ПРОИЗВОДНЫЕ ДЕКАПЕПТИДОВ И СОДЕРЖАЩАЯ ИХ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Изобретение относится к пептидным соединениям, а именно к декапептидам формулы I: Х-Х1 -X2-Х3-Ser-Tyr-Х6 -Leu-X8-Pro-X10 (I), где Х- ацил; X1=D-Nal; Х2=D-Cpa; Х3=D-Рal; Х6=D-Cit; D-Hei, D-Orn, D-Lys, D-Neu; Х8= Orn, Arg, Lys, L-Neu ; X10= D-AlaNH2, Neu является остатком формулы IX или IV; Z - группа -O- или -S-, п = 1-6. Фармацевтическая композиция обладает LHRH - антагонистической активностью. Преимущество соединений 1 в том, что их фармакологическое действие очень высоко и побочные действия в форме выделения гистамина удерживаются на низком уровне. 2 с. и 4 з.п.ф-лы.

Цетиловые эфиры @ -пиперидино- или @ -морфолинокротоновой кислоты в качестве ингибиторов коррозии стали и чугуна в индустриальном масле

Изобретение касается гетероциклических веществ, в частности цетиловых эфиров / -пиперидинокротоновой и / -мор- фолинокротоновой кислот в качестве ингибиторов коррозии стали и чугуна в индустриальном мас/;е. Цель-.создание новых более эффективных веществ указанного класса. Синтез ведут реакцией цетилового эфира ацетоуксус ной кислоты с пиперидином или морфолином при кипячении в бензоле . Выход, %; т.пл.. °С; брутто-ф-ла I) 85: 42-44: C25H47N02; II): 80:49-50: . Использование 1 %-ного раствора новых веществ в масле И-12А ингибирует коррозию стали Ст 10 и чугуна СЧ 20 в течение 39 и 34-х циклов против 30 циклов с известным ингибитором АКОР-1 (10%-ный раствор). 1 табл. (Л С ...

Способ получения замещенного 6-фенил-1,2,4-триазол-/4,3-в/-пиридазина

Способ получения производных акриловой кислоты

Изобретение относитс  к моноциклическим аминам, в частности к производным акриловой кислоты ф-лы @ , где R 1 - нитрил, группа - COOR 2, где R 2 - метил или этил X-CL или F X 1-H или F X 2 - CL или F, которые  вл ютс  промежуточными продуктами дл  синтеза антибактериальных лекарственных средств. Цель - упрощение процесса и повышение выхода целевого продукта. Получение ведут реакцией бензоилгалогенида с производным карбоновой кислоты в среде инертного растворител  и акцептора кислоты с последующей обработкой полученного соединени  циклопропиламином в среде инертного растворител .

Способ получения пиперазинсодержащих углеводородов или их кислотно-аддитивных солей

Изобретение касается производных пиперазина и, в частности, способа получения пиперазинсодержащих углеводородов (ПУВ) общей формулы М - Z - М, где М - группа - (CH2)M- CR3R4- (CH2)N- C6H3R1R2 R1и R2, одинаковые или различные, - Н, СН3, С1-С4-алкоксил, C, BR, F, - CF3, ацетоксигруппа R3- H или OH R4=H или (R4+R3) - кислород, если M=1 и N=0 M и N означают 0,1,2, причем (M+N)≠3 Z - -K-CR6R7- X - CR8R9-K- R6-R9, одинаковые или различные, - H или CH3, или R6и R7и/или R8и R9- кислород X - C1-C2- алкилен (он может быть замещен - OH) K - группа - @ А- -СН2- или - CH2-CH2- R5-H или 2-4 метильные группы у атомов углерода пиперазинового кольца, или их кислотно-аддитивных солей, обладающих антиаллергической и противовоспалительной активностью, которые могут найти применение в медицине. Цель изобретения - создание новых более активных веществ указанного класса. Синтез ПУВ ведут реакцией соединения формулы H - Z - H и соединения формулы M - Y, где Z, M - см.выше Y - галоген, взятых в соотношении 1:(2 ...

Tertiäre alkyl funktionalisierte Piperazin-Derivate

NEUE ARYLGLYCINAMIDDERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN

Schaedlingsbekaempfungsmittel

TRIARYLMETHANVERBINDUNGEN ZUR BEHANDLUNG VON KREBS, AKTINISCHER KERATOSE UND KAPOSISARKOM

AMINO-THIOLESTER-VERBINDUNGEN, DIESE ENTHALTENDE PHARMAZEUTISCHE UND KOSMETISCHE ZUSAMMENSETZUNGEN UND IHRE ANWENDUNGEN

Piperidinomethylverbindungen und Verfahren zu ihrer Herstellung

3,4,5-TRIETHOXYBENZYL PROPIONITRILES AND ACRYLONITRILES

Improvements in or relating to amines and aminonitriles and preparation thereof

An aminonitrile of formula where R is an aryl thienyl pyridyl or furyl group, Y is an alkylene bridge of 2-3 carbon atoms, -N=B is an aliphatic tertiary amino group, and R1 is cyclopentenyl or cyclohexenyl is prepared by treatment of where A is cyclopentylidene or cyclohexylidene with the compound Halogen-Y-N=B in the presence of a strong base. The resultant aminonitrile may be heated with a suspension of sodamide in an inert solvent to give an amine where the unsatisfied valencies of the carbon atom adjacent to the group R are satisfied by a cyclohexylidene group, a cyclopentylidene group, a cyclohexenyl group and hydrogen, or a cyclopentenyl group and hydrogen (the two different types of compound being tautomeric). The group -N=B may be dialkylamino or a cyclic amino group, e.g. morpholinyl, piperidinyl or pyrrolidinyl. Salts may be formed of the aminonitriles and the amines with acids or lower ...

Phenol esters of amino acids

Novel compounds of the general formula (wherein each of R1 and R2 represents an alkyl or alkoxy group or a halogen atom, each of R and R5 represents H or an alkyl or aryl group, and represents a heterocyclic group) are prepared by condensing an appropriate o,o1-disubstituted phenol with an a -halocarboxylic acid halide and condensing the resulting a -haloacyl ester with a secondary heterocyclic base. The products may be converted to non-toxic acid addition salts.ALSO:Local anaesthetic compositions, e.g. injectable solutions, sprays, ointments or pastes, contain, in association with a therapeutically acceptable solid or liquid carrier or diluent, one or more compounds of the general formula (wherein each of R1 and R2 represents an alkyl or alkoxy group or a halogen atom, each of R and R5 represents H or an alkyl or aryl group, and represents a heterocyclic group) or non-toxic acid addition salts thereof ...

NOVEL BEZ[e]INDENE AND PHENANTHRENE DERIVATIVES

... 1298219 Steroid precursors F HOFFMANNLA ROCHE & CO AG 20 Nov 1969 [22 Nov 1968] 28140/71 Divided out of 1298214 Heading C2C The invention comprises d, I and dl compounds of Formula I wherein m is 1 or 2; R1 is C 1-5 primary alkyl; R2 is lower alkyl; and Z4 is di- (lower alkoxy) -methylene, phenylenedioxymethylene, a methylene group substituted by a divalent -ORO-, -ORS-, -SRS- or -ORNH- group (where R is lower alkylene), or is a group of formula wherein R6 is H or lower aliphatic or alicyclic hydrocarbyl and R7 is H, lower alkyl, (lower alkoxy)-(lower alkyl), phenyl-(lower alkyl) or tetrahydropyran-2-yl. The term "lower" means having up to 8 carbon atoms. Compounds I are prepared from compounds II [wherein R2 and R3 are identical lower alkyl groups or one of R2 and R3 is H and the other is lower alkyl, and Z2 is as defined for Z4 above or is #- (lower acyloxy)- or -R6-methylene (where ...

Process for the manufacture of basic ethers of basic esters

Basic ether-basic esters are obtained by reacting a diphenyl N-substituted aminoalkoxy-acetic acid non-basic ester, wherein said phenyl groups may carry substituents inert to the reagents used, with an N-disubstituted-aminoalkyl alcohol under anhydrous or substantially anhydrous conditions in the presence of an alkaline agent, e.g. an alkali metal. The substituents on the N atoms of the initial materials may be alkyl, alkenyl or form part of a piperidino or morpholino radical. Detailed examples are given. Specification 610,198 is referred to.

Preparation of amide derivatives used as antagonists

A asymmetric synthesis is provided for preparing optically active amides of formula and their salts. In the formula X represents or R represents a mono or bicyclic aryl or heteroaryl group, Rü is an aryl or heteroaryl radical, Ré is H or lower alkyl, R* superscript dot; dot above * is H, C* three eighths *~ kyl, C* superscript dot; dot above * cloalkyl, cycloalkyl-alkyl, aryl or arylalkyl group, or Ré are Râ together with the nitrogen atom from a heterocyclic ring. The products are useful as 5-HT 1A antagonists. Novel diesters useful as intermediates in the process are also disclosed.

SULPHONE AND SULPHOXIDE INTERMEDIATES

... 1321867 Sulphones and sulphoxides WELLCOME FOUNDATION Ltd (Burroughs Wellcome & Co (USA) Inc) 29 May 1970 [16 May 1969] 25983/70 Divided out of 1261455 Heading C2C Novel compounds of Formulae I and II: (in which R1 is H or alkoxy when R2 is one or more substituents selected from halogen atoms and alkyl, amido and amino groups, or R1 is 2 or more alkoxy groups when R2 is H or is as defined above, and n is 1 or 2) are prepared by reacting a compound of Formula III: with a compound of formula CH 3 .SO n .CH 3 in the presence of a base sufficiently strong to provide the methylsulphinyl or methylsulphylon carbanion, to produce a compound I, and if desired reducing this to form a compound II. Compounds II react with #-substituted propionitriles of formula NC.CR 2 .CR 2 .Z (where Z is alkoxy, alkylthio or amino) to produce #-substituted--benzylacrylonitriles of Formula IV: which in turn react with guanidine to form 2,4 - diamino - 5 - (R1,R2 Подробнее

Tertiary (1-naphthyl)-alkylamines

Novel alkylamines of the general formula wherein R1 is a group of the formula -(CH2)2-N = R3 (wherein -N = R3 represents a saturated heterocyclic group which may contain a further hetero atom) and R2 represents any group represented by R1 or (when -N = R3 is a morpholino group) a hydrogen atom or an alkyl group containing at least 3 carbon atoms; and non-toxic acid addition salts thereof, are prepared by reacting a nitrile of the formula with an alkali metal amide or, when R2 is H, reducing an amide of the formula wherein -N = R3 is a morpholino group. Pharmaceutical compositions comprise as active ingredient a compound of the first general formula above and a pharmaceutical carrier or excipient. The compositions may be in solid or liquid form for oral administration or may be administered parenterally. The compositions are stated to have antiarrhythmic activity.

Unsaturated nitriles and esters and derivatives thereof

... 1,129,955. Substituted acetylenic-amines. JOHN WYETH & BROS. Ltd. 28 Feb., 1967 [3 March, 1966], No. 9319/66. Heading C2C. Novel compounds of Formula I and salts thereof wherein m is 0 or 1, Ar and Ar1 are each phenyl, naphthyl, or a phenyl radical substituted by an alkoxy, aralkoxy, halogen or alkyl radical, X is cyano or a carboxylic radical or a salt, ester or amide thereof, R1 is H or methyl, R2 and R3 are each C 1-4 alkyl or aralkyl or together with the nitrogen atom form a heterocyclic ring which may contain a further hetero atom and which may be substituted by a methyl or phenyl group, are prepared by reacting a nitrile or ester of Formula II with formaldehyde or paraformaldehyde and an amine HN.R2.R3and if desired hydrolysing the ester or nitrile so formed. Compounds of Formula II are prepared by reaction of a compound of Formula IV wherein M is an alkali metal, with a halide of formula Hal-CHR1-C#CH. Compounds of Formula ...

A PROCESS FOR THE MANUFACTURE OF 19-NORSTEROIDS

... 1298214 19-Norsteroid synthesis F HOFF. MANN-LA ROCHE & CO AG 20 Nov 1969 [22 Nov 1968] 56793/69 Headings C2C and C2U The invention comprises the preparation of d-, l- and dl-19-norsteroids of partial Formula (I) by three routes from d-, l- and dl-19-isoxazolyl-de-A-steroids of partial Formula (II) wherein R2 and R3 are identical C 1-8 alkyl groups or one of R2 and R3 is H and the other is C 1-8 alkyl, and R4 is H or a C 1-7 alkyl group having one CH 2 group less than R2 or R3. Route 1 comprises hydrogenation of (II) to yield a 4-azagon-2-ene of partial Formula (A) treatment of which with an anhydrous strong base yields a 4-azagona-2,5(10)-diene of partial Formula (D) hydrolysis of which yields a de-A-steroid of partial Formula (C) cyclization of which yields (I). The specific examples do not illustrate this route. Route 2 comprises hydrogenation of (II) to yield (A) as in route 1, treatment of (A) with an aqueous strong base ...

BENZYLPYRIMIDINES

a-aryl-a,a bis (w-disubstituted amino)alkyl-acetamides and related compoundss

A compound corresponding to the following general formula: wherein R<1> represents C1-C7 alkyl or C5 or C6 cycloalkyl; R<2> represents C1-C7 alkyl; or R<1> and R<2>, together with the nitrogen atom to which they are attached, complete on azamonocyclic ring which may contain at least one further heteroatom and which may be substituted once or twice by phenyl or C1-C4 alkyl; Ar represent pyridyl, trifluoromethylphenyl, biphenylyl, phenyl which may be substituted once or twice by halogen or C1-C4 alkyl, 1- or 2- naphthyl which may be substituted by halogen or C1-C4 alkyl, or C3-C6 cycloalkyl which may be substituted by C1-C4 alkyl or cyclohexyl; and Alk<1> and Alk<2> each independently represents C2-C4 alkylene; or a non- toxic pharmacologically acceptable acid addition salt thereof. Such compounds may be prepared by reacting an appropriate disubstituted acetonitrile with an appropriate haloalkylamine and subsequently hydrolyzing the resulting nitrile using concentrated sulphuric acid ...

METHOD FOR PREPARATION OF 4-SUBSTITUTED-3-ANILINO-5-PYRAZOLONES

... 1455967 4 - Substituted - 3 - arylamine- 5-pyrazolones FUJI PHOTO FILM CO Ltd 14 Jan 1975 [14 Jan 1974] 1636/75 Heading C2C [Also in Division G2] 4 - Substituted - 3 - arylamino - 5 - pyrazolone represented by the general Formula (I) wherein R1 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted aralkyl group or an optionally substituted aryl group; R2 represents one or two substituents selected from a hydrogen or halogen atom, and alkyl, alkoxy, alkylthio, alkylsulphonic acid, carbamido, acylamino, cyano, alkoxycarbonyl, sulphonamino, sulphamoyl, diacylamino, carbamoyl, carboxy, sulpho and nitro groups; and Y represents an alkylamino, dialkylamino, sulphonamino, acylamino, diacylamino, arylamino or diarylamino group, or a nitrogen-containing heterocyclic group bonded via the nitrogen atom in the heterocyclic ring or a releasable group bonded via an oxygen atom, some of which are novel, are prepared by conducting a ring-closing ...

N,n-disubstituted amides of aryl acetic acids

The invention comprises N : N-disubstituted arylacetic acid amides of the general formula R.CHR1.COR2 (wherein R is an aryl group, including halo- and alkyl-substituted aryl groups; R1 represents an alkyl, aralkyl, dialkylaminoalkyl, alkoxyalkyl, heterocyclic, alicyclic, heterocyclic alkyl, or arylalkyl carbamoyl methyl group; R2 represents dialkylamino, -N-morpholino-, piperidino-, pyrrolidino-, -N-(alkyl) aralkyl, or -N-(alkyl) aryl) and, when R1 contains an amine substituent, acid addition and quaternary salts thereof; also a process for the preparation of the amides by condensing in substantially equimolar proportions and in the presence of a strongly basic condensing agent an amide of formula RCH2COR2 with a compound R1Y, wherein Y is the residue of a strong acid such as hydrochloric, hydrobromic or p-toluene sulphonic acid; the amides may then be converted to their acid addition salts or quaternary salts with alkyl esters of which the alkyl group contains at most six carbon atoms.

Improvements in and relating to diquaternary compounds and the manufacture thereof

The invention comprises diquaternary compounds of the general formula wherein R1 and R2 are the same or different and are each a cycloalkyl group or a phenyl group which may optionally be substituted by one or more halogen, lower alkyl or lower alkoxy substituents ; X is (CH2)n or (CH2)2.O.(CH2)2, n being an integer from 2 to 10 ; N+1 is a quaternary nitrogen atom carrying two alkyl groups having together up to 5 carbon atoms, preferably 2 or 3 carbon atoms, or which together form part of a pyrrolidino, piperidino or morpholino ring; N+2 is a quaternary nitrogen atom carrying at least one alkyl group of 1 to 4 carbon atoms and either two further alkyl groups of a total of up to 9 carbon atoms, preferably 3 to 6 carbon atoms, or forming part of a pyrrolidino piperidino or morpholino ring ; Y is an alkylene chain of 2 to 10, preferably 2 to 6, carbon atoms, or N+1-Y-N+2 is a piperazine ring in which N+1 is a quaternary nitrogen atom carrying an alkyl group of up to ...

2,4-DIAMINO-5-BENZYLPYRIMIDINES AND A PROCESS FOR THEIR PREPARATION

NOVEL BEZ[e]INDENE AND PHENANTHRENE DERIVATIVES

... 1298218 Steroid precursors F HOFFMANNLA ROCHE & CO AG 20 Nov 1969 [22 Nov 1968] 28139/71 Divided out of 1298214 Heading C2C The invention comprises d, I and dl compounds of Formulµ Ia and Ib wherein m is 1 or 2; R1 is C 1-5 primary alkyl; R2 and R3 are identical lower alkyl groups or one of R2 and R3 is H and the other is lower alkyl; Z1 is carbonyl, (lower alkylenedioxy)- methylene, di - (lower alkoxy) - methylene, phenylenedioxy-methylene or a group of formula where R5 is H, lower alkyl, (lower alkoxy)- (lower alkyl), phenyl-(lower alkyl), tetrahydropyran-2-yl or lower acyl and R6 is H or lower aliphatic or alicyclic hydrocarbyl; and Z2 is di- (lower alkoxy) - methylene, phenylenedioxymethylene, a methylene group substituted by a divalent -ORO-, -ORS-, -SRS- or -ORNH- group (where R is lower alkylene), or is a group of Formula III defined above. The term " lower" means having up to 8 carbon atoms. Compounds ...

... 1452413 N-(-Cyanobenzyl) piperazines and homopiperazines FUJI CHEMICAL INDUSTRY CO Ltd and NIPPON CHEMIPHAR CO Ltd 25 July 1974 [18 Aug 1973 (2) 16 July 1974 (3) 16 Aug 1973] 32888/74 Heading C2C The invention comprises compounds of general formula and acid additive salts thereof, where R 1 is halogen or lower alkoxy, R 2 and R 3 are hydrogen or lower alkoxy, R 4 is hydrogen or lower alkyl, R 5 is hydrogen, -COOR 6 (R 6 is lower alkyl) (R 7 is lower alkoxy and m is 0, 1, 2 or 3), -R 8 COOR 9 (R 8 is lower alkylene and R 9 is lower alkyl) -CH 2 CONR 10 R 11 (R 10 and R 11 are hydrogen or lower alkyl or jointly form an alkylene group) or where n is 2 or 3; "lower" here means containing up to 3 carbon atoms. These compounds are prepared (a) by reacting an aromatic aldehyde or ketones of formula with a piperazine or homopiperazine of formula or an acid addition salt thereof, in the presence of hydrogen cyanide or a salt thereof, or (b) by reacting a compound of formula or an acid addition salt ...

“1-arylpyrroles pesticides and processes for their preparation and their use”.

New agents pesticides and in particular mollusquicides.

PROCEDURE FOR THE PRODUCTION OF NEW HYDRAULIC XY AETHYLIDEN CYANESSIGSAEURE ANILIDEN AS WELL AS OF THEIR PHYSIOLOGICAL COMPATIBLE ONE SALTS

PROCEDURE FOR the PRODUCTION of NEW 3-ARYL-2 PIPERAZINYL PROPIONSAEUREN AND THEIR SALTS

PROCEDURE FOR THE PRODUCTION OF NEW SYMMETRICAL ALPHA ARYL ALPHA, ALPHA DI (OMEGA (DIISOPROPYLAMINO) ALKYL) ACETAMIDE

LYMPHOZYTEN FUNCTION ANTIGEN-1 ANTAGONISTS

PROCEDURE FOR the PRODUCTION OF NEW ONE 1,4-DIPHENYLPYRAZOLDERIVATEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN PHENOXYPROPYLAMINDERIVATEN UND DEREN SALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN 2,4-DIAMINO -5-THIOPBENZYLPYRIMIDINEN UND IHREN SAEURE- ADDITIONSSALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN SUBSTI- TUIERTEN 6-PHENYL-1,2,4-TRIAZOLO-(4,3-B)PYRI- DAZINEN UND DEREN SALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN ALPHA-ARYL-ALPHA,ALPHA-BIS-(OMEGA(DISUBSTITUIER - AMINO)-ALKYL)ACETAMIDEN

PROCEDURE FOR THE PRODUCTION OF NEW ALPHA ARYL ALPHA, ALPHA-BIS (OMEGA (OF DISUBSTITUIERTES AMINO) ALKYL) ACETAMIDEN

PROCEDURES FOR the PRODUCTION OF NEW SUBSTI TUIERTEN 6-PHENYL-1,2,4-TRIAZOLO (4,3-B) PYRI DAZINEN AND THEIR SALTS

PROCEDURE FOR the PRODUCTION OF NEW SUBSTITUTED N-ECYL-n '' - (3-AMINO-2-CYANO-ACRYLOYL) - FORMAMIDRAZONEN AND THEIR TAUTOMEREN AND SALTING

ARYLCYCLOBUTYLALKYLAMINE AND YOUR USE AS ANTI-DEPRESSIVE DRUGS.

UNTIL (PIPERAZINYL AND/OR HOMOPIPERAZINYL) - ALKANES.

USE OF BENZOYLALANINEN AS CORROSION INHIBITORS FOR WAESSRIGE SYSTEMS.

TERTIARY ALKYL FUNKTIONALISIERTE PIPERAZIN DERIVATIVES

Procedure for the production of new Isoxazolderivate

LHRH ANTAGONIST AND INTERMEDIATE PRODUCTS

MUSCARIN ANTAGONIST

PESTICIDES 1-ARYLPYRROLE

ARYL GLYCINE AMIDE DERIVATIVES, PROCEDURES FOR YOUR PRODUCTION AND THESE CONNECTIONS ABSTENTION PHARMACEUTICAL COMPOSITIONS

Procedure for the production of new Isoxazolderivate

Procedure for the production of new Isoxazolderivate

Procedure for the production of new Isoxazolderivaten, their Ketalen and salts

PIPERAZINE DERIVATIVES

TRI(LOWER ALKOXY)BENZENE DERIVATIVE

4-(diarylmethyl)-1-piperazinyl derivatives

Lymphocyte function antigen-1 antagonists

PYRAZOLE DERIVATIVES

LHRH ANTAGONISTS AND INTERMEDIATE PRODUCTS

ARYLCYCLOBUTYLALKYLAMINES

PROCESS FOR THE PREPARATION OF BENZINDENES

NAPHTALENIC AMINOALKYL DERIVATIVES, THE ACID ADDITION SALTS THEREOF AND THE PROCESS FOR PREPARING SAME, AS WELL AS THE APPLICATION IN THERAPEUTICS OF THESE DERIVATIVES AND SALTS

HYPOTENSIVE AGENTS

This disclosure describes novel phenyl and substituted 6-phenyl-1,2,4-triazolo¢4,3-b!pyridazines and processes for thier preparation of formula I wherein R1, R2, and R3 are each individually selected from the group consisting of hydrogen and alkyl of up to 3 carbon atoms, and R4 is hydrogen or one or more groups which may be the same or different chosen from fluoro, chloro, bromo, cyano, trifluoromethyl, nitro, amino, acetamido, carbamoyl, thiocarbamoyl, or alkyl of up to 4 carbon atoms, provided that (a) at least one of R1 and R2 is hydrogen;(b) when R1, R2 and R4 are all hydrogen, then R3 is other than methyl; and(c) when R2 and R3 are both methyl, then both R1 and R4 are other than hydrogen. These compounds find use as hypotensive agents and anxiolytic agents.

2,5-PYRROLIDINEDIONE DERIVATIVES USEFUL AS ANTIARRHYTHMIC AGENTS

2,4-DIAMINO-5-BENZYLPYRIMIDINES AND PROCESS FOR THE MANUFACTURE THEREOF

PHOTOGRAPHIC ELEMENT HAVING 1-AMINO-4-CYANO-1,3-BUTADIENE DERIVATIVE AS ULTRAVIOLET FILTER

4-(DIARYLMETHYL)-1-PIPERAZINYL DERIVATIVES

A compound of formula (I) wherein X, Y, X' & Y' are selected from hydrogen, halogen, substituted or unsubstituted alkyl (linear, branched or cyclo), aryl, alkyloxy and haloalkyl group; R1, R2, R3 & R4 are selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz., N, S, O), substituted or unsubstituted alkenyl or alkynyl groups of carbon 2 to 6, wherein the substituents R1 & R2 on the piperazinyl moiety are either syn or anti to each other and optionally R3 and R4 together with the carbons to which they are attached form a monocyclic saturated or aryl or substituted aryl or heteroaryl or substituted heteroaryl ring containing one or more hetero atoms selected from N, S and O with a ring size ranging from 3 to 6; with a proviso that when R3 & R4 together do not form part of a ring they may exist in either E or Z configuration;R5 is (CH2)n-O- CH2-CO-Z wherein ...

LHRH ANTAGONISTS AND INTERMEDIATE PRODUCTS

The invention concerns LHRH antagonists of the general formula (I), in which X is an acyl group, X1 is a D-Nal, X2 is D-(4-C1)-Phe, X3 is D-(3)-Pal, X6 is D-Cit or D-Neu, X8 is L-Arg or L-Neu, at least one of the groups X6 and X8 being a Neu, and X10 is D-Ala-NH2, Neu being a group formulae (II), (III) or (IV), wherein W is one of the group (a), (b), (c), or (d). The invention includes drugs containing a compound of formula (I), plus the usual auxiliaries and carriers. These drugs are suitable for use in cases of carcinoma of the prostate and in endometriosis, as well as for fertility control.

A PROCESS FOR THE RESOLUTION OF (+-)-.ALPHA.-[2-[ACETYL(1-METHYLETHYL)AMINO]ETHYL]-.ALPHA.-(2-CHLOROPHENYL)-1-PIPERIDINEBUTANAMIDE

2122584 9313087 PCTABS00024 A process for the resolution of (+-)-.alpha.-[2-[acetyl(1-methylethyl)amino]ethyl]-.alpha.-(2-chlorophenyl)-1_ -piperidinebutanamide having structure (I) into its (+) and (-) enantiomers using camphorsulfonic acid.

BENZOYLETHYLENE DERIVATIVE

A benzoylethylene derivative represented by general formula (I) and a salt thereof wherein R1 to R5 represent each hydrogen, -OR9 (R9 being hydrogen, C1C5 alkyl, etc.), etc.; R6 represents hydrogen, C1-C5 alkyl, etc.; R7 represents hydrogen, cyano, C1-C5 alkyl, -SOqR15 (q being 0, 1 or 2, and R15 being thienyl, phenyl, etc.), etc.; and R8 represents cyano, -CR22R23X (R22 and R23 being each hydrogen, C1-C5 alkyl, etc., and X being -NR24R25 (wherein R24 and R25 represent each C1-C5 alkyl, or R24 and R25 are combined together to represent alkylene, etc.)), etc. The derivative has potent activities of tyrosine kinase inhibition and cancer cell growth inhibition and is useful as a carcinostatic agent.

PIPERIDINE DERIVATIVES AS NEUROKININ ANTAGONISTS

The invention relates to compounds of formula (I), wherein X, i, j, n, n', A, A', R2, R3, and U are as decribed herein. The compounds of the invention are NK1 or NK2 or NK3 receptor antagonists and as such are useful in the treatment of diseases such as asthma.

PIPERIDINE AND PIPERAZINE DERIVATIVES AND THEIR USE AS MUSCARINIC ANTAGONISTS

Di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R22, R28, X, Y and Z a s defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.

Verfahren zur Darstellung von Diphenyl-piperidinoäthyl-essigsäureäthylester.

Verfahren zur Herstellung von Diphenyl-piperidinoäthyl-essigsäuremethylester.

Procédé de fabrication de N-benzhydryl-N'-benzylpipérazines

Verfahren zur Herstellung von Diphenyl-piperidinoäthyl-essigsäureisopropylester.

Verfahren zur Herstellung eines basischen Säureamides.

Verfahren zur Herstellung von Diphenyl-morpholinoäthyl-essigsäureäthylester.

Verfahren zur Herstellung von Diphenyl-morpholinoäthyl-essigsäuremethylester.

Verfahren zur Herstellung von N-monosubstituierten Amiden vona-Aminoalkyl-a-phenyl-essigsäuren

Verfahren zur Herstellung quaternärer Aminoalkylester organischer Säuren

Verfahren zur Herstellung eines haltbaren Thrombinpräparates von gesteigerter Wirksamkeit.

Verfahren zur Herstellung des Brommethylats des Diphenyl-(2-piperidyl-(1')-äthyl)-acetamids.

Verfahren zur Herstellung eines quaternären Ammoniumsalzes

Procédé de fabrication d'acides carboxyliques

Verfahren zur Herstellung substituierter Butyramide

Procédé de préparation de dérivés d'ammonium biquaternaires

Verfahren zur Herstellung von Aminoalkyl-1-naphthylacetamiden

Procédé de préparation de nouveaux anesthésiques

PROCEDURE FOR the PRODUCTION OF 2,4-DIAMINO-5-BENZYLPYRIMIDINEN.

1-p-benzoyl-2-methyl-3-indolyl acetic acid derivs

... (A) Improved method for R = NeO or Me2N. (B) The intermediates II and IV (and possibly V-VIII inc.).

Verfahren zur Herstellung von Derivaten des a-Piperazino-phenylacetonitrils

Verfahren zur Herstellung von Benzodiazepin-Derivaten

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. 146.-. (canceled)47. A compound selected fromtert-butyl 4-[(4-{[(6-methyl-3-pyridyl)amino]carbonylamino}benzoxazol-2-yl) methyl]piperazinecarboxylate;methyl 4-[(4-{[(6-methyl-3-pyridyl)amino]carbonylamino}benzoxazol-2-yl) methyl]piperazinecarboxylate;N-{2-[(4-acetylpiperazinyl)methyl]benzoxazol-4-yl}[(6-methyl(3-pyridyl))amino]carboxamide;N-(2-{[4-(N,N-dimethylcarbamoyl)piperazinyl]methyl}benzoxazol-4-yl)[(6-methyl(3-pyridyl))amino]carboxamide;[(6-methyl(3-pyridyl))amino]-N-(2-{[4-(methylsulfonyl)piperazinyl]methyl}benzoxazol-4-yl)carboxamide;N-(2-{[4-(azetidinylsulfonyl)piperazinyl]methyl}benzoxazol-4-yl)[(6-methyl(3-pyridyl))amino]carboxamide;N-(2-{[4-(ethylsulfonyl)piperazinyl]methyl}benzoxazol-4-yl)[(6-methyl(3-pyridyl))amino]carboxamide;[(6-methyl(3-pyridyl))amino]-N-[2-({4-[(methylethyl)sulfonyl]piperazinyl}methyl)benzoxazol-4-yl]carboxamide;N-(2-{[4-(cyclopropylsulfonyl)piperazinyl]methyl}benzoxazol-4-yl)[(6-methyl(3-pyridyl))amino]carboxamide;N-(2-{[4-(azetidinylcarbonyl)piperazinyl]methyl}benzoxazol-4-yl)[(6-methyl(3-pyridyl))amino]carboxamide;[(6-methyl(3-pyridyl))amino]-N-(2-{[4-(morpholin-4-ylcarbonyl)piperazinyl]methyl}benzoxazol-4-yl)carboxamide;[(6-methyl(3-pyridyl))amino]-N-[2-({4-[(4-methylpiperazinyl)carbonyl]piperazinyl}methyl)benzoxazol-4-yl]carboxamide;[(6-methyl(3-pyridyl))amino]-N-(2-{[4-(pyrrolidinylcarbonyl)piperazinyl]methyl}benzoxazol-4-yl)carboxamide;[(6-methyl(3-pyridyl))amino]-N-(2-{[4-(piperidylcarbonyl)piperazinyl]methyl}benzoxazol-4-yl)carboxamide;N-[2-({4-[(1,1-dioxo(1,4-thiazaperhydroin-4-yl))carbonyl]piperazinyl}methyl)benzoxazol-4-yl][(6-methyl(3-pyridyl))amino]carboxamide;N-[2-({4-[(4-acetylpiperazinyl)carbonyl]piperazinyl}methyl)benzoxazol-4-yl][(6-methyl(3-pyridyl))amino]carboxamide; and1-(6-methylpyridin-3-yl)- ...

ISOPRENYL COMPOUNDS AND METHODS THEREOF

Among other things, the present invention provides novel isoprenyl compounds capable of effectively modulating inflammatory responses and pharmaceutical, cosmetic, cosmeceutical and topical compositions comprising these isoprenyl compounds. Anti-inflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with inflammation. Proinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with suppression of inflammatory responses. Thus, the present invention also provides methods useful in the treatment or prevention of diseases or conditions associated with inflammation as well as methods useful in the treatment or prevention of diseases or conditions associated with suppression of inflammatory responses. 2. (canceled)3. The compound according to claim 1 , wherein L is selected from a bivalent claim 1 , branched or unbranched claim 1 , saturated or unsaturated claim 1 , Chydrocarbon chain wherein one or more methylene units of L is independently replaced by —NH— claim 1 , —C(O)— claim 1 , —CH═CH— claim 1 , C-Ccycloalkylene claim 1 , C-Cheterocycloalkylene claim 1 , 8-10-membered bicyclic heterocyclic moiety claim 1 , an optionally substituted arylene and optionally substituted heteroarylene claim 1 , and wherein L is optionally substituted by one or more groups selected from halogen claim 1 , substituted or unsubstituted C-Calkyl claim 1 , and —NHC(O)CH.5. The compound according to claim 1 , wherein L is selected from a bivalent claim 1 , branched or unbranched claim 1 , saturated or unsaturated claim 1 , Chydrocarbon chain wherein one or more methylene units of L is independently replaced by —NH— claim 1 , —C(O)— claim 1 , —C(═CH)— claim 1 , —CH═CH— claim 1 , C-Ccycloalkylene claim 1 , 8-10-membered bicyclic heterocyclic moiety claim 1 , an optionally substituted arylene and optionally substituted heteroarylene claim 1 , and wherein L is optionally ...

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 114-. (canceled)16. The compound of claim 15 , wherein Chelator is a radical of:1,4,7,10-tetraazacyclododecane-N,N′,N″,N′″-tetraacetic acid (DOTA);N,N″-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N″-diacetic acid (HBED-CC);1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA);2-(4,7-bis(carboxymethyl)-1,4,7-triazonan-1-yl)pentanedioic acid (NODAGA);2-(4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)pentanedioic acid (DOTAGA);1,4,7-triazacyclononane phosphinic acid (TRAP);1,4,7-triazacyclononane-1-[methyl(2-carboxyethyl)phosphinic acid]-4,7-bis[methyl(2-hydroxymethyl)phosphinic acid] (NOPO);3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene-3,6,9-triacetic acid (PCTA);N′-{5-[Acetyl(hydroxy)amino]pentyl}-N-[5-({4-[(5-aminopentyl)(hydroxy)amino]-4-oxobutanoyl}amino)pentyl]-N-hydroxysuccinamide (DFO);diethylenetriaminepentaacetic acid (DTPA);trans-cyclohexyl-diethylenetriaminepentaacetic acid (CHX-DTPA);1-oxa-4,7,10-triazacyclododecane-4,7,10-triacetic acid (oxo-Do3A);p-isothiocyanatobenzyl-DTPA (SCN-Bz-DTPA);1-(p-isothiocyanatobenzyI)-3-methyl-DTPA (1B3M);2-(p-isothiocyanatobenzyI)-4-methyl-DTPA (1M3B); or1-(2)-methyl-4-isocyanatobenzyl-DTPA (MX-DTPA).18. A radiolabeled compound of .19. A radiolabeled compound of .20. A metal complex comprising a radionuclide and a compound of .21. The metal complex of claim 20 , wherein the radionuclide is selected from Zr claim 20 , Sc claim 20 , In claim 20 , Y claim 20 , Ga claim 20 , Lu claim 20 , Tc claim 20 , Cu claim 20 , Cu claim 20 , Gd claim 20 , Gd claim 20 , Gd claim 20 , Bi claim 20 , or Ac.22. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable ...

BIS(PHOSPHINE)-CARBODICARBENE CATALYST COMPLEXES AND METHODS OF USING THE SAME

An organometallic complex of a tridentate bis(phosphine)-carbodicarbene ligand and a transition metal, is described. In some embodiments the ligand has the structure of Formula (I): The complexes are useful in methods of making an allylic amine carried out by reacting a 1,3-diene with a substituted amine in the presence of such an organometallic complex to produce by intermolecular hydroamination the allylic amine. 1. An organometallic complex , comprising:(a) a tridentate bis(phosphine)-carbodicarbene ligand, and(b) a transition metal.4. The complex of claim 1 , wherein said transition metal is selected from the group consisting of ruthenium claim 1 , nickel claim 1 , palladium claim 1 , platinum claim 1 , rhodium claim 1 , iridium claim 1 , cobalt claim 1 , iron claim 1 , silver claim 1 , gold claim 1 , and molybdenum.5. The complex of claim 2 , wherein R claim 2 , R claim 2 , R claim 2 , and Rare each independently selected alkyl or aryl.6. The complex of claim 2 , wherein at least one R′ is S-L- claim 2 , where S is a solid support and L is a linking group.7. The complex of claim 2 , wherein each R′ is independently hydrogen claim 2 , halo claim 2 , loweralkyl claim 2 , loweralkoxy claim 2 , or hydroxyl.8. A reaction mixture comprising an organometallic complex of claim 1 , a solvent claim 1 , a 1-3 claim 1 , diene substrate claim 1 , and a substituted amine substrate.11. A method of making an allylic amine claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'reacting a 1,3-diene with a substituted amine in the presence of an organometallic complex of in a catalytic amount to produce by intermolecular hydroamination said allylic amine.'}14. A tridentate bis(phosphine)-carbodicarbene pincer ligand. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/979,749, filed Apr. 15, 2014, the disclosure of which is incorporated by reference herein in its entirety.The present invention concerns carbodicarbene ligands, ...

CRYSTALLINE FORMS OF NEUROTROPHIN MIMETIC COMPOUNDS AND THEIR SALTS

The present invention includes crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and crystalline forms of salts and/or solvates of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms. 166.-. (canceled)67. A sulfuric acid addition salt of (2S ,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide made by the process of contacting a solution of (2S ,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide in a solvent with sulfuric acid in a mole ratio of about 0.75:1 or more of sulfuric acid to (2S ,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and separating the sulfuric acid addition salt of (2S ,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide formed from said solvent.68. The sulfuric acid addition salt of claim 67 , wherein said sulfuric acid addition salt exhibits an X-ray powder diffraction pattern under Cu—K-α radiation comprising peaks at 21.784±0.5; 22.468±0.5; and 19.277±0.5 degrees two-theta claim 67 , optionally further comprising peaks at 24.618±0.5 and 15.499±0.5 degrees two-theta.69. The sulfuric addition salt of claim 67 , wherein said sulfuric acid addition salt of (2S claim 67 ,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide exhibits a Raman spectrum comprising peaks at 2980±10; 2943±10; 2889±10; and 1033±10 cm claim 67 , optionally further comprising peaks at 975±10 and 851±10 cm.70. The sulfuric acid addition salt of claim 67 , wherein the mole ratio of sulfuric acid to (2S claim 67 ,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide is about 2:1.71. The sulfuric acid addition salt of claim 67 , wherein the solvent comprises an alcohol.72. The sulfuric acid addition salt of claim 67 , wherein the solvent comprises ethanol.73. The sulfuric acid addition salt of claim 67 , wherein the solution of (2S claim 67 ,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide in a ...

CRYSTALLINE FORMS OF NEUROTROPHIN MIMETIC COMPOUNDS AND THEIR SALTS

The present invention includes crystalline forms of (2S,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and salts thereof. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic uses of the crystalline forms. 1. A crystalline form of (2S ,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide tetra(monohydrogensulfate) , monosulfate that exhibits an X-ray powder diffraction pattern comprising peaks at about 8.01±0.3; 9.85±0.3; 21.30±0.3; and 21.99±0.3 degrees two-theta.2. The crystalline form of claim 1 , wherein the X-ray powder diffraction pattern further comprises peaks at about 15.01±0.3; 18.06±0.3; 18.88±0.3; 24.27±0.3 and 15.499±0.3 degrees two-theta.3. A pharmaceutical composition comprising a crystalline form of .4. A method for treating a disorder involving degeneration or dysfunction of cells expressing p75 comprising administering to a patient in need of such treatment a therapeutically effective amount of a pharmaceutical composition of .5. The method of claim 4 , wherein the disorder is a neurodegenerative disorder.6. The method of claim 4 , wherein the disorder is selected from the group consisting of Alzheimer's disease claim 4 , Huntington's disease claim 4 , Pick's disease claim 4 , amyotrophic lateral sclerosis claim 4 , epilepsy claim 4 , Parkinson's disease claim 4 , spinal cord injury claim 4 , stroke claim 4 , hypoxia claim 4 , ischemia claim 4 , brain injury claim 4 , diabetic neuropathy claim 4 , peripheral neuropathy claim 4 , nerve transplantation claim 4 , multiple sclerosis claim 4 , peripheral nerve injury claim 4 , and hair loss.7. A pharmaceutical composition comprising a crystalline form of . The present application is a continuation-in-part of U.S. application Ser. No. 15/682,389, entitled “CRYSTALLINE FORMS OF NEUROTROPHIN MIMETIC COMPOUNDS AND THEIR SALTS,” filed Aug. 21, 2017 which is a continuation of U.S. application Ser. No. 14/972,506, entitled “CRYSTALLINE FORMS OF ...

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 114-. (canceled)16. The compound of claim 15 , wherein the compound is lyophilized.17. The compound of claim 15 , further comprising a pharmaceutically acceptable carrier claim 15 , wherein the compound and the pharmaceutically acceptable carrier are lyophilized.18. The compound of claim 17 , wherein the pharmaceutically acceptable carrier is selected from mannitol claim 17 , lactose claim 17 , glucose claim 17 , and albumin.21. The compound of claim 20 , wherein the radionuclide is chosen from Zr claim 20 , Sc claim 20 , In claim 20 , Y claim 20 , Ga claim 20 , Lu claim 20 , Tc claim 20 , Cu claim 20 , Cu claim 20 , Gd claim 20 , Gd claim 20 , Gd claim 20 , Bi claim 20 , or Ac.22. The compound of claim 20 , wherein the radionuclide is chosen from Cu claim 20 , Cu claim 20 , Ga claim 20 , Lu claim 20 , or Ac.23. The compound of claim 20 , wherein the radionuclide is Ga.24. The compound of claim 20 , wherein the radionuclide is Lu.25. The compound of claim 20 , wherein the radionuclide is Ac.26. The compound of claim 20 , wherein the radionuclide is chosen from Cu or Cu.27. The compound of claim 21 , wherein the radionuclide is chosen from Cu claim 21 , Cu claim 21 , Ga claim 21 , Lu claim 21 , or Ac.28. The compound of claim 21 , wherein the radionuclide is Ga.29. The compound of claim 21 , wherein the radionuclide is Lu.30. The compound of claim 21 , wherein the radionuclide is Ac.31. The compound of claim 21 , wherein the radionuclide is chosen from Cu or Cu.33. The composition of claim 32 , wherein the radionuclide is chosen from Zr claim 32 , Sc claim 32 , In claim 32 , Y claim 32 , Ga claim 32 , Lu claim 32 , Tc claim 32 , Cu claim 32 , Cu claim 32 , Gd ...

TREPROSTINIL DERIVATIVE COMPOUNDS AND METHODS OF USING SAME

Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used. 181-. (canceled)83. The compound of claim 82 , wherein Ris Pand Ris H.84. The compound of claim 82 , wherein Ris H and Ris P.85. The compound of claim 82 , wherein Ris Pand Ris P.88. The compound of claim 82 , wherein each of Rto Ris H.89. The compound of claim 82 , wherein at least one of Rto Ris deuterium.90. The compound of claim 82 , wherein Z is —OH claim 82 , —OR claim 82 , —N(R)Ror P.91. The compound of claim 82 , wherein Z is P.92. The compound of claim 82 , wherein Z is —OH.93. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers or excipients.94. The pharmaceutical composition of claim 93 , which is formulated for transdermal delivery claim 93 , optionally via a patch.95. A method of treating pulmonary hypertension claim 82 , comprising administering to a subject in need of treatment a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof.96. The method of claim 95 , wherein the pulmonary hypertension is pulmonary arterial hypertension.97. The method of claim 95 , wherein the compound is administered orally claim 95 , topically or parenterally.98. The method of claim 97 , wherein the compound is administered transdermally claim 97 , optionally via a patch.99. The method of claim 95 , further comprising administering an additional therapeutic agent.100. The method of claim 99 , wherein the additional therapeutic agent is selected from the group consisting of vasoactive agents claim 99 , diuretics claim 99 , anticoagulants and cardiac glycosides. This application is ...

MEROCYANINE DERIVATIVES

Disclosed are compounds of formula (1) and (2) and/or E/E-, E/Z- or Z/Z geometrical isomer forms thereof; wherein R1-R5, R1-R11 and A are defined as in description. The compounds are used as UV absorbers for protecting household products from photolytic and oxidative degradation, as plastic additives, preferably for food and pharmaceutical packaging applications, for preventing photo-degradation of food by incorporation of the compounds of formula (1′) and/or (2′) into transparent food containers, for protection of UV-A sensitive drugs from photo-degradation by incorporation of UV absorber in transparent blister foils or transparent pharmacy containers, as additives for photographic and printing applications, as additives for electronic applications and protecting the ingredients in agriculture applications. 4. Compounds of formula (1) according to claim 1 , wherein Ris C-Calkyl claim 1 , which is optionally substituted by one or more than one hydroxy.5. Compounds of formula (1) according to claim 1 , wherein{'sub': 6', '1', '12, 'Ris C-Calkyl which is substituted by one or more than one hydroxy;'}{'sub': 1', '2', '4', '22', '1', '2', '2', 'n, 'one of Rand Ris C-Calkyl; or Rand Rtogether with the nitrogen atom linking them form a —(CH)— ring which is optionally interrupted by —O— and/or —NH—; and'}{'sub': 4', '5, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'Rand Rand n are defined as in .'}6. Compounds of formula (2) according to claim 1 , wherein{'sub': 11', '2', 'm', '12, 'Ris a radical of formula (1a) —(CH)—R, wherein'}{'sub': 12', '1', '12', '1', '6', '1', '6, 'Ris C-Calkyl; or C-Calkoxy-C-Calkyl;'}m is a number from 1 to 5; and{'sub': 7', '8', '9', '10, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'R, R, R, Rand A are defined as in .'}7. Compounds according to claim 1 , wherein in formulas (1) and (2){'sub': 1', '2', '7', '8, 'Rand Rand Rand Rrespectively together with the linking nitrogen atom form a piperidyl radical or a morpholinyl radical.'}8. ...

Indole derivatives and their use as protein kinase inhibitors

The present invention relates inter alia to a compound of formula (I) wherein R 1 , R 2 and R 3 , are as defined in the specification and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of fibrotic diseases or interstitial lung diseases, in particular idiopathic pulmonary fibrosis.

TREPROSTINIL DERIVATIVE COMPOUNDS AND METHODS OF USING SAME

Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used. 147-. (canceled)49. The compound of claim 48 , wherein R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , and Rare H.50. The compound of claim 48 , wherein at least one of R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , R claim 48 , and Rare is deuterium.51. The compound of claim 48 , wherein Lis —O-alkylene-C(O)—.52. The compound of claim 48 , wherein Lis —O-alkylene-OC(O)—.53. The compound of claim 48 , wherein Lis a bond.54. The compound of claim 48 , wherein the alkylene group is a C-Calkylene group.55. The compound of claim 48 , wherein the alkylene group is a Calkylene group.56. (canceled)5863-. (canceled)66. A composition comprising a compound of claim 48 , or and one or more pharmaceutically acceptable excipients.67. The composition of claim 66 , which is formulated for transdermal delivery.6870-. (canceled)71. A method of treating pulmonary hypertension claim 66 , comprising administering to a subject in need of treatment a therapeutically effective amount of a compound of claim 66 , or or a pharmaceutically acceptable salt thereof.72. The method of claim 71 , wherein the pulmonary hypertension is pulmonary arterial hypertension.73. The method of claim 71 , wherein the compound is administered transdermally. This application claims priority to U.S. provisional application 61/751,608 filed Jan. 11, 2013 ...

Deuterium Substituted Fumarate Derivatives

Provided is a compound of formula (I): 2. The compound of claim 1 , wherein Ris hydrogen or —CH.3. The compound of claim 2 , wherein Ris —CHD claim 2 , —CHD claim 2 , or —CD.4. The compound of claim 1 , wherein Ris —CD3.5. The compound of claim 4 , wherein Ris —CHD claim 4 , —CHD claim 4 , or —CD3.6. (canceled)7. The compound of claim 1 , wherein both of Rand Rare deuterium.8. The compound of claim 1 , wherein Ris hydrogen or —CH claim 1 , —CHD claim 1 , —CHD claim 1 , or —CD.9. (canceled)10. (canceled)11. A compound of formula (I) wherein the compound is (H)dimethyl fumaric acid ester claim 1 , (H)methyl fumaric acid ester claim 1 , (H)dimethyl fumaric acid ester claim 1 , dimethyl fumaric(2 claim 1 ,3-H) acid ester claim 1 , methyl fumaric(2 claim 1 ,3-H) acid ester claim 1 , ethyl fumaric(2 claim 1 ,3-H) acid ester claim 1 , (H)methyl fumaric(2 claim 1 ,3-H) acid ester claim 1 , (H)dimethyl fumaric(2 claim 1 ,3-H) acid ester claim 1 , methyl (2-morpholino-2-oxoethyl) fumaric(2 claim 1 ,3-H) acid ester claim 1 , methyl (4-morpholino-1-butyl) fumaric(2 claim 1 ,3-H) acid ester claim 1 , 2-(benzoyloxy)ethyl methyl fumaric(2 claim 1 ,3-H) acid ester claim 1 , 2-(benzoyloxy)ethyl (H)methyl fumaric acid ester claim 1 , (S)-2-((2-amino-3-phenylpropanoyl)oxy)ethyl methyl fumaric(2 claim 1 ,3-H) acid ester claim 1 , or (S)-2-((2-amino-3-phenylpropanoyl)oxy)ethyl (H)methyl fumaric acid ester.12. A method of activating the Nrf2 pathway claim 1 , comprising contacting cells with a sufficient amount of a compound of .13. A method of treating claim 1 , prophylaxis claim 1 , or amelioration of one or more neurodegenerative diseases claim 1 , comprising administering to a subject claim 1 , in need of treatment for the neurodegenerative disease an effective amount of a compound of .14. The method of claim 13 , wherein the neurodegenerative disease is one or more diseases selected from the group consisting of Multiple Sclerosis claim 13 , Amyotrophic Lateral Sclerosis claim 13 , ...

Phenyl-Piperazine Derivatives As Serotonin Reuptake Inhibitors

The invention provides compounds represented by the general formula I 2. The compound according to claim 1 , provided that the compound is not 1-(2-phenoxyphenyl)piperazine.3. The compound according to claim 1 , provided that the compound is not 1-[2-(2-Methoxyphenoxy)phenyl]piperazine claim 1 , 1-[2-(2 claim 1 ,6-dimethoxyphenoxy)phenyl]-[1 claim 1 ,4]-diazepane claim 1 , 1-{2-[3-(dimethylamino)phenoxy]phenyl}piperazine claim 1 , 1-[2-(4-methylphenoxy)phenyl]piperazine claim 1 , 1-[2-(3-methylphenoxy)phenyl]piperazine claim 1 , 1-[2-(3-chlorophenoxy)phenyl]piperazine claim 1 , 1-[2-(3-methoxyphenoxy)phenyl]piperazine and 1-(2-phenoxyphenyl)-piperazine.4. The compound according to claim 1 , wherein p is 0 claim 1 , 1 or 2.5. The compound according to claim 1 , wherein Ris C-alkyl.6. The compound according to claim 1 , wherein m is 1 or 2.7. The compound according to claim 1 , wherein q is 0 claim 1 , 1 or 2.8. The compound according to claim 1 , wherein Ris trifluoromethyl claim 1 , or C-alkyl.9. The compound according to claim 1 , wherein s is 1 or 2.10. The compound according to claim 1 , wherein Ris selected from the group consisting of halogen claim 1 , C-alkoxy claim 1 , C-sulfanyl claim 1 , C-alkyl claim 1 , hydroxy or trifluoromethyl.11. The compound according to claim 1 , said compound being1-[2-(2-Trifluoromethylphenylsulfanyl)phenyl]piperazine,1-[2-(4-Bromophenylsulfanyl)phenyl]piperazine,1-{2-[4-(Methylsulfanyl)phenylsulfanyl]phenyl}piperazine,1-[2-(4-Hydroxyphenylsulfanyl]phenyl}piperazine,1-[2-(2,4-Dimethylphenylsulfanyl)phenyl]piperazine,1-[2-(3,5-Dimethylphenylsulfanyl)phenyl]piperazine,1-[2-(2,6-Dimethylphenylsulfanyl)phenyl]piperazine,1-[2-(2,5-Dimethylphenylsulfanyl)phenyl]piperazine,1-[2-(2-Trifluoromethylphenylsulfanyl)phenyl][1,4]diazepane,1-[2-(3-Methylphenylsulfanyl)phenyl]-[1,4]-diazepane,1-[2-(4-Butylphenoxy)phenyl]piperazine,1-[2-(4-Methoxyphenoxy)phenyl]piperazine,2-(4-Methylphenylsulfanyl)phenyl-1-piperazine,1-[2-(4-Chlorophenylsulfanyl) ...

Phenyl-Piperazine Derivatives As Serotonin Reuptake Inhibitors

The invention provides compounds represented by the general formula I 115-. (canceled)17. The process of claim 16 , wherein each Ris independently C-alkyl.18. The process of claim 16 , wherein the compound of formula Ia is 1-[2-(2 claim 16 ,4-dimethylphenylsulfanyl)phenyl]piperazine.19. 1-[2-(2 claim 16 ,4-Dimethylphenylsulfanyl)phenyl]piperazine or an acid addition salt thereof obtained in the process of .21. The process of claim 20 , wherein each Ris independently C-alkyl.22. The process of claim 20 , wherein the compound of formula Ia is 1-[2-(2 claim 20 ,4-dimethylphenylsulfanyl)phenyl]piperazine.23. 1-[2-(2 claim 20 ,4-Dimethylphenylsulfanyl)phenyl]piperazine or an acid addition salt thereof obtained in the process of .25. The process of claim 24 , wherein each Ris independently C-alkyl.26. The process of claim 24 , wherein the compound of formula Ia is 1-[2-(2 claim 24 ,4-dimethylphenylsulfanyl)phenyl]piperazine.27. 1-[2-(2 claim 24 ,4-Dimethylphenylsulfanyl)phenyl]piperazine or an acid addition salt thereof obtained in the process of . The present invention relates to novel compounds which are serotonin reuptake inhibitors and as such effective in the treatment of for example depression and anxiety.Selective serotonin reuptake inhibitors (hereinafter referred to as SSRIs) have become first choice therapeutics in the treatment of depression, certain forms of anxiety and social phobias, because they are effective, well tolerated and have a favourable safety profile compared to the classic tricyclic antidepressants.However, clinical studies on depression indicate that non-response to SSRIs is substantial, up to 30%. Another, often neglected, factor in antidepressant treatment is compliance, which has a rather profound effect on the patient's motivation to continue pharmacotherapy.First of all, there is the delay in therapeutic effect of SSRIs. Sometimes symptoms even worsen during the first weeks of treatment. Secondly, sexual dysfunction is a side effect common ...

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) AS AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 114-. (canceled)16. A composition comprising:{'claim-ref': {'@idref': 'CLM-00015', 'claim 15'}, '(1) the compound and/or a salt thereof according to ; and'}(2) optionally a pharmaceutically acceptable carrier.17. The composition of claim 16 ,wherein the composition further comprises an excipient, andwherein the excipient is different from said pharmaceutically acceptable carrier.18. The composition of claim 16 , wherein the composition is a buffered solution.19. The composition of claim 16 , wherein the pharmaceutically acceptable carrier is selected from mannitol claim 16 , lactose claim 16 , glucose claim 16 , albumin claim 16 , or a combination thereof.21. A composition comprising:{'claim-ref': {'@idref': 'CLM-00020', 'claim 20'}, '(1) the compound and/or a salt thereof according to ; and'}(2) optionally a pharmaceutically acceptable carrier.22. The composition of claim 21 ,wherein the composition further comprises an excipient, andwherein the excipient is different from said pharmaceutically acceptable carrier.23. The composition of claim 21 , wherein the composition is a buffered solution.24. The composition of claim 21 , wherein the pharmaceutically acceptable carrier is selected from mannitol claim 21 , lactose claim 21 , glucose claim 21 , and albumin.26. A composition comprising:{'claim-ref': {'@idref': 'CLM-00025', 'claim 25'}, '(1) the compound and/or a salt thereof according to ; and'}(2) optionally a pharmaceutically acceptable carrier.27. The composition of claim 26 ,wherein the composition further comprises an excipient, andwherein the excipient is different from said pharmaceutically acceptable carrier.28. The composition of claim 26 , wherein ...

TREPROSTINIL DERIVATIVE COMPOUNDS AND METHODS OF USING SAME

Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used. 157-. (canceled)60. The compound of claim 58 , wherein R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , and Rare H.61. The compound of claim 58 , wherein at least one of R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , R claim 58 , and Ris deuterium.62. (canceled)64. (canceled)65. (canceled)66. A composition comprising a compound of or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers or excipients.67. The composition of claim 66 , which is formulated for transdermal delivery.68. The composition of claim 66 , which is formulated for transdermal delivery with a patch.6972-. (canceled)73. A method of treating pulmonary hypertension claim 58 , comprising administering to a subject in need of treatment a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof.74. (canceled)75. (canceled)76. The method of claim 73 , wherein the compound is administered orally claim 73 , topically or parenterally.77. The method of claim 76 , wherein the compound is administered transdermally.78. The method of claim 73 , wherein the pulmonary hypertension is pulmonary arterial hypertension.79. The method of claim 73 , further comprising administering an additional therapeutic agent.80. The method of claim 79 , wherein the additional therapeutic agent is ...

CATIONIC LIPID

Provided are a cationic lipid which facilitates the introduction of a nucleic acid into, for example, a cell or the like; a composition containing the cationic lipid and a nucleic acid; a method for introducing a nucleic acid into a cell by using a composition containing the cationic lipid and the nucleic acid; and the like. The cationic lipid is, for example, a cationic lipid represented by formula (A): formula (A): 2. The cationic lipid according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each tetradecyl claim 1 , hexadecyl claim 1 , (Z)-tetradec-9-enyl claim 1 , (Z)-hexadec-9-enyl claim 1 , (Z)-octadec-6-enyl claim 1 , (Z)-octadec-9-enyl claim 1 , (E)-octadec-9-enyl claim 1 , (Z)-octadec-11-enyl claim 1 , (9Z claim 1 ,12Z)-octadeca-9 claim 1 ,12-dienyl claim 1 , (9Z claim 1 ,12Z claim 1 ,15Z)-octadeca-9 claim 1 ,12 claim 1 ,15-trienyl claim 1 , (Z)-icos-11-enyl claim 1 , (11Z claim 1 ,14Z)-icosa-11 claim 1 ,14-dienyl claim 1 , or (Z)-docos-13-enyl.3. The cationic lipid according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each hexadecyl claim 1 , (Z)-hexadec-9-enyl claim 1 , (Z)-octadec-6-enyl claim 1 , (Z)-octadec-9-enyl claim 1 , (9Z claim 1 ,12Z)-octadeca-9 claim 1 ,12-dienyl claim 1 , (Z)-icosa-11-enyl claim 1 , or (11Z claim 1 ,14Z)-icosa-11 claim 1 ,14-dienyl.4. The cationic lipid according to claim 1 , wherein Xis alkylene having 1 to 3 carbon atoms claim 1 , and Xis a single bond or methylene.5. The cationic lipid according to claim 1 , wherein Xis methylene or ethylene.6. The cationic lipid according to claim 1 , wherein Rand Rmay be the same or different claim 1 , and are each methyl or ethyl claim 1 , or are combined together to form n-pentylene or n-hexylene.7. The cationic lipid according to claim 1 , wherein Rand Rare combined together to form n-propylene or n-butylene claim 1 , and Ris methyl or ethyl.8. The cationic lipid according to claim 1 , wherein ...

NANOMATERIALS

Lipid nanoparticle compositions for delivery of nucleic acids are described. In various embodiments the lipid nanoparticle contains an ionizable lipid of the Formula (I). Methods of using such lipid nanoparticle compositions to achieve targeted delivery of therapeutic cargo without the need for a targeting ligand are also provided. 2. The compound of claim 1 , wherein Ris C-Calkenyl with 2 units of unsaturation.4. The compound of claim 1 , wherein Xis absent or —O—.5. (canceled)7. The compound of claim 6 , wherein Xis hydrogen.8. The compound of claim 1 , wherein Xis absent.10. The compound of claim 9 , wherein Xis hydrogen.11. The compound of claim 9 , wherein Xis hydroxyl and a is 1.12. The compound of claim 9 , wherein Xis —NRRand a is 1.13. The compound of claim 1 , wherein Xis absent claim 1 , O— claim 1 , or —NR—.14. (canceled)15. (canceled)16. The compound of claim 1 , wherein Xis selected from the group consisting of: 4- to 8-membered heterocyclyl optionally substituted with 1 or 2 C-Calkyl groups claim 1 , 5- to 6-membered heteroaryl optionally substituted with 1 or 2 C-Calkyl groups claim 1 , 5- to 6-membered aryl optionally substituted with 1 or 2 C-Calkyl groups claim 1 , 4- to 7-membered cycloalkyl optionally substituted with 1 or 2 C-Calkyl groups.17. (canceled)18. (canceled)19. (canceled)20. The compound of claim 1 , wherein Xis absent claim 1 , O— claim 1 , or —NR—.21. (canceled)22. (canceled)23. The compound of claim 1 , wherein Xis 4- to 8-membered heterocyclyl optionally substituted with 1 or 2 C-Calkyl groups claim 1 , 5- to 6-membered heteroaryl optionally substituted with 1 or 2 C-Calkyl groups claim 1 , 5- to 6-membered aryl optionally substituted with 1 or 2 C-Calkyl groups claim 1 , or 4- to 7-membered cycloalkyl optionally substituted with 1 or 2 C-Calkyl groups.24. (canceled)25. (canceled)26. (canceled)27. The compound of claim 1 , wherein b is 0.28. The compound of claim 1 , wherein b is an integer between 1 and 6.29. The compound of ...

METHODS OF TREATMENT AND PREVENTION OF EYE DISEASES

The present invention provides compositions and methods useful for treating and preventing neovascular AMD by inhibition of CCR3. The compositions and methods are useful for treating and preventing diseases and disorders such as but not limited to, neovascular AMD 1. A method of treating and/or preventing an ocular disorder or disease associated with neovascularization in a subject , the method comprising identifying a subject with , or at risk of developing an ocular disease or disorder associated with neovascularization , and administering to the subject in need thereof a pharmaceutical composition comprising an agent for inhibiting the activity and/or expression of the CCR3 protein.2. The method of claim 1 , wherein the ocular disease or disorder is neovascular AMD.3. A method of treating and/or preventing an ocular disorder or disease associated with increased choroidal vascular permeability in a subject claim 1 , the method comprising identifying a subject with claim 1 , or at risk of developing neovascular AMD or disorder associated with increased choroidal vascular permeability claim 1 , and administering to the subject in need thereof a pharmaceutical composition comprising an agent for inhibiting the activity and/or expression of the CCR3 protein.4. The method of claim 1 , wherein the ocular disease or disorder is dry or geographic atrophy AMD.5. A method of treating and/or preventing AMD in a subject with claim 1 , or at risk of AMD claim 1 , comprising administering to the subject a pharmaceutical composition comprising an agent which inhibits the activity and/or expression of CCR3 protein.6. The method of claim 5 , wherein inhibition of the CCR3 protein reduces or stops a symptom of AMD.7. A method of treating and/or preventing AMD in a subject with claim 5 , or at risk of AMD claim 5 , comprising administering to the subject a pharmaceutical composition comprising an agent which inhibits the activity and/or expression of CCR3 protein claim 5 , wherein ...

Phenyl-Piperazine Derivatives As Serotonin Reuptake Inhibitors

The invention provides compounds represented by the general formula I 115-. (canceled)16. A pharmaceutical composition , comprising:1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine or a hydrobromic acid addition salt thereof, andat least one pharmaceutically acceptable carrier or diluent.17. The composition of claim 16 , wherein the composition comprises a hydrobromic acid addition salt of 1-[2-(2 claim 16 ,4-dimethylphenylsulfanyl)phenyl]piperazine.18. The composition of claim 17 , wherein the composition is a tablet.19. The composition of claim 18 , wherein the composition comprises 1-[2-(2 claim 18 ,4-dimethylphenylsulfanyl)phenyl]piperazine in an amount of from 0.01 mg to 100 mg.201. A method for the treatment of an affective disorder in a human in need thereof claim 18 , comprising administering to the human an amount of the composition of claim comprising a therapeutically effective amount of 1-[2-(2 claim 18 ,4-dimethylphenylsulfanyl)phenyl]piperazine or a hydrobromic acid addition salt thereof.21. The method of claim 20 , wherein the affective disorder is depression.22. The method of claim 20 , wherein the affective disorder is an anxiety disorder.23. The method of claim 22 , wherein the anxiety disorder is general anxiety disorder or panic disorder.24. The method of claim 20 , wherein the affective disorder is obsessive compulsive disorder.25. The method of claim 20 , wherein the composition comprises a therapeutically effective amount of a hydrobromic acid addition salt of 1-[2-(2 claim 20 ,4-dimethylphenylsulfanyl)phenyl]piperazine.26. The method of claim 25 , wherein the affective disorder is depression.27. The method of claim 25 , wherein the affective disorder is an anxiety disorder.28. The method of claim 27 , wherein the anxiety disorder is general anxiety disorder or panic disorder.29. The method of claim 25 , wherein the affective disorder is obsessive compulsive disorder.30. The method of claim 25 , wherein the composition is a tablet.31. The ...

PYRIMIDINE AND PYRAZINE HDAC1,2 INHIBITORS

Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity. 2. The compound of claim 1 , wherein:{'sup': 1', '3, 'Ris selected from the group consisting of halo, phenyl, thiazole, and thienyl, wherein phenyl is optionally substituted with R;'}{'sup': 2', '4', '4', '4, 'Ris selected from the group consisting of heterocycloalkyl, OR, and N(H)R, wherein heterocycloalkyl is optionally substituted with R;'}{'sup': '3', 'sub': 1', '4', '2', '1', '4, 'Ris C-Calkyl or —OSON(H)C-Calkyl;'}{'sup': '4', 'sub': 1', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'Ris independently, at each occurrence, selected from the group consisting of C-Calkyl, —(C-Calkyl)-O—(C-Calkyl), —C(O)—C-Calkyl, and -heterocycloalkyl-C(O)-heterocycloalkyl, wherein C-Calkyl is optionally substituted with —OH; and'}n is 1 or 2.3. The compound of or claim 1 , wherein:{'sup': 1', '3, 'Ris selected from the group consisting of halo, phenyl, thienyl, and thiazole, wherein phenyl is optionally substituted with R;'}{'sup': 2', '4', '4', '4, 'Ris selected from the group consisting of piperazine, OR, and N(H)R, wherein piperazine is optionally substituted with R;'}{'sup': '3', 'sub': '2', 'Ris methyl or —OSON(H)Me;'}{'sup': '4', 'sub': 1', '3', '1', '2', '1', '3, 'Ris independently, at each occurrence, selected from the group consisting of C-Calkyl, —(C-Calkyl)-O-methyl, —C(O)-methyl, and -piperadine-C(O)-piperazine, wherein C-Calkyl is optionally substituted with —OH; and'}n is 1 or 2.5. The compound of wherein:{'sup': '5', 'Ris phenyl or thienyl; and'}{'sup': '6', 'sub': 1', '2, 'Ris piperazine or O—(C-Calkyl)-O-methyl.'}7. The compound of claim 6 , wherein:{'sup': '8', 'Ris selected from the group consisting of furanyl, phenyl, and thienyl;'}{'sup': 9', '10, 'sub': 1', '4, 'Ris N(H)Ror heterocycloalkyl, wherein heterocycloalkyl is optionally substituted with C-Calkyl; and'}{' ...

Crystalline forms of neurotrophin mimetic compounds and their salts

The present invention includes crystalline forms of (2S,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and salts thereof. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic uses of the crystalline forms.

TREPROSTINIL DERIVATIVE COMPOUNDS AND METHODS OF USING SAME

Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used. 170-. (canceled)72. The compound of claim 71 , wherein Ris Pand Ris H.73. The compound of claim 71 , wherein Ris H and Ris P.74. The compound of claim 71 , wherein Ris Pand Ris P.75. The compound of claim 71 , wherein each of Rto Ris H.76. The compound of claim 71 , wherein at least one of Rto Ris deuterium.77. The compound of claim 71 , wherein Z is —OR.78. The compound of claim 71 , wherein Z is P.79. The compound of claim 71 , wherein Z is —N(R)R.80. The compound of claim 71 , wherein Z is —OH.82. A composition comprising a compound of or a pharmaceutically acceptable salt thereof and at least one other component.83. The composition of claim 82 , which is formulated for transdermal delivery.84. The composition of claim 83 , which is formulated for transdermal delivery with a patch.85. The composition of claim 82 , further comprising at least one solvent.86. A method of treating pulmonary hypertension claim 71 , comprising administering to a subject in need of treatment a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof.87. The method of claim 86 , wherein the pulmonary hypertension is pulmonary arterial hypertension.88. The method of claim 86 , wherein the compound is administered transdermally.89. The method of claim 88 , wherein the compound is administered via a transdermal patch. This application claims priority to U.S. provisional application 61/751,608 filed Jan. 11, 2013 which is incorporated herein by reference in its entirety for all purposes.Pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH) is a disease which can result in death and is ...

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 4. A radiolabeled compound comprising the compound of .5. A metal complex comprising a radionuclide and a compound of .6. The metal complex of claim 5 , wherein the radionuclide is In claim 5 , Y claim 5 , Ga claim 5 , Lu claim 5 , Tc claim 5 , Cu claim 5 , Gd claim 5 , Gd claim 5 , Gd claim 5 , Bi claim 5 , Ac or Fe.7. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable salt claim 1 , or ester thereof claim 1 , and a pharmaceutically acceptable carrier.8. The compound of for use in a method of imaging in a patient.9. The compound of for use in a method of diagnosing prostate cancer and/or metastasis thereof.10. The compound of for use in a method of treating prostate cancer and/or metastasis thereof.11. A pharmaceutical composition comprising the metal complex of claim 5 , or a pharmaceutically acceptable salt claim 5 , or ester thereof claim 5 , and a pharmaceutically acceptable carrier.12. The metal complex of for use in a method of imaging in a patient.13. The metal complex of for use in a method of diagnosing prostate cancer and/or metastasis thereof.14. The metal complex of for use in a method of treating prostate cancer and/or metastasis thereof. This application is a continuation-in-part application of international patent application Serial No. PCT/EP2014/002808 filed Oct. 17, 2014, which published as PCT Publication No. WO 2015/055318 on Apr. 23, 2015, which claims benefit of European patent application Serial Nos. 13004991.9 filed Oct. 18, 2013 and 14175612.2 filed Jul. 3, 2014.The foregoing applications, and all documents cited therein or during their prosecution (“appln cited documents”) and all documents cited ...

LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib). 4. A radiolabeled compound comprising the compound of .5. A metal complex comprising a radionuclide and a compound of .6. The metal complex of claim 5 , wherein the radionuclide is In claim 5 , Y claim 5 , Ga claim 5 , Lu claim 5 , Tc claim 5 , Cu claim 5 , Gd claim 5 , Gd claim 5 , Gd claim 5 , Bi claim 5 , Ac or Fe.7. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable salt claim 1 , or ester thereof claim 1 , and a pharmaceutically acceptable carrier.8. The compound of for use in a method of imaging in a patient.9. The compound of for use in a method of diagnosing prostate cancer and/or metastasis thereof.10. The compound of for use in a method of treating prostate cancer and/or metastasis thereof.11. A pharmaceutical composition comprising the metal complex of claim 5 , or a pharmaceutically acceptable salt claim 5 , or ester thereof claim 5 , and a pharmaceutically acceptable carrier.12. The metal complex of for use in a method of imaging in a patient.13. The metal complex of for use in a method of diagnosing prostate cancer and/or metastasis thereof.14. The metal complex of for use in a method of treating prostate cancer and/or metastasis thereof. This application is a continuation-in-part application of international patent application Serial No. PCT/EP2014/002808 filed Oct. 17, 2014, which published as PCT Publication No. WO 2015/055318 on Apr. 23, 2015, which claims benefit of European patent application Serial Nos. 13004991.9 filed Oct. 18, 2013 and 14175612.2 filed Jul. 3, 2014.The foregoing applications, and all documents cited therein or during their prosecution (“appln cited documents”) and all documents cited ...

TREPROSTINIL DERIVATIVE COMPOUNDS AND METHODS OF USING SAME

Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used. 170-. (canceled)72. The compound of claim 71 , wherein Ris Pand Ris H.73. The compound of claim 71 , wherein Ris H and Ris P.74. The compound of claim 71 , wherein Ris Pand Ris P.75. The compound of claim 71 , wherein each of Rto Ris H.76. The compound of claim 71 , wherein at least one of Rto Ris deuterium.77. The compound of claim 71 , wherein Z is —OR.78. The compound of claim 71 , wherein Z is P.79. The compound of claim 71 , wherein Z is —N(R)R.80. The compound of claim 71 , wherein Z is −OH.82. A composition comprising a compound of or a pharmaceutically acceptable salt thereof and at least one other component.83. The composition of claim 82 , which is formulated for transdermal delivery.84. The composition of claim 83 , which is formulated for transdermal delivery with a patch.85. The composition of claim 82 , further comprising at least one solvent.86. A method of treating pulmonary hypertension claim 71 , comprising administering to a subject in need of treatment a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof.87. The method of claim 86 , wherein the pulmonary hypertension is pulmonary arterial hypertension.88. The method of claim 86 , wherein the compound is administered transdermally.89. The method of claim 88 , wherein the compound is administered via a transdermal patch. This application claims priority to U.S. provisional application 61/751,608 filed Jan. 11, 2013 which is incorporated herein by reference in its entirety for all purposes.Pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH) is a disease which can result in death and is ...

Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

Labeled inhibitors of prostate specific membrane antigen (PSMA) as agents for the treatment of prostate cancer

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

前列腺特异性膜抗原(psma)的标记的抑制剂，它们作为显影剂和用于治疗前列腺癌的药剂的用途

本发明总体上涉及放射药剂的领域和它们在核医学中作为示踪物、显影剂和用于治疗各种前列腺癌的疾病状态的用途。因此，本发明涉及由通式(1a)或(1b)表示的化合物。

前列腺特异性膜抗原（psma）的标记的抑制剂及其用途

本申请提供前列腺特异性膜抗原（PSMA）的标记的抑制剂及其用途。本发明总体上涉及放射药剂的领域和它们在核医学中作为示踪物、显影剂和用于治疗各种前列腺癌的疾病状态的用途。因此，本发明涉及由通式(1a)或(1b)表示的化合物。

一种卤素取代化合物及其制备方法和应用

本发明涉及一种卤素取代化合物的制备方法，如式Ⅰ所示的哌嗪衍生物与如式Ⅵ所示的卤代乙酰卤衍生物反应生成如式Ⅱ所示的卤素取代化合物。本发明还涉及一种卤素取代化合物制备吡唑衍生物的制备方法，如式Ⅱ所示的卤素取代化合物与甲基肼反应，关吡唑环生成如式Ⅳ所示的卤素取代烷基‑1‑甲基吡唑衍生物；或与甲基肼苯甲醛腙反应，生成如式Ⅲ所示的腙化合物，在酸的作用下，关吡唑环生成如式Ⅳ所示的卤素取代烷基‑1‑甲基吡唑衍生物。本发明还涉及中间体化合物的结构。本发明的卤素取代化合物和吡唑衍生物的制备方法适于产业化生产。

2-фторированное производное ацил-3-аминоакрилонитрила и способ его получения

1. Способ получения соединения, представленного приведенной ниже формулой (3), при котором подвергают взаимодействию соединение, представленное приведенной ниже формулой (1), с соединением, представленным приведенной ниже формулой (2): ! ! где в формуле (1) Rf представляет собой алкильную группу, имеющую от 1 до 6 атомов углерода, которая замещена по меньшей мере одним атомом фтора, а Х представляет собой атом галогена, гидроксигруппу или карбонилоксигруппу; ! ! где в формуле (2) R1 и R2 каждый независимо представляет собой атом водорода, алкильную группу, имеющую от 1 до 6 атомов углерода, циклоалкильную группу, имеющую от 3 до 6 атомов углерода, арильную группу, которая может быть замещена, арилалкильную группу, которая может быть замещена, ацильную группу, имеющую от 1 до 6 атомов углерода, которая может быть замещена, или группу атомов, которая образует 5- или 6-членное кольцо, содержащее 4 или 5 атомов углерода, атом азота, с которым связаны R1 и R2, и 0 или 1 гетероатом, отличающийся от атома азота, с которым связаны R1 и R2, а R3 представляет собой атом водорода, алкильную группу, имеющую от 1 до 6 атомов углерода, циклоалкильную группу, имеющую от 3 до 6 атомов углерода, арильную группу, которая может быть замещена, или арилалкильную группу, которая может быть замещена; ! ! и где в формуле (3) Rf, R1, R2 и R3 имеют те же значения, как описано выше. !2. Способ по п.1, где R1 и R2 каждый независимо представляет собой алкильную группу, имеющую от 1 до 6 атомов углерода, циклоалкильную группу, имеющую от 3 до 6 атомов углерода, или группу атомов, которая образует 5- или 6-членное кольцо, содержащее 4 или 5 атомов углерода и 0 или 1 гетероатом, с атомом азота, с кот� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2009 124 415 (13) A (51) МПК C07C 253/30 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (71) Заявитель(и): Мицуй Кемикалс Агро, ИНК (JP) (21)(22) Заявка: 2009124415/04, 18.12.2007 Приоритет(ы): ( ...

process for preparing compounds, and, compound.

Novel photoinitiators

A photoinitiator selected from the group consisting of an acylphosphine oxide, a α-hydroxy-ketone and a α-amino-ketone, characterized in that the photoinitiator includes at least one aliphatic disulfide as functional group.

Novel photoinitiators

A photoinitiator selected from the group consisting of an acylphosphine oxide, a α-hydroxy-ketone and a α-amino-ketone, characterized in that the photoinitiator includes at least one aliphatic disulfide as functional group.

Crystalline forms of neurotrophin mimetic compounds and their salts

The present invention includes crystalline forms of (2S,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and salts thereof. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic uses of the crystalline forms.

Chemical agents for protection of 1-arylpyrroles, insectoacaricidonematocidal composition, and process for controlling insects

FIELD: agriculture. SUBSTANCE: product of general formula: of compound (Ia) wherein n is 0.1 or 2; X-R 2 S(O) n is R 2 -alkyl, C 1 -C 3 -haloalkyl; C 1 -C 3 is hydrogen, alkyl, alkylthio, cyanoalkyl containing 1-3 carbon atoms; R 1 is chlorial, alkyl or difluoroalkyl containing 1-3 carbon atoms; Y is trifluoromethyl provided that when R 3 is chlorine or fully substituted fluoroalkyl; R 3 cannot be hydrogen in compound (Ic); R 1 is halogen, R 2 S(O) n , n is 0, 1 or 2; R 2 is haloalkyl; C 1 -C 3 is bromine, C 1 -C 3 -alkylthio, C 1 -C 3 -alkoxy-C 1 -C 3 - alkylideneimino; R 3 is hydrogen; Y is chlorine, Insectoacaricidohemotocidal composition comprises 0.1 wt % of product and the desired additives balance. Process for controlling insects by applying 100 g/ha to the habitats thereof. EFFECT: improved properties of the composition. 13 cl, 2 tbl 617СсС60с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ЗВО“” 2092 479 ' (51) МПК 13) СЛ С 070 207/34, А 01 М 43/36 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 4895762/04, 04.06.1991 (30) Приоритет: 05.06.1970 Ц$ 533.470 (46) Дата публикации: 10.10.1997 (56) Ссылки: Ц, патент, 4013445, кл. А 01 М 9/28, ЛЭ7ТГ ЕК, патент, 2066492, кл. С 07 О 21100, 1911. ЕК, патент, 2183158, кл. А 01 М 9/22, 19171. (71) Заявитель: Рон-Пуленк Агрошими (ЕК) (72) Изобретатель: Филип Рейд Тиммонс[Ц$], Рассел Джеймс Аутколт[Ц$], Патрисиа Л.Квятковски[Ц $], Энибел Лоупс[ 4$], Пол.А.Кейн[Ц$], Дэвид Нил СинодисЦ$], Ли С.Холл[Ц$]|, Жан-Пьер А.Вор[ЕК] (73) Патентообладатель: Рон-Пуленк Агрошими (ЕК) (54) ПРОИЗВОДНЫЕ 1-АРИЛПИРРОЛОВ, ИНСЕКТОАКАРИЦИДОНЕМАТОЦИДНАЯ КОМПОЗИЦИЯ И СПОСОБ БОРЬБЫ С НАСЕКОМЫМИ (57) Реферат: Использование: химические средства защиты растений, в качестве вещества, обладающего инсектоакарицидонематоцидной активностью. Сущность изобретения: продукт общей формулы | х ч 1 3 Е Е С1 1 у для соединения 1а Х - К 25(О)„, где п - О, 1, 2, В- - С1-Сз-алкил, С1-Сз-галогеналкил, В! - водород, алкил, алкилтио ...

Novel Diaminomethylidene Derivatives (NOVEL DIAMINCMETHYLIDENE DERIVATIVE)

본 발명은 화학식 (1)로 표시되는 신규한 디아미노메틸리덴 유도체 및 그의 약제학적으로 허용가능한 염에 관한 것이다: [식중, R 1 은 수소, C 1 -C 6 알킬기, C 3 -C 6 시클로알킬기 등이고; R 2 는, 하기식 등의 기등이고; R 3 는 수소원자, C 1 -C 6 알킬기 등이고; X는 O, S, CHNO 2 , C(COOR 4 )CN, C(CN) 2 등이다]. 상기 화합물은 소화계 질병치료용으로 사용되는 위장 활성 촉진제로서 유용하다.

Its use as a labeling inhibitor of prostate-specific membrane antigen (PSMA), imaging agents and agents for the treatment of prostate cancer

Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer

일반적으로 본 발명은 방사성 의약품 분야 및 핵의학에서의 추적자, 조영제로서의 이의 용도, 및 다양한 질환 상태의 전립선암의 치료에 있어서의 이의 용도에 관한 것이다. 따라서, 본 발명은 화학식 Ia 또는 화학식 Ib로 표시되는 화합물에 관한 것이다. In general, the present invention relates to tracers in the field of radiopharmaceuticals and nuclear medicine, their use as contrast agents, and their use in the treatment of prostate cancer of various disease states. Accordingly, the present invention relates to a compound represented by formula (Ia) or (Ib).

N-(2-(2-(dialkylamino)ethoxy)ethyl)carboxamides and hydrochlorides thereof, having antiarrhythmic activity, and pharmaceutical compositions based thereon

FIELD: medicine; pharmacology.SUBSTANCE: invention refers to pharmacology, namely to compounds of the following general formula, which exhibit antiarrhythmic activity. In said formula when R=CH, and n=0, then NR=NCHor NCHO; when R=CHOCH, and n=1, then NR=N(CH), NCH, NCHor NCHO; when R=CHOCH, and n=0, then NR=NCHor NCHO; when R=2,4-Cl-CHOCH, and n=1, then NR=N(CH), NCH, NCHor NCHO; when R=2,4-Cl-CHOCH, and n=0, then NR=NCHor NCHO, wherein NCHmeans pyrrolidino, NCH– piperidino, NCHO – morpholino. Invention also relates to a medicinal agent and a pharmaceutical composition, which include said compounds.EFFECT: disclosed are N-(2-(2-(dialkylamino)ethoxy)ethyl)carboxamides and hydrochlorides thereof, having antiarrhythmic activity, and pharmaceutical compositions based thereon.3 cl, 4 tbl, 3 dwg, 20 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 712 638 C1 (51) МПК C07C 235/34 (2006.01) C07D 295/145 (2006.01) C07D 295/15 (2006.01) A61K 31/165 (2006.01) A61K 31/40 (2006.01) A61K 31/4453 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A61K 31/5375 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61P 9/06 (2006.01) (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07C 235/34 (2019.08); C07D 295/145 (2019.08); C07D 295/15 (2019.08); A61K 31/165 (2019.08); A61K 31/40 (2019.08); A61K 31/4453 (2019.08); A61K 31/5375 (2019.08); A61P 9/06 (2019.08) (21)(22) Заявка: 2019109598, 02.04.2019 02.04.2019 Дата регистрации: 30.01.2020 (45) Опубликовано: 30.01.2020 Бюл. № 4 2 7 1 2 6 3 8 (73) Патентообладатель(и): Федеральное государственное бюджетное образовательное учреждение высшего образования "МИРЭА - Российский технологический университет" (РТУ МИРЭА) (RU), Федеральное государственное бюджетное учреждение "Национальный медицинский исследовательский центр кардиологии" Министерства здравоохранения Российской Федерации (ФГБУ "НМИЦ кардиологии" Минздрава России) (RU) R U (56) Список документов, цитированных в отчете о поиске: RU 2645080 C1, 15.02.2018. RU 2130922 C1, 27.05.1999. Е.Я. БОРИСОВА и др. Антиаритмики ...

Labeled inhibitors of Prostate Specific Membrane Antigen (PSMA) and uses thereof

本申请提供前列腺特异性膜抗原(PSMA)的标记的抑制剂及其用途。本发明总体上涉及放射药剂的领域和它们在核医学中作为示踪物、显影剂和用于治疗各种前列腺癌的疾病状态的用途。因此，本发明涉及由通式(1a)或(1b)表示的化合物。

Amide derivatives

본 발명은 광학적으로 활성인 일반식(A)의 아미드 및 이의 염의 제조를 위한 신규한 비대칭적 합성법에 관한 것이다. 상기 일반식에서, X는 -N-(a) 또는 -CH-(b)를 나타내고, R은 모노 또는 바이사이클릭 아릴 또는 헤테로아릴 그룹을 나타내며, R 1 은 아릴 또는 헤테로아릴 라디칼을 나타내고, R 2 및 R 3 본원에서 정의한 의미를 갖는다. 당해 생성물은 5-HT 1A 길항제로서 유용하다. 본 발명의 방법에 유용한 중간체인 신규한 디에스테르도 기술되어 있다.

Merocyanine derivatives for cosmetic use.

Merocyanine derivatives

화학식 1 및 화학식 2의 화합물 및/또는 그의 E/E-, E/Z- 또는 Z/Z-기하 이성질체 형태가 개시되며, 여기서 R1 내지 R5, R1 내지 R11 및 A는 명세서에 정의된 바와 같다. 화합물은 광분해성 및 산화성 분해로부터 가정용 제품의 보호를 위한 UV 흡수제로서, 바람직하게는 식품 및 약품 포장 용도를 위한 플라스틱 첨가제로서, 화학식 1' 및/또는 화학식 2'의 화합물을 투명 식품 용기에 도입시킴으로써 식품의 광-분해를 방지하기 위해, UV 흡수제를 투명 블리스터 호일 또는 투명 약품 용기에 도입시킴으로써 광-분해로부터 UV-A 감수성 약물을 보호하기 위해, 사진 및 인쇄 용도를 위한 첨가제로서, 전자제품 용도를 위한 첨가제로서, 및 농업 용도에서 성분을 보호하기 위해 사용된다. <화학식 1> <화학식 2> <화학식 1'> <화학식 2'> Compounds of Formula 1 and Formula 2 and / or their E / E-, E / Z- or Z / Z- geometric isomeric forms are disclosed wherein R1 to R5, R1 to R11 and A are as defined herein. The compound is a UV absorber for the protection of household products from photodegradable and oxidative degradation, preferably as a plastic additive for food and pharmaceutical packaging applications, by introducing a compound of formula 1 'and / or formula 2' into a transparent food container. As an additive for photography and printing applications, to protect UV-A sensitive drugs from photo-degradation by introducing UV absorbers into transparent blister foils or transparent chemical containers to prevent photo-degradation of foods. As an additive for and for protecting the components in agricultural applications. <Formula 1> <Formula 2> <Formula 1 '> <Formula 2 '>

Preparation of optically pure beta-amino acids having affinity for the alpha-2-delta protein

公开了用于制备光学活性β－氨基酸的材料和方法，它们与钙通道的α－2－δ亚单位结合，可用于治疗疼痛、纤维肌痛和多种精神与睡眠疾患。该方法包括使手性烯丙基胺与2－炔酸酯在路易斯酸和碱的存在下反应，得到手性叔烯胺，在与氨反应后氢化，得到光学活性β－氨基酸。

Indole derivatives and their use as protein kinase inhibitors

The present invention relates inter alia to a compound of formula (I) wherein R1, R2 and R3, are as defined in the specification and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of fibrotic diseases or interstitial lung diseases, in particular idiopathic pulmonary fibrosis.

2,2'-Bis(dicyclopenthylphosphino)-1-1'-binaphthyl and metal complexes thereof

2,2′-bis(dicyclopentylphosphino)-1,1′-binaphthyl is prepared by the reactions: The optical resolution of the racemic (IX) is effected by adding an ethyl acetate solution, of (+) or (-) dibenzoyltartaric acid, recrystallisation, solution in chloroform, adding NaOH, distillation and recrystallisation. The product (I) forms a complex with a transition metal, e.g. Rh, Pd, Ru, Ir or Ni, and the complexes are useful as catalysts, e.g. for asymmetric hydrogenation, giving high yields.

2,2'-Bis(dicyclopenthylphosphino)-1-1'-binaphthyl and metal complexes thereof

MARKED MEMBRANE-SPECIFIC PROSTATIC ANTIGEN (PSMA) INHIBITORS INCLUDING CARBOXYL GROUPS AND A MODIFIED BINDER REGION, IMAGING AGENTS, AND UNDERSTANDING PHARMACEUTICAL AGENTS

Esta referido a compuestos de Formula Ia o Ib, en donde: Z es -CO2H, -SO2H, -SO3H, -SO4H, -PO2H, -PO3H, -PO4H2; n es 0, 1; Y es arilo, alquilarilo, ciclopentilo, entre otros; m es 1, 2, 3, 4; X es naftilo, fenilo, bifenilo, entre otros; Quelante es DOTA, HBED-CC, NOTA, entre otros. Estos compuestos son radiofarmacos y se emplean en medicina nuclear como trazadores, agentes formadores de imagenes y para el tratamiento de diversos estados patologicos de cancer de prostata. It refers to compounds of Formula Ia or Ib, where: Z is -CO2H, -SO2H, -SO3H, -SO4H, -PO2H, -PO3H, -PO4H2; n is 0.1; Y is aryl, alkylaryl, cyclopentyl, among others; m is 1, 2, 3, 4; X is naphthyl, phenyl, biphenyl, among others; Chelator is DOTA, HBED-CC, NOTE, among others. These compounds are radiopharmaceuticals and are used in nuclear medicine as tracers, imaging agents, and for the treatment of various disease states of prostate cancer.

NOVEL AMINOALKYL NAPHTHALENIC DERIVATIVES, THEIR ACID ADDING SALTS AND THE PREPARATION PROCESS AND THE THERAPEUTIC APPLICATION OF SUCH DERIVATIVES AND SALTS

Alpha-piperazino-beta-benzoylpropionic acids - - with analgesic,analeptic,anticonvulsant and other activity

Cpds. of formula where R is 1-4C alkyl, -CH2CO2R' where R' is 1-4C alkyl or where R2, R3 are H, 1-4C alkyl or R2, R3 and the attached N-atom may be pyrrolidino, piperazino or morpholino. Cpds. have analgesic, analeptic, anticonvusant, anxiolytic, hypotensive, vasodilator and diuretic activity. Pref. by reaction of 2-benzoylacrylic acid with 1-substd. piperazines. Cpds. have low toxicity.

Patent FR4670M

Xanthinoxidase-inhibitory substd. formamidrazones - prepd. by reacting 4-pyrimidinone and amine

N-Acyl-N''-(3-amino-2-cyano-acryloyl) formamidrazones of formula (I) : and their tautomers and salts with (in)org. acids (in which R1 and R2 are same or different H or opt. branched 1-7C alkyl, with proviso that R1 and R2 are not both H, R1+R2 may form 2-5C alkylene in which one methylene group is opt. replaced by -O, -S or -NR7 forming . e.g. 3-aza-, 3-thia-, 3-oxo-pentamethylene and pentamethylene, R1 and R2 are pref. methyl or together from 3-oxo-pentamethylene R7=H or 1-7C alkyl; R3 = 4- N,N-dipropylsulphamoyl - phenyl, pyridyl-(3), pyridyl-(4), 1,3,5-triphenylpyrazolyl -(4) -methyl, 1,2,3,6-tetrahydro-2,6-dioxopyrimidinyl-(4), thiazolidinyl-(4), 1- 6-methoxynaphthyl-(2) -ethyl, 1-methyl-1-(4- 1,2,3,4-tetrahydronaphthyl-(1) -phenoxy) -ethyl, (3-trifluoromethyl phenoxy)-(4-chlorophenyl)-methyl, 3-acetyl-thiazoliol-inyl-(4) and esp. 1-methyl-1-(4-chlorophenoxy)-ethyl) have xanthinoxidase inhibitory activity and may be used against gout, coronary insufficiency and anti-arrhythmia. Depending on R3 cpds. (I) also have lipid-lowering-, uricosuric-, antiphlogistic-, esp. anti-rheumatic- and liver-protecting activity. (I) are also inters. for other active cpds. such as 4(1H)-pyrimidinones used esp. against gout.

Crystalline forms of neurotrophin mimetic compounds and their salts

The present invention includes crystalline forms of (2S,3S)-2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and salts thereof. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic uses of the crystalline forms.

NOVEL AMINOALKYL NAPHTHALENIC DERIVATIVES, THEIR ACID ADDITION SALTS AND THE PREPARATION METHOD THEREOF AND THE THERAPEUTIC USE OF THESE DERIVATIVES AND SALTS

NOUVEAUX DERIVES AMINOALKYL NAPHTALENIQUES REPONDANT A LA FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE: -R ET R SONT IDENTIQUES OU DIFFERENTS ET REPRESENTENT UN ATOME D'HYDROGENE OU UN GROUPE ALKYLE COMPORTANT DE 1 A 4 ATOMES DE CARBONE OU FORMENT CONJOINTEMENT AVEC L'ATOME D'AZOTE AUQUEL ILS SONT LIES, UN RADICAL HETEROCYCLIQUE CHOISI PARMI LES SUIVANTS: PYRROLIDINO, PIPERIDINO, HEXAMETHYLENEIMINO, MORPHOLINO, PIPERAZINO, METHYL-4 PIPERAZINO; -N1, 2 OU 3; -R REPRESENTE UN ATOME D'HYDROGENE OU D'HALOGENE OU UN GROUPE METHYLE; ET -R REPRESENTE UN ATOME D'HYDROGENE OU D'HALOGENE OU UN GROUPE METHYLE OU METHOXY,AINSI QUE LEURS SELS D'ADDITION D'ACIDE ORGANIQUE OU MINERAL. CES DERIVES ET SELS SONT UTILISABLES EN THERAPEUTIQUE, NOTAMMENT COMME ANTIDEPRESSEURS ETOU ANALGESIQUES. NEW AMINOALKYL NAPHTHALENIC DERIVATIVES RESPONDING TO THE FORMULA: (CF DRAWING IN BOPI) IN WHICH: -R AND R ARE THE SAME OR DIFFERENT AND REPRESENT A HYDROGEN ATOM OR AN ALKYL GROUP CONTAINING FROM 1 TO 4 ATOMES OF CARBON OR CONJOIN 'NITROGEN ATOM TO WHICH THEY ARE BOUND, A HETEROCYCLIC RADICAL CHOSEN FROM THE FOLLOWING: PYRROLIDINO, PIPERIDINO, HEXAMETHYLENEIMINO, MORPHOLINO, PIPERAZINO, METHYL-4 PIPERAZINO; -N1, 2 OR 3; -R REPRESENTS A HYDROGEN OR HALOGEN ATOM OR A METHYL GROUP; ET -R REPRESENTS A HYDROGEN OR HALOGEN ATOM OR A METHYL OR METHOXY GROUP, AS WELL AS THEIR ADDITIONAL SALTS OF ORGANIC OR MINERAL ACID. THESE DERIVATIVES AND SALTS CAN BE USED THERAPEUTICALLY, IN PARTICULAR AS ANTIDEPRESSANTS AND OR ANALGESICS.

Beta-amino-alpha-aryloxymethylacrylonitrile - and 2,4-diamino-5-benzylpyrimidine derivs. useful as antibacterial agents

Cpds. of the formula: Ar-CH2-C(CN)=CH-NR5R6 (I) (where Ar is phenyl (opt. subst.) and NR5R6 is an aliph., heterocyclic or aromatic amino group in which one of R5 and R6 can be H) substantially free of contamination by the isomeric beta-amino-alpha-benzylidene-propionitriles are claimed; processes for their manufacture are also claimed. 2,4-Diamino-5-benzyl-pyrimidines (e.g. trimethoprim) having antimalarial and antibacterial activity are prepd. by reacting (I) with guanidine. Hydrolysis of (I) with aqs. acid gives new (and claimed) cpds. Ar-C(CN)=CH-OH, alkylation of which gives corr. beta-(lower alkoxy)-alpha-benzyl-acrylonitriles.

Alpha-phenyl alpha-piperidino acetic acid derivatives and their preparation

Process for the preparation of substituted alpha-alpha-diphenyl-gamma-amino 1 butyramides

Process for the catalytic preparation of substituted aminocyanoesters

PROCESS FOR PREPARING GLYCOCOLS NITRILS

Phenylacetic acid derivatives and their preparation

Patent FR2320095B1

Process for the preparation of amino acids such as 1-phenyl-2,3-dimethyl-5-pyrazolonyl- (4) -morpholino-acetic acid

Pyrazolo(3,4-d)pyrimidines

PROCESS FOR PREPARING TERTIARY AMINES

Naphtalenic aminoalkyl derivatives, the acid addition salts thereof and the process for preparing same, as well as the application in therapeutics of these derivatives and salts

Title : "New naphtalenic aminoalkyl derivatives, the acid addition salts thereof and the process for preparing same, as well as the application in therapeutics of these derivatives and salts" (Invention of Alain-René SCHOOFS, Guy BOURGERY, Bernard BUCHER) Applicant : DELALANDE S.A. ABSTRACT OF THE DISCLOSURE New naphtalenic aminoalkyl derivatives corresponding to the for-mula : (I) in which : - R1 and R2 are identical or different and represent a hydrogen atom or an alkyl group comprising 1 to 4 carbon atoms or form, conjointly with the nitrogen atom to which they are linked, a heterocyclic radical chosen from the following : pyrrolidino, piperidino, hexamethyleneimino, morpholino, piperazino, 4-methyl piperazino ; - n = 1, 2 or 3 ; - R represent a hydrogen or halogen atom or a methyl group; and - R3 represents a hydrogen or halogen atom or a methyl or methoxy group, as well as the organic or mineral acid addition salts thereof. These derivatives and salts are usable in therapeutics, more particularly as antidepressants and/or analgesics.

Antiandrogenic n-(3,5-dilower alkyl-4-heterocyclic)methyl)phthalimides

A NOVEL CLASS OF NON-STERODIAL ANTIANDROGENIC COMPOUNDS ARE DESCRIBED. THE COMPOUNDS CAN BE GENERICALLY DESIGNATED AS N-((3,5-DILOWER ALKYL-4-HETEROCYCLIC)METHYL)PHTHALIMIDES AND DERIVATIVES OF THE AROMATIC RING THEREOF.

Pyrazolo(3,4d) pyrimidines

ARYL PYROLES, THE PROCEDURE FOR THEIR PREPARATION AND THEIR USE AS PESTICIDE COMPOUNDS.

4-thiouracil compounds as fog inhibitors

4-Thiouracil compounds, including novel 4-thiouracil compounds, are prepared by reacting ammonia or primary amine with novel adducts of an alkoxycarbonyl isothiocyanate and a tertiary enamine. The 4-thiouracil compounds are useful photographic fog inhibitors.

Condensn products of erythromycyl-amine with aldehydes - antibiotic erythromycin derivs active against gram negative and gram positive bacteria

DERIVATIVES OF AMIDES AND PROCEDURE FOR THEIR PREPARATION.

Se describe un procedimiento para preparar una amida ópticamente activa de la fórmula general (Ver Fórmula); o una sal farmacéuticamente aceptable de la misma, donde X representa -N- o -CH-, R representa un grupo arilo o heteroarilo mono- o bicíclico, R1 es un radical arilo o heteroarilo, R2 es hidrógeno o alquilo inferior, R3 es hidrógeno, un grupo alquilo de 1 a 10 átomos de carbono, cicloalquilo de 3 a 12 átomos de carbono, ciclo-alquil-alquilo inferior, aril o arilalquilo inferior o R2 y R3 junto con el átomo de nitrógeno al cual ambos están unidos, representan un anillo heterocíclico saturado, que puede contener un heteroátomo adicional, el procedimiento comprende condensar un aldehído de la fórmula (Ver Fórmula); (donde R1 y R2 y R3 son como se definen anteriormente) con una amina de la fórmula (Ver Fórmula); (donde X y R son como se definen anteriormente).

Patent JPS6224428B2

Pesticidal 1-arylpyrroles

Substituted-1-arylpyrrole compounds of general formula (I) below, are useful as pesticides, in particular for the control of insects, arachnids, and nematodes. Processes to make the compounds and intermediates used for their preparation are described. Additionally, compositions containing the compounds and methods of use therefore are provided. Preferred compounds are the compounds of general formula (I) ##STR1## wherein typically preferred substituents are: X is halogen or a group R 5 S(O) n , in which n is 0, 1, or 2 and R 5 is CH 3 , CF 3 , CCl 3 , CF 2 Cl, CFCl 2 , CF 2 Br, CHF 2 , CHCl 2 or CHClF; R 1 is H, F, Cl, Br, OCH 3 , SCH 3 , or CH 3 optionally substituted; R 2 is CN; R 3 is H, F, Cl, Br, OCH 3 , or CH 3 optionally substituted; Y is CF 3 , CF 3 O, H, F, Cl or Br; X 1 and X 4 are individually H, F, Cl, Br, CH 3 , OCH 3 or SCH 3 ; and X 2 and X 3 are each H.

Pyrimidine derivatives

ABSTRACT OF THE DISCLOSURE This invention provides 2,4-diamino-5-thiobenzyl pyrimidines of the formula wherein R denotes hydrogen, an alkyl group, a lower alkoxy group or a halogen atom and R' denotes an alkyl group. The invention provides such novel pyrimidine derivatives, processes for the preparation thereof, pharmaceutical compositions containing them, their use in pharmacy and their pharmacologically acceptable acid addition salts.

A procedure for preparing substituted benzoic acid dimetilsulfoxidos and dimetilsulfonas. (Machine-translation by Google Translate, not legally binding)

A method of preparing dimethylsulfoxide and dimethylsufones of substituted benzoic acid of formula (IX) **(See formula)** where R1 is one or more alkoxy groups, preferably containing 1 to 4 carbon atoms (eg methoxy, ethoxy, n-propoxy, t-butoxy), R2 is an optional substituent, such as a halogen atom, especially chlorine, bromine or iodine, an alcohol group, preferably containing from 1 to 4 carbon atoms (eg, methyl, ethyl, propyl or butyl), an amido group or an amino group, and n is 1 or 2, which comprises making react a benzoic acid derivative of formula (VIII) **(See formula)** where R1 and R2 are as defined above and R is an alcohol group preferably having 1 to 4 carbon atoms, with a compound of formula (VII) CH3.SOn.CH3 (VII) where n is 1 or 2, in the presence of a base, strong enough to provide the appropriate carbanion in a suitable amount, for the reaction. (Machine-translation by Google Translate, not legally binding)

PROCESS FOR PREPARING 4-HYDROXY- AND 4,6-DIHYDROXY-PYRAZOLO SQUARE CLAMP TO 3,4-D SQUARE CLAMP TO PYRIMIDINES

Process for preparing 2-(aminomethylidene)-4,4-difluoro-3-oxobutyric esters

The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters, 2-(aminomethylidene)-4,4-difluoro-3-oxobutteric esters of the formula (I) in which R 1 , R 2 and R 3 independently of one another are C 1 -C 6 -alkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -alkenyl, C 3 -C 10 -cycloalkyl or benzyl or NR 2 R 3 is a 5- to 10-membered heterocyclic radical, to a process for preparing compounds of the formula (I) wherein an appropriate 3-aminoacrylic ester is reacted with difluoroacetyl fluoride and to the use of compounds of the formula (I) in the process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.

Merocyanine derivatives for cosmetic use

The use is described of merocyanine derivatives of formula (1), wherein R 1 and R 2 are each independently of the other hydrogen; C 1 -C 22 alkyl; cyclo-C 3 C 8 alkyl; or unsubstituted or C 1 -C 5 alkyl- or C 1 -C 5 alkoxy-substituted C 6 -C 20 aryl; orl; or R 1 and R 2 together with the nitrogen atom linking them form a —(CH 2 ) m — ring which is uninterrupted or, interrupted by —O— or by —NH—; R 3 is a cyano group; —COOR 5 ; —CONHR 5 ; —COR 5 ; or —SO 2 R 5 ; R 4 is a cyano group; —COOR 6 ; —CONHR 6 ; —COR 6 ; or —SO 2 R 6 ; R 5 and R 6 are each independently of the other C 1 -C 22 alkyl; or unsubstituted or C 1 -C 5 alkyl substituted C 6 -C 20 aryl; or R 3 and R 4 together or R 5 and R 6 together form in a 5- to 7-membered, monocyclic, carbocyclic or heterocyclic ring; Z 1 , and Z 2 are each independently of the other a —(CH 2 ) n — group which is uninterrupted or interrupted by —O—, —S—, or by —NR 7 —, and/or is unsubstituted or substituted by C 1 -C 5 alkyl; R 7 is (C l C 5 alkyl; 1 is from 1 to 4; m is from 1 to 7; n is from 1 to 4; when n=2, R 1 , R 5 or R 6 is a bivalent alkyl group; or R 1 , and R 2 together with the 2 nitrogen atoms linking them form a —(CH 2 ) m — ring; when n=3, R 1 , R 5 or R 6 is a trivalent alkyl group; when n=4, R 1 , R 5 or R 6 is a tetravalent alkyl group; and R 1 , and R 2 in formula (1) are not simultaneously hydrogen, in protecting human and animal hair and skin from UV radiation.

Synthesis of substituted 2,4-diamino-5-benzylpyrimidine and sulphone intermediates therefor

Patent FR2212147A1

Derivatives of 1, 4-bismethylene cyclohexane and 1, 4-bismethylene cyclohexadiene and processes of preparation

Cosmetic preparation comprising merocyanine derivatives

Preparación cosmética que comprende al menos uno o más compuestos de fórmulaoen las queR1 y R2 son, cada uno independientemente del otro, hidrógeno; alquilo C1-C22; ciclo-alquilo C3-C8; o arilo C6-C20 no sustituido o sustituido con alquilo C1-C6 o alcoxilo C1-C6; o R1 y R2 junto con el átomo de nitrógenoque los une forman un anillo -(CH2)m que contiene nitrógeno que no está interrumpido o está interrumpidopor -O- o por -NH-;R3 es un grupo ciano; -COOR5; -CONHR5; -COR5; -SO2R5; o -CONR1R5;R4 es un grupo ciano; -COOR6; -CONHR6; -COR6; -SO2R6; o -CONR2R6;R5 y R6 son, cada uno independientemente del otro, alquilo C1-C22; ciclo-alquilo C3-C8; 20 o arilo C6-C20 nosustituido o sustituido con alquilo C1-C6;o R3 y R4 juntos o R5 y R6 juntos forman un anillo monocíclico, carbocíclico o heterocíclico de 5 a 7miembros;R8 es hidrógeno; alquilo C1-C22; o arilo C6-C20 no sustituido o sustituido con alquilo C1-C5 o alcoxilo C1-C5;R9 es un grupo ciano; -COOR11; -CONHR11; -COR11; o -SO2R11;R10 es un grupo ciano; -COOR12; -CONHR12; -COR12; o -SO2R12;R11 y R12 son, cada uno independientemente del otro, alquilo C1-C22; o arilo C6-C20 no sustituido o sustituidocon alquilo C1-C5;o R11 y R12 juntos forman un anillo monocíclico, carbocíclico o heterocíclico de 5 a 7 miembros;Z1 y Z2 son, cada uno independientemente del otro, un grupo -(CH2)l- que no está interrumpido o estáinterrumpido por -O-, -S- o por -NR7-, y/o no está sustituido o está sustituido con alquilo C1-C6;R7 es alquilo C1-C5;I es desde 1 hasta 4;m es desde 1 hasta 7;n es desde 1 hasta 4;cuando n >= 2. Cosmetic preparation comprising at least one or more compounds of formulao in which R1 and R2 are, independently of each other, hydrogen; C1-C22 alkyl; C3-C8 cyclo-alkyl; or C6-C20 aryl unsubstituted or substituted with C1-C6 alkyl or C1-C6 alkoxy; or R1 and R2 together with the nitrogen atom that binds them together form a ring - (CH2) m containing nitrogen that is not interrupted or interrupted by -O- or by -NH-; R3 is a ...

New phenylacetic acid esters, their production and compositions containing them

The invention comprises 2-alkoxy-ethyl a -phenyl-a -piperidino acetates, their acid addition salts, and the preparation thereof by reacting a 2-alkoxy ethyl ester of an a -phenyl-a -halogeno-acetic acid with piperidine in the presence of a binding agent for hydrogen halide. 2 - n - Butoxy - ethyl a - phenyl - a - chloro - acetate is prepared from 2-n-butoxyethanol and a -phenyl-a -chloroacetic acid chloride.ALSO:Therapeutic compositions, particularly cough-relieving compositions, comprise a 2-alkoxyethyl a -phenyl-a -piperidinoacetate or an acid addition salt thereof, particularly a hydrochloride or hydrobromide, with a pharmaceutically acceptable diluent.

Benzylpyrimidine derivatives

1449387 Benzylpyrimidines F HOFF- [8 Nov 1973 (2)] 48425/74 Heading C2C [Also MANNLA ROCHE & CO AG 8 Nov 1974 in Division A5] Novel compounds of Formula I wherein R<SP>1</SP> and R<SP>3</SP> are C 1-4 alkyl, R<SP>3</SP> is halogen, A is O attached to ring N and n is 0 or 1 are prepared by one of the following methods (a) guanidine is reacted with a compound of Formula IIa or IIb wherein R<SP>4</SP> is C 1-6 alkyl or both R 4 link to give C 1-6 alkylene and R<SP>5</SP> is a leaving group; (b) reacting ammonia with a compound of Formula III wherein X is Cl, Br alkylmercapto alkylsulphonyl or one may be amino; (c) reductively removing X<SP>1</SP> from a compound of Formula IV wherein X<SP>1</SP> is Cl, Br or OH; or (d) subjecting a compound of Formula I above where n = 0 to N oxidation. Intermediates are prepared as in divisional Specification 1,449,388.

4-Homoisotwistane-aminoacid amides and pharmaceutical compositions containing same

4-Homoisotwistane-aminoacid amides having the for mula wherein a is 0 or 1, R 1 is hydrogen or lower alkyl, A is lower alkylene or lower alkylidene, and R 2 and R 3 , which can be the same or different, are hydrogen, lower alkyl, cycloalkyl, benzyl or substituted benzyl, or is a saturated heterocyclic ring, acid addition salts thereof and pharmaceutical compositions containing same, possess anti-viral activity and reduced activity on the central nervous system.

Patent DE2650961C2

AROMATIC AND NITROGEN DERIVATIVES OF ACETAMIDE, THEIR PREPARATION AND THEIR THERAPEUTIC USE AS ANTIARRHYTHMICS

Dérivés aromatiques et azotés de l'acétamide, leur préparation et leurs utilisations thérapeutiques. Ces composés répondent à la formule : Aromatic and nitrogen derivatives of acetamide, their preparation and therapeutic uses. These compounds correspond to the formula:

Amino acrylates

2-fluorinated acyl-3-aminoacrylonitrile derivative and method for producing the same

PROCESS FOR THE PREPARATION OF ANTI-BACTERIALLY ACTIVE PHARMACEUTICAL PREPARATIONS AND PROCESS FOR THE PREPARATION OF 5-BENZYL-2,4-DIAMINOPYRIMIDINE DERIVATIVES SUITABLE FOR USE

1-arylpyrroles, pesticidal agent in which said compounds are comprised and method of fighting plant pest by making use of the compounds

Substituované 1-arylpyrroly obecného vzorce II, kde typicky X představuje halogen nebo skupinu obecného vzorce R.sup.5.n.S(O).sub.n.n., kde n znamená číslo 0, 1 nebo 2 a R.sup.5 .n.představuje CF.sub.3.n., CCl.sub.3.n., CF.sub.2.n.Cl, CFCl.sub.2.n., CF.sub.2.n.Br, CHF.sub.2.n., CHCl.sub.2 .n.nebo CHClF; R.sup.1 .n.znamená vodík, brom, SCH.sub.3.n., popřípadě substituovanou methylskupinu nebo alkoxyalkylidenimino; R.sup.2 .sup..n.znamená kyanoskupinu; R.sup.3 .n.znamená vodík, chlor nebo popřípadě substituovanou methylskupinu; Y znamená trifluormethylskupinu nebo chlor; každý ze symbolů X.sup.1 .n.a X.sup.4 .n.znamená chlor a X.sup.2 .n.a X.sup.3 .sup..n.znamenají atomy vodíku, jsou užitečné jako pesticidy, zejména pro potlačování hmyzu, pavoukovců a nematodů. Dále jsou popsány způsoby výroby těchto sloučenin a meziproduktů a také pesticidní prostředky na bázi těchto účinných sloučenin.ŕ Substituted 1-arylpyrroles of the general formula II wherein X is typically halogen or a group of the general formula R 5 is (5) S (O) sbnn where n is 0, 1 or 2 and R 5 is n. is CF 3, CCl 3, CF 3, Cl, CF 3, CF 3, Br, CHF. sub.2, CHCl3, or CHClF; R5 is hydrogen, bromo, SCH3, optionally substituted methyl or alkoxyalkylidenimino; R &lt; 2 &gt; is a cyano group; R5 is hydrogen, chloro or optionally substituted methyl; Y is trifluoromethyl or chloro; each X.sup.1 for X.sup.4 is a hydrogen atom and is useful as a pesticide, especially for the X.sup.4. suppression of insects, arachnids and nematodes. Further disclosed are methods for making such compounds and intermediates, as well as pesticidal compositions based on these active compounds

3-Amino-2-benzoyl-acrylic-acid derivatives and process for their preparation

3-Amino-2-benzoyl-acrylsäurederivate der Formel I <IMAGE> in der R¹, R², R³, X, X¹, X², und X³ die in der Beschreibung angegebene Bedeutung haben, werden hergestellt, indem man Benzoylhalogenide der Formel II mit 3-Aminoacrylsäurederivaten der Formel III umsetzt. <IMAGE> Die Verbindungen der Formel I sind Zwischenprodukte für die Herstellung antibakterieller Arzneimittel. 3-Amino-2-benzoyl-acrylic acid derivatives of the formula I <IMAGE> in which R¹, R², R³, X, X¹, X², and X³ have the meaning given in the description are prepared by adding benzoyl halides of the formula II with 3 -Aminoacrylic acid derivatives of the formula III. <IMAGE> The compounds of formula I are intermediates for the manufacture of antibacterial drugs.

PROCEDURE FOR THE PREPARATION OF CERTAIN STATED N-SUBSTITUTED BETA-AMINO-ALFA-BENZYLACRYLNITRILE DERIVATIVES

Patent DK135534C

2,2'-bis (dicyclopentylphosphino) -1,1'-binaphthyl and metal complexes thereof.