Способ получения замещенных аминокетонов или соответствующих аминоспиртов

Substd. (meth)acrylamide prodn. from alkyl (meth)acrylate and amine - using di:alkyl tin oxide and alkyl titanate catalyst to suppress michael addn.

In the prodn. of N-substd. (meth)acrylamides (I) by reacting alkali (meth)acrylates (II) with aliphatic or aromatic amines (III) at 50-180 deg.C, using a dialkyl Sn oxide (IV) as catalyst, as in DE2816516, an alkyl titanate (V) is also used as catalyst. (IV) catalyses aminolysis of the ester gp. and suppresses Michael addn. of (III) to the double bond of (II). (V) causes further, synergistic suppression of the formation of Michael adduct (VI), e.g. the addn. of 1% (V) reduces (VI) formation from 5-10% to 1% and increases the (I) yield to 98%, whereas the use of 1% (V) alone give 20% (VI) and 80% (I).

Verfahren zur Herstellung von neuen stickstoffhaltigen, als Textilhilfsmittel geeigneten, kationenaktiven Kondensationsprodukten

Verfahren zur Herstellung von ungesaettigten Acylaminomethyl-aminen

AMINO PROPANOL DERIVATIVES, PROCEDURES FOR THEIR PRODUCTION, USE THE SAME AND THESE CONTAINING DRUGS.

ANTI-CHOLINERGIC CONNECTIONS, PHARMACEUTICAL COMPOSITIONS AND TREATMENT PROCEDURES.

PROCEDURE FOR THE PRODUCTION OF ANTI-OXIDIZING AMIDES.

N-ACYL-2-ARYLCYCLOPROPYLMETHYLAMIN-DERIVATE AS MELATONERGI MEANS

Procedure for the production of Alkylenglykol di (acrylamide N methyl) - ethers

ANTICHOLINERGIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHOD OF TREATMENT

PROCESS FOR THE PREPARATION OF ANTIOXIDANT AMIDES

An inexpensive and nonhazardous process for the preparation of an amide wherein an organic acid reacting with an aryl amino to form an intermediate hydroxy aryl amide and then dehydrating the hydroxy aryl amide to form a ?, .beta. unsaturated amide.

POLYHYDROXYBENZOIC ACID DERIVATIVES

The present invention provides polyhydroxy-substituted benz-, phenylacet- and mandelamidines, amidates, amidoximes and hydroxyamidoximes-ribonucleotide reductase inhibitors, and free radical scavengers, of the general formula (I) wherein n is 2-5, m is 0 or 1, R' is NOH or NH, R is NH2 or NHOH when R' is NOH, R is NH2 or O-C1-3 alkyl when R'is NH, and R" is H or OH; and pharmaceutically acceptable acid addition salts thereof. These compounds are useful in the treatment of disease conditions involving excess free radical formation in the body, or in the treatment of certain neoplasms.

AMPHIPHILE LIPIDIC COMPOSITIONS, PROCESS FOR THEIR PREPARATION AND USES, PARTICULARLY AS COSMETICS AND IN DERMATOLOGY

COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS

Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides, such as rhGH. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration, are provided, and methods of preparation of the modified amino acid compound are provided.

COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS

Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides, such as rhGH. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration, are provided, and methods of preparation of the modified amino acid compound are provided.

NOVEL POTENT INDUCERS OF TERMINAL DIFFERENTIATION AND METHODS OF USE THEREOF

The present invention provides the compound having structure (I), wherein ea ch of R1 and R2 are independently the same as or different from each other; whe n R1 and R2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiazoleami no group; when R1 and R2 are different, R1 = R3-N-R4, wherein each of R3 and R4 are independently the same as or different from each other and are a hydroge n atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranch ed alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridi ne group, or R3 and R4 bond together to form a piperidine group and R2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8. The present invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. Moreove r, the ...

Verfahren zur Herstellung eines neuen N-Polyoxy-alkylaminderivats.

Verfahren zur Herstellung eines neuen N-Polyoxy-alkylaminderivats.

Verfahren zur Herstellung eines neuen N-Polyoxy-alkylaminderivats.

Verfahren zur Herstellung eines neuen N-Polyoxy-alkylaminderivats.

Verfahren zur Herstellung eines neuen N-Polyoxy-alkylaminderivats.

Verfahren zur Herstellung von basischen Amiden

Verfahren zur Herstellung von basischen Amiden

Verfahren zur Herstellung stickstoffhaltiger Kondensationsprodukte

Verfahren zur Herstellung stickstoffhaltiger Kondensationsprodukte

Verfahren zur Herstellung stickstoffhaltiger Kondensationsprodukte

Verfahren zur Herstellung stickstoffhaltiger Kondensationsprodukte

Verfahren zur Herstellung stickstoffhaltiger Kondensationsprodukte

Verfahren zur Herstellung stickstoffhaltiger Kondensationsprodukte

Procédé de préparation de nouveaux agents tensio-actifs

Procédé d'obtention du N-cinnamoyl-P-aminophénol

Composition à activité superficielle

Stabile wässrige Dispersion von selbstvernetzenden Mischpolymerisaten

Verfahren zur Herstellung von unsymmetrischen Methylen-bis-Carbonsäureamiden

Verfahren zur Herstellung von Alkylenglykol-di(-acrylamid-N-methyl)-äthern

Verfahren zur Herstellung von 2,5-Diacylamino-3,6-diamino-1,4-benzochinonen

Verfahren zur Herstellung von perfluorierten polyamiden Polymeren

BASIC SUBSTITUTED ANTHRACHINONE AND DIHYDROANTHRACHINONE, YOUR PRODUCTION AND PHARMACEUTICAL PREPARATIONS.

THE AMPHIPHILIC LIPID COMPOUNDS, PROCESS FOR THEIR PREPARATION AND THEIR USES, ESPECIALLY IN COSMETICS AND DERMOPHARMACY.

ESTER A-BISABOLOLIQUE D'ACIDE FARNESYL-CARBOXYLIQUE, AGENT DE STABILISATION DES MUQUEUSES, ET PROCEDE POUR SA FABRICATION

Ce composé de la formule III ci-après est un nouvel agent de stabilisation des muqueuses qui présente des activités antiinflammatoires et anti-ulcérantes. Il est synthétisé par estérification de l'acide farnésyl-carboxylique ou de ses dérivés avec l' alpha -bisabolol ou ses dérivés. Ce composé est particulièrement intéressant dans le traitement de l'ulcère gastrique.

LEUCO-ANTHRAQUINONES ET LEURS FORMES TAUTOMERES, LEURS PROCEDES DE PREPARATION ET LEUR UTILISATION POUR LUTTER CONTRE LES MALADIES CANCEREUSES

L'invention concerne des nouveaux composés chimiques, répondant à la formule générale suivante : ...

PROCEEDED OF PREPARATION OF NR, N-DIALKYLAMIDES Of ACIDS MONOCARBOXYLIQUES HAS NON-SATURATION ALPHA, BETA-OLEFINIQUE

NOVEL AMPHIPHILIC LIPID COMPOUNDS, PROCESS FOR THEIR PREPARATION AND THEIR APPLICATIONS, PARTICULARLY IN COSMETICS AND DERMOPHARMACY

Pentafluorocinnamic acid anilides immunosuppressives

(A) Aminoalkylthio- and aminoalkoxy-(2,3,4,5,6-pentafluorophenyl)acryloylanilides of general formula (I): R and R1=H, lower alkyl (max. C7) or aralkyl pref. phenyl-lower alkyl opt. substd. by 1 or 2 halogen, lower alkyl, lower alkoxy or amino; X= -O- or -S-. (B) Salts such as acid addition salts of (I) with inorganic and organic acids and quaternary ammonium salts. (I) have immunosuppressive activity and may be used to prevent transplant rejection of organs or skin in dogs and mice or the suppression of antibody reaction in mice after injection of red blood cells of sheep.

ACYL DERIVATIVES OF SUBSTITUTED BIS-ARYLALKLAMINES

Process for the production of naked, nu'- (alpha, Omega-dihydroxyalcoylène) - (a)-carboxamides

ALKANOLAMINE DERIVATIVES

PRODUCTION OF ALKYLENE GLYCOL DI?(ACRYLAMIDE?N? METHYL) ETHERS

ANTICHOLINERGIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHOD OF TREATMENT

A compound having formula (I), wherein R1 is the esterification residue of an alcohol (R1-OH) having from 1 to 8 carbon atoms; R2 is a substituted or unsubstituted aryl, cycloalkyl or alkyl group having from 1 to 8 carbon atoms; R3 is H or R2; n is an integer from 0 to 4; X is (II), (III), (IV), (V), (VI), (VII) or (VIII); m is an integer from 0 to 4; R4 is an 8-aza-bicyclo[3.2.1]octane residue or its 6,7-epoxy derivative, (IX) or (X), ortho, meta- or para- substituted alkyl pyridine, (XI) or (XII). The esters are prepared in two steps to the tertiary compounds and in three steps to the quaternary compounds from the phenylmalonic acid. Provided are anticholinergic compounds which exhibit anticholinergic properties and which induce mydriasis as well as pharmaceutical compositions and methods of treatment embodying those compounds which are more effective and less toxic than those presently available.

PREPARATION OF N,N-DIALKYLACYLAMIDES

Preparation of methacrylamides

An improved process for the preparation of methacrylamides from primary amines, methacrylic esters, and base catalysts such as alkoxides and amides. Some products are obtained in the form useful as comonomers in the preparation of elastomers.

N-PERFLUOROALKANOYLAMINO-AND N- PERFLUOROALKANOYLAMINOALKYL ACRYLAMIDES

Stable aqueous dispersions of cross-linking copolymers and process for the production thereof

The invention comprises unsaturated amines of formula in which Y represents the group -OH, -COOH, -COO Me, -SO3H, -SO3Me, , -CH = CH2, or -O-[-(CH2)n-O]z-H, where Me is a metal atom or the ammonium radical, R1 and R11 are saturated aliphatic or cycloaliphatic hydrocarbon radicals containing 1 to 7 carbon atoms, aralkyl radicals or aryl radicals, n is 1 to 4 and z is 1 to 25, x is 1 to 20, R1 and X are hydrogen atoms or saturated aliphatic or cycloaliphatic hydrocarbon radicals containing 1 to 7 carbon atoms, and R2 is a hydrogen atom, a saturated aliphatic, cycloaliphatic, aralkyl, or aryl radical, having 1 to 12 carbon atoms, or the group -(CH2)x-Y where x and Y are as above. The unsaturated amines are prepared by reacting together at 30 DEG to 100 DEG C. an unsaturated carboxylic acid amide of formula where X and R1 are as above, with formaldehyde and an amine of formula where Y, x and R2 are as above. Compounds ...

NEW AMPHIPHILIC LIPID COMPOUNDS

Basically substituted amides and a process for preparing them

The invention comprises compounds of the formula: (wherein R is an a , b -unsaturated aliphatic group with 4 to 9 carbon atoms which may contain further double linkages or an aromatic group, or a furyl or thienyl radical or an a , b -unsaturated aralkenyl group; R1 is an alkyl radical of 1 to 4 carbon atoms; R2 is a hydroxy group or an alkoxy group of 1 to 4 carbon atoms; A is an alkylene radical of 2 to 4 carbon atoms; and R3 and R4 are alkyl radicals each containing 1 to 4 carbon atoms or -NR3R4 is a 5- or 6-membered saturated heterocyclic ring which may contain an oxygen atom) and their acid-addition salts; and their preparation by reacting the appropriate acid R.COOH or a reactive funtional derivative thereof with the appropriate amine. The radical R may contain halogen atoms or hydroxy, acyloxy or alkoxy groups as substituents. Examples are given and a list of salt-forming organic and inorganic acids is provided. 2-(m-methoxyphenyl) -2- dimethylaminopropylbutylamine ...

NEW POTENT INDUCTORS OF THE TERMINAL DIFFERENTIATION AND METHODS OF YOUR USE

HOMOBIFUNKTIONELLE AGENTS TO THE CLUTCH OF ENZYMES UN THEIR SIMILAR ONE TO ANTIBODIES AND THEIR SIMILAR ONE

VERFAHREN ZUR HERSTELLUNG VON NEUEN ANTHRA- CHINONDERIVATEN, IHREN TAUTOMEREN FORMEN UND PHARMAKOLOGISCH ANNEHMBAREN SAEUREADDITIONS- SALZEN

TEXTILE TREATMENT MEANS.

NEW ONES NAPHTALENE AND INDANDERIVATE, THESE CONNECTIONS CONTAINING DRUGS AND PROCEDURES FOR THEIR PRODUCTION.

Procedure for the production of 2,5-Diacylamino-3,6-diamino-1,4-benzochinonen

Acrylamide-Based Crosslinking Monomers, Their Preparation, And Uses Thereof

A process for preparing an acrylamide-based crosslinking monomer comprising reacting in the presence of a catalyst an isocyanate compound containing at least two isocyanate groups with one of acrylic acid or methacrylic acid. These acrylamide-based crosslinking monomers are used in the preparation of coating compositions, adhesive compositions curable by applying thermal or radiation energy, and in the preparation of cation or anion exchange membranes.

ACYL DERIVATIVES OF SUBSTITUTED BIS-ARYL ALKYL AMINES

ANTICHOLINERGIC COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHOD OF TREATMENT

A compound having the formula - - - - (I) Wherein: R1 is the esterification residue of a pharmaceutically acceptable non-toxic, substituted or unsubstituted, straight cyclic or branched chain alcohol (R1-OH) having from 1 to 8 carbon atoms such that the ester group, COOR1, is metabolically hydrolyzable to the free alcohol, R1-OH, and a non-toxic metabolite of said compound following administration thereof to a human or non-human animal; R2 is a substituted or unsubstituted aryl, cycloalkyl or alkyl group having from 1 to 8 carbon atoms; R3 is H or R2; n is an integer from 0 to 4; X is ; , wherein R8 is H or straight or branched chain alkyl having from 1 to 5 carbon atoms; ; , wherein R9 and R10 may be the same or different and may be H or lower alkyl having from 1 to 5 carbon atoms; ; or ; m is an integer from 0 to 4; R4 is or , wherein R5 and R6 may be the same or different and are alkyls having from 1 to 5 carbon atoms; ...

New asymmetrical amides of acids methylene-(a)-carboxylic and proceeded for their preparation

PROCEEDED OF PREPARATION OF NR, N-DIALKYLAMIDES Of ACIDS MONOCARBOXYLIQUES HAS NON-SATURATION ALPHA, BETA-OLEFINIQUE

New nitrogenized products of condensation, proceeded for their preparation and their use

New hydroaromatic compounds

LEUCO ANTHRAQUINONES AND THEIR TAUTOMERIC FORMS, PROCESSES FOR THEIR PREPARATION AND THEIR USE IN THE CONTROL OF DISEASES CANCER

PREPARATION OF OLEFINICALLY UNSATURATED N,N-DIALKYLAMIDES AND THEIR USE

PROCESS FOR PREPARING AROMATIC AMIDE ANTIOXIDANTS

A process for the preparation of aromatic amide antioxidants from a simple aliphatic or aromatic ester and primary amine in the presence of a metal alkoxide and an alcohol. Unsaturated products produced using this process are sufficiently pure to use as comonomers in the preparation of elastomers.

PENTAFLUOROCINNAMANILIDE DERIVATIVES

POLYMERISABLE COMPOUNDS WITH AN IONIC STRUCTURE

Verfahren zur Herstellung von 2, 5-Diacylamino-3, 6-diamino-benzochinonen-1, 4

New amphiphilic lipid compounds

Amphiphilic lipid compound having the formula: (I) in which: R1 denotes a C7-C21 alkyl or alkenyl radical, R2 denotes a saturated or unsaturated C7-C31 hydrocarbon radical, COA denotes a group chosen from the following groups: a) COOM, M being H, Na, K, NH4 or a substituted ammonium ion derived from an amine, b) B being a radical derived from mono- or polyhydroxylated primary or secondary amines and R denoting a hydrogen atom or a methyl, ethyl or hydroxyethyl radical, c) Q denoting a substituted aminoalkyl or ammonioalkyl radical and R having the meaning indicated for b), and d) COOZ, Z representing the residue of a C3-C7 polyol, and a process for its preparation. Cosmetic or dermopharmaceutical composition comprising the said compound and especially an aqueous dispersion of liposomes.

Improvements in or relating to polyfunctional compounds and polymers modified with said compounds

The invention comprises compounds of the formulae where X is CO or SO2; A is divalent acyclic aliphatic of at least 3 carbon atoms; D is alkylene or substituted alkylene of 3 or 4 carbon atoms; R2 is hydrogen, C1- 5 alkyl or hydroxymethyl; R3 is C1- 5 alkyl; Z and Z1 are CH2 = CR-, QCH2CHR- or R1OCH2CHR-, where R and R1 are hydrogen or C1- 5 alkyl and Q is (a) the radical corresponding to a conjugate base of a Lowry-Bronsted acid of dissociation constant in water between 5 x 10-2 and 5 x 10-5, or (b) the residue of a tertiary ammonium cation; and NYN in the last formula above is the residue of a cyclic bis-secondary amine; and in the last formula above, when Z is R1OCH2CHR-, then Z1 is CH2=CHR- or QCH2CHR-. The radical A includes alkylene, alkenylene, polyoxyethylene, polyoxypropylene and hydroxyalkylene; NYN includes piperazines, pyrazolidines, and 1,4-bis-alkylaminocycloalkanes; Q includes -OSO3M, -SSO3M, -OCOCH3, -OCOH, -OCOC2H5, pyridinium and benzyldimethylammonium ...

ANTHRAQUINONE DERIVATIVES

ACYL DERIVATIVES OF SUBSTITUTED BIS-ARYLALKLAMINES

... 1332930 Acyl derivatives DEUTSCHE GOLDUND SILBER-SCHEIDEANSTALT 18 Dec 1970 [18 Dec 1969] 60193/70 Heading C2C The invention comprises acyl derivatives of the formula in whieh Ar is phenyl or naphthyl; X is O or OH plus. H; Y is optionally substituted C 1-4 alkylene; R1 is acyloxy, acyloxyalkoxy, aeylamino, or -N(alkyl)acyl; R4 is H or C 1-6 alkyl; R5 is H, C 1-6 alkyl or acyl; and R2, R3, R6 and R? each are H, halogen, OH, C 1-6 alkoxy, acyloxy, amine, alkylamino, dialkylamino, acylamino, NO 2 , C 1-6 alkyl, C 1-6 haloalkyl or C 1-6 alkylthio, and acid addition salts thereof. Compounds of the above Formula I in which X is O are prepared by reacting ketones of the Formula II with amines of the Formula VII wherein W is -NHR5, in the presence of formaldehyde or formaldehyde donors, or by reacting compounds of the formula or in which R8 and R9 each are C 1-6 alkyl or together with the N atom to which they are ...

PROCEDURES FOR THE PRODUCTION OF NEW ANTHRA CHINONDERIVATEN, ITS TAUTOMEREN FORMS AND PHARMAKOLOGISCH ACCEPTABLE ONE SAEUREADDITIONS SALTS

NICHTIONI SURFACE ACTIVE CONNECTIONS AND PHOTOGRAPHIC MATERIALS, IT CONTAINING.

PROCEDURE FOR THE PRODUCTION OF NEW OF SUBSTITUTING BENZOCYCLOALKENYLALKANE

AMINO ACID DERIVATIVES AND THEIR PROCEDURES FOR THE PRODUCTION.

PROCEDURE FOR THE PRODUCTION OF NEW OF SUBSTITUTING BENZOCYCLOALKENYLALKANE

Compounds and compositions for delivering active agents

AMINO ANTHRAQUINONES AND THEIR LEUCO-FORMS, AND USE TO INHIBIT CANCERS

NOVEL POTENT INDUCERS OF TERMINAL DIFFERENTIATION AND METHODS OF USE THEREOF

FLUORINATED PENTENE DIAMINE DERIVATIVES

PERFLUOROALKYLMALEINAMIDES AND PERFLUOROALKYLFUMARAMIDES

PURIFICATION OF METHACRYLAMIDOPROPYLTRIMETHYLAMMONIUM CHLORIDE

ETHOXYLATED AMINE COMPOUNDS HAVING CLAY SOIL REMOVAL/ANTI-REDEPOSITION PROPERTIES USEFUL IN DETERGENT COMPOSITIONS

ALKANOLAMINE DERIVATIVES

NOVEL COMPOUNDS AMPHIPHILIC LIPID, PROCESS FOR THEIR PREPARATION AND USES THEREOF, PARTICULARLY IN COSMETICS AND DERMOPHARMACEUTICAL

Pentafluorocinnamic acid anilides immunosuppressives

PROCEEDED OF PREPARATION Of ACRYLAMIDES AND METHACRYLAMIDES SUBSTITUTE FOR NITROGEN

METHOD FOR MODIFYING DERIVATIVES OF AMINO ACIDS AND PEPTIDES, COMPOUNDS PRODUCED, AND USE

The invention relates to a novel method for modifying hydroxylated cyclic amino acids, especially 4-hydroxyproline, which is a commercial, relatively cheap, natural amino acid, in order to provide other amino acids of high optical purity. The initial step of the process is a free-radical excision, and the excision product converts itself into non-proteinogenic amino acids by means of reactions such as reduction, reductive amination, and Horner-Wadsworth-Emmons reactions. The method is characterised in that it is applicable to the selective modification of peptides. The invention also relates to the products of said method, such as amino acids that are N-alkylated and/or have side chains with groups of amino, hydroxyl, alkenyl etc., and to the peptidic derivatives thereof of interest as pharmaceuticals, catalysts, molecular imaging probes etc.

PROCESS FOR THE PREPARATION OF PROTECTED L-ALANINE DERIVATIVES

The present invention is directed to a novel process for the preparation of protected L-alanine derivatives, useful as intermediates in the synthesis of compounds useful as mu/delta opioid modulators. 2. The process as in claim 1 , wherein the oxidizing agent is selected from the group consisting of hydrogen peroxide claim 1 , LiOH and LiOOH.3. The process as in claim 2 , wherein the oxidizing agent is hydrogen peroxide.4. The process as in claim 1 , wherein the oxidizing agent is 30% hydrogen peroxide and is present in an excess amount.5. The process as in claim 1 , wherein the inorganic base is potassium carbonate.6. The process as in claim 1 , wherein the inorganic base is present in an amount in the range of from about 1.0 to about 3.0 molar equivalents.7. The process as in claim 1 , wherein the third organic solvent is DMSO.8. The process as in claim 1 , wherein the compound of formula (I-B) is reacted with the oxidizing agent at a temperature in the range of from about room temperature to about 60° C.9. A compound prepared according to a process as in . This application is a divisional of U.S. Ser. No. 12/606,730, filed Oct. 27, 2009, (now allowed), which is derived from and claims priority to U.S. Provisional App. No. 61/108,649, filed Oct. 27, 2008, the entire contents of each of which are incorporated by reference herein.The present invention is directed to a novel process for the preparation of protected L-alanine derivatives, useful as intermediates in the synthesis of compounds useful as mu/delta opioid modulators.The opioid receptors were identified in the mid-1970's, and were quickly categorized into three sub-sets of receptors (mu, delta and kappa). More recently the original three types of receptors have been further divided into sub-types. Also known is that the family of opioid receptors are members of the G-protein coupled receptor (GPCR) super-family. More physiologically pertinent are the well established facts that opioid receptors are found ...

DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE

Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved. 3. A compound according to claim 1 , wherein Z is a bond or —CH—.4. A compound according to claim 1 , wherein X claim 1 , Xand Xare each hydrogen.5. A compound according to claim 1 , wherein A is —CHCH—.6. A compound according to claim 1 , wherein Rand Rare independently hydrogen or methyl.7. A compound according to claim 1 , wherein Ris hydrogen or C-Calkyl.8. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable carrier.9. A method for treating a disease in a subject comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering to a subject an effective amount of a compound according to ; wherein the disease comprises eye disease.'}10. The method of claim 9 , wherein the eye disease comprises glaucoma or a neurodegenerative eye disease.11. A method of modulating kinase activity comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'contacting a cell with a compound according to in an amount effective to modulate kinase activity.'}12. The method of claim 11 , wherein the cell is in a subject.13. A method of reducing intraocular pressure comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'contacting a cell with a compound according to in an amount effective to reduce intraocular pressure.'}14. The method of claim 13 , wherein the cell is in a subject. This application is a continuation of U.S. patent application Ser. No. 13/768,594 filed Feb. 15, 2013 which is a divisional of U.S. patent application Ser. No. 12/ ...

Functionalized Graphene Barrier Element

Described herein are functionalized graphene compositions that have gas, fluid, and/or vapor resistant properties. Also described are barrier elements based on the aforementioned compositions. Also described is a barrier device that incorporates the barrier element and further comprises a substrate and a protective coating, encompassing the barrier element. 1. A graphene compound comprising an optionally functionalized graphene directly bonded to —NH—R—NHCOR′ or —CO—NH—R—NHCOR′;{'sub': '1-20', 'wherein R is optionally substituted Chydrocarbylene; and'}{'sub': 1-30', '3-30, 'R′ is optionally substituted Chydrocarbyl or Cheteroaryl.'}2. The compound of claim 1 , wherein the optionally functionalized graphene is a reduced graphene oxide.3. The compound of claim 1 , wherein the optionally functionalized graphene is a graphene oxide.4. The compound of claim 1 , having a molar ratio of nitrogen to carbon that is about 0.001 to about 0.2.5. The compound of claim 1 , having a molar ratio of nitrogen to carbon that is about 0.02 to about 0.1.6. The compound of claim 1 , having molar ratio of oxygen to carbon that is about 0.01 to about 1.7. The compound of claim 1 , having molar ratio of oxygen to carbon that is about 0.2 to about 0.8.8. The compound of claim 1 , further represented by a formula CHNO.9. The compound of claim 1 , wherein R is Calkylene.10. The compound of claim 1 , wherein R is Calkylene.11. The compound of claim 1 , wherein R is —(CH)—.12. The compound of claim 1 , wherein R′ is Calkyl.13. The compound of claim 1 , wherein R′ is —CH.14. A barrier element comprising a compound of claim 1 , wherein the barrier element is transparent.15. The barrier element of claim 14 , wherein the barrier element has a gas permeability of less than 0.100 cc/m-day.16. The barrier element of claim 14 , wherein the element has a moisture permeability of less than 10.0 gm/m-day.17. The barrier element of claim 14 , wherein the element has a transparency of at least about 80%.18. ...

NOVEL DRUG TARGET SITE WITHIN GP120 OF HIV

The present invention relates to a method of designing an inhibitor of the binding of HIV (human immunodeficiency virus) glycoprotein (gp)120 to a CD4-receptor or to the integrin alpha4 beta7 (a4b7). The inhibitor interacts with at least two amino acid residues comprised in six motifs within the 3-dimensional structure of gp120. Also provided are compounds, pharmaceutical compositions thereof and uses thereof in the development of an inhibitor of the binding of a HIV gp120 to a CD4-receptor or an integrin alpha4 beta7 (a4b7). The inhibitors are useful for the prevention or treatment of an HIV infection and/or diseases associated with an HIV infection. 1. A method of confirming that a known compound is an inhibitor of the binding of HIV (human immunodeficiency virus) glycoprotein (gp)120 to a CD4-receptor comprising(a) bringing into contact a HIV gp120 or a peptidomimetic reflecting the three-dimensional structure of said gp120 and the known compound; wherein a first motif of said six motifs comprises the amino acid sequence DIISLWDQSLKPCVKLT (SEQ ID NOS 3 (HIV-1) or 9 (HIV-2));', 'wherein a second motif of said six motifs comprises the amino acid sequence NVSTVQCTHGIRPVVSTQLLLNGSLAE (SEQ ID NOS 4 (HIV-1) or 10 (HIV-2)) and wherein the interaction with any amino acid residue of said second motif is with any one or more of residues 14-18 of SEQ ID NOS 4 (HIV-1) or 10 (HIV-2);', 'wherein a third motif of said six motifs comprises the amino acid sequence SGGDPEIVMHSFNCGGEFFYCN (SEQ ID NOS 5 (HIV-1) or 11 (HIV-2));', 'wherein a fourth motif of said six motifs comprises the amino acid sequence CPKISFEP (SEQ ID NOS 6 (HIV-1) or 14 (HIV-2));', 'wherein a fifth motif of said six motifs comprises the amino acid sequence FRPGGGDMRDNWRSELYKYKVV (SEQ ID NO: 7 (HIV-1)); and', 'wherein a sixth motif of said six motifs comprises the amino acid sequence CSS,', 'said gp120 of HIV comprising or consisting of:', '(i) the sequence of SEQ ID NO: 2;', '(ii) the sequence encoded by the ...

Patent FR2423482B1

Process for preparing aromatic amide antioxidants

TREAD FOR PNEUMATIC TIRE Abstract of the Invention A tread capable of being used in all seasons and weather conditions comprising of a substantially centrally located rib which extends circumferentially about the tire, a plurality of independent projections placed about the remaining portion of the tire. The independent projections are placed so as to provide for two circumferentially extending grooves, one on either side of the central rib and a plurality of laterally extending grooves which extend from each central groove to the tread edge of the tire. The tread has a low net to gross ratio.

Amides

Compounds having the formula <FORM:0833655/IV (b)/1> in which x is 1 or 4, y being 3 when x is 1 and 2 when x is 4, Z is a straight or branched C1-7 alkylene radical, and R and R1 are C1-7 alkyl groups, are prepared by reacting an octadecadienoic or octadecatrienoic acid of the formula <FORM:0833655/IV (b)/2> at a sub-normal temperature with an equimolar amount of a C1-7 alkyl chloroformate in presence of an equimolar amount of an aliphatic tertiary amine having C1-7 aliphatic radicals and further reacting the resulting intermediate acylalkyl carbonate with a dialkylaminoalkyl amine of the formula H2N-Z-NRR1.

Process of producing p-phenylene diamines

Patent FR2474028B1

Substituted 1,3-diaminopropanes

Acylated 3-amino-5-hydroxy-2, 4, 6-triiodobenzoic acid and esters and salts thereof

New p-aminophenol derivatives and their preparation process

Crystalline forms of broflanilide

The present invention relates to crystalline forms of the insecticide broflanilide (compound I), in particular to a crystalline form B, and to different processes for converting said crystalline form B into a crystalline form A or vice versa.

Method of making polymerizable liquid mixtures

ABSTRACT OF THE DISCLOSURE What is disclosed is a method for the quaternization of tertiary aminoalkyl esters or tertiary aminoalkyl amides of acrylic acid or of methacrylic acid in admixture with from 30 to 80 percent, by weight of the mixture, of acrylamide employing an alkylating agent in the absence of water to form, in high yield and in short reaction time, a mixture containing the corresponding quaternization products in the form of a fluid mixture which can be used directly for the preparation of copolymers of acrylamide.

Substituted 1,3-diaminopropanes

N min -Acyl-N-alkyl-1,3-diaminopropanes of formula R<1>CONH(CH2)3NHR<2> (where R<1> is R- or RNH where R is a substituted or unsubstituted hydrocarbon group and R<2> is alkyl) are prepared by selectively acylating N-alkyl-1,3-diaminopropanes. In the process a N-alkyl-1,3-aminopropane is reacted with an aldehyde to form a hexahydropyrimidine, the hexahydropyrimidine is acylated and the acylated hexahydropyrimidine is then hydrolysed to give the product.

2,4,6-Triiod-5-substituted-amino-isophthalate esters useful as X-ray contrast agents for medical diagnostic imaging

Improved catalysttfree manufacture of nn*tertiary aminoalkyl*acrylamide

Acidyl polyalkylene polyamines

Iodinated agents and X-ray imaging compositions containing them

Compounds having the structure         (Z)̵-COO-L-CO₂M    wherein (Z)̵-COO is the residue of an iodinated aromatic acid;    M is H, a cation, (̵CH₂CH₂O)̵ m H, and (̵CH₂CH(OH)O)̵ p H;    m is an integer from 1 to 150;    p is an integer from 1 to 50; and    L is one or more divalent linking groups selected from alkylene, cycloalkylene, arylene, arylenealkylene, and alkylenearylene are particularly useful as wetting agents in x-ray imaging compositions and in methods for x-ray diagnostic imaging.

Iodinated wetting agents

Improvements in or relating to Amino-Benzoic Acid Derivatives

1,161,287. Substituted benzoic acids. WILLIAM H. RORER Inc. 31 May, 1968, No. 26305/68. Heading C2C. Novel compounds of formula wherein R is H or -COCH 3 , are prepared by reduction of the corresponding nitro compound or benzyl ester thereof followed when R is COCH 3 by acetylation. O - [p - Nitrobenzoyl] - salicylic acid or its benzyl ester or sodium salt are prepared by reacting p-nitrobenzoyl chloride with the corresponding phenol. Pharmaceutical compositions in conventional forms for oral or parenteral administration and having anti-inflammatory and anti-pyretic activity comprise an above novel compound and a carrier therefor.

Acyl derivatives of substituted bis-arylalkylamino compounds

Compounds of the formula ##STR1## wherein Ar is phenyl or naphthyl, X is oxygen or the group ##STR2## Y is substituted or unsubstituted alkylene of 1-4 carbon atoms, R 1 is acyloxy, acyloxyalkoxy, acylamino or is --N(Alkyl)(Acyl, R 4 is hydrogen or lower alkyl, R 5 is hydrogen, lower alkyl or acyl, and R 2 , R 3 , R 6 and R 7 are the same or different and are hydrogen, halogen, hydroxy, lower alkoxy, acyloxy, amino, alkylamino, dialkylamino, acylamino, nitro, lower alkyl, lower halogeno alkyl, or lower alkylthio, Acyl in these radicals being derived from [a] saturated or unsaturated, straight, or branched, substituted or unsubstituted fatty acids of 2-10 carbon atms, [b] substituted or unsubstituted benzoic acids, [c] lower aliphatic mono esters of carbonic acid, or [d] the carbonic acid phenyl mono ester; And pharmaceutically acceptable salts of these compounds; optically active isomers thereof and diastereomers. The compounds have antiphlogistic, analgesic, antipyretic, broncholytic and coronary circulation regulatory action.

METHOD FOR THE PREPARATION OF 2 K DIACYLAMINE 3 6 DIAMINO 1 4 BENZO QUINONI

Iodized Wetting Agent

본원은 X-선 이미징 조성물내 습윤제로서 특히 유용한 하기구조식 화합물. (Z)-COO는 아이오드화 방향족산의 잔기, M은 H, 흑종의 양이온, -(CH 2 CH 2 O) m H 및 -(CH 2 CH 2 (OH)O)-pH, m은 1-150의 정수 ; p는 1-50의 정수 ; 및 L은 알킬렌, 싸이클로 알킬렌, 아릴렌, 아릴렌알킬렌, 및 알킬렌아릴렌에서 선택된 한개이상의 2가 연결기에 관한다.

Substituted 1,3-diaminopropanes

ABSTRACT SUBSTITUTED 1,3-DIAMINOPROPANES N'-Acyl-N-alkyl-1,3-diaminopropanes of formula R1CONH(CH2)3NHR2 where R1 is R- or RNH where R is a substituted or unsubstituted hydrocarbon group and R2 is alkyl) are prepared by selectively acylating N-alkyl-1,3-diaminopropanes. In the process a N-alkyl 1,3-aminopropane is reacted with an aldebyde to form a hexahydropyrimidine, the hexahydropyrimidine is acylated and the acylated hexahydropyrimidine is then hydrolysed to give the product.

Process for the preparation of amphoteric surfactants

Process for preparing aromatic amide antioxidants.

Procede de preparation d'amides aromatiques a titre d'antioxydants a partir d'un ester aliphatique ou aromatique et d'une amine primaire en presence d'un alcoxyde metallique et d'un alcool. Les produits non satures obtenus par ce procede sont suffisamment purs pour pouvoir etre utilises comme comonomeres dans la preparation des elastomeres. Process for preparing aromatic amides as antioxidants from an aliphatic or aromatic ester and from a primary amine in the presence of a metal alkoxide and an alcohol. The unsaturated products obtained by this process are sufficiently pure to be able to be used as comonomers in the preparation of elastomers.

AN IMPROVED PROCEDURE FOR THE SYNTHESIS OF ARILAMIDES AL-FA, BETA-UNSATURATED

PREPARATION OF N N DIALKYLAMIDES D MONOCARBOXYLIC ACIDS ALPHA BETA CLEFINICALLY UNSATURATED

Amidoalkylamine glyceride wax

Procedimento per la preparazione delle acril e metacril ammidi n.sostituite

塩化メタクリルアミドプロピルトリメチルアンモニウムの精製方法

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Linear and cyclic aromatic oligoamides, methods of making same and uses thereof

The present disclosure provides linear and cyclic oligoamides. The present disclosure also provides methods of making and uses of linear and cyclic oligoamides. The linear and/or cyclic oliogoamides may be used in methods such as, for example, forming transmembrane pores for transmembrane transport of hydrogen-bond acceptors and/or ions, sequestering hydrogen-bond acceptors and/or ions (e.g., anions), or the like. Compounds of the present disclosure may be used to enrich materials with ions (e.g., lithium). Compounds of the present disclosure may have the following structure: Structure (I) or Structure (II)

Ioderte benzoylacetater og -ketater

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Verfahren zur Herstellung wachsartiger Fettsaeurediamide

Joderade bensoylacetaler och -ketaler

Olive-green sulfur dye and process of making same.

Biologically active compounds

带有双端胺基的酰胺类化合物及其制备方法和应用

本申请提供一种带有双端胺基的酰胺类化合物，具有通式(I)。其中，A和B独立地选自取代或未取代的C1～C18亚烷基、C2～C18亚烯基、C2～C18亚炔基、C6～C18亚芳基、C5～C18亚杂芳基或其任意组合。本申请还提供所述酰胺类化合物的制备方法和应用。

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Verfahren zur gewinnung von reinem methacrylamidopropyltrimethylammoniumchlorid

Linear and cyclic aromatic oligoamides, methods of making same, and uses thereof

The present disclosure provides linear and cyclic oligoamides. The present disclosure also provides methods of making and uses of linear and cyclic oligoamides. The linear and/or cyclic oliogoamides may be used in methods such as, for example, forming transmembrane pores for transmembrane transport of hydrogen-bond acceptors and/or ions, sequestering hydrogen-bond acceptors and/or ions (e.g., anions), or the like. Compounds of the present disclosure may be used to enrich materials with ions (e.g., lithium). Compounds of the present disclosure may have the following structure: Structure (I) or Structure (II)

Linear and cyclic aromatic oligoamides, methods of making same, and uses thereof

The present disclosure provides linear and cyclic oligoamides. The present disclosure also provides methods of making and uses of linear and cyclic oligoamides. The linear and/or cyclic oliogoamides may be used in methods such as, for example, forming transmembrane pores for transmembrane transport of hydrogen-bond acceptors and/or ions, sequestering hydrogen-bond acceptors and/or ions (e.g., anions), or the like. Compounds of the present disclosure may be used to enrich materials with ions (e.g., lithium). Compounds of the present disclosure may have the following structure: Structure (I) or Structure (II)

Oligoamidas aromaticas lineales y ciclicas, metodos para hacer las mismas y usos de las mismas.

La presente descripción proporciona oligoamidas lineales y cíclicas. La presente descripción también presenta métodos para fabricar y usar oligoamidas lineales y cíclicas. Las oligoamidas lineales y/o cíclicas pueden usarse en nétodos tales como, por ejemplo, para formar poros transmembrana para el transporte transmembrana de aceptores y/o iones de enlaces de hidrógeno, secuestrar aceptores y/o iones de enlaces de hidrógeno (por ejemplo, aniones), o similares. Los compuestos de la presente divulgación se pueden usar para enriquecer materiales con iones (por ejemplo, litio). Los compuestos de la presente divulgación pueden tener la siguiente estructura: (Ver estructura).

Linear and cyclic aromatic oligoamides, methods of making same and uses thereof

The present disclosure provides linear and cyclic oligoamides. The present disclosure also provides methods of making and uses of linear and cyclic oligoamides. The linear and/or cyclic oliogoamides may be used in methods such as, for example, forming transmembrane pores for transmembrane transport of hydrogen-bond acceptors and/or ions, sequestering hydrogen-bond acceptors and/or ions (e.g., anions), or the like. Compounds of the present disclosure may be used to enrich materials with ions (e.g., lithium). Compounds of the present disclosure may have the following structure: Structure (I) or Structure (II)

Linear and cyclic aromatic oligoamides, methods of making same and uses thereof

The present disclosure provides linear and cyclic oligoamides. The present disclosure also provides methods of making and uses of linear and cyclic oligoamides. The linear and/or cyclic oliogoamides may be used in methods such as, for example, forming transmembrane pores for transmembrane transport of hydrogen-bond acceptors and/or ions, sequestering hydrogen-bond acceptors and/or ions (e.g., anions), or the like. Compounds of the present disclosure may be used to enrich materials with ions (e.g., lithium). Compounds of the present disclosure may have the following structure: Structure (I) or Structure (II)

Iodinated aromatic acid(z) derivatives; x-ray contrast agents and use

Iodinated benzoyl acetals and ketals and pharmaceutical compositions containing them

Iodinated benzoyl acetals and ketals process to prepare the said compounds and x-ray contrast compositions containing them

Jodatut bentsoyyliasetaalit ja -ketaalit

Iodized benzoylacetals and benzoylketals

Ioderte benzoylacetater og -ketater

Forbindelser som har strukturen: hvor (Z-)COO er resten av en lodert aromatisk syre; R er alkyl, cykloalkyl, aryl, aralkyl, ¿C¿alkyl, ¿C¿aryl, eller alkenyl; R1 er H, alkyl, cykloalkyl, aryl, aralkyl eller -(CH2- )nC02R3 R2 er H, alkyl, cykloalkyl, aryl, aralkyl, (-CH2- )nC02R4; eller en OR O l II ¿ (CH2 )p¿C¿O¿C--fZ ) gruppe , Ri hvor Z, R og R1 er som definert ovenfor: eller R1 og R2 tatt sammen med det karbonatom til hvilket de er festet representerer cykloalkyl; R3 er H, alkyl, cykloalkyl, aryl eller aralkyl; R4 er H, alkyl, cykloalkyl, aryl eller aralkyl; og m, n og p er uavhengig et helt tall fra O til 17; forutsatt at R1 og R2 ikke begge kan være H; som er nyttige i fremstillingen av røntgenkontrast- preparater for medisinsk avbildning, samt fremgangs- måter for røntgendiagnostisk avbildning.

Verfahren zur Herstellung von unsymmetrischen Methylen-bis-Methacrylsaeureamiden

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New series of organic compounds

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Linear and cyclic aromatic oligoamides, methods of making same and uses thereof

The present disclosure provides linear and cyclic oligoamides. The present disclosure also provides methods of making and uses of linear and cyclic oligoamides. The linear and/or cyclic oliogoamides may be used in methods such as, for example, forming transmembrane pores for transmembrane transport of hydrogen-bond acceptors and/or ions, sequestering hydrogen-bond acceptors and/or ions (e.g., anions), or the like. Compounds of the present disclosure may be used to enrich materials with ions (e.g., lithium). Compounds of the present disclosure may have the following structure: Structure (I) or Structure (II)

Yellow sulfur dye and process of making same.

Brown sulfur dye and process of making same.

Verfahren zur herstellung von n-(3-dimethylaminopropyl)-methacrylamid

Verfahren zur Darstellung von Fettsaeurederivaten

Olefinic aryl amide process

Manufacture of antioxidant amide

Process for the preparation of antioxidant amides

Procedimiento mejorado para la preparacion de alfa,beta aril amidas insaturadas

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Process for the preparation of antioxidant amides

Aperfeicoamento em processo para a sintese de arilmidas alfa, beta insaturadas

Olefinic aryl amide process

Verfahren zur herstellung antioxydierender amide.

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邻氨基苯甲酰胺系化合物的制造方法

本发明提供一种特定的邻氨基苯甲酰胺系化合物或其盐的制造方法。提供式(I)所示的邻氨基苯甲酰胺系化合物或其盐的制造方法，包括使式(II)所示的化合物选择性地卤化的工序， 式中、R 1a 和R 3 分别独立地为卤素或卤代烷基；R 2 为环丙基烷基或环丁基烷基；Hal为氯原子或溴原子， 式中、R 1a 、R 2 和R 3 如上所述。

Verfahren zur Herstellung von Alkylenglykol-di(-acrylamid-N-methyl)-aethern

Verfahren zur herstellung von alkylenglykol-bis eckige klammer auf (meth) acrylamidomethyl eckige klammer zu-aethern

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