepared by reacting a compound of formula with a compound of formula in which Z represents a halogen atom and X represents an unsubstituted amino group, or a nitro, azo or acylamino group, a nitro, azo or acylamino group in the resulting compound is converted into the amino group by reduction or hydrolysis, any resulting bis-para-X-benzenesulphonyl compound is split to form a mono-para-X-benzenesulphonyl compound and, if desired, a resulting compound is N1-alkanoylated ...

New pyrazole derivatives

Novel compounds of Formula (I) where R is hydrogen, methyl or hydroxymethyl, R1 is hydrogen or methyl, X is hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen, amino, mono- or di-(lower alkyl)-amino, or acetylamino, X1 is hydrogen or lower alkyl, Y is hydrogen, lower alkyl, lower alkenyl, or the group CH2SO3M where M is an alkali metal or one equivalent of an alkaline earth metal, and Y1 is lower alkyl, lower alkenyl or cycloalkyl, and acid addition salts thereof with acids having non-toxic, pharmaceutically acceptable anions, are prepared (1) where R is hydrogen or methyl and Y is other than a methanesulphonate group, by alkylating, alkenylating or cycloalkylating the corresponding 1-phenyl-4-aminopyrazole to introduce one or both of the radicals Y and Y1, e.g. by treating the starting material with a lower alkyl halide, lower alkenyl halide or di-(lower alkyl)-sulphate and decomposing the resulting quaternary salt or the corresponding quaternary base by alkali treatment ...

Process for the production of a therapeutically useful sulphonamide

The missing text comprises compounds of the formula wherein X is a nitro or acylamino group, such as acetylamino, the process for preparing these compounds by condensing 1-phenyl-5-amino- 2,3-dihydropyrazole with a benzenesulphonyl halide X.C6H4.SO2 halogen, in an aqueous medium, at a pH of not less than 11, and also the preparation of 1-phenyl-5-p-aminobenzene sulphonamido-pyrazole by oxidising the above dihydro-pyrazoles with bromine or with hydro gen peroxide in acetic or formic acid in the presence of iodine or an iodide and converting X into an amino group, e.g. by hydrolysis in the case where X is an acylamino group, or by reduction, preferably by catalytic hydro genation, when X is a nitro group. 1 - Phenyl - 5 - amino-2,3-dihydropyrazole is made by treating b -cyanoethyl phenylhydrazine with a mineral acid such as aqueous hydro chloric acid. Specifications 865,708 and 865,709 are referred to.

HETERO ARYL DERIVATIVES WITH GROUPS OF ACETYLENES OF ABSTENTIONS SULFONE AMIDE AND PHOSPHINSÄUREAMID HYDROXAMIC ACID DERIVATIVES AS TACE INHIBITORS

SUBSTITUTED BIPHENYLISOXAZOLSULFONAMIDE

INHIBITION of the P38 KINASE ACTIVITY BY SUBSTITUTED HETERO-CYCLIC UREA

VASOPRESSIN V1A ANTAGONIST

MORE THIOLESTER AND YOUR APPLICATIONS

N-(1-arylpyrazol-4l)sulfonamides and their use as parasiticides

Pyrazol-1-yl benzene sulfonamides as CCR9 antagonists

PYRAZOL-1-YL BENZENE SULFONAMIDES AS CCR9 ANTAGONISTS Abstract Compounds of formula (I) are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulphonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9) mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.

Vasopressin V1A antagonists

Vasopressin V1A antagonists

Sulfonamides as GPR40- and GPR120-agonists

The invention relates to compounds acting as agonists of G-protein coupled receptor 120 (GPR120) and/or 40 (GPR40), and having formula (I). Said compounds are useful in the treatment of diseases or disorders modulated by GPR120 and/or GPR40 such as diabetes (particularly type 2 diabetes), impaired oral glucose tolerance, insulin resistance, obesity, obesity related disorders, metabolic syndrome, dyslipidemia, elevated LDL, elevated triglycerides, obesity induced inflammation, osteoporosis and obesity related cardiovascular disorders.

Sulfonamides as GPR40- and GPR120-agonists

The invention relates to compounds acting as agonists of G-protein coupled receptor 120 (GPR120) and/or 40 (GPR40), and having formula (I). Said compounds are useful in the treatment of diseases or disorders modulated by GPR120 and/or GPR40 such as diabetes (particularly type 2 diabetes), impaired oral glucose tolerance, insulin resistance, obesity, obesity related disorders, metabolic syndrome, dyslipidemia, elevated LDL, elevated triglycerides, obesity induced inflammation, osteoporosis and obesity related cardiovascular disorders.

NITROGEN CONTAINING HETEROAROMATICS AS FACTOR XA INHIBITORS

The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.

NEW ANTIVIRAL AGENTS AGAINST INFECTION HEPATITIS B VIRUS

АЗОТСОДЕРЖАЩИЕ ГЕТЕРОАРОМАТИЧЕСКИЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА Ха, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ЛЕЧЕНИЯ

... 1. Соединение формулы I или его стереоизомер или фармацевтически приемлемая соль, где кольцо М содержит, кроме J, 0-3 атома N, при условии, что если М содержит 2 атома N, тогда R1bотсутствует, и если М содержит 3 атома N, тогда R1aи R1bотсутствуют; J представляет собой N или NH; D выбран из CN, C(=NR8)NR7R9, NHC(=NR8)NR7R9, NR8CH(=NR7), C(O)NR7 R8и (CR8R9)tNR7R8, при условии, что D присоединен к Е в мета- или пара-положении относительно G, Е выбран из фенила, пиридила, пиримидила, пиразинила, пиридазинила и пиперидинила, замещенных 1 R; альтернативно, D-E-G вместе представляют пиридил, замещенный 1 R; R выбран из Н, галогена, (CH2 )tOR3, C1-4алкила, ОСF3и СF3; G отсутствует или выбран из NHCH2, ОСН2и SCH2 , при условии, что, когда s равно 0, тогда G присоединен к атому углерода кольца М; Z выбран из C1-4алкилена, (CH2)rO(CH2)r, (CH2)rNR3(CH2)r, (CH2)rC(O)(CH2)r, (CH2)rC(O)О(СН2)r, (СН2)rОС(О)(СН2)r, (CH2)rC(O)NR3(CH2)r, (CH2)rNR3C(О)(СН2)r, (СН2)rОС(О)О(СН2)r, (СН2)rОС(О)NR3(CH2)r, (CH2 ...

SULFONAMIDES AS GPR40- AND GPR120-AGONISTS

PYRAZOLODIAZEPINONE COMPOUNDS

Method of preparation of new sulfanilamido-pyrazoles

PHOTOGRAPHIC MATERIAL CONTAINING COLOUR COUPLERS

PYRAZOL-1-YL BENZENE SULFONAMIDES AS CCR9 ANTAGONISTS

Compounds of formula (I) are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.

N-ALKYL-N-PHENYLHYDROXYLAMINE COMPOUNDS CONTAINING METAL CHELATING GROUPS, THEIR PREPARATION AND THEIR THERAPEUTIC USES

The present invention provides novel N-alkyl-N-phenylhydroxylamine derivatives containing metal chelating groups, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species (ROS) and/or excess Zn ions, in particular stroke, Parkinson's disease and Alzheimer's disease. The compounds of the invention possess similar or superior LPO inhibition activity to the reference compounds of Trolox and Ebselen. While showing lower toxicity, they also effectively inhibit the cerebral neuronal cell death caused by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.

VASOPRESSIN V1A ANTAGONISTS

VASOPRESSIN V1a ANTAGONIST

PROBLEM TO BE SOLVED: To provide a vasopressin V1a receptor antagonist useful as a therapeutic agent for such as dysmenorrhea (primary dysmenorrhea and/or secondary dysmenorrhea), early labor pain, hypertension, Raynaud's disease, cerebral edema, motion sickness, hyperlipemia, small cell lung cancer, depression, anxiety, hyponatremia, liver cirrhosis and congestive heart failure. SOLUTION: Compounds are represented by general formula 1b or tautomers or pharmaceutically acceptable salts of the compounds. COPYRIGHT: (C)2011,JPO&INPIT ...

5-SULFONAMIDE-1-ARYL-PYRAZOLES

АГОНИСТЫ РЕЦЕПТОРА ОКСИТОЦИНА ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ ЦЕНТРАЛЬНОЙ НЕРВНОЙ СИСТЕМЫ

FIELD: chemistry. SUBSTANCE: group of inventions includes the novel benzene-sulfonamide derivatives, the claimed compounds pharmaceutical compositions, and the compound of formula (I) use as the oxytocin receptor agonist and their use for the medicinal preparation with the oxytocin receptor agonist activity manufacturing. Technical result: compounds of formula (I) have the good oxytocin receptor affinity . EFFECT: group of inventions can find application in the treatment of autism, stress, including post-traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, mental disorders and memory losses, alcohol abstinence, drug addiction and for the Prader-Willi syndrome treatment. 8 cl, 3 tbl, 26 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 664 705 C2 (51) МПК A61K 31/415 (2006.01) A61K 31/427 (2006.01) A61K 31/433 (2006.01) A61K 31/4439 (2006.01) A61K 31/506 (2006.01) C07D 417/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 401/04 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 231/42 (2006.01) C07D 403/04 (2006.01) A61P 43/00 (2006.01) (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК A61K 31/415 (2018.05); A61K 31/427 (2018.05); A61K 31/433 (2018.05); A61K 31/506 (2018.05); C07D 417/04 (2018.05); C07D 401/04 (2018.05); C07D 231/42 (2018.05); A61P 43/00 (2018.05) 2015130950, 14.01.2014 (24) Дата начала отсчета срока действия патента: 14.01.2014 21.08.2018 (73) Патентообладатель(и): Ф. ХОФФМАНН-ЛЯ РОШ АГ (CH) Приоритет(ы): (30) Конвенционный приоритет: 17.01.2013 EP 13151632.0 (43) Дата публикации заявки: 21.02.2017 Бюл. № 6 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 17.08.2015 (86) Заявка PCT: 2 6 6 4 7 0 5 EP 2014/050526 (14.01.2014) (87) Публикация заявки PCT: WO 2014/111356 (24.07.2014) Адрес для переписки: 197101, Санкт-Петербург, а/я 128, "АРСПАТЕНТ", М.В. Хмара (54) АГОНИСТЫ РЕЦЕПТОРА ОКСИТОЦИНА ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ ЦЕНТРАЛЬНОЙ НЕРВНОЙ СИСТЕМЫ (57) Реферат: Группа изобретений включает новые рецептору окситоцина. ...

АГОНИСТЫ РЕЦЕПТОРА ОКСИТОЦИНА ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ ЦЕНТРАЛЬНОЙ НЕРВНОЙ СИСТЕМЫ

Аза-арил-1Н-пиразол-1-ил-сульфонамиды

... 1. Соединение или соль формулы (I)гдеRвыбран из группы, содержащей замещенный или незамещенный Салкил, замещенный или незамещенный Салкокси, замещенный или незамещенный Салкиламино и замещенный или незамещенный Сгетероциклил;R- Н, F, Cl или замещенный или незамещенный Cалкокси; илиRи Rвместе с атомами углерода, к которым они присоединены, образуют неароматическое карбоциклическое кольцо или гетероциклическое кольцо;R- Н, замещенный или незамещенный Cалкил, замещенный или незамещенный Салкокси или гало;R- Н или F;R- Н, F, Cl или -СН;R- Н, гало, -CN, -COR, -CONH, -NH, замещенный или незамещенный Салкил, замещенный или незамещенный Cалкокси или замещенный или незамещенный Саминоалкил;R- Н или замещенный или незамещенный Cалкил;Rи Rмогут вместе образовывать карбоциклическое кольцо;L - связь, -СН- или -СН(СН)-;каждый из А, А, А, А, А, А, Аи Анезависимо выбран из группы, состоящей из N, N-O и -CR-; где, по крайней мере, один и не более двух из А, А, А, А, А, А, Аи А-N или N-O;R- каждый независимо ...

HEMMUNG DER p38 KINASE AKTIVITÄT DURCH SUBSTITUIERTEN HETEROCYCLISCHEN HARNSTOFFEN

Procedure for the production of the new 2-Phenyl-3 (p-amino-benzolsulfonamido) - 5-äthyl-pyrazols, its N4-Formaldehydkondensationsprodukte, the salts and N1-Acylderivate of it

Procedure for the production of new Pyrazoldiazepinon connections as well as their salts

Procedure for the production of new Pyrazoldiazepinonverbindungen as well as their salts

IONENKANAL HEMMER

NITROGENOUS HETEROCYCLEN AS FACTOR XA HEMMER

Vasopressin V1A antagonists

Therapeutically active compositions and their method of use

Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.

Heteroaryl acetylenic sulfonamide and phosphinic acid amide hydroxamic acid TACE inhibitors

Ppargamma modulators

Pyrazol-1-yl benzene sulfonamides as CCR9 antagonists

PYRAZOL-1-YL BENZENE SULFONAMIDES AS CCR9 ANTAGONISTS Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.

SULFUR SUBSTITUTED SULFONYLAMINOCARBOXYLIC ACID N-ARYLAMIDES, THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL PREPARATIONS COMPRISING THEM

The present invention relates to compounds of formula (I), wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of formula (I) are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of formula (I), to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of formula (I).

NOVEL ANTIVIRAL AGENTS AGAINST HBV INFECTION

The present invention is directed toward novel compounds and novel methods of use of said compounds of the formula (I), useful as nucleocapsid assembly inhibitors for the treatment of viruses, especially but not exclusively, including pregenomic RNA encapsidation inhibitors of HBV for the treatment of Hepatitis B virus (HBV) infection and related conditions. (Formula (I)) Including hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein A, R1, R2, R3, R4, R5, R6, R7, and R8 are defined herein.

VASOPRESSIN V1A ANTAGONISTS

The present invention concerns compounds inter alia according to general formula: (1a). Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.

VASOPRESSIN V1A ANTAGONISTS

The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of primary dysmenorrhoea. (see formula I) ...

COLORED PHOTOGRAPHIC DIRECT POSITIVE IMAGES

Method of preparation of new 3-arylsulfonylamino-pyrazoles

PESTICIDAL 5-SUBSTITUTED-OXYALKYLAMINO-1-ARYLPYRAZOLE DERIVATIVES

The invention relates to 5-substituted- oxyalkylaminopyrazole derivatives of formula (I) or salts thereof wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths). © KIPO & WIPO 2007 ...

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.

AZA-ARYL 1H-PYRAZOL-1-YL BENZENE SULFONAMIDES

Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists. 2. The compound of or salt thereof claim 1 , wherein one of Aor Ais N or N—O claim 1 , and the remaining of A claim 1 , A claim 1 , A claim 1 , A claim 1 , A claim 1 , A claim 1 , A claim 1 , and Aare —CR— claim 1 , where each Ris selected independently.3. The compound of or salt thereof claim 1 , wherein two of claim 1 , AA claim 1 , A claim 1 , Ais N or N—O claim 1 , and the remaining of A claim 1 , A claim 1 , A claim 1 , A claim 1 , A claim 1 , A claim 1 , A claim 1 , and Aare —CR— claim 1 , where each Ris selected independently.6. The compound of or salt thereof claim 5 , where{'sup': '1', 'sub': 2', '3', '3', '2', '3', '3', '3', '2', '2', '3', '2', '2', '3', '2', '3', '2', '3', '3', '2', '3', '3', '2', '3', '2', '3, 'Ris selected from the group consisting of: —CHCH, —CH(CH), —C(CH), —C(CH)CHCH, —C(CHCH)CN, —C(OH)(CH), —OCH, —OCHCH, —OCH(CH), —OC(CH), —OCHCH(CH), —OCF, and morpholino;'}{'sup': '2', 'Ris H, F, or Cl; or'}{'sup': 1', '2, 'sub': 3', '2', '2', '3', '2', '2', '2, 'Rand Rmay together form —OC(CH)CH— or —C(CH)CHCH—;'}{'sup': '3', 'sub': 3', '3, 'Ris H, —CH, or —OCH;'}{'sup': '4', 'Ris H or F;'}{'sup': '5', 'Ris H;'}{'sup': '6', 'sub': 3', '2', '3', '3', '2', '3', '7', '2', '2', '2', '3', '3', '2', '3', '2', '2', '2, 'Ris H, —CH, —CHCH, —CH(CH), —CH, —CHF, —CHF, —CFCH, —CF, —CHOCH, —CHOH, —CHCN, —CN, or —CONH; and'}{'sup': '8', 'sub': 3', '3', '2', '3', '2', '3', '2, 'each Ris independently selected from the group consisting of H, F, Cl, Br, —CH, —OH, —OCH, —OCHCH, —NH, —N(CH), and —CN.'}7. The compound of or salt thereof claim 6 , ...

AZA-ARYL 1H-PYRAZOL-1-YL BENZENE SULFONAMIDES

Compounds are provided that act as potent antagonists of the CCR(9) receptor for treating Sjogren's syndrome. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions. 4. The compound of or salt thereof claim 3 , where{'sup': '1', 'sub': 2', '3', '3', '2', '3', '3', '3', '2', '2', '3', '2', '2', '3', '2', '3', '2', '3', '3', '2', '3', '3', '2', '3', '2', '3, 'Ris selected from the group consisting of: —CHCH, —CH(CH), —C(CH), —C(CH)CHCH, —C(CHCH)CN, —C(OH)(CH), —OCH, —OCHCH, —OCH(CH), —OC(CH), —OCHCH(CH), —OCF, and morpholino;'}{'sup': '2', 'Ris H, F, or Cl; or'}{'sup': 1', '2, 'sub': 3', '2', '2', '3', '2', '2', '2, 'Rand Rmay together form —OC(CH)CH— or —C(CH)CHCH—;'}{'sup': '3', 'sub': 3', '3, 'Ris H, —CH, or —OCH;'}{'sup': '4', 'Ris H or F;'}{'sup': '5', 'Ris H;'}{'sup': '6', 'sub': 3', '2', '3', '3', '2', '3', '7', '2', '2', '2', '3', '3', '2', '3', '2', '2', '2, 'Ris H, —CH, —CHCH, —CH(CH), —CH, —CHF, —CHF, —CFCH, —CF, —CHOCH, —CHOH, —CHCN, —CN, or —CONH; and'}{'sup': '8', 'sub': 3', '3', '2', '3', '2', '3', '2, 'each Ris independently selected from the group consisting of H, F, Cl, Br, —CH, —OH, —OCH, —OCHCH, —NH, —N(CH), and —CN.'}5. The compound of or salt thereof claim 4 , where Ris —C(CH).6. The compound of or salt thereof claim 7 , where{'sup': '2', 'Ris H or F;'}{'sup': '3', 'Ris H;'}{'sup': '4', 'Ris H; and'}{'sup': '6', 'sub': 3', '2', '2', '3, 'Ris —CH, —CHF, —CHF, or —CF.'}8. The method of claim 1 , wherein the subject is human.9. The method of claim 1 , wherein the administering is oral claim 1 , parenteral claim 1 , rectal claim 1 , transdermal claim 1 , sublingual claim 1 , nasal or topical.10. The method of claim 1 , further comprising administering an anti-inflammatory or analgesic agent. This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Patent Application No. 62/360,149, filed Jul. 8, 2016, and titled “AZA-ARYL 1H-PYRAZOL-1-YL BENZENE SULFONAMIDES,” which is ...

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 ...

NOVEL ANTIVIRAL AGENTS AGAINST HBV INFECTION

The present invention provides novel compounds of formula (I) and methods of use thereof. In certain embodiments, the compounds of the invention are useful as nucleocapsid assembly inhibitors. In other embodiments, the compounds of the invention are useful as pregenomic RNA encapsidation inhibitors of Hepatitis B virus (HBV). In yet other embodiments, the compounds of the invention are useful for the treatment of viral infection, including HBV and related viral infections. 45-. (canceled)6. The compound of claim 1 , wherein{'sup': '3', 'Ris selected from the group consisting of optionally substituted aryl, optionally substituted benzyl, optionally substituted alkylaryl, optionally substituted heteroaryl, and optionally substituted alkylheteroaryl; and'}{'sup': '4', 'where present, Ris hydrogen.'}7. The compound of claim 6 , wherein{'sup': '3', 'Ris selected from a group consisting of optionally substituted phenyl, optionally substituted benzyl, optionally substituted benzoisoxazolyl, optionally substituted benzooxazolyl, optionally substituted furyl, optionally substituted imidazolyl, optionally substituted indoyl, optionally substituted isoxazolyl, optionally substituted isothiazolyl, optionally substituted oxazolyl, optionally substituted pyrazolyl, optionally substituted pyridin-2-on-yl, optionally substituted pyridyl, optionally substituted pyrrolyl, optionally substituted quinolinyl, optionally substituted thiazolyl optionally substituted thienyl, and optionally substituted methylpyridyl.'}9. The compound of claim 7 , wherein the optional substitution of Rcomprises at least one halo or Calkyl.10. (canceled)12. The compound of claim 1 , wherein{'sup': 5', '7, 'Rand Rare independently at each occurrence H or F; and'}{'sup': 6', '8, 'sub': 1-3', '1-3, 'Rand Rare independently at each occurrence hydrogen, chloro, fluoro, Calkyl, or Calkoxy.'}14. The compound of claim 1 , wherein{'sup': 5', '7', '8, 'R, R, and Rare each H; and'}{'sup': '6', 'Ris hydrogen, chloro, ...

Aza-aryl 1h-pyrazol-1-yl benzene sulfonamides

Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.

SYNTHETIC LETHAL TARGETING OF GLUCOSE TRANSPORT

The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells. 1. A method for inhibiting cell growth or proliferation of a cell that is HIF pathway proficient comprising contacting a cell wherein the cell is HIF pathway proficient with a therapeutic entity , wherein the therapeutic entity inhibits the activity of GLUT1 and wherein the therapeutic entity preferentially inhibits the growth or proliferation of neoplastic cells versus normal cells.2. The method of claim 1 , wherein the inhibiting of growth or proliferation of the neoplastic cells results in cell death.5. The method of claim 1 , wherein the therapeutic entity comprises a compound selected from the group consisting of4-(Phenylsulfonamidomethyl)-N-(pyridin-2-yl)benzamide;4-(Phenylsulfonamidomethyl)-N-(pyridin-3-yl)benzamide;4-(Phenylsulfonamidomethyl)-N-(pyridin-4-yl)benzamide;4-(Phenylsulfonamidomethyl)-N-(thiazol-2-yl)benzamide;4-(Phenylsulfonamidomethyl)-N-(1H-pyrazol-3-yl)benzamide;4-(Phenylsulfonamidomethyl)-N-(quinolin-3-yl)benzamide;4-(Phenylsulfonamidomethyl)-N-(quinolin-5-yl)benzamide;4-(Phenylsulfonamidomethyl)-N-(pyrazin-2-yl)benzamide;4-(Phenylsulfonamidomethyl)-N-(pyrimidin-2-yl)benzamide;4-((2-Methylphenylsulfonamido)methyl)-N-(pyridin-3-yl)benzamide;4-((2-Fluorophenylsulfonamido)methyl)-N-(pyridin-3-yl)benzamide;4-((2-Chlorophenylsulfonamido)methyl)-N-(pyridin-3-yl)benzamide;4-((2-Bromophenylsulfonamido)methyl)-N-(pyridin-3-yl)benzamide;Methyl 2-(N-(4-(Pyridin-3-ylcarbamoyl)benzyl)sulfamoyl)benzoate;N-(Pyridin-3-yl)-4-((2-(trifluoromethyl)phenylsulfonamido)methyl)benzamide;4-((2-Cyanophenylsulfonamido)methyl)-N-(pyridin-3-yl)benzamide;4-((3-Aminophenylsulfonamido)methyl)-N-(pyridin-3-yl)benzamide;4-((3-Methylphenylsulfonamido)methyl)-N-(pyridin-3-yl)benzamide;4-((3-Fluorophenylsulfonamido)methyl)-N-(pyridin-3-yl)benzamide;4-((3-Bromophenylsulfonamido)methyl)-N ...

N-myristoyl transferase inhibitors

The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors.

AZA-ARYL 1H-PYRAZOL-1-YL BENZENE SULFONAMIDES

Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists. 3. The compound of or salt thereof claim 2 , wherein Ris selected from the group consisting of: —CHCH claim 2 , —CH(CH) claim 2 , —C(CH) claim 2 , —C(CH)CHCH claim 2 , —C(CHCH)CN claim 2 , —C(OH)(CH) claim 2 , —OCH claim 2 , —OCHCH claim 2 , —OCH(CH) claim 2 , —OC(CH) claim 2 , —OCHCH(CH) claim 2 , —OCF claim 2 , and morpholino;{'sup': '2', 'Ris H, F, or Cl; or'}{'sup': '3', 'sub': 3', '3, 'Ris H, —CH, or —OCH;'}{'sup': '4', 'Ris H or F;'}{'sup': '5', 'Ris H;'}{'sup': '6', 'sub': 3', '2', '3', '3', '2', '3', '7', '2', '2', '2', '3', '3', '2', '3', '2', '2', '2, 'Ris H, —CH, —CHCH, —CH(CH), —CH, —CHF, —CHF, —CFCH, —CF, —CHOCH, —CHOH, —CHCN, —CN, or —CONH; and'}{'sup': '8', 'sub': 3', '3', '2', '3', '2', '3', '2, 'each Ris independently selected from the group consisting of H, F, Cl, Br, —CH, —OH, —OCH, —OCHCH, —NH, —N(CH), and —CN.'}4. The compound of or salt thereof claim 2 , wherein{'sup': '1', 'sub': 3', '3, 'Ris —C(CH);'}{'sup': '2', 'Ris H or F;'}{'sup': '3', 'Ris H;'}{'sup': '4', 'Ris H;'}{'sup': '5', 'Ris H; and'}{'sup': '6', 'sub': 3', '2', '2', '3, 'Ris —CH, —CHF, —CHF, or —CF.'}6. The compound of or salt thereof claim 5 , wherein{'sup': '1', 'sub': 2', '3', '3', '2', '3', '3', '3', '2', '2', '3', '2', '2', '3', '2', '3', '2', '3', '3', '2', '3', '3', '2', '3', '2', '3, 'Ris selected from the group consisting of: —CHCH, —CH(CH), —C(CH), —C(CH)CHCH, —C(CHCH)CN, —C(OH)(CH), —OCH, —OCHCH, —OCH(CH), —OC(CH), —OCHCH(CH), —OCF, and morpholino; and'}{'sup': '2', 'Ris H, F, or Cl; or'}{'sup': 1', '2, 'sub': 3', '2', '2', '3', '2', '2', '2, 'Rand ...

Anti-cancer compositions and methods

Compositions and pharmaceutical compositions including one or more selenium-containing COX-2 inhibitors are provided according to aspects of the present invention. Methods of treating a subject having or suspected of having cancer are provided according to aspects of the present invention which include administering a therapeutically effective amount of a pharmaceutical composition including a selenium-containing COX-2 inhibitor.

Acly inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

SULFONAMIDES AS GPR40- AND GPR120-AGONISTS

The invention relates to compounds acting as agonists of G-protein coupled receptor 120 (GPR120) and/or 40 (GPR40), and having formula (I): 117-. (canceled)19. The compound according to claim 18 , wherein A is phenyl claim 18 , naphthyl claim 18 , biphenyl or a saturated or unsaturated five-membered ring heterocycle having five ring atoms wherein 1 claim 18 , 2 claim 18 , 3 or 4 ring atoms are independently selected from N claim 18 , O and S.20. The compound according to claim 18 , wherein the five-membered ring heterocycle is selected from the group consisting of thienyl claim 18 , furyl claim 18 , pyrrolyl claim 18 , imidazolyl claim 18 , thiazolyl claim 18 , oxazolyl claim 18 , pyrazolyl claim 18 , isothiazolyl claim 18 , isoxazolyl claim 18 , 1 claim 18 ,2 claim 18 ,3-triazolyl claim 18 , tetrazolyl claim 18 , 1 claim 18 ,2 claim 18 ,3-thiadiazolyl claim 18 , 1 claim 18 ,2 claim 18 ,3-oxadiazolyl claim 18 , 1 claim 18 ,2 claim 18 ,4-triazolyl claim 18 , 1 claim 18 ,2 claim 18 ,4-thiadiazolyl claim 18 , 1 claim 18 ,2 claim 18 ,4-oxadiazolyl claim 18 , 1 claim 18 ,3 claim 18 ,4-triazolyl claim 18 , 1 claim 18 ,3 claim 18 ,4-thiadiazolyl claim 18 , 1 claim 18 ,3 claim 18 ,4-oxadiazolyl claim 18 , and benzimidazole claim 18 , which rings may optionally be partially saturated.21. The compound according to claim 18 , wherein R claim 18 , R claim 18 , Rare independently selected from the group consisting of —H claim 18 , -halogen claim 18 , —CF claim 18 , —OMe claim 18 , —OH claim 18 , phenyl claim 18 , —OPh claim 18 , —OCHPh claim 18 , —OCHOMe claim 18 , —OCHCN—NO claim 18 , —NH claim 18 , —NMe claim 18 , linear or branched C-Calkyl and —O(CH)—S(O)Me.22. The compound according to claim 18 , wherein n is 0 or 1.23. The compound according to claim 18 , wherein Ris in position meta on the aromatic ring.24. The compound according to claim 18 , wherein Y is a straight chain C-Chydrocarbon which may be saturated or unsaturated.25. The compound according to claim 18 , which ...

Aza-Aryl 1H-Pyrazol-yl Benzene Sulfonamides

Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists. 3. The compound of or salt thereof claim 2 , wherein{'sup': '1', 'sub': 2', '3', '3', '2', '3', '3', '3', '2', '2', '3', '2', '2', '3', '2', '3', '2', '3', '3', '2', '3', '3', '2', '3', '2', '3, 'Ris selected from the group consisting of: —CHCH, —CH(CH), —C(CH), —C(CH)CHCH, —C(CHCH)CN, —C(OH)(CH), —OCH, —OCHCH, —OCH(CH), —OC(CH), —OCHCH(CH), —OCF, and morpholino;'}{'sup': '2', 'Ris H, F, or Cl; or'}{'sup': '3', 'sub': 3', '3, 'Ris H, —CH, or —OCH;'}{'sup': '4', 'Ris H or F;'}{'sup': '5', 'Ris H;'}{'sup': '6', 'sub': 3', '2', '3', '3', '2', '3', '7', '2', '2', '2', '3', '3', '2', '3', '2', '2', '2, 'Ris H, —CH, —CHCH, —CH(CH), —CH, —CHF, —CHF, —CFCH, —CF, —CHOCH, —CHOH, —CHCN, —CN, or —CONH; and'}{'sup': '8', 'sub': 3', '3', '2', '3', '2', '3', '2, 'each Ris independently selected from the group consisting of H, F, Cl, Br, —CH, —OH, —OCH, —OCHCH, —NH, —N(CH), and —CN.'}4. The compound of or salt thereof claim 2 , wherein{'sup': '1', 'sub': 3', '3, 'Ris —C(CH);'}{'sup': '2', 'Ris H or F;'}{'sup': '3', 'Ris H;'}{'sup': '4', 'Ris H;'}{'sup': '5', 'Ris H; and'}{'sup': '6', 'sub': 3', '2', '2', '3, 'Ris —CH, —CHF, —CHF, or —CF.'}5. The compound of or salt thereof claim 3 , wherein Ris —C(CH).6. The compound of or salt thereof claim 5 , wherein{'sup': '2', 'Ris H or F;'}{'sup': '3', 'Ris H;'}{'sup': '4', 'Ris H; and'}{'sup': '6', 'sub': 3', '2', '2', '3, 'Ris —CH, —CHF, —CHF, or —CF.'}9. The composition of claim 8 , wherein{'sup': '1', 'sub': 2', '3', '3', '2', '3', '3', '3', '2', '2', '3', '2', '2', '3', '2', '3', '2', '3', '3', '2', '3', '3', '2', '3', ...

CHEMICAL COMPOUNDS

The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or pharmaceutically acceptable salts thereof: 2. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a ‘C-linked’ 5-membered heteroaryl containing one or two nitrogen atoms and one sulphur atom claim 1 , wherein said heteroaryl is optionally substituted by one or two X.3. The compound according to or a pharmaceutically acceptable salt thereof claim 2 , wherein said heteroaryl is optionally substituted by one X.4. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a ‘C-linked’ 5-membered heteroaryl containing one or two nitrogen atoms and one oxygen atom claim 1 , wherein said heteroaryl is optionally substituted by one or two X.5. The compound according to or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris a ‘C-linked’ 5-membered heteroaryl containing one nitrogen atom and one oxygen atom claim 4 , wherein said heteroaryl is substituted by one X.6. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein each Xis independently selected from: F; Cl; or (C-C)alkyl optionally substituted by one claim 1 , two or three F.7. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , Rand Rare independently selected from: H; halogen; CN; (C-C)alkyl; or (C-C)alkyloxy; and Ris selected from: halogen; CN; (C-C)alkyl; or (C-C)alkyloxy.8. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H or halogen wherein said halogen is F; Ris H; Ris halogen wherein said halogen is Cl claim 1 , Br claim 1 , or I; CN or (C-C)alkyl; and Ris H.9. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris phenyl substituted by one claim 1 , two or three X.10. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris ‘ ...

NOVEL ANTIVIRAL AGENTS AGAINST HBV INFECTION

The present invention is directed toward novel compounds and novel methods of use of said compounds of the formula (I), useful as nucleocapsid assembly inhibitors for the treatment of viruses, especially but not exclusively, including pregenomic RNA encapsidation inhibitors of HBV for the treatment of Hepatitis B virus (HBV) infection and related conditions. 161-. (canceled)63. The compound of claim 62 , wherein a substituted group is substituted with at least one selected from the group consisting of Calkyl claim 62 , Chaloalkyl claim 62 , Calkenyl claim 62 , Calkynyl claim 62 , Ccycloalkyl claim 62 , —F claim 62 , —Cl claim 62 , —Br claim 62 , —I claim 62 , —CN claim 62 , —NO claim 62 , —OR claim 62 , —SR claim 62 , —N(R) claim 62 , —NRC(O)R claim 62 , —SOR claim 62 , —SOOR claim 62 , —SON(R) claim 62 , —C(O)R claim 62 , —C(O)OR claim 62 , —C(O)N(R) claim 62 , aryl claim 62 , heterocyclyl claim 62 , or heteroaryl claim 62 , wherein each occurrence of Ris independently selected from the group consisting of hydrogen claim 62 , Calkyl claim 62 , Chaloalkyl claim 62 , Calkenyl claim 62 , Calkynyl claim 62 , and Ccycloalkyl claim 62 , or two Runits taken together with the atom(s) to which they are bound form optionally substituted 3- to 7-membered carbocyclyl or optionally substituted 3- to 7-membered heterocyclyl.64. The compound of claim 62 , wherein the heteroaryl is selected from the group consisting of diazolyl claim 62 , imidazolyl claim 62 , imidazolyl claim 62 , triazinyl claim 62 , thiazolyl claim 62 , isothiazolyl claim 62 , oxazolyl claim 62 , isoxazolinyl claim 62 , furanyl claim 62 , thiophenyl claim 62 , pyrimidinyl claim 62 , pyridinyl claim 62 , tetrazolyl claim 62 , benzofuranyl claim 62 , benzothiophenyl claim 62 , benzoxazolyl claim 62 , benzthiazolyl claim 62 , benztriazolyl claim 62 , cinnolinyl claim 62 , naphthyridinyl claim 62 , phenanthridinyl claim 62 , 7H-purinyl claim 62 , 9H-purinyl claim 62 , 6-amino-9H-purinyl claim 62 , 5H-pyrrolo[3 ...

COMPOUNDS WITH ANTIMICROBIAL ACTIVITY

This invention relates to compounds of formula 1, 2 or 3 3. A pharmaceutical composition for treatment or prevention of bacterial or protozoal infections claim 1 , comprising the compound of .4. The pharmaceutical composition of claim 3 , wherein said pharmaceutical composition is in the form of tablets claim 3 , capsules claim 3 , lozenges claim 3 , troches claim 3 , hard candies claim 3 , powders claim 3 , sprays claim 3 , creams claim 3 , salves claim 3 , suppositories claim 3 , jellies claim 3 , gels claim 3 , pastes claim 3 , lotions claim 3 , ointments claim 3 , aqueous suspensions claim 3 , injectable solutions claim 3 , elixirs claim 3 , or syrups.5. The pharmaceutical composition of claim 3 , wherein said pharmaceutical composition comprises 5% to 70% by weight of said compound.6Enterococcus faecalis, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter cloacae, Escherichia coliStreptococcus pneumoniae.. The pharmaceutical composition of claim 3 , wherein said bacterial or protozoal infections are caused by microorganism selected from the group consisting of claim 3 , and7. A method to inhibit NusB-NusE interaction in a microorganism claim 1 , comprising the step of contacting the compound of with said microorganism.8. The method of claim 7 , wherein said NusB is selected from NusB E81 claim 7 , NusB Y18 and NusB E75 claim 7 , and NusE is selected from NusE H15 claim 7 , NusE D19 and NusE R16.9Enterococcus faecalis, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter cloacae, Escherichia coliStreptococcus pneuroniae.. The method of claim 7 , wherein said microorganism is selected from the group consisting of claim 7 , and10. A method of treating or preventing bacterial or protozoal infections in a subject claim 1 , comprising a step of administering a therapeutically effective amount of the compound of to said subject.11. The method of claim 10 , ...

Oxytocin receptor agonists for the treatment of CNS diseases

The invention relates to the use of a compound of formula I 2. The method of claim 1 , wherein the compound of formula I is selected from the group consisting of4-Chloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamideN-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide4-Ethyl-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide4-Propyl-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide2-Chloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide4-Difluoromethoxy-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide4-Chloro-N-[2-(4-fluoro-phenyl)-2H-pyrazol-3-yl]-benzenesulfonamide4-Cyano-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamideN-[2-(4-Methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-4-trifluoromethyl-benzenesulfonamide4-Chloro-N-[2-(4-methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide4-Ethyl-N-[2-(4-methyl-thiazol-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamideN-(2-Pyrimidin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamide2,4-Dichloro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide4-Chloro-2-fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamide4-(1-Fluoro-ethyl)-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-benzenesulfonamideN-[2-(4-Methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-4-trifluoromethyl-benzenesulfonamide4-Chloro-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide4-Ethyl-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamide4-Cyano-N-[2-(4-methyl-pyridin-2-yl)-2H-pyrazol-3-yl]-benzenesulfonamideN-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethylsulfanyl-benzenesulfonamide4-Trifluoromethyl-N-[2-(2-trifluoromethyl-pyrimidin-4-yl)-2H-pyrazol-3-yl]-benzenesulfonamide2-Fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamideN-(2-Pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethanesulfonyl-benzenesulfonamide3-Fluoro-N-(2-pyridin-2-yl-2H-pyrazol-3-yl)-4-trifluoromethyl-benzenesulfonamideN-[2-(3-Cyclopropyl-[1,2,4]thiadiazol-5-yl)-2H-pyrazol-3-yl]-4-ethyl- ...

COMPOUNDS WITH ANTIMICROBIAL ACTIVITY

This invention relates to compounds of formula 1, 2 or 3 3. A pharmaceutical composition for treatment or prevention of bacterial or protozoal infections claim 1 , comprising the compound of .4. The pharmaceutical composition of claim 3 , wherein said pharmaceutical composition is in the form of tablets claim 3 , capsules claim 3 , lozenges claim 3 , troches claim 3 , hard candies claim 3 , powders claim 3 , sprays claim 3 , creams claim 3 , salves claim 3 , suppositories claim 3 , jellies claim 3 , gels claim 3 , pastes claim 3 , lotions claim 3 , ointments claim 3 , aqueous suspensions claim 3 , injectable solutions claim 3 , elixirs claim 3 , or syrups.5. The pharmaceutical composition of claim 3 , wherein said pharmaceutical composition comprises 5% to 70% by weight of said compound.6Enterococcus faecalis, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter cloacae, Escherichia coliStreptococcus pneumoniae.. The pharmaceutical composition of claim 3 , wherein said bacterial or protozoal infections are caused by microorganism selected from the group consisting of claim 3 , and7. A method to inhibit NusB-NusE interaction in a microorganism claim 1 , comprising the step of contacting the compound of with said microorganism.8. The method of claim 7 , wherein said NusB is selected from NusB E81 claim 7 , NusB Y18 and NusB E75 claim 7 , and NusE is selected from NusE H15 claim 7 , NusE D19 and NusE R16.9Enterococcus faecalis, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter cloacae, Escherichia coliStreptococcus pneuroniae.. The method of claim 7 , wherein said microorganism is selected from the group consisting of claim 7 , and10. A method of treating or preventing bacterial or protozoal infections in a subject claim 1 , comprising a step of administering a therapeutically effective amount of the compound of to said subject.11. The method of claim 10 , ...

PPARγMODULATORS

[과제] 지방세포의 분화의 항진을 억제하고, 줄기세포로부터 분화하는 골아세포의 형성 및 분화를 촉진시키는 퇴행기 골다공증의 치료약 또는 지방세포의 과도한 형성이나 간기능이상, 혈관장애, 심장장애 등의 성질을 갖지 않는 당뇨병 치료약이 될 수 있는 PPARγ모듈레이터를 제공하는 것을 목적으로 한다. [해결수단] 하기 화학식으로 표시되는 화합물 또는 그의 약리상 허용되는 염: (식 중, A 는 페닐기 등, B 는 아릴기 등, X 는 산소원자 등, n 은 0 또는 1 을 나타냄).

N-(1-arylpyrazol-4l) sulfonamides and their use as parasiticides

The invention relates to a sulfonamide compound of formula (I) or a pharmaceutically, veterinarily or agriculturally acceptable salt or solvate thereof, where the groups R 1 -R 5 are described in the description, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.

N-(1-arylpyrazol-4L)sulfonamides and their use as parasiticides

The invention relates to a sulfonamide compound of formula (I) or a pharmaceutically, veterinarily or agriculturally acceptable salt or solvate thereof, where the groups R 1 -R 5 are described in the description, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.

Substituted 5-carboxamidopyrazoles and substituted [1,2,4] triazoles as antiviral substances

5-membered heterocyclic compound

Disclosed is a compound having an excellent inhibitory activity on the secretion of an acid and having an anti-tumor effect and the like. Specifically disclosed is a compound represented by the formula (I) or a salt thereof. (I) wherein the ring A represents a saturated or unsaturated 5-membered heterocyclic ring having, besides a carbon atom, at least one hetero atom selected from a nitrogen atom, an oxygen atom and a sulfur atom as a ring-constituting atom; the ring-constituting atoms X1 and X2 are the same as or different from each other and independently represent C or N; the ring-constituting atoms X3 and X4 are the same as or different from each other and independently represent C, N, O or S (provided that a pyrrole ring having N as X1 is excluded from the scope of the ring A), and the ring-constituting atoms X3 and X4 may independently have a substituent selected from an alkyl which may be substituted, an acyl, a hydroxy which may be substituted, a mercapto which may be substituted, an amino which may be substituted, a halogen, a cyano and a nitro when each of the ring-constituting atom X3 or X4 is C or N; R1 and R2 independently represent a cyclic group which may have a substituent; R3 and R4 independently represent H or an alkyl or, together with the adjacent N, form a nitrogenated heterocyclic ring; and Y represents a spacer.

NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS

The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.

5-membered heterocyclic compound

Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like. A compound represented by the formula (I) or a salt thereof: wherein ring A is as defined in claim 1; R 1 and R 2 are each a cyclic group optionally having substituent(s); R 3 and R 4 are each H or alkyl, or R 3 and R 4 form, together with the adjacent N, an nitrogen-containing heterocycle; and Y is a spacer.

5-Membered heterocyclic compound

Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like. A compound represented by the formula (I) or a salt thereof: wherein ring A is a saturated or unsaturated 5-membered heterocycle containing, as a ring-constituting atom besides carbon atoms, at least one heteroatom selected from a nitrogen atom, an oxygen atom and a sulfur atom, the ring-constituting atoms X 1 and X 2 are the same or different and each is C or N, the ring-constituting atoms X 3 and X 4 are the same or different and each is C, N, O or S (provided that a pyrrole ring wherein X 1 is N is excluded from ring A), and when the ring-constituting atom X 3 or X 4 is C or N, each ring-constituting atom optionally has substituent(s) selected from an optionally substituted alkyl, an acyl, an optionally substituted hydroxy, an optionally substituted mercapto, an optionally substituted amino, a halogen, a cyano and a nitro; R 1 and R 2 are each a cyclic group optionally having substituent(s); R 3 and R 4 are each H or alkyl, or R 3 and R 4 form, together with the adjacent N, an nitrogen-containing heterocycle; and Y is a spacer.

Novel benzenesulfonamide derivatives and uses thereof

The present invention relates to a novel benzenesulfonamide derivative or a pharmaceutically acceptable salt thereof and a use thereof, and more particularly to a novel benzenesulfonamide derivative having mTORC1 (Mammalian target of rapamycin complex 1) &Lt; / RTI &gt; The benzenesulfonamide derivative of formula (I) according to the present invention inhibits the binding between LRS and RagD and thus has an excellent effect of inhibiting the activation of mTORC1. Therefore, the benzenesulfonamide derivative of formula (I) Neurodegenerative diseases such as autoimmune diseases, diabetes, obesity, respiratory-obstructive diseases, fibrosis, Pompe disease, lysosomal storage disease, Alzheimer's disease, Parkinson's disease and Huntington's disease, cardiovascular diseases and parasitic infections And can be very usefully used for the prevention or treatment of selected diseases.

Cyanoguanidine-substituted pyrazolines

Die vorliegende Erfindung betrifft das Gebiet der Blutgerinnung. Die vorliegende Erfindung betrifft insbesondere die Verwendung von Cyanoguanidin-substituierten Pyrazolinen als Arzneimittel, neue Cyanoguanidin-substituierte Pyrazoline und Verfahren zu ihrer Herstellung sowie ihre Verwendung zur Herstellung von Arzneimitteln zur Behandlung und/oder Prophylaxe von Krankheiten, insbesondere von Herz-Kreislauf-Erkrankungen, vorzugsweise von thromboembolischen Erkrankungen.

Vasopressin v1a antagonists

본 발명은 특히 식 1a에 따른 화합물에 관한 것이다. 본 발명의 화합물은 바소프레신 V 1a 수용체 길항제이다. 이러한 화합물의 약학적 조성물은 월경통 치료에 유용하다. 바소프레신, 길항제

(3-Sulfur atom substituted phenyl) pyrazole derivatives

Process for the manufacture of a sulfonamidopyrazole and intermediate products for its implementation

Aza-aryl-1-h-pyrazol-1-yl-sulphonamides

FIELD: pharmacology. SUBSTANCE: invention relates to compounds of formula (I) , in which radicals and characters have values specified in the claims and their versions. The proposed compounds act as potent antagonists of CCR (9) receptor. Animal testing has shown that these compounds are useful for treatment of inflammation, disease with a hallmark for CCR (9). The compounds as a whole are arylsulfamide derivatives and are used in pharmaceutical compositions, methods for treatment of CCR (9) mediated diseases and as a control in assays for identification of CCR (9) antagonists. EFFECT: increased efficiency of compounds application. 26 cl, 2 tbl, 33 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 401/04 (2006.01) C07D 403/04 (2006.01) C07D 401/06 (2006.01) C07D 405/14 (2006.01) C07D 471/04 (2006.01) A61K 31/4709 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A61K 31/4725 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61K 31/502 (2006.01) A61K 31/517 (2006.01) A61K 31/4375 (2006.01) (12) 2014136216, 28.02.2013 (24) Дата начала отсчета срока действия патента: 28.02.2013 04.08.2017 29.02.2012 US 61/604,998 (43) Дата публикации заявки: 20.04.2016 Бюл. № 11 (72) Автор(ы): ЧЕН Кси (US), ФАН Юнфа (US), ФАН Пингчен (US), КРАСИНСКИ Антони (US), ЛИ Лианфа (US), ЛУИ Ребекка М (US), МкМАХОН Джеффрей П. (US), Поверс Джей П. (US), ЗЕНГ Юибин (US), ЖАНГ Пенглие (US) (73) Патентообладатель(и): ХЕМОЦЕНТРИКС, Инк. (US) (45) Опубликовано: 04.08.2017 Бюл. № 22 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 29.09.2014 (56) Список документов, цитированных в отчете о поиске: EA 200901583 A1, 29.10.2010. ЕА (86) Заявка PCT: 15710 В1, 31.10.2011. WO 2005/113513 A2, 01.12.2005. US 2013/028328 (28.02.2013) C 2 (87) Публикация заявки PCT: 2 6 2 7 2 6 8 Приоритет(ы): (30) Конвенционный приоритет: C 2 A61K 31/5377 (2006.01) A61P 1/00 (2006.01) A61P 11/06 (2006.01) A61P 19/02 (2006.01) A61P 29/00 (2006.01) A61P 37/06 (2006.01) A61P 37/08 (2006.01) A61P 35/00 (2006.01) R U Дата регистрации: 2 6 2 7 ...

Pyrazol-1-yl benzene sulfonamides as ccr9 antagonists

Compounds of formula (I) are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.

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.

Process for preparing nu, nu'-methylene-bis-3- (p-amino-benzenesulfonamido) -2-phenyl-pyrazole

N-(1-arylpyrazol-4yl) sulfonamides and their use as parasiticides

The invention relates to a sulfonamide compound of formula (I) or a pharmaceutically, veterinarily or agriculturally acceptable salt or solvate thereof, where the groups R1-R5 are described in the description, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.

Pyrazol-1-yl benzene sulfonamides as CCR9 antagonists

本发明涉及作为CCR9拮抗剂的吡唑‑1‑基苯磺酰胺。提供起CCR(9)受体的有效拮抗剂作用的式(I)化合物。动物试验表明这些化合物可用于治疗炎症，一种CCR(9)的标志疾病。所述化合物总的来讲是芳基磺酰胺衍生物，可用于治疗CCR(9)介导的疾病的药物组合物、方法中，并在用于鉴定CCR(9)拮抗剂的测定法中作为对照。

Vasopressin v1a antagonists, pharmaceutical composition and use of said antagonists

antagonistas de vasopressina v1a a presente invenção concerne a compostos, entre outras coisas, de acordo com a fórmula geral 1a. os compostos de acordo com a invenção são antagonistas de receptor de vasopressina v~ 1a~. as composições farmacêuticas das compostos são úteis como tratamento de dismenorréia. Vasopressin Antagonists v1a The present invention relates to compounds, among other things, according to general formula 1a. The compounds according to the invention are vasopressin receptor antagonists. The pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhea.

Nitrogen containing heteroaromtics as factor XA inhibitors

PPAR- modulators

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.

Novel sulfonamides and process for their preparation

SULPHONYLAMINE-CARBOXYLIC ACIDS N-ARILAMIDS REPLACED WITH SULFUR, PROCEDURE FOR THE PREPARATION AND PREPARATION OF PHARMACEUTICAL CONTAINING THEM

N-arilamidas de ácidos sulfonilamino-carboxílicos sustituidas con azufre, de la fórmula (1), en la cual A1 representa un radical bivalente de la serie fenileno, naftileno y heteroarileno, todos los cuales pueden estar sustituidos por uno o más sustituyentes, iguales o diferentes, seleccionados de la serie consistente en: halógeno, alquilo C1-5, fenilo, tolilo, CF3, NO2, OH, -O-C1-5-alquilo, -O-O-C2-4-alquil-O-C1-3-alquilo, C1-2-alquilendioxi, NH2, -NH-C1-3-alquilo, -N(C1-3-alquilo)2, -NH-CHO, -NH-CO-C1-5-alquilo, -CN, -CO-NH2, -CO-C1-3-alquilo, -CO-N(C1-3-alquilo)2, -CO-OH, -CO-O-C1-5-alquilo, heterociclilo, CHO, -CO-(C1-5-alquilo)2, -S(O)n-C1-4-alquilo, -S(O)n-fenilo y -S(O)n-tolilo; el anillo A2, que abarca los átomos de carbono que llevan los grupos C(=X)-NH- y NH-SO2R2, representa un anillo benzol, un anillo naftalina, un carbociclo de 3 a 7 miembros, saturado o parcialmente no saturado, un heterociclo monocíclico de 5 a 7 miembros, saturado, parcialmente no saturado, o aromático, que contiene uno o más heteroátomos de anillo seleccionados de la serie consistente en N, O y S, o un heterociclo bicíclico de 8 a 10 miembros, saturado, parcialmente no saturado, o aromático, que lleva uno o varios heteroátomos de anillo seleccionados de la serie consistente en N, O y S; R1 representa arilo, heterociclilo o C1-18-alquilo, que puede estar sustituido por uno o más radicales R4, iguales o diferentes, o cuando el número n en el grupo R1-S(O)n- vale 2, también representa NR5R6, o cuando el número n en el grupo R1-S(O)n- vale 0, también representa -CN; R2 representa arilo, heterociclilo, NR5R6 o alquilo C1-10 que puede estar sustituido por uno o más radicales R4, iguales o diferentes; R3 representa uno o más radicales, iguales o diferentes, seleccionados de entre la siguiente serie: hidrógeno, halógeno, CF3, OH, -O-C1-7-alquilo, -O-C2-4-alquil-O-C1-7-alquilo, -O-arilo, C1-2-alquilendioxi, NO2, -CN, NR7R8, -CO-NR7R8, -CO-OH, -CO-C1-5-alquilo, heterociclilo, S(O)n-C1-5- ...

Aza-aryl 1h-pyrazol-1-yl benzene sulfonamides as ccr(9) antagonists

Vasopressin v1a antagonists

本发明尤其涉及按照通式1a的化合物。按照本发明的化合物是血管升压素V 1a 受体拮抗剂。该化合物的药物组合物用作治疗痛经。

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.

Aza-aryl 1H-pyrazol-1-YL benzene sulfonamides

Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.

Novel antiviral agents against hbv infection

The present invention is directed toward novel compounds and novel methods of use of said compounds of the formula (I), useful as nucleocapsid assembly inhibitors for the treatment of viruses, especially but not exclusively, including pregenomic RNA encapsidation inhibitors of HBV for the treatment of Hepatitis B virus (HBV) infection and related conditions. (Formula (I)) Including hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein A, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are defined herein.

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

Novel thiolesters and uses thereof

This invention pertains to the discovery of a novel family of thiolesters and uses thereof. Also provided for are viricidal compounds and pharmaceutical formulations comprising these novel thiolesters. The invention also provides thiolester-inactivated viruses and thiolester-complexed viral proteins.

N-(1-arylpyrazol-4yl) sulfonamides and their use as parasiticides

The invention relates to a sulfonamide compound of formula (I) or a pharmaceutically, veterinarily or agriculturally acceptable salt or solvate thereof, where the groups R1-R5 are described in the description, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.

Compounds and compositions for treating conditions associated with sting activity

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

Sulfonamides as gpr40- and gpr120-agonists

The invention relates to compounds acting as agonists of G-protein coupled receptor 120 (GPR120) and/or 40 (GPR40), and having formula (I). Said compounds are useful in the treatment of diseases or disorders modulated by GPR120 and/or GPR40 such as diabetes (particularly type 2 diabetes), impaired oral glucose tolerance, insulin resistance, obesity, obesity related disorders, metabolic syndrome, dyslipidemia, elevated LDL, elevated triglycerides, obesity induced inflammation, osteoporosis and obesity related cardiovascular disorders.

Pyrazol-1-yl benzene sulfonamides as ccr9 antagonists ccr9 -1-

Small molecule inhibitors of the pleckstrin homology domain and methods for using same

Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

5-SULPHONAMIDO-1-ARYL-PYRAZOLES, THEIR PREPARATION AND USE AS HERBICIDES

PRODUCTION AND USE OF ORTHO-SULFONAMIDO-HETEROARYLHYDROXAMIC ACIDS AS MATRIX METALLOPROTEINASE AND TACE INHIBITORS

Amino pyrazole derivatives useful for the treatment of obesity and other disorders

Amino pyrazole derivatives of the formula: which are ligands for the neuropeptide Y, subtype 5 receptor and pharmaceutical compositions containing an amino pyrazole derivative as the active ingredient are described. The amino pyrazole derivatives are useful in the treatment of disorders and diseases associated with the NPY receptor subtype Y5.

Sulfur-substituted N-arylamides of sulfonylaminocarboxylic acid, process of their preparation, their use and pharmaceutical preparations in which they are comprised

therapeutic active compositions and their method of use

composições ativas terapêuticas e seu métodos de uso. são fornecidos métodos para tratar um câncer caracterizado pela presença de um alelo mutuante de idh1 compreendendo administrar a um sujeito em necessidade do mesmo um composto descrito aqui. therapeutic active compositions and their methods of use. Methods are provided for treating a cancer characterized by the presence of an idh1 mutant allele comprising administering to a subject in need thereof a compound described herein.

PPAR gamma modulators

The present invention has a purpose for providing a PPAR gamma modulator which can be a therapeutic agent for retrograde osteoporosis in which excessive differentiation of adipocytes was inhibited and formation and differentiation of osteoblasts from stem cells is facilitated or that for diabetes mellitus without characteristics such as excessive adipogenesis, liver dysfunction, vascular disorders, heart diseases and the like. ÄSolutionÜ A compound of the following formula or a pharmacologically acceptable salt thereof: <CHEM> wherein A represents a phenyl group or the like, B represents an aryl group or the like, X represents an oxygen atom or the like, and n represents 0 or 1.

Sulfur substituted sulfonylaminocarboxylic acid nm-arylamides, their preparation, their use and pharmaceutical preparations comprising them

Vasopressin v1a antagonists

본 발명은 특히 식 1a에 따른 화합물에 관한 것이다. 본 발명의 화합물은 바소프레신 V 1a 수용체 길항제이다. 이러한 화합물의 약학적 조성물은 월경통 치료에 유용하다. 바소프레신, 길항제

Novel antiviral agents against hbv infection

구체적으로 B형 간염(HBV) 및 관련 상태 치료를 위하여 HBV의 프레게놈(pregenomic) RNA 포집화(encapsidation) 저해제를 포함하나, 이에 국한되지 않는 바이러스 치료를 위한 뉴클레오캡시드 어셈블리 저해제로써 유능한 화학식 (I)의 신규한 화합물들과 이들 화합물들을 이용하는 신규한 방법들에 관한 것이다. 이의 수화물, 용매화합물, 약제학적으로 수용가능한 염들, 전구약물 그리고 이들의 복합물들이 포함되며, 여기서 A, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , 그리고 R 8 은 본 명세서에서 정의된 바와 같다. (I) as a nucleoside assembly inhibitor for the treatment of viruses, including, but not limited to, pregenomic RNA encapsidation inhibitors of HBV for hepatitis B (HBV) ) And novel methods of using these compounds. R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are independently selected from the group consisting of hydrates, solvates, pharmaceutically acceptable salts, prodrugs, Lt; / RTI &gt; are as defined herein.

Vasopressin via antagonists

The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of primary dysmenorrhoea. (see formula 1a)

Sulfonylaminocarboxylic acid N-arylamides substituted with sulfur

Bu bulus A1,A2,R1,R2,R3,X ve n'nin istemlerde tanimlandigi gibi oldugu formül (I)'in bilesikleri ile ilgilidir ve bu bilesikler örnegin yüksek tansiyon,angina pectrois, kalp yetmezligi, tromboz ya da aterosklerosis gibi kalp damar hastaliklari gibi hastaliklarin tedavisi ve önlenmesinde kullanilabilen ve farmakolojik olarak etkin degerli bilesiklerdir. Formül formül I'e ait bilesikler bedendeki döngüsel guanosin monofosfat (cGMP) üretimini ayarlayabilme yetisine sahiptir ve genelde dagitilmis bir cGMP dengesi ile iliskili olan hastaliklarin tedavisi ve önlenmesinde kullanilmaya uygundurlar. This invention relates to compounds of formula (I) wherein A1, A2, R1, R2, R3, X, and n are as defined in the claims, and these compounds are cardiovascular, such as high blood pressure, angina pectrois, heart failure, thrombosis, or atherosclerosis. They are pharmacologically effective valuable compounds that can be used in the treatment and prevention of diseases such as diseases. The compounds of formula formula I have the ability to adjust the production of cyclic guanosine monophosphate (cGMP) in the body and are generally suitable for use in the treatment and prevention of diseases associated with a distributed cGMP balance.

Compositions useful as inhibitors of voltage-gated ion channels

Ppargamma modulators

New sulfonamides which can be used in therapy, in particular as chemotherapeutic agents.

Substituted biphenyl isoxazole sulfonamides

Pyrazolodiazepinone compounds

Compounds of the general formula (R 1 =Me, Et R 2 =alkyl(<4C), allyl R 3 =H, Me X 1 =H, Cl, CF 3 ) and their salts are prepared by (a) reacting a compound of the formula with a C 1-4 alkyl ester of glycine. or a salt thereof, (b) reacting a compound of the formula (X 2 =Br, Cl, I) or a salt thereof with ammonia, (c) cyclizing a compound (which may be prepared in situ) of the formula or (d) reacting a compound of the formula with X 2 CH 2 COX 3 (X 3 = Br, Cl) in the presence of a base, optionally followed in each case by methylation and/or salt formation with an acid or (when R 3 =H) base. The preparation of 1,3-dimethyl-4-nitropyrazole - 5 - carboxylic acid, 1 - ethyl - 3 - methyl- 4 - nitropyrazole - 5 - carboxylic acid, 1 - isopropyl - 3 - methyl - 4 - nitropyrazole - 5 - carboxylic acid, 3 - ethylpyrazole - 5 - carboxylic acid ethyl ester, 3-ethyl-1-methylpyrazole-5-carboxylic acid monohydrate, 3-ethyl-1-methyl-4-nitropyrazole - 5 - carboxylic acid, 1,3 - diethylpyrazole - 5 - carboxylic acid ethyl ester, 1,3- diethylpyrazole - 5 - carboxylic acid, 1,3 - diethyl - 4 - nitropyrazole - 5 - carboxylic acid, 4 - amino - -1 - ethyl - 3 - methylpyrazole - 5 - carboxylic acid, 5 - benzoyl - 1,3 - dimethyl - 4 - nitropyrazole, 5 - benzoyl - 1 - ethyl - 3 - methyl - 4 - nitropyrazole, 5 - benzoyl - 1 - isopropyl - 3 - methyl- 4 - nitropyrazole, 5 - benzoyl - 3 - ethyl - -1 - methyl- 4 - nitropyrazole, 5 - benzoyl - 1,3 - diethyl - 4 - nitropyrazole, 4 - amino - 5 - benzoyl - 1,3 - di - methylpyrazole and its hydrochloride, 4 - amino- 5 - benzoyl - 1 - ethyl - 3 - methylpyrazole and its hydrochloride monohydrate, 4 - amino - 5 - benzoyl - 1 - isopropyl - 3 - methylpyrazole and its hydrochloride, 4 - amino - 5 - benzoyl - 3 - ethyl- 1 - methylpyrazole, 4 - amino - 5 - benzoyl - 1,3- diethylpyrazole and its - hydrochloride, 4 - bromo - 1 - (2,3 - dibromopropyl) - 3 - methylpyrazole - 5 - carboxylic acid, 1 - allyl - 4 - bromo - 3 - methylpyrazole - 5 - carboxylic acid, 1 ...

N-myristoyl transferase inhibitors

The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors.

PYRAZOL-1-YL BENZENE SULFONAMIDES AS CCR9 ANTAGONISTS, THEIR COMPOSITION AND METHOD OF MODULATE CCR FUNCTION(9) IN A CELL

PIRAZOL-1-IL BENZENO SULFONAMIDAS COMO ANTAGONISTAS DE CCR9. Os compostos de fórmula I são proporcionados os quais atuam como antagonistas potentes do receptor CCR (9). Os testes em animais demonstram que esses compostos são úteis para o tratamento de inflamação, uma doença de marca para CCR (9). Os compostos são geralmente derivados de aril sulfonamida e são úteis em composições farmacêuticas, métodos para o tratamento de doenças mediadas por CCR (9), e como controles em ensaios para a identificação de antagonistas CCR (9). PYRAZOL-1-YL BENZENE SULFONAMIDES AS CCR9 ANTAGONISTS. Compounds of formula I are provided which act as potent CCR receptor antagonists (9). Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for RCC (9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for treating CCR-mediated diseases (9), and as controls in assays for the identification of CCR antagonists (9).

Novel antiviral agents against hbv infection.

La presente invención se orienta a nuevos compuestos y nuevos métodos de uso de dichos compuestos de la fórmula (I), útiles como inhibidores de agrupaciones de nucleocápside para el tratamiento de virus, especialmente, pero no en forma exclusiva, que incluye los inhibidores de encapsidación del ARN pregenómico del VHB para el tratamiento de la infección por el virus de la Hepatitis B (VHB) y afecciones relacionadas; inclusive hidratos, solvatos, sales farmacéuticamente aceptables, profármacos y complejos de estos, donde A, R1, R2, R,3 R4, R5, R6, R7 y R8 se definen en la presente.

Protein-protein interaction stabilizers

Provided herein, inter alia , are stabilizers of protein-protein interactions and methods of identifying and using the same.

4,6-dihydro-pyrazolo [43-e] [1,4] diazepin-5-one compounds

Novel antiviral agents against hbv infection

The present invention is directed toward novel compounds and novel methods of use of said compounds of the formula (I), useful as nucleocapsid assembly inhibitors for the treatment of viruses, especially but not exclusively, including pregenomic RNA encapsidation inhibitors of HBV for the treatment of Hepatitis B virus (HBV) infection and related conditions. (Formula (I)) Including hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein A, R1, R2, R3, R4, R5, R6, R7, and R8 are defined herein.

Photographic silver halide material containing 2-equivalent yellow couplers

Desirable 2-equivalent yellow couplers carry at the coupling position a monocyclic pyrrole, diazole or triazole ring attached to the coupling position of the yellow coupler by a nitrogen atom, which ring can be split off in the coupling reaction. Photographic 2-equivalent yellow couplers with nitrogen-containing heterocyclic splittable groups having such nitrogen bonded to the coupling position of the couplers, are prepared by reacting a corresponding 2-equivalent yellow coupler containing a halogen such as chlorine in the coupling position with the nitrogen-containing heterocyclic compound that supplies the splittable group, in the presence of base and in the further presence of hexamethylphosphoric acid triamide as solvent.

INHIBITION OF THE ACTIVITY OF P38 CINASA USING REPLACED HETEROCYCLIC UREAS.

Un método para el tratamiento de una enfermedad mediada por p38 distinta del cáncer, que comprende administrar un compuesto de fórmula I **fórmula** en la cual B es un resto arilo o heteroarilo hasta tricíclico sustituido o no sustituido que puede tener hasta 30 átomos de carbono que tiene al menos una estructura aromática de 5 ó 6 miembros que contiene 0-4 miembros del grupo constituido por nitrógeno, oxígeno y azufre, en la cual si B es un grupo sustituido, está sustituido conunoo más sustituyentes seleccionados independientemente del grupo constituido por halógeno, hasta perhalosustitución, y Xn, en el cual n es 0-3 y cada X se selecciona independientemente del grupo constituido por -CN, -CO2R5,-C(O)NR5 R5'', -C(O)R5, -NO2, -OR5, -SR5, -NR5 R5'', -NR5 C-(O)-OR5'', -NR5 C(O)R5'', alquilo C1-C10, alquenilo C2-C10, alcoxi C1-C10, cicloalquilo C3-C10, arilo C6-C14, alcarilo C7-C24, heteroarilo C3-C13, alc-heteroarilo C4-C23, alquilo C1-C10 sustituido, alquenilo C2-C10 sustituido, alcoxi C1-C10 sustituido, cicloalquilo C3-C10 sustituido, alc-heteroarilo C4-C23 sustituido e -Y-Ar; en el cual si X es un grupo sustituido, está sustituido con uno o más sustituyentes seleccionados independientemente del grupo constituido por -CN, -CO2R5, -C(O)R5, -C(O)NR5 R5'', -OR5, -SR5, -NR5 R5'',-NO2, -NR5 C-(O)R5'',-NR5 C-(O)OR5'', y halógeno hasta per-halosustitución; donde R5 y R5'' se seleccionan independientemente de H, alquilo C1-C10, alquenilo C2-C10, cicloalquilo C3-C10, arilo C6-C14, heteroarilo C3-C13, alcarilo C7-C24, alc-heteroarilo C4-C23, alquilo C1-C10 hasta per-halosustituido, cicloalquilo C3-C10 hasta per-halosustituido, alquenilo C2-C10 hasta per-halosustituido,arilo C6-C14 hasta per-halosustituido y heteroarilo C3-C13 hasta per-halosustituido,donde Y es -O-, -S-, -N(R5 )-, -(CH2)-m, -C(O)-, -CH(OH)-, -(CH2)mO-, -(CH2)mS-, -(CH2)mN(R5 )-, -O(CH2)m-, -CHX a -, -NR5 C(O)NR5 R5''-, -NR5 C(O ...

Sulfonamide compounds and their use as tnap inhibitors

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 ...

AMINO PIRAZOL DERIVATIVES USED IN THE TREATMENT OF OBESITY AND OTHER DISORDERS.

Un compuesto de **fórmula** en la que cada R1 y R2 se selecciona independientemente entre el grupo compuesto por hidrógeno, alquilo C1-C6, sulfonilamino, y arilsulfonilo no sustituido o sustituido; siendo los sustituyentes del arilsulfonilo uno o más sustituyentes seleccionados independientemente entre halógeno, alquilo C1-C6, alcoxi C1-C6, trifluorometilo o trifluorometoxi; R3 se selecciona entre el grupo compuesto por arilo no sustituido o sustituido y heteroarilo no sustituido o sustituido; siendo los sustituyentes del arilo o heteroarilo uno o más sustituyentes seleccionados independientemente entre halógeno, alquilo C1-C6, alcoxi C1- C6, trifluorometilo, trifluorometoxi, amino, alquilamino C1- C6 o di(alquil C1-C6)amino; L se selecciona entre el grupo compuesto por arilo no sustituido o sustituido, heteroarilo no sustituido o sustituido y cicloalquilo C3-C8; siendo los sustituyentes del arilo o heteroarilo uno o más sustituyentes seleccionados independientemente entre halógeno, alquilo C1- C4 o trifluorometilo; n es un entero seleccionado entre 0 o 1; X se selecciona entre el grupo compuesto por sulfonilamino, aminocarbonilo, carbonilo, carbonilamino, sulfonilo, sulfonilaminoalquilo C1-C6, alquil C1-C6- aminosulfonilo, y di(arilsulfonilo no sustituido o sustituido)-amino; siendo los sustituyentes del grupo arilo uno o más sustituyentes seleccionados independientemente entre halógeno, alquilo C1-C6, alcoxi C1-C6, trifluorometilo, trifluorometoxi, alquil C1-C6- carbonilamino, amino, alquilamino C1-C6 o di(alquil C1- C6)amino, y donde los dos grupos arilo del di(arilsulfonilo no sustituido o sustituido)amino tienen el mismo patrón de sustitución. A compound of ** formula ** in which each R1 and R2 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, sulfonylamino, and unsubstituted or substituted arylsulfonyl; the arylsulfonyl substituents being one or more substituents independently selected from halogen, C1-C6 alkyl, C1-C6 alkoxy, ...

Sulfur substituted sulfonylaminocarboxylic acid N-arylamides, their preparation, their use and pharmaceutical preparations comprising them

The present invention relates to compounds of the formula I wherein A 1 , A 2 , R 1 , R 2 , R 3 , X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.

SUBSTITUTED 5-CARBOXYAMIDE PYRAZOLES AND Ä1,2,4ÜTRIAZOLE AS VIRUZIDE

Substituted 5-carboxyamide pyrazoles and [1,2,4]triazoles as antiviral agents

The present invention provides compounds of formula I wherein X, Y, R1-R7 are as defined herein. Compositions containing these compounds, and methods for inhibiting HCV RNA-dependent RNA polymerase and treating hepatitis C and related disorders using these compounds and compositions are also provided. (I)

N-myristoyl transferase inhibitors

The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors.

Heteroaryl acetylenic sulfonamide and phosphinic acid amide hydroxamic acid tace inhibitors.

Heterocycle-benzoic acid derivatives, pharmaceutical compositions comprising them and uses thereof

The present invention relates to compounds with vasopressin V1a antagonist activity and to pharmaceutical compositions comprising such compounds. The present invention also relates to the use of vasopressin V1a antagonists for the treatment of certain physiological disorders, such as Raynaud's disease and dysmenorrhoea (primary dysmenorrhoea and/or secondary dysmenorrhoea).

5-CARBOXIAMIDO PIRAZOLES AND (1,2,4) TRIAZOLS AS ANTIVIRAL AGENTS.

Un compuesto de Fórmula (I): **(Ver fórmula)** o una sal, solvato o éster del mismo farmacéuticamente aceptable, en la cual: X es C(R8) o N; R8 es H; halo, CF3, alquilo C1-C6, haloalquilo C1-C6, -OH, -SH, alcoxi C1-C6, alquiltio C1-C6, -NH2, -NH(alquilo C1-C6) o -N(alquilo C1-C6)2; Y es C(O) o S(O)2; R1 es -CO2R9, -C(O)R9, -C(O)NR9R10, -NR9C(O)R10, -NR9SO2R10, -NR9SO2NR9R10, -C(O)N(R9)OR10, -NR9C (O)NR9R10, -NR9C(O)OR10, -C(O)NR9SO2R10, -C(O)NR9NR9R10, -CN,-NR9C(O)CF3, -NR9SO2CF3, -CH=NOR21, -C(O)NR9CN, -C(O)NR9(CR19R20)1-12R11, -C(O)N((R19R20)1-12R11)2, -NR9C(O)NR9(CR19R20)1-12CO2R9, H, -OH, hidroxialquilo C1-C6, alquilo C1-C6, tetrazolilo no sustituido, tetrazolilo sustituido con uno o más restos que pueden ser iguales o diferentes y que son seleccionados independientemente del grupo que consta de alquilo, cicloalquilo, halo y arilo, tienilo no sustituido, tienilo sustituido con uno o más restos que pueden ser iguales o diferentes y que son seleccionados independientemente del grupo que consta de alquilo, cicloalquilo, halo y arilo; R2 es cicloalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, alquilo o cicloalquilo, donde cada miembro de R2 está sustituido opcionalmente con 1-4 restos R12; R3 es H o alquilo C1-C6; R4 es H, alquilo C1-C6 o alcoxi C1-C6; R5 es H, alquilo C1-C6 o alcoxi C1-C6; R6 es cicloalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, alquilo o cicloalquilalquilo, donde cada miembro de R2 está sustituido opcionalmente con 1-4 restos R12; R7 es H o alquilo C1-C6; o R6 y R7, cuando están unidos al mismo nitrógeno, son opcionalmente tomados junto con el nitrógeno unido para formar un anillo de cinco a siete miembros que tiene 0-1 heteroátomo adicional seleccionado de N, O o S (además de dicho nitrógeno unido), donde dicho anillo de cinco a siete miembros está sustituido opcionalmente con 1-3 restos R18; cada R9 es independientemente H, alquilo, cicloalquilo, cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, ...

Compound with antibacterial activity

本发明涉及具有化学式1、2或3的化合物， 以及其药学上可接受的盐和溶剂化物，其特征在于X 1 ,Y,R 1 ,R 2 ,R 3 ,R 4 ,and R 5 均如本文所定义。所述化合物乃抗菌剂，可用于治疗各种细菌和原虫感染以及与此类感染有关的疾病。本发明亦涉及含有所述化合物的药物组合物，以及通过施用具有化学式1、2或3的化合物以治疗细菌和原虫感染的方法。

New sulphonamides and process for preparing same

C2C The invention comprises sulpha-pyrazole compounds of the formula: <FORM:0955303/C2/1> wherein R is an isopropyl, n-butyl, secondary butyl or pentyl-(3) group and salts, such as alkali-metal, alkaline earth metal or earth metal salts, thereof, together with the corresponding intermediate 2-substituted-3-p-acetylaminobenzenesulphonamide-pyrazoles. The sulpha-pyrazoles are made by reacting a p-acetylaminobenzenesulphonyl chloride with a 2-R-3-aminopyrazole and hydrolysing the resulting acetylsulphanilyl-pyrazole. 2-R-3-Amino-pyrazoles wherein R is isopropyl, n-butyl, or pentyl-(31) are made by hydrolyzing and decarboxylating the corresponding 4-carbethoxy compound. 2-Secondary-butyl-3-amino pyrazole is made by heating the 4-cyano compound with concentrated hydrochloric acid. Pharmaceutical and veterinary preparations for the treatment of bacterial infections comprise the above sulpha-pyrazole compounds in admixture or conjunction with an organic or inorganic, solid or liquid carrier suitable for enteral, parenteral or local administration. The preparations may suitably take the form of tablets, dragees, ointments, creams, solutions, suspensions or emulsions, or, for veterinary use, an animal feedstuff or feedstuff additive.

Nitrogen-containing heteroaromatic compounds as factor Xa inhibitors

Therapeutically active compositions and methods of their use