8305 results about "Acyl group" patented technology

Compounds of the formulaeLAn-Z-X—WwD and BZ-X—WwDwherein: D is a drug moiety; L is a ligand; B is a blocking group; A is an optional acyl unit; Z is an amino acid or a peptide residue; X is an aminobenzyl ether self-immolative spacer group; W is an optional second self-immolative group; n is an integer of 0 or 1; and w is an integer of 0 or 1, and compositions of said compounds with pharmaceutically acceptable carrier, diluent and / or excipient, and methods of delivery the drug D via the compounds.

Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I):including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

A class of 2′-fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein[0001]Base is a purine or pyrimidine base;[0002]R1 is OH, H, OR3, N3, CN, halogen, including F, or CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy, and base refers to a purine or pyrimidine base;[0003]R2 is H, phosphate, including monophosphate, diphosphate, triphosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of providing a compound wherein R2 is H or phosphate; sulfonate ester including alkyl or arylalkyl sulfonyl including methanesulfonyl, benzyl, wherein the phenyl group is optionally substituted with one or more substituents as described in the definition of aryl given above, a lipid, an amino acid, peptide, or cholesterol; and[0004]R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of being cleaved to the parent compound, or a pharmaceutically acceptable salt thereof.

Nucleic acid compositions encoding polypeptide products with diglyceride acyltransferase activity, as well as the polypeptide products encoded thereby and methods for producing the same, are provided. The subject polypeptide and nucleic acid compositions find use in a variety of applications, including research, diagnostic, and therapeutic agent screening applications, as well as in treatment therapies and in the production of triacylglycerols.

The light emitting device of the present invention relates to a light emitting device which is characterized in that it is a device with an emissive substance present between an anode and cathode, and which emits light by means of electrical energy, and said device has a least one type of compound denoted by (a) to (d) below. (a) A compound having a plurality of 1,7-phenanthroline skeletal structures (b) A benzoquinoline derivative (c) A spiro compound represented by general formula (1) A1 and A2 are each selected from single bonds, substituted or unsubstituted alkyl chains, ether chains, thioether chains, ketone chains and substituted or unsubstituted amino chains. However, A1<> A2. Z represents carbon or silicon. R1 to R16 are each selected from hydrogen, alkyl group, cycloalkyl group, aralkyl group, alkenyl group, cycloalkenyl group, alkynyl group, hydroxyl group, mercapto group, alkoxy group, alkylthio group, aryl ether group, aryl thioether group, aryl group, heterocyclic group, halogen, haloalkane, haloalkene, haloalkyne, cyano group, aldehyde group, carbonyl group, carboxyl group, ester group, carbamoyl group, amino group, nitro group, silyl group, siloxanyl group and a cyclic structure formed with an adjacent substituent. (d) A tetraphenylmethane derivative represented by general formula (2) R17 to R36 are each selected from hydrogen, alkyl group, cycloalkyl group, aralkyl group, alkenyl group, cycloalkenyl group, alkynyl group, hydroxyl group, mercapto group, alkoxy group, alkylthio group, aryl ether group, aryl thioether group, aryl group, heterocyclic group, halogen, haloalkane, haloalkene, haloalkyne, cyano group, aldehyde group, carbonyl group, carboxyl group, ester group, carbamoyl group, amino group, nitro group, silyl group, siloxanyl group and a cyclic structure formed with an adjacent substituent. However, at least one of R17 to R36 is selected from substituents represented by general formula (3). -X-Ar (3) X is a single bond or is selected from the following, and Ar denotes a condensed aromatic ring or heteroaromatic ring. In the case where X is phosphorus oxide, then Ar represents an aromatic hydrocarbon or heteroaromatic ring. n is an natural number.

The present invention provides a novel pyrimidine compound having an excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action. More specifically, it provides a compound represented by the following formula, a salt thereof or a solvate of them. In the formula, R1 and R2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a cycloalkenyl group having three to eight carbon atoms which may be substituted, a 5 to 14-membered non-aromatic heterocyclic group which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, an acyl group having one to six carbon atoms which may be substituted or an alkylsulfonyl group having one to six carbon atoms which may be substituted; R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, a nitrogen atom which may be substituted, an oxygen atom which may be substituted or a sulfur atom which may be substituted; R4 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted or a 5 to 14-membered non-aromatic heterocyclic group having at least one or more unsaturated bonds which may be substituted; and R5 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted or a 5 to 14-membered aromatic heterocyclic group which may be substituted.

Skin care compositions containing N-acyl amino acid, particularly N-acyl derivatives of Phenylalanine or Tyrosine, their isomers, or their salts; at least one other skin care active selected from sugar amines, vitamin B3, retinoids, peptides, dialkanoyl hydroxyproline, hexamidine, salicylic acid, and phytosterol; and a dermatologically acceptable carrier for the N-acyl amino acid and the skin care active. The invention further relates to methods for regulating the condition of mammalian keratinous tissue wherein the methods each comprise the step of topically applying to the keratinous tissue of a mammal needing such treatment, a safe and effective amount of the skin care composition of the invention.

The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and / or toxic compounds and is readily amenable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug compounds and methods for synthesizing these 1-acyl-alkyl derivatives.

It is an object of the present invention to obtain a phosphorescent compound to be used for a light-emitting element, a light-emitting element that uses the phosphorescent compound and has a higher luminous efficiency, and a light-emitting device that uses the light-emitting element and has poser consumption reduced. The present invention provides an organometallic complex comprising a moiety represented by the following general formula (1). The organometallic complex is applied to a light-emitting element, and a light-emitting device reduced in power consumption is manufactured by using the light-emitting element. (where R1 to R4 are individually any one of hydrogen, a halogen atom, an acyl group, an alkyl group, an alkoxyl group, an aryl group, a cyano group, and a heterocyclic group, Ar is one of an aryl group having an electron-withdrawing group and a heterocyclic group having electron-withdrawing group, and M is one of an element of Group 9 and an element of Group 10)

The invention relates to polymers with antimicrobial properties, consisting of: a) 99-40 wt % non functional vinylically polymerizable monomers and b) 1-60 wt % functional vinylically polymerizable monomers of general formula (I) wherein V=vinyl, (meth)acroyl, allyl or styryl, A=a possibly available linking unit, which can be alkyl, aryl, arylalkyl or hydroxy alkyl, which can also be interrupted by hetero atoms, e.g. by hetero atoms in urethane, carbonate, ester, amide or ether groups, wherein y=0 or is 1, Hsp=a hydrophilic spacer of general formula (i) -(O-CH2-CH2)r- and / or (ii) -(O-CH2-CH(CH3))s with r=0-40, s=0-40 and r+s=2-40, also m=1.2 or 3 and R1=CH3, ethyl or benzyl, R2=an alkyl radical with 8-20 C-atoms, wherein t=1, 2 or 3 and X-=Cl-, Br-, I- or alkyl sulphate.

Disclosed are compounds of Formula 1,whereinR1 is halogen, C1-C2 haloalkyl or C1-C2 haloalkoxy;R2 is H, halogen or cyano;R3 is H, halogen or CF3;R4 is H, C2-C7 alkylcarbonyl or C2-C7 alkoxycarbonyl; andR5 is C1-C6 alkyl or C1-C6 haloalkyl, each substituted with one substituent independently selected from hydroxy, C1-C6 alkoxy, C1-C6 alkylthio, C1-C6 alkylsulfinyl, C1-C6 alkylsulfonyl, C2-C7 alkylaminocarbonyl, C3-C9 dialkylaminocarbonyl, C2-C7 haloalkylaminocarbonyl and C3-C9 halodialkylaminocarbonyl.Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.

The invention discloses a method for preparing bi-(sulfonyl fluoride) imine and (fluorinated alkyl sulfonyl fluorine sulfonyl) imine alkali metal salt. The method comprises the following steps of: reacting sulfamide and thionyl chloride and chlorosulfonic acid to prepare bi-(sulfonyl chlorine) imine and (fluorinated alkyl sulfonyl chlorine sulfonyl) imine, reacting with antimony trifluoride and potassium carbonate (rubidium or caesium) to obtain corresponding high-purity bi-(sulfonyl fluoride) imine potassium (rubidium or caesium) salt or (fluorinated alkyl sulfonyl fluorine sulfonyl) imine potassium (rubidium or caesium) salt, performing double decomposition exchange reaction using the potassium (rubidium or caesium) salt with the lithium perchlorate (or sodium) or lithium tetrafluoroborate (or sodium) in the aprotic polar solvent to obtain corresponding lithium (or sodium) salt with high purity. The method in the invention has the characteristics of simple operating steps, easy separation and extraction of output, high purity and yield, no environmental pollution, and the like, and is suitable for mass industrial production.

Dithioamine reducing agents useful for the reduction of disulfide bonds. The reducing agents of this invention are useful, for example, to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins and other biological molecules. Reducing agents of this invention are useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. The invention provides S-acylated dithioamines which can be selectively activated reducing agents by removal of the S-acyl groups enzymatically or chemically. The invention further provides dithiane precursors of thioamino reducing agents. The invention provides dithioamine reducing agents, S-acylated dithioamines and dithianes which are immobilized on surfaces, including among others, glass, quartz, microparticles, nanoparticles and resins.

The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl.In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat meningiomas; to treat uterine leiomyomas; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce cervical ripening; to induce labor; and for contraception.

Disclosed are novel compounds useful for prevention or control of diseases derived from fungi, a process for producing the same, and novel antifungal agents using the novel compounds. The compounds useful for prevention and treatment of diseases derived from fungi according to the present invention include novel compounds represented by formula (I). The compounds represented by formula (I) have potent antifungal activity against diseases derived from fungi, and do not have phytotoxicity to mammals and agricultural and garden plants, from which diseases should be eliminated, and, even when applied to agricultural and garden plants, have high photostability.whereinR1 represents isobutyryl, tigloyl, isovaleryl, or 2-methylbutanoyl;R2 represents a hydrogen atom, an aromatic carboxylic acid residue, or a protective group of amino; and R3 represents a hydrogen atom, nitro, amino, acylamino, or N,N-dialkylamino, excluding the case where, when R1 represents isobutyryl, tigloyl, isovaleryl, or 2-methylbutanoyl with R3 representing a hydrogen atom, R2 represents a 3-hydroxypicolinic acid residue, 3-hydroxy-4-methoxypicolinic acid residue, or a 3,4-dimethoxypicolinic acid residue.

This invention discloses a fluorine-containing polymer and its application as ion exchange fiber material. The fluorine-containing polymer is a perfluoro resin containing sulfonylfluoride groups, and is shown in formula 1. The fluorine-containing polymer has ion exchange function, and is prepared by free radical copolymerization of perfluorosulfonyl vinyl ether, tetrafluoroethylene and hexafluoropropylene in the presence of dispersant, solvent and initiator. The dispersant / solvent is mixed solution of melamine derivative containing linear perfluoro hydrocarbon and water. The fluorine-containing polymer can be melt-spun into polymer fibers, which can be woven into fiber network that can be used as the reinforcing network material for ion exchange membranes and chlor-alkali ion membrane to reinforce and improve the ion exchange ability.

Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I):wherein: R1 is hydrogen, cyano, halogen, R8, formyl, —C(O)R8, —C(O)OR8, —C(O)NR9R10, or —C(S)NH2; R2 is R8 or —S(O)mR11; R3 is methyl, ethyl or C1-C4 haloalkyl; R4, R5 and R7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R12, —S(O)nR12 or SF5; Z is a nitrogen atom or C—R13; R8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R9 is hydrogen, alkyl, haloalkyl or alkoxy; R10 is hydrogen, alkyl, haloalkyl or alkoxy; R11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R12 is alkyl or haloalkyl; R13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.

The present invention discloses one kind of medicine precursors containing long chain fatty acyl group substituted venlafaxine in the structure as shown in general expression I and its medicinal salt and hydrate. The present invention also discloses the preparation process of the medicine precursors and their application in preventing and treating diseases of central nerve system. The medicine precursors of the present invention has half life near or over 10 hr, and compared with venlafaxine, they has excellent long-acting effect.

The present invention provides a compound of the formula:wherein Ar represents an aromatic group which may be substituted;X represents methylene, S, SO, SO2 or CO;Y represents a spacer having a main chain of 2 to 5 atoms;n represents an integer of 1 to 5;i) R1 and R2 each represents a hydrogen atom or a lower alkyl which may be substituted,ii) R1 and R2 form, taken together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring which may be substituted, oriii) R1 or R2 together with -(CH2)n-N= form, bonded to a component atom of Ring B, a spiro-ring which may be substituted;Ring A represents an aromatic ring which may be substituted;Ring B represents a 4- to 7-membered nitrogen-containing non-aromatic ring which may be further substituted by alkyl or acyl,with a proviso that X represents S, SO, SO2 or CO when Ring A has as a substituent a group represented by the formula:where R11 represents alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or a group represented by the formula:where R12 represents alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or a salt thereof; which has an excellent somatostatin receptor binding inhibition action.

A polymerizable composition contains (A) a polymerization initiator that is an acetophenone-based compound or an acylphosphine oxide-based compound, (B) a polymerizable compound, (C) at least either a tungsten compound or a metal boride, and (D) an alkali-soluble binder.

The present invention relates to a series of prodrugs of inhibitors of DP-IV with improved properties. The compounds can be used for the treatment of a number of human diseases, including impaired glucose tolerance and type II diabetes. The compounds of the invention are described by general formula (1); wherein R1 is H or CN; R2 is selected from CH2R5, CH2CH2R5 and C(R3)(R4)—X2—(CH2)aR5; R3 and R4 are each independently selected from H and Me; R5 is selected from CON(R6)(R7), N(R8)C(=0)R9, N(R8)C(═S)R9, N(R8)SO2R10 and N(R8)R10; R6 and R7 are each independently R11(CH2)b or together they are —(CH2)2-Z-(CH2)2— or CH2-o-C6H4-Z-CH2—; R8 is H or Me; R9 is selected from R11(CH2)b, R11(CH2)bO and N(R6)(R7); R10 is R11(CH2)b; R11 is selected from H, alkyl, optionally substituted aryl, optionally substituted aroyl, optionally substituted arylsulphonyl and optionally substituted heteroaryl; R12 is selected from H2NCH(R13)CO, H2NCH(R14)CONHCH(R15)CO, C(R16)═C(R17)COR18 and R19OCO; R13, R14 and R15 are selected from the side chains of the proteinaceous amino acids; R16 is selected from H, lower alkyl (C1-C6) and phenyl; R17 is selected from H and lower alkyl (C1-C6); R18 is selected from H, lower alkyl (C1-C6), OH, O-(lower alkyl (C1-C6)) and phenyl; R19 is selected from lower alkyl (C1-C6), optionally substituted phenyl and R20C(=0)OC(R21)(R22); R20, R21 and R22 are each independently selected from H and lower alkyl (C1-C6); Z is selected from a covalent bond, —(CH2)c—, —O—, —SOd— and —N(R10)—; X1 is S or CH2; X2 is O, S or CH2; a is 1, 2 or 3; b is 0-3; c is 1 or 2; and d is 0, 1 or 2.

The present invention provides an azolylacylquanidine compound of formula I The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.

Cosmetic compositions containing a micronized metal oxide along with a 4-substituted resorcinol derivatives of the general formula I exhibit improved storage stability: where each R1 and R2, independently, represents a hydrogen atom, —CO—R (acyl group), —COO—R, CONHR; where R represents saturated or unsaturated, linear, branched or cyclic C1-C18 hydrocarbon groups; andR3 represents (1) an alkyl group, having from 1 to 18 carbon atoms, preferably having from 2 to 12 carbon atoms, with or without substitution of one or more hydrogen atoms of a linear alkyl group with a methyl or ethyl group; e.g., R3 constitutes linear or branched chain alkyls, or (2) a group of the general formula formula (II) Where X is preferably H, n is 0 to 3 and the dashed lines represents an optional double bond.

An object of the present invention is to provide a metal oxide particle which exercises more excellent ultraviolet absorbency as a matter of course and combines therewith merits of, for example, either being shifted in ultraviolet absorption edge toward the longer wavelength side and being excellent also in the absorption efficiency of a long-wavelength range of ultraviolet rays, or having good transparency and, for example, even in cases where added into or coated onto substrates, not damaging the transparency or hue of the substrates. As a means of achieving this object, a metal oxide particle according to the present invention is a metal oxide particle such that a hetero-element is contained in a particle comprising an oxide of a specific metal element (M), wherein the metal oxide particle is: 1) a metal oxide particle in the form of a fine particle wherein the hetero-element is at least one specific metal element (M′); 2) a metal oxide particle wherein the hetero-element includes at least two specific metal elements (M′); 3) a metal oxide particle wherein: the hetero-element is a more specified metal element (M′) and at least a part thereof is 2 in valence; or the metal element (M) is a more specified metal element and the metal oxide particle is in a specific range in crystal grain diameter in the vertical direction to each of the (002) plane and the (100) plane; or 4) a metal oxide particle wherein: the hetero-element is at least one specific nonmetal element and an acyl group is contained in the particle; or the hetero-element includes at least two specific nonmetal elements; or the hetero-element is at least one specific nonmetal element and a component derived from a metal element (M′) other than the metal element (M) is contained in the particle.

The present invention provides a medicinal composition having an excellent antitumor activity. That is, it provides a medicinal composition comprising a sulfonamide compound, a sulfonate compound or a salt of them, which is represented by the following formula: (wherein ring A represents an aromatic ring which may have a substituent group; ring B represents a 6-membered unsaturated hydrocarbon ring which may have a substituent group etc.; ring C represents a 5-membered hetero-ring containing one or two nitrogen atoms, and the ring C may have a substituent group; W represents a single bond or -CH=CH-; X represents -NH- etc.; and Y represents a carbon atom or a nitrogen atom; and Z represents -NH- etc.), particularly N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide or a salt thereof, combined with at least one substance selected from (1) irinotecan hydrochloride trihydrate; (2) mitomycin C; (3) 5-fluorouracil; (4) cisplatin; (5) gemcitabine hydrochloride; (6) doxorubicin; (7) taxol; (8) carboplatin; (9) oxaliplatin; (10) capecitabine; and (11) a salt of the above-mentioned (1) to (10).