СИНТЕЗ АМИДОВ 6,7,-ДИГИДРО-5Н-ИМИДАЗО [1.2-А] ИМИДАЗОЛ-3-СУЛЬФОНОВОЙ КИСЛОТЫ

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2007 106 927 (13) A (51) ÌÏÊ C07D 487/04 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007106927/04, 25.07.2005 (71) Çà âèòåëü(è): ÁÅÐÈÍÃÅÐ ÈÍÃÅËÜÕÀÉÌ ÈÍÒÅÐÍÀÖÈÎÍÀËÜ ÃÌÁÕ (DE) (30) Êîíâåíöèîííûé ïðèîðèòåò: 27.07.2004 US 60/591,398 (43) Äàòà ïóáëèêàöèè çà âêè: 10.09.2008 Áþë. ¹ 25 (87) Ïóáëèêàöè PCT: WO 2006/014828 (09.02.2006) Àäðåñ äë ïåðåïèñêè: 101000, Ìîñêâà, Ì.Çëàòîóñòèíñêèé ïåð., ä.10, êâ.15, "ÅÂÐÎÌÀÐÊÏÀÒ", È.À.Âåñåëèöêîé (57) Ôîðìóëà èçîáðåòåíè 1. Ñïîñîá ïîëó÷åíè ñîåäèíåíè ôîðìóëû I R U A 2 0 0 7 1 0 6 9 2 7 A (54) ÑÈÍÒÅÇ ÀÌÈÄΠ6,7,-ÄÈÃÈÄÐÎ-5Í-ÈÌÈÄÀÇÎ [1.2-À] ÈÌÈÄÀÇÎË-3-ÑÓËÜÔÎÍÎÂÎÉ ÊÈÑËÎÒÛ â êîòîðîé R 1 âûáðàí èç ãðóïïû, âêëþ÷àþùåé áðîì, òðèôòîðìåòîêñèãðóïïó, öèàíîãðóïïó è ïèðèìèäèí-5-èë, íåîá çàòåëüíî ìîíî- èëè äèçàìåùåíûé ñ ïîìîùüþ NH2; è R 2 è R 3 âñå íåçàâèñèìî âûáðàíû èç ãðóïïû, âêëþ÷àþùåé (A) âîäîðîä; è Ñòðàíèöà: 1 RU 2 0 0 7 1 0 6 9 2 7 (86) Çà âêà PCT: US 2005/026147 (25.07.2005) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 27.02.2007 (72) Àâòîð(û): ÂÀÍ Ñ îöóíü (US), ÂÈÐÒ Òîìàñ (DE), ÍÈÊÎËÀ Òîìàñ (DE), ×ÆÀÍ Ëè (US), ÔÐÓÒÎÑ Ðîõåëèî-Ïåðåñ (US), ÑÞÉ Èáî (US), ÐÈÂÑ Äàéàíà Ñ. (US), ÊÐÈØÍÀÌÓÐÒÈ Äõèëååïêóìàð (US), ÍÀÌÌÈ Ëîðåíñ Äæîí (US), ÂÀÐÑÎËÎÍÀ Ðè÷àðä Äæ. (US), ÊÐÅÁÅÐ Þòòà (DE), ÑÅÍÀÍÀßÊÅ Êðèñ Õüþ (US) A 2 0 0 7 1 0 6 9 2 7 R U ãäå R 6 è R 7 íåçàâèñèìî âûáðàíû èç ãðóïïû, âêëþ÷àþùåé Í è ëèíåéíûé è çàìåùåííûé Ñ1-Ñ4àëêèë, íåîá çàòåëüíî çàìåùåííûé ñ ïîìîùüþ ÎÍ. 3. Ñïîñîá ïî ï.1, â êîòîðîì ñîåäèíåíèå ôîðìóëû XXII ïîëó÷àþò ñïîñîáîì, âêëþ÷àþùèì Ñòðàíèöà: 2 A R 2 è R 3, ñîâìåñòíî ñ àòîìîì àçîòà, ñ êîòîðûì îíè ñâ çàíû, îáðàçóþò ôðàãìåíò, âûáðàííûé èç ãðóïïû, âêëþ÷àþùåé è 2 0 0 7 1 0 6 9 2 7 2. Ñïîñîá ïî ï.1, â êîòîðîì R 1 âûáðàí èç ãðóïïû, âêëþ÷àþùåé áðîì, òðèôòîðìåòîêñèãðóïïó, öèàíîãðóïïó è ïèðèìèäèí-5-èë; R 2 îáîçíà÷àåò Í; è R 3 îáîçíà÷àåò -CH(R 8)C(O)NH2, ãäå R 8 îáîçíà÷àåò ëèíåéíóþ èëè ðàçâåòâëåííóþ C1-Ñ3àëêèëüíóþ ãðóïïó; ...

SUBSTITUIERTE HETEROCYCLISCHE VERBINDUNGEN UND DEREN VERWENDUNG ZUR BEHANDLUNG MULTIPLER MEDIKAMENTENRESISTENZ

Verfahren zur Aufhebung des durch optische Aufheller erzielten Aufhelleffektes

FUSED RING INDOLE DERIVATIVES

... 1366133 Fused-ring indolines JOHN WYETH & BRO Ltd 14 Dec 1971 [11 Jan 1971 2 Sept 1971 6 Dec 1971] 1250/71 40959/71 and 56467/71 Heading C2C The invention comprises compounds of formula and their acid addition or quaternary ammonium salts, wherein R is OH (or its C 1-6 alkyl, aryl- C 1-6 -alkyl or tetrahydropyracyl ether, or ester derivative); R1 is aryl (mono- or bicyclic), C 1-6 alkyl (possibly aryl- or amino-substituted), or up to C 6 alkenyl or alkynyl; or RR1 is O=, or (when n is 1) its alkylene or di-(C 1-6 alkyl) ketal; R2, R5 are each H, OH, halogen, NH 2 (possibly mono- or di-C 1-6 -alkyl substituted), or C 1-6 alkyl, haloalkyl or alkoxy, or (when RR1 is O = or a ketal thereof) NO 2 ; R3, R4 are each H or C 1-6 alkyl, or R3 is H and R4 is OH; n is 0-2; and R6 (present only when the optional bond represented by the broken line is absent) is H, acyl, C 1-6 alkyl (possibly substituted by aryl ...

CHLORINATED MANDELAMIDINES

... 1415709 Chlorinated mandelamidines M SOUCHARD 23 Nov 1973 [24 Nov 1972] 54618/73 Heading C2C Novel 2 - ( - hydroxy - 2 - chlorobenzyl)- #2-imidazoline, in the form of its hydrochloride salt, is prepared by treating o-chlorobenzaldehyde with aqueous sodium bisulphite, aqueous KCN and HCl and reacting the resulting 2-chloromandeliminoethyl ether hydrochloride with ethylene diamine. Novel 2 - ( - acetyloxy - 2 - chlorobenzyl)- #2-imidazoline, in the form of its hydrochloride salt, is prepared by treating 2-(-hydroxy-2- chlorobenzyl) - #2 - imidazoline hydrochloride with acetic anhydride. Novel 3,4 - dichloromandelamidrazone, in the form of its hydrochloride salt, is prepared by reacting 3,4-dichloromandeliminoethyl ether hydrochloride with hydrazine monohydrate. Novel. 2 - ( - hydroxy - 2,6 - dichlorobenzyl)- #2 - imidazoline, in the form of its hydrochloride salt, is prepared by reacting 2,6- dichloromandelimino-ethyl ether hydrochloride with ethylene diamine ...

NITROMETHYLENE HEXAHYDROPYRIMIDINES

NITROMETHYLENE HEXAHYDROPYRIMIDINES

Novel Cyclic and Non-Cyclic Amidines as Anthelmintic Agents

... 1,195,455. Styryl cyclic amidines. CHAS. PFIZER & CO. Inc. 8 Feb., 1968 [9 Nov., 1967], No. 6399/68. Addition to 1,131,847. Heading C2C. Novel compounds of formula wherein R 1 is SH or alkylthio and Z is ethylene or trimethylene, are prepared either by reacting a compound of Formula II wherein X is vinylene and W is cyano or an imino ester group with an amine of formula H 2 N-Z-NHCH 3 or where W in II is of formula with dimethylamine or by reacting a compound wherein -X-W in Formula II is CHO with a compound of formula Anthelmintic compositions comprise an above novel compound or salt and a carrier therefor and may be in forms suitable for oral or parenteral administration.

Cyclic amidines and compositions containing them

A liquid hydrocarbon fuel has dissolved therein at least one cyclic amidine of the general formula wherein R1 is C1-C24 alkyl, phenyl, naphthyl, benzyl, or said aryl groups substituted with one or more alkyl groups contributing a total of not more than 16 carbon atoms; R2 is hydrogen or C1-C24 alkyl; or R1 and R2 together with the nitrogen atom to which they are joined represent a morpholino, thiamorpholino, piperidino or pyrrolidinyl group; X represents ethylene, ethenylene, trimethylene, alkyl- or alkenyl-substituted ethylene having a total of up to 20 carbon atoms, 1,2-cyclohexylene or alkyl-substituted 1,2-cyclohexylene having a total of up to 16 carbon atoms, 1,2-cyclohexenylen or alkyl-substituted 1,2-cyclohexenylene having a total of up to 16 carbon atoms, 3,6-methano-1,2 - cyclohexylene and 3,6 - methano - 1,2 - cyclohexenylene; R3 represents hydrogen, 2-hydroxyethyl, 2 - amino - ethyl, 2- or 3-hydroxypropyl, 2- or 3-aminopropyl, 2- or 3-(2-aminoethyl) aminopropyl ...

Process for impregnating leather and leather substitutes

To improve the dynamic resistance and impermeability to water of leather, e.g. substitute leather, it is impregnated with a salt of one or more than one carboxylic acid of high molecular weight, e.g. selected from fatty acids having 10 to 20 carbon atoms per molecule, such as unsaturated or branched-chain fatty acids, and one or more than one basic imidazoline and/or pyrimidine derivatives having the general formula: in which R1 is a hydrocarbon residue having 9 to 20 carbon atoms derived from one or more than one carboxylic acid of high molecular weight, R2 is an alkylene residue having 2 or 3 carbon atoms, m is 1 to 3 and n is 2 or 3. R1 may be aliphatic, aliphatic-cycloaliphatic, aliphatic-aromatic, unsaturated or a branched chain, and may be derived from fatty acids obtained from natural fats and oils. The salt is preferably applied in the form of a 5 to 30%, by weight, solution in a specified, volatile organic solvent, as by immersion, spreading, brushing or ...

Process for preparing 2-[2-(Substituted) Vinyl] Amidines

... 1,161,185. 2 - (2 - (Substituted) vinyl)- cyclic amidines. CHAS PFIZER & CO. Inc. 7 Feb., 1968 [28 Feb., 1967; 1 Dec., 1967], No. 6156/68. Addition to 1,108,207. Heading C2C. 2 - [2 - Substituted) vinyl] - cyclic amidines having the formula are produced in a process which comprises condensing, at a temperature between 50‹ C. and 150‹ C., a compound of the formula where R 2 is and R 3 is ethyl, Cl, Br or I; R 4 is H or methyl; R 5 is F, mercapto, methylthio, Cl, Br, or I; with a compound of the formula where Y is an ethylene or trimethylene group and if desired reacting the free base thus obtained with a suitable non-toxic acid to obtain the corresponding salt product. The by-product water is removed by use of a molecular sieve, e.g. the synthetic "Linde Molecular sieves," or by reason of the water forming an azeotrope with the reaction-inert solvent, e.g. benzene or toluene, or by the condensation being conducted at a temperature of from about 100‹ C. to about 150‹ C. in the absence of ...

PRODUCTION OF 1,3-DIAZA-HETEROCYCLES

Tetrahydropyrimidine carburettor detergent

Motor gasoline additives which inhibit the formation of deposits in carburetters consist of one or more tetrahydropyrinidines of formula in which R is an aliphatic hydrocarbon radical containing 8 - 18 carbon atoms and R1 is a naphthenyl radical. The tetrahydropyridines are usually used in the form of mixtures and are added to motor gasoline in an amount of 1 -200 lbs. per thousand barrels. The gasoline may also contain small amounts of tetraethyl lead, phenylene diamine, N,N1-disalicylidene-1, 2-propamediamine, 2,6-di-tert-butyl-4-methyl phenol, cresyl diphenyl phosphate and glyceryl mono-oleate.ALSO:The invention comprises tetrahydropyrimidines of formula in which R is an aliphatic hydrocarbon radical containing from 8 to 18 carbon atoms and R1 is a naphthenyl radical. They may be prepared by reacting at elevated temperature at least one naphthenic acid with at least one aliphatic hydrocarbon substituted propylenediamine of formula RNHCH2CH2CH2NH2 ...

Improvements in and relating to fungicidal compositions

A tetrahydropyrimidine compound having the formula wherein R is an aliphatic hydrocarbon radical having from 6 to 8 carbon atoms and R1 is a methyl radical or hydrogen is prepared by reacting N-substituted aliphatic trimethylenediamines with either acetic acid or formic acid in the absence of a solvent and at a temperature in the range of from 600 to 625 degrees Fahrenheit to produce cyclization and eliminate 2 mols. of water. Examples of the aliphatic hydrocarbon radicals include n-alkyl radicals such as hexyl, heptyl, octyl, decyl, undecyl, dodecyl, tridecyl, tetradecyl, pentadecyl, hexadecyl, heptadecyl, and octadecyl; and n-alkenyl radicals such as octadecenyl, octadecadienyl, and octadecatrienyl. These n-aliphatic hydrocarbon radicals can also be employed as mixtures, as, for example, as derived from animal and vegetable oil fatty acids such as coconut oil, tallow, soybean oil and cottonseed oil. Examples of many specified compounds are 2-methyl-3-coco-3,4,5,6 ...

A method for preparing polybasic compounds.

Method of preparation of new derivatives of benzamidobenzanilide

New 2 (nitromethylene) - 1,3-diazacycloalcanes, insecticidal compositions the container and their use to fight against undesirable insects.

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

VERFAHREN ZUM HERSTELLEN VON NEUEN ALPHA-(3,4-DICHLORPHENYL)-2-IMIDAZOLIN-2-YL (ODER 1,4,5,6-TETRA HYDROPYRIMIDIN-2-YL) METHANOLDERIVATEN UND VON DEREN SALZEN

VERFAHREN ZUR HERSTELLUNG VON 2- (OMEGA-AMINOALKYL) -1,3-HETEROCYCLEN

BIOELECTRICALLY ACTIVE TEXTILE SUPPORT

SUBSTITUTED HETERO-CYCLIC CONNECTIONS AND THEIR USE TO THE TREATMENT OF THE MULTIPLE MEDICINE RESISTANCE

PROCEDURE FOR PLASTICIZING WASHED TEXTILES AND MEANS FOR DURCHFUHRUNG THE SAME

PROCEDURE FOR THE PRODUCTION OF TRIAC CLAY/TONE AMINE

BITUMINOUS MIXTURE

HETERO-CYCLIC CONNECTIONS.

MUSCARINAGONISTEN

PROCEDURE FOR PLASTICIZING WASHED TEXTILES AND MEANS FOR DURCHFUHRUNG THE SAME

BITUMINOESE MISCHUNG

Procedure for the production of new Benzamidobenzanilid derivatives

Procedure for the production of new urea derivatives

PROCEDURE FOR KRYOPROTEKTION OF CELLS

Procedure for the production of new Tetrahydropyrimidinen and their salts

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

PROCEDURE FOR THE PRODUCTION OF VALUABLE MATERIAL FROM ORGANISMS

3,4-DICHLOROPHENYL-2-IMIDAZOLINE (OR PYRMIDINE)- METHANOL DERIVATIVES

1,3-diazacycloalkyl oxime derivatives

Benzamidine derivatives

HETEROCYCLIC COMPOUNDS

SPIROHEPTANE SALICYLAMIDES AND RELATED COMPOUNDS AS INHIBITORS OF ROCK

The present invention provides compounds of Formula (I): N R' (R3)4 0 R"l o (J) 5 or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same. - 609- ...

VINYL-SUBSTITUTED TERTRAHYDROPYRIMIDINES

5-PHENYL-1,4,5,6-TETRAHYDROPYRIMIDINE DERIVATIVES

ADRENERGIC AMIDINES

ADRENERGIC COMPOUNDS Disclosed herein are adrenergic compounds represented by the formula wherein m is 0, 1 or 2; R1, R2, R3 are taken from the group consisting of hydrogen, hydroxy, loweralkyl, loweralkoxy, halo, or NHSO2R wherein R is taken from the group consisting of hydrogen, loweralkyl or arylalkyl, provided that R1, R2, R3 cannot simultaneously be hydrogen, and provided that when one of R1, R2, R3 is halo, the other two cannot simultaneously be hydrogen; R1 and R2 or R2 and R3 taken together can form a methylenedioxy or ethylenedioxy bridge; and R4 and R5 are hydrogen or taken together form a closed ring of the formula wherein n is 1 or 2, and the dashed line represents a single or double bond when n is 1, and R6 is taken from the group consisting of hydrogen, loweralkyl, or arylalkyl, and the pharmaceutically acceptable salts thereof.

HETEROCYCLIC OXIMES AS PESTICIDES

Heterocyclic oximes of the general formula: wherein n = 2, 3 or 4; X represents oxygen, sulphur, NR (wherein R represents a hydrogen atom, an alkyl, alkenyl, alkynyl, haloalkyl, aryl, alkaryl or aralkyl group) or CR2R3, wherein R2 and R3 each individually represents a hydrogen or halogen atom, or an alkyl group or wherein R2 and R3 together may form a carbocyclic ring structure which may contain one or more hetero atoms in the ring Y represents a hydrogen atom or an alkyl, haloalkyl, cyanoalkyl, acyl or optionally substituted carbamoyl group , wherein R4 and R5 each individually represents hydrogen or alkyl) and R1 represents 8 hydrogen atom or a (cyclo)alkyl, haloalkyl, alkoxy, aryloxy or an aryl group optionally substituted by one or more halogen atoms, nitro groups or an alkyl or alkoxy group or fused with a heterocyclic or carbocyclic ring, or a heterocyclic group or an optionally substituted amino group and which include, when Y represents a hydrogen atom, the tautomeric form represented ...

SUBSTITUTED BIS-BENZIMIDAZOLYL COMPOUNDS; PREPARATION AND USE THEREOF

... of the disclosure: The present invention describes novel substituted bisbenzimidazolyl compounds and a process for preparing same. These novel compounds can be used as cbemotherapeutics; they are suitable for combating parasitosis, especially protozoal and virus diseases on human beings and animals.

PROCESS FOR THE PREPARATION OF 1-SUBSTITUTED 2-METHYL-TETRAHYDROPYRIMIDINES

PROCESS FOR THE PREPARATION OF 1-SUBSTITUTED 2-METHYL-TETRAHYDRO-PYRIMIDINES 1-substituted 2-methyl-tetrahydropyrimidines are prepared by reacting an N-substituted propylene diamine with an acetoacetic acid ester or amide at a temperature of from 0 to 80.degree.C and removing the water produced in the reaction at a temperature of from 0 to 80.degree.C.

CYCLIC AMIDINE COMPOUNDS

There is provided cyclic amidine compounds of the following formula (I) wherein: A1 and A2 are hydrogen atom, optionally substituted alkyl group; optionally substituted aryl group; or optionally substituted heterocyclic group; and X is -C(R1,R2)-C(R3,R4)-, -C(R5)=C(R6)-, -C(R7,R8)-C(R9,R10)- C(R11,R12)-, or -C(R13,R14)-C(R15,R16)-NH- (wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11R12, R13, R14, R15 and R16 are hydrogen atom; halogen atom; optionally substituted alkyl group; optionally substituted aryl group; or optionally substituted heterocyclic group;or pharmaceutically acceptable salts thereof. These compounds have good affinity for .alpha.4.beta.2 nicotinic acetylcholine receptors and activate the same to thereby exert a preventive or therapeutic effect on cerebral dysfunction.

MELANOCORTIN-4 RECEPTOR BINDING COMPOUNDS AND METHODS OF USE THEREOF

MC4-R binding compounds of the formula (I): B-Z-E wherein B is an anchor moiety, Z is a central moiety, and E is an MC4-R interacting moiety are discussed. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also discussed.

CYCLIC AMIDINE BASED CORROSION INHIBITORS WHICH INHIBIT CORROSION CAUSED BY CO.SUB.2 AND H.SUB.2S

SUBSTITUTED BIS-BENZIMIDAZOLYL COMPOUNDS; PREPARATION AND USE THEREOF

PROCESS FOR THE SEPARATION OF PYRIMIDINE DERIVATIVES FROM AQUEOUS SOLUTIONS

The invention relates to a process for the separation and purification of pyrimidine derivatives, particularly tetrahydropyrimidines, in particular 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinecarboxylic acids (ectoine) from aqueous solutions by a combination of adsorption using inorganic solids (zeolites) and crossflow filtration.

NOVEL N-(ARYLSULPHONYL)AMINO ACID DERIVATIVES, THEIR PREPARATION PROCESS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

L'invention concerne des composés de formule (I) dans laquelle R1 à R9, R16 et R17 sont tels que définis à la revendication (1). Ces composés sont pharmacologiquement actifs.

Verfahren zur Bekämpfung von schädlichen pflanzlichen Kleinlebewesen.

Verfahren zur Bekämpfung von Pilzen

Verfahren zur Herstellung neuer Harnstoff- und Thioharnstoffderivate

Verfahren zur Herstellung neuer Harnstoffderivate

Derivs of tetrahydrpyrimidines,imidazolin and tetrahydro - -1,3-diazepin - with diuretic anti-inflammatory,cardiovascular,hypogl

Cpds. of formula (where n = 0, 1 or 2; R3 and R4 are same or different H or lower alkyl; or R3 = H and R4 = hydroxy; Ph = phenyl opt. mono- or poly-substd. with hydroxyl, lower alkyl lower alkoxy, halo-lower alkyl, halogen, amino or mono- di(lower)alkylamino; R = hydroxyl, acyloxy, alkoxy or halogen; R1 = opt. substd. phenyl or naphthyl; or R + R1 form together an oxo-group; R6 = H, lower alkyl lower alkenyl or acyl. Acid-addition salts of (I) are included. Prepd. by reacting a cpd. (II) with an organometal cpd. which can convert the ketone function to where R8 = as signified for R1; the reaction is then opt. followed by one or more acylation, displacement, substitution or addition reactions. PRef. organometal cpds. are Grignard reagents R8MgY where Y = halogen, or alkali metal cpds. such as R8Li. Reaction in inert solvent such as ethers.

Verfahren zur Herstellung von Derivaten von Guanidin

Herbizide Zubereitung

2-2-arylvinyl-1 4 5 6-tetrahydropyrimidines and 2-2-arylvinyl-2-imidaz - olines

Compounds and acid addition salts thereof (I) where Y is R2 is H; CH3; C2H5; Cl; Br; or F R3 is H or CH3 R4 is H or lower alkyl R5 is Cl, Br, iodo, F or OH R1 is H or CH3 n is 2 or 3 No compound is specifically claimed The compounds (I) are useful as intermediates in the synthesis of compounds of formula (II), which have anthelmintic activity.

Verfahren zur Herstellung von Isothiouronium-Verbindungen

Tetrahydropyrimidine and imidazoline derivs

Cpds. (I) and their acid addn. salts. R1 = H, alkyl, Ph opt. substd. by mono/di-halo/alkyl/alkoxy, amino, CF3; phenalkyl thienyl, pyridyl, furyl, naphthyl and tetrahydro-2-naphthyl R2 = R3 = H, halogen, alkyl, alkoxy, or R2 = H and R3 = halogen, NH2, alkyl-NH, alkyl, alkoxy; n = 2,3 (all alkyl radicals have is not > 6C) As antidepressants; also (n = 3) diuretics and (n = 2) anorexiants.

Tetrahydropyrimidine and imidazoline derivs

Cpds. (I) and their acid addn. salts. R1 = H, alkyl, Ph opt. substd. by mono/di-halo/alkyl/alkoxy, amino, CF3; phenalkyl thienyl, pyridyl, furyl, naphthyl and tetrahydro-2-naphthyl R2 = R3 = H, halogen, alkyl, alkoxy, or R2 = H and R3 = halogen, NH2, alkyl-NH, alkyl, alkoxy; n = 2,3 (all alkyl radicals have is not > 6C) As antidepressants; also (n = 3) diuretics and (n = 2) anorexiants.

Guanidines and isothioureas adjuvants for diptheria and

... (A) Cpds. contng. a cation (CH3(CH2)m-A-(CH2)n-XC(NHR2)NHR')+ (I) and corresp. free bases. Where R' = (1-4C) alkyl R2 = (1-4C) alkyl or 2-phenoxyethyl X = NH or S A = O or methylene n = 2-3 m = 11-15. (B) Antigenic vaccines contg. (I) particularly tetanus toxoid. Adjuvants for diphtheria and tetanus vaccines to improve their antigenic properties. Salts of N-2-dodecyloxyethyl-(II), N-3-dodecyloxypropyl-, N-2-hexadecyloxyethyl-, N'N"-dimethylguanidinium cation and of N-hexadecyl-N'-methyl-N"-2-phenoxyethylguanidium cation. Salts of S.hexadecyl and S.octadecyl-N, N'-dimethylthiuronium and their use in prepn. of (I).

Verfahren zur Herstellung von Benzamidobenzanilid-Derivaten

Verfahren zur Herstellung von Benzamidobenzanilid-Derivaten

Verfahren zur Herstellung neuer mehrbasischer Verbindungen

Tetrahydropyrimidine and imidazoline derivs

Cpds. (I) and their acid addn. salts. R1 = H, alkyl, Ph opt. substd. by mono/di-halo/alkyl/alkoxy, amino, CF3; phenalkyl thienyl, pyridyl, furyl, naphthyl and tetrahydro-2-naphthyl R2 = R3 = H, halogen, alkyl, alkoxy, or R2 = H and R3 = halogen, NH2, alkyl-NH, alkyl, alkoxy; n = 2,3 (all alkyl radicals have is not > 6C) As antidepressants; also (n = 3) diuretics and (n = 2) anorexiants.

Tetrahydropyrimidine and imidazoline derivs

Cpds. (I) and their acid addn. salts. R1 = H, alkyl, Ph opt. substd. by mono/di-halo/alkyl/alkoxy, amino, CF3; phenalkyl thienyl, pyridyl, furyl, naphthyl and tetrahydro-2-naphthyl R2 = R3 = H, halogen, alkyl, alkoxy, or R2 = H and R3 = halogen, NH2, alkyl-NH, alkyl, alkoxy; n = 2,3 (all alkyl radicals have is not > 6C) As antidepressants; also (n = 3) diuretics and (n = 2) anorexiants.

Bis-anilides with basic substituents - having chemotherapeutic activity

Verfahren zum Imprägnieren von Leder und Lederaustauschstoffen

Verfahren zur Herstellung mehrbasischer Verbindungen

Verfahren zur Herstellung von in 2-Stellung der Vinylgruppe substituierten cyclischen 2-Vinylamidinen

Improved process for 1,4,5,6-tetrahydro-2-substd- - vinyl-(pyrimidines and 2-imidazolines) anthelmintics

Method for the preparation of 1, 4, 5, 6-tetrahydro-2-((2-substituted) vinyl)-pyrimidines and imidazolines of the general formula (I). where R2 = and R3 = hydrogen, methyl, ethyl, chloro, bromine, or iodine. and R4 = hydrogen or methyl, and R5 = hydrogen, chlorine, bromine, iodine, fluorine, methyl, ethyl, mercapto, methylthio, ethoxy, propoxy, or butoxy R1 = hydrogen or methyl, Y = ethylene or trimethylene and the acid addition salts of (I). The compounds have anti-parasitic activity.

Verfahren zur Herstellung von Amidinen

Cyclic bis-amidine cpds - esp useful as tuberculostats

Title cpds. of formula (I) (where R' is di- or triemthylene in which the individual H- atoms may be replaced by alkyl gps. which together contain is not >6 C-atoms, and A is -CO- or CO-B-CO- in which B is R2 substd. phenylene, R2 substd. phenyleneamino, R2 substd. phenylenediamino or styrylene, R2 being H, halogen, amino, NO2, OH, alkyl, alkoxy, alkylthio, acylamino or aminocarbonyl), which are esp. of use as tuberculostats, for the therapy of trypanosoma infections, and for combatting cancer (esp. leukaemia), are prepd. by reacting corresponding cpds. in which the terminal heterocyclic gps. are replaced by-CS-NH2 gps. with diamines of formula H2N-R1-NH2 and isolating the product in the form of the free base or of an acid addition salt.

Cyclic bis-amidine cpds - esp useful as tuberculostats

Title cpds. of formula (I) (where R1 is di- or trimethylene in which the individual H-atoms may be replaced by alkyl gps. which together contain is not >6 C-atoms, R2 is H or is not >6C alkyl, n is 0 or 1, and A is CO or-CO-B-CO in which B is R4 substd. phenylene, R4 substd. phenylene amino, R4 substd. phenylene-diamino or styrylene, R4 being H, halogen, amino, NO2, OH, alkyl, alkoxy, alkylthio, acylamino or aminocarbonyl), which are esp. useful as tuberculostats, for the therapy of trypanosoma infections, and for combating cancer, are prepd. by reacting corresponding cpds. in which the terminal heterocyclic gps. are replaced by gps. of formula -C(=NR2)-O-Alkyl with diamines of formula H2-N-R1-NH2, the products being isolated in the form of the free base or of an acid addition salt.

Cyclic bis-amidine cpds - esp useful as tuberculostats

Cpds. are as in CH 525896, having the same chemotherapeutic activity, and are prepared by reacting corresponding cpds, in which the terminal heterocyclic gps. are replaced by alkoxycarbonyl gps. with diamines of formula H2N-R1-NH2, the product being isolated in the form of the free base or of an acid addition salt.

[...] DE [...] DE [...] PHENYL- [...][...].

Pesticide containing 2-(nitromethylene)-1,3-diazacycloalkanes

Blood brain barrier-penetrating oximes for cholistenerases reactivation

The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.

ANTIBACTERIAL COMPOUNDS TARGETING ISOPRENOID BIOSYNTHESIS

With the rise in resistance to antibiotics such as methicillin, there is a need for new drugs. The invention provides small molecules that inhibit cellular drug targets such as UPPS and FPPS by interacting with binding pockets, thereby preventing enzyme function. Compounds described herein are also active against (MIC90˜0.25 μg/mL), can potently synergize with methicillin (fractional inhibitory concentration index=0.25), and are protective in a mouse infection model. The invention therefore provides numerous compounds for anti-bacterial treatments and for restoring sensitivity to drugs such as methicillin, using combination therapies. 2. The method of wherein the bisphenylamidine or bisphenylalkyne compound additionally binds to site 1 claim 1 , site 2 claim 1 , or site 3 claim 1 , or a combination thereof claim 1 , of UPPS.3. The method of wherein the bisphenylamidine or bisphenylalkyne compound does not bind to site 1 of UPPS.4. The method of wherein the bisphenylamidine or bisphenylalkyne compound inhibits UPPS with an ICvalue of less than about 1 μM.5. The method of wherein the bisphenylamidine or bisphenylalkyne compound inhibits UPPS with an ICvalue of less than about 150 nM.6. The method of wherein the linker is an optionally substituted phenyl claim 1 , biphenyl claim 1 , naphthyl claim 1 , fluorene claim 1 , carbazole claim 1 , diphenyl ether claim 1 , 1 claim 1 ,3-diphenylurea claim 1 , vinylbenzene claim 1 , divinylbenzene claim 1 , or phenylethyl.16. A pharmaceutical composition comprising a compound of in combination with a pharmaceutically acceptable carrier or excipient.19. A pharmaceutical composition comprising a compound of in combination with a pharmaceutically acceptable carrier or excipient.20. (canceled) This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application No. 61/733,141, filed Dec. 4, 2012, which is incorporated herein by reference.This invention was made with government support under Contract Nos. ...

Substituted 1,1'-biphenyl compounds, analogues thereof, and methods using same

The present invention includes substituted 3,3′bis(phenoxymethyl)-1,1′-biphenyl compounds, analogues thereof, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient.

CONTRAST AGENTS FOR MAGNETIC RESONANCE IMAGING

The present invention provides contrast agents of the formula [N(A,A,A) M](counter ion(s)) for use in a diagnostic method practiced on the human or animal body. It also refers to the contrast agents, as well as pharmaceutical compositions containing same. Further, it relates to a method of in vitro medical imaging, especially of diagnostic imaging, comprising administering said compound to a sample. 118.-. (canceled)19. A method of diagnostic imaging which comprises administering a patient a contrast agent according .20. The method according to claim 19 , wherein the contrast agent is a magnetic resonance imaging contrast agent.21. The method according to claim 19 , wherein the transition metal is Fe claim 19 , Co claim 19 , Ni claim 19 , and Cu.22. The method according to claim 19 , wherein the contrast agent is water-soluble.23. The method according to claim 19 , wherein A claim 19 , A claim 19 , and Aare the same.24. The method according to claim 19 , wherein the diagnostic method is medical imaging.26. The method according to claim 19 , wherein the counter ion(s) is/are selected from the group consisting of acetate (OAc) claim 19 , chloride (Cl) claim 19 , iodide (I) claim 19 , bromide (Br) claim 19 , nitrate (NO) claim 19 , triflate (OTf) and sulfate (SO).27. The method according to claim 19 , wherein{'sub': 1', '4', '5', '6', '3', '2, 'R, R, R, and Rare independently selected from the group consisting of: H, F, Cl, Br, I methyl, OMe, OH, and CF, wherein Ris H, or OH; and'}{'sub': 3', '3, 'R═H or CH.'}28. The method according to claim 19 , wherein{'sub': 1', '2', '3', '4', '5', '6, 'R, R, R, R, R, and Rare independently selected from the group consisting of{'sub': 3', '1-4', '1-4', '3-7', '3-7', '4-12', '2', '4-12, 'H, OH, SH, CF, CN, halogen, optionally substituted Calkyl, Cheteroalkyl, Ccycloalkyl, Cheterocycloalkyl, Caryl C(O)NHor C(O)OH and Cheteroaryl groups.'}{'sub': 6', '1-4, 'wherein Ris H, OH, or an Calkyl; and'}{'sup': '2', 'sub': 2', '1', '3', '4', ' ...

SPIROHEPTANE SALICYLAMIDES AND RELATED COMPOUNDS AS INHIBITORS OF ROCK

The present invention provides compounds of Formula (I): 1. A compound selected from the group consisting of:N-[6-(2-carbamoylphenoxy)spiro[3.3]heptan-2-yl]-5-methyl-1-phenyl-1H-pyrazole-4-carboxamide,N-[6-(2-carbamoylphenoxy)spiro[3.3]heptan-2-yl]-1-methyl-1H-indazole-3-carboxamide,N-[6-(2-carbamoylphenoxy)spiro[3.3]heptan-2-yl]-6-(2-hydroxy-2-methylpropoxy)pyrazolo[1,5-a]pyridine-3-carboxamide,N-[6-(2-carbamoylphenoxy)spiro[3.3]heptan-2-yl]-6-(oxolan-3-yloxy)pyrazolo[1,5-a]pyridine-3-carboxamide,N-[6-(2-carbamoylphenoxy)spiro[3.3]heptan-2-yl]-3-methoxy-4-(1H-pyrazol-4-yl)benzamide,2-({6-[6-(2-hydroxy-2-methylpropoxy)pyrazolo[1,5-a]pyridine-3-amido]spiro[3.3]heptan-2-yl}oxy)pyridine-3-carboxamide,3-({6-[6-(2-hydroxy-2-methylpropoxy)pyrazolo[1,5-a]pyridine-3-amido]spiro[3.3]heptan-2-yl}oxy)pyrazine-2-carboxamide,4-({6-[6-(2-hydroxy-2-methylpropoxy)pyrazolo[1,5-a]pyridine-3-amido]spiro[3.3]heptan-2-yl}oxy)pyrimidine-5-carboxamide,2-[(6-{6-[(1,3-difluoropropan-2-yl)oxy]pyrazolo[1,5-a]pyridine-3-amido}spiro[3.3]heptan-2-yl)oxy]pyridine-3-carboxamide,2-({6-[6-(3,3,3-trifluoropropoxy)pyrazolo[1,5-a]pyridine-3-amido]spiro[3.3]heptan-2-yl}oxy)pyridine-3-carboxamide,2-({6-[6-(oxan-4-yloxy)pyrazolo[1,5-a]pyridine-3-amido]spiro[3.3]heptan-2-yl}oxy)pyridine-3-carboxamide,N-{6-[(3-carbamoylpyridin-2-yl)oxy]spiro[3.3]heptan-2-yl}-2,3-dihydro-1H-indole-1-carboxamide,N-{6-[(3-carbamoylpyridin-2-yl)oxy]spiro[3.3]heptan-2-yl}-5-cyano-2,3-dihydro-1H-isoindole-2-carboxamide,Benzyl N-[6-(2-carbamoylphenoxy)spiro[3.3]heptan-2-yl]carbamate,N-[(aR)-6-(2-carbamoylphenoxy)spiro[3.3]heptan-2-yl]-7-cyclopropyl-6-(2-hydroxy-2-methylpropoxy)pyrazolo[1,5-a]pyridine-3-carboxamide,N-[(aR)-6-(2-carbamoylphenoxy)spiro[3.3]heptan-2-yl]-6-(2-hydroxy-2-methylpropoxy)pyrazolo[1,5-a]pyridine-3-carboxamide,N-{6-[(3-carbamoylpyridin-2-yl)oxy]spiro[3.3]heptan-2-yl}-5-methoxy-2,3-dihydro-1H-indole-1-carboxamide,N-[(aR)-6-(2-carbamoylphenoxy)spiro[3.3]heptan-2-yl]-7-(3,3,3-trifluoropropoxy)imidazo[1,2-a] ...

GUANICIDE COMPOUND AND FUNGICIDE

A novel guanidine compound having excellent fungicidal activity is represented by formula [I]. (In the formula, Y represents a divalent group represented by formula [II] (wherein each of R-Rindependently represents a hydrogen atom or the like) or the like; each of X and Z independently represents an unsubstituted or substituted alkylene group or the like; each of Qand Qindependently represents a single bond or the like; each of Aand Aindependently represents an unsubstituted or substituted divalent heterocyclic compound residue or the like; and each of R-Rindependently represents a hydrogen atom or the like.) 3. A fungicide comprising at least one selected from a compound and a salt as defined in as an active ingredient thereof.4. A plant disease-controlling agent comprising at least one selected from a compound and a salt as defined in as an active ingredient thereof. The present invention relates to a guanidine compound and a fungicide. More particularly, the present invention relates to a novel guanidine compound which has excellent fungicidal activity, is safe to use, and can be industrially advantageously synthesized, as well as a fungicide or a plant disease-controlling agent containing the guanidine compound as an active ingredient thereof.The present invention claims priority on the basis of Japanese Patent Application No. 2015-113376 filed in Japan on Jun. 3, 2015, the contents of which are incorporated herein by reference.Patent Document 1, 2, 3, and 4 disclose that some arylamidine compounds have controlling effects against fungi or plant disease pathogens. In addition, fungicides or plant disease-controlling agents containing the arylamidine compounds as active ingredients thereof have been proposed.The present invention aims to provide a novel guanidine compound which has excellent fungicidal activity, is safe to use, and can be industrially advantageously synthesized, as well as a fungicide or a plant disease-controlling agent containing the guanidine ...

MALIGNANT AND NON-MALIGNANT DISEASE TREATMENT WITH RAS ANTAGONISTS

The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition. The present disclosure also describes a method for inhibiting such Ras-induced or mediated cellular processes. The method entails administering a Ras antagonist in an amount effective to inhibit such cellular processes. 1. A Ras antagonist represented by the Formula (I):{'br': None, 'sup': 1', '2', '3', '4, 'R-R-R-R\u2003\u2003(I)'} [{'sup': '3', 'sub': '2', 'Rrepresents S, O, N, SO, SO, or Se; and'}, {'sup': '4', 'Rrepresents farnesyl or geranyl-geranyl; and'}], 'wherein [{'sup': '2', 'Rrepresents a 5-membered heterocyclic ring with at least one heteroatom; and'}, {'sup': '1', 'Rrepresents a 5- or 6-membered heterocyclic ring with at least one heteroatom.'}], 'wherein at least one of2. The Ras antagonist of claim 1 , wherein the heteroatoms of Ror Rare selected from the group consisting of O claim 1 , N claim 1 , S claim 1 , SO claim 1 , and SO.3. The Ras antagonist of claim 1 , wherein claim 1 , when Rrepresents a 5-membered heterocyclic ring with one or two heteroatoms claim 1 , Rrepresents CN claim 1 , C(═O)R claim 1 , S(═O)(═O)R claim 1 , COM claim 1 , SOM claim 1 , or an N(R)-substituted tetrazole: [{'sup': 5', '6', '7, 'Rrepresents hydrogen, hydroxyl, C1-C4 alkyloxy, C2-C4 alkenyloxy, C1-C4 hydroxyalkyloxy, C1-C4 aminoalkyloxy, or NRR;'}, {'sup': 6', '7', '6', '7, 'Rrepresents hydrogen, hydroxyl, C1-C4 alkyl, C2-C4 alkenyl, C1-C4 aminoalkyl, C1-C4 hydroxyalkyl, C1-C4 alkyloxy, or C1-C4 alkylamino, and Rrepresents hydrogen, C1-C4 alkyl, C2-C4 alkenyl, C1-C4 aminoalkyl, C1-C4 hydroxyalkyl, C1-C4 alkyloxy, or C1-C4 alkylamino, or wherein Rand Rtogether form a ring comprising morpholine, ...

AMIDINE CATALYST FOR CURABLE COMPOSITIONS

The present invention relates to an amidine of the formula (I) and its use as a catalyst for crosslinking a curable composition. The amidine of the formula (I) contains at least one aliphatic amidine group. It is substantially odorless and nonvolatile at room temperature and accelerates the crosslinking of curable compositions very efficiently, without impairing the storage stability of the compositions. It is particularly suitable for compositions based on polymers containing silane groups, with which it is compatible, as a result of which such compositions do not have a tendency to separation or migration or evaporation of the catalyst. 1. An amidine of the formula (I){'br': None, 'sub': r', 'p, '[Q\ue8a0L\ue8a0Q′-Z]\u2003\u2003(I)'}Where p is an integer from 1 to 6 and r is an integer from 0 to 5, where (p+r) is an integer from 1 to 6, 'or, in the case that r=0 and p=1, may also be a hydrogen radical,', 'L is a (p+r)-valent hydrocarbyl radical having an average molecular weight in the range from 15 to 20 000 g/mol, optionally having heteroatoms,'}Q is a reactive group selected from glycidoxy, N-aziridinyl, (meth)acrylate, (meth)acrylamide, (meth)acrylonitrile, maleate, maleamide, maleimide, fumarate, fumaramide, itaconate, itaconamide, crotonate and crotonamide,Q′ is a divalent connecting unit formed from the reaction of a reactive Q group with HZ, and Z is an aliphatic amidine group bonded via a nitrogen atom,where every Z is separated from every other Z by at least 2 carbon atoms,and where, in the case that r=0 and p=1 and of (meth)acrylamide or maleamide or fumaramide or itaconamide or crotonamide as reactive Q group, L and Q′ may also together be a monovalent hydrocarbyl radical having 5 to 20 carbon atoms and having heteroatoms in the form of amide groups and optionally ether or ester groups.3. An amidine as claimed in wherein Rand Rtogether are R.4. An amidine as claimed in claim 1 , wherein p is 1 or 2 or 3 and r is 0.6. A process for preparing the amidine ...

COMPOSITION CONTAINING ECTOINE OR HYDROXYECTOINE AS AN ACTIVE SUBSTANCE FOR PROMOTING THE REGENERATION OF INJURED BODY TISSUE

The invention relates to a composition containing as active agent ectoine, hydroxyectoine, glucosylglycerol and/or salts, esters or amides of these compounds for promoting the regeneration of injured body tissue. The invention has special significance for the treatment of chronic wounds or ulcers. 1. A method of promoting tissue regeneration of injured body tissue in a patient in need thereof wherein the injured body tissue is an ulcer or a chronic ulcer , comprising administering to the patient an effective amount of a composition comprising as active agent glucosylglycerol and/or esters this compound for use in said regeneration of injured body tissue , wherein the injury to the body tissue is a wound , diabetic foot syndrome or an ulcer , wherein the ulcer is ulcus cruris , decubitus , malum perforans , durum ulcer , mole ulcer , rodent's ulcer or corneal ulcer.2. The method according to claim 1 , characterized in that the injury of the body tissue is of traumatic nature.3. The method according to claim 1 , characterized in that the injury of the body tissue is an anal fissure or hemorrhoids injury.4. The method according to claim 1 , characterized in that the glucosylglycerol is 2-O -α-glucosylglycerol or 2-O-β-glucosylglycerol.5. The method according to claim 4 , characterized in that the glucosylglycerol is 2-O-α-D-glucosylglycerol.6. The method of claim 1 , characterized in that the injury of the body tissue is mucositis.7. The method of claim 6 , wherein the mucositis is due to an adverse effect of chemotherapy or radiotherapy.8. The method of claim 6 , wherein the patient is immunocompromised.9. The method of claim 1 , characterized in that the body tissue is skin or mucous membrane.10. The method of claim 1 , characterized in that the injury of the body tissue is a thermal wound due to burns claim 1 , scalds or frostbite claim 1 , a burn claim 1 , chemical burn or a wound due to ionizing radiation.11. The method of claim 1 , characterized in that the ...

MALIGNANT AND NON-MALIGNANT DISEASE TREATMENT WITH RAS ANTAGONISTS

The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition. The present disclosure also describes a method for inhibiting such Ras-induced or mediated cellular processes. The method entails administering a Ras antagonist in an amount effective to inhibit such cellular processes. 9. The compound of claim 1 , wherein Rrepresents imidazoline claim 1 , imidazole claim 1 , pyrazole claim 1 , pyrrole claim 1 , oxazole claim 1 , thiazole claim 1 , 1 claim 1 ,4 claim 1 ,5 claim 1 ,6-tetrahydropyrimidine claim 1 , triazole claim 1 , or N(R)-substituted tetrazole; and [{'sup': '9', 'Rrepresents hydrogen or C1-C4 alkyl;'}, 'the optionally substituted phenyl ring is substituted with Cl, Br, F, I, C1-C4 alkyl, or C1-C4 alkoxy, amino, mono- or di-substituted amino; and', 'the nitrogen substitutent on the phenyl ring is C1-C4 alkyl., 'wherein10. A method of inhibiting Ras-induced proliferation of cells associated with neurofibromatosis type 1 (NF-1) claim 1 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering to a patient the compound of in an amount effective to inhibit Ras-induced proliferation of cells associated with NF-1.'}11. The method of claim 10 , wherein the cells are associated with a neurofibroma.12. The method of claim 10 , wherein the cells are associated with a malignant peripheral nerve sheath tumor (MPNST).14. A method of inhibiting Ras-induced proliferation of cells associated with cancer claim 10 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering to a patient having malignant tumor cells that express activated Ras proteins the compound of in an amount effective to inhibit Ras- ...

Gem-disubstituted pyrrolidines, piperazines, and diazepanes, and compositions and methods of making the same

Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).

AMIDINE CATALYST FOR CURABLE COMPOSITIONS

The present invention relates to an amidine of the formula (I) and its use as a catalyst for crosslinking a curable composition. The amidine of the formula (I) contains at least one aliphatic amidine group. It is substantially odorless and nonvolatile at room temperature and accelerates the crosslinking of curable compositions very efficiently, without impairing the storage stability of the compositions. It is particularly suitable for compositions based on polymers containing silane groups, with which it is compatible, as a result of which such compositions do not have a tendency to separation or migration or evaporation of the catalyst. 4. An amidine as claimed in claim 1 , wherein L is triethoxysilylpropyl or trimethoxysilylpropyl.6. An amidine as claimed in wherein Rand Rtogether are R.7. A process for preparing the amidine of the formula (I) as claimed in claim 1 , wherein at least one amidine of the formula HZ is reacted with at least one functional compound of the formula LQ]wherein p is 1 and r is 0,L is a monovalent hydrocarbyl radical having 1 to 6 carbon atoms and containing an alkoxysilane group, andQ is a glycidoxy group.9. A method comprising applying as catalyst for the crosslinking of a curable composition the amidine of the formula (I) as claimed in .10. A method as claimed in claim 9 , wherein the curable composition is an epoxy resin composition or a polyurethane composition or an epoxy resin/polyurethane composition or a cyanate ester resin composition or a composition containing silane groups.11. A method as claimed claim 10 , wherein the curable composition is a composition based on polymers containing silane groups selected from the group consisting of polyorganosiloxanes having terminal silane groups and organic polymers containing silane groups.12. A curable composition comprising at least one amidine of the formula (I) as claimed in .13. The composition as claimed in claim 12 , wherein it further comprises at least one polymer containing ...

Amidines and amidine analogs for the treatment of bacterial infections and potentiation antibiotics

Compounds and methods for the treatment of a bacterial infection or the potentiation of an antibiotic in treating a bacterial infection are described herein.

COMPOSITION CONTAINING ECOTINE OR HYDROXYECOTINE AS AN ACTIVE SUBSTANCES FOR PROMOTING THE REGENERATION OF INJURED BODY TISSUE

The invention relates to a composition containing as active agent ectoine, hydroxyectoine, glucosylglycerol and/or salts, esters or amides of these compounds for promoting the regeneration of injured body tissue. The invention has special significance for the treatment of chronic wounds or ulcers. 1. Composition containing as active agent ectoine , hydroxyectoine , glucosylglycerol and/or salts , esters or amides of these compounds for promoting the regeneration of injured body tissue.2. Composition according to claim 1 , characterized in that the body tissue is skin or mucous membrane.3. Composition according to claim 1 , characterized in that the injury of the body tissue is of traumatic nature.4. Composition according to claim 1 , characterized in that the injury of the body tissue is an ulcer.5. Composition according to claim 1 , characterized in that the injury is a chronic injury claim 1 , in particular a chronic wound or a chronic ulcer.6. Composition according to claim 5 , characterized in that the injury of the body tissue is due to the diabetic foot syndrome.7. Composition according to claim 1 , characterized in that the injury of the body tissue is due to a decubitus ulcer.8. Composition according to claim 1 , characterized in that the injury of the body tissue is an anal fissure or hemorrhoids injury.9. Composition according to claim 1 , characterized in that the glucosylglycerol is 2-O-α-glucosylglycerol or 2-O-β-glucosylglycerol.10. Composition according to claim 9 , characterized in that the glucosylglycerol is 2-O-α-D-glucosylglycerol.11arnica montanaarnicacapsicumhypericum perforatumcardiospermum halicacabumhamamelis virginianacalendula officinalismelilotus officinalisechium vulgareangelica sinensismatricaria recutitaallium cepaachillea millefoliumglycyrrhizaechinacea purpurea. Composition according to claim 1 , characterized in that the composition contains a substance or a plurality of further substances to be selected from: dexpanthenol or ...

USE OF PENTA-SUBSTITUTED TETRAHYDROPYRIMIDINES IN PREPARATION OF THERMO-SENSITIVE FLUORESCENT MATERIALS

The present invention provides use of penta-substituted tetrahydropyrimidines in preparation of thermo-sensitive fluorescent materials. Said penta-substituted tetrahydropyrimidine compounds have linear temperature dependence of red-edge excitation wavelength (LTDREEW). When different excitation wavelengths are chosen, such compounds present fluorescence color and/or fluorescence intensity on-off switching in different temperature ranges. Also their fluorescence intensity ratios or fluorescence intensities exhibit good linear relation or power function relation to temperature, which can be used as the thermo-sensitive fluorescent materials with high sensitivity and wide temperature range (0-450 K). 2. The use of claim 1 , wherein the use of said penta-substituted tetrahydropyrimidine is in preparation of chemical and/or biological temperature fluorescent sensors or probes.3. The use of claim 1 , wherein Ris Calkyls.4. The use of claim 1 , wherein Ris selected from a group consisting of Clinear or branched alkyls claim 1 , substituted Calkyls claim 1 , Ccycloalkyls claim 1 , Caryls and substituted Caryls.5. The use of claim 1 , wherein Ris Caryls or substituted Caryls.6. The use of claim 1 , wherein Ris selected from a group consisting of Clinear or branched alkyls claim 1 , substituted Calkyls claim 1 , Ccycloalkyls claim 1 , Caryls and substituted Caryls.7. The use of claim 1 , wherein substituents are selected from a group consisting of halogens claim 1 , Cperhalogenated alkyls claim 1 , Chalogenated alkyls claim 1 , hydroxyl claim 1 , Clinear or branched alkoxys claim 1 , nitryl claim 1 , cyano claim 1 , amino claim 1 , Cmonoalkyl aminos claim 1 , Cdialkyl aminos claim 1 , Cmonocycloalkyl aminos claim 1 , Cmonoheterocycloalkyl aminos claim 1 , Cmonoaryl aminos claim 1 , Calkyl acylaminos claim 1 , Caryl acylaminos claim 1 , amino carbonyls claim 1 , Cmonoalkyl amino carbonyls claim 1 , Cdialkyl amino carbonyls claim 1 , Calkyl acyls claim 1 , Caryl acyls claim 1 , ...

NOVEL COMPOUND AND EPOXY RESIN COMPOSITION CONTAINING SAME

An epoxy resin composition excellent in storage stability and curability is provided. Particularly, a compound of general formula (I) and an epoxy resin composition containing the compound as a curing agent are provided. 5. The epoxy resin composition of claim 3 , being a one-pack type thermosetting epoxy resin composition.6. The epoxy resin composition of claim 4 , being a one-pack type thermosetting epoxy resin composition. This invention relates to a novel compound and an epoxy resin composition containing the same. More particular, it relates to a specific dicyanamide or thiocyanate salt and a one-pack type thermosetting epoxy resin composition containing the salt and having excellent storage stability and curability.Epoxy resins exhibit high adhesion to various substrates. Cured products of epoxy resins have relatively excellent properties, such as heat resistance, chemical resistance, electric characteristics, and mechanical characteristics, and, are useful in a wide range of applications, including coatings, adhesives, and molding materials.Conventional epoxy resin compositions are mostly of two-pack type in which an epoxy resin component is mixed with a curing agent or a curing accelerator on use. A two-pack type epoxy resin composition is characterized by curability at ambient or low temperature. Nevertheless, a two-pack epoxy resin composition is disadvantageous in that the two packs must be metered and mixed immediately before use and that the pot life of the composition is short and therefore has a limited use, for example, meeting difficulty in applying to automatic machinery. To eliminate these disadvantages, a one-pack type epoxy resin composition has been demanded.In order to develop a one-pack type curing resin composition, a curing agent that does not react at room temperature but commences reaction to cure upon heating, i.e., a latent curing agent is necessary. Latent curing agents so far proposed include dicyandiamide, dibasic acid hydrazides, ...

INHIBITORS OF CREATINE TRANSPORT AND USES THEREOF

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer. 3. The method of claim 2 , wherein said method comprises the suppression of metastatic colonization of said migrating cancer in the liver.4. The method of claim 2 , wherein said migrating cancer is metastatic cancer.5. The method of claim 4 , wherein the metastatic cancer comprises cells exhibiting migration and/or invasion of migrating cells.6. The method of claim 4 , wherein said metastatic cancer comprises cells exhibiting endothelial recruitment and/or angiogenesis.7. The method of claim 2 , wherein said migrating cancer spreads via seeding the surface of the peritoneal claim 2 , pleural claim 2 , pericardial claim 2 , or subarachnoid spaces.8. The method of claim 2 , wherein said migrating cancer spreads via the lymphatic system.9. The method of claim 2 , wherein said migrating cancer spreads hematogenously.10. The method of claim 2 , wherein said migrating cancer is a cell migration cancer.11. The method of claim 10 , wherein said cell migration cancer is a non-metastatic cell migration cancer.12. The method of claim 11 , where said cell migration cancer is ovarian cancer claim 11 , mesothelioma claim 11 , or primary lung cancer.13. The method of claim 1 , wherein said cancer is breast cancer claim 1 , colon cancer claim 1 , renal cell cancer claim 1 , non-small cell lung cancer claim 1 , hepatocellular carcinoma claim 1 , gastric cancer claim 1 , ovarian cancer claim 1 , pancreatic cancer claim 1 , esophageal cancer claim 1 , prostate cancer claim 1 , sarcoma claim 1 , or melanoma.14. The method of claim 1 , wherein said cancer is gastrointestinal cancer.15. The method of claim 14 , wherein said gastrointestinal cancer is esophageal cancer claim 14 , stomach cancer claim 14 , pancreatic cancer claim 14 , liver cancer claim 14 , ...

THERAPEUTIC COMPOUNDS

The invention provides methods for producing analgesia in an animal comprising administering to the animal a compound of the formula Ia′, Ib′, Ic′, and Id′:

Blood Brain Barrier-Penetrating Oximes for Cholinesterase Reactivation

The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system. 2. The compound of wherein:{'sub': 1', '2', '3', '1', '5', '2', '5', '2', '5', '3', '6', '3', '6', '6', '12, 'R, R, and Rare each independently selected from the group consisting of hydrogen, C-Coptionally substituted alkyl, C-Coptionally substituted alkenyl, C-Coptionally substituted alkynyl, C-Coptionally substituted cycloalkyl, C-Coptionally substituted cycloalkenyl, C-Coptionally substituted aryl, 5- and 6-membered optionally substituted heteroaryls containing 1-3 atoms selected from the group consisting of nitrogen, oxygen, and sulfur;'}{'sub': 4', '1', '5', '2', '5', '2', '5', '3', '6', '3', '6', '6', '12, 'Ris selected from the group consisting of a bond, oxygen, sulfur, nitrogen, C-Coptionally substituted alkylene, C-Coptionally substituted alkenyl, C-Coptionally substituted alkynyl, C-Coptionally substituted cycloalkyl, C-Coptionally substituted cycloalkenyl, C-Coptionally substituted aryl, 5- and 6-membered optionally substituted heteroaryls containing 1-3 atoms selected from the group consisting of nitrogen, oxygen, and sulfur;'}{'sub': 5', '1', '5', '2', '5', '2', '5', '3', '6', '3', '6', '6', '12, 'Ris selected from the group consisting of hydrogen, C-Coptionally substituted alkyl, C-Coptionally substituted alkenyl, C-Coptionally substituted alkynyl, C-Coptionally substituted cycloalkyl, C-Coptionally substituted cycloalkenyl, C-Coptionally substituted aryl, 5- and 6-membered optionally substituted heteroaryls containing 1-3 atoms selected from the group consisting of nitrogen, oxygen, and sulfur;'}{'sub': '6', 'Ris selected from the group consisting of hydrogen, an oxime protecting group selected from the group consisting ...

PHENYL IMIDAZOLINE COMPOUND HAVING AMINOMETHYL GROUP OR SALT THEREOF, OR PHENYL TETRAHYDROPYRIMIDINE COMPOUND HAVING AMINOMETHYL GROUP OR SALT THEREOF, AND PRODUCTION METHOD FOR SUCH COMPOUNDS OR SALTS THEREOF

In order to provide a novel phenyl imidazoline compound having an aminomethyl group, a novel phenyl tetrahydropyrimidine compound having an aminomethyl group, or the like, a compound according to the present invention or a salt thereof is represented by the following formula (1): 5. An epoxy resin curing agent claim 1 , comprising a compound according to claim 1 , or a salt thereof.6. An epoxy resin composition claim 1 , comprising:an epoxy resin; and{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'an epoxy resin curing agent according to .'} The present invention relates to a phenyl imidazoline compound having an aminomethyl group or a salt thereof, or a phenyl tetrahydropyrimidine compound having an aminomethyl group or a salt thereof, and a production method for such compounds or salts thereof.Phenyl imidazoline compounds and phenyl tetrahydropyrimidine compounds are useful compounds as building blocks for medicinal products since they are biologically and/or pharmacologically active. In addition, these compounds are useful as raw materials or additives for polymers. Phenyl imidazoline is a known curing agent and/or curing accelerator for epoxy resins and it is one of the important compounds serving as raw materials for compositions. As examples of such compounds, Patent Document 1 describes a diamino-s-triazine compound having an imidazoline ring, and Non-Patent Document 1 describes 2-phenylimidazole having an imidazoline ring. Non-Patent Document 2 describes methods for producing cyanophenyl imidazoline and cyanophenyl tetrapyrimidine. In the meantime, meta-xylenediamine (MXDA)—an example aminomethyl benzene compound having an aminomethyl group—is used as a raw material for polyamides and polyurethanes, and, in particular, it is widely known as an epoxy resin curing agent. Such meta-xylenediamine is also one of the important compounds serving as a raw material for compositions. Non-Patent Document 1 describes such aminomethyl group-containing meta- ...

CHIRAL 1,3-DIARYLIMIDAZOLIUM SALT CARBENE PRECURSOR, SYNTHESIS METHOD THEREFOR, METAL SALT COMPOUND AND APPLICATION THEREOF

Chiral 1, 3-diarylimidazole salt carbene precursors, their methods of preparation, particularly transition metal complexes and their use in chemical synthesis are provided. In particular, an air and moisture stable chiral 1, 3-diarylimidazole carbene precursor Cu (I) complex has been prepared and applied to highly regio- and enantioselective Markovnikov hydroboration of unactivated terminal alkenes to form chiral boronic esters. Moreover, these new chiral NHCs can be potentially applied in various metal-catalyzed asymmetric transformations. 6. The method according to claim 5 , whereinin method a), the reaction is conducted under solvent-free condition;and/or in method a), the halomethyl alkyl ether is chloromethyl ether and/or bromomethyl ether.and/or in method a), the molar ratio between the compound S′ to halomethyl alkyl ether is 1:5 to 1:30;and/or in method a), the temperature used herein is generally 80° C. to 130° C.;and/or in method b), the solvent used herein is one or more selected from the group consisting of nitrile solvents, halogenated hydrocarbon solvents, amide solvents and ether solvents;{'sub': 2', '3', '2', '3', '2', '3, 'and/or in method b), the base used herein is an organic base and/or inorganic base; the organic base is preferably tertiary amine, e.g., DIPEA and/or trimethylamine; the preferable inorganic base used herein is alkali carbonate, which is one or more selected from the group consisting of NaCO, KCOand CsCO;'}and/or in method b), the molar ratio of base to the compound M6 is generally 0.9 to 1.5;and/or in method b), the molar ratio of the compound S2 to the compound M6 is generally 1.2 to 5;and/or in method b), the temperature used herein is 50° C. to 100° C.;{'sub': 4', '4', '4, 'and/or in method c), the formula NHX used herein is NHCl or NHBr;'}{'sub': '4', 'and/or in method c), the molar ratio of NHX to the compound M8 is 1.2 to 3;'}and/or in method c), the volume molar ratio of triethyl orthoformate to the compound M8 is 3 to 15 ...

Inhibitors of the n-terminal domain of the androgen receptor

The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.

N-acylsulfonamide apoptosis promoters

本发明公开了抑制抗细胞程序死亡蛋白家族成员活性的N－酰基磺酰胺化合物，包含所述化合物的组合物，以及所述化合物在制备用于治疗疾病的药物中的应用，所述疾病是在其期间有一个或多个抗细胞程序死亡蛋白家族成员表达的疾病。

用于促进损伤的身体组织再生的包含活性物质的组合物

本发明涉及一种用于促进损伤的身体组织的再生的组合物，其包含作为活性剂的四氢嘧啶、羟基四氢嘧啶、甘油葡萄糖苷和/或这些化合物的盐、酯或酰胺。本发明具有用于治疗慢性伤口或溃疡的特殊意义。

Apoptosis promoters

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

Apoptosis promoters

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

N-acylsulfonamide apoptosis promoters

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

Acyclic compounds and methods for treating multidrug resistance

Substituted acyclic compounds are disclosed. The compounds are useful for treating multidrug resistance. The compounds can be formulated in compositions with a carrier and, optionally, a therapeutic agent. One suitable substituted acyclic compound has the formula:

Method of obtaining n-substituted trichloracetamidines or salts thereof

N1-((Pyrazol-1-Ymethyl)-2-Methylphenyl)-Phatalamide Derivatives And Related Compounds Insecticides

Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C 1-6 alkylsulfonyloxy, C 1-6 alkylsulfinyl, C 1-6 alkylsulfenyl or C 1-6 alkylsulfonyl, R 1 represents C 1-6 alkyl, C 1-6 alkylthio-C 1-6 alkyl, or C 1-6 alkyl, m represents 0 or 1, A represents O, S, SO, SO 2 , CH 2 or CH(CH 3 ), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.

Heterocycle-substituted n-phenyl-phthalamide derivatives, related compounds and their use as insecticides

Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C 1-6 alkylsulfonyloxy, C 1-6 alkylsulfinyl, C 1-6 alkylsulfenyl or C 1-6 alkylsulfonyl, R 1 represents C 1-6 alkyl, C 1-6 alkylthio-C 1-6 alkyl, or C 1-6 alkyl, m represents 0 or 1, A represents O, S, SO, SO 2 , CH 2 or CH(CH 3 ), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.

Heterocycle-substituted, n-phenyl-phthalamide derivatives, related compounds and their use as insecticides

Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C 1-6 alkylsulfonyloxy, C 1-6 alkylsulfinyl, C 1-6 alkylsulfenyl or C 1-6 alkylsulfonyl, R 1 represents C 1-6 alkyl, C 1-6 alkylthio-C 1-6 alkyl, C 1-6 alkylsulfinyl-C 1-6 alkyl or C 1-6 alkylsulfonyl-C 1-6 alkyl, Y represents halogen or C 1-6 alkyl, m represents 0 or 1, A represents O, S, SO, SO 2 , CH 2 or CH(CH 3 ), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.

Subtype selective nmda receptor ligands and the use thereof

Diamine derivative

Disclosed is a diamine derivative represented by the following general formula (I): [wherein Q represents an oxygen atom or the like, RG represents a hydrogen atom or the like, RI represents AA (wherein p and r may be the same as or different from each other and respectively represent 0 or the like, RA represents a hydrogen atom or the like, and RB and RC may be the same as or different from each other and respectively represent a hydrogen atom or the like), RH represents a hydrogen atom or the like, and RJ represents BB (wherein q and s may be the same as or different from each other and respectively represent 0 or the like, RD represents a hydrogen atom or the like, and RE and RF may be the same as or different from each other and respectively represent a hydrogen atom or the like)].

The preparation method and applications of a kind of chirality six-membered heterocycle carbene precursor salt

本发明涉及有机合成领域，具体为具有四氢嘧啶骨架的手性六元氮杂环卡宾前体盐的合成及其应用。本发明所述的手性六元氮杂环卡宾前体化合物为具有式(Ⅲ)所示结构的化合物或者其如式(Ⅲ’)所示的对映异构体： R 1 选自苯基、1‑萘基、2‑萘基、苄基、异丙基、异丁基、仲丁基、叔丁基或环己基；R 2 选自氯离子、溴离子、四氟硼酸根离子或六氟磷酸根离子，优选自氯离子和四氟硼酸根离子；R 3 选自氢、1‑萘甲酰基、2‑萘甲酰基、2,4,6‑三甲基苯甲酰基、对甲氧基苯甲酰基或对叔丁基苯甲酰基。本发明开发一种C 2 对称的新型手性六元氮杂环卡宾前体化合物的合成方法，扩大其在药物中间体合成及有机不对称合成反应中的应用范畴。

Process for separating pyrimidine derivatives from aqueous solutions

Separation and purification of pyrimidine derivatives (I), especially tetrahydro-pyrimidines, from aqueous solution comprises: (i) contacting the solution with an acidic zeolite (II) to adsorb (I) at a suitable pH; and (ii) recovering (I) by desorption and another pH value.

Process for the separation of tetrahydropyrimidine derivatives

Die Erfindung betrifft ein Verfahren zur Auftrennung von Tetra-hydropyrimidin-Derivaten, insbesondere 2-Methyl-1,4,5,6-tetrahydropyrimidin-4-Carbonsäuren (Ectoine) und 2-Methyl,5-Hydroxyl-1,4,5,6-tetrahydropyrimidin-4-Carbonsäuren (Hydroxyectoine), die nebeneinander in wäßrigen Lösungen, insbesondere Fermentationsbrühen vorliegen, durch selektive Adsorption einer Komponente an Zeolithen. The invention relates to a method for the separation of tetrahydropyrimidine derivatives, in particular 2-methyl-1,4,5,6-tetrahydropyrimidine-4-carboxylic acids (ectoins) and 2-methyl, 5-hydroxyl-1,4,5, 6-tetrahydropyrimidine-4-carboxylic acids (hydroxyectoins), which are present next to one another in aqueous solutions, in particular fermentation broths, by selective adsorption of a component on zeolites.

Method for separating and isolating in a highly purified manner low molecular, similar structured compounds, particularly tetrahydropyrimidine derivatives and fission products thereof

The invention relates a method for separating and isolating in a highly purified manner low molecular, similar structured compounds, particularly tetrahydropyrimidine derivatives, for example, 1,4,5,6-tetrahydro-2-methyl-4-pyrimidane carboxylic acids (ectoines) or firoines (α mannosylglycerate, α mannosylglyceramide) and the fission products thereof. The fission products are separated with the aid of a pure alcoholic or aqueous solution or mixtures thereof in at least one method of separation and are separated, in particular, in at least two identical or different methods of separation.

2-nitro-5-phenoxyphenyl compound, its manufacture and herbicidal and plant growth regulant agent containing it

Patent IN170284B

Ionizable lipid molecule, preparation method thereof and application thereof in preparation of lipid nanoparticles

本发明公开了一种可离子化脂质分子、其制备方法、包含其的组合物、其在制备用作将核酸递送至细胞的载体中的应用及其在制备脂质纳米颗粒LNP的应用，通过改进可离子化脂质分子的结构并对LNP组分方案的调整，提高mRNA‑LNP制剂的作用效力。本发明的可离子化脂质分子具有式(I)的结构： 所述可离子化脂质分子与磷脂、胆固醇、聚乙二醇通过微流控合成获得LNP，得到的LNP能提高负载物‑mRNA在细胞内的翻译表达水平，提高mRNA‑LNP制剂的作用效力，给予个性化mRNA‑LNP制剂的理论治疗提供了理论基础。

Method of preparing nitrocompound

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

Nitromethylene-tetrahydropyrimidine derivative, production method and insecticide, acaricide, sentinelicide

Muscarinic agonists

Substituted 1,4,5,6 -tetrahydropyrimidine compositions, substituted 1,2,3,6-tetrahydropyrimidine compositions and substituted 3,4,5,6-tetrahydropyridine compositions are disclosed. They are useful for stimulating muscarinic receptors including, for example, treating the symptoms of cognitive disorders, especially impared memory, which are associated with decreased acetylcholine synthesis and cholinergic cell degeneration.

Muscarinic agonist compounds

A muscarinic agonist compound having the structure (I) or (II): ##STR1## where R is methyl or dimethylamino; or ##STR2## where R' is dimethylamino.

Benzoisothiazolopyrimidine derivative and salt thereof,and viral infection inhibitor and drug

Provided is a novel compound having anti-virus activity. The compound or a salt thereof, is characterized by being represented by formula (I). R 1 -R 3 independently represent a H atom, halogen atom, C1-6 alkyl group, C1-6 alkoxy group, C2-6 alkenyl group, C2-6 alkynyl group, C2-6 alkylene group, aryl group, heteroaryl group, nitro group, alkyl carbonyl amino group with a C1-6 alkyl group, C1-6 fluoroalkyl group, amino group, C1-3 mono- or di-alkyl amino group, benzoyl amino group, azide group, carboxyl group, C1-3 alkyl carbonyl group, C1-3 alkoxy carbonyl group, carbamoyl group, naphthyl group, heteroaryl group, styryl group, C1-3 alkylthio group, or C1-6 hydroxy alkyl group, may be substituted with a substituent, and may be the same or different; R 1 and R 2 , and R 2 and R 3 may be crosslinked, and a crosslink between adjacent substituents may contain a heteroatom; R 4 represents a C1-5 linear alkylene group or a heteroatom, may be substituted with a substituent, and when R 4 is an alkylene group, substituents on the alkylene group may bind to one another to form a crosslinked structure or a ring structure; X 1 and X 2 independently represent a heteroatom, may be substituted with a substituent, may be the same or different, and may be crosslinked.

Synthetic method of 1,2-dimethyl-1,4,5,6-tetrahydropyrimidine

本发明提供的1,2‑二甲基‑1,4,5,6‑四氢嘧啶合成方法，通过添加硫代乙酰胺或者硫化氢作为催化剂，大大缩短了N‑甲基丙二胺与乙腈的反应时间，在较短的反应时间内得到了高收率，极大的提高了反应的经济性。

NOVEL ARYLSULFONAMIDE DERIVATIVES AND THEIR USE IN THERAPEUTICS

Substituted heterocyclic compounds and their use as fungicides

(57)【要約】 本発明は新規な置換された複素環式化合物、それらの複数の製造方法および殺菌・殺カビ剤としてのそれらの使用、並びに中間体、それらの複数の製造方法および殺菌・殺カビ剤としてのそれらの使用に関する。

Nitro-substituted heterocyclic compounds

Novel nitro-substituted heterocyclic compounds of the formula (I) and the use of the new compounds as insecticides.

Novel tetrahydropyrimidine derivatives, process for their preparation and insecticides containing same as active ingredients

The invention relates to compounds represented by general formula (I) (wherein R 1 , R 3 and R 4 , which may be the same or different, each represents an optionally substituted heterocyclic methyl group, hydrogen, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted phenyl group, α, β, ψ, δ or ε (wherein R 5 , R 6 , R 7 , R 8 , R 9 and R 10 , which may be the same or different, each represents an optionally substituted heterocyclic methyl group, hydrogen, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, or an optionally substituted phenyl group, and n represents 0, 1 or 2), R 2 represents an optionally substituted heterocyclic methyl group, hydrogen, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, or an optionally substituted phenyl group, provided that the cases wherein R 1 represents hydrogen, R 2 , R 3 and R 4 represent each a benzyl group and wherein R 2 represents hydrogen and R 1 , R 3 and R 4 represent each a benzyl group are excluded), a process for preparing same, and insecticides containing same as active ingredients.

Patent JPH0360414B2

Process for producing 3-heterocyclic derivatives of 4-nitro-2-chloro(or 2,6-dichloro)-4-trifluoromethydiphenyl esters

Amidine catalyst for curable compositions

N- (ARYLSULFONYL) AMINO ACID DERIVATIVES, THEIR PREPARATION, THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

NEW PERHALOGENOALCOYLAMIDINES SUBSTITUTED AS HEART STIMULANTS

New derivatives of benzamidobenzanilide.

Process Improvements for the Preparation of Cyclic Substituted Vinyl Amidines

Patent FR2207706A1

Process for the production of nu-vinylamidines

Impregnation process for leathers and leather substitutes

Process for the preparation of tetrahydropyrimidine derivatives

Process for the preparation of nu-sulfonylamidines

Synthesis of 6,7-dihydro-5h-imidazo[1,2-a]imidazole-3-sulfonic acid amides.

Se describe procedimiento de etapas multiples para preparar compuesto de la formula 1: en la que R' a son como se ha definido en la presente. Los compuestos de la formula 1 inhiben la union de moleculas humanas de adhesion intercelular a las integrinas leucocitarias. Corno resultado, estos compuestos son utiles en el tratamiento de enfermedades inflamatorias y mediadas por inmunocitos.

Systemic fungicidal salicylic acid ester(s) - 3,4,5,6-tetra:hydro:pyrimidin-2-yl-methyl and 2-imidazolin-2-yl methyl esters of 5-methyl 3-norbornyl-(2) salicylic acid

Exo or endo 5-methyl-3-(2-norbornyl- salicylic acid esters of formula (I) racemates, enantiomers and their acid addn. salts are novel (where m is 0 or 1). (I) are prepd. prepd. by reaction of the salicylic acid with halomethyl, imidazole or halomethyl tetrahydropyrimidine in inert solvent in presence of mineral base and opt. catalyst. Systemic fungicides active against Fusarium roseum, Rizoctonia solani, Phomopsis viticola, Alternaria tenuis, Uromyces phaseoli, Peronospora viticola, Botrytis fabae, Botrytis cinerea, Penicillium expansum, Aspergillus niger, Phytophtora infestans and Erysiphe graminis. They are generally applied to crops at 50-2000 g/ha. Activity tests are described.

Biocidal composition for agricultural use

Pesticidal organophosphorus compsns - stabilized by 2- (pyridyl or phenyl)vinyl-imidazolines and-tetrahydropyrimidines

Pesticidal compsns. contg. as active component, a cpd. of formula: (where R is an org. gp. of 1-4C; Z is O or S; X, X' are halogen esp. Cl, Br; stabilized by 0.1-10% of a cpd. of formula where n is 2 or 3; X is NH or NR where R is alkyl; Ar is pyridyl or phenyl opt. substd. by one or two alkyl, halogen, OH, -OMe, -OEt or NO2 gps. and >=1 of the stabilizers described in the parent patent. The stabilized compsns. are insecticidal and anthelmintic, and pref. contain dichlorvos as the active component.

Hypoglycaemic (2)-substd. (1,3)-diaza-heterocyclic cpds. - e.g. (2)-benzhydrylimino-imidalodine prepd. e.g. by reacting (2)-mercapto-imidazolines with amines

New 2-substd. 1-3-diaza heterocyclic cpds. are of formula (I) and their salts. In the formula R1 is H, halogen, lower alkyl or lower alkoxy; R2 is H, lower alkoxycarbonyl, aliphatic acyl, or aromatic acyl the aromatic ring of which may be substd. by halogen, lower alkyl, lower alkoxy, acyl and/or acyloxy. R3 is H, lower alkyl, lower hydroxyalkyl or aralkyl, R4 is H, lower alkyl or aryl. R6 is cyclohexyl, pyridyl, or phenyl opt. substd. by halogen, lower alkyl or lower alkoxy. A is -N=, -N(lower alkyl)- or CH2. n is 2, 3 or 4. Broken lines indicate the optional presence of a double bond. (I)have hypoglycaemic and blood platelet aggregation inhibiting activity, and are free from undesirable side-effects. Specific (I) include 2-benzhydrylimino-imidazolidine. In an example, this is prepd. by refluxing 7.3 g benzhydrylamine and 4.88 g 2-methylthio-2-imidazoline hydriodide 3 hrs. in 10 ml methanol.

Process for preparing trisubstituted hydrazinium chlorides

Cyclic formamidine prepn

Cpds. of formula: (where each R is H, aliphatic, cycloaliphatic, arylaliphatic, or aromatic, and n is 2,3 or 4) are prepd. by passing cpds. of formula NRR1- CR2 n -NHR1 (where one R1 is H or -CHO and the other is -CHO) over activated silica or silicate at 400-600 degrees C. The products are useful as chemical intermediates. Previous methods used reagents that were toxic or expensive; this method avoids these reagents.

Amidine catalysts for curable compositions

本发明涉及式(I)的脒及其作为用于交联可固化组合物的用途。式(I)的脒包含至少一个脂族脒基。其在室温下基本上无气味并且不挥发并且非常有效地加速可固化组合物的交联，而不会影响组合物的储存稳定性。其特别适用于基于含硅烷基团的聚合物的组合物，与所述组合物具有非常好的相容性，因此所述组合物不倾向于出现催化剂的分离或迁移或蒸发。

Heterocyclic compounds

Novel insecticides of the formula ##STR1## in which n is 0 or 1, X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R 9 variously represent hydrogen or specified organic radicals.

Benzamidine derivatives

Antitumoral tetrahydropyrimidines

Antitumoral compounds of the formula (I) wherein x is O, S or Nr, obtained from a maze coral of the family Meandrinidae, genus Meandrina, species meandrites, or derivatives thereof are useful as antitumoral agents.

Novel heterocyclic compounds

Novel insecticides of the formula ##STR1## in which n is 0 or 1, X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R 9 variously represent hydrogen or specified organic radicals.

PHARMACEUTICAL COMPOUNDS WITH ANTI-SECRET ACTION AND PREPARATION PROCEDURE

Heterocyclic compounds

Die vorliegende Erfindung betrifft neue heterocyclische Verbindungen der Formel (I) <IMAGE> worin N 0 oder 1, R¹, R², R<5> und R<6> unabhängig voneinander ein Wasserstoffatom oder eine Alkylgruppe bedeuten, R³ und R<4> unabhängig voneinander ein Wasserstoffatom, eine Hydroxygruppe oder eine Alkylgruppe bezeichnen, wenn n 1 bezeichnet, R² eine Einfachbindung zusammen mit R<5> zu bilden vermag, X ein Schwefelatom, ein Sauerstoffatom oder die folgenden Gruppen bedeutet: -?-R<7> oder -?H-R<8> worin R<7> und R<8> die im Anmeldetext angegebene Bedeutung haben, R ein Wasserstoffatom oder eine Alkylgruppe bedeutet, Y ein Stickstoffatom oder die Gruppe =?-R<9> bedeutet, worin R<9> die im Anmeldungstext angegebene Bedeutung hat und Z die im Anmeldungstext angegebene Bedeutung hat. The present invention relates to new heterocyclic compounds of the formula (I) <IMAGE> wherein N 0 or 1, R 1, R 2, R 5 and R 6 independently of one another represent a hydrogen atom or an alkyl group, R 3 and R 4 independently from each other denote a hydrogen atom, a hydroxyl group or an alkyl group, if n denotes 1, R² is able to form a single bond together with R <5>, X denotes a sulfur atom, an oxygen atom or the following groups: -? - R <7> or - ? HR <8> in which R <7> and R <8> have the meaning given in the application text, R represents a hydrogen atom or an alkyl group, Y represents a nitrogen atom or the group =? - R <9>, where R <9> has the meaning given in the application text and Z has the meaning given in the application text.

2-Substituted heterocyclic compounds and their use in treating multidrug resistance

N-HETEROCYCLIC CARBEN-TYPE CHIRAL LIGANDS FOR ASYMMETRICAL CATALYSIS.

Composés de formule (I) ou de formule (II) dans lesquelles X est un anion ; n<1>= 0, 1, 2 ; n<2> = 1 à 4 ; R<1> est un alkyl en C1 à C6, ou un cycloalkyl en C5 ou C6 éventuellement substitué, ou un perhalogénoalkyl en C1 C6 ; R<2> est un alkyl en C1 à C8, ou un cycloalkyl en C5 ou C6 éventuellement substitué, ou un aryl éventuellement substitué, ou un naphtyl éventuellement substitué, ou un radical -CH3-n(Aryl)n avec n=1 à 3, ou un radical -CH(R)Z où R est un hydrogène, ou une alkyl en C1 à C6, ou un cycloalkyl en C5 ou C6 éventuellement substitué, ou un perhalogénoalkyl en C1 à C6; Z est un alkyl en C1 à C8, ou un cycloalkyl en C5 ou C6, ou un radical de formule : Y est un hydrogène, ou un OR<9>, ou SR<10>, ou un P(R<11>)2, ou un halogène ou un OSO2R<12> ; n<3> = 1 à 4 ;R<3>, R<4>, R<5>, R<6>, R<7>, R<8>, R<9>, R<10>, R<11>, R<12>, sont, indépendamment, un H, ou un alkyl en C1 à C6, ou un perhalogénoalkyl en C1 à C6, ou un cycloalkyl en C5 ou C6 éventuellement substitué ou un aryl; R<3> et R<4> d'une part et R<6> et R<7> d'autre part pouvant former un cycle à 3, 4, 5, 6 et 7 chaînons ; R<5> et R<8> pouvant former indépendamment un cycle aromatique à 6 chaînons. Compounds of formula (I) or of formula (II) in which X is an anion; n <1> = 0, 1, 2; n <2> = 1 to 4; R <1> is C1 to C6 alkyl, or optionally substituted C5 or C6 cycloalkyl, or C1 to C6 perhaloalkyl; R <2> is a C1 to C8 alkyl, or an optionally substituted C5 or C6 cycloalkyl, or an optionally substituted aryl, or an optionally substituted naphthyl, or a radical -CH3-n (Aryl) n with n = 1 to 3, or a radical -CH (R) Z where R is hydrogen, or a C1 to C6 alkyl, or an optionally substituted C5 or C6 cycloalkyl, or a C1 to C6 perhaloalkyl; Z is a C1 to C8 alkyl, or a C5 or C6 cycloalkyl, or a radical of the formula: Y is a hydrogen, or ...

2-nitro-5-phenoxyphenyloxazole,-oxazine,-imdazole,- pyrimidine or -thiazole derivatives

Prostaglandin analogs

Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. A, X, J, E, and Z are as described herein. These compounds are useful for treating diseases.

Organic compounds

The invention relates to naphthalene carboxylic acid and isoquinoline carboxylic acid amides, and related compounds of formula (I) and their uses as pharmaceuticals.

Compound and composition epoxy resin containing it

本发明提供储存稳定性优异、且固化性优异的环氧树脂组合物，具体而言，提供下述通式(I)表示的化合物及包含其作为固化剂的环氧树脂组合物。式中，R 1 为可以包含氮原子的烃基、且可形成可以具有取代基的环状结构，R 2 表示氢原子、烷基、芳基、或者可以与R 1 一起形成不饱和键，R 3 表示氢原子、烷基或芳基，X表示二氰胺根或硫氰酸根，

Melanocortin-4 receptor binding compounds and methods of use thereof

Provided are MC4-R binding compounds of the formula XVII: (XVII), wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, Z5, t, s, and R are as described in the specification. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also provided.

Process for preparing quaternized imidazoline fabric conditioning compounds

PROCESS FOR PREPARING QUATERNIZED IMIDAZOLINE FABRIC CONDITINOING COMPOUNDS Theresa Rosario Jansen Glen D. Lichtenwalter ABSTRACT OF THE DISCLOSURE Disclosed is a high yield process for quaternizing imidazoline ester compounds in the absence of lower alcohol solvents and under anhydrous conditions. The reaction product of this process contains a quaternized imidazoline ester fabric softening compound and, optionally, an imidazoline ester compound. In the process of this invention, an imidazoline ester compound is initially heated to form an anhydrous melt. This anhydrous melt is subsequently contacted with a quaternizing agent selected from small chain organic halides and sulfates. The imidazoline ester compound and quaternizing agent are then reacted under anhydrous conditions for a period of time sufficient for substantially all of said quaternizing agent to react with said imidazoline ester compound to form a quaternized imidazoline ester compound of the formula: X- (II)

Method for preparation of imidazoline or pyrimidine derivatives or theirs physiologically tolerated acid-additive salts

New pharmacologically active heterocyclic derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders of the following formula wherein R is hydrogen atom or C₁₋₉ alkyl optionally substituted by 2 or 3 radicals, which may be identical or different from each other, selected from aryl, cycloalkyl, hydroxy and carboxamide; R₁ may be any group indicated for R, or NHR₄, in which R₄ is hydrogen atom, C₁₋₄ alkyl substituted by -OOCR₅, in which R₅ is methyl sub­stituted by 2 or 3 radicals, which may be identical or different from each other, selected from aryl, cycloalkyl and hydroxy, or a cycloalkyl substituted by another cycloalkyl; R₂ is hydrogen atom, C₁₋₄ alkyl, a radical -OOCR₅, in which R₅ is as hereinbefore defined; R₃ is hydrogen atom or C₁₋₄ alkyl; n is 0, 1 or 2 provided that at least one among R, R₁, R₂ and R₃ is different from hydrogen atom. The tautomers of the compounds of formula (I) and acid addition salts thereof, as well as the processes for their preparation and pharmaceu­tical compositions containing them are also described

Prostaglandin analogs

Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. A, X, J, E, and Z are as described herein. These compounds are useful for treating diseases.

Insecticide compositions containing nitro-methylene derivative and process for producing the active component

INSECTICIDES, MITICIDES, TICICIDES AND NEMATICIDES

Die vorliegende Erfindung beschreibt(1) ein Nitromethylen-tetrahydropyrimidin-Derivat der allgemeinen Formel (I),in der X fuer Halogen steht,(2)Verfahren und Herstellung des Nitromethylen-tetrahydropyrimidin-Derivats der allgemeinen Formel (I),(3)insektizide, mitizide und nematizide Mittel, die als Wirkstoff das Nitromethylen-tetrahydropyrimidin-Derivat der allgemeinen Formel (I) enthalten, und(4)ein Verfahren zur Bekaempfung schaedlicher Insekten, Milben oder Zecken und Nematoden, bei dem das Nitromethylen-tetrahydropyrimidin-Derivat der allgemeinen Formel (I) entweder allein oder in Kombination mit Verduennungsmittel (einem Loesungsmittel und/oder einem Streckmittel und/oder einem Traeger) und/oder einem oberflaechenaktiven Mittel und, falls weiterhin erforderlich, einem Stabilisator, einem Haftmittel und einem synergistischen Mittel zur Einwirkung gebracht wird. The present invention describes (1) a nitromethylene-tetrahydropyrimidine derivative represented by the general formula (I) in which X is halogen, (2) the method and preparation of the nitromethylene-tetrahydropyrimidine derivative represented by the general formula (I), (3) insecticides , miticidal and nematicidal agents containing as active ingredient the nitromethylene-tetrahydropyrimidine derivative of the general formula (I), and (4) a method for controlling harmful insects, mites or ticks and nematodes, wherein the nitromethylene-tetrahydropyrimidine derivative is the general Formula (I) is applied either alone or in combination with a disintegrating agent (a solvent and / or extender and / or vehicle) and / or a surfactant and, if necessary, a stabilizer, an adhesive and a synergistic agent ,

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- ...

Synthesis of 6,7-dihydro-5h-imidazoý1,2-a¨imidazole-3-sulfonic acid amides

Disclosed is a multi-step process for preparing a compound of Formula I wherein R1 to R3 are as defined herein. The compounds of Formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.

Arylsulphonamide derivatives and use thereof as b1 bradykinin receptor antagonists

CHIRAL LIGANDS OF N-HETEROCYCLIC CARBENE TYPE FOR ASYMMETRIC CATALYSIS.

NETSUGENZOKARAAKANKOZAIRYO

Procss for preparation of hetero cyclic compounds

내용 없음. No content.

Substituted bis-benzimidazolyl compounds and pharmaceutical compositions

Preparation of saturated imidazolinium salts and related compounds

本发明公开了饱和咪唑啉鎓盐及相关化合物的制备方法，该方法包括甲脒与诸如二卤代乙烷之类的化合物和任选的碱的反应。或者，咪唑啉鎓盐及相关化合物可在一步法中制得而无需纯化甲脒反应物。这些方法可以在无溶剂的反应条件下以优良的产率获得多种咪唑啉鎓盐及相关化合物。