2407 results about "Lactam" patented technology

Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming lactam bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, substitution of carboxy terminal amino acids, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (K-RNRNNIA) and SEQ ID NO: 28 (KRNR).

A polyamide molding composition with the following constitution is described:

• • (A) from 30 to 100% by weight of at least one 10T/6T copolyamide, where this is composed of
    • (A1) from 40 to 95 mol % of 10T units, formed from the monomers 1,10-decanediamine and terephthalic acid
    • (A2) from 5 to 60 mol % of 6T units, formed from the monomers 1,6-hexanediamine and terephthalic acid
  • (B) from 0 to 70% by weight of reinforcing materials and/or fillers
  • (C) from 0 to 50% by weight of additives and/or further polymers

where the entirety of components A to C is 100%, with the proviso that in component (A) up to 30 mol %, based on the entirety of the dicarboxylic acids, of the terephthalic acid can have been replaced by other aromatic, aliphatic, or cycloaliphatic dicarboxylic acids, and with the proviso that in component (A) up to 30 mol % of 1,10-decanediamine and respectively 1,6-hexanediamine, based on the entirety of the diamines, can have been replaced by other diamines, and with the proviso that not more than 30 mol % in component (A), based on the entirety of the monomers, can have been formed via lactams or amino acids. Uses of this polyamide molding composition are moreover described, as also are processes for the preparation of these polyamide molding compositions.

The invention provides compounds of formula (1),

and the pharmaceutically acceptable salt thereof, wherein R¹, n and R² are as described herein; compositions thereof; and uses thereof.

A compound of formula (I):

The invention discloses a novel-structured 1-substituent pyridyl-lactam pyrazole compound, with the structure shown in the general formula I; the definitions of each substituent group are stated in the instruction book. The compound in the general formula I is provided with excellent insecticidal and sterilizing activity and can be used to control pests and diseases. The technical proposal of the invention also comprises an intermediate for preparing the compound in the general formula I; the structure of the intermediate is shown in the general formula IV, and the definitions of each substituent group in the formula IV are stated in the instruction book.

The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.

The present invention provides a hydrogel composition capable of preventing the intrusion of micro-organisms into body cavities or body openings of mammals comprising of a poly(N-vinyl lactam), a polysaccharide and water.

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

A polyamide molding composition which can be used for production of a printable or printed item contains a) at most 90 parts by weight of a polyamide obtained from a lactam or from an amino carboxylic acid having at least 10 carbon atoms; and b) from 10 to 100 parts by weight of PA1010, wherein a total of components a) and b) is 100 parts by weight.

There is disclosed hydrogel compositions comprising a combination of at least two of three components selected from non-acidic poly (N-vinyl lactam), chitosan derivatives and water-soluble multifunctional amine-containing polymers in various ratios. The hydrogels are useful as cavity-filling wound dressings, burn dressings, drug delivery systems, cosmetic masks, conductive electrodes, prostheses and wraps.

An antimicrobial composition comprising (a) a cationic surfactant derived from the condensation of fatty acids and esterified dibasic amino acids, such as lauric arginate and (b) an antibiotic, such as of β-lactam antibiotics, polypeptides, quinolones. The composition may be used as a stand alone antimicrobial formulation, or in combination with medical articles or medical devices.

The present invention provides compositions, therapeutic combinations and methods including: (a) at least one selective CB₁ antagonist; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity, metabolic syndrome and lowering plasma levels of sterols or 5α-stanols.

The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.

Transparent polyamide molding materials are provided which are characterized in that they have a melting enthalpy between 0 and 12 J/g and the polyamides are constituted of

100 mole-% of a diamine mixture having 10-70 mole-% of PACM [bis-(4-amino-cyclohexyl)-methane] with less than 50 wt.-% of trans,trans-isomer and 90-30 mole-% of MACM [bis-(4-amino-3-methyl-cyclohexyl)-methane], wherein, optionally, 0-10 mole-% can be replaced by other aliphatic diamines having 6 to 12 C atoms, cycloaliphatic, alkyl-substituted cycloaliphatic, branched aliphatic diamines or multiamines having 3 to 12 amino groups or mixtures thereof, and

100 mole-% of long-chain aliphatic dicarboxylic acids having 8 to 14 C atoms or mixtures of these dicarboxylic acids, wherein 0-10 mole-% can be replaced by other aromatic or cycloaliphatic dicarboxylic acids having 8 to 16 C atoms, which are especially selected from the group consisting of isophthalic acid, terephthalic acid, naphthalenedicarboxylic acid, cyclohexanedicarboxylic acid or mixtures thereof, and

wherein, optionally, 0-10 mole-% of the other long-chain aliphatic diamines and 0-10 mole-% of the other long-chain aliphatic dicarboxylic acids can be added as 0-20 mole-% of ω-aminocarboxylic acids having 6 to 12 C atoms or lactams having 6 to 12 C atoms.

Further, methods for producing the polyamide moulding materials and methods for producing and further treating moulded articles from the polyamide moulding materials are provided. Especially, the present invention relates to glasses and lenses which are obtainable from the polyamide moulding materials.

Acrylate copolymer pressure-sensitive adhesive constructions are described which provide excellent retention of rivet properties. Tenting around rivets is minimized even after undergoing thermal aging while in contact with additive rich films like PVC. This is achieved by the inclusion of a synergistic amount of an N-vinyl lactam monomer and acid monomer with the bulk of the monomers being an alkyl acrylate save and/or methacrylate esters. A concomitant increase in cohesive strength is also achieved which affords good removal characteristics. The use of appropriate adhesive blends is further disclosed which allows retention of these features while also improving cold temperature properties.

Provided are an optically-active diazabicyclooctane derivative represented by a formula (F) that is useful as a medicinal intermediate of a ss-lactamase inhibitor, and a method for manufacturing the same. In the formula (F), R1 represents CO2R, CO2M, or CONH2; R represents a methyl group, a tert-butyl group, an allyl group, a benzyl group, or a 2,5-dioxopyrrolidine-1-yl group; M represents a hydrogen atom, an inorganic cation, or an organic cation; and R2 represents a benzyl group or an allyl group.

The invention relates to a method of modulating poly(ADP-ribose)polymerase-1 (PARP-1) activity in a mammal comprising administering to a mammal an effective amount of an organic aromatic compound having from 4 to about 35 carbon atoms, wherein said organic aromatic compound is capable of binding the arginine-34 moiety located in Zinc finger-1 of the PARP-1 enzyme and wherein said organic aromatic compound has electron donating capabilities such that it's π-electron system will interact with the positively charged (cationic) guanidinium moiety of the specific arginine-34 residue of the Zinc-1 finger of PARP-1 and does not contain benzamide or lactam substituents. In particular, substituted benzopyrones and substituted indoles and their pharmaceutical compositions containing such compounds that modulate the activity of PARP-1, are described. The invention is also directed to the composition of matter, kits and methods for their therapeutic and/or prophylactic use in treating diseases and disorders described herein, by administering effective amounts of such compounds. Preferably, the compositions and methods provided herein inhibit PARP activity.

The invention discloses a method for synthesizing cabazitaxel, and belongs to the field of medicine synthesis. In the method, oppolzer reagent is used as a chiral source, and (3R,4S)-beta-lactam with optical purity ee of 98 percent is obtained by five steps. Under the action of a proper alkali, hydroxyls on C-7 and C-10 in 10-baccatine III are methylated selectively to form 7,10-dimethoxy-10-baccatine III in one step. Then beta-lactam is used to esterify the 7,10-dimethoxy-10-baccatine III under an alkaline condition, and then cabazitaxel with a purity of 99 percent can be obtained by a step of removing protective groups. In the synthesis method, the steps are short and the conditions are mild.

The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I)

wherein R_a and R_b each denote a C1-6 alkyl group or the like; X_a denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.

A polyamide moulding composition with the following constitution is described:

• (a) from 40 to 90% by weight of a copolyamide, where this is composed of
• (a1) 1,6-hexanediamine and 1,10-decanediamine and also
• (a2) terephthalic acid and at least one other polyamide-forming monomer selected from the group of: dicarboxylic acid having from 8 to 18 carbon atoms, laurolactam, aminolauric acid, and/or mixtures thereof;
• (b) from 10 to 40% by weight of macromolecular plasticizers, with the proviso that these can have been replaced to some extent by low-molecular-weight plasticizers;
• (c) from 0 to 20% by weight of additives and/or added substances.

Uses of this type of moulding composition are also described, in particular for the production of a fuel line, cooling line, oil line or urea line for the automobile sector, as also are production processes to give mouldings.

An epoxy composition for applications such as one-part adhesives, coatings, prepreg and molding compounds that includes leuco dyes, particularly those comprising a N,N-dialkylamino-, N,N-diarylamino-, or cycloalkylamino-functional group on one of the aromatic rings, as a co-catalyst or co-curing agent. The use of the leuco dye co-catalyst provides improved curing speed of the epoxy composition comprising a latent curing agent/catalyst such as Novacure imidazole microcapsules while maintaining the shelf-life stability. The epoxy may also include a secondary co-catalyst that includes amides and lactams, particularly those comprising a N,N-dialkylamino-, N,N-diarylamino-, or dicycloalkylamino-functional group. Secondary cocatalysts of low mobility at the storage conditions, such as those with a long chain substitutent, dimeric or oligomeric amides or lactams, are particularly preferred. The improved epoxy composition is implemented as adhesives for manufacturing an anisotropic conductive film (ACF) and also for connecting, encapsulating, or packaging of electronic devices.

The invention relates to a method for producing a composite material (33) consisting of reinforcing elements (29) and a thermoplastic polyamide, said method permitting high-speed production with continuous process control, using simple equipment. The method is characterized by the following steps: the supplied reinforcing elements (29) are impregnated with a lactam melt (11) that is activated for anionic polymerization, at a temperature at which the activated lactam melt (11) does not polymerize; the impregnated reinforcing element (30) is heated and polymerized in a heating unit (17) without passing through a heated die and in an essentially contactless manner; the resultant hot polymerized composite material (31) is cooled in a cooling unit (18). The lactam melt (11) that is activated for anionic polymerization is produced by first melting the lactam or more precisely the mixture of lactams to obtain a monomer melt (3) and a liquid initiator (6) is added to the monomer melt (3) immediately prior to the impregnation process of the reinforcing element (29), said liquid initiator (6) containing simultaneously the activator and the catalyst function in solute form.