5230 results about "Benzyl group" patented technology

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.

Compounds of formula 1 are modulators of P2X3 useful for the treatment of pain and genito-urinary, gastrointestinal, and respiratory disorders:

wherein

• • R¹ is —C(═S)CH₃, pyridyl, pyrimidinyl, pyrazinyl, thiazolyl, furyl, furylcarbonyl, acetyl, or carbamoyl; R^2a and R^2b are independently H, methyl, or ethyl; R³ is H or methyl; Y is a bond, —(CR⁴R⁵)_n— or —CR⁴═CR⁵—; wherein R⁴ and R⁵ are each independently H or methyl and n is 1 or 2; X is N or CH; A is phenyl, 5-membered heterocyclyl, or 6-membered heterocyclyl; R⁶, R⁷ and R⁸ are each independently H, halo, lower alkyl, cycloalkyl, alkylthio, alkylthio-lower alkyl, alkylsulfonyl-lower alkyl, di(lower alkyl)amino-lower alkyl, morpholinyl-lower alkyl, 4-methyl-piperazinyl-methyl, trifluoromethyl, pyridyl, tetrazolyl, thiophenyl, phenyl, biphenyl, or benzyl (where thiophenyl, phenyl and benzyl are substituted with 0-3 lower alkyl, halo, sulfonamido, trifluoromethyl, lower alkoxy or lower alkylthio) or R⁶ and R⁷ together form a 5-membered or 6-membered carbocyclic or heterocyclic ring substituted with 0-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, oxo, halo, thiophenyl-lower alkyl, phenyl, benzyl (where phenyl and benzyl are substituted with 0-3 lower alkyl, halo, sulfonamido, trifluoro-methyl, lower alkoxy, lower alkylthio, amino-lower alkyl, lower alkylamino-lower alkyl, or di(lower alkyl)amino-lower alkyl); and pharmaceutically acceptable salts thereof; wherein when R¹ is pyrimidin-2-yl, X is N, Y is a bond and A is oxazol-5-yl the carbon atom at position 4 in said oxazol-5-yl is not substituted by propyl when the carbon atom at position 2 in said oxazol-5-yl is substituted by substituted phenyl and the carbon atom at position 4 in said oxazol-5-yl is not substituted by phenyl when the carbon atom at position 2 is substituted by unsubstituted or substituted phenyl.

The invention relates to a crystalline form of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.

Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from:

or the diamines and diisocyanates thereof, wherein each X represents a member independently selected from —CH₂COO— (glycolic acid moiety), —CH(CH₃)COO— (lactic acid moiety), —CH₂CH₂OCH₂COO— (dioxanone), —CH₂CH₂CH₂CH₂CH₂COO— (caprolactone moiety), —(CH₂)_yCOO— where y is one of the numbers 2, 3, 4 or 6-24 inclusive, and —(CH₂CH₂O)_z′CH₂COO— where z′ is an integer between 2 and 24, inclusive; each Y represents a member independently selected from —COCH₂O— (glycolic ester moiety), —COCH(CH₃)O— (lactic ester moiety), —COCH₂OCH₂CH₂O— (dioxanone ester), —COCH₂CH₂CH₂CH₂CH₂O— (caprolactone ester), —CO(CH₂)_mO— where m is an integer between 2, 3, 4 or 6-24 inclusive, —COCH₂O(CH₂CH₂O)_n— where n is an integer between 2 and 24, inclusive; R′ is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; p is an integer between 1 and 4, inclusive; and Rn represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid and —NO₂, which is attached directly to an aromatic ring or attached through an aliphatic chain. Absorbable polymers prepared from these compounds are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention and other implantable medical devices.

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.

Compounds which are 1-(2'-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2,3 and 4); X is selected from aminoacyl groups corresponding to the natural amino acids, acyl groups R3CO, groups R4COOC(R5)(R6)OCO, methoxycarbonyl, ethoxycarbonyl and benzyloxycarbonyl; R1 is selected from H, C1-C6 alkyl residues, (CH2)aNHW1, (CH2)bCOW2, (CH2)cOW3, CH(Me)OW4, (CH2)d-C6H4-W5 and (CH2)eSW6, where a is 2-5, b is 1-4, c is 1-2, d is 1-2, e is 1-3, W1 is COW6, CO2W6 or SO2W6, W2 is OH, NH2, OW6 or NHW6, W3 is H or W6, W4 is H or W6, W5 is H, OH or OMe, and W6 is C1-C6 alkyl, optionally substituted phenyl, optionally substituted heteroaryl or benzyl and R2 is selected from H and (CH2)n-C5H3N-Y, where n is 2-4 and Y is H, F, Cl, NO2 or CN, or R1 and R2 together are -(CH2)p-where p is 3 or 4; R3 is selected from H, C1-C6 alkyl and phenyl; R4 is selected from H, C1-C6 alkyl, benzyl and optionally substitued phenyl; R5 and R6 are each independently selected from H and C<highlight>

The invention relates to crystalline forms of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((R)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.

The hair treatment composition contains preferably from 0.01 to 20 percent by weight of at least one N-hydroxyalkyl-O-benzyl chitosan and from 0.01 to 20 percent by weight of at least one other hair treatment effective ingredient. The at least one N-hydroxyalkyl-O-benzyl chitosan has at least one hydroxylalkyl group, preferably a hydroxyethyl, hydroxypropyl or hydroxybutyl group, and has from 2 to 20 carbon atoms. Various methods of treating hair with hair treatment compositions containing one or more of the N-hydroxyalkyl-O-benzyl chitosans are described.

Nitric oxide releasing oxindole prodrugs are described which are useful in methods of treating or preventing pain, inflammation, fever, or gastrointestinal lesions in a patient in need of such treatment, or of modifying an inflammatory disease or condition by favorably affecting the outcome thereof in said patient, wherein there is administered to said patient a therapeutically effective amount of a compound of Formula (I): and pharmaceutically acceptable salts thereof. In preferred embodiments, X is a covalent bond; RA and RB are both hydrogen; n is the integer 4; Y is -O-; Z is -NO2; RC is a member selected from the group consisting essentially of 5-Cl and 5-F; RD is a member selected from the group consisting essentially of 6-Cl and 6-F; and RE is a member selected from the group consisting essentially of benzyl, 2-furyl, 2-thienyl, 5-chloro-2-thienyl and 5-trifluoromethyl-2-thienyl.

Crystalline molecular sieves are prepared using a mixture comprising an organic structure directing agent capable of forming the molecular-sieve and an N,N,N-trialkyl benzyl quaternary ammonium cation.

A non-aqueous electrolyte for use in an electrochemical cell comprising: (a) at least one organic solvent; (b) at least one electrolytically active salt represented by the formula:in which: M' is selected from a group consisting of magnesium, calcium, aluminum, lithium and sodium; Z is selected from a group consisting of aluminum, boron, phosphorus, antimony and arsenic; R represents radical selected from the following groups: alkyl, alkenyl, aryl, phenyl, benzyl, and amido; X is a halogen (I, Br, Cl, F); m=1-3; and n=0-5 and q=6 in the case of Z=phosphorus, antimony and arsenic, and n=0-3 and q=4 in the case of Z=aluminum and boron. Rechargeable, high energy density electrochemical cells containing an intercalation cathode, a metal anode, and an electrolyte of the above-described type are also disclosed.

Aqueous heavy duty liquid laundry detergent compositions useful for laundering fabrics and providing cleaning and softening benefits. Such detergent compositions contain at least 5%, by weight of the composition, of a surfactant component; from about 0.1% to about 10% of a quaternary ammonium fabric-softening agent having the formula

wherein R₁ and R₂ are individually selected from the group consisting of C₁-C₄ alkyl, C₁-C₄ hydroxy alkyl, benzyl, and —(C₂H₄O)_xH where x has a value from about 2 to about 5; X is an anion; and (1) R₃ and R₄ are each a C₈-C₁₄ alkyl or (2) R₃ is a C₈-C₂₂ alkyl and R₄ is selected from the group consisting of C₁-C₁₀ alkyl, C₁-C₁₀ hydroxy alkyl, benzyl, and —(C₂H₄O)_xH where x has a value from about 2 to about 5; and such compositions contain less than 10 ppm of trimethylamine and dimethylamine impurities.

The present invention relates to a catalyst composition for ethylene oligomerization and the use thereof. Such catalyst composition includes chromium compound, ligand containing P and N, activator and accelerator; wherein the chromium compound is selected from the group consisting of acetyl acetone chromium, THF-chromium chloride and/or Cr(2-ethylhecanoate)₃; general formula of the ligand containing P and N is shown as:

in which R₁, R₂, R₃ and R₄ are phenyl, benzyl, or naphthyl. R₅ is isopropyl, butyl, cyclopropyl, cyclopentyl, cyclohexyl or fluorenyl; the activatior is methyl aluminoxane, ethyl aluminoxane, propyl aluminoxane and/or butyl aluminoxane; general formula of the accelerator is X₁R₆X₂, in which X₁ and X₂ are F, Cl, Br, I or alkoxyl, R₆ is alkyl or aryl; the molar ratio of a, b, c and d is 1:0.5˜10:50˜3000:0.5˜10. After mixing the four components mentioned previously under nitrogen atmosphere for 10 minutes, they are incorporated to the reactor, or these four components are incorporated directly into the reactor. Then ethylene is introduced for oligomerization. Such catalyst can be used in producing 1-octene through ethylene oligomerization. It is advantageous in high catalysing activity, high 1-octene selectivity, etc. The catalytic activity is more than 1.0×10⁶ g product·mol⁻¹ Cr ·h⁻¹, the fraction of C₈ linear α-olefin is more than 70% by mass.

Personal care composition comprising from about 0.05% to about 5% of at least one aquaporin-stimulating compound selected from the group consisting of xanthine, caffeine; 2-amino-6-methyl-mercaptopurine; 1-methyl xanthine; 2-aminopurine; theophylline; theobromine; adenine; adenosine; kinetin; p-chlorophenoxyacetic acid; 2,4-dichlorophenoxyacetic acid; indole-3-butyric acid; indole-3-acetic acid methyl ester; beta-naphthoxyacetic acid; 2,3,5-triiodobenzoic acid; adenine hemisulfate; n-benzyl-9-(2-tetrahydropyranyl)adenine; 1,3-diphenylurea; 1-phenyl-3-(1,2,3-thiadiazol-5-yl)urea; zeatin; indole-3-acetic acid; 6-benzylaminopurine; alpha-napthaleneacetic acid; 6-2-furoylaminopurine; green tea extract; white tea extract; menthol; tea tree oil; ginsenoside-RB1; ginsenoside-RB3; ginsenoside-RC; ginsenoside-RD; ginsenoside-RE; ginsenoside-RG1; ginseng root extract; ginseng flower extract; pomegranate extract, extracts from Ajuga turkestanica; extracts from viola tricolor and combinations thereof; an additional ingredient selected from the group consisting of niacinamide, glycerin and mixtures thereof, and a dermatologically-acceptable carrier.

The present invention relates to processes for preparing a glucopyranosyl-substituted benzyl-benzene derivative of general formula III,

wherein R¹ is defined according to claim 1.

Provided herein is a poly(ester amide) (PEA) polymer blend and a polymeric coating containing the PEA polymer blend. The PEA polymer blend has a T_g above the T_g of poly(ester amide benzyl ester) (PEA-Bz) or the T_g of poly(ester amide TEMPO). The PEA polymer blend can form a coating on an implantable device, one example of which is a stent. The coating can optionally include a biobeneficial material and/or optionally with a bioactive agent. The implantable device can be used to treat or prevent a disorder such as one of atherosclerosis, thrombosis, restenosis, hemorrhage, vascular dissection or perforation, vascular aneurysm, vulnerable plaque, chronic total occlusion, claudication, anastomotic proliferation for vein and artificial grafts, bile duct obstruction, ureter obstruction, tumor obstruction, and combinations thereof.

The invention describes a phosphate structure containing substituted benzyl, wherein the phosphate structure is shown as a formula (I) and a formula (II). The phosphate structure can be used as prodrugs for various nucleoside analogues including non-cyclic nucleoside, carbon-cyclic nucleoside, furan-cyclic nucleoside and the like, and enhance bioactivity of nucleoside compounds, and thus the structure can be applied in treatment for virus infections and cancers.

A composition comprising: (a) polyethylene; (b) as a scorch inhibitor, [1,3,5-tris(4-tert-butyl-3-hydroxy-2,6-dimethylbenzyl)-1,3,5-triazine-2,4,6-(1H,3H,5H)-trione]; (c) a thioester; (d) a hindered amine stabilizer; and (e) an organic peroxide.